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)
  • General Health & Medical Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Animal Behavior & Ethology (AREA)
  • Medicinal Chemistry (AREA)
  • Epidemiology (AREA)
  • Engineering & Computer Science (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Proteomics, Peptides & Aminoacids (AREA)
  • Oil, Petroleum & Natural Gas (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Endocrinology (AREA)
  • Diabetes (AREA)
  • Gastroenterology & Hepatology (AREA)
  • Zoology (AREA)
  • Physiology (AREA)
  • Nutrition Science (AREA)
  • Immunology (AREA)
  • Biophysics (AREA)
  • Molecular Biology (AREA)
  • Dispersion Chemistry (AREA)
  • Emergency Medicine (AREA)
  • Organic Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Obesity (AREA)
  • Hematology (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 2012-10-17
EP12188872.1 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

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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)

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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
JP6910950B2 (ja) 2015-01-12 2021-07-28 エンテリス・バイオファーマ・インコーポレイテッドＥｎｔｅｒｉｓ Ｂｉｏｐｈａｒｍａ，Ｉｎｃ． 固形経口剤形
JP2018505173A (ja) * 2015-01-29 2018-02-22 ノヴォ ノルディスク アー／エス 錠剤コアと即時放出コーティングとを含む経口ｇｌｐ−１投与用の医薬組成物
US10265384B2 (en) 2015-01-29 2019-04-23 Novo Nordisk A/S Tablets comprising GLP-1 agonist and enteric coating
US10588974B2 (en) 2016-04-22 2020-03-17 Receptor Holdings, Inc. Fast-acting plant-based medicinal compounds and nutritional supplements
EA201892396A1 (ru) 2016-12-02 2019-04-30 Ресептор Лайф Сайенсиз, Инк. Быстродействующие растительные лекарственные соединения и биологически активные добавки
IL281938B2 (en) * 2018-10-26 2024-04-01 Novo Nordisk As Stable semaglutide compositions and uses thereof
UY38480A (es) 2018-11-19 2020-06-30 Receptor Holdings Inc Aminoácidos grasos n-acilados para reducir la variabilidad de absorción en composiciones a base de cannabinoides
PE20221575A1 (es) 2020-02-18 2022-10-06 Novo Nordisk As Formulaciones farmaceuticas
EP4222176A4 (en) 2020-09-30 2024-02-28 Beijing QL Biopharmaceutical Co., Ltd. POLYPEPTIDE CONJUGATES AND METHODS OF USE
CN114272511B (zh) * 2021-01-12 2023-08-01 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
US20260027062A1 (en) * 2022-03-03 2026-01-29 Cyprumed Gmbh Improved oral pharmaceutical formulations of therapeutic peptides and proteins
KR20240163717A (ko) 2022-03-30 2024-11-19 베이징 큐엘 바이오파마슈티컬 컴퍼니 리미티드 폴리펩티드 접합체의 액체 약학 조성물 및 그의 사용 방법
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
JP3149958B2 (ja) 1996-08-30 2001-03-26 ノボ ノルディスク アクティーゼルスカブ Ｇｌｐ―１誘導体
JP2002504518A (ja) 1998-02-27 2002-02-12 ノボ ノルディスク アクティーゼルスカブ 部分的に構造化されたミセルー様凝集体を形成する、２５％を超えるヘリックス−含有率を有するｇｌｐ−１誘導体
WO1999043708A1 (en) 1998-02-27 1999-09-02 Novo Nordisk A/S Glp-1 derivatives of glp-1 and exendin with protracted profile of action
WO1999043706A1 (en) 1998-02-27 1999-09-02 Novo Nordisk A/S Derivatives of glp-1 analogs
AU2610899A (en) 1998-02-27 1999-09-15 Novo Nordisk A/S N-terminally modified glp-1 derivatives
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
KR101241862B1 (ko) 2003-09-19 2013-03-13 노보 노르디스크 에이/에스 신규 ｇｌｐ-1 유도체
CA2550050A1 (en) 2003-12-18 2005-06-30 Novo Nordisk A/S Novel glp-1 analogues linked to albumin-like agents
JP2007537141A (ja) 2003-12-18 2007-12-20 ノボ　ノルディスク　アクティーゼルスカブ 新規なｇｌｐ−１化合物
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
ES2564167T3 (es) 2004-07-08 2016-03-18 Novo Nordisk A/S Conjugados de polipéptidos de acción prolongada que contienen una fracción tetrazol
US7544714B2 (en) * 2004-07-16 2009-06-09 University Of Massachusetts Lipid-amino acid conjugates and methods of use
EP2330126B1 (en) 2004-10-07 2015-12-23 Novo Nordisk A/S Protracted exendin-4 compounds
JP5755398B2 (ja) 2005-03-18 2015-07-29 ノヴォ ノルディスク アー／エス 伸長されたｇｌｐ−１化合物
TWI372629B (en) 2005-03-18 2012-09-21 Novo Nordisk As Acylated glp-1 compounds
EP2057189B1 (en) 2006-08-25 2013-03-06 Novo Nordisk A/S Acylated exendin-4 compounds
ES2672770T3 (es) 2007-09-05 2018-06-18 Novo Nordisk A/S Derivados del péptido-1 similar al glucagón y su uso farmacéutico
WO2009030771A1 (en) 2007-09-05 2009-03-12 Novo Nordisk A/S Peptides derivatized with a-b-c-d- and their therapeutical use
WO2009030774A1 (en) 2007-09-05 2009-03-12 Novo Nordisk A/S Truncated glp-1 derivatives and their therapeutical use
US20100317057A1 (en) 2007-12-28 2010-12-16 Novo Nordisk A/S Semi-recombinant preparation of glp-1 analogues
US20140056953A1 (en) * 2011-04-14 2014-02-27 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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CN104717972A (zh) 2015-06-17
US20150273069A1 (en) 2015-10-01
EP2908844A1 (en) 2015-08-26
WO2014060472A1 (en) 2014-04-24

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