HRP20171726T1 - Derivati eksendin-4 kao dvostruki glp1/glukagon agonisti - Google Patents
Derivati eksendin-4 kao dvostruki glp1/glukagon agonisti Download PDFInfo
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- HRP20171726T1 HRP20171726T1 HRP20171726TT HRP20171726T HRP20171726T1 HR P20171726 T1 HRP20171726 T1 HR P20171726T1 HR P20171726T T HRP20171726T T HR P20171726TT HR P20171726 T HRP20171726 T HR P20171726T HR P20171726 T1 HRP20171726 T1 HR P20171726T1
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- carboxy
- butyryl
- ethoxy
- amino acid
- acid residue
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- 125000004122 cyclic group Chemical group 0.000 claims 1
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Claims (31)
1. Peptidni spoj koji ima formulu (I):
R1-Z-R2(I)
naznačen time da Z je peptidni dio koji ima formulu (II)
[image]
X2 predstavlja aminokiselinski ostatak koji se bira od Ser, D-Ser i Aib,
X3 predstavlja aminokiselinski ostatak koji se bira od Gln, His i α-amino- funkcionaliziranog Gln, pri čemu Gln može biti funkcionaliziran tako da H iz skupine α-NH2 je supstituiran s (C1-C4)-alkil,
X14 predstavlja aminokiselinski ostatak koji se bira od Lys, Orn, Dab i Dap, pri čemu je -NH2 skupina bočnog lanca funkcionalizirana s -C(O)-R5,
X15 predstavlja aminokiselinski ostatak koji se bira od Glu i Asp,
X16 predstavlja aminokiselinski ostatak koji se bira od Ser, Lys i Glu,
X17 predstavlja aminokiselinski ostatak koji se bira od Arg, Glu, Gln, Leu i Lys,
X18 predstavlja aminokiselinski ostatak koji se bira od Arg i Ala,
X20 predstavlja aminokiselinski ostatak koji se bira od Gln, Arg, Lys i Aib,
X21 predstavlja aminokiselinski ostatak koji se bira od Asp, Leu i Glu,
X28 predstavlja aminokiselinski ostatak koji se bira od Asn, Arg, Lys, Aib, Ser, Glu, Asp i Ala,
X29 predstavlja aminokiselinski ostatak koji se bira od Gly, Ala, D-Ala i Thr,
X35 predstavlja aminokiselinski ostatak koji se bira od Ala ili Glu,
X39 je Ser ili je odsutan,
X40 je ili odsutan ili predstavlja Lys, pri čemu -NH2 skupina bočnog lanca može biti funkcionalizirana s -C(O)-R5 i
R5 je lipofilna skupina koja se bira od acikličke ravne ili razgranate (C4-C30) zasićene ili nezasićene ugljikovodične skupine, i/ili cikličke zasićene, nezasićene ili aromatske skupine, pri čemu lipofilna skupina može se vezati na -NH2 skupinu bočnog lanca pomoću poveznice koja se bira od (β-Ala)1-4, (γ-Glu)1-4, (ε-Ahx)1-4, ili (GABA)1-4 u svim stereoizomernim oblicima;
R1 predstavlja N-terminalnu skupinu peptidnog spoja i odabran je od NH2 i mono- ili bisfunkcionaliziranog NH2,
R2 predstavlja C-terminalnu skupinu peptidnog spoja i odabran je od
(i) OH ili funkcionaliziranog OH i
(ii) NH2 ili mono- ili bisfunkcionaliziranog NH2,
ili njegova sol ili solvat, i
pri čemu je spoj dvostruki agonist receptora GLP-1 i glukagona.
2. Spoj prema zahtjevu 1, naznačen time da
X14 predstavlja aminokiselinski ostatak koji se bira od Lys, Orn, Dab i Dap, pri čemu je -NH2 skupina bočnog lanca funkcionalizirana s -C(O)-R5,
X40 predstavlja Lys, pri čemu -NH2 skupina bočnog lanca može biti funkcionalizirana s -C(O)-R5, i -C(O)-R5 odabran je od
(S)-4-karboksi-4-heksadekanoilamino-butiril-, (S)-4-karboksi-4-oktadekanoilamino-butiril-,4-Heksadekanoil amino-butiril-, 4-{3-[(R)-2,5,7,8-tetrametil-2-((4R,8R)-4,8,12-trimetil-tridecil)-kroman-6-iloksikarbonil]-propionil amino}-butiril-, 4-oktadekanoilamino-butiril-, 4-((Z)-oktadek-9-enoilamino)-butiril-, 6-[(4,4-Difenil-ciklo heksiloksi)-hidroksi-fosforiloksi]-heksanoil-, Heksadekanoil-, (S)-4-karboksi-4-(15-karboksi-penta dekanoil amino)-butiril-, (S)-4-karboksi-4-{3-[3-((2S,3R,4S,5R)-5-karboksi-2,3,4,5-tetrahidroksi-pentanoil amino)-propionilamino]-propionilamino}-butiril, (S)-4-karboksi-4-{3-[(R)-2,5,7,8-tetrametil-2-((4R,8R)-4,8,12-trimetil-tridecil)-kroman-6-iloksikarbonil]-propionilamino}-butiril-, (S)-4-karboksi-4-((9Z,12Z)-oktadeka-9,12-dienoil amino)-butiril-, (S)-4-karboksi-4-[6-((2S,3R,4S,5R)-5-karboksi-2,3,4,5-tetrahidroksi-pentanoilamino)-heksanoil amino]-butiril, (S)-4-karboksi-4-((2S,3R,4S,5R)-5-karboksi-2,3,4,5-tetrahidroksi-pentanoilamino)-butiril, (S)-4-karboksi-4-tetradekanoilamino-butiril-, (S)-4-(11-Benziloksikarbonil-undekanoilamino)-4-karboksi-butiril, (S)-4-karboksi-4-[11-((2S,3R,4R,5R)-2,3,4,5,6-pentahidroksi-heksilkarbamoil)-undekanoilamino]-butiril-, (S)-4-karboksi-4-((Z)-oktadek-9-enoilamino)-butiril-, (S)-4-karboksi-4-(4-dodeciloksi-benzoilamino)-butiril-, (S)-4-karboksi-4-henicosanoilamino-butiril-, (S)-4-karboksi-4-docosanoilam ino-butiril-, (S)-4-karboksi-4-((Z)-nonadek-10-enoilamino)-butiril-, (S)-4-karboksi-4-(4-deciloksi-benzoilamino)-butiril-, (S)-4-karboksi-4-[(4'-octiloksi-bifenil-4-karbonil)-amino]-butiril-, (S)-4-karboksi-4-(12-fenil-dodekanoilamino)-butiril-, (S)-4-karboksi-4-icosanoilamino-butiril-, (S)-4-karboksi-4-((S)-4-karboksi-4-heksadekanoilamino-butirilamino)-butiril-, (S)-4-karboksi-4-((S)-4-karboksi-4-oktadekanoilamino-butirilamino)-butiril-, 3-(3-Oktadekanoilamino-propionilamino)-propionil-, 3-(3-Heksadekanoilamino-propionilamino)-propionil-, 3-Heksadekanoilam ino-propionil-, (S)-4-karboksi-4-[(R)-4-((3R,5S,7R,8R,9R,10S,12S,13R,14R,17R)-3,7,12-trihidroksi-8,10,13-trimetil-heksadecahidro-ciklopenta[a]fenanthren-17-il)-pentanoilamino]-butiril-, (S)-4-karboksi-4-[(R)-4-((3R,5R,8 R,9S,10S, 13R,14S, 17R)-3-hidroksi-10,13-dimetilheksadecahidro-ciklopenta[a]fenanthren-17-il)-pentanoilamino]-butiril-, (S)-4-karboksi-4-((9S,10R)-9,10,16-trihidroksiheksadekanoilamino)-butiril-, tetradekanoil-, 11-karboksi-undekanoil-, 11-Benziloksikarbonil-undekanoil, (S)-4-karboksi-4-((S)-4-karboksi-4-tetradekanoilamino-butirilamino)-butiril-, 6-[Hidroksi-(naphthalen-2-iloksi)-fosforiloksi]-heksanoil-, 6-[Hidroksi-(5-fenil-pentiloksi)-fosforiloksi]-heksanoil-, 4-(Naphthalene-2-sulfonilamino)-4-okso-butiril-, 4-(Bifenil-4-sulfonilamino)-4-okso-butiril-, (S)-4-karboksi-4-{(S)-4-karboksi-4-[2-(2-{2-[2-(2-{2-[(S)-4-karboksi-4-(17-karboksi-heptadekanoilamino)-butirilamino]-etoksi}-etoksi)-acetilamino]-etoksi}-etoksi)-acetilamino]-butirilamino}-butiril-, (S)-4-karboksi-4-[2-(2-{2-[2-(2-{2-[(S)-4-karboksi-4-(17-karboksi-heptadekanoilamino)-butirilamino]-etoksi}-etoksi)-acetilamino]-etoksi}-etoksi)-acetilamino]-butiril, (S)-4-karboksi-2-{(S)-4-karboksi-2-[2-(2-{2-[2-(2-{2-[(S)-4-karboksi-4-(17-karboksi-heptadekanoilamino)-butirilamino]-etoksi}-etoksi)-acetilamino]-etoksi}-etoksi)-acetilamino]-butirilamino}-butiril, (S)-4-karboksi-2-[2-(2-{2-[2-(2-{2-[(S)-4-karboksi-4-(17-karboksi-heptadekanoilamino)-butirilamino]-etoksi}-etoksi)-acetilamino]-etoksi}-etoksi)-acetilamino]-butiril, (S)-4-karboksi-4-{(S)-4-karboksi-4-[2-(2-{2-[(S)-4-karboksi-4-(17-karboksiheptadekanoilamino)-butirilamino]-etoksi}-etoksi)-acetilamino]-butirilamino}-butiril, (S)-4-karboksi-4-[2-(2-{2-[(S)-4-karboksi-4-(17-karboksi-heptadekanoilamino)-butirilamino]-etoksi}-etoksi)-acetilamino]-butiril,(S)-4-karboksi-2-{(S)-4-karboksi-2-[2-(2-{2-[(S)-4-karboksi-4-(17-karboksi-heptadekanoilamino)-butirilamino]-etoksi}-etoksi)-acetilamino]-butirilamino}-butiril, (S)-4-karboksi-2-[2-(2-{2-[(S)-4-karboksi-4-(17-karboksi-heptadekanoilamino)-butirilamino]-etoksi}-etoksi)-acetilamino]-butiril, 2-(2-{2-[2-(2-{2-[(S)-4-karboksi-4-(17-karboksi-heptadekanoilamino)-butirilamino]-etoksi}-etoksi)-acetilamino]-etoksi}-etoksi)-acetil-, 2-(2-{2-[(S)-4-karboksi-4-(17-karboksi-heptadekanoilamino)-butirilamino]-etoksi}-etoksi)-acetil, (S)-4-karboksi-4-((S)-4-karboksi-4-{(S)-4-karboksi-4-[(S)-4-karboksi-4-(19-karboksi-nonadekanoilamino)-butirilamino]-butirilamino}-butirilamino)-butiril, 2-(2-{2-[2-(2-{2-[(S)-4-karboksi-4-(16-1 H-tetrazol-5-il-heksadekanoilamino)-butirilamino]-etoksi}-etoksi)-acetilamino]-etoksi}-etoksi)-acetil, 2-(2-{2-[2-(2-{2-[(S)-4-karboksi-4-(16-karboksiheksadekanoilamino)-butirilamino]-etoksi}-etoksi)-acetilamino]-etoksi}-etoksi)-acetil, (S)-4-karboksi-4-{(S)-4-karboksi-4-[(S)-4-karboksi-4-(17-karboksi-heptadekanoilamino)-butirilamino]-butirilamino}-butiril, (S)-4-karboksi-4-((S)-4-karboksi-4-{2-[2-(2-{2-[2-(2-{(S)-4-karboksi-4-[10-(4-karboksi-fenoksi)-dekanoilamino]-butirilamino}-etoksi)-etoksi]-acetilamino}-etoksi)-etoksi]-acetilamino}-butiril, (S)-4-karboksi-4-{(S)-4-karboksi-4-[2-(2-{2-[2-(2-{2-[(S)-4-karboksi-4-(7-karboksi-heptanoilamino)-butirilamino]-etoksi}-etoksi)-acetilamino]-etoksi}-etoksi)-acetilamino]-butirilamino}-butiril, (S)-4-karboksi-4-{(S)-4-karboksi-4-[2-(2-{2-[2-(2-{2-[(S)-4-karboksi-4-(11-karboksi-undekanoilamino)-butirilamino]-etoksi}-etoksi)-acetilamino]-etoksi}-etoksi)-acetilamino]-butirilamino}-butiril, (S)-4-karboksi-4-{(S)-4-karboksi-4-[2-(2-{2-[2-(2-{2-[(S)-4-karboksi-4-(13-karboksi-tridekanoilamino)-butirilamino]-etoksi}-etoksi)-acetilamino]-etoksi}-etoksi)-acetilamino]-butirilamino}-butiril, (S)-4-karboksi-4-{(S)-4-karboksi-4-[2-(2-{2-[2-(2-{2-[(S)-4-karboksi-4-(15-karboksi-pentadekanoilamino)-butirilamino]-etoksi}-etoksi)-acetilamino]-etoksi}-etoksi)-acetilamino]-butirilamino}-butiril, i (S)-4-karboksi-4-{(S)-4-karboksi-4-[2-(2-{2-[2-(2-{2-[(S)-4-karboksi-4-(19-karboksi-nonadekanoilamino)-butirilamino]-etoksi}-etoksi)-acetilamino]-etoksi}-etoksi)-acetilamino]-butirilamino}-butiril.
3. Spoj prema bilo kojem od zahtjeva 1 - 2,
naznačen time da
R1 je NH2,
R2 je NH2 ili
R1 i R2 su NH2.
4. Spoj prema bilo kojem od zahtjeva 1 - 3
naznačen time da
X14 je Lys, koji je funkcionaliziran sa skupinom -C(O)R5, pri čemu R5 je kao što je opisano u bilo kojem od zahtjeva 1 - 2.
5. Spoj prema bilo kojem od zahtjeva 1, 3, 4, naznačen time da
X14 je Lys, koji je funkcionaliziran sa skupinom -C(O)R5, pri čemu R5 sadrži lipofilni dio, acikličku linearnu ili razgranatu (C12-C22) zasićenu ugljikovodičnu skupinu vezanu izravno na -NH2 skupinu bočnog lanca ili vezanu na -NH2 skupinu bočnog lanca pomoću poveznice odabrane iz skupine koju čine ß-Ala, γ-Glu, ß-Ala-ß-Ala i γ-Glu-γ-Glu u svim stereoizomernim oblicima.
6. Spoj prema bilo kojem od zahtjeva 1 - 5, naznačen time da
X2 predstavlja aminokiselinski ostatak koji se bira od D-Ser i Aib,
X3 predstavlja Gln,
X14 predstavlja aminokiselinski ostatak koji se bira od Lys i Orn,
pri čemu je -NH2 skupina bočnog lanca funkcionalizirana s -C(O)-R5,
X15 predstavlja aminokiselinski ostatak koji se bira od Glu i Asp,
X16 predstavlja aminokiselinski ostatak koji se bira od Ser i Glu,
X17 predstavlja aminokiselinski ostatak koji se bira od Arg, Gln i Lys,
X18 predstavlja aminokiselinski ostatak koji se bira od Arg i Ala,
X20 predstavlja aminokiselinski ostatak koji se bira od Gln, Arg, Lys i Aib,
X21 predstavlja aminokiselinski ostatak koji se bira od Asp, Leu i Glu,
X28 predstavlja aminokiselinski ostatak koji se bira od Asn, Arg, Lys, Aib, Ser i Ala,
X29 predstavlja aminokiselinski ostatak koji se bira od Gly, Ala ili Thr,
X35 predstavlja Ala,
X39 je Ser ili je odsutan,
X40 je ili odsutan ili predstavlja Lys, pri čemu -NH2 skupina bočnog lanca može biti funkcionalizirana s -C(O)-R5 i
-C(O)-R5 je kao što je definirano u zahtjevu 1.
7. Spoj prema bilo kojem od zahtjeva 1 - 6, naznačen time da X20 predstavlja aminokiselinski ostatak koji se bira od Gln, Lys i Aib.
8. Spoj prema bilo kojem od zahtjeva 1 - 7, naznačen time da
X2 predstavlja aminokiselinski ostatak koji se bira od D-Ser i Aib,
X3 predstavlja Gln,
X14 predstavlja Lys, pri čemu je -NH2 skupina bočnog lanca funkcionalizirana s jednom od skupina odabranih od 3-(3-oktadekanoilamino-propionilamino)-propionil-, 4-heksadekanoilamino-butiril-, 4-{3-[(R)-2,5,7,8-tetrametil-2-((4R,8R)-4,8,12-trimetil-tridecil)-kroman-6-iloksikarbonil]-propionilamino}-butiril-, 4-oktadekanoilamino-butiril-, 4-((Z)-oktadek-9-enoilamino)-butiril-, heksadekanoil-, (S)-4-karboksi-4-((Z)-oktadek-9-enoilamino)-butiril-, (S)-4-karboksi-4-(4-dodeciloksibenzoilamino)-butiril-, (S)-4-karboksi-4-henicosanoilamino-butiril-, (S)-4-karboksi-4-docosanoilamino-butiril-, (S)-4-karboksi-4-((Z)-nonadek-10-enoilamino)-butiril-, (S)-4-karboksi-4-(4-deciloksibenzoilamino)-butiril-, (S)-4-karboksi-4-[(4'-octiloksi-bifenil-4-karbonil)-amino]-butiril-, (S)-4-karboksi-4-(12-fenildodekanoilamino)-butiril-, (S)-4-karboksi-4-((S)-4-karboksi-4-heksadekanoilamino-butirilamino)-butiril-, (S)-4-karboksi-4-((S)-4-karboksi-4-oktadekanoilamino-butirilamino)-butiril-, (S)-4-karboksi-4-{3-[(R)-2,5,7,8-tetrametil-2-((4R,8R)-4,8,12-trimetil-tridecil)-kroman-6-iloksikarbonil]-propionilamino}-butiril-, (S)-4-karboksi-4-((9Z,12Z)-oktadeka-9,12-dienoilamino)-butiril-, (S)-4-karboksi-4-oktadekanoilamino-butiril- i (S)-4-karboksi-4-heksadekanoilaminobutiril-,
X15 predstavlja Glu,
X16 predstavlja Ser,
X17 predstavlja aminokiselinski ostatak koji se bira od Arg, Gln i Lys,
X18 predstavlja Ala,
X20 predstavlja Gln,
X21 predstavlja Asp,
X28 predstavlja Ala,
X29 predstavlja Gly,
X35 predstavlja Ala,
X39 je Ser
X40 je odsutan.
9. Spoj prema bilo kojem od zahtjeva 1 - 5, naznačen time da
X2 predstavlja Aib,
X3 predstavlja Gln,
X14 predstavlja Lys, pri čemu je -NH2 skupina bočnog lanca funkcionalizirana, naročito sa (S)-4-karboksi-4-heksadekanoilaminobutiril- i (S)-4-karboksi-4-oktadekanoilamino-butiril-;
X15 predstavlja aminokiselinski ostatak koji se bira od Asp i Glu,
X16 predstavlja aminokiselinski ostatak koji se bira od Ser i Glu,
X17 predstavlja aminokiselinski ostatak koji se bira od Gln i Lys,
X18 predstavlja Ala,
X20 predstavlja aminokiselinski ostatak koji se bira od Gln i Lys,
X21 predstavlja aminokiselinski ostatak koji se bira od Asp i Leu,
X28 predstavlja Ala,
X29 predstavlja aminokiselinski ostatak koji se bira od Gly i D-Ala,
X35 predstavlja Ala,
X39 je Ser,
X40 je odsutan.
10. Spoj prema bilo kojem od zahtjeva 1 - 5, naznačen time da
X2 predstavlja D-Ser,
X3 predstavlja Gln,
X14 predstavlja Lys, pri čemu je -NH2 skupina bočnog lanca funkcionalizirana, naročito sa (S)-4-karboksi-4-heksadekanoilaminobutiril- ili heksadekanoil-;
X15 predstavlja aminokiselinski ostatak koji se bira od Glu i Asp,
X16 predstavlja aminokiselinski ostatak koji se bira od Ser i Glu,
X17 predstavlja aminokiselinski ostatak koji se bira od Arg, Glu i Lys
X18 predstavlja aminokiselinski ostatak koji se bira od Arg i Ala,
X20 predstavlja aminokiselinski ostatak koji se bira od Gln, Lys i Aib,
X21 predstavlja aminokiselinski ostatak koji se bira od Asp i Leu,
X28 predstavlja aminokiselinski ostatak koji se bira od Ala i Asn,
X29 predstavlja Gly,
X35 predstavlja Ala,
X39 je Ser,
X40 je odsutan.
11. Spoj prema bilo kojem od zahtjeva 1 - 5, naznačen time da
X2 predstavlja aminokiselinski ostatak koji se bira od Aib i D-Ser;
X3 predstavlja aminokiselinski ostatak koji se bira od Gln i His;
X14 predstavlja Lys, pri čemu je -NH2 skupina bočnog lanca funkcionalizirana s jednom od skupina odabranih od (S)-4-karboksi-4-heksadekanoilamino-butiril-, (S)-4-karboksi-4-oktadekanoilaminobutiril-, (S)-4-karboksi-4-((S)-4-karboksi-4-heksadekanoilaminobutirilamino)-butiril-, (S)-4-karboksi-4-((S)-4-karboksi-4-oktadekanoilamino-butirilamino)-butiril-, 3-(3-Oktadekanoilaminopropionila-mino)-propionil-, 3-(3-Heksadekanoilamino-propionilamino)-propionil-, (S)-4-karboksi-4-henicosanoilamino-butiril-, 4-Heksadekanoilamino-butiril- i 4-oktadekanoilamino-butiril-,
X15 predstavlja aminokiselinski ostatak koji se bira od Asp i Glu;
X16 predstavlja aminokiselinski ostatak koji se bira od Ser i Glu;
X17 predstavlja aminokiselinski ostatak koji se bira od Arg, Gln, Lys i Leu;
X18 predstavlja aminokiselinski ostatak koji se bira od Arg i Ala;
X20 predstavlja aminokiselinski ostatak koji se bira od Gln, Aib i Lys;
X21 predstavlja aminokiselinski ostatak koji se bira od Asp i Glu;
X28 predstavlja aminokiselinski ostatak koji se bira od Asn, Ser, Aib, Ala i Arg;
X29 predstavlja aminokiselinski ostatak koji se bira od Gly, Thr, Ala i D-Ala;
X35 predstavlja Ala;
X39 predstavlja Ser i
X40 je odsutan.
12. Spoj prema bilo kojem od zahtjeva 1 - 7, naznačen time da
funkcionalizirani Lys na položaju 14 je funkcionaliziran na njegovoj ε-amino skupini s -C(O)-R5, i -C(O)-R5 je (S)-4-karboksi-4-heksadekanoilamino-butiril, (S)-4-karboksi-4-oktadekanoilamino-butiril, heksadekanoil ili oktadekanoil.
13. Spoj prema zahtjevu 12, naznačen time da
X2 predstavlja aminokiselinski ostatak koji se bira od Aib i D-Ser;
X3 predstavlja Gln;
X14 predstavlja Lys, pri čemu je -NH2 skupina bočnog lanca funkcionalizirana s jednom od skupina odabranih od (S)-4-karboksi-4-heksadekanoilamino-butiril, (S)-4-karboksi-4-oktadekanoilamino-butiril, heksadekanoil i oktadekanoil;
X15 predstavlja Glu;
X16 predstavlja Ser;
X17 predstavlja aminokiselinski ostatak koji se bira od Arg, Gln i Lys;
X18 predstavlja Ala;
X20 predstavlja Gln;
X21 predstavlja Asp;
X28 predstavlja Ala;
X29 predstavlja Gly;
X35 predstavlja Ala;
X39 predstavlja Ser i
X40 je odsutan.
14. Spoj prema bilo kojem od zahtjeva 1 - 5, naznačen time da
X2 predstavlja Aib,
X3 predstavlja Gln,
X14 predstavlja Lys, pri čemu je -NH2 skupina bočnog lanca funkcionalizirana, naročito sa (S)-4-karboksi-4-henicosanoilaminobutiril- i (S)-4-karboksi-4-oktadekanoilamino-butiril-;
X15 predstavlja Asp,
X16 predstavlja aminokiselinski ostatak koji se bira od Lys i Glu,
X17 predstavlja aminokiselinski ostatak koji se bira od Arg i Glu,
X18 predstavlja aminokiselinski ostatak koji se bira od Ala i Arg,
X20 predstavlja aminokiselinski ostatak koji se bira od Gln i Lys,
X21 predstavlja aminokiselinski ostatak koji se bira od Asp i Leu,
X28 predstavlja Ala,
X29 predstavlja aminokiselinski ostatak koji se bira od Gly i D-Ala,
X35 predstavlja Ala,
X39 je Ser,
X40 je odsutan.
15. Spoj prema bilo kojem od zahtjeva 1-14, naznačen time da se bira od spojeva iz SEQ ID NO.: 4-10, 16-22, 24-81, 84-129, 133-164, 166-181 ili njegova sol ili solvat.
16. Spoj prema bilo kojem od zahtjeva 1-14, naznačen time da se bira od spojeva iz SEQ ID NO.: 4-10, 16-22, 24-81, 84-129, 133-164, 166-181, 196-205, 207-223, 226-229 ili njegova sol ili solvat.
17. Spoj prema zahtjevu 1, naznačen time da je spoj prikazan sa SEQ ID NO.: 24, ili njegova sol ili solvat.
18. Spoj prema zahtjevu 1, naznačen time da je spoj prikazan sa SEQ ID NO.: 35, ili njegova sol ili solvat.
19. Spoj prema zahtjevu 1, naznačen time da je spoj prikazan sa SEQ ID NO.: 36, ili njegova sol ili solvat.
20. Spoj prema zahtjevu 1, naznačen time da je spoj prikazan sa SEQ ID NO.: 44, ili njegova sol ili solvat.
21. Spoj prema zahtjevu 1, naznačen time da je spoj prikazan sa SEQ ID NO.: 97, ili njegova sol ili solvat.
22. Spoj prema bilo kojem od zahtjeva 1-21, naznačen time da ima visoku topljivost kod kiselih vrijednosti pH, npr. kod pH 4.5 na 25°C, i/ili kod fizioloških vrijednosti pH, npr. kod pH 7.4 na 25°C, pri čemu je topljivost kod navedene pH vrijednosti i/ili navedenih pH vrijednosti naročito najmanje 0.5 mg/ml, ili najmanje 1.0 mg/ml.
23. Spoj prema bilo kojem od zahtjeva 1-22 naznačen time da je za upotrebu u medicini, naročito u ljudskoj medicini.
24. Spoj za uporabu prema zahtjevu 23 naznačen time da je prisutan kao aktivno sredstvo u farmaceutskom pripravku zajedno s barem jednim farmaceutski prihvatljivim nosačem.
25. Spoj za uporabu prema zahtjevu 23 ili 24 zajedno s barem jednim dodatnim terapeutski aktivnim sredstvom, naznačen time da je dodatno terapeutski aktivno sredstvo odabrano iz niza koji čine inzulin i derivati inzulina, GLP-1, analozi GLP-1 i agonisti GLP-1 receptora, polimerno vezani GLP-1 i analozi GLP-1, dvostruki agonisti GLP1/GIP, PYY3-36 ili njihovi analozi, polipeptid gušterače ili njegovi analozi, agonisti receptora Glukagona, agonisti ili antagonisti GIP receptora, antagonisti ili inverzni agonisti grelina, ksenin i njegovi analozi, inhibitori DDP-IV, inhibitori SGLT2, dvostruki inhibitori SGLT2 / SGLT1, bigvanidi tiazolidindioni, dvostruki agonisti PPAR, sulfoniluree, meglitinidi, inhibitori alfa-glukozidaze, amilin i analozi amilina, agonisti GPR119, agonisti GPR40, agonisti GPR120, agonisti GPR142, sistemski ili nisko apsorbirajući TGR5 agonisti, Cikloset, inhibitori 11-beta-HSD, aktivatori glukokinaze, inhibitori DGAT, inhibitori protein tirozinfosfataze 1, inhibitori glukoza-6-fosfataze, inhibitori fruktoza-1,6-bisfosfataze, inhibitori glikogen fosforilaze, inhibitori fosfoenol piruvat karboksikinaze, inhibitori glikogen sintaze kinaze, inhibitori piruvat dehidrogenaze kinaze, alfa2-antagonisti, antagonisti CCR-2, modulatori glukoznog transportera-4, agonisti somatostatin receptora 3, inhibitori HMG-CoA-reduktaze, fibrati, nikotinska kiselina i njezini derivati, agonisti receptora 1 nikotinske kiseline, PPAR-alfa, gama ili alfa/gama) agonisti ili modulatori, PPAR-delta agonisti, ACAT inhibitori, inhibitori apsorpcije kolesterola, tvari za vezanje žučnih kiselina, IBAT inhibitori, MTP inhibitori, modulatori PCSK9, regulatori LDL receptora prema gore pomoću za jetru selektivnih agonista ß receptora hormona štitnjače, spojevi koji podižu HDL, modulatori metabolizma lipida, inhibitori PLA2, pojačivači ApoA-I, agonisti receptora hormona štitnjače, inhibitori sinteze kolesterola, omega-3 masne kiseline i njihovi derivati, aktivne tvari za liječenje pretilosti, kao što su Sibutramin, Tesofenzin, Orlistat, antagonisti CB-1 receptora, MCH-1 antagonisti, agonisti i djelomični agonisti MC4 receptora, NPY5 ili NPY2 antagonisti, NPY4 agonisti, beta-3-agonisti, leptin ili mimetici leptina, agonisti receptora 5HT2c, ili kombinacije bupropion/naltrekson (CONTRAVE), bupropion/zonisamid (EMPATIC), bupropion/fentermin ili pramlintid/metreleptin, QNEXA (Fentermin+ topiramat), inhibitori lipaze, inhibitori angiogeneze, antagonisti H3, inhibitori AgRP, trostruki inhibitori unosa monoamina (norepinefrin i acetilkolin), MetAP2 inhibitori, nazalna formulacija diltiazema - blokatora kalcijevih kanala, antisense protiv proizvodnje receptora faktora rasta fibroblasta 4, prohibitin ciljajući peptid-1, lijekovi za utjecanje na visoki krvni tlak, kronično zatajenje srca ili aterosklerozu, kao što su antagonisti angiotenzin II receptora, inhibitori ACE, inhibitori ECE, diuretici, beta-blokatori, antagonisti kalcija, centralno djelujući hipertenzijski lijekovi, antagonisti alfa-2-adrenergičnog receptora, inhibitori neutralne endopeptidaze, inhibitori agregacije trombocita.
26. Spoj za uporabu prema zahtjevu 23 ili 24 zajedno s barem jednim dodatnim terapeutski aktivnim sredstvom, naznačen time da dodatno terapeutski aktivno sredstvo naročito je spoj GLP-1 i/ili inzulinski spoj i/ili gastrointestinalni peptid.
27. Spoj za uporabu prema zahtjevu 23 ili 24 zajedno s barem jednim dodatnim terapeutski aktivnim sredstvom, naznačen time da dodatno terapeutski aktivno sredstvo naročito je inzulin ili derivat inzulina.
28. Spoj za uporabu prema zahtjevu 23 ili 24, naznačen time da je farmaceutski pripravak za parenteralnu primjenu, poželjno u obliku injektibilne jedinične doze, naročito u obliku olovke.
29. Spoj za uporabu prema bilo kojem od zahtjeva 23 - 28 naznačen time da je za liječenje ili prevenciju hiperglikemije, dijabetesa tipa 2, poremećene tolerancije glukoze, dijabetesa tipa 1, pretilosti, metaboličkog sindroma i neurodegenerativnih poremećaja, naročito za odgađanje ili sprječavanje napredovanja bolesti kod dijabetesa tipa 2, liječenje metaboličkog sindroma, liječenje pretilosti ili sprječavanje prekomjerne težine, za smanjenje unosa hrane, povećanje potrošnje energije, smanjenje tjelesne težine, odgađanje napredovanja poremećene tolerancije glukoze (IGT) na dijabetes tipa 2; odgađanje napredovanja iz dijabetesa tipa 2 u dijabetes koji zahtijeva inzulin; za reguliranje apetita; izazivanje sitosti; sprečavanje ponovnog dobivanja težine nakon uspješnog gubitka težine; liječenje bolesti ili stanja povezanih s prekomjernom težinom ili pretilosti; liječenje bulimije; liječenje prejedanja; liječenje ateroskleroze, hipertenzije, IGT, dislipidemije, koronarne bolesti srca, steatoze jetre, liječenje otrovanja beta-blokatorom.
30. Spoj za uporabu prema bilo kojem od zahtjeva 23 - 29 naznačen time da je za liječenje ili prevenciju hiperglikemije, dijabetesa tipa 2, pretilosti i metaboličkog sindroma ili za smanjenje tjelesne težine.
31. Spoj za uporabu prema bilo kojem od zahtjeva 23 - 29 naznačen time da je za istodobno liječenje pretilosti i dijabetesa.
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