Patent ID: 6342602
Filing Date: 2002-01-29
Classification: A61P,C07C,C07D

Abstract:
A compound of the formula wherein X is NRâ€² where Râ€² is H or alkyl of 1 to 6 carbons;R1 is independently H or alkyl of 1 to 6 carbons; R2 is independently hydrogen, or lower alkyl of 1 to 6 carbons; R3 is independently hydrogen, lower alkyl of 1 to 6 carbons or F; m is an integer having the value of 0-2; o is an integer having the value of 0-4; p is an integer having the value of 0-2; r is an integer having the value 0-2 with the proviso that when Z is O the sum of p and r is at least 1; Y is heteroaryl selected from a group consisting of pyridyl, thienyl, furyl, pyridazinyl, pyrimidinyl, pyrazinyl, thiazolyl, oxazolyl, imidazolyl and pyrazolyl, said heteroaryl groups being optionally substituted with one or two R2 groups; W is a substituent selected from the group consisting of F, Br, Cl, I, C1-6 alkyl, fluoro substituted C1-6 alkyl, NO2, N3, OH, OCH2CH3, OCH2OCH3, C1-10 alkyl, tetrazol, CN, SO2C1-6-alkyl, SO2C1-6-alkyl, SO2C1-6-fluoro substituted alkyl, SO-C1-6 alkyl, CO-C1-6alkyl, COOR8, phenyl, phenyl itself substituted with a W group other than with phenyl or substituted phenyl; L is â€”(C&boxH;Z)â€”NHâ€” or â€”HNâ€”(C&boxH;Z)â€”Z is O or S; A is (CH2)q where q is 0-5, lower branched chain alkyl having 3-6 carbons, cycloalkyl having 3-6 carbons, alkenyl having 2-6 carbons and 1 or 2 double bonds, alkynyl having 2-6 carbons and 1 or 2 triple bonds, and B is COOH or a pharmaceutically acceptable salt thereof, COOR8, CONR9R10, â€”CH2OH, CH2OR11, CH2OCOR11, CHO, CH(OR12)2, CHOR13O, â€”COR7, CR7(OR12)2, CR7OR13O, where R7 is an alkyl, cycloalkyl or alkenyl group containing 1 to 5 carbons, R8 is an alkyl group of 1 to 10 carbons or trimethylsilylalkyl where the alkyl group has 1 to 10 carbons, or a cycloalkyl group of 5 to 10 carbons, or R8 is phenyl or lower alkylphenyl, R9 and R10 independently are hydrogen, an alkyl group of 1 to 10 carbons, or a cycloalkyl group of 5-10 carbons, or phenyl or lower alkylphenyl, R11 is lower alkyl, phenyl or lower alkylphenyl, R12 is lower alkyl, and R13 is divalent alkyl radical of 2-5 carbons.