AR091478A1 - Analogos de glucagon que exhiben actividad de receptor de gip (peptido insulinotropico dependiente de glucosa) - Google Patents
Analogos de glucagon que exhiben actividad de receptor de gip (peptido insulinotropico dependiente de glucosa)Info
- Publication number
- AR091478A1 AR091478A1 ARP130102143A AR091478A1 AR 091478 A1 AR091478 A1 AR 091478A1 AR P130102143 A ARP130102143 A AR P130102143A AR 091478 A1 AR091478 A1 AR 091478A1
- Authority
- AR
- Argentina
- Prior art keywords
- amino acid
- receptor
- glucagon analog
- glucagon
- optionally
- Prior art date
Links
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
- A61K38/00—Medicinal preparations containing peptides
- 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
- A61K38/26—Glucagons
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P3/00—Drugs for disorders of the metabolism
- A61P3/04—Anorexiants; Antiobesity agents
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P3/00—Drugs for disorders of the metabolism
- A61P3/08—Drugs for disorders of the metabolism for glucose homeostasis
- A61P3/10—Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P5/00—Drugs for disorders of the endocrine system
- A61P5/48—Drugs for disorders of the endocrine system of the pancreatic hormones
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P5/00—Drugs for disorders of the endocrine system
- A61P5/48—Drugs for disorders of the endocrine system of the pancreatic hormones
- A61P5/50—Drugs for disorders of the endocrine system of the pancreatic hormones for increasing or potentiating the activity of insulin
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P7/00—Drugs for disorders of the blood or the extracellular fluid
- A61P7/12—Antidiuretics, e.g. drugs for diabetes insipidus
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K38/00—Medicinal preparations containing peptides
Landscapes
- Health & Medical Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Medicinal Chemistry (AREA)
- General Health & Medical Sciences (AREA)
- Diabetes (AREA)
- Endocrinology (AREA)
- Engineering & Computer Science (AREA)
- Pharmacology & Pharmacy (AREA)
- Animal Behavior & Ethology (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Zoology (AREA)
- Proteomics, Peptides & Aminoacids (AREA)
- Gastroenterology & Hepatology (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Molecular Biology (AREA)
- Toxicology (AREA)
- Biochemistry (AREA)
- Biophysics (AREA)
- Genetics & Genomics (AREA)
- Hematology (AREA)
- Obesity (AREA)
- Epidemiology (AREA)
- Immunology (AREA)
- Emergency Medicine (AREA)
- Child & Adolescent Psychology (AREA)
- Peptides Or Proteins (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Measurement And Recording Of Electrical Phenomena And Electrical Characteristics Of The Living Body (AREA)
- Measuring Pulse, Heart Rate, Blood Pressure Or Blood Flow (AREA)
Abstract
Se proporcionan en la presente análogos de glucagón, se contemplan para usar en el tratamiento de diabetes y obesidad. En formas de realización de ejemplo, el análogo de glucagón de las presentes descripciones exhiben una EC50 en el receptor de GLP que está dentro del rango nanomolar o picomolar. Reivindicación 1: Un análogo de glucagón nativo, que opcionalmente comprende la secuencia de aminoácidos de SEQ ID Nº 140, que comprende: A) en la posición 1 un aminoácido que comprende una cadena lateral de Tyr, His, Thio Ala o Phe, en donde el carbono a del aminoácido en la posición 1 se une con una estructura seleccionada del grupo que consiste en: (i) H₂N-(CH₂)-; (ii) H₂N-; (iii) H(acetil)N-(CH₂)₀₋₁-; y (iv) H- o CH₃-; B) en cualquiera de las posiciones 9, 10, 12, 20 ó 37 - 43 un aminoácido acilado o aminoácido alquilado, opcionalmente en donde el grupo acilo o alquilo se liga con el aminoácido por medio de un espaciador; C) una a hélice que estabiliza el aminoácido en una o varias de las posiciones 16 - 21; y D) hasta diez modificaciones de aminoácidos adicionales respecto del glucagón nativo; en donde el aminoácido en la posición 1 es un estereoisómero L o estereoisómero D, en donde, opcionalmente, el aminoácido en la posición 1 es distinto de L-His, L-Tyr y L-Phe, en donde, cuando el análogo de glucagón carece de un resto hidrofílico, el análogo de glucagón exhibe una EC50 en el receptor de GIF humano inferior o de aproximadamente 0,5 nM y en donde el análogo de glucagón tiene una selectividad inferior a 100 veces por el receptor de GLP-1 humano versus el receptor de GLP.
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201261662874P | 2012-06-21 | 2012-06-21 | |
| US201361787973P | 2013-03-15 | 2013-03-15 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| AR091478A1 true AR091478A1 (es) | 2015-02-04 |
Family
ID=48692696
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| ARP130102143 AR091478A1 (es) | 2012-06-21 | 2013-06-18 | Analogos de glucagon que exhiben actividad de receptor de gip (peptido insulinotropico dependiente de glucosa) |
Country Status (30)
| Country | Link |
|---|---|
| US (2) | US9868772B2 (es) |
| EP (1) | EP2864350B1 (es) |
| JP (1) | JP6300239B2 (es) |
| KR (1) | KR20150039748A (es) |
| CN (1) | CN104583233B (es) |
| AR (1) | AR091478A1 (es) |
| AU (1) | AU2013277372B2 (es) |
| BR (1) | BR112014031671A2 (es) |
| CA (1) | CA2877127A1 (es) |
| CL (1) | CL2014003421A1 (es) |
| CO (1) | CO7170125A2 (es) |
| CR (1) | CR20150015A (es) |
| DK (1) | DK2864350T3 (es) |
| EA (1) | EA029025B1 (es) |
| ES (1) | ES2674946T3 (es) |
| HR (1) | HRP20180936T1 (es) |
| HU (1) | HUE039267T2 (es) |
| IL (1) | IL236386B (es) |
| MX (1) | MX356000B (es) |
| MY (1) | MY185217A (es) |
| PE (1) | PE20150863A1 (es) |
| PH (1) | PH12014502857A1 (es) |
| PL (1) | PL2864350T3 (es) |
| PT (1) | PT2864350T (es) |
| RS (1) | RS57347B1 (es) |
| SG (1) | SG11201408491SA (es) |
| SI (1) | SI2864350T1 (es) |
| TR (1) | TR201808818T4 (es) |
| TW (1) | TWI644920B (es) |
| WO (1) | WO2013192130A1 (es) |
Families Citing this family (41)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| UY34763A (es) | 2012-04-26 | 2013-10-31 | Bristol Myers Squibb Co | Inhibidores de la agregación plaquetaria |
| TR201808818T4 (tr) * | 2012-06-21 | 2018-07-23 | Novo Nordisk As | Gip reseptör aktivitesi sergileyen glukagon analogları. |
| UA116217C2 (uk) | 2012-10-09 | 2018-02-26 | Санофі | Пептидна сполука як подвійний агоніст рецепторів glp1-1 та глюкагону |
| KR20150096684A (ko) | 2012-12-21 | 2015-08-25 | 사노피 | 엑센딘-4 유도체 |
| DK3004155T3 (da) | 2013-05-28 | 2022-01-03 | Takeda Pharmaceuticals Co | Peptidforbindelse |
| WO2015086729A1 (en) | 2013-12-13 | 2015-06-18 | Sanofi | Dual glp-1/gip receptor agonists |
| EP3080149A1 (en) | 2013-12-13 | 2016-10-19 | Sanofi | Dual glp-1/glucagon receptor agonists |
| EP3080150B1 (en) | 2013-12-13 | 2018-08-01 | Sanofi | Exendin-4 peptide analogues as dual glp-1/gip receptor agonists |
| WO2015086730A1 (en) | 2013-12-13 | 2015-06-18 | Sanofi | Non-acylated exendin-4 peptide analogues |
| JP2017504598A (ja) * | 2013-12-20 | 2017-02-09 | 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 | 脂質化インクレチン受容体リガンドヒト免疫グロブリンｆｃ−領域融合ポリペプチド |
| 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 |
| 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 |
| US9932381B2 (en) | 2014-06-18 | 2018-04-03 | Sanofi | Exendin-4 derivatives as selective glucagon receptor agonists |
| WO2016065090A1 (en) | 2014-10-24 | 2016-04-28 | Merck Sharp & Dohme Corp. | Co-agonists of the glucagon and glp-1 receptors |
| MA40709B1 (fr) | 2014-12-30 | 2019-07-31 | Hanmi Pharmaceutical Co Ltd | Dérivé du glucagon à stabilité améliorée |
| AR105319A1 (es) | 2015-06-05 | 2017-09-27 | Sanofi Sa | Profármacos que comprenden un conjugado agonista dual de glp-1 / glucagón conector ácido hialurónico |
| DK3322437T3 (da) | 2015-06-30 | 2024-03-25 | Hanmi Pharmaceutical Co Ltd | Glukagonderivat og en sammensætning omfattende et langtidsvirkende konjugat af samme |
| AR105284A1 (es) | 2015-07-10 | 2017-09-20 | Sanofi Sa | Derivados de exendina-4 como agonistas peptídicos duales específicos de los receptores de glp-1 / glucagón |
| TWI622596B (zh) | 2015-10-26 | 2018-05-01 | 美國禮來大藥廠 | 升糖素受體促效劑 |
| CN108697768B (zh) | 2015-12-23 | 2022-07-22 | 约翰霍普金斯大学 | 长效glp-1r激动剂作为神经***病状和神经退行性病状的治疗方法 |
| TN2018000231A1 (en) * | 2015-12-31 | 2019-10-04 | Hanmi Pharm Ind Co Ltd | Long-acting conjugate of triple glucagon/glp-1/gip receptor agonist |
| CA3024962A1 (en) | 2016-05-24 | 2017-11-30 | Takeda Pharmaceutical Company Limited | Peptide compound |
| EP3479841A4 (en) | 2016-06-29 | 2020-03-04 | Hanmi Pharm. Co., Ltd. | GLUCAGON DERIVATIVE, CONJUGATE THEREOF, COMPOSITION COMPRISING SAME, AND THERAPEUTIC USE THEREOF |
| AR110301A1 (es) | 2016-12-02 | 2019-03-13 | Sanofi Sa | Compuestos como agonistas peptídicos de receptores de glp1 / glucagón / gip |
| TW201833132A (zh) | 2016-12-02 | 2018-09-16 | 法商賽諾菲公司 | 作為肽類ｇｌｐ１／升糖素／ｇｉｐ三重受體激動劑之新穎化合物 |
| JOP20180028A1 (ar) | 2017-03-31 | 2019-01-30 | Takeda Pharmaceuticals Co | مركب ببتيد |
| CN115304666A (zh) * | 2017-11-24 | 2022-11-08 | 浙江道尔生物科技有限公司 | 一种治疗代谢疾病的胰高血糖素类似物 |
| WO2019197469A1 (en) | 2018-04-10 | 2019-10-17 | Sanofi-Aventis Deutschland Gmbh | Lixisenatide synthesis with capping |
| JP7434169B2 (ja) | 2018-04-10 | 2024-02-20 | サノフィ－アベンティス・ドイチュラント・ゲゼルシャフト・ミット・ベシュレンクテル・ハフツング | 固相からの固相結合ペプチドの切断方法 |
| CA3097939A1 (en) * | 2018-05-04 | 2019-11-07 | Novo Nordisk A/S | Gip derivatives and uses thereof |
| TW202015735A (zh) | 2018-05-30 | 2020-05-01 | 法商賽諾菲公司 | 包含ｇｌｐ－１／升糖素／ｇｉｐ三重受體促效劑、連接子及透明質酸之接合物 |
| US11166910B2 (en) * | 2019-01-25 | 2021-11-09 | Nordiccan A/S | Cannabinoid chewing gum with sugar alcohols |
| EP4112637A4 (en) * | 2020-02-24 | 2024-04-03 | Shenzhen Turier Biotech Co., Ltd. | POLYPEPTIDE COMPOUND AND ITS USE FOR PREVENTING OR TREATMENT OF DIABETES OR DIABETES COMPLICATIONS |
| CN113493503B (zh) * | 2020-04-08 | 2022-08-05 | 浙江道尔生物科技有限公司 | 一种肠促胰岛素类似物及其制备方法和用途 |
| MX2023000303A (es) | 2020-07-22 | 2023-02-09 | Novo Nordisk As | Coagonistas de los receptores del peptido 1 similar al glucagon (glp-1) y del polipeptido insulinotropico dependiente de glucosa (gip) adecuados para el suministro oral. |
| EP4249505A1 (en) | 2020-12-23 | 2023-09-27 | Zhejiang Doer Biologics Co., Ltd. | Long-acting glucagon derivative |
| EP4289860A1 (en) * | 2021-01-22 | 2023-12-13 | Shenzhen Turier Biotech Co., Ltd. | Use of polypeptide compound in prevention or treatment of inflammatory bowel disease and intestinal fibrosis related thereto |
| 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 |
| CN115490760B (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 |
| JP7402574B1 (ja) | 2023-03-15 | 2023-12-21 | 株式会社合同資源 | α－ヨード置換カルボン酸 |
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| 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 |
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| ATE458534T1 (de) | 2002-10-04 | 2010-03-15 | Microchips Inc | Medizinische vorrichtung zur gesteuerten arzneimittelverabreichung sowie herzüberwachung und/oder herzstimulation |
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| FR2902092B1 (fr) | 2006-06-07 | 2008-09-05 | Sapelem Soc Par Actions Simpli | Appareil de manutention de charge |
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| BRPI0810140A2 (pt) | 2007-04-19 | 2014-10-29 | Dong A Pharm Co Ltd | Composição de microempresa biodegradável adequada para a liberação controlada de um peptídeo de controle de glicose e formulação da mesma |
| EP2185701A4 (en) | 2007-08-15 | 2011-03-02 | Amunix Operating Inc | COMPOSITIONS AND METHODS FOR ENHANCING THE PRODUCTION OF RECOMBINANT POLYPEPTIDES |
| EP2676673B1 (en) * | 2008-06-17 | 2016-11-16 | Indiana University Research and Technology Corporation | Glucagon/glp-1 receptor co-agonists |
| WO2010011439A2 (en) | 2008-06-17 | 2010-01-28 | Indiana University Research And Technology Corporation | Gip-based mixed agonists for treatment of metabolic disorders and obesity |
| PE20120332A1 (es) | 2008-12-19 | 2012-04-14 | Univ Indiana Res & Tech Corp | Profarmacos de peptido de la superfamilia de glucagon basado en amida |
| PE20120914A1 (es) * | 2009-06-16 | 2012-08-22 | Univ Indiana Res & Tech Corp | Compuestos glucagon activo de receptor de gip |
| IN2012DN06437A (es) | 2010-01-27 | 2015-10-09 | Univ Indiana Res & Tech Corp | |
| KR20130062931A (ko) * | 2010-05-13 | 2013-06-13 | 인디애나 유니버시티 리서치 앤드 테크놀로지 코퍼레이션 | 핵 호르몬 수용체 활성을 나타내는 글루카곤 슈퍼패밀리 펩티드 |
| EP2588126A4 (en) * | 2010-06-24 | 2015-07-08 | Univ Indiana Res & Tech Corp | GLUCAGON SUPERFAMILY AMIDE PEPTIDE PRODRUGS |
| CA2839867A1 (en) * | 2011-06-22 | 2012-12-27 | Indiana University Research And Technology Corporation | Glucagon/glp-1 receptor co-agonists |
| US9156902B2 (en) * | 2011-06-22 | 2015-10-13 | Indiana University Research And Technology Corporation | Glucagon/GLP-1 receptor co-agonists |
| TR201808818T4 (tr) * | 2012-06-21 | 2018-07-23 | Novo Nordisk As | Gip reseptör aktivitesi sergileyen glukagon analogları. |
| JP6657230B2 (ja) * | 2014-09-24 | 2020-03-04 | 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 | インクレチン−インスリンコンジュゲート |
-
2013
- 2013-06-18 TR TR2018/08818T patent/TR201808818T4/tr unknown
- 2013-06-18 EP EP13731246.8A patent/EP2864350B1/en not_active Not-in-force
- 2013-06-18 SI SI201331079T patent/SI2864350T1/en unknown
- 2013-06-18 PT PT137312468T patent/PT2864350T/pt unknown
- 2013-06-18 TW TW102121585A patent/TWI644920B/zh not_active IP Right Cessation
- 2013-06-18 EA EA201590065A patent/EA029025B1/ru not_active IP Right Cessation
- 2013-06-18 MX MX2014015556A patent/MX356000B/es active IP Right Grant
- 2013-06-18 HU HUE13731246A patent/HUE039267T2/hu unknown
- 2013-06-18 AU AU2013277372A patent/AU2013277372B2/en not_active Ceased
- 2013-06-18 PL PL13731246T patent/PL2864350T3/pl unknown
- 2013-06-18 BR BR112014031671A patent/BR112014031671A2/pt not_active Application Discontinuation
- 2013-06-18 MY MYPI2014003510A patent/MY185217A/en unknown
- 2013-06-18 JP JP2015518506A patent/JP6300239B2/ja not_active Expired - Fee Related
- 2013-06-18 WO PCT/US2013/046229 patent/WO2013192130A1/en active Application Filing
- 2013-06-18 AR ARP130102143 patent/AR091478A1/es unknown
- 2013-06-18 PE PE2014002465A patent/PE20150863A1/es not_active Application Discontinuation
- 2013-06-18 ES ES13731246.8T patent/ES2674946T3/es active Active
- 2013-06-18 DK DK13731246.8T patent/DK2864350T3/en active
- 2013-06-18 CN CN201380043984.5A patent/CN104583233B/zh not_active Expired - Fee Related
- 2013-06-18 SG SG11201408491SA patent/SG11201408491SA/en unknown
- 2013-06-18 RS RS20180728A patent/RS57347B1/sr unknown
- 2013-06-18 CA CA2877127A patent/CA2877127A1/en not_active Abandoned
- 2013-06-18 US US14/408,813 patent/US9868772B2/en not_active Expired - Fee Related
- 2013-06-18 KR KR20157001447A patent/KR20150039748A/ko active IP Right Grant
-
2014
- 2014-12-17 CL CL2014003421A patent/CL2014003421A1/es unknown
- 2014-12-21 IL IL236386A patent/IL236386B/en active IP Right Grant
- 2014-12-22 PH PH12014502857A patent/PH12014502857A1/en unknown
-
2015
- 2015-01-19 CO CO15009514A patent/CO7170125A2/es unknown
- 2015-01-19 CR CR20150015A patent/CR20150015A/es not_active Application Discontinuation
-
2017
- 2017-12-04 US US15/830,158 patent/US20180105569A1/en not_active Abandoned
-
2018
- 2018-06-15 HR HRP20180936TT patent/HRP20180936T1/hr unknown
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