Patent ID: 6294671
Filing Date: 2001-09-25
Classification: A61P,C07D

Abstract:
A compound of formula (I): ##STR9##or a stereoisomer or pharmaceutically acceptable salt form thereof, wherein:R is phenyl, and is substituted with 2-5 R.sup.3 groups;R.sup.1 is selected from H, C.sub.1-4 alkyl, C.sub.2-4 alkenyl, C.sub.2-4 alkynyl, halo, --CN, C.sub.1-4 haloalkyl, NR.sup.6 R.sup.7, NR.sup.8 COR.sup.9, --OR.sup.10, SH and --S(O).sub.n R.sup.11 ;R.sup.2 is NR.sup.6a R.sup.7a ;R.sup.3 is independently selected at each occurrence from C.sub.1-10 alkyl substituted with 0-2 R.sup.a, C.sub.2-10 alkenyl substituted with 0-2 R.sup.a, C.sub.2-10 alkynyl substituted with 0-2 R.sup.a, C.sub.3-6 cycloalkyl substituted with 0-2 R.sup.a, (C.sub.3-6 cycloalkyl)C.sub.1-4 alkyl substituted with 0-2 R.sup.a, --NO.sub.2, halo, --CN, C.sub.1-4 haloalkyl, --NR.sup.6 R.sup.7, NR.sup.8 COR.sup.13a, --NR.sup.8 C(O)OR.sup.13a, --COR.sup.13, --OR.sup.10a, --CONR.sup.6 R.sup.7, --NR.sup.8 CONR.sup.6 R.sup.7, --C(O)OR.sup.10a, SH, and --S(O).sub.n R.sup.12 ;R.sup.a is independently selected at each occurrence from C.sub.1-4 alkyl, --NO.sub.2, halo, --CN, --NR.sup.6 R.sup.7, --NR.sup.8 COR.sup.13a, --NR.sup.8 C(O)OR.sup.13a, --COR.sup.13, --OR.sup.10a, --CONR.sup.6 R.sup.7, --NR.sup.8 CONR.sup.6 R.sup.7, --C(O)OR.sup.10a, SH, and --S(O).sub.n R.sup.12 ;R.sup.6 is independently at each occurrence selected from H, C.sub.1-4 alkyl, C.sub.3-6 cycloalkyl and (C.sub.3-6 cycloalkyl)methyl;R.sup.6a is independently selected at each occurrence from H, C.sub.1-6 alkyl substituted with 0-2 R.sup.b, C.sub.2-6 alkenyl substituted with 0-2 R.sup.b, C.sub.2-6 alkynyl substituted with 0-2 R.sup.b, C.sub.1-4 haloalkyl, C.sub.3-6 cycloalkyl substituted with 0-2 R.sup.b, (C.sub.3-6 cycloalkyl)C.sub.1-4 alkyl substituted with 0-2 R.sup.b, aryl substituted with 0-2 R.sup.b, (aryl)C.sub.1-4 alkyl substituted with 0-2 R.sup.b, heteroaryl substituted with 0-2 R.sup.b, (heteroaryl)C.sub.1-4 alkyl substituted with 0-2 R.sup.b, heterocyclyl substituted with 0-2 R.sup.b, and (heterocyclyl)C.sub.1-4 alkyl substituted with 0-2 R.sup.b ;R.sup.b is independently selected at each occurrence from C.sub.1-4 alkyl, --NO.sub.2, halo, --CN, --NR.sup.6b R.sup.7a, --NR.sup.8 COR.sup.13a, --NR.sup.8 C(O)OR.sup.13a, --COR.sup.13, --OR.sup.10a, --CONR.sup.6b R.sup.7a, --NR.sup.8 CONR.sup.6b R.sup.7a, --C(O)OR.sup.10a, SH, and --S(O).sub.n R.sup.12 ;R.sup.6b is independently at each occurrence selected from H, C.sub.1-4 alkyl, C.sub.3-6 cycloalkyl and (C.sub.3-6 cycloalkyl)methyl;R.sup.7 is independently at each occurrence selected from H, C.sub.1-4 alkyl, C.sub.3-6 cycloalkyl and (C.sub.3-6 cycloalkyl)methyl;R.sup.7a is independently selected at each occurrence from H, C.sub.1-6 alkyl, phenyl, benzyl, C.sub.3-6 cycloalkyl, (C.sub.3-6 cycloalkyl)methyl, and C.sub.1-4 haloalkyl;alternatively, NR.sup.6a R.sup.7a is selected from piperidine, pyrrolidine, morpholine, thiomorpholine, thiomorpholine-oxide, and thiomorpholine-dioxide, and is substituted with 0-1 Re;R.sup.e is C.sub.1-4 alkyl;alternatively, NR.sup.6a R.sup.7a is piperazine or N-methylpiperazine, and is substituted with 0-1 R.sup.f ;R.sup.f is selected from C.sub.1-4 alkyl, C(O)C.sub.1-4 alkyl, C(O)benzyl, C(O)OC.sub.1-4 alkyl, C(O)O-benzyl, SO.sub.2 |--C.sub.1-4 alkyl, SO.sub.2 -benzyl, and SO.sub.2 -phenyl;R.sup.8 is independently at each occurrence selected from H, C.sub.1-4 alkyl, C.sub.3-6 cycloalkyl and (C.sub.3-6 cycloalkyl)C.sub.1-4 alkyl;R.sup.9 is independently at each occurrence selected from H, C.sub.1-4 alkyl, C.sub.3-6 cycloalkyl and (C.sub.3-6 cycloalkyl)C.sub.1-4 alkyl;R.sup.10 is independently at each occurrence selected from H, C.sub.1-4 alkyl, C.sub.1-4 haloalkyl, C.sub.3-6 cycloalkyl, and (C.sub.3-6 cycloalkyl)C.sub.1-4 alkyl;R.sup.10a is independently selected at each occurrence from H, C.sub.1-6 alkyl, phenyl, benzyl, C.sub.3-6 cycloalkyl, (C.sub.3-6 cycloalkyl)C.sub.1-4 alkyl, (C.sub.1-4 alkoxy)C.sub.1-4 alkyl, and C.sub.1-4 haloalkyl;R.sup.10b is independently selected at each occurrence from H, C.sub.1-6 alkyl, C.sub.2-4 alkenyl, phenyl, benzyl, C.sub.3-6 cycloalkyl, (C.sub.3-6 cycloalkyl)C.sub.1-4 alkyl, (C.sub.1-4 alkoxy)C.sub.1-4 alkyl, and C.sub.1-4 haloalkyl;R.sup.11 is independently at each occurrence selected from C.sub.1-4 alkyl, C.sub.1-4 haloalkyl, and C.sub.3-6 cycloalkyl;R.sup.12 is independently at each occurrence selected from C.sub.1-4 alkyl, C.sub.1-4 haloalkyl, (C.sub.1-4 alkoxy)C.sub.1-4 alkyl, C.sub.3-6 cycloalkyl, (C.sub.3-6 cycloalkyl)C.sub.1-4 alkyl, aryl, and (aryl)C.sub.1-4 alkyl;R.sup.13 is independently at each occurrence selected from H, C.sub.1-6 alkyl, phenyl, benzyl, C.sub.3-6 cycloalkyl, and (C.sub.3-6 cycloalkyl)C.sub.1-4 alkyl;R.sup.13a is independently at each occurrence selected from C.sub.1-6 alkyl, phenyl, benzyl, C.sub.3-6 cycloalkyl, and (C.sub.3-6 cycloalkyl)C.sub.1-4 alkyl;aryl is independently at each occurrence selected from phenyl and naphthyl, and is substituted with 0-3 R.sup.g ;R.sup.g is independently at each occurrence selected from C.sub.1-6 alkyl, C.sub.3-6 cycloalkyl, halo, C.sub.1-4 haloalkyl, cyano, nitro, --OR.sup.10a, SH, --S(O).sub.n R.sup.15, --COR.sup.16, --C(O)OR.sup.16, --OC(O)R.sup.17, --NR.sup.8 COR.sup.16a, --NR.sup.8 CONR.sup.6a R.sup.7a, --NR.sup.8 C(O)OR.sup.16a, --NR.sup.6a R.sup.7a, and --CONR.sup.6a R.sup.7a ;R.sup.15 is independently at each occurrence selected from C.sub.1-4 alkyl, C.sub.1-4 haloalkyl, (C.sub.1-4 alkoxy)C.sub.1-4 alkyl, C.sub.3-6 cycloalkyl, (C.sub.3-6 cycloalkyl)C.sub.1-4 alkyl, phenyl, benzyl, (phenyl)C.sub.1-4 alkyl and (naphthyl)C.sub.1-4 alkyl;R.sup.16 is independently at each occurrence selected from H, C.sub.1-6 alkyl, phenyl, benzyl, C.sub.3-6 cycloalkyl, and (C.sub.3-6 cycloalkyl)C.sub.1-4 alkyl;R.sup.16a is independently at each occurrence selected from C.sub.1-6 alkyl, phenyl, benzyl, C.sub.3-6 cycloalkyl, and (C.sub.3-6 cycloalkyl)C.sub.1-4 alkyl;R.sup.17 is independently at each occurrence selected from C.sub.1-4 alkyl, C.sub.1-4 haloalkyl, (C.sub.1-4 alkoxy)C.sub.1-4 alkyl, C.sub.3-6 cycloalkyl, (C.sub.3-6 cycloalkyl)C.sub.1-4 alkyl, phenyl, benzyl, (phenyl)C.sub.1-4 alkyl, (naphthyl)C.sub.1-4 alkyl, heteroaryl and (heteroaryl)C.sub.1-4 alkyl;heteroaryl is independently at each occurrence selected from pyridyl, pyrimidinyl, triazinyl, furanyl, quinolinyl, isoquinolinyl, thienyl, imidazolyl, thiazolyl, indolyl, pyrrolyl, oxazolyl, benzofuranyl, benzothienyl, benzthiazolyl, isoxazolyl, pyrazolyl, triazolyl, tetrazolyl, and indazolyl, and is substituted with 0-3 R.sup.h ;heterocyclyl is saturated or partially saturated heteroaryl, substituted with 0-3 R.sup.h ; andR.sup.h is independently at each occurrence selected from C.sub.1-6 alkyl, C.sub.3-6 cycloalkyl, halo, C.sub.1-4 haloalkyl, cyano, nitro, --OR.sup.10a, SH, --S(O).sub.n R.sup.15, --COR.sup.16, --C(O)OR.sup.16, --OC(O)R.sup.18, --NR.sup.8 COR.sup.16a, NR.sup.8 CONR.sup.6a R.sup.7a, --NR.sup.8 CO.sub.2 R.sup.16a, --NR.sup.6a R.sup.7a, and --CONR.sup.6a R.sup.7a ;R.sup.18 is independently selected at each occurrence from C.sub.1-6 alkyl, C.sub.3-6 cycloalkyl, phenyl and benzyl; andn is independently at each occurrence selected from 0, 1 and 2.