Amido-thiophene compounds and their use
    1.
    发明授权
    Amido-thiophene compounds and their use 有权
    酰胺 - 噻吩化合物及其用途

    公开(公告)号:US08614209B2

    公开(公告)日:2013-12-24

    申请号:US13615497

    申请日:2012-09-13

    IPC分类号: A61K31/55 C07D223/00

    摘要: 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.

    摘要翻译: 本发明一般涉及治疗化合物领域。 更具体地说,本发明涉及特别是抑制1型11β-羟类固醇脱氢酶(11beta-HSD1)的某些酰氨基噻吩化合物。 本发明还涉及包含这些化合物的药物组合物,以及这些化合物和组合物在体外和体内都用于抑制1型11β-羟类固醇脱氢酶的用途; 治疗通过抑制1型11β-羟类固醇脱氢酶而改善的病症; 治疗代谢综合征,其包括诸如2型糖尿病和肥胖症的疾病,以及包括胰岛素抵抗,高血压,脂质障碍和心血管疾病如缺血性(冠心病)心脏病的相关疾病; 治疗CNS疾病如轻度认知障碍和早期痴呆,包括阿尔茨海默氏病; 等等

    3,3-disubstituted-(8-aza-bicyclo[3.2.1]oct-8-yl)-[5-(1H-pyrazol-4-yl)-thiophen-3-yl]-methanones as inhibitors of 11 (β)-HSD1
    7.
    发明授权
    3,3-disubstituted-(8-aza-bicyclo[3.2.1]oct-8-yl)-[5-(1H-pyrazol-4-yl)-thiophen-3-yl]-methanones as inhibitors of 11 (β)-HSD1 有权
    3,3-二取代 - (8-氮杂 - 双环[3.2.1]辛-8-基) - [5-(1H-吡唑-4-基) - 噻吩-3-基] - 甲酮作为11 &bgr;) - HSD1

    公开(公告)号:US09365564B2

    公开(公告)日:2016-06-14

    申请号:US13642963

    申请日:2011-03-10

    摘要: The present invention pertains generally to the field of therapeutic compounds. More specifically the present invention pertains to certain 3,3-disubstituted-(8-aza-bicyclo[3.2.1]oct-8-yl)-[5-(1H-pyrazol-4-yl)-thiophen-3-yl]-methanone, 3,3-disubstituted-(6-aza-bicyclo[3.1.1]hept-6-yl)-[5-(1H-pyrazol-4-yl)-thiophen-3-yl]-methanone, and 4,4-disubstituted piperidin-1-yl)-[5-(1H-pyrazol-4-yl)-thiophen-3-yl]-methanone compounds of the following formula 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.

    摘要翻译: 本发明一般涉及治疗化合物领域。 更具体地,本发明涉及某些3,3-二取代 - (8-氮杂 - 双环[3.2.1]辛-8-基) - [5-(1H-吡唑-4-基) - 噻吩-3-基 ] - 甲酮,3,3-二取代 - (6-氮杂 - 双环[3.1.1]庚-6-基) - [5-(1H-吡唑-4-基) - 噻吩-3-基] - 甲酮, 和4,4-二取代哌啶-1-基) - [5-(1H-吡唑-4-基) - 噻吩-3-基] - 甲酮化合物,其特别是抑制11-羟基类固醇脱氢酶 类型1(11&bgr; -HSD1)。 本发明还涉及包含这些化合物的药物组合物,以及这些化合物和组合物在体外和体内的用途,以抑制1型的1β-羟基类固醇脱氢酶; 治疗通过抑制11型β-羟基类固醇脱氢酶1改善的病症; 治疗代谢综合征,其包括诸如2型糖尿病和肥胖症的疾病,以及包括胰岛素抵抗,高血压,脂质障碍和心血管疾病如缺血性(冠心病)心脏病的相关疾病; 治疗CNS疾病如轻度认知障碍和早期痴呆,包括阿尔茨海默氏病; 等等

    HEIGHT-ADJUSTABLE WINDOW AIR CONDITIONER SUPPORT
    10.
    发明申请
    HEIGHT-ADJUSTABLE WINDOW AIR CONDITIONER SUPPORT 审中-公开
    高度可调式WINDOW AIR CONDITIONER支持

    公开(公告)号:US20080164390A1

    公开(公告)日:2008-07-10

    申请号:US11620695

    申请日:2007-01-07

    IPC分类号: F24F13/32

    CPC分类号: F24F13/32

    摘要: The present invention is directed to a height adjustable window air conditioner support that is rotatably adjusted to fit between a window air conditioner and a window ledge. In one embodiment, the support consists of two conjoined and threaded plastic cylindrical shafts, each of which, have a support platform on the opposing end.

    摘要翻译: 本发明涉及一种高度可调节的窗户空调支架,其被可旋转地调节以配合在窗户空调和窗台之间。 在一个实施例中,支撑件由两个连接和螺纹的塑料圆柱形轴组成,每个轴在其相对端具有支撑平台。