3-Aminocarbonyl-1,4-dihydropyridine-5-carboxylic acid compounds, process for preparation and use thereof, and pharmaceutical composition containing the same.

摘要

Novel 3-aminocarbonyl-1,4-dihydropyridine-5-­carboxylic acid compounds of the formula:
<Chemistry id="chema01" num="0001"><Image id="ia01" he="42" wi="90" file="IMGA0001.TIF" imgContent="chem" imgFormat="TIFF" /></Chemistry> wherein R¹ is H, C<Sub>1-5</Sub> alkyl, C<Sub>2-5</Sub> alkenyl, C<Sub>3-5</Sub> alkynyl, C<Sub>3-­8</Sub> cycloalkyl, R² is C<Sub>1-10</Sub> alkyl, and the NO₂ group is substituted at ortho- or meta-position, provided that when the NO₂ group is substituted at ortho-position and R² is methyl, R¹ is C<Sub>3-5</Sub> alkyl, C<Sub>2-5</Sub> alkenyl, C<Sub>3-5</Sub> alkynyl, or C<Sub>3-­8</Sub> cycloalkyl, and when the NO₂ group is substituted at meta-­position and R¹ is H, R² is C<Sub>3-10</Sub> alkyl, which have excellent hypotensive, vasodilating activities and in pharma­ceutical compositions are useful for the prophylaxis and treatment of hypertension, ischemic heart diseases and cerebral and peripheral circulation diseases. Also process for preparing these compounds and their use are disclosed.