Merck Sharp + Dohme Corp.

Merck Canada Inc.

Matthew L Maddess

Michael D Altman

Alan B Northrup

Ryan D Otte

John Michael Ellis

Binyuan Sun

Brandon D Cash

Hua Zhou

Jongwon Lim

John S Wai

Maria Emilia Di Francesco

Daniel Guay

Peter D Williams

Jacques Yves Gauthier

Michelle R Machacek

B Wesley Trotter

Yves Ducharme

Shankar Venkatraman

Solomon D Kattar

David Joseph Guerin

Wayne J Thompson

Andrew M Haidle

Dai-Shi Su

Brian M Andresen

Alessia Petrocchi

Tony Siu

Michael Hale Reutershan

Kenneth L Arrington

Mark W Embrey

Christian Fischer

Peter Emmanuel Maligres

John W Butcher

Matthew Christopher

Zhiguo Jake Song

Jonathan B Grimm

Sandra Lee Knowles

Brandon Mitsuo Taoka

Anthony Donofrio

Thorsten E Fisher

Kaleen Konrad Childers

Kerrie Spencer

Vouy Linh Truong

Christian Beaulieu

Sathesh P Bhat

Tao Pei

Joel S Robichaud

Bernard Cote

Eric Thomas Romeo

Adam J Schell

Jingjun Yin

Hyun Chong Woo

Chaomin Li

Dilrukshi Vitharana

David C Dubost

Richard C A Isaacs

Michael Shevlin

Neil A Strotman

Dietrich P Steinhuebel

Richard G Ball

Eric J Choi

Sarah L Trice

Kristina Dupont-Gaudet

Brandon M Taoka

Neil Campbell

Jason Burch

Michael D Altmann

Kerrie B Spencer

Brendan M O'BOYLE

Solomon Kattar

Eric Romeo

Michael H Reutershan

Brendan M O'boyle

Jean-Francois Fournier

Sathesh Bhat

The invention provides certain pyrazine-2-carboxamide compounds of the Formula (I) or pharmaceutically acceptable salts thereof, wherein A, B, and X are as defined herein. The invention also provides pharmaceutical compositions comprising such compounds, and methods of using the compounds for treating diseases or conditions mediated by Spleen Tyrosine Kinase (Syk). 

2-pyrazine carboxamides as spleen tyrosine kinase inhibitors

The present invention provides novel pyrazole derivatives of formula I which are potent inhibitors of spleen tyrosine kinase, and are useful in the treatment and prevention of diseases mediated by said enzyme, such as asthma, COPD, rheumatoid arthritis, and cancer.

Pyrazolyl derivatives as Syk inhibitors

Compounds of Formula I are inhibitors of HIV integrase and inhibitors of HIV replication: wherein X, X, Y, R, R, Rand Rare defined herein. The compounds are useful for the prophylaxis or treatment of infection by HIV and the prophylaxis, treatment, or delay in the onset or progression of AIDS. The compounds are employed against HIV infection and AIDS as compounds per se (or as hydrates or solvates thereof) or in the form of pharmaceutically acceptable salts. The compounds and their salts can be employed as ingredients in pharmaceutical compositions, optionally in combination with other antivirals, immunomodulators, antibiotics or vaccines. Processes for making compounds of Formula I and intermediates thereof are also described.

HIV integrase inhibitors

Growing community of inventors

Boston, MA, United States of America

Matthew L Maddess