1-(α,α-diphenylacetyl)-4-(3-trifluoromethylphenyl)-1,2,3,6-tetrahydropyridine

• 分子结构分类: 有机化合物 - 苯类化合物 - 苯和取代衍生物
• 英文名称: 1-(α,α-diphenylacetyl)-4-(3-trifluoromethylphenyl)-1,2,3,6-tetrahydropyridine
• 英文别名: 1-(α, α-Diphenylacetyl)-4-(3-trifluoromethylphenyl)-1,2,3,6-tetrahydropyridine；1-(alpha,alpha-Diphenylacetyl)-4-(3-trifluoromethylphenyl)-1,2,3,6-tetrahydropyridine；2,2-diphenyl-1-[4-[3-(trifluoromethyl)phenyl]-3,6-dihydro-2H-pyridin-1-yl]ethanone
• 化学式: C₂₆H₂₂F₃NO
• 分子量: 421.462
• InChiKey: WDDWUDFUIOHLFD-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  5.8
• 重原子数：
  31
• 可旋转键数：
  4
• 环数：
  4.0
• sp3杂化的碳原子比例：
  0.19
• 拓扑面积：
  20.3
• 氢给体数：
  0
• 氢受体数：
  4

反应信息

• 作为反应物：
  描述：

  1-(α,α-diphenylacetyl)-4-(3-trifluoromethylphenyl)-1,2,3,6-tetrahydropyridine 在 lithium aluminium tetrahydride 作用下， 以 乙醚 为溶剂， 反应 1.0h， 生成 1-(2,2-diphenylethyl)-4-(3-trifluoromethylphenyl)-1,2,3,6-tetrahydropyridine
  参考文献：
  名称：

  Use of 4-substituted tetrahydropyridines for making medicines acting on TGF-&bgr;1

  摘要：

  该发明涉及使用化合物(I)的方法，用于制备用于增加循环、细胞和细胞外TGF-β1水平的药物组合物。

  公开号：

  US06342505B1
• 作为产物：
  描述：

  二苯基乙酰氯 、 4-[3-(三氟甲基)苯基]-1,2,3,6-四氢吡啶 在 三乙胺 作用下， 以 二氯甲烷 为溶剂， 反应 1.0h， 生成 1-(α,α-diphenylacetyl)-4-(3-trifluoromethylphenyl)-1,2,3,6-tetrahydropyridine
  参考文献：
  名称：

  Use of 4-substituted tetrahydropyridines for making medicines acting on TGF-&bgr;1

  摘要：

  该发明涉及使用化合物(I)的方法，用于制备用于增加循环、细胞和细胞外TGF-β1水平的药物组合物。

  公开号：

  US06342505B1

文献信息

• Use of tetrahydropyridine derivatives to prepare medicines for treating diseases causing demyelination
  申请人：Sanofi-Synthelabo

  公开号：US06344464B1

  公开（公告）日：2002-02-05

  The invention relates to the use of tetrahydropyridine derivatives of the formula in which: R1 is a halogen or a CF3, (C1-C4)alkyl or (C1-C4)alkoxy group; Y is a nitrogen atom or a CH group; Z′ and Z″ are each hydrogen or a (C1-C3)alkyl group, or one is hydrogen and the other is a hydroxyl group, or the two together are an oxo group; and Z is: a phenyl radical; a phenyl radical monosubstituted by a substituent X, X being: (a) a (C1-C6)alkyl, (C1-C6)alkoxy, (C3-C7)carboxyalkyl, (C1-C4)alkoxycarbonyl(C1-C6)alkyl, (C3-C7)carboxyalkoxy or (C1-C4)alkoxycarbonyl(C1-C6)alkoxy group; (b) a group selected from (C3-C7)cycloalkyl, (C3-C7)cycloalkoxy, (C3-C7)cycloalkylmethyl, (C3-C7)cycloalkylamino and cyclohexenyl, it being possible for said group to be substituted by a halogen, hydroxy, (C1-C4)alkoxy, carboxy, (C1-C4)alkoxycarbonyl, amino or mono- or di-(C1-C4)alkylamino group; or (c) a group selected from phenyl, phenoxy, phenylamino, N—(C1-C3)alkyl-phenylamino, phenylmethyl, phenylethyl, phenylcarbonyl, phenylthio, phenylsulfonyl, phenylsulfinyl and styryl, it being possible for said group to be monosubstituted or polysubstituted on the phenyl group by a halogen, CF3, (C1-C4)alkyl, (C1-C4)alkoxy, cyano, amino, mono- or di-(C1-C4)alkylamino, (C1-C4)acylamino, carboxy, (C1-C4)alkoxycarbonyl, aminocarbonyl, mono- or di-(C1-C4)alkylaminocarbonyl, amino(C1-C4)alkyl, hydroxy(C1-C4)alkyl or halogeno(C1-C4)alkyl group; a phenyl radical disubstituted by a substituent R2, R2 being a halogen or a hydroxy, methyl, ethyl, (C3-C6)alkyl, (C1-C4)alkoxy or trifluoromethyl group, and by a substituent X, X being as defined above; a 1-naphthyl or 2-naphthyl radical; or a 1-naphthyl or 2-naphthyl radical substituted in the 5-, 6-, 7- and/or 8-positions by one or two hydroxy groups, one or two (C1-C4)alkoxy groups or a 6,7-methylenedioxy group; or Z″ is hydrogen and Z and Z′ are each independently an unsubstituted or mono-, di- or tri-substituted phenyl group, or a pharmaceutically acceptable salt and solvate thereof, for the preparation of pharmaceutical compositions intended for treating diseases which cause demyelination.

  该发明涉及以下公式的四氢吡啶衍生物的使用：其中：R1是卤素或CF3，(C1-C4)烷基或(C1-C4)烷氧基；Y是氮原子或CH基团；Z′和Z″分别是氢或(C1-C3)烷基，或一个是氢而另一个是羟基，或两者一起是氧代基；而Z是：苯基团；一个被取代基X单取代的苯基团，X是：(a) (C1-C6)烷基，(C1-C6)烷氧基，(C3-C7)羧基烷基，(C1-C4)烷氧羰基(C1-C6)烷基，(C3-C7)羧基烷氧基或(C1-C4)烷氧羰基(C1-C6)烷氧基团；(b) 选择自(C3-C7)环烷基，(C3-C7)环烷氧基，(C3-C7)环烷基甲基，(C3-C7)环烷基氨基和环己烯基的基团，该基团可以被卤素，羟基，(C1-C4)烷氧基，羧基，(C1-C4)烷氧羰基，氨基或单取代或双取代的(C1-C4)烷基氨基团取代；或(c) 选择自苯基，苯氧基，苯胺基，N—(C1-C3)烷基-苯胺基，苯甲基，苯乙基，苯羰基，苯硫醚，苯磺酰基，苯亚磺酰基和芳基的基团，该基团可以在苯基上被卤素， ，(C1-C4)烷基，(C1-C4)烷氧基，氰基，氨基，单取代或双取代的(C1-C4)烷基氨基，(C1-C4)酰氨基，羧基，(C1-C4)烷氧羰基，氨基羰基，单取代或双取代的(C1-C4)烷基氨基羰基，氨基(C1-C4)烷基，羟基(C1-C4)烷基或卤代(C1-C4)烷基团单取代或多取代；一个被取代基R2二取代的苯基团，R2是卤素或羟基，甲基，乙基，(C3-C6)烷基，(C1-C4)烷氧基或三氟甲基团，并且被定义如上的取代基X；一个1-萘基或2-萘基团；或一个在5、6、7和/或8位被一个或两个羟基，一个或两个(C1-C4)烷氧基或一个6,7-亚甲二氧基基团取代的1-萘基或2-萘基团；或Z″是氢，Z和Z′各自独立地是未取代或单取代，二取代或三取代的苯基团，或其药学上可接受的盐和溶剂，用于制备用于治疗导致髓鞘脱失的疾病的药物组合物。
• Diphenylalkyl-tetrahydropyridines, process for their preparation, and
  申请人：Sanofi-Synthelabo

  公开号：US06124318A1

  公开（公告）日：2000-09-26

  The invention relates to compounds of the formula ##STR1## in which: Y is --CH-- or --N--; R.sub.1 is a halogen or a CF.sub.3, (C.sub.1 -C.sub.4)alkyl or (C.sub.1 -C.sub.4)alkoxy group; R.sub.2 and R.sub.3 are each hydrogen or a (C.sub.1 -C.sub.3)alkyl; n is 0 or 1; and Ph.sub.1 and Ph.sub.2 are each independently an unsubstituted, monosubstituted or polysubstituted phenyl group; to a process for their preparation and to the pharmaceutical compositions containing them. These compounds have neurotrophic and neuroprotective activity.

  本发明涉及以下式子的化合物：##STR1## 其中：Y是--CH--或--N--；R.sub.1是卤素或CF.sub.3，(C.sub.1-C.sub.4)烷基或(C.sub.1-C.sub.4)烷氧基；R.sub.2和R.sub.3分别是氢或(C.sub.1-C.sub.3)烷基；n为0或1；Ph.sub.1和Ph.sub.2各自独立地是未取代、单取代或多取代的苯基；以及包含它们的制备过程和药物组合物。这些化合物具有神经营养和神经保护活性。
• Use of 4-substituted tetrahydropyridines for the manufacture of medicaments acting upon TGF-beta 1
  申请人：——

  公开号：US20040157868A1

  公开（公告）日：2004-08-12

  The invention relates to the use of a compound of formula (I): 1 for the preparation of pharmaceutical compositions for increasing the circulating, cellular and extracellular levels of TGF-&bgr;1.

  本发明涉及使用公式（I）的化合物制备药物组合物以增加TGF-β1的循环、细胞和细胞外水平。
• Use of 4-substituted tetrahydropyridines for the manufacture of medicament s acting upon TGF-beta 1
  申请人：——

  公开号：US20020091143A1

  公开（公告）日：2002-07-11

  The invention relates to the use of a compound of formula (I): 1 for the preparation of pharmaceutical compositions for increasing the circulating, cellular and extracellular levels of TGF-&bgr;1.

  本发明涉及使用式(I)的化合物制备药物组合物，用于增加循环、细胞和细胞外基质中TGF-&bgr;1的水平。
• Use of 4-substituted tetrahydropyridines for the manufacture of medicaments acting upon TGF-&bgr;1
  申请人：Sanofi-Synthelabo

  公开号：US06693118B2

  公开（公告）日：2004-02-17

  The invention relates to the use of a compound of formula (I): for the preparation of pharmaceutical compositions for increasing the circulating, cellular and extracellular levels of TGF-&bgr;1.

  本发明涉及使用式（I）的化合物用于制备药物组合物，以增加TGF-&bgr;1的循环、细胞和细胞外水平。