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1. 发明授权

US08202893B2 Cannabinergic lipid ligands 有权
标题翻译：大麻素类脂质配体
公开(公告)号：US08202893B2
公开(公告)日：2012-06-19
申请号：US11577156
申请日：2005-10-12
申请人： Alexandros Makriyannis , Chen Li , Dai Lu
发明人： Alexandros Makriyannis , Chen Li , Dai Lu
IPC分类号： A61K31/44
CPC分类号： C07C233/21 , C07C233/09 , C07C233/11 , C07C233/29 , C07C233/36 , C07C235/08 , C07C235/28 , C07C235/50 , C07C237/16 , C07C247/08 , C07C255/23 , C07C271/12 , C07C271/16 , C07C271/24 , C07C271/28 , C07C331/22 , C07C2601/02 , C07C2601/04 , C07C2601/14 , C07C2602/42 , C07C2603/74 , C07D277/18 , C07D277/46
摘要： One aspect of this disclosure relates generally to lipid compounds that exert diverse effects in the endocannabinoid system, such as regulating CB1 and CB2 receptor or moderating other bio-macromolecules within the endocannabinoid system. Some of the compounds showed improved receptor binding affinity, and/or improved receptor subtype selectivity, and improved bio-stability. Some of the compounds exhibit activities to regulate the enzymes that moderate the bio-disposal of endogenous cannabinoids, such as the fatty acid amide hydrolase (FAAH). Some of the compounds exhibit activities to inhibit the anandamide transporter. Other aspects of the invention are pharmaceutical preparations employing these ligands and methods of administering therapeutically effective amounts of the preparations to provide a physiological effect.
摘要翻译：本公开的一个方面通常涉及在内源性大麻素系统中发挥不同作用的脂质化合物，例如调节CB1和CB2受体或调节内源性大麻素系统内的其他生物大分子。一些化合物显示改善的受体结合亲和力，和/或改善的受体亚型选择性，以及改进的生物稳定性。一些化合物表现出调节调节内源大麻素的生物处理的酶的活性，例如脂肪酸酰胺水解酶（FAAH）。一些化合物表现出抑制丙二胺转运蛋白的活性。本发明的其它方面是使用这些配体的药物制剂和施用治疗有效量的制剂以提供生理作用的方法。

2. 发明申请

US20090163557A1 Cannabinergic Lipid Ligands 有权
标题翻译：大麻素类脂质配体
公开(公告)号：US20090163557A1
公开(公告)日：2009-06-25
申请号：US11577156
申请日：2005-10-12
申请人： Alexandros Makriyannis , Chen Li , Dai Lu
发明人： Alexandros Makriyannis , Chen Li , Dai Lu
IPC分类号： A61K31/44 , C07C57/00 , A61K31/20 , A61K31/16 , A61K31/22 , A61K31/17 , A61K31/425
CPC分类号： C07C233/21 , C07C233/09 , C07C233/11 , C07C233/29 , C07C233/36 , C07C235/08 , C07C235/28 , C07C235/50 , C07C237/16 , C07C247/08 , C07C255/23 , C07C271/12 , C07C271/16 , C07C271/24 , C07C271/28 , C07C331/22 , C07C2601/02 , C07C2601/04 , C07C2601/14 , C07C2602/42 , C07C2603/74 , C07D277/18 , C07D277/46
摘要： One aspect of this disclosure relates generally to lipid compounds that exert diverse effects in the endocannabinoid system, such as regulating CB1 and CB2 receptor or moderating other bio-macromolecules within the endocannabinoid system. Some of the compounds showed improved receptor binding affinity, and/or improved receptor subtype selectivity, and improved bio-stability. Some of the compounds exhibit activities to regulate the enzymes that moderate the bio-disposal of endogenous cannabinoids, such as the fatty acid amide hydrolase (FAAH). Some of the compounds exhibit activities to inhibit the anandamide transporter. Other aspects of the invention are pharmaceutical preparations employing these ligands and methods of administering therapeutically effective amounts of the preparations to provide a physiological effect.
摘要翻译：本公开的一个方面通常涉及在内源性大麻素系统中发挥不同作用的脂质化合物，例如调节CB1和CB2受体或调节内源性大麻素系统内的其他生物大分子。一些化合物显示改善的受体结合亲和力，和/或改善的受体亚型选择性，以及改进的生物稳定性。一些化合物表现出调节调节内源大麻素的生物处理的酶的活性，例如脂肪酸酰胺水解酶（FAAH）。一些化合物表现出抑制丙二胺转运蛋白的活性。本发明的其它方面是使用这些配体的药物制剂和施用治疗有效量的制剂以提供生理作用的方法。

3. 发明授权

US07183313B2 Keto cannabinoids with therapeutic indications 有权
标题翻译：酮托大麻素具有治疗适应症
公开(公告)号：US07183313B2
公开(公告)日：2007-02-27
申请号：US10647544
申请日：2003-08-25
申请人： Alexandros Makriyannis , Dai Lu , Xin-Zhong Lai
发明人： Alexandros Makriyannis , Dai Lu , Xin-Zhong Lai
IPC分类号： A61K31/366 , C07D311/80
CPC分类号： A61K49/0052 , C07D311/80
摘要： Novel tricyclic cannabinoid compounds are presented. Some of these compounds exhibit fluorescence properties. The fluorescent cannabinoid compounds are typically endogenously fluorescent. Some of these compounds, when administered in a therapeutically effective amount to an individual or animal, result 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：提出了新型三环类大麻素化合物。这些化合物中的一些显示荧光性质。荧光大麻素化合物通常是内源荧光的。当以治疗有效量施用于个体或动物时，这些化合物中的一些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。

4. 发明授权

US06939977B2 Analgesic and immunomodulatory cannabinoids 失效
标题翻译：止痛和免疫调节大麻素
公开(公告)号：US06939977B2
公开(公告)日：2005-09-06
申请号：US10309686
申请日：2002-12-04
申请人： Alexandros Makriyannis , Dai Lu , Atmaram Khanolkar
发明人： Alexandros Makriyannis , Dai Lu , Atmaram Khanolkar
IPC分类号： C07D311/80 , C07D407/04 , C07D409/04 , C07D311/02 , C07D311/78 , C07D31/80
CPC分类号： C07D407/04 , C07D311/80 , C07D409/04
摘要： Disclosed are novel compounds represented by the following structural formula: R-X-Y; and physiologically acceptable salts thereof. R is a tricyclic core of a cannabinoid or substituted cannabinoid. X is a covalent bond, —CH2— or —CHR1—, wherein R1 a C1 to C3 substituted or unsubstituted alkyl group. Y is a heterocyclic ring, a substituted heterocyclic ring, a carbocyclic ring, a substituted carbocyclic ring, a fused bicyclic ring system, a substituted fused bicyclic ring system, a bridged bicyclic ring system, a substituted bridged bicyclic ring system, a bridged tricyclic ring system or a substituted bridged tricyclic ring system. Also disclosed is a method of stimulating a CB1 and/or CB2 receptor in a subject. The method comprises administering to the subject a therapeutically effective amount of R-X-Y.
摘要翻译：公开了由以下结构式表示的新化合物：<？in-line-formula description =“In-line formula”end =“lead”？> RXY; <？in-line-formula description =“In-line Formulas” 末端=“尾”→其生理学上可接受的盐。 R是大麻素或取代大麻素的三环核心。 X是共价键，-CH 2 - 或-CHR 1 - ，其中R 1，C 1至C 3取代或未取代的烷基。 Y是杂环，取代的杂环，碳环，取代的碳环，稠合双环系统，取代的稠合双环体系，桥连双环体系，取代的桥连双环体系，桥连三环系统或取代的桥接三环系统。还公开了刺激受试者中的CB1和/或CB2受体的方法。该方法包括向受试者施用治疗有效量的R-X-Y。

5. 发明申请

US20050074408A1 Keto cannabinoids with therapeutic indications 有权
标题翻译：酮托大麻素具有治疗适应症
公开(公告)号：US20050074408A1
公开(公告)日：2005-04-07
申请号：US10647544
申请日：2003-08-25
申请人： Alexandros Makriyannis , Dai Lu
发明人： Alexandros Makriyannis , Dai Lu
IPC分类号： A61K20060101 , A61K31/35 , A61K31/353 , A61K31/436 , A61K31/4375 , A61K31/473 , A61K31/5377 , A61K49/00 , C07D221/12 , C07D311/04 , C07D311/74 , C07D311/80 , C07D413/12 , C07D471/04 , C07D491/052 , C07D493/04 , G01N21/64 , G01N33/52
CPC分类号： A61K49/0052 , C07D311/80
摘要： Novel tricyclic cannabinoid compounds are presented. Some of these compounds exhibit fluorescence properties. The fluorescent cannabinoid compounds are typically endogenously fluorescent. Some of these compounds, when administered in a therapeutically effective amount to an individual or animal, result 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：提出了新型三环类大麻素化合物。这些化合物中的一些显示荧光性质。荧光大麻素化合物通常是内源荧光的。当以治疗有效量施用于个体或动物时，这些化合物中的一些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。

6. 发明申请

US20070135388A1 Novel Bicyclic Cannabinoids 有权
标题翻译：新型双环大麻素
公开(公告)号：US20070135388A1
公开(公告)日：2007-06-14
申请号：US11609580
申请日：2006-12-12
申请人： Alexandros Makriyannis , Spyridon Nikas , Atmaram Khanolkar , Ganeshsingh Thakur , Dai Lu
发明人： Alexandros Makriyannis , Spyridon Nikas , Atmaram Khanolkar , Ganeshsingh Thakur , Dai Lu
IPC分类号： A61K31/665 , A61K31/5375 , A61K31/426 , A61K31/421 , A61K31/12
CPC分类号： C07C49/747 , C07C29/03 , C07C37/055 , C07C41/20 , C07C41/30 , C07C45/296 , C07C45/54 , C07C45/567 , C07C45/71 , C07C49/753 , C07C49/83 , C07C251/44 , C07C331/24 , C07C2601/08 , C07C2602/42 , C07D317/26 , C07D339/06 , C07C49/433 , C07C39/23 , C07C39/17 , C07C39/18 , C07C43/215 , C07C43/21 , C07C35/28
摘要： Bicyclic-cannabinoids and methods of preparation and use 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 may be useful to treat a number of physiological conditions.
摘要翻译：提出了双环类大麻素及其制备和使用方法。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。

7. 发明申请

US20050239874A1 Novel analgesic and immunomodulatory cannabinoids 审中-公开
标题翻译：新型镇痛和免疫调节大麻素
公开(公告)号：US20050239874A1
公开(公告)日：2005-10-27
申请号：US11127455
申请日：2005-05-12
申请人： Alexandros Makriyannis , Dai Lu , Atmaram Khanolkar , Zhaoxing Meng
发明人： Alexandros Makriyannis , Dai Lu , Atmaram Khanolkar , Zhaoxing Meng
IPC分类号： C07D311/80 , C07D407/04 , C07D409/04 , A61K31/353
CPC分类号： C07D407/04 , C07D311/80 , C07D409/04
摘要： Disclosed are novel compounds represented by the following structural formula: R—X—Y; and physiologically acceptable salts thereof. R is a tricyclic core of a cannabinoid or substituted cannabinoid. X is a covalent bond, —CH2— or —CHR1—, wherein R1 a C1 to C3 substituted or unsubstituted alkyl group. Y is a heterocyclic ring, a substituted heterocyclic ring, a carbocyclic ring, a substituted carbocyclic ring, a fused bicyclic ring system, a substituted fused bicyclic ring system, a bridged bicyclic ring system, a substituted bridged bicyclic ring system, a bridged tricyclic ring system or a substituted bridged tricyclic ring system. Also disclosed is a method of stimulating a CB1 and/or CB2 receptor in a subject. The method comprises administering to the subject a therapeutically effective amount of R—X—Y.
摘要翻译：公开了由以下结构式表示的新化合物：<？in-line-formula description =“In-line formula”end =“lead”？> R-X-Y; <？in-line-formula description =“In-line Formulas”end =“tail”？>及其生理上可接受的盐。 R是大麻素或取代大麻素的三环核心。 X是共价键，-CH 2 - 或-CHR 1 - ，其中R 1，C 1至C 3取代或未取代的烷基。 Y是杂环，取代的杂环，碳环，取代的碳环，稠合双环系统，取代的稠合双环体系，桥连双环体系，取代的桥连双环体系，桥连三环系统或取代的桥接三环系统。还公开了刺激受试者中的CB1和/或CB2受体的方法。该方法包括向受试者施用治疗有效量的R-X-Y。

8. 发明授权

US07446229B2 Bicyclic cannabinoids 有权
标题翻译：双环大麻素
公开(公告)号：US07446229B2
公开(公告)日：2008-11-04
申请号：US11609580
申请日：2006-12-12
申请人： Alexandros Makriyannis , Spyridon P. Nikas , Atmaram D. Khanolkar , Ganeshsingh A. Thakur , Dai Lu
发明人： Alexandros Makriyannis , Spyridon P. Nikas , Atmaram D. Khanolkar , Ganeshsingh A. Thakur , Dai Lu
IPC分类号： C07C49/115 , C07C49/23 , C07D311/78 , A61K31/35
CPC分类号： C07C49/747 , C07C29/03 , C07C37/055 , C07C41/20 , C07C41/30 , C07C45/296 , C07C45/54 , C07C45/567 , C07C45/71 , C07C49/753 , C07C49/83 , C07C251/44 , C07C331/24 , C07C2601/08 , C07C2602/42 , C07D317/26 , C07D339/06 , C07C49/433 , C07C39/23 , C07C39/17 , C07C39/18 , C07C43/215 , C07C43/21 , C07C35/28
摘要： Bicyclic-cannabinoids and methods of preparation and use 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 may be useful to treat a number of physiological conditions.
摘要翻译：提出了双环类大麻素及其制备和使用方法。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。

9. 发明授权

US6166066A Cannabinoids selective for the CB2 receptor 失效
标题翻译：大麻素对CB2受体有选择性
公开(公告)号：US6166066A
公开(公告)日：2000-12-26
申请号：US304718
申请日：1999-05-04
申请人： Alexandros Makriyannis , Atmaram Khanolkar , Dai Lu
发明人： Alexandros Makriyannis , Atmaram Khanolkar , Dai Lu
IPC分类号： C07D311/78 , A61K31/35
CPC分类号： C07D311/78
摘要： Disclosed are novel cannabinoids which are selective for the CB2 receptor. The novel cannabinoids comprise a substituted or unsubstituted tricyclic cannabinoid core and a substituted or unsubstituted C5-C8 carbocyclic ring, five to eight-membered heterocyclic ring or a seven to ten membered bicyclic ring system fused to the monhydroxylated phenyl ring of the cannabinoid core. Also disclosed are methods of suppressing the immune system in a subject by administering to the subject a (e.g. immunosuppressive amount) effective amount of a novel cannabinoid described above.
摘要翻译：公开了对CB2受体具有选择性的新型大麻素。新型大麻素包含取代或未取代的三环大麻素核心和取代或未取代的C5-C8碳环，五至八元杂环或与大麻素核心的单羟基化苯环稠合的七至十元双环体系。还公开了通过向受试者施用有效量的上述新型大麻素（例如免疫抑制量）来抑制受试者的免疫系统的方法。

10. 发明申请

US20070155701A1 KETO CANNABINOIDS WITH THERAPEUTIC INDICATIONS 审中-公开
标题翻译：具有治疗适应症的KETO CANNABINOIDS
公开(公告)号：US20070155701A1
公开(公告)日：2007-07-05
申请号：US11619931
申请日：2007-01-04
申请人： Alexandros Makriyannis , Dai Lu
发明人： Alexandros Makriyannis , Dai Lu
IPC分类号： A61K31/675 , A61K31/541 , A61K31/5377 , A61K31/496 , A61K31/473 , A61K31/382 , A61K31/353 , C07D417/02 , C07D413/02 , C07D409/02 , C07D405/02
CPC分类号： C07D311/80 , A61K49/0021 , A61K49/0052 , C07D491/052
摘要： Novel tricyclic cannabinoid compounds are presented. Some of these compounds exhibit fluorescence properties. The fluorescent cannabinoid compounds are typically endogenously fluorescent. Some of these compounds, when administered in a therapeutically effective amount to an individual or animal, result 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：提出了新型三环类大麻素化合物。这些化合物中的一些显示荧光性质。荧光大麻素化合物通常是内源荧光的。当以治疗有效量施用于个体或动物时，这些化合物中的一些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。

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