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    Fused-ring heterocycles for the treatment of atherosclerosis
    2.
    发明授权
    Fused-ring heterocycles for the treatment of atherosclerosis 失效
    用于治疗动脉粥样硬化的融合环杂环

    公开(公告)号：US5478830A

    公开(公告)日：1995-12-26

    申请号：US889892

    申请日：1992-05-29

    申请人： C. Anne Higley ,  Ruth R. Wexler ,  Richard G. Wilde

    发明人： C. Anne Higley ,  Ruth R. Wexler ,  Richard G. Wilde

    IPC分类号： C07D487/04 ,  A61K31/44 ,  A61K31/505 ,  A61K31/52

    CPC分类号： C07D487/04

    摘要： This invention relates to pyrazolo pyrimidines for the treatment of atherosclerosis as inhibitors of acyl--CoA, cholesterol acyetransferase (ACAT), and their use as antihypercholesterolemic agents, pharmaceutical compositions and preparation, and having the formula (I): ##STR1## wherein: A and Q are selected independently from CH or N with no more than two nitrogens per ring:D, E, and G are selected independently from CR.sup.1 or N with no more than two nitrogens per ring;X is S(O).sub.r, O, NR.sup.4 or CH.sup.2 ;J is C.sub.2 -C.sub.10 alkyl, C.sub.3 -C.sub.10 branched alkyl, C.sub.3 -C.sub.10 alkenyl or C.sub.3 -C.sub.10 alkynyl;Y is O, S, H.sub.2 or NH:Z is NHR.sup.3, OR.sup.3 or R.sup.3 :R.sup.1 is selected independently from H, NO.sub.2, Br, Cl, F, CF.sub.3, CN, CH.sub.3 S(O).sub.r, C.sub.1 -C.sub.8 alkyl or alloxy, C.sub.3 -C.sub.8, branched alkyl, C.sub.1 -C.sub.4 carboalkoxy, NR.sup.5 R.sup.6 or NR.sup.5 COR.sup.6 ;R.sup.2 is C.sub.1 -C.sub.8 alkyl, C.sub.3 -C.sub.8 branched alkyl, C.sub.3 -C.sub.7 cycloalkyl, C.sub.3 -C.sub.8 alkenyl or alkynyl, C.sub.7 -C.sub.14 araalkyl where the aryl group is optionally substituted; phenyl optionally substituted benzyl optionally substituted 2-, 3-, or 4- pyridinyl, pyrimidinyl: or biphenyl:R.sup.3 is C.sub.1 -C.sub.8 alkyl, C.sub.3 -C.sub.8 branched alkyl, C.sub.3 -C.sub.7 cycloalkyl, C.sub.4 -C.sub.10 cycloallylalkyl, C.sub.3 -C.sub.6 alkenyl or alkynyl, C.sub.1 -C.sub.3 perfluoroalkyl, C.sub.7 -C.sub.14 araalkyl where the aryl group is optionally substituted phenyl optionally substituted benzyl optionally substituted 2-, 3-, or 4- pyridinyl, pyrimidinyl; or biphenyl:R.sup.4 is H, C.sub.1 -C.sub.6 alkyl or benzyl;R.sup.5 and R.sup.6 are selected independently from H or C.sub.1 -C.sub.4 alkyl;r is 0 to 2:or a pharmaceutically acceptable salt thereof.

    摘要翻译： 本发明涉及用于治疗动脉粥样硬化的吡唑并嘧啶作为酰基辅酶A，胆固醇转氨酶（ACAT）的抑制剂及其作为抗高胆固醇血症药物，药物组合物和制剂的用途，并具有式（I）：其中： A和Q独立地选自CH或N，每个环不多于两个氮：D，E和G独立地选自CR1或N，每个环不多于两个氮; X是S（O）r，O，NR 4或CH 2; J是C 2 -C 10烷基，C 3 -C 10支链烷基，C 3 -C 10链烯基或C 3 -C 10炔基; Y是O，S，H2或NH：Z是NHR3，OR3或R3：R1独立地选自H，NO2，Br，Cl，F，CF3，CN，CH3S（O）r，C1-C8烷基或烯氧基， C3-C8，支链烷基，C1-C4烷氧羰基，NR5R6或NR5COR6; R2是C1-C8烷基，C3-C8支链烷基，C3-C7环烷基，C3-C8链烯基或炔基，其中芳基任选被取代的C7-C14芳烷基; 苯基任选取代的苄基任选取代的2-，3-或4-吡啶基，嘧啶基或联苯基：R3是C1-C8烷基，C3-C8支链烷基，C3-C7环烷基，C4-C10环烯基烷基，C3-C6烯基或 炔基，C1-C3全氟烷基，C7-C14芳烷基，其中芳基是任选取代的苯基任选取代的苄基任选取代的2-，3-或4-吡啶基，嘧啶基; 或联苯基：R 4是H，C 1 -C 6烷基或苄基; R 5和R 6独立地选自H或C 1 -C 4烷基; r为0〜2：或其药学上可接受的盐。

    HETEROCYCLIC INHIBITORS OF BACTERIAL PEPTIDYL TRNA HYDROLASE AND USES THEREOF
    6.
    发明申请
    HETEROCYCLIC INHIBITORS OF BACTERIAL PEPTIDYL TRNA HYDROLASE AND USES THEREOF 审中-公开
    细菌肽类TRNA水解物的杂环抑制剂及其用途

    公开(公告)号：US20100069380A1

    公开(公告)日：2010-03-18

    申请号：US12441929

    申请日：2007-09-21

    申请人： Soongyu Choi ,  Arthur Branstrom ,  Scott A. Gothe ,  Richard Lipman ,  Tamil Arasu ,  Richard G. Wilde

    发明人： Soongyu Choi ,  Arthur Branstrom ,  Scott A. Gothe ,  Richard Lipman ,  Tamil Arasu ,  Richard G. Wilde

    IPC分类号： C07D491/052 ,  A61K31/5377 ,  A61K31/4741 ,  C07D491/22 ,  C07D491/16 ,  A61P31/04 ,  A61K31/4743 ,  A61K31/506 ,  C07D491/147 ,  C07D491/153 ,  A61K31/4375

    CPC分类号： C07D417/04 ,  C07D413/14 ,  C07D417/14 ,  C07D419/14 ,  C07D487/04

    摘要： Provided herein are compounds that modulate the activity of a bacterial peptidyl tRNA hydrolase, including compositions and dosage forms comprising the compounds. Further provided herein are methods for screening and identifying compounds that modulate the activity of a bacterial peptidyl tRNA hydrolase. In particular, provided herein are assays for the identification of compounds that inhibit or reduce the activity of a bacterial peptidyl tRNA hydrolase. The methods provided herein provide a simple, sensitive assay for high-throughput screening of libraries of compounds to identify pharmaceutical leads useful for preventing, treating, and managing a bacterial infection or one or more symptoms thereof. Further provided herein are methods for preventing or inhibiting bacterial proliferation as well as methods for preventing, treating, and/or managing a bacterial infection using such compounds and compositions.

    摘要翻译： 本文提供调节细菌肽基tRNA水解酶的活性的化合物，包括组合物和包含该化合物的剂型。 本文还提供了筛选和鉴定调节细菌肽基tRNA水解酶活性的化合物的方法。 特别地，本文提供了用于鉴定抑制或降低细菌肽基tRNA水解酶的活性的化合物的测定法。 本文提供的方法提供了一种用于高通量筛选化合物文库的简单敏感测定，以鉴定可用于预防，治疗和管理细菌感染或其一种或多种症状的药物引线。 本文还提供了用于预防或抑制细菌增殖的方法以及使用这些化合物和组合物预防，治疗和/或控制细菌感染的方法。