Hoffmann-la Roche Inc.

F. Hoffmann-la Roche Ag

European Molecular Biology Laboratory

Savira Pharmaceuticals Gmbh

Rutgers, the State University of New Jersey

Roche Palo Alto LLC

Achyutharao Sidduri

Jefferson Wright Tilley

Robert Alan Goodnow, Jr

Sung-Sau So

Matthew Michael Hamilton

Agnieszka Kowalczyk

Fariborz Firooznia

Tai-An Lin

Romyr Dominique

Qi Qiao

Helmut Heinrich Buschmann

Ronald Charles Hawley

Mark Smith

Paul Gillespie

Shaoqing Chen

Eric Mertz

Stephen Cusack

Norbert Handler

Oliver Szolar

Andrea Wolkerstorfer

Li Chen

Yimin Qian

David Michael Goldstein

Matthew C Lucas

Ryan Craig Schoenfeld

Wylie Solang Palmer

Christophe Michoud

Jenny Tan

Gerald Lewis Kaplan

Jianping Lou

James Patrick Dunn

Ce Wang

Robert W Guthrie

Javier De Vicente Fidalgo

Kin-Chun Thomas Luk

Peter Michael Wovkulich

Michael Soth

Zhuming Zhang

Ramakanth Sarabu

Nader Fotouhi

Allen John Lovey

Wendy Lea Corbett

Johannes Cornelius Hermann

Leyi Gong

Stephen Matthew Lynch

Hongju Li

Kshitij Chhabilbhai Thakkar

Joshua Jahmil Kennedy-Smith

Tai-Nang Huang

Joan Heather Hogg

Fernando Padilla

Stephen Deems Gabriel

Kenneth Gregory Hull

Tania M Silva

Xiaohu Zhang

Xiaochun Han

Teresa Alejandra Trejo-Martin

Joshua Kennedy-Smith

Lubica Raptova

Parcharee Tivitmahaisoon

David Budd

Levi Gong

Counde O'yang

Jayne Chin

Robert Alan Goodnow Jr

Stephen M Lynch

The present disclosure relates to compounds having an improved solubility thereby increasing their bioavailability, lower dosages, etc. The target compounds, may include but are not limited to, macrophage migration inhibitory factor (MIF) inhibitors, epidermal growth factor receptor (EGRF) inhibitors, kinase inhibitors and prodrugs of alpha4 beta1 and alpha4 beta7 integrin antagonists. An illustrative compound is shown below:

Isoidide derivatives and methods of making and using same

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 present disclosure relates to compounds having an improved solubility thereby increasing their bioavailability, lower dosages, etc. The target compounds, may include but are not limited to, macrophage migration inhibitory factor (MIF) inhibitors, epidermal growth factor receptor (EGRF) inhibitors, kinase inhibitors and prodrugs of alpha4 beta1 and alpha4 beta7 integrin antagonists. An illustrative compound is shown below: 

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 present invention relates to a compound having the general formula (V), optionally in the form of a pharmaceutically acceptable salt, solvate, polymorph, codrug, cocrystal, prodrug, tautomer, racemate, enantiomer, or diastereomer or mixture thereof, which are useful in treating, ameliorating or preventing a viral disease. Furthermore, specific combination therapies are disclosed.

Substituted 1,5-naphthyridines as endonuclease inhibitors

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 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 inflammatory diseases and disorders such as, for example, pulmonary fibrosis.

N-alkyltriazole compounds as LPAR antagonists

The present invention relates to a compound having the general formula (V), optionally in the form of a pharmaceutically acceptable salt, solvate, polymorph, codrug, cocrystal, prodrug, tautomer, racemate, enantiomer, or diastereomer or mixture thereof, which are useful in treating, ameloriating or preventing a viral disease. Furthermore, specific combination therapies are disclosed.

Substituted naphthyridines for the treatment, amelioration or prevention of a viral disease

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 inflammatory diseases and disorders such pulmonary fibrosis. 

LPAR&#x2014;substituted cyanopyrazole compounds

The present invention relates to a compound having the general formula (I), optionally in the form of a pharmaceutically acceptable salt, solvate, polymorph, codrug, cocrystal, prodrug, tautomer, racemate, enantiomer, or diastereomer or mixture thereof, which are useful in treating, ameloriating or preventing a viral disease. Furthermore, specific combination therapies are disclosed.

Pyrimidone derivatives and their use in the treatment, amelioration or prevention of a viral disease

The invention is concerned with the compounds of formula (I): and pharmaceutically acceptable salts thereof, wherein R, R, Rand 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 or partial agonists at the CRTH2 receptor and may be useful in treating diseases and disorders associated with that receptor such as asthma.

Substituted naphthylacetic acids

Compounds of formula I modulate jnk and cdk: or a pharmaceutically acceptable salt thereof, where R, R, R, R, and m are defined herein.

Benzotriazole kinase modulators

Piperidinyl naphthylacetic acids

The present invention relates to the use of novel pyrrolopyrazine derivatives of Formula I, wherein the variables are defined as described herein, which inhibit JAK and SYK and are useful for the treatment of auto-immune and inflammatory diseases.

Pyrrolopyrazine kinase inhibitors

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Livingston, NJ, United States of America

Achyutharao Sidduri