- OGA INHIBITOR COMPOUNDS
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The present invention relates to O-GlcNAc hydrolase (OGA) inhibitors. The invention is also directed to pharmaceutical compositions comprising such compounds, to processes for preparing such compounds and compositions, and to the use of such compounds and compositions for the prevention and treatment of disorders in which inhibition of OGA is beneficial, such as tauopathies, in particular Alzheimer's disease or progressive supranuclear palsy; and neurodegenerative diseases accompanied by a tau pathology, in particular amyotrophic lateral sclerosis or frontotemporal lobe dementia caused by C9ORF72 mutations; or alpha synucleinopathies, in particular Parkinson's disease, dementia due to Parkinson's (or neurocognitive disorder due to Parkinson's disease), dementia with Lewy bodies, multiple system atrophy, or alpha synucleinopathy caused by Gaucher's disease.
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Page/Page column 61; 66
(2021/06/26)
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- Discovery of β2 adrenergic receptor ligands using biosensor fragment screening of tagged wild-type receptor
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G-protein coupled receptors (GPCRs) are the primary target class of currently marketed drugs, accounting for about a quarter of all drug targets of approved medicines. However, almost all the screening efforts for novel ligand discovery rely exclusively on cellular systems overexpressing the receptors. An alternative ligand discovery strategy is a fragment-based drug discovery, where low molecular weight compounds, known as fragments, are screened as initial starting points for optimization. However, the screening of fragment libraries usually employs biophysical screening methods, and as such, it has not been routinely applied to membrane proteins. We present here a surface plasmon resonance biosensor approach that enables, cell-free, label-free, fragment screening that directly measures fragment interactions with wild-type GPCRs. We exemplify the method by the discovery of novel, selective, high affinity antagonists of human β2 adrenoceptor.
- Aristotelous, Tonia,Ahn, Seungkirl,Shukla, Arun K.,Gawron, Sylwia,Sassano, Maria F.,Kahsai, Alem W.,Wingler, Laura M.,Zhu, Xiao,Tripathi-Shukla, Prachi,Huang, Xi-Ping,Riley, Jennifer,Besnard, Jeremy,Read, Kevin D.,Roth, Bryan L.,Gilbert, Ian H.,Hopkins, Andrew L.,Lefkowitz, Robert J.,Navratilova, Iva
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supporting information
p. 1005 - 1010
(2013/10/22)
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- N-HETEROARYL COMPOUNDS WITH CYCLIC BRIDGING UNIT FOR THE TREATMENT OF PARASITIC DISEASES
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This invention relates to certain N-heteroaryl compounds that are generally useful as medicaments, more specifically as medicaments for animals. The medicament can preferably be used for the treatment of helminth infections and the treatment of parasitosis, such as caused by helminth infections. This invention also relates to uses of the compounds to make medicaments and treatments comprising the administration of the compounds to animals in need of the treatments. This invention also relates to the preparation of the N-heteroaryl compounds. Moreover this invention relates to pharmaceutical compositions and kits comprising the compounds.
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Page/Page column 83
(2012/04/17)
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- INHIBITORS OF FUNGAL INVASION
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This invention relates to various anti-fungall agents including agents that are inhibitors of fungal invasion.
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Drawing sheet 33
(2010/02/09)
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