Patent ID: 6118017
Filing Date: 2000-09-12
Classification: A61P,C07C

Abstract:
A compound of Formula (I): ##STR6## wherein: R.sub.1 is --(CR.sub.4 R.sub.5).sub.n C(O)O(CR.sub.4 R.sub.5).sub.m R.sub.6, --(CR.sub.4 R.sub.5).sub.n C(O)NR.sub.4 (CR.sub.4 R.sub.5).sub.m R.sub.6, --(CR.sub.4 R.sub.5).sub.n O(CR.sub.4 R.sub.5).sub.m R.sub.6, or --(CR.sub.4 R.sub.5).sub.r R.sub.6 wherein the alkyl moieties may be unsubstituted or substituted with one or more fluorines;m is 0 to 2;n is 1 to 4;r is 0 to 6;R.sub.4 and R.sub.5 are independently hydrogen or C.sub.1-2 alkyl;R.sub.6 is hydrogen, methyl, hydroxyl, aryl, halo substituted aryl, aryloxy C.sub.1-3 alkyl, halo substituted aryloxy C.sub.1-3 alkyl, indanyl, indenyl, C.sub.7-11 polycycloalkyl C.sub.3-6 cycloalkyl, or a C.sub.4-6 cycloalkyl containing one or two unsaturated bonds, wherein the cycloalkyl or heterocyclic moiety may be unsubstituted or substituted by 1 to 3 methyl groups, one ethyl group or an hydroxyl group;provided that:a) when R.sub.6 is hydroxyl, then m is 2; orb) when R.sub.6 is hydroxyl, then r is 2 to 6; orc) when R.sub.6 is 2-tetrahydropyranyl, 2-tetrahydrothiopyranyl, 2-tetrahydrofuranyl, or 2-tetrahydrothienyl, then m is 1 or 2; ord) when R.sub.6 is 2-tetrahydropyranyl, 2-tetrahydrothiopyranyl, 2-tetrahydrofuranyl, or 2-tetrahydrothienyl, then r is 1 to 6;e) when n is 1 and m is 0, then R.sub.6 is other than H in --(CR.sub.4 R.sub.5).sub.n O(CR.sub.4 R.sub.5).sub.m R.sub.6 ;X is VR.sub.2, halogen, nitro, NR.sub.4 R.sub.5, or formyl amine;V is O or S(O).sub.m' ;m' is 0, 1, or 2;X.sub.2 is O or NR.sub.8 ;R.sub.2 is --CH.sub.3 or --CH.sub.2 CH.sub.3 unsubstituted or substituted by 1 or more fluorines;R.sub.3 is halogen, C.sub.1-4 alkyl, halo-substituted C.sub.1-4 alkyl, CH.sub.2 NHC(O)C(O)NH.sub.2, --CH.dbd.CR.sub.8' R.sub.8', cyclopropyl optionally substituted by R.sub.8', CN, OR.sub.8, CH.sub.2 OR.sub.8, NR.sub.8 R.sub.10, CH.sub.2 NR.sub.8 R.sub.10, C(Z)H, C(O)OR.sub.8, C(O)NR.sub.8 R.sub.10, or C.tbd.CR.sub.8 ;Z is O, NR.sub.9, NOR.sub.8, NCN, C(--CN).sub.2, CR.sub.8 CN, CR.sub.8 NO.sub.2, CR.sub.8 C(O)OR.sub.8, CR.sub.8 C(O)NR.sub.8 R.sub.8, C(--CN)NO.sub.2, C(--CN)C(O)OR.sub.9, C(--CN)C(O)NR.sub.8 R.sub.8 ;A is O, NR.sub.7, NCR.sub.4 R.sub.5 C.sub.2-6 alkenyl, NOR.sub.14, NOR.sub.15, NOCR.sub.4 R.sub.5 C.sub.2-6 alkenyl, NNR.sub.4 R.sub.14, NNR.sub.4 R.sub.15, NCN, NNR.sub.8 C(O)NR.sub.8 R.sub.14, NNR.sub.8 C(S)NR.sub.8 R.sub.14 ;R.sub.7 is --(CR.sub.4 R.sub.5).sub.q R.sub.12 or C.sub.1-6 alkyl wherein the R.sub.12 or C.sub.1-6 alkyl group is unsubstituted or substituted one or more times by methyl or ethyl unsubstituted or substituted by 1-3 fluorines, --F, --Br, --Cl, --NO.sub.2, --NR.sub.10 R.sub.11, --C(O)R.sub.8, --CO.sub.2 R.sub.8, --O(CH.sub.2).sub.q R.sub.8, --CN, --C(O)NR.sub.10 R.sub.11, --O(CH.sub.2).sub.q C(O)NR.sub.10 R.sub.11, --O(CH.sub.2).sub.q C(O)R.sub.8, --NR.sub.10 C(O)NR.sub.10 R.sub.11, --NR.sub.10 C(O)R.sub.11, --NR.sub.10 C(O)OR.sub.9, --NR.sub.10 C(O)R.sub.13, --C(NR.sub.10)NR.sub.10 R.sub.11, --C(NCN)NR.sub.10 R.sub.11, --C(NCN)SR.sub.9, --NR.sub.10 C(NCN)SR.sub.9, --NR.sub.10 C(NCN)NR.sub.10 R.sub.11, NR.sub.10 S(O).sub.2 R.sub.9, --S(O).sub.m' R.sub.9, --NR.sub.10 C(O)C(O)NR.sub.10 R.sub.11, --NR.sub.10 C(O)C(O)R.sub.10, or R.sub.13 ;q is 0, 1, or 2;R.sub.12 is R.sub.13, C.sub.3 -C.sub.7 cycloalkyl, (2-, 3- or 4-pyridyl), pyrimidyl, pyrazolyl, (1- or 2-imidazolyl), pyrrolyl, piperazinyl, piperidinyl, morpholinyl, furanyl, (2- or 3-thienyl), quinolinyl, naphthyl, or phenyl;R.sub.8 is hydrogen or R.sub.9 ;R.sub.8' is R.sub.8 or fluorine;R.sub.9 is C.sub.1-4 alkyl unsubstituted or substituted by one to three fluorines;R.sub.10 is OR.sub.8 or R.sub.11 ;R.sub.11 is hydrogen, or C.sub.1-4 alkyl unsubstituted or substituted by one to three fluorines; or when R.sub.10 and R.sub.11 are as NR.sub.10 R.sub.11 they may together with the nitrogen form a 5 to 7 membered ring comprised only of carbon atoms or carbon atoms and at least one heteroatom selected from O, N, or S;R.sub.13 is oxazolidinyl, oxazolyl, thiazolyl, pyrazolyl, triazolyl, tetrazolyl, imidazolyl, imidazolidinyl, thiazolidinyl, isoxazolyl, oxadiazolyl, or thiadiazolyl, and each of these heterocyclic rings is connected through a carbon atom and each may be unsubstituted or substituted by one or two C.sub.1-2 alkyl groups;R.sub.14 is hydrogen or R.sub.7 ; or when R.sub.8 and R.sub.14 are as NR.sub.8 R.sub.14 they may together with the nitrogen form a 5 to 7 membered ring comprised only of carbon atoms or carbon atoms and at least one heteroatom selected from O, N, or S; provided that:R.sub.15 is C(O)R.sub.14, C(O)NR.sub.4 R.sub.14, S(O).sub.2 R.sub.7, or S(O).sub.2 NR.sub.4 R.sub.14 ;or a pharmaceutically acceptable salt thereof.