Celgene International Ii Sarl

Receptos, Inc.

Respivert Limited

Topivert Pharma Limited

Michael Knaggs

Premji Meghani

Esther Martinborough

Marcus F Boehm

Liming Huang

Manisha Moorjani

Junko Tamiya

Andrew Richard Novak

Thomas Fowler

Adam Richard Yeager

Enugurthi Brahmachary

Mark T Griffith

Daniel Glynn

Mark Mills

Stephen Thom

Matthew Colin Thor Fyfe

Stephen Malcolm Thom

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.

GLP-1 receptor modulators

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.

There are provided compounds of formula I, wherein Rto R, X, X, Ar, L, A, A, E and G have meanings given in the description, which compounds have antiinflammatory activity (e.g. through inhibition of one or more of members of: the family of p38 mitogen-activated protein kinase enzymes; Syk kinase; and members of the Src family of tyrosine kinases) and have use in therapy, including in pharmaceutical combinations, especially in the treatment of inflammatory diseases, including inflammatory diseases of the lung, eye and intestines.

Kinase inhibitors

The invention relates to compounds that modulate the glucagon-like peptide 1 (GLP-1) receptor, methods of their synthesis, and methods of their therapeutic and/or prophylactic use. Such compounds are act as modulators or potentiators of GLP-1 receptor on their own, or with receptor ligands including GLP-1 peptides 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 bind the glucagon-like peptide 1 receptor (GLP-1) receptor are provided including compounds which are modulators of the GLP-1 receptors and compounds which are capable of inducing a stabilizing effect on the receptor for use in structural analysis of the GLP-1 receptor. Methods of synthesis, methods of therapeutic and/or prophylactic use, and methods of use in stabilizing GLP-1 receptor in vitro for crystallization of the GLP-1 receptor of such compounds are provided.

GLP-1 receptor stabilizers and modulators

Compounds that bind the glucagon-like peptide 1 receptor (GLP-1) receptor are provided including compounds which are modulators of the GLP-1 receptors and compounds which are capable of inducing a stabilizing effect on the receptor for use in structural analyses of the GLP-1 receptor. Methods of synthesis, methods of therapeutic and/or prophylactic use, and methods of use in stabilizing GLP-1 receptor in vitro for crystallization of the GLP-1 receptor of such compounds are provided.

Growing community of inventors

Burton-on-Trent, United Kingdom

Michael Knaggs