1-(3,4-Dimethoxybenzoyl)-2-methyl-2,3-dihydro-4(1H)-quinolinone | 367509-04-4

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 喹啉及其衍生物
• 英文名称: 1-(3,4-Dimethoxybenzoyl)-2-methyl-2,3-dihydro-4(1H)-quinolinone
• 英文别名: 1-(3,4-Dimethoxybenzoyl)-2-methyl-2,3-dihydroquinolin-4-one
• CAS: 367509-04-4
• 化学式: C₁₉H₁₉NO₄
• 分子量: 325.364
• InChiKey: OMEGXVMERZICDP-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  2.8
• 重原子数：
  24
• 可旋转键数：
  3
• 环数：
  3.0
• sp3杂化的碳原子比例：
  0.26
• 拓扑面积：
  55.8
• 氢给体数：
  0
• 氢受体数：
  4

反应信息

• 作为反应物：
  描述：

  1-(3,4-Dimethoxybenzoyl)-2-methyl-2,3-dihydro-4(1H)-quinolinone 在 sodium tetrahydroborate 作用下， 以 四氢呋喃 、 甲醇 为溶剂， 反应 2.0h， 以82%的产率得到cis-1-(3,4-dimethoxybenzoyl)-2-methyl-1,2,3,4-tetrahydro-4-quinolinol
  参考文献：
  名称：

  EP1382598

  摘要：

  公开号：
• 作为产物：
  描述：

  2,3-二氢-2-甲基-4(1h)-喹啉酮 、 3,4-二甲氧基苯甲酰氯 在 吡啶 作用下， 反应 16.0h， 以65%的产率得到1-(3,4-Dimethoxybenzoyl)-2-methyl-2,3-dihydro-4(1H)-quinolinone
  参考文献：
  名称：

  EP1382598

  摘要：

  公开号：

文献信息

• Soluble beta amyloid precursor protein secretion promoters
  申请人：——

  公开号：US20030216398A1

  公开（公告）日：2003-11-20

  According to the present invention, there are provided compounds represented by formula (I): 1 [wherein R 1 and R 2 represent hydrogen atom, a lower alkyl group, etc.; ring A is an optionally substituted benzene ring, X is oxygen atom, etc.; and Y represents CH or N] or salts thereof, or prodrugs thereof, and use thereof as well as processes of manufacturing these compounds. The compounds of the present invention and the like possess a potent soluble beta amyloid precursor protein secretion promoting activity and suppress the functional disorders or apoptosis of cells, in particular neurons, mediated by the secreted soluble beta amyloid precursor proteins having a neurotrophic factor like property.

  根据本发明提供了以下公式（I）所代表的化合物：其中R1和R2代表氢原子、较低的烷基基团等；环A是一个可选择取代的苯环，X是氧原子等；Y代表CH或N；或其盐，或其前药，以及这些化合物的制造方法。本发明的化合物及类似化合物具有强大的可溶性β淀粉样前体蛋白分泌促进活性，并抑制细胞（特别是神经元）介导的具有类似神经营养因子特性的分泌可溶性β淀粉样前体蛋白引起的功能障碍或细胞凋亡。
• Novel heterocyclic derivatives
  申请人：——

  公开号：US20040157850A1

  公开（公告）日：2004-08-12

  The object of the present invention is to provide soluble &bgr;-amyloid precursor protein secretory stimulators, which are effective in treating neurodegenerative diseases as well as cerebrovascular disorder-induced neuronopathy. More specifically, the present invention provides a novel compound of the following Formula (I) or a salt or prodrug thereof: 1 [wherein R 1 and R 2 each represent a hydrogen atom or a lower alkyl group, etc., Ar 1 and the ring B each represent an optionally substituted aromatic group, the ring A represents an optionally substituted benzene ring, the ring C represents an optionally substituted 4- to 8-membered ring which may further be condensed with an optionally substituted ring, X represents CH or N, and Y represents CH or N].

  本发明的目的是提供可溶性β-淀粉样前体蛋白分泌刺激剂，其对治疗神经退行性疾病以及脑血管疾病引起的神经病变具有有效性。更具体地说，本发明提供了以下式（I）的新化合物或其盐或前药：1 [其中，R1和R2分别代表氢原子或较低的烷基等，Ar1和环B分别代表可选取代的芳香族基团，环A代表可选取代的苯环，环C代表可选取代的4-至8-成员环，可以进一步与可选取代的环融合，X代表CH或N，Y代表CH或N]。
• SOLUBLE BETA AMYLOID PRECURSOR PROTEIN SECRETION PROMOTERS
  申请人：Takeda Chemical Industries, Ltd.

  公开号：EP1283055A1

  公开（公告）日：2003-02-12

  According to the present invention, there are provided compounds represented by formula (I): [wherein R1 and R2 represent hydrogen atom, a lower alkyl group, etc.; ring A is an optionally substituted benzene ring, X is oxygen atom, etc.; and Y represents CH or N] or salts thereof, or prodrugs thereof, and use thereof as well as processes of manufacturing these compounds. The compounds of the present invention and the like possess a potent soluble beta amyloid precursor protein secretion promoting activity and suppress the functional disorders or apoptosis of cells, in particular neurons, mediated by the secreted soluble beta amyloid precursor proteins having a neurotrophic factor like property.

  根据本发明，提供了式(I)代表的化合物： [其中 R1 和 R2 代表氢原子、低级烷基等；环 A 是任选取代的苯环，X 是氧原子等；Y 代表 CH 或 N]或其盐或其原药及其用途以及制造这些化合物的工艺。本发明的化合物及其类似物具有强效的可溶性β淀粉样前体蛋白分泌促进活性，可抑制由分泌的具有类似神经营养因子特性的可溶性β淀粉样前体蛋白介导的细胞，特别是神经元的功能紊乱或凋亡。
• NOVEL HETEROCYCLIC DERIVATIVES
  申请人：Takeda Chemical Industries, Ltd.

  公开号：EP1382598A1

  公开（公告）日：2004-01-21

  The object of the present invention is to provide soluble β-amyloid precursor protein secretory stimulators, which are effective in treating neurodegenerative diseases as well as cerebrovascular disorder-induced neuronopathy. More specifically, the present invention provides a novel compound of the following Formula (I) or a salt or prodrug thereof: [wherein R1 and R2 each represent a hydrogen atom or a lower alkyl group, etc., Ar1 and the ring B each represent an optionally substituted aromatic group, the ring A represents an optionally substituted benzene ring, the ring C represents an optionally substituted 4- to 8-membered ring which may further be condensed with an optionally substituted ring, X represents CH or N, and Y represents CH or N].

  本发明的目的是提供可溶性β-淀粉样前体蛋白分泌刺激剂，它能有效治疗神经退行性疾病以及脑血管疾病引起的神经元病变。更具体地说，本发明提供了下式（I）的新型化合物或其盐或原药： [其中 R1 和 R2 分别代表氢原子或低级烷基等，Ar1 和环 B 分别代表任选取代的芳香基团，环 A 代表任选取代的苯环，环 C 代表任选取代的 4 至 8 元环，可进一步缩合任选取代的环，X 代表 CH 或 N，Y 代表 CH 或 N]。
• US6930104B2
  申请人：——

  公开号：US6930104B2

  公开（公告）日：2005-08-16