2-[2-(8-tert-butyl-4-methyl-3,4-dihydro-2H-benzo[1,4]oxazin-6-yl)-2-oxo-ethyl]-6-ethoxy-3-imino-2,3-dihydro-1H-isoindole-5-carboxylic acid methylamide | 763921-38-6

• 分子结构分类: 有机化合物 - 有机杂环化合物
• 英文名称: 2-[2-(8-tert-butyl-4-methyl-3,4-dihydro-2H-benzo[1,4]oxazin-6-yl)-2-oxo-ethyl]-6-ethoxy-3-imino-2,3-dihydro-1H-isoindole-5-carboxylic acid methylamide
• 英文别名: 2-[2-(8-tert-butyl-4-methyl-2,3-dihydro-1,4-benzoxazin-6-yl)-2-oxoethyl]-6-ethoxy-3-imino-N-methyl-1H-isoindole-5-carboxamide
• CAS: 763921-38-6
• 化学式: C₂₇H₃₄N₄O₄
• 分子量: 478.591
• InChiKey: IQNPLQANKDKNSF-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  3.6
• 重原子数：
  35
• 可旋转键数：
  7
• 环数：
  4.0
• sp3杂化的碳原子比例：
  0.44
• 拓扑面积：
  95
• 氢给体数：
  2
• 氢受体数：
  6

文献信息

• 2-IMINOPYRROLIDINE DERIVATES
  申请人：Eisai Co., Ltd.

  公开号：EP1391451A1

  公开（公告）日：2004-02-25

  A 2-iminopyrrolidine derivative represented by the formula: wherein ring B represents a benzene ring, pyridine ring, etc.; R101 - R103 represent hydrogen, halogen, C1-6 alkyl, etc.; R5 represents hydrogen, C1-6 alkyl, C1-6 alkoxy-C1-6 alkyl, etc.; R6 represents hydrogen, C1-6 alkyl, C1-6 alkyloxycarbonyl, etc.; Y1 represents a single bond, -CH2-, etc.; Y2 represents a single bond, -CO-, etc.; and Ar represents hydrogen, a group represented by the formula: [wherein R10-R14 represent hydrogen, C1-6 alkyl, hydroxyl, C1-6 alkoxy, etc.; and R11 and R12 or R12 and R13 may bond together to form a 5- to 8-membered heterocyclic ring], etc.}, or a salt thereof.

  一种由式表示的 2-亚氨基吡咯烷衍生物： 其中环B代表苯环、吡啶环等；R101-R103代表氢、卤素、C1-6烷基等；R5代表氢、C1-6烷基、C1-6烷氧基-C1-6烷基等；R6代表氢、C1-6烷基、C1-6烷氧基羰基等；Y1代表单键、-CH2-等；Y2代表单键、-CO-等；Ar代表氢、由式代表的基团： [其中 R10-R14 代表氢、C1-6 烷基、羟基、C1-6 烷氧基等；R11 和 R12 或 R12 和 R13 可键合在一起形成 5 至 8 元杂环]等}、 或其盐。
• METHODS AND COMPOSITIONS FOR TREATING CARDIAC DYSFUNCTIONS
  申请人：Mackman Nigel

  公开号：US20090022729A1

  公开（公告）日：2009-01-22

  The present invention provides methods and pharmaceutical compositions for treating or preventing cardiac dysfunctions (e.g., cardiac hypertrophy, cardiac remodeling, or heart failure) in subjects who have or are likely to develop cardiomyopathies. Some of the methods are directed to therapeutic or prophylactic treatment of cardiac dysfunctions in subjects having undergone myocardial injuries such as cardiac ischemia/reperfusion or myocardial infarction. Typically, these methods comprising administering to the subjects a therapeutic composition comprising a compound which can specifically inhibit PAR1 mediated signaling or down-regulate the cellular level of PAR1.
• COMBINATION THERAPIES COMPRISING PAR1 ANTAGONISTS WITH NAR AGONISTS
  申请人：Perelman Michael Sidney

  公开号：US20110065676A1

  公开（公告）日：2011-03-17

  The present invention is directed to a pharmaceutical composition comprising an effective amount of at least one PAR1 antagonist, at least one NAR agonist, optionally, an effective amount of at least one cardiovascular agent, and, optionally, a pharmaceutically acceptable carrier. The present invention also provides for the use of theses pharmaceutical compositions to treat various diseases associated with thrombosis.
• US7244730B2
  申请人：——

  公开号：US7244730B2

  公开（公告）日：2007-07-17
• [EN] COMBINATION THERAPIES COMPRISING PAR1 ANTAGONISTS WITH PAR4 ANTAGONISTS<br/>[FR] THÉRAPIES DE COMBINAISON COMPRENANT DES ANTAGONISTES DE RÉCEPTEUR 1 ACTIVÉ PAR PROTÉASE (PAR1) ASSOCIÉS À DES ANTAGONISTES RÉCEPTEUR 4 ACTIVÉ PAR PROTÉASE (PAR4)
  申请人：SCHERING CORP

  公开号：WO2009124103A2

  公开（公告）日：2009-10-08

  The present invention is directed to a pharmaceutical composition comprising an effective amount of at least one PAR1 antagonist, at least one PAR4 antagonist, optionally, an effective amount of at least one cardiovascular agent, and, optionally, a pharmaceutically acceptable carrier. The present invention also provides for the use of theses pharmaceutical compositions to treat various diseases associated with thrombosis.