Abstract: Solid dosage form for the controlled release of flavoxate hydrochloride is described. The dosage form includes a matrix allowing gradual release of the flavoxate hydrochloride contained within it, a suitable binder which limits the dimensions of the finished solid dosage form, and an acidifying agent which ensures stability of the flavoxate hydrochloride with time and improves its release profile by making it independent of pH.

Abstract: Novel antihypertensive and coronary dilating asymmetric diesters of 1,4-dihydro-2,6-dimethylpyridine-3,5-dicarboxylic acid (or the stereoisomers or pharmaceutically acceptable acid addition salts thereof) have the general formula (I): ##STR1## wherein Ph is phenyl, Ar is 2-nitrophenyl, 3-nitrophenyl, 2,3-dichlorophenyl or benzofurazan-4-yl, A is a straight or branched chain alkylene radical having from 2 to 6 carbon atoms, R is a straight or branched chain alkyl radical having from 1 to 6 carbon atoms, optionally mono-substituted by an alkoxy substituent having from 1 to 6 carbon atoms, R.sub.1 is hydrogen, hydroxy or an alkyl radical having from 1 to 4 carbon atoms, and R.sub.2 is hydrogen or methyl. The subject diesters are facilely prepared from the aldehydes ArCHO and esters of acetoacetic and 3-aminocrotonic acids.

Abstract: N-piperazinylalkanoylanilides of the formula ##STR1## wherein n is 0, 1 or 2, each of R and R.sub.1 is H or alkyl, and each of R.sub.2, R.sub.3 and R.sub.4 is H, halogen, alkyl, hydroxyalkyl, alkoxy, aralkoxy, alkylthio, aralkylthio, alkylsulphonyl, alkylsulphenyl, NO.sub.2, NH.sub.2, alkylamino, acylamino, ureido, alkylureido, alkylsulphonylamino, CF.sub.3, acyl, CN, COOH, alkoxycarbonyl, NH.sub.2 CO, SO.sub.3 H, guanidinosulphonyl, carbamoyloxy, OH, acyloxy, alkylsulphonyloxy, alkylenedioxy or SO.sub.2 NR.sub.5 R.sub.6 wherein each of R.sub.5 and R.sub.6 is H, alkyl, aryl or acyl and their pharmaceutically acceptable acid addition salts, are antihypertensive agents.

Abstract: The novel flavonyl-1,4-dihydropyridines having the general formula (I): ##STR1## are therapeutically effective calcium antagonists and smooth muscle relaxant.

Abstract: Novel antihypertensive and coronary dilating asymmetric diesters of 1,4-dihydro-2,6-dimethylpyridine-3,5-dicarboxylic acid (or the stereoisomers or pharmaceutically acceptable acid addition salts thereof) have the general formula (I): ##STR1## wherein Ph is phenyl, Ar is 2-nitrophenyl, 3-nitrophenyl, 2,3-dichlorophenyl or benzofurazan-4-yl, A is a straight or branched chain alkylene radical having from 2 to 6 carbon atoms, R is a straight or branched chain alkyl radical having from 1 to 6 carbon atoms, optionally mono-substituted by an alkoxy substituent having from 1 to 6 carbon atoms, R.sub.1 is hydrogen, hydroxy or an alkyl radical having from 1 to 4 carbon atoms, and R.sub.2 is hydrogen or methyl. The subject diesters are facilely prepared from the aldehydes ArCHO and esters of acetoacetic and 3-aminocrotonic acids.

Abstract: Novel antihypertensive and coronary dilating asymmetric diesters of 1,4-dihydro-2,6-dimethyl-pyridine-3,5-dicarboxylic acid (or the stereoisomers or pharmaceutically acceptable acid addition salts thereof) have the general formula (I): ##STR1## wherein Ph is phenyl, Ar is 2-nitrophenyl, 3-nitrophenyl, 2,3-dichlorophenyl or benzofurazan-4-yl, A is a straight or branched chain alkylene radical having from 2 to 6 carbon atoms, R is a straight or branched chain alkyl radical having from 1 to 6 carbon atoms, optionally mono-substituted by an alkoxy substituent having from 1 to 6 carbon atoms, R.sub.1 is hydrogen, hydroxy or an alkyl radical having from 1 to 4 carbon atoms, and R.sub.2 is hydrogen or methyl. The subject diesters are facilely prepared from the aldehydes ArCHO and esters of acetoacetic and 3-aminocrotonic acids.

Abstract: Novel piperazine derivatives having the general formula: ##STR1## wherein R is hydrogen or lower alkyl, A is straight or branched chain lower alkyl, and R.sub.1 and R.sub.2 are each hydrogen, amino, alkylamino, dialkylamino, mono- or di(hydroxyalkyl)amino, morpholino, pyrrolidino, piperidino, N-alkylpiperazino, 1,3-dithiolan-2-ylidenamino, or N-alkylureido, with the proviso that at least one of R.sub.1 and R.sub.2 is other than hydrogen, or the isomeric mixtures, individual enantiomers or pharmaceutically acceptable acid addition salts thereof, are therapeutically useful antianaphylactic and antibronchospastic agents.

Abstract: Novel 3-methylflavone-8-carboxylates having the structural formula (I): ##STR1## wherein Z is N-methylpiperidinyl, tropinyl or quinuclidinyl, or a group having the structural formula (II): ##STR2## in which n is 0 or 1, R is hydrogen or alkyl having from 1 to 4 carbon atoms, or phenyl, R.sub.1 is hydrogen or alkyl having from 1 to 4 carbon atoms, R.sub.2 is hydrogen or hydroxy, and further wherein R, R.sub.1 and R.sub.2 may together form, with the carbon atoms from which they depend, a cycloalkyl ring having from 4 to 6 carbon atoms, and R.sub.3 is hydrogen or alkyl having from 1 to 4 carbon atoms, with the proviso that R, R.sub.1, R.sub.2 and R.sub.3 cannot at the same time all be hydrogen, and the pharmaceutically acceptable salts thereof, are effective smooth muscle relaxants, calcium blockers, anaesthetics and anti-inflammatories.

Abstract: The N-substituted-4-(optionally substituted)-2-, 3- or 4-piperidyl N-(7- or 8-substituted-4-quinolyl)-anthraniloyloxyalkanoates having the structural formula (I): ##STR1## in which R is a straight or branched chain alkyl radical having from 1 to 4 carbon atoms; an alkenyl or alkynyl radical having from 2 to 6 carbon atoms; a benzyl, phenethyl, 4-nitrophenethyl or 4-aminophenethyl radical; or a phenacyl, benzoylethyl, .beta.-hydroxyphenethyl or .alpha.-hydroxyphenylpropyl radical, optionally substituted on the phenyl ring by one or more halogen atom, trifluoromethyl, nitro or amino substituents, or an alkyl substituent having from 1 to 4 carbon atoms or an alkoxy substituent having from 1 to 4 carbon atoms; R.sub.1 is a hydrogen atom or a phenyl radical; each of R.sub.2 and R.sub.3 is independently a hydrogen atom or an alkyl radical having from 1 to 4 carbon atoms; one of R.sub.4 and R.sub.5 is a chlorine atom or a trifluoromethyl radical and the other of R.sub.4 and R.sub.

Abstract: Therapeutically active 2- and 3-substituted benzoic acid derivatives having the general formula ##STR1## wherein X is OH, NH.sub.2 or an anilino group having the phenyl ring unsubstituted or substituted by chlorine or by a 4-ethoxy group; or ##STR2## wherein X is NH.sub.2 or an anilino group having the phenyl ring unsubstituted or substituted by chlorine or by a 4-ethoxy group; pharmacologically acceptable mineral or organic acid addition salts including quaternary ammonium salts of those compounds having a basic nitrogen atom and alkaline or alkaline earth metal salts of those compounds wherein X is OH.Compounds of the formula wherein X is amino or anilino are prepared by reacting 3-propionylsalicyclic acid or a functional derivative thereof with ammonia or an amine in an anhydrous solvent.

Abstract: Novel derivatives of 3H-1,5-benzodiazepine and of their salts of addition with acids, including their quaternary ammonium salts, having the general formula: ##EQU1## are provided. Such compounds are effective therapeutically against a large spectrum of gram positive bacteria and APR8 influenza virus. The invention also provides a novel method of preparing compounds having the formula: ##EQU2## wherein R and R' are the same as above, by reacting orthophenylenediamine with a benzoyldithioacetic acid having the formula: ##EQU3## wherein R and R' are as defined above.