ES2509883T3 - Antagonistas de glucagón - Google Patents
Antagonistas de glucagón Download PDFInfo
- Publication number
- ES2509883T3 ES2509883T3 ES08845852.6T ES08845852T ES2509883T3 ES 2509883 T3 ES2509883 T3 ES 2509883T3 ES 08845852 T ES08845852 T ES 08845852T ES 2509883 T3 ES2509883 T3 ES 2509883T3
- Authority
- ES
- Spain
- Prior art keywords
- glucagon
- kda peg
- seq
- pla6
- antagonism
- 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
Links
- MASNOZXLGMXCHN-ZLPAWPGGSA-N glucagon Chemical compound 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 description 50
- 108060003199 Glucagon Proteins 0.000 title abstract description 30
- 102000051325 Glucagon Human genes 0.000 title abstract description 29
- 229960004666 glucagon Drugs 0.000 title abstract description 29
- 239000005557 antagonist Substances 0.000 title abstract description 5
- 150000001413 amino acids Chemical group 0.000 abstract description 3
- NWCHELUCVWSRRS-SECBINFHSA-N (2r)-2-hydroxy-2-phenylpropanoic acid Chemical group OC(=O)[C@@](O)(C)C1=CC=CC=C1 NWCHELUCVWSRRS-SECBINFHSA-N 0.000 abstract 2
- 125000002887 hydroxy group Chemical group [H]O* 0.000 abstract 1
- 150000003839 salts Chemical class 0.000 abstract 1
- 238000006467 substitution reaction Methods 0.000 abstract 1
- 230000008485 antagonism Effects 0.000 description 10
- 108090000765 processed proteins & peptides Proteins 0.000 description 9
- 230000008878 coupling Effects 0.000 description 4
- 238000010168 coupling process Methods 0.000 description 4
- 238000005859 coupling reaction Methods 0.000 description 4
- 125000003088 (fluoren-9-ylmethoxy)carbonyl group Chemical group 0.000 description 3
- 230000008484 agonism Effects 0.000 description 3
- 102000004196 processed proteins & peptides Human genes 0.000 description 3
- NQRYJNQNLNOLGT-UHFFFAOYSA-N Piperidine Chemical compound C1CCNCC1 NQRYJNQNLNOLGT-UHFFFAOYSA-N 0.000 description 2
- 125000002252 acyl group Chemical group 0.000 description 2
- 230000006320 pegylation Effects 0.000 description 2
- 239000011347 resin Substances 0.000 description 2
- 229920005989 resin Polymers 0.000 description 2
- -1 spacer amino acid Chemical class 0.000 description 2
- JXGYPHBCPYMHSR-OYKVQYDMSA-N (2s)-2,6-diamino-7-(9h-fluoren-9-ylmethoxy)-7-oxoheptanoic acid Chemical group C1=CC=C2C(COC(=O)C(N)CCC[C@H](N)C(O)=O)C3=CC=CC=C3C2=C1 JXGYPHBCPYMHSR-OYKVQYDMSA-N 0.000 description 1
- JGFZNNIVVJXRND-UHFFFAOYSA-N N,N-Diisopropylethylamine (DIPEA) Chemical compound CCN(C(C)C)C(C)C JGFZNNIVVJXRND-UHFFFAOYSA-N 0.000 description 1
- 125000000539 amino acid group Chemical group 0.000 description 1
- 125000003178 carboxy group Chemical group [H]OC(*)=O 0.000 description 1
- 239000003153 chemical reaction reagent Substances 0.000 description 1
- 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 1
- 239000000539 dimer Substances 0.000 description 1
- 230000000694 effects Effects 0.000 description 1
- 230000008030 elimination Effects 0.000 description 1
- 238000003379 elimination reaction Methods 0.000 description 1
- 125000002485 formyl group Chemical group [H]C(*)=O 0.000 description 1
- 238000011065 in-situ storage Methods 0.000 description 1
- 230000005764 inhibitory process Effects 0.000 description 1
- 238000006386 neutralization reaction Methods 0.000 description 1
- 230000003389 potentiating effect Effects 0.000 description 1
- 125000006239 protecting group Chemical group 0.000 description 1
- 102000004169 proteins and genes Human genes 0.000 description 1
- 108090000623 proteins and genes Proteins 0.000 description 1
- 102000005962 receptors Human genes 0.000 description 1
- 108020003175 receptors Proteins 0.000 description 1
- 239000007787 solid Substances 0.000 description 1
- 125000005931 tert-butyloxycarbonyl group Chemical group [H]C([H])([H])C(OC(*)=O)(C([H])([H])[H])C([H])([H])[H] 0.000 description 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
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P3/00—Drugs for disorders of the metabolism
-
- 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
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K38/00—Medicinal preparations containing peptides
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- Organic Chemistry (AREA)
- General Health & Medical Sciences (AREA)
- Medicinal Chemistry (AREA)
- Diabetes (AREA)
- Endocrinology (AREA)
- Animal Behavior & Ethology (AREA)
- Veterinary Medicine (AREA)
- General Chemical & Material Sciences (AREA)
- Obesity (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Hematology (AREA)
- Pharmacology & Pharmacy (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Public Health (AREA)
- Toxicology (AREA)
- Genetics & Genomics (AREA)
- Proteomics, Peptides & Aminoacids (AREA)
- Zoology (AREA)
- Gastroenterology & Hepatology (AREA)
- Biochemistry (AREA)
- Biophysics (AREA)
- Molecular Biology (AREA)
- Child & Adolescent Psychology (AREA)
- Emergency Medicine (AREA)
- Peptides Or Proteins (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
- Medicinal Preparation (AREA)
- Medicines Containing Antibodies Or Antigens For Use As Internal Diagnostic Agents (AREA)
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US98378307P | 2007-10-30 | 2007-10-30 | |
| US983783P | 2007-10-30 | ||
| PCT/US2008/080973 WO2009058662A2 (en) | 2007-10-30 | 2008-10-23 | Glucagon antagonists |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| ES2509883T3 true ES2509883T3 (es) | 2014-10-20 |
Family
ID=40591715
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| ES08845852.6T Active ES2509883T3 (es) | 2007-10-30 | 2008-10-23 | Antagonistas de glucagón |
Country Status (12)
| Country | Link |
|---|---|
| US (1) | US8981047B2 (enExample) |
| EP (1) | EP2217701B9 (enExample) |
| JP (1) | JP5669582B2 (enExample) |
| AR (1) | AR069110A1 (enExample) |
| AU (1) | AU2008318986B2 (enExample) |
| CA (1) | CA2707861A1 (enExample) |
| CL (1) | CL2008003222A1 (enExample) |
| ES (1) | ES2509883T3 (enExample) |
| MX (1) | MX2010004297A (enExample) |
| PE (1) | PE20091393A1 (enExample) |
| TW (1) | TW200920404A (enExample) |
| WO (1) | WO2009058662A2 (enExample) |
Families Citing this family (53)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CA2628241C (en) | 2005-11-07 | 2016-02-02 | Indiana University Research And Technology Corporation | Glucagon analogs exhibiting physiological solubility and stability |
| EP2124974B1 (en) | 2007-01-05 | 2017-03-15 | Indiana University Research and Technology Corporation | Glucagon analogs exhibiting enhanced solubility in physiological ph buffers |
| EP2487184A1 (en) | 2007-02-15 | 2012-08-15 | Indiana University Research and Technology Corporation | Glucagon/GLP-1 receptor co-agonists |
| 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 |
| KR20110039230A (ko) | 2008-06-17 | 2011-04-15 | 인디애나 유니버시티 리서치 앤드 테크놀로지 코퍼레이션 | 생리학적 ｐＨ 완충액에서 강화된 용해도 및 안정성을 나타내는 글루카곤 유사체 |
| AU2009260302B2 (en) | 2008-06-17 | 2014-10-23 | Indiana University Research And Technology Corporation | Glucagon/GLP-1 receptor co-agonists |
| BRPI0915282A2 (pt) | 2008-06-17 | 2017-02-07 | Univ Indiana Res & Tech Corp | agonistas mistos baseados no gip para o tratamento de distúrbios metabólicos e obesidade |
| SG172291A1 (en) | 2008-12-19 | 2011-07-28 | Univ Indiana Res & Tech Corp | 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" |
| GB0917072D0 (en) * | 2009-09-29 | 2009-11-11 | Univ Ulster | Peptide analogues of glucagon for diabetes therapy |
| AU2010317842A1 (en) | 2009-11-16 | 2012-07-12 | Mellitech | [1,5]-diazocin derivatives |
| US8703701B2 (en) | 2009-12-18 | 2014-04-22 | Indiana University Research And Technology Corporation | Glucagon/GLP-1 receptor co-agonists |
| CN102834108A (zh) | 2010-01-27 | 2012-12-19 | 印第安纳大学研究及科技有限公司 | 用于治疗代谢紊乱和肥胖症的胰高血糖素拮抗剂-gip激动剂偶联物和组合物 |
| WO2011107494A1 (de) | 2010-03-03 | 2011-09-09 | Sanofi | Neue aromatische glykosidderivate, diese verbindungen enthaltende arzneimittel und deren verwendung |
| US20130053310A1 (en) * | 2010-03-26 | 2013-02-28 | Novo Nordisk A/S | Novel glucagon analogues |
| CN103179976A (zh) | 2010-05-13 | 2013-06-26 | 印第安纳大学研究及科技有限公司 | 呈现g蛋白偶联受体活性的胰高血糖素超家族肽 |
| CN103079587B (zh) | 2010-05-13 | 2016-05-11 | 印第安纳大学研究及科技有限公司 | 呈现核激素受体活性的胰高血糖素超家族肽 |
| US8530413B2 (en) | 2010-06-21 | 2013-09-10 | Sanofi | Heterocyclically substituted methoxyphenyl derivatives with an oxo group, processes for preparation thereof and use thereof as medicaments |
| CN103179979A (zh) | 2010-06-24 | 2013-06-26 | 印第安纳大学研究及科技有限公司 | 基于酰胺的胰高血糖素超家族肽前药 |
| TW201221505A (en) | 2010-07-05 | 2012-06-01 | Sanofi Sa | Aryloxyalkylene-substituted hydroxyphenylhexynoic acids, process for preparation thereof and use thereof as a medicament |
| 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 |
| TW201215388A (en) | 2010-07-05 | 2012-04-16 | Sanofi Sa | (2-aryloxyacetylamino)phenylpropionic acid derivatives, processes for preparation thereof and use thereof as medicaments |
| KR101382593B1 (ko) | 2010-07-21 | 2014-04-10 | 한미사이언스 주식회사 | 신규한 지속형 글루카곤 결합체 및 이를 포함하는 비만 예방 및 치료용 약학적 조성물 |
| WO2012059762A1 (en) | 2010-11-03 | 2012-05-10 | Arecor Limited | Novel composition comprising glucagon |
| EA201390941A1 (ru) | 2010-12-22 | 2013-12-30 | Индиана Юниверсити Рисерч Энд Текнолоджи Корпорейшн | Аналоги глюкагона, проявляющие активность на рецепторе gip |
| EP2694095B1 (en) | 2011-04-05 | 2018-03-07 | Longevity Biotech, Inc. | Compositions comprising glucagon analogs and methods of making and using the same |
| CN103857408B (zh) | 2011-06-22 | 2017-04-12 | 印第安那大学科技研究公司 | 胰高血糖素/glp‑1受体协同激动剂 |
| BR112013032717A2 (pt) | 2011-06-22 | 2017-01-24 | Univ Indiana Res & Tech Corp | coagonistas do receptor de glucagon/glp-1 |
| WO2013037390A1 (en) | 2011-09-12 | 2013-03-21 | Sanofi | 6-(4-hydroxy-phenyl)-3-styryl-1h-pyrazolo[3,4-b]pyridine-4-carboxylic acid amide derivatives as kinase inhibitors |
| WO2013045413A1 (en) | 2011-09-27 | 2013-04-04 | Sanofi | 6-(4-hydroxy-phenyl)-3-alkyl-1h-pyrazolo[3,4-b]pyridine-4-carboxylic acid amide derivatives as kinase inhibitors |
| ES2672880T3 (es) | 2011-11-17 | 2018-06-18 | Indiana University Research And Technology Corporation | Péptidos de la superfamilia de glucagón que muestran actividad de receptor de glucocorticoides |
| CN104185639B (zh) | 2012-03-01 | 2018-06-19 | 诺和诺德股份有限公司 | Glp-1前体药物 |
| WO2013192129A1 (en) | 2012-06-21 | 2013-12-27 | Indiana University Research And Technology Corporation | Glucagon analogs exhibiting gip receptor activity |
| EP2895506A1 (en) * | 2012-09-17 | 2015-07-22 | Imperial Innovations Limited | Peptide analogues of glucagon and glp1 |
| UA116217C2 (uk) | 2012-10-09 | 2018-02-26 | Санофі | Пептидна сполука як подвійний агоніст рецепторів glp1-1 та глюкагону |
| MX2015008077A (es) | 2012-12-21 | 2015-10-30 | Sanofi Sa | Derivados de exendina-4 como agonistas dobles de glp1/gip o trigonal de glp1-gip/glucagon. |
| EP3077008B1 (en) | 2013-12-06 | 2023-10-04 | Jie Han | Bioreversable promoieties for nitrogen-containing and hydroxyl-containing drugs |
| WO2015086729A1 (en) | 2013-12-13 | 2015-06-18 | Sanofi | Dual glp-1/gip receptor agonists |
| WO2015086733A1 (en) | 2013-12-13 | 2015-06-18 | Sanofi | Dual glp-1/glucagon receptor agonists |
| EP3080152A1 (en) | 2013-12-13 | 2016-10-19 | Sanofi | Non-acylated exendin-4 peptide analogues |
| EP3080150B1 (en) | 2013-12-13 | 2018-08-01 | Sanofi | Exendin-4 peptide analogues as dual glp-1/gip receptor agonists |
| JP2017509603A (ja) | 2014-02-18 | 2017-04-06 | ノヴォ ノルディスク アー／エス | 安定なグルカゴン類似体及び低血糖症の処置のための使用 |
| 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 |
| 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 |
| 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 |
| AR105319A1 (es) | 2015-06-05 | 2017-09-27 | Sanofi Sa | Profármacos que comprenden un conjugado agonista dual de glp-1 / glucagón conector ácido hialurónico |
| 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 |
| GB201611077D0 (en) | 2016-06-24 | 2016-08-10 | Arecor Ltd | Novel composition |
| TW201832783A (zh) | 2016-12-02 | 2018-09-16 | 法商賽諾菲公司 | 包含ｇｌｐ－１／胰高血糖素雙重激動劑、連接子和透明質酸的接合物 |
| JP2021505597A (ja) * | 2017-12-07 | 2021-02-18 | アドシア | ヒトグルカゴンおよびコポリアミノ酸を含む注射水溶液の形態の組成物 |
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-
2008
- 2008-10-23 WO PCT/US2008/080973 patent/WO2009058662A2/en not_active Ceased
- 2008-10-23 CA CA2707861A patent/CA2707861A1/en not_active Abandoned
- 2008-10-23 ES ES08845852.6T patent/ES2509883T3/es active Active
- 2008-10-23 MX MX2010004297A patent/MX2010004297A/es active IP Right Grant
- 2008-10-23 JP JP2010532154A patent/JP5669582B2/ja not_active Expired - Fee Related
- 2008-10-23 EP EP08845852.6A patent/EP2217701B9/en not_active Not-in-force
- 2008-10-23 US US12/739,342 patent/US8981047B2/en not_active Expired - Fee Related
- 2008-10-23 AU AU2008318986A patent/AU2008318986B2/en not_active Ceased
- 2008-10-29 CL CL2008003222A patent/CL2008003222A1/es unknown
- 2008-10-29 AR ARP080104739A patent/AR069110A1/es unknown
- 2008-10-30 PE PE2008001856A patent/PE20091393A1/es not_active Application Discontinuation
- 2008-10-30 TW TW097141806A patent/TW200920404A/zh unknown
Also Published As
| Publication number | Publication date |
|---|---|
| HK1143994A1 (en) | 2011-01-21 |
| AU2008318986B2 (en) | 2014-12-04 |
| CL2008003222A1 (es) | 2009-02-27 |
| WO2009058662A3 (en) | 2010-01-07 |
| WO2009058662A2 (en) | 2009-05-07 |
| EP2217701B1 (en) | 2014-07-02 |
| EP2217701A2 (en) | 2010-08-18 |
| JP2011502155A (ja) | 2011-01-20 |
| TW200920404A (en) | 2009-05-16 |
| AR069110A1 (es) | 2009-12-30 |
| MX2010004297A (es) | 2010-05-03 |
| AU2008318986A1 (en) | 2009-05-07 |
| EP2217701A4 (en) | 2011-06-15 |
| PE20091393A1 (es) | 2009-09-11 |
| US20120122783A1 (en) | 2012-05-17 |
| EP2217701B9 (en) | 2015-02-18 |
| JP5669582B2 (ja) | 2015-02-12 |
| US8981047B2 (en) | 2015-03-17 |
| CA2707861A1 (en) | 2009-05-07 |
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