4-(2,5-二氟苯基)-1,3-噻唑-2-胺 | 383132-01-2

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 唑类
• 中文名称: 4-(2,5-二氟苯基)-1,3-噻唑-2-胺
• 英文名称: 2-amino-4-(2,5-difluorophenyl)thiazole
• 英文别名: 4-(2,5-Difluorophenyl)-1,3-thiazol-2-amine
• CAS: 383132-01-2
• 化学式: C₉H₆F₂N₂S
• mdl: MFCD02663893
• 分子量: 212.223
• InChiKey: PYWJLXKHBXFBDN-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  2.5
• 重原子数：
  14
• 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：
  67.2
• 氢给体数：
  1
• 氢受体数：
  5

反应信息

• 作为反应物：
  描述：

  (R)-2-苄基丁二酸 4-叔丁酯 、 4-(2,5-二氟苯基)-1,3-噻唑-2-胺 生成 (R)-3-benzyl-4-((4-(2,5-difluorophenyl)thiazol-2-yl)amino)-4-oxobutanoic acid
  参考文献：
  名称：

  COMPOUNDS, PHARMACEUTICAL COMPOSITION AND METHODS FOR USE IN TREATING METABOLIC DISORDERS

  摘要：

  本发明涉及式（I）的新化合物及其在治疗代谢性疾病方面的应用。

  公开号：

  US20110230477A1
• 作为产物：
  描述：

  2,5-二氟苯乙酮 、 硫脲 、 以the same operation as the Example 395(1) gave the title compound的产率得到4-(2,5-二氟苯基)-1,3-噻唑-2-胺
  参考文献：
  名称：

  ANTIALLERGIC AGENTS

  摘要：

  一种预防和/或治疗过敏性疾病和/或子宫内膜异位症和/或子宫肌瘤的药物，其包括以下通式（I）所表示的化合物或其药学上可接受的盐、水合物和溶剂化物作为活性成分，其中X表示连接基，其主链中原子数为2至5（该连接基可以被取代），A表示氢原子或乙酰基，E表示芳基或取代的杂芳基，环Z表示苯环，除了由公式-O-A表示的基团，该苯环还可以具有一个或多个取代基团，其中A的含义与上述定义相同，而由公式-X-E表示的基团中，每个X和E的含义也与上述定义相同，或者是一个杂环，除了由公式-O-A表示的基团，该杂环还可以具有一个或多个取代基团，其中A的含义与上述定义相同，而由公式-X-E表示的基团中，每个X和E的含义也与上述定义相同。

  公开号：

  US20080090779A1

文献信息

• THERAPEUTIC COMPOUNDS AND RELATED METHODS OF USE
  申请人：Suzuki Masaki

  公开号：US20150307477A1

  公开（公告）日：2015-10-29

  Methods of treating disorders using compounds that modulate striatal-enriched tyrosine phosphatase (STEP) are described herein. Exemplary disorders include schizophrenia and cognitive deficit.

  本文描述了利用调节纹状体富集的酪氨酸磷酸酶（STEP）的化合物来治疗疾病的方法。示例疾病包括精神分裂症和认知缺陷。
• Metabotropic glutamate receptor modulators
  申请人：Kalvinsh Ivars

  公开号：US20070299113A1

  公开（公告）日：2007-12-27

  The invention relates to imidazothiazole derivatives as well as their pharmaceutically acceptable salts. The invention further relates to a process for the preparation of such compounds. The compounds of the invention are group I mGluR modulators and are therefore useful for the control and prevention of various disorders, including acute and/or chronic neurological disorders.

  该发明涉及咪唑硫唑衍生物及其药用可接受的盐。该发明还涉及一种制备此类化合物的方法。该发明的化合物是I类mGluR调节剂，因此对于控制和预防各种疾病，包括急性和/或慢性神经系统疾病，具有用处。
• Nf-kb activation inhibitors
  申请人：Muto Susumu

  公开号：US20060089395A1

  公开（公告）日：2006-04-27

  A medicament having inhibitory activity against NF-κB activation which comprises as an active ingredient a substance selected from the group consisting of a compound represented by the following general formula (I) and a pharmacologically acceptable salt thereof, and a hydrate thereof and a solvate thereof: wherein A represents hydrogen atom or acetyl group, E represents a 2,5-di-substituted or a 3,5-di-substituted phenyl group, or a monocyclic or a fused polycyclic heteroaryl group which may be substituted, provided that the compound wherein said heteroaryl group is circle around (1)} a fused polycyclic heteroaryl group wherein the ring which binds directly to —CONH— group in the formula (I) is a benzene ring, circle around (2)} unsubstituted thiazol-2-yl group, or circle around (3)} unsubstituted benzothiazol-2-yl group is excluded, ring Z represents an arene which may have one or more substituents in addition to the group represented by formula —O-A wherein A has the same meaning as that defined above and the group represented by formula —CONH-E wherein E has the same meaning as that defined above, or a heteroarene which may have one or more substituents in addition to the group represented by formula —O-A wherein A has the same meaning as that defined above and the group represented by formula —CONH-E wherein E has the same meaning as that defined above.

  一种药物具有抑制NF-κB活化作用，其包括以下通式(I)所表示的化合物或其药学上可接受的盐、水合物和溶剂化物作为活性成分，其中A代表氢原子或乙酰基，E代表2,5-二取代或3,5-二取代苯基或单环或融合的多环杂环芳基，其可以被取代，但在所述杂环芳基是圆圈(1)}在公式(I)中直接结合—CONH—基团的环为苯环的融合多环杂环芳基，圆圈(2)}未取代的噻唑-2-基团，或者圆圈(3)}未取代的苯并噻唑-2-基团时，不包括该化合物，环Z代表一个芳香烃，除了由公式—O-A所表示的基团外，它也可以有一个或多个取代基，其中A具有与上述定义相同的含义，公式—CONH-E所表示的基团E具有与上述定义相同的含义。
• Inhibitors against the activation of ap-1 and nfat
  申请人：Muto Susumu

  公开号：US20060100257A1

  公开（公告）日：2006-05-11

  A medicament inhibiting the activation of AP-1 which comprises as an active ingredient a substance selected from the group consisting of a compound represented by the following general formula (I) and a pharmacologically acceptable salt thereof, and a hydrate thereof and a solvate thereof: wherein X represents a connecting group whose number of atoms in the main chain is 2 to 5 (said connecting group may be substituted), A represents hydrogen atom or acetyl group, E represents an aryl group which may be substituted or a hetero aryl group which may be substituted, ring Z represents an arene which may have one or more substituents in addition to the group represented by formula —O-A wherein A has the same meaning as that defined above and the group represented by formula —X-E wherein each of X and E has the same meaning as that defined above, or a heteroarene which may have one or more substituents in addition to the group represented by formula —O-A wherein A has the same meaning as that defined above and the group represented by formula —X-E wherein each of X and E has the same meaning as that defined above.

  一种药物，抑制AP-1的激活，其活性成分为以下通式（I）所表示的化合物或其药学上可接受的盐、水合物或溶剂化物中所选的一种，其中X代表连接基，其主链中的原子数为2至5（该连接基可以被取代），A代表氢原子或乙酰基，E代表芳基或取代的杂芳基，环Z代表芳烃，除了由式—O-A所表示的基团外，可能还有一个或多个取代基，其中A具有上述定义的相同含义，由式—X-E所表示的基团中，X和E的每一个具有上述定义的相同含义，或者是一个杂芳烃，可能还有一个或多个取代基，其中A具有上述定义的相同含义，由式—X-E所表示的基团中，X和E的每一个具有上述定义的相同含义。
• Medicament for treatment of diabetes
  申请人：Muto Susumu

  公开号：US20060111409A1

  公开（公告）日：2006-05-25

  A medicament for preventive and/or therapeutic treatment of diabetes or complications of diabetes which comprises as an active ingredient a substance selected from the group consisting of a compound represented by the following general formula (I) and a pharmacologically acceptable salt thereof, and a hydrate thereof and a solvate thereof: wherein X represents a connecting group whose number of atoms in the main chain is 2 to 5 (said connecting group may be substituted), A represents hydrogen atom or acetyl group, E represents an aryl group which may be substituted or a hetero aryl group which may be substituted, ring Z represents an arene which may have one or more substituents in addition to the group represented by formula —O— A wherein A has the same meaning as that defined above and the group represented by formula —X-E wherein each of X and E has the same meaning as that defined above, or a heteroarene which may have one or more substituents in addition to the group represented by formula —O-A wherein A has the same meaning as that defined above and the group represented by formula —X-E wherein each of X and E has the same meaning as that defined above.

  一种用于预防和/或治疗糖尿病或糖尿病并发症的药物，其活性成分为以下通式（I）所表示的化合物或其药学上可接受的盐、水合物或溶剂化物之一： 其中，X代表主链中原子数为2到5的连接基（该连接基可以被取代），A代表氢原子或乙酰基，E代表可以被取代的芳基或杂环芳基，环Z代表可以具有一个或多个取代基的芳基，除了由公式—O—A所表示的基团外，该芳基可以具有公式—X-E所表示的基团，其中每个X和E的含义与上述定义相同，或者可以具有一个或多个取代基的杂环芳基，除了由公式—O—A所表示的基团外，该杂环芳基可以具有公式—X-E所表示的基团，其中每个X和E的含义与上述定义相同。