Elzasonan metabolite M5 | 1809092-96-3

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 二嗪烷类
• 英文名称: Elzasonan metabolite M5
• 英文别名: (2Z)-4-(3,4-dichlorophenyl)-2-[[2-(4-methyl-4-oxidopiperazin-4-ium-1-yl)phenyl]methylidene]thiomorpholin-3-one
• CAS: 1809092-96-3
• 化学式: C22H23Cl2N3O2S
• 分子量: 464.4
• InChiKey: NTVFZSKOMHUELL-STZFKDTASA-N

计算性质

• 辛醇/水分配系数(LogP)：
  4.5
• 重原子数：
  30
• 可旋转键数：
  3
• 环数：
  4.0
• sp3杂化的碳原子比例：
  0.32
• 拓扑面积：
  66.9
• 氢给体数：
  0
• 氢受体数：
  4

文献信息

• Aralkyl and aralkylidene heterocyclic lactams and imides
  申请人：——

  公开号：US20020049214A1

  公开（公告）日：2002-04-25

  The present invention relates to compounds of the formula I 1 wherein R 1 , R 2 , R 3 , X, Y and the dashed line are as defined in the specification, to intermediates for their preparation, to pharmaceutical compositions containing them and to their medicinal use as psychotherapeutic agents.

  本发明涉及公式I1中的化合物，其中R1、R2、R3、X、Y和虚线如规范中所定义，以及用于它们制备的中间体，含有它们的药物组合物以及它们作为精神治疗剂的药用。
• Combination of gamma-aminobutyric acid modulators and 5-HT1B receptor antagonists
  申请人：Howard Ralph Harry

  公开号：US20050182049A1

  公开（公告）日：2005-08-18

  The present invention relates to a pharmaceutical composition for treating a disorder or condition selected from the group consisting of hypertension, depression, generalized anxiety disorder, phobias, posttraumatic stress disorder, avoidant personality disorder, sexual dysfunction, eating disorders, obesity, chemical dependencies, cluster headache, migraine, pain, Alzheimer's disease, obsessive-compulsive disorder, panic disorder, memory disorders, Parkinson's diseases, endocrine disorders, cerebellar atazia, gastrointestinal tract disorders, negative symptoms of schizophrenia, premenstrual syndrome, Fibromyalgia Syndrome, stress incontinence, Tourette syndrome, trichotillomania, kleptomania, male impotence, cancer, chronic paroxysmal hemicrania and headache in a mammal, preferably a human, comprising (i) a γ-aminobutyric acid modulator or a pharmaceutically acceptable salt thereof, (ii) a 5-HT 1B receptor antagonist or a pharmaceutically acceptable salt thereof, wherein the 5-HT 1B receptor antagonist is selected from the group consisting of (A) a compound of the formula I as described in the specification and (B) a compound of the formula II as described in the specification, and optionally (iii) a pharmaceutically acceptable carrier.

  本发明涉及一种药物组合物，用于治疗选自由高血压、抑郁症、广泛性焦虑症、恐惧症、创伤后应激障碍、回避型人格障碍、性功能障碍、进食障碍、肥胖症、化学依赖性、丛集性头痛、偏头痛、疼痛、阿尔茨海默病、强迫症、惊恐障碍、记忆障碍、帕金森病、内分泌失调症、小脑躁狂症、胃肠道疾病、精神分裂症的阴性症状、经前期综合征、纤维肌痛、帕金森病、内分泌失调、小脑萎缩、胃肠道失调、精神分裂症的阴性症状、经前期综合征、纤维肌痛综合征、压力性尿失禁、抽动秽语综合征、秽语综合征、盗窃癖、男性阳痿、癌症、慢性阵发性头痛和哺乳动物（最好是人类）的头痛，包括 (i) γ-氨基丁酸调节剂或其药学上可接受的盐、 (ii) 5-HT 1B 受体拮抗剂或其药学上可接受的盐、 其中 5-HT 1B 受体拮抗剂选自由以下组成的组 (A) 如说明书所述的式 I 化合物和 (B) 如说明书所述的式 II 化合物，以及 (iii) 可选的药学上可接受的载体。
• Combination of atypical antipsychotics and 5HT-1B receptor antagonists
  申请人：Brodney A. Michael

  公开号：US20050256112A1

  公开（公告）日：2005-11-17

  The present invention relates to a pharmaceutical composition for treating, for example, a disorder or condition selected from the group consisting of hypertension, depression, generalized anxiety disorder, phobias, posttraumatic stress disorder, avoidant personality disorder, sexual dysfunction, eating disorders, obesity, chemical dependencies, cluster headache, migraine, pain, Alzheimer's disease, obsessive-compulsive disorder, panic disorder, memory disorders, Parkinson's diseases, endocrine disorders, cerebellar ataxia, gastrointestinal tract disorders, negative symptoms of schizophrenia, premenstrual syndrome, Fibromyalgia Syndrome, stress incontinence, Tourette syndrome, trichotillomania, kleptomania, male impotence, cancer, chronic paroxysmal hemicrania and headache in a mammal, preferably a human, comprising (i) an atypical antipsychotic or a pharmaceutically acceptable salt thereof, (ii) a 5-HT 1B receptor antagonist or a pharmaceutically acceptable salt thereof, wherein the 5-HT 1B receptor antagonist is selected from the group consisting of (A) a compound of the formula I as described in the specification and (B) a compound of the formula II as described in the specification, and optionally (iii) a pharmaceutically acceptable carrier.

  本发明涉及一种药物组合物，用于治疗例如选自以下组别的疾病或病症：高血压、抑郁症、广泛性焦虑症、恐惧症、创伤后应激障碍、回避型人格障碍、性功能障碍、饮食失调、肥胖症、化学依赖、丛集性头痛、偏头痛、疼痛、阿尔茨海默病、强迫症、惊恐障碍、记忆障碍、帕金森病、内分泌失调、小脑共济失调、胃肠道疾病、精神分裂症的阴性症状、经前期综合征、纤维肌痛、在哺乳动物（最好是人类）中用于治疗记忆障碍、帕金森病、内分泌失调、小脑共济失调、胃肠道疾病、精神分裂症的阴性症状、经前期综合征、纤维肌痛综合征、压力性尿失禁、抽动秽语综合征、毛细血管扩张症、盗窃癖、男性阳痿、癌症、慢性阵发性颅内出血和头痛，包括 (i) 非典型抗精神病药或其药学上可接受的盐、 (ii) 一种 5-HT 1B 受体拮抗剂或其药学上可接受的盐，其中 5-HT 1B 受体拮抗剂选自(A)本说明书所述的式 I 化合物和(B)本说明书所述的式 II 化合物组成的组，以及可选的(iii)药学上可接受的载体。
• BENZYL(IDENE)-LACTAMS AND THEIR USE AS 5HT1-RECEPTOR LIGANDS
  申请人：Pfizer Products Inc.

  公开号：EP1339696A1

  公开（公告）日：2003-09-03
• COMBINATION OF CRF ANTAGONISTS AND 5-HT 1B RECEPTOR ANTAGONISTS
  申请人：Pfizer Products Incorporated

  公开号：EP1703918A2

  公开（公告）日：2006-09-27