abstract |
REFERS TO COMPOUNDS DERIVED FROM 2- (1H-PYRAZOLO [3,4-d] PYRIMIDIN-1-ILMETHYL) QUINAZOLIN-4 (3H) -ONE OF FORMULA (I) WHERE R1 IS H, ALKYL (C1-C15) IN WHERE ONE OR SEVERAL CARBONS CAN BE REPLACED BY A HETEROATOM SUCH AS O, N, AMONG OTHERS AND IS OPTIONALLY SUBSTITUTED WITH HALOGEN, ARYL, HETEROARIL, AMONG OTHERS; R3a IS HYDROXYL; R3b IS H, HYDROXYL, HALO, CN, AMONG OTHERS; R4 AND R5 ARE EACH H OR ALKYL (C1-C3); X IS ARYL (C6-C10) OR HETEROARYL (C5-C9) SUBSTITUTED WITH R2a AND R2b, WHERE R2a IS H, ALKYL (C1-C3), HALO, CN, AMONG OTHERS; R2b IS H, ALKYL (C1-C3), HALO, HALOALKYL (C1-C3). THE PREFERRED COMPOUNDS ARE: 2 - ((4-AMINO-3- (3-HYDROXYPHENYL) -1H-PIRAZOLO [3,4-d] PYRIMIDIN-1-IL) METHYL) -3- (2-CHLOROBENZYL) -5-ETHINYLQUINAZOLINE -4 (3H) -ONA; 6- (2 - ((4-AMINO-3- (4-HYDROXYPHENYL) -1H-PYRAZOLO [3,4-d] PYRIMIDIN-1-IL) METHYL) -3- (2-CHLOROBENZYL) -4-OXO- 3,4-DIHYDROQUINAZOLINE-5-IL) HEX-5-INOICO; 2-ACETAMIDO-N- (3- (2 - ((4-AMINO-3- (3-HYDROXYPHENYL) -1H-PYRAZOLO [3,4-d] PYRIMIDIN-1-IL) METHYL) -3- (2- CHLOROBENZYL) -4-OXO-3,4-DIHYDROQUINAZOLIN-5-IL) PROP-2-IN-1-IL) ACETAMIDE; AMONG OTHERS. IT ALSO REFERS TO A PHARMACEUTICAL COMPOSITION. SUCH COMPOUNDS ARE INHIBITORS OF PHOSPHOINOSITIDA 3-KINASES (PI3 KINASES), BEING USEFUL IN THE TREATMENT OF ASTHMA, CYSTIC FIBROSIS, SINUSITIS, ALLERGIC DERMATITIS |