- COMPOUNDS USEFUL AS INHIBITORS OF CHOLINE KINASE
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The present invention relates to compounds useful as inhibitors of choline kinase. The invention also provides pharmaceutically acceptable compositions comprising said compounds and methods of using the compositions in the treatment of various disease, conditions, or disorders. The invention also provides processes for preparing compounds of the inventions.
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Paragraph 00159
(2013/04/10)
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- Synthesis and Muscarinic Activities of Quinuclidin-3-yltriazole and -tetrazole Derivatives
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The synthesis of 15 methyl or unsubstituted 1,2,3-triazoles, 1,2,4-triazoles, and tetrazoles additionally substituted with a 1-azabicyclooctan-3-yl group is described.The potency and efficacy of these compounds as muscarinic ligands were determined in radioligand binding assays using oxotremorine and quinuclidinyl benzilate.Potency and efficacy were found in compounds in which the azole moiety was attached to the azabicyclic ring either through a carbon atom or a nitrogen atom.Electrostatic potential maps of both the C-linked and the novel N-linked series of compounds were calculated.A relationship between position and depth of the electrostatic minima relative to the azabicyclic ring and the potency and efficacy of the compounds was determined.
- Wadsworth, Harry J.,Jenkins, Sarah M.,Orlek, Barry S.,Cassidy, Frederick,Clark, Michael S. G.,et al.
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p. 1280 - 1290
(2007/10/02)
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- Novel Quinuclidine-Based Ligands for the Muscarinic Cholinergic Receptor
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Recent clinical studies on Alzheimer's patients have implied that only agents displaying high efficacy at the cortical muscarinic receptor have yielded encouraging results.This paper describes the design, synthesis, and biochemical characterization of nov
- Saunders, John,Cassidy, Mark,Freedman, Stephen B.,Harley, Elizabeth A.,Iversen, Leslie L.,et al.
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p. 1128 - 1138
(2007/10/02)
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