TW201143791A - Glucagon superfamily peptides exhibiting G protein-coupled receptor activity - Google Patents
Glucagon superfamily peptides exhibiting G protein-coupled receptor activity Download PDFInfo
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- TW201143791A TW201143791A TW100116894A TW100116894A TW201143791A TW 201143791 A TW201143791 A TW 201143791A TW 100116894 A TW100116894 A TW 100116894A TW 100116894 A TW100116894 A TW 100116894A TW 201143791 A TW201143791 A TW 201143791A
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- ILVXOBCQQYKLDS-UHFFFAOYSA-N pyridine N-oxide Chemical compound [O-][N+]1=CC=CC=C1 ILVXOBCQQYKLDS-UHFFFAOYSA-N 0.000 description 1
- 150000004728 pyruvic acid derivatives Chemical class 0.000 description 1
- IUVKMZGDUIUOCP-BTNSXGMBSA-N quinbolone Chemical compound O([C@H]1CC[C@H]2[C@H]3[C@@H]([C@]4(C=CC(=O)C=C4CC3)C)CC[C@@]21C)C1=CCCC1 IUVKMZGDUIUOCP-BTNSXGMBSA-N 0.000 description 1
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- YGSDEFSMJLZEOE-UHFFFAOYSA-N salicylic acid Chemical class OC(=O)C1=CC=CC=C1O YGSDEFSMJLZEOE-UHFFFAOYSA-N 0.000 description 1
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- 235000021286 stilbenes Nutrition 0.000 description 1
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- KDYFGRWQOYBRFD-UHFFFAOYSA-L succinate(2-) Chemical compound [O-]C(=O)CCC([O-])=O KDYFGRWQOYBRFD-UHFFFAOYSA-L 0.000 description 1
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- PXQLVRUNWNTZOS-UHFFFAOYSA-N sulfanyl Chemical compound [SH] PXQLVRUNWNTZOS-UHFFFAOYSA-N 0.000 description 1
- 125000000020 sulfo group Chemical group O=S(=O)([*])O[H] 0.000 description 1
- BDHFUVZGWQCTTF-UHFFFAOYSA-M sulfonate Chemical compound [O-]S(=O)=O BDHFUVZGWQCTTF-UHFFFAOYSA-M 0.000 description 1
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- 150000003892 tartrate salts Chemical class 0.000 description 1
- KBGARADQEFGKIS-UHFFFAOYSA-N tert-butyl 4-[(2,6-difluoro-4-pyridin-3-ylphenoxy)methyl]piperidine-1-carboxylate Chemical compound C1CN(C(=O)OC(C)(C)C)CCC1COC1=C(F)C=C(C=2C=NC=CC=2)C=C1F KBGARADQEFGKIS-UHFFFAOYSA-N 0.000 description 1
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Classifications
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- 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
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- 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
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- 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
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- 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
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- A61K47/64—Drug-peptide, drug-protein or drug-polyamino acid conjugates, i.e. the modifying agent being a peptide, protein or polyamino acid which is covalently bonded or complexed to a therapeutically active agent
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- A61P1/16—Drugs for disorders of the alimentary tract or the digestive system for liver or gallbladder disorders, e.g. hepatoprotective agents, cholagogues, litholytics
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- A61P25/28—Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
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- 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
- C07K19/00—Hybrid peptides, i.e. peptides covalently bound to nucleic acids, or non-covalently bound protein-protein complexes
Landscapes
- Health & Medical Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- Chemical & Material Sciences (AREA)
- General Health & Medical Sciences (AREA)
- Medicinal Chemistry (AREA)
- Engineering & Computer Science (AREA)
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- Pharmacology & Pharmacy (AREA)
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- Public Health (AREA)
- Animal Behavior & Ethology (AREA)
- Organic Chemistry (AREA)
- Proteomics, Peptides & Aminoacids (AREA)
- Epidemiology (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Gastroenterology & Hepatology (AREA)
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- Zoology (AREA)
- Molecular Biology (AREA)
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- Biophysics (AREA)
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- Psychiatry (AREA)
- Child & Adolescent Psychology (AREA)
- Emergency Medicine (AREA)
- Hospice & Palliative Care (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
- Peptides Or Proteins (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
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| US33443310P | 2010-05-13 | 2010-05-13 |
Publications (1)
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| TW201143791A true TW201143791A (en) | 2011-12-16 |
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| TW100116894A TW201143791A (en) | 2010-05-13 | 2011-05-13 | Glucagon superfamily peptides exhibiting G protein-coupled receptor activity |
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| US (2) | US9145451B2 (OSRAM) |
| EP (1) | EP2568993A4 (OSRAM) |
| JP (1) | JP6050746B2 (OSRAM) |
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| RU (1) | RU2012153753A (OSRAM) |
| TW (1) | TW201143791A (OSRAM) |
| WO (1) | WO2011143208A1 (OSRAM) |
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| EP2570133B1 (en) | 2005-11-07 | 2016-03-23 | Indiana University Research and Technology Corporation | Glucagon analogs exhibiting physiological solubility and stability |
| WO2008086086A2 (en) | 2007-01-05 | 2008-07-17 | Indiana University Research And Technology Corporation | Glucagon analogs exhibiting enhanced solubility in physiological ph buffers |
| KR20090119876A (ko) | 2007-02-15 | 2009-11-20 | 인디애나 유니버시티 리서치 앤드 테크놀로지 코퍼레이션 | 글루카곤/ｇｌｐ-1 수용체 공동-항진물질 |
| JP5631201B2 (ja) | 2007-03-28 | 2014-11-26 | プレジデント アンド フェローズ オブ ハーバード カレッジ | ステッチングされたポリペプチド |
| WO2009058662A2 (en) | 2007-10-30 | 2009-05-07 | Indiana University Research And Technology Corporation | Glucagon antagonists |
| WO2009058734A1 (en) | 2007-10-30 | 2009-05-07 | Indiana University Research And Technology Corporation | Compounds exhibiting glucagon antagonist and glp-1 agonist activity |
| AR072159A1 (es) | 2008-06-17 | 2010-08-11 | Univ Indiana Res & Tech Corp | Analogos de glucagon, basados en (peptido insulinotropico dependiente de la glucosa) gip para el tratamiento de trastornos metabolicos y obesidad |
| 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 |
| JP5753779B2 (ja) | 2008-06-17 | 2015-07-22 | 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 | 生理学的ｐＨの緩衝液中で向上した溶解性及び安定性を示すグルカゴン類縁体 |
| WO2010071807A1 (en) | 2008-12-19 | 2010-06-24 | Indiana University Research And Technology Corporation | Amide based glucagon superfamily peptide prodrugs |
| BRPI1014508A2 (pt) | 2009-06-16 | 2016-04-05 | Univ Indiana Res & Tech Corp | análogos de peptídeo de glucagon, dimer de dois peptídeos de glucagon, composição farmacêutica deles derivada e métodos para seu uso" |
| WO2011075393A2 (en) | 2009-12-18 | 2011-06-23 | Indiana University Research And Technology Corporation | Glucagon/glp-1 receptor co-agonists |
| BR112012018585A2 (pt) * | 2010-01-27 | 2017-01-10 | Univ Indiana Res & Tech Corp | conjungados e composições de glucagon antagonista-gip agonista para o tratamento de distúrbios metabólicos e de obesidade |
| JP6121323B2 (ja) | 2010-05-13 | 2017-05-10 | 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 | 核内ホルモン受容体の活性を示すグルカゴンスーパーファミリーのペプチド |
| WO2011143208A1 (en) | 2010-05-13 | 2011-11-17 | Indiana University Research And Technology Corporation | Glucagon superfamily peptides exhibiting g protein-coupled receptor activity |
| KR20130102470A (ko) | 2010-06-24 | 2013-09-17 | 인디애나 유니버시티 리서치 앤드 테크놀로지 코퍼레이션 | 아미드계 글루카곤 슈퍼패밀리 펩티드 프로드러그 |
| MX355543B (es) | 2010-08-13 | 2018-04-20 | Aileron Therapeutics Inc Star | Macrociclos peptidomiméticos. |
| JP6086067B2 (ja) | 2010-12-22 | 2017-03-01 | インディアナ ユニヴァーシティ リサーチ アンド テクノロジー コーポレイション | Ｇｉｐレセプター活性を示すグルカゴンアナローグ |
| ES2692187T3 (es) | 2011-06-10 | 2018-11-30 | Hanmi Science Co., Ltd. | Nuevos derivados de oxintomodulina y composición farmacéutica para el tratamiento de obesidad que lo comprende |
| PH12013502517A1 (en) | 2011-06-17 | 2014-01-20 | Hanmi Science Co Ltd | A conjugate comprising oxyntomodulin and an immunoglobulin fragment, and use thereof |
| US8729017B2 (en) | 2011-06-22 | 2014-05-20 | Indiana University Research And Technology Corporation | Glucagon/GLP-1 receptor co-agonists |
| MX347703B (es) | 2011-06-22 | 2017-05-09 | Univ Indiana Res & Tech Corp | Co-agonistas del receptor de glucagon/glp-1. |
| TWI643868B (zh) | 2011-10-18 | 2018-12-11 | 艾利倫治療公司 | 擬肽巨環化合物 |
| KR20140097151A (ko) | 2011-11-17 | 2014-08-06 | 인디애나 유니버시티 리서치 앤드 테크놀로지 코퍼레이션 | 글루코코르티코이드 수용체 활성을 나타내는 글루카곤 슈퍼패밀리 펩티드 |
| EP2819688A4 (en) | 2012-02-15 | 2015-10-28 | Aileron Therapeutics Inc | PEPTIDOMIMETIC MACROCYCLES CROSS-LINKED WITH TRIAZOLE AND THIOETHER |
| SG11201404648PA (en) | 2012-02-15 | 2014-09-26 | Aileron Therapeutics Inc | Peptidomimetic macrocycles |
| US9340600B2 (en) | 2012-06-21 | 2016-05-17 | Indiana University Research And Technology Corporation | Glucagon analogs exhibiting GIP receptor activity |
| KR101968344B1 (ko) | 2012-07-25 | 2019-04-12 | 한미약품 주식회사 | 옥신토모듈린 유도체를 포함하는 고지혈증 치료용 조성물 |
| UA116217C2 (uk) | 2012-10-09 | 2018-02-26 | Санофі | Пептидна сполука як подвійний агоніст рецепторів glp1-1 та глюкагону |
| KR20150082307A (ko) | 2012-11-01 | 2015-07-15 | 에일러론 테라퓨틱스 인코포레이티드 | 이치환 아미노산 및 이의 제조 및 사용 방법 |
| KR101993393B1 (ko) | 2012-11-06 | 2019-10-01 | 한미약품 주식회사 | 옥신토모듈린 유도체를 포함하는 당뇨병 또는 비만성 당뇨병 치료용 조성물 |
| ES2748158T3 (es) | 2012-11-06 | 2020-03-13 | Hanmi Pharm Ind Co Ltd | Formulación líquida de conjugado de proteínas que comprende la oxintomodulina y un fragmento de inmunoglobulina |
| MX362190B (es) | 2012-12-21 | 2019-01-08 | Sanofi Sa | Agonistas duales de glp1/gip o trigonales de glp1/gip/glucagon. |
| AU2014359894B2 (en) | 2013-12-06 | 2020-09-17 | Baikang (Suzhou) Co., Ltd | Bioreversable promoieties for nitrogen-containing and hydroxyl-containing drugs |
| 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 |
| WO2015086729A1 (en) | 2013-12-13 | 2015-06-18 | Sanofi | Dual glp-1/gip receptor agonists |
| WO2015086728A1 (en) | 2013-12-13 | 2015-06-18 | Sanofi | Exendin-4 peptide analogues as dual glp-1/gip receptor agonists |
| AR098614A1 (es) * | 2013-12-18 | 2016-06-01 | Lilly Co Eli | Compuesto para el tratamiento de hipoglicemia severa |
| AR098616A1 (es) | 2013-12-18 | 2016-06-01 | Lilly Co Eli | Péptido para el tratamiento de hipoglicemia severa |
| WO2015111971A1 (ko) * | 2014-01-23 | 2015-07-30 | 동국대학교 산학협력단 | Gpr119 리간드를 유효성분으로 포함하는 비알콜성 지방간 질환의 예방 또는 치료용 약학적 조성물 |
| KR101665846B1 (ko) * | 2014-01-23 | 2016-10-12 | 동국대학교 산학협력단 | Gpr119 리간드를 유효성분으로 포함하는 비알콜성 지방간 질환의 예방 또는 치료용 약학적 조성물 |
| 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 |
| 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 |
| US9932381B2 (en) | 2014-06-18 | 2018-04-03 | Sanofi | Exendin-4 derivatives as selective glucagon receptor agonists |
| 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 |
| SG11201702223UA (en) | 2014-09-24 | 2017-04-27 | Aileron Therapeutics Inc | Peptidomimetic macrocycles and uses thereof |
| MD20170055A2 (ro) | 2014-10-24 | 2017-09-30 | Merck Sharp & Dohme Corp | Co-agonişti ai receptorilor glucagonului şi GLP-1 |
| KR102418477B1 (ko) | 2014-12-30 | 2022-07-08 | 한미약품 주식회사 | 글루카곤 유도체 |
| EP3575314B1 (en) | 2014-12-30 | 2024-02-14 | Hanmi Pharm. Co., Ltd. | Glucagon derivative |
| BR112017014194A2 (pt) | 2015-01-23 | 2018-01-09 | Novartis Ag | conjugados de ácido graxo de apelina sintéticos com meia-vida melhorada |
| KR20170129879A (ko) | 2015-03-20 | 2017-11-27 | 에일러론 테라퓨틱스 인코포레이티드 | 펩티드모방 거대고리 및 이의 용도 |
| US20180074053A1 (en) * | 2015-04-03 | 2018-03-15 | Zhongmin Ma | Treatment of diabetes using agonists of the mas-related gpcr d |
| AR105319A1 (es) | 2015-06-05 | 2017-09-27 | Sanofi Sa | Profármacos que comprenden un conjugado agonista dual de glp-1 / glucagón conector ácido hialurónico |
| EP3322437B1 (en) | 2015-06-30 | 2024-01-17 | Hanmi Pharm. Co., Ltd. | Glucagon derivative and a composition comprising a long acting conjugate of the same |
| 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 |
| EP3144413B1 (en) * | 2015-09-21 | 2018-04-25 | ATOTECH Deutschland GmbH | Plating bath composition for electroless plating of gold |
| TWI622596B (zh) | 2015-10-26 | 2018-05-01 | 美國禮來大藥廠 | 升糖素受體促效劑 |
| WO2017075583A2 (en) * | 2015-10-30 | 2017-05-04 | The Research Foundation For The State University Of New York | Oxyntomodulin analogs and methods of making and using same |
| KR101946516B1 (ko) * | 2015-11-19 | 2019-02-11 | (주)파메딕스 | Gpr119 리간드를 유효성분으로 포함하는 간 섬유화 예방 또는 치료용 약학적 조성물 |
| US10493125B2 (en) | 2015-12-09 | 2019-12-03 | Merck Sharp & Dohme Corp. | Co-agonists of the glucagon and GLP-1 receptors |
| KR102508651B1 (ko) | 2015-12-23 | 2023-03-13 | 더 존스 홉킨스 유니버시티 | 신경계 및 신경변성 상태의 요법으로서 장기간 작용하는 glf-1r 작용제 |
| CN116059389A (zh) | 2015-12-31 | 2023-05-05 | 韩美药品株式会社 | 胰高血糖素/glp-1/gip受体三重激动剂的长效缀合物 |
| WO2017160669A1 (en) * | 2016-03-18 | 2017-09-21 | Merck Sharp & Dohme Corp. | Insulin-incretin conjugates |
| BR112018077457A2 (pt) | 2016-06-29 | 2019-04-02 | Hanmi Pharm. Co., Ltd. | composição farmacêutica para evitar ou tratar hiperinsulinismo congênito e seu método, hipoglicemia e seu método, síndrome metabólica e seu método e peptídeo isolado |
| KR102708681B1 (ko) | 2018-02-13 | 2024-09-26 | 길리애드 사이언시즈, 인코포레이티드 | Pd-1/pd-l1 억제제 |
| EP3781556B1 (en) | 2018-04-19 | 2025-06-18 | Gilead Sciences, Inc. | Pd-1/pd-l1 inhibitors |
| EP3788063B1 (en) | 2018-05-04 | 2023-08-09 | Novo Nordisk A/S | Gip derivatives and uses thereof |
| CN118221646A (zh) | 2018-07-13 | 2024-06-21 | 吉利德科学公司 | Pd-1/pd-l1抑制剂 |
| KR102635333B1 (ko) | 2018-10-24 | 2024-02-15 | 길리애드 사이언시즈, 인코포레이티드 | Pd-1/pd-l1 억제제 |
| EP4021909A4 (en) | 2019-08-29 | 2023-08-30 | David C. Martin | Biofunctional thiophene monomers |
| WO2021083306A1 (zh) * | 2019-10-31 | 2021-05-06 | 东莞市东阳光生物药研发有限公司 | Glp-1/gcg双受体激动剂多肽 |
| EP3842060A1 (en) * | 2019-12-23 | 2021-06-30 | Merck Sharp & Dohme Corp. | Stapled lactam co-agonists of the glucagon and glp-1 receptors |
| EP4161577A1 (en) * | 2020-06-03 | 2023-04-12 | Københavns Universitet | Glp1r agonist nmdar antagonist conjugates |
| JP2023550594A (ja) * | 2020-10-30 | 2023-12-04 | ノヴォ ノルディスク アー／エス | Ｇｌｐ－１、ｇｉｐ、およびグルカゴン受容体三重作動薬 |
| JP7688891B2 (ja) * | 2021-01-18 | 2025-06-05 | 国立大学法人東海国立大学機構 | ペプチド |
| WO2023069452A1 (en) * | 2021-10-19 | 2023-04-27 | Oncogenuity, Inc. | Salt bridge modified peptide nucleic acid compositions and methods of use thereof |
| CA3239054A1 (en) | 2021-12-02 | 2023-06-08 | Kobenhavns Universitet | Peptide-drug conjugates for treatment of neurodegenerative diseases |
| CN114317549B (zh) * | 2022-01-08 | 2022-08-19 | 河南大学 | 毒蕈型c型乙酰胆碱受体在飞蝗防治中的应用 |
| CN117757023B (zh) * | 2023-12-27 | 2025-04-29 | 西安石油大油气科技有限公司 | 含甜菜碱型表面活性剂的高盐低渗油藏驱油剂及制备方法 |
Family Cites Families (112)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| 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 |
| US5539084A (en) | 1989-02-17 | 1996-07-23 | Coselco Mimotopes Pty. Ltd. | Method for the use and synthesis of peptides |
| 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 |
| 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 |
| 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 |
| WO1997029180A1 (en) | 1996-02-06 | 1997-08-14 | 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) |
| IL138214A0 (en) | 1998-03-09 | 2001-10-31 | Zealand Pharmaceuticals As | Pharmacolgically 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 |
| JP2002526554A (ja) | 1998-10-07 | 2002-08-20 | メディカル カレッジ オブ ジョージア リサーチ インスティチュート，インコーポレイテッド | 骨親和性ホルモンとして用いられるグルコース依存性インスリン親和性ペプチド |
| JP2002534512A (ja) | 1999-01-15 | 2002-10-15 | ノボ ノルディスク アクティーゼルスカブ | 非ペプチドｇｌｐ−１アゴニスト |
| GB0404124D0 (en) | 2004-02-25 | 2004-03-31 | Univ Ulster | Antagonists of GIP |
| ATE272650T1 (de) | 1999-03-29 | 2004-08-15 | Uutech Ltd | Analoge des magensaft inhibierenden peptides und ihre verwendung für die behandlung von diabetes |
| DK1180121T3 (da) | 1999-05-17 | 2004-03-01 | Conjuchem Inc | Langtidsvirkende insulinotrope peptider |
| EP1356295A2 (en) | 2000-04-27 | 2003-10-29 | Bionebraska, Inc. | Gastric inhibitory polypeptide diagnostic test for detecting susceptibility to type-2 diabetes, impaired glucose tolerance, or impaired fasting glucos |
| US6677136B2 (en) | 2000-05-03 | 2004-01-13 | Amgen Inc. | Glucagon antagonists |
| JP2004503565A (ja) | 2000-06-14 | 2004-02-05 | サイトヴァックス・バイオテクノロジーズ・インコーポレーテッド | 構造特異的ペプチドを生産するためのコイルドコイル構造的骨格の使用 |
| AU2001264791B2 (en) | 2000-06-16 | 2006-11-23 | Eli Lilly And Company | Glucagon-like peptide-1 analogs |
| WO2002010195A2 (en) | 2000-08-02 | 2002-02-07 | Theratechnologies Inc. | Modified peptides with increased potency |
| US6846831B2 (en) | 2000-08-15 | 2005-01-25 | Cpd, Llc | Method of treating the syndrome of lipodystrophy |
| US6262062B1 (en) | 2000-08-15 | 2001-07-17 | Cpd, Llc | Method of treating the syndrome of coronary heart disease risk factors in humans |
| 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 |
| ES2367891T3 (es) | 2000-09-29 | 2011-11-10 | Schering Corporation | Interleucina-10 pegilada. |
| 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 |
| JP2005509409A (ja) | 2001-08-08 | 2005-04-14 | ジェンザイム・コーポレーション | 糖尿病および他の血糖疾患の治療方法 |
| CN1635900A (zh) | 2001-08-28 | 2005-07-06 | 伊莱利利公司 | Glp－1和基础胰岛素的预混合物 |
| GB0121709D0 (en) | 2001-09-07 | 2001-10-31 | Imp College Innovations Ltd | Food inhibition agent |
| 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 |
| 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 |
| EP1572892A4 (en) | 2001-10-18 | 2007-08-22 | Bristol Myers Squibb Co | HUMAN GLUCAGON-LIKE-PEPTIDE-1 MIMICS AND THEIR USE IN THE TREATMENT OF DIABETES AND RELATED CONDITIONS |
| JP2005508360A (ja) | 2001-10-19 | 2005-03-31 | イーライ・リリー・アンド・カンパニー | Ｇｌｐ−１およびインスリンの二相混合物 |
| JP2005518408A (ja) | 2001-12-29 | 2005-06-23 | ノボ ノルディスク アクティーゼルスカブ | 異常脂肪血症を治療するための、ｇｌｐ−１化合物と他の薬物との組み合わせ使用 |
| 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 |
| WO2003103572A2 (en) | 2002-06-04 | 2003-12-18 | Eli Lilly And Company | Modified glucagon-like peptide-1 analogs |
| JP2006502100A (ja) | 2002-06-11 | 2006-01-19 | エーザイ株式会社 | 細胞の異常消失に関わる障害の治療のための、および／または、肥満の治療のためのｇｉｐ活性を有する化合物の使用 |
| AU2003248676A1 (en) | 2002-06-15 | 2003-12-31 | Enteromed, Inc. | Treatment of non-alcoholic fatty liver disease |
| EP1539210A4 (en) | 2002-09-06 | 2006-06-07 | Bayer Pharmaceuticals Corp | GLP-1 RECEPTOR MODIFIED AGONISTS AND THEIR PHARMACOLOGICAL METHODS OF USE |
| US7192922B2 (en) | 2002-11-19 | 2007-03-20 | Allegheny-Singer Research Institute | Method of treating left ventricular dysfunction |
| US20050059605A1 (en) | 2003-01-31 | 2005-03-17 | Krishna Peri | Chemically modified metabolites of regulatory peptides and methods of producing and using same |
| EP1626981A4 (en) | 2003-03-04 | 2006-11-22 | Biorexis Pharmaceutical Corp | PROTEINS PROTECTED AGAINST DIPEPTIDYLPEPTIDASE |
| US20070060512A1 (en) * | 2003-03-04 | 2007-03-15 | Homayoun Sadeghi | Dipeptidyl-peptidase protected protein |
| EA009366B1 (ru) | 2003-03-19 | 2007-12-28 | Эли Лилли Энд Компани | Связанные с полиэтиленгликолем соединения гпп-1 |
| JP4698579B2 (ja) | 2003-04-08 | 2011-06-08 | イエダ リサーチ アンド デベロップメント カンパニー リミテッド | 可逆的ｐｅｇ化薬物 |
| CA2525574C (en) | 2003-05-15 | 2015-06-30 | Trustees Of Tufts College | Stable analogs of peptide and polypeptide therapeutics |
| KR101293507B1 (ko) | 2003-06-03 | 2013-08-06 | 노보 노르디스크 에이/에스 | 안정화된 약학적 펩티드 조성물 |
| WO2004105790A1 (en) | 2003-06-03 | 2004-12-09 | Novo Nordisk A/S | Stabilized pharmaceutical peptide compositions |
| AU2004251145C1 (en) | 2003-06-12 | 2011-04-14 | Eli Lilly And Company | GLP-1 analog fusion proteins |
| US20050124550A1 (en) | 2003-06-18 | 2005-06-09 | Peri Krishna G. | Compounds that modulate the glucagon response and uses thereof |
| KR101241862B1 (ko) | 2003-09-19 | 2013-03-13 | 노보 노르디스크 에이/에스 | 신규 ｇｌｐ-1 유도체 |
| 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 |
| AU2004298424A1 (en) | 2003-12-18 | 2005-06-30 | Novo Nordisk A/S | Novel 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 |
| EP2390264A1 (en) | 2005-02-11 | 2011-11-30 | Amylin Pharmaceuticals Inc. | GIP analog and hybrid polypeptides with selectable propperties |
| 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 |
| KR101011081B1 (ko) | 2005-05-13 | 2011-01-25 | 일라이 릴리 앤드 캄파니 | Ｐｅｇ화된 ｇｌｐ-1 화합물 |
| SI1891105T1 (sl) | 2005-06-13 | 2012-07-31 | Imp Innovations Ltd | Analogi oksintomodulina in njihovi učinki na prehranjevalno vedenje |
| EP2330124B1 (en) | 2005-08-11 | 2015-02-25 | Amylin Pharmaceuticals, LLC | Hybrid polypeptides with selectable properties |
| 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 |
| US20090170762A1 (en) | 2005-09-08 | 2009-07-02 | Uutech Limited | Treatment of Diabetes Related Obesity |
| WO2007047834A2 (en) | 2005-10-18 | 2007-04-26 | Biocon Limited | Oral peptide conjugates for metabolic diseases |
| EP2570133B1 (en) | 2005-11-07 | 2016-03-23 | Indiana University Research and Technology Corporation | Glucagon analogs exhibiting physiological solubility and stability |
| WO2007100535A2 (en) | 2006-02-22 | 2007-09-07 | Merck & Co., Inc. | Oxyntomodulin derivatives |
| EP2241327A1 (en) | 2006-03-15 | 2010-10-20 | Novo Nordisk A/S | Mixtures of Amylin and Insulin |
| WO2007109354A2 (en) | 2006-03-21 | 2007-09-27 | Amylin Pharmaceuticals, Inc. | Peptide-peptidase inhibitor conjugates and methods of using same |
| CA2655923A1 (en) * | 2006-07-06 | 2008-01-10 | Amylin Pharmaceuticals, Inc. | Glucagon-like peptides and uses thereof |
| WO2008022015A2 (en) | 2006-08-11 | 2008-02-21 | Trustees Of Tufts College | Retro-inverso incretin analogues, and methods of use thereof |
| JP5399244B2 (ja) | 2006-08-17 | 2014-01-29 | 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 | 選択可能な特性を持つｄｐｐ−ｉｖ耐性ｇｉｐハイブリッドポリペプチド |
| EP2057189B1 (en) | 2006-08-25 | 2013-03-06 | Novo Nordisk A/S | Acylated exendin-4 compounds |
| CN104193815A (zh) | 2006-09-08 | 2014-12-10 | Ambrx公司 | 经修饰的人类血浆多肽或Fc骨架和其用途 |
| 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 |
| US8617531B2 (en) | 2006-12-14 | 2013-12-31 | Bolder Biotechnology, Inc. | Methods of making proteins and peptides containing a single free cysteine |
| WO2008086086A2 (en) | 2007-01-05 | 2008-07-17 | Indiana University Research And Technology Corporation | Glucagon analogs exhibiting enhanced solubility in physiological ph buffers |
| KR20090119876A (ko) | 2007-02-15 | 2009-11-20 | 인디애나 유니버시티 리서치 앤드 테크놀로지 코퍼레이션 | 글루카곤/ｇｌｐ-1 수용체 공동-항진물질 |
| EP2190873B1 (en) | 2007-09-05 | 2015-07-22 | Novo Nordisk A/S | Truncated glp-1 derivatives and their therapeutical use |
| EP2190872B1 (en) | 2007-09-05 | 2018-03-14 | Novo Nordisk A/S | Glucagon-like peptide-1 derivatives and their pharmaceutical use |
| EP2200626A4 (en) | 2007-09-07 | 2012-02-15 | Ipsen Pharma Sas | ANALOGUE OF EXENDIN-4 AND EXENDIN-3 |
| EP2036539A1 (en) | 2007-09-11 | 2009-03-18 | Novo Nordisk A/S | Stable formulations of amylin and its analogues |
| EP2200635A1 (en) | 2007-09-11 | 2010-06-30 | Novo Nordisk A/S | Mixture comprising an amylin peptide and a protracted insulin |
| EP2036923A1 (en) | 2007-09-11 | 2009-03-18 | Novo Nordisk A/S | Improved derivates of amylin |
| WO2009058734A1 (en) | 2007-10-30 | 2009-05-07 | Indiana University Research And Technology Corporation | Compounds exhibiting glucagon antagonist and glp-1 agonist activity |
| WO2009058662A2 (en) | 2007-10-30 | 2009-05-07 | Indiana University Research And Technology Corporation | Glucagon antagonists |
| US20110065633A1 (en) | 2008-01-30 | 2011-03-17 | Indiana University Research And Technology Corporation | Ester-based peptide prodrugs |
| MX2010008024A (es) | 2008-02-01 | 2010-12-21 | Ascendis Pharma As | Profarmaco que comprende un enlazador que se puede separar por si mismo. |
| 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 |
| AR072159A1 (es) | 2008-06-17 | 2010-08-11 | Univ Indiana Res & Tech Corp | Analogos de glucagon, basados en (peptido insulinotropico dependiente de la glucosa) gip para el tratamiento de trastornos metabolicos y obesidad |
| JP5753779B2 (ja) | 2008-06-17 | 2015-07-22 | 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 | 生理学的ｐＨの緩衝液中で向上した溶解性及び安定性を示すグルカゴン類縁体 |
| US20110237493A1 (en) | 2008-12-19 | 2011-09-29 | Indiana University Research And Technology Corporation | Dipeptide linked medicinal agents |
| WO2010071807A1 (en) | 2008-12-19 | 2010-06-24 | Indiana University Research And Technology Corporation | Amide based glucagon superfamily peptide prodrugs |
| WO2010096052A1 (en) | 2009-02-19 | 2010-08-26 | Merck Sharp & Dohme Corp. | Oxyntomodulin analogs |
| BRPI1014508A2 (pt) | 2009-06-16 | 2016-04-05 | Univ Indiana Res & Tech Corp | análogos de peptídeo de glucagon, dimer de dois peptídeos de glucagon, composição farmacêutica deles derivada e métodos para seu uso" |
| WO2011075393A2 (en) | 2009-12-18 | 2011-06-23 | 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 |
| BR112012018585A2 (pt) | 2010-01-27 | 2017-01-10 | Univ Indiana Res & Tech Corp | conjungados e composições de glucagon antagonista-gip agonista para o tratamento de distúrbios metabólicos e de obesidade |
| 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 |
| JP6121323B2 (ja) | 2010-05-13 | 2017-05-10 | 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 | 核内ホルモン受容体の活性を示すグルカゴンスーパーファミリーのペプチド |
| WO2011143208A1 (en) | 2010-05-13 | 2011-11-17 | Indiana University Research And Technology Corporation | Glucagon superfamily peptides exhibiting g protein-coupled receptor activity |
| KR20130102470A (ko) | 2010-06-24 | 2013-09-17 | 인디애나 유니버시티 리서치 앤드 테크놀로지 코퍼레이션 | 아미드계 글루카곤 슈퍼패밀리 펩티드 프로드러그 |
| 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 |
-
2011
- 2011-05-10 WO PCT/US2011/035912 patent/WO2011143208A1/en not_active Ceased
- 2011-05-10 MX MX2012013005A patent/MX2012013005A/es not_active Application Discontinuation
- 2011-05-10 CN CN2011800371114A patent/CN103179976A/zh active Pending
- 2011-05-10 EP EP20110781136 patent/EP2568993A4/en not_active Withdrawn
- 2011-05-10 CA CA 2797089 patent/CA2797089A1/en not_active Abandoned
- 2011-05-10 BR BR112012028707A patent/BR112012028707A2/pt not_active IP Right Cessation
- 2011-05-10 US US13/697,017 patent/US9145451B2/en not_active Expired - Fee Related
- 2011-05-10 RU RU2012153753/04A patent/RU2012153753A/ru not_active Application Discontinuation
- 2011-05-10 KR KR20127029584A patent/KR20130111923A/ko not_active Withdrawn
- 2011-05-10 JP JP2013510239A patent/JP6050746B2/ja not_active Expired - Fee Related
- 2011-05-12 AR ARP110101648 patent/AR081042A1/es unknown
- 2011-05-13 TW TW100116894A patent/TW201143791A/zh unknown
-
2015
- 2015-08-28 US US14/838,991 patent/US20160051688A1/en not_active Abandoned
Also Published As
| Publication number | Publication date |
|---|---|
| MX2012013005A (es) | 2013-02-26 |
| JP6050746B2 (ja) | 2016-12-21 |
| AR081042A1 (es) | 2012-05-30 |
| US20160051688A1 (en) | 2016-02-25 |
| CA2797089A1 (en) | 2011-11-17 |
| CN103179976A (zh) | 2013-06-26 |
| EP2568993A1 (en) | 2013-03-20 |
| JP2013533849A (ja) | 2013-08-29 |
| US9145451B2 (en) | 2015-09-29 |
| RU2012153753A (ru) | 2014-06-20 |
| WO2011143208A1 (en) | 2011-11-17 |
| BR112012028707A2 (pt) | 2019-09-24 |
| KR20130111923A (ko) | 2013-10-11 |
| US20130116172A1 (en) | 2013-05-09 |
| EP2568993A4 (en) | 2014-02-19 |
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