DK1436012T3 - Polymerkonjugater af opioidantagonister - Google Patents

Polymerkonjugater af opioidantagonister Download PDF

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Publication number
DK1436012T3
DK1436012T3 DK02795531.9T DK02795531T DK1436012T3 DK 1436012 T3 DK1436012 T3 DK 1436012T3 DK 02795531 T DK02795531 T DK 02795531T DK 1436012 T3 DK1436012 T3 DK 1436012T3
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Denmark
Prior art keywords
polymer
pharmaceutical composition
opioid
conjugate
group
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DK02795531.9T
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English (en)
Inventor
Michael David Bentley
Michael James Roberts
Xiaoming Shen
Lin Cheng
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Nektar Therapeutics
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Publication of DK1436012T3 publication Critical patent/DK1436012T3/da

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    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/47—Quinolines; Isoquinolines
    • A61K31/485—Morphinan derivatives, e.g. morphine, codeine
    • 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
    • A61K47/56—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 an organic macromolecular compound, e.g. an oligomeric, polymeric or dendrimeric molecule
    • A61K47/59—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 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
    • A61K47/60—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 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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/08—Drugs for disorders of the alimentary tract or the digestive system for nausea, cinetosis or vertigo; Antiemetics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/10—Laxatives
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00—Drugs for dermatological disorders
    • A61P17/04—Antipruritics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/02—Drugs for disorders of the nervous system for peripheral neuropathies
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/04—Centrally acting analgesics, e.g. opioids
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]

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  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
  • Veterinary Medicine (AREA)
  • Chemical & Material Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Medicinal Chemistry (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Organic Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Epidemiology (AREA)
  • Neurosurgery (AREA)
  • Pain & Pain Management (AREA)
  • Neurology (AREA)
  • Biomedical Technology (AREA)
  • Dermatology (AREA)
  • Hospice & Palliative Care (AREA)
  • Rheumatology (AREA)
  • Otolaryngology (AREA)
  • Emergency Medicine (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Medicinal Preparation (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)

Claims (14)

1. Farmaceutisk sammensætning omfattende: et polymerkonjugat, eller et farmaceutisk acceptabelt salt deraf, omfattende en poly(ethylenglycol)polymer kovalent bundet til en opioidantagonist, hvori polymerens molekylevægt er mindre end 2000 Da, og en farmaceutisk acceptabel bærer, hvori polymerkonjugatet har strukturen hvori:
POLY er poly(ethylenglycol)polymeren X er en hydrolytisk stabil binding; Y er allyl; Z er H eller OH; og den stiplede linje repræsenterer en valgfri dobbeltbinding.
2. Farmaceutisk sammensætning ifølge krav 1, hvor opioidantagonisten er naloxon.
3. Farmaceutisk sammensætning ifølge krav 1, hvori den hydrolytisk stabile binding er valgt fra gruppen bestående af amid, amin, carbamat, ether, thioether og urinstof.
4. Farmaceutisk sammensætning ifølge krav 1, hvori polymerens molekylvægt er mindre end ca. 1000 Da.
5. Farmaceutisk sammensætning ifølge krav 1, hvori polymerens molekylvægt er mindre end ca. 800 Da.
6. Farmaceutisk sammensætning ifølge krav 1, hvori X er -NH-(CHR0)m-O- eller -NH-C(O)-(CHR0)m-O-, m eller n er 1-12 og hver Ro uafhængigt er H eller CrCe alkyl.
7. Farmaceutisk sammensætning ifølge krav 1, hvori X er et heteroatom.
8. Farmaceutisk sammensætning ifølge krav 1, der yderligere omfatter en opioidagonist.
9. Farmaceutisk sammensætning ifølge krav 8, hvori opioidagonisten er valgt fra gruppen bestående af alfentanil, bremazocin, buprenorphin, butorphanol, kodein, cyclazocin, dezocin, diacetylmorfin, dihydrokodein, fentanyl, hydrocodon, hydromorphon, levorphanol, meperidin (pethidin), methadon, morfin, nalbuphin, noscapin, oxycodon, oxymorphon, papaverin, pentazocin, pethidin, phenazocin, propiram, propoxyphen, sufentanil, thebain og tramadol.
10. Farmaceutisk sammensætning ifølge krav 1 til anvendelse til behandling af en bivirkning resulterende fra administrationen af en opioidagonist til et pattedyr.
11. Farmaceutisk sammensætning ifølge krav 10, hvori bivirkningen er valgt fra gruppen bestående af kvalme, forstoppelse og pruritus.
12. Farmaceutisk sammensætning ifølge krav 10, hvori den farmaceutiske sammensætning administreres oralt.
13. Farmaceutisk sammensætning ifølge krav 10, hvori den farmaceutiske sammensætning administreres sammen med opioidagonisten.
14. Farmaceutisk sammensætning ifølge krav 13, hvori polymerkonjugatet og opioidagonisten er formuleret i en enkelt doseringsenhed.
DK02795531.9T 2001-10-18 2002-10-18 Polymerkonjugater af opioidantagonister DK1436012T3 (da)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US33040001P 2001-10-18 2001-10-18
PCT/US2002/033325 WO2003032990A2 (en) 2001-10-18 2002-10-18 Polymer conjugates of opioid antagonists

Publications (1)

Publication Number Publication Date
DK1436012T3 true DK1436012T3 (da) 2018-01-22

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DK15172363.2T DK2939696T3 (da) 2001-10-18 2002-10-18 Polymerkonjugater af opioidantagonister
DK02795531.9T DK1436012T3 (da) 2001-10-18 2002-10-18 Polymerkonjugater af opioidantagonister

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Country Status (15)

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US (4) US7056500B2 (da)
EP (3) EP2939696B1 (da)
JP (2) JP4814488B2 (da)
KR (2) KR101009309B1 (da)
AU (1) AU2002360284B2 (da)
CA (1) CA2463938C (da)
CY (1) CY1119906T1 (da)
DK (2) DK2939696T3 (da)
ES (2) ES2569262T3 (da)
HK (1) HK1215171A1 (da)
LT (1) LT1436012T (da)
MX (1) MXPA04003597A (da)
PT (2) PT2939696E (da)
SI (2) SI1436012T1 (da)
WO (1) WO2003032990A2 (da)

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