- SULFONYLUREA DERIVATIVES AND USES THEREOF
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The present disclosure relates to compounds of Formula (I) and to their prodrugs, pharmaceutically acceptable salts, pharmaceutical compositions, methods of use, and methods for their preparation. The compounds disclosed herein are useful for inhibiting the maturation of cytokines of the IL-1 family by inhibiting inflammasomes and may be used in the treatment of disorders in which inflammasome activity is implicated, such as inflammatory, autoinflammatory and autoimmune diseases and cancers.
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Paragraph 01545-01546
(2020/12/30)
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- HETEROCYCLIC COMPOUNDS AND USES THEREOF
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Compounds and pharmaceutical compositions of formulae (I), (XI) and (XII) as PI3 kinase modulators and their use in the treatment of diseases such as cancer.
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Paragraph 00563
(2013/03/26)
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- HETEROCYCLIC COMPOUNDS AND USES THEREOF
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Compounds and pharmaceutical compositions that modulate kinase activity, including PI3 kinase activity, and compounds, pharmaceutical compositions, and methods of treatment of diseases and conditions associated with kinase activity, including PI3 kinase activity, are described herein.
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Page/Page column 00704
(2013/03/26)
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- HETEROCYCLIC COMPOUNDS AND USES THEREOF
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Compounds and pharmaceutical compositions that modulate kinase activity, including PI3 kinase activity, and compounds, pharmaceutical compositions, and methods of treatment of diseases and conditions associated with kinase activity, including PI3 kinase activity, are described herein.
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Paragraph 0771; 0839
(2013/10/22)
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- Discovery of (+)-N-(3-aminopropyl)-N-[1-(5-benzyl-3-methyl-4-oxo-[1,2] thiazolo[5,4- d ]pyrimidin-6-yl)-2-methylpropyl]-4-methylbenzamide (AZD4877), a kinesin spindle protein inhibitor and potential anticancer agent
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Structure-activity relationship analysis identified (+)-N-(3-aminopropyl)- N-[1-(5-benzyl-3-methyl-4-oxo-[1,2]thiazolo[5,4-d]pyrimidin-6-yl) -2-methylpropyl]-4-methylbenzamide (AZD4877), from a series of novel kinesin spindle protein (KSP) inhibitors, as exhibiting both excellent biochemical potency and pharmaceutical properties suitable for clinical development. The selected compound arrested cells in mitosis leading to the formation of the monopolar spindle phenotype characteristic of KSP inhibition and induction of cellular death. A favorable pharmacokinetic profile and notable in vivo efficacy supported the selection of this compound as a clinical candidate for the treatment of cancer.
- Theoclitou, Maria-Elena,Aquila, Brian,Block, Michael H.,Brassil, Patrick J.,Castriotta, Lillian,Code, Erin,Collins, Michael P.,Davies, Audrey M.,Deegan, Tracy,Ezhuthachan, Jayachandran,Filla, Sandra,Freed, Ellen,Hu, Haiqing,Huszar, Dennis,Jayaraman, Muthusamy,Lawson, Deborah,Lewis, Paula M,Nadella, Murali V. P.,Oza, Vibha,Padmanilayam, Maniyan,Pontz, Timothy,Ronco, Lucienne,Russell, Daniel,Whitston, David,Zheng, Xiaolan
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p. 6734 - 6750
(2011/12/04)
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- Selected fused heterocyclics and uses thereof
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This invention relates to novel compounds having the structural formula (I) and to their pharmaceutical compositions and to their methods of use. These novel compounds provide a treatment or prophylaxis of cancer.
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Page/Page column 19
(2008/06/13)
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