ethyl 2-[3-(aminomethyl)-4-butoxy-2-isobutyl-1-oxo-1,2-dihydro-6-isoquinolyl]-1,3-thiazole-4-carboxylate | 779319-04-9

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 异喹啉及其衍生物
• 英文名称: ethyl 2-[3-(aminomethyl)-4-butoxy-2-isobutyl-1-oxo-1,2-dihydro-6-isoquinolyl]-1,3-thiazole-4-carboxylate
• 英文别名: Ethyl 2-[3-(aminomethyl)-4-butoxy-2-(2-methylpropyl)-1-oxoisoquinolin-6-yl]-1,3-thiazole-4-carboxylate
• CAS: 779319-04-9
• 化学式: C₂₄H₃₁N₃O₄S
• 分子量: 457.594
• InChiKey: ZEIBESNNLHERGM-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  3.9
• 重原子数：
  32
• 可旋转键数：
  11
• 环数：
  3.0
• sp3杂化的碳原子比例：
  0.46
• 拓扑面积：
  123
• 氢给体数：
  1
• 氢受体数：
  7

文献信息

• Fused heterocyclic compounds
  申请人：——

  公开号：US20040082607A1

  公开（公告）日：2004-04-29

  The present invention provides a compound of the formula: wherein ring A is an optionally substituted 5 to 10-membered aromatic ring; R 1 and R 2 are the same or different and each is an optionally substituted hydrocarbon group or an optionally substituted heterocyclic group; X is a bond and the like; and L is a divalent hydrocarbon group, and a salt thereof, except 3-(aminomethyl)-2,6,7-trimethyl-4-phenyl-1(2H)-isoquinolinone, 3-(aminomethyl)-2-methyl-4-phenyl-1(2H)-isoquinolinone, 3-(aminomethyl)-6-chloro-2-methyl-4-phenyl-1(2H)-isoquinolinone and 3-(aminomethyl)-2-isopropyl-4-phenyl-1(2H)-isoquinolinone. The compound shows a superior peptidase-inhibitory activity and is useful as an agent for the prophylaxis or treatment of diabetes and the like. 1

  本发明提供了一种化合物，其化学式如下：其中环A是一个可选择取代的5至10成员芳香环；R1和R2相同或不同，每个都是一个可选择取代的碳氢化合物基团或可选择取代的杂环基团；X是一个键等；L是一个二价碳氢基团，以及其盐，但不包括3-(氨甲基)-2,6,7-三甲基-4-苯基-1(2H)-异喹啉酮，3-(氨甲基)-2-甲基-4-苯基-1(2H)-异喹啉酮，3-(氨甲基)-6-氯-2-甲基-4-苯基-1(2H)-异喹啉酮和3-(氨甲基)-2-异丙基-4-苯基-1(2H)-异喹啉酮。该化合物表现出优越的肽酶抑制活性，并可用作糖尿病的预防或治疗剂等。
• Controlled release composition
  申请人：Nagahara Naoki

  公开号：US20060177509A1

  公开（公告）日：2006-08-10

  The present invention provides a controlled release composition showing release of an active ingredient (proton pump inhibitor) controlled in two or more steps at different release rates, which contains 1) a release-controlled part A capable of controlling release of the active ingredient to occur at a predetermined rate, 2) a release-controlled part B capable of controlling release of the active ingredient to occur at a predetermined rate lower than the release rate of the release-controlled part A, and where necessary, 3) a release-controlled part C capable of controlling release of the active ingredient to occur at a predetermined rate faster than the release rate of the release-controlled part B, wherein the release of the active ingredient from the release-controlled part B precedes the release of the active ingredient from the release-controlled part A (when release-controlled part C is contained, the release of the active ingredient from the release-controlled part C precedes the release of the active ingredient from the release-controlled part B).

  本发明提供了一种控制释放组合物，该组合物显示出活性成分（质子泵抑制剂）在不同的释放速率下控制释放，其中包括1）能够控制活性成分以预定速率释放的释放控制部分A，2）能够控制活性成分以比释放控制部分A更低的预定速率释放的释放控制部分B，必要时还包括3）能够控制活性成分以比释放控制部分B更快的预定速率释放的释放控制部分C，其中活性成分从释放控制部分B的释放先于从释放控制部分A的释放（当包含释放控制部分C时，从释放控制部分C的释放先于从释放控制部分B的释放）。
• Remedy for Diabetes
  申请人：Suzuki Nobuhiro

  公开号：US20070259927A1

  公开（公告）日：2007-11-08

  The present invention provides an agent for increasing the pancreatic insulin content useful for the treatment of diabetes and the like. In one embodiment, the present invention provides an agent for increasing the pancreatic insulin content, which contains a blood glucose lowering drug that does not stimulate insulin secretion, and a dipeptidyl-peptidase IV inhibitor in combination.

  本发明提供了一种增加胰岛素含量的药剂，用于治疗糖尿病等疾病。在一种实施方案中，本发明提供了一种增加胰岛素含量的药剂，其中包含一种不刺激胰岛素分泌的降血糖药物和一种二肽基肽酶IV抑制剂的组合。
• SUSTAINED RELEASE PREPARATION
  申请人：Takeda Pharmaceutical Company Limited

  公开号：EP1537880A1

  公开（公告）日：2005-06-08

  The sustained-release preparation of the present invention, which contains a dipeptidyl peptidase IV inhibitor and a hydrophilic polymer, can appropriately inhibit the DPP-IV activity, and is superior in convenience or compliance.

  本发明的缓释制剂含有二肽基肽酶 IV 抑制剂和亲水性聚合物，可以适当抑制 DPP-IV 的活性，在方便性或顺应性方面更胜一筹。
• CONTROLLED RELEASE COMPOSITION
  申请人：Takeda Pharmaceutical Company Limited

  公开号：EP1607088A1

  公开（公告）日：2005-12-21

  The present invention provides a controlled release composition showing release of an active ingredient (proton pump inhibitor) controlled in two or more steps at different release rates, which contains 1) a release-controlled part A capable of controlling release of the active ingredient to occur at a predetermined rate, 2) a release-controlled part B capable of controlling release of the active ingredient to occur at a predetermined rate lower than the release rate of the release-controlled part A, and where necessary, 3) a release-controlled part C capable of controlling release of the active ingredient to occur at a predetermined rate faster than the release rate of the release-controlled part B, wherein the release of the active ingredient from the release-controlled part B precedes the release of the active ingredient from the release-controlled part A (when release-controlled part C is contained, the release of the active ingredient from the release-controlled part C precedes the release of the active ingredient from the release-controlled part B).

  本发明提供了一种控释组合物，其活性成分（质子泵抑制剂）的释放可通过两个或多个步骤以不同的释放速率进行控制，该组合物包含 1) 能够控制活性成分以预定速率释放的释放控制部分 A、 2) 能控制活性成分以低于释放控制部分 A 的释放速率的预定速率释放的释放控制部分 B，必要时， 3) 能控制活性成分以快于释放控制部分 B 的释放速率的预定速率释放的释放控制部分 C、其中，活性成分从释放控制部分 B 的释放先于活性成分从释放控制部分 A 的释放（当包含释放控制部分 C 时，活性成分从释放控制部分 C 的释放先于活性成分从释放控制部分 B 的释放）。