公开(公告)号：US20060040957A1

公开(公告)日：2006-02-23

申请号：US10071032

申请日：2002-02-08

Applicant: Richard Dyer ,  William Harter ,  James Hicks ,  Adam Johnson ,  Jie Li ,  William Roark ,  Kevon Shuler

Inventor： Richard Dyer ,  William Harter ,  James Hicks ,  Adam Johnson ,  Jie Li ,  William Roark ,  Kevon Shuler

IPC: A61K31/519 ,  C07D498/04

CPC classification number: C07D487/04 ,  C07D513/04

Abstract: Selective MMP-13 inhibitors are bicyclic pyrimidines of the Formula I or a pharmaceutically acceptable salt thereof, wherein R1 is hydrogen or alkyl; R2, R3, and R4 include hydrogen, halo, alkyl, C≡C(CH2)m aryl, CO2 alkyl, CO2(CH2)m aryl, COHN alkyl, and CONH(CH2)m aryl; and X is O, S, SO, SO2, CH2, C═O, CHOH, NH, or NR5. A compound of Formula I, or a pharmaceutically acceptable salt thereof, is useful for treating cancer or arthritis.

Abstract translation: 选择性MMP-13抑制剂是式I的二环嘧啶或其药学上可接受的盐，其中R 1是氢或烷基; R 2，R 3和R 4包括氢，卤素，烷基，C≡C（CH 2）2， ）芳基，CO 2烷基，CO 2（CH 2 CH 2）m， 芳基，COHN烷基和CONH（CH 2 CH 2）m芳基; X是O，S，SO，SO 2，CH 2，C-O，CHOH，NH或NR 5。 式I化合物或其药学上可接受的盐可用于治疗癌症或关节炎。