HRP20100543T1 - Glp-1 pegilirani spojevi - Google Patents

Glp-1 pegilirani spojevi Download PDF

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Publication number
HRP20100543T1
HRP20100543T1 HR20100543T HRP20100543T HRP20100543T1 HR P20100543 T1 HRP20100543 T1 HR P20100543T1 HR 20100543 T HR20100543 T HR 20100543T HR P20100543 T HRP20100543 T HR P20100543T HR P20100543 T1 HRP20100543 T1 HR P20100543T1
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HR
Croatia
Prior art keywords
compound according
pegylated glp
glp
val
cys46
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HR20100543T
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English (en)
Inventor
Zhang Lianshan
Mark Vick Andrew
Lee Junior Millican Rohn
Philip Mayer John
Glaesner Wolfgang
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Eli Lilly And Company
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Publication of HRP20100543T1 publication Critical patent/HRP20100543T1/hr

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    • 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
    • C07K14/605—Glucagons
    • 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
    • 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
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • 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
    • 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
    • A61P3/04—Anorexiants; Antiobesity agents
    • 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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Organic Chemistry (AREA)
  • Medicinal Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Diabetes (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Endocrinology (AREA)
  • Zoology (AREA)
  • Proteomics, Peptides & Aminoacids (AREA)
  • Obesity (AREA)
  • Epidemiology (AREA)
  • Toxicology (AREA)
  • Hematology (AREA)
  • Gastroenterology & Hepatology (AREA)
  • Biochemistry (AREA)
  • Biophysics (AREA)
  • Genetics & Genomics (AREA)
  • Molecular Biology (AREA)
  • Emergency Medicine (AREA)
  • Child & Adolescent Psychology (AREA)
  • Peptides Or Proteins (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Medicinal Preparation (AREA)
  • Polyethers (AREA)

Abstract

Di-PEGilirani GLP-1 spoj s aminokiselinskim slijedom formule: naznačen time štoXaa8 je: D-Ala, Gly, Val, Leu, Ile, Ser ili Thr; Xaa22 je: Gly, Glu, Asp ili Lys; Xaa33 je: Val ili Ile; Xaa46 je: Cys ili Cys-NH2;te gdje jedna molekula PEG je kovalentno vezana na Cys45, a jedna molekula PEG je kovalentno vezana na Cys46 ili Cys46-NH2.Patent sadrži još 12 patentnih zahtjeva.

Claims (13)

1. Di-PEGilirani GLP-1 spoj s aminokiselinskim slijedom formule: [image] naznačen time što Xaa8 je: D-Ala, Gly, Val, Leu, Ile, Ser ili Thr; Xaa22 je: Gly, Glu, Asp ili Lys; Xaa33 je: Val ili Ile; Xaa46 je: Cys ili Cys-NH2; te gdje jedna molekula PEG je kovalentno vezana na Cys45, a jedna molekula PEG je kovalentno vezana na Cys46 ili Cys46-NH2.
2. Di-PEGilirani GLP-1 spoj u skladu s patentnim zahtjevom 1, naznačen time što Xaa8 je Gly ili Val, a Xaa22 je Gly ili Glu.
3. Di-PEGilirani GLP-1 spoj u skladu s patentnim zahtjevom 1 ili zahtjevom 2, naznačen time što Xaa8 je Val, a Xaa22 je Glu.
4. Di-PEGilirani GLP-1 spoj u skladu s bilo kojim od patentnih zahtjeva 1 do 3, naznačen time što Xaa8 je Val, Xaa22 je Glu, Xaa33 je Ile, i Xaa46 je Cys-NH2.
5. Di-PEGilirani GLP-1 spoj u skladu s bilo kojim od patentnih zahtjeva 1 do 4, naznačen time što molekule PEG imaju molekulsku težinu između 5.000 i 40.000 Da.
6. Di-PEGilirani GLP-1 spoj u skladu s bilo kojim od patentnih zahtjeva 1 do 4, naznačen time što molekule PEG imaju molekulsku težinu između 20.000 i 60.000 Da.
7. Di-PEGilirani GLP-1 spoj u skladu s bilo kojim od patentnih zahtjeva 1 do 4, naznačen time što molekule PEG imaju molekulsku težinu između 20.000 i 40.000 Da.
8. Di-PEGilirani GLP-1 spoj u skladu s bilo kojim od patentnih zahtjeva 1 do 4, naznačen time što svaka od molekula PEG upotrijebljena u reakciji PEGilacije je 20.000 Da velika nerazgranati metoksi-PEG-maleimid.
9. Di-PEGilirani GLP-1 spoj u skladu s bilo kojim od prethodnih patentnih zahtjeva, naznačen time što molekule PEG su vezane istodobno.
10. Di-PEGilirani GLP-1 spoj u skladu s bilo kojim od prethodnih patentnih zahtjeva, naznačen time što spojnica koju čine PEGilacijska mjesta Cys45 i Cys46 ili Cys46-NH2 je vezana na C-kraj GLP-1 spoja.
11. Di-PEGilirani GLP-1 spoj u skladu s bilo kojim od patentnih zahtjeva 1 do 10, naznačen time što je namijenjen upotrebi kao medikament.
12. Di-PEGilirani GLP-1 spoj u skladu s bilo kojim od patentnih zahtjeva 1 do 10, naznačen time što je namijenjen upotrebi u liječenju dijabetesa neovisnog o inzulinu ili pretilosti.
13. Upotreba di-PEGiliranog GLP-1 spoja u skladu s bilo kojim od patentnih zahtjeva 1 do 10, naznačena time što je navedeni spoj namijenjen proizvodnji medikamenta za liječenje dijabetesa neovisnog o inzulinu ili pretilosti.
HR20100543T 2005-05-13 2010-10-05 Glp-1 pegilirani spojevi HRP20100543T1 (hr)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US68068805P 2005-05-13 2005-05-13
PCT/US2006/018284 WO2006124529A1 (en) 2005-05-13 2006-05-11 Glp-1 pegylated compounds

Publications (1)

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HRP20100543T1 true HRP20100543T1 (hr) 2010-11-30

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Country Status (25)

Country Link
US (1) US8183340B2 (hr)
EP (1) EP1881850B1 (hr)
JP (2) JP5225074B2 (hr)
KR (1) KR101011081B1 (hr)
CN (1) CN101166545B (hr)
AT (1) ATE482724T1 (hr)
AU (1) AU2006247734B2 (hr)
BR (1) BRPI0609676A2 (hr)
CA (1) CA2608311C (hr)
CY (1) CY1110853T1 (hr)
DE (1) DE602006017202D1 (hr)
DK (1) DK1881850T3 (hr)
EA (1) EA012442B1 (hr)
ES (1) ES2350852T3 (hr)
HR (1) HRP20100543T1 (hr)
IL (1) IL186772A0 (hr)
ME (1) ME02786B (hr)
MX (1) MX2007014052A (hr)
NO (1) NO20076415L (hr)
PL (1) PL1881850T3 (hr)
PT (1) PT1881850E (hr)
RS (1) RS51637B (hr)
SI (1) SI1881850T1 (hr)
UA (1) UA90896C2 (hr)
WO (1) WO2006124529A1 (hr)

Families Citing this family (77)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
DK1965823T3 (en) 2005-11-04 2016-08-22 Glaxosmithkline Llc Corp Service Company Methods of administering hypoglycemics
ES2572952T3 (es) 2005-11-07 2016-06-03 Indiana University Research And Technology Corporation Análogos de glucagón que muestran solubilidad y estabilidad fisiológicas
ES2390286T3 (es) 2005-12-16 2012-11-08 Nektar Therapeutics Conjugados poliméricos de GLP-1
WO2008019147A2 (en) 2006-08-04 2008-02-14 Amylin Pharmaceuticals, Inc. Use of exendins, exendin agonists and glp-1 receptor agonists for altering the concentration of fibrinogen
BRPI0715160A2 (pt) 2006-08-08 2013-06-11 Sanofi Aventis imidazolidina-2,4-dionas substituÍdas por arilamimoaril-alquil-, processo para preparÁ-las, medicamentos compeendendo estes compostos, e seu uso
JP2008169195A (ja) 2007-01-05 2008-07-24 Hanmi Pharmaceutical Co Ltd キャリア物質を用いたインスリン分泌ペプチド薬物結合体
WO2008086086A2 (en) 2007-01-05 2008-07-17 Indiana University Research And Technology Corporation Glucagon analogs exhibiting enhanced solubility in physiological ph buffers
CA2677932A1 (en) 2007-02-15 2008-08-21 Indiana University Research And Technology Corporation Glucagon/glp-1 receptor co-agonists
GB2448895A (en) * 2007-05-01 2008-11-05 Activotec Spp Ltd GLP-1 like compounds and uses thereof
US9353170B2 (en) 2007-06-08 2016-05-31 Sanofi-Aventis Deutschland Gmbh Long-acting transient polymer conjugates of exendin
JP2010535781A (ja) * 2007-08-03 2010-11-25 イーライ リリー アンド カンパニー 肥満に対する処置
EP2025674A1 (de) 2007-08-15 2009-02-18 sanofi-aventis Substituierte Tetrahydronaphthaline, Verfahren zu ihrer Herstellung und ihre Verwendung als Arzneimittel
CA2707861A1 (en) 2007-10-30 2009-05-07 Indiana University Research And Technology Corporation Glucagon antagonists
MX2010004298A (es) 2007-10-30 2010-05-03 Univ Indiana Res & Tech Corp Compuestos que exhiben actividad antagonista de glucagon y agonista de glp-1.
DE102007063671A1 (de) 2007-11-13 2009-06-25 Sanofi-Aventis Deutschland Gmbh Neue kristalline Diphenylazetidinonhydrate, diese Verbindungen enthaltende Arzneimittel und deren Verwendung
US20090149673A1 (en) * 2007-12-05 2009-06-11 Semprus Biosciences Corp. Synthetic non-fouling amino acids
TWI451876B (zh) * 2008-06-13 2014-09-11 Lilly Co Eli 聚乙二醇化之離脯胰島素化合物
CN102105159B (zh) 2008-06-17 2015-07-08 印第安纳大学研究及科技有限公司 基于gip的混合激动剂用于治疗代谢紊乱和肥胖症
PE20100255A1 (es) 2008-06-17 2010-04-25 Univ Indiana Res & Tech Corp Co-agonistas del receptor de glucagon/glp-1
US8450270B2 (en) 2008-06-17 2013-05-28 Indiana University Research And Technology Corporation Glucagon analogs exhibiting enhanced solubility and stability in physiological pH buffers
WO2010003624A2 (en) 2008-07-09 2010-01-14 Sanofi-Aventis Heterocyclic compounds, processes for their preparation, medicaments comprising these compounds, and the use thereof
IT1392655B1 (it) * 2008-11-20 2012-03-16 Bio Ker S R L Site-specific monoconjugated insulinotropic glp-1 peptides.
WO2010068601A1 (en) 2008-12-08 2010-06-17 Sanofi-Aventis A crystalline heteroaromatic fluoroglycoside hydrate, processes for making, methods of use and pharmaceutical compositions thereof
BRPI0922969A2 (pt) 2008-12-19 2019-09-24 Univ Indiana Res & Tech Corp pró-farmaco de amida baseado na superfamília de glucagon peptídeo.
IN2012DN00377A (hr) 2009-06-16 2015-08-21 Univ Indiana Res & Tech Corp
CN101993485B (zh) * 2009-08-20 2013-04-17 重庆富进生物医药有限公司 促胰岛素分泌肽类似物同源二聚体及其用途
EP2470552B1 (en) 2009-08-26 2013-11-13 Sanofi Novel crystalline heteroaromatic fluoroglycoside hydrates, pharmaceuticals comprising these compounds and their use
PL2513140T3 (pl) 2009-12-16 2016-04-29 Novo Nordisk As Podwójnie acylowane pochodne glp-1
EP2512503A4 (en) 2009-12-18 2013-08-21 Univ Indiana Res & Tech Corp COAGONISTS OF GLUCAGON / GLP-1 RECEPTOR
AR079344A1 (es) 2009-12-22 2012-01-18 Lilly Co Eli Analogo peptidico de oxintomodulina, composicion farmaceutica que lo comprende y uso para preparar un medicamento util para tratar diabetes no insulinodependiente y/u obesidad
AR079345A1 (es) 2009-12-22 2012-01-18 Lilly Co Eli Analogo peptidico de oxintomodulina
MX2012008603A (es) 2010-01-27 2013-01-25 Univ Indiana Res & Tech Corp Conjugados de antagonista de glucagon-agonista de gip y composiciones para el tratamiento de desordenes metabolicos y obesidad.
WO2011107494A1 (de) 2010-03-03 2011-09-09 Sanofi Neue aromatische glykosidderivate, diese verbindungen enthaltende arzneimittel und deren verwendung
DE102010015123A1 (de) 2010-04-16 2011-10-20 Sanofi-Aventis Deutschland Gmbh Benzylamidische Diphenylazetidinone, diese Verbindungen enthaltende Arzneimittel und deren Verwendung
CN102946875A (zh) 2010-05-05 2013-02-27 贝林格尔.英格海姆国际有限公司 组合疗法
ES2661228T3 (es) 2010-05-13 2018-03-28 Indiana University Research And Technology Corporation Péptidos de la superfamilia de glucagón que muestran actividad de receptor nuclear de hormona
CA2797089A1 (en) 2010-05-13 2011-11-17 Indiana University Research And Technology Corporation Glucagon superfamily peptides exhibiting g protein-coupled receptor activity
WO2011143788A1 (en) * 2010-05-17 2011-11-24 Zhejiang Beta Pharma Inc. Novel glucagon like peptide analogs, composition, and method of use
EP2582709B1 (de) 2010-06-18 2018-01-24 Sanofi Azolopyridin-3-on-derivate als inhibitoren von lipasen und phospholipasen
US8530413B2 (en) 2010-06-21 2013-09-10 Sanofi Heterocyclically substituted methoxyphenyl derivatives with an oxo group, processes for preparation thereof and use thereof as medicaments
RU2580317C2 (ru) 2010-06-24 2016-04-10 Индиана Юниверсити Рисерч Энд Текнолоджи Корпорейшн Пептидные пролекарства, принадлежащие к суперсемейству амид-содержащих глюкагонов
TW201215388A (en) 2010-07-05 2012-04-16 Sanofi Sa (2-aryloxyacetylamino)phenylpropionic acid derivatives, processes for preparation thereof and use thereof as medicaments
TW201215387A (en) 2010-07-05 2012-04-16 Sanofi Aventis Spirocyclically substituted 1,3-propane dioxide derivatives, processes for preparation thereof and use thereof as a medicament
TW201221505A (en) 2010-07-05 2012-06-01 Sanofi Sa Aryloxyalkylene-substituted hydroxyphenylhexynoic acids, process for preparation thereof and use thereof as a medicament
WO2012088116A2 (en) 2010-12-22 2012-06-28 Indiana University Research And Technology Corporation Glucagon analogs exhibiting gip receptor activity
US20130035281A1 (en) 2011-02-09 2013-02-07 Boehringer Ingelheim International Gmbh Pharmaceutical composition, methods for treating and uses thereof
US8828994B2 (en) 2011-03-08 2014-09-09 Sanofi Di- and tri-substituted oxathiazine derivatives, method for the production thereof, use thereof as medicine and drug containing said derivatives and use thereof
US8871758B2 (en) 2011-03-08 2014-10-28 Sanofi Tetrasubstituted oxathiazine derivatives, method for producing them, their use as medicine and drug containing said derivatives and the use thereof
WO2012120055A1 (de) 2011-03-08 2012-09-13 Sanofi Di- und trisubstituierte oxathiazinderivate, verfahren zu deren herstellung, ihre verwendung als medikament sowie sie enthaltendes arzneimittel und deren verwendung
WO2012120052A1 (de) 2011-03-08 2012-09-13 Sanofi Mit carbozyklen oder heterozyklen substituierte oxathiazinderivate, verfahren zu deren herstellung, diese verbindungen enthaltende arzneimittel und deren verwendung
US8828995B2 (en) 2011-03-08 2014-09-09 Sanofi Branched oxathiazine derivatives, method for the production thereof, use thereof as medicine and drug containing said derivatives and use thereof
CN102786590A (zh) * 2011-05-19 2012-11-21 江苏豪森药业股份有限公司 分枝型peg修饰的glp-1类似物及其可药用盐
DK2723367T3 (en) 2011-06-22 2017-07-17 Univ Indiana Res & Tech Corp Glucagon / GLP-1 receptor-CO-AGONISTS
BR112013032717A2 (pt) 2011-06-22 2017-01-24 Univ Indiana Res & Tech Corp coagonistas do receptor de glucagon/glp-1
US20130035298A1 (en) 2011-07-08 2013-02-07 Boehringer Ingelheim International Gmbh Pharmaceutical composition, methods for treating and uses thereof
EP2567959B1 (en) 2011-09-12 2014-04-16 Sanofi 6-(4-hydroxy-phenyl)-3-styryl-1h-pyrazolo[3,4-b]pyridine-4-carboxylic acid amide derivatives as kinase inhibitors
WO2013037390A1 (en) 2011-09-12 2013-03-21 Sanofi 6-(4-hydroxy-phenyl)-3-styryl-1h-pyrazolo[3,4-b]pyridine-4-carboxylic acid amide derivatives as kinase inhibitors
WO2013045413A1 (en) 2011-09-27 2013-04-04 Sanofi 6-(4-hydroxy-phenyl)-3-alkyl-1h-pyrazolo[3,4-b]pyridine-4-carboxylic acid amide derivatives as kinase inhibitors
WO2013074910A1 (en) 2011-11-17 2013-05-23 Indiana University Research And Technology Corporation Glucagon superfamily peptides exhibiting glucocorticoid receptor activity
US20130303554A1 (en) 2012-05-14 2013-11-14 Boehringer Ingelheim International Gmbh Use of a dpp-4 inhibitor in sirs and/or sepsis
EP2849755A1 (en) 2012-05-14 2015-03-25 Boehringer Ingelheim International GmbH A xanthine derivative as dpp -4 inhibitor for use in the treatment of podocytes related disorders and/or nephrotic syndrome
WO2013174768A1 (en) 2012-05-24 2013-11-28 Boehringer Ingelheim International Gmbh A xanthine derivative as dpp -4 inhibitor for use in the treatment of autoimmune diabetes, particularly lada
TWI599575B (zh) 2012-06-21 2017-09-21 印第安納大學科技研究公司 表現ｇｉｐ受體活性之胰高血糖素類似物
CN102827270A (zh) * 2012-09-13 2012-12-19 无锡和邦生物科技有限公司 一种聚乙二醇化艾塞那肽衍生物及其用途
CN105142621A (zh) 2012-10-24 2015-12-09 国家健康科学研究所 用于预防或治疗糖尿病和促进β-细胞存活的TPL2激酶抑制剂
CN105377306B (zh) 2013-06-20 2020-03-17 诺和诺德股份有限公司 Glp-1衍生物和其用途
JP6139712B2 (ja) 2013-07-04 2017-05-31 ノヴォ ノルディスク アー／エス Ｇｌｐ−１様ペプチドの誘導体及びその使用
WO2015081891A1 (en) 2013-12-06 2015-06-11 Baikang (Suzhou) Co., Ltd Bioreversable promoieties for nitrogen-containing and hydroxyl-containing drugs
US11572398B2 (en) 2014-11-27 2023-02-07 Novo Nordisk A/S GLP-1 derivatives and uses thereof
US10046058B2 (en) 2014-12-02 2018-08-14 Rezolute, Inc. Use of hydrophobic organic acids to increase hydrophobicity of proteins and protein conjugates
EP3233898A1 (en) 2014-12-17 2017-10-25 Novo Nordisk A/S Glp-1 derivatives and uses thereof
ES2805743T3 (es) 2015-03-24 2021-02-15 Inst Nat Sante Rech Med Método y composición farmacéutica para uso en el tratamiento de la diabetes
CN107708679A (zh) 2015-06-04 2018-02-16 安特里阿比奥有限公司 用于制备位点特异性蛋白质偶联物的胺聚乙二醇化方法
CN106699870A (zh) * 2016-12-14 2017-05-24 江苏师范大学 长效非洲爪蟾胰高血糖素样肽‑1（glp‑1）类似物及其应用
WO2019106193A1 (en) 2017-12-01 2019-06-06 University Of Copenhagen Peptide hormone with one or more o-glycans
CN110964116A (zh) * 2018-09-26 2020-04-07 北京辅仁瑞辉生物医药研究院有限公司 GLP1-Fc融合蛋白及其缀合物
CN114478744A (zh) * 2020-11-13 2022-05-13 成都奥达生物科技有限公司 一种长效glp-1拮抗剂

Family Cites Families (25)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US4179337A (en) * 1973-07-20 1979-12-18 Davis Frank F Non-immunogenic polypeptides
US4343898A (en) 1980-02-11 1982-08-10 Novo Industri A/S Process for preparing esters of human insulin
US5120712A (en) 1986-05-05 1992-06-09 The General Hospital Corporation Insulinotropic hormone
US5445090A (en) 1991-07-25 1995-08-29 Mim Industries, Inc. Interchangeable clamp for use in a sewing machine
US5446090A (en) 1993-11-12 1995-08-29 Shearwater Polymers, Inc. Isolatable, water soluble, and hydrolytically stable active sulfones of poly(ethylene glycol) and related polymers for modification of surfaces and molecules
US5932462A (en) 1995-01-10 1999-08-03 Shearwater Polymers, Inc. Multiarmed, monofunctional, polymer for coupling to molecules and surfaces
US6277819B1 (en) 1996-08-30 2001-08-21 Eli Lilly And Company Use of GLP-1 or analogs in treatment of myocardial infarction
US6006753A (en) 1996-08-30 1999-12-28 Eli Lilly And Company Use of GLP-1 or analogs to abolish catabolic changes after surgery
US6214966B1 (en) 1996-09-26 2001-04-10 Shearwater Corporation Soluble, degradable poly(ethylene glycol) derivatives for controllable release of bound molecules into solution
UA65549C2 (uk) 1996-11-05 2004-04-15 Елі Ліллі Енд Компані Спосіб регулювання ожиріння шляхом периферійного введення аналогів та похідних glp-1 (варіанти) та фармацевтична композиція
US6448369B1 (en) 1997-11-06 2002-09-10 Shearwater Corporation Heterobifunctional poly(ethylene glycol) derivatives and methods for their preparation
PT1061954E (pt) 1998-03-12 2004-10-29 Nektar Therapeutics Al Corp Derivados de poli(etileno glicol) com grupos reactivos proximos
SE9802080D0 (sv) 1998-06-11 1998-06-11 Hellstroem Pharmaceutical composition for the treatment of functional dyspepsia and/or irritable bowel syndrome and new use of substances therein
EP1306091A3 (en) 1998-07-31 2003-05-21 Novo Nordisk A/S Stimulation of beta cell proliferation
MY155270A (en) 1998-09-24 2015-09-30 Lilly Co Eli Use of glp-1 or analogs in treatment of stroke
DE60026073T2 (de) 1999-12-22 2006-09-28 Nektar Therapeutics Al, Corp., Huntsville Sterisch gehinderte derivate von wasserlöslichen polymeren
US6413507B1 (en) 1999-12-23 2002-07-02 Shearwater Corporation Hydrolytically degradable carbamate derivatives of poly (ethylene glycol)
EP1695983B1 (en) * 2000-06-16 2009-03-04 Eli Lilly & Company Glucagon-like peptide-1 analogs
US6436386B1 (en) 2000-11-14 2002-08-20 Shearwater Corporation Hydroxyapatite-targeting poly (ethylene glycol) and related polymers
UA81897C2 (uk) * 2000-12-07 2008-02-25 Эли Лилли Энд Компани Гетерологічний пептидильований глюкагон-1-подібний білок та його застосування для для виготовлення лікарського засобу для лікування пацієнтів, що страждають на ожиріння та/або інсулінонезалежний діабет
AU2003200839B2 (en) * 2002-01-08 2008-12-11 Eli Lilly And Company Extended glucagon-like peptide-1 analogs
JP2006520818A (ja) * 2003-03-19 2006-09-14 イーライ リリー アンド カンパニー ポリエチレングリコール結合ｇｌｐ−１化合物
CN1802386B (zh) * 2003-06-12 2010-12-15 伊莱利利公司 Glp-1类似物融合蛋白质
MXPA05013564A (es) * 2003-06-12 2006-03-09 Lilly Co Eli Proteinas de fusion.
CN1586625A (zh) * 2004-07-21 2005-03-02 上海第二医科大学附属瑞金医院 用于肿瘤显像和治疗的联合物及其制备方法

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