Roche Palo Alto LLC

Hoffmann-La Roche Inc.

F. Hoffmann-La Roche Ag

Michael Soth

Yan Lou

Rama K Kondru

Timothy D Owens

Nolan James Dewdney

Johannes Cornelius Hermann

Robert Than Hendricks

Joel McIntosh

Stephen Matthew Lynch

Tobias Gabriel

Bradley E Loe

Eric Brian Sjogren

Counde O'Yang

Hanbiao Yang

Remy Lemoine

Zachary Kevin Sweeney

Matthew C Lucas

Todd Richard Elworthy

Joshua Jahmil Kennedy-Smith

Fernando Padilla

Nidhi Arora

Joe Timothy Bamberg

David Bernard Smith

David Michael Goldstein

Javier De Vicente Fidalgo

Kin-Chun Thomas Luk

Alam Jahangir

Allen John Lovey

Roland Joseph Billedeau

David Garrett Loughhead

Hongju Li

Joshua Kennedy-Smith

Joshua Paul Gergely Taygerly

David George Putman

Daisy Joe DuBois

Sanja Novakovic

Matthew Michael Hamilton

Ce Wang

Achyutharao Sidduri

Peter Michael Wovkulich

Ryan Craig Schoenfeld

Shaoqing Chen

Calvin Wesley Yee

Daisy Joe Du Bois

Xiaohu Zhang

Teresa Alejandra Trejo-Martin

Kristen Lynn McCaleb

Jaehyeon Park

Nam T Le

Niala Bhagirath

Calvin Yee

Xao-Fa Lin

Bradley E Loc

Counde O'yang

Mark Bartlett

Stephen M Lynch

The present invention relates to the use of novel compounds of formula I: wherein all variable substituents are defined as described herein, which are SYK inhibitors and are useful for the treatment of auto-immune and inflammatory diseases. 

Inhibitors of SYK

The present invention relates to the use of novel triazolopyridine derivatives of formula I: wherein all variable substituents are defined as described herein, which are SYK inhibitors and are useful for the treatment of auto-immune and inflammatory diseases.

Pyridazine amide compounds useful as SYK inhibitors

This application discloses 5-phenyl-1H-pyridin-2-one and 6-phenyl-2H-pyridazin-3-one derivatives according to generic Formulae I-IV: wherein, variables R, X, Y, Y, Y, Y, Y, n and m are defined as described herein, which inhibit Btk. The compounds disclosed herein are useful to modulate the activity of Btk and treat diseases associated with excessive Btk activity. The compounds are further useful to treat inflammatory and auto immune diseases associated with aberrant B-cell proliferation such as rheumatoid arthritis. Also disclosed are compositions comprising compounds of Formulae I-IV and at least one carrier, diluent or excipient.

Inhibitors of bruton's tyrosine kinase

Compounds of formula and pharmaceutically acceptable salts thereof are described, as well as the pharmaceutical compositions containing said compounds and their pharmaceutically acceptable salts, and the use of said compounds and pharmaceutical compositions for the treatment, control or amelioration of AML.

Imidazo pyrazines

The present invention relates to the use of novel pyrrolopyrazine derivatives of Formula I, wherein the variables are defined as described herein, which inhibit JAK and SYK and are useful for the treatment of auto-immune and inflammatory diseases.

Pyrrolopyrazine kinase inhibitors

The present invention relates to the use of novel compounds of Formula I, wherein the variables m, n, p, q, Q, r, R, R', X, X&#x2032;, Y, Z, Z, and Zare defined as described herein, which inhibit JAK and are useful for the treatment of auto-immune and inflammatory diseases.

Inhibitors of JAK

This application discloses 5-phenyl-1H-pyrazin-2-one derivatives according to generic Formulae I-V: wherein, variables Q, R, Y, Y, Y, Y, Y, n and m are defined as described herein, which inhibit Btk. The compounds disclosed herein are useful to modulate the activity of Btk and treat diseases associated with excessive Btk activity. The compounds are further useful to treat inflammatory and auto immune diseases associated with aberrant B-cell proliferation such as rheumatoid arthritis. Also disclosed are compositions comprising compounds of Formulae I-V and at least one carrier, diluent or excipient.

Inhibitors of Burton's tyrosine kinase

The present invention relates to the use of novel pyrrolopyrazine derivatives of Formula I, wherein the variables n, p, q, Q, X, X' and Y are defined as described herein, which inhibit JAK and SYK and are useful for the treatment of auto-immune and inflammatory diseases.

The present invention relates to the use of novel pyrrolopyrazine derivatives of Formula I, wherein the variables Q, R, R, and Y are defined as described herein, which inhibit JAK and SYK and are useful for the treatment of auto-immune and inflammatory diseases.

This application discloses 6-Phenyl-imidazo[1,2-a]pyrazine derivatives according to generic Formulae I-V: wherein, variables Q, R, Y, Y, Y, Y, n, and m are defined as described herein, which inhibit Btk. The compounds disclosed herein are useful to modulate the activity of Btk and treat diseases associated with excessive Btk activity. The compounds are further useful to treat inflammatory and auto immune diseases associated with aberrant B-cell proliferation such as rheumatoid arthritis. Also disclosed are compositions comprising compounds of Formulae I-V and at least one carrier, diluent or excipient.

Inhibitors of Bruton's tyrosine kinase

This application discloses novel imidazo[1,2-a]pyridine and imidazo[1,2-b]pyridazine derivatives according to Formulae I-VI: wherein R, R', R&#x2033;, Q, X, and Y are defined as described herein, which inhibit Btk. The compounds disclosed herein are useful to modulate the activity of Btk and treat diseases associated with excessive Btk activity. The compounds are further useful to treat inflammatory and auto immune diseases associated with aberrant B-cell proliferation such as rheumatoid arthritis. Also disclosed are compositions containing compounds of Formulae I-VI and at least one carrier, diluent or excipient.

The present invention relates to the use of novel pyrrolopyrazine derivatives of Formula I, wherein the variables Q and Rand Rare defined as described herein, which inhibit JAK and SYK and are useful for the treatment of auto-immune and inflammatory diseases.

This application discloses 6-Phenyl-imidazo[1,2-a]pyridine and 6-Phenyl-imidazo[1,2-b]pyridazine derivatives according to generic Formulae I-V: wherein, variables Q, R, X, Y, Y, Y, Y, n, and m are defined as described herein, which inhibit Btk. The compounds disclosed herein are useful to modulate the activity of Btk and treat diseases associated with excessive Btk activity. The compounds are further useful to treat inflammatory and auto immune diseases associated with aberrant B-cell proliferation such as rheumatoid arthritis. Also disclosed are compositions comprising compounds of Formulae I-V and at least one carrier, diluent or excipient.

The present invention relates to the use of novel macrocyclic compounds of Formula I, wherein the variables Q, Q, Q, Q, and Qare defined as described herein, which inhibit JAK and are useful for the treatment of auto-immune and inflammatory diseases.

Macrocyclic inhibitors of JAK

Growing community of inventors

Milpitas, CA, United States of America

Michael Soth