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 (cg-RX-API-DMAC7.html) |
| EP (1) | EP2217701B9 (cg-RX-API-DMAC7.html) |
| JP (1) | JP5669582B2 (cg-RX-API-DMAC7.html) |
| AR (1) | AR069110A1 (cg-RX-API-DMAC7.html) |
| AU (1) | AU2008318986B2 (cg-RX-API-DMAC7.html) |
| CA (1) | CA2707861A1 (cg-RX-API-DMAC7.html) |
| CL (1) | CL2008003222A1 (cg-RX-API-DMAC7.html) |
| ES (1) | ES2509883T3 (cg-RX-API-DMAC7.html) |
| MX (1) | MX2010004297A (cg-RX-API-DMAC7.html) |
| PE (1) | PE20091393A1 (cg-RX-API-DMAC7.html) |
| TW (1) | TW200920404A (cg-RX-API-DMAC7.html) |
| WO (1) | WO2009058662A2 (cg-RX-API-DMAC7.html) |
Families Citing this family (53)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| ES2572952T3 (es) | 2005-11-07 | 2016-06-03 | Indiana University Research And Technology Corporation | Análogos de glucagón que muestran solubilidad y estabilidad fisiológicas |
| RU2477286C2 (ru) | 2007-01-05 | 2013-03-10 | Индиана Юниверсити Рисерч Энд Текнолоджи Корпорейшн | АНАЛОГИ ГЛЮКАГОНА, ОБЛАДАЮЩИЕ ПОВЫШЕННОЙ РАСТВОРИМОСТЬЮ В БУФЕРАХ С ФИЗИОЛОГИЧЕСКИМ ЗНАЧЕНИЕМ pH |
| MX2009008241A (es) | 2007-02-15 | 2009-10-08 | Univ Indiana Res & Tech Corp | Co-agonistas de receptor de glucagon/glp-1. |
| US8980830B2 (en) | 2007-10-30 | 2015-03-17 | Indiana University Research And Technology Corporation | Peptide compounds exhibiting glucagon antagonist and GLP-1 agonist activity |
| ES2509883T3 (es) | 2007-10-30 | 2014-10-20 | Indiana University Research And Technology Corporation | Antagonistas de glucagón |
| 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 |
| WO2009155257A1 (en) | 2008-06-17 | 2009-12-23 | Indiana University Research And Technology Corporation | Glucagon analogs exhibiting enhanced solubility and stability physiological ph buffers |
| AR072160A1 (es) | 2008-06-17 | 2010-08-11 | Univ Indiana Res & Tech Corp | Co-agonistas del receptor de glucagon/glp-1 |
| AU2009327418A1 (en) | 2008-12-19 | 2010-06-24 | Indiana University Research And Technology Corporation | Amide based glucagon superfamily peptide prodrugs |
| US9150632B2 (en) * | 2009-06-16 | 2015-10-06 | Indiana University Research And Technology Corporation | GIP receptor-active glucagon compounds |
| GB0917072D0 (en) * | 2009-09-29 | 2009-11-11 | Univ Ulster | Peptide analogues of glucagon for diabetes therapy |
| EP2501685A1 (en) | 2009-11-16 | 2012-09-26 | 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 |
| US8551946B2 (en) * | 2010-01-27 | 2013-10-08 | Indiana University Research And Technology Corporation | Glucagon antagonist-GIP agonist conjugates and compositions for the treatment of metabolic disorders and obesity |
| WO2011107494A1 (de) | 2010-03-03 | 2011-09-09 | Sanofi | Neue aromatische glykosidderivate, diese verbindungen enthaltende arzneimittel und deren verwendung |
| CN102933598A (zh) * | 2010-03-26 | 2013-02-13 | 诺沃—诺迪斯克有限公司 | 新型胰高血糖素类似物 |
| US9145451B2 (en) | 2010-05-13 | 2015-09-29 | Indiana University Research And Technology Corporation | Glucagon superfamily peptides exhbiting G protein coupled receptor activity |
| 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 |
| 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 |
| RU2580317C2 (ru) | 2010-06-24 | 2016-04-10 | Индиана Юниверсити Рисерч Энд Текнолоджи Корпорейшн | Пептидные пролекарства, принадлежащие к суперсемейству амид-содержащих глюкагонов |
| 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 |
| TW201221505A (en) | 2010-07-05 | 2012-06-01 | Sanofi Sa | Aryloxyalkylene-substituted hydroxyphenylhexynoic acids, process 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 |
| EP2635296B1 (en) | 2010-11-03 | 2014-12-24 | Arecor Limited | Novel composition comprising glucagon |
| PE20140186A1 (es) | 2010-12-22 | 2014-02-13 | Univ Indiana Res & Tech Corp | Analogos de glucagon que presentan actividad de receptor de gip |
| US9790262B2 (en) | 2011-04-05 | 2017-10-17 | Longevity Biotech, Inc. | Compositions comprising glucagon analogs and methods of making and using the same |
| CN103748109A (zh) | 2011-06-22 | 2014-04-23 | 印第安纳大学研究及科技有限公司 | 胰高血糖素/glp-1受体共同激动剂 |
| JP6179864B2 (ja) | 2011-06-22 | 2017-08-16 | 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 | グルカゴン／ｇｌｐ−１レセプタコ−アゴニスト |
| 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 |
| EP2780031B1 (en) | 2011-11-17 | 2018-03-07 | Indiana University Research and Technology Corporation | Glucagon superfamily peptides exhibiting glucocorticoid receptor activity |
| US9452225B2 (en) | 2012-03-01 | 2016-09-27 | Novo Nordisk A/S | GLP-1 prodrugs |
| EP2864351B1 (en) | 2012-06-21 | 2016-08-10 | Indiana University Research and Technology Corporation | Glucagon analogs exhibiting gip receptor activity |
| US9546205B2 (en) * | 2012-09-17 | 2017-01-17 | 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 |
| CA2895875A1 (en) | 2012-12-21 | 2014-06-26 | Sanofi | Exendin-4 derivatives |
| AU2014359894B2 (en) | 2013-12-06 | 2020-09-17 | Baikang (Suzhou) Co., Ltd | Bioreversable promoieties for nitrogen-containing and hydroxyl-containing drugs |
| EP3080154B1 (en) | 2013-12-13 | 2018-02-07 | Sanofi | Dual glp-1/gip 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 |
| WO2015086733A1 (en) | 2013-12-13 | 2015-06-18 | Sanofi | Dual glp-1/glucagon 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 |
| 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 |
| MA55068A (fr) | 2014-10-24 | 2022-01-05 | Merck Sharp & Dohme | Co-agonistes des récepteurs du glucagon et du glp-1 |
| 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 |
| KR20200107951A (ko) * | 2017-12-07 | 2020-09-16 | 아도시아 | 인간 글루카곤 및 코-폴리아미노산을 포함하는 주사용 수용액 형태의 조성물 |
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| WO1998024464A1 (en) | 1996-12-03 | 1998-06-11 | Trustees Of Boston University | Specific antagonists for glucose-dependent insulinotropic polypeptide (gip) |
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-
2008
- 2008-10-23 ES ES08845852.6T patent/ES2509883T3/es active Active
- 2008-10-23 WO PCT/US2008/080973 patent/WO2009058662A2/en not_active Ceased
- 2008-10-23 MX MX2010004297A patent/MX2010004297A/es active IP Right Grant
- 2008-10-23 US US12/739,342 patent/US8981047B2/en not_active Expired - Fee Related
- 2008-10-23 JP JP2010532154A patent/JP5669582B2/ja not_active Expired - Fee Related
- 2008-10-23 CA CA2707861A patent/CA2707861A1/en not_active Abandoned
- 2008-10-23 AU AU2008318986A patent/AU2008318986B2/en not_active Ceased
- 2008-10-23 EP EP08845852.6A patent/EP2217701B9/en not_active Not-in-force
- 2008-10-29 AR ARP080104739A patent/AR069110A1/es unknown
- 2008-10-29 CL CL2008003222A patent/CL2008003222A1/es unknown
- 2008-10-30 TW TW097141806A patent/TW200920404A/zh unknown
- 2008-10-30 PE PE2008001856A patent/PE20091393A1/es not_active Application Discontinuation
Also Published As
| Publication number | Publication date |
|---|---|
| US20120122783A1 (en) | 2012-05-17 |
| EP2217701B9 (en) | 2015-02-18 |
| EP2217701B1 (en) | 2014-07-02 |
| PE20091393A1 (es) | 2009-09-11 |
| AR069110A1 (es) | 2009-12-30 |
| EP2217701A4 (en) | 2011-06-15 |
| TW200920404A (en) | 2009-05-16 |
| AU2008318986A1 (en) | 2009-05-07 |
| CL2008003222A1 (es) | 2009-02-27 |
| WO2009058662A3 (en) | 2010-01-07 |
| MX2010004297A (es) | 2010-05-03 |
| AU2008318986B2 (en) | 2014-12-04 |
| EP2217701A2 (en) | 2010-08-18 |
| CA2707861A1 (en) | 2009-05-07 |
| JP5669582B2 (ja) | 2015-02-12 |
| US8981047B2 (en) | 2015-03-17 |
| HK1143994A1 (en) | 2011-01-21 |
| WO2009058662A2 (en) | 2009-05-07 |
| JP2011502155A (ja) | 2011-01-20 |
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