CA3013650A1 - Rapadocins, inhibitors of equilibrative nucleoside transporter 1 and uses thereof - Google Patents

Rapadocins, inhibitors of equilibrative nucleoside transporter 1 and uses thereof Download PDF

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Publication number
CA3013650A1
CA3013650A1 CA3013650A CA3013650A CA3013650A1 CA 3013650 A1 CA3013650 A1 CA 3013650A1 CA 3013650 A CA3013650 A CA 3013650A CA 3013650 A CA3013650 A CA 3013650A CA 3013650 A1 CA3013650 A1 CA 3013650A1
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Prior art keywords
mleu
improvement
dpro
mphe
phg
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Abandoned
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CA3013650A
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English (en)
French (fr)
Inventor
Jun Liu
Jingxin Wang
Zhaoli Sun
Sam Hong
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Johns Hopkins University
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Johns Hopkins University
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Publication of CA3013650A1 publication Critical patent/CA3013650A1/en
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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
    • C07K5/10—Tetrapeptides
    • C07K5/1002—Tetrapeptides with the first amino acid being neutral
    • C07K5/1005—Tetrapeptides with the first amino acid being neutral and aliphatic
    • C07K5/1008—Tetrapeptides 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
    • C07K7/00—Peptides having 5 to 20 amino acids in a fully defined sequence; Derivatives thereof
    • C07K7/02—Linear peptides containing at least one abnormal peptide link
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K38/00—Medicinal preparations containing peptides
    • A61K38/04—Peptides having up to 20 amino acids in a fully defined sequence; Derivatives thereof
    • A61K38/07—Tetrapeptides
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K38/00—Medicinal preparations containing peptides
    • A61K38/04—Peptides having up to 20 amino acids in a fully defined sequence; Derivatives thereof
    • A61K38/12—Cyclic peptides, e.g. bacitracins; Polymyxins; Gramicidins S, C; Tyrocidins A, B or C
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K47/00—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
    • A61K47/50—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates
    • A61K47/51—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent
    • A61K47/54—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent the modifying agent being an organic compound
    • A61K47/545—Heterocyclic compounds
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/0012—Galenical forms characterised by the site of application
    • A61K9/0014—Skin, i.e. galenical aspects of topical compositions
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    • A61K9/0019—Injectable compositions; Intramuscular, intravenous, arterial, subcutaneous administration; Compositions to be administered through the skin in an invasive manner
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    • A—HUMAN NECESSITIES
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    • A—HUMAN NECESSITIES
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    • A61P9/12—Antihypertensives
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D498/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D498/12—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms in which the condensed system contains three hetero rings
    • C07D498/18—Bridged systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D519/00—Heterocyclic compounds containing more than one system of two or more relevant hetero rings condensed among themselves or condensed with a common carbocyclic ring system not provided for in groups C07D453/00 or C07D455/00
    • 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)
  • Life Sciences & Earth Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • General Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
  • Public Health (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Cardiology (AREA)
  • Biomedical Technology (AREA)
  • Neurology (AREA)
  • Neurosurgery (AREA)
  • Epidemiology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Immunology (AREA)
  • Proteomics, Peptides & Aminoacids (AREA)
  • Gastroenterology & Hepatology (AREA)
  • Pain & Pain Management (AREA)
  • Oncology (AREA)
  • Pulmonology (AREA)
  • Dermatology (AREA)
  • Communicable Diseases (AREA)
  • Diabetes (AREA)
  • Hematology (AREA)
  • Rheumatology (AREA)
  • Ophthalmology & Optometry (AREA)
  • Genetics & Genomics (AREA)
  • Molecular Biology (AREA)
  • Biochemistry (AREA)
  • Biophysics (AREA)
  • Hospice & Palliative Care (AREA)
  • Virology (AREA)
  • Gynecology & Obstetrics (AREA)
CA3013650A 2016-02-04 2017-02-03 Rapadocins, inhibitors of equilibrative nucleoside transporter 1 and uses thereof Abandoned CA3013650A1 (en)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US201662291428P 2016-02-04 2016-02-04
US62/291,428 2016-02-04
PCT/US2017/016494 WO2017136717A1 (en) 2016-02-04 2017-02-03 Rapadocins, inhibitors of equilibrative nucleoside transporter 1 and uses thereof

Publications (1)

Publication Number Publication Date
CA3013650A1 true CA3013650A1 (en) 2017-08-10

Family

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Family Applications (1)

Application Number Title Priority Date Filing Date
CA3013650A Abandoned CA3013650A1 (en) 2016-02-04 2017-02-03 Rapadocins, inhibitors of equilibrative nucleoside transporter 1 and uses thereof

Country Status (9)

Country Link
US (2) US10774110B2 (https=)
EP (2) EP3411032B1 (https=)
JP (1) JP7022069B2 (https=)
CN (2) CN113999281A (https=)
AU (1) AU2017214557B2 (https=)
CA (1) CA3013650A1 (https=)
ES (1) ES2837484T3 (https=)
MX (2) MX380313B (https=)
WO (1) WO2017136717A1 (https=)

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US10774110B2 (en) * 2016-02-04 2020-09-15 The Johns Hopkins University Rapadocins, inhibitors of equilibrative nucleoside transporter 1 and uses thereof
CA3013783A1 (en) * 2016-02-04 2017-08-10 The Johns Hopkins University Rapaglutins, novel inhibitors of glut and use thereof
US11066416B2 (en) 2016-02-04 2021-07-20 The Johns Hopkins University Rapafucin derivative compounds and methods of use thereof
TW202126323A (zh) * 2019-10-01 2021-07-16 約翰斯赫普金斯大學 雷帕弗辛（Ｒａｐａｆｕｃｉｎ）衍生化合物及其使用方法
AR121777A1 (es) * 2020-04-07 2022-07-06 iTeos Belgium SA Derivados de diamina macrocíclica como inhibidores de ent para el tratamiento de cánceres, y combinación de estos con antagonistas del receptor de adenosina
JP2024537110A (ja) * 2021-10-06 2024-10-10 アイテオ ベルギウム エスエー Ｅｎｔ１阻害活性を有する大環状化合物
WO2023056910A1 (en) * 2021-10-06 2023-04-13 iTeos Belgium SA Processes for preparing a macrocyclic compound having ent1 inhibiting activity

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US10774110B2 (en) 2016-02-04 2020-09-15 The Johns Hopkins University Rapadocins, inhibitors of equilibrative nucleoside transporter 1 and uses thereof
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AU2017214557B2 (en) 2022-05-19
US20190031716A1 (en) 2019-01-31
CN113999281A (zh) 2022-02-01
US10774110B2 (en) 2020-09-15
AU2017214557A1 (en) 2018-08-16
US11555054B2 (en) 2023-01-17
EP3782636B1 (en) 2024-05-15
WO2017136717A1 (en) 2017-08-10
MX2018009407A (es) 2018-11-09
EP3411032A1 (en) 2018-12-12
MX380313B (es) 2025-03-12
EP3411032B1 (en) 2020-09-30
CN108697701B (zh) 2021-10-26
EP3782636A1 (en) 2021-02-24
US20200392182A1 (en) 2020-12-17
JP7022069B2 (ja) 2022-02-17
MX2021002588A (es) 2021-04-19
EP3411032A4 (en) 2019-08-14
ES2837484T3 (es) 2021-06-30
JP2019508397A (ja) 2019-03-28
CN108697701A (zh) 2018-10-23

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