申请人:Kyorin Pharmaceutical Co., Ltd
公开号:US07601843B2
公开(公告)日:2009-10-13
There are provided compounds represented by the following general formula (I):
[where R1 is 5-methylpyridin-2-yl, p-tolyl or mesityl, R2 is one of the following general formulas (II)-(IX):
(where R3 is C1-C4 alkyl, R4 is H or C1-C4 alkyl, R5 is H, 3-pyridylmethyl or 4-pyridylmethyl, and R6 is 2,4-dihydroxybenzyl, 3-pyridylmethyl or 4-pyridylmethyl), or when R1 is mesityl, R2 is the following formula (X)],
and pharmaceutically acceptable salts thereof. The compounds exhibit pruritus-inhibiting action, and are useful for prevention or of itching and pruritus caused by reaction against insect-inflicted wounds, reaction against environmental allergens, skin infections or external parasite infections, or caused to renal dialysis patient.
以下是通用式(I)所代表的化合物:[其中R1是5-甲基吡啶-2-基,对甲基苯基或三甲基苯基,R2是以下通用式(II)-(IX)之一:(其中R3是C1-C4烷基,R4是H或C1-C4烷基,R5是H,3-吡啶甲基或4-吡啶甲基,R6是2,4-二羟基苯甲基,3-吡啶甲基或4-吡啶甲基),或当R1是三甲基苯基时,R2是以下式子(X)],以及其药学上可接受的盐。这些化合物具有止痒作用,可用于预防或治疗由昆虫叮咬引起的瘙痒和瘙痒反应,环境过敏原引起的反应,皮肤感染或外部寄生虫感染引起的瘙痒,或透析患者引起的瘙痒。