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HRP20151260T1 - Supstituirani nikotinamidi kao modulatori kcnq2/3 - Google Patents

Supstituirani nikotinamidi kao modulatori kcnq2/3 Download PDF

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HRP20151260T1
HRP20151260T1 HRP20151260TT HRP20151260T HRP20151260T1 HR P20151260 T1 HRP20151260 T1 HR P20151260T1 HR P20151260T T HRP20151260T T HR P20151260TT HR P20151260 T HRP20151260 T HR P20151260T HR P20151260 T1 HRP20151260 T1 HR P20151260T1
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methyl
pyridine
carboxylic acid
alkyl
fluorophenyl
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Sven KÜHNERT
Beatrix Merla
Gregor Bahrenberg
Wolfgang Schröder
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Grünenthal GmbH
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Claims (14)

1. Supstituirani nikotinamidi s općom formulom (1), [image] naznačeni time da A1 označava CR10R11 ili S; A2 označava CR12R13, C(=O), O, S, S(=O) ili S(=O)2; R1 označava C1-10-alkil ili C2-10-heteroalkil, svaki zasićen ili nezasićen, razgranat ili nerazgranat, nesupstituiran ili jednostruko- ili polisupstituiran; C3-10-cikloalkil ili heterociklil, svaki zasićen ili nezasićen, nesupstituiran ili jednostruko- ili polisupstituiran, aril ili heteroaril, svaki nesupstituiran ili jednostruko- ili polisupstituiran; C3-10-cikloalkil ili heterociklil premošten preko C1-8-alkila ili C2-8-heteroalkila, svaki zasićen ili nezasićen, nesupstituiran ili jednostruko- ili polisupstituiran, gdje alkilni ili heteroalkilni lanac može svaki biti razgranat ili nerazgranat, zasićen ili nezasićen, nesupstituiran, jednostruko- ili polisupstituiran; ili aril ili heteroaril premošten preko C1-8-alkila ili C2-8-heteroalkila, svaki nesupstituiran ili jednostruko- ili polisupstituiran, gdje alkilni ili heteroalkilni lanac može svaki biti razgranat ili nerazgranat, zasićen ili nezasićen, nesupstituiran, jednostruko- ili polisupstituiran; R2, R3 i R4 svaki označava, neovisno jedan od drugoga, H; F; Cl; Br; I; NO2; CF3; CN; OH; OCF3; SH; SCF3; metil; CH2-metil; CH2-OH; C2-6-alkil; O-C1-6-alkil, S-C1-6-alkil, svaki zasićen ili nezasićen, razgranat ili nerazgranat, nesupstituiran ili jednostruko- ili polisupstituiran; C3-7-cikloalkil, zasićen ili nezasićen, razgranat ili nerazgranat, nesupstituiran ili jednostruko- ili polisupstituiran; NRaRb, gdje Ra i Rb, svaki označava, neovisno jedan od drugoga, H ili C1-4-alkil, zasićen ili nezasićen, razgranat ili nerazgranat, nesupstituiran ili jednostruko- ili polisupstituiran, ili Ra i Rb zajedno s atomom dušika koji iste spaja tvore heterociklil, zasićen ili nezasićen, razgranat ili nerazgranat, nesupstituiran ili jednostruko- ili polisupstituiran; R5, R6, R7, R8, R10, R11, R12 i R13 svaki označava, neovisno jedan od drugoga, H; F; Cl; Br; I; NO2; CF3; CN; OH; OCF3; SH; SCF3; C1-10-alkil, C2-10-heteroalkil, O-C1-10-alkil ili S-C1-10-alkil, svaki zasićen ili nezasićen, razgranat ili nerazgranat, nesupstituiran ili jednostruko- ili polisupstituiran; C3-10-cikloalkil, zasićen ili nezasićen, razgranat ili nerazgranat, nesupstituiran ili jednostruko- ili polisupstituiran; pod uvjetom da A2 ne može predstavljati S, S(=O) ili S(=O)2 ako R5, R6, R7 i R8 svaki označava H, i A1 označava S; ili R5 i R6 ili R7 i R8 ili R10 i R11 ili R12 i R13 ili R5 i R11 ili R5 i R13 ili R7 i R13 ili R7 i R11 ili R11 i R13 imaju C3-8-cikloalkil ili heterociklil s tri do osam članova u prstenu, svaki zasićen ili nezasićen, nesupstituiran ili jednostruko- ili polisupstituiran zajedno s atomom ili atomima ugljika koji ih povezuju; gdje relevantni preostali supstituenti R5, R6, R7, R8, R10, R11, R12 i R13 imaju gore navedeno značenje; ili R5 i R7 tvore C3-8-cikloalkil, zasićen ili nezasićen, nesupstituiran ili jednostruko- ili polisupstituiran zajedno s atomom ili atomima ugljika koji ih povezuju; ili heterociklil s tri do osam članova u prstenu, nezasićen, nesupstituiran ili jednostruko- ili polisupstituiran; gdje relevantni preostali supstituenti R6, R8, R10, R11, R12 i R13 imaju gore navedeno značenje; R9 označava C3-10-cikloalkil ili heteroalkil, svaki zasićen ili nezasićen, nesupstituiran ili jednostruko- ili polisupstituiran; aril ili heteroaril, svaki nesupstituiran ili jednostruko- ili polisupstituiran; ili označava CRcRd, gdje Rc i Rd svaki označava, neovisno jedan od drugoga, C1-4-alkil, svaki zasićen ili nezasićen, razgranat ili nerazgranat, nesupstituiran ili jednostruko- ili polisupstituiran; pod uvjetom da se vezanje heteroarila ili heterociklila ostvaruje preko ugljikovoga atoma u heteroarilu ili heterociklilu gdje A2 označava O ili S, i R9 označavaju heterociklil, zasićen ili nezasićen, nesupstituiran ili jednostruko- ili polisupstituiran; ili heteroaril, nesupstituiran ili jednostruko- ili polisupstituiran; pri čemu "alkil supstituiran", "heteroalkil supstituiran", "heterociklil supstituiran" i "cikloalkil supstituiran" označava supstituciju jednog ili više vodikovih atoma, svaki neovisno jedan od drugog, s F; Cl; Br; I; NO2; CF3; CN; =O; C1-8-alkilom; C2-8-heteroalkilom; arilom; heteroarilom, C3-10-cikloalkilom; heterociklilom; arilom, heteroarilom, C3-10-cikloalkilom ili heterociklilom premoštenim preko C1-8-alkila ili C2-8-heteroalkila; CHO; C(=O)C1-8-alkilom; C(=O)arilom; C(=O)heteroarilom; CO2H; C(=O)O-C1-8-alkilom; C(=O)O=arilom; C(=O)O-heteroarilom; CONH2; C(=O)NH-C1-8-alkilom; C(=O)N(C1-8-alkil)2; C(=O)NH-arilom, C(=O)N(aril)2; C(=O)NH-heteroarilom; C(=O)N(heteroaril)2; C(=O)N(C1-8-alkil)(aril); C(=O)N(C1-8-alkil)(heteroaril); C(=O)N(heteroaril)(aril); OH; O-C1-8-alkilom; OCF3; O-(C1-8-alkil)-OH; O-(C1-8-alkil)-O-C1-8-alkilom; O-benzilom; O-arilom; O-heteroarilom; O-C(=O)C1-8-alkilom; O-C(=O)arilom; O-C(=O)heteroarilom; NH2; NH-C1-8-alkilom; N(C1-8-alkil)2; NH-C(=O)C1-8-alkilom; N(C1-8-alkil)-C(=O)C1-8-alkilom; N(C(=O)C1-8-alkil2; NH-C(=O)-arilom; NH-C(=O)=heteroarilom; SH; S-C1-8-alkilom; SCF3; S-benzilom; S-arilom; S-heteroarilom; S(=O)2C1-8-alkilom; S(=O)2arilom; S(=O)2heteroarilom; S(=O)2OH; S(=O)2O-C1-8-alkilom; S(=O)2O-arilom; S(=O)2O-heteroarilom; S(=O)2-NH-C1-8-alkilom; S(=O)2-NH-arilom; i S(=O)2-NH-C1-8-heteroarilom; pri čemu "aril supstituiran" i "heteroaril supstituiran" označava supstituciju jednog ili više vodikovih atoma, svaki neovisno jedan od drugog, s F; Cl; Br; I; NO2; CF3; CN; C1-8-alkilom; C2-8-heteroalkilom; arilom; heteroarilom; C3-10-cikloalkilom; heterociklilom; arilom, heteroarilom, C3-10-cikloalkilom ili heterociklilom premoštenim preko C1-8-alkila ili C2-8-heteroalkila; CHO; C(=O)C1-8-alkilom; C(=O)arilom; C(=O)heteroarilom; C(=O)O-C1-8-alkilom; C(=O)O=arilom; C(=O)O-heteroarilom; CONH2; C(=O)NH-C1-8-alkilom; C(=O)N(C1-8-alkil)2; C(=O)NH-arilom, C(=O)N(aril)2; C(=O)NH-heteroarilom; C(=O)N(heteroaril)2; C(=O)N(C1-8-alkil)(aril); C(=O)N(C1-8-alkil)(heteroaril); C(=O)N(heteroaril)(aril); OH; O-C1-8-alkilom; OCF3; O-(C1-8-alkil)-OH; O-(C1-8-alkil)-O-C1-8-alkilom; O-benzilom; O-arilom; O-heteroarilom; O-C(=O)C1-8-alkilom; O-C(=O)arilom; O-C(=O)heteroarilom; NH2; NH-C1-8-alkilom; N(C1-8-alkil)2; NH-C(=O)C1-8-alkilom; N(C1-8-alkil)-C(=O)C1-8-alkilom; N(C(=O)C1-8-alkil2; NH-C(=O)-arilom; NH-C(=O)=heteroarilom; SH; S-C1-8-alkilom; SCF3; S-benzilom; S-arilom; S-heteroarilom; S(=O)2C1-8-alkilom; S(=O)2arilom; S(=O)2heteroarilom; S(=O)2OH; S(=O)2O-C1-8-alkilom; S(=O)2O-arilom; S(=O)2O-heteroarilom; S(=O)2-NH-C1-8-alkilom; S(=O)2-NH-arilom; i S(=O)2-NH-C1-8-heteroarilom; u obliku slobodnih spojeva ili soli fiziološki kompatibilnih kiselina ili baza.
2. Supstituirani nikotinamidi prema zahtjevu 1, naznačeni time da A1 označava S; i A2 označava CR12R13, O, S ili S(=O)2.
3. Supstituirani nikotinamidi prema zahtjevu 1 ili 2, naznačeni time da R1 označava dio strukture (T1) [image] pri čemu R14a i R14b, svaki neovisno jedan od drugog, označavaju H; F; Cl; Br; I; NO2; CF3; CN; OH; OCF3; NH2; C1-4-alkil, O-C1-4-alkil, NH-C1-4-alkil, N(C1-4-alkil)2, svaki zasićen ili nezasićen, razgranat ili nerazgranat, nesupstituiran ili jednostruko- ili polisupstituiran s jednim ili više supstituenata, svaki odabran međusobno neovisno iz skupine koja predstavlja i koja sadrži F, Cl, Br, I, O-C1-4-alkil, OH i OCF3; C3-10-cikloalkil ili heterociklil, svaki zasićen ili nezasićen, nesupstituiran ili jednostruko- ili polisupstituiran s jednim ili više supstituenata, svaki neovisno odabran iz skupine koju čine F, Cl, Br, I, C1-4-alkil, OH, =O, O-C1-4-alkil, OCF3, NH2, NH-C1-4-alkil i N(C1-4-alkil)2; m označava 0, 1, 2 ili 3; Y označava O ili NR15, gdje R15 označava H; C1-4-alkil označava zasićen ili nezasićen, razgranat ili nerazgranat, nesupstituiran ili jednostruko- ili polisupstituiran s jednim ili više supstituenata, svaki neovisno odabran iz skupine koju čine F, Cl, Br, I, C1-4-alkil, OH, O-C1-4-alkil, OCF3, NH2, NH-C1-4-alkil i N(C1-4-alkil)2; ili označava C3-10-cikloalkil, zasićen ili nezasićen, nesupstituiran ili jednostruko- ili polisupstituiran s jednim ili više supstituenata, svaki neovisno odabran iz skupine koju čine F, Cl, Br, I, C1-4-alkil, OH, O-C1-4-alkil, OCF3, NH2, NH-C1-4-alkil i N(C1-4-alkil)2; n označava 0 ili 1, B označava C1-8-alkil, zasićen ili nezasićen, razgranat ili nerazgranat, nesupstituiran ili jednostruko- ili polisupstituiran s jednim ili više supstituenata, svaki neovisno odabran iz skupine koju čine F, Cl, Br, I, NO2, CN, OH, =O, O-C1-4-alkil, OCF3, C(=O)-OH, CF3, NH2, NH(C1-4-alkil), N(C1-4-alkil)2, SH, S-C1-4-alkil, SCF3 i S(=O)2OH; C3-10-cikloalkil ili heterociklil, svaki zasićen ili nezasićen, nesupstituiran ili jednostruko- ili polisupstituiran s jednim ili više supstituenata, svaki neovisno odabran iz skupine koju čine F, Cl, Br, I, NO2, CN, OH, O-C1-8-alkil, OCF3, C1-8-alkil, C(=O)-OH, CF3, NH2, NH(C1-8-alkil), N(C1-8-alkil)2, SH, S-C1-8-alkil, SCF3, S(=O)2OH, benzil, fenil, piridil i tienil, gdje benzil, fenil, piridin, tienil, mogu svaki biti nesupstituirani ili jednostruko- ili polisupstituirani s jednim ili više supstituenata, koji su svaki odabrani neovisno jedan od drugog iz skupine koju čine F, Cl, Br, I, NO2, CN, OH, O-C1-8-alkil, OCF3, C1-8-alkil, C(=O)-OH, CF3, NH2, NH(C1-8-alkil), N(C1-8-alkil)2, SH, S-C1-8-alkil, SCF3 i S(=O)2OH; aril ili heteroaril, svaki nesupstituiran ili jednostruko- ili polisupstituiran s jednim ili više supstituenata, koji su svaki odabrani neovisno jedan od drugog iz skupine koju čine F, Cl, Br, I, NO2, CN, OH, O-C1-8-alkil, OCF3, C1-8-alkil, C(=O)-OH, CF3, NH2, NH(C1-8-alkil), N(C1-8-alkil)2, SH, S-C1-8-alkil, SCF3 i S(=O)2OH, benzil, fenil, piridil i tienil, gdje benzil, fenil, piridil, tienil mogu svaki biti nesupstituirani ili jednostruko- ili polisupstituirani s jednim ili više supstituenata, koji su svaki odabrani neovisno jedan od drugog iz skupine koju čine F, Cl, Br, I, NO2, CN, OH, O-C1-8-alkil, OCF3, C1-8-alkil, C(=O)-OH, CF3, NH2, NH(C1-8-alkil), N(C1-8-alkil)2, SH, S-C1-8-alkil, SCF3 i S(=O)2OH;
4. Supstituirani nikotinamidi prema zahtjevu 3, naznačeni time da R14a i R14b, svaki neovisno jedan od drugog, označavaju H; F; Cl; Br; I; NO2; CF3; CN; metil; etil; n-propil; izo-propil; ciklopropil; n-butil; sek.-butil; tert.-butil; CH2CF3; OH; O-metil; O-etil; O-(CH2)2-O-CH3; O-(CH2)2-OH; OCF3; NH2; NH-metil; N(metil)2; NH-etil; N(etil)2; ili N(metil)(etil); m je 0, 1 ili 2; n je 0; i B označava C1-4-alkil, zasićen, razgranat ili nerazgranat, nesupstituiran ili jednostruko- ili polisupstituiran s jednim ili više supstituenata, svaki neovisno odabran iz skupine koju čine F, Cl, Br, I, OH, O-C1-4-alkil, OCF3 i CF3; C3-10-cikloalkil, zasićen, nesupstituiran; fenil, naftil, piridil, tienil, svaki nesupstituiran ili jednostruko- ili dvostruko- ili trostruko-supstituiran s jednim, dva ili tri supstituenta, svaki neovisno odabran iz skupine koju čine F, Cl, Br, I, NO2, CN, OH, O-C1-4-alkil, OCF3, C1-4-alkil, C(=O)-OH, CF3, NH2, NH(C1-4-alkil), N(C1-4-alkil)2, SH, S-C1-4-alkil, SCF3, S(=O)2OH.
5. Supstituirani nikotinamidi prema jednom od zahtjeva 1-4, naznačeni time da R2, R3 i R4 svaki označavaju, neovisno jedan od drugoga, H; F; Cl; Br; I; NO2; CF3; CN; OH; OCF3; SH; SCF3; metil; CH2-O-metil; CH2-OH; C2-6-alkil; O-C1-6-alkil, S-C1-6-alkil, svaki zasićen ili nezasićen, razgranat ili nerazgranat, nesupstituiran ili jednostruko- ili polisupstituiran s jednim ili više supstituenata odabranih, neovisno jedan od drugoga, iz skupine koja sadrži F, Cl, Br, I, OH, =O i O-C1-4-alkil; C3-7-cikloalkil, zasićen ili nezasićen, razgranat ili nerazgranat, nesupstituiran; NRaRb, gdje Ra i Rb svaki označava, neovisno jedan od drugoga, H ili C1-4-alkil, zasićen ili nezasićen, razgranat ili nerazgranat, nesupstituiran ili jednostruko- ili polisupstituiran s jednim ili više supstituenata odabranih, neovisno jedan od drugoga, iz skupine koja sadrži OH, =O i O-C1-4-alkil, ili Ra i Rb zajedno s atomom dušika koji iste spaja tvore heterociklil, zasićen ili nezasićen, razgranat ili nerazgranat, nesupstituiran ili jednostruko- ili polisupstituiran s C1-4-alkilom.
6. Supstituirani nikotinamidi prema zahtjevu 5, naznačeni time da R2, R3 i R4 svaki označava, neovisno jedan od drugoga, H; F; Cl; Br; I; metil; etil; n-propil; izo-propil; ciklopropil; CN; CF3; O-metil; OCF3; S-metil; SCF3.
7. Supstituirani nikotinamidi prema jednom od zahtjeva 1-6, naznačeni time da R5, R6, R7, R8, R10, R11, R12 i R13 poželjno svaki označava, neovisno jedan od drugoga, H; F; Cl; Br; I; NO2; CF3; CN; OH; OCF3; SH; SCF3; metil; etil; n-propil; izo-propil; n-butil, sek.-butil, tert.-butil, O-metil; O-etil; O-(CH2)2-O-CH3; O-(CH2)2-OH; S-metil; S-etil; ciklopropil, ciklobutil; ciklopentil; cikloheksil; ili R5 i R6 ili R7 i R8 ili R10 i R11 ili R12 i R13 ili R5 i R11 ili R5 i R7 ili R5 i R13 ili R7 i R13 ili R7 i R11 ili R11 i R13 tvore ciklopropil, ciklobutil, ciklopentil ili cikloheksil zajedno s ugljikovim atomom(ima) koje iste spaja, svaki nesupstituiran ili jednostruko- ili polisupstituiran s jednim ili više supstituenata, svaki nesupstituiran; gdje relevantni preostali supstituenti R5, R6, R7, R8, R10, R11, R12 i R13 imaju gore navedeno značenje.
8. Supstituirani nikotinamidi prema jednom od zahtjeva 1-7, naznačeni time da R9 označava C3-10-cikloalkil ili heterociklil, svaki zasićen ili nezasićen, nesupstituiran ili jednostruko- ili polisupstituiran s jednim ili više supstituenata, svaki odabran neovisno jedan od drugog iz skupine koju čine F, Cl, Br, I, NO2, CN, OH, =O, O-C1-4-alkil, OCF3, C1-4-alkil, CF3, SH, S-C1-4-alkil i SCF3; aril ili heteroaril, svaki nesupstituiran ili jednostruko- ili polisupstituiran s jednim ili više supstituenata, koji su svaki odabrani neovisno jedan od drugog iz skupine koju čine F, Cl, Br, I, NO2, CN, OH, O-C1-4-alkil, OCF3, C1-4-alkil, CF3, NH2, NH(C1-4-alkil), N(C1-4-alkil)2, SH, S-C1-4-alkil i SCF3; ili označava CRcRd, gdje Rc i Rd, svaki neovisno jedan od drugog, supstituiraju C1-4-alkil, zasićen ili nezasićen, razgranat ili nerazgranat, nesupstituiran ili jednostruko- ili polisupstituiran s jednim ili više supstituenata, svaki odabran neovisno jedan od drugog iz skupine koju čine F, Cl, Br, I, OH, O-C1-4-alkil, CF3, OCF3 i SCF3.
9. Supstituirani nikotinamidi prema jednom od zahtjeva 1-8, naznačeni time da R9 označava fenil, piridil i tienil, nesupstituiran ili jednostruko- ili polisupstituiran s jednim ili više supstituenata, svaki odabran neovisno jedan od drugog iz skupine koju čine F, Cl, Br, I, CN, OH, O-C1-4-alkil, OCF3, C1-4-alkil, CF3, SH, S-C1-4-alkil i SCF3.
10. Supstituirani nikotinamidi prema jednom od zahtjeva 1-9, naznačeni time da A1 označava S; i A2 označava CR12R13; R1 označava dio strukture (T1-1) [image] gdje R14a i R14b, svaki neovisno jedan od drugog, označavaju H; F; Cl; Br; I; metil; etil; n-propil; izo-propil; n-butil; sek.-butil; tert.-butil; OH; O-metil; O-etil; O-(CH2)2-O-CH3; ili O-(CH2)2-OH; m označava 0, 1 ili 2; B označava metil; etil; n-propil; izo-propil; n-butil; sek.-butil; tert.-butil; ciklopropil; ciklobutil; ciklopentil; cikloheksil; cikloheptil; adamantil; biciklo[2.2.1]heptil; biciklo[2.2.2]oktil; fenil, piridil, tienil, svaki nesupstituiran ili jednostruko-, dvostruko- ili trostruko-supstituiran s jednim, dva ili tri supstituenta, svaki odabran neovisno jedan od drugog iz skupine koju čine F, Cl, Br, I, NO2, CN, OH, O-C1-4-alkil, OCF3, C1-4-alkil, C(=O)-OH, CF3, NH2, NH(C1-4-alkil), N(C1-4-alkil)2, SH, S-C1-4-alkil, SCF3, S(=O)2OH; R2, R3 i R4, svaki neovisno jedan od drugog, označavaju H; F; Cl; metil; etil; CF3 ili O-metil; R5, R6, R7, R8, R10, R11, R12 i R13, svaki neovisno jedan od drugog, označavaju H; F; Cl; metil; etil; n-propil, izo-propil; ciklopropil; R9 označava fenil, piridil i tienil, nesupstituiran ili jednostruko- ili polisupstituiran s jednim ili više supstituenata, svaki odabran neovisno jedan od drugog iz skupine koju čine F, Cl, Br, I, CN, metil, etil, n-propil, izo-propil, n-butil, sek.-butil, tert.-butil, O-metil, O-etil, O-n-propil, O-izo-propil, O-butil, O-sek.-butil, O-tert.-butil, OH, OCF3, CF3, SH, S-C1-4-alkil i SCF3.
11. Supstituirani nikotinamidi prema jednom od zahtjeva 1-10, naznačeni time da su odabrani iz skupine koju čine 1 amid 2-(3-fenil-propilsulfanil)-N-(tiofen-2-il-metil)-piridin-3-karboksilne kiseline; 2 amid 2-(3-cikloheksil-propilsulfanil)-N-(tiofen-2-il-metil)-piridin-3-karboksilne kiseline; 3 amid 2-[(3-okso-fenil-propil)sulfanil]-N-(tiofen-2-il-metil)-piridin-3-karboksilne kiseline; 4 amid N-(tiofen-2-il-metil)-2-[2-[3-(trifluorometil)-fenoksi]-etilsulfanil]-piridin-3-karboksilne kiseline; 5 amid 2-(4-metil-pentilsulfanil)-N-(tiofen-2-il-metil)-piridin-3-karboksilne kiseline; 7 amid 2-(4-fenil-butil)-N-(tiofen-2-il-metil)-piridin-3-karboksilne kiseline; 8 amid 2-[(3-benzosulfonil)-propil]- N-(cikloheksil-metil)-piridin-3-karboksilne kiseline; 9 amid N-(cikloheksil-metil)-2-(4-fenil-butil)- piridin-3-karboksilne kiseline; 10 amid 2-[3-benzosulfonil)-propil]-N-(tiofen-2-il-metil)-piridin-3-karboksilne kiseline; 12 amid N-(tiofen-2-il-metil)-2-[3-[[3-(trifluorometil)fenil]sulfonil]-propil]-piridin-3-karboksilne kiseline; 13 amid N-(tiofen-2-il-metil)-2-[3-[[3-(trifluoro-metil)fenil]sulfanil]-propil]-piridin-3-karboksilne kiseline; 16 amid 2-(2-fenilsulfanil-propilsulfanil)-N-(tiofen-2-il-metil)-piridin-3-karboksilne kiseline; 17 amid 2-[3-(4-fluorofenil)-propilsulfanil]-N-(tiofen-2-il-metil)-piridin-3-karboksilne kiseline; 18 amid N-(tiofen-2-il-metil)-2-[3-[3-(trifluorometil)fenil]-propilsulfanil]-piridin-3-karboksilne kiseline; 19 amid 2-[2-[(4-fluorofenil)sulfanil]-propilsulfanil]-N-(tiofen-2-il-metil)-piridin-3-karboksilne kiseline; 20 amid N-(tiofen-2-il-metil)-2-[2-[[3-(trifluorometil)fenil]sulfanil]-propilsulfanil]-piridin-3-karboksilne kiseline; 21 amid N-(tiofen-2-il-metil)-2-[4-[3-(trifluorometil)-fenil]-butil]-piridin-3-karboksilne kiseline; 22 amid 2-[4-(4-fluorofenil)-butil]-N-(tiofen-2-il-metil)-piridin-3-karboksilne kiseline; 23 amid 2-(3-fenilsulfanil-propil)-N-(tiofen-2-il-metil)-piridin-3-karboksilne kiseline; 24 amid 2-[(1-metil-fenilsulfanil-etil)sulfanil]-N-(tiofen-2-il-metil)-piridin-3-karboksilne kiseline; 25 amid N-(cikloheptil-metil)-2-[4-[3-(trifluorometil)fenil]-butil]-piridin-3-karboksilne kiseline; 26 amid N-(5-biciklo[2.2.1]heptanil-metil)-2-[4-[3-(trifluorometil)fenil]-butil]-piridin-3-karboksilne kiseline; 27 amid N-(5-biciklo[2.2.1]heptanil-metil)-2-[3-[3-(trifluorometil)fenil]-propilsulfanil]-piridin-3-karboksilne kiseline; 28 amid N-(5-biciklo[2.2.1]heptanil-metil)-2-(4-metil-pentilsulfanil)-piridin-3-karboksilne kiseline; 29 amid N-(cikloheptil-metil)-2-[3-[(4-fluorofenil)sulfanil]-propil]-piridin-3-karboksilne kiseline; 30 amid N-(5-biciklo[2.2.1]heptanil-metil)-2-[3-[(4-fluorofenil)sulfanil]-propil]-piridin-3-karboksilne kiseline; 31 amid N-(cikloheptil-metil)-2-[3-[[3-(trifluorometil)fenil]sulfonil]-propil]-piridin-3-karboksilne kiseline; 32 amid N-(5-biciklo[2.2.1]heptanil-metil)-2-[3-[[3-(trifluorometil)fenil]sulfonil]-propil]-piridin-3-karboksilne kiseline; 33 amid N-(5-biciklo[2.2.1]heptanil-metil)-2-(3-fenil-propilsulfanil)-piridin-3-karboksilne kiseline; 34 amid N-(5-biciklo[2.2.1]heptanil-metil)-2-[3-[4-(trifluorometil)-fenil]-propilsulfanil]-piridin-3-karboksilne kiseline; 35 amid N-(5-biciklo[2.2.1]heptanil-metil)-2-[3-(4-klorofenil)-propilsulfanil]-piridin-3-karboksilne kiseline; 36 amid N-[(3,5-difluoro-fenil)-metil]-2-[3-(4-fluorofenil)-propilsulfanil]-piridin-3-karboksilne kiseline; 37 amid N-[(5-kloro-tiofen-2-il)-metil]-2-[3-(4-fluorofenil)-propilsulfanil]-piridin-3-karboksilne kiseline; 38 amid N-[(2,2-dimetil-ciklopropil)-metil]-2-[3-(4-fluorofenil)-propilsulfanil]-piridin-3-karboksilne kiseline; 39 amid N-(5-biciklo[2.2.1]heptanil-metil)-2-[3-(3-fluorofenil)-propilsulfanil]-piridin-3-karboksilne kiseline; 40 amid N-(cikloheksil-metil)-2-[3-(4-fluorofenil]-propilsulfanil]-piridin-3-karboksilne kiseline; 41 amid N-(cikloheptil-metil)-2-[3-(4-fluorofenil]-propilsulfanil]-piridin-3-karboksilne kiseline; 43 amid N-(5-biciklo[2.2.1]heptanil-metil)-2-[[3-(4-fluorofenil)-3-okso-propil]sulfanil]-piridin-3-karboksilne kiseline; 44 amid N-(5-biciklo[2.2.1]heptanil-metil)-2-[(3-okso-fenil-propil)sulfanil]-piridin-3-karboksilne kiseline; 45 amid N-(5-biciklo[2.2.1]heptanil-metil)-2-(heksilsulfanil)-piridin-3-karboksilne kiseline; 46 amid N-(5-biciklo[2.2.1]heptanil-metil)-2-(2-fenoksi-etilsulfanil)-piridin-3-karboksilne kiseline; 47 amid N-(5-biciklo[2.2.1]heptanil-metil)-2-[2-[3-(trifluorometil)-fenoksi]-etilsulfanil]-piridin-3-karboksilne kiseline; 48 amid 2-[3-(4-fluorofenil)-propilsulfanil]-N-(3,3,3-trifluoro-propil)-piridin-3-karboksilne kiseline; 49 amid N-(5-biciklo[2.2.1]heptanil-metil)-2-[2-(4-fluoro-fenoksi)-etilsulfanil]-piridin-3-karboksilne kiseline; 52 amid N-(5-biciklo[2.2.1]heptanil-metil)-2-(3-naftalen-1-il-propilsulfanil)-piridin-3-karboksilne kiseline; 53 amid N-(5-biciklo[2.2.1]heptanil-metil)-2-[3-[3-fluoro-4-(trifluorometil)-fenil]-propilsulfanil]-piridin-3-karboksilne kiseline; 54 amid N-(5-biciklo[2.2.1]heptanil-metil)-2-[3-[4-fluoro-3-(trifluorometil)-fenil]-propilsulfanil]-piridin-3-karboksilne kiseline; 55 amid N-(ciklooktil-metil)-2-[3-(4-fluorofenil)-propilsulfanil]-piridin-3-karboksilne kiseline; 56 amid N-(5-biciklo[2.2.1]heptanil-metil)-2-[3-(4-metoksifenil)-propilsulfanil]-piridin-3-karboksilne kiseline; 57 amid 2-[3-(4-fluorofenil)-propilsulfanil]-N-[(4metoksifenil)-metil]-piridin-3-karboksilne kiseline; 59 amid 2-[3-(4-fluorofenil)-propilsulfanil]-N-[[3-(trifluorometil)fenil]-metil]-piridin-3-karboksilne kiseline; 60 amid N-(5-biciklo[2.2.1]heptanil-metil)-2-[3-(3,4-difluoro-fenil)-propilsulfanil]-piridin-3-karboksilne kiseline; 61 amid N-(5-biciklo[2.2.1]heptanil-metil)-2-[3-(3,5-difluoro-fenil)-propilsulfanil]-piridin-3-karboksilne kiseline; 62 amid N-(5-biciklo[2.2.1]heptanil-metil)-2-[3-(2,4-difluoro-fenil)-propilsulfanil]-piridin-3-karboksilne kiseline; 63 amid N-[(2-fluorofenil)-metil]-2-[3-(4-fluorofenil)-propilsulfanil]- piridin-3-karboksilne kiseline; 64 amid N-[(3-fluorofenil)-metil]-2-[3-(4-fluorofenil)-propilsulfanil]- piridin-3-karboksilne kiseline; 65 amid N-[(4-fluorofenil)-metil]-2-[3-(4-fluorofenil)-propilsulfanil]-piridin-3-karboksilne kiseline; 66 amid N-benzil-2-[3-(4-fluorofenil)-propilsulfanil]-piridin-3-karboksilne kiseline; 67 amid N-(5-biciklo[2.2.1]heptanil-metil)-2-[(1-metil-3-fenil-propil)sulfanil]-piridin-3-karboksilne kiseline; 68 amid N-(5-biciklo[2.2.1]heptanil-metil)-2-[3-(3,4,5-trifluoro-fenil)-propilsulfanil]- piridin-3-karboksilne kiseline; 69 amid N-(5-biciklo[2.2.1]heptanil-metil)-2-[3-[3-fluoro-5-(trifluorometil)-fenil]-propilsulfanil]- piridin-3-karboksilne kiseline; 70 amid N-(5-biciklo[2.2.1]heptanil-metil)-2-[3-(3-metoksifenil)-propilsulfanil]-piridin-3-karboksilne kiseline; 71 amid N-[(3,4-difluoro-fenil)-metil]-2-[3-(4-fluorofenil)-propilsulfanil]-piridin-3-karboksilne kiseline; 72 amid N-(2,3-dihidro-benzofuran-5-il-metil)-2-[3-(4-fluorofenil)-propilsulfanil]-piridin-3-karboksilne kiseline; 73 amid N-(5-biciklo[2.2.1]heptanil-metil)-2-[3-(3-hidroksifenil)-propilsulfanil]-piridin-3-karboksilne kiseline; 74 amid N-(5-biciklo[2.2.1]heptanil-metil)-2-[[3-(4-fluorofenil)-1-metilpropil]sulfanil]-piridin-3-karboksilne kiseline; 75 amid N-(5-biciklo[2.2.1]heptanil-metil)-2-[[3-(4-fluorofenil)-2-metil-propil]sulfanil]- piridin-3-karboksilne kiseline; 76 amid 2-[3-(4-fluorofenil)-propilsulfanil]-N-[(2-metoksifenil)-metil]-piridin-3-karboksilne kiseline; 77 amid 2-[3-(4-fluorofenil)-propilsulfanil]-N-[(3-metoksifenil)-metil]-piridin-3-karboksilne kiseline; 78 amid 2-[3-(4-fluorofenil)-propilsulfanil]-N-fenetil-piridin-3-karboksilne kiseline; 79 amid 2-[3-(4-fluorofenil)-propilsulfanil]-N-[[4-(trifluorometiloksi)-fenil]-metil]-piridin-3-karboksilne kiseline; 80 amid 2-[3-(4-fluorofenil)-propilsulfanil]-N-[[4-(trifluorometil)-fenil]-metil]-piridin-3-karboksilne kiseline; 81 amid 2-[3-(4-fluorofenil)-propilsulfanil]-N-(2-piridin-3-il-etil)-piridin-3-karboksilne kiseline; 82 amid 2-[3-(4-fluorofenil)-propilsulfanil]-N-(2-piridin-2-il-etil)-piridin-3-karboksilne kiseline; 83 amid 2-[3-(4-fluorofenil)-propilsulfanil]-N-[(2-hidroksifenil)-metil]-piridin-3-karboksilne kiseline; 84 amid 2-[3-(4-fluorofenil)-propilsulfanil]-N-[(3-hidroksifenil)-metil]-piridin-3-karboksilne kiseline; 85 amid 2-[3-(4-fluorofenil)-propilsulfanil]-N-[2-(m-toliol)-etil]-piridin-3-karboksilne kiseline; 86 amid 2-[3-(4-fluorofenil)-propilsulfanil]-N-[2-(o-toliol)-etil]-piridin-3-karboksilne kiseline; 87 amid 2-[3-(4-fluorofenil)-propilsulfanil]-N-[[3-(trifluorometiloksi)-fenil]-metil]-piridin-3-karboksilne kiseline; 88 amid 2-[3-(4-fluorofenil)-propilsulfanil]-N-[(4-hidroksifenil)-metil]-piridin-3-karboksilne kiseline; 89 amid 2-[3-(4-fluorofenil)-propilsulfanil]-N-(2-piridin-4-il-etil)-piridin-3-karboksilne kiseline; 90 amid 2-[3-(4-fluorofenil)-propilsulfanil]-N-[2-(p-toliol)-etil]-piridin-3-karboksilne kiseline; 91 amid N-(5-biciklo[2.2.1]heptanil-metil)-2-[3-(4-fluorofenil)-butilsulfanil]-piridin-3-karboksilne kiseline; 92 amid N-(5-biciklo[2.2.1]heptanil-metil)-2-[3-(2,4,5-trifluoro-fenil)-propilsulfanil]- piridin-3-karboksilne kiseline; 93 amid 2-[3-(4-fluorofenil)-propilsulfanil]-N-(3-piridin-2-il-propil)-piridin-3-karboksilne kiseline; 94 amid 2-[3-(4-fluorofenil)-propilsulfanil]-N-(3-piridin-3-il-propil)-piridin-3-karboksilne kiseline; 95 amid 2-[3-(4-fluorofenil)-propilsulfanil]-N-(3-piridin-4-il-propil)-piridin-3-karboksilne kiseline; 96 amid 2-[3-(4-fluorofenil)-propilsulfanil]-N-propil-piridin-3-karboksilne kiseline; 97 amid N-butil-2-[3-(4-fluorofenil)-propilsulfanil]- piridin-3-karboksilne kiseline; 98 amid 2-(3-piridin-3-il-propilsilfanil)-N-(tiofen-2-il-metil)-piridin-3-karboksilne kiseline; 99 amid 2-[3-(p-toliol)-propilsulfanil]-N-(tiofen-2-il-metil)-piridin-3-karboksilne kiseline; 100 amid 2-(4-fenil-butilsulfanil)-N-(tiofen-2-il-metil)-piridin-3-karboksilne kiseline; 101 amid 2-(3-piridin-4-il-propilsulfanil)-N-(tiofen-2-il-metil)-piridin-3-karboksilne kiseline; 102 amid 2-(3-naftalen-2-il-propilsulfanil)-N-(tiofen-2-il-metil)-piridin-3-karboksilne kiseline; 103 amid 2-[3-(m-toliol)-propilsulfanil]-N-(tiofen-2-il-metil)-piridin-3-karboksilne kiseline; 104 amid N-(tiofen-2-il-metil)-2-(3-tiofen-2-il-propilsulfanil)-piridin-3-karboksilne kiseline; 105 amid 2-[(1-metil-3-fenil-propil)sulfanil]-N-(tiofen-2-il-metil)-piridin-3-karboksilne kiseline; 106 amid N-(tiofen-2-il-metil)-2-(3-tiofen-3-il-propilsulfanil)-piridin-3-karboksilne kiseline; 107 amid 2-[[1-metil-3-[3-(trifluorometil)fenil]-propil]sulfanil]-N-(tiofen-2-il-metil)-piridin-3-karboksilne kiseline; 108 amid 2-[(2-benzil-cikloheksil)sulfanil]-N-(tiofen-2-il-metil)-piridin-3-karboksilne kiseline; 109 amid 2-[3-[3-metil-5-(trifluorometil)-fenil]-propilsulfanil]-N-(tiofen-2-il-metil)-piridin-3-karboksilne kiseline; 110 amid 2-[4-(3,4-difluoro-fenil)-butilsulfanil]-N-(tiofen-2-il-metil)-piridin-3-karboksilne kiseline; 111 amid 2-(3-piridin-2-il-propilsulfanil)-N-(tiofen-2-il-metil)-piridin-3-karboksilne kiseline; 113 amid 2-[3-[4-metil-3-(trifluorometil)-fenil]-propilsulfanil]-N-(tiofen-2-il-metil)-piridin-3-karboksilne kiseline; 114 amid 2-[(3-fenil-cikloheksil)sulfanil]-N-(tiofen-2-il-metil)-piridin-3-karboksilne kiseline; 116 amid 2-[[3,3-difluoro-3-(4-fluorofenil)-propil]sulfanil-N-(3,3-dimetil-butil)-piridin-3-karboksilne kiseline; 117 amid N-(cikloheptil-metil)-2-[[3,3-difluoro-3-(4-fluorofenil)-propil]sulfanil]-piridin-3-karboksilne kiseline; 118 amid 2-[[3,3-difluoro-3-(4-fluorofenil)-propil]sulfanil]-N-(tiofen-2-il-metil)-piridin-3-karboksilne kiseline; 119 amid 2-[3-(4-fluorofenil)-propilsulfanil]-N-(1,2,3,4-tetrahidro-naftalen-2-il-metil)-piridin-3-karboksilne kiseline; 120 amid N-(2,3-dihidro-1H-inden-2-il-metil)-2-[3-(4-fluorofenil)-propilsulfanil]-piridin-3-karboksilne kiseline; 121 amid N-(1,3-benzodioksol-5-il-metil)-2-[3-(4-fluorofenil)-propilsulfanil]-piridin-3-karboksilne kiseline; 122 amid 2-[3-(4-fluorofenil)-propilsulfanil]-N-[(3-fenil-fenil)-metil]-piridin-3-karboksilne kiseline; 123 amid 2-[3-(4-fluorofenil)-propilsulfanil]-N-[(3-metil-cikloheksil)-metil]-piridin-3-karboksilne kiseline; 124 amid 2-[[3,3-difluoro-3-(4-fluorofenil)-propil]sulfanil]-N-[(4-fluorofenil)-metil]-piridin-3-karboksilne kiseline; 125 amid N-(3,3-dimetil-2-okso-butil)-2-[3-(4-fluorofenil)-propilsulfanil]-piridin-3-karboksilne kiseline; 127 amid 2-[3-(4-fluorofenil)-propilsulfanil]-N-(piridin-3-il-metil)-piridin-3-karboksilne kiseline; 128 amid 2-[3-(4-fluorofenil)-propilsulfanil]-N-(piridin-4-il-metil)-piridin-3-karboksilne kiseline; 129 metil ester 3-[[[2-[3-(4-fluorofenil)-propilsulfanil]-piridin-3-karboksil]amino]-metil]-benzojeve kiseline; 130 amid 2-[3-(4-fluorofenil)-propilsulfanil]-N-[3-(2-metoksifenil)-propil]-piridin-3-karboksilne kiseline; 132 amid N-[(4-fluorofenil)-metil]-2-[[1-metil-3-[3-(trilfuorometil)fenil]-propil]sulfanil]-piridin-3-karboksilne kiseline; 133 amid 2-[3-(4-fluorofenil)-propilsulfanil]-N-(3-metil-butil)-piridin-3-karboksilne kiseline; 134 amid 2-[3-(4-fluorofenil)-propilsulfanil]-N-(tetrahidro-piran-2-il-metil)-piridin-3-karboksilne kiseline; 135 amid 2-[3-(4-fluorofenil)-propilsulfanil]-N-[3-(1H-pirazol-1-il)-propil]-piridin-3-karboksilne kiseline; 136 amid 2-[3-(4-fluorofenil)-propilsulfanil]-N-(naftalen-2-il-metil)-piridin-3-karboksilne kiseline; 137 amid N-(2,3-dihidro-[1,4]benzodioksin-6-il-metil)-2-[3-(4-fluorofenil)-propilsulfanil]-piridin-3-karboksilne kiseline; 138 amid 2-[3-(4-fluorofenil)-propilsulfanil]-N-[(3-morfolin-4-il-fenil)-metil]-piridin-3-karboksilne kiseline; 139 amid N-(2,3-dihidro-benzofuran-6-il-metil)-2-[3-(4-fluorofenil)-propilsulfanil]-piridin-3-karboksilne kiseline; 140 amid 2-[3-(4-fluorofenil)-propilsulfanil]-N-[[3-(1H-pirazol-1-il)-fenil]-metil]-piridin-3-karboksilne kiseline; 141 amid 2-[3-(4-fluorofenil)-propilsulfanil]-N-[3-(1H-[1,2,3]triazol-1-il)-propil]-piridin-3-karboksilne kiseline; 142 amid N-(7-biciklo[2.2.1]heptanil-metil)-2-[3-(4-fluorofenil)-propilsulfanil]-piridin-3-karboksilne kiseline; 144 amid 2-[3-(4-fluorofenil)-propilsulfanil]-N-(tiazol-2-il-metil)-piridin-3-karboksilne kiseline; 145 amid 2-[3-(4-fluorofenil)-propilsulfanil]-N-(tiazol-5-il-metil)-piridin-3-karboksilne kiseline; 146 amid 2-[3-(4-fluorofenil)-propilsulfanil]-N-(oksazol-2-il-metil)-piridin-3-karboksilne kiseline; 148 amid N-(3,3-dimetil-butil)-2-[3-(4-fluorofenil)-propilsulfanil]-4-metil-piridin-3-karboksilne kiseline; 149 amid N-(3,3-dimetil-butil)-2-[[1-metil-3-[3-(trifluorometil)fenil]-propil]sulfanil]-piridin-3-karboksilne kiseline; 150 amid 2-[3-(4-fluorofenil)-propilsulfanil]-N-(kinolin-7-il-metil)-piridin-3-karboksilne kiseline; 151 amid 2-[3-(4-fluorofenil)-propilsulfanil]-N-[(3-piridin-2-il-fenil)-metil]-piridin-3-karboksilne kiseline; 152 amid 2-[3-(4-fluorofenil)-propilsulfanil]-N-[(3-piridin-3-il-fenil)-metil]-piridin-3-karboksilne kiseline; 153 amid N-(3,3-dimetil-butil)-2-[[(1R)-1-metil-3-fenil-propil]sulfanil]-piridin-3-karboksilne kiseline; 154 kiseline amid N-(3,3-dimetil-butil)-2-[[(11S)-1-metil-3-fenil-propil]sulfanil]-piridin-3-karboksilne; 155 amid 2-[(2-benzil-ciklopentil)sulfanil]-N-(3,3-dimetil-butil)-piridin-3-karboksilne kiseline; 156 amid N-(7-biciklo[2.2.1]heptanil-metil)-2-[3-[3-(trifluorometil)fenil]-propilsulfanil]- piridin-3-karboksilne kiseline; 157 amid 2-[3-(4-fluorofenil)-propilsulfanil]-N-[3-(1H-[1,2,4]triazol-1-il)-propil]-piridin-3-karboksilne kiseline; 158 amid 2-[3-(4-fluorofenil)-propilsulfanil]-N-([1,3,4]oksadiazol-2-il-metil)-piridin-3-karboksilne kiseline; 159 amid 2-[3-(4-fluorofenil)-propilsulfanil]-N-[(3-piridin-4-il-fenil)-metil]-piridin-3-karboksilne kiseline; 160 amid N-[[4-(ciklopropilmetil)-3,4-dihidro-2H-[1,4]benzoksazin-6-il]-metil]-2-[3-(4-fluorofenil)-propilsulfanil]-piridin-3-karboksilne kiseline; 161 amid N-[(4-etil-3,4-dihidro-2H-[1,4]benzoksazin-6-il)-metil]-2-[3-(4-fluorofenil)-propilsulfanil]-piridin-3-karboksilne kiseline; 162 amid 2-[3-(4-fluorofenil)-propilsulfanil]-N-[(4-metil-3,4-dihidro-2H-[1,4]benzoksazin-6-il)-metil]-piridin-3-karboksilne kiseline; 163 amid 2-[3-(4-fluorofenil)-propilsulfanil]-N-(3-metil-3-fenil-butil)-piridin-3-karboksilne kiseline; 164 amid N-(7-biciklo[2.2.1]heptanil-metil)-2-[[3,3-difluoro-3-(4-fluorofenil)-propil]sulfanil]- piridin-3-karboksilne kiseline; 165 amid 2-[[3,3-difluoro-3-[3-(trifluorometil)fenil]-propil]sulfanil]-N-[(4-fluorofenil)-metil]-piridin-3-karboksilne kiseline; 166 amid 2-[[3,3-difluoro-3-[3-(trifluorometil)fenil]-propil]sulfanil]-N-(3,3-dimetil-butil)-piridin-3-karboksilne kiseline 168 amid 2-[[3,3-difluoro-3-(4-(fluorofenil)propil]sulfanil]-N-[(3-fluorofenil)-metil]-piridin-3-karboksilne kiseline; 170 amid N-butil-2-[[3,3-(difluoro-3-(4-fluorofenil)-propil]sulfanil]-piridin-3-karboksilne kiseline; 171 amid 2-[[3,3-difluoro-3-(4-(fluorofenil)propil]sulfanil]-N-[(2-metoksi-etil)-piridin-3-karboksilne kiseline; 172 amid 2-[3-(4-fluorofenil)-propilsulfanil]-N-(2-metoksi-etil)-piridin-3-karboksilne kiseline; 173 amid N-[(4-fluoro-2-hidroksi-fenil)-metil]-2-[3-(4-fluorofenil)-propilsulfanil]-piridin-3-karboksilne kiseline; 174 amid 2-[3-(4-fluorofenil)-propilsulfanil]-N-(furan-2-il-metil)-piridin-3-karboksilne kiseline; 175 amid 2-[3-(4-fluorofenil)-propilsulfanil]-N-[(5-metil-furan-2-il)-metil]-piridin-3-karboksilne kiseline; 176 amid N-[(4-fluorofenil)-metil]-2-[[3-(4-fluorofenil)-1-metil-propil]sulfanil]-piridin-3-karboksilne kiseline; 177 amid 2-[[3-(4-(fluorofenil)-1-metil-propil]sulfanil]-N-(3-metil-butil)-piridin-3-karboksilne kiseline; 178 amid N-(7-biciklo[2.2.1]heptanil-metil)-2-[[3-(4-fluorofenil)-1-metil-propil]sulfanil]-piridin-3-karboksilne kiseline; 179 amid 2-[[3,3-difluoro-3-(4-(fluorofenil)propil]sulfanil-N-(tetrahidro-furan-2-il-metil)-piridin-3-karboksilne kiseline; 180 amid 2-[[3,3-difluoro-3-(4-fluorofenil)-propil]sulfanil]-N-(tetrahidro-piran-2-il-metil)-piridin-3-karboksilne kiseline; 181 amid 2-[3-(4-fluorofenil)-propilsulfanil]-N-(tetrahidro-furan-2-il-metil)-piridin-3-karboksilne kiseline; 182 amid 2-[3-(4-fluorofenil)-propilsulfanil]-N-(2-metoksi-3,3-dimetil-butil)-piridin-3-karboksilne kiseline; 183 amid 2-[[3,3-difluoro-3-(4-fluorofenil)-propil]sulfanil]-N-(m-toliol-metil)-piridin-3-karboksilne kiseline; 184 amid 2-[[3,3-difluoro-3-(4-fluorofenil)-propil]sulfanil]-N-[(3,5-dimetil-fenil)-metil]-piridin-3-karboksilne kiseline; 185 amid 2-[[3,3-difluoro-3-(4-fluorofenil)-propil]sulfanil]-N-propil-piridin-3-karboksilne kiseline; 186 amid 2-[[3,3-difluoro-3-(4-fluorofenil)-propil]sulfanil]-N-heksil-piridin-3-karboksilne kiseline; 187 amid 2-[[3,3-difluoro-3-(4-fluorofenil)-propil]sulfanil]-N-(tetrahidro-furan-3-il-metil)-piridin-3-karboksilne kiseline; 188 amid 2-[[3,3-difluoro-3-(4-fluorofenil)-propil]sulfanil]-N-(tetrahidro-piran-3-il-metil)-piridin-3-karboksilne kiseline; 189 amid 2-[[3,3-difluoro-3-(4-fluorofenil)-propil]sulfanil]-N-(tetrahidro-piran-4-il-metil)-piridin-3-karboksilne kiseline; 190 amid 2-[[3,3-difluoro-3-(4-fluorofenil)-propil]sulfanil]-N-(furan-2-il-metil)-piridin-3-karboksilne kiseline; 191 amid 2-[[3,3-difluoro-3-(4-fluorofenil)-propil]sulfanil]-N-[(5-metil-furan-2-il)-metil]-piridin-3-karboksilne kiseline; 192 amid 2-[[3,3-difluoro-3-(4-fluorofenil)-propil]sulfanil]-N-pentil-piridin-3-karboksilne kiseline; 193 amid 2-[[3,3-difluoro-3-(4-fluorofenil)-propil]sulfanil]-N-(3-metoksi-butil)-piridin-3-karboksilne kiseline; 194 amid 2-[[3,3-difluoro-3-(4-fluorofenil)-propil]sulfanil]-N-(2-metoksi-propil)-piridin-3-karboksilne kiseline; 195 amid 2-[[3,3-difluoro-3-(4-fluorofenil)-propil]sulfanil]-N-(2-metoksi-butil)-piridin-3-karboksilne kiseline; 196 metil ester 3-[[2-[[3,3-difluoro-3-(4-fluorofenil)-propil]sulfanil]-piridin-3-karbonil]amino]-propionske kiseline; 197 3-[[2-[[3,3-difluoro-3-(4-fluorofenil)-propil]sulfanil]-piridin-3-karbonil]amino]- propionska kiselina; 198 amid 2-[[3,3-difluoro-3-(4-fluorofenil)-propil]sulfanil]-N-(2-dimetilaminoetil)-piridin-3-karboksilne kiseline; 199 amid 2-[[3-(3,4-difluoro-fenil)-1-metil-propil]sulfanil]-N-[(4-fluorofenil)-metil]-piridin-3-karboksilne kiseline; 200 amid 2-[[3-(3,4-difluoro-fenil)-1-metil-propil]sulfanil]-N-(3-metil-butil)-piridin-3-karboksilne kiseline; 201 amid N-[(4-fluorofenil)-metil]-2-[[3-(3-fluorofenil)-1-metil-propil]sulfanil]-piridin-3-karboksilne kiseline; 202 amid 2-[[3-(3-fluorofenil)-1-metil-propil]sulfanil]-N-(3-metil-butil)-piridin-3-karboksilne kiseline; 203 amid N-(3-metil-butil)-2-[[1-metil-3-[3-(trifluorometil)fenil]-propil]sulfanil]-piridin-3-karboksilne kiseline; 204 amid 2-[[3-(3,4-difluoro-fenil)-3,3-difluoro-propil]sulfanil]-N-[(4-fluorofenil)-metil]-piridin-3-karboksilne kiseline; 205 amid N-(1-biciklo[2.2.1]heptanil-metil)-2-[[3,3-difluoro-3-(4-fluorofenil)-propil]sulfanil]- piridin-3-karboksilne kiseline; 206 amid N-(1-biciklo[2.2.1]heptanil-metil)-2-[3-(4-fluorofenil)-propilsulfanil]-piridin-3-karboksilne kiseline; 207 amid N-[(4-fluorofenil)-metil]-2-[3-[3-(trifluorometil)fenil]-propilsulfanil]-piridin-3-karboksilne kiseline; 208 amid N-(3-metil-butil)-2-[3-[3-(trifluorometil)fenil]-propilsulfanil]-piridin-3-karboksilne kiseline; 209 amid 2-[[3-(3,4-difluoro-fenil)-3,3-difluoro-propil]sulfanil]-N-(3-metil-butil)-piridin-3-karboksilne kiseline; 210 amid N-(7-biciklo[2.2.1]heptanil-metil)-2-[[3-(3,4-difluoro-fenil)-3,3-difluoro-propil]sulfanil]- piridin-3-karboksilne kiseline; 211 amid 2-[[3,3-difluoro-3-(4-fluorofenil)-propil]sulfanil]-N-(2-hidroksi-etil)-piridin-3-karboksilne kiseline; 224 amid N-[(4-fluoro-2-metoksi-fenil)metil]-2-[3-(4-fluorofenil)-propilsulfanil]-piridin-3-karboksilne kiseline; ili njihove fiziološki kompatibilne soli.
12. Lijekovi naznačeni time da sadrže barem jedan supstituirani nikotinamid prema jednom od zahtjeva 1 do 11, svaki u obliku jednog stereoizomera ili njihove smjese, slobodnih spojeva i/ili njihovih fiziološki kompatibilnih soli, kao i mogućih pogodnih aditiva i/ili pomoćnih sredstava i/ili mogućih dodatnih aktivnih tvari.
13. Uporaba barem jednog supstituiranog nikotinamida prema jednom od zahtjeva 1 do 11, svakog u obliku jednog stereoizomera ili njihove smjese, slobodnog spoja i/ili njegovih fiziološki kompatibilnih soli, naznačena time da je za proizvodnju lijeka za liječenje boli, epilepsije, poremećaja anksioznosti, ovisnosti, manije, bipolarnih poremećaja, migrene, kognitivnih bolesti, diskinezije povezane s distonijom i/ili urinarne inkontinencije.
14. Supstituirani nikotinamid prema jednom od zahtjeva 1 do 11, svaki u obliku jednog stereoizomera ili njihove smjese, slobodnog spoja i/ili njegovih fiziološki kompatibilnih soli, naznačen time da je za liječenje boli, epilepsije, poremećaja anksioznosti, ovisnosti, manije, bipolarnih poremećaja, migrene, kognitivnih bolesti, diskinezije povezane s distonijom i/ili urinarne inkontinencije.
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