Patent ID: 6284755
Filing Date: 2001-09-04
Classification: A61P,C07D

Abstract:
A compound of the formula I: ##STR69##wherein:R.sup.1a, R.sup.1b and R.sup.1c are independently selected from:a) hydrogen,b) unsubstituted or substituted aryl, unsubstituted or substituted heterocycle, C.sub.3 -C.sub.10 cycloalkyl, C.sub.2 -C.sub.6 alkenyl, C.sub.2 -C.sub.6 alkynyl, R.sup.9 S(O).sub.q --, CN, NO.sub.2, R.sup.8 C(O)--, R.sup.8 OC(O)--, (R.sup.8).sub.2 NC(O)--, --N(R.sup.15).sub.2, --OR.sup.15, --N(R.sup.8)S(O).sub.q R.sup.8 or N.sub.3 ;c) C.sub.1 -C.sub.6 alkyl, unsubstituted or substituted by unsubstituted or substituted aryl, unsubstituted or substituted heterocycle, 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.q --, CN, R.sup.8 C(O)--, R.sup.8 OC(O)--, N(R.sup.8).sub.2, N.sub.3, or R.sup.8 C(O)O--;R.sup.1 is independently selected from:a) H,b) unsubstituted or substituted C.sub.1 -C.sub.6 alkyl,c) unsubstituted or substituted aryl,d) unsubstituted or substituted heterocycle,e) --(C.sub.1 -C.sub.6 alkyl)N(R.sup.8).sub.2,f) --R.sup.8 C(O)R.sup.8,g) --(C.sub.1 -C.sub.6 alkyl)OR.sup.8,h) --N(R.sup.8).sub.2,i) --OR.sup.8,j) --R.sup.8 NHC(O)R.sup.8,k) --R.sup.8 C(O)N(R.sup.8).sub.2,l) CF.sub.3,m) halo,n) --C(O)OR.sup.8,o) C.sub.2 -C.sub.6 alkynyl,p) C.sub.2 -C.sub.6 alkenyl,q) perfluoroalkyl,r) N.sub.3,s) NO.sub.2,t) CN,u) R.sup.9 S(O).sub.q --,v) --(C.sub.1 -C.sub.6 alkyl)NR.sup.8 C(O)N(R.sup.8).sub.2, andw) --(C.sub.1 -C.sub.6 alkyl)R.sup.14 ;R.sup.2 is independently selected from:a) hydrogen,b) CN,c) NO.sub.2,d) halogen,e) aryl, unsubstituted or substituted,f) heteroaryl, unsubstituted or substituted,g) C.sub.1 -C.sub.6 alkyl, unsubstituted or substituted,h) OR.sup.8,i) N.sub.3,j) R.sup.9 S(O).sub.q,k) R.sup.8 HC.dbd.CH--, andl) R.sup.8 C.ident.C--;R.sup.3 is independently selected from:a) H,b) CN,c) NO.sub.2,d) halogen,e) C.sub.1 -C.sub.6 alkyl, unsubstituted or substituted,f) OR.sup.8,g) aryl, unsubstituted or substituted,h) heteroaryl, unsubstituted or substituted, andi) CF.sub.3 ;R.sup.5 and R.sup.6 are independently selected from:a) H,b) CN,c) NO.sub.2,d) halogen,e) C.sub.1 -C.sub.6 alkyl, unsubstituted or substituted,f) N.sub.3,g) R.sup.9 S(O).sub.q,h) --HC.dbd.CH.sub.2,i) HC.ident.C--,j) aryl, unsubstituted or substituted,k) heterocycle, unsubstituted or substituted,l) CF.sub.3 O--,m) CF.sub.3 CH.sub.2 O--,n) C.sub.3 -C.sub.10 cycloalkyl,o) CF.sub.3,p) --(C.sub.1 -C.sub.6 alkyl)N(R.sup.8).sub.2,q) --(C.sub.1 -C.sub.6 alkyl)OR.sup.8,r) OR.sup.8,S) N(R.sup.8).sub.2,t) --C(O)(C.sub.1 -C.sub.6 alkyl),u) --(C.sub.1 -C.sub.6 alkyl)C(O)R.sup.8,v) --C(O)O(C.sub.1 -C.sub.6 alkyl),w) --C(O)N(R.sup.8).sub.2,x) --(C.sub.1 -C.sub.6 alkyl)NR.sup.8 C(O)N(R.sup.8).sub.2,y) --(C.sub.1 -C.sub.6 alkyl)NR.sup.8 C(O)R.sup.8,z) --C.sub.2 -C.sub.6 alkynyl,aa) --C.sub.2 -C.sub.6 alkenyl,bb) --(C.sub.1 -C.sub.6 alkyl)N.sub.3,cc) --(C.sub.1 -C.sub.6 alkyl)NR.sup.8 S(O).sub.q, anddd) --(C.sub.1 -C.sub.6 alkyl)NR.sup.8 (C.sub.1 -C.sub.6 alkyl)N(R.sup.8).sub.2 ;R.sup.8 is independently selected from hydrogen, unsubstituted or substituted C.sub.1 -C.sub.6 alkyl, unsubstituted or substituted aralkyl, unsubstituted or substituted heterocycle and unsubstituted or substituted aryl;R.sup.9 is independently selected from unsubstituted or substituted C.sub.1 -C.sub.6 alkyl, unsubstituted or substituted benzyl and unsubstituted or substituted aryl;R.sup.14 is unsubstituted saturated heterocycle;R.sup.15 is independently selected froma) hydrogen, unsubstituted or substituted aryl, unsubstituted or substituted heterocycle, C.sub.3 -C.sub.10 cycloalkyl, C.sub.2 -C.sub.6 alkenyl, C.sub.2 -C.sub.6 alkynyl, R.sup.9 S(O).sub.2 --, R.sup.8 C(O)--, R.sup.8 OC(O)--, (R.sup.8).sub.2 NC(O)--, andb) C.sub.1 -C.sub.6 alkyl, unsubstituted or substituted by unsubstituted or substituted aryl, unsubstituted or substituted heterocycle, 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.q --, CN, R.sup.8 C(O)--, R.sup.8 OC(O)--, N(R.sup.8).sub.2, N.sub.3, or R.sup.8 C(O)O--;A.sup.1 and A.sup.2 are independently selected from:a) a bond,b) --HC.dbd.CH--,c) --C.ident.C--,d) O,e) S(O).sub.q,f) OC(O),g) C(O),h) C(O)O, andi) NR.sup.8 ;A.sup.3 is selected from a bond, --C(.dbd.O)--, ##STR70##and C.sub.3 -C.sub.6 cycloalkyl;M is CH.sub.2 ;Q is C(.dbd.O);W is selected from:a) heterocycle, andb) aryl;Y is selected from:a) aryl, andb) heterocycle;Z is selected from:a) aryl,b) heterocycle,c) C.sub.3 -C.sub.6 cycloalkyl, andd) a bond;m is 0, 1, 2, 3 or 4;n is 0, 1, 2, 3 or 4;p is 0, 1, 2, 3 or 4;q is 0, 1 or 2;r is 0, 1, 2, 3, or 4;s is 0, 1, 2, 3 or 4;t is 0, 1, 2 or 3; andx is 0, 1, 2 or 3;provided that the moiety ##STR71##does not represent a bond; andprovided that if attachment of ##STR72##to the rest of the molecule is through a nitrogen ring atom, then A.sup.1 is NR.sup.8, O, or S(O).sub.q ;provided that the sum of variables x and t will be equal to 3;or a pharmaceutically acceptable salt, an optical isomer or stereoisomer thereof.