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)
  • Medicinal Chemistry (AREA)
  • General Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • 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)
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 (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
EP3166933B1 (en) 2014-07-14 2018-08-01 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
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

Family Cites Families (13)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2005105827A2 (en) * 2004-04-15 2005-11-10 Proteolix, Inc. Compounds for proteasome enzyme inhibition
AU2005243140A1 (en) * 2004-05-10 2005-11-24 Proteolix, Inc. Synthesis of amino acid keto-epoxides
WO2006063154A1 (en) * 2004-12-07 2006-06-15 Proteolix, 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
KR20110073584A (ko) 2008-10-21 2011-06-29 오닉스 세라퓨틱스, 인크. 펩티드 에폭시케톤과의 병용 요법
MX2012011604A (es) * 2010-04-07 2013-02-27 Onyx Therapeutics Inc Inhibidor de inmunoproteasoma de péptido epoxicetona cristalino.
EP4144354B1 (en) 2011-08-30 2025-11-26 Trustees Of Tufts College Fap-activated proteasome inhibitors for treating solid tumors
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
JP2015526433A (ja) * 2012-08-14 2015-09-10 フルオリノブ ファーマ インコーポレイテッド フッ素化エポキシケトン系化合物、およびプロテアソーム阻害物質としてのその使用
CA2881986A1 (en) * 2012-08-21 2014-02-27 Fluorinov Pharma Inc. Fluorinated epoxyketone-based tetrapeptide compounds and uses thereof as proteasome inhibitors
EP3166933B1 (en) 2014-07-14 2018-08-01 Centrax International Inc. Epoxyketone compounds for enzyme inhibition

Also Published As

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

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