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    ANGIOGENIC RESORCINOL DERIVATIVES
    2.
    发明申请
    ANGIOGENIC RESORCINOL DERIVATIVES 审中-公开
    生殖因子衍生物

    公开(公告)号：WO2011006099A1

    公开(公告)日：2011-01-13

    申请号：PCT/US2010/041575

    申请日：2010-07-09

    申请人： NORTHEASTERN UNIVERSITY ,  MAKRIYANNIS, Alexandros ,  NIKAS, Spyridon, P. ,  ALAPAFUJA, Shakiru, O.

    发明人： MAKRIYANNIS, Alexandros ,  NIKAS, Spyridon, P. ,  ALAPAFUJA, Shakiru, O.

    IPC分类号： A61K8/00 ,  A61K8/18

    CPC分类号： C07C39/42 ,  C07B57/00 ,  C07B59/001 ,  C07B2200/05 ,  C07B2200/07 ,  C07C39/23 ,  C07C69/732 ,  C07C247/10 ,  C07C255/36 ,  C07C2601/16 ,  C07C2602/42

    摘要： Novel resorcinol derivatives and methods of preparation and use are presented. These compounds can stimulate angiogenesis as a biological function triggered by the activation of one cannabinoid receptor distinct from CB1 and CB2. Thus, these compounds are specific ligands for one cannabinoid receptor distinct from CB1 and CB2. The invented compounds, when administered in a therapeutically effective amount to an individual or animal, results in a sufficiently high level of that compound in the individual or animal to cause a physiological response. The physiological response may be useful to treat a number of physiological conditions.

    摘要翻译： 介绍了新型间苯二酚衍生物及其制备方法。 这些化合物可以刺激血管发生，作为一种不同于CB1和CB2的一种大麻素受体激活引发的生物学功能。 因此，这些化合物是与CB1和CB2不同的一种大麻素受体的特异性配体。 当以治疗有效量施用于个体或动物时，本发明的化合物在个体或动物中导致足够高的该化合物水平以引起生理反应。 生理反应可用于治疗许多生理条件。

    FATTY ACID AMIDE HYDROLASE INHIBITORS
    5.
    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。

    FATTY ACID AMIDE HYDROLASE INHIBITORS
    6.
    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：WO2008013963A2

    公开(公告)日：2008-01-31

    申请号：PCT/US2007/016953

    申请日：2007-07-27

    申请人： UNIVERSITY OF 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： A61K31/4745

    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 hot 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。 与其中脂肪酰胺水解酶（FAAH）作用被热抑制的系统相比，它们还将增强其他外源性大麻素配体的作用，并使它们以较低的浓度产生它们的作用。 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。