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公开(公告)号:US20050070583A1
公开(公告)日:2005-03-31
申请号:US10693161
申请日:2003-10-24
申请人: Lone Jeppesen , John Mogensen , Ingrid Pettersson , Per Sauerberg , Pavel Pihera , Miroslav Havranek
发明人: Lone Jeppesen , John Mogensen , Ingrid Pettersson , Per Sauerberg , Pavel Pihera , Miroslav Havranek
IPC分类号: C07C59/68 , C07C69/712 , C07C323/20 , A61K31/445 , A61K31/325 , A61K31/40
CPC分类号: C07C323/20 , C07C59/68 , C07C69/712
摘要: Novel compounds of the general formula (I), the use of these compounds as pharmaceutical compositions, pharmaceutical compositions comprising the compounds and methods of treatment employing these compounds and compositions. The present compounds may be useful in the treatment and/or prevention of conditions mediated by Peroxisome Proliferator-Activated Receptors (PPAR), in particular the PPARδ suptype.
摘要翻译: 通式(I)的新型化合物,这些化合物作为药物组合物的用途,包含该化合物的药物组合物和使用这些化合物和组合物的治疗方法。 本发明化合物可用于治疗和/或预防由过氧化物酶体增殖物激活受体(PPAR)介导的病症,特别是PPARdelta suptype。
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公开(公告)号:US20060111366A1
公开(公告)日:2006-05-25
申请号:US11265794
申请日:2005-10-11
申请人: Henrik Andersen , Gita Camilla Kampen , Inge Christensen , John Mogensen , Annette Larsen , John Kilburn
发明人: Henrik Andersen , Gita Camilla Kampen , Inge Christensen , John Mogensen , Annette Larsen , John Kilburn
IPC分类号: A61K31/496 , A61K31/495 , A61K31/453 , A61K31/165 , A61K31/445
CPC分类号: A61K45/06 , A61K31/16 , A61K31/415 , C07D209/02 , 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。
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公开(公告)号:US20060106008A1
公开(公告)日:2006-05-18
申请号:US11247847
申请日:2005-10-11
IPC分类号: A61K31/55 , A61K31/4745 , A61K31/4196
CPC分类号: C07D471/04 , A61K31/4745 , A61K31/4985 , A61K31/519 , A61K31/5513 , A61K45/06 , C07D487/04 , C07D487/08
摘要: The use of fused 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 fused 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: 已经描述了使用稠合的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。 还描述了一类新的稠合的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。
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公开(公告)号:US20080108598A1
公开(公告)日:2008-05-08
申请号:US12006765
申请日:2008-01-03
申请人: Henrik Andersen , Gita Camilla Kampen , Inge Christensen , John Mogensen , Annette Larsen , John Kilburn
发明人: Henrik Andersen , Gita Camilla Kampen , Inge Christensen , John Mogensen , Annette Larsen , John Kilburn
CPC分类号: A61K45/06 , A61K31/16 , A61K31/415 , C07D209/02 , 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。
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公开(公告)号:US20070270408A1
公开(公告)日:2007-11-22
申请号:US11254118
申请日:2005-10-11
IPC分类号: A61K31/505 , A61K31/496 , A61K31/5377 , A61K31/541 , A61K31/55 , A61P3/00 , A61P3/10
CPC分类号: A61K31/496 , A61K31/505 , A61K31/5377 , A61K31/541 , A61K31/55
摘要: The use of substituted pyrazolo[1,5-a]pyrimidines 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 pyrazolo[1,5-a]pyrimidines 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: 描述了使用取代的吡唑并[1,5-a]嘧啶来调节1β-羟基类固醇脱氢酶(11betaHSD1)的活性以及这些化合物作为药物组合物的用途。 还有一类新的取代的吡唑并[1,5-a]嘧啶在治疗中的用途,包含该化合物的药物组合物以及它们在制备药物中的用途。本发明化合物是调节剂,更具体地说是活性抑制剂 的11betaHSD1,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。
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公开(公告)号:US20060100235A1
公开(公告)日:2006-05-11
申请号:US11246455
申请日:2005-10-07
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。
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