4-(4-Methyl-piperazin-1-ylmethyl)-N-[4-methyl-3-(4-pyridin-2-yl-thiazol-2-ylamino)-phenyl]-benzamide

• 分子结构分类: 有机化合物 - 苯类化合物 - 苯和取代衍生物
• 英文名称: 4-(4-Methyl-piperazin-1-ylmethyl)-N-[4-methyl-3-(4-pyridin-2-yl-thiazol-2-ylamino)-phenyl]-benzamide
• 英文别名: 4-[(4-methylpiperazin-1-yl)methyl]-N-[4-methyl-3-[(4-pyridin-2-yl-1,3-thiazol-2-yl)amino]phenyl]benzamide
• 化学式: C₂₈H₃₀N₆OS
• 分子量: 498.6
• InChiKey: DPMDFBZMFUUHEC-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  4.3
• 重原子数：
  36
• 可旋转键数：
  7
• 环数：
  5.0
• sp3杂化的碳原子比例：
  0.25
• 拓扑面积：
  102
• 氢给体数：
  2
• 氢受体数：
  7

反应信息

• 作为反应物：
  描述：

  N-{4-Methyl-3-[4-(5-methyl-pyridin-3-yl)-thiazol-2-ylamino]-phenyl}-4-(4-methyl-piperazin-1-ylmethyl)-benzamide 、 3-Iodo-4(4-methyl-piperazin-1-ylmethyl)-N-[4-methyl-3-(4-pyridin-3-yl-thiazol-2-ylmethyl)-phenyl]-benzamide 、 N-[4-Methyl-3-(4-pyridin-3-yl-thiazol-2-ylamino)-phenyl]-4-[3-(4-trifluoromethyl-phenyl)-ureidomethyl]-benzamide 、 、 3,5-Dibromo-N-[4-methyl-3-(4-pyridin-3-yl-thiazol-2-ylamino)-phenyl]-4-piperidin-1-ylmethyl-benzamide 、 4-(4-Methyl-piperazin-1-ylmethyl)-N-[4-methyl-3-(4-pyridin-2-yl-thiazol-2-ylamino)-phenyl]-benzamide 、 N-{3-[4-(3-Fluoro-phenyl)-thiazol-2-ylamino]-4-methyl-phenyl}-4-(4-methyl-piperazin-1-ylmethyl)-benzamide 、 生成 4-(1-Methoxy-ethyl)-N-[4-methyl-3-(4-pyridin-3-yl-thiazol-2-ylmethyl)-phenyl]-benzamide
  参考文献：
  名称：

  2-(3-aminoaryl)amino-4-aryl-thiazoles and their use as c-kit inhibitors

  摘要：

  从公式（I）的2-（3-氨基芳基）氨基-4-芳基噻唑中选择的新化合物，可以选择性地调节、调控和/或抑制某些与细胞增殖、代谢、过敏和退行性疾病有关的原生和/或突变酪氨酸激酶介导的信号传导。更具体地说，这些化合物是有效而选择性的c-kit抑制剂。

  公开号：

  US20050239852A1

文献信息

• [EN] 2-(3-AMINOARYL)AMINO-4-ARYL-THIAZOLES AND THEIR USE AS C-KIT INHIBITORS<br/>[FR] 2-(3-AMINOARYL)AMINO-4-ARYL-THIAZOLES ET LEUR UTILISATION EN TANT QUE INHIBITEURS DE C-KIT
  申请人：AB SCIENCE

  公开号：WO2004014903A1

  公开（公告）日：2004-02-19

  The present invention relates to novel compounds selected from 2-(3-aminoaryl)amino-4-aryl-thiazoles of formula (I) that selectively modulate, regulate, and/or inhibit signal transductions mediated by certain native and/or mutant tyrosine kinases implicated in a variety of human and animal diseases such as cell proliferative, metabolic, allergic, and degenerative disorders. More particularly, these compounds are potent and selective c-kit inhibitors.

  本发明涉及从式（I）的2-(3-氨基芳基)氨基-4-芳基噻唑中选择的新化合物，该化合物能选择性地调节、调控和/或抑制由某些参与多种人类和动物疾病的一些天然和/或突变酪氨酸激酶介导的信号传导，如细胞增殖、代谢、过敏和变性障碍。更具体地说，这些化合物是有效且选择性的c-kit抑制剂。
• [EN] USE OF C-KIT INHIBITORS FOR TREATING TYPE II DIABETES<br/>[FR] UTILISATION D'INHIBITEURS DE C-KIT POUR LE TRAITEMENT DU DIABETE DE TYPE II
  申请人：AB SCIENCE

  公开号：WO2005016323A2

  公开（公告）日：2005-02-24

  The present invention relates to a method for treating type II diabetes, comprising administering a compound capable of depleting mast cells to a human in need of such treatment. Such compounds can be chosen from non-toxic, selective and potent c-kit inhibitors.

  本发明涉及一种治疗II型糖尿病的方法，包括向需要此类治疗的人类施用能够耗竭肥大细胞的化合物。这样的化合物可以选择来自无毒、选择性和有效的c-kit抑制剂。
• Use of c-kit inhibitors for treating type II diabetes
  申请人：Moussy Alain

  公开号：US20070032521A1

  公开（公告）日：2007-02-08

  The present invention relates to a method for treating type II diabetes, comprising administering a compound capable of depleting mast cells to a human in need of such treatment. Such compounds can be chosen from non-toxic, selective and potent c-kit inhibitors.

  本发明涉及一种治疗II型糖尿病的方法，包括向需要此类治疗的人类施用能够消耗肥大细胞的化合物。这些化合物可以选择来自非毒性、选择性和有效的c-kit抑制剂。
• [EN] USE OF TYROSINE KINASE INHIBITORS FOR TREATING CEREBRAL ISCHEMIA<br/>[FR] UTILISATION D'INHIBITEURS DE TYROSINE KINASE POUR LE TRAITEMENT DE L'ISCHEMIE CEREBRALE
  申请人：AB SCIENCE

  公开号：WO2004096225A2

  公开（公告）日：2004-11-11

  The present invention relates to a method for treating cerebral ischemia, comprising administering a compound capable of depleting mast cells or a compound inhibiting mast cells degranulation to a human in need of such treatment. Such compounds can be chosen from tyrosine kinase inhibitors and more particularly non-toxic, selective and potent c-kit inhibitors. Preferably, said inhibitor is unable to promote death of IL-3 dependent cells cultured in presence of IL-3. Preferred compounds are 2-(3-amino)arylamino-4-aryl-thiazoles or 4-(4-methylpiperazine-l-ylmethyl)-N-[4-methyl-3-(4-pyridine-3-yl)pyrimidine-2­ylamino)phenyl]benzamide(imatinib).

  本发明涉及一种治疗脑缺血的方法，包括向需要此类治疗的人类患者给予能够耗竭肥大细胞或抑制肥大细胞去颗粒化的化合物。此类化合物可以选自酪氨酸激酶抑制剂，尤其是无毒、选择性和有效的c-kit抑制剂。首选的抑制剂不能促进在IL-3存在的情况下培养的依赖于IL-3的细胞死亡。首选化合物是2-(3-氨基)芳基氨基-4-芳基噻唑或4-(4-甲基哌嗪-1-基甲基)-N-[4-甲基-3-(4-吡啶-3-基)嘧啶-2-基氨基)苯基]苯甲酰胺（伊马替尼）。
• Use of tyrosine kinase inhibitors for treating cerebral ischemia
  申请人：Kinet Jean-Pierre

  公开号：US20070191267A1

  公开（公告）日：2007-08-16

  The present invention relates to a method for treating cerebral ischemia, comprising administering a compound capable of depleting mast cells or a compound inhibiting mast cells degranulation to a human in need of such treatment. Such compounds can be chosen from tyrosine kinase inhibitors and more particularly non-toxic, selective and potent c-kit inhibitors. Preferably, said inhibitor is unable to promote death of IL-3 dependent cells cultured in presence of IL-3.

  本发明涉及一种治疗脑缺血的方法，包括向需要此类治疗的人类患者给予能够耗竭肥大细胞或抑制肥大细胞脱颗粒的化合物。这些化合物可以选择酪氨酸激酶抑制剂，特别是无毒、选择性和有效的c-kit抑制剂。优选地，所述抑制剂不能促进在IL-3存在的情况下培养的IL-3依赖性细胞的死亡。