申请人:Lazzari Paolo
公开号:US20050282798A1
公开(公告)日:2005-12-22
Tricyclic pyrazole derivatives of the following formula (I) having affinity for the cannabinoidergic CB1 and/or CB2 receptors:
wherein:
A represents a group selected from one of the following: (CH
2
)
t
—, —(CH
2
)—S(O)
z
—, or —S(O)
z
—(CH
2
)—, B is a heteroaryl, optionally substituted; R is a group selected from the following: alkyl, aryl, arylalkyl or arylalkenyl, not substituted or having from one to four substituents, equal to or different from each other; R′ is a group selected from the following:
an ether group of formula —(CH
2
)—O—(CH
2
)
v
—R″, a ketonic group of formula —C(O)-Z′, wherein Z′ is as defined below; a substituent having an hydroxyl function of formula —CH(OH)-Z′; an amide substituent of formula —C(O)—NH-T′.
具有亲和力的三环吡唑衍生物的化学式(I),对大麻素受体CB1和/或CB2具有亲和力:
其中:
A代表从以下之一选择的基团:(CH2)t—,—(CH2)—S(O)z—,或—S(O)z—(CH2)—,
B是杂环芳基,可选择性取代;
R是从以下选择的基团:烷基,芳基,芳基烷基或芳基烯基,未取代或具有从一个到四个取代基,彼此相等或不同;
R′是从以下选择的基团:具有化学式—(CH2)—O—(CH2)v—R″的醚基团,具有化学式—C(O)-Z′的酮基团,其中Z′如下所定义;具有化学式—CH(OH)-Z′的羟基取代基;具有化学式—C(O)—NH-T′的酰胺取代基。