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HRP20180916T1 - Inhibitori demetilaze od lsd1 na bazi arilciklopropilamina i njihova medicinska uporaba - Google Patents

Inhibitori demetilaze od lsd1 na bazi arilciklopropilamina i njihova medicinska uporaba Download PDF

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Publication number
HRP20180916T1
HRP20180916T1 HRP20180916TT HRP20180916T HRP20180916T1 HR P20180916 T1 HRP20180916 T1 HR P20180916T1 HR P20180916T T HRP20180916T T HR P20180916TT HR P20180916 T HRP20180916 T HR P20180916T HR P20180916 T1 HRP20180916 T1 HR P20180916T1
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HR
Croatia
Prior art keywords
compound
phenyl
trans
compound according
cyclopropylamino
Prior art date
Application number
HRP20180916TT
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English (en)
Inventor
Alberto ORTEGA MUÑOZ
Matthew Colin Thor Fyfe
Marc Martinell Pedemonte
Iñigo TIRAPU FERNANDEZ DE LA CUESTA
Maria de los Ángeles ESTIARTE-MARTÍNEZ
Original Assignee
Oryzon Genomics, S.A.
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Application filed by Oryzon Genomics, S.A. filed Critical Oryzon Genomics, S.A.
Publication of HRP20180916T1 publication Critical patent/HRP20180916T1/hr

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    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
    • A61K31/42—Oxazoles
    • A61K31/422—Oxazoles not condensed and containing further heterocyclic rings
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    • A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
    • A61K31/4245—Oxadiazoles
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Claims (29)

1. Spoj, naznačen time, da ima Formulu (I) ili njegova farmaceutski prihvatljiva sol ili njegov solvat: u kojoj: (A) je aril-skupina ili heteroaril-skupina, pri čemu navedena aril-skupina ili navedena heteroaril-skupina ima n supstituenata (R3); (B) je –O-CH2-fenil ili fenil, pri čemu navedeni fenil ili dio molekule fenila obuhvaćen u navedenom –O-CH2-fenilu, ima n supstituenata (R2); (D) je monociklička heteroaril-skupina, pri čemu navedena heteroaril-skupina ima jedan supstituent (R1), i nadalje time, da je navedena heteroaril-skupina kovalentno vezana na ostatak molekule preko prstenskog atoma ugljika; (R1) je –NH2; svaki (R2) je neovisno odabran od sljedećih: alkil, alkenil, alkinil, ciklil, amino, amido, C-amido, alkilamino, hidroksil, nitro, halo, haloalkil, haloalkoksi, cijano, sulfinil, sulfonil, sulfonamid, alkoksi, acil, karboksil, karbamat ili urea; svaki (R3) je neovisno odabran od sljedećih: alkil, alkenil, alkinil, ciklil, amino, amido, C-amido, alkilamino, hidroksil, nitro, halo, haloalkil, haloalkoksi, cijano, sulfinil, sulfonil, sulfonamid, alkoksi, acil, karboksil, karbamat ili urea; i n je neovisno 0, 1, 2, 3, ili 4.
2. Spoj prema zahtjevu 1, naznačen time, da (A) je fenil, piridinil, tiofenil, pirolil, furanil, ili tiazolil, i nadalje time, da (A) ima n supstituenata (R3).
3. Spoj prema zahtjevu 1, naznačen time, da (A) je fenil ili piridil, i nadalje time, da navedeni fenil ili navedeni piridil ima n supstituenata (R3).
4. Spoj prema bilo kojem od zahtjeva 1 do 3, naznačen time, da (A) ima n supstituenata (R3).
5. Spoj prema bilo kojem od zahtjeva 1 do 4, naznačen time, da (B) ima 0 ili 1 supstituent (R2).
6. Spoj prema bilo kojem od zahtjeva 1 do 5, naznačen time, da (D) je tiazolil, oksadiazolil, oksazolil, izoksazolil, tiadiazolil, triazinil, piridazinil, pirazinil, piridinil, ili pirimidinil, i nadalje time, da navedeni tiazolil, navedeni oksadiazolil, navedeni oksazolil, navedeni izoksazolil, navedeni tiadiazolil, navedenitriazinil, navedeni piridazinil, navedeni pirazinil, navedeni piridinil, ili navedeni pirimidinil ima jedan supstituent (R1).
7. Spoj prema bilo kojem od zahtjeva 1 do 6, naznačen time, da (D) je oksadiazolil, pri čemu navedeni oksadiazolil ima jedan supstituent (R1).
8. Spoj prema bilo kojem od zahtjeva 1 do 7, naznačen time, da (R2) je neovisno odabran od hidroksila, halo ili haloalkila.
9. Spoj prema bilo kojem od zahtjeva 1 do 8, naznačen time, da su supstituenti na dijelu molekule ciklopropila u trans-konfiguraciji.
10. Spoj prema zahtjevu 1, naznačen time, da je navedeni spoj odabran od sljedećih: 5-(((trans)-2-(4-(benziloksi)fenil)ciklopropilamino)metil)pirimidin-2-amin; 5-(((trans)-2-(4-(benziloksi)fenil)ciklopropilamino)metil)tiazol-2-amin; 5-(((trans)-2-(6-(3-trifluorometil)fenil)piridin-3-il)ciklopropilamino)metil)pirimidin-2-amin; 5-(((trans)-2-(6-(3-trifluorometil)fenil)piridin-3-il)ciklopropilamino)metil)tiazol-2-amin; 3-(5-((trans)-2-((2-aminopirimidin-5-il)metilamino)ciklopropil)piridin-2-il)fenol; 3-(5-((trans)-2-((2-aminotiazol-5-il)metilamino)ciklopropil)piridin-2-il)fenol; 4'-((trans)-2-((2-aminopirimidin-5-il)metilamino)ciklopropil)bifenil-3-ol; 4'-((trans)-2-((2-aminotiazol-5-il)metilamino)ciklopropil)bifenil-3-ol; 5-(((trans)-2-(4-(benziloksi)fenil)ciklopropilamino)metil)-1,2,4-oksadiazol-3-amin; 5-(((trans)-2-(4-(benziloksi)fenil)ciklopropilamino)metil)-1,3,4-oksadiazol-2-amin; ili njegova farmaceutski prihvatljiva sol ili njegov solvat.
11. Spoj prema zahtjevu 1, naznačen time, da navedeni spoj je: 5-(((trans)-2-(4-(benziloksi)fenil)ciklopropilamino)metil)-1,3,4-oksadiazol-2-amin; ili njegova farmaceutski prihvatljiva sol ili njegov solvat.
12. Spoj prema bilo kojem od zahtjeva 9 do 11, naznačen time, da navedeni spoj je optički aktivan stereoizomer.
13. Spoj prema bilo kojem od zahtjeva 9 do 12, naznačen time, da navedeni spoj je (-) stereoizomer.
14. Spoj prema bilo kojem od zahtjeva 9 do 12, naznačen time, da navedeni spoj je (+) stereoizomer.
15. Spoj prema zahtjevu 1, naznačen time, da navedeni spoj je: (-) 5-(((trans)-2-(4-(benziloksi)fenil)ciklopropilamino)metil)-1,3,4-oksadiazol-2-amin; ili njegova farmaceutski prihvatljiva sol ili njegov solvat.
16. Farmaceutski pripravak, naznačen time, da on obuhvaća spoj prema bilo kojem od zahtjeva 1 do 15 i farmaceutski prihvatljiv nosač.
17. Spoj prema bilo kojem od zahtjeva 1 do 15, ili farmaceutski pripravak prema zahtjevu 16, naznačen time, da se upotrebljava kao lijek.
18. Spoj prema bilo kojem od zahtjeva 1 do 15, naznačen time, da se upotrebljava u liječenju ili prevenciji neurološke bolesti ili neurološkog poremećaja.
19. Spoj za uporabu prema zahtjevu 18, naznačen time, da navedeni spoj je: 5-(((trans)-2-(4-(benziloksi)fenil)ciklopropilamino)metil)-1,3,4-oksadiazol-2-amin; ili njegova farmaceutski prihvatljiva sol ili njegov solvat.
20. Spoj za uporabu prema zahtjevu 18, naznačen time, da navedeni spoj je: (-) 5-(((trans)-2-(4-(benziloksi)fenil)ciklopropilamino)metil)-1,3,4-oksadiazol-2-amin; ili njegova farmaceutski prihvatljiva sol ili njegov solvat.
21. Spoj za uporabu prema bilo kojem od zahtjeva 18 do 20, naznačen time, da je navedena neurološka bolest ili navedeni neurološki poremećaj odabrana/odabran od sljedećih: depresija, Alzheimerova bolest, Huntingtonova bolest, Parkinsonova bolest, amiotrofna lateralna skleroza, frontotemporalna demencija ili demencija s Lewy tijelima.
22. Spoj za uporabu prema bilo kojem od zahtjeva 18 do 21, naznačen time, da navedena neurološka bolest ili navedeni neurološki poremećaj je Alzheimerova bolest.
23. Spoj za uporabu prema bilo kojem od zahtjeva 18 do 21, naznačen time, da navedena neurološka bolest ili navedeni neurološki poremećaj je Huntingtonova bolest.
24. Spoj za uporabu prema bilo kojem od zahtjeva 18 do 21, naznačen time, da navedena neurološka bolest ili navedeni neurološki poremećaj je Parkinsonova bolest.
25. Spoj za uporabu prema bilo kojem od zahtjeva 18 do 21, naznačen time, da navedena neurološka bolest ili navedeni neurološki poremećaj je amiotrofna lateralna skleroza.
26. Spoj prema bilo kojem od zahtjeva 1 do 15, naznačen time, da se upotrebljava u liječenju ili prevenciji raka.
27. Spoj za uporabu prema zahtjevu 26, naznačen time, da je navedeni rak odabran od sljedećih: rak prostate, rak dojke, rak pluća, kolorektalni rak, rak mozga, rak kože, rak krvi, leukemija, limfom, ili mijelom.
28. Spoj prema bilo kojem od zahtjeva 1 do 15, naznačen time, da se upotrebljava u liječenju ili prevenciji virusne infekcije.
29. Spoj prema bilo kojem od zahtjeva 1 do 15, naznačen time, da se upotrebljava u liječenju ili prevenciji virusne reaktivacije nakon latentnog stanja.
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