ES2558155T3 - Compuestos que muestran actividad antagonista de glucacón y agonista de GLP-1 - Google Patents
Compuestos que muestran actividad antagonista de glucacón y agonista de GLP-1 Download PDFInfo
- Publication number
- ES2558155T3 ES2558155T3 ES08845541.5T ES08845541T ES2558155T3 ES 2558155 T3 ES2558155 T3 ES 2558155T3 ES 08845541 T ES08845541 T ES 08845541T ES 2558155 T3 ES2558155 T3 ES 2558155T3
- Authority
- ES
- Spain
- Prior art keywords
- glucagon
- glp
- lactam
- pla6
- peptide
- 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.)
- Active
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- 239000005557 antagonist Substances 0.000 title abstract description 31
- 239000003877 glucagon like peptide 1 receptor agonist Substances 0.000 title abstract description 9
- 230000000694 effects Effects 0.000 title description 19
- 150000001875 compounds Chemical class 0.000 title description 2
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- 108060003199 Glucagon Proteins 0.000 abstract description 65
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- 125000001433 C-terminal amino-acid group Chemical group 0.000 abstract description 3
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- KDXKERNSBIXSRK-UHFFFAOYSA-N Lysine Natural products NCCCCC(N)C(O)=O KDXKERNSBIXSRK-UHFFFAOYSA-N 0.000 description 5
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- RTZKZFJDLAIYFH-UHFFFAOYSA-N Diethyl ether Chemical compound CCOCC RTZKZFJDLAIYFH-UHFFFAOYSA-N 0.000 description 4
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- 102100032882 Glucagon-like peptide 1 receptor Human genes 0.000 description 4
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- BFYLULHOYZNWPC-UHFFFAOYSA-N n-[[4,5-dimethyl-1-[(2-methylphenyl)methyl]imidazol-2-yl]methyl]-2,4-dimethoxy-n-(3-methylbutyl)benzamide Chemical compound COC1=CC(OC)=CC=C1C(=O)N(CCC(C)C)CC1=NC(C)=C(C)N1CC1=CC=CC=C1C BFYLULHOYZNWPC-UHFFFAOYSA-N 0.000 description 4
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- 125000001151 peptidyl group Chemical group 0.000 description 4
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- 125000003607 serino group Chemical group [H]N([H])[C@]([H])(C(=O)[*])C(O[H])([H])[H] 0.000 description 3
- 230000000087 stabilizing effect Effects 0.000 description 3
- LMDZBCPBFSXMTL-UHFFFAOYSA-N 1-Ethyl-3-(3-dimethylaminopropyl)carbodiimide Substances CCN=C=NCCCN(C)C LMDZBCPBFSXMTL-UHFFFAOYSA-N 0.000 description 2
- FPQQSJJWHUJYPU-UHFFFAOYSA-N 3-(dimethylamino)propyliminomethylidene-ethylazanium;chloride Chemical compound Cl.CCN=C=NCCCN(C)C FPQQSJJWHUJYPU-UHFFFAOYSA-N 0.000 description 2
- DKIDEFUBRARXTE-UHFFFAOYSA-N 3-mercaptopropanoic acid Chemical compound OC(=O)CCS DKIDEFUBRARXTE-UHFFFAOYSA-N 0.000 description 2
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- 239000004472 Lysine Chemical group 0.000 description 2
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- 238000003556 assay Methods 0.000 description 2
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- 235000014113 dietary fatty acids Nutrition 0.000 description 2
- AJDPNPAGZMZOMN-UHFFFAOYSA-N diethyl (4-oxo-1,2,3-benzotriazin-3-yl) phosphate Chemical compound C1=CC=C2C(=O)N(OP(=O)(OCC)OCC)N=NC2=C1 AJDPNPAGZMZOMN-UHFFFAOYSA-N 0.000 description 2
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- PFKFTWBEEFSNDU-UHFFFAOYSA-N 1,1'-Carbonyldiimidazole Substances C1=CN=CN1C(=O)N1C=CN=C1 PFKFTWBEEFSNDU-UHFFFAOYSA-N 0.000 description 1
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- XABCFXXGZPWJQP-UHFFFAOYSA-N 3-aminoadipic acid Chemical compound OC(=O)CC(N)CCC(O)=O XABCFXXGZPWJQP-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
- A61K38/00—Medicinal preparations containing peptides
- A61K38/16—Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof
-
- 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
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
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| 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 |
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| TW201215388A (en) | 2010-07-05 | 2012-04-16 | Sanofi Sa | (2-aryloxyacetylamino)phenylpropionic acid derivatives, processes for preparation thereof and use thereof as medicaments |
| TW201215387A (en) | 2010-07-05 | 2012-04-16 | Sanofi Aventis | Spirocyclically substituted 1,3-propane dioxide derivatives, processes for preparation thereof and use thereof as a medicament |
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-
2008
- 2008-10-27 WO PCT/US2008/081333 patent/WO2009058734A1/en not_active Ceased
- 2008-10-27 CA CA2702289A patent/CA2702289A1/en not_active Abandoned
- 2008-10-27 ES ES08845541.5T patent/ES2558155T3/es active Active
- 2008-10-27 JP JP2010532174A patent/JP5771005B2/ja not_active Expired - Fee Related
- 2008-10-27 MX MX2010004298A patent/MX2010004298A/es active IP Right Grant
- 2008-10-27 AU AU2008318876A patent/AU2008318876B2/en not_active Ceased
- 2008-10-27 US US12/740,206 patent/US8980830B2/en not_active Expired - Fee Related
- 2008-10-27 EP EP08845541.5A patent/EP2214691B1/en not_active Not-in-force
- 2008-10-30 TW TW097141893A patent/TW200920395A/zh unknown
- 2008-10-30 AR ARP080104771A patent/AR069136A1/es unknown
- 2008-10-30 CL CL2008003243A patent/CL2008003243A1/es unknown
- 2008-10-30 PA PA20088802301A patent/PA8802301A1/es unknown
- 2008-10-30 PE PE2008001855A patent/PE20090932A1/es not_active Application Discontinuation
Also Published As
| Publication number | Publication date |
|---|---|
| CA2702289A1 (en) | 2009-05-07 |
| CL2008003243A1 (es) | 2009-02-27 |
| AR069136A1 (es) | 2009-12-30 |
| WO2009058734A1 (en) | 2009-05-07 |
| EP2214691A1 (en) | 2010-08-11 |
| HK1141984A1 (en) | 2010-11-26 |
| JP5771005B2 (ja) | 2015-08-26 |
| PA8802301A1 (es) | 2009-06-23 |
| WO2009058734A4 (en) | 2009-07-23 |
| AU2008318876A1 (en) | 2009-05-07 |
| PE20090932A1 (es) | 2009-07-15 |
| US8980830B2 (en) | 2015-03-17 |
| MX2010004298A (es) | 2010-05-03 |
| JP2011502159A (ja) | 2011-01-20 |
| US20110098217A1 (en) | 2011-04-28 |
| AU2008318876B2 (en) | 2014-05-15 |
| EP2214691B1 (en) | 2015-09-30 |
| TW200920395A (en) | 2009-05-16 |
| EP2214691A4 (en) | 2011-01-05 |
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