5-(3-chlorophenyl)-α-(4-chlorophenyl)-4,5-dihydro-α-(1-methyl-1H-imidazol-5-yl)tetrazolo[1,5-a]quinazoline-7-methanol

• 分子结构分类: 有机化合物 - 苯丙烷和聚酮 - 二芳基庚烷
• 英文名称: 5-(3-chlorophenyl)-α-(4-chlorophenyl)-4,5-dihydro-α-(1-methyl-1H-imidazol-5-yl)tetrazolo[1,5-a]quinazoline-7-methanol
• 英文别名: (4-Chlorophenyl)-[5-(3-chlorophenyl)-4,5-dihydrotetrazolo[1,5-a]quinazolin-7-yl]-(3-methylimidazol-4-yl)methanol；(4-chlorophenyl)-[5-(3-chlorophenyl)-4,5-dihydrotetrazolo[1,5-a]quinazolin-7-yl]-(3-methylimidazol-4-yl)methanol
• 化学式: C₂₅H₁₉Cl₂N₇O
• 分子量: 504.378
• InChiKey: JUMDFLZNHJCMKW-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  5.2
• 重原子数：
  35
• 可旋转键数：
  4
• 环数：
  6.0
• sp3杂化的碳原子比例：
  0.12
• 拓扑面积：
  90.4
• 氢给体数：
  2
• 氢受体数：
  5

反应信息

• 作为反应物：
  描述：

  5-(3-chlorophenyl)-α-(4-chlorophenyl)-4,5-dihydro-α-(1-methyl-1H-imidazol-5-yl)tetrazolo[1,5-a]quinazoline-7-methanol 以 甲苯 为溶剂， 反应 6.0h， 以27%的产率得到9-(3-chlorophenyl)-α-(4-chlorophenyl)-4,9-dihydro-α-(1-methyl-1H-imidazol-5-yl)-tetrazolo[5,1-b]quinazoline-7-methanol
  参考文献：
  名称：

  [EN] FARNESYL TRANSFERASE INHIBITING TRICYCLIC QUINAZOLINE DERIVATIVES SUBSTITUTED WITH CARBON-LINKED IMIDAZOLES OR TRIAZOLES
  [FR] DERIVES DE QUINAZOLINE TRICYLIQUE INHIBANT LA FARNESYL TRANSFERASE SUBSTITUES AVEC DES IMIDAZOLES OU DES TRIAZOLES A LIAISON CARBONE

  摘要：

  本发明涉及具有法尼醇转移酶抑制活性的新型化合物，其化学结构式为(I)，其中r、s、t、R1、R2、R3、R4、R5和R6具有定义的含义；其制备方法、含有它们的组合物以及它们作为药物的用途。

  公开号：

  WO2003087101A1

文献信息

• SYNERGISTIC MODULATION OF FLT3 KINASE USING A FLT3 INHIBITOR AND A FARNESYL TRANSFERASE INHIBITOR
  申请人：Baumann Andrew Christian

  公开号：US20060281788A1

  公开（公告）日：2006-12-14

  The invention is directed to a method of inhibiting FLT3 tyrosine kinase activity or expression or reducing FLT3 kinase activity or expression in a cell or a subject comprising the administration of a farnesyl transferase inhibitor and a FLT3 kinase inhibitor selected from compounds of Formula I′: Included within the present invention is both prophylactic and therapeutic methods for treating a subject at risk of (or susceptible to) developing a cell proliferative disorder or a disorder related to FLT3.

  本发明涉及一种抑制FLT3酪氨酸激酶活性或表达或减少细胞或受试者中FLT3激酶活性或表达的方法，包括管理法尼基转移酶抑制剂和从公式I'的化合物中选择的FLT3激酶抑制剂。 本发明包括用于治疗处于发展细胞增殖障碍或与FLT3相关障碍风险（或易感性）的受试者的预防和治疗方法。
• SYNERGISTIC MODULATION OF FLT3 KINASE USING AMINOPYRIMIDINES KINASE MODULATORS
  申请人：Baumann Andrew Christian

  公开号：US20060281755A1

  公开（公告）日：2006-12-14

  The invention is directed to a method of inhibiting FLT3 tyrosine kinase activity or expression or reducing FLT3 kinase activity or expression in a cell or a subject comprising the administration of a farnesyl transferase inhibitor and a FLT3 kinase inhibitor selected from aminopyrimidine compounds of Formula I′: where R 3 , B, Z, r and R 1 are as defined herein. Included within the present invention is both prophylactic and therapeutic methods for treating a subject at risk of (or susceptible to) developing a cell proliferative disorder or a disorder related to FLT3.

  这项发明涉及一种抑制FLT3酪氨酸激酶活性或表达或减少细胞或受试者中FLT3激酶活性或表达的方法，包括给予一种法尼基转移酶抑制剂和一种从式I′的氨基嘧啶化合物中选择的FLT3激酶抑制剂：其中R3、B、Z、r和R1如本文所定义。本发明涵盖了用于治疗处于发展细胞增殖障碍或与FLT3有关的障碍风险（或易感）的受试者的预防和治疗方法。
• SYNERGISTIC MODULATION OF FLT3 KINASE USING AMINOQUINOLINE AND AMINOQUINAZOLINE KINASE MODULATORS
  申请人：Baumann Andrew Christian

  公开号：US20060281771A1

  公开（公告）日：2006-12-14

  The invention is directed to a method of inhibiting FLT3 tyrosine kinase activity or expression or reducing FLT3 kinase activity or expression in a cell or a subject comprising the administration of a farnesyl transferase inhibitor and a FLT3 kinase inhibitor selected from aminoquinoline and aminoquinazoline compounds of Formula I′: where R 1 , R 2 , R 3 , B, Z, Q, p, q and X are as defined herein. Included within the present invention is both prophylactic and therapeutic methods for treating a subject at risk of (or susceptible to) developing a cell proliferative disorder or a disorder related to FLT3.

  该发明涉及一种抑制细胞或受试者中FLT3酪氨酸激酶活性或表达，或减少FLT3激酶活性或表达的方法，包括给予一种法尼基转移酶抑制剂和一种从式I′的氨基喹啉和氨基喹唑化合物中选择的FLT3激酶抑制剂的组合，其中R1、R2、R3、B、Z、Q、p、q和X如本处所定义。本发明涵盖了预防和治疗方法，用于治疗患有细胞增殖紊乱或与FLT3相关的疾病风险（或易感）的受试者。
• SYNERGISTIC MODULATION OF FLT3 KINASE USING THIENOPYRIMIDINE AND THIENOPYRIDINE KINASE MODULATORS
  申请人：Baumann Andrew Christian

  公开号：US20060281769A1

  公开（公告）日：2006-12-14

  The invention is directed to a method of inhibiting FLT3 tyrosine kinase activity or expression or reducing FLT3 kinase activity or expression in a cell or a subject comprising the administration of a farnesyl transferase inhibitor and a FLT3 kinase inhibitor selected from thienopyrimidine and thienopyridine compounds Formula I′ and Formula II′: where R 1 , R 3 , B, Z, Q, p, q and X are as defined herein. Included within the present invention is both prophylactic and therapeutic methods for treating a subject at risk of (or susceptible to) developing a cell proliferative disorder or a disorder related to FLT3.

  该发明涉及一种抑制细胞或受试者中FLT3酪氨酸激酶活性或表达的方法，或减少FLT3激酶活性或表达的方法，包括给予一种法尼基转移酶抑制剂和一种从噻吩吡啶和噻吩吡啶化合物Formula I'和Formula II'中选择的FLT3激酶抑制剂：其中R1、R3、B、Z、Q、p、q和X的定义如本文所述。本发明涵盖了治疗患有细胞增殖紊乱或与FLT3相关的疾病风险（或易感）的受试者的预防和治疗方法。
• Dosing regimen
  申请人：——

  公开号：US20030060450A1

  公开（公告）日：2003-03-27

  This invention relates to a method of treatment and dosing regimen for treating mammalian tumors by the discontinuous administration of a farnesyl transferase inhibitor over an abbreviated one to five day dosing schedule.

  本发明涉及一种治疗哺乳动物肿瘤的方法和剂量方案，通过在缩短的1至5天剂量计划中间断地给予法尼酰转移酶抑制剂进行治疗。