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DK2041068T3 - Positivt ladede, vandopløselige prodrugs af ibuprofen med meget hurtig hudpenetrationshastighed - Google Patents

Positivt ladede, vandopløselige prodrugs af ibuprofen med meget hurtig hudpenetrationshastighed Download PDF

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DK2041068T3
DK2041068T3 DK06780126.6T DK06780126T DK2041068T3 DK 2041068 T3 DK2041068 T3 DK 2041068T3 DK 06780126 T DK06780126 T DK 06780126T DK 2041068 T3 DK2041068 T3 DK 2041068T3
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ibuprofen
composition
compound
alkyloxy
alkenyl
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DK06780126.6T
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Chongxi Yu
Lina Xu
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Techfields Biochem Co Ltd
Chongxi Yu
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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C233/00—Carboxylic acid amides
    • C07C233/01—Carboxylic acid amides having carbon atoms of carboxamide groups bound to hydrogen atoms or to acyclic carbon atoms
    • C07C233/34—Carboxylic acid amides having carbon atoms of carboxamide groups bound to hydrogen atoms or to acyclic carbon atoms having the nitrogen atom of at least one of the carboxamide groups bound to a carbon atom of a hydrocarbon radical substituted by amino groups
    • C07C233/35—Carboxylic acid amides having carbon atoms of carboxamide groups bound to hydrogen atoms or to acyclic carbon atoms having the nitrogen atom of at least one of the carboxamide groups bound to a carbon atom of a hydrocarbon radical substituted by amino groups with the substituted hydrocarbon radical bound to the nitrogen atom of the carboxamide group by an acyclic carbon atom
    • C07C233/40—Carboxylic acid amides having carbon atoms of carboxamide groups bound to hydrogen atoms or to acyclic carbon atoms having the nitrogen atom of at least one of the carboxamide groups bound to a carbon atom of a hydrocarbon radical substituted by amino groups with the substituted hydrocarbon radical bound to the nitrogen atom of the carboxamide group by an acyclic carbon atom having the carbon atom of the carboxamide group bound to an acyclic carbon atom of a carbon skeleton containing six-membered aromatic rings
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00—Drugs for disorders of the respiratory system
    • A61P11/06—Antiasthmatics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P15/00—Drugs for genital or sexual disorders; Contraceptives
    • 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
    • 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
    • A61P17/10—Anti-acne agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00—Drugs for skeletal disorders
    • A61P19/02—Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
    • 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
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/06—Antimigraine agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P27/00—Drugs for disorders of the senses
    • A61P27/02—Ophthalmic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P27/00—Drugs for disorders of the senses
    • A61P27/02—Ophthalmic agents
    • A61P27/06—Antiglaucoma agents or miotics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P27/00—Drugs for disorders of the senses
    • A61P27/02—Ophthalmic agents
    • A61P27/14—Decongestants or antiallergics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P27/00—Drugs for disorders of the senses
    • A61P27/16—Otologicals
    • 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]
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C211/00—Compounds containing amino groups bound to a carbon skeleton
    • C07C211/62—Quaternary ammonium compounds
    • C07C211/63—Quaternary ammonium compounds having quaternised nitrogen atoms bound to acyclic carbon atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C327/00—Thiocarboxylic acids
    • C07C327/20—Esters of monothiocarboxylic acids
    • C07C327/30—Esters of monothiocarboxylic acids having sulfur atoms of esterified thiocarboxyl groups bound to carbon atoms of hydrocarbon radicals substituted by nitrogen atoms, not being part of nitro or nitroso groups

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • General Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
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  • Veterinary Medicine (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Ophthalmology & Optometry (AREA)
  • Pain & Pain Management (AREA)
  • Dermatology (AREA)
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  • Neurosurgery (AREA)
  • Rheumatology (AREA)
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  • Orthopedic Medicine & Surgery (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Immunology (AREA)
  • Reproductive Health (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
  • Medicinal Preparation (AREA)

Claims (16)

1. Forbindelser med strukturen 1
i struktur 1 repræsenterer Ri H, én af en hvilken som helst alkyl, alkyloxy, alkenyl, eller alkynylrester med op til 12 carbonatomer, eller arylrester; R2 repræsenterer H, én af en hvilken som helst alkyl, alkyloxy, alkenyl eller alkynylrester med op til 12 carbonatomer, eller arylrester; R3 repræsenterer Η; X repræsenterer S; A' repræsenterer en hvilken som helst negativ ion; og n= 0, 1, 2, 3, 4, 5, 6, 7, 8, 9 eller 10.
2. Fremgangsmåde til fremstilling af forbindelser ifølge krav 1, hvor syrehalogenider eller blandede anhydrider af struktur 2 er omsat med forbindelser med strukturen 3, hvor
i struktur 2 Y repræsenterer halogen, alkoxycarbonyl eller substitueret aryloxy-carbonyloxy, og hvor
i struktur 3 Ri repræsenterer H, én af en hvilken som helst alkyl, alkyloxy, alkenyl, eller alkynylrester med op til 12 carbonatomer, eller arylrester; R2 repræsenterer H, én af en hvilken som helst alkyl, alkyloxy, alkenyl eller alkynylrester med op til 12 carbonatomer eller arylrester; X repræsenterer S; og n=0, 1, 2, 3, 4, 5, 6, 7, 8, 9 eller 10.
3. Fremgangsmåde til fremstilling af forbindelser ifølge krav 1, hvor forbindelserne er fremstillet af ibuprofen ved omsætning med forbindelser med strukturen 3 ved anvendelse af koblingsreagenser, hvor
i struktur 3 Ri repræsenterer H, én af en hvilken som helst alkyl, alkyloxy, alkenyl, eller alkynylrester med op til 12 carbonatomer, eller arylrester; R2 repræsenterer H, én af en hvilken som helst alkyl, alkyloxy, alkenyl eller alkynylrester med op til 12 carbonatomer, eller arylrester; X repræsenterer S; og n=0, 1, 2, 3, 4, 5, 6, 7, 8, 9 eller 10, og koblingsreagenset er udvalgt fra N,N'-dicyclohexylcarbodiimid, N, N'-diisopropylcarbodiimid, 0-(benzotriazol-1 -yl)-N,N,N',N'-tetramethyluroniumtetrafluorborat, O-(benzotriazol-1 -yl)-N,N,N',N’-tetramethyluroniumhexafluorphosphat og benzotriazol-1 -yl-oxy-tris (dimethylamino)phosphoniumhexafluorphosphat.
4. Forbindelse ifølge lerav 1 eller sammensætning, der mindst omfatter én forbindelse ifølge krav 1 som en aktiv ingrediens til anvendelse i behandlingen af en hvilken som helst tilstand, der kan behandles med ibuprofen, hos mennesker eller dyr, hvor forbindelsen eller sammensætningen administreres oralt, hvor de tilstande, der kan behandles med ibuprofen, er udvalgt fra gruppen indbefattende tandpine, hovedpine, akut migrænehovedpine, smerte of arthritis, inflammatorisk smerte, dysmenorrhoe, feber, cancer, Bartters syndrom, anterior og posterior kronisk uveitis, IUD-associeret uterusblødning, kvalme, radiation-induceret opkastning, diabetisk neuropati, hæmofil arthropati, knogletab og solskoldning.
5. Forbindelser med strukturen 1
i struktur 1 repræsenterer Ri H, én af en hvilken som helst alkyl, alkyloxy, alkenyl, eller alkynylrester med op til 12 carbonatomer, eller arylrester; R2 repræsenterer H, én af en hvilken som helst alkyl, alkyloxy, alkenyl eller alkynylrester med op til 12 carbonatomer, eller arylrester; R3 repræsenterer Η; X repræsenterer O eller S; A' repræsenterer en hvilken som helst negativ ion; og n= 0, 1, 2, 3, 4, 5, 6, 7, 8, 9 eller 10, eller sammensætning, der mindst omfatter én forbindelse med struktur 1 som en aktiv ingrediens til anvendelse i behandlingen af en hvilken som helst tilstand, der kan behandles med ibuprofen, hos mennesker eller dyr, hvor forbindelsen eller sammensætningen administreres transdermalt, hvor de tilstande, der kan behandles med ibuprofen, er udvalgt fra gruppen indbefattende tandpine, hovedpine, akut migrænehovedpine, smerte ved arthritis, inflammatorisk smerte, dysmenorrhoe, feber, cancer, Bartters syndrom, anterior og posterior kronisk uveitis, IUD-associeret uterusblødning, kvalme, radiation-induceret opkastning, diabetisk neuropati, hæmofil arthropati, knogletab og solskoldning.
6. Forbindelse eller sammensætning til anvendelse ifølge krav 5, hvor forbindelsen eller sammensætningen er i form af en opløsning, spray, lotion, salve, emulsion eller gel, og administreres transdermalt til en hvilken som helst del af kroppen for at afgive terapeutisk effektive plasmaniveauer.
7. Forbindelse ifølge krav 1 eller sammensætning, der omfatter mindst én forbindelse ifølge krav 1 som en aktiv ingrediens til anvendelse i behandlingen af smerte, hvor forbindelsen eller sammensætningen administreres topisk på det betændte område i en terapeutisk effektiv mængde.
8. Forbindelse eller sammensætning til anvendelse ifølge krav 7, hvor smerten er hovedpine, tandpine og muskelsmerte og arthritis og anden inflammatorisk smerte.
9. Forbindelse ifølge krav 1 eller sammensætning, der omfatter mindst én forbindelse ifølge krav 1 som en aktiv ingrediens til anvendelse i behandlingen af acne, solskoldning eller andre hudforstyrrelser, og hvor forbindelsen eller sammensætningen er i form af en opløsning, spray, lotion, salve, emulsion eller gel.
10. Forbindelser med strukturen 1
i struktur 1, Ri repræsenterer H, én af en hvilken som helst alkyl, alkyloxy, alkenyl, eller alkynylrester med op til 12 carbonatomer, eller arylrester; R2 repræsenterer H, én af en hvilken som helst alkyl, alkyloxy, alkenyl eller alkynylrester med op til 12 carbonatomer, eller arylrester; R3 repræsenterer Η; X repræsenterer O eller S; A" repræsenterer en hvilken som helst negativ ion; og 11= 0, 1, 2, 3, 4, 5, 6, 7, 8, 9 eller 10, eller sammensætning, der mindst omfatter én forbindelse med struktur 1 som en aktiv ingrediens til anvendelse i behandlingen af acne, solskoldning eller andre hudforstyrrelser, hvor forbindelsen eller sammensætningen er i form af en opløsning, spray, lotion, salve, emulsion eller gel, og hvor forbindelse eller sammensætning administreres transdermalt.
11. Forbindelse ifølge krav 1 eller sammensætning, der mindst omfatter én forbindelse ifølge krav 1 som en aktiv ingrediens til anvendelse i behandlingen af astma, hvor forbindelsen eller sammensætningen administreres ved spraying gennem munden eller næsten eller andre kropsdele.
12. Forbindelse ifølge krav 1 eller sammensætning, der mindst omfatter én forbindelse ifølge krav 1 som en aktiv ingrediens til anvendelse i behandlingen af en hvilken som helst inflammatorisk øjensygdom, ocular smerte efter homhindeoperation, glaukom eller inflammatorisk øre- og/eller smertefuld tilstand hos mennesker eller dyr.
13. Forbindelse eller sammensætning til anvendelse ifølge krav 12, hvor den inflammatoriske øre-og/'eller smertefulde tilstand er otitis.
14. Transdermale, terapeutiske anvendelsessystemer for forbindelser med strukturen 1
i struktur 1 repræsenterer Ri H, én af en hvilken som helst alkyl, alkyloxy, alkenyl, eller alkynylrester med op til 12 carbonatomer, eller arylrester; R2 repræsenterer H, én af en hvilken som helst alkyl, alkyloxy, alkenyl eller alkynylrester med op til 12 carbonatomer, eller arylrester; R3 repræsenterer Η; X repræsenterer O eller S; A" repræsenterer en hvilken som helst negativ ion; og n= 0, 1, 2, 3, 4, 5, 6, 7, 8, 9 eller 10, eller sammensætning, der mindst omfatter én forbindelse med struktur 1 som en aktiv ingrediens til anvendelse i behandlingen af en hvilken som helst tilstand, der kan behandles med ibuprofen, hos mennesker eller dyr, hvor transdermale, terapeutiske anvendelsessystemer gør det muligt for ibuprofen konstant at nå optimale terapeutiske blodnivcaucr for at øge effektivitet og reducere bivirkningerne af ibuprofen, hvor de tilstande, der kan behandles med ibuprofen, er udvalgt fra gruppen indbefattende tandpine, hovedpine, akut migrænehovedpine, arthritissmerte, inflammatorisk smerte, dysmenorrhoe, feber, cancer, Bartters syndrom, anterior og posterior kronisk uveitis, IUD-associeret uterusblødning, kvalme, radiation-induceret opkastning, diabetisk neuropati, hæmofil arthropati, knoglctab og solskoldning.
15. Transdermale, terapeutiske anvendelsessystemer ifølge krav 14, kendetegnet ved, at disse systemer er en bandage eller et patch, der omfatter ét aktivt stofholdigt matrixlag og et impermeabelt bagsidelag.
16. Transdermale, terapeutiske anvendelsessystemer ifølge krav 14-15, kendetegnet ved, at systemet har en beholder til aktivt stof, der har en permeabel bund, der vender ind mod huden.
DK06780126.6T 2006-07-18 2006-07-18 Positivt ladede, vandopløselige prodrugs af ibuprofen med meget hurtig hudpenetrationshastighed DK2041068T3 (da)

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PCT/IB2006/052461 WO2008010025A1 (en) 2006-07-18 2006-07-18 Positively charged water-soluble prodrugs of ibuprofen with very fast skin penetration rate

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EP (2) EP2041068B1 (da)
JP (1) JP5144658B2 (da)
CN (1) CN101489985B (da)
AU (1) AU2006346288A1 (da)
CA (1) CA2657636C (da)
DK (1) DK2041068T3 (da)
ES (1) ES2616315T3 (da)
HU (1) HUE033687T2 (da)
PL (1) PL2041068T3 (da)
PT (1) PT2041068T (da)
WO (1) WO2008010025A1 (da)

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EP3210964A1 (en) 2017-08-30
EP2041068B1 (en) 2017-01-25
CN101489985B (zh) 2014-01-08
HUE033687T2 (en) 2017-12-28
JP2009543857A (ja) 2009-12-10
ES2616315T3 (es) 2017-06-12
CA2657636C (en) 2021-11-09
EP2041068A4 (en) 2010-09-29
AU2006346288A1 (en) 2008-01-24
WO2008010025A1 (en) 2008-01-24
EP2041068A1 (en) 2009-04-01
HK1135958A1 (en) 2010-06-18
JP5144658B2 (ja) 2013-02-13
CA2657636A1 (en) 2008-01-24
CN101489985A (zh) 2009-07-22
PT2041068T (pt) 2017-02-17

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