Patent ID: 6172076
Filing Date: 2001-01-09
Classification: C07D

Abstract:
A compound illustrated by the formula I: ##STR129##wherein:R.sup.1a and R.sup.1b are independently selected from:a) hydrogen, orb) C.sub.1 -C.sub.6 alkyl unsubstituted or substituted by unsubstituted or substituted aryl, C.sub.3 -C.sub.10 cycloalkyl, C.sub.2 -C.sub.6 alkenyl, C.sub.2 -C.sub.6 alkynyl, R.sup.8 O--, R.sup.9 S(O).sub.m --, R.sup.8 C(O)NR.sup.8 --, CN, (R.sup.8).sub.2 N--C(NR.sup.8)--, R.sup.8 C(O)--, R.sup.8 OC(O)--, N.sub.3, --N(R.sup.8).sub.2, or R.sup.9 OC(O)--NR.sup.8 --;R.sup.1 is selected from:a) unsubstituted or substituted aryl, C.sub.3 -C.sub.10 cycloalkyl, C.sub.2 -C.sub.6 alkenyl, C.sub.2 -C.sub.6 alkynyl, perfluoroalkyl, F, Cl, Br, R.sup.8 O--, R.sup.9 S(O).sub.m --, R.sup.8 C(O)NR.sup.8 --, CN, NO.sub.2, R.sup.8.sub.2 N--C(NR.sup.8)--, R.sup.8 C(O)--, R.sup.8 OC(O)--, N.sub.3, --N(R.sup.8).sub.2, or R.sup.9 OC(O)NR.sup.8 --, andb) C.sub.1 -C.sub.6 alkyl unsubstituted or substituted by aryl, C.sub.3 -C.sub.10 cycloalkyl, C.sub.2 -C.sub.6 alkenyl, C.sub.2 -C.sub.6 alkynyl, perfluoroalkyl, F, Cl, Br, R.sup.8 O--, R.sup.9 S(O).sub.m --, R.sup.8 C(O)NH--, CN, H.sub.2 N--C(NH)--, R.sup.8 C(O)--, R.sup.8 OC(O)--, N.sub.3, --N(R.sup.8).sub.2, or R.sup.8 OC(O)NH--;R.sup.2 is independently selected from:a) hydrogen,b) unsubstituted or substituted aryl, C.sub.3 -C.sub.10 cycloalkyl, C.sub.2 -C.sub.6 alkenyl, C.sub.2 -C.sub.6 alkynyl, perfluoroalkyl, F, ClBr, R.sup.8 O--, R.sup.9 S(O).sub.m --, R.sup.8 C(O)NR.sup.8 --, CN, NO.sub.2, R.sup.8.sub.2 N--C(NR.sup.8)--, R.sup.8 C(O)--, R.sup.8 OC(O)--, N.sub.3, --N(R.sup.8).sub.2, or R.sup.9 OC(O)NR.sup.8 --, andc) C.sub.1 -C.sub.6 alkyl unsubstituted or substituted by aryl, C.sub.3 -C.sub.10 cycloalkyl, C.sub.2 -C.sub.6 alkenyl, C.sub.2 -C.sub.6 alkynyl, perfluoroalkyl, F, Cl, Br, R.sup.8 O--, R.sup.9 S(O).sub.m --, R.sup.8 C(O)NH--, CN, H.sub.2 N--C(NH)--, R.sup.8 C(O)--, R.sup.8 OC(O)--, N.sub.3, --N(R.sup.8).sub.2, or R.sup.8 OC(O)NH--;R.sup.3 is selected from:a) hydrogen,b) C.sub.2 -C.sub.6 alkenyl, C.sub.2 -C.sub.6 alkynyl, C.sub.3 -C.sub.6 cycloalkyl, perfluoroalkyl, F, Cl, Br, R.sup.8 O--, R.sup.9 S(O).sub.m --, R.sup.8 C(O)NR.sup.8 --, CN, NO.sub.2, (R.sup.8).sub.2 N--C--(NR.sup.8)--, R.sup.8 C(O)--, R.sup.8 OC(O)--, N.sub.3, --N(R.sup.8).sub.2, or R.sup.9 OC(O)NR.sup.8 --, andc) C.sub.1 -C.sub.6 alkyl, unsubstituted or substituted by perfluoroalkyl, F, Cl, Br, R.sup.8 O--, R.sup.9 S(O).sub.m --, R.sup.8 C(O)NR.sup.8 --, CN, (R.sup.8).sub.2 N--C(NR.sup.8)--, R.sup.8 C(O)--, R.sup.8 OC(O)--, N.sub.3, --N(R.sup.8).sub.2, or R.sup.9 OC(O)NR.sup.8 --;R.sup.4a and R.sup.4b independently are selected from:H, .dbd.O, unsubstituted or substituted C.sub.1-8 alkyl, or unsubstituted or substituted aryl;R.sup.4c and R.sup.5 independently are selected from:H, .dbd.O, unsubstituted or substituted C.sub.1-8 alkyl, unsubstituted or substituted C.sub.2-8 alkenyl, unsubstituted or substituted aryl, ##STR130##and --S(O).sub.2 R.sup.6, wherein the substituted group is substituted with one or more of:1) aryl, unsubstituted or substituted with one or two groups selected from:a) C.sub.1-4 alkyl,b) (CH.sub.2).sub.p OR.sup.6,c) (CH.sub.2).sub.p NR.sup.6 R.sup.7,d) halogen,e) C.sub.1-4 perfluoroalkyl,2) C.sub.3-6 cycloalkyl,3) OR.sup.6,4) SR.sup.6, S(O)R.sup.6, SO.sub.2 R.sup.6,5) --NR.sup.6 R.sup.7 ##STR131##15) C.sub.1-8 alkyl,16) C.sub.1-8 perfluoroalkyl, or17) halo;R.sup.6, R.sup.7 and R.sup.7a are independently selected from: H, C.sub.1-4 alkyl, C.sub.3-6 cycloalkyl, aryl, C.sub.1-4 perfluoroalkyl, unsubstituted or substituted with one or two substituents selected from:a) C.sub.1-4 alkoxy,b) substituted or unsubstituted aryl,c) halogen,d) HO, ##STR132##g) --S(O).sub.m R.sup.9, orh) N(R.sup.8).sub.2 ; orR.sup.8 is independently selected from hydrogen, C.sub.1 -C.sub.6 alkyl, benzyl, 2,2,2-trifluoroethyl and aryl;R.sup.9 is independently selected from C.sub.1 -C.sub.6 alkyl and aryl;A.sup.1 and A.sup.2 are bonds;X.sup.1 and X.sup.3 are N(H).sub.w ;X.sup.2 and X.sup.5 are C(H).sub.y ;X.sup.4 is selected from:C(H).sub.y, N(H).sub.w, O, C.dbd.O, S(O).sub.2, and PO(OMe);u is 0;V is an aryl,W is an imidazolyl;m is 0, 1 or 2;n is 0, 1, 2, 3 or 4;p is 0 1, 2, 3 or 4;r is independently 0 to 5;s is 1 or 2;t is 1;w is 0 or 1; andy is 1 or 2;dashed lines represent optional double bondsor the pharmaceutically acceptable salts or the optical isomers thereof.