http://rdf.ncbi.nlm.nih.gov/pubchem/patent/ES-2661510-T3

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filingDate 2012-12-14-04:00^^<http://www.w3.org/2001/XMLSchema#date>
grantDate 2018-04-02-04:00^^<http://www.w3.org/2001/XMLSchema#date>
inventor http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_7e65d4f3c8ae991af7119c9217789f09
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publicationDate 2018-04-02-04:00^^<http://www.w3.org/2001/XMLSchema#date>
publicationNumber ES-2661510-T3
titleOfInvention Use of inhibitors of PI3K activity or function
abstract 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, morpholinyl, thiomorpholinyl, piperazinyl, azepanyl, tiepanyl or oxepanyl; each of which is unsubstituted or substituted with 1-5 substituents independently selected from oxo, halogen, C1-C8 alkyl, halo-C1-C8 alkyl, hydroxy-C1-C8 alkyl, hydroxy, C1-C8 alkoxy, C1-C8-alkoxy-C1-C8-alkyl, amino, N-C1-C8-alkyl-amino, N, N-di-C1-C8-amino-alkyl, C1-C8-carbonyl, halo-alkyl- C1-C8-carbonyl, hydroxy-C1-C8-alkylcarbonyl or C1-C8-alkoxy-C1-C8-carbonyl; wherein 'heterocyclyl' can be attached to a heteroatom or a carbon atom and where the N and / or S heteroatoms can also optionally be oxidized to various oxidation states; wherein 'heteroaryl' is selected from furanyl, thiophenyl, pyrrolyl, imidazolyl, pyrazolyl, thiazolyl, isothiazolyl, oxazolyl, isoxazolyl, 1,2,5-oxadiazolyl, 1,2,4-oxadiazolyl, 1,2,3-oxadiazolyl , 1,3,4-oxadiazolyl, 1,2,5-thiadiazolyl, 1,2,4-thiadiazolyl, 1,2,3-thiadiazolyl, 1,3,4-thiadiazolyl, 1,2,3-triazolyl, 1 , 2,4-triazolyl, 1,2,5-triazolyl, pyridyl, pyrimidinyl, pyrazinyl, pyridazinyl, 1,2,3-triazinyl, 1,2,4-triazinyl or 1,3,5-triazinyl; each of which is unsubstituted or substituted with 1-5 substituents independently selected from halogen, C1-C8 alkyl, halo-C1-C8 alkyl, hydroxy-C1-C8 alkyl, hydroxyl, C1-C8 alkoxy, alkoxy C1-C8-C1-C8-alkyl, amino, N-C1-C8-alkyl-amino, N, N-di-C1-C8-amino, alkyl-C1-C8-carbonyl, halo-C1-alkyl C8-carbonyl, hydroxy-C1-C8-alkylcarbonyl or C1-C8-alkoxy-C1-C8-alkylcarbonyl; wherein "heteroaryl" can be attached to a heteroatom or a carbon atom and where the N and / or S heteroatoms can also optionally be oxidized to various oxidation states; R2 is selected from phenyl, naphthyl, pyridyl, pyrimidinyl, pyrazinyl, pyridazinyl, quinolinyl or isoquinolinyl, each of which is unsubstituted or substituted with 1-5 substituents independently selected from halogen, cyano, nitrogen, C1-C8 alkyl, halo-C1-C8alkyl, hydroxy-C1-C8-alkyl, hydroxyl, C1-C8-alkoxy, C1-C8-alkoxy-C1-C8-alkyl, amino, N-C1-C8-amino-alkyl, N, N- di-C1-C8-amino-alkyl, C1-C8-carbonyl alkyl, halo-C1-C8-alkylcarbonyl, hydroxy-C1-C8-alkylcarbonyl or C1-C8-alkoxy-C1-C8- carbonyl; R3 is selected from H, C1-C4 alkyl or halo-C1-C4 alkyl; and m is selected from 0 or 1.
priorityDate 2011-12-15-04:00^^<http://www.w3.org/2001/XMLSchema#date>
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