The patent badge is an abbreviated version of the USPTO patent document. The patent badge does contain a link to the full patent document.

The patent badge is an abbreviated version of the USPTO patent document. The patent badge covers the following: Patent number, Date patent was issued, Date patent was filed, Title of the patent, Applicant, Inventor, Assignee, Attorney firm, Primary examiner, Assistant examiner, CPCs, and Abstract. The patent badge does contain a link to the full patent document (in Adobe Acrobat format, aka pdf). To download or print any patent click here.

Date of Patent:
Mar. 04, 2014

Filed:

Jul. 01, 2008
Applicants:

Wen-lian Wu, Edison, NJ (US);

Thomas A. Bara, Scotch Plains, NJ (US);

Duane A. Burnett, Bernardsville, NJ (US);

John W. Clader, Cranford, NJ (US);

Martin S. Domalski, Verona, NJ (US);

Yan Jin, Princeton, NJ (US);

Hubert B. Josien, Jersey City, NJ (US);

Hongmei LI, Warren, NJ (US);

Xian Liang, Monmouth Junction, NJ (US);

Dmitri A. Pissarnitski, Scotch Plains, NJ (US);

Thavalakulamgara K. Sasikumar, Edison, NJ (US);

Jesse K. Wong, Monroe Township, NJ (US);

Ruo Xu, Watchung, NJ (US);

Zhiqiang Zhao, Scotch Plains, NJ (US);

Paul Mcnamara, Scotch Plains, NJ (US);

Inventors:

Wen-Lian Wu, Edison, NJ (US);

Thomas A. Bara, Scotch Plains, NJ (US);

Duane A. Burnett, Bernardsville, NJ (US);

John W. Clader, Cranford, NJ (US);

Martin S. Domalski, Verona, NJ (US);

Yan Jin, Princeton, NJ (US);

Hubert B. Josien, Jersey City, NJ (US);

Hongmei Li, Warren, NJ (US);

Xian Liang, Monmouth Junction, NJ (US);

Dmitri A. Pissarnitski, Scotch Plains, NJ (US);

Thavalakulamgara K. Sasikumar, Edison, NJ (US);

Jesse K. Wong, Monroe Township, NJ (US);

Ruo Xu, Watchung, NJ (US);

Zhiqiang Zhao, Scotch Plains, NJ (US);

Paul McNamara, Scotch Plains, NJ (US);

Assignee:

Merck Sharp & Dohme Corp., Rahway, NJ (US);

Attorneys:
Primary Examiner:
Int. Cl.
CPC ...
C07D 311/80 (2006.01); C07D 493/04 (2006.01); A61K 31/352 (2006.01);
U.S. Cl.
CPC ...
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.


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