RYU, JE HO,柳济虎,柳濟虎,KIM, SHIN AE,金信爱,金信愛,RYU, KEUN HO,柳根镐,柳根鎬,KIM, JAE SUN,金载善,金載善,KIM, NAM HO,金南镐,金南鎬,HAN, HYE YOUNG,韩蕙英,韓蕙英,KIM, YONG HYUK,金容赫,金容赫,YOUN, WON-NO,尹愿老,尹願老,LEE, YOON-JUNG,李允静,李允靜,SON, HYU
申请号：
TW100115922
公开号：
TWI491603B
申请日:
2011.05.06
申请国别(地区):
TW
年份:
2015
代理人:
摘要：
Provided are picolinamide and pyrimidine-4-carboxamide compounds, a method for preparing the same, a pharmaceutical composition containing the same, and a medical use using the compound as an agent for preventing, regulating, and treating diseases related to regulation of glucocorticoids by using selective inhibitory activity of the compound for an 11β-HSD1 enzyme.The picolinamide and pyrimidine-4-carboxamide compounds of the present invention are selective inhibitors of human-derived 11β-HSD1 enzymes, and are useful in an agent for preventing, regulating, and treating diseases related to glucocorticoid regulation in which human-derived 11β-HSD1 enzymes are involved, for example, metabolic syndromes such as, type 1 and type 2 diabetes, diabetes later complications, latent autoimmune diabetes adult (LADA), insulin tolerance syndromes, obesity, impaired glucose tolerane (IGT), impaired fasting glucose (IFG), damaged glucose tolerance, dyslipidemia, atherosclerosis, hypertension, etc.提供甲吡啶醯胺與嘧啶-4-甲醯胺化合物、其製造方法、含其之醫藥組合物、及一種藉由利用該化合物對於11β-羥基類固醇脫氫酶1(11β-HSD1)酵素的選擇性抑制活性,而使用該化合物作為一用於預防、調節、及治療與糖皮質素調控相關之疾病之藥劑的醫療用途。本發明之甲吡啶醯胺與嘧啶-4-甲醯胺化合物係衍生自人類之11β-羥基類固醇脫氫酶1酵素的選擇性抑制劑,且可用作一藥劑以預防、調節、及治療涉及衍生自人類之11β-羥基類固醇脫氫酶1酵素之與糖皮質素調控相關的疾病,例如,代謝症候群如第1型與第2型糖尿病、糖尿病晚期併發症、成人遲發型自體免疫糖尿病(LADA)、胰島素耐受性症候群、肥胖、血糖耐受性異常(IGT)、空腹血糖異常(IFG)、血糖耐受性受損、高血脂、動脈粥樣硬化、及高血壓等。
