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    Benzamide and sulfonamide substituted aminoguanidines and alkoxyguanidines as protease inhibitors
    23.
    发明授权
    Benzamide and sulfonamide substituted aminoguanidines and alkoxyguanidines as protease inhibitors 有权
    苯甲酰胺和磺酰胺取代的氨基胍和烷氧基胍作为蛋白酶抑制剂

    公开(公告)号：US06344486B1

    公开(公告)日：2002-02-05

    申请号：US09283241

    申请日：1999-04-01

    申请人： Richard M. Soll ,  Tianbao Lu ,  Bruce E. Tomczuk ,  Thomas P. Markotan ,  Colleen Siedem

    发明人： Richard M. Soll ,  Tianbao Lu ,  Bruce E. Tomczuk ,  Thomas P. Markotan ,  Colleen Siedem

    IPC分类号： A61K31165

    CPC分类号： C07D213/40 ,  C07C279/00 ,  C07D211/16 ,  C07D211/62 ,  C07D213/74 ,  C07D217/06 ,  C07D295/192

    摘要： The present invention is directed to aminoguanidine and alkoxyguanidine compounds, including compounds of Formula I: wherein X is O or NH, L is —O— or —SO2—, and R1-R4, R9-R19, Ra, Rb, Rc, Y, Z, n and m are set forth in the specification, as well as hydrates, solvates or pharmaceutically acceptable salts thereof, that inhibit proteolytic enzymes such as thrombin. Also described are methods for preparing the compounds of Formula I. Certain of the compounds exhibit antithrombotic activity via direct, selective inhibition of thrombin, or are intermediates useful for forming compounds having antithrombotic activity. The invention includes a composition for inhibiting loss of blood platelets, inhibiting formation of blood platelet aggregates, inhibiting formation of fibrin, inhibiting thrombus formation, and inhibiting embolus formation in a mammal. Other uses of compounds of the invention are as anticoagulants either embedded in or physically linked to materials used in the manufacture of devices used in blood collection, blood circulation, and blood storage.

    摘要翻译： 本发明涉及氨基胍和烷氧基胍化合物，包括式I化合物：其中X为O或NH，L为-O-或-SO 2 - ，R 1 -R 4，R 9 -R 19，R a，R b，R c，Y ，Z，n和m在说明书中列出，以及抑制蛋白水解酶如凝血酶的水合物，溶剂合物或其药学上可接受的盐。 还描述了制备式I化合物的方法。某些化合物通过直接，选择性抑制凝血酶表现出抗血栓形成活性，或者是用于形成具有抗血栓形成活性的化合物的中间体。 本发明包括用于抑制血小板损失，抑制血小板聚集体形成，抑制纤维蛋白形成，抑制血栓形成和抑制哺乳动物栓塞形成的组合物。 本发明化合物的其它用途是作为抗凝剂，其嵌入或用于制造用于采血，血液循环和血液储存中的装置的材料中物理连接。

    Methods for treatment of asthma using S-oxybutynin
    24.
    发明授权
    Methods for treatment of asthma using S-oxybutynin 失效
    使用S-奥昔布宁治疗哮喘的方法

    公开(公告)号：US06294582B1

    公开(公告)日：2001-09-25

    申请号：US09574106

    申请日：2000-05-17

    申请人： Thomas P. Jerussi

    发明人： Thomas P. Jerussi

    IPC分类号： A61K31165

    CPC分类号： A61K9/008 ,  A61K9/2018 ,  A61K9/2059 ,  A61K31/216 ,  Y10S514/826

    摘要： Substantially optically pure S-oxybutynin, or a pharmaceutically acceptable salt thereof, is administered as a treatment for asthma. Such treatment is provided while reducing the adverse effects associated with the administration of racemic oxybutynin.

    摘要翻译： 施用基本上光学纯的S-奥昔布宁或其药学上可接受的盐作为哮喘治疗。 提供这样的治疗，同时减少与外消旋奥昔布宁的施用相关的不良反应。

    Neuropeptide antagonists
    26.
    发明授权
    Neuropeptide antagonists 失效
    神经肽拮抗剂

    公开(公告)号：US06197822B1

    公开(公告)日：2001-03-06

    申请号：US09491293

    申请日：2000-01-25

    申请人： Marlys Hammond

    发明人： Marlys Hammond

    IPC分类号： A61K31165

    CPC分类号： A61K31/165 ,  A61K31/167 ,  A61K31/235

    摘要： The compound is a neuropeptide Y antagonist and is effective in treating feeding disorders, cardiovascular diseases and other physiological disorders.

    摘要翻译： 该复合物是神经肽Y拮抗剂，并且有效治疗进食障碍，心血管疾病和其他生理障碍。

    Steroid sulphatase inhibitors
    27.
    发明授权
    Steroid sulphatase inhibitors 失效
    类固醇硫酸酶抑制剂

    公开(公告)号：US06187766B1

    公开(公告)日：2001-02-13

    申请号：US09238345

    申请日：1999-01-27

    申请人： Michael John Reed ,  Barry Victor Potter

    发明人： Michael John Reed ,  Barry Victor Potter

    IPC分类号： A61K31165

    CPC分类号： A61K31/37 ,  C07D311/16 ,  C07D311/30 ,  C07D311/32 ,  C07D311/36 ,  C07J41/0072

    摘要： A method of inhibiting steroid sulphatase activity in a subject in need of same as described. The method comprises administering to said subject a steroid sulphatase inhibiting amount of a ring system compound; which ring system compound comprises a ring to which is attached a sulphamate group of the formula wherein each of R1 and R2 is independently selected from H, alkyl, alkenyl, cycloalkyl and aryl, or together represent alkylene optionally containing one or more hetero atoms or groups in the alkylene chain; and wherein said compound is an inhibitor of an enzyme having steroid sulphatase activity (E.C.3.1.6.2); and if the sulphamate group of said compound is replaced with a sulphate group to form a sulphate compound and incubated with a steroid sulphatase enzyme (E.C.3.1.6.2) at a pH 7.4 and 37° C. it would provide a Km value of less than 50 &mgr;M.

    摘要翻译： 一种抑制需要与上述相同的对象的类固醇硫酸酯酶活性的方法。该方法包括向所述受试者施用抑制甾类硫酸酯酶的量的环系化合物; 所述环系化合物包含与R 1和R 2各自独立地选自H，烷基，烯基，环烷基和芳基的或者一起表示任选含有一个或多个杂原子或基团的亚烷基 亚烷基链; 并且其中所述化合物是具有类固醇硫酸酯酶活性的酶的抑制剂（E.C.3.1.6.2）; 并且如果所述化合物的氨基磺酸酯基团被硫酸根基团替代以形成硫酸盐化合物，并在pH 7.4和37℃下与类固醇硫酸酶（EC3.1.6.2）一起温育，则其将提供小于 50亩。

    Method for treating fungal infections
    28.
    发明授权
    Method for treating fungal infections 失效
    治疗真菌感染的方法

    公开(公告)号：US06180679B2

    公开(公告)日：2001-01-30

    申请号：US09367236

    申请日：1999-10-20

    申请人： Chuan Shih ,  Daniel Charles Williams

    发明人： Chuan Shih ,  Daniel Charles Williams

    IPC分类号： A61K31165

    CPC分类号： A61K31/395

    摘要： The present invention provides a method for controlling fungal growth, mycotic infections, yeast infections and parasitic infections using a therapeutically effective amount of a compound selected from Compounds (I-V). Further provided is a method for providing mdr inhibition using a therapeutically effective amount of a compound of formula (IA). Also provided is an antifungal composition comprising at least five percent (5%) by weight of a compound selected from Compounds (I-V).

    摘要翻译： 本发明提供使用治疗有效量的选自化合物（I-V）的化合物来控制真菌生长，真菌感染，酵母菌感染和寄生虫感染的方法。 还提供了使用治疗有效量的式（IA）化合物来提供mdr抑制的方法。 还提供了包含至少5重量％（5重量％）选自化合物（I-V）的化合物的抗真菌组合物。

    Anticonvulsant enantiomeric amino acid derivatives
    30.
    再颁专利
    Anticonvulsant enantiomeric amino acid derivatives 有权
    抗惊厥对映异构氨基酸衍生物

    公开(公告)号：USRE38551E1

    公开(公告)日：2004-07-06

    申请号：US10058634

    申请日：2002-01-28

    申请人： Harold Kohn

    发明人： Harold Kohn

    IPC分类号： A61K31165

    摘要： The present invention is directed to a compound in the R configuration about the asymmetric carbon in the following formula: pharmaceutical compositions containing same and the use thereof in treating CNS disorders in animals.