FIELD: medicine; pharmaceutics.
SUBSTANCE: invention relates to a compound of Chemical formula 1 or a pharmaceutically acceptable salt thereof, which have the property of breaking down or inhibiting the androgen receptor (AR). In the formulas below, R1 is H, halogen, haloC1-6alkyl or C1-6alkoxy, R2 is H or C1-4alkyl, X1, X3, X4 and X5 are each independently CH or N, X2 is CR3 or N, R3 is H, C1-6alkyl, halogen or -OH, n is 0, 1 or 2, m is 0 or 1, L represents Chemical formula 2, A1, A2 and A3 each independently represents a direct bond, -O-, -N(R4)-, -C(O)-, -CC-, -C(O)NH-, -NHC(O)-, -C(O)CH2NH- or -C(O)CH2O-, R4 is H or C1-6 alkyl, B1, B2 and B3 each independently represent a direct bond or any of the following substitutes, each of R4' independently represents H, C1-4alkyl, halogenC1-4alkyl, halogen or -OH, q1-q6 each independently represents integer from 0 to 4, E represents Chemical formula 3 or 4, X6, X7, X8 and X9 each independently represents CH or N, Y is -C(R6)2-, -C(O)- or -N=N-, Z is a direct bond, -N(R6) - or -C(O)NH-, R5 and R5' each independently represents H, C1-4alkyl, halogen, halogenC1-4alkyl or C1-4alkoxy, each independently represents H, C1-4alkyl or halogenC1-4alkyl. Invention also relates to a pharmaceutical composition containing said compound or a pharmaceutically acceptable salt thereof, and to a method of treating or preventing an androgen receptor-related disease using the same.
EFFECT: destruction or inhibition of the androgen receptor.
9 cl, 6 tbl, 206 ex
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Authors
Dates
2024-04-15—Published
2021-07-19—Filed