HRP20210165T1 - Čvrsta disperzija amorfnog oblika (r)-1(2,2-difluorobenzo(d)(1,3)dioksol-5-il)-n-(1-(2,3-dihidroksipropil)-6-fluoro-2-(1-hidroksi-2-metilpropan-2-il)-1h-indol-5-il)-ciklopropankarboksamida - Google Patents
Čvrsta disperzija amorfnog oblika (r)-1(2,2-difluorobenzo(d)(1,3)dioksol-5-il)-n-(1-(2,3-dihidroksipropil)-6-fluoro-2-(1-hidroksi-2-metilpropan-2-il)-1h-indol-5-il)-ciklopropankarboksamida Download PDFInfo
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- HRP20210165T1 HRP20210165T1 HRP20210165TT HRP20210165T HRP20210165T1 HR P20210165 T1 HRP20210165 T1 HR P20210165T1 HR P20210165T T HRP20210165T T HR P20210165TT HR P20210165 T HRP20210165 T HR P20210165T HR P20210165 T1 HRP20210165 T1 HR P20210165T1
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- 239000007962 solid dispersion Substances 0.000 title claims 24
- MJUVRTYWUMPBTR-MRXNPFEDSA-N 1-(2,2-difluoro-1,3-benzodioxol-5-yl)-n-[1-[(2r)-2,3-dihydroxypropyl]-6-fluoro-2-(1-hydroxy-2-methylpropan-2-yl)indol-5-yl]cyclopropane-1-carboxamide Chemical compound FC=1C=C2N(C[C@@H](O)CO)C(C(C)(CO)C)=CC2=CC=1NC(=O)C1(C=2C=C3OC(F)(F)OC3=CC=2)CC1 MJUVRTYWUMPBTR-MRXNPFEDSA-N 0.000 title claims 8
- 229920000642 polymer Polymers 0.000 claims 12
- 239000008194 pharmaceutical composition Substances 0.000 claims 11
- 229920000639 hydroxypropylmethylcellulose acetate succinate Polymers 0.000 claims 10
- 239000004094 surface-active agent Substances 0.000 claims 9
- OKKJLVBELUTLKV-UHFFFAOYSA-N Methanol Chemical group OC OKKJLVBELUTLKV-UHFFFAOYSA-N 0.000 claims 6
- 239000003814 drug Substances 0.000 claims 6
- 238000000034 method Methods 0.000 claims 6
- 229940124597 therapeutic agent Drugs 0.000 claims 6
- 201000003883 Cystic fibrosis Diseases 0.000 claims 5
- DBMJMQXJHONAFJ-UHFFFAOYSA-M Sodium laurylsulphate Chemical group [Na+].CCCCCCCCCCCCOS([O-])(=O)=O DBMJMQXJHONAFJ-UHFFFAOYSA-M 0.000 claims 5
- ZUAAPNNKRHMPKG-UHFFFAOYSA-N acetic acid;butanedioic acid;methanol;propane-1,2-diol Chemical compound OC.CC(O)=O.CC(O)CO.OC(=O)CCC(O)=O ZUAAPNNKRHMPKG-UHFFFAOYSA-N 0.000 claims 5
- 201000010099 disease Diseases 0.000 claims 5
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- 230000007812 deficiency Effects 0.000 claims 4
- 201000010064 diabetes insipidus Diseases 0.000 claims 4
- 235000010979 hydroxypropyl methyl cellulose Nutrition 0.000 claims 4
- UFVKGYZPFZQRLF-UHFFFAOYSA-N hydroxypropyl methyl cellulose Chemical group OC1C(O)C(OC)OC(CO)C1OC1C(O)C(O)C(OC2C(C(O)C(OC3C(C(O)C(O)C(CO)O3)O)C(CO)O2)O)C(CO)O1 UFVKGYZPFZQRLF-UHFFFAOYSA-N 0.000 claims 4
- 229920003088 hydroxypropyl methyl cellulose Polymers 0.000 claims 4
- 239000001866 hydroxypropyl methyl cellulose Substances 0.000 claims 4
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- 239000003795 chemical substances by application Substances 0.000 claims 3
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- PURKAOJPTOLRMP-UHFFFAOYSA-N ivacaftor Chemical group C1=C(O)C(C(C)(C)C)=CC(C(C)(C)C)=C1NC(=O)C1=CNC2=CC=CC=C2C1=O PURKAOJPTOLRMP-UHFFFAOYSA-N 0.000 claims 2
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- VEXZGXHMUGYJMC-UHFFFAOYSA-M Chloride anion Chemical compound [Cl-] VEXZGXHMUGYJMC-UHFFFAOYSA-M 0.000 claims 1
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- AIMMVWOEOZMVMS-UHFFFAOYSA-N cyclopropanecarboxamide Chemical compound NC(=O)C1CC1 AIMMVWOEOZMVMS-UHFFFAOYSA-N 0.000 claims 1
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Classifications
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- C07—ORGANIC CHEMISTRY
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- C07D209/00—Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom
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Claims (20)
1. Čvrsta disperzija koja sadrži čvrsti ključni amorfni (R)-1-(2,2-difluorobenzo[d][1,3]dioksol-5-il)-N-(1-(2,3-dihidroksipropil)-6-fluoro-2-(1-hidroksi-2-metilpropan-2-il)-1H-indol-5-il)ciklopropankarboksamid i polimer, pri čemu čvrsti ključni amorfni (R)-1-(2,2-difluorobenzo[d][1,3]dioksol-5-il)-N-(1-(2,3-dihidroksipropil)-6-fluoro-2-(1-hidroksi-2-metilpropan-2-il)-1H-indol-5-il)ciklopropankarboksamid sadrži manje od oko 5% kristalnog (R)-1-(2,2-difluorobenzo[d][1,3]dioksol-5-il)-N-(1-(2,3-dihidroksipropil)-6-fluoro-2-(1-hidroksi-2-metilpropan-2-il)-1H-indol-5-il)ciklopropankarboksamida, pri čemu je polimer hidroksipropilmetilceluloza (HPMC) ili hidroksipropilmetilcelulozni acetat sukcinat (HPMCAS).
2. Čvrsta disperzija prema zahtjevu 1, pri čemu je polimer prisutan u količini od 10% masenih udjela do 80% masenih udjela; ili pri čemu je polimer prisutan u količini od 30% masenih udjela do 60% masenih udjela; ili pri čemu je polimer prisutan u količini od oko 49.5% masenih udjela.
3. Čvrsta disperzija prema zahtjevu 1 ili zahtjevu 2, pri čemu je (R)-1-(2,2-difluorobenzo[d][1,3]dioksol-5-il)-N-(1-(2,3-dihidroksipropil)-6-fluoro-2-(1-hidroksi-2-metilpropan-2-il)-1H-indol-5-il)ciklopropankarboksamid prisutan u količini od 10% masenih udjela do 80% masenih udjela; ili pri čemu je (R)-1-(2,2-difluorobenzo[d][1,3]dioksol-5-il)-N-(1-(2,3-dihidroksipropil)-6-fluoro-2-(1-hidroksi-2-metilpropan-2-il)-1H-indol-5-il)ciklopropankarboksamid prisutan u količini od 30% masenih udjela do 60% masenih udjela; ili pri čemu je (R)-1-(2,2-difluorobenzo[d][1,3]dioksol-5-il)-N-(1-(2,3-dihidroksipropil)-6-fluoro-2-(1-hidroksi-2-metilpropan-2-il)-1H-indol-5-il)ciklopropankarboksamid prisutan u količini od oko 50% masenih udjela.
4. Čvrsta disperzija prema bilo kojem od patentnih zahtjeva 1 do 3, koja dalje sadrži površinski aktivno sredstvo.
5. Čvrsta disperzija prema zahtjevu 4, pri čemu je površinski aktivno sredstvo natrijev lauril sulfat, i pri čemu je površinski aktivno sredstvo prisutno u količini od 0.1% masenih udjela do 5% masenih udjela; ili pri čemu je površinski aktivno sredstvo prisutno u količini od oko 0.5% masenih udjela.
6. Čvrsta disperzija prema zahtjevu 4, pri čemu je polimer hidroksipropilmetilcelulozni acetat sukcinat (HPMCAS) u količini od oko 49.5% masenih udjela, površinski aktivno sredstvo je natrijev lauril sulfat u količini od oko 0.5% masenih udjela, i (R)-1-(2,2-difluorobenzo[d][1,3]dioksol-5-il)-N-(1-(2,3-dihidroksipropil)-6-fluoro-2-(1-hidroksi-2-metilpropan-2-il)-1H-indol-5-il)ciklopropankarboksamid je prisutan u količini od oko 50% masenih udjela.
7. Farmaceutski sastav koji sadrži:
(a) čvrstu disperziju prema bilo kojem od zahtjeva 1 do 6; i
(b) farmaceutski prihvatljiv nosač.
8. Farmaceutski sastav prema zahtjevu 7, dalje sadrži dodatno terapeutsko sredstvo, pri čemu je dodatno terapeutsko sredstvo izabrano između mukolitičkog sredstva, bronhodilatatora, antibiotika, anti-infektivnog sredstva, antiupalnog sredstva, CFTR potencijatora, ili nutricionističkog sredstva.
9. Farmaceutski sastav prema zahtjevu 8, pri čemu je dodatno sredstvo N-(5-hidroksi-2,4-diterc-butil-fenil)-4-okso-1H-hinolin-3-karboksamid.
10. Postupak za dobivanje čvrste disperzije prema zahtjevu 1 koji obuhvaća:
(a) formiranje smjese koja sadrži (R)-1-(2,2-difluorobenzo[d][1,3]dioksol-5-il)-N-(1-(2,3-dihidroksipropil)-6-fluoro-2-(1-hidroksi-2-metilpropan-2-il)-1H-indol-5-il)ciklopropankarboksamid, polimer, i rastvarač; pri čemu je polimer hidroksipropilmetilcelulozni (HPMC) ili hidroksipropilmetilcelulozni acetat sukcinat (HPMCAS); opcionalno, gdje je rastvarač metanol; i
(b) sušenje raspršivanjem smjese da bi se formirala čvrsta disperzija.
11. Postupak prema zahtjevu 10, pri čemu je polimer hidroksipropilmetilcelulozni acetat sukcinat (HPMCAS), i pri čemu je polimer prisutan u količini od 10% masenih udjela do 80% masenih udjela čvrste disperzije; ili pri čemu je polimer prisutan u količini od oko 49.5% masenih udjela čvrste disperzije.
12. Postupak prema bilo kojem od zahtjeva 10 do 11, pri čemu smjesa dalje sadrži površinski aktivno sredstvo, pri čemu je površinski aktivno sredstvo natrijev lauril sulfat (SLS), i pri čemu je površinski aktivno sredstvo prisutno u količini od 0.1% masenih do 5% masenih čvrste disperzija; ili pri čemu je površinski aktivno sredstvo prisutno u količini od oko 0.5% masenih udjela čvrste disperzije.
13. Postupak prema zahtjevu 10, pri čemu je polimer hidroksipropilmetilcelulozni acetat sukcinat (HPMCAS) u količini od oko 49.5% masenih udjela čvrste disperzija, rastvarač je metanol, i smjesa dalje obuhvaća natrijev lauril sulfat u količini od oko 0.5% masenih udjela čvrste disperzije.
14. Čvrsta disperzija prema bilo kojem od zahtjeva 1 do 6, ili farmaceutski sastav prema bilo kojem od zahtjeva 7 do 9, za upotrebu u postupku liječenja bolesti u kojima posreduje CFTR kod subjekta, gdje je bolest koja je posredovana CFTR izabrana između cistične fibroze, astme, dimom izazvane COPD, kroničnog bronhitisa, rinosinuzitisa, konstipacije, pankreatitisa, insuficijencijegušterače, muškog steriliteta izazvanog kogenitalnim obostranim nedostatkom vas deferensa (CBAVD), blage bolesti pluća, idiopastkog pankreatitisa, alergijske bronhopulmonarne asperiloze (ABPA), bolesti jetre, nasljednog emfizema, nasljedne hemokromatoze, nedostatka koagulacije-fibrinolize, nedostataka proteina C , nasljednog angioedema tipa 1, nedostatka obrade lipida, obiteljske hiperkolesterolemija, hilomikronemije tipa 1, abetalipoproteinemije, bolesti nagomilavanja lizozoma, I-stanične bolesti/pseudo-Hurlera, mukopolisaharidoze, Sandhof/Tay-Sachs, Crigler-Najjar tipa II, poliendokrinopatije/hiperinsulemije, šećerne bolesti, Laronovog patuljastog rasta, nedostatka mileoperoksidaze, primarnog hipoparatiroidizama, melanoma, glikanoze CDG tipa 1, kongenitalnog hipertiroidizma, osteogenezis imperfekte, nasljedne hipofibrinogenemije, nedostatka ACT , dijabetes insipidusa (DI), neurofizealnog DI, neprogenog DI, Charcot-Marie Tooth sindroma, Perlizaeus-Merzbacherove bolesti, neurodegenerativne bolesti, Alzheimerove bolesti, Parkinsonove bolesti, amiotrofne lateralne skleroze, progresivne supranuklearne paralize, Pickove bolesti, nekoliko neuroloških poremećaja poliglutamina, Huntingtona, spinocerebelarne ataksije tipa I, spinalne i bulbarne mišićne atrofije, atrofije dentato-rubro-palido-luisiane, miotonične distrofije, spongiformne encefalopatije, nasljedne Creutzfeldt-Jakobove bolesti (uslijed nedostatka obrade proteina priona), Fabryjeve bolesti, Straussler-Scheinker sindroma, COPD, bolesti suhog oka, Sjogrenove bolesti, osteoporoze, osteopenije, Gorhamovog sindroma, kloridne kanalopatije, miotonije kongenita (oblici Thomson i Becker), Barterov sindroma tipa III, Dentove bolesti, hiperekpleksije, epilepsije, hiperekpleksije, bolesti skladištenja lizozoma, Angelmanovog sindroma, primarne cilijarne diskinezije (PCD), nasljedog poremećaja strukture i/ili funkcije cilija, PCD sa situs inversus (takođe poznat kao Kartagenerov sindrom ), PCD sa situs inversus, ili ciliarne aplazije.
15. Čvrsta disperzija, ili farmaceutski sastav za upotrebu kao u zahtjevu 14, pri čemu je CFTR posredovana bolest cistična fibroza.
16. Čvrsta disperzija, ili farmaceutski sastav, za upotrebu prema zahtjevu 14 ili zahtjevu 15, pri čemu subjekt ima transmembranski receptor cistične fibroze (CFTR) sa ΔF508 mutacijom, ili pri čemu subjekt ima transmembranski receptor cistične fibroze (CFTR) sa R117H mutcijom, ili pri čemu subjekt ima transmembranski receptor cistične (CFTR) sa G551D mutacijom.
17. Čvrsta disperzija, ili farmaceutski sastav, za upotrebu kao prema bilo kojem od zahtjeva 14-16, pri čemu postupak obuhvaća davanje dodatnog terapeutskog sredstva, pri čemu je terapeutsko sredstvo izabrano od mukolitičkog sredstva, bronhodilatatora, antibiotika, antiinfektivnog sredstva, antiupalnog sredstva, CFTR potencijatora, ili nutricionističkog sredstva.
18. Čvrsta disperzija, ili farmaceutski sastav za upotrebu prema zahtjevu 17, pri čemu je dodatno terapeutsko sredstvo N-(5-hidroksi-2,4-ditert-butilfenil)-4-okso-1H-hinolin-3-karboksamid.
19. Čvrsta disperzija, ili farmaceutski sastav za upotrebu kao u zahtjevu 17 ili zahtjevu 18, pri čemu je dodatno terapeutsko sredstvo davano istovremeno, prije ili poslije davanja čvrste disperzije prema bilo kojem od zahtjeva 1 do 6, ili farmaceutski sastav prema bilo kojem od zahtjeva 7 do 9.
20. Komplet koji sadrži čvrstu disperziju prema bilo kojem od zahtjeva 1 do 6, ili farmaceutski sastav prema bilo kojem od zahtjeva 7-9, i njegova uputstva za upotrebu.
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EP14172991.3A EP2826776B1 (en) | 2010-03-25 | 2011-03-25 | Solid dispersion of amorphous form of (r)-1(2,2-difluorobenzo(d)(1,3)dioxol-5-yl)-n-(1-(2,3-dihydroxypropyl)-6-fluoro-2-(1-hydroxy-2-methylpropan-2-yl)-1h-indol-5-yl)-cyclopropanecarboxamide |
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HRP20210165TT HRP20210165T1 (hr) | 2010-03-25 | 2021-02-01 | Čvrsta disperzija amorfnog oblika (r)-1(2,2-difluorobenzo(d)(1,3)dioksol-5-il)-n-(1-(2,3-dihidroksipropil)-6-fluoro-2-(1-hidroksi-2-metilpropan-2-il)-1h-indol-5-il)-ciklopropankarboksamida |
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