Hoffmann-la Roche Inc.

Genentech, Inc.

F. Hoffmann-la Roche Ag

Kyungjin Kim

Shawn David Erickson

Sherrie Lynn Pietranico-Cole

Warren William McComas

Hans G Richter

Rainer Eugen Martin

Henrietta Dehmlow

Ulrike Obst Sander

Caterina Bissantz

Qingjie Ding

Paul Gillespie

Allen John Lovey

Christoph Ullmer

Jefferson Wright Tilley

Patrizio Mattei

Yimin Qian

Steven Gregory Mischke

Lin Yi

Prabha Saba Karnachi

Agostino Perrotta

Sung-Sau So

Peter Michael Wovkulich

Christine E Brotherton-Pleiss

Hongju Li

Kshitij Chhabilbhai Thakkar

Steven Joseph Berthel

Nan Jiang

Emily Aijun Liu

Zhi Chen

Joseph P Lyssikatos

Li Chen

Anthony A Estrada

Huifen Chen

Robert Francis Kester

Nader Fotouhi

Nancy-Ellen Haynes

Mark Edward Zak

Xin-Jie Chu

Weiya Yun

Shaoqing Chen

Johannes Cornelius Hermann

Kevin Richard Guertin

Adrian Wai-Hing Cheung

Nathan Robert Scott

Lida Qi

Qiang Zhang

Chun Ma

John Guilfoyle Mullin, Jr

Hong Wang

Christoph Ulmer

John Guifoyle Mullin, Jr

This invention relates to novel 3-aminopyridines of the formula wherein B, Band Rto Rare as defined in the description and in the claims, as well as pharmaceutically acceptable salts thereof. These compounds are GPBAR1 agonists and can be used as medicaments for the treatment of diseases such as type II diabetes.

3-amino-pyridines as GPBAR1 agonists

The invention is concerned with the compounds of formula (I): and salts thereof, wherein X, Y, Z, R, R, R, R, R, Rand Rare defined in the detailed description and claims. In addition, the present invention relates to methods of manufacturing and using the compounds of Formula (I) as well as pharmaceutical compositions containing such compounds. The compounds may be useful in treating diseases and conditions mediated by TRPA1, such as pain.

Substituted sulfonamide compounds

The invention is concerned with the compounds of formula (I): and pharmaceutically acceptable salts thereof, wherein Y, R1, R2 and R3 are defined in the detailed description and claims. In addition, the present invention relates to methods of manufacturing and using the compounds of formula (I) as well as pharmaceutical compositions containing such compounds. The compounds of formula (I) are antagonists of the TRPA1 channel and may be useful in treating inflammatory diseases and disorders associated with that channel.

Substituted phenylcarbamate compounds

This invention relates to novel 3-aminopyridines of the formula 

This invention relates to novel 1-hydroxyimino-3-phenyl-propanes of the formula wherein Rto Rare as defined in the description and in the claims, as well as pharmaceutically acceptable salts thereof. These compounds are GPBAR1 agonists and may be used as medicaments for the treatment of diseases such as type II diabetes.

1-hydroxyimino-3-phenyl-propanes

This invention relates to novel phenyl amide or pyridyl amide derivatives of the formula wherein A, A, B, Band Rto Rare as defined in the description and in the claims, as well as pharmaceutically acceptable salts thereof. These compounds are GPBAR1 agonists and can be used as medicaments for the treatment of diseases such as type II diabetes.

4-phenoxy-nicotinamide or 4-phenoxy-pyrimidine-5-carboxamide compounds

There are provided compounds of the formula (I) wherein Q, Rand Rare defined herein. The compounds have activity as anticancer agents.

Pyrrolopyrimidone and pyrrolopyridone inhibitors of tankyrase

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

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 obesity, hyperphagia, anxiety, depression and related disorders and diseases.

MCH receptor antagonists

The invention relates to pyrimido[5,4-e][1,2,4]triazine-5,7-diamine compounds which are useful for inhibiting protein tyrosine phosphatases, particularly PTP1B, and are useful for lowering blood glucose concentrations in mammals.

Diaminopyrroloquinazolines compounds as protein tyrosine phosphatase inhibitors

Novel diaminothiazoles of formula (I): are discussed. These compounds selectively inhibit the activity of Cdk4 and are thus useful in the treatment or control of cancer, in particular, the treatment or control of solid tumors. This invention also provides pharmaceutical compositions containing such compounds and methods of treating or controlling cancer, most particularly, the treatment or control of breast, lung, colon, and prostate tumors.

Diaminothiazoles

Disclosed are novel diaminothiazoles that are selective inhibitors of Cdk4. These compounds and their pharmaceutically acceptable salts and esters are anti-proliferative agents useful in the treatment or control of solid tumors, in particular breast, colon, lung and prostate tumors. Also disclosed are pharmaceutical compositions containing these compounds as well as intermediates useful in the preparation of the compounds.

Intermediates useful in the preparation of diaminothiazoles

Diaminothiazoles having antiproliferative activity

The present invention provides compounds having formula (II): wherein X, n, R&#x2013;Rare defined herein, or a pharmaceutically acceptable salt thereof. The invention also provides a pharmaceutical composition comprising a therapeutically effective amount of a compound represented by formula (II) and a pharmaceutically acceptable carrier or excipient. The invention further provides a method for treating cancer comprising administering to a patient in need of such treatment a therapeutically effective amount of a compound represented by formula (II).

Substituted piperidines

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Livingston, NJ, United States of America

Kyungjin Kim