2-(1H-1,2,3-triazol-5-yl)Pyrimidine

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 二嗪类
• 英文名称: 2-(1H-1,2,3-triazol-5-yl)Pyrimidine
• 英文别名: 2-(2H-triazol-4-yl)pyrimidine
• 化学式: C₆H₅N₅
• 分子量: 147.14
• InChiKey: AKVRGYUHJCVPHH-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  -0.4
• 重原子数：
  11
• 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：
  67.4
• 氢给体数：
  1
• 氢受体数：
  4

文献信息

• [EN] TRIAZOLYL PYRIMIDINONE COMPOUNDS AS PDE2 INHIBITORS<br/>[FR] COMPOSÉS DE TRIAZOLYL PYRIMIDINONE EN TANT QU'INHIBITEURS DE PDE2
  申请人：MERCK SHARP & DOHME

  公开号：WO2016145614A1

  公开（公告）日：2016-09-22

  The present invention is directed to pyrimidine carboxamide compounds of formula I which are useful as therapeutic agents for the treatment of central nervous system disorders associated with phosphodiesterase 2 (PDE2). The present invention also relates to the use of such compounds for treating neurological and psychiatric disorders, such as schizophrenia, psychosis, Parkinson's disease, Parkinson's disease dementia (PDD), or Huntington's disease, and those associated with striatal hypofunction or basal ganglia dysfunction.

  本发明涉及式I的嘧啶甲酰胺化合物，该化合物作为治疗与磷酸二酯酶2（PDE2）相关的中枢神经系统障碍的治疗剂是有用的。本发明还涉及使用这些化合物来治疗神经和精神障碍，如精神分裂症、精神病、帕金森病、帕金森病痴呆（PDD）或亨廷顿病，以及与纹状体功能减退或基底神经节功能障碍相关的疾病。
• [EN] DIHYDROOROTATE DEHYDROGENASE INHIBITORS WITH SELECTIVE ANTI-MALARIAL ACTIVITY<br/>[FR] INHIBITEURS DE DIHYDROOROTATE DÉSHYDROGÉNASE PRÉSENTANT UNE ACTIVITÉ ANTIPALUDÉENNE SÉLECTIVE
  申请人：UNIV TEXAS

  公开号：WO2009082691A1

  公开（公告）日：2009-07-02

  Compounds according to Formula (I), Formula (II), Formula (III), Formula (V), Formula (VI), or to Formula (VII), and pharmaceutical compositions of compounds that conform to Formula (IV) or (Formula VIII): where R1 through R33 are prescribed, selectively inhibit P. falciparum dihydroorotate dehydrogenase. Accordingly, a method for preventing and treating malaria attaches to such compounds, as well as to pharmaceutically acceptable salts, solvates, stereoisomers, tautomers, and prodrugs thereof.

  根据公式（I），公式（II），公式（III），公式（V），公式（VI）或公式（VII）合成的化合物，以及符合公式（IV）或（公式VIII）的化合物的药物组合物，其中R1至R33被规定，选择性地抑制疟原虫脱氢鸟嘌呤酸脱氢酶。因此，一种预防和治疗疟疾的方法涉及与这些化合物以及其药用可接受的盐，溶剂化物，立体异构体，互变异构体和前药结合。
• [EN] PROCESS FOR THE PREPARATION OF ROSUVASTATIN VIA NOVEL INTERMEDIATES<br/>[FR] PROCÉDÉ DE PRÉPARATION DE ROSUVASTATINE PAR LE BIAIS DE NOUVEAUX INTERMÉDIAIRES
  申请人：IND SWIFT LAB LTD

  公开号：WO2015037018A1

  公开（公告）日：2015-03-19

  The present invention provides an industrially advantageous and cost-effective process for preparation of rosuvastatin of formula I or pharmaceutically acceptable salts thereof, [Formula I should be inserted here], via novel intermediates of formulae II and III. [Formula II should be inserted here], wherein R is selected from, R1 is selected from hydrogen, straight or branched chain alkyl group preferably C1-C4; [Formula III should be inserted here]. The present invention also provides novel and efficient processes for the preparation of compounds of formulae II and III, and converting these to rosuvastatin of formula I or pharmaceutically acceptable salts thereof.

  本发明提供了一种工业上具有优势和经济效益的制备公式I或其药学上可接受的盐的罗伐司汀的过程，[公式I应在此处插入]，通过公式II和III的新型中间体。[公式II应在此处插入]，其中R从中选择，R1从氢，直链或支链烷基，优选为C1-C4；[公式III应在此处插入]。本发明还提供了制备公式II和III化合物的新型高效过程，并将其转化为公式I或其药学上可接受的盐的罗伐司汀。
• [EN] COMPOUNDS AND METHODS<br/>[FR] COMPOSES ET PROCEDES
  申请人：SMITHKLINE BEECHAM CORP

  公开号：WO2003031434A1

  公开（公告）日：2003-04-17

  Disclosed are compounds of formula (I) wherein the formula variables are as defined herein. The compounds of this invention are non-peptide, reversible inhibitors of type 2 methionine aminopeptidase. Also disclosed is the use of such compounds in treating conditions mediated by angiogenesis, such as cancer, haemangioma, proliferative retinopathy, rheumatoid arthritis, atherosclerotic neovascularization, psoriasis, ocular neovascularization and obesity.

  本发明揭示了式(I)的化合物，其中式变量如本文所定义。本发明的化合物是非肽类，可逆抑制剂，可抑制2型蛋氨酸氨肽酶。本发明还揭示了这些化合物在治疗由血管生成介导的疾病方面的用途，如癌症、血管瘤、增生性视网膜病变、类风湿性关节炎、动脉粥样硬化性新生血管形成、牛皮癣、眼部新生血管形成和肥胖症。
• Compounds and methods
  申请人：——

  公开号：US20040192914A1

  公开（公告）日：2004-09-30

  Disclosed are compounds of the formula: 1 wherein the formula variables are as defined herein. The compounds of this invention are non-peptide, reversible inhibitors of type 2 methionine aminopeptidase. Also disclosed is the use of such compounds in treating conditions mediated by angiogenesis, such as cancer, haemangioma, proliferative retinopathy, rheumatoid arthritis, atherosclerotic neovascularization, psoriasis, ocular neovascularization and obesity.

  本发明揭示了式1的化合物：其中式中的变量在此定义。本发明的化合物是非肽类、可逆抑制剂2型甲硫氨酰肽酶。本发明还揭示了这些化合物在治疗通过血管生成介导的疾病中的应用，例如癌症、血管瘤、增生性视网膜病变、类风湿性关节炎、动脉粥样硬化性新生血管形成、牛皮癣、眼部新生血管形成和肥胖症。