JP2014502985A5 - - Google Patents
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- Publication number
- JP2014502985A5 JP2014502985A5 JP2013549807A JP2013549807A JP2014502985A5 JP 2014502985 A5 JP2014502985 A5 JP 2014502985A5 JP 2013549807 A JP2013549807 A JP 2013549807A JP 2013549807 A JP2013549807 A JP 2013549807A JP 2014502985 A5 JP2014502985 A5 JP 2014502985A5
- Authority
- JP
- Japan
- Prior art keywords
- ethoxy
- glp
- compound
- amino
- acetyl
- 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- Withdrawn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
- 125000001301 ethoxy group Chemical group [H]C([H])([H])C([H])([H])O* 0.000 claims 20
- -1 GLP-1 compound Chemical class 0.000 claims 14
- 239000002245 particle Substances 0.000 claims 14
- 101710198884 GATA-type zinc finger protein 1 Proteins 0.000 claims 11
- 102100025101 GATA-type zinc finger protein 1 Human genes 0.000 claims 11
- 125000002924 primary amino group Chemical group [H]N([H])* 0.000 claims 11
- 125000000218 acetic acid group Chemical group C(C)(=O)* 0.000 claims 10
- 239000007864 aqueous solution Substances 0.000 claims 8
- 229910052751 metal Inorganic materials 0.000 claims 8
- 239000002184 metal Substances 0.000 claims 8
- 150000001875 compounds Chemical class 0.000 claims 6
- 125000004063 butyryl group Chemical group O=C([*])C([H])([H])C([H])([H])C([H])([H])[H] 0.000 claims 5
- 239000008194 pharmaceutical composition Substances 0.000 claims 5
- 239000000243 solution Substances 0.000 claims 5
- 238000000034 method Methods 0.000 claims 4
- 239000000203 mixture Substances 0.000 claims 4
- 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
- 150000003839 salts Chemical group 0.000 claims 3
- 229920001661 Chitosan Polymers 0.000 claims 2
- 102000007327 Protamines Human genes 0.000 claims 2
- 108010007568 Protamines Proteins 0.000 claims 2
- 239000012062 aqueous buffer Substances 0.000 claims 2
- 239000011575 calcium Substances 0.000 claims 2
- 239000003814 drug Substances 0.000 claims 2
- 239000011777 magnesium Substances 0.000 claims 2
- 239000011572 manganese Substances 0.000 claims 2
- 229940048914 protamine Drugs 0.000 claims 2
- 239000000725 suspension Substances 0.000 claims 2
- XLYOFNOQVPJJNP-UHFFFAOYSA-N water Substances O XLYOFNOQVPJJNP-UHFFFAOYSA-N 0.000 claims 2
- OYPRJOBELJOOCE-UHFFFAOYSA-N Calcium Chemical compound [Ca] OYPRJOBELJOOCE-UHFFFAOYSA-N 0.000 claims 1
- 108010011459 Exenatide Proteins 0.000 claims 1
- HTQBXNHDCUEHJF-XWLPCZSASA-N Exenatide Chemical compound C([C@@H](C(=O)N[C@@H]([C@@H](C)CC)C(=O)N[C@@H](CCC(O)=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](CCCCN)C(=O)N[C@@H](CC(N)=O)C(=O)NCC(=O)NCC(=O)N1[C@@H](CCC1)C(=O)N[C@@H](CO)C(=O)N[C@@H](CO)C(=O)NCC(=O)N[C@@H](C)C(=O)N1[C@@H](CCC1)C(=O)N1[C@@H](CCC1)C(=O)N1[C@@H](CCC1)C(=O)N[C@@H](CO)C(N)=O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CCCNC(N)=N)NC(=O)[C@@H](NC(=O)[C@H](C)NC(=O)[C@H](CCC(O)=O)NC(=O)[C@H](CCC(O)=O)NC(=O)[C@H](CCC(O)=O)NC(=O)[C@H](CCSC)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CO)NC(=O)[C@H](CC(C)C)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)CNC(=O)[C@@H](N)CC=1NC=NC=1)[C@@H](C)O)[C@@H](C)O)C(C)C)C1=CC=CC=C1 HTQBXNHDCUEHJF-XWLPCZSASA-N 0.000 claims 1
- 108010019598 Liraglutide Proteins 0.000 claims 1
- YSDQQAXHVYUZIW-QCIJIYAXSA-N Liraglutide Chemical compound C([C@@H](C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCC(O)=O)C(=O)NCC(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](C)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCCNC(=O)CC[C@H](NC(=O)CCCCCCCCCCCCCCC)C(O)=O)C(=O)N[C@@H](CCC(O)=O)C(=O)N[C@@H](CC=1C=CC=CC=1)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](CCCNC(N)=N)C(=O)NCC(=O)N[C@@H](CCCNC(N)=N)C(=O)NCC(O)=O)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=C(O)C=C1 YSDQQAXHVYUZIW-QCIJIYAXSA-N 0.000 claims 1
- XVVOERDUTLJJHN-UHFFFAOYSA-N Lixisenatide Chemical compound C=1NC2=CC=CC=C2C=1CC(C(=O)NC(CC(C)C)C(=O)NC(CCCCN)C(=O)NC(CC(N)=O)C(=O)NCC(=O)NCC(=O)N1C(CCC1)C(=O)NC(CO)C(=O)NC(CO)C(=O)NCC(=O)NC(C)C(=O)N1C(CCC1)C(=O)N1C(CCC1)C(=O)NC(CO)C(=O)NC(CCCCN)C(=O)NC(CCCCN)C(=O)NC(CCCCN)C(=O)NC(CCCCN)C(=O)NC(CCCCN)C(=O)NC(CCCCN)C(N)=O)NC(=O)C(CCC(O)=O)NC(=O)C(C(C)CC)NC(=O)C(NC(=O)C(CC(C)C)NC(=O)C(CCCNC(N)=N)NC(=O)C(NC(=O)C(C)NC(=O)C(CCC(O)=O)NC(=O)C(CCC(O)=O)NC(=O)C(CCC(O)=O)NC(=O)C(CCSC)NC(=O)C(CCC(N)=O)NC(=O)C(CCCCN)NC(=O)C(CO)NC(=O)C(CC(C)C)NC(=O)C(CC(O)=O)NC(=O)C(CO)NC(=O)C(NC(=O)C(CC=1C=CC=CC=1)NC(=O)C(NC(=O)CNC(=O)C(CCC(O)=O)NC(=O)CNC(=O)C(N)CC=1NC=NC=1)C(C)O)C(C)O)C(C)C)CC1=CC=CC=C1 XVVOERDUTLJJHN-UHFFFAOYSA-N 0.000 claims 1
- FYYHWMGAXLPEAU-UHFFFAOYSA-N Magnesium Chemical compound [Mg] FYYHWMGAXLPEAU-UHFFFAOYSA-N 0.000 claims 1
- PWHULOQIROXLJO-UHFFFAOYSA-N Manganese Chemical compound [Mn] PWHULOQIROXLJO-UHFFFAOYSA-N 0.000 claims 1
- 108010039918 Polylysine Proteins 0.000 claims 1
- DLSWIYLPEUIQAV-UHFFFAOYSA-N Semaglutide Chemical compound CCC(C)C(NC(=O)C(Cc1ccccc1)NC(=O)C(CCC(O)=O)NC(=O)C(CCCCNC(=O)COCCOCCNC(=O)COCCOCCNC(=O)CCC(NC(=O)CCCCCCCCCCCCCCCCC(O)=O)C(O)=O)NC(=O)C(C)NC(=O)C(C)NC(=O)C(CCC(N)=O)NC(=O)CNC(=O)C(CCC(O)=O)NC(=O)C(CC(C)C)NC(=O)C(Cc1ccc(O)cc1)NC(=O)C(CO)NC(=O)C(CO)NC(=O)C(NC(=O)C(CC(O)=O)NC(=O)C(CO)NC(=O)C(NC(=O)C(Cc1ccccc1)NC(=O)C(NC(=O)CNC(=O)C(CCC(O)=O)NC(=O)C(C)(C)NC(=O)C(N)Cc1cnc[nH]1)C(C)O)C(C)O)C(C)C)C(=O)NC(C)C(=O)NC(Cc1c[nH]c2ccccc12)C(=O)NC(CC(C)C)C(=O)NC(C(C)C)C(=O)NC(CCCNC(N)=N)C(=O)NCC(=O)NC(CCCNC(N)=N)C(=O)NCC(O)=O DLSWIYLPEUIQAV-UHFFFAOYSA-N 0.000 claims 1
- 230000002378 acidificating effect Effects 0.000 claims 1
- 239000000872 buffer Substances 0.000 claims 1
- 229910052791 calcium Inorganic materials 0.000 claims 1
- 150000001767 cationic compounds Chemical class 0.000 claims 1
- NKLCHDQGUHMCGL-UHFFFAOYSA-N cyclohexylidenemethanone Chemical group O=C=C1CCCCC1 NKLCHDQGUHMCGL-UHFFFAOYSA-N 0.000 claims 1
- 229960001519 exenatide Drugs 0.000 claims 1
- 239000008240 homogeneous mixture Substances 0.000 claims 1
- 229960002701 liraglutide Drugs 0.000 claims 1
- 108010004367 lixisenatide Proteins 0.000 claims 1
- 229960001093 lixisenatide Drugs 0.000 claims 1
- 229910052749 magnesium Inorganic materials 0.000 claims 1
- 229910052748 manganese Inorganic materials 0.000 claims 1
- 208000030159 metabolic disease Diseases 0.000 claims 1
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims 1
- 229920000724 poly(L-arginine) polymer Polymers 0.000 claims 1
- 108010011110 polyarginine Proteins 0.000 claims 1
- 229920000656 polylysine Polymers 0.000 claims 1
- 108090000765 processed proteins & peptides Proteins 0.000 claims 1
- 108010060325 semaglutide Proteins 0.000 claims 1
- 229950011186 semaglutide Drugs 0.000 claims 1
- 108010048573 taspoglutide Proteins 0.000 claims 1
- WRGVLTAWMNZWGT-VQSPYGJZSA-N taspoglutide 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)NC(C)(C)C(=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(C)(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 WRGVLTAWMNZWGT-VQSPYGJZSA-N 0.000 claims 1
- 229950007151 taspoglutide Drugs 0.000 claims 1
- JBQYATWDVHIOAR-UHFFFAOYSA-N tellanylidenegermanium Chemical compound [Te]=[Ge] JBQYATWDVHIOAR-UHFFFAOYSA-N 0.000 claims 1
Applications Claiming Priority (5)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| EP11151456.8 | 2011-01-19 | ||
| EP11151456 | 2011-01-19 | ||
| US201161436804P | 2011-01-27 | 2011-01-27 | |
| US61/436,804 | 2011-01-27 | ||
| PCT/EP2012/050785 WO2012098188A1 (en) | 2011-01-19 | 2012-01-19 | Glp-1 particles and compositions |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| JP2014502985A JP2014502985A (ja) | 2014-02-06 |
| JP2014502985A5 true JP2014502985A5 (https=) | 2015-03-12 |
Family
ID=43899633
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2013549807A Withdrawn JP2014502985A (ja) | 2011-01-19 | 2012-01-19 | Ｇｌｐ−１粒子および組成物 |
Country Status (5)
| Country | Link |
|---|---|
| US (1) | US20140004198A1 (https=) |
| EP (1) | EP2665470A1 (https=) |
| JP (1) | JP2014502985A (https=) |
| CN (1) | CN103298456A (https=) |
| WO (1) | WO2012098188A1 (https=) |
Families Citing this family (11)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN104055735B (zh) * | 2013-03-22 | 2016-08-03 | 深圳翰宇药业股份有限公司 | 一种萨摩鲁泰的脂质体及其制备方法 |
| ES2741507T3 (es) * | 2014-04-07 | 2020-02-11 | Novo Nordisk As | Compuestos de glp-1 acilados doblemente |
| DK3244878T3 (da) | 2015-01-12 | 2022-10-17 | Enteris Biopharma Inc | Faste orale sammensætningsformer |
| US20180221451A1 (en) * | 2015-08-13 | 2018-08-09 | Sun Pharma Advanced Research Company Limited | Long acting liraglutide compositions |
| CN109195622A (zh) * | 2016-03-01 | 2019-01-11 | 深圳翰宇药业股份有限公司 | 一种药物组合物及其制备方法 |
| RU2018134132A (ru) * | 2016-03-31 | 2020-04-30 | Сан Фарма Эдвэнст Рисёрч Кампани Лимитэд | Вязкоупругий гель лираглутида, адаптированный для однократного недельного или однократного двухнедельного применения |
| KR102665710B1 (ko) | 2017-08-24 | 2024-05-14 | 노보 노르디스크 에이/에스 | Glp-1 조성물 및 그 용도 |
| CN115484935A (zh) | 2020-02-14 | 2022-12-16 | G2G生物公司 | 包括含有glp-1类似物或其药学上可接受的盐的缓释微球的药物组合物 |
| KR102253318B1 (ko) * | 2020-06-02 | 2021-05-18 | (주)위바이오트리 | 금속 상 변환 화합물 및 이의 제조 방법 |
| CN111888334B (zh) * | 2020-06-28 | 2022-03-18 | 苏州天微肽生物医药科技有限公司 | 一种利拉鲁肽微球缓释剂及其制备方法和应用 |
| CN115887351B (zh) * | 2023-01-03 | 2023-05-05 | 中科微针（北京）科技有限公司 | 一种glp-1受体激动剂类药物微针组合物、由其制备得到的微针及其制备方法和应用 |
Family Cites Families (10)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO1995005848A1 (en) * | 1993-08-24 | 1995-03-02 | Novo Nordisk A/S | Protracted glp-1 |
| US5705483A (en) * | 1993-12-09 | 1998-01-06 | Eli Lilly And Company | Glucagon-like insulinotropic peptides, compositions and methods |
| IL128332A0 (en) | 1996-08-30 | 2000-01-31 | Novo Nordisk As | GLP-1 derivatives |
| US6451762B1 (en) | 1997-10-24 | 2002-09-17 | Novo Nordisk A/S | Aggregates of human insulin derivatives |
| AU2002308706A1 (en) | 2001-06-01 | 2002-12-16 | Eli Lilly And Company | Glp-1 formulations with protracted time action |
| AU2002322403A1 (en) * | 2001-08-23 | 2003-03-10 | Eli Lilly And Company | Glucagon-like peptide-1 analogs |
| TWI362392B (en) | 2005-03-18 | 2012-04-21 | Novo Nordisk As | Acylated glp-1 compounds |
| US20100022457A1 (en) * | 2006-05-26 | 2010-01-28 | Bristol-Myers Squibb Company | Sustained release glp-1 receptor modulators |
| KR100805208B1 (ko) * | 2007-03-27 | 2008-02-21 | 주식회사 펩트론 | 엑센딘 함유 서방성 제제 조성물, 엑센딘 함유 서방성미립구 및 이의 제조 방법 |
| WO2008133908A2 (en) * | 2007-04-23 | 2008-11-06 | Intarcia Therapeutics, Inc. | Suspension formulations of insulinotropic peptides and uses thereof |
-
2012
- 2012-01-19 EP EP12700491.9A patent/EP2665470A1/en not_active Withdrawn
- 2012-01-19 US US13/980,166 patent/US20140004198A1/en not_active Abandoned
- 2012-01-19 JP JP2013549807A patent/JP2014502985A/ja not_active Withdrawn
- 2012-01-19 WO PCT/EP2012/050785 patent/WO2012098188A1/en not_active Ceased
- 2012-01-19 CN CN2012800058571A patent/CN103298456A/zh active Pending
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