Boehringer Ingelheim Pharmaceuticals, Inc.

Boehringer Ingelheim International Gmbh

Boehringer Ingelheim Pharma Gmbh & Co Kg

Aerie Pharmaceuticals, Inc.

Anthony S Prokopowicz

Roger John Snow

Tina Marie Morwick

Daniel R Goldberg

Neil Moss

Hidenori Takahashi

Abdelhakim Hammach

Sabine K Schlyer

Frank Wu

Michael Robert Turner

John David Ginn

Frank Himmelsbach

Georg Dahmann

Weimin Liu

Alexander Pautsch

Todd Bosanac

Daniel Kuzmich

Martin Steegmaier

Robert Sibley

Mario G Cardozo

Thomas Martin Kirrane, Jr

Steffen Steurer

Usha R Patel

Andreas Schoop

Xiao-Jun Wang

Walter Spevak

Donghong Amy Gao

Daniel Richard Marshall

Martin Lenter

Matt Aaron Tschantz

Bernd Krist

Scott E Jakes

Di Wu

Helmut Wittneben

Erick Richard Young

Cheng-Kon Shih

Martha Priscilla Brown

Jessi Marie Wildeson

Mark E Labadia

Robert D Selliah

Eugene Richard Hickey

Erick Richard Roush Young

Ronald John Sorcek

Wang Mao

Gisela Schnapp

Jennifer A Kowalski

Gisela Schapp

Sabine Schyler

Thomas Martin Kirrane

Jessi Wildeson Jones

Disclosed are novel substituted 2H-isoquinolin-1-one and 3H-quinazolin-4-one derivatives useful as inhibitors of Rho kinase and for treating a variety of diseases and disorders that are mediated or sustained through the activity of Rho kinase, including cardiovascular diseases, pharmaceutical compositions comprising such compounds, methods for using such compounds and processes for making such compounds.

Rho kinase inhibitors

Isoquinolinone Rho kinase inhibitors

The present invention relates to compounds of formula (I): and pharmaceutically acceptable salts thereof, wherein Rto R, A, B, D and X are as defined herein. The invention also relates to pharmaceutical compositions comprising these compounds, methods of using these compounds in the treatment of various diseases and disorders, processes for preparing these compounds and intermediates useful in these processes.

CXCR3 receptor antagonists

The present invention relates to trisubstituted pyrimidines of formula (I) wherein

Pyrimidine derivatives

The present invention relates to compounds of formula (I): and pharmaceutically acceptable salts thereof, wherein Rto R, A, B, X, Y and n are as defined herein. The invention also relates to pharmaceutical compositions comprising these compounds, methods of using these compounds in the treatment of various diseases and disorders, processes for preparing these compounds and intermediates useful in these processes.

The invention provides compounds according to formula (I) their use and methods for preparation wherein A, X, Y, R1, R2 and R3 are defined herein. The compounds of the invention inhibit specific serine/threonine kinases involved in inflammatory processes and aberrant cell proliferation, and are thus useful for treating associated diseases and pathological conditions such as Pim kinase-mediated diseases and pathological conditions involving inflammation, including Chron's disease, inflammatory bowel disease, rheumatoid arthritis, and chronic inflammatory disease, or aberrant cell proliferation including various cancers.

Pyrazine compounds, their use and methods of preparation

The present invention relates to trisubstituted pyrimidines of formula (I) wherein0Rto Rare defined as in claim, which are suitable for the treatment of illnesses characterized by excessive or abnormal cell proliferation, the use thereof for preparing a pharmaceutical composition with the abovementioned properties, and processes for the preparation thereof.

The invention provides methods relating to a screening assay format that can be applied to broad members of the protein kinase gene family. The assay uses a series of labeled, active site probes described herein that can be displaced by an inhibitor agent. The Kfor the inhibitor compound is derived based on the Kof the probe for the kinase and the dose response of the inhibitor agent. The invention also provides active site probes suitable for use with the screening method.

Fluorescent probes for use in protein kinase inhibitor binding assay

The invention provides methods relating to a novel screening assay format that can be applied to broad members of the protein kinase gene family. The assay uses a series of labeled, active site probes described herein that can be displaced by an inhibitor agent. The Kfor the inhibitor compound is derived based on the Kof the probe for the kinase and the dose response of the inhibitor agent. The invention also provides active site probes suitable for use with the screening method.

Disclosed are novel compounds of formula (I):wherein Ar, X, Y, P, Q and Het are defined herein, which are useful as inhibitors of certain protein tyrosine kinases and are thus useful for treating diseases resulting from inappropriate cell proliferation, which include autoimmune diseases, chronic inflammatory diseases, allergic diseases, transplant rejection and cancer, as well as conditions resulting from cerebral ischemia, such as stroke. Also disclosed are pharmaceutical compositions comprising these compounds, processes for preparing these compounds and novel intermediate compounds useful in these processes.

Heterocyclic compounds useful as inhibitors of tyrosine kinases

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Stormville, NY, United States of America

Anthony S Prokopowicz