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51. 发明授权

US08293724B2 Therapeutic applications of fatty acid amide hydrolase inhibitors 失效
标题翻译：脂肪酸酰胺水解酶抑制剂的治疗应用
公开(公告)号：US08293724B2
公开(公告)日：2012-10-23
申请号：US12755227
申请日：2010-04-06
申请人： George Kunos , Alexandros Makriyannis
发明人： George Kunos , Alexandros Makriyannis
IPC分类号： A61K31/69 , A61K31/10 , A61K317/06 , C07F5/02 , C07F9/02
CPC分类号： C07C309/82
摘要： Fatty acid amide hydrolase (FAAH) is an enzyme responsible for the degradation of oleamide (an endogenous sleep-inducing lipid) and anandamide (an endogenous ligand for cannabinoid receptors). Disclosed herein are potent inhibitors of FAAH and methods for their use for treating a variety of disorder, including hypertension and cardiac hypertrophy.
摘要翻译：脂肪酸酰胺水解酶（FAAH）是负责降解油酰胺（内源性睡眠诱导性脂质）和anandamide（大麻素受体的内源性配体）的酶。本文公开了FAAH的有效抑制剂及其用于治疗多种障碍（包括高血压和心脏肥大）的方法。

52. 发明授权

US08293211B2 CB1 receptor antagonists and uses thereof 有权
标题翻译： CB1受体拮抗剂及其用途
公开(公告)号：US08293211B2
公开(公告)日：2012-10-23
申请号：US12157578
申请日：2008-06-11
申请人： Alexandros Makriyannis , Venkata K Vemuri
发明人： Alexandros Makriyannis , Venkata K Vemuri
IPC分类号： A61K49/00 , A61K31/5377 , A61K31/454
CPC分类号： A61K31/5377 , A61K31/454 , A61K45/06 , A61K49/0008 , C07D401/12 , C07D413/12
摘要： Neutral antagonists of the CB1 cannabinoid receptor, means for identifying neutral antagonists of the CB1 cannabinoid receptor, and uses thereof. Antagonists of the CB1 cannabinoid receptor can be used to prevent, treat or reduce the severity of various medical conditions and symptoms, including, but not limited to obesity, appetite disorder, another metabolic disorder, drug addiction and/or mental illness. Administering neutral CB1 cannabinoid receptor antagonists in place of or in combination with known CB1 cannabinoid receptor antagonists or inverse CB1 cannabinoid receptor agonists in an individual or animal to treat a medical condition with a reduction of unwanted side effects. A method of detecting a neutral CB1 cannabinoid receptor antagonist, including identifying a candidate compound; subjecting the candidate compound to one or more of a cAMP assay, CB1 competitive binding assay, food intake assay, thermoregulation assay, or emesis assay; and selecting the compound if it exhibits neutral antagonist activity.
摘要翻译： CB1大麻素受体的中性拮抗剂，用于鉴定CB1大麻素受体的中性拮抗剂的手段及其用途。 CB1大麻素受体的拮抗剂可用于预防，治疗或降低各种医学状况和症状的严重性，包括但不限于肥胖症，食欲障碍，另一种代谢紊乱，药物成瘾和/或精神疾病。管理中性CB1大麻素受体拮抗剂代替或与已知的CB1大麻素受体拮抗剂或反向CB1大麻素受体激动剂组合在个体或动物中以治疗不利副作用的医疗状况。检测中性CB1大麻素受体拮抗剂的方法，包括鉴定候选化合物; 使候选化合物进行cAMP测定，CB1竞争性结合测定，食物摄取测定，体温调节测定或呕吐测定中的一种或多种; 并选择化合物，如果它具有中性拮抗剂活性。

53. 发明申请

US20120095047A1 Novel Heteropyrrole Analogs Acting on Cannabinoid Receptors 有权
标题翻译：新型异丙吡咯类似物作用于大麻素受体
公开(公告)号：US20120095047A1
公开(公告)日：2012-04-19
申请号：US13334163
申请日：2011-12-22
申请人： Alexandros Makriyannis , Rajesh Thotapally , Venkata Kiran Rao Vemuri , Teresa Olszewska
发明人： Alexandros Makriyannis , Rajesh Thotapally , Venkata Kiran Rao Vemuri , Teresa Olszewska
IPC分类号： A61K31/4545 , A61K31/454 , C07D401/14 , C07D403/10 , A61K31/4178 , C07D417/14 , C07D233/88 , A61K31/4164 , C07D233/90 , A61P25/30 , A61P3/04 , A61P25/18 , A61P25/08 , A61P25/22 , A61P25/00 , A61P25/06 , A61P1/08 , A61P43/00 , A61P25/14 , A61P25/16 , A61P25/04 , A61P25/28 , A61P25/24 , A61P25/32 , A61P25/36 , A61P25/34 , A61P35/00 , A61P29/00 , C07D401/12
CPC分类号： C07D233/90 , C07D401/10 , C07D403/10 , C07D417/10
摘要： Disclosed are biologically active hetero pyrrole analogs such as imidazoles, thiazoles, oxazoles and pyrazoles capable of interacting with the CB1 and/or the CB2 cannabinoid receptors. One aspect discloses hetero pyrrole analogs acting as antagonists for the CB1 and/or the CB2 receptors. Another aspect discloses hetero pyrrole analogs having selectivity for the CB1 or CB2 cannabinoid receptor. Also disclosed are pharmaceutical preparations employing the disclosed analogs and methods of administering therapeutically effective amounts of the disclosed analogs to provide a physiological effect.
摘要翻译：公开了能够与CB1和/或CB2大麻素受体相互作用的生物活性杂吡咯类似物，例如咪唑，噻唑，恶唑和吡唑。一方面公开了作为CB1和/或CB2受体拮抗剂的杂吡咯类似物。另一方面公开了对CB1或CB2大麻素受体具有选择性的异构吡咯类似物。还公开了采用公开的类似物的药物制剂和施用治疗有效量的所公开的类似物以提供生理作用的方法。

54. 发明授权

US08097752B2 Antiprotozoal ring-substituted phospholipids 有权
标题翻译：抗原雄激素环取代磷脂
公开(公告)号：US08097752B2
公开(公告)日：2012-01-17
申请号：US10531324
申请日：2003-10-29
申请人： Theodora Calogeropoulou , Maria Koufaki , Nikolaos Avlonitis , Alexandros Makriyannis
发明人： Theodora Calogeropoulou , Maria Koufaki , Nikolaos Avlonitis , Alexandros Makriyannis
IPC分类号： C07D295/037 , C07D211/06 , C07F9/38 , C07C209/00 , A61K31/14 , A61K31/44 , A61K31/5375 , A61K31/662 , A61P33/02
CPC分类号： C07F9/6533 , C07F9/091 , C07F9/117 , C07F9/59
摘要： Disclosed are novel ring containing phospholipids represented by the structural formula A-X—PO3—W and physiologically acceptable salts thereof and a process for the preparation of these compounds. The compounds can be used for the treatment of protozoal diseases and especially leishmaniasis.
摘要翻译：公开了由结构式A-X-PO 3 -W表示的新型环状磷脂及其生理学上可接受的盐以及这些化合物的制备方法。该化合物可用于治疗原生动物疾病，特别是利什曼病。

55. 发明申请

US20110166138A1 Inhibitors of Fatty Acid Amide Hydrolase and Monoacylglycerol Lipase for Modulation of Cannabinoid Receptors 有权
标题翻译：脂肪酸酰胺水解酶和单酰甘油脂肪酶抑制剂用于调节大麻素受体
公开(公告)号：US20110166138A1
公开(公告)日：2011-07-07
申请号：US12933322
申请日：2009-03-17
申请人： Alexandros Makriyannis , Lakshmipathi Pandarinathan , Nikolai Zvonok , Teija Parkkari , Lauren Chapman
发明人： Alexandros Makriyannis , Lakshmipathi Pandarinathan , Nikolai Zvonok , Teija Parkkari , Lauren Chapman
IPC分类号： A61K31/5377 , A61K31/41 , C07D257/04 , A61K31/4439 , C07D401/06 , C07D413/06 , A61K31/454 , A61K31/438 , C07D491/113 , A61K31/496 , C07D403/06 , A61K31/522 , C07D473/28 , A61K31/4192 , C07D249/18 , A61K31/437 , C07D471/04 , A61K31/4164 , C07D233/90 , A61P29/00 , A61P25/00 , A61P3/00 , A61P35/00 , C12Q1/34 , C12Q1/44 , G01N33/573
CPC分类号： G01N33/9406 , A61K31/41 , A61K31/415 , C07D231/12 , C07D233/56 , C07D235/08 , C07D249/08 , C07D249/18 , C07D263/22 , C07D401/12 , C07D471/04 , C07D473/00 , C07D473/28 , G01N21/6428 , G01N2333/70571 , G01N2333/92 , G01N2333/98 , G01N2500/02 , G01N2500/20
摘要： Disclosed are compounds and compositions that inhibit the action of fatty acid amide hydrolase (FAAH) and monoacylglycerol lipase (MGL), methods of inhibiting FAAH and MGL, methods of modulating cannabinoid receptors, and methods of treating various disorders related to modulation of cannabinoid receptors.
摘要翻译：公开了抑制脂肪酰胺水解酶（FAAH）和单酰基甘油脂肪酶（MGL）的作用的化合物和组合物，抑制FAAH和MGL的方法，调节大麻素受体的方法，以及治疗与大麻素受体调节有关的各种疾病的方法。

56. 发明申请

US20100234379A1 Dual modulation of endocannabinoid transport and fatty-acid amide hydrolase for treatment of excitotoxicity 审中-公开
标题翻译：双重调节内源性大麻素转运和脂肪酸酰胺水解酶治疗兴奋性毒性
公开(公告)号：US20100234379A1
公开(公告)日：2010-09-16
申请号：US11494852
申请日：2006-07-28
申请人： Ben A. Bahr , Alexandros Makriyannis , David A. Karanian
发明人： Ben A. Bahr , Alexandros Makriyannis , David A. Karanian
IPC分类号： A61K31/5377 , A61K31/10 , A61K31/255 , A61K31/12 , A61K31/27 , A61K31/4402 , A61K31/4245 , A61K31/428 , A61K31/167 , A61K31/16 , A61K31/454 , A61P25/00
CPC分类号： A61K31/5377 , A61K31/10 , A61K31/12 , A61K31/16 , A61K31/167 , A61K31/255 , A61K31/27 , A61K31/4245 , A61K31/428 , A61K31/4402 , A61K31/454
摘要： The endocannabinoid transporter and FAAH are sites of modulation that allow pharmacological enhancement of protective endocannabinergic signals. Selective inhibitors of the transporter and inhibitors of FAAH caused additive augmentation of endogenous signaling events mediated by the cannabinoid CB1 receptor. Disruption of such signals has been shown to prevent neuronal maintenance processes and increase vulnerability to brain damage. Here, blocking endocannabinoid inactivation enhanced cannabinergic activity and ameliorated cellular disturbances associated with excitotoxicity. Modulating the endocannabinoid system in this way also prevented excitotoxic behavioral abnormalities including memory impairment. Collectively, these results indicate that increasing endocannabinoid responses by inhibiting the endocannabinoid transported and/or the inhibiting FAAH leads to molecular, cellular, and functional protection against excitotoxic insults like stroke and traumatic brain injury.
摘要翻译：内源性大麻素转运蛋白和FAAH是允许药理学增强保护性内源性抗生素能信号的调节位点。转运蛋白的选择性抑制剂和FAAH抑制剂引起大麻素CB1受体介导的内源性信号传导事件的相加增加。已经显示这种信号的破坏可以防止神经元维持过程并增加对脑损伤的易感性。在这里，阻断内源性大麻素失活增强大麻素能活性和改善与兴奋性毒性相关的细胞紊乱。以这种方式调节内源性大麻素系统也可以防止兴奋性毒性行为异常，包括记忆障碍。总的来说，这些结果表明，通过抑制内源性大麻素运输和/或抑制FAAH来增加内源性大麻素反应导致分子，细胞和功能保护免受诸如中风和创伤性脑损伤的兴奋性毒性损伤。

57. 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。

58. 发明授权

US07276613B1 Retro-anandamides, high affinity and stability cannabinoid receptor ligands 有权
标题翻译：复方昂丹酰胺，高亲和力和稳定性大麻素受体配体
公开(公告)号：US07276613B1
公开(公告)日：2007-10-02
申请号：US10110862
申请日：2000-10-18
申请人： Alexandros Makriyannis , Qian Liu , Andreas Goutopoulos
发明人： Alexandros Makriyannis , Qian Liu , Andreas Goutopoulos
IPC分类号： C07C231/00 , C07C233/00 , C07D265/30
CPC分类号： C07C233/05 , C07C233/65 , C07C235/06 , C07C271/12 , C07C275/06
摘要： Novel retro-anandamides are presented which have high 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 in individuals and animals for treatment of pain, glaucoma, epilepsy, nausea associated with chemotherapy, as well as suppression of the immune system, enhancement of appetite and in treatment of certain mental disorders.
摘要翻译：提出了对大麻素CB1和/或CB2受体位点具有高亲和力的新型复方壬酰胺。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个体和动物中用作治疗疼痛，青光眼，癫痫，与化学疗法相关的恶心以及抑制免疫系统，增加食欲和治疗某些精神障碍。

59. 发明授权

US07057076B2 Bicyclic and tricyclic cannabinoids 有权
标题翻译：双环和三环类大麻素
公开(公告)号：US07057076B2
公开(公告)日：2006-06-06
申请号：US10483482
申请日：2002-07-11
申请人： Alexandros Makriyannis , Spyridon P Nikas , Atmaram D Khanolkar
发明人： Alexandros Makriyannis , Spyridon P Nikas , Atmaram D Khanolkar
IPC分类号： C07C49/115 , C07C49/23 , C07D311/78 , A61K31/35
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。

60. 发明申请

US20060105998A1 Antiprotozoal ring-substiuted phospholipids 有权
标题翻译：抗原卟啉环取代的磷脂
公开(公告)号：US20060105998A1
公开(公告)日：2006-05-18
申请号：US10531324
申请日：2003-10-29
申请人： Theodora Calogeropoulou , Maria Koufaki , Nikolaos Avlonitis , Alexandros Makriyannis
发明人： Theodora Calogeropoulou , Maria Koufaki , Nikolaos Avlonitis , Alexandros Makriyannis
IPC分类号： A61K31/675 , C07F9/6533 , C07F9/576
CPC分类号： C07F9/6533 , C07F9/091 , C07F9/117 , C07F9/59
摘要： Disclosed are novel ring containing phospholipids represented by the structural formula A-X—PO3—W and physiologically acceptable salts thereof and a process for the preparation of these compounds. The compounds can be used for the treatment of protozoal diseases and especially leishmaniasis.
摘要翻译：公开了由结构式A-X-PO 3 -W表示的新型环状磷脂及其生理学上可接受的盐及其制备方法。该化合物可用于治疗原生动物疾病，特别是利什曼病。

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