7-Fluoro-5-(cyclopropylethynyl)-1,5-dihydro-5-(trifluoromethyl)-1,4-benzodiazepin-2-one | 1349434-15-6

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 喹啉及其衍生物
• 英文名称: 7-Fluoro-5-(cyclopropylethynyl)-1,5-dihydro-5-(trifluoromethyl)-1,4-benzodiazepin-2-one
• 英文别名: 5-(2-cyclopropylethynyl)-7-fluoro-5-(trifluoromethyl)-1H-1,4-benzodiazepin-2-one
• CAS: 1349434-15-6
• 化学式: C₁₅H₁₀F₄N₂O
• 分子量: 310.251
• InChiKey: UHWIUIGHOGHXCX-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  3.1
• 重原子数：
  22
• 可旋转键数：
  1
• 环数：
  3.0
• sp3杂化的碳原子比例：
  0.33
• 拓扑面积：
  41.5
• 氢给体数：
  1
• 氢受体数：
  6

文献信息

• [DE] AMINOTHIOPHENCARBONSÄUREAMIDE UND IHRE VERWENDUNG ALS PHOSPHODIESTERASE INHIBITOREN<br/>[EN] AMINOTHIOPHENE CARBOXYLIC ACID AMIDES AND THE USE THEREOF AS PHOSPHODIESTERASE INHIBITORS<br/>[FR] AMIDES D'ACIDE CARBOXYLIQUE D'AMINOTHIOPHENE ET LEUR UTILISATION COMME INHIBITEURS DE PHOSPHODIESTERASE
  申请人：MERCK PATENT GMBH

  公开号：WO1998016521A1

  公开（公告）日：1998-04-23

  (DE) Aminothiophencarbonsäureamide der Formel (I) sowie deren physiologisch unbedenklichen Salze, worin R1, R2, R3, R4, R5, A und n die in Anspruch 1 angegebenen Bedeutungen haben, zeigen eine Phosphodiesterase V-Hemmung und können zur Behandlung von Erkrankungen des Herz-Kreislaufsystems und zur Therapie von Potenzstörungen eingesetzt werden.(EN) Aminothiophene carboxylic acid amides having formula (I) and their physiologically harmless salts, wherein R1, R2, R3, R4, R5, A and n have the meaning given in claim 1, demonstrate phosphodiesterase V inhibition and can be used to treat cardiovascular diseases and in therapy for disturbances of potency.(FR) L'invention concerne des amides d'acide carboxylique d'aminothiophène de la formule (I) et leurs sels physiologiquement non toxiques. Dans cette formule, R1, R2, R3, R4, R5, A et n ont la signification mentionnée dans la revendication 1. Ces amides d'acide carboxylique d'aminothiophène montrent une inhibition dans la région V de la phosphodiestérase et s'utilisent pour traiter des maladies du système cardio-vasculaire et pour soigner des troubles de l'érection .

  The text describes a class of chemical compounds known as aminothiophene carboxylic acid amides, which are effective inhibitors of phosphodiesterase type 5 (PDE5). These compounds, along with their physiologically harmless salts, are utilized in treating cardiovascular diseases and erectile dysfunction. The key structural elements of these compounds, denoted by R1 to R5, A, and n, are detailed in a specific claim. The compounds' ability to inhibit PDE5 enhances blood flow by maintaining cyclic GMP levels, making them valuable in therapies targeting circulatory and erectile health.
• AMINOTHIOPHENCARBONSÄUREAMIDE UND IHRE VERWENDUNG ALS PHOSPHODIESTERASE INHIBITOREN
  申请人：MERCK PATENT GmbH

  公开号：EP0934301A1

  公开（公告）日：1999-08-11
• 1,4-BENZODIAZEPIN-2-ONES USEFUL AS HIV REVERSE TRANSCRIPTASE INHIBITORS
  申请人：Du Pont Pharmaceuticals Company

  公开号：EP1183242A2

  公开（公告）日：2002-03-06
• US6462037B1
  申请人：——

  公开号：US6462037B1

  公开（公告）日：2002-10-08
• [EN] 1,4-BENZODIAZEPIN-2-ONES USEFUL AS HIV REVERSE TRANSCRIPTASE INHIBITORS<br/>[FR] INHIBITEURS DE TRANSCRIPTASE INVERSE DU VIH A BASE DE 1,4-BENZODIAZEPIN-2-ONES
  申请人：DU PONT PHARM CO

  公开号：WO2000073284A2

  公开（公告）日：2000-12-07

  The present invention relates to 1,4-benzodiazepin-2-ones of Formula (I) or stereoisomeric forms, stereoisomeric mixtures, or pharmaceutically acceptable salt forms thereof, which are useful as inhibitors of HIV reverse transcriptase, and to pharmaceutical compositions and diagnostic kits comprising the same, and methods of using the same for treating viral infection or as an assay standard or reagent.