Patent ID: 6096762
Filing Date: 2000-08-01
Classification: A61P,C07D

Abstract:
A compound having the formula (I): ##STR20## and pharmaceutically acceptable salts thereof: wherein W is CH.sub.2, O, NH, or N--(C.sub.1 -C.sub.4)-alkyl;wherein J is hydrogen, (C.sub.1 -C.sub.4)-alkyl or benzyl;wherein K is (C.sub.1 -C.sub.4)-straight or branched alkyl, benzyl or cyclohexylmethyl, or wherein J and K may be taken together to form a 5-7 membered heterocyclic ring which may contain a heteroatom selected from the group consisting of O, S, SO, and SO.sub.2 ;wherein the stereochemistry at carbon position 1 is R or S;wherein Z is Q or --(CH.sub.2).sub.m --C(H)Q'A;wherein m is 0-3;wherein Q is hydrogen, CHL-Ar, (C.sub.1 -C.sub.6)-straight or branched alkyl, (C.sub.2 -C.sub.6)-straight or branched alkenyl, (C.sub.5 -C.sub.7)-cycloalkyl, (C.sub.5 -C.sub.7)-cycloalkenyl, Ar substituted (C.sub.1 -C.sub.6)-alkyl, (C.sub.2 -C.sub.6)-alkenyl or ##STR21## wherein L and G are independently hydrogen, (C.sub.1 -C.sub.6)-straight or branched alkyl, (C.sub.2 -C.sub.6)-straight or branched alkenyl;wherein T is Ar or substituted cyclohexyl with substituents at positions 3 and 4 which are independently selected from the group consisting of hydrogen, hydroxyl, O--(C.sub.1 -C.sub.4)-alkyl or O--(C.sub.2 -C.sub.4)-alkenyl and carbonyl;wherein D is (C.sub.1 -C.sub.6)-straight or branched alkyl, (C.sub.2 -C.sub.6)-straight or branched alkenyl, (C.sub.5 -C.sub.7)-cycloalkyl or (C.sub.5 -C.sub.7)-cycloalkenyl substituted with (C.sub.1 -C.sub.4)-straight or branched alkyl or (C.sub.2 -C.sub.4)-straight or branched alkenyl, O--(C.sub.1 -C.sub.4)-straight or branched alkyl, O--(C.sub.2 -C.sub.4)-straight or branched alkenyl, [(C.sub.1 -C.sub.4)-alkyl or (C.sub.2 -C.sub.4)-alkenyl]-Ar or Ar;wherein Ar is a carbocyclic aromatic group selected from the group consisiting of phenyl, 1-naphthyl, 2-naphthyl, indenyl, azulenyl, fluorenyl, and anthracenyl;wherein Ar may contain one to three substituents which are independently selected from the group consisting of hydrogen, halogen, hydroxyl, hydroxymethyl, nitro, trifluoromethyl, trifluoromethoxy, (C.sub.1 -C.sub.6)-straight or branched alkyl, (C.sub.2 -C.sub.6)-straight or branched alkenyl, O--[(C.sub.1 -C.sub.4)-straight or branched alkyl], O-benzyl, O-phenyl, 1,2-methylenedioxy, amino, carboxyl, N-[(C.sub.1 -C.sub.5)-straight or branched alkyl or (C.sub.2 -C.sub.5)-straight or branched alkenyl] carboxamides, N,N-di-[(C.sub.1 -C.sub.5)-straight or branched alkyl or (C.sub.2 -C.sub.5)-straight or branched alkenyl] carboxamides, N-benzylcarboxamide, O--X, CH.sub.2 --(CH.sub.2).sub.p --X, O--(CH.sub.2).sub.p --X, (CH.sub.2).sub.p --O--X, and CH.dbd.CH--X;wherein X is 4-methoxyphenyl;wherein p is 0-2;wherein Q' and A are independently hydrogen, Ar, (C.sub.1 -C.sub.10)-straight or branched alkyl, (C.sub.2 -C.sub.10)-straight or branched alkenyl or alkynyl, (C.sub.5 -C.sub.7)cycloalkyl substituted-straight (C.sub.1 -C.sub.6)-straight or branched alkyl, (C.sub.2 -C.sub.6)-straight or branched alkenyl or alkynyl, (C.sub.5 -C.sub.7)-cycloalkenyl substituted (C.sub.1 -C.sub.6)-straight or branched alkyl, (C.sub.2 -C.sub.6)-straight or branched alkenyl or alkynyl, or Ar substituted (C.sub.1 -C.sub.6)-straight or branched alkyl, (C.sub.2 -C.sub.6)-straight or branched alkenyl or alkynyl wherein, in each case, any one of the CH.sub.2 groups of said alkyl, alkenyl or alkynyl chains may be optionally replaced by a heteroatom selected from the group consisting of O, S, SO, SO.sub.2 and NR, wherein R is selected from the group consisting of hydrogen, (C.sub.1 -C.sub.4)-straight or branched alkyl, (C.sub.2 -C.sub.4)-straight or branched alkenyl or alkynyl, and (C.sub.1 -C.sub.4)-bridging alkyl wherein a bridge is formed between the nitrogen and a carbon atom of said heteroatom-containing chain to form a ring, and wherein said ring is optionally fused to an Ar group; or ##STR22## wherein G' is hydrogen, (C.sub.1 -C.sub.6)-straight or branched alkyl or (C.sub.2 -C.sub.6)-straight or branched alkenyl or alkynyl.