发明申请
US20090036478A1 Substituted hydroxyethyl amine compounds as beta-secretase modulators and methods of use
有权
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基本信息:
- 专利标题: Substituted hydroxyethyl amine compounds as beta-secretase modulators and methods of use
- 专利标题(中):取代的羟乙基胺化合物作为β-分泌酶调节剂和使用方法
- 申请号:US12154497 申请日:2008-05-23
- 公开(公告)号:US20090036478A1 公开(公告)日:2009-02-05
- 发明人: Wenge Zhong , Stephen Hitchcock , Vinod F. Patel , Michael Croghan , Thomas Dineen , Daniel Horne , Matthew Kaller , Charles Kreiman , Patricia Lopez , Holger Monenschein , Thomas Nguyen , Lewis Pennington , Qiufen Xue , Bryant Yang , Yuan Cheng
- 申请人: Wenge Zhong , Stephen Hitchcock , Vinod F. Patel , Michael Croghan , Thomas Dineen , Daniel Horne , Matthew Kaller , Charles Kreiman , Patricia Lopez , Holger Monenschein , Thomas Nguyen , Lewis Pennington , Qiufen Xue , Bryant Yang , Yuan Cheng
- 申请人地址: US CA Thousand Oaks
- 专利权人: AMGEN INC.
- 当前专利权人: AMGEN INC.
- 当前专利权人地址: US CA Thousand Oaks
- 主分类号: A61K31/438
- IPC分类号: A61K31/438 ; C07D221/20 ; C07D233/54 ; A61K31/4178 ; A61P25/28 ; A61P25/00
摘要:
The present invention comprises a new class of compounds useful for the modulation of Beta-secretase enzyme activity and for the treatment of Beta-secretase mediated diseases, including Alzheimer's disease (AD) and related conditions. In one embodiment, the compounds have a general Formula I wherein R1a, R1b, R1c, B, W, R3, R4 and R5 are defined herein. In another embodiment, the invention provides compounds of general Formula II wherein A1, A2, A3, A4, R1a, R1b, R1c, R2, R4, R5, W, X and Z are defined herein.The invention also includes use of these compounds in pharmaceutical compositions for treatment, prophylactic or therapeutic, of disorders and conditions related to the activity of beta-secretase protein. Such disorders include, for example, Alzheimer's Disease (AD), cognitive deficits and impairment, schizophrenia and other similar central nervous system conditions. The invention also comprises further embodiments of Formula II, intermediates and processes useful for the preparation of compounds of Formulas I and II.
摘要(中):
本发明包括可用于调节β-分泌酶酶活性和用于治疗β-分泌酶介导的疾病(包括阿尔茨海默病(AD))和相关病症的新一类化合物。 在一个实施方案中,化合物具有通式I,其中R 1a,R 1b,R 1c,B,W,R 3,R 4和R 5在本文中定义。 在另一个实施方案中,本发明提供通式II的化合物,其中A1,A2,A3,A4,R1a,R1b,R1c,R2,R4,R5,W,X和Z如本文所定义。 本发明还包括在药物组合物中用于治疗,预防或治疗与β-分泌酶蛋白活性相关的病症和病症的用途。 这些疾病包括例如阿尔茨海默病(AD),认知缺陷和损伤,精神分裂症和其他类似的中枢神经系统疾病。 本发明还包括式II的其它实施方案,可用于制备式I和II化合物的中间体和方法。
公开/授权文献:
IPC结构图谱:
A | 人类生活必需 |
--A61 | 医学或兽医学;卫生学 |
----A61K | 医用、牙科用或梳妆用的配制品 |
------A61K31/00 | 含有机有效成分的医药配制品 |
--------A61K31/33 | .杂环化合物 |
----------A61K31/335 | ..仅有氧作为环杂原子的,例如制霉色基素 |
------------A61K31/40 | ...有仅以1个氮作为环杂原子的五元环的,例如舒必利、琥珀酰亚胺、托尔米丁、甲氧吡丁苯 |
--------------A61K31/438 | ....与碳环或杂环螺环稠合的环系 |