HRP20110061T1 - Izum koji se odnosi na glp-1 i eksendin - Google Patents
Izum koji se odnosi na glp-1 i eksendin Download PDFInfo
- Publication number
- HRP20110061T1 HRP20110061T1 HR20110061T HRP20110061T HRP20110061T1 HR P20110061 T1 HRP20110061 T1 HR P20110061T1 HR 20110061 T HR20110061 T HR 20110061T HR P20110061 T HRP20110061 T HR P20110061T HR P20110061 T1 HRP20110061 T1 HR P20110061T1
- Authority
- HR
- Croatia
- Prior art keywords
- glp
- derivatives
- peptide
- accordance
- glu
- Prior art date
Links
- 101100337060 Caenorhabditis elegans glp-1 gene Proteins 0.000 title 1
- DTHNMHAUYICORS-KTKZVXAJSA-N Glucagon-like peptide 1 Chemical group C([C@@H](C(=O)N[C@@H]([C@@H](C)CC)C(=O)N[C@@H](C)C(=O)N[C@@H](CC=1C2=CC=CC=C2NC=1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](C(C)C)C(=O)N[C@@H](CCCCN)C(=O)NCC(=O)N[C@@H](CCCNC(N)=N)C(N)=O)NC(=O)[C@H](CCC(O)=O)NC(=O)[C@H](CCCCN)NC(=O)[C@H](C)NC(=O)[C@H](C)NC(=O)[C@H](CCC(N)=O)NC(=O)CNC(=O)[C@H](CCC(O)=O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CC=1C=CC(O)=CC=1)NC(=O)[C@H](CO)NC(=O)[C@H](CO)NC(=O)[C@@H](NC(=O)[C@H](CC(O)=O)NC(=O)[C@H](CO)NC(=O)[C@@H](NC(=O)[C@H](CC=1C=CC=CC=1)NC(=O)[C@@H](NC(=O)CNC(=O)[C@H](CCC(O)=O)NC(=O)[C@H](C)NC(=O)[C@@H](N)CC=1N=CNC=1)[C@@H](C)O)[C@@H](C)O)C(C)C)C1=CC=CC=C1 DTHNMHAUYICORS-KTKZVXAJSA-N 0.000 claims abstract 17
- 108090000765 processed proteins & peptides Proteins 0.000 claims abstract 17
- 102000007446 Glucagon-Like Peptide-1 Receptor Human genes 0.000 claims abstract 8
- 108010086246 Glucagon-Like Peptide-1 Receptor Proteins 0.000 claims abstract 8
- 150000001412 amines Chemical class 0.000 claims abstract 4
- 239000000824 cytostatic agent Substances 0.000 claims abstract 4
- 230000001085 cytostatic effect Effects 0.000 claims abstract 4
- 102100025101 GATA-type zinc finger protein 1 Human genes 0.000 claims 16
- 101710198884 GATA-type zinc finger protein 1 Proteins 0.000 claims 16
- 239000002872 contrast media Substances 0.000 claims 4
- 201000010099 disease Diseases 0.000 claims 4
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims 4
- 239000007850 fluorescent dye Substances 0.000 claims 4
- 230000003211 malignant effect Effects 0.000 claims 4
- 238000002560 therapeutic procedure Methods 0.000 claims 4
- QPCDCPDFJACHGM-UHFFFAOYSA-N N,N-bis{2-[bis(carboxymethyl)amino]ethyl}glycine Chemical group OC(=O)CN(CC(O)=O)CCN(CC(=O)O)CCN(CC(O)=O)CC(O)=O QPCDCPDFJACHGM-UHFFFAOYSA-N 0.000 claims 3
- 239000002246 antineoplastic agent Substances 0.000 claims 3
- 239000003795 chemical substances by application Substances 0.000 claims 3
- 229940127089 cytotoxic agent Drugs 0.000 claims 3
- 238000002372 labelling Methods 0.000 claims 3
- RXACEEPNTRHYBQ-UHFFFAOYSA-N 2-[[2-[[2-[(2-sulfanylacetyl)amino]acetyl]amino]acetyl]amino]acetic acid Chemical compound OC(=O)CNC(=O)CNC(=O)CNC(=O)CS RXACEEPNTRHYBQ-UHFFFAOYSA-N 0.000 claims 2
- XEEYBQQBJWHFJM-UHFFFAOYSA-N Iron Chemical compound [Fe] XEEYBQQBJWHFJM-UHFFFAOYSA-N 0.000 claims 2
- PXHVJJICTQNCMI-UHFFFAOYSA-N Nickel Chemical compound [Ni] PXHVJJICTQNCMI-UHFFFAOYSA-N 0.000 claims 2
- WDLRUFUQRNWCPK-UHFFFAOYSA-N Tetraxetan Chemical compound OC(=O)CN1CCN(CC(O)=O)CCN(CC(O)=O)CCN(CC(O)=O)CC1 WDLRUFUQRNWCPK-UHFFFAOYSA-N 0.000 claims 2
- 150000001413 amino acids Chemical group 0.000 claims 2
- 239000002738 chelating agent Substances 0.000 claims 2
- 230000001268 conjugating effect Effects 0.000 claims 2
- ZYGHJZDHTFUPRJ-UHFFFAOYSA-N coumarin Chemical compound C1=CC=C2OC(=O)C=CC2=C1 ZYGHJZDHTFUPRJ-UHFFFAOYSA-N 0.000 claims 2
- 230000001472 cytotoxic effect Effects 0.000 claims 2
- 238000003745 diagnosis Methods 0.000 claims 2
- NOESYZHRGYRDHS-UHFFFAOYSA-N insulin Chemical compound N1C(=O)C(NC(=O)C(CCC(N)=O)NC(=O)C(CCC(O)=O)NC(=O)C(C(C)C)NC(=O)C(NC(=O)CN)C(C)CC)CSSCC(C(NC(CO)C(=O)NC(CC(C)C)C(=O)NC(CC=2C=CC(O)=CC=2)C(=O)NC(CCC(N)=O)C(=O)NC(CC(C)C)C(=O)NC(CCC(O)=O)C(=O)NC(CC(N)=O)C(=O)NC(CC=2C=CC(O)=CC=2)C(=O)NC(CSSCC(NC(=O)C(C(C)C)NC(=O)C(CC(C)C)NC(=O)C(CC=2C=CC(O)=CC=2)NC(=O)C(CC(C)C)NC(=O)C(C)NC(=O)C(CCC(O)=O)NC(=O)C(C(C)C)NC(=O)C(CC(C)C)NC(=O)C(CC=2NC=NC=2)NC(=O)C(CO)NC(=O)CNC2=O)C(=O)NCC(=O)NC(CCC(O)=O)C(=O)NC(CCCNC(N)=N)C(=O)NCC(=O)NC(CC=3C=CC=CC=3)C(=O)NC(CC=3C=CC=CC=3)C(=O)NC(CC=3C=CC(O)=CC=3)C(=O)NC(C(C)O)C(=O)N3C(CCC3)C(=O)NC(CCCCN)C(=O)NC(C)C(O)=O)C(=O)NC(CC(N)=O)C(O)=O)=O)NC(=O)C(C(C)CC)NC(=O)C(CO)NC(=O)C(C(C)O)NC(=O)C1CSSCC2NC(=O)C(CC(C)C)NC(=O)C(NC(=O)C(CCC(N)=O)NC(=O)C(CC(N)=O)NC(=O)C(NC(=O)C(N)CC=1C=CC=CC=1)C(C)C)CC1=CN=CN1 NOESYZHRGYRDHS-UHFFFAOYSA-N 0.000 claims 2
- 230000001404 mediated effect Effects 0.000 claims 2
- 201000011519 neuroendocrine tumor Diseases 0.000 claims 2
- -1 ornithine Chemical class 0.000 claims 2
- BBEAQIROQSPTKN-UHFFFAOYSA-N pyrene Chemical compound C1=CC=C2C=CC3=CC=CC4=CC=C1C2=C43 BBEAQIROQSPTKN-UHFFFAOYSA-N 0.000 claims 2
- 102000005962 receptors Human genes 0.000 claims 2
- 108020003175 receptors Proteins 0.000 claims 2
- QGKMIGUHVLGJBR-UHFFFAOYSA-M (4z)-1-(3-methylbutyl)-4-[[1-(3-methylbutyl)quinolin-1-ium-4-yl]methylidene]quinoline;iodide Chemical compound [I-].C12=CC=CC=C2N(CCC(C)C)C=CC1=CC1=CC=[N+](CCC(C)C)C2=CC=CC=C12 QGKMIGUHVLGJBR-UHFFFAOYSA-M 0.000 claims 1
- VGIRNWJSIRVFRT-UHFFFAOYSA-N 2',7'-difluorofluorescein Chemical compound OC(=O)C1=CC=CC=C1C1=C2C=C(F)C(=O)C=C2OC2=CC(O)=C(F)C=C21 VGIRNWJSIRVFRT-UHFFFAOYSA-N 0.000 claims 1
- UWMHHZFHBCYGCV-UHFFFAOYSA-N 2,3,2-tetramine Chemical compound NCCNCCCNCCN UWMHHZFHBCYGCV-UHFFFAOYSA-N 0.000 claims 1
- GOLORTLGFDVFDW-UHFFFAOYSA-N 3-(1h-benzimidazol-2-yl)-7-(diethylamino)chromen-2-one Chemical compound C1=CC=C2NC(C3=CC4=CC=C(C=C4OC3=O)N(CC)CC)=NC2=C1 GOLORTLGFDVFDW-UHFFFAOYSA-N 0.000 claims 1
- HBBSDZXXUIHKJE-UHFFFAOYSA-N 6-hydrazinylpyridine-3-carboxylic acid Chemical compound NNC1=CC=C(C(O)=O)C=N1 HBBSDZXXUIHKJE-UHFFFAOYSA-N 0.000 claims 1
- 239000012099 Alexa Fluor family Substances 0.000 claims 1
- VYZAMTAEIAYCRO-UHFFFAOYSA-N Chromium Chemical compound [Cr] VYZAMTAEIAYCRO-UHFFFAOYSA-N 0.000 claims 1
- RYGMFSIKBFXOCR-UHFFFAOYSA-N Copper Chemical compound [Cu] RYGMFSIKBFXOCR-UHFFFAOYSA-N 0.000 claims 1
- 229910052692 Dysprosium Inorganic materials 0.000 claims 1
- 229910052693 Europium Inorganic materials 0.000 claims 1
- 229910052688 Gadolinium Inorganic materials 0.000 claims 1
- 229910052689 Holmium Inorganic materials 0.000 claims 1
- 102000004877 Insulin Human genes 0.000 claims 1
- 108090001061 Insulin Proteins 0.000 claims 1
- 102000014150 Interferons Human genes 0.000 claims 1
- 108010050904 Interferons Proteins 0.000 claims 1
- 102000015696 Interleukins Human genes 0.000 claims 1
- 108010063738 Interleukins Proteins 0.000 claims 1
- AHLPHDHHMVZTML-BYPYZUCNSA-N L-Ornithine Chemical compound NCCC[C@H](N)C(O)=O AHLPHDHHMVZTML-BYPYZUCNSA-N 0.000 claims 1
- 239000004472 Lysine Substances 0.000 claims 1
- KDXKERNSBIXSRK-UHFFFAOYSA-N Lysine Natural products NCCCCC(N)C(O)=O KDXKERNSBIXSRK-UHFFFAOYSA-N 0.000 claims 1
- AHLPHDHHMVZTML-UHFFFAOYSA-N Orn-delta-NH2 Natural products NCCCC(N)C(O)=O AHLPHDHHMVZTML-UHFFFAOYSA-N 0.000 claims 1
- UTJLXEIPEHZYQJ-UHFFFAOYSA-N Ornithine Natural products OC(=O)C(C)CCCN UTJLXEIPEHZYQJ-UHFFFAOYSA-N 0.000 claims 1
- 239000010103 Podophyllin Substances 0.000 claims 1
- 229910052777 Praseodymium Inorganic materials 0.000 claims 1
- 229940123237 Taxane Drugs 0.000 claims 1
- 229940122803 Vinca alkaloid Drugs 0.000 claims 1
- 229940045714 alkyl sulfonate alkylating agent Drugs 0.000 claims 1
- 150000008052 alkyl sulfonates Chemical class 0.000 claims 1
- 229940045799 anthracyclines and related substance Drugs 0.000 claims 1
- 239000003242 anti bacterial agent Substances 0.000 claims 1
- 229940088710 antibiotic agent Drugs 0.000 claims 1
- 229940045687 antimetabolites folic acid analogs Drugs 0.000 claims 1
- 229940045985 antineoplastic platinum compound Drugs 0.000 claims 1
- 210000000621 bronchi Anatomy 0.000 claims 1
- VSJKWCGYPAHWDS-FQEVSTJZSA-N camptothecin Chemical class C1=CC=C2C=C(CN3C4=CC5=C(C3=O)COC(=O)[C@]5(O)CC)C4=NC2=C1 VSJKWCGYPAHWDS-FQEVSTJZSA-N 0.000 claims 1
- CZPLANDPABRVHX-UHFFFAOYSA-N cascade blue Chemical compound C=1C2=CC=CC=C2C(NCC)=CC=1C(C=1C=CC(=CC=1)N(CC)CC)=C1C=CC(=[N+](CC)CC)C=C1 CZPLANDPABRVHX-UHFFFAOYSA-N 0.000 claims 1
- 238000002512 chemotherapy Methods 0.000 claims 1
- 229910052804 chromium Inorganic materials 0.000 claims 1
- 239000011651 chromium Substances 0.000 claims 1
- 150000001875 compounds Chemical class 0.000 claims 1
- 230000021615 conjugation Effects 0.000 claims 1
- 229940039231 contrast media Drugs 0.000 claims 1
- 229910052802 copper Inorganic materials 0.000 claims 1
- 239000010949 copper Substances 0.000 claims 1
- 229960000956 coumarin Drugs 0.000 claims 1
- 235000001671 coumarin Nutrition 0.000 claims 1
- 231100000433 cytotoxic Toxicity 0.000 claims 1
- KBQHZAAAGSGFKK-UHFFFAOYSA-N dysprosium atom Chemical compound [Dy] KBQHZAAAGSGFKK-UHFFFAOYSA-N 0.000 claims 1
- OGPBJKLSAFTDLK-UHFFFAOYSA-N europium atom Chemical compound [Eu] OGPBJKLSAFTDLK-UHFFFAOYSA-N 0.000 claims 1
- GVEPBJHOBDJJJI-UHFFFAOYSA-N fluoranthrene Natural products C1=CC(C2=CC=CC=C22)=C3C2=CC=CC3=C1 GVEPBJHOBDJJJI-UHFFFAOYSA-N 0.000 claims 1
- GNBHRKFJIUUOQI-UHFFFAOYSA-N fluorescein Chemical compound O1C(=O)C2=CC=CC=C2C21C1=CC=C(O)C=C1OC1=CC(O)=CC=C21 GNBHRKFJIUUOQI-UHFFFAOYSA-N 0.000 claims 1
- 150000002224 folic acids Chemical class 0.000 claims 1
- UIWYJDYFSGRHKR-UHFFFAOYSA-N gadolinium atom Chemical group [Gd] UIWYJDYFSGRHKR-UHFFFAOYSA-N 0.000 claims 1
- UKVFVQPAANCXIL-FJVFSOETSA-N glp-1 (1-37) amide Chemical compound C([C@@H](C(=O)N[C@@H]([C@@H](C)CC)C(=O)N[C@@H](C)C(=O)N[C@@H](CC=1C2=CC=CC=C2NC=1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](C(C)C)C(=O)N[C@@H](CCCCN)C(=O)NCC(=O)N[C@@H](CCCNC(N)=N)C(=O)NCC(O)=O)NC(=O)[C@H](CCC(O)=O)NC(=O)[C@H](CCCCN)NC(=O)[C@H](C)NC(=O)[C@H](C)NC(=O)[C@H](CCC(N)=O)NC(=O)CNC(=O)[C@H](CCC(O)=O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CC=1C=CC(O)=CC=1)NC(=O)[C@H](CO)NC(=O)[C@H](CO)NC(=O)[C@@H](NC(=O)[C@H](CC(O)=O)NC(=O)[C@H](CO)NC(=O)[C@@H](NC(=O)[C@H](CC=1C=CC=CC=1)NC(=O)[C@@H](NC(=O)CNC(=O)[C@H](CCC(O)=O)NC(=O)[C@H](C)NC(=O)[C@H](CC=1NC=NC=1)NC(=O)[C@H](CCCNC(N)=N)NC(=O)[C@H](CCC(O)=O)NC(=O)[C@H](CC=1C=CC=CC=1)NC(=O)[C@H](CCC(O)=O)NC(=O)[C@H](CC(O)=O)NC(=O)[C@@H](N)CC=1NC=NC=1)[C@@H](C)O)[C@@H](C)O)C(C)C)C1=CC=CC=C1 UKVFVQPAANCXIL-FJVFSOETSA-N 0.000 claims 1
- 239000003102 growth factor Substances 0.000 claims 1
- KJZYNXUDTRRSPN-UHFFFAOYSA-N holmium atom Chemical compound [Ho] KJZYNXUDTRRSPN-UHFFFAOYSA-N 0.000 claims 1
- 229940088597 hormone Drugs 0.000 claims 1
- 239000005556 hormone Substances 0.000 claims 1
- 238000000338 in vitro Methods 0.000 claims 1
- 229940125396 insulin Drugs 0.000 claims 1
- 206010022498 insulinoma Diseases 0.000 claims 1
- 229940047124 interferons Drugs 0.000 claims 1
- 229940047122 interleukins Drugs 0.000 claims 1
- 229910052742 iron Inorganic materials 0.000 claims 1
- DLBFLQKQABVKGT-UHFFFAOYSA-L lucifer yellow dye Chemical compound [Li+].[Li+].[O-]S(=O)(=O)C1=CC(C(N(C(=O)NN)C2=O)=O)=C3C2=CC(S([O-])(=O)=O)=CC3=C1N DLBFLQKQABVKGT-UHFFFAOYSA-L 0.000 claims 1
- WPBNNNQJVZRUHP-UHFFFAOYSA-L manganese(2+);methyl n-[[2-(methoxycarbonylcarbamothioylamino)phenyl]carbamothioyl]carbamate;n-[2-(sulfidocarbothioylamino)ethyl]carbamodithioate Chemical compound [Mn+2].[S-]C(=S)NCCNC([S-])=S.COC(=O)NC(=S)NC1=CC=CC=C1NC(=S)NC(=O)OC WPBNNNQJVZRUHP-UHFFFAOYSA-L 0.000 claims 1
- HAWPXGHAZFHHAD-UHFFFAOYSA-N mechlorethamine Chemical class ClCCN(C)CCCl HAWPXGHAZFHHAD-UHFFFAOYSA-N 0.000 claims 1
- 229910052759 nickel Inorganic materials 0.000 claims 1
- 230000003287 optical effect Effects 0.000 claims 1
- 125000000962 organic group Chemical group 0.000 claims 1
- 229960003104 ornithine Drugs 0.000 claims 1
- 208000021255 pancreatic insulinoma Diseases 0.000 claims 1
- 229960003330 pentetic acid Drugs 0.000 claims 1
- 108060006184 phycobiliprotein Proteins 0.000 claims 1
- 150000003058 platinum compounds Chemical class 0.000 claims 1
- 229940068582 podophyllin Drugs 0.000 claims 1
- PUDIUYLPXJFUGB-UHFFFAOYSA-N praseodymium atom Chemical compound [Pr] PUDIUYLPXJFUGB-UHFFFAOYSA-N 0.000 claims 1
- 238000002360 preparation method Methods 0.000 claims 1
- 125000000561 purinyl group Chemical class N1=C(N=C2N=CNC2=C1)* 0.000 claims 1
- 150000003230 pyrimidines Chemical class 0.000 claims 1
- PYWVYCXTNDRMGF-UHFFFAOYSA-N rhodamine B Chemical compound [Cl-].C=12C=CC(=[N+](CC)CC)C=C2OC2=CC(N(CC)CC)=CC=C2C=1C1=CC=CC=C1C(O)=O PYWVYCXTNDRMGF-UHFFFAOYSA-N 0.000 claims 1
- 238000009738 saturating Methods 0.000 claims 1
- 238000002603 single-photon emission computed tomography Methods 0.000 claims 1
- 208000000649 small cell carcinoma Diseases 0.000 claims 1
- 239000000126 substance Substances 0.000 claims 1
- TXEYQDLBPFQVAA-UHFFFAOYSA-N tetrafluoromethane Chemical compound FC(F)(F)F TXEYQDLBPFQVAA-UHFFFAOYSA-N 0.000 claims 1
- MPLHNVLQVRSVEE-UHFFFAOYSA-N texas red Chemical compound [O-]S(=O)(=O)C1=CC(S(Cl)(=O)=O)=CC=C1C(C1=CC=2CCCN3CCCC(C=23)=C1O1)=C2C1=C(CCC1)C3=[N+]1CCCC3=C2 MPLHNVLQVRSVEE-UHFFFAOYSA-N 0.000 claims 1
- JUFFVKRROAPVBI-PVOYSMBESA-N chembl1210015 Chemical compound C([C@@H](C(=O)N[C@@H]([C@@H](C)CC)C(=O)N[C@@H](CCC(O)=O)C(=O)N[C@@H](CC=1C2=CC=CC=C2NC=1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CC(=O)N[C@H]1[C@@H]([C@@H](O)[C@H](O[C@H]2[C@@H]([C@@H](O)[C@@H](O)[C@@H](CO[C@]3(O[C@@H](C[C@H](O)[C@H](O)CO)[C@H](NC(C)=O)[C@@H](O)C3)C(O)=O)O2)O)[C@@H](CO)O1)NC(C)=O)C(=O)NCC(=O)NCC(=O)N1[C@@H](CCC1)C(=O)N[C@@H](CO)C(=O)N[C@@H](CO)C(=O)NCC(=O)N[C@@H](C)C(=O)N1[C@@H](CCC1)C(=O)N1[C@@H](CCC1)C(=O)N1[C@@H](CCC1)C(=O)N[C@@H](CO)C(N)=O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CCCNC(N)=N)NC(=O)[C@@H](NC(=O)[C@H](C)NC(=O)[C@H](CCC(O)=O)NC(=O)[C@H](CCC(O)=O)NC(=O)[C@H](CCC(O)=O)NC(=O)[C@H](CCSC)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CO)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CC(O)=O)NC(=O)[C@H](CO)NC(=O)[C@@H](NC(=O)[C@H](CC=1C=CC=CC=1)NC(=O)[C@@H](NC(=O)CNC(=O)[C@H](CCC(O)=O)NC(=O)CNC(=O)[C@@H](N)CC=1NC=NC=1)[C@@H](C)O)[C@@H](C)O)C(C)C)C1=CC=CC=C1 JUFFVKRROAPVBI-PVOYSMBESA-N 0.000 abstract 2
- LMHMJYMCGJNXRS-IOPUOMRJSA-N exendin-3 Chemical compound C([C@@H](C(=O)N[C@@H]([C@@H](C)CC)C(=O)N[C@@H](CCC(O)=O)C(=O)N[C@@H](CC=1C2=CC=CC=C2NC=1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CC(N)=O)C(=O)NCC(=O)NCC(=O)N1[C@@H](CCC1)C(=O)N[C@@H](CO)C(=O)N[C@@H](CO)C(=O)NCC(=O)N[C@@H](C)C(=O)N1[C@@H](CCC1)C(=O)N1[C@@H](CCC1)C(=O)N1[C@@H](CCC1)C(=O)N[C@@H](CO)C(N)=O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CCCNC(N)=N)NC(=O)[C@@H](NC(=O)[C@H](C)NC(=O)[C@H](CCC(O)=O)NC(=O)[C@H](CCC(O)=O)NC(=O)[C@H](CCC(O)=O)NC(=O)[C@H](CCSC)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CO)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CC(O)=O)NC(=O)[C@H](CO)NC(=O)[C@@H](NC(=O)[C@H](CC=1C=CC=CC=1)NC(=O)[C@@H](NC(=O)CNC(=O)[C@H](CC(O)=O)NC(=O)[C@H](CO)NC(=O)[C@@H](N)CC=1N=CNC=1)[C@H](C)O)[C@H](C)O)C(C)C)C1=CC=CC=C1 LMHMJYMCGJNXRS-IOPUOMRJSA-N 0.000 abstract 2
- 108010011459 Exenatide Proteins 0.000 abstract 1
- 108091006116 chimeric peptides Proteins 0.000 abstract 1
- 230000000694 effects Effects 0.000 abstract 1
- 229960001519 exenatide Drugs 0.000 abstract 1
- 108010015174 exendin 3 Proteins 0.000 abstract 1
- 239000003446 ligand Substances 0.000 abstract 1
- 230000010534 mechanism of action Effects 0.000 abstract 1
- GCYXWQUSHADNBF-AAEALURTSA-N preproglucagon 78-108 Chemical class C([C@@H](C(=O)N[C@@H]([C@@H](C)CC)C(=O)N[C@@H](C)C(=O)N[C@@H](CC=1C2=CC=CC=C2NC=1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](C(C)C)C(=O)N[C@@H](CCCCN)C(=O)NCC(=O)N[C@@H](CCCNC(N)=N)C(=O)NCC(O)=O)NC(=O)[C@H](CCC(O)=O)NC(=O)[C@H](CCCCN)NC(=O)[C@H](C)NC(=O)[C@H](C)NC(=O)[C@H](CCC(N)=O)NC(=O)CNC(=O)[C@H](CCC(O)=O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CC=1C=CC(O)=CC=1)NC(=O)[C@H](CO)NC(=O)[C@H](CO)NC(=O)[C@@H](NC(=O)[C@H](CC(O)=O)NC(=O)[C@H](CO)NC(=O)[C@@H](NC(=O)[C@H](CC=1C=CC=CC=1)NC(=O)[C@@H](NC(=O)CNC(=O)[C@H](CCC(O)=O)NC(=O)[C@H](C)NC(=O)[C@@H](N)CC=1N=CNC=1)[C@@H](C)O)[C@@H](C)O)C(C)C)C1=CC=CC=C1 GCYXWQUSHADNBF-AAEALURTSA-N 0.000 abstract 1
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07K—PEPTIDES
- C07K14/00—Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof
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Abstract
Derivati peptida GLP-1 koji, u cijelosti ili djelomično, sadrže aminokiselinske sljedove (H)-1His-2Asp-3Glu-4Phe-5Glu-6Arg-7His-8Ala-9Glu-10Gly-11Thr-12Phe-13Thr-14Ser-15Asp-16Val-17Ser-18Ser-19Tyr-20Leu-21Glu-22Gly-23Gln-24Ala-25Ala-26Lys-27Glu-28Phe-29Ile-30Ala-31Trp-32Leu-33Val-34Lys-35Gly-36Arg-37Gly-(OH) peptida GLP-1 (1-37), naznačeni time što- su modificirani aminom na C-kraju i vežu se na GLP-1 receptor N-krajem, te- da se sastoje od GLP-1 (x-y)A, gdje x je broj 7, y je broj 36, a A je vezna skupina smještena na C-kraju, radi vezanja signalnih molekula, - te što vezna skupina A je lizin. Patent sadrži još 18 patentnih zahtjeva.
Claims (19)
1. Derivati peptida GLP-1 koji, u cijelosti ili djelomično, sadrže aminokiselinske sljedove
(H)-1His-2Asp-3Glu-4Phe-5Glu-6Arg-7His-8Ala-9Glu-10Gly-11Thr-12Phe-13Thr-14Ser-15Asp-16Val-17Ser-18Ser-19Tyr-20Leu-21Glu-22Gly-23Gln-24Ala-25Ala-26Lys-27Glu-28Phe-29Ile-30Ala-31Trp-32Leu-33Val-34Lys-35Gly-36Arg-37Gly-(OH)
peptida GLP-1 (1-37),
naznačeni time što
■ su modificirani aminom na C-kraju i vežu se na GLP-1 receptor N-krajem, te
■ da se sastoje od GLP-1 (x-y)A, gdje x je broj 7, y je broj 36, a A je vezna skupina smještena na C-kraju, radi vezanja signalnih molekula,
■ te što vezna skupina A je lizin.
2. Derivati peptida GLP-1 u skladu s patentnim zahtjevom 1, naznačeni time što vezna skupina A je amino kiselina sa slobodnim aminom poput ornitina, ili organska skupina sa slobodnim aminom.
3. Derivati peptida GLP-1 u skladu s bilo kojim od patentnih zahtjeva 1 do 2, naznačeni time što se na veznu skupinu A konjugira kelirajuće sredstvo za obilježavanje radionuklidima, ili kontrastni medij za MRT, fluorescentno bojilo, ili kemoterapeutik.
4. Derivati peptida GLP-1 u skladu s prethodnim patentnim zahtjevima, naznačeni time što kelirajuće sredstvo je N,N-Bis(2[bis(karboksimetil)amino]etil)glicin), DOTA (1,4,7,10-tetraazaciklododekan-1,4,7,10-tetraoctena kiselina, HYNIC (6-hidrazinopiridin-3-karboksilna kiselina), MAG3 (merkaptoacetilglicilglicilglicin), N4 (1,4,8,11-tetraazaundekan) i njihovi poznati derivati, po mogućnosti DTPA (dietilenetriaminpentaoctena kiselina).
5. Derivati peptida GLP-1 u skladu s prethodnim patentnim zahtjevima, naznačeni time što obilježavanje je konjugiranje radionuklida, kontrastni medij za MRT, fluorescentno bojilo i/ili kemoterapeutik.
6. Derivati peptida GLP-1 u skladu s prethodnim patentnim zahtjevima, naznačeni time što fluorescentna bojila se osobito bira iz skupine koju čine fluorescein, rodamin, kumarin, BODIPY, piren (kaskadno modrilo), lucifersko žutilo, fikoobiliprotein, cijanin, aleksa fluor, oregonsko zelenilo, teksaško crvenilo, kumarin i njihovi derivati.
7. Derivati peptida GLP-1 u skladu s prethodnim patentnim zahtjevima, naznačeni time što radionuklid se osobito bira iz skupine koju čine F-18, Cu-64, Ga-67, Ga-68, Y-86, Y-90, Tc-99m, In-111, I-123, I-124, I-131, Lu-177, Re-186, Re-188, Pt-195m, Ac-225, At-211, Bi-213, Sm-153 ili Er-169.
8. Derivati peptida GLP-1 u skladu s prethodnim patentnim zahtjevima, naznačeni time što kontrastni medij za MRT je gadolinij, mangan, željezo, europij, bakar, nikal, krom, praseodimij, disprozij ili holmij, ili njihovi spojevi, ili perfluorugljik, ili F-19, H-1, P-31, Na-19.
9. Derivati peptida GLP-1 u skladu s prethodnim patentnim zahtjevima, naznačeni time što kemoterapeutik se osobito bira iz skupine koju čine alkilsulfonati, etilimini, nitrozoharska sredstva, derivati dušičnog iperita, analozi folne kiseline, analozi purina, analozi pirimidina, derivati podofilina, taksani, Vinca alkaloidi, antraciklini, drugi citostatski antibiotici, spojevi platine, derivati kamptotecina, hormoni, čimbenici rasta, interferoni ili interleukini, ili tvari citostatskog ili citotoksičnog djelovanja.
10. Derivati peptida GLP-1 u skladu s prethodnim patentnim zahtjevima, naznačeni time što se obilježavanje provodi konjugiranjem radionuklida radi primjene in vitro zasićivanjem mjesta vezanja s natInCl3.
11. Upotreba derivata peptida GLP-1 u skladu s prethodnim patentnim zahtjevima, naznačena time što su navedeni derivati namijenjeni pripravi sredstva za dijagnosticiranje i terapiju dobroćudnih i zloćudnih bolesti čiji je čimbenik ekspresija GLP-1 receptora.
12. Derivati peptida GLP-1 u skladu s patentnim zahtjevima 1 do 10, naznačeni time što su namijenjeni upotrebi u određivanju gustoće stanica koje proizvode inzulin in a tkivo.
13. Derivati peptida GLP-1 u skladu s patentnim zahtjevima 1 do 10, naznačeni time što su namijenjeni upotrebi u određivanju ekspresije GLP-1 receptora ili njihove gustoće.
14. Sredstvo za dijagnosticiranje i terapiju dobroćudnih i zloćudnih bolesti čiji je čimbenik ekspresija GLP-1 receptora, naznačen time što sadrži obilježene derivate peptida GLP-1 u skladu s patentnim zahtjevom 1.
15. Sredstvo za dijagnosticiranje i terapiju dobroćudnih i zloćudnih bolesti čiji je čimbenik ekspresija GLP-1 receptora, naznačen time što sadrži neobilježene derivate peptida GLP-1 u skladu s patentnim zahtjevom 1.
16. Sredstvo u skladu s patentnim zahtjevom 14, naznačeno time što obilježavanje se sastoji u konjugiranju radionuklida, MRT kontrastnih medija, fluorescentnih bojila i/ili kemoterapeutika.
17. Sredstvo u skladu s patentnim zahtjevom 14 i patentnim zahtjevom 15, naznačeno time što je namijenjeno upotrebi u dijagnosticiranju i terapiji dobroćudnih i zloćudnih bolesti čiji je čimbenik ekspresija GLP-1 receptora.
18. Sredstvo u skladu s patentnim zahtjevom 14 i patentnim zahtjevom 15, naznačeno time što je namijenjeno upotrebi u dijagnosticiranju i terapiji neuroendokrinih tumora (NET), osobito inzulinoma i karcinoma malih stanica bronha.
19. Sredstvo u skladu s patentnim zahtjevom 14, naznačeno time što je namijenjeno upotrebi u scintigrafiji, PET, SPECT, MRT, optičkom dijagnosticiranju, kemoterapiji posredstvom receptora, citostatskoj ili citotoksičnoj terapiji posredstvom receptora, te u radiopeptidnoj terapiji.
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| DE102004043153A DE102004043153B4 (de) | 2004-09-03 | 2004-09-03 | Erfindung betreffend GLP-1 und Exendin |
| PCT/DE2005/001503 WO2006024275A2 (de) | 2004-09-03 | 2005-08-26 | Erfindung betreffend glp-1 und exendin |
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| HRP20110061T1 true HRP20110061T1 (hr) | 2011-02-28 |
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| HR20110061T HRP20110061T1 (hr) | 2004-09-03 | 2011-01-27 | Izum koji se odnosi na glp-1 i eksendin |
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| SI3456340T1 (sl) | 2007-01-08 | 2022-08-31 | The Trustees Of The University Of Pennsylvania | Antagonisti receptorja za GLP-1 za uporabo pri zdravljenju prirojenega hiperinsulinizma |
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| EP0915910B1 (de) * | 1996-06-05 | 2006-01-18 | Roche Diagnostics GmbH | Exendin-analoga, verfahren zu deren herstellung und diese enthaltende arzneimittel |
| AU3247799A (en) * | 1998-02-27 | 1999-09-15 | Novo Nordisk A/S | Glp-1 derivatives of glp-1 and exendin with protracted profile of action |
| AU2610599A (en) * | 1998-02-27 | 1999-09-15 | Novo Nordisk A/S | N-terminally truncated glp-1 derivatives |
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| DK1105409T3 (da) * | 1999-05-17 | 2006-07-03 | Conjuchem Inc | Beskyttelse af endogene terapeutiske peptider fra peptidaseaktivitet ved konjugering med blodkomponenter |
| CA2501421A1 (en) * | 1999-05-17 | 2000-11-23 | Conjuchem Inc. | Long lasting exendin-4 |
| US6528486B1 (en) * | 1999-07-12 | 2003-03-04 | Zealand Pharma A/S | Peptide agonists of GLP-1 activity |
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2004
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2005
- 2005-08-26 DE DE502005010449T patent/DE502005010449D1/de active Active
- 2005-08-26 PL PL08020703T patent/PL2070946T3/pl unknown
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- 2005-08-26 MX MX2007002455A patent/MX2007002455A/es active IP Right Grant
- 2005-08-26 WO PCT/DE2005/001503 patent/WO2006024275A2/de active Application Filing
- 2005-08-26 RU RU2007112115/10A patent/RU2420536C2/ru not_active IP Right Cessation
- 2005-08-26 EP EP08020703.8A patent/EP2070946B1/de not_active Not-in-force
- 2005-08-26 RU RU2010148447/10A patent/RU2489443C2/ru not_active IP Right Cessation
- 2005-08-26 CN CN2011101471272A patent/CN102304179A/zh active Pending
- 2005-08-26 PL PL10012756T patent/PL2301962T3/pl unknown
- 2005-08-26 EP EP05778889A patent/EP1784422B1/de active Active
- 2005-08-26 AU AU2005279537A patent/AU2005279537C1/en not_active Ceased
- 2005-08-26 EP EP10012756.2A patent/EP2301962B1/de not_active Not-in-force
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- 2005-08-26 KR KR1020077007577A patent/KR101237152B1/ko not_active IP Right Cessation
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