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1. 发明申请

WO2013116366A1 NON-ANTICOAGULANT SULFATED OR SULFONATED POLYSACCHARIDES 审中-公开
标题翻译：非抗血清磺化或磺化多糖
公开(公告)号：WO2013116366A1
公开(公告)日：2013-08-08
申请号：PCT/US2013/023892
申请日：2013-01-30
申请人： BAXTER INTERNATIONAL INC. , BAXTER HEALTHCARE S.A. , DOCKAL, Michael , SCHEIFLINGER, Fritz , KNAPPE, Sabine , TILL, Susanne , HAI, Ton , SANDERS, Paul , DANDE, Prasad , JIANG, Cong
发明人： DOCKAL, Michael , SCHEIFLINGER, Fritz , KNAPPE, Sabine , TILL, Susanne , HAI, Ton , SANDERS, Paul , DANDE, Prasad , JIANG, Cong
IPC分类号： A61K31/715 , A61P7/04
CPC分类号： A61K31/737 , A61K31/715 , A61K45/06 , C07H5/10 , C08B37/0012 , A61K2300/00
摘要： The present invention provides non-anticoagulant sulfated or sulfonated polysaccharides (NASPs), which accelerate the blood clotting process. Also provided are pharmaceutical formulations comprising a NASP of the invention in conjunction with a pharmaceutically acceptable excipient and, in various embodiments, these formulations are unit dosage formulations. The invention provides a NASP formulation, which is orally bioavailable. Also provided are methods for utilizing the compounds and formulations of the invention to promote blood clotting in vivo as therapeutic and prophylactic agents and in vitro as an aid to studies of the blood clotting process.
摘要翻译：本发明提供非抗凝血剂硫酸化或磺化多糖（NASP），其加速凝血过程。还提供了包含本发明的NASP与药学上可接受的赋形剂的药物制剂，并且在各种实施方案中，这些制剂是单位剂量制剂。本发明提供了口服生物可利用的NASP制剂。还提供了利用本发明的化合物和制剂在体内促进血液凝固作为治疗和预防剂的方法，并且在体外作为血液凝固过程的研究的辅助。

2. 发明申请

WO2009137256A1 BIOLOGICALLY ACTIVE PEPTIDES 审中-公开
标题翻译：生物活性肽
公开(公告)号：WO2009137256A1
公开(公告)日：2009-11-12
申请号：PCT/US2009/040857
申请日：2009-04-16
申请人： BAXTER INTERNATIONAL INC. , BAXTER HEALTHCARE S.A. , SCHEIFLINGER, Friedrich , DOCKAL, Michael
发明人： SCHEIFLINGER, Friedrich , DOCKAL, Michael
IPC分类号： C07K7/06 , C07K7/08
CPC分类号： C07K7/06 , A61K38/00 , C07K1/04 , C07K7/08 , C07K14/755 , Y02P20/55
摘要： A peptide or peptide derivative comprising: (i) WDLYFEIVW (SEQ ID NO: 1 ); or (ii) a variant amino acid sequence comprising one, two, three or four L-amino acid substitutions in WDLYFEIVW (SEQ ID NO: 1 ); or (iii) the retro-inverso variant of the peptide or peptide derivative of either one of parts (i) and (ii), wherein said peptide or peptide derivative has procoagulant activity. A peptide or peptide derivative comprising: (i) an amino acid sequence comprising imfwydcye; or (ii) a variant amino acid sequence comprising one, two, three, four, five or six amino acid substitutions in imfwydcye, wherein said peptide or peptide derivative has procoagulant activity.
摘要翻译：一种肽或肽衍生物，其包含：（i）WDLYFEIVW（SEQ ID NO：1）; 或（ii）在WDLYFEIVW（SEQ ID NO：1）中包含一个，两个，三个或四个L-氨基酸取代的变体氨基酸序列; 或（iii）部分（i）和（ii）中任一项的肽或肽衍生物的逆转型变体，其中所述肽或肽衍生物具有促凝活性。一种肽或肽衍生物，其包含：（i）包含成纤维细胞的氨基酸序列; 或（ii）在成纤维细胞中包含一个，两个，三个，四个，五个或六个氨基酸取代的变体氨基酸序列，其中所述肽或肽衍生物具有促凝活性。

3. 发明申请

WO2011115712A8 TFPI INHIBITORS AND METHODS OF USE 审中-公开
标题翻译： TFPI抑制剂及其使用方法
公开(公告)号：WO2011115712A8
公开(公告)日：2013-10-10
申请号：PCT/US2011024604
申请日：2011-02-11
申请人： BAXTER INT , BAXTER HEALTHCARE SA , DOCKAL MICHAEL , HARTMANN RUDOLF , FRIES MARKUS , SCHEIFLINGER FRIEDRICH , EHRLICH HARTMUT , REINEKE ULRICH , OSTERKAMP FRANK , POLAKOWSKI THOMAS
发明人： DOCKAL MICHAEL , HARTMANN RUDOLF , FRIES MARKUS , SCHEIFLINGER FRIEDRICH , EHRLICH HARTMUT , REINEKE ULRICH , OSTERKAMP FRANK , POLAKOWSKI THOMAS
IPC分类号： A61K38/18 , A61K38/16 , C40B40/10
CPC分类号： A61K38/10 , A61K38/00 , A61K2121/00 , C07K1/14 , C07K7/08 , C07K14/00 , C07K14/8114 , G01N33/68 , G01N2333/745 , G01N2333/8114 , G01N2333/96444 , G01N2333/96447 , G01N2500/02 , G01N2500/04 , G01N2500/20 , G06F19/16 , G06F19/18
摘要： The invention provides peptides that bind Tissue Factor Pathway Inhibitor (TFPI), including TFPI-inhibitory peptides, and compositions thereof. The peptides may be used to inhibit a TFPI, enhance thrombin formation in a clotting factor-deficient subject, increase blood clot formation in a subject, treat a blood coagulation disorder in a subject, purify TFPI, and identify a TFPI-binding compound.
摘要翻译：本发明提供了结合组织因子途径抑制剂（TFPI）（包括TFPI抑制肽）及其组合物的肽。肽可以用于抑制TFPI，增强凝血因子缺陷的受试者中的凝血酶形成，增加受试者的血块形成，治疗受试者的血液凝固障碍，纯化TFPI和鉴定TFPI结合化合物。

4. 发明申请

WO2011115712A3 TFPI INHIBITORS AND METHODS OF USE 审中-公开
标题翻译： TFPI抑制剂和使用方法
公开(公告)号：WO2011115712A3
公开(公告)日：2011-11-24
申请号：PCT/US2011024604
申请日：2011-02-11
申请人： BAXTER INT , BAXTER HEAL THCARE S A , DOCKAL MICHAEL , HARTMANN RUDOLF , FRIES MARKUS , SCHEIFLINGER FRIEDRICH , EHRLICH HARTMUT , REINEKE ULRICH , OSTERKAMP FRANK , POLAKOWSKI THOMAS
发明人： DOCKAL MICHAEL , HARTMANN RUDOLF , FRIES MARKUS , SCHEIFLINGER FRIEDRICH , EHRLICH HARTMUT , REINEKE ULRICH , OSTERKAMP FRANK , POLAKOWSKI THOMAS
IPC分类号： A61K38/18 , A61K38/16 , C40B40/10
CPC分类号： A61K38/10 , A61K38/00 , A61K2121/00 , C07K1/14 , C07K7/08 , C07K14/00 , C07K14/8114 , G01N33/68 , G01N2333/745 , G01N2333/8114 , G01N2333/96444 , G01N2333/96447 , G01N2500/02 , G01N2500/04 , G01N2500/20 , G06F19/16 , G06F19/18
摘要： The invention provides peptides that bind Tissue Factor Pathway Inhibitor (TFPI), including TFPI-inhibitory peptides, and compositions thereof. The peptides may be used to inhibit a TFPI, enhance thrombin formation in a clotting factor-deficient subject, increase blood clot formation in a subject, treat a blood coagulation disorder in a subject, purify TFPI, and identify a TFPI-binding compound.
摘要翻译：本发明提供了结合组织因子途径抑制剂（TFPI）的肽，包括TFPI抑制肽及其组合物。所述肽可用于抑制TFPI，增强凝血因子缺陷受试者中的凝血酶形成，增加受试者的血块形成，治疗受试者中的凝血障碍，纯化TFPI并鉴定TFPI结合化合物。

5. 发明申请

WO2010071894A3 TFPI INHIBITORS AND METHODS OF USE 审中-公开
公开(公告)号：WO2010071894A3
公开(公告)日：2010-06-24
申请号：PCT/US2009/069060
申请日：2009-12-21
申请人： BAXTER INTERNATIONAL INC. , BAXTER HEALTHCARE S.A. , 3B PHARMACEUTICALS GMBH , COSMIX MOLECULAR BIOLOGICALS GMBH , DOCKAL, Michael , EHRLICH, Hartmut , SCHEIFLINGER, Friedrich , REIMER, Ulf , REINEKE, Ulrich , POLAKOWSKI, Thomas , SCHNEIDER, Eberhard
发明人： DOCKAL, Michael , EHRLICH, Hartmut , SCHEIFLINGER, Friedrich , REIMER, Ulf , REINEKE, Ulrich , POLAKOWSKI, Thomas , SCHNEIDER, Eberhard
IPC分类号： A61K38/00
摘要： The invention provides peptides that bind Tissue Factor Pathway Inhibitor (TFPI), including TFPI-inhibitory peptides, and compositions thereof. The peptides may be used to inhibit a TFPI, enhance thrombin formation in a clotting factor-deficient subject, increase blood clot formation in a subject, and/or treat a blood coagulation disorder in a subject.

6. 发明申请

WO2013116383A1 NON-ANTICOAGULANT SULFATED OR SULFONATED SYNTHETIC POLYMERS 审中-公开
标题翻译：非抗坏血酸硫化或磺化合成聚合物
公开(公告)号：WO2013116383A1
公开(公告)日：2013-08-08
申请号：PCT/US2013/023919
申请日：2013-01-30
申请人： BAXTER INTERNATIONAL INC. , BAXTER HEALTHCARE S.A. , DOCKAL, Michael , SCHEIFLINGER, Fritz , KNAPPE, Sabine , TILL, Susanne , HAI, Ton , SANDERS, Paul
发明人： DOCKAL, Michael , SCHEIFLINGER, Fritz , KNAPPE, Sabine , TILL, Susanne , HAI, Ton , SANDERS, Paul
IPC分类号： A61K31/795 , A61P7/04
CPC分类号： A61K31/795 , A61K31/37 , A61K31/7024 , A61K31/727 , A61K38/37 , A61K38/4846 , A61K2300/00
摘要： The present invention provides pharmaceutical formulations including a non-anticoagulant, non-saccharide polymer that with at least one sulfate or sulfonate moiety. The pharmaceutical formulations of the invention are of use to improve blood clotting in a subject. Also provided are useful analytical methods utilizing these polymers to query the dynamics of blood clotting in vitro.
摘要翻译：本发明提供药物制剂，其包含与至少一种硫酸盐或磺酸盐部分的非抗凝血剂，非糖类聚合物。本发明的药物制剂可用于改善受试者的血液凝固。还提供了使用这些聚合物来查询体外血液凝固动力学的有用的分析方法。

7. 发明申请

WO2010071894A2 TFPI INHIBITORS AND METHODS OF USE 审中-公开
标题翻译： TFPI抑制剂及其使用方法
公开(公告)号：WO2010071894A2
公开(公告)日：2010-06-24
申请号：PCT/US2009069060
申请日：2009-12-21
申请人： BAXTER INT , BAXTER HEALTHCARE SA , 3B PHARMACEUTICALS GMBH , COSMIX MOLECULAR BIOLOG GMBH , DOCKAL MICHAEL , EHRLICH HARTMUT , SCHEIFLINGER FRIEDRICH , REIMER ULF , REINEKE ULRICH , POLAKOWSKI THOMAS , SCHNEIDER EBERHARD
发明人： DOCKAL MICHAEL , EHRLICH HARTMUT , SCHEIFLINGER FRIEDRICH , REIMER ULF , REINEKE ULRICH , POLAKOWSKI THOMAS , SCHNEIDER EBERHARD
IPC分类号： A61K38/10 , A61P7/02 , C07K7/08
CPC分类号： C07K14/4703 , A61K38/00 , A61K47/551 , A61K47/557 , A61K47/60 , C07K7/08 , C07K14/001
摘要： The invention provides peptides that bind Tissue Factor Pathway Inhibitor (TFPI), including TFPI-inhibitory peptides, and compositions thereof. The peptides may be used to inhibit a TFPI, enhance thrombin formation in a clotting factor-deficient subject, increase blood clot formation in a subject, and/or treat a blood coagulation disorder in a subject.
摘要翻译：本发明提供了结合组织因子途径抑制剂（TFPI）（包括TFPI抑制肽）及其组合物的肽。肽可以用于抑制TFPI，增强凝血因子缺陷受试者中的凝血酶形成，增加受试者中的血块形成和/或治疗受试者的血液凝固障碍。

8. 发明申请

WO2010066869A3 PREPARATIONS BASED ON FIBRINOGEN AND SULFATED POLYSACCHARIDES 审中-公开
公开(公告)号：WO2010066869A3
公开(公告)日：2010-06-17
申请号：PCT/EP2009/066897
申请日：2009-12-11
申请人： BAXTER INTERNATIONAL INC. , BAXTER HEALTHCARE S.A. , DOCKAL, Michael , SCHEIFLINGER, Friedrich , HEDRICH, Hans Christian , TSCHETSCHKOWITSCH, Klaus
发明人： DOCKAL, Michael , SCHEIFLINGER, Friedrich , HEDRICH, Hans Christian , TSCHETSCHKOWITSCH, Klaus
IPC分类号： A61L26/00 , A61L24/04
摘要： The present invention provides a preparation comprising fibrinogen and a sulfated polysaccharide as a one component composition or as a kit of parts comprising fibrinogen and sulfated polysaccharide as separated components. The present invention further provides a fibrin clot like structure obtainable by a defined process, a hemostatic patch, a two-component syringe system and various uses of the described preparations, fibrin clot like structures and patches.

9. 发明申请

US20110206655A1 FVIII-INDEPENDENT FIX-MUTANT PROTEINS FOR HEMOPHILIA A TREATMENT 有权
标题翻译：用于HEMOPHILIA治疗的FVIII独立固定蛋白
公开(公告)号：US20110206655A1
公开(公告)日：2011-08-25
申请号：US13096894
申请日：2011-04-28
申请人： Dockal Michael , Hartmann Rudolf , Scheiflinger Friedrich
发明人： Dockal Michael , Hartmann Rudolf , Scheiflinger Friedrich
IPC分类号： A61K38/48 , C12N9/50 , C07H21/00 , C12N15/63 , C12N5/10 , A61P7/04 , A61P7/00
CPC分类号： C12N9/644 , A61K38/00 , C12Y304/21022
摘要： The present invention relates to recombinant blood coagulation factor IX (rFIX) mutants having factor VIII (FVIII) independent factor X (FX) activation potential. Five full length FIX proteins with combinations of mutations of amino acids important for functional activity of FIX and FIX wild type were cloned and expressed in HEK 293 cells. The proteins were tested by an activated partial thromboplastin time (aPTT) assay in FVIII-depleted plasma as well as in FVIII-inhibited patient plasma. In FVIII-depleted plasma functional activity of the FIX mutants was calculated as increased FVIII equivalent activity. The mutant proteins had increased FVIII equivalent activity. In FVIII-inhibited patient plasma the FEIBA equivalent activity was calculated for analysis of FVIII independent FX activation potential. The proteins had also increased FEIBA equivalent activity. Furthermore, the pre-activated FIX proteins had an increased activity in FIX-depleted plasma containing FVIII inhibitors. Therefore these FIX mutants are alternatives as bypassing agents for treatment of FVIII inhibitor patients.
摘要翻译：本发明涉及具有因子VIII（FVIII）独立因子X（FX）活化电位的重组凝血因子IX（rFIX）突变体。在HEK 293细胞中克隆并表达具有FIX和FIX野生型功能活性重要的氨基酸突变组合的五个全长FIX蛋白。通过在FVIII消除的血浆以及FVIII抑制的患者血浆中的活化部分凝血活酶时间（aPTT）测定来测试蛋白质。在FVIII消耗的血浆中，FIX突变体的功能活性被计算为增加的FVIII当量活性。突变蛋白具有增加的FVIII当量活性。在FVIII抑制的患者血浆中，计算FEIBA等效活性以分析FVIII独立的FX激活电位。蛋白质也增加了FEIBA等效活性。此外，预活化的FIX蛋白在含有FVIII抑制剂的FIX耗尽血浆中具有增加的活性。因此，这些FIX突变体是用于治疗FVIII抑制剂患者的旁路药物的替代物。

10. 发明申请

WO2011115712A2 TFPI INHIBITORS AND METHODS OF USE 审中-公开
标题翻译： TFPI抑制剂及其使用方法
公开(公告)号：WO2011115712A2
公开(公告)日：2011-09-22
申请号：PCT/US2011/024604
申请日：2011-02-11
申请人： BAXTER INTERNATIONAL INC , BAXTER HEAL THCARE S.A. , 3B PHARMACEUTICALS GMBH , DOCKAL, Michael , HARTMANN, Rudolf , FRIES, Markus , SCHEIFLINGER, Friedrich , EHRLICH, Hartmut , REINEKE, Ulrich , OSTERKAMP, Frank , POLAKOWSKI, Thomas
发明人： DOCKAL, Michael , HARTMANN, Rudolf , FRIES, Markus , SCHEIFLINGER, Friedrich , EHRLICH, Hartmut , REINEKE, Ulrich , OSTERKAMP, Frank , POLAKOWSKI, Thomas
IPC分类号： A61K38/18
CPC分类号： A61K38/10 , A61K38/00 , A61K2121/00 , C07K1/14 , C07K7/08 , C07K14/00 , C07K14/8114 , G01N33/68 , G01N2333/745 , G01N2333/8114 , G01N2333/96444 , G01N2333/96447 , G01N2500/02 , G01N2500/04 , G01N2500/20 , G06F19/16 , G06F19/18
摘要： The invention provides peptides that bind Tissue Factor Pathway Inhibitor (TFPI), including TFPI-inhibitory peptides, and compositions thereof. The peptides may be used to inhibit a TFPI, enhance thrombin formation in a clotting factor-deficient subject, increase blood clot formation in a subject, treat a blood coagulation disorder in a subject, purify TFPI, and identify a TFPI-binding compound.
摘要翻译：本发明提供了结合组织因子途径抑制剂（TFPI），包括TFPI抑制肽的肽及其组合物。肽可以用于抑制TFPI，增强凝血因子缺陷受试者中的凝血酶形成，增加受试者中的血块形成，治疗受试者的血液凝固障碍，纯化TFPI和鉴定TFPI结合化合物。

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