DK2409975T3 - Faste dispersioner omfattende et amorf legeme bestående af en heterocyklisk anti-tumor-forbindelse - Google Patents

Faste dispersioner omfattende et amorf legeme bestående af en heterocyklisk anti-tumor-forbindelse Download PDF

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DK2409975T3
DK2409975T3 DK11168461.9T DK11168461T DK2409975T3 DK 2409975 T3 DK2409975 T3 DK 2409975T3 DK 11168461 T DK11168461 T DK 11168461T DK 2409975 T3 DK2409975 T3 DK 2409975T3
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alkyl
optionally substituted
solid dispersion
solid
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Tadaaki Sugama
Nobuhiro Ishihara
Yoshiharu Tanaka
Masayuki Takahashi
Shinichi Yaguchi
Tetsuo Watanabe
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Zenyaku Kogyo Kk
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Claims (8)

1. Fast dispersion omfattende: et amorf legeme bestående af en heterocyklisk forbindelse, som repræsenteres med den generelle formel (I): [Chem. 1]
- (I) hvor X står for et nitrogenatom eller CH; Ri og R2, begge eller hver især, står for et hydrogenatom, en hydroxylgrup-pe, et halogen, en aminogruppe, en Ci-C6 alkylaminogruppe, en Ci-C6 al-koxygruppe, en CrC6 alkylgruppe eller en cyanogruppe; R3 står for et hydrogenatom, en difluoromethylgruppe, en aminogruppe, en CrC6 alkylaminogruppe, en methyl- eller en hydroxymethylgruppe; R4 og R5 står for et hydrogenatom eller en C1-C6 alkylgruppe; og R6 står for en morpholino (eventuelt substitueret med 1 til 2 C1-C6 alkylgrup-per), en pyrrolidinyl (eventuelt substitueret med en hydroxy C1-C6 alkylgruppe), en piperidino (eventuelt substitueret med 1 til 2 oxygenatomer, en hy-droxylgruppe, en formyl-, eller en CrC6 alkylgruppe), en piperazinyl (eventuelt substitueret med 1 til 2 oxygenatomer, hvor nitrogen ved position 4 eventuelt substitueres med en substituent udvalgt fra gruppen bestående af formyl, hydroxyl C-i-Ce alkyl, CrC6 alkoxycarbonyl, oxo CrC6 alkyl, aromatisk carbonyl, benzylcarbonyl og substitueret carbamoyl), eller en 1,4-diazepano (eventuelt substitueret med 1 til 2 oxygenatomer, hvor nitrogen ved position 4 eventuelt substitueres med en substituent udvalgt fra gruppen bestående af formyl, hydroxy CrCe alkyl, CrC6 alkoxycarbonyl, oxo CrC6 alkyl, aromatisk carbonyl, benzylcarbonyl og substituteret carbamoyl); eller et hydrat deraf, et solvat deraf eller et farmaceutisk acceptabelt salt deraf; og en fast polymer udvalgt blandt hydroxypropylcellulose og hypromellose, hvor masseforholdet af den heterocykliske forbindelse, hydratet deraf; solvatet deraf eller det farmaceutisk acceptable salt deraf og den faste polymer er 1:1 til 1:5.
2. Fast dispersion ifølge krav 1, hvor det amorfe legeme fremstilles med en sprøjtetørringsfremgangsmåde, en blandet slibningsfremgangsmåde, en fusionsfremgangsmåde eller en opløsningsfremgangsmåde.
3. Fast dispersion ifølge krav 1, hvor masseforholdet er 1:2 til 2:5.
4. Fast dispersion ifølge et af kravene 1 til 3, yderligere omfattende et hjælpestof, et sprængningsmiddel eller et smøremiddel.
5. Formulering omfattende den faste dispersion ifølge et af kravene 1 til 4, tilvejebragt i form af et pulver, et fint granulat, et granulat, en tablet eller en kapsel.
6. Fremgangsmåde til fremstilling af en fast dispersion ifølge krav 1, omfattende de følgende trin: i) opløse hydroxypropylcellulose eller hypromellose og en heterocyklisk forbindelse repræsenteret med den generelle formel (I): [Chem.2]
- (I) hvor X står for et nitrogenatom eller CH; Ri og R2, begge eller hver især, står for et hydrogenatom, en hydroxylgrup-pe, et halogen, en aminogruppe, en C1-C6 alkylaminogruppe, en CrC6 al-koxygruppe, en CrC6 alkylgruppe eller en cyanogruppe; R3 står for et hydrogenatom, en difluoromethylgruppe, en aminogruppe, en CrC6 alkylaminogruppe, en methyl- eller en hydroxymethylgruppe; R4 og R5 står for et hydrogenatom eller en CrC6 alkylgruppe; og R6 står for en morpholino (eventuelt substitueret med 1 til 2 CrC6 alkylgrup-per), en pyrrolidinyl (eventuelt substitueret med en hydroxy Ci-C6 alkylgruppe), en piperidino (eventuelt substitueret med 1 til 2 oxygenatomer, en hy-droxylgruppe, en formyl-, eller en CrC6 alkylgruppe), en piperazinyl (eventu elt substitueret med 1 til 2 oxygenatomer, hvor nitrogen ved position 4 eventuelt substitueres med en substituent udvalgt fra gruppen bestående af formyl, hydroxyl C-i-C6 alkyl, CrC6 alkoxycarbonyl, oxo CrC6 alkyl, aromatisk carbonyl, benzylcarbonyl og substitueret carbamoyl), eller en 1,4-diazepano (eventuelt substitueret med 1 til 2 oxygenatomer, hvor nitrogen ved position 4 eventuelt substitueres med en substituent udvalgt fra gruppen bestående af formyl, hydroxy CrC6 alkyl, CrC6 alkoxycarbonyl, oxo CrC6 alkyl, aromatisk carbonyl, benzylcarbonyl og substituteret carbamoyl); eller et hydrat deraf, et solvat deraf eller et farmaceutisk acceptabelt salt deraf; i et opløsningsmiddel til fremstilling af en forsyningsopløsning; ii) forstøvning af forsyningsopløsningen; og iii) tørring af den forstøvede forsyningsopløsning for at opnå den faste dispersion.
7. Fast dispersion ifølge et af kravene 1 til 4 til anvendelse i behandlingen af faste tumorer, sarkomer, carcinomer, hematologiske neoplasmer, autoimmune sygdomme, funktionsforstyrrelser i organ i forbindelse med autoimmune sygdomme, afvisningsreaktion, graft versus host sygdom, inflammatoriske tarmsygdomme, inflammatoriske eller allergiske hudsygdomme, inflammatoriske eller allergiske luftvejssygdomme, allergisk conjunctivitis og rhinitis, og sygdomme fremkaldt ved infektion af gramnegative bakterier eller coronavi-rus.
8. Formulering ifølge krav 5 til anvendelse i behandlingen af faste tumorer, sarkomer, carcinomer, hematologiske neoplasmer, autoimmune sygdomme, funktionsforstyrrelser i organ i forbindelse med autoimmune sygdomme, afvisningsreaktion, graft versus host sygdom, inflammatoriske tarmsygdomme, inflammatoriske eller allergiske hudsygdomme, inflammatoriske eller allergiske luftvejssygdomme, allergisk conjunctivitis og rhinitis, og sygdomme fremkaldt ved infektion af gramnegative bakterier eller coronavirus.
DK11168461.9T 2007-11-22 2008-11-21 Faste dispersioner omfattende et amorf legeme bestående af en heterocyklisk anti-tumor-forbindelse DK2409975T3 (da)

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JP2007303332 2007-11-22
EP08852868A EP2218718A1 (en) 2007-11-22 2008-11-21 Amorphous form of heterocyclic compound, solid dispersion and medicinal preparation each comprising the same, and process for production of the same

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JP7280111B2 (ja) 2019-05-28 2023-05-23 ファナック株式会社 モータ制御装置

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KR101576695B1 (ko) 2015-12-10
JP5479912B2 (ja) 2014-04-23
CN101883765B (zh) 2014-10-01
CA2706536A1 (en) 2009-05-28
US8227463B2 (en) 2012-07-24
EP2218718A1 (en) 2010-08-18
US20100249063A1 (en) 2010-09-30
TWI482768B (zh) 2015-05-01
KR20100108533A (ko) 2010-10-07
JPWO2009066775A1 (ja) 2011-04-07

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