COOKE, Nigel Graham,FERNANDES GOMES DOS SANTOS, Paulo Antonio,FURET, Pascal,HEBACH, Christina,HÖGENAUER, Klemens,HOLLINGWORTH, Gregory,KALIS, Christoph,LEWIS, Ian,SMITH, Alexander Baxter,SOLDERMANN, N
申请号：
ES12818825
公开号：
ES2661510T3
申请日:
2012.12.14
申请国别(地区):
ES
年份:
2018
代理人:
摘要：
A PI3K inhibitor, in which said inhibitor has an inhibitory action on the isoform of the PI3K delta, for use in the treatment of immunopathology in a subject suffering from a disease or a disorder selected from acute and cerebral malaria, by means of of functional inhibition of TLR9 of the infected subject, in which the PI3K inhibitor is selected from tetrahydro-pyrido-pyrimidine compounds of formula (I) and / or tautomers and / or N-oxides and / or pharmaceutically acceptable salts of the same, ** (See formula) ** in which: Y is selected from O or NR3； R1 is selected from phenyl, pyridyl, pyrimidinyl, pyrazinyl, pyridazinyl, 1,2,3-triazinyl, 1,2,4-triazinyl, 1,3,5-triazinyl, or -C (O) -R4 in which R4 is selected from C1-C8 alkyl, halo-C1-C8 alkyl, hydroxy-C1-C8 alkyl, C1-C8 alkoxy-C1-C8 alkyl, C1-C8 alkyl-sulfonyl-C1-C8 alkyl, heterocyclyl , heterocyclyl-oxy, heterocyclyl-C1-C8-alkyl, cycloalkyl-C3-C12, cycloalkyl-C3-C12-alkyl-C1-C8, heteroaryl, heteroaryl-oxy, heteroaryl-C1-C8 alkyl, hydroxy, C1-alkoxy C8, amino, N-C1-C8-amino-alkyl or N, N-di-C1-C8-alkyl-amino, wherein `C1-C8-alkyl 'in N-C1-C8-amino-alkyl and N , N-di-C1-C8-alkyl-amino may be substituted or unsubstituted with halogen, hydroxy or C1-C4 alkoxy； wherein "C3-C12 cycloalkyl" in C3-C12 cycloalkyl and C3-C12-cycloalkyl-C1-C8 alkyl may be substituted or unsubstituted with 1-5 substituents independently selected from oxo, halogen, C1-alkyl C8, halo-C1-C8 alkyl, hydroxy-C1-C8 alkyl, hydroxy, C1-C8 alkoxy, C1-C8 alkoxy-C1-C8 alkyl, amino, N-C1-C8-amino-alkyl, N, N-dialkyl-C1-C8-amino, alkyl-C1-C8-carbonyl, halo-C1-C8-alkylcarbonyl, hydroxy-C1-C8-alkylcarbonyl or C1-C8-alkoxy-C1-C8-alkyl carbonyl； wherein 'heterocyclyl' is selected from oxyranyl, aziridinyl, oxetanyl, thienyl, acetylinyl, pyrrolidinyl, tetrahydrofuranyl, tetrahydrothiophenyl, 2,3-dihydrofuranyl, 2,5-dihydrofuranyl, 2,3-dihydrothiophenyl, 1-pyrrolinyl, 2- pyrrolinyl , 3-pyrrolinyl, tetrahydropyranyl, piperidinyl, tetrahydrothiopyranyl, morpho
