SUBSTITUTED PYRIDINES AS INHIBITORS OF DNMT1

The invention is directed to substituted pyridine derivatives. Specifically, the invention is directed to compounds according to Formula (Iar): (Iar) wherein Yar, X1ar, X2ar, R1ar, R2ar, R3ar, R4ar and R5ar are as defined herein; or a pharmaceutically acceptable salt or prodrug thereof. The compound...

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Bibliographische Detailangaben
Hauptverfasser:	ADAMS, Nicholas David, RUEDA BENEDE, Maria Lourdes, MILLER, William Henry, KING, Bryan Wayne, REIF, Alexander Joseph, SCHMIDT, Stanley J, EVANS, Karen Anderson, FOSBENNER, David T, WIGGALL, Kenneth, BENOWITZ, Andrew B, LI, Mei, ROMERIL, Stuart Paul
Format:	Patent
Sprache:	eng ; fre
Schlagworte:	CHEMISTRY HETEROCYCLIC COMPOUNDS HUMAN NECESSITIES HYGIENE MEDICAL OR VETERINARY SCIENCE METALLURGY ORGANIC CHEMISTRY PREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS ORMEDICINAL PREPARATIONS
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Beschreibung
Zusammenfassung:	The invention is directed to substituted pyridine derivatives. Specifically, the invention is directed to compounds according to Formula (Iar): (Iar) wherein Yar, X1ar, X2ar, R1ar, R2ar, R3ar, R4ar and R5ar are as defined herein; or a pharmaceutically acceptable salt or prodrug thereof. The compounds of the invention are selective inhibitors of DNMT1 and can be useful in the treatment of cancer, pre-cancerous syndromes, beta hemoglobinopathy disorders, sickle cell disease, sickle cell anemia, and beta thalassemia, and diseases associated with DNMT1 inhibition. 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 DNMT1 activity and treatment of disorders associated therewith using a compound of the invention or a pharmaceutical composition comprising a compound of the invention. L'invention concerne des dérivés substitués de pyridine. Plus particulièrement, l'invention concerne des composés selon la formule (Iar) : (Iar) dans laquelle Yar, X1ar, X2ar, R1ar, R2ar, R3ar, R4ar et R5ar sont tels que définis dans la description ; ou un sel ou un promédicament pharmaceutiquement acceptable correspondant. Les composés de l'invention sont des inhibiteurs sélectifs de DNMT1 et peuvent être utiles dans le traitement du cancer, de syndromes précancéreux, de troubles de bêta-hémoglobinopathie, de la drépanocytose, de l'anémie drépanocytaire et de la bêta-thalassémie et de maladies associées à l'inhibition du DNMT1. Par conséquent, l'invention concerne en outre des compositions pharmaceutiques comprenant un composé de l'invention. L'invention concerne en plus encore des procédés d'inhibition de l'activité de la DNMT1 et de traitement de troubles associés à celle-ci à l'aide d'un composé de l'invention ou d'une composition pharmaceutique comprenant un composé de l'invention.