Glaxosmithkline Intellectual Property (no.2) Limited

Frank Preugschat

Robert B Perni

Rodolfo Cadilla

Bruce G Szczepankiewicz

Karsten Koppetsch

Brad Richard Henke

David Norman Deaton

Curt Haffner

J David Becherer

Christie Schulte

Provided herein are stereoisomerically pure ester and carbonate analogues of nicotinamide riboside and nicotinamide riboside hydride, and pharmaceutical compositions and uses thereof. The stereoisomerically pure ester and carbonate analogues of nicotinamide riboside and nicotinamide riboside hydride may be used to treat a disease or disorder that would benefit from increased NAD levels including a mitochondrial disease or disorder, insulin resistance, a metabolic syndrome, diabetes, obesity, for increasing insulin sensitivity in a subject, or to treat or prevent a skin condition. The compounds have general formulas (I) or (II): wherein Ris &#x2014;C(&#x2550;O)&#x2014;X&#x2014;(C-Cstraight chain or branched) alkyl or &#x2014;C(&#x2550;O)&#x2014;X&#x2014;(C-Cstraight chain or branched) alkenyl; each Ris independently selected from hydrogen, and a &#x2014;C(O)&#x2014;X&#x2014;(C-Cstraight chain or branched) alkyl or a &#x2014;C(O)&#x2014;X&#x2014;(C-Cstraight chain or branched) alkenyl; and X is a covalent bond or O.

Nicotinamide riboside analogs and pharmaceutical compositions and uses thereof

Compounds of Formula I and methods of treating diseases of metabolism by modulating cellular NAD+ levels through the inhibition of the CD38 enzyme, are disclosed. 

CD38 inhibitors and methods of treatment

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Research Triangle Park, NC, United States of America

Frank Preugschat