HRP20210073T1 - Selektivni agonisti receptora glukagona s kelatnim dijelom za svrhe prikazivanja - Google Patents

Selektivni agonisti receptora glukagona s kelatnim dijelom za svrhe prikazivanja Download PDF

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HRP20210073T1
HRP20210073T1 HRP20210073TT HRP20210073T HRP20210073T1 HR P20210073 T1 HRP20210073 T1 HR P20210073T1 HR P20210073T T HRP20210073T T HR P20210073TT HR P20210073 T HRP20210073 T HR P20210073T HR P20210073 T1 HRP20210073 T1 HR P20210073T1
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amino acid
do3a
cys
acid selected
lys
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HRP20210073TT
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Torsten Haack
Oliver Plettenburg
Andreas Evers
Michael Wagner
Martin Bossart
Romain Bertrand
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Antaros Medical Ab
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    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07KPEPTIDES
    • C07K14/00Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof
    • C07K14/435Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof from animals; from humans
    • C07K14/575Hormones
    • C07K14/605Glucagons
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K38/00Medicinal preparations containing peptides
    • A61K38/16Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof
    • A61K38/17Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof from animals; from humans
    • A61K38/22Hormones
    • A61K38/28Insulins
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K45/00Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
    • A61K45/06Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00Drugs for disorders of the metabolism
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00Drugs for disorders of the metabolism
    • A61P3/08Drugs for disorders of the metabolism for glucose homeostasis
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00Drugs for disorders of the metabolism
    • A61P3/08Drugs for disorders of the metabolism for glucose homeostasis
    • A61P3/10Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07KPEPTIDES
    • C07K14/00Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof
    • C07K14/435Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof from animals; from humans
    • C07K14/575Hormones
    • C07K14/57563Vasoactive intestinal peptide [VIP]; Related peptides
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K38/00Medicinal preparations containing peptides
    • YGENERAL TAGGING OF NEW TECHNOLOGICAL DEVELOPMENTS; GENERAL TAGGING OF CROSS-SECTIONAL TECHNOLOGIES SPANNING OVER SEVERAL SECTIONS OF THE IPC; TECHNICAL SUBJECTS COVERED BY FORMER USPC CROSS-REFERENCE ART COLLECTIONS [XRACs] AND DIGESTS
    • Y02TECHNOLOGIES OR APPLICATIONS FOR MITIGATION OR ADAPTATION AGAINST CLIMATE CHANGE
    • Y02ATECHNOLOGIES FOR ADAPTATION TO CLIMATE CHANGE
    • Y02A50/00TECHNOLOGIES FOR ADAPTATION TO CLIMATE CHANGE in human health protection, e.g. against extreme weather
    • Y02A50/30Against vector-borne diseases, e.g. mosquito-borne, fly-borne, tick-borne or waterborne diseases whose impact is exacerbated by climate change

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
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  • Medicinal Chemistry (AREA)
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  • Diabetes (AREA)
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  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Obesity (AREA)
  • Chemical Kinetics & Catalysis (AREA)
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  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Medicines Containing Antibodies Or Antigens For Use As Internal Diagnostic Agents (AREA)

Claims (15)

1. Peptidni spoj formule (I): [image] naznačen time što X2 predstavlja aminokiselinu odabranu između Ser i d-Ser, X3 predstavlja aminokiselinu odabranu između Gln i His, X7 predstavlja aminokiselinu odabranu između Thr i Aib, X10 predstavlja aminokiselinski ostatak odabran između Tyr, Leu, Val, Ile, Phe, fenilglicina, Thr, 2-fluorofenilalanina, Cikloheksilglicina i terc-leucina, X12 predstavlja aminokiselinu odabranu između Lys, Arg i Cys (VS-DO3A), X13 predstavlja aminokiselinu odabranu između Gln, Tyr i Cys (VS-DO3A), X14 predstavlja aminokiselinski ostatak odabran između Leu, Nle i Cys (VS-DO3A), X15 predstavlja aminokiselinu odabranu između Glu i Asp, X16 predstavlja aminokiselinu odabranu između Ser, Glu, Aib i Cys (VS-DO3A), X17 predstavlja aminokiselinu odabranu između Arg, Gln, Lys, Ala i Cys (VS-DO3A), X18 predstavlja aminokiselinu odabranu između Arg, Lys i Ala, X20 predstavlja aminokiselinu odabranu između Gln, Glu, Aib, Lys i Cys (VS-DO3A), ako je X16 Glu, a X20 Lys, bočni lanci X16 i X20 mogu formirati ciklički prsten preko laktama, X21 predstavlja aminokiselinski ostatak odabran između Asp i Glu, X28 predstavlja aminokiselinu odabranu između Ala i β-Ala, X29 predstavlja aminokiselinski ostatak odabran između Gly i Thr, X32 predstavlja aminokiselinu odabranu između Glu i Ser, X40 predstavlja aminokiselinu odabranu između Cys (VS-DO3A), Cys (VS-NO2A), Cys (mal-DOTA), Cys (mal-NOTA), Cys (mal-NODAGA), Lys (DOTA), Lys (NOTA), Lys (PEG-DOTA) i Lys (VS-DO3A) ili X40 mogu biti odsutni ako jedna od aminokiselina X12, X13, X14, X16, X17 ili X20 je Cys (VS-DO3A), pri čemu DOTA, NOTA, DO3A, NO2A ili NODAGA mogu biti neopterećeni ili opterećeni metalnim ionom odabranim između Gd3+, Ga3+, Cu2+, (Al-F)2+, Y3+, Tc3+, In3+, Lu3+ i Re3+, R1 predstavlja OH ili NH2; i pri čemu je spoj agonist receptora glukagona; ili metalni kompleks ili njegova sol ili solvat.
2. Spoj formule (I) prema zahtjevu 1, naznačen time što X2 predstavlja aminokiselinu odabranu između Ser i d-Ser, X3 je Gln, X7 predstavlja aminokiselinu odabranu između Thr i Aib, X10 predstavlja aminokiselinski ostatak odabran između Tyr, Leu, Ile, X12 je Lys, X13 je Gln, X14 predstavlja aminokiselinski ostatak odabran između Leu i Nle, X15 predstavlja aminokiselinu odabranu između Glu i Asp, X16 predstavlja aminokiselinu odabranu između Ser i Glu, X17 predstavlja aminokiselinu odabranu između Arg i Gln, X18 je Arg, X20 predstavlja aminokiselinu odabranu između Gln i Lys, ako je X16 Glu i X20 Lys, bočni lanci X16 i X20 mogu formirati ciklički prsten preko laktama, X21 predstavlja aminokiselinski ostatak odabran između Asp i Glu, X28 je Ala, X29 predstavlja aminokiselinski ostatak odabran između Gly i Thr, X32 je Glu, X40 je Cys (VS-DO3A), pri čemu DO3A može biti neopterećen ili opterećen metalnim ionom odabranim između Gd3+, Ga3+, Cu2+, (Al-F)2+, Y3+, Tc3+, In3+, Lu3+ i Re3+, R1 predstavlja OH ili NH2; ili metalni kompleks ili njegova sol ili solvat.
3. Spoj formule (I) prema zahtjevu 1, odabran između spojeva SEQ ID NO: 3 - 90, kao i metalni kompleks, njegove soli ili solvati.
4. Spoj formule (I) prema bilo kojem od zahtjeva 1 do 3, odabran između spojeva SEQ ID NO: 6, 8, 13, 14, 35, 36, 49, 50, 60, 61, 79, 80, 85 i 86, kao i metalni kompleks, njegove soli ili solvati.
5. Spoj formule (I) prema bilo kojem od zahtjeva 1 do 4, naznačen time što su DOTA, NOTA, DO3A, NO2A ili NODAGA opterećeni (i) metalnim ionom Ga3+, ili (ii) metalnim ionom Gd3+.
6. Spoj formule (I) prema bilo kojem od zahtjeva 1 do 4, naznačen time što su DOTA, NOTA, DO3A, NO2A ili NODAGA opterećeni (i) metalnim radionukleotidnim ionom (Cu-64)2+, (Ga-68)3+, (Al-F-18)2+, (Y-86)3+, (ii) s metalnim radionukleotidnim ionom (Ga-67)3+, (Tc-99m)3+, (In-111)3+ ili (iii) s metalnim radionukleotidnim ionom odabranim od (Cu-67)2+, (Y-90)3+, (In-111)3+, (Lu-177)3+, (Re-186)3+ i (Re-188)3+.
7. Farmaceutski pripravak koji sadrži najmanje jedan spoj prema bilo kojem od zahtjeva 1 - 6 ili fiziološki prihvatljivu sol ili solvat bilo kojeg od njih.
8. Spoj prema bilo kojem od zahtjeva 1-6 koji je prisutan kao aktivno sredstvo u farmaceutskom pripravku, zajedno s najmanje jednim farmaceutski prihvatljivim nosačem.
9. Spoj prema bilo kojem od zahtjeva 1 - 6 za vizualizaciju receptora glukagona u živim subjektima i relevantnim tkivima.
10. Spoj prema bilo kojem od zahtjeva 1 - 6 za uporabu u medicini, posebno u humanoj medicini.
11. Spoj prema zahtjevu 5 (ii) za vizualizaciju receptora glukagona u živim subjektima i relevantnim tkivima pomoću MRI.
12. Spoj prema zahtjevu 6 (i) za vizualizaciju receptora glukagona u živim subjektima i relevantnim tkivima pomoću PET-a.
13. Spoj prema zahtjevu 6 (ii) za vizualizaciju receptora glukagona u živim subjektima i relevantnim tkivima pomoću SPECT-a.
14. Spoj prema zahtjevu 6 (iii) za uporabu u radioterapiji.
15. Spoj prema bilo kojem od zahtjeva 1 do 6 za uporabu u liječenju hipoglikemije, povećanja razine glukoze u krvi ili kao dodatna terapija inzulinom, pri čemu se komponenta posebno daje parenteralno.
HRP20210073TT 2015-12-14 2021-01-14 Selektivni agonisti receptora glukagona s kelatnim dijelom za svrhe prikazivanja HRP20210073T1 (hr)

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EP15307000 2015-12-14
PCT/EP2016/080553 WO2017102613A1 (en) 2015-12-14 2016-12-12 Selective glucagon receptor agonists comprising a chelating moiety for imaging purposes
EP16819291.2A EP3389697B1 (en) 2015-12-14 2016-12-12 Selective glucagon receptor agonists comprising a chelating moiety for imaging purposes

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US (1) US11046743B2 (hr)
EP (1) EP3389697B1 (hr)
JP (1) JP6986516B2 (hr)
KR (1) KR20180086270A (hr)
CN (1) CN108697767B (hr)
AU (1) AU2016372245B2 (hr)
BR (1) BR112018011892A2 (hr)
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HU (1) HUE053079T2 (hr)
IL (1) IL259961A (hr)
LT (1) LT3389697T (hr)
MX (1) MX2018007323A (hr)
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RU (1) RU2018125958A (hr)
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DE102004043153B4 (de) 2004-09-03 2013-11-21 Philipps-Universität Marburg Erfindung betreffend GLP-1 und Exendin
CN101282991A (zh) * 2005-05-26 2008-10-08 布里斯托尔-迈尔斯斯奎布公司 N-端修饰的胰高血糖素样肽-1受体调节剂
WO2007139589A1 (en) 2006-05-26 2007-12-06 Bristol-Myers Squibb Company Sustained release glp-1 receptor modulators
UA116217C2 (uk) * 2012-10-09 2018-02-26 Санофі Пептидна сполука як подвійний агоніст рецепторів glp1-1 та глюкагону
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EP3389697B1 (en) 2020-12-16
PL3389697T3 (pl) 2021-04-19
JP2019508480A (ja) 2019-03-28
ES2846023T3 (es) 2021-07-28
SI3389697T1 (sl) 2021-02-26
WO2017102613A1 (en) 2017-06-22
AU2016372245B2 (en) 2020-07-16
LT3389697T (lt) 2021-02-10
SG11201804993RA (en) 2018-07-30
CN108697767A (zh) 2018-10-23
RU2018125958A3 (hr) 2020-06-09
CA3008052A1 (en) 2017-06-22
PT3389697T (pt) 2021-01-22
DK3389697T3 (da) 2021-01-11
US20200262885A1 (en) 2020-08-20
US11046743B2 (en) 2021-06-29
BR112018011892A2 (pt) 2018-12-04
RU2018125958A (ru) 2020-01-20
CA3008052C (en) 2024-01-02
HUE053079T2 (hu) 2021-06-28
CN108697767B (zh) 2022-04-15
MX2018007323A (es) 2019-01-10
IL259961A (en) 2018-07-31
KR20180086270A (ko) 2018-07-30
JP6986516B2 (ja) 2021-12-22
AU2016372245A1 (en) 2018-07-26
EP3389697A1 (en) 2018-10-24

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