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1. 发明申请

WO03005960A3 NOVEL BICYCLIC AND TRICYCLIC CANNABINOIDS 审中-公开
标题翻译：新型双环和三聚氰胺
公开(公告)号：WO03005960A3
公开(公告)日：2003-06-19
申请号：PCT/US0221961
申请日：2002-07-11
申请人： UNIV CONNECTICUT , MAKRIYANNIS ALEXANDROS , NIKAS SPYRIDON P , KHANOLKAR ATMARAM D
发明人： MAKRIYANNIS ALEXANDROS , NIKAS SPYRIDON P , KHANOLKAR ATMARAM D
IPC分类号： A61K31/122 , A61K31/352 , A61K31/385 , A61P1/08 , A61P5/00 , A61P9/00 , A61P9/02 , A61P15/00 , A61P17/00 , A61P25/02 , A61P25/04 , A61P25/08 , A61P25/14 , A61P25/16 , A61P25/18 , A61P25/24 , A61P25/28 , A61P27/06 , A61P29/00 , A61P31/18 , A61P37/02 , A61P39/02 , A61P43/00 , C07C37/50 , C07C39/19 , C07C45/54 , C07C49/747 , C07D311/80 , C07D339/06 , C07D409/04 , C07D409/06 , C07C49/115 , A61K31/35 , C07C49/215 , C07C49/23 , C07C49/796 , C07C49/83 , C07D311/78
CPC分类号： C07D409/04 , C07C37/055 , C07C39/23 , C07C45/54 , C07C49/747 , C07C2601/08 , C07D311/80 , C07D339/06 , C07D409/06 , C07C39/17 , C07C39/18
摘要： Novel bicyclic-cannabinoids and hexahydrocannabinol analogs are presented. These 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 useful to treat a number of physiological conditions.
摘要翻译：提出了新的双环大麻素和六氢大麻酚类似物。当以治疗有效量施用于个体或动物时，这些化合物导致个体或动物中该化合物足够高的水平以引起生理反应。生理反应可用于治疗许多生理条件。

2. 发明申请

WO2008013963A3 FATTY ACID AMIDE HYDROLASE INHIBITORS 审中-公开
标题翻译：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。

4. 发明公开

EP1414775A4 NOVEL BICYCLIC AND TRICYCLIC CANNABINOIDS 有权
标题翻译： NEAC BICYCLISCHE UND TRICYCLISCHE CANNABINOIDE
公开(公告)号：EP1414775A4
公开(公告)日：2005-06-29
申请号：EP02749947
申请日：2002-07-11
申请人： UNIV CONNECTICUT
发明人： MAKRIYANNIS ALEXANDROS , NIKAS SPYRIDON P , KHANOLKAR ATMARAM D
IPC分类号： A61K31/122 , A61K31/352 , A61K31/385 , A61P1/08 , A61P5/00 , A61P9/00 , A61P9/02 , A61P15/00 , A61P17/00 , A61P25/02 , A61P25/04 , A61P25/08 , A61P25/14 , A61P25/16 , A61P25/18 , A61P25/24 , A61P25/28 , A61P27/06 , A61P29/00 , A61P31/18 , A61P37/02 , A61P39/02 , A61P43/00 , C07C37/50 , C07C39/19 , C07C45/54 , C07C49/747 , C07D311/80 , C07D339/06 , C07D409/04 , C07D409/06 , C07C49/115 , A61K31/35 , C07C49/215 , C07C49/23 , C07C49/796 , C07C49/83 , C07D311/78
CPC分类号： C07D409/04 , C07C37/055 , C07C39/23 , C07C45/54 , C07C49/747 , C07C2601/08 , C07D311/80 , C07D339/06 , C07D409/06 , C07C39/17 , C07C39/18

5. 发明专利

CA2658887C FATTY ACID AMIDE HYDROLASE INHIBITORS 未知
公开(公告)号：CA2658887C
公开(公告)日：2016-08-23
申请号：CA2658887
申请日：2007-07-27
申请人： UNIV CONNECTICUT
发明人： MAKRIYANNIS ALEXANDROS , NIKAS SPYRIDON P , ALAPAFUJA SHAKIRU O , SHUKLA VIDYANAND G
IPC分类号： C07C49/255 , A61K31/10 , A61K31/12 , A61K31/222 , A61K31/27 , A61K31/4245 , A61K31/428 , A61K31/4402 , C07C49/84 , C07C69/738 , C07C271/06 , C07C317/10 , C07C317/18 , C07D213/50 , C07D271/10 , C07D275/06
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.

6. 发明专利

AU2004200538B2 Novel bicyclic and tricyclic cannabinoids 未知
公开(公告)号：AU2004200538B2
公开(公告)日：2008-08-21
申请号：AU2004200538
申请日：2004-02-12
申请人： UNIV CONNECTICUT
发明人： NIKAS SPYRIDON P , MAKRIYANNIS ALEXANDROS , KHANOLKAR ATMARAM D
IPC分类号： C07D409/06 , C07C45/54 , C07D311/80 , C07D339/06 , C07D409/04

7. 发明专利

CA2658887A1 FATTY ACID AMIDE HYDROLASE INHIBITORS 未知
公开(公告)号：CA2658887A1
公开(公告)日：2008-01-31
申请号：CA2658887
申请日：2007-07-27
申请人： UNIV CONNECTICUT
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
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 endoge nous 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 activati on 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 hydrol ase (FAAH) action is not inhibited. Thus, a compound that inhibits the inact ivation of endogenous cannabinoid ligands by fatty acid amide hydrolase (FAA H) may increase the levels of endocannabinoids and, thus, enhance the activa tion of cannabinoid receptors. Thus, the compound may not directly modulate the cannabinoid receptors but has the effect of indirectly stimulating the c annabinoid receptors by increasing the levels of endocannabinoid ligands. It may also enhance the effects and duration of action of other exogenous cann abinergic ligands that are administered in order to elicit a cannabinergic r esponse.

9. 发明专利

CA2452881C NOVEL BICYCLIC AND TRICYCLIC CANNABINOIDS 未知
公开(公告)号：CA2452881C
公开(公告)日：2012-03-06
申请号：CA2452881
申请日：2002-07-11
申请人： UNIV CONNECTICUT
发明人： MAKRIYANNIS ALEXANDROS , NIKAS SPYRIDON P , KHANOLKAR ATMARAM D
IPC分类号： C07C49/115 , A61K31/122 , A61K31/35 , A61K31/352 , A61K31/385 , A61P1/08 , A61P5/00 , A61P9/00 , A61P9/02 , A61P15/00 , A61P17/00 , A61P25/02 , A61P25/04 , A61P25/08 , A61P25/14 , A61P25/16 , A61P25/18 , A61P25/24 , A61P25/28 , A61P27/06 , A61P29/00 , A61P31/18 , A61P37/02 , A61P39/02 , A61P43/00 , C07C37/50 , C07C39/19 , C07C45/54 , C07C49/215 , C07C49/23 , C07C49/747 , C07C49/796 , C07C49/83 , C07D311/78 , C07D311/80 , C07D339/06 , C07D409/04 , C07D409/06
摘要： Novel bicyclic-cannabinoids and hexahydrocannabinol analogs according to formula 1 are presented. These 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 useful to treat a number of physiological conditions (see formula I)

10. 发明专利

AU2004200538A1 Novel bicyclic and tricyclic cannabinoids 未知
公开(公告)号：AU2004200538A1
公开(公告)日：2004-03-11
申请号：AU2004200538
申请日：2004-02-12
申请人： UNIV CONNECTICUT
发明人： KHANOLKAR ATMARAM D , NIKAS SPYRIDON P , MAKRIYANNIS ALEXANDROS
IPC分类号： C07C45/54 , C07D311/80 , C07D339/06 , C07D409/04 , C07D409/06

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