Millennium Pharmaceuticals Limited

Matthew Stirling

Steven P Langston

Lei Zhu

Eric L Elliott

Quentin J McCubbin

Marianne Langston

Ian G Armitage

Michael A Patane

Christopher F Claiborne

Stephen G Stroud

Natalie Alysia Dales

Todd B Sells

Courtney A Cullis

Christopher Blackburn

Gabriel S Weatherhead

Ashley Sue McCarron

Hiro Mizutani

Omar Stradella

Hirotake Mizutani

Quentin J Mccubbin

Ashley Sue Mccarron

Eric L Elliot

Omar G Stradella

The present invention provides processes and synthetic intermediate (Ia) for the synthesis of 4-substituted ((1S, 2S, 4R)-2-hydroxy-4-{7H-pyrrolo[2,3-d]pyrimidin-7-yl}cyclopentyl)methyl sulfamates. These sulfamate compounds are E1 activating enzyme inhibitors, and are useful for the treatment of disorders of cell proliferation, particularly cancer, and other disorders associated with E1 activity. 

Process for the synthesis of E1 activating enzyme inhibitors

Disclosed are chemical entities which are inhibitors of Nedd8-activating enzyme (NAE), namely, the compound {(1S,2S,4R)-4-[(6-{[(1R,2S)-5-chloro-2-methoxy-2,3-dihydro-1H-inden-1-yl]amino}pyrimidin-4-yl)oxy]-2-hydroxycyclopentyl}methyl sulfamate and pharmaceutically acceptable salts thereof; solid state forms thereof; and prodrugs thereof. Also disclosed are methods of using the chemical entities to treat disorders such as cancer.

Inhibitors of NEDD8-activating enzyme

The present invention provides sulfamoylating reagents of formula RN&#x2014;S(O)X, wherein X is a cyclic tertiary amine or a nitrogen-containing heteroaryl and Ris an amine protecting group or hydrogen.

Sulfamoylating reagents

Disclosed are processes and synthetic intermediates for the synthesis of compounds of formula (V) wherein the variables have the definitions contained herein. Such compounds are E1 activating enzyme inhibitors, and are useful for the treatment of disorders of cell proliferation, particularly cancer, and other disorders associated with E1 activity. 

The present invention provides novel compounds useful as inhibitors of protein kinases. The invention also provides pharmaceutical compositions comprising the compounds of the invention and methods of using the compositions in the treatment of various diseases.

Lactam compounds useful as protein kinase inhibitors

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Boston, MA, United States of America

Matthew Stirling