Hoffmann-la Roche Inc.

Hoffmann-le Roche Inc.

F. Hoffmann-la Roche Ag

Robert Alan Goodnow, Jr

Paul Gillespie

Achyutharao Sidduri

Agnieszka Kowalczyk

Jefferson Wright Tilley

Matthew Michael Hamilton

Kang Le

Romyr Dominique

Qi Qiao

Nader Fotouhi

Jianping Cai

Qiang Zhang

Sung-Sau So

Alexander Mayweg

Fariborz Firooznia

Nancy-Ellen Haynes

Sherrie Lynn Pietranico-Cole

Kevin Richard Guertin

Kshitij Chhabilbhai Thakkar

Tai-An Lin

Nathan Robert Scott

Michael Paul Myers

Li Chen

Bernd Kuhn

Werner Neidhart

Yi Heng Chen

Jens-Uwe Peters

Guido Galley

Daniel Hunziker

Yun He

Hongying Yun

Shawn David Erickson

Kin-Chun Thomas Luk

Peter Michael Wovkulich

Kurt E Amrein

Zhuming Zhang

Steven Gregory Mischke

Binh Vu

Xin-Jie Chu

Norman Kong

Waleed Danho

Shaoqing Chen

John Frederick Boylan

Christophe Michoud

Jenny Tan

Lee Apostle McDermott

Lida Qi

Nicholas J S Huby

John Anthony Moliterni

Joseph Swistok

Pamela Loreen Rossman

Steve Yik-Kai Tam

Zhenshan Zhang

Wajiha Khan

Kevin W Anderson

David Charles Fry

Joseph Anthony Bilotta

Jean-Baptiste Blanc

Jianping Lou

Bruce Lester Banner

Richard Jones

Jayne Chin

Binh Thanh Vu

The invention relates to the chitosan polymer derivatives of formula I: and pharmaceutically acceptable salts and esters thereof, wherein Y, X, X, R, R, and n are defined in the detailed description and claims. The chitosan polymer derivatives of formula I bind to or associate with alpha-4-beta-1 (&#x3b1;4&#x3b2;1) and alpha-V-beta-3 (&#x3b1; V&#x3b2;3) integrin dimers and can be used in delivery formulations to deliver drugs, nucleic acids, or other therapeutic compounds to tissues or cells expressing such integrins. 

Chitosan covalently linked with small molecule integrin antagonist for targeted delivery

The invention relates to compounds of formula (I), wherein R1, R2, and n are defined in the detailed description and claims. In particular, the present invention relates to the compounds of formula I for use in the manufacture and delivery of conjugated moieties such as small molecules, peptides, nucleic acids, fluorescent moieties, and polymers which are linked to LFA-1 integrin antagonists to target cells expressing LFA-1. 

Integrin antagonist conjugates for targeted delivery to cells expressing LFA-1

The invention relates to compounds of formula (I): wherein R, R, and n are defined in the detailed description and claims. In particular, the present invention relates to the compounds of formula (I) for use in the manufacture and delivery of conjugated moieties such as small molecules, peptides, nucleic acids, fluorescent moieties, and polymers which are linked to alpha-V-beta-3 integrin antagonists to target cells expressing alpha-V-beta-3. 

Integrin antagonist conjugates for targeted delivery to cells expressing alpha-V-beta-3

The invention relates to compounds of formula I: wherein R1, R2, and n are defined in the detailed description and claims. In particular, the present invention relates to the compounds of formula I for use in the manufacture and delivery of conjugated moieties such as small molecules, peptides, nucleic acids, fluorescent moieties, and polymers which are linked to VLA-4 integrin antagonists to target cells expressing VLA-4. 

Integrin antagonist conjugates for targeted delivery to cells expressing VLA-4

Provided herein are neuropeptide-2 receptor agonists of the formula (I):Y&#x2014;R&#x2014;R&#x2014;X&#x2014;R&#x2014;R&#x2014;R&#x2014;R&#x2014;R&#x2014;R&#x2014;R&#x2014;R&#x2014;R&#x2014;R&#x2014;R&#x2014;R&#x2014;NH&#x2003;&#x2003;(I) (SEQ ID NO: 1),as well as pharmaceutically acceptable salts, derivatives and fragments 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, obesity and diabetes.

Neuropeptide-2 receptor (Y-2R) agonists

The invention is concerned with the compounds of formula I: and pharmaceutically acceptable salts and esters thereof, wherein R-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 of formula I are antagonists at the CRTH2 receptor and may be useful in treating diseases and disorders associated with that receptor such as asthma.

Substituted aminotetralines

The invention is concerned with the compounds of formula I: and pharmaceutically acceptable salts and esters thereof, wherein R-R, A, B, Q, W, and X 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 at the CRTH2 receptor and may be useful in treating diseases and disorders associated with that receptor such as asthma.

Bi-aryl aminotetralines

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, COPD.

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Leukotriene B4 inhibitors

The invention is directed to compounds of formula (1) and pharmaceutically acceptable salts thereof, methods for the preparation thereof, and methods of use thereof.

Thiazolyl-benzimidazoles

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.

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

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, obesity.

Inhibitors of stearoyl-CoA desaturase

Thiazoles as inhibitors of 11&#x3b2;-hydroxysteroid dehydrogenase

Growing community of inventors

Gillette, NJ, United States of America

Robert Alan Goodnow, Jr