首页> 外国专利> compound or a salt, solvate, tautomer or n-oxide thereof, use of a compound, methods for the prophylaxis or treatment of an unhealthy protein kinase b-mediated condition and condition to treat a disease or condition for inhibiting a protein kinase b and a protein kinase a, to modulate a cellular process, to treat an immune disorder in a mammal and to induce apoptosis in a cancer cell, pharmaceutical composition, and process for the preparation of a compound.

compound or a salt, solvate, tautomer or n-oxide thereof, use of a compound, methods for the prophylaxis or treatment of an unhealthy protein kinase b-mediated condition and condition to treat a disease or condition for inhibiting a protein kinase b and a protein kinase a, to modulate a cellular process, to treat an immune disorder in a mammal and to induce apoptosis in a cancer cell, pharmaceutical composition, and process for the preparation of a compound.

机译:化合物或其盐,溶剂化物,互变异构体或正氧化物,该化合物的用途,预防或治疗不健康的蛋白激酶b介导的病症的方法以及治疗抑制蛋白激酶b和a的疾病或病症的条件蛋白激酶a,调节细胞过程,治疗哺乳动物的免疫疾病并诱导癌细胞的凋亡,药物组合物和化合物的制备方法。

摘要

"compound or a salt, solvate, tautomer or oxide thereof, use of a compound, methods for the prophylaxis or treatment of an unhealthy protein kinase b-mediated condition and condition, to treat a disease or condition, to inhibit a protein kinase b and a protein kinase a, to modulate a cellular process, to treat an immune disorder in a mammal and to induce apoptosis in a cancer cell, pharmaceutical composition, and process for the preparation of a compound. " The invention provides compounds of formula: having protein kinase b inhibitory activity: wherein a is a saturated hydrocarbon linker group containing from 1 to 7 carbon atoms, the linker group having a maximum chain length of 5 atoms, extending between r ^ 1 ^ and nr ^ 2 ^ r ^ 3 ^ and a maximum bitch length of 4 atoms, extending between and nr ^ 2 ^ r ^ 3 ^, wherein one of the carbon atoms of the linker group may be optionally be substituted with an oxygen or nitrogen atom; and wherein the carbon atoms of the linker group a may optionally contain one or more substituents selected from oxo, fluoro and hydroxy, provided that the hydroxy group, when present, is not located on a carbon atom with respect to the group nr 2 provided that the oxo group, when present, is located on a carbon atom with respect to the group nr ^ 2 ^ r ^ 3 ^; and is a monocyclic or bicyclic carbocyclic or heterocyclic group; R1 is an aryl or heteroaryl group; and r ^ 2 ^, r ^ 3 ^, r ^ 4 ^ and r ^ 5 ^ are as defined in the claims. Pharmaceutical compositions containing the compounds, methods for preparing the compounds and their use as anticancer agents are also provided.
机译:“化合物或其盐,溶剂化物,互变异构体或氧化物,在预防或治疗不健康的蛋白激酶b介导的疾病和病症的方法,用途,治疗疾病或抑制蛋白激酶b和蛋白激酶a,调节细胞过程,治疗哺乳动物的免疫疾病并诱导癌细胞的凋亡,药物组合物和化合物的制备方法。激酶b抑制活性:其中a为含1至7个碳原子的饱和烃连接基,该连接基的最大链长为5个原子,在r ^ 1 ^和nr ^ 2 ^ r ^ 3 ^之间延伸,而a最大母位长度为4个原子,在nr ^ 2 ^ r ^ 3 ^和nr ^ 2 ^之间延伸,其中连接基团的碳原子之一可以任选地被氧或氮原子取代;并且其中连接基团a的碳原子可任选地包含一个或多个选自氧代,氟代和羟基的取代基,条件是该羟基(当存在时)相对于基团nr 2不位于碳原子上,当存在时,氧代基团相对于基团nr ^ 2 ^ r ^ 3 ^位于碳原子上;并且是单环或双环碳环或杂环基团; R1是芳基或杂芳基; r ^ 2 ^,r ^ 3 ^,r ^ 4 ^和r ^ 5 ^如权利要求中所定义。还提供了包含所述化合物的药物组合物,制备所述化合物的方法及其作为抗癌剂的用途。

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