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
- MASNOZXLGMXCHN-ZLPAWPGGSA-N glucagon Chemical class C([C@@H](C(=O)N[C@H](C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CC=1C2=CC=CC=C2NC=1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCSC)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H]([C@@H](C)O)C(O)=O)C(C)C)NC(=O)[C@H](CC(O)=O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](C)NC(=O)[C@H](CCCNC(N)=N)NC(=O)[C@H](CCCNC(N)=N)NC(=O)[C@H](CO)NC(=O)[C@H](CC(O)=O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CC=1C=CC(O)=CC=1)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CO)NC(=O)[C@H](CC=1C=CC(O)=CC=1)NC(=O)[C@H](CC(O)=O)NC(=O)[C@H](CO)NC(=O)[C@@H](NC(=O)[C@H](CC=1C=CC=CC=1)NC(=O)[C@@H](NC(=O)CNC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CO)NC(=O)[C@@H](N)CC=1NC=NC=1)[C@@H](C)O)[C@@H](C)O)C1=CC=CC=C1 MASNOZXLGMXCHN-ZLPAWPGGSA-N 0.000 title abstract 8
- 108010004460 Gastric Inhibitory Polypeptide Proteins 0.000 title 2
- 230000000694 effects Effects 0.000 title 1
- 230000001747 exhibiting effect Effects 0.000 title 1
- 150000001413 amino acids Chemical group 0.000 abstract 10
- 102000005962 receptors Human genes 0.000 abstract 3
- 108020003175 receptors Proteins 0.000 abstract 3
- COLNVLDHVKWLRT-QMMMGPOBSA-N L-phenylalanine Chemical compound OC(=O)[C@@H](N)CC1=CC=CC=C1 COLNVLDHVKWLRT-QMMMGPOBSA-N 0.000 abstract 2
- OUYCCCASQSFEME-QMMMGPOBSA-N L-tyrosine Chemical compound OC(=O)[C@@H](N)CC1=CC=C(O)C=C1 OUYCCCASQSFEME-QMMMGPOBSA-N 0.000 abstract 2
- OKTJSMMVPCPJKN-UHFFFAOYSA-N Carbon Chemical compound [C] OKTJSMMVPCPJKN-UHFFFAOYSA-N 0.000 abstract 1
- 102000051325 Glucagon Human genes 0.000 abstract 1
- 108060003199 Glucagon Proteins 0.000 abstract 1
- 101001015516 Homo sapiens Glucagon-like peptide 1 receptor Proteins 0.000 abstract 1
- 101000950847 Homo sapiens Macrophage migration inhibitory factor Proteins 0.000 abstract 1
- 101000985642 Homo sapiens Metallothionein-3 Proteins 0.000 abstract 1
- HNDVDQJCIGZPNO-YFKPBYRVSA-N L-histidine Chemical compound OC(=O)[C@@H](N)CC1=CN=CN1 HNDVDQJCIGZPNO-YFKPBYRVSA-N 0.000 abstract 1
- 208000008589 Obesity Diseases 0.000 abstract 1
- 125000000218 acetic acid group Chemical group C(C)(=O)* 0.000 abstract 1
- 125000002252 acyl group Chemical group 0.000 abstract 1
- 125000000217 alkyl group Chemical group 0.000 abstract 1
- 229910052799 carbon Inorganic materials 0.000 abstract 1
- 206010012601 diabetes mellitus Diseases 0.000 abstract 1
- 229960004666 glucagon Drugs 0.000 abstract 1
- 238000012986 modification Methods 0.000 abstract 1
- 230000004048 modification Effects 0.000 abstract 1
- 235000020824 obesity Nutrition 0.000 abstract 1
- 125000006850 spacer group Chemical group 0.000 abstract 1
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) |
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| CN104583218B (zh) | 2012-04-26 | 2018-04-24 | 百时美施贵宝公司 | 作为蛋白酶活化受体4(par4)抑制剂用于治疗血小板聚集的咪唑并噻二唑和咪唑并吡嗪的衍生物 |
| SI2864350T1 (en) * | 2012-06-21 | 2018-08-31 | Indiana University Research And Technology Corporation | GLUCAGON ANALOGUE ANALOGUE WITH ACTIVITY OF GIP RECEPTOR |
| UA116217C2 (uk) | 2012-10-09 | 2018-02-26 | Санофі | Пептидна сполука як подвійний агоніст рецепторів glp1-1 та глюкагону |
| SI2934568T1 (en) | 2012-12-21 | 2018-03-30 | Sanofi | Dual GLP1 / GIP or trigonal agonists GLP1 / GIP / glucagon |
| UA118558C2 (uk) | 2013-05-28 | 2019-02-11 | Такеда Фармасьютікал Компані Лімітед | Пептидна сполука |
| 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 |
| 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 |
| TW201609795A (zh) | 2013-12-13 | 2016-03-16 | 賽諾菲公司 | 作為雙重ｇｌｐ－１／ｇｉｐ受體促效劑的艾塞那肽－４（ｅｘｅｎｄｉｎ－４）胜肽類似物 |
| WO2015086729A1 (en) | 2013-12-13 | 2015-06-18 | Sanofi | Dual glp-1/gip receptor agonists |
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| CN102105159B (zh) | 2008-06-17 | 2015-07-08 | 印第安纳大学研究及科技有限公司 | 基于gip的混合激动剂用于治疗代谢紊乱和肥胖症 |
| TWI474832B (zh) * | 2008-06-17 | 2015-03-01 | Univ Indiana Res & Tech Corp | 胰高血糖素／ｇｌｐ-１受體共同激動劑 |
| PE20120332A1 (es) | 2008-12-19 | 2012-04-14 | Univ Indiana Res & Tech Corp | Profarmacos de peptido de la superfamilia de glucagon basado en amida |
| RU2012101274A (ru) | 2009-06-16 | 2013-07-27 | Индиана Юниверсити Рисерч Энд Текнолоджи Корпорейшн | Соединения глюкагона, активные в отношении рецептора gip |
| MX2012008603A (es) | 2010-01-27 | 2013-01-25 | Univ Indiana Res & Tech Corp | Conjugados de antagonista de glucagon-agonista de gip y composiciones para el tratamiento de desordenes metabolicos y obesidad. |
| 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 |
| MX2012014576A (es) * | 2010-06-24 | 2013-02-21 | Univ Indiana Res & Tech Corp | Profarmacos de peptido de la superfamilia de glucagon basado en amida. |
| KR20140043793A (ko) * | 2011-06-22 | 2014-04-10 | 인디애나 유니버시티 리서치 앤드 테크놀로지 코퍼레이션 | 글루카곤/glp-1 수용체 공동-작용물질 |
| SI2723367T1 (sl) * | 2011-06-22 | 2017-08-31 | Indiana University Research And Technology Corporation | Koagonisti receptorja glukanona/GLP-1 |
| SI2864350T1 (en) * | 2012-06-21 | 2018-08-31 | Indiana University Research And Technology Corporation | GLUCAGON ANALOGUE ANALOGUE WITH ACTIVITY OF GIP RECEPTOR |
| 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 |
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- 2013-06-18 KR KR20157001447A patent/KR20150039748A/ko not_active Abandoned
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