Hoffmann-la Roche Inc.

USA As Represented by Secretary of the Navy

F. Hoffmann-la Roche Ag

Lida Qi

Kevin Richard Guertin

Jefferson Wright Tilley

Paul Gillespie

Fariborz Firooznia

Nancy-Ellen Haynes

Adrian Wai-Hing Cheung

Qiang Zhang

Yimin Qian

Eric Mertz

Sherrie Lynn Pietranico-Cole

Kshitij Chhabilbhai Thakkar

Robert Dale Chapman

Nathan Robert Scott

Jenny Tan

Nicholas Marcopulos

Theodore Axenrod

Jianguang Sun

Xiao-Pei Guan

Sung-Sau So

Shawn David Erickson

Ramakanth Sarabu

Robert Alan Goodnow, Jr

Nader Fotouhi

Kyungjin Kim

Jianping Cai

Pamela Loreen Rossman

Warren William McComas

Kevin W Anderson

Chun Ma

Stuart Hayden

Prabha Saba Karnachi

John A Brinkman

Joseph Anthony Bilotta

Jagdish Kumar Racha

Michael Paul Myers

Adrian Wai-Hing

Christine M Lukacs-Lesburg

Kevin William DrANDERSON

The invention relates to JNK inhibitors and corresponding methods, formulations, and compositions for inhibiting JNK and treating JNK-mediated disorders. The application discloses JNK inhibitors, as described below in Formula I: wherein the variables are as defined herein. The compounds and compositions disclosed herein are useful to modulate the activity of JNK and treat diseases associated with JNK activity. Disclosed are methods and formulations for inhibiting JNK and treating JNK-mediated disorders, and the like, with the compounds, and processes for making said compounds, and corresponding compositions, disclosed herein.

Aminomethyl quinolone compounds

Adamantyl compounds

Provided herein are compounds of the formula (I): as well as pharmaceutically acceptable salts thereof, wherein the substituents are as those disclosed in the specification. These compounds, and the pharmaceutical compositions containing them, are useful for the treatment of metabolic diseases and disorders such as, for example, type II diabetes mellitus.

GPR119 receptor agonists

There are presented compounds of the formula  or a pharmaceutically acceptable salt thereof, which are active adenosine A2B receptor antagonists and useful in the treatment of diabetes, diabetic retinopathy, asthma and diarrhea.

Substituted thiazolo[5,4-d]pyrimidine urea derivatives

Provided herein are compounds of the formula (I): as well as pharmaceutically acceptable salts thereof, wherein the substituents are as those disclosed in the specification. These compounds, and the pharmaceutical compositions containing them, are useful for the treatment of diseases such as, for example, type II diabetes mellitus and metabolic syndrome.

Inhibitors of 11&#x3b2;-Hydroxysteroid Dehydrogenase

Adamantyl-pyrazole carboxamides as inhibitors of 11&#x3b2;-hdroxysteroid dehydrogenase

There are presented compounds of the formula or a pharmaceutically acceptable salt thereof, which are useful in the treatment of diabetes, diabetic retinopathy, asthma and diarrhea.

Substituted N-acyl-2-aminothiazoles

This invention involves a new class of compounds, certain geminal-dinitro-substituted heterocycles, including geminal-bis(difluoramino)-substituted heterocyclic nitramines and the production thereof. More specifically, this invention involves the production of 3,3-bis(difluoramino)octahydro-1,5,7,7-tetranitro-1,5-diazocine (TNFX), which may be formulated into explosives and propellant oxidizers. The method of making a 3,3-bis(difluoramino)octahydro-1,5,7,7-tetranitro-1,5-diazocine comprises reacting a hexahydro-7,7-dinitro-1,5-bis(nitrobenzenesulfonyl)-1,5-diazocin-3(2 H)-one with a difluoramine source to produce a 3,3-bis(difluoramino)octahydro-7,7-dinitro-1,5-bis(nitrobenzenesulfonyl)-1,5-diazocine and reacting said 3,3-bis(difluoramino)octahydro-7,7-dinitro-1,5-bis(nitrobenzenesulfonyl)-1,5-diazocine with a highly reactive nitrating reagent in the presence of a strong Lewis acid, such as antimony pentafluoride, boron triflate or boron fluorosulfonate.

Geminal-dinitro-1-5 diazocine derivatives

This invention involves a new class of compounds, certain geminal-dinitro-substituted heterocycles, including geminal-bis(difluoramino)-substituted heterocyclic nitramines and the production thereof. More specifically, this invention involves the production of 3,3-bis(difluoramino)octahydro-1,5,7,7-tetranitro-1,5-diazocine (TNFX), which may be formulated into explosives and propellant oxidizers. The method of making a 3,3-bis(difluoramino)octahydro-1,5,7,7-tetranitro-1,5-diazocine comprises reacting a hexahydro-7,7-dinitro-1,5-bis(nitrobenzenesulfonyl)-1,5-diazocin-3(2H)-one with a difluoramine source to produce a 3,3-bis(difluoramino)octahydro-7,7-dinitro-1,5-bis(nitrobenzenesulfonyl)-1,5-diazocine and reacting said 3,3-bis(difluoramino)octahydro-7,7-dinitro-1,5-bis(nitrobenzenesulfonyl)-1,5-diazocine with a highly reactive nitrating reagent in the presence of a strong Lewis acid, such as antimony pentafluoride, boron triflate or boron fluorosulfonate.

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Leonia, NJ, United States of America

Lida Qi