首页> 外国专利> Therapeutically active compounds based on indazole bioisostere replacement of catechol in PDE4 inhibitors

Therapeutically active compounds based on indazole bioisostere replacement of catechol in PDE4 inhibitors

机译:PDE4抑制剂中基于吲唑生物等排取代邻苯二酚的治疗活性化合物

摘要

This application is directed to therapeutically active compositions of matter are useful for treating or preventing inflammatory bowel disease and conditions including joint inflammation, Crohn's disease and inflammatory bowel disease; respiratory diseases such as chronic obstructive pulmonary disease (COPD) including asthma, chronic bronchitis, and pulmonary emphysema; infectious diseases including endotoxic shock and toxic shock syndrome; immune diseases including systemic lupus erythematosis and psoriasis; and other diseases including bone resorption diseases and reperfusion injury; wherein said composition of matter comprises a compound which is an inhibitor of phosphodiesterase isozyme 4 (PDE4) and wherein an indazole is one essential component of said compound's overall chemical structure, and wherein said indazole constitutes a bioisosteric replacement of a catechol component or functional derivative thereof in a known compound having the same said therapeutic activity and the same remaining said components of its overall chemical structure. Included are compounds of Formula (IA) or (IB): embedded image;wherein the variable are defined as set forth in the specification.
机译:本申请涉及用于治疗或预防炎症性肠疾病和病症的治疗活性物质组合物,所述疾病和病症包括关节炎症,克罗恩氏病和炎症性肠疾病。呼吸系统疾病,例如慢性阻塞性肺疾病(COPD),包括哮喘,慢性支气管炎和肺气肿;传染病,包括内毒素休克和中毒性休克综合症;免疫性疾病,包括系统性红斑狼疮和牛皮癣;以及其他疾病,包括骨吸收疾病和再灌注损伤;其中所述物质组合物包含作为磷酸二酯酶同工酶4(PDE4)抑制剂的化合物,并且其中吲唑是所述化合物整体化学结构的一种基本成分,并且其中所述吲唑构成儿茶酚成分或其功能性衍生物的生物立体替代物在已知化合物中具有相同的所述治疗活性并且在其整体化学结构中其余相同的组分。包括式(IA)或(IB)的化合物:<化学类别=“ =” CHM-US-00001“> <图像alt =”嵌入式图像“ file =” US06716978-20040406-C00001.GIF“ he =” 139.45365“ imgContent =“ undefined” imgFormat =“ GIF” wi =“ 153.3735” /> ;其中变量的定义如说明书中所述。

著录项

  • 公开/公告号US6716978B2

    专利类型

  • 公开/公告日2004-04-06

    原文格式PDF

  • 申请/专利权人 PFIZER INC;

    申请/专利号US19990381446

  • 发明设计人 ANTHONY MARFAT;

    申请日1999-09-20

  • 分类号C07D2315/60;

  • 国家 US

  • 入库时间 2022-08-21 23:12:53

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