YOSHIMURA, SEIJI,吉村诚司,吉村誠司,KAWANO, NORIYUKI,河野则征,河野則征,KAWANO, TOMOAKI,河野友昭,SASUGA, DAISUKE,流石大辅,流石大輔,KOIKE, TAKANORI,小池贵德,小池貴德,WATANABE, HIDEYUKI,渡边英之,渡邊英之,FUKUDOME, HIROKI,福留裕树,福留裕樹,SHIRAISHI, N
申请号:
TW098122420
公开号:
TWI465439B
申请日:
2009.07.02
申请国别(地区):
TW
年份:
2014
代理人:
摘要:
[Problem] A compound, which can be used for preventing or treating diseases, in which 11²-hydroxysteroid dehydrogenase type 1 (11²-HSD1) is concerned, in particular, diabetes, insulin resistance, dementia, schizophrenia and depression, is provided. [Means for Solution] It was found that a triazole derivative, in which one of the 3- and 5-positions of the triazole ring has (di)alkylmethyl or cycloalkyl, each of which is substituted with -O- (aryl or a heterocyclic group, each of which may be substituted, or lower alkylene-cycloalkyl), and the other thereof has aryl, a heterocyclic group or cycloalkyl, each of which may be substituted, or a pharmaceutically acceptable salt thereof exhibits potent 11²-HSD1 inhibitory action. From the above, the triazole derivative of the present invention can be used for preventing or treating diabetes, insulin resistance, dementia, schizophrenia and depression.本發明係提供一種可使用於11β-羥基類固醇去氫酶型1(11β-HSD1)相關的疾病,特別是糖尿病、胰島素拮抗性、失智症、精神分裂症、憂鬱的預防或治療之化合物。其解決手段係發現三氮唑環的3位及5位之一方具有各被-O-(各被取代亦可的芳基或雜環基、或者、低級烷撐-環烷基)取代的(二)烷基甲基或環烷基、另一方具有各被取代亦可的芳基、雜環基或環烷基為特徵之三氮唑衍生物或其製藥學上被容許的鹽,具有強烈的11β-HSD1抑制活性。因此,本發明的三氮唑衍生物可使用於糖尿病、胰島素拮抗性、失智症、精神分裂症、憂鬱的預防或治療。