HRP20221279T1 - Modulatori somatostatina i njihove uporabe - Google Patents

Modulatori somatostatina i njihove uporabe Download PDF

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HRP20221279T1
HRP20221279T1 HRP20221279TT HRP20221279T HRP20221279T1 HR P20221279 T1 HRP20221279 T1 HR P20221279T1 HR P20221279T T HRP20221279T T HR P20221279TT HR P20221279 T HRP20221279 T HR P20221279T HR P20221279 T1 HRP20221279 T1 HR P20221279T1
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quinolin
difluorophenyl
fluoro
pyrido
octahydro
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HRP20221279TT
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Jian Zhao
Sangdon Han
Sun Hee Kim
Shimiao Wang
Yunfei Zhu
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Crinetics Pharmaceuticals, Inc.
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Claims (24)

1. Spoj koji ima sljedeću strukturu, ili njegova farmaceutski prihvatljiva sol, solvat, dijastereomerna mješavina, ili pojedinačni enantiomeri: [image] naznačen time što: svako Ra je neovisno vodik, F, Cl, Br, -CH3, -CH2F, -CHF2, -CF3, -CN, -OH, -OCH3, -OCF3, -CH2OH ili -CH2CH2OH; svako Rb je neovisno vodik, F, Cl, Br, -CH3, -CH2F, -CHF2, -CF3, -CN, -OH, -OCH3, ili -OCF3; m je 1 ili 2; n je 0, 1 ili 2; RB je [image] ili [image] svako Rc je neovisno vodik, F, Cl, Br, -CH3, -CH2CH3, -CH2CH2CH3, -CH(CH3)2, -CH2CH2CH2CH3, -CH2CH(CH3)2, -CH(CH3)(CH2CH3), -C(CH3)3, -CH2OH, -CH2CN, - CH2F, -CHF2, -CF3, -CN, -OH, -OCH3, -OCH2CH3, -OCF3, -CO2H, -CO2CH3, -CO2CH2CH3, -CH2CO2H, -CH2CO2CH3, -CH2CO2CH2CH3, -C(=O)NH2, -C(=O)NHCH3, -C(=O)NHOCH3, -C(=O)N(CH3)2, -SO2N(CH3)2, -C(=NOCH3)H, -CH2C(=O)NH2, -CH2C(=O)NHCH3, -CH2C(=O)N(CH3)2, -NH2, -NHCH3, -N(CH3)2, -NHCO2CH3, -NHSO2CH3, -CH2NH2, -CH2NHCH3, -CH2N(CH3)2, -CH(CF3)NH2, azetidinil, ili pirolidinil; svako Rd je neovisno vodik, F, Cl, Br, -CH3, -CH2CH3, -CH2CH2CH3, -CH(CH3)2, -CH2CH2CH2CH3, -CH2CH(CH3)2, -CH(CH3)(CH2CH3), -C(CH3)3, -CH2OH, -CH2CN, -CH2F, -CHF2, -CF3, pirolil, imidazolil, pirazolil, triazolil, tetrazolil, -CN, -OH, -OCH3, -OCH2CH3, -OCF3, -OCH2OCH3, -OCH2OCH2CH3, -OCH2CH2OH, -C(=O)NHOCH3, -C(=NOH)H, -C(=NOCH3)H, -CH2C(=O)NH2, -NH2, -NHCO2CH3, -NHSO2CH3, -NH(C=O)NHCH3, -NH(C=O)NHOCH3 ili -CH(CF3)NH2; ili ako su jedan Rc i jedan Rd na susjednim atomima RB tada su susjedne Rc i Rd grupe uzete zajedno sa atomima koji su između za koje su vezani tako da formiraju 5- ili 6-člani monociklični heterociklus; p je 1 ili 2; q je 0, 1 ili 2; X je CRf ili N; Y je CRf ili N; Z je CRf ili N; Re je vodik, F, Cl, Br, -CH3, -CH2CH3, -CH2F, -CHF2, -CF3, -CN, -OH, -OCH3, - OCH2CH3, ili -OCF3; svako Rf je neovisno vodik, F, Cl, Br, -CH3, -CH2CH3, -CH2F, -CHF2, -CF3, -CN, -OH, -OCH3, -OCH2CH3, ili -OCF3; R1 je vodik; R2 je vodik, metil, etil, 2-fluoroetil, 2-hidroksietil, 2-metoksietil, n-propil, i-propil, ciklopropil, 3-fluoropropil, 3-metoksipropil, n-butil, i-butil, sek-butil, ciklobutil, terc-butil ili oksetanil; R5 je vodik, F, Cl, Br, -OH, -OCH3, -NH2, -NHCH3, -N(CH3)2, -OCH2CH3, -OCF3, -CH3, -CH2CH3, -CH2F, -CHF2, -CF3, -CN, -C(=O)OCH3, -C(=O)NH2, -C(=O)NHCH3, ili -C(=O)N(CH3)2; ili R2 i R5 su uzeti zajedno sa atomima koji su između za koje su vezani tako da formiraju azetidinil, pirolidinil, piperidinil, morfolinil, tiomorfolinil, piperazinil, ili azepanil.
2. Spoj prema patentnom zahtjevu 1, ili njegova farmaceutski prihvatljiva sol, solvat, dijastereomerna mješavina, ili pojedinačni enantiomeri, naznačen time što: svako Ra je neovisno vodik, F, Cl, Br, -CH3, -CH2F, -CHF2, -CF3, -CN, -OH, -OCH3, -OCF3, -CH2OH ili -CH2CH2OH; svako Rb je neovisno vodik, F, Cl, Br, -CH3, -CH2F, -CHF2, -CF3, -CN, -OH, -OCH3, ili -OCF3; svako Rc je neovisno vodik, F, Cl, Br, -CH3, -CH2F, -CHF2, -CF3, -CN, -OH, -OCH3, -OCF3, -NH2, -C(=O)NH2, -C(=NOCH3)H, -SO2N(CH3)2, azetidinil, ili pirolidinil; svako Rd je neovisno vodik, F, Cl, Br, -CH3, -CH2F, -CHF2, -CF3, -CN, -OH, -OCH3, -OCF3, -OCH2OCH3, -CH2OH, -OCH2CH2OH, -C(=O)NHOCH3, -NH2, -NHCO2CH3, -NH(C=O)NHOCH3 ili -CH2C(=O)NH2; ili ako su jedan Rc i jedan Rd na susjednim atomima RB tada su susjedne Rc i Rd grupe uzete zajedno sa atomima koji su između za koje su vezani tako da formiraju 5-člani monociklični heterociklus.
3. Spoj prema patentnom zahtjevu 1 ili patentnom zahtjevu 2, naznačen time što spoj ima sljedeću strukturu, ili njegova farmaceutski prihvatljiva sol, solvat, dijastereomerna mješavina ili pojedinačni enantiomeri: [image]
4. Spoj prema bilo kojem od patentnih zahtjeva 1 to 3, ili njegova farmaceutski prihvatljiva sol, solvat, dijastereomerna mješavina, ili pojedinačni enantiomeri, naznačen time što: svako Ra je neovisno vodik, F, Cl, Br, -CH3, -CH2F, -CHF2, -CF3, -CN, -OH, -OCH3, -OCF3, -CH2OH ili -CH2CH2OH; svako Rb je neovisno vodik, F, Cl, Br, -CH3, -CH2F, -CHF2, -CF3, -CN, -OH, -OCH3, ili -OCF3; svako Rc je neovisno vodik, F, Cl, Br, -CH3, -CH2F, -CHF2, -CF3, -CN, -OH, -OCH3, -OCF3, -NH2, -C(=O)NH2, -C(=NOCH3)H, -SO2N(CH3)2, azetidinil ili pirolidinil; svako Rd je neovisno vodik, F, Cl, Br, -CH3, -CH2F, -CHF2, -CF3, -CN, -OH, -OCH3, -OCF3, -OCH2OCH3, -CH2OH, -OCH2CH2OH, -C(=O)NHOCH3, -NH2, -NHCO2CH3, -NH(C=O)NHOCH3, ili -CH2C(=O)NH2; Re je vodik, F, Cl, Br, -CH3, -CH2F, -CHF2, -CF3, -CN, -OH, -OCH3, ili -OCF3; svako Rf je vodik; R1 je vodik; R2 je vodik; R5 je vodik, F, Cl, Br, -OH, -OCH3, -NH2, -NHCH3, -N(CH3)2, -OCH2CH3, -OCF3, -CH3, -CH2CH3, -CH2F, -CHF2, -CF3, -CN, -C(=O)OCH3, -C(=O)NH2, -C(=O)NHCH3, ili -C(=O)N(CH3)2; ili R2 i R5 su uzeti zajedno sa atomima koji su između za koje su vezani tako da formiraju piperidinil, morfolinil, tiomorfolinil, ili piperazinil.
5. Spoj prema bilo kojem od patentnih zahtjeva 1 do 4, ili njegova farmaceutski prihvatljiva sol, solvat, dijastereomerna mješavina, ili pojedinačni enantiomeri, naznačen time što: svako Ra je neovisno vodik, F, Cl, -CH3, -CF3, -CN, -OH, -OCH3, -OCF3, -CH2OH ili -CH2CH2OH svako Rb je neovisno vodik, F, Cl, -CH3, -CF3, -CN, -OH, -OCH3, ili -OCF3; svako Rc je neovisno vodik, F, Cl, -CH3, -CF3, -CN, -OH, -OCH3, ili -OCF3; svako Rd je neovisno vodik, F, Cl, -CH3, -CF3, -CN, -OH, -OCH3, -OCF3, ili -NH2; X je CRf; Y je CRf; i Z je CRf; ili X je N; Y je CRf; i Z je CRf; ili X je CRf; Y je N; i Z je CRf; ili X je CRf; Y je CRf; i Z je N; Re je vodik, F, ili Cl; svako Rf je vodik; R1 je vodik; R2 je vodik; R5 je vodik; ili R2 i R5 su uzeti zajedno sa atomima koji su između za koje su vezani tako da formiraju morfolinil.
6. Spoj prema bilo kojem od patentnih zahtjeva 1 do 3, naznačen time što spoj ima sljedeću strukturu Formule (AVb), ili njegova farmaceutski prihvatljiva sol, solvat, dijastereomerna mješavina, ili pojedinačni enantiomeri: [image] naznačen time što: RB je [image] R1 je vodik; R2 je vodik, metil, etil, 2-fluoroetil, 2-hidroksietil, 2-metoksietil, n-propil, i-propil, ciklopropil, 3-fluoropropil, 3-metoksipropil, n-butil, i-butil, sek-butil, ciklobutil, terc-butil, ili oksetanil; R5 je vodik, F, Cl, Br, -OH, -OCH3, -NH2, -NHCH3, -N(CH3)2, -OCH2CH3, -OCF3, -CH3, -CH2CH3, -CH2F, -CHF2, -CF3, -CN, -C(=O)OCH3, -C(=O)NH2, -C(=O)NHCH3, ili -C(=O)N(CH3)2; ili R2 i R5 su uzeti zajedno sa atomima koji su između za koje su vezani tako da formiraju azetidinil, pirolidinil, piperidinil, morfolinil, tiomorfolinil, piperazinil, ili azepanil.
7. Spoj prema patentnom zahtjevu 6, ili njegova farmaceutski prihvatljiva sol, solvat, dijastereomerna mješavina, ili pojedinačni enantiomeri, naznačen time što: Ra je vodik, F, Cl, Br, -CH3, -CH2F, -CHF2, -CF3, -CN, -OH, -OCH3, -OCF3, -CH2OH ili -CH2CH2OH; Rb je vodik, F, Cl, Br, -CH3, -CH2F, -CHF2, -CF3, -CN, -OH, -OCH3, ili -OCF3; svako Rc je neovisno vodik, F, Cl, Br, -CH3, -CH2F, -CHF2, -CF3, -CN, -OH, -OCH3, -OCF3, -NH2, -C(=O)NH2, -C(=NOCH3)H, -SO2N(CH3)2, azetidinil, ili pirolidinil; svako Rd je neovisno vodik, F, Cl, Br, -CH3, -CH2F, -CHF2, -CF3, -CN, -OH, -OCH3, -OCF3, -OCH2OCH3, -CH2OH, -OCH2CH2OH, -C(=O)NHOCH3, -NH2, -NHCO2CH3, -NH(C=O)NHOCH3, ili -CH2C(=O)NH2; Re je vodik, F, Cl, Br, -CH3, -CH2F, -CHF2, -CF3, -CN, -OH, -OCH3, ili -OCF3; R1 je vodik; R2 je vodik; R5 je vodik, F, Cl, Br, -OH, -OCH3, -NH2, -NHCH3, -N(CH3)2, -OCH2CH3, -OCF3, -CH3, -CH2CH3, -CH2F, -CHF2, -CF3, -CN, -C(=O)OCH3, -C(=O)NH2, -C(=O)NHCH3, ili -C(=O)N(CH3)2; ili R2 i R5 su uzeti zajedno sa atomima koji su između za koje su vezani tako da formiraju piperidinil, morfolinil, tiomorfolinil ili piperazinil.
8. Spoj prema patentnom zahtjevu 6 ili patentnom zahtjevu 7, ili njegova farmaceutski prihvatljiva sol, solvat, dijastereomerna mješavina, ili pojedinačni enantiomeri, naznačen time što: Ra je vodik, F, Cl, -CH3, -CF3, -CN, -OH, -CH2OH, -CH2CH2OH, -OCH3, ili -OCF3; Rb je vodik, F, Cl, -CH3, -CF3, -CN, -OH, -OCH3, ili -OCF3; svako Rc je neovisno vodik, F, Cl, -CH3, -CF3, -CN, -OH, -NH2, -OCH3, -OCF3, - CONH2, ili -C(=NOCH3)H; svako Rd je neovisno vodik, F, Cl, -CH3, -CF3, -CN, -OH, -NH2, -OCH3, ili -OCF3; R1 je vodik; R2 je vodik; R5 je vodik; ili R2 i R5 su uzeti zajedno sa atomima koji su između za koje su vezani tako da formiraju morfolinil.
9. Spoj prema patentnom zahtjevu 1, naznačen time što, spoj je: 1-1: 3-[4-(4-aminopiperidin-1-il)-7-kloro-3-(3,5-dimetilfenil)cinolin-6-il]-5-fluorobenzamid; 1-2: 3-[4-(4-aminopiperidin-1-il)-7-kloro-3-(3,5-dimetilfenil)cinolin-6-il]-2-hidroksibenzonitril; 1-4: 3-[4-(4-aminopiperidin-1-il)-7-kloro-3-(3-fluoro-5-metilfenil)cinolin-6-il]-5-fluorobenzamid; 1-5: 3-{4-[trans-4-amino-3-fluoropiperidin-1-il]-7-kloro-3-(3-fluoro-5-metilfenil)cinolin-6-il}-5-fluorobenzamid; 1-6: 3-{4-[cis-4-amino-3-fluoropiperidin-1-il]-7-kloro-3-(3-fluoro-5-metilfenil)cinolin-6-il}-5-fluorobenzamid; 1-7: 3-[4-(4-aminopiperidin-1-il)-7-kloro-3-(3-fluoro-5-metilfenil)cinolin-6-il]-2-hidroksibenzonitril; 1-8: 5-[4-(4-aminopiperidin-1-il)-7-kloro-3-(3-fluoro-5-metilfenil)cinolin-6-il]-2,3-dihidro-1H-1,3-benzodiazol-2-on; 1-9: 4-[4-(4-aminopiperidin-1-il)-7-kloro-3-(3-fluoro-5-metilfenil)cinolin-6-il]-2,3-dihidro-1H-1,3-benzodiazol-2-on; 1-10: 3-{4-[trans-4-amino-3-metoksipiperidin-1-il]-7-kloro-3-(3-fluoro-5-metilfenil)cinolin-6-il}-5-fluorobenzamid; 1-11: 3-[4-(4-aminopiperidin-1-il)-7-kloro-3-(3,5-diklorofenil)cinolin-6-il]-2-hidroksibenzonitril; 1-12: 3-[4-(4-aminopiperidin-1-il)-7-kloro-3-(3-kloro-5-metilfenil)cinolin-6-il]-5-fluoro-2-hidroksibenzonitril; 1-13: 3-[4-(4-aminopiperidin-1-il)-3-(3-fluoro-5-metilfenil)cinolin-6-il]-5-fluorobenzamid; 1-14: 3-[4-(4-aminopiperidin-1-il)-3-(3,5-difluorofenil)cinolin-6-il]-5-fluorobenzamid; 1-16: 5-[4-(4-aminopiperidin-1-il)-3-(3-fluoro-5-metilfenil)cinolin-6-il]-2,3-dihidro-1H-1,3-benzodiazol-2-on; 1-17: 3-[4-(4-aminopiperidin-1-il)-3-(3-fluoro-5-metilfenil)cinolin-6-il]-2-hidroksibenzonitril; 1-18: 3-[4-(4-aminopiperidin-1-il)-3-(3-kloro-5-metilfenil)cinolin-6-il]-2-hidroksibenzonitril; 1-19: 3-[4-(4-aminopiperidin-1-il)-3-(3-kloro-5-fluorofenil)cinolin-6-il]-2-hidroksibenzonitril; 1-20: 3-[4-(4-aminopiperidin-1-il)-3-(3,5-difluorofenil)cinolin-6-il]-2-hidroksibenzonitril; 1-21: 3-[4-(4-aminopiperidin-1-il)-3-(3,5-diklorofenil)cinolin-6-il]-2-hidroksibenzonitril; 1-22: 3-[4-(4-aminopiperidin-1-il)-3-(3-kloro-5-metilfenil)cinolin-6-il]-5-fluoro-2-hidroksibenzonitril; 1-23: 6-[4-(4-aminopiperidin-1-il)-3-(3-kloro-5-metilfenil)cinolin-6-il]-4-fluoro-2,3-dihidro-1H-1,3-benzodiazol-2-on; 1-24: 4-[4-(4-aminopiperidin-1-il)-3-(3-kloro-5-metilfenil)cinolin-6-il]-6-fluoro-2,3-dihidro-1H-1,3-benzodiazol-2-on; 1-25: 3-[7-kloro-3-(3-fluoro-5-metilfenil)-4-{4-[(2-fluoroetil)amino]piperidin-1-il}cinolin-6-il]-5-fluorobenzamid; 1-26: 3-{4-[trans-4-amino-3-hidroksipiperidin-1-il]-7-kloro-3-(3-fluoro-5-metilfenil)cinolin-6-il}-5-fluorobenzamid; 1-27: 3-[4-(4-aminopiperidin-1-il)-7-kloro-3-(3,5-diklorofenil)cinolin-6-il]-5-fluoro-2-hidroksibenzonitril; 1-28: 6-[4-(4-aminopiperidin-1-il)-3-(3,5-diklorofenil)cinolin-6-il]-4-fluoro-2,3-dihidro-1H-1,3-benzodiazol-2-on; 1-29: 2-[4-(4-aminopiperidin-1-il)-3-(3-kloro-5-metilfenil)cinolin-6-il]-6-fluorofenol; 1-30: 3-[4-(4-aminopiperidin-1-il)-3-(3,5-diklorofenil)cinolin-6-il]-5-fluorobenzamid; 1-31: 3-[3-(3,5-diklorofenil)-4-{4-[(oksetan-3-il)amino]piperidin-1-il}cinolin-6-il]-5-fluorobenzamid; 1-33: 3-[3-(3,5-diklorofenil)-4-{4-[(2-fluoroetil)amino]piperidin-1-il}cinolin-6-il]-5-fluorobenzamid; 1-35: 3-[7-kloro-3-(3-kloro-5-metilfenil)-4-{4-[(2-fluoroetil)amino]piperidin-1-il}cinolin-6-il]-5-fluorobenzamid; 1-36: 3-[7-kloro-3-(3-kloro-5-metilfenil)-4-{4-[(2-fluoroetil)amino]piperidin-1-il}cinolin-6-il]-5-fluoro-2-hidroksibenzonitril; 1-38: 3-[7-kloro-3-(3-kloro-5-metilfenil)-4-{4-[(oksetan-3-il)amino]piperidin-1-il}cinolin-6-il]-5-fluorobenzamid; 1-39: 3-[7-kloro-3-(3-kloro-5-metilfenil)-4-{4-[(oksetan-3-il)amino]piperidin-1-il}cinolin-6-il]-5-fluoro-2-hidroksibenzonitril; 1-40: 3-[3-(3-kloro-5-metilfenil)-4-{4-[(oksetan-3-il)amino]piperidin-1-il}cinolin-6-il]-5-fluoro-2-hidroksibenzonitril; 1-41: 3-{4-[trans-4-amino-3-fluoropiperidin-1-il]-7-kloro-3-(3-kloro-5-metilfenil)cinolin-6-il}-5-fluorobenzamid; 1-42: 6-[4-(4-aminopiperidin-1-il)-7-kloro-3-(3-kloro-5-metilfenil)cinolin-6-il]piridin-2-karboksamid; 1-43: 6-[4-(4-aminopiperidin-1-il)-7-kloro-3-(3-kloro-5-metilfenil)cinolin-6-il]-5-kloropiridin-2-karboksamid; 1-44: 2-[4-(4-aminopiperidin-1-il)-7-kloro-3-(3-kloro-5-metilfenil)cinolin-6-il]piridin-4-karboksamid; 1-45: 2-[4-(4-aminopiperidin-1-il)-3-(3-kloro-5-metilfenil)cinolin-6-il]-6-fluoro-3-metilfenol; 1-48: 3-{4-[cis-oktahidro-1H-pirido[3,4-b]morfolin-6-il]-3-(3-kloro-5-metilfenil)cinolin-6-il}-5-fluorobenzamid; 1-49: 3-{4-[trans-oktahidro-1H-pirido[3,4-b]morfolin-6-il]-3-(3-kloro-5-metilfenil)cinolin-6-il}-5-fluorobenzamid; 1-51: 3-{4-[trans-oktahidro-1H-pirido[3,4-b]morfolin-6-il]-3-(3,5-diklorofenil)cinolin-6-il}-2-hidroksibenzonitril; 1-52: 3-{4-[trans-oktahidro-1H-pirido[3,4-b]morfolin-6-il]-3-(3-kloro-5-metilfenil)cinolin-6-il}-2-hidroksibenzonitril; 1-53: 3-{4-[trans-oktahidro-1H-pirido[3,4-b]morfolin-6-il]-3-(3-fluoro-5-metilfenil)cinolin-6-il}-2-hidroksibenzonitril; 1-54: 3-{4-[trans-oktahidro-1H-pirido[3,4-b]morfolin-6-il]-3-(3,5-difluorofenil)cinolin-6-il}-2-hidroksibenzonitril; 1-55: 5-{4-[trans-oktahidro-1H-pirido[3,4-b]morfolin-6-il]-3-(3,5-difluorofenil)cinolin-6-il}-4-aminopiridin-3-karbonitril; 1-56: 5-{4-trans-oktahidro-1H-pirido[3,4-b]morfolin-6-il]-3-(3-fluoro-5-metilfenil)cinolin-6-il}-4-aminopiridin-3-karbonitril; 1-57: 2-{4-[trans-oktahidro-1H-pirido[3,4-b]morfolin-6-il]-3-(3,5-difluorofenil)cinolin-6-il}-3-aminopiridin-4-karbonitril; 1-58: 2-{4-[trans-oktahidro-1H-pirido[3,4-b]morfolin-6-il]-3-(3-fluoro-5-metilfenil)cinolin-6-il}-3-aminopiridin-4-karbonitril; ili njegova farmaceutski prihvatljiva sol, solvat, dijastereomerna mješavina, ili pojedinačni enantiomeri.
10. Spoj prema patentnom zahtjevu 1, naznačen time što, spoj je: 2-1: 3-[4-(4-aminopiperidin-1-il)-3-(3-fluoro-5-metilfenil)hinolin-6-il]-2-hidroksibenzonitril; 2-2: 3-[4-(4-aminopiperidin-1-il)-3-(3,5-difluorofenil)hinolin-6-il]-2-hidroksibenzonitril; 2-3: 3-{4-[trans-4-amino-3-metoksipiperidin-1-il]-3-(3,5-difluorofenil)hinolin-6-il}-2-hidroksibenzonitril; 2-4: 3-{4-[trans-4-amino-3-metoksipiperidin-1-il]-3-(3,5-difluorofenil)hinolin-6-il}benzonitril; 2-5: 3-[4-(4-aminopiperidin-1-il)-3-(3,5-difluorofenil)hinolin-6-il]benzonitril; 2-6: 2-[4-(4-aminopiperidin-1-il)-3-(3,5-difluorofenil)hinolin-6-il]fenol; 2-7: 6-[4-(4-aminopiperidin-1-il)-3-(3-fluoro-5-metilfenil)hinolin-6-il]piridin-2-karboksamid; 2-8: 4-[4-(4-aminopiperidin-1-il)-3-(3-fluoro-5-metilfenil)hinolin-6-il]-2,3-dihidro-1H-1,3-benzodiazol-2-on; 2-9: 5-[4-(4-aminopiperidin-1-il)-3-(3-fluoro-5-metilfenil)hinolin-6-il]-2,3-dihidro-1H-1,3-benzodiazol-2-on; 2-10: 3-[4-(4-aminopiperidin-1-il)-3-(3,5-difluorofenil)hinolin-6-il]-5-fluoro-2-hidroksibenzonitril; 2-16: 3-[4-(4-aminopiperidin-1-il)-3-(3-fluoro-5-metilfenil)hinolin-6-il]-5-fluoro-2-hidroksibenzonitril; 2-19: 3-{4-[trans-oktahidro-1H-pirido[3,4-b]morfolin-6-il]-3-(3,5-difluorofenil)hinolin-6-il}-2-hidroksibenzonitril; 2-20: 3-{4-[trans-oktahidro-1H-pirido[3,4-b]morfolin-6-il]-3-(3-fluoro-5-metilfenil)hinolin-6-il}-2-hidroksibenzonitril; 2-58: 3-{4-[cis-4-amino-3-hidroksipiperidin-1-il]-3-(3,5-difluorofenil)hinolin-6-il}-2-(metoksimetoksi)benzonitril; 2-59: 3-{4-[(3R,4R)-4-amino-3-fluoropiperidin-1-il]-3-(3,5-difluorofenil)hinolin-6-il}-2-hidroksibenzonitril; 2-60: 3-{4-[cis-4-amino-3-hidroksipiperidin-1-il]-3-(3,5-difluorofenil)hinolin-6-il}-2-hidroksibenzonitril; 2-61: 3-{4-[(3S,4R)-4-amino-3-metoksipiperidin-1-il]-3-(3,5-difluorofenil)hinolin-6-il}-2-hidroksibenzonitril; 2-62: 3-{4-[(3R,4S)-4-amino-3-metoksipiperidin-1-il]-3-(3,5-difluorofenil)hinolin-6-il}-2-(metoksimetoksi)benzonitril; 2-63: 3-{4-[cis-4-amino-3-hidroksipiperidin-1-il]-3-(3,5-difluorofenil)hinolin-6-il}-5-fluoro-2-hidroksibenzonitril; 2-65: 3-[4-(4-aminopiperidin-1-il)-3-(3,5-difluorofenil)hinolin-6-il]-2-(2-hidroksietoksi)benzonitril; 2-66: 3-{4-[(3R,4S)-4-amino-3-metoksipiperidin-1-il]-3-(3,5-difluorofenil)hinolin-6-il}-2-hidroksibenzonitril; 2-75: 5-[4-(4-aminopiperidin-1-il)-3-(3,5-difluorofenil)hinolin-6-il]-6-(azetidin-1-il)piridin-3-karbonitril; 2-76: 5-[4-(4-aminopiperidin-1-il)-3-(3,5-difluorofenil)hinolin-6-il]-6-(azetidin-1-il)piridin-3-karboksamid; 2-77: 2-amino-3-[4-(4-aminopiperidin-1-il)-3-(3,5-difluorofenil)hinolin-6-il]benzonitril; 2-78: 3-[4-(4-aminopiperidin-1-il)-3-(3,5-difluorofenil)hinolin-6-il]-2-(metoksimetoksi) benzonitril; 2-80: 6-{4-[trans-oktahidro-1H-pirido[3,4-b]morfolin-6-il]-3-(3,5-difluorofenil)hinolin-6-il}-4-fluoro-2,3-dihidro-1H-1,3-benzodiazol-2-on; 2-81: 2-[4-(4-aminopiperidin-1-il)-3-(3,5-difluorofenil)hinolin-6-il]-6-[-(metoksiimino)metil] fenol; 2-83: metil N-{2-[4-(4-aminopiperidin-1-il)-3-(3,5-difluorofenil)hinolin-6-il]-4,6-difluorofenil}karbamat; 2-84: 3-{4-[trans-4-amino-3-metoksipiperidin-1-il]-3-(3,5-difluorofenil)hinolin-6-il}-2-(metoksimetoksi)benzonitril; 2-85: 6-{4-[trans-oktahidro-1H-pirido[3,4-b]morfolin-6-il]-3-(3,5-difluorofenil)hinolin-6-il}piridin-2-karboksamid; 2-86: N-{2-[4-(4-aminopiperidin-1-il)-3-(3,5-difluorofenil)hinolin-6-il]-4,6-difluorofenil}metansulfonamid; 2-92: trans-4-amino-1-[6-(3-cijano-2-hidroksifenil)-3-(3,5-difluorofenil)hinolin-4-il]piperidin-3-karbonitril; 2-94: cis-4-amino-1-[6-(3-cijano-2-hidroksifenil)-3-(3,5-difluorofenil)hinolin-4-il]piperidin-3-karbonitril; 2-99: 3-[4-(4-aminopiperidin-1-il)-3-(3,5-difluorofenil)hinolin-6-il]-4,5-difluoro-2-hidroksibenzonitril; 2-100: 3-{4-[trans-oktahidro-1H-pirido[3,4-b]morfolin-6-il]-3-(3,5-difluorofenil)hinolin-6-il}-4,5-difluoro-2-hidroksibenzonitril; 2-102: 3-{4-[trans-4-amino-3-metoksipiperidin-1-il]-3-(3,5-difluorofenil)hinolin-6-il}-4,5-difluoro-2-hidroksibenzonitril; 2-103: 3-[4-(4-aminopiperidin-1-il)-3-(3-fluoro-5-metilfenil)hinolin-6-il]-4,5-difluoro-2-hidroksibenzonitril; 2-104: 3-{4-[trans-oktahidro-1H-pirido[3,4-b]morfolin-6-il]-3-(3-fluoro-5-metilfenil)hinolin-6-il}-4,5-difluoro-2-hidroksibenzonitril; 2-106: 3-{4-[trans-4-amino-3-metoksipiperidin-1-il]-3-(3-fluoro-5-metilfenil)hinolin-6-il}-4,5-difluoro-2-hidroksibenzonitril; 2-107: 3-{4-[cis-4-amino-3-hidroksipiperidin-1-il]-3-(3-fluoro-5-metoksifenil)hinolin-6-il}-4,5-difluoro-2-hidroksibenzonitril; 2-108: 2-[4-(4-aminopiperidin-1-il)-3-(3,5-difluorofenil)hinolin-6-il]-4,6-difluoro-3-metilfenol; 2-109: 2-{4-[trans-oktahidro-1H-pirido[3,4-b]morfolin-6-il]-3-(3,5-difluorofenil)hinolin-6-il}-4,6-difluoro-3-metilfenol; 2-111: 2-{4-[trans-4-amino-3-metoksipiperidin-1-il]-3-(3,5-difluorofenil)hinolin-6-il}-4,6-difluoro-3-metilfenol; 2-112: 2-{4-[trans-4-amino-3-metoksipiperidin-1-il]-3-(3-fluoro-5-metilfenil)hinolin-6-il}-4,6-difluoro-3-metilfenol; 2-113: cis-4-amino-1-[6-(3,5-difluoro-2-hidroksi-6-metilfenil)-3-(3-fluoro-5-metoksifenil)hinolin-4-il]piperidin-3-ol; 2-114: 2-[4-(4-aminopiperidin-1-il)-3-(3,5-difluorofenil)hinolin-6-il]-4-fluoro-6-[(metoksiimino)metil]fenol; 2-115: 2-[4-(4-aminopiperidin-1-il)-3-(3-fluoro-5-metilfenil)hinolin-6-il]-6-[(metoksiimino)metil]fenol; 2-116: 2-[4-(4-aminopiperidin-1-il)-3-(3-fluoro-5-metilfenil)hinolin-6-il]-4-fluoro-6-[(metoksiimino)metil]fenol; 2-117: 2-[4-(4-aminopiperidin-1-il)-3-(3-fluoro-5-metilfenil)hinolin-6-il]-3,4-difluoro-6-[(metoksiimino)metil]fenol; 2-118: 2-{4-[trans-oktahidro-1H-pirido[3,4-b]morfolin-6-il]-3-(3-fluoro-5-metilfenil)hinolin-6-il}-4-fluoro-6-[(1E)-(metoksiimino)metil]fenol; 2-119: trans-4-amino-1-[6-(3-cijano-5,6-difluoro-2-hidroksifenil)-3-(3,5-difluorofenil)hinolin-4-il]piperidin-3-karbonitril; 2-120: cis-4-amino-1-[6-(3-cijano-5,6-difluoro-2-hidroksifenil)-3-(3,5-difluorofenil)hinolin-4-il]piperidin-3-karbonitril; 2-121: trans-4-amino-1-[6-(3-cijano-5,6-difluoro-2-hidroksifenil)-3-(3-fluoro-5-metilfenil)hinolin-4-il]piperidin-3-karbonitril; 2-122: cis-4-amino-1-[6-(3-cijano-5,6-difluoro-2-hidroksifenil)-3-(3-fluoro-5-metilfenil)hinolin-4-il]piperidin-3-karbonitril; 2-123: metil N-{2-[4-(4-aminopiperidin-1-il)-3-(3,5-difluorofenil)hinolin-6-il]-3,4,6-trifluorofenil}karbamat; 2-124: metil N-{3-[4-(4-aminopiperidin-1-il)-3-(3,5-difluorofenil)hinolin-6-il]-5-fluoropiridin-4-il}karbamat; 2-125: metil N-{3-[4-(4-aminopiperidin-1-il)-3-(3,5-difluorofenil)hinolin-6-il]-5-cijanopiridin-4-il}karbamat; 2-126: 1-[3-(3,5-difluorofenil)-6-{3-fluoro-2-[(hidroksiimino)metil]fenil}hinolin-4-il]piperidin-4-amin; 2-127: 1-(6-{3-kloro-2-[(hidroksiimino)metil]fenil}-3-(3,5-difluorofenil)hinolin-4-il)piperidin-4-amin; 2-128: 3-[4-(4-aminopiperidin-1-il)-3-(3,5-difluorofenil)hinolin-6-il]-2-[(hidroksiimino)metil] benzonitril; 2-129: 1-[3-(3,5-difluorofenil)-6-{3-fluoro-2-[(metoksiimino)metil]fenil}hinolin-4-il]piperidin-4-amin; 2-130: 1-(6-{3-kloro-2-[(metoksiimino)metil]fenil}-3-(3,5-difluorofenil)hinolin-4-il)piperidin-4-amin; 2-131: 3-[4-(4-aminopiperidin-1-il)-3-(3,5-difluorofenil)hinolin-6-il]-2-[(1E)-(metoksiimino) metil]benzonitril; 2-132: 1-{6-[3-(1-amino-2,2,2-trifluoroetil)fenil]-3-(3,5-difluorofenil)hinolin-4-il}piperidin-4-amin; 2-133: 1-{6-[2-(1-amino-2,2,2-trifluoroetil)-3-fluorofenil]-3-(3,5-difluorofenil)hinolin-4-il}piperidin-4-amin; 2-134: 2-[4-(4-aminopiperidin-1-il)-3-(3,5-difluorofenil)hinolin-6-il]-6-kloro-3,4-difluorofenol; 2-135: 2-{4-[trans-oktahidro-1H-pirido[3,4-b]morfolin-6-il]-3-(3,5-difluorofenil)hinolin-6-il}-6-kloro-3,4-difluorofenol; 2-136: 2-[4-(4-aminopiperidin-1-il)-3-(3,5-difluorofenil)hinolin-6-il]-6-kloro-4-fluorofenol; 2-137: 2-[4-(4-aminopiperidin-1-il)-3-(3,5-difluorofenil)hinolin-6-il]-6-klorofenol; 2-138: 2-{4-[trans-oktahidro-1H-pirido[3,4-b]morfolin-6-il]-3-(3,5-difluorofenil)hinolin-6-il}-6-klorofenol; 2-139: 1-{2-[4-(4-aminopiperidin-l-il)-3-(3,5-difluorofenil)hinolin-6-il]-4,6-difluorofenil}-3-metoksiurea; 2-140: 1-(2-{4-[trans-oktahidro-1H-pirido[3,4-b]morfolin-6-il]-3-(3,5-difluorofenil)hinolin-6-il}-4,6-difluorofenil)-3-metoksiurea; 2-141: 6-[4-(4-aminopiperidin-1-il)-3-(3,5-difluorofenil)hinolin-6-il]-4-kloro-2,3-dihidro-1H-1,3-benzodiazol-2-on; 2-142: 5-[4-(4-aminopiperidin-1-il)-3-(3,5-difluorofenil)hinolin-6-il]-2,3-dihidro-1,3-benzoksazol-2-on; 2-143: metil trans-4-amino-1-[6-(3-cijano-2-hidroksifenil)-3-(3,5-difluorofenil)hinolin-4-il]piperidin-3-karboksilat; 2-144: 2-{4-[trans-oktahidro-1H-pirido[3,4-b]morfolin-6-il]-3-(3,5-difluorofenil)hinolin-6-il}-6-fluorofenol; 2-146: trans-4-amino-1-[6-(3-cijano-2-hidroksifenil)-3-(3,5-difluorofenil)hinolin-4-il]piperidin-3-karboksamid; 2-147: 3-[4-(4-aminopiperidin-1-il)-3-(3,5-difluorofenil)hinolin-6-il]-5-kloro-4-fluoro-2-hidroksibenzonitril; 2-148: metil N-{2-[4-(4-aminopiperidin-1-il)-3-(3,5-difluorofenil)hinolin-6-il]-6-cijanofenil} karbamat; 2-149: trans-4-amino-1-[6-(3-cijano-2-hidroksifenil)-3-(3,5-difluorofenil)hinolin-4-il]-N-metilpiperidin-3-karboksamid; 2-150: 2-[4-(4-aminopiperidin-1-il)-3-(3,5-difluorofenil)hinolin-6-il]-3,4,6-trifluorofenol; 2-151: trans-4-amino-1-[6-(3-cijano-2-hidroksifenil)-3-(3,5-difluorofenil)hinolin-4-il]-N,N-dimetilpiperidin-3-karboksamid; 2-152: 1-[3-(3,5-difluorofenil)-6-{5-fluoro-4-[(hidroksiimino)metil]piridin-3-il}hinolin-4-il]piperidin-4-amin; 2-153: N-[(2-{4-[trans-oktahidro-1H-pirido[3,4-b]morfolin-6-il]-3-(3,5-difluorofenil)hinolin-6-il}-6-fluorofenil)metiliden]hidroksilamin; 2-154: N-[(2-{4-[(trnas)-oktahidro-1H-pirido[3,4-b]morfolin-6-il]-3-(3,5-difluorofenil)hinolin-6-il}-4,6-difluorofenil)metiliden]hidroksilamin; 2-155: N-[(2-{4-[trans-oktahidro-1H-pirido[3,4-b]morfolin-6-il]-3-(3-fluoro-5-metoksifenil)hinolin-6-il}-6-fluorofenil)metiliden]hidroksilamin; 2-156: 4-[trans-oktahidro-1H-pirido[3,4-b]morfolin-6-il]-6-[3-fluoro-2-(1H-imidazol-2-il)fenil]-3-(3-fluoro-5-metoksifenil)hinolin; 2-157: 4-[trans-oktahidro-1H-pirido[3,4-b]morfolin-6-il]-6-[3-fluoro-2-(1H-imidazol-5-il)fenil]-3-(3-fluoro-5-metoksifenil)hinolin; 2-158: 3-{4-[trans-oktahidro-1H-pirido[3,4-b]morfolin-6-il]-3-(3-fluoro-5-metoksifenil)hinolin-6-il}-4,5-difluoro-2-hidroksibenzonitril; 2-159: 3-{4-[trans-oktahidro-1H-pirido[3,4-b]morfolin-6-il]-3-(3-fluoro-5-metoksifenil)hinolin-6-il}-4,5-difluoro-2-hidroksibenzonitril; 2-160: 2-{4-[trans-oktahidro-1H-pirido[3,4-b]morfolin-6-il]-3-(3-fluoro-5-metoksifenil)hinolin-6-il}-3,4,6-trifluorofenol; 2-161: 1-[3-(3-fluoro-5-metoksifenil)-6-(2,3,5-trifluoro-6-hidroksifenil)hinolin-4-il]piperidin-4-ol; 2-162: 1- {3-[4-(4-aminopiperidin-1-il)-3-(3,5-difluorofenil)hinolin-6-il]-5-hidroksipiridin-4-il}-3-metoksiurea; 2-163: 1-{2-[4-(4-aminopiperidin-1-il)-3-(3-fluoro-5-metoksifenil)hinolin-6-il]-6-klorofenil}-3-metoksiurea; 2-164: 1-{2-[4-(4-aminopiperidin-1-il)-3-(3-fluoro-5-metoksifenil)hinolin-6-il]-4,6-difluorofenil}-3-metoksiurea; 2-165: metil N-{2-[4-(4-aminopiperidin-1-il)-3-(3-fluoro-5-metoksifenil)hinolin-6-il]-4,6-difluorofenil}karbamat; 2-166: 1-(6-{3-fluoro-2-[(hidroksiimino)metil]fenil}-3-(3-fluoro-5-metoksifenil)hinolin-4-il)piperidin-4-amin; 2-167: metil N-{2-[4-(4-aminopiperidin-1-il)-3-(3-fluoro-5-metoksifenil)hinolin-6-il]-6-cijanofenil}karbamat; 2-168: 1-(6-{5-fluoro-4-[(hidroksiimino)metil]piridin-3-il}-3-(3-fluoro-5-metilfenil)hinolin-4-il)piperidin-4-amin; 2-169: 3-[4-(4-aminopiperidin-1-il)-3-(3-fluoro-5-metilfenil)hinolin-6-il]-5-fluoropiridin-4-amin; 2-170: metil (trans)-4-amino-1-[6-(3-cijano-2-hidroksifenil)-3-(3,5-difluorofenil)hinolin-4-il]piperidin-3-karboksilat; 2-171: metil N-{3-[4-(4-ammopiperidin-1-il)-3-(3-fluoro-5-metilfenil)hinolin-6-il]-5-fluoropiridin-4-il}karbamat; 2-172: 1-{3-[4-(4-aminopiperidin-1-il)-3-(3-fluoro-5-metilfenil)hinolin-6-il]-5-fluoropiridin-4-il}-3-metoksiurea; 2-173: metil N-{2-[4-(4-ammopiperidin-1-il)-3-(3-fluoro-5-metoksifenil)hinolin-6-il]-6-fluorofenil}karbamat; 2-174: 1-{2-[4-(4-aminopiperidin-1-il)-3-(3-fluoro-5-metoksifenil)hinolin-6-il]-6-fluorofenil}-3-metoksiurea; 2-176: 1-(6-{5-fluoro-4-[(hidroksiimino)metil]piridin-3-il}-3-[3-fluoro-5-(trifluorometil)fenil] hinolin-4-il)piperidin-4-amin; 2-177: 4-amino-5-[4-(4-aminopiperidin-l-il)-3-(3,5-difluorofenil)hinolin-6-il]piridin-3-karbonitril; 2-178: 3-[4-(4-aminopiperidin-1-il)-3-(3-fluoro-5-metilfenil)hinolin-6-il]-5-fluoropiridin-2-amin; 2-179: 2-amino-3-[4-(4-aminopiperidin-1-il)-3-(3,5-difluorofenil)hinolin-6-il]-4,5-difluorobenzonitril; 2-180: metil N-{2-[4-(4-aminopiperidin-1-il)-3-(3,5-difluorofenil)hinolin-6-il]-6-cijano-3,4-difluorofenil}karbamat; 2-181: 3-[4-(4-aminopiperidin-1-il)-3-(3-fluoro-5-metilfenil)hinolin-6-il]-5-kloropiridin-4-amin; 2-182: metil N-{3-[4-(4-aminopiperidin-1-il)-3-(3-fluoro-5-metilfenil)hinolin-6-il]-5-fluoropiridin-2-il}karbamat; 2-183: 1-{3-[4-(4-aminopiperidin-1-il)-3-(3-fluoro-5-metilfenil)hinolin-6-il]-5-fluoropiridin-2-il}-3-metoksiurea; 2-184: metil N-{3-[4-(4-aminopiperidin-1-il)-3-(3-fluoro-5-metilfenil)hinolin-6-il]-5-kloropiridin-4-il}karbamat; 2-185: metil N-{2-[4-(4-aminopiperidin-1-il)-3-(3,5-difluorofenil)hinolin-6-il]-4-cijanofenil} karbamat; 2-186: 1-{3-[4-(4-aminopiperidin-1-il)-3-(3-fluoro-5-metilfenil)hinolin-6-il]-5-kloropiridin-4-il}-3-metoksiurea; 2-187: 4-amino-5-[4-(4-aminopiperidin-1-il)-3-(3-fluoro-5-metilfenil)hinolin-6-il]piridin-3-karbonitril; 2-189: 1-{2-[4-(4-aminopiperidin-1-il)-3-(3,5-difluorofenil)hinolin-6-il]-4-cijanofenil}-3-metoksiurea; 2-190: 3-{4-[(4aS,8aS)-oktahidro-1H-pirido[3,4-b]morfolin-6-il]-3-(3,5-difluorofenil)hinolin-6-il}-2-hidroksibenzonitril; 2-192: 1-(6-{5-kloro-4-[(hidroksiimino)metil]piridin-3-il}-3-(3,5-difluorofenil)hinolin-4-il)piperidin-4-amin; 2-193: 3-{4-[(4aR,8aR)-oktahidro-1H-pirido[3,4-b]morfolin-6-il]-3-(3,5-difluorofenil)hinolin-6-il}-2-hidroksibenzonitril; 2-194: 3-[4-(4-aminopiperidin-1-il)-3-(3,5-difluorofenil)hinolin-6-il]-5-fluoro-2-(metoksimetoksi)benzonitril; 2-195: 1-[3-(3,5-difluorofenil)-6-{3-[(hidroksiimino)metil]piridin-2-il}hinolin-4-il]piperidin-4-amin; 2-196: 1-[3-(3,5-difluorofenil)-6-{2-[(hidroksiimino)metil]piridin-3-il}hinolin-4-il]piperidin-4-amin; 2-197: metil N-{2-[4-(4-aminopiperidin-1-il)-3-(3-fluoro-5-metilfenil)hinolin-6-il]-4,6-difluorofenil}karbamat; 2-200: 1-[3-(3,5-difluorofenil)-6-{6-[(hidroksiimino)metil]piridin-2-il}hinolin-4-il]piperidin-4-amin; 2-202: 1-[3-(3,5-difluorofenil)-6-{3-fluoro-2-[(hidroksiimino)metil]-6-metilfenil}hinolin-4-il]piperidin-4-amin; 2-205: metil N-{2-[4-(4-ammopiperidin-1-il)-3-(3-fluoro-5-metilfenil)hinolin-6-il]-6-cijano-3,4-difluorofenil}karbamat; 2-207: 1-(2-{4-[cis-4-amino-3-metoksipiperidin-1-il]-3-(3-fluoro-5-metilfenil)hinolin-6-il}-4,6-difluorofenil)-3-metoksiurea; 2-208: 1-{2-[4-(4-aminopiperidin-1-il)-3-(3-fluoro-5-metilfenil)hinolin-6-il]-6-cijano-3,4-difluorofenil}-3-metilurea; 2-209: metil N-{2-[4-(4-aminopiperidin-1-il)-3-(3-fluoro-5-metilfenil)hinolin-6-il]-6-fluorofenil}karbamat; 2-213: 4-[4-(4-aminopiperidin-1-il)-3-(3-fluoro-5-metilfenil)hinolin-6-il]-2-[(metoksiimino) metil]fenol; 2-215: 1-{3-[4-(4-aminopiperidin-1-il)-3-(3-fluoro-5-metilfenil)hinolin-6-il]-4-metilpiridin-2-il}-3-metoksiurea; 2-217: trans-1-(6-{3-fluoro-2-[(hidroksiimino)metil]fenil}-3-(3-fluoro-5-metilfenil)hinolin-4-il)-3-metoksipiperidin-4-amin; 2-218: metil N-(2-{4-[trans-4-amino-3-metoksipiperidin-1-il]-3-(3-fluoro-5-metilfenil)hinolin-6-il}-6-cijanofenil)karbamat; 2-219: cis-3-{4-[4-amino-3-hidroksipiperidin-1-il]-3-(3-fluoro-5-metilfenil)hinolin-6-il}-5-fluoro-2-hidroksibenzonitril; 2-221: 2-{4-[trans-oktahidro-1H-pirido[3,4-b]morfolin-6-il]-3-(3-fluoro-5-metilfenil)hinolin-6-il}-6-[(metoksiimino)metil]fenol; 2-222: 1-{2-[4-(4-aminopiperidin-1-il)-3-(3-fluoro-5-metilfenil)hinolin-6-il]-4-cijanofenil}-3-metoksiurea; 2-223: 1-{3-[4-(4-aminopiperidin-1-il)-3-(3-fluoro-5-metilfenil)hinolin-6-il]-5-fluorofenil}-3-metoksiurea; 2-226: 1-{3-[4-(4-aminopiperidin-1-il)-3-(3-fluoro-5-metilfenil)hinolin-6-il]piridin-2-il}-3-metoksiurea; 2-227: cis-4-amino-1-(6-{3-fluoro-2-[(hidroksiimino)metil]fenil}-3-(3-fluoro-5-metilfenil)hinolin-4-il)piperidin-3-ol; 2-235: metil N-(2-{4-[trans-4-amino-3-metoksipiperidin-1-il]-3-(3-fluoro-5-metilfenil)hinolin-6-il}-4,6-difluorofenil)karbamat; 2-236: 1-(2-{4-[trans-4-amino-3-metoksipiperidin-1-il]-3-(3-fluoro-5-metilfenil)hinolin-6-il}-4,6-difluorofenil)-3-metoksiurea; 2-237: 1-{2-[4-(4-aminopiperidin-1-il)-3-(3-fluoro-5-metilfenil)hinolin-6-il]-4-cijano-6-fluorofenil}-3-metoksiurea; 2-239: 1-{3-[4-(4-aminopiperidin-1-il)-3-(3-fluoro-5-metilfenil)hinolin-6-il]-6-metilpiridin-2-il}-3-metoksiurea; 2-240: 1-{4-[4-(4-aminopiperidin-1-il)-3-(3-fluoro-5-metilfenil)hinolin-6-il]fenil}-3-metoksiurea; 2-241: 2-[4-(4-aminopiperidin-1-il)-3-(3,5-difluorofenil)hinolin-6-il]-6-bromo-3,4-difluorofenol; 2-243: 2- {4-[trans-oktahidro-1H-pirido[3,4-b]morfolin-6-il]-3-(3,5-difluorofenil)hinolin-6-il}-6-[(1E)-(metoksiimino)metil]fenol; 2-244: 5-{4-[trans-oktahidro-1H-pirido[3,4-b]morfolin-6-il]-3-(3,5-difluorofenil)hinolin-6-il}-4-aminopiridin-3-karbonitril; 2-246: 3-{4-[trans-oktahidro-1H-pirido[3,4-b]morfolin-6-il]-3-(3,5-difluorofenil)hinolin-6-il}piridin-2-amin; 2-247: 2-{4-[trans-oktahidro-1H-pirido[3,4-b]morfolin-6-il]-3-(3,5-difluorofenil)hinolin-6-il}-4-metilpiridin-3-amin; 2-248: 3-{4-[trans-oktahidro-1H-pirido[3,4-b]morfolin-6-il]-3-(3,5-difluorofenil)hinolin-6-il}piridin-2-ol; 2-250: 2-[4-(4-aminopiperidin-1-il)-3-(3,5-difluorofenil)hinolin-6-il]-4-metilpiridin-3-amin; 2-251: 2-{4-[trans-oktahidro-1H-pirido[3,4-b]morfolin-6-il]-3-(3,5-difluorofenil)hinolin-6-il}-3-hidroksipiridin-4-karbonitril; 2-254: 5-{4-[trans-oktahidro-1H-pirido[3,4-b]morfolin-6-il]-3-(3,5-difluorofenil)hinolin-6-il}-4-hidroksipiridin-3-karbonitril; 2-256: 3-{4-[trans-oktahidro-1H-pirido[3,4-b]morfolin-6-il]-3-(3,5-difluorofenil)hinolin-6-il}-5-fluoropiridin-4-ol; 2-258: 2-{4-[trans-oktahidro-1H-pirido[3,4-b]morfolin-6-il]-3-(3,5-difluorofenil)hinolin-6-il}-4-metilpiridin-3-ol; 2-259: 3-{4-[trans-oktahidro-1H-pirido[3,4-b]morfolin-6-il]-3-(3,5-difluorofenil)hinolin-6-il}-5-fluoropiridin-2-ol; 2-261: 2-{4-[trans-oktahidro-1H-pirido[3,4-b]morfolin-6-il]-3-(3,5-difluorofenil)hinolin-6-il}-3-fluoropiridin-4-karbonitril; 2-262: 2-{4-[trans-oktahidro-1H-pirido[3,4-b]morfolin-6-il]-3-(3,5-difluorofenil)hinolin-6-il}-3-aminopiridin-4-karbonitril; 2-263: 2-{4-[trans-oktahidro-1H-pirido[3,4-b]morfolin-6-il]-3-(3,5-difluorofenil)hinolin-6-il}piridin-3-ol; 2-264: N-[(3-{4-[trans-oktahidro-1H-pirido[3,4-b]morfolin-6-il]-3-(3,5-difluorofenil)hinolin-6-il}piridin-2-il)metiliden]hidroksilamin; 2-265: 2-{4-[trans-oktahidro-1H-pirido[3,4-b]morfolin-6-il]-3-(3,5-difluorofenil)hinolin-6-il}-5-fluoropiridin-3-amin; 2-266: 3-4-[trans-oktahidro-1H-pirido [3,4-b] morfolin-6-il]-3-(3,5-difluorofenil)hinolin-6-il}-5-[(metoksiimino)metil]piridin-4-amin; 2-269: 2- {4-[trans-oktahidro-1H-pirido [3,4-b] morfolin-6-il]-3-(3,5-difluorofenil)hinolin-6-il}-4-[(metoksiimino)metil]piridin-3-amin; 2-273: 1-(3-{4-[trans-oktahidro-1H-pirido [3,4-b] morfolin-6-il]-3-(3,5-difluorofenil)hinolin-6-il}piridin-2-il)-3-metoksiurea; 2-275: 2- {4-[trans-oktahidro-1H-pirido[3,4-b]morfolin-6-il]-3-(3,5-difluorofenil)hinolin-6-il}-4-kloropiridin-3-amin; 2-283: 2-{4-[trans-oktahidro-1H-pirido[3,4-b]morfolin-6-il]-3-(3,5-difluorofenil)hinolin-6-il}piridin-3-amin; 2-284: 2-{4-[trans-oktahidro-1H-pirido[3,4-b]morfolin-6-il]-3-(3,5-difluorofenil)hinolin-6-il}-4-metoksipiridin-3-amin; 2-285: 2-{4-[(4αR,8αR)-oktahidro-1H-pirido[3,4-b]morfolin-6-il]-3-(3,5-difluorofenil)hinolin-6-il}-6-[(metoksiimino)metil]fenol; 2-286: 2-{4-[(4aS,8aS)-oktahidro-1H-pirido[3,4-b]morfolin-6-il]-3-(3,5-difluorofenil)hinolin-6-il}-6-[(metoksiimino)metil]fenol; 2-287: 2-{4-[(4aR,8aR)-oktahidro-1H-pirido[3,4-b]morfolin-6-il]-3-(3,5-difluorofenil)hinolin-6-il}-4-[(metoksiimino)metil]piridin-3-amin; 2-288: 2-{4-[(4aS,8aS)-oktahidro-1H-pirido[3,4-b]morfolin-6-il]-3-(3,5-difluorofenil)hinolin-6-il}-4-[(metoksiimino)metil]piridin-3-amin; 2-289: 2-{4-[(4αR,8αR)-oktahidro-1H-pirido[3,4-b]morfolin-6-il]-3-(3,5-difluorofenil)hinolin-6-il}-3-aminopiridin-4-karbonitril; 2-290: 2-{4-[(4aS,8aS)-oktahidro-1H-pirido[3,4-b]morfolin-6-il]-3-(3,5-difluorofenil)hinolin-6-il}-3-aminopiridin-4-karbonitril; 2-291: (5-{4-[(4aR,8aR)-oktahidro-1H-pirido[3,4-b]morfolin-6-il]-3-(3,5-difluorofenil)hinolin-6-il}-4-aminopiridin-3-karbonitril; 2-292: (5-{4-[(4αS,8αS)-oktahidro-1H-pirido[3,4-b]morfolin-6-il]-3-(3,5-difluorofenil)hinolin-6-il}-4-aminopiridin-3-karbonitril; 2-293: 3-{4-[(4αR,8αR)-oktahidro-1H-pirido[3,4-b]morfolin-6-il]-3-(3,5-difluorofenil)hinolin-6-il}piridin-2-amin; 2-294: 3-{4-[(4aS,8aS)-oktahidro-1H-pirido[3,4-b]morfolin-6-il]-3-(3,5-difluorofenil)hinolin-6-il}piridin-2-amin; 2-295: 2-{4-[(4αR,8αR)-oktahidro-1H-pirido[3,4-b]morfolin-6-il]-3-(3,5-difluorofenil)hinolin-6-il}-4-metilpiridin-3 -amin; 2-296: 2-{4-[(4αS,8αS)-oktahidro-1H-pirido[3,4-b]morfolin-6-il]-3-(3,5-difluorofenil)hinolin-6-il}-4-metilpiridin-3-amin; 2-297: 2-{4-[(4αR,8αR)-oktahidro-1H-pirido[3,4-b]morfolin-6-il]-3-(3,5-difluorofenil)hinolin-6-il}-4-metilpiridin-3-ol; 2-298: 2-{4-[(4aS,8aS)-oktahidro-1H-pirido[3,4-b]morfolin-6-il]-3-(3,5-difluorofenil)hinolin-6-il}-4-metilpiridin-3-ol; 2-299: 3-{4-[(4αR,8αR)-oktahidro-1H-pirido[3,4-b]morfolin-6-il]-3-(3,5-difluorofenil)hinolin-6-il}-5-fluoro-2-hidroksibenzonitril; 2-300: 3-{4-[(4αS,8αS)-oktahidro-1H-pirido[3,4-b]morfolin-6-il]-3-(3,5-difluorofenil)hinolin-6-il}-5-fluoro-2-hidroksibenzonitril; ili njegova farmaceutski prihvatljiva sol, solvat, dijastereomerna mješavina, ili pojedinačni enantiomeri.
11. Spoj prema patentnom zahtjevu 1, naznačen time što, spoj je: 3-1: 3-[8-(4-aminopiperidin-1-il)-7-(3-fluoro-5-metilfenil)-1,5-naftiridin-2-il]-5-fluorobenzamid; 3-2: 3-[8-(4-aminopiperidin-1-il)-7-(3-fluoro-5-metilfenil)-1,5-naftiridin-2-il]-5-fluoro-2-hidroksibenzonitril; 3-3: 4-[8-(4-aminopiperidin-1-il)-7-(3-fluoro-5-metilfenil)-1,5-naftiridin-2-il]-6-fluoro-2,3-dihidro-1H-1,3-benzodiazol-2-on; 3-4: 5-[8-(4-aminopiperidin-1-il)-7-(3-fluoro-5-metilfenil)-1,5-naftiridin-2-il]-2,3-dihidro-1H-1,3-benzodiazol-2-on; 3-5: 6-[8-(4-aminopiperidin-1-il)-7-(3-fluoro-5-metilfenil)-1,5-naftiridin-2-il]-4-fluoro-2,3-dihidro-1H-1,3-benzodiazol-2-on; 3-6: 3-[8-(4-aminopiperidin-1-il)-7-(3-kloro-5-metilfenil)-1,5-naftiridin-2-il]-5-fluoro-2-hidroksibenzonitril; 3-7: 3-[8-(4-aminopiperidin-1-il)-7-(3-fluoro-5-metilfenil)-1,5-naftiridin-2-il]-2-hidroksibenzonitril; 3-8: 2-[8-(4-aminopiperidin-1-il)-7-(3-fluoro-5-metilfenil)-1,5-naftiridin-2-il]-6-fluorofenol; 3-9: 6-[8-(4-aminopiperidin-1-il)-7-(3,5-difluorofenil)-1,5-naftiridin-2-il]-4-fluoro-2,3-dihidro-1H-1,3-benzodiazol-2-on; 3-10: 6-{8-[trans-oktahidro-1H-pirido[3,4-b]morfolin-6-il]-7-(3,5-difluorofenil)-1,5-naftiridin-2-il}-4-fluoro-2,3-dihidro-1H-1,3-benzodiazol-2-on; 3-11: 4-{8-[trans-oktahidro-1H-pirido[3,4-b]morfolin-6-il]-7-(3-fluoro-5-metilfenil)-1,5-naftiridin-2-il}-6-fluoro-2,3-dihidro-1H-1,3-benzodiazol-2-on; 3-12: 4-{8-[trans-oktahidro-1H-pirido[3,4-b]morfolin-6-il]-7-(3,5-difluorofenil)-1,5-naftiridin-2-il}-1H,2H,3H-imidazo[4,5-c]piridin-2-on; ili njegova farmaceutski prihvatljiva sol, solvat, dijastereomerna mješavina, ili pojedinačni enantiomeri.
12. Spoj prema patentnom zahtjevu 1, naznačen time što, spoj je: 4-1: 3-[5-(4-aminopiperidin-1-il)-6-(3,5-difluorofenil)-1,8-naftiridin-3-il]-2-hidroksibenzonitril; 4-2: 3-[5-(4-aminopiperidin-1-il)-6-(3-fluoro-5-metilfenil)-1,8-naftiridin-3-il]-2-hidroksibenzonitril; 4-3: 3-[5-(4-aminopiperidin-1-il)-6-(3-fluoro-5-metilfenil)-1,8-naftiridin-3-il]-5-fluoro-2-hidroksibenzonitril; 4-4: 3-[5-(4-aminopiperidin-1-il)-6-(3-kloro-5-metilfenil)-1,8-naftiridin-3-il]-2-hidroksibenzonitril; 4-5: 3-{5-[(4αR,8αR)-oktahidro-1H-pirido[3,4-b]morfolin-6-il]-6-(3-fluoro-5-metilfenil)-1,8-naftiridin-3-il}-2-hidroksibenzonitril; 4-6: 3-{5-[(4αS,8αS)-oktahidro-1H-pirido[3,4-b]morfolin-6-il]-6-(3-fluoro-5-metilfenil)-1,8-naftiridin-3-il}-2-hidroksibenzonitril; 4-7: 3-{5-[(4αR,8αR)-oktahidro-1H-pirido[3,4-b]morfolin-6-il]-6-(3-fluoro-5-metilfenil)-1,8-naftiridin-3-il}-5-fluoro-2-hidroksibenzonitril; 4-8: 3-{5-[(4αS,8αS)-oktahidro-1H-pirido[3,4-b]morfolin-6-il]-6-(3-fluoro-5-metilfenil)-1,8-naftiridin-3-il}-5-fluoro-2-hidroksibenzonitril; 4-9: 3-{5-[(4αR,8αR)-oktahidro-1H-pirido[3,4-b]morfolin-6-il]-6-(3,5-difluorofenil)-1,8-naftiridin-3-il}-5-fluoro-2-hidroksibenzonitril; 4-10: 3-{5-[(4αS,8αS)-oktahidro-1H-pirido[3,4-b]morfolin-6-il]-6-(3,5-difluorofenil)-1,8-naftiridin-3-il}-5-fluoro-2-hidroksibenzonitril; 4-11: 2-{5-[(4αR,8αR)-oktahidro-1H-pirido[3,4-b]morfolin-6-il]-6-(3-fluoro-5-metilfenil)-1,8-naftiridin-3-il}-3-aminopiridin-4-karbonitril; 4-12: 2-{5-[(4aS,8aS)-oktahidro-1H-pirido[3,4-b]morfolin-6-il]-6-(3-fluoro-5-metilfenil)-1,8-naftiridin-3-il}-3-aminopiridin-4-karbonitril; 4-13: 5-{5-[(4αR,8αR)-oktahidro-1H-pirido[3,4-b]morfolin-6-il]-6-(3,5-difluorofenil)-1,8-naftiridin-3-il}-4-aminopiridin-3-karbonitril; 4-14: 5-{5-[(4αS,8αS)-oktahidro-1H-pirido[3,4-b]morfolin-6-il]-6-(3,5-difluorofenil)-1,8-naftiridin-3-il}-4-aminopiridin-3-karbonitril; 4-15: 2-{5-[(4αR,8αR)-oktahidro-1H-pirido[3,4-b][1,4]oksazin-6-il]-6-(3-fluoro-5-metilfenil)-1,8-naftiridin-3-il}-3-aminopiridin-4-karbonitril; 4-16: 2-{5-[(4αS,8αS)-oktahidro-1H-pirido[3,4-b][1,4]oksazin-6-il]-6-(3-fluoro-5-metilfenil)-1,8-naftiridin-3-il}-3-aminopiridin-4-karbonitril; 4-17: 2-{5-[(4αR,8αR)-oktahidro-1H-pirido[3,4-b][1,4]oksazin-6-il]-6-(3-kloro-5-fluorofenil)-1,8-naftiridin-3-il}-3-aminopiridin-4-karbonitril; 4-18: 2-{5-[(4αS,8αS)-oktahidro-1H-pirido[3,4-b][1,4]oksazin-6-il]-6-(3-kloro-5-fluorofenil)-1,8-naftiridin-3-il}-3-aminopiridin-4-karbonitril; 4-19: 2-{5-[(4αR,8αR)-oktahidro-1H-pirido[3,4-b][1,4]oksazin-6-il]-6-(3-kloro-5-metilfenil)-1,8-naftiridin-3-il}-3-aminopiridin-4-karbonitril; 4-20: 2-{5-[(4aS,8aS)-oktahidro-1H-pirido[3,4-b][1,4]oksazin-6-il]-6-(3-kloro-5-metilfenil)-1,8-naftiridin-3-il}-3-aminopiridin-4-karbonitril; 4-21: 2-{5-[(4αR,8αR)-oktahidro-1H-pirido[3,4-b][1,4]oksazin-6-il]-6-(3,5-difluorofenil)-1,8-naftiridin-3-il}-4-[(metoksiimino)metil]piridin-3-amin; 4-22: 2-{5-[(4αS,8αS)-oktahidro-1H-pirido[3,4-b][1,4]oksazin-6-il]-6-(3,5-difluorofenil)-1,8-naftiridin-3-il}-4-[(metoksiimino)metil]piridin-3-amin; 4-23: 2-{5-[(4αR,8αR)-oktahidro-1lH-pirido[3,4-b][1,4]oksazin-6-il]-6-(3-kloro-5-metilfenil)-1,8-naftiridin-3-il}-4-[(metoksiimino)metil]piridin-3-amin; 4-24: 2-{5-[(4αS,8αS)-oktahidro-1H-pirido[3,4-b][1,4]oksazin-6-il]-6-(3-kloro-5-metilfenil)-1,8-naftiridin-3-il}-4-[(metoksiimino)metil]piridin-3-amin; 4-25: 3-{5-[(4αR,8αR)-oktahidro-1H-pirido[3,4-b][1,4]oksazin-6-il]-6-(3,5-difluorofenil)-1,8-naftiridin-3-il}-2-hidroksibenzonitril; 4-26: 3-{5-[(4αS,8αS)-oktahidro-1H-pirido[3,4-b][1,4]oksazin-6-il]-6-(3,5-difluorofenil)-1,8-naftiridin-3-il}-2-hidroksibenzonitril; 4-27: 3-{5-[(4αR,8αR)-oktahidro-1H-pirido[3,4-b][1,4]oksazin-6-il]-6-(3-kloro-5-fluorofenil)-1,8-naftiridin-3-il}-2-hidroksibenzonitril; 4-28: 3-{5-[(4αS,8αS)-oktahidro-1H-pirido[3,4-b][1,4]oksazin-6-il]-6-(3-kloro-5-fluorofenil)-1,8-naftiridin-3-il}-2-hidroksibenzonitril; 4-29: 3-{5-[(4αR,8αR)-oktahidro-1H-pirido[3,4-b][1,4]oksazin-6-il]-6-(3-fluoro-5-metoksifenil)-1,8-naftiridin-3-il}-2-hidroksibenzonitril; 4-30: 3-{5-[(4αS,8αS)-oktahidro-1H-pirido[3,4-b][1,4]oksazin-6-il]-6-(3-fluoro-5-metoksifenil)-1,8-naftiridin-3-il}-2-hidroksibenzonitril; 4-31: 3-{5-[(4αR,8αR)-oktahidro-1H-pirido[3,4-b][1,4]oksazin-6-il]-6-(3-kloro-5-metilfenil)-1,8-naftiridin-3-il}-2-hidroksibenzonitril; 4-32: 3-{5-[(4αS,8αS)-oktahidro-1H-pirido[3,4-b][1,4]oksazin-6-il]-6-(3-kloro-5-metilfenil)-1,8-naftiridin-3-il}-2-hidroksibenzonitril; 4-33: 3-{5-[(4αR,8αR)-oktahidro-1H-pirido[3,4-b][1,4]oksazin-6-il]-6-(3,5-diklorofenil)-1,8-naftiridin-3-il}-2-hidroksibenzonitril; 4-34: 3-{5-[(4αS,8αS)-oktahidro-1H-pirido[3,4-b][1,4]oksazin-6-il]-6-(3,5-diklorofenil)-1,8-naftiridin-3-il}-2-hidroksibenzonitril; 4-35: 3-{5-[(4αR,8αR)-oktahidro-1H-pirido[3,4-b][1,4]oksazin-6-il]-6-(3,5-difluorofenil)-1,8-naftiridin-3-il}piridin-2-amin; 4-36: 3-{5-[(4αS,8αS)-oktahidro-1H-pirido[3,4-b][1,4]oksazin-6-il]-6-(3,5-difluorofenil)-1,8-naftiridin-3-il}piridin-2-amin; 4-37: 3-{5-[(4αR,8αR)-oktahidro-1H-pirido[3,4-b][1,4]oksazin-6-il]-6-(3-fluoro-5-metilfenil)-1,8-naftiridin-3-il}piridin-2-amin; 4-38: 3-{5-[(4αS,8αS)-oktahidro-1H-pirido[3,4-b][1,4]oksazin-6-il]-6-(3-fluoro-5-metilfenil)-1,8-naftiridin-3-il}piridin-2-amin; 4-39: 3-{5-[(4αR,8αR)-oktahidro-1H-pirido[3,4-b][1,4]oksazin-6-il]-6-(3-fluoro-5-metoksifenil)-1,8-naftiridin-3-il}piridin-2-amin; 4-40: 3-{5-[(4αS,8αS)-oktahidro-1H-pirido[3,4-b][1,4]oksazin-6-il]-6-(3-fluoro-5-metoksifenil)-1,8-naftiridin-3-il}piridin-2-amin; 4-41: 3-{5-[(4αR,8αR)-oktahidro-1H-pirido[3,4-b][1,4]oksazin-6-il]-6-(3-kloro-5-fluorofenil)-1,8-naftiridin-3-il}piridin-2-amin; 4-42: 3-{5-[(4αS,8αS)-oktahidro-1H-pirido[3,4-b][1,4]oksazin-6-il]-6-(3-kloro-5-fluorofenil)-1,8-naftiridin-3-il}piridin-2-amin; 4-43: 3-{5-[(4αR,8αR)-oktahidro-1H-pirido[3,4-b][1,4]oksazin-6-il]-6-(3-kloro-5-metilfenil)-1,8-naftiridin-3-il}piridin-2-amin; 4-44: 3-{5-[(4αS,8αS)-oktahidro-1H-pirido[3,4-b][1,4]oksazin-6-il]-6-(3-kloro-5-metilfenil)-1,8-naftiridin-3-il}piridin-2-amin; 4-45: 3-{5-[(4αR,8αR)-oktahidro-1H-pirido[3,4-b][1,4]oksazin-6-il]-6-(3,5-diklorofenil)-1,8-naftiridin-3-il}piridin-2-amin; 4-46: 3-{5-[(4αS,8αS)-oktahidro-1H-pirido[3,4-b][1,4]oksazin-6-il]-6-(3,5-diklorofenil)-1,8-naftiridin-3-il}piridin-2-amin; ili njegova farmaceutski prihvatljiva sol, solvat, dijastereomerna mješavina, ili pojedinačni enantiomeri.
13. Spoj prema patentnom zahtjevu 1, naznačen time što spoj ima sljedeću strukturu: [image] ili njegova farmaceutski prihvatljiva sol, ili solvat.
14. Farmaceutski pripravak koji sadrži spoj prema bilo kojem od patentnih zahtjeva 1 do 12, ili njegovu farmaceutski prihvatljivu sol, solvat, dijastereomernu mješavinu ili pojedinačne enantiomere, i najmanje jedan farmaceutski prihvatljiv ekscipijens.
15. Farmaceutski pripravak koji sadrži spoj prema patentnom zahtjevu 13, ili njegovu farmaceutski prihvatljivu sol ili solvat, i najmanje jedan farmaceutski prihvatljiv ekscipijens.
16. Farmaceutski pripravak prema patentnom zahtjevu 14 ili patentnom zahtjevu 15, naznačen time što je farmaceutski pripravak u obliku tablete, pilule ili kapsule.
17. Spoj prema bilo kojem od patentnih zahtjeva 1 do 12, ili njegova farmaceutski prihvatljiva sol, solvat, dijastereomerna mješavina, ili pojedinačni enantiomeri, za uporabu kao lijek.
18. Spoj prema patentnom zahtjevu 13, ili njegova farmaceutski prihvatljiva sol ili solvat, za uporabu kao lijek.
19. Spoj prema bilo kojem od patentnih zahtjeva 1 do 12, ili njegova farmaceutski prihvatljiva sol, solvat, dijastereomerna mješavina, ili pojedinačni enantiomeri, za uporabu u liječenju akromegalije, neuroendokrinog tumora, oftalmičke bolesti ili stanja, neuropatije, nefropatije, respiratorne bolesti ili stanja, raka, bola, neurodegenerativne bolesti ili stanja, upalne bolesti ili stanja, psihijatrijske bolesti ili stanja ili njihovih kombinacija.
20. Spoj prema patentnom zahtjevu 13, ili njegova farmaceutski prihvatljiva sol ili solvat, za uporabu u liječenju akromegalije, neuroendokrinog tumora, oftalmičke bolesti ili stanja, neuropatije, nefropatije, respiratorne bolesti ili stanja, raka, bola, neurodegenerativne bolesti ili stanja, upalne bolesti ili stanja, psihijatrijske bolesti ili stanja ili njihovih kombinacija.
21. Farmaceutski pripravak prema bilo kojem od patentnih zahtjeva 14 do 16 za uporabu u liječenju akromegalije, neuroendokrinog tumora, oftalmičke bolesti ili stanja, neuropatije, nefropatije, respiratorne bolesti ili stanja, raka, bola, neurodegenerativne bolesti ili stanja, upalne bolesti ili stanja, psihijatrijske bolesti ili stanja ili njihovih kombinacija.
22. Spoj prema bilo kom od patentnih zahtjeva 1 do 12, ili njegova farmaceutski prihvatljiva sol, solvat, dijastereomerna mješavina, ili pojedinačni enantiomeri, za uporabu u liječenju akromegalije, neuroendokrinog tumora ili njihovih kombinacija.
23. Spoj prema patentnom zahtjevu 13, ili njegova farmaceutski prihvatljiva sol ili solvat, za uporabu u liječenju akromegalije, neuroendokrinog tumora ili njihovih kombinacija.
24. Farmaceutski pripravak prema bilo kojem od patentnih zahtjeva 14 do 16 za uporabu u liječenju akromegalije, neuroendokrinog tumora ili njihovih kombinacija.
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