4-[3-(4-bromo-2-fluoro-phenylamino)-propyl]-tetrahydro-pyran-4-carboxylic acid methyl ester | 1228674-40-5

• 分子结构分类: 有机化合物 - 有机酸及其衍生物 - 羧酸及其衍生物
• 英文名称: 4-[3-(4-bromo-2-fluoro-phenylamino)-propyl]-tetrahydro-pyran-4-carboxylic acid methyl ester
• 英文别名: Methyl 4-[3-(4-bromo-2-fluoroanilino)propyl]oxane-4-carboxylate
• CAS: 1228674-40-5
• 化学式: C₁₆H₂₁BrFNO₃
• 分子量: 374.25
• InChiKey: JEBIORJDMGSMEL-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  3.4
• 重原子数：
  22
• 可旋转键数：
  7
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.56
• 拓扑面积：
  47.6
• 氢给体数：
  1
• 氢受体数：
  5

文献信息

• [EN] SUBSTITUTED TETRAHYDROPYRAN SPIRO PYRROLIDINONE AND PIPERIDINONE, PREPARATION AND THERAPEUTIC USE THEREOF<br/>[FR] PYRROLIDINONE ET PIPÉRIDINONE SPIRO À SUBSTITUTION DE TÉTRAHYDROPYRANNE, SA PREPARATION ET SON UTILISATION THÉRAPEUTIQUE
  申请人：SANOFI AVENTIS

  公开号：WO2010065798A1

  公开（公告）日：2010-06-10

  The present invention discloses and claims a series of substituted N-phenyl-bipyrrolidine carboxamides of formula (I) Wherein R1, R2, m, n and p are as described herein. More specifically, the compounds of this invention are modulators of H3 receptors and are, therefore, useful as pharmaceutical agents, especially in the treatment and/or prevention of a variety of diseases modulated by H3 receptors including diseases associated with the central nervous system. Additionally, this invention also discloses methods of preparation of substituted N-phenyl-bipyrrolidine carboxamides and intermediates therefor.

  本发明披露并声称一系列式（I）的取代N-苯基双吡咯烷羧酰胺化合物，其中R1、R2、m、n和p如本文所述。更具体地说，本发明的化合物是H3受体调节剂，因此在制药剂中非常有用，特别是在治疗和/或预防由H3受体调节的各种疾病中，包括与中枢神经系统相关的疾病。此外，本发明还披露了取代N-苯基双吡咯烷羧酰胺及其中间体的制备方法。
• SUBSTITUTED TETRAHYDROPYRAN SPIRO PYRROLIDINONE AND PIPERIDINONE, PREPARATION AND THERAPEUTIC USE THEREOF
  申请人：GAO Zhongli

  公开号：US20110251225A1

  公开（公告）日：2011-10-13

  The present disclosure relates to a series of substituted N-phenyl-bipyrrolidine carboxamides of formula (I): wherein R 1 , R 2 , m, n and p are as described herein. More specifically, the compounds of this invention are modulators of H3 receptors and are, therefore, useful as pharmaceutical agents, especially in the treatment and/or prevention of a variety of diseases modulated by H3 receptors including diseases associated with the central nervous system. Additionally, methods of preparation of substituted N-phenyl-bipyrrolidine carboxamides and intermediates therefore are disclosed.

  本公开涉及一系列置换的N-苯基-双吡咯烷羧酰胺化合物，化学式为（I）：其中R1、R2、m、n和p如本文所述。更具体地说，本发明的化合物是H3受体的调节剂，因此在治疗和/或预防包括与中枢神经系统相关的多种疾病在内的受H3受体调节的疾病中，特别是作为药物剂量是有用的。此外，还公开了置换的N-苯基-双吡咯烷羧酰胺及其中间体的制备方法。
• US8217052B2
  申请人：——

  公开号：US8217052B2

  公开（公告）日：2012-07-10
• US8383814B2
  申请人：——

  公开号：US8383814B2

  公开（公告）日：2013-02-26