KR101357117B1 - 폴리에틸렌글라이콜 또는 이의 유도체로 페길화된 엑센딘-4 유사체, 이의 제조방법 및 이를 유효성분으로 함유하는 당뇨병 예방 또는 치료용 약학적 조성물 - Google Patents

폴리에틸렌글라이콜 또는 이의 유도체로 페길화된 엑센딘-4 유사체, 이의 제조방법 및 이를 유효성분으로 함유하는 당뇨병 예방 또는 치료용 약학적 조성물 Download PDF

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KR101357117B1
KR101357117B1 KR1020110062858A KR20110062858A KR101357117B1 KR 101357117 B1 KR101357117 B1 KR 101357117B1 KR 1020110062858 A KR1020110062858 A KR 1020110062858A KR 20110062858 A KR20110062858 A KR 20110062858A KR 101357117 B1 KR101357117 B1 KR 101357117B1
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exendin
polyethylene glycol
peg
pegylated
derivatives
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Korean (ko)
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KR20130008665A (ko
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이성권
김원배
이슬기
김태형
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비앤엘델리팜 주식회사
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Priority to EP12804683.6A priority patent/EP2727605B1/en
Priority to JP2014518803A priority patent/JP6084215B2/ja
Priority to US13/882,361 priority patent/US20130217622A1/en
Priority to PCT/KR2012/005137 priority patent/WO2013002580A2/ko
Priority to CA2839410A priority patent/CA2839410C/en
Priority to ES12804683.6T priority patent/ES2674581T3/es
Priority to AU2012276478A priority patent/AU2012276478B2/en
Priority to DK12804683.6T priority patent/DK2727605T3/en
Priority to CN201280003243.XA priority patent/CN103338790B/zh
Publication of KR20130008665A publication Critical patent/KR20130008665A/ko
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Publication of KR101357117B1 publication Critical patent/KR101357117B1/ko
Assigned to (주)디앤디파마텍 reassignment (주)디앤디파마텍 권리의 전부이전등록 Assignors: 비앤엘델리팜 주식회사
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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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
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    • 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
    • A61K47/02—Inorganic compounds
    • 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
    • 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
    • A61K38/2278—Vasoactive intestinal peptide [VIP]; Related peptides (e.g. Exendin)
    • 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
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    • 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
    • A61K47/30—Macromolecular organic or inorganic compounds, e.g. inorganic polyphosphates
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    • 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
    • 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
    • A61K9/0019—Injectable compositions; Intramuscular, intravenous, arterial, subcutaneous administration; Compositions to be administered through the skin in an invasive manner
    • A—HUMAN NECESSITIES
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    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/20—Pills, tablets, discs, rods
    • A61K9/2004—Excipients; Inactive ingredients
    • A61K9/2013—Organic compounds, e.g. phospholipids, fats
    • A61K9/2018—Sugars, or sugar alcohols, e.g. lactose, mannitol; Derivatives thereof, e.g. polysorbates
    • 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
    • A61K9/20—Pills, tablets, discs, rods
    • A61K9/2004—Excipients; Inactive ingredients
    • A61K9/2022—Organic macromolecular compounds
    • A61K9/205—Polysaccharides, e.g. alginate, gums; Cyclodextrin
    • A61K9/2059—Starch, including chemically or physically modified derivatives; Amylose; Amylopectin; Dextrin
    • 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
    • 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
    • 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07K—PEPTIDES
    • C07K14/00—Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof
    • C07K14/435—Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof from animals; from humans
    • C07K14/575—Hormones
    • C07K14/57563—Vasoactive intestinal peptide [VIP]; Related peptides

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  • Chemical & Material Sciences (AREA)
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  • General Health & Medical Sciences (AREA)
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  • Bioinformatics & Cheminformatics (AREA)
  • Endocrinology (AREA)
  • Molecular Biology (AREA)
  • Zoology (AREA)
  • Proteomics, Peptides & Aminoacids (AREA)
  • Organic Chemistry (AREA)
  • Gastroenterology & Hepatology (AREA)
  • Vascular Medicine (AREA)
  • Biochemistry (AREA)
  • Biophysics (AREA)
  • Immunology (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Inorganic Chemistry (AREA)
  • Diabetes (AREA)
  • Genetics & Genomics (AREA)
  • Toxicology (AREA)
  • Oil, Petroleum & Natural Gas (AREA)
  • Dermatology (AREA)
  • Emergency Medicine (AREA)
  • Hematology (AREA)
  • Obesity (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Medicinal Preparation (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Peptides Or Proteins (AREA)
  • Preparation Of Compounds By Using Micro-Organisms (AREA)
KR1020110062858A 2011-06-28 2011-06-28 폴리에틸렌글라이콜 또는 이의 유도체로 페길화된 엑센딘-4 유사체, 이의 제조방법 및 이를 유효성분으로 함유하는 당뇨병 예방 또는 치료용 약학적 조성물 Active KR101357117B1 (ko)

Priority Applications (11)

Application Number Priority Date Filing Date Title
KR1020110062858A KR101357117B1 (ko) 2011-06-28 2011-06-28 폴리에틸렌글라이콜 또는 이의 유도체로 페길화된 엑센딘-4 유사체, 이의 제조방법 및 이를 유효성분으로 함유하는 당뇨병 예방 또는 치료용 약학적 조성물
DK12804683.6T DK2727605T3 (en) 2011-06-28 2012-06-28 EXENDIN-4 ANALOG PEGYLED WITH POLYETHYLENE LYCOL OR A DERIVATIVE THEREOF, PROCEDURE FOR PREPARING IT AND PHARMACEUTICAL COMPOSITION FOR PREVENTION OR TREATMENT OF DIABLE SUBSTANCES,
US13/882,361 US20130217622A1 (en) 2011-06-28 2012-06-28 Exendin-4 analogue pegylated with polyethylene glycol or derivative thereof, preparation method thereof, and pharmaceutical compostion for preventing or treating diabetes, containing same as active ingredient
PCT/KR2012/005137 WO2013002580A2 (ko) 2011-06-28 2012-06-28 폴리에틸렌글라이콜 또는 이의 유도체로 페길화된 엑센딘-4 유사체, 이의 제조방법 및 이를 유효성분으로 함유하는 당뇨병 예방 또는 치료용 약학적 조성물
CA2839410A CA2839410C (en) 2011-06-28 2012-06-28 Pegylated analogues of exendin-4
ES12804683.6T ES2674581T3 (es) 2011-06-28 2012-06-28 Análogo de exendina-4 pegilado con polietilenglicol o derivado del mismo, método de preparación del mismo y composición farmacéutica para evitar o tratar diabetes, que contiene el mismo como principio activo
EP12804683.6A EP2727605B1 (en) 2011-06-28 2012-06-28 Exendin-4 analogue pegylated with polyethylene glycol or derivative thereof, preparation method thereof, and pharmaceutical composition for preventing or treating diabetes, containing same as active ingredient
JP2014518803A JP6084215B2 (ja) 2011-06-28 2012-06-28 ポリエチレングリコールまたはその誘導体でｐｅｇ化されたエキセンジン−４類似体、その調製法、および活性成分としてこれを含有する、糖尿病を予防または処置するための薬学的組成物
CN201280003243.XA CN103338790B (zh) 2011-06-28 2012-06-28 用聚乙二醇或其衍生物聚乙二醇化的唾液素‑4类似物、其制备方法以及含有其作为活性成分的用于预防或治疗糖尿病的药物组合物
AU2012276478A AU2012276478B2 (en) 2011-06-28 2012-06-28 Exendin-4 analogue pegylated with polyethylene glycol or derivative thereof, preparation method thereof, and pharmaceutical composition for preventing or treating diabetes, containing same as active ingredient
US15/413,029 US10406230B2 (en) 2011-06-28 2017-01-23 Exendin-4 analogue pegylated with polyethylene glycol or derivative thereof, preparation method thereof, and pharmaceutical composition for preventing or treating diabetes, containing same as active ingredient

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
KR1020110062858A KR101357117B1 (ko) 2011-06-28 2011-06-28 폴리에틸렌글라이콜 또는 이의 유도체로 페길화된 엑센딘-4 유사체, 이의 제조방법 및 이를 유효성분으로 함유하는 당뇨병 예방 또는 치료용 약학적 조성물

Publications (2)

Publication Number Publication Date
KR20130008665A KR20130008665A (ko) 2013-01-23
KR101357117B1 true KR101357117B1 (ko) 2014-02-06

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KR1020110062858A Active KR101357117B1 (ko) 2011-06-28 2011-06-28 폴리에틸렌글라이콜 또는 이의 유도체로 페길화된 엑센딘-4 유사체, 이의 제조방법 및 이를 유효성분으로 함유하는 당뇨병 예방 또는 치료용 약학적 조성물

Country Status (10)

Country Link
US (2) US20130217622A1 (https=)
EP (1) EP2727605B1 (https=)
JP (1) JP6084215B2 (https=)
KR (1) KR101357117B1 (https=)
CN (1) CN103338790B (https=)
AU (1) AU2012276478B2 (https=)
CA (1) CA2839410C (https=)
DK (1) DK2727605T3 (https=)
ES (1) ES2674581T3 (https=)
WO (1) WO2013002580A2 (https=)

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KR20240155737A (ko) 2023-04-20 2024-10-29 전북대학교산학협력단 폴리에틸렌글리콜을 이용한 분자 전달 방법

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UA116217C2 (uk) 2012-10-09 2018-02-26 Санофі Пептидна сполука як подвійний агоніст рецепторів glp1-1 та глюкагону
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EP3080152A1 (en) 2013-12-13 2016-10-19 Sanofi Non-acylated exendin-4 peptide analogues
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