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Last Updated: March 19, 2026

Claims for Patent: 9,227,918


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Summary for Patent: 9,227,918
Title:Short acting phenylalkylamine calcium channel blockers and uses thereof
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.
Inventor(s):Martin P. Maguire, Elise Rioux, Harry J. Leighton
Assignee: Milestone Pharmaceuticals Inc
Application Number:US14/305,626
Patent Claims: 1. A short-acting pharmaceutical composition comprising a compound having the formula: or a pharmaceutically acceptable addition salt thereof, or any enantiomer or diastereomer thereof, wherein each a, b, c, d, e, and f is, independently, —CH2—, —O—, —S—, or a single bond; each R11, R12, R13, R14, R15, R16, and R17 is, independently: H, lower alkyl, lower alkyl substituted with —CO2(lower alkyl), lower alkyl substituted with —CO2(lower alkoxyalkyl), lower alkyl substituted with fluorine or chlorine, lower alkoxyalkyl, lower alkoxyalkyl substituted with —CO2(lower alkyl), lower alkoxyalkyl substituted with —CO2(lower alkoxyalkyl), lower alkoxyalkyl substituted with fluorine or chlorine, or CO2R10; each R10 is, independently, lower alkyl or lower alkoxyalkyl; R18 is H or CN, or CO2R10; and R19 is H, g is a single bond, and R20 is H, wherein at least one of R11, R12, R13, R14, R15, R16, and R17, is CO2R10, lower alkyl substituted by —CO2(lower alkyl), lower alkyl substituted with —CO2(lower alkoxyalkyl), lower alkoxyalkyl substituted with —CO2(lower alkyl), or lower alkoxyalkyl substituted with —CO2(lower alkoxyalkyl).

2. The pharmaceutical composition of claim 1, wherein said compound, before being inactivated metabolically, produces the desired effect from 1 minute to 30 minutes.

3. A pharmaceutical composition comprising a compound selected from the group consisting of:

4. The pharmaceutical composition of claim 3, wherein said compound is selected from the group consisting of:

5. The pharmaceutical composition of claim 3, wherein said compound is

6. The pharmaceutical composition of claim 1, wherein said pharmaceutical composition is formulated for treating a condition selected from the group consisting of: ischemic heart conditions; and cardiac arrhythmia.

7. The pharmaceutical composition of claim 3, wherein said pharmaceutical composition is formulated for treating a condition selected from the group consisting of: ischemic heart conditions; and cardiac arrhythmia.

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