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US07671062B2 Modulators of chemokine receptor activity, crystalline forms and process 有权
N - （（1R，2S，5R）-5-（异丙基（甲基）氨基）-2 - （（S）-2-氧代-3-（6-三氟甲基）喹唑啉-4-基亚氨基）吡咯烷-1-基 ）CYCLOHEXYL）乙酰胺和其他调节剂的化学接受者活性，结晶形式和过程。

  • Patent Title: Modulators of chemokine receptor activity, crystalline forms and process
  • Patent Title (中): N - （（1R，2S，5R）-5-（异丙基（甲基）氨基）-2 - （（S）-2-氧代-3-（6-三氟甲基）喹唑啉-4-基亚氨基）吡咯烷-1-基 ）CYCLOHEXYL）乙酰胺和其他调节剂的化学接受者活性，结晶形式和过程。
  • Application No.: US11782704
    Application Date: 2007-07-25
  • Publication No.: US07671062B2
    Publication Date: 2010-03-02
  • Inventor: Michael G. Yang , Robert J. Cherney
  • Applicant: Michael G. Yang , Robert J. Cherney
  • Applicant Address: US NJ Princeton
  • Assignee: Bristol-Myers Squibb Company
  • Current Assignee: Bristol-Myers Squibb Company
  • Current Assignee Address: US NJ Princeton
  • Agent Terence J. Bogie; Laurelee A. Duncan
  • Main IPC: A61K31/517
  • IPC: A61K31/517
Modulators of chemokine receptor activity, crystalline forms and process
Abstract:
The present invention provides a novel antagonist or partial agonists/antagonists of MCP-1 receptor activity: N-((1R,2S,5R)-5-(isopropyl(methyl)amino)-2-((S)-2-oxo-3-(6-(trifluoromethyl)quinazolin-4-ylamino)pyrrolidin-1-yl)cyclohexyl)acetamide, or a pharmaceutically acceptable salt, solvate or prodrug, thereof, having an unexpected combination of desirable pharmacological characteristics. Crystalline forms of the present invention are also provided. Pharmaceutical compositions containing the same and methods of using the same as agents for the treatment of inflammatory diseases, allergic, autoimmune, metabolic, cancer and/or cardiovascular diseases is also an objective of this invention. The present disclosure also provides a process for preparing compounds of Formula (I), including N-((1R,2S,5R)-5-(isopropyl(methyl)amino)-2-((S)-2-oxo-3-(6-(trifluoromethyl)quinazolin-4-ylamino)pyrrolidin-1-yl)cyclohexyl)acetamide: wherein R1, R8, R9, R10, and are as described herein. Compounds that are useful intermediates of the process are also provided herein.
Abstract(Chinese):

本发明提供MCP-1受体活性的新型拮抗剂或部分激动剂/拮抗剂：N - （（1R，2S，5R）-5-（异丙基（甲基）氨基）-2 - （（S） -3-（6-（三氟甲基）喹唑啉-4-基氨基）吡咯烷-1-基）环己基）乙酰胺或其药学上可接受的盐，溶剂合物或前药，具有期望的药理学特征的意想不到的组合。 还提供了本发明的结晶形式。 含有该组合物的药物组合物以及使用其作为治疗炎性疾病，过敏性，自身免疫性，代谢性，癌症和/或心血管疾病的药剂的方法也是本发明的目的。 本公开还提供制备式（I）化合物的方法，包括N - （（1R，2S，5R）-5-（异丙基（甲基）氨基）-2 - （（S）-2-氧代-3 - （6-（三氟甲基）喹唑啉-4-基氨基）吡咯烷-1-基）环己基）乙酰胺其中R 1，R 8，R 9，R 10如本文所述。 本文还提供了该方法有用中间体的化合物。

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