(5CI)-噻唑并[4,5-c]吡啶-2-醇 | 857970-39-9

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 吡啶及其衍生物
• 中文名称: (5CI)-噻唑并[4,5-c]吡啶-2-醇
• 中文别名: 噻唑并[4,5-C]吡啶-2-醇
• 英文名称: 3H-thiazolo[4,5-c]pyridin-2-one
• 英文别名: 3H-Thiazolo[4,5-c]pyridin-2-on；Thiazolo[4,5-c]pyridin-2-ol；3H-[1,3]thiazolo[4,5-c]pyridin-2-one
• CAS: 857970-39-9
• 化学式: C₆H₄N₂OS
• mdl: MFCD16878302
• 分子量: 152.177
• InChiKey: JHQMMHCYMPQTRT-UHFFFAOYSA-N

物化性质

• 熔点：
  256 °C
• 密度：
  1.466±0.06 g/cm3(Predicted)

计算性质

• 辛醇/水分配系数(LogP)：
  0.6
• 重原子数：
  10
• 可旋转键数：
  0
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.0
• 拓扑面积：
  67.3
• 氢给体数：
  1
• 氢受体数：
  3

反应信息

• 作为产物：
  描述：

  3-氨基-4-吡啶硫醇 在 氢氧化钾 、 双氧水 作用下， 生成 (5CI)-噻唑并[4,5-c]吡啶-2-醇
  参考文献：
  名称：

  Takahashi et al., Pharmaceutical Bulletin, 1955, vol. 3, p. 356,359

  摘要：

  DOI：

文献信息

• Imaging Agents Useful for Identifying AD Pathology
  申请人：Kolb Hartmuth C.

  公开号：US20100098634A1

  公开（公告）日：2010-04-22

  Provided herein are compounds and compositions which comprise the formulae as disclosed herein, wherein the compound is an amyloid binding compound. An amyloid binding compound according to the invention may be administered to a patient in amounts suitable for in vivo imaging of amyloid deposits, and distinguish between neurological tissue with amyloid deposits and normal neurological tissue. Amyloid probes of the invention may be used to detect and quantitate amyloid deposits in diseases including, for example, Down's syndrome, familial Alzheimer's Disease. In another embodiment, the compounds may be used in the treatment or prophylaxis of neurodegenerative disorders. Also provided herein are methods of allowing the compound to distribute into the brain tissue, and imaging the brain tissue, wherein an increase in binding of the compound to the brain tissue compared to a normal control level of binding indicates that the mammal is suffering from or is at risk of developing a neurodegenerative disease.

  本文提供的化合物和组合物包含如下所述的公式，其中该化合物是一种淀粉样蛋白结合化合物。本发明的淀粉样蛋白结合化合物可以以适量的方式用于体内成像淀粉样沉积物，以区分含有淀粉样沉积物的神经组织和正常神经组织。本发明的淀粉样探针可以用于检测和定量测量包括唐氏综合症、家族性阿尔茨海默病在内的疾病中的淀粉样沉积物。在另一实施例中，这些化合物可以用于治疗或预防神经退行性疾病。本文还提供了一种使化合物分布到脑组织中并成像脑组织的方法，其中与正常结合水平相比，化合物与脑组织的结合增加表明哺乳动物正在患有或有发展神经退行性疾病的风险。
• ACETIC ACID AMIDE DERIVATIVE HAVING INHIBITORY ACTIVITY ON ENDOTHELIAL LIPASE
  申请人：Shionogi & Co., Ltd.

  公开号：US20140288302A1

  公开（公告）日：2014-09-25

  A pharmaceutical composition including a compound of formula (I): its pharmaceutically acceptable salt, or a solvate thereof. Ring A is nitrogen-containing hetero ring, Ring A may be substituted with a substituent other than a group represented by formula: —C(R 1 R 2 )—C(═O)—NR 3 R 4 and a group represented by formula: —R 5 , a broken line represents presence or absence of a bond, Z is —NR 6 —, ═N—, —O—, or —S—, R 6 is halogen or substituted or unsubstituted alkyl, R 1 and R 2 are each independently hydrogen, halogen, hydroxy, cyano, nitro, carboxy or substituted or unsubstituted alkyl, R 3 is hydrogen or substituted or unsubstituted alkyl, R 4 is hydrogen or substituted or unsubstituted alkyl, R 3 and R 4 taken together with the adjacent nitrogen atom to which they are attached may form a substituted or unsubstituted ring, R 5 is hydrogen, halogen, hydroxy, cyano, nitro, carboxy, substituted or unsubstituted alkyl, substituted or unsubstituted alkenyl, or substituted or unsubstituted alkynyl.

  一种包括化合物(I)的制药组合物：其药学上可接受的盐或其溶剂合物。环A是含氮杂环，环A可以用除了公式所表示的基团之外的取代基团取代：—C(R1R2)—C(═O)—NR3R4和公式表示的基团：—R5，其中断线表示键的存在或不存在，Z是—NR6—，═N—，—O—或—S—，R6是卤素或取代或未取代的烷基，R1和R2各自独立地是氢、卤素、羟基、氰基、硝基、羧基或取代或未取代的烷基，R3是氢或取代或未取代的烷基，R4是氢或取代或未取代的烷基，R3和R4与它们所连接的相邻氮原子一起可以形成取代或未取代的环，R5是氢、卤素、羟基、氰基、硝基、羧基、取代或未取代的烷基、取代或未取代的烯基或取代或未取代的炔基。
• ACETIC ACID AMIDE DERIVATIVE HAVING INHIBITORY ACTIVITY ON VASCULAR ENDOTHELIAL LIPASE
  申请人：Shionogi & Co., Ltd.

  公开号：EP2351744B1

  公开（公告）日：2015-01-07
• 3, 5-DISUBSTITUTED AND 3,5,7-TRISUBSTITUTED-3H-OXAZOLO AND 3H-THIAZOLO [4,5-d]PYRIMIDIN-2-ONE COMPOUNDS AND PRODRUGS THEREOF
  申请人：Anadys Pharmaceuticals, Inc.

  公开号：EP1824482A1

  公开（公告）日：2007-08-29
• EP1824482A4
  申请人：——

  公开号：EP1824482A4

  公开（公告）日：2009-08-26