公开(公告)号：US20230250081A1

公开(公告)日：2023-08-10

申请号：US18163151

申请日：2023-02-01

Applicant: Board of Regents, The University of Texas System

Inventor： Philip JONES ,  Michael J. SOTH ,  Jason P. BURKE ,  Kang LE ,  Gang LIU

IPC: C07D401/14 ,  A61K31/501 ,  A61K45/06 ,  A61P35/00 ,  A61K31/337

CPC classification number: C07D401/14 ,  A61K31/501 ,  A61K45/06 ,  A61P35/00 ,  A61K31/337 ,  C07B2200/13

Abstract: 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.

公开(公告)号：US20220267311A1

公开(公告)日：2022-08-25

申请号：US17654301

申请日：2022-03-10

Applicant: Board of Regents, The University of Texas System

Inventor： Michael J. SOTH ,  Gang LIU ,  Kang LE ,  Jason CROSS ,  Philip JONES

IPC: C07D413/14 ,  C07D401/04 ,  C07D471/04 ,  C07D417/14 ,  C07D401/14 ,  C07D405/14

Abstract: 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).

公开(公告)号：US20210206745A1

公开(公告)日：2021-07-08

申请号：US17124051

申请日：2020-12-16

Applicant: Board of Regents, The University of Texas System

Inventor： Philip JONES ,  Michael J. SOTH ,  Jason P. BURKE ,  Kang LE ,  Gang LIU

IPC: C07D401/14 ,  A61K31/501 ,  A61K45/06 ,  A61P35/00 ,  A61K31/337

Abstract: 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.

公开(公告)号：US20190308978A1

公开(公告)日：2019-10-10

申请号：US16378309

申请日：2019-04-08

Applicant: Board of Regents, The University of Texas System

Inventor： Kang LE ,  Michael J. SOTH ,  Gang LIU ,  Philip JONES ,  Jason Bryant CROSS ,  Timothy Joseph MCAFOOS ,  Christopher L. CARROLL ,  Richard T. LEWIS

IPC: C07D487/04 ,  C07D519/00

Abstract: 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.

公开(公告)号：US20190270736A1

公开(公告)日：2019-09-05

申请号：US16412050

申请日：2019-05-14

Applicant: Board of Regents, The University of Texas System

Inventor： Maria Emilia DI FRANCESCO ,  Philip JONES ,  Timothy HEFFERNAN ,  Matthew M. HAMILTON ,  Zhijun KANG ,  Michael J. SOTH ,  Jason P. BURKE ,  Kang LE ,  Christopher Lawrence CARROLL ,  Wylie S. PALMER ,  Richard LEWIS ,  Timothy MCAFOOS ,  Barbara CZAKO ,  Gang LIU ,  Jay THEROFF ,  Zachary HERRERA ,  Anne YAU

IPC: C07D417/14 ,  A61K31/497 ,  C07D493/08 ,  A61K31/444 ,  C07D403/14 ,  C07D405/14 ,  A61K31/4192 ,  A61K31/4439 ,  C07D401/14 ,  A61K31/501 ,  C07D403/06 ,  A61K31/433 ,  C07D417/06 ,  A61K45/06 ,  A61K31/454

Abstract: 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.

公开(公告)号：US20190092764A1

公开(公告)日：2019-03-28

申请号：US16121198

申请日：2018-09-04

Applicant: Board of Regents, The University of Texas System

Inventor： Michael J. SOTH ,  Gang LIU ,  Kang LE ,  Jason CROSS ,  Philip JONES

IPC: C07D413/14 ,  C07D471/04 ,  C07D401/04 ,  C07D405/14 ,  C07D401/14 ,  C07D417/14

Abstract: 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).

公开(公告)号：US20170174661A1

公开(公告)日：2017-06-22

申请号：US15387560

申请日：2016-12-21

Applicant: Board of Regents, The University of Texas System

Inventor： Philip JONES ,  Michael J. SOTH ,  Jason B. BURKE ,  Kang LE ,  Gang LIU

IPC: C07D401/14 ,  A61K45/06 ,  A61N5/10 ,  A61K31/501

CPC classification number: C07D401/14 ,  A61K31/501 ,  A61K45/06 ,  C07B2200/13

Abstract: 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.

公开(公告)号：US20240360121A1

公开(公告)日：2024-10-31

申请号：US18597265

申请日：2024-03-06

Applicant: Board of Regents, The University of Texas System

Inventor： Maria Emilia DI FRANCESCO ,  Philip JONES ,  Timothy HEFFERNAN ,  Matthew M. HAMILTON ,  Zhijun KANG ,  Michael J. SOTH ,  Jason P. BURKE ,  Kang LE ,  Christopher Lawrence CARROLL ,  Wylie S. PALMER ,  Richard LEWIS ,  Timothy MCAFOOS ,  Barbara CZAKO ,  Gang LIU ,  Jay THEROFF ,  Zachary HERRERA ,  Anne YAU

IPC: C07D417/14 ,  A61K31/4192 ,  A61K31/433 ,  A61K31/4439 ,  A61K31/444 ,  A61K31/454 ,  A61K31/497 ,  A61K31/501 ,  A61K45/06 ,  C07D401/14 ,  C07D403/06 ,  C07D403/14 ,  C07D405/14 ,  C07D417/06 ,  C07D493/08

CPC classification number: C07D417/14 ,  A61K31/4192 ,  A61K31/433 ,  A61K31/4439 ,  A61K31/444 ,  A61K31/454 ,  A61K31/497 ,  A61K31/501 ,  A61K45/06 ,  C07D401/14 ,  C07D403/06 ,  C07D403/14 ,  C07D405/14 ,  C07D417/06 ,  C07D493/08

Abstract: 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.

公开(公告)号：US20230124815A1

公开(公告)日：2023-04-20

申请号：US17660541

申请日：2022-04-25

Applicant: Board of Regents, The University of Texas System

Inventor： Maria Emilia DI FRANCESCO ,  Philip JONES ,  Timothy HEFFERNAN ,  Matthew M. HAMILTON ,  Zhijun KANG ,  Michael J. SOTH ,  Jason P. BURKE ,  Kang LE ,  Christopher Lawrence CARROLL ,  Wylie S. PALMER ,  Richard LEWIS ,  Timothy MCAFOOS ,  Barbara CZAKO ,  Gang LIU ,  Jay THEROFF ,  Zachary HERRERA ,  Anne YAU

IPC: C07D417/14 ,  A61K31/4439 ,  A61K45/06 ,  C07D417/06 ,  A61K31/433 ,  C07D403/06 ,  A61K31/501 ,  C07D401/14 ,  A61K31/454 ,  A61K31/4192 ,  C07D405/14 ,  C07D403/14 ,  A61K31/444 ,  C07D493/08 ,  A61K31/497

Abstract: 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.

公开(公告)号：US20190144425A1

公开(公告)日：2019-05-16

申请号：US16241596

申请日：2019-01-07

Applicant: Board of Regents, The University of Texas System

Inventor： Philip JONES ,  Michael J. SOTH ,  Jason P. BURKE ,  Kang LE ,  Gang LIU

IPC: C07D401/14 ,  A61K31/501 ,  A61K45/06

Abstract: 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.