JP7084918B2 - Usp30の阻害剤としての活性を有するシアノピロリジン誘導体 - Google Patents

Usp30の阻害剤としての活性を有するシアノピロリジン誘導体 Download PDF

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JP7084918B2
JP7084918B2 JP2019517227A JP2019517227A JP7084918B2 JP 7084918 B2 JP7084918 B2 JP 7084918B2 JP 2019517227 A JP2019517227 A JP 2019517227A JP 2019517227 A JP2019517227 A JP 2019517227A JP 7084918 B2 JP7084918 B2 JP 7084918B2
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alkyl
carbonitrile
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hydrogen
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リー ストックリー マーティン
イアン ケンプ マーク
マディン アンドリュー
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ミッション セラピューティクス リミティド
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    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D487/00Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/02Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
    • C07D487/04Ortho-condensed systems
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P21/00Drugs for disorders of the muscular or neuromuscular system
    • AHUMAN NECESSITIES
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    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P21/00Drugs for disorders of the muscular or neuromuscular system
    • A61P21/02Muscle relaxants, e.g. for tetanus or cramps
    • AHUMAN NECESSITIES
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    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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    • A61P25/00Drugs for disorders of the nervous system
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    • A61P25/16Anti-Parkinson drugs
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    • A61P25/18Antipsychotics, i.e. neuroleptics; Drugs for mania or schizophrenia
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
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    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/28Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
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    • A61P27/02Ophthalmic agents
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    • A61P3/00Drugs for disorders of the metabolism
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    • A61P3/00Drugs for disorders of the metabolism
    • A61P3/08Drugs for disorders of the metabolism for glucose homeostasis
    • A61P3/10Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • A61P35/02Antineoplastic agents specific for leukemia
    • AHUMAN NECESSITIES
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    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system
    • A61P9/10Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
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    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D401/00Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/02Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
    • C07D401/12Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a chain containing hetero atoms as chain links
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D403/00Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/02Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
    • C07D403/12Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings linked by a chain containing hetero atoms as chain links
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    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D417/00Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
    • C07D417/02Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings
    • C07D417/12Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings linked by a chain containing hetero atoms as chain links
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    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D471/00Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
    • C07D471/02Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
    • C07D471/04Ortho-condensed systems
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D498/00Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D498/02Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms in which the condensed system contains two hetero rings
    • C07D498/04Ortho-condensed systems

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  • Health & Medical Sciences (AREA)
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  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
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  • Biomedical Technology (AREA)
  • Diabetes (AREA)
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  • Urology & Nephrology (AREA)
  • Vascular Medicine (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
JP2019517227A 2016-09-30 2017-10-02 Usp30の阻害剤としての活性を有するシアノピロリジン誘導体 Active JP7084918B2 (ja)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
GB1616627.4 2016-09-30
GBGB1616627.4A GB201616627D0 (en) 2016-09-30 2016-09-30 Novel compounds
PCT/GB2017/052949 WO2018060742A1 (en) 2016-09-30 2017-10-02 Cyanopyrrolidine derivatives with activity as inhibitors of usp30

Publications (3)

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JP2019532950A JP2019532950A (ja) 2019-11-14
JP2019532950A5 JP2019532950A5 (https=) 2020-11-12
JP7084918B2 true JP7084918B2 (ja) 2022-06-15

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JP2019517227A Active JP7084918B2 (ja) 2016-09-30 2017-10-02 Usp30の阻害剤としての活性を有するシアノピロリジン誘導体

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US (1) US11084821B2 (https=)
EP (1) EP3519412B1 (https=)
JP (1) JP7084918B2 (https=)
CN (1) CN109790169B (https=)
GB (1) GB201616627D0 (https=)
MA (1) MA46339A (https=)
WO (1) WO2018060742A1 (https=)

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GB201522768D0 (en) 2015-12-23 2016-02-03 Mission Therapeutics Ltd Novel compounds
GB201602854D0 (en) 2016-02-18 2016-04-06 Mission Therapeutics Ltd Novel compounds
GB201603779D0 (en) 2016-03-04 2016-04-20 Mission Therapeutics Ltd Novel compounds
GB201604638D0 (en) 2016-03-18 2016-05-04 Mission Therapeutics Ltd Novel compounds
GB201604647D0 (en) 2016-03-18 2016-05-04 Mission Therapeutics Ltd Novel compounds
JP6959252B2 (ja) 2016-03-24 2021-11-02 ミッション セラピューティクス リミティド Dub阻害剤としての1−シアノピロリジン誘導体
ES2850349T3 (es) 2016-09-27 2021-08-27 Mission Therapeutics Ltd Derivados de cianopirrolidina con actividad como inhibidores de USP30
GB201616511D0 (en) 2016-09-29 2016-11-16 Mission Therapeutics Limited Novel compounds
TWI771327B (zh) 2016-10-05 2022-07-21 英商使命醫療公司 新穎化合物
GB201708652D0 (en) 2017-05-31 2017-07-12 Mission Therapeutics Ltd Novel compounds and uses
JP7208931B2 (ja) 2017-06-20 2023-01-19 ミッション セラピューティクス リミティド Dub阻害剤としての活性をもつ置換シアノピロリジン類
BR112020003725A2 (pt) 2017-10-06 2020-11-03 Forma Therapeutics, Inc. inibição da peptidase 30 específica de ubiquitina
EA202092001A1 (ru) * 2018-03-27 2021-01-29 ПиТиСи ТЕРАПЬЮТИКС, ИНК. Соединения для лечения болезни гентингтона
JP7449242B2 (ja) * 2018-05-17 2024-03-13 フォーマ セラピューティクス,インコーポレイテッド ユビキチン特異的ペプチダーゼ30(usp30)阻害剤として有用な縮合二環化合物
JP7434285B2 (ja) * 2018-08-14 2024-02-20 アムジエン・インコーポレーテツド N-シアノ-7-アザノルボルナン誘導体及びその使用
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GB201905371D0 (en) 2019-04-16 2019-05-29 Mission Therapeutics Ltd Novel compounds
GB201905375D0 (en) 2019-04-16 2019-05-29 Mission Therapeutics Ltd Novel compounds
GB201912674D0 (en) 2019-09-04 2019-10-16 Mission Therapeutics Ltd Novel compounds
WO2021204856A1 (en) 2020-04-08 2021-10-14 Mission Therapeutics Limited N-cyanopyrrolidines with activity as usp30 inhibitors
IL298526A (en) 2020-05-28 2023-01-01 Mission Therapeutics Ltd N-(1-cyano-pyrrolidin-3-yl)-5-(3-(trifluoromethyl)phenyl)oxazole-2-carboxamide derivatives and the corresponding oxadiazole derivatives as usp30 inhibitors for the treatment of mitochondrial dysfunction
BR112022019722A2 (pt) 2020-06-04 2022-12-20 Mission Therapeutics Ltd N-cianopirrolidinas com atividade como inibidores de usp30
DK4161929T3 (da) 2020-06-08 2025-08-18 Mission Therapeutics Ltd 1-(5-(2-cyanopyridin-4-yl)oxazol-2-carbonyl)-4-methylhexahydropyrrolo[3,4-b]pyrrol-5(1h)-carbonitril som usp30-hæmmer til anvendelse i behandling af mitokondriedysfunktion, cancer og fibrose
GB202016800D0 (en) 2020-10-22 2020-12-09 Mission Therapeutics Ltd Novel compounds
CN118834147A (zh) * 2021-09-22 2024-10-25 杭州天玑济世生物科技有限公司 一类具有萘胺结构的小分子化合物及其应用
US20250034122A1 (en) 2021-12-01 2025-01-30 Mission Therapeutics Limited Substituted n-cyanopyrrolidines with activity as usp30 inhibitors
CN114877158B (zh) * 2022-04-15 2023-06-23 四川轻化工大学 一种非开挖原位修复管道用内衬管表面改性方法
GB202408928D0 (en) 2024-06-21 2024-08-07 Mission Therapeutics Ltd Novel compounds
GB202411060D0 (en) 2024-07-29 2024-09-11 Mission Therapeutics Ltd Novel compounds

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ES2850349T3 (es) 2016-09-27 2021-08-27 Mission Therapeutics Ltd Derivados de cianopirrolidina con actividad como inhibidores de USP30
GB201616511D0 (en) 2016-09-29 2016-11-16 Mission Therapeutics Limited Novel compounds
TWI771327B (zh) 2016-10-05 2022-07-21 英商使命醫療公司 新穎化合物
GB201708652D0 (en) 2017-05-31 2017-07-12 Mission Therapeutics Ltd Novel compounds and uses
JP7208931B2 (ja) 2017-06-20 2023-01-19 ミッション セラピューティクス リミティド Dub阻害剤としての活性をもつ置換シアノピロリジン類

Patent Citations (7)

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Publication number Priority date Publication date Assignee Title
WO2001077073A1 (en) 2000-04-06 2001-10-18 Merck Frosst Canada & Co. Cathepsin cysteine protease inhibitors
WO2009129370A1 (en) 2008-04-18 2009-10-22 Glaxo Group Limited Cathepsin c inhibitors
WO2014041111A1 (en) 2012-09-17 2014-03-20 F. Hoffmann-La Roche Ag Usp30 inhibitors and methods of use
WO2015054555A1 (en) 2013-10-10 2015-04-16 The Regents Of The University Of Michigan Deubiquitinase inhibitors and methods for use of the same
WO2016004272A1 (en) 2014-07-02 2016-01-07 Pharmacyclics Llc Inhibitors of bruton's tyrosine kinase
WO2016046530A1 (en) 2014-09-23 2016-03-31 Mission Therapeutics Ltd Novel compounds
WO2016065226A1 (en) 2014-10-24 2016-04-28 Bristol-Myers Squibb Company Indole carboxamides compounds useful as kinase inhobitors

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WO2018060742A1 (en) 2018-04-05
CN109790169B (zh) 2022-03-29
US11084821B2 (en) 2021-08-10
EP3519412B1 (en) 2021-12-01
US20200199126A1 (en) 2020-06-25
MA46339A (fr) 2019-08-07
JP2019532950A (ja) 2019-11-14
CN109790169A (zh) 2019-05-21
EP3519412A1 (en) 2019-08-07
GB201616627D0 (en) 2016-11-16

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