Exelixis Patent Company LLC

Pfizer Corporation

Sarah Hudson

Raju Mohan

Michael M Morrissey

Venkataiah Bollu

Brenton Todd Flatt

Benjamin Pratt

Jackaline Dalgard Julien

Brant Clayton Boren

Nadia Haq

Richard Martin

Chakrapani Subramanyam

Tie-Lin Wang

Lawrence Nathan Tumey

Xiao-Hui Gu

Beth C Vetelino

Carolyn Leverett

Sai Chetan K Sukuru

Venkata Ramana Doppalapudi

Abhijit S Bhat

Longfei Xie

The present invention is directed to novel cytotoxic tubulysin analogs and derivatives, to antibody drug conjugates thereof, and to methods for using the same to treat medical conditions including cancer.

Tubulysin analogs and methods for their preparation

TGR5 agonists of structural formula VIII(Q), wherein X, R, R, and Rare defined in the specification, pharmaceutically acceptable salts thereof, compositions thereof, and use of the compounds and compositions for treating diseases. The invention also comprises use of the compounds in and for the manufacture of medicaments, particularly for treating diseases. 

TGR5 agonists

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.

Triazole and imidazole derivatives for use as TGR5 agonists in the treatment of diabetes and obesity

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San Diego, CA, United States of America

Sarah Hudson