CN104144704B - Glp‑1受体激动剂肽胃泌素缀合物 - Google Patents

Glp‑1受体激动剂肽胃泌素缀合物 Download PDF

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Publication number
CN104144704B
CN104144704B CN201280060332.8A CN201280060332A CN104144704B CN 104144704 B CN104144704 B CN 104144704B CN 201280060332 A CN201280060332 A CN 201280060332A CN 104144704 B CN104144704 B CN 104144704B
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peptide
compound
peptide conjugate
8ado
solvate
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CN104144704A (zh
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雅各布·林德·托尔博尔格
特赖因·斯科夫隆德·吕厄·内鲁普
克尔德·福斯格劳
托尔文·奥斯特尔隆德
多尔特·伦纳特·克里斯藤森·阿尔姆霍尔特
隆娜·弗罗斯特·拉森
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Zealand Pharma AS
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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
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    • A61K38/17—Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof from animals; from humans
    • A61K38/22—Hormones
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  • Proteomics, Peptides & Aminoacids (AREA)
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CN201280060332.8A 2011-11-03 2012-11-02 Glp‑1受体激动剂肽胃泌素缀合物 Active CN104144704B (zh)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US201161555435P 2011-11-03 2011-11-03
US61/555,435 2011-11-03
PCT/EP2012/071766 WO2013064669A1 (en) 2011-11-03 2012-11-02 Glp-1 receptor agonist peptide gastrin conjugates

Publications (2)

Publication Number Publication Date
CN104144704A CN104144704A (zh) 2014-11-12
CN104144704B true CN104144704B (zh) 2018-03-23

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US (2) US9259477B2 (enExample)
EP (1) EP2773377B1 (enExample)
JP (1) JP6359972B2 (enExample)
KR (1) KR20140100947A (enExample)
CN (1) CN104144704B (enExample)
AR (1) AR088636A1 (enExample)
AU (1) AU2012331053A1 (enExample)
BR (1) BR112014010780A2 (enExample)
CA (1) CA2853884A1 (enExample)
EA (1) EA028951B9 (enExample)
MX (1) MX2014005351A (enExample)
TW (1) TW201326194A (enExample)
WO (1) WO2013064669A1 (enExample)

Families Citing this family (13)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
BR112012027759A2 (pt) 2010-04-27 2017-08-15 Zealand Pharma As Conjugados de peptídeos de agonistas de receptores glp-1 e gastrina e seu uso
AU2012331053A1 (en) 2011-11-03 2014-05-29 Zealand Pharma A/S GLP-1 receptor agonist peptide gastrin conjugates
CA2929459C (en) 2013-11-06 2022-05-03 Zealand Pharma A/S Gip-glp-1 dual agonist compounds and methods
KR102310392B1 (ko) 2013-11-06 2021-10-13 질랜드 파마 에이/에스 글루카곤-ｇｌｐ-1-ｇｉｐ 삼원 효능제 화합물
ES2883345T3 (es) 2014-10-29 2021-12-07 Zealand Pharma As Compuestos agonistas del GIP y métodos
WO2016168388A2 (en) 2015-04-14 2016-10-20 Palatin Technologies, Inc. Therapies for obesity, diabetes and related indications
CN109195983B (zh) * 2016-03-10 2022-05-17 深圳君圣泰生物技术有限公司 胰岛新生多肽和类似物的缀合物及其方法
CA3043151A1 (en) 2016-12-09 2018-06-14 Zealand Pharma A/S Acylated glp-1/glp-2 dual agonists
JP7046990B2 (ja) * 2017-06-29 2022-04-04 ユレカ・ソシエテ・ア・レスポンサビリテ・リミテ 医薬的特性が改善されたプロドラッグペプチド
CN109248323B (zh) * 2017-07-14 2023-09-08 杭州先为达生物科技有限公司 酰化的glp-1衍生物
CN109331173B (zh) * 2018-12-17 2021-05-07 中国医学科学院医学实验动物研究所 胃泌素-二氧化硅微球及其用途
CN112759640B (zh) * 2020-12-09 2023-09-08 江苏师范大学 一类glp-1/胃泌素受体双重激动剂及其应用
GB202308304D0 (en) * 2023-06-02 2023-07-19 Univ Ulster A fusion peptide for activation of the apj and/or glp-1 receptors

Citations (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN1961000A (zh) * 2004-02-11 2007-05-09 安米林药品公司 具有可选择特性的杂合多肽
WO2007095737A1 (en) * 2006-02-21 2007-08-30 Waratah Pharmaceuticals Inc. Combination therapy for the treatment of diabetes comprising an exendin agonist and a gastrin compound

Family Cites Families (100)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US4288627A (en) 1980-02-12 1981-09-08 Phillips Petroleum Company Oxidation of thiols employing cobalt molybdate/triethylamine catalyst
US5120712A (en) 1986-05-05 1992-06-09 The General Hospital Corporation Insulinotropic hormone
US5614492A (en) 1986-05-05 1997-03-25 The General Hospital Corporation Insulinotropic hormone GLP-1 (7-36) and uses thereof
US5118666A (en) 1986-05-05 1992-06-02 The General Hospital Corporation Insulinotropic hormone
US5545618A (en) 1990-01-24 1996-08-13 Buckley; Douglas I. GLP-1 analogs useful for diabetes treatment
WO1991011457A1 (en) 1990-01-24 1991-08-08 Buckley Douglas I Glp-1 analogs useful for diabetes treatment
WO1991017243A1 (en) 1990-05-09 1991-11-14 Novo Nordisk A/S A cellulase preparation comprising an endoglucanase enzyme
DK36392D0 (da) 1992-03-19 1992-03-19 Novo Nordisk As Anvendelse af kemisk forbindelse
US5846747A (en) 1992-03-25 1998-12-08 Novo Nordisk A/S Method for detecting glucagon-like peptide-1 antagonists and agonists
DK39892D0 (da) 1992-03-25 1992-03-25 Bernard Thorens Peptid
US5424286A (en) 1993-05-24 1995-06-13 Eng; John Exendin-3 and exendin-4 polypeptides, and pharmaceutical compositions comprising same
AU7531094A (en) 1993-08-24 1995-03-21 Novo Nordisk A/S Protracted glp-1
DE69426304T2 (de) 1993-09-07 2001-03-15 Amylin Pharmaceuticals, Inc. Methoden zur regulation der den magen und darm betreffenden motilitaet
US5705483A (en) 1993-12-09 1998-01-06 Eli Lilly And Company Glucagon-like insulinotropic peptides, compositions and methods
US5512549A (en) 1994-10-18 1996-04-30 Eli Lilly And Company Glucagon-like insulinotropic peptide analogs, compositions, and methods of use
US5523449A (en) 1995-05-17 1996-06-04 Bayer Corporation Process for preparing phosphorodichlorido-dithioates by reacting alkylmercaptans with phosphorus trichloride in the presence of sulfur
DK0915910T3 (da) 1996-06-05 2006-05-22 Roche Diagnostics Gmbh Exendin-analoger, fremgangsmåder til fremstilling deraf samt lægemidlter der indeholder disse
US6110703A (en) 1996-07-05 2000-08-29 Novo Nordisk A/S Method for the production of polypeptides
JP2001501593A (ja) 1996-08-08 2001-02-06 アミリン・ファーマシューティカルズ，インコーポレイテッド 胃腸運動を調節するための方法
US7235627B2 (en) 1996-08-30 2007-06-26 Novo Nordisk A/S Derivatives of GLP-1 analogs
US6268343B1 (en) 1996-08-30 2001-07-31 Novo Nordisk A/S Derivatives of GLP-1 analogs
US6277819B1 (en) 1996-08-30 2001-08-21 Eli Lilly And Company Use of GLP-1 or analogs in treatment of myocardial infarction
US6384016B1 (en) 1998-03-13 2002-05-07 Novo Nordisk A/S Stabilized aqueous peptide solutions
ES2283025T3 (es) 1996-08-30 2007-10-16 Novo Nordisk A/S Derivados de glp-1.1.
US6006753A (en) 1996-08-30 1999-12-28 Eli Lilly And Company Use of GLP-1 or analogs to abolish catabolic changes after surgery
US6458924B2 (en) 1996-08-30 2002-10-01 Novo Nordisk A/S Derivatives of GLP-1 analogs
CA2265454A1 (en) 1996-09-09 1998-03-19 Zealand Pharmaceuticals A/S Peptide prodrugs containing an alpha-hydroxyacid linker
ATE290014T1 (de) 1996-09-09 2005-03-15 Zealand Pharma As Festphasen-peptidsynthese
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
WO1998022577A1 (en) 1996-11-15 1998-05-28 Maria Grazia Masucci Fusion proteins having increased half-lives
EP1629849B2 (en) 1997-01-07 2017-10-04 Amylin Pharmaceuticals, LLC Pharmaceutical compositions comprising exendins and agonists thereof
US6410511B2 (en) 1997-01-08 2002-06-25 Amylin Pharmaceuticals, Inc. Formulations for amylin agonist peptides
US6136784A (en) 1997-01-08 2000-10-24 Amylin Pharmaceuticals, Inc. Amylin agonist pharmaceutical compositions containing insulin
EP0981611A1 (en) 1997-02-05 2000-03-01 1149336 Ontario Inc. Polynucleotides encoding proexendin, and methods and uses thereof
US5846937A (en) 1997-03-03 1998-12-08 1149336 Ontario Inc. Method of using exendin and GLP-1 to affect the central nervous system
WO1998050351A1 (en) 1997-05-07 1998-11-12 Max-Planck-Gesellschaft zur Förderung der Wissenschaften e.V., Berlin New cysteine derivatives, processes for their production, and pharmaceuticals containing them
CA2299425A1 (en) 1997-08-08 1999-02-18 Amylin Pharmaceuticals, Inc. Novel exendin agonist compounds
US7157555B1 (en) 1997-08-08 2007-01-02 Amylin Pharmaceuticals, Inc. Exendin agonist compounds
US7220721B1 (en) 1997-11-14 2007-05-22 Amylin Pharmaceuticals, Inc. Exendin agonist peptides
PT1032587E (pt) 1997-11-14 2008-04-21 Amylin Pharmaceuticals Inc Novos compostos agonistas de exendina
NZ504258A (en) 1997-11-14 2002-12-20 Amylin Pharmaceuticals Inc Exendin 3 and 4 agonist compounds for the treatment of diabetes
US7223725B1 (en) 1997-11-14 2007-05-29 Amylin Pharmaceuticals, Inc. Exendin agonist compounds
AU1617399A (en) 1997-12-05 1999-06-28 Eli Lilly And Company Glp-1 formulations
CA2320371C (en) 1998-02-13 2012-01-17 Amylin Pharmaceuticals, Inc. Inotropic and diuretic effects of exendin and glp-1
US6703359B1 (en) 1998-02-13 2004-03-09 Amylin Pharmaceuticals, Inc. Inotropic and diuretic effects of exendin and GLP-1
WO1999043708A1 (en) 1998-02-27 1999-09-02 Novo Nordisk A/S Glp-1 derivatives of glp-1 and exendin with protracted profile of action
DE69942307D1 (de) 1998-02-27 2010-06-10 Novo Nordisk As N-terminal veränderte glp-1 abkömmlinge
EP1950224A3 (en) 1998-03-09 2008-12-17 Zealand Pharma A/S Pharmacologically active peptide conjugates having a reduced tendency towards enzymatic hydrolysis
WO1999049788A1 (en) 1998-03-30 1999-10-07 Focus Surgery, Inc. Ablation system
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
ES2553108T3 (es) 1998-08-10 2015-12-04 The Government Of The United States Of America, As Represented By The Secretary, Department Of Health And Human Services Diferenciación de células no productoras de insulina en células productoras de insulina mediante GLP-1 o exendina-4 y utilizaciones de las mismas
AU6294899A (en) 1998-10-07 2000-04-26 Medical College Of Georgia Research Institute, Inc. Glucose-dependent insulinotropic peptide for use as an osteotropic hormone
US6284725B1 (en) 1998-10-08 2001-09-04 Bionebraska, Inc. Metabolic intervention with GLP-1 to improve the function of ischemic and reperfused tissue
US7399489B2 (en) 1999-01-14 2008-07-15 Amylin Pharmaceuticals, Inc. Exendin analog formulations
DK1143989T3 (da) 1999-01-14 2007-04-16 Amylin Pharmaceuticals Inc Exendiner til glucagonundertrykkelse
AU777564B2 (en) 1999-01-14 2004-10-21 Amylin Pharmaceuticals, Inc. Novel exendin agonist formulations and methods of administration thereof
US6451987B1 (en) 1999-03-15 2002-09-17 Novo Nordisk A/S Ion exchange chromatography of proteins and peptides
HUP0200297A3 (en) 1999-03-17 2002-09-30 Novo Nordisk As Method for acylating peptides and the glutaminic acid derivatives as acylating agents
US6451974B1 (en) 1999-03-17 2002-09-17 Novo Nordisk A/S Method of acylating peptides and novel acylating agents
US6271241B1 (en) 1999-04-02 2001-08-07 Neurogen Corporation Cycloalkyl and aryl fused aminoalkyl-imidazole derivatives: modulators and GLP-1 receptors
US6924264B1 (en) 1999-04-30 2005-08-02 Amylin Pharmaceuticals, Inc. Modified exendins and exendin agonists
WO2000066629A1 (en) 1999-04-30 2000-11-09 Amylin Pharmaceuticals, Inc. Modified exendins and exendin agonists
US6329336B1 (en) 1999-05-17 2001-12-11 Conjuchem, Inc. Long lasting insulinotropic peptides
US7601691B2 (en) 1999-05-17 2009-10-13 Conjuchem Biotechnologies Inc. Anti-obesity agents
US6506724B1 (en) 1999-06-01 2003-01-14 Amylin Pharmaceuticals, Inc. Use of exendins and agonists thereof for the treatment of gestational diabetes mellitus
US6344180B1 (en) 1999-06-15 2002-02-05 Bionebraska, Inc. GLP-1 as a diagnostic test to determine β-cell function and the presence of the condition of IGT and type II diabetes
US6528486B1 (en) 1999-07-12 2003-03-04 Zealand Pharma A/S Peptide agonists of GLP-1 activity
EP1076066A1 (en) 1999-07-12 2001-02-14 Zealand Pharmaceuticals A/S Peptides for lowering blood glucose levels
US6586438B2 (en) 1999-11-03 2003-07-01 Bristol-Myers Squibb Co. Antidiabetic formulation and method
NZ519752A (en) 2000-10-20 2005-04-29 Amylin Pharmaceuticals Inc Treatment of hibernating myocardium and diabetic cardiomyopathy with a GLP-1 peptide
GB0121709D0 (en) 2001-09-07 2001-10-31 Imp College Innovations Ltd Food inhibition agent
EP1837031B1 (en) 2002-06-07 2009-10-14 Waratah Pharmaceuticals, Inc. Compositions and methods for treating diabetes
ES2327328T3 (es) 2002-07-04 2009-10-28 Zealand Pharma A/S Glp-1 y procedimientos para el tratamiento de la diabetes.
RU2376314C2 (ru) 2002-10-02 2009-12-20 Зилэнд Фарма А/С Стабилизированные соединения эксендина-4
US7192922B2 (en) 2002-11-19 2007-03-20 Allegheny-Singer Research Institute Method of treating left ventricular dysfunction
US7623530B2 (en) 2003-11-20 2009-11-24 Nokia Corporation Indication of service flow termination by network control to policy decision function
CA2554458A1 (en) 2004-01-30 2005-08-11 Waratah Pharmaceuticals, Inc. The combined use of glp-1 agonists and gastrin for regulating blood glucose levels
US8076288B2 (en) 2004-02-11 2011-12-13 Amylin Pharmaceuticals, Inc. Hybrid polypeptides having glucose lowering activity
TW200716159A (en) * 2005-06-09 2007-05-01 Univ Maryland Method of use of antagonists of zonulin to prevent the loss of or to regenerate pancreatic cells
AU2007221366B2 (en) 2006-02-22 2012-08-23 Msd Italia S.R.L. Oxyntomodulin derivatives
NZ576260A (en) 2006-11-08 2012-04-27 Zealand Pharma As GLUCAGON-LIKE-PEPTIDE-2 (GLP-2) ANALOGUES comprising one of more substitutions as compared to h[Gly2]GLP-2
WO2008071010A1 (en) 2006-12-12 2008-06-19 Waratah Pharmaceuticals Inc. Combination treatments with selected growth/hormone regulatory factors for diabetes and related diseases
TWI428346B (zh) 2006-12-13 2014-03-01 Imp Innovations Ltd 新穎化合物及其等對進食行為影響
EA017849B1 (ru) 2007-02-15 2013-03-29 Индиана Юниверсити Рисерч Энд Текнолоджи Корпорейшн Соагонисты глюкагоновых/glp-1-рецепторов
FR2917552B1 (fr) 2007-06-15 2009-08-28 Sagem Defense Securite Procede de regulation de la gigue de transmission au sein d'un terminal de reception
WO2008152403A1 (en) 2007-06-15 2008-12-18 Zealand Pharma A/S Glucagon analogues
GB2455553B (en) 2007-12-14 2012-10-24 Nuaire Ltd Motor mounting assembly for an axial fan
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
JP5635530B2 (ja) 2008-12-15 2014-12-03 ジーランド ファーマ アクティーゼルスカブ グルカゴン類似体
KR20150116912A (ko) 2008-12-15 2015-10-16 질랜드 파마 에이/에스 글루카곤 유사체
US8680049B2 (en) 2008-12-15 2014-03-25 Zealand Pharma A/S Glucagon analogues
ES2439499T3 (es) 2008-12-15 2014-01-23 Zealand Pharma A/S Análogos de glucagón
WO2010096052A1 (en) 2009-02-19 2010-08-26 Merck Sharp & Dohme Corp. Oxyntomodulin analogs
WO2011084808A2 (en) * 2009-12-21 2011-07-14 Amunix Operating Inc. Bifunctional polypeptide compositions and methods for treatment of metabolic and cardiovascular diseases
BR112012018104A2 (pt) 2010-01-20 2017-10-17 Zeland Pharma As tratamento de doenças cardíacas
BR112012027759A2 (pt) 2010-04-27 2017-08-15 Zealand Pharma As Conjugados de peptídeos de agonistas de receptores glp-1 e gastrina e seu uso
AU2012331053A1 (en) 2011-11-03 2014-05-29 Zealand Pharma A/S GLP-1 receptor agonist peptide gastrin conjugates
TWI608013B (zh) 2012-09-17 2017-12-11 西蘭製藥公司 升糖素類似物
MX368436B (es) 2013-10-17 2019-10-03 Zealand Pharma As Analogos de glucagon acilados.
US9988429B2 (en) 2013-10-17 2018-06-05 Zealand Pharma A/S Glucagon analogues

Patent Citations (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN1961000A (zh) * 2004-02-11 2007-05-09 安米林药品公司 具有可选择特性的杂合多肽
WO2007095737A1 (en) * 2006-02-21 2007-08-30 Waratah Pharmaceuticals Inc. Combination therapy for the treatment of diabetes comprising an exendin agonist and a gastrin compound

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