Exelixis, Inc.

Exelixis Patent Company LLC

The Mclean Hospital Corporation

University of Rochester

X-ceptor Therapeutics, Inc.

Richard Martin

Raju Mohan

Jason H. Wu

Tie-lin Wang

Brett Busch

Brenton T. Flatt

Xiao-hui Gu

Xiao-Hui Gu

Tie-Lin Wang

Brenton Todd Flatt

Brett Bradley Busch

Michael Charles Nyman

Jason H Wu

Edwin J Schweiger

William C Stevens, Jr

Yinong Xie

Yong Wang

Timothy Patrick Forsyth

Lynne Canne Bannen

John L Neumeyer

Larry Wayne Mann

Morrison B Mac

Jeff Z Chen

Grace Mann

Brant Clayton Boren

Ronald Griffith

Lisa Esther Dalrymple

Jean M Bidlack

Shao Po Lu

Brett Murphy

William C Stevens

Wei Xu

Michael M Morrissey

Venkataiah Bollu

Vasu Jammalamadaka

Benjamin Pratt

Jackaline Dalgard Julien

Nadia Haq

Shao-Po Lu

Sarah Hudson

Jeff Chen

William Stevens

Brenton T Flatt

Methods of using compounds of the invention, such as compounds of Formulae IIa, IIb, IIc, or IId and pharmaceutically acceptable salts thereof are disclosed. The compounds are useful in treating, preventing, inhibiting or ameliorating the symptoms of a disease or disorder that is modulated or otherwise affected by nuclear receptor activity, or in which nuclear receptor activity is implicated.

Imidazole based LXR modulators

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

Compounds of the invention, such as compounds of Formulae IIa, IIb, IIc or IId, and pharmaceutically acceptable salts, isomers, and prodrugs thereof, are useful as modulators of the activity of liver X receptors, where R, R, R, Rand G are defined herein. Pharmaceutical compositions containing the compounds and methods of using the compounds are also disclosed. 

Compounds, compositions and methods for modulating the activity of receptors are provided. In particular, compounds and compositions are provided for modulating the activity of receptors and for the treatment, prevention, or amelioration of one or more symptoms of disease or disorder directly or indirectly related to the activity of the receptors.

Azepinoindole derivatives as pharmaceutical agents

Compounds, compositions and methods are provided for modulating the activity of receptors and for the treatment, prevention, or amelioration of one or more symptoms of disease or disorder related to the activity of the receptors.

Azepine derivatives as pharmaceutical agents

Compounds, compositions and methods for modulating the activity of receptors are provided. In particular compounds and compositions are provided for modulating the activity of receptors and for the treatment, prevention, or amelioration of one or more symptoms of disease or disorder directly or indirectly related to the activity of the receptors.

Pyrrole derivatives as pharmaceutical agents

Azepinoindole and pyridoindole derivatives as pharmaceutical agents

Compounds of the invention are disclosed, such as compounds of formulae LX-LXIV, and pharmaceutically acceptable salts, isomers, or prodrugs thereof, which are useful as modulators of the activity of liver X receptors (LXR) and Farnesoid X receptors (FXR), where R, R, R, R, J, J, G, G, and Q are defined herein. Pharmaceutical compositions containing the compounds and methods of using the compounds are also disclosed. 

LXR and FXR modulators

The invention is based in part on the discovery that nonselective &#x3ba; agonists that possess &#x3bc; receptor-mediated effects in addition to their &#x3ba; agonist effects can decrease cocaine self-administration more effectively and with fewer undesirable side effects than can highly selective &#x3ba; agonists. The invention includes a number of new compounds having both nonselective &#x3ba; opioid receptor agonist activity and additional activity at &#x3bc; opioid receptors. These compounds are useful for the treatment of cocaine abuse, and can also be radiolabeled for use as imaging agents, e.g., the N-fluoroalkyl and iodoalkyl derivatives can be used, respectively, for positron emission tomography (PET) and single photon computed tomography (SPECT) brain imaging.

Treatment of cocaine abuse using N-substituted derivatives of morphinan

N-substituted derivatives of morphinan and uses thereof

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San Diego, CA, United States of America

Xiao-Hui Gu