HRP20150462T1 - Derivat 1,2,4-triazolona - Google Patents

Derivat 1,2,4-triazolona Download PDF

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HRP20150462T1
HRP20150462T1 HRP20150462TT HRP20150462T HRP20150462T1 HR P20150462 T1 HRP20150462 T1 HR P20150462T1 HR P20150462T T HRP20150462T T HR P20150462TT HR P20150462 T HRP20150462 T HR P20150462T HR P20150462 T1 HRP20150462 T1 HR P20150462T1
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oxo
dihydro
acetamide
ethyl
triazol
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HRP20150462TT
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Takeshi Kuwada
Mitsukane Yoshinaga
Tomoko Ishizaka
Daisuke Wakasugi
Shin-Ichi Shirokawa
Nobutaka Hattori
Youichi Shimazaki
Naoki Miyakoshi
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Taisho Pharmaceutical Co., Ltd
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Claims (13)

1. Derivat 1,2,4-triazolona prikazan s Formulom (1A): [image] u Formuli (1A), R1 predstavlja C1-5 alkil proizvoljno supstituiran s jednom do tri skupine odabrane iz skupine koju čine hidroksi, halogeni atomi, cijano, C3-7 cikloalkil, i C1-5 alkoksi; C3-7 cikloalkil, ili 4- do 8-člani zasićeni heterocikal; R2 predstavlja atom vodika ili C1-5 alkil; R3 predstavlja aril ili heteroaril proizvoljno supstituiran s jednom ili dvije skupine odabrane iz skupine koju čine C1-5 alkoksi, C1-5 alkil, halogeni atomi, trifluorometil, trifluorometoksi, cijano, hidroksi, difluorometoksi, i C1-5 alkilsulfonil; R4 i R5 mogu biti isti ili različiti i svaki predstavlja atom vodika, C1-5 alkil proizvoljno supstituiran s jednom do tri skupine odabrane iz skupine koju čine hidroksi, halogeni atomi, cijano, C3-7 cikloalkil, i C1-5 alkoksi; C3-7 cikloalkil, ili 4- do 8-člani zasićeni ili nezasićeni heterocikal koji u prstenu sadrži jedan ili više atoma dušika, kisika, ili sumpora proizvoljno supstituiran s jednom ili dvije skupine odabrane iz skupine koju čine hidroksi, C1-5 alkil, C1-5 alkoksi, halogeni atomi, cijano, C2-5 alkanoil, te trifluorometil; ili R4 i R5 proizvoljno, zajedno sa susjednim dušikovim atomom, tvore 4- do 8-člani zasićeni ili nezasićeni heterocikal koji proizvoljno u prstenu sadrži jedan ili više atoma dušika, kisika, ili sumpora, pored susjednog dušikovog atoma, u prstenu proizvoljno supstituiran s jednom ili dvije skupine odabrane iz skupine koju čine hidroksi, C1-5 alkil proizvoljno supstituiran s jednim ili dva hidroksi; C1-5 alkoksi, halogenim atomima, cijano, C2-5 alkanoil, okso, aminokarbonilom, mono-C1-5 alkilaminokarbonilom, di-C1-5 alkilaminokarbonilom, trifluorometilom, i amino proizvoljno supstituiran s jednom ili dvije skupine odabrane iz skupine koju čine C1-5 alkil i C2-5 alkanoil; i 4- do 8-člani zasićeni ili nezasićeni heterocikal koji proizvoljno ima C1-5 alkilensku skupinu koja unakrsno povezuje dva različita atoma ugljika u prstenu ili tvore 2-oksa-6-azaspiro[3.3]hept-6-il ili 7-oksa-2-azaspiro[3.5]non-2-il; A predstavlja fenilen ili 6-člani heteroarilen proizvoljno supstituiran s jednim ili dvije skupine odabrane od halogenih atoma i C1-5 alkoksi; X predstavlja jednostruku vezu, -O-, ili -NR6-; R6 predstavlja atom vodika, C1-5 alkil, ili C2-5 alkanoil; Ra predstavlja atom vodika ili C1-5 alkil; i n je cijeli broj od 0 do 3, ili farmaceutski prihvatljiva sol derivata 1,2,4-triazolona.
2. Derivat 1,2,4-triazolona ili njegova farmaceutski prihvatljiva sol prema zahtjevu 1 naznačen time da R4 i R5 mogu biti isti ili različiti i svaki predstavlja atom vodika, C1-5 alkil proizvoljno supstituiran s jednom do tri skupine odabrane iz skupine koju čine hidroksi, halogeni atomi, cijano, C3-7 cikloalkil, i C1-5 alkoksi; C3-7 cikloalkil, ili 4- do 8-člani zasićeni ili nezasićeni heterocikal koji u prstenu sadrži jedan ili više atoma dušika, kisika, ili sumpora proizvoljno supstituiran s jednom ili dvije skupine odabrane iz skupine koju čine hidroksi, C1-5 alkil, C1-5 alkoksi, halogeni atomi, cijano, C2-5 alkanoil, i trifluorometil; ili R4 i R5 proizvoljno, zajedno sa susjednim dušikovim atomom, tvore 4- do 8-člani zasićeni ili nezasićeni heterocikal koji proizvoljno u prstenu sadrži jedan ili više atoma dušika, kisika, ili sumpora, pored susjednog dušikovog atoma, proizvoljno supstituiran s jednom ili dvije skupine odabrane iz skupine koju čine hidroksi, C1-5 alkil proizvoljno supstituiran s jednim ili dva hidroksi; C1-5 alkoksi, halogenim atomima, cijano, C2-5 alkanoil, okso, aminokarbonilom, mono-C1-5 alkilaminokarbonilom, di-C1-5 alkilaminokarbonilom, i trifluorometilom, te 4- do 8-članim zasićenim ili nezasićenim heterociklom koji proizvoljno ima C1-5 alkilensku skupinu koja unakrsno povezuje dva različita atoma ugljika u prstenu) ili tvori 2-oksa-6-azaspiro[3.3]hept-6-il; i n je cijeli broj od 1 do 3.
3. Derivat 1,2,4-triazolona ili njegova farmaceutski prihvatljiva sol prema zahtjevu1 naznačen time da R3 predstavlja aril ili heteroaril proizvoljno supstituiran s jednom ili dvije skupine odabrane iz skupine koju čine C1-5 alkoksi, C1-5 alkil, halogeni atomi, trifluorometil, trifluorometoksi, cijano, hidroksi, i difluorometoksi; R4 i R5 mogu biti isti ili različiti i svaki predstavlja atom vodika, C1-5 alkil proizvoljno supstituiran s jednom do tri skupine odabrane iz skupine koju čine hidroksi, halogeni atomi, cijano, C3-7 cikloalkil, i C1-5 alkoksi; C3-7 cikloalkil, ili 4- do 8-člani zasićeni ili nezasićeni heterocikal koji u prstenu sadrži jedan ili više atoma dušika, kisika, ili sumpora proizvoljno supstituiran s jednom ili dvije skupine odabrane iz skupine koju čine hidroksi, C1-5 alkil, C1-5 alkoksi, halogeni atomi, cijano, C2-5 alkanoil, te trifluorometil; ili R4 i R5 proizvoljno, zajedno sa susjednim dušikovim atomom, tvore 4- do 8-člani zasićeni ili nezasićeni heterocikal koji proizvoljno u prstenu sadrži jedan ili više atoma dušika, kisika, ili sumpora, pored susjednog dušikovog atoma, proizvoljno supstituiran s jednom ili dvije skupine odabrane iz skupine koju čine hidroksi; C1-5 alkil proizvoljno supstituiran s jednim ili dva hidroksi; C1-5 alkoksi, halogenim atomima, cijano, C2-5 alkanoil, okso, aminokarbonilom, mono-C1-5 alkilaminokarbonilom, di-C1-5 alkilaminokarbonil, i trifluorometilom, te 4- do 8-članim zasićenim ili nezasićenim heterociklom koji proizvoljno ima C1-5 alkilensku skupinu koja unakrsno povezuje dva različita atoma ugljika u prstenu; ili tvori 2-oksa-6-azaspiro[3.3]hept-6-il; A predstavlja fenilen ili 6-člani heteroarilen; Ra predstavlja atom vodika; i n je cijeli broj od 1 do 3.
4. Derivat 1,2,4-triazolona ili njegova farmaceutski prihvatljiva sol prema bilo kojem zahtjevu od 1 do 3, naznačen time da R1 je C1-5 alkil; R2 je atom vodika; i R3 je fenil ili piridil proizvoljno supstituiran s jednom ili dvije skupine odabrane iz skupine koju čine C1-5 alkil, C1-5 alkoksi, halogeni atomi, cijano, hidroksi, trifluorometil, difluorometoksi, i trifluorometoksi.
5. Derivat 1,2,4-triazolona ili njegova farmaceutski prihvatljiva sol prema bilo kojem zahtjevu od 1 do 4, naznačen time da A je fenilen, piridindiil, ili pirimidindiil proizvoljno supstituiran s jednom ili dvije skupine odabrane od halogenih atoma i C1-5 alkoksi.
6. Derivat 1,2,4-triazolona ili njegova farmaceutski prihvatljiva sol prema bilo kojem zahtjevu od 1 do 4, naznačen time da A je fenilen ili piridindiil proizvoljno supstituiran s jednom ili dvije skupine odabrane od halogenih atoma i C1-5 alkoksi.
7. Derivat 1,2,4-triazolona ili njegova farmaceutski prihvatljiva sol prema zahtjevu 6, naznačen time da A predstavlja bilo koju od Formula (2) do (4): [image]
8. Derivat 1,2,4-triazolona ili njegova farmaceutski prihvatljiva sol prema bilo kojem zahtjevu od 1 do 7, naznačen time da X je jednostruka veza; n je cijeli broj 1; te R4 i R5 proizvoljno, zajedno sa susjednim dušikovim atomom, tvore 4- do 8-člani zasićeni ili nezasićeni heterocikal koji proizvoljno u prstenu sadrži jedan ili više atoma dušika, kisika, ili sumpora, pored susjednog dušikovog atoma, proizvoljno supstituiran s jednom ili dvije skupine odabrane iz skupine koju čine hidroksi, C1-5 alkil proizvoljno supstituiran s jednim ili dva hidroksi; C1-5 alkoksi, halogenim atomima, cijano, C2-5 alkanoil, okso, aminokarbonilom, mono-C1-5 alkilaminokarbonil, di-C1-5 alkilaminokarbonil, i trifluorometil, i 4- do 8-članim zasićenim ili nezasićenim heterociklom koji proizvoljno ima C1-5 alkilensku skupinu koja unakrsno povezuje dva različita atoma ugljika u prstenu; ili tvore 2-oksa-6-azaspiro[3.3]hept-6-il.
9. Derivat 1,2,4-triazolona ili njegova farmaceutski prihvatljiva sol prema bilo kojem zahtjevu od 1 do 8, naznačen time da R4 i R5, zajedno sa susjednim dušikovim atomom, tvore 5- ili 6-člani zasićeni heterocikal koji proizvoljno u prstenu sadrži jedan ili više atoma dušika, kisika, ili sumpora, pored susjednog dušikovog atoma, proizvoljno supstituiran s jednom ili dvije skupine odabrane iz skupine koju čine hidroksi i C1-5 alkil, i 5- ili 6-člani zasićeni heterocikal koji proizvoljno ima C1-5 alkilensku skupinu koja unakrsno povezuje dva različita atoma ugljika u prstenu; ili tvore 2-oksa-6-azaspiro[3.3]hept-6-il.
10. Derivat 1,2,4-triazolona ili njegova farmaceutski prihvatljiva sol prema bilo kojem zahtjevu od 1 do 8, naznačen time da R4 i R5, zajedno sa susjednim dušikovim atomom, tvore 6-člani zasićeni heterocikal koji proizvoljno sadrži jedan ili više atoma kisika, pored susjednog dušikovog atoma, u prstenu proizvoljno supstituiran s jednim ili dva hidroksi, te 6-člani zasićeni heterocikal koji proizvoljno ima C1-5 alkilensku skupinu koja unakrsno povezuje dva različita atoma ugljika u prstenu; ili tvore 2-oksa-6-azaspiro[3.3]hept-6-il.
11. Jedna tvar, ili smjesa dvije ili više tvari naznačena time da su odabrane iz skupine koja sadrži slijedeće spojeve i njihove farmaceutski prihvatljive soli prema zahtjevu 1: 2-[3-(3-klorofenil)-1-{4-[2-(morfolin-4-il)etil]fenil}-5-okso-1,5-dihidro-4H-1,2,4-triazol-4-il]-N-(propan-2-il)acetamid, 2-[3-(3-klorofenil)-1-{4-[2-(3-hidroksipirolidin-1-il)etil]fenil}-5-okso-1,5-dihidro-4H-1,2,4-triazol-4-il]-N-(propan-2-il)acetamid, 2-[3-(3-klorofenil)-1-(4-{2-[3-(hidroksimetil)pirolidin-1-il]etil}fenil)-5-okso-1,5-dihidro-4H-1,2,4-triazol-4-il]-N-(propan-2-il)acetamid, 2-[3-(3-klorofenil)-1-{4-[2-(3-hidroksi-8-azabiciklo[3.2.1]okt-8-il)etil]fenil -5-okso-1,5-dihidro-4H-1,2,4-triazol-4-il]-N-(propan-2-il)acetamid, 2-[3-(3-klorofenil)-1-{4-[2-(8-oksa-3-azabiciklo[3.2.]okt-3-il)etil]fenil}-5-okso-1,5-dihidro-4H-1,2,4-triazol-4-il]-N-(propan-2-il)acetamid, 2-[3-(3-klorofenil)-1-{4-[2-(3-oksa-8-azabiciklo[3.2.1]okt-8-il)etil]fenil}-5-okso-1,5-dihidro-4H-1,2,4-triazol-4-il]-N-(propan-2-il)acetamid, 2-[3-(3-klorofenil)-5-okso-1-{4-[2-(piperidin-1-il)etil]fenil}-1,5-dihidro-4H-1,2,4-triazol-4-il]-N-(propan-2-il)acetamid, 2-[3-(3-klorofenil)-1-{4-[2-(1,4-oksazepan-4-il)etil]fenil}-5-okso-1,5-dihidro-4H-1,2,4-triazol-4-il]-N-(propan-2-il)acetamid, 2-[3-(3-klorofenil)-1-{5-[2-(morfolin-4-il)etil]piridin-2-il}-5-okso-1,5-dihidro-4H-1,2,4-triazol-4-il]-N-(propan-2-il)acetamid, 2-[3-(3-klorofenil)-1-{5-[2-(3-hidroksi-8-azabiciklo[3.2.1]okt-8-il)etil]piridin-2-il}-5-okso-1,5-dihidro-4H-1,2,4-triazol-4-il]-N-(propan-2-il)acetamid, 2-[3-(3-klorofenil)-1-{5-[2-(3-oksa-8-azabiciklo[3.2.1]okt-8-il)etil]piridin-2-il}-5-okso-1,5-dihidro-4H-1,2,4-triazol-4-il]-N-(propan-2-il)acetamid, 2-[3-(3-klorofenil)-1-{6-[2-(morfolin-4-il)etil]piridin-3-il}-5-okso-1,5-dihidro-4H-1,2,4-triazol-4-il]-N-(propan-2-il)acetamid, N-tert-butil-2-[3-(3-klorofenil)-1-{4-[2-(morfolin-4-il)etil]fenil}-5-okso-1,5-dihidro-4H-1,2,4-triazol-4-il]acetamid, 2-[3-(3-klorofenil)-1-{4-[2-(morfolin-4-il)etil]fenil}-5-okso-1,5-dihidro-4H-1,2,4-triazol-4-il]-N-(1,1,1-trifluoropropan-2-il)acetamid, 2-[3-(3-klorofenil)-1-{4-[2-(morfolin-4-il)etil]fenil}-5-okso-1,5-dihidro-4H-1,2,4-triazol-4-il]-N-(1-hidroksi-2-metilpropan-2-il)acetamid, 2-[3-(3-klorofenil)-1-{4-[2-(morfolin-4-il)etil]fenil}-5-okso-1,5-dihidro-4H-1,2,4-triazol-4-il]-N-ciklobutilacetamid, 2-[3-(3-klorofenil)-1-{4-[2-(morfolin-4-il)etil]fenil}-5-okso-1,5-dihidro-4H-1,2,4-triazol-4-il]-N-(oksetan-3-il)acetamid, 2-[3-(3-klorofenil)-1-{4-[2-(morfolin-4-il)etil]fenil}-5-okso-1,5-dihidro-4H-1,2,4-triazol-4-il]-N-(ciklopropilmetil)acetamid, 2-[3-(3-metoksifenil)-1-{4-[2-(morfolin-4-il)etil]fenil}-5-okso-1,5-dihidro-4H-1,2,4-triazol-4-il]-N-(propan-2-il)acetamid, 2-[3-(4-fluoro-3-metoksifenil)-5-okso-1-{4-[2-(piperidin-1-il)etil]fenil}-1,5-dihidro-4H-1,2,4-triazol-4-il]-N-(propan-2-il)acetamid, 2-[3-(4-fluoro-3-metoksifenil)-1-{4-[2-(morfolin-4-il)etil]fenil}-5-okso-1,5-dihidro-4H-1,2,4-triazol-4-il]-N-(propan-2-il)acetamid, 2-[3-(4-fluoro-3-metoksifenil)-1-{4-[2-(3-hidroksi-8-azabiciklo[3.2.1]okt-8-il)etil]fenil}-5-okso-1,5-dihidro-4H-1,2,4-triazol-4-il]-N-(propan-2-il)acetamid, 2-[3-(4-fluoro-3-metoksifenil)-1-{4-[2-(3-oksa-8-azabiciklo[3.2.1]okt-8-il)etil]fenil}-5-okso-1,5-dihidro-4H-1,2,4-triazol-4-il]-N-(propan-2-il)acetamid, 2-[3-(4-fluoro-3-metoksifenil)-1-{5-[2-(morfolin-4-il)etil]piridin-2-il-5-okso-1,5-dihidro-4H-1,2,4-triazol-4-il]-N-(propan-2-il)acetamid, 2-[3-(4-fluoro-3-metoksifenil)-1-{5-[2-(3-hidroksi-8-azabiciklo[3.2.1]okt-8-il)etil]piridin-2-il}-5-okso-1,5-dihidro-4H-1,2,4-triazol-4-il]-N-(propan-2-il)acetamid, 2-[3-(4-fluoro-3-metoksifenil)-1-{5-[2-(3-oksa-8-azabiciklo[3.2.1]okt-8-il)etil]piridin-2-il}-5-okso-1,5-dihidro-4H-1,2,4-triazol-4-il]-N-(propan-2-il)acetamid, 2-[3-(3-kloro-4-fluorofenil)-5-okso-1-{4-[2-(piperidin-1-il)etil]fenil}-1,5-dihidro-4H-1,2,4-triazol-4-il]-N-(propan-2-il)acetamid, 2-[3-(3-kloro-4-fluorofenil)-1-{4-[2-(morfolin-4-il)etil]fenil}-5-okso-1,5-dihidro-4H-1,2,4-triazol-4-il]-N-(propan-2-il)acetamid, 2-[3-(3-kloro-4-fluorofenil)-1-{4-[2-(2-oksa-6-azaspiro[3.3]hept-6-il)etil]fenil}-5-okso-1,5-dihidro-4H-1,2,4-triazol-4-il]-N-(propan-2-il)acetamid, 2-[3-(3-kloro-4-fluorofenil)-1-{4-[2-(1,4-oksazepan-4-il)etil]fenil}-5-okso-1,5-dihidro-4H-1,2,4-triazol-4-il]-N-(propan-2-il)acetamid, 2-[3-(3-kloro-4-fluorofenil)-1-{4-[2-(3-oksa-8-azabiciklo[3.2.]okt-8-il)etil]fenil}-5-okso-1,5-dihidro-4H-1,2,4-triazol-4-il]-N-(propan-2-il)acetamid, 2-[3-(3-kloro-4-fluorofenil)-1-{4-[2-(3-hidroksi-8-azabiciklo[3.2.1]okt-8-il)etil]fenil}-5-okso-1,5-dihidro-4H-1,2,4-triazol-4-il]-N-(propan-2-il)acetamid, 2-[3-(3-kloro-4-fluorofenil)-5-okso-1-{5-[2-(piperidin-1-il)etil]piridin-2-il}-1,5-dihidro-4H-1,2,4-triazol-4-il]-N-(propan-2-il)acetamid, 2-[3-(3-kloro-4-fluorofenil)-1-{5-[2-(morfolin-4-il)etil]piridin-2-il}-5-okso-1,5-dihidro-4H-1,2,4-triazol-4-il]-N-(propan-2-il)acetamid, 2-[3-(3-kloro-4-fluorofenil)-1-{5-[2-(2-oksa-6-azaspiro[3.3]hept-6-il)etil]piridin-2-il}-5-okso-1,5-dihidro-4H-1,2,4-triazol-4-il]-N-(propan-2-il)acetamid, 2-[3-(3-kloro-4-fluorofenil)-1-{5-[2-(3-oksa-8-azabiciklo[3.2.1]okt-8-il)etil]piridin-2-il}-5-okso-1,5-dihidro-4H-1,2,4-triazol-4-il]-N-(propan-2-il)acetamid, 2-[3-(3-cijanofenil)-1-{4-[2-(morfolin-4-il)etil]fenil}-5-okso-1,5-dihidro-4H-1,2,4-triazol-4-il]-N-(propan-2-il)acetamid, 2-[3-(3-fluorofenil)-1-{4-[2-(morfolin-4-il)etil]fenil}-5-okso-1,5-dihidro-4H-1,2,4-triazol-4-il]-N-(propan-2-il)acetamid, 2-(1-{4-[2-(morfolin-4-il)etil]fenil}-5-okso-3-fenil-1,5-dihidro-4H-1,2,4-triazol-4-il)-N-(propan-2-il)acetamid, 2-[3-(3-klorofenil)-1-{3-fluoro-4-[2-(morfolin-4-il)etil]fenil}-5-okso-1,5-dihidro-4H-1,2,4-triazol-4-il]-N-(propan-2-il)acetamid, 2-[3-(3-klorofenil)-1-{3-fluoro-4-[2-(3-oksa-8-azabiciklo[3.2.]okt-8-il)etil]fenil}-5-okso-1,5-dihidro-4H-1,2,4-triazol-4-il]-N-(propan-2-il)acetamid, 2-[3-(3-klorofenil)-1-{3-metoksi-4-[2-(morfolin-4-il)etil]fenil}-5-okso-1,5-dihidro-4H-1,2,4-triazol-4-il]-N-(propan-2-il)acetamid, 2-[3-(3-klorofenil)-1-{3-metoksi-4-[2-(3-oksa-8-azabiciklo[3.2.1]okt-8-il)etil]fenil}-5-okso-1,5-dihidro-4H-1,2,4-triazol-4-il]-N-(propan-2-il)acetamid, 2-[3-(3-klorofenil)-1-{4-[2-(morfolin-4-il)propil]fenil}-5-okso-1,5-dihidro-4H-1,2,4-triazol-4-il]-N-(propan-2-il)acetamid, 2-[3-(3-klorofenil)-1-{4-[2-(3-oksa-8-azabiciklo[3.2.1]okt-8-il)propil]fenil}-5-okso-1,5-dihidro-4H-1,2,4-triazol-4-il]-N-(propan-2-il)acetamid, 2-[3-(3-klorofenil)-1-{5-[2-(morfolin-4-il)propil]piridin-2-il}-5-okso-1,5-dihidro-4H-1,2,4-triazol-4-il]-N-(propan-2-il)acetamid, 2-[3-(3-klorofenil)-1-{5-[2-(3-oksa-8-azabiciklo[3.2.]okt-8-il)propil]piridin-2-il}-5-okso-1,5-dihidro-4H-1,2,4-triazol-4-il]-N-(propan-2-il)acetamid, N-tert-butil-2-[3-(3-klorofenil)-1-{5-[2-(morfolin-4-il)etil]piridin-2-il}-5-okso-1,5-dihidro-4H-1,2,4-triazol-4-il]acetamid, N-tert-butil-2-[3-(3-klorofenil)-1-{5-[2-(3-oksa-8-azabiciklo[3.2.1]okt-8-il)etil]piridin-2-il}-5-okso-1,5-dihidro-4H-1,2,4-triazol-4-il]acetamid, 2-[3-(3-metoksifenil)-1-{4-[2-(3-oksa-8-azabiciklo[3.2.1]okt-8-il)etil]fenil}-5-okso-1,5-dihidro-4H-1,2,4-triazol-4-il]-N-(propan-2-il)acetamid, N-tert-butil-2-[3-(3-metoksifenil)-1-{5-[2-(morfolin-4-il)etil]piridin-2-il}-5-okso-1,5-dihidro-4H-1,2,4-triazol-4-il]acetamid, N-tert-butil-2-[3-(3-metoksifenil)-1-{5-[2-(3-oksa-8-azabiciklo[3.2.1]okt-8-il)etil]piridin-2-il}-5-okso-1,5-dihidro-4H-1,2,4-triazol-4-il]acetamid, 2-[3-(2-bromo-5-klorofenil)-1-{4-[2-(morfolin-4-il)etil]fenil}-5-okso-1,5-dihidro-4H-1,2,4-triazol-4-il]-N-(propan-2-il)acetamid, 2-(3-[3-(metilsulfonil)fenil]-1-{4-[2-(morfolin-4-il)etil]fenil}-5-okso-1,5-dihidro-4H-1,2,4-triazol-4-il)-N-(propan-2-il)acetamid, 2-[3-(3-klorofenil)-1-{4-[2-(morfolin-4-il)etil]fenil}-5-okso-1,5-dihidro-4H-1,2,4-triazol-4-il]-N-(propan-2-il)acetamid, (+)-2-[3-(3-klorofenil)-1-{5-[2-(3-oksa-8-azabiciklo[3.2.1]okt-8-il)propil]piridin-2-il -5-okso-1,5-dihidro-4H-1,2,4-triazol-4-il]-N-(propan-2-il)acetamid, (-)-2-[3-(3-klorofenil)-1-{5-[2-(3-oksa-8-azabiciklo[3.2.1]okt-8-il)propil]piridin-2-il}-5-okso-1,5-dihidro-4H-1,2,4-triazol-4-il]-N-(propan-2-il)acetamid, 2-[3-(4-fluoro-3-metoksifenil)-1-{4-[2-(3-oksa-8-azabiciklo[3.2.1]okt-8-il)propil]fenil}-5-okso-1,5-dihidro-4H-1,2,4-triazol-4-il]-N-(propan-2-il)acetamid, 2-[3-(4-fluoro-3-metoksifenil)-1-{5-[2-(3-oksa-8-azabiciklo[3.2.1]okt-8-il)propil]piridin-2-il}-5-okso-1,5-dihidro-4H-1,2,4-triazol-4-il]-N-(propan-2-il)acetamid, N-tert-butil-2-[3-(3-metoksifenil)-1-{4-[2-(3-oksa-8-azabiciklo[3.2.1]okt-8-il)propil]fenil}-5-okso-1,5-dihidro-4H-1,2,4-triazol-4-il]acetamid, N-tert-butil-2-[3-(3-metoksifenil)-1-{5-[2-(3-oksa-8-azabiciklo[3.2.1]okt-8-il)propil]piridin-2-il}-5-okso-1,5-dihidro-4H-1,2,4-triazol-4-il]acetamid, 2-[3-(6-metoksipiridin-2-il)-1-{4-[2-(morfolin-4-il)etil]fenil}-5-okso-1,5-dihidro-4H-1,2,4-triazol-4-il]-N-(propan-2-il)acetamid, i 2-[3-(6-metoksipiridin-2-il)-1-{4-[2-(3-oksa-8-azabiciklo[3.2.1]okt-8-il)etil]fenil}-5-okso-1,5-dihidro-4H-1,2,4-triazol-4-il]-N-(propan-2-il)acetamid.
12. Farmaceutski pripravak naznačen time da kao aktivni sastojak sadrži derivat 1,2,4-triazolona ili njegovu farmaceutski prihvatljivu sol prema bilo kojem zahtjevu od 1 do 11.
13. Derivat 1,2,4-triazolona ili njegova farmaceutski prihvatljiva sol prema bilo kojem zahtjevu od 1 do 11 naznačen time da je za uporabu u sprječavanju ili liječenju poremećaja raspoloženja, anksioznosti, shizofrenije, Alzheimerove bolesti, Parkinsonove bolesti, Huntingtonove koreje, poremećaja prehrane, hipertenzije, gastrointestinalne bolesti, ovisnost o drogama, epilepsije, cerebralne infarkcije, cerebralna ishemije, cerebralnog edema, ozljede glave, upale, imunološki povezane bolesti, ili alopecije.
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