HRP20171915T1 - Spojevi korisni kao inhibitori atr kinaze i kombinirane terapije koje ih koriste - Google Patents

Spojevi korisni kao inhibitori atr kinaze i kombinirane terapije koje ih koriste Download PDF

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HRP20171915T1
HRP20171915T1 HRP20171915TT HRP20171915T HRP20171915T1 HR P20171915 T1 HRP20171915 T1 HR P20171915T1 HR P20171915T T HRP20171915T T HR P20171915TT HR P20171915 T HRP20171915 T HR P20171915T HR P20171915 T1 HRP20171915 T1 HR P20171915T1
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John Robert Pollard
Philip Michael Reaper
Mohammed ASMAL
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Vertex Pharmaceuticals Incorporated
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Claims (16)

1. Spoj predstavljen sljedećom strukturnom formulom: [image] ili njegova farmaceutski prihvatljiva sol; u kombinaciji s dodatnim terapeutskim sredstvom, naznačen time što navedeno dodatno terapeutsko sredstvo inhibira protein za reparaciju isijecanjem baza; i gdje je protein za reparaciju isijecanjem baza PARP1 ili PARP2; za upotrebu u a) poticanju stanične smrti u tumorskoj stanici kod pacijenta; ili b) povećanju osjetljivosti stanica na sredstva koja oštećuju DNK kod pacijenta.
2. Spoj predstavljen sljedećom strukturnom formulom: [image] ili njegova farmaceutski prihvatljiva sol; u kombinaciji s dodatnim terapeutskim sredstvom, naznačen time što navedeno dodatno terapeutsko sredstvo inhibira protein za reparaciju isijecanjem baza; i gdje je protein za reparaciju isijecanjem baza PARP1 ili PARP2; za upotrebu u liječenju tumora kod pacijenta.
3. Spoj za upotrebu prema patentnom zahtjevu 1 ili 2, gdje spoj predstavlja [image]
4. Spoj za upotrebu prema patentnom zahtjevu 1 ili 2, gdje spoj predstavlja farmaceutski prihvatljivu sol spojeva [image]
5. Spoj ili njegova farmaceutski prihvatljiva sol za upotrebu prema bilo kojem od patentnih zahtjeva 1-4, naznačen time što: a) navedena stanica predstavlja tumorsku stanicu koja ima defekt u ATM signalnoj kaskadi, ili navedena tumorska stanica ili tumor ima defekt u ATM signalnoj kaskadi; na primjer gdje naveden defekt predstavlja izmijenjenu ekspresiju ili aktivnost jednog ili više od sljedećeg: ATM, p53, CHK2, MRE11, RAD50, NBS1, 53BP1, MDC1, H2AX, MCPH1/BRIT1, CTIP, i SMC1; ili b) gdje navedena stanica predstavlja tumorsku stanicu koja eksprimira onkogen koji oštećuje DNK, ili navedena tumorska stanica ili tumor eksprimira onkogen koji oštećuje DNK; na primjer, gdje navedena tumorska stanica, tumor, ili stanica ima izmijenjenu ekspresiju ili aktivnost jednog ili više od sljedećeg: K-Ras, N-Ras, H-Ras, Raf, Myc, Mos, E2F, Cdc25A, CDC4, CDK2, Ciklin E, Ciklin A, i Rb.
6. Spoj ili njegova farmaceutski prihvatljiva sol za upotrebu prema bilo kojem od patentnih zahtjeva 1-5, naznačen time što naveden tumor, tumorska stanica, ili stanica ima defekt u proteinu za reparaciju isijecanjem baza; i gdje je, izborno, protein za reparaciju isijecanjem baza PARP1 ili PARP2.
7. Spoj ili njegova farmaceutski prihvatljiva sol za upotrebu prema bilo kojem od patentnih zahtjeva 1-6, gdje je navedeno dodatno terapeutsko sredstvo Olaparib (također poznat kao AZD2281 ili KU-0059436), Iniparib (također poznat kao BSI-201 ili SAR240550), Veliparib (također poznat kao ABT-888), Rukaparib (također poznat kao PF-01367338), CEP-9722, INO-1001, MK-4827, E7016, BMN673, ili AZD2461.
8. Spoj predstavljen sljedećom strukturnom formulom: [image] ili njegova farmaceutski prihvatljiva sol; u kombinaciji sa dodatnim terapeutskim sredstvom, gdje navedeno dodatno terapeutsko sredstvo inhibira protein za reparaciju isijecanjem baza; i gdje je protein za reparaciju isijecanjem baza PARP1 ili PARP2; za upotrebu a) kao radiosenzibilizator ili hemosenzibilizator kod pacijenta; ili b) u liječenju pacijenta koji ima tumor sa defektom u odgovoru na oštećenje DNK (DDR); na primjer, gdje je naveden defekt mutacija ili gubitak ATM, p53, CHK2, MRE11, RAD50, NBS1, 53BP1, MDC1, H2AX, MCPH1/BRIT1, CTIP, ili SMC1.
9. Spoj za upotrebu prema patentnom zahtjevu 8, gdje je spoj [image]
10. Spoj za upotrebu prema patentnom zahtjevu 8, gdje spoj predstavlja farmaceutski prihvatljivu sol spojeva [image]
11. Spoj ili njegova farmaceutski prihvatljiva sol za upotrebu prema bilo kojem od patentnih zahtjeva 8-10, gdje naveden tumor, tumorska stanica, ili stanica ima defekt u proteinu za reparaciju isijecanjem baza; gdje izborno, protein za reparaciju isijecanjem baza predstavlja PARP1 ili PARP2.
12. Spoj ili njegova farmaceutski prihvatljiva sol za upotrebu prema bilo kojem od patentnih zahtjeva 8-11, gdje je navedeno dodatno terapeutsko sredstvo Olaparib (također poznat kao AZD2281 ili KU-0059436), Iniparib (također poznat kao BSI-201 ili SAR240550), Veliparib (također poznat kao ABT-888), Rukaparib (također poznat kao PF-01367338), CEP-9722, INO-1001, MK-4827, E7016, BMN673, ili AZD2461.
13. Spoj ili njegova farmaceutski prihvatljiva sol za upotrebu prema bilo kojem od patentnih zahtjeva 1-7, gdje navedena stanica ili tumorska stanica predstavlja stanicu izabranu iz grupe koja se sastoji od stanice oralnog tumora, stanice tumora srca, stanice tumora pluća, stanice gastrointestinalnog tumora, stanice tumora genitourinarnog trakta, stanice tumora jetre, stanice tumora kosti, stanice tumora živčanog sustava, stanice ginekološkog tumora, stanice tumora kože, stanice tumora tiroidne žljezde i stanice tumora adrenalne žljezde; na primjer, gdje navedena stanica ili tumorska stanica predstavlja stanicu iz oralnog tumora izabranu iz grupe koja se sastoji od: tumora bukalne šupljine, tumora usne, tumora jezika, tumora usta, i faringealnog tumora; gdje navedena stanica ili tumorska stanica predstavlja stanicu iz tumora srca izabranu iz grupe koja se sastoji od: sarkoma (angiosarkoma, fibrosarkoma, rabdomiosarkoma, liposarkoma), miksoma, rabdomioma, fibroma, lipoma, i teratoma; gdje navedena stanica ili tumorska stanica predstavlja stanicu iz tumora pluća izabranu iz grupe koja se sastoji od: bronhogenih karcinoma (skvamoznih stanica, epidermoidnog karcinoma, nediferenciranih karcinoma malih stanica, nediferenciranih karcinoma velikih stanica, adenokarcinoma), alveolarnog (bronhiolarnog) karcinoma, bronhijalnog adenoma, sarkoma, limfoma, hondromatoznog hamartoma, i mezotelioma; gdje navedena stanica ili tumorska stanica predstavlja stanicu iz gastrointestinalnog tumora izabranu iz grupe koja se sastoji od: ezofagealnog tumora (karcinoma skvamoznih stanica, larinksa, adenokarcinoma, leiomiosarkoma, limfoma), tumora želuca (karcinoma, limfoma, leiomiosarkoma), tumora pankreasa (duktalnog adenokarcinoma, insulinoma, glukagonoma, gastrinoma, karcinoidnih tumora, vipoma), tumora tankog crijeva (adenokarcinoma, limfoma, karcinoidnih tumora, Karpošijevog sarkoma, leiomioma, hemangioma, lipoma, neurofibroma, fibroma), tumora debelog crijeva (adenokarcinoma, tubularnog adenoma, adenoma vilusa, hamartoma, leiomioma), tumora debelog crijeva, tumora debelog crijeva-rektuma, kolorektalnog tumora, i tumora rektuma; gdje navedena stanica ili tumorska stanica predstavlja stanicu iz tumora genitourinarnog trakta izabranu iz grupe koja se sastoji od: tumora bubrega (adenokarcinoma, Vilmsovog tumora [nefroblastoma], limfoma), tumora mokraćnog mjehura, uretralnog tumora (karcinoma skvamoznih stanica, karcinoma prijelaznih stanica, adenokarcinoma), tumora prostate (adenokarcinoma, sarkoma), i tumora testisa (seminoma, teratoma, embrionalnog karcinoma, teratokarcinoma, horiokarcinoma, sarkoma, karcinoma interstitialnih stanica, fibroma, fibroadenoma, adenomatoidnih tumora, lipoma); gdje navedena stanica ili tumorska stanica predstavlja stanicu iz tumora jetre izabranu iz grupe koja se sastoji od: hepatoma (hepatocelularnog karcinoma), holangiokarcinoma, hepatoblastoma, angiosarkoma, hepatocelularnog adenoma, hemangioma, i tumora žučnih puteva; gdje navedena stanica ili tumorska stanica predstavlja stanicu iz tumora kosti izabrana iz grupe koja se sastoji od: osteogenog sarkoma (osteosarkoma), fibrosarkoma, malignog fibroznog histiocitoma, hondrosarkoma, Juingovog sarkoma, malignog limfoma (sarkoma retikularnih stanica), multiplog mijeloma, malignog tumora hordoma s gigantskim stanicama, osteohondroma (koštano-hrskavičave egzostoze), benignog hondroma, hondroblastoma, hondromiksofibroma, osteoidnog osteoma, i tumora gigantskih stanica; gdje navedena stanica ili tumorska stanica predstavlja stanicu iz tumora živčanog sustava izabranu iz grupe koja se sastoji od: tumora lubanje (osteoma, hemangioma, granuloma, ksantoma, osteitisa deformansa), meningealnog tumora (meningioma, meningiosarkoma, gliomatoze), tumora mozga (astrocitoma, meduloblastoma, glioma, ependimoma, germinoma [pinealoma], multiformnog glioblastoma, oligodendroglioma, švanoma, retinoblastoma, kongenitalnih tumora), tumora leđne moždine, neurofibroma, meningioma, glioma, i sarkoma; gdje navedena stanica ili tumorska stanica predstavlja stanicu iz ginekološkog tumora izabranu iz grupe koja se sastoji od: tumora maternice (endometrijalnog karcinoma), cervikalnog tumora (cervikalnog karcinoma, pretumorske cervikalne displazije), tumora jajnika (karcinoma jajnika [seroznog cistadenokarcinoma, mukoznog cistadenokarcinoma, neklasificiranog karcinoma], tumora granulozno-tekućih stanica, tumora Sertoli-Leydig-ovih stanica, disgerminoma, malignog teratoma), tumora vulve (karcinoma skvamoznih stanica, intraepitelijalnog karcinoma, adenokarcinoma, fibrosarkoma, melanoma), vaginalnih tumora (karcinoma bistrih stanica, karcinoma skvamoznih stanica, botrioidnog sarkoma (embrionalnog rabdomiosarkoma), tumora Falopijevih tuba (karcinoma), i tumora dojke; gdje navedena stanica ili tumorska stanica predstavlja stanicu iz tumora kože izabranu iz grupe koja se sastoji od: malignog melanoma, karcinoma bazalnih stanica, karcinoma skvamoznih stanica, Karpošijevog sarkoma, keratoakantoma, displastičnih madeža, lipoma, angioma, i dermatofibroma; gdje navedena stanica ili tumorska stanica predstavlja stanicu iz tumora tiroidne žljezde izabranu iz grupe koja se sastoji od: papilarnog tiroidnog karcinoma, folikularnog tiroidnog karcinoma; medularnog tiroidnog karcinoma, multiple endokrine neoplazije tipa 2A, multiple endokrine neoplazije tipa 2B, familijanog medularnog tiroidnog tumora, feohromocitoma, i paraganglioma; i gdje navedena stanica ili tumorska stanica predstavlja stanicu iz tumora adrenalnih žljezda i izborno naveden tumor adrenalnih žljezda predstavlja neuroblastom; na primjer, gdje navedena stanica ili tumorska stanica predstavlja stanicu iz tumora pluća ili tumora pankreasa; gdje navedena stanica ili tumorska stanica predstavlja stanicu iz tumora pluća, tumora glave i vrata, tumora pankreasa, tumora želuca, ili tumora mozga; ili gdje navedena stanica ili tumorska stanica predstavlja stanicu iz nesitnostaničnog tumora pluća, sitnostaničnog tumora pluća, tumora pankreasa, tumora žučnih puteva, tumora glave i vrata, tumora mokraćnog mjehura, kolorektalnog tumora, glioblastoma, ezofagealnog tumora, tumora dojke, hepatocelularnog karcinoma, ili tumora jajnika.
14. Spoj ili njegova farmaceutski prihvatljiva sol za upotrebu prema bilo kojem od patentnih zahtjeva 8-12, gdje je naveden tumor solidni tumor izabran iz grupe koja se sastoji od: oralnog tumora, tumora srca, tumora pluća, gastrointestinalnog tumora, tumora genitourinarnog trakta, tumora jetre, tumora kosti, tumora živčanog sustava, ginekološkog tumora, tumora kože, tumora tiroidne žljezde i tumora adrenalne žljezde; na primjer, gdje naveden tumor predstavlja oralni tumor izabran iz grupe koja se sastoji od: tumora bukalne šupljine, tumora usne, tumora jezika, tumora usta, i faringealnog tumora; gdje naveden tumor predstavlja tumor srca izabran iz grupe koja se sastoji od: sarkoma (angiosarkoma, fibrosarkoma, rabdomiosarkoma, liposarkoma), miksoma, rabdomioma, fibroma, lipoma, i teratoma; gdje naveden tumor predstavlja tumor pluća izabran iz grupe koja se sastoji od: bronhogenih karcinoma (skvamoznih stanica, epidermoidnog karcinoma, nediferenciranih karcinoma malih stanica, nediferenciranih karcinoma velikih stanica, adenokarcinoma), alveolarnog (bronhiolarnog) karcinoma, bronhijalnog adenoma, sarkoma, limfoma, hondromatoznog hamartoma, i mezotelioma; gdje naveden tumor predstavlja gastrointestinalni tumor izabran iz grupe koja se sastoji od: ezofagealnog tumora (karcinoma skvamoznih stanica, larinksa, adenokarcinoma, leiomiosarkoma, limfoma), tumora želuca (karcinoma, limfoma, leiomiosarkoma), tumora pankreasa (duktalnog adenokarcinoma, insulinoma, glukagonoma, gastrinoma, karcinoidnih tumora, vipoma), tumora tankog crijeva (adenokarcinoma, limfoma, karcinoidnih tumora, Karpošijevog sarkoma, leiomioma, hemangioma, lipoma, neurofibroma, fibroma), tumora debelog crijeva (adenokarcinoma, tubularnog adenoma, adenoma vilusa, hamartoma, leiomioma), tumora debelog crijeva, tumora debelog crijeva-rektuma, kolorektalnog tumora, i tumora rektuma; gdje naveden tumor predstavlja tumor genitourinarnog trakta izabran iz grupe koja se sastoji od: tumora bubrega (adenokarcinoma, Vilmsovog tumora [nefroblastoma], limfoma), tumora mokraćnog mjehura, uretralnog tumora (karcinoma skvamoznih stanica, karcinoma prijelaznih stanica, adenokarcinoma), tumora prostate (adenokarcinoma, sarkoma), i tumora testisa (seminoma, teratoma, embrionalnog karcinoma, teratokarcinoma, horiokarcinoma, sarkoma, karcinoma interstitialnih stanica, fibroma, fibroadenoma, adenomatoidnih tumora, lipoma); gdje naveden tumor predstavlja tumor jetre izabran iz grupe koja se sastoji od: hepatoma (hepatocelularnog karcinoma), holangiokarcinoma, hepatoblastoma, angiosarkoma, hepatocelularnog adenoma, hemangioma, i tumora žučnih puteva; gdje naveden tumor predstavlja tumor kosti izabran iz grupe koja se sastoji od: osteogenog sarkoma (osteosarkoma), fibrosarkoma, malignog fibroznog histiocitoma, hondrosarkoma, Juingovog sarkoma, malignog limfoma (sarkoma retikularnih stanica), multiplog mijeloma, malignog tumora hordoma sa gigantskim stanicama, osteohronfroma (koštano-hrskavičave egzostoze), benignog hondroma, hondroblastoma, hondromiksofibroma, osteoidnog osteoma, i tumora gigantskih stanica; gdje gdje naveden tumor predstavlja tumor živčanog sustava izabran iz grupe koja se sastoji od: tumora lubanje (osteoma, hemangioma, granuloma, ksantoma, osteitisa deformansa), meningealnog tumora (meningioma, meningiosarkoma, gliomatoze), tumora mozga (astrocitoma, meduloblastoma, glioma, ependimoma, germinoma [pinealoma], multiformnog glioblastoma, oligodendroglioma, švanoma, retinoblastoma, kongenitalnih tumora), tumora kičmene moždine, neurofibroma, meningioma, glioma, i sarkoma; gdje naveden tumor predstavlja ginekološki tumor izabran iz grupe koja se sastoji od: tumora maternice (endometrijalnog karcinoma), cervikalnog tumora (cervikalnog karcinoma, pretumorske cervikalne displazije), tumora jajnika (karcinoma jajnika [seroznog cistadenokarcinoma, mukoznog cistadenokarcinoma, neklasificiranog karcinoma], tumora granulozno-tekalnih stanica, tumora Sertoli-Leydig-ovih stanica, disgerminoma, malignog teratoma), tumora vulve (karcinoma skvamoznih stanica, intraepitelijalnog karcinoma, adenokarcinoma, fibrosarkoma, melanoma), vaginalnih tumora (karcinoma bistrih stanica, karcinoma skvamoznih stanica, botrioidnog sarkoma (embrionalnog rabdomiosarkoma), tumora Falopijevih tuba (karcinoma), i tumora dojke; gdje naveden tumor predstavlja tumor kože izabran iz grupe koja se sastoji od: malignog melanoma, karcinoma bazalnih stanica, karcinoma skvamoznih stanica, Karpošijevog sarkoma, keratoakantoma, displastičnih mladeža, lipoma, angioma, i dermatofibroma; gdje naveden tumor predstavlja tumor tiroidne žljezde izabran iz grupe koja se sastoji od: papilarnog tiroidnog karcinoma, folikularnog tiroidnog karcinoma; medularnog tiroidnog karcinoma, multiple endokrine neoplazije tipa 2A, multiple endokrine neoplazije tipa 2B, familijanog medularnog tiroidnog tumora, feohromocitoma, i paraganglioma; i gdje naveden tumor adrenalnih žlezda predstavlja neuroblastom; na primjer, gdje naveden tumor predstavlja tumor pluća ili pankreasa; gdje naveden tumor predstavlja tumor pluća, tumor glave i vrata, tumor pankreasa, tumor želuca, ili tumor mozga; ili gdje naveden tumor predstavlja nesitnostanični tumor pluća, sitnostanični tumor pluća, tumor pankreasa, tumor žučnih puteva, tumor glave i vrata, tumor mokraćnog mjehura, kolorektalni tumor, glioblastom, ezofagealni tumor, tumor dojke, hepatocelularni karcinom, ili tumor jajnika.
15. Spoj ili njegova farmaceutski prihvatljiva sol za upotrebu u liječenju tumora prema bilo kojem od patentnih zahtjeva 2-7, gdje naveden tumor predstavlja solidni tumor izabran iz grupe koja se sastoji od: oralnog tumora, tumora srca, tumora pluća, gastrointestinalnog tumora, tumora genitourinarnog trakta, tumora jetre, tumora kosti, tumora živčanog sustava, ginekološkog tumora, tumora kože, tumora tiroidne žljezde i tumora adrenalne žljezde; na primjer, gdje naveden tumor predstavlja oralni tumor izabran iz grupe koja se sastoji od: tumora bukalne šupljine, tumora usne, tumora jezika, tumora usta, i faringealnog tumora; gdje naveden tumor predstavlja tumor srca izabran iz grupe koja se sastoji od: sarkoma (angiosarkoma, fibrosarkoma, rabdomiosarkoma, liposarkoma), miksoma, rabdomioma, fibroma, lipoma, i teratoma; gdje naveden tumor predstavlja tumor pluća izabran iz grupe koja se sastoji od: bronhogenih karcinoma (skvamoznih stanica, epidermoidnog karcinoma, nediferenciranih karcinoma malih stanica, nediferenciranih karcinoma velikih stanica, adenokarcinoma), alveolarnog (bronhiolarnog) karcinoma, bronhijalnog adenoma, sarkoma, limfoma, hondromatoznog hamartoma, i mezotelioma; gdje naveden tumor predstavlja gastrointestinalni tumor izabran iz grupe koja se sastoji od: ezofagealnog tumora (karcinoma skvamoznih stanica, larinksa, adenokarcinoma, leiomiosarkoma, limfoma), tumora želuca (karcinoma, limfoma, leiomiosarkoma), tumora pankreasa (duktalnog adenokarcinoma, insulinoma, glukagonoma, gastrinoma, karcinoidnih tumora, vipoma), tumora tankog crijeva (adenokarcinoma, limfoma, karcinoidnih tumora, Karpošijevog sarkoma, leiomioma, hemangioma, lipoma, neurofibroma, fibroma), tumora debelog crijeva (adenokarcinoma, tubularnog adenoma, adenoma vilusa, hamartoma, leiomioma), tumora debelog crijeva, tumora debelog crijeva-rektuma, kolorektalnog tumora, i tumora rektuma; gdje naveden tumor predstavlja tumor genitourinarnog trakta izabran iz grupe koja se sastoji od: tumora bubrega (adenokarcinoma, Vilmsovog tumora [nefroblastoma], limfoma), tumora mokraćnog mjehura, uretralnog tumora (karcinoma skvamoznih stanica, karcinoma prelaznih stanica, adenokarcinoma), tumora prostate (adenokarcinoma, sarkoma), i tumora testisa (seminoma, teratoma, embrionalnog karcinoma, teratokarcinoma, horiokarcinoma, sarkoma, karcinoma interstitialnih stanica, fibroma, fibroadenoma, adenomatoidnih tumora, lipoma); gdje naveden tumor predstavlja tumor jetre izabran iz grupe koja se sastoji od: hepatoma (hepatocelularnog karcinoma), holangiokarcinoma, hepatoblastoma, angiosarkoma, hepatocelularnog adenoma, hemangioma, i tumora žučnih puteva; gdje naveden tumor predstavlja tumor kosti izabran iz grupe koja se sastoji od: osteogenog sarkoma (osteosarkoma), fibrosarkoma, malignog fibroznog histiocitoma, hondrosarkoma, Juingovog sarkoma, malignog limfoma (sarkoma retikularnih stanica), multiplog mijeloma, malignog tumora hordoma sa gigantskim stanicama, osteohronfroma (koštano-hrskavičave egzostoze), benignog hondroma, hondroblastoma, hondromiksofibroma, osteoidnog osteoma, i tumora gigantskih stanica; gdje naveden tumor predstavlja tumor živčanog sustava izabran iz grupe koja se sastoji od: tumora lubanje (osteoma, hemangioma, granuloma, ksantoma, osteitisa deformansa), meningealnog tumora (meningioma, meningiosarkoma, gliomatoze), tumora mozga (astrocitoma, meduloblastoma, glioma, ependimoma, germinoma [pinealoma], multiformnog glioblastoma, oligodendroglioma, švanoma, retinoblastoma, kongenitalnih tumora), tumora kičmene moždine, neurofibroma, meningioma, glioma, i sarkoma; gdje naveden tumor predstavlja ginekološki tumor izabran iz grupe koja se sastoji od: tumora maternice (endometrijalnog karcinoma), cervikalnog tumora (cervikalnog karcinoma, pretumorske cervikalne displazije), tumora jajnika (karcinoma jajnika [seroznog cistadenokarcinoma, mukoznog cistadenokarcinoma, neklasificiranog karcinoma], tumora granulozno-tekalnih stanica, tumora Sertoli-Leydig-ovih stanica, disgerminoma, malignog teratoma), tumora vulve (karcinoma skvamoznih stanica, intraepitelijalnog karcinoma, adenokarcinoma, fibrosarkoma, melanoma), vaginalnih tumora (karcinoma bistrih stanica, karcinoma skvamoznih stanica, botrioidnog sarkoma (embrionalnog rabdomiosarkoma), tumora Falopijevih tuba (karcinoma), i tumora dojke; gdje naveden tumor predstavlja tumor kože izabran iz grupe koja se sastoji od: malignog melanoma, karcinoma bazalnih stanica, karcinoma skvamoznih stanica, Karpošijevog sarkoma, keratoakantoma, displastičnih mladeža, lipoma, angioma, i dermatofibroma; gdje naveden tumor predstavlja tumor tiroidne žljezde izabran iz grupe koja se sastoji od: papilarnog tiroidnog karcinoma, folikularnog tiroidnog karcinoma; medularnog tiroidnog karcinoma, multiple endokrine neoplazije tipa 2A, multiple endokrine neoplazije tipa 2B, familijanog medularnog tiroidnog tumora, feohromocitoma, i paraganglioma; i gdje naveden tumor adrenalnih žlezda predstavlja neuroblastom; na primjer, gdje naveden tumor predstavlja tumor pluća ili pankreasa; gdje naveden tumor predstavlja tumor pluća, tumor glave i vrata, tumor pankreasa, tumor želuca, ili tumor mozga; ili gdje naveden tumor predstavlja nesitnostanični tumor pluća, sitnostanični tumor pluća, tumor pankreasa, tumor žučnih puteva, tumor glave i vrata, tumor mokraćnog mjehura, kolorektalni tumor, glioblastom, ezofagealni tumor, tumor dojke, hepatocelularni karcinom, ili tumor jajnika.
16. Spoj ili njegova farmaceutski prihvatljiva sol za upotrebu prema bilo kojem od patentnih zahtjeva 1-15, u kombinaciji sa sredstvom koje oštećuje DNK; gdje je navedeno sredstvo koje oštećuje DNK prikladno za bolest koja se liječi; i navedeno sredstvo koje oštećuje DNK je zajedno sa navedenim spojem u vidu pojedinačnog doznog oblika ili odvojeno od navedenog spoja kao dio višedoznog oblika; na primjer, gdje je navedeno sredstvo koje oštećuje DNK hemoterapija ili zračna terapija; izborno, gdje je navedeno sredstvo koje oštećuje DNK ionizirajuće zračenje, radiomimetik neokarzinostatin, sredstvo na bazi platine, inhibitor Topo I, inhibitor Topo II, antimetabolit, alkilirajuće sredstvo, alkil sulfonati, ili antibiotik; na primjer, gdje je navedeno sredstvo na bazi platine cisplatin, oksaliplatin, karboplatin, nedaplatin, Lobaplatin, triplatin tetranitrat, pikoplatin, satraplatin, proLindak, ili aroplatin; naveden inhibitor Topo I je kamptotecin, topotekan, irinotekan/SN38, rubitekan, ili belotekan; naveden inhibitor Topo II je etopozid, daunorubicin, doksorubicin, aklarubicin, epirubicin, idarubicin, amrubicin, pirarubicin, valrubicin, zorubicin, ili tenipozid; naveden antimetabolit je aminopterin, metotreksat, pemetreksed, raltitreksed, pentostatin, kladribin, klofarabin, fludarabin, tioguanin, merkaptopurin, 6-merkaptopurin, fluorouracil, 5-fluorouracil, kapecitabin, tegafur, karmofur, floksuridin, citarabin, gemcitabin, azacitidin, ili hidroksiurea; navedeno alkilirajuće sredstvo je izabrano iz grupe koja se sastoji od azotnih iperita, nitrozourea, triazena, alkil sulfonata, prokarbazina, aziridina; mekloretamina, ciklofosfamida, ifosfamida, trofosfamida, klorambucila, melfalana, prednimustina, bendamustina, uramustina, estramustina, karmustina, lomustina, semustina, fotemustina, nimustina, ranimustina, streptozocina, busulfana, manosulfana, treosulfana, karbokvona, tioTEPA, triazikvona, trietilenmelamina, prokarbazina, dakarbazina, temozolomida, altretamina, i mitobronitola; i naveden antibiotik je izabran iz grupe koja se sastoji od hidroksiuree, antraciklina, antracenediona, antibiotika iz porodice Streptomyces, aktinomicina, bleomicina, mitomicina, i plikamicina; na primjer, gdje navedeno sredstvo koje oštećuje DNK predstavlja jedno ili više od sljedećeg: cisplatin, karboplatin, gemcitabin, etopozid, temozolomid, i ionizirajućeg zračenja
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