DK2939696T3 - Polymerkonjugater af opioidantagonister - Google Patents
Polymerkonjugater af opioidantagonister Download PDFInfo
- Publication number
- DK2939696T3 DK2939696T3 DK15172363.2T DK15172363T DK2939696T3 DK 2939696 T3 DK2939696 T3 DK 2939696T3 DK 15172363 T DK15172363 T DK 15172363T DK 2939696 T3 DK2939696 T3 DK 2939696T3
- Authority
- DK
- Denmark
- Prior art keywords
- polymer
- opioid
- polymer conjugate
- conjugate
- formula
- Prior art date
Links
- 229920000642 polymer Polymers 0.000 title claims description 159
- 239000003887 narcotic antagonist Substances 0.000 title description 12
- -1 bremazocin Chemical compound 0.000 claims description 52
- RTZKZFJDLAIYFH-UHFFFAOYSA-N Diethyl ether Chemical compound CCOCC RTZKZFJDLAIYFH-UHFFFAOYSA-N 0.000 claims description 32
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- 150000003839 salts Chemical class 0.000 claims description 20
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Classifications
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- 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
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- A—HUMAN NECESSITIES
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- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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- A—HUMAN NECESSITIES
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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- A61P25/02—Drugs for disorders of the nervous system for peripheral neuropathies
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- A—HUMAN NECESSITIES
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- 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
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- A—HUMAN NECESSITIES
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- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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- Bioinformatics & Cheminformatics (AREA)
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- Pain & Pain Management (AREA)
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- Rheumatology (AREA)
- Hospice & Palliative Care (AREA)
- Otolaryngology (AREA)
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- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
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- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
Claims (11)
1. Polymerkonjugat ifølge formlen:
eller farmaceutisk acceptabelt salt deraf, hvori: Y er allyl; Z er OH; X er en binding valgt blandt amid, amin, carbamat, ether, thioether eller urea; og POLY har formlen CH3O- (CH2CH20)n- CH2CH2- hvori n er fra 2 til 45.
2. Farmaceutisk sammensætning omfattende et polymerkonjugat og en farmaceutisk acceptabel bærer, hvori polymerkonjugatet har formlen:
eller farmaceutisk acceptabelt salt deraf, hvori: Y er allyl; Z er OH; X er en binding valgt blandt amid, amin, carbamat, ether, thioether eller urea; og POLY har formlen CH3O- (CH2CH20)n- CH2CH2- hvori n er fra 2 til 45.
3. Polymerkonjugat eller farmaceutisk sammensætning ifølge krav 1 eller krav 2, hvori n er fra 2 til 20.
4. Polymerkonjugat ifølge krav 1 eller farmaceutisk sammensætning ifølge krav 2, hvori POLY har en molekylvægt på fra 100 Da til 500 Da.
5. Farmaceutisk sammensætning omfattende et polymerkonjugat; en opioidagonist; og en farmaceutisk acceptabel bærer, hvori polymerkonjugatet har formlen:
eller farmaceutisk acceptabelt salt deraf, hvori: Y er allyl; Z er OH; X er en binding valgt blandt amid, amin, carbamat, ether, thioether eller urea; og POLY har formlen CH30- (CH2CH20)n- CH2CH2- hvori n er fra 2 til 45.
6. Farmaceutisk sammensætning ifølge krav 5, 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, phenazocin, propiram, propoxyphen, sufentanil, thebain og tramadol.
7. Polymerkonjugat til anvendelse i behandlingen af forstoppelse som følge af indgivelse af en opioidagonist, hvori polymerkonjugatet har formlen:
eller farmaceutisk acceptabelt salt deraf, hvori: Y er allyl; Z er OH; X er en binding valgt blandt amid, amin, carbamat, ether, thioether eller urea; og POLY har formlen CH3O- (CH2CH20)n- CH2CH2- hvori n er fra 2 til 45.
8. Polymerkonjugat til anvendelse i behandlingen af kvalme som følge af indgivelse af en opioidagonist, hvori polymerkonjugatet har formlen:
eller farmaceutisk acceptabelt salt deraf, hvori: Y er allyl; Z er OH; X er en binding valgt blandt amid, amin, carbamat, ether, thioether eller urea; og POLY har formlen CH3O- (CH2CH2O) n- CH2CH2- hvori n er fra 2 til 45.
9. Polymerkonjugat til anvendelse i behandlingen af pruritus som følge af indgivelse af en opioidagonist, hvori polymerkonjugatet har formlen:
eller farmaceutisk acceptabelt salt deraf, hvori: Y er allyl; Z er OH; X er en binding valgt blandt amid, amin, carbamat, ether, thioether eller urea; og POLY har formlen CH3O- (CH2CH20)nCH2CH2- hvori n er fra 2 til 45.
10. Polymerkonjugat til anvendelse ifølge krav 5, 7, 8 eller 9, hvori n er fra 2 til 20.
11. Polymerkonjugat til anvendelse ifølge krav 5, 7, 8 eller 9, hvori POLY har en molekylevægt på fra 100 Da til 500 Da.
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US33040001P | 2001-10-18 | 2001-10-18 | |
| EP02795531.9A EP1436012B1 (en) | 2001-10-18 | 2002-10-18 | Polymer conjugates of opioid antagonists |
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| Publication Number | Publication Date |
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| DK2939696T3 true DK2939696T3 (da) | 2016-05-23 |
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| DK02795531.9T DK1436012T3 (da) | 2001-10-18 | 2002-10-18 | Polymerkonjugater af opioidantagonister |
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| DK02795531.9T DK1436012T3 (da) | 2001-10-18 | 2002-10-18 | Polymerkonjugater af opioidantagonister |
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| EP (3) | EP2236161A1 (da) |
| JP (2) | JP4814488B2 (da) |
| KR (2) | KR100974842B1 (da) |
| AU (1) | AU2002360284B2 (da) |
| CA (1) | CA2463938C (da) |
| CY (1) | CY1119906T1 (da) |
| DK (2) | DK2939696T3 (da) |
| ES (2) | ES2654819T3 (da) |
| HK (1) | HK1215171A1 (da) |
| LT (1) | LT1436012T (da) |
| MX (1) | MXPA04003597A (da) |
| PT (2) | PT2939696E (da) |
| SI (2) | SI2939696T1 (da) |
| WO (1) | WO2003032990A2 (da) |
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| US20030158220A1 (en) * | 1997-11-03 | 2003-08-21 | Foss Joseph F. | Use of methylnaltrexone and related compounds to treat chronic opioid use side effects |
| US6274591B1 (en) * | 1997-11-03 | 2001-08-14 | Joseph F. Foss | Use of methylnaltrexone and related compounds |
| MXPA02003176A (es) * | 1999-10-04 | 2002-09-30 | Shearwater Corp | Neuropeptidos estabilizados por polimero. |
| MXPA04003597A (es) | 2001-10-18 | 2004-07-30 | Nektar Therapeutics Al Corp | Conjugados polimericos de antagonistas opiaceos. |
| CA2840490C (en) * | 2002-01-18 | 2017-02-28 | Biogen Idec Ma Inc. | Polyalkylene glycol with moiety for conjugating biologically active compounds |
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2009
- 2009-04-30 JP JP2009111653A patent/JP5570137B2/ja not_active Expired - Lifetime
- 2009-10-06 US US12/574,335 patent/US8349307B2/en not_active Expired - Fee Related
-
2012
- 2012-11-29 US US13/689,640 patent/US8617530B2/en not_active Expired - Lifetime
-
2016
- 2016-03-17 HK HK16103153.9A patent/HK1215171A1/zh not_active IP Right Cessation
-
2018
- 2018-02-12 CY CY20181100170T patent/CY1119906T1/el unknown
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