- Achieving multi-isoform PI3K inhibition in a series of substituted 3,4-dihydro-2H-benzo[1,4]oxazines
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The SAR and pharmacokinetic profiles of a series of multi-isoform PI3K inhibitors based on a 3,4-dihydro-2H-benzo[1,4]oxazine scaffold are disclosed.
- Perry, Benjamin,Alexander, Rikki,Bennett, Gavin,Buckley, George,Ceska, Tom,Crabbe, Tom,Dale, Verity,Gowers, Lewis,Horsley, Helen,James, Lynwen,Jenkins, Kerry,Crepy, Karen,Kulisa, Claire,Lightfoot, Helen,Lock, Chris,Mack, Stephen,Morgan, Trevor,Nicolas, Anne-Lise,Pitt, Will,Sabin, Verity,Wright, Sara
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- LIGAND-DIRECTED COVALENT MODIFICATION OF PROTEIN
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The present invention relates to enzyme inhibitors. More specifically, the present invention relates to ligand-directed covalent modification of proteins; method of designing same; pharmaceutical formulation of same; and method of use.
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(2013/03/26)
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- PI3 KINASE INHIBITORS AND USES THEREOF
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The present invention provides compounds, compositions thereof, and methods of using the same.
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- FUSED THIAZOLE AND THIOPHENE DERIVATIVES AS KINASE INHIBITORS
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A series of fused bicyclic thiazole and thiophene derivatives which are substituted in the 2-position by an optionally substituted morpholin-4-yl moiety, and in the 4-position by hydroxy, oxo or an amine moiety, being selective inhibitors of PI3 kinase enzymes, are accordingly of benefit in medicine, for example in the treatment of inflammatory, autoimmune, cardiovascular, neurodegenerative, metabolic, oncological, nociceptive or ophthalmic conditions. (I)
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Page/Page column 99
(2009/07/17)
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- PYRROLOTHIAZOLES AS PI3-KINASE INHIBITORS
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A series of 4,5-dihydro-6H-pyrrolo[3,4-d][1,3]thiazol-6-one derivatives, and analogues thereof, which are substituted in the 2-position by an optionally substituted morpholin-4-yl moiety, being selective inhibitors of PI3 kinase enzymes, are accordingly o
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Page/Page column 73-74
(2009/07/17)
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- TRICYCLIC KINASE INHIBITORS
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A series of fused tricyclic thiazole and thiophene derivatives which are substituted in the 2-position of the thiazole or thiophene ring by an optionally substituted morpholin-4-yl moiety, being selective inhibitors of PI3 kinase enzymes, are accordingly
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Page/Page column 104
(2009/07/17)
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- FUSED THIAZOLE DERIVATIVES AS KINASE INHIBITORS
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A series of 6,7-dihydro[1,3]thiazolo[5,4-c]pyridin-4(5H)-one derivatives, and analogues thereof, which are substituted in the 2-position by an optionally substituted morpholin-4-yl moiety, being selective inhibitors of PI3 kinase enzymes, are accordingly of benefit in medicine, for example in the treatment of inflammatory, autoimmune, cardiovascular, neurodegenerative, metabolic, oncological, nociceptive or ophthalmic conditions.
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Page/Page column 184
(2008/06/13)
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