6-(2-氟苯基)吡啶-3-醇 | 859538-49-1

• 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: 6-(2-氟苯基)吡啶-3-醇
• 英文名称: 6-(2-fluoro-phenyl)-pyridin-3-ol
• 英文别名: 6-(2-fluorophenyl)pyridin-3-ol
• CAS: 859538-49-1
• 化学式: C₁₁H₈FNO
• 分子量: 189.189
• InChiKey: KDPOGXMMTHAGIX-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  2.3
• 重原子数：
  14
• 可旋转键数：
  1
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.0
• 拓扑面积：
  33.1
• 氢给体数：
  1
• 氢受体数：
  3

反应信息

• 作为反应物：
  描述：

  6-(2-氟苯基)吡啶-3-醇 、 溴乙酸甲酯 在 sodium hydride 作用下， 以 N,N-二甲基甲酰胺 为溶剂， 反应 3.0h， 以80%的产率得到(6-(2-fluorophenyl)pyridin-3-yloxy)acetic acid methyl ester
  参考文献：
  名称：

  Heteroaryl-substituted amides comprising a saturated linker group, and their use as pharmaceuticals

  摘要：

  本发明涉及式I的N-烷基酰胺， 其中A、Het、X、R1、R2和R3的含义如权利要求中指出的，这些化合物能够调节内皮型一氧化氮（NO）合酶的转录，并且是有价值的药物活性化合物。具体而言，式I的化合物可以上调内皮型NO合酶的表达，并可用于那些需要增加所述酶的表达、增加NO水平或使降低的NO水平正常化的情况。本发明还涉及制备式I化合物的方法，包含它们的药物组合物，以及使用式I化合物用于制造刺激内皮型NO合酶表达或治疗包括动脉粥样硬化、血栓、冠心病、高血压和心力衰竭等各种疾病的药物。

  公开号：

  EP1741709A1
• 作为产物：
  描述：

  在 氢氧化钾 、 水 、 盐酸 作用下， 以 甲醇 、 水 为溶剂， 反应 2.0h， 生成 6-(2-氟苯基)吡啶-3-醇
  参考文献：
  名称：

  Heteroaryl-substituted carboxamides and use thereof for the stimulation of the expression of NO synthase

  摘要：

  本发明涉及公式I的杂环取代羧酰胺，其中Het、A、X、R1、R2和R3具有索引中指示的含义，这些化合物调节内皮一氧化氮（NO）合酶的转录，并且是有价值的药理活性化合物。具体地，公式I的化合物上调内皮一氧化氮合酶酶的表达，并可应用于需要增加该酶的表达或增加NO水平或正常化降低的NO水平的情况。该发明还涉及公式I化合物的制备方法，包括它们的药物组合物，以及公式I化合物用于制造刺激内皮一氧化氮合酶表达或治疗各种疾病的药物的用途，包括心血管疾病，如动脉粥样硬化、血栓形成、冠状动脉疾病、高血压和心脏功能不全等。

  公开号：

  EP1939181A1

文献信息

• 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]。
• HETEROARYL-SUBSTITUTED CARBOXAMIDES AND THEIR USE AS PHARMACEUTICALS
  申请人：STROBEL Hartmut

  公开号：US20100016337A1

  公开（公告）日：2010-01-21

  The present invention relates to heteroaryl-substituted carboxamides of the formula I, in which Het, A, X, R 1 , R 2 and R 3 have the meanings indicated in the claims, which modulate the transcription of endothelial nitric oxide (NO) synthase and are valuable pharmacologically active compounds. Specifically, the compounds of the formula I upregulate the expression of the enzyme endothelial NO synthase and can be applied in conditions in which an increased expression of said enzyme or an increased NO level or the normalization of a decreased NO level is desired. The invention further relates to processes for the preparation of compounds of the formula I, to pharmaceutical compositions comprising them, and to the use of compounds of the formula I for the manufacture of a medicament for the stimulation of the expression of endothelial NO synthase or for the treatment of various diseases including cardiovascular disorders such as atherosclerosis, thrombosis, coronary artery disease, hypertension and cardiac insufficiency, for example.

  本发明涉及公式I的杂环取代羧酰胺，其中Het、A、X、R1、R2和R3在权利要求中所示，它们调节内皮型一氧化氮（NO）合酶的转录，并且是有价值的药理活性化合物。具体来说，公式I的化合物上调内皮型一氧化氮合酶的表达，并可应用于需要增加该酶的表达或增加NO水平或恢复降低的NO水平的情况。本发明还涉及制备公式I化合物的方法，包括它们的制药组成物，以及公式I化合物用于制造用于刺激内皮型NO合酶表达或治疗各种疾病的药物，包括心血管疾病，如动脉粥样硬化、血栓形成、冠状动脉疾病、高血压和心力衰竭等。
• 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。
• Heteroaryl-Substituted Amides Comprising A Saturated Linker Group, And Their Use As Pharmaceuticals
  申请人：STROBEL Harmut

  公开号：US20080171739A1

  公开（公告）日：2008-07-17

  The present invention relates to N-alkylamides of the formula I, in which A, Het, X, R 1 , R 2 and R 3 have the meanings indicated in the claims, which modulate the transcription of endothelial nitric oxide (NO) synthase and are valuable pharmacologically active compounds. Specifically, the compounds of the formula I upregulate the expression of the enzyme endothelial NO synthase and can be applied in conditions in which an increased expression of said enzyme or an increased NO level or the normalization of a decreased NO level is desired. The invention further relates to processes for the preparation of compounds of the formula I, to pharmaceutical compositions comprising them, and to the use of compounds of the formula I for the manufacture of a medicament for the stimulation of the expression of endothelial NO synthase or for the treatment of various diseases including cardiovascular disorders such as atherosclerosis, thrombosis, coronary artery disease, hypertension and cardiac insufficiency, for example.

  本发明涉及公式I的N-烷基酰胺，其中A，Het，X，R1，R2和R3具有所述声明中指示的含义，这些化合物调节内皮一氧化氮（NO）合酶的转录，并是有价值的药理活性化合物。具体地，公式I的化合物上调内皮一氧化氮合酶酶的表达，并可应用于需要增加该酶的表达或增加NO水平或规范降低的NO水平的情况。本发明还涉及制备公式I化合物的过程，包括它们的制药组合物，以及公式I化合物用于制造刺激内皮一氧化氮合酶表达或治疗各种疾病的药物的用途，包括心血管疾病，如动脉粥样硬化，血栓形成，冠状动脉疾病，高血压和心脏功能不全等。
• Heteroaryl-substituted carboxamides and their use as pharmaceuticals
  申请人：Sanofi-Aventis

  公开号：US08188291B2

  公开（公告）日：2012-05-29

  The present invention relates to heteroaryl-substituted carboxamides of the formula I, in which Het, A, X, R1, R2 and R3 have the meanings indicated in the claims, which modulate the transcription of endothelial nitric oxide (NO) synthase and are valuable pharmacologically active compounds. Specifically, the compounds of the formula I upregulate the expression of the enzyme endothelial NO synthase and can be applied in conditions in which an increased expression of said enzyme or an increased NO level or the normalization of a decreased NO level is desired. The invention further relates to processes for the preparation of compounds of the formula I, to pharmaceutical compositions comprising them, and to the use of compounds of the formula I for the manufacture of a medicament for the stimulation of the expression of endothelial NO synthase or for the treatment of various diseases including cardiovascular disorders such as atherosclerosis, thrombosis, coronary artery disease, hypertension and cardiac insufficiency, for example.

  本发明涉及式I的杂环取代羧酰胺，其中Het，A，X，R1，R2和R3具有所述索权要求中指示的含义，这些化合物调节内皮型一氧化氮（NO）合酶的转录，并且是有价值的药理活性化合物。具体而言，式I的化合物上调内皮型NO合酶的表达，并可应用于需要增加该酶的表达或增加NO水平或正常化降低的NO水平的情况下。本发明还涉及制备式I的化合物的方法，包括它们的制药组合物以及使用式I的化合物制造用于刺激内皮型NO合酶表达或治疗各种疾病的药物，包括心血管疾病如动脉粥样硬化，血栓形成，冠状动脉疾病，高血压和心脏功能不全等。