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1.发明授权Methods of screening for compounds that modulate TAFIa activity, compounds, and methods of using the compounds 失效筛选调节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
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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公开(公告)号：US5606017A
公开(公告)日：1997-02-25
申请号：US468162
申请日：1995-06-06
申请人： David Willner , Pamela A. Trail , H. Dalton King , Sandra J. Hofstead , Robert S. Greenfield , Gary R. Braslawsky
发明人： David Willner , Pamela A. Trail , H. Dalton King , Sandra J. Hofstead , Robert S. Greenfield , Gary R. Braslawsky
IPC分类号： A61K31/70 , A61K31/7028 , A61K31/7034 , A61K31/704 , A61K31/7042 , A61K31/7048 , A61K39/395 , A61K47/48 , A61P35/00 , A61P35/04 , C07G11/00 , C07H15/252 , C07H17/04 , C07K1/113 , C07K14/00 , C07K14/42 , C07K14/485 , C07K14/495 , C07K14/52 , C07K14/54 , C07K14/55 , C07K14/575 , C07K14/62 , C07K14/65 , C07K14/705 , C07K16/00 , C07K19/00 , C07K5/00 , C07D475/00 , C07H15/24 , C07H19/00
CPC分类号： A61K47/48684 , A61K47/48407 , A61K47/48692 , A61K47/48715
摘要： Provided are drug/ligand compounds of Formula (I): ##STR1## in which D is a drug moiety;n is an integer from 1 to 10;p is an integer from 1 to 6;Y is O or NH.sub.2.sup.+ Cl.sup.- ;z is 0 or 1;q is about 1 to about 10;X is a ligand; and,A is a Michael Addition Adduct.In a preferred embodiment, the ligand is an immunoglobulin, preferably a chimeric antibody or fragment thereof. Also provided are formulations comprising as an active ingredient a compound of Formula (I), intermediates useful for preparing the compounds of Formula (I), processes for preparing the compounds of Formula (I), and methods for using the compounds of the invention.
摘要翻译： 提供式（I）的药物/配体化合物：其中D是药物部分; n是1至10的整数; p是1至6的整数; Y是O或NH2 + Cl-; z为0或1; q为约1至约10; X是配体; A是迈克尔加成加成物。 在优选的实施方案中，配体是免疫球蛋白，优选嵌合抗体或其片段。 还提供了包含作为活性成分的式（I）化合物，可用于制备式（I）化合物的中间体，制备式（I）化合物的方法和使用本发明化合物的方法的制剂。
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3.发明授权
公开(公告)号：US5349066A
公开(公告)日：1994-09-20
申请号：US865062
申请日：1992-04-08
IPC分类号： A61K31/70 , A61K31/7028 , A61K31/7034 , A61K31/704 , A61K39/395 , A61K47/48 , A61P35/00 , C07C323/42 , C07C323/44 , C07D213/71 , C07D309/30 , C07H15/252 , C07K16/00 , C12N15/02 , C12P21/08 , C07D211/72 , C07C229/00 , C07C241/00
CPC分类号： C07H15/252 , A61K47/48338 , A61K47/48407 , A61K47/48715 , C07C323/44 , C07D213/71
摘要： The present invention provides novel N-substituted hydrazine bifunctional compounds, novel N-substituted hydrazone derivatives of a cytotoxic reagent incorporating the bifunctional compounds, novel conjugates containing at least one cytotoxic reagent molecule reacted with the bifunctional compound and bound to a molecule reactive with a target cell population, methods for their production, and pharmaceutical compositions and methods for delivering cytotoxic reagents to a target population of cells. The hydrazone bonds of the conjugates of the invention permit the release of free cytotoxic reagent from the conjugates in the acidic external or internal environment of the target cells. The bifunctional compounds, derivatives, conjugates and methods of the invention are useful in antibody-or ligand-mediated drug delivery systems for the preferential killing of a target cell population to treat diseases such as cancers, infections and autoimmune disorders.
摘要翻译： 本发明提供新型N-取代肼双功能化合物，结合双功能化合物的细胞毒性试剂的新N-取代腙衍生物，含有至少一种与双功能化合物反应的细胞毒性试剂分子的结合物，并结合至与靶标反应的分子 细胞群，其生产方法，以及用于将细胞毒性试剂递送至靶细胞群的药物组合物和方法。 本发明的轭合物的腙键可以在靶细胞的酸性外部或内部环境中从缀合物释放游离的细胞毒素试剂。 本发明的双功能化合物，衍生物，缀合物和方法可用于抗体或配体介导的药物递送系统，用于优先杀死靶细胞群以治疗疾病如癌症，感染和自身免疫性疾病。
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公开(公告)号：US20080280920A1
公开(公告)日：2008-11-13
申请号：US12096479
申请日：2006-12-07
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。
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5.发明授权Method of preparation of stabilized thrombin-activatable fibrinolysis inhibitor (TAFI) and methods of use thereof 有权稳定凝血酶激活性纤维蛋白溶解抑制剂（TAFI）的制备方法及其使用方法公开(公告)号：US06808927B2
公开(公告)日：2004-10-26
申请号：US10116095
申请日：2002-04-04
IPC分类号： G01N3353
CPC分类号： C12N9/48 , A61K38/05 , A61K38/363 , A61K38/49 , Y10S435/975 , A61K2300/00
摘要： The invention is directed in part to a purified form of stabilized activated thrombin-activatable fibrinolysis inhibitor (TAFIa). The invention is further directed to a method of producing stabilized TAFIa. The invention is also directed to methods for therapeutic use of stabilized TAFIa such as in the treatment, prevention or management of diseases via an anti-coagulant effect. The invention is also directed to methods for therapeutic use of inhibitors of TAFIa such as in the treatment, prevention or management of diseases via a procoagulant effect. The invention is also directed to methods of diagnostic use of stabilized TAFIa such as a standard in a chromogenic or a fluorometric carboxypeptidase activity assay. The present invention is also directed to kits comprising stabilized TAFIa useful in measuring carboxypepetidase activity.
摘要翻译： 本发明部分地涉及纯化形式的稳定的活化凝血酶活化纤维蛋白溶解抑制剂（TAFIa）。 本发明进一步涉及一种制备稳定的TAFIa的方法。 本发明还涉及用于治疗性使用稳定的TAFIa的方法，例如通过抗凝血剂作用治疗，预防或治疗疾病。 本发明还涉及治疗性使用TAFIa抑制剂的方法，例如通过促凝血作用治疗，预防或治疗疾病。 本发明还涉及诊断性使用稳定的TAFIa的方法，例如在显色或荧光羧肽酶活性测定中的标准。 本发明还涉及包含可用于测量羧基肽酶活性的稳定的TAFIa的试剂盒。
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6.发明授权Methods of screening for compounds that modulate TAFIa activity, compounds, and methods of using the compounds 有权筛选调节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
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。
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7.发明申请Methods of screening for compounds that modulate TAFIa activity, compounds, and methods of using the compounds 有权筛选调节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
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。
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8.发明授权Methods for measuring ADAMTS13 activity and protein on platelets and in plasma 有权测量血小板和血浆中ADAMTS13活性和蛋白质的方法公开(公告)号：US07270976B2
公开(公告)日：2007-09-18
申请号：US10894702
申请日：2004-07-19
IPC分类号： C12Q1/37
CPC分类号： C12Q1/37 , C12Q2337/00
摘要： Provided are assays to detect ADAMTS13 activity using peptide substrates. These assays can be used for diagnostic applications and to evaluate treatment of thrombotic thrombocytopenic purpura (TTP). Also provided is a novel form of ADAMTS13 found on platelets.
摘要翻译： 提供使用肽底物检测ADAMTS13活性的测定法。 这些测定法可用于诊断应用并评估治疗血栓性血小板减少性紫癜（TTP）。 还提供了在血小板上发现的ADAMTS13的新型形式。
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9.发明申请METHODS OF SCREENING FOR COMPOUNDS THAT MODULATE TAFIA ACTIVITY, COMPOUNDS, AND METHODS OF USING THE COMPOUNDS 审中-公开用于调节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
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。
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公开(公告)号：US07470519B2
公开(公告)日：2008-12-30
申请号：US10526167
申请日：2003-08-29
IPC分类号： G01N33/53
CPC分类号： C12Q1/37 , C12Q1/56 , G01N33/57415 , G01N33/57426 , G01N33/6893 , G01N33/86 , G01N2333/81 , G01N2800/085 , G01N2800/224 , G01N2800/226 , G01N2800/32
摘要： The invention relates to a diagnostic assay for selectively measuring levels of the 35kD form of thrombin-activatable fibrinolysis inhibitor (TAFIa or TAFIai), or a derivative or variant thereof, but not the TAFI proenzyme (TAFI) or the N-terminal activation peptide of TAFI.
摘要翻译： 本发明涉及用于选择性测量35kD形式的凝血酶激活性纤维蛋白溶解抑制剂（TAFIa或TAFIai）或其衍生物或变体，而不是TAFI酶原（TAFI）或N末端活化肽 TAFI。
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