CN104884078B - 用于口服肽递送的脂肪酸酰化d‑氨基酸 - Google Patents

用于口服肽递送的脂肪酸酰化d‑氨基酸 Download PDF

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Publication number
CN104884078B
CN104884078B CN201380054364.1A CN201380054364A CN104884078B CN 104884078 B CN104884078 B CN 104884078B CN 201380054364 A CN201380054364 A CN 201380054364A CN 104884078 B CN104884078 B CN 104884078B
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daa
amino acid
sodium
potassium
insulin
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Expired - Fee Related
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CN201380054364.1A
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Chinese (zh)
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CN104884078A (zh
Inventor
弗兰蒂泽克·胡巴勒克
弗洛里安·安德斯·弗格
A.马克霍夫
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Novo Nordisk AS
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Novo Nordisk AS
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    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/0012—Galenical forms characterised by the site of application
    • A61K9/0053—Mouth and digestive tract, i.e. intraoral and peroral administration
    • A61K9/006—Oral mucosa, e.g. mucoadhesive forms, sublingual droplets; Buccal patches or films; Buccal sprays
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K38/00—Medicinal preparations containing peptides
    • A61K38/16—Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof
    • A61K38/17—Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof from animals; from humans
    • A61K38/22—Hormones
    • A61K38/28—Insulins
    • 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
    • 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
    • A61K47/06—Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite
    • A61K47/08—Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite containing oxygen, e.g. ethers, acetals, ketones, quinones, aldehydes, peroxides
    • A61K47/10—Alcohols; Phenols; Salts thereof, e.g. glycerol; Polyethylene glycols [PEG]; Poloxamers; PEG/POE alkyl ethers
    • 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
    • A61K47/06—Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite
    • A61K47/16—Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite containing nitrogen, e.g. nitro-, nitroso-, azo-compounds, nitriles, cyanates
    • A61K47/18—Amines; Amides; Ureas; Quaternary ammonium compounds; Amino acids; Oligopeptides having up to five amino acids
    • 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
    • A61K47/06—Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite
    • A61K47/22—Heterocyclic compounds, e.g. ascorbic acid, tocopherol or pyrrolidones
    • 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
    • A61K47/44—Oils, fats or waxes according to two or more groups of A61K47/02-A61K47/42; Natural or modified natural oils, fats or waxes, e.g. castor oil, polyethoxylated castor oil, montan wax, lignite, shellac, rosin, beeswax or lanolin
    • 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
    • A61K47/62—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 a protein, peptide or polyamino acid
    • A61K47/64—Drug-peptide, drug-protein or drug-polyamino acid conjugates, i.e. the modifying agent being a peptide, protein or polyamino acid which is covalently bonded or complexed to a therapeutically active agent
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/0012—Galenical forms characterised by the site of application
    • A61K9/0053—Mouth and digestive tract, i.e. intraoral and peroral administration
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/10—Dispersions; Emulsions
    • A61K9/107—Emulsions ; Emulsion preconcentrates; Micelles
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/10—Dispersions; Emulsions
    • A61K9/107—Emulsions ; Emulsion preconcentrates; Micelles
    • A61K9/1075—Microemulsions or submicron emulsions; Preconcentrates or solids thereof; Micelles, e.g. made of phospholipids or block copolymers
    • 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
    • A61K47/62—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 a protein, peptide or polyamino acid

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  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Epidemiology (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Engineering & Computer Science (AREA)
  • Proteomics, Peptides & Aminoacids (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Oil, Petroleum & Natural Gas (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Molecular Biology (AREA)
  • Physiology (AREA)
  • Nutrition Science (AREA)
  • Dispersion Chemistry (AREA)
  • Immunology (AREA)
  • Diabetes (AREA)
  • Endocrinology (AREA)
  • Zoology (AREA)
  • Gastroenterology & Hepatology (AREA)
  • Biophysics (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Peptides Or Proteins (AREA)
  • Medicinal Preparation (AREA)
CN201380054364.1A 2012-10-17 2013-10-16 用于口服肽递送的脂肪酸酰化d‑氨基酸 Expired - Fee Related CN104884078B (zh)

Applications Claiming Priority (5)

Application Number Priority Date Filing Date Title
EP12188807.7 2012-10-17
EP12188807 2012-10-17
US201261715412P 2012-10-18 2012-10-18
US61/715412 2012-10-18
PCT/EP2013/071575 WO2014060447A1 (en) 2012-10-17 2013-10-16 Fatty acid acylated d-amino acids for oral peptide delivery

Publications (2)

Publication Number Publication Date
CN104884078A CN104884078A (zh) 2015-09-02
CN104884078B true CN104884078B (zh) 2017-06-20

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CN201380054364.1A Expired - Fee Related CN104884078B (zh) 2012-10-17 2013-10-16 用于口服肽递送的脂肪酸酰化d‑氨基酸

Country Status (5)

Country Link
US (2) US20150265710A1 (enExample)
EP (1) EP2908846A1 (enExample)
JP (1) JP6285447B2 (enExample)
CN (1) CN104884078B (enExample)
WO (1) WO2014060447A1 (enExample)

Families Citing this family (6)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2015162195A1 (en) * 2014-04-23 2015-10-29 Novo Nordisk A/S Fatty acid acylated amino acids for oral peptide delivery
CN115942970A (zh) * 2020-08-18 2023-04-07 密歇根大学董事会 N-酰基氨基酸产物及用途
EP4299057A1 (en) 2022-06-30 2024-01-03 Adocia Solid compositions comprising a peptide or a protein and an acylated amino acid
US20250000948A1 (en) 2021-11-15 2025-01-02 Adocia Solid compositions comprising a peptide or a protein and an acylated amino acid
EP4180060A1 (en) 2021-11-15 2023-05-17 Adocia Solid compositions comprising a peptide or a protein and an acylated amino acid
EP4299071A1 (en) * 2022-07-01 2024-01-03 Adocia Compositions comprising a peptide or a protein and an acylated amino acid

Citations (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP0432039A2 (en) * 1989-12-05 1991-06-12 NIPPON OILS & FATS CO., LTD. Antipsychotic drug comprising an acylaminoacid
EP1656951A1 (en) * 2004-11-12 2006-05-17 Xigen S.A. Conjugates with enhanced cell uptake activity
CN103458873A (zh) * 2011-04-14 2013-12-18 诺沃—诺迪斯克有限公司 用于口服肽递送的脂肪酸酰化的氨基酸

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US4966848A (en) * 1988-02-08 1990-10-30 The General Hospital Corporation Isolation, purification, characterization, cloning and sequencing of N α-acetyltransferase
US5223421A (en) * 1989-10-25 1993-06-29 The General Hospital Corporation Identification of methionine Nα-acetyltransferase
JPH0543889A (ja) * 1991-08-19 1993-02-23 Kanebo Ltd 洗浄剤組成物
US5688489A (en) * 1995-09-15 1997-11-18 Resolution Pharmaceuticals, Inc. Non-receptor mediated imaging agents
FR2767064B1 (fr) * 1997-08-07 1999-11-12 Centre Nat Rech Scient Procede de liberation d'un principe actif contenu dans une emulsion multiple
EP1265638A1 (en) 1999-11-12 2002-12-18 Pharmaderm Laboratories Ltd. Compositions for transdermal and transmucosal administration of therapeutic agents
US6656499B1 (en) * 1999-11-12 2003-12-02 Pharmaderm Laboratories, Ltd. Composition for transdermal and dermal administration of interferon-α
FR2828102B1 (fr) * 2001-03-28 2004-07-09 Ifc Sa Utilisation des lipoaminoacides dans une composition pharmaceutique comme promoteur et systeme disperse a usage pharmaceutique contenant de tels composes
US6951655B2 (en) 2001-10-11 2005-10-04 Imi Biomed, Inc. Pro-micelle pharmaceutical compositions
US8088734B2 (en) 2003-01-21 2012-01-03 Unigene Laboratories Inc. Oral delivery of peptides
BRPI0413276B8 (pt) 2003-08-05 2021-05-25 Novo Nordisk As derivado de insulina, complexo de zinco do mesmo, e, composição farmacêutica
US20050282756A1 (en) 2004-06-18 2005-12-22 Mehta Nozer M Oral delivery of peptide pharmaceutical compositions
US7544714B2 (en) * 2004-07-16 2009-06-09 University Of Massachusetts Lipid-amino acid conjugates and methods of use
ES2601839T3 (es) 2006-09-22 2017-02-16 Novo Nordisk A/S Análogos de insulina resistentes a proteasas
EP2514406A1 (en) 2007-06-01 2012-10-24 Novo Nordisk A/S Spontaneously dispersible preconcentrates including a peptide drug in a solid or semisolid carrier
DK2254906T3 (en) 2008-03-18 2017-01-23 Novo Nordisk As Protease-stabilized acylated insulin analogues
EP2370059A1 (en) * 2008-11-28 2011-10-05 Novo Nordisk A/S Pharmaceutical compositions suitable for oral administration of derivatized insulin peptides
JP5123922B2 (ja) 2009-12-02 2013-01-23 独立行政法人科学技術振興機構 融合糖タンパク質から成るエンベロープを有する逆行性輸送ウィルスベクター系

Patent Citations (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP0432039A2 (en) * 1989-12-05 1991-06-12 NIPPON OILS & FATS CO., LTD. Antipsychotic drug comprising an acylaminoacid
EP1656951A1 (en) * 2004-11-12 2006-05-17 Xigen S.A. Conjugates with enhanced cell uptake activity
CN103458873A (zh) * 2011-04-14 2013-12-18 诺沃—诺迪斯克有限公司 用于口服肽递送的脂肪酸酰化的氨基酸

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Publication number Publication date
CN104884078A (zh) 2015-09-02
WO2014060447A1 (en) 2014-04-24
US20170258711A1 (en) 2017-09-14
EP2908846A1 (en) 2015-08-26
JP2015533369A (ja) 2015-11-24
JP6285447B2 (ja) 2018-02-28
US20150265710A1 (en) 2015-09-24

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