Glaxo Group Limited

Glaxosmithkline Intellectual Property Development Limited

Glaxosmithkline LLC

Christopher E Neipp

Michael R Palovich

Brent W McCleland

Sonia M Thomas

Dramane Ibrahim Laine

Jian Wang

Zehong Wan

Vipulkumar Kantibhai Patel

Eric Steven Manas

Xiaomin Zhang

Joseph E Pero

Matthew Robert Sender

Raphael Anthony Rivero

Xichen Lin

Jeffrey K Kerns

Qi Jin

Jakob Busch-Petersen

Guoliang Lin

Damane I Laine

Jeffrey Charles Boehm

Katherine L Widdowson

Hong Nie

Michael Lindenmuth

Jianghe Deng

Wei Fu

Huijie Li

Dramane I Laine

Brent W Mccleland

Brent W Mcceland

The present invention relates to novel compounds that inhibit Lp-PLAactivity, processes for their preparation, to compositions containing them and to their use in the treatment of diseases associated with the activity of Lp-PLA, for example Alzheimer's disease.

Compounds

Disclosed are 4-amino-2-butenamides of Formula (I) having pharmacological activity, pharmaceutical compositions containing them, and methods for the treatment of diseases mediated by the cathepsin C enzyme such as chronic obstructive pulmonary disease. 

Cathepsin C inhibitors

Methods of using Muscarinic Acetylcholine Receptor Antagonists are provided.

Muscarinic acetylcholine receptor antagonists

Muscarinic Acetylcholine Receptor Antagonists and methods of using them are provided.

The invention is directed to novel indole carboxamide derivatives. Specifically, the invention is directed to compounds according to formula I: where R1, R2, R3, U and V are defined below and to pharmaceutically acceptable salts thereof. The compounds of the invention are inhibitors of IKK2 and can be useful in the treatment of disorders associated with inappropriate IKK2 (also known as IKK&#x3b2;) activity, such as rheumatoid arthritis, asthma, and COPD (chronic obstructive pulmonary disease). Accordingly, the invention is further directed to pharmaceutical compositions comprising a compound of the invention. The invention is still further directed to methods of inhibiting IKK2 activity and treatment of disorders associated therewith using a compound of the invention or a pharmaceutical composition comprising a compound of the invention.

Chemical compounds

The invention is directed to novel indole carboxamide derivatives. Specifically, the invention is directed to compounds according to formula (I): wherein R1, R2, R3, R4, and m are as defined herein. The compounds of the invention are inhibitors of IKK2 and can be useful in the treatment of disorders associated with inappropriate IKK2 (also known as IKK&#x3b2;) activity, such as rheumatoid arthritis, asthma, rhinitis, and COPD (chronic obstructive pulmonary disease). Accordingly, the invention is further directed to pharmaceutical compositions comprising a compound of the invention. The invention is still further directed to methods of inhibiting IKK2 activity and treatment of disorders associated therewith using a compound of the invention or a pharmaceutical composition comprising a compound of the invention.

Indole carboxamides as IKK2 inhibitors

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King of Prussia, PA, United States of America

Christopher E Neipp