公开(公告)号：US5049555A

公开(公告)日：1991-09-17

申请号：US286153

申请日：1988-12-19

申请人： Waclaw J. Rzeszotarski ,  Maria E. Guzewska ,  Suzanne R. Ellenberger ,  Lisa H. Conti ,  John W. Ferkany ,  Donald J. Kyle

发明人： Waclaw J. Rzeszotarski ,  Maria E. Guzewska ,  Suzanne R. Ellenberger ,  Lisa H. Conti ,  John W. Ferkany ,  Donald J. Kyle

IPC分类号： A61K31/66

CPC分类号： A61K31/66

摘要： The invention pertains to a method and pharmaceutical compositions for treating, preventing or reducing neurodegeneration associated with chronic central nervous system or hypoxic, ischemic and hypoglycemic injury to the central nervous system and for the treatment of anxiety through the use of 2-amino-.omega.-phosphonoalkanoic acids having a cycloalkyl group bridging adjacent carbons on the alkyl chain, their pharmaceutically acceptable salts and derivatives as neuroprotectants and anxiolytics.

摘要翻译： 本发明涉及用于治疗，预防或减少与中枢神经系统的慢性中枢神经系统或缺氧，缺血和低血糖损伤有关的神经退行性疾病和通过使用2-氨基-ω- 在烷基链上具有邻接碳原子的环烷基的膦酰基链烷酸，其药学上可接受的盐和衍生物作为神经保护剂和抗焦虑剂。

公开(公告)号：US5395827A

公开(公告)日：1995-03-07

申请号：US171629

申请日：1993-12-22

申请人： Waclaw J. Rzeszotarski ,  Suzanne R. Ellenberger ,  Maria E. Guzewska ,  John W. Ferkany ,  Gregory S. Hamilton ,  Raymond J. Patch ,  Edward W. Karbon, Jr

发明人： Waclaw J. Rzeszotarski ,  Suzanne R. Ellenberger ,  Maria E. Guzewska ,  John W. Ferkany ,  Gregory S. Hamilton ,  Raymond J. Patch ,  Edward W. Karbon, Jr

IPC分类号： A61K31/66 ,  C07F9/38

CPC分类号： C07F9/3882 ,  A61K31/66 ,  C07F9/3834

摘要： The present invention pertains to antagonists of excitatory amino acid neurotransmitter receptor antagonists, their method of preparation as well as compositions containing them which have the general formula: ##STR1## wherein n and m independently are 0, 1, 2, or 3; R.sub.1 is selected from the group consisting of hydrogen and R.sub.2 ; R.sub.2 is selected from the group consisting of hydrogen, halogen, halomethyl, nitro, amino, alkoxy, hydroxyl, hydroxymethyl, C.sub.1 to C.sub.6 lower alkyl, C.sub.7 to C.sub.12 higher alkyl, aryl and aralkyl, wherein if R.sub.2 is hydrogen, R.sub.1 is not hydrogen; R.sub.3 is selected from the group consisting of hydrogen and C.sub.1 to C.sub.6 lower alkyl; the stereoisomers thereof in their resolved or racemic form, and pharmaceutically acceptable salts thereof.

摘要翻译： 本发明涉及兴奋性氨基酸神经递质受体拮抗剂的拮抗剂，它们的制备方法以及含有它们的组合物，它们具有以下通式：其中n和m独立地是0,1,2或3; R1选自氢和R2; R2选自氢，卤素，卤代甲基，硝基，氨基，烷氧基，羟基，羟甲基，C1至C6低级烷基，C7至C12高级烷基，芳基和芳烷基，其中如果R2是氢，R1不是氢 ; R3选自氢和C1至C6低级烷基; 其立体异构体以其分辨或外消旋形式，及其药学上可接受的盐。

公开(公告)号：US20100041587A1

公开(公告)日：2010-02-18

申请号：US12540062

申请日：2009-08-12

申请人： R. Stephen PORTER ,  Kristen K. Flaharty ,  James E. Tcheng ,  John W. Ferkany

发明人： R. Stephen PORTER ,  Kristen K. Flaharty ,  James E. Tcheng ,  John W. Ferkany

IPC分类号： A61K38/16 ,  A61K31/727

CPC分类号： A61K31/445 ,  A61K31/5377 ,  A61K31/5513 ,  A61K31/727 ,  A61K38/49 ,  A61K2300/00

摘要： The invention features methods for preventing platelet activation and aggregation and for treating individuals suffering from conditions or undergoing procedures that may result in unwanted platelet aggregation. The methods are based on the intravenous, subcutaneous, or transdermal administration of a platelet activation or aggregation inhibitor, e.g., xemilofiban, followed by oral administration of the same or a different platelet activation or aggregation inhibitor. The treatment may commence prior to a medical or surgical procedure or after the outbreak of an adverse medical condition, either of which results in the activation of platelets that may lead to thrombus formation, and may continue thereafter.

摘要翻译： 本发明的特征在于防止血小板活化和聚集以及治疗患有可能导致不想要的血小板聚集的病症或经历程序的个体的方法。 该方法基于静脉内，皮下或透皮给药血小板活化或聚集抑制剂，例如替莫非溴，然后口服施用相同或不同的血小板活化或聚集抑制剂。 治疗可以在医疗或手术过程之前或在不良医学状况爆发之后开始，其中任何一种导致血小板的激活，其可能导致血栓形成，并且可以继续。

公开(公告)号：US4906638A

公开(公告)日：1990-03-06

申请号：US136751

申请日：1987-12-22

申请人： Michael J. Pontecorvo ,  John W. Ferkany

发明人： Michael J. Pontecorvo ,  John W. Ferkany

IPC分类号： A61K31/135 ,  A61K31/00 ,  A61K31/215 ,  A61K31/415 ,  A61K31/42 ,  A61K31/435 ,  A61K31/44 ,  A61K31/445 ,  A61K31/46 ,  A61K31/47 ,  A61K31/485 ,  A61K31/495 ,  A61K31/54 ,  A61K31/55 ,  A61K31/675 ,  A61K45/00 ,  A61P25/00 ,  A61P25/08 ,  A61P43/00

CPC分类号： A61K31/495 ,  A61K31/485 ,  A61K31/54 ,  A61K31/55

摘要： A pharmaceutical composition comprises an anti-epileptic drug that does not inhibit, enhance or otherwise modify dextromethorphan binding to the central nervous system dextromethorphan receptor and an effective amount of dextromethorphan to potentiate the anticonvulsant activity of the drug. Other related compounds similar to dextromethorphan which inhibit or enhance dextromethorphan binding to the dextromethorphan site in the brain are also suitable as potentiating agents for the anticonvulsants. A method of treating epilepsy and other convulsions include the steps of introducing to the patient an effective amount of the compound comprising an anti-epileptic drug and potentiating amount of dextromethorphan or one of the related compounds.

摘要翻译： 药物组合物包含不抑制，增强或以其它方式改变右美沙芬结合中枢神经系统右美沙芬受体的抗癫痫药物和有效量的右美沙芬以增强药物的抗惊厥活性。 类似于右美沙芬的其他相关化合物，其抑制或增强右美沙芬与脑中右美沙芬位点的结合也适合作为抗惊厥药的增效剂。 治疗癫痫和其他惊厥的方法包括向患者引入有效量的包含抗癫痫药物和增强量的右美沙芬或相关化合物之一的化合物的步骤。