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HRP20120989T1 - Peptidi koji se vežu za receptor eritropoetina - Google Patents

Peptidi koji se vežu za receptor eritropoetina Download PDF

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Publication number
HRP20120989T1
HRP20120989T1 HRP20120989TT HRP20120989T HRP20120989T1 HR P20120989 T1 HRP20120989 T1 HR P20120989T1 HR P20120989T T HRP20120989T T HR P20120989TT HR P20120989 T HRP20120989 T HR P20120989T HR P20120989 T1 HRP20120989 T1 HR P20120989T1
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peptide
peg
peptide dimer
daltons
molecular weight
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HRP20120989TT
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English (en)
Inventor
Christopher P. Holmes
Qun Yin
Guy Lalonde
Peter J. Schatz
David Tumelty
Balu Palani
Genet Zemede
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Affymax, Inc.
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Publication of HRP20120989T1 publication Critical patent/HRP20120989T1/hr

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    • C07ORGANIC CHEMISTRY
    • C07KPEPTIDES
    • C07K14/00Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof
    • C07K14/001Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof by chemical synthesis
    • 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
    • A61K38/10Peptides having 12 to 20 amino acids
    • 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
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    • 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
    • A61P31/00Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/12Antivirals
    • A61P31/14Antivirals for RNA viruses
    • A61P31/18Antivirals for RNA viruses for HIV
    • 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
    • A61P37/00Drugs for immunological or allergic disorders
    • A61P37/02Immunomodulators
    • 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
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    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P7/00Drugs for disorders of the blood or the extracellular fluid
    • 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
    • A61P7/04Antihaemorrhagics; Procoagulants; Haemostatic agents; Antifibrinolytic agents
    • 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
    • A61P7/00Drugs for disorders of the blood or the extracellular fluid
    • A61P7/08Plasma substitutes; Perfusion solutions; Dialytics or haemodialytics; Drugs for electrolytic or acid-base disorders, e.g. hypovolemic shock
    • 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
    • A61P9/10Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07KPEPTIDES
    • C07K14/00Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof
    • 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
    • C07K14/475Growth factors; Growth regulators
    • C07K14/505Erythropoietin [EPO]
    • 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
    • C07K7/08Linear peptides containing only normal peptide links having 12 to 20 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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Claims (37)

1. Peptid s 17 do 40 aminokiselinskih ostataka u dužini koji sadrži sekvencu aminokiselina: LYACHX0GPITX1VCQPLR (SEQ ID NO: 1), gdje je X0 ostatak izabran između metionina (M) i homoserin metiletera (Hsm), i X1 je ostatak izabran između triptofana (W), 1-naftilalanina (1-nal), i 2-naftilalanina (2-nal), gdje se taj peptid veže za i aktivira receptor eritropoetina (EPO-R).
2. Peptid prema zahtjevu 1, gdje je N-kraj tog peptida acetiliran.
3. Peptid prema zahtjevu 1 ili zahtjevu 2, taj peptid sadrži sekvencu aminokiselina izabranu između: [image] [image]
4. Peptid prema bilo kojem od zahtjeva 1 do 3, gdje je peptid monomer.
5. Peptid prema bilo kojem od zahtjeva 1 do 4, koji dalje sadrži jedan ili više polimera topljivih u vodi koji su kovalentno povezani s peptidom.
6. Peptid prema zahtjevu 5, gdje je polimer topljiv u vodi polietilenglikol (PEG).
7. Peptid prema zahtjevu 6, gdje taj PEG sarži linearnu nerazgranatu molekulu s molekularnom težinom od 500 do 60,000 Daltona.
8. Peptid prema zahtjevu 7, gdje PEG ima molekularnu težinu manju od 20,000 Daltona.
9. Peptid prema zahtjevu 7, gdje PEG ima molekularnu težinu od 20,000 do 60,000 Daltona.
10. Peptid prema bilo kojem od zahtjeva 6-7 i 9, gdje PEG ima molekularnu težinu od 20,000 do 40,000 Daltona.
11. Peptid prema zahtjevu 7, gdje su dvije PEG jedinke kovalentno vezane za peptid, svaki od tih PEG sadrži linearnu nerazgranatu molekulu.
12. Peptid prema zahtjevu 11, gdje svaki PEG ima molekularnu težinu od 20,000d 30,000 Daltona.
13. Peptidni dimer koji sadrži dva monomera, oba ta monomera su peptid prema bilo kojem od zahtjeva 1 do 3 i 5 do 12.
14. Peptidni dimer prema zahtjevu 13, gdje je peptid homodimer.
15. Peptidni dimer prema zahtjevu 13, sadrži: (a) prvi peptidni lanac; (b) drugi peptidni lanac; i (c) povezujuću jedinku koja spaja prvi i drugi peptidni lanac, gdje su oba, i prvi peptidni lanac i drugi peptidni lanac, peptidi prema zahtjevu 1.
16. Peptidni dimer prema zahtjevu 15, gdje barem jedan od prvog peptidnog lanca i drugog peptidnog lanca sadrži sekvencu aminokiselina izabranu između: [image] [image]
17. Peptidni dimer prema zahtjevu 15, gdje povezujuća jedinka obuhvaća formulu: -NH-R3-NH- gdje R3 je C1-6 alkilen.
18. Peptidni dimer prema zahtjevu 17, gdje je povezujuća jedinka ostatak lizina.
19. Peptidni dimer prema zahtjevu 15, gdje povezujuća jedinka obuhvaća formulu: -CO-(CH2)n-X-(CH2)m-CO- gdje je n cijeli broj od 0 do je cijeli broj od 1 do 10, X se izabire između O, S, N(CH2)pNR1, NCO(CH2)pNR1, i CHNR1, R1 se izabire između H, Boc, i Cbz, i p je cijeli broj od 1 do 10.
20. Peptidni dimer prema zahtjevu 19, gdje su n i m svaki 1, X je NCO(CH2)pNR1, p je 2, i R1 je H.
21. Peptidni dimer prema zahtjevu 15, dalje sadrži u vodi topljivi polimer.
22. Peptidni dimer prema zahtjevu 21, gdje je u vodi topljivi polimer kovalentno vezan za povezujuću jedinku.
23. Peptidni dimer prema zahtjevu 15, dalje sadrži razmaknicu.
24. Peptidni dimer prema zahtjevu 23, gdje razmaknica obuhvaća formulu: -NH-(CH2)α-[O-(CH2)β]γ-Oδ-(CH2)ε-Y- gdje α, β, i ε su cijeli brojevi čije su vrijednosti nezavisno izabrane između 1 do 6, δ je 0 ili 1, γ je cijeli broj izabran između 0 do 10, i Y je izabran između NH ili CO, uz uvjet da je 2 kada je γ veći od 1.
25. Peptidni dimer prema zahtjevu 24 gdje je svaki od α, β, i ε jednak 2, svaki od γ i δ je 1, i Y je NH.
26. Peptidni dimer prema zahtjevu 23, dalje sadrži jedan ili više u vodi topljivih polimera.
27. Peptidni dimer prema zahtjevu 26, gdje je u vodi topljivi polimer kovalentno vezan za razmaknicu.
28. Peptidni dimer prema zahtjevu 21 ili 26, gdje je u vodi topljivi polimer polietilenglikol (PEG).
29. Peptidni dimer prema zahtjevu 28, gdje PEG je linearni nerazgranati PEG s molekularnom težinom od 500 do 60,000 Daltona.
30. Peptidni dimer prema zahtjevu 28 ili 29, gdje PEG ima molekularnu težinu od 500 do manje od 20,000 Daltona.
31. Peptidni dimer prema zahtjevu 28 ili 29, gdje PEG ima molekularnu težinu od 20,000 do 60,000 Daltona.
32. Peptidni dimer prema zahtjevu 28, 29 ili 31, gdje PEG ima molekularnu težinu od 20,000 do 40,000 Daltona.
33. Peptidni dimer prema zahtjevu 28, gdje su dvije PEG jedinke kovalentno vezane za peptid, svaki od tih PEG sadrži linearnu nerazgranatu molekulu.
34. Peptidni dimer prema zahtjevu 33, gdje svaki PEG ima molekularnu težinu od 20,000 do 30,000 Daltona.
35. Peptid ili peptidni dimer prema bilo kojem od zahtjeva 1 do 34 za uporabu u liječenju poremećaja naznačenog manjkom eritropoetina ili niskom ili manjkavom populacijom crvenih krvnih stanica.
36. Peptid ili peptidni dimer za uporabu prema zahtjevu 35, gdje se poremećaj izabire iz skupine koja obuhvaća: zadnji stupanj zatajenja bubrega ili dijaliza; anemija povezana s AIDS-om, autoimunom bolesti ili malignitetom; betatalasemija; cistična fibroza; rana anemija preuranjene zrelosti; anemija povezana s kroničnom inflamatornom bolesti; ozljeda leđne moždine; akutni gubitak krvi; starenje; i stanja neoplastične bolesti praćena abnormalnom eritropoezom.
37. Farmaceutski oblik koji sadrži: (i) peptid ili peptidni dimer prema bilo kojem od zahtjeva 1 do 34; i (ii) farmaceutski prihvatljivi nosač.
HRP20120989TT 2003-05-12 2004-05-12 Peptidi koji se vežu za receptor eritropoetina HRP20120989T1 (hr)

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Application Number Priority Date Filing Date Title
US47024503P 2003-05-12 2003-05-12
PCT/US2004/014886 WO2004101611A2 (en) 2003-05-12 2004-05-12 Peptides that bind to the erythropoietin receptor

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HRP20120989T1 true HRP20120989T1 (hr) 2013-01-31

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US (4) US7528104B2 (hr)
EP (1) EP1625156B1 (hr)
JP (1) JP4949844B2 (hr)
KR (2) KR20120094001A (hr)
CN (1) CN1823088B (hr)
AU (1) AU2004238868B2 (hr)
BR (1) BRPI0411172A (hr)
CA (1) CA2525497A1 (hr)
DK (1) DK1625156T3 (hr)
EA (1) EA010099B1 (hr)
ES (1) ES2395413T3 (hr)
HR (1) HRP20120989T1 (hr)
IL (1) IL198844A0 (hr)
IS (1) IS8167A (hr)
MX (1) MXPA05012313A (hr)
NO (1) NO20055847L (hr)
NZ (1) NZ543935A (hr)
PL (1) PL1625156T3 (hr)
PT (1) PT1625156E (hr)
SI (1) SI1625156T1 (hr)
WO (1) WO2004101611A2 (hr)
ZA (1) ZA200509971B (hr)

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