7-[[(1-Pyrimidin-2-ylpiperidin-4-yl)methylamino]methyl]-5,6,7,8-tetrahydronaphthalen-1-ol

• 分子结构分类: 有机化合物 - 苯类化合物 - 四氢化萘
• 英文名称: 7-[[(1-Pyrimidin-2-ylpiperidin-4-yl)methylamino]methyl]-5,6,7,8-tetrahydronaphthalen-1-ol
• 化学式: C₂₁H₂₈N₄O
• 分子量: 352.5
• InChiKey: VGMLXKZEOBNMJG-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  3.2
• 重原子数：
  26
• 可旋转键数：
  5
• 环数：
  4.0
• sp3杂化的碳原子比例：
  0.52
• 拓扑面积：
  61.3
• 氢给体数：
  2
• 氢受体数：
  5

文献信息

• [EN] BICYCLIC AROMATIC COMPOUNDS AS THERAPEUTIC AGENTS<br/>[FR] COMPOSES BICYCLIQUES AROMATIQUES UTILISES COMME AGENTS THERAPEUTIQUES
  申请人：KNOLL AG

  公开号：WO1995007274A1

  公开（公告）日：1995-03-16

  (EN) Compounds of formula (I) and pharmaceutically acceptable salts thereof in which A is methylene or -O-; B is methylene or -O-; and g is 0, 1, 2, 3 or 4; U is an alkylene chain optionally substitued by one or more alkyl; Q represents a divalent group containing nitrogen atoms; having utility in the treatment of central nervous system disorders, for example depression, anxiety, psychoses (for example schizophrenia), tardive dyskinesia, Parkinson's disease, obesity, hypertension, Tourette's syndrome, sexual dysfunction, drug addiction, drug abuse, cognitive disorders, Alzheimer's disease, senile dementia, obsessive-compulsive behaviour, panic attacks, eating disorders and anorexia, cardiovascular and cerebrovascular disorders, non-insulin dependent diabetes mellitus, hyperglycaemia, constipation, arrhythmia, disorders of the neuroendocrine system, stress, prostatic hypertrophy, and spasticity.(FR) Composés de la formule (I) et sels pharmaceutiquement acceptables de ces composés; formule dans laquelle A représente méthylène ou -O-; B représente méthylène ou -O-; et g vaut 0, 1, 2, 3, ou 4; U représente une chaîne alkylène éventuellement substituée par au moins un alkyle; et Q représente un groupe bivalent contenant des atomes d'azote. Ces composés conviennent au traitement de troubles du système nerveux central, tels que la dépression, l'anxiété, les psychoses (la schizophrénie, notamment), la dyskinésie tardive, la maladie de Parkinson, l'obésité, l'hypertension, le syndrome de Tourette, le dysfonctionnement sexuel, la toxicomanie, l'abus des drogues, les troubles cognitifs, la maladie d'Alzheimer, la démence sénile, les névroses obsessionnelles, les crises de panique, les troubles alimentaires et l'anorexie, les affections cardiovasculaires et cérébrovasculaires, le diabète sucré non insulino-dépendant, l'hyperglycémie, la constipation, l'arythmie cardiaque, les troubles du système endocrinien, le stress, l'hypertrophie prostatique et la spasmodicité.

  化合物的化学式为(I)，其药物可接受的盐包括：其中A为亚甲基或-O-；B为亚甲基或-O-；g为0、1、2、3或4；U为一种可以被一个或多个烷基取代的烷基链；Q代表含有氮原子的二价基团。这些化合物适用于治疗中枢神经系统疾病，例如抑郁症、焦虑症、精神病（例如精神分裂症）、迟发性运动障碍、帕金森病、肥胖症、高血压、杜雷特综合征、性功能障碍、药物成瘾、药物滥用、认知障碍、阿尔茨海默病、老年性痴呆、强迫症、惊恐发作、进食障碍和厌食症、心血管和脑血管疾病、非胰岛素依赖型糖尿病、高血糖、便秘、心律失常、神经内分泌系统疾病、压力、前列腺肥大和痉挛症。
• BICYCLIC AROMATIC COMPOUNDS AS THERAPEUTIC AGENTS
  申请人：Knoll AG

  公开号：EP0717739A1

  公开（公告）日：1996-06-26
• BICYCLIC AROMATIC COMPOUNDS FOR TREATING DRUG ADDICTION
  申请人：Knoll GmbH

  公开号：EP1198234A2

  公开（公告）日：2002-04-24
• US5767116A
  申请人：——

  公开号：US5767116A

  公开（公告）日：1998-06-16
• [EN] THERAPEUTIC AGENTS<br/>[FR] AGENTS THERAPEUTIQUES
  申请人：KNOLL AG

  公开号：WO2001002391A2

  公开（公告）日：2001-01-11

  Compounds of formula (I) and pharmaceutically acceptable salts thereof in which A is methylene or -O-; B is methylene or -O-; and g is 0, 1, 2, 3 or 4; R1 represents, halo, optionally substituted alkyl, optionally substituted alkoxy, optionally substituted alkylthio, hydroxy, acyloxy, hydroxymethyl, cyano, alkanoyl, alkoxycarbonyl, optionally N-substituted carbamoyl, carbamoylmethyl, sulphamoyl or sulphamoylmethyl, an amino group optionally substituted by one or two alkyl groups, or two adjacent R1 groups together with the carbon atoms to which they are attached form a fused benz ring; R2 is H, alkyl or alkoxy; R3 and R4, which are the same or different, are H, or alkyl; U is an alkylene chain optionally substituted by one or more alkyl; Q represents a divalent group of formula (IIa, IIb or IIc) in which V is a bond or an alkylene chain optionally substituted by one or more alkyl; V' is an alkylene chain optionally substituted by one or more alkyl; X is a bond or an alkylene chain and X' is an alkylene chain, provided that the total number of carbon atoms in X and X' amounts to 3 or 4; R5 is H, or alkyl; and T represents an optionally substituted aromatic group which optionally contains one or more N atoms, provided that T is not 2-pyrimidinyl when A is -O-; have utility in reducing cravings to food or an addictive substance.