(7S)-4'-fluoro-7'-(2-fluoropyridin-3-yl)-2'-methoxy-3,4-dihydro-2H-spiro[imidazo[1,5-a]pyrimidine-8,9'-xanthen]-6-amine | 1393483-80-1

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 苯并吡喃
• 英文名称: (7S)-4'-fluoro-7'-(2-fluoropyridin-3-yl)-2'-methoxy-3,4-dihydro-2H-spiro[imidazo[1,5-a]pyrimidine-8,9'-xanthen]-6-amine
• 英文别名: (8S)-4'-fluoro-7'-(2-fluoropyridin-3-yl)-2'-methoxyspiro[3,4-dihydro-2H-imidazo[1,5-a]pyrimidine-8,9'-xanthene]-6-amine
• CAS: 1393483-80-1
• 化学式: C₂₄H₁₉F₂N₅O₂
• 分子量: 447.444
• InChiKey: NRCWGDBHISLYPV-DEOSSOPVSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  2.7
• 重原子数：
  33
• 可旋转键数：
  2
• 环数：
  6.0
• sp3杂化的碳原子比例：
  0.21
• 拓扑面积：
  85.3
• 氢给体数：
  1
• 氢受体数：
  7

文献信息

• [EN] SPIRO-AMINO-IMIDAZO-FUSED HETEROCYCLIC COMPOUNDS AS BETA-SECRETASE MODULATORS AND METHODS OF USE<br/>[FR] COMPOSÉS HÉTÉROCYCLIQUES SPIRO-AMINO-IMIDAZO-CONDENSÉS EN TANT QUE MODULATEURS DE LA BÊTA-SECRÉTASE ET MÉTHODES D'UTILISATION
  申请人：AMGEN INC

  公开号：WO2012112462A1

  公开（公告）日：2012-08-23

  The present invention provides a new class of compounds useful for the modulation of beta-secretase enzyme (BACE) activity. The compounds have a general Formula I, wherein variables A1, A3, A4, A5, A6, A8, R2, R7, X, Y and Z of Formula I are defined herein. The invention also provides pharmaceutical compositions comprising the compounds, and corresponding uses of the compounds and compositions for treatment of disorders and/or conditions related to plaque formation and deposition, resulting from the activity of BACE. Such BACE mediated disorders include, for example, Alzheimer's Disease, cognitive deficits and impairments, schizophrenia and other central nervous system conditions and disorders. The invention further provides compounds of Formulas II and III, and of sub-formulas of Formulas I, II and III, intermediates and processes and methods useful for the preparation of compounds of Formulas I-III.

  本发明提供了一类新的化合物，用于调节β-分泌酶（BACE）活性。这些化合物具有一般的化学式I，其中化学式I中的变量A1、A3、A4、A5、A6、A8、R2、R7、X、Y和Z在此处被定义。本发明还提供了包括这些化合物的药物组合物，以及这些化合物和组合物用于治疗与斑块形成和沉积相关的疾病和/或症状的对应用途，这些疾病和症状是由BACE的活性引起的。这种由BACE介导的疾病包括阿尔茨海默病、认知缺陷和损伤、精神分裂症和其他中枢神经系统疾病。本发明还提供了化学式II和III的化合物，以及化学式I、II和III的亚式化合物、中间体和有用于制备化学式I-III的化合物的过程和方法。
• Spiro-Amino-Imidazo-Fused Heterocyclic Compounds as Beta-secretase Modulators and Methods of Use
  申请人：Epstein Oleg

  公开号：US20140038954A1

  公开（公告）日：2014-02-06

  The present invention provides a new class of compounds useful for the modulation of beta-secretase enzyme (BACE) activity. The compounds have a general Formula I, wherein variables A 1 , A 3 , A 4 , A 5 , A 6 , A 8 , R 2 , R 7 , X, Y and Z of Formula I are defined herein. The invention also provides pharmaceutical compositions comprising the compounds, and corresponding uses of the compounds and compositions for treatment of disorders and/or conditions related to plaque formation and deposition, resulting from the activity of BACE. Such BACE mediated disorders include, for example, Alzheimer's Disease, cognitive deficits and impairments, schizophrenia and other central nervous system conditions and disorders. The invention further provides compounds of Formulas II and III, and of sub-formulas of Formulas I, II and III, intermediates and processes and methods useful for the preparation of compounds of Formulas I-III.

  本发明提供了一类新的化合物，用于调节β-分泌酶（BACE）酶活性。该化合物具有一般式I，其中式I中的变量A1、A3、A4、A5、A6、A8、R2、R7、X、Y和Z在此定义。本发明还提供了包含该化合物的制药组合物，并提供了该化合物和组合物用于治疗与斑块形成和沉积相关的疾病和/或状况的相应用途。这些BACE介导的疾病包括阿尔茨海默病、认知缺陷和障碍、精神分裂症和其他中枢神经系统疾病和障碍等。本发明还提供了II和III式化合物，以及I、II和III式亚式化合物的中间体、制备化合物I-III的方法和过程。
• US8962859B2
  申请人：——

  公开号：US8962859B2

  公开（公告）日：2015-02-24