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    Broadspectrum heterocyclic substituted phenyl containing sulfonamide HIV protease inhibitors
    31.
    发明授权
    Broadspectrum heterocyclic substituted phenyl containing sulfonamide HIV protease inhibitors 失效
    支链杂环取代苯基含磺酰胺HIV蛋白酶抑制剂

    公开(公告)号：US07763641B2

    公开(公告)日：2010-07-27

    申请号：US10499221

    申请日：2002-12-20

    申请人： Sandrine Marie Helene Vendeville ,  Wim Gaston Verschueren ,  Abdellah Tahri ,  Samuel Leo Christiaan Moors ,  Montserrat Erra Sola

    发明人： Sandrine Marie Helene Vendeville ,  Wim Gaston Verschueren ,  Abdellah Tahri ,  Samuel Leo Christiaan Moors ,  Montserrat Erra Sola

    IPC分类号： A61K31/42 ,  A61K31/44 ,  A61K31/425 ,  C07D277/54

    CPC分类号： C07D231/12 ,  C07C311/18 ,  C07C2603/18 ,  C07D233/64 ,  C07D233/88 ,  C07D263/32 ,  C07D277/40 ,  C07D277/42 ,  C07D277/46 ,  C07D417/04 ,  C07D417/12 ,  C07D417/14 ,  C07D493/04 ,  C07D513/04

    摘要： The present invention concerns the compounds having the formula (I), N-oxides, salt, stereoisomeric forms, racemic mixtures, prodrugs, esters and metabolites thereof, wherein Haryl is an aromatic monocyclic, bicyclic or tricyclic heterocycle having 3 to 14 ring members which contains one or more heteroatom ring members selected from nitrogen, oxygen and sulfur and which may optionally be substituted on (i) one or more carbon atoms by C1-6alkyl, halogen, hydroxy, optionally mono- or disubstituted amino, nitro, cyano, haloC1-6alkyl, carboxyl, C3-7cycloalkyl, optionally mono- or disubstituted aminocarbonyl, methylthio, methylsulfonyl, aryl, —(R7a)n—M—R7b, Het1 and Het2; whereby the optional substituents on any amino function are independently selected from R5 and —A—R6; and on (ii) a nitrogen atom if present by hydroxy or —A—R6. It further relates to their use as broadspectrum HIV protease inhibitors, processes for their preparation as well as pharmaceutical compositions and diagnostic kits comprising them. It also concerns combinations thereof with another anti-retroviral agent, and to their use in assays as reference compounds or as reagents.

    摘要翻译： 本发明涉及具有式（I）的化合物，N-氧化物，盐，立体异构形式，外消旋混合物，前药，酯和代谢物，其中Haryl是具有3至14个环成员的芳族单环，双环或三环杂环， 含有一个或多个选自氮，氧和硫的杂原子环成员，并且其可任选地在（i）一个或多个碳原子上被C 1-6烷基，卤素，羟基，任选单或二取代的氨基，硝基，氰基，卤代 烷基，羧基，C 3-7环烷基，任选的单或二取代的氨基羰基，甲硫基，甲基磺酰基，芳基， - （R 7a）n-M-R 7b，Het 1和Het 2; 其中任何氨基官能团上的任选取代基独立地选自R5和-A-R6; 和（ii）如果存在羟基或-A-R 6的氮原子。 它还涉及它们作为广谱的HIV蛋白酶抑制剂，其制备方法以及药物组合物和包含它们的诊断试剂盒的用途。 它还涉及与另一种抗逆转录病毒剂的组合，以及它们在测定中用作参考化合物或作为试剂。

    REMEDY FOR OVERACTIVE BLADDER COMPRISING ACETIC ACID ANILIDE DERIVATIVE AS THE ACTIVE INGREDIENT
    37.
    发明申请
    REMEDY FOR OVERACTIVE BLADDER COMPRISING ACETIC ACID ANILIDE DERIVATIVE AS THE ACTIVE INGREDIENT 审中-公开
    用于包含作为活性成分的乙酸酰胺衍生物的超级叶片的补救

    公开(公告)号：US20090093529A1

    公开(公告)日：2009-04-09

    申请号：US12333357

    申请日：2008-12-12

    申请人： Toshiyuki Takasu ,  Shuichi Sato ,  Masashi Ukai ,  Tatsuya Maruyama

    发明人： Toshiyuki Takasu ,  Shuichi Sato ,  Masashi Ukai ,  Tatsuya Maruyama

    IPC分类号： A61K31/426 ,  A61P13/10

    CPC分类号： A61K31/426 ,  C07D277/40

    摘要： (R)-2-(2-aminothiazol-4-yl)-4′-[2-[(2-hydroxy-2-phenylethyl)amino]ethyl]acetic acid anilide or its salt shows a potent bladder relaxation effect in “isolated rat bladder smooth muscle relaxation test”, dose-dependently lowers the contraction frequency of rhythmic bladder contractions in “rat rhythmic bladder contraction measurement test” and, moreover, prolongs the urination intervals in “urination functions measurement test on cyclophosphamide-induced overactive bladder model rat”. Owing to these effects, the above compound is useful as a remedy for overactive bladder.

    摘要翻译： （R）-2-（2-氨基噻唑-4-基）-4' - [2 - [（2-羟基-2-苯乙基）氨基]乙基]乙酰苯胺或其盐在“ 孤立的大鼠膀胱平滑肌松弛试验“，在”大鼠节律性膀胱收缩测定试验“中剂量依赖性地降低了节律性膀胱收缩的收缩频率，此外，在”环磷酰胺诱导的膀胱过度活动膀胱模型的排尿功能测量试验“中延长了排尿间隔 鼠”。 由于这些效果，上述化合物可用作膀胱过度活动症的补救剂。

    TARGETED BONE MARROW PROTECTION AGENTS
    38.
    发明申请
    TARGETED BONE MARROW PROTECTION AGENTS 审中-公开
    目标骨骼保护剂

    公开(公告)号：US20090011975A1

    公开(公告)日：2009-01-08

    申请号：US12183813

    申请日：2008-07-31

    申请人： Joseph R. Garlich ,  Donald L. Durden ,  Tim C. Smith

    发明人： Joseph R. Garlich ,  Donald L. Durden ,  Tim C. Smith

    IPC分类号： A61K31/663 ,  A61K31/428 ,  A61K31/429 ,  A61K38/02 ,  C07D513/04 ,  C07F9/6539 ,  C07D277/38 ,  C07D277/82 ,  A61P35/00

    CPC分类号： C07D513/04 ,  A61K31/428 ,  A61K31/429 ,  A61K31/662 ,  A61K31/663 ,  A61K41/00 ,  C07D277/40

    摘要： The invention provides a method of inhibiting cell death in a mammal. The method comprises administering to a mammal an effective amount of a composition comprising a cell protection factor covalently linked to a bone targeting agent via a linkage that is cleaved under physiological conditions, whereby the cell protection factor is released from the bone targeting agent in vivo to inhibit cell death. The invention further provides a compound comprising a cell protection factor covalently attached to a bone targeting agent via a linker that is cleaved under physiological conditions.

    摘要翻译： 本发明提供一种抑制哺乳动物细胞死亡的方法。 该方法包括向哺乳动物施用有效量的组合物，其包含通过在生理条件下被切割的连接物与骨靶向剂共价连接的细胞保护因子，由此细胞保护因子在体内从骨靶向剂释放到 抑制细胞死亡。 本发明还提供一种化合物，其包含通过在生理条件下切割的接头共价连接至骨靶向剂的细胞保护因子。