Patent ID: 6245763
Filing Date: 2001-06-12
Classification: A61P,C07D,C07K

Abstract:
A compound having the Formula VII: ##STR135##or a solvate, hydrate or pharmaceutically acceptable salt thereof; wherein:R.sup.1 is alkyl, cycloalkyl, cycloalkylalkyl, alkenyl, alkynyl, aryl, aralkyl, any of which may be optionally substituted;Z is --SO.sub.2 --, --OCO--, or --CO--;Het is selected from the group consisting of ##STR136##whereR.sup.3 and R.sup.5 are independently hydrogen, alkyl, cycloalkyl, alkenyl, alkynyl, optionally substituted aryl, optionally substituted aralkyl, trifluoromethyl, halogen, hydroxyalkyl, cyano, nitro, carboxamido, alkoxycarbonylmethyl, carboxymethyl, --CO.sub.2 R.sup.x, --CH.sub.2 OR.sup.x or --OR.sup.x,where R.sup.x, in each instance, is independently one of hydrogen, alkyl or cycloalkyl wherein said alkyl or cycloalkyl groups may optionally have one or more unsaturations;R.sup.6 is hydrogen, alkyl, aralkyl, aryl, cyano(C.sub.2-10)alkyl, hydroxy(C.sub.2-10)alkyl, alkoxy(C.sub.2-10)alkyl, mono- and di-alkylamino(C.sub.2-10)alkyl, or carboxyalkyl;R.sup.7 is hydrogen, C.sub.1-4 alkyl, or C.sub.2-4 alkenyl;R.sup.8 is hydrogen, alkyl, alkenyl, aralkyl, aryl, hydroxyalkyl, aminoalkyl, monoalkylamino (C.sub.2-10)alkyl, dialkylamino(C.sub.2-10)alkyl or carboxyalkyl;R.sup.12, R.sup.13, R.sup.14 and R.sup.15 are independently hydrogen, alkyl, aralkyl, aryl, hydroxyalkyl, aminoalkyl, monoalkylaminoalkyl, dialkylaminoalkyl or carboxyalkyl;or R.sup.12 and R.sup.13 are taken together to form --(CH.sub.2).sub.y --, where y is 2 to 5, while R.sup.14 and R.sup.15 are defined as above;or R.sup.14 and R.sup.15 are taken together to form --(CH.sub.2).sub.q --, where q is 2 to 5, while R.sup.12 and R.sup.13 are defined as above;or R.sup.12 and R.sup.14 are taken together to form --(CH.sub.2).sub.r --, where r is 0 (a bond) or 1 to 4, while R.sup.13 and R.sup.15 are defined as above;X is oxygen or NR.sup.9,where R.sup.9 is hydrogen, alkyl, cycloalkyl or aryl, wherein said alkyl, cycloalkyl or aryl can be optionally substituted with amino, monoalkylamino, dialkylamino, alkoxy, hydroxy, carboxy, alkoxycarbonyl, aryloxycarbonyl, aralkoxycarbonyl, aryl, heteroaryl, acylamino, cyano or trifluoromethyl;R.sup.a, R.sup.b and R.sup.c are independently hydrogen, alkyl, hydroxy, alkoxy, aryloxy, aralkoxy, alkoxycarbonyloxy, cyano or --CO.sub.2 R.sup.w, where ##STR137##where R.sup.d and R.sup.e are independently hydrogen, C.sub.1-6 alkyl, C.sub.2-6 alkenyl or phenyl, R.sup.f is hydrogen, C.sub.1-6 alkyl, C.sub.2-6 alkenyl or phenyl, R.sup.g is hydrogen, C.sub.1-6 alkyl, C.sub.2-6 alkenyl or phenyl, and R.sup.h is aralkyl or C.sub.1-6 alkyl;n is from zero to 8; andm is from zero to 6.