- HETEROCYCLYC SULFONAMIDES HAVING EDG-I ANTAGONISTIC ACTIVITY
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The invention relates to chemical compounds of formula (I), (Ia) and (Ib) or pharmaceutically acceptable salts thereof, which possess Edg-1 antagonistic activity and are accordingly useful for their anti-cancer activity and thus in methods of treatment of the human or animal body. The invention also relates to processes for the manufacture of said chemical compounds, to pharmaceutical compositions containing them and to their use in the manufacture of medicaments for use in the production of an anti-cancer effect in a warm-blooded animal, such as man.
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Page/Page column 178
(2008/12/05)
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- Regioselective synthesis of an imidazo[4,5-c]pyridine through selective acylation of 3,4-diaminopyridine: Synthesis of CP-885,316
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CP-885,316 (1), an imidazo[4,5-c]pyridine, 4, was prepared from 3,4-diaminopyridine (9). Two routes were demonstrated using the regioselective introduction of either an acetamide at the 3-position or a tert-butylcarbamate at the 4-position.
- Caron, Stephane,Do, Nga M.,McDermott, Ruth E.,Bahmanyar
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p. 257 - 261
(2012/12/22)
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- (1H-Imidazo[4,5-c]pyridin-2-yl)-1,2,5-oxadiazol-3-ylamine derivatives: A novel class of potent MSK-1-inhibitors
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A novel series of imidazo[4,5-c]pyridines bearing a 1,2,5-oxadiazol-3- ylamine functionality has been developed. These are potent inhibitors of mitogen and stress-activated protein kinase-1.
- Bamford, Mark J.,Alberti, Michael J.,Bailey, Nicholas,Davies, Susannah,Dean, David K.,Gaiba, Alessandra,Garland, Stephen,Harling, John D.,Jung, David K.,Panchal, Terence A.,Parr, Christopher A.,Steadman, Jon G.,Takle, Andrew K.,Townsend, James T.,Wilson, David M.,Witherington, Jason
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p. 3402 - 3406
(2007/10/03)
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- Process for preparing haloalkyl pyrimidines
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The invention is a process for producing haloalkyl pyrimidines as intermediates in the production of benzimidazole and/or pyridylimidazole derivatives having high selectivity and/or high affinity to the benzodiazepine site of GABAA receptors.
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- Substituted ring-fused imidazole derivative: GABAA receptors ligands
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Substituted ring-fused imidazole derivatives that bind to GABAA receptors are provided. Such compounds may be used to modulate ligand binding to GABAA receptors in vivo or in vitro, and are particularly useful in the treatment of a v
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- Benzimidazole and pyridylimidazole derivatives
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This invention relates to benzimidazoles, pyridylimidazoles and related bicyclic heteroaryl compounds, all of which may be described by of Formula I The invention is particularly related to such compounds that bind with high selectivity and high affinity to the benzodiazepine site of GABAA receptors. This invention also relates to pharmaceutical compositions comprising such compounds and to the use of such compounds in treatment of certain central nervous system (CNS) diseases. Novel processes for preparing compounds of Formula I are disclosed. This invention also relates to the use of benzimidazoles, pyridylimidazoles and related bicyclic heteroaryl compounds of Formula I in combination with one or more other CNS agents to potentiate the effects of the other CNS agents. Additionally this invention relates to the use such compounds as probes for the localization of GABAA receptors in tissue sections.
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