It is intended to provide antipruritics (drugs to control itching, antiitch agents and drugs to stop itching). It is found out that a compound having an agonistic activity to the cannabinoid receptor shows an antipruritics effect.
Pyridone derivatives having a binding activity to the cannabinoid type 2 recepter
申请人:TADA Yukio
公开号:US20100081686A1
公开(公告)日:2010-04-01
It was found that the compound having a binding activity to the cannabinoid type 2 receptor represented by the formula (I):
wherein R
1
is a group represented by the formula: —Y
1
—Y
2
—Y
3
—R
a
wherein Y
1
is single bond or the like; Y
2
is —C(═O)—NH— or the like; Y
3
is optionally substituted aryl or the like; R
2
is hydrogen or the like; R
3
is alkyl or the like; R
4
is alkyl or the like; R
5
is optionally substituted alkyl or the like; or R
3
and R
4
taken together with the adjacent atom form cyclic group or the like.
发现化合物具有与cannabinoid type 2受体结合活性,该化合物的公式为(I):其中R1是由公式表示的基团:—Y1—Y2—Y3—Ra,其中Y1是单键或类似物;Y2是—C(═O)—NH—或类似物;Y3是可选择的取代芳基或类似物;R2是氢或类似物;R3是烷基或类似物;R4是烷基或类似物;R5是可选择的取代烷基或类似物;或R3和R4与相邻原子结合形成环状基团或类似物。
Levene; Marker, Journal of Biological Chemistry, 1933, vol. 103, p. 373,376, 380
作者:Levene、Marker
DOI:——
日期:——
ANTIPRURITICS
申请人:SHIONOGI & CO., LTD.
公开号:EP1477186B1
公开(公告)日:2009-11-11
2-PYRIDONE DERIVATIVES HAVING AFFINITY FOR CANNABINOID TYPE 2 RECEPTOR