Abstract: 7-Substituted lower alkyl hept-6-enoates and 4-hydroxytetrahydropyran-2-ones bearing 6-olefinic substituents (e.g.,) ethyl erythro-3,5-dihydroxy-7-phenyl-hept-6-enoates are prepared by a multi-step process. The process involves 3-protected-lower alkyl 3,5-dihydroxy-hept-6-enoates, which are obtained by cleaving corresponding 6.alpha.-vinyl-4.beta.-protected hydroxy-tetrahydro 2H-pyran-2-ones. The final products are useful as anti hypercholesteremic agents.

Abstract: Process for preparing alkanoic acid or their esters by rearrangement of alpha-halo-ketones in protic medium and in the presence of a non-noble metal salt.The protic medium is preferably an aliphatic alcohol having low molecular weight or water and the reaction is carried out at a temperature from 0.degree. C. to the boiling-point of the diluent or of the diluents mixture.

Abstract: A method for the production of an .alpha.-aryl-alkanoic acid represented by the general formula II: ##STR1## wherein R.sup.3 stands for a hydrogen atom or an alkyl group and Ar for an aromatic residue, characterized by subjecting an .alpha.-haloalkyl-aryl ketal represented by the general formula I: ##STR2## wherein Ar has the same meaning as defined above, R.sup.1 and R.sup.2 independently stand for an alkyl group and embrace the case wherein they jointly form a cyclic acetal, R.sup.3 has the same meaning as defined above, and X stands for a halogen atom to a rearrangement reaction in the presence of at least one zinc compound selected from the group consisting of oxide, hydroxide, sulfide, carbonate, and basic carbonate of zinc and subsequently hydrolyzing the product of said rearrangement reaction.

Abstract: A compound of the formula ##STR1## and intermediates useful in preparing same.

Abstract: New interphenylene prostaglandin (PGH) analogs are prepared by a method which involves reacting a bicyclic olefin, an acetylene compound and a benzylic halide together, in the presence of a palladium(O) catalyst in a single-step synthesis. By this technique a large number of new interphenylene PGH analogs can be prepared, which are useful as inhibitors of arachidonic acid induced platelet aggregation.

Abstract: Certain 6-(substituted-naphthyl)hydrocarbyl-4-hydroxytetrahydropyran-2-ones are unexpectedly potent in the treatment of familial hypercholesterolemia, hyperlipemia and atherosclerosis by virtue of their ability to inhibit the enzyme, 3-hydroxy-3-methylglutaryl-coenzyme A reductase (HMG-CoA reductase).

Abstract: .alpha.-Arylalkanoic acids or esters, orthoesters or amides thereof are prepared by forming an .alpha.-hydroxy ketal or thioketal of an aryl alkyl ketone, activating the .alpha.-hydroxy substituent with an esterifying agent to form the corresponding ketal or thioketal ester substrate, wherein the ester group is sufficiently labile to non-catalytically disassociate from the substrate in a protic or dipolar, aprotic solvent, maintaining the ester substrate in contact with the protic or dipolar, aprotic solvent or mixtures thereof for a time sufficient to form the corresponding .alpha.-arylakanoic acid or ester, orthoester or amide thereof, and optionally concomitantly or sequentially hydrolyzing any ester, orthoester or amide formed to the corresponding .alpha.-arylalkanoic acid.

Abstract: Bicycloheptane substituted ether prostaglandin analogs are provided having the structural formula ##STR1## wherein X is O or ##STR2## and including all stereoisomers thereof. The compounds are cardiovascular agents useful, for example, in the treatment of thrombotic disease.

Abstract: A process is described for the preparation of alpha-hydroxyl-alkanoic acids of formula ##STR1## which are known anti-inflammatory agents or intermediates for known pharmaceutical products. The process consists essentially in the rearrangement of phenolates of formula ##STR2## wherein Ar is an unsubstituted or substituted phenyl or naphthyl, in aqueous environment or in an organic medium, at temperatures comprised within the range of from 0.degree. to 100.degree. C. and within short times, followed by either acid or alkaline hydrolysis.

Abstract: The invention relates to new 2,3,4-trinor-1,5-inter-m-phenylene-PGI.sub.2 derivatives of the formula (I) ##STR1## wherein A stands for carboxy, cyano, tetrazolyl or --COOR.sup.3 or --CONR.sup.1 R.sup.2 ;R.sup.3 is C.sub.1-4 alkyl or an equivalent of a pharmacologically acceptable cation:R.sup.1 and R.sup.2 each stands for hydrogen, phenyl; C.sub.1-5 alkyl, optionally substituted by carboxy, hydroxy, phenyl or C.sub.2-5 alkoxycarbonyl; or C.sub.1-4 alkylsulfonyl; orR.sup.1 and R.sup.2 together form an .alpha.,.omega.-alkylene chain containing 3-6 carbon atoms;B stands for oxygen or methylene;Y is optionally bromo-substituted vinylene or a --C.tbd.C-- group:R.sup.4 stands for hydrogen or tetrahydro-pyran-2-yl;R.sup.5 represents an alkyl group containing 5-9 carbon atoms, which can be optionally interrupted by one or more oxygen atom(s) or --CH.dbd.CH-- or --C.tbd.

Abstract: Novel compounds of the following general formula: ##STR1##

Abstract: An improved process for the resolution of (+)-6-methoxy-.alpha.-methyl-2-naphthaleneacetic acid into the corresponding enantiomers by using L-threo-(+)-2-amino-1-(4-nitrophenyl)-1,3-propanediol and L-threo-(+)-2-amino-1-(4-methylmercaptophenyl)-1,3-propanediol.

Abstract: The invention relates to a process for the resolution of mixtures of D and L-6-methoxy-alpha-methyl-2-naphthaleneacetic acid in their respective antipodes.L-threo(+)-2-amino-1-p-nitrophenyl-1,3-propandiol is proposed as new resolving agent.

Abstract: Alpha-alkyl-alkanoic acids are prepared by heating at boiling temperature a mixture of an alpha-halogen-alkyl-arylketone in a saturated aliphatic diol or in a mixture of saturated aliphatic diols in the presence of a Broensted's acid and by successively alkalifying the reaction mixture.

Abstract: This invention relates to a process for preparing an alpha-arylalkanoic acid or salt thereof which comprises the rearrangement of an alpha-halo-alkylarylketal in neutral or slightly alkaline conditions, in the presence of a dipolar aprotic diluent and of a protic substance having a high dielectric constant, and the subsequent hydrolysis of the thus obtained ester.

Abstract: A process for preparing d-.alpha.-(6-methoxy-2-naphthyl)propionic acid, which comprises hydrolyzing an ester of d-.alpha.-(6-methoxy-2-naphthyl)propionic acid in an aqueous solution containing a basic catalyst.

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: Process for preparing an arylalkanoic acid by adding iodine to a mixture of an arylalkanone and an excess of an orthoester, heating of the mixture thus obtained, adding an inorganic base and finally an acid.

Abstract: Provided is a process for preparing a diaryl or a mixture of diaryls represented by any or a combination of the following formulae (II), (III) and (V), characterized in that a diaryliodonium salt represented by the following formula (I) is reacted in a solvent in the presence of a transition metal catalyst and a reducing metal at a temperature in the range of room temperature to 100.degree. C.:[Ar.sub.1 -I.sup..sym. -Ar.sub.2 ]X.sup..crclbar. (I)Ar.sub.1 -Ar.sub.1 (II)Ar.sub.1 -Ar.sub.2 (III)Ar.sub.2 -Ar.sub.2 (IV)wherein Ar.sub.1 and Ar.sub.2, which may be alike or different, are each an aryl group which may have a substituent group or groups and X.sup..crclbar. is a counter ion which is inert to said reaction.

Abstract: Pharmaceutically useful optically active .alpha.-arylalkanoic acids or esters, ortho esters, or amides thereof are stereoselectively prepared by contacting an aryl magnesium Grignard reagent with an optically active .alpha.-substituted acyl halide to form the optically active aryl .alpha.-substituted alkyl ketone, which is ketalized and rearranged to the desired optically active .alpha.-arylalkanoic acid or the corresponding ester, ortho ester or amide. In an alternate embodiment, the aryl .alpha.-substituted alkyl ketone is reduced to the corresponding alkanol, which is rearranged to the .alpha.-arylalkanal. The alkanal so produced is converted to the desired optically active .alpha.-arylalkanoic acid by conventional methods.

Abstract: An aromatic ionomeric copolymer having arylether and arylsulfone linkages has been prepared by condensation of both:(a) The alkali metal bisphenate salts of 9,9-bis(4-hydroxyphenyl-fluoren-4-carboxylic acid, optionally with up to 99 mol percent of another dihydric phenol based on the combined bisphenates in the mixture;and(b) dihalodiphenylsulfones where the halogen is selected from chlorine or fluorine.The copolymers are useful inter alia as ion exchange materials and permselective membranes.A process of preparing and purifying the carboxylic acid containing bisphenol monomer is described.

Abstract: Compounds of the formula ##STR1## wherein R is hydrogen or lower alkyl, X is hydrogen or halogen, and A is the group ##STR2## wherein R.sub.1 is hydrogen, acyl or lower alkyl, R.sub.2 is hydrogen or lower alkyl, m is an integer from 2 to 4, n is an integer from 1 to 3, and t is an integer from 1 to 5, provided that R.sub.1 is adjacent to --(CH.sub.2).sub.m --O(CH.sub.2).sub.m ].sub.n O--, and, when R.sub.2 is hydrogen, salts thereof with pharmaceutically acceptable bases, are described. The compounds of formula I are useful as agents for the treatment of allergic conditions.

Abstract: Novel compounds of the following general formula: ##STR1##

Abstract: A process is disclosed for the preparation of optically active alpha-arylalkanoic acids, consisting in the rearrangement of optically active alpha-(haloalkyl)-aryl-ketals and in submitting to hydrolysis the so-obtained esters of alpha-arylalkanoic acids.The rearrangement reaction is carried out under neutral or slightly alkaline conditions in a polar protic medium.

Abstract: A process is disclosed for the preparation of optically active alpha-arylalkanoic acids, consisting in the rearrangement of optically active (alpha-haloalkyl)-aryl-ketals and in submitting to hydrolysis the thus obtained esters of alpha-arylalkanoic acids. The rearrangement reaction is carried out under neutral or alightly alkaline conditions, in an aprotic dipolar diluent and in the presence of a protic substance having a high dielectric constant.

Abstract: This invention relates to a method of synthesis of certain substituted carboxylic acids useful in lowering serum triglyceride and total cholesterol levels in mammals (including man) represented by the general formula I:Ar.sup.1 --Ar.sup.2 (I)whereinAr.sup.1 is selected from ##STR1## Ar.sup.2 is selected from ##STR2## and R is selected from C.sub.1-5 alkyl, halogen, perhalo-C.sub.1-4 alkyl, C.sub.1-4 alkoxy, phenyl, C.sub.1-4 acyl, C.sub.1-6 alkoxycarbonyl, amino or hydroxy.

Abstract: Process for preparing esters of 2-(6'-methoxy-2'-naphthyl)-propionic acids via rearrangement of ketals of 2-iodo-1-(6'-methoxy-2'-naphthyl)-propan-1-one in a protic medium.

Abstract: Naphthalenyloxy carboxylic acids of the formula ##STR1## wherein X, R, m and n are as hereinafter set forth, are described. The compounds of formula I are antagonists of slow reacting substance of anaphylaxis (SRS-A), which renders them useful as agents for the treatment of allergic conditions.

Abstract: Process for the optical resolution of (.+-.)2-(6'methoxy-2'-naphthyl)-propionic acid by adding from 0.45 to 0.65 mole of (S)-alpha-phenylethylamine to each mole of said acid in chloroform.

Abstract: The compound 15-cyclohexyl-9-deoxy-13,14-dihydro-2',9.alpha.-methano-3-oxa-4,5,6,16,17, 18,19,20-octanor-3,7(1',3-interphenylene)PGF.sub.1 and pharmacologically acceptable salts thereof.

Abstract: .alpha.-Arylalkanoic acids or esters, orthoesters or amides thereof are prepared by forming an .alpha.-hydroxy ketal or thioketal of an aryl alkyl ketone, activating the .alpha.-hydroxy substituent with an esterifying agent to form the corresponding ketal or thioketal ester substrate, wherein the ester group is sufficiently labile to non-catalytically disassociate from the substrate in a protic or dipolar, aprotic solvent, maintaining the ester substrate in contact with the protic or dipolar, aprotic solvent or mixtures thereof for a time sufficient to form the corresponding .alpha.-arylakanoic acid or ester, orthoester or amide thereof, and optionally concomitantly or sequentially hydrolyzing any ester, orthoester or amide formed to the corresponding .alpha.-arylalkanoic acid.

Abstract: Compounds of the formula ##STR1## wherein R is hydrogen or lower alkyl, X is hydrogen or halogen, and A is the group ##STR2## wherein R.sub.1 is hydrogen, acyl or lower alkyl, R.sub.2 is hydrogen or lower alkyl, m is an integer from 2 to 4, n is an integer from 1 to 3, and t is an integer from 1 to 5, provided that R.sub.1 is adjacent to --(CH.sub.2).sub.m [O(CH.sub.2).sub.m ].sub.n O--, and, when R.sub.2 is hydrogen, salts thereof with pharmaceutically acceptable bases, are described. The compounds of formula I are useful as agents for the treatment of allergic conditions.

Abstract: Rearrangement of alpha-halo-alkylarylketals in neutral or weakly alkaline conditions and in the presence of a polar-protic medium and subsequent hydrolysis of the thus obtained esters, in the same reaction medium, to afford the corresponding alpha-arylalkanoic acids or their salts which are particularly useful as anti-inflammatory, analgesic and antipyretic agents.

Abstract: Novel compounds of the following general formula: ##STR1##

Abstract: The present specification provides novel analogs of carbacyclin (CBA.sub.2), 6a-carba-prostacyclin (6a-carba-PGI.sub.2), which have pronounced prostacyclin-like pharmacological activity, e.g., as platelet anti-aggregatory agents. Specifically the novel chemical analogs of CBA.sub.2 are those substituted by fluoro (C-5), alkyl (C-9), interphenylene (C-5), methano (C-6a,9), and an additional (olefinic) valence bond (C-6a,9). Further provided are benzindene analogs of CBA.sub.2 and substituted forms thereof, i.e., 9-deoxy-2', 9-methano (or 2', 9-methano)-3-oxa-4,5,6-trinor-3,7-(1',3'-interphenylene)-PGF.sub.1 compounds. Also provided are a variety of novel chemical intermediates, e.g., substituted bicyclo[3.3.0]octane intermediates, and chemical process utilizing such intermediates which are useful in the preparation of the novel CBA.sub.2 analogs.

Abstract: There is presented a process for the manufacture of hexahydronaphthacene derivatives of the general formula ##STR1## wherein one of R.sup.1 and R.sup.2 represents a hydrogen atom and the other represents a hydrogen atom or a hydroxy group of R.sup.1 and R.sup.2 together represent a protected oxo group, R.sup.3 represents a hydrogen atom or a hydroxy or acyloxy group and R.sup.4 represents a lower alkyl or esterified carboxy group or a group of the formula ##STR2## wherein R.sup.5 and R.sup.6 together form an oxo group or a protected oxo group and X represents a hydrogen atom or a hydroxy or acyloxy group or ##STR3## in which n stands for 1 or 2 and Y represents a hydrogen atom or an alkyl or acyl group.Also presented are certain of the novel derivatives per se and various novel intermediates in the process.

Abstract: There are described compounds of formula I, ##STR1## in which Ra, Rb, Rc, Rd, Re, Rf and Rg, which may be the same or different, each represent hydrogen, amino, hydroxy, alkoxy, alkenyloxy, halogen, acyl, alkenyl, alkyl, or alkoxy substituted by phenyl,Rh is hydrogen, alkyl or --COOH.X is a hydrocarbon chain containing from 2 to 10 carbon atoms and optionally substituted by a hydroxy group,A has no significance or represents Y, OY, or SY and Y represents a C 1 to 4 hydrocarbon chain which is optionally substituted by alkyl C 1 to 4,E and G, which may be the same or different, each represent --O--, --S-- or --CH.sub.2 --, provided that at least one of E and G is --O-- or --S--,L, together with the carbon atoms to which it is attached, forms a benzene, furan, thiophene, pyrrole, or pyran-2-one ring,and pharmaceutically acceptable derivatives thereof.

Abstract: Cis-bicyclo[3.3.0]octane derivatives corresponding to the formula ##STR1## wherein R.sub.1 is hydrogen, a lower alkyl group or a cation and wherein R.sub.2 represents a cyclohexyl or an adamantyl group. In these compounds the phenyl radical may be arranged with respect to the double bond in the EZ- or in the E-configuration and at the carbon atom bearing the group R.sub.2 the molecule may have the RS- or S-configuration. The compounds are prepared by reacting compounds of the formulae ##STR2## wherein R.sub.1 and R.sub.2 have the same meaning as above and R.sub.6 represents hydrogen or a protecting group. Medicaments containing these compounds act as inhibitors of blood platelet aggregation and (in higher doses) as blood pressure lowering agents.

Abstract: Process for preparing esters of aryl alkanoic acids via oxidation of the corresponding ketones with bromine or iodine in the presence of a metal halide and an alcohol.The thus obtained esters are then easily hydrolized to give the corresponding aryl alkanoic acids which are particularly useful as anti-inflammatory, analgesic and anti-pyretic agents.

Abstract: (+)-6-methoxy-.alpha.-methyl-2-naphthalene acetate of N,N"-bis (4-chlorophenyl)-3,12-diimino-2,4,11,13-tetraazatetradecan-diimidoamide, possessing the formula (I) ##STR1## has high bioavailability by the cutaneous route which enables it to be used topically for the treatment of dermatoses, infected wounds, scalds, bedsores, inflammations of the oral cavity, vulvovaginitis, etc.

Abstract: A compound of the formula ##STR1## wherein X.sup.1 is a free or esterified carboxyl group, a hydroxymethyl group, a cyano group, a group of the formula: ##STR2## (R.sup.a and R.sup.b are each independently a hydrogen atom, a C.sub.1 -C.sub.4 alkyl group, a C.sub.3 -C.sub.7 cycloalkyl group, a benzyl group, a phenyl group, a phenyl group substituted with a halogen atom or a C.sub.1 -C.sub.4 alkyl group, or, when taken together with the adjacent nitrogen atom to which they are attached, they represent a 5 to 7-membered saturated heterocyclic group) or a group of the formula: ##STR3## (R.sup.a and R.sup.b are each as defined above), Y is an ethylene group or a vinylene group, R.sup.1 is a hydrogen atom, a hydroxyl group or a protected hydroxyl group, R.sup.2 is a hydrogen atom or R.sub.1 and R.sub.2, when taken together, means a single linkage to form a double bond between the carbon atoms which they are linked, R.sup.3 is a hydroxyl group or a protected hydroxyl group, R.sup.4 is a hydrogen atom or a C.sub.

Abstract: Novel compounds of the following general formula: ##STR1##

Abstract: Novel compounds of the following formula: ##STR1##

Abstract: Novel compounds of the following general formula: ##STR1##

Abstract: Novel compounds of the following general formula: ##STR1##

Abstract: Prostaglandin I.sub.2 analogues of the formula: ##STR1## [wherein the symbol between the carbon atoms in positions 5 and 6 represents a single or double bond, Y represents ethylene or trans-vinylene, R.sup.1 represents hydrogen, alkyl of 1 to 12 carbon atoms, aralkyl of 7 to 12 carbon atoms, cycloalkyl of 4 to 7 carbon atoms optionally substituted by alkyl of 1 to 4 carbon atoms, phenyl optionally substituted by chlorine, trifluoromethyl, alkyl of 1 to 4 carbon atoms or phenyl, a --C.sub.m H.sub.2m COOR.sup.7 group (wherein m represents an integer of from 1 to 12 and R.sup.7 represents alkyl of 1 to 4 carbon atoms), a --C.sub.n H.sub.2n OR.sup.8 group (wherein n represents an integer of from 2 to 12 and R.sup.8 represents hydrogen or alkyl of 1 to 4 carbon atoms) or a ##STR2## group (wherein R.sup.9 and R.sup.10 each represent alkyl of 1 to 4 carbon atoms and n is as hereinbefore defined), R.sup.2 represents hydrogen or a hydroxy-protecting group, R.sup.

Abstract: New inter-m-phenylene-PGI.sub.2 derivatives are prepared of the general formula I ##STR1## wherein R.sup.1 stands for hydrogen, alkyl containing 1 to 4 carbon atoms or a pharmaceutically acceptable primary, secondary, tertiary or quaternary ammonium cation or a metal cation,R.sup.2 and R.sup.3 stand independently on each other for hydrogen, alkanoly, aroyl or an acetal type or alkyl silyl type protecting group,R.sup.4 represents hydrogen or an alkyl group containing 1 to 4 carbon atoms,X stands for oxygen, or a--CH.sub.2 --group,Y stands for--C.tbd.C-- or a trans--CH.dbd.CW group, wherein W stands for chlorine, bromine or fluorine,Z represents an alkyl group having 6 to 9 carbon atoms, optionally substituted by one or more alkyl groups containing 1 to 4 carbon atoms or fluorine or it stands for an optionally substituted arylmethyl or aryloxy methyl group.The new compounds are active ingredients of pharmaceutical compositions having antiaggregatory activity.

Abstract: Arylacetic acid derivatives of the formula ##STR1## with R.sup.1, R.sup.2 and R.sup.3 specifically defined and which are useful as antirheumatic and antiinflammatory pharmaceuticals are prepared by catalytic hydrogenation of new compounds of the formula ##STR2## in which R and R.sup.10 are also specifically defined. The method of making the latter compound is also set forth.

Abstract: The invention concerns adducts of 1,8-dihydroxy-9-anthrone, of formula: ##STR1## in which: R.sub.1 and R.sub.2, taken together, form one of the following divalent residues: ##STR2## R.sub.3, R.sub.4, R'.sub.4, R.sub.5 and R'.sub.5 representing H, an alkyl group having 1-8 C with the exception of R.sub.5 =R'.sub.5 =CH.sub.3, a monohydroxyalkyl group with 2-8 C, possibly interrupted by one or more oxygens, a cycloalkyl group having 4-6 C, a phenyl group, or a benzyl group.Utilization of the compounds (I) in human or veterinary medicine, in particular in the treatment of psoriasis and or warts, and in cosmetics.

Abstract: A series of ester and salt derivatives of fluorene-9-carboxylic acid and fluorene-1-carboxylic acid exhibit significant plant growth regulating properties, useful in controlling the size, shape, dormancy time, flowering time and/or fruit setting of plants, depending upon the concentrations used. They may also be used to control the growth rate, texture and color of turf grass. Presently preferred compounds include the cis-2,5-dimethylpyrrolidine salt of 1-fluorenecarboxylic acid, 9-cis-2,5-dimethyl-1-pyrrolidinyl-2-chlorofluorene-9-carboxylic acid, methyl ester, the 2,6-dimethylpiperidine salt of 1-fluorenecarboxylic acid, and the cis-2,5-dimethylpyrrolidine salt of 9-hydroxyfluorene-9-carboxylic acid.