JP2002504518A5 - - Google Patents
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- Publication number
- JP2002504518A5 JP2002504518A5 JP2000533137A JP2000533137A JP2002504518A5 JP 2002504518 A5 JP2002504518 A5 JP 2002504518A5 JP 2000533137 A JP2000533137 A JP 2000533137A JP 2000533137 A JP2000533137 A JP 2000533137A JP 2002504518 A5 JP2002504518 A5 JP 2002504518A5
- Authority
- JP
- Japan
- Prior art keywords
- glp
- lys
- arg
- glutamyl
- hexadecanoyl
- 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.)
- Withdrawn
Links
- -1 α -hexadecanoyl Chemical group 0.000 description 38
- 101800004266 Glucagon-like peptide 1(7-37) Proteins 0.000 description 37
- GCYXWQUSHADNBF-AAEALURTSA-N preproglucagon 78-108 Chemical compound C([C@@H](C(=O)N[C@@H]([C@@H](C)CC)C(=O)N[C@@H](C)C(=O)N[C@@H](CC=1C2=CC=CC=C2NC=1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](C(C)C)C(=O)N[C@@H](CCCCN)C(=O)NCC(=O)N[C@@H](CCCNC(N)=N)C(=O)NCC(O)=O)NC(=O)[C@H](CCC(O)=O)NC(=O)[C@H](CCCCN)NC(=O)[C@H](C)NC(=O)[C@H](C)NC(=O)[C@H](CCC(N)=O)NC(=O)CNC(=O)[C@H](CCC(O)=O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CC=1C=CC(O)=CC=1)NC(=O)[C@H](CO)NC(=O)[C@H](CO)NC(=O)[C@@H](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(O)=O)NC(=O)[C@H](C)NC(=O)[C@@H](N)CC=1N=CNC=1)[C@@H](C)O)[C@@H](C)O)C(C)C)C1=CC=CC=C1 GCYXWQUSHADNBF-AAEALURTSA-N 0.000 description 34
- 125000002642 gamma-glutamyl group Chemical group 0.000 description 31
- DTHNMHAUYICORS-KTKZVXAJSA-N Glucagon-like peptide 1 Chemical compound C([C@@H](C(=O)N[C@@H]([C@@H](C)CC)C(=O)N[C@@H](C)C(=O)N[C@@H](CC=1C2=CC=CC=C2NC=1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](C(C)C)C(=O)N[C@@H](CCCCN)C(=O)NCC(=O)N[C@@H](CCCNC(N)=N)C(N)=O)NC(=O)[C@H](CCC(O)=O)NC(=O)[C@H](CCCCN)NC(=O)[C@H](C)NC(=O)[C@H](C)NC(=O)[C@H](CCC(N)=O)NC(=O)CNC(=O)[C@H](CCC(O)=O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CC=1C=CC(O)=CC=1)NC(=O)[C@H](CO)NC(=O)[C@H](CO)NC(=O)[C@@H](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(O)=O)NC(=O)[C@H](C)NC(=O)[C@@H](N)CC=1N=CNC=1)[C@@H](C)O)[C@@H](C)O)C(C)C)C1=CC=CC=C1 DTHNMHAUYICORS-KTKZVXAJSA-N 0.000 description 17
- 101800000224 Glucagon-like peptide 1 Proteins 0.000 description 9
- 102100040918 Pro-glucagon Human genes 0.000 description 9
- 239000008194 pharmaceutical composition Substances 0.000 description 9
- 125000001312 palmitoyl group Chemical group O=C([*])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])[H] 0.000 description 3
- 238000002983 circular dichroism Methods 0.000 description 2
- NGJOFQZEYQGZMB-KTKZVXAJSA-N (4S)-5-[[2-[[(2S,3R)-1-[[(2S)-1-[[(2S,3R)-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[2-[[(2S)-5-amino-1-[[(2S)-1-[[(2S)-1-[[(2S)-6-amino-1-[[(2S)-1-[[(2S)-1-[[(2S,3S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-6-amino-1-[[2-[[(1S)-4-carbamimidamido-1-carboxybutyl]amino]-2-oxoethyl]amino]-1-oxohexan-2-yl]amino]-3-methyl-1-oxobutan-2-yl]amino]-4-methyl-1-oxopentan-2-yl]amino]-3-(1H-indol-3-yl)-1-oxopropan-2-yl]amino]-1-oxopropan-2-yl]amino]-3-methyl-1-oxopentan-2-yl]amino]-1-oxo-3-phenylpropan-2-yl]amino]-4-carboxy-1-oxobutan-2-yl]amino]-1-oxohexan-2-yl]amino]-1-oxopropan-2-yl]amino]-1-oxopropan-2-yl]amino]-1,5-dioxopentan-2-yl]amino]-2-oxoethyl]amino]-4-carboxy-1-oxobutan-2-yl]amino]-4-methyl-1-oxopentan-2-yl]amino]-3-(4-hydroxyphenyl)-1-oxopropan-2-yl]amino]-3-hydroxy-1-oxopropan-2-yl]amino]-3-hydroxy-1-oxopropan-2-yl]amino]-3-methyl-1-oxobutan-2-yl]amino]-3-carboxy-1-oxopropan-2-yl]amino]-3-hydroxy-1-oxopropan-2-yl]amino]-3-hydroxy-1-oxobutan-2-yl]amino]-1-oxo-3-phenylpropan-2-yl]amino]-3-hydroxy-1-oxobutan-2-yl]amino]-2-oxoethyl]amino]-4-[[(2S)-2-[[(2S)-2-amino-3-(1H-imidazol-4-yl)propanoyl]amino]propanoyl]amino]-5-oxopentanoic acid Chemical compound C([C@@H](C(=O)N[C@@H]([C@@H](C)CC)C(=O)N[C@@H](C)C(=O)N[C@@H](CC=1C2=CC=CC=C2NC=1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](C(C)C)C(=O)N[C@@H](CCCCN)C(=O)NCC(=O)N[C@@H](CCCNC(N)=N)C(O)=O)NC(=O)[C@H](CCC(O)=O)NC(=O)[C@H](CCCCN)NC(=O)[C@H](C)NC(=O)[C@H](C)NC(=O)[C@H](CCC(N)=O)NC(=O)CNC(=O)[C@H](CCC(O)=O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CC=1C=CC(O)=CC=1)NC(=O)[C@H](CO)NC(=O)[C@H](CO)NC(=O)[C@@H](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(O)=O)NC(=O)[C@H](C)NC(=O)[C@@H](N)CC=1NC=NC=1)[C@@H](C)O)[C@@H](C)O)C(C)C)C1=CC=CC=C1 NGJOFQZEYQGZMB-KTKZVXAJSA-N 0.000 description 1
- 101800004295 Glucagon-like peptide 1(7-36) Proteins 0.000 description 1
- 125000000337 alpha-glutamyl group Chemical group 0.000 description 1
- 239000007951 isotonicity adjuster Substances 0.000 description 1
- 125000000400 lauroyl group Chemical group O=C([*])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])[H] 0.000 description 1
- 125000002801 octanoyl group Chemical group C(CCCCCCC)(=O)* 0.000 description 1
- 239000003755 preservative agent Substances 0.000 description 1
- 230000002335 preservative effect Effects 0.000 description 1
- 108090000765 processed proteins & peptides Proteins 0.000 description 1
- 239000004094 surface-active agent Substances 0.000 description 1
- XLYOFNOQVPJJNP-UHFFFAOYSA-N water Substances O XLYOFNOQVPJJNP-UHFFFAOYSA-N 0.000 description 1
Applications Claiming Priority (5)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| DK0272/98 | 1998-02-27 | ||
| DK26898 | 1998-02-27 | ||
| DK0268/98 | 1998-02-27 | ||
| DK27298 | 1998-02-27 | ||
| PCT/DK1999/000084 WO1999043341A1 (en) | 1998-02-27 | 1999-02-25 | Glp-1 derivatives with helix-content exceeding 25 %, forming partially structured micellar-like aggregates |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| JP2002504518A JP2002504518A (ja) | 2002-02-12 |
| JP2002504518A5 true JP2002504518A5 (https=) | 2009-10-22 |
Family
ID=26063652
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2000533137A Withdrawn JP2002504518A (ja) | 1998-02-27 | 1999-02-25 | 部分的に構造化されたミセルー様凝集体を形成する、25%を超えるヘリックス−含有率を有するglp−1誘導体 |
Country Status (6)
| Country | Link |
|---|---|
| EP (1) | EP1061946B1 (https=) |
| JP (1) | JP2002504518A (https=) |
| AT (1) | ATE265224T1 (https=) |
| AU (1) | AU2610799A (https=) |
| DE (1) | DE69916811T2 (https=) |
| WO (1) | WO1999043341A1 (https=) |
Families Citing this family (60)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO1998005351A1 (en) | 1996-08-08 | 1998-02-12 | Amylin Pharmaceuticals, Inc. | Methods for regulating gastrointestinal motility |
| WO2001051071A2 (en) * | 2000-01-11 | 2001-07-19 | Novo Nordisk A/S | Transepithelial delivery of glp-1 derivatives |
| JP2003525908A (ja) | 2000-03-08 | 2003-09-02 | ノボ ノルディスク アクティーゼルスカブ | 血清脂質の低下 |
| ATE424413T1 (de) | 2000-06-16 | 2009-03-15 | Lilly Co Eli | Analoge des glucagon-ähnlichen peptids-1 |
| CA2430934C (en) | 2000-12-01 | 2011-06-21 | Takeda Chemical Industries, Ltd. | A method of producing sustained-release preparations of a bioactive substance using high-pressure gas |
| BR0116024A (pt) * | 2000-12-07 | 2005-12-13 | Lilly Co Eli | Proteìna de fusão heteróloga e uso da mesma |
| AU2002316811A1 (en) | 2001-06-28 | 2003-03-03 | Novo Nordisk A/S | Stable formulation of modified glp-1 |
| CN1363654A (zh) * | 2001-07-19 | 2002-08-14 | 上海华谊生物技术有限公司 | 生产促胰岛素分泌肽glp-1(7-36)的基因工程菌以及生产glp-1(7-36)的方法 |
| CA2458371A1 (en) | 2001-08-23 | 2003-03-06 | Eli Lilly And Company | Glucagon-like peptide-1 analogs |
| BRPI0408978B8 (pt) | 2003-04-08 | 2021-07-27 | Novo Nordisk As | processos para regenerar uma fase estacionária cromatográfica |
| WO2004089985A1 (en) | 2003-04-11 | 2004-10-21 | Novo Nordisk A/S | Stable pharmaceutical compositions |
| EP1633391B1 (en) | 2003-06-03 | 2011-10-19 | Novo Nordisk A/S | Stabilized pharmaceutical peptide compositions |
| ATE541582T1 (de) | 2003-06-03 | 2012-02-15 | Novo Nordisk As | Stabilisierte pharmazeutische glp-1 peptid zusammensetzungen |
| RU2401276C2 (ru) * | 2003-09-19 | 2010-10-10 | Ново Нордиск А/С | Производные глюкагон-подобного пептида-1 (glp-1) |
| JP2007537981A (ja) * | 2003-09-19 | 2007-12-27 | ノボ ノルディスク アクティーゼルスカブ | 新規の血漿タンパク質親和性タグ |
| KR101241862B1 (ko) * | 2003-09-19 | 2013-03-13 | 노보 노르디스크 에이/에스 | 신규 glp-1 유도체 |
| TR201906789T4 (tr) | 2003-11-20 | 2019-05-21 | Novo Nordisk As | Üretim ve enjeksiyon cihazlarında kullanım için en uygun olan propilen glikol ihtiva eden peptit formülasyonları. |
| ATE498404T1 (de) | 2003-12-09 | 2011-03-15 | Novo Nordisk As | Regulierung der nahrungspräferenz mit glp-1- agonisten |
| US7521527B2 (en) | 2003-12-16 | 2009-04-21 | Societe De Conseils De Recherches Et D'applications Scientifiques, S.A.S. | GLP-1 pharmaceutical compositions |
| JP2008501765A (ja) | 2004-06-11 | 2008-01-24 | ノボ ノルディスク アクティーゼルスカブ | Glp−1アゴニストを用いた薬剤誘発性肥満の中和 |
| US8710181B2 (en) | 2004-08-31 | 2014-04-29 | Novo Nordisk A/S | Use of tris(hydroxymethyl) aminomethane for the stabilization of peptides, polypeptides and proteins |
| US8030273B2 (en) | 2004-10-07 | 2011-10-04 | Novo Nordisk A/S | Protracted exendin-4 compounds |
| US7893017B2 (en) | 2004-10-07 | 2011-02-22 | Novo Nordisk A/S | Protracted GLP-1 compounds |
| RU2413530C9 (ru) | 2004-11-12 | 2021-05-18 | Ново Нордиск А/С | Стабильные препараты инсулинотропных пептидов |
| JP5755398B2 (ja) | 2005-03-18 | 2015-07-29 | ノヴォ ノルディスク アー/エス | 伸長されたglp−1化合物 |
| TWI372629B (en) | 2005-03-18 | 2012-09-21 | Novo Nordisk As | Acylated glp-1 compounds |
| KR20110039348A (ko) | 2008-08-06 | 2011-04-15 | 노보 노르디스크 헬스 케어 악티엔게젤샤프트 | 연장된 생체내 효능을 가지는 콘쥬게이트된 단백질 |
| JP5816097B2 (ja) | 2009-01-22 | 2015-11-18 | ノヴォ・ノルディスク・ヘルス・ケア・アーゲー | 安定な成長ホルモン化合物 |
| JP6086528B2 (ja) | 2009-08-06 | 2017-03-01 | ノヴォ・ノルディスク・ヘルス・ケア・アーゲー | 長期のインビボ有効性を有する成長ホルモン |
| JP5980689B2 (ja) | 2010-01-22 | 2016-08-31 | ノヴォ・ノルディスク・ヘルス・ケア・アーゲー | 安定な成長ホルモン化合物 |
| CN118767117A (zh) | 2010-01-22 | 2024-10-15 | 诺沃—诺迪斯克保健股份有限公司 | 体内功效延长的生长激素 |
| US9168288B2 (en) | 2010-04-09 | 2015-10-27 | Mount Sinai Hospital | Methods for treating disorders of the gastrointestinal tract using a GLP-1 agonist |
| WO2011136361A1 (ja) | 2010-04-30 | 2011-11-03 | 株式会社 三和化学研究所 | 生理活性物質等の生体内安定性向上のためのペプチド及び生体内安定性が向上した生理活性物質 |
| MX377589B (es) | 2010-12-16 | 2025-03-10 | Novo Nordisk As | Composiciones sólidas que comprenden agonista de glp-1 y sal del ácido n-(8-(2-hidroxibenzoil)amino)caprílico. |
| EP3542790B1 (en) | 2012-03-22 | 2023-09-13 | Novo Nordisk A/S | Compositions comprising a delivery agent and preparation thereof |
| CN104203266B (zh) | 2012-03-22 | 2017-12-26 | 诺和诺德股份有限公司 | Glp‑1肽组合物及其制备 |
| EP2873422A4 (en) | 2012-07-10 | 2015-12-30 | Takeda Pharmaceutical | PHARMACEUTICAL PREPARATION FOR INJECTION |
| US20150273069A1 (en) | 2012-10-17 | 2015-10-01 | Novo Nordisk A/S | Fatty acid acylated amino acids for oral peptide delivery |
| US11045523B2 (en) | 2013-04-05 | 2021-06-29 | Novo Nordisk Healthcare Ag | Formulation of growth hormone albumin-binder conjugate |
| DK3006045T3 (en) | 2014-10-07 | 2017-07-17 | Cyprumed Gmbh | Pharmaceutical formulations for oral administration of peptide or protein drugs |
| EP3359181A1 (en) | 2015-10-07 | 2018-08-15 | Cyprumed GmbH | Pharmaceutical formulations for the oral delivery of peptide drugs |
| WO2018065634A1 (en) | 2016-10-07 | 2018-04-12 | Cyprumed Gmbh | Pharmaceutical compositions for the nasal delivery of peptide or protein drugs |
| HRP20240485T1 (hr) | 2017-08-24 | 2024-07-05 | Novo Nordisk A/S | Pripravci glp-1 i njihova upotreba |
| PL3746111T3 (pl) | 2018-02-02 | 2024-01-15 | Novo Nordisk A/S | Stałe kompozycje zawierające agonistę glp-1 i sól kwasu n-(8-(2- hydroksybenzoilo)amino kaprylowego i substancję poślizgową |
| EP3773475A1 (en) | 2018-04-06 | 2021-02-17 | Cyprumed GmbH | Pharmaceutical compositions for the transmucosal delivery of therapeutic peptides and proteins |
| TWI829687B (zh) | 2018-05-07 | 2024-01-21 | 丹麥商諾佛 儂迪克股份有限公司 | 包含glp-1促效劑與n-(8-(2-羥基苯甲醯基)胺基)辛酸之鹽的固體組成物 |
| KR20210109552A (ko) | 2018-12-21 | 2021-09-06 | 지앙수 헨그루이 메디슨 컴퍼니 리미티드 | 이중특이적 단백질 |
| PE20230819A1 (es) | 2020-02-18 | 2023-05-19 | Novo Nordisk As | Composiciones y usos de glp-1 |
| EP4142695B1 (en) | 2020-04-29 | 2025-11-05 | Novo Nordisk A/S | Solid compositions comprising a glp-1 agonist and histidine |
| WO2022049310A1 (en) | 2020-09-07 | 2022-03-10 | Cyprumed Gmbh | Improved pharmaceutical formulations of glp-1 receptor agonists |
| CN114729060B (zh) | 2020-09-30 | 2022-11-25 | 北京质肽生物医药科技有限公司 | 多肽缀合物和使用方法 |
| WO2023012263A1 (en) | 2021-08-04 | 2023-02-09 | Novo Nordisk A/S | Solid oral peptide formulations |
| EP4323413A4 (en) | 2022-03-30 | 2025-10-15 | Beijing Ql Biopharmaceutical Co Ltd | LIQUID PHARMACEUTICAL COMPOSITIONS OF POLYPEPTIDE CONJUGATES AND METHODS OF USE THEREOF |
| JP2026502943A (ja) | 2022-12-30 | 2026-01-27 | アルギファルマ エーエス | 経口投与されるポリペプチド治療剤の全身バイオアベイラビリティを高める組成物および方法 |
| WO2024165571A2 (en) | 2023-02-06 | 2024-08-15 | E-Therapeutics Plc | Inhibitors of expression and/or function |
| CN116730902B (zh) * | 2023-08-07 | 2023-11-21 | 杭州湃肽生化科技有限公司 | 一种合成利拉鲁肽的方法 |
| WO2025125576A2 (en) | 2023-12-15 | 2025-06-19 | E-Therapeutics Plc | Inhibitors of expression and/or function |
| WO2025133348A1 (en) | 2023-12-22 | 2025-06-26 | E-Therapeutics Plc | Inhibitors of expression and/or function |
| EP4686757A1 (en) | 2024-07-31 | 2026-02-04 | e-therapeutics PLC | Inhibitors of expression and/or function |
| WO2025196502A1 (en) | 2024-03-20 | 2025-09-25 | North Carolina Agricultural & Technical State University | Choline kinase inhibitors as a therapeutic treatment for obesity |
Family Cites Families (5)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| ATE110083T1 (de) * | 1986-05-05 | 1994-09-15 | Gen Hospital Corp | Insulinotropes hormon. |
| US5614492A (en) * | 1986-05-05 | 1997-03-25 | The General Hospital Corporation | Insulinotropic hormone GLP-1 (7-36) and uses thereof |
| JPH04504246A (ja) * | 1989-03-20 | 1992-07-30 | ザ・ジェネラル・ホスピタル・コーポレーション | インシュリン刺激ホルモン |
| ATE164852T1 (de) * | 1990-01-24 | 1998-04-15 | Douglas I Buckley | Glp-1-analoga verwendbar in der diabetesbehandlung |
| IL128332A0 (en) * | 1996-08-30 | 2000-01-31 | Novo Nordisk As | GLP-1 derivatives |
-
1999
- 1999-02-25 EP EP99906077A patent/EP1061946B1/en not_active Expired - Lifetime
- 1999-02-25 DE DE69916811T patent/DE69916811T2/de not_active Expired - Lifetime
- 1999-02-25 WO PCT/DK1999/000084 patent/WO1999043341A1/en not_active Ceased
- 1999-02-25 AT AT99906077T patent/ATE265224T1/de not_active IP Right Cessation
- 1999-02-25 AU AU26107/99A patent/AU2610799A/en not_active Abandoned
- 1999-02-25 JP JP2000533137A patent/JP2002504518A/ja not_active Withdrawn
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