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.
The Institute Of Cancer Research : Royal Cancer Hospital;Cancer Research Technology Limited;Astex Therapeutics Limited
发明人:
David Winter Walker,Gordon Saxty,Hannah Fiona Sore,Ian Collins,Marinus Leendert Verdonk,Paul Graham Wyatt,Robert Downham,Robert Georg Boyle,Robin Arthur Ellis Carr,Steven John Woodhead,Valerio Berdini,DAVID WINTER WALKER,GORDON SAXTY,HANNAH FIONA SORE,IAN COLLINS,Marinus Lee
申请号：
BRPI0418078
公开号：
BRPI0418078A8
申请日:
2004.12.23
申请国别(地区):
BR
年份:
2018
代理人:
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."composto ou um seu sal, solvato, tautômero ou nóxido, uso de um composto, métodos para a profilaxia ou tratamento de um estado ou condição doentia mediada pela proteína quinase b e mediada pela proteína quinase a, para tratar uma doença ou condição, para inibir uma proteína quinase b e uma proteína quinase a, para modular um processo celular, para tratar um distúrbio imune e
