6-ethylsulfonylpyridin-3-ol | 859536-32-6

• 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
• 英文名称: 6-ethylsulfonylpyridin-3-ol
• 英文别名: 6-ethanesulfonyl-pyridin-3-ol；6-(ethylsulfonyl)-3-pyridinol；6-(Ethanesulfonyl)pyridin-3-ol
• CAS: 859536-32-6
• 化学式: C₇H₉NO₃S
• 分子量: 187.219
• InChiKey: HESMCLAOUJVQCA-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  0.4
• 重原子数：
  12
• 可旋转键数：
  2
• 环数：
  1.0
• sp3杂化的碳原子比例：
  0.29
• 拓扑面积：
  75.6
• 氢给体数：
  1
• 氢受体数：
  4

反应信息

• 作为反应物：
  描述：

  Pyrazine-2-carboxylic acid (5-fluoro-4-(2-cyano-6-fluoro-phenoxy)-2-nitro-phenyl)-amide 、 6-ethylsulfonylpyridin-3-ol 以The entitled compound was obtained as a white solid in the same method as in Example 400 (step 3) or in accordance with the method的产率得到5-(2-Fluoro-6-cyano-phenoxy)-2-pyrazin-2-yl-6-(6-ethanesulfonyl-pyridin-3-yloxy)-1H-benzimidazole
  参考文献：
  名称：

  Novel 2-Heteroaryl-Substituted Benzimidazole Derivative

  摘要：

  提供了一种葡萄糖激酶激活剂；提供了糖尿病的治疗和/或预防，或者提供了糖尿病的治疗和/或预防，例如视网膜病变、肾病、神经病、缺血性心脏病、动脉硬化，以及肥胖症的治疗和/或预防。葡萄糖激酶激活剂的特征在于包含通式（I-0）的2-杂环芳基取代苯并咪唑衍生物或其药学上可接受的盐：[在公式中，X表示碳原子或氮原子；X1、X2、X3和X4分别独立地表示碳原子或氮原子；环A表示公式（II）的5-或6-成员含氮芳香杂环：（在公式中，X表示碳原子或氮原子）；R1表示芳基等；R2表示羟基等；R3表示-C1-6烷基等；R4表示-C1-6烷基等；X5表示-O-等；a表示1、2或3的整数；q表示0到2的整数；m表示0到2的整数]。

  公开号：

  US20080070928A1
• 作为产物：
  描述：

  5-bromo-2-ethylsulfanyl-pyridine 在 吡啶盐酸盐 、 间氯过氧苯甲酸 作用下， 以 甲醇 、 二氯甲烷 为溶剂， 反应 12.0h， 生成 6-ethylsulfonylpyridin-3-ol
  参考文献：
  名称：

  BROMODOMAIN INHIBITORS

  摘要：

  本发明涉及替代杂环衍生物化合物，包括所述化合物的组合物，以及通过抑制溴结构域介导的蛋白质乙酰赖氨酸区域的识别来进行表观遗传调控的所述化合物和组合物的用途。所述组合物和方法对于癌症和肿瘤性疾病的治疗是有用的。

  公开号：

  US20150111885A1

文献信息

• Heteroarylcarbamoylbenzene derivative
  申请人：IIno Tomoharu

  公开号：US20060167053A1

  公开（公告）日：2006-07-27

  Compounds represented by formula (I): as well as their pharmaceutically acceptable salts are disclosed. The compounds are useful as glucokinase activating agents for the treatment of diabetes and related conditions. Compositions and methods of treatment are also included.

  公式（I）所代表的化合物及其药学上可接受的盐被披露。这些化合物可用作激活葡萄糖激酶的药剂，用于治疗糖尿病及相关疾病。还包括治疗组合物和方法。
• Novel 2-Heteroaryl-Substituted Benzimidazole Derivative
  申请人：Nonoshita Katsumasa

  公开号：US20080070928A1

  公开（公告）日：2008-03-20

  A glucokinase activator is provided; and a remedy and/or a preventive for diabetes, or a remedy and/or a preventive for diabetes such as retinopathy, nephropathy, neurosis, ischemic cardiopathy, arteriosclerosis, and further a remedy and/or a preventive for obesity are provided. A glucokinase activator characterized by containing a 2-heteroaryl-substituted benzimidazole derivative of a general formula (I-0) or its pharmaceutically-acceptable salt: [in the formula, X represents a carbon atom or a nitrogen atom; X 1 , X 2 , X 3 and X 4 each independently represent a carbon atom or a nitrogen atom; the ring A represents a 5- or 6-membered nitrogen-containing aromatic hetero ring of a formula (II): (in the formula, X represents a carbon atom or a nitrogen atom); R 1 represents an aryl, etc.; R 2 represents a hydroxy, etc.; R 3 represents a —C 1-6 alkyl, etc.; R 4 represents a —C 1-6 alkyl, etc.; X 5 represents —O—, etc.; a indicates an integer of 1, 2 or 3; q indicates an integer of from 0 to 2; m indicates an integer of from 0 to 2].

  提供了一种葡萄糖激酶激活剂；提供了糖尿病的治疗和/或预防，或者提供了糖尿病的治疗和/或预防，例如视网膜病变、肾病、神经病、缺血性心脏病、动脉硬化，以及肥胖症的治疗和/或预防。葡萄糖激酶激活剂的特征在于包含通式（I-0）的2-杂环芳基取代苯并咪唑衍生物或其药学上可接受的盐：[在公式中，X表示碳原子或氮原子；X1、X2、X3和X4分别独立地表示碳原子或氮原子；环A表示公式（II）的5-或6-成员含氮芳香杂环：（在公式中，X表示碳原子或氮原子）；R1表示芳基等；R2表示羟基等；R3表示-C1-6烷基等；R4表示-C1-6烷基等；X5表示-O-等；a表示1、2或3的整数；q表示0到2的整数；m表示0到2的整数]。
• Heteroarylcarbamoylbenzene derivatives
  申请人：Iino Tomoharu

  公开号：US20090018056A1

  公开（公告）日：2009-01-15

  Compounds having glucokinase activating effects and being useful as treatments for diabetes, which are represented by the following formula (I): [wherein X 1 represents oxygen, etc., X 2 represents oxygen, etc., R 1 represents a group on Ring A such as alkylsulfonyl, etc., R 2 represents C3-7 cyclic alkyl optionally substituted with a halogen, etc., R 3 represents a substituent on Ring B such as lower alkyl, etc., formula (II): [Chemical Formula 1] represents 6- to 10-membered aryl, etc., and formula (III): [Formula 1] represents monocyclic or bicyclic heteroaryl optionally having on Ring B a substituent represented by R 3 above, wherein the carbon atom of Ring B which is bonded to the nitrogen atom of the amide group of formula (I) forms a C═N bond with the nitrogen atom of the ring], as well as their pharmaceutically acceptable salts.

  具有激活葡萄糖激酶效果且可用作糖尿病治疗的化合物，其化学式如下（I）：[其中X1代表氧等，X2代表氧等，R1代表环A上的基团，例如烷基磺酰等，R2代表C3-7环状烷基，可选择地被卤素等取代，R3代表环B上的取代基，例如低烷基等，化学式（II）：[化学式1]代表6到10成员芳基等，化学式（III）：[化学式1]代表单环或双环杂芳基，可选择地在环B上具有由上述R3代表的取代基，其中环B的碳原子与化学式（I）的酰胺基团的氮原子形成C═N键与环的氮原子结合]，以及其药学上可接受的盐。
• Aryloxy-Substituted Benzimidazole Derivatives
  申请人：Hashimoto Noriaki

  公开号：US20080125429A1

  公开（公告）日：2008-05-29

  A glucokinase activator is provided; and a treatment and/or a preventive for diabetes, or a treatment and/or a preventive for diabetes such as retinopathy, nephropathy, neurosis, ischemic cardiopathy, arteriosclerosis, and further a treatment and/or a preventive for obesity are provided. The invention relates to a compound of a formula (I): [wherein R 1 and R 2 represent a hydrogen, etc.; R 3 represents a hydrogen atom, a halogen atom, etc.; R 4 each independently represents a hydrogen atom, a lower alkyl group, etc.; Q represents a carbon atom, a nitrogen atom or a sulfur atom (the sulfur atom may be mono- or di-substituted with an oxo group); R 5 and R 6 each represent a hydrogen atom, a lower alkyl group, etc.; X 1 , X 2 , X 3 and X 4 each independently represent a carbon atom or a nitrogen atom; Z represents an oxygen atom, a sulfur atom or a nitrogen atom; Ar represents an aryl or heteroaryl group optionally mono to tri-substituted with a group selected from the substituent group β; ring A represents a 5- or 6-membered nitrogen-containing heteroaromatic group; m indicates an integer of from 1 to 6; n indicates an integer of from 0 to 3; p indicates an integer of from 0 to 2 (provided that at least two of X 1 to X 4 are carbon atoms); q indicates 0 or 1] or its pharmaceutically-acceptable salt, which has an effect of glucokinase activation and is useful as a treatment for diabetes.

  本发明提供了一种葡萄糖激酶激活剂；以及用于糖尿病的治疗和/或预防，或用于糖尿病如视网膜病变、肾病、神经病、缺血性心脏病、动脉硬化等的治疗和/或预防，以及用于肥胖症的治疗和/或预防。本发明涉及一种化合物的公式(I)：[其中R1和R2分别表示氢等；R3表示氢原子、卤原子等；R4各自独立地表示氢原子、低级烷基等；Q表示碳原子、氮原子或硫原子（硫原子可以是单取代或双取代的氧基）；R5和R6各自表示氢原子、低级烷基等；X1、X2、X3和X4各自独立地表示碳原子或氮原子；Z表示氧原子、硫原子或氮原子；Ar表示芳基或杂环芳基，可选择性地单取代至三取代于β取代基；环A表示一个含氮的5-或6成员杂芳基；m表示1至6的整数；n表示0至3的整数；p表示0至2的整数（前提是X1至X4中至少有两个是碳原子）；q表示0或1]或其药学上可接受的盐，具有葡萄糖激酶激活的作用，并且可用作糖尿病的治疗。
• 2-HETEROARYL-SUBSTITUTED INDOLE DERIVATIVE
  申请人：Takahashi Keiji

  公开号：US20090118304A1

  公开（公告）日：2009-05-07

  Disclosed is a compound represented by the formula (I) below, which has a glucokinase-activating effect and is thus useful for treatment of diabetes or obesity, or a pharmaceutically acceptable salt thereof. In the formula, R 1 represents an aryl or the like; R 11 represents an aryl or the like; R 2 represents a formyl or the like, R 3 represents a C 1-6 alkyl or the like; R 3 represents a hydrogen atom or the like; Z 1 represents —O— or the like; Z 2 represents —O— or the like; Y 1 -Y 4 respectively represent a carbon atom or a nitrogen atom; ring A represents a heteroaryl group; X represents a carbon atom or the like; m represents an integer of 0-2; and q represents an integer of 0-2.

  本发明涉及一种化合物，其公式如下（I），具有激活葡萄糖激酶的作用，因此可用于治疗糖尿病或肥胖症，或其药学上可接受的盐。在公式中，R1代表芳基或类似物; R11代表芳基或类似物; R2代表甲酰基或类似物，R3代表C1-6烷基或类似物; R3代表氢原子或类似物; Z1代表—O—或类似物; Z2代表—O—或类似物; Y1-Y4分别代表碳原子或氮原子; 环A代表杂环芳基; X代表碳原子或类似物; m代表0-2的整数; q代表0-2的整数。