Method for treating and preventing inflammation and atherosclerosis
    2.
    发明授权
    Method for treating and preventing inflammation and atherosclerosis 失效
    治疗和预防炎症和动脉粥样硬化的方法

    公开(公告)号:US6001866A

    公开(公告)日:1999-12-14

    申请号:US51002

    申请日:1998-03-20

    CPC分类号: A61K31/454 A61K31/40

    摘要: This invention provides a method for treating or preventing inflammation or atherosclerosis in mammals comprising administering an effective amount of a 15-LO inhibitor of Formula I: ##STR1## wherein: R.sup.1 is hydrogen or C.sub.1 -C.sub.6 alkyl;R.sup.2, R.sup.3, R.sup.4, and R.sup.5 independently are hydrogen, C.sub.1 -C.sub.6 alkyl, nitro, halo, CN, OR.sup.6, NR.sup.6 R.sup.7, --CO.sub.2 R.sup.6, CONR.sup.6 R.sup.7, CH.sub.2 OR.sup.6, or CH.sub.2 NR.sup.6 R.sup.7, and R.sup.2 and R.sup.3, and R.sup.4 and R.sup.5, when attached to adjacent ring atoms, can be --(CH.sub.2).sub.3 or 4 --;in which R.sup.6 and R.sup.7 independently are hydrogen, C.sub.1 -C.sub.6 alkyl, phenyl or benzyl, and when taken together with the nitrogen to which they are attached, R.sup.6 and R.sup.7 can complete a cyclic ring having from 3 to 7 carbon atoms; ##STR2## in which R.sup.8, R.sup.8', R.sup.9, and R.sup.9' independently are hydrogen or C.sub.1 -C.sub.6 alkyl, n is 0, 1, or 2, and Z.sup..crclbar. is an anion, and pharmaceutically acceptable salts thereof.

    摘要翻译: PCT No.PCT / US96 / 14242 Sec。 371日期:1998年3月20日 102(e)1998年3月20日PCT PCT 1996年9月5日PCT公布。 公开号WO97 / 12613 日本1997年4月10日本发明提供了治疗或预防哺乳动物炎症或动脉粥样硬化的方法,其包括给予有效量的式I的15-LO抑制剂:其中:R1是氢或C1-C6烷基; R2,R3,R4和R5独立地是氢,C1-C6烷基,硝基,卤素,CN,OR6,NR6R7,-CO2R6,CONR6R7,CH2OR6或CH2NR6R7,R2和R3,R4和R5连接到 相邻的环原子可以是 - (CH 2)3或4-; 其中R6和R7独立地是氢,C1-C6烷基,苯基或苄基,当与它们所连接的氮一起时,R6和R7可以完成具有3至7个碳原子的环; 其中R8,R8',R9和R9'独立地是氢或C1-C6烷基,n是0,1或2,并且Z( - )是一个阴离子,及其药学上可接受的盐。

    Coumarin derivatives as protease inhibitors and antiviral agents
    4.
    发明授权
    Coumarin derivatives as protease inhibitors and antiviral agents 失效
    香豆素衍生物作为蛋白酶抑制剂和抗病毒剂

    公开(公告)号:US5510375A

    公开(公告)日:1996-04-23

    申请号:US155728

    申请日:1993-11-19

    IPC分类号: C07D311/56 A61K31/35

    CPC分类号: C07D311/56

    摘要: The present invention relates to novel coumarin derivatives and related compounds which potently inhibit the HIV aspartyl protease blocking HIV infectivity. The coumarin derivatives are useful in the development of therapies for the treatment of viral infections and diseases, including AIDS. The present invention is also directed to methods of synthesis of multifunctionalized coumarins and of related structures.

    摘要翻译: 本发明涉及有效抑制HIV天冬氨酰蛋白酶阻断HIV感染性的新型香豆素衍生物和相关化合物。 香豆素衍生物可用于开发用于治疗病毒感染和疾病(包括AIDS)的治疗。 本发明还涉及多功能香豆素的合成方法和相关结构。

    Tricyclic pyrone derivatives as protease inhibitors and antiviral agents
    5.
    发明授权
    Tricyclic pyrone derivatives as protease inhibitors and antiviral agents 失效
    三环吡喃酮衍生物作为蛋白酶抑制剂和抗病毒剂

    公开(公告)号:US5504104A

    公开(公告)日:1996-04-02

    申请号:US155412

    申请日:1993-11-19

    摘要: The present invention relates to novel substituted tricyclic pyrones and related structures which potently inhibit the HIV aspartyl protease blocking HIV infectivity. The tricyclic pyrone derivatives are useful in the development of therapies for the treatment of vital infections and diseases, including AIDS. The present invention is also directed to methods of synthesis of multifunctionalized tricyclic pyrones and of related structures.

    摘要翻译: 本发明涉及新型取代的三环pyrones和有效抑制HIV天冬氨酰蛋白酶阻断HIV感染性的相关结构。 三环吡喃酮衍生物可用于开发用于治疗重要感染和疾病(包括AIDS)的治疗。 本发明还涉及合成多功能三环pyrones和相关结构的方法。