JP2014503526A5 - - Google Patents
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- JP2014503526A5 JP2014503526A5 JP2013543814A JP2013543814A JP2014503526A5 JP 2014503526 A5 JP2014503526 A5 JP 2014503526A5 JP 2013543814 A JP2013543814 A JP 2013543814A JP 2013543814 A JP2013543814 A JP 2013543814A JP 2014503526 A5 JP2014503526 A5 JP 2014503526A5
- Authority
- JP
- Japan
- Prior art keywords
- composition according
- amino
- salt
- hydroxybenzoyl
- glp
- 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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- 239000000203 mixture Substances 0.000 claims description 34
- 125000001424 substituent group Chemical group 0.000 claims description 16
- 239000003877 glucagon like peptide 1 receptor agonist Substances 0.000 claims description 12
- 235000014113 dietary fatty acids Nutrition 0.000 claims description 7
- 229930195729 fatty acid Natural products 0.000 claims description 7
- 239000000194 fatty acid Substances 0.000 claims description 7
- -1 (2-hydroxybenzoyl) amino Chemical group 0.000 claims description 5
- 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 description 3
- 102100025101 GATA-type zinc finger protein 1 Human genes 0.000 claims description 2
- 101710198884 GATA-type zinc finger protein 1 Proteins 0.000 claims description 2
- 125000005313 fatty acid group Chemical group 0.000 claims description 2
- 150000003839 salts Chemical class 0.000 claims 12
- 150000001768 cations Chemical class 0.000 claims 3
- WWZKQHOCKIZLMA-UHFFFAOYSA-N octanoic acid Chemical compound CCCCCCCC(O)=O WWZKQHOCKIZLMA-UHFFFAOYSA-N 0.000 claims 2
- 239000008247 solid mixture Substances 0.000 claims 2
- RUVRGYVESPRHSZ-UHFFFAOYSA-N 2-[2-(2-azaniumylethoxy)ethoxy]acetate Chemical class NCCOCCOCC(O)=O RUVRGYVESPRHSZ-UHFFFAOYSA-N 0.000 claims 1
- 239000005635 Caprylic acid (CAS 124-07-2) Substances 0.000 claims 1
- 108010011459 Exenatide Proteins 0.000 claims 1
- 101800004266 Glucagon-like peptide 1(7-37) Proteins 0.000 claims 1
- DGAQECJNVWCQMB-PUAWFVPOSA-M Ilexoside XXIX Chemical compound C[C@@H]1CC[C@@]2(CC[C@@]3(C(=CC[C@H]4[C@]3(CC[C@@H]5[C@@]4(CC[C@@H](C5(C)C)OS(=O)(=O)[O-])C)C)[C@@H]2[C@]1(C)O)C)C(=O)O[C@H]6[C@@H]([C@H]([C@@H]([C@H](O6)CO)O)O)O.[Na+] DGAQECJNVWCQMB-PUAWFVPOSA-M 0.000 claims 1
- 208000008589 Obesity Diseases 0.000 claims 1
- DLSWIYLPEUIQAV-UHFFFAOYSA-N Semaglutide Chemical group 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
- 239000002253 acid Substances 0.000 claims 1
- 238000007792 addition Methods 0.000 claims 1
- 159000000007 calcium salts Chemical class 0.000 claims 1
- JUFFVKRROAPVBI-PVOYSMBESA-N chembl1210015 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(=O)N[C@H]1[C@@H]([C@@H](O)[C@H](O[C@H]2[C@@H]([C@@H](O)[C@@H](O)[C@@H](CO[C@]3(O[C@@H](C[C@H](O)[C@H](O)CO)[C@H](NC(C)=O)[C@@H](O)C3)C(O)=O)O2)O)[C@@H](CO)O1)NC(C)=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 JUFFVKRROAPVBI-PVOYSMBESA-N 0.000 claims 1
- 230000037430 deletion Effects 0.000 claims 1
- 238000012217 deletion Methods 0.000 claims 1
- 239000003814 drug Substances 0.000 claims 1
- 229960001519 exenatide Drugs 0.000 claims 1
- 108010063245 glucagon-like peptide 1 (7-36)amide Proteins 0.000 claims 1
- 238000003780 insertion Methods 0.000 claims 1
- 230000037431 insertion Effects 0.000 claims 1
- 235000020824 obesity Nutrition 0.000 claims 1
- WWZKQHOCKIZLMA-UHFFFAOYSA-M octanoate Chemical compound CCCCCCCC([O-])=O WWZKQHOCKIZLMA-UHFFFAOYSA-M 0.000 claims 1
- 229960002446 octanoic acid Drugs 0.000 claims 1
- 239000000546 pharmaceutical excipient Substances 0.000 claims 1
- XAEFZNCEHLXOMS-UHFFFAOYSA-M potassium benzoate Chemical compound [K+].[O-]C(=O)C1=CC=CC=C1 XAEFZNCEHLXOMS-UHFFFAOYSA-M 0.000 claims 1
- GCYXWQUSHADNBF-AAEALURTSA-N preproglucagon 78-108 Chemical group 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 1
- 229950011186 semaglutide Drugs 0.000 claims 1
- 108010060325 semaglutide Proteins 0.000 claims 1
- 239000011734 sodium Substances 0.000 claims 1
- 229910052708 sodium Inorganic materials 0.000 claims 1
- 159000000000 sodium salts Chemical class 0.000 claims 1
- 238000006467 substitution reaction Methods 0.000 claims 1
- 208000001072 type 2 diabetes mellitus Diseases 0.000 claims 1
- 150000004665 fatty acids Chemical class 0.000 description 1
- 108090000765 processed proteins & peptides Proteins 0.000 description 1
Applications Claiming Priority (5)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| EP10195285.1 | 2010-12-16 | ||
| EP10195285 | 2010-12-16 | ||
| US201061425087P | 2010-12-20 | 2010-12-20 | |
| US61/425,087 | 2010-12-20 | ||
| PCT/EP2011/073060 WO2012080471A1 (en) | 2010-12-16 | 2011-12-16 | Solid compositions comprising a glp-1 agonist and a salt of n-(8-(2-hydroxybenzoyl)amino)caprylic acid |
Related Child Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2016045452A Division JP2016117759A (ja) | 2010-12-16 | 2016-03-09 | Ｇｌｐ−１アゴニストとｎ−（８−（２−ヒドロキシベンゾイル）アミノ）カプリル酸の塩とを含む固形組成物 |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2014503526A JP2014503526A (ja) | 2014-02-13 |
| JP2014503526A5 true JP2014503526A5 (enExample) | 2015-02-12 |
| JP5902194B2 JP5902194B2 (ja) | 2016-04-13 |
Family
ID=43903993
Family Applications (2)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2013543814A Active JP5902194B2 (ja) | 2010-12-16 | 2011-12-16 | Ｇｌｐ−１アゴニストとｎ−（８−（２−ヒドロキシベンゾイル）アミノ）カプリル酸の塩とを含む固形組成物 |
| JP2016045452A Withdrawn JP2016117759A (ja) | 2010-12-16 | 2016-03-09 | Ｇｌｐ−１アゴニストとｎ−（８−（２−ヒドロキシベンゾイル）アミノ）カプリル酸の塩とを含む固形組成物 |
Family Applications After (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2016045452A Withdrawn JP2016117759A (ja) | 2010-12-16 | 2016-03-09 | Ｇｌｐ−１アゴニストとｎ−（８−（２−ヒドロキシベンゾイル）アミノ）カプリル酸の塩とを含む固形組成物 |
Country Status (21)
| Country | Link |
|---|---|
| US (7) | US9278123B2 (enExample) |
| EP (3) | EP3730127A1 (enExample) |
| JP (2) | JP5902194B2 (enExample) |
| KR (1) | KR101925620B1 (enExample) |
| CN (2) | CN105963685B (enExample) |
| AU (1) | AU2011343190B2 (enExample) |
| BR (1) | BR112013014942B1 (enExample) |
| CA (1) | CA2821886A1 (enExample) |
| DK (2) | DK2651398T3 (enExample) |
| ES (1) | ES2661676T3 (enExample) |
| HR (1) | HRP20180425T1 (enExample) |
| HU (1) | HUE036066T2 (enExample) |
| LT (1) | LT2651398T (enExample) |
| MX (2) | MX377589B (enExample) |
| PL (2) | PL2651398T3 (enExample) |
| PT (1) | PT2651398T (enExample) |
| RS (2) | RS60321B1 (enExample) |
| RU (1) | RU2600440C3 (enExample) |
| SI (2) | SI3326620T1 (enExample) |
| SM (1) | SMT201800117T1 (enExample) |
| WO (1) | WO2012080471A1 (enExample) |
Families Citing this family (84)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2012080471A1 (en) | 2010-12-16 | 2012-06-21 | Novo Nordisk A/S | Solid compositions comprising a glp-1 agonist and a salt of n-(8-(2-hydroxybenzoyl)amino)caprylic acid |
| HUE031405T2 (en) | 2011-04-12 | 2017-07-28 | Novo Nordisk As | Double-acylated GLP-1 derivatives |
| DK2827845T3 (en) * | 2012-03-22 | 2019-04-01 | Novo Nordisk As | COMPOSITIONS INCLUDING A PROCEDURE AND PREPARING THEREOF |
| MY171146A (en) * | 2012-03-22 | 2019-09-27 | Novo Nordisk As | Compositions of glp-1 peptides and preparation thereof |
| HRP20231613T1 (hr) | 2012-03-22 | 2024-03-15 | Novo Nordisk A/S | Pripravci koji sadrže sredstvo za unošenje i njihova priprava |
| US9993430B2 (en) | 2012-06-20 | 2018-06-12 | Novo Nordisk A/S | Tablet formulation comprising semaglutide and a delivery agent |
| SI2866825T1 (sl) | 2012-07-01 | 2020-07-31 | Novo Nordisk A/S | Uporaba dolgo delujočih peptidov GLP-1 |
| UA116217C2 (uk) | 2012-10-09 | 2018-02-26 | Санофі | Пептидна сполука як подвійний агоніст рецепторів glp1-1 та глюкагону |
| WO2014096149A1 (en) | 2012-12-21 | 2014-06-26 | Sanofi | Exendin-4 Derivatives |
| WO2014138241A1 (en) | 2013-03-05 | 2014-09-12 | Enteris Biopharma, Inc. | Pharmaceuticals for oral delivery |
| 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 |
| PT2991671T (pt) * | 2013-05-02 | 2018-11-05 | Novo Nordisk As | Dosagem oral de compostos de glp-1 |
| WO2015086729A1 (en) | 2013-12-13 | 2015-06-18 | Sanofi | Dual glp-1/gip receptor agonists |
| TW201609795A (zh) | 2013-12-13 | 2016-03-16 | 賽諾菲公司 | 作為雙重ｇｌｐ－１／ｇｉｐ受體促效劑的艾塞那肽－４（ｅｘｅｎｄｉｎ－４）胜肽類似物 |
| 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 |
| 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 |
| 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 |
| 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 |
| US9932381B2 (en) | 2014-06-18 | 2018-04-03 | Sanofi | Exendin-4 derivatives as selective glucagon receptor agonists |
| DK3006045T3 (en) * | 2014-10-07 | 2017-07-17 | Cyprumed Gmbh | Pharmaceutical formulations for oral administration of peptide or protein drugs |
| CN105777872B (zh) * | 2014-12-16 | 2019-06-07 | 深圳翰宇药业股份有限公司 | 一种萨摩鲁肽的纯化方法 |
| ES2929218T3 (es) | 2015-01-12 | 2022-11-28 | Enteris Biopharma Inc | Formas farmacéuticas orales sólidas |
| US10265384B2 (en) * | 2015-01-29 | 2019-04-23 | Novo Nordisk A/S | Tablets comprising GLP-1 agonist and enteric coating |
| HK1247838A1 (zh) * | 2015-02-09 | 2018-10-05 | Entera Bio Ltd. | 骨质疏松症的治疗 |
| WO2016168388A2 (en) | 2015-04-14 | 2016-10-20 | Palatin Technologies, Inc. | Therapies for obesity, diabetes and related indications |
| AR105319A1 (es) | 2015-06-05 | 2017-09-27 | Sanofi Sa | Profármacos que comprenden un conjugado agonista dual de glp-1 / glucagón conector ácido hialurónico |
| TW201706291A (zh) | 2015-07-10 | 2017-02-16 | 賽諾菲公司 | 作為選擇性肽雙重ｇｌｐ－１／升糖素受體促效劑之新毒蜥外泌肽（ｅｘｅｎｄｉｎ－４）衍生物 |
| EP3423481B1 (en) | 2016-03-03 | 2020-10-07 | Novo Nordisk A/S | Glp-1 derivatives and uses thereof |
| WO2017186896A1 (en) * | 2016-04-28 | 2017-11-02 | Novo Nordisk A/S | Semaglutide in cardiovascular conditions |
| SG11201901070YA (en) | 2016-08-17 | 2019-03-28 | Entera Bio Ltd | Formulations for oral administration of active agents |
| JOP20190060A1 (ar) | 2016-09-26 | 2019-03-26 | Chugai Pharmaceutical Co Ltd | مشتق بيرازولو بيريدين له تأثير مساعد لمستقبل glp-1 |
| IL270152B2 (en) * | 2017-04-25 | 2024-10-01 | Proteus Digital Health Inc | Lisinopril compositions with an ingestible event marker |
| TWI797133B (zh) * | 2017-06-09 | 2023-04-01 | 丹麥商諾佛 儂迪克股份有限公司 | 用於經口投予的固體組成物 |
| US11291629B2 (en) | 2017-06-27 | 2022-04-05 | Bioserentach Co., Ltd. | Mucoadhesive oral preparation |
| HRP20240485T1 (hr) | 2017-08-24 | 2024-07-05 | Novo Nordisk A/S | Pripravci glp-1 i njihova upotreba |
| CN120241968A (zh) | 2017-10-12 | 2025-07-04 | 诺和诺德股份有限公司 | 用于药物治疗的司美鲁肽 |
| MA53076B1 (fr) * | 2018-02-02 | 2023-11-30 | Novo Nordisk As | Compositions solides comportant un agoniste glp-1, du sel d'acide n-(8-(2-hydroxybenzoyl)amino)caprylate et un lubrifiant |
| 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 |
| CN120617159A (zh) | 2018-10-26 | 2025-09-12 | 诺和诺德股份有限公司 | 稳定的司美鲁肽组合物及其用途 |
| WO2020152304A1 (en) | 2019-01-24 | 2020-07-30 | Novo Nordisk A/S | Roller compactor and method of dry granulation using a roller compactor |
| KR20210150436A (ko) | 2019-04-10 | 2021-12-10 | 장피트 | 화학식 (i)의 화합물 및 glp-1 수용체 효현제를 포함하는 병용 요법 |
| EP4009958A1 (en) | 2019-08-07 | 2022-06-15 | Novo Nordisk A/S | Solid compositions comprising an egf(a) derivative and a salt of n-(8-(2-hydroxybenzoyl)amino)caprylic acid |
| EP4009957B1 (en) * | 2019-08-07 | 2023-10-11 | Novo Nordisk A/S | Solid composition comprising a pyy compound and a salt of n-(8-(2-hydroxybenzoyl)amino)caprylic acid |
| CN114340655A (zh) * | 2019-09-02 | 2022-04-12 | 诺和诺德股份有限公司 | 生产包含glp-1肽的片剂的方法 |
| CN114375229B (zh) | 2019-09-06 | 2024-09-06 | 诺和诺德股份有限公司 | 分级分离用于药物组合物的颗粒的方法和设备 |
| MX2022004779A (es) * | 2019-11-06 | 2022-06-14 | Novo Nordisk As | Agonistas del receptor del péptido 1 similar al glucagón (glp-1) en demencia. |
| JP2023502004A (ja) | 2019-11-07 | 2023-01-20 | ノヴォ ノルディスク アー／エス | Ｇｌｐ－１作動薬、ｓｇｌｔ２阻害剤、およびｎ－（８－（２－ヒドロキシベンゾイル）アミノ）カプリル酸の塩を含む固形組成物 |
| JP2023500031A (ja) | 2019-11-07 | 2023-01-04 | ノヴォ ノルディスク アー／エス | Ｐｃｓｋ９阻害剤およびｎ－（８－（２－ヒドロキシベンゾイル）アミノ）カプリル酸の塩を含む固形組成物 |
| JP7777085B2 (ja) * | 2020-04-29 | 2025-11-27 | ノヴォ ノルディスク アー／エス | Ｇｌｐ－１作動薬およびヒスチジンを含む固形組成物 |
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