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 |
|---|---|---|---|---|
| MX2020008387A (es) * | 2018-05-08 | 2020-12-11 | Vtv Therapeutics Llc | Usos terapeuticos de agonistas glp1r. |
| 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 |
| JP2023528726A (ja) * | 2020-04-01 | 2023-07-06 | ハンジョウ ジョンメイ フアドン ファーマシューティカル シーオー．，エルティーディー． | Ｇｌｐ１ｒアゴニスト遊離塩基の薬学的に許容される酸塩類およびその調製法 |
| CN120981457A (zh) | 2023-09-14 | 2025-11-18 | 歌礼制药(中国)有限公司 | Glp-1r激动剂及其治疗方法 |
| TW202521534A (zh) | 2023-11-24 | 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 |
| 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 |
|---|---|---|---|---|
| PL330145A1 (en) * | 1996-05-20 | 1999-04-26 | Searle & Co | Pharmaceutic preparations containing sodium and potassum oxaprosin salt as well as that formed from tris |
| 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 |
| CA2463615C (en) * | 2001-10-30 | 2011-07-26 | Applied Research Systems Ars Holding N.V. | Oxindole hydrazide modulators of protein tyrosine phosphatases (ptps) |
| US20050038098A1 (en) * | 2003-04-18 | 2005-02-17 | Catherine Tachdjian | Substituted dihydronaphthalene and isochroman compounds for the treatment of metabolic disorders, cancer and other diseases |
| EA018225B1 (ru) | 2008-03-07 | 2013-06-28 | Транстек Фарма, Инк. | Соединения оксадиазоантрацена для лечения диабета |
| EP2272822A4 (en) * | 2008-03-31 | 2012-01-18 | Renascience Co Ltd | PLASMINOG ACTIVATOR-1 HEMMER |
| CN102056897B (zh) * | 2008-06-05 | 2014-05-07 | 旭化成制药株式会社 | 磺酰胺化合物及其用途 |
| DK2370440T3 (en) * | 2008-12-08 | 2014-12-08 | Glaxosmithkline Llc | 8-Chloro-3-pentyl-3,7-dihydro-1H-purine-2,6-dion2-amino-2- (hydroxymethyl) -1,3-propandiolanhydrat for the treatment of diseases |
| US20110064806A1 (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 WO PCT/US2013/033091 patent/WO2013142569A1/en not_active Ceased
- 2013-03-20 IN IN7867DEN2014 patent/IN2014DN07867A/en unknown
- 2013-03-20 CA CA2868033A patent/CA2868033A1/en not_active Abandoned
- 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 JP JP2015501876A patent/JP2015510947A/ja not_active Ceased
- 2013-03-20 MX MX2014010366A patent/MX352804B/es active IP Right Grant
- 2013-03-20 KR KR1020147026362A patent/KR102158992B1/ko active Active
- 2013-03-20 NZ NZ629203A patent/NZ629203A/en not_active IP Right Cessation
- 2013-03-20 SG SG11201405353VA patent/SG11201405353VA/en unknown
- 2013-03-20 ES ES13765015.6T patent/ES2674951T3/es active Active
- 2013-03-20 CN CN201380015508.2A patent/CN104202977A/zh active Pending
-
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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