- 专利标题: 2,3-diaryl-pyrazolo[1,5-b]pyridazines derivatives, their preparation and their use as cyclooxygenase, 2 (COX-2) inhibitors
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申请号: US10974893申请日: 2004-10-27
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公开(公告)号: US20050113377A1公开(公告)日: 2005-05-26
- 发明人: Paul Beswick , Charanjit Bountra , Ian Campbell , Neil Mathews , Alan Naylor
- 申请人: Paul Beswick , Charanjit Bountra , Ian Campbell , Neil Mathews , Alan Naylor
- 优先权: GB9718792.6 19970905; GB9727116.7 19971223
- 主分类号: A61K31/00
- IPC分类号: A61K31/00 ; A61K31/50 ; A61K31/5025 ; A61P1/04 ; A61P3/10 ; A61P7/06 ; A61P9/00 ; A61P11/00 ; A61P11/06 ; A61P17/00 ; A61P17/02 ; A61P19/02 ; A61P19/06 ; A61P25/06 ; A61P25/16 ; A61P25/28 ; A61P27/02 ; A61P27/16 ; A61P29/00 ; A61P35/00 ; C07D487/04 ; A61K31/503
摘要:
The invention provides a pharmaceutical composition comprising a compound of formula (I) or a pharmaceutically acceptable salt, solvate, ester or salt or solvate of such ester, of a compound of formula (I) in which: R0 is halogen, C1-6alkyl, C1-6alkoxy, C1-6alkoxy substituted by one or more fluorine atoms, or O(CH2)nNR4R5; R1 and R2 are independently selected from H, C1-6alkyl, C1-6alkyl substituted by one or more fluorine atoms, C1-6alkoxy, C1-6hydroxyalkyl, SC1-6alkyl, C(O)H, C(O)C1-6alkyl, C1-6alkylsulphonyl, C1-6alkoxy substituted by one or more fluorine atoms, O(CH2)nCO2C1-6alkyl, O(CH2)nSC1-6alkyl, (CH2)nNR4R5, (CH2)nSC1-6alkyl or C(O)NR4R5; with the proviso that when R0 is at the 4-position and is halogen, at least one of R1 and R2 is C1-6alkylsulphonyl, C1-6alkoxy substituted by one or more fluorine atoms, O(CH2)nCO2C1-6alkyl, O(CH2)nSC1-6alkyl, (CH2)nNR4R5 or (CH2)nSC1-6alkyl, C(O)NR4R5; R3 is C1-6alkyl or NH2; R4 and R5 are independently selected from H and C1-6alkyl or, together with the nitrogen atom to which they are attached, form a 4-8 membered saturated ring; and n is 1-4; and an inhibitor of the release, or action, of tumour necrosis factor α.