HRP20120876T1 - Brzo disocirajuä†i antagonisti dopamin 2 receptora - Google Patents

Brzo disocirajuä†i antagonisti dopamin 2 receptora Download PDF

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HRP20120876T1
HRP20120876T1 HRP20120876AT HRP20120876T HRP20120876T1 HR P20120876 T1 HRP20120876 T1 HR P20120876T1 HR P20120876A T HRP20120876A T HR P20120876AT HR P20120876 T HRP20120876 T HR P20120876T HR P20120876 T1 HRP20120876 T1 HR P20120876T1
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4alkyl
halo
substituents
independently selected
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Gregor James Macdonald
Xavier Jean Michel Langlois
José Manuel Bartolomé-Nebreda
Michiel Luc Maria Van Gool
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Janssen Pharmaceutica N.V.
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    • C07D237/06Heterocyclic compounds containing 1,2-diazine or hydrogenated 1,2-diazine rings not condensed with other rings having three double bonds between ring members or between ring members and non-ring members
    • C07D237/10Heterocyclic compounds containing 1,2-diazine or hydrogenated 1,2-diazine rings not condensed with other rings having three double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
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Claims (10)

1. Spoj formule (I) [image] ili njegov stereoizomerni oblik, naznačen time da R1 je kloro, trifluorometil ili cijano; R2 je fenil; fenil supstituiran sa 1, 2 ili 3 supstituenta koji su svaki nezavisno odabrani iz skupine koja sadrži halo, cijano, C1-4alkil, C1-4alkiloksi, C1-4alkilsulfonil, perfluoroC1-4alkil, perfluoroC1-4alkiloksi, diC1-4alkilamino, hidroksil, i fenil proizvoljno supstituiran sa 1, 2 ili 3 supstituenta koji su svaki nezavisno odabrani iz skupine koja sadrži halo, C1-4alkil i perfluoroC1-4alkil; tienil; tienil supstituiran sa 1 ili 2 supstituenta koji su svaki nezavisno odabrani iz skupine koja sadrži halo i C1-4alkil; naftil; piridinil; pirolil; benzotiazolil; indolil; kinolinil; C3-8cikloalkil; ili C5-7cikloalkenil; R3 je vodik, C1-4alkil, C1-4alkiloksi ili halo; R4 i R5 su svaki nezavisno vodik ili C1-4alkil, ili R4 i R5 zajedno tvore C1-4alkandiil; n je 1 ili 2; i R6 je vodik, C1-4alkil, hidroksiC2-4alkil, C3-6cikloalkil, C3-6cikloalkil-C1-4alkil, piridinilmetil, ili fenilmetil proizvoljno supstituiran na fenilu sa 1, 2 ili 3 supstituenta koji su svaki nezavisno odabrani iz skupine koja sadrži halo, cijano, C1-4alkil, C1-4alkiloksi, C1-4alkilsulfonil, perfluoroC1-4alkil, perfluoroC1-4alkiloksi i diC1-4alkilamino ; ili R5 i R6 zajedno tvore C2-5alkandiil; ili njegova farmaceutski prihvatljiva sol ili njegov solvat.
2. Spoj prema zahtjevu 1 naznačen time da R1 je kloro, trifluorometil ili cijano; R2 je fenil; fenil supstituiran sa 1, 2 ili 3 supstituenta koji su svaki nezavisno odabrani iz skupine koja sadrži halo, cijano, C1-4alkil, C1-4alkiloksi, C1-4alkilsulfonil, perfluoroC1-4alkil, perfluoroC1-4alkiloksi, diC1-4alkilamino, hidroksil, i fenil supstituiran sa 1, 2 ili 3 supstituenta koji su svaki nezavisno odabrani iz skupine koja sadrži halo, C1-4alkil i perfluoroC1-4alkil; tienil; tienil supstituiran sa 1 ili 2 supstituenta koji su svaki nezavisno odabrani iz skupine koja sadrži halo i C1-4alkil; naftil; piridinil; pirolil; benzotiazolil; indolil; kinolinil; C3-8cikloalkil; ili C5-7cikloalkenil; R3 je vodik, C1-4alkil ili halo; R4 i R5 su svaki nezavisno vodik ili C1-4alkil, ili R4 i R5 zajedno tvore C1-4alkandiil; n je 1 ili 2; i R6 je vodik, C1-4alkil, hidroksiC2-4alkil, C3-6cikloalkil, C3-6cikloalkilC1-4alkil, ili fenilmetil supstituiran na fenilu sa 1, 2 ili 3 supstituenta koji su svaki nezavisno odabrani iz skupine koja sadrži halo, cijano, C1-4alkil, C1-4alkiloksi, C1-4alkilsulfonil, perfluoroC1-4alkil, perfluoroC1-4alkiloksi i diC1-4alkilamino ; ili R5 i R6 zajedno tvore C2-5alkandiil; ili njegova farmaceutski prihvatljiva sol ili njegov solvat.
3. Spoj prema zahtjevu 1 naznačen time da R1 je trifluorometil ili cijano; R2 je fenil; fenil supstituiran sa 1, 2 ili 3 supstituenta koji su svaki nezavisno odabrani iz skupine koja sadrži halo, cijano, C1-4alkil, C1-4alkiloksi, C1-4alkilsulfonil, perfluoroC1-4alkil, diC1-4alkilamino, hidroksil, i fenil supstituiran sa 1, 2 ili 3 supstituenta koji su svaki nezavisno odabrani iz skupine koja sadrži halo, C1-4alkil i perfluoroC1-4alkil; tienil; tienil supstituiran sa 1 ili 2 supstituenta koji su svaki nezavisno odabrani iz skupine koja sadrži halo i C1-4alkil; naftil; piridinil; pirolil; benzotiazolil; indolil; kinolinil; C3-8cikloalkil; ili C5-7cikloalkenil; R3 je vodik; R4 i R5 su svaki nezavisno vodik ili C1-4alkil; n je 1; R6 je vodik, metil, etil, ciklopropil, ili fenilmetil supstituiran na fenilu sa 1, 2 ili 3 supstituenta koji su svaki nezavisno odabrani iz skupine koja sadrži halo, cijano, C1-4alkil, C1-4alkiloksi, C1-4alkilsulfonil, perfluoroC1-4alkil i diC1-4alkilamino ; ili R5 i R6 zajedno tvore C2-5alkandiil; ili njegova farmaceutski prihvatljiva sol ili njegov solvat.
4. Spoj prema zahtjevu 1 naznačen time da R1 je trifluorometil; R2 je fenil; fenil supstituiran sa 1, 2 ili 3 supstituenta koji su svaki nezavisno odabrani iz skupine koja sadrži halo, cijano, C1-4alkil, C1-4alkiloksi, C1-4alkilsulfonil, perfluoroC1-4alkil, diC1-4alkilamino, hidroksil, i fenil supstituiran sa 1, 2 ili 3 supstituenta koji su svaki nezavisno odabrani iz skupine koja sadrži halo, C1-4alkil i perfluoroC1-4alkil; tienil; tienil supstituiran sa 1 ili 2 supstituenta koji su svaki nezavisno odabrani iz skupine koja sadrži halo i C1-4alkil; naftil; piridinil; pirolil; benzotiazolil; indolil; kinolinil; C3-8cikloalkil; ili C5-7cikloalkenil; R3 je vodik; R4 i R5 su svaki nezavisno vodik ili metil; n je 1; R6 je vodik, etil ili (3,5-difluorofenil)metil; ili R5 i R6 zajedno tvore 1,3-propandiil; ili njegova farmaceutski prihvatljiva sol ili njegov solvat.
5. Spoj prema zahtjevu 1 naznačen time da spoj je 4-fenil-6-piperazin-1-il-3-trifluorometil-piridazin.
6. Spoj prema zahtjevu 1 naznačen time da spoj je 4-fenil-6-piperazin-1-il-3-trifluorometil-piridazin monohidroklorid.
7. Farmaceutski pripravak naznačen time da sadrži terapeutski učinkovitu količinu spoja kako je definirano u zahtjevu 1.
8. Spoj kako je definiran u zahtjevu 1 naznačen time da je za uporabu kao lijek.
9. Spoj kako je definiran u zahtjevu 8 naznačen time da je za uporabu kao antipsihotik.
10. Spoj kako je definiran u zahtjevu 8 naznačen time da je za uporabu kao lijek kod liječenja ili sprečavanja shizofrenije; poremećaja shizofrenog oblika; shizoafektivnog poremećaja; sumanutog poremećaja; kratkog psihotičnog poremećaja; dijeljenog psihotičnog poremećaja; psihotičnog poremećaja zbog općeg zdravstvenog stanja; psihotičnog poremećaja izazvanog drogama; psihotičnog poremećaja koji nije drugačije definiran; psihoze povezane s demencijom; teškog depresivnog poremećaja; distimije; predmenstrualnog disforičnog poremećaja; depresivnog poremećaja koji nije drugačije definiran; bipolarnog poremećaja I; bipolarnog poremećaja II; ciklotimije; bipolarnog poremećaja koji nije drugačije definiran; poremećaja raspoloženja zbog općeg zdravstvenog stanja; poremećaja raspoloženja izazvanog drogom; poremećaja raspoloženja koji nije drugačije definiran; općeg anksioznog poremećaja; opsesivno-kompulzivnog poremećaja; paničnog poremećaja; akutnog stresnog poremećaja; post-traumatskog stresnog poremećaja; mentalne zaostalosti; pervazivnih razvojnih poremećaja; poremećaja pažnje; poremećaja pažnje/hiperaktivnosti; poremećaja narušenog ponašanja; poremećaja osobnosti paranoidnog tipa; poremećaja osobnosti shizoidnog oblika; poremećaja osobnosti od shizotipičnog oblika; poremećaja sa tikovima; Touretteovog sindroma; ovisnosti o supstancama; zlouporabe supstanci; odvikavanja od supstanci; trikotilomanije; te stanja gdje je narušena spoznaja; Alzheimerove bolesti; Parkinsonove bolesti; Huntingdonove bolesti; Lewy Body demencije; demencija zbog HIV-a; demencije zbog Creutzfeldt-Jakobove bolesti; amnestičnih poremećaja; blagog kognitivnog poremećaja; senilnog spoznajnog propadanja; poremećaja hranjenja kao što su anoreksija i bulimija; te pretilost.
HRP20120876AT 2007-02-13 2012-10-30 Brzo disocirajuä†i antagonisti dopamin 2 receptora HRP20120876T1 (hr)

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EP07102222 2007-02-13
PCT/EP2008/051597 WO2008098892A1 (en) 2007-02-13 2008-02-11 Fast dissociating dopamine 2 receptor antagonists

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EP (1) EP2121630B1 (hr)
JP (1) JP5225292B2 (hr)
KR (1) KR101486408B1 (hr)
CN (1) CN101605764B (hr)
AR (1) AR065333A1 (hr)
AU (1) AU2008214716B2 (hr)
BR (1) BRPI0807492A2 (hr)
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CL (1) CL2008000440A1 (hr)
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EA (1) EA017508B1 (hr)
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HR (1) HRP20120876T1 (hr)
IL (1) IL200310A (hr)
JO (1) JO2849B1 (hr)
MX (1) MX2009008616A (hr)
MY (1) MY148899A (hr)
NZ (1) NZ578560A (hr)
PA (1) PA8768901A1 (hr)
PE (1) PE20081665A1 (hr)
PL (1) PL2121630T3 (hr)
PT (1) PT2121630E (hr)
RS (1) RS52515B (hr)
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SI (1) SI2121630T1 (hr)
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