[7-Ethyl-3-methyl-6-(2-(4-methylphenyl)benzyl)-8-oxamoylpyrrolo[ 1,2-a]pyrazin-1-yl]oxyacetic acid | 245757-41-9

• 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: [7-Ethyl-3-methyl-6-(2-(4-methylphenyl)benzyl)-8-oxamoylpyrrolo[ 1,2-a]pyrazin-1-yl]oxyacetic acid
• 英文别名: 2-[7-Ethyl-3-methyl-6-[[2-(4-methylphenyl)phenyl]methyl]-8-oxamoylpyrrolo[1,2-a]pyrazin-1-yl]oxyacetic acid
• CAS: 245757-41-9
• 化学式: C₂₈H₂₇N₃O₅
• 分子量: 485.539
• InChiKey: WZZIAEJVVRIIQD-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  5.2
• 重原子数：
  36
• 可旋转键数：
  9
• 环数：
  4.0
• sp3杂化的碳原子比例：
  0.21
• 拓扑面积：
  124
• 氢给体数：
  2
• 氢受体数：
  6

文献信息

• Method for the treatment of renal dysfunction with spla2 inhibitors
  申请人：——

  公开号：US20030087944A1

  公开（公告）日：2003-05-08

  A method is disclosed for the treatment of of the symptoms associated with renal dysfunction by administering to an animal in need thereof a therapeutically effective amount of a sPLA 2 inhibitor, such as a 1H-indole-3-glyoxylamide.

  本方法揭示了一种治疗与肾功能障碍相关症状的方法，通过向需要治疗的动物施用一种治疗有效量的 sPLA2 抑制剂，如 1H-吲哚-3-甘酰胺。
• PYRROLO[1,2-a]PYRAZINE sPLA 2 INHIBITOR
  申请人：SHIONOGI & CO., LTD.

  公开号：EP1066290A1

  公开（公告）日：2001-01-10
• US6407104B1
  申请人：——

  公开号：US6407104B1

  公开（公告）日：2002-06-18
• [EN] PYRROLO[1,2-a]PYRAZINE sPLA2 INHIBITOR<br/>[FR] DERIVE DE PYRROLO[1,2-a]PYRAZINE INHIBANT sPLA2
  申请人：SHIONOGI & CO., LTD.

  公开号：WO1999051605A1

  公开（公告）日：1999-10-14

  (EN) Formula (I), wherein R1 is -(L1)-R6 wherein L1 is a divalent linking group of 1 to 18 atoms or the like, and R6 is a carbocyclic ring substituted by at least one non-interfering substituent or the like; R2 is C1 to C3 alkyl, C3 to C4 cycloalkyl or the like group; R3 is -(L2)-(acidic group); R4 and R5 are hydrogen atoms, non-interfering substituents, carbocyclic groups or the like; RA is -C(=X)-C(=X)-NH2 or the like; and X is independently oxygen atom or sulfur atom; the prodrugs thereof, their pharmaceutically acceptable salts, or their solvates, and a composition for inhibiting sPLA2 containing them as effective ingredients.(FR) L'invention concerne un composé de la formule (I) dans laquelle R1 est -(L1)-R6 (L1 étant un groupe de liaison bivalent de 1 à 18 atomes ou autres; et R6 étant un noyau carbocyclique substitué par au moins un substituant passif ou autre); R2 est un groupe alkyle C1-C3, cycloalkyle C3-C4 ou autre; R3 est -(L2)-(groupe acide); R4 et R5 sont des atomes d'hydrogène, des substituants passifs, des groupes carbocycliques ou autres; RA est -C(=X)-C(=X)-NH2 ou autre; et X est indépendamment un atome d'oxygène ou un atome de soufre. L'invention concerne en outre des promédicaments obtenus à partir dudit composé, leurs sels pharmaceutiquement acceptables ou leurs solvats, et une composition les contenant en tant que principes actifs et pouvant inhiber sPLA2.
• [EN] COMPOSITIONS CONTAINING POTENTIAL SPLA2 INHIBITORS FOR THE TREATMENT OF PAIN<br/>[FR] COMPOSITIONS CONTENANT DES INHIBITEURS POTENTIELS DE SPLA2 AFIN DE TRAITER LA DOULEUR
  申请人：LILLY CO ELI

  公开号：WO2001066111A1

  公开（公告）日：2001-09-13

  A method is disclosed for the treatment of pain by administering to an animal in need thereof a therapeutically effective amount of a sPLA2 inhibitor, such as a 1H-indole-3-glyoxylamide or sPLA2 inhibitor in combination with propoxyphene.