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    PROCESSES FOR THE PREPARATION OF S1P1 RECEPTOR MODULATORS AND CRYSTALLINE FORMS THEREOF
    3.
    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
    4.
    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）。