4-[2-[[4-Chloro-3-(3-cyanoquinolin-2-yl)benzoyl]-methylamino]phenoxy]butanoic acid | 1070889-84-7

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 喹啉及其衍生物
• 英文名称: 4-[2-[[4-Chloro-3-(3-cyanoquinolin-2-yl)benzoyl]-methylamino]phenoxy]butanoic acid
• CAS: 1070889-84-7
• 化学式: C₂₈H₂₂ClN₃O₄
• 分子量: 499.953
• InChiKey: AGNVMWJKIVFJKH-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  5
• 重原子数：
  36
• 可旋转键数：
  8
• 环数：
  4.0
• sp3杂化的碳原子比例：
  0.14
• 拓扑面积：
  104
• 氢给体数：
  1
• 氢受体数：
  6

文献信息

• GONADOTROPIN-RELEASING HORMONE RECEPTOR ANTAGONISTS AND METHODS RELATING THERETO
  申请人：Beaton Graham

  公开号：US20100152207A1

  公开（公告）日：2010-06-17

  GnRH receptor antagonists are disclosed which have utility in the treatment of a variety of sex-hormone related conditions in both men and women. The compounds of this invention have the structure, wherein R 1a , R 1b , R 1c , R 1d , R 2 , R 2a , and A are as defined herein, including stereoisomers, esters, solvates and pharmaceutically acceptable salts thereof. Also disclosed are compositions containing a compound of this invention in combination with a pharmaceutically acceptable carrier, as well as methods relating to the use thereof for antagonizing gonadotropin-releasing hormone in a subject in need thereof.

  本发明揭示了GnRH受体拮抗剂，其在治疗男性和女性的多种性激素相关疾病中具有实用性。本发明的化合物具有以下结构，其中R1a，R1b，R1c，R1d，R2，R2a和A的定义如本文所述，包括立体异构体，酯类，溶剂合物和其药学上可接受的盐。本发明还揭示了含有本发明化合物与药学上可接受的载体的组合物，以及与其相关的方法，用于在需要的受试者中对抗促性腺激素释放激素。
• Gonadotropin-releasing hormone receptor antagonists and methods relating thereto
  申请人：Neurocrine Biosciences, Inc.

  公开号：US10336769B2

  公开（公告）日：2019-07-02

  GnRH receptor antagonists are disclosed which have utility in the treatment of a variety of sex-hormone related conditions in both men and women. The compounds of this invention have the structure: wherein R1a, R1b, R1c, R1d, R2, R2a, and A are as defined herein, including stereoisomers, esters, solvates and pharmaceutically acceptable salts thereof. Also disclosed are compositions containing a compound of this invention in combination with a pharmaceutically acceptable carrier, as well as methods relating to the use thereof for antagonizing gonadotropin-releasing hormone in a subject in need thereof.

  本发明公开了 GnRH 受体拮抗剂，可用于治疗男性和女性的各种性激素相关疾病。本发明的化合物具有如下结构： 其中 R1a、R1b、R1c、R1d、R2、R2a 和 A 如本文所定义，包括其立体异构体、酯类、溶剂和药学上可接受的盐类。此外，还公开了含有本发明化合物与药学上可接受的载体结合的组合物，以及有关使用其在有需要的受试者体内拮抗促性腺激素释放激素的方法。
• US8084614B2
  申请人：——

  公开号：US8084614B2

  公开（公告）日：2011-12-27
• US8481738B2
  申请人：——

  公开号：US8481738B2

  公开（公告）日：2013-07-09
• US8952161B2
  申请人：——

  公开号：US8952161B2

  公开（公告）日：2015-02-10