- WDR5-MYC INHIBITORS
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Substituted N-phenyl sulfonamide compounds inhibit WDR5-MYC interactions, and the compounds and their pharmaceutical compositions are useful for treating disorders and conditions in a subject, such as cancer cell proliferation.
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Paragraph 00732-00733
(2021/02/05)
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- C-ABL TYROSINE KINASE INHIBITORY COMPOUND EMBODIMENTS AND METHODS OF MAKING AND USING THE SAME
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Disclosed herein are embodiments of a compound that inhibits c-Abl tyrosine kinase (also referred to herein as "c-Abl"). The compound embodiments described herein are novel c-Abl inhibitors that can bind to c-Abl at an allosteric site and inhibit its activity in various pathways. The compound embodiments also are capable of crossing the blood brain barrier and therefore are useful in inhibiting c-Abl activity as it affects pathways and/or proteins in the brain. The compound embodiments described herein are effective therapeutic agents for treating diseases involving c-Abl, such as cancers, motor neuron diseases, and neurodegenerative diseases. Also disclosed herein are embodiments of methods for making and using the c- Abl inhibitory compound embodiments.
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Page/Page column 95
(2019/10/01)
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- Discovery and Optimization of Salicylic Acid-Derived Sulfonamide Inhibitors of the WD Repeat-Containing Protein 5-MYC Protein-Protein Interaction
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The treatment of tumors driven by overexpression or amplification of MYC oncogenes remains a significant challenge in drug discovery. Here, we present a new strategy toward the inhibition of MYC via the disruption of the protein-protein interaction betwee
- Macdonald, Jonathan D.,Chacón Simon, Selena,Han, Changho,Wang, Feng,Shaw, J. Grace,Howes, Jennifer E.,Sai, Jiqing,Yuh, Joannes P.,Camper, Demarco,Alicie, Bethany M.,Alvarado, Joseph,Nikhar, Sameer,Payne, William,Aho, Erin R.,Bauer, Joshua A.,Zhao, Bin,Phan, Jason,Thomas, Lance R.,Rossanese, Olivia W.,Tansey, William P.,Waterson, Alex G.,Stauffer, Shaun R.,Fesik, Stephen W.
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p. 11232 - 11259
(2019/12/25)
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- BENZO-FUSED HETEROCYCLIC DERIVATIVES USEFUL AS AGONISTS OF GPR120
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The present invention is directed to benzo-fused heterocyclic derivatives, pharmaceutical compositions containing them and their use in the treatment of disorders and conditions modulated by GPR120. More particularly, the compounds of the present invention are agonists of GPR120, useful in the treatment of, such as for example, Type II diabetes mellitus.
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Paragraph 0733
(2014/09/30)
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- ANILINOPYRAZOLE DERIVATIVES USEFUL FOR THE TREATMENT OF DIABETES
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The present invention relates to anilinopyrazole compounds of formula (1) in which R3 represents an aromatic 5- or 6-membered heteroaromatic ring which is optionally fused to phenyl, said heterocycle or fused heterocycle is optionally substituted, X represents a carboxylic acid, ester or amide, or sulfonamide, and the remaining groups are as defined in the text. It also relates to pharmaceutical compositions containing these materials and, and methods for treating diabetes and related disorders using these materials.
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Page/Page column 53
(2010/11/26)
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