Patent ID: 6358951
Filing Date: 2002-03-19
Classification: A61P,C07D

Abstract:
A compound of the Formula I: or a stereoisomeric mixture thereof, diastereomerically enriched, diastereomerically pure, enantiomerically enriched or enantiomerically pure isomer thereof, or a prodrug of such compound, mixture or isomer thereof, or a pharmaceutically acceptable salt of the compound, mixture, isomer or prodrug,wherein:HET is a heterocyclic moiety selected from the group consisting of f is 0 or 1; n and w are each 1; Y2 is oxygen; R1 is (C1-C10)alkyl, â€”(CH2)tâ€”A1, or â€”(CH2)qâ€”(C3-C7)cycloalkyl; where the alkyl and cycloalkyl groups in the definition of R1 are optionally substituted with (C1-C4)alkyl, hydroxy, (C1-C4)alkoxy, carboxyl, â€”CONH2, â€”S(O)m(C1-C6)alkyl, â€”CO2(C1-C4)alkyl ester, 1H-tetrazol-5-yl or 1, 2 or 3 fluoro groups; q is 0, 1, 2, 3 or 4; t is 0, 1, 2 or 3; R2 is hydrogen, (C1-C8)alkyl, â€”(C0-C3)alkyl-(C3-C8)cycloalkyl, or phenyl; where the (C1-C8)alkyl group in the definition of R2 is optionally substituted with hydroxy, CF3, or 1, 2 or 3 independently selected halogens; R3 is phenyl-CH2â€”Oâ€”CH2â€”, phenyl-CH2â€”CH2â€”CH2â€”, naphthyl-CH2, 3-indolyl-methyl; said phenyl being optionally substituted with up to three fluoro or chloro; R4 is hydrogen or methyl; X4 is hydrogen; R6 is â€”(CRaRb)aâ€”Eâ€”(CRaRb)bâ€”, where the â€”(CRaRb)aâ€” group is attached to the carbonyl carbon of the amide group of the compound of formula I and the â€”(CRaRb)b group is attached to the terminal nitrogen atom of the compound of formula I; E is â€”CH&boxH;CHâ€” or an aromatic moiety selected from â€ƒsaid aromatic moiety in the definition of E optionally substituted with up to three halo, hydroxy, â€”N(Rc)(Rc), (C1-C6)alkyl or (C1-C6)alkoxy; Ra and Rb are, for each occurrence, independently hydrogen or methyl; Rc, for each occurrence, is independently hydrogen or (C1-C6)alkyl; a and b are independently 0, 1, 2 or 3; R7 and R8 are each independently hydrogen or (C1-C3) alkyl optionally substituted with up to two hydroxyl groups; A1 is phenyl, pyridyl or thiazolyl; A1 in the definition of R1 is optionally substituted with up to three substituents, each substituent independently selected from the group consisting of F, Cl, OCF3, OCF2H, CF3, CH3, or OCH3; m for each occurrence is independently 0, 1 or 2.