CN105960399B - 酶抑制剂环氧酮化合物 - Google Patents

酶抑制剂环氧酮化合物 Download PDF

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CN105960399B
CN105960399B CN201580002532.1A CN201580002532A CN105960399B CN 105960399 B CN105960399 B CN 105960399B CN 201580002532 A CN201580002532 A CN 201580002532A CN 105960399 B CN105960399 B CN 105960399B
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compound
disease
synthesis
esi
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CN105960399A (zh
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杨金夫
岑坚
范晓青
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Ningbo Saint Kin Biological Medicine Technology Co Ltd
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Ningbo Saint Kin Biological Medicine Technology Co Ltd
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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
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00—Drugs for disorders of the respiratory system
    • A—HUMAN NECESSITIES
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    • 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
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    • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
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    • 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
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    • 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
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    • 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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K38/00—Medicinal preparations containing peptides

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
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  • Medicinal Chemistry (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)
CN201580002532.1A 2014-07-14 2015-07-14 酶抑制剂环氧酮化合物 Active CN105960399B (zh)

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

Publications (2)

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CN105960399A CN105960399A (zh) 2016-09-21
CN105960399B true CN105960399B (zh) 2018-09-25

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US (2) US10640533B2 (https=)
EP (1) EP3166933B1 (https=)
JP (1) JP6608442B2 (https=)
KR (2) KR102360356B1 (https=)
CN (1) CN105960399B (https=)
DK (1) DK3166933T3 (https=)
ES (1) ES2704056T3 (https=)
PT (1) PT3166933T (https=)
TR (1) TR201816372T4 (https=)
WO (1) WO2016011088A2 (https=)

Cited By (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US10787482B2 (en) 2014-07-14 2020-09-29 Centrax International Inc. Epoxyketone compounds for enzyme inhibition

Families Citing this family (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2021072212A1 (en) * 2019-10-11 2021-04-15 Mayo Foundation For Medical Education And Research Proteasome inhibitors
CN118255835A (zh) * 2022-12-27 2024-06-28 上海美悦生物科技发展有限公司 三肽环氧酮化合物、药物组合物及其制备方法和用途
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 (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2013033396A2 (en) * 2011-08-30 2013-03-07 Trustees Of Tufts College Fap-activated proteasome inhibitors for treating solid tumors
WO2014026282A1 (en) * 2012-08-14 2014-02-20 Abdelmalik Slassi Fluorinated epoxyketone-based compounds and uses thereof as proteasome inhibitors

Family Cites Families (11)

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WO2005105827A2 (en) 2004-04-15 2005-11-10 Proteolix, Inc. Compounds for proteasome enzyme inhibition
US20050256324A1 (en) * 2004-05-10 2005-11-17 Proteolix, Inc. Synthesis of amino acid keto-epoxides
HUE027850T2 (en) * 2004-12-07 2016-11-28 Onyx Therapeutics Inc Preparation for proteasome inhibition
RU2453556C2 (ru) 2005-11-09 2012-06-20 Протеоликс, Инк. Соединения для ингибирования фермента
WO2008140782A2 (en) * 2007-05-10 2008-11-20 Proteolix, Inc. Compounds for enzyme inhibition
AU2009308516B2 (en) 2008-10-21 2016-08-25 Onyx Therapeutics, Inc. Combination therapy with peptide epoxyketones
NZ602872A (en) * 2010-04-07 2014-05-30 Onyx Therapeutics Inc Crystalline peptide epoxyketone immunoproteasome inhibitor
CA2879454A1 (en) 2012-07-19 2014-01-23 Drexel University Novel sigma receptor ligands and methods of modulating cellular protein homeostasis using same
WO2014018807A1 (en) * 2012-07-26 2014-01-30 Centrax International, Inc. Peptide epoxyketone compounds
CA2881986A1 (en) 2012-08-21 2014-02-27 Fluorinov Pharma Inc. Fluorinated epoxyketone-based tetrapeptide compounds and uses thereof as proteasome inhibitors
KR102360356B1 (ko) 2014-07-14 2022-02-08 센트랙스 인터내셔널, 아이엔씨. 효소 억제를 위한 에폭시케톤 화합물

Patent Citations (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2013033396A2 (en) * 2011-08-30 2013-03-07 Trustees Of Tufts College Fap-activated proteasome inhibitors for treating solid tumors
WO2014026282A1 (en) * 2012-08-14 2014-02-20 Abdelmalik Slassi Fluorinated epoxyketone-based compounds and uses thereof as proteasome inhibitors

Non-Patent Citations (3)

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Title
Design, Synthesis and Biological Evaluation of Peptidyl Epoxyketone Proteasome Inhibitors Composed of b-amino Acids;Jiankang Zhang 等;《Chem. Biol. Drug Des.》;20140604;第84卷(第5期);第497-504页 *
Selective Inhibitor of Proteasome’s Caspase-like Sites Sensitizes Cells to Specific Inhibition of Chymotrypsin-like Sites;Matthew Britton 等;《Chemistry & Biology》;20091224;第16卷(第12期);第1278–1289页 *
环氧酮肽蛋白酶体抑制剂的构效关系及基于分子相似性的分子设计;吕娟 等;《化学研究与应用》;20120930;第24卷(第9期);第1376-1388页 *

Cited By (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US10787482B2 (en) 2014-07-14 2020-09-29 Centrax International Inc. Epoxyketone compounds for enzyme inhibition

Also Published As

Publication number Publication date
KR102360356B1 (ko) 2022-02-08
WO2016011088A3 (en) 2016-08-11
DK3166933T3 (en) 2018-11-26
CN105960399A (zh) 2016-09-21
TR201816372T4 (tr) 2018-11-21
KR102462240B1 (ko) 2022-11-03
ES2704056T3 (es) 2019-03-14
US20200087343A1 (en) 2020-03-19
PT3166933T (pt) 2018-12-06
KR20210093378A (ko) 2021-07-27
WO2016011088A2 (en) 2016-01-21
EP3166933B1 (en) 2018-08-01
EP3166933A4 (en) 2017-07-19
US10787482B2 (en) 2020-09-29
EP3166933A2 (en) 2017-05-17
JP2017522383A (ja) 2017-08-10
KR20170041747A (ko) 2017-04-17
US10640533B2 (en) 2020-05-05
US20170158734A1 (en) 2017-06-08
JP6608442B2 (ja) 2019-11-20

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