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 .omega.-[4-(2-pyridyl)-piperazino]-alkanoylanilide compounds having the structural formula (I): ##STR1## wherein n is 1, 2 or 3, each of R, R.sub.1, R.sub.2 R.sub.3, and R.sub.4 is independently hydrogen, halogen, alkyl, alkoxy, OH, NH.sub.2, CF.sub.3, CN, alkylthio, 1-hydroxyalkyl, alkanoyl, NH.sub.2 CO, NH.sub.2 SO.sub.2, alkoxycarbonyl, alkylsulfonyl, benzyloxy, alkanoylamino, NH.sub.2 CONH, 3-phenylureido, 3-alkylureido or alkoxyoxalylamino, R.sub.5 is hydrogen or alkyl, and R.sub.6 is hydrogen or alkoxy, and the pharmaceutically acceptable salts thereof, are effective antianaphylactics, antibronchospastics, antihistaminics, sedatives, analgesics, antiserotonics and blood-pressure-lowering agents.

Abstract: The novel anthranilic acid derivatives having the structural formula (I): ##STR1## wherein n is 0, 1 or 2, one of R.sub.1 and R.sub.2 is chloro or trifluoromethyl and the other is hydrogen, and R is 2-oxo-3-oxolanyl or 2-oxo-3-oxazolidinyl, are effective analgesics 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: Novel cystine derivatives having the structural formula (I): ##STR1## wherein R is benzyloxycarbonyl or tosyl, and the pharmaceutically acceptable acid addition salts thereof, are effective expectorants and antitussives, and are also effective for the liquescence of respiratory tract fluids.

Abstract: Imidazole derivatives of the formula I and pharmaceutically acceptable acid addition salts thereof are provided: ##STR1## In the formula, R.sub.4 1- or 2-naphthyl, optionally substituted with Cl, Br, or I; 1,2,3,4-tetrahydro-6-naphthyl; 3-duryl, optionally 6-substituted by Cl, Br, I, NO.sub.2, CH.sub.3 or benzyl; mesityl, phenyl 2-, 3- or 4-substituted by OH, NH.sub.2, NO.sub.2, CH.sub.3 CONH, phenyl, phenoxy, cyclohexyl, phenylthio, benzylthio, C.sub.1 -C.sub.6 alkyl or C.sub.1 C.sub.6 alkylthio; 4-bibenzylyl; 3,4-dihydroxyphenyl,n=0, 1 or 2 and(a) R=H, alkyl having 1 to 6 carbon atoms or phenyl R.sub.1 =H, alkyl having 1 to 6 carbon atoms or phenyl one of R.sub.2 and R.sub.3 =H the other of R.sub.2 and R.sub.3 =H, OH, benzoyloxy, C.sub.2 -C.sub.7 alkanoyloxy, N-(C.sub.1 -C.sub.6 alkyl)-carbamoyloxy, N,N-[di-(C.sub.1 C.sub.6)alkyl]-carbamoyloxy, but if R.sub.2 =R.sub.3 =H then R=R.sub.1 =H, or(b) R=H, C.sub.1 -C.sub.6 alkyl, phenyl R.sub.1 =H, C.sub.1 -C.sub.6 alkyl, phenyl R.sub.2 +R.sub.

Abstract: There are provided 2,4-dichloro-4'-phenyl-.alpha.-(N-imidazolyl-methyl)-dibenzyl ether, 2,4-dichloro-4'-phenylthio-.alpha.-(N-imidazolyl-methyl)-dibenzyl ether and pharmaceutically acceptable acid addition salts thereof. These compounds show activity against some fungi, yeasts and gram positive aerobic and anaerobic bacteria. The new compounds can be prepared by condensing 1-(2',4'-dichlorophenyl)-2-(N-imidazolyl)-ethanol with 4-chloromethyl-biphenyl, 4-bromomethyl-biphenyl, 1-phenylthio-4-chloromethyl-benzene or 1-phenylthio-4-bromomethyl-benzene in a solvent, most preferably dimethylsulphoxide.

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.