HRP20191163T1 - Heteroaromatski spojevi i njihova upotreba kao dopaminskih liganda d1 - Google Patents

Heteroaromatski spojevi i njihova upotreba kao dopaminskih liganda d1 Download PDF

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HRP20191163T1
HRP20191163T1 HRP20191163TT HRP20191163T HRP20191163T1 HR P20191163 T1 HRP20191163 T1 HR P20191163T1 HR P20191163T T HRP20191163T T HR P20191163TT HR P20191163 T HRP20191163 T HR P20191163T HR P20191163 T1 HRP20191163 T1 HR P20191163T1
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alkyl
cycloalkyl
group
haloalkyl
alkoxy
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Michael Aaron Brodney
Jennifer Elizabeth Davoren
Amy Beth Dounay
Ivan Viktorovich Efremov
David Lawrence Firman Gray
Michael Eric GREEN
Jaclyn Louise HENDERSON
Chewah LEE
Scot Richard MENTE
Steven Victor O'neil
Bruce Nelsen Rogers
Lei Zhang
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Pfizer Inc.
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Publication of HRP20191163T1 publication Critical patent/HRP20191163T1/hr

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Claims (22)

1. Spoj Formule I: , ili njegova farmaceutski prihvatljiva sol, naznačen time što: svakog od T1, T2, T3 i T4 se neovisno bira iz skupine koju čine H, halogen, -CN, -SF5, -OH, -N(Ra)(Rb), -C(=O)-N(Ra)(Rb), -C(=O)-ORc, -C(=O)-Rd, C1-6 alkil, C1-6 halogenalkil, C2-6 alkenil, C2-6 alkinil, C1-6 alkoksi, C1-6 halogenalkoksi, -S-(C1-6 alkil), C3-7 cikloalkil, 4- do 7-eročlani heterocikloalkil, C3-7 cikloalkoksi, 5- ili 6-eročlani heteroaril, ciklopropilmetil, te ciklobutilmetil, gdje svaki od C1-6 alkil, C2-6 alkenil, C2-6 alkinil, -S-(C1-6 alkil), te C1-6 alkoksi može biti supstituiran s jednim ili više supstituenata, od kojih se svakog neovisno bira iz skupine koju čine halogen, -OH, -CN, -N(Ra)(Rb), C1-4 alkoksi, C1-4 halogenalkoksi, te -S-(C1-4 alkil); te gdje svaki od C3-7 cikloalkil, 4- do 7-eročlani heterocikloalkil, C3-7 cikloalkoksi, 5- ili 6-eročlani heteroaril, ciklopropilmetil, te ciklobutilmetil u T1, T2, i T3 može biti supstituiran s jednim ili više supstituenata, od kojih se svakog neovisno bira iz skupine koju čine halogen, -OH, -CN, okso, -N(Ra)(Rb), -C(=O)OH, -C(=O)-C1-4 alkil, -C(=O)-O-C1-4 alkil, -C(=O)-N(Ra)(Rb), C1-4 alkil, C1-4 halogenalkil, C1-4 hidroksilalkil, C1-4 cijanoalkil, C1-4 alkoksi, C1-4 halogenalkoksi, te -S-(C1-4 alkil); L1 se bira iz skupine koju čine O i S; svakog od Ra i Rb se neovisno bira iz skupine koju čine H, C1-4 alkil, C3-7 cikloalkil, te ciklopropilmetil; ili Ra i Rb zajedno s N atomom na kojeg su vezani tvore 4- do 7-eročlani heterocikloalkil, koji može biti supstituiran s jednim ili više supstituenata, od kojih se svakog neovisno bira iz skupine koju čine halogen, -OH, -CN, okso, -NH2, -NH(C1-4 alkil), -N(C1-4 alkil)2, -C(=O)OH, -C(=O)-C1-4 alkil, -C(=O)-O-C1-4 alkil, -C(=O)-NH2, -C(=O)-NH(C1-4 alkil), - C(=O)-N(C1-4 alkil)2, C1-4 alkil, C1-4 halogenalkil, C1-4 hidroksilalkil, C1-4 cijanoalkil, C1-4 alkoksi, -S-(C1-4 alkil), te C1-4 halogenalkoksi; svaki od Rc i Rd je neovisno C1-4 alkil, C3-4 cikloalkil-C1-2 alkil-, ili C3-4 cikloalkil; Q1 je Q1b: , uz uvjet da je atom ugljika u prstenu Q1 vezan na benzenski prsten Formule I; svaki od X1 i X2 je neovisno O ili S; svaki od R1, R2, R3 i R4 se neovisno bira iz skupine koju čine H, halogen, -OH, -NO2, -CN, -SF5, C1-6 alkil, C1-6 halogenalkil, C1-6 halogenalkoksi, C2-6 alkenil, C2-6 alkinil, C3-7 cikloalkil, 4- do 10-eročlani heterocikloalkil, -N(R5)(R6), -N(R7)(C(=O)R8), -C(=O)-N(R5)(R6), -C(=O)-R8, -C(=O)-OR8, -N(R7)(S(=O)2R8), -S(=O)2N(R5)(R6), -SR8, te -OR8, gdje svaki od C1-6 alkil, C3-7 cikloalkil, i heterocikloalkil može biti supstituiran s 1, 2 ili 3 supstituenta, od kojih se svakog neovisno bira iz skupine koju čine halogen, -CN, okso, -OH, C1-4 alkil, C1-4 alkoksi, C1-4 halogenalkil, C1-4 halogenalkoksi, C3-6 cikloalkil, -N(R5)(R6), -N(R7)(C(=O)R8), -C(=O)-OR8, -C(=O)H, -C(=O)R8, -C(=O)N(R5)(R6), -N(R7)(S(=O)2R8), -S(=O)2-N(R5)(R6), -SR8, te -OR8; ili R2 i R4 zajedno s dva atoma ugljika na koje su vezani tvore kondenzirani 5- ili 6-eročlani heteroaril, kondenzirani 5- ili 6-eročlani heterocikloalkilni prsten, kondenzirani 5- ili 6-eročlani cikloalkilni prsten, ili kondenzirani benzenski prsten, gdje svaki od kondenziranih prstena može biti supstituiran s 1, 2 ili 3 supstituenta, od kojih se svakog neovisno bira iz skupine koju čine halogen, -CN, -OH, C1-4 alkil, C1-4 alkoksi, C1-4 halogenalkil, te C1-4 halogenalkoksi, te gdje kondenzirani heterocikloalkilni prsten ili kondenzirani cikloalkilni prsten može biti dodatno supstituiran s 1, 2 ili 3 okso; R5 je H, C1-4 alkil, C1-4 halogenalkil ili C3-7 cikloalkil; R6 je H ili se bira iz skupine koju čine C1-4 alkil, C1-4 halogenalkil, C3-7 cikloalkil, 4- do 10-eročlani heterocikloalkil, C6-10 aril, 5- do 10-eročlani heteroaril, (C3-7 cikloalkil)-C1-4 alkil-, (4- do 10-eročlani heterocikloalkil)-C1-4 alkil-, (C6-10 aril)-C1-4 alkil-, te (5- do 10-eročlani heteroaril)-C1-4 alkil-, gdje svaki od odabira iz skupine može biti supstituiran s 1, 2, 3 ili 4 supstituenta, od kojih se svakog neovisno bira iz skupine koju čine -OH, -CN, C1-4 alkil, C3-7 cikloalkil, C1-4 hidroksilalkil, -S-C1-4 alkil, -C(=O)H, -C(=O)-C1-4 alkil, -C(=O)-O-C1-4 alkil, -C(=O)-NH2, -C(=O)-N(C1-4 alkil)2, C1-4 halogenalkil, C1-4 alkoksi, te C1-4 halogenalkoksi; ili R5 i R6 zajedno s N atomom na kojeg su vezani tvore 4- do 10-eročlani heterocikloalkil ili 5- do 10-eročlani heteroaril, od kojih svaki može biti supstituiran s 1, 2, 3, 4 ili 5 supstituenata, od kojih se svakog neovisno bira iz skupine koju čine halogen, -OH, okso, -C(=O)H, -C(=O)-C1-4 alkil, -C(=O)OH, -C(=O)-OC1-4 alkil, -C(=O)-NH2, -C(=O)-N(C1-4 alkil)2, -CN, C1-4 alkil, C1-4 alkoksi, C1-4 hidroksilalkil, C1-4 halogenalkil, te C1-4 halogenalkoksi; R7 se bira iz skupine koju čine H, C1-4 alkil, te C3-7 cikloalkil; R8 se bira iz skupine koju čine C1-6 alkil, C3-7 cikloalkil, 4- do 10-eročlani heterocikloalkil, C6-10 aril, 5- do 10-eročlani heteroaril, (C3-7 cikloalkil)-C1-4 alkil-, (4- do 10-eročlani heterocikloalkil)-C1-4 alkil-, (C6-10 aril)-C1-4 alkil-, te (5- do 10-eročlani heteroaril)-C1-4 alkil-, gdje svaki od odabira iz skupine može biti supstituiran s 1, 2 ili 3 supstituenta, od kojih se svakog neovisno bira iz skupine koju čine halogen, -CF3, -CN, -OH, okso, -S-C1-4 alkil, C1-4 alkil, C1-4 halogenalkil, C2-6 alkenil, C2-6 alkinil, C3-7 cikloalkil, C1-4 alkoksi, te C1-4 halogenalkoksi; R10 se bira iz skupine koju čine halogen, -OH, -CN, -SF5, -NO2, C1-6 alkil, C1-6 halogenalkil, C1-6 hidroksilalkil, C1-6 alkoksi, C1-6 halogenalkoksi, C3-7 cikloalkil, C2-6 alkenil, C2-6 alkinil, C6-10 aril, 4- do 10-eročlani heterocikloalkil, 5- do 10-eročlani heteroaril, (C3-7 cikloalkil)-C1-4 alkil-, (4- do 10-eročlani heterocikloalkil)-C1-4 alkil-, (C6-10 aril)-C1-4 alkil-, (5- do 10-eročlani heteroaril)-C1-4 alkil-, -N(R5)(R6), -N(R7)(C(=O)R8), -S(=O)2N(R5)(R6), -C(=O)-N(R5)(R6), -C(=O)-R8, -C(=O)-OR8, -SR8, te -OR8, gdje svaki od C1-6 alkil, C3-7 cikloalkil, C6-10 aril, 4- do 10-eročlani heterocikloalkil, 5- do 10-eročlani heteroaril, (C3-7 cikloalkil)-C1-4 alkil-, (4- do 10-eročlani heterocikloalkil)-C1-4 alkil-, (C6-10 aril)-C1-4 alkil-, te (5- do 10-eročlani heteroaril)-C1-4 alkil- može biti supstituiran s 1, 2, 3 ili 4 supstituenta, od kojih se svakog neovisno bira iz skupine koju čine halogen, -OH, -CN, -NO2, C1-4 alkil, C1-4 hidroksilalkil, C1-4 alkoksi, -N(R5)(R6), -S-(C1-4 alkil), -S(=O)2-(C1-4 alkil), C6-10 ariloksi, [(C6-10 aril)-C1-4 alkiloksi- koji može biti supstituiran s 1 ili 2 C1-4 alkil], okso, -C(=O)H, -C(=O)-C1-4 alkil, -C(=O)O-C1-4 alkil, -C(=O)NH2, -NHC(=O)H, -NHC(=O)-(C1-4 alkil), C3-7 cikloalkil, a 5- ili 6-eročlani heteroaril, C1-4 halogenalkil, te C1-4 halogenalkoksi; R10A se bira iz skupine koju čine H, C1-6 alkil, C1-6 hidroksilalkil, C2-6 alkenil, -S(=O)2N(R5)(R6), -C(=O)-N(R5)(R6), -C(=O)-R8, -C(=O)-OR8, -SR15, -C(R14)2-OH, -C(R14)2-OS(=O)2H, -C(R14)2-OP(=O)(OH)2, -C(R14)2-OR15, -C(R14)2-OC(=O)-R15, -C(R14)2-N(R5)(R6); R10B se bira iz skupine koju čine H, C1-6 alkil, C1-6 halogenalkil, C1-6 hidroksilalkil, C3-7 cikloalkil, C3-6 alkenil, C3-6 alkinil, C6-10 aril, 4- do 10-eročlani heterocikloalkil, 5- do 10-eročlani heteroaril, (C3-7 cikloalkil)-C1-4 alkil-, (4- do 10-eročlani heterocikloalkil)-C1-4 alkil-, (C6-10 aril)-C1-4 alkil-, (5- do 10-eročlani heteroaril)-C1-4 alkil-, -S(=O)2N(R5)(R6), -C(=O)-N(R5)(R6), -C(=O)-R8, i -C(=O)-OR8, gdje svaki od C1-6 alkil, C3-7 cikloalkil, C6-10 aril, 4- do 10-eročlani heterocikloalkil, 5- do 10-eročlani heteroaril, (C3-7 cikloalkil)-C1-4 alkil-, (4- do 10-eročlani heterocikloalkil)-C1-4 alkil-, (C6-10 aril)-C1-4 alkil-, te (5- do 10-eročlani heteroaril)-C1-4 alkil-, može biti supstituiran s 1, 2, 3 ili 4 supstituenta, od kojih se svakog neovisno bira iz skupine koju čine halogen, -OH, -CN, -NO2, C1-4 alkil, C1-4 hidroksilalkil, C1-4 alkoksi, -N(R5)(R6), -S-(C1-4 alkil), -S(=O)2-(C1-4 alkil), C6-10 ariloksi, [(C6-10 aril)-C1-4 alkiloksi- koji može biti supstituiran s 1 ili 2 C1-4 alkil], okso, -C(=O)H, -C(=O)-C1-4 alkil, -C(=O)O-C1-4 alkil, -C(=O)NH2, -NHC(=O)H, -NHC(=O)-(C1-4 alkil), -OC(=O)-C1-4 alkil, C3-7 cikloalkil, a 5- ili 6-eročlani heteroaril, C1-4 halogenalkil, te C1-4 halogenalkoksi; svaki R14 je neovisno H ili se bira iz skupine koju čine C1-10 alkil, C3-14 cikloalkil, C2-10 alkenil, C2-10 alkinil, C6-10 aril, 4- do 10-eročlani heterocikloalkil, 5- do 10-eročlani heteroaril, (C3-14 cikloalkil)-C1-10 alkil-, (4- do 14-eročlani heterocikloalkil)-C1-10 alkil-, (C6-10 aril)-C1-10 alkil-, (5- do 10-eročlani heteroaril)-C1-10 alkil-, gdje svaki od odabira između skupina može biti supstituiran s 1, 2, 3 ili 4 supstituenta, od kojih se svakog neovisno bira iz skupine koju čine halogen, -OH, -CN, -NO2, C1-4 alkil, C1-4 hidroksilalkil, C1-4 alkoksi, -N(R5)(R6), -N(R7)C(=O)R8, -N(R7)C(=O)OR8, -N(R7)S(=O)2R8, -S(=O)2N(R5)(R6), -C(=O)-N(R5)(R6), -C(=O)-R8, -C(=O)-OR8, -SR8, -OR8, -S(=O)2-R8, C6-10 ariloksi, [(C6-10 aril)-C1-4 alkiloksi-koji može biti supstituiran s 1 ili 2 C1-4 alkil], okso, -C(=O)H, -NHC(=O)H, C3-7 cikloalkil, a 5- ili 6-eročlani heteroaril, C1-4 halogenalkil, te C1-4 halogenalkoksi; R15 se bira iz skupine koju čine C1-20 alkil, C3-14 cikloalkil, C2-20 alkenil, C2-20 alkinil, C6-10 aril, 4- do 14-eročlani heterocikloalkil, 5- do 10-eročlani heteroaril, (C3-14 cikloalkil)-C1-20 alkil-, (4- do 10-eročlani heterocikloalkil)-C1-20 alkil-, (C6-10 aril)-C1-20 alkil-, (5- do 10-eročlani heteroaril)-C1-20 alkil-, gdje svaki od odabira između skupina može biti supstituiran s 1, 2, 3 ili 4 supstituenta, od kojih se svakog neovisno bira iz skupine koju čine halogen, -OH, -CN, -NO2, C1-4 alkil, C1-4 hidroksilalkil, C1-4 alkoksi, -N(R5)(R6), -N(R7)C(=O)R8, -N(R7)C(=O)OR8, -N(R7)S(=O)2R8, -S(=O)2N(R5)(R6), -C(=O)-N(R5)(R6), -C(=O)-R8, -C(=O)-OR8, -SR8, -OR8, -S(=O)2-R8, C6-10 ariloksi, [(C6-10 aril)-C1-4 alkiloksi- koji može biti supstituiran s 1 ili 2 C1-4 alkil], okso, -C(=O)H, -NHC(=O)H, C3-7 cikloalkil, a 5- ili 6-eročlani heteroaril, C1-4 halogenalkil, te C1-4 halogenalkoksi; i t2 je 0 ili 1.
2. Spoj u skladu s patentnim zahtjevom 1, ili njegova farmaceutski prihvatljiva sol, naznačen time što je spoj Formule I spoj Formule IB-1, IB-2, IB-3, IB-4 ili IB-5, IB-6, IB-7, IB-8, IB-9 ili IB-10:
3. Spoj u skladu s bilo kojim od patentnih zahtjeva 1 ili 2, ili njegova farmaceutski prihvatljiva sol, naznačen time što: R10 se bira iz skupine koju čine -CN, C1-4 alkil, C3-4 cikloalkil, ciklopropilmetil, te ciklobutilmetil, gdje C1-4 alkil u R10 može biti supstituiran s 1, 2, 3 ili 4 supstituenta, od kojih se svakog neovisno bira iz skupine koju čine halogen, -OH, -CN, C1-4 alkoksi, te C1-4 halogenalkoksi; te gdje svaki od C3-4 cikloalkila, ciklopropilmetila, te ciklobutilmetila u R10 može biti supstituiran s 1, 2, 3 ili 4 supstituenta, od kojih se svakog neovisno bira iz skupine koju čine halogen, -OH, -CN, C1-4 alkil, C1-4 halogenalkil, C1-4 hidroksilalkil, C1-4 alkoksi, te C1-4 halogenalkoksi; R10A se bira iz skupine koju čine H, C1-3 alkil, C1-3 hidroksilalkil, C2-4 alkenil, -S(=O)2N(R5)(R6), -C(=O)-N(R5)(R6), -C(=O)-R8, -C(=O)-OR8, -C(R14)2-OH, -C(R14)2-OS(=O)2H, -C(R14)2-OP(=O)(OH)2, -C(R14)2-OR15, te -C(R14)2-OC(=O)-R15; i R10B se bira iz skupine koju čine C1-4 alkil, C3-4 cikloalkil, ciklopropilmetil, te ciklobutilmetil, gdje C1-4 alkil u R10B može biti supstituiran s 1, 2, 3 ili 4 supstituenta, od kojih se svakog neovisno bira iz skupine koju čine halogen, -OH, -CN, C1-4 alkoksi, te C1-4 halogenalkoksi; te gdje svaki od C3-4 cikloalkila, ciklopropilmetila, te ciklobutilmetila u R10B može biti supstituiran s 1, 2, 3 ili 4 supstituenta, od kojih se svakog neovisno bira iz skupine koju čine halogen, -OH, -CN, C1-4 alkil, C1-4 halogenalkil, C1-4 hidroksilalkil, C1-4 alkoksi, te C1-4 halogenalkoksi.
4. Spoj u skladu s bilo kojim od patentnih zahtjeva 1 do 3, ili njegova farmaceutski prihvatljiva sol, naznačen time što se svakog od R10 i R10B neovisno bira iz skupine koju čine C1-3 alkil, C1-3 halogenalkil, te ciklopropil.
5. Spoj u skladu s bilo kojim od patentnih zahtjeva patentnim zahtjevom 1 do 4, ili njegova farmaceutski prihvatljiva sol, naznačen time što je svaki od R10 i R10B neovisno metil ili etil.
6. Spoj u skladu s bilo kojim od patentnih zahtjeva 1 do 5, ili njegova farmaceutski prihvatljiva sol, naznačen time što se svakog od R1 i R2 neovisno bira iz skupine koju čine H, halogen, -CN, C1-6 alkil, C1-6 halogenalkil, C1-6 alkoksi, C1-6 halogenalkoksi, C3-6 cikloalkil, -C(=O)-(C1-4 alkil), te C(=O)-O-(C1-4 alkil), gdje svaki od C1-6 alkil i C3-6 cikloalkil može biti supstituiran s 1, 2 ili 3 supstituenta, od kojih se svakog neovisno bira između halogena, -OH, -CN, C1-4 alkil, C1-4 halogenalkila, C1-4 alkoksi, te C1-4 halogenalkoksi.
7. Spoj u skladu s bilo kojim od patentnih zahtjeva 1 do 6, ili njegova farmaceutski prihvatljiva sol, naznačen time što je svaki od R1 i R2 neovisno H, metil ili halogen.
8. Spoj u skladu s bilo kojim od patentnih zahtjeva 1 do 7, ili njegova farmaceutski prihvatljiva sol, naznačen time što je svaki od R1 i R2 H.
9. Spoj u skladu s bilo kojim od patentnih zahtjeva 1 do 8, ili njegova farmaceutski prihvatljiva sol, naznačen time što se svakog od R3 i R4 neovisno bira iz skupine koju čine H, halogen, -CN, - C1-4 alkil, C1-4 alkoksi, te C3-4 cikloalkil, gdje svaki od C1-4 alkil i C1-4 alkoksi u R3 i R4 može biti supstituiran s 1, 2 ili 3 supstituenta, od kojih se svakog neovisno bira između halogena, -OH, C1-4 alkoksi, te C1-4 halogenalkoksi; te gdje C3-4 cikloalkil u R3 i R4 može biti supstituiran s 1, 2 ili 3 supstituenta, od kojih se svakog neovisno bira između halogena, -OH, C1-4 alkila, C1-4 halogenalkila, C1-4 alkoksi, te C1-4 halogenalkoksi.
10. Spoj u skladu s bilo kojim od patentnih zahtjeva 1 do 9, ili njegova farmaceutski prihvatljiva sol, naznačen time što je R3 H; a R4 je H, halogen, ili metil, gdje metil može biti supstituiran s 1, 2 ili 3 supstituenta, od kojih se svakog neovisno bira iz skupine koju čine halogen, -OH, te C1-4 alkoksi.
11. Spoj u skladu s bilo kojim od patentnih zahtjeva 1 do 10, ili njegova farmaceutski prihvatljiva sol, naznačen time što je R3 H, a R4 je metil.
12. Spoj u skladu s bilo kojim od patentnih zahtjeva 1 do 11, ili njegova farmaceutski prihvatljiva sol, naznačen time što se svakog od T1, T2, T3 i T4 neovisno bira iz skupine koju čine H, halogen, -CN, C1-4 alkil, C1-4 halogenalkil, C2-4 alkenil, C1-4 alkoksi, C1-4 halogenalkoksi, te C3-4 cikloalkil, gdje svaki od C1-4 alkila, C2-4 alkenila, te C1-4 alkoksi u T1, T2, T3 i T4 može biti supstituiran s jednim ili više supstituenata, od kojih se svakog neovisno bira iz skupine koju čine halogen, -OH, -CN, C1-4 alkoksi, te C1-4 halogenalkoksi; te gdje C3-4 cikloalkil u T1, T2, T3 i T4 može biti supstituiran s jednim ili više supstituenata, od kojih se svakog neovisno bira iz skupine koju čine halogen, -OH, -CN, C1-4 alkil, C1-4 halogenalkil, C1-4 hidroksilalkil, C1-4 cijanoalkil, C1-4 alkoksi, te C1-4 halogenalkoksi.
13. Spoj u skladu s bilo kojim od patentnih zahtjeva 1 do 12, ili njegova farmaceutski prihvatljiva sol, naznačen time što se svakog od T1, T2, T3 i T4 neovisno bira iz skupine koju čine H, halogen, C1-4 alkil, C1-4 hidroksilalkil, C1-4 halogenalkil, C1-4 alkoksi, C1-4 halogenalkoksi, C3-4 cikloalkil, te C3-4 halogencikloalkil.
14. Spoj u skladu s bilo kojim od patentnih zahtjeva 1 do 13, ili njegova farmaceutski prihvatljiva sol, naznačen time što se T1 bira iz skupine koju čine halogen, ciklopropil, halogenciklopropil, metil, C1 halogenalkil, metoksi, te C1 halogenalkoksi; a T4 je H.
15. Spoj u skladu s patentnim zahtjevom 1, naznačen time što je (–)-6-{4-[(3-ciklopropilpiridin-2-il)oksi]-2-metilfenil}-1,5-dimetilpirimidin-2,4(1H,3H)-dion, ili njegova farmaceutski prihvatljiva sol.
16. Spoj u skladu s patentnim zahtjevom 1, naznačen time što je (–)-6-{4-[(3-klor-5-fluorpiridin-2-il)oksi]-2-metilfenil}-1,5-dimetilpirimidin-2,4(1H,3H)-dion, ili njegova farmaceutski prihvatljiva sol.
17. Spoj u skladu s patentnim zahtjevom 1, naznačen time što je 6-{4-[(3-klorpiridin-2-il)oksi]-2-metilfenil}-5-etil-1-metilpirimidin-2,4(1H,3H)-dion, ili njegova farmaceutski prihvatljiva sol.
18. Spoj u skladu s patentnim zahtjevom 1, naznačen time što je (–)-1,5-dimetil-6-(2-metil-4-{[3-(trifluormetil) piridin-2-il]oksi}fenil)pirimidin-2,4(1H,3H)-dion, ili njegova farmaceutski prihvatljiva sol.
19. Spoj u skladu s patentnim zahtjevom 1, naznačen time što je (–)-6-{4-[(3-klor-5-metilpiridin-2-il)oksi]-2-metilfenil}-1,5-dimetilpirimidin-2,4(1H,3H)-dion, ili njegova farmaceutski prihvatljiva sol.
20. Farmaceutski pripravak, naznačen time što sadrži spoj u skladu s bilo kojim od patentnih zahtjeva 1 do 19, ili njegovu farmaceutski prihvatljivu sol, kao i farmaceutski prihvatljivu podlogu.
21. Spoj u skladu s bilo kojim od patentnih zahtjeva 1 do 19, ili njegova farmaceutski prihvatljiva sol, naznačen time što je namijenjen upotrebi u liječenju poremećaja kojeg se bira između shizofrenije, kognitivnog poremećaja, poremećaja nedostatka pažnje uz hiperaktivnost (ADHD), impulzivnosti, kompulzivnog kockanja, prekomjernog jedenja, poremećaja iz spektra autizma, blagog kognitivnog poremećaja (MCI), staračkog slabljenja kognitivnih funkcija, demencije, sindroma nemirnih nogu (RLS), Parkinsonove bolesti, Huntingtonove koreje, anksioznosti, depresije, velikog depresivnog poremećaja (MDD), depresije otporne na liječenje (TRD), bipolarnmog poremećaja, kronične apatije, anhedonije, kroničnog umora, posttraumatskog stresnog poremećaja, sezsonskog afektivnog poremećaja, poremećaja socijalne anksioznosti, postpartalne depresija, serotoninskog sindroma, zloupotrebe tvari i ovisnosti o narkoticima, recidiva zloupotrebe narkotika, Touretteovog sindroma, tardivne diskinezije, pospanosti, prekomjerne pospanosti po danu, kaheksjie, nedostatka pažnje, spolne disfunkcije, migrene, sistemnog eritematoznog lupusa (SLE), hiperglikemije, ateroskleroze, dislipidemije, pretilosti, dijabetesa, sepse, postishemijeske tubularne nekroze, bubrežne insuficijencije, hiponatriemije, resistentnog edema, narkolepsje, hipertenzije, kongestivne srčane insuficijencije, postoperativne okularne hipotonije, poremećaja spavanja, te boli.
22. Spoj namijenjen upotrebi u skladu s patentnim zahtjevom 21, naznačen time što se poremećaj bira između shizofrenije, kognitivnog poremećaja, blagog kognitivnog poremećaja (MCI), staračkog slabljenja kognitivnih funkcija, demencije, te Parkinsonove bolesti.
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FI3421462T3 (fi) 2023-06-26
TN2015000547A1 (fr) 2017-04-06
KR20160014665A (ko) 2016-02-11
PL3421462T3 (pl) 2023-09-11
US9107923B2 (en) 2015-08-18
CU20150180A7 (es) 2016-05-30

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