Basic esters exhibiting an antagonistic activity to calcium, process for the preparation thereof and pharmaceutical compositions therefrom

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United States of America Patent

PATENT NO 4894460
SERIAL NO

06563008

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Abstract

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Basic esters of 1,4-dihydropyridine-3,5-dicarboxylic acid of formula (I) ##STR1## are described, in which R.sup.1 is a linear or branched alkyl radical containing 1-5 carbon atoms which is unsubstituted or substituted by an alkoxy group; R.sup.2 is phenyl or a nitro phenyl radical; R.sup.3 is phenyl, phenyl substituted by one to three radicals selected from (C.sub.1-4)alkyl, (C.sub.1-4)alkoxy, fluoro, chloro, bromo, nitro, cyano, COOR in which R is alkyl of 1 to 4, trifluo carbon atoms, romethyl, hydroxy, amino, mono- or di-alkylamino, mono- or di-acylamino, mercapto, S(O).sub.n -alkyl with n=0, 1 or 2, (C.sub.1-5)acyl, carbamoyl, ureido or R.sup.3 is a 5 or 6 membered heteroaryl monocyclic radical which contains one or more heteroatoms which are N, O or S such as unsubstituted pyridyl, pyrazinyl, pyrimidyl, furyl, imidazolyl, thienyl, thiazolyl, 1,2,3-triazolyl, 1,2,4-triazolyl or mono-, di- or tri-substituted with alkyl, alkoxy, halogen or trifluoromethyl; X is a linear or branched alkylen radical containing between 2 and 5 carbon atoms which is unsubstituted or substituted by an alkoxy group and their racemates, enantiomers and diastereoisomers and addition salts thereof with a pharmaceutically acceptable acid. The novel compounds exhibit calcium antagonistic activity.

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PIERREL S P A 88 DEPRETIS STREET NAPOLI A CORP OF ITALYNot Provided

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Inventor(s)

Inventor Name Address # of filed Patents Total Citations
Casagrande, Cesare Arese, IT 37 232
de, Marchi Franco Milan, IT 3 63
Nicola, Massimo Pavia, IT 11 83
Tricerri, Silvia Z Carimate, IT 2 4

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