公开(公告)号：WO2016004418A1

公开(公告)日：2016-01-07

申请号：PCT/US2015/039153

申请日：2015-07-03

Applicant: BOARD OF REGENTS, UNIVERSITY OF TEXAS SYSTEM

Inventor： HEFFERNAN, Timothy ,  TONIATTI, Carlo ,  KOVACS, Jeffrey ,  GIULIANI, Virginia ,  SPENCE, Nakia ,  DI FRANCESCO, Maria, Emilia ,  BRISTOW, Christopher, A.

IPC: A61P39/06

CPC classification number: A61K31/501 ,  A61K45/06 ,  A61K2300/00

Abstract: Disclosed herein are methods of treating a subject having an altered NRF2/KEAP1 pathway, and compounds and compositions useful in such treatment. Also disclosed herein are methods of evaluating whether to administer a compound that inhibits glutathione production or a glutaminase inhibitor to a subject.

Abstract translation: 本文公开了治疗具有改变的NRF2 / KEAP1途径的受试者的方法，以及可用于这种治疗的化合物和组合物。 本文还公开了评估是否向受试者施用抑制谷胱甘肽产生的化合物或谷氨酰胺酶抑制剂的方法。

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：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：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.