KR102462240B1 - 효소 억제를 위한 에폭시케톤 화합물 - Google Patents

효소 억제를 위한 에폭시케톤 화합물 Download PDF

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KR102462240B1
KR102462240B1 KR1020217022768A KR20217022768A KR102462240B1 KR 102462240 B1 KR102462240 B1 KR 102462240B1 KR 1020217022768 A KR1020217022768 A KR 1020217022768A KR 20217022768 A KR20217022768 A KR 20217022768A KR 102462240 B1 KR102462240 B1 KR 102462240B1
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mmol
pharmaceutical composition
compound
proteasome
disease
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KR20210093378A (ko
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진푸 양
샤오칭 미쉘 판
지엔 제임스 천
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센트랙스 인터내셔널, 아이엔씨.
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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07K—PEPTIDES
    • C07K5/00—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
    • C07K5/04—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing only normal peptide links
    • C07K5/06—Dipeptides
    • C07K5/06008—Dipeptides with the first amino acid being neutral
    • C07K5/06078—Dipeptides with the first amino acid being neutral and aromatic or cycloaliphatic
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K38/00—Medicinal preparations containing peptides
    • 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
    • A61P17/00—Drugs for dermatological disorders
    • A61P17/14—Drugs for dermatological disorders for baldness or alopecia
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00—Drugs for skeletal disorders
    • A61P19/08—Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
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    • A61P21/00—Drugs for disorders of the muscular or neuromuscular 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
    • A61P27/00—Drugs for disorders of the senses
    • A61P27/02—Ophthalmic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/12—Antivirals
    • A61P31/14—Antivirals for RNA viruses
    • A61P31/18—Antivirals for RNA viruses for HIV
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P33/00—Antiparasitic agents
    • 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
    • A61P37/00—Drugs for immunological or allergic disorders
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00—Drugs for immunological or allergic disorders
    • A61P37/02—Immunomodulators
    • A61P37/06—Immunosuppressants, e.g. drugs for graft rejection
    • 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
    • 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
    • C07K—PEPTIDES
    • C07K5/00—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
    • C07K5/02—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing at least one abnormal peptide link
    • C07K5/0202—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing at least one abnormal peptide link containing the structure -NH-X-X-C(=0)-, X being an optionally substituted carbon atom or a heteroatom, e.g. beta-amino acids
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07K—PEPTIDES
    • C07K5/00—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
    • C07K5/04—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing only normal peptide links
    • C07K5/08—Tripeptides
    • C07K5/0802—Tripeptides with the first amino acid being neutral
    • C07K5/0804—Tripeptides with the first amino acid being neutral and aliphatic
    • C07K5/0806—Tripeptides with the first amino acid being neutral and aliphatic the side chain containing 0 or 1 carbon atoms, i.e. Gly, Ala
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07K—PEPTIDES
    • C07K5/00—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
    • C07K5/04—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing only normal peptide links
    • C07K5/08—Tripeptides
    • C07K5/0821—Tripeptides with the first amino acid being heterocyclic, e.g. His, Pro, Trp

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • General Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Animal Behavior & Ethology (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Proteomics, Peptides & Aminoacids (AREA)
  • Molecular Biology (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Genetics & Genomics (AREA)
  • Biophysics (AREA)
  • Biochemistry (AREA)
  • Immunology (AREA)
  • Crystallography & Structural Chemistry (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Neurology (AREA)
  • Virology (AREA)
  • Oncology (AREA)
  • Biomedical Technology (AREA)
  • Neurosurgery (AREA)
  • Communicable Diseases (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Tropical Medicine & Parasitology (AREA)
  • Rheumatology (AREA)
  • Epidemiology (AREA)
  • Psychiatry (AREA)
  • Dermatology (AREA)
  • AIDS & HIV (AREA)
  • Pain & Pain Management (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Cardiology (AREA)
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KR1020217022768A 2014-07-14 2015-07-14 효소 억제를 위한 에폭시케톤 화합물 Active KR102462240B1 (ko)

Applications Claiming Priority (4)

Application Number Priority Date Filing Date Title
US201462024024P 2014-07-14 2014-07-14
US62/024,024 2014-07-14
KR1020177004070A KR102360356B1 (ko) 2014-07-14 2015-07-14 효소 억제를 위한 에폭시케톤 화합물
PCT/US2015/040459 WO2016011088A2 (en) 2014-07-14 2015-07-14 Epoxyketone compounds for enzyme inhibition

Related Parent Applications (1)

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KR1020177004070A Division KR102360356B1 (ko) 2014-07-14 2015-07-14 효소 억제를 위한 에폭시케톤 화합물

Publications (2)

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KR20210093378A KR20210093378A (ko) 2021-07-27
KR102462240B1 true KR102462240B1 (ko) 2022-11-03

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KR1020217022768A Active KR102462240B1 (ko) 2014-07-14 2015-07-14 효소 억제를 위한 에폭시케톤 화합물
KR1020177004070A Active KR102360356B1 (ko) 2014-07-14 2015-07-14 효소 억제를 위한 에폭시케톤 화합물

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Country Status (10)

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US (2) US10640533B2 (enExample)
EP (1) EP3166933B1 (enExample)
JP (1) JP6608442B2 (enExample)
KR (2) KR102462240B1 (enExample)
CN (1) CN105960399B (enExample)
DK (1) DK3166933T3 (enExample)
ES (1) ES2704056T3 (enExample)
PT (1) PT3166933T (enExample)
TR (1) TR201816372T4 (enExample)
WO (1) WO2016011088A2 (enExample)

Families Citing this family (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP6608442B2 (ja) 2014-07-14 2019-11-20 セントラックス インターナショナル，インコーポレイテッド 酵素阻害に用いられるエポキシケトン化合物
WO2021072212A1 (en) * 2019-10-11 2021-04-15 Mayo Foundation For Medical Education And Research Proteasome inhibitors
TWI869142B (zh) * 2022-12-27 2025-01-01 大陸商上海美悦生物科技發展有限公司 三肽環氧酮化合物、藥物組合物及其製備方法和用途

Citations (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2014018807A1 (en) 2012-07-26 2014-01-30 Centrax International, Inc. Peptide epoxyketone compounds

Family Cites Families (12)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
BRPI0509879A (pt) 2004-04-15 2007-10-16 Proteolix Inc compostos para inibição enzimática
US20050256324A1 (en) 2004-05-10 2005-11-17 Proteolix, Inc. Synthesis of amino acid keto-epoxides
PT2261236E (pt) * 2004-12-07 2015-10-30 Onyx Therapeutics Inc Composição para a inibição de proteassoma
NZ595196A (en) 2005-11-09 2013-03-28 Proteolix Inc Peptide-based compounds for enzyme inhibition
WO2008140782A2 (en) 2007-05-10 2008-11-20 Proteolix, Inc. Compounds for enzyme inhibition
EA035100B1 (ru) * 2008-10-21 2020-04-28 Оникс Терапьютикс, Инк. Комбинированная терапия с применением пептид эпоксикетонов
RU2012147246A (ru) * 2010-04-07 2014-05-20 Оникс Терапьютикс, Инк. Кристаллический пептидный эпоксикетонный ингебитор иммунопротеасомы
EP4144354B1 (en) * 2011-08-30 2025-11-26 Trustees Of Tufts College Fap-activated proteasome inhibitors for treating solid tumors
US9388126B2 (en) 2012-07-19 2016-07-12 Drexel University Sigma receptor ligands and methods of modulating cellular protein homeostasis using same
AU2013302269A1 (en) * 2012-08-14 2015-03-12 Trillium Therapeutics Inc. Fluorinated epoxyketone-based compounds and uses thereof as proteasome inhibitors
CA2881986A1 (en) 2012-08-21 2014-02-27 Fluorinov Pharma Inc. Fluorinated epoxyketone-based tetrapeptide compounds and uses thereof as proteasome inhibitors
JP6608442B2 (ja) 2014-07-14 2019-11-20 セントラックス インターナショナル，インコーポレイテッド 酵素阻害に用いられるエポキシケトン化合物

Patent Citations (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2014018807A1 (en) 2012-07-26 2014-01-30 Centrax International, Inc. Peptide epoxyketone compounds

Non-Patent Citations (1)

* Cited by examiner, † Cited by third party
Title
J. Zhang 등, Chem. Biol. Drug Des., vol.84, p.497-504 (2014.06.03.)

Also Published As

Publication number Publication date
EP3166933B1 (en) 2018-08-01
DK3166933T3 (en) 2018-11-26
KR102360356B1 (ko) 2022-02-08
JP6608442B2 (ja) 2019-11-20
ES2704056T3 (es) 2019-03-14
EP3166933A4 (en) 2017-07-19
JP2017522383A (ja) 2017-08-10
US10640533B2 (en) 2020-05-05
US20200087343A1 (en) 2020-03-19
US10787482B2 (en) 2020-09-29
TR201816372T4 (tr) 2018-11-21
CN105960399B (zh) 2018-09-25
WO2016011088A2 (en) 2016-01-21
PT3166933T (pt) 2018-12-06
KR20170041747A (ko) 2017-04-17
CN105960399A (zh) 2016-09-21
US20170158734A1 (en) 2017-06-08
EP3166933A2 (en) 2017-05-17
KR20210093378A (ko) 2021-07-27
WO2016011088A3 (en) 2016-08-11

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