DK2863921T3 - Polymer-nsaid-konjugat - Google Patents

Polymer-nsaid-konjugat Download PDF

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DK2863921T3
DK2863921T3 DK13809454.5T DK13809454T DK2863921T3 DK 2863921 T3 DK2863921 T3 DK 2863921T3 DK 13809454 T DK13809454 T DK 13809454T DK 2863921 T3 DK2863921 T3 DK 2863921T3
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polymer
nsaid
group
acid
conjugate
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Asha Marina D'souza
Andrew Craig Donohue
Russell John Tait
Adrian Sulistio
Florian Hans Maximilian Graichen
Sarah Man Yee Ng
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Polyactiva Pty Ltd
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    • 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
    • A61K47/593—Polyesters, e.g. PLGA or polylactide-co-glycolide
    • 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
    • A61K31/535—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one oxygen as the ring hetero atoms, e.g. 1,2-oxazines
    • A61K31/5375—1,4-Oxazines, e.g. morpholine
    • A61K31/5383—1,4-Oxazines, e.g. morpholine ortho- or peri-condensed with heterocyclic ring systems
    • 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
    • A61K31/185—Acids; Anhydrides, halides or salts thereof, e.g. sulfur acids, imidic, hydrazonic or hydroximic acids
    • A61K31/19—Carboxylic acids, e.g. valproic acid
    • A61K31/192—Carboxylic acids, e.g. valproic acid having aromatic groups, e.g. sulindac, 2-aryl-propionic acids, ethacrynic acid 
    • 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
    • A61K31/185—Acids; Anhydrides, halides or salts thereof, e.g. sulfur acids, imidic, hydrazonic or hydroximic acids
    • A61K31/19—Carboxylic acids, e.g. valproic acid
    • A61K31/195—Carboxylic acids, e.g. valproic acid having an amino group
    • A61K31/196—Carboxylic acids, e.g. valproic acid having an amino group the amino group being directly attached to a ring, e.g. anthranilic acid, mefenamic acid, diclofenac, chlorambucil
    • 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
    • A61K31/40—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil
    • A61K31/403—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil condensed with carbocyclic rings, e.g. carbazole
    • A61K31/404—Indoles, e.g. pindolol
    • A61K31/405—Indole-alkanecarboxylic acids; Derivatives thereof, e.g. tryptophan, indomethacin
    • 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
    • A61K31/40—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil
    • A61K31/407—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil condensed with other heterocyclic ring systems, e.g. ketorolac, physostigmine
    • A—HUMAN NECESSITIES
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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
    • A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
    • A61K31/415—1,2-Diazoles
    • A61K31/416—1,2-Diazoles condensed with carbocyclic ring systems, e.g. indazole
    • A—HUMAN NECESSITIES
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    • A—HUMAN NECESSITIES
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    • 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
    • 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
    • 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
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    • A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • A61P29/02—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID] without antiinflammatory effect
    • A—HUMAN NECESSITIES
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    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
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    • 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
    • A61K31/4738—Quinolines; Isoquinolines ortho- or peri-condensed with heterocyclic ring systems
    • A61K31/4745—Quinolines; Isoquinolines ortho- or peri-condensed with heterocyclic ring systems condensed with ring systems having nitrogen as a ring hetero atom, e.g. phenantrolines

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Claims (16)

1. Polymer-NSAID-konjugat, der omfatter en bionedbrydelig polymerhovedkæde og et ikke-steroidt antiinflammatorisk lægemiddel (NSAID), der er konjugeret i sidekæde til polymerhovedkæden via en arylesterbinding mellem en carboxylsyregruppe, der er til stede på NSAID’et, og en oxygenholdig substituent, der er til stede på en arylgruppe, der forbundet med polymerhovedkæden.
2. Polymer-NSAID-konjugat, der omfatter en bionedbrydelig polymerhovedkæde og et ikke-steroidt antiinflammatorisk lægemiddel (NSAID), der er konjugeret til polymerhovedkæden, hvor konjugatet omfatter som en del af dets polymerhovedkæde flere dele med formlen (I):
grupperne X, (Ar)n, O og D i delen med formlen (I) er i en sidekæde fra polymerhovedkæden; R er udvalgt fra gruppen bestående af en eventuelt substitueret alifatisk gruppe og en eventuelt substitueret aryl; X er en binding eller en linkergruppe; Ar er en eventuelt substitueret aryl; D er carboxylsyreresten af en ester dannet med et substitueret alkansyre-NSAID; og n er et heltal udvalgt fra 0 og 1, og når n er 0, er X en binding, forudsat, når R omfatter en eventuelt substitueret alifatisk gruppe, at n er 1, og når R omfatter en eventuelt substitueret aryl, at n er 0 eller 1.
3. Polymer-NSAID-konjugat ifølge krav 1 eller krav 2, hvor konjugatet omfatter som en del af dets polymerhovedkæde en del med formlen (II):
A og B, der kan være ens eller forskellige, hver repræsenterer en bionedbrydelig polymerhovedkæde og er (i) bundet til -Y-R(X-(Ar)n-0-D)-Y-delen som vist i formlen (II) via en bionedbrydelig del, og (ii) eventuelt, mindst én af A og B omfatter en hydrofil gruppe; R er udvalgt fra gruppen bestående af en eventuelt substitueret alifatisk gruppe og en eventuelt substitueret aryl; Y ved hver forekomst uafhængigt er udvalgt fra gruppen bestående af -O-, -C(O)-og -NRa-, hvor Ra er H eller CrC4-alkyl; X er en binding eller en linkergruppe; Ar er en eventuelt substitueret aryl; D er carboxylsyreresten af esteren dannet med et substitueret alkansyre-NSAID; og n er et heltal udvalgt fra 0 og 1, og når n er 0, så er X en binding, forudsat, når R omfatter en eventuelt substitueret alifatisk gruppe, at n er 1, og når R omfatter et eventuelt substitueret aryl, at n er 0 eller 1.
4. Polymer-NSAID-konjugat, der omfatter en bionedbrydelig polymerhovedkæde og et ikke-steroidt antiinflammatorisk lægemiddel (NSAID) konjugeret til polymerhovedkæden, hvor polymer-NSAID-konjugatet er opnået ved polymerising af et NSAID-monomerkonjugat med formlen (IV):
Y1 og Y2 hver uafhængigt repræsenterer en reaktiv funktionel gruppe, eller Y1 og Y2 sammen er en del af en cyklisk gruppe, der i stand til ringåbning; R2 er udvalgt fra gruppen bestående af en eventuelt substitueret alifatisk gruppe og en eventuelt substitueret aryl; X er en binding eller en linkergruppe; Ar er en eventuelt substitueret aryl; D er carboxylsyreresten af esteren dannet med et substitueret alkansyre-NSAID; og n er et heltal udvalgt fra 0 og 1, og når n er 0, er X en binding, forudsat, når R2 omfatter en eventuelt substitueret alifatisk gruppe, at n er 1, og når R2 omfatter en eventuelt substitueret aryl, at n er 0 eller 1; med mindst én monomer, der omfatter forenelig kemisk funktionalitet, eventuelt i nærvær af mindst én comonomer.
5. Polymer-NSAID-konjugat ifølge krav 4, hvor co-monomeren er til stede og omfatter en polymer- eller oligomerdel udvalgt fra gruppen bestående af poly(ethylenglycol), poly(mælkesyre-co-glycolsyre) (PLGA), poly(1,5-dioxepan-2-on) (PDOO), poly(glycerolacetat) (PGAc), poly(hydroxybutyrat), poly(glycerolphosphat), en aminosyrepolymer og en aminosyreoligomer.
6. Polymer-NSAID-konjugat ifølge et hvilket som helst af kravene 2 til 5, hvor n er 1 og X er en eventuelt substitueret linkergruppe, der omfatter en funktionel gruppe udvalgt fra gruppen bestående af -O-, -C(0)0-, -OC(O)-, -C(O)-, -0C(0)NH-, - NHC(0)0-, -0C6H40-, -0C(0)[CH2]n-, hvor n' = 1 til 5, -C(0)NRa-og -NRaC(0)-, hvor Ra er H eller Ci-C4-alkyl.
7. Polymer-lægemiddel ifølge et hvilket som helst af kravene 2 til 6, hvor gruppen -X-(Ar)n-0- er -0C(0)-C5-i2-aryl-0-.
8. Polymer-NSAID-konjugat ifølge krav 2, hvor delen af formlen (I) er:
9. Polymer-NSAID-konjugat ifølge krav 1 eller krav 2, hvor polymerhovedkæden omfatter en polymer udvalgt fra gruppen bestående af polyesterpolymerer, polyanhydridpolymerer, polycarbonatpolymerer, polyamidpolymerer, polyimidpolymerer, polyurethanpolymerer, polyureapolymerer, polysaccharider, polypeptider, copolymerer deraf og kombinationer deraf.
10. Polymer-NSAID-konjugat ifølge krav 3, hvor delen af formlen (II) har en struktur med formlen (Ile):
11. Polymer-NSAID-konjugat ifølge krav 3 eller krav 10, hvor A og B uafhængigt omfatter en polymer udvalgt fra gruppen bestående af polyurethaner, polyestere, poly(urethan-ethere), poly(ester-ethere), poly(urethan-estere) og poly(ester-urethaner).
12. Polymer-NSAID-konjugat ifølge et hvilket som helst af kravene 1 til 3, hvor konjugatet omfatter en hydrofil gruppe.
13. Polymer-NSAID-konjugat ifølge krav 12, hvor den hydrofile gruppe er inkorporeret i konjugatet (i) som en del af polymerhovedkæden, (ii) i en sidekædegruppe, der er kovalent bundet til og i en sidekæde fra polymerhovedkæden, eller (iii) kombinationer deraf.
14. Polymer-NSAID-konjugat ifølge krav 13, hvor den hydrofile gruppe omfatter mindst én udvalgt fra gruppen bestående af poly(ethylenglycol), poly(mælkesyre -co-glycolsyre) (PLGA), poly(1,5-dioxepan-2-on) (PDOO), poly(glycerolacetat) (PGAc), poly(hydroxybutyrat), poly(glycerolphosphat), en aminosyrepolymer (såsom polylysin, polyglutaminsyre), en aminosyreoligomer, dioler med lav molekylvægt (for eksempel C2-C4-dioler, såsom ethylenglycol, propandiol, propylenglycol, butandiol), trioler med lav molekylvægt (for eksempel glycerol), polyoler med lav molekylvægt (for eksempel mannitol, xylitol, sorbitol), aminosyrer (lysin, glutaminsyre), mælkesyre, glycolsyre, hydroxysyrer (for eksempel hydroxysmørsyre), 1,5-dioxepan-2-on, glycerolacetat, glycerolphosphat, eller kombinationer deraf, eller copolymerer deraf.
15. Polymer-NSAID-konjugat ifølge et hvilket som helst af kravene 2 til 14, hvor D er syreresten af et alkansyre-NSAID med formlen (III):
E repræsenterer et eventuelt substitueret ringsystem; J er udvalgt fra gruppen bestående af en binding eller en funktionel gruppe; R4 og R5 hver uafhængigt er udvalgt fra gruppen bestående af en binding og en eventuelt substitueret alifatisk gruppe.
16. Polymer-NSAID-konjugat ifølge et hvilket som helst af kravene 2 til 15, hvor D er syreresten af et alkansyre-NSAID udvalgt fra gruppen bestående af aceclofenac, alminoprofen, amfenac, carprofen, diclofenac, enfenaminsyre, etodolac, flufenamsyre, meclofenaminsyre, mefenaminsyre, nifluminsyre, tolfenaminsyre, bendazac, benoxaprofen, bermoprofen, bucloxinsyre, butibufen, cinmetacin, clidanac, clopirac, dexibuprofen, dexketoprofen, felbinac, fenbufen, fenclozinsyre, fenoprofen, fentiazac, flunoxaprofen, flunixin, flurbiprofen, ibuprofen, indomethacin, isofezolac, isoxepac, ketoprofen, licofelon, lonazolac, loxoprofen, lumiracoxib, metiazininsyre, mofezolac, naproxen, oxaprozin, pirazolac, pirprofen, pranoprofen, protizininsyre, sulindac, suprofen, tiaprofeninsyre, tolmetin, bermoprofen, bucloxinsyre, isoxepac, ketoprofen, loxoprofen, zaltoprofen, balsalazid, fendosal, olsalazin, ximoprofen, mesalamin, sulfasalazin, acetylsalicylsyre, alclofenac, aspirin, benoxaprofen, 5-bromsalicylsyreacetat, cinchophen, diacerein, dipyrocetyl, fosfosal, ibufenac, indoprofen, clometacin, ketorolac, zomepirac, actarit, clonixin, salicylamid-O-eddikesyre, diflunisal, gentisinsyre og salsalat.
DK13809454.5T 2012-06-26 2013-06-26 Polymer-nsaid-konjugat DK2863921T3 (da)

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Families Citing this family (8)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2017041095A1 (en) * 2015-09-03 2017-03-09 Allegheny-Singer Research Institute Hydrophilic fentanyl derivatives
MY188794A (en) * 2015-09-11 2022-01-03 Polyactiva Pty Ltd Polymer conjugate comprising a bioactive agent
KR101795302B1 (ko) 2016-09-22 2017-11-09 순천향대학교 산학협력단 퇴행성 뇌질환 예방 또는 치료용 약학 조성물
JP7355649B2 (ja) * 2017-03-14 2023-10-03 ポリアクティヴァ・プロプライエタリー・リミテッド 薬物－ポリマーコンジュゲート
KR20260011205A (ko) * 2017-10-05 2026-01-22 소니그룹주식회사 프로그램가능한 중합체성 약물
CN112154158A (zh) * 2018-03-22 2020-12-29 持田制药株式会社 连接有非甾体抗炎化合物的海藻酸衍生物
US12509469B2 (en) 2019-08-07 2025-12-30 Ripple Therapeutics Corporation Compositions and methods for the treatment of pain and dependence disorders
WO2021220061A2 (en) 2020-05-01 2021-11-04 Ripple Therapeutics Corporation Heterodimer compositions and methods for the treatment of ocular disorders

Family Cites Families (10)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP0195582B1 (en) 1985-03-14 1990-01-24 SMITH KLINE DAUELSBERG GmbH 5-aminosalicylic acid derivatives of non-steroidal antiinflammatory acids
CA2167818A1 (en) * 1993-08-02 1995-02-09 Robert George Whittaker Therapeutic compound - fatty acid conjugates
EP1898955A2 (en) * 2005-06-17 2008-03-19 Nektar Therapeutics AL, Corporation Polymer-based compositions and conjugates of non-steroidal anti-inflammatory drugs
WO2007149456A2 (en) * 2006-06-19 2007-12-27 Vanderbilt University Methods and compositions for diagnostic and therapeutic targeting of cox-2
CN101977631A (zh) * 2008-03-18 2011-02-16 日本化药株式会社 生理活性物质的高分子量偶联物
GB0810359D0 (en) * 2008-06-06 2008-07-09 Univ Belfast Composition
IT1391812B1 (it) * 2008-07-29 2012-01-27 Maria Grazia Rimoli Profarmaco galattosilato del ketorolac ad uso analgesico e antinfiammatorio con migliori caratteristiche farmacocinetiche e profilo tossicologico del farmaco di partenza
US8535655B2 (en) * 2008-10-10 2013-09-17 Polyactiva Pty Ltd. Biodegradable polymer—bioactive moiety conjugates
PT2355853T (pt) * 2008-10-10 2017-03-15 Polyactiva Pty Ltd Conjugados polímero biodegradável ¿ unidade bioativa
JP2014510762A (ja) * 2011-04-12 2014-05-01 ポリアクティヴァ・プロプライエタリー・リミテッド ポリマーにコンジュゲートしたプロスタグランジン類似体

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US20150150999A1 (en) 2015-06-04
BR112014032620A2 (pt) 2017-06-27
KR20150022914A (ko) 2015-03-04
WO2014000033A1 (en) 2014-01-03
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AU2013284342A1 (en) 2014-12-18
ZA201409119B (en) 2016-01-27
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CN104797257A (zh) 2015-07-22
CA2876728A1 (en) 2014-01-03
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TR201809741T4 (tr) 2018-07-23
PT2863921T (pt) 2018-07-17
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