Yan Jin

US Patent:

20110236400, Sep 29, 2011

Filed:

Jul 1, 2008

Appl. No.:

12/665580

Inventors:

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
Jesse K. Wong - Monroe Township NJ, US
Ruo Xu - Watchung NJ, US
Zhiqiang Zhao - Scotch Plains NJ, US
Paul E. McNamara - Scotch Plains NJ, US

International Classification:

A61K 39/395
C07D 493/04
C07D 311/80
C07D 407/12
A61K 31/35
A61K 31/352
A61K 31/381
A61P 25/28
A61P 29/00
A61P 31/00
C07C 201/12
C07C 67/343

US Classification:

4241721, 549387, 549390, 549 60, 514455, 514444, 560 20, 560 81

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.