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公开(公告)号:US11306096B2
公开(公告)日:2022-04-19
申请号:US16080229
申请日:2017-03-17
Applicant: MISSION THERAPEUTICS LIMITED
Inventor: Alison Jones , Mark Ian Kemp , Martin Lee Stockley , Michael David Woodrow
IPC: C07D487/04 , A61K31/4162 , A61P35/00 , C07D519/00
Abstract: The present invention relates to novel compounds and methods for the manufacture of 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 the use of DUB or desumoylating inhibitors in the treatment of cancer. Described herein are compounds of formula (I) or a pharmaceutically acceptable salt thereof, wherein R1a, R1b, R1c and R1d each independently represent hydrogen, optionally substituted C1-C6 alkyl or R1a and R1b together form an optionally substituted C3-C6 cycloalkyl ring, or R1c and R1d together form an optionally substituted C3-C6 cycloalkyl ring; A is a 5 membered nitrogen-containing aromatic ring and is substituted with at least one optionally substituted 5 to 10 membered monocyclic or bicyclic heteroaryl or aryl ring attached through an optional linker.
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公开(公告)号:US11352339B2
公开(公告)日:2022-06-07
申请号:US16087515
申请日:2017-03-23
Applicant: MISSION THERAPEUTICS LIMITED
Inventor: Alison Jones , Mark Ian Kemp , Martin Lee Stockley , Michael David Woodrow
IPC: C07D401/14 , C07D403/04 , C07D403/14 , C07D413/04 , C07D413/14 , C07D417/14
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 30 or ubiquitin specific peptidase 30 (USP30). The novel compounds have formula (I): (Formula (I)) or are pharmaceutically acceptable salts thereof, wherein: R1a, R1b, R1c, R1d, R1e and R1f each independently represent hydrogen, optionally substituted C1-C6 alkyl or optionally substituted C3-C4 cycloalkyl, or R1b and R1c together form an optionally substituted C3-C6 cycloalkyl ring, or R1d and R1e together form an optionally substituted C3-C6 cycloalkyl ring; R2 represents hydrogen or optionally substituted C1-C6 alkyl; A represents an optionally further substituted 5 to 10 membered monocyclic or bicyclic heteroaryl, heterocyclyl or aryl ring; L represents a covalent bond or linker; B represents an optionally substituted 3 to 10 membered monocyclic or bicyclic heterocyclyl, heteroaryl, cycloalkyl or aryl ring; and when -A-L-B is at position x attachment to A is via a carbon ring atom of A, and either: A cannot be triazolopyridazinyl, triazolopyridinyl, imidazotriazinyl, imidazopyrazinyl or pyrrolopyrimidinyl; or B cannot be substituted with phenoxyl; or B cannot be cyclopentyl when L is an oxygen atom.
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公开(公告)号:US11236092B2
公开(公告)日:2022-02-01
申请号:US16843408
申请日:2020-04-08
Applicant: MISSION THERAPEUTICS LIMITED
Inventor: Mark Ian Kemp , Martin Lee Stockley , Michael David Woodrow , Alison Jones
IPC: C07D471/10 , C07D471/20 , C07D498/20 , C07D487/10
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.
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公开(公告)号:US10654853B2
公开(公告)日:2020-05-19
申请号:US16078518
申请日:2017-03-02
Applicant: MISSION THERAPEUTICS LIMITED
Inventor: Mark Ian Kemp , Martin Lee Stockley , Michael David Woodrow , Alison Jones
IPC: C07D471/10 , C07D471/20 , C07D498/20 , C07D487/10
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.
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公开(公告)号:US11945797B2
公开(公告)日:2024-04-02
申请号:US17674943
申请日:2022-02-18
Applicant: MISSION THERAPEUTICS LIMITED
Inventor: Alison Jones , Mark Ian Kemp , Martin Lee Stockley , Michael David Woodrow
IPC: C07D401/14 , C07D403/04 , C07D403/14 , C07D413/04 , C07D413/14 , C07D417/14
CPC classification number: C07D401/14 , C07D403/04 , C07D403/14 , C07D413/04 , C07D413/14 , C07D417/14
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 30 or ubiquitin specific peptidase 30 (USP30). The novel compounds have formula (I): (Formula (I)) or are pharmaceutically acceptable salts thereof, wherein: R1a, R1b, R1c, R1d, R1e and R1f each independently represent hydrogen, optionally substituted C1-C6 alkyl or optionally substituted C3-C4 cycloalkyl, or R1b and R1c together form an optionally substituted C3-C6 cycloalkyl ring, or R1d and R1e together form an optionally substituted C3-C6 cycloalkyl ring; R2 represents hydrogen or optionally substituted C1-C6 alkyl; A represents an optionally further substituted 5 to 10 membered monocyclic or bicyclic heteroaryl, heterocyclyl or aryl ring; L represents a covalent bond or linker; B represents an optionally substituted 3 to 10 membered monocyclic or bicyclic heterocyclyl, heteroaryl, cycloalkyl or aryl ring; and when -A-L-B is at position x attachment to A is via a carbon ring atom of A, and either: A cannot be triazolopyridazinyl, triazolopyridinyl, imidazotriazinyl, imidazopyrazinyl or pyrrolopyrimidinyl; or B cannot be substituted with phenoxyl; or B cannot be cyclopentyl when L is an oxygen atom.
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公开(公告)号:US11414402B2
公开(公告)日:2022-08-16
申请号:US16615040
申请日:2018-05-30
Applicant: MISSION THERAPEUTICS LIMITED
Inventor: Martin Lee Stockley , Mark Ian Kemp , Andrew Madin , Michael David Woodrow
IPC: C07D487/04 , C07D403/12 , C07D207/14 , C07D401/12 , C07D401/14 , C07D403/14 , C07D498/04
Abstract: The present invention relates to a class of sulfonamide-substituted cyanopyrrolidines of Formula (Ia) and (Ib) with activity as inhibitors of deubiquitilating enzymes, in particular, ubiquitin C-terminal hydrolase L1 (UCHL1) and 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: (Formulae (Ia), (Ib)).
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公开(公告)号:US11014912B2
公开(公告)日:2021-05-25
申请号:US16334836
申请日:2017-09-27
Applicant: MISSION THERAPEUTICS LIMITED
Inventor: Martin Lee Stockley , Mark Ian Kemp , Andrew Madin , Michael David Woodrow , Alison Jones
IPC: C07D403/14 , C07D403/06 , C07D413/12 , C07D471/04
Abstract: The present invention relates to substituted-cyanopyrrolidines of Formula (I) 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. (I)
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公开(公告)号:US10590075B2
公开(公告)日:2020-03-17
申请号:US16060299
申请日:2016-12-21
Applicant: Mission Therapeutics Limited
Inventor: Mark Ian Kemp , Michael David Woodrow
IPC: C07D207/16 , A61K31/4025 , C07D403/12 , C07D413/14 , C07D413/12 , C07D417/12 , C07D417/14 , C07D207/10 , A61P35/00 , C07D401/12
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.
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