138449-64-6Relevant academic research and scientific papers
AZACYCLIC OR AZABICYCLIC COMPOUNDS, THEIR PREPARATION AND USE
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, (2008/06/13)
The present invention relates to therapeutically active azacyclic or azabicyclic compounds of formula (I), a method of preparing the same and to pharmaceutical compositions comprising the compounds. The novel compounds are useful as stimulants of the cognitive function of the forebrain and hippocampus of mammals and especially in the treatment of Alzheimer's disease. (A), (B) or (C), wherein R and R1 are as defined in claim 1.
Functionally Selective M1 Muscarinic Agonists. 3. Side Chains and Azacycles Contributing to Functional Muscarinic Selectivity among Pyrazinylazacycles
Ward, John S.,Merritt, Leander,Calligaro, David O.,Bymaster, Frank P.,Shannon, Harlan E.,et al.
, p. 3469 - 3481 (2007/10/03)
In an attempt to improve upon the M1 agonist activity of the selective M1 agonist xanomeline and related compounds, the M1 muscarinic efficacies and potencies of 3- and 6-substituted pyrazinylazacycles were varied by changing both the 3- and 6-substituents as well as the azacycle.Significant improvements in efficacy and potency over the previously prepared tetrahydropyridine 19 were obtained with the quinuclidine 5i.The M1 activity of 5i showed some enantioselectivity with (S)-5i being ca. 4-fold more potent than (R)-5i.Like 19 and xanomeline, 5i was a functionally selective M1 agonist that showed greater functional selectivity of than widely studied pyrazinylquinuclidine 5n (L-689,660).The improved functional selectivity of 5i over 5n could be attributed to the additional binding interactions between the hexyloxy side chain of 5i and the M1 receptor that are not available to 5n.Although 5i may show M1 functional selectivity comparable to xanomelline, 5i is less efficacious and potent M1 agonist than xanomeline.
Heterocyclic compounds their preparation and use
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, (2008/06/13)
The present invention relates to therapeutically active azacyclic or azabicyclic compounds, a method of preparing the same and to pharmaceutical compositions comprising the compounds. The novel compounds are useful as stimulants of the cognitive function of the forebrain and hippocampus of mammals and especially in the treatment of Alzheimer's disease.
