Astrazeneca Ab

Glaxosmithkline Intellectual Property (No.2) Limited

Supergen, Inc

Krzysztof Swierczek

William Alexander Denny

Abdelmalik Slassi

David J Bearss

Koc-Kan Ho

Hariprasad Vankayalapati

Methvin Benjamin Isaac

Yong Xu

Pasit Phiasivongsa

Sanjeev Redkar

Fupeng Ma

Ian Egle

Joshua Clayton

Michael David Saunders

Babu Joseph

Kevin Bret Wright

Thomas Francis Hendrickson

Swarna Gamage

Darby Brooke

Brian John Stevens

The invention is directed to substituted heteroaryl derivatives. Specifically, the invention is directed to compounds according to Formula Q: wherein D, L, M, W, X, Y, and Z are defined herein. The compounds of the invention are inhibitors of DNA methyltransferase (DNMT) activity&#x2014;including DNMT1, DNMT3a, or DNMT3b&#x2014;and are useful in the treatment of cancer and hyperproliferative diseases. Accordingly, the invention is further directed to pharmaceutical compositions comprising a compound of the invention. The invention is still further directed to methods of inhibiting DNMT activity and treatment of disorders associated therewith using a compound of the invention or a pharmaceutical composition comprising a compound of the invention.

Chemical compounds

Quinoline derivatives, particularly 4-(4-(4-(quinolin-4-ylamino)benzamido)phenylthio)pyrrolidine-2-carboxylic acid; 3-(4-(4-(quinolin-4-ylamino)benzamido)phenylthio)pyrrolidine; N-(4-(piperidin-4-ylthio)phenyl)-4-(quinolin-4-ylamino)-benzamide; and N-(4-(piperidin-3-ylthio)phenyl)-4-(quinolin-4-ylamino)-benzamide, or a physiologically acceptable salt thereof, are provided. Such quinoline derivatives can be used for modulation of DNA methylation, such as effective inhibition of methylation of cytosine at the C-5 position, for example via selective inhibition of DNA methyltransferase DNMT1. Methods for synthesizing numerous 4-anilinoquinoline derivatives and for modulating DNA methylation are provided. Also provided are methods for formulating and administering these compounds or compositions to treat conditions such as cancer and hematological disorders.

Quinoline derivatives for modulating DNA methylation

The present invention is directed to compounds of Formula I: Wherein R, R, Y, m and n are further defined in the description. The invention also relates to processes for the preparation of the compounds and to new intermediates employed in the preparation, pharmaceutical compositions containing the compounds, and to the use of the compounds in therapy.

Oxazolidinone compounds and their use as metabotropic glutamate receptor potentiators

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West Jordan, UT, United States of America

Krzysztof Swierczek