4-(4-fluorobenzylidene)piperidine hydrochloride

• 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: 4-(4-fluorobenzylidene)piperidine hydrochloride
• 英文别名: 4-(4-fluorobenzylidene)-piperidine hydrochloride；4-[(4-fluorophenyl)methylidene]piperidine;hydrochloride
• 化学式: C₁₂H₁₄FN*ClH
• 分子量: 227.709
• InChiKey: ALVRAPXLHVZNHU-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  3.01
• 重原子数：
  15
• 可旋转键数：
  1
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.33
• 拓扑面积：
  12
• 氢给体数：
  2
• 氢受体数：
  2

反应信息

• 作为反应物：
  描述：

  4-(4-fluorobenzylidene)piperidine hydrochloride 、 2-哌啶羧酸,1-乙基-,(2S)- 生成 ((2S)-1-Ethylpiperidin-2-yl)-[4-(4-fluoro Benzylidene)piperidin-1-yl]methanone Hydrochloride
  参考文献：
  名称：

  Modulators of the cholesterol biosynthetic pathway

  摘要：

  本发明涉及调节胆固醇生物合成途径的方法。体内胆固醇水平与许多病理状态相关。本发明的方法改变了参与胆固醇生物合成的基因的转录水平。本发明的方法可用于治疗由胆固醇生物合成途径介导的疾病。

  公开号：

  US20030191110A1
• 作为产物：
  描述：

  tert-butyl 4-(4-fluorobenzylidene)piperidine-1-carboxylate 以 乙酸乙酯 为溶剂， 以96%的产率得到4-(4-fluorobenzylidene)piperidine hydrochloride
  参考文献：
  名称：

  Modulators of the cholesterol biosynthetic pathway

  摘要：

  本发明涉及调节胆固醇生物合成途径的方法。体内胆固醇水平与许多病理状态相关。本发明的方法改变了参与胆固醇生物合成的基因的转录水平。本发明的方法可用于治疗由胆固醇生物合成途径介导的疾病。

  公开号：

  US20030191110A1

文献信息

• Heteroaromatic derivatives
  申请人：Taisho Pharmaceutical Co., Ltd.

  公开号：US06291467B1

  公开（公告）日：2001-09-18

  An aromaheterocyclic derivative represented by the formula: wherein Z is a group represented by the following formula: wherein Ar1 is a phenyl group or a phenyl group substituted with a halogen atom or an alkyl group of 1 to 5 carbon atoms, R2 is an alkyl group of 1 to 5 carbon atoms, Y is a hydrogen atom, a mercapto group, an alkylthio group of 1 to 5 carbon atoms, an amino group or an amino group substituted with one or two alkyl groups having 1 to 5 carbon atoms, Ar2 is a phenyl group of one or two substituents selected from the group consisting of a halogen atom, an alkyl group of 1 to 5 carbon atoms, an alkoxy group of 1 to 5 carbon atoms, a hydroxyl group and a trifluoromethyl group, or a phenyl group, B1-B2 is CH—CO or C═C(R1) (wherein R1 is a hydrogen atom or an alkyl group of 1 to 5 carbon atoms), and n is an integer of 1 to 4, or a pharmaceutically acceptable salt thereof, which is a dopamine D4 receptor antagonist compound having an antipsychotic action without causing extrapyramidal diseases.

  一种芳香杂环衍生物，其结构式如下：其中Z为以下结构式所示的基团：其中Ar1为苯基或被卤素原子或1至5个碳原子的烷基取代的苯基，R2为1至5个碳原子的烷基，Y为氢原子、巯基、1至5个碳原子的烷硫基、氨基或被一个或两个1至5个碳原子的烷基取代的氨基，Ar2为具有一个或两个选自卤素原子、1至5个碳原子的烷基、1至5个碳原子的烷氧基、羟基和三氟甲基的取代基的苯基，或苯基，B1-B2为CH—CO或C═C(R1)（其中R1为氢原子或1至5个碳原子的烷基），n为1至4的整数，或其药学上可接受的盐，该化合物是一种具有抗精神病作用而不引起锥体外系疾病的D4多巴胺受体拮抗剂。
• Piperazine and piperidine derivatives
  申请人：——

  公开号：US20040034019A1

  公开（公告）日：2004-02-19

  The present invention relates to piperazine and piperidine derivatives, which are especially useful for treating or preventing neuronal damage, particularly damage associated with neurological diseases. These compounds are also useful for stimulating nerve growth. The invention also provides compositions comprising the compounds of the present invention and methods of utilizing those compositions for treating or preventing neuronal damage or for stimulating nerve growth.

  本发明涉及哌嗪和哌啶衍生物，特别适用于治疗或预防神经元损伤，特别是与神经系统疾病相关的损伤。这些化合物还可用于促进神经生长。本发明还提供了包括本发明化合物的组合物以及利用这些组合物治疗或预防神经元损伤或促进神经生长的方法。
• THIAZOLE DERIVATIVES
  申请人：TAISHO PHARMACEUTICAL CO. LTD

  公开号：EP0816362A1

  公开（公告）日：1998-01-07

  The present invention relates to a thiazole derivative represented by formula (I) wherein Ar1 represents a substituted or unsubstituted phenyl or thienyl group, Y1 and Y2 are different and each represents a nitrogen atom or a sulfur atom, R1 represents a hydrogen atom, a C1 to C5 alkyl group, a phenyl group, or an amino group unsubstituted or mono- or di-substituted with a C1 to C5 alkyl group, and R2 represents a substituted or unsubstituted nitrogen heterocycle group, or a pharmaceutically acceptable salt thereof. The compound of the present invention are a dopamine D4 receptor antagonist which has an antipsychotic effect without causing any extrapyramidal disorder.

  本发明涉及一种由式(I)表示的噻唑衍生物，其中Ar1代表一个取代或未取代的苯基或噻吩基团，Y1和Y2不同，每个代表一个氮原子或硫原子，R1代表一个氢原子，一个C1到C5烷基基团，一个苯基，或一个未取代或单取代或双取代的氨基基团，其取代基为C1到C5烷基基团，R2代表一个取代或未取代的氮杂环基团，或其药用可接受的盐。本发明的化合物是多巴胺D4受体拮抗剂，具有抗精神病作用，而不会导致任何锥体外症状障碍。
• [EN] NEW HETEROCYCLIC CARBOXYLIC ACID AMIDE DERIVATIVES<br/>[FR] NOUVEAUX DERIVES AMIDES D'ACIDE CARBOXYLIQUE HETEROCYCLIQUE
  申请人：RICHTER GEDEON VEGYESZET

  公开号：WO2006010969A1

  公开（公告）日：2006-02-02

  The invention relates to new heterocyclic carboxylic acid amide derivatives of formula (I) - wherein the meaning of X is hydrogen or halogen atom, hydroxy, cyano, C1-C4 alkylsulfonamido optionally substituted by a halogen atom or halogen atoms, C1-C4 alkanoylamido optionally substituted by a halogen atom or halogen atoms, arylsulfonamido groups, is -CH= group or -N= atom, Z is one or more hydrogen or halogen atom, C1-C4 alkyl, C1-C4 alkoxy, cyano, trifluoromethyl, trifluoromethoxy group and to the salts thereof, which are antagonists of NMDA receptor or are intermediates for preparing thereof.

  该发明涉及公式（I）的新杂环羧酸酰胺衍生物，其中X的含义是氢或卤素原子，羟基，氰基，C1-C4烷基磺酰胺（可选择地由卤素原子或卤素原子取代），C1-C4烷酰胺（可选择地由卤素原子或卤素原子取代），芳基磺酰胺基团，-CH=基团或-N=原子，Z是一个或多个氢或卤素原子，C1-C4烷基，C1-C4烷氧基，氰基，三氟甲基，三氟甲氧基团及其盐，这些衍生物是NMDA受体的拮抗剂或用于其制备的中间体。
• 2-carbonylthiazole derivatives and use of the same
  申请人：Taisho Pharmaceutical Co., Ltd.

  公开号：US06166033A1

  公开（公告）日：2000-12-26

  This invention provides a 2-carbonylthiazole derivative represented by formula (I): ##STR1## wherein each of Ar.sup.1 and Ar.sup.2 represents a phenyl group or a substituted phenyl group; R.sup.1 represents an alkoxy group having 1 to 5 carbon atoms, a hydroxyl group or an amino group; Y.sup.1 --Y.sup.2 represents CH--CO or C.dbd.CR.sup.2, wherein R.sup.2 represents a hydrogen atom or an alkyl group having 1 to 5 carbon atoms; and n is an integer of from 1 to 4, or a pharmaceutically acceptable salt thereof. The disclosed compounds are useful as drugs for preventing and treating dopamine D receptor-related morbid states such as schizophrenia and problematic behavior caused by cerebrovascular accidents and senile dementia and do not induce extrapyramidal disorders as side effects.

  本发明提供了由公式(I)表示的2-羰基噻唑衍生物：##STR1## 其中Ar.sup.1和Ar.sup.2分别表示苯基或取代苯基；R.sup.1表示具有1到5个碳原子的烷氧基，羟基或氨基；Y.sup.1--Y.sup.2表示CH--CO或C.dbd.CR.sup.2，其中R.sup.2表示氢原子或具有1到5个碳原子的烷基；n为1到4的整数，或其药学上可接受的盐。所述化合物可用作预防和治疗多巴胺D受体相关的病态状态，如精神分裂症和脑血管意外和老年性痴呆引起的问题行为的药物，并不会引起锥体外系障碍作为副作用。