Array Biopharma Inc.

Ventirx Pharmaceuticals, Inc.

Cytochroma Inc.

The Johns Hopkins University

Astrazeneca Ab

Hong Woon Yang

Joseph P Lyssikatos

Eli M Wallace

James F Blake

George A Doherty

Allison L Marlow

Jeongbeob Seo

Laurence Edward Burgess

Gary H Posner

Jay A White

Robert Hershberg

Byung-Chul Suh

Glenville Jones

T Brian Hurley

Jim Blake

Qiang Wang

J Jeffry Howbert

Kevin Koch

Robert D Groneberg

Brad Newhouse

Charles Todd Eary

Kenneth R Crawford

James Jeffry Howbert

Uttam Saha

Gregory Dietsch

John David Pittam

John Leonard

Zachary Jones

Venkat Kusukuntla

Richard Storey

Pavel Krasik

Heung Bae Jeon

Brian Hurley

Rebecca Jane Booth

Mark Hatcher

Ji-Long Jiang

HeungBae Jeon

Mark Richard Fielding

Steven M Silverman

Jae Kyoo Lee

Nathan Nielsen

Alexander Tretyakov

Alison Marlow

Richard Anthony Storey

Venkat Reddy Kusukuntla

Provided are compositions and methods useful for modulation of signaling through the Toll-like receptors TLR7 and/or TLR8. The compositions and methods have use in treating or preventing disease, including cancer, autoimmune disease, fibrotic disease, cardiovascular disease, infectious disease, inflammatory disorder, graft rejection, or graft-versus-host disease.

Substituted benzoazepines as toll-like receptor modulators

Provided are compositions and methods useful for modulation of signaling through the Toll-like receptors TLR7 and/or TLR8. The compositions and methods have use in treating or preventing disease, including cancer, autoimmune disease, infectious disease, inflammatory disorder, graft rejection, and graft-verses-host disease.

The disclosure describes method of synthesis of substituted benzazepine derivatives. Preferred methods according to the disclosure allow for large-scale preparation of benzazepine compounds having low levels of metal impurities. In some embodiments, preferred methods according to the disclosure also allow for the preparation of benzazepine derivatives without the use of chromatographic purification methods and in better yield than previously used methods for preparing such compounds. The methods disclosed herein find utility in synthetic organic chemistry as well as medicinal chemistry.

Methods of synthesis of benzazepine derivatives

Disclosed are crystalline forms of 2-(2-fluoro-4-iodophenylamino)-N-(2-hydroxyethoxy)-1,5-dimethyl-6-oxo-1,6-dihydropyridine-3-carboxamide useful in the treatment of hyperproliferative diseases, such as cancer and inflammation, in mammals, and inflammatory conditions. Also disclosed are methods of using such compounds in the treatment of hyperproliferative diseases in mammals and pharmaceutical compositions containing such compounds.

Crystalline forms of 2-(2-flouro-4-iodophenylamino)-N-(2-hydroxyethoxy)-1,5-dimethyl-6-oxo-1,6-dihydropyridine-3-carboxamide

Disclosed are compounds of the Formula V and pharmaceutically acceptable salts and prodrugs thereof, wherein R, R, R, Rand R, and W are as defined in the specification. Such compounds are MEK inhibitors and useful in the treatment of hyperproliferative diseases, such as cancer and inflammation, and inflammatory conditions in mammals. Also disclosed are methods of using such compounds in the treatment of hyperproliferative diseases and inflammatory conditions in mammals and pharmaceutical compositions containing such compounds.

6-oxo-1,6-dihydropyridine derivatives as inhibitors of MEK and methods of use thereof

The present invention provides novel D-ring and side-chain analogs of 1&#x3b1;,25-dihydroxyvitamin D, compositions comprising these compounds and methods of using these compounds as selective inhibitors of CYP24. In particular, the compounds of the invention are useful for treating diseases which benefit from a modulation of the levels of 1&#x3b1;,25-dihydroxyvitamin D, for example, cell-proliferative disorders.

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Disclosed are compounds of the Formula I and pharmaceutically acceptable salts and prodrugs thereof, wherein R, R, R, Rand R, W, X and Y are as defined in the specification. Such compounds are MEK inhibitors and useful in the treatment of hyperproliferative diseases, such as cancer and inflammation, in mammals, and inflammatory conditions. Also disclosed are methods of using such compounds in the treatment of hyperproliferative diseases in mammals and pharmaceutical compositions containing such compounds.

Substituted pyridazines inhibitors of MEK

Disclosed are compounds of the Formula I and pharmaceutically acceptable salts and prodrugs thereof, wherein R, R, R, R, R, and W are as defined in the specification. Such compounds are MEK inhibitors and are useful in the treatment of hyperproliferative diseases, such as cancer and inflammation, and inflammatory conditions in mammals. Also disclosed are methods of using such compounds in the treatment of hyperproliferative and inflammatory diseases in mammals and pharmaceutical compositions containing such compounds.

Heterocyclic inhibitors of MEK and methods of use thereof

Disclosed are compounds of the Formula I 

Bicyclic inhibitors of MEK and methods of use thereof

Disclosed are compounds of the Formulas I and V and pharmaceutically acceptable salts and prodrugs thereof, wherein R, R, R, Rand R, W, X and Y are as defined in the specification. Such compounds are MEK inhibitors and useful in the treatment of hyperproliferative diseases, such as cancer and inflammation, in mammals, and inflammatory conditions. Also disclosed are methods of using such compounds in the treatment of hyperproliferative diseases in mammals and pharmaceutical compositions containing such compounds.

Dihydropyridine and dihydropyridazine derivatives as inhibitors of MEK and methods of use thereof

Disclosed are compounds of the Formula I and pharmaceutically acceptable salts and prodrugs thereof, wherein R, R, R, Rand R, W, X and Y are as defined in the specifications. Such compounds are MEK inhibitors and useful in the treatment of hyperproliferative diseases, such as cancer and inflammation, in mammals, and inflammatory conditions. Also disclosed are methods of using such compounds in the treatment of hyperproliferative diseases in mammals and pharmaceutical compositions containing such compounds.

Disclosed are compounds of the Formula I and pharmaceutically acceptable salts and prodrugs thereof, wherein R, R, R, Rand R, W, X, Y and Z are as defined in the specification. Such compounds are MEK inhibitors and are useful in the treatment of hyperproliferative diseases, such as cancer and inflammation, in mammals, and inflammatory conditions. Also disclosed are methods of using such compounds in the treatment of hyperproliferative diseases in mammals and pharmaceutical compositions containing such compounds.

Disclosed are methods of treating inflammatory diseases and disorders, such as arthritis and inflammatory bowel disease, in mammals.

Method of treating inflammatory diseases

Growing community of inventors

Superior, CO, United States of America

Hong Woon Yang