Patent ID: 6642225
Filing Date: 2003-11-04
Classification: A61K,A61P,C07D

Abstract:
A compound of the formula I wherein R is carboxy, esterified carboxy or amidated carboxy;R1 and R3 are independently lower alkyl, (hydroxy, lower alkoxy, amino, acylamino, mono- or di-lower alkylamino or mercapto)-lower alkyl, lower alkyl-(thio, sulfinyl or sulfonyl)-lower alkyl, cycloalkyl, aryl, biaryl, (cycloalkyl, aryl or biaryl)-lower alkyl, or (carboxy, esterified carboxy or amidated carboxy)-lower alkyl; R2 is hydrogen, lower alkyl, cycloalkyl, aryl, biaryl, arylaminocarbonyl, or aryl-(oxy, thio or amino); n is 1 or 2; Y is lower-alkylene or lower alkenylene; or a pharmaceutically acceptable salt thereof; and wherein in the above definitions, aryl represents carbocylic or heterocyclic aryl; heterocyclic aryl represents monocyclic or bicyclic heterocyclic aryl; monocyclic heterocyclic aryl represents optionally substituted thiazolyl, thienyl, furanyl or pyridyl; optionally substituted thiazolyl represents thiazolyl or thiazolyl substituted by lower alkyl; optionally substituted thienyl represents thienyl or thienyl substituted by lower alkyl; optionally substituted furanyl represents furanyl or furanyl substituted by lower alkyl; optionally substituted pyridyl represents pyridyl or pyridyl substituted by lower alkyl, halogen or cyano; bicyclic heterocyclic aryl represents optionally substituted quinolinyl, isoquinolinyl, indolyl or benzothiazolyl; optionally substituted quinolinyl represents quinolinyl or quinolinyl substituted by hydroxy, lower alkyl, lower alkoxy or halogen; optionally substituted isoquinolinyl represents isoquinolinyl or isoquinolinyl substituted by hydroxy, lower alkyl, lower alkoxy or halogen; optionally substituted indolyl represents indolyl, indolyl substituted on carbon by hydroxy, lower alkyl, lower alkoxy or halogen, or indolyl substituted on nitrogen by lower alkyl or aryl-lower alkyl; optionally substituted benzothiazolyl represents benzothiazolyl or benzothiazolyl substituted by hydroxy, lower alkyl, lower alkoxy or halogen; biaryl represents phenyl substituted by carbocyclic or heterocyclic aryl; esterified carboxy represents carboxy esterified in form of a pharmaceutically acceptable ester selected from a lower alkyl ester, a cycloalkyl ester, a lower alkenyl ester, a benzyl ester and a mono- or di-substituted lower alkyl ester; and a mono- or di-substituted lower alkyl ester represents an &ohgr;-(amino, mono- or di-lower alkylamino, carboxy, lower alkoxycarbonyl)-lower alkyl ester or an &agr;-(lower alkanoyloxy, lower alkoxycarbonyl or di-lower alkylaminocarbonyl)-lower alkyl ester; or amidated carboxy represents carboxy derivatized in form of a pharmaceutically acceptable amide selected from the unsubstituted amide, an N-mono-lower alkyl amide, an N,N-di-lower alkylamide and an amide of a cyclic amine.