SI2844637T1 - Substituirani 3-haloalilaminski inhibitorji SSAO in njihova uporaba - Google Patents
Substituirani 3-haloalilaminski inhibitorji SSAO in njihova uporaba Download PDFInfo
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Claims (18)
- Substituirani 3-haloalilaminski inhibitorji SSAO in njihova uporaba Patentni zahtevki1. Spojina s formulo II:Formula II ali farmacevtsko sprejemljiva sol, solvat ali polimorfna oblika le-te; kjer: R5 je nesubstituirana fenilenska skupina ali fenilenska skupina, substituirana z eno ali več skupinami, neodvisno izbranimi izmed alkila, halo, alkoksi in haloalkila; R6 je izbran izmed:7 S R in R sta neodvisno izbrana iz skupine, ki jo sestavljajo vodik, po izbiri substituiran Ci.6alkil in po izbiri substituiran C3.7cikloalkil; in X je kisik;kjer se izraz "alkil" nanaša na monovalentne ravnoverižne ali razvejene nasičene ogljikovodikove ostanke, ki imajo 1-6 atomov ogljika, in kjer se izraz "halo" nanaša na fluor, klor, brom in jod, in kjer se izraz "alkoksi" nanaša na ravnoverižne ali razvejene alkiloksi skupine, kjer je alkil, kot je definirano prej, in kjer izraz "po izbiri substituiran(a)" pomeni, da je skupina, na katero se ta izraz nanaša, lahko nesubstituirana ali je lahko substituirana z eno ali več skupinami, neodvisno izbranimi izmed halogena, Ci-C6alkila, C2-C6alkenila, Ci-C6haloalkila, Ci-C6alkoksi, hidroksi(Ci.6)alkila, C3-C6cikloalkila, C(O)H, C(O)OH, NHC(O)H, NHC(O)CrC4alkila, C(O)CrC4alkila, NH2, NHCrC4alkila, N(CrC4alkila)2, NO2, OH in CN.
- 2. Spojina po zahtevku 1, kjer je R5 nesubstituirana fenilenska skupina ali fenilenska skupina, substituirana z eno ali več skupinami, neodvisno izbranimi izmed metila, fluora, klora, broma, OCH3 in CF3.
- 3. Spojina po katerem koli od zahtevkov 1 ali 2, kjer sta R7 in R8 oba vodik, R7 in R8 sta oba C i.6alkil ali je R7 vodik in je R8 Ci^alkil.
- 4. Spojina po katerem koli od zahtevkov 1-3, kjer je R6:kjer sta R7 in R8 definirana v zahtevku 1 ali 3.
- 5. Spojina po katerem koli od zahtevkov 1-3, kjer je R6:7 2 kjer sta R in R definirana v zahtevku 1 ali 3.
- 6. Spojina po zahtevku 1, kjer je spojina izbrana iz skupine, ki jo sestavljajo:ali farmacevtsko sprejemljiva sol ali solvat le-teh.
- 7. Spojina po zahtevku 1, kjer je spojina (£)-4-(2-(aminometil)-3-fluoroaliloksi)-/V-terc.-butilbenzamid ali farmacevtsko sprejemljiva sol ali solvat le-tega.
- 8. Farmacevtsko sprejemljiva sol spojine po katerem koli od zahtevkov 1-7.
- 9. Farmacevtsko sprejemljiva sol po zahtevku 8, označena s tem, da je kislinska adicijska sol.
- 10. Farmacevtsko sprejemljiva sol po zahtevku 9, označena s tem, da je kislinska adicijska sol izbrana iz skupine, ki jo sestavljajo hidrokloridi, hidrobromidi, sulfati, formiati, acetati, laktati malati, tartrati, citrati, askorbati, sukcinati, maleati, butirati, valerati in fumarati.
- 11. Farmacevtsko sprejemljiva sol po zahtevku 10, označena s tem, daje kislinska adicijska sol hidrokloridna sol.
- 12. Farmacevtsko sprejemljiva sol po zahtevku 11, pri čemer je farmacevtsko sprejemljiva sol hidroklorid (£)-4-(2-(aminometil)-3-fluoroaliloksi)-2V-ierc.-butilbenzamida.
- 13. Sestavek, ki obsega spojino po katerem koli od zahtevkov 1-7 ali farmacevtsko sprejemljivo sol po katerem koli od zahtevkov 8-12 ali slovat le-te in vsaj en farmacevtsko sprejemljiv ekscipient, nosilec ali razredčilo.
- 14. Spojina po katerem koli od zahtevkov 1-7 ali farmacevtsko sprejemljiva sol po katerem koli od zahtevkov 8-12 ali slovat le-te za uporabo pri postopku zdravljenja bolezni, povezane ali modulirane s proteinom SSAO/VAP-1, ki obsega dajanje individuumu, ki to potrebuje, terapevtsko učinkovite količine spojine ali farmacevtsko sprejemljive soli ali slovata le-te, kjer je bolezen vnetje, fibroza, bolezen, inducirana z diabetesom, nevroinflamatoma bolezen ali rak.
- 15. Spojina ali farmacevtsko sprejemljiva sol ali solvat za uporabo po zahtevku 14, kjer je vnetje povezano z jetrno boleznijo, respiratorno boleznijo, cistično fibrozo, astmo ali kronično obstrukcijsko pljučno boleznijo ali očesno boleznijo.
- 16. Spojina ali farmacevtsko sprejemljiva sol ali solvat za uporabo po zahtevku 14, kjer je bolezen bolezen, inducirana z diabetesom, izbrana iz skupine, ki jo sestavljajo diabetična nefropatija, glomeruloskleroza, diabetična retinopatija, nealkoholna zamaščenost jeter in horoidna neovaskularizacija.
- 17. Spojina ali farmacevtsko sprejemljiva sol ali solvat za uporabo po zahtevku 14 kjer je bolezen izbrana iz skupine, ki jo sestavljajo cistična fibroza, jetrna fibroza, jetrna ciroza, ledvična fibroza, skleroderma, idiopatična pljučna fibroza in fibroza, inducirana z radiacijo.
- 18. Spojina ali farmacevtsko sprejemljiva sol ali solvat za uporabo po zahtevku 17, označena s tem, da je bolezen nealkoholna zamaščenost jeter, nealkoholni steatohepatitis (NASH) ali bolezen, inducirana z alkoholom, ki vodi do ciroze jeter.
Applications Claiming Priority (3)
Application Number | Priority Date | Filing Date | Title |
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US201261641814P | 2012-05-02 | 2012-05-02 | |
EP13784562.4A EP2844637B1 (en) | 2012-05-02 | 2013-04-05 | Substituted 3-haloallylamine inhibitors of ssao and uses thereof |
PCT/AU2013/000356 WO2013163675A1 (en) | 2012-05-02 | 2013-04-05 | Substituted 3-haloallylamine inhibitors of ssao and uses thereof |
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SI2844637T1 true SI2844637T1 (sl) | 2018-07-31 |
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Families Citing this family (51)
Publication number | Priority date | Publication date | Assignee | Title |
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ES2668300T3 (es) * | 2012-05-02 | 2018-05-17 | Boehringer Ingelheim International Gmbh | Inhibidores de SSAO de 3-haloamidina sustituida y usos de los mismos |
GB201304526D0 (en) | 2013-03-13 | 2013-04-24 | Proximagen Ltd | New compounds |
WO2015189534A1 (en) | 2014-06-12 | 2015-12-17 | Proximagen Limited | Vap-1 inhibitors for treating muscular dystrophy |
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