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Condensed heteroaromatic pyrrolidinones as SYK inhibitors
专利权人:
TAKEDA PHARMACEUTICAL COMPANY LIMITED
发明人:
ARIKAWA, YASUYOSHI,JONES, BENJAMIN,LAM, BETTY,NIE, ZHE,SMITH, CHRISTOPHER,TAKAHASHI, MASASHI,DONG, QING,FEHER, VICTORIA
申请号:
ES10800835
公开号:
ES2545616T3
申请日:
2010.12.17
申请国别(地区):
ES
年份:
2015
代理人:
摘要:
A compound of Formula 1, ** Formula ** or a pharmaceutically acceptable salt thereof, wherein: G is C (R5); L1 and L2 are each independently selected from -NH- and a link; R1 and R2 are each independently selected from hydrogen, halo, C1-3 alkyl, and C1-3 haloalkyl, or R1 and R2, together with the atom to which they are attached, form a C3-6 cycloalkyl; R3 is selected from C2-6 alkyl, C3-8 cycloalkyl, C2-5 heterocyclyl, and C1-9 heteroaryl, each optionally substituted with one to five substituents independently selected from halo, oxo, -NO2, -CN, R6 and R7; R4 is selected from C3-8 cycloalkyl, C2-5 heterocyclyl, C6-14 aryl, and C1-9 heteroaryl, each optionally substituted with one to five substituents independently selected from halo, oxo, -CN, R6 and R7 ; R5 is selected from hydrogen, halo, -CN, C1-4 alkyl, C2-4 alkenyl, C2-4 alkynyl, C2-5 heterocyclyl, C1-5 heteroaryl and R10, wherein the alkyl, alkenyl, alkynyl moieties are , each optionally substituted with one to five substituents independently selected from halo, -CN, oxo and R10, and wherein the heterocyclyl moiety has 3 to 6 ring atoms and the heteroaryl moiety has 5 or 6 atoms of ring, and the heterocyclyl and heteroaryl moieties are each optionally substituted with one to four substituents independently selected from halo, -NO2, -CN, C1-4 alkyl, C2-4 alkenyl, C2-4 alkynyl, C1 haloalkyl -4 and R10; each R6 is independently selected from -OR8, -N (R8) R9, -NR8C (O) R9, -C (O) R8, -C (O) OR8, - C (O) N (R8) R9, - C (O) N (R8) OR9, -C (O) N (R8) S (O) 2R9, -N (R8) S (O) 2R9, -S (O) nR8, and -S (O) 2N (R8) R9; each R7 is independently selected from C1-6 alkyl, C2-6 alkenyl, C2-6 alkynyl, C3- 6- cycloalkyl m-, C6-14- (CH2) m- aryl, C2-5- (heterocyclyl) CH2) m-, and C1-9 heteroaryl- (CH2) m-, each optionally substituted with one to five substituents independently selected from halo, oxo, -NO2, -CN, C1-6 alkyl, C1-6 haloalkyl and R10; each R8 and R9 is independently selected from hydrogen or from C1-6 alkyl, C2-6
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