JP2017514801A5 - - Google Patents
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- Publication number
- JP2017514801A5 JP2017514801A5 JP2016561311A JP2016561311A JP2017514801A5 JP 2017514801 A5 JP2017514801 A5 JP 2017514801A5 JP 2016561311 A JP2016561311 A JP 2016561311A JP 2016561311 A JP2016561311 A JP 2016561311A JP 2017514801 A5 JP2017514801 A5 JP 2017514801A5
- Authority
- JP
- Japan
- Prior art keywords
- xaa
- chem
- glu
- lys
- arg
- 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.)
- Granted
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- 125000000896 monocarboxylic acid group Chemical group 0.000 claims 6
- 150000001408 amides Chemical class 0.000 claims 5
- 150000002148 esters Chemical class 0.000 claims 5
- 150000003839 salts Chemical class 0.000 claims 5
- HNDVDQJCIGZPNO-YFKPBYRVSA-N L-histidine Chemical compound OC(=O)[C@@H](N)CC1=CN=CN1 HNDVDQJCIGZPNO-YFKPBYRVSA-N 0.000 claims 4
- 108090000765 processed proteins & peptides Proteins 0.000 claims 4
- 102100025101 GATA-type zinc finger protein 1 Human genes 0.000 claims 3
- 101710198884 GATA-type zinc finger protein 1 Proteins 0.000 claims 3
- 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 claims 3
- 101800004266 Glucagon-like peptide 1(7-37) Proteins 0.000 claims 3
- 229940024606 amino acid Drugs 0.000 claims 3
- 206010012601 diabetes mellitus Diseases 0.000 claims 3
- 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 claims 3
- WLNMZODBWIWRGN-SSDOTTSWSA-N (2R)-2-amino-2-formyl-3-(1H-imidazol-5-yl)propanoic acid Chemical compound C(=O)[C@](N)(CC1=CNC=N1)C(=O)O WLNMZODBWIWRGN-SSDOTTSWSA-N 0.000 claims 2
- OQQDUMSNEFAJOO-MRVPVSSYSA-N (2r)-2-amino-2-(1h-imidazol-5-ylmethyl)-3-oxobutanoic acid Chemical compound CC(=O)[C@@](N)(C(O)=O)CC1=CN=CN1 OQQDUMSNEFAJOO-MRVPVSSYSA-N 0.000 claims 2
- ACZFBYCNAVEFLC-YFKPBYRVSA-N (S)-3-(imidazol-5-yl)lactic acid Chemical compound OC(=O)[C@@H](O)CC1=CN=CN1 ACZFBYCNAVEFLC-YFKPBYRVSA-N 0.000 claims 2
- FVTVMQPGKVHSEY-UHFFFAOYSA-N 1-AMINOCYCLOBUTANE CARBOXYLIC ACID Chemical compound OC(=O)C1(N)CCC1 FVTVMQPGKVHSEY-UHFFFAOYSA-N 0.000 claims 2
- PAJPWUMXBYXFCZ-UHFFFAOYSA-N 1-aminocyclopropanecarboxylic acid Chemical compound OC(=O)C1(N)CC1 PAJPWUMXBYXFCZ-UHFFFAOYSA-N 0.000 claims 2
- HNDVDQJCIGZPNO-RXMQYKEDSA-N D-histidine Chemical compound OC(=O)[C@H](N)CC1=CN=CN1 HNDVDQJCIGZPNO-RXMQYKEDSA-N 0.000 claims 2
- 229930195721 D-histidine Natural products 0.000 claims 2
- 150000001413 amino acids Chemical class 0.000 claims 2
- ZCKYOWGFRHAZIQ-UHFFFAOYSA-N dihydrourocanic acid Chemical compound OC(=O)CCC1=CNC=N1 ZCKYOWGFRHAZIQ-UHFFFAOYSA-N 0.000 claims 2
- 201000010099 disease Diseases 0.000 claims 2
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims 2
- 229960002885 histidine Drugs 0.000 claims 2
- 239000013067 intermediate product Substances 0.000 claims 2
- 230000002265 prevention Effects 0.000 claims 2
- GOJUJUVQIVIZAV-UHFFFAOYSA-N 2-amino-4,6-dichloropyrimidine-5-carbaldehyde Chemical group NC1=NC(Cl)=C(C=O)C(Cl)=N1 GOJUJUVQIVIZAV-UHFFFAOYSA-N 0.000 claims 1
- 208000024172 Cardiovascular disease Diseases 0.000 claims 1
- 208000002249 Diabetes Complications Diseases 0.000 claims 1
- 206010012655 Diabetic complications Diseases 0.000 claims 1
- 208000030814 Eating disease Diseases 0.000 claims 1
- 208000019454 Feeding and Eating disease Diseases 0.000 claims 1
- -1 GLP-1 compound Chemical class 0.000 claims 1
- 208000018522 Gastrointestinal disease Diseases 0.000 claims 1
- 101800000224 Glucagon-like peptide 1 Proteins 0.000 claims 1
- 125000003178 carboxy group Chemical group [H]OC(*)=O 0.000 claims 1
- 230000003915 cell function Effects 0.000 claims 1
- 235000014632 disordered eating Nutrition 0.000 claims 1
- 239000003814 drug Substances 0.000 claims 1
- 150000002632 lipids Chemical class 0.000 claims 1
- 238000004519 manufacturing process Methods 0.000 claims 1
- 201000010065 polycystic ovary syndrome Diseases 0.000 claims 1
- 125000006239 protecting group Chemical group 0.000 claims 1
- 0 CC([C@](CCC(NCCOCCOCC(NCCOCCOCC(*)=O)=O)=O)NC(CCCCC=CCCOc1cc(C(O)=O)ccc1)=O)(O)O Chemical compound CC([C@](CCC(NCCOCCOCC(NCCOCCOCC(*)=O)=O)=O)NC(CCCCC=CCCOc1cc(C(O)=O)ccc1)=O)(O)O 0.000 description 1
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| EP14163697.7 | 2014-04-07 | ||
| EP14163697 | 2014-04-07 | ||
| PCT/EP2015/057442 WO2015155151A1 (en) | 2014-04-07 | 2015-04-07 | Double-acylated glp-1 compounds |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2017514801A JP2017514801A (ja) | 2017-06-08 |
| JP2017514801A5 true JP2017514801A5 (cg-RX-API-DMAC7.html) | 2018-05-10 |
| JP6768515B2 JP6768515B2 (ja) | 2020-10-14 |
Family
ID=50434120
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2016561311A Active JP6768515B2 (ja) | 2014-04-07 | 2015-04-07 | 二重アシル化glp−1化合物 |
Country Status (6)
| Country | Link |
|---|---|
| US (1) | US10689429B2 (cg-RX-API-DMAC7.html) |
| EP (1) | EP3129041B1 (cg-RX-API-DMAC7.html) |
| JP (1) | JP6768515B2 (cg-RX-API-DMAC7.html) |
| CN (1) | CN106132985B (cg-RX-API-DMAC7.html) |
| ES (1) | ES2741507T3 (cg-RX-API-DMAC7.html) |
| WO (1) | WO2015155151A1 (cg-RX-API-DMAC7.html) |
Families Citing this family (23)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2016168388A2 (en) | 2015-04-14 | 2016-10-20 | Palatin Technologies, Inc. | Therapies for obesity, diabetes and related indications |
| JP7053480B2 (ja) | 2016-03-03 | 2022-04-12 | ノヴォ ノルディスク アー/エス | Glp-1誘導体及びその使用 |
| AR112015A1 (es) | 2017-06-09 | 2019-09-11 | Novo Nordisk As | Composiciones sólidas para administración oral |
| EP4360651A3 (en) | 2017-08-24 | 2024-07-17 | Novo Nordisk A/S | Glp-1 compositions and uses thereof |
| RS64643B1 (sr) | 2018-02-02 | 2023-10-31 | Novo Nordisk As | Čvrste kompozicije koje sadrže glp-1 agonist i so n-(8-(2-hidroksibenzoil)amino)kaprilne kiseline i lubrikant |
| WO2019200594A1 (zh) * | 2018-04-19 | 2019-10-24 | 杭州先为达生物科技有限公司 | 酰化的glp-1衍生物 |
| 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 |
| BR112021006823A2 (pt) | 2018-10-11 | 2021-07-27 | Intarcia Therapeutics, Inc. | polipeptídeos análogos de amilina humana e métodos de uso |
| CN111378027B (zh) * | 2018-12-29 | 2022-04-15 | 万新医药科技(苏州)有限公司 | 一种索玛鲁肽前体的制备方法 |
| BR112022002189A2 (pt) * | 2019-09-02 | 2022-04-26 | Novo Nordisk As | Processo de produção de um comprimido, e, comprimido |
| WO2021089678A1 (en) | 2019-11-06 | 2021-05-14 | Novo Nordisk A/S | Glp-1 receptor agonists in dementia |
| US20220395559A1 (en) | 2019-11-07 | 2022-12-15 | Novo Nordisk A/S | Solid compositions comprising a glp-1 agonist, an sglt2 inhibitor and a salt of n-(8-(2-hydroxybenzoyl)amino)caprylic acid |
| KR20220143036A (ko) | 2020-02-18 | 2022-10-24 | 노보 노르디스크 에이/에스 | 약학적 제형 |
| 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 |
| JP2023542867A (ja) * | 2020-09-11 | 2023-10-12 | グリンプス バイオ, インコーポレイテッド | 疾患の検出/診断、病期分類、モニタリング及び処置のための生体外でのプロテアーゼ活性検出 |
| CN115925994B (zh) | 2020-09-30 | 2023-09-22 | 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 |
| CA3252113A1 (en) | 2022-03-30 | 2023-10-05 | Beijing Ql Biopharmaceutical Co., Ltd. | Liquid pharmaceutical compositions of polypeptide conjugates and their methods of use |
| WO2024110614A1 (en) | 2022-11-25 | 2024-05-30 | Novo Nordisk A/S | Oral administration of peptide therapeutics, such as glp-1 |
| WO2024165571A2 (en) | 2023-02-06 | 2024-08-15 | E-Therapeutics Plc | Inhibitors of expression and/or function |
| 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 |
| 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 (18)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| IL128332A0 (en) | 1996-08-30 | 2000-01-31 | Novo Nordisk As | GLP-1 derivatives |
| WO1999043708A1 (en) | 1998-02-27 | 1999-09-02 | Novo Nordisk A/S | Glp-1 derivatives of glp-1 and exendin with protracted profile of action |
| DE69942306D1 (de) | 1998-02-27 | 2010-06-10 | Novo Nordisk As | Abkömmlinge von glp-1 analogen |
| PL202367B1 (pl) | 1998-12-07 | 2009-06-30 | Sod Conseils Rech Applic | Związki stanowiące analogi GLP-1, kompozycje zawierające te związki oraz zastosowanie tych związków |
| JP2003516322A (ja) | 1999-11-12 | 2003-05-13 | ノボ ノルディスク アクティーゼルスカブ | ベータ細胞変性抑制のためのglp−1アゴニストの使用 |
| US6693094B2 (en) * | 2001-03-22 | 2004-02-17 | Chrono Rx Llc | Biguanide and sulfonylurea formulations for the prevention and treatment of insulin resistance and type 2 diabetes mellitus |
| US7291594B2 (en) | 2002-10-11 | 2007-11-06 | Sanwa Kagaku Kenkyusho Co., Ltd. | GLP-1 derivative and preparation thereof absorbable via mucous membrane |
| US20060286129A1 (en) | 2003-12-19 | 2006-12-21 | Emisphere Technologies, Inc. | Oral GLP-1 formulations |
| TWI362392B (en) | 2005-03-18 | 2012-04-21 | Novo Nordisk As | Acylated glp-1 compounds |
| WO2009030771A1 (en) | 2007-09-05 | 2009-03-12 | Novo Nordisk A/S | Peptides derivatized with a-b-c-d- and their therapeutical use |
| CN102686607B (zh) * | 2009-12-16 | 2014-10-29 | 诺沃—诺迪斯克有限公司 | 双酰化glp-1衍生物 |
| US9006178B2 (en) * | 2010-11-09 | 2015-04-14 | Novo Nordisk A/S | Double-acylated GLP-1 derivatives with a linker |
| EP2665470A1 (en) * | 2011-01-19 | 2013-11-27 | Novo Nordisk A/S | Glp-1 particles and compositions |
| EP3225631B1 (en) | 2011-04-12 | 2019-01-09 | Novo Nordisk A/S | Double-acylated glp-1 derivatives |
| JP6126097B2 (ja) * | 2011-09-06 | 2017-05-10 | ノヴォ ノルディスク アー/エス | Glp−1誘導体 |
| EP2846823B1 (en) | 2012-05-08 | 2019-12-04 | Novo Nordisk A/S | Double-acylated glp-1 derivatives |
| WO2013167455A1 (en) * | 2012-05-08 | 2013-11-14 | Novo Nordisk A/S | Double-acylated glp-1 derivatives |
| HK1217443A1 (zh) * | 2013-01-29 | 2017-01-13 | 奥莎迪药品管理有限公司 | 用於糖尿病的口服治疗的药物组合物 |
-
2015
- 2015-04-07 WO PCT/EP2015/057442 patent/WO2015155151A1/en not_active Ceased
- 2015-04-07 CN CN201580018073.6A patent/CN106132985B/zh active Active
- 2015-04-07 ES ES15713772T patent/ES2741507T3/es active Active
- 2015-04-07 US US15/301,960 patent/US10689429B2/en active Active
- 2015-04-07 JP JP2016561311A patent/JP6768515B2/ja active Active
- 2015-04-07 EP EP15713772.0A patent/EP3129041B1/en active Active