JP2012512645A5 - - Google Patents
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- JP2012512645A5 JP2012512645A5 JP2011541497A JP2011541497A JP2012512645A5 JP 2012512645 A5 JP2012512645 A5 JP 2012512645A5 JP 2011541497 A JP2011541497 A JP 2011541497A JP 2011541497 A JP2011541497 A JP 2011541497A JP 2012512645 A5 JP2012512645 A5 JP 2012512645A5
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- JP
- Japan
- Prior art keywords
- seq
- factor
- protein
- replaced
- derivative
- 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.)
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- 108010014173 Factor X Proteins 0.000 claims 10
- 229920001184 polypeptide Polymers 0.000 claims 9
- 108090000765 processed proteins & peptides Proteins 0.000 claims 9
- 102000004196 processed proteins & peptides Human genes 0.000 claims 9
- 150000001413 amino acids Chemical group 0.000 claims 8
- 108090000190 Thrombin Proteins 0.000 claims 7
- 235000004279 alanine Nutrition 0.000 claims 7
- 229960004072 thrombin Drugs 0.000 claims 7
- DHMQDGOQFOQNFH-UHFFFAOYSA-N Glycine Chemical compound NCC(O)=O DHMQDGOQFOQNFH-UHFFFAOYSA-N 0.000 claims 6
- QNAYBMKLOCPYGJ-REOHCLBHSA-N L-alanine Chemical compound C[C@H](N)C(O)=O QNAYBMKLOCPYGJ-REOHCLBHSA-N 0.000 claims 6
- 108020001507 fusion proteins Proteins 0.000 claims 6
- 102000037865 fusion proteins Human genes 0.000 claims 6
- DCXYFEDJOCDNAF-UHFFFAOYSA-N Asparagine Natural products OC(=O)C(N)CC(N)=O DCXYFEDJOCDNAF-UHFFFAOYSA-N 0.000 claims 5
- KZSNJWFQEVHDMF-BYPYZUCNSA-N L-valine Chemical compound CC(C)[C@H](N)C(O)=O KZSNJWFQEVHDMF-BYPYZUCNSA-N 0.000 claims 5
- 101800004937 Protein C Proteins 0.000 claims 5
- 101800001700 Saposin-D Proteins 0.000 claims 5
- 102400000827 Saposin-D Human genes 0.000 claims 5
- KZSNJWFQEVHDMF-UHFFFAOYSA-N Valine Natural products CC(C)C(N)C(O)=O KZSNJWFQEVHDMF-UHFFFAOYSA-N 0.000 claims 5
- 229960001230 asparagine Drugs 0.000 claims 5
- 235000009582 asparagine Nutrition 0.000 claims 5
- 230000002265 prevention Effects 0.000 claims 5
- 229960000856 protein c Drugs 0.000 claims 5
- 235000018102 proteins Nutrition 0.000 claims 5
- 102000004169 proteins and genes Human genes 0.000 claims 5
- 108090000623 proteins and genes Proteins 0.000 claims 5
- 239000004474 valine Substances 0.000 claims 5
- FWMNVWWHGCHHJJ-SKKKGAJSSA-N 4-amino-1-[(2r)-6-amino-2-[[(2r)-2-[[(2r)-2-[[(2r)-2-amino-3-phenylpropanoyl]amino]-3-phenylpropanoyl]amino]-4-methylpentanoyl]amino]hexanoyl]piperidine-4-carboxylic acid Chemical compound C([C@H](C(=O)N[C@H](CC(C)C)C(=O)N[C@H](CCCCN)C(=O)N1CCC(N)(CC1)C(O)=O)NC(=O)[C@H](N)CC=1C=CC=CC=1)C1=CC=CC=C1 FWMNVWWHGCHHJJ-SKKKGAJSSA-N 0.000 claims 4
- COLNVLDHVKWLRT-QMMMGPOBSA-N L-phenylalanine Chemical compound OC(=O)[C@@H](N)CC1=CC=CC=C1 COLNVLDHVKWLRT-QMMMGPOBSA-N 0.000 claims 4
- 230000004988 N-glycosylation Effects 0.000 claims 4
- COLNVLDHVKWLRT-UHFFFAOYSA-N phenylalanine Natural products OC(=O)C(N)CC1=CC=CC=C1 COLNVLDHVKWLRT-UHFFFAOYSA-N 0.000 claims 4
- 239000004471 Glycine Substances 0.000 claims 3
- DCXYFEDJOCDNAF-REOHCLBHSA-N L-asparagine Chemical compound OC(=O)[C@@H](N)CC(N)=O DCXYFEDJOCDNAF-REOHCLBHSA-N 0.000 claims 3
- MTCFGRXMJLQNBG-UHFFFAOYSA-N Serine Natural products OCC(N)C(O)=O MTCFGRXMJLQNBG-UHFFFAOYSA-N 0.000 claims 3
- MTCFGRXMJLQNBG-REOHCLBHSA-N (2S)-2-Amino-3-hydroxypropansäure Chemical compound OC[C@H](N)C(O)=O MTCFGRXMJLQNBG-REOHCLBHSA-N 0.000 claims 2
- 101800001401 Activation peptide Proteins 0.000 claims 2
- 102400000069 Activation peptide Human genes 0.000 claims 2
- 108010074860 Factor Xa Proteins 0.000 claims 2
- 208000032843 Hemorrhage Diseases 0.000 claims 2
- AGPKZVBTJJNPAG-WHFBIAKZSA-N L-isoleucine Chemical compound CC[C@H](C)[C@H](N)C(O)=O AGPKZVBTJJNPAG-WHFBIAKZSA-N 0.000 claims 2
- ROHFNLRQFUQHCH-YFKPBYRVSA-N L-leucine Chemical compound CC(C)C[C@H](N)C(O)=O ROHFNLRQFUQHCH-YFKPBYRVSA-N 0.000 claims 2
- ROHFNLRQFUQHCH-UHFFFAOYSA-N Leucine Natural products CC(C)CC(N)C(O)=O ROHFNLRQFUQHCH-UHFFFAOYSA-N 0.000 claims 2
- ONIBWKKTOPOVIA-UHFFFAOYSA-N Proline Natural products OC(=O)C1CCCN1 ONIBWKKTOPOVIA-UHFFFAOYSA-N 0.000 claims 2
- 125000000613 asparagine group Chemical group N[C@@H](CC(N)=O)C(=O)* 0.000 claims 2
- 208000034158 bleeding Diseases 0.000 claims 2
- 229960000310 isoleucine Drugs 0.000 claims 2
- AGPKZVBTJJNPAG-UHFFFAOYSA-N isoleucine Natural products CCC(C)C(N)C(O)=O AGPKZVBTJJNPAG-UHFFFAOYSA-N 0.000 claims 2
- 239000003055 low molecular weight heparin Substances 0.000 claims 2
- 229940127215 low-molecular weight heparin Drugs 0.000 claims 2
- 239000004475 Arginine Substances 0.000 claims 1
- 102100022641 Coagulation factor IX Human genes 0.000 claims 1
- 102100026735 Coagulation factor VIII Human genes 0.000 claims 1
- 201000003542 Factor VIII deficiency Diseases 0.000 claims 1
- 208000009292 Hemophilia A Diseases 0.000 claims 1
- 101000911390 Homo sapiens Coagulation factor VIII Proteins 0.000 claims 1
- 206010020608 Hypercoagulation Diseases 0.000 claims 1
- CKLJMWTZIZZHCS-REOHCLBHSA-N L-aspartic acid Chemical compound OC(=O)[C@@H](N)CC(O)=O CKLJMWTZIZZHCS-REOHCLBHSA-N 0.000 claims 1
- KDXKERNSBIXSRK-UHFFFAOYSA-N Lysine Natural products NCCCCC(N)C(O)=O KDXKERNSBIXSRK-UHFFFAOYSA-N 0.000 claims 1
- 239000004472 Lysine Substances 0.000 claims 1
- 208000007536 Thrombosis Diseases 0.000 claims 1
- 125000003295 alanine group Chemical group N[C@@H](C)C(=O)* 0.000 claims 1
- 239000003146 anticoagulant agent Substances 0.000 claims 1
- 229940127219 anticoagulant drug Drugs 0.000 claims 1
- ODKSFYDXXFIFQN-UHFFFAOYSA-N arginine Natural products OC(=O)C(N)CCCNC(N)=N ODKSFYDXXFIFQN-UHFFFAOYSA-N 0.000 claims 1
- 229940009098 aspartate Drugs 0.000 claims 1
- 230000000740 bleeding effect Effects 0.000 claims 1
- 201000010099 disease Diseases 0.000 claims 1
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims 1
- 208000009429 hemophilia B Diseases 0.000 claims 1
- 230000003027 hypercoagulation Effects 0.000 claims 1
- 238000000034 method Methods 0.000 claims 1
- 102000039446 nucleic acids Human genes 0.000 claims 1
- 108020004707 nucleic acids Proteins 0.000 claims 1
- 150000007523 nucleic acids Chemical class 0.000 claims 1
- 230000008685 targeting Effects 0.000 claims 1
Applications Claiming Priority (7)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| EP08305990.7 | 2008-12-19 | ||
| EP08305990A EP2199387A1 (en) | 2008-12-19 | 2008-12-19 | Serine protease derivatives and uses for the prevention and/or the treatment of blood coagulation disorders |
| EP09305349.4 | 2009-04-23 | ||
| EP09305349 | 2009-04-23 | ||
| US22296009P | 2009-07-03 | 2009-07-03 | |
| US61/222960 | 2009-07-03 | ||
| PCT/EP2009/067632 WO2010070137A1 (en) | 2008-12-19 | 2009-12-21 | Serine protease derivatives and uses in the prevention or the treatment of blood coagulation disorders |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2012512645A JP2012512645A (ja) | 2012-06-07 |
| JP2012512645A5 true JP2012512645A5 (enExample) | 2013-02-14 |
| JP5833448B2 JP5833448B2 (ja) | 2015-12-16 |
Family
ID=41718355
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2011541497A Expired - Fee Related JP5833448B2 (ja) | 2008-12-19 | 2009-12-21 | セリンプロテアーゼ誘導体および血液凝固疾患の予防または処置における使用 |
Country Status (9)
| Country | Link |
|---|---|
| US (3) | US8436144B2 (enExample) |
| EP (1) | EP2358874B1 (enExample) |
| JP (1) | JP5833448B2 (enExample) |
| KR (1) | KR20110114587A (enExample) |
| CN (2) | CN104262479A (enExample) |
| AU (1) | AU2009329493B2 (enExample) |
| CA (1) | CA2747065A1 (enExample) |
| ES (1) | ES2629099T3 (enExample) |
| WO (1) | WO2010070137A1 (enExample) |
Families Citing this family (14)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| MX336958B (es) * | 2005-11-15 | 2016-02-05 | Philadelphia Children Hospital | Metodos y composiciones para modular la hemostasia. |
| KR102069498B1 (ko) | 2007-09-28 | 2020-01-23 | 포톨라 파마슈티컬스, 인코포레이티드 | 인자 Ｘａ 저해제에 대한 안티도트 및 그것을 사용하는 방법 |
| CA2743496C (en) | 2008-11-14 | 2018-03-27 | Portola Pharmaceuticals, Inc. | Antidotes for factor xa inhibitors and methods of using the same in combination with blood coagulating agents |
| JP5833448B2 (ja) * | 2008-12-19 | 2015-12-16 | アンスティチュ ナショナル ドゥ ラ サンテ エ ドゥ ラ ルシェルシュ メディカル | セリンプロテアーゼ誘導体および血液凝固疾患の予防または処置における使用 |
| PL3604510T3 (pl) | 2009-03-30 | 2025-07-28 | Alexion Pharmaceuticals, Inc. | Antidota na inhibitory czynnika xa i sposoby ich stosowania |
| 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 |
| JP6514893B2 (ja) * | 2011-09-30 | 2019-05-15 | ザ・チルドレンズ・ホスピタル・オブ・フィラデルフィアＴｈｅ Ｃｈｉｌｄｒｅｎ’Ｓ Ｈｏｓｐｉｔａｌ Ｏｆ Ｐｈｉｌａｄｅｌｐｈｉａ | 止血を調節するための組成物および方法 |
| KR102049900B1 (ko) | 2012-07-25 | 2019-11-28 | 카탈리스트 바이오사이언시즈, 인코포레이티드 | 변형 인자 x 폴리펩티드 및 이의 용도 |
| HK1215196A1 (zh) | 2013-01-31 | 2016-08-19 | 辉瑞公司 | 用於抵消因子xa抑制的组合物和方法 |
| FR3001729B1 (fr) * | 2013-02-04 | 2015-03-06 | Lab Francais Du Fractionnement | Mutants du facteur x |
| CN105008530A (zh) * | 2013-03-12 | 2015-10-28 | 诺和诺德股份有限公司 | 凝血酶敏感性凝固因子x分子 |
| CN112195169A (zh) | 2013-09-24 | 2021-01-08 | 辉瑞大药厂 | 包含重组人凝血因子Xa蛋白的异质性群体的组合物 |
| US10676730B2 (en) | 2015-01-07 | 2020-06-09 | Inserm (Institut National De La Sante Et De La Recherche Medicale) | Mutated factor X polypeptides and uses thereof for the treatment of haemophilia |
| EP3328998A1 (en) | 2015-07-27 | 2018-06-06 | INSERM (Institut National de la Santé et de la Recherche Médicale) | Mutated factor x polypeptides and uses thereof for the treatment of haemophilia |
Family Cites Families (18)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US4861719A (en) | 1986-04-25 | 1989-08-29 | Fred Hutchinson Cancer Research Center | DNA constructs for retrovirus packaging cell lines |
| US4992373A (en) | 1987-12-04 | 1991-02-12 | Eli Lilly And Company | Vectors and compounds for direct expression of activated human protein C |
| US5278056A (en) | 1988-02-05 | 1994-01-11 | The Trustees Of Columbia University In The City Of New York | Retroviral packaging cell lines and process of using same |
| US4981952A (en) | 1988-10-04 | 1991-01-01 | Eli Lilly And Company | Method for the purification of vitamin K-dependent proteins |
| US5670488A (en) | 1992-12-03 | 1997-09-23 | Genzyme Corporation | Adenovirus vector for gene therapy |
| MY110664A (en) | 1992-05-21 | 1999-01-30 | Lilly Co Eli | Protein c derivatives |
| JP3866760B2 (ja) | 1993-02-22 | 2007-01-10 | ザ ロックフェラー ユニバーシティ | 一過性トランスフェクションによる高力価のヘルパーフリーのレトロウイルスの生産 |
| FR2712812B1 (fr) | 1993-11-23 | 1996-02-09 | Centre Nat Rech Scient | Composition pour la production de produits thérapeutiques in vivo. |
| IL116816A (en) | 1995-01-20 | 2003-05-29 | Rhone Poulenc Rorer Sa | Cell for the production of a defective recombinant adenovirus or an adeno-associated virus and the various uses thereof |
| US6013516A (en) | 1995-10-06 | 2000-01-11 | The Salk Institute For Biological Studies | Vector and method of use for nucleic acid delivery to non-dividing cells |
| FR2831170B1 (fr) * | 2001-10-19 | 2004-03-19 | Inst Nat Sante Rech Med | Proteines c modifiees activables directement par la thrombine |
| FR2841904B1 (fr) * | 2002-07-03 | 2004-08-20 | Inst Nat Sante Rech Med | Analogues de facteurs x clivables par la thrombine |
| EP1651252B1 (en) | 2003-07-08 | 2014-11-26 | The Scripps Research Institute | Activated protein c variants with normal cytoprotective activity but reduced anticoagulant activity |
| EP1769092A4 (en) | 2004-06-29 | 2008-08-06 | Europ Nickel Plc | IMPROVED LIXIVIATION OF BASE METALS |
| RU2396347C2 (ru) * | 2004-08-17 | 2010-08-10 | Ксл Бехринг Гмбх | Модифицированные витамин к-зависимые полипептиды |
| EP1820508A1 (en) * | 2006-02-21 | 2007-08-22 | CSL Behring GmbH | Coagulation factor X polypeptides with modified activation properties |
| CN101765560B (zh) | 2007-08-01 | 2012-09-26 | 陶氏环球技术公司 | 制备层状剥离石墨烯的高效率方法 |
| JP5833448B2 (ja) * | 2008-12-19 | 2015-12-16 | アンスティチュ ナショナル ドゥ ラ サンテ エ ドゥ ラ ルシェルシュ メディカル | セリンプロテアーゼ誘導体および血液凝固疾患の予防または処置における使用 |
-
2009
- 2009-12-21 JP JP2011541497A patent/JP5833448B2/ja not_active Expired - Fee Related
- 2009-12-21 EP EP09796378.9A patent/EP2358874B1/en not_active Not-in-force
- 2009-12-21 WO PCT/EP2009/067632 patent/WO2010070137A1/en not_active Ceased
- 2009-12-21 CN CN201410496015.1A patent/CN104262479A/zh active Pending
- 2009-12-21 CA CA2747065A patent/CA2747065A1/en not_active Abandoned
- 2009-12-21 ES ES09796378.9T patent/ES2629099T3/es active Active
- 2009-12-21 AU AU2009329493A patent/AU2009329493B2/en not_active Ceased
- 2009-12-21 CN CN200980157388.3A patent/CN102325880B/zh not_active Expired - Fee Related
- 2009-12-21 US US13/139,367 patent/US8436144B2/en not_active Expired - Fee Related
- 2009-12-21 KR KR1020117016908A patent/KR20110114587A/ko not_active Ceased
-
2013
- 2013-01-02 US US13/732,465 patent/US8518400B2/en not_active Expired - Fee Related
- 2013-06-04 US US13/909,323 patent/US8741286B2/en not_active Expired - Fee Related
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