SI2643322T1 - Soli in kristalinične oblike apoptozo inducirajočega sredstva - Google Patents
Soli in kristalinične oblike apoptozo inducirajočega sredstva Download PDFInfo
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- C—CHEMISTRY; METALLURGY
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- C07D471/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
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- A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
- A61K31/4353—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom ortho- or peri-condensed with heterocyclic ring systems
- A61K31/437—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom ortho- or peri-condensed with heterocyclic ring systems the heterocyclic ring system containing a five-membered ring having nitrogen as a ring hetero atom, e.g. indolizine, beta-carboline
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- A61K31/4353—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom ortho- or peri-condensed with heterocyclic ring systems
- A61K31/4375—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom ortho- or peri-condensed with heterocyclic ring systems the heterocyclic ring system containing a six-membered ring having nitrogen as a ring heteroatom, e.g. quinolizines, naphthyridines, berberine, vincamine
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- A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
- A61K31/496—Non-condensed piperazines containing further heterocyclic rings, e.g. rifampin, thiothixene or sparfloxacin
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Claims (35)
- EP 2 643 322 BI Soli in kristalinične oblike apoptozo inducirajočega sredstva Patentni zahtevki1. Spojina, ki ima sistematično ime 4-(4-{[2-(4-klorofenil)-4,4-dimetilcikloheks-l-en-l-il]metil}piperazin-l-il)-N-({3-nitro-4-[(tetrahidro-2H-piran-4-ilmetil)amino]fenil}sulfonil)-2-(lH-pirolo[2,3-b]piridin-5-iloksi)benzamid (spojina 1) ali njena sol v kristalinični obliki.
- 2. Spojina po zahtevku 1, kjer je kristalinična oblika anhidrat proste baze spojine 1, označen s tem, da ima rentgenski praškovni difraktogram, ki ima vsaj en vrh, izbran izmed tistih pri 6,3, 7,1, 9,0, 9,5, 12,5, 14,5, 14,7, 15,9, 16,9, in 18,9 stopinj 2Θ (vzorec A), pri čemer je vsak vrh ± 0,2 stopinj 2Θ, kadar izmerimo pri okoli 25 °C s Cu Ka sevanjem pri 1,54178 A.
- 3. Spojina po zahtevku 1, kjer je kristalinična oblika anhidrat proste baze spojine 1, označen s tem, da ima rentgenski praškovni difraktogram, ki ima vsaj en vrh, izbran izmed tistih pri 5,8, 7,7, 8,3, 9,9, 13,0, 13,3, 14,2, 15,3, 16,6, 17,9, 18,3, 19,8, 20,7, 21,2, 21,9, 22,5, 23,6 in 24,1 stopinj 20 (vzorec B), pri čemer je vsak vrh ± 0,2 stopinj 20, kadar merimo pri okoli 25 °C s Cu Ka sevanjem pri 1,54178 A.
- 4. Spojina po zahtevku 1, kjer je kristalinična oblika hidrat proste baze spojine 1 označen s tem, da ima rentgenski praškovni difraktogram, ki ima vsaj en vrh, izbran izmed tistih pri 5,8, 7,6, 7,9, 10,7, 11,7, 14,0, 15,3, 15,8, 17,4, 18,3, 19,9, 20,4, 20,7, 22,5, 24,9, 25,8 in 26,7 stopinj 20 (vzorec C), pri čemer je vsak vrh ± 0,2 stopinj 20, kadar ga izmerimo pri okoli 25 °C s Cu Ka sevanjem pri 1,54178 A.
- 5. Spojina po zahtevku 1, kjer je kristalinična oblika hidrat proste baze spojine 1, označen s tem, da ima rentgenski praškovni difraktogram, ki ima vsaj en vrh, izbran izmed tistih pri 3,3, 6,4, 7,1, 7,3, 10,1, 11,4, 13,2, 14,4, 14,6, 15,1, 15,8, 16,2, 17,2, 17,6, 18,0, 18,6, 19,0, 19,5, 19,8, 20,2, 20,7, 21,0, 22,5, 23,0, 26,0, 28,9 in 29,2 stopinj 20 (vzorec D), pri čemer je vsak vrh ± 0,2 stopinj 20, kadar ga izmerimo pri okoli 25 °C s Cu Ka sevanjem pri 1,54178 A.
- 6. Spojina po zahtevku 1, kjer je kristalinična oblika diklorometan solvat proste baze spojine 1, označena s tem, da ima rentgenski praškovni difraktogram, ki ima vsaj en vrh, izbran izmed tistih pri 5,9, 7,1, 9,6, 10,0, 10,7, 11,1, 13,2, 14,8 in 18,2 stopinj 20, pri čemer je vsak vrh ± 0,2 stopinj 20 (vzorec E), kadar ga izmerimo pri okoli 25 °C s Cu Ka sevanjem pri 1,54178 A.
- 7. Spojina po zahtevku 1, kjer je kristalinična oblika diklorometan solvat proste baze spojine 1, označen s tem, da ima monolitski tip mreže in P21/n prostorsko skupino, ki ima dolžine enotske celice za tri osi okoli (a) 13,873 A, (b) 12,349 A, (c) 29,996 A in tri kote enotske celice okoli (a) 90,00°, (β) 92,259° in (γ) 90,00°.
- 8. Spojina po zahtevku 1, kjer je kristalinična oblika etilacetatni solvat proste baze spojine 1, označen s tem, da ima rentgenski praškovni difraktogram, ki ima vsaj en vrh, izbran izmed tistih pri 5,8, 7,1, 9,5, 9,9, 10,6, 11,6, 13,1, 13,8, 14,8, 16,0, 17,9, 20,2, 21,2, 23,2, 24,4 in 26,4 stopinj 20 (vzorec F), pri čemer je vsak vrh ± 0,2 stopinj 20, kadar ga izmerimo pri okoli 25 °C s Cu K„ sevanjem pri 1,54178 A.
- 9. Spojina po zahtevku 1, kjer je kristalinična oblika etilacetatni solvat proste baze spojine 1, označen s tem, da ima rentgenski praškovni difraktogram, ki ima vsaj en vrh, izbran izmed tistih pri 3,3, 6,5, 7,0, 7,3, 9,2, 9,7, 11,2, 11,4, 11,9, 12,9, 14,4, 14,9, 15,8, 16,2, 17,2, 17,4, 17,8, 18,5, 18,9, 19,4, 20,1, 20,7, 20,9, 22,0, 22.7, 23,4, 23,8, 24,7, 25,9, 27,0 in 28,9 stopinj 20 (vzorec G), pri čemer je vsak vrh ± 0,2 stopinj 20, kadar ga izmerimo pri okoli 25 °C s Cu Ka sevanjem pri 1.54178 A.
- 10. Spojina po zahtevku 1, kjer je kristalinična oblika acetonitrilni solvat proste baze spojine 1, označen s tem, da ima rentgenski praškovni difraktogram, ki ima vsaj en vrh, izbran izmed tistih pri 5,8, 7,4, 7,6, 10,2, 13,0, 13,6, 14,9, 16,4, 17,0, 17,5, 18.2, 19,4, 19,7, 20,4, 21,0, 21,2, 21,8, 22,4, 22,9, 24,2, 24,3, 26,1 in 29,2 stopinj 20 (vzorec H), pri čemer je vsak vrh ± 0,2 stopinj 20, kadar ga izmerimo pri okoli 25 °CsCuKe sevanjem pri 1,54178 A.
- 11. Spojina po zahtevku 1, kjer je kristalinična oblika acetonitrilni solvat proste baze spojine 1, označen s tem, da ima triklinski tip mreže in Pl prostorsko skupino, ki ima dolžine enotske celice za tri osi okoli (a) 12,836 A, (b) 13,144 A, (c) 15,411 A in tri kote enotske celice okoli (a) 92,746°, (β) 95,941° in (γ) 113,833°.
- 12. Spojina po zahtevku 1, kjer je kristalinična oblika acetonitrilni solvat proste baze spojine 1, označen s tem, da ima rentgenski praškovni difraktogram, ki ima vsaj en vrh, izbran izmed tistih pri 6,4, 6,9, 7,7, 8,8, 9,4, 11,1, 12,3, 12,8, 16,5, 17,0, 17,4, 18,3, 18,6, 19,0, 19,2, 20,3, 21,6, 22,3, 22,9 in 23,7 stopinj 20 (vzorec I), pri čemer je vsak vrh ± 0,2 stopinj 20, kadar ga izmerimo pri okoli 25 °C s Cu K<, sevanjem pri 1,54178 A.
- 13. Spojina po zahtevku 1, kjer je kristalinična oblika acetonitrilni solvat proste baze spojine 1, označen s tem, da ima rentgenski praškovni difraktogram, ki ima vsaj en vrh, izbran izmed tistih pri 6,0, 6,8, 8,0, 9,0, 9,7, 11,2, 11,9, 12,6, 14,7, 15,0, 15.2, 15,8, 16,4, 16,6, 17,6, 17,8, 17,9, 18,7, 20,2, 20,8, 21,6, 22,2, 22,6, 23,3, 23.8, 24,0, 24,4, 26,8, 27,1, 28,0 in 28,2 stopinj 20 (vzorec J), pri čemer je vsak vrh ± 0,2 stopinj 20, kadar ga izmerimo pri okoli 25 °C s Cu K« sevanjem pri 1.54178 A.
- 14. Sol po zahtevku 1, kjer je kristalinična oblika hidroklorid spojine 1, označen s tem, da ima rentgenski praškovni difraktogram, ki ima vsaj en vrh, izbran izmed tistih pri 5,1, 5,9, 7,7, 9,9, 10,2, 10,8, 13,6, 14,0, 15,4, 15,9, 16,2, 17,6, 18,3, 18,7, 19,7, 19,9, 20,1, 20,4, 20,7, 20,9, 22,9 in 26,2 stopinj 20 (vzorec K), pri čemer je vsak vrh ± 0,2 stopinj 20, kadar ga izmerimo pri okoli 25 °C s Cu Ka sevanjem pri 1,54178 A.
- 15. Sol po zahtevku 1, kjer je kristalinična oblika hidroklorid spojine 1, označen s tem, da ima triklinski tip mreže in Pl prostorsko skupino, ki ima dolžine enotske celice za tri osi okoli (a) 10,804 A, (b) 12,372 A, (c) 19,333 A in tri kote enotske celice okoli (a) 76,540°, (p) 87,159° in (γ) 70,074°.
- 16. Sol po zahtevku 1, kjer je kristalinična oblika hidroklorid hidrat spojine 1, označen s tem, da ima rentgenski praškovni difraktogram, ki ima vsaj en vrh, izbran izmed tistih pri 4,6, 8,7, 9,6, 9,9, 12,3, 14,9, 15,7, 17,6, 18,1, 18,4, 19,3, 19,6, 21,0, 23,3, 23,9, 24,8, 26,5, 27,2, 27,4, 29,0 in 30,1 stopinj 20 (vzorec L), pri čemer je vsak vrh ± 0,2 stopinj 20, kadar ga izmerimo pri okoli 25 °C s Cu Ka sevanjem pri 1,54178 A.
- 17. Sol po zahtevku 1, kjer je kristalinična oblika sulfat spojine 1, označen s tem, da ima rentgenski praškovni difraktogram, ki ima vsaj en vrh, izbran izmed tistih pri 4,8, 7,7, 8,3, 9,7, 10,2, 12,0, 12,6, 14,5, 15,4, 17,4, 17,9, 18,4, 19,1, 19,5, 21,0, 22,4, 23,3, 23,9, 25,1 in 26,8 stopinj 20 (vzorec M), pri čemer je vsak vrh ± 0,2 stopinj 20, kadar ga izmerimo pri okoli 25 °C s Cu K„ sevanjem pri 1,54178 A.
- 18. Farmacevtski sestavek, ki obsega spojino ali sol po katerem koli od zahtevkov 1 do 17 in en ali več farmacevtsko sprejemljivih ekscipientov.
- 19. Postopek za pripravo farmacevtske raztopine spojine 1 ali njene soli, ki obsega raztapljanje spojine ali soli po katerem koli od zahtevkov 1 do 17 v farmacevtsko sprejemljivem topilu ali zmesi topil.
- 20. Spojina ali sol po katerem koli od zahtevkov 1 do 17 ali farmacevtski sestavek, ki obsega spojino ali sol po katerem koli od zahtevkov 1 do 17 in en ali več farmacevtsko sprejemljivih ekscipientov za uporabo v postopku za zdravljenje bolezni, ki je značilna po apoptotski difimkciji in/ali prekomerni ekspresiji anti-apoptotskega Bcl-2 družinskega proteina ("Bcl-2 family protein"), kjer je bolezen neoplastična, imunska ali avtoimunska bolezen.
- 21. Spojina ali sol ali farmacevtski sestavek za uporabo po zahtevku 20, kjer naveden postopek obsega dajanje navedene spojine ali soli ali navedenega farmacevtskega sestavka po oralni, parenteralni, sublingvalni, bukalni, intranazalni, pljučni, topični, transdermalni, intradermalni, okulami, otični, rektalni, vaginalni, intragastrični, intrakranialni, intrasinovialni ali intraartikulami poti.
- 22. Spojina ali sol ali farmacevtski sestavek za uporabo po zahtevku 20, kjer je neoplastična bolezen izbrana iz skupine, ki jo sestavljajo rak, mezoteliom, rak sečnega mehurja, pankreatični rak, rak kože, rak glave ali vratu, kožni ali intraokulami melanom, ovarijski rak, rak dojke, rak maternice, karcinom jajcevodov, karcinom endometrija, karcinom, cerviksa, karcinom vagine, karcinom vulve, kostni rak, rak kolona, rektalni rak, rak analne regije, rak želodca, gastrointestinalni rak, gastrični rak, kolorektalni rak, duodenalni rak, kronična limfocitna levkemija, ezofagealni rak, rak tankega črevesa, rak endokrinega sistema, rak ščitnice, rak obščitnice, rak nadledvične žleze, sarkom, mehkega tkiva, rak uretra, rak penisa, testikulami rak, hepatocelulami rak, hepatični rak, rak žolčevoda, primarni ali sekundami tumor centralnega živčnega sistema, primarni ali sekundami tumor možganov, Hodgkinova bolezen, kronična ali akutna levkemija, kronična mieloidna levkemija, limfocitni limfom, limfoblastna levkemija, folikulami limfom, limfoidna malignost T-celičnega ali B-celičnega izvora, melanom, multipli mielom, oralni rak, nedrobnocelični pljučni rak, rak prostate, drobnocelični pljučni rak, rak ledvic in/ali sečevoda, karcinom renalnih celic, karcinom renalnega pelvisa, neoplazma centralnega živčnega sistema, primarni limfom centralnega živčnega sistema, ne-Hodgkinov limfom, tumor spinalne osi, gliom možganskega debla, adenom hipofize, adrenokortikalni rak, rak žolčnika, rak vranice, holangiokarcinom, fibrosarkom, nevroblastom, retinoblastom in njihove kombinacije.
- 23. Spojina ali sol ali farmacevtski sestavek za uporabo po zahtevku 20, kjer je bolezen limfoidna malignost.
- 24. Spojina ali sol ali farmacevtski sestavek za uporabo po zahtevku 23, kjer je limofidna malignost ne-Hodgkinov limfom, kronična limfoidna levkemija ali akutna limfocitna levkemija.
- 25. Spojina ali sol ali farmacevtski sestavek za uporabo po zahtevku 20, kjer naveden postopek obsega oralno dajanje navedene spojine ali soli ali navedenega farmacevtskega sestavka v odmerku od okoli 50 mg do okoli 1000 mg spojine 1 ali njene soli na dan pri povprečnem intervalu zdravljenja okoli od 3 ure do okoli 7 dni.
- 26. Spojina ali sol ali farmacevtski sestavek po zahtevku 20, kjer naveden postopek obsega oralno dajanje navedene spojine ali soli ali navedenega farmacevtskega sestavka enkrat dnevno v odmerku od 200 mg do okoli 400 mg ekvivalenta proste baze spojine 1 na dan.
- 27. Disperzija spojine ali soli po katerem koli od zahtevkov 1 do 17 za uporabo v postopku za zdravljenje bolezni, značilne po apoprozni disfunkciji in/ali prekomerni ekspresiji anti-apoptotskega Bcl-2 družinskega proteina, kjer je bolezen neoplastična, imunska ali avtoimunska bolezen.
- 28. Disperzija za uporabo po zahtevku 27, kjer naveden postopek obsega dajanje navedene disperzije po oralni, parenteralni, sublingvalni, bukalni, intranazalni, pljučni, topični, transdermalni, intradermalni, okulami, otični, rektalni, vaginalni, intragastrični, intrakranialni, intrasinovialni ali intraartikulami poti.
- 29. Disperzija za uporabo po zahtevku 27, kjer je neoplastična bolezen izbrana iz skupine, ki jo sestavljajo rak, mezoteliom, rak sečnega mehurja, pankreatični rak, rak kože, rak glave ali vratu, kožni ali intraokulami melanom, ovarijski rak, rak dojke, rak maternice, karcinom jajcevodov, karcinom endometrija, karcinom, cerviksa, karcinom vagine, karcinom vulve, kostni rak, rak kolona, rektalni rak, rak analne regije, rak želodca, gastrointestinalni rak, gastrični rak, kolorektalni rak, duodenalni rak, kronična limfocitna levkemija, ezofagealni rak, rak tankega črevesa, rak endokrinega sistema, rak ščitnice, rak obščitnice, rak nadledvične žleze, sarkom, mehkega tkiva, rak uretra, rak penisa, testikulami rak, hepatocelulami rak, hepatični rak, rak žolčevoda, primarni ali sekundami tumor centralnega živčnega sistema, primarni ali sekundami tumor možganov, Hodgkinova bolezen, kronična ali akutna levkemija, kronična mieloidna levkemija, limfocitni limfom, limfoblastna levkemija, folikulami limfom, limfoidna malignost T-celičnega ali B-celičnega izvora, melanom, multipli mielom, oralni rak, nedrobnocelični pljučni rak, rak prostate, drobnocelični pljučni rak, rak ledvic in/ali sečevoda, karcinom renalnih celic, karcinom renalnega pelvisa, neoplazma centralnega živčnega sistema, primarni limfom centralnega živčnega sistema, ne-Hodgkinov limfom, tumor spinalne osi, gliom možganskega debla, adenom hipofize, adrenokortikalni rak, rak žolčnika, rak vranice, holangiokarcinom, fibrosarkom, nevroblastom, retinoblastom in njihove kombinacije.
- 30. Disperzija za uporabo po zahtevku 27, kjer je bolezen limfoidna malignost.
- 31. Disperzija za uporabo po zahtevku 30, kjer je limfoidna malignost ne-Hodgkinov limfom, kronična limfoidna levkemija ali akutna limfocitna levkemija.
- 32. Disperzija za uporabo po zahtevku 27, kjer naveden postopek obsega oralno dajanje disperzije v odmerku od okoli 50 mg do 1000 mg spojine 1 ali njene soli na dan pri povprečnem intervalu zdravljenja od okoli 3 ur do okoli 7 dni.
- 33. Disperzija za uporabo po zahtevku 27, kjer naveden postopek obsega oralno dajanje navedene disperzije enkrat dnevno v odmerku od okoli 200 mg do okoli 400 mg ekvivalenta proste baze spojine 1 na dan.
- 34. Spojina po zahtevku 1, ki ima sistematično ime 4-(4-{[2-(4-klorofenil)-4,4-dimetilcikloheks-l-en-l-il]metil}piperazin-l-il)-N-({3-nitro-4-[(tetrahidro-2H-piran-4-ilmetil)amino]fenil}sulfonil)-2-(lH-pirolo[2,3-b]piridin-5-iloksi)benzamid hidroklorid v kristalinični obliki.
- 35. Spojina po zahtevku 1, ki ima sistematično ime 4-(4-{[2-(4-klorofenil)-4,4-dimetilcikloheks-1 -en-1 -il]metil}piperazin-1 -il)-N-({3-nitro-4-[(tetrahidro-2H-piran-4-ilmetil)amino]fenil}sulfonil)-2-(lH-pirolo[2,3-b]piridin-5-iloksi)benzamid sulfat v kristalinični obliki.
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