CA2829122C - 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
CA2829122C
CA2829122C CA2829122A CA2829122A CA2829122C CA 2829122 C CA2829122 C CA 2829122C CA 2829122 A CA2829122 A CA 2829122A CA 2829122 A CA2829122 A CA 2829122A CA 2829122 C CA2829122 C CA 2829122C
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French (fr)
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CA2829122A1 (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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    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K47/00Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
    • A61K47/50Medicinal 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
    • A61K47/51Medicinal 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
    • A61K47/56Medicinal 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
    • A61K47/59Medicinal 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
    • A61K47/60Medicinal 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07KPEPTIDES
    • C07K14/00Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof
    • C07K14/435Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof from animals; from humans
    • C07K14/575Hormones
    • C07K14/57563Vasoactive intestinal peptide [VIP]; Related peptides
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07KPEPTIDES
    • C07K1/00General methods for the preparation of peptides, i.e. processes for the organic chemical preparation of peptides or proteins of any length
    • C07K1/06General 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00Drugs for disorders of the metabolism
    • A61P3/08Drugs for disorders of the metabolism for glucose homeostasis
    • A61P3/10Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07KPEPTIDES
    • C07K14/00Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof
    • C07K14/435Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof from animals; from humans
    • C07K14/575Hormones
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K38/00Medicinal preparations containing peptides
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K38/00Medicinal preparations containing peptides
    • A61K38/16Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof
    • A61K38/17Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof from animals; from humans
    • A61K38/22Hormones
    • YGENERAL 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
    • Y02TECHNOLOGIES OR APPLICATIONS FOR MITIGATION OR ADAPTATION AGAINST CLIMATE CHANGE
    • Y02PCLIMATE CHANGE MITIGATION TECHNOLOGIES IN THE PRODUCTION OR PROCESSING OF GOODS
    • Y02P20/00Technologies relating to chemical industry
    • Y02P20/50Improvements relating to the production of bulk chemicals
    • Y02P20/55Design 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)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Diabetes (AREA)
  • Epidemiology (AREA)
  • Hematology (AREA)
  • Emergency Medicine (AREA)
  • Obesity (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Analytical Chemistry (AREA)
  • Peptides Or Proteins (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Medicinal Preparation (AREA)
CA2829122A 2011-03-30 2012-03-05 Site-directed mono-substituted pegylated exendin analog and preparation method therefor Active CA2829122C (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
CA2829122A1 CA2829122A1 (en) 2012-10-04
CA2829122C true CA2829122C (en) 2022-05-03

Family

ID=46929417

Family Applications (1)

Application Number Title Priority Date Filing Date
CA2829122A Active CA2829122C (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)

Families Citing this family (15)

* Cited by examiner, † Cited by third party
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
PT2934568T (pt) 2012-12-21 2018-01-04 Sanofi Sa Agonistas duplos de glp1/gip ou trigonais de glp1/gip/glucagina
TW201609799A (zh) 2013-12-13 2016-03-16 賽諾菲公司 雙重glp-1/gip受體促效劑
TW201609795A (zh) 2013-12-13 2016-03-16 賽諾菲公司 作為雙重glp-1/gip受體促效劑的艾塞那肽-4(exendin-4)胜肽類似物
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
TW201609796A (zh) 2013-12-13 2016-03-16 賽諾菲公司 非醯化之艾塞那肽-4(exendin-4)胜肽類似物
KR101768446B1 (ko) * 2014-03-21 2017-08-17 애니젠 주식회사 신규한 엑세나타이드 유사체 및 그의 용도
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
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
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
CN115703825A (zh) * 2021-08-17 2023-02-17 派格生物医药(苏州)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

Family Cites Families (14)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
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
US7662915B2 (en) * 2003-01-18 2010-02-16 Pegsphere Co., Ltd. Peptides having protected amines of untargeted sites, methods for production thereof and of specifically conjugated PEG peptides using the same
BRPI0407936A (pt) * 2003-03-19 2006-02-21 Lilly Co Eli composto de glp-1 peguilado, método de estimular o receptor de glp-1 em um indivìduo, e, uso de composto glp-1 peguilado
WO2006037811A2 (en) * 2004-10-07 2006-04-13 Novo Nordisk A/S Protracted exendin-4 compounds
WO2007061148A1 (en) * 2005-11-24 2007-05-31 Pegsphere Co., Ltd. Site-specific peg conjugates of glp-1 and methods for production thereof
KR100890989B1 (ko) * 2006-06-01 2009-03-31 이강춘 폴리에틸렌글리콜 또는 이의 유도체로 단일 수식된 엑센딘,이의 제조방법 및 이의 용도
CN102827284B (zh) * 2006-11-14 2015-07-29 上海仁会生物制药股份有限公司 带有聚乙二醇基团的Exendin或其类似物及其制剂和用途
WO2008130066A1 (en) * 2007-04-20 2008-10-30 Kang Choon Lee Mono modified exendin with polyethylene glycol or its derivatives and uses thereof
US7935877B2 (en) * 2007-04-20 2011-05-03 Master Key, Llc System and method for music composition
AU2010225523B2 (en) * 2009-03-20 2012-05-24 Hanmi Science Co., Ltd. Method for preparing a site-specific physiologically active polypeptide conjugate
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
BR112012007374A2 (pt) * 2009-09-30 2019-09-24 Glaxo Group Ltd composição, formulação oral, injetável, inalável ou nebulizável, e, ácido nucleico isolado ou recombinante
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

Also Published As

Publication number Publication date
CN106928341A (zh) 2017-07-07
RU2013147468A (ru) 2015-05-10
JP2014510735A (ja) 2014-05-01
CA2829122A1 (en) 2012-10-04
KR102005385B1 (ko) 2019-07-30
US20140142037A1 (en) 2014-05-22
BR112013024706B1 (pt) 2022-10-11
KR20140033023A (ko) 2014-03-17
AU2012237899A1 (en) 2013-09-19
CN106928341B (zh) 2021-06-01
BR112013024706A2 (pt) 2016-09-06
EP2692730B1 (en) 2018-11-14
WO2012130015A1 (zh) 2012-10-04
EP2692730A1 (en) 2014-02-05
JP6297969B2 (ja) 2018-03-20
EP2692730A4 (en) 2015-04-01
RU2625015C2 (ru) 2017-07-11
CN102718868A (zh) 2012-10-10
AU2012237899B2 (en) 2017-04-13

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