Abstract: The invention relates to novel compounds of formula I which are inhibitors of deubiquitylating enzymes (DUBs) and/or desumoylating enzymes. In particular, the invention relates to the inhibition of ubiquitin C-terminal hydrolase 7 or ubiquitin specific peptidase 7 (USP7). The invention further relates to methods for the preparation of these compounds and to their use in the treatment of cancer.
Type:
Grant
Filed:
March 17, 2017
Date of Patent:
June 16, 2020
Assignee:
MISSION THERAPEUTICS LIMITED
Inventors:
Karl Richard Gibson, Alison Jones, Mark Ian Kemp, Andrew Madin, Martin Lee Stockley, Gavin Alistair Whitlock, Michael D Woodrow, Keith Allan Menear
Abstract: Substituted Cyanopyrrolidines with Activity as DUB Inhibitors The present invention relates to a class of substituted-cyanopyrrolidines of formula (Ia), (Ib), and (Ic), with activity as inhibitors of deubiquitilating enzymes, in particular, ubiquitin C-terminal hydrolase 30 or ubiquitin specific peptidase 30 (USP30), having utility in a variety of therapeutic areas including cancer and conditions involving mitochondrial dysfunction (Ia).
Abstract: The present invention relates to novel compounds and method for the manufacture of inhibitors of deubiquitylating enzymes (DUBs). In particular, the invention relates to the inhibition of ubiquitin C-terminal hydrolase L1 (UCHL1) and ubiquitin C-terminal hydrolase 30 or ubiquitin specific peptidase 30 (USP30). The invention further relates to the use of DUB inhibitors in the treatment of cancer and conditions involving mitochondrial dysfunction. Compounds of the invention include compounds having the formula (I) or a pharmaceutically acceptable salt thereof, wherein R1, R2, R3, R4, R5, R6, R7, R8 and R9 are as defined herein.
Type:
Grant
Filed:
July 14, 2016
Date of Patent:
June 2, 2020
Assignee:
MISSION THERAPEUTICS LIMITED
Inventors:
Mark Kemp, Martin Stockley, Alison Jones
Abstract: The present invention relates to novel compounds and methods for the manufacture of inhibitors of deubiquitylating enzymes (DUBs). In particular, the invention relates to the inhibition of Cezanne 1. The invention further relates to the use of DUB inhibitors in the treatment of cancer.
Type:
Grant
Filed:
March 2, 2017
Date of Patent:
May 19, 2020
Assignee:
MISSION THERAPEUTICS LIMITED
Inventors:
Mark Ian Kemp, Martin Lee Stockley, Michael David Woodrow, Alison Jones
Abstract: The present invention relates to novel compounds of formula (I) and methods for the manufacture of inhibitors of deubiquitylating enzymes (DUBs). In particular, the invention relates to the inhibition of ubiquitin C-terminal hydrolase 30 or ubiquitin specific peptidase 30 (USP30). The invention further relates to the use of DUB inhibitors in the treatment of conditions involving mitochondrial dysfunction and in the treatment of cancer.
Type:
Grant
Filed:
February 16, 2017
Date of Patent:
May 5, 2020
Assignee:
MISSION THERAPEUTICS LIMITED
Inventors:
Karl Richard Gibson, Alison Jones, Mark Ian Kemp, Andrew Madin, Martin Lee Stockley, Gavin Alistair Whitlock, Michael D. Woodrow
Abstract: The present invention relates to novel compounds and methods for the manufacture of inhibitors of deubiquitylating enzymes (DUBs). In particular, the invention relates to the inhibition of Cezanne 1 and ubiquitin C-terminal hydrolase 30 or Ubiquitin Specific Peptidase 30 (USP30). The invention further relates to the use of DUB inhibitors in the treatment of cancer. Compounds of the invention include compounds having the formula (I): pharmaceutically acceptable salt thereof, wherein R1a, R1b, R1c, R1d, R1e, R1f and A are as defined herein.
Abstract: The present invention relates to materials and methods for high throughput monitoring of target engagement of isopeptidases, such as deubiquitylating enzymes by, inter alia, small molecule inhibitors. In particular the invention relates to development of high throughput assays to measure isopeptidase activity in biological samples, such as cells, animal tissues, animal tumours, human tissue or patient-derived biopsies.
Type:
Grant
Filed:
June 15, 2015
Date of Patent:
January 7, 2020
Assignee:
Mission Therapeutics Limited
Inventors:
Xavier Jacq, Quentin Gueranger, Jeanine Ann Harrigan
Abstract: The present invention relates to novel compounds and methods for the manufacture of inhibitors of deubiquitylating enzymes (DUBs). In particular, the invention relates to the inhibition of ubiquitin C-terminal hydrolase L1 (UCHL1). The invention further relates to the use of DUB inhibitors in the treatment of cancer and other indications. Compounds of the invention include compounds having the formula (I) or a pharmaceutically acceptable salt thereof, wherein R1 to R8 are as defined herein.
Type:
Grant
Filed:
February 12, 2018
Date of Patent:
August 27, 2019
Assignee:
MISSION THERAPEUTICS LIMITED
Inventors:
Alison Jones, Mark Ian Kemp, Martin Lee Stockley, Karl Gibson, Gavin Alistair Whitlock, Andrew Madin
Abstract: The present invention relates to novel compounds and method for the manufacture of inhibitors of deubiquitylating enzymes (DUBs). In particular, the invention relates to the inhibition of ubiquitin C-terminal hydrolase 30 (USP30). The invention further relates to the use of DUB inhibitors in the treatment of conditions involving mitochondrial dysfunction and cancer. Compounds of the invention include compounds having the formula (II) or a pharmaceutically acceptable salt thereof, wherein R1, R2, R3, R4, R5, R8, R9, R10, R12, Z, Y and m are as defined herein.
Type:
Grant
Filed:
March 24, 2016
Date of Patent:
July 9, 2019
Assignee:
Missions Therapeutics Limited
Inventors:
Alison Jones, Mark Kemp, Martin Stockley, Karl Gibson, Gavin Whitlock