Invention Grant
- Patent Title: Tetrahydropyranochromene gamma secretase inhibitors
- Patent Title (中): 四氢吡喃色烯γ分泌酶抑制剂
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Application No.: US12665580Application Date: 2008-07-01
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Publication No.: US08664411B2Publication Date: 2014-03-04
- Inventor: 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
- Applicant: 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
- Applicant Address: US NJ Rahway
- Assignee: Merck Sharp & Dohme Corp.
- Current Assignee: Merck Sharp & Dohme Corp.
- Current Assignee Address: US NJ Rahway
- Agent Susan Hess; John C. Todaro; Henry Jeanette
- International Application: PCT/US2008/008192 WO 20080701
- International Announcement: WO2009/008980 WO 20090115
- Main IPC: C07D311/80
- IPC: C07D311/80 ; C07D493/04 ; A61K31/352

Abstract:
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.
Public/Granted literature
- US20110236400A1 TETRAHYDROPYRANOCHROMENE GAMMA SECRETASE INHIBITORS Public/Granted day:2011-09-29
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