5-([1,1‘-biphenyl]-4-yl)-3-ethylthieno[2,3-d]pyrimidine-2,4(1H,3H)-dione | 1032737-46-4

• 分子结构分类: 有机化合物 - 苯类化合物 - 苯和取代衍生物
• 英文名称: 5-([1,1‘-biphenyl]-4-yl)-3-ethylthieno[2,3-d]pyrimidine-2,4(1H,3H)-dione
• 英文别名: 3-ethyl-5-(4-phenylphenyl)-1,3-dihydrothiopheno[2,3-d]pyrimidine-2,4-dione；3-ethyl-5-(4-phenylphenyl)-1H-thieno[2,3-d]pyrimidine-2,4-dione
• CAS: 1032737-46-4
• 化学式: C₂₀H₁₆N₂O₂S
• 分子量: 348.425
• InChiKey: KNPYSQZWEQYUEK-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  4.3
• 重原子数：
  25
• 可旋转键数：
  3
• 环数：
  4.0
• sp3杂化的碳原子比例：
  0.1
• 拓扑面积：
  77.6
• 氢给体数：
  1
• 氢受体数：
  3

文献信息

• A2A ADENOSINE RECEPTOR ANTAGONISTS
  申请人：Elzein Elfatih

  公开号：US20070208040A1

  公开（公告）日：2007-09-06

  The present invention relates to novel compounds that are A 2A adenosine receptor antagonists, and to their use in treating mammals for various disease states, such as obesity, CNS disorders, including the “movement disorders” (Parkinson's disease, Huntington's Chorea, and catelepsy), and cerebral ischemia, excitotoxicity, cognitive and physiological disorders, depression, ADHD, and drug addiction (alcohol, amphetamine, cannabinoids, cocaine, nicotine, and opioids) and to their use in the enhancement of immune response. The invention also relates to methods for the preparation of such compounds, and to pharmaceutical compositions containing them.

  本发明涉及一种新型化合物，它们是A2A腺苷受体拮抗剂，并且用于治疗哺乳动物的各种疾病状态，如肥胖、中枢神经系统紊乱，包括“运动障碍”（帕金森病、亨廷顿舞蹈症和猫病）、脑缺血、兴奋毒性、认知和生理紊乱、抑郁症、注意力缺陷多动障碍（ADHD）以及药物成瘾（酒精、安非他明、大麻素、可卡因、尼古丁和阿片类药物），以及用于增强免疫应答。该发明还涉及制备这类化合物的方法，以及含有它们的药物组合物。
• [EN] BENZOTHIADIAZINE DERIVATIVES AND COMPOSITIONS COMPRISING THE SAME FOR TREATING DISORDERS MEDIATED BY ADENOSINE<br/>[FR] DÉRIVÉS DE BENZOTHIADIAZINE ET COMPOSITIONS LES COMPRENANT POUR TRAITER DES TROUBLES MÉDIÉS PAR L'ADÉNOSINE
  申请人：DCB USA LLC

  公开号：WO2020139803A1

  公开（公告）日：2020-07-02

  Disclosed herein are novel inhibitors of CD73. More specifically, the novel CD73 inhibitors are derived from benzothiadiazine. Further, the present disclosure is related to the use of said benzothiadiazine derivatives in the treatment of diseases and/or disorders mediated by adenosine, such as AIDS, an autoimmune disease, atherosclerosis, a cancer, an infectious disease, ischemia-reperfusion injury and pre-cancerous syndrome. Also encompassed in the present disclosure are pharmaceutical compositions comprising said benzothiadiazine derivatives.

  本文披露了CD73的新型抑制剂。更具体地说，这些新型CD73抑制剂是从苯并噻二嗪中派生出来的。此外，本公开涉及使用该苯并噻二嗪衍生物治疗由腺苷介导的疾病和/或紊乱，如艾滋病、自身免疫性疾病、动脉粥样硬化、癌症、传染病、缺血再灌注损伤和癌前综合征。本公开还包括包含该苯并噻二嗪衍生物的制药组合物。
• [EN] A2A ADENOSINE RECEPTOR ANTAGONISTS<br/>[FR] ANTAGONISTES DU RECEPTEUR A2A DE L'ADENOSINE
  申请人：CV THERAPEUTICS INC

  公开号：WO2007103776A2

  公开（公告）日：2007-09-13

  [EN] The present invention relates to novel compounds that are A2A adenosine receptor antagonists, and to their use in treating mammals for various disease states, such as obesity, CNS disorders, including the "movement disorders" (Parkinson's disease, Huntington's Chorea, and catelepsy), and cerebral ischemia, excitotoxicity, cognitive and physiological disorders, depression, ADHD, and drug addiction (alcohol, amphetamine, cannabinoids, cocaine, nicotine, and opioids) and to their use in the enhancement of immune response. The invention also relates to methods for the preparation of such compounds, and to pharmaceutical compositions containing them.
  [FR] La présente invention concerne de nouveaux composés qui sont des antagonistes du récepteur A2A de l'adénosine, et leur utilisation dans le cadre du traitement de divers états pathologiques chez les mammifères, tels que l'obésité, les troubles du SNC, y compris les 'troubles du mouvement' (la maladie de Parkinson, la chorée d'Huntington, et la catalepsie), et l'ischémie cérébrale, l'excitotoxicité, les troubles cognitifs et physiologiques, la dépression, le TDAH et la toxicomanie (alcool, amphétamine, cannabinoïdes, cocaïne, nicotine et opioïdes), et leur utilisation pour l'amplification de la réponse immunitaire. L'invention concerne également des procédés de préparation de tels composés et des compositions pharmaceutiques les contenant.