Inventors:
Venkataiah Bollu - San Diego CA, US
Brant Clayton Boren - San Diego CA, US
Jackaline Dalgard Julien - Del Mar CA, US
Brenton T. Flatt - Poway CA, US
Nadia Haq - Waltham MA, US
Sarah Hudson - San Diego CA, US
Raju Mohan - Encinitas CA, US
Michael Morrissey - Danville CA, US
Benjamin Pratt - Encinitas CA, US
Richard Martin - San Diego CA, US
Xiao-Hui Gu - Potomac MD, US
Assignee:
EXELIXIS PATENT COMPANY LLC - SAN FRANCISCO CA
International Classification:
A61K 31/5377, A61K 31/498, A61K 31/473, A61K 31/423, A61K 31/4196, C07D 233/84, C07D 413/06, C07D 403/06, C07D 403/12, C07D 249/12, A61K 31/4164, C07D 405/14, A61P 3/00, A61P 3/04, A61P 9/10, A61P 3/10, A61P 3/06, C12N 5/02
US Classification:
5142362, 435375, 514249, 514314, 514379, 514381, 514383, 514398, 544132, 544353, 546167, 548241, 548252, 5482642, 5483251
Abstract:
The present invention comprises TGR5 agonists of structural formula I,wherein X, R, R, and Rare defined herein, as well as N-oxides of them and pharmaceutically acceptable salts thereof. The invention further comprises composition comprising the compounds, N-oxides, and/or pharmaceutically acceptable salts thereof. The invention also comprises use of the compounds and compositions for treating diseases in which TGR5 is a mediator or is implicated. The invention also comprises use of the compounds in and for the manufacture of medicaments, particularly for treating diseases in which TGR5 is a mediator or is implicated.