HRP20160084T1 - Spojevi 3,4-dihidropirazino[2,3-b]pirazin-2(1h)-ona kao inhibitori mtor kinaze za onkološke indikacije i bolesti povezane s mtor/p13k/akt putom - Google Patents
Spojevi 3,4-dihidropirazino[2,3-b]pirazin-2(1h)-ona kao inhibitori mtor kinaze za onkološke indikacije i bolesti povezane s mtor/p13k/akt putom Download PDFInfo
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- HRP20160084T1 HRP20160084T1 HRP20160084TT HRP20160084T HRP20160084T1 HR P20160084 T1 HRP20160084 T1 HR P20160084T1 HR P20160084T T HRP20160084T T HR P20160084TT HR P20160084 T HRP20160084 T HR P20160084T HR P20160084 T1 HRP20160084 T1 HR P20160084T1
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- Prior art keywords
- dihydropyrazino
- pyridin
- pyrazin
- triazol
- disease
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Claims (19)
1. Spoj koji ima formulu (II):
[image]
ili farmaceutski prihvatljiva sol, stereoizomer ili tautomer istog, naznačen time, da:
R1 je piridil supstituiran s jednim ili više supstituenata neovisno odabranih iz skupine koja se sastoji od supstituiranog ili nesupstituiranog C1-8 alkila, supstituiranog ili nesupstituiranog heterociklila, halogena, aminokarbonila, cijano, hidroskialkila, -OR i -NR2, pri čemu je svaki R neovisno H ili supstituirani ili nesupstituirani C1-4 alkil;
R2 je supstituiran ili nesupstituiran cikloalkil; i R3 je H ili supstituirano ili nesupstituirani C1-8 alkil;
pri čemu određenje "supstituiran" označava supstituciju bilo kojim od supstituenata navedenim u naknadnim patentnim zahtjevima ili s halogenom; alkilom; hidroksilom; alkoksi; alkoksialkilom; amino; alkilaminom; karboksi; nitro; cijano; tiolom; tioeterom; iminom; imidom; amidinom; gvnidinom; enaminom; aminokarbonilom; acilaminom; fosfonatom; fosfinom; tiokarbonilom; sulfonilom; sulfonom; sulfonamidom; ketonom; aldehidom; esterom; ureom; uretanom; oksimom; hidroksil aminom; alkoksiaminom; aralkoksiaminom; N-oksidom; hidrazinom; hidrazidom; hidrazonom; azidom; izocijanatom; izotiocijanatom; cijanatom; tiocijanatom; kisikom (=O); B(OH)2, O(alkil)aminokarbonilom; cikloalkilom, koji može biti monociklički ili spojeni ili rastavljeni policiklički; heterociklilom, koji može biti monociklički ili spojeni ili rastavljeni policiklički; monociklički ili spojeni ili rastavljeni policiklički aril ili heteroaril; ariloksi; aralkiloksi; heterocikliloski; ili heterociklil alkoksi.
2. Spoj u skladu s patentnim zahtjevom 1, naznačen time, da R3 jeste H.
3. Spoj u skladu s patentnim zahtjevom 1 ili 2, naznačen time, da R1 je piridil supstituiran s hidroksialkilom; ili gdje je piridil supstituiran sa supstituiranim ili nesupstituiranim triazolilom i supstituiranim ili nesupstituiranim C1-8 alkilom.
4. Spoj u skladu s patentnim zahtjevom 1, naznačen time, da je spoj:
7-(6-(1H-1,2,4-triazol-3-il)piridin-3-il)-1-(cis-4-metoksicikloheksil)-3,4-dihidropirazino[2,3-b]pirazin-2(1H)-on;
7-(6-(1H-1,2,4-triazol-3-il)piridin-3-il)-1-(cis-4-hidroksicikloheksil)-3,4-dihidropirazino[2,3-b]pirazin-2(1H)-on;
7-(6-(1H-1,2,4-triazol-3-il)piridin-3-il)-1-(trans-4-hidroksicikloheksil)-3,4-dihidropirazino[2,3-b]pirazin-2(1H)-on;
7-(6-(1H-1,2,4-triazol-3-il)piridin-3-il)-1-(trans-4-metoksicikloheksil)-3,4-dihidropirazino[2,3-b]pirazin-2(1H)-on;
1-(trans-4-metoksicikloheksil)-7-(4-metil-6-(1H-1,2,4-triazol-3-il)piridin-3-il)-3,4-dihidropirazino[2,3-b]pirazin-2(1H)-on;
7-(6-(2-hidroksipropan-2-il)piridin-3-il)-1-((1R,3R)-3-metoksiciklopentil)-3,4-dihidropirazino[2,3-b]pirazin-2(1H)-on;
7-(6-(2-hidroksipropan-2-il)piridin-3-il)-1-((1S,3R)-3-metoksiciklopentil)-3,4-dihidropirazino[2,3-b]pirazin-2(1H)-on;
7-(6-(2-hidroksipropan-2-il)piridin-3-il)-1-((1S,3S)-3-metoksiciklopentil)-3,4-dihidropirazino[2,3-b]pirazin-2( H)-on;
7-(6-(2-hidroksipropan-2-il)piridin-3-il)-1-((1R,3S)-3-metoksiciklopentil)-3,4-dihidropirazino[2,3-b]pirazin-2(1H)-on;
1-(trans-4-hidroksicikloheksil)-7-(2-metil-6-(4H-1,2,4-triazol-3-il)piridin-3-il)-3,4-dihidropirazino[2,3-b]pirazin-2(1H)-on;
1-(cis-4-hidroksicikloheksil)-7-(2-metil-6-(4H-1,2,4-triazol-3-il)piridin-3-il)-3,4-dihidropirazino[2,3-b]pirazin-2(1H)-on;
1-(trans-4-hidroksicikloheksil)-7-(6-(2-hidroksipropan-2-il)piridin-3-il)-3,4-dihidropirazino[2,3-b]pirazin-2(1H)-on;
1-(cis-4-hidroksicikloheksil)-7-(6-(2-hidroksipropan-2-il)piridin-3-il)-3,4-dihidropirazino[2,3-b]pirazin-2(1H)-on;
1-((1S,3R)-3-metoksiciklopentil)-7-(2-metil-6-(4H-1,2,4-triazol-3-il)piridin-3-il)-3,4-dihidropirazino[2,3-b]pirazin-2(1H)-on;
1-((1R,3R)-3-metoksiciklopentil)-7-(2-metil-6-(4H-1,2,4-triazol-3-il)piridin-3-il)-3,4-dihidropirazino[2,3-b]pirazin-2(1H)-on;
1-((1R,3S)-3-metoksiciklopentil)-7-(2-metil-6-(4H-1,2,4-triazol-3-il)piridin-3-il)-3,4-dihidropirazino[2,3-b]pirazin-2(1H)-on;
1-((1S,3S)-3-metoksiciklopentil)-7-(2-metil-6-(4H-1,2,4-triazol-3-il)piridin-3-il)-3,4-dihidropirazino[2,3-b]pirazin-2( 1H)-on;
1 -(trans-4-metoksicikloheksil)-7-(2-metil-6-(4H-1,2,4-triazol-3-il)piridin-3-il)-3,4-dihidropirazino[2,3-b]pirazin-2(1H)-on; ili
7-(6-(2-hidroksipropan-2-il)piridin-3-il)-1-(trans-4-metoksicikloheksil)-3,4-dihidropirazino[2,3-b]pirazin-2(1H)-on,
ili farmaceutski prihvatljiva sol, stereoizomer ili tautomer istog.
5. Spoj u skladu s patentnim zahtjevom 1, naznačen time, da je spoj 7-(6-(1H-1,2,4-triazol-3-il)piridin-3-il)-1-(cis-4-hidroksicikloheksil)-3,4-dihidropirazino[2,3-b]pirazin-2(1H)-on ili farmaceutski prihvatljiva sol, stereoizomer ili tautomer istog.
6. Spoj u skladu s patentnim zahtjevom 1, naznačen time, da je spoj 7-(6-(2-hidroksipropan-2-il)piridin-3-il)-1-((1R,3R)-3-metoksiciklopentil)-3,4-dihidropirazino[2,3-b]pirazin-2(1H)-on ili farmaceutski prihvatljiva sol, stereoizomer ili tautomer istog.
7. Spoj u skladu s patentnim zahtjevom 1, naznačen time, da je spoj 1-(trans-4-hidroksicikloheksil)-7-(2-metil-6-(4H-1,2,4-triazol-3-il)piridin-3-il)-3,4-dihidropirazino[2,3-b]pirazin-2(1H)-on ili farmaceutski prihvatljiva sol, stereoizomer ili tautomer istog.
8. Spoj u skladu s patentnim zahtjevom 1, naznačen time, da je spoj 1-(trans-4-hidroksicikloheksil)-7-(6-(2-hidroksipropan-2-il)piridin-3-il)-3,4-dihidropirazino[2,3-b]pirazin-2(1H)-on ili farmaceutski prihvatljiva sol, stereoizomer ili tautomer istog.
9. Spoj u skladu s patentnim zahtjevom 1, naznačen time, da je spoj 1-((1S,3R)-3-metoksiciklopentil)-7-(2-metil-6-(4H-1,2,4-triazol-3-il)piridin-3-il)-3,4-dihidropirazino[2,3-b]pirazin-2(1H)-on ili farmaceutski prihvatljiva sol, stereoizomer ili tautomer istog.
10. Spoj u skladu s patentnim zahtjevom 1, naznačen time, da je spoj 7-(6-(2-hidroksipropan-2-il)pyudin-3-il)-1-(trans-4-metoksicikloheksil)-3,4-dihidropirazino[2,3-b]pirazin-2(1H)-on ili farmaceutski prihvatljiva sol, stereoizomer ili tautomer istog.
11. Spoj u skladu s patentnim zahtjevom 1, naznačen time, da je spoj 7-(6-(2-hidroksipropan-2-il)pyudin-3-il)-1-((1R,3S)-3-metoksiciklopentil)-3,4-dihidropirazino[2,3-b]pirazin-2(1H)-on ili farmaceutski prihvatljiva sol, stereoizomer ili tautomer istog.
12. Spoj u skladu s patentnim zahtjevom 1, naznačen time, da je spoj 1-(cis-4-hidroksicikloheksil)-7-(2-metil-6-(4H-1,2,4-triazol-3-il)piridin-3-il)-3,4-dihidropirazino[2,3-b]pirazin-2(1H)-on ili farmaceutski prihvatljiva sol, stereoizomer ili tautomer istog.
13. Spoj u skladu s patentnim zahtjevom 1, naznačen time, da je spoj 1-((1R,3S)-3-metoksiciklopentil)-7-(2-metil-6-(4H-1,2,4-triazol-3-il)piridin-3-il)-3,4-dihidropirazino[2,3-b]pirazin-2(1H)-on ili farmaceutski prihvatljiva sol, stereoizomer ili tautomer istog.
14. Farmaceutski pripravak, naznačen time, da sadrži učinkovitu količinu spoja u skladu s bilo kojim od patentnih zahtjeva 1 do 13, po izboru prikladan za oralnu, parenteralnu, mukoznu, transdermalnu ili lokalnu primjenu.
15. Spoj u skladu s bilo kojim od patentnih zahtjeva 1 do 13 ili farmaceutski pripravak u skladu s patentnim zahtjevom 14, naznačen time, da se koristi u postupku liječenja ili sprječavanja karcinoma, upalnih stanja, imunoloških stanja, neurodegenerativnih bolesti, dijabetesa, pretilosti, neuroloških poremećaja, bolesti povezanih sa starosnom dobi ili srčanožilnih stanja.
16. Spoj ili farmaceutski pripravak za uporabu u skladu s patentnim zahtjevom 15, naznačen time, da je karcinom glave, vrata, oka, usta, grla, jednjaka, bronhija, grkljana, ždrijela, prsa, kosti, pluća, debelog crijeva, rektuma, želuca, prostate, mokraćnog mjehura, maternice, vrata maternice, dojki, jajnika, mošnji, kože, tiroidne žlijezde, krvi, limfnih čvorova, bubrega, jetre, gušterače, mozga, središnjeg živčanog sustava ili solidni tumori i tumori krvi; ili kada je upalno stanje psorijaza, astma, alergijski rinitis, bronhitis, kronična opstruktivna plućna bolest, cistična fibroza, upalna bolest crijeva, sindrom iritabilnog crijeva, Crohnova bolest, sluzavi kolitis, ulcerozni kolitis ili pretilost; ili kada je imunološko stanje reumatoidni artritis, reumatoidni spondilitis, osteoartritis, multipla skleroza, lupus, upalna bolest crijeva, ulceracijski kolitis, Crohnova bolest, mijastenija gravis, Gravova bolest, encefalomijelitis, dijabetes tipa II, dermatomiozitis ili odbacivanje usadka; ili kada je stanje povezano sa starosnom dobi te uzrokuje karcinom, pretilost, dijabetes melitus tipa II, autoimunu bolest, srčanožilnu bolest ili neuronske degeneracije.
17. Spoj u skladu s bilo kojim od patentnih zahtjeva 1 do 13 ili farmaceutski pripravak u skladu s patentnim zahtjevom 14, naznačen time, da se koristi u inhibiciji kinaze u stanici u kojoj je ekspresija rečene kinaze, po izboru gdje je kinaza mTOR, DNA-PK ili PI3K ili kombinacija istih.
18. In vitro postupak inhibicije kinaze u stanici u kojoj je ekspresija rečene kinaze, naznačena time, da se sastoji od dovođenja u dodir rečene stanice s učinkovitom količinom spoja iz bilo kojeg od patentnih zahtjeva 1 do 13, po izboru gdje je kinaza mTOR, DNA-PK ili PI3K ili kombinacija istih.
19. Spoj u skladu s bilo kojim od patentnih zahtjeva 1 do 13 ili farmaceutski pripravak u skladu s patentnim zahtjevom 14, naznačen time, da se koristi u postupku liječenja ili sprječavanja stanja koja se mogu liječiti ili spriječiti inhibicijom putova kinaze, po izboru kada je put kinaze mTOR/PI3K/Akt put; pri čemu stanje po izboru može biti višestruki mijelom, limfom stanica plašta, difuzni limfom velikih B stanica, akutni mijeloični limfom, folikularni limfom, kronična limfocitna leukemija; karcinom dojke, pluća, endometrija, jajnika, želuca, vrata ili prostate; glioblastoma; karcinoma bubrega; hepatocelularnog karcinoma; karcinoma debelog crijeva; neuroendokrinih tumora; tumora glave i vrata; sarkoma; tumorskih sindroma koji proizilaze izravno ili neizravno iz genetskih nedostataka u PTEN, TSC1, TSC2, NF1, AMPK, LKB1, VHL or PKD1; Cowdenova bolest, Cowdenov sindrom, Cowdenu-sličan sindrom, Bannayan-Zonana sindrom, Bannayan-Riley-Ruvalcaba sindrom, Lhermitte-Duclos bolest, karcinom endometrija, kompleks gomoljaste skleroze, limfangiolejomiomatoza, neurofibromatoza 1, Peutz-Jeghers sindrom, karcinom stanica bubrega, von Hippel-Lindau bolest, Proteus sindrom ili policistična bolest bubrega; reumatoidni artritis; reumatoidni spondilitis; osteoartritis; giht; astma, bronhitis; alergijski rinitis; kronična opstruktivna plućna bolest; cistična fibroza; upalna bolest crijeva; sindroma iritabilnog kolona; sluzav kolitis; ulceroznog kolitisa; Crohnova bolest; Huntingtonove bolesti; gastritis; ezofagitis; hepatitis; pankreatitisa; nefritis; Multipla skleroza; eritemski lupus; ateroskleroza; restenoze nakon angioplastike; hipertrofije lijeve klijetke; infarkt miokarda; moždani udar; ishemijskog oštećenja srca, pluća, crijeva, bubrega, jetre, gušterače, slezene i mozga; akutna ili kronična odbacivanja presađenog organa; očuvanje organa za transplantaciju; zatajenja organa ili gubitak udova; transplantacijske bolesti; endotoksinski šok; višestruko otkazivanje organa; psorijaza; opekline uslijed izloženosti požaru, kemikalijama ili zračenju; ekcem; dermatitis; presatka kože; ishemije; ishemična stanja povezanih s kirurgijom ili traumatskim ozljedama; epilepsija; Alzheimerova bolest; Parkinsonova bolest; imunološki odgovor na bakterijske ili virusne infekcije; kaheksiju; angiogenih i proliferativnih bolesti.
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HRP20171069TT HRP20171069T1 (hr) | 2008-10-27 | 2017-07-12 | Inhibitori mtor kinaze za onkološke indikacije i bolesti povezane s putom mtor/p13k/akt |
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