Exelixis Patent Company LLC

Vertex Pharmaceuticals, Inc.

Exelixis, Inc.

Bristol-myers Squibb Compnay

Lycia Therapeutics, Inc.

Brett Bradley Busch

Raju Mohan

Richard Martin

William C Stevens, Jr

Tie-Lin Wang

Brenton Todd Flatt

Xiao-Hui Gu

Mark Thomas Miller

Jinglan Zhou

Sara Sabina Hadida Ruah

Andreas Peter Termin

Jason McCartney

Corey Don Anderson

Peter Grootenhuis

Thomas Cleveland

Haripada Khatuya

Bryan A Frieman

Johnny Uy

Prasuna Paraselli

Michael Charles Nyman

Alexander Russell Abela

Edwin J Schweiger

Yinong Xie

Shao Po Lu

Fredrick Van Goor

Robert Michael Hughes

Ali Keshavarz-Shokri

Beili Zhang

Pramod Virupax Joshi

Paul Krenitsky

Timothy Richard Coon

Jeremy J Clemens

Fabrice Pierre

Ellen K Kick

Weichao George Chen

Fabrice Jean Denis Pierre

Vito Melillo

Sara E Swift

Minson Baek

Anton V Gulevich

Ping Kang

Clara Kuang-Ju Hsia

Timothy Alcacio

Senait G Ghirmai

Jason H Wu

Carl V Vogel

Rachel McAuley-Aoki

Wei Xu

Jason Gustaf Lewis

Eric Douglas Turtle

Venkataiah Bollu

David Andrew Siesel

Justin T Ernst

Nicholas Ronald Wurtz

Garrick Kenneth Packard

Vasu Jammalamadaka

Brant Clayton Boren

Meriah Neissel Valente

Mandar Shrikrishna Bodas

Claudia Averbuj

Prasanna Savanor Maddu Rao

Shao-Po Lu

Haiying Zhang

Tie Lin Wang

Xiao Hui Gu

Alla Venu

Jeevanprakash Shetty

William C Stevens

Jason Mccartney

Paul John Krenitsky

Rachel Mcauley-Aoki

The present disclosure provides a class of compounds including a ligand moiety that specifically binds to a cell surface asialoglycoprotein receptor (ASGPR). The cell surface ASGPR binding compounds can trigger the receptor to internalize into the cell a bound compound. The ligand moieties of this disclosure can be linked to a variety of moieties of interest without impacting the specific binding to, and function of, the cell surface receptor ASGPR. Also provided are compounds that are conjugates of the ligand moieties linked to a biomolecule, such as an antibody, which conjugates can harness cellular pathways to remove specific proteins of interest from the cell surface or from the extracellular milieu. Also provided herein methods of using the conjugates to target a polypeptide of interest for sequestration and/or lysosomal degradation.

ASGPR cell surface receptor binding compounds and conjugates

Compounds of Formula (I): pharmaceutically acceptable salts thereof, deuterated derivatives of any of the foregoing, and metabolites of any of the foregoing are disclosed. Pharmaceutical compositions comprising the same, methods of treating cystic fibrosis using the same, and methods for making the same are also disclosed.

Modulators of Cystic Fibrosis Transmembrane Conductance regulator, pharmaceutical compositions, methods of treatment, and process for making the modulators

Compounds of Formula I: pharmaceutically acceptable salts thereof, deuterated derivatives of any of the foregoing, and metabolites of any of the foregoing are disclosed. Pharmaceutical compositions comprising the same, methods of treating cystic fibrosis using the same, and methods for making the same are also disclosed.

Modulator of cystic fibrosis transmembrane conductance regulator, pharmaceutical compositions, methods of treatment, and process for making the modulator

Modulators of cystic fibrosis transmembrane conductance regulator, pharmaceutical compositions, methods of treatment, and process for making the modulators

The present invention provides compounds of Formula I and Formula II: or pharmaceutically acceptable salts or solvates thereof, as modulators of liver X receptors (LXRs), and compositions comprising any of such novel compounds and methods of use thereof. These compounds are useful as medicaments for treatment and/or prophylaxis for diseases or conditions related to activity of LXRs. 

LXR modulators

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

Compounds of the invention, such as compounds of Formulae Ia, Ib, Ic, or Id and pharmaceutically acceptable salts, isomers, and prodrugs thereof, which are useful as modulators of the activity of liver X receptors, where R1, R2, R21, R3, and G are defined herein. Pharmaceutical compositions containing the compounds and methods of using the compounds are also disclosed. 

Modulators of LXR

Compounds, pharmaceutically acceptable salts, isomers, or prodrugs thereof, of the invention are disclosed, which are useful as modulators of the activity of liver X receptors (LXR). Pharmaceutical compositions containing the compounds and methods of using the compounds are also disclosed.

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 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

Compounds of the following general structure for use in compositions and methods for modulating the activity of nuclear receptors are provided: The compounds are useable in compositions and methods for modulating the estrogen related receptors and are agonists, partial agonists, antagonists. or inverse agonists of ERR or ERR&#x3b1;.

Benzylthiazolone inhibitors of estrogen-related receptors (ERR)

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San Diego, CA, United States of America

Brett Bradley Busch