公开(公告)号：US20070021611A1

公开(公告)日：2007-01-25

申请号：US11353697

申请日：2006-02-14

申请人： Brian McGuinness ,  Stuart Rosenblum ,  Joseph Kozlowski ,  Gopinadhan Anilkumar ,  Seong Kim ,  Neng-Yang Shih ,  Chung-Her Jenh ,  Paul Zavodny ,  Douglas Hobbs ,  Guizhen Dong ,  Yuefei Shao ,  Lisa Zawacki ,  Cangming Yang ,  Carolyn Carroll

发明人： Brian McGuinness ,  Stuart Rosenblum ,  Joseph Kozlowski ,  Gopinadhan Anilkumar ,  Seong Kim ,  Neng-Yang Shih ,  Chung-Her Jenh ,  Paul Zavodny ,  Douglas Hobbs ,  Guizhen Dong ,  Yuefei Shao ,  Lisa Zawacki ,  Cangming Yang ,  Carolyn Carroll

IPC分类号： C07D401/00

CPC分类号： C07D401/12 ,  C07D211/58 ,  C07D401/14 ,  C07D405/14 ,  C07D413/14 ,  C07D417/14

摘要： The present application discloses a compound, or enantiomers, stereoisomers, rotamers, tautomers, racemates or prodrug of said compound, or pharmaceutically acceptable salts, solvates or esters of said compound, or of said prodrug, said compound having the general structure shown in Formula 1: and the pharmaceutically acceptable salts, solvates and esters thereof. Also disclosed is a method of treating chemokine mediated diseases, such as, palliative therapy, curative therapy, prophylactic therapy of certain diseases and conditions such as inflammatory diseases (non-limiting example(s) include, psoriasis), autoimmune diseases (non-limiting example(s) include, rheumatoid arthritis, multiple sclerosis), graft rejection (non-limiting example(s) include, allograft rejection, xenograft rejection), infectious diseases (e.g, tuberculoid leprosy), fixed drug eruptions, cutaneous delayed-type hypersensitivity responses, ophthalmic inflammation, type I diabetes, viral meningitis and tumors using a compound of Formula 1.

摘要翻译： 本申请公开了所述化合物或所述前体药物的所述化合物或其药学上可接受的盐，溶剂合物或酯的化合物或对映异构体，立体异构体，旋转异构体，互变异构体或前药，所述化合物具有式1所示的一般结构 ：及其药学上可接受的盐，溶剂化物和酯。 还公开了治疗趋化因子介导的疾病的方法，例如姑息治疗，疗效治疗，某些疾病和疾病如炎性疾病的预防性治疗（非限制性实例，牛皮癣），自身免疫性疾病（非限制性的 例如，类风湿性关节炎，多发性硬化症），移植排斥反应（非限制性实例包括，同种异体移植排斥反应，异种移植物排斥），感染性疾病（例如结核性麻风病），固定药物爆发，皮肤迟发型超敏反应 应答，眼部炎症，I型糖尿病，病毒性脑膜炎和使用式1的化合物的肿瘤。

公开(公告)号：US20070141603A1

公开(公告)日：2007-06-21

申请号：US11598469

申请日：2006-11-13

申请人： Barbara Dalie ,  Xuedong Fan ,  Daniel Lundell ,  Charles Lunn ,  Jimmy Tan ,  Paul Zavodny

发明人： Barbara Dalie ,  Xuedong Fan ,  Daniel Lundell ,  Charles Lunn ,  Jimmy Tan ,  Paul Zavodny

IPC分类号： C12Q1/68 ,  C07H21/04 ,  C12P21/06 ,  C12N9/64

CPC分类号： C12N9/6489 ,  C12N9/6424 ,  C12Q1/37 ,  C12Y304/24086 ,  G01N2333/525 ,  G01N2333/96486

摘要： The present invention provides isolated human and bovine TNF-α convertases, nucleic acids and; recombinant vectors encoding the same, host cells comprising the nucleic acids and vectors, and methods for making the convertases using the host cells. This invention further provides antibodies and antigen binding fragments thereof which specifically bind to the convertases and are useful for treating medical conditions caused or mediated by TNF-α. Also provided are screening methods for identifying specific inhibitors of mammalian TNF-α convertases, and for identifying nucleic acids encoding such convertases.

摘要翻译： 本发明提供分离的人和牛TNF-α转化酶，核酸和 编码其的重组载体，包含核酸和载体的宿主细胞，以及使用宿主细胞制备转化酶的方法。 本发明进一步提供与转化酶特异性结合的抗体及其抗原结合片段，可用于治疗由TNF-α引起或介导的医学病症。 还提供了用于鉴定哺乳动物TNF-α转化酶的特异性抑制剂的筛选方法，以及用于鉴定编码这种转化酶的核酸。