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
administration
disease
synthesis
solution
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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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    • 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
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/12—Antivirals
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    • A61P35/00—Antineoplastic agents
    • 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
    • A—HUMAN NECESSITIES
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    • 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
    • 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)
  • General Health & Medical Sciences (AREA)
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  • 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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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

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

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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)

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 (2)

* 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
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 (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

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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
US9388126B2 (en) 2012-07-19 2016-07-12 Drexel University 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
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 (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)

* Cited by examiner, † Cited by third party
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

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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
KR102462240B1 (ko) 2022-11-03
US20200087343A1 (en) 2020-03-19
US10787482B2 (en) 2020-09-29
TR201816372T4 (tr) 2018-11-21
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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