KR102360356B1 - 효소 억제를 위한 에폭시케톤 화합물 - Google Patents

효소 억제를 위한 에폭시케톤 화합물 Download PDF

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KR102360356B1
KR102360356B1 KR1020177004070A KR20177004070A KR102360356B1 KR 102360356 B1 KR102360356 B1 KR 102360356B1 KR 1020177004070 A KR1020177004070 A KR 1020177004070A KR 20177004070 A KR20177004070 A KR 20177004070A KR 102360356 B1 KR102360356 B1 KR 102360356B1
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mmol
proteasome
pharmaceutical composition
cancer
synthesis
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KR20170041747A (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
    • 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
    • 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
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    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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    • A—HUMAN NECESSITIES
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    • A61P17/00—Drugs for dermatological disorders
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    • 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
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    • 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
    • C07K5/04—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)
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  • Life Sciences & Earth Sciences (AREA)
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  • General Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
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  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Proteomics, Peptides & Aminoacids (AREA)
  • Molecular Biology (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Biophysics (AREA)
  • Biochemistry (AREA)
  • Genetics & Genomics (AREA)
  • Immunology (AREA)
  • Crystallography & Structural Chemistry (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Neurology (AREA)
  • Neurosurgery (AREA)
  • Rheumatology (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Tropical Medicine & Parasitology (AREA)
  • Biomedical Technology (AREA)
  • Virology (AREA)
  • Communicable Diseases (AREA)
  • Oncology (AREA)
  • Epidemiology (AREA)
  • AIDS & HIV (AREA)
  • Hospice & Palliative Care (AREA)
  • Dermatology (AREA)
  • Pain & Pain Management (AREA)
  • Vascular Medicine (AREA)
  • Cardiology (AREA)
  • Urology & Nephrology (AREA)
KR1020177004070A 2014-07-14 2015-07-14 효소 억제를 위한 에폭시케톤 화합물 Active KR102360356B1 (ko)

Priority Applications (1)

Application Number Priority Date Filing Date Title
KR1020217022768A KR102462240B1 (ko) 2014-07-14 2015-07-14 효소 억제를 위한 에폭시케톤 화합물

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US201462024024P 2014-07-14 2014-07-14
US62/024,024 2014-07-14
PCT/US2015/040459 WO2016011088A2 (en) 2014-07-14 2015-07-14 Epoxyketone compounds for enzyme inhibition

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KR1020217022768A Division KR102462240B1 (ko) 2014-07-14 2015-07-14 효소 억제를 위한 에폭시케톤 화합물

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KR20170041747A KR20170041747A (ko) 2017-04-17
KR102360356B1 true KR102360356B1 (ko) 2022-02-08

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

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US (2) US10640533B2 (cg-RX-API-DMAC7.html)
EP (1) EP3166933B1 (cg-RX-API-DMAC7.html)
JP (1) JP6608442B2 (cg-RX-API-DMAC7.html)
KR (2) KR102360356B1 (cg-RX-API-DMAC7.html)
CN (1) CN105960399B (cg-RX-API-DMAC7.html)
DK (1) DK3166933T3 (cg-RX-API-DMAC7.html)
ES (1) ES2704056T3 (cg-RX-API-DMAC7.html)
PT (1) PT3166933T (cg-RX-API-DMAC7.html)
TR (1) TR201816372T4 (cg-RX-API-DMAC7.html)
WO (1) WO2016011088A2 (cg-RX-API-DMAC7.html)

Families Citing this family (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2016011088A2 (en) 2014-07-14 2016-01-21 Centrax International, Inc. Epoxyketone compounds for enzyme inhibition
US20240092831A1 (en) * 2019-10-11 2024-03-21 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
WO2026041079A1 (zh) * 2024-08-23 2026-02-26 江苏正大清江制药有限公司 肽环氧酮类化合物及其制备方法和应用

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)

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Publication number Priority date Publication date Assignee Title
ATE494298T1 (de) * 2004-04-15 2011-01-15 Proteolix Inc Verbindungen zur proteasomenzymhemmung
AU2005243140A1 (en) * 2004-05-10 2005-11-24 Proteolix, Inc. Synthesis of amino acid keto-epoxides
EP2261236B1 (en) * 2004-12-07 2015-07-15 Onyx Therapeutics, Inc. Composition for proteasome inhibition
EP2623113B1 (en) * 2005-11-09 2017-05-31 Onyx Therapeutics, Inc. Compound for enzyme inhibition
WO2008140782A2 (en) 2007-05-10 2008-11-20 Proteolix, Inc. Compounds for enzyme inhibition
JP5675629B2 (ja) 2008-10-21 2015-02-25 オニキス セラピューティクス， インク．Ｏｎｙｘ Ｔｈｅｒａｐｅｕｔｉｃｓ， Ｉｎｃ． ペプチドエポキシケトンを用いた併用療法
CA2795559A1 (en) * 2010-04-07 2011-11-03 Onyx Therapeutics, Inc. Crystalline peptide epoxyketone immunoproteasome inhibitor
EP4706663A3 (en) 2011-08-30 2026-05-20 Trustees Of Tufts College FAP-ACTIVATED PROTEASOME INHIBITORS USED TO TREAT SOLID TUMORS
WO2014015157A2 (en) 2012-07-19 2014-01-23 Philadelphia Health & Education Corporation Novel sigma receptor ligands and methods of modulating cellular protein homeostasis using same
CA2881999A1 (en) * 2012-08-14 2014-02-20 Abdelmalik Slassi Fluorinated epoxyketone-based compounds and uses thereof as proteasome inhibitors
WO2014029022A1 (en) * 2012-08-21 2014-02-27 Abdelmalik Slassi Fluorinated epoxyketone-based tetrapeptide compounds and uses thereof as proteasome inhibitors
WO2016011088A2 (en) 2014-07-14 2016-01-21 Centrax International, Inc. Epoxyketone compounds for enzyme inhibition

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
DK3166933T3 (en) 2018-11-26
EP3166933A4 (en) 2017-07-19
KR102462240B1 (ko) 2022-11-03
KR20170041747A (ko) 2017-04-17
US10640533B2 (en) 2020-05-05
JP2017522383A (ja) 2017-08-10
EP3166933B1 (en) 2018-08-01
CN105960399B (zh) 2018-09-25
US20200087343A1 (en) 2020-03-19
TR201816372T4 (tr) 2018-11-21
US20170158734A1 (en) 2017-06-08
CN105960399A (zh) 2016-09-21
JP6608442B2 (ja) 2019-11-20
US10787482B2 (en) 2020-09-29
WO2016011088A3 (en) 2016-08-11
KR20210093378A (ko) 2021-07-27
PT3166933T (pt) 2018-12-06
ES2704056T3 (es) 2019-03-14
EP3166933A2 (en) 2017-05-17
WO2016011088A2 (en) 2016-01-21

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