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Isotopically enriched arylsulfonamide CCR3 antagonists
专利权人:
AXIKIN PHARMACEUTICALS; INC.
发明人:
LY, TAI,POTTER, GARRETT
申请号:
ES11707755
公开号:
ES2542404T3
申请日:
2011.03.01
申请国别(地区):
ES
年份:
2015
代理人:
摘要:
A compound of Formula I: ** Formula ** or an enantiomer, a mixture of enantiomers, a mixture of two or more diastereomers, a tautomer, or a mixture of two or more tautomers thereof; or a pharmaceutically acceptable salt, solvate or hydrate thereof; where: R1, R2, R3, R4, R5 and R8 are each independently (a) hydrogen, deuterium, halo, cyano, nitro or guanidine; (b) C 1-6 alkyl, C 2-6 alkenyl, C 2-6 alkynyl, C 3-7 cycloalkyl, C 6-14 aryl, heteroaryl, heterocyclyl or C 7-15 aralkyl; 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) 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, - NR1bR1c, - NR1bR1c, - NR1bR1c, - NR1bR1c (-) O) 2NR1bR1c, -SR1a, -S (O) R1a, -S (O) 2R1a, - S (O) NR1bR1c or -S (O) 2NR1bR1c R6, R7 and R9 are each deuterium; R10 and R11 are each independently (a) hydrogen; or (b) C 1-6 alkyl, C 2-6 alkenyl, C 2-6 alkynyl, C 3-7 cycloalkyl, C 6-14 aryl, heteroaryl, heterocyclyl or C 7-15 aralkyl; or R10 and R11 are linked together to form a heterocyclyl; R12 is (a) hydrogen; (b) C 1-6 alkyl, C 2-6 alkenyl, C 2-6 alkynyl, C 3-7 cycloalkyl, C 6-14 aryl, heteroaryl, heterocyclyl or C 7-15 aralkyl; or (c) -C (O) R1a, -C (O) OR1a, -C (O) NR1bR1c, - C (NR1a) NR1bR1c, -S (O) R1a, -S (O) 2R1a, -S (O ) NR1bR1c or -S (O) 2NR1bR1c; L is C1-6 alkylene; X is O or S; and each of R1a, R1b, R1c and R1d is independently hydrogen, deuterium, C1-6 alkyl, C2-6 alkenyl, C2-6 alkynyl, C3-7 cycloalkyl, heteroaryl, heterocyclyl or C6-14 aryl; or each pair of R1b and R1c together with the N atom to which it is attached independently form a heteroaryl or heterocyclyl; where each alkyl, alkylene, alkenyl, alkynyl, cycloalkyl, aryl, aralkyl, heterocyclyl and heteroaryl in R1, R2, R3, R4, R5, R8, R10, R11, R12, R1a, R1b, R1c, R1d
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