HRP20130867T1 - Kondenzirani heterocikliäśki spojevi 2-cijanofenila, te njihovi pripravci i uporaba - Google Patents

Kondenzirani heterocikliäśki spojevi 2-cijanofenila, te njihovi pripravci i uporaba Download PDF

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HRP20130867T1
HRP20130867T1 HRP20130867AT HRP20130867T HRP20130867T1 HR P20130867 T1 HRP20130867 T1 HR P20130867T1 HR P20130867A T HRP20130867A T HR P20130867AT HR P20130867 T HRP20130867 T HR P20130867T HR P20130867 T1 HRP20130867 T1 HR P20130867T1
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pyrido
pyrimidin
dihydro
benzonitrile
methyl
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Zhi-Liang Wei
Matthew Alexander James Duncton
John Kincaid
Michael G. Kelly
Donogh O'mahony
Zhan Wang
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Evotec Ag
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Claims (33)

1. Spoj prema formuli 1: [image] naznačen time da R1 je cikloalkil, cikloheteroalkil, aril ili heteroaril nesupstituiran ili supstituiran sa jednom ili više R4 skupina; ili kada R1 je supstituiran i odabran od kinolinila, izokinolinila, kinoksalina, metilendioksifenila, imidazopiridila, benzoksazolila, i indolila, tada je R1 supstituiran sa Me, Et, Pr, izo-Pr, Ph, Cl, F, Br, CN, OH, OMe, OEt, OPh, COPh, CO2Me, CH2-N-morfolino, CH2-N-(4-Me-piperidino), NH2, CONH2, CF3, CHF2, OCF3, OCHF2, t-Bu, SMe, CH=CH-CO2H, SOMe, SO2Me, SO2CF3, SO2NH2, SO3H, SO3Me, ciklopropilom; ili kada R1 je [image] tada je indeks n' odabran od 1-5 i svaki R5 je neovisno odabran iz skupine koja sadrži vodik, supstituiran ili nesupstituiran alkil, supstituiran ili nesupstituiran acil, supstituiran ili nesupstituiran acilamino, supstituiran ili nesupstituiran alkilamino, supstituiran ili nesupstituiran alkiltio, supstituiran ili nesupstituiran alkoksi, ariloksi, alkoksikarbonil, supstituiran alkoksikarbonil, supstituiran ili nesupstituiran alkilarilamino, arilalkiloksi, supstituiran arilalkiloksi, amino, aril, supstituiran aril, arilalkil, sulfo, supstituiran sulfo, supstituiran sulfonil, supstituiran sulfinil, supstituiran sulfanil, azido, supstituiran ili nesupstituiran karbamoil, karboksil, cijano, supstituiran ili nesupstituiran cikloalkil, supstituiran ili nesupstituiran cikloheteroalkil, supstituiran ili nesupstituiran dialkilamino, halo, heteroariloksi, supstituiran ili nesupstituiran heteroaril, supstituiran ili nesupstituiran heteroalkil, hidroksi, nitro, i tiol; R2 je H, supstituiran ili nesupstituiran C1-C6 alkil ili cikloalkil; svaki R3 i R4 je neovisno odabran iz skupine koja sadrži H, alkil, acil, acilamino, alkilamino, alkiltio, alkoksi, alkoksikarbonil, alkilarilamino, arilalkiloksi, amino, aril, arilalkil, sulfo, supstituiran sulfo, supstituiran sulfonil, supstituiran sulfinil, supstituiran sulfanil, azido, karbamoil, karboksil, cijano, cikloalkil, cikloheteroalkil, dialkilamino, halo, heteroariloksi, heteroaril, heteroalkil, hidroksi, nitro, i tiol; m je 1, 2, 3 ili 4; ili R3 je supstituiran alkil; ili farmaceutski prihvatljiva sol, solvat, tautomer ili njihova izotopna varijanta.
2. Spoj prema formuli 2: [image] naznačen time da R1, R2 i R4, R5 su kao u zahtjevu 1; i R3 je halo, supstituiran ili nesupstituiran C1-C6 alkil ili cikloalkil; ili farmaceutski prihvatljiva sol, solvat, tautomer ili njihova izotopna varijanta.
3. Enantiomerno čist spoj prema zahtjevu 2 prema formuli 3a ili 3b: [image] naznačen time da R1, R2 i R4, R5 su kao u zahtjevu 1; i R3 je halo, supstituiran ili nesupstituiran C1-C6 alkil ili cikloalkil; ili farmaceutski prihvatljiva sol, solvat, tautomer ili njihova izotopna varijanta.
4. Spoj prema bilo kojem zahtjevu od 1-3, naznačen time da R1 je supstituiran ili nesupstituiran aril ili heteroaril.
5. Spoj prema bilo kojem zahtjevu od 1-3, naznačen time da R1 je supstituiran ili nesupstituiran bicikloaril, bicikloalkil, ili bicikloheteroaril.
6. Spoj prema bilo kojem zahtjevu od 1-3, naznačen time da R1 je nesupstituiran fenil, piridil ili pirimidinil.
7. Spoj prema bilo kojem zahtjevu od 1-3, naznačen time da R1 je odabran od nesupstituiranog kinolinila, izokinolinila, kinoksalina, metilendioksifenila, imidazopiridila, benzoksazolila, te indolila.
8. Spoj prema bilo kojem zahtjevu od 1-3, naznačen time da R1 je odabran od kinolinila, izokinolinila, kinoksalina, metilendioksifenila, imidazopiridila, benzoksazolila, i indolila, supstituiranih sa Me, Et, Pr, izo-Pr, Ph, Cl, F, Br, CN, OH, OMe, OEt, OPh, COPh, CO2Me, CH2-N-morfolino, CH2-N-(4-Me-piperidino), NH2, CONH2, CF3, CHF2, OCF3, OCHF2, t-Bu, SMe, CH=CH-CO2H, SOMe, SO2Me, SO2CF3, SO2NH2, SO3H, SO3Me, ciklopropilom.
9. Spoj prema bilo kojem zahtjevu od 1-3, naznačen time da R1 je [image] i pri čemu je indeks n' odabran od 1-5 i svaki R5 je neovisno odabran iz skupine koja sadrži vodik, supstituiran ili nesupstituiran alkil, supstituiran ili nesupstituiran acil, supstituiran ili nesupstituiran acilamino, supstituiran ili nesupstituiran alkilamino, supstituiran ili nesupstituiran alkiltio, supstituiran ili nesupstituiran alkoksi, ariloksi, alkoksikarbonil, supstituiran alkoksikarbonil, supstituiran ili nesupstituiran alkilarilamino, arilalkiloksi, supstituiran arilalkiloksi, amino, aril, supstituiran aril, arilalkil, sulfo, supstituiran sulfo, supstituiran sulfonil, supstituiran sulfinil, supstituiran sulfanil, azido, supstituiran ili nesupstituiran karbamoil, karboksil, cijano, supstituiran ili nesupstituiran cikloalkil, supstituiran ili nesupstituiran cikloheteroalkil, supstituiran ili nesupstituiran dialkilamino, halo, heteroariloksi, supstituiran ili nesupstituiran heteroaril, supstituiran ili nesupstituiran heteroalkil, hidroksi, nitro, i tiol.
10. Spoj prema zahtjevu 9, naznačen time da indeks n' je 1, 2 ili 3.
11. Spoj prema zahtjevu 9, naznačen time da indeks n' je 1 ili 2.
12. Spoj prema bilo kojem zahtjevu od 9-11, naznačen time da svaki R5 je neovisno odabran od H, Me, Et, Pr, izo-Pr, Ph, Cl, F, Br, CN, OH, OMe, OEt, OPh, COPh, CO2Me, CH2-N-morfolino, CH2-N-(4-Me-piperidino), NH2, CONH2, CF3, CHF2, OCF3, OCHF2, t-Bu, SMe, CH=CH-CO2H, SOMe, SO2Me, SO2CF3, SO2NH2, SO3H, SO3Me, ciklopropila, triazolila, morfolinila, i piridila.
13. Spoj prema zahtjevu 1, naznačen time da spoj je prema formuli 4a, 4b, ili 4c: [image] i pri čemu R2 je kao u zahtjevu 1; R3 je kao u zahtjevu 2; i R5 kao u zahtjevu 9.
14. Spoj prema bilo kojem zahtjevu od 9-13, naznačen time da svaki R5 je neovisno odabran od H, Me, Et, Pr, izo-Pr, Ph, Cl, F, CN, OH, OMe, OEt, OPh, CF3, CHF2, OCF3, OCHF2, t-Bu, SO2Me, SO2CF3, i SO3Me.
15. Spoj prema bilo kojem zahtjevu od 9-13, naznačen time da R5 je H, Cl, F, Me, CF3, ili OMe.
16. Spoj prema bilo kojem zahtjevu od 1-15, naznačen time da R2 je odabran od H, Me, Et, n-Pr, t-Bu, CF3, CH2OH, CH2CH2OH, CH2CH2OAc, CH2(CH2)2OH, CH2CH2NHMe, CH2NMe2, CH2CH2NMe2, CH2CONH2, CH2CONMe2, CH2COOH, CH2CH2COOH, CH2(CH2)2COOH, CH2OMe, i CH2CH2OMe.
17. Spoj prema bilo kojem zahtjevu od 1-15, naznačen time da R2 je odabran od CH2NR2'R2", CH2CH2NR2'R2", i CH2CH2CH2NR2'R2"; i pri čemu R2' i R2" se mogu spojiti da tvore heterociklički prsten.
18. Spoj prema bilo kojem zahtjevu od 1-15, naznačen time da je R2 odabran od ciklopropila, ciklobutila ili cikloheksila.
19. Spoj prema bilo kojem zahtjevu od 1-15, naznačen time da R2 je Me.
20. Spoj prema bilo kojem zahtjevu od 1-15, naznačen time da R2 je CH2OH ili CH2CH2OH.
21. Spoj prema bilo kojem zahtjevu od 1-20, naznačen time da je R3 supstituiran ili nesupstituiran alkil.
22. Spoj prema bilo kojem zahtjevu od 1-20, naznačen time da R3 je Me ili CF3.
23. Spoj prema bilo kojem zahtjevu od 1-20, naznačen time da R3 je halo.
24. Spoj prema bilo kojem zahtjevu od 1-20, naznačen time da R3 je Cl.
25. Spoj prema zahtjevu 1, naznačen time da spoj je prema formuli 5a, 5b, ili 5c: [image] i pri čemu R2 je kao u zahtjevu 1; i R5 kao u zahtjevu 9.
26. Spoj prema zahtjevu 25, naznačen time da R2 je H, Me, Et, CH2OH, ili CH2CH2OH.
27. Spoj prema zahtjevu 25, naznačen time da R5 je H, Cl, F, Me, CF3, ili OMe.
28. Spoj prema zahtjevu 1, naznačen time da je odabran iz skupine koja sadrži: 5-Metil-2-{4-[(6-trifluorometil-piridin-3-ilmetil)-amino]-7,8-dihidro-5H-pirido[4,3-d]pirimidin-6-il}-benzonitril; 5-Bromo-2-{4-[(6-trifluorometil-piridin-3-ilmetil)-amino]-7,8-dihidro-5H-pirido[4,3-d]pirimidin-6-il -benzonitril; 5-Ciklopropil-2-{4-[(6-trifluorometil-piridin-3-ilmetil)-amino]-7,8-dihidro-5H-pirido[4,3-d]pirimidin-6-il}-benzonitril; 5-Kloro-2-{4-[(6-trifluorometil-piridin-3-ilmetil)-amino]-7,8-dihidro-5H-pirido[4,3-d]pirimidin-6-il}-benzonitril; 5-Trifluorometil-2-{4-[(6-trifluorometil-piridin-3-ilmetil)-amino]-7,8-dihidro-5H-pirido[4,3-d]pirimidin-6-il}-benzonitril; 5-Bromo-2-{4-[(R)-1-(6-trifluorometil-piridin-3-il)-etilamino]-7,8-dihidro-5H-pirido[4,3-d]pirimidin-6-il}-benzonitril; 5-Metil-2-{4-[(R)-1-(6-trifluorometil-piridin-3-il)-etilamino]-7,8-dihidro-5H-pirido[4,3-d]pirimidin-6-il}-benzonitril; 5-Kloro-2-{4-[(R)-1-(6-trifluorometil-piridin-3-il)-etilamino]-7,8-dihidro-5H-pirido[4,3-d]pirimidin-6-il}-benzonitril; 5-Fluoro-2-{4-[(6-trifluorometil-piridin-3-ilmetil)-amino]-7,8-dihidro-5H-pirido[4,3-d]pirimidin-6-il}-benzonitril; 2-{4-[(6-Trifluorometil-piridin-3-ilmetil)-amino]-7,8-dihidro-5H-pirido[4,3-d]pirimidin-6-il}-benzonitril; 5-Kloro-2-{4-[(2-metil-6-trifluorometil-piridin-3-ilmetil)-amino]-7,8-dihidro-5H-pirido[4,3-d]pirimidin-6-il}-benzonitril; 5-Kloro-2-{4-[(6-dimetilamino-piridin-3-ilmetil)-amino]-7,8-dihidro-5H-pirido[4,3-d]pirimidin-6-il}-benzonitril; 5-Kloro-2-{4-[(6-metoksi-piridin-3-ilmetil)-amino]-7,8-dihidro-5H-pirido[4,3-d]pirimidin-6-il}-benzonitril; 5-Bromo-2-{4-[(6-metoksi-piridin-3-ilmetil)-amino]-7,8-dihidro-5H-pirido[4,3-d]pirimidin-6-il}-benzonitril; 2-{4-[(6-Metoksi-piridin-3-ilmetil)-amino]-7,8-dihidro-5H-pirido[4,3-d]pirimidin-6-il}-5-metil-benzonitril; 5-Kloro-2-{4-[(3-kloro-5-trifluorometil-piridin-2-ilmetil)-amino]-7,8-dihidro-5H-pirido[4,3-d]pirimidin-6-il}-benzonitril; 5-Kloro-2-{4-[(5-trifluorometil-piridin-2-ilmetil)-amino]-7,8-dihidro-5H-pirido[4,3-d]pirimidin-6-il}-benzonitril; tert-butil ester (R)-3-[6-(4-Kloro-2-cijano-fenil)-5,6,7,8-tetrahidro-pirido[4,3-d]pirimidin-4-ilamino]-3-(6-metoksi-piridin-3-il)-propionske kiseline; (R)-3-[6-(4-Kloro-2-cijano-fenil)-5,6,7,8-tetrahidro-pirido[4,3-d]pirimidin-4-ilamino]-3-(6-metoksi-piridin-3-il)-propionska kiselina; 5-Kloro-2-{4-[(R)-3-hidroksi-1-(6-trifluorometil-piridin-3-il)-propilamino]-7,8-dihidro-5H-pirido[4,3-d]pirimidin-6-il}-benzonitril; 2- {4-[(R)-3-Hidroksi-1-(6-metil-piridin-3-il)-propilamino]-7,8-dihidro-5H-pirido[4,3-d]pirimidin-6-il}-5-metil-benzonitril; 2- {4-[(R)-1-(6-Difluorometil-piridin-3-il)-3-hidroksi-propilamino]-7,8-dihidro-5H-pirido[4,3-d]pirimidin-6-il}-5-metil-benzonitril; 2-{4-[(S)-2-Hidroksi-1-(6-metoksi-piridin-3-il)-etilamino]-7,8-dihidro-5H-pirido[4,3-d]pirinfdin-6-il}-5-metil-benzonitril; 2-{4-[(R)-3-Hidroksi-1-(6-metoksi-piridin-3-il)-propilamino]-7,8-dihidro-5H-pirido[4,3-d]pirimidin-6-il}-5-metil-benzonitril; 2-{4-[3-Hidroksi-1-(6-trifluorometil-piridin-3-il)-propilamino]-7,8-dihidro-5H-pirido[4,3-d]pirimidin-6-il}-5-metil-benzonitril; 2-{4-[(S)-2-Metoksi-1-(6-metoksi-piridin-3-il)-etilamino]-7,8-dihidro-5H-pirido[4,3-d]pirimidin-6-il}-5-metil-benzonitril; 2-{4-[(6-Kloro-piridin-3-ilmetil)-amino]-7,8-dihidro-5H-pirido[4,3-d]pirimidin-6-il}-5-metil-benzonitril; 2- {4-[(5-Kloro-piridin-2-ilmetil)-amino]-7,8-dihidro-5H-pirido[4,3-d]pirimidin-6-il}-5-metil-benzonitril; 5-Metil-2-{4-[(piridin-2-ilmetil)-amino]-7,8-dihidro-5H-pirido[4,3-d]pirimidin-6-il}-benzonitril; 2-{4-[(5-Ciklopropil-piridin-2-ilmetil)-amino]-7,8-dihidro-5H-pirido[4,3-d]pirimidin-6-il}-5-metil-benzonitril; 2-{4-[(4-Amino-2-metil-pirimidin-5-ilmetil)-amino]-7,8-dihidro-5H-pirido[4,3-d]pirimidin-6-il}-5-metil-benzonitril; 2-{4-[(3,5-Dikloro-piridin-2-ilmetil)-amino]-7,8-dihidro-5H-pirido[4,3-d]pirimidin-6-il}-5-metil-benzonitril; 2-{4-[(6-Etil-piridin-3-ilmetil)-amino]-7,8-dihidro-5H-pirido[4,3-d]pirimidin-6-il}-5-metil-benzonitril; 5-Kloro-2-{4-[(R)-3-hidroksi-1-(6-metoksi-piridin-3-il)-propilamino]-7,8-dihidro-5H-pirido[4,3-d]pirimidin-6-il}-benzonitril; 5-Kloro-2-{4-[(S)-2-hidroksi-1-(6-metoksi-piridin-3-il)-etilamino]-7,8-dihidro-5H-pirido[4,3-d]pirimidin-6-il}-benzonitril; 2-[4-(3-Cijano-benzilamino)-7,8-dihidro-5H-pirido[4,3-d]pirimidin-6-il]-5-metilbenzonitril; 2-{4-[(Imidazo[1,2-a]piridin-7-ilmetil)-amino]-7,8-dihidro-5H-pirido[4,3-d]pirimidin-6-il}-5-metil-benzonitril; 2-{4-[(Benzooksazol-5-ilmetil)-amino]-7,8-dihidro-5H-pirido[4,3-d]pirimidin-6-il}-5-metil-benzonitril; 5-Metil-2-{4-[(2-metil-pirimidin-5-ilmetil)-amino]-7,8-dihidro-5H-pirido[4,3-d]pirimidin-6-il}-benzonitril; 5-Metil-2-[4-(4-metil-3-[1,2,4]triazol-1-il-benzilamino)-7,8-dihidro-5H-pirido[4,3-d]pirimidin-6-il]-benzonitril; (R)-3-[6-(2-Cijano-4-metil-fenil)-5,6,7,8-tetrahidro-pirido[4,3-d]pirimidin-4-ilamino]-3-(6-metoksi-piridin-3-il)-propionska kiselina; (R)-3-[6-(2-Cijano-4-metil-fenil)-5,6,7,8-tetrahidro-pirido[4,3d]pirimidin-4-ilamino]-3-(6-metoksi-piridin-3-il)-propionamid; (R)-3-[6-(2-Cijano-4-metil-fenil)-5,6,7,8-tetrahidro-pirido[4,3-d]pirimidin-4-ilamino]-3-(6-metoksi-piridin-3-il)-N,N-dimetil-propionamid; 5-Kloro-2-{4-[(imidazo[1,2-a]piridin-7-ilmetil)-amino]-7,8-dihidro-5H-pirido[4,3-d]pirimidin-6-il}-benzonitril; 5-Kloro-2-{4-[(2-metil-pirimidin-5-ilmetil)-amino]-7,8-dihidro-5H-pirido[4,3-d]pirimidin-6-il}-benzonitril; 2-{4-[(S)-2-Hidroksi-1-(6-trifluorometil-piridin-3-il)-etilamino]-7,8-dihidro-5H-pirido[4,3-d]pirimidin-6-il}-5-metil-benzonitril; 5-Kloro-2-{4-[(S)-2-hidroksi-1-(6-trifluorometil-piridin-3-il)-etilamino]-7,8-dihidro-5H-pirido[4,3-d]pirimidin-6-il}-benzonitril; 2-[4-(3-Fluoro-4-metil-benzilamino)-7,8-dihidro-5H-pirido[4,3-d]pirimidin-6-il]-5-metil-benzonitril; 5-Metil-2-[4-(4-metil-3-metilsulfanil-benzilamino)-7,8-dihidro-5H-pirido[4,3-d]pirimidin-6-il]-benzonitril; 2-[4-(4-Kloro-3-[1,2,4]triazol-4-il-benzilamino)-7,8-dihidro-5H-pirido[4,3-d]pirimidin-6-il]-5-metil-benzonitril; 5-Kloro-2-[4-(3-[1,2,4]triazol-4-il-benzilamino)-7,8-dihidro-5H-pirido[4,3-d]pirimidin-6-il]-benzonitril; 5-Kloro-2-[4-(4-kloro-3-[1,2,4]triazol-4-il-benzilamino)-7,8-dihidro-5H-pirido[4,3-d]pirimidin-6-il]-benzonitril; 5-Metil-2-[4-(3-[1,2,4]triazol-4-il-benzilamino)-7,8-dihidro-5H-pirido[4,3-d]pirimidin-6-il]-benzonitril; 2-{4-[(4-Amino-2-metoksi-pirimidin-5-ilmetil)-amino]-7,8-dihidro-5H-pirido[4,3-d]pirimidin-6-il}-5-metil-benzonitril; 2-[4-(3-Jodo-4-metil-benzilamino)-7,8-dihidro-5H-pirido[4,3-d]pirimidin-6-il]-5-metil-benzonitril; 5-Kloro-2-{4-[(R)-1-(2-metoksi-pirimidin-5-il)-etilamino]-7,8-dihidro-5H-pirido[4,3-d]pirimidin-6-il}-benzonitril; 2-{4-[(R)-1-(2-Metoksi-pirimidin-5-il)-etilamino]-7,8-dihidro-5H-pirido[4,3-d]pirimidin-6-il}-5-metil-benzonitril; 2-[4-(3-Metansulfonil-4-metil-benzilamino)-7,8-dihidro-5H-pirido[4,3-d]pirimidin-6-il]-5-metil-benzonitril; 2-{4-[(S)-2-Hidroksi-1-(2-metoksi-pirimidin-5-il)-etilamino]-7,8-dihidro-5H-pirido[4,3-d]pirimidin-6-il}-5-metil-benzonitril; 2-{4-[(2-Izopropil-pirimidin-5-ilmetil)-amino]-7,8-dihidro-5H-pirido[4,3-d]pirimidin-6-il}-5-metil-benzonitril; 5-Kloro-2-{4-[(R)-1-(6-difluorometil-piridin-3-il)-3-hidroksi-propilamino]-7,8-dihidro-5H-pirido[4,3-d]pirimidin-6-il}-benzonitril; 5-Metil-2-[4-(4-metil-3-morfolin-4-il-benzilamino)-7,8-dihidro-5H-pirido[4,3-d]pirimidin-6-il]-benzonitril; 2-{4-[(R)-3-Hidroksi-1-(6-trifluorometil-piridin-3-il)-propilamino]-7,8-dihidro-5H-pirido[4,3-d]pirimidin-6-il}-5-metil-benzonitril; 2-{4-[(S)-3-Hidroksi-1-(6-trifluorometil-piridin-3-il)-propilamino]-7,8-dihidro-5H-pirido[4,3-d]pirimidin-6-il}-5-metil-benzonitril; 5-Metil-2-{4-[(R)-1-(2-metil-pirimidin-5-il)-etilamino]-7,8-dihidro-5H-pirido[4,3-d]pirimidin-6-il}-benzonitril; 5-Metil-2-{4-[(S)-1-(2-metil-pirimidin-5-il)-etilamino]-7,8-dihidro-5H-pirido[4,3-d]pirimidin-6-il}-benzonitril; 2-{4-[(2-Metoksi-pirimidin-5-ilmetil)-amino]-7,8-dihidro-5H-pirido[4,3-d]pirimidin-6-il}-5-metil-benzonitril; 5-Kloro-2-{4-[(2-metoksi-pirimidin-5-ilmetil)-amino]-7,8-dihidro-5H-pirido[4,3-d]pirimidin-6-il}-benzonitril; 2-{4-[(S)-1-(6-Difluorometil-piridin-3-il)-2-hidroksi-etilamino]-7,8-dihidro-5H-pirido[4,3-d]pirimidin-6-il}-5-metil-benzonitril; 2-[4-(4-Kloro-3-metansulfonil-benzilamino)-7,8-dihidro-5H-pirido[4,3-d]pirimidin-6-il]-5-metil-benzonitril; 5-Kloro-2-{4-[(S)-1-(6-difluorometil-piridin-3-il)-2-hidroksi-etilamino]-7,8-dihidro-5H-pirido[4,3-d]pirimidin-6-il}-benzonitril; 5-Kloro-2-{4-[(S)-2-hidroksi-1-(2-metil-pirimidin-5-il)-etilamino]-7,8-dihidro-5H-pirido[4,3-d]pirimidin-6-il}-benzonitril; 2-{4-[(S)-2-Hidroksi-1-(2-metil-pirimidin-5-il)-etilamino]-7,8-dihidro-5H-pirido[4,3-d]pirimidin-6-il}-5-metil-benzonitril; 5-Kloro-2-{4-[(R)-1-(2-metil-pirimidin-5-il)-etilamino]-7,8-dihidro-5H-pirido[4,3-d]pirimidin-6-il}-benzonitril; 5-Kloro-2-[4-(3-metansulfonil-4-metil-benzilamino)-7,8-dihidro-5H-pirido[4,3-d]pirimidin-6-il]-benzonitril; propil ester (R)-3-[6-(2-cijano-4-metil-fenil)-5,6,7,8-tetrahidro-pirido[4,3-d]pirimidin-4-ilamino]-3-(6-trifluorometil-piridin-3-il) octene kiseline 5-Kloro-2-{4-[(S)-2-hidroksi-1-(2-metoksi-pirimidin-5-il)-etilamino]-7,8-dihidro-5H-pirido[4,3-d]pirimidin-6-il}-benzonitril; 5-Metil-2-{4-[(kinoksalin-6-ilmetil)-amino]-7,8-dihidro-5H-pirido[4,3-d]pirimidin-6-il}-benzonitril; 5-Metil-2-{4-[(kinolin-2-ilmetil)-amino]-7,8-dihidro-5H-pirido[4,3-d]pirimidin-6-il}-benzonitril; 2- {4-[(1H-Indol-6-ilmetil)-amino]-7,8-dihidro-5H-pirido[4,3-d]pirimidin-6-il}-5-metil-benzonitril; 2-{4-[(Benzo[1,3]dioksol-5-ilmetil)-amino]-7,8-dihidro-5H-pirido[4,3-d]pirimidin-6-il}-5-metil-benzonitril; 2-[4-(1-Benzo[1,3]dioksol-5-il-etilamino)-7,8-dihidro-5H-pirido[4,3-d]pirimidin-6-il]-5-metil-benzonitril; 5-Kloro-2-{4-[(kinoksalin-6-ilmetil)-amino]-7,8-dihidro-5H-pirido[4,3-d]pirimidin-6-il}-benzonitril; 5-Metil-2-[4-(1-pirazin-2-il-etilamino)-7,8-dihidro-5H-pirido[4,3-d]pirimidin-6-il]-benzonitril; 5-Metil-2-[4-(1-kinoksalin-6-il-etilamino)-7,8-dihidro-5H-pirido[4,3-d]pirimidin-6-il]-benzonitril; 2-{4-[(S)-1-(2-Metoksi-pirimidin-5-il)-etilamino]-7,8-dihidro-5H-pirido[4,3-d]pirimidin-6-il}-5-metil-benzonitril; 2-{4-[1-(4-Kloro-3-metansulfonil-fenil)-etilamino]-7,8-dihidro-5H-pirido[4,3-d]pirimidin-6-il}-5-metil-benzonitril; 2-[4-((R)-1-Benzo[1,3]dioksol-5-il-etilamino)-7,8-dihidro-5H-pirido[4,3-d]pirimidin-6-il]-5-metil-benzonitril; 2-[4-((S)-1-Benzo[1,3]dioksol-5-il-etilamino)-7,8-dihidro-5H-pirido[4,3-d]pirimidin-6-il]-5-metil-benzonitril; 2-{4-[1-(3-Metansulfonil-4-metil-fenil)-etilamino]-7,8-dihidro-5H-pirido[4,3-d]pirimidin-6-il}-5-metil-benzonitril; 5-Metil-2-{4-[(kinolin-7-ilmetil)-amino]-7,8-dihidro-5H-pirido[4,3-d]pirimidin-6-il}-benzonitril; 2-{4-[(R)-1-(4-Kloro-3-metansulfonil-fenil)-etilamino]-7,8-dihidro-5H-pirido[4,3-d]pirimidin-6-il}-5-metil-benzonitril; 2-{4-[(S)-1-(4-Kloro-3-metansulfonil-fenil)-etilamino]-7,8-dihidro-5H-pirido[4,3-d]pirimidin-6-il}-5-metil-benzonitril; 5-Metil-2-[4-((R)-1-kinoksalin-6-il-etilamino)-7,8-dihidro-5H-pirido[4,3-d]pirimidin-6-il]-benzonitril; i 5-Metil-2-[4-((S)-1-kinoksalin-6-il-etilamino)-7,8-dihidro-5H-pirido[4,3-d]pirimidin-6-il]-benzonitril; ili farmaceutski prihvatljiva sol, solvat, stereoizomer, tautomer ili njihova izotopna varijanta.
29. Farmaceutski pripravak naznačen time da sadrži farmaceutski prihvatljiv nosač i farmaceutski učinkovitu količinu spoja prema bilo kojem zahtjevu od 1-28.
30. Spoj prema bilo kojem zahtjevu od 1-28, naznačen time da je za uporabu kao farmaceutski pripravak.
31. Spoj prema bilo kojem zahtjevu od 1-28, naznačen time da je za uporabu u postupku za liječenja ili sprečavanja bolesti ili stanja odabranog od: boli uključujući akutnu, upalnu i neuropatsku bol, kroničnu bol, zubobolju i glavobolju uključujući migrenu, cluster glavobolje i glavobolje tenzijskog tipa, Parkinsonove bolesti, te multiple skleroze; bolesti i poremećaja koji su posredovani ili rezultiraju sa neuroupalom, traumatskom ozljedom mozga, te encefalitisom; centralno posredovanih neuropsihijatrijskih bolesti i poremećaja, depresivne manije, bipolarne bolesti, anksioznosti, shizofrenije, poremećaja prehrane, poremećaja spavanja i spoznajnih poremećaja; disfunkcije prostate, mokraćnog mjehura i crijeva, urinarne inkontinencije, oklijevanja kod mokrenja, rektalne preosjetljivosti, fekalne inkontinencije, benigne hipertrofije prostate i upalne bolesti crijeva; bolesti i poremećaja dišnog sustava i dišnih puteva, alergijskog rinitisa, astme i reaktivnih bolesti dišnih puteva i kronične opstruktivne plućne bolesti; bolesti i poremećaja koji su posredovani ili rezultiraju sa upalom, artritisom, reumatoidnim artritisom i osteoartritisom, infarktom miokarda, raznih autoimunih bolesti i poremećaja, uveitisa i ateroskleroze, svrbeža/pruritusa, psorijaze; pretilosti; lipidnih poremećaja; raka; krvnog tlaka; stanja ozljeda leđne moždine koja proizlaze iz ili se odnose na disfunkciju imuniteta; te bubrežnih poremećaja.
32. Spoj za uporabu u postupku prema zahtjevu 31, naznačen time da bol je visceralna bol.
33. Spoj za uporabu u postupku prema zahtjevu 32, naznačen time da je visceralna bol povezana sa gastroezofagealnom refluksnom bolesti, sindromom iritabilnog crijeva, upalnom bolesti crijeva, pankreatitisom, ginekološkim ili urološkim poremećajima.
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