N-Boc-aminopentyl thiourea | 296270-64-9

• 分子结构分类: 有机化合物 - 有机酸及其衍生物 - 羧酸及其衍生物
• 英文名称: N-Boc-aminopentyl thiourea
• 英文别名: (5-thioureido-pentyl)-carbamic Acid tert-butyl Ester；tert-butyl N-[5-(carbamothioylamino)pentyl]carbamate
• CAS: 296270-64-9
• 化学式: C₁₁H₂₃N₃O₂S
• 分子量: 261.389
• InChiKey: SYQQSNJVINBWHS-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  1.3
• 重原子数：
  17
• 可旋转键数：
  8
• 环数：
  0.0
• sp3杂化的碳原子比例：
  0.82
• 拓扑面积：
  109
• 氢给体数：
  3
• 氢受体数：
  3

反应信息

• 作为反应物：
  描述：

  N-Boc-aminopentyl thiourea 在 三乙胺 、 三氟乙酸 作用下， 以 乙醇 、 二氯甲烷 为溶剂， 生成 2-[5-(Dimethylsulfamoylamino)pentylamino]-4-pyridin-2-yl-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
• 作为产物：
  描述：

  N-(5-氨基戊基)氨基甲酸叔丁酯 在 potassium carbonate 作用下， 以 四氢呋喃 、 甲醇 、 水 为溶剂， 生成 N-Boc-aminopentyl thiourea
  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

• THIAZOLE DERIVATIVES
  申请人：——

  公开号：US20030225141A1

  公开（公告）日：2003-12-04

  Compounds of formula I are provided 1 as well as pharmaceutically acceptable salts and esters thereof, wherein R 1 to R 5 , n, m and A have the significance disclosed in the specification, and can be used for the treatment or prevention of arthritis, cardiovascular diseases, diabetes, renal failure, eating disorders and obesity.

  提供了式I的化合物，以及其药学上可接受的盐和酯，其中R1至R5，n，m和A的含义如规范中所披露的那样，并可用于治疗或预防关节炎、心血管疾病、糖尿病、肾衰竭、进食障碍和肥胖症。
• [EN] THIAZOLE DERIVATIVES AS NPY RECEPTOR ANTAGONISTS<br/>[FR] DERIVES THIAZOLES UTILISES COMME ANTAGONISTES DU RECEPTEUR NPY
  申请人：HOFFMANN LA ROCHE

  公开号：WO2003072577A1

  公开（公告）日：2003-09-04

  Compounds of formula (I) as well as pharmaceutically acceptable salts and esters thereof, wherein R1 to R5, n, m and A have the significance given in claim 1, can be used in the form of pharmaceutical preparations for the treatment or prevention of arthritis, cardiovascular diseases, diabetes, renal failure, eating disorders and obesity.

  公式（I）的化合物，以及其药学上可接受的盐和酯，其中R1到R5，n，m和A的含义如权利要求书1所述，可以用作制备药物治疗或预防关节炎，心血管疾病，糖尿病，肾衰竭，进食障碍和肥胖症。
• Selective NPY (Y5) antagonists
  申请人：Marzabadi R. Mohammad

  公开号：US20050137240A1

  公开（公告）日：2005-06-23

  This invention is directed to bicyclic and tricyclic compounds which are selective antagonists for NPY (Y5) receptors. 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. The 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. This 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.

  本发明涉及选择性拮抗NPY（Y5）受体的双环和三环化合物。本发明提供一种制药组合物，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合而成的制药组合物。本发明还提供了制备制药组合物的方法，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用于治疗异常状态的制药组合物，其中减少人类Y5受体活性可缓解该异常状态。
• Thiazole derivatives
  申请人：Hoffmann-La Roche Inc.

  公开号：US06686381B2

  公开（公告）日：2004-02-03

  Compounds of formula I are provided as well as pharmaceutically acceptable salts and esters thereof, wherein R1 to R5, n, m and A have the significance disclosed in the specification, and can be used for the treatment or prevention of arthritis, cardiovascular diseases, diabetes, renal failure, eating disorders and obesity.

  提供了I式化合物及其药学上可接受的盐和酯，其中R1至R5、n、m和A具有规范中披露的意义，可用于治疗或预防关节炎、心血管疾病、糖尿病、肾功能衰竭、进食障碍和肥胖症。
• 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。