5-Amino-N-methylcarbamoylindolin | 62368-26-7

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 吲哚及其衍生物
• 英文名称: 5-Amino-N-methylcarbamoylindolin
• 英文别名: 5-amino-2,3-dihydro-indole-1-carboxylic acid methylamide；5-Amino-N-methyl-2,3-dihydro-1H-indole-1-carboxamide；5-amino-N-methyl-2,3-dihydroindole-1-carboxamide
• CAS: 62368-26-7
• 化学式: C₁₀H₁₃N₃O
• 分子量: 191.233
• InChiKey: YPHZBKGLGOMMGW-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  0.5
• 重原子数：
  14
• 可旋转键数：
  0
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.3
• 拓扑面积：
  58.4
• 氢给体数：
  2
• 氢受体数：
  2

反应信息

• 作为产物：
  描述：

  5-Amino-1-methyl-1H-indole-2-carboxylic acid methyl ester 5-Amino-1-methyl-1H-indole-2-carboxylic acid ethyl ester 、 、 、 5-氨基吲哚-2-甲酸乙酯 、 、 5-amino-1H-indole-2-carboxylic acid dimethylamide 、 、 methyl 6-amino-1-methyl-1H-indol-2-carboxylate 、 生成 5-Amino-N-methylcarbamoylindolin
  参考文献：
  名称：

  Substituted pyridinyl-pyrimidines and their use as medicaments

  摘要：

  本发明涉及一种新的取代吡啶基嘧啶类化合物，其化学式为1，其中环A是一个五元饱和或不饱和的碳环，可选地包含一、两个或三个杂原子，每个杂原子独立地从N、S和O的群组中选择，其中R1、R2、R4、R3、R5和R6如权利要求1所定义，环A还可选择地被一个或两个进一步的取代基所取代，以及上述化合物的药学上可接受的盐、对映体、立体异构体、混合物、水合物和溶剂化物。

  公开号：

  US08772305B2

文献信息

• SUBSTITUTED PYRIDINYL-PYRIMIDINES AND THEIR USE AS MEDICAMENTS
  申请人：Dahmann Georg

  公开号：US20130023502A1

  公开（公告）日：2013-01-24

  The invention relates to new substituted pyridinyl-pyrimidines of formula 1 wherein ring A is a five-membered saturated or unsaturated carbocyclic ring which optionally comprises one, two or three heteroatoms each independently from each other selected from the group N, S and O, wherein R 1 , R 2 , R 4 , R 3 , R 5 and R 6 are defined as in claim 1 and wherein ring A is further optionally substituted by one or two further substituents and the pharmaceutically acceptable salts, diastereomers, enantiomers, racemates, hydrates and solvates of the aforementioned compounds.

  该发明涉及公式1中的新取代吡啶基嘧啶化合物， 其中环A是一个含有五个成员的饱和或不饱和碳环，该环可选地包含一个、两个或三个异原子，每个异原子独立地选自N、S和O组成， 其中R1、R2、R4、R3、R5和R6如权利要求书中所定义，并且环A进一步可选地被一个或两个进一步取代基取代，以及上述化合物的药用盐、二对映体、对映体、消旋体、水合物和溶剂化合物。
• [EN] SUBSTITUTED PYRIDINYL-PYRIMIDINES AND THEIR USE AS MEDICAMENTS<br/>[FR] PYRIDINYL-PYRIMIDINES SUBSTITUÉES ET LEUR UTILISATION EN TANT QUE MÉDICAMENTS
  申请人：BOEHRINGER INGELHEIM INT

  公开号：WO2012101013A1

  公开（公告）日：2012-08-02

  The invention relates to new substituted pyridinyl-pyrimidines of formula 1 wherein ring A is a five-membered saturated or unsaturated carbocyclic ring which optionally comprises one, two or three heteroatoms each independently from each other selected from the group N, S and O, wherein R1, R2, R4, R3, R5 and R6 are defined as in claim 1 and wherein ring A is further optionally substituted by one or two further substituents and the pharmaceutically acceptable salts, diastereomers, enantiomers, racemates, hydrates and solvates of the aforementioned compounds.

  该发明涉及公式1中的新取代吡啶基嘧啶，其中环A是一个五元饱和或不饱和碳环，可选地包含一个、两个或三个异原子，每个异原子独立地选自N、S和O组，其中R1、R2、R4、R3、R5和R6如权利要求1中所定义，环A进一步可选地被一个或两个进一步取代基取代，以及上述化合物的药学上可接受的盐、二对映体、对映体、消旋体、水合物和溶剂化合物。
• SUBSTITUTED PIPERIDINES AS CCR3 ANTAGONISTS
  申请人：GRUNDL Marc

  公开号：US20100261687A1

  公开（公告）日：2010-10-14

  Object of the present invention are novel substituted compounds of the formula 1, wherein A, R 1 , R 2 , R 3 and R 4 are defined as in the description. Another object of the present invention is to provide antagonists of CCR3, more particularly to provide pharmaceutical compositions comprising a pharmaceutically acceptable carrier and a therapeutically effective amount of at least one of the compounds of the present invention or a pharmaceutically acceptable salt thereof.

  本发明的对象是公式1的新型取代化合物，其中A、R1、R2、R3和R4的定义如描述中所述。本发明的另一个对象是提供CCR3的拮抗剂，更具体地提供包含药用可接受载体和本发明化合物中至少一种或其药用可接受盐的治疗有效量的药物组合物。
• [EN] SUBSTITUTED ARYLSULFONYLAMINOMETHYLPHOSPHONIC ACID DERIVATIVES, THEIR PREPARATION AND THEIR USE IN THE TREATMENT OF TYPE I AND II DIABETES MELLITUS<br/>[FR] DÉRIVÉS SUBSTITUÉS DE L'ACIDE ARYLSULFONYLAMINOMÉTHYLPHOSPHONIQUE, LEUR PRÉPARATION ET LEUR UTILISATION POUR TRAITER LE DIABÈTE SUCRÉ DE TYPE I ET DE TYPE II
  申请人：BOEHRINGER INGELHEIM INT

  公开号：WO2009016119A1

  公开（公告）日：2009-02-05

  The present invention relates to substituted arylsulphonylaminomethylphosphonic acid derivatives of general formula (I) wherein R, X, Y and Z are defined as in claim 1, the tautomers, enantiomers, diastereomers, mixtures thereof and salts thereof which have valuable pharmacological properties, particularly the suppression of the interaction of glycogen phosphorylase a with the GL subunit of glycogen-associated protein phosphatase 1 (PP1), and their use as pharmaceutical compositions.

  本发明涉及一般式(I)的取代芳基磺酰氨甲基膦酸衍生物，其中R、X、Y和Z如权利要求书中所定义，其互变异构体、对映体、非对映体、它们的混合物及其盐具有有价值的药理特性，特别是抑制糖原磷酸化酶a与糖原相关蛋白磷酸酶1（PP1）的GL亚基的相互作用，并将其用作药物组成物。
• SUBSTITUTED ARYLSULFONYLAMINOMETHYLPHOSPHONIC ACID DERIVATIVES, THEIR PREPARATION AND THEIR USE IN THE TREATMENT OF TYPE I AND II DIABETES MELLITUS
  申请人：Wagner Holger

  公开号：US20100210595A1

  公开（公告）日：2010-08-19

  The present invention relates to substituted arylsulphonylaminomethyl-phosphonic acid derivatives of general formula wherein R, X, Y and Z are defined as in claim 1 , the tautomers, enantiomers, diastereomers, mixtures thereof and salts thereof which have valuable pharmacological properties, particularly the suppression of the interaction of glycogen phosphorylase a with the G L subunit of glycogen-associated protein phosphatase 1 (PP1), and their use as pharmaceutical compositions.

  本发明涉及一种一般式为R、X、Y和Z如权利要求1中所定义的取代芳基磺酰胺甲基膦酸衍生物，其互变异构体、对映异构体、顺反异构体、其混合物及其盐具有有价值的药理学性质，特别是抑制糖原磷酸化酶a与糖原相关蛋白磷酸酶1（PP1）的GL亚基相互作用，并将其用作制药组合物。