Patent ID: 6127391
Filing Date: 2000-10-03
Classification: A61K,A61P,B41J,C07C,C07D,C07K

Abstract:
A compound of formula I ##STR806## wherein R.sup.1 and R.sup.2 are independently hydrogen, or C.sub.1-6 -alkyl optionally substituted with aryl;a and b are independently 1 or 2;G is --O--(CH.sub.2).sub.k --R.sup.27a ; ##STR807## wherein R.sup.27, R.sup.28, R.sup.29, R.sup.30, R.sup.31, R.sup.32 and R.sup.33 independently are hydrogen, halogen, aryl, C.sub.1-6 -alkyl or C.sub.1-6 -alkoxy;k is 0, 1 or 2;R.sup.27a is phenyl;D is ##STR808## wherein R.sup.3, R.sup.7, R.sup.8 and R.sup.9 are independently hydrogen or C.sub.1-6 -alkyl optionally substituted with halogen, amino, hydroxyl or aryl;n, m and q are independently 0, 1, 2, or 3;p is 0 or 1;M is --CR.sup.11 .dbd.CR.sup.11a --, aryl, --O--, or --S--;R.sup.11 and R.sup.11a are independently hydrogen, or C.sub.1-6 -alkyl optionally substituted with aryl;when E is--CONR.sup.12 R.sub.13, --(CH.sub.2).sub.v --NR.sup.12 SO.sub.2 R.sup.14, --(CH.sub.2).sub.v --NR.sup.12 COR.sup.13, --CH.sub.2).sub.v --OR.sup.13b, --(CH.sub.2).sub.v OCOR.sup.13, --CH(R.sup.12)R.sup.13, --(CH.sub.2).sub.v --NR.sup.12 --CS--NR.sup.13 R.sup.14, --(CH.sub.2).sub.v --NR.sup.12 --CO--NR.sup.13 R.sup.14, ##STR809## wherein X is --N(R.sup.15)--, --O--, --S--,V is --C(R.sup.16).dbd. or --N.dbd.,Y is --C(R.sup.17).dbd. or --N.dbd.,Z is --C(R.sup.18).dbd. or --N.dbd.,R.sup.15 is hydrogen or C.sub.1-6 -alkyl optionally substituted with aryl, R.sup.16, R.sup.17 and R.sup.18 independently are hydrogen, --COOR.sup.19, --CONR.sup.20 R.sup.21, --(CH.sub.2).sub.w NR.sup.20 R.sup.21, --(CH.sub.2).sub.w OR.sup.18, --(CH.sub.2).sub.w R.sup.19 or halogen;R.sup.12, R.sup.13, R.sup.19, R.sup.20 and R.sup.21 independently are hydrogen or C.sub.1-6 -alkyl optionally substituted with halogen, --N(R.sup.22)R.sup.23, --CF.sub.3, hydroxyl, C.sub.1-6 -alkoxy, C.sub.1-6 -alkoxycarbonyl, C.sub.1-6 -alkylcarbonyloxy or aryl,or R.sup.13 is ##STR810## wherein Q is --CH< or --N<,K and L are independently --CH.sub.2 --, --CO--, --O--, --S--, --NR.sup.25 -- or a valence bond, where R.sup.26 is hydrogen or C.sub.1-6 -alkyl;t and u are independently 0, 1, 2, 3 or 4;R.sup.13a is C.sub.1-6 alkyl substituted with aryl;R.sup.14 is C.sub.1-6 alkyl;R.sup.22 and R.sup.23 are independently hydrogen or C.sub.1-6 -alkyl;v and w are independently 0, 1, 2 or 3: orD isR.sup.7 --NH--(CR.sup.8 R.sup.9).sub.p --(CH.sub.2).sub.m --M--(CHR.sup.10).sub.o --(CH.sub.2).sub.n --wherein R.sup.7, R.sup.8 , R.sup.9 and R.sup.10 are independently hydrogen or C.sub.1-6, alkyl optionally substituted with halogen, amino, hydroxyl or aryl;R.sup.7 and R.sup.8 or R.sup.7 and R.sup.8' or R.sup.8 and R.sup.8 optionally forming --(CH.sub.2).sub.i --U--(CH.sub.2).sub.j --, wherein i and j are independently are 1 or 2 and U is --O--, --S-- or a valence bond;n and m are independently 0, 1, 2, or 3;o and p are independently 0 or 1;M is --CR.sup.11 .dbd.CR.sup.11a, aryl, --O--, or --S--;R.sup.11 and R.sup.11a are independently hydrogen, or C.sub.1-6 -alkyl optionally substituted with aryl,when E is--CONR.sup.12 R.sup.13, --(CH.sub.2).sub.v --NR.sup.12 SO.sub.2 R.sup.14, --(CH.sub.2).sub.v --NR.sup.12 COR.sup.13, --(CH.sub.2).sub.v --OR.sup.13a, --CH.sub.2).sub.v --OCOR.sup.13, --CH(R.sup.12)R.sup.13, --(CH.sub.2).sub.v --NR.sup.12 --CS--NR.sup.14 or --(CH.sub.2).sub.v --NR.sup.12 --CO--NR.sup.13 R.sup.14,whereinR.sup.12 and R.sup.13 independently are hydrogen or C.sub.1-6 -alkyl optionally substituted with halogen, --CONR.sup.22 R.sup.23, --N(R.sup.22)R.sup.23, --CF.sub.3, hydroxyl, C.sub.1-6 -alkoxy, C.sub.1-6 -alkoxycarbonyl, C.sub.1-6 -alkylcarbonyloxy or aryl;or R.sup.13 is ##STR811## wherein Q is --CH< or --N<,K and L are independently --CH.sub.2 --, --CO--, --O--, --S--, --NR.sup.28 -- or a valence bond,where R.sup.28 is hydrogen or C.sub.1-6 alkyl;t and u are independently 0, 1, 2, 3 or 4;R.sup.13a is C.sub.1-6 alkyl substituted with aryl;R.sup.14 is C.sub.1-6 alkyl;R.sup.22 and R.sup.23 are independently hydrogen or C.sub.1-6 alkyl;v and w are independently 0, 1, 2 or 3:or a pharmaceutically acceptable salt thereof.