Takeda Pharmaceutical Company Limited

Takeda San Diego, Inc.

Anthony R Gangloff

Andrew John Jennings

Jason W Brown

Jeffrey Alan Stafford

Phong H Vu

Jerome C Bressi

Andre A Kiryanov

Benjamin Jones

Sheldon Cao

Xiao-Yi Xiao

Lily Kwok

Steven John Woodhead

Bheema Rao Paraselli

Walter Keung

Stephen W Kaldor

Nicholas Scorah

Mark Sabat

Haixia Wang

Robert J Skene

Steve Swann

Jacek Nowakowski

Simone Bigi

Michael G Tennant

Hasanthi P Wijesekera

Andre K Kiryanov

Disclosed are compounds of formula 1: which are useful as inhibitors of TBK1. Also disclosed are pharmaceutical compositions which contain the compounds, methods for treatment of conditions associated with TBK1, and processes for making the compounds and intermediates thereof.

Heteroarylamide inhibitors of TBK1

The present invention provides compounds of formula 1: which are useful as inhibitors of TBK-1, pharmaceutical compositionst thereof, methods for treatment of conditions associated with TBK1, processes for making the compounds and intermediates thereof.

Disclosed are compounds of the following formula: in which R, R, R, R, R, R, u, and X are defined in the specification. Also disclosed are pharmaceutical compositions, kits, and articles of manufacture, which contain the compounds, methods and intermediates useful for making the compounds, and methods of using the compounds to treat diseases, disorders, and conditions related to PARP activity.

Substituted pyrido[3,2-e]pyrrolo[1,2-a]pyrazines as inhibitors of poly(ADP-ribose)polymerase (PARP)

Compounds of the following formula are provided for use with PARP: wherein the variables are as defined herein. Also provided are pharmaceutical compositions, kits, and articles of manufacture comprising such compounds, methods and intermediates useful for making the compounds, and methods of using the compounds.

Poly (ADP-ribose) polymerase (PARP) inhibitors

Disclosed are compounds of the following formula: 

Substituted pyrido[2,3-b]pyrazines

Compounds of the following formula are provided for use in inhibiting Poly (ADP-ribose) Polymerase (PARP): wherein the variables are defined herein. Also provided are pharmaceutical compositions, kits and articles of manufacture comprising such compounds, methods and intermediates useful for making the compounds, and methods of using the compounds.

Disclosed are compounds of the following formula: in which R, R, R, R, R, X, and q are defined in the specification. Also disclosed are pharmaceutical compositions, kits, and articles of manufacture, which contain the compounds, methods and intermediates useful for making the compounds, and methods of using the compounds to treat diseases, disorders, and conditions related to PARP activity.

Substituted derivatives of pyrido[3,2-e][1,4]thiazino[4,3-a]pyrazine and pyrido[3,2-e][1,4]oxazino[4,3-a]pyrazine

Disclosed are compounds of the following formula: in which R, R, R, R, R, R, X, and m are defined in the specification. Also disclosed are pharmaceutical compositions, kits, and articles of manufacture, which contain the compounds, methods and intermediates useful for making the compounds, and methods of using the compounds to treat diseases, disorders, and conditions related to PARP activity.

Substituted 7,8,9,10-tetrahydro-5H-dipyrido[1,2-a:3',2&#x2032;-e]pyrazin-6(6aH)-ones

Substituted 6a,7,8,9-tetrahydropyrido[3,2-e]pyrrolo[1,2-a]pyrazin-6(5H)-ones

Compounds, pharmaceutical compositions, kits and methods are provided for use with HDAC that comprise a compound selected from the group consisting of: wherein the substituents are as defined herein.

Histone deacetylase inhibitors

Compounds, pharmaceutical compositions, kits and methods useful for inhibiting HDAC, thereby treating a disease state for which HDAC possess activity that contributes to the pathology and/or symptomology of the disease state. The compound is selected from the group consisting of: 

Compounds, pharmaceutical compositions, kits and methods are provided for use with histone deacetylases (HDACs) that comprise a compound of the formulae: wherein the variables are as defined herein.

The invention relates to compounds of the following formula that may be used to inhibits kinases, as well as compositions of matter and kits comprising these compounds. The present invention also relates to methods for inhibiting kinases, as well as treatment methods using compounds according to the present invention. 

Growing community of inventors

San Diego, CA, United States of America

Anthony R Gangloff