Receptos, Inc.

Celgene International Ii Sarl

Neurocrine Biosciences, Inc.

Boehringer Ingelheim International Gmbh

The Scripps Research Institute

Junko Tamiya

Liming Huang

Esther Martinborough

Marcus F Boehm

Adam Richard Yeager

Manisha Moorjani

Enugurthi Brahmachary

Thomas Fowler

Premji Meghani

Andrew Richard Novak

Michael Knaggs

Robert Peach

Michael Allen Hanson

Jennifer L Brooks

Fiona Lorraine Scott

Gregg Alan Timony

Brian Dyck

Troy Vickers

Philip Turnbull

Mark T Griffith

Daniel Glynn

Mark Mills

Peter G Schultz

Manoj N Kumar

Jonathan Bryant Grey

Martin W Rowbottom

Arnab Kumar Chatterjee

Chen Chen

Warren Stanfield Wade

Timothy Richard Coon

Hank Michael James Petrassi

Neil Ashweek

Dongpei Wu

Lin Zhang

Joseph Pontillo

Anil Gupta

Nicole Harriott

Luke L Lairson

Joe Anh Tran

William Vernier

Val S Goodfellow

Marcos Steinberg

Manoj Kumar

Junhua Fan

Florence Jovic

Emily Chin

Chenguang Yu

Ramkumar Modukuri

Yang Tran

Ana Maria Gamo Albero

Matthew Richard Crittall

Brahmachary Enugurthi

Greg P Iacobini

Kevan Grant

Maria Ieva

Raffaele Pasceri

Hanae Benelkebir

Tom Fowler

Mingzhu Zhang

Mehrak Kiankarimi

Sarah Clough

Arnab Chatterjee

Mike Petrassi

Emily N Chin

Ana Maria Albero

The invention provides compounds having STimulator of INterferon Genes (STING) agonistic bioactivity that can be used in the treatment of tumors in patients afflicted therewith. The compounds are of formula (I): as defined herein. Compounds for practice of a method of the invention can be delivered via oral delivery for systemic exposure, as well as delivered intratumorally. Antitumor therapy using a compound of formula (I) can further comprise administration of an effective dose of an immune-checkpoint targeting drug.

Agonists of stimulator of interferon genes sting

Compounds are provided that modulate the glucagon-like peptide 1 (GLP-1) receptor, as well as products containing such compounds, and methods of their use and synthesis. Such compounds have the structure of Formula (I) below: (I) or pharmaceutically acceptable salts thereof, wherein A, J, W, Y, Z, R, R, Rand Rare as defined herein. 

GLP-1 receptor modulators

Compounds are provided having the structure of the following Formula I: where R, R, R, Rand Rare as defined herein. Pharmaceutical compositions comprising such compounds, as well as methods related to their manufacture and use, are also provided.

CXCR3 receptor agonists

Compounds are provided that modulate the glucagon-like peptide 1 (GLP-1) receptor, as well as methods of their synthesis, and methods of their therapeutic and/or prophylactic use. Such compounds can act as modulators or potentiators of GLP-1 receptor on their own, or with incretin peptides such as GLP-1(7-36) and GLP-1(9-36), or with peptide-based therapies, such as exenatide and liraglutide, and have the following general structure (where '' represents either or both the R and S form of the compound): where A, B, C, Y, Y, Z, R, R, R, R, R, W, n, p and q are as defined herein.

Compounds that selectively modulate the sphingosine 1 phosphate receptor are provided including compounds which modulate subtype 1 of the S1P receptor. Methods of chiral synthesis of such compounds are provided. Uses, methods of treatment or prevention and methods of preparing inventive compositions including inventive compounds are provided in connection with the treatment or prevention of diseases, malconditions, and disorders for which modulation of the sphingosine 1 phosphate receptor is medically indicated.

Selective sphingosine 1 phosphate receptor modulators and methods of chiral synthesis

Compounds are provided that modulate the glucagon-like peptide 1 (GLP-1) receptor, as well as methods of their synthesis, and methods of their therapeutic and/or prophylactic use. Such compounds can act as modulators or potentiators of GLP-1 receptor on their own, or with incretin peptides such as GLP-1(7-36), GLP-1(9-36), and oxyntomodulin, or with peptide-based therapies, such as exenatide and liraglutide, and have the following general structure (where '' represents either or both the R and S form of the compound): where A, B, C, R, R, R, R, R, n, p and q are as defined herein.

Compounds that bind the glucagon-like peptide 1 (GLP-1) receptor, methods of their synthesis, methods of their therapeutic and/or prophylactic use, and methods of their use in stabilizing GLP-1 receptor in vitro for crystallization of the GLP-1 receptor are provided. Certain compounds may have activity as modulators or potentiators with respect to glucagon receptor, GIP receptor, GLP-1 and GLP-2 receptors, and PTH receptor on their own or in the presence of receptor ligands such as GIP(1-42), PTH(1-34), Glucagon(1-29), GLP-2(1-33), GLP-1(7-36), GLP-1(9-36), oxyntomodulin and exendin variants.

GLP-1 receptor stabilizers and modulators

Compounds that selectively modulate the sphingosine 1 phosphate receptor are provided including compounds which modulate subtype 1 of the S1P receptor. Methods of chiral synthesis of such compounds is provided. Uses, methods of treatment or prevention and methods of preparing inventive compositions including inventive compounds are provided in connection with the treatment or prevention of diseases, malconditions, and disorders for which modulation of the sphingosine 1 phosphate receptor is medically indicated.

Selective heterocyclic sphingosine 1 phosphate receptor modulators

Sphingosine 1 phosphate receptor modulators and methods of chiral synthesis

Compounds that bind the glucagon-like peptide 1 (GLP-1) receptor, methods of their synthesis, methods of their therapeutic and/or prophylactic use, and methods of their use in stabilizing GLP-1 receptor in vitro for crystallization of the GLP-1 receptor are provided. Certain compounds may have activity as modulators or potentiators with respect to glucagon receptor, GIP receptor, GLP-1 and GLP-2 receptors, and PTH receptor on their own or in the presence of receptor ligands such as GIP(1-42), PTH(1-34), Glucagon(1-29), GLP-2(1-33), GLP-1 (7-36), GLP-1 (9-36), oxyntomodulin and exendin variants.

Growing community of inventors

Carlsbad, CA, United States of America

Junko Tamiya