HRP20151036T1 - Novi derivati (heterocikal/tetrahidropiridin)-(piperazinil)-1-alkanon i (heterocikal/dihidropirolidin)-(piperazinil)-1-alkanon, i njihova uporaba kao inhibitora p75 - Google Patents

Novi derivati (heterocikal/tetrahidropiridin)-(piperazinil)-1-alkanon i (heterocikal/dihidropirolidin)-(piperazinil)-1-alkanon, i njihova uporaba kao inhibitora p75 Download PDF

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HRP20151036T1
HRP20151036T1 HRP20151036TT HRP20151036T HRP20151036T1 HR P20151036 T1 HRP20151036 T1 HR P20151036T1 HR P20151036T T HRP20151036T T HR P20151036TT HR P20151036 T HRP20151036 T HR P20151036T HR P20151036 T1 HRP20151036 T1 HR P20151036T1
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Croatia
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compound
pyridin
dihydro
ethanone
thiophen
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HRP20151036TT
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Marco Baroni
Françoise Bono
Sandrine Delbary-Gossart
Valentina Vercesi
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Sanofi
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Claims (13)

1. Spoj koji odgovara formuli (I): [image] u kojoj: - n predstavlja 1 ili 2; - m predstavlja 0 ili 1; - A predstavlja kondenziranu heterocikličku skupinu s formulom (Y) [image] i B predstavlja vodikov atom; ili A predstavlja vodikov atom; i B predstavlja kondenziranu heterocikličku skupinu s formulom (Y) [image] kondenzirani heterocikal s formulom Y može biti spojen na ostatak molekule preko bilo kojeg od dostupnih atoma ugljika, i u kojoj: - U upotpunjuje: - bilo aromatsku ili zasićenu 6-atomsku jezgru, koja sadrži jedan ili dva atoma dušika, te jezgra može biti supstituirana s jednim ili dva halogena atoma, jednom ili dvije (C1-C4)alkil ili (C1-C4)alkoksi skupine, ili jednim ili dva perfluoroalkil radikala; - ili aromatsku ili zasićenu 5-atomsku jezgru, koja sadrži atom dušika, kisika ili sumpora, te jezgra može biti supstituirana s jednom ili dvije skupine (C1-C4)alkil; - X i X1 predstavljaju CH ili N; - R i R1 koji se nalaze na bilo kojem od dostupnih položaja, neovisno predstavljaju vodikov atom, halogeni atom, skupinu (C1-C4)alkil, (C1-C4)alkoksi, perfluoroalkil ili trifluorometoksi radikal, cijano ili skupinu COOH, COOalkil, CONR3R4 ili NHCOR3; - -W- je heterocikal s dušikom, odabran od: -W- = [image] - 1-2 predstavlja 1 ili 2; - 1-3 predstavlja 1, 2 ili 3; - R2 predstavlja skupinu s formulom: [image] - u kojoj R5 i R6, koji se nalaze na bilo kojem od dostupnih položaja, neovisno predstavljaju vodikov atom, halogeni atom, skupinu (C1-C4)alkil ili (C1-C4)alkoksi, trifluorometil ili trifluorometoksi radikal, cijano ili skupinu COOH, COOalkil, COOcikloalkil, SOalkil, SO2alkil, CONR3R4, NR3R4 ili NHCOR3; ili jedna od skupina R5 i R6 može također predstavljati heterocikal odabran od: [image] [image] - Z predstavlja atom kisika ili sumpora; - R3 i R4 predstavljaju vodik ili skupinu (C1-C6) alkil; u obliku baze ili kisele adicijske soli.
2. Spoj prema zahtjevu 1, naznačen time da - A predstavlja kondenziranu heterocikličku skupinu s formulom (Y) [image] i B predstavlja vodikov atom; ili A predstavlja vodikov atom; i B predstavlja kondenziranu heterocikličku skupinu s formulom (Y) [image] kondenzirani heterocikal s formulom Y eventualno može biti vezan na ostatak molekule preko bilo kojeg od dostupnih atoma ugljika benzenske jezgre; u obliku baze ili kisele adicijske soli.
3. Spoj prema bilo kojem od zahtjeva 1 i 2, naznačen time da R i R1 koji se nalaze na bilo kojem od dostupnih položaja, neovisno predstavljaju vodikov atom, halogeni atom ili skupinu (C1-C4)alkil ili COOalkil; u obliku baze ili kisele adicijske soli.
4. Spoj prema jednom od zahtjeva 1 do 3, naznačen time da: - -W- je heterocikal s dušikom, odabran od: -W- = [image] - R3 i R4 predstavljaju vodikov atom ili metilnu skupinu; u obliku baze ili kisele adicijske soli.
5. Spoj prema jednom od zahtjeva 1 do 4, naznačen time da: - R2 predstavlja skupinu s formulom: [image] - R5 i R6, koji se nalaze na bilo kojem od dostupnih položaja, neovisno predstavljaju vodikov atom, trifluorometil radikal ili skupinu COOH, COOalkil ili COOcikloalkil; ili jedna od skupina R5 i R6 može također predstavljati heterocikal odabran od: [image] - Z predstavlja atom kisika ili sumpora; i/ili - R3 i R4 predstavljaju vodik ili metilnu skupinu; u obliku baze ili kisele adicijske soli.
6. Spoj prema bilo kojem od zahtjeva 1 do 5, naznačen time da je odabran iz skupa koji čine: - Spoj 1: 1-(4-benzo[b]tiofen-7-il-3,6-dihidro-2H-piridin-1-il)-2-(3,5-dimetil-2,3,5,6-tetrahidro[1,2']bipirazinil-4-il)etanon; - Spoj 2: 1-(4-benzo[b]tiofen-7-il-3,6-dihidro-2H-piridin-1-il)-2-(8-pirimidin-2-il-3,8-diazabiciklo[3.2.1]okt-3-il)etanon; - Spoj 3: 1-(4-benzo[b]tiofen-5-il-3,6-dihidro-2H-piridin-1-il)-2-(8-pirimidin-2-il-3,8-diazabiciklo[3.2.1]okt-3-il)etanon; - Spoj 4: 1-(4-benzo[b]tiofen-7-il-3,6-dihidro-2H-piridin-1-il)-2-[(2S,6R)-2,6-dimetil-4-(5-trifluorometilpiridin-2-il)piperazin-1-il]etanon; - Spoj 5: 1-(4-benzo[b]tiofen-5-il-3,6-dihidro-2H-piridin-1-il)-2-((2S,5R)-2,5-dimetil-2,3,5,6-tetrahidro[1,2']bipirazinil-4-il)etanon; - Spoj 6: 1-(4-benzo[b]tiofen-7-il-3,6-dihidro-2H-piridin-1-il)-2-((2S,5R)-2,5-dimetil-2,3,5,6-tetrahidro[1,2']bipirazinil-4-il)etanon; - Spoj 7: 1-(4-benzo[b]tiofen-5-il-3,6-dihidro-2H-piridin-1-il)-2-[(2S,6R)-2,6-dimetil-4-(5-trifluorometilpiridin-2-il)piperazin-1-il]etanon; - Spoj 8: 1-(4-benzo[b]tiofen-7-il-3,6-dihidro-2H-piridin-1-il)-2-[8-(5-trifluorometilpiridin-2-il)-3,8-diazabiciklo[3.2.1]okt-3-il]etanon; - Spoj 9: 1-(4-benzo[b]tiofen-7-il-3,6-dihidro-2H-piridin-1-il)-2-[(2R,5S)-2,5-dimetil-4-(5-trifluorometilpiridin-2-il)piperazin-1-il]etanon; - Spoj 10: 2-[(2S,6R)-2,6-dimetil-4-(5-trifluorometilpiridin-2-il)piperazin-1-il]-1-[4-(2-metilbenzo[b]tiofen-7-il)-3,6-dihidro-2H-piridin-1-il]etanon; - Spoj 11: 2-[(2S,6R)-2,6-dimetil-4-(5-trifluorometilpiridin-2-il)piperazin-1-il]-1-[4-(2-propilbenzo[b]tiofen-7-il)-3,6-dihidro-2H-piridin-1-il]etanon; - Spoj 12: 1-(4-benzo[b]tiofen-7-il-3,6-dihidro-2H-piridin-1-il)-2-[5-(5-trifluorometilpiridin-2-il)-2,5-diazabiciklo[2.2.1]hept-2-il]etanon; - Spoj 13: 1-(4-benzo[b]tiofen-6-il-3,6-dihidro-2H-piridin-1-il)-2-[(2R,5S)-2,5-dimetil-4-(5-trifluorometilpiridin-2-il)piperazin-1-il]etanon; - Spoj 14: 1-(4-benzofuran-7-il-3,6-dihidro-2H-piridin-1-il)-2-[(2R,5S)-2,5-dimetil-4-(5-trifluorometilpiridin-2-il)piperazin-1-il]etanon; - Spoj 15: 1-[4-(2-metilbenzo[b]tiofen-5-il)-3,6-dihidro-2H-piridin-1-il]-2-(8-pirimidin-2-il-3,8-diazabiciklo[3.2.1]okt-3-il)etanon; - Spoj 16: 1-[4-(2-metilbenzo[b]tiofen-5-il)-3,6-dihidro-2H-piridin-1-il]-2-[4-(5-trifluorometilpiridin-2-il)piperazin-1-il]etanon; - Spoj 17: 4-{2-[4-(2-metilbenzo[b]tiofen-5-il)-3,6-dihidro-2H-piridin-1-il]-2-oksoetil}-1-(5-trifluorometilpiridin-2-il)piperazin-2-on; - Spoj 18: 2-[(2S,6R)-2,6-dimetil-4-(5-trifluorometilpiridin-2-il)piperazin-1-il]-1-[4-(2-metilbenzo[b]tiofen-5-il)-3,6-dihidro-2H-piridin-1-il]etanon; - Spoj 19: 1-(4-benzo[b]tiofen-7-il-3,6-dihidro-2H-piridin-1-il)-2-((2S,6R)-2,6-dimetil-4-kinolin-2-ilpiperazin-1-il)etanon; - Spoj 20: 1-(4-kinolin-8-il-3,6-dihidro-2H-piridin-1-il)-2-[4-(5-trifluorometilpiridin-2-il)piperazin-1-il]etanon; - Spoj 21: 1-[4-(2,3-dihidrobenzo[1,4]dioksin-6-il)-3,6-dihidro-2H-piridin-1-il]-2-[4-(5-trifluorometilpiridin-2-il)piperazin-1-il]etanon; - Spoj 22: 2-[8-(5-fluoropirimidin-2-il)-3,8-diazabiciklo[3.2.1]okt-3-il]-1-[4-(2-metilbenzo[b]tiofen-5-il)-3,6-dihidro-2H-piridin-1-il]etanon; - Spoj 23: 1-(4-benzofuran-7-il-3,6-dihidro-2H-piridin-1-il)-2-[8-(5-fluoropirimidin-2-il)-3,8-diazabiciklo[3.2.1]okt-3-il]etanon; - Spoj 24: 1-[4-(2,3-dihidrobenzo[1,4]dioksin-6-il)-3,6-dihidro-2H-piridin-1-il]-2-[8-(5-fluoropirimidin-2-il)-3,8-diazabiciklo[3.2.1]okt-3-il]etanon; - Spoj 25: 2-[8-(5-fluoropirimidin-2-il)-3,8-diazabiciklo[3.2.1]okt-3-il]-1-(4-thieno[3,2-c]piridin-4-il-3,6-dihidro-2H-piridin-1-il)etanon; - Spoj 26: 1-(4-benzofuran-3-il-3,6-dihidro-2H-piridin-1-il)-2-[8-(5-fluoropirimidin-2-il)-3,8-diazabiciklo[3.2.1]okt-3-il]etanon; - Spoj 27: 2-[8-(5-fluoropirimidin-2-il)-3,8-diazabiciklo[3.2.1]okt-3-il]-1-[4-(1H-indol-3-il)-3,6-dihidro-2H-piridin-1-il]etanon; - Spoj 28: 1-[4-(6-fluoro-1H-indol-3-il)-3,6-dihidro-2H-piridin-1-il]-2-[8-(5-fluoropirimidin-2-il)-3,8-diazabiciklo[3.2.1]okt-3-il]etanon; - Spoj 29: 1-(4-benzo[b]tiofen-3-il-3,6-dihidro-2H-piridin-1-il)-2-[8-(5-fluoropirimidin-2-il)-3,8-diazabiciklo[3.2.1]okt-3-il]etanon; - Spoj 30: 4-{2-[4-(1H-indol-3-il)-3,6-dihidro-2H-piridin-1-il]-2-oksoetil}-1-(5-trifluorometilpiridin-2-il)piperazin-2-on; - Spoj 31: 4-[2-(4-benzo[b]tiofen-7-il-3,6-dihidro-2H-piridin-1-il)-2-oksoetil]-1-(5-trifluorometilpiridin-2-il)piperazin-2-on; - Spoj 32: 4-[2-(4-benzofuran-7-il-3,6-dihidro-2H-piridin-1-il)-2-oksoetil]-1-(5-trifluorometilpiridin-2-il)piperazin-2-on; - Spoj 33: 1-(4-benzofuran-7-il-3,6-dihidro-2H-piridin-1-il)-2-[4-(5-trifluorometilpiridin-2-il)piperazin-1-il]etanon; - Spoj 34: 1-(4-benzofuran-7-il-3,6-dihidro-2H-piridin-1-il)-2-[(2S,6R)-2,6-dimetil-4-(5-trifluorometilpiridin-2-il)piperazin-1-il]etanon; - Spoj 35: 1-(4-benzofuran-7-il-3,6-dihidro-2H-piridin-1-il)-2-((2S,6R)-2,6-dimetil-4-pirimidin-5-ilpiperazin-1-il)etanon; - Spoj 36: 1-(4-benzofuran-7-il-3,6-dihidro-2H-piridin-1-il)-2-[(2S,6R)-4-(5-fluoropirimidin-2-il)-2,6-dimetilpiperazin-1-il]etanon; - Spoj 37: 1-(4-benzofuran-7-il-3,6-dihidro-2H-piridin-1-il)-2-[(2S,6R)-2,6-dimetil-4-(6-trifluorometilpiridin-3-il)piperazin-1-il]etanon; - Spoj 38: 2-[(2S,6R)-4-(5-fluoropirimidin-2-il)-2,6-dimetilpiperazin-1-il]-1-[4-(2-metilbenzo[b]tiofen-5-il)-3,6-dihidro-2H-piridin-1-il]etanon; - Spoj 39: 2-[(2S,6R)-2,6-dimetil-4-(6-trifluorometilpiridin-3-il)piperazin-1-il]-1-[4-(2-metilbenzo[b]tiofen-5-il)-3,6-dihidro-2H-piridin-1-il]etanon; - Spoj 40: 2-((2S,6R)-2,6-dimetil-4-pirimidin-5-ilpiperazin-1-il)-1-[4-(2-metilbenzo[b]tiofen-5-il)-3,6-dihidro-2H-piridin-1-il]etanon; - Spoj 41: 1-(4-benzo[b]tiofen-5-il-3,6-dihidro-2H-piridin-1-il)-2-((2S,6R)-2,6-dimetil-4-pirimidin-5-ilpiperazin-1-il)etanon; - Spoj 42: 1-(4-benzo[b]tiofen-5-il-3,6-dihidro-2H-piridin-1-il)-2-[(2S,6R)-4-(5-fluoropirimidin-2-il)-2,6-dimetilpiperazin-1-il)etanon; - Spoj 43: 4-[2-(4-benzo[b]tiofen-5-il-3,6-dihidro-2H-piridin-1-il)-2-oksoetil]-1-(5-trifluorometilpiridin-2-il)piperazin-2-on; - Spoj 44: 1-[4-(2,3-dihidrobenzo[1,4]dioksin-6-il)-3,6-dihidro-2H-piridin-1-il]-2-[(2S,6R)-4-(5-fluoropirimidin-2-il)-2,6-dimetilpiperazin-1-il]etanon; - Spoj 45: 1-[4-(2,3-dihidrobenzo[1,4]dioksin-6-il)-3,6-dihidro-2H-piridin-1-il]-2-[(2S,6R)-2,6-dimetil-4-(6-trifluorometilpiridin-3-il)piperazin-1-il]etanon; - Spoj 46: 1-(4-benzo[b]tiofen-5-il-3,6-dihidro-2H-piridin-1-il)-2-[4-(5-trifluorometilpiridin-2-il)piperazin-1-il]etanon; - Spoj 47: 1-(4-benzo[b]tiofen-5-il-3,6-dihidro-2H-piridin-1-il)-2-[(2S,6R)-2,6-dimetil-4-(6-trifluorometilpiridin-3-il)piperazin-1-il]etanon; - Spoj 48: 5-{(3S,5R)-4-[2-(4-benzo[b]tiofen-4-il-3,6-dihidro-2H-piridin-1-il)-2-oksoetil]-3,5-dimetilpiperazin-1-il}piridin-2-karboksilna kiselina; - Spoj 49: 4-{2-[4-(2,3-dihidrobenzo[1,4]dioksin-6-il)-3,6-dihidro-2H-piridin-1-il]-2-oksoetil}-1-(6-trifluorometilpiridin-3-il)piperazin-2-on; - Spoj 50: 1-(4-benzo[b]tiofen-7-il-3,6-dihidro-2H-piridin-1-il)-2-[4-(6-trifluorometilpiridin-3-il)piperazin-1-illetanon; - Spoj 51: Metil 5-{(3S,5R)-4-[2-(4-benzofuran-7-il-3,6-dihidro-2H-piridin-1-il)-2-oksoetil]-3,5-dimetilpiperazin-1-il}piridin-2-carboksilate; - Spoj 52: Metil 6-{(3S,5R)-4-[2-(4-benzo[b]tiofen-5-il-3,6-dihidro-2H-piridin-1-il)-2-oksoetil]-3,5-dimetilpiperazin-1-il}nikotinat; - Spoj 53: 1-(4-benzo[b]tiofen-7-il-3,6-dihidro-2H-piridin-1-il)-2-[(2S,6R)-4-(5-fluoropirimidin-2-il)-2,6-dimetilpiperazin-1-il]etanon; - Spoj 54: 1-(4-benzo[b]tiofen-7-il-3,6-dihidro-2H-piridin-1-il)-2-[(2S,6R)-2,6-dimetil-4-(6-trifluorometilpiridin-3-il)piperazin-1-il]etanon; - Spoj 55: 1-(4-benzo[b]tiofen-7-il-3,6-dihidro-2H-piridin-1-il)-2-((2S,6R)-2,6-dimetil-4-pirimidin-5-ilpiperazin-1-il)etanon; - Spoj 56: 6-{(3S,5R)-4-[2-(4-benzo[b]tiofen-5-il-3,6-dihidro-2H-piridin-1-il)-2-oksoetil]-3,5-dimetilpiperazin-1-illnikotinska kiselina; - Spoj 57: 6-{(3S,5R)-4-[2-(4-benzofuran-7-il-3,6-dihidro-2H-piridin-1-il)-2-oksoetil]-3,5-dimetilpiperazin-1-il}nikotinska kiselina; - Spoj 58: Metil 6-{(3S,5R)-4-[2-(4-benzo[b]tiofen-7-il-3,6-dihidro-2H-piridin-1-il)-2-oksoetil]-3,5-dimetilpiperazin-1-il}nikotinat; - Spoj 59: 6-{(3S,5R)-4-[2-(4-benzo[b]tiofen-7-il-3,6-dihidro-2H-piridin-1-il)-2-oksoetil]-3,5-dimetilpiperazin-1-il}nikotinska kiselina; - Spoj 60: 4-[2-(4-benzofuran-5-il-3,6-dihidro-2H-piridin-1-il)-2-oksoetil]-1-(5-trifluorometilpiridin-2-il)piperazin-2-on; - Spoj 61: Metil 6-((3S,5R)-3,5-dimetil-4-{2-[4-(2-metilbenzo[b]tiofen-5-il)-3,6-dihidro-2H-piridin-1-il]-2-oksoetil}piperazin-1-il)nikotinat; - Spoj 62: 6-((3S,5R)-3,5-dimetil-4-{2-[4-(2-metilbenzo[b]tiofen-5-il-)-3,6-dihidro-2H-piridin-1-il]-2-oksoetil}piperazin-1-il)nikotinska kiselina; - Spoj 63: 1-(5-benzofuran-7-il-3,6-dihidro-2H-piridin-1-il)-2-[(2S,6R)-2,6-dimetil-4-(5-trifluorometilpiridin-2-il)piperazin-1-il]etanon; - Spoj 64: Etil 6-{(3S,5R)-4-[2-(4-benzofuran-7-il-3,6-dihidro-2H-piridin-1-il)-2-oksoetil]-3,5-dimetilpiperazin-1-il}nikotinat; - Spoj 65: Metil 6-{3-[2-(4-benzofuran-7-il-3,6-dihidro-2H-piridin-1-il)-2-oksoetil]-3,8-diazabiciklo[3.2.1]okt-8-il}nikotinat; - Spoj 66: Metil 7-(1-{2-[(2S,6R)-2,6-dimetil-4-(5-trifluorometilpiridin-2-il)piperazin-1-il]acetil}-1,2,3,6-tetrahidropiridin-4-il)benzo[b]tiofen-2-carboksilate; - Spoj 67: Metil 5-(1-{2-[(2S,6R)-2,6-dimetil-4-(5-trifluorometilpiridin-2-il)piperazin-1-il]acetil}-1,2,3,6-tetrahidropiridin-4-il)benzo[b]tiofen-2-carboksilate; - Spoj 68: 2-[(2S,6R)-2,6-dimetil-4-(5-trifluorometilpiridin-2-il)piperazin-1-il]-1-[4-(2-propilbenzo[b]tiofen-5-il)-3,6-dihidro-2H-piridin-1-il]etanon; - Spoj 69: Metil 6-{3-[2-(4-benzo[b]tiofen-7-il-3,6-dihidro-2H-piridin-1-il)-2-oksoetil]-3,8-diazabiciklo[3.2.1]okt-8-il}nikotinat; - Spoj 70: Metil 6-{3-[2-(4-benzo[b]tiofen-5-il-3,6-dihidro-2H-piridin-1-il)-2-oksoetil]-3,8-diazabiciklo[3.2.1]okt-8-il}nikotinat; - Spoj 71: 6-{3-[2-(4-benzo[b]tiofen-7-il-3,6-dihidro-2H-piridin-1-il)-2-oksoetil]-3,8-diazabiciklo[3.2.1]okt-8-il}nikotinska kiselina; - Spoj 72: 2-[(2S,6R)-2,6-dimetil-4-(5-trifluorometil-piridin-2-il)piperazin-1-il]-1-[4-(7-fluorobenzofuran-5-il)-3,6-dihidro-2H-piridin-1-il]etanon; - Spoj 73: 1-[4-(2,3-dimetilbenzofuran-6-il)-3,6-dihidro-2H-piridin-1-il]-2-[(2S,6R)-2,6-dimetil-4-(5-trifluorometilpiridin-2-il)piperazin-1-il]etanon; - Spoj 74: 2-[(2S,6R)-2,6-dimetil-4-(5-trifluorometilpiridin-2-il)piperazin-1-il]-1-(4-kinolein-2-il-3,6-dihidro-2H-piridin-1-il)etanon; - Spoj 75: 1-(4-benzofuran-5-il-3,6-dihidro-2H-piridin-1-il)-2-(2,3,5,6-tetrahidro[1,2']bipirazinil-4-il)etanon; - Spoj 76: Metil 6-{3-[2-okso-2-(4-thieno[3,2-c]piridin-4-il-3,6-dihidro-2H-piridin-1-il)etil]-3,8-diazabiciklo[3.2.1]okt-8-il}nikotinat; - Spoj 77: Metil 6-(3-{2-[4-(2-metilbenzo[b]tiofen-5-il)-3,6-dihidro-2H-piridin-1-il]-2-oksoetil}-3,8-diazabiciklo[3.2.1]okt-8-il)nikotinat; - Spoj 78: 1-(4-benzofuran-7-il-3,6-dihidro-2H-piridin-1-il)-2-(4-piridin-3-il-[1,4]diazepan-1-il)etanon; - Spoj 79: 6-{3-[2-okso-2-(4-thieno[3,2-c]piridin-4-il-3,6-dihidro-2H-piridin-1-il)etil]-3,8-diazabiciklo[3.2.1]okt-8-il}nikotinska kiselina; - Spoj 80: 6-(3-{2-[4-(2-metilbenzo[b]tiofen-5-il)-3,6-dihidro-2H-piridin-1-il]-2-oksoetil}-3,8-diazabiciklo[3.2.1]okt-8-il)nikotinska kiselina; - Spoj 81: Metil 6-{3-[2-(3-benzofuran-7-il-2,5-dihidropirol-1-il)-2-oksoetil]-3,8-diazabiciklo[3.2.1]okt-8-il}nikotinat; - Spoj 82: Metil 6-{3-[2-(3-benzo[b]tiofen-7-il-2,5-dihidropirol-1-il)-2-oksoetil]-3,8-diazabiciklo[3.2.1]okt-8-il}nikotinat; - Spoj 83: 4-[2-(3-benzofuran-7-il-2,5-dihidropirol-1-il)-2-oksoetil]-1-(5-trifluorometilpiridin-2-il)piperazin-2-on; - Spoj 84: 6-{3-[2-(4-benzofuran-7-il-2,3-dihidropirol-1-il)-2-oksoetil]-3,8-diazabiciklo[3.2.1]okt-8-il}nikotinska kiselina; - Spoj 85: 6-{3-[2-(5-benzo[b]tiofen-7-il-3,4-dihidro-2H-piridin-1-il)-2-oksoetil]-3,8-diazabiciklo[3.2.1]okt-8-il}nikotinska kiselina; - Spoj 86: 6-{3-[2-(4-benzo[b]tiofen-7-il-2,3-dihidropirol-1-il)-2-oksoetil]-3,8-diazabiciklo[3.2.1]okt-8-il}nikotinska kiselina; - Spoj 87: Metil 6-(3-{2-[4-(2,3-dihidrobenzo[1,4]dioksin-6-il)-3,6-dihidro-2H-piridin-1-il]-2-oksoetil}-3,8-diazabiciklo[3.2.1]okt-8-il)nikotinat; - Spoj 88: 2-{(3S,5R)-4-[2-(4-benzo[b]tiofen-7-il-3,6-dihidro-2H-piridin-1-il)-2-oksoetil]-3,5-dimetilpiperazin-1-il}pirimidin-5-karboksilna kiselina; - Spoj 89: 3-(6-{3-[2-(4-benzofuran-7-il-3,6-dihidro-2H-piridin-1-il)-2-oksoetil]-3,8-diazabiciklo[3.2.1]okt-8-il)}piridin-3-il)-4H-[1,2,4]oksadiazol-5-on; - Spoj 90: 3-(6-{3-[2-(4-benzo[b]tiofen-7-il-3,6-dihidro-2H-piridin-1-il)-2-oksoetil]-3,8-diazabiciklo[3.2.1]okt-8-il}piridin-3-il)-4H-[1,2,4]oksadiazol-5-on; - Spoj 91: 6-(3-{2-[4-(2-metilbenzo[b]tiofen-5-il)-3,6-dihidro-2H-piridin-1-il]-2-oksoetil}-3,8-diazabiciklo[3.2.1]okt-8-il)nikotinonitril; - Spoj 92: 1-(4-benzofuran-7-il-3,6-dihidro-2H-piridin-1-il)-2-[(2S,6R)-4-(3-kloro-5-trifluorometilpiridin-2-il)-2,6-dimetilpiperazin-1-il]etanon; - Spoj 93: 1-(4-benzofuran-7-il-3,6-dihidro-2H-piridin-1-il)-2-(8-piridin-3-il-3,8-diazabiciklo[3.2.1]okt-3-il)etanon; - Spoj 94: 6-{3-[2-(4-benzofuran-7-il-3,6-dihidro-2H-piridin-1-il)-2-oksoetil]-3,8-diazabiciklo[3.2.1]okt-8-il}nikotinonitril; - Spoj 95: 1-(4-benzofuran-7-il-3,6-dihidro-2H-piridin-1-il)-2-[5-(5-trifluorometilpiridin-2-il)-2,5-diazabiciklo[2.2.1]hept-2-il]etanon; - Spoj 96: ciklobutil 6-(3-{2-[4-(2-metilbenzo[b]tiofen-5-il)-3,6-dihidro-2H-piridin-1-il]-2-oksoetil}-3,8-diazabiciklo[3.2.1]okt-8-il)nikotinat; - Spoj 97: 2-[(2S,6R)-2,6-dimetil-4-(5-trifluorometilpiridin-2-il)piperazin-1-il]-1-[4-(1H-indol-3-il)-3,6-dihidro-2H-piridin-1-il]etanon; - Spoj 98: 1-[4-(1H-indol-3-il)-3,6-dihidro-2H-piridin-1-il]-2-(4-kinolin-2-ilpiperazin-1-il)etanon; - Spoj 99: 1-(4-benzofuran-7-il-3,6-dihidro-2H-piridin-1-il)-2-[4-(7-klorokinolin-4-il)piperazin-1-il]etanon; - Spoj 100: 2-[(2S,6R)-4-(5-fluoropirimidin-2-il)-2,6-dimetilpiperazin-1-il]-1-[4-(1H-indol-3-il)-3,6-dihidro-2H-piridin-1-il]etanon; - Spoj 101: 1-(4-benzo[b]tiofen-7-il-3,6-dihidro-2H-piridin-1-il)-2-[(2S,6R)-4-(5-kloropiridin-2-il)-2,6-dimetilpiperazin-1-il]etanon; - Spoj 102: 1-(4-benzo[b]tiofen-7-il-3,6-dihidro-2H-piridin-1-il)-2-((2R,5S)-2,5-dimetil-2,3,5,6-tetrahidro-[1,2']bipirazinil-4-il)etanon; - Spoj 103: 1-(4-benzo[b]tiofen-7-il-3,6-dihidro-2H-piridin-1-il)-2-[8-(5-fluoropirimidin-2-il)-3,8-diazabiciklo[3.2.1]okt-3-il]etanon; - Spoj 104: 1-(4-benzo[b]tiofen-7-il-3,6-dihidro-2H-piridin-1-il)-2-[8-(6-trifluorometilpiridin-2-il)-3,8-diazabiciklo[3.2.1]okt-3-il]etanon; - Spoj 105: 1-(4-benzo[b]tiofen-7-il-3,6-dihidro-2H-piridin-1-il)-2-(4-kinolin-2-ilpiperazin-1-il)etanon; - Spoj 106: 1-(4-benzo[b]tiofen-7-il-3,6-dihidro-2H-piridin-1-il)-2-[4-(7-kloro-kinolin-4-il)piperazin-1-il]etanon; - Spoj 107: 1-(4-benzo[b]tiofen-7-il-3,6-dihidro-2H-piridin-1-il)-2-[4-(5-kloro-piridin-2-il)piperazin-1-il]etanon; - Spoj 108: 2-[4-(6-kloropiridin-2-il)piperazin-1-il]-1-[4-(1H-indol-3-il)-3,6-dihidro-2H-piridin-1-il]etanon; - Spoj 109: 1-[4-(1H-indol-3-il)-3,6-dihidro-2H-piridin-1-il]-2-[4-(5-trifluorometilpiridin-2-il)piperazin-1-il]etanon; - Spoj 110: 2-((2S,6R)-2,6-dimetil-4-kinolin-2-il-piperazin-1-il)-1-[4-(1H-indol-3-il)-3,6-dihidro-2H-piridin-1-il]etanon; - Spoj 111: 1-(4-benzo[b]tiofen-7-il-3,6-dihidro-2H-piridin-1-il)-2-(4-piridin-3-il[1,4]diazepan-1-il)etanon; - Spoj 112: 1-(4-benzo[b]tiofen-7-il-3,6-dihidro-2H-piridin-1-il)-2-[4-(5,6-dikloropiridin-2-il)piperazin-1-il]etanon; - Spoj 113: 1-(4-benzo[b]tiofen-7-il-3,6-dihidro-2H-piridin-1-il)-2-[4-(6-bromopiridin-2-il)piperazin-1-il]etanon; - Spoj 114: 1-[4-(2-metilbenzo[b]tiofen-5-il)-3,6-dihidro-2H-piridin-1-il]-2-(4-kinolin-2-ilpiperazin-1-il)etanon; - Spoj 115: 1-(4-benzo[b]tiofen-7-il-3,6-dihidro-2H-piridin-1-il)-2-[5-(6-trifluorometilpiridazin-3-il)-2,5-diazabiciklo[2.2.1]hept-2-il]etanon; - Spoj 116: 1-[4-(2-metilbenzo[b]tiofen-5-il)-3,6-dihidro-2H-piridin-1-il]-2-[4-(6-trifluorometilpiridin-2-il)piperazin-1-il]etanon; - Spoj 117: 2-[4-(7-klorokinolin-4-il)piperazin-1-il]-1-[4-(2-metilbenzo[b]tiofen-5-il)-3,6-dihidro-2H-piridin-1-il]etanon; - Spoj 118: 4-[2-okso-2-(4-thieno[3,2-c]piridin-4-il-3,6-dihidro-2H-piridin-1-il)etil]-1-(5-trifluorometilpiridin-2-il)piperazin-2-on; - Spoj 119: 1-(4-benzofuran-7-il-3,6-dihidro-2H-piridin-1-il)-2-[(2S,6R)-2,6-dimetil-4-(5-thiazol-2-ilpiridin-2-il)piperazin-1-il]etanon; - Spoj 120: 1-(4-benzofuran-7-il-3,6-dihidro-2H-piridin-1-il)-2-{(2S,6R)-2,6-dimetil-4-[5-(2-metil-2H-tetrazol-5-il)piridin-2-il]piperazin-1-il}etanon; - Spoj 121: 2-[(2S,6R)-2,6-dimetil-4-(5-trifluorometilpiridin-2-il)piperazin-1-il]-1-(4-kinolin-2-il-3,6-dihidro-2H-piridin-1-il)etanon; - Spoj 122: 4-[2-okso-2-(4-kinolin-2-il-3,6-dihidro-2H-piridin-1-il)etil]-1-(5-trifluorometilpiridin-2-il)piperazin-2-on; - Spoj 123: 1-(4-kinolin-2-il-3,6-dihidro-2H-piridin-1-il)-2-[8-(5-trifluorometilpiridin-2-il)-3,8-diazabiciklo[3.2.1]okt-3-il]etanon; - Spoj 124: 1-(4-benzofuran-7-il-3,6-dihidro-2H-piridin-1-il)-2-{8-[5-(1-metil-1H-tetrazol-5-il)piridin-2-il]-3,8-diazabiciklo[3.2.1]okt-3-il}etanon; - Spoj 125: 1-(4-benzofuran-7-il-3,6-dihidro-2H-piridin-1-il)-2-[(2S,6R)-4-(5-metanesulfonil-piridin-2-il)-2,6-dimetilpiperazin-1-il]etanon; u obliku baze ili kisele adicijske soli.
7. Postupak za pripremanje spoja s formulom (I) prema bilo kojem od zahtjeva 1 do 6, naznačen time da zajedno reagiraju spoj s formulom (II): [image] u kojoj A, B, m i n su definirani prema bilo kojem od zahtjeva 1 do 6 i Hal predstavlja halogeni atom, i spoj s općom formulom (III): H-W-R2     (III) u kojoj W i R2 su definirani prema bilo kojem od zahtjeva 1 do 6.
8. Lijek, naznačen time da sadrži spoj s formulom (I) prema bilo kojem od zahtjeva 1 do 6, ili adicijsku sol tog spoja s farmaceutski prihvatljivom kiselinom.
9. Farmaceutski pripravak, naznačen time da sadrži spoj s formulom (I) prema bilo kojem od zahtjeva 1 do 6, ili farmaceutski prihvatljivu sol, te također barem jedno farmaceutski prihvatljivo pomoćno sredstvo.
10. Spoj prema bilo kojem od zahtjeva 1 do 6, naznačen time da je lijek.
11. Spoj prema bilo kojem od zahtjeva 1 do 6, naznačen time da je za pripravu lijeka za prevenciju ili liječenje središnjih i perifernih neurodegenerativnih bolesti, staračke demencije, epilepsije, Alzheimerove bolesti, Parkinsonove bolesti, Huntingtonove koreje, Downovog sindroma, prionskih bolesti, amnezije, shizofrenije, depresije, bipolarnog poremećaja, amiotrofne lateralne skleroze, multiple skleroze, kardiovaskularnih poremećaja, post-ishemijskih oštećenja srca, kardiomiopatija, infarkta miokarda, srčane insuficijencije, srčane ishemije, cerebralnog infarkta; perifernih neuropatija, oštećenja očnog živca i rožnice, degeneracije pigmenta mrežnice, glaukoma, ishemije mrežnice, makularne degeneracije, ozljede leđne moždine, trauma glave, ateroskleroze, stenoze, poremećaja zarastanja rana, alopecije, pankreatitisa, fibroze jetre, raka, tumora, metastaza, leukemija, respiratornih poremećaja, upale pluća, alergije, astme, kronične opstruktivne plućne bolesti, kutane, somatske, visceralne i neurološke boli, kronične neuropatske i upalne boli, autoimunih bolesti, reumatoidnog artritisa, ankiloznog spondilitisa, psorijaznog artritisa, psorijaze s naslagama, prijeloma kostiju, bolesti kostiju i osteoporoze.
12. Spoj prema jednom od zahtjeva 1 do 6 naznačen time da je inhibitor dimerizacije receptor p75NTR.
13. Uporaba spoja prema jednom od zahtjeva 1 do 6, naznačena time da je za pripravu lijekova koji su korisni u liječenju i prevenciji središnjih i perifernih neurodegenerativnih bolesti, staračke demencije, epilepsije, Alzheimerove bolesti, Parkinsonove bolesti, Huntingtonove koreje, Downovog sindroma, prionskih bolesti, amnezije, shizofrenije, depresije, bipolarnog poremećaja, amiotrofne lateralne skleroze, multiple skleroze , kardiovaskularnih poremećaja, post-ishemijskih oštećenja srca, kardiomiopatija, infarkta miokarda, srčane insuficijencije, srčane ishemije, cerebralnog infarkta; perifernih neuropatija, oštećenja očnog živca i rožnice, degeneracije pigmenta mrežnice, glaukoma, ishemije mrežnice, makularne degeneracije, ozljede leđne moždine, trauma glave, ateroskleroze, stenoze, poremećaja zarastanja rana, alopecije, pankreatitisa, fibroze jetre, raka, tumora, metastaza, leukemija, respiratornih poremećaja, upale pluća, alergije, astme, kronične opstruktivne plućne bolesti, kutane, somatske, visceralne i neurološke boli, kronične neuropatske i upalne boli, autoimunih bolesti, reumatoidnog artritisa, ankiloznog spondilitisa, psorijaznog artritisa, psorijaze s naslagama, prijeloma kostiju, bolesti kostiju i osteoporoze.
HRP20151036TT 2009-12-14 2015-09-30 Novi derivati (heterocikal/tetrahidropiridin)-(piperazinil)-1-alkanon i (heterocikal/dihidropirolidin)-(piperazinil)-1-alkanon, i njihova uporaba kao inhibitora p75 HRP20151036T1 (hr)

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FR0906025A FR2953836B1 (fr) 2009-12-14 2009-12-14 Nouveaux derives (heterocycle-tetrahydro-pyridine)-(piperazinyl)-1-alcanone et (heterocycle-dihydro-pyrrolidine)-(piperazinyl)-1-alcanone et leur utilisation comme inhibiteurs de p75
EP10801663.5A EP2513088B1 (fr) 2009-12-14 2010-12-13 Nouveaux dérivés (hétérocycle-tétrahydro-pyridine)-(piperazinyl)-1-alcanone et (hétérocycle-dihydro-pyrrolidine)-(pipérazinyl)-1-alcanone et leur utilisation comme inhibiteurs de p75
PCT/FR2010/052686 WO2011080445A1 (fr) 2009-12-14 2010-12-13 NOUVEAUX DERIVES (HETEROCYCLE-TETRAHYDRO-PYRIDINE)-(PIPERAZINYL)-1-ALCANONE ET (HETEROCYCLE-DIHYDRO-PYRROLIDINE)-(PIPERAZINYL)-1-ALCANONE ET LEUR UTILISATION COMME INHIBITEURS DE p75

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