他扎朵林 | 87936-76-3

• 分子结构分类: 有机化合物 - 苯类化合物 - 苯和取代衍生物
• 中文名称: 他扎朵林
• 英文名称: Tazadolene
• 英文别名: 1-[(2E)-2-benzylidenecyclohexyl]azetidine
• CAS: 87936-76-3；87936-75-2；87936-77-4
• 化学式: C₁₆H₂₁N
• 分子量: 227.34
• InChiKey: DOWWDQZIFWLREB-FYWRMAATSA-N

物化性质

• 沸点：
  347.7±21.0 °C(Predicted)
• 密度：
  1.082±0.06 g/cm3(Predicted)

计算性质

• 辛醇/水分配系数(LogP)：
  3.5
• 重原子数：
  17
• 可旋转键数：
  2
• 环数：
  3.0
• sp3杂化的碳原子比例：
  0.5
• 拓扑面积：
  3.2
• 氢给体数：
  0
• 氢受体数：
  1

反应信息

• 作为产物：
  描述：

  (E)-2-(phenylmethylene)cyclohexanamine 、 1,3-二溴丙烷 生成 他扎朵林
  参考文献：
  名称：

  SZMUSZKOVICZ, J.

  摘要：

  DOI：

文献信息

• Pharmaceutical preparation comprising an active dispersed on a matrix
  申请人：——

  公开号：US20040058896A1

  公开（公告）日：2004-03-25

  The present invention relates to the field of pharmaceutical technology and describes a novel advantageous preparation for an active ingredient. The novel preparation is suitable for producing a large number of pharmaceutical dosage forms. In the new preparation an active ingredient is present essentially uniformly dispersed in an excipient matrix composed of one or more excipients selected from the group of fatty alcohol, triglyceride, partial glyceride and fatty acid ester.

  本发明涉及制药技术领域，描述了一种新的有利的活性成分制备方法。这种新的制备方法适用于生产大量的药物剂型。在这种新的制备方法中，活性成分基本上均匀地分散在由脂肪醇、甘油三酯、部分甘油酯和脂肪酸酯等多种赋形剂中选择的一种或多种赋形剂组成的赋形剂基质中。
• Nitrate prodrugs able to release nitric oxide in a controlled and selective way and their use for prevention and treatment of inflammatory, ischemic and proliferative diseases
  申请人：Scaramuzzino, Giovanni

  公开号：EP1336602A1

  公开（公告）日：2003-08-20

  New pharmaceutical compounds of general formula (I): F-(X)q where q is an integer from 1 to 5, preferably 1; -F is chosen among drugs described in the text, -X is chosen among 4 groups -M, -T, -V and -Y as described in the text. The compounds of general formula (I) are nitrate prodrugs which can release nitric oxide in vivo in a controlled and selective way and without hypotensive side effects and for this reason they are useful for the preparation of medicines for prevention and treatment of inflammatory, ischemic, degenerative and proliferative diseases of musculoskeletal, tegumental, respiratory, gastrointestinal, genito-urinary and central nervous systems.

  通式（I）的新药物化合物：F-（X）q，其中q是1到5的整数，最好是1；-F是在文本中描述的药物中选择的，-X是在文本中描述的4个组-M，-T，-V和-Y中选择的。通式（I）的化合物是硝酸盐前药，可以在体内以受控和选择性的方式释放一氧化氮，而不会产生降压副作用，因此它们非常适用于制备用于预防和治疗肌肉骨骼，皮肤，呼吸，消化，泌尿和中枢神经系统的炎症，缺血，退行性和增生性疾病的药物。
• 2-(Phenylmethylene)cycloalkyl-azetidines
  申请人：The Upjohn Company

  公开号：US04652559A1

  公开（公告）日：1987-03-24

  2-(Phenylmethylene)cycloalkylamines and -azetidines of the formula ##STR1## and acid addition salts thereof, e.g., 1-[2-(phenylmethylene)cyclohexyl]azetidine, and related compounds, which have analgesic, antidepressant and mixed analgesic/antidepressant central nervous system (CNS) activities, and which are useful in treating pain and/or depression in mammals including humans. The invention provides processes for preparing the compounds as well as compositions containing the compounds and methods for using the compounds as analgesic and/or antidepressant drugs for humans and valuable mammalian animals.

  本发明涉及公式为##STR1##的2-(苯亚甲基)环烷胺和-氮杂环烷化合物及其酸加成盐，例如1-[2-(苯亚甲基)环己基]氮杂环烷和相关化合物。这些化合物具有镇痛、抗抑郁和混合镇痛/抗抑郁中枢神经系统(CNS)活性，并且对于治疗哺乳动物包括人类的疼痛和/或抑郁有用。本发明提供制备这些化合物的方法以及含有这些化合物的组合物和使用这些化合物作为人类和有价值的哺乳动物的镇痛和/或抗抑郁药物的方法。
• Diagnostic/therapeutic agents
  申请人：Klaveness Jo

  公开号：US20050002865A1

  公开（公告）日：2005-01-06

  Targetable diagnostic and/or therapeutically active agents, e.g. ultrasound contrast agents, comprising a suspension in an aqueous carrier liquid of a reporter comprising gas-containing or gas-generating material, said agent being capable of forming at least two types of binding pairs with a target.

  可定位的诊断和/或治疗活性剂，例如超声对比剂，包括悬浮在水载体液中的报告物，该报告物包含含气体或生成气体的材料，该剂能够与目标形成至少两种结合对。
• 2-(Phenylmethylene)cycloalkylamines and -azetidines
  申请人：The Upjohn Company

  公开号：US04540690A1

  公开（公告）日：1985-09-10

  2-(Phenylmethylene)cycloalkylamines and -azetidines of the formula ##STR1## and acid addition salts thereof, e.g., 1-[2-(phenylmethylene)cyclohexyl]azetidine, and related compounds, which have analgesic, antidepressant and mixed analgesic/antidepressant central nervous system (CNS) activities, and which are useful in treating pain and/or depression in mammals including humans. The invention provides processes for preparing the compounds as well as compositions containing the compounds and methods for using the compounds as analgesic and/or antidepressant drugs for humans and valuable mammalian animals.

  本发明涉及公式为##STR1##的2-(苯亚甲基)环烷胺和-氮杂环烷化合物及其酸加成盐，例如1-[2-(苯亚甲基)环己基]氮杂环烷和相关化合物，其具有镇痛、抗抑郁和混合性镇痛/抗抑郁的中枢神经系统(CNS)活性，并且对于治疗哺乳动物包括人类的疼痛和/或抑郁症具有用途。本发明提供了制备该化合物的方法，以及含有该化合物的组合物和使用该化合物作为人类和有价值的哺乳动物的镇痛和/或抗抑郁药物的方法。