发明公开
- 专利标题: PYRIMIDINE COMPOUNDS
- 专利标题(中): 称为白细胞介素-12(IL-12)抑制剂的嘧啶化合物
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申请号: EP02804468.3申请日: 2002-11-27
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公开(公告)号: EP1458687A2公开(公告)日: 2004-09-22
- 发明人: ONO, Mitsunori , SUN, Lijun , PRZEWLOKA, Teresa , ZHANG, Shijie , KOSTIK, Elena , YING, Weiwen , WADA, Yumiko , KOYA, Keizo , WU, Yaming , ZHOU, Dan , TATSUTA, Noriaki
- 申请人: Synta Pharmaceuticals Corporation
- 申请人地址: 45 Hartwell Avenue Lexington, MA 02421 US
- 专利权人: Synta Pharmaceuticals Corporation
- 当前专利权人: Synta Pharmaceuticals Corporation
- 当前专利权人地址: 45 Hartwell Avenue Lexington, MA 02421 US
- 代理机构: Schnappauf, Georg Dr.
- 优先权: US742 20011130; US192347 20020710
- 国际公布: WO2003047516 20030612
- 主分类号: C07D239/32
- IPC分类号: C07D239/32 ; C07D239/38 ; C07D239/47 ; C07D239/50 ; C07D239/52 ; C07D239/56 ; C07D279/06 ; A61K31/506 ; A61K31/295 ; A61P29/00
摘要:
This invention features pyrimidine compounds of formula (I): R1 is formula (II), aryl, or heteroaryl; each of R2 and R4, independently, is Rc, halogen, nitro, cyano, isothionitro, SR?c, or ORc¿; or R¿2? and R4, taken together, is carbonyl; R3 is R?c¿, alkenyl, alkynyl, ORc, OC(O)Rc, S02R?c, S(O)Rc, S(0¿2)NR?cRd, SRc, NRcRd, NRcCORd, NRcC(O)ORd, NRcC(O)NRcRd, NRcS0¿2Rd, CORc, C(O)ORc, or C(O)NRcRd; R5 is H or alkyl; n is 0, 1, 2, 3, 4, 5, or 6; X is O, S, S(O), S(02), or NRc; Y is a covalent bond, CH¿2?, C(O), C=N-R?c¿, C=N-ORc, C=N-SR¿c?, O, S, S(O), S(02), or NR?c¿; Z is N or CH; one of U and V is N, and the other is CRc; and W is O, S, S(O), S(0¿2), NR?c, or NC(O)Rc; in which each of R?a and Rb¿, independently, is H, alkyl, aryl, heteroaryl; and each of R?c and Rd¿, independently, is H, alkyl, aryl, heteroaryl, cyclyl, heterocyclyl, or alkylcarbonyl. The compounds are useful for treating IL-12 overproduction related diseases (e.g., rheumatoid arthritis, sepsis, Crohn's disease, multiple sclerosis, psoriasis, or insulin-dependent diabetes mellitus).
公开/授权文献
- EP1458687B1 PYRIMIDINE COMPOUNDS AS INTERLEUKIN-12 (IL-12) INHIBITORS 公开/授权日:2012-01-11
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