HRP20211386T1 - Sredstva sa visokim afinitetom za ciljano djelovanje na membranski antigen specifičan za prostatu za endoradioterapiju raka prostate - Google Patents

Sredstva sa visokim afinitetom za ciljano djelovanje na membranski antigen specifičan za prostatu za endoradioterapiju raka prostate Download PDF

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HRP20211386T1
HRP20211386T1 HRP20211386TT HRP20211386T HRP20211386T1 HR P20211386 T1 HRP20211386 T1 HR P20211386T1 HR P20211386T T HRP20211386T T HR P20211386TT HR P20211386 T HRP20211386 T HR P20211386T HR P20211386 T1 HRP20211386 T1 HR P20211386T1
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tumors
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Sangeeta Ray
Martin G. Pomper
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The Johns Hopkins University
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    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
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    • A61P13/00Drugs for disorders of the urinary system
    • A61P13/08Drugs for disorders of the urinary system of the prostate
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
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Claims (12)

1. Spoj formule (I): [image] naznačen time da: Z je tetrazol ili CO2Q; Q je H ili zaštitna grupa, pri čemu je zaštitna grupa odabrana iz grupe koja se sastoji od benzila, p-metoksibenzila (PMB), tercijarnog butila (t-Bu), metoksimetila (MOM), metoksietoksimetila (MEM), metiltiometila (MTM), tetrahidropiranila (THP), tetrahidrofuranila (THF), benziloksimetila (BOM), trimetilsilila (TMS), trietilsilila (TES), t-butildimetilsilila (TBDMS), i trifenilmetila (tritil, Tr); m je cijeli broj odabran iz grupe koja se sastoji od 1, 2, 3, 4, i 5; R je -CH2-R1; R1 je odabran iz grupe koja se sastoji od: [image] pri čemu je X neovisno Br ili I; L je veznik odabran iz grupe koja se sastoji od C1-C6 alkilena i C3-C6 cikloalkilena, i arilena; W je odabran iz grupe koja se sastoji od -NR2-(C=O)-, -NR2-(C=S)-, -(C=O)-NR2-, i -(C=S)-NR2-; pri čemu u svakom pojavljivanju L i W može biti isti ili različit; R2 je H ili C1-C4 alkil; n je cijeli broj odabran iz grupe koja se sastoji od 1, 2, i 3; i Ch je kelatno sredstvo koje sadrži radiometal odabran iz grupe koja se sastoji od 68Ga, 64Cu, 86Y, 90Y, 89Zr, 111In, 99mTc, 177Lu, 153Sm, 186Re, 188Re, 67Cu, 212Pb, 225Ac, 213Bi, 212Bi, 212Pb, 67Ga, 203Pb, 47Sc, i 166Ho, pri čemu je kelatno sredstvo odabrano iz grupe koja se sastoji od: [image] [image] [image] i njegovih farmaceutski prihvatljivih soli.
2. Spoj prema patentnom zahtjevu 1, naznačen time da je spoj formule (I) odabran iz grupe koja se sastoji od: [image] [image] [image] [image] [image] [image] [image] [image] [image] [image] [image] i [image]
3. Spoj formule (I) za uporabu u liječenju jednog ili više tumora ili stanica koje eksprimiraju membranski antigen specifičan za prostatu (PSMA), naznačen time da spoj formule (I) sadrži: [image] pri čemu: Z je tetrazol ili CO2Q; Q je H ili zaštitna grupa, pri čemu je zaštitna grupa odabrana iz grupe koja se sastoji od benzila, p-metoksibenzila (PMB), tercijarnog butila (t-Bu), metoksimetila (MOM), metoksietoksimetila (MEM), metiltiometila (MTM), tetrahidropiranila (THP), tetrahidrofuranila (THF), benziloksimetila (BOM), trimetilsilila (TMS), trietilsilila (TES), t-butildimetilsilila (TBDMS), i trifenilmetila (tritil, Tr); m je cijeli broj odabran iz grupe koja se sastoji od 1, 2, 3, 4, i 5; R je -CH2-R1; R1 je odabran iz grupe koja se sastoji od: [image] pri čemu je X neovisno Br ili I; L je veznik odabran iz grupe koja se sastoji od C1-C6 alkilena i C3-C6 cikloalkilena, i arilena; W je odabran iz grupe koja se sastoji od -NR2-(C=O)-, -NR2-(C=S)-, -(C=O)-NR2-, i -(C=S)-NR2-; pri čemu u svakom pojavljivanju L i W može biti isti ili različit; R2 je H ili C1-C4 alkil; n je cijeli broj odabran iz grupe koja se sastoji od 1, 2, i 3; i Ch je kelatno sredstvo koje sadrži radiometal odabran iz grupe koja se sastoji od 68Ga, 64Cu, 86Y, 90Y, 89Zr, 111In, 99mTc, 177Lu, 153Sm, 186Re, 188Re, 67Cu, 212Pb, 225Ac, 213Bi, 212Bi, 212Pb, 67Ga, 203Pb, 47Sc, i 166Ho, pri čemu je kelatno sredstvo odabrano iz grupe koja se sastoji od: [image] [image] [image] i njihovih farmaceutski prihvatljivih soli.
4. Spoj za uporabu prema patentnom zahtjevu 3, naznačen time da je spoj odabran iz grupe koja se sastoji od: [image] [image] [image] [image] [image] [image] [image] [image] [image] [image] i [image]
5. Spoj za uporabu prema patentnom zahtjevu 3 ili patentnom zahtjevu 4, naznačen time da je jedan ili više tumora ili stanica koje eksprimiraju PSMA odabran iz grupe koja se sastoji od: tumora ili stanica prostate, metastaziranog tumora ili stanica prostate, tumora ili stanica pluća, tumora ili stanica bubrega, glioblastoma, tumora ili stanica gušterače, tumora ili stanica mjehura, sarkoma, melanoma, tumora ili stanica dojke, tumora ili stanica debelog crijeva, germinativnih stanica, feokromocitoma, tumora ili stanica jednjaka, tumora ili stanica želuca, i njihovih kombinacija.
6. Spoj za uporabu prema patentnom zahtjevu 3 ili patentnom zahtjevu 4, naznačen time da jedan ili više tumora ili stanica koje eksprimiraju PSMA su tumor ili stanice prostate.
7. Spoj za uporabu prema patentnom zahtjevu 3 ili patentnom zahtjevu 4, naznačen time da liječenje rezultira u inhibiciji rasta tumora.
8. Postupak za liječenje jednog ili više tumora ili stanica koje eksprimiraju membranski antigen specifičan za prostatu (PSMA) in vitro ili ex vivo, naznačen time da postupak sadrži kontaktiranje jednog ili više in vitro ili ex vivo tumora ili stanica koje eksprimiraju PSMA sa efikasnom količinom spoja formule (I), pri čemu spoj formule (I) sadrži: [image] pri čemu: Z je tetrazol ili CO2Q; Q je H ili zaštitna grupa, pri čemu je zaštitna grupa odabrana iz grupe koja se sastoji od benzila, p-metoksibenzial (PMB), tercijarnog butila (t-Bu), metoksimetila (MOM), metoksietoksimetila (MEM), metiltiometila (MTM), tetrahidropiranila (THP), tetrahidrofuranila (THF), benziloksimetila (BOM), trimetilsilila (TMS), trietilsilila (TES), t-butildimetilsilila (TBDMS), i trifenilmetila (tritil, Tr); m je cijeli broj odabran iz grupe koja se sastoji od 1, 2, 3, 4, i 5; R je -CH2-R1; R1 je odabran iz grupe koja se sastoji od: [image] pri čemu je X neovisno Br ili I; L je veznik odabran iz grupe koja se sastoji od C1-C6 alkilena i C3-C6 cikloalkilena, i arilena; W je odabran iz grupe koja se sastoji od -NR2-(C=O)-, -NR2-(C=S)-, -(C=O)-NR2-, i -(C=S)-NR2-; pri čemu u svakom pojavljivanju L i W može biti isti ili različit; R2 je H ili C1-C4 alkil; n je cijeli broj odabran iz grupe koja se sastoji od 1, 2, i 3; i Ch je kelatno sredstvo koje sadrži radiometal odabran iz grupe koja se sastoji od 68Ga, 64Cu, 86Y, 90Y, 89Zr, 111In, 99mTc, 177Lu, 153Sm, 186Re, 188Re, 67Cu, 212Pb, 225Ac, 213Bi, 212Bi, 212Pb, 67Ga, 203Pb, 47Sc, i 166Ho, pri čemu je kelatno sredstvo odabrano iz grupe koja se sastoji od: [image] [image] [image] i njihovih farmaceutski prihvatljivih soli.
9. Postupak prema patentnom zahtjevu 8, naznačen time da je spoj odabrano iz grupe koja se sastoji od: [image] [image] [image] [image] [image] [image] [image] [image] [image] [image] [image] [image] [image] [image] [image] [image] i [image]
10. Postupak prema patentnom zahtjevu 8, naznačen time da je jedan ili više tumora ili stanica koje eksprimiraju PSMA odabrano iz grupe koja se sastoji od: tumora ili stanica prostate, metastaziranog tumora ili stanica prostate, tumora ili stanica pluća, tumora ili stanica bubrega, glioblastoma, tumora ili stanica gušterače, tumora ili stanica mjehura, sarkoma, melanoma, tumora ili stanica dojke, tumora ili stanica debelog crijeva, germinativnih stanica, feokromocitoma, tumora ili stanica jednjaka, tumora ili stanica želuca, i njihovih kombinacija.
11. Postupak prema patentnom zahtjevu 8, naznačen time da jedan ili više tumora ili stanica koje eksprimiraju PSMA su tumor ili stanice prostate.
12. Postupak prema patentnom zahtjevu 8, naznačen time da liječenje rezultira u inhibiciji rasta tumora.
HRP20211386TT 2016-03-22 2021-08-31 Sredstva sa visokim afinitetom za ciljano djelovanje na membranski antigen specifičan za prostatu za endoradioterapiju raka prostate HRP20211386T1 (hr)

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US201662311697P 2016-03-22 2016-03-22
PCT/US2017/023508 WO2017165473A1 (en) 2016-03-22 2017-03-22 Prostate-specific membrane antigen targeted high-affinity agents for endoradiotherapy of prostate cancer
EP17771028.2A EP3433238B1 (en) 2016-03-22 2017-03-22 Prostate-specific membrane antigen targeted high-affinity agents for endoradiotherapy of prostate cancer

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HRP20211386TT HRP20211386T1 (hr) 2016-03-22 2021-08-31 Sredstva sa visokim afinitetom za ciljano djelovanje na membranski antigen specifičan za prostatu za endoradioterapiju raka prostate

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US (2) US11458213B2 (hr)
EP (3) EP3925952B1 (hr)
JP (3) JP7073270B2 (hr)
KR (3) KR20220063298A (hr)
CN (2) CN109311827B (hr)
AU (1) AU2017238181B2 (hr)
BR (1) BR112018069507A2 (hr)
CA (1) CA3018709A1 (hr)
CL (1) CL2018002683A1 (hr)
CY (1) CY1124487T1 (hr)
DK (2) DK3433238T3 (hr)
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FI (1) FI3925952T3 (hr)
HR (2) HRP20240215T1 (hr)
HU (2) HUE055607T2 (hr)
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MX (1) MX2018011519A (hr)
PH (1) PH12018502048A1 (hr)
PL (2) PL3925952T3 (hr)
PT (2) PT3433238T (hr)
RS (2) RS62274B1 (hr)
RU (2) RU2021115958A (hr)
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SI (2) SI3433238T1 (hr)
TR (1) TR201813644T1 (hr)
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