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    Method of treating tumors
    67.
    发明授权
    Method of treating tumors 失效
    治疗肿瘤的方法

    公开(公告)号：US5648071A

    公开(公告)日：1997-07-15

    申请号：US409549

    申请日：1995-03-24

    Applicant: Robert L. Hunter ,  Alexander Duncan

    Inventor： Robert L. Hunter ,  Alexander Duncan

    IPC: A61K31/765 ,  A61K38/44 ,  A61K38/49 ,  A61K31/74

    CPC classification number: A61K38/49 ,  A01N1/021 ,  A01N1/0226 ,  A61K31/765 ,  A61K38/446

    Abstract: In accordance with the present invention, a method is provided for treating tumors. More particularly, the present invention relates to a method for treating tumors comprising injecting a solution of certain ethylene oxide-propylene oxide surface-active copolymers and a solution containing chemotherapeutic agents into a human or animal with a tumor. The solutions can be injected simultaneously or separately at different times. In addition, the surface-active copolymer and the chemotherapeutic agent can be in the same solution. The surface-active copolymer can be an ethylene oxide-propylene oxide condensation product with the following general formula:HO(C.sub.2 H.sub.4 O).sub.b (C.sub.3 H.sub.6 O).sub.a (O.sub.2 H.sub.4 O).sub.b Hwherein a is an integer such that the hydrophobe represented by (C.sub.3 H.sub.6 O) has a molecular weight of approximately 950 to 4000 daltons, preferably approximately 1200 to 3500 daltons, and b is an integer such that the hydrophile portion represented by (C.sub.2 H.sub.4 O) constitutes approximately 50% to 90% by weight of the compound.

    Abstract translation: 根据本发明，提供了一种治疗肿瘤的方法。 更具体地，本发明涉及一种治疗肿瘤的方法，包括将某些环氧乙烷 - 环氧丙烷表面活性共聚物的溶液和含有化学治疗剂的溶液注射到具有肿瘤的人或动物中。 溶液可以在不同时间同时或分开注射。 此外，表面活性共聚物和化学治疗剂可以在相同的溶液中。 表面活性共聚物可以是具有以下通式的环氧乙烷 - 环氧丙烷缩合产物：HO（C 2 H 4 O）b（C 3 H 6 O）a（O 2 H 4 O）b H其中a是（C 3 H 6 O）表示的疏水基具有 分子量为约950至4000道尔顿，优选约1200至3500道尔顿，b为使（C 2 H 4 O）表示的亲水部分构成化合物的约50重量％至90重量％的整数。

    Enhancement of thrombolytic therapy with deglycosylated forms of plasminogen
    68.
    发明授权
    Enhancement of thrombolytic therapy with deglycosylated forms of plasminogen 失效
    用去糖基化形式的纤溶酶原增强血栓溶解治疗

    公开(公告)号：US5637299A

    公开(公告)日：1997-06-10

    申请号：US461172

    申请日：1995-06-05

    Applicant: Jan McDonagh ,  Myoung H. Lee

    Inventor： Jan McDonagh ,  Myoung H. Lee

    IPC: A61K38/16 ,  A61K38/48 ,  A61K38/49 ,  C12N9/64 ,  C12N9/68

    CPC classification number: A61K38/484 ,  A61K38/166 ,  A61K38/49

    Abstract: This invention provides an improved method for enhancing the activity of thrombolytic agents, including t-PA, scu-PA, tcu-PA, streptokinase, acylated plasminogen-streptokinase activator complex (APSAC), mixtures of these, and other activators of plasminogen. The enhancement method comprises supplementation of plasma plasminogen levels with deglycosylated forms of glu- and lys-plasminogen. Deglycosylated plasminogen refers herein to glu- or lys-plasminogen 2 having a single oligosaccharide chain at Thr.sub.345, plasminogens having a single oligosaccharide chain at Asn.sub.288, and unglycosylated forms of plasminogen. The work described herein shows that a less glycosylated form of plasminogen (glu-plasminogen 2) has a higher affinity for fibrin clots than a more glycosylated plasminogen (glu-plasminogen 1). Based on this work, it is believed that glycosylation of plasminogen inhibits binding of plasminogen to fibrin clots, perhaps due to steric hindrance, and further, that deglycosylated forms of plasminogen may be more effective enhancers of scu-PA in thrombolytic therapy than fully glycosylated forms of plasminogen. Improved enhancement of the activity of thrombolytic agents allows the use of lower therapeutic doses and thus, is expected to relieve some of the bleeding and other side effects of thrombolytic therapy.

    Abstract translation: 本发明提供了一种增强溶栓剂（包括t-PA，scu-PA，tcu-PA，链激酶，酰化纤溶酶原 - 链激酶激活剂复合物（APSAC））及其混合物和纤溶酶原激活剂的活性的改进方法。 增强方法包括用去糖基化形式的葡萄糖和溶血纤溶酶原补充血浆纤溶酶原水平。 糖基化纤维蛋白溶酶原是指在Thr345具有单个寡糖链的葡糖或溶酶体纤溶酶原2，在Asn288具有单个寡糖链的纤溶酶原和未糖基化形式的纤溶酶原。 本文所述的工作表明，较多糖基化的纤溶酶原（glu-plasminogen 1），较少的糖基化形式的纤溶酶原（glu-plasminogen 2）对纤维蛋白凝块具有更高的亲和力。 基于这项工作，据信纤维蛋白溶酶原的糖基化抑制纤维蛋白溶酶原与纤维蛋白凝块的结合，这可能是由于空间位阻引起的，此外，溶纤溶酶原的去糖基化形式可能是完全糖基化形式的溶栓治疗中scu-PA的更有效的增强剂 的纤溶酶原。 改善溶栓剂活性的增强使得可以使用较低的治疗剂量，因此预期可以缓解溶栓治疗的一些出血和其它副作用。

    Use of intra-platelet urokinase-type plasminogen activators for long-term inhibition of thrombosis
    69.
    发明授权
    Use of intra-platelet urokinase-type plasminogen activators for long-term inhibition of thrombosis 失效
    使用血小板尿激酶型纤溶酶原激活剂长期抑制血栓形成

    公开(公告)号：US5626841A

    公开(公告)日：1997-05-06

    申请号：US254922

    申请日：1994-06-07

    Applicant: Victor Gurewich

    Inventor： Victor Gurewich

    IPC: A61K38/49 ,  C12N15/57 ,  C12N9/64 ,  C12N9/72

    CPC classification number: A61K38/49

    Abstract: A method of adjunctive therapy to inhibit reocclusions in a patient, e.g., after thrombolytic therapy or angioplasty, by administering to the patient a bolus of an amount of purified pro-urokinase ("pro-UK") that inhibits the formation of occlusive thrombi without inducing a systemic effect in the patient, the pro-UK is administered after the completion of the thrombolytic treatment and periodically thereafter for the duration of therapy, and becomes incorporated into the outer membrane of the platelets of the patient, thereby increasing the T.sub. 1/2 of the pro-UK in plasma, which is about 7 to 8 minutes, to about 4 to 5 days, and inhibiting reocclusion without inducing a systemic effect.

    Abstract translation: 一种辅助治疗方法，例如在溶栓治疗或血管成形术之后，通过对患者施用一定量的纯化的尿激酶（“pro-UK”），其抑制闭塞血栓的形成而不在 在患者中引起全身效应，在溶栓治疗完成后施用pro-UK，并在治疗期间定期施用，并且将其并入患者血小板的外膜中，从而增加T + E ，英制血浆中的1/2 + EE，其为约7至8分钟至约4至5天，并且抑制再闭合而不引起全身作用。

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