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54 条记录 (耗时 0.042 秒)

    Cyclic oxyguanidine pyrazinones as protease inhibitors
    21.
    发明授权
    Cyclic oxyguanidine pyrazinones as protease inhibitors 有权
    环氧乙酰吡嗪酮作为蛋白酶抑制剂

    公开(公告)号：US07030110B2

    公开(公告)日：2006-04-18

    申请号：US10263663

    申请日：2002-10-04

    申请人： Aihua Wang ,  Bruce Edward Tomczuk ,  Tianbao Lu ,  Richard M. Soll ,  John Curtis Spurlino ,  Roger Francis Bone

    发明人： Aihua Wang ,  Bruce Edward Tomczuk ,  Tianbao Lu ,  Richard M. Soll ,  John Curtis Spurlino ,  Roger Francis Bone

    IPC分类号： A61K31/535 ,  A61K31/497 ,  A61K31/4965 ,  A61K31/553 ,  A61K31/55

    CPC分类号： C07D413/12 ,  C07D413/14

    摘要： Cyclic oxyguanidine pyrazinone compounds are described, including compounds of the Formula I: wherein R3, R4, R5, W, and A are as set forth in the specification, as well as hydrates, solvates or pharmaceutically acceptable salts thereof. The compounds of the invention are potent inhibitors of proteases, especially trypsin-like serine proteases, such as chymotrypsin, trypsin, thrombin, plasmin and factor Xa. Certain of the compounds exhibit antithrombotic activity via direct, selective inhibition of thrombin. Compositions for inhibiting loss of blood platelets, inhibiting formation of blood platelet aggregates, inhibiting formation of fibrin, inhibiting thrombus formation, and inhibiting embolus formation are described. 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, such as catheters, blood dialysis machines, blood collection syringes and tubes, blood lines and stents. Additionally, the compounds can be detectably labeled and employed for in vivo imaging of thrombi.

    摘要翻译： 描述了环状氧基胍吡嗪酮化合物，包括式I化合物：其中R 3，R 4，R 5，W和A是 如说明书中所述，以及其水合物，溶剂合物或其药学上可接受的盐。 本发明的化合物是蛋白酶的有效抑制剂，特别是胰蛋白酶样丝氨酸蛋白酶，如胰凝乳蛋白酶，胰蛋白酶，凝血酶，纤溶酶和因子Xa。 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。 描述了抑制血小板损失，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栓塞形成的组合物。 本发明化合物的其它用途是作为凝血剂或者物理上连接于用于血液收集，血液循环和血液储存（例如导管，血液透析机，采血注射器和管）中使用的装置的制造中使用的材料的抗凝剂， 血线和支架。 另外，化合物可以被可检测地标记并用于血栓的体内成像。

    Cyclic oxyguanidine pyrazinones as protease inhibitors
    23.
    发明授权
    Cyclic oxyguanidine pyrazinones as protease inhibitors 有权
    环氧乙酰吡嗪酮作为蛋白酶抑制剂

    公开(公告)号：US06476016B2

    公开(公告)日：2002-11-05

    申请号：US09905883

    申请日：2001-07-17

    申请人： Aihua Wang ,  Bruce Edward Tomczuk ,  Tianbao Lu ,  Richard M. Soll ,  John Curtis Spurlino ,  Roger Francis Bone

    发明人： Aihua Wang ,  Bruce Edward Tomczuk ,  Tianbao Lu ,  Richard M. Soll ,  John Curtis Spurlino ,  Roger Francis Bone

    IPC分类号： C07D41312

    CPC分类号： C07D413/12 ,  C07D413/14

    摘要： Cyclic oxyguanidine pyrazinone compounds are described, including compounds of the Formula I: wherein R3, R4, R5, W, and A are as set forth in the specification, as well as hydrates, solvates or pharmaceutically acceptable salts thereof. The compounds of the invention are potent inhibitors of proteases, especially trypsin-like serine proteases, such as chymotrypsin, trypsin, thrombin, plasmin and factor Xa. Certain of the compounds exhibit antithrombotic activity via direct, selective inhibition of thrombin. Compositions for inhibiting loss of blood platelets, inhibiting formation of blood platelet aggregates, inhibiting formation of fibrin, inhibiting thrombus formation, and inhibiting embolus formation are described. 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, such as catheters, blood dialysis machines, blood collection syringes and tubes, blood lines and stents. Additionally, the compounds can be detectably labeled and employed for in vivo imaging of thrombi.

    摘要翻译： 描述了环状氧基胍吡嗪酮化合物，包括式I的化合物：其中R 3，R 4，R 5，W和A如说明书中所述，以及其水合物，溶剂合物或其药学上可接受的盐。 本发明的化合物是蛋白酶的有效抑制剂，特别是胰蛋白酶样丝氨酸蛋白酶，如胰凝乳蛋白酶，胰蛋白酶，凝血酶，纤溶酶和因子Xa。 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。 描述了抑制血小板损失，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栓塞形成的组合物。 本发明化合物的其它用途是作为凝血剂或者物理上连接于用于血液收集，血液循环和血液储存（例如导管，血液透析机，采血注射器和管）中使用的装置的制造中使用的材料的抗凝剂， 血线和支架。 另外，化合物可以被可检测地标记并用于血栓的体内成像。

    (3,4-dioxocyclobuten-1-yl)chromene, indene, and dihydronaphthalenone derivatives as smooth muscle relaxants
    26.
    发明授权
    (3,4-dioxocyclobuten-1-yl)chromene, indene, and dihydronaphthalenone derivatives as smooth muscle relaxants 失效
    （3,4-二氧杂环丁烯-1-基）色烯，茚和二氢萘酮衍生物作为平滑肌松弛剂

    公开(公告)号：US5482942A

    公开(公告)日：1996-01-09

    申请号：US267691

    申请日：1994-06-28

    申请人： Richard M. Soll ,  Paul J. Dollings

    发明人： Richard M. Soll ,  Paul J. Dollings

    IPC分类号： A61K31/35 ,  A61K31/352 ,  A61P9/00 ,  A61P9/02 ,  A61P11/00 ,  A61P13/02 ,  A61P15/00 ,  C07C225/20 ,  C07D311/58 ,  A61K31/495 ,  A61K31/415 ,  C07C229/40 ,  C07D211/82 ,  C07D241/02 ,  C07D311/74 ,  C07D407/02

    CPC分类号： C07D311/58

    摘要： This invention relates to novel 4-(3,4-dioxocyclobuten-1-yl)chromenes and dihydronaphthalenones and 3-(3,4-dioxocyclobuten-1-yl)indenes and salts thereof having smooth muscle relaxing activity, to their use in the treatment of hypertension as well as for treatment of peripheral vascular disease, congestive heart failure, disorders involving excessive smooth muscle contraction of the urinary tract such as incontinence or of the gastrointestinal tract such as irritable bowel syndrome, asthma, and hair loss and to pharmaceutical compositions containing an invention compound. The present invention discloses compounds represented by the formula (I): ##STR1## wherein: R.sub.1 and R.sub.2, independent from each other, are selected from the following: C.sub.1-6 perfluoroalkoxy, C.sub.1-6 perfluoroalkyl, C.sub.1-6 alkyl, C.sub.1-6 alkoxy, hydroxyl, C.sub.1-6 alkoxycarbonyl, nitro, cyano, halogen, C.sub.1-6 alkylsulfonamido, C.sub.1-6 perfluoroalkylsulfonamido, amino, C.sub.1-6 acylamino, C.sub.1-6 perfluoroacylamino, mono or di-C.sub.1-12 alkylamino, C.sub.1-6 alkylsulfonyl, C.sub.6-10 arylsulfonyl, carboxyl, C.sub.1-12 mono or di-alkylaminocarbonyl, or hydrogen;a and b together form an --O-- linkage, C.dbd.O, or a direct bond:R.sub.3 and R.sub.4, independent from each other, are H or C.sub.1-6 alkyl, optionally substituted by fluorine;R.sub.5 is amino or C.sub.1-12 mono alkylamine;R.sub.6 is H, C.sub.1-6 perfluoroalkyl, C.sub.1-6 alkyl, C.sub.6-10 aryl, or mono or bicyclic heteroaryl containing 1-3 heteroatoms selected from N, O, or S.

    摘要翻译： 本发明涉及具有平滑肌松弛活性的新型4-（3,4-二氧杂环丁烯-1-基）色烯和二氢萘酮及其3-（3,4-二氧杂环丁烯-1-基）茚及其盐，用于 治疗高血压以及治疗周围血管疾病，充血性心力衰竭，涉及尿路过度平滑肌收缩的疾病，例如失禁或胃肠道，例如肠易激综合征，哮喘和脱发，以及药物组合物 含有发明化合物。 本发明公开了由式（I）表示的化合物：其中：R 1和R 2彼此独立地选自如下：C 1-6全氟烷氧基，C 1-6全氟烷基，C 1-6烷基，C 1 1-6烷氧基，羟基，C 1-6烷氧基羰基，硝基，氰基，卤素，C 1-6烷基磺酰氨基，C 1-6全氟烷基磺酰氨基，氨基，C 1-6酰氨基，C 1-6全氟酰基氨基，单或二-C 1-12烷基氨基， 6烷基磺酰基，C 6-10芳基磺酰基，羧基，C 1-12单或二烷基氨基羰基或氢; a和b一起形成O-键，C = O或直接键：R 3和R 4彼此独立地是H或任选被氟取代的C 1-6烷基; R5是氨基或C1-12单烷基胺; R 6是H，C 1-6全氟烷基，C 1-6烷基，C 6-10芳基或含有1-3个选自N，O或S的杂原子的单或双环杂芳基。

    Radiolabeled 1-aryl pyrazoles, the synthesis thereof and the use thereof as pest GABA receptor ligands
    29.
    发明授权
    Radiolabeled 1-aryl pyrazoles, the synthesis thereof and the use thereof as pest GABA receptor ligands 有权
    放射性标记的1-芳基吡唑，其合成及其作为害虫GABA受体配体的用途

    公开(公告)号：US06409988B1

    公开(公告)日：2002-06-25

    申请号：US09606051

    申请日：2000-06-29

    申请人： Daljit S. Dhanoa ,  Sanath Meegalla ,  Dario Doller ,  Richard M. Soll

    发明人： Daljit S. Dhanoa ,  Sanath Meegalla ,  Dario Doller ,  Richard M. Soll

    IPC分类号： A61K5100

    CPC分类号： C07D231/44 ,  A61K51/0423 ,  A61K51/0453

    摘要： The present invention is directed to radiolabeled compounds of Formula I: or salts thereof, where R1 represents R8, R8O, R8SO2, R8SO or R8S in which R8 is tritiated or deuterated methyl; X is halo, cyano, C1-6 alkoxycarbonyl, C2-6 alkynyl, optionally substituted C6-14 aryl or an optionally substituted 5- to 7-membered heteroaromatic ring linked to thiazole via a carbon-carbon bond; R2 is hydrogen or amino; and R3-R7 are defined in the specification. The invention is also directed to methods of using such compounds for demonstrating specific insect GABA receptors, qualitatively screening for compounds acting on an insect GABA receptor or quantitatively assaying concentrations of a compound acting on an insect GABA receptor.

    摘要翻译： 本发明涉及放射性标记的式I化合物或其盐，其中R 1表示R8，R8O，R8SO2，R8SO或R8S，其中R8为氚化或氘代甲基; X为卤素，氰基，C1-6烷氧基羰基，C2-6 炔基，任选取代的C 6-14芳基或经由碳 - 碳键与噻唑连接的任选取代的5至7元杂芳环; R 2是氢或氨基; 本发明还涉及使用这些化合物来证明特异性昆虫GABA受体的方法，定性筛选作用于昆虫GABA受体的化合物或定量测定作用于昆虫GABA受体的化合物的浓度 。