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公开(公告)号：US07514409B2
公开(公告)日：2009-04-07
申请号：US10591820
申请日：2005-03-07
申请人： William K. Hagmann , Linus S. Lin , Ping Liu , Richard A. Mumford , Thomas S. Reger , Nicholas D. Smith , Nicholas S. Stock , Jasmine Zunic
发明人： William K. Hagmann , Linus S. Lin , Ping Liu , Richard A. Mumford , Thomas S. Reger , Nicholas D. Smith , Nicholas S. Stock , Jasmine Zunic
IPC分类号： A61K38/05
CPC分类号： C07K5/06026 , C07D401/12 , C07D401/14
摘要： Compounds of Formula I are antagonists of VLA-4, and as such are useful in the inhibition or prevention of cell adhesion and cell-adhesion mediated pathologies. These compounds may be formulated into pharmaceutical compositions and are suitable for use in the treatment of inflammatory bowel disease including ulcerative colitis and Crohn's disease, multiple sclerosis, asthma, and rheumatoid arthritis.
摘要翻译： 式I的化合物是VLA-4的拮抗剂，因此可用于抑制或预防细胞粘附和细胞粘附介导的病症。 这些化合物可以配制成药物组合物，并且适用于治疗包括溃疡性结肠炎和克罗恩病，多发性硬化，哮喘和类风湿性关节炎的炎性肠病。
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公开(公告)号：US20090048308A1
公开(公告)日：2009-02-19
申请号：US11918100
申请日：2006-04-10
IPC分类号： A61K31/4439 , C07D401/12 , A61P35/02 , A61P9/10 , A61P35/00 , A61P11/06 , A61P19/02 , A61P1/00
CPC分类号： C07D401/12
摘要： 4-Thio, 4-sulfinyl and 4-sulfonyl proline derivatives of the present invention are antagonists of the VLA-4 integrin and are useful in the treatment, prevention and suppression of diseases mediated by VLA-4-binding and cell adhesion and activation. Moreover, the compounds of the present invention demonstrate significant receptor occupancy of VLA-4 bearing cells after oral administration and are suitable for once-, twice-, or thrice-a-day oral administration. This invention also relates to compositions containing such compounds and methods of treatment using such compounds.
摘要翻译： 本发明的4-硫代，4-亚磺酰基和4-磺酰基脯氨酸衍生物是VLA-4整联蛋白的拮抗剂，可用于治疗，预防和抑制由VLA-4结合和细胞粘附和活化介导的疾病。 此外，本发明的化合物在口服给药后显示VLA-4携带细胞的显着受体占有率，并且适合于一天一次，两次或每日三次口服给药。 本发明还涉及含有这些化合物的组合物和使用这些化合物的治疗方法。
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