公开(公告)号：US6117836A

公开(公告)日：2000-09-12

申请号：US307609

申请日：1994-12-02

申请人： Uma Sinha ,  David L. Wolf

发明人： Uma Sinha ,  David L. Wolf

IPC分类号： A61K38/36 ,  A61K38/00 ,  A61K38/17 ,  A61K38/43 ,  A61K38/47 ,  A61K39/395 ,  A61P7/02 ,  A61P29/00 ,  C07K14/42 ,  C07K14/745 ,  C07K16/36 ,  C12N9/64 ,  C07K4/00 ,  C07K16/18

CPC分类号： C12N9/6432 ,  A61K38/1709 ,  A61K38/47 ,  C07K14/42 ,  C07K14/745 ,  C07K16/36 ,  C12Y304/21006 ,  Y10S436/827

摘要： Reagents that specifically bind a carbohydrate target wherein sialic acid is linked at the nonreducing terminus of a glycoside to a galactose or galactosamine residue through an .alpha.2-6 linkage are able to inhibit the conversion of human Factor X to human Factor Xa. These reagents (SA/Gal/GalNAc binding reagents) as well as other strategies for inhibiting the conversion of Factor X to Factor Xa are useful in treating thrombosis, inflammation and other conditions associated with excess thrombin activity.

摘要翻译： PCT No.PCT / US93 / 02203。 371日期1994年12月2日第 102（e）1994年12月2日PCT PCT 1993年3月11日PCT公布。 公开号WO93 / 18782 日期1993年9月30日特异性结合碳水化合物靶标的试剂，其中唾液酸通过α2-6键在糖苷的非还原性末端连接到半乳糖或半乳糖胺残基，能够抑制人因子X转化为人因子 Xa。 这些试剂（SA / Gal / GalNAc结合试剂）以及抑制因子X转化成因子Xa的其它策略可用于治疗血栓形成，炎症和与过量凝血酶活性相关的其它病症。

公开(公告)号：US5968897A

公开(公告)日：1999-10-19

申请号：US16403

申请日：1998-01-30

申请人： David L. Wolf ,  Uma Sinha

发明人： David L. Wolf ,  Uma Sinha

IPC分类号： C12N15/09 ,  A61K38/00 ,  A61K38/43 ,  A61K38/46 ,  A61K38/48 ,  A61P7/04 ,  C07K14/745 ,  C12N9/64 ,  C12P21/00 ,  A61K38/36 ,  A61F13/00 ,  A61K35/16 ,  C07K14/435

CPC分类号： C12N9/6464 ,  C07K14/745 ,  C12N9/6432 ,  C12N9/647 ,  C12Y304/21006 ,  C12Y304/21069 ,  A61K38/00 ,  Y10S514/834 ,  Y10S530/83

摘要： Analogs of blood factors which are transiently inactive are useful in treatment of diseases characterized by thrombosis. In addition, modified forms of activated blood factors that generate the active blood factor in serum but have extended half-lives are useful in treating hemophilic conditions. These modified forms of the blood factor may be acylated forms which are slowly deacylated in vivo.

摘要翻译： 短暂失活的血液因子的类似物可用于治疗以血栓形成为特征的疾病。 此外，在血清中产生活性血因子但具有延长半衰期的活化血液因子的修饰形式可用于治疗嗜血性病症。 血液因子的这些修饰形式可以是在体内缓慢脱酰基化的酰化形式。

公开(公告)号：US5583107A

公开(公告)日：1996-12-10

申请号：US268003

申请日：1994-06-29

申请人： David L. Wolf ,  Uma Sinha

发明人： David L. Wolf ,  Uma Sinha

IPC分类号： C12N15/09 ,  A61K38/00 ,  A61K38/43 ,  A61K38/46 ,  A61K38/48 ,  A61P7/04 ,  C07K14/745 ,  C12N9/64 ,  C12P21/00 ,  A61K38/36 ,  A61K35/16 ,  C07K14/435 ,  C07K14/475

CPC分类号： C12N9/6464 ,  C07K14/745 ,  C12N9/6432 ,  C12N9/647 ,  C12Y304/21006 ,  C12Y304/21069 ,  A61K38/00 ,  Y10S514/834 ,  Y10S530/83

摘要： Analogs of blood factors which are transiently inactive are useful in treatment of diseases characterized by thrombosis. In addition, modified forms of activated blood factors that generate the active blood factor in serum but have extended half-lives are useful in treating hemophilic conditions. These modified forms of the blood factor may be acylated forms which are slowly deacylated in vivo.

公开(公告)号：US5837679A

公开(公告)日：1998-11-17

申请号：US469301

申请日：1995-06-06

申请人： David L. Wolf ,  Uma Sinha

发明人： David L. Wolf ,  Uma Sinha

IPC分类号： C12N15/09 ,  A61K38/00 ,  A61K38/43 ,  A61K38/46 ,  A61K38/48 ,  A61P7/04 ,  C07K14/745 ,  C12N9/64 ,  C12P21/00 ,  A61K38/36 ,  A61K35/14 ,  C07K1/06 ,  C07K14/475

CPC分类号： C12N9/6464 ,  C07K14/745 ,  C12N9/6432 ,  C12N9/647 ,  C12Y304/21006 ,  C12Y304/21069 ,  A61K38/00 ,  Y10S514/834 ,  Y10S530/83

摘要： Analogs of blood factors which are transiently inactive are useful in treatment of diseases characterized by thrombosis. In addition, modified forms of activated blood factors that generate the active blood factor in serum but have extended half-lives are useful in treating hemophilic conditions. These modified forms of the blood factor may be acylated forms which are slowly deacylated in vivo.

公开(公告)号：US5990079A

公开(公告)日：1999-11-23

申请号：US16400

申请日：1998-01-30

申请人： David L. Wolf ,  Uma Sinha

发明人： David L. Wolf ,  Uma Sinha

IPC分类号： C12N15/09 ,  A61K38/00 ,  A61K38/43 ,  A61K38/46 ,  A61K38/48 ,  A61P7/04 ,  C07K14/745 ,  C12N9/64 ,  C12P21/00 ,  A61K38/36 ,  A61F13/00 ,  A61K35/16 ,  C07K14/435

CPC分类号： C12N9/6464 ,  C07K14/745 ,  C12N9/6432 ,  C12N9/647 ,  C12Y304/21006 ,  C12Y304/21069 ,  A61K38/00 ,  Y10S514/834 ,  Y10S530/83

摘要： Analogs of blood factors which are transiently inactive are useful in treatment of diseases characterized by thrombosis. In addition, modified forms of activated blood factors that generate the active blood factor in serum but have extended half-lives are useful in treating hemophilia conditions. These modified forms of the blood factor may be acylated forms which are slowly deacylated in vivo.

摘要翻译： 短暂失活的血液因子的类似物可用于治疗以血栓形成为特征的疾病。 此外，在血清中产生活性血因子但具有延长半衰期的活化血液因子的修饰形式可用于治疗血友病病症。 血液因子的这些修饰形式可以是在体内缓慢脱酰基化的酰化形式。

公开(公告)号：US5798332A

公开(公告)日：1998-08-25

申请号：US302226

申请日：1994-09-06

申请人： Uma Sinha ,  David L. Wolf

发明人： Uma Sinha ,  David L. Wolf

IPC分类号： A61K38/36 ,  A61K38/00 ,  A61K38/17 ,  A61K38/43 ,  A61K38/47 ,  A61K39/395 ,  A61P7/02 ,  A61P29/00 ,  C07K14/42 ,  C07K14/745 ,  C07K16/36 ,  C12N9/64 ,  A61K38/16

CPC分类号： C12N9/6432 ,  A61K38/1709 ,  A61K38/47 ,  C07K14/42 ,  C07K14/745 ,  C07K16/36 ,  C12Y304/21006 ,  Y10S436/827

摘要： Reagents that specifically bind a carbohydrate target wherein sialic acid is linked at the nonreducing terminus of a glycoside to a galactose or galactosamine residue through an .alpha.2-6 linkage are able to inhibit the conversion of human Factor X to human Factor Xa. These reagents (SA/Gal/GalNAc binding reagents) as well as other strategies for inhibiting the conversion of Factor X to Factor Xa are useful in treating thrombosis, inflammation and other conditions associated with excess thrombin activity.

摘要翻译： 特异性结合碳水化合物靶标的试剂能够抑制人因子X向人因子Xa的转化，其中唾液酸在糖苷的非还原性末端通过α2-6键连接到半乳糖或半乳糖胺残基。 这些试剂（SA / Gal / GalNAc结合试剂）以及抑制因子X转化成因子Xa的其它策略可用于治疗血栓形成，炎症和与过量凝血酶活性相关的其它病症。

公开(公告)号：US20130237493A1

公开(公告)日：2013-09-12

申请号：US13823714

申请日：2011-09-30

申请人： Uma Sinha ,  Anjali Pandey

发明人： Uma Sinha ,  Anjali Pandey

IPC分类号： A61K31/506 ,  A61K31/7076

CPC分类号： A61K31/7076 ,  A61K31/506 ,  A61K2300/00

摘要： The present invention is directed to pharmaceutical compositions and methods of using combination therapies containing 4-(cyclopropylamino)-2-(4-(4-(ethylsulfonyl)piperazin-1-yl)phenylamino)pyrimidine-5-carboxamide, or a pharmaceutically acceptable salt thereof, and fludarabine for the treatment of cell proliferative disorders, such as undesired acute myeloid leukemia (AML), chronic lymphocytic leukemia (CLL), non-Hodgkin lymphoma (NHL), including diffuse large B cell lymphoma (DLBCL); mantle cell lymphoma, acute lymphocytic leukemia (ALL), follicular lymphoma, Burkitt's lymphoma, small Lymphocytic Lymphoma (SLL) and multiple myeloma.

摘要翻译： 本发明涉及使用含有4-（环丙基氨基）-2-（4-（4-（乙基磺酰基）哌嗪-1-基）苯基氨基）嘧啶-5-甲酰胺或其药学上可接受的组合疗法的药物组合物和方法 其盐和氟​​达拉滨用于治疗细胞增殖性疾病，例如不期望的急性骨髓性白血病（AML），慢性淋巴细胞白血病（CLL），非霍奇金淋巴瘤（NHL），包括弥漫性大B细胞淋巴瘤（DLBCL）; 套细胞淋巴瘤，急性淋巴细胞白血病（ALL），滤泡淋巴瘤，伯基特淋巴瘤，小淋巴细胞淋巴瘤（SLL）和多发性骨髓瘤。

公开(公告)号：US08455441B2

公开(公告)日：2013-06-04

申请号：US13414499

申请日：2012-03-07

申请人： Genmin Lu ,  David R. Phillips ,  Patrick Andre ,  Uma Sinha

发明人： Genmin Lu ,  David R. Phillips ,  Patrick Andre ,  Uma Sinha

IPC分类号： A61K39/00

CPC分类号： A61K38/4846 ,  A61K38/00 ,  A61K38/4826 ,  A61K38/4833 ,  A61K38/4853 ,  A61K39/00 ,  A61K47/60 ,  C07K14/435 ,  C12N9/6432 ,  C12Y304/21006

摘要： The present invention relates antidotes to anticoagulants targeting factor Xa. The antidotes are factor Xa protein derivatives that bind to the factor Xa inhibitors thereby substantially neutralizing them but do not assemble into the prothrombinase complex. The derivatives describe herein lack or have reduced intrinsic coagulant activity. Disclosed herein are methods of stopping or preventing bleeding in a patient that is currently undergoing anticoagulant therapy with a factor Xa inhibitor.

摘要翻译： 本发明涉及靶向因子Xa的抗凝剂的解毒剂。 解毒剂是与因子Xa抑制剂结合的因子Xa蛋白衍生物，从而基本上中和它们，但不组装到凝血酶原酶复合物中。 本文所述的衍生物缺乏或具有降低的内在凝结剂活性。 本文公开了在目前正在进行使用因子Xa抑制剂进行抗凝治疗的患者中停止或预防出血的方法。

公开(公告)号：US08455439B2

公开(公告)日：2013-06-04

申请号：US12616735

申请日：2009-11-11

申请人： Genmin Lu ,  Uma Sinha

发明人： Genmin Lu ,  Uma Sinha

IPC分类号： A61K38/57 ,  A61K35/14 ,  C07K14/745 ,  C07K14/81

CPC分类号： A61K38/36 ,  A61K35/16 ,  A61K38/16 ,  A61K38/37 ,  A61K38/482 ,  A61K38/4826 ,  A61K38/4833 ,  A61K38/4846 ,  A61K38/4853 ,  A61K45/06 ,  A61K2300/00

摘要： The present invention relates to antidotes of anticoagulants targeting factor Xa which antidotes are used in combination with blood coagulating agents or other heparin antidotes to prevent or reduce bleeding in a subject. The antidotes described herein have reduced or no intrinsic coagulant activity. Disclosed herein are methods of stopping or preventing bleeding in a patient that is or will be undergoing anticoagulant therapy with a factor Xa inhibitor.

摘要翻译： 本发明涉及抗凝剂靶向因子Xa的解毒剂，该解毒剂与凝血剂或其他肝素解毒剂组合使用以预防或减少受试者的出血。 本文所述的解毒剂具有降低或没有固有的凝结剂活性。 本文公开的是在患者中停止或预防出血的方法，该患者将使用因子Xa抑制剂进行或将要进行抗凝治疗。

公开(公告)号：US20120269788A1

公开(公告)日：2012-10-25

申请号：US13414499

申请日：2012-03-07

申请人： Genmin Lu ,  David R. Phillips ,  Patrick Andre ,  Uma Sinha

发明人： Genmin Lu ,  David R. Phillips ,  Patrick Andre ,  Uma Sinha

IPC分类号： A61K38/48 ,  C12N9/96 ,  C12N15/57 ,  A61P7/04 ,  C12N5/10 ,  C12N1/19 ,  A61K48/00 ,  A61P39/02 ,  C12N9/64 ,  C12N1/21

CPC分类号： A61K38/4846 ,  A61K38/00 ,  A61K38/4826 ,  A61K38/4833 ,  A61K38/4853 ,  A61K39/00 ,  A61K47/60 ,  C07K14/435 ,  C12N9/6432 ,  C12Y304/21006

摘要： The present invention relates antidotes to anticoagulants targeting factor Xa. The antidotes are factor Xa protein derivatives that bind to the factor Xa inhibitors thereby substantially neutralizing them but do not assemble into the prothrombinase complex. The derivatives describe herein lack or have reduced intrinsic coagulant activity. Disclosed herein are methods of stopping or preventing bleeding in a patient that is currently undergoing anticoagulant therapy with a factor Xa inhibitor.

摘要翻译： 本发明涉及靶向因子Xa的抗凝剂的解毒剂。 解毒剂是与因子Xa抑制剂结合的因子Xa蛋白衍生物，从而基本上中和它们，但不组装到凝血酶原酶复合物中。 本文所述的衍生物缺乏或具有降低的内在凝结剂活性。 本文公开了在目前正在进行使用因子Xa抑制剂进行抗凝治疗的患者中停止或预防出血的方法。