SI2684880T1 - Derivat dispiropirolidina - Google Patents
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Claims (24)
- DERIVAT DISPIROPIROLIDINA PATENTNI ZAHTEVKI1. Spojina, ki je predstavljena s splošno formulo (1), ali njena sol:kjer obroč A predstavlja spiro-vezani 4- do 6-členski nasičeni ogljikovodikov obroč, ki ima lahko enega ali več substituentov, izbranih iz skupine 1, ali spiro-vezani 6-členski nasičeni heterociklični obroč, ki ima lahko enega ali več substituentov, izbranih iz skupine 1; obroč B predstavlja benzenski obroč, ki ima lahko enega ali več substituentov, izbranih iz skupine 2, piridinski obroč, ki ima lahko enega ali več substituentov, izbranih iz skupine 2, ali pirimidinski obroč, ki ima lahko enega ali več substituentov, izbranih iz skupine 2; R1 predstavlja arilno skupino, ki ima lahko enega ali več substituentov, izbranih iz skupine 3, heteroarilno skupino, ki ima lahko enega ali več substituentov, izbranih iz skupine 3, C3-C6 cikloalkilno skupino, ki ima lahko enega ali več substituentov, izbranih iz skupine 3, ali C3-C6cikloalkenilno skupino, ki ima lahko enega ali več substituentov, izbranih iz skupine 3; R2 predstavlja CrC6 alkilno skupino, ki je lahko substituirana z enim ali več halogenimi atomi ali z eno ali več hidroksi skupinami, ali atom dušika; in R3 predstavlja skupino, ki je predstavljena z naslednjimi splošnimi formulami (2), (3) ali (4):kjer v formuli (2) R4 in R5 vsak neodvisno predstavljata hidroksi skupino, C1-C6 alkilno skupino ali C1-C6 alkoksi skupino, ali R4 in R5, skupaj z ogljikovimi atomi, na katere sta vezani skupina R4 oziroma skupina R5, lahko tvorita 4- do 6-členski nasičeni ogljikovodikov obroč; v formuli (3) prekinjena črta v obročni strukturi nakazuje, da je vez morda dvojna vez, R6 predstavlja C1-C6 alkilno skupino, ki ima lahko enega ali več substituentov, izbranih iz skupine 4, karbamoilno skupino, ki ima lahko enega ali več substituentov, izbranih iz skupine 5, 5- ali 6-člensko heteroarilno skupino, ki vsebuje dušik in ki je lahko substituirana z okso skupino ali z eno ali več C1-C6 alkilnimi skupinami, ki so lahkosubstituirane z okso skupino ali z eno hidroksi skupino, hidroksi skupino, ali -NR’R”, kjer R’ in R” vsak neodvisno predstavljata C1-C6 alkilno skupino, ki je lahko substituirana z enim ali več halogenimi atomi, z okso skupino ali z od eno do tremi hidroksi skupinami, C3-C4 cikloalkilno skupino, ki je lahko substituirana z od enim do tremi halogenimi atomi ali z od eno do tremi hidroksi skupinami, ali atom dušika, ali R’ in R” skupaj z dušikovim atomom, na katerega sta vezana R’ in R”, lahko tvorita od 4- do 7-člensko heterociklično skupino, ki vsebuje dušik in ki ima lahko enega ali več substituentov, izbranih iz C1-C6 alkilne skupine in hidroksi skupine. R7 predstavlja C1-C6 alkilno skupino, ki je lahko substituirana z eno hidroksi skupino, s hidroksi skupino ali z atomom dušika, ali R6 in R7 lahko skupaj tvorita spiro-vezani 4- do 6-členski ogljikovodikov obroč ali spiro-vezani 4- do 6-členski heterociklični obroč, ki vsebuje dušik. R8 je odsoten ali predstavlja enega ali več substituentov, izbranih iz hidroksi skupine, Ci-C6 alkil skupine in C1-C6 alkoksi skupine, in Z predstavlja CH2, NH ali kisikov atom; in v formuli (4) R9 predstavlja C1-C6 alkilno skupino, ki ima lahko enega ali več substituentov, izbranih iz skupine 4, karbamoil skupino, ki ima lahko enega ali več substituentov, izbranih iz skupine 5, 5- ali 6-člensko heteroarilno skupino, ki vsebuje dušik in ki je lahko substituirana z okso skupino ali z eno ali več C1-C6 alkil skupinami, ki so lahko substituirane z okso skupino ali z eno hidroksi skupino, s hidroksi skupino, ali -NR’R”, kjer R’ in R” vsak neodvisno predstavljata C-i-Ce alkilno skupino, ki je lahko substituirana z od enim do tremi halogenimi atomi, z okso skupino ali z od eno do tremi hidroksi skupinami, C3-C4 cikloalkilno skupino, ki je lahko substituirana z od enim do tremi halogenimi atomi ali z od eno do tremi hidroksi skupinami, ali atom dušika, ali R’ in R” skupaj z dušikovim atomom, na katerega sta vezana R’ in R”, lahko tvorita od 4- do 7-člensko heterociklično skupino, ki vsebuje dušik in ki ima lahko enega ali več substituentov, izbranih iz Ο-ι-Οθ alkilne skupine in hidroksi skupine. R10 predstavlja C1-C6 alkilno skupino, ki je lahko substituirana z eno hidroksi skupino, s hidroksi skupino ali z atomom dušika, ali R9 in R10 lahko skupaj tvorita spiro-vezani 4- do 6-členski ogljikovodikov obroč ali spiro-vezani 4- do 6-členski heterociklični obroč, ki vsebuje dušik, in R11 je odsoten ali predstavlja enega ali več substituentov, izbranih iz hidroksi skupine, C1-C6 alkilne skupine in C1-C6 alkoksi skupine: Skupina 1: halogeni atom, CrC6 alkilna skupina, ki je lahko substituirana z od enim do treh halogenih atomov, Ci-Ce alkoksi skupina in ciano skupina, Skupina 2: halogeni atom, C1-C6 alkilna skupina, ki je lahko substituirana z od enim do treh halogenih atomov, C3-C4 cikloalkilna skupina, ki je lahko substituirana z od enim do treh halogenih atomov, vinilna skupina, etinilna skupina, ciano skupina in C1-C6 alkoksi skupina, Skupina 3: halogeni atom, C1-C6 alkilna skupina, ki je lahko substituirana z od enim do treh halogenih atomov ali z od eno do tremi hidroksi skupinami, C3-C4 cikloalkilna skupina, ki je lahko substituirana z od enim do treh halogenih atomov ali z od eno do treh hidroksi skupin, vinilna skupina, etinilna skupina, ciano skupina, -OR’, -NR’R”, -COOR’ in -CONHR’, kjer R’ in R” vsak neodvisno predstavljata C1-C6 alkilno skupino, ki je lahko substituirana z od enim do tremi halogenimi atomi ali z od eno do tremi hidroksi skupinami, C3-C4 cikloalkilno skupino, ki je lahko substituirana z od enim do tremi halogenimi atomi ali z od eno do tremi hidroksi skupinami, ali atom dušika, ali R’ in R” skupaj z dušikovim atomom, na katerega sta vezana R’ in R”, lahko tvorita od 4- do 7-člensko heterociklično skupino, ki vsebuje dušik in ki ima lahko enega ali več substituentov, izbranih iz C1-C6 alkilne skupine in hidroksi skupine. Skupina 4: halogeni atom, hidroksi skupina, karbamoil skupina, morfolino skupina, Ci-C6alkoksi skupina, C1-C6 alkilsulfonil skupina in -NR’R”, kjer R’ in R” vsak neodvisno predstavljata C1-C6 alkilno skupino, ki je lahko substituirana z od enim do tremi halogenimi atomi, z od eno do tremi hidroksi skupinami, ali okso skupino, C3-C4 cikloalkilno skupino, ki je lahko substituirana z od enim do tremi halogenimi atomi ali z od eno do tremi hidroksi skupinami, ali atom dušika, ali R’ in R” skupaj z dušikovim atomom, na katerega sta vezana R’ in R”, lahko tvorita od 4- do 7-člensko heterociklično skupino, ki vsebuje dušik in ki ima lahko enega ali več substituentov, izbranih iz C1-C6 alkilne skupine in hidroksi skupine, in Skupina 5: C1-C6 alkilna skupina, ki je lahko substituirana z od enim do tremi halogenimi atomi, z od enim do tremi hidroksi skupinami, ali Ο-ι-Οθ alkoksi skupina, C3-C6 cikloalkilna skupina, C1-C6 alkoksi skupina in tetrahidropiranilna skupina.
- 2. Spojina po zahtevku 1, kjer obroč B predstavlja benzenski obroč, ki ima lahko enega ali več substituentov, ki so vezani na 5- ali 6-položaj, izbran izmed halogenega atoma, C1-C6 alkilne skupine, ki je lahko substituirana z od enim do tremi halogenimi atomi, ciano skupine ter C1-C6 alkoksi skupine.
- 3. Spojina po zahtevku 1, kjer obroč B predstavlja piridinski obroč, ki ima lahko enega substituenta, ki je vezan na 6-položaj in je izbran iz halogenega atoma, C1-C6 alkilne skupine, ki je lahko substituirana z od enim do tremi halogenimi atomi, ciano skupine in od Ο-Οβ alkoksi skupine.
- 4. Spojina po kateremkoli izmed predhodnih zahtevkov, kjer R1 predstavlja fenilno skupino, ki ima lahko en atom klora, vezan na 3-položaj, ali atom klora in atom fluora, vezana na 3- oziroma na 2-položaj.
- 5. Spojina po kateremkoli izmed zahtevkov od 1 do 3, kjer R1 predstavlja piridilno skupino, ki ima lahko en atom klora, vezan na 2-položaj, ali atom klora in atom fluora, vezana na 2- oziroma 3-položaj.
- 6. Spojina po zahtevku 1, ki je predstavljena s splošno formulo (7), ali njena sol: kjerimajo obroči A, R2 in R3 enake pomene kot obroč A, R2 oziroma R3 v zahtevku 1;R12, R13 in R16 predstavljajo skupino, ki je izbrana iz halogenega atoma, C1-C6 alkilne skupine, ki je lahko substituirana z od enim do tremi halogenimi atomi, ter ciano skupino; in R14 je odsoten ali predstavlja enega ali več substituentov, izbranih iz halogenega atoma, C1-C6 alkilne skupine, ki je lahko substituirana z od enim do tremi halogenimi atomi, in ciano skupino.
- 7. Spojina po zahtevku 1, ki je predstavljena s splošno formulo (8), ali njena sol: kjerimajo obroči A, R2 in R3 enake pomene kot obroč A, R2 oziroma R3 v zahtevku 1; R12, R13 in R16 predstavljajo skupino, ki je izbrana iz halogenega atoma, C1-C6 alkilne skupine, ki je lahko substituirana z od enim do tremi halogenimi atomi, ter ciano skupino; in R14 je odsoten ali predstavlja enega ali več substituentov, izbranih iz halogenega atoma, C1-C6 alkilne skupine, ki je lahko substituirana z od enim do tremi halogenimi atomi, in ciano skupino.
- 8. Spojina po zahtevku 1, ki je izbrana iz naslednjih skupin, ali njena sol:
- 9. Spojina po zahtevku 1, ki je (3'R,4'S,5'R)-N-[(3R,6S)-6-karbamoiltetrahidro-2H-piran-3-il]-6"-kloro-4,-(2-kloro-3-fluoropiridin-4-il)-4,4-dimetil-2"-okso-1",2"-dihidrodispiro[cikloheksan-1,2'-pirolidin-3',3"-indol]-5'-larboksamid hidroklorid.
- 10. Spojina po zahtevku 1, ki je (3'R,4'S,5'R)-N-[(3R,6S)-6-karbamoiltetrahidro-2H-piran-3-il]-6"-kloro-4'-(2-kloro-3-fluoropiridin-4-il)-4,4-dimetil-2"-okso-1",2"-dihidrodispiro[cikloheksan-1,2'-pirolidin-3',3"-indol]-5'-karboksamid sulfat.
- 11. Spojina po zahtevku 1, ki je (3'R,4'S,5'R)-N-[(3R,6S)-6-karbamoiltetrahidro-2H-piran-3-il]-6"-kloro-4'-(2-kloro-3-fluoropiridin-4-il)-4,4-dimetil-2"-okso-1"l2"-dihidrodispiro[cikloheksan-1,2'-pirolidin-3',3"-indol]-5'-karboksamid metansulfonat.
- 12. Spojina po zahtevku 1, ki je (3'R,4'S,5'R)-N-[(3R,6S)-6-karbamoiltetrahidro-2H-piran-3-il]-6"-kloro-4,-(2-kloro-3-fluoropiridin-4-il)-4,4-dimetil-2"-okso-1",2"-dihidrodispiro[cikloheksan-1,2'-pirolidin-3',3"-indol]-5'-karboksamid etansulfonat.
- 13. Spojina po zahtevku 1, ki je (3'R,4'S,5'R)-N-[(3R,6S)-6-karbamoiltetrahidro-2H-piran-3-il]-6"-kloro-4'-(2-kloro-3-fluoropiridin-4-il)-4,4-dimetil-2"-okso-1",2"-dihidrodispiro[cikloheksan-1,2'-pirolidin-3',3"-indol]-5'-karboksamid benzensulfonat.
- 14. Spojina po zahtevku 1, ki je (3'R,4'S,5'R)-N-[(3R,6S)-6-karbamoiltetrahidro-2H-piran-3-il]-6"-kloro-4'-(2-kloro-3-fluoropiridin-4-il)-4,4-dimetil-2"-okso-1",2"-dihidrodispiro[cikloheksan-1,2'-pirolidin-3',3"-indol]-5'-karboksamid p-toluensulfonat.
- 15. Spojina po zahtevku 1, ki je (3'R,4,S,5'R)-6"-kloro-4,-(2-kloro-3-fluoropiridin-4-il)-N-{(3R,6S)-6-[1-hidroksietil]tetrahidro-2H-piran-3-il}-4,4-dimetil-2"-okso- 1 ",2"-dihidrodispiro[cikloheksan-1,2'-pirolidin-3',3"-indol]-5'-karboksamid benzensulfonat. 16. (2S,5R)-5-({[(3'R,4,S,5'R)-6"-kloro-4,-(2-kloro-3-fluoropiridin-4-il)-4,4-dimetil-2"-okso-1",2"-dihidrodispiro[cikloheksan-1,2,-pirolidin-3',3"-indol]-5'-il]karbonil}amino)tetrahidro-2H-piran-2-karboksilna kislina.
- 17. Zdravilo, ki vsebuje spojino po kateremkoli izmed zahtevkov od 1 do 8 ali njeno sol, ali spojino po kateremkoli izmed zahtevkov od 9 do 16, kot aktivno sestavino.
- 18. Farmacevtska sestava, ki vsebuje spojino po kateremkoli izmed zahtevkov od 1 do 8 ali njeno sol, ali spojino po kateremkoli izmed zahtevkov od 9 do 16 ter farmacevtsko sprejemljivi nosilec.
- 19. Spojina po kateremkoli izmed zahtevkov od 1 do 8 ali njena sol, ali spojina po kateremkoli izmed zahtevkov od 9 do 16, za uporabo kot zaviralec Mdm2.
- 20. Spojina po kateremkoli izmed zahtevkov od 1 do 8 ali njena sol, ali spojina po kateremkoli izmed zahtevkov od 9 do 16, za uporabo kot zaviralec Mdm2 ubikvitin ligaze.
- 21. Spojina po kateremkoli izmed zahtevkov od 1 do 8 ali njena sol, ali spojina po kateremkoli izmed zahtevkov od 9 do 16, za uporabo kot zaviralec p53-Mdm2 veziva.
- 22. Spojina po kateremkoli izmed zahtevkov od 1 do 8 ali njena sol, ali spojina po kateremkoli izmed zahtevkov od 9 do 16, za uporabo kot zaviralec p53 transkripcijske aktivnosti.
- 23. Spojina po kateremkoli izmeed zahtevkov od 1 do 8 ali njena sol, ali spojina po kateremkoli izmed zahtevkov od 9 do 16, za uporabo kot zaviralec p53 degradacije.
- 24. Spojina po kateremkoli izmed zahtevkov od 1 do 8 ali njena sol, ali spojina po kateremkoli izmed zahtevkov od 9 do 16, za uporabo za zdravljenje raka.
- 25. Spojina za uporabo po zahtevku 24, kjer je rak rak na pljučih, rak na dojkah, rak na prostati, rak na črevesju, akutna mieloična levkemija, maligni limfom, retinoblastom, nevroblastom ali sarkom.
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