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1. 发明申请

US20100048657A1 CONTROL OF MALIGNANT CELLS PROLIFERATION THROUGH THE INHIBITION OF CASEIN KINASE 2 审中-公开
标题翻译：通过抑制CASEIN KINASE 2抑制恶性细胞的增殖
公开(公告)号：US20100048657A1
公开(公告)日：2010-02-25
申请号：US12441077
申请日：2007-09-11
申请人： Michael Kalafatis
发明人： Michael Kalafatis
IPC分类号： A61K31/4184 , A61K31/4192 , A61P35/02
CPC分类号： A61K31/4192
摘要： Methods and related compositions are disclosed for treating an array of myeloproliferative disorders and hematological malignancies. In particular, treatment methods and compositions for treating chronic myelogenous leukemia are disclosed. The methods and compositions utilize certain casein kinases, and specifically CK2α agents.
摘要翻译：公开了治疗一系列骨髓增生性疾病和血液恶性肿瘤的方法和相关组合物。特别地，公开了治疗慢性骨髓性白血病的治疗方法和组合物。方法和组合物利用某些酪蛋白激酶，特别是CK2α试剂。

2. 发明申请

US20070299013A1 Exosite-Directed Thrombin Inhibitors 审中-公开
标题翻译：异位导向凝血酶抑制剂
公开(公告)号：US20070299013A1
公开(公告)日：2007-12-27
申请号：US10571989
申请日：2004-07-01
申请人： Michael Kalafatis
发明人： Michael Kalafatis
IPC分类号： A61K38/08 , A61K38/07 , A61P7/02 , C07K5/10 , C07K7/06
CPC分类号： C07K14/745 , A61K38/00 , C07K5/1021
摘要： Disclosed are an amino acid sequence of the human blood clotting factor Va, peptides containing such sequence, and additional peptides of interest that significantly inhibit thrombin generation. Also disclosed are pharmaceutical compositions containing these peptides and related therapeutic methods for inhibiting thrombin generation and treating blood coagulation disorders.
摘要翻译：公开了人血液凝固因子Va的氨基酸序列，含有该序列的肽，以及显着抑制凝血酶产生的另外的目的肽。还公开了含有这些肽的药物组合物和用于抑制凝血酶产生和治疗凝血障碍的相关治疗方法。

3. 发明授权

US06248548B1 Thrombosis prophylaxis for factor Vleiden carriers 失效
标题翻译：凝血因子Vleiden携带者的血栓预防
公开(公告)号：US06248548B1
公开(公告)日：2001-06-19
申请号：US09431103
申请日：1999-11-01
申请人： Cornelis Van't Veer , Michael Kalafatis , Kenneth G. Mann
发明人： Cornelis Van't Veer , Michael Kalafatis , Kenneth G. Mann
IPC分类号： C12Q156
CPC分类号： A61K38/57
摘要： Persons having the Factor VLEIDEN mutation and a lower than average plasma level of TFPI have been found to be at elevated risk of thrombosis. Prophylactic methods for reducing the risk of thrombosis employ the administration of TFPI to achieve higher levels in the plasma.
摘要翻译：已经发现具有因子VLEIDEN突变和低于平均血浆TFPI水平的人处于升高的血栓形成风险。降低血栓形成风险的预防方法使用TFPI的施用以在血浆中达到更高的水平。

4. 发明授权

US5977057A Thrombosis prophylaxis for factor V.sup.LEIDEN carriers 失效
标题翻译：凝血因子VLEIDEN载体的血栓预防
公开(公告)号：US5977057A
公开(公告)日：1999-11-02
申请号：US707782
申请日：1996-05-08
申请人： Cornelis Van't Veer , Michael Kalafatis , Kenneth G. Mann
发明人： Cornelis Van't Veer , Michael Kalafatis , Kenneth G. Mann
IPC分类号： G01N33/50 , A61K38/55 , A61K38/57 , A61P7/02 , C07K14/745 , C07K14/81 , A01N37/18 , A61K38/00 , C12Q1/56
CPC分类号： A61K38/57
摘要： Persons having the Factor V.sup.LEIDEN mutation and a lower than average plasma level of TFPI have been found to be at elevated risk of thrombosis. Prophylactic methods for reducing the risk of thrombosis employ the administration of TFPI to achieve higher levels in the plasma.
摘要翻译：已经发现具有因子VLEIDEN突变和低于平均血浆TFPI水平的人处于升高的血栓形成风险。降低血栓形成风险的预防方法使用TFPI的施用以在血浆中达到更高的水平。

5. 发明授权

US06703364B2 Thrombin generation inhibitors 有权
公开(公告)号：US06703364B2
公开(公告)日：2004-03-09
申请号：US09911129
申请日：2001-07-23
申请人： Michael Kalafatis , Kenneth G. Mann
发明人： Michael Kalafatis , Kenneth G. Mann
IPC分类号： A61K3800
CPC分类号： C07K14/745 , A61K38/00
摘要： Peptides derived from amino acids 307 to 356 of the human blood coagulation factor Va are provided. Such peptides comprise: i) a length of between 3 and 50 amino acids, ii) a minimum of 3 contiguous amino acids from the 307-356 heavy chain region of factor Va, excluding peptide segments comprising amino acids 311 to 325 and amino acids 321 to 335, iii) optional additional amino acids at one or both ends of the contiguous amino acids such that the entire peptide is at least 60% identical to a sequence within 307 to 356 of factor Va, and iv) have an IC50 of between 50 nM to 500 &mgr;M for inhibition of prothrombinase. The present invention also provides a pharmaceutical composition comprising one or more prothrombinase-inhibiting peptide segments. The present invention also provides administration of the pharmaceutical composition to human subjects for the purpose of preventing thrombotic disorders.

6. 发明申请

US20100267638A1 EXOSITE-DIRECTED THROMBIN INHIBITORS 审中-公开
公开(公告)号：US20100267638A1
公开(公告)日：2010-10-21
申请号：US12720068
申请日：2010-03-09
申请人： Michael Kalafatis
发明人： Michael Kalafatis
IPC分类号： A61K38/36 , A61P7/02
CPC分类号： C07K14/745
摘要： Disclosed are an amino acid sequence of the human blood clotting factor Va, peptides containing such sequence, and additional peptides of interest that significantly inhibit thrombin generation. Also disclosed are pharmaceutical compositions containing these peptides and related therapeutic methods for inhibiting thrombin generation and treating blood coagulation disorders.
摘要翻译：公开了人血液凝固因子Va的氨基酸序列，含有该序列的肽，以及显着抑制凝血酶产生的另外的目的肽。还公开了含有这些肽的药物组合物和用于抑制凝血酶产生和治疗凝血障碍的相关治疗方法。

7. 发明申请

US20090054507A1 CONTROL OF MALIGNANT CELLS BY KINASE INHIBITION 审中-公开
标题翻译：通过激酶抑制对恶性细胞的控制
公开(公告)号：US20090054507A1
公开(公告)日：2009-02-26
申请号：US12201693
申请日：2008-08-29
申请人： Michael Kalafatis
发明人： Michael Kalafatis
IPC分类号： A61K31/4184 , A61K31/4192
CPC分类号： A61K31/4184 , A61K31/4192
摘要： Inhibitors of casein kinase 2 are described that have been found to arrest uncontrolled cell proliferation, thereby suggesting their use in cancer treatment strategies. Specific applications include treating breast cancer, colon cancer, melanoma, chronic myelogenous leukemia, bladder cancer, renal cancer, and brain cancer. Various methods and compositions utilizing the inhibitors are described.
摘要翻译：已经发现已经发现已经发现抑制不受控制的细胞增殖的酪蛋白激酶2的抑制剂，从而表明它们在癌症治疗策略中的应用。具体应用包括治疗乳腺癌，结肠癌，黑素瘤，慢性骨髓性白血病，膀胱癌，肾癌和脑癌。描述了利用抑制剂的各种方法和组合物。

8. 发明授权

US07074892B2 Thrombin generation inhibitors 有权
标题翻译：凝血酶生成抑制剂
公开(公告)号：US07074892B2
公开(公告)日：2006-07-11
申请号：US10795795
申请日：2004-03-08
申请人： Michael Kalafatis , Kenneth G. Mann
发明人： Michael Kalafatis , Kenneth G. Mann
IPC分类号： A61K38/08 , A61K38/07 , A61K38/00 , A61K35/14
CPC分类号： C07K14/745 , A61K38/00
摘要： Peptides derived from amino acids 307 to 356 of the human blood coagulation factor Va are provided. Such peptides comprise: i) a length of between 3 and 50 amino acids, ii) a minimum of 3 contiguous amino acids from the 307–356 heavy chain region of factor Va, excluding peptide segments comprising amino acids 311 to 325 and amino acids 321 to 335, iii) optional additional amino acids at one or both ends of the contiguous amino acids such that the entire peptide is at least 60% identical to a sequence within 307 to 356 of factor Va, and iv) have an IC50 of between 50 nM to 500 μM for inhibition of prothrombinase. The present invention also provides a pharmaceutical composition comprising one or more prothrombinase-inhibiting peptide segments. The present invention also provides administration of the pharmaceutical composition to human subjects for the purpose of preventing thrombotic disorders.
摘要翻译：提供了源自人凝血因子Va的氨基酸307至356的肽。这样的肽包括：i）3至50个氨基酸的长度，ii）来自因子Va的307-356重链区域的最少3个连续氨基酸，不包括包含氨基酸311至325的氨基酸和氨基酸321 至335，iii）连续氨基酸的一端或两端的任选的另外的氨基酸，使得整个肽与因子Va的307至356之间的序列至少60％相同，和iv）具有IC < 50nM至50μM之间，用于抑制凝血酶原酶。本发明还提供了包含一种或多种凝血酶原酶抑制肽片段的药物组合物。为了防止血栓形成障碍，本发明还提供了将药物组合物给予受试者。

9. 发明授权

US5856114A Immunologic detection of factor VA fragments in hemorrhagic and thrombotic clinical settings 失效
标题翻译：在出血性和血栓性临床环境中的因子VA片段的免疫检测
公开(公告)号：US5856114A
公开(公告)日：1999-01-05
申请号：US606549
申请日：1996-02-26
申请人： Kenneth G. Mann , Michael Kalafatis
发明人： Kenneth G. Mann , Michael Kalafatis
IPC分类号： G01N33/86 , C12Q1/56
CPC分类号： G01N33/86 , G01N2333/96463
摘要： The present invention is directed to immunochemical detection procedures, e.g., using both Western blotting and direct immunoassays, for fragments of Factor Va, which can thus be used; (a) in a predictive manner to evaluate the existence and/or extent of a thrombotic complication; (b) to monitor the efficacy of prophylaxis for a thrombotic condition; and (c) as a means to evaluate potential risk of hemorrhage during thrombolytic therapy.
摘要翻译：本发明涉及免疫化学检测程序，例如使用Western印迹和直接免疫测定两者，因此可以使用因子Va片段; （a）以预测方式评估血栓并发症的存在和/或程度; （b）监测预防血栓形成的疗效; 和（c）作为评估溶栓治疗期间出血潜在风险的手段。

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