BENZOTHIADIAZINE COMPOUNDS

The invention is directed to substituted benzothiadiazine derivatives. Specifically, the invention is directed to compounds according to Formula (I):wherein R, R1, R2, R3, R4 and R5 are as defined herein. The compounds of the invention are inhibitors of CD73 and can be useful in the treatment of can...

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Main Authors DUFFY, Kevin J, RIDGERS, Lance Howard, GRAYBILL, Todd L, LIAN, Yiqian, KIESOW, Terence John, ADAMS, Jerry Leroy, MOORE, Michael Lee, RALPH, Jeffrey M, ATOR, Laura E
Format Patent
LanguageEnglish
French
Published 15.06.2017
Subjects
CHEMISTRY
HETEROCYCLIC COMPOUNDS
HUMAN NECESSITIES
HYGIENE
MEDICAL OR VETERINARY SCIENCE
METALLURGY
ORGANIC CHEMISTRY
PREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
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Summary:The invention is directed to substituted benzothiadiazine derivatives. Specifically, the invention is directed to compounds according to Formula (I):wherein R, R1, R2, R3, R4 and R5 are as defined herein. The compounds of the invention are inhibitors of CD73 and can be useful in the treatment of cancer, pre-cancerous syndromes and diseases associated with CD73 inhibition, such as AIDS, autoimmune diseases, infections, atherosclerosis, and ischemia-reperfusion injury. 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 CD73 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 de benzothiadiazine substitués. L'invention concerne en particulier des composés de formule (I), dans lesquels R, R1, R2, R3, R4 et R5 sont tels que définis dans la description. Les composés de l'invention sont des inhibiteurs de CD73 et peuvent être utiles dans le traitement du cancer, de syndromes précancéreux et de maladies associées à l'inhibition de CD73, telles que le SIDA, les maladies auto-immunes, les infections, l'athérosclérose, et une lésion de reperfusion ischémique. Par conséquent, l'invention concerne en outre des compositions pharmaceutiques comprenant un composé de l'invention. L'invention concerne en outre des procédés d'inhibition de l'activité de CD73 et le traitement de troubles associés à celui-ci à l'aide d'un composé de l'invention ou d'une composition pharmaceutique comprenant un composé de l'invention.
Bibliography:Application Number: WO2016IB57415