HRP20201416T1 - Terapeutska sredstva na bazi sintetaze lantionin c-sličan 2 - Google Patents

Terapeutska sredstva na bazi sintetaze lantionin c-sličan 2 Download PDF

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HRP20201416T1
HRP20201416T1 HRP20201416TT HRP20201416T HRP20201416T1 HR P20201416 T1 HRP20201416 T1 HR P20201416T1 HR P20201416T T HRP20201416T T HR P20201416TT HR P20201416 T HRP20201416 T HR P20201416T HR P20201416 T1 HRP20201416 T1 HR P20201416T1
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Croatia
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diyl
alkyl
compound
diamine
disease
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HRP20201416TT
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Josep Bassaganya-Riera
Adria CARBO BARRIOS
Richard GANDOUR
Julian D. Cooper
Raquel Hontecillas
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Landos Biopharma, Inc.
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Publication of HRP20201416T1 publication Critical patent/HRP20201416T1/hr

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Claims (15)

1. Spoj, naznačen time, da je predstavljen sljedećom formulom: [image] ili njegova farmaceutski prihvatljiva sol ili njegov ester, u kojoj: Q je piperazin-1,4-diil; 2,5-diazabiciklo[2.2.1]heptan-2,5-diil; 2,5-diazabiciklo[2.2.2]oktan-2,5-diil; 1,4-diazepan-1,4-diil; benzen-1,4-diamin-N1,N4-diil; etan-1,2-diamin-N1,N2-diil; N1,N2-dialkiletan-1,2-diamin-N1,N2-diil; propan-1,3-diamin-N1,N3-diil; N1,N3-dialkilpropan-1,3-diamin-N1,N3-diil; 1,4-diaminoantracen-9,10-dion-1,4-diil; C6-aren-1,4-diamin-N1,N4-diil gdje je aren supstituiran s jednim do četiri supstituenta na pozicijama 2, 3, 5 ili 6 i pritom su supstituenti neovisno odabrani iz skupine koju čine: -C(O)O(C1 do C6)alkil, OH, O(C1 do C6)alkil, (C1 do C6)alkil, CF3, F, Cl i Br; ili supstituirani piperazin-1,4-diil gdje je piperazin supstituiran s jednim do osam supstituenata na pozicijama 2, 3, 5 ili 6 i pritom su supstituenti neovisno odabrani iz skupine koju čine: (C1 do C6)alkil, aril, aril(C1 do C6)alkil, C(O)OH i C(O)O(C1 do C6)alkil; svaki od A1 i A1' je neovisno N ili CR6; svaki od A2 i A2' je neovisno N ili CR7; A3 je NR8; A3' je NR8, O ili S; svaki od A4 i A4' je neovisno N ili CR9; svaki od A5 i A5' je neovisno N ili CR10; svaki od A6 i A6' je neovisno N ili CR11; i ako su prisutni R1, R1', R2, R2', R3, R3', R4, R4', R6, R7, R8, R9, R10 i R11, u svakom pojavljivanju su neovisno odabrani iz skupine koju čine: vodik, alkil, halo, trifluorometil, dialkilamino gdje je svaki alkil isti ili različit, -NH2, alkilamino i arilalkil.
2. Spoj prema patentnom zahtjevu 1, naznačen time, da jedan od A1 i A1' ili oba je/su N.
3. Spoj prema patentnom zahtjevu 2, naznačen time, da jedan od A2 i A2' ili oba je/su CH, A3 je NH, A4 je N, A5 je CH i A6 je CH.
4. Spoj prema patentnom zahtjevu 2, naznačen time, da jedan od A2 i A2' ili oba je/su CH, jedan od A3 i A3' ili oba je/su NH, jedan od A4 i A4' ili oba je/su N, jedan od A5 i A5' ili oba je/su CH, te jedan od A6 i A6' ili oba je/su CH.
5. Spoj prema bilo kojem od patentnih zahtjeva 1 do 4, naznačen time, da Q je piperazin-1,4-diil; 2,5-diazabiciklo[2.2.1]heptan-2,5-diil; 2,5-diazabiciklo[2.2.2]oktan-2,5-diil; 1,4-diazepan-1,4-diil; N1,N2-dialkiletan-1,2-diamin-N1,N2-diil; N1,N3-dialkilpropan-1,3-diamin-N1,N3-diil; 1,4-diaminoantracen-9,10-dion-1,4-diil; C6-aren-1,4-diamin-N1,N4-diil gdje je aren supstituiran s jednim do četiri supstituenta na pozicijama 2, 3, 5 ili 6 i pritom je svaki supstituent neovisno odabran iz skupine koju čine: -C(O)O(C1 do C6)alkil, OH, O(C1 do C6)alkil, (C1 do C6)alkil, CF3, F, Cl i Br; ili supstituirani piperazin-1,4-diil gdje je piperazin supstituiran s jednim do osam supstituenata na pozicijama 2, 3, 5 ili 6 i pritom je svaki supstituent neovisno odabran iz skupine koju čine: (C1 do C6)alkil, aril, aril(C1 do C6)alkil, C(O)OH i C(O)O(C1 do C6)alkil.
6. Spoj prema patentnom zahtjevu 1, naznačen time, da ako su prisutni R1, R1', R2, R2', R3, R3', R4, R4', R6, R7, R8, R9, R10 i R11, u svakom pojavljivanju su neovisno odabrani iz skupine koju čine: vodik, alkil, halo i trifluorometil.
7. Spoj prema patentnom zahtjevu 1, naznačen time, da spoj ima sljedeću strukturu: [image] [image] ; [image] [image] [image] ili njegove soli.
8. Spoj prema patentnom zahtjevu 1, naznačen time, da spoj ima sljedeću strukturu: [image] ili njegove soli.
9. Spoj prema bilo kojem od prethodnih patentnih zahtjeva, naznačen time, da se upotrebljava u postupku liječenja zarazne bolesti, autoimune bolesti, dijabetesa ili kronične upalne bolesti.
10. Spoj za uporabu prema patentnom zahtjevu 9, naznačen time, da se upotrebljava u postupku liječenja zarazne bolesti, gdje zarazna bolest obuhvaća virusnu bolest, opcionalno gdje virusna bolest obuhvaća zarazu gripom.
11. Spoj za uporabu prema patentnom zahtjevu 9, naznačen time, da se upotrebljava u postupku liječenja autoimune bolesti, gdje autoimuna bolest obuhvaća autoimunu upalnu bolest, te pritom autoimuna upalna bolest obuhvaća upalnu bolest crijeva.
12. Spoj za uporabu prema patentnom zahtjevu 11, naznačen time, da se kod autoimune upalne bolesti radi o ulcerativnom kolitisu.
13. Spoj za uporabu prema patentnom zahtjevu 11, naznačen time, da se kod autoimune upalne bolesti radi o Crohnovoj bolesti.
14. Spoj za uporabu prema patentnom zahtjevu 9, naznačen time, da se upotrebljava u postupku liječenja dijabetesa, gdje se kod dijabetesa radi o dijabetesu tipa 1 ili dijabetesu tipa 2.
15. Spoj za uporabu prema patentnom zahtjevu 9, naznačen time, da se upotrebljava u postupku liječenja kronične upalne bolesti, gdje kronična upalna bolest obuhvaća metabolički sindrom.
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