ES2672880T3 - Péptidos de la superfamilia de glucagón que muestran actividad de receptor de glucocorticoides - Google Patents
Péptidos de la superfamilia de glucagón que muestran actividad de receptor de glucocorticoides Download PDFInfo
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- ES2672880T3 ES2672880T3 ES12849285.7T ES12849285T ES2672880T3 ES 2672880 T3 ES2672880 T3 ES 2672880T3 ES 12849285 T ES12849285 T ES 12849285T ES 2672880 T3 ES2672880 T3 ES 2672880T3
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- 229960003957 dexamethasone Drugs 0.000 description 1
- UREBDLICKHMUKA-CXSFZGCWSA-N dexamethasone Chemical compound C1CC2=CC(=O)C=C[C@]2(C)[C@]2(F)[C@@H]1[C@@H]1C[C@@H](C)[C@@](C(=O)CO)(O)[C@@]1(C)C[C@@H]2O UREBDLICKHMUKA-CXSFZGCWSA-N 0.000 description 1
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- BTCSSZJGUNDROE-UHFFFAOYSA-N gamma-aminobutyric acid Chemical compound NCCCC(O)=O BTCSSZJGUNDROE-UHFFFAOYSA-N 0.000 description 1
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Classifications
-
- 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
- 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
- A61K47/54—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 compound
- A61K47/554—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 compound the modifying agent being a steroid plant sterol, glycyrrhetic acid, enoxolone or bile acid
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous 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
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- 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
- A61P3/06—Antihyperlipidemics
-
- 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
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K38/00—Medicinal preparations containing peptides
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07K—PEPTIDES
- C07K2319/00—Fusion polypeptide
- C07K2319/70—Fusion polypeptide containing domain for protein-protein interaction
- C07K2319/71—Fusion polypeptide containing domain for protein-protein interaction containing domain for transcriptional activaation, e.g. VP16
- C07K2319/715—Fusion polypeptide containing domain for protein-protein interaction containing domain for transcriptional activaation, e.g. VP16 containing a domain for ligand dependent transcriptional activation, e.g. containing a steroid receptor domain
Landscapes
- Health & Medical Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- Chemical & Material Sciences (AREA)
- General Health & Medical Sciences (AREA)
- Medicinal Chemistry (AREA)
- Organic Chemistry (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- Animal Behavior & Ethology (AREA)
- Pharmacology & Pharmacy (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Diabetes (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Obesity (AREA)
- Hematology (AREA)
- Endocrinology (AREA)
- Proteomics, Peptides & Aminoacids (AREA)
- Gastroenterology & Hepatology (AREA)
- Epidemiology (AREA)
- Zoology (AREA)
- Biophysics (AREA)
- Biochemistry (AREA)
- Toxicology (AREA)
- Genetics & Genomics (AREA)
- Molecular Biology (AREA)
- Botany (AREA)
- Neurology (AREA)
- Biomedical Technology (AREA)
- Neurosurgery (AREA)
- Child & Adolescent Psychology (AREA)
- Emergency Medicine (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
- Peptides Or Proteins (AREA)
- Medicinal Preparation (AREA)
- Immunology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
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| US201161561094P | 2011-11-17 | 2011-11-17 | |
| US201161561094P | 2011-11-17 | ||
| PCT/US2012/065492 WO2013074910A1 (en) | 2011-11-17 | 2012-11-16 | Glucagon superfamily peptides exhibiting glucocorticoid receptor activity |
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| ES2672880T3 true ES2672880T3 (es) | 2018-06-18 |
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| ES12849285.7T Active ES2672880T3 (es) | 2011-11-17 | 2012-11-16 | Péptidos de la superfamilia de glucagón que muestran actividad de receptor de glucocorticoides |
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| CA (1) | CA2847246A1 (cg-RX-API-DMAC7.html) |
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| WO (1) | WO2013074910A1 (cg-RX-API-DMAC7.html) |
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| EP2443146B1 (en) | 2009-06-16 | 2016-10-05 | Indiana University Research And Technology Corporation | Gip receptor-active glucagon compounds |
| EA031230B1 (ru) | 2011-06-22 | 2018-12-28 | Индиана Юниверсити Рисерч Энд Текнолоджи Корпорейшн | Агонисты глюкагонового рецептора/glp-1-рецептора |
| UA116217C2 (uk) | 2012-10-09 | 2018-02-26 | Санофі | Пептидна сполука як подвійний агоніст рецепторів glp1-1 та глюкагону |
| RS57531B1 (sr) | 2012-12-21 | 2018-10-31 | Sanofi Sa | Derivati eksendina-4 kao dualni glp1/gip- ili trigonalni glp1/gip/glukagon agonisti |
| EP3080150B1 (en) | 2013-12-13 | 2018-08-01 | Sanofi | Exendin-4 peptide analogues as dual glp-1/gip receptor agonists |
| WO2015086729A1 (en) | 2013-12-13 | 2015-06-18 | Sanofi | Dual glp-1/gip receptor agonists |
| WO2015086733A1 (en) | 2013-12-13 | 2015-06-18 | Sanofi | Dual glp-1/glucagon 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 |
| 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 |
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| US9932381B2 (en) | 2014-06-18 | 2018-04-03 | Sanofi | Exendin-4 derivatives as selective glucagon receptor agonists |
| GB2528436A (en) * | 2014-07-15 | 2016-01-27 | Lancaster Univ Business Entpr Ltd | Treatment of neurological diseases |
| GB201414098D0 (en) | 2014-08-08 | 2014-09-24 | Illumina Cambridge Ltd | Modified nucleotide linkers |
| PE20171154A1 (es) * | 2014-12-30 | 2017-08-16 | Hanmi Pharm Ind Co Ltd | Derivados de glucagon con estabilidad mejorada |
| AR105319A1 (es) | 2015-06-05 | 2017-09-27 | Sanofi Sa | Profármacos que comprenden un conjugado agonista dual de glp-1 / glucagón conector ácido hialurónico |
| TWI669309B (zh) * | 2015-06-22 | 2019-08-21 | 美商美國禮來大藥廠 | 升糖素及glp-1共激動劑化合物 |
| KR102005456B1 (ko) | 2015-06-30 | 2019-07-30 | 한미약품 주식회사 | 신규 글루카곤 유도체 및 이의 지속형 결합체를 포함하는 조성물 |
| 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 |
| JP7026044B2 (ja) | 2015-12-23 | 2022-02-25 | ザ・ジョンズ・ホプキンス・ユニバーシティー | 神経性状態および神経変性状態の治療としての長時間作用型GLP-1rアゴニスト |
| MX2018008128A (es) | 2015-12-31 | 2018-12-06 | Hanmi Pharm Ind Co Ltd | Conjugado persistente de triple activador que activa el receptor de glucagon, glp-1 y gip. |
| RU2760007C2 (ru) * | 2016-05-16 | 2021-11-22 | Интарсия Терапьютикс, Инк. | Полипептиды, селективные к рецепторам глюкагона, и способы их применения |
| MX2019000019A (es) | 2016-06-29 | 2019-05-06 | Hanmi Pharm Ind Co Ltd | Derivado de glucagon, conjugado del mismo, composicion que comprende el mismo y uso terapeutico del mismo. |
| EP3856768A2 (en) * | 2018-09-24 | 2021-08-04 | Takeda Pharmaceutical Company Limited | Gip receptor agonist peptide compounds and uses thereof |
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| EP3842060A1 (en) * | 2019-12-23 | 2021-06-30 | Merck Sharp & Dohme Corp. | Stapled lactam co-agonists of the glucagon and glp-1 receptors |
| WO2022090447A1 (en) * | 2020-10-30 | 2022-05-05 | Novo Nordisk A/S | Glp-1, gip and glucagon receptor triple agonists |
| EP4154913A1 (en) * | 2021-09-28 | 2023-03-29 | Københavns Universitet | Conjugates of glucagon and ampk activators |
| TW202330584A (zh) * | 2022-01-20 | 2023-08-01 | 丹麥商諾佛 儂迪克股份有限公司 | 前藥及其用途 |
Family Cites Families (132)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US4450150A (en) | 1973-05-17 | 1984-05-22 | Arthur D. Little, Inc. | Biodegradable, implantable drug delivery depots, and method for preparing and using the same |
| US4275152A (en) | 1977-02-03 | 1981-06-23 | Eastman Kodak Company | Hydrolysis of protein-bound cholesterol esters |
| PT83613B (en) | 1985-10-28 | 1988-11-21 | Lilly Co Eli | Process for the selective chemical removal of a protein amino-terminal residue |
| EP0272253A4 (en) | 1986-03-07 | 1990-02-05 | Massachusetts Inst Technology | METHOD FOR IMPROVING GLYCOPROTE INSTABILITY. |
| IN165717B (cg-RX-API-DMAC7.html) | 1986-08-07 | 1989-12-23 | Battelle Memorial Institute | |
| ATE123780T1 (de) | 1989-02-17 | 1995-06-15 | Chiron Mimotopes Pty Ltd | Verfahren zur verwendung und herstellung von peptiden. |
| CA2024855C (en) | 1990-09-07 | 1997-12-09 | Boehringer Ingelheim (Canada) Ltd./ Boehringer Ingelheim (Canada) Ltee | Process and intermediates for producing glucagon |
| JPH04145099A (ja) | 1990-10-05 | 1992-05-19 | Sanwa Kagaku Kenkyusho Co Ltd | Gip様活性を有するポリペプチド誘導体及びその用途 |
| US5510459A (en) | 1991-01-17 | 1996-04-23 | Zymogenetics, Inc. | Glucagon antagonists |
| JP3266311B2 (ja) | 1991-05-02 | 2002-03-18 | 生化学工業株式会社 | 新規ポリペプチドおよびこれを用いる抗hiv剤 |
| US5359030A (en) | 1993-05-10 | 1994-10-25 | Protein Delivery, Inc. | Conjugation-stabilized polypeptide compositions, therapeutic delivery and diagnostic formulations comprising same, and method of making and using the same |
| US5480867A (en) | 1993-12-29 | 1996-01-02 | The Rockefeller University | Glucagon analogs with serine replacements |
| US5512549A (en) | 1994-10-18 | 1996-04-30 | Eli Lilly And Company | Glucagon-like insulinotropic peptide analogs, compositions, and methods of use |
| US5691309A (en) | 1995-01-31 | 1997-11-25 | Eli Lilly And Company | Anti-obesity proteins |
| US5869602A (en) | 1995-03-17 | 1999-02-09 | Novo Nordisk A/S | Peptide derivatives |
| DE19530865A1 (de) | 1995-08-22 | 1997-02-27 | Michael Dr Med Nauck | Wirkstoff sowie Mittel zur parenteralen Ernährung |
| CA2208215A1 (en) | 1995-10-12 | 1997-04-17 | Supergen, Inc. | Liposome formulations of 5.beta. steroids |
| AU2263197A (en) | 1996-02-06 | 1997-08-28 | Eli Lilly And Company | Diabetes therapy |
| AU724326B2 (en) | 1996-09-09 | 2000-09-14 | Zealand Pharmaceuticals A/S | Peptide prodrugs containing an alpha-hydroxyacid linker |
| 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 |
| WO1998024464A1 (en) | 1996-12-03 | 1998-06-11 | Trustees Of Boston University | Specific antagonists for glucose-dependent insulinotropic polypeptide (gip) |
| US6303144B1 (en) | 1998-02-10 | 2001-10-16 | Welfide Corporation | Preparations with controlled release |
| CA2321026A1 (en) | 1998-03-09 | 1999-09-16 | Zealand Pharmaceuticals A/S | Pharmacologically active peptide conjugates having a reduced tendency towards enzymatic hydrolysis |
| US20030236190A1 (en) | 1998-09-02 | 2003-12-25 | Renuka Pillutla | Isulin and IGF-1 receptor agonists and antagonists |
| US6410508B1 (en) | 1998-10-07 | 2002-06-25 | Med College Georgia Res Inst | Glucose-dependent insulinotropic peptide for use as an osteotropic hormone |
| GB2344287A (en) | 1998-12-03 | 2000-06-07 | Ferring Bv | Controlled release pharmaceutical formulation |
| AU3033500A (en) | 1999-01-15 | 2000-08-01 | Agouron Pharmaceuticals, Inc. | Non-peptide glp-1 agonists |
| GB0404124D0 (en) | 2004-02-25 | 2004-03-31 | Univ Ulster | Antagonists of GIP |
| AU3441400A (en) | 1999-03-29 | 2000-10-16 | Uutech Limited | Peptide |
| US7601691B2 (en) | 1999-05-17 | 2009-10-13 | Conjuchem Biotechnologies Inc. | Anti-obesity agents |
| AU2001257278A1 (en) | 2000-04-27 | 2001-11-07 | Bionebraska, Inc. | Gastric inhibitory polypeptide diagnostic test for detecting susceptibility to type-2 diabetes, impaired glucose tolerance, or impaired fasting glucose |
| US6677136B2 (en) | 2000-05-03 | 2004-01-13 | Amgen Inc. | Glucagon antagonists |
| WO2001096368A2 (en) | 2000-06-14 | 2001-12-20 | Cytovax Biotechnologies, Inc. | Use of coiled-coil structural scaffold to generate structure-specific peptides |
| ES2275685T3 (es) | 2000-06-16 | 2007-06-16 | Eli Lilly And Company | Analogos del peptido similar a glucagon 1. |
| BR0113178A (pt) | 2000-08-02 | 2004-04-06 | Theratechnologies Inc | Peptìdeos biológicos modificados com potência aumentada |
| US6846831B2 (en) | 2000-08-15 | 2005-01-25 | Cpd, Llc | Method of treating the syndrome of lipodystrophy |
| US6528520B2 (en) | 2000-08-15 | 2003-03-04 | Cpd, Llc | Method of treating the syndrome of coronary heart disease risk factors in humans |
| US20020045572A1 (en) | 2000-08-15 | 2002-04-18 | Cpd, Llc | Method of treating the syndrome of type 2 diabetes in humans |
| US6262062B1 (en) | 2000-08-15 | 2001-07-17 | Cpd, Llc | Method of treating the syndrome of coronary heart disease risk factors in humans |
| EP1324779B1 (en) | 2000-09-29 | 2011-07-20 | Schering Corporation | Pegylated interleukin-10 |
| AU2002228608A1 (en) | 2000-12-13 | 2002-06-24 | Eli Lilly And Company | Amidated glucagon-like peptide-1 |
| EP2022505B1 (en) | 2001-07-31 | 2011-12-14 | The Government of the United States of America, as represented by the Secretary of the Department of Health and Human Services | GLP-1, exendin-4, peptide analogs and uses thereof |
| WO2003014318A2 (en) | 2001-08-08 | 2003-02-20 | Genzyme Corporation | Methods for treating diabetes and other blood sugar disorders |
| AU2002322403A1 (en) | 2001-08-23 | 2003-03-10 | Eli Lilly And Company | Glucagon-like peptide-1 analogs |
| US7238663B2 (en) | 2001-08-28 | 2007-07-03 | Eli Lilly And Company | Pre-mixes of GLP-1 and basal insulin |
| GB0121709D0 (en) | 2001-09-07 | 2001-10-31 | Imp College Innovations Ltd | Food inhibition agent |
| US7041646B2 (en) | 2001-10-05 | 2006-05-09 | Bayer Pharmaceuticals Corporation | Methods of treating type 2 diabetes with peptides acting as both GLP-1 receptor agonists and glucagon receptor antagonists |
| AR036711A1 (es) | 2001-10-05 | 2004-09-29 | Bayer Corp | Peptidos que actuan como agonistas del receptor del glp-1 y como antagonistas del receptor del glucagon y sus metodos de uso farmacologico |
| MXPA04003553A (es) | 2001-10-18 | 2004-07-22 | Bristol Myers Squibb Co | Mimeticos del peptido-1 similares aglucagon humano y su uso en tratamiento de diabetes y condiciones relacionadas. |
| EP1448222A4 (en) | 2001-10-19 | 2006-05-17 | Lilly Co Eli | BIPHASIC MIXTURES OF GLP-1 AND INSULIN |
| WO2003059378A2 (en) | 2001-12-29 | 2003-07-24 | Novo Nordisk A/S | Combined use of a glp-1 compound and another drug for treating dyslipidemia |
| CA2468700A1 (en) | 2002-01-08 | 2003-07-17 | Eli Lilly And Company | Extended glucagon-like peptide-1 analogs |
| US20030232761A1 (en) | 2002-03-28 | 2003-12-18 | Hinke Simon A. | Novel analogues of glucose-dependent insulinotropic polypeptide |
| AU2003239478A1 (en) | 2002-06-04 | 2003-12-22 | Eli Lilly And Company | Modified glucagon-like peptide-1 analogs |
| WO2003103697A2 (en) | 2002-06-11 | 2003-12-18 | Cell Therapeutics Scandinavia Ab | Use of compounds having gip activity for the treatment of disorders associated with abnormal loss of cells and/or for the treatment of obesity |
| US20040029805A1 (en) | 2002-06-15 | 2004-02-12 | Wolfe M. Michael | Prevention and treatment of nonalcoholic fatty liver disease (NAFLD) by antagonism of the receptor to glucose-dependent insulinotropic polypeptide (GIP) |
| JP2006501820A (ja) | 2002-09-06 | 2006-01-19 | バイエル・フアーマシユーチカルズ・コーポレーシヨン | 修飾glp−1受容体アゴニストおよびそれらの薬理学的使用法 |
| US7917208B2 (en) | 2002-10-04 | 2011-03-29 | Microchips, Inc. | Medical device for controlled drug delivery and cardiac monitoring and/or stimulation |
| US7192922B2 (en) | 2002-11-19 | 2007-03-20 | Allegheny-Singer Research Institute | Method of treating left ventricular dysfunction |
| CA2512729C (en) | 2003-01-09 | 2014-09-16 | Macrogenics, Inc. | Identification and engineering of antibodies with variant fc regions and methods of using same |
| US20050059605A1 (en) | 2003-01-31 | 2005-03-17 | Krishna Peri | Chemically modified metabolites of regulatory peptides and methods of producing and using same |
| WO2004078777A2 (en) | 2003-03-04 | 2004-09-16 | Biorexis Pharmaceutical Corporation | Dipeptidyl-peptidase protected proteins |
| US7557183B2 (en) | 2003-03-19 | 2009-07-07 | Eli Lilly And Company | Polyethylene glycol linked GLP-1 compounds |
| ES2512499T3 (es) | 2003-04-08 | 2014-10-24 | Yeda Research And Development Co., Ltd. | Fármacos pegilados reversibles |
| TWI353991B (en) | 2003-05-06 | 2011-12-11 | Syntonix Pharmaceuticals Inc | Immunoglobulin chimeric monomer-dimer hybrids |
| AU2004240630B2 (en) | 2003-05-15 | 2010-10-07 | Trustees Of Tufts College | Stable analogs of peptide and polypeptide therapeutics |
| CA2527743A1 (en) | 2003-06-03 | 2004-12-09 | Novo Nordisk A/S | Stabilized pharmaceutical peptide compositions |
| JP2007524592A (ja) | 2003-06-03 | 2007-08-30 | ノボ・ノルデイスク・エー/エス | 安定化された薬学的ペプチド組成物 |
| MXPA05013565A (es) | 2003-06-12 | 2006-03-09 | Lilly Co Eli | Proteinas de fusion analogas al glp-1. |
| US20050124550A1 (en) | 2003-06-18 | 2005-06-09 | Peri Krishna G. | Compounds that modulate the glucagon response and uses thereof |
| JP4949838B2 (ja) | 2003-09-19 | 2012-06-13 | ノヴォ ノルディスク アー/エス | 新規glp−1誘導体 |
| US7364875B2 (en) | 2003-10-30 | 2008-04-29 | Cresent Innovations, Inc. | Method for producing medical and commercial grade poly-gamma-glutamic acid of high molecular weight |
| EP1704165B1 (en) | 2003-12-18 | 2010-03-17 | Novo Nordisk A/S | Glp-1 compounds |
| US20060286129A1 (en) | 2003-12-19 | 2006-12-21 | Emisphere Technologies, Inc. | Oral GLP-1 formulations |
| US20080318837A1 (en) | 2003-12-26 | 2008-12-25 | Nastech Pharmaceutical Company Inc. | Pharmaceutical Formation For Increased Epithelial Permeability of Glucose-Regulating Peptide |
| SG158158A1 (en) | 2004-12-22 | 2010-01-29 | Centocor Inc | Glp-1 agonists, compositions, methods and uses |
| EP1853627A2 (en) | 2005-02-11 | 2007-11-14 | Amylin Pharmaceuticals, Inc. | Gip analog and hybrid polypeptides with selectable properties |
| WO2006097536A2 (en) | 2005-03-18 | 2006-09-21 | Novo Nordisk A/S | Dimeric peptide agonists of the glp-1 receptor |
| WO2006121904A1 (en) | 2005-05-06 | 2006-11-16 | Bayer Pharmaceuticals Corporation | Glucose-dependent insulinotropic polypeptide (gip) receptor agonists and their pharmacological methods of use |
| CN101166545B (zh) | 2005-05-13 | 2011-06-15 | 伊莱利利公司 | Glp-1聚乙二醇化的化合物 |
| WO2006134340A2 (en) | 2005-06-13 | 2006-12-21 | Imperial Innovations Limited | Oxyntomodulin analogues and their effects on feeding behaviour |
| EP1922336B1 (en) | 2005-08-11 | 2012-11-21 | Amylin Pharmaceuticals, LLC | Hybrid polypeptides with selectable properties |
| US20090170762A1 (en) | 2005-09-08 | 2009-07-02 | Uutech Limited | Treatment of Diabetes Related Obesity |
| US20090286722A1 (en) | 2005-09-08 | 2009-11-19 | Utech Limited | Analogs of Gastric Inhibitory Polypeptide as a Treatment for Age Related Decreased Pancreatic Beta Cell Function |
| BRPI0615573A2 (pt) | 2005-09-08 | 2011-05-24 | Tufts College | análogos de glp-1 estabilizados |
| US7846445B2 (en) | 2005-09-27 | 2010-12-07 | Amunix Operating, Inc. | Methods for production of unstructured recombinant polymers and uses thereof |
| US8338368B2 (en) | 2005-11-07 | 2012-12-25 | Indiana University Research And Technology Corporation | Glucagon analogs exhibiting physiological solubility and stability |
| EP1991574B1 (en) | 2006-02-22 | 2016-10-12 | Merck Sharp & Dohme Corp. | Oxyntomodulin derivatives |
| JP5312054B2 (ja) | 2006-03-15 | 2013-10-09 | ノボ・ノルデイスク・エー/エス | アミリンとインスリンの混合物 |
| JP5412273B2 (ja) | 2006-03-21 | 2014-02-12 | アミリン・ファーマシューティカルズ,リミテッド・ライアビリティ・カンパニー | ペプチド−ぺプチダーゼ阻害剤及びその使用 |
| CA2648936C (en) | 2006-04-20 | 2013-07-09 | Amgen Inc. | Glp-1 compounds |
| EP2020989A2 (en) | 2006-05-15 | 2009-02-11 | Wisconsin Allumni Research Foundation | Pulmonary delivery of 1,25-dihydroxyvitamin d3 and co-administration of parathyroid hormone or calcitonin |
| FR2902092B1 (fr) | 2006-06-07 | 2008-09-05 | Sapelem Soc Par Actions Simpli | Appareil de manutention de charge |
| WO2008022015A2 (en) | 2006-08-11 | 2008-02-21 | Trustees Of Tufts College | Retro-inverso incretin analogues, and methods of use thereof |
| WO2008021560A2 (en) | 2006-08-17 | 2008-02-21 | Amylin Pharmaceuticals, Inc. | Dpp-iv resistant gip hybrid polypeptides with selectable properties |
| EP2057189B1 (en) | 2006-08-25 | 2013-03-06 | Novo Nordisk A/S | Acylated exendin-4 compounds |
| JP5840345B2 (ja) | 2006-09-08 | 2016-01-06 | アンブルックス, インコーポレイテッドAmbrx, Inc. | 修飾ヒト血漿ポリペプチドまたは修飾ヒトFc足場タンパク質ならびにこれらの利用 |
| EP2102355B1 (en) | 2006-12-14 | 2016-03-02 | Bolder Biotechnology, Inc. | Long acting proteins and peptides and methods of making and using the same |
| EP2124974B1 (en) | 2007-01-05 | 2017-03-15 | Indiana University Research and Technology Corporation | Glucagon analogs exhibiting enhanced solubility in physiological ph buffers |
| US8454971B2 (en) | 2007-02-15 | 2013-06-04 | Indiana University Research And Technology Corporation | Glucagon/GLP-1 receptor co-agonists |
| EP2139458A4 (en) | 2007-04-19 | 2013-01-23 | Dong A Pharm Co Ltd | COMPOSITION OF BIODEGRADABLE MICROSPHERES WITH CONTROLLED RELEASE OF A GLUCOSE REGULATING PEPTIDE AND RELATED FORMULA |
| EP2185701A4 (en) | 2007-08-15 | 2011-03-02 | Amunix Operating Inc | COMPOSITIONS AND METHODS FOR ENHANCING THE PRODUCTION OF RECOMBINANT POLYPEPTIDES |
| WO2009030738A1 (en) | 2007-09-05 | 2009-03-12 | Novo Nordisk A/S | Glucagon-like peptide-1 derivatives and their pharmaceutical use |
| CN101842386A (zh) | 2007-09-05 | 2010-09-22 | 诺沃-诺迪斯克有限公司 | 截短的glp-1衍生物和它们的治疗用途 |
| US20100256056A1 (en) | 2007-09-07 | 2010-10-07 | Zheng Xin Dong | Analogues of exendin-4 and exendin-3 |
| CN101854948A (zh) | 2007-09-11 | 2010-10-06 | 诺沃-诺迪斯克有限公司 | 含有胰岛淀粉样多肽类和长效胰岛素的合剂 |
| EP2036539A1 (en) | 2007-09-11 | 2009-03-18 | Novo Nordisk A/S | Stable formulations of amylin and its analogues |
| EP2036923A1 (en) | 2007-09-11 | 2009-03-18 | Novo Nordisk A/S | Improved derivates of amylin |
| MX2010004297A (es) | 2007-10-30 | 2010-05-03 | Univ Indiana Res & Tech Corp | Antagonistas de glucagon. |
| ES2558155T3 (es) | 2007-10-30 | 2016-02-02 | Indiana University Research And Technology Corporation | Compuestos que muestran actividad antagonista de glucacón y agonista de GLP-1 |
| WO2009058944A2 (en) * | 2007-11-01 | 2009-05-07 | Bristol-Myers Squibb Company | Nonsteroidal compounds useful as modulators of glucocorticoid receptor ap-1 and /or nf- kappa b activity and use thereof |
| EP2249853A4 (en) | 2008-01-30 | 2012-12-26 | Univ Indiana Res & Tech Corp | ESTER BASED PEPTIDE PRODRUGS |
| RS58948B1 (sr) | 2008-02-01 | 2019-08-30 | Ascendis Pharma As | Prolek koji sadrži linker koji se može sam odcepiti |
| TWI474835B (zh) * | 2008-06-17 | 2015-03-01 | Univ Indiana Res & Tech Corp | 用於治療代謝病症及肥胖症之基於gip之混合激動劑 |
| KR20110039230A (ko) | 2008-06-17 | 2011-04-15 | 인디애나 유니버시티 리서치 앤드 테크놀로지 코퍼레이션 | 생리학적 pH 완충액에서 강화된 용해도 및 안정성을 나타내는 글루카곤 유사체 |
| JP5775450B2 (ja) | 2008-06-17 | 2015-09-09 | インディアナ ユニバーシティー リサーチ アンド テクノロジー コーポレーションIndiana University Research And Technology Corporation | グルカゴン/glp−1受容体コアゴニスト |
| US20110212053A1 (en) | 2008-06-19 | 2011-09-01 | Dapeng Qian | Phosphatidylinositol 3 kinase inhibitors |
| WO2010044867A1 (en) | 2008-10-15 | 2010-04-22 | Intarcia Therapeutics, Inc. | Highly concentrated drug particles, formulations, suspensions and uses thereof |
| RU2550696C2 (ru) | 2008-12-19 | 2015-05-10 | Индиана Юниверсити Рисерч Энд Текнолоджи Корпорейшн | Основанные на амидах пролекарства пептидов глюкагонового надсемейства |
| MX2011006527A (es) * | 2008-12-19 | 2011-08-17 | Univ Indiana Res & Tech Corp | Agentes medicinales unidos a dipeptido. |
| WO2010096052A1 (en) | 2009-02-19 | 2010-08-26 | Merck Sharp & Dohme Corp. | Oxyntomodulin analogs |
| EP2443146B1 (en) | 2009-06-16 | 2016-10-05 | Indiana University Research And Technology Corporation | Gip receptor-active glucagon compounds |
| US20110009347A1 (en) * | 2009-07-08 | 2011-01-13 | Yin Liang | Combination therapy for the treatment of diabetes |
| US8703701B2 (en) | 2009-12-18 | 2014-04-22 | Indiana University Research And Technology Corporation | Glucagon/GLP-1 receptor co-agonists |
| 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 |
| IN2012DN06437A (cg-RX-API-DMAC7.html) | 2010-01-27 | 2015-10-09 | Univ Indiana Res & Tech Corp | |
| AR080592A1 (es) | 2010-03-26 | 2012-04-18 | Lilly Co Eli | Peptido con actividad para el gip-r y glp-1-r, formulacion famaceutica que lo comprende, su uso para preparar un medicamento util para el tratamiento de diabetes mellitus y para inducir la perdida de peso |
| CN103079587B (zh) | 2010-05-13 | 2016-05-11 | 印第安纳大学研究及科技有限公司 | 呈现核激素受体活性的胰高血糖素超家族肽 |
| KR20130111923A (ko) | 2010-05-13 | 2013-10-11 | 인디애나 유니버시티 리서치 앤드 테크놀로지 코퍼레이션 | G-단백결합 수용체 활성을 나타내는 글루카곤 슈퍼패밀리 펩티드 |
| RU2580317C2 (ru) | 2010-06-24 | 2016-04-10 | Индиана Юниверсити Рисерч Энд Текнолоджи Корпорейшн | Пептидные пролекарства, принадлежащие к суперсемейству амид-содержащих глюкагонов |
| WO2011163473A1 (en) | 2010-06-25 | 2011-12-29 | Indiana University Research And Technology Corporation | Glucagon analogs exhibiting enhanced solubility and stability in physiological ph buffers |
-
2012
- 2012-11-16 CN CN201280049164.2A patent/CN103957927B/zh not_active Expired - Fee Related
- 2012-11-16 WO PCT/US2012/065492 patent/WO2013074910A1/en not_active Ceased
- 2012-11-16 MX MX2014003579A patent/MX2014003579A/es unknown
- 2012-11-16 BR BR112014007124A patent/BR112014007124A2/pt unknown
- 2012-11-16 RU RU2014117678/04A patent/RU2014117678A/ru not_active Application Discontinuation
- 2012-11-16 ES ES12849285.7T patent/ES2672880T3/es active Active
- 2012-11-16 CA CA 2847246 patent/CA2847246A1/en not_active Abandoned
- 2012-11-16 EP EP12849285.7A patent/EP2780031B1/en not_active Not-in-force
- 2012-11-16 HK HK14112265.7A patent/HK1198810A1/xx unknown
- 2012-11-16 JP JP2014542489A patent/JP6324315B2/ja active Active
- 2012-11-16 KR KR20147012192A patent/KR20140097151A/ko not_active Withdrawn
- 2012-11-16 US US13/679,121 patent/US8859491B2/en not_active Expired - Fee Related
Also Published As
| Publication number | Publication date |
|---|---|
| MX2014003579A (es) | 2015-04-10 |
| JP2015504431A (ja) | 2015-02-12 |
| US20130157934A1 (en) | 2013-06-20 |
| EP2780031A4 (en) | 2015-08-05 |
| EP2780031A1 (en) | 2014-09-24 |
| KR20140097151A (ko) | 2014-08-06 |
| CA2847246A1 (en) | 2013-05-23 |
| US8859491B2 (en) | 2014-10-14 |
| HK1198810A1 (en) | 2015-06-12 |
| CN103957927B (zh) | 2016-11-09 |
| JP6324315B2 (ja) | 2018-05-16 |
| BR112014007124A2 (pt) | 2017-06-13 |
| EP2780031B1 (en) | 2018-03-07 |
| WO2013074910A1 (en) | 2013-05-23 |
| CN103957927A (zh) | 2014-07-30 |
| RU2014117678A (ru) | 2015-12-27 |
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