首页> 外国专利> 3- (SUBSTITUTED AMINO) PYRAZOLO 3,4-d PYRIMIDINES AS EFRIN B (EphB) KINASE INHIBITORS AND VASCULAR EPITELIAL GROWTH FACTOR 2 (VEGFR2) KINASE

3- (SUBSTITUTED AMINO) PYRAZOLO 3,4-d PYRIMIDINES AS EFRIN B (EphB) KINASE INHIBITORS AND VASCULAR EPITELIAL GROWTH FACTOR 2 (VEGFR2) KINASE

机译:3-(取代的氨基酸)吡唑并[3,4-d]嘧啶类药物作为EFRIN B(EphB)激酶抑制剂和血管内皮生长因子2(VEGFR2)激酶

摘要

1. The compound of the formula! ! where R1 is hydrogen, unsubstituted or substituted alkyl, or unsubstituted or substituted aryl; ! R2 is hydrogen, halo, unsubstituted or substituted aryl, unsubstituted or substituted cycloalkyl, unsubstituted or substituted alkyl, substituted carbonyl or unsubstituted or substituted heterocyclyl; ! R3 is hydrogen, halo, C1-C4 alkyl, C1-C4 alkoxy or cyano; ! each R4, independently of any of the others present, is a halo group, in particular fluoro, methyl, methoxy, or C1-4alkylpiperazine C1-4alkyl; ! And denotes C (= O) -N (R5) or N (R5) -C (= O), where! R5 is hydrogen or unsubstituted or substituted alkyl; ! R6 is hydrogen or unsubstituted or substituted alkyl; ! X is CH or N; and! n denotes from 0 to 2,! in free or salt form. ! 2. The compound according to claim 1 of formula I, where! R1 is hydrogen,! unsubstituted or substituted C1-C7 alkyl, for example methyl, ethyl or propyl, which may be linear or branched one or more times, and which is unsubstituted or substituted by one or more, preferably up to three, substituents independently selected from the group consisting of unsubstituted or substituted heterocyclyl as described below for R2, in particular a pyrrolidino group, a piperidino group, a piperidino group substituted with an amino group or an N-mono- or N, N-di- [C1-C7 alkyl, phenyl and / or phenyl C1-C7 alkyl) amino group, unsubstituted or N-C1-C7alki substituted piperidinyl bonded via a ring carbon atom, such as 1-isopropylpiperidin-4-yl, a piperazino group, a C1-C7 alkylpiperazino group such as a 4- (methyl, ethyl or isopropyl) piperazino group, morpholino group
机译:1.配方的化合物! !其中R1是氢,未取代或取代的烷基,或未取代或取代的芳基; ! R2为氢,卤素,未取代或取代的芳基,未取代或取代的环烷基,未取代或取代的烷基,取代的羰基或未取代或取代的杂环基; ! R3是氢,卤素,C1-C4烷基,C1-C4烷氧基或氰基; !每个R 4,独立于所存在的任何其他基团,是卤素基团,特别是氟,甲基,甲氧基或C 1-4烷基哌嗪C 1-4烷基; !并表示C(= O)-N(R5)或N(R5)-C(= O),其中! R5是氢或未取代或取代的烷基; ! R6是氢或未取代或取代的烷基; ! X为CH或N;和! n表示从0到2!呈游离或盐形式。 ! 2.根据权利要求1的式I的化合物,其中! R1是氢!未取代或取代的C 1 -C 7烷基,例如甲基,乙基或丙基,其可以是直链或支化一次或多次,并且未被取代或被一个或多个,优选至多三个独立地选自以下的取代基取代如下对R 2所述的未取代或取代的杂环基,特别是吡咯烷基,哌啶子基,被氨基或N-单或N,N-二-[C 1 -C 7烷基,苯基和N-取代的哌啶子基。 (或苯基C1-C7烷基)氨基,未取代的或经环碳原子键合的N-C1-C7烷基取代的哌啶基,例如1-异丙基哌啶-4-基,哌嗪子基,C1-C7烷基哌嗪子基4-(甲基,乙基或异丙基)哌嗪基,吗啉基

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