JP2015510947A5 - - Google Patents
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- Publication number
- JP2015510947A5 JP2015510947A5 JP2015501876A JP2015501876A JP2015510947A5 JP 2015510947 A5 JP2015510947 A5 JP 2015510947A5 JP 2015501876 A JP2015501876 A JP 2015501876A JP 2015501876 A JP2015501876 A JP 2015501876A JP 2015510947 A5 JP2015510947 A5 JP 2015510947A5
- Authority
- JP
- Japan
- Prior art keywords
- solid composition
- composition according
- medicament
- phenyl
- manufacture
- 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.)
- Ceased
Links
- 239000008247 solid mixture Substances 0.000 claims 25
- -1 4′-cyano-biphenyl-4-yl Chemical group 0.000 claims 11
- 150000001875 compounds Chemical class 0.000 claims 10
- 239000003814 drug Substances 0.000 claims 10
- 238000004519 manufacturing process Methods 0.000 claims 10
- XBDQKXXYIPTUBI-UHFFFAOYSA-N Propionic acid Substances CCC(O)=O XBDQKXXYIPTUBI-UHFFFAOYSA-N 0.000 claims 5
- CDBYLPFSWZWCQE-UHFFFAOYSA-L Sodium Carbonate Chemical compound [Na+].[Na+].[O-]C([O-])=O CDBYLPFSWZWCQE-UHFFFAOYSA-L 0.000 claims 4
- 230000008020 evaporation Effects 0.000 claims 4
- 238000001704 evaporation Methods 0.000 claims 4
- 239000001866 hydroxypropyl methyl cellulose Substances 0.000 claims 4
- 229920003088 hydroxypropyl methyl cellulose Polymers 0.000 claims 4
- 235000010979 hydroxypropyl methyl cellulose Nutrition 0.000 claims 4
- UFVKGYZPFZQRLF-UHFFFAOYSA-N hydroxypropyl methyl cellulose Chemical group OC1C(O)C(OC)OC(CO)C1OC1C(O)C(O)C(OC2C(C(O)C(OC3C(C(O)C(O)C(CO)O3)O)C(CO)O2)O)C(CO)O1 UFVKGYZPFZQRLF-UHFFFAOYSA-N 0.000 claims 4
- 239000011230 binding agent Substances 0.000 claims 3
- 239000000546 pharmaceutical excipient Substances 0.000 claims 3
- KDYFGRWQOYBRFD-UHFFFAOYSA-L succinate(2-) Chemical compound [O-]C(=O)CCC([O-])=O KDYFGRWQOYBRFD-UHFFFAOYSA-L 0.000 claims 3
- 239000004094 surface-active agent Substances 0.000 claims 3
- LENZDBCJOHFCAS-UHFFFAOYSA-N tris Chemical compound OCC(N)(CO)CO LENZDBCJOHFCAS-UHFFFAOYSA-N 0.000 claims 3
- WQZGKKKJIJFFOK-GASJEMHNSA-N Glucose Natural products OC[C@H]1OC(O)[C@H](O)[C@@H](O)[C@@H]1O WQZGKKKJIJFFOK-GASJEMHNSA-N 0.000 claims 2
- 229920001214 Polysorbate 60 Polymers 0.000 claims 2
- UIIMBOGNXHQVGW-UHFFFAOYSA-M Sodium bicarbonate Chemical compound [Na+].OC([O-])=O UIIMBOGNXHQVGW-UHFFFAOYSA-M 0.000 claims 2
- ZUAAPNNKRHMPKG-UHFFFAOYSA-N acetic acid;butanedioic acid;methanol;propane-1,2-diol Chemical compound OC.CC(O)=O.CC(O)CO.OC(=O)CCC(O)=O ZUAAPNNKRHMPKG-UHFFFAOYSA-N 0.000 claims 2
- 125000002915 carbonyl group Chemical group [*:2]C([*:1])=O 0.000 claims 2
- 235000014113 dietary fatty acids Nutrition 0.000 claims 2
- 239000000194 fatty acid Substances 0.000 claims 2
- 229930195729 fatty acid Natural products 0.000 claims 2
- 239000008103 glucose Substances 0.000 claims 2
- 239000000203 mixture Substances 0.000 claims 2
- 239000001267 polyvinylpyrrolidone Substances 0.000 claims 2
- 229920000036 polyvinylpyrrolidone Polymers 0.000 claims 2
- 235000013855 polyvinylpyrrolidone Nutrition 0.000 claims 2
- BWHMMNNQKKPAPP-UHFFFAOYSA-L potassium carbonate Chemical compound [K+].[K+].[O-]C([O-])=O BWHMMNNQKKPAPP-UHFFFAOYSA-L 0.000 claims 2
- 229910000029 sodium carbonate Inorganic materials 0.000 claims 2
- 208000030814 Eating disease Diseases 0.000 claims 1
- 208000019454 Feeding and Eating disease Diseases 0.000 claims 1
- 102000051325 Glucagon Human genes 0.000 claims 1
- 108060003199 Glucagon Proteins 0.000 claims 1
- 101001015516 Homo sapiens Glucagon-like peptide 1 receptor Proteins 0.000 claims 1
- 208000008589 Obesity Diseases 0.000 claims 1
- 239000002202 Polyethylene glycol Substances 0.000 claims 1
- UIIMBOGNXHQVGW-DEQYMQKBSA-M Sodium bicarbonate-14C Chemical compound [Na+].O[14C]([O-])=O UIIMBOGNXHQVGW-DEQYMQKBSA-M 0.000 claims 1
- DBMJMQXJHONAFJ-UHFFFAOYSA-M Sodium laurylsulphate Chemical compound [Na+].CCCCCCCCCCCCOS([O-])(=O)=O DBMJMQXJHONAFJ-UHFFFAOYSA-M 0.000 claims 1
- AOBORMOPSGHCAX-UHFFFAOYSA-N Tocophersolan Chemical compound OCCOC(=O)CCC(=O)OC1=C(C)C(C)=C2OC(CCCC(C)CCCC(C)CCCC(C)C)(C)CCC2=C1C AOBORMOPSGHCAX-UHFFFAOYSA-N 0.000 claims 1
- 206010067584 Type 1 diabetes mellitus Diseases 0.000 claims 1
- 239000008280 blood Substances 0.000 claims 1
- 210000004369 blood Anatomy 0.000 claims 1
- 230000001419 dependent effect Effects 0.000 claims 1
- 235000014632 disordered eating Nutrition 0.000 claims 1
- 230000030136 gastric emptying Effects 0.000 claims 1
- MASNOZXLGMXCHN-ZLPAWPGGSA-N glucagon Chemical compound C([C@@H](C(=O)N[C@H](C(=O)N[C@@H](CCC(N)=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](CCSC)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H]([C@@H](C)O)C(O)=O)C(C)C)NC(=O)[C@H](CC(O)=O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](C)NC(=O)[C@H](CCCNC(N)=N)NC(=O)[C@H](CCCNC(N)=N)NC(=O)[C@H](CO)NC(=O)[C@H](CC(O)=O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CC=1C=CC(O)=CC=1)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CO)NC(=O)[C@H](CC=1C=CC(O)=CC=1)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(N)=O)NC(=O)[C@H](CO)NC(=O)[C@@H](N)CC=1NC=NC=1)[C@@H](C)O)[C@@H](C)O)C1=CC=CC=C1 MASNOZXLGMXCHN-ZLPAWPGGSA-N 0.000 claims 1
- 229960004666 glucagon Drugs 0.000 claims 1
- 230000002401 inhibitory effect Effects 0.000 claims 1
- 230000003914 insulin secretion Effects 0.000 claims 1
- 235000020824 obesity Nutrition 0.000 claims 1
- 229920001223 polyethylene glycol Polymers 0.000 claims 1
- 239000011736 potassium bicarbonate Substances 0.000 claims 1
- 229910000028 potassium bicarbonate Inorganic materials 0.000 claims 1
- 235000015497 potassium bicarbonate Nutrition 0.000 claims 1
- 229910000027 potassium carbonate Inorganic materials 0.000 claims 1
- 235000011181 potassium carbonates Nutrition 0.000 claims 1
- TYJJADVDDVDEDZ-UHFFFAOYSA-M potassium hydrogencarbonate Chemical compound [K+].OC([O-])=O TYJJADVDDVDEDZ-UHFFFAOYSA-M 0.000 claims 1
- 150000003839 salts Chemical class 0.000 claims 1
- 230000028327 secretion Effects 0.000 claims 1
- 229910000030 sodium bicarbonate Inorganic materials 0.000 claims 1
- 235000017557 sodium bicarbonate Nutrition 0.000 claims 1
- 235000017550 sodium carbonate Nutrition 0.000 claims 1
- 235000019333 sodium laurylsulphate Nutrition 0.000 claims 1
- 239000001488 sodium phosphate Substances 0.000 claims 1
- RYFMWSXOAZQYPI-UHFFFAOYSA-K trisodium phosphate Chemical group [Na+].[Na+].[Na+].[O-]P([O-])([O-])=O RYFMWSXOAZQYPI-UHFFFAOYSA-K 0.000 claims 1
- 229910000406 trisodium phosphate Inorganic materials 0.000 claims 1
- 235000019801 trisodium phosphate Nutrition 0.000 claims 1
- 208000001072 type 2 diabetes mellitus Diseases 0.000 claims 1
- 229940053446 vitamin E d-alpha Drugs 0.000 claims 1
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201261614265P | 2012-03-22 | 2012-03-22 | |
| US61/614,265 | 2012-03-22 | ||
| PCT/US2013/033091 WO2013142569A1 (en) | 2012-03-22 | 2013-03-20 | Tris(hydroxymethyl)aminomethane salts of a small-molecule glp1r agonist and pharmaceutical compositions and uses thereof |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| JP2015510947A JP2015510947A (ja) | 2015-04-13 |
| JP2015510947A5 true JP2015510947A5 (https=) | 2016-05-19 |
Family
ID=49223316
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2015501876A Ceased JP2015510947A (ja) | 2012-03-22 | 2013-03-20 | 小分子ｇｌｐ１ｒアゴニストのトリス（ヒドロキシメチル）アミノメタン塩ならびにその医薬組成物および使用 |
Country Status (16)
| Country | Link |
|---|---|
| US (1) | US9198901B2 (https=) |
| EP (1) | EP2854526B1 (https=) |
| JP (1) | JP2015510947A (https=) |
| KR (1) | KR102158992B1 (https=) |
| CN (1) | CN104202977A (https=) |
| AU (1) | AU2013235167B2 (https=) |
| CA (1) | CA2868033A1 (https=) |
| EA (1) | EA201491749A1 (https=) |
| ES (1) | ES2674951T3 (https=) |
| HK (1) | HK1199371A1 (https=) |
| IL (1) | IL234615B (https=) |
| IN (1) | IN2014DN07867A (https=) |
| MX (1) | MX352804B (https=) |
| NZ (1) | NZ629203A (https=) |
| SG (1) | SG11201405353VA (https=) |
| WO (1) | WO2013142569A1 (https=) |
Families Citing this family (6)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| EP3790549A1 (en) * | 2018-05-08 | 2021-03-17 | vTv Therapeutics LLC | Therapeutic uses of glp1r agonists |
| US12459954B2 (en) | 2020-04-01 | 2025-11-04 | Hangzhou Zhongmei Huadong Pharmaceutical Co., Ltd. | Crystalline form a of GLP-1 receptor agonist and preparation method therefor |
| WO2021196951A1 (zh) * | 2020-04-01 | 2021-10-07 | 杭州中美华东制药有限公司 | Glp-1受体激动剂游离碱的药学上可接受的酸式盐及其制备方法 |
| TW202521533A (zh) | 2023-09-14 | 2025-06-01 | 香港商歌禮製藥(中國)有限公司 | Glp-1r 激動劑及其治療方法 |
| US12291530B1 (en) | 2023-11-24 | 2025-05-06 | Ascletis Pharma (China) Co., Limited | GLP-1R agonist and therapeutic method thereof |
| WO2025158275A1 (en) | 2024-01-24 | 2025-07-31 | Pfizer Inc. | Combination therapy using glucose-dependent insulinotropic polypeptide receptor antagonist compounds and glp-1 receptor agonist compounds |
Family Cites Families (10)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| BR9710448A (pt) * | 1996-05-20 | 1999-08-17 | Searle & Co | Formula-{es farmac-uticas de sal de pot ssio sÄdioe tris oxaprozina |
| AR024076A1 (es) * | 1999-05-25 | 2002-09-04 | Smithkline Beecham Corp | Sales de cis-[4-ciano-4-(3-ciclopentiloxi-4-metoxifenil) ciclohexan-1-carboxilato] |
| JP2004520393A (ja) * | 2001-02-05 | 2004-07-08 | ドクター・レディーズ・ラボラトリーズ・リミテッド | ヘテロ環化号物の薬学的に許容可能な塩 |
| US7696231B2 (en) * | 2001-10-30 | 2010-04-13 | Laboratoires Serono Sa | Oxindole hydrazide modulators of protein tyrosine phosphatases (PTPs) |
| CN1774246A (zh) * | 2003-04-18 | 2006-05-17 | 因齐特圣迭戈公司 | 用于治疗代谢失调、癌症和其它疾病的取代异色满化合物 |
| US7727983B2 (en) * | 2008-03-07 | 2010-06-01 | Transtech Pharma, Inc. | Oxadiazoanthracene compounds for the treatment of diabetes |
| WO2009123241A1 (ja) * | 2008-03-31 | 2009-10-08 | 株式会社レナサイエンス | プラスミノーゲンアクチベーターインヒビター－１阻害剤 |
| RU2502730C2 (ru) * | 2008-06-05 | 2013-12-27 | Асахи Касеи Фарма Корпорейшн | Сульфонамидные соединения и их применение |
| US9163024B2 (en) * | 2008-12-08 | 2015-10-20 | Glaxosmithkline Llc | Tris salts of 8-chloro-3-pentyl-3,7-dihydro-1H-purine-2,6-dione |
| WO2011031620A1 (en) * | 2009-09-11 | 2011-03-17 | Transtech Pharma, Inc. | Solid compositions comprising an oxadiazoanthracene compound and methods of making and using the same |
-
2013
- 2013-03-20 EA EA201491749A patent/EA201491749A1/ru unknown
- 2013-03-20 CN CN201380015508.2A patent/CN104202977A/zh active Pending
- 2013-03-20 ES ES13765015.6T patent/ES2674951T3/es active Active
- 2013-03-20 JP JP2015501876A patent/JP2015510947A/ja not_active Ceased
- 2013-03-20 CA CA2868033A patent/CA2868033A1/en not_active Abandoned
- 2013-03-20 SG SG11201405353VA patent/SG11201405353VA/en unknown
- 2013-03-20 EP EP13765015.6A patent/EP2854526B1/en active Active
- 2013-03-20 HK HK14112910.6A patent/HK1199371A1/xx unknown
- 2013-03-20 AU AU2013235167A patent/AU2013235167B2/en active Active
- 2013-03-20 KR KR1020147026362A patent/KR102158992B1/ko active Active
- 2013-03-20 IN IN7867DEN2014 patent/IN2014DN07867A/en unknown
- 2013-03-20 NZ NZ629203A patent/NZ629203A/en not_active IP Right Cessation
- 2013-03-20 WO PCT/US2013/033091 patent/WO2013142569A1/en not_active Ceased
- 2013-03-20 MX MX2014010366A patent/MX352804B/es active IP Right Grant
-
2014
- 2014-09-11 IL IL234615A patent/IL234615B/en not_active IP Right Cessation
- 2014-09-18 US US14/489,890 patent/US9198901B2/en active Active
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