Pyrrolidine, 1-[(2S,3R)-2-amino-3-methyl-1-oxopentyl]- | 177931-21-4

• 分子结构分类: 有机化合物 - 有机酸及其衍生物 - 羧酸及其衍生物
• 英文名称: Pyrrolidine, 1-[(2S,3R)-2-amino-3-methyl-1-oxopentyl]-
• 英文别名: (2S,3R)-2-amino-3-methyl-1-pyrrolidin-1-ylpentan-1-one
• CAS: 177931-21-4
• 化学式: C₁₀H₂₀N₂O
• 分子量: 184.28
• InChiKey: IMCMJLZQYAUSFW-BDAKNGLRSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  1
• 重原子数：
  13
• 可旋转键数：
  3
• 环数：
  1.0
• sp3杂化的碳原子比例：
  0.9
• 拓扑面积：
  46.3
• 氢给体数：
  1
• 氢受体数：
  2

文献信息

• NOVEL INHIBITORS OF GLUTAMINYL CYCLASE
  申请人：Buchholz Mirko

  公开号：US20080267911A1

  公开（公告）日：2008-10-30

  Compounds of formula (I), combinations and uses thereof for disease therapy, or a pharmaceutically acceptable salt, solvate or polymorph thereof, including all tautomers and stereoisomers thereof wherein: R 1 represents and R 2 , R 3 , R 4 , R 5 , R 6 , X 1 , X 2 , X 3 , X 4 , Y and Z are as defined throughout the description and the claims.

  式(I)的化合物，其组合物及用途用于疾病治疗，或其药学上可接受的盐、溶剂化合物或多晶形式，包括其所有互变异构体和立体异构体，其中： R1代表，而R2、R3、R4、R5、R6、X1、X2、X3、X4、Y和Z如描述和权利要求中所定义。
• [EN] NOVEL INHIBITORS<br/>[FR] NOUVEAUX INHIBITEURS
  申请人：PROBIODRUG AG

  公开号：WO2018178384A1

  公开（公告）日：2018-10-04

  The invention relates to a compound of formula (I): A-B-D-E (I) or a pharmaceutically acceptable salt, solvate or polymorph thereof, including all tautomers and stereoisomers thereof, wherein: A is selected from monocyclic and bicyclic heteroaryl, which may independently substituted by alkyl or amino; B is selected from alkyl, heteroalkyl, alkyl-amino, aryl, heteroaryl, cycloalkyl, heterocyclyl and alkylene, wherein said groups may independently be substituted by alkyl; D is selected from aryl-amino, heteroaryl-amino, cycloalkyl-amino, heterocyclyl, heterocyclyl-amino, urea, thioamide, thiourea, sulfonamide, sulfoximine and sulfamoyl, wherein said aryl, heteroaryl, cycloalkyl and heterocyclyl groups may independently be substituted; and E is selected from aryl, heteroaryl, cycloalkyl, heterocyclyl, wherein said aryl, heteroaryl, cycloalkyl and heterocyclyl groups may independently be substituted. The compounds of formula (I) are inhibitors of glutaminyl cyclase (QC, EC 2.3.2.5). QC catalyzes the intramolecular cyclization of N-terminal glutamine residues into pyroglutamic acid (5-oxo-prolyl, pGlu*) under liberation of ammonia and the intramolecular cyclization of N- terminal glutamate residues into pyroglutamic acid under liberation of water.

  该发明涉及以下式(I)的化合物：A-B-D-E (I)或其药学上可接受的盐、溶剂或多型体，包括其所有互变异构体和立体异构体，其中：A选自可以独立由烷基或氨基取代的单环和双环杂环基；B选自烷基、杂环烷基、烷基氨基、芳基、杂芳基、环烷基、杂环烷基和烷基烯，其中这些基团可以独立地被烷基取代；D选自芳基氨基、杂芳基氨基、环烷基氨基、杂环烷基、杂环烷基氨基、脲、硫代酰胺、硫脲、磺酰胺、亚砜和磺酰胺，其中这些芳基、杂芳基、环烷基和杂环烷基基团可以独立地被取代；E选自芳基、杂芳基、环烷基、杂环烷基，其中这些芳基、杂芳基、环烷基和杂环烷基基团可以独立地被取代。式(I)的化合物是谷氨酰环化酶（QC，EC 2.3.2.5）的抑制剂。QC催化N-末端谷氨酸残基的分子内环化成吡咯谷氨酸（5-氧代脯氨酰，pGlu*），释放氨气，并催化N-末端谷氨酸残基的分子内环化成吡咯谷氨酸，释放水。
• NOVEL INHIBITORS
  申请人：Heiser Ulrich

  公开号：US20110092501A1

  公开（公告）日：2011-04-21

  The invention relates to novel pyrrolidine derivatives of formula (I): wherein R 1 , R 2 and R 3 are as defined herein, as inhibitors of glutaminyl cyclase (QC, EC 2.3.2.5). QC catalyzes the intramolecular cyclization of N-terminal glutamine residues into pyroglutamic acid (5-oxo-prolyl, pGlu*) under liberation of ammonia and the intramolecular cyclization of N-terminal glutamate residues into pyroglutamic acid under liberation of water.

  本发明涉及新颖的吡咯烷衍生物，其具有如下公式(I)：其中R1、R2和R3如本文所述定义，作为谷氨酰胺环化酶（QC，EC 2.3.2.5）的抑制剂。谷氨酰胺环化酶催化N末端谷氨酰胺残基形成焦谷氨酸（5-氧代脯氨酸，pGlu*）的分子内环化，并释放氨，以及催化N末端谷氨酸残基形成焦谷氨酸的分子内环化，并释放水。
• ENZYME INHIBITORS
  申请人：Thormann Michael

  公开号：US20070244177A1

  公开（公告）日：2007-10-18

  There is dislosed herein compounds of formula (I), wherein: R 1 , R 2 , R 3 , R 4 and R 5 are defined throughout the description and the claims. The compounds of formula (I) are useful for the treatment of neurological diseases and neurodegenerative diseases, e.g. anxiety, depression, Alzheimer's disease etc.

  本文披露了公式（I）的化合物，其中：R1、R2、R3、R4和R5在描述和权利要求中有定义。公式（I）的化合物可用于治疗神经疾病和神经退行性疾病，例如焦虑、抑郁、阿尔茨海默病等。
• Dipeptidyl peptidase IV inhibitors and their uses for lowering blood pressure levels
  申请人：——

  公开号：US20030176357A1

  公开（公告）日：2003-09-18

  The present invention provides new uses of DPIV-inhibitors of the present invention, and their corresponding pharmaceutically acceptable acid addition salt forms, for lowering blood pressure levels.

  本发明提供了本发明的DPIV抑制剂的新用途，以及其相应的药用可接受的酸盐形式，用于降低血压水平。