SI2459176T1 - Kristalizacijski postopek in biološka uporabnost - Google Patents

Kristalizacijski postopek in biološka uporabnost Download PDF

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Publication number
SI2459176T1
SI2459176T1 SI201031592T SI201031592T SI2459176T1 SI 2459176 T1 SI2459176 T1 SI 2459176T1 SI 201031592 T SI201031592 T SI 201031592T SI 201031592 T SI201031592 T SI 201031592T SI 2459176 T1 SI2459176 T1 SI 2459176T1
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complex
lysine
zoledronic acid
crystalline
water
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SI201031592T
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English (en)
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Mazen Hanna
Ning Shan
Miranda Cheney
David Weyna
Raymond K. Houck
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Gruenenthal Gmbh
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    • 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
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    • A61K31/365Lactones
    • A61K31/375Ascorbic acid, i.e. vitamin C; Salts thereof
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    • 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
    • A61K47/62Medicinal 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
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    • A61P19/00Drugs for skeletal disorders
    • A61P19/08Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease
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    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00Drugs for skeletal disorders
    • A61P19/08Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease
    • A61P19/10Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease for osteoporosis
    • 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
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    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
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    • A61P35/00Antineoplastic agents
    • A61P35/04Antineoplastic agents specific for metastasis
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    • A61P37/00Drugs for immunological or allergic disorders
    • A61P37/02Immunomodulators
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    • AHUMAN NECESSITIES
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    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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    • AHUMAN NECESSITIES
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    • C07ORGANIC CHEMISTRY
    • C07FACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
    • C07F9/00Compounds containing elements of Groups 5 or 15 of the Periodic Table
    • C07F9/02Phosphorus compounds
    • C07F9/547Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom
    • C07F9/645Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom having two nitrogen atoms as the only ring hetero atoms
    • C07F9/6503Five-membered rings
    • C07F9/6506Five-membered rings having the nitrogen atoms in positions 1 and 3
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    • C07ORGANIC CHEMISTRY
    • C07BGENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
    • C07B2200/00Indexing scheme relating to specific properties of organic compounds
    • C07B2200/13Crystalline forms, e.g. polymorphs

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  • Health & Medical Sciences (AREA)
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  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
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  • Pyridine Compounds (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
  • Preparation Of Compounds By Using Micro-Organisms (AREA)

Claims (10)

  1. Kristalizacij ski postopek in biološka uporabnost Patentni zahtevki
    1. Kristaliničen molekulski kompleks, ki obsega zoledronsko kislino ali njeno sol in sotvorca, izbranega izmed lizina ali glicina.
  2. 2. Molekulski kompleks, izbran iz skupine, ki jo sestavljajo: kompleks kristalinične zoledronske kisline, vode in L-lizina; kompleks kristalinične zoledronske kisline, vode in DL-lizina; kompleks kristalinične zoledronske kisline, vode in glicina; kompleks kristalinične zoledronske kisline, L-lizina in vode, označen z rentgenskim praškovnim difrakcijskim vzorcem, ki ima vrhove pri 2Θ ~ (9,0, 14,4, 18,1, 26,0 in 29,6)° ± 0,2°; kompleks kristalinične zoledronske kisline, L-lizina in vode, označen z rentgenskim praškovnim difrakcijskim vzorcem, ki ima vrhove pri 2Θ ~ (9,6, 10,7, 14,3, 21,4, 23,5)° ± 0,2°; kompleks kristalinične zoledronske kisline, DL-lizina in vode, označen z rentgenskim praškovnim difrakcijskim vzorcem, ki ima vrhove pri 2Θ ~ (8,3, 11,8, 12,3, 15,8 in 20,8)° ± 0,2°; kompleks kristalinične zoledronske kisline, DL-lizina in vode, označen z rentgenskim praškovnim difrakcijskim vzorcem, ki ima vrhove pri 2Θ « (9,1, 14,7, 18,0, 21,2 in 26,0)° ± 0,2°; kompleks kristalinične zoledronske kisline in glicina, označen z rentgenskim praškovnim difrakcijskim vzorcem, ki ima vrhove pri 2Θ ~ (10,2, 17,8, 19,9, 22,9 in 28,1)° ±0,2°; kompleks kristalinične zoledronske kisline, DL-lizina in vode, označen z rentgenskim praškovnim difrakcijskim vzorcem, ki ima vrhove pri 2Θ ~ (9,7, 10,8, 14,4, 18,9, 21,4)° ±0,2°; kompleks kristalinične zoledronske kisline, DL-lizina, etanola in vode, označen z rentgenskim praškovnim difrakcijskim vzorcem, ki ima vrhove pri 2Θ ~ (8,8, 9,7, 17,6, 23,1 in 26,5)° ±0,2°; kadar zberemo rentgenske praškovne difrakcijske vzorce v območju kota 2Θ 3-40° z uporabo sevanja Cu Κα z λ = 1,540562 A.
  3. 3. Sestavek, ki obsega kristalinični molekulski kompleks, ki obsega zoledronsko kislino ali njeno sol in lizin po zahtevku 1 ali 2 ter prebitno količino lizina, glicina ali njunih zmesi, prednostno prebitno količino lizina.
  4. 4. Sestavek, ki obsega kristalinični molekulski kompleks, ki obsega zoledronsko kislino ali njeno sol in glicin po zahtevku 1 ali 2 ter prebitno količino glicina, lizina ali njunih zmesi, prednostno prebitno količino glicina.
  5. 5. Farmacevtski sestavek, ki obsega kristalinični molekulski kompleks po zahtevku 1 ali 2 ali sestavek po zahtevku 3 ali 4 in farmacevtsko sprejemljiv ekscipient.
  6. 6. Farmacevtski sestavek po zahtevku 5, kjer je sestavek peroralna trdna odmema oblika.
  7. 7. Farmacevtski sestavek po zahtevku 6, kjer je sestavek peroralna odmema oblika izbrana izmed tablete, kapsule in tekoče suspenzije trdnega molekulskega kompleksa.
  8. 8. Molekulski kompleks po zahtevku 1 ali 2, sestavek po zahtevku 4 ali 5 ali farmacevtski sestavek po katerem koli od zahtevkov 6-8 za uporabo kot zdravilo.
  9. 9. Molekulski kompleks po zahtevku 1 ali 2, sestavek po zahtevku 3 ali 4 ali farmacevtski sestavek po katerem koli od zahtevkov 5-6 za uporabo pri zdravljenju in/ali preprečevanju bolezenskih stanj, povezanih z osteoporozo, hiperkalciemijo, kostnimi metastazami, induciranimi z rakom, Pagetove bolezni ali adjuvantnih ali neoadjuvantnih terapij pri raku.
  10. 10. Molekulski kompleks po zahtevku 1 ali 2, sestavek po zahtevku 3 ali 4 ali farmacevtski sestavek po katerem koli od zahtevkov 5-7 za uporabo pri povečevanju biološke uporabnosti ali permeabilnosti zoledronske kisline ali njene soli pri pacientu, ki to potrebuje.
SI201031592T 2009-07-31 2010-07-30 Kristalizacijski postopek in biološka uporabnost SI2459176T1 (sl)

Applications Claiming Priority (8)

Application Number Priority Date Filing Date Title
US23022209P 2009-07-31 2009-07-31
US28803609P 2009-12-18 2009-12-18
US30211010P 2010-02-06 2010-02-06
US31287910P 2010-03-11 2010-03-11
US31850310P 2010-03-29 2010-03-29
US35954410P 2010-06-29 2010-06-29
PCT/US2010/043892 WO2011014766A2 (en) 2009-07-31 2010-07-30 Crystallization method and bioavailability
EP10805109.5A EP2459176B1 (en) 2009-07-31 2010-07-30 Crystallization method and bioavailability

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EP (2) EP2459176B1 (sl)
JP (1) JP5852569B2 (sl)
KR (1) KR101813728B1 (sl)
CN (1) CN102573809B (sl)
AU (2) AU2010278860B2 (sl)
CA (1) CA2769633C (sl)
CY (1) CY1121952T1 (sl)
DK (1) DK2459176T3 (sl)
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HR (1) HRP20171755T1 (sl)
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IL (1) IL217828B (sl)
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NO (1) NO2459176T3 (sl)
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