- BENZIMIDAZOLE DERIVATIVES AS RLK and ITK INHIBITORS
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The present disclosure is directed to certain inhibitors of RLK and ITK of formula (I), pharmaceutical compositions comprising such compounds, and method of treating diseases mediated by inhibition of RLK and ITK.
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Page/Page column 77
(2015/09/28)
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- BENZIMIDAZOLE DERIVATIVES AS ITK INHIBITORS
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The present disclosure is directed to certain inhibitors of kinases such as ITK, BLK, BMX, BTK, JAK3, TEC, TXK, HER2 (ERBB2), or HER4 (ERBB4), in particular ITK, pharmaceutical compositions comprising such compounds, and method of treating diseases mediated by such kinases.
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Page/Page column 93; 94
(2014/03/25)
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- HETEROCYCLIC COMPOUNDS AND METHODS OF USE
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Formula I compounds, including stereoisomers, geometric isomers, tautomers, metabolites and pharmaceutically acceptable salts thereof, are useful for inhibiting the delta isoform of PI3K, and for treating disorders mediated by lipid kinases such as inflammation, immunological disorders, and cancer. Methods of using compounds of Formula I for in vitro, in situ, and in vivo diagnosis, prevention or treatment of such disorders in mammalian cells, or associated pathological conditions, are disclosed.
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Page/Page column 123
(2012/08/27)
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- Identification of potent, noncovalent fatty acid amide hydrolase (FAAH) inhibitors
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Starting from a series of ureas that were determined to be mechanism-based inhibitors of FAAH, several spirocyclic ureas and lactams were designed and synthesized. These efforts identified a series of novel, noncovalent FAAH inhibitors with in vitro potency comparable to known covalent FAAH inhibitors. The mechanism of action for these compounds was determined through a combination of SAR and co-crystallography with rat FAAH.
- Gustin, Darin J.,Ma, Zhihua,Min, Xiaoshan,Li, Yihong,Hedberg, Christine,Guimaraes, Cris,Porter, Amy C.,Lindstrom, Michelle,Lester-Zeiner, Dianna,Xu, Guifen,Carlson, Timothy J.,Xiao, Shouhua,Meleza, Cesar,Connors, Richard,Wang, Zhulun,Kayser, Frank
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p. 2492 - 2496
(2011/05/15)
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- Compounds with antiparasitic activity, applications thereof to the treatment of infectious diseases caused by apicomplexans
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The Invention relates to compounds having an antiparasitic activity, and to their use as a drug, in particular as a drug for the prevention and/or treatment of parasitic diseases caused by apicomplexans. The invention also relates to pharmaceutical compositions containing those compounds.
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Page/Page column 26
(2009/01/20)
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- 3-substituted piperidines comprising urea functionality, and methods of use thereof
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One aspect of the present invention relates to novel heterocyclic compounds comprising urea functionality. A second aspect of the present invention relates to the use of the novel heterocyclic compounds comprising urea functionality as ligands for various cellular receptors, including opioid receptors, other G-protein-coupled receptors and ion channels. An additional aspect of the present invention relates to the use of the novel heterocyclic compounds comprising urea functionality as analgesics.
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