申请人:Webster Scott Peter
公开号:US20130012545A1
公开(公告)日:2013-01-10
The present invention pertains generally to the field of therapeutic compounds. More specifically the present invention pertains to certain amido-thiophene compounds that, inter alia, inhibit 11β-hydroxysteroid dehydrogenase type 1 (11β-HSD1). The present invention also pertains to pharmaceutical compositions comprising such compounds, and the use of such compounds and compositions, both in vitro and in vivo, to inhibit 11β-hydroxysteroid dehydrogenase type 1; to treat disorders that are ameliorated by the inhibition of 11β-hydroxysteroid dehydrogenase type 1; to treat the metabolic syndrome, which includes disorders such as type 2 diabetes and obesity, and associated disorders including insulin resistance, hypertension, lipid disorders and cardiovascular disorders such as ischaemic (coronary) heart disease; to treat CNS disorders such as mild cognitive impairment and early dementia, including Alzheimer's disease; etc.
本发明通常涉及治疗化合物领域。更具体地,本发明涉及某些酰胺噻吩化合物,其在其他方面抑制11β-羟化固醇脱氢酶1型(11β-HSD1)。本发明还涉及包括这些化合物的制药组合物,并且在体内外使用这些化合物和组合物来抑制11β-羟化固醇脱氢酶1型;治疗通过抑制11β-羟化固醇脱氢酶1型改善的疾病;治疗代谢综合征,包括2型糖尿病和肥胖症等疾病,以及相关疾病,包括胰岛素抵抗、高血压、脂质代谢紊乱和缺血性(冠状动脉)心脏病等心血管疾病;治疗CNS疾病,如轻度认知障碍和早期痴呆,包括阿尔茨海默病等。