2-[(5-bromothiophen-2-yl)-(2-methylpyrazol-3-yl)methoxy]-N,N-dimethylethanamine

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 噻吩类
• 英文名称: 2-[(5-bromothiophen-2-yl)-(2-methylpyrazol-3-yl)methoxy]-N,N-dimethylethanamine
• 化学式: C₁₃H₁₈BrN₃OS
• 分子量: 344.27
• InChiKey: WESVJPSLEXWFPP-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  2.4
• 重原子数：
  19
• 可旋转键数：
  6
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.46
• 拓扑面积：
  58.5
• 氢给体数：
  0
• 氢受体数：
  4

文献信息

• THIENYLAZOLYLALCOXYETHANAMINES, THEIR PREPARATION AND THEIR APPLICATION AS MEDICAMENTS
  申请人：LABORATORIOS DEL DR. ESTEVE, S.A.

  公开号：EP1072266A1

  公开（公告）日：2001-01-31

  The thienylazolylalkoxyethanamines (I) where R1 is a hydrogen atom, a halogen atom or a lower alkyl radical; R2, R3 and R4 represent, independently, a hydrogen atom or a lower alkyl radical; and Az represents a five-member nitrogenated hetercyclic aromatic group, N-methyl-substituted, that contains from one to three nitrogen atoms. They have analgesic activity in mammals, including humans. The compounds (I) can be obtained, for example, by reaction of a derivative of hydroxy-thienylazol (IV) with a derivative of a suitable N-(ethyl)amine. The compounds (IV) are useful intermediates in the synthesis of the compounds (I). The compounds (I) have an application in human and/or veterinary medicine.

  噻唑烷氧基乙胺（I），其中 R1 是氢原子、卤素原子或低级烷基；R2、R3 和 R4 分别代表氢原子或低级烷基；Az 代表含有 1 至 3 个氮原子的 N-甲基取代的五元氮杂环芳香基团。它们对包括人类在内的哺乳动物具有镇痛活性。例如，通过羟基噻吩唑的衍生物（IV）与合适的 N-（乙基）胺的衍生物反应，可以得到化合物（I）。化合物（IV）是合成化合物（I）的有用中间体。化合物 (I) 可应用于人类和/或兽医领域。
• UTILIZATION OF ARYL(OR HETEROARYL)AZOLYLCARBINOL DERIVATIVES IN THE PREPARATION OF A MEDICAMENT FOR THE TREATMENT OF TROUBLES MEDIATED BY AN EXCESS OF SUBSTANCE P
  申请人：LABORATORIOS DEL DR. ESTEVE, S.A.

  公开号：EP1103243A2

  公开（公告）日：2001-05-30

  The derivatives of aryl(or heteroaryl)azolylcarbinol (I) wherein Ar is optionally substituted phenyl or thienyl, R1 is a hydrogen atom, a cyclohexyl group, N-methylpiperidyl group, phenyl group, vinyl group or C1-C4 alkyl group; R2 is H, dialkylaminoalkyl, alkylazaheterocycloalkyl or azaheterocyclylalkyl and Het is a nitrogenated aromatic heterocycle of 5 members which contains from 1 to 3 nitrogen atoms and is optionally substituted, are useful for the treatment of troubles which are mediated by an excess of substance P, specially certain troubles of the central nervous system such as anxiety, depression, schizophrenia, maniaco-depressive psychosis, sexual dysfunction, drug addiction, cognitive troubles, locomotion troubles, etc. in mammals, including human beings.

  芳基(或杂芳基)偶氮基甲醇的衍生物(I) 其中 Ar 是任选取代的苯基或噻吩基，R1 是氢原子、环己基、N-甲基哌啶基、苯基、乙烯基或 C1-C4 烷基；R2 是 H、二烷基氨基烷基、烷基杂环烷基或杂环烷基，Het 是含有 1 至 3 个氮原子并被任选取代的 5 个成员的氮化芳香杂环，可用于治疗由过量 P 物质介导的疾病，特别是中枢神经系统的某些疾病，如焦虑症、抑郁症、精神分裂症、躁狂抑郁性精神病、性功能障碍、药物成瘾、认知障碍、运动障碍等。等。
• Active substance combination comprising a carbinol composition and an opioid
  申请人：LABORATORIOS DEL DR. ESTEVE, S.A.

  公开号：EP1584335A2

  公开（公告）日：2005-10-12

  The present invention relates to an active substance combination comprising at least one substituted carbinol compound and at least one opioid, a medicament comprising said active substance combination, a pharmaceutical formulation comprising said active substance combination and the use of said active substance combination for the manufacture of a medicament.

  本发明涉及一种由至少一种取代的甲醇化合物和至少一种阿片类药物组成的活性物质组合、一种由所述活性物质组合组成的药物、一种由所述活性物质组合组成的药物制剂以及使用所述活性物质组合制造药物。
• Derivatives of aryl (or heteroaryl) azolylcarbinols (in particular cizolirtin citrate) for the treatment of opioid addiction
  申请人：Laboratorios Dr. Esteve S.A.

  公开号：EP1632227A1

  公开（公告）日：2006-03-08

  The present invention refers to the use of derivatives of aryl (or heteroaryl) azolylcarbinols of general formula (I), and their physiologically acceptable salts, as medicinal products for human and/or animal therapeutics for the treatment of the symptoms of central neuropathic pain, especially certain subtypes of central neuropathic pain, as well as treatment of the disease causing the symptoms, the prevention or the prophylaxis of the symptoms of central neuropathic pain, especially certain subtypes of central neuropathic pain, as well as the prevention or the prophylaxis of the disease causing the symptoms. The preferred compound is Cizolirtin Citrate.

  本发明是指将通式（I）的芳基（或杂芳基）唑基甲醇的衍生物及其生理上可接受的盐类作为人类和/或动物治疗的药物产品，用于治疗中枢神经病理痛的症状，尤其是某些亚型的中枢神经病理痛，以及治疗引起中枢神经病理痛症状的疾病，预防中枢神经病理痛的症状，尤其是某些亚型的中枢神经病理痛、特别是某些亚型的中枢神经病理痛，以及治疗引起症状的疾病，预防中枢神经病理痛的症状，特别是某些亚型的中枢神经病理痛，以及预防引起症状的疾病。首选化合物是枸橼酸西唑利汀。
• Derivatives of aryl (or heteroaryl) azolylcarbinols for the treatment of central neuropathic pain
  申请人：Laboratorios Dr. Esteve S.A.

  公开号：EP1642577A1

  公开（公告）日：2006-04-05

  The present invention refers to the use of derivatives of aryl (or heteroaryl) azolylcarbinols of general formula (I), and their physiologically acceptable salts, as medicinal products for human and/or animal therapeutics for the treatment of the symptoms of central neuropathic pain, especially certain subtypes of central neuropathic pain, as well as treatment of the disease causing the symptoms, the prevention or the prophylaxis of the symptoms of central neuropathic pain, especially certain subtypes of central neuropathic pain, as well as the prevention or the prophylaxis of the disease causing the symptoms.

  本发明是指将通式（I）的芳基（或杂芳基）唑基甲醇的衍生物及其生理上可接受的盐类作为人类和/或动物治疗的药物产品，用于治疗中枢神经病理痛的症状，尤其是某些亚型的中枢神经病理痛，以及治疗引起中枢神经病理痛症状的疾病，预防中枢神经病理痛的症状，尤其是某些亚型的中枢神经病理痛、特别是某些亚型的中枢神经病理痛，以及治疗引起症状的疾病，预防中枢神经病理痛的症状，特别是某些亚型的中枢神经病理痛，以及预防引起症状的疾病。