Short acting phenylalkylamine calcium channel blockers and uses thereof
Inventors
Maguire, Martin P. • Rioux, Elise • Leighton, Harry J.
Assignees
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Publication Number
US-10010523-B2
Publication Date
2018-07-03
Expiration Date
Abstract
The present invention relates to the use of a pharmaceutically effective amount of an short-acting calcium channel blocking compound to treat ischemic heart conditions, cardiac arrhythmias, hypertensive crisis in an emergency room setting, hypertension before, during, or after surgery, no-reflow phenomenon following reperfusion, and diseases associated with decreased skeletal muscle blood flow. The invention also relates to pharmaceutical compositions formulated for use in such methods and to kits for such methods.
Core Innovation
The disclosure relates to chemical compounds defined by a formula, including pharmaceutically acceptable addition salts and enantiomers thereof. The description presents specific chemical structures and alternative nomenclature for exemplified compounds included in the invention, including Table 1 compounds, Table 2 amine/general structure B examples, and Table 3 compounds of Formula 1.
The document also describes a set of oxalate salt forms of a compound, where the salt variants are labeled as 3s- through 3aq-oxalate. Each salt variant is presented with a chemical structure for that oxalate salt form, and the content focuses on identifying and showing different oxalate salt variants within the labeled set.
The disclosure further addresses calcium channel binding inhibition in an assay context and links the compound set to calcium channel inhibitory potency measured as Ki in whole brain membranes. The presentation includes compound members identified using a numbering scheme, with entries such as 3a-oxalate, 3b-oxalate, 3c-oxalate, verapamil-oxalate, verapamil-HCl, D-600, and desmethoxyverapamil (D-888).
Claims Coverage
The provided independent claim is directed to a compound defined by a chemical formula, including pharmaceutically acceptable addition salts and enantiomers. The claim coverage is centered on the formula-defined chemical entity, with no additional independent claim refinements provided in the input items.
Formula-defined compound with pharmaceutically acceptable addition salts and enantiomers
A compound having the formula, or a pharmaceutically acceptable addition salt, or enantiomer thereof.
The independent claim scope covers a formula-defined compound, together with pharmaceutically acceptable addition salts and enantiomers. The provided content supports specific oxalate salt embodiments and related compound examples within that compositional scope.
Stated Advantages
Not explicitly described in patent.
Documented Applications
Not explicitly described in patent.
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