HRP20200664T1 - Čvrsti oblici 3-(6-(1-(2,2-difluorobenzo[d][1,3]dioksol-5-il) ciklopropankarboksamido)-3-metilpiridin-2-il) benzojeve kiseline - Google Patents

Čvrsti oblici 3-(6-(1-(2,2-difluorobenzo[d][1,3]dioksol-5-il) ciklopropankarboksamido)-3-metilpiridin-2-il) benzojeve kiseline Download PDF

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HRP20200664T1
HRP20200664T1 HRP20200664TT HRP20200664T HRP20200664T1 HR P20200664 T1 HRP20200664 T1 HR P20200664T1 HR P20200664T T HRP20200664T T HR P20200664TT HR P20200664 T HRP20200664 T HR P20200664T HR P20200664 T1 HRP20200664 T1 HR P20200664T1
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Ali Keshavarz-Shokri
Beili Zhang
Mariusz Krawiec
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Vertex Pharmaceuticals Incorporated
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Claims (27)

1. Farmaceutski sastav koji sadrži: 3-(6-(1-(2,2-difluorobenzo[d][1,3]dioksol-5-il)ciklopropankarboksamido)-3-metilpiridin-2-il)benzojevu kiselinu karakteriziranu kao oblik I; farmaceutski prihvatljiv nosač; i dodatno terapeutsko sredstvo izabrano između mukolitičnog sredstva, bronhodilatora, antibiotika, anti-infektivnog sredstva, anti-upalnog sredstva, modulatora regulatora transmembranske provodljivosti u cističnoj fibrozi (CFTR), ili nutritivnog sredstva, gdje je oblik I karakteriziran kao kristalni oblik koji ima monoklinični kristalni sistem, prostornu grupu P21/n, i sljedeće dimenzije jedinične stanice: a = 4.9626 (7) Å α = 90° b = 12.2994 (18) Å β = 93.938 (9)° c = 33.075 (4) Å γ = 90°, i/ili gdje je oblik I karakteriziran s jednim ili više vrhova na 15.4 stupnjeva ± 0.2 stupnja, 16.3 stupnjeva ± 0.2 stupnja, i 14.5 stupnjeva ± 0.2 stupnja u difrakciji redgneskih zraka na prahu dobivenih pomoću Cu K alfa zračenja na 40 kV, 35 mA.
2. Farmaceutski sastav prema zahtjevu 1, gdje je dodatno terapeutsko sredstvo CFTR modulator.
3. Farmaceutski sastav prema zahtjevu 1 ili zahtjevu 2, gdje je CFTR modulator N-(5-hidroksi-2,4-diterc-butil-fenil)-4-okso-1H-kinolin-3-karboksamid.
4. Farmaceutski sastav prema bilo kojem od zahtjeva 1 do 3, za upotrebu u postupku liječenja cistične fibroze.
5. Upotreba farmaceutskog sastava prema bilo kojem od zahtjeva 1 do 3, u proizvodnji lijeka za liječenje cistične fibroze.
6. 3-(6-(1-(2,2-difluorobenzo[d][1,3]dioksol-5-il)ciklopropankarboksamido)-3-metilpiridin-2-il)benzojeva kiselina karakterizirana kao oblik I, za upotrebu u postupku liječenja cistične fibroze kod sisavca, gdje postupak obuhvaća davanje sisavcu efikasne količine oblika I; i gdje postupak obuhvaća davanje dodatnog terapeutskog sredstva; gdje je oblik I kao što je definirano u zahtjevu 1.
7. 3-(6-(1-(2,2-Difluorobenzo[d][1,3]dioksol-5-il)ciklopropankarboksamido)-3-metilpiridin-2-il)benzojeva kiselina karakterizirana kao oblik I za upotrebu prema zahtjevu 6, gdje je dodatno terapeutsko sredstvo N-(5-hidroksi-2,4-diterc-butilfenil)-4-okso-1H-kinolin-3-karboksamid.
8. 3-(6-(1-(2,2-Difluorobenzo[d][1,3]dioksol-5-il)ciklopropankarboksamido)-3-metilpiridin-2-il)benzojeva kiselina karakterizirana kao oblik I za upotrebu prema zahtjevu 6 ili zahtjevu 7, gdje je oblik I davan zajedno sa, prije ili poslije dodatnog terapeutskog sredstva.
9. N-(5-hidroksi-2,4-diterc-butil-fenil)-4-okso-1H-kinolin-3-karboksamid za upotrebu u postupku liječenja cistične fibroze kod sisavca, gdje postupak obuhvaća davanje sisavcu efikasne količine N-(5-hidroksi-2,4-diterc-butilfenil)-4-okso-1H-kinolin-3-karboksamida; i gdje postupak obuhvaća davanje dodatnog terapeutskog sredstva koje je 3-(6-(1-(2,2-difluorobenzo[d][1,3]dioksol-5-il) ciklopropankarboksamido)-3-metilpiridin-2-il)benzojeva kiselina karakterizirana kao oblik I; gdje je oblik I kao što je definirano u zahtjevu 1.
10. N-(5-hidroksi-2,4-diterc-butil-fenil)-4-okso-1H-kinolin-3-karboksamid za upotrebu kao u zahtjevu 9, gdje je N-(5-hidroksi-2,4-diterc-butil-fenil)-4-okso-1H-kinolin-3-karboksamid davan zajedno, prije ili poslije 3-(6-(1-(2,2-Difluorobenzo[d][1,3]dioksol-5-il)ciklopropankarboksamido)-3-metilpiridin-2-il)benzojeve kiseline karakterizirane kao oblik I.
11. Upotreba 3-(6-(1-(2,2-difluorobenzo[d][1,3]dioksol-5-il)ciklopropankarboksamido)-3-metilpiridin-2-il)benzojeve kiseline karakterizirane kao oblik I u proizvodnji lijeka za liječenje cistične fibroze kod sisavca, gdje je lijek pripremljen za davanje sisavcu u efikasnoj količini; i gdje je lijek pripremljen za davanje s dodatnim terapeutskim sredstvom; gdje je oblik I kao što je definirano u zahtjevu 1.
12. Upotreba prema zahtjevu 11, gdje je dodatno terapeutsko sredstvo N-(5-hidroksi-2,4-diterc-butil-fenil)-4-okso-1H-kinolin-3-karboksamid.
13. Upotreba prema zahtjevu 11 ili zahtjevu 12, gdje je lijek pripremljen za davanje zajedno sa, prije ili poslije dodatnog terapeutskog sredstva.
14. Upotreba N-(5-hidroksi-2,4-diterc-butil-fenil)-4-okso-1H-kinolin-3-karboksamida u proizvodnji lijeka za liječenje cistične fibroze kod sisavaca, gdje je lijek pripremljen za davanje u efikasnoj količini ; i gdje je lijek pripremljen za davanje sa dodatnim terapeutskim sredstvom koje je 3-(6-(1-(2,2-difluorobenzo[d][1,3]dioksol-5-il)ciklopropankarboksamido)-3-metilpiridin-2-il)benzojeva kiselina karakterizirana kao oblik I; gdje je oblik I kao što je definirano u zahtjevu 1 .
15. Upotreba prema zahtjevu 14, gdje je lijek pripremljen za davanje zajedno, prije ili poslije dodatnog terapeutskog sredstva.
16. Farmaceutski sastav prema zahtjevu 1, gdje je oblik I karakteriziran kao kristalni oblik koji ima monoklinični kristalni sistem, prostornu grupu P21/n, i sljedeće dimenzije jedinične stanice: a = 4.9626 (7) Å α = 90° b = 12.2994 (18) Å β = 93.938 (9)° c = 33.075 (4) Å γ = 90°.
17. Farmaceutski sastav prema zahtjevu 1, gdje je oblik I karakteriziran sa jednim ili više vrhova na 15.4 stupnjeva ± 0.2 stupnja, 16.3 stupnjeva ± 0.2 stupnja, i 14.5 stupnjeva ± 0.2 stupnja u difrakciji redgneskih zraka na prahu dobivenih pomoću Cu K alfa zračenja na 40 kV, 35 mA.
18. Farmaceutski sastav prema zahtjevu 1, gdje je oblik I karakteriziran kao kristalni oblik koji ima monoklinični kristalni sistem, prostornu grupu P21/n, i sljedeće dimenzije jedinične stanice: a = 4.9626 (7) Å α = 90° b = 12.2994 (18) Å β = 93.938 (9)° c = 33.075 (4) Å γ = 90°, i gdje je oblik I karakteriziran sa jednim ili više vrhova na 15.4 stupnjeva ± 0.2 stupnja, 16.3 stupnjeva ± 0.2 stupnja, i 14.5 stupnjeva ± 0.2 stupnja u difrakciji redgneskih zraka na prahu dobivenih pomoću Cu K alfa zračenja na 40 kV, 35 mA.
19. Farmaceutski sastav prema bilo kojem od zahtjeva 1, 17, ili 18, gdje je oblik 1 karakteriziran vrhovima na 15.4 stupnjeva ± 0.2 stupnja, 16.3 stupnjeva ± 0.2 stupnja, i 14.5 stupnjeva ± 0.2 stupnja.
20. Farmaceutski sastav prema prema bilo kojem od zahtjeva 1, ili 17-19, gdje je oblik 1 dalje karakteriziran vrhom na 14.8 stupnjeva ± 0.2 stupnja.
21. Farmaceutski sastav prema bilo kojem od zahtjeva 1, ili 17-20, gdje je oblik 1 dalje karakteriziran vrhom na 17.8 stupnjeva ± 0.2 stupnja.
22. Farmaceutski sastav prema bilo kojem od zahtjeva 1, ili 17-21, gdje je oblik 1 dalje karakteriziran vrhom na 16.6 stupnjeva ± 0.2 stupnja.
23. Farmaceutski sastav prema bilo kojem od zahtjeva 1, ili 17-22, gdje je oblik 1 dalje karakteriziran vrhom na 7.8 stupnjeva ± 0.2 stupnja.
24. Farmaceutski sastav prema bilo kojem od zahtjeva 1, ili 17-23, gdje je oblik 1 dalje karakteriziran vrhom na 26.0 stupnjeva ± 0.2 stupnja.
25. Farmaceutski sastav prema bilo kojem od zahtjeva 1, ili 17-24, gdje je oblik 1 dalje karakteriziran vrhom na 21.6 stupnjeva ± 0.2 stupnja.
26. Farmaceutski sastav prema bilo kojem od zahtjeva 1, ili 17-25, gdje je oblik 1 dalje karakteriziran vrhom na 23.3 stupnjeva ± 0.2 stupnja.
27. Farmaceutski sastav prema bilo kojem od zahtjeva 1, ili 17-19, gdje je oblik 1 dalje karakteriziran vrhom na 14.8 stupnjeva ± 0.2 stupnja, 17.8 stupnjeva ± 0.2 stupnja, 16.6 stupnjeva ± 0.2 stupnja, 7.8 stupnjeva ± 0.2 stupnja, 26.0 stupnjeva ± 0.2 stupnja, 21.6 stupnjeva ± 0.2 stupnja, i 23.3 stupnjeva ± 0.2 stupnja.
HRP20200664TT 2007-12-07 2020-04-24 Čvrsti oblici 3-(6-(1-(2,2-difluorobenzo[d][1,3]dioksol-5-il) ciklopropankarboksamido)-3-metilpiridin-2-il) benzojeve kiseline HRP20200664T1 (hr)

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US1216207P 2007-12-07 2007-12-07
EP16198922.3A EP3170818B1 (en) 2007-12-07 2008-12-04 Solid forms of 3-(6-(1-(2,2-difluorobenzo[d][1,3]dioxol-5-yl) cyclopropanecarboxamido)-3-methylpyridin-2-yl) benzoic acid

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HRP20170241TT HRP20170241T2 (hr) 2007-12-07 2017-02-14 Čvrsti oblici 3-(6-(1-(2,2-difluorobenzo[d][1,3]dioksol-5-il)ciklopropankarboksamido)-3-metilpiridin-2-il)benzojeve kiseline
HRP20200664TT HRP20200664T1 (hr) 2007-12-07 2020-04-24 Čvrsti oblici 3-(6-(1-(2,2-difluorobenzo[d][1,3]dioksol-5-il) ciklopropankarboksamido)-3-metilpiridin-2-il) benzojeve kiseline

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US (8) US8507534B2 (hr)
EP (3) EP3170818B1 (hr)
JP (6) JP2011506330A (hr)
KR (3) KR20100101130A (hr)
CN (2) CN101910156B (hr)
AU (1) AU2008333845C1 (hr)
BR (1) BRPI0821039B8 (hr)
CA (2) CA2986286C (hr)
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