SUBSTITUTED PYRROLE DERIVATIVE

摘要

The present invention provides a novel pyrrole derivative having excellent androgen receptor antagonism, which is represented by the formula (I): wherein R<SUP>1</SUP>represents a hydrogen atom, a cyano group or a group represented by the formula COOR<SUP>A</SUP> (wherein R<SUP>A</SUP> represents an optional substituted C<SUB>1-6</SUB> alkyl group), R<SUP>2</SUP> and R<SUP>4</SUP> are the same or different, and each represents a hydrogen atom, a C<SUB>1-6</SUB> alkyl group, a C<SUB>3-6</SUB> cycloalkyl group, a trifluoromethyl group, an amino-C<SUB>1-6</SUB> alkyl group, a mono-or di-substituted amino-C<SUB>1-6</SUB> alkyl group, an optionally halogenated C<SUB>1-6</SUB> alkyl group substituted with an optionally substituted hydroxyl group, a C<SUB>2-6</SUB> alkenyl group substituted with an optionally substituted hydroxyl group, a C<SUB>1-6</SUB> alkyl group substituted with an optionally substituted and optionally oxidized thiol group, an optionally substituted with and optionally oxidized thiol group, a cyano group, an acyl group, an optionally substituted oxazolyl group or a 1,3-dioxolan-2-yl group, R<SUP>3</SUP> represents a group represented by the formula (a): (wherein X represents a halogen atom, Y represents a carbon atom or a nitrogen atom, Alk represents an optionally substituted C <SUB>1-4</SUB> alkylene group, and R<SUP>B</SUP> represents a hydrogen atom or an acyl group), and R<SUP>5</SUP> represents a phenyl group which has a cyano group at a 4-position or a 3-position thereof, and may be further substituted, or a salt thereof. The present invention also provides an androgen receptor antagonist containing the pyrrole derivative, or a salt thereof.