Abstract: This invention relates to a 1,4-dihydropyridine-3,5-dicarboxylate derivative represented by the following general formula (I): ##STR1## wherein R means an imidazolyl or pyridyl group, R.sub.1 denotes a hydrogen or halogen atom or a nitro or trifluoromethyl group, R.sub.2 is a lower alkyl group, X is CH or N, A means a lower alkylene group, ##STR2## B being a lower alkylene or O-lower alkylene group, ##STR3## R.sub.4 being a hydrogen atom or lower alkyl group, or ##STR4## m denotes a number of 1-3, and n stands for 1 or 2. The derivative has vasodilative effects, hyperkinemic effects, platelet aggregation inhibitory effects, thromboxane A.sub.2 formation inhibitory effects and so on, and are hence useful as a pharmaceutical product such as vasodilator, antihypertensive, antithrombotic agent, antiarteriosclerotic agent or the like.

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: The present invention are 2-(2-aryl-2-oxo-alkylidene) analogs of 1,2,3,4-tetrahydropyridine-3,5-pyridinecarboxylic acids and particularly esters thereof having valuable calcium antagonist and positive inotropic activity useful in the treatment of cardiovascular disorders, pharmaceutical compositions and methods of use therefor.

Abstract: This invention relates to a novel 1,4-dihydropyridine derivative of the formula ##STR1## wherein R2 is pyridyl, or a salt thereof. These compounds have a vasodilating activity and a platelet aggregation inhibiting activity. Also disclosed are pharmaceutical compositions containing the same.

Abstract: The preparation of esters of 1,4-dihydropyridine, useful in the prevention and treatment of cardiovascular disorders such as atheroma, of the formula ##STR1## wherein X is a phenyl moiety and Y is piperazine, piperidine or an amide of a benzenecarboxylic acid, is described.

Abstract: This invention relates to a 1,4-dihydropyridine derivative of the formula ##STR1## wherein Y represents an oxygen or sulfur atom or a vinylene group, Z represents an oxygen or sulfur atom or an alkylene group, R.sup.2 represents an imidazolyl or pyridyl group and the remaining substituents are herein defined. These compounds have a vasodilating activity and a platelet aggregation inhibiting activity.

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-Dihydropyridines of the formula ##STR1## in which R.sup.1 is hydrogen, or alkyl optionally substituted by halogen, nitro, cyano, alkoxy, carboxyl, alkoxycarbonyl or carboxamide,R.sup.2 is hydrogen or alkyl,R.sup.3 is hydrogen, alkyl, carboxyl, alkoxycarbonyl or aryl optionally substituted by hydroxyalkyl, carboxyl, sulphoxy, acloxyalkyl, or ##STR2## R.sup.4 is alkyl, aryl, heteroaryl, aralkyl, heteroaralkyl, ##STR3## X is oxygen, sulphur or NH, and n is 1 to 6,or physiologically acceptable salts thereof, which are active in combating thromboembolic and ischaemic disorders.

Abstract: Novel 2-(2-alkoxy-2-oxoethylidene)-1,2,3,4-tetrahydro-6-methyl-4-[2-(substituted )phenyl]-3,5-pyridinedicarboxylic acid dialkyl ester derivatives having novel inotropic and hypotensive activity, processes for their manufacture, pharmaceutical compositions, and methods for using said compounds and compositions are described.

Abstract: A method for alleviating cisplatin compound-induced nephrotoxicity in animals comprising administering to the animal an effective amount of a polar dithiocarbamate compound. The polar dithiocarbamate compounds have the formula: ##STR1## In the above formula, R.sup.1 and R.sup.2 are hydrocarbon groups and R.sup.1, R.sup.2, or both R.sup.1 and R.sup.2 contain a polar group substituted thereon. M is a pharmaceutically acceptable cation and n is an integer of from 1 to 3.Novel polar dithiocarbamate compounds are disclosed as well.

Abstract: Pyridinecarboxylic esters of dopamine and of its N-alkyl derivatives, salts thereof with pharmaceutically acceptable organic or inorganic acids, process for preparing them and pharmaceutical compositions containing them which are particularly useful in the treatment of cardiovascular and renal disorders.

Abstract: 1,4-Dihydropyridine-3,5-dicarboxylic acid ester derivatives of the general formula: ##STR1## or acid addition salts thereof, wherein W is --CH.dbd. or --N.dbd.; Y is --CH.dbd.CH--, --O--, --S--, --CH.dbd.N(O)p-- (p is zero or 1) or --N(R)-- (R is hydrogen or lower alkyl); X.sup.1, X.sup.2 and X.sup.3 are the same or different, and are each hydrogen, halogen, nitro, trifluoromethyl, cyano or lower alkylthio; Z is aryl or 5- or 6-membered aromatic heterocyclic ring (which may have a substituent or two or three substituents which may be the same or different, and the substituent may be halogen, lower alkyl, lower alkoxy, lower alkanoylamino, cyano, nitro, lower alkylthio, trifluoromethyl, sulfamoyl, di-lower alkylsulfamoyl, amino or di-lower alkylamino); ##STR2## is 5- to 7-membered heterocyclic ring which may have nitrogen atom, oxygen atom, sulfur atom or unsaturated bond on the ring, and may be substituted by lower alkyl, lower alkoxycarbonyl, lower alkanoylamino, ethylenedioxy or --(CH.sub.2).sub.m --OR.sup.

Abstract: Compounds of the formula I ##STR1## in which n represents 1, 2 or 3, Ar represents a carbocyclic or heterocyclic aryl radical, Ac represents the acyl radical of an acid, Z represents a radical --OR.sub.7 or --NR.sub.8 R.sub.9, R.sub.1 represents hydrogen, unsubstituted or substituted lower alkyl, a carbocyclic or heterocyclic aryl radical or free, etherified or esterified hydroxy, R.sub.2 and R.sub.3, independently of one another, each represents hydrogen, unsubstituted or substituted lower alkyl, formyl or functionally modified formyl, carboxy or functionally modified carboxy, a carbocyclic or heterocyclic aryl radical or unsubstituted or mono- or di-substituted amino, R.sub.4 represents hydrogen or lower alkyl, R.sub.5 and R.sub.6, independently of one another, each represents hydrogen, unsubstituted or substituted lower alkyl or a carbocyclic or heterocyclic aryl radical, R.sub.7, R.sub.8 and R.sub.

Abstract: Carboxylic acid esters are produced by the reaction of a carboxylic acid halide with a carbonate ester in the presence of an initiator. The reaction of a dicarboxylic acid dihalide and a bis(alkyl carbonate) ester produces a polymeric polyester.

Abstract: A process for the preparation of 1,4-oxazepinones and thiones having the formula: ##STR1## wherein A is an aromatic ring selected from benzene, naphthalene, quinoline or pyridine; n is 1 to 3; Z is an amino radical; R is hydrogen, loweralkyl, cycloalkyl or phenylloweralkyl; and R.sup.4 and R.sup.5 are hydrogen and loweralkyl starting from chloroaromatic carboxylates and alkanolamines is disclosed.

Abstract: This invention is directed to acid terminated azomethines formed by reacting aromatic dialdehydes or aromatic diketones with amino-carboxylic acid compounds. These oligomers may be reacted with epoxy resins to produce polymer material having high glass transition temperatures.

Abstract: 1,2,3,4-Tetrahydropyridines of the formula ##STR1## in which R.sup.1 is optionally substituted aryl or heterocyclic,R.sup.2 is an organic radical,X is a nitrile or ester,R.sup.3 and R.sup.5 are identical or different and each represent hydrogen, a straight-chain or branched or salts thereof with physiologically tolerated acids are antihypertensives.

Abstract: Novel compounds of the formula: ##STR1## wherein R.sup.2 is an aromatic or heterocyclic group, which may optionally be substituted, R.sup.2 is a methyl group, a hydroxymethyl group, a nitroxymethyl group, a formyl group, a nitrogen-containing five-membered ring-methyl group, an acetal-methyl group, a trialkylsilyloxymethyl group, an alkyl- or aryl-sulfonyloxymethyl group, an alkyl- or aryl-sulfonylaminocarbonyloxymethyl group, an acyloxymethyl group, an alkoxycarbonyloxymethyl group, a halogenomethyl group, an alkoxymethyl group, an aryloxymethyl group, a cyano group, a carbamoyl group which may optionally be substituted, a carbamoyloxymethyl group which may optionally be substituted, a thiocarbamoyloxymethyl group which may optionally be substituted, and an alkoxycarbonyl group, n is an integer of 1 to 20, and ##STR2## provided that n is an integer of 9 to 20 when ##STR3## and, at the same time, R.sup.

Abstract: 4-Cyano-2-azetidinone derivatives represented by the formula ##STR1## wherein R.sup.1 is an amino group which may be acylated or protected, X is a hydrogen atom or a methoxy group and W is a hydrogen atom or a sulfo group, and methods of producing the same, for example, as represented by ##STR2## wherein R.sup.2 is an acylated or protected amino group, Y is a halogen atom or a group having the formula --OCOR.sup.3, --SCOR.sup.3 or --S(O).sub.n --R.sup.3 (R.sup.3 being a hydrocarbyl group and n an integer 1 or 2), R.sup.4 is an amino group which may be acylated or protected and X is as defined above. Compounds [I] are useful as advantageous intermediates for the synthesis of optically active 4-substituted-2-azetidinone derivatives, and, when W=SO.sub.3 H, [I] are also useful as antimicrobial agents and as beta-lactamase inhibitors.

Abstract: 1,2,3,4-Tetrahydropyridines of the formula ##STR1## in which R.sup.1 is optionally substituted aryl or heterocyclic,R.sup.2 is an organic radical, X is a nitrile or an esterR.sup.3 and R.sup.5 are identical or different and each represent hydrogen, a straight-chain or branched or salts thereof with physiologically tolerated acids are antihypertensives.

Abstract: Disclosed are compounds of the general formula: ##STR1## wherein R.sub.1 is amino, an acylated amino or a protected amino group, X is hydrogen or methoxy, and R' is hydrogen, R or R.sup.4 wherein R is an organic residue attached to the azetidine ring through a carbon atom therein and R.sub.4 is azido, a halogen, an amino group which may optionally be acylated or a group of the formula --OR.sub.5, ##STR2## or --S--S--R.sub.5 wherein R.sub.5 is an organic residue and n is 0, 1 or 2, and pharmaceutically acceptable salts and esters thereof.The compounds have antimicrobial and/or .beta.-lactamase-inhibitory activity and are of value as drugs for human beings and domesticated animals.

Abstract: .alpha.-Cyanoacrylic acid lower alkyl esters, and their corresponding amides, characterized by having a heterocyclic containing mercapto radical as one .beta.-substituent and an alkylthio, alkenylthio or a heterocyclic containing mercapto radical as another .beta.-substituent are useful for treating ulcers and for suppressing gastric acid secretion.

Abstract: This invention provides an improved process for direct hydrogenation of a carboxylic acid to its corresponding alcohol with synthesis gas in the presence of a homogeneous catalyst comprising a ruthenium compound and a Lewis Acid metal halide.

Abstract: New compounds of general formula ##STR1## and salts therewith of pharmaceutically acceptable acids, wherein R and R.sub.1 independently represent a hydrogen atom or a straight or branched alkyl group having from 1 to 5 carbon atoms, and n is an integer from 4 to 12; and of general formula ##STR2## wherein R'.sub.1 represents a straight or branched alkyl group having from 2 to 4 carbon atoms, W represents hydroxymethyl or the COOM group in which M stands for a hydrogen atom, an alkali metal or an equivalent of an alkali earth metal and n is an integer from 6 to 8. The compounds are useful in treating hyperlipidaemia.

Abstract: A dihydropyridine compound of the formula: ##STR1## or a pharmaceutically acceptable acid addition salt thereof, wherein Het is 5- or 6-membered aromatic heteroaryl, R.sup.1 and R.sup.2 are each lower alkyl, R.sup.3 is lower alkyl, R.sup.4 is hydrogen, lower alkyl or aralkyl, R.sup.5 is lower alkyl or aralkyl, and n is 1 or 2. Such compounds are useful as therapeutic agents for myocardial and cerebral ischemic syndroms and hypertension.

Abstract: This invention relates to 2-amino-3-hydroxy, and 3-carboxy pyridine derivatives, in which the amino group is substituted by a methylthioethyl, butyl or oxypropyl group bearing a terminal heterocyclic group. The compounds have histamine H.sub.2 -antagonist activity. A specific compound of this invention is 2-[2-(2-guanidino-4-thiazolylmethylthio)ethyl]amino pyridine 3-carboxylic acid.

Abstract: The invention concerns compounds of formula ##STR1## and acid addition and quaternary ammonium salts thereof, wherein the dotted line represents an optional bond, Ar represents a ring system of formula ##STR2## in which Q is O,S,--CR.sup.7 .dbd.CR.sup.8 --, --N.dbd.CR.sup.8 -- and --N.dbd.N--; R.sup.4, R.sup.5 and R.sup.6, and R.sup.7 and R.sup.8 when present, each represent hydrogen or defined substituents and additionally either R.sup.4 and R.sup.5 when adjacent or R.sup.6 and R.sup.8 when adjacent, together with the carbon atoms to which they are attached also represent a fused five or six membered carbocyclic or heterocyclic ring optionally carrying one or more defined substituents; R is an optionally substituted aryl or heteroaryl radical or a cycloalkyl radical containing 5 to 7 carbon atoms; R.sup.1, R.sup.2, R.sup.3 and R.sup.9 are each hydrogen or a lower alkyl group; n is 0 or 1; X is .dbd.O, .dbd.S or .dbd.NH; Y is --O-- or a direct bond and Z is --CO-- or --CH.sub.

Abstract: Novel compounds having vasodilation and hypotensive effects are represented by the formula ##STR1## where R.sup.1 is halogen, nitro, cyano or lower alkoxy; each of R.sup.2 and R.sup.3 is lower alkyl, lower haloalkyl, lower alkoxyalkyl, aralkyloxyalkyl, aryloxyalkyl, lower alkenoxyalkyl, N,N-di-lower alkylaminoalkyl, N-lower alkyl-N-aralkylaminoalkyl, piperidylalkyl, 4-lower alkyl piperazinylalkyl, norpholinoalkyl or 1-pyrrolidinylalkyl; R.sup.4 is lower alkyl; A is lower alkylene; and R.sup.5 is hydrogen, lower alkyl, cycloalkyl of 3 to 7 carbon atoms, or aryl unsubstituted or substituted by one or two substituents selected from halogen, nitro, lower alkyl, lower alkoxy, di-lower alkylamino and cyano.Also disclosed are processes for their preparation.

Abstract: The nicotinic ester of (3-4)-O-isopropylidene pyridixole having the formula: ##STR1## shows analgesic and anti-inflammatory activity.

Abstract: 6-Aminonicotinic acid is reacted with an alkali carbonate selected from the group consisting of sodium carbonate and potassium carbonate. The reaction is carried out at elevated temperature and in dimethylformamide. The 6-aminonicotinic acid alkali salt so produced is reacted with 3-chloromethylpyridine hydrochloride. The reaction is carried out at elevated temperature and in dimethylformamide. The desired nicotinyl ester is thus produced.

Abstract: Mercaptoalkylpyridines carrying an ethenyl or ethynyl substituent are prepared from known pyridine compounds, principally pyridoxine, by known chemical procedures, and are useful in the treatment of rheumatoid arthritis and related inflammatory diseases.

Abstract: Aromatic acids having the following formula ##STR1## have been found to be effective plant growth regulants especially for the treatment of corn plants.

Abstract: The invention relates to a novel process and novel intermediates useful in the preparation of sympathomimetic amines. The pharmacologically useful final products, which are acyl derivatives of mono- and dihydroxy aromatic amines (e.g., catechol amines) can be prepared in optically active or racemic form by reacting the corresponding mono- or dihydroxy aromatic amine with a reagent capable of forming the N-tert-butoxycarbonyl derivative thereof; reacting the novel intermediate thus obtained with an acyloxymethyl chloride to afford the corresponding novel mono- or diacylated N-protected aromatic amine; and removing the N-protecting group therefrom.

Abstract: The present invention relates to compounds which are derivatives of 1,4-dihydropyridine-3-carbothiol acids of the formula: ##STR1## wherein R is hydrogen, an alkyl, aryl, heteryl;R' is a lower alkyl, aralkyl;R" is an alkoxy, alkylthio, aralkylthio;R"' is methyl;R"'+R" is phenylene (ortho-).The compounds of the present invention reveal a coronarodilating activity, and are useful in medicine.

Abstract: Derivatives of benzoylphenoxyalkanoic acids corresponding to the formula: ##STR1## wherein: X represents for example a halogen, R.sup.1 and R.sup.2 represent for example alkyl groups, R represents for example an aminoacid; and the salts thereof are new products showing antilipaemic and anticholesterolemic pharmacological activity.

Abstract: A compound of the formula: ##STR1## wherein R.sub.1, R.sub.2 and R.sub.3 each represents a member selected from the group consisting of hydrogen and nicotinoyl, with the proviso that R.sub.1, R.sub.2 and R.sub.3 do not all simultaneously represent hydrogen, and the nontoxic acid addition salts thereof.

Abstract: The invention relates to a novel process and novel intermediates useful in the preparation of sympathomimetic amines. The pharmacologically useful final products, which are acyl derivatives of mono- and dihydroxy aromatic amines (e.g., catechol amines) can be prepared in optically active or racemic form by reacting the corresponding mono- or dihydroxy aromatic amine with a reagent capable of forming the N-tert-butoxycarbonyl derivative thereof; reacting the novel intermediate thus obtained with an acyloxymethyl chloride to afford the corresponding novel mono- or diacylated N-protected aromatic amine; and removing the N-protecting group therefrom.

Abstract: This invention relates to 2-substituted and 2,6-disubstituted penem compounds of the formula ##STR1## wherein Y is hydrogen, halo or certain organic substituents and X represents certain organic substituents. Also included in the invention are pharmaceutically acceptable salts of the above compounds and derivatives of the above compounds in which the carboxyl group at the 3-position is protected as by an easily removable ester protecting group. The compounds of the present invention are potent antibacterial agents or are of use as intermediates in the preparation of such agents.

Abstract: The invention relates to fluorine-containing 1,4-dihydropyridine compounds and method for their preparation. Also included are compositions containing said fluorine-containing 1,4-dihydropyridine compounds and the use of said compounds and compositions as agents for influencing circulation.

Abstract: Disclosed are antibiotic cephalosporins (I) of the formula: ##STR1## Wherein the stylized radical attached to the 7-amino nitrogen of the cephalosporin moiety represents a nitrogen-containing heterocyclic group (mono- or polycyclic); R is, inter alia, hydrogen, alkyl, heterocyclylalkyl, aryl, alkenyl, aralkyl, --NR.sub.2, --OR, COOR, CONR.sub.2 or CN; A is conventionally known in the cephalosporin art; and R.sup.2 is H, or loweralkoxyl; X is O, CH.sub.2, or NR.sup.7 (R.sup.7 is, inter alia, hydrogen, alkyl or aralkyl. Also disclosed are the pharmaceutically acceptable salt and ester derivatives of I; processes for the preparation of such compounds, pharmaceutical compositions comprising such compounds; and methods of treatment comprising administering such compounds and compositions when an antibiotic effect is indicated.

Abstract: The present invention relates to compounds which are derivatives of 1,4-dihydropyridine-3-carbothiol acids of the formula: ##STR1## wherein R is hydrogen, an alkyl, aryl, heteryl;R' is a lower alkyl, aralkyl;R" is an alkoxy, alkylthio, aralkylthio;R"' is methyl;R'"+R" is phenylene (ortho-).The compounds of the present invention reveal a coronarodilating activity, and are useful in medicine.

Abstract: New mercaptoacyl derivatives of 4,5-dihydro-1H-pyrrole-2-carboxylic acids and 1,4,5,6-tetrahydropyridine-2-carboxylic acids having the general formula ##STR1## are useful as hypotensive agents.

Abstract: Carboxylic acid anhydrides are contacted with hydrogen in the presence of an insoluble metal hydrogenation catalyst and strong protonic acid to produce 1,1-diesters.

Abstract: Steroids of the formula ##STR1## wherein R.sub.1 and R.sub.2 are identical or different and each is hydrogen or the residue of an organic or inorganic acid,and for the esters (R.sub.1 or R.sub.2 is not H) capable of salt formation, the salts thereof, possess valuable pharmacological properties, e.g., good antiandrogenic activity with low progestational activity.

Abstract: New compounds which have the general formula ##STR1## are useful as hypotensive agents.

Abstract: The circulation provides new aminoalkylidene-amino-1,4-dihydropyridines which influence the circulatory system and are useful, for instance, as antihypertensive agents. Also included in the invention are methods for the preparation of said dihydropyridines, compositions containing them and methods for their use.

Abstract: Mono-, di- and tri-esters of 3-(hydroxy or hydroxymethyl)-4-hydroxy-.alpha.-(aminomethyl)benzyl alcohols, obtained by methods involving reduction of the corresponding mono- and di-ester ketones, are useful for producing sympathomimetic effects, such as bronchodilation, of long duration with low cardiovascular stimulating effect, in warm-blooded mammals.

Abstract: D-homopregnanes of the formula ##STR1## wherein R.sup.6 is hydrogen, chloro, fluoro or methyl; X is .beta.-hydroxymethylene or carbonyl; R.sup.17a is hydroxy, lower alkanoyloxy or aroyloxy; R.sup.21 is hydrogen, chloro, fluoro, hydroxy, lower alkanoyloxy, aroyloxy, sulfate or phosphate; and the dotted line in the 1,2-position of the A-ring denotes an additional carbon-carbon bondAnd pharmaceutically acceptable salts thereof, processes for the preparation thereof and pharmaceutical compositions containing them as the active ingredient are disclosed. The D-homopregnanes of the present invention exhibit hormonal activity and are useful for the treatment of inflammation.

Abstract: Compounds of the formula ##STR1## wherein R is hydrogen, ##STR2## R.sub.1 and R.sub.2 are independently selected from hydrogen, lower alkyl, and cycloalkyl or R.sub.1 and R.sub.2 taken together with the nitrogen atom to which they are attached form a ring of the formula ##STR3## N IS 0 OR AN INTEGER FROM 1 TO 3; M IS AN INTEGER FROM 1 TO 3; R.sub.3 and R.sub.4 are independently selected from hydrogen and lower alkyl; X is hydrogen, halogen, lower alkyl, lower alkoxy, or nitro; and their salts; are disclosed. These compounds possess useful antiinflammatory properties.

Abstract: New compounds which have the general formula ##STR1## ARE USEFUL AS HYPOTENSIVE AGENTS.