RU2625015C2 - Сайт-специфически монопегилированные аналоги эксендина и способ их получения - Google Patents

Сайт-специфически монопегилированные аналоги эксендина и способ их получения Download PDF

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RU2625015C2
RU2625015C2 RU2013147468A RU2013147468A RU2625015C2 RU 2625015 C2 RU2625015 C2 RU 2625015C2 RU 2013147468 A RU2013147468 A RU 2013147468A RU 2013147468 A RU2013147468 A RU 2013147468A RU 2625015 C2 RU2625015 C2 RU 2625015C2
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RU2013147468A
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RU2013147468A (ru
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Пэн ЮЭ
Peng Yue
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Шанхай Бенемае Фармасьютикал Корпорэйшн
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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)
  • 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)
RU2013147468A 2011-03-30 2012-03-05 Сайт-специфически монопегилированные аналоги эксендина и способ их получения RU2625015C2 (ru)

Applications Claiming Priority (4)

Application Number Priority Date Filing Date Title
CN1.201110078314.X2011 2011-03-30
CN201110078314.?2011 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
RU2013147468A RU2013147468A (ru) 2015-05-10
RU2625015C2 true RU2625015C2 (ru) 2017-07-11

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RU2013147468A RU2625015C2 (ru) 2011-03-30 2012-03-05 Сайт-специфически монопегилированные аналоги эксендина и способ их получения

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

Citations (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2007061148A1 (en) * 2005-11-24 2007-05-31 Pegsphere Co., Ltd. Site-specific peg conjugates of glp-1 and methods for production thereof
EA009366B1 (ru) * 2003-03-19 2007-12-28 Эли Лилли Энд Компани Связанные с полиэтиленгликолем соединения гпп-1
CN101125207A (zh) * 2006-11-14 2008-02-20 上海华谊生物技术有限公司 带有聚乙二醇基团的Exendin或其类似物及其制剂和用途
WO2008130666A2 (en) * 2007-04-20 2008-10-30 Master Key, Llc System and method for music composition
WO2010107256A2 (en) * 2009-03-20 2010-09-23 Hanmi Pharm. Co., Ltd. Method for preparing a site-specific physiologically active polypeptide conjugate

Family Cites Families (9)

* 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
WO2006037811A2 (en) * 2004-10-07 2006-04-13 Novo Nordisk A/S Protracted exendin-4 compounds
KR100890989B1 (ko) * 2006-06-01 2009-03-31 이강춘 폴리에틸렌글리콜 또는 이의 유도체로 단일 수식된 엑센딘,이의 제조방법 및 이의 용도
WO2008130066A1 (en) * 2007-04-20 2008-10-30 Kang Choon Lee Mono modified exendin with polyethylene glycol or its derivatives and uses thereof
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

Patent Citations (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EA009366B1 (ru) * 2003-03-19 2007-12-28 Эли Лилли Энд Компани Связанные с полиэтиленгликолем соединения гпп-1
WO2007061148A1 (en) * 2005-11-24 2007-05-31 Pegsphere Co., Ltd. Site-specific peg conjugates of glp-1 and methods for production thereof
CN101125207A (zh) * 2006-11-14 2008-02-20 上海华谊生物技术有限公司 带有聚乙二醇基团的Exendin或其类似物及其制剂和用途
WO2008130666A2 (en) * 2007-04-20 2008-10-30 Master Key, Llc System and method for music composition
WO2010107256A2 (en) * 2009-03-20 2010-09-23 Hanmi Pharm. Co., Ltd. Method for preparing a site-specific physiologically active polypeptide conjugate

Non-Patent Citations (1)

* Cited by examiner, † Cited by third party
Title
KUBETZKO S. et al., Protein PEGylation Decreases Observed Target Association Rates via a Dual Blocking Mechanism, Mol. Pharm., 2005, v. 68, p. 1439-1454. *

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
CA2829122C (en) 2022-05-03
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
CN102718868A (zh) 2012-10-10
AU2012237899B2 (en) 2017-04-13

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