6-bromo-2-ethoxycarbonylaminothiazolo/4,5-b/pyrazine | 112342-70-8

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 二嗪类
• 英文名称: 6-bromo-2-ethoxycarbonylaminothiazolo/4,5-b/pyrazine
• 英文别名: ethyl (6-bromo[1,3]thiazolo[4,5-b]pyrazin-2-yl)carbamate；ethyl (6-bromothiazolo[4,5-b]pyrazin-2-yl)carbamate；ethyl N-(6-bromo-[1,3]thiazolo[4,5-b]pyrazin-2-yl)carbamate
• CAS: 112342-70-8
• 化学式: C₈H₇BrN₄O₂S
• 分子量: 303.139
• InChiKey: XXOZIYKQVRGKHL-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  2.2
• 重原子数：
  16
• 可旋转键数：
  3
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.25
• 拓扑面积：
  105
• 氢给体数：
  1
• 氢受体数：
  6

反应信息

• 作为反应物：
  描述：

  6-bromo-2-ethoxycarbonylaminothiazolo/4,5-b/pyrazine 在 sodium hydroxide 作用下， 反应 5.0h， 以71%的产率得到2-氨基-6-溴噻唑并[4,5-B]吡嗪
  参考文献：
  名称：

  Koren, Bozidar; Stanovnik, Branko; Tisler, Miha, Heterocycles, 1987, vol. 26, # 3, p. 689 - 697

  摘要：

  DOI：
• 作为产物：
  描述：

  异硫氰酰甲酸乙酯 、 2-氨基-3,5-二溴吡嗪 生成 6-bromo-2-ethoxycarbonylaminothiazolo/4,5-b/pyrazine
  参考文献：
  名称：

  Koren, Bozidar; Stanovnik, Branko; Tisler, Miha, Heterocycles, 1987, vol. 26, # 3, p. 689 - 697

  摘要：

  DOI：

文献信息

• [EN] HETEROAROMATIC COMPOUNDS AS INHIBITORS OF STEAROYL-COENZYME A DELTA-9 DESATURASE<br/>[FR] COMPOSÉS HÉTÉROAROMATIQUES EN TANT QU'INHIBITEURS DE LA STÉAROYL-COENZYME A DELTA-9 DÉSATURASE
  申请人：MERCK FROSST CANADA LTD

  公开号：WO2010037225A1

  公开（公告）日：2010-04-08

  Heteroaromatic compounds of structural formula (I) are inhibitors of stearoyl-coenzyme A delta-9 desaturase (SCD). The compounds of the present invention are useful for the prevention and treatment of conditions related to abnormal lipid synthesis and metabolism, including cardiovascular disease, such as atherosclerosis; obesity; Type 2 diabetes; insulin resistance; hyperglycemia; Metabolic Syndrome; neurological disease; cancer; and liver steatosis.

  结构式（I）的杂环芳香化合物是硬脂酰辅酶A 9-去饱和酶（SCD）的抑制剂。本发明的化合物可用于预防和治疗与异常脂质合成和代谢相关的疾病，包括心血管疾病，如动脉粥样硬化；肥胖；2型糖尿病；胰岛素抵抗；高血糖；代谢综合征；神经系统疾病；癌症；以及肝脂肪变性。
• Oxime Derivative and Preparations Thereof
  申请人：Sugawara Kazutoshi

  公开号：US20080132479A1

  公开（公告）日：2008-06-05

  The problem of the present invention is to provide a useful compound as a glucokinase activating agent, which is the oxime derivative of the formula [I]: wherein Ring A is aryl or heteroaryl; Q is cycloalkyl, heterocycle, alkyl or alkenyl; Ring T is heteroaryl or heterocycle; R 1 and R 2 are independently hydrogen atom, halogen atom, cycloalkylsulfonyl or the like; R 3 and R 4 are independently hydrogen atom, hydroxy, oxo, halogen atom or the like; R 5 is hydrogen atom, halogen atom, cyano, nitro, tetrazolyl or the like; or a pharmaceutically acceptable salt thereof.

  本发明的问题是提供一种有用的化合物作为葡萄糖激酶活化剂，其为式[I]的肟衍生物：其中，环A是芳基或杂芳基；Q是环烷基，杂环，烷基或烯基；环T是杂芳基或杂环；R1和R2分别是氢原子，卤素原子，环烷基磺酰基或类似物；R3和R4分别是氢原子，羟基，氧代，卤素原子或类似物；R5是氢原子，卤素原子，氰基，硝基，四唑基或类似物；或其药学上可接受的盐。
• OXIME DERIVATIVE AND PREPARATIONS THEREOF
  申请人：Sugawara Kazutoshi

  公开号：US20090291936A1

  公开（公告）日：2009-11-26

  The problem of the present invention is to provide a useful compound as a glucokinase activating agent, which is the oxime derivative of the formula [I]: wherein Ring A is aryl or heteroaryl; Q is cycloalkyl, heterocycle, alkyl or alkenyl; Ring T is heteroaryl or heterocycle; R 1 and R 2 are independently hydrogen atom, halogen atom, cycloalkylsulfonyl or the like; R 3 and R 4 are independently hydrogen atom, hydroxy, oxo, halogen atom or the like; R 5 is hydrogen atom, halogen atom, cyano, nitro, tetrazolyl or the like; or a pharmaceutically acceptable salt thereof.

  本发明的问题是提供一种有用的化合物作为葡萄糖激酶活化剂，该化合物是公式[I]的肟衍生物： 其中，环A是芳基或杂环芳基；Q是环烷基、杂环、烷基或烯基；环T是杂环芳基或杂环；R1和R2分别是氢原子、卤素原子、环烷基磺酰基或类似物；R3和R4分别是氢原子、羟基、氧代、卤素原子或类似物；R5是氢原子、卤素原子、氰基、硝基、四唑基或类似物；或其药学上可接受的盐。
• HETEROAROMATIC COMPOUNDS AS INHIBITORS OF STEAROYL-COENZYME A DELTA-9 DESATURASE
  申请人：Leclerc Jean-Philippe

  公开号：US20110166152A1

  公开（公告）日：2011-07-07

  Heteroaromatic compounds of structural formula (I) are inhibitors of stearoyl-coenzyme A delta-9 desaturase (SCD). The compounds of the present invention are useful for the prevention and treatment of conditions related to abnormal lipid synthesis and metabolism, including cardiovascular disease, such as atherosclerosis; obesity; Type 2 diabetes; insulin resistance; hyperglycemia; Metabolic Syndrome; neurological disease; cancer; and liver steatosis.

  结构式（I）的杂环芳香化合物是硬脂酰辅酶A Δ-9去饱和酶（SCD）的抑制剂。本发明的化合物可用于预防和治疗与异常脂质合成和代谢有关的疾病，包括心血管疾病，如动脉粥样硬化;肥胖症; 2型糖尿病;胰岛素抵抗;高血糖;代谢综合征;神经系统疾病;癌症;和脂肪肝。
• ACETIC ACID AMIDE DERIVATIVE HAVING INHIBITORY ACTIVITY ON ENDOTHELIAL LIPASE
  申请人：Masuda Koji

  公开号：US20110251386A1

  公开（公告）日：2011-10-13

  Disclosed is a compound which is useful as an endothelial lipase inhibitor. A pharmaceutical composition having inhibitory activity on endothelial lipase comprising a compound represented by the formula: its pharmaceutically acceptable salt, or a solvate thereof, wherein Ring A is nitrogen-containing hetero ring, Ring A may be substituted with a substituent other than a group represented by the formula: —C(R 1 R 2 )—C(═O)—NR 3 R 4 and a group represented by the formula: —R 5 , a broken line represents the presence or the absence of a bond, Z is —NR 6 —, ═N—, —O—, or —S—, R 6 is halogen, substituted or unsubstituted alkyl or the like, 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, substituted or unsubstituted alkyl or the like, 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, substituted or unsubstituted alkynyl or the like.

  公开了一种作为内皮酯酶抑制剂有用的化合物。一种具有内皮酯酶抑制活性的药物组合物，包括下式所示的化合物：其药学上可接受的盐或其溶剂合物，其中，环A是含氮杂环，环A可以被除了由下式表示的基团：—C(R1R2)—C(═O)—NR3R4和由下式表示的基团：—R5以外的基团取代，其中，一条虚线表示键的存在或不存在，Z为—NR6—，═N—，—O—或—S—，R6为卤素，取代或未取代的烷基或类似物，R1和R2各自独立地为氢、卤素、羟基、氰基、硝基、羧基或取代或未取代的烷基，R3为氢或取代或未取代的烷基，R4为氢、取代或未取代的烷基或类似物，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为氢、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、取代或未取代的炔基或类似物。