Roche Palo Alto LLC

Syntex (u.s.a.) Inc.

F. Hoffmann-la Roche Ag

Leyi Gong

Denis John Kertesz

Robert Stephen Wilhelm

David Bernard Smith

David Michael Goldstein

Francisco Xavier Talamas

Wylie Solang Palmer

Joan Heather Hogg

Xiaochun Han

Tania M Silva

Deborah Carol Reuter

Yun-chou Tan

James Patrick Dunn

Counde O'Yang

Alam Jahangir

Humberto Bartolome Arzeno

Teresa Alejandra Trejo-Martin

Kristen Lynn McCaleb

Lubica Raptova

Parcharee Tivitmahaisoon

Frederick Arthur Brookfield

Eric Brian Sjogren

Michael Patrick Dillon

Bernd Buettelmann

Achyutharao Sidduri

Gary A Peltz

David Mark Rotstein

Christophe Michoud

Shao-Yong Wu

Bradley E Loe

Donald Roy Hirschfeld

Pravin Iyer

Jaehyeon Park

Andrew Grupe

Geneviève N Boice

Sarah C Abbot

Lubov Konstantinovna Filonova

David Berard Smith

Ferenc Makra

Florence Eustache

Patricia Ann Day-Lollini

Yun-Chou Tan

Erin M O'Brien

Lubov Filonova

Tania Silva

Inhibitors of JNK

The invention relates to JNK inhibitors and corresponding methods, formulations, and compositions for inhibiting JNK and treating JNK-mediated disorders. The application discloses JNK inhibitors, as described below in Formula I: wherein p, q, Y', r, R, R, X, X, X, X, and Xare as defined herein. The compounds and compositions disclosed herein are useful to modulate the activity of JNK and treat diseases associated with JNK activity. Disclosed are methods and formulations for inhibiting JNK and treating JNK-mediated disorders, and the like, with the compounds, and processes for making said compounds, and corresponding compositions, disclosed herein.

This application discloses novel pyrimidinyl pyridone derivatives according to Formula I, wherein R, R, and Rare defined as described herein, which inhibit JNK. The compounds disclosed herein are useful to modulate the activity of JNK and treat diseases associated with excessive JNK activity. The compounds are useful to treat autoimmune, inflammatory, metabolic, and neurological diseases as well as cancer. Also disclosed are compositions comprising the compound of Formula I and methods of treatment comprising administering a therapeutically effective amount of the compound of Formula I to a subject in need thereof.

Pyrimidinyl pyridone inhibitors of JNK

Compounds of formula I modulate JNK: wherein the variables are as defined herein.

JNK modulators

This application discloses novel pyrimidinyl pyridone derivatives according to formula I, wherein A, R, R, R, and m are defined as described herein, which inhibit JNK. The compounds disclosed herein are useful to modulate the activity of JNK and treat diseases associated with excessive JNK activity. The compounds are useful to treat autoimmune, inflammatory, metabolic, and neurological diseases as well as cancer. Also disclosed are compositions comprising the compound of formula I and methods of treatment comprising administering a therapeutically effective amount of the compound of formula I to a subject in need thereof.

Pyrimidinyl pyridone inhibitors of kinases

Compounds of formula I modulate JNK: wherein where Ris H, lower acyl, or an amino acid,

The invention relates to prodrugs of JNK inhibitors and corresponding methods, formulations, and compositions for inhibiting JNK and treating JNK-mediated disorders. The application discloses prodrugs of JNK inhibitors, as described below in formula I: wherein m, n, p, q, Q, r, R, R, R, X, X, X, X, X, X, Y, Y, Zand Zare as defined herein. The compounds and compositions disclosed herein are useful to modulate the activity of JNK and treat diseases associated with JNK activity. Disclosed are methods and formulations for inhibiting JNK and treating JNK-mediated disorders, and the like, with the compounds, and processes for making said compounds, and corresponding compositions, disclosed herein.

Compounds of formula I are effective modulators of JNK: wherein

Dihydroquinone and dihydronaphthridine inhibitors of JNK

The present invention relates to propionamide compounds of formula I for use as antiinflammatory agents: wherein R, Rand Rare as defined herein and pharmaceutically acceptable salts thereof. The invention also relates to methods of using the compounds of formula I and pharmaceutical compositions comprising the compounds of formula I.

Propionamide compounds as antiinflammatory agents

This invention relates to the use of inhibitors of glycogen synthase kinase-3&#x3b2; to increase bone formation.

Methods for increasing bone formation using inhibitors of glycogen synthase kinase-3&#x3b2;

The present invention relates to compounds of formula I: wherein A, X, R, Rand Rare as defined herein and pharmaceutically acceptable salts thereof. The invention also relates to methods of using the compounds of formula I and pharmaceutical compositions comprising the compounds of formula I.

Glucocorticoid receptor modulators as antiinflammatory agents

Compounds having the formula (I),Ar&#x2014;(F)-(E)-(CRR)&#x2014;(CHR)-(T)-(Q)-Ar,are useful as CCR-3 receptor antagonists, wherein T is a bridged heterocyclyl group having one N atom and a bridge of one to two bridgehead carbon atoms; Ar and Arare aryl or heteroaryl; F is alkylene, alkenylene, or a bond; E is &#x2014;C(&#x2550;O)N(R)&#x2014;, &#x2014;SON(R)&#x2014;, &#x2014;N(R)C(&#x2550;O)N(R)&#x2014;, &#x2014;N(R)SON(R)&#x2014;, &#x2014;N(R)C(&#x2550;S)N(R)&#x2014;, &#x2014;N(R)C(&#x2550;O)&#x2014;, &#x2014;N(R)SO&#x2014;, &#x2014;N(R)C(&#x2550;O)CH(R)&#x2014;, or CH(R)C(&#x2550;O)N(R)&#x2014;; Q is &#x2014;C(&#x2550;O)&#x2014; or Calkylene; and R, R, R, R, R, R, R, and Rare defined as set forth in the specification.

Bridged bicyclic amine derivatives useful as CCR-3 receptor antagonists

This invention relates to certain cyclic amine derivatives of Formula (I)that are CCR-3 receptor antagonists, pharmaceutical compositions containing them, methods for their use and methods for preparing these compounds.

Cyclic amine derivatives-CCR-3 receptor antagonists

Growing community of inventors

San Mateo, CA, United States of America

Leyi Gong