JP2016500682A - 経口ペプチドデリバリーのための脂肪酸アシル化アミノ酸 - Google Patents

経口ペプチドデリバリーのための脂肪酸アシル化アミノ酸 Download PDF

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JP2016500682A
JP2016500682A JP2015537240A JP2015537240A JP2016500682A JP 2016500682 A JP2016500682 A JP 2016500682A JP 2015537240 A JP2015537240 A JP 2015537240A JP 2015537240 A JP2015537240 A JP 2015537240A JP 2016500682 A JP2016500682 A JP 2016500682A
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glp
ethoxy
sodium
amino acid
certain embodiments
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JP2016500682A5 (enExample
Inventor
シモン・ビェルレガード
フローリアン・フエガー
ステファン・バックレー
フランティセク・ヒューバレック
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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
    • 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
    • A61K47/183—Amino acids, e.g. glycine, EDTA or aspartame
    • 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
    • A61K38/26—Glucagons
    • 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
    • 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
    • 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
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/48—Preparations in capsules, e.g. of gelatin, of chocolate
    • A61K9/4841—Filling excipients; Inactive ingredients
    • A61K9/4858—Organic compounds
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00—Drugs for disorders of the metabolism
    • A61P3/08—Drugs for disorders of the metabolism for glucose homeostasis
    • A61P3/10—Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
    • 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
    • A61K47/14—Esters of carboxylic acids, e.g. fatty acid monoglycerides, medium-chain triglycerides, parabens or PEG fatty acid esters
    • 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
    • A61K47/26—Carbohydrates, e.g. sugar alcohols, amino sugars, nucleic acids, mono-, di- or oligo-saccharides; Derivatives thereof, e.g. polysorbates, sorbitan fatty acid esters or glycyrrhizin
    • 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
    • A61K9/48—Preparations in capsules, e.g. of gelatin, of chocolate
    • A61K9/4841—Filling excipients; Inactive ingredients
    • A61K9/4866—Organic macromolecular compounds

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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)
  • Pharmacology & Pharmacy (AREA)
  • Epidemiology (AREA)
  • Engineering & Computer Science (AREA)
  • Proteomics, Peptides & Aminoacids (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Oil, Petroleum & Natural Gas (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Endocrinology (AREA)
  • Diabetes (AREA)
  • Immunology (AREA)
  • Zoology (AREA)
  • Nutrition Science (AREA)
  • Gastroenterology & Hepatology (AREA)
  • Physiology (AREA)
  • Biophysics (AREA)
  • Dispersion Chemistry (AREA)
  • Molecular Biology (AREA)
  • Emergency Medicine (AREA)
  • Hematology (AREA)
  • Obesity (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Organic Chemistry (AREA)
  • Medicinal Preparation (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Peptides Or Proteins (AREA)
JP2015537240A 2012-10-17 2013-10-16 経口ペプチドデリバリーのための脂肪酸アシル化アミノ酸 Withdrawn JP2016500682A (ja)

Applications Claiming Priority (5)

Application Number Priority Date Filing Date Title
EP12188872.1 2012-10-17
EP12188872 2012-10-17
US201261715416P 2012-10-18 2012-10-18
US61/715,416 2012-10-18
PCT/EP2013/071618 WO2014060472A1 (en) 2012-10-17 2013-10-16 Fatty acid acylated amino acids for oral peptide delivery

Publications (2)

Publication Number Publication Date
JP2016500682A true JP2016500682A (ja) 2016-01-14
JP2016500682A5 JP2016500682A5 (enExample) 2016-12-08

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JP2015537240A Withdrawn JP2016500682A (ja) 2012-10-17 2013-10-16 経口ペプチドデリバリーのための脂肪酸アシル化アミノ酸

Country Status (5)

Country Link
US (1) US20150273069A1 (enExample)
EP (1) EP2908844A1 (enExample)
JP (1) JP2016500682A (enExample)
CN (1) CN104717972A (enExample)
WO (1) WO2014060472A1 (enExample)

Cited By (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP2019528237A (ja) * 2017-08-24 2019-10-10 ノヴォ ノルディスク アー／エス Ｇｌｐ−１組成物及びその使用
JP2023541827A (ja) * 2020-09-07 2023-10-04 サイプルメド ゲーエムベーハー Ｇｌｐ－１受容体アゴニストの改善された医薬製剤

Families Citing this family (18)

* 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
US9833411B2 (en) 2015-01-12 2017-12-05 Enteris Biopharma, Inc. Solid oral dosage forms
JP7211704B2 (ja) * 2015-01-29 2023-01-24 ノヴォ ノルディスク アー／エス Ｇｌｐ－１アゴニスト及び腸溶コーティングを含む錠剤
US20180263915A1 (en) * 2015-01-29 2018-09-20 Novo Nordisk A/S Pharmaceutical Composition for Oral GLP-1 Administration Comprising a Tablet Core and Immediate Release Coating
KR102393596B1 (ko) 2016-04-22 2022-05-04 리셉터 홀딩스, 인크. 속효성 식물-계 의약 화합물 및 영양 보충제
EA201892396A1 (ru) 2016-12-02 2019-04-30 Ресептор Лайф Сайенсиз, Инк. Быстродействующие растительные лекарственные соединения и биологически активные добавки
JP7422754B2 (ja) * 2018-10-26 2024-01-26 ノヴォ ノルディスク アー／エス 安定性セマグルチド組成物およびその使用
AR117118A1 (es) 2018-11-19 2021-07-14 Receptor Holdings Inc Aminoácidos grasos n-acilados para reducir la variabilidad de absorción en composiciones a base de cannabinoides
BR112022013795A2 (pt) 2020-02-18 2022-09-13 Novo Nordisk As Composição farmacêutica líquida, e, kit
JP2023545684A (ja) 2020-09-30 2023-10-31 ベイジン キューエル バイオファーマシューティカル カンパニー，リミテッド ポリペプチドコンジュゲートおよび使用の方法
WO2022152131A1 (zh) * 2021-01-12 2022-07-21 广州新济药业科技有限公司 司美格鲁肽可溶性微针贴片及其制备方法
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
EP4299057A1 (en) 2022-06-30 2024-01-03 Adocia Solid compositions comprising a peptide or a protein and an acylated amino acid
JP2025508982A (ja) * 2022-03-03 2025-04-10 サイプルメド ゲーエムベーハー 治療用ペプチドおよびタンパク質の改善された経口医薬製剤
EP4323413A4 (en) 2022-03-30 2025-10-15 Beijing Ql Biopharmaceutical Co Ltd LIQUID PHARMACEUTICAL COMPOSITIONS OF POLYPEPTIDE CONJUGATES AND METHODS OF USE THEREOF
KR20250144708A (ko) * 2024-03-27 2025-10-13 한국과학기술연구원 올리고감마글루탐산 유도체 기반의 신규한 지질 및 이를 포함하는 지질나노입자와 이의 용도
US12544349B1 (en) 2024-12-30 2026-02-10 Adocia Compositions comprising pemvidutide and an acylated amino acid

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US5629020A (en) * 1994-04-22 1997-05-13 Emisphere Technologies, Inc. Modified amino acids for drug delivery
DK39892D0 (da) 1992-03-25 1992-03-25 Bernard Thorens Peptid
US5869602A (en) 1995-03-17 1999-02-09 Novo Nordisk A/S Peptide derivatives
IL128332A0 (en) 1996-08-30 2000-01-31 Novo Nordisk As GLP-1 derivatives
WO1999043706A1 (en) 1998-02-27 1999-09-02 Novo Nordisk A/S Derivatives of glp-1 analogs
AU3247799A (en) 1998-02-27 1999-09-15 Novo Nordisk A/S Glp-1 derivatives of glp-1 and exendin with protracted profile of action
EP1061946B1 (en) 1998-02-27 2004-04-28 Novo Nordisk A/S Glp-1 derivatives with helix-content exceeding 25 %, forming partially structured micellar-like aggregates
JP2002506792A (ja) 1998-02-27 2002-03-05 ノボ ノルディスク アクティーゼルスカブ Ｎ末端修飾ｇｌｐ−１誘導体
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
CA2539253A1 (en) 2003-09-19 2005-03-31 Novo Nordisk A/S Albumin-binding derivatives of therapeutic peptides
AU2004298424A1 (en) 2003-12-18 2005-06-30 Novo Nordisk A/S Novel GLP-1 compounds
BRPI0417684A (pt) 2003-12-18 2007-03-20 Novo Nordisk As composto, composição farmacêutica, e, uso de um composto
US20060286129A1 (en) * 2003-12-19 2006-12-21 Emisphere Technologies, Inc. Oral GLP-1 formulations
WO2006003781A1 (ja) 2004-06-30 2006-01-12 Pioneer Corporation バックアップ装置および車載機器
ES2542228T3 (es) 2004-07-08 2015-08-03 Novo Nordisk A/S Marcas de prolongación polipeptídica que comprenden un resto de tetrazol
US7544714B2 (en) * 2004-07-16 2009-06-09 University Of Massachusetts Lipid-amino acid conjugates and methods of use
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TWI372629B (en) * 2005-03-18 2012-09-21 Novo Nordisk As Acylated glp-1 compounds
BRPI0608516A2 (pt) 2005-03-18 2010-11-16 Novo Nordisk As análogo de glp-1, método para aumentar o tempo de ação em um paciente de um análogo de glp-1, composição farmacêutica, e, uso de um composto
US20090318353A1 (en) 2006-08-25 2009-12-24 Novo Nordisk A/S Acylated Exendin-4 Compounds
US20100261637A1 (en) 2007-09-05 2010-10-14 Novo Nordisk A/S Peptides derivatized with a-b-c-d- and their therapeutical use
ES2672770T3 (es) 2007-09-05 2018-06-18 Novo Nordisk A/S Derivados del péptido-1 similar al glucagón y su uso farmacéutico
US20100292133A1 (en) 2007-09-05 2010-11-18 Novo Nordisk A/S Truncated glp-1 derivaties and their therapeutical use
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EP2696847A1 (en) * 2011-04-14 2014-02-19 Novo Nordisk A/S Fatty acid acylated amino acids for oral peptide delivery

Cited By (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP2019528237A (ja) * 2017-08-24 2019-10-10 ノヴォ ノルディスク アー／エス Ｇｌｐ−１組成物及びその使用
JP2023541827A (ja) * 2020-09-07 2023-10-04 サイプルメド ゲーエムベーハー Ｇｌｐ－１受容体アゴニストの改善された医薬製剤

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EP2908844A1 (en) 2015-08-26
US20150273069A1 (en) 2015-10-01
CN104717972A (zh) 2015-06-17
WO2014060472A1 (en) 2014-04-24

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