4-(1,3-Oxazol-5-yl)benzoyl chloride | 679807-12-6

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 唑类
• 英文名称: 4-(1,3-Oxazol-5-yl)benzoyl chloride
• CAS: 679807-12-6
• 化学式: C₁₀H₆ClNO₂
• 分子量: 207.61
• InChiKey: KMOWXQMLYMQYGP-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  2.5
• 重原子数：
  14
• 可旋转键数：
  2
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.0
• 拓扑面积：
  43.1
• 氢给体数：
  0
• 氢受体数：
  3

反应信息

• 作为反应物：
  描述：

  2-methyl-4-(2-methyl-[1,3′]bipyrrolidinyl-1′-yl)phenylamine 、 4-(1,3-Oxazol-5-yl)benzoyl chloride 生成 N-[2-methyl-4-(2-methyl-[1,3']bipyrrolidinyl-1'-yl)-phenyl]-4-oxazol-5-yl-benzamide
  参考文献：
  名称：

  Substituted N-phenyl-bipyrrolidine carboxamides and therapeutic use thereof

  摘要：

  本发明披露和声明了一系列公式(I)的取代N-苯基双吡咯烷羧酰胺化合物。其中R、R1、R2、R3和R4如本文所述。更具体地说，本发明的化合物是H3受体调节剂，因此在治疗和/或预防包括与中枢神经系统相关的多种H3受体调节的疾病中，特别是作为药物剂量，是非常有用的。此外，本发明还披露了取代N-苯基双吡咯烷羧酰胺化合物及其中间体的制备方法。

  公开号：

  US08618159B2

文献信息

• [EN] PGD2 RECEPTOR ANTAGONISTS FOR THE TREATMENT OF INFLAMMATORY DISEASES<br/>[FR] ANTAGONISTES DE RECEPTEUR DE LA PROSTAGLANDINE D2 POUR LE TRAITEMENT DE MALADIES INFLAMMATOIRES
  申请人：MILLENNIUM PHARM INC

  公开号：WO2005100321A1

  公开（公告）日：2005-10-27

  Disclosed herein are compounds represented by Structural Formula: (I) and (I-A). Also disclosed is the use of such compounds for inhibiting the G-protein coupled receptor referred to as chemoattractant receptor-homologous molecule expressed on Th2, or simply 'CRTH2' for the treatment of inflammatory disorders. The variables in Structural Formula (I) and (I-A) are defined herein.

  本文披露了由结构式(I)和(I-A)表示的化合物。还披露了利用这些化合物抑制称为趋化剂受体同源分子表达在Th2上的G蛋白偶联受体，简称为'CRTH2'，用于治疗炎症性疾病。结构式(I)和(I-A)中的变量在此处被定义。
• [EN] SUBSTITUTED N-PHENYL-BIPYRROLIDINE CARBOXAMIDES AND THERAPEUTIC USE THEREOF<br/>[FR] CARBOXAMIDES DE N-PHÉNYL-BIPYRROLIDINE SUBSTITUÉS ET LEUR UTILISATION THÉRAPEUTIQUE
  申请人：SANOFI AVENTIS

  公开号：WO2009052065A1

  公开（公告）日：2009-04-23

  The present invention discloses and claims a series of substituted N-phenyl-bipyrrolidine carboxamides of formula (I), Wherein R, R1, R2, R3 and R4 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.

  本发明公开并声明了一系列式(I)的取代N-苯基-双吡咯烷羧酰胺，其中R、R1、R2、R3和R4如本文所述。更具体地说，本发明的化合物是H3受体调节剂，因此在制药方面特别有用，尤其是在治疗和/或预防通过H3受体调节的各种疾病，包括与中枢神经系统相关的疾病。此外，本发明还公开了取代N-苯基-双吡咯烷羧酰胺及其中间体的制备方法。
• PGD2 receptor antagonists for the treatment of inflammatory diseases
  申请人：Ghosh Shomir

  公开号：US20050256158A1

  公开（公告）日：2005-11-17

  Disclosed herein are compounds represented by Structural Formula (I) and (I-A): Also disclosed is the use of such compounds for inhibiting the G-protein coupled receptor referred to as chemoattractant receptor-homologous molecule expressed on Th2, or simply “CRTH2” for the treatment of inflammatory disorders. The variables in Structural Formula (I) and (I-A) are defined herein.

  本文揭示了由结构式（I）和（I-A）表示的化合物：还披露了利用这些化合物抑制称为Th2表达的G蛋白偶联受体的化学引诱受体同源分子，简称“CRTH2”，用于治疗炎症性疾病。结构式（I）和（I-A）中的变量在此处被定义。
• SUBSTITUTED N-PHENYL-BIPYRROLIDINE CARBOXAMIDES AND THERAPEUTIC USE THEREOF
  申请人：CZECHTIZKY Werngard

  公开号：US20100173897A1

  公开（公告）日：2010-07-08

  The present invention discloses and claims a series of substituted N-phenyl-bipyrrolidine carboxamides of formula (I). Wherein R, R 1 , R 2 , R 3 and R 4 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.

  本发明揭示和声明了一系列取代的N-苯基双吡咯烷羧酰胺化合物，其化学式为(I)，其中R、R1、R2、R3和R4如本文所述。更具体地，本发明的化合物是H3受体调节剂，因此在治疗和/或预防包括与中枢神经系统相关的多种H3受体调节的疾病方面，特别是作为药物剂量是有用的。此外，本发明还揭示了取代的N-苯基双吡咯烷羧酰胺及其中间体的制备方法。
• PGD2 RECEPTOR ANTAGONISTS FOR THE TREATMENT OF INFLAMMATORY DISEASES
  申请人：MILLENNIUM PHARMACEUTICALS, INC.

  公开号：EP1556047A2

  公开（公告）日：2005-07-27