[EN] BENZIMIDAZOLONE GLP-1 RECEPTOR AGONIST AND USE THEREOF [FR] AGONISTE DU RÉCEPTEUR DE GLP-1, LA BENZIMIDAZOLONE ET SON UTILISATION [ZH] 苯并咪唑酮类GLP-1受体激动剂及其用途
[EN] BENZIMIDAZOLONE GLP-1 RECEPTOR AGONIST AND USE THEREOF [FR] AGONISTE DU RÉCEPTEUR DE GLP-1, LA BENZIMIDAZOLONE ET SON UTILISATION [ZH] 苯并咪唑酮类GLP-1受体激动剂及其用途
[Problems] A compound, which is useful as an active ingredient of a pharmaceutical composition, for example, a pharmaceutical composition for treating chronic renal failure and/or diabetic nephropathy, is provided.
[Solving Means] The present inventors have conducted extensive studies on a compound having an EP4 receptor antagonistic activity, and confirmed that the amide compound of the present invention has an EP4 receptor antagonistic activity, thereby completing the present invention. The amide compound of the present invention has an EP4 receptor antagonistic activity, and can be used as an active ingredient of a pharmaceutical composition for preventing and/or treating various EP4-related diseases, for example, chronic renal failure and/or diabetic nephropathy, and the like.
[Problems] A compound, which is useful as an active ingredient of a pharmaceutical composition, for example, a pharmaceutical composition for treating chronic renal failure and/or diabetic nephropathy, is provided.
[Solving Means] The present inventors have conducted extensive studies on a compound having an EP4 receptor antagonistic activity, and confirmed that the amide compound of the present invention has an EP4 receptor antagonistic activity, thereby completing the present invention. The amide compound of the present invention has an EP4 receptor antagonistic activity, and can be used as an active ingredient of a pharmaceutical composition for preventing and/or treating various EP4-related diseases, for example, chronic renal failure and/or diabetic nephropathy, and the like.
4-(Indol-7-ylcarbonylaminomethyl)cyclohexanecarboxylic acid derivatives as EP4 receptor antagonists useful for the treatment of chronic renal failure or diabetic nephropathy
申请人:Astellas Pharma Inc.
公开号:EP2565191A1
公开(公告)日:2013-03-06
The present invention relates to amide compounds of formula I which are EP4 receptor antagonists and useful for treating chronic renal failure and/or diabetic nephropathy.
Ring D is a group of formula II;
V and W are CH;
R45 is -CH2-B5;
B5 represents a bicyclic hetero ring which may be substituted with one or more groups selected from the group consisting of halogen and C1-6 alkyl;
R46 is H, halogen, C1-6 alkyl which may be substituted with one or more halogens, or -O-C1-6 alkyl;
-NR1-YR2 - is -NH-CH2-;
Ring E is cyclohexane-1,4-diyl; and
-Z-R3 is -CO2H.
本发明涉及式 I 的酰胺化合物,它们是 EP4 受体拮抗剂,可用于治疗慢性肾衰竭和/或糖尿病肾病。
环 D 是式 II 的基团;
V 和 W 是 CH;
R45 是-CH2-B5;
B5 代表可被一个或多个选自卤素和 C1-6 烷基的基团取代的双环杂环;
R46 是 H、卤素、可被一个或多个卤素取代的 C1-6 烷基或 -O-C1-6 烷基;
-NR1-YR2-是-NH-CH2-;
环 E 是环己烷-1,4-二基;以及
-Z-R3为-CO2H。