DK2513140T3 - Dobbeltacylerede GLP-1-derivater - Google Patents

Dobbeltacylerede GLP-1-derivater Download PDF

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DK2513140T3
DK2513140T3 DK10788095.7T DK10788095T DK2513140T3 DK 2513140 T3 DK2513140 T3 DK 2513140T3 DK 10788095 T DK10788095 T DK 10788095T DK 2513140 T3 DK2513140 T3 DK 2513140T3
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ethoxy
amino
acetyl
glp
carboxy
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DK10788095.7T
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Patrick William Garibay
Jane Spetzler
Lars Linderoth
Jesper Lau
Per Sauerberg
János Tibor Kodra
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Novo Nordisk As
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Claims (13)

1. Derivat af en GLP-1 analogi, hvilken analogi omfatter en første K-rest ved en position svarende til position 37 af GLP-1 (7-37) (SEQ ID NO: 1), en anden K-rest ved en position svarende til position 26 af GLP-l(7-37), hvori den første K-rest er designeret K37, og den anden K-rest er designeret K26, hvilken analogi har maksimalt ti aminosyremodifikationer sammenlignet med GLP-1 (7-37), herunder K37 og et Q eller et R ved en position svarende til position 34 af GLP-1 (7-37); hvilken derivat omfatter to albuminbindingsdele bundet til henholdsvis K26 og K37, hvori albuminbindingsdelen omfatter en forlængende del med formlen
hvori y er et heltal i området 7-15; eller et farmaceutisk acceptabelt salt, amid eller ester deraf.
2. Derivat ifølge krav 1, hvori analogien har maksimalt fem aminosyremodifikationer.
3. Derivat ifølge ethvert af krav 1-2, hvori analogien omfatter Imp7 og/eller Aib8.
4. Derivat ifølge ethvert af krav 1-3, hvori analogien omfatter Aib8.
5. Derivat ifølge ethvert af krav 1-4, hvori analogien ikke omfatter H31 og Q34.
6. Derivat ifølge ethvert af krav 1-5, hvori analogien omfatter følgende aminosy remodifikationer sammenlignet med GLP-l(7-37) (SEQ ID NO: 1): 8Aib, 34R, 37K.
7. Derivat ifølge ethvert af krav 1-6, hvori analogien har følgende aminosyremodifikationer sammenlignet med GLP-l(7-37) (SEQ ID NO: 1): 8Aib, 34R, 37K.
8. Derivat ifølge ethvert af krav 1-7, hvori y er 9.
9. Derivat ifølge ethvert af krav 1-8, hvori albuminbindingsdelen yderligere omfatter Chem. 6 og/eller Chem. 5: Chem. 6:
hvori k er et heltal i området 1-5, og n er et heltal i området 1-5.
10. Forbindelse valgt blandt følgende: A/£26-[2-(2-12-[10-(4-Karboxyfenoxy)decanoylamino]ethoxy} ethoxy)acetyl], Νε37- [2-(2-{2-[lO-(4-Karboxyfenoxy)decanoylamino]ethoxy}ethoxy)acetyl]- [Aib8,Arg34,Lys37]GLP-l(7-37)-peptid, Chem. 20:
A/e26{2-[2-(2-{2-[2-(2-{(S)-4-Karboxy-4-[10-(4-karboxyfenoxy)decanoylamino] butyrylamino}ethoxy)ethoxy]acetylamino}ethoxy)ethoxy]acetyl}, Α/ε37-{2-[2-(2-{2-(2-(2-{(S)-4-karboxy-4-[10-(4-karboxyfenoxy)decanoylamino]butyrylamino} ethoxy)ethoxy]acetylamino}ethoxy)ethoxy]acetyl}-[Aib8,Arg34,Lys37]GLP-l(7-37) -peptid, Chem. 21:
/\/£26-{2-[2-(2-{2-[2-(2-{(S)-4-Karboxy-4-[ 16-(4- karboxyfenoxy)hexadecanoylamino]butyrylamino}ethoxy) ethoxy]acetylamino> ethoxy)ethoxy]acetyl>, A/e37-{2-[2-(2-{2-[2-(2-{(S)-4-Karboxy-4-[16-(4- karboxyfenoxy)hexadecanoylamino]butyrylamino}ethoxy)ethoxy] acetyla- mino>ethoxy)ethoxy]acetyl>-[Aib8,Arg34,Lys37]GLP-l (7-37) -peptid, Chem. 32:
/V£26-{2-[2-(2-{(S)-4-Karboxy-4-[10-(4-karboxyfenoxy)decanoylamino] butyryla-mino}ethoxy)-ethoxy]acetyl}, A/e37-{2-[2-(2-{(S)-4-Karboxy-4-[ 10-(4- karboxyfenoxy)decanoylamino]-butyrylamino}ethoxy)ethoxy]acetyl} [Aib8, Arg34, Lys37]GLP-l (7-37)-peptid, Chem. 34:
A/£26-[2-(2-[2-(2-[2-(2-[4-(10-(4-Karboxyfenoxy)decanoylamino)-4(S)-karboxybutyrylamino]ethoxy)ethoxy]acetylamino)ethoxy]ethoxy)acetyl]-/V£37-[2-(2-[2-(2-[2-(2-[4-(10-(4-Karboxyfenoxy)decanoylamino)-4(S)-karboxybutyrylamino] ethoxy)ethoxy]acetylamino) ethoxy]ethoxy) acetyl] [Aib8,His31,Gin34,Lys37]GLP-l(7-37) -peptid, Chem. 36:
A/e26-((S)-4-Karboxy-4-{(S)-4-karboxy-4-[10-(4-karboxyfenoxy)-decanoylamino]butyrylamino>butyryl), /Ve37-((S)-4-Karboxy-4-{(S)-4-karboxy-4-[10-(4-karboxyfenoxy)-decanoylamino]butyrylamino}butyryl)[Aib8, Arg34, Lys37] GLP-l(7-37)-peptid, Chem. 38:
A/9-{2-[2-(lH-Imidazol-4-yl)etylkarbamoyl]-2-metylpropionyl)·^ -{2-[2-(2-(2- [2-(2-{(S)-4-Karboxy-4-[10-(4-karboxyfenoxy)decanoylamino]butyrylamin°} ethoxy)ethoxy]acetylamino}ethoxy)ethoxy]acet yl}, /ve57-{2-[2-(2-{2-[2-(2-{(S)-
4-Karboxy-4-[10-(4-karboxyfenoxy)decanoylamino]butyrylamino}ethoxy) eth- oxy]acetylamino}ethoxy)ethoxy]acetyl} [Arg34, Lys37]GLP-l(9-37)-peptid, Chem. 42:
A/e26-[2-[2-[2-[[2-[2-[2-[[(4S)-4-karboxy-4-[10-(4-karboxyfenoxy) decanoyl-amino]butanoyl]amino]ethoxy]ethoxy]acetyl]amino]ethoxy]ethoxy]acetyl],N£57-[2-[2-[2-[[2-[2-[2-[[(4S)-4-karboxy-4-[10-(4-karboxyfenoxy) decanoylamino] butanoyl]amino]ethoxy]ethoxy]acetyl]amino]ethoxy]ethoxy]acetyl]-[Imp7, Arg34, Lys37]-GLP-l-(7-37)-peptid, Chem. 47:
N£26-[2-[2-[2-[[2-[2-[2-[[(4S)-4-karboxy-4-[10-(4-karboxyfenoxy)decanoyl-amino]butanoyl]amino]ethoxy] ethoxy]acetyl]amino]ethoxy]ethoxy]acetyl], Νε57-[2-[2-[2-[[2-[2-(2-[[(4S)-4-karboxy-4-[10-(4-karboxyfenoxy)decanoylamino]bu-tanoyl]amino]ethoxy]ethoxy]acetyl]amino]ethoxy]ethoxy]acetyl]-[Arg34,Lys37]-GLP-l-(7-37)-peptid, Chem. 48:
N£26-[2-[2-[2-[[2-[2-[2-[[(4S)-4-karboxy-4-[10-(4-karboxyfenoxy) deca- noylamino]butanoyl]amino]ethoxy]ethoxy]acetyl]amino] ethoxy]ethoxy]acetyl], /V£57-[2-[2-[2-[[2-[2-[2-[[(4S)-4-karboxy-4-[10-(4-karboxyfenoxy)decanoyl-amino]butanoyl]amino]ethoxy] ethoxy]acetyl]amino]ethoxy]ethoxy]acetyl]-[Aib8, Gly9, Arg34, Lys37]-GLP-l-(7-37)-peptid, Chem. 49:
N£26-[2-[2-[2-[[2-[2-[2-[[(4S)-4-karboxy-4-[10-(4-karboxyfenoxy)decanoyl-amino]butanoyl]amino]ethoxy]ethoxy]acetyl]amino]ethoxy]ethoxy]a cetyl], Νε37-[2-[2-[2-[[2-[2-[2-[[(4S)-4-karboxy-4-[10-(4-karboxyfenoxy)decanoylamino]bu-tanoyl]amino]ethoxy]ethoxy]acetyl]amino]ethoxy]ethoxy]acetyl]-[Aib8, Arg23, Arg34, Lys37]-GLP-l-(7-37)-peptid, Chem. 50:
Ne26-[2-[2-[2-[[2-[2-[2-[[(4S)-4-karboxy-4-[10-(4-karboxyfenoxy) deca- noylamino]butanoyl]amino]ethoxy]ethoxy] acetyl]amino]ethoxy]ethoxy]acetyl], Ne37-[2-[2-[2-[[2-[2-[2-[[(4S)-4-karboxy-4-[10-(4-karboxyfenoxy) deca- noylamino]butanoyl]amino]ethoxy]ethoxy] acetyl]amino]ethoxy]ethoxy]a cetyΠΕΗ is31,Gin34,Lys37]-GLP-l-(7-37)-peptid, Chem. 52:
Ne26-[(4S)-4-karboxy-4-[[2-[2-[2-[[2-[2-[2-[10-(4-karboxyfenoxy)decanoyl-amino]ethoxy]ethoxy]acetyl]amino]ethoxy]ethoxy]acetyl]amino]butanoyl], Νε37-[(4S)-4-karboxy-4-[[2-[2-[2-[[2-[2-[2-[10-(4-karboxyfenoxy)decanoylamino] ethoxy]ethoxy]acetyl]amino]ethoxy]ethoxy]acetyl]amino]butanoyl]-[His31, Gin34, Lys37]-GLP-l-(7-37)-peptid, Chem. 55:
N£26-[2-[2-[2-[[2-[2-[2-[[(4S)-4-karboxy-4-[10-(4-karboxyfenoxy)decanoyl-amino]butanoyl]amino]ethoxy]ethoxy]acetyl] amino]ethoxy]ethoxy]acetyl], Νε37-[2-[2-[2-[[2-[2-[2-[[(4S)-4-karboxy-4-[10-(4-karboxyfenoxy)decanoylamino]bu-tanoyl]amino]ethoxy]ethoxy]acetyl]amino]ethoxy]ethoxy]acetyl]-[Gln9, Arg34, Lys37]-GLP-l-(7-37)-peptid, Chem, 56:
Ne26-[2-[2-[2-[[2-[2-[2-[[(4S)-4-karboxy-4-[10-(4-karboxyfenoxy)decanoylami-no]butanoyl]amino]ethoxy]ethoxy]acetyl]amino]ethoxy]ethoxy]acetyl], Νε37-[2-[2-[2-[[2-[2-[2-[[(4S)-4-karboxy-4-[10-(4-karboxyfenoxy)decanoylamino] buta-noyl]amino]ethoxy]ethoxy]acetyl]amino]ethoxy]ethoxy]acetyl]-[Glu30, Arg34, Lys37]-GLP-l-(7-37)-peptid, Chem. 57:
N£26-[2-[2-[2-[[2-[2-[2-[[(4S)-4-karboxy-4-[8-(4-karboxyfenoxy) oc- tanoylamino]butanoyl]amino]ethoxy]ethoxy]acetyl]amino] ethoxy]ethoxy]a cetyl], N£37-[2-[2-[2-[[2-[2-[2-[[(4S)-4-karboxy-4-[8-(4-karboxyfenoxy) oc-tanoylamino]butanoyl]amino]ethoxy]ethoxy]acetyl]amino]ethoxy]ethoxy]acetyl]-[Aib8,Arg34,Lys37]-GLP-l-(7-37)-peptid, Chem. 58:
Ne26-[2-[2-[2-[[2-[2-[2-[[(4S)-4-karboxy-4-[8-(4-karboxyfenoxy) oc- tanoylamino]butanoyl]amino]ethoxy]ethoxy]acetyl]amino] ethoxy]ethoxy]acetyl], N£37-[2-[2-[2-[[2-[2-[2-[[(4S)-4-karboxy-4-[8-(4-karboxyfenoxy)octanoylamino] butanoyl]amino]ethoxy]ethoxy]acetyl]amino]ethoxy]ethoxy]acetyl]-[Arg34,Lys37]-GLP-l-(7-37)-peptid, Chem. 59:
N{9>-[2,2-dimetyl-3-oxo-3-(pyridin-2-ylmetylamino)propanoyl], Νε26-[2-[2-[2-[[2-[2-[2-[[(4S)-4-karboxy-4-[10-(4-karboxyfenoxy)decanoylamino]butanoyl] amino]ethoxy]ethoxy]acetyl]amino] ethoxy]ethoxy]a cetyl], Νε37-[2-[2-[2-[[2-[2-[2-[[(4S)-4-karboxy-4-[10-(4-karboxyfenoxy) decanoylamino]butanoyl]amino] ethoxy]ethoxy]acetyl]amino]ethoxy]ethoxy]acetyl]-[Arg34,Lys37]-GLP-l-(9-37)- peptid, Chem. 60:
Ne26-[2-[2-[2-[[2-[2-[2-[[(4S)-4-karboxy-4-[10-(4-karboxyfenoxy)decanoyl-amino]butanoyl]amino]ethoxy]ethoxy]acetyl]amino]ethoxy]ethoxy]acetyl], Νε37-[2-[2-[2-[[2-[2-[2-[[(4S)-4-karboxy-4-[10-(4-karboxyfenoxy)decanoyl-amino]butanoyl]amino]ethoxy]ethoxy]acetyl]amino]ethoxy]ethoxy]acetyl]-[Arg34, Lys37]-GLP-l-(7-37)-peptidyl-Gly, Chem. 61:
Ne26-[2-[2-[2-[[2-[2-[2-[[(4S)-4-karboxy-4-[10-(4-karboxyfenoxy) deca- noylamino]butanoyl]amino]ethoxy]ethoxy]acetyl]amino] ethoxy]ethoxy]a cetyl], Ne37-[2-[2-[2-[[2-[2-[2-[[(4S)-4-karboxy-4-[10-(4-karboxyfenoxy) deca- noylamino]butanoyl]amino]ethoxy]ethoxy]acetyl]amino]ethoxy]ethoxy]acetyl]-[Arg34,Gly36,Lys37]-GLP-l-(7-37)-peptid, Chem. 62: |
N£26-[2-[2-[2-[[2-[2-[2-[[(4S)-4-karboxy-4-[9-(4-karboxyfenoxy)nonanoylamino] butanoyl]amino]ethoxy]ethoxy]acetyl]amino]ethoxy]ethoxy]acetyl], Νε37-[2-[2-[2-[[2-[2-[2-[[(4S)-4-karboxy-4-[9-(4-karboxyfenoxy)nonanoylamino] buta- noyl]amino]ethoxy]ethoxy]acetyl]amino]ethoxy]ethoxy]acetyl]-[Arg34,Lys37]-GLP- l-(7-37)-peptid, Chem. 63:
N£26-[2-[2-[[2-[2-[2-[[(4S)-4-karboxy-4-[10-(4-karboxyfenoxy)decanoyiamino] butanoyl]amino]ethoxy]ethoxy]acetyl]amino]ethoxy]ethoxy]acetyl], Νε57-[2-[2-[2-[[2-[2-[2-[[(4S)-4-karboxy-4-[10-(4-karboxyfenoxy)decanoylamino] buta-noyl]amino]ethoxy]ethoxy]acetyl]amino]ethoxy]ethoxy]acetyl]-[Arg34,Lys37]'GLP-l-(7-37)-peptidyl-Glu, Chem. 65:
Ne26-[2-[2-[2-[[2-[2-[2-[[(2S)-4-karboxy-2-[10-(4-karboxyfenoxy) deca- noylamino] butanoyl]amino]ethoxy]ethoxy]acetyl]amino]ethoxy]ethoxy]acetyl], Ne37-[2-[2-[2-[[2-[2-[2-[[(2S)-4-karboxy-2-[10-(4-karboxyfenoxy) deca' noylamino]butanoyl]amino]ethoxy]ethoxy]acetyl]amino]ethoxy]ethoxy]acetyl]- [Aib8,Arg34,Lys37]-GLP-l-(7-37)-peptid, Chem. 67:
Ne26-[2-[2-[2-[[2-[2-[2-[[(4S)-4-karboxy-4-[8-(4-karboxyfenoxy) octanoylami-no]butanoyl]amino]ethoxy]ethoxy]acetyl]amino]ethoxy]ethoxy]acetyl], Νε37-[2-[2-[2-[[2-[2-[2-[[(4S)-4-karboxy-4-[8-(4-karboxyfenoxy) octanoylaminojbuta-noyl]amino]ethoxy]ethoxy]acetyl]amino]ethoxy]ethoxy]acetyl]-[Arg34, Gly36, Lys37]-GLP-l-(7-37)-peptid, og Chem. 68:
eller et farmaceutisk acceptabelt salt, amid eller ester deraf.
11. Forbindelse ifølge ethvert af krav 1-10, til anvendelse som medikament.
12. Forbindelse ifølge ethvert af krav 1-10, til anvendelse ved behandling og/eller forebyggelse af alle former for diabetes og relaterede sygdommer, såsom spiseforstyrrelser, hjerte-kar sygdomme, mave-tarm sygdomme, diabetiske komplikationer, kritisk sygdom og/eller poycystisk ovariesyndrom; og/eller til forbedring af lipidparametre, forbedring af β-celle funktion, og/eller til forsinkelse eller forebyggelse af udvikling i diabetisk sygdom.
13. Anvendelse af en forbindelse ifølge ethvert af krav 1-10 ved fremstilling af et medikament til behandling og/eller forebyggelse af alle former for diabetes og relaterede sygdomme, såsom spiseforstyrrelser, hjerte-kar sygdomme, mave-tarm sygdomme, diabetiske komplikationer, kritisk sygdom og/eller poycystisk ovariesyndrom; og/eller til forbedring af lipidparametre, forbedring af β-celle funktion, og/eller til forsinkelse eller forebyggelse af udvikling i diabetisk sygdom.
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