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 (8) | US9278123B2 (enExample) |
| EP (3) | EP3326620B1 (enExample) |
| JP (2) | JP5902194B2 (enExample) |
| KR (1) | KR101925620B1 (enExample) |
| CN (2) | CN103260608A (enExample) |
| AU (1) | AU2011343190B2 (enExample) |
| BR (1) | BR112013014942B1 (enExample) |
| CA (1) | CA2821886A1 (enExample) |
| DK (2) | DK3326620T3 (enExample) |
| ES (1) | ES2661676T3 (enExample) |
| HR (1) | HRP20180425T1 (enExample) |
| HU (1) | HUE036066T2 (enExample) |
| LT (1) | LT2651398T (enExample) |
| MX (2) | MX377589B (enExample) |
| PL (2) | PL3326620T3 (enExample) |
| PT (1) | PT2651398T (enExample) |
| RS (2) | RS56998B1 (enExample) |
| RU (1) | RU2600440C3 (enExample) |
| SI (2) | SI2651398T1 (enExample) |
| SM (1) | SMT201800117T1 (enExample) |
| WO (1) | WO2012080471A1 (enExample) |
Families Citing this family (95)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| 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. |
| AU2012241894B2 (en) | 2011-04-12 | 2015-12-03 | Novo Nordisk A/S | Double-acylated GLP-1 derivatives |
| KR102072202B1 (ko) * | 2012-03-22 | 2020-01-31 | 노보 노르디스크 에이/에스 | Ｇｌｐ-1 펩티드의 조성물 및 그것의 제조 |
| ES2715308T3 (es) | 2012-03-22 | 2019-06-03 | Novo Nordisk As | Composiciones que comprenden un agente de suministro y su preparación |
| HUE064694T2 (hu) | 2012-03-22 | 2024-04-28 | Novo Nordisk As | Továbbítószert tartalmazó készítmények és elõállításuk |
| WO2013189988A1 (en) * | 2012-06-20 | 2013-12-27 | Novo Nordisk A/S | Tablet formulation comprising a peptide and a delivery agent |
| HUE049152T2 (hu) | 2012-07-01 | 2020-09-28 | Novo Nordisk As | Hosszantartó hatású GLP-1 peptidek alkalmazása |
| UA116217C2 (uk) | 2012-10-09 | 2018-02-26 | Санофі | Пептидна сполука як подвійний агоніст рецепторів glp1-1 та глюкагону |
| HUE035803T2 (en) | 2012-12-21 | 2018-05-28 | Sanofi Sa | Dual GLP1 / GIP or trigonal GLP1 / GIP / glucagon agonists |
| US9457086B2 (en) | 2013-03-05 | 2016-10-04 | 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 |
| RS58039B1 (sr) | 2013-05-02 | 2019-02-28 | Novo Nordisk As | Oralno doziranje glp-1 jedinjenja |
| WO2015086728A1 (en) | 2013-12-13 | 2015-06-18 | Sanofi | Exendin-4 peptide analogues as dual glp-1/gip receptor agonists |
| EP3080154B1 (en) | 2013-12-13 | 2018-02-07 | Sanofi | Dual glp-1/gip receptor agonists |
| WO2015086730A1 (en) | 2013-12-13 | 2015-06-18 | Sanofi | Non-acylated exendin-4 peptide analogues |
| TW201609797A (zh) | 2013-12-13 | 2016-03-16 | 賽諾菲公司 | 雙重ｇｌｐ－１／升糖素受體促效劑 |
| 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 |
| 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 |
| 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 |
| 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 |
| CA2973099C (en) | 2015-01-12 | 2021-09-14 | Enteris Biopharma, Inc. | Solid oral dosage forms |
| JP7211704B2 (ja) * | 2015-01-29 | 2023-01-24 | ノヴォ ノルディスク アー／エス | Ｇｌｐ－１アゴニスト及び腸溶コーティングを含む錠剤 |
| WO2016128972A1 (en) * | 2015-02-09 | 2016-08-18 | Entera Bio Ltd. | Formulations for oral administration of active agents with controlled absorption profile |
| 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 |
| WO2017149070A1 (en) | 2016-03-03 | 2017-09-08 | Novo Nordisk A/S | Glp-1 derivatives and uses thereof |
| PL3448416T3 (pl) * | 2016-04-28 | 2022-11-07 | Novo Nordisk A/S | Semaglutyd w schorzeniach sercowo-naczyniowych |
| MX2019001850A (es) | 2016-08-17 | 2019-05-15 | Entera Bio Ltd | Formulaciones para administracion oral de principios activos. |
| JOP20190060A1 (ar) | 2016-09-26 | 2019-03-26 | Chugai Pharmaceutical Co Ltd | مشتق بيرازولو بيريدين له تأثير مساعد لمستقبل glp-1 |
| AU2018258170B2 (en) * | 2017-04-25 | 2023-06-29 | Otsuka Pharmaceutical Co., Ltd. | Lisinopril compositions with an ingestible event marker |
| AR112015A1 (es) * | 2017-06-09 | 2019-09-11 | Novo Nordisk As | Composiciones sólidas para administración oral |
| US11291629B2 (en) | 2017-06-27 | 2022-04-05 | Bioserentach Co., Ltd. | Mucoadhesive oral preparation |
| BR112020002804A2 (pt) | 2017-08-24 | 2020-07-28 | Novo Nordisk A/S | composição farmacêutica líquida, e, kit |
| CA3078652A1 (en) | 2017-10-12 | 2019-04-18 | Novo Nordisk A/S | Semaglutide in medical therapy |
| AR114353A1 (es) | 2018-02-02 | 2020-08-26 | Novo Nordisk As | Composiciones sólidas que comprenden un agonista del glp-1 y una sal del ácido n-(8-(2-hidroxibenzoil)amino)caprílico |
| 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 |
| MY206306A (en) | 2018-10-26 | 2024-12-07 | Novo Nordisk As | Stable semaglutide compositions and uses thereof |
| EP3914383B1 (en) | 2019-01-24 | 2026-07-15 | Novo Nordisk A/S | Method of dry granulation using a roller compactor |
| WO2020180534A1 (en) | 2019-03-01 | 2020-09-10 | President And Fellows Of Harvard College | Methods and compositions for protein delivery |
| WO2020208205A1 (en) | 2019-04-10 | 2020-10-15 | Genfit | Combination therapy comprising compounds of formula (i) and glp-1 receptor agonists |
| CN114222581A (zh) | 2019-08-07 | 2022-03-22 | 诺和诺德股份有限公司 | 包含egf(a)衍生物和n-(8-(2-羟基苯甲酰基)氨基)辛酸的盐的固体组合物 |
| 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 |
| JP7767264B2 (ja) * | 2019-09-02 | 2025-11-11 | ノヴォ ノルディスク アー／エス | Ｇｌｐ－１ペプチドを含む錠剤を生成するためのプロセス |
| JP7615129B2 (ja) * | 2019-09-06 | 2025-01-16 | ノヴォ ノルディスク アー／エス | 医薬組成物における使用のための顆粒の分別のための方法および機器 |
| CA3154744A1 (en) | 2019-11-06 | 2021-05-14 | Sarah FRIEDRICH | Glp-1 receptor agonists in dementia |
| 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 |
| 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 |
| AU2020418207A1 (en) | 2019-12-30 | 2022-08-25 | Gan & Lee Pharmaceuticals Co., Ltd. | Long-acting GLP-1 compound |
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