Abstract: The synthesis and application of N(1)-n-alkyl-pyrimidinium-salts are described. These surfactants have a very small critical micelle concentration (CMC) in the order of 10.sup.-5 -10.sup.-7 Mol/Liter. These N(1)-n-alkyl-pyrimidinium components have pharmacological activities and can act as antimetabolites.

Abstract: A dihydropyridine.rarw..fwdarw. pyridinium salt type of redox, or chemical, delivery system for the site-specific and/or site-enhanced delivery of a radionuclide to the brain is provided. A chelating agent capable of chelating with a radionuclide and having a primary, secondary or tertiary amino function can be converted to the corresponding analogue in which said function is replaced with a dihydropyridine.rarw. .fwdarw. pyridinium salt redox system and then complexed with a radionuclide to provide a new radiopharmaceutical that, in its lipoidal dihydropyridine form, penetrates the blood-brain barrier ("BBB") and allows increased levels of radionuclide concentration in the brain, particularly since oxidation of the dihydropyridine moiety in vivo to the ionic pyridinium salt retards elimination from the brain while elimination from the general circulation is accelerated.This radionuclide delivery system is well suited for use in scintigraphy and similar radiographic techniques.

Abstract: Compounds are described of the formula ##STR1## wherein R.sub.1 and R.sub.4 independently represent a C.sub.1-4 alkyl group;R.sub.2 and R.sub.3 independently represent a C.sub.1-6 straight or branched alkyl chain or alkoxy group;R.sub.5 represents a straight or branched chain C.sub.1-13 alkyl group or a C.sub.5-8 cycloalkyl group which may be substituted by a C.sub.1-3 alkyl substituent;R.sub.6 represents a halogen atom or a straight or branched C.sub.1-3 alkyl group.R.sub.7 represents a C.sub.1-4 alkyl group [optionally substituted by hydroxy, C.sub.1-3 alkoxy or trifluoromethyl or by a group NR.sub.8 R.sub.9 where NR.sub.8 R.sub.9 forms a saturated 5 to 7 membered ring optionally containing an additional heleroatom which is oxygen]; or R.sub.7 represents a phenylC.sub.1-2 alkyl group in which the portion is optionally substituted by 1 to 3 C.sub.1-3 alkyl or C.sub.1-3 alkoxy groups or halogen atoms.

Abstract: A process for preparing a 2-carbamoylocxyalkyl-1,4-dihydropyridine derivative represented by the general formula: ##STR1## which comprises: (a) reacting a 3-amino-3-carbamoyloxyalkylacrylic acid derivative represented by the general formula: ##STR2## with a benzylidene compound represented by the general formula: ##STR3## (b) reacting the 3-amino-3-carbamoyloxyalkylacrylic acid derivative of the general formula II with an aldehyde compound represented by the general formula: ##STR4## and a .beta.-keto-ester compound represented by the general formula:R.sup.4 --CO--CH.sub.2 --COOR.sup.2 (V)(c) reacting a 3-carbamoyloxyalkylpropiolic acid derivative represented by the general formula: ##STR5## with the benzylidene compound of the general formula III and ammonia or its salt; or(d) reacting the 3-carbamoyloxyalkylpropiolic acid derivative of the general formula VI with the aldehyde compound of the general formula IV, the .beta.-keto-ester compound of the general formula V and ammonia or its salt.

Abstract: Dihydropyridines having unsaturated side chains are disclosed. The compounds are useful anti-ischemic and antihypertensive agents.

Abstract: Compounds of formula I ##STR1## wherein R.sub.1 and R.sub.3, which are the same or different, are alkoxycarbonyl, acetyl, cyano, nitro, benzoyl or amino-carbonyl groups,R.sub.2 is differently substituted aryl or heteroaryl group;R.sub.4 is a C.sub.1 -C.sub.12 alkyl group optionally substituted by amino, alkoxyl, amine, etc. groups; alkenyl, or alkinyl groups; optionally substituted aryl or heteroaryl groups.Compounds I are useful as antihypertensives in human therapy.

Abstract: Circulation active compounds of the formula ##STR1## in which R.sup.1 is phenyl or heterocyclyl substituted by nitro, trifluoromethyl or other radicals,R.sup.2 is optionally substituted alkyl or other radicalR.sup.3 and R.sup.5 are hydrogen, methyl or other radicals,R.sup.4 is hydrogen or optionally substituted alkyl,X is from 2 to 15, andR.sup.6 is ##STR2## and physiologically acceptable salts thereof.

Abstract: Improved process for preparing pyridine-2,3-dicarboxylic acid compounds of the formula: ##STR1## wherein R.sup.1 and R.sup.3 are each H, (un)substituted alkyl, or (un)substituted phenyl; R.sup.2 is H, (un)substituted alkyl, (un)substituted phenyl, alkylthio, alkoxy, (un)substituted phenylthio, (un)substituted phenoxy, halogen, alkoxycarbonyl, aminocarbonyl which may optionally be substituted, or cyano; or both of R.sup.1 and R.sup.2 or both R.sup.2 and R.sup.3 may combined together to form a divalent alkylene; and R.sup.4 and R.sup.

Abstract: A 1,4-dihydropyridine derivative represented by the formula ##STR1## wherein R.sup.1 is a hydrogen atom, an alkoxy group having 1 to 4 carbon atoms, a mercapto group, an alkylcarbonylthio group in which the alkyl group has 1 to 4 carbon atoms or a benzoylthio group, R.sup.2 is a mercapto group, an alkylcarbonylthio group in which the alkyl group has 1 to 4 carbon atoms, a benzoylthio group or a 2-cyanoethylthio group, A and B are the same or different and are each an alkylene group having 1 to 4 carbon atoms, and X is a hydrogen atom, a halogen atom, a nitro group or a trifluoromethyl group is disclosed. These compounds increase the therapeutic effect of drug-resistant cancers.

Abstract: Compounds are described of the formula ##STR1## wherein R.sub.1 and R.sub.4 independently represent a C.sub.1-4 alkylgroup;R.sub.2 and R.sub.3 independently represent a C.sub.1-6 straight orbranched alkyl chain or alkoxy group;R.sub.4 represents a C.sub.1-4 alkyl group;R.sub.5 represents a group CH.dbd.CR.sub.6 R.sub.7 where R.sub.6 is a hydrogen atom or C.sub.1-3 alkyl group and R.sub.7 represents an aryl, pyridyl or cyano group; or R.sub.5 represents the group C.tbd.CR.sub.8 where R.sub.8 is an aryl group.The compounds represented by formula (I) reduce intracellular calcium ion concentration by limiting transmembranal calcium ion influx and thus may be useful for the treatment of cardiovascular disorders such as hypertension.

Abstract: A process for the ozonization of unsaturated organic compounds in a reaction column through which the unsaturated compounds--in solution in a protic solvent--and an ozone-containing carrier gas and an inert coolant are passed downward in co-current flow to provide for an improved coolant effect and an increased ozonization yield where the coolant comprises a compound gaseous or liquid at ambient temperature with a boiling point preferably in the range from +20.degree. C. to -200.degree. C. The boiling point of the coolant is preferably at least 5.degree. C. below the ozonization temperature.

Abstract: Compounds of formula I wherein R.sub.1 is an alkoxy carbonyl, aminocarbonyl, acetyl, benzyl, cyano or nitro group; R.sub.2 is as optionally substituted phenyl, aryl, hetaryl residue; R.sub.3 is an alkoxy-carbonyl group, X is an oxygen or sulphur atom, R.sub.4 is hydrogen, an optionally substituted alkyl, cycloalkyl, alkenyl group, Y is a single bond oxygen, sulphur or substituted nitrogen atom.Compounds of formula I are prepared by acylation from a 2-mercaptomethyl-1,4-dihydropyridine and are useful in therapy.

Abstract: Compounds are described of the formula ##STR1## wherein R.sub.1 represents a formyl or nitrile group or a group OCH.sub.2 A where A represents hydroxy, C.sub.1-4 alkoxy or D(CH.sub.2).sub.n NR.sub.7 R.sub.8 (where R.sub.7 and R.sub.8 independently represent hydrogen or C.sub.1-4 alkyl and n is 2 or 3);R.sub.2 and R.sub.3 independently represent a C.sub.1-6 straight or branched alkyl chain or alkoxy group;R.sub.4 represents a C.sub.1-4 alkyl group;R.sub.5 represents a straight or branched chain C.sub.1-13 alkyl group or a C.sub.5-8 cycloalkyl group which may be substituted by a C.sub.1-3 alkyl substituent;R.sub.6 represents a halogen atom or a straight or branched C.sub.1-3 alkyl group.The compounds represented by formula (I) reduce intracellular calcium ion concentration by limiting transmembranal calcium ion influx and thus may be useful for the treatment of cardiovascular disorders such as hypertension.

Abstract: Optically active compounds of formula 1 ##STR1## wherein R.sub.1 is H or lower alkyl;R.sub.2 and R.sub.6 are each independently lower alkyl, aryl, or arylalkyl;R.sub.3 is CN, NO.sub.2, CO.sub.2 R.sub.5, CONHR.sub.5, SO.sub.2 R.sub.5, or P(O)(OR.sub.5).sub.2, where R.sub.5 is lower alkyl, lower alkoxyalkyl, aryl, or arylalkyl;R.sub.4 is aryl, heterocyclyl, or fused-ring heterocyclyl, optionally substituted with one, two, or three halo, NO.sub.2, CN, lower alkyl, lower alkoxy, lower alkylamino, CF.sub.3, OCH.sub.2 F, or OCF.sub.3 ;are prepared by fractional crystallization from hot organic solvent and water in the presence of a suitable optically active amine base.

Abstract: Pyridines of formula I ##STR1## wherein R.sub.1 is acetyl, benzoyl, cyano, nitro, alkoxycarbonyl or aminocarbonyl groups; R.sub.2 is an optionally substituted aryl or a heterocyclic group; and .phi. is a sulphurated residue such as alkylthio, cycloakylthio, arylthio, heteroarylthio, aminoalkylthio.Compounds I are useful in therapy in cardiovascular field.

Abstract: This invention provides novel compounds represented by the general formula: ##STR1## R.sub.1 and R.sub.2 are each independently selected from the group consisting of hydrocarbyl radicals and heteroatom-substituted hydrocarbyl radicals, wherein said heteroatoms are selected from the group consisting of nitrogen, oxygen, sulfur, phosphorus and halogen atoms; A is a straight or branched chain hydrocarbon moiety containing from 1 to 12 carbon atoms and from 0 to 2 double bonds; R.sub.3 is selected from the group consisting of oxa- or dioxacycloalkanyl radicals which may be substituted with one or more hydroxy, keto, lower alkyl, phenyl or alkylenedioxy radicals; R.sub.4 is an aryl or heteroaryl radical; and R.sub.5 is a lower alkyl radical or A-R.sub.3 ; and pharmaceutically-acceptable salts thereof. These compounds are useful for treating coronary insufficiency, hypertension, angina pectoris, cardiac arrythmia, heart attack, or coronary vasospasm.

Abstract: Dihydropyridine derivatives represented by formula (I): ##STR1## wherein R.sub.1, R.sub.2, R.sub.3 and R.sub.6, which may be the same or different, each represents an alkyl group, a cycloalkyl group or an alkoxyalkyl group; R.sub.4 and R.sub.5, which may be the same or different, each represents a hydrogen atom, a halogen atom, a nitro group, a halogenated alkyl group, an alkylsulfonyl group, a halogenated alkoxy group, an alkylsulfinyl group, an alkyl group, a cycloalkyl group, an alkxoy group, a cyano group, an alkoxycarbonyl group or an alkylthio group (provided that R.sub.4 and R.sub.5 are not hydrogen atoms at the same time); X represents a vinylene group or an azomethine group; A and B are each an alkylene group or an alkenylene group; R.sub.7 and R.sub.8, which may be the same or different, each represents a hydrogen atom, an alkyl group, an alkenyl group, an aralkyl group, an aryl group, or a heterocyclic group (provided that R.sub.7 and R.sub.

Abstract: In the preparation of nitrenedipine by reaction of an ylidene compound of the formula ##STR1## with an enamine compound of the formula ##STR2## the improvement which comprises effecting the reaction in the presence of a catalytic amount of diisopropylamine acetate or dimethylbenzylamine acetate. The product is produced in high yield with reduced amounts of symmetrical by-products.

Abstract: The present invention relates to novel asymmetrical esters derived from 1,4-dihydropyridine-3,5-dicarboxylic acid, of the formula: ##STR1## in which: R.sub.1 represents a C.sub.1 -C.sub.4 alkyl group, R.sub.2 represents a C.sub.1 -C.sub.4 alkyl group, a benzyl group, a benzoyl group or a phenyl group optionally substituted by one or more C.sub.1 -C.sub.4 alkoxy, C.sub.1 -C.sub.4 alkyl, cyano, nitro, hydroxyl or trifluoromethyl groups or by one or more halogen atoms, and R.sub.3 and R.sub.4, which are identical or different, each represent the hydrogen atom, a nitro group or a chlorine atom,their optical isomers and diastereoisomers and also the corresponding addition salts.These novel esters are useful in therapy, especially as antihypertensives.

Abstract: 1,4-Dihydropyridine anti-ischaemic and antihypertensive agent of the formula: ##STR1## or a pharmaceutically acceptable salt thereof, wherein R is 2-chlorophenyl, 2,3-dichlorophenyl or 2-chloro-3-trifluoromethylphenyl;R.sup.1 and R.sup.2 are each independently C.sub.1 -C.sub.4 alkyl;X is O or S;R.sup.3 is H or C.sub.1 -C.sub.4 alkyl; andR.sup.4 is 1,2,4-triazol-1-ylmethyl, imidazol-1-ylmethyl, azidomethyl, 2,4,5-trimethylimidazol-1-ylmethyl, 3,4-dihydro-4-oxopyrimidin-2-ylthiomethyl, pyrimidin-2-ylthiomethyl; pyrimidin-2-ylaminomethyl, 3,4-dihydro-4-oxopyrimidin-2-ylaminomethyl, 2-aminopyrimidin-4-yloxymethyl, methoxymethyl, 2-furyl, 2-pyridylmethyl, imidazol-2-yl, hydroxymethyl, aminomethyl, 1,2,4-triazol-4-ylmethyl or 2-hydroxyethyl, and intermediates leading thereto.

Abstract: Novel phenoxy derivatives are provided which can be represented by the general formula: ##STR1## wherein the various substituents are as defined, and include compounds such as benzyl 6-[p-[5-(1-imidazolyl)pentyloxy]phenoxy]-2,2-dimethylhexanoate.The invention also encompasses pharmaceutical compositions containing the derivatives and their use in treating tumors.

Abstract: The invention provides novel amino acids and peptides containing them which comprise a dihydropyridine.revreaction.pyridinium salt-type redox system and which provide site-specific and sustained delivery of pharmacologically active peptides to the brain. These new amino acids contain a redox system appended directly or via an alkylene bridge to the carbon atom adjacent to the carboxyl carbon and may be incorporated into a peptide chain at a variety of positions, including non-terminal positions.

Abstract: Dihydropyridine derivatives of the formula ##STR1## wherein R.sub.1, R.sub.2, R.sub.3, R.sub.4, R.sub.5, A, B are defined as in the specification and nontoxic acid-addition salts thereof, have an excellent calcium blocking action (Ca-antagonist), and antihypertensive action, a platelet aggregation-inhibiting action, a phosphodiesterase-inhibiting action and the like, and thus are useful as a medicine, such as a coronary vasocilator, a cerebral hyperkinemic, antihypertensive, thrombosis-preventing or -treating agents, phosphodiesterase-inhibitor or the like. Pharmaceutical compositions and methods of use are also disclosed.

Abstract: Improved pharmaceutical salts of amlodipine, particularly the besylate salt, and pharmaceutical compositions thereof. These salts find utility as anti-ischaemic and anti-hypertensive agents.

Abstract: A pharmaceutical preparation is disclosed which is made up of a micelle or a vesicle each consisting of a cationic tenside with a monovalent ion and a hydrophobic cyclic or linear peptide, dispersed in a solvent whose pH value lies between pH 7-pH 8, the critical micellization concentration (cmc) lying in the range of 1.0 . 10.sup.-7 to 7.0 . 10.sup.-5 mol/liter. The preparation disclosed have in particular the advantage that by the increasing of the hydrophobicity of the alkyl or aryl chain or the radical at the N.sup.+ tenside both the membrane permeability is increased and furthermore the pharmaceutical active substance, in particular linear and cyclic tyrocidines (A-E), can be transferred actively into the cytosol. They thus act on the transcription level. In addition, linear and cyclic tyrocidines in particular have antiviral effects.

Abstract: A dihydropyridine of the formula: ##STR1## wherein R.sup.1 and R.sup.2 each is alkyl, alkenyl or alkoxyalkyl, wherein R.sup.3 and R.sup.4 each is alkyl, wherein benzene ring A is unsubstituted or bears one or more additional substituents selected from halogeno, cyano, nitro, trifluoromethyl and alkyl, or bears the substituent .dbd.N--O--N.dbd. attached to the 5- and 6-positions, wherein Ar is as defined in the specification, wherein p is 0 or 1, wherein X is --O-- or --S--, and wherein Y is straight-or branched-chain alkylene or alkenylene each of 2 to 12 carbon atoms which may optionally be interrupted by one or two groups selected from oxygen, sulphur, imino, substituted imino, phenylene, substituted phenylene, pyridylene, cycloalkylene, 1,4-piperazinediyl, 1,4-piperidinediyl and amido groups; or an acid-addition salt thereof, processes for their manufacture and pharmaceutical compositions containing them.

Abstract: A novel method is disclosed for the preparation of 2,3-pyridine-dicarboxylates by the reaction of a ketoester such as dimethyl oxalacetate with an .alpha.,.beta.-unsaturated aldehyde or ketone such as 2-ethylacrolein and at least 1 molar equivalent of ammonium salt in suitable solvent utilizing a dehydrogenation catalyst such as palladium on carbon.

Abstract: Compounds of general formula I: ##STR1## in which: Ar represents a phenyl radical optionally containing one to five identical or different substituents, representing a halogen atom, an alkoxy radical containing 1 to 4 carbon atoms, an alkylthio radical containing 1 to 4 carbon atoms, a trihalomethyl radical or a methylenedioxy radical,Y, Z, Y.sub.1, Z.sub.1, W, V, U, m, n, R.sub.1, R.sub.2 are as defined in the specification. The compounds are used as calcium modulators.

Abstract: Circulation active compounds of the formula ##STR1## in which R.sup.1 is phenyl or heterocyclyl substituted by nitro, trifluoromethyl or other radicals,R.sup.2 is optionally substituted alkyl or other radicalR.sup.3 and R.sup.5 are hydrogen, methyl or other radicals,R.sup.4 is hydrogen or optionally substituted alkyl,X is from 2 to 15, andR.sup.6 is ##STR2## and physiologically acceptable salts thereof.

Abstract: A process is disclosed for the preparation of a compound of formula (I): ##STR1## where Ar is aryl or substituted aryl and R.sup.3 and R.sup.4 are the same or different and each is alkyl, which process comprises hydrognating a compound of formula (II): ##STR2## wherein Ar, R.sup.3 and R.sup.4 are as defined with respect to formula (I) and Hal is a halogen atom.Compounds of formula (I) are useful as chemical intermediates.

Abstract: Labellable reagents for fluormetric assays comprise a cyclic condensation product of a .beta.-diketone, an aldehyde and an NH.sub.2 -bearing macromolecule, for example an antigen or antibody or a substance having an active group to which an antibody or antigen is linked. The reagents can chelate lanthanide metal ions such as Eu(II) and Tb(III) to form fluorescing complexes which can be used as labelled reagents for fluorometric assay of organic substances, for example antigens, antibodies and other substances occurring in body fluids.

Abstract: The invention relates to optically active 1,4-dihydropyridine compounds of Formulas Ia and Ib as defined hereinabove which are effective for influencing circulation. Also included in the invention are compositions containing said optically active compounds and methods for the use of said compounds and compositions.

Abstract: There is provided a dihydropyridine derivative having the formula ##STR1## wherein R'.sub.1 denotes methyl, chlorine, bromine, fluorine, trifluoromethyl, nitro, cyano or methoxy, R.sub.7 denotes benzyl; and the dihydropyridine links to the 2-, 3-, or 4-position of the pyridine.The compound has an activity as a Ca-antagonist, and is useful for treating vascular disorders such as coronary artery disease, celebral artery disease, hypertension and the like.

Abstract: This invention provides compounds useful for treating coronary insufficiency, hypertension, angina pectoris, cardiac arrythmia, heart attack or coronary vasospasm and represented by the general formula: ##STR1## R.sub.1 and R.sub.2 are each independently selected from the group consisting of lower alkyl, N-alkylphthalimido and derivatives of N-alkylphthalimido, wherein said N-alkyl group comprises at least 2 carbon atoms;A is a straight or branched chain hydrocarbon moiety containing from 1 to 12 carbon atoms and from 0 to 2 double bonds;R.sub.3 is selected from the group of radicals consisting of hydrogen, --NH.sub.2 and --NCS;R.sub.4 is an aryl or heteroaryl radical; andR.sub.5 is a lower alkyl radical or A--R.sub.3 ; provided that when R.sub.3 is a hydrogen radical at least one of R.sub.1 and R.sub.2 is not lower alkyl, including both pure enantiomers as well as mixtures thereof; andpharmaceutically-acceptable salts thereof.

Abstract: Compounds of formula I ##STR1## wherein R is hydrogen or lower alkyl; R.sub.1 is acetyl, benzoyl, cyano, nitro, carboxy, alkoxycarbonyl or aminocarbonyl groups; R.sub.2 is an optionally substituted aryl or hetaryl residue; R.sub.3 is a carboxy or alkoxycarbonyl group; A is a cyclopropyl group or a group of formula --CH.dbd.CH-- and R.sub.4 is a phenyl or heteroaryl group, optionally mono, di or tri-substituted, are useful in radical scavenging therapy.

Abstract: Novel compounds, that is, alkoxy- and phenoxy-alkyl esters of 2,6-dimethyl-4-(2-difluoromethoxyphenyl)-1,4-dihydropyridine-3,5-dicarboxy li c acid have the following general formula useful for producing hypotensive and vasodilation effects.

Abstract: The present invention provides pyridine derivatives of following general formula (I) or a physiologically acceptable acid addition salt thereof: ##STR1## wherein R.sub.1 is a hydrogen atom or a hydroxy group, R.sub.2 and R.sub.3, which may be the same or different, each is a lower alkyl group, and n is an integer of 1 to 6. The invention also provides for producing the pyridine derivative and pharmaceutical compositions containing the same. The compounds (I) possess anti-arrhythmic activity.

Abstract: Dihydropyridines of formula I ##STR1## wherein R is hydrogen or lower alkyl; R.sub.1 is a CN, NO.sub.2, COCH.sub.3, COPh group, a carboalkoxy or carboamide group; R.sub.2 is an aromatic or heteroaromatic, mono- or bicyclic eventually substituted phenyl group; R.sub.3 is a carboalkoxy group; while A is a halogen atom or an ammonium or phosphonium residue. The compounds I are useful as antihypertensive, antitumoral, antimetastatic, antithrombotic, and/or antiischemic agent.

Abstract: Disclosed herein are 3,5-pyridinedicarboxylic acid derivatives having halogen substitution at the 4 position which are useful as herbicides and herbicide precursors.

Abstract: Optically active nitrogen-containing heterocycles of the formula I according to claim 1 are suitable as components for ferroelectric liquid crystalline materials.

Abstract: The invention relates to new substituted dihydropyridine derivatives of the general formula (I), ##STR1## wherein R.sup.1 and R.sup.6 are as defined herein after, the racemic and optically active variants as well as mixtures thereof, furthermore the acid addition salts of these compounds, pharmaceutical compositions containing the same and a process for the preparation thereof.The compounds of the general formula (I) can be advantageously applied for the treatment of pathologically severe hypertensions, their toxicity is low and they possess an advantageous therapeutic index.

Abstract: There are disclosed novel 2,6-substituted-3,5-pyridinedicarboxylic acids, esters, salts, amides, halides, and cyano compounds useful as herbicides, and as intermediates which provide herbicides.

Abstract: 1,4-Dihydropyridine derivatives represented by the formula ##STR1## wherein one of R.sup.1 and R.sup.2 is cycloalkylmethyl group and the other is a group of ##STR2## in which R.sup.3 is hydrogen atom or lower alkyl group and R.sup.4 is hydrogen atom, hydroxyl radical, carboxyl radical, alkoxycarbonyl group, carbamoyl radical, phenyl radical, substituted phenyl radical or trialkylsilyl group, or R.sup.3 and R.sup.4 may be bonded each other, and n and m are an integer of 1 to 6, respectively salts thereof, a process for the preparation of same as well as a pharmaceutical agent comprising the compound or salt, as an effective ingredient.

Abstract: 1,4-Dihydropyridine derivatives of the formula (1): ##STR1## wherein X is a halogen; R.sup.1 is a straight, branched or cyclic alkyl group having 1 to 10 carbon atoms, the group --(CH.sub.2).sub.n -Y [where n is an integer of 0 to 8, provided that n is an integer of 2 to 8 when Y is not bonded to COO-- through carbon; Y is a cyclic alkyl group having 3-6 carbon atoms, an aryl group having 6-10 carbon atoms, a pyrrolidinyl group, an imidazolidinyl group, a thienyl group, a furyl group, an imidazolyl group, a pyridyl group, a pyrimidinyl group, a morpholinyl group, a thiomorpholinyl group or a pyrrolizidinyl group, the group ##STR2## (where D is an aryl or aralkyl group having 6-15 carbon atoms which may be substituted by a halogenated alkyl group), or a 3-piperidinyl group substituted by a phenylalkyl group of 7-10 carbon atoms which may be substituted by one or two halogens], the group --(CH.sub.2).sub.

Abstract: The invention relates to novel 1,4-dihydropyridine-3-carboxylic acid phenoxyaliphatylphenyleneoxyalkyl esters of the formula ##STR1## in which Ac represents an acyl group, X represents oxy or optionally substituted imino, A represents a divalent aliphatic hydrocarbon radical interrupted by a group --X.sub.1 --Ph--X.sub.2 -- in which at least one of the radicals X.sub.1 and X.sub.2 represents oxy and a radical X.sub.1 or X.sub.2 that is other than oxy represents a direct bond, and Ph represents an optionally substituted phenylene radical, and R represents an optionally substituted phenyl, pyridyl or 1-oxidopyridyl, (1,3-dioxa)indanyl or benzofurazanyl radical, R.sub.1 represents an optionally substituted phenyl or indolyl radical, R.sub.2 represents an aliphatic hydrocarbon radical and R.sub.3 represents an aliphatic radical, cyano or amino, and acid addition salts thereof.

Abstract: The present invention provides a novel method for the preparation of pyridine-2,3-dicarboxylic acids by the oxidation of 8-substituted quinolines.

Abstract: A series of compounds of the 1,4-dihydropyridine class with a 3-carboxylate group linked to an alkyleneaminoalkylene heteroatom have been prepared possessing the general formula ##STR1## wherein R.sup.2, R.sup.5 and R.sup.6 are independently selected from lower (C.sub.1-4)alkyl, hydroxy-lower-alkylene, lower alkoxy-lower-alkylene, lower alkylamino-lower-alkylene or lower dialkyl-amino-lower-alkylene; R.sup.7 is selected from hydrogen, lower alkyl, phenyl-lower-alkylene, or phenylthio-lower-alkylene; n is the integer 2 or 3; X is a chemical bond, --O--, --S--, ##STR2## or --NR.sup.9 -- wherein R.sup.9 is hydrogen, lower alkyl, phenyl, or phenyl-lower-alkylene with the proviso that when X is a chemical bond, Z is a 3-indolyl ring; and Z is selected from the group consisting of phenyl substituted with 1 to 3 substituents independently chosen from among hydrogen, lower alkyl, or lower alkoxy, phenyl-lower-alkylene, or 3-indolyl.

Abstract: A process for the preparation of a fluoroaromatic or fluoroheterocyclic compound, which comprises diazotizing the corresponding amino-aromatic or amino-heterocyclic compound in hydrogen fluoride and decomposing the diazonium salt in the diazotization mixture so formed, characterized in that decomposition is carried out at super atmospheric pressure.

Abstract: Compounds of the formula ##STR1## in which R represents a carbocyclic or heterocyclic aryl radical, R.sub.1 represents lower alkyl, one of the groups R.sub.2 and R.sub.3 represents lower alkyl and the other represents lower alkyl, cyano aor amino, X represents oxygen or the group --NH--, Alk.sub.1 represents lower alkylene or optionally substituted phenyl-lower alkylene, which separates the group X from the nitrogen atom by at least two carbon atoms, R.sub.4 represents hydrogen, lower alkyl or optionally substituted phenyl-lower alkyl, Z represents the group --(C.dbd.O)-- or a single bond, Alk.sub.2 represents lower alkylene which separates the groups Z and Y preferably by from 2 to 4 carbon atoms, Y represents the group --(C.dbd.O)-- and Ar.sub.1 represents a monocyclic, carbocyclic or heterocyclic aryl radical, and salts of such compounds having salt-forming properties, have cardiovascular properties, especially coronary dilatory and anti-hypertensive properties.

Abstract: Circulation active, e.g. antihypertensive novel methionine-substituted dihydropyridines of the formula ##STR1## in which R.sup.1 is phenyl or a heterocyclic radical, or a physiologically acceptable salt thereof.