Roche Palo Alto LLC

Principia Biopharma Inc.

Hoffmann-la Roche Inc.

Roche Diabetes Care, Inc.

F. Hoffmann-la Roche Ag

Timothy D Owens

Yan Lou

Rama K Kondru

Michael Soth

Robert Than Hendricks

Kenneth Albert Brameld

Johannes Cornelius Hermann

David Michael Goldstein

Joel McIntosh

Nolan James Dewdney

Bradley E Loe

Francisco Javier Lopez-Tapia

Todd Richard Elworthy

Daisy Joe DuBois

David Bernard Smith

Zachary Kevin Sweeney

Fariborz Firooznia

Roland Joseph Billedeau

Stephen Matthew Lynch

Christine E Brotherton-Pleiss

Hanbiao Yang

Saul Jaime-Figueroa

Joshua Paul Gergely Taygerly

Peter Michael Wovkulich

Calvin Wesley Yee

Buelent Kocer

Steven Joseph Berthel

Stephen Deems Gabriel

Jenny Tan

Xiaochun Han

Remy Lemoine

Joe Timothy Bamberg

Joshua Kennedy-Smith

Lucja Orzechowski

Ramona Hilgenkamp

Yimin Qian

Sung-Sau So

Matthew C Lucas

Keith Adrian Walker

Harvey B Buck, Jr

Alam Jahangir

Keshab Sarma

Kshitij Chhabilbhai Thakkar

Randall K Riggles

Daisy Joe Du Bois

Jutta Wanner

Jaehyeon Park

Omar Jose Morales

Daniel Fishlock

Steven Sethofer

Thomas D Hahn

Mike Limbaugh

Steven Berthel

Shu Hai Zhao

Bradley E Loc

Mark Bartlett

Jun-Bae Hong

Calvin Yee

Ronald J Hill

Provided herein are compounds, such as a compound of Formula (I), or a pharmaceutically acceptable salt thereof, that are immunoproteasome (such as LMP2 and LMP7) inhibitors. The compounds described herein can be useful for the treatment of diseases treatable by inhibition of immunoproteasomes. Also provided herein are pharmaceutical compositions containing such compounds and processes for preparing such compounds.

Immunoproteasome inhibitors

Provided herein are compounds, such as a compound of Formula (I), or a pharmaceutically acceptable salt thereof that are immunoproteasome (such as LMP2 and LMP7) inhibitors. The compounds described herein can be useful for the treatment of diseases treatable by inhibition of immunoproteasomes. Also provided herein are pharmaceutical compositions containing such compounds and processes for preparing such compounds.

A slot die shim for use with a slot die, the slot die shim including a first channel configured to receive a first coating, a second channel configured to receive a second coating, and a third channel configured to receive a third coating. The slot die shim simultaneously dispenses the first coating through the first channel, the second coating through the second channel, and the third coating through the third channel onto a substrate. The coatings can be applied at different flow rates and include different test reagents. A vacuum force is applied to the first, second, and third coatings to control a width and a thickness of each of the coatings and a gap or distance between the coatings. The first, second, and third coatings are placed near one another or directly in contact with one another to minimize the area required for the coatings.

Multi-reagent slot die coating process and useful devices

The present disclosure provides compounds of formula (I) that are tyrosine kinase inhibitors, in particular Bruton tyrosine kinase ('BTK') inhibitors, and are therefore useful for the treatment of diseases treatable by inhibition of BTK such as cancer, autoimmune, inflammatory, and thromboembolic diseases. Also provided are pharmaceutical compositions containing such compounds and processes for preparing such compounds. 

Heterocycle comprising tyrosine kinase inhibitors

Provided herein are compounds, such as a compound of Formula (I), as described herein, or a pharmaceutically acceptable salt thereof, that are immunoproteasome (such as LMP2 and LMP7) inhibitors. The compounds described herein can be useful for the treatment of diseases treatable by inhibition of immunoproteasomes. Also provided herein are pharmaceutical compositions containing such compounds and processes for preparing such compounds.

The present disclosure provides compounds that are Large Multifunctional Protease 7 (LMP7) inhibitors and are therefore useful for the treatment of diseases treatable by inhibition of LMP7. Also provided are pharmaceutical compositions containing such compounds and processes for preparing such compounds.

LMP7 inhibitors

The present disclosure is directed to certain inhibitors of RLK and ITK of formula (I), pharmaceutical compositions comprising such compounds, and method of treating diseases mediated by inhibition of RLK and ITK. 

Benzimidazole derivatives as RLK and ITK inhibitors

The present disclosure provides compounds that are tyrosine kinase inhibitors, in particular Bruton tyrosine kinase ('BTK') inhibitors, and are therefore useful for the treatment of diseases treatable by inhibition of BTK such as cancer, autoimmune, inflammatory, and thromboembolic diseases. Also provided are pharmaceutical compositions containing such compounds and processes for preparing such compounds.

Tyrosine kinase inhibitors

The present disclosure is directed to certain inhibitors of kinases such as ITK, BLK, BMX, BTK, JAK3, TEC, TXK, HER2 (ERBB2), or HER4 (ERBB4), in particular ITK, pharmaceutical compositions comprising such compounds, and method of treating diseases mediated by such kinases.

Benzimidazole derivatives as ITK inhibitors

This application discloses 6-(2-Hydroxymethyl-phenyl)-2-methyl-2H-pyridazin-3-one derivatives according to generic Formula I: wherein, variables X, R, 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 Formula I and at least one carrier, diluent or excipient.

Inhibitors of bruton's tyrosine kinase

This application discloses compounds according to generic Formula I: wherein the variables are defined as described herein, and 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 Formula I and at least one carrier, diluent or excipient.

Inhibitors of bruton'S tyrosine kinase

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.

This application discloses compounds according to generic Formula I: wherein all variables 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 Formula I and at least one carrier, diluent or excipient.

Growing community of inventors

Mountain View, CA, United States of America

Timothy D Owens