6-bromo-2-(4-fluoro-phenyl)-imidazo[1,2-a]pyrimidine | 944581-05-9

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 唑类
• 英文名称: 6-bromo-2-(4-fluoro-phenyl)-imidazo[1,2-a]pyrimidine
• 英文别名: 6-Bromo-2-(4-fluorophenyl)imidazo[1,2-a]pyrimidine
• CAS: 944581-05-9
• 化学式: C₁₂H₇BrFN₃
• mdl: MFCD11036001
• 分子量: 292.11
• InChiKey: DCJOLGXJMBTJEY-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  3.6
• 重原子数：
  17
• 可旋转键数：
  1
• 环数：
  3.0
• sp3杂化的碳原子比例：
  0.0
• 拓扑面积：
  30.2
• 氢给体数：
  0
• 氢受体数：
  3

文献信息

• Imidazo[1,2-a]azine and their use as pharmaceuticals
  申请人：sanofi-aventis

  公开号：EP1964841A1

  公开（公告）日：2008-09-03

  Imidazo[1,2-a]azines and their use as pharmaceuticals The present invention relates to derivatives of imidazo[1,2-a]azines of the formula (I), in which X, R, R1 to R3 and n 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Imidazo[1,2-a]azines衍生物及其作为药物的用途。该发明涉及公式(I)中的imidazo[1,2-a]azines衍生物，其中X、R、R1至R3和n具有权利要求中指示的含义，这些衍生物调节内皮型一氧化氮（NO）合成酶的转录，并且是有价值的药理活性化合物。具体而言，公式I的化合物上调内皮型NO合成酶的表达，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。本发明还涉及公式I化合物的制备方法，包括含有它们的药物组合物，以及公式I化合物用于制造刺激内皮型NO合成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、冠心病、高血压和心脏功能不全等。
• IMIDAZO[1,2-a]AZINES AND THEIR USE AS PHARMACEUTICALS
  申请人：ZOLLER Gerhard

  公开号：US20100137321A1

  公开（公告）日：2010-06-03

  The present invention relates to derivatives of imidazo[1,2-a]azines of formula I, in which R, R1 to R3, X, Y and n 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 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 formula I, to pharmaceutical compositions comprising them, and to the use of compounds of formula I 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的咪唑[1,2-a]嘧啶衍生物，其中R，R1至R3，X，Y和n具有声明中指定的含义，这些化合物调节内皮型一氧化氮（NO）合酶的转录并具有药理活性。具体而言，公式I的化合物上调内皮型NO合酶的表达，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。本发明还涉及制备公式I的化合物的方法，包括它们的制药组合物，以及使用公式I的化合物刺激内皮型NO合酶的表达或治疗各种疾病，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。
• IMIDAZO[1,2-A]AZINES AND THEIR USE AS PHARMACEUTICALS
  申请人：Sanofi-Aventis

  公开号：EP2129676A1

  公开（公告）日：2009-12-09
• US8044050B2
  申请人：——

  公开号：US8044050B2

  公开（公告）日：2011-10-25
• [EN] IMIDAZO[1,2-A]AZINES AND THEIR USE AS PHARMACEUTICALS<br/>[FR] IMIDAZO[1,2-A]AZINES ET LEUR UTILISATION COMME MÉDICAMENTS
  申请人：SANOFI AVENTIS

  公开号：WO2008104279A1

  公开（公告）日：2008-09-04

  [EN] The present invention relates to derivatives of imidazo[1,2-a]azines of the formula (I), in which R, R1 to R3, X, Y and n 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.
  [FR] La présente invention concerne des dérivés d'imidazo[1,2,a]azines représentés par la formule générale (I). Dans cette formule, R, R1 à R3, X, Y et n désignent des éléments indiqués dans les revendications. Ces dérivés modulent la transcription du monoxyde d'azote synthase endothélial et sont des composés précieux pour leur activité pharmacologique. Plus précisément, les composés représentés par la formule générale (I) régulent à la hausse l'expression de l'enzyme monoxyde d'azote synthase endothélial et peuvent être utilisés dans des conditions dans lesquelles une expression accrue de ladite enzyme ou une concentration élevée de monoxyde d'azote ou la normalisation d'une concentration réduite de monoxyde d'azote est souhaitée. L'invention concerne également des procédés destinés à la préparation de composés représentés par la formule générale (I), des compositions pharmaceutiques comprenant ces composés, ainsi que l'utilisation de composés représentés par la formule générale (I) pour la fabrication d'un médicament destiné à la stimulation de l'expression du monoxyde d'azote synthase endothélial ou au traitement de diverses maladies, y compris des troubles cardiovasculaires, tels que l'athérosclérose, la thrombose, la coronaropathie, l'hypertension et l'insuffisance cardiaque, par exemple.