JP2009507018A5 - - Google Patents
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- Publication number
- JP2009507018A5 JP2009507018A5 JP2008529147A JP2008529147A JP2009507018A5 JP 2009507018 A5 JP2009507018 A5 JP 2009507018A5 JP 2008529147 A JP2008529147 A JP 2008529147A JP 2008529147 A JP2008529147 A JP 2008529147A JP 2009507018 A5 JP2009507018 A5 JP 2009507018A5
- Authority
- JP
- Japan
- Prior art keywords
- acid
- pharmaceutical composition
- argatroban
- amino
- methyl
- 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
Links
- 239000008194 pharmaceutical composition Substances 0.000 claims 13
- KXNPVXPOPUZYGB-XYVMCAHJSA-N argatroban Chemical compound OC(=O)[C@H]1C[C@H](C)CCN1C(=O)[C@H](CCCN=C(N)N)NS(=O)(=O)C1=CC=CC2=C1NC[C@H](C)C2 KXNPVXPOPUZYGB-XYVMCAHJSA-N 0.000 claims 10
- 229960003856 argatroban Drugs 0.000 claims 10
- 125000002924 primary amino group Chemical group [H]N([H])* 0.000 claims 10
- -1 aminoiminomethyl Chemical group 0.000 claims 9
- QTBSBXVTEAMEQO-UHFFFAOYSA-N Acetic acid Chemical compound CC(O)=O QTBSBXVTEAMEQO-UHFFFAOYSA-N 0.000 claims 6
- 230000003204 osmotic effect Effects 0.000 claims 6
- 239000000243 solution Substances 0.000 claims 6
- 239000002253 acid Substances 0.000 claims 5
- 125000001147 pentyl group Chemical group C(CCCC)* 0.000 claims 5
- 125000000472 sulfonyl group Chemical group *S(*)(=O)=O 0.000 claims 5
- LFQSCWFLJHTTHZ-UHFFFAOYSA-N Ethanol Chemical compound CCO LFQSCWFLJHTTHZ-UHFFFAOYSA-N 0.000 claims 4
- FAPWRFPIFSIZLT-UHFFFAOYSA-M Sodium chloride Chemical compound [Na+].[Cl-] FAPWRFPIFSIZLT-UHFFFAOYSA-M 0.000 claims 4
- 239000003795 chemical substances by application Substances 0.000 claims 4
- 238000000034 method Methods 0.000 claims 4
- KRKNYBCHXYNGOX-UHFFFAOYSA-N citric acid Chemical compound OC(=O)CC(O)(C(O)=O)CC(O)=O KRKNYBCHXYNGOX-UHFFFAOYSA-N 0.000 claims 3
- 238000007911 parenteral administration Methods 0.000 claims 3
- FEWJPZIEWOKRBE-JCYAYHJZSA-N Dextrotartaric acid Chemical compound OC(=O)[C@H](O)[C@@H](O)C(O)=O FEWJPZIEWOKRBE-JCYAYHJZSA-N 0.000 claims 2
- DHMQDGOQFOQNFH-UHFFFAOYSA-N Glycine Chemical compound NCC(O)=O DHMQDGOQFOQNFH-UHFFFAOYSA-N 0.000 claims 2
- VEXZGXHMUGYJMC-UHFFFAOYSA-N Hydrochloric acid Chemical compound Cl VEXZGXHMUGYJMC-UHFFFAOYSA-N 0.000 claims 2
- NBIIXXVUZAFLBC-UHFFFAOYSA-N Phosphoric acid Chemical compound OP(O)(O)=O NBIIXXVUZAFLBC-UHFFFAOYSA-N 0.000 claims 2
- WCUXLLCKKVVCTQ-UHFFFAOYSA-M Potassium chloride Chemical compound [Cl-].[K+] WCUXLLCKKVVCTQ-UHFFFAOYSA-M 0.000 claims 2
- FEWJPZIEWOKRBE-UHFFFAOYSA-N Tartaric acid Natural products [H+].[H+].[O-]C(=O)C(O)C(O)C([O-])=O FEWJPZIEWOKRBE-UHFFFAOYSA-N 0.000 claims 2
- BJEPYKJPYRNKOW-UHFFFAOYSA-N alpha-hydroxysuccinic acid Natural products OC(=O)C(O)CC(O)=O BJEPYKJPYRNKOW-UHFFFAOYSA-N 0.000 claims 2
- BDAGIHXWWSANSR-UHFFFAOYSA-N methanoic acid Natural products OC=O BDAGIHXWWSANSR-UHFFFAOYSA-N 0.000 claims 2
- 239000000203 mixture Substances 0.000 claims 2
- 239000011780 sodium chloride Substances 0.000 claims 2
- 230000003381 solubilizing effect Effects 0.000 claims 2
- 239000011975 tartaric acid Substances 0.000 claims 2
- 235000002906 tartaric acid Nutrition 0.000 claims 2
- BJEPYKJPYRNKOW-REOHCLBHSA-N (S)-malic acid Chemical compound OC(=O)[C@@H](O)CC(O)=O BJEPYKJPYRNKOW-REOHCLBHSA-N 0.000 claims 1
- OSWFIVFLDKOXQC-UHFFFAOYSA-N 4-(3-methoxyphenyl)aniline Chemical compound COC1=CC=CC(C=2C=CC(N)=CC=2)=C1 OSWFIVFLDKOXQC-UHFFFAOYSA-N 0.000 claims 1
- CYDQOEWLBCCFJZ-UHFFFAOYSA-N 4-(4-fluorophenyl)oxane-4-carboxylic acid Chemical compound C=1C=C(F)C=CC=1C1(C(=O)O)CCOCC1 CYDQOEWLBCCFJZ-UHFFFAOYSA-N 0.000 claims 1
- QTBSBXVTEAMEQO-UHFFFAOYSA-M Acetate Chemical compound CC([O-])=O QTBSBXVTEAMEQO-UHFFFAOYSA-M 0.000 claims 1
- UXVMQQNJUSDDNG-UHFFFAOYSA-L Calcium chloride Chemical compound [Cl-].[Cl-].[Ca+2] UXVMQQNJUSDDNG-UHFFFAOYSA-L 0.000 claims 1
- KRKNYBCHXYNGOX-UHFFFAOYSA-K Citrate Chemical compound [O-]C(=O)CC(O)(CC([O-])=O)C([O-])=O KRKNYBCHXYNGOX-UHFFFAOYSA-K 0.000 claims 1
- RGHNJXZEOKUKBD-SQOUGZDYSA-M D-gluconate Chemical compound OC[C@@H](O)[C@@H](O)[C@H](O)[C@@H](O)C([O-])=O RGHNJXZEOKUKBD-SQOUGZDYSA-M 0.000 claims 1
- 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 1
- 239000004471 Glycine Substances 0.000 claims 1
- WHUUTDBJXJRKMK-VKHMYHEASA-N L-glutamic acid Chemical compound OC(=O)[C@@H](N)CCC(O)=O WHUUTDBJXJRKMK-VKHMYHEASA-N 0.000 claims 1
- JVTAAEKCZFNVCJ-UHFFFAOYSA-M Lactate Chemical compound CC(O)C([O-])=O JVTAAEKCZFNVCJ-UHFFFAOYSA-M 0.000 claims 1
- 229910019142 PO4 Inorganic materials 0.000 claims 1
- 229940122388 Thrombin inhibitor Drugs 0.000 claims 1
- 235000011054 acetic acid Nutrition 0.000 claims 1
- 229910000147 aluminium phosphate Inorganic materials 0.000 claims 1
- 239000003708 ampul Substances 0.000 claims 1
- 239000007864 aqueous solution Substances 0.000 claims 1
- WPYMKLBDIGXBTP-UHFFFAOYSA-N benzoic acid Chemical compound OC(=O)C1=CC=CC=C1 WPYMKLBDIGXBTP-UHFFFAOYSA-N 0.000 claims 1
- WQZGKKKJIJFFOK-VFUOTHLCSA-N beta-D-glucose Chemical compound OC[C@H]1O[C@@H](O)[C@H](O)[C@@H](O)[C@@H]1O WQZGKKKJIJFFOK-VFUOTHLCSA-N 0.000 claims 1
- 239000001110 calcium chloride Substances 0.000 claims 1
- 229910001628 calcium chloride Inorganic materials 0.000 claims 1
- 235000015165 citric acid Nutrition 0.000 claims 1
- 239000008121 dextrose Substances 0.000 claims 1
- 235000019253 formic acid Nutrition 0.000 claims 1
- 229940050410 gluconate Drugs 0.000 claims 1
- 229930195712 glutamate Natural products 0.000 claims 1
- 235000011167 hydrochloric acid Nutrition 0.000 claims 1
- 238000001802 infusion Methods 0.000 claims 1
- 229940001447 lactate Drugs 0.000 claims 1
- 229940049920 malate Drugs 0.000 claims 1
- 239000001630 malic acid Substances 0.000 claims 1
- 235000011090 malic acid Nutrition 0.000 claims 1
- NBIIXXVUZAFLBC-UHFFFAOYSA-K phosphate Chemical compound [O-]P([O-])([O-])=O NBIIXXVUZAFLBC-UHFFFAOYSA-K 0.000 claims 1
- 239000010452 phosphate Substances 0.000 claims 1
- 235000011007 phosphoric acid Nutrition 0.000 claims 1
- 239000001103 potassium chloride Substances 0.000 claims 1
- 235000011164 potassium chloride Nutrition 0.000 claims 1
- 239000001540 sodium lactate Substances 0.000 claims 1
- 235000011088 sodium lactate Nutrition 0.000 claims 1
- 229940005581 sodium lactate Drugs 0.000 claims 1
- 235000000346 sugar Nutrition 0.000 claims 1
- 150000008163 sugars Chemical class 0.000 claims 1
- 239000003868 thrombin inhibitor Substances 0.000 claims 1
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US71340305P | 2005-09-01 | 2005-09-01 | |
| US60/713,403 | 2005-09-01 | ||
| PCT/US2006/033432 WO2007027565A2 (en) | 2005-09-01 | 2006-08-28 | Argatroban formulation comprising an acid as solubilizer |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2009507018A JP2009507018A (ja) | 2009-02-19 |
| JP2009507018A5 true JP2009507018A5 (enExample) | 2009-09-24 |
| JP5189980B2 JP5189980B2 (ja) | 2013-04-24 |
Family
ID=37809398
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2008529147A Expired - Fee Related JP5189980B2 (ja) | 2005-09-01 | 2006-08-28 | 可溶化剤として酸を含むアルガトロバン処方物 |
Country Status (22)
| Country | Link |
|---|---|
| US (3) | US7642271B2 (enExample) |
| EP (1) | EP1948133B1 (enExample) |
| JP (1) | JP5189980B2 (enExample) |
| KR (3) | KR20080042155A (enExample) |
| CN (2) | CN101257890B (enExample) |
| AT (1) | ATE514416T1 (enExample) |
| AU (1) | AU2006285097B2 (enExample) |
| BR (1) | BRPI0616127B8 (enExample) |
| CA (1) | CA2617920C (enExample) |
| CY (1) | CY1112109T1 (enExample) |
| DK (1) | DK1948133T3 (enExample) |
| ES (1) | ES2368758T3 (enExample) |
| IL (2) | IL189290A (enExample) |
| IN (1) | IN2015DN03947A (enExample) |
| MX (1) | MX2008002177A (enExample) |
| NZ (1) | NZ565821A (enExample) |
| PL (1) | PL1948133T3 (enExample) |
| PT (1) | PT1948133E (enExample) |
| RU (1) | RU2416393C2 (enExample) |
| SI (1) | SI1948133T1 (enExample) |
| WO (1) | WO2007027565A2 (enExample) |
| ZA (1) | ZA200802667B (enExample) |
Families Citing this family (15)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| IN2015DN03947A (enExample) * | 2005-09-01 | 2015-10-02 | Baxter Int | |
| US7589106B2 (en) | 2006-09-27 | 2009-09-15 | Eagle Pharmaceuticals, Inc. | Alcohol free formulation of argatroban |
| US7687516B2 (en) * | 2006-09-27 | 2010-03-30 | Eagle Pharmaceuticals, Inc. | Alcohol free formulation of argatroban |
| US20100076019A1 (en) * | 2006-10-11 | 2010-03-25 | Eagle Pharmaceuticals, Inc. | Alcohol free formulation of argatroban |
| US7915290B2 (en) * | 2008-02-29 | 2011-03-29 | Baxter International Inc. | Argatroban formulations and methods for making and using same |
| US20090221637A1 (en) * | 2008-02-29 | 2009-09-03 | Baxter International Inc. | Solid-state salt argatroban formulations and methods for producing and using the same |
| CN101598725B (zh) * | 2009-06-23 | 2012-07-18 | 南通大学附属医院 | 阿加曲班在血细胞和生化常规分析中的应用 |
| PL2616064T3 (pl) | 2010-10-21 | 2020-02-28 | Rtu Pharmaceuticals Llc | Gotowe do zastosowania formulacje ketorolaku |
| CN102120026A (zh) * | 2011-03-03 | 2011-07-13 | 天津市炜杰科技有限公司 | 以醇作为增溶剂的21(s)阿加曲班静脉注射液 |
| CN102119922A (zh) * | 2011-03-03 | 2011-07-13 | 天津市炜杰科技有限公司 | 以酸作为增溶剂的21(s)阿加曲班静脉注射液 |
| CN102228677A (zh) * | 2011-06-17 | 2011-11-02 | 天津市炜杰科技有限公司 | 以酸作为增溶剂的21(r)阿加曲班静脉注射液 |
| TWI632921B (zh) * | 2011-10-19 | 2018-08-21 | 大塚製藥股份有限公司 | 口服溶液 |
| EP3383494A4 (en) * | 2015-12-04 | 2019-08-07 | The Regents of The University of California | Histone deacetylase INHIBITORS |
| CN107773533A (zh) * | 2016-08-26 | 2018-03-09 | 四川科瑞德制药股份有限公司 | 一种新型凝血酶抑制剂及其制备方法 |
| CN115381927A (zh) * | 2022-09-20 | 2022-11-25 | 晓恩医药包装材料(安庆)有限公司 | 一种用于治疗缺血性脑梗塞的药物预灌装注射剂 |
Family Cites Families (16)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| SE420919B (sv) * | 1973-08-13 | 1981-11-09 | Mitsubishi Chem Ind | Forfarande for framstellning av n?722-dansyl-l-argininderivat och farmaceutiskt godtagbara syradditionssalter derav |
| US5214052A (en) * | 1987-07-28 | 1993-05-25 | Mitsubishi Kasei Corporation | Method for dissolving arginineamides and pharmaceutical compositions containing them |
| US5506241A (en) * | 1992-03-18 | 1996-04-09 | Mitsubishi Chemical Corporation | Argatroban preparations for ophthalmic use |
| CA2091715A1 (en) | 1992-03-18 | 1993-09-19 | Mitsubishi Kasei Corporation | Argatroban preparations for ophthalmic use |
| JPH06219949A (ja) * | 1993-01-25 | 1994-08-09 | Mitsubishi Kasei Corp | 抗トロンビン剤及びその製造方法 |
| JPH06219948A (ja) * | 1993-01-25 | 1994-08-09 | Mitsubishi Kasei Corp | 抗トロンビン剤及びその製造方法 |
| JPH07228532A (ja) * | 1993-04-22 | 1995-08-29 | Senju Pharmaceut Co Ltd | 水性液剤、その有効成分の溶解性向上方法および安定化方法 |
| CA2121723A1 (en) | 1993-04-22 | 1994-10-23 | Yoshifumi Ikejiri | Aqueous agent |
| US5998019A (en) | 1993-11-16 | 1999-12-07 | Baxter International Inc. | Multi-layered polymer structure for medical products |
| US5849843A (en) | 1993-11-16 | 1998-12-15 | Baxter International Inc. | Polymeric compositions for medical packaging and devices |
| FR2715566B1 (fr) * | 1994-02-03 | 1996-03-08 | Synthelabo | Solutions aqueuses concentrées d'argatroban. |
| US5840733A (en) | 1996-07-01 | 1998-11-24 | Redcell, Canada, Inc. | Methods and compositions for producing novel conjugates of thrombin inhibitors and endogenous carriers resulting in anti-thrombins with extended lifetimes |
| JPH10316569A (ja) * | 1997-05-19 | 1998-12-02 | Mitsubishi Chem Corp | アルガトロバンの可溶化方法及びそれによるアルガトロバン含有外用水性薬剤 |
| WO2004083201A1 (ja) * | 2003-03-20 | 2004-09-30 | Mitsubishi Pharma Corporation | アルギニンアミド類を含有する医薬製剤 |
| US20060198836A1 (en) | 2003-07-17 | 2006-09-07 | Smithkline Beecham Corporation | Method of treating hit patients with argatroban |
| IN2015DN03947A (enExample) * | 2005-09-01 | 2015-10-02 | Baxter Int |
-
2006
- 2006-08-28 IN IN3947DEN2015 patent/IN2015DN03947A/en unknown
- 2006-08-28 KR KR1020087007748A patent/KR20080042155A/ko not_active Ceased
- 2006-08-28 US US11/510,981 patent/US7642271B2/en active Active
- 2006-08-28 RU RU2008112311/15A patent/RU2416393C2/ru active
- 2006-08-28 CN CN2006800322085A patent/CN101257890B/zh not_active Expired - Fee Related
- 2006-08-28 EP EP06802424A patent/EP1948133B1/en not_active Not-in-force
- 2006-08-28 KR KR1020147000036A patent/KR101753949B1/ko not_active Expired - Fee Related
- 2006-08-28 CN CN201210353437.4A patent/CN102895179B/zh not_active Expired - Fee Related
- 2006-08-28 WO PCT/US2006/033432 patent/WO2007027565A2/en not_active Ceased
- 2006-08-28 KR KR1020157025457A patent/KR20150108430A/ko not_active Ceased
- 2006-08-28 AT AT06802424T patent/ATE514416T1/de active
- 2006-08-28 NZ NZ565821A patent/NZ565821A/en not_active IP Right Cessation
- 2006-08-28 SI SI200631063T patent/SI1948133T1/sl unknown
- 2006-08-28 DK DK06802424.9T patent/DK1948133T3/da active
- 2006-08-28 BR BRPI0616127A patent/BRPI0616127B8/pt not_active IP Right Cessation
- 2006-08-28 JP JP2008529147A patent/JP5189980B2/ja not_active Expired - Fee Related
- 2006-08-28 MX MX2008002177A patent/MX2008002177A/es active IP Right Grant
- 2006-08-28 ES ES06802424T patent/ES2368758T3/es active Active
- 2006-08-28 CA CA2617920A patent/CA2617920C/en not_active Expired - Fee Related
- 2006-08-28 PL PL06802424T patent/PL1948133T3/pl unknown
- 2006-08-28 PT PT06802424T patent/PT1948133E/pt unknown
- 2006-08-28 AU AU2006285097A patent/AU2006285097B2/en not_active Ceased
-
2008
- 2008-02-05 IL IL189290A patent/IL189290A/en active IP Right Grant
- 2008-03-26 ZA ZA200802667A patent/ZA200802667B/xx unknown
-
2009
- 2009-12-28 US US12/647,854 patent/US8034830B2/en active Active
- 2009-12-28 US US12/647,841 patent/US7985757B2/en active Active
-
2010
- 2010-09-16 IL IL208183A patent/IL208183A0/en unknown
-
2011
- 2011-08-30 CY CY20111100825T patent/CY1112109T1/el unknown
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