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6-amino-7-deaza-purine derivatives, a process for its preparation and its use as kinase inhibitors

机译:6-氨基-7-脱氮嘌呤衍生物,其制备方法及其作为激酶抑制剂的用途

摘要

A compound of formula (I) ** Formula ** characterized in that R1 is hydrogen, methyl, cyclopropyl or COR6, where R6 is methyl; R2 is hydrogen or an optionally substituted group selected from linear or branched (C1-C8) alkyl, (C3-C8) cycloalkyl, aryl, heteroaryl, a 3- to 4- or 6- to 7-membered heterocyclyl ring, where one or more atoms Carbon atoms are replaced by nitrogen, sulfur, or oxygen, and a 5-membered heterocyclyl ring where one or more carbon atoms are replaced by nitrogen or sulfur; R3 is hydrogen, (C1-C8) alkyl, (C2-C8) alkenyl, heterocyclyl, aryl or heteroaryl; A is C = C; R4 is hydrogen, halogen, hydroxyl, an optionally substituted (C1-C3) alkyl or cyano; R5 is a group -L-R7, where R7 is hydrogen or an optionally substituted group selected from linear (C1-C8) alkyl, (C3-C8) cycloalkyl and aryl; and L is -CON (Y) -, -NHCO-, -SO2N (Y) -, -NHSO2-, -NHCOCH2-, -CH2CONH-, where Y is hydrogen or, taken together with the nitrogen atom to which they are attached , Y and R7 can form an optionally substituted 3-6 membered heterocyclyl, optionally containing an additional heteroatom selected from nitrogen, sulfur or oxygen; or pharmaceutically acceptable salts thereof, with the proviso that if L is -CH2CONH-, then R2 is different from hydrogen, and that a compound where R2 is cycloalkyl (C5) is excluded.
机译:式(I)**式**的化合物,其特征在于,R 1是氢,甲基,环丙基或COR 6,其中R 6是甲基; R 2是氢或选自直链或支链(C 1 -C 8)烷基,(C 3 -C 8)环烷基,芳基,杂芳基,3至4或6至7元杂环基环的任选取代的基团,其中一个或更多原子碳原子被氮,硫或氧取代,以及一个五元杂环基环,其中一个或多个碳原子被氮或硫取代; R3是氢,(C1-C8)烷基,(C2-C8)烯基,杂环基,芳基或杂芳基; A是C> = C; R4为氢,卤素,羟基,任选取代的(C1-C3)烷基或氰基; R5是基团-L-R7,其中R7是氢或选自直链(C1-C8)烷基,(C3-C8)环烷基和芳基的任选取代的基团;并且L是-CON(Y)-,-NHCO-,-SO 2 N(Y)-,-NHSO 2-,-NHCOCH 2-,-CH 2 CONH-,其中Y是氢或与它们所连接的氮原子一起,Y和R 7可以形成任选取代的3-6元杂环基,任选地含有选自氮,硫或氧的另外的杂原子;或其药学上可接受的盐,条件是如果L为-CH2CONH-,则R2与氢不同,并且排除其中R2为环烷基(C5)的化合物。

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