HRP20120271T1 - Novi p2x7r antagonisti i njihova uporaba - Google Patents

Novi p2x7r antagonisti i njihova uporaba Download PDF

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HRP20120271T1
HRP20120271T1 HR20120271T HRP20120271T HRP20120271T1 HR P20120271 T1 HRP20120271 T1 HR P20120271T1 HR 20120271 T HR20120271 T HR 20120271T HR P20120271 T HRP20120271 T HR P20120271T HR P20120271 T1 HRP20120271 T1 HR P20120271T1
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indol
bromo
chloro
hydroxypropyl
cycloheptylacetamide
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HR20120271T
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B�S Michael
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Affectis Pharmaceuticals Ag
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Abstract

Spoj opće formule: naznačen time da, - R1 je mono- ili bicikloalkilalkilna skupina ili mono- ili bicikloalkilna skupina; - R2 je odabran od ravnog ili razgranatog C1-C5 alkila koji može proizvoljno biti supstituiran sa -OH, -CH2-OH,

Claims (19)

1. Spoj opće formule: [image] naznačen time da, - R1 je mono- ili bicikloalkilalkilna skupina ili mono- ili bicikloalkilna skupina; - R2 je odabran od ravnog ili razgranatog C1-C5 alkila koji može proizvoljno biti supstituiran sa -OH, -CH2-OH, C1-C5 alkoksi, NH2-, N(Ra)2-, NHRa-, CN-, CF3, halogenom, piperidino, morfolino, pirolidino, 5H-tetrazolilpropilom, metilkarbamoil, dimetilkarbamoil, ili etilmetilkarbamoil, pri čemu Ra je C1-C5 alkil; - R3, R4, R5, R6 su kod svakog pojavljivanja nezavisno odabrani od vodika, halogena, metila, metoksi, cijano ili trifluorometila; - a, b, c, d su kod svakog pojavljivanja nezavisno odabrani od ugljika ili dušika, x je CH ili N; ili njegova farmaceutski prihvatljiva sol ili solvat.
2. Spoj prema zahtjevu 1, naznačen time da R2 je supstituiran sa jednim ili dva supstituenta odabrana od -OH, -CH2-OH, C1-C5 alkoksi, -NH2, NHRa, -CN, -CF3, halogena, piperidino, morfolino, pirolidino ili 5H-tetrazolilpropila.
3. Spoj prema zahtjevu 1 ili 2, naznačen time da R1 je skupina odabrana od ciklopentila, ciklopentilmetila, cikloheksila, cikloheksilmetila, cikloheptila, cikloheptilmetila, biciklo[2.2.2]oktan-1-il i biciklo[2.2.2]oktan-1-ilmetila.
4. Spoj prema zahtjevu 3, naznačen time da R2 je C1-C5 alkil ili C2-C5 hidroksialkil.
5. Spoj prema bilo kojem od zahtjeva 1 do 4, naznačen time da barem dva od R3, R4, R5 i R6 su vodik.
6. Spoj prema bilo kojem od zahtjeva 1 do 5, naznačen time da x je CH.
7. Spoj prema bilo kojem od zahtjeva 1 do 5, naznačen time da x je N.
8. Spoj prema bilo kojem od zahtjeva 1 do 7, naznačen time da a, b, c, i d su C.
9. Spoj prema bilo kojem od zahtjeva 1 do 7, naznačen time da jedan od a, b, c i d je N.
10. Spoj prema bilo kojem od zahtjeva 1 do 9 naznačen time da je odabran od: - N-(4-kloro-1-(2-hidroksietil)-1H-indol-3-il)-2-cikloheptilacetamida, - N-(4-bromo-1-(2-hidroksietil)-1H-indol-3-il)-2-cikloheptilacetamida, - N-(4-kloro-1-(2-hidroksietil)-1H-indol-3-il)-2-cikloheksilacetamida, - N-(4-bromo-1-(2-hidroksietil)-1H-indol-3-il)-2-cikloheksilacetamida, - N-(4-kloro-1-(2-hidroksipropil)-1H-indol-3-il)-2-cikloheptilacetamida, - N-(4-bromo-1-(2-hidroksipropil)-1H-indol-3-il)-2-cikloheptilacetamida, - N-(4-kloro-1-(hidroksimetil)-1H-indol-3-il)-3-cikloheksilpropanamida, - N-(4-bromo-1-(hidroksimetil)-1H-indol-3-il)-3-cikloheksilpropanamida, - N-(4-kloro-1-(hidroksimetil)-1H-indol-3-il)-3-cikloheptilpropanamida, - N-(4-bromo-1-(hidroksimetil)-1H-indol-3-il)-3-cikloheptilpropanamida, - N-(4-kloro-1-(2-hidroksietil)-1H-pirolo[2,3-b]piridin-3-il)-2-cikloheksilacetamida, - N-(4-bromo-1-(2-hidroksietil)-1H-pirolo[2,3-b]piridin-3-il)-2-cikloheksilacetamida, - N-(4-kloro-1-(2-hidroksietil)-1H-pirolo[2,3-b]piridin-3-il)2-cikloheptilacetamida, - N-(4-bromo-1-(2-hidroksietil)-1H-pirolo[2,3-b]piridin-3-il)-2-cikloheptilacetamida, - N-(4-kloro-1-(2-hidroksipropil)-1H-pirolo[2,3-b]piridin-3-il)-2-cikloheptilacetamida, - N-(4-bromo-1-(2-hidroksipropil)-1H-pirolo[2,3-b]piridin-3-il)-2-cikloheptilacetamida, - N-(4-kloro-1-(2-hidroksietil)-1H-pirolo[2,3-b]piridin-3-il)-3-cikloheksilpropanamida, - N-(4-bromo-1-(2-hidroksietil)-1H-pirolo[2,3-b]piridin-3-il)-3-cikloheksilpropanamida, - N-(4-kloro-1-(2-hidroksipropil)-1H-indol-3-il)-2-cikloheksilacetamida, - N-(4-bromo-1-(2-hidroksipropil)-1H-indol-3-il)-2-cikloheksilacetamida, - 2-(biciklo[2.2.2]oktan-1-il)-N-(4-kloro-1-(2-hidroksipropil)-1H-indol-3-il)acetamida, - 2-(biciklo[2.2.2]oktan-1-il)-N-(4-bromo-1-(2-hidroksipropil)-1H-indol-3-il)acetamida, - N-(4-kloro-1-(2-hidroksipropil)-1H-indol-3-il)-3-cikloheksilpropanamida, - N-(4-bromo-1-(2-hidroksipropil)-1H-indol-3-il)-3-cikloheksilpropanamida, - N-(4-kloro-1(-2-hidroksipropil)-1H-indol-3-il)-3-cikloheptilpropanamida, - N-(4-bromo-1-(2-hidroksipropil)-1H-indol-3-il)-3-cikloheptilpropanamida, - N-(4-kloro-1-(1,3-dihidroksipropan-2-il)-1H-indol-3-il)-2-cikloheksilaceamida, - N-(4-bromo-1-(1,3-dihidroksipropan-2-il)-1H-indol-3-il)-2-cikloheksilacetamida, - N-(4-kloro-1-(1,3-dihidroksipropan-2-il)-1H-indol-3-il)-2-cikloheptilacetamida, - N-(4-bromo-1-(1,3-dihidroksipropan-2-il)-1H-indol-3-il)-2-cikloheptilacetamida, - 2-(biciklo[2.2.2]oktan-1-il)-N-(4-kloro-1-(1,3-dihidroksipropan-2-il)-1H-indol-3-il)acetamida - 2-(biciklo[2.2.2]oktan-1-il)-N-(4-bromo-1-(1,3-dihidroksipropan-2-il)-1H-indol-3-il)acetamida, - N-(4-kloro-1-(1,3-dihidroksipropan-2-il)-1H-indol-3-il)-3-cikloheksilpropanamida, - N-(4-bromo-1-(1,3-dihidroksipropan-2-il)-1H-indol-3-il)-3-cikloheksilpropanamida, - N-(4-kloro-1-(1,3-dihidroksipropan-2-il)-1H-indol-3-il)-3-cikloheptilpropanamida, - N-(4-bromo-1-(1,3-dihidroksipropan-2-il)-1H-indol-3-il)-3-cikloheptilpropanamida, - N-(1-(3-amino-2-hidroksipropil)-4-kloro-1H-indol-3-il)-2-cikloheksilacetamida, - N-(1-(3-amino-2-hidroksipropil)-4-bromo-1H-indol-3-il)-2-cikloheksilacetamida, - N-(1-(3-amino-2-hidroksipropil)-4-kloro-1H-indol-3-il)-2-cikloheptilacetamida, - N-(1-(3-amino-2-hidroksipropil)-4-bromo-1H-indol-3-il)-2-cikloheptilacetamida, - N-(1-(3-amino-2-hidroksipropil)-4-kloro-1H-indol-3-il)-2-(biciklo[2.2.2]oktan-1-il)acetamida, - N-(1-(3-amino-2-hidroksipropil)-4-bromo-1H-indol-3-il)-2-(biciklo[2.2.2]oktan-1-il)acetamida, - N-(1-(3-amino-2-hidroksipropil)-4-kloro-1H-indol-3-il)-3-cikloheksilpropanamida, - N-(1-(3-amino-2-hidroksipropil)-4-bromo-1H-indol-3-il)-3-cikloheksilpropanamida, - N-(1-(3-amino-2-hidroksipropil)-4-kloro-1H-indol-3-il)-3-cikloheptilpropanamida, - N-(1-(3-amino-2-hidroksipropil)-4-bromo-1H-indol-3-il)-3-cikloheptilpropanamida, - N-(4-kloro-1-metil-1H-indol-3-il)-2-cikloheksilacetamida, - N-(4-bromo-1-metil-1H-indol-3-il)-2-cikloheksilacetamida, - N-(4-kloro-1-metil-1H-indol-3-il)-2-cikloheptilacetamida, - N-(4-bromo-1-metil-1H-indol-3-il)-2-cikloheptilacetamida, - 2-(biciklo[2.2.2]oktan-1-il)-N-(4-kloro-1-metil-1H-indol-3-il)acetamida, - 2-(biciklo[2.2.2]oktan-1-il)-N-(4-bromo-1-metil-1H-indol-3-il)acetamida, - N-(4-kloro-1-metil-1H-indol-3-il)-3-cikloheksilpropanamida, - N-(4-bromo-1-metil-1H-indol-3-il)-3-cikloheksilpropanamida, - N-(4-kloro-1-metil-1H-indol-3-il)-3-cikloheptilpropanamida, - N-(4-bromo-1-metil-1H-indol-3-il)-3-cikloheptilpropanamida, - N-(4-kloro-1-(2-hidroksi-3-(metilamino)propil)-1H-indol-3-il)-2-cikloheksilacetamida, - N-(4-bromo-1-(2-hidroksi-3-(metilamino)propil)-1H-indol-3-il)-2-cikloheksilacetamida, - N-(4-kloro-1-(2-hidroksi-3-(metilamino)propil)-1H-indol-3-il)-2-cikloheptilacetamida. - N-(4-bromo-1-(2-hidroksi-3-(metilamino)propil)-1H-indol-3-il)-2-cikloheptilacetamida, - 2-(biciklo[2.2.2]oktan-1-il)-N-(4-kloro-1-(2-hidroksi-3-(metilamino)propil)-1H-indol-3-il)acetamida, te - 2-(biciklo[2.2.2]oktan-1-il)-N-(4-bromo-1-(2-hidroksi-3-(metilamino)propil)-1H-indol-3-il)acetamida.
11. Farmaceutski pripravak naznačen time da sadrži spoj prema bilo kojem od zahtjeva 1 do 10.
12. Farmaceutski pripravak prema zahtjevu 11, naznačen time da nadalje sadrži dodatni aktivni spoj u odvojenom ili jediničnom obliku doziranja za istovremeno ili sekvencijalno davanje, pri čemu dodatni aktivni spoj je odabran od NSAID-a, TNF-α inhibitora, TACE inhibitora, kortikosteroida, β2-adrenergijskih receptorskih agonista, anti-depresijskih lijekova, antipsihotičkih lijekova, inhibitora biosinteze leukotriena, 5-LO inhibitora, FLAP-antagonista, antagonista receptora leukotriena LTB4, LTC4, LTD4 i LTE4, PDE4 inhibitora, antihistaminskih H1 receptorskih antagonista, gastroprotektivnih H2 receptorskih antagonista, agonista α1- i α2-adrenoceptorskih vazokonstrikcijskih simpatomimetičkih sredstava, antikolinergijskih sredstava, β1- do β4-adrenoceptorskih agonista, metilksantina, natrijevog kromoglikata, muskarimskih receptorskih antagonista, IGF-1 mimetika, inhibitora triptaze, PAF antagonista, ICE inhibitora, IMPDH inhibitora, inhibitora adhezije molekula, katepsina, inhibitora MAP kinaze, inhibitora glukoza-6 fosfat dehidrogenaze, kinin-B1- i B2-receptorskih antagonista, sredstava protiv gihta, inhibitora ksantin oksidaze, urikozurika, sekretagoga hormona rasta, TGFβ, PDGF, faktora rasta fibroblasta, GM-CSF, kapsaicin kreme, Tahikinin NK1 i NK3 receptorskih antagonista, inhibitora elastaze, inhibitora MMPS, antitumorskih sredstava, antivirusnih sredstava, kardiovaskularnih sredstava, CNS sredstava, osteoporoznih sredstava i imunosupresivnih sredstava.
13. Farmaceutski pripravak prema zahtjevu 11 ili 12 naznačen time da je za uporabu kod liječenja afektivnih poremećaja.
14. Farmaceutski pripravak naznačen time da je za uporabu kod liječenja afektivnih poremećaja prema zahtjevu 13, pri čemu afektivni poremećaj je odabran od depresije, tjeskobe, bipolarnog poremećaja i shizofrenije.
15. Farmaceutski pripravak prema zahtjevu 11 ili 12, naznačen time da je za uporabu kod liječenja neurodegenerativnih bolesti i poremećaja, bolesti i poremećaja koji su posredovani sa ili rezultiraju sa neurološkim upalama i središnje posredovanim neuropsihijatrijskim bolestima i poremećajima.
16. Farmaceutski pripravak prema zahtjevu 11 ili 12, naznačen time da je za uporabu kod liječenja boli, upalnih procesa, te degenerativnih stanja.
17. Farmaceutski pripravak za uporabu kod liječenja upalnih procesa i degenerativnih stanja prema zahtjevu 16, naznačen time da je upalni proces odabran od reumatoidnog artritisa, osteoporoze i kronične opstruktivne plućne bolesti.
18. Farmaceutski pripravak za uporabu kod liječenja upalnih procesa i degenerativnih stanja prema zahtjevu 16, naznačen time da je degenerativno stanje odabrano od glaukoma, makularne degeneracije povezane sa starenjem, uveitisa, neuropatske boli, multiple skleroze, amiotrofične lateralne skleroze, Parkinsonove bolesti i Alzheimerove bolesti.
19. Farmaceutski pripravak prema zahtjevu 11 ili 12, naznačen time da je za uporabu kod liječenja neuropatske boli.
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US8268861B2 (en) 2012-09-18
DK2243772T3 (da) 2012-02-13
US20110212992A1 (en) 2011-09-01
CY1112758T1 (el) 2016-02-10
ZA201108305B (en) 2012-08-29
SMT201200017B (it) 2012-07-10
KR20120006547A (ko) 2012-01-18
AU2010237302A1 (en) 2011-12-01
MX2011010810A (es) 2012-01-12
US20100267762A1 (en) 2010-10-21

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