2-Amino-4-methyl-5-(pyridin-4-yl)thiazole | 94284-30-7

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 唑类
• 英文名称: 2-Amino-4-methyl-5-(pyridin-4-yl)thiazole
• 英文别名: 4-methyl-5-pyridin-4-yl-thiazol-2-ylamine；2-Amino-4-methyl-5-(4-pyridyl)thiazole；4-methyl-5-pyridin-4-yl-1,3-thiazol-2-amine
• CAS: 94284-30-7
• 化学式: C₉H₉N₃S
• mdl: MFCD11185024
• 分子量: 191.257
• InChiKey: FFLLFDZJLHNKDQ-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  1.6
• 重原子数：
  13
• 可旋转键数：
  1
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.111
• 拓扑面积：
  80
• 氢给体数：
  1
• 氢受体数：
  4

反应信息

• 作为反应物：
  描述：

  2-Amino-4-methyl-5-(pyridin-4-yl)thiazole 、 异氰酰乙酸乙酯 以 DMF (N,N-dimethyl-formamide) 为溶剂， 生成 [3-(4-methyl-5-pyridin-4-yl-thiazol-2-yl)-ureido]-acetic acid ethyl ester
  参考文献：
  名称：

  [EN] INHIBITORS OF PHOSPHATIDYLINOSITOL 3-KINASE
  [FR] INHIBITEURS DE PHOSPHATIDYLINOSITOL 3-KINASE

  摘要：

  式(I)中的化合物以自由形式或盐形式存在，其中R1、R2、R3和R4的含义如规范中所示，适用于治疗由磷脂酰肌醇3-激酶介导的疾病。还描述了含有这些化合物的药物组合物以及制备这些化合物的过程。

  公开号：

  WO2004096797A1

文献信息

• Thiazole derivatives and pharmaceutical composition comprising the same
  申请人：Fujisawa Pharmaceutical Co., Ltd.

  公开号：US04649146A1

  公开（公告）日：1987-03-10

  The invention relates to novel pharmaceutical compounds for treatment for ulcer of the formula: ##STR1## wherein R.sup.1 is lower alkyl, carboxy, hydroxymethyl, halomethyl, lower alkylthiomethyl or hydroxyiminomethyl, R.sup.2 is hydrogen, hydroxy, lower alkyl, pyridyl, amino, lower alkylamino, pyridylamino or guanidino optionally substituted with dimethylaminomethylene, R.sup.3 is dihydroisoquinolyl which may be substituted with halogen, lower alkyl, lower alkoxy, carboxy, hydroxy, pyridyl, amino, lower alkylamino, pyridylamino or guanidino, Q is --CO--, and n is an integer of 0 or 1, and pharmaceutically acceptable salts thereof.

  该发明涉及一种用于治疗溃疡的新型药物化合物，其化学式为：##STR1## 其中R.sup.1为较低的烷基、羧基、羟甲基、卤代甲基、较低的烷基硫甲基或羟基亚甲基，R.sup.2为氢、羟基、较低的烷基、吡啶基、氨基、较低的烷基氨基、吡啶基氨基或胍基，可选择地取代二甲氨基亚甲基，R.sup.3为二氢异喹啉基，可取代卤素、较低的烷基、较低的烷氧基、羧基、羟基、吡啶基、氨基、较低的烷基氨基、吡啶基氨基或胍基，Q为--CO--，n为0或1，以及其药学上可接受的盐。
• Inhibitors of phosphatidylinositol 3-kinase
  申请人：Bruce Ian

  公开号：US20070032487A1

  公开（公告）日：2007-02-08

  Compounds of formula I in free or salt form, wherein R 1 , R 2 , R 3 and R 4 have the meanings as indicated in the specification, are useful for treating conditions that are mediated by mediated by phosphatidylinositol 3-kinase. Pharmaceutical compositions that contain the compounds and a process for preparing the compounds are also described.

  公式I的化合物以自由或盐形式存在，其中R1、R2、R3和R4的含义如规范中所示，可用于治疗由磷脂酰肌醇3-激酶介导的疾病。还描述了含有这些化合物的制药组合物以及制备这些化合物的过程。
• 5-Heteroaryl Thiazoles And Their Use As PI3K Inhibitors
  申请人：Bengtsson Malena

  公开号：US20080132502A1

  公开（公告）日：2008-06-05

  The invention provides thiazole derivatives of formula (I), or pharmaceutically acceptable salts thereof in which Ring A, R 1 , R 2 and R 3 are as defined in the specification; a processes for their preparation; pharmaceutical compositions containing them; and their use in therapy, for example in the treatment of disease mediated by a PI3K enzyme and/or a mTOR kinase.

  本发明提供式(I)的噻唑衍生物或其药学上可接受的盐，其中环A、R1、R2和R3如说明书中所定义；一种制备它们的方法；含有它们的制药组合物；以及它们在治疗中的用途，例如用于治疗由PI3K酶和/或mTOR激酶介导的疾病。
• THIAZOLE DERIVATIVES AND THEIR USE AS ANTI-TUMOUR AGENTS
  申请人：Arnould Jean-Claude (Retired)

  公开号：US20090076009A1

  公开（公告）日：2009-03-19

  The invention concerns thiazole derivatives of Formula I or pharmaceutically-acceptable salts thereof, wherein each of R, Ring A, m, R 1 , R 2 and R 3 has any of the meanings defined hereinbefore in the description; processes for their preparation, pharmaceutical compositions containing them and their use in therapy, for example in the treatment of disease mediated by a PI3K enzyme and/or a mTOR kinase.

  本发明涉及式I的噻唑衍生物或其药学上可接受的盐，其中R、环A、m、R1、R2和R3中的每一个都具有前述描述中定义的任何含义；其制备方法、包含它们的制药组合物以及它们在治疗中的用途，例如用于治疗由PI3K酶和/或mTOR激酶介导的疾病。
• Organic compounds
  申请人：Bruce Ian

  公开号：US20100120865A1

  公开（公告）日：2010-05-13

  The present invention concerns a compound of formula (I), or a pharmaceutically acceptable salt, or solvate thereof, wherein the groups Ri-Rs are defined in the description, to compositions and use of the compounds in the treatment of diseases ameloriated by inhibition of phosphatidylinositol 3-kinase.

  本发明涉及一种式（I）的化合物，或其药学上可接受的盐或溶剂，其中Ri-Rs基团在说明中定义，以及该化合物在治疗通过抑制磷脂酰肌醇3-激酶改善的疾病中的组合物和用途。