Patent ID: 6069163
Filing Date: 2000-05-30
Classification: A61P,C07C,C07D

Abstract:
A compound having the formula I: ##STR57## or a pharmaceutically acceptable salt thereof wherein: R1 is 1) C1-10alkyl, 2) C2-10alkenyl, 3) C2-10alkynyl, 4) Cy, 5) Cy-C1-10alkyl, 6) Cy-C2-10alkenyl, 7) Cy-C2-10alkynyl,  wherein alkyl, alkenyl, and alkynyl are optionally substituted with one to four substituents independently selected from R.sup.a ; and Cy is optionally substituted with one to four substituents independently selected from R.sup.b ;R.sup.2 and R.sup.3 together with the atoms to which they are attached form a ring of 4 to 7 members containing 0-1 additional heteroatoms independently selected from oxygen, sulfur and nitrogen, wherein said ring may be isolated or benzo-fused, and optionally substituted with one to four substituents independently selected from R.sup.b ;R.sup.4 is 1) hydrogen, 2) C.sub.1-10 alkyl, 3) Cy, or 4) Cy-C.sub.1-10 alkyl;  wherein alkyl is optionally substituted with one to four substituents independently selected from R.sup.a, and Cy is optionally substituted with one to four substituents independently selected from R.sup.b ;R.sup.5 is selected from the group consisting of 1) hydrogen, 2) C.sub.1-10 alkyl, 3) C.sub.2-10 alkenyl, 4) C.sub.2-10 alkynyl, 5) aryl, 6) aryl C.sub.1-10 alkyl, 7) heteroaryl, and 8) heteroaryl C.sub.1-10 alkyl,  wherein alkyl, alkenyl and alkynyl are optionally substituted with one to four substituents independently selected from R.sup.a, and aryl and heteroaryl are optionally substituted with one to four substituents independently selected from R.sup.b ;R.sup.6 is 1) hydrogen, 2) C.sub.1-10 alkyl, 3) C.sub.2-10 alkenyl, 4) C.sub.2-10 alkynyl, 5) Cy, 6) Cy-C.sub.1-10 alkyl, 7) Cy-C.sub.2-10 alkenyl, 8) Cy-C.sub.2-10 alkynyl, 9) Ar.sup.1 --Ar.sup.2 --C.sub.1-10 alkyl, 10) Ar.sup.1 --Ar.sup.2 --C.sub.2-10 alkenyl, 11) Ar.sup.1 --Ar.sup.2 --C.sub.2-10 alkynyl, 12) Ar.sup.1 --C.sub.2 alkynyl-Ar.sup.2 --C.sub.1-10 alkyl, 13) Ar.sup.1 --C.sub.2 alkenyl-Ar.sup.2 --C.sub.1-10 alkyl, 14) Ar.sup.1 --Ar.sup.2,  wherein Ar.sup.1 and Ar.sup.2 are independently aryl or heteroaryl, and each is optionally substituted with one to four substituents independently selected from R.sup.b ; alkyl, alkenyl and alkynyl are optionally substituted with one to four substituents independently selected from R.sup.a ; and Cy is optionally substituted with one to four substituents independently selected from R.sup.b except aryl and heteroaryl;R.sup.a is 1) --CF.sub.3 ; 2) --OR.sup.d, 3) --NO.sub.2, 4) halogen 5) --S(O).sub.m R.sup.d, 6) --SR.sup.d, 7) --S(O).sub.2 OR.sup.d, 8) --S(O).sub.m NR.sup.d R.sup.e, 9) --NR.sup.d R.sup.e, 10) --O(CR.sup.f R.sup.g).sub.n NR.sup.d R.sup.e, 11) --C(O)R.sup.d, 12) --CO.sub.2 R.sup.d, 13) --CO.sub.2 (CR.sup.f R.sup.g).sub.n CONR.sup.d R.sup.e, 14) --OC(O)R.sup.d, 15) --CN, 16) --C(O)NR.sup.d R.sup.e, 17) --NR.sup.d C(O)R.sup.e, 18) --OC(O)NR.sup.d R.sup.e, 19) --NR.sup.d C(O)OR.sup.e, 20) --NR.sup.d C(O)NR.sup.d R.sup.e, or 21) --CR.sup.d (N--OR.sup.e);  R.sup.b is 1) a group selected from R.sup.a, 2) C.sub.1-10 alkyl, 3) C.sub.2-10 alkenyl, 4) C.sub.2-10 alkynyl, 5) aryl C.sub.1-10 alkyl, 6) heteroaryl C.sub.1-10 alkyl, 7) aryl, or 8) heteroaryl;  wherein alkyl, alkenyl, alkynyl, aryl, heteroaryl are optionally substituted with a group independently selected from R.sup.c ;R.sup.c is 1) halogen, 2) amino, 3) carboxy, 4) C.sub.1-4 alkyl, 5) C.sub.1-4 alkoxy, 6) hydroxy, 7) aryl, 8) aryl C.sub.1-4 alkyl, or 9) aryloxy;  R.sup.d and R.sup.e are independently selected from the group consisting of 1) hydrogen, 2) C.sub.1-10 alkyl, 3) C.sub.2-10 alkenyl, 4) C.sub.2-10 alkynyl, 5) Cy, and 6) Cy C.sub.1-10 alkyl,  wherein alkyl, alkenyl, alkynyl and Cy is optionally substituted with one to four substituents independently selected from R.sup.c ; orR.sup.d and R.sup.e together with the atoms to which they are attached form a heterocyclic ring of 5 to 7 members containing 0-2 additional heteroatoms independently selected from oxygen, sulfur and nitrogen;R.sup.f and R.sup.g are independently selected from hydrogen, C.sub.1-10 alkyl, Cy and Cy C.sub.1-10 alkyl; orR.sup.f and R.sup.g together with the carbon to which they are attached form a ring of 5 to 7 members containing 0-2 heteroatoms independently selected from oxygen, sulfur and nitrogen;R.sup.h is 1) hydrogen, 2) C.sub.1-10 alkyl, 3) C.sub.2-10 alkenyl, 4) C.sub.2-10 alkynyl, 5) cyano, 6) aryl, 7) aryl C.sub.1-10 alkyl, 8) heteroaryl, 9) heteroaryl C.sub.1-10 alkyl, or 10) --SO.sub.2 R.sup.i ;  wherein alkyl, alkenyl, and alkynyl are optionally substituted with one to four substituents independently selected from R.sup.a ; and aryl and heteroaryl are each optionally substituted with one to four substituents independently selected from R.sup.b ;R.sup.i 1) C.sub.1-10 alkyl, 2) C.sub.2-10 alkenyl, 3) C.sub.2-10 alkynyl, or 4) aryl;  wherein alkyl, alkenyl, alkynyl and aryl are each optionally substituted with one to four substituents independently selected from R.sup.c ;Cy is cycloalkyl, heterocyclyl, aryl, or heteroaryl;m is an integer from 0 to 2;n is an integer from 0 to 2;X is 1) --C(O)OR.sup.d, 2) --P(O)(OR.sup.d)(OR.sup.e) 3) --P(O)(R.sup.d)(OR.sup.e) 4) --S(O).sub.m OR.sup.d, 5) --C(O)NR.sup.d R.sup.h, 6) 5-tetrazolyl, or 7) CONHSO.sub.2 R.sup.i ; and  Y is 1) --C(O)--, 2) --O--C(O)--, 3) --NR.sup.e --C(O)--, 4) --S(O).sub.2 --, 5) --P(O)-- 6) --C(O)C(O)--.