3-(3-Methoxyanilino)butanoic acid | 933693-40-4

• 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: 3-(3-Methoxyanilino)butanoic acid
• CAS: 933693-40-4
• 化学式: C₁₁H₁₅NO₃
• 分子量: 209.245
• InChiKey: MQSKEVROJHNGCX-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  2.4
• 重原子数：
  15
• 可旋转键数：
  5
• 环数：
  1.0
• sp3杂化的碳原子比例：
  0.36
• 拓扑面积：
  58.6
• 氢给体数：
  2
• 氢受体数：
  4

反应信息

• 作为反应物：
  描述：

  3-(3-Methoxyanilino)butanoic acid 在 palladium on activated charcoal 4-二甲氨基吡啶 、 PPA 、 氢气 、 溶剂黄146 作用下， 以 四氢呋喃 为溶剂， 生成 (2R,4R)-4-Ethyl-7-methoxy-2-methyl-3,4-dihydro-2H-quinoline-1-carboxylic acid tert-butyl ester
  参考文献：
  名称：

  Nonsteroidal androgen receptor agonists based on 4-(trifluoromethyl)-2H-pyrano[3,2-g]quinolin-2-one

  摘要：

  A series of 2H-pyrano[3,2-g]quinolin-2-ones was prepared and tested for the ability to modulate the transcriptional activity of the human androgen receptor (hAR). The parent compound, 4-(trifluoromethyl)-2H-pyrano[3,2-g]quinolin-2-one, displayed moderate interaction with hAR, but substituted analogues were potent hAR modulators in vitro as mesaured by an hAR cotransfection assay in CV-I cells and bound to hAR with high affinity in a whole cell assay. Several analogues were able to activate hAR-mediated gene transcription more potently and efficaciously than dihydrotestosterone. (C) 1999 Elsevier Science Ltd. All rights reserved.

  DOI：

  10.1016/s0960-894x(99)00118-3
• 作为产物：
  描述：

  巴豆酸 、 间氨基苯甲醚 以 甲苯 为溶剂， 生成 3-(3-Methoxyanilino)butanoic acid
  参考文献：
  名称：

  Nonsteroidal androgen receptor agonists based on 4-(trifluoromethyl)-2H-pyrano[3,2-g]quinolin-2-one

  摘要：

  A series of 2H-pyrano[3,2-g]quinolin-2-ones was prepared and tested for the ability to modulate the transcriptional activity of the human androgen receptor (hAR). The parent compound, 4-(trifluoromethyl)-2H-pyrano[3,2-g]quinolin-2-one, displayed moderate interaction with hAR, but substituted analogues were potent hAR modulators in vitro as mesaured by an hAR cotransfection assay in CV-I cells and bound to hAR with high affinity in a whole cell assay. Several analogues were able to activate hAR-mediated gene transcription more potently and efficaciously than dihydrotestosterone. (C) 1999 Elsevier Science Ltd. All rights reserved.

  DOI：

  10.1016/s0960-894x(99)00118-3

文献信息

• Fused, Tricyclic Sulfonamide Inhibitors of Gamma Secretase
  申请人：Konradi W. Andrei

  公开号：US20080021056A1

  公开（公告）日：2008-01-24

  The invention provides compounds of formula I: or pharmaceutically salts thereof where R 1 , R 2 , and the A, B, and C-rings are as defined herein. Compounds of formula I are useful in treating or preventing cognitive disorders, such as Alzheimer's disease. The invention also encompasses pharmaceutical compositions comprising compounds or salts of formula I, methods of preparing the desired compounds, and methods of treating cognitive disorders, such as Alzheimer's disease, using the compounds or salts of formula I.

  该发明提供了公式I的化合物： 或其药用盐，其中R 1 ，R 2 和A、B和C环如本文所定义。公式I的化合物在治疗或预防认知障碍，如阿尔茨海默病方面是有用的。该发明还涵盖了包括公式I的化合物或盐的药物组合物，制备所需化合物的方法，以及使用公式I的化合物或盐治疗认知障碍，如阿尔茨海默病的方法。
• Fused, tricyclic sulfonamide inhibitors of gamma secretase
  申请人：Elan Pharmaceuticals Inc.

  公开号：EP2450358A1

  公开（公告）日：2012-05-09

  The invention provides compounds of formula I: or pharmaceutically salts thereof, where R1, R2 and the A, B, and C-rings are as defined herein. Compounds of formula I are useful in treating or preventing cognitive disorders, such as Alzheimer's disease. The invention also encompasses pharmaceutical compositions comprising compounds or salts of formula I, methods of preparing the desired compunds, and methods of treating cognitive disorders, such as Alzheimer's disease, using the compounds or salts of formula I.

  本发明提供了式 I 的化合物： 或其药用盐，其中 R1、R2 和 A、B 及 C 环如本文所定义。式 I 的化合物可用于治疗或预防认知障碍，如阿尔茨海默病。本发明还包括包含式 I 化合物或盐的药物组合物、制备所需组合物的方法以及使用式 I 化合物或盐治疗认知障碍（如阿尔茨海默病）的方法。
• FUSED, TRICYCLIC SULFONAMIDE INHIBITORS OF GAMMA SECRETASE
  申请人：Elan Pharmaceuticals Inc.

  公开号：EP2038280A2

  公开（公告）日：2009-03-25
• [EN] FUSED, TRICYCLIC SULFONAMIDE INHIBITORS OF GAMMA SECRETASE<br/>[FR] SULFONAMIDES TRICYCLIQUES CONDENSÉS INHIBITEURS DE GAMMA-SECRÉTASE
  申请人：ELAN PHARM INC

  公开号：WO2007143523A2

  公开（公告）日：2007-12-13

  (EN) The invention provides compounds of formula (I): or pharmaceutically salts thereof, where R1, R2 and the A, B, and C-rings are as defined herein. Compounds of formula (I) are useful in treating or preventing cognitive disorders, such as Alzheimer's disease. The invention also encompasses pharmaceutical compositions comprising compounds or salts of formula (I), methods of preparing the desired compunds, and methods of treating cognitive disorders, such as Alzheimer's disease, using the compounds or salts of Formula (I).(FR) La présente invention concerne des composés de formule I : ou des sels pharmaceutiquement acceptables de ceux-ci, où R1, R2 et les cycles A, B et C sont comme présentement défini. Les composés de formule I sont utiles dans le traitement ou la prévention de troubles cognitifs, tels que la maladie d'Alzheimer. L'invention concerne en outre des compositions pharmaceutiques comprenant des composés ou sels de formule I, des procédés de préparation des composés souhaités, et des procédés de traitement de troubles cognitifs, tels que la maladie d'Alzheimer, utilisant les composés ou sels de Formule(I).
• Nonsteroidal androgen receptor agonists based on 4-(trifluoromethyl)-2H-pyrano[3,2-g]quinolin-2-one
  作者：James P. Edwards、Robert I. Higuchi、David T. Winn、Charlotte L.F. Pooley、Thomas R. Caferro、Lawrence G. Hamann、Lin Zhi、Keith B. Marschke、Mark E. Goldman、Todd K. Jones

  DOI：10.1016/s0960-894x(99)00118-3

  日期：1999.4

  A series of 2H-pyrano[3,2-g]quinolin-2-ones was prepared and tested for the ability to modulate the transcriptional activity of the human androgen receptor (hAR). The parent compound, 4-(trifluoromethyl)-2H-pyrano[3,2-g]quinolin-2-one, displayed moderate interaction with hAR, but substituted analogues were potent hAR modulators in vitro as mesaured by an hAR cotransfection assay in CV-I cells and bound to hAR with high affinity in a whole cell assay. Several analogues were able to activate hAR-mediated gene transcription more potently and efficaciously than dihydrotestosterone. (C) 1999 Elsevier Science Ltd. All rights reserved.