(RS)-1-[bis(4-chlorophenyl)methyl]-3-[(3,5-bis(trifluoro-methyl)phenyl)(methylsulfonyl)methyl]azetidine | 359401-15-3

• 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: (RS)-1-[bis(4-chlorophenyl)methyl]-3-[(3,5-bis(trifluoro-methyl)phenyl)(methylsulfonyl)methyl]azetidine
• 英文别名: 1-[Bis(4-chlorophenyl)methyl]-3-[[3,5-bis(trifluoromethyl)phenyl]-methylsulfonylmethyl]azetidine
• CAS: 359401-15-3
• 化学式: C₂₆H₂₁Cl₂F₆NO₂S
• 分子量: 596.421
• InChiKey: JDKNIOKNNHGRQA-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  7.4
• 重原子数：
  38
• 可旋转键数：
  6
• 环数：
  4.0
• sp3杂化的碳原子比例：
  0.31
• 拓扑面积：
  45.8
• 氢给体数：
  0
• 氢受体数：
  9

文献信息

• Azetidine derivatives, their preparation and pharmaceutical compositions containing them
  申请人：——

  公开号：US20010027193A1

  公开（公告）日：2001-10-04

  Compounds of formula: 1 in which R represents a CR 1 R 2 , C═C(R 5 )SO 2 R 6 or C═C(R 7 )SO 2 alk radical, their preparation and the pharmaceutical compositions containing them.

  式1中R代表CR1R2、C═C(R5)SO2R6或C═C(R7)SO2烷基基团，它们的制备以及含有它们的药物组合物。
• Use of a CB1 Antagonist for Treating Side Effects and Negative Symptoms of Schizophrenia
  申请人：BLACK Mark

  公开号：US20080221078A1

  公开（公告）日：2008-09-11

  The present invention discloses and claims a method of treating cognition deficits in a patient suffering from schizophrenia by administering to said patient a therapeutically effective amount of a CB1 receptor antagonist as described herein. In another aspect, this invention also discloses and claims a combination of one or more CB1 receptor antagonists and of one or more antipsychotic agents useful in the treatment of psychiatric disorders. The combination of this invention provides synergistic results in that the combination improves positive and negative symptoms of schizophrenia, weight gain and catalepsy.

  本发明揭示并声明了一种治疗患有精神分裂症的患者认知缺陷的方法，通过向该患者施用本文所述的CB1受体拮抗剂的治疗有效剂量。在另一个方面，本发明还揭示并声明了一种CB1受体拮抗剂和一种或多种抗精神病药物的组合，用于治疗精神障碍。本发明的这种组合提供了协同效果，改善了精神分裂症的阳性和阴性症状、体重增加和猫病。
• Combination of a CB1 receptor antagonist and of a product which activatives dopaminergic neurotransmission in the brain, the pharmaceutical compositions comprising them and their use in the treatment of parkinson's disease
  申请人：Aventis Pharma S.A.

  公开号：US20040209861A1

  公开（公告）日：2004-10-21

  The present invention relates to the combination of one or more CB1 antagonist azetidine derivatives and of one or more products which activate dopaminergic neurotransmission in the brain, to the pharmaceutical compositions comprising them and to their use in the treatment of Parkinson's disease.

  本发明涉及一种或多种CB1拮抗剂氮杂环衍生物和一种或多种促进脑内多巴胺能神经传递的产物的组合，以及包含它们的制药组合物，用于治疗帕金森病。
• Pharmacological uses of azetidine derivatives
  申请人：Achard Daniel

  公开号：US20050130953A1

  公开（公告）日：2005-06-16

  A method of treating or preventing Alzheimer's disease, Parkinson's Disease and/or schizophrenia, this method comprising administering to a patient in need of such treatment a compound of formula: in which R, R 3 and R 4 are as defined in the specification.

  一种治疗或预防阿尔茨海默病、帕金森病和/或精神分裂症的方法，该方法包括向需要此类治疗的患者施用以下化合物：其中R、R3和R4如规范中所定义。
• Compositions pour le traitement de la maladie de parkinson contentant un antagoniste du récepteur CB1 et un produit qui active la neurotransmission dompaminerque dans le cerveau
  申请人：Aventis Pharma S.A.

  公开号：EP1649849A2

  公开（公告）日：2006-04-26

  La présente invention concerne l'association de un ou plusieurs dérivés d'azétidine antagonistes CB1 et de un ou plusieurs produits qui activent la neurotransmission dopaminergique dans le cerveau, les compositions pharmaceutiques les contenant et leur utilisation pour le traitement de la maladie de Parkinson.

  本发明涉及一种或多种 CB1 拮抗剂氮杂环丁烷衍生物与一种或多种激活脑内多巴胺能神经递质的产品的组合、含有它们的药物组合物及其在治疗帕金森病中的用途。