- Imidazole and imidazoline derivatives and uses thereof
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This invention is directed to novel imidazole and imidazoline derivatives which are selective agonists for cloned human α2 adrenergic receptors. This invention is also related to the use of these compounds for the treatment of any disease where
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- Synthesis and structure-activity relationships of fused imidazopyridines: A new series of benzodiazepine receptor ligands
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2-Arylimidazo[4,5-c]quinolines and analogous fused imidazopyridines were synthesized and evaluated as benzodiazepine receptor ligands. Affinity to the receptors was greatly affected by the bulkiness of the aryl group at the 2- position, compared to the pyrazoloquinolines such as CGS-9896. Derivatives with an isoxazole moiety at the 2-position showed high binding affinity and in vivo activity. In the imidazo[4,5-c]quinoline series, substitution at the 6-position decreased or abolished activity. Most derivatives with an unsubstituted isoxazolyl group showed antagonist or inverse agonist activity except for the 7-halo analogues, which exhibited agonist activity. On the other hand, 5-methylisoxazol-3-yl or 3-methylisoxazol-5-yl derivatives generally exhibited agonist activity. A similar substitution effect on the isoxazole moiety was observed in the imidazopyridines fused with a nonaromatic ring. From the detailed pharmacological evaluation, S-8510, 2- (3-isoxazolyl)-3,6,7,9-tetrahydroimidazo[4,5-d]pyrano[4,3-b]pyridine monophosphate, possessing weak inverse agonist activity was selected as a therapeutic candidate for the treatment of some symptoms of senile dementia.
- Takada, Susumu,Sasatani, Takashi,Chomei, Nobuo,Adachi, Makoto,Fujishita, Toshio,Eigyo, Masami,Murata, Shunji,Kawasaki, Kazuo,Matsushita, Akira
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p. 2844 - 2851
(2007/10/03)
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- Condensed imidazopyridine derivatives
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A compound of the formula: STR1 wherein R is an optionally substituted aryl group or an optionally substituted aromatic heterocycle group; A ring is a 5 to 9 membered alicyclic group, in which one or more of carbon atoms constituting said A ring may be replaced by O, or S and said A ring may have alkyl as a substituent, or a pharmaceutically acceptable salt thereof.
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