DK3166933T3 - EPOXYKETONE COMPOUNDS FOR ENZYME INHIBITION - Google Patents

EPOXYKETONE COMPOUNDS FOR ENZYME INHIBITION Download PDF

Info

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
Authority
DK
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
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Application filed by Centrax Int Inc filed Critical Centrax Int Inc
Application granted granted Critical
Publication of DK3166933T3 publication Critical patent/DK3166933T3/en

Links

Classifications

    • 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
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00—Drugs for dermatological disorders
    • A61P17/14—Drugs for dermatological disorders for baldness or alopecia
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • 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
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P21/00—Drugs for disorders of the muscular or neuromuscular system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • 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
    • C07K5/02—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

Landscapes

  • 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) KR102360356B1 (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 (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

Family Cites Families (13)

* Cited by examiner, † Cited by third party
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
WO2014018807A1 (en) * 2012-07-26 2014-01-30 Centrax International, Inc. Peptide epoxyketone compounds
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

Also Published As

Publication number Publication date
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
KR102360356B1 (ko) 2022-02-08
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

Similar Documents

Publication Publication Date Title
JP5740383B2 (ja) 酵素阻害のための化合物
EP3262051B1 (en) Selective bace1 inhibitors
EP3388427B1 (en) Derivatives of dolastatin 10 and auristatins
US10787482B2 (en) Epoxyketone compounds for enzyme inhibition
JPWO1993003054A1 (ja) 新規なテトラペプチド誘導体
DE69132439T2 (de) Inhibitoren retroviraler Proteasen
JPWO1998009949A1 (ja) 新規アセトアミド誘導体およびプロテアーゼ阻害剤
US20120004229A1 (en) Substituted diketopiperazines and their use as oxytocin antagonists
CN105164117A (zh) 二肽和三肽环氧酮蛋白酶抑制剂
WO2014018807A1 (en) Peptide epoxyketone compounds
EP2920182A1 (en) Macrocyclic compounds and uses thereof
CN109180780B (zh) 多肽环氧酮化合物
CN119403815A (zh) 二脱氢-3’-脱氧-4’-乙炔基胸苷和相关化合物以及它们在治疗医学疾患中的用途
EP2896623A1 (en) CRYSTAL OF N-[2-({2-[(2S)-2-CYANOPYRROLIDIN-1-YL]-2- OXOETHYL}AMINO)-2-METHYLPROPYL]-2-METHYLPYRAZOLO[1,5-a]PYRIMIDINE-6-CARBOXAMIDE
HK1228891A1 (en) Epoxyketone compounds for enzyme inhibition
JP3782507B2 (ja) 新規なn−メチルプロリン誘導体
Rao et al. Synthesis and Characterization of Novel Atazanavir Analogs