申请人:Piomelli Daniele
公开号:US20120010283A1
公开(公告)日:2012-01-12
Fatty acid amide hydrolase inhibitors of the Formula:
are provided wherein X is NH, CH
2
, O, or S; Q is O or S; Z is O or N; R is an aromatic moiety selected from the group consisting of substituted or unsubstituted aryl; substituted or unsubstituted biphenylyl, substituted or unsubstituted naphthyl, and substituted or unsubstituted phenyl; substituted or unsubstituted terphenylyl; substituted or unsubstituted cycloalkyl, heteroaryl, or alkyl; and R
1
and R
2
are independently selected from the group consisting of H, substituted or unsubstituted alkyl, substituted or unsubstituted heteroalkyl, and substituted or unsubstituted phenyl, substituted or unsubstituted biphenylyl, substituted or unsubstituted aryl, and substituted or unsubstituted heteroaryl; with the proviso that if Z is O, one of R
1
and R
2
is absent, and that if Z is N, optionally R
1
and R
2
may optionally be taken together to form a substituted or unsubstituted N-heterocycle or substituted or unsubstituted heteroaryl with the N atom to which they are each attached. Pharmaceutical compositions comprising the compounds of Formula I and methods of using them to inhibit FAAH and/or treat appetite disorders, glaucoma, pain, insomnia, and neurological and psychological disorders including anxiety disorders, epilepsy, and depression are provided.
提供了公式为的脂肪酸酰胺水解酶抑制剂:其中X为NH,CH2,O或S;Q为O或S;Z为O或N;R为从取代或未取代芳基;取代或未取代联苯基;取代或未取代萘基;取代或未取代苯基;取代或未取代三苯基基;取代或未取代环烷基,杂环芳基或烷基中选择的芳香基;R1和R2分别选择自H,取代或未取代烷基,取代或未取代杂环烷基,取代或未取代苯基,取代或未取代联苯基,取代或未取代芳基和取代或未取代杂环芳基的群中;但是如果Z为O,则R1和R2中的一个不存在,如果Z为N,则可选地将R1和R2结合在一起形成取代或未取代的N-杂环或取代或未取代的杂环芳基,与它们各自连接的N原子。提供了包含公式I化合物的制药组合物以及使用它们来抑制FAAH和/或治疗食欲障碍,青光眼,疼痛,失眠以及神经和心理障碍,包括焦虑症,癫痫和抑郁症的方法。