JP6297969B2 - 部位特異的モノｐｅｇ化エキセンジン類似体およびその調製方法 - Google Patents

部位特異的モノｐｅｇ化エキセンジン類似体およびその調製方法 Download PDF

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JP6297969B2
JP6297969B2 JP2014501409A JP2014501409A JP6297969B2 JP 6297969 B2 JP6297969 B2 JP 6297969B2 JP 2014501409 A JP2014501409 A JP 2014501409A JP 2014501409 A JP2014501409 A JP 2014501409A JP 6297969 B2 JP6297969 B2 JP 6297969B2
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JP2014510735A (ja
JP2014510735A5 (OSRAM
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鵬 岳
鵬 岳
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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
    • 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
    • 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
    • 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)
JP2014501409A 2011-03-30 2012-03-05 部位特異的モノｐｅｇ化エキセンジン類似体およびその調製方法 Active JP6297969B2 (ja)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
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
CN201110078314.X 2011-03-30
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 (3)

Publication Number Publication Date
JP2014510735A JP2014510735A (ja) 2014-05-01
JP2014510735A5 JP2014510735A5 (OSRAM) 2015-04-23
JP6297969B2 true JP6297969B2 (ja) 2018-03-20

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JP2014501409A Active JP6297969B2 (ja) 2011-03-30 2012-03-05 部位特異的モノｐｅｇ化エキセンジン類似体およびその調製方法

Country Status (10)

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

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* 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
SG10201705097PA (en) 2012-12-21 2017-07-28 Sanofi Sa Functionalized exendin-4 derivatives
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
EP3080154B1 (en) 2013-12-13 2018-02-07 Sanofi Dual glp-1/gip receptor agonists
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
WO2015086728A1 (en) 2013-12-13 2015-06-18 Sanofi Exendin-4 peptide analogues as dual glp-1/gip receptor agonists
KR101768446B1 (ko) 2014-03-21 2017-08-17 애니젠 주식회사 신규한 엑세나타이드 유사체 및 그의 용도
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
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
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
AR105284A1 (es) 2015-07-10 2017-09-20 Sanofi Sa Derivados de exendina-4 como agonistas peptídicos duales específicos de los receptores de glp-1 / glucagón
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

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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
WO2004065412A1 (en) * 2003-01-18 2004-08-05 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
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
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
DK2408800T3 (en) * 2009-03-20 2016-08-29 Hanmi Science Co Ltd A process for the preparation of a site-specific conjugate of a physiologically active polypeptide
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
SG10201406063XA (en) * 2009-09-30 2014-11-27 Glaxo Group Ltd Drug fusions and conjugates with extended half life
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
AU2012237899A1 (en) 2013-09-19
JP2014510735A (ja) 2014-05-01
BR112013024706B1 (pt) 2022-10-11
KR20140033023A (ko) 2014-03-17
US20140142037A1 (en) 2014-05-22
CA2829122A1 (en) 2012-10-04
EP2692730A1 (en) 2014-02-05
CN102718868A (zh) 2012-10-10
AU2012237899B2 (en) 2017-04-13
EP2692730A4 (en) 2015-04-01
RU2625015C2 (ru) 2017-07-11
CN106928341B (zh) 2021-06-01
CA2829122C (en) 2022-05-03
CN106928341A (zh) 2017-07-07
WO2012130015A1 (zh) 2012-10-04
EP2692730B1 (en) 2018-11-14
KR102005385B1 (ko) 2019-07-30
BR112013024706A2 (pt) 2016-09-06
RU2013147468A (ru) 2015-05-10

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