3-(6-溴吡啶-3-基)丙酸 | 1036227-86-7

• 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: 3-(6-溴吡啶-3-基)丙酸
• 英文名称: 3-(6-bromopyridin-3-yl)propanoic acid
• 英文别名: 3-(6-bromo-pyridin-3-yl)-propionic acid；3-(6-Bromopyridin-3-yl)propanoic acid
• CAS: 1036227-86-7
• 化学式: C₈H₈BrNO₂
• 分子量: 230.061
• InChiKey: VNZWQWJMCMQTJL-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  1.6
• 重原子数：
  12
• 可旋转键数：
  3
• 环数：
  1.0
• sp3杂化的碳原子比例：
  0.25
• 拓扑面积：
  50.2
• 氢给体数：
  1
• 氢受体数：
  3

反应信息

• 作为反应物：
  描述：

  3-(6-溴吡啶-3-基)丙酸 在 sodium hexamethyldisilazane 、 三甲基乙酰氯 、 氯化铵 、 N,N-二异丙基乙胺 、 N-[(dimethylamino)-3-oxo-1H-1,2,3-triazolo[4,5-b]pyridin-1-yl-methylene]-N-methylmethanaminium hexafluorophosphate 作用下， 以 四氢呋喃 、 二氯甲烷 为溶剂， 反应 8.0h， 生成 (S)-tert-butyl 4-amino-3-((6-bromopyridin-3-yl)methyl)-4-oxobutanoate
  参考文献：
  名称：

  [EN] BETA-TETRAZOLYL-PROPIONIC ACIDS AS METALLO-BETA-LACTAMASE INHIBITORS
  [FR] ACIDES BÊTA-TÉTRAZOLYLE-PROPIONIQUES UTILES EN TANT QU'INHIBITEURS DES MÉTALLO-BÊTA-LACTAMASES

  摘要：

  本发明涉及公式I的化合物，这些化合物是金属β-内酰胺酶抑制剂，以及这些化合物的合成和与β-内酰胺类抗生素一起使用以克服抗性的用途。

  公开号：

  WO2015171474A1

文献信息

• Heteroaryl-substituted carboxamides and use thereof for the stimulation of the expression of NO synthase
  申请人：sanofi-aventis

  公开号：EP1939181A1

  公开（公告）日：2008-07-02

  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。
• [EN] NOVEL NON-CODING HETEROCYCLIC AMINO ACIDS (NCHAA) AND THEIR USE AS HERBICIDES<br/>[FR] NOUVEAUX ACIDES AMINÉS HÉTÉROCYCLIQUES NON CODANTS (NCHAA) ET LEUR UTILISATION EN TANT QU'HERBICIDES
  申请人：FORTEPHEST LTD

  公开号：WO2020250223A1

  公开（公告）日：2020-12-17

  The invention relates to a novel substituted amino acids, agricultural compositions comprising the novel substituted amino acids, and their use for controlling undesired plant growth alone or in combination with crop protection agents such as pesticides or plant growth regulators.

  该发明涉及一种新型的替代氨基酸，包括该新型替代氨基酸的农业组合物，以及它们用于单独或与农作物保护剂（如杀虫剂或植物生长调节剂）结合控制不受欢迎的植物生长的用途。
• 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。
• 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。
• SUBSTITUTED PYRIDINE SPLEEN TYROSINE KINASE (SYK) INHIBITORS
  申请人：Merck Sharp & Dohme Corp.

  公开号：US20150148327A1

  公开（公告）日：2015-05-28

  The invention provides certain substituted pyridines of the Formula (I) or pharmaceutically acceptable salts thereof, wherein R 1 , R 2 , R 3 , R 4 , R cy , C y , and t are as defined herein. The invention also provides pharmaceutical compositions comprising such compounds, and methods of using the compounds for treating diseases or conditions mediated by Spleen Tyrosine Kinase (Syk) kinase.

  本发明提供了以下公式（I）的某些取代吡啶或其药学上可接受的盐，其中R1，R2，R3，R4，Rcy，Cy和t如本文所定义。 本发明还提供了包含这种化合物的制药组合物，并且提供了使用这些化合物治疗由脾酪氨酸激酶（Syk）激酶介导的疾病或病症的方法。