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FI3727461T3 - EPHA2:lle spesifisiä bisyklisiä peptidiligandeja - Google Patents

EPHA2:lle spesifisiä bisyklisiä peptidiligandeja

Info

Publication number
FI3727461T3
FI3727461T3 FIEP18829926.7T FI18829926T FI3727461T3 FI 3727461 T3 FI3727461 T3 FI 3727461T3 FI 18829926 T FI18829926 T FI 18829926T FI 3727461 T3 FI3727461 T3 FI 3727461T3
Authority
FI
Finland
Prior art keywords
compound
cancer
pharmaceutical composition
seq
harg
Prior art date
Application number
FIEP18829926.7T
Other languages
English (en)
Inventor
Liuhong Chen
Philip Huxley
Silvia Pavan
Rietschoten Katerine Van
Original Assignee
Bicycletx Ltd
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
Priority claimed from GBGB1721259.8A external-priority patent/GB201721259D0/en
Priority claimed from GBGB1804102.0A external-priority patent/GB201804102D0/en
Priority claimed from GBGB1818603.1A external-priority patent/GB201818603D0/en
Application filed by Bicycletx Ltd filed Critical Bicycletx Ltd
Application granted granted Critical
Publication of FI3727461T3 publication Critical patent/FI3727461T3/fi

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Classifications

    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/535—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one oxygen as the ring hetero atoms, e.g. 1,2-oxazines
    • A61K31/5365—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one oxygen as the ring hetero atoms, e.g. 1,2-oxazines ortho- or peri-condensed with heterocyclic ring systems
    • 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
    • A61K38/05—Dipeptides
    • 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
    • A61K38/10—Peptides having 12 to 20 amino acids
    • 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
    • A61K47/62—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 a protein, peptide or polyamino acid
    • 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
    • A61K47/62—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 a protein, peptide or polyamino acid
    • A61K47/64—Drug-peptide, drug-protein or drug-polyamino acid conjugates, i.e. the modifying agent being a peptide, protein or polyamino acid which is covalently bonded or complexed to a therapeutically active agent
    • 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
    • A61K47/62—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 a protein, peptide or polyamino acid
    • A61K47/64—Drug-peptide, drug-protein or drug-polyamino acid conjugates, i.e. the modifying agent being a peptide, protein or polyamino acid which is covalently bonded or complexed to a therapeutically active agent
    • A61K47/6415—Toxins or lectins, e.g. clostridial toxins or Pseudomonas exotoxins
    • 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
    • A61K47/62—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 a protein, peptide or polyamino acid
    • A61K47/65—Peptidic linkers, binders or spacers, e.g. peptidic enzyme-labile linkers
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07K—PEPTIDES
    • C07K7/00—Peptides having 5 to 20 amino acids in a fully defined sequence; Derivatives thereof
    • C07K7/04—Linear peptides containing only normal peptide links
    • C07K7/08—Linear peptides containing only normal peptide links having 12 to 20 amino acids

Landscapes

  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Proteomics, Peptides & Aminoacids (AREA)
  • Veterinary Medicine (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
  • Public Health (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Epidemiology (AREA)
  • Organic Chemistry (AREA)
  • Molecular Biology (AREA)
  • Gastroenterology & Hepatology (AREA)
  • Immunology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Genetics & Genomics (AREA)
  • Biochemistry (AREA)
  • Biophysics (AREA)
  • Toxicology (AREA)
  • Peptides Or Proteins (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Medicinal Preparation (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)

Claims (10)

PATENTTIVAATIMUKSET
1. Yhdiste, joka yhdiste on BCY6136 tai sen farmaseuttisesti hyväksyttävä suola, jolloin mainitulla yhdisteellä BCY6136 on rakenne: DN Oa N ; NOT Lb aN 02 0E meveom o Y ux SNE AN ON SÅN BOYSOGG vo Hoi o + H AN BDCYS136 HN YO — jolloin BCY6099 on sekvenssin SEQ ID NO: 2 mukainen polypeptidi (B-Ala)-Sari0-A(HArg)D-Ci(HyP)LVNPLCiiLHP(D-Asp)W(HArg)Cii (SEQ ID NO: 2) jolloin Sar on sarkosiini, HArg on homoarginiini ja HyP on hydroksiproliini; jolloin sekvenssin SEQ ID NO: 2 mukainen polypeptidi on syklisoitu Ci:ssä, Cii:ssä ja Cii:ssä 1,1’,1”-(1,3,5-triatsinaani-1,3,5-triyyli)triprop-2-en-1-onilla (TATA).
2. Patenttivaatimuksen 1 mukainen yhdiste, jolloin sekvenssi SEO ID NO: 2 on amidoitu C-terminuksessa.
3. Patenttivaatimuksen 1 tai 2 mukainen yhdiste, jolloin farmaseuttisesti hyväksyttävä suola on valittu vapaasta haposta tai natrium-, kalium-, kalsium- tai ammoniumsuolasta.
4. Farmaseuttinen koostumus, joka käsittää jonkin patenttivaatimuksista 1-3 mukaista yhdistettä yhdessä yhden tai useamman farmaseuttisesti hyväksyttävän apuaineen kanssa.
5. Jonkin patenttivaatimuksista 1-3 mukainen yhdiste tai patenttivaatimuksen 4 mukainen farmaseuttinen koostumus käytettäväksi sellaisen sairauden tai häiriön — ehkäisyyn, tukahduttamiseen tai hoitoon, jolle on ominaista EphAZ2:n likailmentyminen sairaassa kudoksessa.
6. Jonkin patenttivaatimuksista 1-3 mukainen yhdiste tai patenttivaatimuksen 4 mukainen farmaseuttinen koostumus käytettäväksi menetelmässä syövän ehkäisemiseksi, tukahduttamiseksi tai hoitamiseksi.
7. Yhdiste — käytettäväksi tai farmaseuttinen koostumus käytettäväksi patenttivaatimuksen 5 mukaisesti, jolloin sairaus tai häiriö on syöpä.
8. Patenttivaatimuksen 6 tai / mukainen yhdiste tai farmaseuttinen koostumus, jossa syöpä on valittu eturauhassyövän, keuhkosyövän, rintasyövän, mahasyövän, —munasarjasyövän, ruokatorven syövän, multippeli myelooman ja fibrosarkooman joukosta.
9. Yhdiste — käytettäväksi tai farmaseuttinen koostumus käytettäväksi patenttivaatimuksen 8 mukaisesti, jolloin keuhkosyöpä on ei-pienisoluinen keuhkokarsinooma (NSCLC) ja/tai jolloin rintasyöpä on kolmoisnegatiivinen — rintasyöpä
10. — Jonkin patenttivaatimuksista 1-3 mukainen yhdiste tai patenttivaatimuksen 4 mukainen farmaseuttinen koostumus käytettäväksi menetelmässä syövän ehkäisemiseksi, tukahduttamiseksi tai hoitamiseksi sitä tarvitsevalla potilaalla, jolloin mainitulla potilaalla on tunnistettu EphA2:n lisääntynyt kopiomäärän variaatio (CNV).
FIEP18829926.7T 2017-12-19 2018-12-19 EPHA2:lle spesifisiä bisyklisiä peptidiligandeja FI3727461T3 (fi)

Applications Claiming Priority (4)

Application Number Priority Date Filing Date Title
GBGB1721259.8A GB201721259D0 (en) 2017-12-19 2017-12-19 Bicyclic peptide ligands specific for EphA2
GBGB1804102.0A GB201804102D0 (en) 2018-03-14 2018-03-14 Bicycle peptide ligands specific for EphA2
GBGB1818603.1A GB201818603D0 (en) 2018-11-14 2018-11-14 Bicyclic peptide ligands specific for epha2
PCT/GB2018/053678 WO2019122863A1 (en) 2017-12-19 2018-12-19 Bicyclic peptide ligands specific for epha2

Publications (1)

Publication Number Publication Date
FI3727461T3 true FI3727461T3 (fi) 2025-08-15

Family

ID=64902125

Family Applications (2)

Application Number Title Priority Date Filing Date
FIEP22161978.6T FI4053145T3 (fi) 2017-12-19 2018-12-19 EphA2:lle spesifisiä peptidiligandeja
FIEP18829926.7T FI3727461T3 (fi) 2017-12-19 2018-12-19 EPHA2:lle spesifisiä bisyklisiä peptidiligandeja

Family Applications Before (1)

Application Number Title Priority Date Filing Date
FIEP22161978.6T FI4053145T3 (fi) 2017-12-19 2018-12-19 EphA2:lle spesifisiä peptidiligandeja

Country Status (27)

Country Link
US (6) US11484602B2 (fi)
EP (4) EP3727460B1 (fi)
JP (4) JP7293231B2 (fi)
KR (2) KR102791088B1 (fi)
CN (4) CN111787955B (fi)
AU (3) AU2018387417C9 (fi)
BR (2) BR112020012246A2 (fi)
CA (2) CA3086257A1 (fi)
CY (1) CY1125367T1 (fi)
DK (3) DK3727461T3 (fi)
ES (3) ES3037964T3 (fi)
FI (2) FI4053145T3 (fi)
HR (2) HRP20220871T1 (fi)
HU (2) HUE073547T2 (fi)
IL (3) IL275440B2 (fi)
LT (2) LT3727460T (fi)
MX (2) MX2020006482A (fi)
PH (1) PH12020550929A1 (fi)
PL (3) PL4053145T3 (fi)
PT (3) PT3727461T (fi)
RS (1) RS67248B1 (fi)
SA (1) SA520412268B1 (fi)
SG (2) SG11202005495UA (fi)
SI (2) SI3727461T1 (fi)
SM (1) SMT202500312T1 (fi)
TW (1) TWI825046B (fi)
WO (2) WO2019122863A1 (fi)

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JP7734891B2 (ja) * 2021-08-17 2025-09-08 天津星聯▲タイ▼生物科技有限公司 新規な構造を有するポリペプチド薬物複合体及びその使用
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