283608-49-1Relevant academic research and scientific papers
2 -MORPHOLINOPYRIMIDINES AND THEIR USE AS PI3 KINASE INHIBITORS
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Page/Page column 98, (2009/06/27)
Morpholino pyrimidines of formula (I): wherein R1 is selected from -Y-R6 and -NR4R5; R2 is a N-containing monocyclic heteroaryl group which is selected from pyridyl, isoxazolyl, imidazolyl, pyrazolyl, pyrrolyl, thiazolyl, pyridazinyl, pyrimidinyl, pyrazinyl, oxazolyl, furanyl, thienyl, triazolyl and tetrazolyl and which is unsubstituted or substituted by halo, -CN, -NR10R11, -OR10, -C(O)R10, -NR10C(O)R11, - N(C(O)R11)2, -NR10C(O)NR10R11, -SO2R10R11, -SO2NR10R11, -C(=O)OR10, -C(=O)NR10R11, halo-C1 -C6 alkyl and unsubstituted C1-C12 alkyl; R3 is selected from H, C1-C6 alkyl and C1-C6 alkoxy; Y is selected from a direct bond, -(CR2)m-, C2-C6 alkenylene, C2-C6 alkynylene, -(CR2)p-O-(CR2) t-, -(CR2)p-NR-(CR2) t, -(CR2)p-NR-(CR2)n-C(O)-, -(CR2)p-NR-C(O)- (CR2)n-, -(CR2)p-C(O)-NR-(CR2) t, -(CR2)p-C(O)-(CR2)n-NR-(CR2)t,- and -(CR2)p- C(O)-(CR2)n-; R6 is selected from an unsaturated 5- to 12-membered carbocyclic or heterocyclic ring, a saturated 5-, 6- or 7- membered N-containing heterocyclic group which is unsubstituted or substituted, C1-C6 alkyl, -NR2, -OR, -NR(CO)R and - C(O)NR2; R4 and R5, which are the same or different, are both C1-C6 alkyl which is unsubstituted or substituted, or R4 and R5 together form, with the nitrogen atom to which they are attached, a saturated 5-, 6- or 7- membered N-containing heterocyclic group which is unsubstituted or substituted; each R, which are the same or different when more than one is present in a given group, is independently H, C1-C6 alkyl which is unsubstituted or substituted or a 5- to 12-membered aryl or heteroaryl group which is unsubstituted or substituted; R10 and R11, which are the same or different, are independently selected from H, C1-C6 alkyl, C2-C6 alkenyl, C2-C6 alkynyl and C3-C8 cycloalkyl; n is 0 or an integer of 1 to 6; m is an integer of 1 to 6; p is 0 or an integer of 1 to 6; and t is 0 or an integer of 1 to 6, with the proviso that t is an integer of 2 to 6 when R6 is linked to Y through a constituent O or N atom of R6; and the pharmaceutically acceptable salts thereof, subject to various provisos, have activity as inhibitors of PI3K and may thus be used to treat diseases and disorders arising from abnormal cell growth, function or behaviour, particularly that associated with PI3 kinase such as cancer, immune disorders, cardiovascular disease, viral infection, inflammation, metabolism/endocrine disorders and neurological disorders. Processes for synthesizing the compounds are also described
BETA-AMYLOID PROTEIN PRODUCTION/SECRETION INHIBITORS
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Page 72, (2010/02/08)
Provided are novel compounds having an inhibitory activity against production or secretion of β-amyloid protein. They embrace compounds represented by the following formula (1): and capable of being replaced with a variety of substituents; and salts thereof, and solvates of any one of them.
