HRP20220463T1 - Farmaceutska kombinacija koja sadrži blokator kalcijevih kanala t-tipa - Google Patents

Farmaceutska kombinacija koja sadrži blokator kalcijevih kanala t-tipa Download PDF

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HRP20220463T1
HRP20220463T1 HRP20220463TT HRP20220463T HRP20220463T1 HR P20220463 T1 HRP20220463 T1 HR P20220463T1 HR P20220463T T HRP20220463T T HR P20220463TT HR P20220463 T HRP20220463 T HR P20220463T HR P20220463 T1 HRP20220463 T1 HR P20220463T1
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phenyl
dione
carboxamide
ethyl
acid
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Melanie KESSLER
Catherine Roch
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Idorsia Pharmaceuticals Ltd
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    • A61K31/197Carboxylic acids, e.g. valproic acid having an amino group the amino and the carboxyl groups being attached to the same acyclic carbon chain, e.g. gamma-aminobutyric acid [GABA], beta-alanine, epsilon-aminocaproic acid or pantothenic acid
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    • A61K31/4015Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil having oxo groups directly attached to the heterocyclic ring, e.g. piracetam, ethosuximide
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    • A61K31/4427Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
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    • A61K31/551Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole having two nitrogen atoms, e.g. dilazep
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    • A61K31/551Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole having two nitrogen atoms, e.g. dilazep
    • A61K31/55131,4-Benzodiazepines, e.g. diazepam or clozapine
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Claims (18)

1. Farmaceutska kombinacija, naznačena time, da sadrži prvi aktivni sastojak koji je N-[1-(5-cijano-piridin-2ilmetil)-1H-pirazol-3-il]-2-[4-(1-trifluorometil-ciklopropil)-fenil]-acetamid ili njegova farmaceutski prihvatljiva sol i drugi aktivni sastojak koji ima antiepileptički učinak, ili njegovu farmaceutski prihvatljivu sol.
2. Farmaceutska kombinacija prema patentnom zahtjevu 1, naznačena time, da se drugi aktivni sastojak bira iz skupine koju čine 5H-dibenzo[b,f]azepin-5-karboksamid, (RS)-3-etil-3-metil-pirolidin-2,5-dion, 6-(2,3-diklorofenil)-1,2,4-triazin-3,5-diamin, (S)-2-(2-oksopirolidin-1-il)butanamid, 10,11-dihidro-10-okso-5H-dibenz[b,f]azepin-5-karboksamid, 2-propilpentanska kiselina, N-(5-sulfamoil-1,3,4-tiadiazol-2-il)acetamid, (2S)-2-[(4R)-2-okso-4-propilpirolidin-1-il]butanamid, 7-kloro-1-metil-5-fenil-1,5-benzodiazepin-2,4-dion, 5-(2-klorofenil)-7-nitro-1,3-dihidro-1,4-benzodiazepin-2-on, (S)-10-acetoksi-10,11-dihidro-5H-dibenz[b,f]azepin-5-karboksamid, (3-karbamoiloksi-2-fenilpropil)karbamat, 1-(aminometil)cikloheksanoctena kiselina, (R)-2-acetamido-N-benzil-3-metoksipropanamid, 5’-(2-cijanofenil)-1’-fenil-2,3’-bipiridinil-6’(1’H)-on, 5-etil-5-fenil-1,3-diazinan-2,4,6-trion, 5,5-difenilimidazolidin-2,4-dion, 2-(2-oksopirolidin-1-il)acetamid, (3S)-3-(aminometil)-5-metilheksanska kiselina, 5-etil-5-fenil-1,3-diazinan-4,6-dion, etil (2-amino-4-((4-fluorobenzil)amino)fenil)karbamat, 1-(2,6-difluorobenzil)-1H-1,2,3-triazol-4-karboksamid, (RS)-(E)-4,4-dimetil-1-[3,4(metilendioksi)-fenil]-1-penten-3-ol, (3R)-1-[4,4-bis(3-metil-2-tienil)-3-buten-1-il]-3-piperidinkarboksilna kiselina, 2,3:4,5-bis-O-(1-metiletiliden)-β-D-fruktopiranoza sulfamat, (RS)-4-aminoheks-5-enska kiselina, i benzo[d]izoksazol-3-ilmetansulfonamid; ili farmaceutski prihvatljiva sol od bilo kojega od prethodno navedenih.
3. Farmaceutska kombinacija prema patentnom zahtjevu 1, naznačena time, da se drugi aktivni sastojak bira iz skupine koju čine 5H-dibenzo[b,f]azepin-5-karboksamid, (RS)-3-etil-3-metil-pirolidin-2,5-dion, 6-(2,3-diklorofenil)-1,2,4-triazin-3,5-diamin, (S)-2-(2-oksopirolidin-1-il)butanamid, 10,11-dihidro-10-okso-5H-dibenz[b,f]azepin-5-karboksamid, i 2-propilpentanska kiselina; ili farmaceutski prihvatljiva sol od bilo kojega od prethodno navedenih.
4. Farmaceutska kombinacija prema patentnom zahtjevu 1, naznačena time, da se drugi aktivni sastojak bira iz skupine koju čine (RS)-3-etil-3-metil-pirolidin-2,5-dion, 6-(2,3-diklorofenil)-1,2,4-triazin-3,5-diamin, (S)-2-(2-oksopirolidin-1-il)butanamid, 2-propilpentanska kiselina, i 5-(2-klorofenil)-7-nitro-1,3-dihidro-1,4-benzodiazepin-2-on; ili farmaceutski prihvatljiva sol od bilo kojega od prethodno navedenih.
5. Farmaceutska kombinacija prema patentnom zahtjevu 1, naznačena time, da se drugi aktivni sastojak bira iz skupine koju čine (S)-2-(2-oksopirolidin-1-il)butanamid, i 2-propilpentanska kiselina; ili farmaceutski prihvatljiva sol od bilo kojega od prethodno navedenih.
6. Farmaceutska kombinacija prema patentnom zahtjevu 1, naznačena time, da drugi aktivni sastojak je (S)-2-(2-oksopirolidin-1-il)butanamid ili njegova farmaceutski prihvatljiva sol.
7. Farmaceutska kombinacija prema patentnom zahtjevu 1, naznačena time, da drugi aktivni sastojak je 2-propilpentanska kiselina ili njezina farmaceutski prihvatljiva sol.
8. Farmaceutska kombinacija prema patentnom zahtjevu 1, naznačena time, da drugi aktivni sastojak je (2S)-2-[(4R)-2-okso-4-propilpirolidin-1-il]butanamid ili njegova farmaceutski prihvatljiva sol.
9. Farmaceutska kombinacija prema bilo kojem od patentnih zahtjeva 1 do 8, naznačena time, da su prvi i drugi aktivni sastojak sadržani u jedinstvenom farmaceutskom pripravku.
10. Farmaceutska kombinacija prema bilo kojem od patentnih zahtjeva 1 do 8, naznačena time, da su prvi i drugi aktivni sastojak sadržani u odvojenim farmaceutskim pripravcima.
11. Farmaceutska kombinacija prema bilo kojem od patentnih zahtjeva 1 do 10, naznačena time, da je za uporabu kao lijek.
12. Farmaceutska kombinacija prema bilo kojem od patentnih zahtjeva 1 do 10, naznačena time, da je za uporabu u prevenciji i/ili liječenju epilepsije.
13. Farmaceutska kombinacija prema bilo kojem od patentnih zahtjeva 1 do 10, naznačena time, da je za uporabu u prevenciji i/ili liječenju toničko-kloničkih konvulzija i/ili malih napadaja konvulzija (apsensa).
14. Farmaceutski pripravak, naznačen time, da kao aktivni sastojak, sadrži N-[1-(5-cijano-piridin-2ilmetil)-1H-pirazol-3-il]-2-[4-(1-trifluorometil-ciklopropil)-fenil]-acetamid, ili njegovu farmaceutski prihvatljivu sol, i najmanje jedno terapijski inertno pomoćno sredstvo, za uporabu kao lijek, pri čemu se farmaceutski pripravak treba davati u kombinaciji s drugim farmaceutskim pripravkom koji kao aktivni sastojak, sadrži 5H-dibenzo[b,f]azepin-5-karboksamid, (RS)-3-etil-3-metil-pirolidin-2,5-dion, 6-(2,3-diklorofenil)-1,2,4-triazin-3,5-diamin, (S)-2-(2-oksopirolidin-1-il)butanamid, 10,11-dihidro-10-okso-5H-dibenz[b,f]azepin-5-karboksamid, 2-propilpentanska kiselina, N-(5-sulfamoil-1,3,4-tiadiazol-2-il)acetamid, (2S)-2-[(4R)-2-okso-4-propilpirolidin-1-il]butanamid, 7-kloro-1-metil-5-fenil-1,5-benzodiazepin-2,4-dion, 5-(2-klorofenil)-7-nitro-1,3-dihidro-1,4-benzodiazepin-2-on, (S)-10-acetoksi-10,11-dihidro-5H-dibenz[b,f]azepin-5-karboksamid, (3-karbamoiloksi-2-fenilpropil)karbamat, 1-(aminometil)cikloheksanoctena kiselina, (R)-2-acetamido-N-benzil-3-metoksipropanamid, 5’-(2-cijanofenil)-1’-fenil-2,3’-bipiridinil-6’(1’H)-on, 5-etil-5-fenil-1,3-diazinan-2,4,6-trion, 5,5-difenilimidazolidin-2,4-dion, 2-(2-oksopirolidin-1-il)acetamid, (3S)-3-(aminometil)-5-metilheksanska kiselina, 5-etil-5-fenil-1,3-diazinan-4,6-dion, etil (2-amino-4-((4-fluorobenzil)amino)fenil)karbamat, 1-(2,6-difluorobenzil)-1H-1,2,3-triazol-4-karboksamid, (RS)-(E)-4,4-dimetil-1-[3,4(metilendioksi)-fenil]-1-penten-3-ol, (3R)-1-[4,4-bis(3-metil-2-tienil)-3-buten-1-il]-3-piperidinkarboksilna kiselina, 2,3:4,5-bis-O-(1-metiletiliden)-β-D-fruktopiranoza sulfamat, (RS)-4-aminoheks-5-enska kiselina, ili benzo[d]izoksazol-3-ilmetansulfonamid; ili njihovu farmaceutski prihvatljivu sol, i najmanje jedno terapijski inertno pomoćno sredstvo.
15. Farmaceutski pripravak, naznačen time, da kao aktivni sastojak, sadrži 5H-dibenzo[b,f]azepin-5-karboksamid, (RS)-3-etil-3-metil-pirolidin-2,5-dion, 6-(2,3-diklorofenil)-1,2,4-triazin-3,5-diamin, (S)-2-(2-oksopirolidin-1-il)butanamid, 10,11-dihidro-10-okso-5H-dibenz[b,f]azepin-5-karboksamid, 2-propilpentanska kiselina, N-(5-sulfamoil-1,3,4-tiadiazol-2-il)acetamid, (2S)-2-[(4R)-2-okso-4-propilpirolidin-1-il]butanamid, 7-kloro-1-metil-5-fenil-1,5-benzodiazepin-2,4-dion, 5-(2-klorofenil)-7-nitro-1,3-dihidro-1,4-benzodiazepin-2-on, (S)-10-acetoksi-10,11-dihidro-5H-dibenz[b,f]azepin-5-karboksamid, (3-karbamoiloksi-2-fenilpropil)karbamat, 1-(aminometil)cikloheksanoctena kiselina, (R)-2-acetamido-N-benzil-3-metoksipropanamid, 5’-(2-cijanofenil)-1’-fenil-2,3’-bipiridinil-6’(1’H)-on, 5-etil-5-fenil-1,3-diazinan-2,4,6-trion, 5,5-difenilimidazolidin-2,4-dion, 2-(2-oksopirolidin-1-il)acetamid, (3S)-3-(aminometil)-5-metilheksanska kiselina, 5-etil-5-fenil-1,3-diazinan-4,6-dion, etil (2-amino-4-((4-fluorobenzil)amino)fenil)karbamat, 1-(2,6-difluorobenzil)-1H-1,2,3-triazol-4-karboksamid, (RS)-(E)-4,4-dimetil-1-[3,4(metilendioksi)-fenil]-1-penten-3-ol, (3R)-1-[4,4-bis(3-metil-2-tienil)-3-buten-1-il]-3-piperidinkarboksilna kiselina, 2,3:4,5bis-O-(1-metiletiliden)-β-D-fruktopiranoza sulfamat, (RS)-4-aminoheks-5-enska kiselina, ili benzo[d]izoksazol-3-ilmetansulfonamid; ili njihovu farmaceutski prihvatljivu sol, i najmanje jedno terapijski inertno pomoćno sredstvo, za uporabu kao lijek, pri čemu se farmaceutski pripravak treba davati u kombinaciji s drugim farmaceutskim pripravkom koji kao aktivni sastojak, sadrži N-[1-(5-cijano-piridin-2ilmetil)-1H-pirazol-3-il]-2-[4-(1-trifluorometil-ciklopropil)-fenil]-acetamid, ili njegovu farmaceutski prihvatljivu sol, i najmanje jedno terapijski inertno pomoćno sredstvo.
16. Komplet od dijelova, naznačen time, da sadrži prvi farmaceutski pripravak koji kao aktivni sastojak, sadrži N-[1-(5-cijano-piridin-2ilmetil)-1H-pirazol-3-il]-2-[4-(1-trifluorometil-ciklopropil)-fenil]-acetamid, ili njegovu farmaceutski prihvatljivu sol, i najmanje jedno terapijski inertno pomoćno sredstvo; i drugi farmaceutski pripravak koji kao aktivni sastojak, sadrži 5H-dibenzo[b,f]azepin-5-karboksamid, (RS)-3-etil-3-metil-pirolidin-2,5-dion, 6-(2,3-diklorofenil)-1,2,4-triazin-3,5-diamin, (S)-2-(2-oksopirolidin-1-il)butanamid, 10,11-dihidro-10-okso-5H-dibenz[b,f]azepin-5-karboksamid, 2-propilpentanska kiselina, N-(5-sulfamoil-1,3,4-tiadiazol-2-il)acetamid, (2S)-2-[(4R)-2-okso-4-propilpirolidin-1-il]butanamid, 7-kloro-1-metil-5-fenil-1,5-benzodiazepin-2,4-dion, 5-(2-klorofenil)-7-nitro-1,3-dihidro-1,4-benzodiazepin-2-on, (S)-10-acetoksi-10,11-dihidro-5H-dibenz[b,f]azepin-5-karboksamid, (3-karbamoiloksi-2-fenilpropil)karbamat, 1-(aminometil)cikloheksanoctena kiselina, (R)-2-acetamido-N-benzil-3-metoksipropanamid, 5’-(2-cijanofenil)-1’-fenil-2,3’-bipiridinil-6’(1’H)-on, 5-etil-5-fenil-1,3-diazinan-2,4,6-trion, 5,5-difenilimidazolidin-2,4-dion, 2-(2-oksopirolidin-1-il)acetamid, (3S)-3-(aminometil)-5-metilheksanska kiselina, 5-etil-5-fenil-1,3-diazinan-4,6-dion, etil (2-amino-4-((4-fluorobenzil)amino)fenil)karbamat, 1-(2,6-difluorobenzil)-1H-1,2,3-triazol-4-karboksamid, (RS)-(E)-4,4-dimetil-1-[3,4(metilendioksi)-fenil]-1-penten-3-ol, (3R)-1-[4,4-bis(3-metil-2-tienil)-3-buten-1-il]-3-piperidinkarboksilna kiselina, 2,3:4,5-bis-O-(1-metiletiliden)-β-D-fruktopiranoza sulfamat, (RS)-4-aminoheks-5-enska kiselina, ili benzo[d]izoksazol-3-ilmetansulfonamid; ili njihovu farmaceutski prihvatljivu sol, i najmanje jedno terapijski inertno pomoćno sredstvo.
17. Farmaceutski pripravak koji kao aktivni sastojak, sadrži N-[1-(5-cijano-piridin-2ilmetil)-1H-pirazol-3-il]-2-[4-(1-trifluorometil-ciklopropil)-fenil]-acetamid, ili njegovu farmaceutski prihvatljivu sol, i najmanje jedno terapijski inertno pomoćno sredstvo, naznačen time, da je za uporabu u prevenciji i/ili liječenju epilepsije, pri čemu se farmaceutski pripravak treba davati u kombinaciji s drugim farmaceutskim pripravkom koji kao aktivni sastojak, sadrži 5H-dibenzo[b,f]azepin-5-karboksamid, (RS)-3-etil-3-metil-pirolidin-2,5-dion, 6-(2,3-diklorofenil)-1,2,4-triazin-3,5-diamin, (S)-2-(2-oksopirolidin-1-il)butanamid, 10,11-dihidro-10-okso-5H-dibenz[b,f]azepin-5-karboksamid, 2-propilpentanska kiselina, N-(5-sulfamoil-1,3,4-tiadiazol-2-il)acetamid, (2S)-2-[(4R)-2-okso-4-propilpirolidin-1-il]butanamid, 7-kloro-1-metil-5-fenil-1,5-benzodiazepin-2,4-dion, 5-(2-klorofenil)-7-nitro-1,3-dihidro-1,4-benzodiazepin-2-on, (S)-10-acetoksi-10,11-dihidro-5H-dibenz[b,f]azepin-5-karboksamid, (3-karbamoiloksi-2-fenilpropil)karbamat, 1-(aminometil)cikloheksanoctena kiselina, (R)-2-acetamido-N-benzil-3-metoksipropanamid, 5’-(2-cijanofenil)-1’-fenil-2,3’-bipiridinil-6’(1’H)-on, 5-etil-5-fenil-1,3-diazinan-2,4,6-trion, 5,5-difenilimidazolidin-2,4-dion, 2-(2-oksopirolidin-1-il)acetamid, (3S)-3-(aminometil)-5-metilheksanska kiselina, 5-etil-5-fenil-1,3-diazinan-4,6-dion, etil (2-amino-4-((4-fluorobenzil)amino)fenil)karbamat, 1-(2,6-difluorobenzil)-1H-1,2,3-triazol-4-karboksamid, (RS)-(E)-4,4-dimetil-1-[3,4(metilendioksi)-fenil]-1-penten-3-ol, (3R)-1-[4,4-bis(3-metil-2-tienil)-3-buten-1-il]-3-piperidinkarboksilna kiselina, 2,3:4,5-bis-O-(1-metiletiliden)-β-D-fruktopiranoza sulfamat, (RS)-4-aminoheks-5-enska kiselina, ili benzo[d]izoksazol-3-ilmetansulfonamid; ili njihovu farmaceutski prihvatljivu sol, i najmanje jedno terapijski inertno pomoćno sredstvo.
18. Farmaceutski pripravak koji kao aktivni sastojak, sadrži 5H-dibenzo[b,f]azepin-5-karboksamid, (RS)-3-etil-3-metil-pirolidin-2,5-dion, 6-(2,3-diklorofenil)-1,2,4-triazin-3,5-diamin, (S)-2-(2-oksopirolidin-1-il)butanamid, 10,11-dihidro-10-okso-5H-dibenz[b,f]azepin-5-karboksamid, 2-propilpentanska kiselina, N-(5-sulfamoil-1,3,4-tiadiazol-2-il)acetamid, (2S)-2-[(4R)-2-okso-4-propilpirolidin-1-il]butanamid, 7-kloro-1-metil-5-fenil-1,5-benzodiazepin-2,4-dion, 5-(2-klorofenil)-7-nitro-1,3-dihidro-1,4-benzodiazepin-2-on, (S)-10-acetoksi-10,11-dihidro-5H-dibenz[b,f]azepin-5-karboksamid, (3-karbamoiloksi-2-fenilpropil)karbamat, 1-(aminometil) cikloheksanoctena kiselina, (R)-2-acetamido-N-benzil-3-metoksipropanamid, 5’-(2-cijanofenil)-1’-fenil-2,3’-bipiridinil-6’(1’H)-on, 5-etil-5-fenil-1,3-diazinan-2,4,6-trion, 5,5-difenilimidazolidin-2,4-dion, 2-(2-oksopirolidin-1-il)acetamid, (3S)-3-(aminometil)-5-metilheksanska kiselina, 5-etil-5-fenil-1,3-diazinan-4,6-dion, etil (2-amino-4-((4-fluorobenzil)amino)fenil)karbamat, 1-(2,6-difluorobenzil)-1H-1,2,3-triazol-4-karboksamid, (RS)-(E)-4,4-dimetil-1-[3,4(metilendioksi)-fenil]-1-penten-3-ol, (3R)-1-[4,4-bis(3-metil-2-tienil)-3-buten-1-il]-3-piperidinkarboksilna kiselina, 2,3:4,5-bis-O-(1-metiletiliden)-β-D-fruktopiranoza sulfamat, (RS)-4-aminoheks-5-enska kiselina, ili benzo[d]izoksazol-3-ilmetansulfonamid; ili njihovu farmaceutski prihvatljivu sol, i najmanje jedno terapijski inertno pomoćno sredstvo, naznačen time, da je za uporabu u prevenciji i/ili liječenju epilepsije, pri čemu se farmaceutski pripravak treba davati u kombinaciji s drugim farmaceutskim pripravkom koji kao aktivni sastojak, sadrži N-[1-(5-cijano-piridin-2ilmetil)-1H-pirazol-3-il]-2-[4-(1-trifluorometil-ciklopropil)-fenil]-acetamid, ili njegovu farmaceutski prihvatljivu sol, i najmanje jedno terapijski inertno pomoćno sredstvo.
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