公开(公告)号：WO2016145383A1

公开(公告)日：2016-09-15

申请号：PCT/US2016/022138

申请日：2016-03-11

Applicant: BOARD OF REGENTS, UNIVERSITY OF TEXAS SYSTEM

Inventor： LEWIS, Richard, Thomas ,  JONES, Philip ,  PETROCCHI, Alessia ,  REYNA, Naphtali ,  HAMILTON, Matthew, Michael ,  LEO, Elisabetta

IPC: A61K31/506 ,  A61K31/505 ,  A61P35/00 ,  C07D403/04 ,  C07D473/16

CPC classification number: C07D403/04 ,  A61K45/06 ,  C07D239/42 ,  C07D239/47 ,  C07D239/48 ,  C07D239/52 ,  C07D239/70 ,  C07D239/95 ,  C07D253/075 ,  C07D401/04 ,  C07D401/12 ,  C07D403/12 ,  C07D405/12 ,  C07D487/08 ,  C07D491/048

Abstract: Disclosed herein are compounds and compositions having the structure of Formula I, which are useful in the treatment of diseases, such as cancer, where inhibition of MTHl is expected to confer an advantage to a patient. Methods of inhibition of MTHl activity in a human or animal subject are also provided.

Abstract translation: 本文公开了具有式I结构的化合物和组合物，其可用于治疗诸如癌症的疾病，其中MTH1的抑制预期赋予患者优势。 还提供了在人或动物受试者中抑制MTH1活性的方法。

公开(公告)号：WO2017210134A1

公开(公告)日：2017-12-07

申请号：PCT/US2017/034806

申请日：2017-05-26

Applicant: BOARD OF REGENTS, UNIVERSITY OF TEXAS SYSTEM

Inventor： JONES, Philip ,  CZAKO, Barbara ,  CROSS, Jason ,  LEONARD, Paul ,  MSEEH, Faika ,  PARKER, Connon, Austin

IPC: A61K31/4162 ,  A61K31/4985 ,  C07D487/04

Abstract: The present invention relates to compounds which may be useful as inhibitors of PTPN11 for the treatment or prevention of cancer and other PTP-mediated diseases. Disclosed herein are new compounds and compounds based on pyrazolopyrazines and their application as pharmaceuticals for the treatment of disease.

Abstract translation: 本发明涉及可用作PTPN11抑制剂用于治疗或预防癌症和其他PTP介导的疾病的化合物。 本文公开了基于吡唑并吡嗪的新化合物和化合物及其作为用于治疗疾病的药物的应用。

公开(公告)号：WO2016033416A1

公开(公告)日：2016-03-03

申请号：PCT/US2015/047361

申请日：2015-08-28

Applicant: BOARD OF REGENTS, UNIVERSITY OF TEXAS SYSTEM ,  PALMER, Wylie ,  JONES, Philip ,  LIU, Gang ,  PETROCCHI, Alessia ,  REYNA, Naphtali ,  SUBRUMANIAN, Govindan ,  THEROFF, Jay ,  YAU, Anne

Inventor： PALMER, Wylie ,  JONES, Philip ,  LIU, Gang ,  PETROCCHI, Alessia ,  REYNA, Naphtali ,  SUBRUMANIAN, Govindan ,  THEROFF, Jay ,  YAU, Anne

IPC: A01N41/02

CPC classification number: C07D471/04 ,  A61K31/4184 ,  A61K31/4196 ,  A61K31/437 ,  A61K31/4439 ,  A61K31/454 ,  A61K31/498 ,  A61K31/5377 ,  A61K45/06 ,  A61N5/10 ,  A61N2005/1098 ,  C07D235/26 ,  C07D401/12 ,  C07D401/14 ,  C07D403/12 ,  C07D405/12 ,  C07D405/14 ,  Y02A50/411 ,  A61K2300/00

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

Abstract translation: 本文公开了可用于治疗含有溴结构域的蛋白质介导的疾病（例如癌症）的化合物和组合物，其具有式I的结构：还提供了抑制人类或动物受试者中含有溴结构域的蛋白质的活性的方法。

公开(公告)号：WO2016004404A2

公开(公告)日：2016-01-07

申请号：PCT/US2015/039134

申请日：2015-07-02

Applicant: BOARD OF REGENTS, UNIVERSITY OF TEXAS SYSTEM

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

IPC: C07D417/14 ,  A61K31/4439

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.

Abstract translation: 本文公开了用于治疗具有式I结构的GLS1介导的疾病例如癌症的化合物和组合物：还提供了抑制人或动物受试者中的GLS1活性的方法。 / p>

公开(公告)号：WO2019014618A1

公开(公告)日：2019-01-17

申请号：PCT/US2018/042128

申请日：2018-07-13

Applicant: BOARD OF REGENTS, UNIVERSITY OF TEXAS SYSTEM

Inventor： DI FRANCESCO, Maria, Emilia ,  JONES, Philip ,  CARROLL, Christopher, Lawrence ,  CROSS, Jason, Bryant ,  RAMASWAMY, Suyambu Kesava, Vijayan ,  JOHNSON, Michael, Garrett ,  LIVELY, Sarah ,  LAPOINTE, David

IPC: A61K31/505 ,  C07D413/14

Abstract: The present disclosure relates to heterocyclic compounds and methods which may be useful as inhibitors of ATR kinase for the treatment or prevention of cancer.

公开(公告)号：WO2017004359A1

公开(公告)日：2017-01-05

申请号：PCT/US2016/040364

申请日：2016-06-30

Applicant: BOARD OF REGENTS, UNIVERSITY OF TEXAS SYSTEM

Inventor： LEWIS, Richard, Thomas ,  JONES, Philip ,  PETROCCHI, Alessia ,  REYNA, Naphtali ,  HAMILTON, Matthew ,  SOTH, Michael, J. ,  HEFFERNAN, Timothy ,  HAN, Michelle ,  BURKE, Jason, P.

IPC: A61K31/501 ,  C07D417/14 ,  C07D207/00

CPC classification number: C07D417/14 ,  A61K31/4439 ,  A61K31/454 ,  A61K31/4545 ,  A61K31/501 ,  A61K45/06 ,  C07D401/14 ,  C07D403/14 ,  A61K2300/00

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

Abstract translation: 本文公开了可用于治疗具有式（I）结构的GLS1介导的疾病例如癌症的化合物和组合物。 还提供了抑制人或动物受试者的GLS1活性的方法。

公开(公告)号：WO2018044808A1

公开(公告)日：2018-03-08

申请号：PCT/US2017/048941

申请日：2017-08-28

Applicant: BOARD OF REGENTS, UNIVERSITY OF TEXAS SYSTEM

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

IPC: A61K31/44 ,  A61K31/4178 ,  C07D401/04

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).

Abstract translation: 本文公开了抑制双亮氨酸拉链（DLK）激酶（MAP3K12）的激酶活性的化合物，药物组合物以及治疗DLK介导的疾病例如由创伤引起的神经疾病的方法 中枢神经系统和外周神经系统神经元损伤（例如中风，创伤性脑损伤，脊髓损伤）或由慢性神经变性疾病（例如阿尔茨海默氏病，额颞叶痴呆，帕金森病，亨廷顿病，肌萎缩侧索硬化，脊髓小脑 共济失调，进行性核上性麻痹，路易体疾病，肯尼迪氏病和其它相关病症），神经病损伤（化学疗法诱导的周围神经病，糖尿病性神经病和相关病症）和由药理学干预（例如化学疗法 诱导认知障碍，也称为化学细胞）。

公开(公告)号：WO2016004417A1

公开(公告)日：2016-01-07

申请号：PCT/US2015/039150

申请日：2015-07-03

Applicant: BOARD OF REGENTS, UNIVERSITY OF TEXAS SYSTEM

Inventor： DI FRANCESCO, Maria, Emilia ,  JONES, Philip ,  HEFFERNAN, Timothy ,  ZHIJUN, Kang ,  SOTH, Michael, P ,  BURKE, Jason, P ,  CARROLL, Christopher Lawrence ,  MCAFOOS, Timothy ,  PALMER, Wylie, S. ,  HERRERA, Zachary ,  HAMILTON, Matthew

IPC: C07D401/06

CPC classification number: C07D401/06 ,  A61K31/00 ,  A61K31/4439 ,  A61K31/444 ,  A61K31/4545 ,  A61K31/501 ,  A61K31/513 ,  A61K31/519 ,  A61K31/5377 ,  A61K31/541 ,  A61K45/06 ,  C07D401/14 ,  C07D403/06 ,  C07D403/14 ,  C07D405/14 ,  C07D409/14 ,  C07D417/06 ,  C07D417/14 ,  C07D487/04

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.

Abstract translation: 本文公开了可用于治疗GLS1介导的疾病（例如癌症）的化合物和组合物，其具有式I的结构：还提供了人或动物受试者的抑制GLS1活性的方法。

公开(公告)号：WO2016004413A3

公开(公告)日：2016-01-07

申请号：PCT/US2015/039143

申请日：2015-07-02

Applicant: BOARD OF REGENTS, UNIVERSITY OF TEXAS SYSTEM

Inventor： DI FRANCESCO, Maria, Emilia ,  JONES, Philip ,  HEFFERNAN, Timothy ,  SOTH, Michael, P. ,  LE, Kang ,  CARROLL, Christopher, Lawrence ,  MCAFOOS, Timothy ,  BURKE, Jason, P. ,  THEROFF, Jay ,  ZANG, Zhijun

IPC: C07D487/04 ,  A61K31/5025

Abstract: Disclosed herein are compounds and compositions useful in the treatment of GLS I mediated diseases, such as cancer, having the structure of Formula I. Methods of inhibition GLS I activity in a human or animal subject are also provided. Accordingly, the inventors herein disclose new compositions and methods for inhibiting glutaminase activity.

公开(公告)号：WO2015130790A2

公开(公告)日：2015-09-03

申请号：PCT/US2015/017533

申请日：2015-02-25

Applicant: BOARD OF REGENTS, UNIVERSITY OF TEXAS SYSTEM ,  JONES, Philip ,  DI FRANCESCO, Maria, Emilia ,  MCAFOOS, Timothy

Inventor： JONES, Philip ,  DI FRANCESCO, Maria, Emilia ,  MCAFOOS, Timothy

IPC: C07D413/14

CPC classification number: A61K31/454 ,  A61K31/4245 ,  A61K31/4439 ,  A61K31/4545 ,  A61K31/4709 ,  A61K31/496 ,  A61K31/5377 ,  A61K31/541 ,  C07D413/14

Abstract: The present disclosure relates to salts of heterocyclic compounds and methods that inhibit HIF pathway activity. The compounds are designed to treat or prevent cancer and other hypoxia-mediated diseases.

Abstract translation: 本公开涉及杂环化合物的盐和抑制HIF通路活性的方法。 该化合物被设计用于治疗或预防癌症和其他缺氧介导的疾病。