1-(5-溴噻唑-2-基)-4-甲基-哌嗪 | 623588-32-9

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 二嗪烷类
• 中文名称: 1-(5-溴噻唑-2-基)-4-甲基-哌嗪
• 英文名称: 1-(5-bromo-thiazol-2-yl)-4-methylpiperazine
• 英文别名: 5-bromo-2-(4-methylpiperazin-1-yl)thiazole；1-(5-Bromo-1,3-thiazol-2-yl)-4-methylpiperazine；5-bromo-2-(4-methylpiperazin-1-yl)-1,3-thiazole
• CAS: 623588-32-9
• 化学式: C₈H₁₂BrN₃S
• 分子量: 262.173
• InChiKey: GYJBJUJPIRBKDA-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  2.2
• 重原子数：
  13
• 可旋转键数：
  1
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.62
• 拓扑面积：
  47.6
• 氢给体数：
  0
• 氢受体数：
  4

反应信息

• 作为反应物：
  描述：

  6-溴-4-氯喹唑啉 、 1-(5-溴噻唑-2-基)-4-甲基-哌嗪 在 正丁基锂 、 异丙醇频哪醇硼酸酯 、 四(三苯基膦)钯 、 palladium diacetate 作用下， 以 四氢呋喃 、 正己烷 、 1,4-二氧六环 为溶剂， 反应 6.0h， 以27%的产率得到5-(6-bromoquinazolin-4-yl)-2-(4-methylpiperazin-1-yl)thiazole
  参考文献：
  名称：

  JP6378918

  摘要：

  公开号：
• 作为产物：
  描述：

  N-甲基哌嗪 、 2,5-二溴噻唑 在 氯仿 、 水 、 Sodium sulfate-III 、 crude material 、 silica gel 、 乙酸乙酯 作用下， 以 N,N-二异丙基乙胺 为溶剂， 反应 51.0h， 生成 1-(5-溴噻唑-2-基)-4-甲基-哌嗪
  参考文献：
  名称：

  2-aminopyridine kinase inhibitors

  摘要：

  具有I式结构的2-氨基吡啶化合物，以及这些化合物的药学上可接受的盐。I式化合物抑制动物（包括人类）中的酪氨酸激酶酶活性，并在治疗和/或预防各种疾病和病况方面有用。特别地，本文披露的化合物是激酶抑制剂，特别是但不限于KDR，Tie-2，Flt3，FGFR3，Ab1，Aurora A，c-Src，IGF-1R，ALK，c-MET，RON，PAK1，PAK2和TAK1，并可用于治疗增殖性疾病，例如但不限于癌症。本发明还涉及一种制备药物组合物的方法，该组合物包括I式化合物或其药学上可接受的盐的治疗有效量以及药学上可接受的载体。本发明还涉及一种通过向患有蛋白激酶活性介导的病症的患者投与上述药物组合物的治疗方法。

  公开号：

  US08178668B2

文献信息

• PYRIDINE AND PYRAZINE DERIVATIVES - 083
  申请人：Barlaam Bernard Christophe

  公开号：US20090118305A1

  公开（公告）日：2009-05-07

  The invention concerns pyridine and pyrazine derivatives of Formula I or a pharmaceutically-acceptable salt thereof, wherein each of W, G 1 , G 2 , G 3 , G 4 , J, Ring A, n 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 the manufacture of a medicament for use in the treatment of cell proliferative disorders.

  本发明涉及式I的吡啶和吡嗪衍生物 或其药用可接受的盐，其中W、G 1 、G 2 、G 3 、G 4 、J、环A、n和R 3 各自具有如前文描述中定义的任何含义；它们的制备过程，包含它们的药物组合物以及它们在制造用于治疗细胞增殖性障碍的药物中的应用。
• 2-AMINOPYRIDINE KINASE INHIBITORS
  申请人：Steinig Arno G.

  公开号：US20090197862A1

  公开（公告）日：2009-08-06

  2-Aminopyridine compounds having the structure of Formula I, and pharmaceutically acceptable salts of these compounds. Compounds of Formula I inhibit the activity of tyrosine kinase enzymes in animals, including humans, and are useful in the treatment and/or prevention of various diseases and conditions. In particular, compounds disclosed herein are inhibitors of kinases, in particular, but not limited to, KDR, Tie-2, Flt3, FGFR3, Ab1, Aurora A, c-Src, IGF-1R, ALK, c-MET, RON, PAK1, PAK2, and TAK1, and can be used in the treatment of proliferative diseases, such as, but not limited to, cancer. The present invention is also directed to a pharmaceutical composition comprising a therapeutically effective amount of a compound of Formula I, or a pharmaceutically acceptable salt thereof, and a pharmaceutically acceptable carrier. The present invention is further directed to a method of treating a patient having a condition which is mediated by protein kinase activity by administering to the patient a therapeutically effective amount of the above-mentioned pharmaceutical composition.

  具有Formula I结构的2-氨基吡啶化合物，以及这些化合物的药用可接受的盐。Formula I的化合物抑制动物（包括人类）中的酪氨酸激酶酶活性，并可用于治疗和/或预防各种疾病和病况。特别地，本文披露的化合物是激酶抑制剂，特别是但不限于KDR、Tie-2、Flt3、FGFR3、Ab1、Aurora A、c-Src、IGF-1R、ALK、c-MET、RON、PAK1、PAK2和TAK1，并可用于治疗增生性疾病，如但不限于癌症。本发明还涉及一种包含Formula I化合物的药物组合物，或其药用可接受的盐，以及药用可接受的载体的药物组合物。本发明还涉及一种通过向患有由蛋白激酶活性介导的病症的患者投与上述药物组合物的治疗方法。
• IRE-1α inhibitors
  申请人：Zeng Qingping

  公开号：US09493435B2

  公开（公告）日：2016-11-15

  The invention provides compounds which directly inhibit IRE-1α activity in vitro, prodrugs, and pharmaceutically acceptable salts thereof. Such compounds and prodrugs are useful for treating diseases associated with the unfolded protein response and can be used as single agents or in combination therapies.

  该发明提供了一些化合物，可以直接抑制体外中的IRE-1α活性，还有它们的前药和药用盐。这些化合物和前药对治疗与未折叠蛋白反应相关的疾病有用，可以作为单一药物或与其他药物组合治疗。
• Inhibitors of histone deacetylase
  申请人：Stokes Elizabeth Elaine Sophie

  公开号：US20050222410A1

  公开（公告）日：2005-10-06

  The invention concerns a compound of the formula (I); wherein Ring A is heterocyclyl; m is 0-4 and each R 1 is a group such as hydroxy, halo, trifluoromethyl and cyano; Ring B is ring such as thienyl, thiadiazolyl, thiazolyl, pyrimidyl, pyrazinyl, pyridazinyl and pyridyl; R 2 is halo and n is 0-2; and each R 4 is a group such as hydroxy, halo, trifluoromethyl and cyano; p is 0-4; and R 3 is amino or hydroxy; or pharmaceutically-acceptable salts or in-vivo-hydrolysable ester or amide thereof; processes for their preparation, pharmaceutical compositions containing them and their use in the treatment of diseases or medical conditions mediated by histone deacetylase.

  本发明涉及式(I)的化合物；其中环A是杂环基；m为0-4，每个R1为羟基、卤素、三氟甲基和氰基等基团；环B是噻吩基、噻二唑基、噻唑基、嘧啶基、吡嗪基、吡啶并嘧啶基和吡啶基等环基；R2为卤素，n为0-2；每个R4为羟基、卤素、三氟甲基和氰基等基团；p为0-4；R3为氨基或羟基；或其药学上可接受的盐或体内可水解的酯或酰胺；其制备方法、含有它们的制药组合物以及它们在治疗组织脱乙酰化酶介导的疾病或医学状况中的应用。
• 2-aminopyridine kinase inhibitors
  申请人：OSI Pharmaceuticals, LLC

  公开号：US08178668B2

  公开（公告）日：2012-05-15

  2-Aminopyridine compounds having the structure of Formula I, and pharmaceutically acceptable salts of these compounds. Compounds of Formula I inhibit the activity of tyrosine kinase enzymes in animals, including humans, and are useful in the treatment and/or prevention of various diseases and conditions. In particular, compounds disclosed herein are inhibitors of kinases, in particular, but not limited to, KDR, Tie-2, Flt3, FGFR3, Ab1, Aurora A, c-Src, IGF-1R, ALK, c-MET, RON, PAK1, PAK2, and TAK1, and can be used in the treatment of proliferative diseases, such as, but not limited to, cancer. The present invention is also directed to a pharmaceutical composition comprising a therapeutically effective amount of a compound of Formula I, or a pharmaceutically acceptable salt thereof, and a pharmaceutically acceptable carrier. The present invention is further directed to a method of treating a patient having a condition which is mediated by protein kinase activity by administering to the patient a therapeutically effective amount of the above-mentioned pharmaceutical composition.

  具有I式结构的2-氨基吡啶化合物，以及这些化合物的药学上可接受的盐。I式化合物抑制动物（包括人类）中的酪氨酸激酶酶活性，并在治疗和/或预防各种疾病和病况方面有用。特别地，本文披露的化合物是激酶抑制剂，特别是但不限于KDR，Tie-2，Flt3，FGFR3，Ab1，Aurora A，c-Src，IGF-1R，ALK，c-MET，RON，PAK1，PAK2和TAK1，并可用于治疗增殖性疾病，例如但不限于癌症。本发明还涉及一种制备药物组合物的方法，该组合物包括I式化合物或其药学上可接受的盐的治疗有效量以及药学上可接受的载体。本发明还涉及一种通过向患有蛋白激酶活性介导的病症的患者投与上述药物组合物的治疗方法。