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68 条记录 (耗时 0.048 秒)

    Pyridinyl modulators of γ-secretase
    7.
    发明授权
    Pyridinyl modulators of γ-secretase 有权
    γ-分泌酶的吡啶基调节剂

    公开(公告)号：US07968725B2

    公开(公告)日：2011-06-28

    申请号：US12478820

    申请日：2009-06-05

    申请人： Tianbao Lu

    发明人： Tianbao Lu

    IPC分类号： C07D213/55 ,  A01N43/40

    CPC分类号： C07D213/74 ,  C07D213/55 ,  C07D401/04 ,  C07D405/04 ,  C07D409/04

    摘要： The present invention relates to compounds of Formula I as shown below, wherein the definitions of A, X, R1 R2, R3, R4, R5, R6, R7, R8, and R9 are provided in the specification. Compounds of Formula I are useful for the treatment of diseases associated with γ-secretase activity, including Alzheimer's disease.

    摘要翻译： 本发明涉及如下所示的式I化合物，其中A，X，R 1，R 2，R 3，R 4，R 5，R 6，R 7，R 8和R 9的定义在说明书中提供。 式I化合物可用于治疗与γ-分泌酶活性相关的疾病，包括阿尔茨海默氏病。

    Substituted 1,4-diazepines and uses thereof
    9.
    发明申请
    Substituted 1,4-diazepines and uses thereof 审中-公开
    取代的1,4-二氮杂及其用途

    公开(公告)号：US20060235007A1

    公开(公告)日：2006-10-19

    申请号：US11452861

    申请日：2006-06-14

    申请人： Tianbao Lu ,  Karen Milkiewicz ,  Pierre Raboisson ,  Maxwell Cummings ,  Raul Calvo ,  Daniel Parks ,  Louis LaFrance ,  Juan Marugan Sanchez ,  Joan Gushue ,  Kristi Leonard

    发明人： Tianbao Lu ,  Karen Milkiewicz ,  Pierre Raboisson ,  Maxwell Cummings ,  Raul Calvo ,  Daniel Parks ,  Louis LaFrance ,  Juan Marugan Sanchez ,  Joan Gushue ,  Kristi Leonard

    IPC分类号： A61K31/5513 ,  C07D403/02 ,  C07D413/02 ,  C07D243/18

    CPC分类号： C07D243/14

    摘要： The present invention is directed to novel 1,4-diazepines, pharmaceutical compositions thereof and the use thereof as inhibitors of HDM2-p53 interactions. Compounds have Formula I: or a solvate, hydrate or pharmaceutically acceptable salt thereof; wherein: R1, R2, R9, R10, Ra, Rd and M are defined herein; X is a bivalent radical of: an alkane, a cycloalkane, an optionally-substituted arene, an optionally-substituted heteroarene, an optionally-substituted arylalkane or an optionally-substituted heteroarylalkane; and R3 is —CO2Rd, —CO2M, —OH, —NHRd, —SO2Rd, —NHCONHRd, optionally-substituted amidino or optionally-substituted guanidino; or R3—X— is hydrogen or an electron pair; R4 is oxygen or —NR9R10; R5 is cycloalkyl, aryl, heteroaryl, cycloalkylalkyl, aralkyl, heteroarylalkyl, or a saturated or partially unsaturated heterocycle, each of which is optionally substituted; and R6, R7 and R8 are independently hydrogen, alkyl, cycloalkyl, aryl, heteroaryl, a saturated or partially unsaturated heterocycle, cycloalkylalkyl, aralkyl or heteroarylalkyl, each of which is optionally substituted; or R6 and R7, together with the carbon atom to which they are attached form a 3- to 7-membered carbocyclic ring optionally substituted 1 to 3 times with Ra.

    摘要翻译： 本发明涉及新的1,4-二氮杂，其药物组合物及其作为HDM2-p53相互作用抑制剂的用途。 化合物具有式I：或其溶剂合物，水合物或其药学上可接受的盐; 其中：R 1，R 2，R 9，R 10，R SUP， >，R d和M在本文中定义; X是二价基团：烷烃，环烷烃，任选取代的芳烃，任选取代的杂芳烃，任选取代的芳基烷烃或任选取代的杂芳基烷烃; 和R 3是-CO 2 R 2，-CO 2 M，-OH，-NHR 0 任选取代的脒基或任选取代的胍基;其中R 1，R 2，R 3，R 4， 或R 3 -X-是氢或电子对; R 4是氧或-NR 9 R 10; R 5是环烷基，芳基，杂芳基，环烷基烷基，芳烷基，杂芳基烷基或饱和或部分不饱和的杂环，其各自任选被取代; R 6和R 8独立地是氢，烷基，环烷基，芳基，杂芳基，饱和或部分不饱和的杂环，环烷基烷基 ，芳烷基或杂芳基烷基，其各自任选被取代; 或R 6和R 7与它们所连接的碳原子一起形成3-至7-元碳环，任选地被R 1取代1至3倍， SUP> a 。

    Aminoguanidines and alkoxyguanidines as protease inhibitors
    10.
    发明授权
    Aminoguanidines and alkoxyguanidines as protease inhibitors 有权
    氨基胍和烷氧基胍作为蛋白酶抑制剂

    公开(公告)号：US06638931B1

    公开(公告)日：2003-10-28

    申请号：US09722363

    申请日：2000-11-28

    申请人： Bruce E. Tomczuk ,  Richard M. Soll ,  Tianbao Lu ,  Cynthia L. Fedde ,  Carl R. Illig ,  Thomas P. Markotan ,  Thomas P. Stagnaro

    发明人： Bruce E. Tomczuk ,  Richard M. Soll ,  Tianbao Lu ,  Cynthia L. Fedde ,  Carl R. Illig ,  Thomas P. Markotan ,  Thomas P. Stagnaro

    IPC分类号： A61K31255

    CPC分类号： C07C309/73 ,  C07C309/75 ,  C07C309/76 ,  C07C309/77 ,  C07C311/16 ,  C07C311/17 ,  C07C311/18 ,  C07C311/19 ,  C07C311/21 ,  C07C317/14 ,  C07C323/66 ,  C07C2601/02 ,  C07C2601/14 ,  C07D211/96 ,  C07D213/42 ,  C07D213/74 ,  C07D215/36 ,  C07D217/02 ,  C07D217/22 ,  C07D239/42 ,  C07D295/13 ,  C07D295/26 ,  C07D307/66

    摘要： Aminoguanidine and alkoxyguanidine compounds, including compounds of the formula: wherein X is O or NR9 and R1-R4, R6-R9, R11, R12, 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 are described. Also described are methods for preparing the compounds of Formula I. The novel compounds of the present 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, 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, comprising a compound of the invention in a pharmaceutically acceptable carrier. 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.

    摘要翻译： 氨基胍和烷氧基胍化合物，包括下式的化合物：其中X是O或NR 9和R 1 -R 4，R 6 -R 9，R 11，R 12， 说明书中列出的R a，R b，R c，Y，Z，n和m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是 描述。 还描述了制备式I化合物的方法。本发明的新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，例如胰凝乳蛋白酶，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，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，其包含本发明化合物在药学上可接受的载体中。 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。