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1. 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。

2. 发明申请

US20060199957A1 Novel bicyclic and tricyclic cannabinoids 失效
标题翻译：新型双环和三环类大麻素
公开(公告)号：US20060199957A1
公开(公告)日：2006-09-07
申请号：US11344762
申请日：2006-01-31
申请人： Alexandros Makriyannis , Spyridon Nikas , Atmaram Khanolkar
发明人： Alexandros Makriyannis , Spyridon Nikas , Atmaram Khanolkar
IPC分类号： C07F7/22 , C07D339/02 , C07D265/30 , C07C255/33 , C07C251/02 , C07C247/06
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。

3. 发明授权

US06995187B1 Peripheral cannabinoid receptor (CB2) selective ligands 有权
标题翻译：外周大麻素受体（CB2）选择性配体
公开(公告)号：US06995187B1
公开(公告)日：2006-02-07
申请号：US10110830
申请日：2000-10-18
申请人： Alexandros Makriyannis , Atmaram Khanolkar
发明人： Alexandros Makriyannis , Atmaram Khanolkar
IPC分类号： A61K31/352 , C07D311/78
CPC分类号： C07D311/80
摘要： Novel polycyclic cannabinoid analogs are presented which have preferentially high affinities for the cannabinoid CB2 receptor sites. The improved receptor affinity makes these analogs therapeutically useful as medications in individuals and animals for treatment of pain, glaucoma, epilepsy, nausea associated with chemotherapy.
摘要翻译：提出了对大麻素CB2受体位点优先具有高亲和力的新型多环类大麻素类似物。改善的受体亲和力使得这些类似物在治疗用于治疗疼痛，青光眼，癫痫，与化学疗法相关的恶心的个体和动物中作为药物治疗有用。

4. 发明授权

US06943266B1 Bicyclic cannabinoid agonists for the cannabinoid receptor 失效
公开(公告)号：US06943266B1
公开(公告)日：2005-09-13
申请号：US10110812
申请日：2000-10-18
申请人： Alexandros Makriyannis , Atmaram Khanolkar
发明人： Alexandros Makriyannis , Atmaram Khanolkar
IPC分类号： C07C49/67 , C07C49/743 , C07C49/753 , C07C67/02
CPC分类号： C07C49/743 , C07C49/67 , C07C49/753
摘要： Novel polycyclic cannabinoid analogs are presented which have preferentially high affinities for the cannabinoid CB2 receptor sites. The improved receptor affinity makes these analogs therapeutically useful as medications in individuals and animals for treatment of pain, glaucoma, epilepsy, nausea associated with chemotherapy.

5. 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。

6. 发明授权

US07335688B2 Bicyclic cannabinoid agonists for the cannabinoid receptor 失效
标题翻译：用于大麻素受体的双环大麻素激动剂
公开(公告)号：US07335688B2
公开(公告)日：2008-02-26
申请号：US11053132
申请日：2005-02-08
申请人： Alexandros Makriyannis , Atmaram Khanolkar
发明人： Alexandros Makriyannis , Atmaram Khanolkar
IPC分类号： A01N35/00 , C07C49/00
CPC分类号： C07C49/743 , C07C49/67 , C07C49/753
摘要： Novel polycyclic cannabinoid analogs are presented which have preferentially high affinities for the cannabinoid CB2 receptor sites. The improved receptor affinity makes these analogs therapeutically useful as medications in individuals and animals for treatment of pain, glaucoma, epilepsy, nausea associated with chemotherapy.
摘要翻译：提出了对大麻素CB2受体位点优先具有高亲和力的新型多环类大麻素类似物。改善的受体亲和力使得这些类似物在治疗用于治疗疼痛，青光眼，癫痫，与化学疗法相关的恶心的个体和动物中作为药物治疗有用。

7. 发明申请

US20050137173A1 Bicyclic cannabinoid agonists for the cannabinoid receptor 失效
标题翻译：用于大麻素受体的双环大麻素激动剂
公开(公告)号：US20050137173A1
公开(公告)日：2005-06-23
申请号：US11053132
申请日：2005-02-08
申请人： Alexandros Makriyannis , Atmaram Khanolkar
发明人： Alexandros Makriyannis , Atmaram Khanolkar
IPC分类号： C07C49/67 , C07C49/743 , C07C49/753 , A61K31/655 , A61K31/12 , A61K31/138 , A61K31/421 , A61K31/426 , A61K31/537
CPC分类号： C07C49/743 , C07C49/67 , C07C49/753
摘要： Novel polycyclic cannabinoid analogs are presented which have preferentially high affinities for the cannabinoid CB2 receptor sites. The improved receptor affinity makes these analogs therapeutically useful as medications in individuals and animals for treatment of pain, glaucoma, epilepsy, nausea associated with chemotherapy.
摘要翻译：提出了对大麻素CB2受体位点优先具有高亲和力的新型多环类大麻素类似物。改善的受体亲和力使得这些类似物在治疗用于治疗疼痛，青光眼，癫痫，与化学疗法相关的恶心的个体和动物中作为药物治疗有用。

8. 发明授权

US07741365B2 Peripheral cannabinoid receptor (CB2) selective ligands 有权
标题翻译：外周大麻素受体（CB2）选择性配体
公开(公告)号：US07741365B2
公开(公告)日：2010-06-22
申请号：US11323560
申请日：2005-12-29
申请人： Alexandros Makriyannis , Atmaram Khanolkar
发明人： Alexandros Makriyannis , Atmaram Khanolkar
IPC分类号： A61K31/352 , C07D311/78
CPC分类号： C07D311/80 , A61K31/366
摘要： Novel polycyclic cannabinoid analogs are presented which have preferentially high affinities for the cannabinoid CB2 receptor sites.
摘要翻译：提出了对大麻素CB2受体位点优先具有高亲和力的新型多环类大麻素类似物。

9. 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。

10. 发明授权

US07161016B1 Cannabimimetic lipid amides as useful medications 有权
标题翻译：制模拟脂质酰胺作为有用的药物
公开(公告)号：US07161016B1
公开(公告)日：2007-01-09
申请号：US09600786
申请日：1999-11-24
申请人： Alexandros Makriyannis , Atmaram Khanolkar , Andreas Goutopoulos
发明人： Alexandros Makriyannis , Atmaram Khanolkar , Andreas Goutopoulos
IPC分类号： C07C231/00
CPC分类号： C07C233/13 , C07C233/09 , C07C235/06 , C07C247/04
摘要： Novel analogs of arachidonylethanolamide are presented which have higher affinities for the cannabinoid CB1 and/or CB2 receptor sites. Further, most of the analogs exhibit greater metabolic stability than arachidonylethanolamide. The improved receptor affinity and selectivity and/or greater metabolic stability make these analogs therapeutically useful as medications for relief of pain caused by cancer and nausea caused by chemotherapy, as well as for peripheral pain. The compounds may also be useful as oral and topical contraceptives, in suppression of the immune system, enhancement of appetite and in treatment of psychomotor disorders, multiple sclerosis and hypertension.
摘要翻译：提出了对大麻素CB1和/或CB2受体位点具有较高亲和力的花生四烯乙醇酰胺的新型类似物。此外，大多数类似物表现出比花生四烯酰乙酰胺更高的代谢稳定性。改善的受体亲和力和选择性和/或更高的代谢稳定性使得这些类似物在治疗上作为缓解由化疗引起的癌症和恶心以及周围性疼痛引起的疼痛的药物治疗有用。所述化合物还可用作口服和局部避孕药，抑制免疫系统，增强食欲和治疗精神运动障碍，多发性硬化和高血压。

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