3-Carbamoyl-indol-carbonsaeure-(2) | 99361-46-3

• 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: 3-Carbamoyl-indol-carbonsaeure-(2)
• 英文别名: 3-carbamoyl-indole-2-carboxylic acid；3-(Aminocarbonyl)-1H-indole-2-carboxylic acid；3-carbamoyl-1H-indole-2-carboxylic acid
• CAS: 99361-46-3
• 化学式: C₁₀H₈N₂O₃
• 分子量: 204.185
• InChiKey: VRCVIRRNAWHKJP-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  0.8
• 重原子数：
  15
• 可旋转键数：
  2
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.0
• 拓扑面积：
  96.2
• 氢给体数：
  3
• 氢受体数：
  3

文献信息

• [EN] HYDROXAMATE-BASED INHIBITORS OF DEACETYLASES<br/>[FR] COMPOSÉS À BASE D'HYDROXAMATE EN TANT QU'INHIBITEURS DES DÉSACÉTYLASES
  申请人：NOVARTIS AG

  公开号：WO2012025155A1

  公开（公告）日：2012-03-01

  The present teachings relate to compounds of Formula I and pharmaceutically acceptable salts, hydrates, esters, and prodrugs thereof, wherein R1, R2, R3, ring A, and ( formula II) are as defined herein. The present teachings also provide methods of preparing compounds of Formula I and methods of using compounds of Formula I in treating, inhibiting, or preventing pathologic conditions or disorders mediated wholly or in part by deacetylases.

  本教导涉及到Formula I的化合物及其药用盐、水合物、酯和前药，其中R1、R2、R3、环A和（Formula II）如本文所定义。本教导还提供了制备Formula I化合物的方法，以及利用Formula I化合物治疗、抑制或预防完全或部分由去乙酰化酶介导的病理状况或疾病的方法。
• Amide derivatives as NMDA receptor antagonists
  申请人：RICHTER GEDEON VEGYESZETI GYAR RT.

  公开号：US20030199552A1

  公开（公告）日：2003-10-23

  New Formula (I) compounds are disclosed having NR2B selective NMDA receptor antagonist activity 1 wherein one of the neighboring R 1 , R 2 , R 3 and R 4 groups is OH or NH2 and the others are each hydrogen , or two of the neighboring R 1 , R 2 R 3 and R 4 groups in given case together with one or more identical or different additional hetero atom and —CH═ and/or —CH 2 — groups forms a 5-6 membered homo- or heterocyclic ring, preferably pyrrole, pyrazole, imidazole, oxazole, oxo-oxazolidine, or 3-oxo-1,4-oxazine ring, and the other two of R 1 , R 2 , R 3 and R 4 groups are is hydrogen atoms, R 5 and R 6 together with the nitrogen between them form a saturated or unsaturated, 4-6 membered heterocyclic ring, which is substituted by hydroxy group, and/or in given case phenyl or phenoxy, phenyl-(C 1 -C 4 alkyl), phenyl-(C 1 -C 4 alkoxy), phenoxy-(C 1 -C 4 alkyl), anilino, phenyl-(C 1 -C 4 alkylamino), [phenyl-(C 1 -C 4 alkyl)]-amino, benzoyl, hydroxy-diphenylmethyl, C 1 -C 4 alkoxycarbonyl-phenoxymethyl or benzhydrylidene group, optionally substituted on the aromatic ring by one or more halogen atom, cyano or hydroxy group, C 1 -C 4 alkyl or C 1 -C 4 alkoxy group, X is independently oxygen, —NH— or a CH2 group, Y is independently a nitrogen atom or a —CH— group, and the salts thereof formed with acids and bases.

  揭示了具有NR2B选择性NMDA受体拮抗活性的新配方(I)化合物，其中相邻的R1、R2、R3和R4基团中的一个是OH或NH2，其他基团均为氢，或者在某些情况下，相邻的R1、R2、R3和R4基团中的两个与一个或多个相同或不同的额外杂原子和—CH和/或—CH2—基团一起形成5-6元素的同源或异源环，优选为吡咯、吡唑、咪唑、噁唑、噁唑烷酮或3-氧代-1,4-噁唑环，并且R1、R2、R3和R4中的另外两个基团是氢原子，R5和R6与它们之间的氮原子一起形成饱和或不饱和的、4-6元素的杂环，该环被羟基取代，或者在某些情况下为苯基或苯氧基、苯基-(C1-C4烷基)、苯基-(C1-C4氧基)、苯氧基-(C1-C4烷基)、苯胺基、苯基-(C1-C4烷基氨基)、[苯基-(C1-C4烷基)]-氨基、苯甲酰基、羟基-二苯甲基、C1-C4烷氧羰基-苯氧基甲基或苯甲亚乙基基团取代的芳环，该芳环上可以进一步取代一个或多个卤素原子、氰基或羟基、C1-C4烷基或C1-C4氧基基团，X独立地为氧、—NH—或CH2基团，Y独立地为氮原子或—CH—基团，以及与酸和碱形成的盐。
• Indoles Useful in the Treatment of Inflammation
  申请人：Pelcman Benjamin

  公开号：US20090042949A1

  公开（公告）日：2009-02-12

  There is provided compounds of formula I, wherein X 1 , T, Y, R 1 , R 2 , R 3 , R 4 and R 5 have meanings given in the description, and pharmaceutically-acceptable salts thereof, which compounds are useful in the treatment of diseases in which inhibition of the activity of a member of the MAPEG family is desired and/or required, and particularly in the treatment of inflammation.

  提供了公式I的化合物，其中X1，T，Y，R1，R2，R3，R4和R5具有描述中给出的含义，并且其药学上可接受的盐，在抑制MAPEG家族成员活性所需和/或所需的疾病的治疗中有用，特别是在治疗炎症方面。
• Indole-2-carboxylic acid amides
  申请人：Bradley Stuart Edward

  公开号：US20110086885A1

  公开（公告）日：2011-04-14

  Compounds represented by Formula (I) or pharmaceutically acceptable salts thereof, are useful in the prophylactic or therapeutic treatment of diabetes, hyperglycemia, hypercholesterolemia, hyperinsulinemia, hyperlipidemia, hypertension, atherosclerosis or tissue ischemia e.g. myocardial ischemia, and as cardioprotectants.

  公式（I）所代表的化合物或其药学上可接受的盐，可用于预防或治疗糖尿病、高血糖、高胆固醇血症、高胰岛素血症、高脂血症、高血压、动脉粥样硬化或组织缺血（例如心肌缺血），并可作为心脏保护剂。
• INDOLE-2-CARBOXYLIC ACID AMIDES
  申请人：Prosidion Limited

  公开号：EP1819672A1

  公开（公告）日：2007-08-22