Yale University

Pfizer Corporation

Warner-lambert Company

Glaxosmithkline Intellectual Property Development Limited

Cambridge Enterprise Limited University of Cambridge

Denton Wade Hoyer

Clarke Bentley Taylor

Matthew Frank Brown

Edmund Lee Ellsworth

Timothy Allan Johnson

Chris Limberakis

Joseph Scott Warmus

Sean Timothy Murphy

Manjinder Singh Lall

Debra Ann Sherry

Elizabeth Spencer

Elias Lolis

Lucian Del Priore

Huey Cai

Mark Fields

Mark Plummer

Charles Francis Donovan

Craig M Crews

Mel C Schroeder

Christopher Fanger

Demetrios Braddock

Joelle Le

John David Harling

Jonathan A Ellman

William L Jorgensen

James Marino Hamby

Sebastien Andre Campos

Karen S Anderson

Timothy Allen Johnson

Ian Edward David Smith

Afjal Hussain Miah

Jessica Elizabeth Reed

Anton Bennett

Julien Michel

Peter C Gareiss

Jeffrey Gustafson

Cleo J Chivikas Connolly

Christopher James Deur

Hyun-Seop Tae

Haya Jamali

Anke G Roth

Francine Foss

Yulia Surovtseva

Dennis Buckley

Alessio Ciulli

Chris Lim-Berakis

Inge Van Molle

The disclosure provides compounds, and compositions comprising such compounds, that can be used to treat CXCR5-expressing cancers, especially angioimmunoblastic T cell lymphoma (AICL) and/or cutaneous T cell lymphoma (CTCL).

CXCR5 antagonists and methods of treating diseases or disorders using same

The invention provides a method of treating retinal degenerations, such as but not limited to anterior segment ocular disorders and/or age-related macular degeneration (AMD), in a subject, the method comprising administering to the subject a pharmaceutical composition comprising an effective amount of a compound of formula (1) or formula (2). In a further aspect, the invention provides compounds of formula (2). In certain embodiments, the compounds of the invention prevent or minimize cellular assault, such as oxidative stress-related cellular assault, and/or promote cell viability.

Compounds and methods for treating or preventing anterior segment ocular disorders and/or retinal degenerations

In one aspect, the invention provides compounds and methods that are useful for treating bacterial infections:

Siderophore conjugated pyrazolidinones, and analogues thereof

The present invention provides compounds and methods for treating, ameliorating, and/or preventing a MKP-5 modulated disease. In certain embodiments, the MKP-5 modulated disease is a fibrotic disease.

Compounds and compositions for treating fibrosis

The present invention relates to bifunctional compounds, which find utility as modulators of targeted ubiquitination, especially inhibitors of a variety of polypeptides and other proteins that are degraded and/or otherwise inhibited by bifunctional compounds of the present invention. In particular, the present invention is directed to compounds, which contain on one end a VHL ligand that binds to the ubiquitin ligase and on the other end a moiety that binds a target protein, such that the target protein is placed in proximity to the ubiquitin ligase to effect degradation (and inhibition) of that protein. The present invention exhibits a broad range of pharmacological activities associated with compounds of the present invention, consistent with the degradation/inhibition of targeted polypeptides.

Compounds and methods for the enhanced degradation of targeted proteins and other polypeptides by an E3 ubiquitin ligase

The invention relates to a compound of formula (I): or a pharmaceutically acceptable salt thereof, thereof, wherein: and pharmaceutically acceptable salts, prodrugs, hydrates, or solvates, thereof, wherein A, B, L-L, A, B, R-R, and m are as defined herein. The invention also relates to pharmaceutical compositions comprising the compounds of formula (I) and their use in treating a bacterial infection.

Hydroxamic acid derivatives useful as antibacterial agents

The invention relates to a compound of formula (I): or a pharmaceutically acceptable salt thereof, thereof, wherein: G is a group of formula (II); and pharmaceutically acceptable salts, prodrugs, hydrates, or solvates, thereof, wherein A, B. L-LA, B, R-Rand m are as defined herein. The invention also relates to pharmaceutical compositions comprising the compounds of formula (I) and their use in treating a bacterial infection.

This invention provides phenyl-substituted pyrimidopyrimidines, dihydropyrimido-pyrimidines, pyridopyrimidines, naphthyridines, and pyridopyrazines of the general formula: that inhibit cyclin-dependent kinase and tyrosine kinase enzymes, methods and intermediate compounds for their synthesis, as well as pharmaceutical compositions and methods for their use in treating, inhibiting or preventing maladies associated with cell proliferative disorders, including angiogenesis, atherosclerosis, restenosis, and cancer.

Kinase inhibitors

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Niantic, CT, United States of America

Denton Wade Hoyer