Patent ID: 6586423
Filing Date: 2003-07-01
Classification: A61P,C07D

Abstract:
A compound of Formula I or a pharmaceutically acceptable salt or stereoisomer thereof, whereinY is S; Q is O or absent; R1 is: 1) Or(C1-C6)perfluoroalkyl, 2) OH, 3) CN, 4) halogen, 5) (C&boxH;O)rOs(C1-C10)alkyl, 6) (C&boxH;O)rOs(C2-C8)cycloalkyl, 7) (C&boxH;O)rOs(C2-C10)alkenyl, 8) (C&boxH;O)rOs(C2-C10)alkynyl, 9) (C&boxH;O)rOsaryl, 10) (C&boxH;O)rOsheterocyclyl, or 11) NRaRb, wherein r and s are independently 0 or 1, and said alkyl, cycloalkyl, alkenyl, alkynyl, aryl, and heterocyclyl is optionally substituted with one or more substituents selected from R7; R2 is R1 or H; R4 is H or (C1-C6)alkyl; R5 is: 1) H, 2) SO2Rc, 3) (C&boxH;O)rRc, wherein r is 0 or 1, or 4) CO2Rc; R7 is: 1) Or(C&boxH;O)sNRaRb, 2) (C&boxH;O)rOsaryl, 3) (C&boxH;O)rOs-heterocyclyl, 4) halogen, 5) OH, 6) oxo, 7) O(C1-C3)perfluoroalkyl, 8) (C1-C3)perfluoroalkyl, 9) (C&boxH;O)rOs(C1-C10)alkyl, 10) CHO, 11) C2H, 12) CN, or 13) (C3-C8)cycloalkyl, wherein r and s are independently 0 or 1, and said aryl, heterocyclyl and cycloalkyl are optionally substituted with one or more substituents selected from Rd; Ra and Rb are independently: 1) H, 2) (C&boxH;O)r( C1-C10)alkyl, 3) (C&boxH;O)r(C3-C6)cycloalkyl, 4) S(O)2Rc, 5) (C&boxH;O)rheterocyclyl, 6) (C&boxH;O)raryl, or 7) CO2Rc, wherein r is 0 or 1 and said alkyl, cycloalkyl, heterocyclyl, and aryl optionally substituted with one or more substituents selected from Rd, or Ra and Rb are taken together with the nitrogen to which they are attached to form a monocyclic or bicyclic heterocycle with 5-7 members in each ring and optionally containing, in addition to the nitrogen, one or two additional heteroatoms selected from N, O and S, said monocyclic or bicyclic heterocycle optionally substituted with one or more substituents selected from Rd; Rc is (C1-C6)alkyl, (C3-C6)cycloalkyl, aryl, or heterocyclyl; Rd is selected from: 1) (C&boxH;O)rOs(C1-C10)alkyl, wherein r and s are independently 0 or 1, optionally substituted with up to three substituents selected from OH, (C1-C6)alkoxy, halogen, CN, oxo, N(Re)2 and S(O)2Rc, 2) Or(C1-C3)perfluoroalkyl, 3) (C0-C6)alkylene-S(O)mRc, wherein m is 0, 1, or 2, 4) oxo, 5) OH, 6) halo, 7) CN, 8) (C3-C6)cycloalkyl, optionally substituted with up to three substituents selected from OH, (C1-C6)alkoxy, halogen, CN, oxo, N(Re)2, and S(O)2Rc, 9) (C0-C6)alkylene-aryl), optionally substituted with up to three substituents selected from Re, 10) (C0-C6)alkylene-heterocyclyl, optionally substituted with up to three substituents selected from Re, 11) (C0-C6)alkylene-N(Re)2, 12) C(O)Rc, 13) CO2Rc, 14) C(O)H, and 15) CO2H; and Re is H, (C1-C6)alkyl, aryl, heterocyclyl, (C3-C6)cycloalkyl or S(O)2Rc; and as used herein, the term â€œheterocycleâ€  or â€œheterocyclylâ€  is a 5- to 10-membered aromatic or nonaromatic, monocyclic or bicyclic, heterocycle, containing from 1 to 4 heteroatoms selected from the group consisting of O, N and S.