SI2833973T1 - Spojine uporabne kot inhibitorji ATR kinaze in njihove kombinacijske terapije - Google Patents
Spojine uporabne kot inhibitorji ATR kinaze in njihove kombinacijske terapije Download PDFInfo
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- SI2833973T1 SI2833973T1 SI201330879T SI201330879T SI2833973T1 SI 2833973 T1 SI2833973 T1 SI 2833973T1 SI 201330879 T SI201330879 T SI 201330879T SI 201330879 T SI201330879 T SI 201330879T SI 2833973 T1 SI2833973 T1 SI 2833973T1
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Claims (16)
- SPOJINE UPORABNE KOT INHIBITORJI ATR KINAZE IN NJIHOVE KOMBINACIJSKE TERAPIJE PATENTNI ZAHTEVKI1. Spojina, ki jo predstavlja naslednja strukturna formula:ali njena farmacevtsko sprejemljiva sol; v kombinaciji z dodatnim terapevtskim sredstvom, kjer omenjeno dodatno terapevtsko sredstvo zavira protein za osnovno popravljanje z izrezovanjem; in kjer je protein za osnovno popravljanje z izrezovanjem PARP1 ali PARP2; za uporabo v a) spodbujanje celične smrti v rakavi celici pri pacientu; ali b) preobčutljivosti celic na DNK škodljive snovi pri pacientu.
- 2. Spojina, ki jo predstavlja naslednja strukturna formula:ali njena farmacevtsko sprejemljiva sol; v kombinaciji z dodatnim terapevtskim sredstvom, kjer omenjeno dodatno terapevtsko sredstvo zavira protein za osnovno popravljanje z izrezovanjem; in kjer je protein za osnovno popravljanje z izrezovanjem PARP1 ali PARP2; za uporabo pri zdravljenju raka pri pacientu.
- 3. Spojina za uporabo po zahtevku 1 ali 2, kjer je spojina
- 4. Spojina za uporabo po zahtevku 1 ali 2, kjer je spojina farmacevtsko sprejemljiva sol
- 5. Spojina ali njena farmacevtsko sprejemljiva sol za uporabo po katerem koli od zahtevkov 1-4, kjer: a) omenjena celica je rakava celica, ki ima napako v ATM signalizacijski kaskadi ali pa ima omenjena rakava celica ali rak napako v ATM signalizacijski kaskadi; na primer pri čemer je omenjena napaka spremenjeno izražanje ali aktivnost ene ali več od naslednjih: ATM, p53, CHK2, MRE11, RAD50, NBS1, 53BP1, MDC1, Η2ΑΧ, MCPH1 / BRIT 1, CTIP in SMC1; ali b) pri čemer je omenjena celica rakava celica, ki izraža onkogen, ki poškoduje DNA, ali rakava celica ali rak izraža onkogen, ki poškoduje DNA; na primer, kjer je omenjena rakava celica, rak ali celica spremenila ekspresijo ali aktivnost enega ali več izmed naslednjih: K-Ras, N-Ras, Η-Ras, Raf, Myc, Mos, E2F, Cdc25A, CDC4, CDK2, Ciklin E, Ciklin A in Rb.
- 6. Spojina ali njena farmacevtsko sprejemljiva sol za uporabo po katerem koli od zahtevkov 1-5, kjer ima omenjeni rak, rakava celica ali celica ima napako v proteinu za osnovno popravljanje z izrezovanjem; in po izbiri, kjer je protein za osnovno popravljanje z izrezovanjem PARP1 ali PARP2.
- 7. Spojina ali njena farmacevtsko sprejemljiva sol za uporabo po katerem koli od zahtevkov 1-6, kjer je omenjeno dodatno terapevtsko sredstvo Olaparib (znan tudi kot AZD2281 ali KU-0059436), Iniparib (znan tudi kot BSI-201 ali SAR240550), Veliparib (znan tudi kot ABT-888), Rucaparib (znano tudi kot PF-01367338), CEP-9722, INO-1001, MK-4827, E7016, BMN673 ali AZD2461.
- 8. Spojina, ki jo predstavlja naslednja strukturna formula:ali njena farmacevtsko sprejemljiva sol; v kombinaciji z dodatnim terapevtskim sredstvom, kjer omenjeno dodatno terapevtsko sredstvo zavira protein za osnovno popravljanje z izrezovanjem; in kjer je protein za osnovno popravljanje z izrezovanjem PARP1 ali PARP2; za uporabo a) kot radio-senzibilizator ali kemo-senzibilizator; ali b) pri zdravljenju pacienta z rakom z napako odziva DNA-poškodbo (DDR); na primer, kjer je omenjena napaka mutacija ali izguba ATM, p53, CHK2, MRE11, RAD50, NBS1, 53BP1, MDC1, Η2ΑΧ, MCPH1/BRIT1, CTIP, ali SMC1.
- 9. Spojina za uporabo po zahtevku 8, kjer je spojina
- 10. Spojina za uporabo po zahtevku 8, kjer je spojina farmacevtsko sprejemljiva sol
- 11. Spojina ali njena farmacevtsko sprejemljiva sol za uporabo po katerem koli od zahtevkov 8-10, kjer omenjeni rak, rakava celica ali celica ima napako v proteinu za osnovno popravljanje z izrezovanjem; po izbiri pri čemer je protein za osnovno popravljanje z izrezovanjem PARP1 ali PARP2.
- 12. Spojina ali njena farmacevtsko sprejemljiva sol za uporabo po katerem koli od zahtevkov 8-11, kjer je omenjeno dodatno terapevtsko sredstvo Olaparib (znan tudi kot AZD2281 ali KU-0059436), Iniparib (znan tudi kot BSI-201 ali SAR240550), Veliparib (znan tudi kot ABT-888), Rucaparib (znano tudi kot PF-01367338), CEP-9722, INO-1001, MK-4827, E7016, BMN673 ali AZD2461.
- 13. Spojina ali njena farmacevtsko sprejemljiva sol za uporabo po katerem koli od zahtevkov 1-7, kjer je omenjena celica ali rakava celica celica, izbrana iz skupine, ki jo sestavljajo peroralna rakava celica, kardialna rakava celica, pljučna rakava celica, gastrointestinalna rakava celica, rakava celica genitourinamih poti, jetrna rakava celica, rakava celica kosti, rakava celica živčnega sistema, ginekološka rakava celica, rakava celica kože, rakava celica ščitnične žleze in rakava celica nadledvične žleze; na primer, kjer je navedena celica ali rakava celica celica izmed peroralnega raka, izbrana iz skupine, ki jo sestavljajo; rak bukalne votline, rak ustnic, rak jezika, rak ust in faringealni rak; kjer je navedena celica ali rakava celica celica izmed kardialnega raka, izbrana iz skupine, ki jo sestavljajo: sarkomi (angiosarkomi, fibrosarkomi, rabdomiosarkomi, liposarkomi), mioksomi, rabdomiomi, fibromi, lipomi, in teratomi; kjer je navedena celica ali rakava celica celica izmed pljučnega raka, izbrana iz skupine, ki jo sestavljajo: bronhogeni karcinomi (skvamozna celica, epidermoidni karcinom, nediferencirani drobno celični karcinomi, nediferencirani veliki celični karcinom, adenokarcinomi), alveolami (bronhiolarni) karcinom, bronhialni adenom, sarkom, limfom, hondromatski hamartom in mezoteliom; kjer je navedena celica ali rakava celica celica izmed gastrointestinalnega raka, izbrana iz skupine, ki jo sestavljajo: ezofagealni rak (karcinom skvamoznih celic, grla, adenokarcinom, leiomiosarkom, limfom), rak želodca (karcinom, limfom, leiomiosarkom), rak trebušne slinavke (duktalni adenokarcinom, insulinom, glukagonom, gastrinom, karcinoidni tumorji, vipom), rak tankega črevesa ali ozkega črevesa (adenokarcinom, limfom, karcinoid tumorji, Karposijev sarkom, leiomiom, hemangiom, lipom, nevrofibrom, fibrom), rak debelega črevesa ali širokega črevesa (adenokarcinom, tubularni adenom, venski adenom, hamartom, leiomiom), rak kolona, rak kolon-rektum, kolorektalni rak in rak rektuma; kjer je omenjena celica ali rakava celica celica izmed raka genitourinarnega trakta, izbrana iz skupine, ki jo sestavljajo: ledvični rak (adenokarcinom, Wilmov tumor [nefroblastom], limfom), rak sečnega mehurja, uretralni rak (karcinom skvamoznih celic, prehodno celični karcinom, adenokarcinom), rak prostate (adenokarcinom, sarkom), in rak testisa (seminom, teratom, embrionalni karcinom, teratokarcinom, horiokarcinom, sarkom, intersticijski celični karcinom, fibrom, fibroadenom, adenomatoidni tumorji, lipom); kjer je omenjena celica ali rakava celica celica iz raka jeter, izbrana iz skupine, ki jo sestavljajo: hepatoma (hepatocelularni karcinom), holangiokarcinom, hepatoblastom, angiosarkomom, hepatocelularni adenom, hemangiom in rak biliamih prehodov; kjer je omenjena celica ali rakava celica celica iz raka kosti, izbranega iz skupine, ki jo sestavljajo: osteogeni sarkom (osteosarkom), fibrosarkomom, maligni fibrozni histiocitom, hondrosarkomom, Evvingov sarkomom, maligni limfom (retikulum celični sarkom), multipli mielom, maligni gigantsko celični tumorn hordom, »osteochronfroma«, (osteokartilaginozne eksostoze), benigni hndrome, hondroblastom, hondromiksofibrom, osteoidni osteom in tumorji gigantskih celic; kjer je omenjena celica ali rakava celica celica raka živčnega sistema, izbrana iz skupine, ki jo sestavljajo: rak lobanje (osteom, hemangiom, granulom, ksantom, osteitis deformans), meningealni rak (meningiom, meningiosarkom, gliomatoza), možganski rak (astrocitom, meduloblastom, gliom, ependimom, germinom [pinealomj, glioblastom multiform, oligodendrogliom, Schvvannoma, retinoblastom, kongenitalni tumorji), rak hrbtenjače, nevrofibrom, meningiom, gliom in sarkom; kjer je omenjena celia ali rakava celica celica ginekološkega raka, izbrana iz skupine, ki jo sestavljajo: rak maternice (endometrijski karcinom), rak materničnega vratu (karcinom materničnega vratu, pred-tumor displazija materničnega vratu), rak jajčnikov (karcinom jajčnikov [serozni cistadenokarcinom, mucinozni cistadenokarcinom, nerazvrščeni karcinom], granuloza-tekalni celični tumorji, tumorji celic Sertoli-Leydig, disgerminom, maligni teratom), vulvami rak (skvamozni celični karcinom, intraepitelijski karcinom, adenokarcinom, fibrosarkom, melanom), vaginalni rak (čista celica karcinom, skvamozno celični karcinom, botrioidni sarkom (embrionalni rabdomiosarkom), rak jajcevodne tubule (karcinom) in rak dojke; kjer je navedena celica ali rakava celica celica kožnega raka, izbranega iz skupine ki jo sestavljajo: maligni melanom, karcinom bazalnih celic, karcinom skvamoznih celic, Karposijev sarkom, keratoakantom, moli displastični nevusi, lipom, angiom in dermatofibrom; kjer je omenjena celica ali rakava celica celica raka ščitnične žleze, izbrane iz skupine, ki jo sestavljajo: papilarni karcinom ščitnice, folikularni karcinom ščitnice; medulami karcinom ščitnice, multipla endokrina neoplazija tipa 2A, multipla endokrina neoplazija tipa 2B, familialnega medularni ščitnični rak, feohromocitom in paragangliom; in kjer je omenjena celica ali rakava celica celica raka nadledvične žleze in po izbiri je omenjeni rak nadledvične žleze nevroblastom; na primer, kjer je omenjena celica ali rakava celica celica raka pljuč ali raka trebušne slinavke; kjer je omenjena celica ali rakava celica celica pljučnega raka, raka glave in vratu, raka trebušne slinavke, raka želodca, ali možganskega raka; ali kjer je omenjena celica ali rakava celica celica ne-drobnoceličnega pljučnega raka, drobnoceličnega pljučnega raka, raka trebušne slinavke, raka biliamega trakta, raka glave in vratu, raka sečnega mehurja, kolorektalnega raka, glioblastoma, ezofagealnega raka, rak dojk, hepatocelulamega karcinoma ali raka jajčnikov.
- 14. Spojina ali njena farmacevtsko sprejemljiva sol za uporabo po katerem koli od zahtevkov 8-12, kjer omenjeni rak je solidni tumor, izbran iz skupine, ki jo sestavljajo; ustni rak, kardialni rak, pljučni rak, gastrointestinalni rak, rak genitourinarnega trakta, rak jeter, kostni rak, rak živčnega sistema, ginekološki rak, kožni rak, rak ščitnične žleze ali rak nadledvične žleze; na primer, kjer je omenjeni rak oralni rak izbran iz skupine, ki jo sestavljajo: rak bukalne votline, rak ustnic, rak jezika, raka ust in faringealni rak; kjer je omenjeni rak kardialni rak, izbran iz skupine, ki jo sestavljajo; sarkom (angiosarkom, fibrosarkom, rabdomiosarkom, liposarkom), miksom, rabdomiom, fibrom, lipom in teratom; kjer je omenjeni rak pljučni rak, izbran iz skupine, ki jo sestavljajo: bronhogenski karcinom (skvamozno celični ali epidermoidna, nediferenciran drobnocelični, nediferenciran veliko celični, adenokarcinom), alveolaren (bronhiolaen) karcinom, bronhialni adenom, sarkom, limfom, hondromatski hamartom in mezoteliom; kjer je omenjeni rak gastrointestinalni rak, izbran iz skupine, ki jo sestavljajo: ezofagealni rak (skvamozni celični karcinom, larinksa, adenokarcinom, leiomiosarkom, limfom), rak želodca (karcinom, limfom, leiomiosarkom), rak trebušne slinavke (duktalni adenokarcinom, insulinom, glukagonom, gastrinom, karcinoidni tumorji, vipom), rak tankega črevesa ali ozkega črevesa (adenokarcinom, limfom, karcinoidni tumorji, Karposijev sarkom, leiomiom, hemangiom, lipom, nevrofibrom, fibrom), rak debelega črevesa ali širokega črevesa (adenokarcinom, tubulami adenom, vilozni adenom, hamartom, leiomiom), rak kolona, rak kolon-rektum, kolorektalni rak; in rak rektuma; kjer je navedeni rak rak genitourinamega trakta, izbran iz skupine, ki jo sestavljajo: ledvični rak (adenokarcinom, VVilmov tumor [nefroblastom], limfom), rak sečnega mehurja in uretralen rak (skvamozni celični karcinom, prehodno celični karcinom, adenokarcinom), rak prostate (adenokarcinom, sarkom), in rak testisa (seminom, teratom, embrionalni karcinom, teratokarcinom, horiokarcinom, sarkom, intersticijski celični karcinom, fibrom, fibroadenom, adenomatoidni tumorji, lipom); kjer je rak rak jeter, izbran iz skupine, ki jo sestavljajo: hepatom (hepatocelularni karcinom), holangiokarcinom, hepatoblastom, angiosarkom, hepatocelularni adenom, hemangiom in rak biliarnih prehodov; kjer je navedeni rak kostni rak izbran iz skupine, ki jo sestavljajo: osteogeni sarkom (osteosarkom), fibrosarkom, maligni fibrozni histiocitom, hondrosarkom, Evvingov sarkom, maligni limfom (retikulum celični sarkom), multipli mielom, maligni gigantocelični tumor hordom, osteochronfroma (osteocartilaginous exostoses), benigni hondrom, hondroblastom, hondromiksofibrom, osteoidni osteom in tumorji gigantskih celic; kjer je omenjeni rak rak živčnega sistema, izbran iz skupine, ki jo sestavljajo: rak lobanje (osteom, hemangiom, granulom, ksantom, osteitis deformans), meningealnega raka (meningiom, meningiosarkom, gliomatoza), raka možganov (astrocitom, meduloblastom, gliom, ependimom, germinom [pinealom], glioblastom multiform, oligodendrogliom, Schvvannoma, retinoblastom, kongenitalni tumorji), rak hrbtenjače, nevrofibrom, meningiom, gliom in sarkom; kjer je omenjeni rak ginekološki rak, izbran iz skupine, ki jo sestavljajo: rak maternice (endometrialni karcinom), rak materničnega vratu (karcinom materničnega vratu, pred-tumorska displazija materničnega vratu), rak jajčnikov (karcinom jajčnikov [serozni cistadenokarcinom, mucinozni cistadenokarcinom, nerazvrščeni karcinom], tumorji granuloznih-tekalnih celic, tumorji celic Sertoli-Leydig, disgerminom, maligni teratom), vulvami rak (karcinom skvamoznih celic, intraepitelijski karcinom, adenokarcinom, fibrosarkom, melanom), vaginalni rak (svetlocelični karcinom, skvamozno celični karcinom, botrioidni sarkom (embrionalni rabdomiosarkom), jajcevodni rak (karcinom) in rak na dojki; kjer je omenjeni rak rak kože, izbran iz skupine, ki jo sestavljajo: maligni melanom, karcinom bazalnih celic, karcinom skvamoznih celic, Karposijev sarkom, keratoakanthoma, moli displastični nevusi, lipom, angiom in dermatofibrom; kjer je omenjeni rak rak ščitnične žleze, izbran iz skupine, ki jo sestavljajo: papilarni karcinom ščitnice, folikularni karcinom ščitnice, medularni ščitnični karcinom, multipla endokrina neoplazija tipa 2A, multipla endokrina neoplazija tipa 2B, familialni medularni rak ščitnice, feohromocitom in paragangliom; in kjer je rak nadledvične žleze nevroblastom; na primer, kjer je omenjeni rak rak pljuč ali trebušne slinavke; kjer je navedeni rak pljučni rak, glave in rak vratu, rak trebušne slinavke, rak želodca ali rak na možganih; ali kjer je omenjeni rak nedrobnocelični pljučni rak, drobnocelični pljučni rak, rak trebušne slinavke, rak biliarnega trakta, rak glave in vratu, rak mehurja, kolorektalni rak, glioblastom, ezofagealni rak, rak dojk, hepatocelularni karcinom ali rak jajčnikov.
- 15. Spojina ali njena farmacevtsko sprejemljiva sol za uporabo pri zdravljenju raka, kot je zahtevano v katerem koli izmed po zahtevku 2-7, kjer je rak soliden tumor, izbran iz skupine, ki jo sestavljajo: oralni rak, kardialni rak, pljučni rak, gastrointestinalni rak, rak genitourinarnega trakta, rak jeter, rak kosti, rak živčevnega sistema, ginekološki rak, kožni rak, rak ščitnične žleze ali rak nadledvične žleze; na primer, kjer je omenjeni rak oralni rak izbran iz skupine, ki jo sestavljajo: rak bukalne votline, rak ustnic, rak jezika, rak ust in faringealni rak; kjer je omenjeni rak kardialni rak, izbran iz skupine, ki jo sestavljajo: sarkom (angiosarkom, fibrosarkom, rabdomiosarkom, liposarkom), miksom, rabdomiom, fibrom, lipom in teratom; kjer je omenjeni rak pljučni rak, izbran iz skupine, ki jo sestavljajo: bronhogenski karcinom (skvamozno celični ali epidermoidni, nediferenciran drobnocelični, nediferenciran veliko celični, adenokarcinom), aiveolaren (bronhiolaren) karcinom, bronhialni adenom, sarkom, limfom, hondromatski hamartom in mezoteliom; kjer je omenjeni rak gastrointestinalni rak, izbran iz skupine, ki jo sestavljajo: ezofagealni rak (skvamozno celični karcinom, larinksa, adenokarcinom, leiomiosarkom, limfom), rak želodca (karcinom, limfom, leiomiosarkom), rak trebušne slinavke (duktalni adenokarcinom, insulinom, glukagonom, gastrinom, karcinoidni tumorji, vipom), rak tankega črevesa ali ozkega črevesa (adenokarcinom, limfom, karcinoidni tumorji, Karposijev sarkom, leiomiom, hemangiom, lipom, nevrofibrom, fibrom), rak debelega črevesa ali širokega črevesa (adenokarcinom, tubulami adenom, villous adenom, hamartom, leiomiom), rak kolona, rak kolon-rektum, kolorektalni rak; in rak rektuma; kjer je navedeni rak rak genitourinamega trakta, izbran iz skupine, ki jo sestavljajo: ledvični rak (adenokarcinom, Wilmov tumor [nefroblastom], limfom), rak sečnega mehurja in uretralni rak (skvamozni celični karcinom, prehodni celični karcinom, adenokarcinom), rak prostate (adenokarcinom, sarkom), in rak testisa (seminom, teratom, embrionalni karcinom, teratokarcinom, horiokarcinom, sarkom, intersticijski celični karcinom, fibrom, fibroadenoa, adenomatoidni tumorji, lipom); kjer je rak rak jeter izbran iz skupine, ki jo sestavljajo: hepatom (hepatocelularni karcinom), holangiokarcinom, hepatoblastom, angiosarkom, hepatocelularni adenom, hemangiom in rak biliarnih prehodov; kjer je navedeni rak kostni rak izbran iz skupine, ki jo sestavljajo: osteogeni sarkom (osteosarkom), fibrosarkom, maligni fibrozni histiocitom, hondrosarkom, Evvingov sarkom, maligni limfom (retikulum celični sarkom), multipli mielom, maligni gigantsko celični tumor hordom, osteochronfroma (osteocartilaginous exostoses), benigni hondrom, hondroblastom, hondromiksofibrom, osteoidni osteom in tumorji gigantskih celic; kjer je omenjeni rak rak živčnega sistema, izbran iz skupine, ki jo sestavljajo: rak lobanje (osteom, hemangiom, granulom, ksantom, osteitis deformans), meningealni rak (meningiom, meningiosarkom, gliomatoza), rak možganov (astrocitom, meduloblastom, gliom, ependimom, germinom [pinealom], multiformni glioblastom, oligodendrogliom, Schvvannoma, retinoblastom, kongenitalni tumorji), rak hrbtenjače, nevrofibrom, meningiom, gliom in sarkom; kjer je omenjeni rak ginekološki rak, izbran iz skupine, ki jo sestavljajo: rak maternice (endometrijski karcinom), rak materničnega vratu (karcinom materničnega vratu, pred-tumorska displazija materničnega vratu), rak jajčnikov (karcinom jajčnikov [serozni cistadenokarcinom, mucinozni cistadenokarcinom, nerazvrščeni karcinom], tumorji granuloznih-tekalnih celic, tumorji celic Sertoli-Leydig, disgerminom, maligni teratom), vulvami rak (karcinom skvamoznih celic, intraepitelijski karcinom, adenokarcinom, fibrosarkom, melanom), vaginalni rak (svetlocelični karcinom, skvamozno celični karcinom, botrioidni sarkom (embrionalni rabdomiosarkom), jajcevodni rak (karcinom) in rak na dojki; kjer je omenjeni rak rak kože, izbran iz skupine, ki jo sestavljajo: maligni melanom, karcinom bazalnih celic, karcinom skvamoznih celic, Karposijev sarkom, keratoakantom, moli displastični nevusi, lipom, angiom in dermatofibrom; kjer je omenjeni rak rak ščitnične žleze, izbran iz skupine, ki jo sestavljajo: papilarni karcinom ščitnice, folikularni karcinom ščitnice, medularni ščitnični karcinom, multipla endokrina neoplazija tipa 2A, multipla endokrina neoplazija tipa 2B, familialni medularni rak ščitnice, feohromocitom in paragangliom; in kjer je omenjeni rak nadledvične žleze nevroblastom; na primer, kjer je omenjeni rak rak pljuč ali trebušne slinavke; kjer je navedeni rak pljučni rak, rak glave in vratu, rak trebušne slinavke, rak želodca ali rak na možganih; ali kjer je omenjeni rak nedrobnocelični pljučni rak, drobnocelični pljučni rak, rak trebušne slinavke, rak biliarnega trakta, rak glave in vratu, rak mehurja, kolorektalni rak, glioblastom.ezofagealni rak, rak dojk, hepatocelularni karcinom ali rak jajčnikov.
- 16. Spojina ali njena farmacevtsko sprejemljiva sol za uporabo po katerem koli od zahtevkov 1-15 v kombinaciji z DNA-škodljivim sredstvom; kjer je omenjeno DNA-škodljivo sredstvo primerno za bolezen, ki se jo zdravi; in omenjeno DNA-škodljivo sredstvo skupaj z navedeno spojino kot eno odmerno obliko ali ločeno od omenjene spojine kot del večkratne dozirne oblike; na primer, kjer je omenjeno DNA-škodljivo sredstvo kemoterapija ali sevalna obravnava; po izbiri, kjer je DNA-škodljivo sredstvo ionizirajoče sevanje, radiomimetični neokarzinostatin, platinimo sredstvo, inhibitor Topo I, inhibitor Topo II, antimetabolit, alkilirno sredstvo, alkil sulfonati ali antibiotik; na primer, kjer je navedeno platinimo sredstvo cisplatin, oksaliplatin, karboplatin, nedaplatin, Lobaplatin, triplatin tetranitrat, pikoplatin, satraplatin, proLindac ali aroplatin; omenjeni inhibitor Topo I je kamptotecin, topotekan, irinotekan/SN38, rubitecan ali belotecan; omenjeni inhibitor Topo II je etoposid, daunorubicin, doksorubicin, aklarubicin, epirubicin, idarubicin, amrubicin, pirarubicin, valrubicin, zorubicin ali tenipozid; navedeni antimetabolit je aminopterin, metotreksat, pemetreksed, raltitreksed, pentostatin, kladribin, klofarabin, fludarabin, tioguanin, merkaptopurin, 6-merkaptopurin, fluorouracil, 5-fluorouracil, kapecitabin, tegafur, karmofur, floksuridin, citarabin, gemcitabin, azacitidin ali hidroksisečnina; omenjeno alkilirno sredstvo se izbere iz skupine, ki jo sestavljajo dušikov iperit, nitrozoureji, triazeni, alkil sulfonati, prokarbazin, aziridini; mekloretamin, ciklofosfamid, ifosfamid, trofosfamid, klorambucil, melfalan, prednimustin, bendamustin, uramustin, estramustin, karmustin, lomustin, semustin, fotemustin, nimustin, ranimustin, streptozocin, busulfan, manosulfan, treosulfan, karboun, tioTEPA, triazikon, trietilenmelamin, prokarbazin, dakarbazin, temozolomid, altretamin in mitobronitol; in omenjeni antibiotik se izbere iz skupine, ki jo sestavljajo hidroksisečnina, antraciklini, antracenedioni, antibiotiki iz družine Streptomyces, aktinomicin, bleomicin, mitomicin, in plikamicin; na primer, kjer je DNA-škodljivo sredstvo eno ali več od naslednjih: cisplatin, karboplatin, gemcitabin, etoposid, temozolomid in ionizirajoče sevanje.
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Families Citing this family (33)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
RS56995B1 (sr) | 2008-12-19 | 2018-05-31 | Vertex Pharma | Derivati pirazina korisni kao inhibitori atr kinaze |
JP5836367B2 (ja) | 2010-05-12 | 2015-12-24 | バーテックス ファーマシューティカルズ インコーポレイテッドVertex Pharmaceuticals Incorporated | Atrキナーゼ阻害剤として有用な化合物 |
US9334244B2 (en) | 2010-05-12 | 2016-05-10 | Vertex Pharmaceuticals Incorporated | Compounds useful as inhibitors of ATR kinase |
AU2012315615A1 (en) | 2011-09-30 | 2014-04-17 | Vertex Pharmaceuticals Incorporated | Processes for making compounds useful as inhibitors of ATR kinase |
CN108464983A (zh) | 2011-09-30 | 2018-08-31 | 沃泰克斯药物股份有限公司 | 用atr抑制剂治疗胰腺癌和非小细胞肺癌 |
DK2833973T3 (en) | 2012-04-05 | 2018-01-02 | Vertex Pharma | Compounds useful as ATR kinase inhibitors and combination therapies thereof |
EP2904406B1 (en) | 2012-10-04 | 2018-03-21 | Vertex Pharmaceuticals Incorporated | Method for measuring atr inhibition mediated increases in dna damage |
LT3486245T (lt) | 2012-12-07 | 2021-08-25 | Vertex Pharmaceuticals Incorporated | 2-amino-n-(piperidin-1-il-piridin-3-il)pirazolo[1,5alfa]pirimidin-3-karboksamidas, kaip atr kinazės inhibitorius |
AP2015008604A0 (en) | 2013-01-23 | 2015-07-31 | Astrazeneca Ab | Chemical compounds |
AU2014360380B2 (en) | 2013-12-06 | 2019-03-21 | Vertex Pharmaceuticals Incorporated | 2-amino-6-fluoro-n-[5-fluoro-pyridin-3-yl]pyrazolo[1,5-a]pyrimidin-3-carboxamide compound useful as ATR kinase inhibitor, its preparation, different solid forms and radiolabelled derivatives thereof |
AU2015271030B2 (en) | 2014-06-05 | 2019-05-16 | Vertex Pharmaceuticals Incorporated | Radiolabelled derivatives of a 2-amino-6-fluoro-n-[5-fluoro-pyridin-3-yl]- pyrazolo [1,5-a] pyrimidin-3-carboxamide compound useful as ATR kinase inhibitor, the preparation of said compound and different solid forms thereof |
KR20170016498A (ko) | 2014-06-17 | 2017-02-13 | 버텍스 파마슈티칼스 인코포레이티드 | Chk1 및 atr 저해제의 병용물을 사용하는 암의 치료 방법 |
TWI700283B (zh) | 2014-08-04 | 2020-08-01 | 德商拜耳製藥公司 | 2-(嗎啉-4-基)-1,7-萘啶 |
SG11201700265VA (en) | 2014-08-22 | 2017-02-27 | Clovis Oncology Inc | High dosage strength tablets of rucaparib |
MX395066B (es) * | 2015-09-30 | 2025-03-24 | Vertex Pharma | Método para tratar cáncer usando una combinación de agentes que dañan el adn e inhibidores de proteína relacionada con ataxia telangiectasia y rad3 (atr). |
US12233060B2 (en) * | 2016-01-08 | 2025-02-25 | The Institute Of Cancer Research: Royal Cancer Hospital | Inhibitors of Ataxia-Telangiectasia Mutated and Rad3-related protein kinase (ATR) for use in methods of treating cancer |
JP6918829B2 (ja) | 2016-01-11 | 2021-08-11 | メリマック ファーマシューティカルズ インコーポレーティッド | 血管拡張性失調症及びRad3関連タンパク質(ATR)の阻害 |
SMT202200173T1 (it) | 2016-06-01 | 2022-05-12 | Athira Pharma Inc | Composti |
AR110995A1 (es) | 2017-02-24 | 2019-05-22 | Bayer Ag | Combinación de inhibidores de quinasa atr con sal de radio-223 |
WO2018153972A1 (en) | 2017-02-24 | 2018-08-30 | Bayer Pharma Aktiengesellschaft | Combination of atr kinase inhibitors and antiandrogens |
JOP20190197A1 (ar) | 2017-02-24 | 2019-08-22 | Bayer Pharma AG | مثبط كيناز ايه تي آر للاستخدام في طريقة لعلاج مرض فرط التكاثر |
US11439623B2 (en) | 2017-04-04 | 2022-09-13 | Case Western Reserve University | Method of modulating ribonucleotide reductase |
WO2018206547A1 (en) | 2017-05-12 | 2018-11-15 | Bayer Pharma Aktiengesellschaft | Combination of bub1 and atr inhibitors |
US11690911B2 (en) | 2017-08-04 | 2023-07-04 | Bayer Aktiengesellschaft | Combination of ATR kinase inhibitors and PD-1/PD-L1 inhibitors |
EP3461480A1 (en) | 2017-09-27 | 2019-04-03 | Onxeo | Combination of a dna damage response cell cycle checkpoint inhibitors and belinostat for treating cancer |
US11712440B2 (en) | 2017-12-08 | 2023-08-01 | Bayer Aktiengesellschaft | Predictive markers for ATR kinase inhibitors |
EP3856251B1 (en) | 2018-09-26 | 2024-10-09 | Merck Patent GmbH | Combination of a pd-1 antagonist, an atr inhibitor and a platinating agent for the treatment of cancer |
AU2019360608A1 (en) | 2018-10-15 | 2021-06-03 | Merck Patent Gmbh | Combination therapy utilizing DNA alkylating agents and ATR inhibitors |
CA3116230A1 (en) | 2018-10-16 | 2020-04-23 | Bayer Aktiengesellschaft | Combination of atr kinase inhibitors with 2,3-dihydroimidazo[1,2-c]quinazoline compounds |
SG11202104460UA (en) | 2018-10-30 | 2021-05-28 | Repare Therapeutics Inc | Compounds, pharmaceutical compositions, and methods of preparing compounds and of their use as atr kinase inhibitors |
US20220249531A1 (en) * | 2019-07-26 | 2022-08-11 | Health Research, Inc. | Treatment of p53-deficient cancers |
US12128050B2 (en) | 2020-11-10 | 2024-10-29 | New Mexico Tech University Research Park Corporation | KP372-1-induced DNA damage as a chemotherapeutic approach to treat cancer |
CN117024413B (zh) * | 2023-10-07 | 2024-01-09 | 天津匠新致成科技有限公司 | 3-氨基吡嗪-2-甲酰胺类靶向蛋白水解嵌合体及其制备方法、药物组合物和应用 |
Family Cites Families (218)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
US4309430A (en) | 1980-06-27 | 1982-01-05 | Merck & Co., Inc. | Pyrazinyl-1,2,4-oxadiazole-5-ones, for treatment of edema, and processes for preparing same |
JPS62270623A (ja) | 1985-12-07 | 1987-11-25 | Daicel Chem Ind Ltd | ビス(4−アミノフエニル)ピラジンおよびその製法、ならびにポリイミドおよびその製法 |
JPS63208520A (ja) | 1987-02-26 | 1988-08-30 | Terumo Corp | ピラジン誘導体を含有する血小板凝集抑制剤 |
US5329012A (en) | 1987-10-29 | 1994-07-12 | The Research Foundation Of State University Of New York | Bis(acyloxmethyl)imidazole compounds |
JPH0272370A (ja) | 1988-09-07 | 1990-03-12 | Konica Corp | 電子写真感光体 |
JPH0272372A (ja) | 1988-09-07 | 1990-03-12 | Konica Corp | 電子写真感光体 |
JPH0374370A (ja) | 1989-08-16 | 1991-03-28 | Terumo Corp | ピラジン誘導体およびこれを含有する血小板凝集抑制剤または抗炎症剤 |
JP2597917B2 (ja) | 1990-04-26 | 1997-04-09 | 富士写真フイルム株式会社 | 新規な色素形成カプラー及びそれを用いたハロゲン化銀カラー写真感光材料 |
US5572248A (en) | 1994-09-19 | 1996-11-05 | Teleport Corporation | Teleconferencing method and system for providing face-to-face, non-animated teleconference environment |
CA2253910A1 (en) | 1996-05-11 | 1997-11-20 | King's College London | Pyrazines |
JP4026876B2 (ja) | 1996-09-05 | 2007-12-26 | 日本食品化工株式会社 | 発光性シクロデキストリン誘導体及びその製造方法 |
JP2002241379A (ja) | 1997-03-21 | 2002-08-28 | Dainippon Pharmaceut Co Ltd | 3−オキサジアゾリルキノキサリン誘導体 |
WO1999044609A1 (en) | 1998-03-03 | 1999-09-10 | Merck & Co., Inc. | FUSED PIPERIDINE SUBSTITUTED ARYLSULFONAMIDES AS β3-AGONISTS |
DE19826671A1 (de) | 1998-06-16 | 1999-12-23 | Hoechst Schering Agrevo Gmbh | 1,3-Oxazolin- und 1,3-Thiazolin-Derivate, Verfahren zu ihrer Herstellung und ihre Verwendung als Schädlingsbekämpfungsmittel |
JP3910365B2 (ja) | 1998-07-16 | 2007-04-25 | 塩野義製薬株式会社 | 抗腫瘍活性を有するピリミジン誘導体 |
US7023913B1 (en) | 2000-06-14 | 2006-04-04 | Monroe David A | Digital security multimedia sensor |
DK1150999T3 (da) | 1999-02-05 | 2006-10-30 | Debiopharm Sa | Cyclosporinderivater og fremgangsmåde til fremstilling deraf |
US6738073B2 (en) | 1999-05-12 | 2004-05-18 | Imove, Inc. | Camera system with both a wide angle view and a high resolution view |
WO2000076982A1 (en) | 1999-06-16 | 2000-12-21 | University Of Iowa Research Foundation | Antagonism of immunostimulatory cpg-oligonucleotides by 4-aminoquinolines and other weak bases |
US7015954B1 (en) | 1999-08-09 | 2006-03-21 | Fuji Xerox Co., Ltd. | Automatic video system using multiple cameras |
US6660753B2 (en) | 1999-08-19 | 2003-12-09 | Nps Pharmaceuticals, Inc. | Heteropolycyclic compounds and their use as metabotropic glutamate receptor antagonists |
DE60037905T2 (de) | 1999-12-17 | 2009-01-29 | Novartis Vaccines and Diagnostics, Inc., Emeryville | Pyrazin-basierte hemmer der glycogen-synthase-kinase 3 |
US6849660B1 (en) | 2000-08-01 | 2005-02-01 | Isis Pharmaceuticals, Inc. | Antimicrobial biaryl compounds |
US6829391B2 (en) | 2000-09-08 | 2004-12-07 | Siemens Corporate Research, Inc. | Adaptive resolution system and method for providing efficient low bit rate transmission of image data for distributed applications |
EP1217000A1 (en) | 2000-12-23 | 2002-06-26 | Aventis Pharma Deutschland GmbH | Inhibitors of factor Xa and factor VIIa |
US8085293B2 (en) | 2001-03-14 | 2011-12-27 | Koninklijke Philips Electronics N.V. | Self adjusting stereo camera system |
US6759657B2 (en) | 2001-03-27 | 2004-07-06 | Kabushiki Kaisha Toshiba | Infrared sensor |
JPWO2002080899A1 (ja) | 2001-03-30 | 2005-01-06 | エーザイ株式会社 | 消化器疾患治療剤 |
US6469002B1 (en) | 2001-04-19 | 2002-10-22 | Millennium Pharmaceuticals, Inc. | Imidazolidine compounds |
CA2446380A1 (en) | 2001-05-08 | 2002-11-14 | Yale University | Proteomimetic compounds and methods |
SE0102438D0 (sv) | 2001-07-05 | 2001-07-05 | Astrazeneca Ab | New compounds |
SE0102439D0 (sv) | 2001-07-05 | 2001-07-05 | Astrazeneca Ab | New compounds |
USRE40794E1 (en) | 2001-09-26 | 2009-06-23 | Merck & Co., Inc. | Crystalline forms of carbapenem antibiotics and methods of preparation |
GB0124939D0 (en) | 2001-10-17 | 2001-12-05 | Glaxo Group Ltd | Chemical compounds |
EP1446387B1 (en) | 2001-11-21 | 2009-11-04 | Pharmacia & Upjohn Company LLC | Substituted aryl 1,4-pyrazine derivatives |
US6992087B2 (en) | 2001-11-21 | 2006-01-31 | Pfizer Inc | Substituted aryl 1,4-pyrazine derivatives |
US20030187026A1 (en) | 2001-12-13 | 2003-10-02 | Qun Li | Kinase inhibitors |
JP4656838B2 (ja) | 2002-02-06 | 2011-03-23 | バーテックス ファーマシューティカルズ インコーポレイテッド | Gsk−3の阻害剤として有用なヘテロアリール化合物 |
US7205304B2 (en) | 2002-03-13 | 2007-04-17 | Janssen Pharmaceutica N.V. | Sulfonyl-Derivatives as novel inhibitors of histone deacetylase |
GB0206860D0 (en) | 2002-03-22 | 2002-05-01 | Glaxo Group Ltd | Compounds |
TWI319387B (en) | 2002-04-05 | 2010-01-11 | Astrazeneca Ab | Benzamide derivatives |
US7043079B2 (en) | 2002-04-25 | 2006-05-09 | Microsoft Corporation | “Don't care” pixel interpolation |
GB0209715D0 (en) | 2002-04-27 | 2002-06-05 | Astrazeneca Ab | Chemical compounds |
US7704995B2 (en) | 2002-05-03 | 2010-04-27 | Exelixis, Inc. | Protein kinase modulators and methods of use |
JP4901102B2 (ja) | 2002-05-03 | 2012-03-21 | エクセリクシス, インク. | プロテインキナーゼモジュレーターおよびその使用方法 |
CA2482838A1 (en) | 2002-05-31 | 2003-12-11 | Eisai Co., Ltd. | Pyrazole compounds and pharmaceutical compositions containing the compound |
AU2003245669A1 (en) | 2002-06-21 | 2004-01-06 | Cellular Genomics, Inc. | Certain aromatic monocycles as kinase modulators |
AU2003249369A1 (en) | 2002-06-21 | 2004-01-06 | Cellular Genomics, Inc. | Certain amino-substituted monocycles as kinase modulators |
WO2004033431A2 (en) | 2002-10-04 | 2004-04-22 | Arena Pharmaceuticals, Inc. | Hydroxypyrazoles for use against metabolic-related disorders |
US20040075741A1 (en) | 2002-10-17 | 2004-04-22 | Berkey Thomas F. | Multiple camera image multiplexer |
US7385626B2 (en) | 2002-10-21 | 2008-06-10 | Sarnoff Corporation | Method and system for performing surveillance |
US20040100560A1 (en) | 2002-11-22 | 2004-05-27 | Stavely Donald J. | Tracking digital zoom in a digital video camera |
SE0203754D0 (sv) | 2002-12-17 | 2002-12-17 | Astrazeneca Ab | New compounds |
SE0203752D0 (sv) | 2002-12-17 | 2002-12-17 | Astrazeneca Ab | New compounds |
DK2476667T3 (da) | 2003-02-26 | 2014-09-15 | Sugen Inc | Aminoheteroaryl-forbindelser som proteinkinase-inhibitorer |
US7684624B2 (en) | 2003-03-03 | 2010-03-23 | Smart Technologies Ulc | System and method for capturing images of a target area on which information is recorded |
CA2517720A1 (en) | 2003-03-11 | 2004-09-23 | Pfizer Products Inc. | Pyrazine compounds as transforming growth factor (tgf) inhibitors |
EP1606266A4 (en) | 2003-03-21 | 2008-06-25 | Smithkline Beecham Corp | CHEMICAL COMPOUNDS |
WO2004084824A2 (en) | 2003-03-24 | 2004-10-07 | Merck & Co., Inc. | Biaryl substituted 6-membered heterocyles as sodium channel blockers |
GB2400101A (en) | 2003-03-28 | 2004-10-06 | Biofocus Discovery Ltd | Compounds capable of binding to the active site of protein kinases |
GB2400514B (en) | 2003-04-11 | 2006-07-26 | Hewlett Packard Development Co | Image capture method |
US20060252741A1 (en) | 2003-05-15 | 2006-11-09 | Colandrea Vincent J | 3-(2-amino-1-azacyclyl)-5-aryl-1,2,4-oxadiazoles as s1p receptor agonists |
WO2004103991A1 (fr) | 2003-05-20 | 2004-12-02 | 'chemical Diversity Research Institute', Ltd. | Piperidines 2-substituees, bibliotheque focalisee et composition pharmaceutique |
US20050123902A1 (en) | 2003-05-21 | 2005-06-09 | President And Fellows Of Harvard College | Human papillomavirus inhibitors |
PE20050206A1 (es) | 2003-05-26 | 2005-03-26 | Schering Ag | Composicion farmaceutica que contiene un inhibidor de histona deacetilasa |
US7986339B2 (en) | 2003-06-12 | 2011-07-26 | Redflex Traffic Systems Pty Ltd | Automated traffic violation monitoring and reporting system with combined video and still-image data |
JP2005020227A (ja) | 2003-06-25 | 2005-01-20 | Pfu Ltd | 画像圧縮装置 |
AR045595A1 (es) | 2003-09-04 | 2005-11-02 | Vertex Pharma | Composiciones utiles como inhibidores de proteinas quinasas |
US7807696B2 (en) | 2003-10-07 | 2010-10-05 | The Feinstein Institute For Medical Research | Isoxazole and isothiazole compounds useful in the treatment of inflammation |
US20050116968A1 (en) | 2003-12-02 | 2005-06-02 | John Barrus | Multi-capability display |
US20080194574A1 (en) | 2003-12-16 | 2008-08-14 | Axxima Pharmaceuticals Ag | Pyrazine Derivatives As Effective Compounds Against Infectious Diseases |
US20070149547A1 (en) | 2004-02-12 | 2007-06-28 | Celine Bonnefous | Bipyridyl amides as modulators of metabotropic glutamate receptor-5 |
US20050276765A1 (en) | 2004-06-10 | 2005-12-15 | Paul Nghiem | Preventing skin damage |
WO2005123672A2 (en) | 2004-06-14 | 2005-12-29 | Takeda San Diego, Inc. | Kinase inhibitors |
US7626021B2 (en) | 2004-07-27 | 2009-12-01 | Sgx Pharmaceuticals, Inc. | Fused ring heterocycle kinase modulators |
EP1778687A2 (en) | 2004-07-27 | 2007-05-02 | SGX Pharmaceuticals, Inc. | Fused ring heterocycle kinase modulators |
MX2007001986A (es) | 2004-08-26 | 2007-05-10 | Pfizer | Compuestos de aminoheteroarilo como inhibidores de proteina quinasa. |
AP2373A (en) | 2004-08-26 | 2012-03-07 | Pfizer | Enantiomerically pure aminoheteroaryl compounds asprotein kinase inhibitors. |
US7730406B2 (en) | 2004-10-20 | 2010-06-01 | Hewlett-Packard Development Company, L.P. | Image processing system and method |
US7705042B2 (en) | 2004-10-22 | 2010-04-27 | Janssen Pharmaceutica Nv | Class of arylamide compounds useful as inhibitors of c-fms kinase |
US8003806B2 (en) | 2004-11-12 | 2011-08-23 | OSI Pharmaceuticals, LLC | Integrin antagonists useful as anticancer agents |
WO2006058120A1 (en) | 2004-11-22 | 2006-06-01 | Vertex Pharmaceuticals Incorporated | Bicyclic inhibitors or rho kinase |
JP4810669B2 (ja) | 2004-11-25 | 2011-11-09 | コニカミノルタホールディングス株式会社 | 有機エレクトロルミネッセンス素子、表示装置及び照明装置 |
GB0428235D0 (en) | 2004-12-23 | 2005-01-26 | Glaxo Group Ltd | Novel compounds |
ZA200704959B (en) | 2004-12-27 | 2009-04-29 | Alcon Inc | Aminopyrazine analogs for treating glaucoma and other rho kinase-mediated diseases |
GB0500492D0 (en) | 2005-01-11 | 2005-02-16 | Cyclacel Ltd | Compound |
US7622583B2 (en) | 2005-01-14 | 2009-11-24 | Chemocentryx, Inc. | Heteroaryl sulfonamides and CCR2 |
GB0501999D0 (en) | 2005-02-01 | 2005-03-09 | Sentinel Oncology Ltd | Pharmaceutical compounds |
CN101163692B (zh) | 2005-02-16 | 2012-01-18 | 先灵公司 | 具有cxcr3拮抗活性的杂环取代的哌嗪 |
CA2605738C (en) | 2005-04-25 | 2013-10-01 | Merck Patent Gesellschaft Mit Beschraenkter Haftung | Novel azaheterocyclic compounds as kinase inhibitors |
WO2006124874A2 (en) | 2005-05-12 | 2006-11-23 | Kalypsys, Inc. | Inhibitors of b-raf kinase |
WO2006135604A2 (en) | 2005-06-09 | 2006-12-21 | Merck & Co., Inc. | Inhibitors of checkpoint kinases |
CA2617413A1 (en) | 2005-08-02 | 2007-02-08 | Lexicon Pharmaceuticals, Inc. | 2-aminoaryl pyridines as protein kinases inhibitors |
WO2007015632A1 (en) | 2005-08-04 | 2007-02-08 | Cgk Co., Ltd. | Atm and atr inhibitor |
US7394926B2 (en) | 2005-09-30 | 2008-07-01 | Mitutoyo Corporation | Magnified machine vision user interface |
US7806604B2 (en) | 2005-10-20 | 2010-10-05 | Honeywell International Inc. | Face detection and tracking in a wide field of view |
AR056786A1 (es) | 2005-11-10 | 2007-10-24 | Smithkline Beecham Corp | Compuesto de 1h- imidazo ( 4,5-c) piridin-2-ilo, composicion farmaceutica que lo comprende, procedimiento para preparar dicha composicion, su uso para preparar unmedicamento, uso de una combinacion que omprende al compuesto y al menos un agente antineoplasico para preparar un medicamento y dicha com |
CA2630460C (en) | 2005-12-01 | 2013-01-08 | F. Hoffmann-La Roche Ag | Heteroaryl substituted piperidine derivatives as l-cpt1 inhibitors |
US7871982B2 (en) | 2005-12-09 | 2011-01-18 | Meiji Seika Kaisha, Ltd. | Lincomycin derivatives and antimicrobial agents comprising the same as active ingredient |
EP1965645A2 (en) | 2005-12-14 | 2008-09-10 | E.I. Du Pont De Nemours And Company | Isoxazolines for controlling invertebrate pests |
CA2629342A1 (en) | 2005-12-22 | 2007-07-05 | Alcon Research, Ltd. | (indazol-5-yl)-pyrazines and (1,3-dihydro-indol-2-one)- pyrazines for treating rho kinase-mediated diseases and conditions |
PE20070978A1 (es) | 2006-02-14 | 2007-11-15 | Novartis Ag | COMPUESTOS HETEROCICLICOS COMO INHIBIDORES DE FOSFATIDILINOSITOL 3-QUINASAS (PI3Ks) |
ITMI20060311A1 (it) | 2006-02-21 | 2007-08-22 | Btsr Int Spa | Dispositivo perfezionato di alimentazione di filo o filatio ad una macchina tessile e metodo per attuare tale alimentazione |
GB0603684D0 (en) | 2006-02-23 | 2006-04-05 | Novartis Ag | Organic compounds |
WO2007096764A2 (en) | 2006-02-27 | 2007-08-30 | Glenmark Pharmaceuticals S.A. | Bicyclic heteroaryl derivatives as cannabinoid receptor modulators |
TW200800203A (en) | 2006-03-08 | 2008-01-01 | Astrazeneca Ab | New use |
KR20090007347A (ko) | 2006-03-22 | 2009-01-16 | 버텍스 파마슈티칼스 인코포레이티드 | 증식성 장애의 치료를 위한 c-MET 단백질 키나제 억제제 |
US7574131B2 (en) | 2006-03-29 | 2009-08-11 | Sunvision Scientific Inc. | Object detection system and method |
JP2009532356A (ja) | 2006-03-31 | 2009-09-10 | シェーリング コーポレイション | キナーゼ阻害物質 |
US7629346B2 (en) | 2006-06-19 | 2009-12-08 | Hoffmann-La Roche Inc. | Pyrazinecarboxamide derivatives as CB1 antagonists |
WO2007147874A1 (en) | 2006-06-22 | 2007-12-27 | Biovitrum Ab (Publ) | Pyridine and pyrazine derivatives as mnk kinase inhibitors |
AU2007261397A1 (en) | 2006-06-22 | 2007-12-27 | Mallinckrodt Llc | Pyrazine derivatives with extended conjugation and uses thereof |
EP1900727A1 (en) | 2006-08-30 | 2008-03-19 | Cellzome Ag | Aminopyridine derivatives as kinase inhibitors |
CA2664378A1 (en) | 2006-09-29 | 2008-04-03 | Novartis Ag | Pyrazolopyrimidines as pi3k lipid kinase inhibitors |
GB0619342D0 (en) | 2006-09-30 | 2006-11-08 | Vernalis R&D Ltd | New chemical compounds |
AU2007304365A1 (en) | 2006-10-04 | 2008-04-10 | F. Hoffmann-La Roche Ag | 3-pyridinecarboxamide and 2-pyrazinecarboxamide derivatives as HDL-cholesterol raising agents |
MX337906B (es) | 2006-10-19 | 2016-03-28 | Signal Pharm Llc | Compuestos de heteroarilo, composiciones de los mismos, y su uso como inhibidores de proteina cinasas. |
WO2008060907A2 (en) | 2006-11-10 | 2008-05-22 | Bristol-Myers Squibb Company | Pyrrolo-pyridine kinase inhibitors |
US20080132698A1 (en) | 2006-11-30 | 2008-06-05 | University Of Ottawa | Use of N-oxide compounds in coupling reactions |
JP2010513232A (ja) | 2006-12-15 | 2010-04-30 | バイエル・シエーリング・ファーマ アクチエンゲゼルシャフト | 3−h−ピラゾロピリジン類及びそれらの塩類、それらを含んで成る医薬組成物類、それらの調製方法及びそれらの使用 |
AU2007338792B2 (en) | 2006-12-20 | 2012-05-31 | Amgen Inc. | Substituted heterocycles and methods of use |
PE20081581A1 (es) | 2006-12-21 | 2008-11-12 | Plexxikon Inc | COMPUESTOS PIRROLO[2,3-b]PIRIDINAS COMO MODULADORES DE QUINASA |
GB0625659D0 (en) | 2006-12-21 | 2007-01-31 | Cancer Rec Tech Ltd | Therapeutic compounds and their use |
JP2010519204A (ja) | 2007-02-16 | 2010-06-03 | アムジエン・インコーポレーテツド | 窒素含有複素環ケトン類およびそれらのc−Met阻害薬としての使用 |
BRPI0808523A2 (pt) | 2007-03-01 | 2014-08-19 | Novartis Vaccines & Diagnostic | Inibidores de pim cinase e métodos de seu uso |
EP2181100A2 (en) | 2007-04-10 | 2010-05-05 | Bayer CropScience AG | Insecticidal aryl isoxazoline derivatives |
JP2008260691A (ja) | 2007-04-10 | 2008-10-30 | Bayer Cropscience Ag | 殺虫性アリールイソオキサゾリン誘導体 |
CL2008001356A1 (es) | 2007-05-10 | 2008-11-14 | Smithkline Beecham Corp | Compuestos derivados de quinoxalina, inhibidores de la pi3 quinasa _(p13ka, pi3ko, pi3b y/o pi3ky); composicion farmaceutica; uso para tratar un trastorno autoinmune, enfermedad inflamatoria, cardiovascular, neurodegerativa, alergia, asma, enfermedad renal, cancer, rechazo de transplante, lesiones pulmonares. |
PE20090717A1 (es) | 2007-05-18 | 2009-07-18 | Smithkline Beecham Corp | Derivados de quinolina como inhibidores de la pi3 quinasa |
EP2167086A1 (en) * | 2007-05-25 | 2010-03-31 | AstraZeneca AB | Combination of chk and parp inhibitors for the treatment of cancers |
UY31137A1 (es) | 2007-06-14 | 2009-01-05 | Smithkline Beecham Corp | Derivados de quinazolina como inhibidores de la pi3 quinasa |
EP2012409A2 (en) | 2007-06-19 | 2009-01-07 | Hitachi, Ltd. | Rotating electrical machine |
EP2157090A4 (en) | 2007-06-21 | 2011-09-07 | Taisho Pharmaceutical Co Ltd | PYRAZINAMIDE COMPOUND |
KR20100037047A (ko) | 2007-06-26 | 2010-04-08 | 렉시컨 파마슈티컬스 인코퍼레이티드 | 세로토닌-매개 질환 및 장애의 치료 방법 |
WO2009005638A2 (en) | 2007-06-27 | 2009-01-08 | Merck & Co., Inc. | Pyridyl and pyrimidinyl derivatives as histone deacetylase inhibitors |
GB0713259D0 (en) | 2007-07-09 | 2007-08-15 | Astrazeneca Ab | Pyrazine derivatives 954 |
US8293747B2 (en) | 2007-07-19 | 2012-10-23 | Merck Sharp & Dohme Corp. | Heterocyclic amide compounds as protein kinase inhibitors |
AU2008275891B2 (en) | 2007-07-19 | 2013-10-10 | H.Lundbeck A/S | 5-membered heterocyclic amides and related compounds |
BRPI0815042A2 (pt) | 2007-08-01 | 2015-02-10 | Pfizer | Compostos de pirazol |
WO2009024825A1 (en) | 2007-08-21 | 2009-02-26 | Astrazeneca Ab | 2-pyrazinylbenzimidazole derivatives as receptor tyrosine kinase inhibitors |
EP2203436A1 (en) | 2007-09-17 | 2010-07-07 | Neurosearch A/S | Pyrazine derivatives and their use as potassium channel modulators |
JP2011500778A (ja) | 2007-10-25 | 2011-01-06 | アストラゼネカ・アクチエボラーグ | ピリジン及びピラジン誘導体−083 |
WO2009099982A1 (en) | 2008-02-04 | 2009-08-13 | Osi Pharmaceuticals, Inc. | 2-aminopyridine kinase inhibitors |
EP2247595B1 (en) | 2008-02-25 | 2011-07-20 | F. Hoffmann-La Roche AG | Pyrrolopyrazine kinase inhibitors |
WO2009106442A1 (en) | 2008-02-25 | 2009-09-03 | F. Hoffmann-La Roche Ag | Pyrrolopyrazine kinase inhibitors |
CA2712507A1 (en) | 2008-02-25 | 2009-09-03 | F. Hoffmann-La Roche Ag | Pyrrolopyrazine kinase inhibitors |
KR20100114095A (ko) | 2008-02-25 | 2010-10-22 | 에프. 호프만-라 로슈 아게 | 피롤로피라진 키나아제 저해제 |
TW200940537A (en) | 2008-02-26 | 2009-10-01 | Astrazeneca Ab | Heterocyclic urea derivatives and methods of use thereof |
WO2009111280A1 (en) | 2008-02-29 | 2009-09-11 | Array Biopharma Inc. | N- (6-aminopyridin-3-yl) -3- (sulfonamido) benzamide derivatives as b-raf inhibitors for the treatment of cancer |
US8268834B2 (en) | 2008-03-19 | 2012-09-18 | Novartis Ag | Pyrazine derivatives that inhibit phosphatidylinositol 3-kinase enzyme |
US8110576B2 (en) | 2008-06-10 | 2012-02-07 | Plexxikon Inc. | Substituted pyrrolo[2,3b]pyrazines and methods for treatment of raf protein kinase-mediated indications |
GB0814364D0 (en) | 2008-08-05 | 2008-09-10 | Eisai London Res Lab Ltd | Diazaindole derivatives and their use in the inhibition of c-Jun N-terminal kinase |
SI2767537T1 (sl) | 2008-08-06 | 2017-08-31 | Medivation Technologies, Inc. | Dihidropiridoftalazinonski inhibitorji poli(adp-riboza) polimeraze (parp) |
CA2731368C (en) | 2008-08-06 | 2013-05-14 | Pfizer Inc. | 6 substituted 2-heterocyclylamino pyrazine compounds as chk-1 inhibitors |
NZ592569A (en) | 2008-10-21 | 2012-05-25 | Vertex Pharma | C-met protein kinase inhibitors |
NZ593316A (en) | 2008-11-10 | 2013-06-28 | Vertex Pharma | Pyrazine compounds useful as inhibitors of atr kinase |
AU2009324894B2 (en) | 2008-11-25 | 2015-04-09 | University Of Rochester | MLK inhibitors and methods of use |
SG171956A1 (en) | 2008-12-05 | 2011-07-28 | Hoffmann La Roche | Pyrrolopyrazinyl urea kinase inhibitors |
RS56995B1 (sr) | 2008-12-19 | 2018-05-31 | Vertex Pharma | Derivati pirazina korisni kao inhibitori atr kinaze |
CA2748099C (en) | 2008-12-22 | 2017-02-28 | Array Biopharma Inc. | 7-phenoxychroman carboxylic acid derivatives |
TW201028410A (en) | 2008-12-22 | 2010-08-01 | Astrazeneca Ab | Chemical compounds 610 |
US8541424B2 (en) | 2008-12-23 | 2013-09-24 | Abbott Laboratories | Anti-viral compounds |
US8492582B2 (en) | 2009-01-30 | 2013-07-23 | Toyama Chemical Co., Ltd. | N-acyl anthranilic acid derivative or salt thereof |
JP5353279B2 (ja) | 2009-02-06 | 2013-11-27 | Jnc株式会社 | セレンテラミド又はその類縁体の製造方法 |
WO2010093425A1 (en) | 2009-02-11 | 2010-08-19 | Sepracor Inc. | Histamine h3 inverse agonists and antagonists and methods of use thereof |
CN101537007A (zh) | 2009-03-18 | 2009-09-23 | 中国医学科学院血液病医院(血液学研究所) | N-(噻吩-2)吡唑并[1,5-a]嘧啶-3-甲酰胺类化合物在制备抗恶性肿瘤药物方面的应用 |
EP2411007A4 (en) | 2009-03-27 | 2012-12-05 | Uab Research Foundation | MODULATION OF MEDIATION TRANSLATION BY IRES SEQUENCES |
AR077468A1 (es) | 2009-07-09 | 2011-08-31 | Array Biopharma Inc | Compuestos de pirazolo (1,5 -a) pirimidina sustituidos como inhibidores de trk- quinasa |
MX2012000711A (es) | 2009-07-15 | 2012-03-16 | Abbott Lab | Inhibidores de pirrolopirazina de cinasas. |
CN102548411B (zh) | 2009-08-07 | 2014-07-02 | 陶氏益农公司 | 杀虫组合物 |
JP2011042639A (ja) | 2009-08-24 | 2011-03-03 | Kowa Co | ビフェニルピラジン化合物及びこれを有効成分として含有するエリスロポエチン産生促進剤 |
CN101671336B (zh) | 2009-09-23 | 2013-11-13 | 辽宁利锋科技开发有限公司 | 芳杂环并嘧啶衍生物和类似物及其制备方法和用途 |
DE102009043260A1 (de) | 2009-09-28 | 2011-04-28 | Merck Patent Gmbh | Pyridinyl-imidazolonderivate |
PL2485731T4 (pl) | 2009-10-06 | 2017-07-31 | Millennium Pharmaceuticals, Inc. | Związki heterocykliczne użyteczne jako inhibitory PDK1 |
EP2498778A1 (en) * | 2009-11-13 | 2012-09-19 | The United States Of America, As Represented By The Secretary, Department of Health and Human Services | Diazeniumdiolated compounds, pharmaceutical compositions, and method of treating cancer |
RS54339B1 (en) | 2010-01-18 | 2016-02-29 | Mmv Medicines For Malaria Venture | NEW ANTIMALARIAN AGENTS |
US8518945B2 (en) | 2010-03-22 | 2013-08-27 | Hoffmann-La Roche Inc. | Pyrrolopyrazine kinase inhibitors |
MX2012011549A (es) | 2010-04-08 | 2013-01-29 | Ah Usa 42 Llc | Derivados de 3,5-difenil-isoxazolina sustituida como insecticidas y acaricidas. |
ES2602475T3 (es) | 2010-04-15 | 2017-02-21 | Tracon Pharmaceuticals, Inc. | Potenciación de la actividad anticáncer por terapia de combinación con inhibidores de la vía BER |
WO2011138751A2 (en) | 2010-05-04 | 2011-11-10 | Pfizer Inc. | Heterocyclic derivatives as alk inhibitors |
WO2011143419A1 (en) | 2010-05-12 | 2011-11-17 | Vertex Pharmaceuticals Incorporated | Pyrazines useful as inhibitors of atr kinase |
JP2013529200A (ja) * | 2010-05-12 | 2013-07-18 | バーテックス ファーマシューティカルズ インコーポレイテッド | Atrキナーゼ阻害剤として有用な化合物 |
US9334244B2 (en) | 2010-05-12 | 2016-05-10 | Vertex Pharmaceuticals Incorporated | Compounds useful as inhibitors of ATR kinase |
EP2568984A1 (en) | 2010-05-12 | 2013-03-20 | Vertex Pharmaceuticals Incorporated | Compounds useful as inhibitors of atr kinase |
NZ603478A (en) | 2010-05-12 | 2014-09-26 | Vertex Pharma | 2 -aminopyridine derivatives useful as inhibitors of atr kinase |
JP5836367B2 (ja) | 2010-05-12 | 2015-12-24 | バーテックス ファーマシューティカルズ インコーポレイテッドVertex Pharmaceuticals Incorporated | Atrキナーゼ阻害剤として有用な化合物 |
JP2013526558A (ja) | 2010-05-20 | 2013-06-24 | エフ.ホフマン−ラ ロシュ アーゲー | Syk及びjak阻害剤としてのピロロピラジン誘導体 |
BR112012029437A2 (pt) | 2010-05-20 | 2017-03-07 | F Hoffmann - La Roche Ag | derivados de pirrolo[2,3-b]pirazina-7-carboxamida e seu uso como inibidores de jak e syk |
AU2011270807A1 (en) | 2010-06-23 | 2013-01-31 | Vertex Pharmaceuticals Incorporated | Pyrrolo- pyrazine derivatives useful as inhibitors of ATR kinase |
CN102311396B (zh) | 2010-07-05 | 2015-01-07 | 暨南大学 | 一种吡嗪类衍生物和其制备方法及在制药中的应用 |
EP2407478A1 (en) | 2010-07-14 | 2012-01-18 | GENETADI Biotech, S.L. | New cyclotetrapeptides with pro-angiogenic properties |
JP5782238B2 (ja) | 2010-07-30 | 2015-09-24 | ルネサスエレクトロニクス株式会社 | 電圧検出回路及びその制御方法 |
WO2012121939A2 (en) | 2011-03-04 | 2012-09-13 | Locus Pharmaceuticals, Inc. | Aminopyrazine compounds |
KR20140014205A (ko) | 2011-03-04 | 2014-02-05 | 렉시컨 파마슈티컬스 인코퍼레이티드 | Mst1 키나제 억제제 및 그의 사용 방법 |
WO2012138938A1 (en) | 2011-04-05 | 2012-10-11 | Vertex Pharmaceuticals Incorporated | Aminopyrazine compounds useful as inhibitors of tra kinase |
JP2014513728A (ja) | 2011-05-17 | 2014-06-05 | プリンシピア バイオファーマ インコーポレイテッド | チロシンキナーゼ阻害剤としてのアザインドール誘導体 |
US9096602B2 (en) | 2011-06-22 | 2015-08-04 | Vertex Pharmaceuticals Incorporated | Substituted pyrrolo[2,3-B]pyrazines as ATR kinase inhibitors |
EP2723746A1 (en) | 2011-06-22 | 2014-04-30 | Vertex Pharmaceuticals Inc. | Compounds useful as inhibitors of atr kinase |
EP2723745A1 (en) | 2011-06-22 | 2014-04-30 | Vertex Pharmaceuticals Inc. | Compounds useful as inhibitors of atr kinase |
AU2012315615A1 (en) | 2011-09-30 | 2014-04-17 | Vertex Pharmaceuticals Incorporated | Processes for making compounds useful as inhibitors of ATR kinase |
EP2751088B1 (en) | 2011-09-30 | 2016-04-13 | Vertex Pharmaceuticals Incorporated | Compounds useful as inhibitors of atr kinase |
CN108464983A (zh) | 2011-09-30 | 2018-08-31 | 沃泰克斯药物股份有限公司 | 用atr抑制剂治疗胰腺癌和非小细胞肺癌 |
US8853217B2 (en) | 2011-09-30 | 2014-10-07 | Vertex Pharmaceuticals Incorporated | Compounds useful as inhibitors of ATR kinase |
IN2014KN00943A (sl) | 2011-09-30 | 2015-08-21 | Vertex Pharma | |
EP2776419B1 (en) | 2011-11-09 | 2016-05-11 | Vertex Pharmaceuticals Incorporated | Pyrazine compounds useful as inhibitors of atr kinase |
WO2013071090A1 (en) | 2011-11-09 | 2013-05-16 | Vertex Pharmaceuticals Incorporated | Compounds useful as inhibitors of atr kinase |
US8846917B2 (en) | 2011-11-09 | 2014-09-30 | Vertex Pharmaceuticals Incorporated | Compounds useful as inhibitors of ATR kinase |
WO2013071094A1 (en) | 2011-11-09 | 2013-05-16 | Vertex Pharmaceuticals Incorporated | Compounds useful as inhibitors of atr kinase |
US8841450B2 (en) | 2011-11-09 | 2014-09-23 | Vertex Pharmaceuticals Incorporated | Compounds useful as inhibitors of ATR kinase |
DK2833973T3 (en) | 2012-04-05 | 2018-01-02 | Vertex Pharma | Compounds useful as ATR kinase inhibitors and combination therapies thereof |
CN103373996A (zh) | 2012-04-20 | 2013-10-30 | 山东亨利医药科技有限责任公司 | 作为crth2受体拮抗剂的二并环衍生物 |
EP2904406B1 (en) | 2012-10-04 | 2018-03-21 | Vertex Pharmaceuticals Incorporated | Method for measuring atr inhibition mediated increases in dna damage |
US8912198B2 (en) | 2012-10-16 | 2014-12-16 | Vertex Pharmaceuticals Incorporated | Compounds useful as inhibitors of ATR kinase |
LT3486245T (lt) | 2012-12-07 | 2021-08-25 | Vertex Pharmaceuticals Incorporated | 2-amino-n-(piperidin-1-il-piridin-3-il)pirazolo[1,5alfa]pirimidin-3-karboksamidas, kaip atr kinazės inhibitorius |
AU2014360380B2 (en) | 2013-12-06 | 2019-03-21 | Vertex Pharmaceuticals Incorporated | 2-amino-6-fluoro-n-[5-fluoro-pyridin-3-yl]pyrazolo[1,5-a]pyrimidin-3-carboxamide compound useful as ATR kinase inhibitor, its preparation, different solid forms and radiolabelled derivatives thereof |
AU2015271030B2 (en) | 2014-06-05 | 2019-05-16 | Vertex Pharmaceuticals Incorporated | Radiolabelled derivatives of a 2-amino-6-fluoro-n-[5-fluoro-pyridin-3-yl]- pyrazolo [1,5-a] pyrimidin-3-carboxamide compound useful as ATR kinase inhibitor, the preparation of said compound and different solid forms thereof |
KR20170016498A (ko) | 2014-06-17 | 2017-02-13 | 버텍스 파마슈티칼스 인코포레이티드 | Chk1 및 atr 저해제의 병용물을 사용하는 암의 치료 방법 |
MX395066B (es) | 2015-09-30 | 2025-03-24 | Vertex Pharma | Método para tratar cáncer usando una combinación de agentes que dañan el adn e inhibidores de proteína relacionada con ataxia telangiectasia y rad3 (atr). |
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