JP2017525704A5 - - Google Patents
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- Publication number
- JP2017525704A5 JP2017525704A5 JP2017509739A JP2017509739A JP2017525704A5 JP 2017525704 A5 JP2017525704 A5 JP 2017525704A5 JP 2017509739 A JP2017509739 A JP 2017509739A JP 2017509739 A JP2017509739 A JP 2017509739A JP 2017525704 A5 JP2017525704 A5 JP 2017525704A5
- Authority
- JP
- Japan
- Prior art keywords
- seq
- chain
- amino acid
- acid sequence
- polypeptide
- 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
- 239000000203 mixture Substances 0.000 claims description 28
- 229920001184 polypeptide Polymers 0.000 claims description 26
- 102000004196 processed proteins & peptides Human genes 0.000 claims description 26
- 108090000765 processed proteins & peptides Proteins 0.000 claims description 26
- 125000003275 alpha amino acid group Chemical group 0.000 claims description 24
- 125000000151 cysteine group Chemical group N[C@@H](CS)C(=O)* 0.000 claims description 24
- FBPFZTCFMRRESA-KVTDHHQDSA-N D-Mannitol Chemical compound OC[C@@H](O)[C@@H](O)[C@H](O)[C@H](O)CO FBPFZTCFMRRESA-KVTDHHQDSA-N 0.000 claims description 20
- 229930195725 Mannitol Natural products 0.000 claims description 20
- 239000000594 mannitol Substances 0.000 claims description 20
- 235000010355 mannitol Nutrition 0.000 claims description 20
- 229930006000 Sucrose Natural products 0.000 claims description 19
- 239000005720 sucrose Substances 0.000 claims description 19
- CZMRCDWAGMRECN-UGDNZRGBSA-N Sucrose Chemical compound O[C@H]1[C@H](O)[C@@H](CO)O[C@@]1(CO)O[C@@H]1[C@H](O)[C@@H](O)[C@H](O)[C@@H](CO)O1 CZMRCDWAGMRECN-UGDNZRGBSA-N 0.000 claims description 16
- 239000013011 aqueous formulation Substances 0.000 claims description 14
- 239000004475 Arginine Substances 0.000 claims description 13
- 229960003121 arginine Drugs 0.000 claims description 13
- 235000009697 arginine Nutrition 0.000 claims description 13
- ODKSFYDXXFIFQN-UHFFFAOYSA-N arginine Natural products OC(=O)C(N)CCCNC(N)=N ODKSFYDXXFIFQN-UHFFFAOYSA-N 0.000 claims description 13
- 238000009472 formulation Methods 0.000 claims description 12
- KWTQSFXGGICVPE-WCCKRBBISA-N Arginine hydrochloride Chemical compound Cl.OC(=O)[C@@H](N)CCCN=C(N)N KWTQSFXGGICVPE-WCCKRBBISA-N 0.000 claims description 6
- 238000002360 preparation method Methods 0.000 claims description 6
- 239000002904 solvent Substances 0.000 claims description 5
- 239000003381 stabilizer Substances 0.000 claims description 5
- 229940123583 Factor Xa inhibitor Drugs 0.000 claims description 4
- 229940024606 amino acid Drugs 0.000 claims description 4
- 235000001014 amino acid Nutrition 0.000 claims description 4
- 150000001413 amino acids Chemical class 0.000 claims description 4
- 238000004108 freeze drying Methods 0.000 claims description 4
- 238000000034 method Methods 0.000 claims description 4
- 125000000637 arginyl group Chemical group N[C@@H](CCCNC(N)=N)C(=O)* 0.000 claims description 3
- 125000000185 sucrose group Chemical group 0.000 claims description 3
- 239000004094 surface-active agent Substances 0.000 claims description 3
- QNZCBYKSOIHPEH-UHFFFAOYSA-N Apixaban Chemical compound C1=CC(OC)=CC=C1N1C(C(=O)N(CC2)C=3C=CC(=CC=3)N3C(CCCC3)=O)=C2C(C(N)=O)=N1 QNZCBYKSOIHPEH-UHFFFAOYSA-N 0.000 claims description 2
- 125000000539 amino acid group Chemical group 0.000 claims description 2
- 229960003886 apixaban Drugs 0.000 claims description 2
- 239000003125 aqueous solvent Substances 0.000 claims description 2
- 229950011103 betrixaban Drugs 0.000 claims description 2
- XHOLNRLADUSQLD-UHFFFAOYSA-N betrixaban Chemical compound C=1C=C(Cl)C=NC=1NC(=O)C1=CC(OC)=CC=C1NC(=O)C1=CC=C(C(=N)N(C)C)C=C1 XHOLNRLADUSQLD-UHFFFAOYSA-N 0.000 claims description 2
- 230000000740 bleeding effect Effects 0.000 claims description 2
- 239000003112 inhibitor Substances 0.000 claims description 2
- 239000012931 lyophilized formulation Substances 0.000 claims description 2
- 238000012986 modification Methods 0.000 claims description 2
- 230000004048 modification Effects 0.000 claims description 2
- 235000018102 proteins Nutrition 0.000 claims description 2
- 108090000623 proteins and genes Proteins 0.000 claims description 2
- 102000004169 proteins and genes Human genes 0.000 claims description 2
- 108010014806 prothrombinase complex Proteins 0.000 claims description 2
- 229960001148 rivaroxaban Drugs 0.000 claims description 2
- KGFYHTZWPPHNLQ-AWEZNQCLSA-N rivaroxaban Chemical compound S1C(Cl)=CC=C1C(=O)NC[C@@H]1OC(=O)N(C=2C=CC(=CC=2)N2C(COCC2)=O)C1 KGFYHTZWPPHNLQ-AWEZNQCLSA-N 0.000 claims description 2
- 238000002560 therapeutic procedure Methods 0.000 claims description 2
- 239000003146 anticoagulant agent Substances 0.000 claims 1
- 229940127219 anticoagulant drug Drugs 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 description 1
- 230000010100 anticoagulation Effects 0.000 description 1
- 239000000243 solution Substances 0.000 description 1
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201462039809P | 2014-08-20 | 2014-08-20 | |
| US62/039,809 | 2014-08-20 | ||
| PCT/US2015/046173 WO2016029061A1 (en) | 2014-08-20 | 2015-08-20 | Lyophilized formulations for factor xa antidote |
Related Child Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2019165981A Division JP2019206595A (ja) | 2014-08-20 | 2019-09-12 | 第Ｘａ因子解毒剤の凍結乾燥製剤 |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2017525704A JP2017525704A (ja) | 2017-09-07 |
| JP2017525704A5 true JP2017525704A5 (cg-RX-API-DMAC7.html) | 2018-09-13 |
| JP6742986B2 JP6742986B2 (ja) | 2020-08-19 |
Family
ID=55351266
Family Applications (4)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2017509739A Active JP6742986B2 (ja) | 2014-08-20 | 2015-08-20 | 第Ｘａ因子解毒剤の凍結乾燥製剤 |
| JP2019165981A Withdrawn JP2019206595A (ja) | 2014-08-20 | 2019-09-12 | 第Ｘａ因子解毒剤の凍結乾燥製剤 |
| JP2021172975A Active JP7416549B2 (ja) | 2014-08-20 | 2021-10-22 | 第Ｘａ因子解毒剤の凍結乾燥製剤 |
| JP2023146769A Pending JP2023158199A (ja) | 2014-08-20 | 2023-09-11 | 第Ｘａ因子解毒剤の凍結乾燥製剤 |
Family Applications After (3)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2019165981A Withdrawn JP2019206595A (ja) | 2014-08-20 | 2019-09-12 | 第Ｘａ因子解毒剤の凍結乾燥製剤 |
| JP2021172975A Active JP7416549B2 (ja) | 2014-08-20 | 2021-10-22 | 第Ｘａ因子解毒剤の凍結乾燥製剤 |
| JP2023146769A Pending JP2023158199A (ja) | 2014-08-20 | 2023-09-11 | 第Ｘａ因子解毒剤の凍結乾燥製剤 |
Country Status (14)
| Country | Link |
|---|---|
| US (6) | US20160237420A1 (cg-RX-API-DMAC7.html) |
| EP (2) | EP3182993B1 (cg-RX-API-DMAC7.html) |
| JP (4) | JP6742986B2 (cg-RX-API-DMAC7.html) |
| KR (3) | KR102867491B1 (cg-RX-API-DMAC7.html) |
| CN (2) | CN107073082B (cg-RX-API-DMAC7.html) |
| AU (3) | AU2015305413B2 (cg-RX-API-DMAC7.html) |
| CA (1) | CA2961739C (cg-RX-API-DMAC7.html) |
| DK (1) | DK3182993T3 (cg-RX-API-DMAC7.html) |
| EA (2) | EA202091385A3 (cg-RX-API-DMAC7.html) |
| ES (1) | ES2814157T3 (cg-RX-API-DMAC7.html) |
| IL (2) | IL250413B (cg-RX-API-DMAC7.html) |
| SG (1) | SG11201701247RA (cg-RX-API-DMAC7.html) |
| WO (1) | WO2016029061A1 (cg-RX-API-DMAC7.html) |
| ZA (1) | ZA201701764B (cg-RX-API-DMAC7.html) |
Families Citing this family (7)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2010117729A1 (en) * | 2009-03-30 | 2010-10-14 | Portola Pharmaceuticals, Inc. | Antidotes for factor xa inhibitors and methods of using the same |
| CA2961739C (en) | 2014-08-20 | 2024-04-30 | Portola Pharmaceuticals, Inc. | Lyophilized formulations for factor xa antidote |
| US20190046450A1 (en) | 2016-02-24 | 2019-02-14 | Portola Pharmaceuticals, Inc. | Lyophilized formulations for factor xa antidote |
| PE20190661A1 (es) | 2016-06-17 | 2019-05-08 | Portola Pharm Inc | Preparacion de derivados del factor xa |
| EP3624828B1 (en) * | 2017-05-18 | 2024-08-07 | Merck Sharp & Dohme LLC | Pharmaceutical formulation comprising incretin-insulin conjugates |
| US20210196568A1 (en) * | 2018-05-21 | 2021-07-01 | Chugai Seiyaku Kabushiki Kaisha | Lyophilized formulation sealed in glass container |
| CN110760479A (zh) * | 2019-05-17 | 2020-02-07 | 上海交通大学医学院附属瑞金医院 | 靶向血小板表达的凝血因子Xa及其应用 |
Family Cites Families (21)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| ATE177752T1 (de) | 1992-12-15 | 1999-04-15 | Corvas Int Inc | Neue inhibitoren von faktor xa |
| CN100553678C (zh) | 1999-02-22 | 2009-10-28 | 巴克斯特国际有限公司 | 新的无白蛋白的因子ⅷ制剂 |
| US6586574B1 (en) * | 1999-08-17 | 2003-07-01 | Nn A/S | Stabilization of freeze-dried cake |
| ES2254385T3 (es) | 2000-02-29 | 2006-06-16 | Millennium Pharmaceuticals, Inc. | Benzamidas e inhibidores relacionados del factor xa. |
| US6586584B2 (en) * | 2001-01-29 | 2003-07-01 | Becton, Dickinson And Company | Sequences and methods for detection of Hepatitis C virus |
| CA2512680A1 (en) * | 2003-01-08 | 2004-07-29 | Chiron Corporation | Stabilized lyophilized compositions comprising tissue factor pathway inhibitor or tissue factor pathway inhibitor variants |
| ATE549317T1 (de) | 2005-11-08 | 2012-03-15 | Millennium Pharm Inc | Pharmazeutische salze und polymorphe aus n-(5- chloro-2-pyridinyl)-2-ää4- ä(dimethylamino)iminomethylübenzoylüaminoü-5- methoxy-benzamid, einem faktor-xa-hemmer |
| JO3324B1 (ar) * | 2006-04-21 | 2019-03-13 | Amgen Inc | مركبات علاجية مجففة بالتبريد تتعلق بالعصارة الهضمية |
| DK2915564T3 (da) * | 2007-09-28 | 2021-02-08 | Alexion Pharma Inc | Antidoter mod faktor XA-inhibitorer og fremgangsmåder til anvendelse deraf |
| CN107050437A (zh) | 2008-09-03 | 2017-08-18 | 奥克塔法马股份有限公司 | 重组制备的因子viii的新型保护组合物 |
| JP5709316B2 (ja) | 2008-11-14 | 2015-04-30 | ポートラ ファーマシューティカルズ， インコーポレイテッド | 第Ｘａ因子阻害剤のための解毒剤および血液凝固剤と組み合わせて該解毒剤を使用する方法 |
| WO2010117729A1 (en) | 2009-03-30 | 2010-10-14 | Portola Pharmaceuticals, Inc. | Antidotes for factor xa inhibitors and methods of using the same |
| EP2453910B1 (en) | 2009-07-15 | 2016-08-31 | Portola Pharmaceuticals, Inc. | Unit dose formulation of antidote for factor xa inhibitors for use in preventing bleeding |
| US20120121580A1 (en) * | 2009-07-28 | 2012-05-17 | Merck Sharp & Dohme Corp. | Methods for producing high concentration lyophilized pharmaceutical formulations |
| US20130165459A1 (en) * | 2010-01-12 | 2013-06-27 | Norvartis Pharma Ag | Pharmaceutical composition and dosage forms of elinogrel and methods of use thereof |
| KR102049254B1 (ko) * | 2010-04-20 | 2019-11-28 | 옥타파마 아게 | 약학 단백질을 위한 신규한 안정화제 |
| US8987285B2 (en) * | 2010-12-03 | 2015-03-24 | Portola Pharmaceuticals, Inc. | Pharmaceutical compositions, dosage forms and new forms of the compound of formula (I), and methods of use thereof |
| US9683020B2 (en) * | 2011-08-01 | 2017-06-20 | Emory University | VLPS containing ligands and methods related thereto |
| AU2012315516B2 (en) * | 2011-09-30 | 2017-05-04 | The Children's Hospital Of Philadelphia | Compositions and methods for modulating hemostasis |
| GB201310946D0 (en) * | 2013-06-19 | 2013-07-31 | Cambridge Entpr Ltd | Antidote |
| CA2961739C (en) * | 2014-08-20 | 2024-04-30 | Portola Pharmaceuticals, Inc. | Lyophilized formulations for factor xa antidote |
-
2015
- 2015-08-20 CA CA2961739A patent/CA2961739C/en active Active
- 2015-08-20 AU AU2015305413A patent/AU2015305413B2/en active Active
- 2015-08-20 CN CN201580048166.3A patent/CN107073082B/zh active Active
- 2015-08-20 SG SG11201701247RA patent/SG11201701247RA/en unknown
- 2015-08-20 EP EP15834421.8A patent/EP3182993B1/en active Active
- 2015-08-20 KR KR1020227045749A patent/KR102867491B1/ko active Active
- 2015-08-20 EP EP20170763.5A patent/EP3750556A1/en active Pending
- 2015-08-20 EA EA202091385A patent/EA202091385A3/ru unknown
- 2015-08-20 DK DK15834421.8T patent/DK3182993T3/da active
- 2015-08-20 KR KR1020177007503A patent/KR102482517B1/ko active Active
- 2015-08-20 CN CN202110363277.0A patent/CN113171447B/zh active Active
- 2015-08-20 KR KR1020257032508A patent/KR20250150675A/ko active Pending
- 2015-08-20 JP JP2017509739A patent/JP6742986B2/ja active Active
- 2015-08-20 WO PCT/US2015/046173 patent/WO2016029061A1/en not_active Ceased
- 2015-08-20 EA EA201790415A patent/EA036091B1/ru unknown
- 2015-08-20 ES ES15834421T patent/ES2814157T3/es active Active
-
2016
- 2016-04-22 US US15/136,810 patent/US20160237420A1/en not_active Abandoned
-
2017
- 2017-02-02 IL IL250413A patent/IL250413B/en active IP Right Grant
- 2017-03-10 ZA ZA2017/01764A patent/ZA201701764B/en unknown
- 2017-11-21 US US15/820,265 patent/US20180320160A1/en not_active Abandoned
-
2019
- 2019-09-12 JP JP2019165981A patent/JP2019206595A/ja not_active Withdrawn
-
2020
- 2020-06-08 US US16/895,448 patent/US11028382B2/en active Active
- 2020-06-08 US US16/895,443 patent/US20200299667A1/en not_active Abandoned
- 2020-08-26 IL IL276960A patent/IL276960B/en unknown
- 2020-12-16 AU AU2020289768A patent/AU2020289768B2/en active Active
-
2021
- 2021-05-28 US US17/334,427 patent/US20210284986A1/en not_active Abandoned
- 2021-10-22 JP JP2021172975A patent/JP7416549B2/ja active Active
-
2023
- 2023-09-11 JP JP2023146769A patent/JP2023158199A/ja active Pending
-
2024
- 2024-09-13 AU AU2024219698A patent/AU2024219698A1/en active Pending
- 2024-11-05 US US18/937,646 patent/US20250163399A1/en active Pending
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