公开(公告)号：EP2239012A3

公开(公告)日：2011-06-15

申请号：EP10164336.9

申请日：2004-04-06

申请人： High Point Pharmaceuticals, LLC

发明人： Andersen, Henrik Sune ,  Kampen, Gita Camilla Tejlgaard ,  Christensen, Inge Thoger ,  Mogensen, John Patrick ,  Larsen, Annette Rosendal ,  Kilburn, John Paul

IPC分类号： A61P3/04 ,  A61K31/16 ,  A61K31/415

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

摘要： The use of substituted amides for modulating the activity of 11β-hydroxysteroid dehydrogenase type 1 (11βHSD1) and the use of these compounds as pharmaceutical compositions, are described. Also a novel class of substituted amides, their use in therapy, pharmaceutical compositions comprising the compounds, as well as their use in the manufacture of medicaments are 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.

公开(公告)号：EP2239012A2

公开(公告)日：2010-10-13

申请号：EP10164336.9

申请日：2004-04-06

申请人： High Point Pharmaceuticals, LLC

发明人： Andersen, Henrik Sune ,  Kampen, Gita Camilla Tejlgaard ,  Christensen, Inge Thoger ,  Mogensen, John Patrick ,  Larsen, Annette Rosendal ,  Kilburn, John Paul

IPC分类号： A61P3/04 ,  A61K31/16 ,  A61K31/415

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

摘要： The use of substituted amides for modulating the activity of 11β-hydroxysteroid dehydrogenase type 1 (11βHSD1) and the use of these compounds as pharmaceutical compositions, are described. Also a novel class of substituted amides, their use in therapy, pharmaceutical compositions comprising the compounds, as well as their use in the manufacture of medicaments are 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： 描述了使用取代的酰胺调节11β-羟基类固醇脱氢酶1型（11²HSD1）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酰胺，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11,2HSD1活性的调节剂，更具体地说是抑制剂，并且可用于治疗，预防和/或预防一系列医学病症，其中期望活性糖皮质激素的细胞内浓度降低。