BENZAMIDE DERIVATIVES AND THEIR USE AS VASOPRESSIN ANTAGONISTS

Abstract: This invention relates to new benzamide derivatives having a vasopressin antagonistic activity, etc., and represented by general formula (I), wherein R<1> is aryl optionally substituted with lower alkoxy, etc., R<2> is lower alkyl, etc., R<3> is hydrogen, etc., R<4> is lower alkoxy, etc., R<5> is hydrogen, etc., A is NH, etc., E is (a), etc., X is -CH=CH-, -CH=N-, or S, and Y is CH or N, and pharmaceutically acceptable salts thereof, to processes for preparation thereof and to a pharmaceutical composition comprising the same.

Description: DESCRIPTION BENZAMIDE DERIVATIVES AND THEIR USE AS VASOPRESSIN ANTAGONISTS TECHNICAL FIELD This invention relates to new benzamide derivatives and pharmaceutically acceptable salts thereof which are useful as a medicament. BACKGROUND ART Some benzamide derivatives have been known as vasopressin antagonist, for example, in PCT International Publication Nos. WO 91/05549 and WO 95/29152, and EP Application Publication No. 0620216. DISCLOSURE OF INVENTION This invention relates to new benzamide derivatives artti pharmaceutically acceptable salts thereof. More particularly, it relates to new benzamide derivatives and pharmaceutically acceptable salts thereof which possess activities as vasopressin antagonistic activity, vasodilating activity, hypotensive activity, activity for inhibiting saccharide release in liver, activity for inhibiting growth of mesangiu cells, water diuretic activity, platelet agglutination inhibitory activity, oxytocin antagonistic activity and the like, to a pharmaceutical composition comprising the same and to a method for the treatment and/or prevention of hypertension, heart failure, renal insufficiency, edema, ascites, vasopressin parasecretion syndrome, hepatocirrhosis, hyponatremia, hypokalemia, diabetic, circulation disorder, cerebrovascular disease (e.g. cerebral edema, cerebral infarction, etc.), Meniere's syndrome (e.g. Meniere's disease, etc.), motion sickness and the like in human beings or animals. One object of this invention is to provide new and useful benzamide derivatives which possess aforesaid activities. Another object of this invention is to provide processe for the preparation of said benzamide derivatives and salts thereof. A further object of this invention is to provide a pharmaceutical composition comprising, as an active ingredient, said benzamide derivatives and pharmaceutically acceptable salts thereof. Still further object of this invention is to provide a therapeutical method for the treatment and/or prevention of aforesaid diseases in human beings or animals, using said benzamide derivatives and pharmaceutically acceptable salts thereof. The object benzamide derivatives of this invention are new and can be represented by the following general formula (I) : wherein R 1 is aryl, cyclo(lower)alkyl or a heterocyclic group, each of which may be substituted with substituent(s) selected from the group consisting of halogen; hydroxy; nitro; amino; acyl; -substituted acyl; acyl (lower)alkylsulfinyl; acyl(lower)alkylsulfonyl; acyloxy; lower alkylamino(lower)alkylcarbamoyloxy; aryl; cyano; a heterocyclic group; lower alkenyl optionally substituted with acyl, substituted acyl, aryl or acyl-substituted aryl; lower alkynyl optionally substituted with amino, acylamino or substituted acylamino; lower alkyl optionally substituted with halogen, amino, lower alkylamino, acylamino, substituted acylamino, hydroxy, acyloxy, acyl (lower)alkanoyloxy, acyl, substituted acyl, acyl (lower)alkoxyimino, aryl or acyl-substituted aryl; lower alkylthio optionally substituted with acyl or substituted acyl; alkoxy optionally substituted with aryl, substituted aryl, hydroxy, acyloxy, amino, lower alkylamino, protected amino, a heterocyclic group, acyl- substituted pyridyl, substituted acyl-substituted pyridyl, halogen, acyl(lower)alkylamino, N-protected- acyl (lower)alkylamino, N-acyl (lower)alkyl-N-lower alkylamino, acyl, substituted acyl, acylamino, substituted acylamino, lower alkylhydrazinocarbonylamino, hydroxyimino, acyl (lower)alkoxyimino, substituted acyl (lower)alkoxyimino, acyl (lower)alkoxy, guanidino or N-protected guanidino; and lower alkenyloxy optionally substituted with acyl or substituted acyl; R 2 is hydrogen; lower alkyl optionally substituted with hydroxy, aryl or acyl; or cyclo(lower)alkyl; R 3 is hydrogen; halogen; hydroxy; acyloxy; substituted acyloxy; lower alkyl optionally substituted with hydroxy or lower alkoxy; lower alkoxy optionally substituted with aryl, amino, protected amino, acyl, hydroxy, cyano or lower alkylthio; nitro; amino; acyl; substituted acyl; or cyclo(lower)alkyloxy; R 4 is hydroxy; halogen; nitro; amino; protected amino; lower alkylamino; acyloxy; amino(lower)alkylamino; N-protected amino(lower)alkylamino; lower alkoxy optionally substituted with hydroxy, aryl, substituted aryl, acyl, substituted acyl, amino, lower alkylamino, acylamino, substituted acylamino, protected amino, a heterocyclic group or guanidino; lower alkylthio optionally substituted with acyl, substituted acyl, amino, lower alkylamino, acylamino, substituted acylamino, protected amino, a heterocyclic group, hydroxy, lower alkylsulfonyloxy, arylsulfonyloxy, ar(lower)alkoxy or substituted ar(lower)alkoxy; lower alkyl substituted with acyl, substituted acyl, amino, lower alkylamino, acylamino, substituted acylamino, protected amino, a heterocyclic group, hydroxy, lower alkylsulfonyloxy or arylsulfonyloxy; lower alkenyl optionally substituted with acyl; lower alkynyl optionally substituted with hydroxy, amino, protected amino, lower alkylsulfonyloxy or arylsulfonyloxy; amino(lower)alkylsulfonyl; N-protected amino(lower)alkylsulfonyl; lower alkylaminosulfonyl; a heterocyclicsulfonyl; amino(lower)alkylsulfinyl; N-protected amino(lower)alkylsulfinyl; piperidyloxy; or N-protected piperidyloxy; R^ is hydrogen, lower alkyl, lower alkoxy or halogen; A is a single bond, 0 or NH; o o E is lower alkylene, lower alkenylene, ___ ___ or o 1 ' a group of the formula : -G-J- in which G is lower alkylene and J is 0 or -N- (wherein R° is hydrogen or N-protective group) ; X is -CH=CH-, -CH=N- or S; and Y is CH or N; and pharmaceutically acceptable salts thereof. The object compound (I) for its salt can be prepared by the processes as illustrated in the following reaction schemes. Process 1 (ID (III) or its salt or its reactive derivative at the carboxy group or the sulfo group, or a salt thereof (la) or its salt Process 2 (IV) (V) or its saslt or its reactive derivative at the carboxy group or a salt thereof (I) or its salt Process 3 or its salt or its salt Process 5 Process 6 or its reactive derivative or its salt at the carboxy group or a salt thereof Process 7 or its reactive derivative or its salt at the carboxy group or a salt thereof Process 8 Process 9 Process χo Process 11 R R R _R ^N^ * R 5 (Igb) (In) or its salt or its salt Process 12 or its salt or its salt H Process 14 (VII) (VIII) (Is ) or its salt or its salt or its salt Process 15 (it) (lu) or its salt or its salt Process 16 Process 17 debenzylation or its salt or its salt Process 18 Process 19 Process? 20 Process 21 or its salt or its salt Process 22 or its salt cr its salt Process 23 or its salt or its salt Process 24 Process 26 (ID (XII) (1-11) or its salt or it salt or its salt Process 2 7 Process 28 Process 29 or its salt or its salt - 16 - Process 30 Process 31 or its reactive derivative or its salt at the carboxy group or a salt thereof Process 32 Process 33 or its salt or its salt Process 34 Process 35 Process 36 or its salt or its salt Process 3 S or its reactive derivative or its salt at the carboxy group or a salt thereof Process 39 or its reactive derivative or its salt at the carboxy group or a salt thereof wherein R 1 , R 2 , R 3 , R 4 , R 5 , A, E, X and Y are each as defined above, o o E a is J_ or JL ° R g is aryl, haloaryl, cyclo(lower)alkyl or a heterocyclic group, each of which is substituted with esterified carboxy; lower alkenyl substituted with esterified carboxy or esterified carboxy-substituted aryl; lower alkyl substituted with esterified carboxy, esterified carboxy(lower)alkanoyloxy or esterified carboxy(lower)alkoxyimino; lower alkylthio substituted with esterified carboxy; alkoxy substituted with esterified carboxy-substituted aryl, esterified carboxy-substituted pyridyl, esterified carboxy(lower)alkylamino, N-protected-esterified carboxy(lower)alkylamino, N-esterified carboxy(lower)alkyl-N-lower alkylamino, esterified carboxy or esterified carboxy(lower)alkoxyimino; or lower alkenyloxy substituted with esterified carboxy; R^ is aryl, haloaryl, cyclo(lower)alkyl or a heterocyclic group, each of which is substituted with carboxy; lower alkenyl substituted with carboxy or carboxy-substituted aryl; lower alkyl substituted with carboxy, carboxy(lower)- alkanoyloxy or carboxy(lower)alkoxyimino; lower alkylthio substituted with carboxy; alkoxy substituted with carboxy-substituted aryl, carboxy-substituted pyridyl, carboxy(lower)- alkylamino, N-protected-carboxy(lower)alkylamino, N-carboxy(lower)alkyl-N-lower alkylamino, carboxy or carboxy(lower)alkoxyimino; or lower alkenyloxy substituted with carboxy; R 4 is lower alkoxy substituted with esterified carboxy; lower alkylthio substituted with esterified carboxy; lower alkyl substituted with esterified carboxy; or lower alkenyl substituted with esterified carboxy; R^ is lower alkoxy substituted with carboxy; lower alkylthio substituted with carboxy; lower alkyl substituted with carboxy; or lower alkenyl substituted with carboxy; R 4 is protected amino; N-protected piperidyloxy; N-protected amino(lower)alkylamino; lower alkoxy substituted with protected amino; lower alkylthio substituted with protected amino; lower alkyl substituted with protected amino; lower alkynyl substituted with protected amino; or N-protected amino(lower)alkylsulfonyl; R^ is amino; piperidyloxy; amino(lower)alkylamino; lower alkoxy substituted with amino; lower alkylthio substituted with amino; lower alkyl substituted with amino; lower alkynyl substituted with amino; or amino(lower)alkylsulfonyl; R^ is aryl, haloaryl, cyclo(lower)alkyl or a heterocyclic group, each of which is substituted with substituted or unsubstituted N-containing heterocycliccarbonyl; carba oyl; substituted or unsubstituted lower alkylcarbamoyl; lower alkenyl substituted with substituted or unsubstituted N-containing heterocycliccarbonyl, carbamoyl, substituted or unsubstituted lower alkylcarbamoyl or N-containing heterocycliccarbonyl-substituted aryl; lower alkyl substituted with substituted or unsubstituted N-containing heterocycliccarbonyl, carbamoyl, substituted or unsubstituted lower alkylcarbamoyl, substituted or unsubstituted N-containing heterocycliccarbonyl (lower)alkanoyloxy, carbamoyl(lower)alkanoyloxy, substituted or unsubstituted lower alkylcarbamoyl (lower)alkanoyloxy, substituted or unsubstituted N-containing heterocycliccarbonyl(lower)alkoxyimino, carbamoyl- (lower)alkoxyimino or substituted or unsubstituted lower alkylcarbamoyl (lower)alkoxyimino; lower alkylthio substituted with substituted or unsubstituted N-containing heterocycliccarbonyl, carbamoyl or substituted or unsubstituted lower alkylcarbamoyl; alkoxy substituted with substituted or unsubstituted N-containing heterocycliccarbonyl- substituted aryl, carbamoyl-substituted aryl, substituted or unsubstituted lower alkylcarbamoyl- substituted aryl, substituted or unsubstituted N-containing heterocycliccarbonyl-substituted pyridyl, carbamoyl-substituted pyridyl, substituted or unsubstituted lower alkylcarbamoyl-substituted pyridyl, substituted or unsubstituted N-containing heterocycliccarbonyl (lower)alkylamino, carbamoyl(lower)alkylamino, substituted or unsubstituted lower alkylcarbamoyl(lower)alkylamino, N-protected- (substituted or unsubstituted N-containing heterocyclic)carbonyl (lower)alkylamino. N-protected-carbamoyl(lower)alkylamino, N-protected substituted or unsubstituted lower alkylcarbamoyl- (lower)alkylamino, N-(substituted or unsubstituted N-containing heterocyclic)carbonyl(lower)alkyl-N- lower alkylamino, N-carbamoyl(lower)alkyl-N-lower alkylamino, substituted or unsubstituted N-lower alkylcarbamoyl-N-lower alkylamino, substituted or unsubstituted N-containing heterocycliccarbonyl, carbamoyl, aminocarbamoyl, pyridylcarbamoyl, N-(lower alkyl)piperazinylcarbonyl, substituted or unsubstituted lower alkylcarbamoyl, substituted or unsubstituted N-containing heterocycliccarbonyl(lower)alkoxyimino, carbamoyl(lower)alkoxyimino or substituted or unsubstituted lower alkylcarbamoyl(lower)alkoxyimino; or lower alkenyloxy substituted with substituted or unsubstituted N-containing heterocycliccarbonyl, carbamoyl or substituted or unsubstituted lower alkylcarbamoyl; R is lower alkoxy, lower alkylthio, lower alkyl or lower alkenyl, each of which is substituted with substituted or unsubstituted N-containing heterocycliccarbonyl, carbamoyl, or substituted or unsubstituted lower alkylcarbamoyl; R is methoxy substituted with aryl or substituted aryl; or lower alkylthio which is substituted with methoxy substituted with aryl or substituted aryl; R 4 is hydroxy; or lower alkylthio substituted with hydroxy; Ri a is hydroxy; R is lower alkyl substituted with hydroxy, aryl, substituted aryl, acyl, amino, lower alkylamino, acylamino, protected amino or a heterocyclic group; or N-protected piperidyl; Z 1 is hydroxy; or acid residue; R is lower alkoxy substituted with hydroxy, aryl, substituted aryl, acyl, amino, lower alkylamino, acylamino, protected amino or a heterocyclic group; or N-protected piperidyloxy; R^ a is lower alkoxy substituted with amino; lower alkylthio substituted with amino; or lower alkyl substituted with amino; R 4 is lower alkoxy substituted with acylamino or substituted acylamino; lower alkylthio substituted with acylamino or substituted acylamino; or lower alkyl substituted with acylamino or substituted acylamino; R is amino; lower alkoxy substituted with amino; lower alkylthio substituted with amino; or lower alkyl substituted with amino; R? is lower alkoxy substituted with lower alkylamino; lower alkylthio substituted with lower alkylamino; lower alkyl substituted with lower alkylamino; lower alkylamino; or N-protected amino(lower)alkylamino; Rj * is acyloxy; Z 2 is acid residue; E j - is lower alkylene; R j is lower alkylthio substituted with amino or protected amino; R^ is lower alkylsulfinyl substituted with amino or protected amino, or lower alkylsulfonyl substituted with amino or protected amino; E_ is lower alkenylene; R^ is aryl which is substituted with methoxy substituted with aryl or substituted aryl; R g is aryl which is substituted with hydroxy; Z 3 is hydroxy; or acid residue; R 8 is lower alkyl optionally substituted with acyl, acylamino, protected amino, aryl, substituted aryl, acyl-substituted pyridyl or N-protected guanidino; R^ is aryl which is substituted with lower alkoxy optionally substituted with acyl, acylamino, protected amino, aryl, substituted aryl, acyl- substituted pyridyl or N-protected guanidino; R 3 is methoxy substituted with aryl; acyloxy; or substituted acyloxy; Z 4 is acid residue; q R^ is lower alkyl optionally substituted with esterified carboxy; Rj~ is lower alkoxy optionally substituted with esterified carboxy; R 3 is lower alkoxy substituted with esterified carboxy; R^ is lower alkoxy substituted with carboxy; R^ is halogen; R 4 is lower alkynyl optionally substituted with hydroxy, amino, protected amino, lower alkylsulfonyloxy or arylsulfonyloxy; R 4 is lower alkylthio, lower alkyl or lower alkynyl, each of which is substituted with hydroxy; Z 5 is halogen; R 10 is lower alkylsulfonyl or arylsulfonyl; Rq is lower alkylthio, lower alkyl or lower alkynyl, each of which is substituted with lower alkylsulfonyloxy or arylsulfonyloxy; R 4 is lower alkylthio, lower alkyl or lower alkynyl, each of which is substituted with phthalimido; R 4 is lower alkyl optionally substituted with hydroxy, amino, protected amino, lower alkylsulfonyloxy or arylsulfonyloxy; E^ is a single bond or lower alkylene; Z 6 is acid residue; R is lower alkyl optionally substituted with aryl or acyl; R q is aryl which is substituted with lower alkoxy substituted with amino; R£ is aryl which is substituted with lower alkoxy substituted with acylamino or substituted acylamino; R! is aryl which is substituted with lower alkoxy substituted with oxopiperidylcarbonyl; R is aryl which is substituted with lower alkoxy substituted with hydroxypiperidylcarbonyl; R^ is aryl which is substituted with lower alkoxy substituted with formyl or oxopiperidylcarbonyl; R j - is aryl which is substituted with lower alkoxy substituted with aminopiperidylcarbonyl or N-lower alkylpiperazinyl; R^ is aryl which is substituted with lower alkoxy substituted with carboxy; R^ is aryl which is substituted with lower alkoxy substituted with lower alkylamino(lower)- alkoxycarbonyl; R Q is aryl which is substituted with lower alkoxy substituted with esterified carboxy; R p is aryl which is substituted with lower alkoxy substituted with hydroxy; R is aryl which is substituted with lower alkoxy substituted with formyl; R is aryl which is substituted with lower alkoxy substituted with cyano-substituted aryl; R g is aryl which is substituted with lower alkoxy substituted with tetrazolyl-substituted aryl; R 4 is lower alkoxy substituted with amino; R 4 is lower alkoxy substituted with guanidino; R is aryl which is substituted with lower alkoxy substituted with protected amino, N-protected amino(lower)alkanoyla ino, N-protected piperazinylcarbonyl or N-protected guanidino; R.1 is aryl which is substituted with lower alkoxy substituted with amino, amino(lower)alkanoylamino, piperazinylcarbonyl or guanidino; R*. is aryl which is substituted with lower alkoxy substituted with phenoxycarbonylamino; R^ is aryl which is substituted with lower alkoxy substituted with N-lower alkylpiperazinylcarbonylamino, dimethylaminopiperidylcarbonylamino, carbamoylamino or dimethylcarbamoylamino; and R 3 is lower alkoxy which is substituted with carbamoyl optionally substituted with lower alkyl. In the above and subsequent description of the present specification, suitable examples of the various definitions to be included within the scope of the invention are explained in detail in the following. The term "lower" is intended to mean a group having 1 to 6 carbon atom(s), unless otherwise provided. The "higher" is intended to mean 7 to 20 carbon atoms, unless otherwise provided. The lower moiety in the terms "cyclo(lower)alkyl" and "cyclo(lower)alkyloxy" is intended to mean a group having 3 to 6 carbon atoms. The lower moiety in the terms "lower alkenyl", "lower alkenyloxy" and "lower alkynyl" is intended to mean a group having 2 to 6 carbon atoms. The term "alkoxy" may included lower alkoxy and higher alkoxy. Suitable "lower alkoxy" and lower alkoxy moiety in the terms "acyl (lower)alkoxy", "acyl(lower)alkoxyimino", "esterified carboxy(lower)alkoxyimino", "carboxy(lower)alkoxyimino", "N-containing heterocycliccarbonyl(lower)alkoxyimino", "carbamoyl(lower)alkoxyimino", "lower alkylcarbamoyl- (lower)alkoxyimino", "lower alkoxycarbonyl" and "ar(lower)alkoxy" may be straight or branched C^-Cg alkoxy such as methoxy, ethoxy, propoxy, isopropoxy, methylpropoxy, butoxy, isobutoxy, tert-butoxy, pentyloxy, hexyloxy or the like. Suitable "higher alkoxy" may be straight or branched c 7 ~ 20 alkoχ y such as heptyloxy, octyloxy, nonyloxy, decyloxy, undecyloxy, dodecyloxy, tridecyloxy, tetradecyloxy, pentadecyloxy, hexadecyloxy, heptadecyloxy, octadecyloxy, nonadecyloxy, eicosyloxy, methylheptyloxy, methyloctyloxy, methylnonyloxy, methyldecyloxy, ethylheptyloxy, ethyloctyloxy, ethylnonyloxy, ethyldecyloxy or the like, in which preferable one is heptyloxy. Suitable "lower alkyl" and lower alkyl moiety in the terms "acyl (lower)alkylsulfinyl", "acyl (lower)alkyl¬ sulfonyl", "lower alkylamino(lower)alkylcarbamoyloxy", "acyl (lower) alkylamino", "N-protected-acyl (lower)- alkylamino", "N-acyl (lower)alkyl-N-lower alkylamino", "lower alkylhydrazinocarbonylamino", "esterified carboxy(lower)alkylamino", "N-protected-esterified carboxy(lower) lkylamino", "N-esterified carboxy(lower)alkyl-N-lower alkylamino", "carboxy(lower)alkylamino", "N-protected-carboxy(lower)- alkylamino", "N-carboxy(lower)alkyl-N-lower alkylamino", "lower alkylcarbamoyl", "lower alkylcarbamoyl(lower)alkanoyloxy", "lower alkylcarbamoyl (lower) lkoxyimino", "lower alkylthio", "N-protected- (substituted or unsubstituted N-containing heterocyclic)carbonyl (lower)alkylamino", "N-protected- carbamoyl (lower) alkylamino", "N-protected-substituted or unsubstituted lower alkylcarbamoyl (lower)alkylamino", "N- (substituted or unsubstituted N-containing heterocyclic)carbonyl (lower)alkyl-N-lower alkylamino", "N-carbamoyl (lower)alkyl-N-lower alkylamino", "N-lower alkylcarbamoyl-N-lower alkylamino", "lower alkylcarbamoyl- (lower)alkoxyimino", "1-hydroxy(lower)alkyl", "1-(lower alkyl)amino(lower)alkyl", "mono(lower)alkylamino". - 28 - "acyl(lower)alkyl", "di(lower)alkylamino", "lower alkylsulfinyl", "lower alkylsulfonyl", "lower alkylamino", "amino(lower)alkylamino", "N-protected amino(lower)alkylamino", "lower alkylsulfonyloxy", "amino(lower)alkylsulfonyl", "N-protected amino(lower)alkylsulfonyl", "lower alkylaminosulfonyl", "amino(lower)alkylsulfinyl" and "N-protected amino(lower)alkylsulfinyl" may be straight or branched C^-Cg alkyl such as methyl, ethyl, propyl, isopropyl, butyl, isobutyl, tert-butyl, pentyl, ethylpropyl, hexyl or the like. Suitable "cyclo(lower)alkyl" and cyclo(lower)alkyl moiety in the term "cyclo(lower)alkyloxy" may be cyclo(C3~Cg)alkyl such as cyclopropyl, cyclobutyl, cyclopentyl or cyclohexyl, in which preferable one is cyclopentyl or cyclohexyl. Suitable "lower alkenyl" and lower alkenyl moiety in the term "lower alkenyloxy" may be straight and branched C2-C5 alkenyl such as ethenyl, propenyl, pentenyl, isopropenyl, butenyl, hexenyl or the like, in which preferable one is ethenyl, propenyl, pentenyl or hexenyl. Suitable "lower alkynyl" may be straight and branched C 2 ~Cg alkynyl such as ethynyl, propargyl, butynyl or the like, in which preferable one is butynyl. Suitable "aryl" and aryl moiety in the terms "haloaryl", "arylsulfonyl", "acyl-substituted aryl", "ar(lower)alkoxy", "substituted ar(lower)alkoxy" and "arylsulfonyloxy" may be phenyl, naphthyl, phenyl substituted with lower alkyl [e.g. tolyl, xylyl, mesityl, cumenyl, di(tert-butyl)phenyl, etc.] and the like, in which preferable one is phenyl, tolyl or xylyl. Suitable "substituted aryl" may be aryl substituted with suitable substituent (s) such as acyl, substituted acyl, N-protected piperazinylsulfonyl, piperazinylsulfonyl, N-lower alkylpiperazinylsulfonyl. hydroxy(lower)alkyl, a heterocyclic(lower)alkyl, halogen, nitro, amino, lower alkylamino, a heterocyclic group [e.g. thiazolyl, oxazolyl, tetrazolyl, oxazolinyl, pyridyl, pyrimidinyl, pyrrolyl optionally substituted with lower alkyl and cyano, etc.], cyano, lower alkoxy or the like, in which preferable one for the substituent of alkoxy for R 1 is aryl substituted with N-methylpiperazinylsulfonyl, N-t-butoxycarbonyl- piperazinylsulfonyl, piperazinylsulfonyl, carboxy, esterified carboxy, N-lower alkylpiperazinylcarbonyl, lower alkanoyl, hydroxy(lower)alkyl, N-lower alkyl- piperazinyl (lower)alkyl, thiazolyl, oxazolyl, tetrazolyl, oxazolinyl, pyridyl, pyrimidinyl, pyrrolyl substituted with lower alkyl and cyano, cyano, lower alkoxy, lower alkylaminopiperidylcarbonyl, and preferable one for R 4 is aryl substituted with halogen, nitro, amino, lower alkylamino or lower alkoxy. Suitable "halogen" and halo moiety in the term "haloaryl" may be fluorine, chlorine, bromine and iodine, in which preferable one is chlorine or bromine. Suitable "lower alkylamino" and lower alkylamino moiety in the terms "lower alkylamino(lower)- alkylcarbamoyloxy", "acyl (lower)alkylamino", "esterified carboxy(lower)alkylamino", "carboxy(lower)alkylamino", "N-containing heterocycliccarbonyl (lower)alkylamino", "carbamoyl (lower)alkylamino", "lower alkylcarbamoyl- (lower)alkylamino" "amino(lower)alkylamino", "N-protected amino(lower)alkylamino", "lower alkyla inosulfonyl" and "lower alkylaminopiperidylcarbonyl" may be mono or di (lower alkyl)amino such as methylamino, ethylamino, propylamino, isopropylamino, butylamino, tert-butylamino, isobutylamino, pentylamino, hexylamino, dimethylamino, diethylamino, dipropylamino, dibutylamino, diisopropylamino, dipentylamino, dihexylamino, N-methylethylamino or the like, in which preferable one is methylamino, dimethylamino or diethylamino. Suitable "1-hydroxy(lower)alkyl" may be 1-hydroxy- (C^-Cg)alkyl such as hydroxymethyl, 1-hydroxyethyl, 1-hydroxypropyl, 1-hydroxybutyl, l-hydroxy-3-methylpropyl or the like, in which preferable one is hydroxymethyl or 1-hydroxyethyl. Suitable "1- (lower alkyl)amino(lower)alkyl" may be 1-mono or di (Cτ_-Cg alkyl)amino(C^-Cg)alkyl such as methylaminomethyl, dimethylaminomethyl, 1-methylaminoethyl, 1-dimethylaminoethyl, ethyla inomethyl, 1-ethylaminoethyl or the like, in which preferable one is methylaminomethyl, dimethylaminomethyl, 1-methylaminoethyl or 1-dimethylaminoethyl. Suitable "heterocyclic group" may be one containing at least one hetero atom selected from nitrogen, sulfur and oxygen atom, and may include saturated or unsaturated, monocyclic or polycyclic heterocyclic group, and preferable heterocyclic group may be N-containing heterocyclic group such as unsaturated 3 to 6-membered heteromonocyclic group containing 1 to 4 nitrogen atoms, for example, pyrrolyl, pyrrolinyl, imidazolyl, pyrazolyl, pyridyl, pyrimidinyl, pyrazinyl, pyridazinyl, triazolyl [e.g. 4H-l,2,4-triazolyl, 1H-1,2,3-triazolyl, 2H-1,2,3- triazolyl, etc.], tetrazolyl [e.g. lH-tetrazolyl, 2H-tetrazolyl, etc.], etc.; saturated 3 to 7-membered heteromonocyclic group containin 1 to 4 nitrogen atoms [e.g. pyrrolidinyl, imidazolidinyl, piperidyl, piperazinyl, homopiperazinyl, etc.]; unsaturated condensed heterocyclic group containing 1 to 5 nitrogen atoms, for example, indolyl, isoindolyl, indolizinyl, benzimidazolyl, quinolyl, isoquinolyl, imidazopyridyl, indazolyl, bεnzotriazolyl, tetrazolo- pyridazinyl [e.g. tetrazolo[1,5-b]pyridazinyl, etc.], etc. unsaturated 3 to 6-membered heteromonocyclic group containing an oxygen atom, for example, pyranyl, furyl. etc . ; saturated 3 to 6-membered heteromonocyclic group containing an oxygen atom, for example, lH-tetrahydropyranyl, tetrahydrofuranyl, etc.; unsaturated, 3 to 6-membered heteromonocyclic group containing 1 to 2 sulfur atoms, for example, thienyl, etc.; unsaturated 3 to 6-membered heteromonocyclic group containing 1 to 2 oxygen atoms and 1 to 3 nitrogen atoms, for example, oxazolyl, isoxazolyl, oxadiazolyl [e.g. 1,2,4-oxadiazolyl, 1,3,4-oxadiazolyl, 1,2,5-oxadiazolyl, etc.], oxazolinyl [e.g. 2-oxazolinyl, etc.], etc.; saturated 3 to 6-membered heteromonocyclic group containing 1 to 2 oxygen atoms and 1 to 3 nitrogen atoms [e.g. morpholinyl, etc.]; unsaturated condensed heterocyclic group containing 1 to 2 oxygen atoms and 1 to 3 nitrogen atoms [e.g. benzofurazanyl, benzoxazolyl, benzoxadiazolyl, etc.]; unsaturated 3 to 6-membered heteromonocyclic group containing 1 to 2 sulfur atoms and 1 to 3 nitrogen atoms, for example, thiazolyl, thiadiazolyl [e.g., 1,2,4-thiadiazolyl, 1,3,4-thiadiazolyl, 1,2,5-thiadiazolyl, etc.], etc.; saturated 3 to 6-membered heteromonocyclic group containing 1 to 2 sulfur atoms and 1 to 3 nitrogen atoms [e.g., thiazolidinyl, etc.]; unsaturated condensed heterocyclic group containing 1 to 2 sulfur atoms and 1 to 3 nitrogen atoms [e.g., benzothiazolyl, benzothiadiazolyl, etc.]; unsaturated condensed heterocyclic group containing 1 to 2 oxygen atoms [e.g. benzofuranyl, benzodioxolyl, etc.] and the like. Said "heterocyclic group" may be substituted with lower alkyl as exemplified above or oxo, in which preferable one is N-methylpiperazinyl, tetrazolyl, morpholinyl, pyrrolidinyl, N-methylpiperidyl, N-methylhomopiperazinyl, lH-tetrahydropyranyl, thienyl, pyridyl, piperidyl or oxopiperidyl. Suitable acyl and acyl moiety in the terms "acyl(lower)alkylsulfinyl", "acyl(lower)alkylsulfonyl", "acyloxy", "acylamino", "acyl(lower)alkanoyloxy", "acyl(lower)alkoxyimino", "acyl(lower)alkylamino", "N- protected-acyl(lower)alkylamino", "N-acyl(lower)alkyl-N- lower alkylamino" and "acyl(lower)alkoxy" may be carboxy, esterified carboxy, carbamoyl, lower alkylcarbamoyl, lower alkanoyl, aroyl, a heterocycliccarbonyl and the like. The esterified carboxy may be substituted or unsubstituted lower alkoxycarbonyl [e.g. methoxycarbonyl, ethoxycarbonyl, propoxycarbonyl, butoxycarbonyl, tert-butoxycarbonyl, hexyloxycarbonyl, 2-iodoethoxycarbonyl, 2,2,2-trichloroethoxycarbonyl, dimethylaminopropoxycarbonyl, dimethylaminoethoxycarbonyl, etc.], substituted or unsubstituted aryloxycarbonyl [e.g. phenoxycarbonyl, 4-nitrophenoxycarbonyl, 2-naphthyloxycarbonyl, etc.], substituted or unsubstituted ar(lower)alkoxycarbonyl [e.g. benzyloxycarbonyl, phenethyloxycarbonyl, benzhydryloxycarbonyl, 4-nitrobenzyloxycarbonyl, 3-methoxy-4-nitrobenzyloxy- carbonyl, etc.], N-containing heterocyclicoxycarbonyl [e.g. N-methylpiperidyloxycarbonyl, etc.] and the like, i which preferable one is lower alkoxycarbonyl, N-methylpiperidyloxycarbonyl, dimethylaminopropoxycarbony or dimethylaminoethoxycarbonyl. The lower alkylcarbamoyl may be mono or di(lower alkyl)carbamoyl such as methylcarbamoyl, ethylcarbamoyl, propylcarba oyl, dimethylcarbamoyl, diethylcarbamoyl, N-methyl-N-ethylcarbamoyl or the like. The lower alkanoyl may be substituted or unsubstituted C^-Cg alkanoyl such as formyl, acetyl, propionyl, butyryl, isobutyryl, valeryl, isovaleryl, pivaloyl, hexanoyl, trifluoroacetyl or the like, in which preferable one is formyl, acetyl or butyryl. The aroyl may be benzoyl, naphthoyl, toluoyl, di(tert-butyl)benzoyl and the like, in which preferable one is benzoyl. The heterocyclic moiety in the terms "a heterocyclic¬ carbonyl", "heterocyclicoxycarbonylamino" and "heterocyclicsulfonyl" may be one mentioned above as a heterocyclic group. Preferred "a heterocycliccarbonyl" may be N-containing heterocycliccarbonyl. The "N-containing heterocycliccarbonyl" may be one containing at least one nitrogen atom in heterocyclic group mentioned above, in which preferable one is N- (lower alkyl)piperazinylcarbonyl (e.g. N-methyl- piperazinylcarbonyl, etc.), N- (lower alkyl)- homopiperazinylcarbonyl (e.g. N-methylhomopiperazinyl- carbonyl, etc.), piperazinylcarbonyl, pyrrodinylcarbonyl, piperidylcarbonyl, morpholinocarbonyl, lower alkylpiperidylcarbonyl (e.g. methylpiperidylcarbonyl, etc.) or oxopiperidylcarbonyl. Suitable "substituted acyl" may be carbamoyl substituted with amino, a heterocyclic group [e.g. N- (lower alkyl)piperazinyl, pyridyl, etc.], lower alkylsulfonyl or arylsulfonyl, substituted lower alkylcarbamoyl [e.g. N-lower alkylamino-N-lower alkylcarbamoyl, pyridyl(lower)alkylcarbamoyl, morpholino(lower)alkylcarbamoyl, bis[hydroxy(lower)alkyl]carbamoyl, hydroxy(lower)alkylcarbamoyl, carbamoyl(lower)alkylcarbamoyl, lower alkylamino(lower)alkylcarbamoyl, N-lower alkyl-N-lower alkylcarbamoyl, etc.], substituted N-containing heterocycliccarbonyl [e.g. trifluoroacetyl- piperazinylcarbonyl, pyridylpiperazinylcarbonyl, hydroxypiperidylcarbonyl, dimethylammopiperidylcarbonyl. diethylaminopiperidylcarbonyl, carbamoylpyrrolidinylcarbonyl, dimethylaminopiperazinylcarbonyl, hydroxyethoxyethyl- piperazinylcarbonyl, pyrrolidinylcarbonylmethyl- piperazinylcarbonyl, etc.], N-protected-N-containing heterocycliccarbonyl [e.g. N-t-butoxycarbonylpiperidyl- carbonyl, N-t-butoxycarbonylpiperazinylcarbonyl, etc.], N-protected amino(lower)alkanoyl, amino(lower)alkanoyl, benzyloxybenzoyl, and the like. "N-Protective group" in "protected amino" may be common N-protective group such as substituted or unsubstituted lower alkanoyl [e.g. formyl, acetyl, propionyl, trifluoroacetyl, etc.], phthaloyl, lower alkoxycarbonyl [e.g. tert-butoxycarbonyl, tert- amyloxycarbonyl, etc.], substituted or unsubstituted aralkyloxycarbonyl [e.g. benzyloxycarbonyl, p-nitrobenzyloxycarbonyl, etc.], 9-fluorenylmethoxycarbonyl, substituted or unsubstituted arenesulfonyl [e.g. benzenesulfonyl, tosyl, etc.], nitrophenylsulfenyl, aralkyl [e.g. trityl, benzyl, etc.] or the like, in which preferable one is phthaloyl, tert- butoxycarbonyl or 9-fluorenylmethoxycarbonyl. "N-protective group" in "N-protected guanidino" may be common N-protective group such as lower alkoxycarbonyl [e.g. tert-butoxycarbonyl, etc.] or the like. Suitable "acid residue" may be halogen [e.g. fluoro, chloro, bromo, iodo] , arenesulfonyloxy [e.g. benzenesulfonyloxy, tosyloxy, etc.], alkanesulfonyloxy [e.g. mesyloxy, ethanesulfonyloxy, etc.], and the like, i which preferable one is halogen. Suitable "lower alkylsulfonyl" and lower alkylsulfonyl moiety in the term "lower alkylsulfonyloxy" may be (C-^-Cg)alkylsulfonyl such as methylsulfonyl, ethylsulfonyl, propylsulfonyl or the like, in which preferable one is methylsulfonyl. Suitable "lower alkylene" may be straight or branched c l~ c 6 alkylene such as methylene, ethylene, propylene or the like, in which preferable one is methylene or ethylene. Suitable "lower alkenylene" may be straight or branched C2~Cg alkenylene such as ethenylene, propenylene or the like, in which preferable one is ethenylene. The substituent(s) on aryl for R 1 may be plural and in such case the substituents may be the same or different. Preferred "aryl" for R 1 may be phenyl or phenyl substituted with lower alkyl. Preferred "cyclo(lower)alkyl" for R 1 may be cyclopentyl. Preferred "a heterocyclic group" for R* may be pyridyl or thienyl. Preferred compound (I) is one having aryl (more preferably phenyl or phenyl substituted with lower alkyl) which may be substituted with lower alkoxy optionally substituted with acylamino or acyl for R 1 , lower alkyl for R 2 , hydrogen, lower alkyl or lower alkoxy for R 3 , hydroxy, or lower alkoxy, lower alkylthio or lower alkyl, each of which may be substituted with hydroxy, aryl, substituted aryl, acyl, amino, lower alkylamino, acylamino, protected amino or a heterocyclic group for R 4 , hydrogen, lower o alkyl, lower alkoxy or halogen for R^, NH for A, ___ for E, -CH=CH- for X, and CH for Y. More preferred compound (I) is one having phenyl or tolyl, each of which is substituted with lower alkoxy substituted with N- (lower alkyl)piperazinylcarbonyl for R , lower alkyl for R 2 , hydrogen, lower alkyl or lower alkoxy for R 3 , lower alkoxy substituted with amino for R 4 , o hydrogen for R 5 , NH for A, ___ for E, -CH=CH- for X and CH for Y. Most preferred compound (I) is one having tolyl 95 - 36 - which is substituted with lower alkoxy substituted with N- (lower alkyl)piperazinylcarbonyl for R , lower alkyl for R 2 , lower alkoxy for R 3 , lower alkoxy substituted with o amino for R 4 , hydrogen for R 5 , NH for A, ___ for E, -CH=CH- for X and CH for Y. Suitable pharmaceutically acceptable salts of the object compound (I) are conventional non-toxic salts and include an acid addition salt such as an inorganic acid addition salt [e.g. hydrochloride, hydrobro ide, sulfate, phosphate, etc.], an organic acid addition salt [e.g. formate, acetate, trifluoroacetate, maleate, tartrate, methanesulfonate, benzenesulfonate, toluenesulfonate, etc.], a metal salt such as an alkali metal salt [e.g. sodium salt, potassium salt, etc.] and an alkaline earth metal salt [e.g. calcium salt, magnesium salt, etc.] and the like. The processes for preparing the object compound (I) are explained in detail in the following. Process 1 The object compound (la) or its salt can be prepared by reacting a compound (II) or its salt with a compound (III) or its reactive derivative at the carboxy group or the sulfo group, or a salt thereof. Suitable salts of the compounds (la) and (II) may be the same as those exemplified for the compound (I) . Suitable salts of the compound (III) and its reactiv derivative at the carboxy group or the sulfo group may be base salts as exemplified for the compound (I) . Suitable reactive derivative at the carboxy group or the sulfo group of the compound (III) may include an acid halide, an acid anhydride containing intramolecular, intermolecular and a mixed ones, an activated amide, an activated ester, and the like. Suitable examples of the reactive derivatives may be an acid chloride; an acid azide; a mixed acid anhydride with an acid such as substituted phosphoric acid [e.g. dialkylphosphoric acid, phenylphosphoric acid, diphenylphosphoric acid, dibenzylphosphoric acid, halogenated phosphoric acid, etc.], dialkylphosphorous acid, sulfurous acid, thiosulfuric acid, sulfuric acid, sulfonic acid [e.g. methanesulfonic acid, etc.], aliphatic carboxylic acid [e.g. acetic acid, propionic acid, butyric acid, isobutyric acid, pivalic acid, pentanoic acid, isopentanoic acid, 2-ethylbutyric acid, trichloroacetic acid, etc.] or aromatic carboxylic acid [e.g. benzoic acid, etc.]; a symmetrical acid anhydride; an activated amide with imidazole, 4-substituted imidazole, dimethylpyrazole, triazole or tetrazole; or an activated ester [e.g. cyanomethyl ester, methoxymethyl ester, dimethyli inomethyl [ (CH3)2N=CH-] ester, vinyl ester, propargyl ester, p-nitrophenyl ester, 2,4-dinitrophenyl ester, trichlorophenyl ester, pentachlorophenyl ester, mesylphenyl ester, phenylazophenyl ester, phenyl thioester, p-nitrophenyl thioester, p-cresyl thioester, carboxymethyl thioester, pyranyl ester, pyridyl ester, piperidyl ester, 8-quinolyl thioester, etc.] or an ester with an N-hydroxy compound [e.g. N,N-dimethylhydroxylamine, l-hydroxy-2- (1H)-pyridone, N-hydroxysuccinimide, N-hydroxyphthalimide, 1-hydroxy-lH-benzotriazole, etc.], and the like. These reactive derivatives can optionally be selected from them according to the kind of the compound (III) to be used. The reaction is usually carried out in a conventional solvent such as water, alcohol [e.g. methanol, ethanol, etc.], acetone, dioxane, acetonitrile, chloroform, methylene chloride, ethylene chloride, tetrahydrofuran, ethyl acetate, N,N-dimethylformamide, pyridine or any other organic solvent which does not adversely influence the reaction. These conventional solvents may also be used in a mixture with water. In this reaction, when the compound (III) is used in a free acid form or its salt form, the reaction is preferably carried out in the presence of a conventional condensing agent such as N,N'-dicyclohexylcarbodiimide; N-cyclohexyl-N'-morpholinoethylcarbodiimide; N-cyclohexyl-N 1 -(4-diethylaminocyclohexyl)carbodiimide; N,N'-diethylcarbodiimide, N,N'-diisopropylcarbodiimide; N-ethyl-N'-(3-dimethylaminopropyl)carbodiimide; N,N'-carbonylbis- (2-methylimidazole) ; pentamethyleneketene-N-cyclohexylimine; diphenylketene-N-cyclohexylimine; ethoxyacetylene; 1-alkoxy-l-chloroethylene; trialkyl phosphite; ethyl polyphosphate; isopropyl polyphosphate; phosphorus oxychloride (phosphoryl chloride) ; phosphorus trichloride; diphenylphosphoryl azide; diphenyl chlorophosphate; diphenylphosphinic chloride; thionyl chloride; oxalyl chloride; lower alkyl haloformate [e.g. ethyl chloroformate, isopropyl chloroformate, etc.]; triphenylphosphme; 2-ethyl-7-hydroxybenzisoxazolium salt; 2-ethyl-5-(m-sulfophenyl)isoxazolium hydroxide intramolecular salt; 1- (p-chlorobenzenesulfonyloxy)-6- chloro-lH-benzotriazole; so-called Vilsmeier reagent prepared by the reaction of N,N-dimethylformamide with thionyl chloride, phosgene, trichloromethyl chloroformate, phosphorus oxychloride, etc.; or the like. The reaction may also-be carried out in the presence of an inorganic or organic base such as an alkali metal bicarbonate, tri (lower)alkylamine, pyridine, 4-dimethylaminopyridine, N- (lower)alkylmorpholine, N,N-di(lower)alkylbenzylamine, or the like. The reaction temperature is not critical, and the reaction is usually carried out under cooling to heating. Process 2 The object compound (I) or its salt can be prepared by reacting a compound (IV) or its salt with a compound (V) or its reactive derivative at the carboxy group or a salt thereof. Suitable salts of the compounds (IV) and (V) and its reactive derivative at the carboxy group may be the same as those exemplified for the compound (I) . This reaction can be carried out in substantially the same manner as Process 1. and therefore the reaction mode and reaction condition (e.g. solvent, reaction temperature, etc.) of this reaction are to be referred to those as explained in Process 1. Process 3 The object compound (Ic) or its salt can be prepared by subjecting a compound (lb) or its salt to deesterification reaction. Suitable salt of the compound (Ic) may be the same as those exemplified for the compound (I) . Suitable salt of the compound (lb) may be an acid addition salt as exemplified for the compound (I) . The reaction is carried out in accordance with a conventional method such as hydrolysis, reduction or the like. The hydrolysis is preferably carried out in the presence of a base or an acid including Lewis acid. Suitable base may include an inorganic base and an organic base such as an alkali metal [e.g. lithium, sodium, potassium, etc.], an alkaline earth metal [e.g. magnesium, calcium, etc.], the hydroxide or carbonate or bicarbonate thereof, trialkylamine [e.g. trimethylamine, triethylamine, etc.], picoline, 1,5-diazabicyclo[4.3.0]- non-5-ene, 1,4-diazabicyclo[2.2.2]octane, 1, 8-diazabicyclo[5.4.0]undec-7-ene, or the like. Suitable acid may include an organic acid [e.g. formic acid, acetic acid, propionic acid, trichloroacetic acid, trifluoroacetic acid, etc.], an inorganic acid [e.g. hydrochloric acid, hydrobromic acid, hydroiodic acid, sulfuric acid, etc.] and Lewis acid [e.g. boron tribro ide, etc.]. The reaction is usually carried out in a solvent such as water, an alcohol [e.g. methanol, ethanol, etc.], xylene, diethylene glycol monomethyl ethyl, methylene chloride, tetrahydrofuran, a mixture thereof or any other solvent which does not adversely influence the reaction. A liquid base or acid can be also used as the solvent. The reaction temperature is not critical and the reaction is usually carried out under cooling to warming. The reduction can be applied preferably for elimination of the ester moiety such as 4-nitrobenzyl, 2-iodoethyl, 2,2,2-trichloroethyl, or the like. The reduction method applicable for the elimination reaction may include chemical reduction and catalitic reduction. Suitable reducing agents to be used in chemical reduction are a combination of metal [e.g. tin, zinc, iron, etc.] or metallic compound [e.g. chromium chloride, chromium acetate, etc.] and an organic or inorganic acid [e.g. formic acid, acetic acid, propionic acid, trifluoroacetic acid, p-toluenesulfonic acid, hydrochloric acid, hydrobromic acid, etc.]. Suitable catalysts to be used in catalytic reduction are conventional ones such -as platinum catalysts [e.g. platinum plate, spongy platinum, platinum black, colloida platinum, platinum oxide, platinum wire, etc.], palladium catalyst [e.g. spongy palladium, palladium black, palladium oxide, palladium on carbon, colloidal palladium palladium on barium sulfate, palladium on barium carbonate, etc.], nickel catalyst [e.g. reduced nickel, nickel oxide, Raney nickel, etc.], cobalt catalyst [e.g. reduced cobalt, Raney cobalt, etc.], iron catalyst [e.g. reduced iron, Raney iron, etc.], copper catalyst [e.g. reduced copper, Raney copper, Ullman copper, etc.] or the like. The reduction is usually carried out in a conventional solvent which does not adversely influence the reaction such as water, an alcohol [e.g. methanol, ethanol, propanol, etc.], N,N-dimethylformamide, or a mixture thereof. Additionally, in case that the above-mentioned acids to be used in chemical reduction are in liquid, they can also be used as a solvent. Further, a suitable solvent to be used in catalytic reduction may be the above-mentioned solvent, and other conventional solvent such as diethyl ether, dioxane, tetrahydrofuran, etc., or a mixture thereof. The reaction temperature of this reduction is not critical and the reaction is usually carried out under cooling to warming. In this reaction, in case that the compound (lb) having lower alkyl substituted with esterified carboxy for R 2 and/or acyloxy, lower alkoxy substituted with esterified carboxy, lower alkylthio substituted with esterified carboxy, or lower alkyl substituted with esterified carboxy for R 4 is used as a starting compound, the compound (Ic) having lower alkyl substituted with carboxy for R 2 and/or hydroxy, lower alkoxy substituted with carboxy, lower alkylthio substituted with carboxy, or lower alkyl substituted with carboxy for R 4 may be obtained according to reaction condition. This case is included within the scope of this reaction. Process 4 The object compound (le) or its salt can be prepared by subjecting a compound (Id) or its salt to deesterification reaction. Suitable salt of the compound (Id) may be an acid addition salt as exemplified for the compound (I) . Suitable salt of the compound (le) may be the same as those exemplified for the compound (I) . This reaction can be carried out in substantially the same manner as hydrolysis in Process 3. and therefore the reaction mode and reaction condition (e.g. solvent, reaction temperature, etc.) of this reaction are to be referred to those as explained in hydrolysis in Process 3. In this reaction, in case that the compound (Id) having aryl, haloaryl, cyclo(lower)alkyl or a heterocyclic group, each of which is substituted with esterified carboxy; lower alkenyl substituted with esterified carboxy; lower alkyl substituted with esterified carboxy, esterified carboxy(lower)alkanoyloxy or esterified carboxy(lower)alkoxyimino; lower alkylthio substituted with esterified carboxy; alkoxy substituted with esterified carboxy-substituted aryl, esterified carboxy- substituted pyridyl, esterified carboxy(lower)alkylamino, N-protected-esterified carboxy(lower)alkylamino, N-esterified carboxy(lower)alkyl-N-lower alkylamino, esterified carboxy or esterified carboxy(lower)alkoxyimino; or lower alkenyloxy substituted with esterified carboxy for R 1 and/or lower alkyl substituted with esterified carboxy for R 2 is used as a starting compound, the compound (le) having aryl, haloaryl, cyclo(lower)alkyl or a heterocyclic group, each of which is substituted with carboxy; lower alkenyl substituted with carboxy; lower alkyl substituted with carboxy, carboxy(lower)alkanoyloxy or carboxy(lower) lkoxyimino; lower alkylthio substituted with carboxy; alkoxy substituted with carboxy-substituted aryl, carboxy-substituted pyridyl, carboxy(lower)- alkylamino, N-protected-carboxy(lower)alkylamino, N-carboxy(lower)alkyl-N-lower alkylamino, carboxy or carboxy(lower)alkoxyimino; or lower alkenyloxy substituted with carboxy for R 1 and/or lower alkyl substituted with carboxy for R 2 may be obtained according to reaction condition. This case is included within the scope of this reaction. Process 5 The object compound (Ig) or its salt can be prepared by subjecting a compound (If) or its salt to elimination reaction of the N-protective group. Suitable salts of the compounds (If) and (Ig) may be acid addition salts as exemplified for the compound (I) . This reaction is carried out in accordance with a conventional method such as hydrolysis, reduction or the like. The hydrolysis is preferably carried out in the presence of a base or an acid including Lewis acid. Suitable base may include an inorganic base and an organic base such as an alkali metal [e.g. sodium, potassium, etc.], an alkaline earth metal [e.g. magnesium, calcium, etc.], the hydroxide or carbonate or bicarbonate thereof, hydrazine, alkylamine [e.g. methylamine, trimethylamine, triethyla ine, etc.], picoline, 1,5-diazabicyclo[4.3.0]non-5-ene, 1,4-diazabicyclo[2.2.2]octane, 1, 8-diazabicyclo[5.4.0]undec-7-ene, or the like. Suitable acid may include an organic acid [e.g. formic acid, acetic acid, propionic acid, trichloroacetic acid, trifluoroacetic acid, etc.], an inorganic acid [e.g. hydrochloric acid, hydrobromic acid, sulfuric acid, hydrogen chloride, hydrogen bromide, hydrogen fluoride, etc.] and an acid addition salt compound [e.g. pyridine hydrochloride, etc.]. The elimination using trihaloacetic acid [e.g. trichloroacetic acid, trifluoroacetic acid, etc.] or the like is preferably carried out in the presence of cation trapping agents [e.g. anisole, phenol, etc.]. The reaction is usually carried out in a solvent such as water, an alcohol [e.g. methanol, ethanol, etc.], methylene chloride, chloroform, tetrachloromethane, tetrahydrofuran, a mixture thereof or any other solvent which does not adversely influence the reaction. A liquid base or acid can be also used as the solvent. The reaction temperature is not critical and the reaction is usually carried out under cooling to heating. The reduction method applicable for the elimination reaction may include chemical reduction and catalytic reduction. Suitable reducing agents to be used in chemical reduction are a combination of metal [e.g. tin, zinc, iron, etc.] or metallic compound [e.g. chromium chloride, chromium acetate, etc.] and an organic or inorganic acid [e.g. formic acid, acetic acid, propionic acid, trifluoroacetic acid, p-toluenesulfonic acid, hydrochloric acid, hydrobromic acid, etc.]. Suitable catalysts to be used in catalytic reduction are conventional ones such as platinum catalysts [e.g. platinum plate, spongy platinum, platinum black, colloidal platinum, platinum oxide, platinum wire, etc.], palladium catalysts [e.g. spongy palladium, palladium black, palladium oxide, palladium on carbon, colloidal palladium, palladium on barium sulfate, palladium on barium carbonate, etc.], nickel catalysts [e.g. reduced nickel, nickel oxide, Raney nickel, etc.], cobalt catalysts [e.g. reduced cobalt, Raney cobalt, etc.], iron catalysts [e.g. reduced iron, Raney iron, etc.], copper catalysts [e.g. reduced copper, Raney copper, Ullman copper, etc.] and th like. In case that the N-protective group is benzyl, the reduction is preferably carried out in the presence of a combination of palladium catalysts [e.g. palladium black, palladium on carbon, etc.] and formic acid or its salt [e.g. ammonium formate, etc.]. The reduction is usually carried out in a conventional solvent which does not adversely influence the reaction such as water, methanol, ethanol, propanol, N,N-dimethylformamide, or a mixture thereof. Additionally, in case that the above-mentioned acids to be used in chemical reduction are in liquid, they can also be used as a solvent. Further, a suitable solvent to be used in catalytic reduction may be the above-mentioned solvent, and other conventional solvent such as diethyl ether, dioxane, tetrahydrofuran, etc. or a mixture thereof. The reaction temperature of this reduction is not critical and the reaction is usually carried out under cooling to heating. In this reaction, in case that the compound (If) having aryl which is substituted with alkoxy substituted with protected amino, N-protected amino(lower)alkanoylamino, N-protected piperazinylcarbonyl or N-protected guanidino for R- is used as a starting compound, the compound (Ig) having aryl which is substituted with alkoxy substituted with amino, amino(lower)alkanoylamino, piperazinylcarbonyl or guanidino for R may be obtained according to reaction condition. This case is included within the scope of this reaction. Process 6 The object compound (Ih) cr its salt can be prepared by reacting a compound (Ic) or its reactive derivative at the carboxy group or a salt thereof with an a ine or its salt. Suitable salt of amine may be an acid addition salt as exemplified for the compound (I) . Suitable salts of the compounds (Ih) and (Ic) and its reactive derivative at the carboxy group may be the same as those exemplified for the compound (I) . Suitable "amine" may be ammonia, substituted or unsubstituted lower alkylamine, substituted or unsubstituted N-containing heterocyclic compound, a heterocyclic group substituted with amino and the like. The substituted or unsubstituted lower alkylamine may be mono or di(lower)alkylamine (e.g. methylamine, ethylamine, propylamine, isopropylamine, butylamine, isobutylamine, pentylamine, hexylamine, dimethylamine, diethylamine, dipropylamine, dibutylamine, di-isopropylamine, dipentylamine, dihexylamine, etc.), pyridyl(lower)alkylamine, (e.g. pyridylmethylamine, etc.), lower alkylamino(lower)alkylamine (e.g. N-dimethylaminoethylamine, N-dimethylaminopropylamine, N-diethylaminoethyl-N-methylamine, etc.) , morpholino(lower)alkylamine (e.g. morpholinoethylamine, etc.) or the like. The substituted or unsubstituted N-containing heterocyclic compound may be a heterocyclic group substituted with amino (e.g. aminopyridine, N-methyl-N'- aminopiperazine, etc.), saturated 5 or 6-membered N-, or N- and S-, or N- and O-containing heterocyclic compound such as pyrrolidine, imidazolidine, piperidine, piperidone, piperazine, lower alkylaminopiperidine (e.g. dimethylaminopiperidine, etc.) , N-(lower)alkylhomopiperazine (e.g. N-methylhomopiperazine, etc.), N-(lower)alkylpiperazine (e.g. N-methylpiperazine, N-ethylpiperazine, etc.), morpholine, thiomorpholine, N-pyridylpiperazine, N-hydroxy(lower)alkoxy(lower)- alkylpiperazine (e.g. N-hydroxyethoxyethylpiperazine, etc.), N-pyrrolidinylcarbonyl(lower)alkylpiperazine (e.g. N-pyrrodidinylcarbonylmethylpiperazine, etc.), or the like, in which preferable one is N-methylpiperazine. This reaction can be carried out in substantially the same manner as Process 1, and therefore the reaction mode and reaction condition (e.g. solvent, reaction temperature, etc.) of this reaction are to be referred to those as explained in Process 1. Process 7 The object compound (Ii) or its salt can be prepared by reacting a compound (le) or its reactive derivative at the carboxy group or a salt thereof with an amine or its salt. Suitable salt of amine may be an acid addition salt as exemplified for the compound (I) . Suitable salts of the compounds (Ii) and (le) and its reactive derivative at the carboxy group may be the same as those exemplified for the compound (I) . This reaction can be carried out in substantially the same manners as Processes 1 and 6. and therefore the reaction mode and reaction condition (e.g. amine, solvent, reaction temperature, etc.) of this reaction are to be referred to those as explained in Processes 1 and 6. Process 8 The object compound (Ik) or its salt can be prepared by subjecting a compound (Ij) or its salt to debenzylation reaction. Suitable salts of the compounds (Ij) and (Ik) may be the same as those exemplified for the compound (I) . This reaction can be carried out in substantially the same manner as hydrolysis using an acid or catalytic reduction in Process 5. and therefore the.reaction mode and reaction condition (e.g. solvent, reaction temperature, etc.) of this reaction are to be referred to those as explained in hydrolysis using an acid or catalylic reduction in Process 5. In this catalytic reduction, in case that the compound (Ij) having nitro for R 3 is used as a starting compound, the compound (Ik) having amino for R 3 may be obtained according to reaction condition. This case is included within the scope of this reaction. Process 9 The object compound [Ii) or its salt can be prepared by reacting a compound (Ika) or its salt with a compound (VI) or its salt. Suitable salts of the compounds (Ika), (1$) and (VI) may be the same as those exemplified for the compound (I) . When the compound (VI) having halogen for Z 1 is used in this reaction, the reaction is preferably carried out in the presence of a base such as an alkali metal (e.g. sodium, potassium, etc.), an alkaline earth metal (e.g. magnesium, calcium, etc.), the hydride or hydroxide or carbonate or bicarbonate thereof. When the compound (VI) having hydroxy for Z* is used in this reaction, the reaction is preferably carried out in the presence of diethyl azodicarboxylate and triphenylphosphine. The reaction is usually carried out in a conventional solvent which does not adversely influence the reaction such as water, dioxane, alcohol (e.g. methanol, ethanol, etc.), acetonitrile, tetrahydrofuran, acetic acid, N,N- dimethylformamide, or a mixture thereof. The reaction temperature is not critical and the reaction can be carried out under cooling to heating. Process I Q The object compound (Im) or its salt can be prepared by reacting a compound (Iga) or its salt with an acylating agent. Suitable salts of the compounds (Iga) and (Im) may be the same as those exemplified for the compound (I) . The acylating agent may include an organic acid represented by the formula : R^-OH, in which R 11 is acyl or substituted acyl as illustrated above, or its reactive derivative. The suitable reactive derivative of organic acid may be a conventional one such as an acid halide [e.g. acid chloride, acid bromide, etc.], an acid azide, an acid anhydride containing intramolecular and intermolecular ones, an activated amide, an activated ester or the like. When free acid is used as an acylating agent, the acylation reaction may preferably be conducted in the presence of a conventional condensing agent such as N,N'-dicyclohexylcarbodiimide or the like. The reaction is usually carried out in a conventional solvent such as water, pyridine, acetone, dioxane, chloroform, methylene chloride, acetonitrile, ethylene chloride, tetrahydrofuran, ethyl acetate, N,N-dimethylformamide, pyridine or any other organic solvent which does not adversely influence the reaction, or a mixture thereof. The reaction is also preferably carried out in the presence of a conventional base such as triethyla ine, pyridine, sodium hydroxide or the like. The reaction temperature is not critical, and the reaction can be carried out under cooling to heating. Process U The object compound (In) or its salt can be prepared by reacting a compound (Igb) or its salt with lower alkanal or N-protected amino(lower)alkanal. in the presence of a reducing agent. Suitable salts of the compounds (Igb) and (In) may be the same as those exemplified for the compound (I) . Suitable lower alkanal may be C^-Cg alkanal such as formaldehyde, ethanal, propanal or the like, in which preferable one is formaldehyde. Suitable N-protected amino(lower)alkanal may be N- protected amino(C^-Cg)alkanal such as phthalimidopropanal or the like. Suitable reducing agent may be diborane, borane-organic amine complex [e.g. borane-pyridine complex, etc.], alkali metal cyanoborohydride [e.g. sodium cyanoborohydride, lithium cyanoborohydride, etc.], sodium borohydride and the like. The reaction is preferably carried out in the presence of molecular sieves. The reaction is usually carried out in a conventional solvent such as water, an alcohol [e.g. methanol, ethanol, etc.], dioxane, tetrahydrofuran, a mixture thereof or any other organic solvent which does not adversely influence the reaction. The reaction may also be carried out in an acidic condition [e.g. presence of acetic acid, sulfuric acid, etc.] and the reaction temperature is not critical, and the reaction is usually carried out under cooling to warming. Process 12 The object compound (Ip) or its salt can be prepared by subjecting a compound (lo) or its salt to reduction. Suitable salts of the compounds (lo) and (Ip) may be the same as those exemplified for the compound (I) . The reduction may include chemical reduction and catalytic reduction, which are carried out in a conventional manner. Suitable reducing agents to be used in chemical reduction are a metal [e.g. thin, zinc, iron, nickel, etc.], a combination of such metal and/or metallic compound [e.g. nickel chloride, chromium chloride. chromium acetate, etc.] and an organic or inorganic acid [e.g. formic acid, acetic acid, propionic acid, trifluoroacetic acid, p-toluenesulfonic acid, hydrochloric acid, hydrobromic acid, etc.], a combination of such metal and/or metallic compound and base [e.g. ammonia, ammonium chloride, sodium hydroxide, etc.], a metal hydride compound such as aluminum hydride compound [e.g. lithium aluminum hydride, sodium aluminum hydride, aluminum hydride, lithium trimethoxyaluminum hydride, lithium tri- t-butoxyaluminum hydride, etc.], borohydride compound [e.g. sodium borohydride, lithium borohydride, sodium cyanoborohydride, tetramethylammonium borohydride, borane, diborane, etc.], a phosphorus compound [e.g. phosphorus trichloride, phosphorus tribromide, triphenylphosphme, triethylphosphine, etc.] and the like. Suitable catalysts to be used in catalytic reduction are conventional ones such as platinum catalysts [e.g. platinum plate, spongy platinum, platinum black, colloidal platinum, platinum oxide, platinum wire, etc.], palladium catalyst [e.g. spongy palladium, palladium black, palladium oxide, palladium on carbon, colloidal palladium, palladium on barium sulfate, palladium on barium carbonate, etc.], nickel catalyst [e.g. reduced nickel, nickel oxide, Raney nickel, etc.], cobalt catalyst [e.g. reduced cobalt, Raney cobalt, etc.], iron catalyst [e.g. reduced iron, Raney iron, etc.], copper catalyst [e.g. reduced copper, Raney copper, Ullman copper, etc.], or the like. The reduction is usually carried out in a solvent. A suitable solvent to be used may be water, and alcohol [e.g. methanol, ethanol, propanol, etc.], acetonitrile or any other conventional organic solvent such as diethyl ether, dioxane, tetrahydrofuran, etc. or a mixture thereof. The reaction temperature is not critical, and the 1795 - 52 - reaction is preferably carried out under cooling to heating. Process 13 The object compound (Ir) or its salt can be prepared by subjecting a compound (Iq) or its salt to deacylation reaction. Suitable salts of the compounds (Iq) and (Ir) may be the same as those exemplified for the compound (I) . This reaction can be carried out in substantially the same manner as Process 3, and therefore the reaction mode and reaction condition (e.g. solvent, reaction temperature, etc.) of this reaction are to be referred to those as explained in Process 3. Process 14 The object compound (Is) or its salt can be prepared by reacting a compound (VII) or its salt with a compound (VIII) or its salt. Suitable salts of the compounds (Is), (VII) and (VIII) may be the same as those exemplified for the compound (I) . This reaction can be carried out in substantially the same manner as Process 9, and therefore the reaction mode and reaction condition (e.g. solvent, reaction temperature, etc.) of this reaction are to be referred to those as explained in Process 9. Process 15 The object compound (lu) or its salt can be prepared by reacting a compound (It) or its salt with an oxidizing agent. Suitable salts of the compounds (It) or (lu) may be the same as those exemplified for the compound (I) . The suitable oxidizing agent may be hydrogen peroxide, Jones reagent, peracid [e.g. peracetic acid, perbenzoic acid, m-chloroperbenzoic acid, etc.], chromic acid, potassium permanganate, alkali metal periodate [e.g. sodium periodate, etc.] and the like. This reaction is usually carried out in a solvent which does not adversely influence the reaction such as acetic acid, dichloromethane, acetone, ethyl acetate, chloroform, water, an alcohol [e.g. methanol, ethanol, etc.], a mixture thereof or the like. The reaction temperature is not critical, and the reaction is usually carried out under cooling to warming. Process 16 The object compound (Iw) or its salt can be prepared by subjecting a compound (Iv) or its salt to catalytic reduction. Suitable salts of the compounds (Iv) and (Iw) may be the same as those exemplified for the compound (I) . This reaction can be carried out in substantially the same manner as catalytic reduction in Process 5, and threfore the reaction mode and reaction condition (e.g. solvent, reaction temperature, etc.) of this reaction are to be referred to those as explained in catalytic reduction in Process 5. Process 17 The object compound (Iy) or its salt can be prepared (to be continued to the next page) by subjecting a compound (Ix) or its salt to debenzylation reaction. Suitable salts of the compounds (Ix) and (Iy) may be the same as those exemplified for the compound (I) . This reaction can be carried out in substantially the same manner as Process 8. and therefore the reaction mode and reaction condition (e.g. solvent, reaction temperature, etc.) of this reaction are to be referred to those as explained in Process 8. Process 18 The object compound (Iz) or its salt can be prepared by reacting a compound (Iy) or its salt with a compound (IX) or its salt. Suitable salts of the compounds (Iy) , (Iz) and (IX) may be the same as those exemplified for the compound (I) . This reaction can be carried out in substantially the same manner as Process 9. and therefore the reaction mode and reaction condition (e.g. solvent, reaction temperature, etc.) of this reaction are to be referred to those as explained in Process 9. Process 19 The object compound (1-2) or its salt can be prepared by subjecting a compound (I-l) or its salt to elimination reaction of the hydroxy protective group. Suitable salts of the compounds (I-l) and (1-2) may be the same as those exemplified for the compound (I) . Suitable hydroxy protective group may be benzyloxy, acyloxy, substituted acyloxy or the like. This reaction can be carried out in substantially the same manner as Processes 8 and 13. and therefore the reaction mode and reaction condition (e.g. solvent, reaction temperature, etc.) of this reaction are to be referred to those as explained in Processes 8 and 13. 795 - 55 - process 20 The object compound (1-3) or its salt can be prepared by reacting a compound (1-2) or its salt with a compound (X) or its salt. Suitable salts of the compounds (1-2), (1-3) and (X) may be the same as those exemplified for the compound (I) . This reaction can be carried out in substantially the same manner as Process 9. and therefore the reaction mode and reaction condition (e.g. solvent, reaction temperature, etc.) of this reaction are to be referred to those as explained in Process 9. Process 21 The object compound (1-4) or its salt can be prepared by subjecting a compound (I-3a) or its salt to deesterification reaction. Suitable salts of the compounds (I-3a) and (1-4) may be the same as those exemplified for the compound (I) . This reaction can be carried out in substantially the same manner as Process 3, and therefore the reaction mode and reaction condition (e.g. solvent, reaction temperature, etc.) of this reaction are to be referred to those as explained in Process 3. Process 22 The object compound (1-6) or its salt can be prepared by reacting a compound (1-5) or its salt with an alkyne compound in the presence of a palladium compound and a copper compound. Suitable salts of the compounds (1-5) and (1-6) may be the same as those exemplified for the compound (I) . Suitable alkyne compound may be lower alkyne optionally substituted with hydroxy, amino, protected amino, lower alkylsulfonyl, arylsulfonyl or the like, in which preferable one is 3-butyn-l-ol. Suitable palladium compound may be bis(triphenylphosphine)palladium(II) chloride, or the like. Suitable copper compound may be copper(I) iodide, or the like. The reaction is usually carried out in a conventional solvent which does not adversely influence the reaction such as tetrahydrofuran, dioxane, ethylamine, or a mixture thereof. The reaction temperature is not critical and the reaction is usually carried out under warming or heating. Process 23 The object compound (I-8a) or its salt can be prepared by reacting a compound (1-7) or its salt with a compound (XI) . Suitable salts of the compounds (1-7) and (I-8a) may be the same as those exemplified for the compound (I) . The reaction is preferably carried out in the presence of a base such as trialkylamine (e.g. trimethylamine, triethylamine, etc.) or the like. The reaction is usually carried out in a conventional solvent which does not adversely influence the reaction such as tetrahydrofuran, methylene chloride or the like. The reaction temperature is not critical and the reaction is usually carried out under cooling to heating. Process 24 The object compound (1-9) or its salt can be prepared by reacting a compound (1-8) or its salt with alkali metal phthalimide. Suitable salts of the compounds (1-8) and (1-9) may be the same as those exemplified for the compound (I) . The reaction is carried out in a conventional solvent which does not adversely influence the reaction such as dimethyl sulfoxide, N,N-dimethylformamide, or the like. The reaction temperature is not critical and the reaction is usually carried out under cooling to heating. Process 25 The object compound (1-10) or its salt can be prepared by reacting a compound (1-6) or its salt with a reducing agent. Suitable salts of the compounds (1-6) and (1-10) may be the same as those exemplified for the compound (I) . Suitable reducing agent may be a combination of nickel chloride and sodium borohydride, and the like. The reaction is carried out in a conventional solvent which does not adversely influence the reaction such as an alcohol (e.g. methanol, ethanol, etc.), tetrahydrofuran, or a mixture thereof. The reaction temperature is not critical and the reaction is usually carried out under cooling to warming. Process 26 The object compound (1-11) or its salt can be prepared by reacting a compound (II) or its salt with a compound (XII) or its salt. Suitable salts of the compounds (1-11), (II) and (XII) may be the same as those exemplified for the compound (I) . This reaction can be carried out in substantially the same manner as Process 11. and therefore the reaction mode and reaction condition (e.g. solvent, reaction temperature, etc.) of this reaction are to be referred to i those as explained in Process 11. \ Process 27 The object compound (1-13) or its salt can be prepared by reacting a compound (1-12) or its salt with a compound (XIII) in the presence of a base. Suitable salts of the compounds (1-12) and (1-13) may be the same as those exemplified for the compound (I) . Suitable base may be an alkali metal (e.g. sodium, potassium, etc.), an alkali metal hydride (e.g. sodium hydride), and the like. The reaction is carried out in a solvent such as N,N- dimethylformamide, tetrahydrofuran, dioxane, a mixture thereof or any other solvent which does not adversely influence the reaction. The reaction temperature is not critical and the reaction is usually carried out under cooling to warming. Process 28 The object compound (1-15) or its salt can be prepared by reacting a compound (1-14) or its salt with an acylating agent. Suitable salts of the compounds (1-14) and (1-15) may be the same as those exemplified for the compound (I) . This reaction can be carried out in substantially the same manner as Process 10. and therefore the reaction mode and reaction condition (e.g. solvent, reaction temperature, etc.) of this reaction are to be referred to those as explained in Process 10. Process 29 The object compound (1-17) or its salt can be prepared by reacting a compound (I-l6a) or its salt with a reducing agent. Suitable salts of the compounds (I-l6a) and (1-17) may be the same as those exemplified for the compound (I) . Suitable reducing agent may be alkali metal borohydride (e.g. sodium borohydride, etc.), and the like. The reaction is carried out in a solvent such as an alcohol (e.g. methanol, ethanol, etc.), tetrahydrofuran. or the like . The reaction temperature is not critical and the reaction is usually carried out under cooling to warming. Process 30 The object compound (1-18) or its salt can be prepared by reacting a compound (1-16) or its salt with an amine compound or its salt in the presence of a reducing agent. Suitable salts of the compounds (1-16) and (1-18) may be the same as those exemplified for the compound (I) . Suitable amine compound may be ammonia, N-lower alkylpiperazine, and the like. Suitable salt of amine compound may be an acid addition salt (e.g. acetate, hydrochloride, etc.), and the like. This reaction can be carried out in substantially the same manner as Process 11. and therefore the reaction mode and reaction condition (e.g. solvent, reaction temperature, etc.) of this reaction are to be referred to those as explained in Process 11. Process 31 The object compound (1-20) or its salt can be prepared by reacting a compound (1-19) or its reactive derivative at the carboxy group or a salt thereof with lower alkylamino(lower)alkanol. Suitable salts of the compounds (1-20) and (1-19) and its reactive derivative at the carboxy group may be the same as those exemplified for the compound (I) . Suitable lower alkylamino(lower)alkanol may be dimethylaminoethanol, and the like. This reaction can be carried out in substantially the same manner as Process 1. and therefore the reaction mode and reaction condition (e.g. solvent, reaction temperature, etc.) of this reaction are to be referred to those as explained in Process 1. Process 32 The object compound (1-22) or its salt can be prepared by reacting a compound (1-21) or its salt with a reducing agent. Suitable salts of the compounds (1-21) and (1-22) may be the same as those exemplified for the compound (I) . Suitable reducing agent may be diborane, lithium aluminum hydride and the like. The reaction is usually carried out in a solvent which does not adversely influence the reaction such as diethyl ether, tetrahydrofuran or the like. The reaction temperature is not critical and the reaction can be carried out under cooling to heating. Process 33 The object compound (1-23) or its salt can be prepared by subjecting a compound (1-22) or its salt to oxidation reaction. Suitable salts of the compounds (1-22) and (1-23) ma be the same as those exemplified for the compound (I) . Suitable oxidizing agent used in this reaction may b manganese dioxide, dimethyl sulfoxide, a mixture of dimethyl sulfoxide and oxalyl chloride and the like. The reaction is usually carried out in a conventiona solvent such as pentane, hexane, benzene, diethyl ether, dimethoxyethane, acetone, chloroform, dichlorom.ethane or any other solvent which does not adversely influence the reaction. Additionally in case that the above-mentioned ■oxidizing agent is liquid, it can be used as a solvent. In this reaction, in case that dimethyl sulfoxide or a mixture of dimethyl sulfoxide and oxalyl chloride is used as an oxidizing agent, the reaction is preferably carried out in the presence of alkali metal iodide (e.g. sodium iodide, etc.) and alkali metal carbonate (e.g. sodium carbonate) or tri(lower)alkylamine (e.g. triethylamine, etc.). The reaction temperature is not critical, and the reaction is usually carried out under cooling to heating. Process 34 The object compound (1-25) or its salt can be prepared by reacting a compound (1-24) or its salt with an azide compound. Suitable salts of the compounds (1-24) and (1-25) may be the same as those exemplified for the compound (I) . Suitable azide compound may be sodium azide, trimethyltin azide and the like. The reaction is usually carried out in a solvent which does not adversely influence the reaction such as dioxane, an aromatic hydrocarbon (e.g. benzene, toluene, xylene) or the like. The reaction temperature is not critical and the reaction is usually carried out under warming to heating. Process 35 The object compound (1-27) or its salt can be prepared by reacting a compound (1-26) or its salt with an isourea compound. Suitable salts of the- compounds (1-26) and (1-27) may be the same as those exemplified for the compound (I) . Suitable isourea compound may be O-alkylisourea (e.g. O-methylisourea, etc.) and the like. The reaction is usually carried out in a solvent which does not adversely influence the reaction such as an alcohol (e.g. methanol, ethanol, etc.) or the like. The reaction temperature is not critical and the reaction is usually carried out under warming to heating. Process 36 The object compound (1-29) or its salt can be prepared by subjecting a compound (1-28) or its salt to elimination reaction of the N-protective group. Suitable salts of the compounds (1-28) and (1-29) may be the same as those exemplified for the compound (I) . This reaction can be carried out in substantially the same manner as Process 5. and therefore the reaction mode and reaction condition (e.g. solvent, reaction temperature, etc.) of this reaction are to be referred to those as explained in Process 5. Process 37 The object compound (1-31) or its salt can be prepared by reacting a compound (1-30) or its salt with N- lower alkylpiperazine, dimethylaminopiperidine, ammonia or N,N-dimethylformamide. Suitable salts of the compounds (1-30) and (1-31) may be the same as those exemplified for the compound (I) . The reaction is usually carried out in a solvent which does not adversely influence the reaction such as N,N-dimethylformamide, dioxane or the like. The reaction temperature is not critical and the reaction is usually carried out under warming to heating. Process 33 The object compound (I-3a) or its salt can be prepared by reacting a compound (1-4) or its reactive derivative at the carboxy group or a salt thereof with a hydroxy compound or a diazo compound. Suitable salts of the compounds (I-3a) and (1-4) and its reactive derivative at the carboxy group may be the same as those exemplified for the compound (I) . Suitable reactive derivative at the carboxy group (1-4) may be acid halide (e.g. acid chloride, acid bromide, etc.) and the like. Suitable hydroxy compound may be an alcohol (e.g. methanol, ethanol, etc.), phenol, naphthol and the like. Suitable diazo compound may be methyldiazomethane, trimethylsilyldiazomethane and the like. The reaction is usually carried out in a conventional solvent such as diethyl ether, tetrahydrofuran, dioxane, methylene chloride, or any other organic solvent which does not adversely influence the reaction. Additionally, in case that the above-mentioned hydroxy compound is in liquid, it can also be used as a solvent. The reaction temperature is not critical and the reaction is usually carried out under cooling to heating. Process 39 The object compound (1-32) or its salt can be prepared by reacting a compound (1-4) or its reactive derivative at the carboxy group or a salt thereof with an amine. Suitable salts of the compounds (1-32) and (1-4) and its reactive derivative at the carboxy group may be the same as those exemplified for the compound (I) . Suitable amine may be ammonia, lower alkylamine (e.g. methylamine, dimethylamine, etc.) and the like. This reaction can be carried out in substantially the same manner as Process 6. and therefore the reaction mode and reaction condition (e.g. solvent, reaction temperature, etc.) of this reaction are to be referred to those as explained in Process 6. The compounds obtained by the above processes can be isolated and purified by a conventional method such as pulverization, recrystallization, column chromatography, reprecipitation, or the like. It is to be noted that the compound (I) and the other compounds may include one or more stereoisomer(s) such as optical isomer(s) or geometrical isomer(s) due to asymmetric carbon atom(s) and double bond(s), and all of such isomers and mixture thereof are included within the scope of this invention. Additionally, it is to be noted that any hydrate of the compound (I) is also included within the scope of this invention. The object compound (I) and pharmaceutically acceptable salts thereof possess activities as vasopressin antagonistic activity, vasodilating activity, hypotensive activity, activity for inhibiting saccharide release in liver, activity for inhibiting growth of mesangium cells, water diuretic activity, platelet agglutination inhibitory activity, oxytocin antagonistic activity and the like, and are useful for the treatment and/or prevention of hypertension, heart failure, renal insufficiency, edema, ascites, vasopressin parasecretion syndrome, hepato- cirrhosis, hyponatremia, hypokalemia, diabetic, circulation disorder, cerebrovascular disease (e.g. cerebral edema, cerebral infarction, etc.), Meniere's syndrome (e.g. Meniere's disease, et.), motion sickness and the like in human beings and animals. In order to illustrate, the usefulness of the object compound (I), the pharmacological data of the compound (I) are shown in the following. Test 1 Vasopressin 1 (VI) receptor binding (i) Test Method : Blood was obtained by venipuncture from normal subjects. Platelet-rich plasma (PRP) was prepared by centrifugation of whole blood at 200 xg for 10 minutes. PRP was centrifuged at 45,000 xg for 30 minutes. The remaining pellet was resuspended in 10 volume of ice cold 100 mM Tris-HCl (pH 7.4) buffer (containing 5 mM MgCl 2 , 0.1% bovine serum albumin and 1 mM EGTA) , and centrifuged at 45,000 xg for 30 minutes again. The final pellet was resuspended in 100 mM Tris-HCl buffer. The resulting membrane preparation was used immediately for the binding assay. Competition assays were conducted at equilibrium (15 minutes at 30°C) by using 1.5 nM 3 H-vasopressin (40-87 Ci/mmol; New England Nuclear) in 100 M Tris-HCl (pH 7.4) buffer. Nonspecific binding was determined by using 1 μM vasopressin. After incubation, reaction was terminated by adding 5 ml of ice-cold 100 mM Tris-HCl (pH 7.4) buffer, and then filtered rapidly through Whatman glass filter (GF/C) . The filter was washed twice with the same buffer. The glass filter was mixed with liquid scintilation cocktail, and radioactivity was counted in a liquid scintilation counter. Competition activity of the test compound was represented by IC50 values. (ii) Test Result : Test 2 Vasopressin 2 (V2) receptor binding (i) Test Method : For binding assays, the receptor cDNA was permanently expressed in Chinese hamster ovary (CHO) cells. CHO cells were transfected with a vector directing expression of the cDNA for the human V2 receptor and the clonal cell lines expressing human V2 receptor was established essentially as described previously (Nakajima, Y., et. al. J. Biol. Chem., 1992, 267, 2437) . DNA-transfected cells were harvested and homogenized in ice cold 250 mM sucrose buffer containing 25 mM Tris- HCl (pH 7.4), 10 mM MgCl 2 , 1 mM EDTA and 5 μg/ml p-amidinophenylmethylsulfonyl fluoride (A-PMSF) . The homogenate was centrifuged at 500 xg for 10 minutes. The supernatant was centrifuged at 100,000 xg for 1 hour. The final pellet was suspended in 25 mM Tris-HCl (pH 7.4) buffer (containing 10 mM MgCl-., 1 mM EDTA and 5 μg/ml A-PMSF), and stored in small aliquots at -80 β C. Competition assays were conducted at equilibrium (2 hours at 22°C) by using 0.5 nM 3 H-vasopressin (40-87 Ci/mmol, New England Nuclear) in 100 mM Tris-HCl (pH 7.4) buffer (containing 5 mM MgCl 2 , 5 μg/ml A-PMSF, 4 μg/ml leupeptin, 40 μg/ml bacitracin, 20 μg/ml chymostatin and 0.1! bovine serum albumin). Nonspecific binding was determined by using 1 μM vasopressin. After incubation, reaction mixture was rapidly filtered through Whatman C glass filter (GF/C) . The filter was washed twice with the same buffer. The radioactivity was counted in a liquid scintilation counter. Competition activity of the test compound was represented by IC50 values. 5 (ii) Test Result For therapeutic purpose, the compound (I) of the present invention can be used in a form of pharmaceutical preparation containing one of said compounds, as an active ingredient, in admixture with a pharmaceutically acceptable carrier such as an organic or inorganic solid, semi-solid or liquid excipient suitable for oral, parenteral or external (topical) administration. The pharmaceutical preparations may be capsules, tablets, dragees, granules, suppositories, solution, lotion, suspension, emulsion, ointment, gel, or the like. If desires, there may be included in these preparations, auxiliary substances, stabilizing agents, wetting or emulsifying agents, buffers and other commonly used additives. While the dosage of the compound (I) will vary depending upon the age and condition of the patient, an average single dose of about 0.1 mg, 1 mg, 10 mg, 50 mg, 100 mg, 250 mg, 500 mg and 1000 mg of the compound (I) may be effective for treating the above-mentioned diseases. In general, amounts between 0.1 mg/body and about 1,000 mg/body may be administered per day. The following Preparations and Examples are given for the purpose of illustrating this invention. Preparation 1 To a solution of [N-methyl-N-(4-nitrobenzoyl]-2- hydroxyaniline (1.2 g) in N,N-dimethylformamide (30 ml) was added potassium carbonate (1.22 g) , ethyl 6-bromohexanoate (1.03 g) and sodium iodide (catalytic amount) at 60°C. The reaction mixture was stirred at same temperature for 8 hours. The reaction mixture was cooled in an ice bath and quenched with IN hydrochloric acid (10 ml) and water (30 ml) . The mixture was extracted with ethyl acetate. The organic phase was washed with water and brine. The organic solution was dried over magnesium sulfate. The solvent was removed by evaporation to give 2- (5-ethoxycarbonylpent-l-yloxy)-[N-methyl-N-(4- nitrobenzoyl) ]aniline (1.7 g) . NMR (CDC1 3 , δ) : 1.26 (3H, t, J=7.5Hz), 1.45-1.58 (2H, m) , 1.67-1.76 (2H, ) , 1.79-1.88 (2H, m) , 2.34 (2H, t, J=7.5Hz), 3.38 (3H, s) , 3.84-4.00 (2H, m), 4.13 (2H, t) , 6.72-6.82 (2H, m) , 7.01 (1H, d, J=7Hz), 7.17 (1H, t, J=7Hz) , 7.45 (2H, d, J=8.5Hz), 7.98 (2H, d, J=8.5Hz) Preparation 2 A solution of 3-methoxy-4-nitro-N-[2-(5- ethoxycarbonylpent-1-yloxy)-4-methylphenyl]-N- methylbenzamide (7.6 g) in ethanol (76 ml) was treated with IN sodium hydroxide solution (33 ml) at ambient temperature and the mixture was stirred at the same temperature for 6 hours. -The reaction was quenched by the dropwise addition of IN hydrochloric acid (35 ml) . The mixture was concentrated and the residue was dissolved in a mixture of ethyl acetate and IN hydrochloric acid. The extracted organic layer was washed with brine and dried over magnesium sulfate. The suspension was filtered and the solvent was removed by evaporation to give 3-methoxy- 4-nitro-N-[2-(5-carboxypent-l-yloxy)-4-methylphenyl]-N- methylbenzamide (7 . 1 g) as an oil . NMR (CDC1 3 , δ) : 1 .48-1 . 63 (2H, m) , 1 . 66-1 .91 (4H, m) , 2.28 (3H, s) , 2.41 (2H, t, J=7Hz) , 3.34 (3H, s ) , 3 . 78 (3H, s) , 3 . 81-3.98 (2H, m) , 6.58- 6. 67 (2H, m) , 6. 89 ( 1H, d, J=8Hz ) , 6. 94 (1H, d, J=8Hz) , 7 . 09 (1H, s) , 7 . 61 (1H, d, J=8Hz ) Preparation 3 3-Methoxy-4-nitro-N-[2-(5-carboxypent-l-yloxy)-4- methylphenyl]-N-methylbenzamide (5.2 g) , 1-methylpiperazine (1.45 g) and 1-hydroxybenzotriazole (1.96 g) were dissolved in N,N-dimethylformamide (50 ml) and the solution was cooled in an ice bath. To the mixture was added N-ethyl-N'-(3-dimethylaminopropyl)- carbodiimide hydrochloride (2.78 g) and the solution was stirred at the same temperature for 30 minutes. The reaction mixture was allowed to warm to ambient temperature and stirring was continued for additional 20 hours. The reaction mixture was diluted with ethyl acetate and the solution was washed successively with saturated sodium hydrogen carbonate and brine, and dried over sodium sulfate. The sodium sulfate was removed and the solvent was removed by evaporation to give oil. The crude material was subjected to a silica gel column chromatography (SiO-; 120 g, 2% methanol in chloroform) to give 3-methoxy-4-nitro-N-methyl-N-[4-methyl-2-[5- (4- methylpiperazin-1-ylcarbonyl)pent-1-yloxy]phenyl]benzamide (6.2 g) . • NMR (CDCI3, δ) : 1.43-1.60 (2H, m) , 1.60-1.92 (4H, m), 2.28 (3H, s), 2.30 (3H, s) , 2.25-2.47 (6H, m), 3.34 (3H, s) , 3.44-3.54 (2H, m) , 3.58-3.70 (2H, m), 3.78 (3H, s) , 3.82-4.03 (2H, m), 6.56- 6.66 (2H, m), 6.86 (1H, d, J=8Hz) , 6.94 (1H, d, J=8Hz), 7.07 (1H, s), 7.61 (1H, d, J=8Hz) Preparation 4 A mixture of 3-methoxy-4-nitro-N-methyl-N-[4-methyl- 2-[5-(4-methylpiperazin-l-ylcarbonyl)pent-l- yloxy]phenyl]benzamide (6.2 g) and iron powder (3.43 g) in a mixture of ethanol (65 ml) and ethyl acetate (6 ml) was refluxed for 2 hours. After being cooled to ambient temperature, the solution was filtered through a bed of Celite and the filtrate was evaporated in vacuo. The residue was diluted with ethyl acetate and the solution was washed with saturated sodium hydrogen carbonate and brine, and dried over magnesium sulfate. The solvent was evaporated in vacuo to give 4-amino-3-methoxy-N-methyl-N- [4-methyl-2-[5-(4-methylpiperazin-l-ylcarbonyl)pent-l- yloxy]phenyl]benzamide (4.7 g) . NMR (CDC1 3 , δ) : 1.43-1.58 (2H, m) , 1.61-1.91 (4H, ) , 2.26 (3H, s), 2.30 (3H, s) , 2.23-2.44 (6H, ), 3.29 (3H, s), 3.41-3.53 (2H, ) , 3.61 (3H, s), 3.57-3.68 (2H, m) , 3.75-4.03 (4H, m) , 6.36- 6.46 (1H, m) , 6.53-6.67 (2H, m) , 6.76-6.89 (3H, ) Preparation 5 The following compounds were obtained according to a similar manner to that of Preparation 4. 1) 4-Amino-N-methyl-N-[2-(5-ethoxycarbonylpent-l- yloxy)phenylbenzamide NMR (CDCI3, δ) : 1.26 (3H, t, J=7.5Hz), 1.41-1.54 (2H, m) , 1.62-1.73 (2H, m) , 1.75-1.84 (2H, m) , 2.32 (2H, t, J=7.5Hz), 3.30 (3H, s) , 3.84 (2H, br) , 3.90 (2H, br) , 4.13 (2H, t) , 6.38 (2H, d, J=8.5Hz), 6.79 (2H, d, J=8.5Hz), 6.99 (2H, s) , 7.09-7.18 (3H, m) 2) 4-Amino-3-methoxy-N-methyl-N-[2-[5-(4- dimethylaminopiperidin-1-yl) carbonylpent-1-yloxy]-4- methylphenyl]benzamide NMR (CDC1 3 , δ) : 1.29-1.95 (10H, ) , 2.23-2.43 (12H, ) , 2.57 (1H, m) , 3.01 (1H, ) , 3.31 (3H, s) , 3.62 (3H, s), 3.73-4.03 (5H, ) , 4.63 (IK, m) , 6.42 (1H, d, J=9Hz), 6.54-6.67 (2H, m) , 6.77- 6.89 (3H, m) 3) 4-Amir.o-N- [2- (5-ethoxycarbonylpent-l-yl)oxy-4- methyljphenyl-N-methylbenzamide MASS (m/z) : 399 (M+l) 4) 4-Amino-N-methyl-N- [4-methyl-2- [4- (4-methylpiperazin- 1-yl) carbonyl]phenylmethoxy]phenylbenzamide NMR (CDCI3, δ) : 2.27 (3H, s) , 2.32 (3H, s) , 2.35- 2.55 (4H, m), 3.31 (3H, s), 3.38-3.54 (2H, m) , 3.66-3.87 (4H, m) , 4.90-5.10 (2H, m) , 6.38 (2H, d, J=8Hz), 6.62-6.69 (2H, m) , 6.94 (1H, d, ϋ=7H∑), 7.13 (2H, d, J=8Hz) , 7.31-7.43 (4H, m) 5) 2- (4-Methoxycarbonyl)phenylmethoxy-4-methylamine NMR (CDCI3, δ) : 2.24 (3H, s) , 3.90 (3H, s), 5.11 (3H, s), 6.60-6.68 (3H, m) , 7.50 (2H, d, J=8Hz) , 8.05 (2H, d, J=8Hz) 6) 4-Amino-3-methoxy-N-methyl-N- [4-methyl-2- [4- (4- methylpiperazin-1-yl) carbonyl]phenylmethoxy] - phenylbenzamide NMR (CDCI3, δ) : 2.28 (3H, s) , 2.33 (3H, s) , 2.37- 2.53 (4H, m) , 3.36 (3H, s) , 3.41-3.54 (2H, m) , 3.57 (3H, s), 3.65-3.90 (4H, m) , 4.90 (1H, d, J=14Hz), 5.06 (1H, d, J=14Hz) , 6.38 (1H, d, J=7Hz), 6.62-6.70 (2H, ) , 6.78 (1H, d, J=7Hz) , 6.84 (1H, s), 6.98 (1H, d, J=7Hz) , 7.33 (2H, d, J=8Hz), 7.41 (2H, d, J=8Hz) 7) Methyl 4-[(E and Z)-2-(2-aminophenyl)ethen-1- yl]benzoate NMR (CDC1 3 , δ) : 3.72 (2H, br) , 3.86 (3Hx2/3, s), 3.90 (3Hxl/3, s), 6.57-7.43 (7H, ) , 7.55 (1H, d, J=7Hz), 7.86 (1H, d, J=7Hz) , 8.01 (7H, d) 8) 4-Amino-3-methoxy-N-[(E and Z)-2-(4-methoxycarbonyl- phenyl)ethen-l-yl]phenyl-N-methylbenzamide NMR (CDC1 3 , δ) : 3.39 (3Hx2/3, s) , 3.40 (3Hxl/3, s) , 3.50 (3Hx2/3, s) , 3.51 (3Hxl/3, s) , 3.81-3.96 (2H, m), 3.84 (3Hx2/3, s) , 3.41 (3Hxl/3, s) , 6.30-8.05 (13H, m) 9) 4-Amino-3-methoxy-N-[2-(4-methoxycarbonyl)- phenylmethoxy-4-methyl]phenyl-N-methylbenzamide NMR (CDCI3, δ) : 2.21 (3H, s) , 3.34 (3H, s) , 3.50 (3H, s), 3.83 (2H, s) , 3.90 (3H, s) , 4.79-5.14 (2H, m) , 6.37 (1H, d, J=7Hz) , 6.60 (1H, s) , 6.70 (1H, d, J=7Hz), 6.77 (1H, d, J=7Hz) , 6.81 (1H, s), 6.99 (1H, d, J=7Hz) , 7.34 (2H, d, J=8Hz) , 8.01 (2K, d, J=8Hz) 10) 2-[3-(Ethoxycarbonylmethyl)oxyprop-1-yl]oxyaniline NMR (CDCI3, δ) : 1.27 (3H, t, J=7.5Hz), 2.08-2.28 (2H, m) , 3.72 (2H, t, J=7.5Hz), 3.79 (2H, s), 4.09 (2H, s), 4.14 (2H, t, J=7.5Hz), 4.21 (2H, q, J=7.5Hz), 6.65-6.82 (4H, m) II) 4-Amino-3-methoxy-N-[2-[3-(ethoxycarbonylmethyl)- oxyprop-l-yl]oxy]phenyl-N-methylbenzamide NMR (CDCI3, δ) : 1.26 (3H, t, J=7.5Hz), 2.03-2.15 (2H, m) , 3.31 (3H, s) , 3.61 (3H, s), 3.69-3.77 (4H, m) , 4.02 (2H, s) , 4.20 (2H, q, J=7.5Hz), 6.41 (1H, d, J=7.5Hz), 6.64-6.89 (4H, m) , 7.00 (IK, d, J=7Hz), 7.13 (1H, t, J=7Hz) 795 - 73 - 12) 2-[ (E)-5-Ethoxycarbonyl-4-penten-l-yl]oxy-4- methylaniline NMR (CDC1 3 , δ) : 1.29 (3H, t, J=7.5Hz), 1.90-2.05 (2H, m), 2.23 (3H, s), 2.35-2.50 (2H, m), 3.65 (2H, br), 4.00 (2H, t, J=7.5Hz), 4.18 (2H, q, J=7.5Hz), 5.98 (1H, d, J=15Hz) , 6.53-6.67 (2H, m), 6.81 (1H, s), 7.00 (1H, dt, J=15, 7.5Hz) 13) 4-Amino-3-methoxy-N-[2-[(E)-5-ethoxycarbonyl-4- penten-1-yl]oxy-4-methyl]phenyl-N-methylbenzamide NMR (CDCI3, δ) : 1.27 (3H, t, J=7.5Hz), 1.84-1.98 (2H, m), 2.36 (3H, s) , 2.31-2.41 (2K, m), 3.29 (3H, s), 3.62 (3H, s) , 3.75-3.96 (4H, m), 4.18 (2H, q, J=7.5Hz), 5.84 (IK, d, J=15Hz), 6.40 (1H, d, J=7Hz), 6.58-6.63 (2H, m) , 6.78-7.01 (4H, ) 14) 2-(5-Ethoxycarbonylpent-l-yloxy)-4-methylaniline NMR (CDCI3, δ) : 1.26 (3H, t, J=7Hz) , 1.45-1.60 (2H, m), 1.63-1.89 (4H, m), 2.25 (3H, s), 2.33 (2H, t, J=7KZ), 3.98 (2H, t, J=7Hz), 4.13 (2H, q, J=7Hz), 6.54-6.68 (3H, m) 15) 3-Methoxy-4-amino-N-(2-benzyloxy-4-methylphenyl)-N- methylbenzamide NMR (CDCI3, δ) : 2.28 (3H, s) , 3.32 (3K, s) , 3.49 (3H, s), 3.83 (2H, br) , 4.80-5.11 (2H, br) , 6.34 (IK, d, J=8Hz), 6.62-6.84 (5H, m) , 6.92 (1H, d, J=8Hz), 7.25-7.39 (4H, m) 16) 4-Amino-3-methyl-N-methyl-N-[2-[5-(4-methylpiperazin- 1-yl)carbonylpent-l-yloxy]-4-methylphenyl]benzamide NMR (CDCI3, δ) : 1.48-1.59 (2H, ) , 1.63-1.88 (4H, m), 2.00 (3H, s), 2.28 (3K, s) , 2.30 (3H, s) , 2.32-2.40 (6H, m) , 3.29 (3H, s), 3.43-3.48 (2H, 95 - 74 - m), 3.62 (4H, br), 3.90 (2H, br) , 6.32 (1H, d, J=7Hz), 6.56-6.61 (2H, m) , 6.83 (1H, d, J=7Hz) , 6.90 (1H, d, J=7Hz), 7.17 (1H, s) 17) 4-Amino-3-hydroxy-N-methyl-N-[2-[5-(4- methylpiperazin-1-yl)carbonylpent-1-yloxy]-4- methylphenyl]benzamide NMR (CDC1 3 , δ) : 1.62 (6H, br) , 2.28 (3K, s), 2.31 (3H, s), 2.38-2.49 (6H, ) , 3.28 (3H, s) , 3.52 (2H, br), 3.67 (2H, br) , 3.78 (2H, br) , 3.91 (2H, br), 6.32-6.38 (1H, m) , 6.57-6.67 (3H, m) , 7.00-7.03 (2H, m) Preparation 6 The following compounds were obtained by reacting the compounds, which were prepared according to a similar manner to that of Preparation 4, with hydrogen chloride. 1) Benzyl 4-amino-3-benzyloxybenzoate hydrochloride NMR (DMSO-dg, δ) : 5.18 (2H, s) , 5.25 (2H, s) , 5.98 (2H, br), 6.78 (1H, d, J=7Hz), 7.29-7.52 (12H, m) 2) Methyl 2-amino-5-thiophenecarboxylate hydrochloride NMR (DMSO-dg, δ) : 3.68 (3H, s) , 5.90 (1H, d, J=5Hz), 7.32-7.37 (2K, m) Preparation 7 The following compounds were obtained according to a similar manner to that of Preparation 1. 1) 2-(3-Hydroxyprop-l-yl)oxynitrobenzene NMR (CDCI3, δ) : 2.07-2.14 (2H, m) , 2.22 (1H, t, J=7.5Hz), 3.90 (2H, dd, J=7.5, 7.5Hz), 4.29 (2H, t, J=7Hz), 7.01 (IK, t, J=7Hz), 7.12 (1H, t. J=7Hz) , 7 .54 (1H, t, J=7Hz) , 7 . 89 (1H, d, J=7Hz) 2) 3- (3-Ethoxycarbonylprop-l-yl)oxy-4-nitrotoluene NMR (CDC1 3 , δ) : 1.24 (3H, t, J=7.5Hz), 2.09-2.19 (2H, m), 2.56 (2H, t, J=7.5Hz), 4.08-4.20 (4H, m) , 6.81 (IK, d, J=7Hz) , 6.97 (IK, s) , 7.77 (7H, d) 3) Benzyl 2- (3-phthalimidopropoxy)benzoate NMR (CDCI3, δ) : 2.08-2.23 (2H, m) , 3.85 (2H, t, J=7Hz), 4.07 (2H, t, J=7Hz) , 5.32 (2H, s) , 6.86- 7.02 (2K, m) , 7.20-7.50 (6H, m) , 7.61-7.74 (2H, m) , 7.75-7.90 (3K, m) 4) 2- (5-Ethoxycarbonylpent-l-yloxy) -4-methylnitrobenzene NMR (CDCI3, δ) : 1.25 (3H, t, J=7Hz) , 1.46-1.63 (2H, m), 1.63-1.78 (2H, ) , 1.79-1.94 (2K, m) , 2.34 (2H, t, J=7Hz), 2.40 (3H, s) , 4.00-4.19 (4H, m) , 6.80 (IK, d, J=9Hz), 6.84 (1H, s) , 7.76 (IK, d, J=9Hz) 5) 2-Benzyloxy-N-tert-butoxycarbonylaniline NMR (CDCI3, δ) : 1.49 (9H, s) , 5.10 (2H, s) , 6.88- 6.98 (3H, m) , 7.09 (1H, s) , 7.32-7.43 (5H, m) , 8.10 (IK, br) 6) Methyl 4- [N- [2- [ (3-tert-butoxycarbonylaminoprop-l- yl)oxy]phenyl] -tert-butoxycarbonylamino]methyl-3- ethoxybenzoate NMR (CDCI3, δ) : 1.33 and 1.42 (total 18H, s), 1.92-2.00 (2H, m) , 3.26-3.32 (2H, m) , 3.70 and 3.77 (total 3H, s) , 3.90 (3H, s) , 4.03 (2H, br) , 4.72 (2K, br), 6.72-6.97 (3K, m) , 7.10-7.23 (2H, m) , 7.40-7.53 (2H, m) , 7.62 (1H, br) 7) l-Benzyloxy-2- (3-tert-butoxycarbonylaminoprop-l- yi) oxybenzene NMR (CDC1 3 , δ) : 1 .40 and 1 .47 (9K, s) , 1 .98-2.06 (2K, m) , 3 .23-3.47 (2H, m) , 4 . 10 (2K, t, J=6Hz) , 5. 18 (2K, s) , 5.42 (1H, br) , 6. 82-6. 90 (4K, ) , 7 .28-7 . 47 (5H, m) 8) Methyl 4-[2-[ (3-tert-butoxycarbonylaminoprop-l- yl)oxymethyl-3-methoxybenzoate NMR (CDCI3, δ) : 1.38 (9H, s) , 2.02 (2H, br) , 3.38 (2H, br), 3.90-3.92 (6H, m) , 4.10-4.16 (2H, m) , 5.23 (1H, s), 5.25 (1H, s), 5.44 (1H, br) , 6.83 6.92 (4H, m) , 7.53-7.57 (2H, m) , 7.65-7.69 (1H, ir.) 9) Benzyl 3-benzyloxy-4-nitrobenzoate NMR (CDCI3, δ) : 5.28 (2K, s) , 5.89 (2H, s), 7.30- 7.48 (9K, m) , 7.70-7.73 (1H, m) , 7.81-7.85 (2H, m) 10) Benzyl 3-benzyloxy-4-[2-[ (3-tert-butoxycarbonylamino prop-l-yl)oxy]benzoyl]aminobenzoate NMR (CDCI3, δ) : 1.38 (9K, s), 1.60-1.70 (2H, m) , 2.95-3.02 (2H, m) , 3.80 (2H, t, J=6Kz) , 4.42 (1H, br), 5.22 (2H, s), 5.38 (2H, s), 6.93 (1H, d, J=8Hz), 7.10 (1H, t, J=7Hz), 7.32-7.50 (12H, m) , 7.71-7.72 (1H, m) , 7.80-7.83 (1H, m) , 8.23 8.28 (IK, m) , 8.78 (IH, d, J=7Hz) 11) Methyl 2-[2-[ (3-tert-butoxycarbonylaminoprop-l- yl)oxy]benzoyl]amino-5-thiophenecarboxylate This compound was used for further reaction without purification. 95 - 77 - Preparation 8 The following compounds were obtained according to a similar manner to that of Preparation 2. 1) 4-[N-Methyl-2- [ (3-tert-butoxycarbonyiaminoprop-l- yi)oxy]benzoyl]amino-3-methoxybenzoic acid NMR (CDC1 3 , δ) : 1.45 (9K, s), 1.97-2.06 (2H, m) , 3.33-3.42 (5H, m) , 3.87 (3H, s) , 3.98-4.07 (2H, ) , 5.27-5.35 (1H, br) , 6.67-6.76 (2K, m) , 7.03- 7.19 (3H, m) , 7.44-7.50 (2H, m) ESI-MASS (m/z) : 459 (M+H) 2) 4-Nitro-N-[2- (4-carboxyphenyl)methoxy-4- ethyl]phenyl-N-methylbenzamide NMR (CDC1 3 , δ) : 2.27 (3K, s) , 3.40 (3H, s), 4.97 (IK, d, J=14Kz), 5.10 (IK, d, J=14Hz) , 6.65 (1H, s), 6.6S (1H, d, J=7Hz), 7.00 (1H, d, J=7Hz) , 7.33-7.49 (4H, m) , 7.97 (2K, d, J=8Hz) , 8.10 (2K, d, J=8Hz) 3) 3-Methoxy-4-nitro-N- [2- (4-carboxy)phenylmethoxy-4- methyl]phenyl-N-methylbenzamide NMR (CDC1 3 , δ) : 2.30 (3H, s), 3.42 (3H, s) , 3.61 (3K, s), 4.92 (1H, d, J=14Hz) , 5.11 (1H, d, J=14Hz), 6.65 (IK, s) , 6.73 (1H, d, J=7Hz) , 6.86 (1H, d, J=7Hz), 7.02-7.08 (2H, m) , 7.48 (2H, d, J=8Hz), 7.54 (1H, d, J=7Hz) , 8.16 (2H, d, J=8Hz) 4) 2- (4-Carboxyphenylmethyl)oxy-4-methyl-N,N- dimethylaniline NMR (CDCI3, δ) : 2.31 (3H, s) , 2.89 (6H, s) , 5.08 (2H, s), 6.76-7.82 (2H, m) , 7.03 (1H, d, J=7Hz) , 7.40 (2H, d, J=8Hz), 7.77 (2K, ά, J=8Hz) 5) 2- [3- (4-Methoxyphenyl)methoxypropyl-l-yl]thiobenzoic acid NMR (CDCI3, δ) : 1 .95-2.06 (2K, ) , 3.03 (2H, t, J=7 .5Hz) , 3 .59 (2H, t, J=7.5Hz) , 3 .77 (3H, s) , 4 .46 (2H, s) , 6.89 (2H, d, J=8Hz) , 7.19 (1H, t, J=7Hz) , 7.16 (2H, d, J=8Kz) , 7.36 (1H, d, J=7Hz) , 7 .45 (1H, t, J=7Kz) , 8.10 (1H, d, J=7Hz) 6) 4-Amino-3-methoxy-N- [2- (4-carboxy) phenylmethoxy-4- methyl ] phenyl -N-methylbenzamide NMR (DMSO-dg, δ) : 2.21 (3K, s) , 3.15 (3H, s) , 3.41 (3H, s) , 4 .95-5.23 (2H, ) , 6.33 (1H, d, J=7Hz) , 6. 63-6.72 (3H, m) , 6.87 (1H, s) , 7 .04 (1H, d, J=7Hz) , 7 .44 (2H, d, J=8Hz) , 7.95 (2H, d, J=8Hz) 7) 4-Amino-3-methoxy-N- [2- [3- (carboxymethyl) oxyprop-1- yl ] oxyphenyl -N-methylbenzamide NMR (CDCI3, δ) : 2. 00-2.12 (2H, m) , 3.32 (3H, s) , 3.60 (3K, s), 3.63-3.74 (2H, m) , 3.89-4.14 (2H, m) , 4.05 (2K, s), 4.50 (2H, br) , 6.40 (1H, d, J=7Hz), 6.80-6.95 (4H, m) , 6.95 (IK, d, J=7Hz) , 7.16 (1H, t, J=7Hz) 8) 4-Amino-3-methoxy-N-[2-[ (E)-5-ethoxycarbonyl-4- penten-l-yl]oxy-4-methyl]phenyl-N-methylbenzamide NMR (CDCI3, δ) : 1.87-1.99 (2H, m) , 2.28 (3H, s) , 2.34-2.45 (2H, m) , 3.31 (3H, s) , 3.61 (3H, s) , 3.71-4.00 (2H, m) , 5.87 (1H, d, J=15Hz) , 6.41 (1H, d, J=7Hz), 6.57-6.68 (2H, m) , 6.80-7.12 (4H, m) 9) 3- (5-Carboxypent-l-yloxy)-4- (tert- butoxycarbonylamino)toluene NMR (CDC1 2 , δ) : 1.45-1.63 (11H, m) , 1.64-1.95 (4H, m), 2.28 (3H, s) , 2.42 (2K, t, J=7Hz) , 3.99 (2H, t, J=7Hz), 6.65 (1H, s) , 6.72 (1H, d, J=8Hz) , 6.98 (1H, s), 7.87 (1H, m) 10) 4-[ (2-3enzyloxy)benzoyljamino-3-chlorobenzoic acid NMR (CDC1 3 , δ) : 5.49 (2H, s) , 7.18 (1H, t, J=6Hz) , 7.32-7.42 (4H, ) , 7.50-7.62 (3H, m) , 7.89-7.93 (2H, Ei), 8.10 (1H, d, J=7Kz), 8.58-8.62 (1H, m) 11) 4- [2- (Benzyloxy) benzoyl ]amino-2-nitrobenzoic acid NMR (DMSO-dg, δ) : 5.22 (2H, s) , 7.10 (1H, t, ' -J=7Hz), 7.28-7.38 (4H, ) , 7.50-7.58 (3H, m) , 7.65-7.69 (1H, ) , 7.86 (2K, s) , 8.16 (1H, s) 12) 2-[2-(Benzyloxy)benzoyl]amino-5-pyridinecarboxylic acid NMR (DMSO-dg, δ) : 5.18 (1H, s) , 5.32 (2H, s) , 6.98- 7.20 (2H, m), 7.29-7.67 (6H, m) , 7.84-7.88 (1H, m) , 8.28-8.37 (2H, } , 8.80 (IK, s) 13) 4-[N-[2-[ (3-tert-Butcxycarbonylaminoprop-l- yl)oxy]phenyl]-tert-butoxycarbonylamino]methyl-3- methoxybenzoic acid NMR (CDCI3, δ) : 1.35 and 1.43 (total 18H, s) , 1.92- 2.00 (2H, ) , 3.28 and 3.32 (total 2H, m) , 3.20 and 3.28 (total 3H, s), 4.02 (2H, br) , 4.77 (2H, br), 6.77-7.99 (3H, m) , 7.10-7.20 (2H, m) , 7.44- 7.56 (2H, m) , 7.69 (1H, br) 14) 4-[2-[ (3-tert-Butoxycarbonylamincprop-l-yl)oxymethyl- 3-methoxybenzoic acid NMR (CDCI3, δ) : 1.37 (9K, s) , 2.05 (2H, br) , 3.40 (2H, br), 3.93 (3H, s), 4.10-4.17 (2H, m) , 5.27 (2H, s), 5.50 (1H, br), 6.87-6.93 (4H, m) , 7.59 (2H, s), 7.72-7.77 (IK, m) 15) 3-Benzyloxy-4-[2-[ (3-tert-butoxycarbonylaminoprop-l- yl)oxy]benzoyl]aminobenzoic acid NMR (DMSO-dg, δ) : 1.30 (9H, s), 1.62-1.72 (2H, m) , 2.88-2.92 (2H, ) , 3.95 (2H, t, J=6Hz), 5.37 (2H, s), 6.80 (1H, br), 7.13 (IK, t, J=7Hz) , 7.21 (1H, d, J=7Hz), 7.30-7.67 (9H, m), 8.08 (1H, d, J=7Kz), 8.60 (IK, d, J=7Hz) 16) 2-[2-[ (3-tert-Butoxycarbonylaminoprop-l- yl)oxy]benzoyl]amino-5-thiophenecarboxylic acid NMR (DMSO-dg, δ) : 1.32 (9H, s), 1.82-1.90 (2H, m) , 3.08-3.14 (2H, m) , 4.10 (2H, t, J=6Hz), 6.81 (1H, d, J=5Hz), 6.93-7.00 (1H, m) , 7.07 (1H, t, J=7Hz), 7.19 (1H, d, J=7Hz), 7.50-7.58 (2H, m) , 7.67 (1H, d, J=7Hz) Preparation 9 The following compounds were obtained according to a similar manner to that of Preparation 3. 1) 3-Methoxy-4-nitro-N-methyl-N-[2-[5-(4- dimethylaminopiperidin-1-yl) carbonylpent-1-yloxy] -4- methylphenyl ] benzamide NMR (CDC1 3 , δ) : 1.30-1 .96 (10H, m) , 2.28 (9H, s) , 2 .30-2 .41 (3H, ) , 2 . 58 (1H, m) , 3 . 02 (1H, m) , 3 .33 (3H, s) , 3.77 (3H, s) , 3.82-4 .00 (3H, m) , 4 . 63 (1H, m) , 6.56-6. 66 (2H, m) , 6. 84 (IK, d, J=9Hz) , 6. 93 (1H, d, J=9Kz) , 7 .06 (1H, s) , 7 . 61 (1H, ' d, J=9Hz) 2) 4-Nitro-N-methyl-N-[4-methyl-2-[4-(4-methylpiperazin- 1-yl)carbonyl]phenylmethoxy]phenylbenzamide NMR (CDCI3, δ) : 2.26 (3H, s), 2.32 (3H, s) , 2.36- 2.57 (4H, m), 3.37 (3H, s), 3.42-3.59 (2K, m) , 3.71-3.89 (2H, m) , 4.94 (IK, d, J=14Hz) , 5.07 (1H, d, J=14Hz), 6.60-6.69 (2H, m) , 6.94 (1H, d, J=7Hz), 7.36-7.50 (5H, m) , 7.95 (2H, d, J=8Hz) 3) 4-Amino-3-methoxy-N-methyl-N- [4-methyl-2- [4- (4- methylpiperazin-1-yl) carbonyl]phenylmethoxy]- phenylbenzamide NMR (CDC1 3 , δ) : 2.28 (3H, s) , 2.33 (3H, s), 2.37- 2.53 (4H, m) , 3.36 (3H, s) , 3.41-3.54 (2H, m) , 3.57 (3H, s), 3.65-3.90 (4H, m) , 4.90 (1H, d, J=14Hz), 5.06 (1H, d, J=14Hz) , 6.38 (1H, d, J=7Hz), 6.62-6.70 (2K, m) , 6.78 (1H, d, J=7Hz) , 6.84 (1H, ε), 6.98 (IK, d, J=7Kz) , 7.33 (2H, d, J=8Hz), 7.41 (2H, d, J=8Kz) 4) 4-Amino-3-methoxy-N- [2- [4- (4 -dimethyl aminopiperidin- 1-yi) carbonyl ]phenylmethoxy-4-methyl]phenyl-N- methylbenzamide NMR (CDCI3, δ) : 1.14-1.58 (2H, m) , 1.75-2.00 (2H, ), 2.26 (3H, s), 2.30 (3H, s) , 2.40 (IK, m) , 2.73-3.10 (4H, m) , 3.36 (3H, s), 3.57 (3K, s), 3.87 (3K, s), 4.83-5.12 (2H, m) , 6.39 (1H, d, J=7Hz), 6.61-6.71 (2H, m) , 6.28 (1H, d, J=7Hz) , 6.33 (1H, s), 6.97 (1H, d, J=7Hz) , 7.33 (2H, d, J=8Hz), 7.40 (2H, d, J=8Hz) 5) 4-Amino-3-methoxy-N-methyl-N-[2-[3-(4- methylpiperazin-1-yl)carbonylmethoxyprop-1- yl]oxy]phenylbenzamide NMR (CDCI3, δ) : 1.98-2.13 (2H, m) , 2.27 (3K, s) , 2.29-2.38 (4H, m) , 3.30 (3H, s) , 3.36-3.47 (2H, a), 3.52-3.74 (4H, ) , 3.60 (3H, s) , 3.94-4.17 (2H, m), 4.11 (2H, s) , 6.42 (1H, d, J=7Hz), 6.78-6.92 (4H, m) , 7.00 (IK, d, J=7Hz) , 7.14 (1H, t, J=7Hz) 6) 4-Amino-3-methoxy-N-[2-[ (E)-5-(4- 95 - 82 - aimethylaminopiperidin-1-yl)carbonyl-4-penten-l- yl]oxy-4-methyl]phenyl-N-methylbenzamide NMR (CDC1 3 , δ) : 1.30-1.47 (2H, m) , 1.80-1.98 (2H, m), 2.21 (3H, s), 2.26 (6H, s), 2.26-2.43 (2H, ), 2.45-3.67 (6K, m) , 3.30 (3H, s) , 3.61 (3H, ε), 3.85 (2H, br) , 3.85-4.04 (2H, m) , 4.62 (1H, m), 6.29 (1H, d, J=15Hz), 6.41 (IK, d, J=7Hz) , 6.57-6.63 (2H, ) , 6.77-6.90 (4K, ) 7) 3-[5-(4-Dimethylaminopiperiαin-l-yl)carbonylpent-l- yioxy]-4-(tert-butoxycarbonylamino)toluene NMR (CDCi^, δ) : 1.27-2.00 (19H, ) , 2.21-2.44 (12H, ), 2.5S (IK, m), 3.01 (1H, m) , 3.89 (IK, m) , 4.00 (2H, t, J=7Kz), 4.64 (1H, m) , 6.64 (1H, s) , 6.72 (1H, d, J=8Hz) , 6.94 (1H, s) , 7.89 (1H, m) Preparation I Q The following compounds were obtained according to a similar manner to that of Example 1. 1) Methyl 4-(2-benzyloxybenzoyl)amino-3-methoxybenzoate NMR (CDCI3, δ) : 3.50 (3H, s), 3.90 (3H, s) , 5.36 (2H, s), 7.08 (1H, d, <T=9Hz), 7.15 (IK, t, J=9Hz), 7.33-7.49 (8H, m) , 7.73 (IK, dd, J=l, 8Hz), 8.30 (1H, d, J=8Hz) , 8.72 (1H, d, J=8Hz) ESI-MASS (m/z) : 392 (M÷H) 2) Methyl 4-(2-acetoxybenz ' oyl)amino-3-methoxybenzoate NMR (CDCI3, δ) : 2.38 (3K, s) , 3.92 (3H, s) , 3.99 (3H, s), 7.19 (1H, d, J=8Hz), 7.38 (1H, t, J=8Hz), 7.55 (1H, t, J=8Hz), 7.60 (1H, s) , 7.75 (1H, dd, J=2, 9Hz), 7.99 (1H, dd, J=l, 9Hz) , 8.66 (IK, d, J=8Hz), 9.03-9.07 (1H, br s) ESI-MASS (m/z) : 344 (M+H) 3) 3-Methoxy-4-nitro-N- [2- (4-methoxycarbonyl) - phenylmethoxy-4-methyl]phenylbenzamide NMR (DMSO-dg, δ) : 2.31 (3H, s) , 3.84 (3H, s), 3.98 (3H, s), 5.27 (2H, s) , 6.81 (1H, d, J=7Hz), 7.00 (1H, s), 7.49 (1H, d, J=7Hz), 7.62 (2K, d, J=8Hz), 7.79 (1H, s), 7.92 (2H, d, J=8Hz) , 8.00 (IK, d, J=7Hz), 9.85 (1H, s) 4) 4-Nitro-3-methoxy-N-[ (E and Z)-2-(4- methoxycarbonylphenyl) ethen-1-yl]phenylbenzamide NMR (CDC1 3 , δ) : 3.87 (3Hx2/3, s) , 3.91 (3Kxl/3, s) , 3.95 (3Kx2/3, s) , 4.00 (3Hxl/3, s) , 6.71-8.20 (13K, ) 5) 3-Methoxy-4-nitro-N- [2- [3- (ethoxycarbonylmethyl) - oxyprop-l-yl]oxy]phenylbenzamide NMR (CDCI3, δ) : 1.22 (3H, t, J=7.5Hz), 2.10-2.23 (2H, m), 3.78 (2H, t, J=7.5Hz), 4.01 (2H, s) , 4.06 (3H, s), 4.14 (2H, q, J=7.5Hz), 4.26 (2H, t, J=7.5Hz), 6.91-7.06 (3H, m) , 7.42 (IK, d, J=7Hz), 7.74 (IK, s), 7.93 (1H, d, J=7Kz) , 8.49 (1H, d, J=7Kz), 7.78 (1H, s) 6) 3-Methoxy-4-nitro-N- [2- [ (E) -5-ethoxycarbonyl-4- penten-1-yl]oxy-4-methyl]phenylbenzamide NMR (CDCI3, δ) : 1.27 (3H, t, J=7.5Hz), 1.93-2.08 (2H, m), 2.27-2.50 (2H, m) , 2.32 (3H, s) , 4.02 (3K, s), 4.01-4.il (2H, m) , 4.18 (2H, q, J=7.5Hz), 5.88 (IK, d, J=15Hz) , 6.72 (IK, s) , 6.83 (IK, t, J=7Hz), 6.99 (1H, dt, J=15, 7.5Hz), 7.35 (IK, d, J=7Hz), 7.81 (1H, s) , 7.92 (1H, d, J=7Hz), 8.28 (1H, d, J=7Hz) , 8.45 (1H, s) 7) 4-Benzyloxy-3-methoxy-N-methyl-N- [2- [5- (4- dimethylaminopiperidin-1-yi) carbonylpent-1-yloxy]-4- methylphenyl]benzamide NMR (DMSO-dg, δ) : 1.35-1.49 (2H, m) , 1.49-1.63 (2H, ), 1.64-1.79 (2H, ) , 2.23 (3H, s), 2.37 (2H, t, J=7Hz), 2.72 (3H, m) , 2.78-3.11 (2H, m) , 3.1 (3H, s), 3.28-3.60 (5H, m) , 3.71-4.13 (5H, m) , 4.43 (1H, m), 4.99 (2H, s), 6.63 (IK, d, J=8Hz), 6.80 (2K, d, J=2Hz), 6.86 (2K, s) , 6.98 (IK, d, J=8Hz), 7.26-7.44 (5K, m) 8) 3-Methoxy-4-nitro-N- (2-benzyloxy-4-methylphenyl) - benzamide NMR (CDC1 3 , δ) : 2.38 (3H, s) , 3.90 (3H, s) , 5.12 (2H, s ) , 6.88 (1H, s) , 7.30 (1H, s) , 7.51 (4H, ε ) , 7 .59 (IK, s) , 7.82 (IK, d, J=8Hz) , 8.37 (IK a, J=8Hz) , 8.53 (IK, br) 9) 3-Methyl-4-nitro-N-methyl-N-[2-[5-(4-methylpiperazin 1-yl)carbonylpent-l-yloxy]-4-methylphenyl]benzamide NMR (CDCI3, δ) : 1.48-1.60 (2H, m) , 1.69-1.77 (2H, ), 1.79-1.90 (2H, ) , 2.25 (3H, s), 2.29 (3H, s), 2.33-2.42 (6H, m) , 2.47 (3H, s), 3.32 (3H, s), 3.45-3.50 (2H, m) , 3.58-3.63 (2H, m) , 3.82- 3.95 (2H, m), 6.55-6.59 (2H, m) , 6.83 (1H, d, J=7Hz), 7.14 (1H, d, J=7Hz), 7.37 (1H, s), 7.70 (1H, d, J=7Hz) 10) Ethyl 4-[ (2-benzyloxy)benzoyl]amino-3-chlorobenzoate NMR (CDCI3, δ) : 1.38 (3H, t, J=7Hz) , 4.34 (2H, q, J=7Hz), 5.38 (1H, s) , 5.39 (1H, s) , 7.03-7.16 (2H, m), 7.33-7.50 (6H, m) , 7.92-7.99 (2H, m) , 8.24-8.32 (1H, m) , 8.73-8.29 (IK, m) II) 3-Hydroxy-4-nitro-N-methyl-N-[2-[5-(4- methylpiperazin-1-yl)carbonylpent-1-yloxy]-4- methylphenyl]benzamide NMR (CDCI3, δ) : 1.48-1.60 (2H, m) , 1.68-1.80 (2H, ), 1.82-1.91 (2H, m) , 2.28 (3H, s), 2.30 (3H, s), 2.37-2.42 (6H, m) , 3.32 (3H, s) , 3.48-3.50 (2H, m), 3.62-3.68 (2H, m) , 3.90-3.97 (2H, m) , 6.57-6.58 (2H, m) , 6.80-6.87 (2H, m) , 7.08-7.10 (1H, m), 7.65 (1H, d, J=7Hz) 12) Ethyl 4-[2-(benzyloxy)benzoyl]amino-2-nitrobenzoate NMR (CDCI3, δ) : 1.32 (3H, t, J=7Hz) , 4.32 (2H, q, J=7Hz), 5.22-5.30 (2H, m) , 7.12-7.27 (2K, m) , 7.37-7.69 (9H, m) , 8.20-8.34 (1H, m) 13) Methyl 2-[2- (benzyloxy)benzoyl]amino-5- pyridinecarboxylate NMR (CDCI3, δ) : 3.92 (3H, s), 5.12 (1H, s) , 5.36 (2K, s), 6.90-7.01 (1H, m) , 7.10-7.18 (2H, m) , 7.32-7.55 (5H, m),8.27-8.34 (2H, m) , 8.46 (1H, d, J=6Hz), 8.87-8.88 (1H, m) 14) Benzyl 4- (2-acetoxybenzoyl)amino-3-benzyloxybenzoate NMR (CDCI3, δ) : 2.05 (3H, s) , 5.20 (2H, s), 5.87 (2K, s), 7.13 (IK, d, J=8Hz), 7.32-7.47 (10H, m), 7.50-7.57 (1H, m) , 7.73 (1H, s), 7.80 (1H, d, J=8Hz), 7.96 (1H, d, J=8Hz) , 8.68 (1H, d, J=7Hz), 9.13 (1H, s) 15) Methyl 2- (2-acetoxybenzoyl)amino-5- thiophenecarboxylate NMR (CDCI3, δ) : 2.39 (3H, s) , 3.88 (3H, s), 6.69 (1H, d, J=5Hz), 7.19-7.21 (1H, m) , 7.35-7.30 (1H, m), 7.52-7.59 (1H, m) , 7.63-7.66 (1H, m) , 7.92-7.95 (1H, m) , 9.18 (1H, s) Preparation 11 The following compound was obtained by reacting the compound, which was prepared according to a similar manner to that of Example 1, with hydrogen chloride. 4-Benzyloxy-3-methoxy-N-methyl-N-[4-methyl-2-[5-(4- methylpiperazin-1-yl)carbonylpent-1-yloxy]phenyl]benzamide hydrochloride NMR (DMSO-dg, δ) : 1.35-1.49 (2H, m) , 1.49-1.63 (2H, ) , 1.64-1.79 (2H, m) , 2.23 (3H, s) , 2.37 (2H, t, J=7Hz), 2.72 (3H, ) , 2.78-3.11 (2H, m) , 3.16 (3H, s), 3.28-3.60 (5K, ) , 3.71-4.13 (5K, m) , 4.43 (IK, m) , 4.99 (2K, s), 6.63 (IK, d, J=8Hz) , 6.60 (2K, d, J=2Hz), 6.86 (2H, s) , 6.98 (1H, d, J=8Hz), 7.26-7.44 (5H, m) reparation 12 The following compound was obtained according to a similar manner to that of Example 4. 4-[2-[ (3-tert-Butoxycarbonylaminoprop-l- yl)oxy]benzoyl]amino-3-methoxybenzoic acid NMR (DMSO-d 6 , δ) : 1.35 (9H, s) , 2.04 (2H, quintet, J=7Kz), 3.13 (2H, q, J=7Hz) , 3.98 (3H, s) , 4.29 (2H, t, J=7Hz), 6.95-7.00 (1H, m) , 7.16 (1H, t, J=8Hz), 7.28 (1H, d, J=8Kz), 7.57-7.65 (3H, m) , 8.11 (IK, dd, J=l, 8Hz) , 8.63 (1H, d, J=8Hz) ESI-MASS (m/z) : 445 (M+H) Preparation 13 The following compounds were obtained according to a similar manner to that of Example 10. 1) 4-Hydroxy-3-methoxy-N-methyl-N-[4-methyl-2-[5-(4- methylpiperazin-1-yl)carbonylpent-1-yloxy]phenyl]- benzamide NMR (CDC1 5 , δ) : 1.44-1.59 (2K, ) , 1.62-1.92 (4H, ) , 2 . 22-2 . 45 ( 12H, m) , 3 . 31 (3H, s ) , 3. 42-3. 53 (2H, m) , 3 . 58-3 .74 ( 5H, m) , 3.77-4 . 02 (2H, m) , 6.53-6.70 (3H, m) , 6. 80-6. 96 (3H, m) 2) Methyl 4- (N-methyl-2-hydroxybenzoylamino)-3- methoxybenzoate NMR (CDC1 3 , δ) : 3.37 (3H, s), 3.69 (3K, s) , 3.91 (3H, s), 6.38 (IK, t, J=8Kz), 6.72 (IK, d, J=8Hz), 6.91 (IK, d, J=8Kz), 7.15 (1H, t, J=8Hz), 7.21 (1H, d, J=9Hz) , 7.49 (1H, a, J=lHz), 7.62 (IK, dd, J=l, 9Kz) ESI-MASS (m/z) : 316 (M÷K) 3) 4-Kydroxy-3-methoxy-N-methyl-N- [2- [5- (4- dimethylaminopiperidin-1-yl) carbonylpent-l-yloxy]-4- methylphenyl]benzamide NMR (CDCI3, δ) : 1.25-2.00 (10H, m) , 2.06-2.40 (6H, m) , 2.52 (IK, m), 2.73 (6H, br s) , 3.02 (1H, m) , 3.30 (3K, s), 3.67 (3K, s) , 3.76-4.07 (3H, m) , 4.82 (IK, m), 6.56-6.72 (3H, m) , 6.78-6.96 (3H, m) 4) Methyl 4- [N- (2-hydroxyphenyl) -tert- butoxycarbonylamino]methyl-3-methoxybenzoate NMR (CDCI3, δ) : 1.38 (9H, ε) , 3.82 and 3.83 (total 3H, ε), 3.90 and 3.91 (total 3H, ε) , 4.88 (2H, ε), 6.80-6.87 (1H, m) , 6.95 (1H, br) , 7.03-7.12 (2H, ' m), 7.25-7.30 (2H, m) , 7.48-7.50 (1H, m) , 7.58-7.60 (1H, ) 5) 2- (3-tert-Butoxycarbonylaminoprop-l-yl) oxyphenol NMR (CDCI3, δ) : 1.45 (9H, ε), 1.95-2.07 (2H, m) , 3.25-3.45 (2H, m) , 4.10 (2H, t, J=6Hz) , 4.68 (1H, br), 6.22 (1H, br) , 6.78-6.97 (4H, m) Preparation 14 The following compounds were obtained according to a similar manner to that of Example 12. 1) Methyl 4-[N-methyl-2-[ (3-tert-butoxycarbonylamino- prop-l-yl)oxy]benzoyl]amino-3-methoxybenzoate NMR (CDC1 3 , δ) : 1.43 (9K, s), 1.95-2.05 (2K, m) , 3.30-3.40 (5K, ) , 3.83 (3K, s) , 3.85 (3H, s) , 3.96-4.04 (2H, m) , 5.23-5.32 (IK, br) , 6.65-6.73 (2H, m), 7.00-7.16 (3H, m) , 7.38-7.45 (2H, m) ESI-MASS (m/z) : 473 (M+H) 2) Methyl 4-[2-[ (3-tert-butoxycarbonylaminoprop-l- yl)oxy]benzoyl]amino-3-methoxybenzoate NMR (CDCI3, δ) : 1.40 (9H, s) , 2.13-2.21 (2H, m) , 3.33 (2H, q, J=7Hz) , 3.92 (3H, s) , 4.00 (3H, s) , 4.29 (2H, t, J=7Hz), 4.72-4.78 (1H, br) , 7.03 (1H, d, J=8Hz), 7.23 (1H, t, J=8Hz) , 7.49 (1H, t, J=8Hz), 7.60 (1H, s), 7.75 (IK, d, J=8Hz) , 8.27 (1H, d, J=8Hz) , 8.77 (1H, d, J=8Hz) ESI-MASS (m/z) : 459 (M+H) 3) 4-Nitro-N-[2-(4-methoxycarbonylphenyl)methoxy-4- methyl]phenyl-N-methylbenzamide NMR (CDCI3, δ) : 2.27 (3H, s), 3.40 (3H, s) , 3.94 (3K, s), 4.95 (1H, d, J=14Hz), 5.09 (1H, d, J=14Hz), 6.62 (IK, ε) , 6.69 (1H, d, J=7Hz) , 6.97 (IK, d, J=7Hz), 7.31-7.49 (4H, m) , 7.95 (2H, d, J=8Hz), 8.10 (2K, d, J=8Hz) Preparation 15 The following compound waε obtained according to a similar manner to that of Example 16. 4-Amino-3-methoxy-N-methyl-N-[4-methyl-2-[5-(4- methylpiperazin-l-yl)carbonylpent-l-yloxy]phenyl]benzamide dihydrochloride NMR (DMSO-dg, δ) : 1.33-1.64 (4K, m) , 1.64-1.81 (2H, m), 2.20 (3H, s) , 2.29-2.43 (2K, m) , 2.73 (3H, s), 2.79-3.10 (4H, m) , 3.14 (3H, s), 3.22-3.56 (4H, m), 3.62 (3H, s), 3.72-4.18 (3K, ) , 4.42 (IK, m) , 6.62 (IK, d, J=8Kz) , 6.74-6.92 (3H, m) , 6.92-7.10 (2K, m) Preparation 16 The following compounds were obtained according to a similar manner to that of Example 43. 1) Methyl 4- (2-hydroxybenzoyl) amino-3-methoxybenzoate NMR (CDC1 3 , δ) : 3.93 (3H, s) , 4.03 (3H, s) , 6.96 (IK, t, J=8Kz), 7.04 (1H, d, J=8Hz) , 7.47 (1H, t, J=8Hz), 7.54 (1H, dd, J=l, 8Hz) , 7.62 (1H, s), 7.76 (1H, d, J=8Hz), 8.51 (1H, d, J=8Hz) , 8.85-8.89 (1H, br s) ESI-MASS (m/z) : 302 (M+H) 2) Benzyl 3-benzyloxy-4- (2-hydroxybenzoyl) aminobenzoate NMR (CDCI3, δ) : 5.23 (2H, s) , 5.38 (2H, s) , 6.82 (1H, t, J=7Hz), 7.01 (1H, d, J=7Hz) , 7.30-7.49 (12H, m), 7.70-7.73 (1H, m) , 7.80-7.83 (1H, ) , 7.52 (1H, d, J=7Hz), 8.95 (1H, s) 3) Methyl 2- (2-hydroxyben ' zoyl)amino-5- thiophenecarboxylate NMR (DMSO-dg, δ) : 3.79 (3H, ε) , 6.95-7.03 (3H, m) , 7.42-7.48 (1H, m) , 7.62-7.64 (IK, m) , 7.88 (1H, d, J=7Hz) Preparation 17 The following compound was obtained according to a similar manner to that of Example 30, 3-Methoxy-4-nitro-N-methyl-N-[4-methyl-2-[4-(4- methylpiperazin-1-yl)carbonyl]phenylmethoxy]- phenylbenzamide NMR (CDC1 3 , δ) : 2.29 (3H, s), 2.35 (3H, s) , 2.38- 2.54 (4H, m), 3.39 (3H, s) , 3.43-3.53 (2H, m) , 3.66 (3H, s), 3.71-3.88 (2H, m) , 4.92 (1H, d, J=14Hz), 5.07 (1H, d, J=14Hz), 6.65-6.72 (2H, ), 6.87 (IK, d, J=7Hz), 6.98 (1H, d, J=7Hz) , 7.03 (1H, s), 7.37 (2H, d, J=8Hz) , 7.45 (2H, d, J=8Hz), 7.56 (IK, d, J=7Kz) Preparation 18 To a mixture of 2-(4-methoxycarbonylphenyl)methoxy-4- methylaniline (420 mg) and 37% formaldehyde solution (69.7 mg) in a mixture of methanol (10 ml) and acetic acid (0.1 ml) was added sodium cyanoborohydride (146 mg) and the mixture was stirred at ambient temperature for 3 hours. The solution was diluted with ethyl acetate (30 ml) and washed successively with saturated aqueous sodium hydrogen carbonate, water and brine. The organic solution was dried over magnesium sulfate and the solvent waε evaporated in vacuo. The residue was purified by silica gel column (chloroform) to give 2-(4- methoxycarbonylphenyl)methoxy-4-methyl-N-methylaniline (356 mg) . NMR (CDCI3, δ) : 2.22 ' (3H, s), 2.80 (3H, s), 3.91 (3K, s), 5.11 (2H, s), 6.53 (IK, d, J=7Hz), 6.63 (1H, s), 6.72 (IK, d, J=7Hz), 7.49 (2H, d, J=8Hz), 8.04 (2H, d, J=8Hz) Preparation 19 A solution of 2-benzyloxy-N-tert- butoxycarbonylaniline (1 g) in N, N-dimethylformamide (40 ml) was treated with sodium hydride (147 mg, 60% w/w in mineral oil) at 0°C. The reaction mixture was stirred at 0 β C for 30 minutes and then at ambient temperature for 1 hour. Methyl 4-bromomethyl-3-methoxybenzoate (909 mg) was added, and the mixture was stirred at ambient temperature for 30 minutes. The reaction was quenched with water and the mixture diluted with ethyl acetate. The organic phase was washed with 0.5N hydrochloric acid, saturated aqueous sodium hydrogen carbonate, and brine. The solution was concentrated in vacuo and the residue was purified by silica gel column chromatography (hexane:ethyl acetate = 9:1) to give methyl 4-[N- [2- (benzyloxy)phenyl-tert- butoxycarbonylamino]methyl-3-methoxybenzoate (1.38 g) . NMR (CDC1 3 , δ) : 1.32 and 1.40 (total 9H, s), 3.65 and 3.71 (total 3H, s), 3.90 (3H, s), 4.77 (2H, s), 5.07 (2H, ε), 6.78-7.00 (3H, ) , 7.09-7.20 (1H, m), 7.27-7.55 (8H, m) Preparation 20 The following compoundε were obtained according to a similar manner to that of Preparation 19. 1) 4-Nitro-3-methoxy-N-[ (E and Z)-2- (4-methoxycarbonyl- phenyl) ethen-l-yl]phenyl-N-methylbenzamide NMR (CDCI3, δ) : 3.40 (3Hx2/3, s) , 3.49 (3Hxl/3, s), 3.54 (3Hxl/3, s), 3.60 (3Hx2/3, ε), 3.86 (3Hx2/3, ε), 3.95 (3Hxl/3, s) , 6.41-8.07 (7H, m) 2) 3-Methoxy-4-nitro-N-[2-[3- (ethoxycarbonylmethyl)- oxyprop-1-yl]oxy]phenyl-N-methylbenzamide NMR (CDCI3, δ) : 1.27 (3H, t, J=7.5Hz), 2.04-2.17 (2H, m) , 3.37 (3H, s) , 3.71 (2H, t, J=7.5Hz), 3.76 (3H, S), 4.06 (3H, s) , 4.20 (2H, q, J=7.5Hz), 6.78-7.01 (4H, ) , 7.04 (1H, s) , 7.19 (IK, t, J=7Kz), 7.60 (IK, d, J=7Hz) 3) 3-Methoxy-4-nitro-N-(2-benzyloxy-4-methylphenyl)-N- methylbenzamide NMR (CDC1 3 , δ) : 2.28 (3H, s), 3.39 (3H, s), 3.58 (3H, s), 4.85 (1H, d, J=12Hz), 5.07 (IK, d, J=12Hz), 6.68 (2H, ε) , 6.83 (IK, d, J=9Hz), 6.96 (IK, d, J=9Hz), 7.00 (1H, s) , 7.30-7.44 (5H, m) , 7.52 (IK, d, J=9Hz) Preparation 21 To an ice bath cooled solution of methyl 2-(3- hydroxyprop-1-yl)thiobenzoate (3.7 g) in N,N- dimethylformamide (30 ml) was added sodium hydride (60% in oil, 719 mg) and the εolution was stirred at the same temperature for 30 minutes. 4-Methoxybenzyl chloride (2.56 g) was added to the solution and the mixture was stirred at ambient temperature for 5 hours. The mixture was diluted with ethyl acetate (100 ml) and the solution was washed with water and brine. The organic phase was dried over magnesium sulfate and the solvent was evaporated in vacuo to give a crude oil. The crude product was purified by silica gel column chromatography (hexane:ethyl acetate = 10:1) to give methyl 2-[3-(4- ethoxyphenyl)methoxyprop-1-yl]thiobenzoate (2.13 g) . NMR (CDCI3, δ) : 1.94-2.07 (2H, ) , 3.03 (2K, t, J=7.5Hz), 3.58 (2K, t, J=7.5Hz), 3.80 (3H, s) , 3.90 (3K, s), 4.39 (2H, q, J=7.5Hz), 4.45 (2H, S), 6.87 (2H, d, J=8Hz), 7.13 (IK, t, J=7Hz) , 7.21-7.46 (4H, m) , 7.96 (1H, d, J=7Hz) Preparation 22 The following compound was obtained according to a similar manner to that of Preparation 21. 2-[3-(Ethoxycarbonylmethyl)oxyprop-1- yl]oxynitrobenzene NMR (CDCI3, δ) : 1.25 (3H, t, J=7.5Hz), 2.08-2.20 (2H, m), 3.73 (2H, t, J=7.5Hz), 4.06 (2H, s) , 4.13-4.32 (4H, ) , 7.01 (1H, m) , 7.10 (1H, d, J=7Hz), 7.50 (1H, t, J=7Hz), 7.82 (1H, d, J=7Hz) Preparation 23 To an ice bath cooled solution of 3-methoxy-4-nitro- N-[2-( -methoxycarbonyl)phenylmethoxy-4-methyl]- phenylbenzamide (7.67 g) in N,N-dimethylformamide (50 ml) was added sodium hydride (60% in oil, 817 mg) and the solution was stirred at the same temperature for 30 minutes. Iodomethane (1.27 ml) was added to the solution and the mixture waε εtirred at ambient temperature for 2 hours. The mixture was diluted with ethyl acetate (100 ml) and the solution was washed with water and brine. The organic phase was dried over magnesium sulfate and the solvent was evaporated in vacuo to give an oil. The oil was solidified with diethyl ether to give 3-methoxy-4- nitro-N-[2-(4-methoxycarbonyl)phenylmethoxy-4- methyl]phenyl-N-methylbenzamide (6.65 g) . NMR (CDCI3, δ) : 2.28 (3H, s) , 3.40 (3H, ε) , 3.60 (3H, ε), 3.94 (3K, ε), 4.91 (IK, d, J=14Hz) , 5.09 (IK, d, J=14Hz), 6.64 (1H, s), 6.71 (1H, d, J=7Hz), 6.84 (1H, d, J=7Hz) , 7.00-7.04 (2H, m) , 7.42 (2H, d, J=8Hz) , 7.52 (1H, d, J=7Hz) , 8.08 (2H, d, J=8Hz) Preparation 24 The following compound was obtained according to a similar manner to that of Preparation 23. 3-Methoxy-4-nitro-N-[2-[ (E)-5-ethoxycarbonyl-4- penten-l-yl]oxy-4-methyl]phenyl-N-methylbenzamide NMR (CDCI3, δ) : 1.28 (3H, t, J=7.5Hz), 1.90-2.00 (2H, m), 2.00 (3H, s) , 2.34-2.45 (2H, m) , 3.35 (3H, s), 3.77 (3H, s) , 3.84-3.97 (2H, ) , 4.19 (2K, q, J=7.5Hz), 5.88 (IK, d, J=15Hz) , 6.58- 6.64 (2K, m), 6.84-7.02 (3H, m) , 7.07 (1H, s), 7.60 (1H, d, J=7Hz) Preparation 25 The following compound was obtained according to a similar manner to that of Example 45. 2-[5-(4-Dimethylaminopiperidin-I-yl)carbonylpent-1- yloxy]-4-methylaniline NMR (CDC1 3 , δ) : 1.18-2.00 (10H, m) , 2.14-2.69 (13H, m), 2.99 (1H, m) , 3.44-4.07 (5H, m) , 4.64 (1H, ) , 6.45-6.70 (3H, m) Preparation 26 The following compound was obtained according to a similar manner to that of Example 38. 2-Hydroxy-N-tert-butoxycarbonylaniline NMR (CDCI3, δ) : 1.55 (9K, s), 6.63 (1H, s) , 6.82- 6.89 (IK, m), 6.97-6.99 (IK, m) , 7.02-7.08 (2H, m) , 8.13 (IK, br) Preparation 27 The following compound was obtained according to a similar manner to that of Example 87. Methyl 2-nitro-5-thiophenecarboxylate NMR (CDCI3, δ) : 3.95 (3H, s) , 7.70 (1H, d, J=5Hz) , 7.86-7.88 (1H, m) Pre p aration 28 To a suspenεion of phoεphonium bromide (1.9 g) in tetrahydrofuran (35 ml) at 0°C was added l.OM lithium bis (trimethylsilyl)amide in tetrahydrofuran (7.88 ml) over 5 minutes period. After 40 minutes, the cooling bath was removed and the red εuεpension was εtirred for 15 minuteε at ambient temperature. The εuεpenεion waε recooled to -78°C, and a εolution of 2-[3-(phthalimido)prop-l- yl]oxybenzaldehyde (1.16 g) in 10 ml of tetrahydrofuran (plus a 5 ml rinse) was added via cannula. The red reaction mixture was stirred at 0°C to ambient temperature. After 20 hours, the solution was quenched by 0.5N hydrochloric acid at 0 β C. The resulting mixture was concentrated and extracted with chloroform. The organic extract was washed with brine and dried over magnesium sulfate, filtered, and concentrated to give 4-[2-[2-[3- (phthalimido)prop-1-yl]oxy]phenyl] inyl-3-methoxybenzoic acid (2.4 g) . NMR (DMSO-dg, δ) : 1.99-2.22 (2H, m) , 3.72-3.94 (5H, m), 3.98-4.17 (2H, m) , 6.38-7.88 (UK, m) Preparation 29 To a suspenεion of sodium hydride (60% oil suspension, 88.3 mg) in N,N-dimethylformamide (6 ml) was added a solution of methyl 4- (2-benzyloxybenzoyl)amino-3- methoxybenzoate (600 mg) in N,N-dimethylformamide (4 ml) and the mixture was stirred at 0°C for 1 hour. Methyl iodide (0.14 ml) was added dropwiεe to the above solution and the mixture was stirred at 0 β C for 30 minuteε. The reaction temperature waε raised to ambient temperature over 30 minuteε and the reaction waε quenched with IN hydrochloric acid, and then the resulting solution was extracted with ethyl acetate. Drying, filtering and removal of solventε afforded a crude product. The crude product was purified by column chromatography (eluent; hexane:ethyl acetate = 3:1) to give methyl 4-(N-methyl-2- benzyloxybenzoylamino)-3-methcxybenzoate (650 mg) . NMR (CDC1 3 , δ) : 3.35 (3K, s) , 3.72 (3H, ε), 3.87 (3K, s), 4.93-5.00 (2H, m) , 6.65 (1H, d, J=8Hz), 6.76 (1H, t, J=8Hz), 7.00-7.12 (2H, ) , 7.18- 7.23 (IK, m), 7.30-7.43 (6H, ) , 8.02 (1H, s) ESI-MASS (m/z) : 406 (M+H) Preparation 3 Q To a solution of (S)-l,3-butanediol (1.0 g) and triethylamine (1.12 g) in dichloromethane (30 ml) was added portionwise p-tolueneεulfonyi chloride (2.12 g) at 0°C, and then the mixture was stirred at ambient temperature for 3 hours and stand overnight. The resulting solution waε diluted with dichloromethane (30 ml) and the organic layer waε waεhed succesεively with IN hydrochloric acid, εaturated εodium bicarbonate aqueouε solution and brine. Drying, filtering and removal of solventε afforded (S)-3-hydroxybutyl p-tolueneεulfonate (2.26 g) . NMR (CDC1 3 , δ) : 1.20 (3H, d, J=8Hz), 1.63-1.77 (1H, ), 1.78-1.93 (1H, m) , 2.47 (3H, s) , 3.89-4.00 (1H, m), 4.08-4.16 (IK, m) , 4.20-4.29 (1H, m) , 7.37 (2H, d, J=9Hz), 7.80 (2H, d, J=9Hz) Pre p aration 31 A mixture of (S)-3-hydroxybutyl p-toluenesulfonate (2.25 g) and phthalimide potassium salt (3.41 g) in N,N- dimethylformamide (40 ml) was εtirred at 60°C for 3.5 hourε. The reεulting mixture waε diluted with water (50 ml) and the aqueouε layer was extracted with ethyl acetate. Drying, filtering and removal of solvents afforded a crude product. The crude product was chromatographed on silica gel (eluent; hexane-ethyl acetate = 2:1) to give (S)-4-(phthalimido-1-yl)-2-butanol (910 mg) . NMR (CDCI3, δ) : 1.22 (3H, d, J=7Hz) , 1.64-1.88 (2H, m) , 2.73 (1H, d, J=4Hz) , 3.68-3.78 (IK, m) , 3 . 82-3 . 89 (2H, m) , 7 . 70-7 . 77 (2H, m) , 7 . 83-7 . 89 (2H, ) Preparation 32 To an ice-bath cooled εolution of 4-methoxycarbonyl- phenylmethyl-tri-phenylphoεphonium bromide (9.75 g) in N,N-dimethylacetamide (50 ml) waε added potassium tert- butoxide (2.23 g) . After being stirred in an ice-bath for 30 minutes, 2-nitrcbenzaldehyde (3.0 g) was added to the solution and the mixture was stirred at the same temperature for 1 hour. The mixture was diluted with ethyl acetate and the solution was washed with water and brine. The organic solution waε dried over magneεium sulfate and the solvent was evaporated in vacuo to give an oil. The crude oil was subjected to silica gel column (10% ethyl acetate in n-hexane) . Trans isomer was eluted first (1.4 g) and next cis and trans mixture (3.7 g) . Methyl 4-[ (E)-2- (2-nitrophenyl)ethen-l-yl]benzoate NMR (CDC1 3 , δ) : 3.92 (3K, s) , 7.10 (1H, d, J=15Hz) , 7.41-7.50 (2H, a), 7.55-7.79 (4K, m) , 8.00 (1H, c, J=7Hz), 8.07 (2H, d, J=8Hz) Methyl 4-[E and Z)-2- (2-nitrophenyl)ethen-1- yl]benzoate NMR (CDCI3, δ) : 3.83 (3Hx2/3 (Z) , s) , 3.91 (3Hxl/3 (E), s), 6.79 (1HX2/3, d, J=12Hz) , 6.98-8.14 (9H+1/3H, m) Preparation 33 To a solution of 3-(3-ethoxycarbonyiprop-l-yl)oxy-4- nitrotoluene (2.67 g) in dichlormethane (30 ml) was added diisobutyialuminum hydride (1.5 M εolution in toluene, 7 ml) at -78°C and the solution was stirred at the same temperature for 2 hours. The reaction was σuenched with addition of small amount of water and a mixture of chloroform (30 ml) and IN hydrochloric acid (20 ml) was added. The organic phase was separated and washed with water and brine. The organic solution was dried over magnesium sulfate and the solvent was evaporated in vacuo to give an oil. A mixture of the crude aldehyde and carbethoxymethylene triphenylphosphorane (3.49 g) in tetrahydrofuran (20 ml) was stirred at ambient temperature overnight and the solvent was evaporated in vacuo. The residue was subjected to silica gel column and the column was eluted with 10% ethyl acetate in n-hexane to give 3- [ (E)-5-ethoxycarbonyl-4-penten-l-yl]oxy-4-nitrotoluene (2.29 g) . NMR (CDC1 3 , δ) : 1.27 (2H, t, J=7.5Hz), 1.93-2.04 (2H, m), 2.37 (3H, s) , 2.40-2.50 (2H, m), 4.09 (2H, t ' , J=7.5Hz), 4.18 (2H, q, J=7.5Hz), 5.89 (1H, d, J=15Hz), 6.80 (IK, d, J=7Hz) , 6.82 (1H, s), 7.00 (IK, dt, J=15, 7.5Hz), 7.78 (1H, d, J=7Hz) Preparation 34 A 300 ml of hydrogenation bottle waε flushed with nitrogen, and 10% palladium on carbon (1.5 g) was added into the bottle. A solution of benzyl 2-(3- phthalimidopropyloxy)benzoate (1.50 g) in methanol (50 ml) and 1,4-dioxane (50 ml) was added to the bottle, along with one drop of acetic acid. The mixture was shaken in a Parr apparatus at 3 atm of hydrogen at 35°C for 8 hourε. The catalyεt was removed by filtration through a bed of Celite, and washed with 1,4-dioxane (20 ml x 2) . The combined solution was concentrated with a rotary evaporator to give crude solid. The crude solid in methanol (57 ml) and 1,4-dioxane (10 ml) was heated and the product was recryεtallized on cooling. The cryεtal was collected by filtration, washed with cold methanol (5 mi) and ari-dried to give 2-(3-phthalimidopropyloxy)- benzoic acid (4.18 g) . mp : 155-157°C NMR (DMSO-dg, δ) : 1.98-2.14 (2K, m) , 3.79 (2H, t, J=7Hz), 4.08 (2H, t, J=7Hz) , 6.99 (1H, dd, J=8, 8Hz), 7.08 (IH, d, J=8Kz) , 7.47 (1H, m), 7.62 (1H, d, J=8Kz), 7.77-7.92 (4K, m) Preparation 35 A mixture of 4-amino-3-methoxy-N-[2-(4- carboxyphεnylmethyl ) oxy-4-methylphenyl]-N-methylbenzamide (500 mg) , ethanola ine (109 mg) , triphenylphoεphine (936 mg) and carbon tetrachloride (0.57 ml) in a mixture of pyridine and acetonitrile (1:1, 15 ml) was stirred at ambient temperature for 18 hours. The solvent waε evaporated and the residue was purified on silica gel column chromatography (SiO ? 0-10% methanol in chloroform) to give 4-amino-3-methoxy-N-[2-[4-[N-(2-hydroxyethyl)- carbamoyl]phenylmethyl]oxy-4-methylphenyl]-N- methylbenzamide (392 mg) . NMR (CDC1 3 , δ) : 2.27 (3H, s) , 3.33 (3H, s), 3.48 (3H, s), 3.60 (2H, σ, J=5Hz) , 3.78-3.84 (2H, m) , 4.97 (2H, br), 6.35 (IH, d, J=8Hz) , 6.61 (IH, s), 6.68-6.79 (3H, m) , 7.04 (IH, d, J=8Hz) , 7.11 (IH, br), 7.26 (2H, d, J=8Hz), 7.76 (2H, d, J=8Hz) Preparation 36 To an ice-cooled 4-amino-3-methoxy-N-[2-[4-[N-(2- nydroxyethyl)carbamoyl]phenylmethyl]oxy-4-methylphenyl]-N- methylbenza ide (387 mg) was added dropwise thionyl chloride (129 mg) , and the mixture was stirred at ambient temperature for 1 hour. The resulting mixture was added aqueouε sodium hydrogen carbonate solution (15 ml) . The solution was extracted with ethyl acetate (10 ml x 3) . The organic layer was washed with brine and dried over magnesium sulfate. The solvent was removed under reduced pressure to give 4-amino-3-methoxy-N-[2-[4-(2-oxazolin-2- yl)phenylmethyl]oxy-4-methylphenyl]-N-methylbenzamide (315 mg) . NMR (CDC1 3 , δ) : 2.26 (3H, s) , 3.35 (3H, ε), 3.52 (3H, ε), 4.08 (2K, t, J=10Hz), 4.25 (2H, t, J=10Hz), 4.94 (IH, br) , 5.07 (IH, br) , 6.40 (IH, c, J=8Hz), 6.40-6.88 (4H, m) , 7.00 (IH, d, J=8Hz), 7.36 (2K, d, J=8Hz) , 7.96 (2H, d, J=8Hz) Preparation 37 To a εolution of 3-bromopropylamine hydrobromide (5.0 g) and diisopropylethylamine (5.90 g) in dichloromethane (80 ml) was added portionwise 9-fluorenylmethoxycarbonyl chloride (5.91 g) and the mixture was stirred at ambient temperature for 3 hours and stand overnight. The resulting mixture was diluted with dichloromethane (50 ml) and the organic layer was washed successively with IN hydrochloric acid and brine. Drying, filtering and removal of solvents afforded a crude product. The crude product was triturated with diethyl ether-hexane (1:5) to give 3- (9-fluorenylmethoxycarbonylamino)propyl bromide (7.82 g) . NMR (CDCI3, δ) : 2.02-2.12 (2K, m) , 3.30-3.45 (4H, ) , 4.21 (IH, t, J=8Hz), 4.44 (2H, d, J=8Hz) , 4.82-4.90 (IH, br) , 7.32 (2H, t, J=8Hz) , 7.40 (2K, t, J=8Hz), 7.58 (2H, d, J=8Hz) , 7.78 (2H, d, J=8Hz) ESI-MASS (m/z) : 360 (M+H) Preparation 38 To a solution of thiosalicylic acid (500 mg) in ethanol (15 ml) and 2N sodium hydroxide aqueous solution (3.2 ml) was added 3-(9-fluorenylmethoxycarbonylamino)- propyl bromide at ambient temperature and the suεpenεion waε εtirred for 2 hourε. The resulting clear solution was diluted with water (20 ml) and acidified with IN hydrochloric acid (6.5 ml). White crystals were collected by filtration and the solid was washed with ethanol-water (1:3, 15 ml) and then with n-hexane - diethyl ether (2:1, 15 ml) to give 2-[3- (9-flucrenylmethoxycarbonylamino)- propylthio]benzoic acid (1.07 g) . NMR (DMSO-dg, δ) : 1.69-1.79 (2K, ) , 2.90 (2H, t, J=8Kz), 3.08-3.18 (2K, a), 4.21 (IK, t, J=6Kz) , 4.32 (2H, d, J=6Hz), 7.20 (IK, t, J=8Hz) , 7.28- 7.45 (6H, m), 7.50 (IH, t, J=8Kz) , 7.68 (2H, d, J=8Hz), 7.85-7.91 (3H, m) ESI-MASS (m/z) : 434 (M+H) Example 1 To a mixture of 2-benzyloxybenzoic acid (1.17 g) and oxalyl chloride (0.536 ml) in dichloromethane (30 ml) was added 2 drops of N,N-dimethylformamide and the mixture was stirred at ambient temperature for 1 hour. After removing a solvent by evaporation, a εolution of residual acid chloride in dichloromethane (5 ml) was added to a mixture of 4-amino-N-methyl-N-[2- (5-ethoxycarbonylpent-l- yloxy)phenyl]benzamide (1.97 g) and triethylamine (1.07 ml) in dichloromethane (5 ml) and the resulting solution was stirred at ambient temperature for 3 hours. The reaction mixture was washed succesεively with IN hydrochloric acid, water (20 ml) and brine (20 ml), and dried over magnesium sulfate. The εolvent waε evaporated to give an oil and the crude product waε purified by silica gel column (chloroform) to give 4-(2- benzyloxybenzoyl)amino-N-methyl-N-[2-(5- ethoxycarbonylpent-1-yloxy)phenyl]benzamide (2.89 g) as a colorless oil. NMR (CDC1 3 , δ) : 1.23 (3H, t, J=7.5Hz), 1.41-1.54 (2K, a), 1.63-1.75 (2H, a), 1.75-1.85 (2H, m) , 2.32 (2K, t, J=7.5Hz), 3.32 (3H, s) , 3.80-3.95 (2H, br), 4.12 (2H, q, J=7.5Hz), 5.18 (2H, s), 6.82-6.90 (2H, a), 6.92-7.00 (3K, ) , 7.07-7.19 (5H, m), 7.38-7.52 (6H, a), 8.27 (IH, d, J=7Hz) Example 2 The following compounds were obtained according to a similar manner to that of Example 1. 1) 4-(2-Benzyloxybenzoyl)amino-N-methyl-N-[2-[3-(4- methylpiperazin-1-yl)carbonylaminoprop-1-yloxy]- phenyl]benzamide NMR (CDC1 3 , δ) : 2.00 (2H, m) , 2.26 (3H, s) , 2.32-2.39 (4H, ) , 3.32 (3K, ε), 3.34-3.41 (6H, a), 3.81-4.02 (2H, m) , 5.20 (2H, ε) , 6.78-7.26 (9H, m), 7.38-7.53 (7K, a), 8.27 (IH, d, J=7Hz) 2) 3-Methoxy-4-(2-nitrobenzoyl)amino-N-methyl-N-[4- methyl-2-[5-(4-methylpiperazin-l-yl)carbonylpent-1- yloxy]phenyl]benzamide NMR (CDCI3, δ) : 1.43-1.60 (2K, m) , 1.61-1.90 (4H, m), 2.30 (6H, s) , 2.31-2.44 (6H, a), 3.33 (3H, ε), 3.44-3.53 (2H, m) , 3.57-3.67 (2H, m) , 3.71 (3K, s), 3.81-4.03 (2H, a), 6.56-6.69 (2H, m) , 6.82-6.99 (2H, a), 7.03 (IH, ε), 7.57-7.66 (2H, a), 7.67-7.76 (IH, a), 8.02-8.13 (2H, m) , 8.21 (IH, d, J=8Hz) 4-(2-Methoxybenzoyl)amino-N-methyl-N-[2-(5- ethoxycarbonylpent-1-yloxy)- -methylphenyl]benzamide NMR (CDCI3, δ) : 1.25 (3H, t, J=7Hz) , 1.43-1.59 (2H, a), 1.63-1.90 (4H, a), 2.26 (3H, s) , 2.34 (2H, t, J=7Hz), 3.32 (3H, s) , 3.79-3.99 (2H, a), 4.02 (3H, s), 4.11 (2H, q, J=7Hz), 6.53-6.66 (2H, a). 6.87 (IK, d, J=8Hz), 7.01 (IH, d, J=8Hz), 7.12 (IH, dd, J=8, 8Hz), 7.29-7.40 (2H, m) , 7.42-7.56 (3H, m), 8.18-8.28 (IH, m) , 9.81 (IH, br ε) 4) 4- (2-Benzyloxybenzoyl) amino-3-methoxy-N-methyl-N- [2- ( 5-ethoxycarbonylpent-l-yloxy ) phenyl ] benzamide NMR (CDC1 3 , δ) : 1.25 (3H, t, J=7Hz) , 1.42-1.58 (2H, m), 1.62-1.90 (4H, m) , 2.32 (2H, t, J=7Hz) , 3.28 (3H, 8), 3.33 (3K, ε), 3.78-4.03 (2H, m) , 4.12 (2H, q, J=7Hz), 5.30 (2H, ε) , 6.72-7.22 (8H, m) , 7.28-7.55 (6H, m) , 8.20-8.29 (IH, m) , 8.38 (IH, α, J=8Hz) 5) 4-[2- (Acetyloxy)benzoyl]amino-3-methoxy-N-methyl-N- [2-[5-(4-dimethylaminopiperidin-l-yl)carbonylpent-1- yloxy]-4-methylphenyl]benzamide NMR (CDCI3, δ) : 1.32-2.01 (10H, m) , 2.21-2.46 (15H, a), 1.57 (IH, m), 3.02 (IH, m) , 3.32 (3H, ε) , 3.79 (3H, ε), 3.83-4.03 (3H, m) , 4.69 (IH, m) , 6.54-6.67 (2H, m) , 6.80-8.33 (8H, m) 6) 4-[2- (Acetyloxy)benzoyl]amino-3-methoxy-N-methyl-N- [4-methyl-2- (5-ethoxycarbonylpent-l-yloxy)phenyl]- benzamide NMR (CDCI3, δ) : 1.26 (3H, t, J=7Hz) , 1.44-1.91 (6H, a), 2.21-2.41 (8H, m) , 3.32 (3H, ε) , 3.80 (3H, ε), 3.82-4.03 (2H, m) , 6.54-6.67 (2H, m) , 6.80- 6.95 (2H, a), 7.07 (IH, s) , 7.15 (IH, d, J=8Hz) , 7.35 (IK, m) , 7.51 (IK, m) , 7.94 (IH, m) , 8.28 (IH, d, J=8Hz), 8.87 (IH, ε) 7) 4-(2-Benzyloxybenzoyl)amino-2-chloro-N-methyl-N-[2- (5-εthoxycarbonylpent-1-yloxy)phenyl]benzamide NMR (CDCI3, δ) : 1.26 (3H, t, J=7Hz) , 1.47-1.98 (6H, a), 2.36 (2H, t, J=7Hz), 3.34 (3H, s) , 3.96 (2H, t, J=7Hz), 4.14 (2K, q, J=7Kz) , 5.17 (2K, s), 6.64-6.82 (3H, m) , 6.96 (IH, d, J=8Hz), 7.02- 7.21 (5K, m), 7.41-7.62 (6H, m) , 8.25 (IH, m) 8) 4-(2-Acetoxybεnzoyl)amino-3-mεthoxy-N-methyl-N-(2- methylphenyl)benzamide NMR (CDC1 3 , δ) : 2.21 (3H, s), 2.31 (3H, s), 3.38 (3H, s), 3.73 (3H, s) , 6.87 (IH, d, J=8Kz) , 7.00 (IH, s), 7.03-7.24 (5H, m) , 7.29-7.43 (IH, m) , 7.51 (IH, dd, J=8, 8Hz), 7.92 (IH, d, J=8Hz) , 8.30 (IK, d, J=8Hz), 8.87 (IK, br s) 4-(3-Benzyloxybenzoyl)amino-3-methoxy-N-methyl-N-[4- mεthyl-2-[5- (4-dimethylaminopiperidin-l- yl)carbonylpent-1-yloxy]phenyl]benzamide NMR (CDCI3, δ) : 1.32-1.42 (2H, a), 1.50-1.58 (2H, m) , 1.67-1.90 (6H, m) , 2.28 (3H, ε), 2.29 (6H, S), 2.37 (2H, t, J=8Hz), 2.52-2.62 (IH, m) , 2.98-3.07 (IH, m) , 3.34 (3H, s) , 3.78 (3H, s), 3.65-3.98 (3H, m) , 4.59-4.67 (IH, m) , 5.12 (2H, s), 6.58 (IK, d, J=8Hz), 6.63 (IH, d, J=8Hz) , 6.84 (IK, d, J=8Kz), 6.92 (IH, d, J=8Hz), 7.02 (IH, s), 7.12-7.17 (IH, m) , 7.33-7.50 (8H, m) , 8.28 (IH, d, J=8Hz), 8.48 (IH, s) ESI-MASS (m/z) : 721 (M+H) 10) 4-(2-Benzyloxybenzoyl)amino-N-[2-(5-ethoxycarbonyl- pent-1-yl)oxy-4-methyl.]phenyl-N-methylbenzamide NMR (CDCI3, δ) : 1.25 (3H, t, J=7.5Hz), 1.43-1.56 (2H, m), 1.65-1.84 (4H, m) , 2.25 (3H, s), 2.32 (2H, t, J=7.5Hz), 3.29 (3H, s) , 3.77-3.93 (2H, a), 4.12 (2K, q, J=7.5Hz), 5.19 (2H, s), 6.51 (2H, a), 6.81 (IH, d, J=7Hz) , 6.98 (2H, d, J=8Hz), 7.07-7.19 (4H, a), 7.39-7.53 (6H, a), 8.27 (IH, d, J=7Hz) 11) 4-(2-Iodobenzoyl)amino-N-[2- (4-methoxyphenyl)- methoxy]phenyl-N-methylbenzamide NMR (CDC1 3 , δ) : 3.35 (3H, s), 3.82 (3H, s), 4.90- 5.05 (2H, a), 6.83 (IH, t, J=7Hz) , 6.89-6.96 (3K, a), 7.04 (IH, d, J=7Hz) , 7.10-7.19 (2H, m) , 7.22-7.32 (4H, m) , 7.37-7.48 (3H, ) , 7.53 (IH, ε), 7.88 (IK, d, J=7Hz) 12) 3-Methoxy-4-[2-(4-methoxyρhεnylmethyl)oxybenzoyl]- amino-N-methyl-N-[4-methyl-2-[4-(4-methylpiperazin-l- yl)carbonyl]phenylmethoxy]phenylbenzamide NMR (CDCI3, δ) : 2.27 (3H, ε), 2.31 (3H, s) , 2.35- 2.52 (2K, m), 3.24 (3H, ε) , 3.37 (3H, ε), 3.40- 3.53 (2H, m), 3.62-3.81 (2H, m) , 3.39 (3H, s) , 4.89 (IH, d, J=14Hz) , 5.06 (IH, d, J=14Kz) , 5.21 (2H, s), 6.61-6.70 (2H, m) , 6.80-7.18 (7H, m) , 7.30-7.45 (7H, m) , 8.22 (IH, d, J=7Kz) , 8.31 (IH, d, J=7Hz) 13) 4- [2- (E) - (2-Ξthoxycarbonylethen-l-yl) benzoyl] amino-3- methoxy-N-methyl-N- [4-methyl- ' 2- [5- (4-methylpiperazin- 1-yl) carbonylρεnt-l-yl]oxy]phεnylbεnzamide NMR (CDCI3, δ) : 1.30 (3K, t, J=7.5Hz), 1.49-1.60 (2K, m) , 1.67-1.77 (2H, m) , 1.79-1.90 (2H, m) , 2.29 (6H, sx2), 2.33-2.43 (6K, m) , 3.33 (3H, ε) , 3.45-3.53 (2H, a), 3.60-3.67 (2H, a), 3.71 (3H, ε), 3.85-4.01 (2H, a), 4.23 (2H, q, J=7.5Hz), 6.40 . (IH, d, J=15Hz), 6.58-6.67 (2H, a), 6.86 (IH, d, J=7Hz), 6.92 (IH, d, J=7Kz) , 7.02 (IH, ε), 7.40-7.52 (2H, a), 7.58 (IH, d, J=7Hz) , 7.68 (IH, d, J=7Hz), 8.02-8.15 (2H, a), 8.27 (IK, d, J=7Hz) 14) 4- (2-Dimethylamino-4-mεthyl)phεnoxymethyl-N-[2- (5- ethoxycarbonylpent-l-yl)oxy-4-methyl]phenylbenzamide 95 - 106 - NMR (CDCI3, δ) : 1.20 (3H, t, J=7.5Kz), 1.45-1.58 (2H, m), 1.66-1.77 (2H, a), 1.80-1.95 (2H, a), 2.25 (3H, s), 2.29-2.34 (2H, a), 2.31 (3H, s) , 2.80 (6H, s), 4.00-4.16 (4H, a), 5.20 (2K, s), 6.68-6.89 (5H, a), 7.58 (2H, d, J=8Hz) , 7.88 (2H, d, J=8Hz), 8.37 (IH, d, J=7Hz), 8.50 (IH, s) 15) 4-(2-Benzyloxy)benzoylaaino-3-aethoxy-N-[ (E and Z)-2- (4-aethoxycarbonylphεnyl)ethen-1-yl]phenyl-N- methylbenzamide NMR (CDCI3, δ) : 3.06 (3Hx2/3, s) , 3.10 (3Hxl/3, s) , 3.40 (3HX2/3, s), 3.43 (3Hxl/3, ε) , 3.46 (3Hx2/3, ε), 3.91 (3Hxl/3, s) , 5.20 (2Hx2/3, s) , 5.27 (2Hxl/3, s), 6.38-8.37 (22H, m) 16) 3-Methoxy-4-[2-[3-(4-methoxyphεnyl)mεthoxyprop-l- yl]thiobenzoyl]amino-N-methyl-N-[4-methyl-2-[5-(4- methylpiperazin-1-yl)carbonylpent-l-yl]oxy]- phenylbenzamide NMR (CDCI3, δ) : 1.44-1.58 (2K, m) , 1.61-1.73 (2H, a), 1.68-1.92 (4H, a), 2.25 (3H, s), 2.27 (3H, s), 2.30-2.41 (6H, a), 2.99 (2H, t, J=7.5Hz), 3.30 (3H, s), 3.43-3.52 (4H, a), 3.57-3.66 (2H, a), 3.70 (3K, s), 3.78 (3H, s) , 3.82-3.90 (2H, a), 4.38 (2H, s), 6.53-6.65 (2H, a), 6.79-6.93 (3K, a), 7.02 (IH, s) , 7.17-7.29 (4H, a), 7.33- 7.45 (2H, a), 7.65 (IK, d, J=7Hz), 8.29 (IH, d, J=7Hz), 8.80 (IH, ε) 17) 4- (2,4-Diaethoxybenzoyl)aaino-3-methoxy-N-mεthyl-N- [4-methyl-2-[5-(4-methylpiperazin-l-yl)carbonylpent- 1-yl]oxy]phenylbenzamide NMR (CDCI3, δ) : 1.43-1.57 (2H, a), 1.64-1.72 (2H, a), 1.72-1.91 (2K, a), 2.24 (3H, s) , 2.27 (3H, s), 2.30-2.40 (6H, m) , 3.31 (3H, s) , 3.42-3.50 (2K, m), 3.59-3.65 (2H, ) , 3.77 (3H, s) , 3.80 (3K, s), 3.80-4.02 (2H, m) , 3.96 (3H, εj , 6.52- 6.63 (2K, m), 6.81-7.04 (5K, m) , 7.79 (IH, m) , 8.38 (IH, d, J=7Kz) 18) 4-[2- (Acetoxy)benzoyl]amino-3-methoxy-N-methyl-N-[4- methyl-2-[5-(4-methyipiperazin-l-yl)carbonylpent-1- yloxy]phenyl]benzamide NMR (CDC1 3 , δ) : 1.47-1.61 (2K, m) , 1.64-1.93 (4H, m), 2.22-2.46 (15H, m) , 3.33 (3H, s), 3.44-3.53 (2H, ) , 3.58-3.68 (2H, a), 3.79 (3H, s) , 3.82- 4.04 (2K, a), 6.54-6.68 [2E, a), 6.80-6.95 (2H, a), 7.04 (IH, s), 7.14 (IH, d, J=8Hz) , 7.35 (IH, a), 7.51 (IH, m) , 7.92 (IH, m) , 8.29 (IH, br d, J=8Hz), 8.86 (IK, s) 19) 4- (2-Benzyloxy-4-methylbenzoyl)amino-3-methoxy-N- methyl-N-[2-[5-(4-methylpiperazin-l-yl)carbonylpent- l-yl]oxy-4-methylphenyl]benzamide NMR (CDCI3, δ) : 1.48-1.61 (2H, m) , 1.69-1.91 (4H, a), 2.28 (3H, s), 2.30 (3H, s) , 2.32-2.44 (6H, m) , 2.38 (3H, ε), 3.20 (3H, s), 3.32 (3H, s), 3.50 (2H, t, J=5Hz), 3.64 (2H, t, J=4Hz) , 3.85- 4.06 (2H, m) , 4.89 (2H, s), 6.60-6.68 (2H, m) , 6.82-6.95 (4H, m) , 7.16 (IH, dd, J=2, 7Kz) , 7.27-7.40 (5H, a), 7.98 (IH, d, J=8Hz) , 8.38 (IH, d, J=8Hz) 20) 4- (2-Benzyloxy-4-methylbenzoyl) amino-3-mεthoxy-N- methyl-N- [2- [5- (4-methylpiperazin-l-yl) carbonylpent- 1-yl ] oxy-4-methylphenyl ] benzamide NMR (CDC1 3 , δ) : 1.47-1.86 (6H, m) , 2.28 (3H, s) , 2.30 (3H, s), 2.36 (3H, s) , 2.32-2.48 (6K, m) , 3.30 (3H, 8), 3.45-3.51 (2H, m) , 3.60-3.66 (2H, a), 3.63 (3H, s) , 3.79-4.00 (2H, a), 5.24 (2H, d, J=9Hz), 6.56-6.68 (2H, a), 6.80-6.93 (5H, a), 7.31-7.58 (5H, a), 8.11 (IH, d, J=8Hz), 8.36 (IH, d, J=8Hz) 21) 4-(2-Benzyloxy-5-methylbenzoyl)amino-3-methoxy-N- methyl-N-[2-[5-(4-methylpiperazin-l-yl)carbonylpent- I-yl]oxy-4-methylphenyl]benzamide NMR (CDC1 3 , δ) : 1.47-1.99 (8K, a), 2.28 (3H, s), 2.31 (3H, s), 2.31-2.45 (6H, a), 3.25 (3H, s) , 3.29 (2H, s), 3.48 (3H, s) , 3.48-3.53 (2H, a), 3.60-3.64 (2H, a), 3.82-4.01 (2H, a), 5.27 (2H, ε), 6.54-6.63 (2H, a), 6.81-6.95 (4H, a), 7.19- 7.47 (7H, a), 8.02 (IH, s) , 8.36 (IH, d, J=8Hz) 22) 4- (2-Benzyloxy-4-chlorobenzoyl) aaino-3-methoxy-N- mεthyl-N- [2- [5- (4-methylpiperazin-l-ylcarbonyl)pent- l-yl]oxy-4-methylphenyl] benzamide NMR (CDCI3, δ) : 1.46-1.86 (6H, a), 2.15-2.31 (2H, a), 2.29 (6H, s), 2.30-2.58 (4H, a), 3.28 (3H, s), 3.49 (2H, t, J=5Hz), 3.60 (3K, s) , 3.61 (2H, t, J=5Hz), 3.85-4. CO (2H, a), 5.15 (2K, s), 6.54-6.67 (2H, m) , 6.83-7.16 (4H, a), 7.34-7.49 (7H, a), 8.01 (IH, d, J=8Hz) , 8.19 (IH, d, J=8Hz) 23) 4-(2-Benzyloxy-4-aethoxybenzoyl)amino-3-methoxy-N- methyl-N-[2-[5-(4-methylpiperazin-l-ylcarbonyl)pent- 1-yl]oxy-4-methylphenyl]benzamide NMR (CDCI3, δ) : 1.44-1.59 (2H, a), 1.63-1.84 (4H, a), 2.28 (3H, s), 2.30 (3H, s) , 2.25-2.40 (6H, a), 3.28 (3H, s), 3.30 (3H, s) , 3.48 (2H, t, J=4Hz), 3.62 (2K, t, J=4Hz) , 3.89-4.01 (2H, a), 5.26 (2H, s), 6.52-6.67 (4K, a), 6.81-6.92 (4H, a), 7.35-7.48 (5K, a), 8.21 (IH, d, J=9Hz) , 8.3 41795 - 109 - ( IH, d, J=8Hz) 24) 4-(2-Acetoxybenzoyl)aminc-3-methoxy-N-(2-benzyloxy-4- ethylphenyl)-N-methylbenzamide NMR (CDC1 3 , δ) : 2.29 (3K, s), 3.39 (3H, s) , 3.60 (3H, ε), 4.88 (IH, d, J=12Hz) , 5.02 (IH, d, J=12Hz), 6.68-6.73 (2H, m) , 6.82 (IH, d, J=8Hz), 7.02 (IK, 8), 7.11-7.20 (2H, m) , 7.31-7.42 (5H, ), 7.46-7.53 (IH, m) , 7.93 (IH, d, J=8Hz), 8.27 (IK, d, J=8Hz), 8.86 (IK, br) 25) 4- (2-Acetoxybenzoyl)amino-3-methoxy-N-[2-[4-(2- oxazolin-2-yl)phenyl εthyl]oxy-4-mεthylphenyl]-N- methylbenzamide NMR (CDCI3, δ) : 2.27 (3H, s) , 2.31 (3H, s) , 3.39 (3H, s), 3.63 (3H, ε) , 4.07 (2H, t, J=10Hz) , 4.42 (2H, t, J=10Hz), 4.91 (IH, d, J=12Hz) , 5.11 (IH, d, J=12Hz), 6.61 (IH, br) , 6.77 (IH, d, J=8Hz), 6.82-7.15 (5H, a), 7.24-7.50 (4H, a), 7.90 (2H, d, J=8Hz) , 8.20 (IH, d, J=8Hz) 26) 4-[2-[3-(9-Fluorenylmethyl)oxycarbonylaminoprop-1- yl]thiobenzoyl]amino-3-methoxy-N-methyl-N-[2-[5-(4- dimethylaminopiperidin-1-yl)carbonylpent-l-yl]oxy-4- methylphenyl]benzamide NMR (CDCI3, δ) : 1.32-1.92 (12H, a), 2.29 (9H, s), 2.39 (2H, t, J=5Hz), 2.60 (IH, t, J=10Hz) , 2.90- 3.12.(3H, m), 3.29 (2H, q, J=5Hz) , 3.33 (3H, s) , 3.75 (3H, ε), 3.82-4.00 (4K, m) , 4.38 (2H, t, J=4Hz), 6.55-6.67 (3H, a), 6.83 (IH, d, J=8Hz) , 6.92 (IH, d, J=8Hz), 7.02 (IK, s) , 7.25-7.46 (6K, a), 7.59 (2H, d, J=7Hz), 7.63 (IH, d, J=8Hz), 7.77 (2H, d, J=8Hz) , 8.30 (IH, d, J=8Hz), 8.70 (IH, s) 27) 4-[2-(Acetyloxy)benzoyl]amino-3-methyl-N-methyl-N-[2- [5- (4-methylpiperazin-l-yl)carbonylpent-l-yloxy]-4- methylphenyl]benzamide NMR (CDC1 3 , δ) : 1.53 (2H, br) , 1.63-1.89 (4H, m) , 2.22 (3H, s), 2.30 (3H, s) , 2.36 (3K, s), 2.22- 2.50 (10K, m) , 3.32-3.38 (3H, m) , 3.52-3.57 (2H, m), 3.67 (2H, br) , 3.95 (2H, br) , 6.61 (2H, s), 6.83-6.93 (2H, m) , 7.02-7.20 (2K, m) , 7.32-7.58 (2H, m), 7.68 (IH, d, J=7Hz) , 7.85 (IH, br) 28) 4- [ (2-Benzyloxy)benzoyl]amino-3-[ (2-bεnzyloxy)- bεnzoyl]oxy-N-methyl-N- [2- [5- (4-methylpiperazin-l- yl ) carbonylpent-1-yloxy] -4-me thylphenyl ] benzamide NMR (CDCI3, δ) : 1.44-1.53 (2H, m) , 1.60-1.87 (4H, a), 2.28 (3H, s), 2.29 (3H, ε) , 2.32-2.38 (7H, a), 3.33 (3H, ε), 3.43 (2H, br) , 3.60 (2H, br) , 3.90 (2H, br), 4.79 (2H, s) , 4.93 (2H, s) , 6.11- 6.20 (3H, m), 6.82-7.43 (18H, a), 7.83-7.88 (IH, a), 8.12-8.15 (IH, a), 8.37-8.42 (IH, a) 29) 4-[4- (Benzyloxy)benzoyl]amino-3-methoxy-N-mεthyl-N- [2-[5- (4-dιaethylaainopιperidin-l-yl)carbonylpent-1- yloxy]-4-methylphenyl]benzamide NMR (CDCI3, δ) : 1.30-1.45 (IH, m) , 1.47-1.58 (2H, a), 1.60-1.75 (4H, a), 1.78-1.91 (2H, a), 2.27 (9K, ε), 2.30-2.40 (3H, a), 2.50-2.63 (IH, a), 2.95-3.07 (IH, a), 3.30 (3H, s) , 3.77 (3H, s) , 3.82-3.98 (4H, a) * 4.56-4.67 (IK, a), 5.11 (2H, s), 6.56-6.62 (2H, a), 6.80-6.93 (2H, a), 7.00- 7.05 (3H, a), 7.34-7.45 (4H, a), 7.78-7.82 (2H, a), 8.22-8.30 (IK, m) , 8.46 (IH, s) 30) 4-[4- (Benzyloxy)bεnzoyl]amιno-3-methoxy-N-methyl-N- [2-[5-(4-methylpiperazin-l-yl)carbonylpent-1-yloxy]- 4-methylphenyl]benzamide - Ill - NMR (CDCI3, δ) : 1.48-1.59 (2H, m) , 1.69-1.90 (4H, m), 2.28 (3H, s) , 2.30 (3H, s), 2.35-2.42 (6H, a), 3.31 (3H, s), 3.48-3.50 (2H, a), 3.62-3.66 (2H, a), 3.78 (3H, s) , 3.82-4.00 (2H, a), 5.13 (2H, s), 6.57-6.60 (2H, a), 6.81-6.92 (2H, a), 7.00-7.02 (3H, m), 7.30-7.43 (5H, m) , 7.78-7.82 (2H, m), 8.27 (IH, d, J=7Ez), 8.43 (IH, s) 31) 4-[2- (Benzyloxy)benzoyl]amino-2-nitro-N-methyl-N-[2- [5-(4-dimethylaminopiperidin-i-yl)carbonylpent-1- yloxy]-4-methylphenyl]benzamide NMR (CDCI3, δ) : 1.30-1.44 (2H, m) , 1.50-1.94 (8H, m) , 2.20 (3H, s) , 2.27 (6K, s) , 2.30-2.43 (3H, a), 2.52-2.63 (IH, a), 2.97-3.10 (IH, a), 3.32 (3H, s), 3.85-3.97 (4K, a), 4.57-4.68 (IH, a), 5.20 (2H, s), 6.41-6.48 (2H, a), 6.52 (IH, s) , 6.90-6.93 (IH, a), 7.11-7.20 (3H, a), 7.32 (IH, s), 7.48-7.59 (6H, m) , 7.69-7.73 (IH, a), 8.29 (IK, d, J=7Hz) 32) 2-[2- (Benzyloxy)benzoyl]amino-N-methyl-N-[2-[5- (4- dimethylaminopiperidin-1-yl)carbonylpent-l-yloxy]-4- methylphenyl]-5-pyridinecarboxaaide NMR (CDCI3, δ) : 1.30-1.44 (2K, a), 1.44-1.60 (2H, a), 1.60-1.95 (6K, ) , 2.20 and 2.28 (total 9H, s), 2.29-2.41 (3H, a), 2.47-2.64 (IH, m) , 2.93- 3.09 (IH, m) , 3.32 (3H, s) , 3.79-3.98 { ή', a), 4.57-4.69 (IK, a), 4.97-5.17 (IH, a), 5.32 (IH, ε), 6.39-6.50 (IH, a), 6.60-6.78 (2H, a), 6.85- 6.90 (IK, a), 7.00-7.12 (2H, a), 7.27-7.50 (7H, a), 7.56-8.25 (2H, a) Example 3 To a mixture of 2-benzyloxybenzoic acid (1.55 g) and oxalyl chloride (1.18 ml) in dichloromethane (30 ml) was added 1 drop of N,N-dimethylformamide and the mixture was stirred at ambient temperature for 1 hour. After removing a solvent by evaporation, a solution of residual acid chloride in dichloromethane (30 ml) was added to a mixture of 4-amino-3-methoxy-N-methyl-N-[4-methyl-2-[5-(4- methylpiperazm-l-ylcarbonyl)pent-l-yloxy]phenyl]benzamide (3.28 g) and pyridine (1.1 ml) in dichloromethane (50 ml) and the mixture was stirred at ambient temperature for 2.5 hours. The mixture was washed with saturated sodium hydrogen carbonate solution and brine, and dried over sodium sulfate. The solvent was removed by evaporation and purified by silica gel column chromatography (Si0 2 ; 85 g, 2% methanol in dichloromethane) to give 4-(2- benzyloxybenzoyl)amino-3-methoxy-N-methyl-N-[2-[5-(4- methylpiperazin-l-ylcarbonyl)pent-l-yloxy]-4- me hylphenyl]benzamide (4.5 g) . NMR (CDC1 3 , δ) : 1.44-1.59 (2H, a), 1.62-1.90 (4H, a), 2.27 (3K, s), 2.28 (3H, s), 2.30-2.43 (6H, m) , 3.30 (3H, s), 3.32 (3K, s), 3.43-3.53 (2H, m) , 3.57-3.67 (2H, ) , 3.78-4.03 (2H, m) , 5.30 (2K, s), 6.52-6.66 (2H, a), 6.78-6.96 (3H, a), 7.04 (IH, d, J=9Kz), 7.10 (IH, dd, J=9, 9Hz) , 7.30-7.49 (6H, a), 8.20-8.28 (IH, a), 8.37 (IH, d, J=9Hz) Example 4 A solution of 4- (2-benzyloxybenzoyl)aaino-N-aethyl-N- [2- (5-ethoxycarbonylpent-l-yloxy)phenyl]benzaaide (2.80 g) in a aixture of ethanol (50 ml) and IN sodium hydroxide solution (10 ml) was stirred at ambient temperaturε for 4 hours. After removing ethanol by evaporation, the aqueous solution was adjusted to pH 2 with IN hydrochloric acid and the mixture was extracted with chloroform (30 x 2) . The organic phase was washed with water (40 ml) and brine (30 ml), and dried over magnesium sulfate. The solvent was evaporated to give 4-(2-benzyloxybenzoyl)- amino-N-methyl-N-[2- (5-carboxylpent-l-yloxy)phenyl]- benzamide (1.76 g) as a colorless oil. NMR (CDC1 3 , δ) : 1.45-1.57 (2H, m) , 1.66-1.83 (4H, a), 2.37 (2H, t, J=7.5Hz), 3.32 (3H, s) , 3.78- 3.96 (2H, br), 5.17 (2K, s) , 6.75-6.82 (2H, a), 6.93-7.02 (3H, a), 7.10-7.22 (5H, a), 7.36-7.51 (6H, m), 8.28 (IH, d, J=7Hz) Example 5 The following compoundε were obtainεd according to a εimilar manner to that of Example 4. 1) 4-[2- (Carboxymethoxy)benzoyl]amino-N-methyl-N-[2-[5- (4-methylpiperazin-l-yl)carbonylpent-1-yloxy]phenyl]- benzamide NMR (CDCI3, δ) : 1.63 (2H, m) , 1.73 (2H, m) , 1.85 (2H, m), 2.28 (3K, s) , 2.35-2.41 (6H, m) , 3.36 (3H, s), 3.47 (2H, m) , 3.61 (2H, m) , 3.91 (2H, m), 4.76 (2H, ε) , 6.72-6.82 (2H, m) , 6.86-7.01 (2H, m) , 7.07-7.16 (2H, m) , 7.35 (2H, d, J=8.5Hz), 7.47 (IH, t, J=7Hz) , 7.72 (2H, d, J=8.5Hz), 8.25 (IH, d, J=7Hz) 2) 4-(2-Aminobenzoyl)amino-N-methyl-N-[2-(5-carboxypent- 1-yloxy)-4-methylphenyl] enzamide NMR (CDCI3, δ) : 1.45-1.59 (2H, m) , 1.64-1.85 (4H, a), 2.27 (3H, ε) , 2.38 (2H, t, J=7Hz) , 3.32 (3H, ε), 3.73-4.00 (2H, m) , 6.56-6.76 (4H, m) , 6.93 (IH, d, J=9Hz), 7.18-7.48 (6H, m) , 7.86 (IH, br ε) 3) 4-(2-Methoxybenzoyl)amino-N-methyl-N-[2-(5- carboxypent-1-yloxy)-4-methylphεnyl]benzamide NMR (CDCI3, δ) : 1.46-1.62 (2K, m) , 1.65-1.88 (4H, a), 2.26 (3H, ε), 2.39 (2H, t, J=7Hz) , 3.33 (3H, ε), 3.73-4.00 (2H, a), 4.01 (3K, s), 6.54-6.68 (2H, a), 6.91 (IK, br d, J=9Hz), 6.99 (IH, d, J=9Hz), 7.10 (IH, dd, J=9, 9Hz), 7.35 (2H, br d, J=9Hz), 7.41-7.57 (3H, a), 8.17-8.27 (IH, m) , 9.84 (IH, br s) 4) 4-(2-Benzyloxybenzoyl)amino-3-aethoxy-N-aethyl-N-[2- (5-carboxypent-l-yloxy)phenyl]benzamide NMR (CDC1 3 , δ) : 1.43-1.60 (2H, a), 1.62-1.88 (4H, a), 2.38 (2H, t, J=7Hz) , 3.28 (3H, s) , 3.34 (3H, s), 3.76-4.02 (2H, a), 5.28 (2H, s) , 6.74-6.85 (2H, a), 6.86-6.97 (2H, a), 6.97-7.20 (4H, a), 7.28-7.50 (6H, m) , 8.16-8.27 (IH, a), 8.36 (IH, a, J=8Hz) 5) 4-[2-[ (3-tert-Butoxycarbonylaminoprop-l- yl)oxy]benzoyl]amino-3-methoxy-N-methyl-N-[2- (5- carboxypent-1-yloxy)-4-methylphenyl]benzamide NMR (CDCI3, δ) : 1.31-1.96 (17H, a), 2.00-2.48 (6H, a), 3.14-3.39 (5H, a), 3.62-4.07 (5H, a), 4.10- 4.30 (2H, a), 4.86 (IH, a), 6.52-6.72 (2H, m) , 6.81-7.16 (5H, m) , 7.37-7.53 (2H, m) , 8.11-8.51 (2H, a) 6) 4-(2-Benzyloxybenzoyl)amino-2-chloro-N-methyl-N-[2- (5-carboxypent-l-yloxy)phenyl]benzamide NMR (CDCI3, δ) : 1.50-1.67 (2H, m) , 1.68-1.98 (4H, a), 2.42 (2H, t, J=7Hz), 3.34 (3H, s), 3.99 (2H, t, J=7Hz), 5.16 (2K, ε), 6.65-6.80 (3H, m) , 6.98 (IH, d, J=8Hz), 7.02-7.22 (5K, a), 7.40-7.61 (6H, a), 8.24 (IH, a) 7) 4- [2- [ (3-tert-Butoxycarbonylaminoprop-l-yl) oxy]- benzoyl]amino-3-mεthoxy-N-methyl-N- [4- (5-carboxypent- 1-yloxy)phenyl]benzamide NMR (CDCI3, δ) : 1.40 (9H, s) , 1.45-1.80 (8H, m) , 2.18-2.27 (2H, a), 2.32-2.40 (2H, a), 3.25-3.35 (2H, a), 3.48 (3H, s), 3.80 (3H, s), 3.93 (2H, t, J=6Hz), 4.19-4.28 (2H, m) , 4.73-4.83 (IH, br), 6.73-6.80 (3H, m) , 6.93-7.12 (6H, m) , 7.46 (IK, t, J=8Hz), 8.17-8.27 (IH, m) ESI-MASS (m/z) : 686 (M+Na) 8) 4-[2-(3-Aminoprop-l-yl)oxybenzoyl]amino-N-[2-(5- carboxypent-1-yl)oxy-4-methyi]phenyl-N- mεthylbenzamide NMR (DMSO-dg, δ) : 1.31-1.80 (6H, a), 1.95-2.07 (4H, a), 2.22 (3H, s), 2.86 (2H, t, J=7.5Hz), 3.16 (3K, s), 3.70 (IH, m) , 3.93 (IH, m) , 4.16 (2H, t, J=7.5Hz), 6.65 (IK, d, J=7Hz) , 6.78 (IH, s) , 7.00-7.10 (2H, m), 7.20 (IH, d, J=7Hz) , 7.23 (2H, d, J=8Hz), 7.43-7.62 (4H, m) 9) 4-[2-[3-(tert-Butoxycarbonyl)aminoprop-1- yl]oxybenzoyl]amino-N-[2-(5-carboxypent-l-yl)oxy-4- mεthyl]phenyl-N-methylbenzamide NMR (CDCI3, δ) : 1.36-1.50 (2H, a), 1.41 (9H, s) , 1.50-1.62 (2K, a), 1.66-1.84 (2H, a), 2.05-2.19 (2H, a), 2.25 (3H, ε) , 2.36-2.44 (2H, a), 3.23- 3.41 (2K, a), 3.31 (3H, ε) , 3.77-4.00 (2H, a), 4.16-4.29 (2H, a), 4.88 (IH, br) , 6.53-6.67 (2H, a), 6.98 (2H, d, J=8Hz) , 7.08 (IH, m) , 7.30-7.53 (3H, a), 8.11 (IH, a) 10) 4-[ (2-Benzyloxy)benzoyl]aaino-N-[2- (3-carboxyprop-l- yl)oxy]phenyl-N-aethylbenzaaide NMR (DMSO-dg, δ) : 1.90-2.01 (2H, a), 2.42 (2H, t, J=7.5Hz), 3.20 (3H, ε) , 3.85-4.02 (2H, a), 5.20 (2H, s), 6.85 (IH, t, J=7Hz) , 6.98 (IH, d, J=7Hz), 7.09 (IK, t, J=7Hz), 7.15-7.37 (6H, m) , 7.49 (2H, d, J=8Hz), 7.62 (IH, d, J=7Hz) 11) 4-(2-Iodobenzoyl)amino-N-[2-(5-carboxypent-l- yl)oxy]phenyl-N-methylbenzamide NMR (CDC1 3 , δ) : 1.45-1.58 (2H, a), 2.65-2.75 (2H, a), 2.75-2.84 (2H, a), 2.35 (2K, t, J=7.5Hz), 3.32 (3H, s), 3.82-3.98 (2H, m) , 6.77-6.86 (2H, m), 7.04 (IK, d, J=7Hz), 7.09-7.21 (2H, m) , 7.28-7.48 (5H, m) , 7.82-7.90 (2H, n) 12) 4- (2-Dimethylamino-4-methyl)phenoxymethyl-N-[2-(5- carboxypent-1-yl)oxy]phenyl-N-methylbenzamide NMR (CDCI3, δ) : 1.38-1.52 (2H, m) , 1.59-1.69 (2H, m) , 1.72-1.85 (2H, a), 2.23 (3H, s) , 2.25 (3H, s), 2.30 (2H, t, J=7.5Hz), 2.75 (6H, s) , 3.33 (3H, s), 3.11-3.25 (2H, a), 3.88-4.00 (2H, a), 5.02 (2K, s), 6.56-6.67 (3H, a), 6.71 (IH, d, J=7Hz), 6.90-6.99 (2H, a), 7.24 (2H, d, J=8Hz) , 7.38 (2H, d, J=8Hz) 13) 3-Methoxy-4-[2-[1-(tert-butoxycarbonyl)piperidin-4- yl]oxybenzoyl]aaino-N-[2- (5-carboxypent-l-yl)oxy-4- mεthyl]phεnyl-N-methylbenzamide NMR (CDCI3, δ) : 1.40-1.57 (2H, m) , 1.45 (9H, s) , 1.60-1.94 (6H, m) , 2.01-2.22 (2H, a), 2.29 (3H, s), 2.38 (2H, t, J=7.5Hz), 2.97-3.20 (2H, m) , 3.33 (3H, s), 3.41 (2H, t, J=7.5Hz), 3.71 (3H, ε), 3.78-4.00 (2H, m) , 4.67 (IH, m) , 6.60-6.65 (2H, m), 6.87-7.12 (5H, a), 7.44 (IH, t, J=7Hz) , 8.20 (IK, d, J=7Hz), 8.40 (IH, d, J=7Hz) 14) 3-Methoxy-4-[2- [3- (tert-butoxycarbonyl) aaino-1- aethylprop-1-yl) oxybenzoyl] aaino-N- [2- (5-carboxypent 1-yl ) oxy-4-aethyl ] phenyl-N-methylbenzamide NMR (CDCI3, δ) : 1.40 (9H, s) , 1.42 (3H, d, J=7.5Hz), 1.43-1.96 (8H, m) , 2.25 (3H, ε), 2.33- 2.42 (2H, m), 3.11-3.33 (2H, m) , 3.33 (3H, s), 3.65-3.97 (5H, m) , 4.70 (IH, a), 6.53-6.70 (2H, a), 6.79-7.13 (4H, a), 7.44 (IH, t, J=7Hz) , 8.23 (IH, a), 8.39 (IH, a) 15) 4-[2-[3- (tεrt-Butoxycarbonylamino)prop-l- yl]oxybenzoyl]amino-3-methoxy-N-[2-(3-carboxypyrid-6- yl)methoxy-4-methylphenyl]-N-methylbenzamide NMR (CDCI3, δ) : 1.40 (9H, s) , 2.05-2.16 (2K, m) , 2.27 (3H, ε), 3.28 (2H, br) , 3.42 (3H, br) , 3.58 (3H, br), 3.86-4.00 (2H, a), 4.10-4.25 (2H, a), 4.95 (IH, br), 5.16 (IH, br) , 6.62 (3H, br) , 6.86-7.18 (4H, a), 7.41 (3H, br) , 8.14 (IH, br) , 8.33 (IH, br), 9.17 (IH, br) 16) 4-[2-(E)-(2-Carboxyethen-l-yl)benzoylaaino-3-methoxy- N-methyl-N-[4-methyl-2-[5-(4-methylpiperazin-l- yl)carbonylpent-1-yl]oxy]phenylbenzamide NMR (CDCI3, δ) : 1.50-2.00 (6H, m) , 2.27-2.52 (10H, a), 2.60-2.81 (2H, a), 3.31 (3H, s) , 3.43-3.66 (2H, a), 3.83-4.22 (7H, a), 5.60 (IH, a), 6.57 (IH, a), 6.65-6.76 (4H, m) , 7.01-7.12 (2H, a), 7.21 (IH, d, J=7Hz), 7.42-7.60 (3H, a), 7.85 (IK, a) 17) 4-[2-(3-Carboxyprop-lryl)oxybenzoyl]amino-3-methoxy- N-methyl-N-[4-methyl-2-[5- (4-methylpipεrazin-l- yl)carbonylpent-1-yl]oxy]phenylbenzamide NMR (CDCI3, δ) : 1.44-1.57 (2H, a), 1.64-1.75 (2H, a), 1.75-1.87 (2H, a), 2.20 (3H, ε) , 2.34 (3H, s), 2.35-2.50 (6H, a), 2.61-2.74 (2H, a), 3.30 (3H, s), 3.33-3.46 (2H, a), 3.49-3.69 (4H, a), 3.75 (3H, s) , 3.90-4.02 (2H, a), 4.17-4.27 (2H, a) , 6.56-6.72 (2H, a) , 6. 83-6. 92 (2H, a) , 6.93- 7 .00 (2H, a) , 7 .07 (IK, t, J=7Hz) , 7 . 43 (IH, t, J=7Hz) , 7.43 (IH, t, J=7Hz) , 8 .20 (IH, d, J=7Hz) , 8 .40 (IH, d, J=7Hz) 18) 4-[2-(Carboxymethoxy)benzoyl]amino-3-methoxy-N- methyl-N-[2-[5-(4-methylpiperazin-l-yl)carbonylpent- 1-yl]oxy-4-methylphenyl]benzamide NMR (CDC1 3 , δ) : 1.51-1.92 (6H, m) , 2.02 (3H, s) , 2.30 (3H, ε), 2.32 (2H, t, J=5Hz) , 2.43-2.68 (4H, a), 3.33 (3H, s) , 3.40-3.55 (4H, m) , 3.72 (3H, s), 3.75-4.07 (2H, a), 4.73 (2H, s), 6.57- 6.68 (2H, a), 6.81-7.10 (6H, a), 7.35-7.45 (IH, a), 8.18 (IH, d, J=7Hz), 8.32 (IH, d, J=8Hz) Example 6 A mixture of 4-[2-[3-(phthalimido)prop-l-yl]oxy]- benzoylamino-N-methyl-N-[2-[5- (4-methylpiperazin-l- yl)carbonylpent-1-yloxy]phenyl]benzamide (470 mg) and hydrazine hydrate (158 mg) in ethanol (5 ml) was stirred at ambient temperature for 6 hours and filtered through a bed of Celite. The filtrate was evaporated and the residue was subjected to silica gel column. The column was eluted with a mixture of chloroform, methanol and aqueous ammonia (10:1:0.1). The object fractions were evaporated to give 4-[2-[ (3-aminoprop-l-yl)oxy]benzoyl]- amino-N-mεthyl-N-[2-[5-(4-methylpiperazin-l-yl)- carbonylpent-1-yloxy]phenyl]benzamide (256 mg) as a colorleεε amorphous. NMR (CDCI3, δ) : 1.56 (2H, m) , 1.74 (2H, a), 1.87 (2H, m), 2.09 (2H, m) , 2.29 (3H, s), 2.34-2.43 (6H, a), 2.97 (2H, t, J=7.5Hz), 3.33 (3H, s) , 3.50 (2H, m) , 3.65 (2H, ) , 3.96 (2H, ) , 4.30 (2H, t, J=7.5Kz), 6.73-6.83 (2H, m) , 6.95-7.03 (2H, m) , 7.77-7.16 (2K, m) , 7.34 (2H, d. J=8.5Hz), 7.42-7.50 (3H, m) , 8.22 (IH, d, J=7Hz) Example 7 The following compoundε wεre obtained according to a similar manner to that of Example 6. 1) 4- [2- (3-Aminoprop-l-yl)oxy]benzoylamino-N-methyl-N- [2-[3- (4-methylpiperazin-l-yl) carbonylaminoprop-1- yloxy]phenyl]benzamide NMR (CDC1 3 , δ) : 2.00 (2H, m) , 2.10 (2H, m) , 2.27 (3H, s), 2.34-2.39 (4H, a), 2.98 (2H, t, J=7.5Hz), 3.35 (3H, s) , 3.35-3.61 (6H, a), 3.98 (2H, a), 4.30 (2K, t, J=7.5Hz), 6.80-6.91 (2H, a), 7.02 (2K, d, J=7Hz) , 7.07-7.21 (3H, a), 7.33-7.51 (5H, a), 8.22 (IH, d, J=7Hz) 2) 4-[2-[ (3-Aminoprop-l-yl)oxy]benzoyl]amino-3-methoxy- N-methyl-N- [4-methyl-2- [5- (4-methylpiperazin-l- yl) carbonylpent-1-yloxy]phenyl]benzamide NMR (CDCI3, δ) : 1.53 (2H, ) , 1.70 (2H, m) , 1.84 (2H, m), 2.07 (2H, m) , 2.26 (3H, s) , 2.28 (3H, s), 2.31-2.40 (6H, m) , 2.90 (2H, t, J=7.5Hz), 3.32 (3H, s), 3.49 (2H, m) , 3.60 (2H, m) , 3.89 (3H, s), 3.82-3.99 (2H, m) , 4.28 (2H, t, J=7.5Hz), 6.54-6.64 (2H, m) , 6.82-6.94 (2H, a), 7.00-7.11 (3H, a), 7.45 (IH, m) , 8.20 (IH, a) , 8.39 (IH, a) 3) (R) -4- [2- [ (4-Aminobut-2-yl) oxy] benzoyl ] amino-3- methoxy-N-methyl-N- [4-methyl-2- [5- (4-methylpipεrazin- 1-yl ) carbonylpent-1-yloxy] phenyl ] benzamide NMR (CDCI3, δ) : 1.42 and 1.45 (total 3K, ε) , 1.50- 1.89 (8H, m), 2.02-2.12 (IK, a), 2.29 (3K, s) , 2.31 (3H, s), 2.33-2.42 (6H, a), 2.84-2.90 (2H, a), 3.33 (3H, s) , 3.46-3.52 (2H, a), 3.60-3.67 (2H, a), 3.80 (3H, ε), 3.87-4.00 (2H, m) , 4.78-4.87 (IH, m), 6.58 (IH, d, J=7Hz), 6.65 (IH, s), 6.82-6.92 (2H, m) , 7.03-7.10 (3H, m) , 7.45 (IH, t, J=8Hz), 8.21 (IH, dd, J=l, 8Hz) , 8.40 (IH, d, J=7Hz) ESI-MASS (m/z) : 674 (M+H) 4) (R)-4-[2-[ (4-Aminobut-2-yl)oxy]benzoyl]amino-3- methoxy-N-mεthyl-N-[4-methyl-2-[5-(4- dimethylaminopiperidin-1-yl)carbonylpent-1- yloxy]phenyl]benzamide NMR (CDC1 3 , δ) : 1.43 and 1.45 (total 3H, s), 1.46- 1.91 (12K, m), 2.02-2.12 (IH, m) , 2.29 (9H, ε), 2.30-2.41 (4H, m) , 2.52-2.63 (IK, a), 2.87 (2H, t, J=8Hz), 2.97-3.07 (IH, m) , 3.35 (3H, ε) , 3.80 (3H, ε), 3.87-3.98 (4H, a), 4.59-4.68 (IH, m) , 4.79-4.88 (IH, m) , 6.59 (IH, d, J=8Hz) , 6.64 (IH, ε), 6.83-6.93 (2H, a), 7.05-7.10 (3H, a), 7.45 (IH, t, J=8Hz), 8.23 (IH, d, J=9Hz) , 8.42 (IH, d, J=8Hz) ESI-MASS (a/z) : 702 (M+H) 5) (S)-4-[2-[ (4-Aainobut-2-yl)oxy]benzoyl]amino-3- methoxy-N-methyl-N-[4-methyl-2-[5-(4- dimethylaminopiperidin-1-yl)carbonylpent-1- yloxy]phenyl]benzamide NMR (CDCI3, δ) : 1.43 and 1.45 (total 3H, s), 1.46- 1.92 (12H, m), 2.02-2.13 (IH, m) , 2.28 (9H, s) , 2.30-2.40 (4H, a), 2.52-2.63 (IH, a), 2.86 (2H, t, J=8Hz), 2.97-3.07 (IH, a), 3.35 (3H, ε) , 3.81 (3K, ε), 3.87-3.98 (4H, a), 4.60-4.68 (IH, m) , 4.79-4.89 (IK, m) , 6.59 (IK, d, J=8Kz) , 6.54 (IK, ε), 6.83-6.93 (2H, m) , 7.05-7.10 (3H, m) , 7.46 (IH, t, J=8Hz), 8.23 (IH, d, J=9Hz) , 8.43 (IH, d, J=8Hz) 95 - 121 - ESI-MASS (m/z) : 702 (M+H) 6) 4-[2-[4-Aminobut-l-yl)oxybenzoyl]amino-N-methyl-N-[2- [5- (4-methylpiperazin-l-yl)carbonylpent-1- yl]oxy]phenylbenzamide NMR (CDC1 3 , δ) : 1.47-1.74 (8H, m) , 1.77-1.88 (2H, a), 1.95-2.06 (2H, a), 2.27 (3H, s) , 2.31-2.40 (4H, a), 2.78 (2H, t, J=7.5Hz), 3.32 (3H, s) , 3.45-3.50 (2H, a), 3.58-3.65 (2H, a), 3.84-3.98 (2H, m), 4.20 (2H, t, J=7.5Hz), 6.72-6.80 (2H, a), 6.93-7.00 (2H, a), 7.04-7.14 (2H, a), 7.30 (2H, d, J=8Hz), 7.40-7.48 (3H, a), 8.19 (IH, d, J=7Hz) 7) 4-[2- (3-Aminoprop-l-yl)oxybenzoyl]amino-N-[2-(5- ethoxycarbonylpent-1-yl)oxy-4-methyl]phenyl-N- methylbenzamide NMR (CDCI3, δ) : 1.24 (3H, t, J=7.5Hz), 1.44-1.56 (2H, m) , 1.63-1.87 (6H, a), 2.06-2.16 (2H, a), 2.28 (3H, s), 2.33 (2H, t, J=7.5Hz), 2.97 (2H, t, J=7.5Hz), 3.30 (3H, s) , 3.82-3.96 (2H, a), 4.11 (2H, q, J=7.5Hz), 4.30 (2H, t, J=7.5Hz), 6.54-6.60 (2H, a), 6.83 (IH, d, J=7Hz) , 7.00 (IH, d, J=7Hz), 7.09 (IH, t, J=7Hz) , 7.30 (2H, d, J=8Hz), 7.41-7.48 (3H, a), 8.20 (IH, d, J=7Hz) 8) 4-[2- (3-Aminoprop-l-yl.)oxybenzoyl]amino-N-mεthyl-N- [2-[3-(4-methylpiperazin-l-yl)carbonylprop-1- ylJoxy]phenylbenzamide NMR (CDCI3, δ) : 2.03-2.17 (2H, m), 2.29 (3H, s) , 2.33-2.42 (2H, m) , 2.53 (2K, t, J=7.5Hz), 2.96 (2H, t, J=7.5Hz), 3.38 (3H, s) , 3.46-3.53 (2H, a), 3.59-3.68 (2H, a), 3.92-4.08 (2H, a), 4.28 (2H, t, J=7.5Hz), 6.77-6.83 (2H, a), 6.93-7.18 (4H, a) , 7 .31 (2H, d, J=8Hz) , 7 .43-7 .5C (3H, m) , 8 .20 (IH, d, J=7Hz) 9) 4-[2- (3-Aminoprop-l-yl)oxybenzoyl]amino-N-methyl-N- [4-methyl-2-[4-(4-methylpiperazin-l-yl)carbonyl]- phenylmethoxy]phenylbenzamide NMR (CDC1 3 , δ) : 2.02-2.14 (2H, m) , 2.37 (3H, s) , 2.30 (3H, s), 2.32-2.51 (4H, m) , 2.94 (2H, t, J=7.5Hz), 3.35 (3H, s) , 3.41-3.57 (2H, m) , 3.67- 3.86 (2H, m) , 4.30 (2H, t, J=7.5Hz), 4.96 (IH, d, J=14Hz), 5.08 (IK, d, J=14Hz) , 6.63-6.71 (2H, m) , 6.95-7.02 (2H, m) , 7.11 (IH, t, J=7Hz), 7.31 (2H, d, J=8Hz), 7.36-7.50 (7H, a), 8.22 (IH, d, J=7Hz) 10) 4-[2-(4-Amino-l-butyn-l-yl)benzoyl]amino-N-methyl-N- [2-[5-(4-methylpiperazin-l-yl)carbonylpent-1- yl]oxy]phenylbenzamide NMR (CDCI3, δ) : 1.42-1.90 (10H, m) , 2.28 (3H, ε) , 2.32-2.41 (6H, m) , 3.37 (3K, s) , 3.46-3.51 (2H, m) , 3.59-3.67 (2K, a), 3.82-4.02 (2H, a), 6.73- 6.82 (2H, a), 7.00 (IK, d, J=7Hz) , 7.08-7.20 (2H, a), 7.35-7.64 (5H, a), 7.81-7.88 (2H, a) 11 ) 4- [2- (4-Aminobut-l-yl) benzoyl ] amino-N-methyl-N- [2- [5- ( -aethylpiperazin-l-yl ) carbonylpent-1- yl ] oxy] phenylbεnzaaide MASS (a/z) : 614 (M+1-) 12 ) 4- [2- (3-Aainoprop-l-yl ) oxybenzoyl ] aaino-3-aethoxy-N- methyl-N- [4-methyl-2- [4- (4-methylpiperazin-l- yl ) carbonyl ] phenylmethoxy] phenylbenzamide NMR (CDCI3, δ) : 2.01-2 .11 (2H, m) , 2 .28 (3H, s ) , 2 .31 (3H, ε) , 2 .33-2.51 (4H, m) , 2 .90 (2H, t, J=7 .5Hz) , 3 .39 (3H, s ) , 3 .40-3 .52 (2H, m) , 3. 61- 3 . 86 (2H, m) , 3 . 67 (3H, s ) , 4 . 79 (2H, t, J=7 .5Hz) , 4 .90 (IH, d, J=14Hz) , 5. 08 (IH, d, J=14Hz) , 6. 61-6.70 (2H, a) , 7.86 ( IH, d, J=7Hz) , 6. 94-7 . 10 (4H, a) , 7 .31-7 . 46 (5H, a) , 8 .20 (IH, d, J=7Hz) , 8 .37 (IH, d, J=7Hz ) 13) 3-Mεthoxy-4-[2-(3-aminoprop-l-yl)oxy]phenylmethyl]- amino-N-methyl-N-[4-methyl-2-[5- (4-methylpiperazin-l- yl)carbonylpent-l-yl]oxy]phenylbεnzamide NMR (CDC1 3 , δ) : 1.45-1.54 (2H, m) , 1.62-1.71 (2H, a), 1.76-1.85 (2H, a), 1.87-2.00 (2H, a), 2.27 (3H, s), 2.30 (3H, s), 2.31-2.40 (4K, m) , 2.90 (2H, t, J=7.5Hz), 3.28 (3H, s) , 3.45-3.50 (2H, a), 3.57-3.64 (2H, a), 3.61 (3H, s) , 3.80-3.97 (2H, a), 4.07 (2H, t, J=7.5Hz), 4.27 (2K, s) , 4.70 (IH, br), 6.37 (IH, d, J=7Hz) , 6.59 (IH, d, J=7Hz), 6.62 (IH, s) , 6.78 (IH, s) , 6.82-6.90 (4H, a), 7.16-7.71 (2H, a) 14) 4-[2-(3-Aminoprop-l-yl)oxybenzoyl]amino-3-methoxy-N- methyl-N-[2-[4-(4-methylpiperazin-l-yl)carbonyl]- phenyleth-1-yl]phenylbenzamide NMR (CDCI3, δ) : 2.00-2.11 (2H, a), 2.29 (3K, s) , 2.32-2.50 (4H, a), 2.61-2.93 (6H, m) , 3.32 (3H, s), 3.35-3.89 (2H, a), 3.59-3.81 (2H, a), 3.71 (3H, s), 4.22-4.32 (2H, a), 6.83 (IH, d, J=7Hz), 6.94-7.33 (11H, a), 7.43 (IH, t, J=7Hz) , 8.20 (IH,. d, J=7Hz), 8..39 (IH, d, J=7Kz) 15) 4-[2-(3-Aminoprop-l-yl)thiobenzoyl]amino-3-methoxy-N- methyl-N-[4-methyl-2-[5-(4-methylpiperazin-l- yl)carbonylpent-1-yl]oxy]phenylbenzamide MASS (m/z) : 676 (M+l) 16) 4-[2- (3-Aminoprop-l-yl)sulfonylbεnzoyl]amino-3- methoxy-N-methyl-N-[4-methyl-2-[5-(4-methylpiperazin- l-yl)carbonylpent-l-yl]oxy]phenylbenzaaide MASS (m/z) : 724 (M+l) 17) 4- [2- (3-Aminoprop-l-yl) oxybenzoyl] amino-3-methoxy-N- [2- [4- (4-dimethylaminopiperidin-l-yl) carbonyl] - phenylmethoxy-4-methyl] phenyl-N-methylbenzamide MASS (m/z) : 708 (M+l ) 18 ) 4- [2- (3-Aminoprop-l-yl) oxybenzoyl] amino-3-methoxy-N- methyl-N- [2- [3- (4-methylpiperazin-l- yl ) carbonylmethoxyprop-1-yl ] oxy] phenylbenzamidε NMR (CDC1 3 , δ) : 2.00-2.14 (4H, a) , 2.23 (3H, s) , 2.29-2.38 (4K, m) , 2.88 (2H, t, J=7.5Kz) , 3.35 (3H, s) , 3.37-3.45 (2H, a) , 3.54-3.61 (2H, a) , 3.66-3.76 (2H, a), 3.77 (3K, s) , 3.94-4.17 (4H, a), 4.30 (2K, t, J=7.5Hz), 6.75-7.18 (8H, a), 7.45 (IK, t, J=7Hz), 8.20 (IH, d, J=7Hz) , 8.42 (IH, d, J=7Hz) 19) 4-[2-(3-Aminoprop-l-yl)oxybenzoyl]amino-3-methoxy-N- [2-[ (E)-5-(4-dimethylaminopiperidin-l-yl)carbonyl-4- penten-1-yl]oxy-4-methyl]phenyl-N-methylbenzamide MASS (m/z) : 686 (M+l) 20) 3-Methoxy-4-[2-[3-(tert-butoxycarbonyl)aminoprop-1- yl]oxybεnzoyl]amino-N-[2- (4-aminobut-l-yl)oxy-4- methyl]phenyl-N-methylbenzamide NMR (CDCI3, δ) : 1.41 (9H, s) , 1.50-1.67 (2H, m) , 1.77-1.89 (2H, m) , 2.06-2.21 (2H, m) , 2.27 (3H, s), 2.80 (2H, t, J=7.5Hz), 3.23-3.36 (2H, a), 3.36 (3H, s), 3.80 (3H, s) , 3.84-4.03 (2H, m) , 4.26 (2H, t, J=7.5Hz), 6.57-6.68 (2K, m) , 6.83- 7.15 (5H, m) , 7.45 (IH, t, J=7Hz) , 8.21 (IH, d, J=7Hz), 8.40 (IH, d, J=7Kz) 21) 4-[2-(3-Aaino-l-aethylprop-l-yl)oxybenzoyl]aaino-3- aethoxy-N-(2-benzyloxy-4-aethyl)phenyl-N- aethylbenzaaide NMR (CDC1 3 , δ) : 1.41 (3H, d, J=7.5Hz), 1.70-1.83 (IH, a), 1.96-2.10 (IH, a), 2.26 (3H, s) , 2.80- 2.89 (2H, a), 3.37 (3H, s) , 3.62 (3H, ε), 4.82 (IH, a), 4.89 (IH, d, J=14Hz), 5.07 (IH, d, J=14Hz), 6.63-6.72 (2H, a), 7.86 (IH, d, J=7Hz) , 6.98 (IH, d, J=7Hz), 7.02-7.11 (3H, m) , 7.28- 7.49 (6K, a), 8.22 (IH, d, J=7Hz) , 8.37 (IH, d, J=7Hz) 22) 4-[2- (4-Aminobut-l-yl)oxybenzoyl]amino-3-methoxy-N- methyl-N-[4-methyl-2-[5-(4-methylpiperazin-l- yl)carbonylpent-1-yl]oxy]phenylbenzamide NMR (CDCI3, δ) : 1.46-2.03 (10H, m) , 2.24 (3H, s) , 2.28 (3H, ε), 2.31-2.40 (6H, m) , 2.73 (2H, t, J=7.5Kz), 3.31 (3H, ε) , 3.44-3.50 (2H, m) , 3.59- 3.65 (2H, a), 3.77 (3H, s) , 3.83-4.00 (2H, a), 4.20 (2H, t, J=7.5Hz), 6.58 (IH, d, J=7Hz) , 7.61 (IH, ε), 6.85 (IH, d, J=7Hz) , 6.90 (IH, d, J=7Hz), 6.87-7.10 (3H, a), 7.45 (IH, t, J=7Hz) , 8.21 (IH, d, J=7Hz), 8.40 (IK, d, J=7Hz) 23) 4-[2- (3-Aainoprop-l-yl)oxy-3-aethylbenzoyl]aaino-3- aethoxy-N-aethyl-N-[2-[5- (4-aεthylpiperazin-l- yl)carbonylpent-1-yl]oxy-4-aethylphenyl]benzaaide NMR (CDCI3, δ) : 1.49-1.91 (6H, a), 1.96-2.07 (2H, a), 2.27 (3H, s), 2.30 (3H, s) , 2.35 (3H, s) , 2.32-2.40 (6H, a), 2.95 (2H, t, J=5Hz) , 3.32 (3K, s), 3.46-3.53 (2H, a), 3.60 ^ 3.67 (2H, a), 3.81 (3H, s), 3.85-4.02 (4H, a), 6.56-6.66 (2H, a), 6.82-7.18 (4H, a), 7.33 (IH, d, J=8Hz) , 7.80 (IH, d, J=7Hz), 8.36 (IK, d, J=7Hz) 24) 4-[2-(3-Aminoprop-l-yl)oxy-4-methylbenzoyl]amino-3- methoxy-N-methyl-N-[2-[5-(4-methylpiperazin-l- ylcarbonyl)pent-1-yloxy]-4-methylphenyl]benzamide NMR (CDC1 3 , δ) : 1.46-1.90 (6H, m) , 2.13-2.25 (2H, m), 2.26 (3H, s), 2.28 (3K, s), 2.30-2.58 (6H, a), 2.37 (3H, s), 2.99 (2K, t, J=5Hz) , 3.30 (3H, ε), 3.49 (3H, ε), 3.49 (2H, t, J=5Hz) , 3.61 (2H, t, J=5Hz), 3.79 (3H, s) , 3.83-3.92 (2H, a), 4.28 (2H, t, J=5Hz), 6.56-6.65 (2H, a), 6.80-6.93 (4H, a), 7.00 (IH, ε), 8.02 (IH, d, J=8Hz), 8.39 (IH, d, J=8Hz) 25) - [2-(3-Aminoprop-l-yl)oxy-5-methylbenzoyl]amino-3- methoxy-N-methyl-N-[2-[5-(4-methylpiperazin-l- yl)carbonylpεnt-1-yl]oxy-4-methylphenyl]benzamide NMR (CDCI3, δ) : 1.49-1.90 (6H, m) , 1.98-2.20 (4H, a), 2.28 (3H, ε), 2.29 (3H, s) , 2.31 (3H, s), 2.31-2.42 (4H, a), 2.95 (2H, t, J=5Hz) , 3.31 (3H, s), 3.50 (2K, t, J=4Hz), 3.62 (2H, t, J=4Hz), 3.79 (3H, s) , 3.80-4.00 (2H, a), 4.25 (2K, t, J=5Hz), 6.57-6.68 (2K, a), 6.82-7.04 (4H, a), 7.24 (IH, d, J=8Hz) , 7.95 (IH, s) , 8.39 (IK, d, J=8Hz) 26) 4-[2-(3-Aminoprop-l-yl)oxy-4-chlorobenzoyl]amino-3- methoxy-N-methyl-N-[2-[5-(4-methylpiperazin-l- yl)carbonylpent-l-yl]oxy-4-methylphenyl]benzamide NMR (CDCI3, δ) : 1.48-1.60 (2H, m) , 1.62-1.90 (2H, ) , 2.10 (2H, t, J=6Hz), 2.27 (3H, s), 2.29 (3H, s), 2.30-2.41 (4H, a), 2.93 (2H, t, J=5Hz) , 3.31 (3H, s), 3.45-3.53 (2H, a), 3.58-3.66 (2H, a), 3.78 (3H, s), 3.82-4.01 (2H, a), 4.29 (2H, t, J=5Hz), 6.55-6.68 (2H, a), 6.80-6.91 (2H, a), 6.99-7.10 (4H, a), 8.13 (IK, d, J=8Hz) , 8.36 (IH, d, J=8Hz) 27) 4-[2- (3-Aminoprop-l-yl)oxy-4-methoxybenzoyl]amino-3- methoxy-N-methyl-N-[2-[5-(4-mεthylpiperazin-l- yl)carbonylpent-l-ylloxy-4-methylphenyl]benzamide NMR (CDC1 3 , δ) : 1.47-1.89 (6H, a), 2.04-2.15 (2H, a), 2.28 (3H, s), 2.30 (3H, s) , 2.31-2.42 (6H, a), 2.93 (2H, t, J=5Hz), 3.31 (3H, s) , 3.44-3.52 (2K, a), 3.57-3.65 (2H, a), 3.79 (3H, s) , 3.83 (3H, s), 3.83-4.00 (2H, m) , 4.26 (2H, t, J=5Hz) , 7.50-7.68 (4H, m) , 6.82-6.95 (2K, ) , 7.03 (3H, s), 8.16 (IH, d, J=8Hz), 8.38 (IH, d, J=8Hz) Example 8 A mixture of 4-(2-benzyloxybenzoyl)amino-N-mεthyl-N- [2- (5-carboxypent-l-yloxy)phenyl]benzaaide (1.76 g) , N- ethyl-N'- (3-dimethylaminopropyl)carbodiimide hydrochloride (714 mg) , N-methylpipεrazine (311 mg) and 1-hydroxy- benzotriazol (504 mg) in N,N-dimethylformamide (20 ml) was stirred at ambient temperature for 2 hours and the mixture was diluted with ethyl acetate (40 ml) . The solution was washed εuccessively with saturated aqueous sodium hydrogen carbonate solution (40 ml), water { ^o nl) and brine (40 ml), and dried over magnesium sulfate. The solvent was evaporated to give 4-(2-benzyloxybenzoyl)amino-N-mεthyl-N- [2-[5- (4-methylpiperazin-l-yl)carbonylpεnt-1- yloxy]phenyl]benzamide (1.98 g) as a colorlesε oil. NMR (CDCI3, δ) : 1.46-1.58 (2H, m) , 1.64-1.88 (4H, a), 2.30 (3H, s), 2.32-2.41 (6H, m) , 3.32 (3H, ε), 3.49 (2H, a),. 3.62 (2H, a), 3.81-4.00 (2H, br), 5.20 (2K, s) , 6.73-6.82 (2H, m) , 6.94-7.00 (3H, a), 7.08-7.20 (5H, a), 7.40-7.53 (6H, a), 8.28 (IH, d, J=7Hz) Example 9 The following compound waε obtained by uεing 4-[2- (carboxymethoxy)benzoyl]amino-N-methyl-N-[2-[5-(4- methylpiperazin-1-yl)carbonylpent-1-yloxy]phenyl]benzamide aε a starting compound according to a similar manner to that of Example 8. 4-[2-[ (4-Methylpiperazin-l-yl)carbonylmethoxy]- benzoyl]amino-N-methyl-N-[2-[5-(4-methylpipεrazin-l- yl)carbonylpent-1-yloxy]phenyl]benzamide MASS : 699 (M+l) Example 10 A solution of 4-(2-benzyloxybεnzoyl)amino-N-methyl-N- [2-[5-(4-methylpiperazin-l-yl)carbonylpent-1- yloxy]phenyl]benzamide (1.90 g) in methanol (30 ml) was hydrogenated under atmospheric presser in the presence of palladium hydroxide (400 mg) for 6 hours and the catalyst was rε ovεd by filtration. The filtrate was evaporated to give 4-(2-hydroxybenzoyl)amino-N-methyl-N-[2-[5-(4- methylpiperazin-1-yl)carbonylpent-1-yloxy]phenyl]benzamide (1.60 g) as a colorless amorphous. NMR (CDC1 3 , δ) : 1.51 (2H, a), 1.66 (2H, a), 1.79 (2H, m) , 2.30 (2H, m) , 2.63-(3K, s) , 2.82-2.95 (4H, a), 3.33 (3H, s) , 3.72 (2H, a), 3.86 (2H, a), 3.99 (2K, a), 6.78-6.93 (3H, a), 7.05 (2H, a), 7.17 (IH, t, J=7Hz), 7.27 (2H, d, J=8.5Hz), 7.40 (IH, t, J=7Hz), 7.53 (2H, d, J=8.5Hz), 7.91 (IH, a), 9.21 (IH, br) Example 11 The following compounds were obtained according to a similar mannεr to that of Example 10. 4-(2-Hydroxybenzoyl)amino-N-methyl-N-[2-[3-(4- methylpiperazin-1-yl)carbonylaminoprop-1- yloxy]phεnyl]bεnzamide NMR (CDCI3, δ) : 2.00 (2H, m) , 2.71 (3H, s) , 2.90- 3 . 09 (4K, a) , 3 .33 (3H, s) , 3.50-3 . 80 (6H, a) , 3. 97 (2K, a) , 6.76-7 . 03 (5H, m) , 7 .11-7.22 (2H, m) , 7 .29-7 .44 (3H, m) , 7 .45-7 .54 (2H, m) , 7 . 88 ( IH, m) 2) 4- (2-Hydroxybenzoyl) amino-3-methoxy-N-methyl-N-[2-[5- (4-methylpipεrazin-l-ylcarbonyl)pεnt-l-yloxy]-4- methylphenyl]benzamide NMR (CDC1 3 , δ) : 1.46-1.62 (2H, m) , 1.65-1.90 (4H, m), 2.29 (3H, s), 2.30-2.43 (2H, m) , 2.82 (3H, s), 2.88-3.30 (4H, m) , 3.31 (3H, s) , 3.48 (3H, ε), 3.79 (3H, s), 3.77-4.07 (6H, m) , 6.58-6.69 (2H, m), 6.84-7.08 (5H, m) , 7.43 (IH, dd, J=9, 9Hz), 7.52 (IH, d, J=9Hz) , 8.20 (IH, d, J=9Hz) , 8.82 (IK, br s) 3) 4- (2-Hydroxybenzoyl) amino-3-methoxy-N-methyl-N- [2- [5- (4-methylpiperazin-l-yl) carbonylpent-1-yloxy]phenyl]- benzamide NMR (CDCI3, δ) : 1.47-1.63 (2H, m) , 1.64-1.90 (4H, a), 2.38 (2H, t, J=7Hz) , 2.78 (3H, s) , 2.90-3.31 (4H, a), 3.33 (3H, s) , 3.77 (3H, s) , 3.80-4.07 (6H, a), 6.77-7.11 (7H, a), 7.12-7.23 (IH, a), 7.37-7.58 (2H, a), 8.21 (IH, d, J=9Hz) , 8.79 (IH, s) 4) 2-Chloro-4-[2- (hydroxy)benzoyl]aaino-N-aethyl-N- [2- [5- (4-aethylpiperazinrl-yl) carbonylpent-1-yloxy] - phenyl]benzaaide NMR (CDCI3, δ) : 1.38-1.98 (6H, a), 2.21-2.46 (2H, a), 2.73 (3H, br s), 2.92-3.25. (4H, a), 3.36 (3H, s), 3.70-4.20 (6H, a), 6.67-6.82 (2H, a), 6.82-7.08 (4H, a), 7.08-7.20 (2H, a), 7.21-7.50 (2H, a), 7.70 (IH, br s), 7.92 (IH, br d, J=8Hz), 9.48 (IH, s) 5) 4-(3-Hydroxybenzoyl)amino-3-methoxy-N-methyl-N-[4- methyl-2-[5-(4-dimethylaminopiperidin-l- yl)carbonylpent-1-yloxy]phenyl]benzamide NMR (CDC1 3 , δ) : 1.34-1.58 (4H, a), 1.64-1.97 (6H, m), 2.28 (3H, ε), 2.32 (6H, ε), 2.33-2.38 (3H, a), 2.51-2.61 (IH, m) , 2.97-3.06 (IH, m) , 3.34 (3H, ε), 3.78-3.81 (3H, br s), 3.85-3.97 (3H, m) , 4.60-4.69 (IH, a), 6.58-6.65 (2H, a), 6.84- 7.06 (4K, a), 7.38-7.60 (3H, a), 8.17-8.23 (IH, ) ESI-MASS (m/z) : 631 (M+H) 6) 4- (2-Kydroxybenzoyl) amino-N- [2- (5-ethoxycarbonylpent- 1-yl) cxy-4-methyl] phenyl-N-methylbenzamide NMR (CDCI3 , δ) : 1 .23 (3H, t, J=7.5Hz) , 1 .41-1.53 (2H, m) , 1 . 62-1 .84 (4H, m) , 2.27 (3H, ε) , 2.32 (2H, t, J=7.5Hz) , 3.31 (3H, s) , 3.78-3.97 (2H, a) , 4 .13 (2H, q, J=7.5Kz) , 6.56-6. 61 (2H, a) , 6.84-6.91 (2H, a) , 7.02 (IH, d, J=7Hz) , 7.28- 7.45 (4H, m) , 7 . 62 (IH, d, J=7Hz) , 8.47 (IH, s) 4-(2-Hydroxybenzoyl)amino-N-methyl-N-[2-[3-(4- methylpiperazin-1-yl)carbonylprop-l-yl]oxy]- phenylbenzamide NMR (CDCI3, δ) : 2.00 (2H, m) , 2.71 (3H, s), 2.90- 3.09 (4K, m), 3.33 (3H, s) , 3.50-3.80 (6H, a), 3.97 (2H, a), 6.76-7.03 (5H, a), 7.11-7.22 (2H, a), 7.29-7.44 (3H, a), 7.45-7.54 (2H, a), 7.88 (IH, m) 8) 4-(2-Hydroxy)benzoylaminc-3-methoxy-N-methyl-N-[2-[4- (4-methylpiperazin-l-yl)carbonyl]phenyleth-1- yl]phεnylbenzamide MASS (m/z) : 607 (M+l) 9) 4- (2-Kydroxy-3-methylbenzoyl)amino-3-methoxy-N- methyl-N-[2-[5- (4-methylpiperazin-l-yl)carbonylpent- l-yl]oxy-4-methylphenyl]bεnzamide NMR (CDC1 3 , δ) : 1.50-1.90 (6H, m) , 2.27 (6H, s), 2.28 (3H, s), 2.33-2.40 (4H, a), 2.70-2.78 (2H, a), 3.30 (3H, s), 3.80 (3H, s) , 3.85-4.10 (6H, a), 6.59-6.65 (2H, a), 6.77-6.97 (6H, a), 8.19 (IH, d, J=8Kz), 8.70 (IK, br s) 10) 4- (2-Hydroxy-4-methylbεnzoyl)amino-3-methoxy-N- methyl-N-[2-[5- (4-methylpiperazin-l-yl)carbonylpent- l-yl]oxy-4-methylphenyl]benzamide NMR (CDCI3, δ) : 1.49-1.91 (6H, a), 2.24 (3H, s) , 2.29 (3H, s), 2.32 (3H, s) , 2.30-2.42 (6H, a), 3.32 (3H, s), 3.49 (2H, t, J=5Kz) , 3.63 (2H, t, J=5Hz), 3.80 (3H, s) , 3.88-4.01 (2H, m) , 6.68- 6.65 (2H, a), 6.80 (IH, s) , 6.84 (IH, d, J=8Hz), 6.93 (IH, d, J=7Hz), 7.03 (IH, s) , 7.37 (IH, d, J=7Hz), 8.19 (IH, d, J=8Hz), 8.71 (IH, br) 11) 4-(2-Hydroxy-4-methylbenzoyl)amino-3-methoxy-N- mεthyl-N-[2-[5-(4-methylpiperazin-l-yl)carbonylpent- 1-yl]oxy-4-methylphenyl]benzamide NMR (CDCI3, δ) : 1.50-1.91 (10H, m) , 2.28 (3H, s) , 2.34 (3H, s) , 2.35 (3H, s) , 2.30-2.41 (6H, a), 2.80 (2H, br), 3.31 (3H, s), 3.80 (3H, s) , 3.81- 4.09 (4H, a), 6.60-6.68 (2H, a), 6.84-7.02 (4H, a), 7.20-7.30 (2H, a), 8.20 (IH, br) , 8.37 (IH, br) 12) 4- (2-Hydroxy-4-chlorobenzoyl)amino-3-methoxy-N- methyl-N-[2-[5- (4-methylpipεrazin-l-yl)carbonylpεnt- l-yl]oxy-4-methylphenyl]benzamide NMR (CDCI3, δ) : 1.46-1.89 (6H, m) , 2.23-2.45 (6H, a), 2.27 (3H, s) , 2.32 (3H, s) , 3.30 (3H, s) , 3 .44-3. 68 (4H, a) , 3.80 (3H, s) , 3.80-3.99 (2H, a) , 6.53-6. 65 (2H, a) , 6.72-7 . 03 (5H, a) , 7.41 (IH, d, J=8Hz) , 8 . 12 (IH, d, J=8Hz) , 8 .74 (IH, br) 13) 4-(2-Kydroxy-4-methoxybenzoyl)amino-3-methoxy-N- methyl-N-[2-[5-(4-methylpiperazin-l-ylcarbonyl)pent- l-yl]cxy-4-methylphenyl]benzamide NMR (CDC1 3 , δ) : 1.48-1.60 (2H, m) , 1.63-1.84 (4H, a), 2.28 (3H, s) , 2.37 (2K, t, J=5Hz), 2.25-2.40 (6H, a), 2.79 (3H, s) , 3.30 (3H, s) , 3.79 (3H, s), 3.82 (3H, s), 3.90-4.01 (2H, a), 6.44-6.50 (2H, ) , 6.60-6.66 (2H, m) , 6.88-6.97 (3H, a), 7.41 (IH, d, J=8Kz), 8.18 (IH, d, J=8Hz) , 8.40 (IH, br) 14) 4- (2-Hydroxybenzoyl)aaino-3-aethoxy-N-aethyl-N-[2-[5- (4-dimethylaminopiperidin-l-yl)carbonylpent-1- yloxy]phenyl]benzamide NMR (CDCI3, δ) : 1.22-1.45 (2H, a), 1.45-1.58 (2H, a), 1.62-1.78 (2H, m) , 1.80-1.96 (4H, a), 2.30 (6H, s), 2.30-2.40 (3H, a), 2.50-2.62 (IH, a), 2.97-2.37 (IH, a), 3.37 (3H, s) , 3.78 (3H, s) , 3.82-4.02 (4H, a), 4.57-4.68 (IH, m) , 6.77-7.02 (8H, m), 7.10-7.20 (IH, m) , 7.37-7.45 (IH, m) , 7.46-7.62 (IH, m) , 8.20 (IH, br) 15) 4- (2-Hydroxybenzoyl)amino-3-chloro-N-methyl-N-[2-[5- (4-dimethylaminopiperidin-l-yl)carbonylpent-1-yloxy] 4-methylphenyl]benzamide NMR (CDCI3, δ) : 1.30-2.08 (10H, a), 2.20-2.60 (13H, a), 2.89-3.05 (IH, a), 3.30 (3H, s), 3.82-4.02 (4H, a), 4.62-4.79 (IH, a), 6.62 (2H, s), 6.73- 7.02 (4H, a), 7.28-7.57 (3H, a), 7.99 (IH, d, J=7Hz), 8.42 (IH, d, J=7Hz) 16) 3-Ethoxy-4-(2-hydroxybenzoyl)aaino-N-aethyl-N-[2-[5- (4-aethylpiperazin-l-yl)carbonylpent-l-yloxy]-4- aethylphenyl]benzaaide NMR (CDC1 3 , δ) : 1.40 (3H, t, J=6Hz) , 1.47-1.57 (2H, a), 1.65-1.72 (2H, a), 1.78-1.88 (2H, m) , 2.27 (3H, s), 2.30 (3H, s), 2.31-2.42 (7H, a), 3.30 (3H, 5), 3.48-3.50 (2H, a), 3.52-3.65 (2H, a), 3.82-4.02 (4H, a), 6.58-6.61 (2H, a), 6.82-6.94 (3H, a), 6.98-7.02 (2H, a), 7.40-7.47 (2H, a), 8.20 (IH, d, J=7Hz), 8.83 (IH, s) 17) 3-Hydroxy-4-(2-hydroxybenzoyl)aaino-N-aethyl-N-[2-[5- (4-aethylpiperazin-l-yl)carbonylpent-1-yloxy]-4- aethylphenyl]benzamide NMR (CDCI3, δ) : 1.62 (2H, br) , 1.75 (2H, br) , 1.85 (2H, br), 2.27 (3H, s) , 2.30 (3H, s) , 2.42 (7H, br), 3.30 (3H, s) , 3.53 (2H, br) , 3.68 (3H, br) , 3.90 (IH, br), 6.52 (IH, s) , 6.63-6.73 (2H, m) , 6.87 (IH, t, J=7Hz), 6.97 (IH, d, J=7Hz) , 7.08 (IH, d, J=7Kz), 7.15 (IH, s), 7.38 (IH, t, J=7Hz), 7.58 (IH, d, J=7Hz), 7.98 (IH, br) , 9.02 (IH, br) 18) 2-(2-Hydroxybenzoyl)amino-N-methyl-N-[2-[5-(4- dimethylaminopipεridin-1-yl)carbonylpεnt-1-yloxy]-4- methylphenyl]-5-pyridinecarboxamide NMR (CDCI3, δ) : 1.32-2.15 (10H, a), 2.29-2.42 (12H, a), 2.47-2.62 (IH, m) , 2.95-3.09 (IH, m) , 3.32 (3H, s), 3.75-4.10 (4H, m) , 4.58-4.77 (2H, m) , 6.33-8.47 (15H, m) 19) 4-(4-Hydroxybenzoyl)amino-3-methoxy-N-methyl-N-[2-[5- (4-dimεthylaminopipεridin-l-yl)carbonylpent-1-yloxy]- 4-methylphenyl]benzamidε NMR (CDCI3, δ) : 1.38-1.55 (4H, a), 1.62-1.72 (2H, 5 - 134 - a), 1.72-1.83 (2H, m) , 1.83-1.97 (2H, a), 2.27 (3H, s), 2.32-2.37 (8H, a), 2.43-2.60 (2H, a), 2.93-3.05 (IH, m) , 3.31 (3H, s), 3.70 (3H, s), 3.78-3.95 (4H, m) , 4.60-4.70 (IH, ) , 6.57-6.60 (2H, m), 6.80-6.97 (5H, a), 7.67 (2H, d, J=7Hz), 8.22 (IH, d, J=7Hz), 8.40 (IH, s) 20) 4-(4-Hydroxybenzoyl)aaino-3-aethoxy-N-aethyl-N-[2-[5- (4-methylpiperazin-l-yl)carbonylpent-l-yloxy]-4- methylphenyl]benzamide NMR (CDC1 3 , δ) : 1.47-1.58 (2K, a), 1.67-1.75 (2H, a), 1.75-1.87 (2H, m) , 2.27 (3H, s) , 2.32 (3H, s), 2.38-2.48 (7H, a), 3.35 (3H, s) , 3.48-3.53 (2H, a), 3.60-3.70 (2H, a), 3.70 (3H, s), 3.80- 3.90 (IH, a), 3.90-4.00 (IH, a), 3.58-3.60 (2H, a), 6.82-6.97 (5H, a), 7.68 (2H, d, J=7Hz) , 8.24 (IH, d, J=7Hz), 8.40 (IH, s) Example 12 A εolution of 4-(2-hydroxybenzoyl)aaino-N-aethyl-N- [2-[5-(4-aethylpiperazin-l-yl)carbonylpent-1- yloxy]phenyl]benzamide (400 mg) in N,N-dimethylformamide (15 ml) waε added potassium carbonate (99 mg) and N-(3- bromopropyUphthalimide (192 mg) and the mixture was stirred at 60°C for 4 hours. The mixture was poured into water (30 ml) and the aqueous solution was extracted with ethyl acetate (20 ml x 2) . The organic phase was washed with water (20 ml) and brine (20 al), and dried over aagnesiua sulfate. The solvent was evaporated to give 4- [2-[3-(phthaliaido)prop-l-yl]oxy]benzoylaaino-N-aethyl-N- [2-[5-(4-aethylpiperazin-l-yl)carbonylpent-1- yloxy]phenyl]benzaaide (484 ag) as a colorlesε amorphous. NMR (CDCI3, δ) : 1.56 (2H, m) , 1.63-1.76 (4H, a), 1.86 (2H, a), 2.30 (3H, s), 2.32-2.41 (6H, a), 3.35 (3H, s) , 3.50 (2K, a), 3.63 (2H, a), 3.83- 3.97 (4H, a), 4.20 (2K, t, J=7.5Hz), 6.73-6.81 (2H, a), 6.92 (IH, d, J=7Hz) , 7.00-7.14 (3H, m) , 7.32 (2H, d, J=8.5Hz), 7.42 (IH, m) , 7.50 (2H, d, J=8.5Hz), 7.65-7.74 (4H, m) , 8.08 (IH, d, J=7Hz), 9.69 (IH, s) Exampl 13 The following compounds were obtained according to a similar manner to that of Example 12. 1) 4- [2- (Ξthoxycarbonylmethoxy)benzoyl]amino-N-methyl-N- [2- [5- (4-methylpiperazin-l-yl) carbonylpent-1- yloxy]phenyl]benzamide NMR (CDC1 3 , δ) : 1.31 (3K, t, J=7.5Hz), 1.62 (2H, a), 1.71 (2H, a), 1.83 (2H, a), 2.29 (3H, s) , 2.33-2.41 (6H, a), 3.35 (3H, ε), 3.49 (2H, a), 3.62 (2H, m), 3.93 (2H, m) , 4.33 (2H, q, J=7.5Hz), 4.76 (2H, s) , 6.72-6.82 (2H, m) , 6.87 (IH, d, J=7Hz), 7.00 (IH, d, J=7Kz) , 7.07-7.18 (2H, m), 7.33 (2H, d, J=8.5Hz), 7.46 (IH, t, J=7Hz), 7.71 (2K, d, J=8.5Hz), 8.26 (IK, d, J=7Hz) 2) 4- [2- (3-Pipεridinoprop-l-yloxy)benzoyl] amino-N- methyl-N-[2-[5- (4-methylpiperazin-l-yl)carbonylpent- 1-yloxy]phenyl]benzamide NMR (CDCI3, δ) : 1.45 (2H, m) , 1.50-1.60 (4H, a), 1.71 (2H, m) , 1.85 (2H, m) , 2.14 (2H, m) , 2.28 (3H, s), 2.30-2.41 (10K, a), 2.49 (2H, t, J=7.5Hz), 3.34 (3H, s) , 3.49 (2H, a), 3.63 (2H, a), 3.94 (2H, a), 4.23 (2H, t, J=7.5Hz), 6.73- 6.82 (2H, m) , 6.96-7.02 (2K, m) , 7.04-7.15 (2H, a), 7.32 (2K, d, J=8.5Hz), 7.43-7.50 (3K, a), 8.22 (IH, d, J=7Hz) 5 - 136 - 3) 4-[2-[2-(Dimethylamino)eth-1-yloxy]benzoyl]amino-N- methyl-N-[2-[5-(4-methylpiperazin-l-yl)carbonylpent- 1-yloxy]phenyl]benzamide NMR (CDC1 3 , δ) : 1.56 (2H, a), 1.70 (2H, m) , 1.85 (2H, m), 2.23 (6H, s), 2.30 (3H, s), 2.33-2.41 (6H, a), 2.78 (2H, t, J=7.5Hz), 3.35 (3H, s) , 3.50 (2H, a), 3.64 (2H, a), 3.93 (2H, a), 4.22 (2H, t, J=7.5Hz), 6.74-6.81 (2H, a), 6.95-7.01 (2H, a), 7.06-7.15 (2H, a), 7.30 (2H, d, ^ J=8.5Hz), 7.43 (IH, a), 7.56 (2H, d, J=8.5Hz), 8.21 (IH, d, J=7Hz) 4) 4-[2-[3-(Phthaliaido)prop-1-yl]oxy]benzoylaaino-N- aethyl-N-[2-[3-(4-aethylpiperazin-l-yl)- carbonylaminoprop-1-yloxy]phenyl]benzamide NMR (CDCI3, δ) : 2.01 (2H, m) , 2.25 (3H, s) , 2.25-2.38 (6H, a), 3.33-3.45 (6H, a), 3.35 (3H, s), 3.87-4.00 (4H, a), 4.21 (2H, t, J=7.5Hz), 6.78-7.00 (3H, a), 7.06-7.20 (3H, a), 7.33-7.56 (4H, a), 7.65-7.75 (4H, a), 7.86 (IH, a), 8.10 (IH, d, J=7Hz), 9.73 (IH, br) 5) 4-[2-[3-(Phthaliaido)prop-l-yl]benzoylamino]-3- methoxy-N-methyl-N-[2-[5-(4-methylpiperazin-l- ylcarbonyl)pent-l-yloxy]-4-methylphenyl]benzamide NMR (CDCI3, δ) : 1.46-1.62 (2H, a), 1.63-1.93 (4H, a), 2.10-2.46 (14H, a), 3.33 (3H, s) , 3.40-3.53 (2H, m), 3.57-3.68 (2H, m) , 3.78 (3H, s) , 3.79- 4.04 (4H, m) , 4.26 (2H, t, J=7Hz) , 6.54-6.68 (2H, m), 6.74-7.11 (5H, a), 7.37-7.48 (IH, a), 7.52-7.63 (3H, m) , 7.66-7.77 (IH, m) , 7.80-7.90 (IH, m) , 8.06-8.23 (2H, a) 6) 3-Methoxy-4-[2-[3-(phthaliaido)prop-1-yl]oxybenzoyl] • aaino-N-aethyl-N-[2-[5-(4-aethylpiperazin-l- 95 - 137 - yl) carbonylpent-1-yloxy]phenyl]benzamide NMR (CDC1 3 , δ) : 1.47-1.63 (2H, a), 1.63-1.93 (6H, a), 2.29 (3H, s), 2.29-2.44 (6H, a), 3.36 (3H, s), 3.44-3.53 (2H, a), 3.58-3.68 (2H, a), 3.76 (3H, s), 3.81-4.05 (4H, a), 4.27 (2H, t, J=7Hz) , 6.74-6.91 (3K, a), 6.92-7.20 (5H, m) , 7.38-7.48 (IK, m), 7.58 (3H, ε), 7.68-7.77 (IK, m) , 7.82- 7.90 (IH, m) , 8.09-8.16 (IH, m) , 8.20 (IH, d, J=9Kz) 7) 3-Methoxy-4-[2-[3- (phthalimido)prop-l-yl]oxybenzoyl]- amino-N-methyl-N- [2- [5- (4-dimethylaminopiperidin-l- yl) carbonylpent-l-yioxy]-4-methylphenyl]benzamide NMR (CDCI3, δ) : 1.32-2.00 (12H, a), 2.16-2.48 (12H, a), 2.57 (IH, a), 3.02 (IH, a), 3.33 (3H, ε), 3.78 (3H, s), 3.80-4.05 (5H, a), 4.27 (2H, t, J=7Hz), 4.64 (IH, m) , 6.56-6.70 (2H, m) , 6.78- 7.12 (5H, m) , 7.43 (IH, m) , 7.59 (2H, s), 7.66- 7.91 (2H, m), 8.05-8.24 (2H, m) 8) 4- [2-[ (3-tert-Butoxycarbonylaminoprop-l- yl) oxy]benzoyl]amino-3-methoxy-N-methyl-N- [2- (5- ethoxycarbonylpent-1-yloxy) -4-methylphenyl]benzamide NMR (CDCI3, δ) : 1.26 (3H, t, J=7Hz) , 1.34-1.92 (17H, m) , 2.23-2.40 (5H, m) , 3.20-3.40 (5H, m) , 3.78 (3H, s), 3.82-4.01 (2H, ) , 4.12 (2H, q, J=7Hz), 4.25 (2H, t, J=7Hz) , 4.78 (IH, ) , 6.52- 6.69 (2H, m), 6.79-7.15 (5K, m) , 7.40-7.52 (2H, m), 8.21 (IK, d, J=8Hz), 8.40 (IH, d, J=8Hz) 9) 2-Chlcro-4-[2-[3- (phthalimido)prop-1-yl]oxybenzoyl] - amino-N-methyl-N-[2-[5- (4-methylpiperazin-l- yl) carbonylpent-1-yloxy]phenyl]benzamide NMR (CDCI3, δ) : 1.51-1.67 (2H, m) , 1.68-1.82 (2H, m), 1.82-2.01 (2K, m) , 2.22-2.48 (11H, m) , 3.38 95 - 138 - (3H, s), 3.47-3.56 (2K, a), 3.58-3.69 (2H, a), 3.90 (2H, t, J=7Hz), 3.94-4.11 (2H, a), 4.21 (2H, t, J=7Hz), 6.69-6.82 (2H, a), 6.93 (IH, d, J=8Hz), 7.02-7.20 (4H, a), 7.30 (IK, a), 7.43 (IH, a), 7.68 (4H, s), 8.07 (IH, a), 9.62 (IH, s) 10) 4-[2-[ (3-tert-Butoxycarbonylaainoprop-l-yl)oxy]- benzoyl]aaino-3-methoxy-N-methyl-N-(2-methylphenyl)- benzamide NMR (CDC1 3 , δ) : 1.41 (9H, s) , 2.02-2.18 (2H, a), 2.21 (3H, ε), 3.21-3.34 (2H, a), 3.39 (3H, s), 3.75 (3H, s), 4.24 (2H, t, J=7Hz) , 4.74 (IH, a), 6.83-7.22 (9K, a), 7.44 (IK, a), 8.20 (IH, a), 8.42 (IH, d, J=8Hz) 11) 4-[3-[ (3-tert-Butoxycarbonylaainoprop-l-yl)oxy]~ benzoyl] amino-3-methoxy-N-methyl-N- [4-methyl-2- [5- (4- dimethylaminopiperidin-1-yl) carbonylpent-1- yloxy] phenyl] benzamide NMR (CDCI3, δ) : 1.32-1.45 (2H,.a), 1.43 (9H, s) , 1.49-1.58 (2H, a), 1.64-1.90 (6H, m) , 1.97-2.03 (2H, m) , 2.29 (3H, s) , 2.30 (6H, ε) , 2.33-2.39 (3H, a), 2.51-2.61 (IH, a), 2.97-3.07 (IH, a), 3.28-3.38 (2H, a), 3.33 (3H, s) , 3.79 (3H, s) , 3.86-3.97 (3H, a), 4.08 (2H, t, J=7Hz) , 4.59- 4.67 (IH, a), 4.70-4.78 (IH, a), 6.57-6.64 (2H, m), 6.84 (IH, d, J=8Hz) , 6.93 (IH, d, J=8Hz) , 7.02 (IK, s), 7.03-7.07 (IH, a), 7.33-7.40 (3H, a), 8.27 (IH, d, J=8Hz), 8.49 (IH, ε) ESI-MASS (a/z) : 788 (M+l) 12) 4-[2-[4- (Phthalimido)but-l-yl]oxybenzoyl]amino-N- methyl-N-[2-[5-(4-methylpiperazin-l-yl)carbonylpent- 1-yl]oxy]phenylbenzamide 1795 - 139 - NMR (CDCI3, δ) .-1.48-1.60 (2H, ) , 1.65-1.77 (4H, a), 1.80-2.06 (6H, a), 2.29 (3H, s) , 2.33-2.41 (6H, a), 3.38 (3K, s), 3.45-3.51 (2K, a), 3.60-3.67 (2H, m), 3.78 (2H, t, J=7.5Hz), 3.88-4.00 (2H, a), 4.23 (2H, d, J=7.5Hz), 6.73-6.42 (2H, a), 6.99 (2H, d, J=8Hz), 7.08-7.17 (2H, m) , 7.36 (2H, d, J=8Kz), 7.44-7.50 (3H, a), 7.68-7.77 (2H, a), 7.81-7.91 (2H, a), 8.22 (IH, d, J=7Hz) 13) 4-[2-[3-(Phthaliaido)prop-1-yl]oxybenzoyl]aaino-N-[2- (5-ethoxycarbonyylpent-l-yl)oxy-4-aethyl]phenyl]-N- methylbenzamide NMR {CDCI3, δ) : 1.24 (3H, t, J=7.5Hz), 1.45-1.57 (2H, m), 1.64-1.88 (4H, m) , 2.25 (3H, ε) , 2.28- 2.37 (4H, m), 3.31 (3H, s), 3.84-3.95 (4H, a), 4.10 (2H, q, J=7.5Hz), 4.20 (2H, t, J=7.5Hz), 6.52-6.62 (2H, m) , 6.88 (IH, d, J=7Hz) , 6.92 (IH, d, J=7Hz), 7.07 (IH, t, J=7Hz) , 7.31 (2H, d, J=8Hz), 7.39-7.50 (3H, ) , 7.62-7.64 (4H, m) , 8.10 (IH, d, J=7Hz), 9.68 (IK, ε) 14) 4-[2-[3- (Phthalimido)prop-1-yi]oxybenzoyl]amino-N- methyl-N-[2-[3-(4-methylpiperazin-l-yl)carbonylprop- 1-yl]oxy]phenylbenzamide MASS (m/z) : 718 (M+l) 15) 4-[2-[3-(Phthalimdo)prop-l-yl]oxybenzoyl]amino-N- methyl-N-[4-methyl-2-[4-(4-methylpiperazin-l- yl)carbonyl]phenylmethoxy]phenylbenzamide NMR (CDCI3, δ) : 2.25 (3H, ε) , 2.25-2.31 (2H, m) , 2.31 (3H, s), 2.36-2.51 (4H, a),.3.38 (3H, s) , 3.63-3.85 (4H, a), 3.91 (2H, t, J=7.5Hz), 4.20 (2H, t, J=7.5Hz), 4.98 (IH, d, J=14Hz) , 5.08 (IH, d, J=14Hz), 6.63-6.70 (2H, a), 6.90-7.00 (2H, a), 7.09 (IH, t, J=7Hz) , 7.32 (2H, d. J=8Hz), 7.40-7.77 (7K, a), 8.10 (IH, d, J=7Hz), 9.70 (IH, s) 16) 4-[2-(3-Hydroxyprop-l-yl)oxybenzoyl]amino-N-methyl-N- [2-[5-(4-methylpiperazin-l-yl)carbonylpent-1- yl]oxy]phenylbenzamide NMR (CDC1 3 , δ) : 1.43-1.56 (2K, a), 1.60-1.86 (4H, m), 2.11-2.23 (2H, a), 2.14 (3H, s), 2.37-2.90 (6H, a), 3.33 (3H, s) , 3.40-3.47 (2H, a), 3.51- 3.59 (2H, a), 3.86 (2H, t, J=7.5Hz), 3.86-4.00 (2H, m) , 4.32 (2H, t, J=7.5Hz), 6.78-6.85 (2H, a), 6.99-7.19 (4H, a), 7.31 (2K, d, J=8Hz) , 7.41-7.53 (3H, a), 8.21 (IH, d, J=8Hz) 17) 4-[2-(3-Aainoprop-l-yl)oxy]benzoyl]amino-3-methoxy-N- methyl-N-[4-methyl-2-[5-(4-methylpiperazin-l-yl)- carbonylpent-1-yl]oxy]phenylbenzamide NMR (CDCI3, δ) : 1.43-1.54 (2H, m) , 1.60-1.70 (2H, m) , 1.74-1.85 (2H, m) , 2.10-2.21 (2H, m) , 2.26 (6H, sx2), 2.30-2.41 (6H, m) , 3.32 (3H, s) , 3.40-3.48 (2H, m) , 3.55-3.61 (2H, m) , 3.77 (3H, 8), 3.77-4.00 (4K, m), 4.31 (2H, t, J=7.5Hz), 6.57-6.63 (2H, a), 6.85-6.92 (2H, a), 7.00-7.11 (3H, a), 7.44 (IK, t, J=7Hz), 8.20 (IH, d, J=7Hz), 8.40 (IH, d, J=7Hz) 18) 3-Methoxy-4-[2-[3-(phthalimido)prop-1-yl]oxybenzoyl]- amino-N-methyl-N-[4-methyi-2-[4-(4-methylpiperazin-l- yl)carbonyl]phenylmethoxy]phenylbenzamide NMR (CDCI3, δ) : 2.19-2.32 (2H, a), 2.25 (3H, s), 2.33 (3H, s), 2.36-2.52 (4H, a), 3.33-3.50 (2H, a), 3.39 (3H, s), 3.67 (3H, s), 3.71-3.91 (4H, a), 4.28 (2H, t, J=7.5Hz), 4.95 (IH, d, J=14Hz) , 5.09 (IH, d, J=14Kz), 6.62-6.72 (2H, m) , 6.81 (IH, d, J=7Hz), 6.93-7.08 (4H, a), 7.34-7.47 (4H, ), 7.59 (IH, a), 7.68-7.75 (2K, a), 7.82- 7.88 (2H, a), 8.10-8.19 (2H, m) 19) 4- [2- (3-Ethoxycarbonylprop-l-yl) oxybenzoyl] amino-3- methoxy-N-methyl-N- [4-methyl-2- [5- (4-mεthylpipεrazin- l-yl)carbonylpent-l-yl] oxy] phenylbenzamide NMR (CDC1 3 , δ) : 1.22 (3H, t, J=7.5Hz), 1.45-1.57 (2H, a), 1.63 (3K, s) , 1.63-1.73 (2H, a), 1.76- 1.88 (2H, a), 2.20-2.32 (2H, a), 2.24 (3H, s), 2.27 (3H, s), 2.32-2.40 (6H, a), 2.50 (2H, t, J=7.5Hz), 3.31 (3H, s), 3.43-3.50 (2H, a), 3.58- 3.67 (2K, a), 3.78 (3K, s) , 3.83-4.00 (2H, a), 4.12 (2K, q, J=7.5Hz), 4.22 (2H, t, J=7.5Hz), 6.57 (IH, d, J=7Hz), 6.62 (IH, s) , 6.80-6.90 (2H, a), 6.97-7.11 (3H, a), 7.45 (IK, t, J=7Hz) , 8.21 (IH, d, J=7Hz), 8.40 (IH, d, J=7Hz) 20) 3-Methoxy-4-[2-[3-(phthaliaido)prop-l-yl]oxy]- phenylaethylaaino-N-aethyl-N- [4-aethyl-2- [5- (4- aethylpiperazin-1-yl) carbonylpent-l-yl]oxy]- phenylbεnzaaide NMR (CDC1 3 , δ) : 1.44-1.57 (2K, a), 1.62-1.72 (2H, a), 1.72-1.95 (4H, a), 2.18 (2H, t, J=7.5Hz), 2.25 (3H, s), 2.28 (3H, s) , 2.28-2.43 (4H, a), 3.28 (3H, s), 3.43-3.50 (2H, a), 3.57-3.65 (2H, a), 3.58 (3H, s), 3.80-3.96 (2H, a), 4.02 (2K, t, J=7.5Hz), 4.24 (2K, s) , 4.80 (IH, s) , 6.27 (IK, .d, J=7Hz), 6.60 (IH, d, J=7Hz) , 6.64 (IK, s), 6.80-6.95 (5K, a), 7.12-7.21 (2H, a), 7.64- 7.88 (4H, a) 21) 3-Methoxy-4-[2-[3- (phthaliaido)prop-1-yl]oxybenzoyl]- aaino-N-aεthyl-N-[2-[4- (4-methylpiperazin-l- yl)carbonyl]phenyleth-1-yl]phenylbenzaaide NMR (CDCI3, δ) : 2.20-2.50 (6H, a), 2.29 (3H, s) , 41795 - 142 - 2. 61-2 .94 ( 6H, a) , 3 .30 (3H, s) , 3 .37-3 . 68 (2H, m) , 3. 68 (3H, s) , 3. 68-3.92 (2H, m) , 4 .20-4 .30 (2H, m) , 6. 80 (IH, d, J=7Hz) , 6.90-6.98 (2H, m) , 7 .05 (IH, t, J=7Hz) , 7.10-7.49 (9H, m) , 7.53- 7 .89 (4H, m) , 8 .12 (IH, d, J=7Hz) , 8 .20 (IH, d, J=7Hz) 22) 3-Methoxy-4-[2-[3-(phthalimido)prop-1-yl]oxybenzoyl]- amino-N-[2-[4-(4-dimethylaminopiperidin-l- yl)carbonyl]phenylmethoxy-4-methyl]phenyl-N- methylbenzamide MASS (m/z) : 824 (M+l) 23) 3-Methoxy-4-[2-[3-(phthalimido)prop-1-yl]oxybenzoyl]- amino-N-methyl-N-[2-[3-(4-methylpiperazin-l- yl)carbonylmethoxyprop-1-yl]oxy]phenylbenzamide NMR (CDC1 3 , δ) : 2.04-2.17 (2H, m) , 2.25 (3H, s) , 2.28-2.40 (6H, m) , 3.33 (3K, s), 3.38-3.46 (2K, m) , 3.54-3.62 (2H, m) , 3.66-3.76 (2H, m) , 3.74 (3H, s), 3.80-3.90 (2H, m) , 3.98-4.11 (4H, m) , 4.28 (2K, t, J=7.5Hz), 6.78-7.10 (7H, m) , 7.14 (IH, t, J=7Hz), 7.43 (IH, t, J=7Hz) , 7.55 (2H, s), 7.68-7.75 (IH, a), 7.81-7.90 (IH, a), 8.13 (IH, d, J=7Hz), 8.20 (IH, d, J=7Hz) 24) 3-Methoxy-4-[2-[3-(phthalimido)prop-1-yl]oxybenzoyl]- amino-N-[2-[ (E)-5-(4-dimethylaminopiperidin-l- yl)carbonyl-4-penten-l-yl]oxy-4-methyl]phenyl-N- methylbenzamide NMR (CDCI3, δ) : 1.27-1.47 (2H, m) , 1.83-2.02 (2H, m), 2.10-2.48 (6H, m) , 2.23 (3H, s) , 2.26 (6H, ε), 2.50-4.13 (8H, m), 3.32 (3H, s), 3.78 (3H, ε), 4.26 (2K, t, J=7.5Hz), 4.62 (2H, m) , 6.32 (IH, d, J=15Hz), 6.57-6.67 (2H, m) , 6.80-7.16 (5H, m), 7.44 (IH, t, J=7Hz) , 7.53-7.88 (5H, a). 7 . 57 (2H, s ) , 8 . 09-8 . 19 (2H, m) 25) 3-Methoxy-4-[2-(pyrid-3-yl)methoxybenzoyl]amino-N- methyl-N-[4-methyl-2-[5-(4-methyipiperazin-l- yl)carbonylpent-l-yl]oxy]phenylbenzamidε NMR (CDC1 3 , δ) : 1.44-1.57 (2H, m) , 1.63-1.72 (2H, a), 1.75-1.86 (2H, a), 2.27 (3H, s), 2.30 (3H, s), 2.32-2.40 [ 6E, a), 3.29 (3H, ε), 3.31 (3H, s), 3.45-3.51 (2H, a), 3.58-3.65 (2H, a), 3.80- 4.00 (2H, a), 5.30 (2H, s), 6.58 (IH, d, J=7Hz) , 6.61 (IH, ε), 6.83 (IH, d, J=7Hz), 6.88-6.92 (_H, a), 7.05 (IH, d, J=7Kz) , 7.14 (IH, t, J=7Kz), 7.29 (IH, m), 7.46 (IH, t, J=7Hz), 7.79 (IH, d, J=7Hz), 8.22 (IH, d, J=7Hz) , 8.37 (IH, d, J=7Hz), 8.62 (6H, d, J=7Hz), 8.73 (IH, s) 26) 3-Methoxy-4-[2-[4-(phthalimido)but-l-yl]oxybenzoyl]- amino-N-methyl-N-[4-methyl-2-[5-(4-methylpiperazin-l- yl)carbonylpent-1-yl]oxy]phenylbenzamide NMR (CDCI3, δ) : 1.46-1.59 (2H, a), 1.65-1.74 (2H, a), 1.78-2.03 (6K, a), 2.26 (3H, s) , 2.30 (3H, s), 2.32-2.41 ( 6ή' , a), 3.31 (3K, s) , 3.43-3.50 (2H, a), 3.60-3.65 (2H, a), 3.74 (2H, t, J=7.5Hz), 3.77 (3K, s) , 3.82-4.01 (2H, a), 4.22 (2K, t, J=7.5Hz), 6.58 (IK, d, J=7Hz) , 6.63 (IH, s), 6.85 (IH, d, J=7Hz), 6.90 (IK, d, J=7Hz) , 7.00 (IH, d, J=7Hz), 7.02 (IH, s), 7.08 (IH, t, J=7Hz), 7.45 (IH, t, J=7Hz) , 7.70-7.76 (2H, a), 7.80-7.87 (2H, a), 8.21 (IH, d, J=7Hz), 8.40 (IH, d, J=7Hz) 27) 4-[2- (3-Dimethylaminoprop-l-yl)oxybenzoyl]amino-3- methoxy-N-methyl-N-[2-[5-(4-methylpiperazin-l- yl)carbonylpent-l-yl]oxy-4-methyiphεnyl]benzamide NMR (CDCi 3 , δ) : 1.50-1.91 (6K, a), 2.07-2.18 (2H, a) , 2 .25 ( 6H, s) , 2 .28 (3H, ε ) , 2 .30 (3H, s) , 2 .32-2 .44 (2H, m) , 2 .48 (2H, t, J=5Hz) , 3 .32 (3H, ε ) , 3.49 (2H, t, J=5Hz) , 3.63 (2H, t, J=3Hz) , 3 .78 (3H, s) , 3.81-3 .92 (2H, a) , 4 .25 (2H, t, J=5Hz) , 6.54-6. 64 (2H, m) , 6. 80-6.91 (2H, m) , 6. 99-7 .11 (4H, m) , 7 .40-7 .48 (IH, m) 8 .18 (IH, d, J=7Hz) , 8 .38 (IH, d, J=7Hz) 28) 4-[2- (Ethoxycarbonylmethoxy)benzoyl]amino-3-methoxy- N-methyl-N-[2-[5-(4-methylpiperazin-l- yl)carbonylpent-l-yl]oxy-4-methylphenyl]benzamide NMR (CDC1 3 , δ) : 1.23 (3H, t, J=5Hz), 1.50-1.91 (6H, m) , 2.28 (3H, s) , 2.31 (3H, s) , 2.35-2.47 (6H, a), 3.33 (3H, s), 3.52 (2H, t, J=5Hz) , 3.67 (2H, t, J=5Hz), 3.76 (3H, s) , 3.84-4.02 (2H, a), 4.24 (2H, q, J=5Hz), 4.85 (2H, s) , 6.55-6.67 (2H, a), 6.81-7.19 (6H, a), 7.41-7.49 (IH, a), 8.20 (IH, d, J=8Hz), 8.34 (IH, d, J=7Hz) 29) 4-[2-[3-(Phthalimido-l-yl)prop-l-yloxy]-3- methylbenzoyl]amino-3-methoxy-N-methyl-N-[2-[5-(4- methylpiperazin-1-yl)carbonylpent-1-yloxy-4- methylphenyl]benzamide NMR (CDCI3, δ) :. 1.50-1.92 (6H, a), 2.14-2.44 (8H, a), 2.25 (3H, s), 2.28 (3H, s), 2.36 (3H, s), 3.33 (3H, s), 3.50 (2H, t, J=5Hz) , 3.58 (2H, t, J=5Hz), 3.63 (2H, t, J=5Hz) , 3.81 (3H, s) , 3.81- 4.03 (8H, a), 6.55-6.68 (2H, a), 6.82-7.38 (6H, a), 7.59-7.88 (5H, a), 8.32 (IH, d, J=8Hz) 30) 4-[2-[3-(Phthalimido-l-yl)prop-l-yl]oxy-4- methylbenzoyl]amino-3-methoxy-N-methyl-N-[2-[5-(4- methylpiperazin-1-yl)carbonylpent-1-yl]oxy-4- methylphenyl]benzamide NMR (CDCI3, δ) : 1.50-1.91 (8H, m) , 2.27 (3H, s) , 2.30 (3H, ε), 2.31-2.42 (6H, a), 2.38 (3H, s) , 3.32 (3H, s), 3.50 (2H, t, J=5Hz) , 3.63 (2H, t, J=5Hz), 3.78 (3H, s), 3.85-4.02 (6H, a), 4.28 (2H, t, J=5Hz), 6.58-6.67 (2H, a), 6.77 (IH, s) , 6.80-6.92 (4H, a), 7.00 (IH, s), 7.58 (4H, ε), 8.01 (IH, d, J=8Hz), 8.18 (IH, d, J=8Hz) 31) 4-[2-[3-(Phthalimido-l-yl)propyloxy]-5- methylbenzoyl]amino-3-mεthoxy-N-methyl-N-[2-[5-(4- methylpiperazin-1-yl)carbonylpent-l-yl]oxy-4- methylphenyl]benzamide NMR (CDC1 3 , δ) : 1.52-1.91 (10H, m) , 2.25 (3H, s) , 2.30 (3H, s), 2.31 (3H, s) , 2.31-2.45 (2H, a), 3.31 (3H, s), 3.50 (2K, t, J=4Hz) , 3.59 (2H, t, J=5Hz), 3.64 (2H, t, J=4Hz) , 3.78 (3H, s) , 3.85- 4.02 (4H, a), 4.24 (2H, t, J=5Kz) , 6.58 (2H, a), 6.81-6.92 (3H, a), 7.00 (IH, s) , 7.25 (IH, d, J=8Hz), 7.59 (3H, s) , 7.71-7.79 (IH, a), 7.82- 7.89 (IK, a), 7.92 (IH, s) , 8.20 (IH, d, J=8Hz) 32) 4-[2-[3-(Phthaliaido-l-yl)propyloxy]-4- chlorobenzoyl]aaino-3-aethoxy-N-aethyl-N-[2-[5-(4- methylpiperazin-1-yl)carbonylpent-l-yl]oxy-4- methylphenyl]benzamide NMR (CDCI3, δ) : 1.45-1.92 (6H, m) , 2.25 (3H, s) , 2.30 (3H, s), 2.29-2.44 (8H, a), 3.32 (3H, s) , 3.46-3.54 (2H, a), 3.61-3.68 (2H, a), 3.78 (3H, s) ,.3.80-4.01 (4H, a), 4.25 (2H, t, J=5Hz) , 6.56-6.77 (2H, a), 6.79-7.04 (7K, a), 7.44 (2H, s), 7.70-7.78 (IH, m) , 7.81-7.88 (IH, a), 8.06 (IK, d, J=8Kz) 33) 4-[2-[3-(Phthaliaido-l-yl)propyloxy]-4- aethoxybenzoyl] aaino-3-aethoxy-N-aethyl-N- [2- [5- (4- aethylpiperazin-1-yl) carbonylpεnt-l-yl]oxy-4- methylphenyl]benzamide NMR (CDC1 3 , δ) : 1.49-1.90 (6H, m) , 2.15-2.24 (2H, a), 2.28 (3H, s), 2.32 (3H, s), 2.30-2.42 (6H, a), 3.33 (3H, s) , 3.50 (2H, t, J=4Hz), 3.60 (2H, t, J=5Hz), 3.63 (2H, t, J=4Kz) , 3.79 (3H, s) , 3.85 (3H, s), 3.82-4.02 (6H, a), 4.24 (2H, t, J=5Hz), 6.57-6.68 (2H, a), 6.82 (IH, d, J=8Hz) , 6.89 (IH, d, J=8Hz), 7.00 (IK, s) , 7.57 (2H, s) , 7.71-7.76 (2H, a), 7.82-7.88 (2H, m) , 8.11 (IH, d, J=9Hz), 8.17 (IK, d, J=8Hz) 34) 4-[2-[3- (tert-Butoxycarbonylamino)prop-l- yl]oxybenzoyl]amino-3-methoxy-N-(2-benzyloxy-4- methylphenyl)-N-methylbenzamide NMR (CDCI3, δ) : 1.40 (9H, s), 2.10 (2H, t, J=5Hz) , 2.29 (3K, s), 3.28 (2K, σ, J=5Hz) , 3.39 (3H, s) , 3.62 (3H, s), 4.21 (2H, t, J=5Hz) , 4.90 (IH, d, J=13Hz), 5.08 (IH, d, J=13Hz) , 6.63-6.71 (3H, a), 6.87 (IH, d, J=7Kz) , 6.96-7.11 (6H, m) , 7.31-7.48 (6H, m) , 8.21 (IH, d, J=8Hz) , 8.38 (IH, d, J=8Kz) 35) 4-[2-[3- (tert-Butoxycarbonylamino)prop-l- yl]oxybenzoyl]amino-3-methoxy-N-[2-[4-(2-oxazolin-2- yl)phenylmethyl]oxy-4-methylphenyl]-N-methylbεnzamide NMR (CDCI3, δ) : 1.40 (9H, s) , 2.09-2.17 (2K, m) , 2.28 (3H, s), 3.27 (IH, q, J=5Hz) , 3.40 (3H, s) , 3.65 (3H, s), 4.05 (2H, t, J=10Hz) , 4.23 (2H, t, J=5Hz), 4.40 (2H, t, J=10Hz), 4.88 (IH, d, J=12Hz), 5.08 (IH, d, J=12Hz) , 6.62 (IH, s), 6.68 (IH, d), 6.97-7.11 (6H, m), .7.32 (IH, d, =8Hz), 7.41 (IH, d, J=8Hz), 7.92 (2H, d, J=8Hz), 8.21 (IH, d, J=8Hz) , 8.37 (IH, d, J=8Hz) 36) 3-Methoxy-4-[2-[3- (phthalimido)prop-1-yl]oxybenzoyl]- amino-N-methyl-N-[2-[5-(4-dimethylaminopiperidin-l- yl)carbonylpent-1-yloxy]phenyl]benzamide NMR (CDC1 3 , δ) : 1.22-1.47 (2H, m) , 1.47-1.80 (6H, a), 1.80-1.92 (4H, a), 2.29 (6H, s), 2.31-2.41 (3H, a), 2.50-2.63 (IH, a), 2.95-3.07 (IH, a), 3.36 (3H, S), 3.48 (IH, s), 3.49 (IH, s) , 3.75 (3H, s), 3.82-4.03 (4H, a), 4.22-4.30 (2H, a), 4.60-4.70 (IK, a), 6.78-6.90 (3H, a), 6.92-7.20 (4H, a), 7.40-7.50 (IH, a), 7.55-7.63 (3H, a), 7.70-7.80 (IH, a), 7.82-7.90 (IH, a), 8.10-8.22 (2H, a) 37) 3-Methyl-4-[2-[ [3-(phthaliaido)prop-1-yl]oxy]- benzoyl]aaino-N-aethyl-N-[2-[5-(4-methylpiperazin-l- yl)carbonylpent-l-yloxy]-4-methylphenyl]benzamide MASS (m/z) : 774 (M+K) 38) 4-[2-[ (3-tert-Butoxycarbonylaminoprop-l- yl)oxy]benzoyl]amino-3-chloro-N-methyl-N-[2-[5- (4- dimethylaminopiperidin-1-yl)carbonylpent-1-yloxy]-4- methylphεnyl]bεnzamidε NMR (CDCI3, δ) : 1.32-1.45 (2H, a), 1.41 (9H, s), 1.48-1.59 (2H, a), 1.62-1.91 (8H, a), 2.08-2.18 (2H, a), 2.27 (6H, s) , 2.28 (3H, s) , 2.30-2.40 (3H, a), 2.52-2.61 (IH, a), 2.97-3.07 (IH, a), 3.22-3.30 (2H, a), 3.30 (3H, s) , 3.83-4.00 (3H, a), 4.30 (2H, t, J=6Hz), 4.57-4.68 (IH, a), 6.60-6.63 (2H, a)., 6.87-6.90 (IH, a), 7.02-7.15 (3H, a), 7.46-7.57 (2H, a), 8.20-8.22 (IH, a), 8.40 (IH, d, J=7Hz) 39) 3-Ethoxy-4-[2-[ [3- (phthalimido)prop-1-yl]oxy]- benzoyl]aaino-N-aethyl-N-[2-[5-(4-aethylpiperazin-l- yl)carbonylpent-l-yloxy]-4-methylphεnyl]benzamide MASS (m/z) : 804 (M-rH) 40) 3-(3-tert-Butoxycarbonylaminoprop-l-yl)oxy-4-[2-[ (3- tert-butoxycarbonylaminoprop-1-yl)oxy]benzoyl]amino- N-methyl-N-[2-[5-(4-methylpiperazin-I- yl)carbonylpent-l-yloxy]-4-methylphenyl]benzamide NMR (CDC1 3 , δ) : 1.40 and 1.43 (total 18H, s), 1.49- 1.60 (2K, m), 1.62-1.98 (6H, m) , 2.00-2.10 (2H, m) , 2.27 (3H, s), 2.29 (3H, s) , 2.31-2.41 (6H, m) , 3.17-3.29 (4H, a), 3.30 (3H, s) , 3.45-3.50 (2K, a), 3.59-3.69 (2H, a), 3.84-4.05 (4H, a), 4.22-4.30 (2H, m) , 5.04 (2H, br) , 6.5 6.63 (2H, m) , 6.85 (IK, d, J=7Kz) , 6.93 (IH, d, J=7Hz) , 6.98-7.03 (2H, m) , 7.09 (IH, t, J=7Hz) , 7.43 (IH, t, J=7Hz), 8.14 (IH, d, J=7Hz), 8.36 (IH, d, J=7Hz) 41) 2-Amino-4-[2-[ (3-tert-butoxycarbonylaminoprop-l- yl)oxy]benzoyl]amino-N-methyl-N-[2-[5-(4- dimethylaminopiperidin-1-yl)carbonylpent-1-yloxy]-4- methylphenyl]benzamide NMR (CDCI3, δ) : 1.25-1.39 (2H, a), 1.42 and 1.46 (total 9H, s), 1.48-1.60 (2H, a), 1.62-1.93 (8H, a), 2.08-2.18 (2K, a), 2.27 and 2.28 (total 9H, s), 2.33-2.39 (3K, a), 2.50-2.60 (IH, a), 2.96- 3.05 (IH, a), 3.29 (3H, s), 3.31-3.40 (2H, a), 3.85-3.98 (3H, a), 4.19 (2K, t, J=6Hz) , 4.57- 4.67 (IH, ) , 6.57-6.59 (IK, m) , 6.63 (2H, s) , 6.78-6.89 (2H, a), 6.96 (IH, d, J=7Hz) , 7.09 (IH, t, J=6Hz), 7.15 (IH, s), 7.40-7.46 (IH, a), 8.17 (IH, d, J=6Hz) 42) 2-[2-[ (3-tert-Butoxycarbonylaainoprop-l- yl)oxy]benzoyl]aaino-N-aεthyl-N-[2-[5-(4- diaethylaainopiperidin-1-yl)carbonylpent-1-yloxy]-4- ethylphenyl]-5-pyridinecarboxaaide NMR (CDCI3, δ) : 1.30 (9H, s) , 1.35-1.93 (12H, a), 2.10-2.22 (2H, a), 2.28 (9K, s) , 2.30-2.40 (3H, m) , 2.50-2.62 (IH, m) , 2.95-3.08 (IH, m) , 3.33 (3H, s), 3.38-3.49 (2H, m), 3.82-3.98 (4H, m) , 4.29 (2K, t, J=6Hz), 4.57-4.67 (IH, m) , 6.60- 6.62 (2H, m) , 6.90 (IH, d, J=6Hz) , 6.99 (IH, d, J=7Hz), 7.09 (IH, t, J=7Hz), 7.44-7.55 (2H, m) , 8.13-8.21 (2H, a), 8.39 (IH, s) Example 14 To an ice bath cooled solution of 4-[2-[ (3-aainoprop- 1-yl)oxy]benzoyl]aaino-N-aethyl-N-[2-[5-(4- aethylpiperazin-1-yl)carbonylpent-1-yloxy]phenyl]benzaaide (200 ag) in dichloroaethane (10 al) werε addεd triεthylaainε (36.2 ag) and acεtic anhydride (36.5 ag) and the mixture was stirred at ambient tεmpεraturε for 4 hours. The reaction mixture was washed successively with water (10 ml), saturated aqueous sodium hydrogεn carbonate εolution (10 ml) and brine (10 ml), and dried over magneεium sulfate. The solvent was evaporated to give 4-[2-[ (3-acetylaminoprop-l-yl)oxy]benzoyl]amino-N-methyl- N-[2-[5- (4-mεthylpipεrazin-l-yl)carbonylpεnt-1- yloxy]phεnyl]bεnzamidε (201 mg) as a colorlεsε amorphous. NMR (CDC1 3 , δ) : 1.51 (2H, m) , 1.62-1.86 (4H, m) , 1.93 (3K, s), 2.11 (2H, ) , 2.29 (3H, s) , 2.30- 2.40 (6H, a), 3.35 (3H, s) , 3.40-3.50 (4H, m) , 3.59 (2H, a), 3.92 (2H, a), 4.18 (2H, t, J=7.5Hz), 6.28 (IH, a), 6.75-6.83 (2H, a), 6.94- 7.17 (4H, a), 7.31 (2H, d, J=8.5Hz), 7.40-7.49 (3H, a), 8.08 (IH, d, J=7Hz) , 9.18 (IH, s) Example 15 To a aixture of 4-[2-[ (3-aainoprop-l- yl)oxy]bεnzoyl]amino-N-mεthyl-N-[2-[5-(4-methylpiperazin- 1-yl)carbonylpent-1-yloxy]phenylJbεnzamide (220 mg) and 37% aqueouε formaldehyde (290 mg) in a mixture of methanol (10 ml) and acetic acid (0.2 ml) waε added sodium cyanoborohydride (44.8 mg) and the mixture was stirred at ambiεnt tεmperature for 4 hours. Thε reaction mixture was diluted with chloroform (20 ml) and the solution was washed successively with saturated aqueous sodium hydrogen carbonate solution (20 ml), water (10 ml) and brine (10 ml) . The organic phase was dried over magnesium sulfate and the solvent was evaporated to give 4-[2-[(3- dimethylaainoprop-1-yl)oxy]benzoyl]amino-N-methyl-N-[2-[5- (4-methylpiperazin-l-yl)carbonylpent-1- yloxy]phenyl]benzamidε (215 mg) as a colorlεss amorphous. NMR (CDC1 3 , δ) : 1.55 (2H, a), 1.73 (2H, a), 1.84 (2H, a), 2.11 (2H, a), 2.20 (6H, s), 2.30 (3H, s), 2.32-2.40 (6H, a), 2.46 (2H, t, J=7.5Hz), 3.35 (3H, 8), 3.49 (2H, a), 3.62 (2H, a), 4.24 (2H, t, J=7.5Hz), 6.74-6.83 (2H, a), 6.97-7.03 (2H, a), 7.07-7.16 (2H, a), 7.32 (2H, d, J=8.5Hz), 7.42-7.50 (3H, a), 8.22 (2H, d, J=7Hz) Example 16 To a solution of 4-[2-[ (3-aminoprop-l-yl)oxy]- benzoyl]amino-N-methyl-N-[2-[5-(4-methylpiperazin-l- yl)carbonylpent-1-yloxy]phenyl]benzamide (250 mg) was added 4N hydrogen chloride in ethyl acetate (1 ml) and the solution was stirred at ambient temperature for 10 minutes. The white solid was filtered and dried under reduced pressure to give 4-[2-[ (3-aminoprop-l- yl)oxy]benzoyl]amino-N-methyl-N-[2-[5-(4-methylpiperazin- 1-yl)carbonylpent-1-yloxy]phenyl]benzamidε dihydrochloridε (205 mg) as a whitε powder. NMR (D 2 0, δ) : 1.40 (2H, m) , 1.59 (2H, a), 1.70 (2H, a}, 2.09 (2H, a), 2.42 (2H, t, J=7.5Hz), 2.92 (3K, s), 2.96-3.17 (6H, a), 3.24 (3H, s), 3.41- 3.59 (2H, a), 3.69 (IH, a), 3.82 (IH, m) , 4.04- 4.20 (3H, m), 4.53 (IH, m) , 6.72 (IH, d, J=7Hz) , 6.81 (IH, t, J=7Hz), 6.93-7.60 (11H, a) Example 17 The following compounds wεre obtainεd according to a similar manner to that of Example 16. 1) 4- [2- [ (3-Acεtylaminoprop-l-yl) oxy]bεnzoyl]amino-N- methyl-N- [2- [5- (4-methylpipεrazin-l-yl) carbonylpεnt- 1-yloxy]phenyl]benzamidε hydrochloride NMR (D 2 0, δ) : 1.38 (2K, m) , 1.50-1.68 (4H, a), 1.48 (2H, a), 1.81 (3H, s) , 2.42 (2H, a), 2.90 (3H, s), 2.97-3.15 (6H, a), 3.24 (3H, s) , 3.40-3.61 (4H, a), 3.71-3.92 (2H, a), 4.14 (IK, a), 4.54 (IH, a), 6.62-6.77 (2H, a), 6.79-6.90 (2H, a), 7.00 (IH, a), 7.11 (IH, a), 7.19-7.33 (5H, a), 7.59 (IH, d, J=7Hz) 2) 4-[2-[ (3-Diaεthylaainoprop-l-yl) oxy]bεnzoyl]aaino-N- aεthyl-N- [2- [5- (4-aεtylpipεrazin-l-yl) carbonylpεnt-1- yloxy]phεnyl]bεnzaaide dihydrochloride NMR (D 2 0, δ) : 1.51 (2H, a), 1.67 (2H, a), 1.81 (2H, a), 2.22 (2H, a), 2.53 (2H, t, J=7.5Hz), 2.65 (6H, s), 2.82 (3H, s), 3.00-3.17 (2H, a), 3.23 (2K, t, J=7.5Hz), 3.37 (3H, s) , 3.89 (IH, m) , 4.13 (IH, m) , 4.07-4.20 (3H, m) , 4.58 (IH, m) , 6.92-7.00 (2H, m) , 7.11-7.18 (2H, m) , 7.26-7.48 (6H, m) , 7.54-7.60 (2H, m) 3) 4- [2- [ (4-Mεthylpipεrazin-l-yl) carbonylmεthoxy] - benzoyl] amino-N-methyl-N- [2- [5- (4-methylpiperazin-l- yl) carbonylpent-1-yloxy]phenyl]benzamidε dihydrochloridε NMR (D 2 0, δ) : 1.36 (2H, a), 1.53 (2H, a), 1.66 (2H, m), 2.98 (6H, ε), 2.91-3.25 (10K, m) , 3.30 (3H, ε), 3.37-3.69 (4H, m) , 3.77-3.96 (2K, m) , 4.35- 4.56 (2K, m), 4.82 (2H, s), 6.75 (IH, d, J=7Hz) , 6.84 (IH, t, J=7Hz), 6.92 (IH, d, J=7Hz) , 7.03- 7.15 (2H, m), 7.22 (IH, d, J=7Hz), 7.29 (2H, d, J=8.5Hz), 7.43-7.58 (3H, m) , 7.80 (IH, d, J=7Hz) 4) 4-[2-(3-Piperidinoprop-l-yloxy)benzoyl]amino-N- methyl-N-[2-[5-(4-methylpiperazin-l-yl)carbonylpent- 1-yloxy]phenyl]benzamide dihydrochloride NMR (D 2 0, δ) : 1.42-1.67 (10H, m) , 1.78 (2H, m) , 2.20 (2H, m), 2.51 (2H, t, J=7.5Hz), 2.65 (2H, a), 2.94 (3H, s), 2.95-3.21 (6H, a), 3.32 (2H, a), 3.35 (3H, s), 3.57 (2H, a), 3.92-4.04 (2H, a), 4.16-4.25 (4H, a), 6.91-6.99 (2H, a), 7.08- 7.17 (2H, a), 7.23-7.47 (6K, a), 7.52-7.60 (2H, m) 5) 4-[2-[2- (Dimethylamino)eth-l-yloxy]benzoyl]amino-N- methyl-N-[2-[5-(4-methylpiperazin-l-yl)carbonylpent- 1-yloxy]phεnyl]bεnzamide dihydrochloride NMR (D 2 0, δ) : 1.52 (2H, m) , 1.68 (2H, m) , 1.81 (2H, a), 2.52 (2H, t, J=7.5Hz), 2.82 (6H, s), 2.93 (3H, s), 2.97-3.21 (4H, a), 3.37 (3K, s), 3.48- 3.62 (2H, a), 3.87 (IH, a), 4.01 (IH, a), 4.24 (IH, a), 4.47 (2H, a), 4.57 (IH, a), 6.92-7.00 (2H, m), 7.13-7.48 (8H, m) , 7.52-7.62 (2H, m) 6) 4-[2- (3-Aminoprop-l-yl)oxy]benzoylamino-N-methyl-N- [2-[3-(4-methylpiperazin-l-yl)carbonylaminoprop-1- yloxy]phenyl]benzamide dihydrochloride NMR (D 2 0, δ) : 2.01 (2H, a), 2.17 (2H, a), 2.91 (3H, s), 2.95-3.46 (8K, a), 3.40 (3H, s) , 3.54 (2H, a), 4.02-4.16 (4H, a), 4.27 (2H, a), 6.93-7.00 (2H, a), 7.12-7.21 (2H, m) , 7.26-7.37 (2H, m) , 7.39-7.48 (4H, a), 7.54-7.64 (2H, m) 7) 4-[2-[ (3-Aminoprop-l-yl)oxy]benzoyl]amino-3-methoxy- N-methyl-N-[4-methyl-2-[5-(4-methylpiperazin-l- yl) carbonylpent-1-yloxy]phenyl]benzamidε dihydrochloride NMR (D 2 0, δ) : 1.43 (2H, m) , 1.60 (2H, m) , 1.72 (2H, a), 2.07 (2H, m) , 2.18 (3H, s), 2.45 (2H, t, J=7.5Hz), 2.90 (3H, s) , 2.92-3.13 (4H, a), 3.30 (3H, s), 3.41-3.63 (4H, a), 3.64 (3H, s) , 3.82 (IH, a), 3.92 (IH, m) , 4.04-4.61 (3H, m) , 4.50 (IH, m) , 6.66-6.74 (3H, m) , 6.93-7.04 (3H, m) , 7.10 (IH, d, J=7Hz), 7.41 (IH, t, J=7Hz), 7.73 (IH, d, J=7Hz) , 7.95 (IH, d, J=7Hz) 8) 4- [2- (3-Aminoprop-l-yl) oxy-4-mεthylbεnzoyl] amino-3- mεthoxy-N-mεthyl-N- [2- [5- (4-methylpiperazin-l- yicarbonyl)pent-1-yloxy]-4-methylphenyl]benzamide dihydrochloride NMR (CDC1 3 , δ) : 1.48-1.96 (8H, a), 2.27 (3H, s) , 2.32-2.42 (2H, a), 2.78 (3H, s) , 3.11-3.22 (2H, a), 3.28 (3H, s), 3.79 (3H, s) , 3.80-4.11 (2H, a), 4.22-4.32 (2K, a), 6.58-6.67 (2K, a), 6.79-6.96 (5H, a), 7.87 (IH, d, J=8Hz) , 8.69-8.75 (IH, a), 9.41 (IH, br) 9) 4- [2- (3-Aminoprop-l-yl) oxy-3-methylbenzoyl] amino-3- methoxy-N-methyl-N- [2- [5- (4-methylpiperazin-l- yl) carbonylpent-l-yl]oxy-4-methylphenyl]benzamide dihydrochloride NMR (CDCI3, δ) : 1.46-1.92 (6H, m) , 2.15-2.57 (4H, m), 2.24 (3K, s) , 2.30 (3H, s) , 2.62-2.98 (6H, m) , 2.80 (3H, s), 3.02-3.29 (4H, m) , 3.28 (3H, s) , 3.73-4.18 (5H, a), 4.46 (IH, br) , 4.62 (IH, br) , 6.56-6.68 (2H, a), 6.81-6.96 (3H, a), 7.10 (IH, dd, J=2, 8Hz), 7.30 (IH, d, J=8Hz) , 1.66-7.77 (IH, a), 8.28-8.52 (4H, a), 9.65 (IH, br) 10) 4- [2- (3-Acetylaainoprop-l-yl)oxybenzoyl]aaino-3-aεthoxy- N-aethyl-N- [2- [5- (4-diaethylaainopiperidin-l- yl)carbonylpent-1-yl]oxy-4-methylphenyl]benzamide hydrochloride NMR (CDC1 3 , δ) : 1.48-1.92 (6H, m) , 1.91 (3H, s) , 1.96-2.25 (2H, m) , 2.30 (3H, s), 2.30-2.39 (2H, m) , 2.68 (6H, s), 3.32 (3K, s) , 3.35-3.47 (2H, m) , 3.76 (3K, s), 4.26 (2H, br) , 4.75 (IK, br) , 6.56-7.12 (6H, a), 7.47 (IK, br), 8.10 (IH, br) , 8.39 (IH, br) 11) 4-[2-(3-Aminoprop-l-yl)oxybenzoyl]amino-3-mεthoxy-N-[2- [4- (3-aminopropionyl)aminobut-l-yl]oxy-4-methylphenyl]- N-methylbenzamide dihydrochloride NMR (CDCI3, δ) : 1.59-1.90 (4H, m) , 2.04-2.15 (2H, m) , 2.27 (3H, s), 2.30-2.44 (2H, m) , 2.87-3.08 (4H, a) 3.21-3.38 (2H, a), 3.30 (3H, s) , 3.75-3.94 (2H, a) 3.76 (3H, ε), 4.21-4.33 (2H, a), 6.55-6.68 (2H, m) 6.86-7.10 (5H, a), 7.29-7.48 (2H, m) , 8.17 (IH, br), 8.35 (IH, br) 12) 4-[2-(3-Guanidinoprop-l-yl)oxybenzoyl]amino-3-mεthoxy-N methyl-N-[2-[5-(4-dimethylaminopiperidin-l- yl)carbonylpent-1-yl]oxy-4-methylphεnyl]bεnzamide dihydrochloride NMR (CDCI3, δ) : 1.49-1.93(6H, m) , 2.05-2.41 (8H, m) , 2.27 (3H, ε), 2.75 (6H, s) , 3.08 (2K, br) , 3.29 (3H, s), 3.47 (2H, br) , 3.67-4.10 (4H, m), 3.77 (3H, s), 4.27 (2H, br) , 6.56-6.71 (2H, m) , 6.81- 7.09 (5H, m) , 7.44 (IH, br) , 7.98-8.19 (2H, m) , 8.28-8.45 (IH, m) 13) 4-(2-Hydroxybenzoyl)amino-3-methoxy-N-methyl-N-[4- methyl-2-[5-(4-methylpiperazin-l-yl)carbonylpent-1- yloxy]phenyl]benzamide hydrochloride NMR (DMSO-dg, δ) : 1.35-1.66 (4K, a), 1.66-1.83 (2H, a), 2.22 (3H, s) , 2.39 (2H, t, J=7Hz) , 2.74 and 2.76 (total 3H, s) , 2.80-3.10 (4H, a), 3.18 (3H, s ) , 3 .28-3 . 63 (2H, a) , 3 . 68 (3H, s) , 3.77-4 .18 (3H, a) , 4 . 34-4 . 52 ( IH, a) , 6. 64 (IH, d, J=9Hz ) , 6. 75- 7 . 12 ( 6H, m) , 7.40 (IH, m) , 7.98 (IH, d, J=9Hz) , 8 .23 (IH, d, J=9Hz) 14) (S)-4-[2-[ (3-Amino-l-methylprop-l-yl)oxy]benzoyl]amino- 3-aethoxy-N-aethyl-N-[4-methyl-2-[5-(4-mεthylpiperazin- 1-yl)carbonylpent-1-yloxy]phenyl]benzamide dihydrochloride NMR (DMSO-dg, δ) : 1.35 (3H, d, J=7Hz) , 1.40-1.65 (4H, a), 1.66-1.82 (2H, a), 1.92-2.20 (2H, a), 2.23 (3H, s), 2.38 (2H, t, J=7Hz), 2.64 (3H, s) , 2.78-3.43 (11H, a), 3.51-4.07 (7H, a), 4.93-5.09 (IH, a), 6.65 (IK, d, J=8Hz), 6.82 (IH, s) , 6.89 (IH, d, J=8Hz), 6.98 (IH, s), 7.04 (IH, d, J=8Hz) , 7.12 (IH, dd, J=8, 8Hz), 7.36 (IH, d, J=8Kz) , 7.57 (IH, dd, J=8, 8Hz), 7.98-8.35 (4H, a) 15) 4- (2-Aminobenzenεsulfonyl)amino-3-mεthoxy-N-mεthyl-N-[4- methyl-2-[5- (4-methylpipεrazin-i-yI)carbonylpεnt-1- yloxy]phenyl]benzamide dihydrochloride NMR (DMSO-dg, δ) : 1.36-1.45 (2H, a), 1.50-1.59 (2K, ) , 1.65-1.73 (2H, m) , 2.23 and 2.29 (total 3H, s) , 2.34-2.42 (4H, m) , 2.77 (3H, d, J=lHz) , 2.92-3.00 (2H, a), 3.11 and 3.13 (total 3H, s), 3.19 (IH, s), 3.36-3.70 (10H, a), 4.03-4.11 (IH, m) , 4.40-4.48 (IH, m) , 6.44-6.50 (IH, m) , 6.60-6.88 (6H, a), 6.94-7.10 (2H, a), 7.27-7.32 (IH, a) ESI-MASS (a/z) : 638 (M+H) 16) (R)-4-[2-[ (4-Aminobut-2-yl)oxy]benzoyl]amino-3-methoxy- N-methyl-N-[4-mεthyl-2-[5- (4-methylpipεrazin-l- yl)carbonylpεnt-1-yloxy]phεnyl]benzamide dihydrochloride NMR (DMSO-dg, δ) : 1.37 and 1.39 (total 3H, s) , 1.40- 1.78 (8H, m) , 1.94-2.12 (3H, m) , 2.23 (3H, s) , 2.30-2.40 (4K, m), 2.87-2.96 (2K, a), 3.18 (3H, s) , 3.32 (3H, s), 3.46-3.58 (2H, a), 3.77 (3H, s), 3.83-3.99 (3H, a), 4.94-5.02 (IH, m) , 6.65 (IH, d, J=8Hz) , 6.82 (IH, s), 6.88 (IH, d, J=8Hz), 6.98 (IH, s) , 7.03 (IH, d, J=8Hz), 7.13 (IH, t, J=8Hz) , 7.33 (IH, d, J=9Hz), 7.58 (IK, t, J=8Hz), 7.88-8.02 (2H, br) , 8.04 (IH, d, J=9Hz), 8.27 (IH, d, J=8Hz) ESI-MASS (m/z) : 674 (M-rH) 17) (R)-4-[2-[ (4-Aminobut-2-yl)oxy]benzoyl]amino-3-methoxy- N-methyl-N-[4-mεthyl-2-[5-(4-dimethylaminopiperidin-l- yl)carbonylpent-1-yloxyjphεnyl]benzamide dihydrochlorid NMR (DMSO-dg, δ) : 1.36 and 1.38 (total 3H, s), 1.40- 1.80 (12K, m), 1.88-2.13 (3H, m) , 2.24 (3H, s) , 2.35 (2H, t, J=8Hz), 2.51 (6H, s), 2.89-3.03 (4H, m), 3.19 (3H, s), 3.76 (3H, s) , 3.83-4.00 (3H, m) , 4.43-4.51 (IH, m) , 4.96-5.03 (IH, m) , 6.65 (IH, d, J=8Hz), 6.83 (IH, s) , 6.87-6.92 (IH, m) , 6.98 (IH, s), 7.03 (IK, d, J=8Kz), 7.14 (IH, t, J=8Hz) , 7.34 (IH, d, J=8Hz), 7.58 (IH, t, J=8Kz) , 8.04 (IH, d, J=8Hz), 8.24-8.30 (IH, m) ESI-MASS (m/z) : 702 (M+H) 18) (S)-4-[2-[ (4-Aminobut-2-yl)oxy]benzoyl]amino-3-methoxy- N-methyl-N-[4-methyl-2-[5-(4-dimethylaminopiperidin-l- yl)carbonylpent-1-yloxy]phεnyl]benzamide dihydrochlorid NMR (DMSO-dg, δ) : 1.35 and 1.38 (total 3H, s), 1.42- 1.79 (12H, m) , 1..88-2.14 (3H, a), 2.25 (3H, s) , 2.36 (2H, t, J=8Hz), 2.51 (6H, s) , 2.89-3.02 (4H, a), 3.20 (3H, s), 3.76 (3H, s) , 3.84-4.00 (3H, a), 4.43-4.50 (IH, a), 4.97-5.03 (IH, a), 6.65 (IH, d, J=8Hz), 6.82 (IK, s), 6.88-6.92 (IH, a), 6.98 (IH, s), 7.02 (IH, d, J=8Hz), 7.15 (IH, t, J=8Hz) , 7.3 (IK, d, J=8Hz), 7.58 (IH, t, J=8Hz), 8.03 (IH, d, J=8Hz), δ.24-8.30 (IH, m) ESI-MASS (m/z) : 702 (M+H) 19) 4- [2- (4-Aminobut-l-yl) oxybenzoyl] amino-N-methyl-N- [2- [5- ( 4-methylpiperazin-l-yl ) carbonylpεnt-1-yl ] oxy] - phenylbenzamide dihydrochloride NMR (D 2 0, δ) : 1.35-1.50 (2H, m) , 1.56-1.64 (2H, m) , 1.68-1.83 (4H, m) , 2.47 (2H, t, J=7.5Hz), 2.82-3.12 (5H, m), 2.92 (3H, s) , 3.33 (3H, s) , 3.43-3.61 (3H, m), 3.81 (IH, m), 3.95 (IH, m) , 6.84 (IH, d, J=7Hz), 6.91 (IH, t, J=7Hz) , 7.00-7.08 (3H, m) , 7.19 (IH, t, J=7Hz), 7.26-7.37 (4H, m) , 7.48 (IH, t, J=7Hz), 7.62 (IH, d, J=7Hz) 20) 4-[2-(3-Aminoprop-l-yl)oxybεnzoyl]amino-N-[2- (5- ethoxycarbonylpent-l-yl)oxy-4-methyl]phεnyl-N- mεthylbεnzamidε hydrochoiride NMR (DMSO-dg, δ) : 1.16 (3H, t, J=7.5Hz), 1.38-1.49 (2H, m), 1.55-1.64 (2H, m) , 1.67-1.77 (2H, m) , 1.98-2.08 (2H, ) , 2.21 (3H, s) , 2.31 (2H, t, J=7.5Hz), 2.87-2.97 (2H, m) , 3.16 (3H, s) , 3.80-3.98 (2H, m) , 4.03 (2H, q, J=7.5Hz), 4.19 (2H, t, J=7.5Hz), 6.62 (IH, d, J=7Hz), 6.80 (IH, s) , 6.98-7.07 (2H, m), 7.15 (IH, d, J=7Hz) , 7.22 (2H, d, J=8Hz), 7.43-7.57 (4H, ) , 7.86-8.00 (3H, br) 21) 4-[2- (3-Aminoprop-l-yl)oxybenzoyl]amino-N-methyl-N-[4- methyl-2-[5-(4-methylpipεrazin-l-yl)carbonylpent-1- yl]oxy]phenylbenzamide. dihydrochloride NMR (DMSO-dg, δ) : 1.38-1.49 (2H, m) , 1.52-1.62 (2H, a), 1.68-1.78 (2H, a), 1.96-2.09 (2H, a), 2.21 (3H, s), 2.38 (2H, t, J=7.5Hz), 2.73 . (3Hxl/2, s), 2.75 (3Hxl/2, s), 2.81-3.07 (4H, a), 3.15 (3K, s) , 3.30-3.54 (4H, a), 3.81-4.21 (5H, a), 4.45 (IH, a), 6.65 (IH, d, J=7Hz), 6.81 (IK, s) , 6.99-7.08 (2H, a), 7.15 (IH, d, J=7Hz) , 7.22 (2H, d, J=8Hz) , 7.45- 7.60 (4H, a), 8.04 (2H, br) 22) 4- [2- (3-Aminoprop-l-yl) oxybenzoyl] amino-N-methyl-N- [2- [3- (4-methylpiperazin-l-yl) carbonylprop-1-yl] oxy] - phenylbenzamide dihydrochloride NMR (DMSO-dg, δ) : 1.90-2.09 (4H, a), 2.48-2.59 (2H, a), 2.72 (3Hxl/2, s), 2.73 (3Hxl/2, s), 2.83-3.10 (4H, a), 3.20 (3H, s) , 3.33-3.56 (3H, m) , 3.88-4.0 (3H, m) , 4.18 (2H, t, J=7.5Hz), 4.47 (IH, m) , 4.80 (IH, m), 6.87 (IH, t, J=7Kz) , 6.98 (IH, d, J=7Hz) , 7.04 (IH, t, J=7Hz), 7.11-7.26 (5H, m) , 7.44-7.59 (4H, m) , 8.05 (2H, br) 23) 4- [2- (3-Aminoprop-l-yl) oxybenzoyl] amino-N-methyl-N- [4- methyl-2- (4-methylpiperazin-l-ylcarbonyl) phenylmethoxy] phenylbenzamide dihydrochloride NMR (DMSO-dg, δ) : 1.97-2.07 (2H, m) , 2.26 (3H, s) , 2.75 (3Hxl/2, s) , 2.77 (3Hxl/2, s) , 2.82-2.95 (2H, a), 3.02-3.14 (2H, a), 3.21 (3H, s) , 3.30-3.49 (4H a), 3.97-4.21 (4H, a), 5.09 (IH, d, J=14Hz) , 5.20 (IH, d, J=14Hz), 6.70 (IH, d, J=7Hz) , 6.93 (IH, s) 7.02-7.25 (5H, a), 7.43-7.57 (8H, a), 7.92-8.04 (3H, br) 24) 4-[2-(3-Hydroxyprop-l-yl)oxybenzoyl]amino-N-methyl-N-[2 [5-(4-methylpiperazin-l-yl)carbonylpent-l-yl]oxy]- phenylbenzamide hydrochloride NMR (DMSO-dg, δ) : 1.39-1.50 (2K, a), 1.52-1.62 (2H, a), 1.69-1.79 (2H, a), 1.84-1.93 (2H, a), 2.40 (2 t, J=7.5Hz), 2.70 (3Hxl/2, s) , 2.72 (3Hxl/2, s), 2.82-3.07 (4H, a), 3.19 (3H, s) , .3.28-3.60 (4H, a) 3.80-3.98 (2H, a), 4.10 (IH, a), 4.17 (2H, t, J=7.5Hz), 4.45 (IH, a), 6.85 (IH, t, J=7Hz), 6.98 (IH, d, J=7Hz), 7.03 (IH, t, J=7Hz) , 7.13-7.24 (5 a), 7.43-7.54 (3H, a), 7.62 (IH, d, J=7Hz) 25) 4-[2- (4-Hydroxy-1-butyn-l-yl)benzoyl]amino-N-methyl-N- [2-[5-(4-aεthylpipεrazin-l-yl)carbonylpent-1-yl]oxy]- phenylbenzaaide hydrochloride NMR (DMSO-dg, δ) : 1.42-1.52 (2H, a), 1.54-1.64 (2H, a), 1.70-1.82 (2H, a), 2.37-2.47 (6H, a), 2.49 (3H, ε), 2.51 (3H, s), 2.84-3.05 (2H, a), 3.32-3.46 (4H, a), 3.84-3.98 (2H, a), 4.08 (IH, a), 4.47 (IH, a), 6.84 (IH, t, J=7Hz), 6.97 (IH, d, J=7Hz), 7.13-7.25 (4K, a), 7.41-7.53 (6H, a) 26) 4-[2-(4-Aminobut-l-yl)benzoyl]amino-N-methyl-N-[2-[5-(4- methylpipεrazin-1-yl)carbonylpεnt-l-yl]oxy]- phenylbenzamide dihydrochloride NMR (DMSO-dg, δ) : 1.39-1.62 (8H, m) , 1.67-1.80 (2H, m), 2.39 (3H, t, J=7.5Hz), 2.50 (3H, s) , 2.63-2.73 (4H, m) , 2.81-3.08 (2H, m) , 3.18 (3H, s), 3.31-3.42 (4H, m), 3.85-4.00 (2H, m) , 4.04 (IH, m) , 4.43 (IH, m), 6.84 (IH, t, J=7Hz), 6.99 (IH, d, J=7Hz) , 7.11-7.42 (6H, m) , 7.50-7.56 (2H, m) , 7.75-7.91 (2H, m) 27) 4-[2-[ (3-Aminoprop-l-yl)oxy]benzoyl]amino-3-methoxy-N- methyl-N-[4-methyl-2-[5- (4-methylpiperazin-l-yl)- carbonylpent-l-yl]oxy]phεnylbεnzamidε hydrochloride NMR (DMSO-dg, δ) : 1.40-1.51 (2H, m) , 1.53-1.62 (2H, a), 1.69-1.80 (2H, m) , 1.98 (3H, s) , 1.98-2.03 (2H, a), 2.22 (3H, s) , 2.39 (2H, t, J=7.5Hz), 2.71 (3Hxl/2, s), 2.74 (3Hxl/2, s) , 2.83-3.05 (2H, a), 3.31-3.50 (3H, a), 3.56 (2K, t, J=7.5Hz), 3.72 (3H, s), 3.81-4.11 (5H, a), 4.32 (2H, t, J=7.5Hz), 4.43 (IH, a), 6.65 (IH, d, J=7Hz), 6..81 (IH, s) , 6.87- 6.95 (2H, a), 7.05 (IH, d, J=7Hz) , 7.11 (IH, t, J=7Hz), 7.26 (IH, d, J=7Hz) , 7.54 (IH, t, J=7Hz) , 8.03 (IH, d, J=7Hz), 8.28 (IH, d, J=7Hz) 28) 3-Methoxy-4-(2-hydroxybenzoyl)amino-N-methyl-N-[4- methyl-2-[4-(4-methylpiperazin-l-yl)carbonyl]- phenylmethoxy]phenylbenzamidε hydrochloride NMR (DMSO-dg, δ) : 2.23 (3H, s) , 2.75 (3Hxl/2, s) , 2.77 (3Hxl/2, s) , 2.97-3.15 (2H, m) , 3.21 (3H, s) , 3.24-3.80 (6H, m) , 5.06 (IH, d, J=14Hz), 5.19 (IH, d, J=14Hz), 6.70 (IH, d, J=7Hz), 6.90-7.01 (3H, m) 7.10 (IH, d, J=7Hz), 7.22 (2H, d, J=8Hz), 7.41 (IH d, J=7Hz), 7.44-7.55 (7K, m) , 7.87 (IH, d, J=7Hz) 29) 4-[2-(3-Aminoprop-l-yl)oxybεnzoyl]amino-3-methoxy-N- methyl-N-[4-methyl-2-[4-(4-methylpiperazin-l- yl)carbonyl]phenylmethoxy]phenylbenzamide dihydrochloride NMR (DMSO-dg, δ) : 2.06-2.19 (2H, a), 2.23 (3H, s) , 2.75 (3H, s), 2.87-2.98 (2H, a), 3.02-3.15 (2H, a) 3.23 (3K, s), 3.32-3.49 (2H, a), 3.65 (3H, s) , 3.71-3.96 (4H, a), 4.29-4.40 (2H, a), 5.04 (IH, d, J=14Hz), 5.20 (IH, d, J=14Hz) , 6.76 (IK, d, J=7Hz) 6.88 (IK, d, J=7Hz), 6.90-6.98 (2H, a), 7.09-7.19 (2H, m), 7.28 (IH, d, J=7Hz) , 7.50-7.62 (2H, m) , 7.98-8.15 (4H, m) , 8.23 (IH, d, J=7Hz) 30) 3-Methoxy-4-[2- (3-aminoprop-l-yl)cxy]phenylmethyl]- amino-N-methyl-N-[4-methyl-2-[5-(4-methylpipεrazin-l- yl)carbonylpent-l-yl]oxy]phenylbεnzamidε trihydrochloridε NMR (DMSO-dg, δ) : 1.35-1.47 (2H, a), 1.49-1.59 (2H, a), 1.64-1.74 (2K, a), 2.00-2.10 (2H, a), 2.22 (3 s), 2.30-2.38 (2H, m) , 2.69 (3Hxl/2, s) , 2.73 (3Hxl/2, s), 2.82-3.03 (6H, a), 3.09 (3K, s) , 3.2 3.41 (2H, a), 3.53 (3H, s) , 3.83-4.12 (6H, a), 4. (2H, s), 4.70 (IH, br), 6.21 (IH, d, J=7Hz) , 6.58 6.66 (2H, a), 6.71-6.99 (5H, a), 7.09 (IK, d, J=7Hz), 7.20 (IH, t, J=7Hz) , 8.02 (2H, br d) 31) 4- (2-Dimεthylamino-4-methyl)phenoxymethyl-N-methyl-N-[4- mεthyl-2-[5-(4-mεthylpipεrazin-l-yl)carbonylpεnt-1- yl]oxy]phεnylbεnzamidε dihydrochloridε NMR (DMSO-dg, δ) : 1.37-1.47 (2H, m) , 1.50-1.61 (2H, a), 1.67-1.80 (2H, a), 2.20 (3H, ε), 2.29 (3H, s), 2.39 (2H, t, J=7.5Hz), 2.71 (3Hxl/2, s), 2.73 (3Hxl/2, s), 2.80-3.58 (4H, a), 3.03 (6H, s) , 3.17 (3H, s), 3.72-4.48 (6H, a), 5.21 (2H, s) , 6.62 (IH, d, J=7Hz), 6.78 (IK, s) , 6.91 (IH, d, J=7Hz) , 7.02 (IH, d, J=7Hz), 7.11 (IH, d, J=7Hz) , 7.26 (2H, d, •J=8Hz), 7.37 (2H, d, J=8Hz) , 7.70 (IH, d, J=7Hz) 32) 4-[2- (3-Aminoprop-l-yI)oxybεnzoyl]amino-3-mεthoxy-N- mεthyl-N-[2-[4- (4-mεthylpipεrazin-l-yl)carbonyl]- phenyleth-1-yl]phenylbenzamide dihydrochloride NMR (DMSO-dg, δ) : 2.06-2.19 (2H, m) , 2.55-3.12 (10H, m), 2.71 (3Hxl/2, s), 2.73 (3Hxl/2, s) , 3.18 (3H, s), 3.23-3.48 (2H, m) , 3.66 (3H, s) , 3.66-3.81 (2H, m), 4.30-4.40 (2H, m) , 6.86-6.90 (2K, a), 7.11 (IH, t, J=7Hz), 7.20-7.42 (9H, m) , 7.59 (IH, t, J=7Hz) , 8.01 (IH, d, J=7Hz), 8.08 (2H, br) , 8.27 (IH, d, J=7Hz) 33) 4-[2- (3-Aminoprop-l-yl)thiobεnzoyl]amino-3-mεthoxy-N- mεthyl-N-[4-mεthyl-2-[5- (4-methylpiperazin-l-yl)- carbonylpent-1-yl]oxy]phenylbenzamide dihydrochloride NMR (DMSO-dg, δ) : 1.40-1.51 (3K, m) , 1.52-1.63 (2H, m), 1.70-1.88 (4H m), 2.23 (3H, s) , 2.40 (3H, t, J=7.5Hz), 2.71 (3Hxl/2, s) , 2.72 (3Hxl/2, s), 2.80- 2.91 (2H, m), 2.94-3.06 (2H, a), 3.17 (3K, s) , 3.32-3.67 (8H, a), 3.60 (3H, s) ,• 3.81-4.10 (3K, a), 4.41 (IH, a), 6.65 (IH, α, J=7Hz), 6.82 (IH, s) , 6.86-6.92 (2K, a), 7.02 (IH, d, J=7Hz) , 7.27 (IH, t, J=7Hz), 7.41-7.52 (3K, a), 7.71 (IH, d, J=7Hz) , 9.37 (IH, s) 34) 4-[2-(3-Aminoprop-l-yl)oxybenzoyl]amino-3-methoxy-N-[2- [4-(4-dimethylaminopiperidin-l-yl)carbonylJphenylmeth- oxy-4-methyl]phenyl-N-methylbenzamide dihydrochloride NMR (DMSO-dg, δ) : 1.57-1.73 (2H, m) , 2.00-2.20 (4H, m), 2.23 (3K, s), 2.70 (3H, s) , 2.71 (3K, s), 2.87 3.05 (3H, m), 3.24 (3H, s) , 3.33-3.50 (IH, m) , 3.6 (3H, s), 3.71-4.05 (4H, m) , 4.37 (2H, t, J=7.5Hz), 5.02 (IH, d, J=14Hz), 5.20 (IH, d, J=14Hz) , 6.73 (IH, d, J=7Hz), 6.86 (IH, d, J=7Hz), 6.96 (2H, s), 7.10-7.19 (2H, m), 7.29 (IH, d, J=7Hz) , 7.43-7.52 (4H, a), 7.58 (IH, t, J=7Hz) , 8.00 (IH, d, J=7Hz) , 8.03 (IH, d, J=7Hz) 35) 4-[2-(3-Aainoprop-l-yl)oxybenzoyl]amino-3-methoxy-N- methyl-N-[2-[3-(4-methylpipεrazin-l-yl)carbonyl- methoxyprop-1-yl]oxy]phenylbεnzamidε dihydrochloride NMR (DMSO-dg, δ) : 1.94-2.04 (2H, m) , 2.10-2.20 (2H, a), 2.71 (3Hxl/2, s), 2.23 (3Hxl/2, s), 2.84-3.10 (6H, a), 3.21 (3H, s) , 3.31-3.50 (2H, a), 3.57-3.8 (4H, a), 3.74 (3H, s) , 3.90-4.01 (2H, a), 4.20 (2Hxl/2, s), 4.22 (2Hxl/2, d) , 4.35 (2H, t, J=7.5Hz), 6.82-6.97 (3H, a), 7.01 (IH, d, J=7Hz) , 7.10-7.28 (4H, a), 7.58 (IH, t, J=7Hz) , 8.03 (IH, d, J=7Hz), 8.27 (IH, d, J=7Hz) 36) 4-[2- (3-Aminoprop-l-yl)oxybenzoyl]amino-3-methoxy-N-[2- [ (E)-5-(4-dimethylaminopipεridin-l-yl)carbonyl-4-pente 1-yl]oxy-4-m thyl]phenyl-N-methylbεnzamidε dihydrochloride NMR (DMSO-dg, δ) : 1.36-1.63 (2H, m) , 1.84-1.92 (2H, a), 1.97-2.08 (2H, m) , 2.10-2.22 (2H, m) , 2.22 (3 s), 2.29-2.43 (2H, a), 2.63 (3K, s), 2.65 (3H, s) , 2.70-2.86 (2H, a), 2.88-3.00 (2H, a), 3.14 (3Hxl/ s), 3.17 (3Hxl/2, s), 3.28-3.42 (2H, a), 3.71 (3H s), 3.84-4.06 (2H, a), 4.37 (2H, t, J=7.5Hz), 4.5 ( IH, m) , 6.52 ( IH, d, J=15Hz) , 6. 60 ( IH, m) , 6.73- 7 . 07 ( 5K, m) , 7 . 13 ( IH, t, J=7Hz) , 7 .27 ( IH, d, J=7Hz) , 7.56 (IH, t, J=7Hz) , 8 .01 (IH, d, J=7Hz) , 8 . 30 ( IH, d, J=7Hz) 37) 4-[2- (3-Aminoprop-l-yl)oxybenzoyl]amino-3-mεthoxy-N- methyl-N-[4-methyl-2-[5-(4-methylpiperidin-l- yl)carbonylpent-I-yl]oxy]phenylbenzamide hydrochloride NMR (CDC1 3 , δ) : 0.88 (3H, d, J=7.5Hz), 0.90-1.10 (2H, a), 1.34-1.61 (6H, a), 1.70-1.80 (2H, a), 2.10-2.20 (2H, a), 2.23 (3H, s) , 2.30 (2H, t, J=7.5Hz), 2.45 (IH, a), 2.85-3.00 (3H, a), 3.18 (3H, s) , 3.74 (3H, s), 3.75-4.02 (4H, a), 4.38 (2H, t, J=7.5Hz), 4.78 (IH, a), 6.65 (IH, d, J=7Hz) , 6.82 (IH, s) , 6.88 (IH, d, J=7Hz) , 6.98 (IH, s) , 7.02 (IH, d, J=7Hz), 7.13 (IH, t, J=7Hz), 7.26 (IH, d, J=7Hz) , 7.59 (IH, t, J=7Hz), 8.00 (IH, d, J=7Hz) , 8.22 (IH, d, J=7Hz) 38) 4- (2,4-Dimethoxybεnzoyl)amino-3-mεthoxy-N-methyl-N-[4- mεthyl-2-[5-(4-mεthylpipεrazin-l-yl)carbonylpent-1- yl]oxy]phεnylbεnzamidε hydrochloridε NMR (DMSO-dg, δ) : 1.40-1.51 (2H, m) , 1.51-1.64 (2H, a), 1.69-1.82 (2H, a), 2.22 (3H, ε), 2.38 (2H, t, J=7.5Hz), 2.73 (3H, s) , 2.81-3.09 (4H, a), 3.19 (3H, ε), 3.25-3.50 (2H, a), 3.76 (6H, sx2), 3.77- 4.15 (3H, m) , 4.00 (3H, ε), 4.44 (IH, m) , 6.64 (IH, d, J=7Hz), 6.81 -(IH, ε), 6.88-6.95 (2H, m) , 7.03 (IH, d, J=7Hz), 7.12-7.23 (2K, m) , 7.57 (IH, m) , 8.29 (IH, d, J=7Hz) 39) 4-[2- (3-Aminoprop-l-yl)oxybεnzoyl]amino-3-mεthoxy-N-[2- (3-aminoprop-l-yl)oxy-4-mεthyl]phenyl-N-methylbεnzamide dihydrochloride NMR (DMSO-dg, δ) : 2.00-2.11 (2H, m) , 2.13-2.20 (2H, a) , 2 .25 (3H, s) , 2 . 87-3 .00 (4H, a) , 3 .19 (3H, s) , 3.77 (3H, s) , 3.89-4.10 (2H, a) , 4 .36 (2H, t, J=7 .5Hz) , 6. 69 (IH, d, J=7Hz) , 6. 82 (IH, s) , 6. 89 (IH, d, J=7Hz) , 7 .04 (IH, s) , 7 . 05 (IH, d, J=7Hz) , 7.15 (IH, d, J=7Hz) , 7.38 (IH, d, J=7Hz) , 7.56 (IH, t, J=7Hz) , 8 . 01 (IH, d, J=7Hz) , 8 .28 (IH, d, J=7Hz) 40) 4-[2-(3-Aainoprop-l-yl)oxybenzoyl]aaino-3-aethoxy-N-[2- (4-aainobut-l-yl)oxy-4-aεthyl]phenyl-N-methylbenzaaide dihydrochloride NMR (DMSO-dg, δ) : 1.66-1.85 (4H, a), 2.10-2.20 (2H, a), 2.22 (3H, s), 2.80-3.01 (4H, m) , 3.18 (3H, s) , 3.75 (3H, s), 3.81-4.03 (2K, a), 4.36 (2H, t, J=7.5Hz), 6.64 (IH, d, J=7Hz) , 6.34 (IH, s) , 6.90 (IK, d, J=7Hz), 6.96 (IH, s) , 7.01 (IH, d, J=7Hz) , 7.14 (IH, t, J=7Hz), 7.27 (IK, d, J=7Hz) , 7.57 (IH, t, J=7Hz), 8.00 (IH, d, J=7Hz), 8.25 (7H, d, J=7Hz) 41) 4-[2- (3-Aminoprop-l-yl)oxybenzoyl]amino-3-mεthoxy-N-[2- (4-acetylaminobut-l-yl)oxy-4-methyl]phenyl-N- methylbenzamidε hydrochloridε NMR (DMSO-dg, δ) : 1.49-1.59 (2H, a), 1.67-1.77 (2H, a), 1.80 (3H, s), 2.06-2.20 (2H, a), 2.21 (3H, s) , 2.86-3.00 (2H, a), 3.03-3.13 (2H, a), 3.18 (3H, s) , 3.74 (3K, s), 3.80-4.02 (2H, a), 4.35 (2H, t, J=7.5Hz), 6.64 (IH, d, J=7Hz) , 7.82 (IH, s), 7.88 (IH, d, J=7Hz), 7.96 (IH, ε), 7.02 (IH, d, J=7Hz), 7.13 (IH, t, J=7Hz), 7.26 (IK, d, J=7Hz), 7.57 (IH t, J=7Hz), 8.00 (IK, d, J=7Hz), 8.23 (IH, d, J=7Hz 42) 4-[2- (3-Aainoprop-l-yl)oxybεnzoyl]aaino-3-mεthoxy-N-[2- (4-aminoacetylaminobut-l-yl)oxy-4-methyl]phenyl-N- methylbenzamide dihydrochloride NMR (DMSO-dg, δ) : 1.53-1.64 (2H, a), 1.70-1.81 (2H, a), 2.09-2.21 (2H, a), 2.22 (3H, s) , 2.86-2.98 (2H m) , 3.11-3.23 (2H, m) , 3.17 (3H, s), 3.47-3.56 (2H, a), 3.65-4.00 (2H, a), 3.76 (3K, s) , 4.38 (2H, t, J=7.5Hz), 6.65 (IK, d, J=7Kz) , 6.82 (IH, s) , 6.89 (IH, d, J=7Hz), 6.95 (IH, s) , 7.03 (IH, d, J=7Hz), 7.12 (IH, t, J=7Hz), 7.25 (IH, d, J=7Hz) , 7.56 (IH, t, J=7Hz), 8.00 (IK, d, J=7Hz) 8.22 (IH, d, J=7Hz) 43) 3-Methoxy-4-[2- (pipεridin-4-yl)oxybenzoyl]aaino-N- aethyl-N-[4-aethyl-2-[5-(4-aεthylpipεrazin-l- yl)carbonylpεnt-1-yl]oxy]phεnylbenzaaide dihydrochloride NMR (DMSO-dg, δ) : 1.38-1.49 (2H, a), 1.49-1.61 (2H, a), 1.66-1.76 (2H, a), 1.85-1.97 (2H, a), 2.20 (3H, ε), 2.67 (2H, t, J=7.5Hz), 2.73 (3Hxl/2, ε), 2.74 (3Hxl/2, ε), 2.80-3.13 (6H, a), 3.13 (3K, s) , 3.22- 3.51 (6K, ) , 3.60-4.13 (3H, a), 3.74 (3H, s) , 4.43 (IH, a), 4.91 (IH, a), 6.65 (IH, d, J=7Hz), 6.81 (IH, ε), 6.89 (IH d, J=7Hz) , 6.96 (IH, s) , 7.03 (IH, d, J=7Hz), 7.12 (IH, _, J=7Hz) , 7.35 (IK, d, J=7Hz), 7.56 (IH, t, J=7Hz), 7.81 (IK, d, J=7Hz) , 8.27 (IH, d, J=7Hz) 44) 4-[2- (3-Amino-l-aethylprop-l-yl)oxybenzoyl]amino-3- mεthoxy-N-mεthyl-N-[4-mεthyl-2-[5- (4-mεthylpipεrazin-l- yl)carbonylpεnt-1-yl]oxy]phεnylbenzamidε dihydrochloride NMR (DMSO-dg, δ) : 1.35 (3H, d, J=7.5Hz), 1.40-1.63 (4H, ) , 1.67-1.80 (2H, m) , 1.90-2.18 (2H, a), 2.22 (3H, 8), 2.39 (2H, t, J=7.5Hz), 2.71 (3Hxl/2, s) , 2.74 (3Hxl/2, s) , 2.80-3.09 (4K, a), 3.18 (3H, s), 3.30-3.52 (4H, a), 3.77 (3H, s) , 3.83-4.18 (3H, a), 4.42 (IH, a), 5.01 (IH, a), 6.64 (IH, d, J=7Hz), 6.81 (IH, ε), 6.89 (IK, d, J=7Hz) , 6.96 (IH, s) , 7.03 (IH, d, J=7Hz), 7.12 (IH, t, J=7Hz) , 7.34 (IH, d, J=7Hz), 7.58 (IH, t, J=7Hz) , 8.03 (IH, d, J=7Hz), 8.28 (IH, d, J=7Hz) 45) 3-Methoxy-4-[2-(pyrid-3-yl)methoxybenzoyl]amino-N- methyl-N-[4-methyl-2-[5-(4-mεthylpiperazin-l- yl)carbonylpent-1-yl]oxy]phenylbenzamide dihydrochloride NMR (DMSO-dg, δ) : 1.36-1.49 (2H, m) , 1.49-1.60 (2H, a), 1.66-1.79 (2H, a), 2.20 (3H, s), 2.39 (2H, t, J=7.5Hz), 2.68 (3Hxl/2, s) , 2.70 (3Hxl/2, s) , 2.80- 3.10 (4H, m) , 3.16 (3K, s) , 3.35 (3K, s) , 3.35-3.60 (2H, m), 3.79-4.11 (3H, m) , 4.41 (IH, a), 5.58 (2H, s), 6.64 (IH, d, J=7Hz), 6.80-6.90 (3H, m) , 7.02 (IH, d, J=7Hz), 7.16 (IH, t, J=7Hz) , 7.33 (IH, d, J=7Hz), 7.57 (IH, t, J=7Kz), 7.93-8.00 (2H, a), 8.19 (IH, d, J=7Hz), 8.55 (IH, d, J=7Hz) , 8.88 (IH, G, J=6Hz), 9.04 (IH, s) 46) 4-[2- (4-Aminobut-l-yl)oxybenzoyl]amino-3-methoxy-N- methyl-N-[4-methyl-2-[5-(4-methylpiperazin-l- yl)carbonylpent-1-yl]oxy]phenylbenzamide dihydrochloride NMR (DMSO-dg, δ) : 1.40-1.50 (2H, ) , 1.50-1.61 (2H, a), 1.66-1.79 (4H, a), 1.86-1.95 (2H, a), 2.21 (3H, s), 2.39 (2K, t, J=7.5Hz), 2.73 (3Hxl/2, s), 2.75 (3Hxl/2, s), 2.79-3.10 (4H, a), 3.19 (3H, s) , 3.31- 3.52 (4H, a), 3.74 (3H, s) , 3.82-4.12 (3H, a), 4.30 (2H, t, J=7.5Hz), 4.43 (IH, a), 6.65 (IH, d, J=7Hz), 7.81 (IH, s), 6.89 (IH, d, J=7Hz) , 6.97 (IH, ε), 7.03 (IH, d, J=7Hz) , 7.12 (IH, t, J=7Hz) , 7.30 (IK, d, J=7Hz), 7.58 (IH, d, J=7Hz) , 8.04 (IH, d, J=7Hz), 8.30 (IH, d, J=7Hz) 47) 4-(2-Kydroxy-5-aεthylbεnzoyl)amino-3-methoxy-N-mεthyl-N- [2-[5-(4-methylpiperazin-l-yl)carbonylpent-l-yl]oxy-4- methylphenyl]benzamide hydrochloride NMR (DMSO-dg, δ) : 1.53-1.96 (6H, a), 2.29 (3H, s) , 2.31 (3K, s), 2.33-2.40 (2H, a), 2.79 (3H, s) , 3.30 (3K, s), 3.79 (3H, s) , 3.80-4.03 (2H, a), 6.63 (2H, br), 6.88-6.98 (4H, a), 7.25 (IH, d, J=8Hz), 8.19 ( IH, d, J=8Hz ) , 8 . 71 ( IH, br) 48) 4- (2-Hydroxy-4-methoxybenzoyl) amino-3-mεthoxy-N-methyl- N- [2- [5- (4-methylpiperazin-l-yl) carbonylpent-1-yl]oxy-4- methylρhenyl]bεnzamidε hydrochloridε NMR (CDC1 3 , δ) : 1.48-1.92 (6K, m) , 2.28 (3H, s) , 2.32-2.45 (2H, a), 2.64-3.05 (4H, a), 2.79 (3H, s) , 3.29 (3K, s), 3.29-3.51 (4H, a), 3.76 (3H, s) , 3.80 (3H, ε ) , 3.81-4.05 (4H, a), 6.43-6.50 (2H, a), 6.61 (IK, br), 6.85-6.96 (3H, a), 7.36-7.43 (IH, a), 8.12-8.18 (IH, a), 8.58 (IH, br) Example 18 The following compounds were obtained by separating the coapounds, which were prepared according to a siailar aanner to Exaaple 4, by using silica gel coluan chroaatography. 1) 4- (2-Benzyloxy) enzoylaaino-3-aεthoxy-N- [ (E) -2- (4- carboxypher.yl ) ethεn-l-yl]phenyl-N-aethylbenzaaide NMR (CDCI3, δ) : 3.08 (3H, s) , 3.41 (3H, s) , 5.19 (2H, s), 6.47 (IK, d, J=14Hz), 6.58 (IH, d, J=14Hz) , 6.73 (2H, d, J-6HΣ), 6.84 (IH, d, J=7Hz) , 6.90-7.10 (5H, a), 7.20-7.40 (8H, a), 7.71 (2H, d, J=8Hz) , 8.26 (IH, d, J=7Hz), 8.38 (IH, d, J=7Hz) 2) 4- (2-Benzyloxy)bεnzoylaaino-3-aεthoxy-N- [ (Z) -2- (4- carboxy hεnyl) ethen-1-yl]phenyl-N-methylbenzamide NMR (CDCI3, δ) : 3.09 (3K, s) , 3.48 (3H, s) , 5.25 (2H, s), 6.72-7.42 (15H, a), 7.51-7.64 (3H, a), 8.10 (2H, d, J=8Hz), 8.22 (IH, d, J=7Hz) , 8.33 (IH, d, J=7Hz) Example 19 The following compound was obtained according to a similar manner to that of Example 4 by using 4- [2- (acetoxy)benzoyl]aaino-3-aethoxy-N-aethyl-N-[4-aethyl-2-(5- εthoxycarbonylpent-1-yloxy)phenyl]benzamidε as a starting compound. 4-[2-(Hydroxy)benzoyl]amino-3-methoxy-N-methyl-N-[4- methyl-2-(5-carboxypent-l-yloxy)phεnyl]benzamide NMR (CDC1 3 , δ) : 1.46-1.61 (2H, a), 1.63-1.90 (4H, a), 2.28 (3H, s), 2.39 (2H, t, J=7Hz) , 3.33 (3K, s) , 3.73-4.00 (5H, a), 6.61 (2H, br s), 6.82-7.11 (5H, a), 7.35-7.53 (2K, a), 8.16 (IH, d, J=8Hz), 8.75 (IH, br ε) Example 20 The following coapoundε were obtained according to a εiailar aanner to that of Exaaole 8. 1) 4-[2-(4-Methoxybenzyl)oxybenzoyl]aaino-N-aethyl-N-[4- aethyl-2-[4- (4-aεthylpipεrazin-l-yl)carbonyl]- phεnylmethoxy]phenylbenzamide NMR (CDCI3, δ) : 2.27 (3K, ε) , 2.31 (3H, s) , 2.35-2.53 (4H, a), 3.32 (3H, s) , 3.39-3.54 (2H, a), 3.67-3.85 (3K, a), 3.82 (3K, ε), 4.95 (IH, d, J=14Hz) , 5.06 (IK, d, J=14Hz), 5.12 (2H, ε) , 6.59-6.67 (2H, a), 6.86-7.02 (5H, a), 7.07-7.21 (4H, a), 7.33-7.52 (7H, a), 8.28 (IH, d, J=7Hz) 2) 4- (2-Benzyloxybenzoyl)aaino-3-aethoxy-N-aethyl-N-[2-[5- (4-methylpipεrazin-l-yl)carbonylpεnt-1-yloxy]phεnyl]- bεnzaaide NMR (CDCI3, δ) : 1.46-1.60 (2H, a), 1.63-1.92 (4H, a), 2.30 (3H, ε), 2.31-2.46 (6H, a), 3.28 (3H, s) , 3.35 (3H, 8), 3.44-3.54 (2H, m) , 3.58-3.69 (2K, a), 3.80-4.04 (2H, a), 5.30 (2H, s) , 6.73-7.22 (8H, a), 7.30-7.49 (6H, a), 8.19-8.28 (IH, a), 8.38 (IH, d, J=9Hz) 3) 4- [2- (Bεnzyloxy)bεnzoyl]amino-2-chloro-N-mεthyl-N-[2- [5- (4-methylpiperazin-l-yl)carbonylpent-l-yloxy]phenyl]- benzamide NMR (CDC1 3 , δ) : 1.48-1.65 (2H, m) , 1.65-1.97 (4H, a), 2.30 (3H, s), 2.32-2.48 (6H, a), 3.34 (3H, s) , 3.43-3.56 (2H, a), 3.58-3.70 (2H, a), 3.97 (2H, t, J=7Hz), 5.16 (2H, ε), 6.63-6.81 (3H, a), 6.96 (IH, d, J=8Hz), 7.02-7.20 (5H, a), 7.40-7.59 (6H, a), 8.24 (IH, a) 4) 4- [2- [ (3-tert-Butoxycarbonylaainoprop-l-yl) oxy]benzoyl] - amino-3-methoxy-N-methyl-N- [4- [5- (4-methylpiperazin-l- yl) carbonylpent-1-yloxy]phenyl]benzaaidε NMR (CDCI3, δ) : 1.42 (9H, ε), 1.45-1.82 (8H, a), ' 2.10-2.19 (2H, a), 2.30 (3H, s) , 2.31-2.41 (6H, a), 3.27-3.35 (2H, a), 3.43-3.50 (5H, a), 3.60-3.67 (2H, a), 3.82 (3H, s) , 3.90 (IH, t, J=7Hz) , 4.27 (IH, t, J=7Hz), 4.75-4.82 (IH, br) , 6.76 (2H, d, J=8Hz), 6.82 (IH, d, J=8Hz) , 6.95-7.04 (3H, m) , 7.07-7.13 (IH, m) , 7.47 (IH, t, J=8Hz) , 8.22 (IH, dd, J=l, 8Hz), 8.42 (IH, d, J=8Hz) ESI-MASS (m/z) : 746 (M+H) 5) 4- [2- [3- (tεrt-Butoxycarbonyl) aminoprop-1-yl]oxybεnzoyl] - amino-N-mεthyl-N- [4-mεthyl-2- [5- (4-methylpipεrazin-l- yl) carbonylpεnt-l-yl]oxy]phεnylbεnzamidε NMR (CDCI3, δ) : 1.40 (9H, s) , 1.45-1.60 (2H, m) , 1.65-1.74 (2H, a), 1.78-1.89 (2H, m) , 2.04-2.15 (2H, m), 2.27 (3K, s), 2.30 (3K, s) , 2.32-2.42 (6H, m), 3.27-3.39 (2K, m) , 3.33 (3H, s) , 3.44-3.50 (2H, m), 3.58-3.64 (2H, m) , 3.82-4.00 (2H, m) , 4.19 (2H, t, J=7.5Hz), 4.86 (IH, br) , 6.55-6.62 (2H, m) , 6.86 (IH, d, J=7Hz), 6.97 (IH, d, J=7Hz) , 7.08 (IH, t, J=7Hz), 7.31 (2H, d, J=8Hz), 7.40-7.53 (3H, m) , 8.13 (IH, d, J=7Hz) , 9.88 (IH, ε) 6) 4-(2-Iodobenzoyl)amino-N-mεthyl-N-[2-[5-(4-methyl- pipεrazin-l-yl)carbonylpent-l-yl]oxy]phenylbenzamidε NMR (CDC1 3 , δ) : 1.43-1.54 (2H, m) , 1.61-1.70 (2H, m) , 1.74-1.86 (2H, m) , 2.28 (3H, s) , 2.28-2.41 (6H, a), 3.34 (3H, 8), 3.44-3.50 (2H, a), 3.52-3.59 (2K, a), 3.73-3.99 (2H, a), 6.77-6.84 (2H, a), 7.03 (IH, d, J=7Hz), 7.10-7.19 (2H, a), 7.29-7.50 (5H, a), 7.80 (IH, s), 7.89 (IH, d, J=7Hz) 7) 4- (2-Dimethylamino-4-methyl)phεnoxymεthyl-N-mεthyl-N-[4- methyl-2-[5-(4-methylpiperazin-l-yl)carbonylpent-1- yl]oxy]phenylbenzamide NMR (CDCI3, δ) : 1.47-1.58 (2H, m) , 1.64-1.75 (2H, m) , 1.77-1.88 (2H, m) , 2.22 (3H, s) , 2.25 (3H, s) , 2.28 (3H, ε), 2.31-2.41 (6H, m) , 2.72 (6H, s) , 3.32 (3H, ε), 3.43-3.51 (2K, m) , 3.58-3.67 (2H, a), 3.79-3.97 (2H, a), 5.02 (2H, s) , 6.49-6.61 (3H, a), 6.71 (IH, d, J=7Hz), 7.80-7.85 (2H, a), 7.19 (2H, d, J=8Hz) , 7.28 (2H, d, J=8Hz) 8) 4- (2-Benzyloxy)benzoylaaino-3-aethoxy-N-aethyl-N-[ (E)-2- [4-(4-aethyloiperazin-l-yl)carbonvl]phenylethen-l- yl]phenylbenzaaide NMR (CDCI3, δ) : 2.11-2.40 (4H, a), 2.17 (3H, s) , 3.11 (3H, s), 3.18-3.38 (2H, a), 3.44 (3H, s) , 3.49-3.68 (2H, a), 5.27 (2H, s) , 6.41 (IH, d, J=14Hz) , 6.56 (IH, d, J=14Hz), 6.70 (2H, d, J=8Hz) , 6.88-7.48 (16H, a), 8.26 (IH, d, J=7Hz) , 8.38 (IH, d, J=7Hz) 9) 3-Methoxy-4-[2-[3-(tert-butoxycarbonylamino)prop-l- yl]oxybenzoyl]amino-N-methyl-N-[4-methyl-2-[5-(4-methyl- piperidin-1-yl)carbonylpent-1-yl]oxy]phenylbenzamide NMR (CDCI3, δ) : 0.93 (3K, d, J=7.5Hz), 0.98-1.14 (2H, ), 1.40 (9H, s), 1.42-1.87 (8H, m) , 2.07-2.17 (2H, m), 2.25 (3H, s) , 2.32 (2H, t, J=7.5Hz), 2.50 (IH, m), 2.97 (IH, ) , 3.21-3.32 (2H, a), 3.32 (IH, s), 3.79 (IH, s), 3.79-4.00 (4K, a), 4.24 (2H, t, J=7.5Hz), 4.55 (IH, a), 4.84 (IH, m) , 6.59 (IH, d, J=7Hz), 6.63 (IH, s) , 6.85 (IH, d, J=7Hz), 6.92 (IH, d, J=7Hz), 6.95-7.13 (3H, a), 7.45 (IK, t, J=7Hz), 8.20 (IH, d, J=7Hz), 8.40 (IH, d, J=7Hz) 10) 3-Methoxy-4-[2-[3- (tert-butoxycarbonylaminc)prop-l- yl]oxybenzoyl]amino-N-[2-[5-[ (2S)-carbamoylpyrrolidin-1- yl]carbonylpεnt-1-yl]oxy-4-mεthyl] henyl-N- methylbenzamide NMR (CDC1 3 , δ) : 1.28-2.20 (12H, m) , 1.39 (9H, s) , 2.27 (3H, s), 3.19-3.25 (2H, a), 3.21 (3H, s) , 3.25-3.61 (2H, a), 3.78 (3H, s) , 3.81-4.03 (2K, a), 4.16-4.29 (2H, a), 4.57 (IH, a), 6.55-6.68 (2H, m) , 6.80-7.13 (5H, m) , 7.44 (IH, t, J=7Hz) , 8.20 (IH, d, J=7Hz), 8.40 (IH, d, J=7Hz) 11) 3-Methoxy-4-[2-[l-(tert-butoxycarbonyl)piperidin-4-yl]- oxybenzoyl]amino-N-methyl-N-[4-methyl-2-[5- (4-methyl- piperazin-1-yl)carbonylpent-1-yl]oxy]phenylbenzamide NMR (CDCI3, δ) : 1.41-1.59 (2H, a), 1.46 (9H, s), 1.69-1.94 (6H, a), 2.00-2.13 (2H, a), 2.26 (3H, s) , 2.29 (3H, s), 2.33-2.41 (8H, a), 2.96-3.17 (2H, a), 3.31 (3K, s), 3.45-3.51 (2H, a), 3.59-3.67 (2H, a), 3.74 (3H, s), 3.80-4.01 (2K, a), 4.68 (IH, a), 6.58-6.63 (2H, a), 6.85 (IH, d, J=7Kz) , 6.90 (IH, d, J=7Hz), 6.99-7.11 (2H, m) , 7.35-7.61 (2H, m) , 8.19 (IH, d, J=7Hz), 8.40 (IH, d, J=7Hz) 12) 3-Methoxy-4-[2-[3- (tert-butoxycarbonyl)amino-1- methylprop-1-yl]oxybenzoyl]amino-N-methyl-N-[4-methyl-2- [5-(4-mεthylpipεrazin-l-yl)carbonylpent-1- yl]oxy]phenylbenzamide NMR (CDCI3, δ) : 1.30 (9H, s), 1.31 (3H, d, J=7.5Hz), 1795 - 172 - 1.45-2.10 (8H, a), 2.27 (3H, s), 2.29 (3H, s), 2.32-2.43 (6H, a), 3.20-3.30 (2H, m) , 3.32 (3H, s), 3.45-3.50 (2H, a), 3.60-3.66 (2H, a), 3.79 (3H, s), 3.82-4.00 (2H, a), 4.72 (IH, a), 6.60 (IH, d, J=7Hz), 6.64 (IH, s), 6.81-6.93 (2H, a), 7.00-7.11 (3H, a), 7.43 (IH, t, J=7Hz), 8.21 (IK, d, J=7Hz), 8.42 (IH, d, J=7Hz) 13) 4-[2-[3-(tert-Butoxycarbonylamino)prop-l-yl]oxybenzoyl]- amino-3-methoxy-N-methyl-N-[2-(5-aminocarbonylpent-l- yl)oxy-4-methylphenyl]benzamide NMR (CDC1 3 , δ) : 1.42 (9H, s), 1.50-1.92 (6H, m) , 2.12-2.26 (2H, a), 2.29 (2H, t, J=5Hz), 2.30 (3H, s), 3.30 (2K, q, J=5Hz), 3.35 (3H, s), 3.77 (3H, s), 3.80-4.02 (2H, a), 4.25 (2H, t, J=5Kz) , 6.61- 6.70 (2H, a), 6.93-7.15 (6H, a), 7.41-7.51 (IH, m), 8.20 (IH, d, J=7Hz), 8.42 (IH, d, J=7Hz) 14) 4-[2-[3-(tert-Butoxycarbonyl)aminoprop-1-yl]oxybenzoyl]- amino-3-methoxy-N-methyl-N-[2-[5-[4-(tert- butoxycarbonyl)piperazin-1-yl]carbonylpεnt-1-yl]oxy-4- methylphenyl]benzamide NMR (CDCl-a, δ) : 1.40 (9H, s) , 1.49 (9H, s) , 1.50-1.90 (6H, m) , 2.12-2.23 (2H, m) , 2.30 (3K, s), 2.39 (2H, t, J=5Hz), 3.30 (2H, q, J=5Hz) , 3.33 (3K, s) , 3.35 3.42 (4K, m) , 3.44 (4H, s), 3.55-3.62 (2H, m) , 3.8 (3H, s), 3.85-4.06 (2H, m) , 4.24 (2H, t, J=5Hz) , 4.93 (IH, br), 6.57-6.66 (2K, a), 6.85-7.13 (6H, a), 7.44-7.52 (IH, a), 8.20 (IH, d, J=7Hz) , 8.41 (IH, d, J=7Hz) 15) 4-[2-[3-(tert-Butoxycarbonyl)aainoprop-1-yl]oxybenzoyl] amino-3-methoxy-N-mεthyl-N-[2-[5-morpholin-4- yl)carbonylpent-l-yl]oxy-4-aethylphenyl]benzamide NMR (CDCI3, δ) : 1.41 (9H, s) , 1.50-1.88 (6H, a). 2.10-2.21 (2H, m), 2.30 (3H, s), 2.36 (2H, t, J=5Hz), 3.30 (2H, q, J=5Hz) , 3.34 (3H, s) , 3.47 (2H, t, J=4Hz), 3.58-3.70 (6H, m) , 3.79 (3H, s) , 3.84-4.03 (2H, ) , 4.25 (2H, t, J=5Hz), 4.89 (IH, br), 6.56-6.68 (2H, m) , 6.84-7.16 (6H, m) , 7.41- 7.51 (2H, m) , 8.20 (IH, d, J=8Hz), 8.41 (IH, d, J=8Hz) 16) 4- [2- [3- (tert-Butoxycarbonyl) aminoprop-1-yl] oxybenzoyl] - amino-3-mεthoxy-N-mεthyl-N- [2- [5- (4-mεthylhomopiperazin- 1-yl) carbonylpent-l-yl]oxy-4-methylphenyl] benzamide NMR (CDC1 3 , δ) : 1.41 (9H, s) , 1.46-1.97 (8K, m) , 2.09-2.21 (2H, m) , 2.29 (3H, s) , 2.32 (2H, t, J=5Hz), 2.33 (3H, s), 2.52-2.66 (4H, m) , 3.30 (2K, q, J=5Hz), 3.33 (3K, s) , 3.50-3.69 (4H, m) , 3.79 (3H, s), 3.84-4.03 (2H, m) , 4.24 (2H, t, J=5Hz) , 4.94 (IH, br), 6.56-6.67 (2H, m) , 6.82-7.12 (6H, m) , 7.40-7.49 (IH, m) , 8.20 (IH, d, J=7Hz) , 8.41 (IH, d, J=8Hz) 17) 4- [2- (3-tert-Butoxycarbonylaminoprop-l-yl) oxybenzoyl] - amino-3-methoxy-N-methyl-N- [2- [5- (2-dimethylaminoeth-l- yl ) aminocarbonylpent-1-yl ] oxy- 4 -me thylphenyl ] benzamidε NMR (CDCI3, δ) : 1.40 (9K, s) , 1.42-1.59 (4E, a), 1.67-1.90 (4H, a), 1.97-2.32 (4H, a), 2.28 (3H, s), 2.34 (6H, s), 2.56 (2H, br) , 3.25-3.42 (4H, m) , 3.32 (2H, ε), 3.50 (IH, s) , 3.78-4.01 (2H, m) , 3.8C (3H, ε), 4.25 (2H, t, J=6Kz) , 4.91 (IH, br) , 6.52- 6.76 (3H, ) , 6.87-7.13 (7K, a), 7.45 (IH, a), 8.19 (IH, d, J=8Hz), 8.41 (IH, br) 18) 4-[2- (3-tεrt-Butoxycarbonylaainoprop-l-yl)oxybenzoyl]- aaino-3-aethoxy-N-aεthyi-N-[2-[5-[N- (3-dimethylamino- prop-1-yl)-N-mεthylcarbamoylpεnt-l-yl]oxy-4- aεthylphenyl]bεnzaaide 41795 - 174 - NMR (CDCI3, δ) : 1.41 (9H, s) , 1.50-1.96 (6H, m) , 2.11-2.25 (2H, a), 2.27 (3H, s), 2.30-2.43 (2H, m) , 2.50 (6K, s), 2.91 and 3.02 (total 3H, s, rotamer) , 3.08 and 3.32 (total 2H, q, rotamer, J=5Kz) , 3.33 (3H, s), 3.43 (2H, t, J=5Hz) , 3.79 (3H, s) , 3.83- 4.02 (2K, a), 4.25 (2H, t, J=5Hz), 6.57-6.68 (2H, a), 6.82-7.13 (6H, m) , 7.42-7.50 (IH, m) , 8.21 (IH, d, J-8HZ), 8.41 (IH, d, J=8Kz) 19) 4-[2-(3-tert-Butoxycarbonylaminoprop-l-yl)oxybenzoyl]- amino-3-methoxy-N-methyl-N-[2-[5-[bis(2-hydroxyeth-l- yl)amino]carbonylpent-1-yl]oxy-4-methylphεnyl]benzamide NMR (CDCI3, δ) : 1.40 (9H, s), 1.55-1.89 (6H, m) , 2.11-2.20 (2H, m), 2.28 (3H, s), 2.40-2.56 (2H, m) , 3.29 (2H, t, J=5Hz), 3.40-3.57 (4H, a), 3.68-4.02 (6H, E), 4.26 (2K, t, J=5Hz), 6.60-6.68 (2H, m) , 6.90-7.15 (6H, a), 7.42-7.51 (IH, m) , 8.19 (IH, d, J=8HZ), 8.40 (IK, d, J=8Hz) 20) 4-[2-(3-tert-Butoxycarbonylaminoprop-l-yl)oxybenzoyl]- amino-3-methoxy-N-methyl-N-[2-[5-(2,2-dimεthyl- hydrazino)carbonylpent-l-yl]oxy-4-methylphenyl]bεnzamide NMR (DMSO-d 6 , δ) : 1.40 (9H, s) , 1.45-1.90 (6H, m) , 2.08-2.20 (2H, a), 2.28 (3K, s) , 2.30-2.45 (2H, a), 2.51 (3H, S), 2.60 (3H, s) , 3.29 (2H, t, J=5Hz) , 3.33 (3H, s), 3.75 (3H, s) , 3.79-4.02 (2H, a), 4.25 (2H, t, J=5Hz), 6.57-6.68 (2H, a), 6.80-7.14 (5H, a), 7.41-7.50 (IK, a), 8.21 (IH, d, J=8Hz) , 8.40- 8.48 (IH, br) 21) 4-[2-(3-tert-Butoxycarbonylaainoprop-l-yl)oxybenzoyl]- aaino-3-aethoxy-N-aethyl-N-[2-[5-(carbamoylmethylamino) carbonylpent-l-yl]oxy-4-methylphenyl]benzamide NMR (CDCI3, δ) : 1.41 (9H, s) , 1.50-1.90 (6H, m) , 2.12-2.19 (2H, m), 2.28 (3H, s) , 2.53 (2H, t. J=5Hz) , 3.30 (2H, t, J=5Hz) , 3.33 (3H, s) , 3 . 80 (3H, s) , 3 . 84-3 .99 (2H, a) , 4 .05 (2H, br) , 4 .25 (2H, t, J=5Hz ) , 4 . 84 (IH, br) , 6.58-6. 67 (2H, a) , 6.72-7.12 ( 6H, a) , 7. 42-7.50 (IH, a) , 8 .18-8.23 (IH, a) , 8 .41 (IH, d, J=8Hz) 22) 4-[2-(3-tert-Butoxycarbonylaainoprop-l-yl)oxybenzoyl]- aaino-3-aethoxy-N-aethyl-N-[2-[5-(carbamoylethylamino)- carbonylpent-1-yl]oxy-4-mεthylphenyl]benzamide NMR (CDC1 3 , δ) : 1.41 (9H, s), 1.46-1.86 (6H, m) , 2.12-2.25 (4H, m) , 2.30 (3K, s) , 2.41 (2H, t, J=5Hz), 3.30 (IH, q, J=5Hz) , 3.37 (3H, s) , 3.49 (IH, q, J=5Kz), 3.79 (3K, s) , 3.82-4.03 (2K, a), 4.27 (2H, t, J=5Hz), 6.45-6.67 (4H, a), 6.88-7.15 (6H, a), 7.43-7.51 (IH, a), 8.20 (IH, d, J=8Hz), 8.41 (IH, d, J=8Hz) 23) 4-[2- (3-tert-Butoxycarbonylaminoprop-l-yl)oxybenzoyl]- amino-3-methoxy-N-methyl-N-[2-[5-(4-diethylamino- piperidin-1-yl)carbonylpent-l-yl]oxy-4-mεthylphεnyl]- benzamide NMR (CDCi 3 , δ) : 1.12 (6K, t, J=5Kz) , 1.41 (9K, s) , 1.42-1.92 (6H, m) , 2.10-2.18 (2H, a), 2.27 (3H, s), 2.27-2.69 (9H, a), 3.26 (2H, t, J=5Hz) , 3.31 (3H, s), 3.77 (3H, s) , 3.87-4.02 (4H, a), 4.23 (2H, t, J=5Hz), 6.54-6.67 (2K, a), 6.72-7.15 (6H, a), 7.42- 7.51 (IH, a), 8.19 (IH, d, J=8Hz) , 8.42 (IH, d, J=8Hz) 24) 4-[2-[3- (tert-Butoxycarbonylamino)prop-l-yl]oxybenzoyl]- amino-3-mεthoxy-N-[2-[3- (4-mεthylpiperazin-l- yl)carbonylpyrid-6-yl]methoxy-4-methylphenyl]-N- methylbenzamidε NMR (CDCI3, δ) : 1.39 (9H, s), 2.06-2.18 (2H, m) , 2.28 (3H, s), 2.31 (3H, s) , 2.35-2.51 (4H, m) , 3.27 (2H, /41795 - 176 - q, J=5HZ), 3.38-3.49 (2H, m) , 3.41 (IH, s), 3.63 (3H, s), 3.68-3.76 (2H, m) , 4.21 (2H, t, J=5Hz) , 4.97 (IH, d, J=12Hz), 5.14 (IH, d, J=12Hz) , 6.58 (IK, ε), 6.72 (IK, d, J=8Hz), 6.91-7.11 (7H, m) , 7.20-7.25 (IH, a), 7.43 (IK, dd, J=2, 8Hz), 7.68 (IH, d, J=8Hz), 8.19 (IK, d, J=8Hz), 8.40 (IH, d, J=8Hz), 8.60 (IH, s) 25) 4-[2-(Benzyloxy)benzoyl]amino-3-methoxy-N-methyl-N-[2- [5-(4-dimethylaminopipεridin-l-yl)carbonylpεnt-1-yloxy]- phεnyl]benzamide NMR (CDC1 3 , δ) : 1.30-1.42 (2H, m) , 1.48-1.58 (2H, a), 1.63-1.93 (6H, a), 2.29 (6H, s) , 2.30-2.40 (3H, a), 2.50-2.60 (IH, a), 2.95-3.06 (IH, a), 3.29 (3H, ε), 3.38 (3H, 8), 3.80-4.00 (4H, a), 4.57-4.70 (IH, a), 5.30 (2H, s), 6.74-7.20 (9H, a), 7.32-7.45 (5H, a), 8.20-8.37 (IH, a), 8.37-8.42 (IH, a) 26) 4-[ (2-Benzyloxy)benzoyl] amino-N-methyl-N- [2- [3- (4- methylpiperazin-1-yl) carbonylprop-l-yl]oxy] - phenybenzamide NMR (CDCI3, δ) : 2.05-2.16 (2H, m) , 2.28 (3H, s) , 2.32-2.40 (4H, m) , 2.50 (2H, t, J=7.5Hz), 3.33 (3H, ε), 3.43-3.50 (2H, a), 3.59-3.65 (2H, a), 3.88-4.05 (2H, a), 5.19 (2H, s) , 6.77-6.84 (2H, m) , 6.95-7.02 (3H, m), 7.09-7.20 (5H, a), 7.39-7.52 (6H, a), 8.27 (IH, d, J=7Hz) Example 21 The following coapoundε were obtained according to siailar aanners to those of Exaaoles 8 and 16. 1) 4-(6-Hydroxy-2-pyridylcarbonyl)aaino-N-aεthyl-N-[4- aethyl-2-[5-(4-aethylpiperazin-l-yl)carbonylpεnt-1- yloxy]phεnvl]bεnzaaidε dihvdrochloridε NMR (CDCI3, δ) : 1.47-1.58 (2H, m) , 1.64-1.73 (2H, m) , 1.78-1.87 (2H, m) , 2.27 (3H, s), 2.29 (3H, s), 2.28-2.41 (8H, m) , 3.33 (3H, s) , 3.45-3.51 (2H, a), 3.59-3.68 (6H, a), 3.86-3.94 (IH, br) , 6.55-6.61 (2H, a), 6.86 (IH, d, J=8Hz), 7.30-7.38 (4H, a), 7.47-7.54 (2K, a), 8.06-8.10 (IH, a) ESI-MASS (a/z) : 574 (M+H) 2) 4-[2- (Methoxy)benzoyl]amino-N-methyl-N-[4-methyl-2-[5- (4-methylpiperazin-l-yl)carbonylpent-1-yloxy]phenyl]- benzamidε hydrochloride NMR (DMSO-dg, δ) : 1.36-1.66 (4H, m) , 1.66-1.83 (2H, m), 2.23 (3H, s), 2.39 (2H, t, J=7Hz) , 2.74 (3H, s), 2.80-3.10 (3H, a), 3.17 (3H, s), 3.23-3.53 (3H, a), 3.86 (3H, s), 3.79-3.99 (2H, a), 4.00-4.17 (IH, a), 4.37-4.52 (IH, a), 6.64 (IH, d, J=9Hz) , 6.79 (IH, s), 6.98-7.09 (2H, a), 7.11-7.28 (3H, a), 7.43-7.64 (4H, a) Example 22 To a solution of 4-amino-3-mεthoxy-N-methyl-N-[4-methyl- 2-[5-(4-methylpipεrazin-l-yl)carbonylpent-1-yloxy]phεnyl]- benzamide (327 mg) and pyridine (80.3 mg) in dichloromethane (6 ml) was added dropwisε 2-nitrobεnzεnεsulfonyl chloridε (150 mg) at ambiεnt tεmpεrature and the mixture was stirred at ambient temperature for 5 hours. The resulting mixture was dilutεd with dichloromethane (10 ml) and the organic layer waε washed successively with saturated sodium bicarbonate aqueous solution and brine. Drying, filtering and rεmoval of solvεnts affordεd a crude product. Thε crude product was chromatographed on silica gel (εluent; 2-4% methanol in chloroform) to give 4-(2-nitrobenzenesulfonyl)- amino-3-mεthoxy-N-mεthyl-N-[4-methyl-2-[5-(4-methylpipεrazin- 1-yl)carbonylpent-1-yloxy]phenyl]benzamide (460 mg) . NMR (CDCI3, δ) : 1.47-1.82 (6H, a), 2.28 (3H, s) , 2.31 (3H, s), 2.35-2.42 (6H, a), 3.30 (3H, s), 3.46-3.53 (5H, a), 3.60-3.68 (4H, a), 6.56-6.96 (6H, a), 7.53-7.88 (4H, a) Example 23 A solution of 4-[2-[2-[3-(phthaliaido)prop-1- yl]oxy]phenyl]vinyl-3-methoxybεnzoic acid (370 mg) in tetrahydrofuran (20 ml) was treated at ambient temperature with triethylamine (246 mg) , N-methyl-4-mεthyl-2-[5-(4- methylpiperazin-1-yl)carbonylpεnt-1-yloxy]aniline (297 mg) , and diphenyl phosphorochloridate (326 mg) . The reaction mixture was stirred at 80 β C for 18 hours. After concentration, the residue was disεolved in chloroform and washed with brine and dried over magnesium sulfate. The crude product was purified by εilica gεl column chromatography (Si0 2 30 g, 3% methanol in chloroform) to givε 4-[2-[2-[ (3-(phthalimido)prop-l-yl)oxy]phenyl]vinyl]-3- methoxy-N-methyl-N-[4-methyl-2-[5-(4-methylpipεrazin-l- yl)carbonylpεnt-1-yloxy]phεnyl]benzamide (550 mg) . NMR (CDC1 3 , δ) : 1.47-1.95 (8H, m) , 2.18-2.44 (12H, a), 3.31 and 3.34 (total 3H, s) , 3.42-3.52 (2H, a), 3.57-3.72 (5H, a), 3.82-4.16 (6K, a), 6.30-7.80 (16H, a) Example 24 The following compounds were obtained according to a similar manner to that of Example 23. 1) 4-[N-Methyl-2-[ (3-tert-butoxycarbonylaminoprop-l-yl)- oxy]benzoyl]amino-3-methoxy-N-methyl-N-[4-methyl-2-[5- (4-mεthylpipεrazin-l-yl)carbonylpent-1-yloxy]phenyl]- benzamide NMR (CDCI3, δ) : 1.40-1.75 (8H, m) , 1.44 (9K, s) , 1.89-1.97 (2H, a), 2.29 (6K, s) , 2.32-2.42 (6H, a) 3.24 (6H, s), 3.26-3.34 (2H, a), 3.44-3.67 (6H, a) 3.77-3.88 (3H, m) , 6.48-6.82 (9H, m) , 6.90-6.96 (IK, m), 7.06-7.13 (IH, m) ESI-MASS (m/z) : 774 (M+H) 2) 4-[2- [ (3-tert-Butoxycarbonylaminoprop-l-yl)oxy]benzoyl]- amino-3-methoxy-N-methyl-N- (4-benzyloxyphenyl)benzamide NMR (CDC1 3 , δ) : 1.42 (9H, s) , 2.09-2.20 (2K, m) , 3.28-3.37 (2H, m) , 3.48 (3H, s) , 3.81 (3H, s) , 4.22-4.33 (2H, m) , 4.70-4.78 (IH, br), 5.00 (2H, s), 6.82-6.88 (3K, m) , 6.97-7.13 (6H, m) , 7.31-7.48 (6H, m), 8.23 (IH, d, J=8Hz), 8.44 (IH, d, J=8Hz) ESI-MASS (m/z) : 640 (M+H) 3) 4-[2-[ (3-tert-Butoxycarbonylaminoprop-l-yl)oxy]benzoyl]- amino-3-benzyloxy-N-mεthyl-N-cyclohexylbenzamide NMR (CDCI3, δ) : 1.01-1.12 (2H, br) , 1.40 (9H, s) , 1.45-1.82 (10H, m) , 2.81-3.07 (5H, m) , 3.80-3.89 (2H, m), 4.40-4.49 (IH, m) , 5.18 (2H, ε), 6.94 (IH, d, J=8Hz), 7.02 (IH, d, J=8Hz), 7.07-7.15 (2H, m) , 7.35-7.48 (6H, a), 8.27 (IH, d, J=8Hz) 8.68 (IH, d, J=8Hz) ESI-MASS (m/z) : 616 (M+H) 4) 4- [ (2-Bεnzyloxy)bεnzoyl] amino-3-chloro-N-mεthyl-N- [2- [5- (4-dimεthylaminopipεridin-l-yl) carbonylpεnt-1-yloxy]-4- methylphenyl]benzamide NMR (CDCI3, δ) : 1.30-1.45 (2H, a), 1.45-1.57 (2H, a), 1.62-1.93 (6H, a), 2.22-2.40 (12H, a), 2.50-2.63 (IK, a), 2.95-3.08 (IH, m) , 3.31 (3H, s), 3.80-4.00 (4H, m), 4.58-4.70 (IH, m) , 5.37 (2H, ε), 6.56-6.62 (2H, m), 6.83-6.88 (IH, a), 7.02-7.13 (3K, a), 7.36-7.47 (7H, a), 8.27 (IH, d, J=7Hz) , 8.42 (IH, d, J=7Hz) 5) 4- [N- [2- [ (3-tert-Butoxycarbonylaainoprop-l- yl)oxy]phenyl]-tert-butoxycarbonylamino]methyl-3- mεthoxy-N-mεthyl-N-[2-[5-(4-methylpiperazin-l- yl)carbonylpεnt-1-yloxy]-4-methylphenyl]benzamide NMR (CDC1 3 , δ) : 1.30 and 1.33 (total 9H, s), 1.43 (9H, s), 1.49-1.60 (2H, a), 1.62-1.98 (6H, m) , 2.28 (3H, s), 2.30 (3H, s), 2.32-2.42 (6H, a), 3.20-3.29 (2H, a), 3.32 (3H, s) , 3.39 (IH, s) , 3.46-3.55 (4H, a), 3.62 (2K, br) , 3.82 (IK, br) , 3.88-4.03 (3H, a), 6.50-6.60 (2H, a), 6.65-7.00 (6H, a), 7.06-7.22 (2H, a) 6) 4-[2-[ (3-tert-Butoxycarbonylaainoprop-l-yl)oxy]phenoxy] aethyi-3-aethoxy-N-aethyl-N-[2-[5-(4-aethylpiperazin-l- yl)carbonylpent-1-yloxyj-4-methylphεnyl]bεnzamidε NMR (CDCI3, δ) : 1.37 (9H, s) , 1.47-1.57 (2H, m) , 1.66-1.73 (2H, a), 1.73-1.88 (2H, a), 1.93-2.02 (2K, a), 2.28 (3H, s), 2.30 (3H, s) , 2.32-2.40 (6H, a), 3.32 (3K, a), 3.25-3.38 (2H, a), 3.47-3.50 (2H a), 3.62-3.67 (2H, a), 3.70 (3H, s), 3.80-3.88 (IK a), 3.90-3.98 (2H, a), 4.07-4.17 (2K, a), 5.10 (2H S), 5.50 (IH, br), 6.53-6.60 (2H, a), 6.70-6.90 (7H, a), 7.15-7.20 (IH, a) 7) 3-Benzyloxy-4-[2-[ (3-tert-butoxycarbonylaainoprop-l- yl)oxy]bεnzoyl]amino-N-methyl-N-[2-[5-(4-methyl- pipεrazin-1-yl)carbonylpεnt-1-yloxy]-4-methylphenyl]- benzamide NMR (CDCI3, δ) : 1.40 (9H, s) , 1.45-1.85 (10H, a), 2.28 (3H, s), 2.29 (3H, s) , 2.32-2.39 (6H, a), 2.90-2.98 (2H, a), 3.30 (3H, s) , 3.47-3.49 (2H, a) 3.60-3.63 (2K, a), 3.77-3.98 (4H, a), 4.97 (2H, s) 6.56-6.60 (2H, a), 6.80 (IK, d, J=7Hz) , 6.89-6.97 (2H, a), 7.04-7.12 (2H, a), 7.33-7.45 (6H, a), 8.1 (IH, d, J=6Hz), 8.41 (IH, d, J=7Hz) 8) 2-[2-[ (3-tert-Butoxycarbonylaminoprop-l-yl) oxy] benzoyl ]- amino-N-mεthyl-N- [2- [5- (4-methylpiperazin-l- yl ) carbonylpent-1-yloxy] -4-me thylphεnyl] -5- thiophεnεcarboxamidε NMR (CDC1 3 , δ) : 1.37 (9H, s) , 1.48-1.62 (2H, m) , 1.62-1.76 (6H, m) , 1.97-2.11 (2H, m) , 2.17-2.38 (9H, m), 2.39 (3H, s), 3.31 (3H, s), 3.33-3.65 (6H, a), 3.87 (IH, br) , 3.94 (IH, br) , 4.02 (IK, s) , 4.13-4.20 (2K, a), 6.40-6.57 (2H, a), 6.74-6.82 (2K, a), 6.92-7.14 (3H, a), 7.40-7.52 (IK, a), 8.10-8.27 (IH, a) Example 25 A solution of (S)-4-[2-[l-methyl-3- (phthalimido)prop-1- yl]oxybenzoyl]aaino-3-aethoxy-N-aethyl-N-[4-aethyl-2-[5-(4- aεthylpipεrazin-1-yl)carbonylpεnt-l-yloxy]phεnyl]bεnzaaidε (1.1 g) in methanol (30 ml) was stirred and treated with 40% methylaminε in methanol (10 ml) . The reaction mixture was refluxed for 30 minutes. Then the solvent was concentrated and purified by εilica gel column chromatography (Si0 2 40 g, chloroform/methanol/ammonia = 90/10/0.5) to give (S)-4-[2- [ (3-amino-l-mεthylprop-l-yl)oxy]bεnzoyl]amino-3-mεthoxy-N- mεthyl-N-[4-mεthyl-2-[5-(4-methylpiperazin-l-yl)- carbonylpent-1-yloxy]phεnyl]benzamide. NMR (CDCI3, δ) : 1.42 (3H, d, J=7Hz) , i.46-1.92 (9H, a), 1.98-2.16 (IH, a), 2.20-2.45 (12H, a), 2.86 (2H, t, J=7Hz), 3.32 (3H, ε), 3.42-3.53 (2H, m) , 3.57-3.67 (2H, m) ' , 3.79 (3H, s) , 3.82-4.03 (2H, m) , 4.73-4.90 (IH, m) , 6.51-6.68 (2H, m) , 6.79-6.95 (2H, a), 6.98-7.12 (3H, a), 7.37-7.49 (IH, a), 8.21 (IH, d, J=8Hz), 8.41 (IH, d, J=8Hz) Example 26 A solution of 4-[2-[ (3-tert-butoxycarbonylaainoprop-l- yl)oxy]benzoyl]amino-3-methoxy-N-mεthyl-N-[2- (5-carboxypent- 1-yloxy)-4-methylphenyl]benzamide (3.5 g) in ethyl acetate (30 ml) was treated at ambient temperature with triethylamine (575 mg), N-methylpiperazine (569 mg) , and diphenylphosphoryl azide (1.56 g) . The reaction mixture was stirred at the same tεmpεraturε for 17 hours. Thε reaction mixture was washed with brine and dried over magnesium sulfate. The crude product was purified by silica gel column chromatography (Si0 2 100 g, 3% methanol in chloroform) to give 4-[2-[(3- tεrt-butoxycarbonylaminoprop-1-yl)oxy]benzoyl]amino-3- methoxy-N-methyl-N-[4-methyl-2-[5-(4-methylpipεrazin-l- yl)carbonylpent-1-yloxy]phenyl]benzamidε (2.93 g) . NMR (CDC1 3 , δ) : 1.40 (9H, s) , 1.42-1.60 (2H, m) , 1.62-1.90 (4H, m), 2.06-2.20 (2H, m) , 2.22-2.42 (12H, m), 3.21-3.36 (5H, m) , 3.42-3.51 (2H, m) , 3.56-3.67 (2H, m) , 3.77 (3H, s) , 3.81-4.02 (2H, m) , 4.23 (2H, t, J=7Hz), 4.86 (IH, m) , 6.51-6.67 (2H, a), 6.79-6.93 (2H, a), 6.94-7.13 (3H, a), 7.44 (IH, a), 8.20 (IH, d, J=8Hz), 8.41 (IH, d, J=8Hz) Example 27 Thε following coapound was obtained according to a siailar manner to that of Example 26. 4-[2-[ (3-tert-Butoxycarbonylaminoprop-l-yl)oxy]benzoyl]- amino-3-methoxy-N-mεthyl-N-[2-[5-(4-dimεthylaminopipεridin-l yl)carbonylpεnt-1-yloxy]-4-methylphenyl]benzamide NMR (CDCI3, δ) : 1.41 (9H, s), 1.46-1.95 (8H, a), 2.06-2.42 (16H, a " ), 2.56 (IH, a), 3.00 (IH, a), 3.22-3.38 (5H, a), 3.79 (3H, s) , 3.83-4.03 (3H, a) 4.25 (2H, t, J=7Hz), 4.61 (IH, a), 4.87 (IH, a), 6.52-6.68 (2H, a), 6.79-6.95 (2K, a), 6.96-7.17 (3H, m), 7.46 (IH, m) , 8.21 (IH, d, J=8Hz), 8.41 (IK, d, J=8Hz) Example 28 To a solution of 4-[2-(3-tert-butoxycarbonylaminoprop-l yl)oxybenzoyl]amino-3-methoxy-N-methyl-N-[2-(5-carboxypent-i yl)oxy-4-methylphenyl]benzamide (300 mg) and N- methylmorpholine (45 mg) , in N,N-dimεthylformamidε (5 ml) wa addεd isobutyl chloroformatε (61 mg) at -15 β C and thε solution was stirrεd at the same temperature for 5 minutes. N,N,N'-Trimethylethylenεdiamine (54 mg) was added to thε solution and thε mixturε was stirrεd at -15 β C for 30 minutεs and thεn at ambient temperature for 1 hour. The mixture was diluted with ethyl acetatε (20 ml) and thε solution was washed successively with aqueous sodium hydrogen carbonate εolution, water (15 ml x 3) and brinε. Thε solution was driεd over potasεium carbonate and the solvent was removεd undεr rεducεd prεssurε. Thε rεεidue was purified on silica gel column chromatography (Si0 2 40 g, 1-5% methanol in chloroform) to give 4-[2- (3-tert-butoxycarbonylaminoprop-l- yl)oxybenzoyl]amino-3-methoxy-N-methyl-N-[2-[5-[ (2- dimethylaminoeth-1-yl)-N-methylaminocarbonyl]pent-l-yl]oxy-4 methylphenyl]bεnzamidε (312 mg) . NMR (CDC1 3 , δ) : 1.40 (9H, s) , 1.44-2.21 (8H, m) , 2.25 (3H, s), 2.27 (6H, s), 2.29-2.50 (4H, a), 2.91 (IH s), 3.00 (2H, s), 3.26-3.51 (4H, m) , 3.31 (3H, s) , 3.77 (3H, s), 3.81-4.02 (2H, m) , 4.22 (2H, t, J=5Hz), 4.88 (IH, br), 6.52-6.68 (2H, m) , 6.79-7.1 (5H, m) , 7.43 (IH, m) , 8.20 (IH, d, J=9Hz) , 8.40 (IH, d, J=8Hz) Example 29 The following compounds were obtainεd according to a similar mannεr to that of Examplε 28. 1) 4-[2-(3-tεrt-Butoxycarbonylaminoprop-l-yl)oxybεnzoyl]- amino-3-methoxy-N-methyl-N-[2-[5- (3-dimethylaminoprop-l yl)aminocarbonylpent-l-yl]oxy-4-methylphenyl]bεnzamide NMR (CDC1 3 / δ) : 1.40 (9H, s) , 1.42-1.57 (2H, a). 5 - 184 - 1.61-1.85 (6H, m), 2.04-2.35 (8H, ) , 2.25 (3H, s) 2.29 (9H, s), 2.46 (2H, t, J=6Hz), 3.20-3.38 (4H, m), 3.30 (3H, s), 3.76 (3K, s) , 3.80-4.00 (2H, m) , 4.24 (2K, t, J=5Hz), 4.90 (IH, br) , 6.61-6.72 (2H, a), 6.84-7.12 (6H, a), 7.43 (IH, d, J=8Hz), 8.20 (IH, d, J=8Hz), 8.41 (IH, d, J=8Hz) 2) 4-[2-(3-tert-Butoxycarbonylaminoprop-l-yl)oxybenzoyl]- amino-3-methoxy-N-methyl-N-[2-[5-(4-oxopiperidin-l- yl)carbor.ylpent-l-yl]oxy-4-methylphenyl]benzamide NMR (CDC1 3 , δ) : 1.40 (9H, s) , 1.50-1.92 (8H, a), 2.1 (2H, t, J=6Hz), 2.29 (2H, t, J=5Hz) , 2.38-2.51 (6 a), 3.30 (2H, t, J=5Hz), 3.32 (3H, s), 3.70-4.05 (6H, a), 3.80 (3H, s), 4.25 (2H, t, J=5Hz), 4.85 (IH, br), 6.55-6.67 (2H, a), 6.83-7.15 (6H, a), 7.40-7.51 (IH, a), 8.20 (IH, d, J=8Hz) , 8.40 (IH, br) 3) 4-[2-(3-tert-Butoxycarbonylaminoprop-l-yl)oxybenzoyl]- amino-3-aethoxy-N-methyl-N-[2-[5-(4-pyridylamino- carbonyl)pe t-1-yl]oxy- -methylphenyl]benzamidε NMR (CDCI3, δ) : 1.40 (9H, s) , 1.50-1.61 (2H, a), 1.75-1.93 (4H, a), 2.09-2.20 (2H, a), 2.30 (3H, s 2.42 (2H, br), 3.30 (IH, q, J=5Hz) , 3.36 (3H, s), 3.70 (3H, s), 3.72-4.00 (2H, a), 4.25 (2H, t, J=5Hz), 4.90 (IH, br), 6.60 (IH, br) , 6.72 (IH, J=8Hz), 6.99-7.12 (6H, a), 7.43-7.51 (IH, a), 7. (IK, d, J=8Hz), 8 ' .19 (IH, d, J=8Hz) , 8.42 (IH, d, J=7Hz), 8.46 (IK, br), 9.22 (IH, br) Example 30 To a εolution of 4-[2-(3-tert-butoxycarbonylaainoprop yl)oxybenzoyl]aaino-3-aethoxy-N-aethyl-N-[2-(5-carboxypent yl)oxy-4-methylphenyl]benzamide (250 mg) and N- methylmorpholine (37 mg) in dichloromethane (5 ml) was add pivaloyl chloride (45 mg) at -15°C. After being stirred at the same temperature for 5 minutes, to the mixture was adde l-amino-4-methylpiperazine (47 mg) and the mixture was εtirred at -15 β C for 1 hour and then εtirred at ambient tempεrature for additional 2 hourε. The reεulting mixture was poured into saturatεd aqueous sodium hydrogen carbonate solution (20 ml) and the solution was extracted with chloroform (15 ml x 3) . The organic layer was washed with brinε and dried over magnesium suifatε. The solvent was evaporated and the residue was purified on silica gεl column chromatography (Si0 30 g, 1-15% mεthanol in chloroform) to give 4-[2- (3-tert-butoxycarbonylaminoprop-l-yl)oxybenzoyl]- amino-3-methoxy-N-methyl-N-[2-[5-(4-mεthylpipεrazin-l- yl)aminocarbonylpent-1-yl]oxy-4-mεthylphenyl]benzamidε (208 mg) . NMR (CDC1 3 , δ) : 1.40 (9H, s), 1.45-1.90 (6H, m) , 2.10-2.19 (2K, a), 2.24 (3H, s), 2.25 (3H, s), 2.5 (2H f t, J=5Hz), 2.54-2.91 (8H, a), 3.30 (2H, t, J«5Hz), 3.34 (3H, s) , 3.75 (3H, s) , 3.80-4.03 (2H, a), 4.24 (2H, t, J=5Hz) , 4.78-4.97 (IH, br) , 6.53- 6.67 (2H, a), 6.73-7.14 (6H, a), 7.40-7.50 (IH, m) 8.21 (IH, d, J=8Hz), 8.45 (IK, d, J=8Hz) Example 31 Thε following compounds wεre obtained according to a similar manner to that of Example 9. 1) 4-[2-(E) -[2-(4-Methylpiperazin-l-yl)carbonylethen-1- yl]bεnzoyl]amino-3-mεthoxy-N-mεthyl-N-[4-methyl-2-[5-(4 methylpipεrazin-l-yl)carbonylpεnt-l-yl]oxy]- phεnylbenzamide NMR (CDCl --,_», δ) : 1.48-1.59 (2H, a), 1.67-1.76 (2H, a), 1.79-1.87 (2H, a), 2.21 (3H, ε) , 2.26 (3H, s) , 2.3 (3H, ε), 2.31-2.44 (10H, a), 3.17-3.25 (2K, a), 3.34 (3H, s) , 3.47-3.52 (2H, a), 3.56-3.67 (3H, a) 95 - 186 - 3.62 (3H, s), 3.82-3.99 (3H, a), 5.71 (IH, m) , 6.60-6.67 (2H, a), 6.86 (IH, d, J=7Hz), 6.92 (IH, d, J=7Hz), 6.98-7.03 (2H, a), 7.14 (IH, d, J=7Hz) 7.43-7.62 (4H, a), 7.85 (IH, d, J=7Hz) 2) 4-[2-f (4-Methylpipεrazin-l-yl)carbonylmethoxy]benzoyl] amino-3-mεthoxy-N-[2-[5-(4-methylpiperazin-l- yl)carbonylpent-l-yl]oxy-4-methylphenyl]benzamide NMR (CDC1 3 , δ) : 1.30-1.90 (6H, a), 2.14 (3H, s) , 2.2 (3H, s), 2.35-2.46 (3H, a), 3.34 (3H, s) , 3.46-3. (4H, a), 3.59-3.68 (4H, a), 3.72 (3K, s), 3.80-4. (2H, a), 4.90 (2H, s) , 6.58-6.68 (2H, a), 6.82-7. (4H, a), 7.13-7.20 (2K, a), 7.46-7.51 (IH, a), 8. (IH, d, J=8Hz), 8.39 (IH, d, J=8Hz) Example 32 A solution of 4-(2-iodobεnzoyl)amino-N-[2-(4- mεthoxyphεnyDmεthoxy]phenyl-N-methylbenzamide (2.30 g) in mixture of dichloromethane (30 ml) and trifluoroacetic acid (15 ml) was stirred at ambient tempεrature for 2 hours and the solvent was evaporated in vacuo. The residual oil was disεolved in chloroform (50 ail) and the solution was washe succeεsively with water (50 ml) , aqueous sodium hydrogen carbonate (50 ml) and brine (25 ml) . The solution was dri over magnesium sulfatε and the solvent was evaporated in vacuo to give 4-(2-iodobenzoyl)amino-N-(2-hydroxy)phεnyl-N mεthylbεnzamidε (1.20 g) . NMR (DMSO-dg, δ) : 3.20 (3K, s) , 6.69 (IH, t, J=7Hz) 6.82 (IH, d, J=7Hz), 6.98-7.05 (3H, m) , 7.40-7.5 (4H, m), 7.90 (IH, d, J=7Hz) , 9.84 (IH, ε) Example 33 The following compoundε werε obtained according to a similar manner to that of Example 32. 1) 4- (2-Hydroxybεnzoyl)amino-N-mεthyl-N-[4-mεthyl-2-[4-(4 methylpiperazin-1-yl)carbonyl]phenylmethoxy]- phenylbenzamide NMR (CDC1 3 , δ) : 2.28 (3H, s), 2.32 (3H, s) , 2.35-2.5 (4H, a), 3.36 (3H, s) , 3.59-3.89 (2H, a), 5.02 (2 s), 6.63-6.72 (2H, a), 6.88 (IH, t, J=7Hz), 7.00 (2H, d, J=8Hz), 7.20-7.46 (9H, a), 7.70 (IH, d, J=7Hz), 8.68 (IH, ε) 2) 3-Methoxy-4- (2-hydroxybenzoyl) amino-N-methyl-N- [4- methyl-2- [4- (4-mεthylpipεrazin-l-yl) carbonyl] - phenylmethoxy] phenylbεnzamidε NMR (CDCI3, δ) : 2.23 (3H, ε), "2.30 (3H, s) , 2.33-2.51 (4H, a), 3.37 (3H, s) , 3.41-3.56 (2H, a), 3.68 (3H ε), 3.72-3.87 (2H, a), 4.91 (IH, d, J=14Hz), 5.09 (IH, d, J=14Hz), 6.63-6.71 (2H, a), 6.35-6.93 (2H, a), 7.00 (2H, d, J=8Hz), 7.33-7.50 (7H, a), 8.14 (IH, d, J=7Hz), 8.72 (IH, s) 3) 4 [2- (3-Hydroxyprop-l-yl)thiobεnzoyl]aaino-3-aethoxy-N- aεthyl-N-[4-aethyl-2-[5- (4-aethylpiperazin-l-yl)- carbonylpεnt-1-yl]oxy]phεnylbεnzaaidε NMR (CDCI3, δ) : 1.44-1.58 (2H, a), 1.61-1.73 (2H, a), 1.77-1.89 (2H, a), 2.28 (3H, ε) , 2.31-2.40 (6H, a) 3.02 (2H, t, J=7.5Kz), 3.31 (3H, s) , 3.42-3.50 (2H a), 3.56-3.65 (2K, a), 3.67-3.78 (7K, a), 3.81-4.0 (2H, a), 6.58-6.67 (2H, a), 6.81-6.95 (2H, a), 7.0 (IH, ε), 7.25 (IH, a), 7.36-7.50 (2H, a), 7.64 (IH d, J=7Hz), 8.30 (IK, d, J=7Hz), 8.77 (IH, ε) Example 34 Thε following coapound waε obtained by uεing 2-nitro-4- (2-benzyloxybenzoyl)aaino-N-aethyl-N-[2-[5-(4-dimethylamino- piperidin-1-yl)carbonylpent-1-yloxy]-4-methylphεnyl]bεnzamid as a starting compound according to a εimilar manner to that of Examplε 10. 2-Amino-4-(2-hydroxybεnzoyl)amino-N-methyl-N-[2-[5-(4- dimethylaminopiperidin-1-yl)carbonylpεnt-1-yloxy]-4- methylphenyl]benzamide NMR (CDC1 3 , δ) : 1.21-2.02 (10H, ) , 2.28-2.44 (12H, a), 2.48-2.69 (IH, a), 2.93-3.08 (IH, a), 3.30 (3 s), 3.80-4.06 (4H, a), 4.68 (IH, br) , 4.73 (2H, s) 5.32 (IH, ε), 6.53-6.62 (3H, a), 6.78-6.96 (5H, a) 7.33-7.44 (IH, a), 7.76-7.88 (IH, a) Example 35 A aixture of 4-(2-hydroxybenzoyl)amino-3-methoxy-N-(2- benzyloxy-4-methyl)phenyl-N-methylbenzamide (550 mg) , 1- (tert-butoxycarbonyl)-4-hydroxypiperidinε (223 mg) , diethyl azodicarboxylatε (193 mg) and triphenylphosphme (291 mg) i tetrahydrofuran (15 ml) was stirred at ambient temperature for 8 hours and the mixture was diluted with ethyl acetate (25 ml) . The solution was washed with water and brine, and organic phase was dried over magnesium sulfate. The solven was evaporated in vacuo and the residue was purified by silica gel column (30% ethyl acetate in n-hexane) to give 3 methoxy-4-[2-[1-(tert-butoxycarbonyl)pipεridin-4- yl]oxybenzoyl]amino-N-(2-benzyloxy-4-methyl)phenyl-N- methylbenzamide (562 mg) . NMR (CDCI3, δ) : 1.44 (9H, s), 1.72-1.90 (2H, m) , 1.95-2.12 (2H, a), 2.27 (3H, s) , 2.95-3.16 (4H, 3.37 (3H, s), 3.60 (3H, s) , 3.73-4.00 (2H, a), 4. (IH, a), 4.88 (IH, d, J=14Hz), 5.08 (IH, d, J=14Hz), 6.65-6.71 (2H, a), 6.86 (IH, d, J=7Hz) , 6.95-7.03 (3H, a), 7.09 (IH, t, J=7Hz) , 7.25-7.5 (6H, a), 8.18 (IH, d, J=7Hz) , 8.35 (IH, d, J=7Hz) Example 36 The following compounds wεre obtained according to a similar manner to that of Example 35. 1) (S) -4- [2- [l-Methyl-3- (phthalimido) prop-1-yl] oxybenzoyl] amino-3-methoxy-N-methyl-N- [4-methyl-2- [5- (4-methyl- pipεrazin-1-yl ) carbonylpent-1-yloxy] phenyl ] benzamidε NMR (CDC1 3 , δ) : 1.43 (3H, d, J=7Hz) , 1.47-1.92 (7H, m), 1.98-2.13 (IH, m) , 2.20-2.47 (12H, m) , 3.32 (3H, s), 3.42-3.53 (2H, a), 3.57-3.67 (2H, a), 3.73-4.05 (7H, a), 4.77 (IH, a), 6.51-6.69 (2H, a) 6.78-7.12 (5H, a), 7.42 (IH, a), 7.57 (4H, s) , 8.08-8.24 (2H, a) 2) (R) -4- [2- [ [4- (Phthaliaido-l-yl)but-2-yl]oxy]bεnzoyl]- amino-3-mεthoxy-N-mεthyl-N- [4-mεthyl-2- [5- (4-methyl- piperazin-1-yl) carbonylpent-1-yloxy]phεnyl]bεnzamide NMR (CDCI3, δ) : 1.44 and 1.47 (total 3H, s), 1.52- 1.92 (8H, m), 2.02-2.12 (IH, m) , 2.28 (3H, ε), 2.3 (3H, ε), 2.33-2.42 (6H, m) , 3.35 (3H, s), 3.47-3.5 (2H, m), 3.60-3.67 (2H, m) , 3.80 (3H, s) , 3.85-4.0 (2H, br), 3.88 (2H, t, J=8Hz), 4.74-4.82 (IH, br) , 6.57-6.69 (2H, m) , 6.81-6.95 (2H, m) , 6.98-7.09 (3H, m) , 7.43 (IH, t, J=8Hz) , 7.53-7.60 (4H, br) , 8.14 (IH, d, J=8Hz), 8.20 (IH, d, J=8Hz) ESI-MASS (m/z) : 804 (M+H) 3) (R)-4-[2-[[4-(Phthalimido-l-yl)but-2-yl]oxy]benzoyl]- amino-3-mεthoxy-N-mεthyl-N- [4-mεthyl-2- [5- (4-dimεthyl- aminopipεridin-1-yl) carbonylpεnt-1-yloxy]phεnyl] - benzamidε NMR (CDCI3, δ) : 1.42 and 1.45 (total 3H, s) , 1.50- 1.90 (12H, m), 2.02-2.10 (IH, a), 2.28 (9H, s) , 2.32-2.41 (4H, m) , 2.52-2.62 (IH, m) , 2.97-3.06 (IH, m) , 3.35 (3H, s), 3.80 (3H, " s) , 3.87 (2H, t, J=8Hz), 3.90-3.97 (2H, a), 4.58-4.68 (IH, a), 4.72- 4.81 (IH, a), 6.57-6.67 (2H, a), 6.81-6.93 (2H, a), 6.98-7.08 (3H, a), 7.43 (IH, t, J=8Hz) , 7.53-7.59 (4H, br s), 8.13 (IH, d, J=8Hz), 8.20 (IH, d, J=8HZ ) 4 ) ( S ) -4-[2-[[4-(Phthalimido-l-yl)but-2-yl]oxy]benzoyl]- aminc-3-methoxy-N-methyl-N-[4-methyl-2-[5-(4-dimethyl- aminopiperidin-1-yl)carbonylpent-1-yloxy]phenyl]- benzamide NMR (CDC1 3 , δ) : 1.42 and 1.44 (total 3H, s), 1.50- 1.91 (12H, m) , 2.02-2.10 (IH, a), 2.29 (9H, s) , 2.32-2.41 (4H, a), 2.52-2.62 (IH, a), 2.95-3.05 (IH, a), 3.36 (3H, s) , 3.80 (3H, s) , 3.S6 (2K, t, J=8Hz), 3.90-3.97 (2H, a), 4.58-4.66 (IK, a), 4.7 4.80 (IK, a), 6.57-6.67 (2H, a), 6.81-6.92 (2H, a 6.98-7.08 (3H, a), 7.44 (IH, t, J=8Hz) , 7.53-7.60 (4H, br ε), 8.13 (IH, d, J=8Hz) , 8.21 (IK, d, J=8Hz) ESI-MASS (a/z) : 832 (M+l) 5) 3-Methoxy-4-[2-[3-(phthaliaido)-1-aethylprop-l- yl]oxybenzoyl]amino-N- (2-benzyloxy-4-methyl) henyl-N- methylbenzamide NMR (CDCI3, δ) : 1.41 (3H, d, J=7.5Hz), 1.96-2.12 (2H a), 2.24 (3H, ε), 2.27-2.42 (2H, a), 3.39 (3H, s) 3.60-3.69 (2H, a), 3.86 (2H, t, J=7.5Hz), 4.77 (I m), 4.94 (IH, d, J=14Hz) , 5.08 (IH, d, J=14Hz), 6.66-6.82 (3K, a), 6.95-7.08 (4K, a), 7.20-7.71 (10H, a), 8.10-8.21 (2K, a) Example 37 The following coapounds were obtained according to a siailar aanner to that of Exaaple 14. 1) 4-[2-(3-Acetylaminoprop-l-yl)oxybenzoyl]amino-3-metho N- (2-acetoxy-4-methylphenyl)-N-methylbenzamide NMR (CDCI3, δ) : 1.86 (3H, s) , 2.10-2.19 (2H, a), 2. (3H, s), 3.41 (2H, q, J=5Hz) , 3.72 (3H, s) , 4.21 (2H, t, J=5Hz) , 5. 94 (IH, br) , 6.85 (IK, s) , 6.90- 7 . 11 ( 6H, m) , 7 . 42-7 . 49 (IH, m) , 8.10 (IH, d, J=8Hz) , 8 .42 (IH, d, J=8Hz) 2) 4-[2- (3-Acetylaminoprop-l-yl)oxybenzoyl]amino-3-methoxy N-methyl-N-[2-[5-(4-dimethylaminopiperidin-l- yl)carbonylpent-1-yl]oxy-4-methylphenyl]benzamide NMR (CDC1 3 , δ) : 1.48-1.64 (2H, m) , 1.58-1.85 (4H, m) , 1.88 (3H, s), 2.12 (2H, t, J=5Hz), 2.29 (6H, s), 2.34-2.42 (2H, a), 2.57 (2H, t, J=5Hz) , 3.30 (2H, q, J=5Hz), 3.32 (3H, s), 3.39 (2K, q, J=5Hz) , 3.72 3.79 (2H, m), 3.76 (3H, s) , 3.83-4.00 (2H, m) , 4.2 (2H, t, J=5Hz), 6.33 (IH, br) , 6.57-6.67 (2H, m) , 6.83-7.10 (6H, m) , 7.43 (IH, dd, J=2, 7Hz), 8.10 (IH, d, J=8Hz), 8.38 (IK, d, J=8Hz) Example 38 To an ice bath cooled solution of 4-[2- (3-aminoprop-l- yl)oxybenzoyl]amino-N-[2- (5-carboxypent-l-yl)oxy-4- methyl]phεnyl-N-mεthylbenzamide (650 mg) in dichloromethane (20 ml) werε addεd triεthyla ine (137- mg) and di-tert- butyldicarbonate (296 mg) and the mixture was stirred at ambient temperature overnight. The solution was washed successivεly with watεr, 10% hydrochloric acid, saturated aqueous sodium hydrogen carbonate and brine, and the organic phase was dried over magnesium sulfate. The solvent was evaporatεd in vacuo to givε 4-[2-[3-(tert-butoxycarbonyl)- aminoprop-1-yl]oxybenzoyl]amino-N-[2-(5-ethoxycarbonylpent-l yl)oxy-4-methyl]phεnyl-N-methylbenzamide (749 mg) . NMR (CDCI3, δ) : 1.25 (3H, t, J=7.5Hz), 1.40 (9H, s) , 1.44-1.56 (2K, a), 1.66-1.76 (2H, a), 1.76-1.87 (2H, m), 2.06-2.15 (2H, a), 2.28 (3H, s) , 2.34 (2H, t, J=7.5Hz), 3.31 (3H, s) , 3.31-3.40 (2H, a), 3.85 3.97 (2H, a), 4.13 (2H, q, J=7.5Hz), 4.21 (2H, t, J=7.5Hz), 4.74 (IH, br) , 6.54-6.62 (2H, a), 6.86 (IH, d, J=7Hz), 6.98 (IH, d, J=7Hz) , 7.09 (IH, d, J=7Hz), 7.32 (2H, d, J=8Hz) , 7.41-7.52 (3H, m) , 8.11 (IH, d, J=7Hz), 9.87 (IK, s) Example 39 The following compound was obtained according to a similar manner to that of Example 38. 3-Methoxy-4-[2-[3-(tert-butoycarbonyl)amino-1- methylprop-l-yl]oxybεnzoyl]amino-N-(2-bεnzyloxy-4-mεthyl)- phenyl-N-methylbenzamide NMR (CDC1 3 , δ) : 1.37 (9H, s), 1.41 (3H, d, J=7.5Hz), 1.84-2.11 (2H, m) , 2.28 (3K, s), 3.20-3.31 (2H, a) 3.40 (3H, s), 3.64 (3H, s), 4.61 (IH, br) , 4.72 (IH, a), 4.90 (IH, d, J=14Hz) , 5.09 (IH, d, J=14Hz), 6.62-6.70 (2H, a), 6.84 (IH, d, J=7Hz) , 6.93-7.12 (4H, a), 7.28-7.72 (6K, m) , 8.22 (IH, d, J=7Hz), 8.36 (IH, d, J=7Hz) Example 40 A solution of aqueous 4M sulfuric acid (0.5 ml) and 3- (phthalimid-l-yl)propanal (189 mg) in tetrahydrofuran (10 m was εlowly added to a solution of 4-(2-aminobenzoylamino)-3 mεthoxy-N-mεthyl-N-[2-[5-(4-methylpipεrazin-l- yl)carbonylpent-1-yloxy]-4-aεthylphεnylbenzaaide (560 ag) i tetrahydrofuran (10 al) followed by the portionwise additio of εodiua borohydridε (59.8 ag) at 0 β C. Thε aixturε was dilutεd with 1,4-dioxane (5 al) and stirred for an addition 1.5 hours at ambient temperature. The mixture was quenched with water (0.5 ml) and concentrated. The residue was partitioned with ethyl acetate and saturated aqueous sodiu hydrogen carbonate. The organic extract was washed with brine and dried over sodium sulfate, concentrated, and purified by silica gel column chromatography (Si0 2 , 30 g, methanol in chloroform) to give 3-aethoxy-4-[2-[3- (phthalimido)prop-1-yl]amino]benzoylamino-N-methyl-N-[2-[5- (4-methylpiperazin-l-yl) carbonylpent-1-yloxy]phenyl]benzamid (200 mg) . NMR (CDC1 3 , δ) : 1.44-1.62 (2H, a), 1.63-1.93 (4H, a), 1.97-2.12 (2H, a), 2.21-2.46 (12H, a), 3.17-3.38 (5H, a), 3.42-3.56 (2H, a), 3.57-3.69 (2K, a), 3.70-4.04 (7H, a), 6.51-6.73 (4H, a), 6.78-6.96 (2H, m), 7.00 (IH, s), 7.20-7.35 (IH, m) , 7.40 (IH d, J=8Hz), 7.53-7.67 (3H, m) , 7.72-7.86 (2H, m) , 8.13 (IH, d, J=8Hz), 8.34 (IK, s) Example 41 A solution of 4- (2-nitrobenzoyl)amino-N-[2-(5- ethoxycarbonylpεnt-1-yloxy)-4-methylphenyl]-N-methylbenzamid (800 mg) , 20% palladium hydroxide (200 mg) in ethanol (20 ml) was stirred under atmospheric pressurε of hydrogεn at ambien tempεrature. After 2 hours, thε reaction mixture was filterεd through a bεd of Celite, and the solvent was removε by rotary εvaporation and thε crudε product was purified by silica gel column chromatography (Si0 30 g, ethyl acetate/hexanε = 3/1) to givε 4-(2-aminobenzoyl)amino-N- methyl-N-[2- (5-ethoxycarbonylpεnt-l-yloxy)-4-mεthylphεnyl]- bεnzamide (700 mg) . NMR (CDCI3, δ) : 1.25 (3H, t, J=7Hz) , 1.41-1.57 (2H, a), 1.63-1.87 (4H, a), 2.27 (3H, s), 2.33 (2H, t, J=7Hz), 3.32 (3H, s) , 3.78-4.00 (2H, a), 4.12 (2K, q, J=7Hz), 5.38-5.56 (2H, m) , 6.55-6.64 (2H, m) , 6.64-6.76 (2H, m)., 6.87 (IH, d, J=9Hz) , 7.22 (IH, d, J=9Hz), 7.28-7.50 (5H, m) , 7.79 (IH, br s) Example 42 The following compound was obtained according to a similar manner to that of Preparation 4. 4- (2-Aminobenzenεsulfonyl)amino-3-mεthoxy-N-mεthyl-N-[4- methyl-2-[5-(4-mεthylpiperazin-l-yl)carbonylpent-1- yloxy]phenyl]benzamide NMR (CDC1 3 , δ) : 1.45-1.54 (2H, m) , 1.65-1.82 (4H, m) , 2.30 (3H, s), 2.33 (3K, s) , 2.35-2.43 (6H, m) , 3.2 (3H, s), 3.46-3.51 (5H, ) , 3.60-3.65 (4H, m) , 4.84-4.89 (2H, m) , 6.56-6.89 (6H, m) , 7.28-7.48 (4H, m) ESI-MASS (m/z) : 638 (M+H) Example 43 A solution of 4-[2-(acetyloxy)bεnzoyl]amino-3-mεthoxy-N methyl-N-[2-[5-(4-dimethylaminopipεridin-l-yl)carbonylpent-1 yloxy]-4-methylphenyl]bεnzamide (400 mg) in methanol (10 ml) was treated with IN sodium hydroxide solution (3 ml) at ambient tempεraturε. After 6 hourε, the reaction mixture wa concentrated in vacuo and extracted with the mixture of dichloromethane and diluted hydrochloric acid. The organic phase was washed with brine and dried over sodium sulfate. The crude product was purified by silica gel column chromatography (Si0 2 30 g, 5% methanol in chloroform) to gi 4-[2-(hydroxy)benzoyl]amino-3-methoxy-N-methyl-N-[2-[5-(4- dιaethylaainopiperidin-1-yl)carbonylpent-l-yloxy]-4- aethylphenyl]benzaaide (290 ag) . NMR (CDCI3, δ) : 1.27-2.00 (10K, a), 2.21-2.46 (12H, a), 2.56 (IH, a), 3.00 (IH, a), 3.33 (3H, s) , 3.8 (3H, s), 3.82-4.05 (4H, a), 4.63 (IH, a), 6.55-6. (2H, a), 6.82-7.09 (5H, a), 7.42 (IH, a), 7.55 (I a), 8.20 (IH, a) • Example 44 The following coapounds wεre obtained according to a siailar aanner to that of Exaaole 43. 1 ) 4- (2-Kydroxybenzoyl) aaino-N-aεthyl-N- [2- (5- ethoxycarbonylpent-1-yloxy) -4-aethylphεnyl]benzaaide NMR (CDCI3, δ) : 1.26 (3H, t, J=7Kz) , 1.42-1.58 (2H, a), 1.61-1.90 (4H, m) , 2.28 (3H, s), 2.33 (2H, t, J=7Hz), 3.32 (3H, s) , 3.80 (3H, s) , 3.81-4.02 (2H, a), 4.12 (2K, q, J=7Hz), 6.53-6.67 (2H, m) , 6.80- 6.93 (3H, m), 7.01 (IH, d, J=8Hz), 7.07 (IH, s) , 7.42 (IH, dd, J=8, 8Hz), 7.49 (IH, d, J=8Hz) , 8.18 (IH, d, J=8Hz), 8.72 (IH, s) 2) 4- (2-Hydrcxybenzoyl) amino-3-methoxy-N-methyl-N- (2- methylphenyl)benzamide NMR (CDCI3, δ) : 2.21 (3H, s), 3.40 (3H, s), 3.78 (3H, s), 6.82-7.23 (9H, m) , 7.37-7.53 (2H, m) , 8.18 (IK, d, J-8Hz), 8.69 (IH, br s) 3) 4- (2-Kydroxybenzoyl) amino-3-methoxy-N-methyl-N- [4- mεthyi-2- [5- (4-mεthylpipεrazin-l-yl) carbonylpent-1- yloxy] phenyl ] benzamide NMR (CDCI3, δ) : 1.42-1.59 (2K, m) , 1.60-1.89 (4H, m) , 2.20-2.46 (12H, ) , 3.32 (3H, s) , 3.42-3.53 (2H, m), 3.57-3.69 (2H, m) , 3.71-4.02 (6H, m) , 6.51-6.68 (2K, r.), 6.79-7.08 (5H, m) , 7.40 (IH, a), 7.51 (IH, d, J-8KZ), 8.18 (IH, d, J=8Hz) , 8.86 (IH, br s) 4) 4- (2-Kydroxybenzoyl) aaino-3-aethoxy-N- (2-bεnzyloxy-4- ae thylphenyl ) -N-aethylbεnzaaidε NMR (CDCI3, δ) : 2.30 (3H, s), 3.38 (3H, s) , 3.63 (3H, s), 4.89 (IH, d, J=13Hz), 5.08 (IH, d, J=13Hz) , 6.62-6.68 (2H, a)-, 6.82-7.00 (6H, a), 7.28-7.42 (5H, a), 7.47 (IH, c, J=8Hz) , 8.13 (IK, d, J=8Hz) , 8.79 (IK, s) 5) 4- (2-Kydroxybenzoyl) aaino-3-aethoxy-N- [2- [4- (2-oxazolin- 2-yl)phεnylaεthyl]oxy-4-aεthylphεnyl]-N-aethylbenzaaidε NMR (CDCI3, δ) : 2.28 (3H, s), 3.40 (3H, s), 3.67 (3H, ε), 4.06 (2H, t, J=10Hz) , 4.41 (2H, t, J=10Hz) , 4 . 92 (IH, d, J=12Hz) , 5.10 (IH, d, J=12Hz) , 6. 60 (IH, s) , 6. 71 (IH, d, J=8Hz) , 6. 87-7 .08 (5H, a) , 7.28 (IH, d, J=8Hz) , 7 . 42 (IH, dd, J=2 , 8Hz) , 7 .5 ( IH, d, J=8Hz) , 8 .16 (IH, d, J=8Hz) , 8 .82 (IH, s) 6) 4-(2-Hydroxybenzoyl)amino-3-methyl-N-methyl-N-[2-[5-(4 methylpiperazin-1-yl)carbonylpent-1-yloxy]-4- methylphenyl]benzamide NMR (CDC1 3 , δ) : 1.48 (2H, br) , 1.60-1.81 (4H, m) , 2.19 (3H, s), 2.28 (3H, s), 2.30-2.35 (3H, m) , 2. (3H, ε), 2.50 (4H, br) , 3.30 (3H, s), 3.52 (2H, br), 3.69 (2H, br) , 3.83 (IH, br) , 3.92 (IH, br) , 6.62 (2H, s), 6.89-6.93 (2H, a), 7.02-7.10 (2H, a 7.35 (IH, s), 7.40-7.47 (IH, a), 7.63-7.70 (2H, a 8.52 (IH, br) Example 45 A solution of 4-[2-[3-(tert-butoxycarbonyl)aminoprop-1 yl]oxybenzoyl]amino-N-methyl-N-[4-methyl-2-[5-(4- methylpiperazin-1-yl)carbonylpent-1-yl]oxy]phenylbenzamide (542 mg) in 90% trifluoroacetic acid (10 ml) was stirred at ambient tempεraturε for 3 hours and the solvent was evaporated in vacuo. The residue was stirred with chlorof (20 al) and saturated aqueous sodium hydrogen carbonate (1 ml) and the organic phase was separated. The solution waε waεhed with brine and driεd over magnesium sulfate. The solvent was evaporatεd in vacuo to give 4-[2-(3-aminoprop- yl)oxybenzoyl]amino-N-methyl-N-[4-methyl-2-[5-(4- methylpiperazin-1-yl)carbonylpent-l-yl]oxy]phenylbεnzamidε (465 mg) . NMR (CDCI3, δ) : 1.47-1.59 (2H, a), 1.67-2.00 (6H, a 2.06-2.66 (2H, a), 2.35 (3H, s), 2.39 (3H, s) , 2.32-2.41 (4H, a), 2.96 (2H, t, J=7.5Hz), 3.31 ( s), 3.45-3.50 (2H, a), 3.58-3.65 (2K, a), 3.89-3 (2K, a), 4.29 (2H, d, J=7.5Kz), 6.54-6.62 (2H, a 6.85 (IK, d, J=7Hz), 7.01 (IH, d, J=7Hz) , 7.10 (IH t, J=7Hz), 7.32 (2H, d, J=8Hz) , 7.43-7.50 (3H, m) , 8.20 (IH, d, J=7Hz) Example 6 Thε following compoundε were obtained according to a εimilar manner to that of Example 45. I) 4-[2-[ (3-Aminoprop-l-yl)oxy]benzoyl]amino-3-mεthoxy-N- methyl-N-[4-methyl-2-[5- (4-mεthylpipεrazin-l- yl)carbonylpent-i-yloxy]phenyl]benzamide NMR (CDC1 3 , δ) : 1.40-1.92 (6H, m) , 1.98-2.12 (2H, m) , 2.19-2.44 (12K, m) , 2.90 (2H, t, J=7Hz) , 3.32 (3H, s), 3.40-3.53 (2H, m) , 3.56-3.68 (2H, m) , 3.78 (3H ε), 3.80-4.02 (2H, m) , 4.28 (2H, t, J=7Hz) , 6.51- 6.67 (2H, m), 6.78-6.95 (2H, m) , 6.97-7.16 (3H, m) 7.44 (IK, m) , 8.21 (IH, d, J=8Hz) , 8.40 (IH, d, J=8Hz) 2) 4-[2-[ (3-Aminoprop-l-yl)oxy]benzoyl]amino-3-mεthoxy-N- mεthyl-N-[2-[5-(4-dimethylaminopiperidin-l- yl)carbonylpent-1-yloxy]-4-methylρhenyl]bεnzamidε NMR (CDCI3, δ) : 1.26-1.92 (12H, m) , 1.98-2.12 (2H, m), 2.27 (9H, s), 2.29-2.42 (3H, m) , 2.56 (IH, m) , 2.89 (2H, t, J=7Hz) , 3.00 (IH, m) , 3.32 (3H, s) , 3.78 (3H, ε), 3.82-4.02 (3K, a), 4.27 (2H, t, J=7Hz), 4.61 (IK, a), 6.52-6.67 (2H, a), 6.79-6.96 (2H, a), 6.97-7.12 (3H, a), 7.43 (IH, a), 8.21 (IH, d, J=8Hz), 8.41 (IH, d, J=8Hz) 3 ) 4- [2- ( 3-Aminoprop-l-yl ) oxybεnzoyl ] amino-3-mεthoxy-N- aεthyl-N- [ 4-aεthyl-2- [ 5- ( 4-aεthylpiperidin-l- yl ) carbonylpent-1-yl ] oxy] phεnylbεnzaaidε NMR (CDCI3 , δ) : 0.95 (3H, d, J=7 .5Hz) , 1 .00-1 . 14 (2H, a) , 1 .46-1 . 90 ( 8K, a) , 2 .01-2 .12 (2H, a) , 2.26 (3H, ε), 2.34 (2H, t, J=7.5Kz), 2.52 (IH, m) , 2.85-3.03 (3H, m), 3.31 (3H, ε), 3.79 (3H, s) , 3.79-4.00 (4H ), 4.32 (2H, t, J=7.5Hz), 4.55 (IH, ) , 6.58 (IH, d, J=7Hz), 6.62 (IH, s) , 6.84 (IH, d, J=7Hz) , 6.90 (IH, d, J=7Hz), 7.00-7.11 (3H, m) , 7.42 (IH, t, J=7Hz), 8.21 (IH, d, J=7Hz), 8.40 (IK, d, J=7Hz) 4) 4-[2-(3-Aminoprop-l-yl)oxybenzoyl]amino-3-mεthoxy-N-[2- [5-[ (2S)-carbamoylpyrrolidin-l-yl]carbonylpent-l-yl]ox 4-mεthyl]phεnyl-N-mεthylbεnzamidε NMR (CDC1 3 , δ) : 1.48-2.20 (12K, m) , 2.28 (3H, s), 2.32-2.40 (2H, m) , 2.88-3.00 (2H, m) , 3.31 (3H, s) 3.33-3.61 (2H, m) , 3.80 (3H, s) , 3.82-3.99 (2H, m) 4.29 (2H, t, J=7Hz), 4.54 # (1H, m) , 6.52-6.63 (2H, a), 6.81-7.10 (5H, a), 7.43 (IH, t, J=7Hz) , 8.14 (IH, d, J=7Hz), 8.38 (IH, d, J=7Hz) 5) 4-[2-(3-Aminoprop-l-yl)oxybenzoyl]amino-3-methoxy-N-[2 (4-aminobut-l-yl)oxy-4-methyl]phenyl-N-methylbεnzamide NMR (CDCI3, δ) : 1.63-1.94 (4H, m) , 1.99-2.18 (2H, m) 2.23 (3H, s), 2.62-3.07 (2K; a), 3.29 (3H, s), 3.29-3.51 (2H, a), 3.75-4.00 (2H, a), 3.76 (3H, ε 4.21 (2H, t, J=7.5Hz), 6.56-6.85 (4H, a), 7.28-7. (2H, a), 8.13 (IH, d, J=7K∑) , 8.40 (IH, d, J=7Hz) 6) 4- [2-(3-Aminoprop-l-yl)oxybenzoyl]amino-3-methoxy-N-[2 (4-acεtylaminobut-l-yl)oxy-4-methyl]phenyl-N- methylbenzamide NMR (CDCI3, δ) : 1.60-1.86 (4H, ) , 2.00 (3H, s) , 2.08-2.20 (2H, a), 2.27 (3H, s) , 2.93-3.03 (2H, a 3.30 (3K, s), 3.30-3.50 (2H, a), 3.77 (3H, s) , 3.83-3.98 (2H, a), 4.26 (2H, t, J=7.5Hz), 6.53-6. (2H, a), 6.86-7.12 (5H, a), 7.42 (IH, t, J=7Hz) , 8.12 (IK, d, J=7Hz), 8.37 (IH, d, =7Hz) 7) 3-Mεthoxy-4-[2- (pipεridin-4-yl)oxybεnzoyl]amino-N-(2- hydroxy-4-methyl)phenyl-N-methylbenzamide NMR (DMSO-dg, δ) : 1.50-1.62 (2H, m) , 1.94-2.05 (2H, m), 2.14 (3H, ε), 2.57 (2H, t, J=7.5Hz), 2.91-3.00 (2H, m), 3.16 (3H, s), 3.75 (3H, s) , 4.73 (IH, m) , 6.48 (IH, d, J=7Hz), 6.64 (IH, s) , 7.87 (IK, d, J=7Hz), 7.92 (IH, d, J=7Kz) , 7.01 (IH, s) , 7.09 (IH, t, J=7Hz), 7.32 (IH, d, J=7Hz) , 7.52 (IK, t, J=7Hz), 8.02 (IH, d, J=7Hz) , 8.27 (lH, d, J=7Hz) 8) 3-Methoxy-4-[2- (pipεridin-4-yl)oxybenzoyl]amino-N- methyl-N-[4-methyl-2-[5-(4-methylpiperazin-l- yl)carbonylpent-1-yl]oxy]phenylbenzamide NMR (CDC1 3 , δ) : 1.46-1.88 (8H, a), 2.07-2.19 (2H, a), 2.26 (3H, s), 2.29 (3H, s), 2.32-2.41 (6H, a), 2.7 (2H, t, J=7.5Hz), 3.10-3.20 (2H, a), 3.32 (3H, s) , 3.45-3.50 (2H, a), 3.60-3.66 (2H, a), 3.80 (3H, s) 3.83-4.00 (2H, a), 4.57 (IH, a), 6.58 (IH, d, J=7Hz), 6.62 (IH, ε), 6.82-6.91 (2H, a), 6.98-7.11 (3H, a), 7.43 (IH, t, J=7Hz) , 8.20 (IH, d, J=7Hz) , 8.40 (IK, d, J=7Kz) 9) 4- [2- (3-Amino-l-methylprop-l-yl)oxybεnzoyl]amino-3- mεthoxy-N-mεthyl-N-[4-methyl-2-[5- (4-mεthylpipεrazin-l- yl)carbonylpεnt-1-yl]oxy]phεnylbεnzamide NMR (CDCI3, δ) : 1.42 (3K, d, J=7.5Hz), 1.46-1.89 (6H, m) , 1.99-2.11 (2H, m) , 2.28 (3H, s) , 2.30 (3H, s), 2.31-2.42 (6H, m)", 2.85 (2H, t, J=7.5Hz), 3.33 (3H, ε), 3.45-3.50 (2H, m) , 3.59-3.66 (2H, m) , 3.80 (3H, 8), 3.84-4.01 (2H, a), 4.80 (IH, a), 6.59 (IH, d, J=7Hz), 6.63 (IH, s) , 6.82-6.92 (2H, a), 7.01-7.10 (3H, a), 7.44 (IH, t, J=7Hz) , 8.22 (IH, d, J=7Hz) , 8.40 (IH, d, J=7Hz) 10) 4-[2- (3-Aminoprop-l-yl)oxybenzoyl]amino-3-mεthoxy-N- mεthyl-N-[2-(5-aminocarbonylpent-l-yl)oxy-4- methylphenyl]benzamide NMR (CDC1 3 , δ) : 1.40-1.59 (2K, m) , 1.61-1.90 (4H, m) , 2.11-2.30 (4H, a), 2.35 (3K, s) , 3.00 (2H, t, J=6Hz), 3.11 (2H, br), 3.29 (3K, s), 3.75 (3H, s) , 3.76-4.02 (2H, a), 4.23 (2H, t, J=5Hz) , 6.00 (IH, br), 6.50 (IH, br), 6.55-6.71 (2K, m) , 6.87-7.12 (5H, m), 7.42 (IH, dd, J=2, 7Hz) , 8.10 (IK, d, J=9Hz), 8.36 (IH, d, J=8Kz) 11) 4-[2-(3-Aminoprop-l-yl)oxybenzoyl]amino-3-methoxy-N- methyl-N-[2-[5-(morpholin-4-yl)carbonylpent-1-yl]oxy-4 methylphenyl]bεnzamide NMR (CDCI3, δ) : 1.48-1.90 (6H, m) , 2.11 (2H, t, J=5Hz), 2.26 (3H, s) , 2.21-2.52 (6H, m) , 2.79-2.9 (3H, m) , 2.96 (2H, t, J=5Hz) , 3.31 (3H, s) , 3.40- 3.49 (2H, a), 3.52-3.62 (2H, a), 3.80 (3H, s), 3.83-4.04 (2H, a), 4.29 (2H, t, J=5Hz) , 6.57-6.68 (2H, a), 6.81-7.12 (6K, a), 7.41-7.50 (IH, a), 8. (IH, d, J=8Hz), 8.39 (IH, d, J=8Hz) 12) 4-[2- (3-Aminoprop-l-yl)oxybenzoyl]amino-3-methoxy-N- mεthyl-N-[2-[5-(4-oxopipεridin-l-yl)carbonylpent-1- yl]oxy]-4-methylphenyl]benzamide NMR (CDCI3, δ) : 1.45-2.05 (8H, ) , 2.11 (2H, t, J=5Hz), 2.28 (3K, s) , 2.41-2.52 (2H, m) , 2.96 (2 t, J=5Hz), 3.31 (3H, s), 3.70-4.61 (8H, a), 6.52- 7.55 (8H, a), 8.02-8.46 (3H, a) 13) 4-[2-(3-Aminoprop-l-yl)oxybenzoyl]amino-3-methoxy-N-( methoxy-4-methylphenyl)-N-methylbεnzamide NMR (DMSO-dg, δ) : 1.90-1.98 (2K, m) , 2.25 (3H, s) , 2.71 (2H, t, J=6Hz), 3.19 (3H, s) , 3.73 (3H, s) , 4.32 (2H, t, J=5Hz), 6.67 (IH, d, J=8Hz) , 6.80-6.9 (2H, m) , 7.26 (IH, d, J=8Hz), 7.55 (IH, dd, J=2,8H 8 . 03 ( IH, d, J=8Hz ) , 8 .29 ( IH, d, J=8Hz ) 14) 4- [2- (3-Aminoprop-l-yl)oxybεnzoyl]amino-3-mεthoxy-N- [2- [4- (thiazol-2-yl)phenylmethyl]oxy-4-methylphenyl]-N- methylbεnzamide NMR (CDC1 3 , δ) : 2.02-2.10 (2H, m) , 2.29 (3H, s) , 2.89 (2H, t, J=5Hz), 3.40 (3H, s) , 3.64 (3H, s) , 4.25 (2H, t, J=5Hz), 4.90 (IH, d, J=llHz) , 5.09 (IH, d, J=llHz), 6.62-6.71 (2H, m) , 6.88 (IH, d, J=8Hz) , 6.98-7.10 (5H, m) , 7.24-7.48 (4K, m) , 7.81 (IH, d, J=3Hz), 7.95 (IH, d, J=8Hz) , 8.20 (IH, d, J=8Hz) , 8.37 (IH, d, J=8Hz) 15) 4- [2- (3-Aminoprop-l-yl)oxybenzoyl] amino-3-methoxy-N- [2- [4- (oxazol-2-yl)phenylmethyl]oxy-4-mεthylphεnyl]-N- methylbenzamidε NMR (CDCI3, δ) : 2.00-2.11 (2H, m) , 2.29 (3H, s) , 2.89 (2H, t, J=5Hz), 3.40 (3H, s), 3.66 (3H, s) , 4.91 (IH, d, J=12Hz), 5.10 (IK, d, J=12Hz), 6.64 (IH, s), 6.70 (IH, d, J=8Hz) , 6.87 (IH, d, J=8Hz) , 7.00 7.12 (4H, m) , 7.21 (IH, s) , 7.25-7.49 (4H, m) , 7.6 (IH, s), 8.04 (IH, d, J=8Hz) , 8.23 (IH, d, J=8Hz) , 8.37 (IH, d, J=8Hz) 16) 4- [2- (3-Aminoprop-l-yl) oxybenzoyl] amir.o-3-mεthoxy-N- [2- [4- (2-oxazolin-2-yl)phεnylmεthyl]oxymεthylphεnyl]-N- mεthylbenzamide NMR (CDCI3, δ) : 2.02-2.11 (2H, m) , 2.28 (3H, s), 2.90 (2H, t, J=5Hz), 3.39 (3H, s), 3.67 (3H, s) , 4.05 (2H, t, J=9Hz), 4.29 (2H, t, J=5Hz) , 4.41 (2H, t, J=5Hz), 4.89 (IH, d, J=12Hz) , 5,09 (IH, d, J=12Hz) , 6.63 (IH, s), 6.70 (IH, d, J=8Hz) , 6.84 (IH, d, J=8Hz), 7.00-7.12 (4K, m) , 7.37 (2H, d, J=8Hz) , 7.41 (IH, d, J=8Hz), 7.93 (2H, d, J=5Hz) , 8.20 (IH, d, J=8Hz), 8.36 (IH, d, J=8Hz) 17) 4-[2-(3-Aminoprop-l-yl)oxybenzoyl]amino-3-methoxy-N-[2- [4-(pyrimidin-2-yl)phenylmεthyl]oxy-4-methylphenyl]-N- mεthylbεnzamidε NMR (CDC1 3 , δ) : 2.05-2.14 (2H, a), 2.27 (3H, s) , 2.8 (2H, t, J=5Hz), 3.38 (3H, s) , 3.64 (3H, s) , 4.24 (2H, t, J=5Hz), 4.94 (IH, d, J=13Hz) , 5.12 (IH, d, J=13Hz), 6.65-6.72 (2H, a), 6.85 (IK, d, J=8Hz) , 6.97-7.18 (5H, a), 7.39-7.46 (3H, a), 8.13 (IK, d, J=8Hzi, 8.35 (IH, d, J=8Hz), 8.41 (2H, d, J=8Hz) , 8.24 (2H, d, J=3Hz) 18) 4-[2-(3-Amιnoprop-l-yl)oxybenzoyl]aaino-3-aethoxy-N-[2 (4-cyanophenylaethyl)oxy-4-methylphenyl]-N- methylbenzamide NMR (CDCI3, δ) : 2.09-2.20 (2H, a), 2.28 (3H, s) , 2.9 (2H, t, J=5Hz), 3.35 (3H, s), 3.65 (3H, s) , 4.24 (2K, br), 4.88 (IH, d, J=12Hz), 5.06 (IE, d, J-12HZ), 6.57 (IH, s) , 6.67-6.80 (2K, a), 6.95-7. (5H, a), 7.35-7.45 (3K, a), 7.62 (2H, d, J=8Hz), 8.11 (IK, d, J=8Hz), 8.30 (IK, d, J=8Hz) 19) 4- [2- (3-Ammoprop-l-yl) oxybenzoyl] amino-3-methoxy-N- methyl-N- [2- [5- (2-dimethylaminoεth-l-yl) oxycarbonyl- pent-1-yl ] oxy-4-methylphεnyl ] benzamide NMR (CDCI3, δ) : 1.47-1.60 (2H, m) , 1.67-1.88 (4H, a) 2.05-2.14 (2H, m) , 2.27 (9H, s) , 2.38 (2K, t, J=6Hz), 2.58 (2H, t, J=5Hz) , 2.92 (2H, t, J=5Hz) , 3.33 (3H, s), 3.80 (3H, s) , 3.86-4.00 (2H, a), 4. (2H, t, J=5Kz), 4.30 (2H, t, J=5Hz) , 6.57-6.67 ( a), 6.87 (IH, dd, J=2, 8Hz), 7.00-7.11 (4H, a), 7.44 (IH, dd, J=2, 8Hz), 8.20 (IH, d, J=8Hz) , 8. (IH, d, J=8Kz) 20) 4-[2-(3-Aminoprop-l-yloxy)bεnzoyl]amino-3-mεthoxy-N-( hydroxy-4- thylphεnyl)-N-mεthylbεnzamidε NMR (DMSO-dg, δ) : 1.92-2.03 (2H, m) , 2.16 (3H, s) , 2.75 (2H, t, J=5Hz), 3.20 (3H, s) , 3.75 (3H, s) , 4.34 (2H, t, J=5Hz), 6.49 (IH, d, J=8Hz) , 6.66 (IH, s) , 6.87 (IH, d, J=8Hz), 6.92 (IH, d, J=8Hz) , 7.12 (IH, dd, J=7, 8Hz), 7.29 (IH, d, J=8Hz), 7.58 (IH, dd, J=2, 8Hz), 8.05 (IH, d, J=8Kz) , 8.27 (IH, d, J=8Kz) 21) 4-[2- (3-Aminoprop-l-yl)oxybenzoyl]amino-3-methoxy-N-[2- [4- (1,5-dimethyl-3-cyanopyrrol-2-yl)phenylmεthyl]oxy-4- methylphenyl]-N-methylbεnzamidε NMR (CDC1 3 , δ) : 2.00-2.11 (2H, m) , 2.14 (3H, s) , 2.21 (3H, s), 2.89 (2H, t, J=5Hz) , 3.40 (3H, s) , 3.45 (3H, s), 3.62 (3H, s) , 4.27 (2H, t, J=5Hz) , 4.89 (IH, d, J=13Hz), 5.13 (IH, d, J=13Hz) , 6.22 (IH, s), 6.68-6.75 (2K, a), 6.89 (IH, d, J=8Kz) , 7.00- 7.12 (5H, a), 7.38-7.47 (6H, a), 8.19 (IH, d, J=8Hz), 8.38 (IH, d, J=8Hz) 22) 4- [2- (3-Aainoprop-l-yloxy) benzoyl] aaino-3-aethoxy-N- [2- [4- (N,N-diaethylureido) but-l-yl ]oxy-4-aε thylphεnyl] -N- methylbenzamide NMR (CDCI3, δ) : 1.62-1.88 (4H, m) , 1.90-2.15 (2H, m) , 2.27 (3H, s), 2.86-2.94 (2H, m) , 2.90 (6H, s) , 3.22-3.35 (2H, a), 3.31 (3H, s), 3.77 (3K, s) , 3.75-3.98 (2H, a), 4.27 (2H, t, J=5Hz) , 6.57-6.70 (2H, a), 6.88-7.11 (6H, a), 7.42 (IH, dd, J=2, 8Hz), 8.19 (IH, d, J=8Hz) , 8.38 (IH, d, J=8Hz) 23) 4-[2- (3-Aminoprop-l-yl)oxybεnzoyl]amino-3-methoxy-N-[2- [3- (4-methylpiperazin-l-yl)carbonylpyrid-6-yl]mεthoxy-4- methylphenyl]-N-methylbenzamide NMR (CDCI3, δ) : 2.09-2.20 (2H, m) , 2.28 (3H, s) , 2.31 (3H, s), 2.34-2.52 (4H, m) , 2.96 (2H, t, J=5Hz) , 3.40 (3H, s), 3.42-3.50 (2H, a), 3.69 (3H, s) , 3.70-3.84 (2H, a), 4.29 (2H, t, J=5Hz) , 4.98 (IH, - 204 - d, J=13Hz) , 5. 18 (IH, d, J=13Hz) , 6. 62 (IH, s) , 6.72 ( IH, d, J=8Hz) , 6.98-7. 11 (5H, m) , 7 .26-7 .34 (IH, a) , 7 .45 (IH, dd, J=2, 8Hz) , 7.73 (IK, d, J=8Hz) , 8 .16 (IH, d, J=8Hz) , 8 .36 (IH, d, J=8Kz) , 8.63 (IH, s) 24) 4- [2-(3-Aminoproo-l-yl)oxybenzoylJamino-3-methoxy-N-[2- [4-(3-dimethylaminoprop-i-yloxycarbonyl)aminobut-1- yl]oxy-4-methylphεnyl]-N-mεthylbenzamide NMR (CDCI3, δ) : 1.62-1.87 (6H, a), 2.02-2.11 (2H, a), 2.27 (6K, s), 2.41 (2H, t, J=5Hz) , 2.91 (2H, t, J=5Hz), 3.22 (2K, q, J=5Hz) , 3.30 (3H, s), 3.78 (3H, s), 3.84-3.95 (2H, a), 4.08 (2H, t, J=5Hz) , 4.27 (2H, t, J=5Hz), 6.60-6.66 (2H, a), 6.90 (IK, d, J=8Hz), 6.99-7.10 (3H, a), 7.44 (IH, dd, J=2, 8Hz), 8.18 (IH, d, J=8Hz), 8.38 (IH, d, J=8Hz) 25) 4-[2- (3-Aminoprop-l-yl)oxybenzoyl]amino-3-mεthoxy-N- aethyl-N-[2-[5- (4-aethylhomopiperazin-l-yl)carbonylpent 1-yl]oxy-4-methylphenyl]benzamide NMR (CDC1 3 , δ) : 1.50-2.18 (8H, m) , 2.30 (3H, s) , 2.32 (2H, t, J=5Hz), 2.33 (3H, s) , 2.53-2.70 (4H, a), 2.93 (2H, t, J=5Hz), 3.35 (3H, s) , 3.52-3.72 (4H, a), 3.80 (3H, s), 3.82-4.09 (2H, a), 4.31 (2H, t, J=5Hz), 6.55-6.70 (2H, a), 6.82-7.18 (6H, a), 7.42 7.53 (IH, a), 8.20 (IH, d, J=8Hz) , 8.41 (IH, d, J=8Hz) 26) 4- [2- ( 3-Aminoprop-l-yl ) oxybenzoyl] amino-3-methoxy-N- methyl-N- [2- [5- (2-dimethylaminoethyl ) aminocarbonylpent l-yl] oxy-4-methylphεnyl] bεnzamide NMR (CDCI3, δ) : 1.45-1.60 (2K, a), 1.66-2.15 (8H, a) 2.22 (6H, s), 2.26 (3K, s) , 2.41 (2H, t, J=5Hz) , 3.22-3.39 (2H, a), 3.31 (3H, s) , 3.70-4.00 (2H, a 3.78 (3H, s) , 4.28 (2H, t, J=5Hz) , 6.37 (IH, br) , 6.59 (2H, br) , 6. 81-7 . 13 ( 6K, m) , 7 .42 (IH, dd, J=2 , 8Hz ) , 8 . 18 ( IK, d, J=8Hz) , 8 . 36 (IH, d, J=8Hz 27) 4-[2- (3-Aminoprop-l-yl)oxybenzoyl]amino-3-mεthoxy-N- methyl-N-[2-[5-[N- (2-dimethylaminoεthyl)-N-methylamino- carbonyl]pent-1-yl]oxy-4-methylphenyl]benzamide NMR (CDC1 3 , δ) : 1.40 (9H, s) , 1.44-2.21 (8H, m) , 2.25 (3H, s), 2.27 (6H, s) , 2.29-2.50 (4H, a), 2.91 (IH, s), 3.00 (2H, s), 3.26-3.51 (4H, a), 3.31 (3H, s) , 3.77 (3H, br s), 3.81-4.02 (2H, a), 4.22 (2H, t, J=5Hz), 4.88 (IH, br) , 6.52-6.68 (2H, br) , 6.79- 7.11 (5H, a), 7.43-7.50 (IH, a), 8.20 (IH, d, J=8Hz), 8.39 (IH, d, J=8Hz) 28) 4-[2-(3-Aminoprop-l-yl)oxybenzoyl]amino-3-methoxy-N- methyl-N-[2-[5-[N- (3-dimεthylaminoprop-l- yl)carbamoyl]pent-1-yl]oxy-4-methylpehεnyljbεnzamidε NMR (CDCI3, δ) : 1.46-1.60 (2H, m) , 1.63-1.99 (8H, m) , 2.03-2.14 (2H, m) , 2.21 (2H, t, J=5Hz) , 2.24 (6H, s), 2.29 (3H, s) , 2.39 (2K, t, J=5Hz) , 2.90 (2H, t, J=6Hz), 3.25-3.37 (2H, a), 3.32 (3H, s) , 3.79 (3K, s), 3.81-4.01 (2K, a), 4.30 (2H, t, J=5Kz) , 6.61 (2H, br), 6.85-7.14 (6H, a), 7.39-7.50 (IH, a), 8.20 (IH, d, J=8Hz), 8.40 (IH, br) 29) 4-[2- (3-Aminoprop-l-yl)oxybenzoyl]amino-3-methoxy-N- mεthyl-N-[2-[5-[N- (3-dimethylaminoρrop-l-yl)-N- methylcarbamoyl]pent-1-yl]oxy-4-mεthylphenyl]benzamide NMR (CDCI3, δ) : 1.52-1.94 (6H, m) , 2.05-2.14 (2H, m) , 2.20 (3H, ε), 2.21 (3H, s) , 2.26 (3K, s) , 2.20-2.45 (6H, s), 2.90 (2K, t, J=5Hz), 2:91 and 2.99 (total 3H, s, rotamer), 3.32 (3H, s), 3.40 (2H, t, J=5Hz) , 3.80 (3H, s), 4.31 (2H, t, J=5Hz) , 6.55-6.67 (2H, a), 7.41-7.49 (2K, a), 8.21 (IH, d, J=8Hz) , 8.42 (IH, d, J=8Hz) 30) 4-[2- (3-Aminoprop-l-yl)oxybenzoyl]amino-3-methoxy-N- methyl-N-[2-[5- (4-hydroxypiperidin-l-yl)carbonylpent-1- yl]oxy-4-mεthylphεnyl]benzamide NMR (CDC1 3 , δ) : 1.43-1.95 (6K, m) , 2.03-2.51 (8H, m) , 2.29 (3H, s), 2.94 (2H, t, J=5Hz) , 2.98-3.22 (4H, a), 3.32 (3H, s), 3.46-3.58 (IH, a), 3.79 (3H, s) , 3.80-4.26 (6H, a), 4.28 (2H, t, J=5Hz) , 6.56-6.67 (2H, a), 6.81-7.13 (6H, a), 7.36 (IH, dd, J=8, 8Hz), 8.10-8.20 (IK, a), 8.33-8.49 (IH, a) 31) 4-[2-(3-Aminoprop-l-yl)oxybenzoyl]ammo-3-methoxy-N- methyl-N-[2-[5-(4-aminopiperidin-l-yl)carbonylpent-1- yl]oxy-4-methylphenyl]benzamide NMR (CDCI3, δ) : 1.51-2.03 (6K, m) , 2.09-2.19 (2H, m) , 2.27 (3H, s), 2.29-2.42 (4H, ) , 2.59-2.71 (2H, m) 2.94 (2H, t, J=5Hz), 2.96-3.11 (3H, m) , 3.33 (3H, s), 3.78 (3H, s), 3.85-4.02 (2H, m) , 4.22 (2H, t, J=5Hz), 6.55-6.67 (2H, m) , 6.81-7.12 (6H, m) , 7.4 (IH, dd, J=8, 8Hz), 8.19 (IH, d, J=8Hz) , 8.40 (IH d, J=8Hz) 32) 4-[2- (3-Aminoprop-l-yl)oxybenzoyl]amino-3-methoxy-N- mεthyl-N-[2-[5-(4-mεthylpipεrazin-l-yl)- aminocarbonylpεnt-l-yl]oxy-4-mεthylphεnyl]bεnzamide NMR (CDCI3, δ) : 1.46-1.89 (6H, m) , 1.93-2.05 (4H, m) 2.25 (6H, s), 2.49 (2H, t, J=5Hz) , 2.52-2.62 (2H, m) , 2.79-2.89 (2H, ) , 2.92 (2H, t, J=5Hz) , 3.31 (3H, s), 3.79 (3K, s) , 3.80-4.01 (2H, m) , 4.28 (2 t, J=5Hz), 6.56-6.64 (2H, m) , 6.80-7.12 (6H, m) , 7.41-7.50 (IH, m) , 8.18 (IH, d, J=8Kz) , 8.40 (IK, d, J=8Hz) 33) 4-[2-(3-Aminoprop-l-yl)oxybenzoyl]amino-3-methoxy-N- methyl-N-[2-[5-[bis(2-hydroxyethy-l-yl)- aminocarbonylpent-l-yl]oxy-4-mεthylphεnyl]bεnzamidε NMR (CDCI3, δ) : 1.54-1.91 (6K, m) , 2.11-2.20 (2H, m) , 2.26 (3H, s), 2.38-2.59 (4H, m) , 3.40-3.57 (4H, m) , 3.61-3.97 (6H, m) , 4.22 (2H, t, J=5Hz) , 6.60-6.68 (2H, m) , 6.88-7.16 (6H, m) , 7.44-7.54 (IH, m) , 8.1 (IH, d, J=8Hz), 8.41 (IH, d, J=8Hz) 34) 4-[2-(3-Aminoprop-l-yl)oxybenzoyl]amino-3-methoxy-N- methyi-N-[2-[5- (2,2-dimethylhydrazino)carbonylpent-1- yl]oxy-4-methylphεnyl]bεnzamidε NMR (CDCI3, δ) : 1.47-1.91 (6H, m) , 2.06-2.40 (4H, m) , 2.28 (3H, s), 2.51 (3H, s) , 2.57 (3H, s) , 2.92 (2H, t, J=5Hz), 3.32 (3H, s) , 3.78 (3H, s) , 3.80-4.02 (2H, m) , 4.28 (2H, t, J=5Hz), 6.55-6.68 (2H, m) , 6.80-7.13 (5H, ) , 7.46 (IH, dd, J=8Hz) , 8.19 (IH, d, J=8Hz), 8.38 (IH, br) 35) 4-[2-(3-Aminoprop-l-yl)oxybenzoyl]amino-3-methoxy-N- mεthyl-N-[2-[5-(carbamoylmεthylamino)carbonylpεnt-1- yl]oxy-4-mεthylphεnyl]bεnzaaidε NMR (CDCI3, δ) : 1.47-1.58 (2H, a), 1.68-1.85 (4H, a), 2.06-2.17 (2H, a), 2.27 (3H, s) , 2.94 (2H, t, J=5Hz), 3.31 (3H, s), 3.80 (3K, s) , 3.81-4.00 (2H, a), 3.89 (2H, d, J=5Kz) , 4.28 (2H, t, J=5Hz) , 5.78 (IH, br), 6.60-6.74 (3H, a), 6.90-7.13 (6H, a), 7.41-7.49 (IH, a), 8.17 (IH, d, J=8Hz) , 8.39 (IH, d, J=8Hz) 36) 4-[2- (3-Aminoprop-l-yl)oxybenzoyl]amino-3-mεthoxy-N- methyl-N-[2-[5- (2-carbamoylethylamino)carbonylpent-1- yl1oxy-4-methylphenyl]benzamidε NMR (CDCI3, δ) : 1.45-1.58 (2K, m) , 1.62-1.84 (4H, m) , 2.14 (2H, t, J=5Hz), 2.22 (2H, t, J=5Hz) , 2.29 (3H, s), 2.40 (2H, t, J=5Hz), 2.98 (2H, br) , 3.30 (3H, s), 3.40-3.55 (2H, a), 3.78 (3H, s) , 3.80-4.01 (2H, a), 4.27 (2H, t, J=5Hz) , 6.58-6.79 (4H, a), 6.88- 7.12 (6H, a), 7.41-7.49 (IH, a), 8.16 (IH, d, J=8Hz), 8.39 (IH, d, J=7Hz) 37) 4-[2-(3-Aminoprop-l-yl)oxybenzoyl]amino-3-methoxy-N- methyl-N-[2-[5-(4-pyridylaminocarbonyl)pent-I-yl]oxy-4 mεthylphεnyl]bεnzamidε NMR (CDC1 3 , δ) : 1.52-1.89 (6H, m) , 2.10-2.22 (2H, m) 2.26 (3H, s), 2.45 (2H, br) , 2.95 (2H, t, J=5Hz), 3.32 (3H, s), 3.72 (3H, s) , 3.82-4.00 (2H, m) , 4. (2H, t, J=5Kz), 6.57-6.72 (2K, m) , 6.90-7.15 (6H, m), 7.46 (IH, dd, J=2, 8Hz) , 7.56 (2H, br) , 8.12 (IH, d, J=8Hz), 8.35-8.50 (3H, m) , 9.46 (IH, br) 38) 4-[2-(3-Aminoprop-l-yl)oxybenzoyl]amino-3-mεthoxy-N- mεthyl-N-[2-[5-[4-(diethylaminopiperidin-1- yl)carbonylpent-1-yl]oxy-4-methylphεnyl]bεnzamidε NMR (CDCI3, δ) : 1.05 (6H, t, J=5Hz) , 1.35-1.95 (10K, a), 2.04-2.13 (2H, a), 2.28 (3H, s) , 2.36 (2H, t, J=5Hz), 2.54 (4K, q, J=5Hz) , 2.56-2.80 (2H, a), 2.91 (2H, t, J=5Hz), 2.93-3.07 (2H, a), 3.33 (3H, s), 3.80 (3K, s), 3.82-4.03 ' (2H, a), 4.30 (2H, t, J=5Hz), 6.56-6.68 (2H, a), 6.81-7.12 (6H, a), 7. 7.49 (IH, a), 8.22 (IH, d, J=7Hz) , 8.41 (IH, d, J=8Hz) 39) 4-[2-(3-Aainoprop-l-yl)oxybεnzoyl]aaino-3-aethoxy-N- aεthyl-N-[2-[6-(4-aεthylpipεrazin-l-yl)hex-l-yl]oxy-4 aεthylphεnyl]bεnzaaidε NMR (CDCI3, δ) : 1.45-1.58 (2H, a), 1.62-1.84 (4H, a 2.14 (2H, t, J=5Hz), 2.29 (3H, s) , 2.40 (2H, t, J=5Hz), 2.98 (2H, br) , 3.30 (3K, s) , 3.40-3.55 ( a), 3.78 (3K, s), 3.80-4.01 (2K, a), 4.27 (2H, t J=5Hz), 6.58-6.79 (4H, a), 7.41-7.49 (IH, a), 8. (IH, d, J=8Hz), 8.39 (IH, d, J=8Hz) 40) 4- [2- (3-Aminoprop-l-yl) oxybenzoyl] amino-3-methoxy-N- [2- [4- (2-pyridyl)phenylaethyl]oxy-4-aethylphenyl]-N- aεthylbεnzaaidε NMR (CDC1 3 , δ) : 1.97-2.08 (2H, a), 2.26 (3H, s) , 2.85 (2H, t, J=5Hz), 3.40 (3H, s), 3.62 (3H, s) , 4.26 (2H, t, J=5Hz), 4.96 (IH, d, J=12Hz) , 5.14 (IH, d, J=12Kz), 6.54-6.62 (2H, a), 6.40 (IH, d, J=7Hz) , 6.98-7.14 (5H, a), 7.39 (IH, d, J=8Hz) , 7.39-7.49 (IH, a), 7.70 (2K, s), 7.98 (IH, d, J=8Hz) , 8.22 (IH, d, J=8Hz), 8.39 (IH d, J=8Hz) , 8.68 (IH, br) 41) 4-[2- (3-Aminoprop-l-yl)oxybεnzoyl]amino-3-mεthoxy-N-[2- [4-[ (4-mεthylpiperazin-l-yl)carbonylamino]but-l-yl]oxy- 4-mεthylphεnylj-N-methylbenzamide NMR (CDCI3, δ) : 1.62-1.88 (4H, m) , 2.30-2.15 (2H, m) , 2.28 (6H, s), 2.34-2.42 (4H, a), 2.93 (2K, t, J=5Hz), 3.25-3.48 (6H, a), 3.33 (3H, s), 3.79 (3H, s), 3.79-3.99 (2H, a), 4.30 (2H, t, J=5Kz) , 6.58- 6.70 (2H, a), 6.90-7.11 (5H, a), 7.45 (IH, dd, J=2 8Hz), 8.20 (IH, d, J=8Kz) , 8.40 (IH, d, J=8Hz) 42) 4-[2- (3-Aminoprop-l-yl)oxybenzoylamino]-3-methoxy-N-[2- [4- [ (4-dimethylaminopiperidin-l-yl)carbonylamino]but-l- yl]oxy-4-methylphenyl]-N-methylbεnzamide NMR (CDCI3, δ) : 1.44-1.98 (8H, a), 2.26 (3H, s) , 2.49 (6H, s), 2.66-2.93 (3H, a), 3.05 (2H, t, J=5Hz) , 3.25-3.32 (2H, a), 3.29 (3H, s) , 3.79 (3H, s) , 3.81-3.99 (2K, a) ' , 4.15-4.29 (4H, a), 6.57-6.64 (2H, a), 6.91-7.12 (5H, a), 7.46 (IH, dd, J=2, 8Hz), 8.04 (IK, d, J=8Hz) , 8.35 (IH, d, J=8Hz) Example 47 The following coapound was obtained by using 4-[2- (3- tert-butoxycarbonylaainoprop-1-yl)oxybenzoyl]amino-3-methoxy N-[2- (3-tεrt-butoxycarbonylaainoprop-l-yl)oxy-4- methyl]phεnyl-N-mεthylbenzamide as a starting compound according to a similar manner to that of Example 45. 4-[2-(3-Aminoprop-l-yl)oxybenzoyl]amino-3-mεthoxy-N-[2 (3-aminoprop-l-yl)oxy-4-methyl]phenyl-N-mεthylbεnzamide NMR (CDC1 3 , δ) : 1.87-1.98 (2H, a), 2.00-2.09 (2H, a), 2.25 (3H, s), 2.83-2.96 (4K, a), 3.30 (3H, s) , 3. (3H, s), 3.87-4.10 (2H, a), 4.27 (2K, t, J=7.5Hz), 6.57-6.66 (2H, a), 6.90 (IH, a), 7.00-7.10 (3H, a) 7.42 (IH, t, J=7Hz), 8.20 (IH, d, J=7Hz) , 8.39 (I d, J=7Hz) Example 48 The following coapounds were obtained according to a siailar manner to that of Example 47. 1) 4-[2-(3-Aminoprop-l-yl)oxybenzoyl]amino-3-methoxy-N-[2 (4-aainoacetylaainobut-I-yl)cxv-4-methyl]phenyl-N- methylbenzamide MASS (m/z) : 592 (M+l) 2) 4-[2-(3-Aminoprop-l-yl)oxybenzoyl]amino-3-methoxy-N- methyl-N-[2-[5- (pioerazin-1-yl)carbonylpεnt-1-yl]oxy-4 mεthylphεnyl]bεnzamidε NMR (CDCI3, δ) : 1.48-1.95 (6H, m) , 2.07-2.20 (2H, a) 2.28 (3H, s), 2.32-2.63 (5H, a), 2.75-3.01 (3H, 3.21 (3H, s), 3.40-3.64 (4H, a), 3.78 (3K, s) , 3.83-4.08 (2K, a) " , 4.27 (2H, t, J=5Hz) , 6.55-6.7 (2H, a), 6.82-7.17 (6H, a), 7.20-7.50 (IH, a), 8. (IH, d, J=7Kz), 8.39 (IK, d, J=SHz) 3) 4-[2-(3-Aminoprop-l-yl)oxybenzoyl]amino-3-methoxy-N-[ [4- (3-aminopropionyl)aminobut-1-yl]oxy- -methylphenyl] N-methylbenzamide NMR (CDCI3, δ) : 1.64-1.88 (4H, a), 2.06-2.19 (2H, a 2 .28 (3H, s ) , 2 . 32-2 . 46 (2H, a) , 2.90-3. 13 (4H, a) 3 .23-3. 44 (2H, a) , 3 .30 (3H, s) , 3 .77 (3H, s) , 3.78-4 . 01 (2H, a) , 4 .27 (2H, br) , 6.55-6. 68 (2H, a) , 6. 88-7 . 11 (5H, a) , 7 .28-7 .50 (2H, a) , 8 .20 (IH Q, J=8Hz) 8 .31 (IH, d, J=8Hz) 4) 4- [2- (3-Aainoprop-l-yl)oxybenzoyl]amino-3-methoxy-N- [2- [4- (pipεridin-4-yl) carbonylaminobut-l-yl]oxy-4- methylphenyl]-N-methylbenzamide NMR (CDC1 3 , δ) : 1.60-1.91 (8H, a), 2.09-2.21 (2H, a), 2.28 (3H, s), 2.70 (IH, br) , 2.97 (2H, t, J=5Hz) , 3.11-3.40 (8H, a), 3.30 (3H, s) , 3.72-3.96 (2H, a) 3.78 (3H, s), 4.28 (2K, t, J=5Hz) , 6.57-6.65 (2H, a), 6.90-7.08 (4H, a), 7.23-7.28 (2H, a), 7.38-7.4 (2H, a), 8.13 (IH, d, J=8Hz) , 8.38 (IH, d, J=8Hz) 5) 4- [2- (3-Aminoprop-l-yl)oxybenzoyl]amino-3-mεthoxy-N- [2- (4-guanidinobut-l-yl) oxy-4-methylphεnyl]-N- methylbεnzamidε NMR (CDCI3, δ) : 1.62-1.80 (4H, m) , 2.05-2.14 (2H, m) , 2.20 (3H, s), 2.55-2.70 (2H, a), 2.94 (2H, t, J=5Hz), 3.31 (3H, s) , 3.62-3.73 (2H, a), 3.72 (3H, s), 4.22 (IH, d, J=5Hz), 6.48 (IH, d, J=8Hz) , 6.61 (IH, s), 6.75 (IH, d, J=8Hz), 6.95-7.09 (5H, a), 7.43 (IH, dd, J=2, 8Hz) , 8.03 (IH, d, J=8Hz) , 8.32 (IH, d, J=8Hz) Example 49 A solution of 4-hydroxy-3-mεthoxy-N-methyl-N-[4-methyl- 2- [5- (4-mεthylpipεrazin-l-yl) carbonylpent-1-yloxy]phenyl] - benzamide (320 mg) in N,N-dimethylformamide (8 ml) was treatεd with sodium hydridε (29.1 mg, 60% w/w in mineral oil) at 0 β C. The reaction mixturε was stirred at 0 β C for 15 minutes and then at ambient temperature for 10 minutes. o-Nitrobenzyl bromide (143 mg) was added, and the reaction mixture was stirred for 2.5 hours. The reaction was quench with water and the mixture was diluted with ethyl acetate. The organic phase was washed with saturated aqueous sodium hydrogen carbonate, and brine. The organic solution was dried over magnesium sulfate, concentrated, and purified by silica gel column chromatography (Si0 2 15 g, 3% methanol in dichloromethane) to give 3-methoxy-4-(2-nitrobenzyloxy)-N- methyl-N-[4-aethyl-2-[5-(4-methylpiperazin-l-yl)carbonylpen 1-yioxy]phenyl]benzamide (210 mg) . NMR (CDC1 3 , δ) : 1.43-1.59 (2H, a), 1.61-1.88 (4H, m) 2.21-2.44 (12H, a), 3.31 (3H, s) , 3.42-3.52 (2H, a), 3.56-3.67 (2H, a), 3.71 (3H, s) , 3.78-4.00 (2 a), 5.46 (3H, s), 6.52-6.67 (3H, a), 6.77-6.91 (2 a), 6.95 (IH, br s), 7.46 (IH, a), 7.64 (IH, a), 7.84 (IH, d, J=8Hz), 8.14 (IK, d, J=8Hz) Example 50 To a solution of 4-[2-(3-aminopropylthio)benzoyl]amino 3-methoxy-N-nethyi-N-[4-methyl-2-[5-(4-mεthylpiperazin-l-yl carbonylpent-1-yloxy]phenyl]benzamide (160 mg) in methanol ml) was added _ suspension of sodium metapεriodate (50.6 m and 5 ml of water. The mixture was stirred for 20 hours a ice-bath temperature and diluted with chloroform. The lo chloroform layer was removed,'and the water layεr was εxtracted with chloroform. The combined organic extracts were dried over anhydrous sodium sulfate. The solvent was removed at reduced pressure, and purified by preparative t layer chromatography (methanol/dichloromethan/ammonia = 10/90/2) to givε free amine (70 mg) . To a solution of thi amine in ethanol (3 al) was added IN hydrochloric acid (0. al) and stirred for 5 ainutes. The solution was concentra to give 4-[2-(3-aminopropylεulfinyl)benzoyl]amino-3-methox N-mεthyl-N-[4-methyl-2-[5-(4-methylpiperazin-l- yl)carbonylpent-1-yloxy]phenyl]benzamide dihydrochloride. NMR (DMSO-dg, δ) : 1.38-1.67 (4H, m) , 1.68-1.88 (2K, a), 1.94-2.13 (2H, m) , 2.22 (3H, s), 2.40 (2H, t, J=7Hz), 2.69-3.12 (9H, m) , 3.12-3.58 (7H, a), 3.62 (3H, s), 3.80-4.17 (3H, m) , 4.43 (IH, a), 6.64 (IH, c, J=8Hz), 6.83 (IK, s), 6.91 (2H, br ε) , 7.04 (IH, d, J-8Hz), 7.53 (IH, a), 7.68 (IH, dd, J=8, 8Hz), 7.85 (IH, dd, J=8, 8Hz), 7.90-8.19 (3H, ε) , 9.84 (IE, s) Example 51 To a εolution of 3-methoxy-4-[2-[3-(phthalimido)prop-1- yl]thiobenzoyl]amino-N-methyl-N-[4-methyl-2-[5-(4- methylpiperazm-1-yl)carbonylpent-1-yl]oxy]phenylbenzamide (150 mg) in dichloromethane (10 ml) waε added m- chloroperbenzcic acid (80.3 mg) and the mixture was stirred at ambient temperature for 2 hours. The solution was washed succeεεively with saturatεd aquεouε εodium hydrogεn carbonatε, water and brinε, and thε organic phaεε was dried over magnesium sulfate. The solvent was evaporated in vacuo ' and the residue was purifiεd by silica gel column (2% methanol in chloroform) to give 3-methoxy-4-[2-[3- (phthalimico)prcp-1-yl]εulfonylbenzoyl]amino-N-methyl-N-[4- methyl-2-[5- (4-aethylpiperazin-l-yl)carbonylpent-1- yl]oxy]phenylbenzamide (150 mg) . MASS (m/z) : 839 (M+l) Example 52 A solution of 4-[2-[2-[ (3-aminioprop-l-yl)oxy]phenyl]- vinyl]-3-methoxy-N-methyl-N-[4-mεthyl-2-[5-(4- mεthylpipεrazin-1-yl)carbonylpεnt-1-yloxy]phεnyl]benzamide (100 mg) , 20% palladium hydroxide (30 mg) in methanol (5 ml) was stirred under atmoεpheric preεsurε of hydrogen at ambient tεmpεrature. After 12 hours, the reaction mixture was filtered through a bed of Celite, and the solvent was removed by rotary evaporation and the crude product was purifiεd by NH-silica gel (chromatorex) column chromatography (Si0 2 10 g. 1% methanol in chloroform) to give free amine. To the solution of amine (80 mg) in ethanol (3 ml) was added IN hydrochloric acid (0.25 ml) and stirred for 5 minutes. The solution was evaporated to give 4-[2-[2-[ (3-aminoprop-l- yl)oxy]phenyl]ethyl]-3-methoxy-N-mεthyl-N-[ -mεthyl-2-[5-(4- methylpiperazin-1-yl)carbonylpent-l-yloxy]phenyl]benzamide dihydrochloride (70 mg) . NMR (DMSO-dg, δ) : 1.36-1.65 (4H, m) , 1.65-1.82 (2H, a), 1.97-2.13 (2H, ) , 2.22 (3H, s), 2.39 (2H, t, J=7Hz), 2.58-3.11 (13H, m) , 3.17 (3H, s) , 3.26-3.6 (5H, m), 3.72-4.21 (5H, m) , 4.42 (IH, m) , 6.63 (I d, J=8Hz), 6.70-7.05 (8H, a), 7.13 (IH, dd, J=8, 8Hz), 8.00-8.24 (2K, a) Example 53 The following compounds were obtained according to a siailar aanner to that of Examplε 10. 1) 4-[2-[ (3-tert-Butoxycarbonylaminoprop-l-yl) oxy]benzoyl] amino-3-methoxy-N-methyl-N- (4-hydroxyphεnyl) bεnzamidε NMR (CDC1 3 , δ) : 1.43 (9H, s) , 1.60-1.68 (2H, m) , 3.16-3.25 (2H, m) , 3.49 (3K, s) , 3.63 (3K, s) , 4.16-4.23 (2H, a), 4.73-4.80 (IH, br) , 6.67-6.74 (3H, a), 6.84-7.01 (5H, a), 7.07-7.14 (2H, a), 7. (IH, t, J=8Hz), 8.16 (IH, d, J=8Hz) , 8.52 (IH, d, J=8Kz) ESI-MASS (a/z) : 550 (M+H) 2) 3-Methoxy-4- [2-[l- (tert-butoxycarbonyl) piperidin-4- yl] oxybenzoyl] aaino-N- (2-hydroxy-4-aethyi)phεnyl-N- aethylbenzaaide NMR (CDCI3, δ) : 1.43 (9H, s) , 1.68-2.10 (4H, a), 2.2 (3H, ε), 2.96-3.17 (2H, a), 3.36 (3H, ε), 3.64-3. (5H, a), 4.60 (IH, a), 6.36-7.03 (7K, a), 7.10 (I t, J=7Hz), 7.43 (IH, t, J=7Hz) , 8.19 (IH, d, J=7 3) 4- [2- (3-Amino-l-methylprop-l-yl) oxybenzoyl] amino-3- mεthoxy-N- (2-hydroxy-4-mεthyl)phεnyl-N-mεthylbenzamide NMR (DMSO-dg, δ) : 1.33 (3H, d, J=7.5Hz), 1.63-1.76 (IH, m), 1.87-1.98 (IH, m) , 2.14 (3K, ε), 2.65 (2K t, J=7.5Hz), 3.18 (3H, ε), 3.74 (3K, ε) , 4.96 (IH, a), 6.47 (IH, d, J=7Hz) , 6.63 (IH, ε) , 6.86 (IH, d J=7Hz), 7.91 (IK, d, J=7Hz), 7.01 (IH, ε) , 7.09 (IK, t, J=7Hz), 7.32 (IH, d, J=7Hz) , 7.52 (IH, t, J=7Hz), 8.04 (IH, d, J=7Hz), 8.30 (IH, d, J=7Hz) 4) 3-Methoxy-4- [2- [3- (tert-butoxycarbonyl) amino-1- mεthylprop-1-yl ] oxybenzoyl ] amino-N- (2-hydroxy-4- methyl ) phenyl-N-mεthylbenzamide NMR (CDC1 3 , δ) : 1.36 (3H, d, J=7.5Hz), 1.40 (9H, ε) , 1.80-2.10 (2H, m) , 2.22(3H, ε) , 3.16-3.28 (2H, m) , 3.35 (3H, s), 3.69 (3H, s), Δ.64 (IH, m) , 4.79 (IH, br), 6.52 (IH, a), 6.70-6.82 (2H, a), 6.91-7.11 (4H, a), 7.41 (IH, t, J=7Hz), 8.21 (IH, d, J=7Hz) , 8.47 (IK, a) 5) 4- (2-Hydroxybenzoylaaino-3-aethoxy-N- (2-hydroxy-4- aethylphenyl) -N-aethylbenzamide NMR (CDCI3, δ) : 2.26 (3H, s), 3.36 (3H, s), 6.56 (IK, a), 6.65-6.86 (4H, m) , 6.96-7.08 (2H, m) , 7.35-7.4 (2H, a), 8.20 (IH, br) , 8.61 (IH, br) 6) 4- [2- [3- (tert-Butoxycarbonylaaino)prop-l-yl]oxybenzoyl] amino-3-methoxy-N- (2-hydroxy-4-methylphenyl) -N- methylbεnzamide NMR (CDCI3, δ) : 1.42 (9H, s) , 1.68 (2K, br) , 1.99 (2K, br), 2.22 (3H, s) , 3.19 (2H, br) , 3.39 (3H, S), 3.49 (2H, br), 5.03 (IK, br) , 6.43-6.72 (6H, a), 7.08 (2H, br) , 7.39 (IH, br) , 8.21 (IH, d, J=8Hz), 8.45 (IH, br) Example 54 The following compounds werε obtainεd according to a similar mannεr to that of Examplε 12. 1) 4-[2-[ (3-tert-Butoxycarbonylaminoprop-l-yl)oxy]benzoyl] amino-3-methoxy-N-methyl-N-[4-(5-ethoxycarbonylpent-l- yloxy)phenyl]benzamide NMR (CDC1 3 , δ) : 1.21-1.29 (3H, a), 1.40 (9H, s) , 1.42-1.90 (8H, a), 2.09-2.19 (2H, m) , 3.27-3.34 (2H, m), 3.47 (3H, s) , 3.82 (3H, ε) , 3.89 (2H, t, J=8Hz), 4.08-4.17 (2H, m) , 4.26 (2H, t, J=8Hz) , 4.70-4.77 (IH, br) , 6.75 (2H, d, J=8Hz) , 6.83 (IH, d, J=8Hz), 6.94-7.02 (3H, m) , 7.07-7.13 (2H, m) , 7.46 (IH, t, J=8Hz), 8.21 (IH, d, J=8Hz) , 8.42 (I d, J=8Hz) ESI-MASS (m/z) : 692 (M+H) 2) 4-[2-Bεnzyloxy)bεnzoyl]amino-N-[2- (3-εthoxycarbonylpro 1-yl)oxy]phenyl-N-methylbεnzamidε NMR (CDC1 3 , δ) : 1.26 (3H, t, J=7.5Hz), 2.03-2.17 (2H m), 2.50 (2H, t, J=7.5Hz), 3.32 (3H, ε) , 3.87-4.0 (2H, ) , 4.16 (2H, q, J=7.5Hz), 5.19 (2H, s), 6.7 (2H, d, J=8Hz), 6.92-7.00 (3H, m) , 7.07-7.21 (5H, m) , 7.38-7.53 (6H, m) , 8.26 (IH, d, J=7Hz) 3) 4- (2-Iodobenzoyl)amino-N-[2-(5-ethoxycarbonylpεnt-l- yl)oxy]phenyl-N-methylbenzamide NMR (CDCl- _a ■ , δ) : 1.24 (3H, t, J=7.5Hz), 1.42-1.55 (2H m), 1.63-1.72 (2H, m) , 1.76-1.88 (2H, m) , 2.31 (2 t, J=7.5Hz), 3.31 (3K, s) , 3.81-3.99 (2H, a), 4.1 (2K, q, J=7.5Hz), 6.76-6.83 (2H, a), 7.00 (IH, d, J=7Hz), 8.08-7.17 (2H, a), 7.29-7.49 (5H, a), 7.6 (IK, s), 7.88 (IH, d, J=7Hz) 4) 3-Methoxy-4-[2-[3-(tert-butoxycarbonyl)aainoprop-1-yl] oxybenzoyl] amino-N- [2- [3- (tert-butoxycarbonyl) aminoprop l-yl]oxy-4-methyl]phenyl-N-methylbεnzamidε NMR (CDC1 3 , δ) : 1.39 (9H, s) , 1.41 (9H, ε), 1.93-1.97 (2H, m), 2.07-2.17 (2H, m) , 2.26 (3H, ε), 3.22-3.3 (4K, a), 3.30 (3H, ε), 3.78 (3H, ε) , 3.82-4.05 (2H, a), 6.60-6.66 (2H, a), 6.86-6.91 (2K, a), 7.00 (IH, d, J=7Hz), 7.03-7.10 (2H, a), 7.43 (IH, t, J=7Hz) , 8.20 (IH, d, J=7Kz), 8.39 (IH, d, J=7Hz) 5) 3-Mεthoxy-4- [2- [3- (tert-butoxycarbonyl) aainoprop-1- yl] oxybenzoyl] aaino-N-aεthyl-N- [4-aethyl-2- [4- (phthaliaido)but-l-yl] oxy]phεnylbenzaaidε NMR (CDCI3, δ) : 1.40 (9H, ε) , 1.85-1.92 (2K, a), 2.10-2.17 (2K, a), 2.27 (3H, s) , 3.22-3.32 (2H, a), 3.28 (3H, s) , 3.74-3.81 (2H, a), 3.81 (3H, s) , 3.92-4.15 (2H, a), 4.24 (2H, t, J=7.5Hz), 6.57-6.65 (2H, a), 6.83-6.90 (2H, a), 6.97-7.14 (3H, a), 7.24 (IH, t, J=7Hz), 7.69-7.77 (2H, a), 7.82-7.91 (2H, a), 8.21 (IH, d, J=7Hz), 8.40 (IH, d, J=7Hz) 6) 3-Mεthoxy-4- [2- [1- (tert-butoxycarboyl) piperidin-4- yl]oxybεnzoyl] aaino-N- [2- (5-εthoxycarbonylpεnt-l-yl) oxy- 4-aethyl]phenyl-N-aethylbenzaaidε NMR (CDCI3, δ) : 1.25 (3H, t, J=7.5Hz), 1.42-1.91 (6H, a), 1.45 (9H, s), 2.02 -2.12 (2H, a), 2.27 (3H, ε), 2.27-2.88 (2H, a), 2.97-3.18 (2H, a), 3.32 (3H, s), 3.40 (2H, t, J=7Hz), 3.74 (3H, s), 3.89-4.00 (2H, m), 4.13 (2H, q, _=7.5Hz), 4.66 (IH, m) , 6.59 (IH, d, J=7Hz), 6.61 (IH, ε, J=7Hz), 6.80-6.92 (2H, a), 6.98-7.12 (3H, a), 7.43 (IH, t, J=7Hz) , 8.19 (IH, d, J=7Hz), 8.39 (IH, d, J=7Hz) 7) 3-Mεthoxy-4- [2- [3- (tert-butoxycarbonyl) amino-1-methyl- prop-1-yl]oxybenzoyl]amino-N- [2- (5-ethoxycarbonylpent-l- yl)oxy-4-methyl]phεnyl-N-mεthylbenzamide NMR (CDCI3, δ) : 1.24 (3H, t, J=7.5Hz), 1.38 (9H, s) , 1.40 (2H, d, J=7.5Hz), 1.41-2.10 (8H, m) , 2.26 (3K s), 2.27-2.33 (2H, m) , 3.23-3.30 (2H, a), 3.30 (3H s), 3.79 (3K, s), 3.83-3.99 (2H, a), 4.12 (2H, q, J=7.5Hz), 4.62-4.77 (2H, a), 6.58-6.63 (2H, a), 6.82 (IH, t, J=7Hz), 7.01 (IH, d, J=7Hz) , 7.05-7.1 (2H, m) , 7.43 (IH, t, J=7Hz), 8.21 (IH, d, J=7Hz) , 8.39 (IH, d, J=7Hz) 8) 4-[2-[3-(tert-Butoxycarbonylamino)prop-l-yl]oxybεnzoyl] amino-3-methoxy-N-(2-methoxy-4-methylphenyl)-N- methylbenzamide NMR (CDCI3, δ) : 1.40 (9H, ε), 2.08-2.20 (2H, m) , 2.29 (3H, ε), 3.28 (2H, q, J=5Hz) , 3.31 (3H, ε), 3.75 (3H, s), 3.80 (3K, s), 4.25 (2H, t, J=5Hz) , 4.74 (IH, br) , 6.59-6.65 (2H, a), 6.89 (IH, d, J=8Hz) , 7.00 (IH, d, J=8Hz), 7.06-7.13 (2K, a), 7.46 (IH, dd, J=2, 8Hz) , 8.21 (IH, d, J=8Hz), 8.40 (IH, d, J=8Hz) 9) 4-[2-[3-(tert-Butoxycarbonylamino)prop-l-yl]oxybenzoyl] amino-3-methoxy-N-[2-[4- (2-pyridyl)phenylmethyl]oxy-4- methylphenyl]-N-methylbεnzamide NMR (CDCI3, δ) : 1.39 (9H, s) , 2.09 (2H, t, J=5Hz) , 2.29 (3H, s), 3.27 (2H, q, J=5Hz) , 3.40 (3H, s) , 3.61 (3H, s), 4.21 (2H, t, J=5Hz) , 4.82 (IH, br) , 4.97 (IH, d, J=12Hz), 5.14 (IH, d, J=12Hz) , 6.55- 6.74 (2H, m) , 6.89-7.12 (7H, a), 7.19-7.24 (IH, a 7.39 (IH, d, J=8Hz), 7.41-7.49 (IH, a), 7.70 (2H, s), 7.99 (IH, d, J=8Kz), 8.21 (IH, d, J=8Hz) , 8.4 (IH, d, J=8Hz), 8.67 (IH, d, J=5Hz) 10) 4-[2-[3-(tert-Butoxycarbonylamino)prop-1-yl]oxybenzoyl amino-3-methoxy-N-[2-[4-(1,5-dimεthyl-3-cyanopyrrol-2- yl)phenylmethyl]oxy-4-methylphenyl)-N-methylbεnzamide NMR (CDCI3, δ) : 1.40 (9H, s) , 2.03-2.15 (2H, m) , 2.1 (3H, ε), 2.30 (3H, ε) , 3.26 (2H, q, J=5Hz) , 3.40 (3H, ε), 3.46 (3K, ε), 3.58 (3H, ε), 4.19 (2H, t, J=5Hz), 4.86 (IH, d, J=12Hz) , 5.10 (IH, d, J=12Kz) , 6.65-6.73 (2H, a), 6.82 (IH, d, J=8Hz) , 6.95-7.10 -(4K, a), 7.34-7.44 (6H, a), 8.00 (IH, ε) , 8.19 (IH, d, J=8Hz), 8.36 (IH, d, J=8Hz) 11) 4-[2-[3- (tert-Butoxycarbonylaaino)prop-l- yl]oxybenzoyl]amino-3-methoxy-N-[2-[4- (thiazol-2- yl)phεnylmethyl]oxy-4-methylphenyl]-N-mεthylbεnzamidε NMR (CDC1 3 , δ) : 1.40 (9K, ε) , 2.05-2.16 (2H, m) , 3.27 (2H, q, J=5Hz), 3.40 (3H, ε) , 3.62 (3H, ε), 4.20 (2H, t, J=5Hz), 4.76 (IH, br) , 4.89 (IH, d, J=12Hz), 5.07 (IH, d, J=12Hz) , 6.62-6.72 (2H, m) , 6.89 (IK, d, J=8Hz), 6.96-7.11 (4H, m) , 7.28 (IH, d, J=3Hz), 7.31 (2H, d, J=8Hz) , 7.42 (IH, dd, J=2, 8Hz), 7.81 (IH, d, J=8Hz) , 7.93 (2H, d, J=8Hz) , 8.00 (IH, ε), 8.20 (IH, d, J=8Hz) , 8.38 (IH, d, J=8Hz) 12) 4-[2-[3- (tert-Butoxycarbonylamio) ' prop-l- yl]oxybenzoyl]amino-3-methoxy-N-[2-[4- (oxazol-2- yl)phenylmethyl]oxy-4-methylphεnyl]-N-mεthylbεnzamide NMR (CDCI3, δ) : 1.40 (9H, ε) , 2.05-2.16 (2H, m) , 2.29 (3H, ε), 3.27 (2H, q, J=5Hz) , 3.40 (3H, ε) , 3.65 (3H, ε), 4.21 (2H, t, J=5Hz) , 4.78 (IH, br) , 4.90 (IH, d, J=13Hz), 5.10 (IH, d, J=13Hz) , 6.64 (IH, ε), 6.70 (IH, d, J=8Hz), 6.85 (IH, d, J=8Hz) , 6.98- 7.17 (5H, m) , 7.20 (IH, ε) , 7.30-7.49 (3H, m) , 7.63 (IH, s), 8.03 (IH, d, J=8Hz) , 8.22 (IH, d, J=8Hz), 8.40 (IH, d, J=8Hz) 13) 4-[2-[3- (tert-Butoxycarbonylamino)prop-l- yl]oxybenzoyl]amino-3-methoxy-N-[2-[4-(pyrimidin-2- yl)phenylmethyl]oxy- -methylphεnyl]-N-mεthylbεnzamide NMR (CDCI3, δ) : 1 .4C (9H, s) , 2 . 05-2 . 16 (2H, m) , 2 .28 (3H, s) , 3.28 (2H, q, J=5Kz) , 3.40 (3H, s) , 3.65 (3H, ε) , 4 .22 (2H, t, J=5Kz) , 4 .78 (IH, br) , 4 .95 ( IH, d, J=12Hz) , 5. 14 (IH, d, J=12Hz) , 6. 65-6.70 (2H, m) , 6. 88 (IH, d, J=8Hz) , 6.96-7 . 19 (5H, m) , 7 .38-7 .46 (3H, a) , 8.21 (IH, d, J=8Hz) , 8 .35-8 .44 (3H, a) , 8 .74 (IH, d, J=3Kz) 4 ) 4- [2- [3- (tert-Butoxycarbonylamino) prop- 1-yl ] oxybenzoyl ] amino-3-methoxy-N- [2- (4-cyanophenylmethyl) oxy-4- methylphεnyl ] -N-methylbenzamide NMR (CDCI3, δ) : 1.41 (9K, s), 2.08-2.20 (2H, a) , 2.3 (3H, s), 3.30 (2K, q, J=5Hz) , 3.40 (3H, s) , 3.68 (3H, s), 4.26 (2H, t, J=5Kz) , 4.89 (IH, d, J=13Hz) 5.09 (IH, d, J=13Hz), 6.60 (IH, s) , 6.73 (IH, d, ϋ=8Hz), 6.98-7.12 (5H, m) , 7.39-7.52 (3H, m) , 7.6 (IH, d, J=8Hz), 8.20 (IK, d, J=8Hz) , 8.34 (IH, d, J=8Hz) 15) 4-[2-[3- (tert-Butoxycarbonylamino)prop-1- yl]oxybenzoyl]aaino-3-aethoxy-N-[2-(4-phthaliaidobut-l yl)oxy-4-aethylphεnyl]-N-aεthylbenzamide NMR (CDCI3, δ) : 1.40 (9H, s), 1.72-1.95 (4H, m) , 2.08-2.19 (2H, m) , 2.29 (3K, s) , 3.31 (2H, q, J=5Hz), 3.33 (3K, s) , 3.79 (2H, t, J=5Hz), 3.81 (3H, s), 3.84-4.06 (2H, m) , 4.25 (2K, t, J=5Hz) , 4.82 (IH, br), 6.57 (IH, d, J=8Hz) , 6.62 (IH, s) , 6.81-6.89 (2H, a)", 6.97 (IH, d, J=8Hz) , 7.04-7.10 (2H, m), 7.40-7.48 (IK, ) , 7.68-7.74 (2K, m) , 7.81-7.89 (2H, a), 8.20 (IK, d, J=8Hz) , 8.39 (IH, d, J=8Hz) 16) 4-[2-[3-(tert-Butoxycarbonylamino)prop-1-yl]oxybenzoyl amino-3-methoxy-N-[2-(3-methoxycarbonylpyrid-6- yl)methoxy-4-methylphenyl]-N-methylbenzamide NMR (CDC1 3 , δ) : 1.39 (9H, ε), 2.07-2.16 (2H, a), 2.27 (3H, s), 3.29 (2H, q, J=5Hz) , 3.42 (3H, s) , 3.63 (3H, s), 3.89 (3H, s) , 4.24 (2H, t, J=5Hz) , 4.95 (IH, d, J=12Hz), 5.08 (IH, d, J=12Hz) , 6.58 (IH, s), 6.73 (IH, d, J=8Hz), 6.89 (IH, d, J=8Hz) , 6.98 (2H, d, J=8Hz), 7.05-7.12 (3H, a), 7.34 (IH, d, J=8Hz), 7.44 (IH, dd, J=2, 8Hz) , 8.20 (IH, d, J=8Hz), 8.28 (IH, d, J=8Hz) , 8.37 (IH, d, J=8Hz) , 9.14 (IH, s) Example 55 The following compound was obtained according to a similar manner to that of Example 35. 4-[2-[3- (tert-Butoxycarbonylamino)prop-l-yl]oxybεnzoyl- amino-3-methoxy-N-[2-[4- (tert-butoxycarbonylguanidino)but-l- yl]oxy-4-methylphenyl]-N-mεthylbεnzamidε NMR (CDCI3, δ) : 1.43 (9H, s) , 1.44 (9H, s), 1.52-1.60 (2H, m) , 1.65-1.74 (2H, m) , 1.92-2.07 (2H, ) , 2.21 (3H, ε), 3.10-3.25 (4H, m) , 3.38 (3H, s) , 3.50 (2H, br), 3.66 (3H, br) , 3.78-4.05 (2H, a), 6.49 (2H, br) , 6.63-6.82 (3H, a), 7-01-7.10 (2K, a), 7.38 (IH, dd, J=2, 8Hz), 8.20 (IH, d, J=8Hz) , 8.44 (IH, br) Exaaple 56 The following coapoundε werε obtained according to a siailar aanner to that of Example 10. 1) 4-[2-[ (3-tert-Butoxycarbonylaminoprop-l-yl)oxy]benzoyl]- amino-3-hydroxy-N-methyl-N-cyclohexylbenzamide NMR (CDCI3, δ) : 1.07-1.17 (2H, a),- 1.41 (9H, s), 1.47-1.76 (8H, a), 2.10-2.20 (2H, a), 2.92-3.00 (2H, a), 3.36-3.44 (2H, a), 3.49 (3H, ε), 4.19-4.27 (2H, a), 4.98-5.06 (IH, br) , 6.87-6.92 (IH, br) , 6.98-7.03 (2H, a), 7.12 (IH, t, J=8Hz) , 7.47 (IH, - 222 - t, J=8Hz), 8.12-8.22 (IH, br) , 8.28 (IH, d, J=8Hz) 9.72-9.80 (IH, br) ESI-MASS (m/z) : 526 (M+H) 2) 4-[2-[ (3-tert-Butoxycarbonylaminoprop-l-yl)oxv]benzoyl] amino-3-hydroxy-N-methyl-N-[2-[5-(4-methylpiperazin-l- yl)carbonylpεnt-l-yloxy]-4-mεthylphεnyl]benzamide NMR (CDC1 3 , δ) : 1.42 (9H, s) , 1.50-1.90 (8H, m) , 2.20-2.22 (2K, a), 2.27 (3H, s) , 2.32 (3H, s), 2.35-2.53 (6H, a), 3.29 (3H, ε), 3.32-3.42 (2H, a) 3.50-3.66 (3H, a), 3.72 (2H, br) , 3.89 (IK, br), 4.20 (2H, t, J=6Hz), 5.29 (IH, br) , 6.54 (IH, s), 6.67 (IH, d, J=7Hz), 6.72 (IH, br) , 6.96-7.10 (4H, a), 7.40-7.47 (IH, a), 8.10 (IH, br) , 8.27 (IH, d, J=6Hz) Example 57 To a solution of 4-[ (2-benzyloxy)benzoyl]amino-3-[ (2- benzyloxy)bεnzoyl]oxy-N-methyl-N-[2-[5-(4-methylpiperazin-l- vl)carbonylpent-l-yloxy]-4-methylphenyl]benzamide (1.2 g) i ethanol (20 ml) was added IN εodium hydroxide εolution (10 ml) and the mixture waε stirred at ambient temperature for hours. The mixture was concentrated in vacuo and the solution was adjusted to pH 7 with IN hydrochloric acid. T solution was extracted with ethyl acetate (20 ml) and the organic layer was washed with brine (20 ml) . The organic layer was dried over magnesium sulfate and the solution was concentrated in vacuo to give 4-[ (2-benzyloxy)benzoyl]amino 3-hydroxy-N-methyl-N-[2-[5-(4-methylpiperazin-l- yl)carbonylpent-l-yloxy]-4-mεthylphεnyl]bεnzamidε (930 mg) NMR (CDCI3, δ) : 1.48-1.59 (2H, a), 1.70 (4H, br) , 2.29-2.42 (13H, a), 3.29 (3H, s) , 3.48 (2H, br) , 3.53 (2H, br), 3.80 (IH, br) , 3.90 (IH, br) , 5.28 (2H, s), 6.53-6.65 (3H, m) , 6.72 (IH, br) , 6.90- 7.12 (4H, m), 7.34-7.37 (3H, m) , 7.40-7.49 (4H, m 8.20-8.27 (IH, a) Example 58 The following compoundε were obtained according to a εimilar manner to that of Example 12. 1) 4-[2-[ (3- ert-Butoxycarbonylaainoprop-1-yl)oxy]benzoyl] amino-3-ethoxycarbonylmethoxy-N-methyl-N- cyclohexylbenzamide NMR (CDC1 3 , δ) : 1.29 (3H, t, J=8Hz) , 1.41 (9H, ε), 1.45-1.85 (10H, m) , 2.07-2.12 (2H, m) , 2.86-3.06 (3K, br), 3.25-3.32 (2K, m) , 4.22-4.33 (4H, m) , 4.76 (2H, s), 4.98-5.07 (IH, br) , 6.91 (IH, s) , 7.01-7.15 (3H, m) , 7.48 (IH, t, J=8Hz) , 8.23 (IH, d, J-8HZ), 8.69 (IH, d, J=8Hz) ESI-MASS (m/z) : 634 (M+Na) 2) 4- [2- [ (3-tert-Butoxycarbonylaminoprop-l-yl)oxy]benzoyl] amino-3-isopropoxy-N-mεthyl-N- [2-[5- (4-mεthylpipεrazin- 1-yl) carbonylpent-l-yloxy]-4-mεthylphεnyl]benzamide NMR (CDCI3, δ) : 1.19-1.28 (6H, a), 1.38 (9H, ε) , 1.46-1.58 (2H, a), 1.65-1.88 (6H, a), 1.99-2.10 (2H, π), 2.25 (3H, ε), 2.29 (3H, ε), 2.32-2.42 (6H, a), 3.15-3.23 (2H, a), 3.31 (3H, s) , 3.45-3.50 (2H, a), 3.60-3.64 (2H, a), 3.84-3.97 (2H, a), 4.24-4.3 (3H, a), 6.56-6.65 (2H, a), 6.85 (IH, d, J=7Hz), 6.94-7.02 (3H, a), 7.10 (IH, t, J=6Hz) , 7.47 (IH, t, J=7Hz), 8.15 (IH, d, J=7Hz) , 8.41 (IH, d, J=7Hz) 3) 4- [2- [ (3-tert-Butoxycarbonylaminoprop-l-yl)oxy]benzoyl] amino-N-mεthyl-N- [2-[5- (4-mεthylpipεrazin-l-yl) carbonyl pent-l-yloxy]-4-methylphenyl]-3-propoxybenzamide NMR (CDCI3, δ) : 0.97 (3H, t, J=7Hz) , 1.42 (9H, ε) , 1.47-1.58 (2H, m) , 1.67-1.88 (8K, a), 1.98-2.10 (2H, a), 2.27 (3H, s) , 2.28 (3H, s) , 2.31-2.41 (6H, 5 m), 3.16-3.26 (2H, m) , 3.31 (3H, s) , 3.45-3.50 (2 m) , 3.58-3.65 (2K, a), 3.84-3.97 (4H, m) , 4.26 (2 t, J=7Hz), 6.58 (IH, d, J=7Hz) , 6.64 (IH, s), 6.8 (IH, d, J=6Hz), 6.95 (IK, d, J=7Hz) , 6.99-7.03 (2 m), 7.09 (IH, t, J=7Hz), 7.45 (IH, t, J=7Hz) , 8.1 (IH, d, J=7Hz), 8.38 (IH, d, J=7Hz) 4) 4-[2-[ (3-tert-Butoxycarbonylaminoprop-l-yi)oxy]benzoyl] amino-3-(3-ethoxycarbonylprop-l-yl)oxy-N-methyl-N-[2-[ (4-methylpipεrazin-l-yl)carbonylpent-l-yloxy]-4- methylphenyl]benzamide NMR (CDCl-a, δ) : 1.11 and 1.23 (total 3H, t, J=6Hz) , 1.40 (9H, s), 1.48-1.60 (2H, a), 1.60-1.75 (4H, a 1.75-1.88 (2H, a), 1.98-2.10 (4H, a), 2.26 (3K, ε 2.29 (3H, s), 2.32-2.42 (8K, a), 3.18-3.28 (2H, a 3.30 (3H, s), 3.45-3.50 (2K, a), 3.62 (2H, br) , 3.88-4.10 (5H, a), 4.27 (2H, t, J=6Hz) , 6.57 (IH, d, J=7Hz), 6.63 (IK, s) , 6.82 (IH, d, J=7Hz) , 6.8 6.92 (IH, a), 6.98-7.10 (3H, a), 7.42 (IH, t, J=6Hz), 8.10-8.13 (IK, a), 8.37 (IH, d, J=7Hz) 5) 4-[2-[ (3-tert-Butoxvcarbonylaainoprop-l-yl)oxy]- benzoyl]aaino-3-ethoxycarbonylaethoxy-N-aethyl-N-[2-[5 (4-aethyloiperazin-l-yl)carbonylpent-l-yloxy]-4- aethylphenyl]bεnzaaide NMR (CDC1 3 , δ) : 1.29 (3K, t, J=7Hz) , 1.39 (9H, s) , 1.46-1.90 (8H, a), 2.00-2.10 (2K, a), 2.28 (3H, 2.29 (3H, ε), 2.30-2.42 (6H, a), 3.18-3.29 (2H, 3.30 (3H, ε), 3.42-3.50 (2H, a), 3.58-3.65 (2H, 3.85-3.97 (2H, a), 4.18-4.29 (4H, a), 4.52 (2H, 6.52-6.13 (2K, a), 6.80 (IH, d, J=7Hz), 6.89-6.9 (3H, a), 7.38-7.48 (IH, a), 8.15 (IH, d, J=7Hz) , 8.41 (IH, d, J=7Hz) 6) 4-[ (2-Benzyloxy)benzoyl]amino-3-ethoxyl-N-methyl-N-[2 [5- (4-methylpipεrazin-l-yl)carbonylpεnt-1-yloxy]-4- methylphenyl]benzamidε NMR (CDC1 3 , δ) : 1.08 (3H, t, J=6Hz) , 1.45-1.57 (2H, a), 1.60-1.75 (2H, a), 1.77-1.87 (2H, a), 2.25 (3H, s), 2.29 (3H, s), 2.31-2.39 (7H, a), 3.30 (3H, s) , 3.46-3.49 (2H, a), 3.60-3.63 (2H, a), 3.70-3.80 (2K, a), 3.82-3.98 (2K, a), 5.34 (2H, s) , 6.52-6.6 (2H, a), 6.80-7.10 (5H, a), 7.27-7.38 (6H, a), 8.20-8.22 (IH, a), 8.38-8.43 (IH, m) Example 59 The following compounds were obtained according to a similar manner to that of Example 4. 1) 4-[2-[ (3-tert-Butoxycarbonylaainoprop-l-yl)oxy]bεnzoyl]- amino-3-carboxymethoxy-N-methyl-N-cyclohεxylbεnzamidε NMR (CDCI3, δ) : 1.03-1.17 (2H, a), 1.39 (9H, s) , 1.45-1.85 (8H, a), 2.03-2.12 (2H, a), 2.85-2.98 (3K, a), 3.21-3.33 (2H, a), 4.23-4.31 (2H, a), 4.73 (3H, s), 5.08-5.13 (IH, br) , 6.98-7.07 (3H, a), 7.10 (IH, t, J=8Hz), 7.48 (IH, t, J=8Hz), 8.18-8.24 (IH, a), 8.56-8.61 (IH, a) ESI-MASS (a/z) : 606 (M+Na) 2) 4-[2-[ (3-Aainoprop-l-yl)oxy]benzoyl]aaino-3- carboxyaethoxy-N-aethyl-N-[2-[5- (4-aethylpiperazin-l- yl)carbonylpεnt-l-yloxy]-4-aεthylphεnyl]benzaaide dihydrochloride NMR (DMSO-dg, δ) : 1.38-1.49 (2H, a), 1.49-1.62 (2H, a), 1.67-1.78 (2H, m) , 2.02-2.34 (13H, a), 2.78- 2.89 (2H, a), 3.38-3.43 (4H, a),..3.58 (3H, s) , 3.89-3.96 (2H, a), 4.00-4.18 (2H, a), 4.30 (2H, br), 6.62 (IH, d, J=6Hz) , 6.72-6.87 (3H, a), 6.89- 6.97 (IH, a), 7.11 (IH, t, J=7Hz) , 7.19 (IH, d, J=7Hz) 7.54 (IH, t, J=6Hz) , 7.94 (IK, d, J=6Hz) , 95 - 226 - 8.22 (IH, d, J=7Hz) 3) 4-[2-[(3-tert-Butoxycarbonylaainoprop-l-yl)oxy]benzoyl] amino-3-carboxymεthoxy-N-mεthyl-N-[2-[5-(4- mεthylpipεrazin-1-yl)carbonylpεnt-l-yloxy]-4- methylphenyl]benzamide MASS (m/z) : 804 (M+H) Example 60 To a mixture of 4-(2-iodobenzoyl)amino-N-mεthyl-N-[2-[ (4-methylpiperazin-l-yl)carbonylpεnt-l-yl]oxy]phεnylbεnzami (1.12 g) and 3-butyn-l-ol (153 mg) in a mixture of tetrahydrofuran (15 ml) and ethyla ine (15 ml) were added bis(triphenylphoεphine)palladiu (II) chloride (23.5 mg) and copper (I) iodide (3.19 mg) and the mixture was refluxed fo 8 hours. The solution was diluted with chloroform (50 ml) and the solution was washed with water and brine. The solution was dried over magnesium sulfate and the solvent w evaporated in vacuo to give an oil. The oil was purified b silica gεl column (2% methanol in chloroform) to give 4-[2- (4-hydroxy-I-butyn-l-yl)benzoyl]aaino-N-aethyl-N-[2-[5- (4- aethylpiperazin-1-yl)carbonylpent-1-yl]oxy]phenylbenzaaide (755 mg) . NMR (CDC1 3 , δ) : 1.44-1.57 (2H, m) , 1.61-1.86 (4H, a) 2.27 (3H, s) , 2.29-2.40 (6H, a), 2.70 (2H, t, J=7.5Hz), 3.33 (3H, s) , 3.44-3.49 (2H, a), 3.53- 3.60 (2H, a), 3.74 (2H, t, J=7.5Hz), 3.79-3.99 ( a), 6.76-6.84 (2H, . a) , 7.06 (IK, d, J=7Hz), 7.13 (IH, t, J=7Hz), 7.34 (2H, d, J=8Hz) , 7.40-7.47 ( a), 7.48-7.56 (3H, a), 7.99 (IH, a), 9.19 (IH, s) Example 61 To an icε cooled solution of 4-[2-(4-hydroxy-1-butyn- yl)benzoyl]aaino-N-aethyl-N-[2-[5-(4-methylpiperazin-l- yl)carbonylpent-1-yl]oxy]phenylbenzaaide (755 ag) in 1795 - 227 - dichloromethane (20 ml) were added triethylamine (150 mg) an ethanεsulfonyl chloride (156 mg) , and the mixture was stirred in an ice bath for 2 hours. The solution was washed succesεively with water, 10% hydrochloric acid, saturated aqueous sodium hydrogen carbonate and brine, and the organic phase was dried over magnesium sulfate. The solvent was evaporated in vacuo to givε 4-[2- (4-methanεεulfonyloxy-l- butyn-l-yl)bεnzoyl]amino-N-mεthyl-N-[2-[5- (4-methylpiperazin 1-yl) carbonylpent-l-yl]oxy]phenylbεnzamide (789 mg) . NMR (CDC1 3 , δ) : 1.49-1.60 (2H, m) , 1.67-1.86 (2K, m) , 1.87-1.90 (2H, m), 2.37 (2H, t, J=7.5Hz), 2.68 (3H s), 2.86-3.06 (6H, m) , 2.92 (3H, s) , 3.31 (3H, s) , 3.77-4.02 (6H, m) , 4.32 (2H, t, J=7.5Hz), 6.77-6.8 (2K, m) , 7.04 (IK, d, J=7Hz), 7.17 (IH, t, J=7Hz), 7.32 (2H, d, J=8Hz) , 7.41-7.53 (5H, m) , 7.90 (IH, a), 8.86 (IH, s) Exaaple 62 The following coapounds werε obtainεd according to a siailar aannεr to that of Exaaplε 61. 1) 4- [2- (4-Mεthanesulfonyloxybut-l-yl)benzoyl] amino-N- methyl-N- [2- [5- (4-methylpiperazin-l-yl)carbonylpent-1- yl]oxy]phεnylbεnzamidε MASS (m/z) : 693 (M+l) 2) 4- [2- (3-Methanesulfonyloxyprop-l-yl) thiobenzoyl]amino-3 methoxy-N-methyl-N- [4-methyl-2- [5- (4-methylpiperazin-l- yl)carbonylpent-l-yl]oxy]ohenylbεnzamide NMR (CDCI3, δ) : 1.48-1.60 (2H, m) , 1.65-1.74 (2H, m) , 1.75-1.86 (2H, m) , 1.98-2.07 (2H, m) , 2.26 (3K, s), 2.30-2.39 (2H, m) , 2.70-2.78 (4H, m) , 2.79-3.42 (2H, m) , 2.90 (3H, s) , 2.95-3.07 (2H, m),3.26 (3H, s), 3.71 (3H, s), 3.80-4.01 (4H, m) , 4.29 (2H, t, J=7.5Kz), 6.56-6.66 (2H, a), 6.82-7.00 (3H, m) , 7 .30 (IH, a) , 7 .39-7 .47 (2H, a) , 7. 60 (IH, d, J=7Hz) , 8 .27 (IH, d, J=7Hz) , 8 .58 (IH, s) Exaaole 63 A aixture of 4-[2-(4-aethanεsulfonyloxy-l-butyn-l- yl)bεnzoyl]aaino-N-aεthyl-N-[2-[5-(4-aεthylpipεrazin-l- yl)carbonylpεnt-1-yl]oxy]phenylbenzaaide (800 ag) and potaεεiua phthalimide (430 mg) in dimethyl εulfoxide (20 ml waε stirred at 60 β C for 5 hours, and the solution was dilut with ethyl acetatε (60 ml) . The solution was washed with water and brine, and dried over magnesium sulfate. Thε solvεnt was εvaporated in vacuo to give 4-[2-[4- (phthalimido)-1-butyn-l-yl]benzoyl]amino-N-mεthyl-N-[2-[5-( methylpiperazin-1-yl)carbonylpent-1-yl]oxy]phenylbenzamide (620 mg) . NMR (CDC1 3 , δ) : 1.50-1.61 (2H, a) , 1.67-1.92 (6H, a) 2.30 (3H, s), 2.33-2.44 (6H, a), 3.38 (3H, ε) , 3.48-3.52 (2H, a), 3.60-3.67 (2H, a), 3.84-4.01 (4H, a), 6.78-6.85 (2H, m) , 7.02 (IH, d, J=7Hz) , 7.09-7.19 (2H, a), 7.30-7.70 (6K, a), 7.70-7.77 (2H, a), 7.81-7.90 (2H, a), 8.18 (IH, a) Exaaole 64 Thε following coapounds werε obtained according to a siailar aanner to that of Example 63. 1) 4-[2-[4-(Phthalimido)but-l-yl]benzoyl]amino-N-[2-[5-( mεthylpiperazin-1-yl)carbonylpent-1-yl]oxy]phεnyl-N- mεthylbεnzaaide MASS (m/z) : 693 (M+l) 2) 3-Mεthoxy-4-[2-[3-(phthalimido)prop-1-yl]thiobεnzoyl] amino-N-m thyl-N-[4-mεthyl-2-[5-(4-methylpiperazin-l- yl)carbonylpent-1-yl]oxy]phenylbenzamide NMR (CDCI3, δ) : 1.47-1.59 (2H, m) , 1.61-1.74 (2H, m 1.78-1.87 (2H, a), 1.92-2.03 (2H, a), 2.26 (3H, s) 2.29 (3H, s), 2.31-2.42 (6H, a), 2.94 (2H, t, J=7.5Hz), 3.31 (3H, s) , 3.45-3.53 (2H, a), 3.58- 3.67 (2H, a), 3.69-3.81 (2H, a), 3.73 (3H, s), 3.84-4.00 (2H, a), 6.55-6.66 (2H, a), 6.80-6.92 (2K, a), 7.02 (IH, s), 7.27 (IH, m) , 7.34-7.44 (2 a), 7.60-7.90 (5H, a), 8.25 (IH, d, J=7Hz), 8.82 (IH, s) Example ξ> To an ice coolεd aixturε of 4-[2-(4-aaino-l-butyn-l- yl)bεnzoyl]amino-N-mεthyl-N-[2-[5-(4-mεthylpiperazin-l- yl)carbonylpεnt-l-yl]oxy]phεnylbεnzamidε (310 mg) , nickεl chloride hexahydratε (181 mg) in a mixturε of tεtrahydrofura (5 ml) and mεthanol (5 ml) waε addεd sodium borohydride (96. mg) in small portions and the mixture was stirred at thε sam tempεrature for 2 hours. The mixture was filtered through bed of Celitε and thε filtratε was εvaporatεd in vacuo. Thε rεsiduε was disεolvεd in chloroform (20 ml)and waεhεd with watεr and brinε. The organic εolution waε dried over magnesium sulfate and the solvent was evaporatεd in vacuo to give a syrup. The residue was purified by silica gel column (chloroform.-methanol:ammonia = 100:10:1) to give 4-[2-(4- aminobut-1-yl)benzoyl]amino-N-methyl-N-[2-[5- (4- methylpiperazin-1-yl)carbonylpent-l-yl]oxy]phenylbenzamidε (295 mg) . MASS (m/z) : 597 (M+l) Example 66 The following compound was obtained according to a similar manner to that of Example 65. 4-[2-(4-hydroxybut-l-yl)benzoyl]amino-N-mεthyl-N-[2-[5- (4-mεthylpipεrazin-l-yl)carbonylpent-l-yl]oxy]phenylbεnzamid MASS (m/z) : 615 (M+l) Example 67 A mixture of 4-ammo-3-mεthoxy-N-mεthyl-N-[4-mεthyl-2- [4-(4-methylpiperazin-l-yl)carbonyl]phenylmethoxy]- phenylbenzamide (200 mg) and salicyl aldehydε (48.6 mg) in mεthanol (10 ml) was refluxed overnight in the presence of molecular sieves (100 mg) . The solution was filtered and t filtrate was treated with sodium borohydride (15.1 mg) at 5 for 2 hours. The reaction mixture was diluted with chloroform (20 al) and the solution was washed with water a brine. The organic solution was dried over magnesium sulfa and the solvent was evaporated in vacuo to give a crudε oil The product was purified by silica gel column (2% methanol chloroform) to give 3-aethoxy-4-(2-hydroxyphenyl)aethylaai N-methyl-N-[ -r.ethyl-2-[4-(4-methyipiperazin-l- yl)carbonyl]phenylmethoxy]phenylbenzamide (152 mg) . NMR (CDC1 3 , δ) : 2.27 (3H, s), 2.32 (3H, ε) , 2.32-2. (4K, a), 3.34 (3H, ε), 3.40-3.55 (2H, m) , 3.52 ( ε), 3.75-3.88 (2H, m) , 4.25-4.34 (2H, ) , 4.63 ( br), 4.42 (IH, d, J=14Hz), 5.08 (IH, d, J=14Hz) , 6.43 (IH, d, J=7Hz), 6.62 (IH, s) , 6.70 (IH, d, J«7Hz), 6.80-6.88 (4H, m) , 7.00 (IH, d, J=7Hz) , 7.09-7.18 (2H, m) , 7.28 (2H, d, J=8Hz) , 7.38 (2H d, J-8HZ) Example 68 The following compound was obtained according to a similar manner to that of Example 67. 3-Methoxy-4-(2-hydroxyphenyl)mεthylamino-N-methyl-N-[ methyl-2-[5- (4-methylpiperazin-l-yl)carbonylpent-1- yl]oxy]phenylbenzamide NMR (CDC1 3 , δ) : 1.41-1.52 (2H, m) , 1.60-1.69 (2H, 1.70-1.80 (2K, m) , 2.25 (3H, s) , 2.29 (3H, ε) , 2.30-2.43 (6H, m) , 3.28 (3H, ε) , 3.34-3.48 (2H, 3.55 (3H, s), 3.65-4.00 (2K, m) , 4.30 (2H, d, J=7Hz), 4.62 (IH, br t, J=7Hz) , 6.51 (IH, d, J=7Hz), 6.57-6.64 (2H, m) , 6.76-6.95 (5H, m) , 7.61- 7.68 (2H, a) Example 69 To an ice bath coolεd solution of 4-(2-dimethylamino-4- methyDphenoxymethyl-N-[2-(5-ethoxycarbonylpent-l- yl)oxy]phεnylbenzamide (860 mg) in N,N-dimεthylformamide (15 ml) was added sodium hydride (60% in oil, 71 mg) and the solution was stirrεd at the same temperature for 30 minutes. Iodomethanε (0.121 ml) was addεd to the solution and the mixture was stirred at ambient temperature for 3 hours. The mixture was diluted with εthyl acetate (50 ml) and the solution was washεd with watεr and brinε. Thε organic phasε was driεd over magnesium sulfate and the solvent was evaporated in vacuo to give a crude oil. Thε crudε product was purified by silica gel column chromatography (1% methanol in chloroform) to give 4-(2-dimethylamino-4-mεthyl)- phεnoxymεthyl-N-[2-(5-εthoxycarbonylpent-l-yl)oxy]phenyl-N- methylbεnzamide (632 mg) . NMR (CDC1 3 , δ) : 1.26 (3H, t, J=7.5Hz), 1.42-1.55 (2H, a), 1.63-1.74 (2H, a), 1.76-1.87 (2H, a), 2.20 (3H, s), 2.23 (3H, ε), 2.33 (2H, t, J=7.5Hz), 2.72 (6H, s), 3.30 (3H, s), 3.76-3.97 (2H, a), 4.12 (2H, q, J=7.5Hz), 5.02 (2H, s) , 6.52-6.60 (3H, a), 6.70 (IH, d, J=7Hz), 6.80-6.88 (2H, a), 7.20 (2H, d, J=8Hz), 7.31 (2H, d, J=8Hz) Exaaole 70 The following coapound was obtained by using 3-aethoxy- 4-[2-[3- (tert-butoxycarbonyl)aminoprop-1-yl]oxybenzoyl]amino- N-[2- (4-aminobut-l-yl)oxy-4-methyl]phεnyl-N-mεthylbenzamide as a starting compound according to a similar manner to that of Example 14. 3-Methoxy-4-[2-[3-(tert-butoxycarbonyl)aminoprop-1- yl]oxybenzoyl]amino-N-[2-(4-acetylaminobut-l-yl)oxy-4- mεthyl]phenyl-N-methylbenzamide NMR (CDC1 3 , δ) : 1.40 (9H, ε), 1.65-1.82 (4H, a), 1.7 (3H, ε), 2.05 (3H, s) , 2.07-2.21 (2H, a), 2.26 (3 s), 3.22-3.38 (2H, a), 3.38 (3H, s), 3.77 (3H, s) , 3.77-3.96 (2H, a), 4.24 (2H, t, J=7.5Hz), 6.53-6. (2H, a), 6.93-7.14 (5H, m) , 7.25 (IH, t, J=7Hz) , 8.20 (IH, d, J=7Hz), 8.43 (7H, d, J=7Hz) Example 71 To a mixture of 3-methoxy-4-[2- [3-(tεrt-butoxycarbonyl) aminoprop-1-yl]oxybenzoyl]amino-N-[2-(4-aminobut-l-yl)oxy-4 aethyl]phenyl-N-aethylbεnzaaidε (365 ag) and N-(tεrt- butoxycarbonyl)glycinε (111 mg) in N,N-dim thylformamide (1 ml) were added N-ethyl-N'-(3-dimethylaminopropyl)carbodiimi hydrochloride (132 mg) and hydroxybenzotriazole (93.2 mg) a the mixture was stirred at ambient temperature overnight. The solution was diluted with εthyl acεtatε (30 ml) and thε solution was washεd succeεεivεly with εaturatεd aqueouε εodium hydrogen carbonate, water and brine. The organic phase was dried over magnesium sulfate and the solvent was evaporated in vacuo to give an amorphous. The crude produc was purified by silica gel column chromatography (1% methan in chloroform) to give 3-methoxy-4-[2-[3-tert- butoxycarbonyl)aminoprop-l-yl]oxybεnzoyl]amino-N-[2-4- (tεrt butoxycarbonylamino)acetylaminobut-l-yl]oxy-4-mεthyl]phεnyl N-mεthylbenzamide (320 mg) . NMR (CDCI3, δ) : 1.39 (9H, s), 1.42 (9H, s) , 1.58-1. (2H, a), 1.70-1.80 (2H, a), 2.05-2.17 (2H, a), 2. (3H, ε), 3.20-3.34 (4H, a), 3.30 (3H, s) , 3.70-3. (4H, a), 3.74 (3H, s) , 4.22 (2H, t, J=7.5Hz), 6. 6.68 (2K, a), 6.88-7.11 (5H, a), 7.45 (IH, t, J=7Hz), 8.20 (IK, d, J=7Hz), 8.28 (IH, d, J=7Hz) Example 72 The following compounds were obtained according to a similar manner to that of Example 71. 1) 4-[2-[3-(tert-Butoxycarbonylamino)prop-1-yl]oxybenzoyl] amino-3-methoxy-N-[2-[4-[3- (tεrt-butoxycarbonyl)- aminopropionylamino]but-l-yl]oxy-4-methylphenyl]-N- mεthylbenzamide NMR (CDC1 3 , δ) : 1.40 (9H, s) , 1.41 (9H, s) , 1.60-1.82 (4H, a), 2.10-2.19 (2H, a), 2.29 (3H, s) , 2.48 (2H, br), 3.25-3.42 (6H, m) , 3.32 (3H, s), 3.79 (3H, s), 3.80-3.97 (2H, m) , 4.25 (2H, t, J=5Hz) , 6.59 (IH, s), 6.67 (IH, d, J=8Hz), 6.94-7.11 (5H, m) , 7.45 (IH, dd, J=2, 8Hz), 8.20 (IH, d, J=8Hz) , 8.39 (IH, d, J=8Hz) 2) 4-[2-[3- (tert-Butoxycarbonylamino)prop-1-yl]oxybenzoyl]- amino-3-methoxy-N-[2-[4-[ [1- (tert-butoxycarbonyl)- piperidin-4-yl]carbonylamino]but-1-yl]oxy-4- methylphεnyl]-4-mεthylbεnzamide NMR (CDC1 3 , δ) : 1.40 (9H, ε), 1.44 (9H, ε) , 1.60-1.81 (8H, a), 2.08-2.18 (2H, a), 2.29 (3H, ε), 2.70 (IH, br), 3.30 (2H, q, J=5Hz) , 3.32 (3H, s) , 3.76 (3H, s), 3.76-4.15 (6H, a), 4.22 (2H, t, J=5Hz) , 6.59 (IH, s), 6.65 (IH, d, J=8Hz) , 6.94-7.10 (6H, a), 7.44 (IH, dd, J=2, 8Hz) , 8.20 (IH, d, J=8Hz) , 8.39 (IH, d, J=8Hz) Example 73 To an ice-coolεd mixture of 4-[2-[3-(tert- butoxycarbonylamino)prop-l-yl]oxybεnzoyl]amino-3-methoxy-N- [2- (4-aminobut-l-yl)oxy-4-methylphεnyl]-N-methylbenzamidε (430 mg) and triεthylaminε (68 mg) in dichloromethane (10 ml) was added phenyl chlorocarbonate (106 mg) dropwise and the εolution waε εtirred at the samε tεmoεraturε for 30 minutes. The resulting mixture was diluted with dichloromethane (10 ml) and the solution was washed succesεively with IN hydrochloric acid εaturated aqueous sodium hydrogen carbonat and brine. The solvent was dried over magnesium sulfate and removed under reduced presεure to give 4-[2-[3- (tert- butoxycarbonylamino)prop-1-yl]oxybenzoyl]amino-3-mεthoxy-N- [ (2-(4-phenoxycarbonylaminobut-l-yl)oxy-4-methylphenyl]-N- methylbenzamide (471 mg) . NMR (CDC1 3 , δ) : 1.40 (9H, s), 1.60-1.90 (4H, m) , 2.08-2.17 (2H, m) , 2.29 (3H, s) , 3.27 (2H, q, J=5Hz), 3.31 (2H, t, J=5Hz) , 3.36 (3H, s) , 3.78 (3H, s), 3.82-4.00 (2H, a), 4.21 (2H, t, J=5Hz) , 4.73 (IH, br), 5.38 (IH, br) , 6.61-6.68 (2H, a), 6.91-6.99 (4H, a), 7.06-7.20 (5H, a), 7.30-7.38 (2H, a), 7.42 (IH, dd, J=2, 8Hz), 8.20 (IH, d, J=8Hz), 8.40 (IH, d, J=8Hz) Example 74 A mixture of 4-[2-[3- (tεrt-butoxycarbonylamino)prop-l- yl]oxybεnzoyl]amino-3-methoxy-N-[2-(4-aminobut-l-yl)oxy-4- methylphenyl]-N-methylbenzamide (120 mg) and 3- (dιmethylamino)prop-l-yl phenyl carbonate (127 mg) in N,N- dimethylformamidε (5 ml) waε εtirrεd at 50 β C for 8 hours. Thε reaction mixture was diluted with ethyl acetate (15 ml) and the solution was washed successively with saturated aqueous sodium bicarbonate solution and brine. The solutio was dried cvεr potassium carbonate. The solvent was evaporated and the residue was purified on silica gel colum chromatography (Si0 2 20 g, 3-15% methanol in chloroform) to give 4-[2-[3-(tert-butoxycarbonylamino)prop-1-yl]oxybenzoyl amino-3-methoxy-N-[2-(3-dimethylaminoprop-l-yl)oxycarbonyl- aaino]but-l-yl]oxy-4-aethylphenylJ-N-aethylbenzaaide (64 ag NMR (CDCI3, δ) : 1.40 (9H, s) , 1.62-1.87 (6H, a), 2.05-2.18 (2H, a), 2.28 (3H, s) , 2.30 (6K, s) , 2. (2H, t, J=5Hz), 3.20-3.32 (4H, a), 3.32 (3H, s) , 3.78 (3H, ε), 3.80-4.00 (2H, a), 4.12 (2H, t, J=5Hz), 4.24 (2H, t, J=5Hz) , 6.59-6.64 (2H, a), 6.88-7.12 (5H, a), 7.44 (IH, dd, J=2, 8Hz) , 8.21 (IH, d, J=8Hz), 8.40 (IH, br) Example 75 To a εolution of 4-[2-[ (3-tεrt-butoxycarbonylaainoprop- 1-yl)oxy]bεnzoyl]aaino-3-aethoxy-N-aethyl-N-[2-[5-(4- oxopipεridin-1-yl)carbonylpεnt-l-yl]oxy-4-aethylphenyl]- bεnzamidε (192 mg) in mεthanol (5 ml) waε added εodium borohydride (19 mg) at ambiεnt tεmperature and the mixturε was εtirrεd at the same temperatε for 1 hour. Thε rεaction was quenched with 0.5N hydrochloric acid (10 ml) and the aixture was extractεd with chloroform (15 ml x 3) . Thε organic layer was washed with aqueous sodium hydrogεn carbonate and brine, and the solution was dried over magnesium sulfate. The solvent was evaporated in vacuo to give 4-[2-[ (3-tert-butoxycarbonylaminoprop-l-yl)oxy]benzoyl]- amino-3-methoxy-N-methyl-N-[2-[5- (4-hydroxypiperidin-l- yl)carbonyipεnt-l-yl]oxy-4-mεthylphεnyl]benzamide (199 mg) . NMR (CDC1 3 , δ) : 1.39 (9H, s) , 1.41-1.99 (10H, a), 2.05-2.20 (2H, a), 2.27 (3H, s) , 2.30-2.51 (2H, a), 3.01-3.22 (2H, a), 3.30 (3H, s), 3.65-4.14 (7H, a), 3.76 (3H, S), 4.22 (2H, t, J=5Hz) , 6.52-6.67 (2H, a), 6.78-7.10 (5H, a), 7.38-7.47 (IH, a), 8.19 (IH, d, J=7Hz), 8.39 (IH, d, J=7Hz) Example 6 To a aixture of 4-[2-[ (3-tert-butoxycarbonylaainoprop-l- yl)oxy]bεnzoyl]aaino-3-aεthoxy-N-aεthyl-N-[2-[5-(4- oxopipεridin-1-yl)carbonylpent-l-yl]oxy-4-aethylphenyl]- bεnzaaidε (250 ag) , aaaoniua acεtate (51 ag) and acetic acid (0.5 al) in methanol (10 ml) was added εodium cyanoborohydride (21 mg) at 0 β C and the mixture waε εtirred at ambient temperature for 12 hours. The mixture was poured into ice-coolεd IN aqueous sodium hydroxide solution (15 ml) and the solution was εxtracted with chloroform (15 ml x 3) . The organic layer was washed with brine and dried over potassium carbonate. The solvent was evaporated in vacuo and the residue was purified by silica gel column chromatography (Si0 2 40 g, 5-15% mεthanol in chloroform) to givε 4-[2-[(3- tert-butoxycarbonylaainoprop-1-yl)oxy]benzoyl]aaino-3- aethoxy-N-aethyl-N-[2-[5-(4-aainopiperidin-l-yl)carbonylpent- l-yl]oxy-4-methylphenyl]benzamide (91 mg) . NMR (CDC1 3 , δ) : 1.41 (9H, s) , 1.45-2.01 (12H, a), 2.09-2.20 (2H, a), 2.28 (3H, s) , 2.23-2.45 (4H, a), 2.56-2.71 (IH, br) , 2.93-3.12 (2H, a), 3.25-3.36 (2H, a), 3.32 (3H, s) , 3.79 (3H, ε), 3.81-4.02 (2H, a), 4.23 (2H, t, J=5Hz) , 4.91-4.08 (IH, br) , 6.56- 6.68 (2H, a), 6.82-7.13 (5H, a), 7.45 (2H, d, J=8Hz), 8.20 (IH, d, J=8Hz) , 8.40 (IH, d, J=8Hz) Example 77 The following compound was obtained according to a similar manner to that of Example 76. 4-[2-(3-tert-Butoxycarbonylaminoprop-l-yl)oxybenzoyl]- amino-3-methoxy-N-mεthyl-N- [2- [6- (4-methylpiperazin-l-yl) hex 1-yl ] oxy-4-methylphenyl ] benzamidε NMR (CDClv δ) : 1.39 (9H, s) , 1.45-1.84 (8H, m) , 2.09-2.22 (2H, m) , 2.27 (3H, ε) , 2.28 (3H, s) , 2.32-2.59 (8H, m) , 3.32 (IH, q, J=5Hz) , 3.34 (3H, s), 3.80 (3H, s)., 3.82-4.01 (2H, m) , 4.28 (2K, _, J=5Hz), 6.56-6.65 (2H, m) , 6.82-7.12 (6H, a), 7.43 7.50 (IH, a), 8.20 (IH, d, J=8Hz) , 8.38 (IH, d, J=8Hz) Example 78 To a aixture of 4- [2- (3-tert-butoxycarbonylaainoprop-l- yl) oxybenzoyl] aaino-3-aethoxy-N-aethyl-N- [2- [5-carboxypent-l yl]oxy-4-methylphenyl]benzamide (250 mg) , 2-dimethylamino- ethanol (99 mg) and 4-dimethylaminopyridine (36 mg) in dichloromethanε (10 ml) was addεd N-ethyl-N'-(3- dimethylaminoprop-1-yl)carbodiimide hydrochloride (71 mg) at 0°C and stirred at the same tempεraturε for 7 hours. Thε mixture was diluted with chloroform (20 ml) and thε solution was washεd with water (20 ml x 2) and brine. The solution was dried ovεr magnεsium sulfatε and thε εolvent was removed under reducεd pressure. This residuε was purifiεd by silica gεl column chromatography (Si0 2 30 g, 1-10% mεthanol in chloroform) to givε 4-[2-(3-tεrt-butoxycarbonylaminoprop-l- yi)oxybenzoyl]amino-3-mεthoxy-N-mεthyl-N-[2-[5- (2-dimεthyl- aminoεth-l-yl)oxycarbonylpεnt-l-yl]oxy-4-mεthylphεyl]- bεnzamidε (238 mg) . NMR (CDC1 3 , δ) : 1.40 (9H, s), 1.45-1.57 (2H, a), 1.65-1.90 (4H, m), 2.10-2.21 (2H, a), 2.28 (9H, s), 2.39 (2H, t, J=5Hz), 2.55 (2H, t, J=5Hz) , 3.30 (2H, t, J=5Hz), 3.32 (3H, ε) , 3.79 (3H, s) , 3.82-4.00 (2H, a), 4.18 (2H, t, J=5Hz) , 4.24 (2H, t, J=5Hz) , 4.75-4.86 (IH, br) , 6.54-6.67 (2H, a), 6.81-7.11 (5H, a), 7.41-7.49 (IH, a), 8.20 (IH, d, J=8Hz) , 8.49 (IH, d, J=8Hz) Example 79 To a solution of 4-[2- (3-tεrt-butoxycarbonylaainoprop-l- yl)oxybenzoyl]aaino-3-aethoxy-N-aεthyl-N-[2- (5- ethoxycarbonylpεnt-1-yl)oxy-4-aethylphenyl]benzaaide (400 ag) in tetrahydrofuran (5 al) was added lithium aluminum hydride (12 mg) at -23 β C and the mixture was stirred at 0 β C for 3 hours. The reaction was quenched with slow addition of 0.5N hydrochloric acid (15 ml) and the solution was stirred at ambient temperature for 20 minuteε. Thε εolution waε εxtractεd with chloroform (15 ml x 3) and thε organic layεr waε washεd with aquεous εaturatεd εodium bicarbonatε εolution and brinε. Thε εolution waε driεd ovεr magnεεium εulfatε and the εolvent waε removed under reduced preεsurε to give 4-[2- (3-tert-butoxycarbonylaminoprop-l-yl)oxybεnzoyl]amino-3- methoxy-N-methyl-N-[2-(6-hydroxyhex-l-yl)oxy-4- mεthylphenyl]benzamidε (456 mg) . NMR (CDC1 3 , δ) : 1.40 (9H, s), 1.45-2.20 (10H, m) , 2.27 (3K, ε), 3.30 (2H, q, J=5Hz) , 3.32 (3H, s) , 3.64 (2H, t, J=5Hz), 3.78 (3H, ' s) , 3.81-4.02 (2H, m), 4.23 (2H, t, J=5Hz), 6.57-6.63 (2H, m) , 6.84- 7.13 (6H, m) , 7.41-7.49 (IH, m) , 8.20 (IH, d, J=7Hz) 8.41 (IH, d, J=7Hz) Example 80 To a εolution of oxalyl chloride (95 mg) in dichloromethane (10 ml) waε added dimethyl εulfoxide (117 mg) dropwiεe at -78 β C. Thε mixturε waε warmed to -15°C and a εolution of 4-[2-(3-tert-butoxycarbonylaminoprop-l- yl)oxybεnzoyl]amino-3-mεthoxy-N-mεthyl-N-[2-(6-hydroxyhex-l- yl)oxy-4-mεthylphenyl]benzamide (450 mg) in dichloromethane (10 ml) waε added thereto. After being εtirred at the same temperature for 10 minutes, to the reaction mixture was adde triethylamine (343 mg) and stirred at the same temperature for 5 minutes. The reεulting εolution waε waraεd to ambient tempεraturε and poured into water. Thε mixturε waε εxtractε with chloroform (15 ml x 3) and thε organic layer waε waεhed with brine. The εolution waε dried over magneεium sulfate and the solvent was evaporated to give 4-[2- (3-tert- butoxycarbonylaminoprop-1-yl)oxybenzoyl]amino-3-methoxy-N- methyl-N-[2-(5-formylpent-l-yl)oxy-4-aethylphenyl]benzaaidε (546 ag) NMR (CDCI3, δ) : 1.40 (9H, s) , 1.50-1.91 (6H, a), 2.11-2.23 (2H, a), 2.27 (3H, s) , 2.50 (2H, t, J=5Hz), 3.31 (IH, q, J=5Hz) , 3.34 (3H, s) , 3.79 (3H, s), 3.85-4.00 (2H, a), 4.27 (2H, t, J=5Hz) , 6.60-6.68 (2H, a), 6.81-7.12 (6H, a), 7.42-7.51 (IH, a), 8.21 (IH, d, J=7Hz) , 8.41 (IH, d, J=7Hz) , 9.89 (IK, s) Example 81 To a εolution of 4-[2-[3- (tert-butoxycarbonyl)aminoprop- 1-yl]oxybenzoyl]amino-3-methoxy-N-[2-(4-cyanophεnylmεthyl)- oxy-4-mεthylphεnyl]-N-methylbenzamidε (360 mg) in xylεnε (8 ml) waε addεd trimεthyltin azidε (218 mg) and thε εolution waε εtirrεd at 120 e C for 3 dayε. Thε εolution was cooled to ambient temperature and 12N hydrochloric acid (10 ml) was added to the solution to decompose tin salt of the tεtrazole compound and the excεsε rεagεnt. Thεn thε εolution waε adjusted to pH 7 with saturated aqueous sodium hydroxide at 0°C, and the solution was extractεd with εthyl acεtate (50 ml x 3) . The organic layer was washed with brine, and dried over magnesium sulfate. The solvent was evaporated to givε a crude product. The crude product was purified by εilica gel column chromatography (Si0 2 30 g, 2-25% methanol in chloroform) to give 4-[2-(3-aminoprop-l-yl)oxybenzoyl]amino- 3-methoxy-N-[2-[4- (tetrazol-5-yl)phεnylmεthyl]oxy-4- mεthylphenyl]-N-methylbenzamidε (227 mg) . NMR (CDC1 3 , δ) : 2.15 (3H, br s) , 2.14-2.26 (2H, a), 3.17 (2H, q, J=5Hz) , 3.40 (3H, s) , 3.57 (3H, s) , 4.20 (2H, t, J=5Hz), 4.95 (IH, d, J=12Hz) , 5.22 (IH, d, J=12Hz), 6.55-6.64 (2H, a), 6.80 (IH, s) , 6.92-7.08 (6H, a), 7.23 (IK, br) , 7.43 (IH, dd, J=2, 8Hz), 7.78 (2H, d, J=8Hz), 8.20 (IH, d, J=8Hz) Example 82 A mixturε of 4-[2- (3-aminoprop-l-yl)oxybεnzoyl]amino-3- mεthoxy-N-methyl-N-[2-[5- (4-dimethylaminopipεridin-l- yl)carbonylpεnt-l-yl]oxy-4-mεthylphεnyl]bεnzamidε (275 mg) and O-methyliεourea (44 mg) in εthanol (5 ml) was rεfluxεd for 3 days. Thε solvεnt waε εvaporatεd in vacuo and thε rεεiduε waε purified on baεic εilica gel column chromatography (Si0 2 17 g, 1-80% methanol in chloroform) to give 4-[2- (3-guanidinoprop-l-yl)oxybenzoyl]amino-3-methoxy-N- methyl-N-[2-[5-(4-dimethylaminopipεridin-l-yl)carbonylpent-1 yl]oxy-4-methylphenyl]benzamide (53 mg) . NMR (CDC1 3 , δ) : 1.40-1.97 (6H, m) , 2.06-2.20 (2H, m) , 2.27 (6K, s), 2.28 (3H, ε), 2.29-2.41 (4H, m) , 2.5 (IK, br), 3.04 (2H, br) , 3.30 (3H, ε) , 3.42 (2H, br), 3.76 (3H, ε) , 3.78 (2H, br) , 3.82-4.01 (2H, a), 4.25 (2H, br) , 6.55-6.68 (2H, a), 6.81-7.09 (5H, m), 7.28 (IH, s), 7.42 (IH, dd, J=2, 8Hz), 0 7.99 (IH, d, J=8Hz), 6.29 (IH, br) Example 83 The following compound was obtained according to a similar manner to that of Example 6. 5 4-[2-[3-(tert-Butoxycarbonylamino)prop-1-yl]oxybenzoyl] amino-3-methoxy-N-[2-(4-aminobut-l-yl)oxy-4-methylphenyl]-N- methylbenzamide NMR (CDCI3, δ) : 1.40 (9K, s) , 1.81-1.99 (4H, a), 0 2.05-2.14 (2H, a), 2.24 (3H, ε) , 3.08 (2H, br) , 3.29 (2H, br), 3.30 (3H, ε) , 3.70 (3H, ε) , 3.76- 3.96 (2K, a), 4.14 (2H, t, J=5Hz), 5.07 (IH, br) , 6.54-6.61 (2K, a), 6.85-7.04 (4H, a), 7.25 (IH, ε) 7.37 (IH, dd, J=2, 8Kz), 8.14 (IH, d, J=8Hz), 8.38 5 (IH, d, J=8Hz) Example 84 To a solution of 4-[2-[3-(tert-butoxycarbonylaaino)pro l-yloxy]benzoylaaino]-3-aethoxy-N- [2-[4-(phenoxycarbonyl- 0 amino)but-l-yi]-4-aethylphεnyl]-N-mεthylbenzamide (200 mg) N,N-dimethylformamidε (5 ml) was added 1-methylpiperazine ( μl) and thε solution was stirrεd at 80 β C for 7 hours. The solution was diluted with ethyl acetate (15 al) and washed succeεεivεly with water (20 al x 4) and brine. The εolvent "5 waε dried over aagnesium sulfatε and removed under reduced presεure. The crude product waε purifiεd on silica gel column chromatography (Si0 2 25 g, chloroform-methanol 2-10%) to give pure 4- [2- [3- (tεrt-butoxycarbonylamino)prop-l- yl]oxybεnzoyl] amino-3-mεthoxy-N- [2- [4- [ (4-methylpiperazin-l- yl) carbonylamino]but-l-yl]oxy-4-methylphεnyl]-N- methylbεnzamide (124 mg) . NMR (CDC1 3 , δ) : 1.40 (9H, s) , 1.60-1.81 (4H, m) , 2.13-2.22 (2H, m) , 2.29 (6H, ε) , 2.39 (4H, br) , 3.79 (3H, s), 3.25-3.51 (8H, m) , 3.32 (3H, ε) , 3.75-3.99 (2H, m) , 4.26 (2H, t, J=5Hz) , 6.57-6.71 (2K, a), 6.92-7.18 (6H, m) , 7.48 (IH, dd, J=2, 8Hz), 8.20 (IH, d, J=8Hz), 8.41 (IH, d, J=8Hz) Example 85 The following compoundε werε obtainεd according to a εimilar manner to that of Example 84. 1) 4- [2- [3- (tert-Butoxycarbonylamino)prop-1-yl]oxybenzoyl]- amino-3-methoxy-N- [2- [4- [ (4-dimethylaminopiperidin-l- yl) carbonylamino]but-l-yl]oxy-4-methylphεnyl]-N- methylber.zamide NMR (CDC1 3 , δ) : 1.40 (9H, s) , 1.65-1.90 (4H, m) , 2.29 (3K, s), 2.30 (6H, s), 2.77 (IH, t, J=llHz) , 3.29 (2H, c, J=5Hz), 3.32 (3H, ε) , 3.78 (3H, s) , 3.85- 4.11 (6H, m) , 4.25 (2H, t, J=5Hz) , 6.55-6.70 (2H, a), 6.92-7.13 (5H, a), 7.45 (IH, dd, J=2, 8Hz) , 8.20 (IH, d, J=8Hz), 8.40 (IH, d, J=8Hz) 2) 4- [2- [3- (tert-Butoxycarbonylaaino)prop-l-yl]oxybenzoyl]- aaino-3-aethoxy-N- [2- (4-ureidobut-l-yl)oxy-4- aethylphεnyl]-N-aεthylbenzaaide NMR (CDCI3, δ) : 1.40 (9H, s) , 1.45-1.80 (4H, a), 2.01-2.11 (2H, a), 2.27 (3H, ε) , 3.22-3.31 (2H, a), 3.30 (3H, ε), 3.65-3.77 (2H, a), 3.71 (3H, ε) , 4.22 (2H, t, J=5Hz), 5.16 (2H, br) , 6.48 (IH, ε) , 6.71 (IH, d, J=8Hz), 6.90-7.15 (5H, a), 7.41 (IH, dd, J=2, 8Hz), 8.11 (IH, d, J=8Hz) , 8.35 (IH, d, J=8Hz) Exaaole 86 To a εolution of 4-[2-[3-(tert-butoxycarbonylaaino)prop l-yloxy]bεnzoylaamo]-3-aethoxy-N-[2- [4- (phenoxycarbonyl- amino) but-l-vl]-4-methylohεnyll-N-mεthylbεnzamidε (150 ag) i N,N-diaethylforaaaide (5 al) was addεd diaεthylaainε hydrochloridε (40 ag) and the aixture was stirred at 80 β C fo 7 hours. The aixture was cooled to aabient teaperature and diluted with ethyl acetate (15 al) . The solution was waεhed with watεr (15 al x 5) and brine, and dried over aagneεiua sulfatε. Thε solvεnt waε rεaovεd in vacuo and thε rεεiduε was purified on silica gel column chromatography (Si0 2 20 g, chloroform-methanol 1-5%) to give 4-[2-[3-(tert- butoxycarbonylamino)prop-l-yloxy]benzoylamino]-3-mεthoxy-N- [2- [4- (N,N-dimethylureido)but-l-yloxy]-4-methylphenyl]-N- methylbenzamide (115 mg) . NMR (CDC1 δ) : 1.40 (9H, s), 1.60-1.87 (4H, ) , 2.06-2.16 (2H, a), 2.28 (3H, s) , 2.90 (6H, s) , 3.3 (2H, q, J=5Hz), 3.34 (3K, s) , 3.79 (3H, s) , 3.85- 4.02 (2H, a), 4.23 (2H, t, J=5Hz) , 6.57-6.64 (2H, a), 6.90-7.10 (5H, a), 7.44 (IH, dd, J=2, 8Hz) , 8.20 (IK, d, J=8Hz), 8.41 (IH, d, J=8Hz) Example 87 To a εolution of 4- [2- [ (3-tert-butoxycarbonylaminoprop- 1-yl) oxy] benzoyl ]amino-3-carboxymεthoxy-N-mεthyl-N- [2- [5- (4- methylpiperazin-1-yl) carbonylpent-l-yloxy] -4-methylphenyl] - benzamide (128 mg) in methanol (5 ml) waε added dropwise trimethylsilyldiazomεthanε (5 ml, 2.0M n-hεxane εolution) a stirred at ambient temperature for 30 minutes. The solutio was concentrated in vacuo and the residue was purified by preparativε thin layεr silica gεl chromatography (chloroform:methanol:28% aqueous ammonia εolution, 50:5:1) givε 4-[2-[ (3-tert-butoxycarbonylaminoprop-l-yl)oxy]benzoyl]- amino-3-mεthoxycarbonylmethoxy-N-methyl-N- [2- [5- (4- methylpiperazin-1-yl) carbonylpent-l-yloxy] -4-me thylphenyl ]- benzamidε (85 mg) . NMR (CDC1 3 , δ) : 1.39 (9H, s), 1.45-1.37 (8H, m) , 2.00-2.10 (2H, m), 2.26 (3H, s), 2.29 (3H, s) , 2.30-2.42 (6H, m) , 3.18-3.27 (2H, m) , 3.30 (3H, s), 3.45-3.51 (2H, a), 3.63 (2H, br) , 3.79 (3H, s), 3.87-3.96 (2H, a), 4.22-4.29 (2H, a), 4.54 (2H, s), 6.53-6.13 (2H, a), 6.77-6.85 (IH, a), 6.89 (IH, br), 6.92-7.02 (2H, a), 7.02-7.10 (IH, a), 7.43- 7.47 (IH, a), 8.14-8.19 (IH, a), 8.40-8.45 (IH, a) Example 88 The following coapound was obtained according to a siailar aanner to that of Exaaplε 8. 4-[2-[ (3-tert-Butoxycarbonylaainoprop-l-yl)oxy]benzoyl]- amino-3-dimethylaminocarbonylmethoxy-N-mεthyl-N-[2-[5- (4- mεthylpipεrazin-1-yl)carbonylpent-l-yloxy]-4-methylphεnyl]- bεnzamidε NMR (CDCI3, δ) : 1.39 (9H, s) , 1.48-1.58 (2H, m) , 1.63-1.88 (6H, m) , 1.97-2.09 (2H, a), 2.28 (3H, s) , 2.30 (3H, s), 2.31-2.42 (6H, a), 2.99 (3H, ε), 3.02 (3H, ε), 3.17-3.27 (2H, a), 3.32 (3H, s) , 3.50 (2H, br), 3.63 (2H, br) , 3.83-3.97 (2H, a), 4.22-4.29 (2H, a), 4.67 (2H, s) , 6.53-6.63 (2H, a), 6.80-6.90 (2H, a), 6.96-7.09 (3H, a), 7.93 (IH, t, J=6Hz) , 8.14 (IH, d, J=6Hz), 8.38 (IH, d, J=7Hz) Example 89 To a εolution of 4-[2-[ (3-tεrt-butoxycarbonylaminoprop- l-yl)oxy]bεnzoyl]amino-3-ethoxycarbonylmethoxy-N-mεthyl-N-[2- [5-(4-methylpiperazin-l-yl)carbonylpεnt-1-yloxy]-4- mεthylphenyl]benzamide (102 mg) in 7.5N ammonia in methanol (5 ml) waε stirred at ambient temperature for 24 hours. The solution was concentrated in vacuo to give 4-[2-[ (3-tert- butoxycarbonylaminoprop-1-yl)oxy]benzoyl]amino-3- aminocarbonylmεthoxy-N-mεthyl-N-[2-[5-(4-methylpiperazin-l- yl)carbonylpεnt-1-yloxy]-4-mεthylphenyl]benzamide (92 mg) . NMR (CDC1 3 , δ) : 1.37 (9H, s), 1.48-1.60 (2H, m) , 1.60-1.75 (4H, m), 1.75-1.88 (2H, ) , 1.97-2.08 (2H, m) , 2.27 (3H, ε), 2.28 (3H, ε), 2.30-2.41 (6H, a), 3.17-3.27 (2H, a), 3.30 (3H, ε) , 3.47 (3H, ε) , 3.52-3.62 (2H, a), 3.90-3.97 (2H, a), 4.16-4.29 (4H, a), 5.85 (IH, br) , 6.57 (IH, d, J=7Hz), 6.67 (IH, ε), 6.75-6.90 (2H, a), 7.00 (IH, d, J=7Hz) , 7.07-7.17 (2H, a), 8.00 (IH, ε) , 8.18-8.21 (IH, a), 8.25 (IH, d, J=7Hz) Exaaple 90 The following compound waε obtained according to a εimilar manner to that of Example 89. 4-[2-[ (3-tert-Butoxycarbonylaminoprop-l-yl)oxy]benzoyl]- amino-3-mεthylaminocarbonylmεthoxy-N-mεthyl-N-[2-[5-(4- methylpipεrazin-1-yl)carbonylpεnt-1-yioxy]-4-mεthylphenyl]- benzamide NMR (CDCI3, δ) : 3.37 (9H, ε), 1.45-1.77 (6H, m) , 1.77-1.88 (2H, m) , 1.96-2.08 (2H, m) , 2.28 (3H, s) , 2.29 (3K, s), 2.29-2.40 (6H, m) , 2.82-2.83 (3H, ε), 3.18-3.27 (2H, m) , 3.30 (3H, ε) , 3.43-3.50 (3H, m) , 3.57 (2H, br), 3.90-3.97 (2H, m) , 4.18-4.30 (3H, m), 6.57 (IH, d, J=6Hz) , 6.65 (IH, ε) , 6.76-6.83 (2H, m) , 7.00 (IH, d, J=7Hz) , 7.06-7.15 (2H, m) , 7.45 (IH, t, J=7Hz), 8.16-8.22 (2H, m) Example 91 Thε following compound was obtained according to similar manners to those of Examples 8 and 16. 4- (2-Aminobenzoyl)amino-N-methyl-N-[4-mεthyl-2-[5-(4- methylpiperazin-1-yl)carbonylpent-l-yloxy]phεnyl]bεnzamidε dihydrochloride NMR (DMSO-dg, δ) : 1.35-1.66 (4K, m) , 1.66-1.82 (2H, a), 2.22 (3H, s) , 2.40 (2H, t, J=7Hz) , 2.73 (3H, s), 2.77-3.11 (3H, a), 3.17 (3H, s) , 3.28-3.56 (3H, a), 3.76-4.17 (3H, a), 4.35-4.52 (IH, a), 6.63 (IH, d, J=9Hz)> 6.79 (IH, ε) , 6.91 (IK, dd, J=9, 9Kz) , 6.98-7.11 (2H, a), 7.22 (2H, d, J=9Hz) , 7.36 (IH, dd, J=9, 9Hz), 7.54 (2H, d, J=9Hz) , 7.69 (IH, d, J=9Kz) Exaaple 92 The following compounds were obtained according to similar manners to those of Exampleε 6 and 16. 1) 4-[2-[ (3-Aminoprop-l-yl)amino]benzoyl]amino-3-methoxy-N- methyl-N-[4-methyl-2-[5-(4-methylpiperazin-l-yl)- carbonylpεnt-1-yloxy]phenyl]bεnzamide trihydrochloride NMR (DMSO-dg, δ) : 1.36-1.65 (4H, a), 1.66-1.92 (4H, a), 2.23 (3H, s), 2.38 (2H, t, J=7Hz) , 2.68-2.77 (3H, a), 2.77-3.12 (4H, a), 3.18 (3H, s) , 3.22 (2H, t, J=7Hz), 3.28-3.56 (3H, a), 3.63 (3H, ε) , 3.75- 4.32 (4H, a), 4.42 (IH, a), 6.58-6.69 (2H, a), 6.78 (IH, d, J=8Hz), 6.83 (IK, ε) , 6.86-6.96 (2H, a), 7.03 (IH, d, J=8Hz), 7.34 (IK, dd, J=8, 8Hz) , 7.61 (IH, d, J=8Hz), 7.67 (IH, d, J=8Hz) , 7.91-8.17 (3H, a), 9.23 (IH, s)- 2) 4-[2-(3-Aminoprop-l-yl)oxybenzoyl]amino-3-methoxy-N- methyl-N-[2-[5- (4-mεthylpiperazin-l-yl)carbonylpent-l- yloxy]phenyl]bεnzamide dihydrochloride NMR (DMSO-dg, δ) : 1.34-1.66 (4H, a), 1.66-1.83 (2H, a), 2.04-2.24 (2H, a), 2.32-2.46 (2H, a), 2.74 (3H, s), 2.79-3.12 (4K, a), 3.22 (3H, ε) , 3.29-3.58 (3H, a), 3.63-4.19 (7H, a), 4.28-4.52 (3H, a), 6.80-7.08 (4H, a), 7.08-7.36 (4H, a), 7.58 (IK, dd, J=9, 9Hz), 8.02 (IH, d, J=9Hz), 8.13 (2H, br s) , 8.28 (IH, d, J=9Hz) 3) 4-[2-(3-Aminoprop-l-yl)oxybenzoyl]amino-3-mεthoxy-N- methyl-N-[2-[5- (4-dimethylaminopiperidin-l-yl)- carbonylpent-l-yloxy]-4-methylphenyl]benzamide dihydrochloride NMR (DMSO-dg, δ) : 1.28-1.82 (8H, m) , 1.90-2.51 (11H, a), 2.64 (6H, s), 2.74-3.06 (3H, a), 3.18 (3H, s) , 3.22-4.08 (6H, a), 4.29-4.41 (2H, a), 4.51 (IH, a), 6.64 (IH, d, J=8Hz), 6.75-7.20 (5H, a), 7.27 (IH, d, J=8Hz), 7.58 (IH, a), 7.94-8.32 (5H, a) 4) 4-[2- (3-Aainoprop-l-yl)oxybenzoyl]aaino-2-chloro-N- aethyl-N-[2-[5-(4-aεthylpipεrazin-l-ylcarbonyl)pent-1- yloxy]phenyl]benzaaidε dihydrochloridε NMR (DMSO-dg, δ) : 1.39-1.68 (4H, a), 1.69-1.90 (2H, a), 1.92-2.12 (2K, a), 2.31-2.50 (2H, a), 2.73 (3H, br s), 2.79-3.10 (4H, a), 3.17-3.61 (7H, a), 3.92- 4.26 (5H, a), 4.42 (IH, a), 6.77 (IH, a), 6.92-7.23 (6H, a), 7.34-7.58 (3H, a), 7.81 (IH, ε) , 7.90-8.14 (3H, m) 5) 4- [2- (3-Aminoprop-l-yl)oxy-5-mεthylbenzoyl] amino-3- mεthoxy-N-mεthyl-N- [2- [5- (4-mεthylpiperazin-l- yl) carbonylpent- 1-yl ]oxy-4 -me thylphenyl] benzamide dihydrochloride NMR (CDC1 3 , δ) : 1.50-1.93 (8H, a), 2.28 (3H, s), 2.28-2.36 (2H, a), 2.31 (3H, s) , 2.79 (3H, s) , 3.09-3.20 (2H, a), 3.29 (3H, s) , 3.80 (3H, s) , 3.85-4.04 (2H, a), 4.18-4.28 (2H, a), 6.57-6.66 (2H, a), 6.80-6.95 (4H, a), 7.20-7.25 (IH, a), 7.7 (IH, br), 8.51 (IH, br) 6) 4- [2- (3-Aminoprop-l-yl)oxy-4-chlorobenzoyl]amino-3- mεthoxy-N-mεthyl-N- [2- [5- (4-mεthylpiperazin-l- yl) carbonylpent-1-yl] oxy-4-methylphenyl]benzamidε dihydrochloridε NMR (CDC1 3 , δ) : 1.45-1.86 (8H, m) , 2.23 (3H, s) , 2.29-2.43 (2H, m) , 2.78 (3K, ε) , 3.05-3.16 (2H, a), 3.23 (3H, ε), 3.78 (3H, s) , 3.82-4.03 (2H, a), 4.18-4.32 (2K, a), 6.54-6.64 (2H, a), 6.78-7.08 (4H, a), 7.94 (IH, d, J=8Hz), 8.58 (IH, br) 7) 4- [2- (3-Aminoprop-l-yl) oxy-4-methoxybenzoyl] amino-3- mεthoxy-N-mεthyl-N- [2- [5- (4-mεthylpipεrazin-l-yl) - carbonylpεnt-1-yl] oxy-4-methylphenyl]benzamidε dihydrochloridε NMR (CDCI3, δ) : 1.40-1.89 (6H, m) , 2.28 (3H, s) , 2.30-2.61 (6H, m) , 2.70-3.04 (4H, a), 3.08-3.25 (2H, m), 3.28 (3H, ε) , 3.80 (6H, ε) , 3.82-4.08 (2H, m) , 4.26 (2H, br) , 6.49-6.66 (4H, m) , 6.78-7.00 (3H, m) , 7.93-8.02 (IH, m) , 8.30 (IH, br) , 8.52 (2H, br) 8) 4-[2-[ (3-Aminoprop-l-yl) oxy]bεnzoyl] amino-3-methoxy-N- mεthyl-N-mεthyl-N- [2- [5- (4-dimethylaminopiperidin-l- yl) carbonylpεnt-1-yloxy]phenyl]benzamidε dihydrochloridε NMR (DMSO-dg, δ) : 1.42 (2H, br) , 1.53 (2H, br) , 1.74 (2H, br), 2.03 (2H, br) , 2.13-2.20 (2H, a), 2.30- 2.38 (2H, a), 2.66 (3H, s), 2.67 (3H, ε) , 2.94 (4H, br), 3.20 (3H, ε) , 3.28-3.40 (2H, m) , 3.73 (3H, s) , 3.82-4.08 (4H, m) , 4.33-4.40 (2H, m) , 4.47-4.57 (IH, a), 6.82-7.00 (4H, a), 7.10-7.29 (4H, a), 7.53-7.60 (IH, a), 8.00 (IH, d, ■ J=7Hz) , 8.22-8.30 (IK, a) 9) 4-[2-[ (3-Aainoprop-l-yl) oxy]benzoyl]aaino-3-aεthyl-N- aethyl-N- [2- [5- (4-aethylpipεrazin-l-yl) carbonylpεnt-1- yloxy]-4-methylphenyl]benzamide dihydrochloride NMR (DMSO-dg, δ) : 1.40-1.53 (2K, a), 1.53-1.65 (2H, a), 1.66-1.82 (2H, a), 2.01-2.13 (2H, a), 2.18 (3H, s), 2.23 (3H, s), 2.36-2.46 (2H, a), 2.73-2.74 (3H, s), 2.78-3.08 (6H, a), 3.18 (3H, s) , 4.27 (2K, br) , 4.40-4.50 (IK, a), 6.65 (IH, d, J=6Hz) , 6.82 (IH, ε), 6.98-7.13 (3H, a), 7.17-7.30 (2K, a) ,7.45-7.57 (2H, a), 7.22 (IH, d, J=6Kz) , 9.67 (IH, s) 10) 4-[2-[ (3-Aminoprop-l-yl)oxy]benzoyl]amino-3-εthoxy-N- methyl-N-[2-[5- (4-methylpiperazin-l-yl)carbonylpent-l- yloxy]-4-methylphεnyl]benzamide dihydrochloride NMR (DMSO-dg, δ) : 1.23 (3H, t, J=6Hz) , 1.38-1.50 (2H, a), 1.50-1.65 (2H, a), 1.65-1.82 (2H, a), 2.05-2.17 (2H, a), 2.21 (3H, s), 2.32-2.43 (2H, a), 2.70-2.73 (3H, a), 2.80-3.08 (7H, m) , 3.18 (3K, s) , 3.22-3.55 (6H, m), 3.92-4.15 (2H, a), 4.32-4.48 (4H, a), 6.63 (IH, d, J=7Hz), 6.83 (IH, ε) , 6.89-6.92 (2H, a), 7.02 (IK, d, J=7Hz), 7.13 (IH, t, J=6Hz) , 7.29 (IH, d, J=7Hz), 7.58 (IH, t, J=7Hz) , 7.99 (IH, d, J=7Hz), 8.18-8.27 (IH, a) Example 93 The following compoundε were obtained according to εimilar manners to those of Examples 1 and 16. 1) 4-[2- (Dimethylamino)benzoyl]amino-3-mεthoxy-N-mεthyl-N- [4-methyl-2-[5- (4-mεthylpipεrazin-l-yl)carbonylpent-l- yloxy]phenyl]bεnzamide dihydrochloride NMR (DMSO-dg, δ) : 1.36-1.65 (4H, m) , 1.67-1.82 (2H, m), 2.22 (3H, s) , 2.38 (2H, t, J=7Hz) , 2.64-3.14 (12H, m), 3.18 (3H, s) , 3.28-3.42 (2H, a), 3.50 (IH, a), 3.73 (3H, s) , 3.79-4.14 (3H, a), 4.42 (IH, a), 6.64 (IH, d, J=8Hz), 6.82 (IH, s) , 6.83-6.97 (2H, a), 7.02 (IH, d, J=8Hz) , 7.35 (IH, m) , 7.52- 7 . 67 (2H, a) , 8 . 07 ( IH, d, J=8Hz ) , 8 . 14 ( IK, a) 2) 4- [2- (Dimethylaminoεulfonyl)benzoyl] amino-3-mεthoxy-N- methyl-N- [4-mεthyl-2- [5- (4-mεthylpipεrazin-l- yl) carbonylpεnt-1-yloxy]phεnyl]bεnzamidε hydrochloridε NMR (DMSO-dg, δ) : 1.38-1.64 (4H, a), 1.67-1.82 (2K, a), 2.23 (3H, s) , 2.38 (2H, t, J=7Hz) , 2.69 (6H, s), 2.74 (3H, s), 2.80-3.12 (4H, a), 3.18 (3H, s) , 3.23-3.52 (2H, a), 3.59 (3H, s) , 3.81-4.16 (3H, a), 4.44 (IK, a), 6.66 (IH, d, J=9Hz), 6.77-6.96 (3H, a), 7.02 (IH, d, J=9Hz), 7.51 (IH, a), 7.60-7.92 (4H, a) 3) 3-Methoxy-4- [2- (aorpholinosulfonyl)benzoyl]amino-N- methyl-N- [4-methyl-2- [5- (4-methylpiperazin-l- yl) carbonylpent-l-yloxy]phεnyl]bεnzamidε hydrochloridε NMR (DMSO-dg, δ) : 1.37-1.65 (4H, m) , 1.66-1.83 (2H, a), 2.23 (3H, s), 2.32-2.44 (2H, a), 2.73 (3H, s), 2.81-3.10 (6H, a), 3.18 (3H, ε) , 3.25-3.71 (11H, a), 3.80-4.20 (3H, a), 4.42 (IH, a), 6.66 (IH, d, J=8Hz), 6.76-6.96 (3H, a), 7.02 (IH, d, J=8Hz) , 7.53 (IH, d, J=8Hz), 7.62-7.93 (4H, a), 8.31 (IH, ε) 4) 4- [2- (Iεoprop-1-yl)oxybenzoyl] amino-3-methoxy-N-methyl- N- [4-methyl-2- [5- (4-methylpiperazin-l-yl) carbonylpent-l- yloxy]phεnyl]bεnzamidε hydrochloridε NMR (DMSO-dg, δ) : 1.39 (6H, d, J=7Hz) , 1.38-1.66 (4H, a), 1.67-1.83 (2H, a), 2.22 (3H, ε) , 2.39 (2H, t, J=7Hz), 2.76 (3H, ε) , 2.82-3.11 (4H, a), 3.18 (3H, ε), 3.74 (3H, ε), 3.79-4.18 (5H, a), 4.36-4.52 (IH, a), 4.98 (IH, a), 6.65 (IH, d, J=8Hz) , 6.73-7.17 (5H, a), 7.30 (IH, d, J=8Kz) , 7.54 (IH, dd, J=8, 8Hz), 8.04 (IH, d, J=8Hz) , 8.31 (IH, d, J=8Hz) Exa ple 94 Thε following compound waε obtainεd according to εimila! manners to those of Examples 16 and 30. 4-[2-[2-[ (3-Aminoprop-l-yi)oxy]phεnyl]vinyl]-3-mεthoxy- N-mεthyl-N-[4-mεthyl-2-[5- (4-mεthylpipεrazin-l- yl)carbonylpent-l-yloxy]phenyl]benzamide dihydrochloride NMR (DMSO-dg, δ) : 1.33-1.64 (4H, m) , 1.64-1.83 (2H, a), 1.95-2.17 (2H, a), 2.22 (3H, s) , 2.39 (2H, t, J=7Hz), 2.72 (3H, ε) , 2.76-3.10 (6H, a), 3.15 and 3.16 (total 3H, s) , 3.28-3.60 (2H, a), 3.64 (3H, s), 3.80-4.20 (5H, a), 4.42 (IH, a), 6.44-7.60 (12H, a), 8.00-8.26 (2E, a) Example 95 The following coapounds were obtained according to siailar aannεrε to thoεε of Exaapleε 1 and 43. 1) 4- (2-Hydroxybenzoyl)aaino-3-aethoxy-N- [2- [4- (4- dimethylaminopiperidin-1-yl) carbonyl-4- methyl ] phenylmethoxy] phenyl-N-methylbεnzamide MASS (m/z) : 637 (M+l) 2) 4- (2-Kydroxy)bεnzoylamino-3-mεthoxy-N-mεthyl-N- [2- [3- (4- methylpiperazin-1-yl) carbonylmεthoxyprop-l-yl]oxy]- phenylbenzamide NMR (CDC1 3 , δ) : 2.05-2.16 (2H, m) , 2.28 (3H, ε), 2.33-2.40 (4H, m) , 3.35 (3K, ε), 3.40-3.45 (2H, m) , 3.57-3.63 (2H, m) , 3.69 (2K, t, J=7.5Hz), 3.78 (3H, ε), 3.94-4.11 (2H, m) , 4.12 (2H, s) , 6.79-7.04 (7H, ), 7.18 (IH, t, J=7Hz), 7.42 (IH, t, J=7Hz) , 7.50 (IH, d, J=7Hz), 8.20 (IH, d, J=7Hz) , 8.81 (IH, s) 3) 4- (2-Hydroxy) benzoyl-3-mεthoxy-N- [2- [ (E) -5- (4- dimεthylaminopipεridm-1-yl) carbonyl-4-penten-l-yl]oxy- 4-methyl]phεnyl-N-aεthylbεnzaaidε NMR (CDCI3, δ) : 1.33-1.53 (2H, a), 1.84-2.05 (4H, a), 2.27 (3H, s), 2.33 (3H, ε) , 2.40 (3H, ε), 2.30-4.13 (11H, a), 3.32 (3H, ε) , 4.67 (IH, a), 6.30 (IH, d, J=15Hz), 6.55-6.66 (2H, a), 6.78-7.56 (8H, a), 8.18 (IK, a) Example 96 The following coapound waε obtained according to similar aanners to those of Exaaplεε 4, 16 and 45. 4-[2-[ (3-Ammoprop-l-yl)oxy]benzoyl]aaino-3- (3- carboxyprop-1-yl)oxy-N-methyl-N-[2-[5- (4-methylpiperazin-l- yl)carbonylpent-l-yloxy]- -methylphεnyl]bεnzamidε dihydrochloride NMR (DMSO-d 6 , δ) : 1.38-1.52 (2H, a), 1.52-1.65 (2H, a), 1.67-1.93 (4H, a), 2.05-2.16 (2H, a), 2.01 (3H, ε), 2.29-2.43 (5H, a), 2.73 (3H, ε), 3.22-3.56 (4H, a), 3.82-4.14 (5H, a), 4.30-4.47 (3H, a), 8.63 (IH, d, J-7H2), 8.81 (IH, ε) , 8.88-8.92 (2H, a), 7.03 (IK, d, J-7HZ), 7.13 (IH, t, J=7Hz), 7.27 (IH, d, J=7Hz), 7.56 (IH, t, J=6Hz), 7.96 (IH, d, J=6Hz) , 8.22 (IH, d, J=7Hz) Example 97 Thε following coapound was obtainεd according to similar mannεrs to thoεe of Preparation 4 and Example 16. 4- (2-Aminobenzyloxy)-3-aεthoxy-N-aεthyl-N-[4-aεthyl-2- [5-(4-aethylpiperazin-l-yl)carbonylpent-l-yloxy]phenyl]- benzamidε dihydrochloridε NMR (DMSO-dg, δ) : 1.35-1.64 (4H, m) , 1.64-1.81 (2H, a), 2.23 (3H, s) , 2.39 (2H, t, J=7Hz) , 2.75 (3H, ε), 2.80-3.09 (2H, a), 3.16 (3H, s) , 3.27-3.50 (2H, a), 3.57 (3H, s) , 3.73-4.15 (5H, a), 4.43 (IH, a), 5.08 (2H, s), 6.64 (IH, d, J=8Hz) , 6.76-7.42 (9H, m) Example 98 The following compound waε obtained according to εimilar manners to those of Examples 14 and 16. 4-[2-(3-Acetylaminoprop-l-yl)oxybenzoyl]amino-3-methoxy- N-methyl-N-[4-methyl-2-[5-(4-methylpiperazin-l- yl)carbonylpent-l-yloxy]phenyl]benzamide hydrochloride NMR (DMSO-dg, δ) : 1.36-1.50 (2H, m) , 1.50-1.64 (2H, a), 1.67-1.84 (2H, a), 1.92-2.06 (2H, a), 2.22 (3H, ε), 2.32-2.44 (2H, a), 2.50 (3H, ε) , 2.74 and 2.75 (total 3H, ε), 2.81-3.08 (3H, a), 3.19 (3H, s) , 3.30-3.54 (3H, a), 3.70 (3H, s) , 3.79-4.16 (3H, a), 4.20-4.30 (2H, a), 6.64 (IH, d, J=8Hz) , 6.81 (IH, ε), 6.83-6.97 (2H, a), 7.03 (IH, d, J=8Hz) , 7.12 (IH, dd, J=8, 8Hz), 7.25 (IH, d, J=8Hz) , 7.51-7.61 (IH, m) , 7.92-8.08 (2H, a), 8.28 (IH, d, J=8Hz) Example 99 The following compound was obtained according to similar manners to those of Examples 15 and 26. 4- [2- (3-Dimethylaminoprop-l-yl)oxybenzoyl]amino-3- mεthoxy-N-mεthyl-N-[2-[5- (4-dimεthylaminopipεridin-l- yl)carbonylpεnt-1-yl]oxy-4-mεthylphenyl]benzamidε dihydrochloride NMR (CDC1 3 , δ) : 1.46-1.87 (6H, a), 2.26 (3H, s) , 2.37 (2H, t, J=5Hz), 2.50 (2H, br) , 2.76 (6H, s) , 2.77 (6H, s), 3.02-3.30 (3H, a), 3.29 (3H, s) , 3.79 (3H, s), 3.80-4.04 (2H, a), 4.33 (2H, br) , 6.54-6.62 (2H, a), 6.72-7.13 (5H, a), 8.05 (IH, d, J=8Hz) , 8.37 (IH, d, J=8Hz), 9.85 (IH, br) Example 100 The following compound was obtained according to similar manners to those of Exampleε 8 and 45. 4- [2- (3-Aminoprop-l-yl)oxybεnzoyl]amino-3-mεthoxy-N- mεthyl-N-[2- (5-dimethylaminocarbonyl)pent-l-yloxy-4- methylphenyl]benzamide NMR (CDC1 3 , δ) : 1.51-2.19 (10H, a), 2.27 (3H, s) , 2.35 (2H, t, J=6Hz), 2.92 (3H, ε), 3.00 (3H, ε) , 3.32 (3H, ε), 3.77 (3K, ε) , 3.80-4.08 (2H, a), 4.29 (2H, t, J=4Hz), 6.55-6.76 (2H, a), 6.83-7.20 (5H, a), 7.46 (IH, br) , 8.21 (IH, d, J=8Hz) , 8.40 (IH, d, J=8Hz) Example 101 The following coapound waε obtained according to siailar aanners to those of Exaaples 16 and 41. 4- (2-Aainobenzoyl)aaino-3-aethoxy-N-aethyl-N-[4-aethyl- 2-[5- (4-aεthylpipεrazin-l-yl)carbonylpent-l-yloxy]phenyl]- benzaaide dihydrochloride NMR (DMSO-dg, δ) : 1.38-1.66 (4H, a), 1.68-1.83 (2H, a), 2.24 (3H, ε) , 2.34-2.44 (2H, a), 2.76 (3H, ε) , 2.80-3.09 (3H, a), 3.19 (3H, s) , 3.30-3.53 (3H, a), 3.64 (3H, s) , 3.80-4.51 (4H, a), 6.60-6.76 (2H, a), 6.79-6.97 (4H, a), 7.05 (IH, d, J=9Hz) , 7.26 (IH, dd, J=9, 9Hz), 7.58-7.72 (2H, a), 9.19 (IH, br s) Exaaole 102 To a εolution of 4-[2-[ (3-aminoprop-l-yl)oxy]benzoyl]- amino-3-methoxy-N-methyl-N-[4-methyl-2-[5-(4-mεthylpipεrazin- 1-yl)carbonylpent-l-yloxy]phenyl]bεnzamidε (7.35 g) in εthanol (230 ml) waε added 0.5M εulfuric acid in ethanol (22.3 ml) at 80°C. The mixturε waε εtirrεd for 24 hourε at ambiεnt temperaturε. The precipitatε waε filtered through a glaεs funnel followed by rinsing with ethanol. The rεsulting white, cryεtalline εolid was dried over air for 7 days to give 4-[2-[ (3-aminoprop-l-yl)oxy]benzoyl]amino-3-methoxy-N- methyl-N-[4-methyl-2-[5-(4-methylpiperazin-l-yl)carbonylpent- l-yloxy]phenyl]benzaaide sulfate (5.2 g) . NMR (DMSO-dg, δ) : 1.35-1.63 (4K, a), 1.65-1.81 (2H, n) , 2.04-2.40 (14H, a), 2.96 (2H, t, J=7Hz) , 3.03- 4.06 (12H, a), 4.35 (2H, t, J=7Hz) , 6.64 (IH, d, J=8Hz), 6.83(IE, s) , 6.89 (IH, d, J=8Hz) , 6.98 (IH, s), 7.02 (IK, d, J=8Hz), 7.13 (IH, dd, J=8, 8Hz) , 7.26 (IH, d, J=8Hz), 7.59 (IH, dd, J=8, 8Hz) , 8.01 (IH, d, J=8Hz), 8.23 (IH, d, J=8Hz) Example 103 To a solution of 4-[2-[ (3-aainoprop-l-yl)oxy]bεnzoyl]- aaino-3-aethoxy-N-aethyl-N-[4-aethyl-2-[5-(4-aethylpiperazin- 1-yl)carbonylpent-l-yloxy]phenyl]benzaaide (10.7 g) in ethanol (155 al) was added a solution of L- (+)tartaric acid (2.43 g) in ethanol (60 ml) at 80°C. The solution was stirred at ambient tεmpεrature for 1 hour. The solvent was removed at reduced pressurε and rεsultirig εolid was dissolved in distilled water (1 C) and the solution was filterεd through micro filtεr and the filtrate was lyophilized to give 4-[2-[ (3-aminoprop-l-yl)oxy]benzoyl]amino-3-methoxy-N-mεthyl- N-[4-aethyl-2-[5-(4-methylpipεrazin-l-yl)carbonylpent-l- yloxy]phenyl]benzamidε tartrate (5.2 g) . NMR (DMSO-dg, δ) : 1.34-1.62 (4H, m) , 1.66-1.81 (2H, a), 2.03-2.38 (T4H, a), 2.96 (2H, t, J=7Hz) , 3.18 (3H, s), 3.37-3.48 (4H, a), 3.74 (3H, ε), 3.80-4.04 (4H, a), 4.33 (2H, t, J=7Hz) , 6.64 (IH, d, J=8Kz) , 6.83 (IK, ε), 6.89 (IH, d, J=8Hz) , 6.97 (IH, s) , 7.02 (IH, d, J=8Hz), 7.13 (IH, dd, J=8, 8Kz) , 7.26 (IH, d, J=8Hz), 7.58 (IK, dd, J=8, 8Hz), 8.02 (IH, d, J=8Hz), 8.25 (IH, d, J=8Hz) Example 104 Thε following compounds wεre obtained according to similar mannεrs to those of Examples 16 and 45. 1) 4-[2-[ (3-Aminoprop-l-yl)oxy]benzoyl]amino-3-mεthoxy-N- mεthyl-N- (2-methylphenyl)benzamidε hydrochloridε NMR (DMSO-dg, δ) : 2.06-2.32 (5H, m) , 2.87-3.05 (2H, m) , 3.26 (3H, s), 3.72 (3K, s), 4.35 (2H, t, J=7Hz), 6.84-6.98 (2K, m) , 7.08-7.36 (6H, m) , 7.58 (IH, dd, J=8, 8Hz), 7.89-8.16 (4H, m) , 8.26 (IH, d, J=8Hz) 2) 4-[3-[ (3-Aminoprop-l-yl)oxy]bεnzoyl]amino-3-mεthoxy-N- methyl-N-[4-mεthyl-2-[5- (4-dimεthylaminopipεridin-l- yl) carbonylpεnt-1-yloxy]phenyl]benzamide dihydrochloride NMR (DMSO-dg, δ) : 1.38-1.78 (12K, m) , 1.98-2.07 (4H, ), 2.24 (3H, s), 2.36 (2H, t, J=8Hz) , 2.43-2.54 (IH, m) , 2.67 (3H, ε) , 2.69 (3H, s), 2.92-3.01 (2H, a), 3.19 (3K, s), 3.64 (3H, s) , 3.88-4.03 (IH, a), 4.13 (2K, t, J=8Hz), 4.48-4.57 (IH, a), 6.65 (IH, d, J=8Hz), 6.82 (IH, s) , 6.88-6.93 (2H, a), 7.03 (IK, d, J=8Hz), 7.17 (IK, d, J=8Hz) , 7.38-7.52 (3H, a), 7.62 (IH, d, J=8Hz) , 7.92-8.01 (2H, br) , 9.33 (IK, s) ESI-MASS (m/z) : 688 (M+H) 3) 4- [N-Mεthyl-2-[ (3-aminoproρ-l-yl)oxy]bεnzoyl]amino-3- methoxy-N-methyl-N- [4-mεthyl-2-[5- (4-mεthylpiperazin-l- yl) carbonylpent-l-yloxy]phenyl]benzamide dihydrochloride NMR (DMSO-dg, δ) : 1.32-1.65 (3H, m) , 2.27 (3H, ε) , 2.33-2.40 (2K, m) , 2.77 (3H, s) , . 2.86-3.02 (5K, a), 3.12 (3H, s), 3.33-3.70 (13H, a), 4.00-4.10 (IH, a), 4.40-4.50 (IK, a), 6.58-6.78 (6H, a), 6.84-7.00 (3H, a), 7.20 (IH, t, J=8Hz) , 7.89-7.97 (2H, br s) ESI-MASS (a/z) : 674 4) 4-[2-[3-Aminoprop-1-yl)oxy]benzoyl]amino-3-methoxy-N- methyl-N-[4-[5- (4-mεthylpipεrazin-l-yl)carbonylpent-l- yloxy]phenyl]benzamide dihydrochloride NMR (DMSO-dg, δ) : 1.37-1.73 (8H, a), 2.12-2.20 (2H, a), 2.37 (2H, t, J=8Hz) , 2.72-2.79 (4H, a), 2.89- 3.01 (4H, a), 3.29-3.40 (4H, a), 3.80 (3H, s), 3.89 (2H, t, J=8Hz), 3.98-4.04 (IH, a), 4.34-4.41 (3H, a), 6.80-6.86 (3H, a), 7.04-7.19 (4H, a), 7.29 (IH, t, J=8Hz),7.59 (IH, t, J=8Kz), 7.95-8.06 (4H, a), 8.27 (IH, d, J=8Hz) ESI-MASS (a/z) : 646 (M+H) 5) 4-[2-(3-Aainoprop-l-yl)oxybenzoyl]aaino-3-aεthoxy-N- aethyl-N-[2-[5-(4-aethylhoaopiperazin-l-yl)carbonylpent- l-yl]oxy-4-aethylphenyl]benzaaide dihydrochloride NMR (CDC1 3 , δ) : 1.47-1.89 (8H, a), 2.27 (3H, ε) , 2.30-2.46 (4H, a), 2.77-2.96 (2H, a), 3.15-3.63 (11H, a), 3.30 (3H, s) , 3.76-4.04 (5H, a), 4.15- 4.40 (2H, m), 6.60 (2H, br) , 6.78-7.11 (5H, m) , 7.43 (IH, br), 7.98-8.05 (IH, m) , 8.29-8.37 (IH, a), 8.52 (2H, br) 6) 4-[2-(3-Aainoprop-l-yl)oxybenzoyl]amino-3-methoxy-N- aethyl-N-[2-[5-(2-diaethylaainoethyl)aainocarbonyl]- pent-1-yl]oxy-4-aethylphεnyl]bεnzaaidε dihydrochloridε NMR (CDCI3, δ) : 1.38-1.87 (6H, a), 2.06-2.45 (4H, a), 2.22 (3K, s), 2.25-2.44 (2H, a), 2.76 (3H, s) , 2.80 (3H, s), 3.07-3.22 (2H, m) , 3.24 (3H, s), 3.54 (2H, br), 3.77-3.95 (2H, m) , 3.80 (3H, ε) , 4.24 (2H, br), 6.57-6.62 (2H, ) , 6.80-7.08 (4H, a), 7.39- 7.47 (IH, a), 7.97 (IH, d, J=8Hz), 8.20-8.38 (2H, a) 7) 4-[2-(3-Aminoprop-l-yl)oxybenzoyl]amino-3-mεthoxy-N- mεthyl-N-[2-[5-[N-(2-dimεthylaminoεthyl)-N-mεthylamino- carbonyl]pent-1-yl]oxy-4-mεthylphenyl]benzamidε dihydrochloride NMR (CDCI3, δ) : 1.37-1.82 (6H, a), 2.22 (3H, s), 2.29-2.47 (4H, a), 2.85 (6H, s), 3.02 (3H, ε), 3.08-3.33 (6H, a), 3.26 (3K, ε), 3.58-3.95 (4H, a), 3.83 (3H, s), 4.28 (3H, br) , 6.55-6.65 (2H, a), 6.82-7.06 (5H, a), 7.39-7.47 (IH, a), 8.03 (IH, d, J=8Hz), 8.33 (IH, br) 8) 4-[2- (3-Aminoprop-l-yl)oxybenzoyl]amino-3-methoxy-N- methyl-N-[2-[5-[N-(3-dimεthylaminoprop-l-yl)carbamoyl]- pεnt-l-yl]oxy-4-mεthylphεnyl]bεnzamidε dihydrochloridε NMR (CDCI3, δ) : 1.37-1.99 (8H, m) , 2.23 (3K, s) , 2.25-2.44 (4H, a), 2.76 (6H, s), 3.05-3.41 (6H, a), 3.22 (3K, s), 3.78-3.94 (2H, a), 4.22 (2H, br) , 6.56 (2H, br), 6.81-7.04 (5K, a), 7.39 (IH, br) , 8.00 (IH, br), 8.29 (IH, br) , 8.56 (3H, br) 9) 4-[2- (3-Aainoprop-l-yl)oxybεnzoyl]amino-3-methoxy-N- aethyl-N-[2-[5-[N- (3-diaεthylaainoprop-l-yl)-N- methylcarbamoyl]pεnt-1-yl]oxy-4-mεthylphεnyl]bεnzamide dihydrochloride NMR (CDCI3, δ) : 1.33-1.99 (8K, m) , 2.26 (3H, s) , 2.26-2.47 (4H, m) , 2.78 (6H, s) , 2.96 (3H, s) , 3.05-3.39 (6H, a), 3.26 (3H, s) , 3.79-3.99 (2H, a), 3.78 (3H, s), 4.30 (2H, br) , 6.62 (2H, a), 6.83- 7.08 (5H, a), 7.45 (IH, br) , 8.01 (IH, br) , 8.35 (IH, br), 8.64 (2H, br) 10) 4-[2- (3-Aainoprop-l-yl)oxybenzoyl]aaino-3-aεthoxy-N- aethyl-N-[2-[5- (4-hydroxypipεridin-l-yl)carbonylpent-1- yl]oxy- -aethylphεnyl]bεnzaaidε hydrochloridε NMR (CDCI3, δ) : 1.32-2.06 (10H, a), 2.23 (3H, s) , 2.25-2.40 (4H, a), 2.99-3.07 (2H, a), 3.23 (3H, ε) , 3.43-4.00 (7H, a), 4.23 (2K, br) , 6.52-6.63 (2H, a), 6.81-7.12 (4H, a), 7.38-7.49 (IH, a), 7.97 (IH, br), 8.30 (IH, br) 11) 4-[2-(3-Aainoprop-l-yl)oxybenzoyl]aaino-3-aεthoxy-N- aethyl-N-[2-[5-(4-aminopiperidin-l-yl)carbonylpent-1- yl]oxy-4-methylphenyl]benzamide dihydrochloride NMR (CDC1 3 , δ) : 1.40-1.85 (12H, a), 2.24 (3H, ε) , 2.28-2.45 (2H), 2.87-3.11 (7H, a), 3.25 (3H, ε) , 3.84-4.00 (2H, a), 3.79 (3H, s) , 4.25 (2H, br) , 6.54-6.63 (2H, a), 6.95-7.09 (4H, a), 7.43 (IH, br), 8.04 (IH, br) , 8.41 (IH, br) 12) 4-[2-(3-Ammoprop-l-yl)oxybenzoyl]aaino-3-aεthoxy-N- aethyl-N-[2-[5- (4-methylpipεrazin-l-yl)aminocarbonyl- pent-l-yl]oxy-4-methylphenyl]benzamidε trihydrochloride NMR (CDCI3, δ) : 1.32-1.80 (6H, m) , 2.04-2.15 (2H, a), 2.26 (3K, s), 2.90-3.36 (10H, m) , 3.24 (3H, s) , 3.76 (3K, s), 3.85-4.02 (2H, m) , 4.26 (2H, br) , 6.54-6.63 (2H, a), 6.75-7.09 (4H, a), 7.40-7.49 (IH, a), 8.00 (IH, d, J=8Hz) , 8.39 (IH, br) , 8.62 (IH, br) 13) 4-[2- (3-Amιnoprop-l-yl)oxybenzoyl]amino-3-methoxy-N- methyl-N-[2-[5-[bis(2-hydroxyeth-l-yl)amino]carbonyl- pent-l-yl]oxy-4-mεthylphenyl]benzamide hydrochloride NMR (CDCI3, δ) : 1.50-1.88 (6H, a), 2.05-2.54 (4H, a), 2.28 (3H, s), 3.03 (2H, br) , 3.30 (3H, s) , 3.41- 3.69 (8H, a), 3.78 (3H, s), 3.82-4.00 (2H, a), 4.23 (2H, br), 6.59-6.69 (2H, a), 6.81-7.22 (4H, a), 7.46 (IH, br), 8.09 (IH, br) , 8.38 (IH, br) 14) 4-[2-(3-Aainoprop-l-yl)oxybenzoyl]aaino-3-aεthoxy-N- aethyl-N-[2-[5-(2,2-diaethylhydrazino)carbonylpent-1- yl]oxy-4-aethylphenyl]benzaaide dihydrochloride NMR (CDCI3, δ) : 1.36-1.82 (6H, a), 2.22 (3H, ε) , 2.26-2.39 (4H, a), 2.88-3.11 (2H, m) , 3.11 (6H, s) , 3.32 (3H, ε), 3.70-3.94 (2E, m) , 3.77 (3H, s), 4.21 (2H, br), 6.52-6.61 (2H, a), 6.80-7.14 (5H, a), 7.42 (IH, br), 7.97 (IH, br) , 8.25 (3H, br) 15) 4-[2-(3-Aainoprop-l-yl)oxybenzoyl]aaino-3-aethoxy-N- aethyl-N-[2-[5- (carbaaoylaethylaaino)carbonylpent-1- yl]oxy-4-methylphenyl]benzamide hydrochloride NMR (CDC1 3 , δ) : 1.20-1.68 (6H, m) , 2.08-2.41 (7H, a), 2.97-3.35 (5H, a), 3.29-4.27 (9H), 6.38-7.04 (6H, a), 7.90-8.29 (6H, a) 16) 4-[2- (3-Aminoprop-l-yl)oxybεnzoyl]amino-3-mεthoxy-N- mεthyl-N-[2-[5- (2-carbamoylethylamino)carbonylpent-1- yl]oxy-4-methylphenyl]benzamidε hydrochloride NMR (CDCI3, δ) : 1.36-1.81 (6E, a), 2.06-2.40 (6H, a), 2.23 (3H, ε), 3.13 (2H, br) , 3.22 (3H, s) , 3.32 (2H, br), 3.55-3.93 (2H, a), 3.78 (3H, s), 4.22 (2H, br), 6.53-6.63 (2H, a), 6.81-7.04 (5H, a), 7.39 (IH, br), 7.77 (IH, br) , 7.99 (IH, br) , 8.28- 8.47 (3H, a) 17) 4-[2- (3-Aminoprop-l-yl)oxybenzoyl]amino-3-methoxy-N- mεthyl-N-[2-[5- (4-pyridylaminocarbonyl)pεnt-1-yl]oxy-4- methylphenyl]benzamide dihydrochloride NMR (CDCI3, δ) : 1.25-1.83 (6H, m) , 2.10-2.49 (4H, m) , 2.22 (3H, s), 2.90-3.37 (2H, a), 3.23 (3K, s) , 3.68-3.95 (2H, a), 3.76 (3H, s) , 4.21 (2H, br) , 6.51-6.63 (2H, a), 6.66-7.04 (6H, a), 7.88-8.51 (7H, a) 18) 4-[2- (3-Aminoprop-l-yl)oxybenzoyl]amino-3-methoxy-N- methyl-N-[2-[5-[4- (diethylaminopipεridin-1- yl)carbonylpεnt-1-yl]oxy-4-mεthylphεnyl]bεnzamidε dihydrochloridε NMR (CDCI3, δ) : 1.38 (6H, t, J=8Hz) , 1.45-1.90 (10H, m), 1.93-2.08 (2H, m) , 2.28 (3H, ε), 2.30-2.48 (2H, m), 2.92-3.23 (5H, m) , 3.25-3.36 (4H, m) , 3.29 (3H, s), 3.69 (3H, s), 3.75-4.08 (3H, a), 4.28 (2H, br) , 6.54-6.65 (2H, a), 6.81-7.08 (5H, a), 7.45 (IK, br), 7.93 (IH, br) , 8.36 (IH, br) 19) 4-[2-(3-Aainoprop-l-yl)oxybenzoyl]aaino-3-aethoxy-N- aεthyl-N-[2-[6- (4-aεthylpipεrazin-l-yl)hex-l-yl]oxy-4- methylphenyl]benzamide trihydrochloride NMR (CDCI3, δ) : 1.36-1.94 (8H, m) , 2.21 (3H, ε) , 2.25-2.42 (2H, a), 2.90-3.39 (6H, a), 3.10 (3H, ε), 3.19 (3H, ε), 3.58-4.04 (6H, a), 3.82 (3H, ε) , 4.18 (IH, br), 6.46-6.63 (2H, a), 6.74-6.98 (4H, a), 7.38 (IK, br), 7.97 (IK, br) , 8.28 (IH, br) , 8.45 (2K, br) 20) 4- [2- (3-Aminoprop-l-yl) oxybenzoyl] amino-3-methoxy-N- [2- [4- (2-pyridyl)phenylaethyl]oxy-4-aethylphεnyl]-N- aethylbenzamide dihydrochloride NMR (CDCI3, δ) : 2.29 (3H, s) , 2.39 (2H, br) , 3.17 (2H, br), 3.37 (3H, s) , 3.44 (3H, br) , 4.12-4.30 (2H, m) , 4.73 (IH, br), 5.07 (IH, br) , 6.61 (IH, br), 6.70-6.79 (2H, m) , 6.94-7.03 (2H, m) , 7.12 (IH, d, J=8Hz), 7.38-7.47 (3H, m) , 7.89-8.23 (5H, a), 8.73 (3H, br), 8.90 (IH, br) 21) 4-[2-(3-Aminoprop-l-yl)oxybenzoyl]amino-3-methoxy-N-[2- [4-[ (4-methylpiperazin-l-yi)carbonylamino]but-l-yl]oxy- 4-mεthylphenyl]-N-methylbenzamide dihydrochloride NMR (CDCI3, δ) : 1.62-2.04 (4H, m) , 2.23 (3H, s) , 2.27-2.40 (2H, a), 2.74 (3H, s), 3.03-3.14 (2H, a), 3.22 (3H, s), 3.35-3.51 (4H, a), 3.78 (3H, s) , 3.85-3.96 (2H, a), 4.26 (2K, br) , 6.57-6.64 (2K, a), 6.67-7.09 (5H, a), 7.42 (IH, a), 7.96 (IH, d, J=8Hz ) , 8 . 30 (IH, d, J=8Hz ) , 8 . 60 (3H, br) 22) 4-[2- (3-Aminoprop-l-yl)oxybεnzoylamino]-3-methoxy-N-[2- [4-[ (4-dimεthylaminopipεridin-l-yl)carbonylamino]but-1- yl]oxy-4-m thylphεnyl]-N-mεthylbenzamide dihydrochloride NMR (CDC1 3 , δ) : 1.58-2.12 (10H, a), 2.27 (3H, s) , 2.30-2.48 (2H, a), 2.57-2.81 (8H, a), 3.05-3.31 (7H, a), 3.27 (3H, s) , 3.75-3.99 (5H, a), 4.27 (IH, br), 6.57-6.63 (2H, a), 6.85-7.09 (5H, a), 7.44 (2H, br), 7.96 (IH, br) , 8.34 (IH, br) , 8.75 (IH, br) 23) 4-[2-(3-Aminoprop-l-yl)oxybenzoyl]amino-3-methoxy-N-[2- (4-ureidobut-l-yl)oxy-4-methylphεnyl]-N-methylbenzamide hydrochloride NMR (CDCI3, δ) : 1.42-1.81 (4H, m) , 2.00-2.15 (2H, m) , 2.25 (3H, s), 2.88 (2H, t, J=5Hz) , 2.92 (2H, br) , 3.30 (3H, s), 3.63-3.80 (2H, a), 3.71 (3H, s), 4.21 (2K, t, J=5Hz), 6.51 (IH, s) , 6.71 (IH, d, J=8Kz) , 6.85-7.12 (5H, a), 7.44 (IH, dd, J=2, 8Hz) , 8.12 (IH, d, J=8Hz), 8.36 (IH, d, J=8Hz) 24) 4-[2-[3-Aminoprop-l-yl)oxy]benzoyl]amino-3-chloro-N- mεthyl-N-[2-[5- (4-dimεthylaminopipεridin-l- yl)carbonylpεnt-1-yloxy]-4-mεthylphεnyl]benzamide dihydrochloride NMR (DMSO-dg, δ) : 1.34-1.50 (2H, a), 1.50-1.62 (2H, m) , 1.65-1.80 (2H, a), 1.98-2.17 (4H, a), 2.22 (3H, s), 2.30-2.40 (2H, a), 2.66 (3H, s), 2.67 (3H, s), 2.85-3.05 (3H, a), 3.17 (3H, s), 3.33 (IH, br) , 3.80-4.07 (3H, a), 4.33-4.42 (2H, a), 4.47-4.57 (IH, a), 6.68 (IH, d, J=7Hz) , 6.82 (IH, s) , 7.08- 7.23 (3H, a), 7.29 (IH, d, J=7Hz), 7.41 (IH, s) , 7.68 (IH, t, J=6Hz), 7.92 (IH, d, J=7Hz) , 8.09 (IH, d, J=7Hz) 25) 3-(3-Aminoprop-l-yl)oxy-4-[2-[3-aminoprop-1-yl)oxy]- bεnzoyl]amino-N-mεthyl-N-[2-[5-(4-methylpiperazin-l- yl)carbonylpent-l-yloxy]-4-methylphεnyl]benzamide trihydrochloride NMR (DMSO-dg, δ) : 1.37-1.50 (2K, m) , 1.50-1.62 (2K, m), 1.67-1.80 (2H, m) , 1.97-2.19 (4H, rc), 2.22 (3K, s), 2.30-2.41 (2H, m) , 2.57 (IH, s) , 2.92 (6H, br) , 3.17 (3H, s), 3.68 (IH, br) , 3.93 (2H, br) , 4.10 (2K, br), 4.40 (2H, br) , 6.66 (IH, d, J=6Hz), 6.78- 6.87 (2H, m), 6.95-7.04 (2H, m) , 7.12 (IH, t, J=6Hz), 7.29(IK, d, J=7Hz) , 7.57 (IH, t, J=6Hz) , 7.93 (IH, d, J=6Hz),8.14 (IK, d, J=7Hz) 26) 2-Amino-4-[2-[ (3-aminoprop-l-yl)oxy]benzoyl]amino-N- methyl-N-[2-[5-(4-dimethylaminopiperidin-l- yl)carbonylpent-l-yloxy]-4-mεthylphεnyl]benzamide trihydrochloride NMR (DMSO-dg, δ) : 1.41-1.51 (2H, m) , 1.51-1.66 (IH, m), 1.74-1.84 (IH, m) , 1.98-2.12 (4H, m) , 2.30-2.40 (2K, m), 2.67 (3H, ε) , 2.68 (3H, ε), 2.89-3.06 (4H, m) , 3.16 (3H, ε), 3.33 (2H, br) , 3.96-4.10 (4H, m) , 4.13-4.20 (2H, m) , 4.47-4.58 (IH, m) , 6.60 (IH, d, J=7Kz), 6.78 (2H, s) , 6.85 (IH, s) , 6.97-7.07 (2H, m), 7.13 (IH, d, J=7Hz), 7.27 (IH, s) , 7.43-7.56 (2E, m) 27) 2-[2-[ (3-Aminoprop-l-yl)oxy]benzoyl]amino-N-methyl-N-[2- [5-(4-dimethylamnopiperidin-l-yl)carbonylpεnt-1-yloxy]- 4-methylphenyl]-5-pyridinecarboxamide trihydrochloride NMR (DMSO-dg, δ) : 1.32-1.80 (8H, m) , 1.97-2.20 (4H, m), 2.22 (3H, s) , 2.27-2.40 (3H, m) , 2.65 (3H, ε) , 2.67 (3H, ε), 2.92-3.10 (4H, m) , 3.19 (3K, s) , 3.33 (IH, br), 3.80-4.07 (3K, m) , 4.22-4.29 (2H, m) , 6.69 (IH, d, J=7Hz), 6.82 (IH, s), 7.07-7.14 (2H, m) , 7.20 (IH, d, J=7Hz), 7.56 (IH, t, J=6Hz) , 7.66 (IH, d, J=6Hz) , 7.78 (IH, d, J=7Hz) , 8.00-8. 04 (IH, a) , 8 .23 (IH, s) 28) 4-[N-[2-[ (3-Aminoprop-l-yl)oxy]phenyl]amino]methyl-3- mεthoxy-N-mεthyl-N-[2-[5-(4-mεthylpiperazin-l- yl)carbonylpent-l-yloxy]-4-mεthylphεnyl]benzamide trihydrochloride NMR (DMSO-dg, δ) : 1.35-1.49 (2H, m) , 1.49-1.62 (2H, a), 1.62-1.79 (2H, a), 2.01-2.16 (2H, a), 2.23 (3H, s), 2.34-2.40 (2H, a), 2.71 and 2.72 (total 3H, s), 2.76-3.12 (8H, a), 3.17 (3H, s) , 3.27-3.41 (2K, a), 3.41-3.54 (4H, a), 3.70-3.81 (IH, a), 3.89-3.98 (IK, a), 4.02-4.08 (3H, a), 4.25 (2H, s), 4.39-4.45 (IH, a), 6.60-6.80 (6H, a), 6.93 (2H, s), 6.98 (IH, d, J=7Hz), 7.10UH, d, J=7Hz) 29) 4-[2-[ (3-Aainoprop-l-yl)oxy]phεnyl]oxyaεthyl-3-aεthoxy- N-aethyl-N-[2-[5- (4-methylpiperazin-l-yl)carbonylpent-l- yloxy]-4-methylphεnyl]bεnzamidε dihydrochloride NMR (DMSO-dg, δ) : 1.39-1.50 (2H, m) , 1.50-1.63 (2H, m) , 1.65-1.82 (2K, a), 1.97-2.10 (2H, a), 2.21 (3H, ε), 2.35-2.41 (2H, a), 2.71 and 2.72 (total 3H, s), 2.78-3.10 (7H, a), 3.18 (3H, ε), 3.29-3.41 (2H, a), 3.41-3.67 (4H, a), 3.82 (IH, br) , 3.89-4.00 (IH, a), 4.00-4.12 (3H, m) , 4.38-4.48 (IK, m) , 4.57 and 4.93 (total 2H, s) , 6.61 (IH, d, J=7Hz) , 6.69-6.97 (6H, a) , 6.97-7.07 (2H, a), 7.20-7.25 (IH, a) 30) 4-[2-[ (3-Aainoprop-l-yl)oxy]benzoyl]aaino-3-benzyloxy-N- aεthyl-N-[2-[5-(4-aethylpiperazin-l-yl)carbonylpent-l- yloxy]-4-aethylphenyl]benzaaidε dihydrochloride NMR (DMSO-dg, δ) : 1.37-1.50 (2H, a), 1.50-1.63 (2H, a), 1.63-1.79 (2H, a), 1.79-1.91 (2H, a), 2.22 (3H, ε), 2.39 (2H, t, J=6Hz), 2.60-2.77 (5H, a), 2.79- 3.10 (4H, a), 3.15 (3H, s), 3.30-3.67 (3H, m) , 6/41795 - 264 - 3.77-4 .12 (5H, a) , 4 .37-4 .49 (IH, m) , 5.06 (2H, s) , 6. 62 (IK, d, J=6Hz) , 6.82 (IH, s) , 6.90 (IH, d, J=7Hz) , 6. 97 (IH, d, J=7Hz) , 7.03 (IH, s) , 7.12 (IH, t, J=7Hz) , 7 .22 (IH, d, J=7Hz) , 7.30-7 .46 (5H, a) , 7.54 (IH, t, J=6Kz) , 7.97 (IH, d, J=7Hz) , 8.23 (IH, d, J=7Hz) 31) 4-[2-[ (3-Aminoprop-l-yl)oxy]benzoyl]amino-3-hydroxy-N- aethyl-N-[2-[5- (4-methylpipεrazin-l-yl)carbonylpent-1- yloxy]-4-methylphenyl]benzamide dihydrochloride NMR (DMSO-dg, δ) : 1.43 (2H, br) , 1.49-1.62 (2H, m) , 1.63-1.82 (2H, a), 2.00-2.40 (16H, a), 2.90-2.97 (2H, a), 3.14 (3H, s) , 3.30-3.50 (5H, a), 3.89 (2H, br), 4.20-4.38 (2H, a), 6.50-6.68 (2H, a), 6.80 (IH, s), 6.87-6.99 (2H, a), 7.12 (IH, t, J=6Hz), 7.22 (IK, d, J=6Hz), 7.49-7.60 (IH, a), 7.97-8.18 (2H, a) 32) 4-[2-[ (3-Aainoprop-l-yl)oxy]benzoyl]aaino-3- ethoxycarbonylaethoxy-N-aethyl-N-[2-[5-(4- aethylpiperazin-1-yl)carbonylpent-l-yloxy]-4- methylphenyl]benzamide dihydrochloride NMR (DMSO-dg, δ) : 1.09 and 1.22 (total 3H, t, J=6Hz) , 1.37-1.51 (2H, m), 1.51-1.66 (2H, a), 1.67-1.80 (2H, a), 2.05-2.18 (2H, a), 2.23 (3H, ε), 2.38 (2H, t, J=6Hz), 2.73-2.74 (3H, a), 2.90-3.10 (5H, a), 3.17 (3K, ε), 3.30-3.58 (2H, a), 3.80-4.00 (2H, a), 4.00-4.20 (3H, a), 4.32-4.50 (3H, a), 4.80 (2H, s), 6.62 (IH, d, J=6Hz), 6.82 (IH, s) , 6.89-6.92 (2H, a), 7.01 (IH, d, J=7Hz), 7.15 (IH, t, J=6Hz), 7.27 (IK, d, J=7Hz), 7.58 (IH, t, J=6Hz) , 8.00 (IH, d, J=6Hz), 8.27 (IH, d, J=7Hz) 33) 4-[2-[ (3-Aminoprop-l-yl)oxy]benzoyl]amino-3- aethoxycarbonylmethoxy-N-aethyl-N-[2-[5- (4- methylpiperazin-1-yl)carbonylpent-l-yloxy]-4- mεthylphεnyl]bεnzamidε dihydrochloridε NMR (DMSO-dg, δ) : 1.35-1.50 (2H, m) , 1.50-1.63 (2H, a), 1.63-1.90 (2H, a), 2.00-2.14 (2H, a), 2.21 (3H, 8), 2.25-2.43 (2H, a), 2.71 (3H, s) , 2.77-3.05 (5H, a), 3.15 (3H, s) , 3.18-3.57 (6H, a), 3.70 (3H, s) , 3.73-4.12 (3K, a), 4.12-4.49 (3H, a) , 4.80 (2H, s) , 6.63 (IK, d, J=7Hz), 6.70-7.20 (5H, a), 7.27 (IH, d, J=7Hz), 7.57 (IH, t, J=7Hz) , 7.93-8.10 (IH, a), 8.23 (IH, d, J=6Hz) 3 ) 4_ 2- [ (3-Aainoprop-l-yl)oxy]benzoyl]aaino-3- dimethylaminocarbonylmεthoxy-N-methyl-N-[2-[5-(4- methylpiperazin-1-yl)carbonylpent-l-yloxy]-4- methylphεnyl]benzamide dihydrochloride NMR (DMSO-dg, δ) : 1.37-1.49 (2H, m), 1.50-1.62 (2H, a), 1.63-1.79 (2H, m) , 1.98-2.10 (2K, a), 2.21 (3H, s), 2.32-2.43 (2H, m) , 2.71 (3H, s) , 2.86 (3H, s) , 2.98 (3H, s), 2.82-3.05 (5H, a), 3.15 (3H, s) , 3.90 (2H, br), 4.02-4.12 (2K, a), 4.28-4.38 (2H, a), 4.38-4.48 (IH, a), 4.83 (2K, s) , 6.62 (IH, d, J=7Hz), 6.80 (IE, s), 6.82-6.92 (2K, a), 7.00 (IH, c, J=7Hz), 7.12 (IH, t, J=7Kz) , 7.23 (IH, d, J=7Hz), 7.55 (IH, t, J=7Hz) , 8.20 (IH, d, J=7Hz) 35) 4-[2-[ (3-Aainoprop-l-yl)oxy]benzoyl]aaino-3- methylaminocarbonylmεthoxy-N-methyl-N-[2-[5-(4- methylpiperazin-1-yl)carbonylpent-l-yloxy]-4- methylphεnyl]bεnzamidε dihydrochloridε NMR (DMSO-dg, δ) : 1.38-1.51 (IH, a), 1.51-1.65 (2H, a), 1.68-1.80 (2H, a), 2.00-2.23. (2H, a), 2.22 (3H, ε), 2.34-2.40 (3H, a), 2.50 (3H, s) , 2.58 (2H, br) , 2.62 (3H, 8), 2.63 (3H, s) , 2.90 (4H, br) , 3.15 (3H, s), 3.88-3.97 (2H, a), 4.26-4.33 (2H, " a), 4.37-4.54 (2H, a), 6.62 (IH, d, J=7Kz) , 6.82 (2H, s) , 6. 88 (IH, d, J=7Hz) , 6.97 (IH, d, J=7Hz) , 7.12 (IH, t, J=7Hz) , 7.22 (IH, d, J=7Hz) , 7 .57 (IH, t, J=7Hz) , 7. 90 (IH, d, J=7Hz) , 8 .12-8 .25 (2H, a) 36) 4-[2-[ (3-Aminoprop-1-yl)oxy]benzoyl]amino-3- aminocarbonylmethoxy-N-methyl-N-[2-[5- (4- methylpiperazin-1-yl)carbonylpent-l-yloxy]-4- mεthylphεnyl]bεnzamide dihydrochloride NMR (DMSO-dg, δ) : 1.38-1.52 (2H, m) , 1.52-1.67 (2H, m), 1.68-1.83 (2H, m) , 2.00-2.15 (2H, m) , 2.23 (3H, s), 2.39 (2H, t, J=6Hz), 2.62 and 2.63 (total 3H, s), 2.72 and 2.73 (total 3H, s) , 2.80-3.10 (6H, m) , 3.15 (3H, s), 3.87-3.98 (2H, m) , 4.03-4.13 (IH, ) , 6.27-6.37 (IH, m) , 6.37-6.56 (2H, m) , 6.62 (IH, d, J=7Hz), 6.82 (2H, s), 6.90 (IH, d, J=7Hz) , 6.98 (IH, d, J=6Kz), 7.12 (IH, t, J=7Hz) , 7.26 (IH, d, J=7Hz), 7.57 (IH, t, J=6Hz) , 7.92 (IH, d, J=7Hz) , 8.13-8.30 (2H, m) 37) 4-[2-[ (3-Aminoprop-l-yl)oxy]bεnzoyl]amino-N-mεthyl-N-[2 [5-(4-mεthylpipεrazin-l-yl)carbonylpent-l-yloxy]-4- methylphenyl]-3-propoxybenzamide dihydrochloride NMR (DMSO-dg, δ) : 0.89 (3H, t, J=6Hz) , 1.37-1.50 (2H, a), 1.50-1.68 (4H, a), 1.68-1.80 (2H, a), 2.02-2.1 (2H, a), 2.20 (3H, s), 2.38 (2H, t, J=6Hz), 2.47 (3H, ε), 2.75-3.12 (5H, a), 3.17 (3H, s) , 3.30-3.4 (2H, a), 3.42-3.56 (IH, m) , 3.80-4.00 (4H, m) , 4.00-4.13 (IH, m), 4.32-4.50 (4H, a), 6.61 (IH, d, J=7Hz), 6.82 (IH, s), 6.88 (IK, s) , 6.94 (IH, d, J=7Hz), 7.02 (IH, d, J=7Hz) , 7.13 (IH, t, J=7Hz) , 7.29 (IH, d, J=7Hz), 7.56 (IH, t, J=7Hz), 7.97 (IH d, J=7Hz), 8.22 (IH, d, J=7Hz) 38) 4-[2-[ (3-Aainoprop-l-yl)oxy]benzoyl]aaino-3-isopropoxy- N-methyl-N-[2-[5-(4-aethylpiperazin-l-yl)carbonylpent-1 yloxy]-4-methylphenyl]bεnzamidε dihydrochloride NMR (DMSO-dg, δ) : 1.10-1.27 (6H, a), 1.37-1.50 (2H, a), 1.50-1.64 (2H, a), 1.67-1.82 (2H, a), 2.03-2.07 (2H, a), 2.22 (3H, s) , 2.39 (2K, t, J=6Hz) , 2.72 and 2.73 (total 3H, s), 2.78-3.12 (6H, a), 3.17 (3H, s), 3.30-3.43 (2H, a), 3.43-3.60 (IH, a), 3.80-4.02 (2H, a), 4.02-4.13 (IH, a), 4.23-4.50 (4H, a), 6.64 (IH, d, J=7Kz) , 6.81-6.90 (2H, a), 6.98 (IH, d, J=7Hz), 7.03 (IH, d, J=7Hz) , 7.13 (IH, t, J=6Hz), 7.32 (IH, d, J=7Hz) 7.56 (IH, t, J=6Hz) , 7.94 (IK, d, J=6Hz), 8.22 (IH, d, J=7Hz) 39) 2-[2-[ (3-Aminoprop-1-yl)oxy]benzoyl]amino-N-mεthyl-N-[2- [5- (4-mεthylpiperazin-l-yl)carbonylpent-l-yloxy]-4- methylphenyl]-5-thiophenεcarboxamidε dihydrochloride NMR (DMSO-dg, δ) : 1.20-1.38 (2H, a), 1.38-1.52 (2H, a), 1.53-1.70 (2H, a), 1.98-2.10 (2H, a), 2.22-2.32 (2H, a), 2.33 (3H, s) , 2.69-2.72 (3H, a), 2.76-3.07 (5H, a), 3.16 (3H, s) , 3.27-3.54 (3H, a), 3.78-4.09 (3H, a), 4.10-4.20 (2H, a), 4.33-4.47 (2H, a), 6.15 (IH, br) , 6.55 (IH, d, J=5Hz), 6.81 (IH, d, J=7Hz) , 6.97 (IH, s), 7.07 (IH, t, J=6Hz) , 7.13-7.20 (2H, a), 7.44-7.60 (2H, a) Example 105 To a solution of 4-[2- [ (3-tert-butoxycarbonylaminoprop- 1-yl)oxy]benzoyl]amino-3-mεthoxy-N-methyl-N- (4- hydroxyphenyl)benzamide (50 mg) in chloroform (3.0 ml) was added a solution of 4N hydrogen chloride in εthyl acεtatε (1.0 ml) and the mixture was stirred at ambient tempεraturε for 2 hours. Thε rεsulting mixture waε evaporated in vacuo and the residue was solidified with diethyl εthεr. Diethyl ethεr was removed in vacuo to give 4-[2-[ (3-aminoρrop-l- yl)oxy]benzoyl]amino-3-mεthoxy-N-methyl-N- (4-hydroxyphenyl)- bεnzamidε hydrochloridε (40 mg) . NMR (DMSO-dg, δ) : 2.11-2.21 (2H, a) , 2. 96 (2H, q, J=8Hz ) , 3 . 30 (3H, s) , 3 .78 (3H, s) , 4 .37 (2H, t, J=8Hz) , 6. 66 (2H, d, J=8Kz) , 6.88 (IH, d, J=8Hz) , 6. 97 ( IH, ε ) , 6. 99 (2H, d, J=8Hz) , 7.15 (IH, t, J=8Hz) , 7 .27 (IH, d, J=8Hz) , 7 .55-7. 62 (IH, a) , 7.97-8.05 (3H, a), 8.28 (IK, d, J=8Kz) , 9.54-9.59 (IK, br s) ESI-MASS (m/z) : 450 (M-r-H) Example 106 The following compound was obtained according to a similar manner to that of Example 105. 4-[2-[ (3-Amιnoprop-l-yl)oxy]benzoyl]amino-3- carboxymethoxy-N-methyl-N-cyclohexylbenzamidε hydrochloride NMR (DMSO-d 6 , δ) : 1.02-1.10 (2H, a), 1.46-1.80 (8H, a), 2.08-2.12 (2H, a), 2.80 (3H, s) , 2.92-2.99 (2H, a), 3.30-3.47 (2H, br) , 4.39 (2H, t, J=7Hz) , 4.96 (2H, s), 6.98-7.04 (2H, br s), 7.18 (IH, t, J=8Hz) , 7.30 (IH, d, J=8Hz), 7.60 (IH, t, J=8Hz), 7.95-8.05 (3H, br), 8.07 (IH, d, J=8Hz) , 8.51 (IH, d, J=8Hz) ESI-MASS (m/z) : 484 (M+H) Example 107 1) A solution of 4-[2-[3- (9-fluorenylaethyDoxycarbonyl- aaininoprop-l-yl]thiobenzoyl]aaino-3-aethoxy-N-aethyl-N-[2- [5- (4-diaethylaminopiperidin-l-yl)carbonylpent-l-yl]oxy-4- mεthylphεnyl]benzamide (110 mg) in a mixture of N,N- dimethylformamide and piperidine (4:1, 5 ml) was stirred at ambient tεmpεraturε for 30 minutεs and thε rεsulting solution was dilutεd with ethyl acetatε (20 ml) . The solution was washed with water (10 ml x 3) and brine, and the solution was dried over potasεium carbonatε. Thε solvεnt was evaporated and the residue was purified on basic silica gεl column chromatography (Si0 2 30 g, 1-15% mεthanol in chloroform) to give 4-[2-(3-aminoprop-l-yl)thiobεnzoyl]amino-3-methoxy-N- methyl-N-[2-[5-(4-dimethylaminopipεridin-l-yl]carbonylpεnt-1- yl]oxy-4-methylphenyl]benzamide. NMR (CDC1 3 , δ) : 1.36-1.92 (12H, m) , 2.29 (6H, s) , 2.30 (3H, s), 2.36 (2H, t, J=5Hz) , 2.59 (IH, t, J=11HZ), 2.77 (2H, t, J=5Hz) , 2.99 (2H, t, J=5Hz) , 3.32 (3H, ε), 3.75 (3H, s) , 3.85-4.03 (4H, ) , 6.57-6.66 (2H, m) , 6.84-6.90 (IH, d, J=8Hz) , 7.02 (IH, s), 7.39-7.48 (3H, m) , 7.65 (IH, d, J=8Hz) , 8.30 (IK, d, J=8Hz), 8.80 (IH, s) 2) To a εolution of the obtained compound in ethanol (5 ml) was added IN hydrochloric acid (0.15 ml). The volatile solvεnt was removed by evaporation and thε rεsidue was lyophilized to give 4-[2- (3-aminoprop-l-yl)thiobenzoyl]amino- 3-methoxy-N-methyl-N-[2-[5-(4-dimethylaminopipεridin-l-yl]- carbonylpent-l-yl)oxy-4-methylphεnyl]bεnzamidε dihydrochloride (45 mg) . NMR (CDCI3, δ) : 1.44-1.92 (6H, m) , 2.02-2.16 (2H, m) , 2.28 (3K, s), 2.30-2.41 (2H, a), 2.73 (6H, br) , 2.99-3.14 (2H, a), 3.27-3.33 (IK, a), 3.31 (3H, s) , 3.62-3.79 (4H, a), 3.71 (3H, s) , 3.82-4.10 (2H, a), 6.55-6.67 (2H, a), 6.83-7.02 (5H, m) , 7.35-7.52 (2H, m), 8.23 (IH, br), 8.54 (2H, br) Example 108 The following compound was obtainεd according to a similar manner to that of Example 15. 4-2- (3-Dimethylaminoprop-l-yl)oxybenzoyl]amino-3- methoxy-N-mεthyl-N-[2-[5-(4-dimethylaminopipεridin-l- yl)carbonylpent-1-yl]oxy-4-methylphenyl]benzamide NMR (CDCI3, δ) : 1.49-1.60 (2H, m) , 1.66-1.95 (4H, m) , 2.21 (6H, s), 2.27 (6H, s), 2.35-2.48 (4H, m) , 2.58 (2H, t, J=llHz), 3.32 (2H, t, J=llHz) , 3.33 (3H, - 270 - •' • 3 80 (3H , .,, 3.82-4.00 ( 2H, „, . 4 . 25 ,_, * ■ »«,. 4.64 < lH , br) , 6 . 55-6 . 64 », «»_,, 6.89 UH, d, »,, ,,., ; 7 ic ,ι,, , _ «« '.__ ι,_rl, a), 7.26 _ s) , 7.40-7.48 (1H , _, , 8 . 21 , J-8 n _ ) , 8.40 (IH, d, J-8H Z)

Claims: C L A I M S 1. A compound of the formula : 5 wherεin R 1 is aryl, cyclo(lowεr)alkyl or a hεtεrocyclic group, each of which may be substitutεd with substituεnt(s) selected from the group consisting of halogen; hydroxy; nitro; amino; acyl; subεtitutεd acyl; 0 acyl(lowεr)alkylsulfinyl; acyl (lowεr)alkylsulfonyl; acyloxy; lower alkylamino(lower)alkylcarbamoyloxy; aryl; cyano; a heterocyclic group; lowεr alkenyl optionally substituted with acyl, substituted acyl, aryl or acyl-substituted aryl; 5 lower alkynyl optionally subεtituted with amino, acylamino or substituted acylamino; lower alkyl optionally substituted with halogen, amino, lower alkylamino, acylamino, substituted acylamino, hydroxy, acyloxy, acyl(lower)alkanoyloxy, Q acyl, substituted acyl, acyl (lower)alkoxyimino, aryl or acyl-substituted aryl; lowεr alkylthio optionally substituted with acyl or substituted acyl; alkoxy optionally substituted with aryl, substituted c aryl, hydroxy, acyloxy, amino, lower alkylamino. protected amino, a heterocyclic group, acyl- substituted pyridyl, substituted acyl-substituted pyridyl, halogen, acyl(lower)alkylamino, N-protected- acyl(lower)alkylamino, N-acyl(lower)alkyl-N-lower alkylamino, acyl, substituted acyl, acylamino, subεtituted acylamino, lower alkylhydrazinocarbonylamino, hydroxyimino, acyl(lower)alkoxyimino, substituted acyl (lower)alkoxyimino, acyl(lower)alkoxy, guanidino or N-protected guanidino; and lower alkenyloxy optionally subεtituted with acyl or substituted acyl; R 2 is hydrogen; lower alkyl optionally substituted with hydroxy, aryl or acyl; or cyclo(lowεr)alkyl; R 3 is hydrogεn; halogen; hydroxy; acyloxy; substituted acyloxy; lower alkyl optionally substituted with hydroxy or lower alkoxy; lower alkoxy optionally substituted with aryl, amino, protectεd amino, acyl, hydroxy, cyano or lowεr alkylthio; nitro; amino; acyl; substitutεd acyl; or cyclo(lower)alkyloxy; R 4 is hydroxy; halogen; nitro; amino; protected amino; lowεr alkylamino; acyloxy; amino(lower)alkylamino; N-protected amino(lower)alkylamino; lower alkoxy optionally substituted with hydroxy, aryl, substituted aryl, acyl, substituted acyl, amino, lower alkylamino, acylamino, substituted acylamino, protectεd amino, a heterocyclic group or guanidino; lower alkylthio optionally substituted with acyl, substituted acyl, amino, lower alkylamino, acylamino, substituted acylamino, protεcted amino, a heterocyclic group, hydroxy, lower alkylsulfonyloxy, arylsulfonyloxy, ar(lower)alkoxy or substituted ar(lower)alkoxy; lowεr alkyl substituted with acyl, substituted acyl, amino, lower alkylamino, acylamino, substituted acylamino, protected amino, a heterocyclic group, hydroxy, lower alkylsulfonyloxy or arylsulfonyloxy; lower alkenyl optionally substituted with acyl; lower alkynyl optionally substituted with hydroxy, amino, protected amino, lower alkylsulfonyloxy or arylsulfonyloxy; amino(lower)alkylsulfonyl; N-protected amino(lower)alkylsulfonyl; lowεr alkylaminosulfonyl; a heterocyclicsulfonyl; amino(lower)alkylsulfinyl; N-protected amino(lowεr)alkylsulfinyl; pipεridyloxy; or N-protected piperidyloxy; R 5 is hydrogen, lower alkyl, lowεr alkoxy or halogen; A is a single bond, 0 or NH; 0 0 E is lowεr alkylene, lower alkenylene, ___ ___ or o a group of the formula : -G-J- R 6 in which G is lower alkylene and J is 0 or -_j- (wherein R 6 is hydrogen or N-protective group) ; X is -CH=CH-, -CH=N- or S; and Y is CH or N; and pharmacεutically acceptable saltε thereof. 2. A compound accordidng to claim 1, wherein R 1 is aryl which may be subεtituted with lower alkoxy optionally εubstituted with acylamino or acyl; R 2 iε lower alkyl; R 3 iε hydrogen, lower alkyl or lower alkoxy; R is hydroxy, or lower alkoxy, lower alkylthio or lowεr alkyl, each of which may be εubstituted with hydroxy, aryl, subεtituted aryl, acyl, amino, lower alkylamino, acylamino, protected amino or a heterocyclic group; R iε hydrogen, lower alkyl, lower alkoxy or halogen; A is NH; 0 E is .c ; X is -CH=CH-; and Y is CH. A compound according to claim 2, wherein R 1 is phenyl or tolyl, each of which is subεtituted with lower alkoxy substituted with acyl; R 3 is lower alkoxy or lower alkyl; and R 4 is lower alkoxy, lower alkylthio or lower alkyl, each of which is substituted with amino or hydroxy. A compound according to claim 3, wherein R 1 is phenyl or tolyl, εach of which is subεtituted with lower alkoxy εubstituted with N-(lower alkyl)pipεrazinylcarbonyl; R J iε lowεr alkoxy; R 4 iε lower alkoxy εubstituted with amino; and R 5 is hydrogen. A process for preparing the formula wherεin R 1 is aryl, cyclo(lowεr)alkyl or a hεterocyclic group, εach of which may be substituted with subεtituent(s) 6/41795 - 275 - selected from the group consisting of halogen; hydroxy; nitro; amino; acyl; subεtituted acyl; acyl(lower)alkylεulfinyl; acyl(lower)alkylεulfonyl; acyloxy; lower alkylamino(lower)alkylcarbamoyloxy; aryl; cyano; a heterocyclic group; lowεr alkεnyl optionally substituted with acyl, substituted acyl, aryl or acyl-subεtituted aryl; lower alkynyl optionally εubεtituted with amino, acylamino or εubstituted acylamino; lower alkyl optionally substituted with halogen, amino, lower alkylamino, acylamino, substituted acylamino, hydroxy, acyloxy, acyl (lowεr)alkanoyloxy, acyl, subεtitutεd acyl, acyl(lowεr)alkoxyimino, aryl or acyl-εubεtitutεd aryl; lowεr alkylthio optionally substitutεd with acyl or substitutεd acyl; alkoxy optionally εubεtitutεd with aryl, substitutεd aryl, hydroxy, acyloxy, amino, lowεr alkylamino, protected amino, a heterocyclic group, acyl- subεtituted pyridyl, εubstituted acyl-substituted pyridyl, halogen, acyl(lowεr)alkylamino, N-protected- acyl(lowεr)alkylamino, N-acyl(lowεr)alkyl-N-lower alkylamino, acyl, subεtituted acyl, acylamino, εubεtituted acylamino, lower alkylhydrazinocarbonylamino, hydroxyimino, acyl (lower)alkoxyimino, εubstituted acyl (lower)alkoxyimino, acyl(lower)alkoxy, guanidino cr N-protected guanidino; and lower alkenyloxy optionally subεtituted with.acyl or εubεtitutεd acyl; R 2 iε hydrogεn; lowεr alkyl optionally εubstituted with hydroxy, aryl or acyl; or cyclo(lower)alkyl; R 3 is hydrogen; halogen; hydroxy; acyloxy; subεtituted acyloxy; lower alkyl optionally εubεtituted with hydroxy or lower alkoxy; lowεr alkoxy optionally substituted with aryl, amino, protected amino, acyl, hydroxy, cyano or lower alkylthio; nitro; amino; acyl; substituted acyl; or cyclo(lower)alkyloxy; 4 is hydroxy; halogen; nitro; amino; protected amino; lower alkylamino; acyloxy; amino(lower)alkylamino; N-protectεd amino(lowεr)alkylamino; lower alkoxy optionally subεtituted with hydroxy, aryl, εubεtituted aryl, acyl, εubεtituted acyl, amino, lowεr alkylamino, acylamino, εubεtitutεd acylamino, protεctεd amino, a heterocyclic group or guanidino; lowεr alkylthio optionally substituted with acyl, subεtituted acyl, amino, lower alkylamino, acylamino, εubstitutεd acylamino, protεcted amino, a heterocyclic group, hydroxy, lower alkylsulfonyloxy, arylsulfonyloxy, ar(lower)alkoxy or substituted ar(lower)alkoxy; or lower alkyl substituted with acyl, substituted acyl, amino, lower alkylamino, acylamino, subεtituted acylamino, protected amino, a hetεrocyclic group, hydroxy, lowεr alkylsulfonyloxy or arylsulfonyloxy; lower alkenyl optionally subεtituted with acyl; lower alkynyl optionally substituted with hydroxy, amino, protected amino, lower alkylsulfonyloxy or arylsulfonyloxy; amino(lower)alkylsulfonyl; N-protected amino(lower)alkylsulfonyl, lower alkylaminosulfonyl; a hetεrocyclicεulfonyl; amino(lower)alkylεulfinyl; N-protected amino(lower)alkylsulfinyl; piperidyloxy; or N-protected piperidyloxy; R^ is hydrogen, lower alkyl, lowεr alkoxy or halogεn; A is a single bond, 0 or NH; 0 0 E is lower alkylene, lower alkenylenε, ___, ___, or a group of the formula : ° -G-J- in which G iε lowεr alkylene and J iε 0 or - (wherεin R° iε hydrogen or N-protectivε group) ; X is -CH=CH-, -CH=N- or S; and Y is CH or N; or pharmacεutically acceptable εalts therεof, which compriεεε, 1) rεacting a compound of the formula : or its salt with a compound of the formula or its reactivε derivative at the carboxy group or the sulfo group, or a εalt thereof to provide a compound of the formula : or its salt, in the above formulas, R 1 , R 2 , R 3 , R 4 , R 5 , X and Y are each as defined 2) reacting a compound of the formula or its salt with a compound of the formula or its reactivε derivative at the carboxy group or a salt thereof to provide a compound of the formula : or its salt, in the above formulas, R 1 , R 2 ',, RR 3 ,, RR 4 ,, R 5 , A, E, X and Y are each as defined above, or subjecting a compound of the formula or its salt to deesterification reaction to provide a compound of the formula : or its salt, in the above formulas, R 2 , R 3 , R 4 , R 5 , A, E, X and Y are each as definεd abovε, R^ is aryl, haloaryl, cyclo(lowεr)alkyl or a hεtεrocyclic group, εach of which is substituted with esterified carboxy; lower alkenyl subεtituted with eεterified carboxy or eεterified carboxy- εubεtituted aryl; lower alkyl εubstituted with esterified carboxy, esterifiεd carboxy(lowεr)alkanoyloxy or εstεrified carboxy(lower)alkoxyimino; lower alkylthio εubεtituted with estεrified carboxy; alkoxy substituted with esterified carboxy- εubεtituted aryl, eεtεrified carboxy-εubstituted pyridyl, esterified carboxy(lower)alkylamino, N-protεcted-esterified carboxy(lower)alkylamino, N-estεrifiεd carboxy(lower)alkyl-N-lower alkylamino, esterified carboxy or esterified carboxy(lower)alkoxyimino; or lower alkenyloxy substituted with esterifiεd carboxy; and R^ is aryl, haloaryl, cyclo(lower)alkyl or a heterocyclic group, each of which iε εubstituted with carboxy; lower alkenyl εubstituted with carboxy; lower alkyl εubεtituted with carboxy or carboxy- substitutεd aryl, carboxy(lower)alkanoyloxy or carboxy(lower)alkoxyimino; lower alkylthio substituted with carboxy; alkoxy substituted with carboxy-substituted aryl, carboxy-substituted pyridyl, carbox (lower)alkylamino, N-protected- carboxy(lower) lkylamino, N-carboxy(lowεr)alkyl-N- lower alkylamino, carboxy or carboxy(lower)alkoxyimino; or lower alkenyloxy substituted with carboxy; or 4) subjecting a compound of the formula : or its salt to dεesterification rεaction to providε a compound of the formula : or its salt, in the above formulas, R 1 , R 2 , R 3 , R 5 , A, E, X and Y are each as defined above, R 4 is lower alkoxy substitutεd with esterifiεd carboxy; lower alkylthio substituted with εster.ified carboxy; lower alkyl subεtituted with esterifiεd carboxy; or lower alkenyl subεtitutεd with εεtεrifiεd carboxy; and R j is lowεr alkoxy substituted with carboxy; lowεr alkylthio subεtituted with carboxy; lower alkyl εubεtituted with carboxy; or lower alkenyl substituted with carboxy; or 5) subjecting a compound of the formula : or its salt to elimination reaction of the N-protective group to provide a compound of the formula : or its salt, in the above formulas, R 1 , R 2 , R 3 , R 5 , A, E, X and Y are each as defined above, R 4 is protected amino; N-protectεd piperidyloxy; N-protectεd amino(lower)alkylamino; lower alkoxy substitutεd with protεctεd amino; lower alkylthio substituted with protectεd amino; lowεr alkyl subεtitutεd with protεctεd amino; lower alkynyl substituted with protectεd amino; or N-protεcted aaino(lower)alkylsulfonyl; and R 4 ! is amino; pipεridyloxy; amino (lowεr)alkylamino; lowεr alkoxy substituted with amino; lower alkylthio substitutεd with amino; lowεr alkyl subεtituted with amino; lower alkynyl εubεtituted with amino; or amino (lowεr) alkylεulfonyl; or 6) rεacting a compound of the formula : or its reactivε dεrivativε at thε carboxy group or a salt thεrεof with an aminε or its salt to providε a compound of the formula : or its salt, in the above formulas, R^, R 2 , R 3 , R 4 , R 5 , A, E, X and Y are each as definεd abovε, and R is aryl, haloaryl, cyclo(lower)alkyl or a heterocyclic group, each of which is substituted with subεtituted or unεubεtituted N-containing heterocycliccarbonyl; carbamoyl; εubεtituted or unsubstituted lower alkylcarbamoyl; lower alkenyl substituted with substituted or unsubεtituted N-containing heterocycliccarbonyl, carbamoyl, εubεtituted or unεubstitutεd lower alkylcarbamoyl or N-containing heterocycliccarbonyl-substituted aryl; 0 lowεr alkyl substitutεd with substitutεd or unsubstitutεd N-containing hεterocycliccarbonyl, carbamoyl, subεtituted or unεubstituted lowεr alkylcarbamoyl, substituted or unsubstituted N-containing heterocycliccarbonyl (lower)alkanoyloxy, carbamoyl(lower)alkanoyloxy, subεtituted or unεubεtituted lower alkylcarbamoyl(lower)alkanoyloxy, substituted or unsubstituted N-containing heterocycliccarbonyl(lower)alkoxyimino, carbamoyl (lower)alkoxyimino or substituted or _ 0 unsubstituted lower alkylcarbamoyl(lower)alkoxyimino; lower alkylthio substituted with substituted or unsubstituted N-containing heterocycliccarbonyl, carbamoyl or substituted or unsubstituted lower alkylcarbamoyl; alkoxy subεtituted with substituted _ c or unsubstituted N-containing heterocycliccarbonyl- substitutεd aryl, carbamoyl-substituted aryl, substituted or unsubstituted lower alkylcarbamoyl- subεtitutεd aryl, εubstitutεd or unsubεtitutεd N- containing hεterocycliccarbonyl-substituted pyridyl, _ n carbamoyl-subεtituted pyridyl, εubstituted or unsubstituted lower alkylcarbamoyl-subεtituted pyridyl, εubstituted or unsubstituted N-containing hεtεrocycliccarbonyl(lowεr)alkylamino, carbamoyl(lowεr)alkylamino, substituted or unsubstituted lowεr alkylcarbamoyl (lowεr)alkylamino. N-protected-(εubεtituted or unεubstituted N-containing hetεrocyclic)carbonyl (lowεr)alkylamino, N-protected-carbamoyl(lower)alkylamino, N-protected- substitutεd or unsubstituted lower alkylcarbamoyl- (lower)alkylamino, N-(subεtituted or unsubstituted N-containing heterocyclic)carbonyl (lower)alkyl-N- lower alkylamino, N-carbamoyl (lower)alkyl-N-lowεr alkylamino, subεtitutεd or unεubεtitutεd N-lower alkylcarbamoyl-N-lower alkylamino, εubstituted or unsubstituted N-containing hetεrccycliccarbonyl, carbamoyl, subεtituted or unεubstituted lower alkylcarbamoyl, substituted or unsubstituted N-containing heterocycliccarbonyl (lower)alkoxyimino, carbamoyl (lower)alkoxyimino or substituted or unsubstituted lower alkylcarbamoyl (lower)alkoxyimino; or lowεr alkεnyloxy subεtituted with εubεtituted or unεubstituted N-containing hetεrocycliccarbonyl, carbamoyl or substitutεd cr unsubεtituted lower alkylcarbamoyl; or 7) reacting a compound of the formula 0 or its rεactivε dεrivative at the carboxy group or a salt thereof with an amine or its salt to ^ provide a compound of the formula : or its salt, the above formulas, R 1 , R 2 , R 3 , P. , R 5 , A, E, X and Y are each as defined above, and R 4 is lower alkoxy, lower alkylthio, lower alkyl, or lower alkenyl each of which is substituted with substituted or unsubstituted N-containing heterocycliccarbonyl, carbamoyl, or subεtituted or unεubstituted lower alkylcarbamoyl; or 8) εubjecting a compound of the formula : or itε εalt to debenzylation reaction to provide a compound of the formula : or its salt, in the above formulas, R 1 , R 2 , R 3 , R 5 , A, E, X and Y are each as defined above, Rf is methoxy substituted with aryl or substituted aryl; or lowεr alkylthio which is substitutεd with mεthoxy substitutεd with aryl or substitutεd aryl; and R 4 is hydroxy; or lowεr alkylthio substitutεd with hydroxy; or 9) rεacting a compound of the formula or its salt with a compound of the formula : -.1 - 7 (VI) or its salt to provide a coapound of the formula or its salt, in the above formulas, R 1 , R 2 , R 3 , R 5 , A, E, X and Y are each as defined above, R 4 is hydroxy; R' is lower alkyl optionally substituted with hydroxy, aryl, subεtitutεd aryl, acyl, amino, lowεr alkylamino, acylamino, protected amino or a hetεrocyclic group; or N-protεctεd piperidyl; Z^ iε hydroxy; or acid reεidue; and R^ iε lower alkoxy substituted with hydroxy, aryl, substituted aryl, " acyl, amino, lower alkylamino, acylamino, protected amino or a hetεrocyclic group; or N-protεcted piperidyloxy; or 10) reacting a compound of the formula or its salt with an acylating agent to provide a compound of the formula : or its salt, in the above formulas, R J R , R , A, E, X and Y are each as dεfinεd abovε, R^ a is lowεr alkoxy substitutεd with amino; lowεr alkylthio subεtituted with amino; or lower alkyl substitutεd with amino; and R 4 is lowεr alkoxy subεtitutεd with acylamino or εubstituted acylamino; lower alkylthio substituted with acylamino or subεtituted acylamino; cr lower alkyl substituted with acylamino or subεtituted acylamino; or 11) reacting a coapound of the formula : or its salt with lower alkanal or N-protected amino(lower)alkanal in the presence of a reducing agent to provide a compound of the formula : or its salt, in the abovε formulas, R 1 , R 2 , R 3 , R 5 , A, E, X and Y arε each as defined above, R 4 ^ is amino; lower alkoxy substitutεd with amino; lowεr alkylthio subεtitutεd with amino; or lowεr alkyl substitutεd with amino; and R 4 is lowεr alkoxy substituted with lower alkylamino; lowεr alkylthio substituted with lower alkylamino; lower alkyl substituted with lower alkylamino; lower alkylamino; or N-protected amino(lower)alkylamino; or 12) subjecting a compound of thε formula : do) or its salt to rεduction to providε a compound of the formula : or itε εalt, in the above formulas, R 1 , R 2 , R 3 , R 5 , A, E, X and Y are each as definεd above, or 13) subjecting a compound of the formula or its salt to deacylation rεaction to providε a compound of thε formula : R or itε salt, in thε abovε formulas; R 1 , R 2 , R 3 , R 5 , A, E, X and Y arε εach as dεfinεd abovε, and R 4 . is acyloxy, or 14) rεacting a compound of thε formula : >r its salt with a compound of the formul. Z 2 its salt to providε compound of thε formula or its salt, in the above formulas, R 1 , R 2 , R 3 , R 4 , R 5 , X and Y are each as defined above, Z 2 is acid rεsiduε, and E j - is lower alkylene, or 15) reacting a compound of the formula : or its salt with an oxidizing agent to provide a compound of the formula : or its salt, in the above formulas, R 1 , R' R 3 , A, E, X and Y arε each as defined above R 4 is lower alkylthio substituted with amino or protεctεd amino; and R 4 is lowεr alkylsulfinyl substituted with amino or protectεd amino, or lowεr alkylsulfonyl subεtitutεd with amino or protεctεd amino; or 16) εubjεcting a compound of thε formula or itε εalt to catalytic rεduction to provide a compound of the formula : or itε εalt, in the above formulas, R 1 , R 2 , R 3 , R 4 , R D , A, E b , X and Y are each as defined above, and E c is lower alkenylεne, or 17) εubjεcting a compound of thε formula : or its salt to dεbenzylation reaction to provide a compound of the formula : or its salt, in the above formulas, R < R 3 , R' A, E, X and Y are each as defined above R < is aryl which is substituted with methoxy substitute with aryl or substitutεd aryl, R g l is aryl which is subεtitutεd with hydroxy, or reacting a compound of the formula or itε εalt with a compound of the formula Z 3 - R 8 (IX) or its salt to provide a compound of the formula 1795 - 298 - or its salt, in the above formulas, R*, R 22 ,, RR 33 ,, R 4 , R 5 , A, E, X and Y are each as defined above. Z 3 is hydroxy, or acid residue, R 8 is lower alkyl optionally subεtituted with acyl, acylamino, protected amino, aryl, εubεtituted aryl, acyl-substituted pyridyl, or N-protected guanidino; and Rf is aryl which is substituted with lower alkoxy optionally substituted with acyl, acylamino, protected amino, aryl, subεtituted aryl, acyl- substituted pyridyl or N-protectεd guanidino; or 19) subjεcting a compound of thε formula : or itε εalt to εlimination reaction of the hydroxy protectivε group to provide a compound of the formula or itε εalt, in the abovε formulaε, R 1 , R 2 , R 4 , R 5 , A, E, X and Y are each aε defined above, and Rr IS methoxy subεtituted with aryl; acyloxy; or εubstituted acyloxy; or 20) reacting a compound of the formula or its salt with a compound of the formula (X) or its salt to providε a compound of the formula or its salt, in the above formulas, R , R 2 , R 4 , R 5 , A, E, X and Y are each as defined abovε, Z 4 is acid residue, R 9 is lower alkyl optionally substituted with esterified carboxy, and Rj 3 is lower alkoxy optionally subεtituted with eεterified carboxy, or 21) subjecting a compound of the formula : or its salt to deesterification reaction to provide a compound of the formula : or its salt, in the above formulas, R 1 , R 2 , R 4 , R 5 , A , E, X, and Y are each as definεd abovε, R 3 is lowεr alkoxy subεtituted with esterifiεd carboxy, and R^ is lowεr alkoxy substitutεd with carboxy, or 22) rεacting a compound of thε formula (1-5) or its salt with an alkynε compound in thε presencε of a palladium compound, a coppεr compound to providε a compound of thε formula : or its salt, in thε abovε formulas, R 1 , R 2 , R 3 , R 5 , A, E, X and Y are each as definεd abovε, R 4 is halogen, and R 4 is lower alkynyl optionally subεtituted with hydroxy, amino, protεcted amino, lower alkylsulfonyloxy or arylsulfonyloxy, or /41795 - 302 - 23) rεacting a compound of the formula or its εalt with a compound of the formula -5_ R 10 (XI) to provide a compound of the formula R or its salt, in the above formulas, R 1 , R 2 , R 3 , R 5 , A, E, X and Y are each as defined above, R 4 is lower alkylthio, lower alkyl or lower alkynyl, each of which is subεtituted with hydroxy, Z 5 is halogen, R 10 is lower alkylsulfonyl or arylsulfonyl, and R 4 iε lower alkylthio, lower alkyl or lower alkynyl. /41795 - 303 - each of which iε substituted with lower alkylsulfonyloxy or arylsulfonyloxy, or 24 ) reacting a compound of the formula : or its salt with alkali mεtal phthalimide to provide a compound of the formula : or its salt, in the above formulas, R 1 , R 2 , R 3 , R 4 , R 5 , A, " E, X and Y are each as dεfined above, and R 4 is lower alkylthio, lower alkyl or lower alkynyl, each of which is subεtituted with phthalimido, or 25) reacting a compound of the formula : 1795 or itε εalt with a reducing agent to provide a compound of the formula : or itε εalt, in the above formulas, R 1 , R 2 , R 3 , R 4 , R 5 ' A, E, X and Y are each as definεd above, and R 4 . is lower alkyl optionally subεtituted with hydroxy, amino, protected amino, lower alkylεulfonyloxy or arylsulfonyloxy, or 26) reacting a compound of the formula : or its salt with a compound of thε formula or its salt to provide a compound of thε formula or its salt, in thε abovε formulas, R 1 , R 2 , R 3 , R 4 , R 5 , X and Y are each as definεd above, and E jj is a single bond or lower alkylene, or 27) reacting a compound of the formula : or its salt with a compound of the formula in the presencε of a basε to provide a compound of the formula : or its salt, in the above formulas, R 1 , R 3 , R 4 , R 5 , G, X and Y are each as definεd abovε, Z° is acid rεsiduε, and 6/41795 - 307 - R 2 is lower alkyl optionally substituted with aryl or acyl, or 28) reacting a compound of the formula or its salt with an acylating agent to provide a compound of the formula : or its salt, in the above formulas, R 2 , R" , R 4 , R , A, E, X and Y are each as defined above, R~ is aryl which is substituted with lower alkoxy substituted with aaino, and R^ is aryl which is substituted with lower alkoxy substituted with acylamino or substituted acylamino, or 29) reacting a compound of the formula or its εalt with a reducing agent to provide a compound of the formula : or itε salt, in the above formulaε, . R 2 , R 3 , R 4 , R- A, E, X and Y are each aε definεd abovε R]; iε aryl which iε εubstitutεd with lowεr alkoxy substitutεd with oxopiperidylcarbonyl, and R- is aryl which is substituted with lower alkoxy εubεtituted with hydroxypiperidylcarbonyl, or 30) reacting a compound of the formula : or its salt with an amine compound or its salt in the prεεence of a reducing agent to provide a compound of the formula : or its salt, in the above formulas, R 2 , R 3 , R 4 , R , A, E, X and Y are each as definεd above, R^ is aryl which is subεtituted with lowεr alkoxy εubεtitutεd with formyl or oxopiperidylcarbonyl. and R is aryl which is subεtituted with lower alkoxy substituted with aminopipεridylcarbonyl or N-lowe. 1 alkylpiperazinyl, or 31) reacting a compound of the formula : (1-19) or its reactive derivative at the carboxy group or a salt therεof with lower alkylamino(lower)alkanol to provide a compound of the formula : 0 or its salt, in the above formulas, R 2 , R 3 , R 4 , R 5 , A, E, X and Y are each as defined above R^ is aryl which is substituted with lower alkoxy substituted with carboxy, and R^ is aryl which is subεtituted with lower alkoxy ^ substituted with lower 6/41795 - 311 - alkylamino(lower)alkoxycarbonyl, or 32) reacting a compound of the formula : or its salt with a reducing agent to provide a compound of thε formula : or its salt, in the above formulas. R 2 , R 3 , R 4 , v / " / E, X ' and Y are each as definεd above. R Q is aryl which is subεtituted with lower alkoxy εubεtituted with eεterifiεd carboxy, and R1 iε aryl which iε εubstituted with lower alkoxy substituted with hydroxy, or 33) subjecting a compound of the formula 1 95 - 312 - or its salt to oxidation reaction to provide a compound of the formula : or its salt, in the above formulas, H 1 , R K 22 ,, RR 33 ,, RR 44 ,, R 5 , A, E, X and Y are each as defined above, and R q is aryl which is substituted with lower alkoxy substituted with formyl, or 34) reacting a compound of the formula or itε salt with an azidε compound to providε a compound of thε formula : or its salt, in thε abovε formulaε, R 2 , R 3 , R 4 , R 5 , A, E, X and Y arε εach aε defined above, R iε aryl which is subεtituted with lowεr alkoxy substitutεd with cyano-subεtitutεd aryl, and R g iε aryl which iε εubεtituted with lower alkoxy εubεtituted with tetrazolyl-substituted aryl, or 35) rεacting a compound of thε formula : or its salt with an isourea compound to provide a compound of the formula : or its salt, in the above formulas, R 1 , R 2 , R 3 , R 5 , A, E, X and Y are each as definεd abovε, R 4 is lower alkoxy substituted with amino, and R 4 is lower alkoxy substituted with guanidino, or 36) subjecting a compound of thε formula : or its εalt to εlimination rεaction of thε N-protεctivε group to providε a compound of the formula : or itε salt, in the abovε formulaε, R 2 , R 3 , R 4 , R 5 , A, E, X and Y arε each aε defined above, R iε aryl which iε εubεtituted with lower alkoxy substituted with protεctεd amino, N-protected amino(lower)alkanoylamino, N-protected piperazinylcarbonyl or N-protected guanidino; and R is aryl which is substituted with lower alkoxy substitutεd with amino, amino(lower)alkanoylamino, piperazinylcarbonyl or guanidino; or 37) rεacting a compound of thε formula or its salt with N-lower alkylpiperazinε, dimethylaminopiperidine, ammonia or N,N- dimεthylformamidε to providε a compound of thε formula or itε εalt, in the above formulaε, R 2 , R 3 , R 4 , R 5 , A, E, X and Y are each as defined above, R^. is aryl which is substituted with lower alkoxy substituted with phenoxycarbonylamino, and R^ is aryl which is substituted with lower alkoxy subεtitutεd with N-lowεr alkylpipεrazinylcarbonylamino, dimεthylaminopipεridylcarbonylamino, carbamoylamin or dimεthylcarbamoylamino, or 38) reacting a compound of the formula : or itε reactive derivativε at thε carboxy group or a εalt thεreof with a hydroxy compound or a diazo compound to provide a compound of the formula : or itε εalt, in the above formulaε, R 1 , Rj 2 , R_3 3 , R_4 4 , R_5 5 , A, E, X and Y are each aε definεd abovε, or 39) reacting a compound of the formula or itε reactive derivativε at thε carboxy group or a εalt thereof with an amine to provide a compound of the formula : or itε salt, in the above formulas, R>1 A , o RR 2 2, R_3, R_4 *1 , RD J -, A, E, X and Y are each as defined above, and R g is lower alkoxy which is subεtituted with carbamoyl optionally εubεtituted with lower alkyl. A pharmaceutical compoεition compriεing a compound of claim 1, aε an active ingrediεnt, in association with a pharmacεutically accεptablε, subεtantially non- toxic carrier or excipient. A compound of claim 1 for uεe aε a medicament. 8. A method of therapεutic treatment and/or prevention of hypertension, heart failurε, rεnal insufficiεncy, εdεma, aεcitεs, vasoprεεεin paraεεcrεtion εyndrome, hepatocirrhoεiε, hyponatrεmia, hypokalεmia, diabεtic, circulation disorder, cerεbrovascular disease, Meniere's syndrome or motion εickneεs which compriseε administering an effective amount of a compound of claim 1 to human beings or animals. 9. Use of a compound of claim 1 for the manufacture of a medicament for treating and/or preventing hypertension, heart failurε, rεnal insufficiεncy, εdεma, ascites, vasopressin parasεcrεtion εyndromε, hεpatocirrhoεiε, hyponatrεmia, hypokalεmia, diabetic, circulation diεorder, cerebrovaεcular diεeaεe, Mεniεre'ε εyndrome or motion εickness in human bεingε or animalε.

Inventors: OHKAWA TAKEHIKO, SATO KENTARO, SAWADA HITOSHI, SETOI HIROYUKI, TANAKA HIROKAZU, ZENKOH TATSUYA, OHKAWA, TAKEHIKO, SATO, KENTARO, SAWADA, HITOSHI, SETOI, HIROYUKI, TANAKA, HIROKAZU, ZENKOH, TATSUYA
Applicants: FUJISAWA PHARMACEUTICAL CO, OHKAWA TAKEHIKO, SATO KENTARO, SAWADA HITOSHI, SETOI HIROYUKI, TANAKA HIROKAZU, ZENKOH TATSUYA, FUJISAWA PHARMACEUTICAL CO., LTD., OHKAWA, TAKEHIKO, SATO, KENTARO, SAWADA, HITOSHI, SETOI, HIROYUKI, TANAKA, HIROKAZU, ZENKOH, TATSUYA
Application year: 1996
Main classification: C07C237
IPC codes: A61K31, A61P1, A61P3, A61P9, A61P13, A61P15, A61P27, A61P43, C07C235, C07C237, C07C243, C07C255, C07C271, C07C279, C07D209, C07D211, C07D213, C07D239, C07D243, C07D295, C07D401