Abstract: A series of novel 1-(phenethyl) and 1-(2-heteroarylethyl)-3-substituted piperidine derivatives have been prepared, including their pharmaceutically acceptable salts and various novel key intermediates therefor. The 3-substituent present in these compounds is an unsubstituted or substituted diphenylmethoxy group or a diphenylmethoxy-derived group, while the 1-substituent is unsubstituted or substituted phenethyl or 1-(2-heteroarylethyl) wherein the heteroaryl moiety is thienyl, pyridyl or pyrazinyl. These compounds in the form of both their racemates and 3R-isomers, are useful in therapy as smooth muscle muscarinic receptor antagonists and therefore, are of value in the treatment diseases associated with altered motility and/or smooth muscle tone.

Abstract: There is provided a process for the preparation of substituted and unsubstituted-2,3-pyridinedicarboxylate compounds by reacting a dialkyl dichlorosuccinate with a dehydrohalogenating agent, an ammonia source and an appropriately substituted .alpha.,.beta.-unsaturated aldehyde or ketone.

Abstract: Agents against drug-resistant tumor cells comprising a 1,4-dihydropyridine derivative represented by the following formula (I): ##STR1## wherein R.sup.1 is an aryl group which may be substituted;R.sup.2 and R.sup.3, which may be the same or different, each is a member selected from the group consisting of an alkyl group, an alkyloxycarbonyl group, an aryloxycarbonyl group, an aralkyloxycarbonyl group, an aminocarbonyl group, a hydroxycarbonyl group, a formyl group, and a cyano group, each of which may be substituted;R.sup.4 and R.sup.5 is a hydrogen atom or a member selected from the group consisting of a lower alkyl group, a hydroxymethyl group, a cyano group, an amino group, a formyl group, and a halogen atom; andR.sup.

Abstract: In one embodiment this invention provides a process for converting a pyridine-2,3-dicarboxylic acid diester to the corresponding cyclic anhydride directly, without any recovery and purification of the pyridine-2,3-dicarboxylic acid intermediate.An important aspect of the invention process is the utility of pure pyridine-2,3-dicarboxylic acid diester starting matter. A procedure for providing pure diester starting material is demonstrated.

Abstract: The present invention provides a process for extracting pyridine- and quinolinedicarboxylic acids from aqueous media. The pyridine- and quinolinedicarboxylic acids are useful in the preparation of herbicidal 2-(2-imidazolin-2-yl)nicotinate and quinoline-3-carboxylate compounds.

Abstract: Process for the preparation of 5-alkylpyridine-2,3-dicarboxylic esters by reaction of 2-oxosuccinic esters with 2-alkylacrolein oximes.

Abstract: 4-alkyl-1,4-dihyropyridines, with PAF-antagonist activity, of formula (I) wherein R is saturated C.sub.1 -C.sub.4, R' is saturated C.sub.1 -C.sub.6 alkyl which may be interrupted by an oxygen atom, or 2-tetrahydrofurfuryl and R.sup.2 is saturated C.sub.1 -C.sub.4 or phenyl, the compound wherein R is methyl, R' is ethyl and R.sup.2 is phenyl remain excluded, are described.The compounds (I) are prepared by: (a) reaction of (II) with (III); (b) reaction of (IV) with (V); (c) reaction of (VI) with (III) and with (VII); (d) reaction of (VIII) with (V) and with (VII); or (e) reaction of (VIII) with (VI) and with (VII) in the presence of ammonia. The compounds (I) are useful due to their antagonist activity of the platelet activating factor.

Abstract: Compounds are described of the formula: ##STR1## and physiologically acceptable salts thereof, in which R.sub.1 -R.sub.7 are defined hereinafter.The compounds represented by formula (I) reduce intracellular calcium ion concentration by limiting transmembranal calcium ion concentration and thus may be useful for the treatment of cardiovascular disorders such as hypertension.

Abstract: A 1,4-dihydropyridine derivative having the formula (I): ##STR1## wherein X is oxygen atom or nitrogen atom; when X is oxygen atom, R.sup.1 is hydrogen atom, a lower alkyl group, a lower cycloalkyl group, a lower alkenyl group or magnesium atom, when X is nitrogen atom, X-R.sup.1 group is NH.sub.2, NHR.sup.1', NR.sup.1' R.sup.1" or ##STR2## in which R.sup.1' is a lower alkyl group or a lower alkoxyalkyl group, R.sup.1" is a lower alkyl group and n is an integer of 2 to 6; R.sup.2 is a lower alkyl group, a lower cycloalkyl group or a lower alkoxyalkyl group and R.sup.3 is a lower alkyl group, formyl group, dimethoxymethyl group, cyano group or amino group, when X is oxygen atom and R.sup.1 is hydrogen atom or magnesium atom, R.sup.3 is methyl group, when X is nitrogen atom, R.sup.3 is methyl group, or a pharmaceutically acceptable salt thereof, some processes for preparing the same and a pharmaceutical composition containing the same.

Abstract: A process for producing a carboxylic acid amide or ester, which comprises reacting an organic chloride having at least one chlorine atom on its ring of a substituted or unsubstituted, aromatic or heterocyclic hydrocarbon with carbon monoxide and an amine or an alcohol in the presence of a base by using as catalysts a palladium compound and a phosphine compound represented by the general formula (V):(R).sub.2 P--X--P(R).sub.2 (V)wherein R is an alkyl group or a substituted or unsubstituted phenyl group, and X is an alkylene group having 1 to 6 carbon atoms ##STR1## or a binaphthyl group.

Abstract: Processes for production of 2,6-substituted-3,5-pyridinedicarboxylic acids, esters, salts, amides, halides, and cyano compounds, useful as herbicides and as intermediates which provide herbicides.

Abstract: Cardioactive dihydropyridines of the formula ##STR1## in which Y is ##STR2## A is H or CH.sub.3, B is --NH, --NH--CO--, --NH--CS--, --NH--COO--, --NH--SO.sub.2 --or --NH--CO--NH-- or --NH--CS--NH--, andR.sup.13 and R.sup.14 each independently is H or an organic radical,and salts thereof. The Y can be hydrolyzed off. The other radicals on the dihydropyridine moiety can also be varied.

Abstract: The invention is directed to processes for the preparation of dimethyl-1,4-dihydro-2,6-dimethyl-4-(2'-nitrophenyl)-pyridine-3,5-dicarbox ylate by reacting 1-methoxy-1-(2'-nitrophenyl)-N-(2'-nitrophenyl)methylene methanamie or 1-(2'-nitrophenyl)-N,N'-bis-(2'-nitrophenyl) methylene methanediamine with methyl acetoacetate in the presence of an amine compound or by reacting the monomeric or trimeric from of 2-nitrobenzaldimine with methyl acetoacetate.

Abstract: Novel dihydropyridine compounds bearing substituted piperidyl substituents are effective heat/light stabilizers for a wide variety of polymer substrates, e.g., for halopolymers such as PVC, and are also effective anti-UV agents and antioxidants for such polymers as polyolefins, polystyrenes, polyalkadienes, polyurethanes, polyamides, polyesters, polycarbonates, polysulfones, polyethersulfones, polyetherketones, acrylic polymers, or copolymers or mixtures thereof.

Abstract: There is provided a process for the preparation of a substituted or unsubstituted 2,3-pyridine or quinolinedicarboxylic acid by hydrolysis of a substituted or unsubstituted 2,3-pyridine or quinolinedicarboxylic acid diester with an acid having an ionization constant pK.sub.a of less than 3.0 followed by isolation of the product as the free acid or an acid salt.

Abstract: O-substituted hydroxylamines (I)H.sub.2 N--O--CH.sub.2 --R(I)where R is H or an organic radical, and their salts are prepared by reacting a cyclic imidoether II of a 1,4- or 1,5-dicarboxylic acid, the said imidoether containing an ether group --O--CH.sub.2 --R, with a basic compound by a method in which a primary aliphatic aminoalcohol III is used as the basic compound and the compound I is, if required, converted to its salts.

Abstract: There is provided a process for the preparation of dialkyl pyridinedicarboxylate compounds and derivatives thereof by reacting a dialkyl chloromaleate or chlorofumarate or a mixture thereof with an ammonium salt optionally in the presence of ammonia and an appropiately substituted .alpha.,.beta.-unsaturated aldehyde or ketone.

Abstract: Described herein is a process for preparation of substituted pyridine dicarboxylate compounds.

Abstract: A process for dehydrofluorination of a 2,6-(bis)trifluoromethyl-dihydropyridine-3,5-dicarbothioic acid ester.

Abstract: A process for dehydrofluorination of a 2,6-(bis) trifluoromethyl-dihydropyridine-3,5-dicarbothioic acid ester.

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.The compounds represented by formula (I) reduce intracellular calcium ion concentration by limiting transmembranal calcium ion reflux and thus may be useful for the treatment of cardiovascular disorders such as hypertension.

Abstract: The present invention relates to 1,4-dihydropyridine of the formula(I) ##STR1## wherein R.sup.1 represents a phenyl group which may be substituted by one or two substituents selected from halogeno, nitro, trifluoromethyl and difluoromethoxy group, or 2,1,3-benzoxadiazole-4-yl group, R.sup.2 represents a lower alkyl or phenyl group, R.sup.3 represents a lower alkyl group and Y represents an oxygen or sulfur atom.The compounds of the formula(I) can be employed for treatment or prevention of cardiovascular diseases.

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 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: 1,4-dihydropyridines of formula I ##STR1## wherein X is --CO.sub.2 R.sub.1, cyano, nitro, --COCH.sub.3 ; each of R and R.sub.1, which are the same or different, is a primary, secondary or tertiary, saturated or unsaturated, linear or branched C.sub.1 -C.sub.6 alkyl group optionally substituted by one or more hydroxy, C.sub.1 -C.sub.7 -monoalkylamino, di-C.sub.1 -C.sub.7 -alkylamino, benzylamino, C.sub.1 -C.sub.6 -alkoxy, phenoxy groups which are optionally substituted; R.sub.2 is hydrogen; R.sub.3 is hydrogen or hydroxy, --OCOR.sub.5, OSO.sub.2 R.sub.6, azide, amino, --NHPO(OR.sub.7).sub.2, --NHCOR.sub.5, C.sub.1 -C.sub.4 -alkoxy or fluorine, chlorine, bromine or iodine, SH, SCOR.sub.6 or C.sub.1 -C.sub.6 -alkylthio, phenylthio or benzylthio; R.sub.4 is an optionally substituted aromatic or an optionally substituted 5- or 6-membered heteroaromatic group; Y is one or more substituents, which may be the same or different, selected from C.sub.1 -C.sub.4 -alkoxy, halogen, nitro, cyano, C.sub.1 -C.sub.

Abstract: Described herein is a process for preparation of substituted pyridine dicarboxylate compounds.

Abstract: The invention concerns compounds of formula ##STR1## or salts thereof; wherein Ar is an optionally substituted aryl radical;R represents hydrogen or an optionally substituted alkyl or aralkyl group;R.sup.1 and R.sup.2 are the same or different and are selected from hydrogen and saturated or unsaturated, cyclic or acyclic aliphatic hydrocarbon residues optionally substituted by one or more groups selected from halogen, OH, carboxy, CN, alkoxy, alkylthio, aryloxy, alkoxycarbonyl, amino, substituted amino, and optionally substituted aryl;A represents a group of formula --XR.sup.3 whereinX is (i) a group of formula --(CHR.sup.6).sub.p --Y--(CHR.sup.7).sub.q --or (ii) a group of formula --(CHR.sup.6).sub.r --O--(CHR.sup.7).sub.qin which formulae: Y represents --S--, NR.sup.8 or a direct bond, p and q each represent 0, 1 or 2 providing that p and q do not both represent 0, 1 or 2 and the other is zero; R.sup.6, R.sup.7 and R.sup.8 independently represent hydrogen or lower alkyl, and R.sup.

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: Hypertension and cardiac insufficiency can be controlled by 4-nitrophenyl-dihydropyridine amides of the formula ##STR1## in which X can be ethylene or the like,Y is pyridyl or --NR.sup.9 R.sup.10, andR.sup.9 and R.sup.10 each independently is hydrogenor an organic group, or together form a ring, and physiologically tolerated salts thereof. Compounds in which R.sup.5 and R.sup.6 are not aryl or aralkyl are new.

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 represents a group ##STR2## (where A is a bond or a methylene group and R.sub.7 is phenyl C.sub.1-4 alkyl; or R.sub.2 represents a group CH.sub.2 CH.sub.2 NR.sub.8 R.sub.9 (where R.sub.8 is hydrogen or C.sub.1-4 alkyl and R.sub.9 is C.sub.1-4 alkyl, phenyl C.sub.1-4 alkyl or benzoyl C.sub.1-4 alkyl); or R.sub.2 represents a C.sub.1-4 alkyl group substituted by nitrile.R.sub.3 represents a C.sub.1-6 straight or brached 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.

Abstract: Compounds of formula I, and pharmaceutical compositions containing compounds of formula I ##STR1## wherein: R.sub.1 is:(a) COCH.sub.3, COC.sub.6 H.sub.5, CN or NO.sub.2 ;(b) COORa wherein Ra is hydrogen, or optionally substituted C.sub.1 -C.sub.6 straight or branched alkyl;R.sub.2 is optionally substituted phenyl; pentafluorophenyl; .alpha.- or .beta.-naphthyl; a five- or six-membered heterocyclic ring; .alpha.-benzo[2,3-b]-1,4-dioxan-.alpha.-yl; or .alpha.-benzofuroxanyl;R.sub.3 is COORa;P is hydrogen, --(CH.sub.2).sub.p --W, or C.sub.1 -C.sub.8 linear or branched alkyl;N--P.sub.1 is the residue of a primary or secondary amino group wherein P.sub.1 is hydrogen, C.sub.1 -C.sub.6 lower linear or branched alkyl group, or --(CH.sub.2).sub.p --W; and P, taken together with P.sub.1 and the nitrogen atom to which P.sub.1 is linked, may form a pyrrolidine or a piperidine ring; W is hydroxymethyl, formyloxymethyl, CO.sub.2 R wherein R is hydrogen or C.sub.1 -C.sub.

Abstract: A 1,4-dihydropyridine derivative represented by the formula ##STR1## wherein X is a hydrogen atom or an alkoxy group having 1 to 4 carbon atoms, A and B are the same or different and are each an alkylene group having 1 to 4 carbon atoms, and a pharmaceutically acceptable salt thereof are useful as the preventive and therapeutical agents of ischemic heart disease and hypertension.

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.

Abstract: Novel 1,4-dihydropyridine derivatives and salts thereof are provided, which can be represented by the formula ##STR1## wherein, Y represents an oxygen atom or a sulfur atom; A represents an alkylene group, an alkenylene group or an alkynylene group; and R.sup.7 and R.sup.8 can represent individual groups or may be combined together with a nitrogen atom(s) to form a pyrrole ring, a piperidine ring, a morpholine ring or a piperazine ring or azepine ring which may be substituted with a lower alkyl group or an aralkyl group. Pharmaceutical compositions containing the derivatives and their use for imparting calcium antagonistic activity are also provided.

Abstract: Polymer matrices, e.g., halogenated polymers such as PVC, polyolefins, polystyrenes, polyalkadiences, etc., are stabilized against the adverse effects of heat and light, by incorporating therein an effective stabilizing amount of a compound of the formula (I): ##STR1## in which n is a number ranging from 1 to 3, and R is a methyl radical or a hydrogen atom.

Abstract: Dihydropyridine derivatives and salts thereof represented by the general formula, ##STR1## which possess excellent calcium antagonist effect, hypotensive effect, platelets aggregation inhibitory effect, phosphodiesterase inhibitory effect, calmodulin inhibitory effect and peroxidized lipid lowering effect, and thus dihydropyridine derivatives and salts thereof are useful as a coronary blood flow improving agent such as coronary vasodilator, hypotensive agent, prophylaxis and treating agents for thrombosis, phophodiesterase inhibitory agent, peroxidized lipid metabolism lowering agent, anti-inflammatory agent and others.

Abstract: The invention relates to new compounds of formula I: ##STR1## in which Ar represents a phenyl radical having one to five identical or different substituents selected from chloro or fluoro,Y, Z, Y.sub.1 and Z.sub.1, which may be identical or different, each represents a hydrogen atom, a straight-chain or branched lower alkyl radical containing 1 to 4 carbon atoms, a cyclopropyl radical, a dicyclopropylmethyl radical, a 2,2-dicyclopropylethyl radical, a 2,2-dicyclopropylethenyl radical, a 3,3-dicyclopropylpropyl radical, a 3,3-dicyclopropyl-1-propenyl radical, a straight-chain or branched alkenyl radical containing 2 to 5 carbon atoms or a phenyl radical substituted with a nitro radical,W represents a straight-chain or branched lower alkyl radical containing 1 to 4 carbon atoms,V represents an oxygen atom,U represents a methyleneoxy radical or an ethyleneoxy radical,m and n, which may be identical or different, each represents an integer which may take a value from 2 to 4, inclusive, R.sub.1 and R.sub.

Abstract: Compounds of formula I ##STR1## wherein R.sub.1 is an alkoxycarbonyl group, acetyl, benzoyl, cyano, nitro or aminocarbonyl;R.sub.2 is an optionally substituted aryl or hetaryl group;R.sub.3 is an alkoxycarbonyl group;.phi. is a thio residue such as alkylthio, cycloalkylthio, arylthio, heteroarylthio, aminoalkylthio,are described.Compounds I are useful in human therapy as antihypertensive, antiulcer, antithrombotic, antiischaemic agents.

Abstract: Cardioactive dihydropyridines of the formula ##STR1## in which Y is ##STR2## A is H or CH.sub.3, B is --NH, --NH--CO--, --NH--CS--, --NH--COO--, --NH--SO.sub.2 --or --NH--CO--NH-- or --NH--CS--NH--, andR.sup.13 and R.sup.14 each independently is H or an organic radical,and salts thereof. The Y can be hydrolyzed off. The other radicals on the dihydropyridine moiety can also be varied.

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 which may be interrupted by an oxygen atom;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 substitutent;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 new process has been found for the preparation of substituted 2-chloropyridine derivatives of the formula (I) ##STR1## wherein R.sup.1 to R.sup.4 have the meanings as defined in the description.The new process is characterized in that pyridine 1-oxides of the formula II ##STR2## are reacted with a chlorine-containing phosphoric acid derivative from the series of the chlorophosphoric esters and chlorophosphoramides in the presence of an inert organic solvent and in the presence of an acid acceptor at temperatures between -20.degree. C. and 200.degree. C., and the resulting product is separated further, if appropriate.Compound (I) is known as an intermediate product for medicaments (cf.DE-A 2,812,585) or for insecticidel nitromethylene derivatives (cf. EP-A 163,855).

Abstract: Fungicidal compounds of the formula (I): ##STR1## and stereoisomers thereof, wherein K is oxygen or sulphur; Z is optionally substituted aryl or optionally substituted heteroaryl; X is O, S(O).sub.n, NR.sup.4, CR.sup.1 R.sup.2, CHR.sup.5, CO, CR.sup.1 (OR.sup.2), C.dbd.CR.sup.1 R.sup.2, CHR.sup.1 CHR.sup.2, CR.sup.1 .dbd.CR.sup.2, CHR.sup.1 CR.sup.2 .dbd.CH, C.dbd.C, OCHR.sup.1, CHR.sup.1 O, OCHR.sup.1 O, S(O).sub.n CHR.sup.1, S(O).sub.n CHR.sup.1 O, CHR.sup.1 S(O).sub.n, CHR.sup.1 OSO.sub.2, NR.sup.4 CHR.sup.1, CHR.sup.1 NR.sup.4, CO.sub.2, O.sub.2 C, SO.sub.2 O, OSO.sub.2, CO.CO, COCHR.sup.1, COCHR.sup.1 O, CHR.sup.1 CO, CHOH.CHR.sup.1, CHR.sup.1.CHOH, ##STR2## CONR.sup.4, OCONR.sup.4, NR.sup.4 CO, CSNR.sup.4, OCS.NR.sup.4, SCO.NR.sup.4, NR.sup.4 CO.sub.2, NR.sup.4 CS, NR.sup.4 CSO, NR.sup.4 COS, NR.sup.4 CONR.sup.4, S(O).sub.n NR.sup.4, NR.sup.4 S(O).sub.n, CS.sub.2, S.sub.2 C, CO.S, SCO, N.dbd.N, N.dbd.CR.sup.1, CR.sup.1 .dbd.N, CHR.sup.1 CHR.sup.2 CH(OH), CHR.sup.1 OCO, CHR.sup.1 SCO, CHR.sup.1 NR.sup.

Abstract: Compounds of formula I ##STR1## wherein R.sub.1 is an alkoxycarbonyl group, acetyl, benzoyl, cyano, nitro or aminocarbonyl;R.sub.2 is an optionally substituted aryl or hetaryl group;R.sub.3 is an alkoxycarbonyl group;.phi. is a thio residue such as alkylthio, cycloalkylthio, arylthio, heteroarylthio, aminoalkylthio,are described.Compounds I are useful in human therapy as antihypertensive, antiulcer, antithrombotic, antiischaemic agents.

Abstract: A pyridine-compound is reacted with fluorine together with a Bronsted acid-compound or Lewis acid to form a N-fluoropyridinium salt which is very active to other compounds but is very selective for the preparation of a desired product and this product is very useful for a fluorine-introducing agent which makes it useful for the preparation of fluoro-compounds such as thyroid inhibitor.

Abstract: A series of compounds useful in treating cardiovascular disorders due to the combined expression of both .beta.-block and calcium-block activity by these agents. This useful combination of actions is effected by a novel combination of structural subunits forming these compounds. Essentially, .beta.-blocking aryloxypropanolamine moieties are attached via their aryl ring or amino nitrogen at one of the carboxylate groups of calcium-blocking 4-aryl-1,4-dihydropyridine-3,5-dicarboxylates. These compounds are prepared from new 4-aryl-1,4-dihydropyridine intermediate compounds.

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: Compounds of formula I ##STR1## wherein R.sub.1 is a cyano, nitro, acetyl, benzoyl or alkoxycarbonyl group;R.sub.2 is an optionally substituted phenyl or heteroaryl group;R.sub.3 is an alkoxycarbonyl group;R.sub.4 is an alkyl group, optionally substituted by hydroxy, amino, phenyl, heterocyclic group; an optionally substituted phenyl group or an heterocyclic group.Compounds I are useful in human therapy as agents able to interact with CA.sup.++ -dependent systems and as anti-tumor agents.

Abstract: The invention relates to a process for producing new compounds of formula I: ##STR1## and isomers thereof, as well as acid addition salts thereof, in which the symbols have the meanings set forth in the specification.

Abstract: Compounds of formula I ##STR1## wherein R.sub.1 is a cyano, nitro, benzoyl, acetyl, amido or alkoxycarbonyl group;R.sub.2 is substituted aryl- or heterocyclic residue;R.sub.3 is alkoxycarbonyl group;R.sub.4 and R.sub.5, being the same or different, are hydrogen, alkyl, aryl or heterocyclic groups;Y is oxygen, sulphur or substituted or unsubstituted nitrogen atom, that can be a part of a heterocyclic ring;n is 0, 1 or 2R6 and R.sub.10, that can be the same or different, are: hydrogen; C.sub.1 -C.sub.6 -alkyl optionally substituted by hydroxy, amino, monoalkyl and dialkylamino, C.sub.1 -C.sub.6 -alkoxy, C.sub.1 -C.sub.6 -alkoxycarbonyl, C.sub.1 -C.sub.3 -carbonyloxy, aryl, heteroaryl and cycloalkyl; a C.sub.1 -C.sub.12 -alkanoyl, aroyl or heteroaryl group optionally substituted by halogen, nitro, amino monoalkylamino, dialkylamino, hydroxy, C.sub.1 -C.sub.6 -alkoxy, C.sub.1 -C.sub.6 -alkoxycarbonyl, C.sub.1 -C.sub.6 -alkylthio, C.sub.1 -C.sub.3 -carbonyloxy, aryl, heteroaryl, cycloalkyl groups.

Abstract: A process for the preparation of optically active 3-de-methylmevalonic acid derivatives, and intermediates A process for the preparation of optically active 3-de-methylmevalonic acid derivatives of the formula I ##STR1## (3,5-dihydroxy carboxylic acid derivatives) or of the formula II ##STR2## (.beta.-hydroxy lactones) in which R, R.sup.1 and Y have the indicated meanings, is described. The invention furthermore relates to aldehydes of the formula XII ##STR3## in which M represents the indicated protective groups. The 3-demethylmevalonic acid derivatives of this invention are useful for lowering cholesterol levels of a host.