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4(HETERO-) ARYL SUBSTITUTED (THIA-/OXA-/PYRA) ZOLES FOR INHIBITION OF TIE-2

机译:用于抑制TIE-2的4(杂)芳基取代(THIA- / OXA- / PYRA)唑

摘要

The inventione relates to a compound of formula (I), wherein V is H or, or, R1 can be independently H, alkyl, alkenyl, cycloalkyl, heteroalkyl, aryl, heteroaryl, arylalkyl, alkylaryl, N-R6R7, N- (CO) R6R7, N-R6 (CO) R7 or N- (CO) -O-R6R7 , R8 can be independently H, alkyl, alkenyl, cycloalkyl, heteroalkyl, aryl, heteroaryl, arylalkyl, alkylaryl, N-R3R4, N- (CO) R3R4, N-R3 (CO) R4, N- (CO) -O-R3R4, O-R3, CO-R3, CO-OR3 or O-CO-R3, R2, R5, can be independently H, alkyl, alkenyl, cycloalkyl, heteroalkyl, aryl, heteroaryl, arylalkyl, alkylaryl, carboxyl, Br, C1, F, CF3, R3, R4, R6, R7 can be independently H, alkyl, alkenyl, cycloalkyl, heteroalkyl, aryl, heteroaryl, arylalkyl, alkylaryl, COOR5 and CO-R5, and may form a ring structure, X, Y, Z can be independently CH or N, and U can be independently S or NH, W can be independently NH, O or S, and racemic-diastereomeric mixtures, optical isomers, and pharmaceutically acceptable salts thereof, to a method of inhibiting the activity of one or more protein kinases by using these compounds in vitro or in cell culture, and to a pharmaceutical composition comprising such a compound and to their use as a medicament.
机译:本发明涉及式(I)的化合物,其中V是H或,或R 1可以独立地是H,烷基,烯基,环烷基,杂烷基,芳基,杂芳基,芳基烷基,烷基芳基,N-R6R7,N-(CO )R6R7,N-R6(CO)R7或N-(CO)-O-R6R7,R8可独立为H,烷基,烯基,环烷基,杂烷基,芳基,杂芳基,芳基烷基,烷基芳基,N-R3R4,N-( CO)R3R4,N-R3(CO)R4,N-(CO)-O-R3R4,O-R3,CO-R3,CO-OR3或O-CO-R3,R2,R5可独立为H,烷基,烯基,环烷基,杂烷基,芳基,杂芳基,芳基烷基,烷基芳基,羧基,Br,Cl,F,CF 3,R3,R4,R6,R7可独立地为H,烷基,烯基,环烷基,杂烷基,芳基,杂芳基,芳基烷基,烷基芳基,COOR5和CO-R5并可以形成环结构,X,Y,Z可以独立地为CH或N,U可以独立地为S或NH,W可以独立地为NH,O或S,且外消旋-非对映异构体混合物,旋光异构体及其药学上可接受的盐,以抑制一种或多种化合物的活性的方法通过在体外或细胞培养中使用这些化合物来制备蛋白激酶,以及用于包含该化合物的药物组合物及其作为药物的用途。

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