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 or condition to be measured by protein kinase a 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 or condition to be measured by protein kinase a 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n-氧化物的用途,化合物的用途,预防或治疗不健康的蛋白激酶b介导的病状或通过蛋白激酶a测量的病状来治疗或治疗以下疾病抑制蛋白激酶b和蛋白激酶a,以调节细胞过程,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 ITS SALT, SOLVATO, TAUTEMERO OR NOXIDE, USE OF A COMPOUND, METHODS FOR PROPHYLAXY OR TREATMENT OF A STATE OR DISEASE MEDIATED BY PROTEIN KINASE A, TO PROTEIN KINASE A, TO TREATE IN OR TO A protein kinase is a protein kinase A, to modulate a cell process, to treat an immune disorder in a mammalian and to induce apoptosis in a cancerous cell, and to make a preparation for the preparation of a cell. 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. R¬ 1¬ and NR¬ 2¬R¬ 3¬ and a maximum bitch length of 4 atoms, extending between E and NR¬ 2¬R¬ 3¬, where one of the carbon atoms of the linker group may optionally be substituted with an oxygen or nitrogen atom; and wherein the carbon atoms of 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. ¬R¬ 3¬ and provided that the oxo group, when present, is located on a carbon atom with respect to the group NR¬ 2¬R¬ 3¬; E is a monocyclic or bicyclic carbocyclic or heterocyclic group; R¬ 1¬ 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,TATEMEMERO或NOXIDE,化合物的使用,由蛋白激酶A介导的状态或疾病的预防或治疗方法,蛋白激酶A的处理或蛋白激酶的处理是一种蛋白激酶A,调节细胞过程,治疗哺乳动物的免疫失调和诱导癌细胞的凋亡,以及制备用于制备细胞的制剂,本发明提供了具有蛋白激酶B抑制活性的下式化合物: :其中A是含有1至7个碳原子的饱和烃连接基团,该连接基团的最大链长为5个原子延伸,R 1 1和NR 2 2 R 3 3以及最大母位长度为4在E和NR 2 -R 3-之间延伸的原子,其中连接基团的一个碳原子可任选被氧或氮原子取代;并且其中连接基团A的碳原子可任选包含一个或一个更多选自氧,氟和氢的取代基xy,条件是羟基存在时相对于基团NR 2不位于碳原子上。¬R3¬羟基存在时相对于基团NR 2不在碳原子上。到组NR¬2¬R¬3¬; E是单环或双环碳环或杂环基团; R1¬是芳基或杂芳基; R 2和R 3,R 4和R 5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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