- Design of A Metabolically Stable Tritium-Tracer of the PI3Kδ-Inhibitor CDZ173 (Leniolisib) as a Tool to Study Liver Metabolites
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In this disclosure, we summarize the preliminary metabolic profiling of the PI3Kδ inhibitor CDZ173 (leniolisib, 1a) obtained from incubations of the unlabeled compound and the synthesis of its metabolically stable tritium isotopologue 1b used for metaboli
- Bauer, Carsten,Luu, Tong,Eggimann, Fabian,Bross, Patrick,Gertsch, Werner,Hu, Cheng,Ramstein, Philippe,Bourgailh, Julien,Gl?nzel, Albrecht,Dix, Ina,Guenat, Christian,Soldermann, Nicolas,Litherland, Karine,Desrayaud, Sandrine,Hengy, Jean-Claude,Pearson, David,Blanz, Joachim,Burkhart, Christoph
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- TETRAHYDROPYRIDO[4,3-D]PYRIMIDINE INHIBITORS OF ATR KINASE
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The present invention relates to tetrahydropyrido[4,3-d]pyrimidine based compounds and methods which may be useful as inhibitors of ATR kinase for the treatment or prevention of cancer.
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Paragraph 0337; 0339
(2018/12/13)
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- TASK CHANNEL ANTAGONISTS
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This invention relates to TASK-1 and/or TASK-3 antagonists and/or their pharmaceutically acceptable salts, compositions and methods for treating and preventing disorders which are caused by activation or by an activated TASK-1 and/or TASK-3, and disorders
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- TASK CHANNEL ANTAGONISTS
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This invention relates to TASK-1 and/or TASK-3 antagonists and/or their pharmaceutically acceptable salts, compositions and methods for treating and preventing disorders which are caused by activation or by an activated TASK-1 and/or TASK-3, and disorders
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- PYRID-2-YL FUSED HETEROCYCLIC COMPOUNDS, AND COMPOSITIONS AND USES THEREOF
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Fused heterocyclic compounds are provided according to formula 1a or 1b: where R1, R2, and R3 are as defined herein. Provided compounds and pharmaceutical compositions thereof are useful for the prevention and treatment of a variety of conditions in mammals including humans, including by way of non-limiting example, pain, inflammation, cognitive disorders, anxiety, depression, and others.
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- 2-Cyanophenyl fused heterocyclic compounds, and compositions and uses thereof
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Fused heterocyclic compounds are provided according to formula 1: where R1, R2, R3, and m are as defined herein. Provided compounds and pharmaceutical compositions thereof are useful for the prevention and treatment of a variety of conditions in mammals including humans, including by way of non-limiting example, pain, inflammation, cognitive disorders, anxiety, depression, and others.
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Page/Page column 23
(2008/12/08)
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- Development and experimental validation of a docking strategy for the generation of kinase-targeted libraries
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A high-throughput docking strategy for the filtering of in silico compounds and the generation of kinase-targeted libraries is described. Systematic docking and scoring in three kinase crystal 3D structures of 123 structurally diverse kinase ligands led to the determination of six thresholds for each kinase. These thresholds were used as filters for the virtual screening of two collections of compounds: a collection of more than 2500 drugs and drug-like compounds (negative control) and a kinase-targeted library of 1440 compounds. This strategy was then experimentally validated by testing 60 compounds from the kinase-targeted library on 41 kinases from five different families. The 60 compounds were split into those passing all the thresholds and the others (30 compounds in each group). The overall hit enrichment was 6.70-fold higher in the first group, validating our approach for the generation of kinase-targeted libraries and the identification of scaffolds with high kinase inhibitory potential.
- Gozalbes, Rafael,Simon, Laurence,Froloff, Nicolas,Sartori, Eric,Monteils, Claude,Baudelle, Romuald
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body text
p. 3124 - 3132
(2009/06/06)
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- Fused heterocyclic compounds, and compositions and uses thereof
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Fused heterocyclic compounds are disclosed that have formula 1: where A, B, L, N, R1, R3, R4′, Y and Z are as defined herein. The compounds and pharmaceutical compositions thereof are useful for the prevention and treatment of a variety of conditions in mammals including humans, including by way of non-limiting example, pain, inflammation, cognitive disorders, anxiety, depression, and others.
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Page/Page column 23; 28
(2008/06/13)
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