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(Aralkylamino substituted in alpha and heteroarylalkylamino) pyrimidinyl and 1,3,5-triazinyl benzimidazoles, pharmaceutical compositions containing them, and these compounds for use in the treatment of proliferative diseases
专利权人:
Inc.;MEI Pharma
发明人:
BROWN, S.,MATTHEWS, David
申请号:
ES12711551
公开号:
ES2608967T3
申请日:
2012.03.27
申请国别(地区):
ES
年份:
2017
代理人:
摘要:
A compound of formula II: ** Formula ** or an enantiomer, a mixture of enantiomers, a mixture of two or more diastereomers, or a variant isotopic thereof; or a pharmaceutically acceptable salt, solvate or hydrate thereof; wherein: X, Y, and Z are each independently N or CRx, with the proviso that at least two of X, Y, and Z are nitrogen atoms; where Rx is hydrogen or C1-6 alkyl; R1 and R2 are each independently (a) hydrogen, cyano, halo, or nitro; (b) C1-6 alkyl, C2-6 alkenyl, C2-6 alkynyl, C3-10 cycloalkyl, C6-14 aryl, C7-15 aralkyl, heteroaryl, or heterocyclyl; or (c) -C (O) R1a, - C (O) OR1a, - (O) NR1bR1c, -C (NR1a) NR1bR1c, -OR1a, - OC (O) R1a, -OC (O) OR1a, -OC (O) NR1bR1c, - OC (>; = NR1a) NR1bR1c, -OS (O) R1a, -OS (O) 2R1a, -OS (O) NR1bR1c, -OS (O) 2NR1bR1c, -NR1bR1c, -NR1aC (O) R1d, - NR1aC (O) OR1d, - NR1aC (O) NR1bR1c, -NR1aC (>; = NR1d) NR1bR1c, -NR1aS (O) R1d, -NR1aS (O) 2R1d, - NR1aS (O) NR1bR1c, -NR1a (ONR1a) ) 2NR1bR1c, -SR1a, -S (O) R1a, -S (O) 2R1a, -S (O) NR1bR1c, oS (O) 2NR1bR1c; wherein each R1a, R1b, R1c, and R1d is independently (i) hydrogen; (ii) C1-6 alkyl, C2-6 alkenyl, C2-6 alkynyl, C3-10 cycloalkyl, C6-14 aryl, C7-15 aralkyl, heteroaryl, or heterocyclyl; or (iii) R1b and R1c together with the N atom to which they are attached form the heterocyclyl; R3 and R4 are each independently hydrogen or C1-6 alkyl; or R3 and R4 join together to form a bond, C1-6 alkylene, C1-6 heteroalkylene, C2-6 alkenylene, or C2-6 heteroalkenylene; R5a is hydrogen or C1-6 alkyl; R5b is C1-6 alkyl or -C (O) OR1a; R5c is - (CR5fR5g) n- (C6-14 aryl) or - (CR5fR5g) n-heteroaryl; R5f and R5g are each independently (a) hydrogen or halo; (b) C1-6 alkyl, C2-6 alkenyl, C2-6 alkynyl, C3-10 cycloalkyl, C6-14 aryl, C7-15 aralkyl, heteroaryl, or heterocyclyl; or (c) -C (O) R1a, -C (O) OR1a, - C (O) NR1bR1c, -C (NR1a) NR1bR1c, -OR1a, -OC (O) R1a, - OC (O) OR1a, - OC (O) NR1bR1c, -OC (>; = NR1a) NR1bR1c, - OS (O) R1a, -OS (O) 2R'a, -OS (O) NR1bR1c, -OS (O) 2NR1bR1c, -NR1b
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