3-Acetamino-hydrocarbostyril | 716-91-6

• 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-Acetamino-hydrocarbostyril
• 英文别名: 3-Acetylamino-dihydro-carbostyril；3-acetylamino-3,4-dihydro-1H-quinolin-2-one；N-(2-oxo-1,2,3,4-tetrahydro-[3]quinolyl)-acetamide；N-(2-Oxo-1,2,3,4-tetrahydro-[3]chinolyl)-acetamid；N-(2-oxo-1,2,3,4-tetrahydroquinolin-3-yl)acetamide；N-(2-oxo-3,4-dihydro-1H-quinolin-3-yl)acetamide
• CAS: 716-91-6
• 化学式: C₁₁H₁₂N₂O₂
• 分子量: 204.228
• InChiKey: NBBOFTFBOZPJEN-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  0.5
• 重原子数：
  15
• 可旋转键数：
  1
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.27
• 拓扑面积：
  58.2
• 氢给体数：
  2
• 氢受体数：
  2

反应信息

• 作为反应物：
  描述：

  3-Acetamino-hydrocarbostyril 在 溴 、 sodium acetate 、 溶剂黄146 作用下， 以 水 为溶剂， 反应 1.5h， 生成 N-(6-bromo-2-oxo-1,2,3,4-tetrahydro-[3]quinolyl)-acetamide
  参考文献：
  名称：

  3,8-DIAMINOTETRAHYDROQUINOLINE DERIVATIVE

  摘要：

  公开号：

  EP2241564B1
• 作为产物：
  描述：

  3-(乙酰氨基)-1,2,3,4-四氢-2-氧代-乙酯-3-喹啉羧酸 在 sodium hydroxide 作用下， 以 乙醇 、 异丁酰胺 、 水 为溶剂， 生成 3-Acetamino-hydrocarbostyril
  参考文献：
  名称：

  3,8-DIAMINOTETRAHYDROQUINOLINE DERIVATIVE

  摘要：

  公开号：

  EP2241564B1

文献信息

• [EN] 1,2,3,4-TETRAHYDROQUINOLINE DERIVATIVES AS INHIBITORS OF THE YAP/TAZ-TEAD ACTIVATION FOR TREATING CANCER<br/>[FR] DÉRIVÉS DE 1,2,3,4-TÉTRAHYDROQUINOLINE SERVANT D'INHIBITEURS DE L'ACTIVATION DE YAP/TAZ-TEAD POUR LE TRAITEMENT DU CANCER
  申请人：UNIV LEUVEN KATH

  公开号：WO2022072741A1

  公开（公告）日：2022-04-07

  The present invention relates to novel compounds of formula (la), to said compounds for use as a medicine, more in particular for the prevention or treatment of diseases mediated by activity of YAP/ TAZ-TEAD transcription, yet more in particular for the prevention or treatment of cancer or fibrosis. The present invention also relates to a method for the prevention or treatment of said diseases comprising the use of the novel compounds. The present invention furthermore relates to pharmaceutical compositions or combination preparations of the novel compounds as well as to said compositions or preparations for use as a medicine, more preferably for the prevention or treatment of diseases mediated by activity of YAP/ TAZ-TEAD transcription, yet more in particular for the prevention or treatment of cancer or fibrosis. The present invention also relates to processes for the preparation of said compounds.

  本发明涉及化合物（la）的新颖化合物，以及将该化合物用作药物，更具体地用于预防或治疗由YAP / TAZ-TEAD转录活性介导的疾病，更具体地用于预防或治疗癌症或纤维化。本发明还涉及一种预防或治疗该疾病的方法，包括使用新颖化合物。本发明还涉及新颖化合物的药物组成物或组合制剂，以及将该组成物或制剂用作药物，更具体地用于预防或治疗由YAP / TAZ-TEAD转录活性介导的疾病，更具体地用于预防或治疗癌症或纤维化。本发明还涉及制备该化合物的方法。
• 3,8-diaminotetrahydroquinoline derivative
  申请人：Zeria Pharmaceutical Co., Ltd.

  公开号：US08299255B2

  公开（公告）日：2012-10-30

  To provide a compound which has a potent agonistic activity on GHS-R and which is useful as a therapeutic agent for systemic wasting diseases such as cachexia. A 3,8-diaminotetrahydroquinoline derivative represented by formula (1a) (wherein X represents CH2, C═O, CH—OR, CH—SR, or CH—NRR′; m is a number of 1 or 2; Ar represents a phenyl group, a naphthyl group, a 5-membered or 6-membered aromatic heterocyclic group having one or two elements selected from S, N, and O, or a similar group; R1 and R2, which may be identical to or different from each other, each represent a hydrogen atom or a methyl group; R3 represents a C1 to C6 alkyl group or a similar group; n is a number of 0 or 1; R4 and R5, which may be identical to or different from each other, each represent a hydrogen atom, or a C1 to C6 alkyl group, etc.; and R6, R7, R, and R′, which may be identical to or different from one another, each represent a hydrogen atom or a C1 to C6 alkyl group), or a salt thereof.

  提供一种在GHS-R上具有强烈激动作用的化合物，可用作治疗全身性消耗性疾病（如恶病质）的治疗剂。该化合物为3,8-二氨基四氢喹啉衍生物，其化学式为（1a），其中X代表CH2、C═O、CH—OR、CH—SR或CH—NRR′；m为1或2；Ar代表苯基、萘基、含有S、N和O中的一种或两种元素的5-或6-成员芳香杂环基或类似基团；R1和R2可以相同或不同，分别代表氢原子或甲基基团；R3代表C1到C6烷基或类似基团；n为0或1；R4和R5可以相同或不同，分别代表氢原子或C1到C6烷基等；而R6、R7、R和R′可以相同或不同，分别代表氢原子或C1到C6烷基。该化合物或其盐可用于治疗全身性消耗性疾病。
• Convergent synthesis of dihydroquinolones from o-aminoarylboronates
  作者：Joachim Horn、Ho Yin Li、Stephen P. Marsden、Adam Nelson、Rachel J. Shearer、Amanda J. Campbell、David House、Gordon G. Weingarten

  DOI：10.1016/j.tet.2009.06.103

  日期：2009.10

  An efficient and convergent one-step synthesis of substituted dihydroquinolin-2-ones from alpha,beta-unsaturated esters and aminoaryl pinacolboronates under rhodium catalysis is reported. The reaction is easily applicable in parallel synthesis format and provides convenient access to this pharmaceutically-relevant motif. (C) 2009 Elsevier Ltd. All rights reserved.
• Sasaki; Ueda, Biochemische Zeitschrift, 1931, vol. 232, p. 260,265
  作者：Sasaki、Ueda

  DOI：——

  日期：——
• US8299255B2
  申请人：——

  公开号：US8299255B2

  公开（公告）日：2012-10-30