Patent ID: 6057345
Filing Date: 2000-05-02
Classification: A61P,C07C,C07D

Abstract:
A compound according to formula (I); ##STR54## wherein: A is phenyl optionally substituted with L, where L is a moiety selected from halo, trifluoromethyl, nitro, hydroxy, amino, (C.sub.1 -C.sub.4)alkylamino, di(C.sub.1 -C.sub.4)alkylamino, cyano, (C.sub.1 -C.sub.6)alkoxy, --S(O).sub.p (C.sub.1 -C.sub.6)alkyl where p is 0, 1 or 2, (C.sub.1 -C.sub.6)alkyl optionally substituted with a group selected from hydroxy, amino, halo, nitro and cyano, --S(O).sub.p CF.sub.3, carbamoyl, (C.sub.1 -C.sub.4)alkylcarbamoyl, di(C.sub.1 -C.sub.4)alkylcarbamoyl, (C.sub.2 -C.sub.6)alkenyl, (C.sub.2 -C.sub.6)alkynyl, (C.sub.2 -C.sub.4)alkenylamino, N--(C.sub.2 -C.sub.4)alkenyl-N-(C.sub.1 -C.sub.4)alkylamino, di--(C.sub.2 -C.sub.4)alkenylamino, S(O).sub.p (C.sub.2 -C.sub.6)alkenyl, (C.sub.2 -C.sub.4)alkenylcarbamoyl, di(C.sub.2 -C.sub.4)alkenylcarbamoyl, (C.sub.3 -C.sub.7)cycloalkyl, (C.sub.3 -C.sub.7)cycloalkyl(C.sub.1 -C.sub.3)alkyl, (C.sub.3 -C.sub.7)cycloalkyl(C.sub.2 -C.sub.3)alkenyl, (C.sub.5 -C.sub.7)cycloalkenyl, C.sub.7)cycloalkenyl(C.sub.1 -C.sub.3)alkyl, (C.sub.5 -C.sub.7)cycloalkenyl(C.sub.2 -C.sub.3)alkenyl, (C.sub.5 -C.sub.7)cycloalkenyl,(C.sub.2 -C.sub.3)alkynyl, (C.sub.1 C.sub.4)alkoxycarbonylamino, (C.sub.1 -C.sub.4)alkanoylamino, (C.sub.1 -C.sub.4)alkanoyl(N--(C.sub.1 -C.sub.4)alkyl)amino, (C.sub.1 -C.sub.4)alkanesulphonamido, benzenesulphonamido, aminosulphonyl, (C.sub.1 -C.sub.4)alkylaminosulphonyl, di(C.sub.1 -C.sub.4)alkylaminosulphonyl, (C.sub.1 -C.sub.4)alkoxycarbonyl, (C.sub.1 -C.sub.4)alkanoyloxy, (C.sub.1 -C.sub.6)alkanoyl, formyl(C.sub.1 -C.sub.4)alkyl, trifluoro(C.sub.1 -C.sub.3)alkylsulphonyl, hydroxyimino(C.sub.1 -C.sub.6)alkyl, (C.sub.1 -C.sub.4)alkoxyimino(C.sub.1 -C.sub.6)alkyl, (C.sub.1 -C.sub.6)alkylcarbamoylamino, oxazolyl, pyridyl, thiazolyl, pyrimidyl, pyrazinyl and pyridazinyl;B is phenylD is phenyl optionally substituted with L;the --Z--B--R.sup.1 and --X--D groups are positioned in a 1-2 relationship to one another on phenyl-ring A;the phenyl-ring A atom positioned ortho to the --X--linking group, in the 3-position relative to the --Z--linking group, is not substituted;R.sup.1 is positioned on the phenyl-ring B in a 1-3 or 1-4 relationship with the --Z--linking group;R.sup.1 is selected from a group of the formula --CONR.sup.a R.sup.a1 wherein R.sup.a is hydrogen, (C.sub.1 -C.sub.6)alkyl, (C.sub.3 -C.sub.7)cycloalkyl, (C.sub.3 -C.sub.7)cycloalkyl(C.sub.1 -C.sub.3)alkyl, (C.sub.5 -C.sub.7)cycloalkenyl or (C.sub.5 -C.sub.7)cycloalkenyl(C.sub.1 -C.sub.3)alkyl, and R.sup.a1 is hydrogen, hydroxy or optionally-substituted: (C.sub.1 -C.sub.10)alkyl, (C.sub.2 -C.sub.10)alkenyl, (C.sub.2 -C.sub.10)alkynyl, (C.sub.3 -C.sub.7)cycloalkyl, (C.sub.3 -C.sub.7)cycloalkyl(C.sub.1 -C.sub.6)alkyl, (C.sub.3 -C.sub.7)cycloalkyl(C.sub.2 -C.sub.6)alkenyl, (C.sub.3 -C.sub.7)cycloalkyl(C.sub.2 -C.sub.6)alkynyl, (C.sub.5 -C.sub.7)cycloalkenyl, (C.sub.3 -C.sub.7)cycloalkenyl(C.sub.1 -C.sub.6)alkyl, (C.sub.5 -C.sub.7)cycloalkenyl(C.sub.2 -C.sub.6)alkenyl, (C.sub.5 -C.sub.7)cycloalkenyl(C.sub.2 -C.sub.6)alkynyl, 5-or 6-membered heteroaryl, 5- or 6-membered heteroaryl(C.sub.1 -C.sub.6)alkyl, 5- or 6-membered saturated or partially-saturated heterocyclyl, or 5- or 6-membered saturated or partially-saturated heterocyclyl(C.sub.1 -C.sub.6)alkyl; or wherein R.sup.a and R.sup.a1 together with the amide nitrogen to which they are attached form an amino acid residue or ester thereof;X is selected from --OCH.sub.2 --, --SCH.sub.2 --, --CH.sub.2 CH.sub.2 --, CH.sub.2 --, --O--, --S-- and --N(R.sup.4)CH.sub.2 --, wherein the left hand atom in each formula is attached to A;Z is selected from groups of the formulae --CH(R.sup.3)CH(R.sup.3)N(R.sup.2)--, --N(R.sup.2)CH(R.sup.3)--, --CH(R .sup.3)P.sup.1 -- where P.sup.1 is oxygen or sulphur, --(CH(R.sup.3)).sub.m -- where m is 2 or 3, and --CH(R.sup.3)N(R.sup.2)--, with the proviso that when Z is --CH(R.sup.3)N(R.sup.2)-- or --(CH(R.sup.3)).sub.m --, X is not --OCH.sub.2 --;R.sup.2 is selected from hydrogen, (C.sub.2 -C.sub.6)alkenyl, (C.sub.2 -C.sub.6)alkynyl, (C.sub.3 -C.sub.6)cycloalkyl, (C.sub.3 -C.sub.6)cycloalkyl(C.sub.1 -C.sub.3)alkyl, (C.sub.3 -C.sub.6)cycloalkyl(C.sub.2 -C.sub.3 )alkenyl, (C5-C.sub.6)cycloalkenyl, (C.sub.5 -C.sub.6)cycloalkenyl(C.sub.1 -C.sub.3)alkyl, (C.sub.5 -C.sub.6)cycloalkenyl(C.sub.2 -C.sub.3)alkenyl, phenyl, phenyl(C.sub.1 -C.sub.3)alkyl, 5- or 6-membered heteroaryl(C.sub.1 -C.sub.3)alkyl and (C.sub.1 -C.sub.6)alkyl optionally substituted by hydroxy, cyano, nitro, amino, halo, (C.sub.1 -C.sub.4)alkanoyl, (C.sub.1 -C.sub.4)alkoxy or trifluoromethyl;R.sup.3 is hydrogen or (C.sub.1 -C.sub.4)alkyl;R.sup.4 is hydrogen or (C.sub.1 -C.sub.4)alkyl; andN-oxides of --NR.sup.2, where chemically possible;S-oxides of sulphur-containing rings where chemically possible;or pharmaceutically-acceptable salts or in vivo-hydrolysable esters or amides thereof.