HRP20170246T4 - Režim doziranja za selektivni agonist s1p1-receptora - Google Patents

Režim doziranja za selektivni agonist s1p1-receptora Download PDF

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HRP20170246T4
HRP20170246T4 HRP20170246TT HRP20170246T HRP20170246T4 HR P20170246 T4 HRP20170246 T4 HR P20170246T4 HR P20170246T T HRP20170246T T HR P20170246TT HR P20170246 T HRP20170246 T HR P20170246T HR P20170246 T4 HRP20170246 T4 HR P20170246T4
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compound
dose
pharmaceutically acceptable
acceptable salt
administered
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HRP20170246TT
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Patrick Brossard
Jasper Dingemanse
Oliver Nayler
Michael Scherz
Beat Steiner
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Actelion Pharmaceuticals Ltd.
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Application filed by Actelion Pharmaceuticals Ltd. filed Critical Actelion Pharmaceuticals Ltd.
Publication of HRP20170246T1 publication Critical patent/HRP20170246T1/hr
Publication of HRP20170246T4 publication Critical patent/HRP20170246T4/hr

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    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/41Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
    • A61K31/425Thiazoles
    • A61K31/4261,3-Thiazoles
    • AHUMAN NECESSITIES
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    • AHUMAN NECESSITIES
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    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/41Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
    • A61K31/425Thiazoles
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
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    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/41Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
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  • Health & Medical Sciences (AREA)
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  • Rheumatology (AREA)
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  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
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Claims (9)

1. Spoj, naznačen time, da je (R)-5-[3-kloro-4-(2,3-dihidroksi-propoksi)-benz[Z]iliden]-2-([Z]-propilimino)-3-o-tolil-tiazolidin-4-on (Spoj 1), ili njegova farmaceutski prihvatljiva sol, koji/koja se upotrebljava u liječenju i/ili prevenciji bolesti ili poremećaja koje/koji su odabrani iz skupine koja se sastoji od: odbacivanja transplantiranih organa, bolesti usadak protiv stanice domaćina, koja je nastala nakon transplantacije matične stanice, autoimunih sindroma izabranih od reumatoidnog artritisa, multiple skleroze, upalne bolesti crijeva odabrane od Crohnove bolesti i ulcerativnog kolitisa, psorijaze, psorijatskog artritisa, Hashimoto-tiroiditisa i uveoretinitisa, atopijske bolesti odabrane od rinitisa, konjunktivitisa i dermatitisa, astme, dijabetesa tipa I, autoimunih bolesti koje su posljedice infekcija izabranih od reumatske groznice i postinfektivnog glomerulonefritisa, solidnih vrsta raka i tumorskih metastaza, pri čemu se Spoj 1 ili njegova farmaceutski prihvatljiva sol treba primjenjivati oralno kod ljudskog pojedinca na takav način, da se za vrijeme inicijalne faze liječenja, Spoj 1 treba davati u inicijalnoj dozi koja je između dva do pet puta ili pet do 16 puta manja nego ciljana doza, sve dok ne prestane daljnje akutno smanjenje srčane frekvencije, gdje se akutno smanjenje srčane frekvencije odnosi na smanjenje brzine rada srca od vrijednosti srčane frekvencije prije uzimanja doze, za 10 ili više udaraca u minuti (bpm) što je maksimalna vrijednost unutar vremena od jednog do tri sata nakon uzimanja lijeka, te nakon toga slijedi podizanje titracije s povećavanjem doze do ciljane doze, pri čemu je ciljana doza 20 ili 40 mg Spoja 1, koja se treba davati p.o. jednom dnevno, dok se doza koja je niža od ciljane doze, treba davati u doznim frekvencijama od jednom do dva puta dnevno, te pritom podizanje titracije do ciljane doze, treba biti učinjeno s jednim ili s nekoliko doznih prirasta.
2. Spoj 1, ili njegova farmaceutski prihvatljiva sol za uporabu prema zahtjevu 1, naznačen/a time, da ciljana doza iznosi 20 mg Spoja 1, koja se treba davati p.o. jednom dnevno.
3. Spoj 1, ili njegova farmaceutski prihvatljiva sol za uporabu prema zahtjevu 1, naznačen/a time, da ciljana doza iznosi 40 mg Spoja 1, koja se treba davati p.o. jednom dnevno.
4. Spoj 1, ili njegova farmaceutski prihvatljiva sol za uporabu prema bilo kojem od zahtjeva 1 do 3, naznačen/a time, da se doza koja je manja od ciljane doze, treba davati pojedincu za vrijeme inicijalnih dva do četiri dana od trajanja liječenja.
5. Spoj 1, ili njegova farmaceutski prihvatljiva sol za uporabu prema zahtjevu 1 ili 2, naznačen/a time, da se Spoj 1 treba davati po 5 mg p.o. jednom dnevno za vrijeme od tri dana tijekom inicijalne faze liječenja, nakon čega slijedi podizanje titracije na 10 mg p.o. jednom dnevno u trajanju od tri dana, dok nakon toga slijedi podizanje titracije na ciljanu dozu od 20 mg koja se treba davati p.o. jednom dnevno.
6. Spoj 1, ili njegova farmaceutski prihvatljiva sol za uporabu prema zahtjevu 1 ili 2, naznačen/a time, da se Spoj 1 treba davati po 5 mg p.o. jednom dnevno u trajanju od tri dana za vrijeme inicijalne faze liječenja, nakon čega slijedi podizanje titracije na ciljanu dozu od 20 mg koja se treba davati p.o. jednom dnevno.
7. Spoj 1, ili njegova farmaceutski prihvatljiva sol za uporabu prema bilo kojem od zahtjeva 1 do 6, naznačen/a time, da su bolesti ili poremećaji koje/koji se trebaju liječiti i/ili prevenirati, odabrani iz skupine koju čine: odbacivanje transplantiranih organa izabranih od bubrega, jetre, srca i pluća; bolest usadak protiv stanice domaćina, koja se pojavila nakon transplantacije matične stanice; autoimuni sindromi izabrani od reumatoidnog artritisa, multiple skleroze, psorijaze, psorijatskog artritisa, Crohnove bolesti i Hashimotoovog tiroiditisa; te atopijski dermatitis.
8. Spoj 1, ili njegova farmaceutski prihvatljiva sol za uporabu prema bilo kojem od zahtjeva 1 do 6, naznačen/a time, da su bolesti ili poremećaji koje/koji se trebaju liječiti i/ili prevenirati, odabrane/i od multiple skleroze i psorijaze.
9. Spoj 1, ili njegova farmaceutski prihvatljiva sol za uporabu prema bilo kojem od zahtjeva 1 do 6, naznačen/a time, da se kod bolesti ili poremećaja koja/koji se treba liječiti, radi o multiploj sklerozi.
HRP20170246TT 2008-03-17 2017-02-15 Režim doziranja za selektivni agonist s1p1-receptora HRP20170246T4 (hr)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
IB2008050995 2008-03-17
EP09721703.8A EP2278960B2 (en) 2008-03-17 2009-03-12 Dosing regimen for a selective sip1 receptor agonist
PCT/IB2009/051030 WO2009115954A1 (en) 2008-03-17 2009-03-12 Dosing regimen for a selective s1p1 receptor agonist

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HRP20170246T1 HRP20170246T1 (hr) 2017-04-07
HRP20170246T4 true HRP20170246T4 (hr) 2020-02-07

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US (6) US8785484B2 (hr)
EP (1) EP2278960B2 (hr)
JP (2) JP4846063B2 (hr)
KR (3) KR101718639B1 (hr)
CN (2) CN101980704A (hr)
AR (1) AR070842A1 (hr)
AU (1) AU2009227629B2 (hr)
BR (1) BRPI0909625B1 (hr)
CA (1) CA2716448A1 (hr)
CY (1) CY1118648T1 (hr)
DK (1) DK2278960T4 (hr)
ES (1) ES2617628T5 (hr)
HR (1) HRP20170246T4 (hr)
HU (1) HUE033168T2 (hr)
IL (1) IL208154A (hr)
LT (1) LT2278960T (hr)
MA (1) MA32233B1 (hr)
MX (1) MX2010009853A (hr)
MY (1) MY177360A (hr)
NZ (1) NZ588505A (hr)
PL (1) PL2278960T5 (hr)
PT (1) PT2278960T (hr)
RU (1) RU2519660C2 (hr)
SI (1) SI2278960T2 (hr)
TW (1) TWI434688B (hr)
WO (1) WO2009115954A1 (hr)
ZA (1) ZA201007367B (hr)

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