HRP20190494T1 - Pro-koagulantski spojevi i postupci njihove uporabe - Google Patents

Pro-koagulantski spojevi i postupci njihove uporabe Download PDF

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Publication number
HRP20190494T1
HRP20190494T1 HRP20190494TT HRP20190494T HRP20190494T1 HR P20190494 T1 HRP20190494 T1 HR P20190494T1 HR P20190494T T HRP20190494T T HR P20190494TT HR P20190494 T HRP20190494 T HR P20190494T HR P20190494 T1 HRP20190494 T1 HR P20190494T1
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HR
Croatia
Prior art keywords
nucleic acid
compound according
compound
vector
conjugate
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HRP20190494TT
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English (en)
Inventor
Karina THORN
Garabet G. TOBY
Adam R. Mezo
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Bioverativ Therapeutics Inc.
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Publication of HRP20190494T1 publication Critical patent/HRP20190494T1/hr

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    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K38/00—Medicinal preparations containing peptides
    • A61K38/16—Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof
    • A61K38/17—Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof from animals; from humans
    • A61K38/36—Blood coagulation or fibrinolysis factors
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K47/00—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
    • A61K47/50—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates
    • A61K47/51—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent
    • A61K47/62—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent the modifying agent being a protein, peptide or polyamino acid
    • A61K47/64—Drug-peptide, drug-protein or drug-polyamino acid conjugates, i.e. the modifying agent being a peptide, protein or polyamino acid which is covalently bonded or complexed to a therapeutically active agent
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P7/00—Drugs for disorders of the blood or the extracellular fluid
    • A61P7/04—Antihaemorrhagics; Procoagulants; Haemostatic agents; Antifibrinolytic agents
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07K—PEPTIDES
    • C07K14/00—Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof
    • C07K14/001—Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof by chemical synthesis
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07K—PEPTIDES
    • C07K14/00—Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof
    • C07K14/435—Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof from animals; from humans
    • C07K14/745—Blood coagulation or fibrinolysis factors
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07K—PEPTIDES
    • C07K7/00—Peptides having 5 to 20 amino acids in a fully defined sequence; Derivatives thereof
    • C07K7/04—Linear peptides containing only normal peptide links
    • C07K7/08—Linear peptides containing only normal peptide links having 12 to 20 amino acids
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K38/00—Medicinal preparations containing peptides

Claims (13)

1. Spoj koji sadrži: (a) sekvencu aminokiseline koja sadrži formulu (I): naznačen time što L je L-leucin; A je L-alanin; S je L-serin; Y je L-tirozin; C1 i C2 su cistein; pri čemu sekvenca aminokiseline sadrži barem jednu od: SEQ ID NO: 4, 9-22, 24-38, 43-54, 61-64, 66-91, 93-97, 99, 104-146, 148-183, 200-202, 204-208, 214-216, 219-222, 226-233, 239-242, 244-246, 260, 265-267, 269-272, 282-293, 296, 307, 315, 337, 339, 346-348, 360, 362, 364, 367-375, 380, 383-386, 389, 392, 400-402, 406, 409-415, 419-421, 424-463, 471-487, 492-495, 526-529, 531, 533, 536-537, 543, 545, 547, 550-555, te PRIRTVGPGSRSASGKLTCLASYCWLFWTGIA; ili (b) retro-, inverzo- ili retro-inverzo varijantu sekvence aminokiseline pod a); ili njezinu farmaceutski prihvatljivu sol ili solvat.
2. Spoj prema zahtjevu 1, naznačen time što sekvenca aminokiseline sadrži barem jednu od: SEQ ID NO: 29, 48-54, 61-64, 66-86, 91, 93-97, 104-146, 148-183, 200-202, 204, 205, 214-216, 219-222, 226-233, 239-242, 244, 270-272, 282-293, 296, 307, 346, 360, 367, 369-370, 374-375, 383, 385, 389, 400-402, 406, 409-414, 419, 420, 424-440, 450-460, 462, 471-487, 492, 494, 526-529, 531, 533, 536-537, 543, 545, 547, 550-555 te PRIRTVGPGSRSASGKLTCLASYCWLFWTGIA.
3. Spoj prema zahtjevu 1 ili zahtjevu 2, naznačen time što je spoj kovalentno vezan dijelom koji produžuje poluživot, izborno pri čemu je dio koji produžuje poluživot odabran od Fc, FcRn vezujućeg liganda, albumina, albumin-vezujućeg liganda, transferina, PEG dijela, PPG dijela, PAS dijela te HES dijela.
4. In vitro postupak povećanja katalitičke aktivnosti (kcat) faktora zgrušavanja krvi, sadrži dovođenje u kontakt faktora zgrušavanja krvi sa spojem prema bilo kojem od zahtjeva 1 do 3.
5. Postupak proizvodnje spoja prema bilo kojem od zahtjeva 1 do 3, postupak sadrži formiranje peptida koji ima sekvencu aminokiseline ili retro-, inverzo- ili retro-inverzo varijantu iste, koristeći sintezu peptida čvrste faze.
6. Konjugat koji sadrži spoj prema bilo kojem od zahtjeva 1 do 3 i prvi heterologni dio, naznačen time što su spoj i prvi heterologni dio vezani jedan na drugi preko prvog izbornog veznika.
7. Konjugat prema zahtjevu 6, koji sadrži strukturu prema Formuli (A1) ili (A2): naznačen time što je Het1 prvi heterologni dio; je m cijeli broj odabran od 0 i 1; je L1 ili odsutan (m=0) ili prisutan (m=1), te kada je prisutan je veznik; je Pep spoj prema bilo kojem od zahtjeva 1 do 3; i je (-) kovalentna veza.
8. Molekula nukleinske kiseline ili set molekula nukleinske kiseline koji šifrira spoj prema bilo kojem od zahtjeva 1 do 3 ili konjugat prema zahtjevu 6 ili 7 ili njihov komplement.
9. Vektor ili set vektora koji sadrži molekulu nukleinske kiseline ili set molekula nukleinske kiseline prema zahtjevu 8 ili njihov komplement.
10. Stanica domaćin koja sadrži vektor ili set vektora prema zahtjevu 9.
11. Farmaceutski pripravak koji sadrži spoj prema bilo kojem od zahtjeva 1 do 3, konjugat prema zahtjevu 6 ili 7, molekulu nukleinske kiseline ili set molekula nukleinske kiseline prema zahtjevu 8 ili vektor ili set vektora prema zahtjevu 9 i farmaceutski prihvatljiv nosač.
12. Spoj prema bilo kojem od zahtjeva 1 do 3, konjugat prema zahtjevu 6 ili 7, molekula nukleinske kiseline ili set molekula nukleinske kiseline prema zahtjevu 8, vektor ili set vektora prema zahtjevu 9, ili farmaceutski pripravak prema zahtjevu 11, za uporabu u liječenju, ublažavanju ili prevenciji bolesti ili poremećaja krvarenja kod subjekta kojemu je to potrebno.
13. Spoj prema bilo kojem od zahtjeva 1 do 3, konjugat prema zahtjevu 6 ili 7, molekula nukleinske kiseline ili set molekula nukleinske kiseline prema zahtjevu 8, vektor ili set vektora prema zahtjevu 9, ili farmaceutski pripravak prema zahtjevu 11, za uporabu u liječenju, ublažavanju ili prevenciji nedostatka faktora zgrušavanja kod sisavca, pri čemu je faktor zgrušavanja odabran iz skupine koja se sastoji od FVII, FVIIa, FVIII, FIX i FXI.
HRP20190494TT 2011-06-10 2019-03-12 Pro-koagulantski spojevi i postupci njihove uporabe HRP20190494T1 (hr)

Applications Claiming Priority (9)

Application Number Priority Date Filing Date Title
US201161495818P 2011-06-10 2011-06-10
US201161496542P 2011-06-13 2011-06-13
US201161496540P 2011-06-13 2011-06-13
US201161496541P 2011-06-13 2011-06-13
US201161496543P 2011-06-13 2011-06-13
US201261600237P 2012-02-17 2012-02-17
US201261605540P 2012-03-01 2012-03-01
PCT/US2012/041777 WO2012170969A2 (en) 2011-06-10 2012-06-09 Pro-coagulant compounds and methods of use thereof
EP12797036.6A EP2717898B1 (en) 2011-06-10 2012-06-09 Pro-coagulant compounds and methods of use thereof

Publications (1)

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HRP20190494T1 true HRP20190494T1 (hr) 2019-07-12

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US (1) US9486507B2 (hr)
EP (2) EP3527218A1 (hr)
AU (1) AU2012267484B2 (hr)
CA (1) CA2838833A1 (hr)
CY (1) CY1121509T1 (hr)
DK (1) DK2717898T3 (hr)
ES (1) ES2724778T3 (hr)
HR (1) HRP20190494T1 (hr)
HU (1) HUE043894T2 (hr)
LT (1) LT2717898T (hr)
PL (1) PL2717898T3 (hr)
PT (1) PT2717898T (hr)
SI (1) SI2717898T1 (hr)
WO (1) WO2012170969A2 (hr)

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