发明公开
EP1068212A1 THIAZOLO 4,5-d]PYRIMIDINES AND PYRIDINES AS CORTICOTROPIN RELEASING FACTOR (CRF) ANTAGONISTS
审中-公开
THIAZOLO¬4,5-D嘧啶和吡啶因子促肾上腺皮质激素释放因子（CRF）拮抗剂
- 专利标题： THIAZOLO 4,5-d]PYRIMIDINES AND PYRIDINES AS CORTICOTROPIN RELEASING FACTOR (CRF) ANTAGONISTS
- 专利标题（中）： THIAZOLO¬4,5-D嘧啶和吡啶因子促肾上腺皮质激素释放因子（CRF）拮抗剂
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申请号： EP99914247.4申请日： 1999-03-29
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公开(公告)号： EP1068212A1公开(公告)日： 2001-01-17
- 发明人: BECK, James, Peter
- 申请人： Du Pont Pharmaceuticals Company
- 申请人地址： 974 Centre Road, WR-1st 18 Wilmington, DE 19807 US
- 专利权人： Du Pont Pharmaceuticals Company
- 当前专利权人： Du Pont Pharmaceuticals Company
- 当前专利权人地址： 974 Centre Road, WR-1st 18 Wilmington, DE 19807 US
- 代理机构： Jones, Alan John
- 优先权： US80537P 19980403
- 国际公布： WO9951608 19991014
- 主分类号： C07D513/04
- IPC分类号： C07D513/04 ; A61K31/505 ; A61K31/44 ; A61K31/425
摘要：
The present invention describes novel thiazolo[4,5-d]pyrimidines of formula (I), or a pharmaceutically acceptable salt thereof, wherein X is CR4 or N; Y is selected from the group: S, O and NR5; R1 is selected from the group: H, C¿1-4? alkyl, C2-4 alkenyl, C2-4 alkynyl, Cl, F, Br, I, -CN, C1-5 haloalkyl, -NR?6R7, -NR6COR7, -OR8¿, -SH, and -S(O)¿nR?9; R2 is selected from the group: -CR?10R11R12, -NR10aR11a, -NHCR10R11R12, -OCR10R11R12¿, and phenyl, wherein the phenyl is substituted with 0-4 Ra; R3 is selected from the group: phenyl, pyridyl, pyrimidyl, napthyl, triazinyl, furanyl, quinolinyl, isoquinolinyl, thienyl, thiazolyl, pyrrolyl, oxazolyl, benzofuranyl, benzothienyl, benzothiazolyl, isoxazolyl, and pyrazolyl, and is substituted with 1 to 4 Rb groups; R4 is selected from the group: H, C¿1-4? alkyl, and C1-4 haloalkyl, halogen, NH2, NH(C1-4 alkyl), NH(C1-4 alkyl)2, CN, OR?8; and R5¿ is -CO(C¿1-4? alkyl) or -CO2(C1-4 alkyl), which are useful as CRF antagonists.
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