Millennium Pharmaceuticals Limited

Takeda Pharmaceutical Company Limited

Steven P Langston

Hirotake Mizutani

Stepan Vyskocil

Edward James Olhava

Stephane Peluso

Dylan Bradley England

Stephen Critchley

Christopher F Claiborne

He Xu

Courtney A Cullis

Gabriel S Weatherhead

Marianne Langston

Matthew O Duffey

Ian G Armitage

Zhigen Hu

Charles McIntyre

Koji Ono

Paul E Fleming

Francois Soucy

Irache B Visiers

Jeffrey P Ciavarri

Tzu-Tshin Wong

Indu T Bharathan

Yingchun Ye

Jeffrey L Gaulin

Roushan Afroze

Lei Zhu

Eric L Elliott

Quentin J McCubbin

Brian Scott Freeze

Matthew Stirling

Mario Girard

Yongbo Hu

Gang Li

Alexandra E Gould

Paul D Greenspan

Martin Ian Cooper

Jeffrey Ciavarri

Reenu Chopra

Hiro Mizutani

Quentin J Mccubbin

Charles Mcintyre

Thomas George Gant

Masaaki Hirose

Mitsuhiro Ito

Masanori Okaniwa

Scott Freeze

Marlo Girard

Hirotake Mitzutani

Francois R Soucy

Irache Visiers

Eric L Elliot

The present disclosure provides STING modulators/agonists, and methods of synthesis and methods for using for the prophylaxis or treatment of cancer and other STING-related diseases. The present disclosure relates to a compound represented by the Formula (I):

Sting modulator compounds, and methods of making and using

The present disclosure provides STING modulators/agonists, and methods of synthesis and methods for using for the prophylaxis or treatment of cancer and other STING-related diseases. The present disclosure relates to a compound represented by the Formula (I): wherein each symbol is as defined in the description, or a pharmaceutically acceptable salt thereof. 

Disclosed are chemical entities which are compounds of formula (I): or pharmaceutically acceptable salts thereof; wherein Y, R, R', R, R, X, X, X, R, Z, and Zhave the values described herein and stereochemical configurations depicted at asterisked positions indicate absolute stereochemistry. Chemical entities according to the disclosure can be useful as inhibitors of Sumo Activating Enzyme (SAE). Further provided are pharmaceutical compositions comprising a compound of the disclosure and methods of using the compositions in the treatment of proliferative, inflammatory, cardiovascular, and neurodegenerative diseases or disorders.

Heteroaryl compounds useful as inhibitors of SUMO activating enzyme

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

Heteroaryl compounds useful as inhibitors of sumo activating enzyme

Disclosed are chemical entities that inhibit ubiquitin-activating enzyme (UAE), each of which is a compound of Formula I: or a pharmaceutically acceptable salt thereof, wherein Y is and W, Z, X, R, Rand Rare defined herein; pharmaceutical compositions comprising the chemical entities; and methods of using the chemical entities. These chemical entities are useful for treating disorders, particularly cell proliferation disorders, including cancers.

Pyrazolopyrimidinyl inhibitors of ubiquitin-activating enzyme

Disclosed is a compound of formula (I): crystalline forms thereof, and solvates thereof; pharmaceutical compositions comprising a pharmaceutically effective amount of the compound of formula (I), or a crystalline form thereof, or a solvate thereof, and a pharmaceutically acceptable carrier or diluent; and the use of a compound of formula (I), or a crystalline form thereof, or a solvate thereof, for treating a patient suffering from, or subject to, a pathological condition capable of being ameliorated by inhibiting an E1 activating enzyme, particularly NAE, including, e.g., cancer.

Hydrochloride salt of((1S,2S,4R)-4-{4-[(1S)-2,3-dihydro-1H-inden-1-ylamino]-7H-pyrrolo[2,3-D]pyrimidin-7-YL}-2-hydroxycyclopentyl) methyl sulfamate

Disclosed are chemical entities which are compounds of formula (I): or pharmaceutically acceptable salts thereof; wherein Y, R, R, R, R, X, X, X, R, Z, and Zhave the values described herein and stereochemical configurations depicted at asterisked positions indicate absolute stereochemistry. Chemical entities according to the disclosure can be useful as inhibitors of Sumo Activating Enzyme (SAE). Further provided are pharmaceutical compositions comprising a compound of the disclosure and methods of using the compositions in the treatment of proliferative, inflammatory, cardiovascular, and neurodegenerative diseases or disorders.

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

This invention relates to compounds that inhibit E1 activating enzymes, pharmaceutical compositions comprising the compounds, and methods of using the compounds. The compounds are useful for treating disorders, particularly cell proliferation disorders, including cancers, inflammatory and neurodegenerative disorders; and inflammation associated with infection and cachexia.

Heteroaryl compounds useful as inhibitors of E1 activating enzymes

Disclosed are compounds of formula (I); or a pharmaceutically acceptable salt thereof; wherein Y, R, R, R, R, X, R, R, R, R, m, and G have the values described herein and stereochemical configurations depicted at asterisked positions indicate absolute stereochemistry, useful as inhibitors of Sumo Activating Enzyme (SAE). Further provided are pharmaceutical compositions comprising a compound of the disclosure and methods of using the compositions in the treatment of proliferative, inflammatory, cardiovascular and neurodegenerative diseases or disorders. 

Heteroaryl inhibitors of sumo activating enzyme

Growing community of inventors

North Andover, MA, United States of America

Steven P Langston