4-hydrazinotetrahydrothiopyrane | 1374652-09-1

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 噻烷
• 英文名称: 4-hydrazinotetrahydrothiopyrane
• 英文别名: (tetrahydro-2H-thiopyran-4-yl)hydrazine hydrochloride；(tetrahydro-2H-thiopyran-4-yl)hydrazine hydrogen chloride；4-hydrazinotetrahydrothiopyran hydrochloride；Hydron;thian-4-ylhydrazine;chloride；hydron;thian-4-ylhydrazine;chloride
• CAS: 1374652-09-1
• 化学式: C₅H₁₂N₂S*ClH
• 分子量: 168.691
• InChiKey: GKVKKLXPZUFGAC-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  0.77
• 重原子数：
  9
• 可旋转键数：
  1
• 环数：
  1.0
• sp3杂化的碳原子比例：
  1.0
• 拓扑面积：
  63.4
• 氢给体数：
  3
• 氢受体数：
  4

安全信息

• 危险性防范说明：
  P261,P280,P301+P312,P302+P352,P305+P351+P338
• 危险性描述：
  H302,H315,H319,H335

反应信息

• 作为反应物：
  描述：

  4-hydrazinotetrahydrothiopyrane 在 N,N-二异丙基乙胺 、 sodium hydroxide 作用下， 以 四氢呋喃 、 乙醇 为溶剂， 反应 18.0h， 生成 6-chloro-1-(tetrahydro-2H-thiopyran-4-yl)-1,5-dihydro-4H-pyrazolo[3,4-d]pyrimidin-4-one
  参考文献：
  名称：

  EP3892623

  摘要：

  公开号：
• 作为产物：
  描述：

  tert-butyl 2-(tetrahydro-4H-thiopyran-4-ylidene)hydrazine-1-carboxylate 在 盐酸 、 sodium cyanoborohydride 、 溶剂黄146 作用下， 以 1,4-二氧六环 为溶剂， 反应 5.0h， 生成 4-hydrazinotetrahydrothiopyrane
  参考文献：
  名称：

  [EN] ANNULATED GLYCOSIDASE INHIBITORS
  [FR] INHIBITEURS DE GLYCOSIDASES ANNELÉS

  摘要：

  式（I）中A、R、W1、W2、W3、W4、W5、W6、L、Q、Rx和u的含义如权利要求书中所述，可用于治疗tau病和阿尔茨海默病。

  公开号：

  WO2019037861A1

文献信息

• COMPOUNDS HAVING PDE9A INHIBITORY ACTIVITY, AND PHARMACEUTICAL USES THEREOF
  申请人：Korea Research Institute of Chemical Technology

  公开号：EP3892622A1

  公开（公告）日：2021-10-13

  The present invention provides a compound having a specific chemical structure and having PDE9A inhibitory activity, or a pharmaceutically acceptable salt thereof. The present invention provides a composition containing the compound or a pharmaceutically acceptable salt thereof. The present invention provides a pharmaceutical use, for treating or preventing PDE9A-related diseases, of the compound according to the present invention, a salt thereof, and a composition containing the compound or salt. The present invention also provides a method for treating or preventing PDE9A-related diseases, the method comprising administering an effective amount of the compound according to the present invention, a salt thereof, or a composition containing the compound or salt to a subject in need of treatment.

  本发明提供了一种具有特定化学结构并具有 PDE9A 抑制活性的化合物或其药学上可接受的盐。本发明提供了一种含有该化合物或其药学上可接受的盐的组合物。本发明提供了根据本发明的化合物、其盐和含有该化合物或盐的组合物的药物用途，用于治疗或预防 PDE9A 相关疾病。本发明还提供了一种治疗或预防PDE9A相关疾病的方法，该方法包括向需要治疗的受试者施用有效量的根据本发明的化合物、其盐或含有该化合物或盐的组合物。
• Tetrahydrothiopy ranphthalazinone derivatives as PDE4 inhibitors
  申请人：Altana Pharma AG

  公开号：US20030166655A1

  公开（公告）日：2003-09-04

  The compounds of formula (I) in which R1, R2, A and Ar have the meanings as given in the description are novel effective PDE4 inhibitors.

  式（I）化合物中 R1、R2、A 和 Ar 的含义如描述中所给。
• EP3892622
  申请人：——

  公开号：——

  公开（公告）日：——
• Novel Selective PDE4 Inhibitors. 3. <i>In Vivo</i> Antiinflammatory Activity of a New Series of N-Substituted <i>cis</i>-Tetra- and <i>cis</i>-Hexahydrophthalazinones
  作者：Margaretha Van der Mey、Hildegard Boss、Armin Hatzelmann、Ivonne J. Van der Laan、Geert J. Sterk、Hendrik Timmerman

  DOI：10.1021/jm0110340

  日期：2002.6.1

  The synthesis and biological activities of a series of N-substituted cis-4a,5,6,7,8,8a-hexa- and cis-4a, 5,8,8a-tetrahydro-2H-phthalazin-1-ones are described. It was found that compounds bearing a cycloalkyl group at the 2-position exhibit the highest PDE4 inhibitory activities (pIC(50) = 8.6-9.4). The N-cycloheptyl- and N-adamantanyltetrahydrophthalazinones (7h, 8, 10, 11) show high in vivo antiinflammatory activities after oral application. Additionally, some phthalazinones were found to exhibit potent suppression of LPS-induced TNFalpha release and show moderate potency against fMLP-stimulated production of ROS.
• TETRAHYDROTHIOPY RANPHTHALAZINONE DERIVATIVES AS PDE4 INHIBITORS
  申请人：ALTANA Pharma AG

  公开号：EP1244654A1

  公开（公告）日：2002-10-02