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1. 发明申请

US20080280920A1 Plasminogen Activator Inhibitor-1 Inhibitors 审中-公开
标题翻译：纤溶酶原激活物抑制剂-1抑制剂
公开(公告)号：US20080280920A1
公开(公告)日：2008-11-13
申请号：US12096479
申请日：2006-12-07
申请人： Latchezar S. Trifonov , Jean Vaugeois , Bhavna Gaikwad , Robert S. Greenfield
发明人： Latchezar S. Trifonov , Jean Vaugeois , Bhavna Gaikwad , Robert S. Greenfield
IPC分类号： A61K31/506 , A61K31/496 , C07D403/14 , A61P35/00 , A61P9/00 , A61P9/10 , C07D401/04
CPC分类号： C07D311/16 , C07C271/28 , C07D213/74 , C07D233/56 , C07D333/60 , C07D401/04 , C07D401/12 , C07D405/06 , C07D409/06 , C07D409/12 , C07D409/14
摘要： Inhibitors of plasminogen activator inhibitor-1 (PAI-I) are provided, which may also act as anti cancer agents, of formulae (I-V).
摘要翻译：提供了还可以作为式（I-V）的抗癌剂的纤溶酶原激活物抑制剂-1（PAI-1）的抑制剂。

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。

5. 发明授权

US06703504B2 Conformationally constrained compounds as dendrimer cores 失效
标题翻译：构象约束的化合物作为树枝状聚合物核心
公开(公告)号：US06703504B2
公开(公告)日：2004-03-09
申请号：US10071206
申请日：2002-02-11
申请人： Clarke Slemon , Bohumil Macel , Latchazar Trifonov , Jean Vaugeois
发明人： Clarke Slemon , Bohumil Macel , Latchazar Trifonov , Jean Vaugeois
IPC分类号： C07D23900
CPC分类号： C08G83/003 , C07C39/17 , C07C39/27 , C07C49/747 , C07C49/753 , C07C237/10 , C07C2603/94
摘要： There are provided novel chemical compounds and their uses in the preparation of polymers and oligomers, and the preparation of such compounds. In certain embodiments there are provided dendritic polymers and oligomers, of a type having at least four polymeric or oligomeric organic chains emanating from a single chemical core, each of the chains being of substantially equal length and substantially the same chemical composition. Such compounds may be referred to as dendrimers. Also provided are novel chemical entities useful as core entities in the preparation of dentrimers. Dendrimers can recognize a core substructure to which the polymeric/oligomeric chains (“dendrons”) are covalenty attached and from which they extend with systematic branching radially outward in a three dimensional fashion, to approximately the same extent to each other. Together, core and dendrons constitute macromolecules possessing a high degree of internal structural replication attributable to the branches.
摘要翻译：提供新颖的化合物及其在制备聚合物和低聚物中的用途以及这些化合物的制备。在某些实施方案中，提供了具有从单个化学核发出的至少四个聚合物或低聚有机链的类型的树枝状聚合物和低聚物，每条链具有基本相同的长度和基本上相同的化学组成。这些化合物可以称为树枝状大分子。还提供了新颖的化学实体，可用作制备残留物的核心实体。树枝状聚合物可以识别聚合物/低聚链（“树枝状”）被共价连接的核心亚结构，并且它们以三维方式径向向外以系统分支延伸到彼此大致相同的程度。核心和树突一起构成具有归属于分枝的高度内部结构复制的大分子。

6. 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。

7. 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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