S1P1 receptor modulator and salt preparation method thereof

The present invention relates to processes and intermediates useful in the preparation of of (R)-2-(7-(4-cyclopentyl-3-(trifluoromethyl)benzyloxy)-1,2,3,4-tetrahydrocyclopenta[b]indol-3-yl)acetic acidof Formula (Ia) and salts thereof, an S1P1 receptor modulator that is useful in the treatment of S1P...

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Hauptverfasser: MA YOU-AN, MARTINELLI MICHAEL JOHN, MONTALBAN ANTONIO GARRIDO, KRISHNAN ASHWIN M, SENGUPTA DIPANJAN, KUHLMAN YOUNG MI, JOHANNSEN STEPHEN R, BUZARD DANIEL J, SATO SUZANNE MICHIKO, GHARBAOUI TAWFIK, DEMATTEI JOHN A
Format: Patent
Sprache:chi ; eng
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Zusammenfassung:The present invention relates to processes and intermediates useful in the preparation of of (R)-2-(7-(4-cyclopentyl-3-(trifluoromethyl)benzyloxy)-1,2,3,4-tetrahydrocyclopenta[b]indol-3-yl)acetic acidof Formula (Ia) and salts thereof, 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 defectin vascular integrity or that are associated with angiogenesis such as may be pathologic (e.g., as may occur in inflammation, tumor development and atherosclerosis). 本发明涉及用于制备式(Ia)的(R)-2-(7-(4-环戊基-3-(三氟甲基)苄基氧基)-1,2,3,4-四氢环戊二烯并[b]吲哚-3-基)乙酸及其盐的方法以及中间体,其为用于治疗S1P1受体相关的病症的S1P1受体调节剂,所述病症为例如淋巴细胞介导的疾病和病症、移植排斥、自身免疫疾病和病症、炎性疾病和病症(例如急性和慢性炎性病症)、癌症以及特征在于血管完整性具有潜在缺陷的病症或者与血管发生相关的病症诸如可以是病理性的那些(例如可发生在炎症、肿瘤发展和动脉粥样硬化中)。