AU2012237899B2 - Site-directed mono-substituted PEGylated Exendin analog and preparation method therefor - Google Patents

Site-directed mono-substituted PEGylated Exendin analog and preparation method therefor Download PDF

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Publication number
AU2012237899B2
AU2012237899B2 AU2012237899A AU2012237899A AU2012237899B2 AU 2012237899 B2 AU2012237899 B2 AU 2012237899B2 AU 2012237899 A AU2012237899 A AU 2012237899A AU 2012237899 A AU2012237899 A AU 2012237899A AU 2012237899 B2 AU2012237899 B2 AU 2012237899B2
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AU2012237899A1 (en
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Peng YUE
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Shanghai Benemae Pharmaceutical Corp
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Shanghai Benemae Pharmaceutical Corp
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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07K—PEPTIDES
    • C07K1/00—General methods for the preparation of peptides, i.e. processes for the organic chemical preparation of peptides or proteins of any length
    • C07K1/06—General methods for the preparation of peptides, i.e. processes for the organic chemical preparation of peptides or proteins of any length using protecting groups or activating agents
    • 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
    • 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
    • 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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K38/00—Medicinal preparations containing peptides
    • 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
    • Y—GENERAL TAGGING OF NEW TECHNOLOGICAL DEVELOPMENTS; GENERAL TAGGING OF CROSS-SECTIONAL TECHNOLOGIES SPANNING OVER SEVERAL SECTIONS OF THE IPC; TECHNICAL SUBJECTS COVERED BY FORMER USPC CROSS-REFERENCE ART COLLECTIONS [XRACs] AND DIGESTS
    • Y02—TECHNOLOGIES OR APPLICATIONS FOR MITIGATION OR ADAPTATION AGAINST CLIMATE CHANGE
    • Y02P—CLIMATE CHANGE MITIGATION TECHNOLOGIES IN THE PRODUCTION OR PROCESSING OF GOODS
    • Y02P20/00—Technologies relating to chemical industry
    • Y02P20/50—Improvements relating to the production of bulk chemicals
    • Y02P20/55—Design of synthesis routes, e.g. reducing the use of auxiliary or protecting groups

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Organic Chemistry (AREA)
  • Medicinal Chemistry (AREA)
  • General Health & Medical Sciences (AREA)
  • Biochemistry (AREA)
  • Biophysics (AREA)
  • Genetics & Genomics (AREA)
  • Endocrinology (AREA)
  • Molecular Biology (AREA)
  • Proteomics, Peptides & Aminoacids (AREA)
  • Gastroenterology & Hepatology (AREA)
  • Zoology (AREA)
  • Toxicology (AREA)
  • Vascular Medicine (AREA)
  • Diabetes (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Animal Behavior & Ethology (AREA)
  • Epidemiology (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Obesity (AREA)
  • Hematology (AREA)
  • Emergency Medicine (AREA)
  • Analytical Chemistry (AREA)
  • Peptides Or Proteins (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Medicinal Preparation (AREA)
AU2012237899A 2011-03-30 2012-03-05 Site-directed mono-substituted PEGylated Exendin analog and preparation method therefor Active AU2012237899B2 (en)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
CN201110078314.X 2011-03-30
CN201110078314XA CN102718868A (zh) 2011-03-30 2011-03-30 定点单取代聚乙二醇化Exendin类似物及其制备方法
PCT/CN2012/071910 WO2012130015A1 (zh) 2011-03-30 2012-03-05 定点单取代聚乙二醇化Exendin类似物及其制备方法

Publications (2)

Publication Number Publication Date
AU2012237899A1 AU2012237899A1 (en) 2013-09-19
AU2012237899B2 true AU2012237899B2 (en) 2017-04-13

Family

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AU2012237899A Active AU2012237899B2 (en) 2011-03-30 2012-03-05 Site-directed mono-substituted PEGylated Exendin analog and preparation method therefor

Country Status (10)

Country Link
US (1) US20140142037A1 (enExample)
EP (1) EP2692730B1 (enExample)
JP (1) JP6297969B2 (enExample)
KR (1) KR102005385B1 (enExample)
CN (2) CN106928341B (enExample)
AU (1) AU2012237899B2 (enExample)
BR (1) BR112013024706B1 (enExample)
CA (1) CA2829122C (enExample)
RU (1) RU2625015C2 (enExample)
WO (1) WO2012130015A1 (enExample)

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Publication number Priority date Publication date Assignee Title
UA116217C2 (uk) 2012-10-09 2018-02-26 Санофі Пептидна сполука як подвійний агоніст рецепторів glp1-1 та глюкагону
HUE035803T2 (en) 2012-12-21 2018-05-28 Sanofi Sa Dual GLP1 / GIP or trigonal GLP1 / GIP / glucagon agonists
WO2015086728A1 (en) 2013-12-13 2015-06-18 Sanofi Exendin-4 peptide analogues as dual glp-1/gip receptor agonists
EP3080154B1 (en) 2013-12-13 2018-02-07 Sanofi Dual glp-1/gip receptor agonists
TW201609797A (zh) 2013-12-13 2016-03-16 賽諾菲公司 雙重ｇｌｐ－１／升糖素受體促效劑
WO2015086730A1 (en) 2013-12-13 2015-06-18 Sanofi Non-acylated exendin-4 peptide analogues
KR101768446B1 (ko) * 2014-03-21 2017-08-17 애니젠 주식회사 신규한 엑세나타이드 유사체 및 그의 용도
TW201625670A (zh) 2014-04-07 2016-07-16 賽諾菲公司 衍生自ｅｘｅｎｄｉｎ－４之雙重ｇｌｐ－１／升糖素受體促效劑
TW201625669A (zh) 2014-04-07 2016-07-16 賽諾菲公司 衍生自艾塞那肽－４（Ｅｘｅｎｄｉｎ－４）之肽類雙重ＧＬＰ－１／升糖素受體促效劑
TW201625668A (zh) 2014-04-07 2016-07-16 賽諾菲公司 作為胜肽性雙重ｇｌｐ－１／昇糖素受體激動劑之艾塞那肽－４衍生物
US9932381B2 (en) 2014-06-18 2018-04-03 Sanofi Exendin-4 derivatives as selective glucagon receptor agonists
AR105319A1 (es) 2015-06-05 2017-09-27 Sanofi Sa Profármacos que comprenden un conjugado agonista dual de glp-1 / glucagón conector ácido hialurónico
TW201706291A (zh) 2015-07-10 2017-02-16 賽諾菲公司 作為選擇性肽雙重ｇｌｐ－１／升糖素受體促效劑之新毒蜥外泌肽（ｅｘｅｎｄｉｎ－４）衍生物
GB201603510D0 (en) * 2016-02-29 2016-04-13 Univ Ulster Compositions for use in the treatment of neurological disease
CN115703825B (zh) * 2021-08-17 2026-01-02 派格生物医药(杭州)股份有限公司 艾塞那肽变体及其聚乙二醇缀合物的制备方法

Citations (3)

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WO2007061148A1 (en) * 2005-11-24 2007-05-31 Pegsphere Co., Ltd. Site-specific peg conjugates of glp-1 and methods for production thereof
WO2008058461A1 (en) * 2006-11-14 2008-05-22 Shanghai Huayi Bio-Lab Co., Ltd. Peg modified exendin or exendin analog and compositions and use thereof
WO2008130066A1 (en) * 2007-04-20 2008-10-30 Kang Choon Lee Mono modified exendin with polyethylene glycol or its derivatives and uses thereof

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CN1162446C (zh) * 2001-05-10 2004-08-18 上海华谊生物技术有限公司 促胰岛素分泌肽衍生物
AU2003206158A1 (en) * 2003-01-18 2004-08-13 Pegsphere Co., Ltd. Peptides having protected amines of untargeted sites, methods for production thereof and of specifically conjugated peg peptides using the same
US7557183B2 (en) * 2003-03-19 2009-07-07 Eli Lilly And Company Polyethylene glycol linked GLP-1 compounds
JP5107713B2 (ja) * 2004-10-07 2012-12-26 ノヴォ ノルディスク アー／エス 遅延性のエキセンディン−４化合物
KR100890989B1 (ko) * 2006-06-01 2009-03-31 이강춘 폴리에틸렌글리콜 또는 이의 유도체로 단일 수식된 엑센딘,이의 제조방법 및 이의 용도
US7935877B2 (en) * 2007-04-20 2011-05-03 Master Key, Llc System and method for music composition
JP5759976B2 (ja) * 2009-03-20 2015-08-05 ハンミ・サイエンス・カンパニー・リミテッド 位置特異的な生理活性ポリペプチド結合体の調製方法
CN101870728A (zh) * 2009-04-23 2010-10-27 派格生物医药(苏州)有限公司 新型Exendin变体及其缀合物
CN101559041B (zh) * 2009-05-19 2014-01-15 中国科学院过程工程研究所 粒径均一的多肽药物缓释微球或微囊制剂及制备方法
KR20120092611A (ko) * 2009-09-30 2012-08-21 글락소 그룹 리미티드 연장된 반감기를 갖는 약물 융합체 및 컨쥬게이트
CN102397558B (zh) * 2010-09-09 2013-08-14 中国人民解放军军事医学科学院毒物药物研究所 Exendin-4类似物的定位聚乙二醇化修饰物及其用途

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* Cited by examiner, † Cited by third party
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WO2007061148A1 (en) * 2005-11-24 2007-05-31 Pegsphere Co., Ltd. Site-specific peg conjugates of glp-1 and methods for production thereof
WO2008058461A1 (en) * 2006-11-14 2008-05-22 Shanghai Huayi Bio-Lab Co., Ltd. Peg modified exendin or exendin analog and compositions and use thereof
WO2008130066A1 (en) * 2007-04-20 2008-10-30 Kang Choon Lee Mono modified exendin with polyethylene glycol or its derivatives and uses thereof

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Also Published As

Publication number Publication date
EP2692730A1 (en) 2014-02-05
WO2012130015A1 (zh) 2012-10-04
JP2014510735A (ja) 2014-05-01
JP6297969B2 (ja) 2018-03-20
BR112013024706B1 (pt) 2022-10-11
CA2829122A1 (en) 2012-10-04
BR112013024706A2 (pt) 2016-09-06
EP2692730A4 (en) 2015-04-01
US20140142037A1 (en) 2014-05-22
CN106928341B (zh) 2021-06-01
KR20140033023A (ko) 2014-03-17
KR102005385B1 (ko) 2019-07-30
CA2829122C (en) 2022-05-03
RU2625015C2 (ru) 2017-07-11
CN106928341A (zh) 2017-07-07
AU2012237899A1 (en) 2013-09-19
CN102718868A (zh) 2012-10-10
EP2692730B1 (en) 2018-11-14
RU2013147468A (ru) 2015-05-10

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