Wyeth

Forma Therapeutics, Inc.

Novo Nordisk Healthcare Ag

Eutropics Pharmaceuticals, Inc.

Pfizer Corporation

Valo Health, Inc.

Valo Early Discovery, Inc.

David James Richard

David R Lancia, Jr

Zhongguo Wang

Anna M Ericsson

Gary Gustafson

Neal Green

Arie Zask

Kevin Joseph Curran

Tatiana Shelekhin

Jeroen Cunera Verheijen

Joshua Aaron Kaplan

Aranapakam Mudumbai Venkatesan

Christoph Martin Dehnhardt

Ariamala Gopalsamy

Semiramis Ayral-Kaloustian

Tarek Suhayl Mansour

Efren Guillermo Delos Santos

Mengxiao Shi

Lorna Mitchell

Zecheng Chen

Osvaldo Dos Santos

Justin Andrew Caravella

Steven Gregory Mischke

Xiaozhang Zheng

Bingsong Han

Hongbin Li

Chase C Smith

Stephanos Ioannidis

Shawn E R Schiller

David Joseph Guerin

Gary Marshall

Michael H Cardone

Kenneth W Bair

Pui Yee Ng

Matthew W Martin

Angela V West

Andrew Kolodziej

Alex J Buckmelter

Alexandre Joseph Buckmelter

Cuixian Liu

Jian Lin

Patrick F Kelly

Scot Mente

Madhu Mondal

Semiramis Aryl-Kaloustian

Sanjeev Forsyth

Maria Ribadeneira

Patricia Schroeder

Jeroen C Verheijen

Christoph M Dehnhardt

David Lancia

David R Lancia

David R Lancia Jr

Shawn ER Schiller

Jr David R Lancia

Andrew F Kolodziej

The present disclosure relates to modulators, such as inhibitors, of at least one pathway chosen from USP28 and USP25, pharmaceutical compositions comprising the inhibitors, and methods of using the inhibitors. The modulators, such as inhibitors, of at least one pathway chosen from USP28 and USP25 can be useful in the treatment of cancers, among other ailments. The present disclosure provides compounds of Formula (I).

Inhibiting deubiquitinase USP25 and USP28

The compound (S)-1-(5-((2,3-dihydro-[1,4]dioxino[2,3-b]pyridin-7-yl)sulfonyl)-3,4,5,6-tetrahydropyrrolo[3,4-c]pyrrol-2(1H)-yl)-3-hydroxy-2-phenylpropan-1-one, or a pharmaceutically acceptable salt thereof, is useful to increase the affinity of hemoglobin for oxygen. Methods and compositions for the treatment of a hemoglobinopathies are provided herein, including certain pharmaceutical compositions for activating PKR.

Activating pyruvate kinase R

The disclosure provides novel chemical compounds useful as activators of PKR. PKR activating compounds are useful in the treatment of disease and disorders associated with modulation of PKR and/or PKM2, such as pyruvate kinase deficiency (PKD).

The disclosure relates to modulating pyruvate kinase and provides novel chemical compounds useful as activators of PKR, as well as various uses of these compounds. PKR activating compounds are useful in the treatment of diseases and disorders associated with PKR and/or PKM2, such as pyruvate kinase deficiency (PKD), sickle cell disease (SCD), and thalassemia.

Pyrrolopyrrole compositions as pyruvate kinase (PKR) activators

Compounds that activate pyruvate kinase R can be used for the treatment of sickle cell disease (SCD). Methods and compositions for the treatment of SCD are provided herein, including a therapeutic compound designated as Compound 1.

Treating sickle cell disease with a pyruvate kinase R activating compound

This disclosure provides compounds and compositions for activating pyruvate kinase R (PKR) and related methods of manufacturing and using these compounds and compositions.

The disclosure relates to USP30 Inhibitor Compounds, pharmaceutically acceptable salts thereof, pharmaceutical compositions comprising same, and medical uses involving same.

Fused pyrrolines which act as ubiquitin-specific protease 30 (USP30) inhibitors

The disclosure relates to USP30 Inhibitor Compounds I, pharmaceutically acceptable salts thereof, pharmaceutical compositions comprising same, and medical uses involving same. (I) 

The disclosure relates to inhibitors of USP28 and/or USP25 useful in the treatment of cancers, inflammation, autoimmune diseases, and infectious diseases, having the Formula: (I), where R, R, R, R, R, R, R, X, and n are described herein. 

Thienopyrazine carboxamides as ubiquitin-specific protease inhibitors

The present disclosure relates to chemical entities useful as inhibitors of Ubiquitin Specific Protease 30 (USP30), pharmaceutical compositions comprising the chemical entities, and methods of using the chemical entities. The chemical entities as disclosed herein can be useful in the treatment of a disease, disorder, or condition involving mitochondrial dysfunction, including neurodegenerative diseases, motor neuron diseases, metabolic disorders, and cancers, among other ailments. Chemical entities disclosed herein include compounds of Formula (II): wherein A, R, R, R, R, R, R, R, R, and m are defined herein.

Inhibiting ubiquitin specific peptidase 30

The disclosure relates to modulating pyruvate kinase and provides novel chemical compounds of formula (I) useful as activators of PKR, as well as various uses of these compounds. PKR activating compounds are useful in the treatment of diseases and disorders associated with PKR and/or PKM2, such as pyruvate kinase deficiency (PKD), sickle cell disease (SCD), and thalassemia. 

The disclosure provides chemical compounds useful as activators of PKR. PKR activating compounds are useful in the treatment of disease and disorders associated with modulation of PKR and/or PKM2, such as pyruvate kinase deficiency (PKD).

Activating pyruvate kinase R and mutants thereof

Growing community of inventors

Warwick, NY, United States of America

David James Richard