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    3-(Diarylmethylene)-8-azabicyclo[3.2.1]octane derivatives
    1.
    发明授权
    3-(Diarylmethylene)-8-azabicyclo[3.2.1]octane derivatives 有权
    3-（二芳基亚甲基）-8-氮杂双环[3.2.1]辛烷衍生物

    公开(公告)号：US06552036B2

    公开(公告)日：2003-04-22

    申请号：US09791246

    申请日：2001-02-22

    申请人： Robert E. Boyd ,  John R. Carson ,  Steven J. Coats ,  Lou Anne Neilson ,  Philip M Pitis ,  Wu-Nan Wu

    发明人： Robert E. Boyd ,  John R. Carson ,  Steven J. Coats ,  Lou Anne Neilson ,  Philip M Pitis ,  Wu-Nan Wu

    IPC分类号： C07D45102

    CPC分类号： C07D451/02 ,  A61K31/439

    摘要： This invention is directed to 3-(diarylmethylene)-8-azabicyclo[3.2.1]octane derivatives useful as &dgr;-opioid or &mgr;-opioid receptor modulators. Depending on their agonist or antagonist effect, the compounds are useful analgesics, immunosuppressants, antiinflammatory agents, agents for the treatment of neurological and psychiatric conditions, medicaments for drug and alcohol abuse, agents for treating gastritis and diarrhea, cardiovascular agents and agents for the treatment of respiratory diseases.

    摘要翻译： 本发明涉及可用作δ-阿片样物质或μ-阿片受体调节剂的3-（二芳基亚甲基）-8-氮杂双环[3.2.1]辛烷衍生物。 根据其激动剂或拮抗剂的作用，化合物是有用的止痛剂，免疫抑制剂，抗炎剂，用于治疗神经和精神病症的药剂，用于药物和酒精滥用的药物，用于治疗胃炎和腹泻的药剂，用于治疗的心血管药剂和药剂 的呼吸系统疾病。

    STEREOSELECTIVE PROCESS FOR PREPARING PURINE DIOXOLANE NUCLEOSIDE DERIVATIVES
    10.
    发明申请
    STEREOSELECTIVE PROCESS FOR PREPARING PURINE DIOXOLANE NUCLEOSIDE DERIVATIVES 审中-公开
    制备嘌呤二氧杂环己烷衍生物的立体选择性方法

    公开(公告)号：US20100210840A1

    公开(公告)日：2010-08-19

    申请号：US12670386

    申请日：2008-07-24

    申请人： Steven J. Coats

    发明人： Steven J. Coats

    IPC分类号： C07D473/16

    CPC分类号： C07D473/16

    摘要： A cost-effective process scale method for preparing purine dioxolane nucleoside derivatives in racemic or optically pure form is disclosed, as are nucleoside derivatives prepared by the method. The method involves reacting a purine or a mono- or polysilylated purine derivative with an activated dioxolane analog to produce the dioxolane nucleoside analog in commercially useful yields. Direct reaction of purine or a mono- or polysilylated purine with dioxolanes takes place with highest reported chemical yields and excellent stereoselectivity when an additive in the form of an alpha cyano carbonyl compound or silylated alpha cyano carbonyl compounds is present in the reaction mixture during the glycosylation reaction.

    摘要翻译： 公开了一种用于制备外消旋或光学纯的形式的嘌呤二氧戊环核苷衍生物的成本有效的工艺规模方法，以及通过该方法制备的核苷衍生物。 该方法包括使嘌呤或单或聚硅酸化嘌呤衍生物与活化的二氧杂环戊烷类似物反应，以商业上有效的收率产生二氧戊环核苷类似物。 在糖基化过程中当反应混合物中存在α氰基羰基化合物或甲硅烷基化α氰基羰基化合物形式的添加剂时，嘌呤或单或多聚化嘌呤与二氧戊环的直接反应发生，报道最高的化学产率和优异的立体选择性 反应。