Roche Palo Alto LLC

Hoffmann-La Roche Inc.

F. Hoffmann-La Roche Ag

Wylie Solang Palmer

Leyi Gong

Juergen Wichmann

Thomas Johannes Woltering

David Michael Goldstein

Erwin Goetschi

Silvia Gatti McArthur

Tania M Silva

Xiaochun Han

David Bernard Smith

Zachary Kevin Sweeney

James Patrick Dunn

Achyutharao Sidduri

Denis John Kertesz

Humberto Bartolome Arzeno

Tobias Gabriel

Christophe Michoud

Nancy Elisabeth Krauss

Joan Heather Hogg

Teresa Alejandra Trejo-Martin

Joshua Kennedy-Smith

Taraneh Mirzadegan

Lubica Raptova

Michael Martin

Parcharee Tivitmahaisoon

Bernd Buettelmann

Alam Jahangir

David Mark Rotstein

Shao-Yong Wu

Bindu Goyal

Bradley E Loe

Silvia Gatti Mcarthur

Joe Timothy Bamberg

Kristen Lynn McCaleb

Deborah Carol Reuter

Yun-chou Tan

Lubov Konstantinovna Filonova

Ferenc Makra

Geneviève N Boice

Erin M O'Brien

Yun-Chou Tan

Levi Gong

Lubov Filonova

Tania Silva

Jürgen Wichmann

Compounds of formula I modulate jnk and cdk: or a pharmaceutically acceptable salt thereof, where R, R, R, R, and m are defined herein.

Benzotriazole kinase modulators

Inhibitors of JNK

Compounds of formula (I) modulate JNK wherein Xand Xare each simultaneously N or CH; Xis CH&#x2014;ROr N&#x2014;SOR, where R is lower alkyl; Ris aryl or heteroaryl, substituted with 0-3 lower alkyl radicals; Ris (II), where Ris H, lower acyl, or an amino acid, or a pharmaceutically acceptable salt thereof. 

JNK modulators

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.

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.

The present invention relates to compounds of formula (I): wherein Rto R, A, M, L, E, G, and J are as defined in the description and claims. The invention also relates to a process for the manufacture of such compounds, pharmaceutical compositions containing them, and methods for treating CNS disorders.

Acetylenyl-pyrazolo-pyrimidine derivatives

The present invention provides for compounds useful for treating an HIV infection, or preventing an HIV infection, or treating AIDS or ARC. The compounds of the invention are of formula I wherein A is A2 and R, R, R, R, R, R, R, Ar, X, X, X, Xand Xare as herein defined. Also disclosed in the present invention are methods of treating an HIV infection with compounds defined herein and pharmaceutical compositions containing said compounds. 

Non-nucleoside reverse transcriptase inhibitors

The present invention provides for compounds useful for treating an HIV infection, or preventing an HIV infection, or treating AIDS or ARC. The compounds of the invention are of formula I wherein A is A1, A2, A3 or A4 and R, R, R, R, R, R, R, Ar, X, X, X, Xand Xare as herein defined. Also disclosed in the present invention are methods of treating an HIV infection with compounds defined herein and pharmaceutical compositions containing said compounds. 

The present invention provides a process for the preparation 6-[3-(hetero)aryloxy-2-fluoro-benzyl]-2H-pyridazin-3-one compounds 1 where R2 is an optionally substituted aryl or an optionally substituted heteroaryl, Ris NO, NH, alkyl, halogen, or a function group readily derived therefrom and Ris hydrogen or alkyl. There also is provided a process for the preparation of phenylacetic acid compounds 2, wherein Rand Rare as defined previously and Ris hydrogen or alkyl, which are useful for the preparation of pyridazinone compounds.

Phenylacetic acid compounds

The present invention provides a process for the preparation of phenylacetic acid compounds 2 where Ris an optionally substituted aryl, Ris NO, NH, alkyl, halogen, or a function group readily derived there from and Ris hydrogen Calkyl, tert-butyl or benzyl The compounds of formula 2a are useful intermediates for the preparation of HIV reverse transcriptase inhibitors 

Process for preparing 3-aryloxy-phenylacetic acid compounds

Growing community of inventors

Mountain View, CA, United States of America

Wylie Solang Palmer