Fused bicyclic compound

Abstract

Disclosed is a novel fused bicyclic compound [I] shown below, which has affinity for a mineralcorticoid receptor (MR) and is useful as an anti-hypertensive agent or the like. Specifically disclosed is a compound represented by the formula [I] or a pharmacologically acceptable salt thereof. [I] wherein the ring A represents a benzene ring which is fused with the adjacent heterocyclic 6-membered ring and has a substituent R1, and which may have a substituent other than R1; R1 represents an alkylsulfonylamino group or the like; R2 and R3 (a) independently represent a hydrogen, an alkyl or a substituted or unsubstituted aryl, (b) together form an oxo, or (c) together with the adjacent carbon atom, form a cycloalkyl; X represents =N-, =C(R4)- or -CH(R4)-; R4 represents (a) a hydrogen, (b) a cyano, (c) a halogen, (d) an alkyl, (e) an alkenyl, (f) a cycloalkyl, (g) an alkanoyl, (h) a carbamoyl or (i) a cycloalkenyl; Ar represents a substituted or unsubstituted aromatic cyclic group; and a dotted line means the presence or absence of a double bond.

Description

technical field The present invention relates to novel fused bicyclic compounds having an affinity for the mineralocorticoid receptor (MR) which are useful in the treatment and / or prophylaxis of diseases or clinical conditions associated with said receptor. Background technique Physiologically active hydrophobic substances having a low molecular weight such as steroid hormones demonstrate their actions via the respective nuclear receptors as their ligands. A group of steroid hormone nuclear receptors forms an inherited superfamily and controls, ie, activates or represses, target gene expression at the transcriptional level by functioning as ligand-dependent transcription factors. Steroid hormone receptors include mineralocorticoid receptor (MR), glucocorticoid receptor (GR), androgen receptor (AR), estrogen receptor (ER) and progesterone receptor (PR). Steroid hormones such as mineralocorticoids (aldosterone) or glucocorticoids (cortisone, etc.), which are ligands for rece...

AI Technical Summary

Problems solved by technology

However, there are no reports on fused bicyclic compounds such as the compounds of the present invention (1,3-benzoxazine derivatives or benzopyran derivatives) having MR modulating activity (such as MR antagonistic activity)

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