1,2-Dimethyloctahydrocyclopenta[c]pyrrole | 87390-54-3

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 吡咯烷类
• 英文名称: 1,2-Dimethyloctahydrocyclopenta[c]pyrrole
• 英文别名: 2,3-dimethyl-3,3a,4,5,6,6a-hexahydro-1H-cyclopenta[c]pyrrole
• CAS: 87390-54-3
• 化学式: C₉H₁₇N
• 分子量: 139.24
• InChiKey: XQSHGZLNOUECCL-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  2
• 重原子数：
  10
• 可旋转键数：
  0
• 环数：
  2.0
• sp3杂化的碳原子比例：
  1.0
• 拓扑面积：
  3.2
• 氢给体数：
  0
• 氢受体数：
  1

文献信息

• Ether Compounds for Treatment of Complement Mediated Disorders
  申请人：Achillion Pharmaceuticals, Inc.

  公开号：US20150239920A1

  公开（公告）日：2015-08-27

  Compounds, methods of use, and processes for making inhibitors of complement factor D comprising Formula I, or a pharmaceutically acceptable salt or composition thereof wherein R 12 or R 13 on the A group is an ether (R 32 ) are provided. The inhibitors described herein target factor D and inhibit or regulate the complement cascade at an early and essential point in the alternative complement pathway, and reduce factor D's ability to modulate the classical and lectin complement pathways. The inhibitors of factor D described herein are capable of reducing the excessive activation of complement, which has been linked to certain autoimmune, inflammatory, and neurodegenerative diseases, as well as ischemia-reperfusion injury and cancer.

  提供了有关制备抑制补体因子D的化合物、使用方法和制备过程，所述化合物包括具有式I的化合物，或其药用可接受的盐或组合物，其中A组上的R12或R13是醚（R32）。本文描述的抑制剂靶向因子D并在替代性补体途径的早期和关键点上抑制或调节补体级联，并减少因子D调节经典和凝集素补体途径的能力。本文描述的因子D抑制剂能够减少过度激活的补体，这与某些自身免疫、炎症和神经退行性疾病、缺血再灌注损伤和癌症有关。
• [EN] ANTI-VIRAL COMPOUNDS FOR TREATING CORONAVIRUS, PICORNAVIRUS, AND NOROVIRUS INFECTIONS<br/>[FR] COMPOSÉS ANTIVIRAUX POUR LE TRAITEMENT D'INFECTIONS À CORONAVIRUS, PICORNAVIRUS ET NOROVIRUS
  申请人：ALIGOS THERAPEUTICS INC

  公开号：WO2021252491A1

  公开（公告）日：2021-12-16

  Provided herein are compounds of Formula (I), or pharmaceutically acceptable salts thereof, pharmaceutical compositions that include a compound described herein (including pharmaceutically acceptable salts of a compound described herein) and methods of synthesizing the same. Also provided herein are methods of treating coronavirus, Picomavirus and Norovims infections with a compound of Formula (I), or a pharmaceutically acceptable salt thereof.

  本文提供了式（I）的化合物或其药用盐，包括包含本文描述的化合物（包括本文描述的化合物的药用盐）的药物组合物以及合成这些化合物的方法。本文还提供了使用式（I）的化合物或其药用盐治疗冠状病毒、皮科病毒和诺如病毒感染的方法。
• PHARMACEUTICAL INTERMEDIATES IN THE SYNTHESIS OF ACE-INHIBITORS AND THE USE THEREOF
  申请人：Porcs-Makkay Marta

  公开号：US20100286404A1

  公开（公告）日：2010-11-11

  The compounds of the general Formula (I), wherein R 1 is aryl or alkyl; R 2 represents alkyl; R 3 represents alkyl or aralkyl, are valuable pharmaceutical intermediates, which can be prepared by reacting a compound of the general Formula (IV) (wherein the definitions of R 1 and R 2 are as above), with at least 2 molar equivalents of the compound of the general Formula (VI) (wherein X represents halogen or tertiary butyloxycarbonyloxy group and R 3 is as defined above). The known compounds of the general Formula (II) (wherein R 1 and R 2 are as defined above) are prepared by reacting the compounds of the general Formula (I) with thionyl chloride. The compounds of the general Formula (I) are new intermediates useful in the synthesis of pharmaceutically active ingredients, particularly in the preparation of ACE-inhibitors, e.g. enalapril, perindopril or ramipril.

  通式（I）化合物中，R1为芳基或烷基；R2代表烷基；R3代表烷基或芳基烷基，是有价值的制药中间体。这些中间体可以通过将通式（IV）化合物（其中R1和R2的定义如上所述）与至少2摩尔当量的通式（VI）化合物（其中X代表卤素或叔丁氧羰氧基，R3如上所定义）反应而制备。通式（II）化合物（其中R1和R2如上所定义）是通过将通式（I）化合物与氯化硫酰反应制备而成。通式（I）化合物是在药物活性成分的合成中有用的新中间体，特别是在ACE抑制剂（例如依那普利、贝那普利或雷米普利）的制备中。
• Process for the preparation of compounds having an ace inhibitory action
  申请人：Jenko Branko

  公开号：US20070072919A1

  公开（公告）日：2007-03-29

  The present invention relates to the process for the preparation of compounds of formula (I) having an ACE inhibitory action wherein carboxy group of stereospecific amino acid is activated with an uranium salt in the presence of an aprotic solvent and an activated amino acid is further transformed with appropriate amine into ACE inhibitor or its precursor.

  本发明涉及一种制备具有ACE抑制作用的式（I）化合物的过程，其中立体特异性氨基酸的羧基在无极性溶剂和铀盐的存在下被活化，然后将活化的氨基酸进一步与适当的胺转化为ACE抑制剂或其前体。
• Phosphonate Compounds for Treatment of Complement Mediated Disorders
  申请人：Achillion Pharmaceuticals, Inc.

  公开号：US20150239921A1

  公开（公告）日：2015-08-27

  Compounds, methods of use, and processes for making inhibitors of complement factor D comprising Formula I, or a pharmaceutically acceptable salt or composition thereof wherein R 12 or R 13 on the A group is a phosphonate (R 32 ) are provided. The inhibitors described herein target factor D and inhibit or regulate the complement cascade at an early and essential point in the alternative complement pathway, and reduce factor D's ability to modulate the classical and lectin complement pathways. The inhibitors of factor D described herein are capable of reducing the excessive activation of complement, which has been linked to certain autoimmune, inflammatory, and neurodegenerative diseases, as well as ischemia-reperfusion injury and cancer.

  提供了包括式子I或其药学上可接受的盐或组合物的补体因子D抑制剂的化合物、使用方法和制备方法，其中在A基团上的R12或R13是磷酸酯（R32）。本文所述的抑制剂靶向因子D，在替代性补体途径的早期和关键点抑制或调节补体级联反应，并减少因子D调节经典和凝集素补体途径的能力。本文所述的因子D抑制剂能够减少过度激活补体，这与某些自身免疫性、炎症性和神经退行性疾病，以及缺血再灌注损伤和癌症有关。