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LRRK2 kinase macrocyclic inhibitors
专利权人:
IPSEN PHARMA S.A.S.;Oncodesign S.A.
发明人:
HOFLACK, Jan,BLOM, Petra
申请号:
ES12798824
公开号:
ES2583477T3
申请日:
2012.09.28
申请国别(地区):
ES
年份:
2016
代理人:
摘要:
A compound of Formula I or a stereoisomer, tautomer, racemic, salt, hydrate, N-oxide or solvate form thereof, wherein A1 and A2 are selected from C and N; where when A1 is C, then A2 is N; and where when A2 is C, then A1 is N; R1 is selected from -H, -halo, -OH, -C1-6 alkyl, -C3-6 cycloalkyl, -O-C1-6 alkyl, -S-C1-6 alkyl, -NR9R10, - (C>; = O ) -R4, -SO2-R4, -CN, -NR9-SO2-R4, -Het1; wherein each of said C1-6 alkyl is optionally and independently substituted with 1 to 3 substituents selected from -halo, -OH, -NR11R12, -O-C1-6 alkyl, -S-C1-6 alkyl; R2 is selected from -H, -halo, -OH, -C 1-6 alkyl, -C 3-6 cycloalkyl, -O-C 1-6 alkyl, -S-C 1-6 alkyl, - (C>; = O) - alkyl C1-6, - (C>; = O) -O-C1-6 alkyl, - (C>; = O) -NR27R28, -Het3, - (C>; = O) -Het3, -SO2-C1-6 alkyl; wherein each of said C1-6 alkyl is optionally and independently substituted with 1 to 3 substituents selected from -halo, -OH, -O-C1-6 alkyl, -S-C1-6 alkyl, -Het3, -Ar2, -NR13R14; R3 is selected from -H, -halo, -OH, -C1-6 alkyl, -C3-6 cycloalkyl, -O-C1-6 alkyl, -S-C1-6 alkyl, - (C>; = O) - alkyl C1-6, - (C>; = O) -O-C1-6 alkyl, -Het2, - (C>; = O) -Het2, - (C>; = O) -NR29R30, -SO2 C1-6 alkyl; wherein each of said C1-6 alkyl is optionally and independently substituted with 1 to 3 substituents selected from -halo, -OH, -C1-6 alkyl, -C1-6 alkyl, -NR15R16, -Het2, -Ar4; R4 is selected from -halo, -OH, -C1-6 alkyl, -O-C1-6 alkyl, -S-C1-6 alkyl, -NR17R18, -Het4; R5 and R7 are each independently selected from -H, -halo, -C 1-6 alkyl, -C 1-6 alkyl, -S-C 1-6 alkyl, -Het5, -Ar1, -C3-6 cycloalkyl, -SO2- Ar3, -SO2, -SO2-C1-6 alkyl, - (C>; = O), - (C>; = O) -C1-6 alkyl, -O- (C>; = O) -C1-6 alkyl, - (C>; = O) -O-C 1-6 alkyl; wherein each of said C1-6 alkyl is optionally and independently substituted with 1 to 3 substituents selected from -halo, -OH, -C1-6 alkyl, -C1-6 alkyl, -Het5, -NR23R24; R6 is selected from -SO2, -SO2-C1-6 alkyl, - (C>; = O), - (C>; = S), - (C>; = O) -O-C1-6 alkyl, - (C>;
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