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Phosphoinositide 3-kinase inhibitor compounds and methods of use
专利权人:
F. HOFFMANN-LA ROCHE AG;GENENTECH, INC.
发明人:
BAYLISS, TRACY,CCHUCKOWREE, IRINA,FOLKES, ADRIAN,OXENFORD, SALLY,WAN, NAN CHI,CASTANEDO, GEORGETTE,GOLDSMITH, RICHARD,GUNZER, JANET,HEFFRON, TIM,MATHIEU, SIMON,OLIVERO, ALAN,STABEN, STEVEN,SUTHERLIN,
申请号:
ES12177885
公开号:
ES2544082T3
申请日:
2007.12.05
申请国别(地区):
ES
年份:
2015
代理人:
摘要:
With compound selected from Formula la and Formula lb: ** Formula ** and stereoisomers, geometric isomers, tautomers, solvates, and pharmaceutically acceptable salts thereof, in which: X is O or S; R1 is a group of the formula: ** Formula ** R2 is selected from H, F, Cl, Br, I, and C1-C6 alkyl; R3 is a monocyclic heteroaryl group selected from pyridyl, isoxazolyl, imidazolyl, pyrazolyl, pyrrolyl, thiazolyl, pyridazinyl, pyrimidinyl, pyrazinyl, oxazolyl, furanyl, thienyl, triazolyl, tetrazolyl group, in which the monocyclic heteroaryl group is substituted with one or more groups selected from F, Cl, Br, I, -CN, -NR10R11, - OR10, -C (O) R10, - NR10C (O) R11, -N (C (O) R11) 2, -NR10C (O) NR10R11 , -NR12S (O) 2R10, -C (>; = O) OR10, - C (>; = O) NR10R11, C1-C12 alkyl and (C1-C12 alkyl) -OR10; R4 and R5 form, together with the N atom to which they are attached, a group selected from piperazine, piperidine, pyrrolidine, oxazolidinone, morpholine, thiomorpholine, diazepane and 2,5-diaza-bicyclo [2.2.1] -heptane, whose group is optionally substituted with one or more groups independently selected from F, Cl, Br, I, -CN, CF3, - NO2, oxo, -C (>; = Y) R10, -C (>; = Y) OR10, -C (>; = Y) NR10R11, - (CR14R15) nNR10R11, - (CR14R15) nNR12SO2R10, - (CR14R15) nOR10, -NR10R11, -NR12C (>; = Y) R10, -NR12C (>; = Y) OR11, -NR12C (>; = Y) NR10R11, -NR12SO2R10,>; = NR12, OR10, -OC (>; = Y) R10, - OC (>; = Y) OR10, -OC (>; = Y) NR10R11, -OS (O) 2 (OR10) , -OP (>; = Y) (OR10) (OR11), -OP (OR10) (OR11), SR10, -S (O) R10, -S (O) 2- (C1-C6 alkyl) -S (O ) 2R10, -S (O) 2R10, -S (O) 2NR10R11, -S (O) (OR10), -S (O) 2 (OR10), -SC (>; = Y) R10, -SC (>; = Y) OR10, - SC (>; = Y) NR10R11, optionally substituted C1-C12 alkyl, optionally substituted C2-C8 alkenyl, optionally substituted C2-C8 alkynyl, optionally substituted C3-C12 carbocyclyl, optionally substituted C2-C20 heterocyclyl stituido, optionally substituted C6-C20 aryl, and optionally substituted C1-C20 heteroary
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