The University of Texas System

Hoffmann-La Roche Inc.

F. Hoffmann-La Roche Ag

Takeda Pharmaceutical Company Limited

Kang Le

Philip Jones

Michael J Soth

Gang Liu

Jason P Burke

Christopher Lawrence Carroll

Timothy Joseph McAfoos

Jason Cross

Richard T Lewis

Matthew Michael Hamilton

Maria Emilia Di Francesco

Robert Alan Goodnow, Jr

Barbara Czako

Timothy P Heffernan

Jay Theroff

Zhijun Kang

Zachary Herrera

Anne Yau

Wylie S Palmer

Yan Lou

Stacy W Remiszewski

Christophe Michoud

Paul Gillespie

Steven Gregory Mischke

Robert Francis Kester

Shaoqing Chen

Jianping Cai

Pijus K Mandal

Andrew Forrest Donnell

Kenneth Carey Rupert

Yi Heng Chen

Kin-Chun Thomas Luk

Peter Michael Wovkulich

Nader Fotouhi

Norman Kong

Xin-Jie Chu

Weiya Yun

John Frederick Boylan

Kenneth C Rupert

Joan Heather Hogg

Agnieszka Kowalczyk

Xiaochun Han

John Anthony Moliterni

Qiang Zhang

Timothy Mcafoos

Martin Weisel

Michael P Soth

Jason B Burke

Disclosed herein is the compound (R)-1-(4-(6-(2-(4-(3,3-difluorocyclobutoxy)-6-methylpyridin-2-yl)acetamido) pyridazin-3-yl)-2-fluorobutyl)-N-methyl-1H-1,2,3-triazole-4-carboxamide, and salt forms and polymorphs thereof demonstrating improved exposure after oral dosing. Methods of inhibition GLS1 activity in a human or animal subject are also provided.

Salt forms and polymorphs of (R)-1-(4-(6-(2-(4-(3,3-difluorocyclobutoxy)-6-methylpyridin-2-yl)acetamido) pyridazin-3-yl)-2-fluorobutyl)-n-methyl-1H-1,2,3-triazole-4-carboxamide

The present disclosure relates to heterocyclic compounds and methods which may be useful as inhibitors of transcription activating proteins such as CBP and P300 for the treatment or prevention of diseases such as proliferative diseases, inflammatory disorders, autoimmune diseases, and fibrotic diseases.

Imidazopiperazine inhibitors of transcription activating proteins

Disclosed herein are compounds and compositions useful in the treatment of GLS1 mediated diseases, such as cancer, having the structure of Formula I: Methods of inhibition GLS1 activity in a human or animal subject are also provided.

GLS1 inhibitors for treating disease

Salt forms and polymorphs of (r)-1-(4-(6-(2-(4-(3,3-difluorocyclobutoxy)-6-methylpyridin-2-yl)acetamido) pyridazin-3-yl)-2-fluorobutyl)-n-methyl-1H-1,2,3-triazole-4-carboxamide

Disclosed herein are compounds which inhibit the kinase activity of dual leucine zipper (DLK) kinase (MAP3K12), pharmaceutical compositions, and methods of treatment of DLK-mediated diseases, such as neurological diseases that result from traumatic injury to central nervous system and peripheral nervous system neurons (e.g. stroke, traumatic brain injury, spinal cord injury), or that result from a chronic neurodegenerative condition (e.g. Alzheimer's disease, frontotemporal dementia, Parkinson's disease, Huntington's disease, amyotrophic lateral sclerosis, spinocerebellar ataxia, progressive supranuclear palsy, Lewy body disease, Kennedy's disease, and other related conditions), from neuropathies resulting from neurological damage (chemotherapy-induced peripheral neuropathy, diabetic neuropathy, and related conditions) and from cognitive disorders caused by pharmacological intervention (e.g. chemotherapy induced cognitive disorder, also known as chemobrain).

Bicyclo[1.1.1]pentane inhibitors of dual leucine zipper (DLK) kinase for the treatment of disease

Disclosed herein are compounds of structural Formula VIIa or VIIb: or a pharmaceutically acceptable salt thereof, and compositions thereof useful in the treatment of GLS1 mediated diseases, such as cancer. Methods of inhibition GLS1 activity in a human or animal subject are also provided.

Imidazopiperazinone inhibitors of transcription activating proteins

Disclosed herein is the compound (R)-1-(4-(6-(2-(4-(3,3-difluorocyclobutoxy)-6-methylpyridin-2-yl)acetamido)pyridazin-3-yl)-2-fluorobutyl)-N-methyl-1H-1,2,3-triazole-4-carboxamide, and salt forms and polymorphs thereof demonstrating improved exposure after oral dosing. Methods of inhibition GLS1 activity in a human or animal subject are also provided.

Salt forms and polymorphs of (R)-1-(4-(6-(2-(4-(3,3-difluorocyclobutoxy)-6-methylpyridin-2-yl)acetamido)pyridazin-3-yl)-2-fluorobutyl)-N-methyl-1H-1,2,3-triazole-4-carboxamide

Disclosed herein are compounds and compositions useful in the treatment of GLS1 mediated diseases, such as cancer, having the structure of Formula I:  Methods of inhibition GLS1 activity in a human or animal subject are also provided.

Salt forms and polymorphs of (R)-1-(4-(6-(2-(4-(3,3-difluorocyclobutoxy)-6-methylpyrdin-2-yl)acetamido) pyridazin-3-yl)-2-fluorobutyl)-N-methyl-1H-1,2,3-triazole-4-carboxamide

Disclosed are compounds of Formula I, or pharmaceutically acceptable salts thereof, wherein W, X, Y, Z, R, R, R, Rand Rare as described in this application, and methods of using said compounds in the treatment of cancer. 

Tetrahydro-benzodiazepinones

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Sugar Land, TX, United States of America

Kang Le