Patent ID: 6310211
Filing Date: 2001-10-30
Classification: A61P,C07D,C07F

Abstract:
A compound of formula IA ##STR363##wherein R.sup.0 isa) --CH.sub.2).sub.n -phenyl substituted with Cl, Br, --O-phenyl, CF.sub.3, or --S-phenyl substituted with ethoxy; provided that when R.sup.0 is a), R.sub.1 is H, F, Cl, or Br; R.sub.2 is H, --CH.dbd.CH-furanyl, or --CH.dbd.CH-phenyl, optionally substituted with methoxy, and R.sub.3 is H;b) --(CH.sub.2).sub.n -phenyl substituted with two Cl atoms or two F atoms provided that the F atom is at 2-, or 6-position of the phenyl ring;c) --(CH.sub.2).sub.n -indolyl,d) --(CH.sub.2).sub.n -benzothiazolyl,e) --(CH.sub.2).sub.n -naphthyl,f) --(CH.sub.2).sub.n -biphenyl,g) --(CH.sub.2).sub.n -tetrahydro-naphthyl,h) --(CH.sub.2).sub.n -fluorenyl;i) --(CH.sub.2).sub.n -Y,j) --(CH.sub.2).sub.p W.sup.1 X.sup.2,k) --(CH.sub.2).sub.p W.sup.1 CH.sub.2 X.sup.1, orl) --(CH.sub.2).sub.n --CHR.sup.9 --(CH.sub.2).sub.n --X.sup.1,wherein R.sup.1 isa) --H,b) --F,c) --Cl,d) --Br,e) --CF.sub.3, orf) --NO.sub.2 ;wherein R.sup.2 isa) --H,b) --C.sub.1 -C.sub.3 alkyl,c) --OH,d) --CF.sub.3,e) --CH.dbd.CH-furanyl,f) --CH.dbd.CH-phenyl substituted by zero (0) or one (1) R.sup.4,g) --CH.dbd.CH-pyridinyl,h) --(CH.sub.2).sub.p -phenyl substituted by zero (0) or one (1) R.sup.4,i) --NHV.sup.1,j) --CH.sub.2 NHV.sup.1, ork) --CH.sub.2 Z.sup.1 ;wherein R.sup.3 isa) --H,b) --OH,c) --CF.sub.3, ord) --C.sub.1 -C.sub.3 alkyl;wherein R.sup.4 isa) --Hb) --F,c) --Cl,d) --Br,e) --NO.sub.2,f) --CF.sub.3,g) --W.sup.1 --R.sup.10,h) --C.sub.1 -C.sub.6 alkyl,i) --C.sub.3 -C.sub.8 cycloalkyl,j) --(CH.sub.2).sub.n -aryl,k) --CH.sub.2 --C.sub.3 -C.sub.8 cycloalkyl,l) --SO.sub.2 NH-indazoylm) --CN,n) --I, oro) --CH.sub.2 --OH;wherein R.sup.8 isa) --C.sub.1 -C.sub.4 alkyl,b) --W.sup.1 --H, orc) --CH.sub.2 W.sup.1 H;wherein R.sup.9 isa) --C.sub.1 -C.sub.7 alkyl,b) --C.sub.3 -C.sub.8 cycloalkyl,c) --C(O)R.sup.11,d) --C(O)NHR.sup.11,e) --CH(OH)R.sup.11,f) --CH.sub.2 OH,g) --CO.sub.2 R.sup.11, orh) -aryl;wherein R.sup.10 isa) --H,b) --C.sub.1 -C.sub.6 alkyl,c) --C.sub.3 -C.sub.8 cycloalkyl,d) --(CH.sub.2).sub.n -aryl optionally substituted with F, Cl, CH.sub.2 OH or --NO.sub.2,e) --CH.sub.2 --C.sub.3 -C.sub.8 cycloalkyl,wherein R.sup.11 isa) --C.sub.1 -C.sub.7 alkyl,b) --C.sub.3 -C.sub.8 cycloalkyl,c) --(CH.sub.2).sub.n X.sup.1, ord) --CH.sub.2 --C.sub.3 -C.sub.8 cycloalkyl;wherein Y isa) --CH(OH)-phenyl,b) --S-phenyl,c) --NHSO.sub.2 -phenyl substituted by one (1), two (2) or three (3) R.sup.4,d) --CN,e) --C.sub.3 -C.sub.8 cycloalkyl substituted by ethoxy, t-butyl or two (2) R.sup.8, orf) -4-cyano-2,3,5,6-tetrafluoro-phenyl;wherein X.sup.1 isa) -aryl substituted by zero (0), one (1), two (2), or three (3) R.sup.4,b) -het substituted by zero (0), one (1) or two (2) R.sup.5,c) --C.sub.7 -C.sub.8 alkyl, provided that when X.sup.1 is alkyl, R.sup.9 is not alkyl;d) --CH(OH)-phenyl,e) --S-phenyl,f) --NHSO.sub.2 -phenyl substituted by one (1), two (2) or three (3) R.sup.4,g) --CN,h) --C.sub.3 -C.sub.8 cycloalkyl substituted by ethoxy, t-butyl or two (2) R.sup.8, ori) -4-cyano-2,3,5,6-tetrafluorophenyl;wherein X.sup.2 isa) -aryl substituted by zero (0), one (1), two (2) or three (3) R.sup.4,b) --C.sub.1 -C.sub.8 alkyl,c) --CH(OH)-phenyl, ord) --C.sub.3 -C.sub.8 cycloalkyl substituted by zero (0), one (1) or two (2) R.sup.8 ;wherein W.sup.1 isa) oxygen, provided that when X.sup.1 or X.sup.2 is phenyl, W.sup.1 is not oxygen,b) --NH, orb) -sulfur,wherein V.sup.1 isa) --R.sub.11,b) --C(O)R.sup.11,c) --SO.sub.2 R.sup.11, ord) --C(O)NHR.sup.11 ;wherein Z.sup.1 isa) --C.sub.1 -C.sub.7 alkyl,b) --C.sub.3 -C.sub.8 cycloalkyl,c) --C(O)R.sup.11,d) --C(O)NHR.sup.11, ore) --CO.sub.2 R.sup.11 ;wherein -aryl isa) -phenyl,b) -naphthyl,c) -biphenyl,d) -tetrahydro-naphthyl, ore) fluorenyl;wherein -het is a 5-membered saturated or unsaturated ring having from one (1) to three (3) heteroatoms selected from the group consisting of nitrogen, oxygen and sulfur,wherein -cycloalkyl is a saturated or unsaturated hydrocarbon ring, optionally fused to a benzene ring;n is zero (0) to six (6), inclusive, provided that where R.sup.0 is a)-h), n is at least one; and p is one (1), two (2) or three (3);or a pharmaceutically acceptable salt or N-oxide thereof.