发明授权
- 专利标题： Tetrahydropyranochromene gamma secretase inhibitors
- 专利标题（中）： 四氢吡喃色烯γ分泌酶抑制剂
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申请号： US12665580申请日： 2008-07-01
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公开(公告)号： US08664411B2公开(公告)日： 2014-03-04
- 发明人: Wen-Lian Wu , Thomas A. Bara , Duane A. Burnett , John W. Clader , Martin S. Domalski , Yan Jin , Hubert B. Josien , Hongmei Li , Xian Liang , Dmitri A. Pissarnitski , Thavalakulamgara K. Sasikumar , Jesse K. Wong , Ruo Xu , Zhiqiang Zhao , Paul McNamara
- 申请人： Wen-Lian Wu , Thomas A. Bara , Duane A. Burnett , John W. Clader , Martin S. Domalski , Yan Jin , Hubert B. Josien , Hongmei Li , Xian Liang , Dmitri A. Pissarnitski , Thavalakulamgara K. Sasikumar , Jesse K. Wong , Ruo Xu , Zhiqiang Zhao , Paul McNamara
- 申请人地址： US NJ Rahway
- 专利权人： Merck Sharp & Dohme Corp.
- 当前专利权人： Merck Sharp & Dohme Corp.
- 当前专利权人地址： US NJ Rahway
- 代理商 Susan Hess; John C. Todaro; Henry Jeanette
- 国际申请： PCT/US2008/008192 WO 20080701
- 国际公布： WO2009/008980 WO 20090115
- 主分类号： C07D311/80
- IPC分类号： C07D311/80 ; C07D493/04 ; A61K31/352
摘要：
Disclosed are novel gamma secretase inhibitors of the formula. Also disclosed are methods of inhibiting gamma-secretase, methods of treating neurodegenerative diseases, and methods of treating Alzheimer's Disease. Also disclosed are processes for preparing alkenes in one reaction step using a mixture of an aldehyde (or ketone) and an alkyl substituted with two electron withdrawing groups, and reacting the mixture with: (a) a sulfonyl halide (e.g., a sulfonyl chloride) and a basic tertiary amine, or, (b) a sulfonyl anhydride and a basic amine, or (c) an aryl-C(O)-halide and a basic tertiary amine, or (d) an aryl-C(O)—O—C(O)-aryl and a basic tertiary amine, or (e) an heteroaryl-C(O)-halide and a basic tertiary amine, or (f) a heteroaryl-C(O)—O—C(O)-heteroaryl and a basic tertiary amine.
公开/授权文献
- US20110236400A1 TETRAHYDROPYRANOCHROMENE GAMMA SECRETASE INHIBITORS 公开/授权日：2011-09-29
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