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    FATTY ACID AMIDE HYDROLASE INHIBITORS
    3.
    发明申请
    FATTY ACID AMIDE HYDROLASE INHIBITORS 审中-公开
    脂肪酸酰胺水解酶抑制剂

    公开(公告)号：WO2008013963A3

    公开(公告)日：2008-11-27

    申请号：PCT/US2007016953

    申请日：2007-07-27

    申请人： UNIV CONNECTICUT ,  MAKRIYANNIS ALEXANDROS ,  NIKAS SPYRIDON P ,  ALAPAFUJA SHAKIRU O ,  SHUKLA VIDYANAND G

    发明人： MAKRIYANNIS ALEXANDROS ,  NIKAS SPYRIDON P ,  ALAPAFUJA SHAKIRU O ,  SHUKLA VIDYANAND G

    IPC分类号： C07D213/02 ,  A61K31/4245 ,  A61K31/425 ,  A61K31/44 ,  C07C233/02 ,  C07D271/06 ,  C07D277/02

    CPC分类号： C07D213/75 ,  C07C17/16 ,  C07C45/41 ,  C07C45/44 ,  C07C45/45 ,  C07C45/673 ,  C07C49/233 ,  C07C49/255 ,  C07C49/84 ,  C07C69/712 ,  C07C69/738 ,  C07C271/12 ,  C07C271/14 ,  C07C271/16 ,  C07C271/24 ,  C07C271/38 ,  C07C271/58 ,  C07C309/68 ,  C07C309/81 ,  C07C309/82 ,  C07C2601/14 ,  C07C2603/74 ,  C07D213/30 ,  C07D213/40 ,  C07D213/50 ,  C07D263/56 ,  C07D271/10 ,  C07D275/06 ,  C07D277/64 ,  C07C22/04 ,  C07C47/277 ,  C07C47/575 ,  C07C49/83

    摘要： Disclosed are compounds of formula R-X-Y that may be used to inhibit the action of fatty acid amide hydrolase (FAAH). Inhibition of fatty acid amide hydrolase (FAAH) will slow the normal degradation and inactivation of endogenous cannabinoid ligands by FAAH hydrolysis and allow higher levels of those endogenous cannabinergic ligands to remain present. These higher levels of endocannabinoid ligands provide increased stimulation of the cannabinoid CBl and CB2 receptors and produce physiological effects related to the activation of the cannabinoid receptors. They will also enhance the effects of other exogenous cannabinergic ligands and allow them to produce their effects at lower concentrations as compared to systems in which fatty acid amide hydrolase (FAAH) action is not inhibited. Thus, a compound that inhibits the inactivation of endogenous cannabinoid ligands by fatty acid amide hydrolase (FAAH) may increase the levels of endocannabinoids and, thus, enhance the activation of cannabinoid receptors. Thus, the compound may not directly modulate the cannabinoid receptors but has the effect of indirectly stimulating the cannabinoid receptors by increasing the levels of endocannabinoid ligands. It may also enhance the effects and duration of action of other exogenous cannabinergic ligands that are administered in order to elicit a cannabinergic response.

    摘要翻译： 公开了可用于抑制脂肪酸酰胺水解酶（FAAH）作用的式R-X-Y的化合物。 脂肪酸酰胺水解酶（FAAH）的抑制将通过FAAH水解减缓内源性大麻素配体的正常降解和失活，并允许更高水平的那些内源性大麻素能配体保持存在。 这些更高水平的内源性大麻素配体提供对大麻素CB1和CB2受体的增加的刺激，并产生与大麻素受体活化相关的生理作用。 它们还将增强其他外源性大麻素能配体的作用，并允许它们在不抑制脂肪酸酰胺水解酶（FAAH）作用的体系下，以较低的浓度产生其作用。 因此，通过脂肪酰胺水解酶（FAAH）抑制内源性大麻素配体失活的化合物可能增加内源性大麻素的含量，从而增强大麻素受体的活化。 因此，化合物不能直接调节大麻素受体，而是通过增加内源性大麻素配体的水平来间接刺激大麻素受体的作用。 它还可以增强其它外源性大麻素能配体的作用和持续时间，以引发大麻素应答。