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公开(公告)号：US20020037857A1
公开(公告)日：2002-03-28
申请号：US09733645
申请日：2000-12-07
发明人： Joseph Edward Semple , Michael I. Weinhouse , Odile Esther Levy , Edwin L. Madison , Amir P. Tamiz
IPC分类号： A61K038/05 , C07K005/078
CPC分类号： C07K5/06139 , A61K38/00 , C07K5/06026 , C07K5/06069
摘要： Novel compounds having activity as non-covalent inhibitors of urokinase and having activity in reducing or inhibiting blood vessel formation are provided. These compounds have Pi a group having an amidino or guanidino moiety or derivative thereof. These compounds are useful in vitro for monitoring plasminogen activator levels and in vivo in treatment of conditions which are ameliorated by inhibition of or decreased activity of urokinase and in treating pathologic conditions wherein blood vessel formation is related to a pathologic condition.
摘要翻译： 提供了具有作为尿激酶非共价抑制剂的活性并具有减少或抑制血管形成活性的新型化合物。 这些化合物具有具有脒基或胍基部分或其衍生物的基团。 这些化合物在体外可用于监测纤溶酶原激活物水平和体内治疗通过抑制或降低尿激酶活性和改善血管形成与病理状况相关的病理状况而改善的病症。
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公开(公告)号：US06096877A
公开(公告)日：2000-08-01
申请号：US249461
申请日：1999-02-12
申请人： George Phillip Vlasuk , Patrick Eric Hugo Stanssens , Joris Hilda Lieven Messens , Marc Josef Lauwereys , Yves Rene LaRoche , Laurent Stephane Jespers , Yannick Georges Jozef Gansemans , Matthew Moyle , Peter W. Bergum
发明人： George Phillip Vlasuk , Patrick Eric Hugo Stanssens , Joris Hilda Lieven Messens , Marc Josef Lauwereys , Yves Rene LaRoche , Laurent Stephane Jespers , Yannick Georges Jozef Gansemans , Matthew Moyle , Peter W. Bergum
IPC分类号： C12N15/09 , A61K35/56 , A61K38/00 , A61P7/02 , C07K14/81 , C12N9/99 , C12N15/12 , C12N15/19 , C07H21/04
CPC分类号： A61K38/55 , C07K14/811 , C12P21/02 , Y10S530/829
摘要： Proteins which have activity as anticoagulants and/or serine protease inhibitors and have at least one NAP domain and are described. Certain of these proteins have factor Xa inhibitory activity and others have activity as inhibitors of factor VIIa/TF. These proteins can be isolated from natural sources as nematodes, chemically synthesized or made by recombinant methods using various DNA expression systems.
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公开(公告)号：US5883077A
公开(公告)日：1999-03-16
申请号：US168964
申请日：1993-12-15
CPC分类号： C07K5/06078 , C07K5/0207 , A61K38/00
摘要： Novel compounds, their salts and compositions related thereto having activity against mammalian factor Xa are disclosed. The novel compounds include peptide aldehyde analogues having substantial potency and specificity as inhibitors of mammalian factor Xa are further disclosed. The compounds are thought useful as inhibitors of factor xa in vitro or as a therapeutic agent for the prevention and treatment of conditions characterized by abnormal thrombosis in mammals. Intermediates useful for the preparation of the novel compounds are also disclosed.
摘要翻译： 公开了与哺乳动物因子Xa具有活性的新型化合物，其盐和与其相关的组合物。 新化合物包括具有显着效力和特异性的肽醛类似物，作为哺乳动物因子Xa的抑制剂被进一步公开。 这些化合物被认为可用作体外因子xa的抑制剂或作为预防和治疗哺乳动物异常血栓形成特征的治疗剂。 还公开了可用于制备新化合物的中间体。
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公开(公告)号：US5872098A
公开(公告)日：1999-02-16
申请号：US461965
申请日：1995-06-05
申请人： George Phillip Vlasuk , Patrick Eric Hugo Stanssens , Joris Hilda Lieven Messens , Marc Jozef Lauwereys , Yves Rene Laroche , Laurent Stephane Jespers , Yannick Georges Jozef Gansemans , Matthew Moyle , Peter W. Bergum
发明人： George Phillip Vlasuk , Patrick Eric Hugo Stanssens , Joris Hilda Lieven Messens , Marc Jozef Lauwereys , Yves Rene Laroche , Laurent Stephane Jespers , Yannick Georges Jozef Gansemans , Matthew Moyle , Peter W. Bergum
CPC分类号： C07K14/811 , A61K38/00
摘要： Proteins which are potent anticoagulants and have at least one NAP domain and are described. These proteins having anticoagulant activity can be isolated from natural sources such as nematodes, chemically synthesized or made by recombinant methods using various DNA expression systems.
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公开(公告)号：US5843442A
公开(公告)日：1998-12-01
申请号：US453047
申请日：1995-05-30
申请人： Howard R. Soule , Terence K. Brunck
发明人： Howard R. Soule , Terence K. Brunck
IPC分类号： A61K38/00 , C07K16/40 , A61K39/395 , C07K16/00 , C07K16/18
摘要： Coagulation protein antagonists are disclosed, which include monoclonal-type antibodies and related cell lines disclosed for the production of specific, neutralizing antibodies against factors VII and VIIa and the tissue factor/factor VIIa bimolecular complex, which antibodies are useful for the prevention or treatment of thrombotic and related diseases, for immunoaffinity isolation and purification of factors VII and VIIa and the tissue factor/factor VIIa complex, and for determination of factors VII or VIIa and the tissue factor/factors VII or VIIa complex in a biological sample.
摘要翻译： 公开了凝血蛋白拮抗剂，其包括公开用于产生针对因子VII和VIIa的特异性中和抗体和组织因子/因子VIIa双分子复合物的单克隆抗体和相关细胞系，所述抗体可用于预防或治疗 血栓形成和相关疾病，用于免疫亲和分离和纯化因子VII和VIIa和组织因子/因子VIIa复合物，以及用于测定生物样品中因子VII或VIIa和组织因子/因子VII或VIIa复合物。
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公开(公告)号：US5789178A
公开(公告)日：1998-08-04
申请号：US458218
申请日：1995-06-02
申请人： Matthew Moyle , David L. Foster , George P. Vlasuk
发明人： Matthew Moyle , David L. Foster , George P. Vlasuk
CPC分类号： C07K16/18 , C07K14/535 , A61K38/00
摘要： Compositions enriched for Neutrophil Inhibitory Factor which inhibit neutrophil activity including adhesion to vascular endothelial cells are provided. Also provided are recombinant Neutrophil Inhibitory Factors which also which inhibit neutrophil activity. Such compositions may comprise a glycoprotein isolated from nematodes. These compositions and recombinant Neutrophil Inhibitory Factors are useful in the therapy of conditions which involve abnormal or undesired inflammatory responses.
摘要翻译： 提供了富含中性粒细胞抑制因子的组合物，其抑制嗜中性粒细胞活性，包括对血管内皮细胞的粘附。 还提供了也抑制中性粒细胞活性的重组嗜中性粒细胞抑制因子。 这样的组合物可以包含从线虫分离的糖蛋白。 这些组合物和重组嗜中性粒细胞抑制因子可用于治疗涉及异常或不期望的炎性反应的病症。
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7.发明授权Methionine sulfone and s-substituted cysteine sulfone derivatives as enzyme inhibitors 失效甲硫氨酸砜和s取代的半胱氨酸砜衍生物作为酶抑制剂
公开(公告)号：US5681844A
公开(公告)日：1997-10-28
申请号：US234811
申请日：1994-04-28
IPC分类号： A61K38/00 , A61P7/02 , C07K5/06 , C07K5/062 , C07K5/072 , C07K5/078 , A61K31/40 , C07D207/06
CPC分类号： C07K5/0606 , A61K38/00
摘要： This invention relates to compounds which inhibit thrombin or factor Xa. The compounds contain an aldehyde functionality and a methionine sulfone or S-substituted cysteine sulfone residue. The compounds and their pharmaceutical compositions are useful for preventing thrombosis in mammals which are suspected of having a condition characterized by abnormal thrombosis.
摘要翻译： 本发明涉及抑制凝血酶或因子Xa的化合物。 该化合物含有醛官能团和甲硫氨酸砜或S-取代的半胱氨酸砜残基。 化合物及其药物组合物可用于预防怀疑具有以异常血栓形成为特征的病症的哺乳动物的血栓形成。
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公开(公告)号：US5656600A
公开(公告)日：1997-08-12
申请号：US37574
申请日：1993-03-25
IPC分类号： A61K38/00 , A61K49/00 , A61K51/08 , A61P7/02 , C07K5/02 , C07K7/02 , C07K14/815 , C07K5/00 , C07K7/00 , C07K17/00
CPC分类号： C07K5/0202 , A61K51/088 , C07K14/815 , A61K2123/00 , A61K38/00
摘要： .alpha.-Ketoamide derivatives, their pharmaceutically acceptable salts, compositions, diagnostic compositions and pharmaceutical compositions, which are useful for preventing or treating in a mammal a pathological condition characterized by thrombosis are described..alpha.-Ketoamide derivatives, their pharmaceutically acceptable salts, compositions and diagnostic compositions, which are useful for in vivo imaging of thrombi in a mammal are also described.Methods of preventing or treating in a mammal a pathological condition characterized by thrombosis and methods of in vivo imaging of thrombi in a mammal are also disclosed.
摘要翻译： 描述了可用于预防或治疗哺乳动物特征在于血栓形成的病理状态的α-甲基酰胺衍生物，其药学上可接受的盐，组合物，诊断组合物和药物组合物。 还描述了可用于哺乳动物血栓体内成像的α-甲基酰胺衍生物，其药学上可接受的盐，组合物和诊断组合物。 还公开了在哺乳动物中预防或治疗血栓形成的特征的病理状态和哺乳动物血栓体内成像方法。
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公开(公告)号：US5597804A
公开(公告)日：1997-01-28
申请号：US139300
申请日：1993-10-18
IPC分类号： A61K38/55 , A61K31/195 , A61K31/198 , A61K31/695 , A61K38/00 , A61K38/06 , A61P7/02 , C07C279/12 , C07C279/36 , C07C307/02 , C07C307/06 , C07C307/08 , C07C307/10 , C07C311/06 , C07C311/13 , C07C311/19 , C07C317/26 , C07D207/16 , C07D211/60 , C07D257/04 , C07D403/06 , C07D403/12 , C07F7/10 , C07K5/06 , C07K5/068 , C07K5/072 , C07K5/078 , C07K5/083 , C07K5/093 , C07K5/097 , C07K5/113 , C07K14/75 , A61K37/00 , C07K5/08 , A61K37/02
CPC分类号： C07D207/16 , C07D211/60 , C07D257/04 , C07K14/75 , C07K5/0606 , C07K5/06086 , C07K5/06113 , C07K5/06139 , C07K5/06165 , C07K5/0806 , C07K5/081 , C07K5/0819 , C07K5/1021 , A61K38/00 , Y10S514/822
摘要： The present invention is directed to N-sulfonyl arginine alpha-keto-amide derivatives, their pharmaceutically acceptable salts and compositions thereof which are useful as antithrombotic agents in mammals and also the use of these compounds as antithrombotic agents. Also, disclosed are methods of using these inhibitors in their various embodiments as therapeutic agents for disease states characterized by disorders of the blood coagulation process. Further disclosed are compounds useful as intermediates in the preparation of these compounds.
摘要翻译： 本发明涉及在哺乳动物中用作抗血栓形成剂的N-磺酰基精氨酸α-酮酰胺衍生物及其药学上可接受的盐和组合物，以及这些化合物作为抗血栓形成剂的用途。 还公开了在各种实施方案中使用这些抑制剂作为以凝血过程紊乱为特征的疾病状态的治疗剂的方法。 进一步公开的是可用作制备这些化合物的中间体的化合物。
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10.发明申请Nucleic acid molecules encoding a transmembrane serine protease 9, the encoded polypeptides and methods based thereon 有权编码跨膜丝氨酸蛋白酶9的核酸分子，编码的多肽和基于其的方法公开(公告)号：US20030166851A1
公开(公告)日：2003-09-04
申请号：US10112221
申请日：2002-03-27
发明人： Edwin Madison , Edgar O. Ong
IPC分类号： C07K001/00 , C07K014/00 , C07K017/00
CPC分类号： C12N9/6424 , Y10S436/809
摘要： Provided herein are type II transmembrane serine protease 9 (MTSP9) polypeptides. Zymogen and activated forms of these polypeptides as well as single and two chain forms of the protease domain are also provided. Methods using the polypeptides to identify compounds that modulate the protease activity of an MTSP9 are provided.
摘要翻译： 本文提供II型跨膜丝氨酸蛋白酶9（MTSP9）多肽。 还提供了这些多肽的酶原和活化形式以及蛋白酶结构域的单链和两链形式。 提供了使用多肽来鉴定调节MTSP9的蛋白酶活性的化合物的方法。
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