利索-全球专利检索

  1. 登录
  2. 注册

搜索结果

26 条记录 (耗时 0.047 秒)

    Substituted tricyclic acid derivatives as S1P1 receptor agonists useful in the treatment of autoimmune and inflammatory disorders
    3.
    发明授权
    Substituted tricyclic acid derivatives as S1P1 receptor agonists useful in the treatment of autoimmune and inflammatory disorders 有权
    取代的三环酸衍生物作为可用于治疗自身免疫性和炎症性疾病的S1P1受体激动剂

    公开(公告)号：US08415484B2

    公开(公告)日：2013-04-09

    申请号：US13060477

    申请日：2009-08-26

    申请人： Robert M. Jones ,  Daniel J. Buzard ,  Andrew M. Kawasaki ,  Sun Hee Kim ,  Lars Thoresen ,  Juerg Lehmann ,  Xiuwen Zhu

    发明人： Robert M. Jones ,  Daniel J. Buzard ,  Andrew M. Kawasaki ,  Sun Hee Kim ,  Lars Thoresen ,  Juerg Lehmann ,  Xiuwen Zhu

    IPC分类号： C07D403/02 ,  C07D487/00 ,  C07D471/14 ,  C07D487/12 ,  C07D401/00 ,  C07D403/14 ,  A61K31/44 ,  A61K31/415 ,  A61K31/40

    CPC分类号： C07D487/04 ,  C07D471/04

    摘要： The present invention relates to certain substituted tricyclic acid derivatives of Formula (I) and pharmaceutically acceptable salts thereof, which exhibit useful pharmacological properties, for example, as agonists of the S1P1 receptor. Also provided by the present invention are pharmaceutical compositions containing compounds of the invention, and methods of using the compounds and compositions of the invention in the treatment of S1P1-associated disorders, for example, psoriasis, rheumatoid arthritis, Crohn's disease, transplant rejection, multiple sclerosis, systemic lupus erythematosus, ulcerative colitis, type I diabetes, acne, myocardial ischemia-reperfusion injury, hypertensive nephropathy, glomerulosclerosis, gastritis, polymyositis, thyroiditis, vitiligo, hepatitis, biliary cirrhosis, microbial infections and associated diseases, viral infections and associated diseases, diseases and disorders mediated by lymphocytes, auto immune diseases, inflammatory diseases, and cancer.

    摘要翻译： 本发明涉及某些取代的式（I）的三环酸衍生物及其药学上可接受的盐，其表现出有用的药理学性质，例如作为S1P1受体的激动剂。 本发明还提供了含有本发明化合物的药物组合物，以及使用本发明化合物和组合物治疗S1P1相关病症的方法，例如牛皮癣，类风湿性关节炎，克罗恩病，移植排斥反应，多发性 硬化症，系统性红斑狼疮，溃疡性结肠炎，I型糖尿病，痤疮，心肌缺血再灌注损伤，高血压肾病，肾小球硬化，胃炎，多发性肌炎，甲状腺炎，白癜风，肝炎，胆汁性肝硬化，微生物感染和相关疾病，病毒感染和相关疾病 ，由淋巴细胞介导的疾病和病症，自身免疫疾病，炎性疾病和癌症。

    PROCESSES FOR THE PREPARATION OF S1P1 RECEPTOR MODULATORS AND CRYSTALLINE FORMS THEREOF
    8.
    发明申请
    PROCESSES FOR THE PREPARATION OF S1P1 RECEPTOR MODULATORS AND CRYSTALLINE FORMS THEREOF 有权
    制备S1P1受体调节剂的方法及其结晶形式

    公开(公告)号：US20120329848A1

    公开(公告)日：2012-12-27

    申请号：US13581846

    申请日：2011-03-02

    申请人： Robert M. Jones ,  Daniel J. Buzard ,  Tawfik Gharbaoui ,  Benjamin R. Johnson ,  Michelle Kasem ,  Thomas O. Schrader ,  Scott Stirn

    发明人： Robert M. Jones ,  Daniel J. Buzard ,  Tawfik Gharbaoui ,  Benjamin R. Johnson ,  Michelle Kasem ,  Thomas O. Schrader ,  Scott Stirn

    IPC分类号： C07D487/04 ,  C07C41/01 ,  A61P37/00 ,  A61P9/10 ,  A61P3/10 ,  A61P17/10 ,  A61P1/16 ,  A61P17/06 ,  A61K31/407 ,  A61P1/04

    CPC分类号： C07D487/04

    摘要： The present invention relates to salts, processes, and process intermediates useful in the preparation of (R)-2-(9-chloro-7-(4-isopropoxy-3-(trifluoromethyl)benzyloxy)-2,3-dihydro-1H-pyrrolo[1,2-a]indol-1-yl)acetic acid of Formula (Ia), salts, and crystalline forms thereof. The compound (R)-2-(9-chloro-7-(4-isopropoxy-3-(trifluoromethyl)benzyloxy)-2,3-dihydro-1H-pyrrolo[1,2-a]indol-1-yl)acetic acid has been identified as an S1P1 receptor modulator that is useful in the treatment of S1P1 receptor-associated disorders, for example, diseases and disorders mediated by lymphocytes, transplant rejection, autoimmune diseases and disorders, inflammatory diseases and disorders (e.g., acute and chronic inflammatory conditions), cancer, and conditions eases characterized by an underlying defect in vascular integrity or that are associated with angiogenesis such as may be pathologic (e.g., as may occur in inflammation, tumor development, and atherosclerosis).

    摘要翻译： 本发明涉及可用于制备（R）-2-（9-氯-7-（4-异丙氧基-3-（三氟甲基）苄氧基）-2,3-二氢-1H- - 吡咯并[1,2-a]吲哚-1-基）乙酸，其盐和结晶形式。 化合物（R）-2-（9-氯-7-（4-异丙氧基-3-（三氟甲基）苄氧基）-2,3-二氢-1H-吡咯并[1,2-a]吲哚-1-基） 乙酸被鉴定为可用于治疗S1P1受体相关疾病的S1P1受体调节剂，例如由淋巴细胞介导的疾病和病症，移植排斥反应，自身免疫性疾病和病症，炎性疾病和病症（例如急性和 慢性炎性病症），癌症和病症特征在于血管完整性的潜在缺陷或与血管发生相关的疾病，例如可能是病理性的（例如，可能发生在炎症，肿瘤发展和动脉粥样硬化中）。

    Processes for the preparation of S1P1 receptor modulators and crystalline forms thereof
    9.
    发明授权
    Processes for the preparation of S1P1 receptor modulators and crystalline forms thereof 有权
    制备S1P1受体调节剂及其结晶形式的方法

    公开(公告)号：US09085581B2

    公开(公告)日：2015-07-21

    申请号：US13581846

    申请日：2011-03-02

    申请人： Robert M. Jones ,  Daniel J. Buzard ,  Tawfik Gharbaoui ,  Benjamin R. Johnson ,  Michelle Kasem ,  Thomas O. Schrader ,  Scott Stirn

    发明人： Robert M. Jones ,  Daniel J. Buzard ,  Tawfik Gharbaoui ,  Benjamin R. Johnson ,  Michelle Kasem ,  Thomas O. Schrader ,  Scott Stirn

    IPC分类号： C07D487/16 ,  A61K31/403 ,  C07D487/04

    CPC分类号： C07D487/04

    摘要： The present invention relates to salts, processes, and process intermediates useful in the preparation of (R)-2-(9-chloro -7-(4-isopropoxy-3-(trifluoromethyl)benzyloxy)-2,3-dihydro-1H-pyrrolo[1,2-a]indol-1-yl)acetic acid of Formula (Ia), salts, and crystalline forms thereof. The compound (R)-2-(9-chloro-7-(4-isopropoxy-3-(trifluoromethyl)benzyloxy)-2,3-dihydro-1H-pyrrolo[1,2-a]indol-1-yl)acetic acid has been identified as an S1P1 receptor modulator that is useful in the treatment of S1P1 receptor-associated disorders, for example, diseases and disorders mediated by lymphocytes, transplant rejection, autoimmune diseases and disorders, inflammatory diseases and disorders (e.g., acute and chronic inflammatory conditions), cancer, and conditions characterized by an underlying defect in vascular integrity or that are associated with angiogenesis such as may be pathologic (e.g., as may occur in inflammation, tumor development, and atherosclerosis).

    摘要翻译： 本发明涉及可用于制备（R）-2-（9-氯-7-（4-异丙氧基-3-（三氟甲基）苄氧基）-2,3-二氢-1H- - 吡咯并[1,2-a]吲哚-1-基）乙酸，其盐和结晶形式。 化合物（R）-2-（9-氯-7-（4-异丙氧基-3-（三氟甲基）苄氧基）-2,3-二氢-1H-吡咯并[1,2-a]吲哚-1-基） 乙酸被鉴定为可用于治疗S1P1受体相关疾病的S1P1受体调节剂，例如由淋巴细胞介导的疾病和病症，移植排斥反应，自身免疫性疾病和病症，炎性疾病和病症（例如急性和 慢性炎性病症），癌症和特征在于血管完整性的潜在缺陷或与血管发生相关的病症，例如可能是病理性的（例如，可能发生在炎症，肿瘤发展和动脉粥样硬化中）。