- COMPOUNDS WITH COMBINED CALCIUM CHANNEL BLOCKER AND β-ADRENERGIC ANTAGONIST OR PARTIAL AGONIST ACTIVITIES FOR TREATMENT OF HEART DISEASE
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The present invention provides compounds possessing inhibitory activity against β-adrenergic receptors and L-type calcium channels. The present invention further provides pharmaceutical compositions comprising such compounds, methods of preparing such compounds, and methods of using such compounds for regulating calcium homeostasis, for treating a disease, disorder or condition in which disregulation of calcium homeostasis is implicated, and for treating hypertension, cardiovascular disease, congestive heart failure, myocardial ischemia, cardiomyopathies, stroke or epilepsy.
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Page/Page column 45
(2008/06/13)
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- COMPOUNDS WITH MIXED PDE-INHIBITORY AND β-ADRENERGIC ANTAGONIST OR PARTIAL AGONIST ACTIVITY FOR TREATMENT OF HEART FAILURE
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This invention provides compounds that possess inhibitory activity against β--adrenergic receptors and phosphodiesterase PDE, including phosphodiesterase 3 (PDE3 ). This invention further provides pharmaceutical compositions comprising such -compounds; methods of using such compounds for treating cardiovascular disease, stroke, epilepsy, ophthalmic disorder or migraine; and methods of preparing pharmaceutical compositions and compounds that possess inhibitory activity against ?-adrenergic receptors and PDE.
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- Multistep solution-phase parallel synthesis of spiperone analogues
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A flexible, multistep parallel synthesis of spiperone analogues is described. A library of 4-substituted piperidines, assembled utilizing reductive amination and acylation protocols, was alkylated either homogeneously or heterogeneously, exploiting a product release only concept, to afford an oxa-series of spiperone analogues. Screening of the products at 5-HT2 and D2 receptors revealed 5-HT(2A) antagonists with improved selectivity compared to spiperone and AMI-193. (C) 2000 Published by Elsevier Science Ltd.
- Hansen, Henrik C.,Olsson, Roger,Croston, Glenn,Andersson, Carl-Magnus
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p. 2435 - 2439
(2007/10/03)
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