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1. 发明授权

US07119068B2 Methods of screening for compounds that modulate TAFIa activity, compounds, and methods of using the compounds 失效
标题翻译：筛选调节TAFIa活性的化合物的方法，化合物和使用该化合物的方法
公开(公告)号：US07119068B2
公开(公告)日：2006-10-10
申请号：US10651659
申请日：2003-08-29
申请人： Robert S. Greenfield , Seong Soo A. An , Latchezar Trifonov , Jean Vaugeois , Clarke Slemon
发明人： Robert S. Greenfield , Seong Soo A. An , Latchezar Trifonov , Jean Vaugeois , Clarke Slemon
IPC分类号： C07C65/01 , C07C65/03 , C07C65/10 , A01N37/36 , A01N31/60
CPC分类号： C12Q1/37 , A61K31/60 , C12Q1/56 , G01N33/573 , G01N33/6893 , G01N33/86 , G01N33/9486 , G01N2500/00
摘要： Provided are methods of screening compounds for any aspirin-related activity other than TAFI inhibition, and also for non-inhibition of TAFI. Compounds identified by the screening methods can be used to treat, prevent or manage in a patient pain, fever, colon cancer, pancreatic cancer or an inflammatory, platelet aggregation, fibrinolytic or hemorrhagic disease or disorder. Also provided is a method of evaluating test compounds for TAFI inhibitory activity wherein the TAFI inhibitory activity of these test compounds is compared to the TAFI inhibitory activity of aspirin or its derivatives or metabolites. Further provided is a method of treating, preventing or managing in a patient, a hemorrhagic or thrombotic disease or disorder with high dose aspirin or aspirin derivatives or metabolites. Also contemplated is a method of treating, preventing or managing in a patient, pain, fever, colon cancer, pancreatic cancer or an inflammatory, platelet aggregation, fibrinolytic or hemorrhagic disease or disorder comprising administering aspirin or a derivative thereof or any other therapeutic having at least one desired therapeutic or prophylactic activity of aspirin to a patient in need thereof and administering to the patient a factor that promotes TAFIa activity, e.g. stablized TAFIa, to ameliorate one or more adverse side effects of the therapeutic. Compounds identified by the methods of the invention are also provided.
摘要翻译：提供了筛选化合物除了TAFI抑制以外的任何阿司匹林相关活性的方法，以及用于非抑制TAFI的方法。通过筛选方法鉴定的化合物可用于治疗，预防或控制患者疼痛，发烧，结肠癌，胰腺癌或炎症，血小板聚集，纤维蛋白溶解或出血性疾病或病症。还提供了评价试验化合物对TAFI抑制活性的方法，其中将这些试验化合物的TAFI抑制活性与阿司匹林或其衍生物或代谢物的TAFI抑制活性进行比较。还提供了一种治疗，预防或控制患者出血性或血栓性疾病或病症的方法，其中高剂量阿司匹林或阿司匹林衍生物或代谢物。还考虑了治疗，预防或控制患者的疼痛，发烧，结肠癌，胰腺癌或炎性，血小板聚集，纤维蛋白溶解或出血性疾病或病症的方法，包括给予阿司匹林或其衍生物或任何其它具有对有需要的患者的阿司匹林的至少一种期望的治疗或预防活性，并向患者施用促进TAFIa活性的因子，例如稳定TAFIa，以改善治疗的一种或多种不良副作用。还提供了通过本发明的方法鉴定的化合物。

2. 发明授权

US07767646B2 Methods of screening for compounds that modulate TAFIa activity, compounds, and methods of using the compounds 有权
标题翻译：筛选调节TAFIa活性的化合物的方法，化合物和使用该化合物的方法
公开(公告)号：US07767646B2
公开(公告)日：2010-08-03
申请号：US11544906
申请日：2006-10-06
申请人： Robert S. Greenfield , Seong Soo A. An , Latchezar Trifonov , Jean Vaugeois , Clarke Slemon
发明人： Robert S. Greenfield , Seong Soo A. An , Latchezar Trifonov , Jean Vaugeois , Clarke Slemon
IPC分类号： C12Q1/00
CPC分类号： C12Q1/37 , A61K31/60 , C12Q1/56 , G01N33/573 , G01N33/6893 , G01N33/86 , G01N33/9486 , G01N2500/00
摘要： Provided are methods of screening compounds for any aspirin-related activity other than TAFI inhibition, and also for non-inhibition of TAFI. Compounds identified by the screening methods can be used to treat, prevent or manage in a patient pain, fever, colon cancer, pancreatic cancer or an inflammatory, platelet aggregation, fibrinolytic or hemorrhagic disease or disorder. Also provided is a method of evaluating test compounds for TAFI inhibitory activity wherein the TAFI inhibitory activity of these test compounds is compared to the TAFI inhibitory activity of aspirin or its derivatives or metabolites. Further provided is a method of treating, preventing or managing in a patient, a hemorrhagic or thrombotic disease or disorder with high dose aspirin or aspirin derivatives or metabolites. Also contemplated is a method of treating, preventing or managing in a patient, pain, fever, colon cancer, pancreatic cancer or an inflammatory, platelet aggregation, fibrinolytic or hemorrhagic disease or disorder comprising administering aspirin or a derivative thereof or any other therapeutic having at least one desired therapeutic or prophylactic activity of aspirin to a patient in need thereof and administering to the patient a factor that promotes TAFIa activity, e.g. stabilized TAFIa, to ameliorate one or more adverse side effects of the therapeutic. Compounds identified by the methods of the invention are also provided.
摘要翻译：提供了筛选化合物除了TAFI抑制以外的任何阿司匹林相关活性的方法，以及用于非抑制TAFI的方法。通过筛选方法鉴定的化合物可用于治疗，预防或控制患者疼痛，发烧，结肠癌，胰腺癌或炎症，血小板聚集，纤维蛋白溶解或出血性疾病或病症。还提供了评价试验化合物对TAFI抑制活性的方法，其中将这些试验化合物的TAFI抑制活性与阿司匹林或其衍生物或代谢物的TAFI抑制活性进行比较。还提供了一种治疗，预防或控制患者出血性或血栓性疾病或病症的方法，其中高剂量阿司匹林或阿司匹林衍生物或代谢物。还考虑了治疗，预防或控制患者的疼痛，发烧，结肠癌，胰腺癌或炎性，血小板聚集，纤维蛋白溶解或出血性疾病或病症的方法，包括给予阿司匹林或其衍生物或任何其它具有对有需要的患者的阿司匹林的至少一种期望的治疗或预防活性，并向患者施用促进TAFIa活性的因子，例如稳定的TAFIa，以改善治疗的一种或多种不良副作用。还提供了通过本发明的方法鉴定的化合物。

3. 发明申请

US20080305508A1 Methods of screening for compounds that modulate TAFIa activity, compounds, and methods of using the compounds 有权
标题翻译：筛选调节TAFIa活性的化合物的方法，化合物和使用该化合物的方法
公开(公告)号：US20080305508A1
公开(公告)日：2008-12-11
申请号：US11544906
申请日：2006-10-06
申请人： Robert S. Greenfield , Seong Soo A. An , Latchezar Trifonov , Jean Vaugeois , Clarke Slemon
发明人： Robert S. Greenfield , Seong Soo A. An , Latchezar Trifonov , Jean Vaugeois , Clarke Slemon
IPC分类号： A61K31/60
CPC分类号： C12Q1/37 , A61K31/60 , C12Q1/56 , G01N33/573 , G01N33/6893 , G01N33/86 , G01N33/9486 , G01N2500/00
摘要： Provided are methods of screening compounds for any aspirin-related activity other than TAFI inhibition, and also for non-inhibition of TAFI. Compounds identified by the screening methods can be used to treat, prevent or manage in a patient pain, fever, colon cancer, pancreatic cancer or an inflammatory, platelet aggregation, fibrinolytic or hemorrhagic disease or disorder. Also provided is a method of evaluating test compounds for TAFI inhibitory activity wherein the TAFI inhibitory activity of these test compounds is compared to the TAFI inhibitory activity of aspirin or its derivatives or metabolites. Further provided is a method of treating, preventing or managing in a patient, a hemorrhagic or thrombotic disease or disorder with high dose aspirin or aspirin derivatives or metabolites. Also contemplated is a method of treating, preventing or managing in a patient, pain, fever, colon cancer, pancreatic cancer or an inflammatory, platelet aggregation, fibrinolytic or hemorrhagic disease or disorder comprising administering aspirin or a derivative thereof or any other therapeutic having at least one desired therapeutic or prophylactic activity of aspirin to a patient in need thereof and administering to the patient a factor that promotes TAFIa activity, e.g. stabilized TAFIa, to ameliorate one or more adverse side effects of the therapeutic. Compounds identified by the methods of the invention are also provided.
摘要翻译：提供了筛选化合物除了TAFI抑制以外的任何阿司匹林相关活性的方法，以及用于非抑制TAFI的方法。通过筛选方法鉴定的化合物可用于治疗，预防或控制患者疼痛，发烧，结肠癌，胰腺癌或炎症，血小板聚集，纤维蛋白溶解或出血性疾病或病症。还提供了评价试验化合物对TAFI抑制活性的方法，其中将这些试验化合物的TAFI抑制活性与阿司匹林或其衍生物或代谢物的TAFI抑制活性进行比较。还提供了一种治疗，预防或控制患者出血性或血栓性疾病或病症的方法，其中高剂量阿司匹林或阿司匹林衍生物或代谢物。还考虑了治疗，预防或控制患者的疼痛，发烧，结肠癌，胰腺癌或炎性，血小板聚集，纤维蛋白溶解或出血性疾病或病症的方法，包括给予阿司匹林或其衍生物或任何其它具有对有需要的患者的阿司匹林的至少一种期望的治疗或预防活性，并向患者施用促进TAFIa活性的因子，例如稳定的TAFIa，以改善治疗的一种或多种不良副作用。还提供了通过本发明的方法鉴定的化合物。

4. 发明申请

US20100310540A1 METHODS OF SCREENING FOR COMPOUNDS THAT MODULATE TAFIA ACTIVITY, COMPOUNDS, AND METHODS OF USING THE COMPOUNDS 审中-公开
标题翻译：用于调节TAFIA活性的化合物的筛选方法，化合物和使用该化合物的方法
公开(公告)号：US20100310540A1
公开(公告)日：2010-12-09
申请号：US12795152
申请日：2010-06-07
申请人： Robert S. Greenfield , Seong Soo A. An , Latchezar Trifonov , Jean Vaugeois , Clarke Slemon
发明人： Robert S. Greenfield , Seong Soo A. An , Latchezar Trifonov , Jean Vaugeois , Clarke Slemon
IPC分类号： A61K38/48 , C12Q1/37 , A61P9/10 , A61P7/02 , A61P7/06 , A61P19/02 , A61K31/609 , C07C271/20 , C07C235/60 , A61K31/60 , A61K38/17 , A61K38/49 , A61K31/616
CPC分类号： C12Q1/37 , A61K31/60 , C12Q1/56 , G01N33/573 , G01N33/6893 , G01N33/86 , G01N33/9486 , G01N2500/00
摘要： Provided are methods of screening compounds for any aspirin-related activity other than TAFI inhibition, and also for non-inhibition of TAFI. Compounds identified by the screening methods can be used to treat, prevent or manage in a patient pain, fever, colon cancer, pancreatic cancer or an inflammatory, platelet aggregation, fibrinolytic or hemorrhagic disease or disorder. Also provided is a method of evaluating test compounds for TAFI inhibitory activity wherein the TAFI inhibitory activity of these test compounds is compared to the TAFI inhibitory activity of aspirin or its derivatives or metabolites. Further provided is a method of treating, preventing or managing in a patient, a hemorrhagic or thrombotic disease or disorder with high dose aspirin or aspirin derivatives or metabolites. Also contemplated is a method of treating, preventing or managing in a patient, pain, fever, colon cancer, pancreatic cancer or an inflammatory, platelet aggregation, fibrinolytic or hemorrhagic disease or disorder comprising administering aspirin or a derivative thereof or any other therapeutic having at least one desired therapeutic or prophylactic activity of aspirin to a patient in need thereof and administering to the patient a factor that promotes TAFIa activity, e.g. stabilized TAFIa, to ameliorate one or more adverse side effects of the therapeutic. Compounds identified by the methods of the invention are also provided.
摘要翻译：提供了筛选化合物除了TAFI抑制以外的任何阿司匹林相关活性的方法，以及用于非抑制TAFI的方法。通过筛选方法鉴定的化合物可用于治疗，预防或控制患者疼痛，发烧，结肠癌，胰腺癌或炎症，血小板聚集，纤维蛋白溶解或出血性疾病或病症。还提供了评价试验化合物对TAFI抑制活性的方法，其中将这些试验化合物的TAFI抑制活性与阿司匹林或其衍生物或代谢物的TAFI抑制活性进行比较。还提供了一种治疗，预防或控制患者出血性或血栓性疾病或病症的方法，其中高剂量阿司匹林或阿司匹林衍生物或代谢物。还考虑了治疗，预防或控制患者的疼痛，发烧，结肠癌，胰腺癌或炎性，血小板聚集，纤维蛋白溶解或出血性疾病或病症的方法，包括给予阿司匹林或其衍生物或任何其它具有对有需要的患者的阿司匹林的至少一种期望的治疗或预防活性，并向患者施用促进TAFIa活性的因子，例如稳定的TAFIa，以改善治疗的一种或多种不良副作用。还提供了通过本发明的方法鉴定的化合物。

5. 发明申请

US20050222096A1 Methods of screening for compounds that modulate TAFIa activity, compounds, and methods of using the compounds 失效
标题翻译：筛选调节TAFIa活性的化合物的方法，化合物和使用该化合物的方法
公开(公告)号：US20050222096A1
公开(公告)日：2005-10-06
申请号：US10651659
申请日：2003-08-29
申请人： Robert Greenfield , Seong An , Latchezar Trifonov , Jean Vaugeois , Clarke Slemon
发明人： Robert Greenfield , Seong An , Latchezar Trifonov , Jean Vaugeois , Clarke Slemon
IPC分类号： A61K31/60 , C12Q1/00 , C12Q1/56 , G01N33/573 , G01N33/68 , G01N33/86 , G01N33/94
CPC分类号： C12Q1/37 , A61K31/60 , C12Q1/56 , G01N33/573 , G01N33/6893 , G01N33/86 , G01N33/9486 , G01N2500/00
摘要： Provided are methods of screening compounds for any aspirin-related activity other than TAFI inhibition, and also for non-inhibition of TAFI. Compounds identified by the screening methods can be used to treat, prevent or manage in a patient pain, fever, colon cancer, pancreatic cancer or an inflammatory, platelet aggregation, fibrinolytic or hemorrhagic disease or disorder. Also provided is a method of evaluating test compounds for TAFI inhibitory activity wherein the TAFI inhibitory activity of these test compounds is compared to the TAFI inhibitory activity of aspirin or its derivatives or metabolites. Further provided is a method of treating, preventing or managing in a patient, a hemorrhagic or thrombotic disease or disorder with high dose aspirin or aspirin derivatives or metabolites. Also contemplated is a method of treating, preventing or managing in a patient, pain, fever, colon cancer, pancreatic cancer or an inflammatory, platelet aggregation, fibrinolytic or hemorrhagic disease or disorder comprising administering aspirin or a derivative thereof or any other therapeutic having at least one desired therapeutic or prophylactic activity of aspirin to a patient in need thereof and administering to the patient a factor that promotes TAFIa activity, e.g. stablized TAFIa, to ameliorate one or more adverse side effects of the therapeutic. Compounds identified by the methods of the invention are also provided.
摘要翻译：提供了筛选化合物除了TAFI抑制以外的任何阿司匹林相关活性的方法，以及用于非抑制TAFI的方法。通过筛选方法鉴定的化合物可用于治疗，预防或控制患者疼痛，发烧，结肠癌，胰腺癌或炎症，血小板聚集，纤维蛋白溶解或出血性疾病或病症。还提供了评价试验化合物对TAFI抑制活性的方法，其中将这些试验化合物的TAFI抑制活性与阿司匹林或其衍生物或代谢物的TAFI抑制活性进行比较。还提供了一种治疗，预防或控制患者出血性或血栓性疾病或病症的方法，其中高剂量阿司匹林或阿司匹林衍生物或代谢物。还考虑了治疗，预防或控制患者的疼痛，发烧，结肠癌，胰腺癌或炎性，血小板聚集，纤维蛋白溶解或出血性疾病或病症的方法，包括给予阿司匹林或其衍生物或任何其它具有对有需要的患者的阿司匹林的至少一种期望的治疗或预防活性，并向患者施用促进TAFIa活性的因子，例如稳定TAFIa，以改善治疗的一种或多种不良副作用。还提供了通过本发明的方法鉴定的化合物。

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