5-Methyl-2-phenyl-4,5,6,7-tetrahydro-thiazol<5,4-c>pyridin | 96635-29-9

• 分子结构分类: 有机化合物 - 有机氮化合物
• 英文名称: 5-Methyl-2-phenyl-4,5,6,7-tetrahydro-thiazol<5,4-c>pyridin
• 英文别名: 5-methyl-2-phenyl-4,5,6,7-tetrahydro-thiazolo[5,4-c]pyridine；5-methyl-2-phenyl-6,7-dihydro-4H-[1,3]thiazolo[5,4-c]pyridine
• CAS: 96635-29-9
• 化学式: C₁₃H₁₄N₂S
• 分子量: 230.334
• InChiKey: UGYOGUSZINTLDZ-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  2.6
• 重原子数：
  16
• 可旋转键数：
  1
• 环数：
  3.0
• sp3杂化的碳原子比例：
  0.31
• 拓扑面积：
  44.4
• 氢给体数：
  0
• 氢受体数：
  3

反应信息

• 作为反应物：
  描述：

  5-Methyl-2-phenyl-4,5,6,7-tetrahydro-thiazol<5,4-c>pyridin 、 富马酸 以 甲醇 为溶剂， 以0.24 g的产率得到5-methyl-2-phenyl-4,5,6,7-tetrahydrothiazole[5,4-c]pyridine fumarate
  参考文献：
  名称：

  New thiazole derivatives as potent and selective 5-hydroxytriptamine 3 (5-HT 3 ) receptor agonists for the treatment of constipation

  摘要：

  The syntheses and biological evaluation of a series of novel indeno[1,2-d]thiazole derivatives are described. Several groups reported 5-HT3 receptor agonists which were mainly evaluated for their activities on the von Bezold-Jarisch reflex (B-J reflex). We discovered that tetrahydrothiazolopyridine derivative 1b had a contractile effect on the isolated guinea pig colon with weak B-J reflex. Our efforts to find a new type of 5-HT3 receptor agonists on the isolated guinea pig colon focused on the synthesis of a fused thiazole derivative 1d modified from 1b and reverse-fused thiazole derivatives (7-10). In this series, 10f (YM-31636) showed high affinity and selectivity for the cloned human 5-HT3 receptor; furthermore, it showed potent and selective 5-HT3 receptor agonistic activity. YM-31636 was examined for its effects on defecation in animals, thus evaluating the compound as an agent against constipation. (C) 2003 Elsevier Science Ltd. All rights reserved.

  DOI：

  10.1016/s0968-0896(02)00557-6
• 作为产物：
  描述：

  4-(2-Chlorethyl)-2-phenyl-thiazol 在 甲酸 作用下， 以 xylene 为溶剂， 反应 22.0h， 生成 5-Methyl-2-phenyl-4,5,6,7-tetrahydro-thiazol<5,4-c>pyridin
  参考文献：
  名称：

  Palazzo,G.; Tavella,M., Gazzetta Chimica Italiana, 1962, vol. 92, p. 1084 - 1092

  摘要：

  DOI：

文献信息

• NOVEL (HETEROCYCLE/CONDENSED PIPERIDINE)-(PIPERAZINYL)-1-ALKANONE OR (HETEROCYCLE/CONDENSED PYRROLIDINE)-(PIPERAZINYL)-1-ALKANONE DERIVATIVES AND USE THEREOF AS p75 INHIBITORS
  申请人：BARONI Marco

  公开号：US20120245149A1

  公开（公告）日：2012-09-27

  The disclosure relates to (heterocycle-fused piperidine)-(piperazinyl)-1-alkanone derivatives and (heterocycle-fused pyrrolidine)-(piperazinyI)-1-alkanone derivatives of formula (I): wherein A, W, R2 and n are as defined in the disclosure, to the method of preparation thereof and the therapeutic use thereof.

  该公开涉及到式(I)的(杂环融合哌啶)-(哌嗪基)-1-烷酮衍生物和(杂环融合吡咯啉)-(哌嗪基)-1-烷酮衍生物： 其中A、W、R2和n如公开所定义，以及其制备方法和治疗用途。
• EP2513108B1
  申请人：——

  公开号：EP2513108B1

  公开（公告）日：2015-04-01
• US8580790B2
  申请人：——

  公开号：US8580790B2

  公开（公告）日：2013-11-12
• US8957211B2
  申请人：——

  公开号：US8957211B2

  公开（公告）日：2015-02-17
• [EN] AMIDE COMPOUNDS<br/>[FR] COMPOSÉS AMIDÉS
  申请人：TAKEDA PHARMACEUTICAL

  公开号：WO2008011130A2

  公开（公告）日：2008-01-24

  (EN) The present invention provides compounds represented by the formula (Ie) and the formula (If) wherein each symbol is as defined in the specification. According to the present invention, these compounds have a DGAT inhibitory activity and are useful for the prophylaxis, treatment or improvement of diseases or pathologies caused by high expression or high activation of DGAT.(FR) La présente invention concerne des composés représentés par la formule (Ie) ou la formule (If) dans lesquelles chaque symbole est tel que défini dans le mémoire descriptif. Selon la présente invention, ces composés ont une activité inhibitrice de la DGAT et ils sont utilisables pour la prophylaxie, le traitement ou l'amélioration de maladies ou de pathologies causées par la sur-expression ou la sur-activation de la DGAT.