Sri International

Roche Palo Alto LLC

F. Hoffmann-la Roche Ag

Jaehyeon Park

Chandraiah Lagisetti

Thomas R Webb

David Bernard Smith

Yan Lou

Eric Brian Sjogren

Frederick Arthur Brookfield

David Michael Goldstein

Michael Patrick Dillon

Timothy D Owens

Michael Soth

Alam Jahangir

Todd Richard Elworthy

Rama K Kondru

Ling Jong

Johannes Cornelius Hermann

Leyi Gong

Robert Than Hendricks

Calvin Wesley Yee

Hanbiao Yang

Joan Heather Hogg

Daisy Joe Du Bois

Xiaochun Han

Remy Lemoine

Joe Timothy Bamberg

Deborah Carol Reuter

Daisy Joe DuBois

Chih-Tsung Chang

Florence Eustache

Mark Bartlett

The disclosure generally relates to substituted purine analogs that are dual CLK2/CDK1 inhibitors or more potent and specific CLK inhibitors to target CLK2 and CDK1 kinases. These compounds may be useful in the treatment of germ-line mutations of the spliceosome leading to the development of cancers and other human disease. This abstract is intended as a scanning tool for purposes of searching in the particular art and is not intended to be limiting of the present invention.

Dual CLK/CDK1 inhibitors for cancer treatment

The invention provides mitogen-activated protein kinase kinase kinase kinase 4 (MAP4K4) inhibitors, and pharmaceutically acceptable salts, hydrides and stereoisomers thereof. The compounds are employed in pharmaceutical compositions, and methods of making and use, including treating a person in need thereof with an effective amount of the compound or composition, and detecting a resultant diminution of tumor cell growth, cancer or metastasis.

MAP4K4 (HGK) inhibitors

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

The present invention relates to the use of novel pyrrolopyrazine derivatives of Formula I, wherein the variables Q and R 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

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Sunnyvale, CA, United States of America

Jaehyeon Park