4-Pyridin-2-yl-2-[5-(sulfamoylamino)pentylamino]-1,3-thiazole | 304008-04-6

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 唑类
• 英文名称: 4-Pyridin-2-yl-2-[5-(sulfamoylamino)pentylamino]-1,3-thiazole
• CAS: 304008-04-6
• 化学式: C₁₃H₁₉N₅O₂S₂
• 分子量: 341.458
• InChiKey: MVIHVFVEMJXOIS-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  1.4
• 重原子数：
  22
• 可旋转键数：
  9
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.38
• 拓扑面积：
  147
• 氢给体数：
  3
• 氢受体数：
  8

反应信息

• 作为产物：
  描述：

  2-[5-(Dimethylsulfamoylamino)pentylamino]-4-pyridin-2-yl-1,3-thiazole 在 氨 作用下， 以 1,4-二氧六环 为溶剂， 反应 24.0h， 生成 4-Pyridin-2-yl-2-[5-(sulfamoylamino)pentylamino]-1,3-thiazole
  参考文献：
  名称：

  5-(2′-Pyridyl)-2-aminothiazoles: Alkyl amino sulfonamides and sulfamides as potent NPY5 antagonists

  摘要：

  Synthesis, SAR and physico-chemical properties of an alkyl aminothiazole series 8 and 16 are described. 2-Pyridylaminothiazole based compounds such as 8c and 16a exhibit high affinity at the NPY5 receptor with desirable cLogPs and solubilities. However, they also suffer from high in vitro and in vivo clearance. Compound 16a partially inhibits the feeding behavior elicited by i.c.v. injection of the selective NPY5 agonist [cPP(1-7), NPY19-23, Ala(31), Aib(32), Gln(34)]-human pancreatic polypeptide polypeptide (cPP). (C) 2011 Elsevier Ltd. All rights reserved.

  DOI：

  10.1016/j.bmcl.2011.08.072

文献信息

• Selective NPY (Y5) antagonists
  申请人：Marzabadi R. Mohammad

  公开号：US20080045524A1

  公开（公告）日：2008-02-21

  This invention is directed to triazine derivatives, bicyclic compounds and tricyclic compounds which are selective antagonists for a NPY (Y5) receptor. The invention provides a pharmaceutical composition comprising a therapeutically effective amount of a compound of the invention and a pharmaceutically acceptable carrier. This invention provides a pharmaceutical composition made by combining a therapeutically effective amount of a compound of this invention and a pharmaceutically acceptable carrier. This invention provides a process for making a pharmaceutical composition comprising combining a therapeutically effective amount of a compound of the invention and a pharmaceutically acceptable carrier. The invention further provides the use of a compound of the invention for the preparation of a pharmaceutical composition for treating an abnormality, wherein the abnormality is alleviated by decreasing the activity of a human Y5 receptor.

  本发明涉及三嗪衍生物、双环化合物和三环化合物，它们是选择性抗NPY（Y5）受体的拮抗剂。本发明提供了一种药物组合物，包括本发明化合物的治疗有效量和药学上可接受的载体。本发明提供了一种由本发明化合物的治疗有效量和药学上可接受的载体组成的药物组合物。本发明提供了一种制备药物组合物的方法，包括将本发明化合物的治疗有效量和药学上可接受的载体组合。本发明进一步提供了使用本发明化合物制备药物组合物，用于治疗异常情况，其中通过降低人类Y5受体的活性来缓解异常情况。
• TRIAZINE DERIVATIVES FOR USE AS SELECTIVE NPY (Y5) ANTAGONISTS
  申请人：H. LUNDBECK A/S

  公开号：EP1816127A1

  公开（公告）日：2007-08-08

  This invention is directed to triazine derivatives, bicyclic compounds and tricyclic compounds which are selective antagonists for a NPY (Y5) receptor. The invention provides a pharmaceutical composition comprising a therapeutically effective amount of a compound of the invention and a pharmaceutically acceptable carrier. This invention provides a pharmaceutical composition made by combining a therapeutically effective amount of a compound of this invention and a pharmaceutically acceptable carrier. This invention provides a process for making a pharmaceutical composition comprising combining a therapeutically effective amount of a compound of the invention and a pharmaceutically acceptable carrier. The invention further provides the use of a compound of the invention for the preparation of a pharmaceutical composition for treating an abnormality, wherein the abnormality is alleviated by decreasing the activity of a human Y5 receptor.

  本发明涉及三嗪衍生物、双环化合物和三环化合物，它们是 NPY（Y5）受体的选择性拮抗剂。本发明提供了一种药物组合物，其中包含治疗有效量的本发明化合物和药学上可接受的载体。本发明提供了一种由治疗有效量的本发明化合物和药学上可接受的载体组合而成的药物组合物。本发明提供了一种制备药物组合物的工艺，该工艺包括将治疗有效量的本发明化合物与药学上可接受的载体相结合。本发明进一步提供了本发明化合物用于制备治疗异常的药物组合物的用途，其中通过降低人Y5受体的活性来缓解异常。
• US7189720B2
  申请人：——

  公开号：US7189720B2

  公开（公告）日：2007-03-13
• 5-(2′-Pyridyl)-2-aminothiazoles: Alkyl amino sulfonamides and sulfamides as potent NPY5 antagonists
  作者：Mathivanan Packiarajan、Heather Coate、Mahesh Desai、Hermogenes N. Jimenez、Emily J. Reinhard、Vrej J. Jubian、Mohammad R. Marzabadi、Gamini Chandrasena、Toni C. Wolinski、Mary W. Walker、Kim Andersen

  DOI：10.1016/j.bmcl.2011.08.072

  日期：2011.11

  Synthesis, SAR and physico-chemical properties of an alkyl aminothiazole series 8 and 16 are described. 2-Pyridylaminothiazole based compounds such as 8c and 16a exhibit high affinity at the NPY5 receptor with desirable cLogPs and solubilities. However, they also suffer from high in vitro and in vivo clearance. Compound 16a partially inhibits the feeding behavior elicited by i.c.v. injection of the selective NPY5 agonist [cPP(1-7), NPY19-23, Ala(31), Aib(32), Gln(34)]-human pancreatic polypeptide polypeptide (cPP). (C) 2011 Elsevier Ltd. All rights reserved.