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35 条记录 (耗时 0.036 秒)

    Selective s1p1/edg1 receptor agonists
    3.
    发明申请
    Selective s1p1/edg1 receptor agonists 审中-公开
    选择性s1p1 / edg1受体激动剂

    公开(公告)号：US20050070506A1

    公开(公告)日：2005-03-31

    申请号：US10501176

    申请日：2003-01-14

    申请人： George Doherty ,  Michael Forrest ,  Richard Hajdu ,  Jeffrey Hale ,  Li Zhen ,  Susanne Mandala ,  Sander Mills ,  Hugh Rosen ,  Edward Scolnick

    发明人： George Doherty ,  Michael Forrest ,  Richard Hajdu ,  Jeffrey Hale ,  Li Zhen ,  Susanne Mandala ,  Sander Mills ,  Hugh Rosen ,  Edward Scolnick

    IPC分类号： A61K31/00 ,  A61K31/66 ,  G01N33/566

    CPC分类号： A61K31/66 ,  A61K31/00 ,  G01N33/566 ,  G01N2500/04

    摘要： The present invention encompasses a method of treating an immunoregulatory abnormality in a mammalian patient in need of such treatment comprising administering to said patient a compound which is an agonist of the S1P1/Edg1 receptor in an amount effective for treating said immunoregulatory abnormality, wherein said compound possesses a selectivity for the S1P1/Edg1 receptor over the S1PR3/Edg3 receptor, said compound administered in an amount effective for treating said immunoregulatory abnormality. Pharmaceutical compositions are included. The invention also encompasses a method of identifying candidate compounds that are agonists of the S1P1/Edg1 receptor and which possesses a selectivity for the S1P1/Edg1 receptor over the S1PR3/Edg3 receptor. The invention further encompasses a method of treating a respiratory disease or condition in a mammalian patient in need of such treatment comprising administering to said patient a compound which is an agonist of the S1P1/Edg1 receptor in an amount effective for treating said respiratory disease or condition, wherein said compound possesses a selectivity for the S1P1/Edg1 receptor over the S1PR3/Edg3 receptor.

    摘要翻译： 本发明包括在需要这种治疗的哺乳动物患者中治疗免疫调节异常的方法，包括以有效治疗所述免疫调节异常的量向所述患者施用作为S1P1 / Edg1受体激动剂的化合物，其中所述化合物 对S1P1 / Edg1受体具有S1PR3 / Edg1受体的选择性，所述化合物以有效治疗所述免疫调节异常的量给药。 包括药物组合物。 本发明还包括鉴定作为S1P1 / Edg1受体的激动剂的候选化合物的方法，并且其具有S1P1 / Edg1受体超过S1PR3 / Edg3受体的选择性。 本发明还包括治疗需要这种治疗的哺乳动物患者的呼吸系统疾病或病症的方法，包括向所述患者施用有效治疗所述呼吸系统疾病或病症的S1P1 / Edg1受体激动剂的化合物 其中所述化合物对S1P1 / Edg1受体具有超过S1PR3 / Edg3受体的选择性。

    2,6-Disubstituted piperiddines as modulators
    10.
    发明申请
    2,6-Disubstituted piperiddines as modulators 失效
    2,6-二取代的哌啶作为调节剂

    公开(公告)号：US20070179158A1

    公开(公告)日：2007-08-02

    申请号：US10586765

    申请日：2005-01-14

    申请人： Lihu Yang ,  Sander Mills ,  Changyou Zhou ,  Stephen Goble ,  Alexander Pasternak

    发明人： Lihu Yang ,  Sander Mills ,  Changyou Zhou ,  Stephen Goble ,  Alexander Pasternak

    IPC分类号： A61K31/506 ,  A61K31/4745 ,  A61K31/46 ,  C07D471/02

    CPC分类号： C07D519/00 ,  C07D451/02 ,  C07D451/04 ,  C07D451/06

    摘要： The present invention is further directed to compounds of formula (I): wherein R1, R2, R3, R4, R5, R6, R7, R8, R9, R10, R16, R17, R18, R19, R20, R21 and R22 are as defined herein) which are modulators of chemokine receptor activity and are useful in the prevention or treatment of certain inflammatory and immunoregulatory disorders and diseases, allergic diseases, atopic conditions including allergic rhinitis, dermatitis, conjunctivitis, and asthma, as well as autoimmune pathologies such as rheumatoid arthritis and atherosclerosis. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which chemokine receptors are involved.

    摘要翻译： 本发明还涉及式（I）的化合物：其中R 1，R 2，R 3，R 4， R 5，R 6，R 7，R 8，R 9，R 9， R 10，R 16，R 17，R 18，R 19，R 16， R 20，R 21，R 22和R 22如本文所定义），其是趋化因子受体活性的调节剂，并且可用于 预防或治疗某些炎性和免疫调节性疾病和疾病，过敏性疾病，特应性病症，包括过敏性鼻炎，皮炎，结膜炎和哮喘，以及自身免疫病态如类风湿性关节炎和动脉粥样硬化。 本发明还涉及包含这些化合物的药物组合物以及这些化合物和组合物在预防或治疗涉及趋化因子受体的疾病中的用途。