HRP20171048T1 - Novi agonisti angiotenzinskog receptora tipa 2 (at2) i njihove upotrebe - Google Patents

Novi agonisti angiotenzinskog receptora tipa 2 (at2) i njihove upotrebe Download PDF

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Publication number
HRP20171048T1
HRP20171048T1 HRP20171048TT HRP20171048T HRP20171048T1 HR P20171048 T1 HRP20171048 T1 HR P20171048T1 HR P20171048T T HRP20171048T T HR P20171048TT HR P20171048 T HRP20171048 T HR P20171048T HR P20171048 T1 HRP20171048 T1 HR P20171048T1
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Croatia
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compound according
peptide compound
abu
xaa1
ala
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HRP20171048TT
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Louwe De Vries
Sieger Adriaan Nelemans
Rick Rink
Antonius Jacobus Marinus Roks
Gert Nikolaas Moll
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Lanthiopep B.V.
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Publication of HRP20171048T1 publication Critical patent/HRP20171048T1/hr

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    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07KPEPTIDES
    • C07K7/00Peptides having 5 to 20 amino acids in a fully defined sequence; Derivatives thereof
    • C07K7/64Cyclic peptides containing only normal peptide links
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07KPEPTIDES
    • C07K7/00Peptides having 5 to 20 amino acids in a fully defined sequence; Derivatives thereof
    • C07K7/04Linear peptides containing only normal peptide links
    • C07K7/14Angiotensins: Related peptides
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K38/00Medicinal preparations containing peptides
    • A61K38/04Peptides having up to 20 amino acids in a fully defined sequence; Derivatives thereof
    • A61K38/12Cyclic peptides, e.g. bacitracins; Polymyxins; Gramicidins S, C; Tyrocidins A, B or C
    • 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
    • A61P11/00Drugs for disorders of the respiratory system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00Drugs for dermatological disorders
    • A61P17/02Drugs for dermatological disorders for treating wounds, ulcers, burns, scars, keloids, or the like
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00Drugs for dermatological disorders
    • A61P17/14Drugs for dermatological disorders for baldness or alopecia
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P7/00Drugs for disorders of the blood or the extracellular fluid
    • A61P7/06Antianaemics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system
    • A61P9/12Antihypertensives
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07KPEPTIDES
    • C07K7/00Peptides having 5 to 20 amino acids in a fully defined sequence; Derivatives thereof
    • C07K7/04Linear peptides containing only normal peptide links
    • C07K7/06Linear peptides containing only normal peptide links having 5 to 11 amino acids
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K38/00Medicinal preparations containing peptides

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • General Health & Medical Sciences (AREA)
  • Organic Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Proteomics, Peptides & Aminoacids (AREA)
  • Epidemiology (AREA)
  • Biophysics (AREA)
  • Biochemistry (AREA)
  • Molecular Biology (AREA)
  • Genetics & Genomics (AREA)
  • Diabetes (AREA)
  • Gastroenterology & Hepatology (AREA)
  • Immunology (AREA)
  • Hematology (AREA)
  • Cardiology (AREA)
  • Dermatology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Oncology (AREA)
  • Pain & Pain Management (AREA)
  • Obesity (AREA)
  • Neurology (AREA)
  • Endocrinology (AREA)
  • Communicable Diseases (AREA)
  • Rheumatology (AREA)
  • Biomedical Technology (AREA)
  • Emergency Medicine (AREA)
  • Neurosurgery (AREA)
  • Pulmonology (AREA)
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Claims (15)

1. Ciklični peptidni spoj koje se sastoji od aminokiselinske sekvence Xaa1- Asp-Arg- Ile/Val- Xaa5- Ile/Val- His- Xaa8, koje sadrži vezu u vidu tioetarskog mosta između bočnih lanaca Xaa5 i Xaa8, tako da Xaa5 i Xaa8 zajedno čine strukturu prema bilo kojoj od općih formula: [image] [image] [image] naznačeno time što su R, R1, R2, R3, R4 i R5 nezavisno odabrani od -H, C1-C10 alkil ili aralkil grupe, pri čemu su poželjno R, R1, R2, R3, R4 i R5 nezavisno odabrani od H i CH3, i pri čemu je Xaa1 izabran iz grupe koja se sastoji od naelektriziranih aminokiselina, aromatičnih aminokiselina i hidrofobnih aminokiselina i njihovih varijanti otpornih na proteazu, ili njegova farmaceutski prihvatljiva sol.
2. Peptidni spoj prema patentnom zahtjevu 1, naznačeno time što je Xaa1 izabran iz grupe koja se sastoji od D-stereoizomera naelektrisanih aminokiselina, aromatičnih aminokiselina i hidrofobnih aminokiselina.
3. Peptidni spoj prema patentnom zahtjevu 1 ili 2, naznačeno time što je Xaa1 pozitivno naelektrizirana aminokiselina, pri čemu poželjno Xaa1 predstavlja Lys ili Arg.
4. Peptidni spoj prema patentnom zahtjevu 1 ili 2, naznačeno time što je Xaa1 negativno naelektrizirana aminokiselina, pri čemu poželjno Xaa1 predstavlja Asp, Glu ili pyroGlu.
5. Peptidni spoj prema patentnom zahtjevu 1 ili 2, naznačeno time što je Xaa1 hidrofobna aminokiselina, pri čemu poželjno Xaa1 predstavlja Ile, Leu ili Val.
6. Peptidni spoj prema patentnom zahtjevu 1 ili 2, naznačeno time što je Xaa1 aromatična aminokiselina, pri čemu poželjno Xaa1 predstavlja Tyr ili Phe.
7. Peptidni spoj prema bilo kojem od prethodnih patentnih zahtjeva, naznačeno time što Xaa5 predstavlja D-stereoizomer.
8. Peptidni spoj prema bilo kojem od prethodnih patentnih zahtjeva, naznačeno time što Xaa8 predstavlja L- stereoizomer.
9. Peptidni spoj prema bilo kojem od prethodnih patentnih zahtjeva, naznačeno time što Xaa5 predstavlja D-stereoizomer i Xaa8 predstavlja L- stereoizomer.
10. Peptidni spoj prema bilo kojem od prethodnih patentnih zahtjeva, koje ima aminokiselinsku sekvencu izabranu iz grupe koja se sastoji od: Lys-Asp-Arg-Val-Abu/Ala-Ile-His-Abu/Ala (K-cAng(1-7)) Asp-Asp-Arg-Val-Abu/Ala-Ile-His-Abu/Ala (D-cAng(1-7)) Tyr-Asp-Arg-Val-Abu/Ala-Ile-His-Abu/Ala (Y-cAng(1-7)) Ile-Asp-Arg-Val-Abu/Ala-Ile-His-Abu/Ala (I-cAng(1-7)) Asn-Asp-Arg-Val-Abu/Ala-Ile-His-Abu/Ala (N-cAng(1-7)) pod uvjetom da peptid ne sadrži dva Abu (2-aminobuterna kiselina) ostatka.
11. Farmaceutska kompozicija koja sadrži peptidni spoj prema bilo kojem od patentnih zahtjeva 1 do 10, i farmaceutski prihvatljiv adjuvans, razblaživač ili nosač.
12. In vitro upotreba peptidnog jedinjenja prema bilo kom od patentnih zahtjeva 1 do 10 kao agonista angiotenzin II receptora tipa 2 (AT2).
13. Peptidni spoj prema bilo kom od patentnih zahtjeva 1 do 10, za upotrebu u liječenju i/ili prevenciji stanja u kome je selektivni agonizam prema AT2 receptoru poželjan i/ili potreban.
14. Peptidni spoj prema bilo kojem od patentnih zahtjeva 1 do 10, za upotrebu u liječenju i/ili prevenciji prema patentnom zahtjevu 13, naznačeno time što je navedeno stanje dijabetes (tipa II), kardiovaskularno oboljenje, hipertenzija, srčana insuficijencija, infekcija, alopecija, anemija, citopenija, oboljenje živaca, inflamacija, fibroza, kancer, akutni respiratorni distres sindrom ili zarastanje rana.
15. Kombinirani proizvod koji sadrži kao zasebne entitete (A) peptidni spoj prema bilo kojem od patentnih zahtjeva 1-10; i (B) spoj odabran od antagonista AT1 receptora i ACE inhibitora, i/ili (C) spoj odabran od agonista Mas receptora i ACE2, naznačen time što je svaka od komponenti (A), (B) i/ili (C) formulirana u smjesi sa farmaceutski prihvatljivim adjuvansom, razblaživačem ili nosačem.
HRP20171048TT 2010-11-23 2017-07-10 Novi agonisti angiotenzinskog receptora tipa 2 (at2) i njihove upotrebe HRP20171048T1 (hr)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
EP10192208A EP2455388A1 (en) 2010-11-23 2010-11-23 Novel angiotensin type 2 (AT2) receptor agonists and uses thereof.
EP11791636.1A EP2643342B1 (en) 2010-11-23 2011-11-22 Novel angiotensin type 2 (at2) receptor agonists and uses thereof
PCT/NL2011/050793 WO2012070936A1 (en) 2010-11-23 2011-11-22 Novel angiotensin type 2 (at2) receptor agonists and uses thereof

Publications (1)

Publication Number Publication Date
HRP20171048T1 true HRP20171048T1 (hr) 2017-10-06

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US (4) US9290540B2 (hr)
EP (2) EP2455388A1 (hr)
JP (2) JP5837087B2 (hr)
KR (1) KR101512916B1 (hr)
CN (1) CN103314006B (hr)
AU (1) AU2011332397B2 (hr)
CA (1) CA2818299C (hr)
CY (1) CY1119036T1 (hr)
DK (1) DK2643342T3 (hr)
ES (1) ES2632553T3 (hr)
HR (1) HRP20171048T1 (hr)
HU (1) HUE035167T2 (hr)
LT (1) LT2643342T (hr)
NZ (1) NZ610732A (hr)
PL (1) PL2643342T3 (hr)
PT (1) PT2643342T (hr)
RS (1) RS56130B1 (hr)
SI (1) SI2643342T1 (hr)
WO (1) WO2012070936A1 (hr)

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PT2643342T (pt) 2017-07-12
CA2818299C (en) 2018-12-04
AU2011332397B2 (en) 2015-11-05
LT2643342T (lt) 2017-09-11
US20190135867A1 (en) 2019-05-09
US9290540B2 (en) 2016-03-22
EP2643342A1 (en) 2013-10-02
KR101512916B1 (ko) 2015-04-16
US9707268B2 (en) 2017-07-18
HUE035167T2 (en) 2018-05-02
CN103314006B (zh) 2016-04-13
DK2643342T3 (en) 2017-07-24
CN103314006A (zh) 2013-09-18
WO2012070936A1 (en) 2012-05-31
ES2632553T3 (es) 2017-09-14
EP2643342B1 (en) 2017-04-12
US20140094400A1 (en) 2014-04-03
US10214563B2 (en) 2019-02-26
CY1119036T1 (el) 2018-01-10
AU2011332397A1 (en) 2013-05-02
PL2643342T3 (pl) 2017-09-29
KR20130099178A (ko) 2013-09-05
RS56130B1 (sr) 2017-10-31
NZ610732A (en) 2014-05-30
US20160220632A1 (en) 2016-08-04
JP5837087B2 (ja) 2015-12-24
SI2643342T1 (sl) 2017-08-31
JP2016074675A (ja) 2016-05-12
EP2455388A1 (en) 2012-05-23
US20170283465A1 (en) 2017-10-05
CA2818299A1 (en) 2012-05-31
JP2014503506A (ja) 2014-02-13

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