JP2018504901A5 - - Google Patents
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- JP2018504901A5 JP2018504901A5 JP2017535417A JP2017535417A JP2018504901A5 JP 2018504901 A5 JP2018504901 A5 JP 2018504901A5 JP 2017535417 A JP2017535417 A JP 2017535417A JP 2017535417 A JP2017535417 A JP 2017535417A JP 2018504901 A5 JP2018504901 A5 JP 2018504901A5
- Authority
- JP
- Japan
- Prior art keywords
- cysteine
- receptor agonist
- acid
- receptor
- pharmaceutical composition
- Prior art date
- Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
- Granted
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- 101800001982 Cholecystokinin Proteins 0.000 claims description 8
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Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| KR20140193800 | 2014-12-30 | ||
| KR10-2014-0193800 | 2014-12-30 | ||
| PCT/KR2015/014422 WO2016108586A1 (ko) | 2014-12-30 | 2015-12-30 | 안정성이 증가된 글루카곤 유도체 |
Related Child Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2020144259A Division JP7079301B2 (ja) | 2014-12-30 | 2020-08-28 | 安定性が増加されたグルカゴン誘導体 |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2018504901A JP2018504901A (ja) | 2018-02-22 |
| JP2018504901A5 true JP2018504901A5 (enExample) | 2019-02-07 |
| JP6797122B2 JP6797122B2 (ja) | 2020-12-09 |
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Family Applications (2)
| Application Number | Title | Priority Date | Filing Date |
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| JP2017535417A Active JP6797122B2 (ja) | 2014-12-30 | 2015-12-30 | 安定性が増加されたグルカゴン誘導体 |
| JP2020144259A Active JP7079301B2 (ja) | 2014-12-30 | 2020-08-28 | 安定性が増加されたグルカゴン誘導体 |
Family Applications After (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2020144259A Active JP7079301B2 (ja) | 2014-12-30 | 2020-08-28 | 安定性が増加されたグルカゴン誘導体 |
Country Status (28)
| Country | Link |
|---|---|
| US (1) | US11135271B2 (enExample) |
| EP (2) | EP3575314B1 (enExample) |
| JP (2) | JP6797122B2 (enExample) |
| KR (1) | KR102291020B1 (enExample) |
| CN (1) | CN107636009B (enExample) |
| AR (1) | AR103322A1 (enExample) |
| AU (1) | AU2015372818A1 (enExample) |
| CL (1) | CL2017001718A1 (enExample) |
| CO (1) | CO2017006308A2 (enExample) |
| CR (1) | CR20170293A (enExample) |
| DO (1) | DOP2017000156A (enExample) |
| EA (1) | EA035527B1 (enExample) |
| EC (1) | ECSP17040923A (enExample) |
| ES (1) | ES2976562T3 (enExample) |
| GT (1) | GT201700150A (enExample) |
| HK (1) | HK1248713A1 (enExample) |
| IL (2) | IL253206B (enExample) |
| MA (1) | MA40709B1 (enExample) |
| MX (1) | MX2017008569A (enExample) |
| MY (1) | MY185334A (enExample) |
| PE (2) | PE20171154A1 (enExample) |
| PH (1) | PH12017501222B1 (enExample) |
| SG (1) | SG11201705376SA (enExample) |
| TN (1) | TN2017000271A1 (enExample) |
| TW (1) | TW201639878A (enExample) |
| UA (1) | UA126960C2 (enExample) |
| WO (1) | WO2016108586A1 (enExample) |
| ZA (1) | ZA201705015B (enExample) |
Families Citing this family (15)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| KR102291020B1 (ko) * | 2014-12-30 | 2021-08-20 | 한미약품 주식회사 | 안정성이 증가된 글루카곤 유도체 |
| FI3322437T3 (fi) * | 2015-06-30 | 2024-02-20 | Hanmi Pharmaceutical Co Ltd | Glukagonijohdannainen ja sen pitkävaikutteisen konjugaatin käsittävä koostumus |
| TWI622596B (zh) | 2015-10-26 | 2018-05-01 | 美國禮來大藥廠 | 升糖素受體促效劑 |
| JP6712323B2 (ja) | 2015-12-31 | 2020-06-17 | ハンミ ファーマシューティカル カンパニー リミテッド | グルカゴン、ｇｌｐ−１及びｇｉｐ受容体のすべてに活性を有する三重活性体 |
| CN122440793A (zh) * | 2016-06-29 | 2026-07-24 | 韩美药品株式会社 | 胰高血糖素衍生物、其缀合物、包含其的组合物、和其治疗用途 |
| EP3578204A4 (en) | 2017-02-03 | 2021-01-06 | Hanmi Pharm. Co., Ltd. | CONJUGATE MADE FROM BIOACTIVE MATERIAL WITH INCREASED RESISTANCE AND USE OF IT |
| EP3708661A4 (en) * | 2017-12-22 | 2021-12-01 | Hanmi Pharm. Co., Ltd. | THERAPEUTIC ENZYMFUSION PROTEIN WITH A NEW STRUCTURE AND ITS USE |
| CN111936159A (zh) * | 2018-01-23 | 2020-11-13 | Xeris药物公司 | 使用微剂量的稳定胰高血糖素治疗减肥术后低血糖症 |
| WO2020130751A1 (ko) | 2018-12-21 | 2020-06-25 | 한미약품 주식회사 | 인슐린 및 글루카곤을 포함하는 약학 조성물 |
| CN109836486B (zh) * | 2019-01-30 | 2020-09-08 | 北京双因生物科技有限公司 | 成纤维生长因子21变体、其融合蛋白及其用途 |
| CA3179603A1 (en) | 2020-05-22 | 2021-11-25 | Hanmi Pharm. Co., Ltd. | Liquid formulation of long-acting conjugate of glucagon derivative |
| BR112023000515A2 (pt) * | 2020-07-15 | 2023-03-21 | Hanmi Pharm Ind Co Ltd | Composição farmacêutica e seu uso |
| US20240197834A1 (en) | 2021-04-09 | 2024-06-20 | Hanmi Pharm. Co., Ltd. | Pharmaceutical composition for preventing or treating chronic renal disease including glucagon derivative |
| KR20230095666A (ko) | 2021-12-22 | 2023-06-29 | 한미약품 주식회사 | 간 표적 물질 및 이의 용도 |
| CN115536739B (zh) * | 2022-07-04 | 2023-04-14 | 北京惠之衡生物科技有限公司 | 一种glp-1受体和gcg受体共激动多肽衍生物的制备方法 |
Family Cites Families (57)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US5408037A (en) | 1991-01-17 | 1995-04-18 | Zymogenetics, Inc. | Methods for detecting glucagon antagonists |
| GB9423277D0 (en) | 1994-11-18 | 1995-01-11 | Univ Nottingham | Pulsed laser deposition of coatings |
| US6096871A (en) | 1995-04-14 | 2000-08-01 | Genentech, Inc. | Polypeptides altered to contain an epitope from the Fc region of an IgG molecule for increased half-life |
| CA2249195A1 (en) | 1996-03-18 | 1997-09-25 | Board Of Regents, The University Of Texas System | Immunoglobin-like domains with increased half lives |
| US6677136B2 (en) | 2000-05-03 | 2004-01-13 | Amgen Inc. | Glucagon antagonists |
| EP1411968B1 (en) | 2001-07-31 | 2008-09-17 | THE GOVERNMENT OF THE UNITED STATES OF AMERICA, as represented by THE SECRETARY, DEPARTMENT OF HEALTH AND HUMAN SERVICES | Glp-1 exendin-4 peptide analogs and uses thereof |
| US7557183B2 (en) | 2003-03-19 | 2009-07-07 | Eli Lilly And Company | Polyethylene glycol linked GLP-1 compounds |
| BRPI0406605B8 (pt) | 2003-11-13 | 2021-05-25 | Hanmi Holdings Co Ltd | conjugado de proteína, método para a preparação do mesmo e composição farmacêutica para intensificar a duração e estabilidade in vivo de um polipeptídeo fisiologicamente ativo |
| US8263084B2 (en) | 2003-11-13 | 2012-09-11 | Hanmi Science Co., Ltd | Pharmaceutical composition for treating obesity-related disease comprising insulinotropic peptide conjugate |
| EP2007804B1 (en) | 2006-04-20 | 2014-06-18 | Amgen, Inc | Glp-1 compounds |
| US20090098130A1 (en) | 2007-01-05 | 2009-04-16 | Bradshaw Curt W | Glucagon-like protein-1 receptor (glp-1r) agonist compounds |
| 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 |
| CN101578102B (zh) * | 2007-01-05 | 2013-07-17 | 印第安纳大学研究及科技有限公司 | 在生理性pH缓冲液中显示增强的溶解性的胰高血糖素类似物 |
| NZ578948A (en) | 2007-02-15 | 2012-03-30 | Univ Indiana Res & Tech Corp | Glucagon/glp-1 receptor co-agonists |
| WO2008152403A1 (en) | 2007-06-15 | 2008-12-18 | Zealand Pharma A/S | Glucagon analogues |
| BRPI0813139A8 (pt) | 2007-06-19 | 2019-01-29 | Glytech Inc | peptídeo glp-1 com adição de cadeia oligossacarídea |
| EP2190872B1 (en) | 2007-09-05 | 2018-03-14 | Novo Nordisk A/S | Glucagon-like peptide-1 derivatives and their pharmaceutical use |
| US20110065633A1 (en) | 2008-01-30 | 2011-03-17 | Indiana University Research And Technology Corporation | Ester-based peptide prodrugs |
| TWI541023B (zh) | 2008-06-17 | 2016-07-11 | 印第安納大學科技研究公司 | 在生理ｐｈ緩衝液中呈現增強之溶解度及穩定性之升糖激素類似物 |
| ES2558842T3 (es) | 2008-06-17 | 2016-02-09 | Indiana University Research And Technology Corporation | Agonistas mixtos a base de GIP para el tratamiento de trastornos metabólicos y obesidad |
| WO2010096052A1 (en) | 2009-02-19 | 2010-08-26 | Merck Sharp & Dohme Corp. | Oxyntomodulin analogs |
| WO2010148089A1 (en) | 2009-06-16 | 2010-12-23 | Indiana University Research And Technology Corporation | Gip receptor-active glucagon compounds |
| JP6054742B2 (ja) | 2009-07-13 | 2016-12-27 | ジーランド ファーマ アクティーゼルスカブ | アシル化グルカゴン類似体 |
| GB0917072D0 (en) | 2009-09-29 | 2009-11-11 | Univ Ulster | Peptide analogues of glucagon for diabetes therapy |
| WO2011075393A2 (en) | 2009-12-18 | 2011-06-23 | Indiana University Research And Technology Corporation | Glucagon/glp-1 receptor co-agonists |
| WO2011088837A1 (en) * | 2010-01-20 | 2011-07-28 | Zealand Pharma A/S | Treatment of cardiac conditions |
| KR20130018410A (ko) | 2010-03-26 | 2013-02-21 | 노보 노르디스크 에이/에스 | 새로운 글루카곤 유사체 |
| RU2012153753A (ru) | 2010-05-13 | 2014-06-20 | Индиана Юниверсити Рисерч Энд Текнолоджи Корпорейшн | Пептиды глюкагонового суперсемейства, обладающие активностью в отношении сопряженных с g-белком рецепторов |
| KR101382593B1 (ko) | 2010-07-21 | 2014-04-10 | 한미사이언스 주식회사 | 신규한 지속형 글루카곤 결합체 및 이를 포함하는 비만 예방 및 치료용 약학적 조성물 |
| NZ612297A (en) | 2010-12-22 | 2015-10-30 | Univ Indiana Res & Tech Corp | Glucagon analogs exhibiting gip receptor activity |
| WO2012150503A2 (en) | 2011-05-03 | 2012-11-08 | Zealand Pharma A/S | Glu-glp-1 dual agonist signaling-selective compounds |
| CA3134906A1 (en) | 2011-05-18 | 2012-11-22 | Mederis Diabetes, Llc | Improved peptide pharmaceuticals for insulin resistance |
| HRP20181591T1 (hr) * | 2011-06-10 | 2018-11-30 | Hanmi Science Co., Ltd. | Novi derivati oksintomodulina i farmaceutski pripravci za liječenje pretilosti koji ih sadrže |
| TWI601744B (zh) * | 2011-06-17 | 2017-10-11 | 韓美科學股份有限公司 | 包含調酸素與免疫球蛋白片段之複合物及其用途 |
| WO2013004983A1 (en) | 2011-07-04 | 2013-01-10 | Imperial Innovations Limited | Novel compounds and their effects on feeding behaviour |
| BR112014007124A2 (pt) * | 2011-11-17 | 2017-06-13 | Univ Indiana Res & Tech Corp | superfamília de peptídeos gluxagon que exibem atividade no receptor glicocorticóide |
| ES2602486T3 (es) | 2012-06-21 | 2017-02-21 | Indiana University Research And Technology Corporation | Análogos de glucagón que muestran actividad de receptor de GIP |
| SI2864350T1 (en) | 2012-06-21 | 2018-08-31 | Indiana University Research And Technology Corporation | GLUCAGON ANALOGUE ANALOGUE WITH ACTIVITY OF GIP RECEPTOR |
| AR094821A1 (es) | 2012-07-25 | 2015-09-02 | Hanmi Pharm Ind Co Ltd | Formulación líquida de un conjugado de péptido insulinotrópico de acción prolongada |
| KR101968344B1 (ko) | 2012-07-25 | 2019-04-12 | 한미약품 주식회사 | 옥신토모듈린 유도체를 포함하는 고지혈증 치료용 조성물 |
| AR092873A1 (es) | 2012-09-26 | 2015-05-06 | Cadila Healthcare Ltd | Peptidos como agonistas triples de los receptores de gip, glp-1 y glugagon |
| EA039082B1 (ru) | 2012-11-06 | 2021-12-01 | Ханми Фарм. Ко., Лтд. | Жидкая композиция белкового конъюгата, содержащего оксинтомодулин и фрагмент иммуноглобулина |
| KR101993393B1 (ko) * | 2012-11-06 | 2019-10-01 | 한미약품 주식회사 | 옥신토모듈린 유도체를 포함하는 당뇨병 또는 비만성 당뇨병 치료용 조성물 |
| EP2922877B1 (en) | 2012-11-20 | 2018-09-05 | Eumederis Pharmaceuticals, Inc. | Improved peptide pharmaceuticals |
| WO2014081872A1 (en) | 2012-11-20 | 2014-05-30 | Mederis Diabetes, Llc | Improved peptide pharmaceuticals for insulin resistance |
| HUE035803T2 (en) | 2012-12-21 | 2018-05-28 | Sanofi Sa | Dual GLP1 / GIP or trigonal GLP1 / GIP / glucagon agonists |
| BR112015025464A2 (pt) | 2013-04-18 | 2017-10-10 | Novo Nordisk As | coagonistas do receptor de glp-1/glucagon estáveis, prolongados para uso médico |
| WO2015022420A1 (en) | 2013-08-16 | 2015-02-19 | Medimmune Limited | Gip and glp-1 receptor dual-agonists for the treatment of diabetes |
| 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 |
| TWI684458B (zh) | 2014-05-30 | 2020-02-11 | 南韓商韓美藥品股份有限公司 | 包含胰島素及ｇｌｐ-１/昇糖素雙重促效劑之治療糖尿病之組成物 |
| TWI772252B (zh) | 2014-09-16 | 2022-08-01 | 南韓商韓美藥品股份有限公司 | 長效glp-1/高血糖素受體雙促效劑治療非酒精性脂肝疾病之用途 |
| CN108271356A (zh) | 2014-09-24 | 2018-07-10 | 印第安纳大学研究及科技有限公司 | 肠降血糖素-胰岛素缀合物 |
| KR102418477B1 (ko) * | 2014-12-30 | 2022-07-08 | 한미약품 주식회사 | 글루카곤 유도체 |
| KR102291020B1 (ko) | 2014-12-30 | 2021-08-20 | 한미약품 주식회사 | 안정성이 증가된 글루카곤 유도체 |
| FI3322437T3 (fi) * | 2015-06-30 | 2024-02-20 | Hanmi Pharmaceutical Co Ltd | Glukagonijohdannainen ja sen pitkävaikutteisen konjugaatin käsittävä koostumus |
| TW201718629A (zh) * | 2015-09-25 | 2017-06-01 | 韓美藥品股份有限公司 | 包含多個生理多肽及免疫球蛋白Ｆｃ區之蛋白質接合物 |
| JP6712323B2 (ja) | 2015-12-31 | 2020-06-17 | ハンミ ファーマシューティカル カンパニー リミテッド | グルカゴン、ｇｌｐ−１及びｇｉｐ受容体のすべてに活性を有する三重活性体 |
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