公开(公告)号：EP1775286A1

公开(公告)日：2007-04-18

申请号：EP06024572.7

申请日：1997-05-30

申请人： The University of Connecticut

发明人： Makriyannis, Alexandros ,  Lin, Sonyan ,  Hill, William Adam

IPC分类号： C07D207/46 ,  A61K31/165 ,  A61K31/10 ,  A61K31/40 ,  C07C239/22

CPC分类号： A61K31/4015 ,  A61K31/185 ,  A61K31/255 ,  C07D207/46

摘要： Disclosed is a method of inhibiting anandamide amidase in an individual or animal and novel inhibitors of anandamide amidase. The disclosed method and novel compounds can be used to reduce pain in an individual or animal suffering from pain, reducing nausea in an individual undergoing chemotherapy, for example cancer chemotherapy, suppressing appetite in an individual, reducing intraocular pressure in the eye of an individual or animal suffering from glaucoma and suppressing the immune system in an individual with an organ transplant.

摘要翻译： 公开了一种抑制个体或动物中的酰胺酰胺酶和新型氨基酰胺酰胺酶抑制剂的方法。 所公开的方法和新化合物可用于减轻患有疼痛的个体或动物的疼痛，减少经历化学疗法的个体的恶心，例如癌症化疗，抑制个体的食欲，降低个体眼中的眼内压或 患有青光眼的动物和用器官移植抑制个体的免疫系统。

公开(公告)号：EP1571147A2

公开(公告)日：2005-09-07

申请号：EP05251224.1

申请日：2005-03-01

申请人： The University of Connecticut

发明人： Makriyannis, Alexandros ,  Liu, Quian ,  Thotapally, Rajesh

IPC分类号： C07D231/14 ,  C07D401/10 ,  C07D409/10 ,  C07D231/12 ,  C07D403/10 ,  C07D231/40 ,  C07F7/22 ,  A61K31/415 ,  A61K31/4155 ,  A61P25/28 ,  A61P25/36

CPC分类号： C07D231/12 ,  C07D231/14 ,  C07D231/40 ,  C07D401/10 ,  C07D401/14 ,  C07D403/10 ,  C07D409/10

摘要： One aspect of the invention is concerned with cannabimimetic pyrazole analogs. Another aspect of the invention is concerned with new and improved pyrazole analogs having high affinities and/or selectivities for the CB1 cannabinoid receptor. A further aspect of the invention is concerned with pharmaceutical preparations employing the inventive analogs and methods of administering therapeutically effective amounts of the inventive analogs to provide a physiological effect.

摘要翻译： 本发明的一个方面涉及大麻仿制吡唑类似物。 本发明的另一方面涉及对CB1大麻素受体具有高亲和力和/或选择性的新的和改进的吡唑类似物。 本发明的另一方面涉及采用本发明类似物的药物制剂和施用治疗有效量的本发明类似物以提供生理作用的方法。

公开(公告)号：EP1571147A3

公开(公告)日：2008-10-08

申请号：EP05251224.1

申请日：2005-03-01

申请人： The University of Connecticut

发明人： Makriyannis, Alexandros ,  Liu, Quian ,  Thotapally, Rajesh

IPC分类号： C07D231/14 ,  C07D401/10 ,  C07D409/10 ,  C07D231/12 ,  C07D403/10 ,  C07D231/40 ,  C07F7/22 ,  A61K31/415 ,  A61K31/4155 ,  A61P25/28 ,  A61P25/36

CPC分类号： C07D231/12 ,  C07D231/14 ,  C07D231/40 ,  C07D401/10 ,  C07D401/14 ,  C07D403/10 ,  C07D409/10

摘要： One aspect of the invention is concerned with cannabimimetic pyrazole analogs. Another aspect of the invention is concerned with new and improved pyrazole analogs having high affinities and/or selectivities for the CB1 cannabinoid receptor. A further aspect of the invention is concerned with pharmaceutical preparations employing the inventive analogs and methods of administering therapeutically effective amounts of the inventive analogs to provide a physiological effect.

公开(公告)号：EP1702617A1

公开(公告)日：2006-09-20

申请号：EP06013196.8

申请日：2000-10-18

申请人： The University of Connecticut

发明人： Makriyannis, Alexandros ,  Deng, Hongfeng

IPC分类号： A61K31/404 ,  A61K31/4045 ,  C07D209/12 ,  C07D209/30 ,  C07D209/40 ,  C07D401/06

CPC分类号： C07D209/12

摘要： Novel cannabimimetic indole derivatives are presented which have preferentially high affinities for one of the cannabinoid CB1 or CB2 receptor sites. The improved receptor affinity makes these analogs therapeutically useful as medications in individual and animals for treatment of pain, glaucoma, epilepsy, nausea associated with chemotherapy.

摘要翻译： 提出了对大麻素CB1或CB2受体位点之一优先具有高亲和力的新型拟人吲哚衍生物。 改善的受体亲和性使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。