Patent ID: 6156745
Filing Date: 2000-12-05
Classification: A61P,C07D

Abstract:
A compound of formula (I): ##STR3## wherein R.sup.1 and R.sup.2 are each independently hydrogen, (C.sub.1 -C.sub.10)alkyl, (C.sub.3 -C.sub.8)cycloalkyl, (C.sub.2 -C.sub.10)alkenyl, (C.sub.2 -C.sub.10)alkynyl, --COOR.sub.a, --CONR.sub.b R.sub.c, cyano, --C(.dbd.O)R.sub.d, --OR.sub.e, aryl, heteroaryl, oxazolidinyl, isoxazolidinyl, morpholinyl, --S(O).sub.m R.sub.f, --NR.sub.g R.sub.h, azido, or halo;R.sup.3 is (C.sub.3 -C.sub.10)alkyl, (C.sub.2 -C.sub.10)alkenyl, (C.sub.2 -C.sub.10)alkynyl, (C.sub.1 -C.sub.10)alkanoyl, (C.sub.3 -C.sub.8)cycloalkyl, aryl, heteroaryl, aryl(C.sub.1 -C.sub.10)alkyl, heteroaryl(C.sub.1 -C.sub.10)alkyl, or --CH.sub.2 R.sub.i, wherein R.sub.i is halo, cyano, cyanato, --OR.sub.j, --NR.sub.k R.sub.l, azido, --SR.sub.m, or (C.sub.3 -C.sub.8)cycloalkyl;R.sup.4 is hydrogen, (C.sub.1 -C.sub.10)alkyl, (C.sub.3 -C.sub.8)cycloalkyl, (C.sub.2 -C.sub.10)alkenyl, (C.sub.2 -C.sub.10)alkynyl, aryl, or heteroaryl;m and n are each independently 0, 1, or 2;each R.sub.a -R.sub.f is independently hydrogen, (C.sub.1 -C.sub.10)alkyl, (C.sub.3 -C.sub.8)cycloalkyl, (C.sub.2 -C.sub.10)alkenyl, (C.sub.2 -C.sub.10)alkynyl, aryl, heteroaryl, oxazolidinyl, isoxazolidinyl, or morpholinyl;each R.sub.g or R.sub.h is independently hydrogen, (C.sub.1 -C.sub.10)alkyl, (C.sub.3 -C.sub.8)cycloalkyl, (C.sub.2 -C.sub.10)alkenyl, (C.sub.2 -C.sub.10)alkynyl, (C.sub.1 -C.sub.10)alkanoyl, aryl, benzyl, phenethyl, heteroaryl oxazolidinyl, isoxazolidinyl, or morpholinyl; or R.sub.g and R.sub.h together with the nitrogen to which they are attached are triazolyl, imidazolyl, oxazolidinyl, isoxazolidinyl, pyrrolyl, morpholino, piperidino, pyrrolidino, pyrazolyl, indolyl, or tetrazolyl;R.sub.j is hydrogen, (C.sub.1 -C.sub.10)alkyl, (C.sub.3 -C.sub.8)cycloalkyl, (C.sub.2 -C.sub.10)alkenyl, (C.sub.2 -C.sub.10)alkynyl, --C(.dbd.O)N(RP).sub.2, aryl, heteroaryl, arylcarbonyl, heteroarylcarbonyl, or (C.sub.1 -C.sub.10)alkanoyl, wherein each R.sub.p is independently hydrogen, (C.sub.1 -C.sub.10)alkyl, aryl, benzyl, phenethyl, or heteroaryl;each R.sub.k or R.sub.l is independently hydrogen, (C.sub.1 -C.sub.10)alkyl, (C.sub.3 -C.sub.8)cycloalkyl, (C.sub.2 -C.sub.10)alkenyl, (C.sub.2 -C.sub.10)alkynyl, (C.sub.1 -C.sub.10)alkanoyl, --C(.dbd.O)N(R.sub.q).sub.2, aryl, benzyl, phenethyl, heteroaryl oxazolidinyl, isoxazolidinyl, or morpholinyl, wherein each R.sub.q is independently hydrogen, (C.sub.1 -C.sub.10)alkyl, aryl, benzyl, phenethyl, or heteroaryl; or R.sub.k and R.sub.l together with the nitrogen to which they are attached are triazolyl, imidazolyl, oxazolidinyl, isoxazolidinyl, pyrrolyl, morpholino, piperidino, pyrrolidino, pyrazolyl, indolyl, or tetrazolyl; andR.sub.m is hydrogen, (C.sub.1 -C.sub.10)alkyl, (C.sub.3 -C.sub.8)cycloalkyl, (C.sub.2 -C.sub.10)alkenyl, (C.sub.2 -C.sub.10)alkynyl, cyano, aryl, benzyl, phenethyl, heteroaryl, oxazolidinyl, isoxazolidinyl, or morpholinyl;wherein any (C.sub.1 -C.sub.10)alkyl, (C.sub.3 -C.sub.8)cycloalkyl, (C.sub.2 -C.sub.10)alkenyl, (C.sub.2 -C.sub.10)alkynyl, (C.sub.1 -C.sub.10)alkanoyl, aryl, benzyl, phenethyl, heteroaryl, arylcarbonyl, heteroarylcarbonyl, oxazolidinyl, isoxazolidinyl, or morpholinyl of R.sup.1 -R.sup.4, R.sub.a -R.sub.m, or R.sub.p -R.sub.q, may optionally be substituted with 1, 2, or 3 Z; and each Z is independently halo, nitro, cyano, hydroxy, (C.sub.1 -C.sub.10)alkyl, (C.sub.3 -C.sub.8)cycloalkyl, (C.sub.1 -C.sub.10)alkoxy, (C.sub.1 -C.sub.10)alkanoyl, (C.sub.2 -C.sub.10)alkanoyloxy, trifluoromethyl, aryl, aryloxy, heteroaryl, or --SR.sub.n, wherein R.sub.n is hydrogen, (C.sub.1 -C.sub.10)alkyl, (C.sub.3 -C.sub.8)cycloalkyl, aryl, benzyl, phenethyl, or heteroaryl;and further wherein any aryl, aryloxy, heteroaryl, benzyl, or phenethyl of Z may optionally be substituted with 1, 2, or 3 substituents selected from the group consisting of halo, nitro, cyano, hydroxy, (C.sub.1 -C.sub.10)alkyl, (C.sub.3 -C.sub.8)cycloalkyl, (C.sub.1 -C.sub.10)alkoxy, (C.sub.1 -C.sub.10)alkanoyl, (C.sub.2 -C.sub.10)alkanoyloxy, benzyloxy, 4-methoxybenzyloxy, and trifluoromethyl;or a pharmaceutically acceptable salt thereof.