公开(公告)号：US20060100235A1

公开(公告)日：2006-05-11

申请号：US11246455

申请日：2005-10-07

申请人： Henrik Andersen ,  Gita, Camilla Kampen ,  Inge Christensen ,  John Mogensen ,  Annette Larsen

发明人： Henrik Andersen ,  Gita, Camilla Kampen ,  Inge Christensen ,  John Mogensen ,  Annette Larsen

IPC分类号： A61K31/4745 ,  A61K31/4439 ,  A61K31/4196

CPC分类号： A61K31/4196 ,  A61K31/4439 ,  A61K31/4745 ,  C07D249/12 ,  C07D401/12 ,  C07D409/04 ,  C07D409/14

摘要： The use of substituted 1,2,4-triazoles for modulating the activity of 11β-hydroxysteroid dehydrogenase type 1 (11βHSD1) and the use of these compounds as pharmaceutical compositions has been described. Also a novel class of substituted 1,2,4-triazoles, their use in therapy, pharmaceutical compositions comprising the compounds, as well as their use in the manufacture of medicaments has been described. The present compounds are modulators and more specifically inhibitors of the activity of 11βHSD1 and may be useful in the treatment, prevention and/or prophylaxis of a range of medical disorders where a decreased intracellular concentration of active glucocorticoid is desirable.

摘要翻译： 已经描述了使用取代的1,2,4-三唑来调节11β-羟类固醇脱氢酶1型（11betaHSD1）的活性以及这些化合物作为药物组合物的用途。 还描述了一类新颖的取代的1,2,4-三唑，它们在治疗中的用途，包含该化合物的药物组合物及其在制备药物中的用途。 本发明化合物是调节剂，更具体地是11betaHSD1活性的抑制剂，并且可用于治疗，预防和/或预防一系列需要活性糖皮质激素的细胞内浓度降低的医学疾病。

公开(公告)号：US20060089349A1

公开(公告)日：2006-04-27

申请号：US11244745

申请日：2005-10-06

申请人： Anette Gundertofte ,  Anker Jorgensen ,  Gita, Camilla Kampen ,  Henrik Andersen ,  Inge Christensen ,  John Kilburn

发明人： Anette Gundertofte ,  Anker Jorgensen ,  Gita, Camilla Kampen ,  Henrik Andersen ,  Inge Christensen ,  John Kilburn

IPC分类号： A61K31/55 ,  A61K31/497 ,  A61K31/454 ,  A61K31/403

CPC分类号： A61K45/06 ,  A61K31/16 ,  A61K31/415 ,  C07D209/02 ,  C07D401/06 ,  C07D401/12 ,  C07D403/12 ,  C07D487/08

摘要： A novel class of compounds of the general formula (I), their use in therapy, pharmaceutical compositions comprising the compounds, as well as their use in the manufacture of medicaments are described. The present compounds modulate the activity of 11β-hydroxysteroid dehydrogenase type 1 (11βHSD1) and are accordingly useful in the treatment of diseases in which such a modulation is beneficial, e.g. the metabolic syndrome.

摘要翻译： 描述了一类新颖的通式（I）化合物，其在治疗中的用途，包含该化合物的药物组合物及其在制备药物中的用途。 本发明化合物调节1型11β-羟类固醇脱氢酶（11betaHSD1）的活性，因此可用于治疗这种调节有益的疾病，例如， 代谢综合征。