HRP20161614T1 - Terapijska sredstva za smanjenje razina paratiroidnog hormona - Google Patents

Terapijska sredstva za smanjenje razina paratiroidnog hormona Download PDF

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Publication number
HRP20161614T1
HRP20161614T1 HRP20161614TT HRP20161614T HRP20161614T1 HR P20161614 T1 HRP20161614 T1 HR P20161614T1 HR P20161614T T HRP20161614T T HR P20161614TT HR P20161614 T HRP20161614 T HR P20161614T HR P20161614 T1 HRP20161614 T1 HR P20161614T1
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HR
Croatia
Prior art keywords
compound according
cysteine
peptide
compound
arginine
Prior art date
Application number
HRP20161614TT
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English (en)
Inventor
Felix Karim
Amos Baruch
Derek Maclean
Kanad Das
Qun Yin
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Kai Pharmaceuticals, Inc.
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Family has litigation
First worldwide family litigation filed litigation Critical https://patents.darts-ip.com/?family=43527590&utm_source=google_patent&utm_medium=platform_link&utm_campaign=public_patent_search&patent=HRP20161614(T1) "Global patent litigation dataset” by Darts-ip is licensed under a Creative Commons Attribution 4.0 International License.
Application filed by Kai Pharmaceuticals, Inc. filed Critical Kai Pharmaceuticals, Inc.
Publication of HRP20161614T1 publication Critical patent/HRP20161614T1/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
    • C07K7/04Linear 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
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/59Compounds containing 9, 10- seco- cyclopenta[a]hydrophenanthrene ring systems
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K47/00Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
    • A61K47/50Medicinal 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
    • A61K47/51Medicinal 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
    • A61K47/56Medicinal 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 an organic macromolecular compound, e.g. an oligomeric, polymeric or dendrimeric molecule
    • A61K47/59Medicinal 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 an organic macromolecular compound, e.g. an oligomeric, polymeric or dendrimeric molecule obtained otherwise than by reactions only involving carbon-to-carbon unsaturated bonds, e.g. polyureas or polyurethanes
    • A61K47/60Medicinal 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 an organic macromolecular compound, e.g. an oligomeric, polymeric or dendrimeric molecule obtained otherwise than by reactions only involving carbon-to-carbon unsaturated bonds, e.g. polyureas or polyurethanes the organic macromolecular compound being a polyoxyalkylene oligomer, polymer or dendrimer, e.g. PEG, PPG, PEO or polyglycerol
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00Medicinal preparations characterised by special physical form
    • A61K9/0012Galenical forms characterised by the site of application
    • A61K9/0019Injectable compositions; Intramuscular, intravenous, arterial, subcutaneous administration; Compositions to be administered through the skin in an invasive manner
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00Medicinal preparations characterised by special physical form
    • A61K9/08Solutions
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P13/00Drugs for disorders of the urinary system
    • A61P13/12Drugs for disorders of the urinary system of the kidneys
    • 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
    • A61P3/12Drugs for disorders of the metabolism for electrolyte homeostasis
    • A61P3/14Drugs for disorders of the metabolism for electrolyte homeostasis for calcium homeostasis
    • 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
    • A61P5/00Drugs for disorders of the endocrine system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P5/00Drugs for disorders of the endocrine system
    • A61P5/14Drugs for disorders of the endocrine system of the thyroid hormones, e.g. T3, T4
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P5/00Drugs for disorders of the endocrine system
    • A61P5/18Drugs for disorders of the endocrine system of the parathyroid hormones
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P5/00Drugs for disorders of the endocrine system
    • A61P5/18Drugs for disorders of the endocrine system of the parathyroid hormones
    • A61P5/20Drugs for disorders of the endocrine system of the parathyroid hormones for decreasing, blocking or antagonising the activity of PTH
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07KPEPTIDES
    • C07K5/00Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
    • C07K5/04Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing only normal peptide links
    • C07K5/10Tetrapeptides
    • C07K5/1002Tetrapeptides with the first amino acid being neutral
    • C07K5/1005Tetrapeptides with the first amino acid being neutral and aliphatic
    • C07K5/1013Tetrapeptides with the first amino acid being neutral and aliphatic the side chain containing O or S as heteroatoms, e.g. Cys, Ser
    • 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
    • A61K2300/00Mixtures or combinations of active ingredients, wherein at least one active ingredient is fully defined in groups A61K31/00 - A61K41/00
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K38/00Medicinal preparations containing peptides

Claims (14)

1. Spoj, koji obuhvaća peptid i konjugirajuću skupinu, gdje peptid sadrži aminokiselinsku sekvencu formule: [image] gdje X1 je D-cistein; X2 je D-arginin, D-alanin, D-valin, D-leucin, D-fenilalanin, D-serin, D-glutamin, D-norleucin ili D-norvalin; X3 je D-arginin; X4 je D-arginin ili ne-kationska aminokiselina, gdje X4 nije glicin, prolin ili aminokiselina s bočnim kiselinskim lancem; X5 je D-arginin; X6 je D-alanin, D-glicin ili D-serin; X7 je D-arginin; gdje su barem dva od X2, X3 i X4 nezavisno kationska podjedinica; i gdje je peptid vezan na svom N-kraju disulfidnom vezom za konjugirajuću skupinu.
2. Spoj prema zahtjevu 1, gdje spoj obuhvaća Ac-crrarar-NH2 (SEQ ID NO:25) ili Ac-carrrar-NH2 (SEQ ID NO:26).
3. Spoj prema zahtjevu 1, gdje peptid po duljini ima 8 do 11, 8 do 10 ili 8 do 9 aminokiselina.
4. Spoj prema bilo kojem od zahtjeva 1 do 3, gdje se konjugirajuća skupina odabire između L-cisteina, D-cisteina, homocisteina, glutationa, pegiliranog cisteina ili polipeptida sa cisteinskim ostatkom.
5. Spoj prema zahtjevu 4, gdje je konjugirajuća skupina cistein pri čemu je cistein N-acetilirani cistein.
6. Spoj prema zahtjevu 4 ili 5, gdje polipeptid sa cisteinskim ostatkom ima jednaku sekvencu kao peptid.
7. Spoj prema zahtjevu 6, gdje spoj obuhvaća: [image] ili [image]
8. Spoj koji se sastoji od peptida koji obuhvaća sekvencu carrrar (SEQ ID NO:2) i konjugirajuće skupine, taj peptid je povezan disulfidnom vezom.
9. Spoj prema zahtjevu 8, gdje je peptid kemijski modificiran na N-kraju, C-kraju ili na oba.
10. Spoj prema zahtjevu 8 ili zahtjevu 9, gdje je spoj Ac-c(C)arrrar-NH2 (SEQ ID NO:3).
11. Spoj prema bilo kojem od zahtjeva 1-5, gdje je spoj Ac-c(C)rrarar-NH2 (SEQ ID NO:28).
12. Pripravak koji sadrži spoj prema bilo kojem od zahtjeva 1 do 11, za uporabu u liječenju subjekta koji pati od sekundarnog hiperparatiroidizma (SHPT) ili hiperkalcemičnog poremećaja.
13. Pripravak koji sadrži spoj prema bilo kojem od zahtjeva 1 do 11, za uporabu u smanjivanju razina paratiroidnog hormona u subjekta.
14. Pripravak prema zahtjevu 12 ili 13, dalje sadrži drugo terapijsko sredstvo koje je vitamin D, analog vitamina D ili sinakalcet hidroklorid.
HRP20161614TT 2009-07-29 2016-12-01 Terapijska sredstva za smanjenje razina paratiroidnog hormona HRP20161614T1 (hr)

Applications Claiming Priority (5)

Application Number Priority Date Filing Date Title
US22969509P 2009-07-29 2009-07-29
US25581609P 2009-10-28 2009-10-28
US31363510P 2010-03-12 2010-03-12
EP10805078.2A EP2459208B1 (en) 2009-07-29 2010-07-29 Therapeutic agents for reducing parathyroid hormone levels
PCT/US2010/043792 WO2011014707A2 (en) 2009-07-29 2010-07-29 Therapeutic agents for reducing parathyroid hormone levels

Publications (1)

Publication Number Publication Date
HRP20161614T1 true HRP20161614T1 (hr) 2017-02-24

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ID=43527590

Family Applications (2)

Application Number Title Priority Date Filing Date
HRP20161614TT HRP20161614T1 (hr) 2009-07-29 2016-12-01 Terapijska sredstva za smanjenje razina paratiroidnog hormona
HRP20190923TT HRP20190923T1 (hr) 2009-07-29 2019-05-17 Terapijska sredstva za smanjenje razina paratirodnog hormona

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HRP20190923TT HRP20190923T1 (hr) 2009-07-29 2019-05-17 Terapijska sredstva za smanjenje razina paratirodnog hormona

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US (10) US8999932B2 (hr)
EP (5) EP4154900A1 (hr)
JP (3) JP5270799B2 (hr)
KR (1) KR101781841B1 (hr)
CN (2) CN107674114B (hr)
AU (1) AU2010278897B2 (hr)
BR (1) BR112012002143B8 (hr)
CA (1) CA2769525C (hr)
CY (3) CY1118388T1 (hr)
DK (2) DK2459208T3 (hr)
ES (2) ES2607954T3 (hr)
FR (1) FR17C1009I2 (hr)
HK (1) HK1167108A1 (hr)
HR (2) HRP20161614T1 (hr)
HU (3) HUE030960T2 (hr)
IL (1) IL217749A (hr)
LT (3) LT3192520T (hr)
LU (1) LUC00008I2 (hr)
MX (1) MX2012001213A (hr)
NO (1) NO2017021I1 (hr)
NZ (1) NZ597922A (hr)
PL (2) PL2459208T3 (hr)
PT (2) PT3192520T (hr)
RU (1) RU2557654C3 (hr)
SG (2) SG10201406921SA (hr)
SI (2) SI2459208T1 (hr)
SM (1) SMT201700014B (hr)
TW (1) TWI520744B (hr)
WO (1) WO2011014707A2 (hr)
ZA (1) ZA201200726B (hr)

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