894075-01-5Relevant academic research and scientific papers
SUBSTITUTED PYRROLE DERIVATIVE
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Page/Page column 104-105, (2010/11/08)
The present invention provides a novel pyrrole derivative having excellent androgen receptor antagonism, which is represented by the formula (I): wherein R1represents a hydrogen atom, a cyano group or a group represented by the formula COORA (wherein RA represents an optional substituted C1-6 alkyl group), R2 and R4 are the same or different, and each represents a hydrogen atom, a C1-6 alkyl group, a C3-6 cycloalkyl group, a trifluoromethyl group, an amino-C1-6 alkyl group, a mono-or di-substituted amino-C1-6 alkyl group, an optionally halogenated C1-6 alkyl group substituted with an optionally substituted hydroxyl group, a C2-6 alkenyl group substituted with an optionally substituted hydroxyl group, a C1-6 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, R3 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 1-4 alkylene group, and RB represents a hydrogen atom or an acyl group), and R5 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.
