4-(methoxymethyl)-2-methylthiazole | 478031-96-8

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 唑类
• 英文名称: 4-(methoxymethyl)-2-methylthiazole
• 英文别名: 4-(Methoxymethyl)-2-methyl-1,3-thiazole
• CAS: 478031-96-8
• 化学式: C₆H₉NOS
• 分子量: 143.21
• InChiKey: FCYNHRFLXBYSAQ-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  1
• 重原子数：
  9
• 可旋转键数：
  2
• 环数：
  1.0
• sp3杂化的碳原子比例：
  0.5
• 拓扑面积：
  50.4
• 氢给体数：
  0
• 氢受体数：
  3

反应信息

• 作为反应物：
  描述：

  4-(methoxymethyl)-2-methylthiazole 在 silver(II) sulfate 、 碘 作用下， 以 甲醇 为溶剂， 反应 16.0h， 以26%的产率得到5-iodo-4-methoxymethyl-2-methyl-thiazole
  参考文献：
  名称：

  [EN] COMT INHIBITORS
  [FR] INHIBITEURS DE COMT

  摘要：

  本发明涉及式(I)的化合物，其中取代基如权利要求1所述，并且其药学上可接受的盐。这些化合物抑制酶儿茶酚-O-甲基转移酶(COMT)。这些化合物可用于治疗帕金森病、抑郁症、认知障碍和运动症状、抗抑郁症、认知障碍、情绪和精神分裂症的消极症状。

  公开号：

  WO2014102233A1

文献信息

• 6-Heteroarylpyridoindolone Derivatives, Their Preparation and Therapeutic Use Thereof
  申请人：MUNEAUX Yvette

  公开号：US20080262020A1

  公开（公告）日：2008-10-23

  The disclosure relates to compounds of formula (I): wherein R 1 , R 2 , R 3 , R 4 , are R 5 are as defined in the disclosure; their preparation method, compositions containing the same and therapeutic use thereof.

  该公开涉及到式(I)的化合物： 其中R1、R2、R3、R4、R5如本公开所定义；它们的制备方法，含有这些化合物的组合物以及它们的治疗用途。
• [EN] 2,3-DIHYDRO-6-NITROIMIDAZO (2,1-B) OXAZOLE COMPOUNDS FOR THE TREATMENT OF TUBERCULOSIS<br/>[FR] COMPOSES 2,3-DIHYDRO-6-NITROIMIDAZO (2,1-B) OXAZOLE POUR LE TRAITEMENT DE LA TUBERCULOSE
  申请人：OTSUKA PHARMA CO LTD

  公开号：WO2005042542A1

  公开（公告）日：2005-05-12

  The present invention provides a 2,3-dihydro-6-nitroimidazo[2,1-b]oxazole compound represented by the following general formula: (1)in the above formula (1), R1 represents a hydrogen atom or C1-C6 alkyl group, n represents an integer of 0 to 6, R1 and -(CH2)nR2 may form a spiro ring represented by the formula (30) below, together with the adjacent carbon atom (in the formula below, RRR represents a piperidyl group which may have substituents on the piperidine ring), (30)and R2 represents a benzothiazolyloxy group, quinolyloxy group, pyridyloxy group or the like. The present compound has an excellent bactericidal action against Mycobacterium tuberculosis, multi-drug-resistant Mycobacterium tuberculosis, and atypical acid-fast bacteria.

  本发明提供了一种由以下一般式表示的2,3-二氢-6-硝基咪唑[2,1-b]噁唑化合物：(1)在上述式(1)中，R1代表氢原子或C1-C6烷基，n代表0至6的整数，R1和-(CH2)nR2可以与下面的式(30)一起形成一个螺环，与相邻的碳原子一起（在下面的式中，RRR代表可能在哌啶环上具有取代基的哌啶基），(30)和R2代表苯并噻唑氧基、喹啉氧基、吡啶氧基或类似物。该化合物对结核分枝杆菌、多药耐药结核分枝杆菌和非典型耐酸细菌具有出色的杀菌作用。
• Hsp90 family protein inhibitors
  申请人：Kitamura Yushi

  公开号：US20070155813A1

  公开（公告）日：2007-07-05

  wherein n is an integer of 0 to 10; R 1 represents substituted or unsubstituted lower alkyl, substituted or unsubstituted lower alkoxy, substituted or unsubstituted cycloalkyl, substituted or unsubstituted lower alkoxycarbonyl, substituted or unsubstituted heterocyclic-alkyl, substituted or unsubstituted aryl, —CONR 7 R 8 , —NR 9 R 10 , etc.; R 2 represents substituted or unsubstituted aryl or a substituted or unsubstituted heterocyclic group, etc.; R 3 and R 5 may be the same or different, each represent a hydrogen atom, substituted or unsubstituted lower alkyl, etc.; R 4 and R 6 may be the same or different, each represent a hydrogen atom, halogen, substituted or unsubstituted lower alkyl, etc.) Provided are an Hsp90 family protein inhibitor comprising, as an active ingredient, a benzene derivative of formula (I) or a prodrug thereof or a pharmaceutically-acceptable salt thereof, etc.

  其中n为0到10的整数；R1代表取代或未取代的低碳基、取代或未取代的低碳氧基、取代或未取代的环烷基、取代或未取代的低碳氧羰基、取代或未取代的杂环烷基、取代或未取代的芳基、-CONR7R8、-NR9R10等；R2代表取代或未取代的芳基或取代或未取代的杂环基等；R3和R5可以相同也可以不同，分别代表氢原子、取代或未取代的低碳基等；R4和R6可以相同也可以不同，分别代表氢原子、卤素、取代或未取代的低碳基等。提供了一种Hsp90家族蛋白抑制剂，其包括以下化合物作为活性成分：公式（I）的苯衍生物或其前药或其药学上可接受的盐等。
• 2,3-Dihydro-6-Nitroimidazo (2,1-b) Oxazole Compounds for the Treatment of Tuberculosis
  申请人：Tsubouchi Hidetsugu

  公开号：US20080119478A1

  公开（公告）日：2008-05-22

  The present invention provides a 2,3-dihydro-6-nitroimidazo[2,1-b]oxazole compound represented by the following general formula: (1) in the above formula (1), R1 represents a hydrogen atom or C1-C6 alkyl group, n represents an integer of 0 to 6, R1 and —(CH2) n R2 may form a spiro ring represented by the formula (30) below, together with the adjacent carbon atom (in the formula below, RRR represents a piperidyl group which may have substituents on the piperidine ring), (30) and R2 represents a benzothiazolyloxy group, quinolyloxy group, pyridyloxy group or the like. The present compound has an excellent bactericidal action against Mycobacterium tuberculosis , multi-drug-resistant Mycobacterium tuberculosis , and atypical acid-fast bacteria.

  本发明提供了一种由下述通式（1）表示的2,3-二氢-6-硝基咪唑[2,1-b]噁唑化合物： 在上述式（1）中，R1代表氢原子或C1-C6烷基，n代表0到6的整数，R1和—(CH2)nR2可以与相邻的碳原子形成如下式（30）所示的螺环，其中，在下式中，RRR代表可能在哌啶环上具有取代基的哌啶基： （30）且R2代表苯并噻唑氧基、喹啉氧基、吡啶氧基或类似基团。该化合物对结核分枝杆菌、多重耐药结核分枝杆菌和非典型酸杆菌具有优异的杀菌作用。
• FACTOR Xa INHIBITORS
  申请人：Jia Zhaozhong J.

  公开号：US20080293704A1

  公开（公告）日：2008-11-27

  The present invention is directed to compounds represented by Formula (I) or a pharmaceutically acceptable salt, ester, or prodrug thereof which are inhibitors of Factor Xa. The present invention is also directed to intermediates used in making such compounds, pharmaceutical compositions containing such compounds, methods to prevent or treat certain conditions characterized by undesired thrombosis and methods of inhibiting the coagulation of a blood sample.

  本发明涉及由公式（I）表示的化合物或其药学上可接受的盐、酯或前药，其为Xa因子的抑制剂。本发明还涉及用于制备这种化合物的中间体，包含这种化合物的制药组合物，预防或治疗某些由不希望的血栓形成所表现出的病症的方法，以及抑制血样的凝血作用的方法。