Patent ID: 6277991
Filing Date: 2001-08-21
Classification: A61K,C07D

Abstract:
A compound of formula Ia or Ib: ##STR81##whereinR.sup.1 is C.sub.1-6 -alkyl; or R.sup.1 is phenyl, arylalkyl or thienyl, each of which is optionally substituted with halogen, cyano, nitro, trifluoromethyl, C.sub.1-6 -alkyl, hydroxy, C.sub.1-6 -alkoxy or --NR.sup.6 R.sup.8, wherein R.sup.6 and R.sup.8 are independently hydrogen or C.sub.1-6 -alkyl;R.sup.2 is aminophenyl, C.sub.1-6 -monoalkylaminophenyl, C.sub.1-6 -dialkylaminophenyl, cyanophenyl, C.sub.2-6 -alkylphenyl, naphthyl, anthryl, furanyl, indanyl, benzothienyl, benzofuranyl, coumarinyl, phenyl, phenoxy, benzodioxinyl or cyanodiphenylmethyl, each of which is optionally substituted with halogen, cyano, nitro, trifluoromethyl, C.sub.1-6 -alkyl, hydroxy, C.sub.1-6 -alkoxy or --C(O)R.sup.7, wherein R.sup.7 is --OH, C.sub.1-6 -alkoxy or --NR.sup.12 R.sup.13, wherein R.sup.12 and R.sup.13 are independently hydrogen or C.sub.1-6 -alkyl;R.sup.3 is hydrogen, C.sub.1-6 -alkyl, phenyl, benzyl or acetyl;R.sup.4 is --(CH.sub.2).sub.m --(CHR.sup.9)--(CH.sub.2)p-AR.sup.11, wherein A is --(C.dbd.O)--, m and p are independently 0 to 4, R.sup.9 is hydrogen, C.sub.1-6 -alkyl, phenyl or arylalkyl, and R.sup.11 is an amino acid residue or a 2 to 4 peptidyl residue with a C-terminal group consisting of either --OCH.sub.3 or --NH.sub.2 ;R.sup.5 is hydrogen or C.sub.1-4 -alkyl;z is --CHR.sup.10, wherein R.sup.10 is hydrogen, C.sub.1-6 -alkyl, phenyl, arylalkyl; or z is C.sub.2-8 -alkylene, C.sub.2-8 -alkenylene or C.sub.2-8 -alkynylene; andn is 2;or a pharmaceutically acceptable salt thereof.