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HRP20110278T1 - 1',3'-disupstituirani-4-fenil,3,4,5,6-tetrahidro-2h,1'h[1,4']bipiridinil-2'-oni - Google Patents

1',3'-disupstituirani-4-fenil,3,4,5,6-tetrahidro-2h,1'h[1,4']bipiridinil-2'-oni Download PDF

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HRP20110278T1
HRP20110278T1 HR20110278T HRP20110278T HRP20110278T1 HR P20110278 T1 HRP20110278 T1 HR P20110278T1 HR 20110278 T HR20110278 T HR 20110278T HR P20110278 T HRP20110278 T HR P20110278T HR P20110278 T1 HRP20110278 T1 HR P20110278T1
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Croatia
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disorder
disorders
nervous system
central nervous
3alkyl
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HR20110278T
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Maria Cid-Nunez Jos�
Avelino Trabanco-Suarez Andr�s
James Macdonald Gregor
Albert Jacques Duvey Guillaume
Johannes L�tjens Robert
Patrick Finn Terry
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Ortho-Mcneil-Janssen Pharmaceuticals
Addex Pharma S.A.
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Application filed by Ortho-Mcneil-Janssen Pharmaceuticals, Addex Pharma S.A. filed Critical Ortho-Mcneil-Janssen Pharmaceuticals
Publication of HRP20110278T1 publication Critical patent/HRP20110278T1/hr

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Abstract

Spoj koji ima formulu (1) ili njegov stereokemijski izomerni oblik, naznačen time, da R1 je C1-6alkil; ili C1-3alkil supstituiran sa C3-7cikloalkil, fenil, ili fenil supstituiran s halo, trifluorometil ili trifluorometoksi; R2 je halo, trifluorometil, C1-3alkil ili ciklopropil; R3 je vodik, fluoro, hidroksil, hidroksiC1-3alkil, hidroksiC1-3alkiloksi, fluoroC1-3alkil, fluoroC1-3alkiloksi ili cijano; i Ar je nesupstituirani fenil; ili fenil supstituiran s n radikalima R4, pri čemu n je 1, 2 ili 3; R4je odabran iz skupine koja sadrži vodik, halo, C1-3alkil, hidroksiC1-3alkil, polihaloC1-3alkil, cijano, hidroksil, amino, karboksil, C1-3alkiloksiC1-3alkil, C1-3alkiloksi, polihaloC1-3alkiloksi,

Claims (12)

1. Spoj koji ima formulu (1) [image] ili njegov stereokemijski izomerni oblik, naznačen time, da R1je C1-6alkil; ili C1-3alkil supstituiran sa C3-7cikloalkil, fenil, ili fenil supstituiran s halo, trifluorometil ili trifluorometoksi; R2 je halo, trifluorometil, C1-3alkil ili ciklopropil; R3 je vodik, fluoro, hidroksil, hidroksiC1-3alkil, hidroksiC1-3alkiloksi, fluoroC1-3alkil, fluoroC1-3alkiloksi ili cijano; i Ar je nesupstituirani fenil; ili fenil supstituiran s n radikalima R4, pri čemu n je 1, 2 ili 3; R4je odabran iz skupine koja sadrži vodik, halo, C1-3alkil, hidroksiC1-3alkil, polihaloC1-3alkil, cijano, hidroksil, amino, karboksil, C1-3alkiloksiC1-3alkil, C1-3alkiloksi, polihaloC1-3alkiloksi, C1-3alkilkarbonil, mono-i di(C1-3alkil)amino, i morfolinil; ili dva susjedna R4 radikala koji zajedno tvore bivalentni radikal formule -N=CH-NH- (a), -CH=CH-NH-(b), ili -O-CH2-CH2-NH- (c); ili R3 i R4 radikal u orto poziciji uzeti zajedno tvore bivalentni radikal formule -CH2-O- (d), ili -O-CH2- (e); ili njegova farmaceutski prihvatljiva sol ili solvat.
2. Spoj prema zahtjevu 1, naznačen time, da R1 je 1-butil, 2-metil-1-propil, 3-metil-1-butil, (ciklopropil)metil ili 2-(ciklopropil)-1-etil; R3 je vodik, fluoro ili cijano; i Ar je nesupstituirani fenil; ili fenil supstituiran s halo, trifluorometil, morfolinil ili hidroksiC1-3alkil; ili njegova farmaceutski prihvatljiva sol ili solvat.
3. Spoj prema zahtjevu 1, naznačen time, da R1 je 1-butil, 3-metil-1-butil, (ciklopropil)metil ili 2-(ciklopropil)-1-etil; R2 je kloro; R3 je vodik ili fluoro; i Ar je nesupstituirani fenil; ili fenil supstituiran s hidroksiC1-3alkil; ili njegova farmaceutski prihvatljiva sol ili solvat.
4. Spoj prema zahtjevu 1, naznačen time, da spomenuti spoj je odabran od: -3’-kloro-1’-ciklopropilmetil-4-fenil-3,4,5,6-tetrahidro-2H,1’H-[1,4’]bipiridinil-2’-ona; -1’-butil-3’-kloro-4-fenil-3,4,5,6-tetrahidro-2H, 1’H-[1,4’]bipiridinil-2’-ona; ili njegove farmaceutski prihvatljive soli ili solvata.
5. Farmaceutski sastav, naznačen time, da sadrži terapeutski učinkovitu količinu spoja prema bilo kojem od zahtjeva 1 do 4 i farmaceutski prihvatljiv nosač ili ekscipijent.
6. Spoj prema bilo kojem od zahtjeva 1 do 4, naznačen time, da se koristi kao lijek.
7. Spoj prema bilo kojem od zahtjeva 1 do 4 ili farmaceutski sastav prema zahtjevu 5, naznačen time, da se koristi za liječenje ili prevenciju stanja kod sisavaca, uključujući i čovjeka, čije je liječenje ili prevencija podržano ili olakšano neuromodulatornim učinkom pozitivnih alosteričnih modulatora mGluR2.
8. Spoj prema bilo kojem od zahtjeva 1 do 4 ili farmaceutski sastav prema zahtjevu 5, naznačen time, da se koristi za liječenje ili prevenciju poremećaja središnjeg nervnog sustava koji je odabran iz skupine sastavljene od anksioznih poremećaja, psihotičkih poremećaja, poremećaja osobnosti, smetnji povezanih sa supstancom, smetnji kod hranjenja, poremećaja raspoloženja, migrena, epilepsije ili konvulzivnih poremećaja, poremećaja djetinjstva, poremećaja spoznaje, neurodegeneracije, neurotoksičnosti i ishemije.
9. Spoj ili sastav prema zahtjevu 8, naznačen time, da poremećaj središnjeg nervnog sustava je poremećaj anksioznosti, odabran iz skupine koja sadrži agorafobiju, opći poremećaj anksioznosti (GAD), opsesivno-kompulzivni poremećaj (OCD), panične smetnje, smetnje od postraumatskog stresa (PTSD), socijalnu fobiju i ostale fobije; ili da je poremećaj središnjeg nervnog sustava psihotički poremećaj odabran iz skupine koja sadrži shizofreniju, iluzijski poremećaj, shizoafektivni poremećaj, shizofrenoformni poremećaj i psihotički poremećaj induciran supstancom; ili da je poremećaj središnjeg nervnog sustava poremećaj osobnosti odabran iz skupine koja sadrži opsesivno-kompulzivni poremećaj osobnosti i shizoidalne, shizotipalne smetnje; ili da je poremećaj središnjeg nervnog sustava poremećaj povezan sa supstancom odabran iz skupine koja sadrži zlostavljanje pod utjecajem alkohola, ovisnost o alkoholu, ustezanje od alkohola, delirij alkoholne apstinencije, psihotički poremećaj induciran alkoholom, ovisnost o amfetaminu, ustezanje od amfetamina, ovisnost o kokainu, ustezanje od kokaina, ovisnost o nikotinu, ustezanje od nikotina, ovisnost o opijatima i ustezanje od opijata; ili da je poremećaj središnjeg nervnog sustava smetnja hranjenja odabrana iz skupine koja sadrži anoreksiju (anorexia nervosa) i bulimiju (bulimia nervosa); ili da je poremećaj središnjeg nervnog sustava poremećaj raspoloženja odabran iz skupine koja sadrži bipolarne poremećaje (I & II), ciklotimički poremećaj, depresiju, distimički poremećaj, značajne depresivne smetnje i poremećaj raspoloženja induciran supstancom; ili da poremećaj središnjeg nervnog sustava je migrena; ili da poremećaj središnjeg nervnog sustava je epilepsija ili konvulzivni poremećaj odabran iz skupine koja sadrži opću nekonvulzivnu epilepsiju, opću konvulzivnu epilepsiju, petit mal status epilepticus, grand mal status epilepticus, djelomičnu epilepsiju sa ili bez oštećenja svjesnosti, infantilne spazme, epilepsiju partialis continua, i ostale oblike epilepsije; ili da je poremećaj središnjeg nervnog sustava poremećaj spoznaje odabran iz skupine koja sadrži delirij, trajan delirij induciran supstancom, demenciju, demenciju uzrokovanu oboljenjem HIV-a, demenciju uzrokovanu Huntingtonovom bolesti, demenciju uzrokovanu Parkinsonovom bolesti, demenciju uzrokovanu Alzheimerovom bolesti, trajnu demenciju induciranu supstancom i blago spoznajno oštećenje.
10. Spoj ili sastav prema zahtjevu 8, naznačen time, da poremećaj djetinjstva je pomanjkanje pažnje/hiperaktivnost.
11. Spoj ili sastav prema zahtjevu 8, naznačen time, da poremećaj središnjeg nervnog sustava je odabran iz skupine koju čine anksioznost, shizofrenija, migrena, depresija i epilepsija.
12. Spoj prema bilo kojem od zahtjeva 1 do 4, naznačen time, da se koristi u kombinaciji sa ortosteričnim agonistom mGluR2 za liječenje ili prevenciju stanja koja su navedena u bilo kojem od zahtjeva 7 do 11.
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