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- Withdrawn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 |
|---|---|---|---|
| DK0268/98 | 1998-02-27 | ||
| DK0272/98 | 1998-02-27 | ||
| DK26898 | 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 |
|---|---|---|---|---|
| ATE493998T1 (de) | 1996-08-08 | 2011-01-15 | Amylin Pharmaceuticals Inc | Pharmazeutische zusammensetzung mit einem exendin-4-peptid |
| WO2001051071A2 (en) * | 2000-01-11 | 2001-07-19 | Novo Nordisk A/S | Transepithelial delivery of glp-1 derivatives |
| ES2253353T3 (es) | 2000-03-08 | 2006-06-01 | Novo Nordisk A/S | Reduccion del colesterol serico. |
| JP4716641B2 (ja) | 2000-06-16 | 2011-07-06 | イーライ リリー アンド カンパニー | グルカゴン様ペプチド−1類似体 |
| 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 |
| IL155812A0 (en) * | 2000-12-07 | 2003-12-23 | Lilly Co Eli | Glp-1 fusion proteins |
| WO2003002136A2 (en) | 2001-06-28 | 2003-01-09 | 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 |
| AU2002322403A1 (en) | 2001-08-23 | 2003-03-10 | Eli Lilly And Company | Glucagon-like peptide-1 analogs |
| KR101198346B1 (ko) | 2003-04-08 | 2012-11-06 | 노보 노르디스크 에이/에스 | 크로마토그래피 고정상의 재생 |
| WO2004089985A1 (en) | 2003-04-11 | 2004-10-21 | Novo Nordisk A/S | Stable pharmaceutical compositions |
| PL1633391T3 (pl) | 2003-06-03 | 2012-03-30 | Novo Nordisk As | Stabilizowane farmaceutycznie kompozycje peptydowe |
| KR101308912B1 (ko) | 2003-06-03 | 2013-09-23 | 노보 노르디스크 에이/에스 | 안정화된 약학적 펩티드 조성물 |
| BR122019021416A2 (https=) * | 2003-09-19 | 2019-12-21 | ||
| EP1667724A2 (en) * | 2003-09-19 | 2006-06-14 | Novo Nordisk A/S | Albumin-binding derivatives of therapeutic peptides |
| RU2401276C2 (ru) * | 2003-09-19 | 2010-10-10 | Ново Нордиск А/С | Производные глюкагон-подобного пептида-1 (glp-1) |
| DK3300721T4 (da) | 2003-11-20 | 2025-03-03 | Novo Nordisk As | Propylenglycol-holdige peptidformuleringer hvilke er optimale til fremstilling og til anvendelse i injektionsindretninger |
| EP2298337B1 (en) | 2003-12-09 | 2017-02-22 | Novo Nordisk A/S | Regulation of food preference using GLP-1 agonists |
| EP1694278A4 (en) | 2003-12-16 | 2009-08-12 | Ipsen Pharma | GLP-1 PHARMACEUTICAL COMPOSITIONS |
| EP1758575A1 (en) | 2004-06-11 | 2007-03-07 | Novo Nordisk A/S | Counteracting drug-induced obesity using glp-1 agonists |
| PL1789434T3 (pl) | 2004-08-31 | 2014-07-31 | Novo Nordisk As | Zastosowanie tris(hydroksymetylo)aminometanu do stabilizacji peptydów, polipeptydów i białek |
| US8030273B2 (en) | 2004-10-07 | 2011-10-04 | Novo Nordisk A/S | Protracted exendin-4 compounds |
| WO2006037810A2 (en) * | 2004-10-07 | 2006-04-13 | Novo Nordisk A/S | Protracted glp-1 compounds |
| MX2007005521A (es) | 2004-11-12 | 2007-05-18 | Novo Nordisk As | Formulaciones estables de peptidos insulinotropicos. |
| US8603972B2 (en) | 2005-03-18 | 2013-12-10 | Novo Nordisk A/S | Extended GLP-1 compounds |
| TWI362392B (en) | 2005-03-18 | 2012-04-21 | Novo Nordisk As | Acylated glp-1 compounds |
| MX2011000847A (es) | 2008-08-06 | 2011-02-25 | Novo Nordisk Healthcare Ag | Proteinas conjugadas con eficacia prolongada in vivo. |
| MX2011007736A (es) | 2009-01-22 | 2011-09-06 | Novo Nordisk Healthcare Ag | Compuestos de hormona del crecimiento estables. |
| WO2011015649A1 (en) | 2009-08-06 | 2011-02-10 | Novo Nordisk Health Care Ag | Growth hormones with prolonged in-vivo efficacy |
| MX338357B (es) | 2010-01-22 | 2016-04-13 | Novo Nordisk Healthcare Ag | Compuestos estables de la hormona de crecimiento. |
| RS59459B1 (sr) | 2010-01-22 | 2019-11-29 | Novo Nordisk Healthcare Ag | Hormoni rasta sa produženom in-vivo efikasnošću |
| WO2011123943A1 (en) | 2010-04-09 | 2011-10-13 | Mount Sinai Hospital | Methods for treating disorders of the gastrointestinal tract using a glp-1 agonist |
| MX2012012383A (es) | 2010-04-30 | 2012-11-30 | Sanwa Kagaku Kenkyusho Co | Peptido para mejorar la bioestabilidad de una sustancia bioactica y sustancia bioactiva que tiene bioestabilidad mejorada. |
| SI2651398T1 (en) | 2010-12-16 | 2018-04-30 | Novo Nordisk A/S | SOLID COMPOSITIONS CONTAINING GLP-1 AGONIST AND SOL N- (8- (2-HYDROXYBENZOIL) AMINO) CAPRICULATE ACIDS |
| ES2965469T3 (es) | 2012-03-22 | 2024-04-15 | Novo Nordisk As | Composiciones que comprenden un agente de suministro y preparación de estas |
| HRP20181447T1 (hr) | 2012-03-22 | 2018-11-02 | Novo Nordisk A/S | Pripravci glp-1 peptida i njihova priprava |
| JP6224586B2 (ja) | 2012-07-10 | 2017-11-01 | 武田薬品工業株式会社 | 注射用製剤 |
| WO2014060472A1 (en) | 2012-10-17 | 2014-04-24 | 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 |
| ES2630106T3 (es) | 2014-10-07 | 2017-08-18 | Cyprumed Gmbh | Formulaciones farmacéuticas para la administración oral de fármacos peptídicos o proteicos |
| JP2018529749A (ja) | 2015-10-07 | 2018-10-11 | シプルメット・ゲーエムベーハー | ペプチド薬物を経口送達するための医薬製剤 |
| WO2018065634A1 (en) | 2016-10-07 | 2018-04-12 | Cyprumed Gmbh | Pharmaceutical compositions for the nasal delivery of peptide or protein drugs |
| KR102665710B1 (ko) | 2017-08-24 | 2024-05-14 | 노보 노르디스크 에이/에스 | Glp-1 조성물 및 그 용도 |
| JP6898518B2 (ja) | 2018-02-02 | 2021-07-07 | ノヴォ ノルディスク アー/エス | Glp−1アゴニスト、n−(8−(2−ヒドロキシベンゾイル)アミノ)カプリル酸の塩及び滑沢剤を含む固形組成物 |
| WO2019193204A1 (en) | 2018-04-06 | 2019-10-10 | 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 |
| CN115947849A (zh) | 2018-12-21 | 2023-04-11 | 江苏恒瑞医药股份有限公司 | 双特异性蛋白 |
| JP7761567B2 (ja) | 2020-02-18 | 2025-10-28 | ノヴォ ノルディスク アー/エス | 医薬製剤 |
| CN115461044B (zh) | 2020-04-29 | 2025-06-10 | 诺和诺德股份有限公司 | 包含glp-1激动剂和组氨酸的固体组合物 |
| EP4210680A1 (en) | 2020-09-07 | 2023-07-19 | 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 |
|---|---|---|---|---|
| JP2583257B2 (ja) * | 1986-05-05 | 1997-02-19 | ザ・ジェネラル・ホスピタル・コーポレーション | インシュリン向性ホルモン |
| US5614492A (en) * | 1986-05-05 | 1997-03-25 | The General Hospital Corporation | Insulinotropic hormone GLP-1 (7-36) and uses thereof |
| ATE193541T1 (de) * | 1989-03-20 | 2000-06-15 | Gen Hospital Corp | Insulinotropes hormon |
| 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 AU AU26107/99A patent/AU2610799A/en not_active Abandoned
- 1999-02-25 JP JP2000533137A patent/JP2002504518A/ja not_active Withdrawn
- 1999-02-25 AT AT99906077T patent/ATE265224T1/de not_active IP Right Cessation
- 1999-02-25 WO PCT/DK1999/000084 patent/WO1999043341A1/en not_active Ceased
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