4-[(二甲基氨基)甲基]-1,3-噻唑-2-胺 | 116252-53-0

• 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-[(二甲基氨基)甲基]-1,3-噻唑-2-胺
• 英文名称: 4-((dimethylamino)methyl)thiazole-2-amine
• 英文别名: 2-amino-4-dimethylaminomethylthiazole；4-dimethylaminomethyl-2-aminothiazole；4-dimethylaminomethyl-thiazol-2-ylamine；4-[(dimethylamino)methyl]-1,3-thiazole-2-amine；4-[(Dimethylamino)methyl]-1,3-thiazol-2-amine
• CAS: 116252-53-0
• 化学式: C₆H₁₁N₃S
• mdl: MFCD11166509
• 分子量: 157.239
• InChiKey: HYQAPLLDHDEUSD-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  0.5
• 重原子数：
  10
• 可旋转键数：
  2
• 环数：
  1.0
• sp3杂化的碳原子比例：
  0.5
• 拓扑面积：
  70.4
• 氢给体数：
  1
• 氢受体数：
  4

反应信息

• 作为反应物：
  描述：

  4-[(二甲基氨基)甲基]-1,3-噻唑-2-胺 、 methyl 5-chlorospiro[indoline-3,3'-pyrrolidine]-1'-carboxylate 、 N,N'-羰基二咪唑 在 4-二甲氨基吡啶 作用下， 以 四氢呋喃 为溶剂， 反应 12.0h， 以34%的产率得到methyl 5-chloro-1-((4-((dimethylamino)methyl)thiazol-2-yl)carbamoyl)spiro[indoline-3,3'-pyrrolidine]-1'-carboxylate
  参考文献：
  名称：

  EP2781521

  摘要：

  公开号：
• 作为产物：
  描述：

  4-(chloromethyl)thiazol-2-amine hydrochloride 、 二甲胺 在 ice 、 乙酸乙酯 、 Brine 、 magnesium sulfate 、 silica gel 作用下， 以 水 为溶剂， 反应 1.0h， 以to give the title compound as white crystals (3.05 g, yield 53%)的产率得到4-[(二甲基氨基)甲基]-1,3-噻唑-2-胺
  参考文献：
  名称：

  Indole derivatives as somatostatin agonists or antagonists

  摘要：

  本发明提供了一种化合物(I)的公式，其中环A代表一种芳香环，可选地具有取代基; B、Y和Ya相同或不同，每个代表一种键等; R1和R2相同或不同，每个代表一个氢原子等; R3代表一个氢原子等; R4和R5相同或不同，每个代表一个氢等; R6代表一种吲哚基，可选地具有取代基; Z和Za相同或不同，每个代表一个氢原子等; 或其盐或前药，具有生长抑素受体结合抑制活性，并用于预防和/或治疗与生长抑素相关的疾病。

  公开号：

  US20060223826A1

文献信息

• [EN] AMINE COMPOUNDS<br/>[FR] DERIVES D'INDOLE SERVANT D'ANTAGONISTE DE SOMATOSTATINE
  申请人：TAKEDA CHEMICAL INDUSTRIES LTD

  公开号：WO2004046107A1

  公开（公告）日：2004-06-03

  The present invention provide a compound of the formula (I) wherein ring A represents an aromatic ring optionally having substituents; B, Y and Ya are the same or different and each represents a bond, etc.; R1 and R2 are the same or different and each represents a hydrogen atom, etc.; R3 represents a hydrogen atom, etc.; R4 and R5 are the same or different and each represents a hydrogen, etc.; R6 represents an indolyl group optionally having substituents; and Z and Za are the same or different and each represents a hydrogen atom, etc.; or a salt thereof or a prodrug thereof, having a somatostatin receptor binding inhibition activity and is useful for preventing and/or treating diseases associated with somatostatin.

  本发明提供了一种公式(I)的化合物，其中环A代表一个具有可选取代基的芳香环；B、Y和Ya相同或不同，分别代表一个键等；R1和R2相同或不同，每个代表一个氢原子等；R3代表一个氢原子等；R4和R5相同或不同，每个代表一个氢等；R6代表一个可选有取代基的吲哚基团；Z和Za相同或不同，每个代表一个氢原子等；或其盐或前药，具有生长抑素受体结合抑制活性，并且用于预防或治疗与生长抑素相关的疾病。
• Indole derivatives as somatostatin agonists or antagonists
  申请人：Abe Hidenori

  公开号：US20060223826A1

  公开（公告）日：2006-10-05

  The present invention provide a compound of the formula (I) wherein ring A represents an aromatic ring optionally having substituents; B, Y and Ya are the same or different and each represents a bond, etc.; R 1 and R 2 are the same or different and each represents a hydrogen atom, etc.; R 3 represents a hydrogen atom, etc.; R 4 and R 5 are the same or different and each represents a hydrogen, etc.; R 6 represents an indolyl group optionally having substituents; and Z and Za are the same or different and each represents a hydrogen atom, etc.; or a salt thereof or a prodrug thereof, having a somatostatin receptor binding inhibition activity and is useful for preventing and/or treating diseases associated with somatostatin.

  本发明提供了一种化合物(I)的公式，其中环A代表一种芳香环，可选地具有取代基; B、Y和Ya相同或不同，每个代表一种键等; R1和R2相同或不同，每个代表一个氢原子等; R3代表一个氢原子等; R4和R5相同或不同，每个代表一个氢等; R6代表一种吲哚基，可选地具有取代基; Z和Za相同或不同，每个代表一个氢原子等; 或其盐或前药，具有生长抑素受体结合抑制活性，并用于预防和/或治疗与生长抑素相关的疾病。
• RHO KINASE INHIBITORS
  申请人：Dahmann Georg

  公开号：US20100041645A1

  公开（公告）日：2010-02-18

  Substituted amide and urea derivatives useful as inhibitors of Rho kinase are described, which inhibitors can be useful in the treatment of various disorders such as cardiovascular diseases, cancer, neurological diseases, renal diseases, bronchial asthma, erectile dysfunction and glaucoma.

  本文介绍了一种替代酰胺和脲衍生物，这些衍生物可用作Rho激酶的抑制剂，在治疗心血管疾病、癌症、神经系统疾病、肾脏疾病、支气管哮喘、勃起功能障碍和青光眼等各种疾病中有用。
• NOVEL SPIROINDOLINE COMPOUND, AND MEDICINAL AGENT COMPRISING SAME
  申请人：KOWA COMPANY, LTD.

  公开号：US20140309207A1

  公开（公告）日：2014-10-16

  The present invention provides a novel compound represented by a general formula (1) as shown below, which has a glucokinase-activating action in the liver and pancreatic β-cells and which is useful as an agent for preventing and/or treating diseases caused by hyperglycemia, such as diabetes. A spiroindoline compound represented by the general formula (1), or a salt thereof, or a solvate of the compound or the salt: [wherein ring A represents a nitrogen-containing 5-10 membered heteroaryl group; R 1 and R 2 , which are the same or different, each represent a hydrogen atom, a halogen atom, a halo C 1-6 alkyl group, a C 6-10 aryl group, a cyano group, a C 1-6 alkyl group optionally having a substituent, a C 2-6 alkenyl group optionally having a substituent, etc.; R 3 represents a hydrogen atom, a C 1-6 alkyl group optionally having a substituent, etc.; and R 4 represents a hydrogen atom, a halogen atom, a C 1-6 alkyl group optionally having a substituent, etc.]

  本发明提供了一种新型化合物，其通式（1）如下所示，具有在肝脏和胰岛β细胞中激活葡萄糖激酶的作用，并可用作预防和/或治疗由高血糖引起的疾病，如糖尿病的药物。该通式（1）表示的螺环吲哚化合物，或其盐，或化合物或盐的溶剂：[其中环A代表含氮的5-10成员杂环基；R1和R2，相同或不同，分别代表氢原子，卤原子，卤代C1-6烷基，C6-10芳基，氰基，C1-6烷基，可选取代基，C2-6烯基，可选取代基等；R3代表氢原子，C1-6烷基，可选取代基等；R4代表氢原子，卤原子，C1-6烷基，可选取代基等。]
• Spiroindoline compound, and medicinal agent comprising same
  申请人：Kowa Company, Ltd.

  公开号：US08921576B2

  公开（公告）日：2014-12-30

  The present invention provides a novel compound represented by a general formula (1) as shown below, which has a glucokinase-activating action in the liver and pancreatic β-cells and which is useful as an agent for preventing and/or treating diseases caused by hyperglycemia, such as diabetes. A spiroindoline compound represented by the general formula (1), or a salt thereof, or a solvate of the compound or the salt: [wherein ring A represents a nitrogen-containing 5-10 membered heteroaryl group; R1 and R2, which are the same or different, each represent a hydrogen atom, a halogen atom, a halo C1-6 alkyl group, a C6-10 aryl group, a cyano group, a C1-6 alkyl group optionally having a substituent, a C2-6 alkenyl group optionally having a substituent, etc.; R3 represents a hydrogen atom, a C1-6 alkyl group optionally having a substituent, etc.; and R4 represents a hydrogen atom, a halogen atom, a C1-6 alkyl group optionally having a substituent, etc.]

  本发明提供了一种新型化合物，其通式（1）如下所示，具有在肝脏和胰岛β细胞中激活葡萄糖激酶的作用，并且可用作预防和/或治疗由高血糖引起的疾病，如糖尿病的药物。通式（1）表示的螺内酰胺化合物，或其盐，或化合物或盐的溶剂:[其中，环A表示含氮的5-10成员杂环基；R1和R2，它们相同或不同，每个表示氢原子，卤原子，卤代C1-6烷基，C6-10芳基，氰基，可选有取代基的C1-6烷基，可选有取代基的C2-6烯基等；R3表示氢原子，可选有取代基的C1-6烷基等；R4表示氢原子，卤原子，可选有取代基的C1-6烷基等。]