AU2021286831A1 - 1-(5-(2-cyanopyridin-4-yl)oxazole-2-carbonyl)-4- methylhexahydropyrrolo[3,4-b]pyrrole-5(1H)-carbonitrile as USP30 inhibitor for use in the treatment of mitochondrial dysfunction, cancer and fibrosis - Google Patents

1-(5-(2-cyanopyridin-4-yl)oxazole-2-carbonyl)-4- methylhexahydropyrrolo[3,4-b]pyrrole-5(1H)-carbonitrile as USP30 inhibitor for use in the treatment of mitochondrial dysfunction, cancer and fibrosis Download PDF

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Publication number
AU2021286831A1
AU2021286831A1 AU2021286831A AU2021286831A AU2021286831A1 AU 2021286831 A1 AU2021286831 A1 AU 2021286831A1 AU 2021286831 A AU2021286831 A AU 2021286831A AU 2021286831 A AU2021286831 A AU 2021286831A AU 2021286831 A1 AU2021286831 A1 AU 2021286831A1
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Prior art keywords
disease
compound
fibrosis
deficiency
pyrrole
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Pending
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AU2021286831A
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Inventor
Mark Ian Kemp
Christopher Andrew Luckhurst
Martin Lee Stockley
Paul William Thompson
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Mission Therapeutics Ltd
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Mission Therapeutics Ltd
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Priority claimed from GBGB2008598.1A external-priority patent/GB202008598D0/en
Priority claimed from GBGB2016758.1A external-priority patent/GB202016758D0/en
Application filed by Mission Therapeutics Ltd filed Critical Mission Therapeutics Ltd
Publication of AU2021286831A1 publication Critical patent/AU2021286831A1/en
Pending legal-status Critical Current

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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/02—Heterocyclic 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
    • C07D487/04—Ortho-condensed systems
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/4427—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
    • A61K31/4439—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. omeprazole
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/16—Drugs for disorders of the alimentary tract or the digestive system for liver or gallbladder disorders, e.g. hepatoprotective agents, cholagogues, litholytics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00—Drugs for disorders of the respiratory system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P13/00—Drugs for disorders of the urinary system
    • A61P13/12—Drugs for disorders of the urinary system of the kidneys
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/28—Drugs 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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00—Drugs for disorders of the metabolism
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00—Drugs for disorders of the metabolism
    • A61P3/08—Drugs for disorders of the metabolism for glucose homeostasis
    • A61P3/10—Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A61P9/10—Drugs 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D417/00—Heterocyclic 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
    • C07D417/02—Heterocyclic 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
    • C07D417/12—Heterocyclic 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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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Biomedical Technology (AREA)
  • Neurosurgery (AREA)
  • Neurology (AREA)
  • Diabetes (AREA)
  • Psychiatry (AREA)
  • Hospice & Palliative Care (AREA)
  • Hematology (AREA)
  • Obesity (AREA)
  • Cardiology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Urology & Nephrology (AREA)
  • Pulmonology (AREA)
  • Vascular Medicine (AREA)
  • Emergency Medicine (AREA)
  • Endocrinology (AREA)
  • Gastroenterology & Hepatology (AREA)
  • Epidemiology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
AU2021286831A 2020-06-08 2021-06-07 1-(5-(2-cyanopyridin-4-yl)oxazole-2-carbonyl)-4- methylhexahydropyrrolo[3,4-b]pyrrole-5(1H)-carbonitrile as USP30 inhibitor for use in the treatment of mitochondrial dysfunction, cancer and fibrosis Pending AU2021286831A1 (en)

Applications Claiming Priority (5)

Application Number Priority Date Filing Date Title
GBGB2008598.1A GB202008598D0 (en) 2020-06-08 2020-06-08 Novel compounds
GB2008598.1 2020-06-08
GBGB2016758.1A GB202016758D0 (en) 2020-10-22 2020-10-22 Novel compounds
GB2016758.1 2020-10-22
PCT/EP2021/065112 WO2021249909A1 (en) 2020-06-08 2021-06-07 1-(5-(2-cyanopyridin-4-yl)oxazole-2-carbonyl)-4-methylhexahydropyrrolo[3,4-b]pyr role-5(1h)-carbonitrile as usp30 inhibitor for use in the treatment of mitochondrial dysfunction, cancer and fibrosis

Publications (1)

Publication Number Publication Date
AU2021286831A1 true AU2021286831A1 (en) 2023-02-02

Family

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Family Applications (1)

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AU2021286831A Pending AU2021286831A1 (en) 2020-06-08 2021-06-07 1-(5-(2-cyanopyridin-4-yl)oxazole-2-carbonyl)-4- methylhexahydropyrrolo[3,4-b]pyrrole-5(1H)-carbonitrile as USP30 inhibitor for use in the treatment of mitochondrial dysfunction, cancer and fibrosis

Country Status (25)

Country Link
US (2) US12655152B2 (enExample)
EP (1) EP4161929B1 (enExample)
JP (1) JP2023528087A (enExample)
KR (1) KR20230022215A (enExample)
CN (1) CN115836073B (enExample)
AU (1) AU2021286831A1 (enExample)
BR (1) BR112022024794A2 (enExample)
CA (1) CA3186148A1 (enExample)
CO (1) CO2022017233A2 (enExample)
DK (1) DK4161929T3 (enExample)
ES (1) ES3040433T3 (enExample)
FI (1) FI4161929T3 (enExample)
HR (1) HRP20250891T1 (enExample)
HU (1) HUE072598T2 (enExample)
IL (1) IL298785B2 (enExample)
LT (1) LT4161929T (enExample)
MD (1) MD4161929T2 (enExample)
MX (1) MX2022015608A (enExample)
PL (1) PL4161929T3 (enExample)
PT (1) PT4161929T (enExample)
RS (1) RS67140B1 (enExample)
SI (1) SI4161929T1 (enExample)
SM (1) SMT202500343T1 (enExample)
WO (1) WO2021249909A1 (enExample)
ZA (1) ZA202213877B (enExample)

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WO2023099561A1 (en) 2021-12-01 2023-06-08 Mission Therapeutics Limited Substituted n-cyanopyrrolidines with activity as usp30 inhibitors
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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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GB202500610D0 (en) 2025-01-16 2025-03-05 Mission Therapeutics Ltd Novel compounds

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CN115836073B (zh) 2024-08-27
ZA202213877B (en) 2024-07-31
KR20230022215A (ko) 2023-02-14
DK4161929T3 (da) 2025-08-18
IL298785B2 (en) 2026-03-01
FI4161929T3 (fi) 2025-07-30
CO2022017233A2 (es) 2023-03-07
MD4161929T2 (ro) 2025-10-31
US20230312580A1 (en) 2023-10-05
CN115836073A (zh) 2023-03-21
JP2023528087A (ja) 2023-07-03
IL298785A (en) 2023-02-01
HUE072598T2 (hu) 2025-11-28
RS67140B1 (sr) 2025-09-30
PL4161929T3 (pl) 2026-01-05
EP4161929B1 (en) 2025-04-30
HRP20250891T1 (hr) 2025-09-26
IL298785B1 (en) 2025-11-01
PT4161929T (pt) 2025-08-05
ES3040433T3 (en) 2025-10-30
WO2021249909A1 (en) 2021-12-16
US12655152B2 (en) 2026-06-16
SMT202500343T1 (it) 2025-11-10
US20260138984A1 (en) 2026-05-21
SI4161929T1 (sl) 2025-10-30
LT4161929T (lt) 2025-09-25
CA3186148A1 (en) 2021-12-16
MX2022015608A (es) 2023-03-03
BR112022024794A2 (pt) 2022-12-27
EP4161929A1 (en) 2023-04-12

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DA3 Amendments made section 104

Free format text: THE NATURE OF THE AMENDMENT IS: AMEND THE INVENTION TITLE TO READ 1-(5-(2-CYANOPYRIDIN-4-YL)OXAZOLE-2-CARBONYL)-4- METHYLHEXAHYDROPYRROLO(3,4-B)PYRROLE-5(1H)-CARBONITRILE AS USP30 INHIBITOR FOR USE IN THE TREATMENT OF MITOCHONDRIAL DYSFUNCTION, CANCER AND FIBROSIS