盐酸吡咯庚汀 | 16378-22-6

• 分子结构分类: 有机化合物 - 苯类化合物 - 二苯并环庚烯
• 中文名称: 盐酸吡咯庚汀
• 英文名称: 1-Ethyl-2-methyl-3-(2-tricyclo[9.4.0.03,8]pentadeca-1(15),3,5,7,11,13-hexaenylidene)pyrrolidine;hydron;chloride
• CAS: 16378-22-6
• 化学式: C22H26ClN
• 分子量: 339.9
• InChiKey: PLJNHZOEOXGWIR-UHFFFAOYSA-N

物化性质

• 熔点：
  250-253°

计算性质

• 辛醇/水分配系数(LogP)：
  5.12
• 重原子数：
  24
• 可旋转键数：
  1
• 环数：
  4.0
• sp3杂化的碳原子比例：
  0.36
• 拓扑面积：
  3.2
• 氢给体数：
  1
• 氢受体数：
  1

文献信息

• NOVEL COMPOUND AND MEDICAL USE THEREOF
  申请人：Kokubo Masaya

  公开号：US20130245074A1

  公开（公告）日：2013-09-19

  Provided is a levodopa prodrug that overcomes the problems attributed to the blood kinetics of levodopa such as large number of doses and the incidence of side effects due to frequent dosing. (2S)-2-Amino-3-(3,4-bis((2-(benzoyloxy)-2-methylpropanoyl)oxy)phenyl)propanoic acid, a salt thereof, or a solvate thereof is a levodopa prodrug, and provides a flat blood concentration-time profile of levodopa through oral administration, and therefore is useful as a preventive and/or therapeutic agent for Parkinson's disease and/or Parkinson's syndrome that overcomes the problems associated with pharmaceutical preparations of levodopa.

  提供了一种左多巴前药，它克服了左多巴的血液动力学问题，例如需要大量剂量和频繁给药导致的副作用。其化学名为(2S)-2-氨基-3-(3,4-双((2-(苯甲酰氧基)-2-甲基丙酰氧)苯基)丙酸，其盐或溶剂化合物是左多巴前药，通过口服给药提供了左多巴平稳的血药浓度时间曲线，因此可用作克服左多巴药物制剂相关问题的帕金森病和/或帕金森综合征的预防和/或治疗药物。
• NOVEL PYRAZOLE DERIVATIVE
  申请人：MOCHIDA PHARMACEUTICAL CO., LTD.

  公开号：US20140378447A1

  公开（公告）日：2014-12-25

  It has been desired to develop a pharmaceutical composition, which is used in agents for preventing and/or treating various diseases related to PDE10 (e.g. mental disorder and neurodegenerative disorder). The present invention provides: compounds having PDE10 inhibitory effect, in particular, compounds having a 4-heteroarylpyrazole-5-carboxylic acid amide structure represented by the following formula (I), or their pharmaceutically acceptable salts, or their solvates; pharmaceutical compositions comprising, as active ingredients, the compounds, or their pharmaceutically acceptable salts, or their solvates; and medical use of the compounds, or their pharmaceutically acceptable salts, or their solvates.

  已经有人希望开发一种药物组合物，用于预防和/或治疗与PDE10相关的各种疾病（例如精神障碍和神经退行性疾病）。本发明提供：具有PDE10抑制作用的化合物，特别是具有以下式（I）所代表的4-杂环芳基吡唑-5-羧酰胺结构的化合物，或其药学上可接受的盐，或其溶剂化物；包含作为活性成分的化合物，或其药学上可接受的盐，或其溶剂化物的药物组合物；以及化合物的医学用途，或其药学上可接受的盐，或其溶剂化物。
• [EN] HYDANTOIN DERIVATIVE<br/>[FR] DÉRIVÉ D'HYDANTOÏNE
  申请人：ONO PHARMACEUTICAL CO

  公开号：WO2021043245A1

  公开（公告）日：2021-03-11

  A compound represented by general formula (I-a) : has a strong DDR1 inhibitory activity, and can be a therapeutic agent for DDR1-related diseases, for example, a cancer, a kidney disease, a cardiovascular disease, a central nervous system disease, or fibrosis.

  一种由一般化学式（I-a）表示的化合物具有强大的DDR1抑制活性，可作为DDR1相关疾病的治疗药物，例如癌症、肾脏疾病、心血管疾病、中枢神经系统疾病或纤维化病。
• Remedies for depression containing ep1 antagonist as the active ingredient
  申请人：——

  公开号：US20040082653A1

  公开（公告）日：2004-04-29

  A pharmaceutical composition for the treatment and/or prevention of depression comprising a compound having an antagonistic activity for EP 1 receptor which a prostaglandin E 2 receptor subtype. EP 1 antagonist is useful for the treatment of depression, for example, endogenous depression, reactive depression, weatherability depression, neurological depressed state, the depressed state of brain organic mental disorder.

  一种用于治疗和/或预防抑郁症的药物组合物，包括一种具有EP1受体拮抗活性的化合物，该受体是前列腺素E2受体亚型。EP1拮抗剂对于治疗抑郁症很有用，例如内源性抑郁症，反应性抑郁症，耐受性抑郁症，神经学抑郁状态，脑器质性心境障碍的抑郁状态。
• NOVEL BENZOFURAN DERIVATIVE, MEDICINAL COMPOSITION CONTAINING THE SAME, AND USES OF THESE
  申请人：Nakamura Tetsuya

  公开号：US20090239860A1

  公开（公告）日：2009-09-24

  The present invention provides compounds represented by general formula (I): or pharmaceutical acceptable salts thereof, wherein R 1 is hydrogen or lower alkyl; R 2 is lower alkyl, halo-lower alkyl, cycloalkyl, heterocycloalkyl, aryl, aralkyl, arylalkenyl, aryloxy-lower alkyl, heteroaryl, heteroaryl-lower alkyl, etc; R 3 , R 4 , R 5 and R 6 are each hydrogen, halogen, cyano, lower alkyl, halo-lower alkyl, lower alkoxy, hydroxy, aryl, etc; provided that at least one of R 3 , R 4 , R 5 and R 6 is other than hydrogen. Compound (I) of the present invention shows a potent adenosine A 2A receptor antagonistic activity, and are useful for treating or preventing a disease mediated by adenosine A 2A receptors such as motor function disorders, depression, anxiety disorders, cognitive function disorders, cerebral ischemia disorders, restless legs syndrome and the like.

  本发明提供了通式(I)所表示的化合物或其药物可接受的盐，其中R1是氢或低碳基；R2是低碳基，卤代低碳基，环烷基，杂环烷基，芳基，芳基烷基，芳基烯基，芳氧基-低碳基，杂芳基，杂芳基-低碳基等；R3、R4、R5和R6均为氢、卤素、氰基、低碳基、卤代低碳基、低碳氧基、羟基、芳基等；其中至少有一个R3、R4、R5和R6不是氢。本发明的化合物(I)表现出强大的腺苷A2A受体拮抗活性，并且可用于治疗或预防由腺苷A2A受体介导的疾病，例如运动功能障碍、抑郁症、焦虑症、认知功能障碍、脑缺血性疾病、不宁腿综合征等。