Janssen Pharmaceutica Nv

Cellzome Limited

Umar S M Maharoof

Chih Yung Ho

Yan Zhang

Jeremy Major

John Harrison

Dana L Johnson

Alison Jones

Robert W Tuman

Svenja Burckhardt

Jay Mei

Robert A Galemmo

The present invention relates to compounds of Formula I as shown below, wherein the definitions of Het, R, RR, R, R, R, R, R, R, and Rare provided in the specification. Compounds of Formula I are useful for the treatment of diseases associated with &#x3b3;-secretase activity, including Alzheimer's disease. 

Piperidinyl and piperazinyl modulators of &#x3b3;-secretase

The present invention relates to compounds of Formula I as shown below, wherein the definitions of A, X, Y, RR, R, R, R, R, R, R, and Rare provided in the specification. Compounds of Formula I are useful for the treatment of diseases associated with &#x3b3;-secretase activity, including Alzheimer's disease. 

Amine linked modulators of &#x3b3;-secretase

The invention is directed to compounds having the following structures: N-(3-ethoxyphenyl)-1,4-dihydro-6-ethoxy-7-(3-hydroxypropoxy)-1-methylindeno[1,2-c]pyrazole-3-amine; 3-[3-(3-Bromo-phenylamino)-6-ethoxy-1-methyl-1,4-dihydro-indeno[1,2-c]pyrazol-7-yloxy]-propan-1-ol;or 3-[3-(2-Chloro-pyridin-4-ylamino)-6-ethoxy-1-methyl-1,4-dihydro-indeno[1,2-c]pyrazol-7-yloxy]-propan-1-ol, and N-oxides, pharmaceutically acceptable salts, solvates, tautomers and stereochemical isomers thereof and the uses of such compounds as inhibitors of tubulin polymerization and for the treatment of solid tumors. The present invention is further directed to pharmaceutical compositions comprising the compounds of the present invention and to methods for treating conditions such as cancers and other cell proliferative disorders.

N-substituted tricyclic 3-aminopyrazoles as anti-mitotic tubulin polymerization inhibitors

Growing community of inventors

North Wales, PA, United States of America

Umar S M Maharoof