二盐酸奎扎替尼 | 1132827-21-4

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 唑类
• 中文名称: 二盐酸奎扎替尼
• 英文名称: Quizartinib Dihydrochloride
• 英文别名: 1-(5-tert-butyl-1,2-oxazol-3-yl)-3-[4-[6-(2-morpholin-4-ylethoxy)imidazo[2,1-b][1,3]benzothiazol-2-yl]phenyl]urea;dihydrochloride
• CAS: 1132827-21-4
• 化学式: C29H34Cl2N6O4S
• 分子量: 633.6
• InChiKey: DHYPGRVMIOATAE-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  6.7
• 重原子数：
  42
• 可旋转键数：
  8
• 环数：
  6.0
• sp3杂化的碳原子比例：
  0.34
• 拓扑面积：
  134
• 氢给体数：
  4
• 氢受体数：
  8

文献信息

• [EN] SYNTHESIS, PHARMACOLOGY AND USE OF NEW AND SELECTIVE FMS-LIKE TYROSINE KINASE 3 (FLT3) FLT3 INHIBITORS<br/>[FR] SYNTHÈSE, PHARMACOLOGIE ET UTILISATION DE NOUVEAUX INHIBITEURS SÉLECTIFS DE LA TYROSINE KINASE 3 DE TYPE FMS FLT3 (FLT3)
  申请人：UNIV REGENSBURG

  公开号：WO2019034538A1

  公开（公告）日：2019-02-21

  The present invention relates to small molecule compounds of formula (I) and their use as FLT3 inhibitors for the treatment of various diseases, such as acute myeloid leukemia (AML). The present invention further relates to methods of synthesizing the compounds and methods of treatment.

  本发明涉及式(I)的小分子化合物及其作为FLT3抑制剂用于治疗各种疾病，如急性髓系白血病（AML）。本发明还涉及合成这些化合物的方法和治疗方法。
• PROCESS FOR THE PREPARATION OF IMIDAZO[2,1-B][1,3]BENZOTHIAZOLE DERIVATIVES
  申请人：Gross Timothy David

  公开号：US20130005966A1

  公开（公告）日：2013-01-03

  Provided herein are process for the preparation of N-(5-ferf-butyl-isoxazol-3-yl)-N′-4-[7-(2-morpholin-4-yl-ethoxy)imidazo[2,1-fe][1,3]benzothiazol-2-yl]phenyl}urea, or a pharmaceutically acceptable salt, solvate, hydrate, or polymorph thereof. N-(5-tert-Butyl-isoxazol-3-yl)-N′-4-[7-(2-morpholin-4-yl-ethoxy)imidazo[2,1-&][1,3]benzo-thiazol-2-yl]phenyl}urea is useful for treating, preventing, and/or managing diseases or conditions, including but not limited to, proliferative diseases, FLT-3 mediated diseases, and cancers. N-(5-ferf-Butyl-isoxazol-3-yl)-N′-4-[7-(2-morpholin-4-yl-ethoxy)imidazo[2,1-&][1,3]benzothiazol-2-yl]phenyl}urea is represented by the structure:

  本文提供了制备N-(5-叔丁基异噁唑-3-基)-N'-4-[7-(2-吗啡啉-4-基-乙氧基)咪唑[2,1-fe][1,3]苯并噻唑-2-基]苯基}脲或其药学上可接受的盐、溶剂化合物、水合物或多晶形式的工艺。N-(5-叔丁基异噁唑-3-基)-N'-4-[7-(2-吗啡啉-4-基-乙氧基)咪唑[2,1-&][1,3]苯并噻唑-2-基]苯基}脲可用于治疗、预防和/或管理疾病或情况，包括但不限于增生性疾病、FLT-3介导的疾病和癌症。N-(5-ferf-叔丁基异噁唑-3-基)-N'-4-[7-(2-吗啡啉-4-基-乙氧基)咪唑[2,1-&][1,3]苯并噻唑-2-基]苯基}脲的结构式为：
• COMBINATION METHOD FOR TREATING CANCER
  申请人：Daiichi Sankyo Company, Limited

  公开号：EP3260119A1

  公开（公告）日：2017-12-27

  It is intended to provide a medicament and a method for treating cancer comprising a compound having MDM2 inhibiting activity and a compound having FLT3 inhibiting activity in combination. The present invention provides a medicament comprising (3'R,4'S,5'R)-N-[(3R,6S)-6-carbamoyltetrahydro-2H-pyran-3-yl]-6"-chloro-4'-(2-chloro-3-fluoropyridin-4-yl)-4,4-dimethyl-2"-oxo-1",2"-dihydrodispiro[cyclohexane-1,2'-pyrrolidine-3',3"-indole]-5'-carboxamide or a pharmaceutically acceptable salt thereof and N-(5-tert-butyl-isoxazol-3-yl)-N'-4-[7-(2-morpholin-4-yl-ethoxy)imidazo[2,1-b][1,3]benzothiazol-2-yl]phenyl}urea or a pharmaceutically acceptable salt thereof in combination, and a treatment method using these compounds or salts in combination.

  本发明旨在提供一种治疗癌症的药物和方法，其中包括一种具有 MDM2 抑制活性的化合物和一种具有 FLT3 抑制活性的化合物。本发明提供了一种药物，其包含(3'R,4'S,5'R)-N-[(3R,6S)-6-氨基甲酰四氢-2H-吡喃-3-基]-6"-氯-4'-(2-氯-3-氟吡啶-4-基)-4,4-二甲基-2"-氧代-1",2"-二氢二螺[环己烷-1,2'-吡咯烷-3'、3"-吲哚]-5'-甲酰胺或其药学上可接受的盐和 N-(5-叔丁基-异恶唑-3-基)-N'-4-[7-(2-吗啉-4-基-乙氧基)咪唑并[2,1-b][1,3]苯并噻唑-2-基]苯基}脲或其药学上可接受的盐组合，以及使用这些化合物或盐组合的治疗方法。
• UREA COMPOUND, PREPARATION METHOD THEREFOR AND MEDICAL USE THEREOF
  申请人：Ancureall Pharmaceutical (Shanghai) Co., Ltd.

  公开号：EP3424924A1

  公开（公告）日：2019-01-09

  Provided are a urea compound represented by general formula (I), a pharmaceutically acceptable salt thereof, a preparation method therefor, and use thereof as an FLT3 tyrosine protein kinase inhibitor, particularly in the prevention and/or treating of cancer.

  本发明提供了通式（I）代表的脲化合物、其药学上可接受的盐、其制备方法，以及其作为FLT3酪氨酸蛋白激酶抑制剂的用途，特别是在预防和/或治疗癌症中的用途。
• FLT3 receptor antagonists for the treatment or the prevention of pain disorders
  申请人：Valmier Jean

  公开号：US10106798B2

  公开（公告）日：2018-10-23

  The present invention relates to FLT3 receptor antagonists or inhibitors of FLT3 receptor gene expression for the treatment or the prevention of pain disorders.

  本发明涉及用于治疗或预防疼痛疾病的 FLT3 受体拮抗剂或 FLT3 受体基因表达抑制剂。