发明授权
US07906551B2 3-substituted-1,5-diarly-2-alkyl-pyrroles highly selective and orally effective COX-2 inhibitors
有权
3-取代-1,5-二烯-2-烷基吡咯高选择性和口服有效的COX-2抑制剂
- 专利标题: 3-substituted-1,5-diarly-2-alkyl-pyrroles highly selective and orally effective COX-2 inhibitors
- 专利标题(中): 3-取代-1,5-二烯-2-烷基吡咯高选择性和口服有效的COX-2抑制剂
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申请号: US12375650申请日: 2006-08-03
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公开(公告)号: US07906551B2公开(公告)日: 2011-03-15
- 发明人: Andrea Cappelli , Maurizio Anzini , Mariangela Biava , Francesco Makovec , Antonio Giordani , Gianfranco Caselli , Lucio Claudio Rovati
- 申请人: Andrea Cappelli , Maurizio Anzini , Mariangela Biava , Francesco Makovec , Antonio Giordani , Gianfranco Caselli , Lucio Claudio Rovati
- 申请人地址: IT Milan
- 专利权人: Rottapharm S.p.A.
- 当前专利权人: Rottapharm S.p.A.
- 当前专利权人地址: IT Milan
- 代理机构: Sughrue Mion, PLLC
- 国际申请: PCT/EP2006/065011 WO 20060803
- 国际公布: WO2008/014821 WO 20080207
- 主分类号: A61K31/40
- IPC分类号: A61K31/40 ; C07D207/30
摘要:
This invention relates to 3-substituted-1,5-diaryl-2-alkyl-pyrroles of Formula I, pharmaceutical compositions containing them, and to their use for the pharmacological treatment of pain and COX-2 over-activation associated disorders. Compounds of this invention are new pyrrole derivatives bearing in position -3 of the pyrrole ring, several variously functionalized, not aliphatic, side chains which confer to the compounds a relevant COX-2 potency and selectivity along with a remarkable oral efficacy. Phenyl rings in position -1 and -5 are variously substituted, but compounds of particular interest are those substituted in position -5 with 4-methylsulphonyl-phenyl or with 4-aminosulphonyl-phenyl groups.
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