1H-咪唑并[4,5-c]吡啶-4-羧酸 | 933728-33-7

• 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: 1H-咪唑并[4,5-c]吡啶-4-羧酸
• 英文名称: 1H-imidazolo[4,5-c]pyridine-4-carboxylic acid
• 英文别名: 1H-imidazo[4,5-c]pyridine-4-carboxylic acid；imidazolo[4,5-c]pyridine-4-carboxylic acid；imidazo[4,5-c]pyridin-4-carboxylic acid；imidazo[4,5-c]pyridine-4-formic acid
• CAS: 933728-33-7
• 化学式: C₇H₅N₃O₂
• mdl: MFCD18803553
• 分子量: 163.136
• InChiKey: MYYGVHLIIVDANU-UHFFFAOYSA-N

物化性质

• 沸点：
  615.7±35.0 °C(Predicted)
• 密度：
  1.617±0.06 g/cm3(Predicted)

计算性质

• 辛醇/水分配系数(LogP)：
  0.3
• 重原子数：
  12
• 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：
  78.9
• 氢给体数：
  2
• 氢受体数：
  4

反应信息

• 作为产物：
  描述：

  1H-咪唑并[4,5-C]吡啶-4-甲腈 在 水 作用下， 以 1,4-二氧六环 为溶剂， 生成 1H-咪唑并[4,5-c]吡啶-4-羧酸
  参考文献：
  名称：

  Structure-guided design of substituted aza-benzimidazoles as potent hypoxia inducible factor-1α prolyl hydroxylase-2 inhibitors

  摘要：

  We report the structure-based design and synthesis of a novel series of aza-benzimidazoles as PHD2 inhibitors. These efforts resulted in compound 22, which displayed highly potent inhibition of PHD2 function in vitro. (C) 2008 Elsevier Ltd. All rights reserved.

  DOI：

  10.1016/j.bmcl.2008.08.012

文献信息

• [EN] BIPHENYL SULFONAMIDES AS DUAL ANGIOTENSIN ENDOTHELIN RECEPTOR ANTAGONISTS<br/>[FR] BIPHENYL SULFONAMIDES EN TANT QUE DOUBLES ANTAGONISTES DE RECEPTEURS D'ANGIOTENSINE ET D'ENDOTHELINE
  申请人：BRISTOL MYERS SQUIBB CO

  公开号：WO2000001389A1

  公开（公告）日：2000-01-13

  Novel biphenyl sulfonamide compounds which are combined angiotensin and endothelin receptor antagonists are claimed along with methods of using such compounds in the treatment of conditions such as hypertension and other diseases, as well as pharmaceutical compositions containing such compounds.

  本发明涉及一种新型的联合血管紧张素和内皮素受体拮抗剂的双苯基磺酰胺类化合物，以及使用这些化合物治疗高血压和其他疾病的方法，以及含有这些化合物的制药组合物。
• [EN] BIPHENYL SULFONAMIDES AS DUAL ANGIOTENSIN ENDOTHELIN RECEPTOR ANTAGONISTS<br/>[FR] BIPHENYL SULFONAMIDES UTILISES COMME DOUBLES ANTAGONISTES DES RECEPTEURS DE L'ANGIOTENSINE ET DE L'ENDOTHELINE
  申请人：BRISTOL MYERS SQUIBB CO

  公开号：WO2001044239A2

  公开（公告）日：2001-06-21

  Novel biphenyl sulfonamide compounds which are combined angiotensin and endothelin receptor antagonists are claimed along with methods of using such compounds in the treatment of conditions such as hypertension and other diseases, as well as pharmaceutical compositions containing such compounds.

  本专利申请涉及一种新型的联合血管紧张素和内皮素受体拮抗剂的新型二苯基磺酰胺化合物，以及使用这些化合物治疗高血压和其他疾病的方法，同时还包括含有这些化合物的制药组合物。
• P2X7 MODULATORS
  申请人：JANSSEN PHARMACEUTICA NV

  公开号：US20160039809A1

  公开（公告）日：2016-02-11

  The present invention is directed to compounds of Formulas (I, Ia, IIa and IIb). The invention also relates to pharmaceutical compositions comprising compounds of Formulas (I, Ia, IIa and IIb). Methods of making and using the compounds of Formulas (I, Ia, IIa and IIb) are also within the scope of the invention.

  本发明涉及化合物I、Ia、IIa和IIb的公式。本发明还涉及包含化合物I、Ia、IIa和IIb的制药组合物。制备和使用化合物I、Ia、IIa和IIb的方法也在本发明的范围内。
• Imidazopyridine derivatives and process for preparation thereof
  申请人：TANABE SEIYAKU CO., LTD.

  公开号：EP0531874A1

  公开（公告）日：1993-03-17

  An imidazopyridine derivative of the formula [I]: wherein R¹ is hydrogen or lower alkyl, R² is hydrogen, lower alkylsulfonyl or a group of the formula: (Z is oxygen atom or two hydrogen, R⁰ is substituted or unsubstituted lower alkyl, lower alkoxy, 5- or 6-membered heteromonocyclic, substituted or unsubstituted phenyl, hydrogen, substituted or unsubstitued amino or lower alkenyl), R³ is carboxyl or lower alkoxycarbonyl and Ring A is substituted or unsubstituted phenyl, and pharmaceutically acceptable salt thereof, and processes for preparation thereof, said imidazopyridine derivatives have excellent angiotensin II antagonistic activities and are useful in prophylaxis and treatment of hypertension.

  式 [I] 的咪唑吡啶衍生物： 其中 R¹ 是氢或低级烷基，R² 是氢、低级烷基磺酰基或式中的一个基团： (Z是氧原子或两个氢，R⁰是取代或未取代的低级烷基、低级烷氧基、5-或 6-元杂环基、取代或未取代的苯基、氢、取代或未取代的氨基或低级烯基）、R³ 是羧基或低级烷氧基羰基，环 A 是取代或未取代的苯基，以及其药学上可接受的盐及其制备方法，所述咪唑吡啶衍生物具有优异的血管紧张素 II 拮抗活性，可用于高血压的预防和治疗。
• Imidazoindolizine derivatives and process for preparation thereof
  申请人：TANABE SEIYAKU CO., LTD.

  公开号：EP0531876A2

  公开（公告）日：1993-03-17

  An imidazoindolizine derivative of the formula [I]: wherein R¹ is lower alkyl, R² is hydrogen, cyano, lower alkyl, lower alkanoyl, lower alkoxycarbonyl, phenyl-lower alkoxycarbonyl, lower alkylsulfonyl, substituted or unsubstituted phenyl, arylcarbonyl, or 5- or 6-membered nitrogen-containing heteromonocyclic group-substituted carbonyl, Ring A is substituted or unsubstituted phenyl, and m is 0 or 1, or a pharmaceutically acceptable salt thereof, and process for preparation thereof, said imidazoindolizine derivatives and pharmaceutically acceptable salts thereof show excellent angiotensin II inhibitory activities and are useful in the prophylaxis or treatment of hypertension.

  式[I]的咪唑吲嗪衍生物： 其中 R¹ 是低级烷基，R² 是氢、氰基、低级烷基、低级烷酰基、低级烷氧基羰基、苯基-低级烷氧基羰基、低级烷基磺酰基、取代或未取代的苯基、芳基羰基或 5 或 6 元含氮杂环基取代的羰基，环 A 是取代或未取代的苯基、和 m 为 0 或 1 的咪唑吲嗪衍生物或其药学上可接受的盐及其制备方法，所述咪唑吲嗪衍生物及其药学上可接受的盐显示出优异的血管紧张素 II 抑制活性，可用于高血压的预防或治疗。