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    1-cyano-pyrrolidine derivatives as DUB inhibitors
    2.
    发明授权
    1-cyano-pyrrolidine derivatives as DUB inhibitors 有权

    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.

    4,6 DIHYDROPYRROLO [3,4-C] PYRAZOLE-5 (1H)-CARBONITRILE DERIVATES FOR TREATING CANCER
    4.
    发明申请
    4,6 DIHYDROPYRROLO [3,4-C] PYRAZOLE-5 (1H)-CARBONITRILE DERIVATES FOR TREATING CANCER 有权

    公开(公告)号：US20210221813A1

    公开(公告)日：2021-07-22

    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 ,  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.

    SUBSTITUTED CYANOPYRROLIDINES WITH ACTIVITY AS DUB INHIBITORS
    9.
    发明申请
    SUBSTITUTED CYANOPYRROLIDINES WITH ACTIVITY AS DUB INHIBITORS 审中-公开

    公开(公告)号：US20200172519A1

    公开(公告)日：2020-06-04

    申请号：US16615709

    申请日：2018-06-19

    Applicant: MISSION THERAPEUTICS LIMITED

    Inventor： Martin Lee STOCKLEY ,  Mark Ian KEMP

    IPC: C07D403/12

    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).

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