2,5-二氧-2,3,4,5-四氢-1H-苯并[E][1,4]二氮杂䓬-8-羧酸 | 195985-12-7

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 苯二氮卓类
• 中文名称: 2,5-二氧-2,3,4,5-四氢-1H-苯并[E][1,4]二氮杂䓬-8-羧酸
• 中文别名: 2,3,4,5-四氢-2,5-二氧代-1H-1,4-苯并二氮杂卓-8-羧酸；2,5-二氧-2,3,4,5-四氢-1H-苯并[E][1,4]二氮杂草-8-羧酸
• 英文名称: 8-[2,3,4,5-Tetrahydro-1H-1,4-benzodiazepin-2,5-dionyl]-carboxylic acid
• 英文别名: 2,5-Dioxo-2,3,4,5-tetrahydro-1H-benzo[e][1,4]diazepine-8-carboxylic acid；2,5-dioxo-3,4-dihydro-1H-1,4-benzodiazepine-8-carboxylic acid
• CAS: 195985-12-7
• 化学式: C₁₀H₈N₂O₄
• mdl: MFCD00798180
• 分子量: 220.185
• InChiKey: RFGPIJJAGNRBBJ-UHFFFAOYSA-N

物化性质

• 沸点：
  680.9±55.0 °C(Predicted)
• 密度：
  1.452

计算性质

• 辛醇/水分配系数(LogP)：
  -0.3
• 重原子数：
  16
• 可旋转键数：
  1
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.1
• 拓扑面积：
  95.5
• 氢给体数：
  3
• 氢受体数：
  4

反应信息

• 作为反应物：
  描述：

  2-Methyl-4-[3-(2-methyl-pyrrolidin-1-ylmethyl)-pyrrolidin-1-yl]-phenylamine 、 2,5-二氧-2,3,4,5-四氢-1H-苯并[E][1,4]二氮杂䓬-8-羧酸 生成 2,5-dioxo-2,3,4,5-tetrahydro-1H-benzo[e][1,4]diazepine-8-carboxylic acid {2-methyl-4-[3-(2-methyl-pyrrolidin-1-ylmethyl)-pyrrolidin-1-yl]-phenyl}-amide
  参考文献：
  名称：

  Substituted N-phenyl-pyrrolidinylmethylpyrrolidine amides and therapeutic use thereof

  摘要：

  本发明披露并声明了一系列式(I)的取代N-苯基吡咯烷基吡咯烷酰胺。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，因此在治疗和/或预防包括与中枢神经系统相关的各种受H3受体调节的疾病中，尤其是有用的药物。此外，本发明还披露了取代吡咯烷基吡咯烷酰胺及其中间体的制备方法。

  公开号：

  US08227504B2

文献信息

• [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。
• [EN] SUBSTITUTED N-PHENYL-PYRROLIDINYLMETHYLPYRROLIDINE AMIDES AND THERAPEUTIC USE THEREOF AS HISTAMINE H3 RECEPTOR MODULATORS<br/>[FR] AMIDES DE N-PHÉNYL-PYRROLIDINYLMÉTHYLPYRROLIDINE SUBSTITUÉS ET LEUR UTILISATION THÉRAPEUTIQUE COMME MODULATEURS DU RÉCEPTEUR H3 DE L'HISTAMINE
  申请人：SANOFI AVENTIS

  公开号：WO2009052063A1

  公开（公告）日：2009-04-23

  The present invention discloses and claims a series of substituted N-phenyl-pyrrolidinylmethylpyrrolidine amides of formula (I) 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 pyrrolidinylmethylpyrrolidine amides and intermediates therefor.

  本发明公开并要求一系列如下所述的化合物的N-苯基-吡咯啉甲基吡咯啉酰胺，其化学式为(I)。更具体地，本发明的这些化合物是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受体调节的疾病中可用作药物。此外，本发明还公开了替代吡咯啉甲基吡咯啉酰胺及其中间体的制备方法。
• Acylated indanyl amines and their use as pharmaceuticals
  申请人：——

  公开号：US20030055093A1

  公开（公告）日：2003-03-20

  The present invention relates to acylated indanyl amines according to the general formula (I) 1 wherein R 1 -R 4 have the meanings given in the description, A is CH 2 , CHOH or CH—(C 1 -C 3 -alkyl), B is CH 2 or CH—(C 1 -C 3 -alkyl), and R 5 is an aryl or heteroaryl group, possibly substituted by the substituents listed in the description. These compounds are useful in the upregulation of endothelial nitric oxide synthase (eNOS), and may therefore be useful for the manufacture of medicaments for the treatment of cardiovascular diseases, stable or unstable angina pectoris, coronary heart disease, Prinzmetal angina, acute coronary syndrome, heart failure, myocardial infarction, stroke, thrombosis, peripheral artery occlusive disease, endothelial dysfunction, atherosclerosis, restenosis, endothelial damage after PTCA, hypertension, essential hypertension, pulmonary hypertension, secondary hypertension, renovascular hypertension, chronic glomerulonephritis, erectile dysfunction, ventricular arrhythmia, diabetes or diabetes complications, nephropathy or retinopathy, angiogenesis, asthma bronchiale, chronic renal failure, cirrhosis of the liver, osteoporosis, restricted memory performance, a restricted ability to learn, or for the lowering of cardiovascular risk of postmenopausal women or after intake of contraceptives.

  本发明涉及通式（I）中的酰化的茚基胺，其中R1-R4具有描述中给出的含义，A为CH2、CHOH或CH—（C1-C3-烷基），B为CH2或CH—（C1-C3-烷基），R5为芳基或杂芳基，可能被描述中列出的取代基取代。这些化合物在上调内皮型一氧化氮合酶（eNOS）方面有用，因此可能用于制造用于治疗心血管疾病、稳定或不稳定心绞痛、冠心病、普林兹梅塔心绞痛、急性冠状综合征、心力衰竭、心肌梗死、中风、血栓形成、周围动脉闭塞性疾病、内皮功能障碍、动脉粥样硬化、再狭窄、PTCA后内皮损伤、高血压、原发性高血压、肺动脉高压、继发性高血压、肾血管性高血压、慢性肾小球肾炎、勃起功能障碍、室性心律失常、糖尿病或糖尿病并发症、肾病或视网膜病变、血管生成、支气管哮喘、慢性肾功能衰竭、肝硬化、骨质疏松症、记忆力受限、学习能力受限，或用于降低绝经后妇女或口服避孕药后心血管风险。
• 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。
• SUBSTITUTED N-PHENYL-PYRROLIDINYLMETHYLPYRROLIDINE AMIDES AND THERAPEUTIC USE THEREOF
  申请人：CZECHTIZKY Werngard

  公开号：US20100173898A1

  公开（公告）日：2010-07-08

  The present invention discloses and claims a series of substituted N-phenyl-pyrrolidinylmethylpyrrolidine amides 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 pyrrolidinylmethylpyrrolidine amides and intermediates therefor.

  本发明揭示并声明了一系列化合物，其为N-苯基-吡咯烷甲基吡咯烷酰胺的取代物，其化学式为(I)，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受体的调节剂，因此在治疗和/或预防多种由H3受体调节的疾病中，特别是中枢神经系统相关疾病中，具有药物学上的用途。此外，本发明还揭示了制备取代的吡咯烷甲基吡咯烷酰胺及其中间体的方法。