4-氯-2-甲氧基甲基嘧啶 | 105950-89-8

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 二嗪类
• 中文名称: 4-氯-2-甲氧基甲基嘧啶
• 英文名称: 4-chloro-2-(methoxymethyl)pyrimidine
• 英文别名: 4-chloro-2-methyloxymethylpyrimidine；2-methoxymethyl-4-chloropyrimidine
• CAS: 105950-89-8
• 化学式: C₆H₇ClN₂O
• 分子量: 158.587
• InChiKey: UQVFDJMABYSNMW-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  0.9
• 重原子数：
  10
• 可旋转键数：
  2
• 环数：
  1.0
• sp3杂化的碳原子比例：
  0.33
• 拓扑面积：
  35
• 氢给体数：
  0
• 氢受体数：
  3

反应信息

• 作为反应物：
  描述：

  4-氯-2-甲氧基甲基嘧啶 在 二甲胺 作用下， 以 乙醇 、 水 为溶剂， 生成 2-methoxymethyl-4-dimethylaminopyrimidine
  参考文献：
  名称：

  Pyrimidylalkylthio benzimidale compounds, pharmaceutical compositions

  摘要：

  本发明涉及2-和4-嘧啶甲基磺酰基（和硫）苯并咪唑，其中嘧啶基被一个可选择取代的氨基基团取代。这些化合物可以抑制外源性和内源性刺激的胃酸分泌。

  公开号：

  US04777172A1
• 作为产物：
  描述：

  2-(甲氧基甲基)-4(1H)-嘧啶酮 在 三氯氧磷 作用下， 生成 4-氯-2-甲氧基甲基嘧啶
  参考文献：
  名称：

  Substituted thienoimidazole derivatives, a process for the preparation

  摘要：

  取代噻唑咪唑衍生物，其制备方法，含有它们的药物组合物，以及将其用作胃酸分泌抑制剂、胃粘膜保护剂和治疗肠道炎症的药物的用途。该发明涉及以下式的化合物：其中A代表T表示-S-、-SO-或-SO2-，R1至R10、X、Y和Z的含义如描述中所示，以及其制备方法、含有它们的药物组合物，以及将其用作胃酸分泌抑制剂、胃粘膜保护剂和治疗肠道炎症的用途。

  公开号：

  US04956366A1

文献信息

• Raf inhibitor compounds and methods of use thereof
  申请人：Miknis Greg

  公开号：US20070049603A1

  公开（公告）日：2007-03-01

  Compounds of Formula I are useful for inhibiting Raf kinase and for treating disorders mediated thereby. Methods of using compounds of Formula I, and stereoisomers, geometric isomers, tautomers, solvates and pharmaceutically acceptable salts thereof, for in vitro, in situ, and in vivo diagnosis, prevention or treatment of such disorders in mammalian cells, or associated pathological conditions are disclosed.

  公式I的化合物对抑制Raf激酶和治疗由此介导的疾病有用。公开了使用公式I的化合物及其立体异构体、几何异构体、互变异构体、溶剂合物和药学上可接受的盐，在哺乳动物细胞中进行体外、体内和体内诊断、预防或治疗此类疾病或相关病理条件的方法。
• Substituted thienoimidazole derivatives, a process for the preparation
  申请人：Hoechst Aktiengesellschaft

  公开号：US04956366A1

  公开（公告）日：1990-09-11

  Substituted thienoimidazole derivatives, a process for the preparation thereof, pharmaceutical compositions containing them, and the use thereof as inhibitors of gastric acid secretion, as gastroprotectives and as medicaments for intestinal inflammations The invention relates to compounds of the formula ##STR1## in which A represents ##STR2## T denotes --S--, --SO-- or --SO.sub.2 --, R.sup.1 to R.sup.10, X, Y and Z have the meanings indicated in the description, to a process for the preparation thereof, to pharmaceutical compositions containing them, and to the use thereof as inhibitors of gastric acid secretion, as gastroprotectives and as medicaments for intestinal inflammations.

  取代噻唑咪唑衍生物，其制备方法，含有它们的药物组合物，以及将其用作胃酸分泌抑制剂、胃粘膜保护剂和治疗肠道炎症的药物的用途。该发明涉及以下式的化合物：其中A代表T表示-S-、-SO-或-SO2-，R1至R10、X、Y和Z的含义如描述中所示，以及其制备方法、含有它们的药物组合物，以及将其用作胃酸分泌抑制剂、胃粘膜保护剂和治疗肠道炎症的用途。
• [EN] AMINOPYRIMIDINES AS SORBITOL DEHYDROGENASE INHIBITORS<br/>[FR] AMINOPYRIMIDINES COMME INHIBITEURS DE SORBITOL DESHYDROGENASE
  申请人：PFIZER PROD INC

  公开号：WO2000059510A1

  公开（公告）日：2000-10-12

  This invention is directed to sorbitol dehydrogenase inhibitory compounds of formula (I), wherein R?1, R2 and R3¿ are as defined in the specification. This invention is also directed to pharmaceutical compositions containing those compounds and methods of treating or preventing diabetic complications, particularly diabetic neuropathy, diabetic nephropathy, diabetic microangiopathy, diabetic macroangiopathy and diabetic cardiomyopathy by administering such compounds to a mammal suffering from diabetes and therefor at risk for developing such complications. This invention is also directed to pharmaceutical compositions comprising a combination of a compound of formula (I) of this invention with an aldose reductase inhibitor and to methods of treating or preventing diabetic complications therewith. This invention is also directed to pharmaceutical compositions comprising a combination of a compound of formula (I) of this invention with an NHE-1 inhibitor and to methods of treating cardiomyopathy and other heart-related problems therewith. This invention is also directed to certain intermediates used in the synthesis of the compounds of formula (I) and to processes for preparing those intermediates.

  本发明涉及式（I）的山梨醇脱氢酶抑制剂，其中R1、R2和R3在说明书中定义。本发明还涉及含有这些化合物的药物组合物，以及通过将这些化合物用于患有糖尿病并因此有患上这些并发症风险的哺乳动物进行治疗或预防糖尿病并发症，特别是糖尿病神经病变、糖尿病肾病、糖尿病微血管病、糖尿病大血管病和糖尿病心肌病的方法。本发明还涉及一种包含本发明式（I）化合物和醛还原酶抑制剂的药物组合物以及用于治疗或预防糖尿病并发症的方法。本发明还涉及一种包含本发明式（I）化合物和NHE-1抑制剂的药物组合物以及用于治疗心肌病和其他心脏相关问题的方法。本发明还涉及用于合成式（I）化合物的某些中间体以及制备这些中间体的方法。
• Sorbitol dehydrogenase inhibitors
  申请人：——

  公开号：US20040077671A1

  公开（公告）日：2004-04-22

  This invention is directed to sorbitol dehydrogenase inhibitory compounds of the formula I, 1 wherein R 1 , R 2 and R 3 are as defined in the specification. This invention is also directed to pharmaceutical compositions containing those compounds and methods of treating or preventing diabetic complications, particularly diabetic neuropathy, diabetic nephropathy, diabetic microangiopathy, diabetic macroangiopathy and diabetic cardiomyopathy by administering such compounds to a mammal suffering from diabetes and therefore at risk for developing such complications. This invention is also directed to pharmaceutical compositions comprising a combination of a compound of formula I of this invention with an aldose reductase inhibitor and to methods of treating or preventing diabetic complications therewith. This invention is also directed to pharmaceutical compositions comprising a combination of a compound of formula I of this invention with an NHE-1 inhibitor and to methods of treating cardiomyopathy and other heart-related problems therewith. This invention is also directed to certain intermediates used in the synthesis of the compounds of formula I and to processes for preparing those intermediates.

  本发明涉及公式I的山梨醇脱氢酶抑制剂，其中R1、R2和R3如规范中所定义。本发明还涉及含有这些化合物的制药组合物以及通过向患有糖尿病且因此有发展这些并发症风险的哺乳动物投与这些化合物来治疗或预防糖尿病并发症，特别是糖尿病神经病、糖尿病肾病、糖尿病微血管病、糖尿病大血管病和糖尿病心肌病的方法。本发明还涉及一种公式I化合物与醛糖还原酶抑制剂的组合物制药组合物以及用于治疗或预防糖尿病并发症的方法。本发明还涉及一种公式I化合物与NHE-1抑制剂的组合物制药组合物以及用于治疗心肌病和其他心脏相关问题的方法。本发明还涉及用于合成公式I化合物的某些中间体以及制备这些中间体的方法。
• Salts of zopolrestat
  申请人：——

  公开号：US20010056095A1

  公开（公告）日：2001-12-27

  This invention relates to [4-oxo-(5-trifluoromethyl-benzothiazol-2-ylmethyl)-3,4-dihydro-phthalazin-1-yl]-acetic acid ethanolamine salt, pharmaceutical compositions thereof and methods of treating diabetic complications in mammals comprising administering to said mammals said salt and said compositions. This invention is also directed to combinations of said diethylamine salt with NHE-1 inhibitors, selective serotonin retuptake inhibitors (SSRIs), glycogen phosphorylase inhibitors (GPIs), sorbitol dehydrogenase inhibitors (SDIs) and antihypertensive agents. Said combinations are useful in treating diabetic complications in mammals.

  本发明涉及[4-氧代-(5-三氟甲基苯并噻唑-2-基甲基)-3,4-二氢-邻苯二氮平-1-基]-乙酸乙醇胺盐，以及其制药组合物和治疗哺乳动物糖尿病并发症的方法，包括向该哺乳动物施用该盐和该组合物。本发明还涉及将该二乙酰胺盐与NHE-1抑制剂、选择性5-羟色胺再摄取抑制剂（SSRIs）、糖原磷酸化酶抑制剂（GPIs）、山梨醇脱氢酶抑制剂（SDIs）和降压药物组合的方法。该组合物在治疗哺乳动物糖尿病并发症方面具有用途。