The present invention pertains generally to the field of therapeutic compounds. More specifically the present invention pertains to certain (4-phenyl-piperidin-1-yl)- [5-(1 H-pyrazol-4-yl)-thiophen-3-yl]-methanone compounds that, inter alia, inhibit 11 β-hydroxysteroid dehydrogenase type 1 (11 β-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 1 1 β-hydroxysteroid dehydrogenase type 1; to treat disorders that are ameliorated by the inhibition of 11 β-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.
本发明一般涉及治疗化合物领域。更具体地说,本发明涉及某些(4-
苯基-
哌啶-1-基)-[5-(1 H-
吡唑-4-基)-
噻吩-3-基]-甲
酮化合物,其中包括抑制11β-羟基甾
酮脱氢酶1(11β-H
SD1)的作用。本发明还涉及包含这些化合物的药物组合物,以及利用这些化合物和组合物在体外和体内抑制11β-羟基甾
酮脱氢酶1的用途;治疗通过抑制11β-羟基甾
酮脱氢酶1而得到改善的疾病;治疗代谢综合征,其中包括2型糖尿病和肥胖等疾病,以及相关疾病,包括
胰岛素抵抗、高血压、脂质紊乱和缺血性(
冠状动脉)心脏病等心血管疾病;治疗轻度认知障碍和早期痴呆等中枢神经系统疾病,包括阿尔茨海默病等。