DK3166933T3 - EPOXYKETONE COMPOUNDS FOR ENZYME INHIBITION - Google Patents

EPOXYKETONE COMPOUNDS FOR ENZYME INHIBITION Download PDF

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Publication number
DK3166933T3
DK3166933T3 DK15821964.2T DK15821964T DK3166933T3 DK 3166933 T3 DK3166933 T3 DK 3166933T3 DK 15821964 T DK15821964 T DK 15821964T DK 3166933 T3 DK3166933 T3 DK 3166933T3
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Denmark
Prior art keywords
compound
mmol
proteasome
synthesis
added
Prior art date
Application number
DK15821964.2T
Other languages
Danish (da)
English (en)
Inventor
Jinfu Yang
Jian James Cen
Xiaoqing Michelle Fan
Original Assignee
Centrax Int Inc
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Publication of DK3166933T3 publication Critical patent/DK3166933T3/en

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    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07KPEPTIDES
    • C07K5/00Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
    • C07K5/04Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing only normal peptide links
    • C07K5/06Dipeptides
    • C07K5/06008Dipeptides with the first amino acid being neutral
    • C07K5/06078Dipeptides with the first amino acid being neutral and aromatic or cycloaliphatic
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00Drugs for disorders of the respiratory system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00Drugs for dermatological disorders
    • A61P17/14Drugs for dermatological disorders for baldness or alopecia
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00Drugs for skeletal disorders
    • A61P19/08Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P21/00Drugs for disorders of the muscular or neuromuscular system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/28Drugs 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P27/00Drugs for disorders of the senses
    • A61P27/02Ophthalmic agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/12Antivirals
    • A61P31/14Antivirals for RNA viruses
    • A61P31/18Antivirals for RNA viruses for HIV
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P33/00Antiparasitic agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00Drugs for immunological or allergic disorders
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00Drugs for immunological or allergic disorders
    • A61P37/02Immunomodulators
    • A61P37/06Immunosuppressants, e.g. drugs for graft rejection
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system
    • A61P9/10Drugs 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07KPEPTIDES
    • C07K5/00Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
    • C07K5/02Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing at least one abnormal peptide link
    • C07K5/0202Peptides 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07KPEPTIDES
    • C07K5/00Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
    • C07K5/04Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing only normal peptide links
    • C07K5/08Tripeptides
    • C07K5/0802Tripeptides with the first amino acid being neutral
    • C07K5/0804Tripeptides with the first amino acid being neutral and aliphatic
    • C07K5/0806Tripeptides with the first amino acid being neutral and aliphatic the side chain containing 0 or 1 carbon atoms, i.e. Gly, Ala
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07KPEPTIDES
    • C07K5/00Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
    • C07K5/04Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing only normal peptide links
    • C07K5/08Tripeptides
    • C07K5/0821Tripeptides with the first amino acid being heterocyclic, e.g. His, Pro, Trp
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K38/00Medicinal preparations containing peptides

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Animal Behavior & Ethology (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Proteomics, Peptides & Aminoacids (AREA)
  • Molecular Biology (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Biochemistry (AREA)
  • Biophysics (AREA)
  • Genetics & Genomics (AREA)
  • Immunology (AREA)
  • Crystallography & Structural Chemistry (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Neurology (AREA)
  • Tropical Medicine & Parasitology (AREA)
  • Biomedical Technology (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Neurosurgery (AREA)
  • Rheumatology (AREA)
  • Virology (AREA)
  • Communicable Diseases (AREA)
  • Oncology (AREA)
  • Epidemiology (AREA)
  • Transplantation (AREA)
  • AIDS & HIV (AREA)
  • Psychiatry (AREA)
  • Urology & Nephrology (AREA)
  • Vascular Medicine (AREA)
  • Cardiology (AREA)
  • Heart & Thoracic Surgery (AREA)
DK15821964.2T 2014-07-14 2015-07-14 EPOXYKETONE COMPOUNDS FOR ENZYME INHIBITION DK3166933T3 (en)

Applications Claiming Priority (2)

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

Publications (1)

Publication Number Publication Date
DK3166933T3 true DK3166933T3 (en) 2018-11-26

Family

ID=55079165

Family Applications (1)

Application Number Title Priority Date Filing Date
DK15821964.2T DK3166933T3 (en) 2014-07-14 2015-07-14 EPOXYKETONE COMPOUNDS FOR ENZYME INHIBITION

Country Status (10)

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

Families Citing this family (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
ES2704056T3 (es) 2014-07-14 2019-03-14 Centrax Int Inc Compuestos de epoxicetona para la inhibición de enzimas
EP4041747A4 (en) * 2019-10-11 2023-10-18 Mayo Foundation for Medical Education and Research PROTEASOME HIBITORS
WO2024140736A1 (zh) * 2022-12-27 2024-07-04 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

Family Cites Families (13)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CA2562411A1 (en) 2004-04-15 2005-11-10 Proteolix, Inc. Compounds for enzyme inhibition
US20050256324A1 (en) * 2004-05-10 2005-11-17 Proteolix, Inc. Synthesis of amino acid keto-epoxides
ES2408216T3 (es) * 2004-12-07 2013-06-19 Onyx Therapeutics, Inc. Composición para la inhibición del proteasoma
US7687456B2 (en) 2005-11-09 2010-03-30 Proteolix, Inc. Compounds for enzyme inhibition
WO2008140782A2 (en) * 2007-05-10 2008-11-20 Proteolix, Inc. Compounds for enzyme inhibition
PE20120059A1 (es) * 2008-10-21 2012-02-27 Onyx Therapeutics Inc Combinaciones farmaceuticas con epoxicetonas peptidicas
WO2011136905A2 (en) 2010-04-07 2011-11-03 Onyx Therapeutics, Inc. Crystalline peptide epoxyketone immunoproteasome inhibitor
HUE060305T2 (hu) * 2011-08-30 2023-02-28 Tufts College FAP-aktivált proteaszóma inhibitorok a szolid tumorok kezelésére
EP2874997A4 (en) 2012-07-19 2016-01-06 Univ Drexel NEW SIGMA RECEPTOR LIGANDS AND METHOD FOR REGULATING CELLULAR PROTEIN HOMEOSTASIS THEREWITH
WO2014018807A1 (en) * 2012-07-26 2014-01-30 Centrax International, Inc. Peptide epoxyketone compounds
WO2014026282A1 (en) * 2012-08-14 2014-02-20 Abdelmalik Slassi Fluorinated epoxyketone-based compounds and uses thereof as proteasome inhibitors
US20150218212A1 (en) * 2012-08-21 2015-08-06 Fluorinov Pharma Inc. Fluorinated epoxyketone-based tetrapeptide compounds and uses thereof as proteasome inhibitors
ES2704056T3 (es) 2014-07-14 2019-03-14 Centrax Int Inc Compuestos de epoxicetona para la inhibición de enzimas

Also Published As

Publication number Publication date
JP6608442B2 (ja) 2019-11-20
ES2704056T3 (es) 2019-03-14
WO2016011088A2 (en) 2016-01-21
CN105960399B (zh) 2018-09-25
US10787482B2 (en) 2020-09-29
TR201816372T4 (tr) 2018-11-21
PT3166933T (pt) 2018-12-06
EP3166933B1 (en) 2018-08-01
US20200087343A1 (en) 2020-03-19
WO2016011088A3 (en) 2016-08-11
KR20210093378A (ko) 2021-07-27
JP2017522383A (ja) 2017-08-10
KR20170041747A (ko) 2017-04-17
US20170158734A1 (en) 2017-06-08
EP3166933A2 (en) 2017-05-17
CN105960399A (zh) 2016-09-21
EP3166933A4 (en) 2017-07-19
US10640533B2 (en) 2020-05-05
KR102462240B1 (ko) 2022-11-03
KR102360356B1 (ko) 2022-02-08

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