Talipexole hydrochloride | 36085-73-1

• 物质功能分类: 有机原料 - 羧酸类化合物及衍生物
• 分子结构分类: 有机化合物 - 有机杂环化合物 - 吖庚因类
• 英文名称: Talipexole hydrochloride
• 英文别名: 6-prop-2-enyl-4,5,7,8-tetrahydro-[1,3]thiazolo[4,5-d]azepin-2-amine;hydrochloride
• CAS: 36085-73-1
• 化学式: C10H16ClN3S
• 分子量: 245.77
• InChiKey: AFOGLDDNZFXNPQ-UHFFFAOYSA-N

物化性质

• 熔点：
  245°C dec.
• 溶解度：
  H2O: >20 mg/mL
• 稳定性/保质期：

  常规情况下不会分解，没有危险反应。

计算性质

• 辛醇/水分配系数(LogP)：
  1.73
• 重原子数：
  15
• 可旋转键数：
  2
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.5
• 拓扑面积：
  70.4
• 氢给体数：
  2
• 氢受体数：
  4

安全信息

• 危险品标志：
  Xn
• 危险类别码：
  R22
• 海关编码：
  2934999090
• 危险性防范说明：
  P280,P305+P351+P338
• 危险性描述：
  H302

制备方法与用途

生物活性

Talipexole dihydrochloride（B-HT 920 dihydrochloride）是一种多巴胺D2受体和α2-肾上腺素受体激动剂，同时是5-HT3受体拮抗剂，具有抗帕金森病活性。

	IC50值（nM）
α2	25
D2受体	-
5-HT3受体	-

体内研究

给猫静脉注射30微克/公斤的Talipexole dihydrochloride（B-HT 920）后，最初导致血压升高，随后则出现长时间的血压和心率下降。在β-肾上腺素能阻断的狗中，通过颈动脉注入血管紧张素引发的迷走神经反射性心动过缓被Talipexole dihydrochloride（B-HT 920）10微克/公斤的硬脑膜内注射所增强。

文献信息

• BICYCLIC COMPOUNDS AND USE AS ANTIDIABETICS
  申请人：Fang Jing

  公开号：US20100029650A1

  公开（公告）日：2010-02-04

  The present invention relates to novel compounds that are useful in the treatment of metabolic disorders, particularly type II diabetes mellitus and related disorders, and also to the methods for the making and use of such compounds.

  本发明涉及一种新型化合物，该化合物在治疗代谢性疾病，特别是Ⅱ型糖尿病及相关疾病方面具有用途，并且还涉及制备和使用这种化合物的方法。
• THERAPEUTIC AGENT FOR PSYCHONEUROTIC DISEASE
  申请人：ONO PHARMACEUTICAL CO., LTD.

  公开号：EP1787657A1

  公开（公告）日：2007-05-23

  The present invention relates to a preventive and/or therapeutic agent for psychoneurotic diseases, comprising an EP3 antagonist represented by the general formula (I): (wherein the meanings of characters are defined in the description). This compound has an antagonistic potency against EP3 and exhibits efficacy through unusual action mechanism as a preventive and/or therapeutic agent for psychoneurotic disorder, psychosomatic disorder, anxiety disorder, depression and disorder caused by stress.

  本发明涉及一种预防和/或治疗心神经疾病的药剂，包括一种由一般公式(I)表示的EP3拮抗剂：（其中字符的含义在描述中定义）。该化合物具有对EP3的拮抗作用，通过不寻常的作用机制作为一种预防和/或治疗心神经紊乱、心身疾病、焦虑症、抑郁症以及由压力引起的疾病的药剂展现出疗效。
• NOVEL PYRAZOLE DERIVATIVE
  申请人：MOCHIDA PHARMACEUTICAL CO., LTD.

  公开号：US20140378447A1

  公开（公告）日：2014-12-25

  It has been desired to develop a pharmaceutical composition, which is used in agents for preventing and/or treating various diseases related to PDE10 (e.g. mental disorder and neurodegenerative disorder). The present invention provides: compounds having PDE10 inhibitory effect, in particular, compounds having a 4-heteroarylpyrazole-5-carboxylic acid amide structure represented by the following formula (I), or their pharmaceutically acceptable salts, or their solvates; pharmaceutical compositions comprising, as active ingredients, the compounds, or their pharmaceutically acceptable salts, or their solvates; and medical use of the compounds, or their pharmaceutically acceptable salts, or their solvates.

  已经有人希望开发一种药物组合物，用于预防和/或治疗与PDE10相关的各种疾病（例如精神障碍和神经退行性疾病）。本发明提供：具有PDE10抑制作用的化合物，特别是具有以下式（I）所代表的4-杂环芳基吡唑-5-羧酰胺结构的化合物，或其药学上可接受的盐，或其溶剂化物；包含作为活性成分的化合物，或其药学上可接受的盐，或其溶剂化物的药物组合物；以及化合物的医学用途，或其药学上可接受的盐，或其溶剂化物。
• [EN] HYDANTOIN DERIVATIVE<br/>[FR] DÉRIVÉ D'HYDANTOÏNE
  申请人：ONO PHARMACEUTICAL CO

  公开号：WO2021043245A1

  公开（公告）日：2021-03-11

  A compound represented by general formula (I-a) : has a strong DDR1 inhibitory activity, and can be a therapeutic agent for DDR1-related diseases, for example, a cancer, a kidney disease, a cardiovascular disease, a central nervous system disease, or fibrosis.

  一种由一般化学式（I-a）表示的化合物具有强大的DDR1抑制活性，可作为DDR1相关疾病的治疗药物，例如癌症、肾脏疾病、心血管疾病、中枢神经系统疾病或纤维化病。
• Glucopyranosyloxypyrazole derivatives and use thereof in medicines
  申请人：Fujikura Hideki

  公开号：US20060094667A1

  公开（公告）日：2006-05-04

  The present invention provides glucopyranosyloxypyrazole derivatives represented by the general formula: wherein R represents a hydrogen atom, a lower alkyl group or a group forming a prodrug;.one of Q and T represents a group represented by the general formula: (wherein P represents a hydrogen atom or a group forming a prodrug), while the other represents a lower alkyl group or a halo(lower alkyl) group; R 2 represents a hydrogen atom, a lower alkyl group, a lower alkoxy group, a lower alkylthio group, a halo (lower alkyl) group or a halogen atom; and with the proviso that P does not represent a hydrogen atom when R represents a hydrogen atom or a lower alkyl group, or pharmaceutically acceptable salts thereof, which exert an inhibitory activity in human SGLT2 and have an improved oral absorption, and therefore are useful as agents for the prevention or treatment of a disease associated with hyperglycemia such as diabetes, diabetic complications or obesity, and pharmaceutically acceptable salts thereof, and pharmaceutical uses thereof.

  本发明提供了由下式表示的葡萄糖吡唑衍生物： 其中，R表示氢原子，低级烷基或形成前药的基团；Q和T中的一个表示由下式表示的基团： （其中，P表示氢原子或形成前药的基团），而另一个表示低级烷基或卤代（低级烷基）基团；R2表示氢原子，低级烷基，低级烷氧基，低级烷基硫基，卤代（低级烷基）基团或卤素原子；但要注意，当R表示氢原子或低级烷基时，P不表示氢原子。本发明的衍生物在人体SGLT2中具有抑制活性，并具有改善口服吸收，因此可用作预防或治疗与高血糖有关的疾病，如糖尿病、糖尿病并发症或肥胖症的药物，以及其药学上可接受的盐和药物用途。