1-吲哚啉羧酸 | 763047-58-1

• 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
• 中文名称: 1-吲哚啉羧酸
• 英文名称: (R)-indoline-carboxylic acid
• 英文别名: indoline carboxylic acid；2S-carboxy-indoline；carboxy indoline；L-indoline carboxylic acid；Indoline-1-carboxylic acid；2,3-dihydroindole-1-carboxylic acid
• CAS: 763047-58-1
• 化学式: C₉H₉NO₂
• 分子量: 163.176
• InChiKey: TYHYESDUJZRBKS-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  1.4
• 重原子数：
  12
• 可旋转键数：
  0
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.22
• 拓扑面积：
  40.5
• 氢给体数：
  1
• 氢受体数：
  2

安全信息

• 海关编码：
  2933990090

反应信息

• 作为反应物：
  描述：

  1-吲哚啉羧酸 以 N,N-二甲基甲酰胺-d7 为溶剂， 生成 吲哚啉
  参考文献：
  名称：

  Solvent-dependent effect by carbon dioxide on the photoreactions of (9-anthryl)alkylamines

  摘要：

  The effect Of CO2 on a photoreaction was first studied systematically by using (9-anthryl)alkylamines (APA, AEA, and AMA) as the starting compound. From close scrutiny of the results, the CO, effect was clearly observed and was well rationalized by the previously reported novel solvent dependence of the amine-CO2 reversible reactions. For instance, the yield of the dimer (h-t from APA or AEA, h-t+h-h from AMA) obtained in MeOH or DMSO was higher under CO2 than under argon and this was ascribed to formation of either ammonium bicarbonate/carbonate in MeOH or carbamic acid in DMSO, which will prevent the nitrogen lone pair from being involved in electron-transfer reactions. In fact, the electron-transfer side reactions producing 1-3 in DMSO were strongly inhibited under CO2. Also, due to formation of noncovalent linkage between the ammonium cation and the carbamate anion in 2-PrOH, the proportion of h-h relative to h-t produced from AMA in 2-PrOH was increased by carrying out the reaction under CO2. (c) 2007 Elsevier Ltd. All rights reserved.

  DOI：

  10.1016/j.tet.2007.09.069
• 作为产物：
  描述：

  (S)-吲哚啉-2-羧酸 以 PtO₂ 、 溶剂黄146 为溶剂， 生成 1-吲哚啉羧酸
  参考文献：
  名称：

  Tripeptidylpeptidase inhibitors

  摘要：

  公式为的化合物，其中取代基的定义如规范中所述，以及治疗与胆囊收缩素失活或过度降解相关的疾病的方法也被披露。

  公开号：

  US06403561B1

文献信息

• [EN] INDOLE DERIVATIVES USEFUL AS HISTAMINE H3 ANTAGONISTS<br/>[FR] DERIVES D'INDOLE UTILISES EN TANT QU'ANTAGONISTES H3 D'HISTAMINE
  申请人：SCHERING CORP

  公开号：WO2004000831A1

  公开（公告）日：2003-12-31

  Disclosed are novel compounds of the formula I wherein M1 is CH or N and M2 is C(R3) or N; R1 is optionally substituted indolyl or an aza derivative thereof; R2 is optionally substituted aryl or heteroaryl; and the remaining variables are as defined in the specification. Also disclosed are pharmaceutical compositions comprising the compounds of formula I. Also disclosed are methods of treating various diseases or conditions, such as, for example, allergy, allergy-induced airway responses, and congestion (e.g., nasal congestion) using the compounds of Formula I. Also disclosed are methods of treating various diseases or conditions, such as, for example, allergy, allergy-induced airway responses, and congestion (e.g., nasal congestion) using the compounds of formula I in combination with a H1 receptor antagonist.

  揭示了式I的新化合物，其中M1为CH或N，M2为C(R3)或N；R1为可选择地取代的吲哚基或其氮杂衍生物；R2为可选择地取代的芳基或杂环芳基；其余变量如规范中所定义。还揭示了包括式I化合物的药物组合物。还揭示了使用式I化合物治疗各种疾病或症状的方法，例如过敏、过敏引起的气道反应和充血（例如，鼻塞）等。还揭示了使用式I化合物与H1受体拮抗剂结合治疗各种疾病或症状的方法，例如过敏、过敏引起的气道反应和充血（例如，鼻塞）等。
• [EN] SUBSTITUTED PYRIMIDINYL AND PYRIDINYL-PYRROLOPYRIDINONES, PROCESS FOR THEIR PREPARATION AND THEIR USE AS KINASE INHIBITORS<br/>[FR] PYRIMIDINYL ET PYRIDINYL-PYRROLOPYRIDINONES SUBSTITUÉS, PROCÉDÉ POUR LEUR PRÉPARATION ET LEUR UTILISATION EN TANT QU'INHIBITEURS DE KINASES
  申请人：NERVIANO MEDICAL SCIENCES SRL

  公开号：WO2014072220A1

  公开（公告）日：2014-05-15

  The present invention relates to substituted pyrimidinyl- and pyridinylpyrrolopyridinone compounds which modulate the activity of protein kinases and are therefore useful in treating diseases caused by dysregulated protein kinase activity, in particular RET family kinases. The present invention also provides methods for preparing these compounds, pharmaceutical compositions comprising these compounds, and methods of treating diseases utilizing pharmaceutical compositions containing these compounds.

  本发明涉及替代嘧啶基和吡啶基吡咯吡啶酮化合物，这些化合物调节蛋白激酶的活性，因此在治疗由失调的蛋白激酶活性引起的疾病，特别是 RET 家族激酶方面具有用途。本发明还提供了制备这些化合物的方法，包括这些化合物的药物组合物，以及利用含有这些化合物的药物组合物治疗疾病的方法。
• Indole derivatives useful as histamine H3 antagonists
  申请人：Schering Corporation

  公开号：US20040019099A1

  公开（公告）日：2004-01-29

  Disclosed are novel compounds of the formula 1 wherein M 1 is CH or N and M 2 is C(R 3 ) or N; R 1 is optionally substituted indolyl or an aza derivative thereof; R 2 is optionally substituted aryl or heteroaryl; and the remaining variables are as defined in the specification. Also disclosed are pharmaceutical compositions comprising the compounds of formula I. Also disclosed are methods of treating various diseases or conditions, such as, for example, allergy, allergy-induced airway responses, and congestion (e.g., nasal congestion) using the compounds of Formula I. Also disclosed are methods of treating various diseases or conditions, such as, for example, allergy, allergy-induced airway responses, and congestion (e.g., nasal congestion) using the compounds of formula I in combination with a H 1 receptor antagonist.

  揭示了以下式的新化合物： 其中M1为CH或N，M2为C(R3)或N；R1为可选择地取代的吲哚基或其氮杂衍生物；R2为可选择地取代的芳基或杂环芳基；其余变量如规范中所定义。 还揭示了包括式I化合物的药物组合物。 还揭示了使用式I化合物治疗各种疾病或症状的方法，例如过敏、过敏引起的气道反应和充血（例如鼻塞）。 还揭示了使用式I化合物与H1受体拮抗剂结合治疗各种疾病或症状的方法，例如过敏、过敏引起的气道反应和充血（例如鼻塞）。
• Benzoyl-piperidine derivatives as dual modulators of the 5-HT2A and D3 receptors
  申请人：Gobbi Luca

  公开号：US20070197531A1

  公开（公告）日：2007-08-23

  The present invention relates to compounds of the general formula as dual modulators of the 5-HT 2a and D 3 receptors useful against CNS disorders, wherein A, R 1 , R 2 , n, p, q and r are as defined in the specification.

  本发明涉及一般公式的化合物，作为5-HT2a和D3受体的双重调节剂，用于对抗中枢神经系统疾病，其中A、R1、R2、n、p、q和r的定义如规范中所述。
• Resolution of Racemic Organic Acids with (1S, 4S)-4[3,4-Dichlorophenyl]-1,2,3,4-Tetrahydro-N-Methyl-1-Naphthaloneamine
  申请人：Satyanarayana Chava

  公开号：US20090253932A1

  公开（公告）日：2009-10-08

  The present invention relates to novel chiral resolving agents and a process for resolution of racemic organic acids and their derivatives of the formula (+, −)—R 1 R 2 CHCOOR3 with Cis-(1S,4S)-4[3,4-dichlorophenyl]-1,2,3,4-tetrahydro-N-methyl-1-naphthaloneamine and its Cis-(1R,4R)-isomer as well as Trans-(1S,4R)-4[3,4-dichlorophenyl]-1,2,3,4-tetrahydro-N-methyl-1-naphthaloneamine and its Trans-(1R,4S)-isomer.

  本发明涉及新颖的手性分离剂以及用于分离具有式（+，−）—R1R2CHCOOR3的消旋有机酸及其衍生物的方法，所述方法使用顺式-(1S,4S)-4[3,4-二氯苯基]-1,2,3,4-四氢-N-甲基-1-萘酮胺及其顺式-(1R,4R)-异构体，以及反式-(1S,4R)-4[3,4-二氯苯基]-1,2,3,4-四氢-N-甲基-1-萘酮胺及其反式-(1R,4S)-异构体。