HRP20230349T1 - Samosastavljeni dvoblok kopolimeri sastavljeni od pegmema i polimernih segmenata koji nose lijek - Google Patents

Samosastavljeni dvoblok kopolimeri sastavljeni od pegmema i polimernih segmenata koji nose lijek Download PDF

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HRP20230349T1
HRP20230349T1 HRP20230349TT HRP20230349T HRP20230349T1 HR P20230349 T1 HRP20230349 T1 HR P20230349T1 HR P20230349T T HRP20230349T T HR P20230349TT HR P20230349 T HRP20230349 T HR P20230349T HR P20230349 T1 HRP20230349 T1 HR P20230349T1
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polymer
formula
drug conjugate
zero
group
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HRP20230349TT
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Rana SANYAL
Amitav SANYAL
Sadik KAGA
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RS Arastirma Egitim Danismanlik Ilac Sanayi Ticaret Anonim Sirketi, Istanbul Teknopark Kulucka Merkezi Sanayi Mah.
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Publication of HRP20230349T1 publication Critical patent/HRP20230349T1/hr

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    • A61K47/6883—Polymer-drug antibody conjugates, e.g. mitomycin-dextran-Ab; DNA-polylysine-antibody complex or conjugate used for therapy
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    • A61K47/6889—Conjugates wherein the antibody being the modifying agent and wherein the linker, binder or spacer confers particular properties to the conjugates, e.g. peptidic enzyme-labile linkers or acid-labile linkers, providing for an acid-labile immuno conjugate wherein the drug may be released from its antibody conjugated part in an acidic, e.g. tumoural or environment
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Claims (15)

1. Konjugat polimer-lijek formule I u obliku blok kopolimera za isporuku terapijskih sredstava [image] naznačen time što • Ri, R2 i R3 su neovisno odabrani između H ili -CH3 • x je prirodni broj između 1-100 • y je prirodni broj između 1-100 • n je prirodni broj između 1-50 i • L je poveznica koja se može cijepati ili L može biti nula pri čemu je terapeutsko sredstvo D vezano izravno na polimerni lanac preko esterske, iminske, amidne, disulfidne, karbonatne, karbamatne, hidrazinske veze i • D je terapeutsko sredstvo koje je kombretastatin ili 5-fluorouracil (5-FU) ili gemcitabin ili klorokin ili doksorubicin • A je krajnja skupina ili A može biti nula • B je krajnja skupina ili B može biti nula.
2. Konjugat polimer-lijek prema zahtjevu 1, naznačen time što je poveznica odabrana iz skupine koja sadrži poli(etilen glikol), aminokiselinu, poli(aminokiselinu) i kratke peptide, po mogućnosti kratki peptid je labilan katepsin B, a najpoželjnije kratki peptid je odabran iz skupine koja sadrži Gly-Phe-Leu-Gly (SEQ ID NO: 1), Val-Cit, Phe-Lys, Val-Ala, Ala-Leu-Ala-Leu (SEQ ID NO: 2).
3. Konjugat polimer-lijek prema zahtjevima 1-2, naznačen time što je poveznica C1-C10 ugljikovodik ili C1-C10 supstituirani ili hetero supstituirani ugljikovodik, koji sadrži funkcionalnu skupinu koja disocira pod fiziološkim uvjetima, poželjno je navedena funkcionalna skupina odabrana od acetala, estera, imina, amida, disulfida, karbonata, hidrazina, karbamata.
4. Konjugat polimer-lijek prema zahtjevu 1, naznačen time što je poveznica nula i terapeutsko sredstvo D je vezano direktno na polimerni lanac preko esterske, iminske, amidne, disulfidne, karbonatne, karbamatne, hidrazinske veze.
5. Konjugat polimer-lijek prema zahtjevima 1-4, naznačen time što je A krajnja skupina koja je fragment sredstva za prijenos lanca (CTA) ili inicijatora ili fragment CTA ili inicijatora konjugiran s ciljanom skupinom ili fragmentom CTA ili inicijatora koji ima reaktivnu funkcionalnu skupinu, poželjno je da je reaktivna skupina odabrana od acetala, hemiacetala, karboksilne kiseline, alkohola, amida, imida, anhidrida, aril halogenida, azo spoja, diazo spoja, hidrazina, azida, karbonata, klorosilana, cijanida, estera, sulfatnog estera, fosfatnog estera, tiofosfatnog estera, izocijanata, izotiocijanata, tiokarbamatnog estera, ditiokarbamatnog estera.
6. Konjugat polimer-lijek prema zahtjevima 1-5, naznačen time što je B krajnja skupina, koja je fragment sredstva za prijenos lanca ili inicijatora.
7. Konjugat polimer-lijek prema zahtjevu 5, naznačen time što je ciljajući dio odabran iz skupine koja sadrži protutijela; fragmente protutijela ili peptide kao što je Ciklo (Arg-Gly-Asp-D-Phe-Lys) (cRGDfK) (SEQ ID No: 3).
8. Polimerni sastavi (nanočestice ili micele) oblikovani s konjugatima polimer-lijek formule I prema zahtjevima 1-7 [image] pri čemu • Ri, R2 i R3 su neovisno odabrani između H ili -CH3 • x je prirodni broj između 1-100 • y je prirodni broj između 1-100 • n je prirodni broj između 1-50 i • L je poveznica koja se može cijepati ili L može biti nula pri čemu je terapeutsko sredstvo D vezano izravno na polimerni lanac preko esterske, iminske, amidne, disulfidne, karbonatne, karbamatne, hidrazinske veze i • D je terapeutsko sredstvo koje je kombretastatin ili 5-fluorouracil ili gemcitabin ili klorokin ili doksorubicin • A je krajnja skupina ili A može biti nula • B je krajnja skupina ili B može biti nula.
9. Polimerni sastavi (nanočestice ili micele) prema zahtjevu 8 koji inkapsuliraju terapeutska sredstva različita od onih vezanih za konjugat polimer-lijek formule I, pri čemu navedena terapeutska sredstva mogu biti odabrana iz skupine koja sadrži analoge nukleozida, antifolate, druge metabolite, inhibitore topoizomeraze I, antracikline, podofilotoksine, taksane, vinca alkaloide, alkilirajuća sredstva, platinate, antihormone, radio-farmaceutike, monoklonska protutijela, inhibitore tirozin kinaze, inhibitore rapamicina (mTOR) kod sisavaca, retinoide, imunomodulacijska sredstva, inhibitore histonske deacetilaze i druga sredstva.
10. Postupak za pripremu konjugata polimer lijek formule I prema zahtjevima 1-7 koji obuhvaća polimerizaciju PEG (met)akrilatnog monomera (formula II) [image] pri čemu • R1 i R3 su neovisno odabrani između H ili -CH3 • n je prirodni broj između 1-50 da se dobije polimer formule IIa [image] pri čemu • A je krajnja skupina ili A može biti nula • B je krajnja skupina ili B može biti nula i zatim (ii) daljnju reakciju formule IIa s (met)akrilat-L-D monomerom (formula IIIa) [image] pri čemu • R2 je odabran između H ili -CH3 • L je poveznica koja se može cijepati ili L može biti nula pri čemu je terapeutsko sredstvo D vezano izravno na polimerni lanac preko esterske, iminske, amidne, disulfidne, karbonatne, karbamatne, hidrazinske veze • D je terapeutsko sredstvo odabrano između kombretastatina ili 5-FU ili gemcitabina ili klorokina ili doksorubicina da se dobije konjugat polimer-lijek formule I.
11. Postupak za pripremu konjugata polimer lijeka formule I prema zahtjevima 1-7 koji uključuje (i) polimerizaciju PEG (met)akrilatnog monomera (Formula II) [image] pri čemu • R1 i R3 su neovisno odabrani između H ili -CH3 • n je prirodni broj između 1-50 da se dobije polimer formule IIa [image] pri čemu • A je krajnja skupina ili A može biti nula • B je krajnja skupina ili B može biti nula zatim (ii) daljnju reakciju formule IIa s (met)akrilat-L-D monomerom (Formula IIIa) [image] • pri čemu R2 je odabran između H ili -CH3 • L je poveznica koja se može cijepati ili L može biti nula pri čemu je terapeutsko sredstvo D vezano izravno na polimerni lanac preko esterske, iminske, amidne, disulfidne, karbonatne, karbamatne, hidrazinske veze • D je terapeutsko sredstvo odabrano između kombretastatina ili 5-FU ili gemcitabina ili klorokina ili doksorubicina da se dobije blok kopolimer i zatim (iii) reakciju formiranog blok kopolimera s ciljanom skupinom da se dobije konjugat polimer-lijek formule I.
12. Konjugat polimer-lijek formule I prema zahtjevima 1-7 koji se može dobiti postupkom prema zahtjevu 10 ili 11.
13. Farmaceutski pripravak, naznačen time što sadrži konjugat polimer-lijek formule I prema zahtjevima 1-7 i/ili polimerni sastav prema zahtjevima 8-9.
14. Konjugat polimer-lijek formule I prema zahtjevima 1-7, naznačen time što se koristi kao lijek za liječenje i/ili profilaksu raka.
15. Polimerni sastav prema zahtjevima 8-9, naznačen time što je za upotrebu kao lijek za liječenje i/ili profilaksu raka.
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