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HRP20170631T1 - Spojevi pirolopirimidina i njihove uporabe - Google Patents

Spojevi pirolopirimidina i njihove uporabe Download PDF

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HRP20170631T1
HRP20170631T1 HRP20170631TT HRP20170631T HRP20170631T1 HR P20170631 T1 HRP20170631 T1 HR P20170631T1 HR P20170631T T HRP20170631T T HR P20170631TT HR P20170631 T HRP20170631 T HR P20170631T HR P20170631 T1 HRP20170631 T1 HR P20170631T1
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HRP20170631TT
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Christopher Thomas Brain
Gebhard Thoma
Moo Je Sung
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Novartis Ag
Astex Therapeutics Ltd.
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Publication of HRP20170631T1 publication Critical patent/HRP20170631T1/hr

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    • C07D487/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
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Claims (16)

1. Spoj, naznačen time, da ima sljedeću formulu (I): [image] ili njegova farmaceutski prihvatljiva sol ili njegov solvat, pri čemu: crtkana linija označava dvostruku vezu; A je N ili CR5; gdje R5 je vodik ili C1-C3-alkil; svaki od R2 i R3 je neovisno odabran iz skupine koju čine: vodik, hidroksil, C1-C3-alkil, C3-C8-cikloalkil, heterociklil, aril, heteroaril, supstituirani C1-C3-alkil, supstituirani C3-C8-cikloalkil, supstituirani heterociklil, supstituirani aril i supstituirani heteroaril; R4 je odabran iz skupine koju čine: C(H)(CH2CH3)2, C(H)(CH2CH3)Ph, CH2CH3, ciklopropil, ciklopentil ili cikloheksil; X je N ili CR11, i Y je CR12; R11 je odabran iz skupine koju čine: halo, vodik, C1-C3-alkil, C1-C3-alkoksi, CN, C=NOH, C=NOCH3, C(O)H, C(O)C1-C3-alkil, C3-C8-cikloalkil, heterociklil, aril, heteroaril, supstituirani C1-C3-alkil, supstituirani C3-C8-cikloalkil, supstituirani heterociklil, supstituirani aril, supstituirani heteroaril, -BNR13R14, -BOR13, -BC(O)R13, -BC(O)OR13, -BC(O)NR13R14, gdje B je veza, C1-C3-alkil ili razgranati C1-C3-alkil; pri čemu je svaki od R13 i R14 neovisno odabran iz skupine koju čine: vodik, C1-C3-alkil, C3-C8-cikloalkil, heterociklil, aril, heteroaril, supstituirani alkil, supstituirani cikloalkil, supstituirani heterociklil, supstituirani aril i supstituirani heteroaril; te R12 je -BC(O)NR13R14; dok B je veza, C1-C3-alkil ili razgranati C1-C3-alkil; gdje je svaki od R13 i R14 neovisno odabran iz skupine koju čine: vodik, C1-C3-alkil, C3-C8-cikloalkil, heterociklil, aril, heteroaril, supstituirani alkil, supstituirani cikloalkil, supstituirani heterociklil, supstituirani aril i supstituirani heteroaril.
2. Spoj prema zahtjevu 1, naznačen time, da A je N.
3. Spoj prema zahtjevu 1, naznačen time, da R2 je H.
4. Spoj prema zahtjevu 1, naznačen time, da R3 je aril-skupina koja je dodatno neovisno supstituirana jednom ili više puta sa sljedećima: halogen, C1-C4-alkoksi, R15-amin, R15-heterocikl ili R15-heteroaril, gdje R15 je veza, C(O), N(H)C(O), N(H)SO2, OC(O) ili (CH2)1-4, dok (CH2)1-4-skupina može biti prekinuta s O, N(CH3) ili N(H).
5. Spoj prema zahtjevu 4, naznačen time, da aril-skupina je fenil.
6. Spoj prema zahtjevu 1, naznačen time, da R3 je fenil-skupina koja je neovisno supstituirana jednom ili više puta sa sljedećima: fluoro, metoksi, dietilamin, R15-piperazinil, R15-morfolinil, R15-piperidinil, R15-triazolil, R15-fenil, R15-piridinil, R15-piperazinil, R15-indazolil, R15-pirolidinil ili R15-imidazolil, pri čemu skupine piperazinil, morfolinil, piperidinil, triazolil, fenil, piridinil, piperazinil, indazolil, pirolidinil ili imidazolil, mogu biti dodatno supstituirane sa sljedećima: C1-C4-alkil, C(O)C1-C4-alkil, S(O)2-C1-C4-alkil, OH, C(O)(CH2)1-3CN ili N(H)C(O)C1-C4-alkil.
7. Spoj prema zahtjevu 1, naznačen time, da R3 je fenil-skupina koja je supstituirana sa sljedećima: N(H)C(O)-aril, C(O)N(H)C1-C4-alkil, C(O)N(C1-C4-alkil)2 ili C(O)N(H)C3-C6-cikloalkil.
8. Spoj prema zahtjevu 1, naznačen time, da je spoj odabran iz skupine koja se sastoji od sljedećih: [image] [image] [image] [image] [image] [image] [image] [image] [image] [image] [image] [image] [image] [image] [image] [image] [image]
9. Spoj prema bilo kojem od zahtjeva 1 do 8, naznačen time, da se upotrebljava u liječenju autoimune bolesti, bolesti zbog odbacivanja transplantata ili tumorskog poremećaja.
10. Spoj za uporabu prema zahtjevu 9, naznačen time, da je autoimuna bolest odabrana iz skupine koja se sastoji od sljedećih: autoimuna hemolitička anemija, autoimuna neonatalna trombocitopenija, idiopatska trombocitopenijska purpura, autoimunocitopenija, hemolitička anemija, antifosfolipidni sindrom, dermatitis, alergijski encefalomijelitis, miokarditis, recidivan polihondritis, reumatska srčana bolest, glomerulonefritis, multipla skleroza, neuritis, uveitis oftalmija, poliendokrinopatije, purpura, Reiterova bolest, sindrom ukočene osobe, autoimuna upala pluća, autizam, Guillain-Barre-sindrom, dijabetes melitus ovisan o inzulinu, autoimuna upala oka, autoimuni tiroiditis, hipertiroidizam, sustavna lupus eritematoza, Goodpastureov sindrom, pemfigus, autominuniteti receptora, autoimuna hemolitička anemija, autoimuna trombocitopenijska purpura, reumatoidni artritis, miješana bolest vezivnog tkiva, polimiositis/dermatomiositis, smrtonosna anemija, idiopatska Addisonova bolest, neplodnost, glomerulonefritis, bulozni pemfigoid, Sjogrenov sindrom, dijabetes melitus, adrenergična otpornost na ljekovite tvari, kronični aktivni hepatitis, primarna ciroza žučnih vodova, vitiligo, vaskulitis, post-MI (stanje nakon infarkta miokarda), kardiotomijski sindrom, urtikarija, atopični dermatitis, astma, upalne miopatije, kronični aktivni hepatitis, primarna ciroza žučnih vodova i bolesti preosjetljivosti posredovane T-stanicama.
11. Spoj za uporabu prema zahtjevu 9, naznačen time, da je odbacivanje transplantata odabrano iz skupine koju čine: reakcija presatka protiv stanice domaćina, odbacivanje povezano s ksenotransplantacijom, odbacivanje transplantata povezano s presađivanjem organa, akutno neprihvaćanje transplantata, obacivanje heterografta ili homografta te ishemijska ili reperfuzijska ozljeda nastala prilikom presađivanja organa.
12. Spoj za uporabu prema zahtjevu 9, naznačen time, da je rak odabran iz sljedeće skupine: rak mjehura, rak glave i vrate, rak dojke, rak želudca, rak jajnika, rak debelog crijeva, rak pluća, rak mozga, rak grla, rak limfnog sustava, genitourinarni rak, gastrointestinalni rak, rak ovarija, rak prostate, gastrički rak, rak kostiju, rak malih stanica pluća, gliom, kolorektalni rak i rak gušterače.
13. Farmaceutski sastav, naznačen time, da obuhvaća spoj prema bilo kojem od zahtjeva 1 do 8, zajedno s farmaceutski prihvatljivim nosačem, i prema potrebi zajedno s ostalim terapeutskim sredstvima.
14. Farmaceutski sastav, naznačen time, da obuhvaća spoj prema bilo kojem od zahtjeva 1 do 8, te je pritom prilagođen za istovremenu ili uzastopnu primjenu sa sljedećim sredstvima: protuupalno sredstvo, antiproliferativno sredstvo, kemoterapeutsko sredstvo, imunosupresivno sredstvo, protutumorsko sredstvo, citotoksično sredstvo ili inhibitor kinaze, koji nisu spoj prema bilo kojem od zahtjeva 1 do 8 niti njegova sol.
15. Farmaceutski sastav prema zahtjevu 14, naznačen time, da se spoj prema bilo kojem od zahtjeva 1 do 8, ili njegova sol, primjenjuje istovremeno ili uzastopno, s jednim ili više od sljedećih sredstava ili njihovih derivata: PTK-inhibitor, ciklosporin A, CTLA4-Ig, protutijela odabrana od sljedećih: anti-ICAM-3, anti-IL-2-receptor, anti-CD45RB, anti-CD2, anti-CD3, anti-CD4, anti-CD80, anti-CD86 i monoklonalno protutijelo OKT3, blokatori međusobnog djelovanja između CD40 i gp39, fuzijski protein konstruiran od CD40 i gp39, inhibitori funkcije NF-kappa-B, nesteroidni protuupalni lijekovi, steroidi, spojevi zlata, antiproliferativna sredstva, FK506, mikofenolat-mofetil, citotoksični lijekovi, TNF-α-inhibitori, protutijela anti-TNF ili topivi TNF-receptor, rapamicin, leflunimid, inhibitori ciklooksigenaze-2, paklitaksel, cisplatin, karboplatin, doksorubicin, karminomicin, daunorubicin, aminopterin, metotreksat, metopterin, mitomicin C, ekteinascidin 743, porfiromicin, 5-fluorouracil, 6-merkaptopurin, gemcitabin, citozin-arabinozid, podofilotoksin, etopozid, etopozid-fosfat, tenipozid, melfalan, vinblastin, vinkristin, leurozidin, epotilon, vindezin ili leurozin.
16. Paket, naznačen time, da obuhvaća spoj prema bilo kojem od zahtjeva 1 do 8, pakiran zajedno s uputama za uporabu u liječenju autoimune bolesti, bolesti kod odbacivanja transplantata ili tumorskog poremećaja.
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