6-[(4-chlorophenyl)hydroxy(1-methyl-1H-imidazol-5-yl)methyl]-4-(3-ethoxyphenyl)-1-methyl-2(1H)-quinolinone

• 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: 6-[(4-chlorophenyl)hydroxy(1-methyl-1H-imidazol-5-yl)methyl]-4-(3-ethoxyphenyl)-1-methyl-2(1H)-quinolinone
• 英文别名: 6-[(4-chloro-phenyl)-hydroxy-(3-methyl-3H-imidazol-4-yl)-methyl]-4-(3-ethoxy-phenyl)-1-methyl-1H-quinolin-2-one；6-[(4-Chlorophenyl)-hydroxy-(3-methylimidazol-4-yl)methyl]-4-(3-ethoxyphenyl)-1-methylquinolin-2-one
• 化学式: C₂₉H₂₆ClN₃O₃
• 分子量: 499.997
• InChiKey: QOFQBGVDXIFFKM-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  4.1
• 重原子数：
  36
• 可旋转键数：
  6
• 环数：
  5.0
• sp3杂化的碳原子比例：
  0.17
• 拓扑面积：
  67.6
• 氢给体数：
  1
• 氢受体数：
  4

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。
• QUINOLINONE FARNESYL TRANSFERASE INHIBITORS FOR THE TREATMENT OF SYNUCLEINOPATHIES AND OTHER INDICATIONS
  申请人：Lansbury, JR. Peter T.

  公开号：US20090253655A1

  公开（公告）日：2009-10-08

  Novel quinolinone farnesyl transferase inhibitors are provided. These new compounds are useful in the treatment or prevention of synucleinopathies, such as Parkinson's Disease, Diffuse Lewy Body Disease, multiple system atrophy, and disorders of brain iron concentration including pantothenate kinase-associated neurodegeneration (e.g., PANK1), or other neurodegenerative/neurological diseases. Provided compounds are also useful in the treatment of proliferative diseases such as cancer, and in the treatment of neurological diseases, such as cognitive impairment, depression, and anxiety. The treatment including administering to a subject a therapeutically effective amount of an inventive farnesyl transferase inhibitor compound.

  提供了新型喹诺酮法尼西基转移酶抑制剂。这些新化合物在治疗或预防突触核蛋白病（如帕金森病、弥漫性莱维小体病、多系统萎缩和脑铁浓度紊乱疾病，包括泛酰辅酶A激酶相关的神经退行性疾病（例如PANK1）或其他神经退行性/神经系统疾病方面具有用处。提供的化合物还可用于治疗癌症等增生性疾病，以及治疗认知障碍、抑郁症和焦虑等神经系统疾病。治疗包括向受试者施用一种创新的法尼西基转移酶抑制剂化合物的治疗有效剂量。
• 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。