ME02754B - Ligandi opioidnih receptora i postupci njihove upotrebe i pripreme - Google Patents

Ligandi opioidnih receptora i postupci njihove upotrebe i pripreme

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Publication number
ME02754B
ME02754B MEP-2017-129A MEP2017129A ME02754B ME 02754 B ME02754 B ME 02754B ME P2017129 A MEP2017129 A ME P2017129A ME 02754 B ME02754 B ME 02754B
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Montenegro
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alkyl
pharmaceutically acceptable
acceptable salt
compound
compound according
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MEP-2017-129A
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German (de)
English (en)
French (fr)
Inventor
Dennis Yamashita
Dimitar Gotchev
Philip Pitis
Xiao-Tao Chen
Guodong Liu
Catherine C K Yuan
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Trevena Inc
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Application filed by Trevena Inc filed Critical Trevena Inc
Publication of ME02754B publication Critical patent/ME02754B/me

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Claims (20)

1. Jedinjenje formule IV-1, ili neka njegova farmaceutski prihvatljiva so,: u kojoj: R21 i R22 su nezavisno H ili CH3; A4 je neki opciono supstituisan cikl formule C(CH2)n, u kojoj n = 2-5, pri čemu je opciona supstitucija halo, cijano, C1-C6 alkil, C1-C6 razgranat alkil, halogenovan C1-C6 alkil, hidroksil, C1-C6 alkiloksi, amino, ili C1-C6 alkilamino; B3 je H ili neki opciono supstituisan C1-C6 alkil, pri čemu je opciona supstitucija halo, hidroksi ili C1-C6 alkoksi; B4 je C1-C6 alkilen; D1 je neki opciono supstituisan monociklični ili biciklični aril ili heteroaril, u kom je svaki prsten neki 5, 6 ili 7-člani prsten, a opciona supstitucija je halo, cijano, C1-C6 alkil, C1-C6 razgranat alkil, halogenovan C1-C6 alkil, hidroksil, C1-C6 alkiloksi, amino, ili C1-C6 alkilamino; i B5 je neki opciono supstituisan monociklični ili biciklični aril ili heteroaril, u kom je svaki prsten neki 5, 6, ili 7-člani prsten, a opciona supstitucija je halo, cijano, C1-C6 alkil, C1-C6 razgranat alkil, halogenovan C1-C6 alkil, hidroksil, C1-C6 alkiloksi, amino, ili C1-C6 alkilamino.
2.Jedinjenje prema zahtevu 1, ili neka njegova farmaceutski prihvatljiva so, koje ima strukturu formule VIII: u kojoj su R26 i R27 nezavisno H ili neki njegov izotop.
3.Jedinjenje prema zahtevu 2, ili neka njegova farmaceutski prihvatljiva so, pri čemu jedinjenje ima formulu IX
4.Jedinjenje prema zahtevima 2 ili 3, ili neka njegova farmaceutski prihvatljiva so, pri čemu jedinjenje ima formulu VII-l
5.Jedinjenje prema nekom od zahteva 2-4, ili neka njegova farmaceutski prihvatljiva so, pri čemu jedinjenje ima formulu X
6. Jedinjenje prema nekom od zahteva 1-5, ili neka njegova farmaceutski prihvatljiva so, kod kog je D1 neki opciono supstituisan fenil, pri čemu je opciona supstitucija halo, cijano, C1-C6 alkil, C1-C6 razgranat alkil, halogenovan C1-C6 alkil, hidroksil, C1-C6 alkiloksi, amino, ili C1-C6 alkilamino ili neki opciono supstituisan piridil, pri čemu je opciona supstitucija halo, cijano, C1-C6 alkil, C1-C6 razgranat alkil, halogenovan C1-C6 alkil, hidroksil, C1-C6 alkiloksi, amino, ili C1-C6 alkilamino.
7.Jedinjenje prema nekom od zahteva 1-5, ili neka njegova farmaceutski prihvatljiva so, kod kog je B5 neki opciono supstituisan monociklični ili biciklični heteroaril, u kom je svaki prsten neki 5, 6, ili 7- člani prsten, a opciona supstitucija je halo, cijano, C1-C6 alkil, C1-C6 razgranat alkil, halogenovan C1-C6alkil, hidroksil, C1-C6 alkiloksi, amino, ili C1-C6 alkilamino.
8.Jedinjenje prema nekom od zahteva 1-5, ili neka njegova farmaceutski prihvatljiva so, kod kog je B5 neki opciono supstituisan aril ili heteroaril odabran iz grupe koju čine pri čemu je opciona supstitucija halo, cijano, C1-C6 alkil, C1-C6 razgranat alkil, halogenovan C1-C6 alkil, hidroksil, C1-C6 alkiloksi, amino, ili C1-C6 alkilamino.
9.Jedinjenje prema zahtevima 1-5, ili neka njegova farmaceutski prihvatljiva so, kod kog je B5 odabran iz grupe koju čine u kojima R23, R24, i R30 su svaki nezavisno nula, H, OH, halo, razgranat ili nerazgranat C1-C6 alkil, cijano, C1-C6alkoksi, amino, C1-C6 haloalkil, ili, R23 i R24 zajedno obrazuju neki aril, heteroaril ili ciki koji je vezan za jedan ili više atoma B5; a R25 je H ili neki opciono supstituisan razgranat ili nerazgranat alkil, pri čemu je opciona supstitucija halo, hidroksi ili C1-C3 alkoksi.
10.Jedinjenje prema zahtevu 9, ili neka njegova farmaceutski prihvatljiva so, kod kog su R23, R24, i R30 svaki nezavisno H, NH2, OH, CI, Br, F, I, OMe, CN, ili CH3.
11.Jedinjenje prema zahtevu 9, ili neka njegova farmaceutski prihvatljiva so, kod kog B5 predstavlja
12.Jedinjenje prema zahtevu 9 ili 11, ili neka njegova farmaceutski prihvatljiva so, kod kog R23 predstavlja C1-C6 alkoksi.
13.Jedinjenje prema nekom od zahteva 1-12, ili neka njegova farmaceutski prihvatljiva so, kod kog B3 predstavlja H ili C1-C6 alkil.
14.Jedinjenje prema zahtevu 1, ili neka njegova farmaceutski prihvatljiva so, koje ima formulu:
15.Jedinjenje prema zahtevu 1, ili neka njegova farmaceutski prihvatljiva so, koje ima formulu:
16.Jedinjenje prema zahtevu 1, ili neka njegova farmaceutski prihvatljiva so, koje ima formulu:
17.Jedinjenje prema zahtevu 1, ili neka njegova farmaceutski prihvatljiva so, koje ima formulu:
18.Farmaceutska kompozicija koja obuhvata jedinjenje, ili neku njegovu farmaceutski prihvatljivu so, prema bilo kom od zahteva 1-17 i neki farmaceutski prihvatljiv nosač.
19.Jedinjenje ili neka njegova farmaceutski prihvatljiva so, ili kompozicija prema bilo kom od zahteva 1-18 za upotrebu u tretiranju bola.
20. Postupak pripreme jedinjenja, ili neke njegove farmaceutski prihvatljive soli, prema zahtevu 2, gde R26 i R27 predstavljaju H, pri čemu taj postupak obuhvata: dovođenje u kontakt pod pogodnim uslovima za obrazovanje jedinjenja koje ima strukturu pod pogodnim uslovima za obrazovanje jedinjenja koje ima strukturu
MEP-2017-129A 2011-03-23 2012-03-23 Ligandi opioidnih receptora i postupci njihove upotrebe i pripreme ME02754B (me)

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Application Number Priority Date Filing Date Title
US201161466809P 2011-03-23 2011-03-23
US201261596808P 2012-02-09 2012-02-09
EP12760456.9A EP2688403B1 (en) 2011-03-23 2012-03-23 Opioid receptor ligands and methods of using and making same
PCT/US2012/030327 WO2012129495A1 (en) 2011-03-23 2012-03-23 Opioid receptor ligands and methods of using and making same

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