Abstract: A solid phase synthesis method and intermediates useful in the process are disclosed for the preparation of diamino diol and diamino alcohol inhibitors of HIV protease.

Abstract: HIV protease inhibitors inhibit or block the biological activity of the HIV protease enzyme, causing the replication of the HIV virus to terminate. These compounds can be prepared by the novel methods of the present invention using the novel inventive intermediates.

Abstract: .alpha.,.alpha.-Difluoro-.beta.-hydroxy thiol esters of Formula (III): ##STR1## wherein: R.sup.c and R.sup.d are independently selected from the group consisting of H, C.sub.1 -C.sub.6 alkyl, substituted C.sub.1 -C.sub.6 alkyl, S-tert-butyl difluorothioacet-2-yl, C.sub.3 -C.sub.8 cycloalkyl, C.sub.3 -C.sub.8 cycloalkenyl, substituted C.sub.3 -C.sub.8 cycloalkyl, substituted C.sub.3 -C.sub.8 cycloalkenyl, aryl, substituted aryl, C.sub.6 -C.sub.10 fused aromatic rings, and substituted C.sub.6 -C.sub.10 fused aromatic rings; orR.sup.c and R.sup.d together make up a ring selected from the group consisting of C.sub.3 -C.sub.8 cycloalkyl, C.sub.3 -C.sub.8 cycloalkenyl, substituted C.sub.3 -C.sub.8 cycloalkyl and substituted C.sub.3 -C.sub.8 cycloalkenyl;R.sup.e is selected from the group consisting of C.sub.1 -C.sub.10 alkyl, substituted C.sub.1 -C.sub.10 alkyl, aryl, substituted aryl, C.sub.3 -C.sub.8 cycloalkyl, C.sub.3 -C.sub.8 cycloalkenyl, substituted C.sub.3 -C.sub.8 cycloalkyl and substituted C.sub.3 -C.sub.

Abstract: Bridged bicyclic aromatic compounds are provided having the structure ##STR1## wherein R.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.5 and n are as defined herein. The novel compounds are useful for modulating gene expression of retinoic acid receptors, vitamin D receptors and thyroid receptors. Pharmaceutical compositions and methods for modulating gene expression are provided as well.

Abstract: The invention provides a method of screening a substance for the ability to effect the formation of a retinoid X receptor homodimer comprising combining the substance and a solution containing retinoid X receptors and determining the presence of homodimer formation. Also provided is a method of screening a substance for an effect on a retinoid X receptor homodimer's ability to bind DNA comprising combining the substance with the homodimer and determining the effect of the compound on the homodimer's ability to bind DNA. A method of inhibiting an activity of a retinoid X receptor heterodimer comprising increasing the formation of a retinoid X receptor homodimer, thereby preventing the retinoid X receptor from forming a heterodimer and preventing the resulting heterodimer activity is also provided. A method of inhibiting an activity of a retinoid X receptor homodimer is also provided.

Abstract: The amide derivative of the present invention is one represented by the following general formula (I) and the dermatologic preparation of the present invention is one containing said amide derivative. ##STR1## wherein R.sup.1 represents a straight-chain or branched, saturated or unsaturated hydrocarbon group carrying 10 to 40 carbon atoms; R.sup.2 represents a straight-chain or branched, saturated or unsaturated hydrocarbon group carrying 3 to 39 carbon atoms; R.sup.3 represents a group containing at least one group represented by the formula: ##STR2## wherein R.sup.4 and R.sup.5 each represents a hydrogen atom or a straight-chain or branched or cyclic, saturated or unsaturated hydrocarbon group, or R.sup.4 and R.sup.

Abstract: A process to make .alpha.,.alpha.-difluoro-.beta.-hydroxy thiol esters of formula (IIIA) ##STR1## comprising reacting a difluoroethanethioate of formula (IVA) ##STR2## with a second reactant selected from the group consisting of aldehydes, ketones, acid halides and esters; in a solvent and in the presence of a strong base; with the proviso that the process is conducted in the absence of a catalyst and in the absence of a silyl containing compound. These thiol esters are useful as intermediates in organic syntheses of pharmaceutical products.

Abstract: The present invention provides to cyclopentane heptanoic acid, 2 heteroaryl alkyl or alkenyl derivatives which may be substituted in the 1-position with hydroxyl, alkyloxy, amino and amido groups, e.g. 1-OH cyclopentane heptanoic acid, 2 heteroarylalkenyl derivatives. In particular, these derivatives are 7-?5-hydroxy-2-(heteroatom-substituted hydroxyhydrocarbyl)-3-hydroxycyclopentyl!heptanoic or heptenoic acids and amine, amide, ether, ester and alchohol derivatives of said acids wherein one or more of said hydroxy groups are replaced with an ether group. These compounds are potent ocular hypotensive and are particularly suited for the management of glaucoma.

Abstract: Fullerene derivatives, methods of preparing the same and methods of using the same, wherein the fullerene derivatives are of the formula I ##STR1##

Abstract: The amide derivative of the present invention is one represented by the following general formula (II) and the dermatologic preparation of the present invention is one containing said amide derivative. ##STR1## wherein R.sup.11 represents a straight-chain or branched hydrocarbon group carrying 10 to 40 carbon atoms; R.sup.12 represents a straight-chain or branched hydrocarbon group carrying 1 to 39 carbon atoms; R.sup.13 represents a hydrogen atom or a hydrocarbon group carrying 1 to 6 carbon atoms; and R.sup.14 represents a hydrogen atom or a hydrocarbon group having a straight-chain, branched or cyclic structure and carrying 1 to 40 carbon atoms which may contain an oxygen atom.

Abstract: A process for producing intermediate compounds 2-deoxy 2,2-difluoro-.beta.-D-ribo-pentopyranose (III) from 3,3-difluoro-4,5,6-O-trihydroxy-5,6-O-(1-ethylpropylidene)hexene (I). The process of preparing intermediate compound (I) involves reacting D-glyceraldehyde pentanide with an organometallic complex of 3-bromo-3,3-difluoropropene. The process of preparing intermediate compound (III) involves ozonolysis and then hydrolysis. The intermediate compounds (I) and (III) are used in the preparation of 2'-deoxy-2',2'-difluorocytidine which is an antiviral agent.

Abstract: A derivative of 3-(7'-oxo-1'-aza-4'-oxabicyclo[3.2.0 ]hept-3'-yl)propionic acid represented by the formula ##STR1## wherein R.sub.1 is a hydrogen atom, a lower alkyl group optionally having one or more cycloalkyl groups, a lower acyl group, a benzoyl group optionally having one or more substituents or a benzyl group optionally having one or more substituents, R.sub.2 is a hydrogen atom or a carboxyl-protecting group, R.sub.3 is a hydroxyl group, an azido group, a benzenesulfonyloxy group optionally having one or more substituents, a lower alkylsulfonyloxy group optionally having one or more substituents, a tri-substituted silyloxy group or an amino group optionally having one or more substituents, provided that when R.sub.1 and R.sub.2 are hydrogen atoms, R.sub.3 is not an amino group, and a salt thereof.

Abstract: Novel pharmaceutically/cosmetically-active adamantyl-substituted polycyclic acetylene compounds have the structural formula (I): ##STR1## wherein Ar is a radical having one of the formulae (a)-(f): ##STR2## and are useful for the treatment of a wide variety of disease states, whether human or veterinary, for example dermatological, rheumatic, respiratory, cardiovascular, bone and ophthalmological disorders, as well as for the treatment of mammalian skin and hair conditions/disorders.

Abstract: A process for making a dialkyl carbonate which comprises reacting urea with a first alcohol in a carbamate reactor at a temperature and pressure sufficient to convert said urea to an alkyl carbamate; and reacting the alkyl carbamate with a second alcohol in the presence of a dialkyl isocyanato alkoxy tin catalyst or derivatives in a carbonate reactor at a temperature and pressure sufficient to convert the alkyl carbamate to a dialkyl carbonate, wherein the molar ratio of alkyl carbamate to second alcohol is in the range between about 2:1 to about 10:1 and wherein dialkyl carbonate is present within the carbonate reactor in an amount between about 1 to about 3 weight %, based on total alkyl carbamate and second alcohol content, and wherein the second alcohol is either the same as or different from the first alcohol or a mixture of alcohols.

Abstract: The invention relates to leukotriene-B.sub.4 antagonists of formula I ##STR1## in which n represents a whole number from 2 to 5,X represents a direct bond, 1 to 6 methylene units, an ortho-, meta- or para-substituted phenyl ring or a meta- or para-substituted pyridine ring,Y represents a bond to a hydrogen atom and simultaneously to a hydroxy group, a double-bound oxygen atom or --O--CH.sub.2 --CH.sub.2 --O--,R.sub.1 and R.sub.2 represent the radical OH, --O--(C.sub.1 -C.sub.4)--alkyl, O--(C.sub.3 -C.sub.6)--cycloalkyl, --O--(C.sub.6 -C.sub.10)--aryl, --O--(C.sub.7 -C.sub.12)--aralkyl, O--(CH.sub.2)--CO-- (C.sub.6 -C.sub.10)--aryl or the radical NHR.sub.3 with R.sub.3 meaning hydrogen, (C.sub.1 -C.sub.4)--alkyl, (C.sub.3 -C.sub.6)--cycloalkyl or (C.sub.7 -C.sub.12)--aralkyl as well as their salts with physiologically compatible bases and their cyclodextrin clathrates.

Abstract: The invention describes the synthesis and use of photoactivated (or caged) fluorescent dyes. Upon illumination at less than about 400 nm the caged dyes release highly fluorescent, water soluble hydroxypyrenesulfonic acid dyes according to the following equation: ##STR1## X, Y, and Z are independently sulfonic acid, a sulfonic acid salt, a hydroxyl group, or hydrogen, with at least one of X, Y, and Z being a sulfonic acid or sulfonic acid salt. LINK is either an ether linkage or a carbonate linkage. BLOCK is a caging group whose photolysis results in liberation of a free hydroxypyrenesulfonic acid dye.The caged fluorescent dyes are useful for application in aqueous solutions, including fluids of biological origin. The caged dyes of the present invention are especially useful for flow tagging velocimetry.

Abstract: The present invention provides a novel synthetic route to a key precursor, i.e., an (S,S)-.alpha.-fluoro-2,2-dimethyl-1,3-dioxolane-4-propanoic acid ester useful in the preparation of FddA and FddC. The instant diastereoselective process utilizes a novel intermediate which contains a chiral auxiliary. The chiral auxiliary can be any chiral auxiliary moiety such as for example an auxiliary containing a substituted oxazolidinone group. The intermediate containing the chiral auxiliary is fluorinated utilizing a fluorination method applied for the first time in the synthesis of fluorinated sugars to give a fluorinated intermediate which after removal of the chiral group provides the desired key intermediate. In summary, in the instant process, a fluorine is introduced diastereoselectively into an intermediate via the reaction of a chiral enolate with an electrophilic fluorinating agent and the intermediate which is fluorinated is derived from mannitol.

Abstract: Dermatological and/or cosmetological compositions containing at least one retinoid of general formula (I), ##STR1## and the use of such compounds for preparing dermatological and/or cosmetological compositions.

Abstract: A process for the preparation of mono-fatty acid or hydroxymono-fatty acid esters of isopropylidene derivatives of a polyglycerol is disclosed. A C6-C22 fatty acid or -hydroxy fatty acid is reacted with isopropylideneglycerol glycidyl ether or diisopropylidenetriglycerol glycidyl ether in a molar ratio of 0.5:1 to 1:0.5 at temperatures of 373473 K. in the presence of a catalyst. The monoisopropylidenediglycerol mono-fatty acid ester or monoisopropylidenediglycerol hydroxy mono-fatty acid ester or diisopropylidenetetraglycerol mono-fatty acid ester or diisopropylidenetetraglycerol hydroxy mono-fatty acid ester obtained is optionally purified by distillation, fractional distillation and/or ion exchange.

Abstract: Fluorinated alkene compounds useful for and methods of controlling nematodes, insects, and acarids that prey on agricultural crops. Polar compounds, for example, 3,4,4-trifluoro-3-butene-1-amine or 3,4,4-trifluoro-3-butenoic acid, are particularly useful for systemic control of pests. Novel method and intermediates for the preparation of 3,4,4-trifluoro-3-butene-1-amine are also provided.

Abstract: The present invention provides organoleptic compositions which upon thermolyis, hydrolysis or both, release an odorant molecule. They find utility, for example, in tobacco, in tobacco paper, and as additives to food, beverages or gum. The compositions contain one or more dicarboalkoxy dioxolane derivatives having the following formula: ##STR1## wherein R.sup.1 and R.sup.2 are, independently, --CO.sub.2 R.sup.3 wherein R.sup.3 is --H.sub.3 or lower alkyl, provided that in at least one of R.sup.1 and R.sup.2, R.sup.3 is lower alkyl; wherein Z is a direct bond, or --CH.dbd.C(R.sup.4)--; where R.sup.4 is --H or alkyl group; and Y is ##STR2## where R.sup.5 and R.sup.6 are independently --H, lower alkyl or --OR.sup.7 where R.sup.7 is --H or lower alkyl.

Abstract: Preparing cyclohexanediones of the formula ##STR1## an aldehyde is reacted with a ketene to give a polymer having the repeating unit ##STR2## wherein n ranges from about 2 to about 1,000. The polymer is hydrolyzed to produce a mixture of an unsaturated acid of the formula R--CH.dbd.C(R.sub.1)--COOH and a hydroxy ester or acid of the formula R--CH(OH)C(R.sub.1)(R.sub.2)--COOR.sub.3, the mixture is then contacted with an esterifying agent to convert the acids to esters. The ester mixture is contacted with a dehydrating agent to convert the hydroxy ester to unsaturated ester of the formula R--CH.dbd.C(R.sub.1)--COOR.sub.3. The unsaturated ester is contacted with a basic catalyst to cyclize it to the cyclic dione ester of the formula ##STR3## and this ester is then hydrolyzed and decarboxylated to give the cyclohexanedione give the productwherein:R is selected, e.g.

Abstract: Heterocyclic-alkylene quinoxalinyloxyphenoxypropanoate compounds exhibit unexpectedly desirable selective herbicidal activity. Also disclosed are compositions comprising such compounds as well as a method of controlling the growth of undesirable plants employing such compounds.

Abstract: A process for preparing 1.alpha.,25(R),26-trihydroxy-22E-ene-cholecalciferol and 1.alpha.,25(S),26-trihydroxy-22E-ene-cholecalciferol.

Abstract: Herbicidal pyrimidine compound having the formula ##STR1## wherein the substitutents A, R.sup.1, R.sup.2, X, Y.sup.1, Y.sup.2, Y.sup.3 and Z are as herein below defined.

Abstract: Alcohols of the formula ##STR1## wherein R.sup.1 and R.sup.2 are each independently methyl or ethyl or together signify pentamethylene, formed by the enzymatic hydrolysis of a corresponding (RS) alkanoic acid ester are intermediates for Vitamin E.

Abstract: Various novel acetal- and aldehyde-containing monomers are prepared. They can be polymerized and copolymerized by conventional polymerization techniques. The polymers contain repeating units derived from one or more ethylenically or allylically unsaturated monomers containing an acetal group or aldehyde group and optionally one or more repeating units derived from ethylenically or allylically unsaturated monomers other than the acetal-containing or aldehyde-containing monomer such as ethylene, vinyl acetate, ethyl acrylate, butyl acrylate, 2-ethylhexyl acrylate, hydroxyethyl acrylate, hydroxypropyl acrylate, methyl methacrylate or acrylic acid. Aqueous emulsions of polymers containing the acetal-containing monomers and a hydroxy-containing monomer are useful as binders for nonwoven fabrics.

Abstract: Ethylenically unsaturated graftable monomers are prepared by reacting hydroxy substituted orthoesters with electrophilic reagents, an alkaline reagent, and a phase transfer catalyst. Preferably the hydroxy orthoester is 4-hydroxymethyl-2-methoxy-2-methyl-1,3-dioxolane, and the preferred reagent is acryloyl chloride with sodium hydroxide as the base and methyltrialkylammonium (C.sub.8-10) chloride as the phase transfer catalyst.

Abstract: There are disclosed halogenated dioxolanes of a specified formula, dioxoles made therefrom, polymers of the dioxoles, and processes for making the dioxolanes.

Abstract: There are disclosed compounds of the formulaA(CH.sub.2).sub.n O--BwhereinA is a group having the formula ##STR1## wherein X is --N-- or ##STR2## Z is ##STR3## R.sup.1 is hydrogen, lower alkyl or phenyl; R.sup.2 is hydrogen or lower alkyl; orR.sup.1 and R.sup.2 taken together form a benzene ring, with the proviso that when X is --N--, Z is other than ##STR4## R.sup.3 is hydrogen or lower alkyl; n is 1-2;B is ##STR5## wherein Y is OR.sup.5 or N(OH)R.sup.8 ;R.sup.4 and R.sup.5 are each, independently, hydrogen or lower alkyl;R.sup.6 is hydrogen, halo or nitro;R.sup.7 is ##STR6## R.sup.

Abstract: (-)-Swainsonine is prepared by the steps of first reacting a compound having the formula: ##STR1## wherein each R.sub.2 is lower alkyl, with (4-carbalkoxybutyl) triphenylphosphonium bromide in a strong base to obtain an alcohol having the formula: ##STR2## wherein R.sub.2 is as defined above and R is C.sub.1 -C.sub.8 alkyl; the alcohol is then reacted with methanesulfonyl chloride or p-toluenesulfonyl chloride or benzenesulfonyl chloride in the presence of a tertiary amine to obtain the corresponding sulfonate. Heating the sulfonate with an azide in an organic solvent yields an imine having the formula: ##STR3## wherein R.sub.2 and R are ad defined above. Treating the imine with an inorganic base, in aqueous alcohol provides upon acidification, the corresponding acid. Heating the acid at reflux temperature in organic solvent, yields an enamide having the formula: ##STR4## wherein R.sub.2 is as defined above.

Abstract: Pyrenthrinoid esters with an indenyl nucleus having the following structural formula ##STR1## wherein the substituents are herein defined, have been shown to be useful as pesticides and in pesticidal compositions.

Abstract: Compound of the formula (I):Q.sup.1 Q(CR.sup.2 .dbd.CR.sup.3).sub.a (CR.sup.4 .dbd.CF)(CR.sup.5 .dbd.CR.sup.6).sub.b C(.dbd.O)NHR.sup.1 (1)or a salt thereof, wherein Q.sup.1 is a phenyl ring or a fused bicyclic ring system containing 9 or 10 ring carbon atoms at least one ring being aromatic, or Q.sup.1 is a dihalovinyl group; Q is an alkyl chain containing 1 to 12 carbon atoms and optionally containing one or two oxygen atoms and/or an unsaturated group --CR.sup.7 .dbd.CR.sup.8 --, or --C.dbd.C--, wherein R.sup.7 and R.sup.8 are selected from hydrogen or halo; a is 0 or 1; b is 0 or 1; the sum of a and b is 0 or 1; R.sup.2, R.sup.3, R.sup.4, R.sup.5 and R.sup.6 are the same or different, and are independently selected from hydrogen, halo and C.sub.1-4 alkyl; R.sup.1 is selected from hydrogen and C.sub.1-6 hydrocarbyl optionally substituted by dioxalanyl, halo, cyano, trifluoromethyl, trifluoromethylthio or C.sub.1-6 alkoxy are disclosed which have pesticidal activity.

Abstract: The present invention provides an optically active 2-methylenecyclopentanone derivative represented by the general formula ##STR1## (wherein R.sup.1 is a protective group for hydroxyl, and the symbol * represents an asymmetric carbon atom).

Abstract: A Derivative of 5-hetero-6-oxo-PGE A derivative of 5-hetero-6-oxo-PGE of the formula: ##STR1## wherein R.sup.1 is (1) a group of the formula: COOR11(2) hydroxymethylcarbonyl,(3) hydroxymethyl or(4) a group of the formula:CO--AAwherein AA is an amino acid-residue,Z is oxygen, sulfur or a group of the formula: NR21 wherein R21 is hydrogen or alkyl of C1--4;R2 is a single-bond or alkylene of C1--4;R3 isi) alkyl of C1-7,ii) cycloalkyl of C4-7 or cycloalkyl of C4-7 substituted by alkyl of C1-7,iii) phenyl, phenoxy, phenyl or phenoxy substituted by one group selected from alkyl of C1-4, halogen and trihalomethyl, is single-bond or a double bond.Possess PG-like activity, especially cytoprotection, and therefore are useful for treatment for and/or prevention of cytodamage.

Abstract: A process for preparing .alpha.,.alpha.-dialkoxy ketones of the formula I ##STR1## where R.sup.1 and R.sup.2 are each, independently of one another, hydrogen, C.sub.1 -C.sub.20 -alkyl, C.sub.3 -C.sub.20 -cycloalkyl, C.sub.4 -C.sub.30 -cycloalkylakyl, C.sub.9 -C.sub.30 -alkylcycloalkyl, unsubstituted or C.sub.1 -C.sub.8 -alkyl, C.sub.1 -C.sub.8 -alkoxy-, halogen-, C.sub.1 -C.sub.4 -haloalkyl-, C.sub.1 -C.sub.4 -haloalkoxy-, phenyl-, phenoxy-, halophenyl-, halophenoxy- and/or cyano-substituted aryl, C.sub.7 -C.sub.20 -aralkyl or heterocyclyl,R.sup.2 is also ##STR2## R.sup.3 and R.sup.4 are each, independently of one another, C.sub.1 -C.sub.20 -alkyl, C.sub.3 -C.sub.20 -cycloalkyl, aryl, C.sub.7 -C.sub.20 -arylalkyl, or together are an unsubstituted or C.sub.1-C.sub.4 -alkyl- substituted C.sub.2 -C.sub.7 -alkylene chain andR.sup.5 is R.sup.1 or together with R.sup.1 is an unsubstituted or C.sub.1 -C.sub.4 -alkyl-substituted C.sub.2 -C.sub.

Abstract: The present invention provides compounds which upon thermolyis, hydrolysis or both, release an odorant molecule. They find utility, for example, in tobacco, in tobacco paper, and as additives to food, beverages or gum. These compounds are dicarboalkoxy dioxolane derivatives having the following formula: ##STR1## wherein R.sup.1 and R.sup.2 are, independently, --CO.sub.2 R.sup.3 wherein R.sup.3 is --H.sub.3 or lower alkyl, provided that in at least one of R.sup.1 and R.sup.2, R.sub.4 is lower alkyl; wherein Z is a direct bond, or --CH.dbd.C(R.sup.4)--; where R.sup.4 is an alkyl group; and Y is, when Z is a direct bond, ##STR2## where R.sup.5 is lower alkyl; and Y, when Z is --CH.dbd.C(R.sup.4)--, ##STR3## where R.sup.6 is H, lower alkyl or OR.sup.7, where R.sup.7 is H or lower alkyl.

Abstract: Heterocyclic-alkylene quinoxalinyloxyphenoxypropanoate compounds having the following formula: ##STR1## wherein n, R.sup.1, R.sup.2 and R.sup.3 are as defined in the specification exhibit unexpectedly desirable selective herbicidal activity. Also disclosed are compositions comprising such compounds as well as a method of controlling the growth of undesirable plants employing such compounds.

Abstract: Polyene aldehydes of the general formula I ##STR1## where R is ##STR2## where R' is alkyl, aryl, aralkyl or cycloalkyl and, if desired, may be further substituted, and the radicals R" are each C.sub.1 -C.sub.4 -alkyl or together form --CH.sub.2 --CH.sub.2 -- or --CH.sub.2 --CH.sub.2 --CH.sub.2 -- bridges which, if desired, may be further substituted by C.sub.1 -C.sub.4 -alkyl, are prepared by catalytic oxidation of the corresponding polyene alcohol with oxygen or an oxygen-containing gas by a process wherein the oxidation is carried out in the presence of the catalyst system comprising 2,2,6,6-tetramethylpiperidine 1-oxide or 4-oxo-2,2,6,6-tetramethylpiperidine 1-oxide and copper(I) chloride.

Abstract: The claimed invention relates to intermediate compounds of the formula ##STR1## wherein R is hydrogen or methyl, R.sub.1 and R.sub.2 each, independently, is hydrogen, lower alkyl or aryl, or taken together are lower alkylene of from 3 to 6 carbon atoms, and the dotted (. . . ) line is an optional bond.

Abstract: The invention concerns a cyclic ether derivative of the formula I, ##STR1## wherein Ar.sup.1 is optionally substituted phenyl or naphthyl;A.sup.1 is (1-6C)alkylene, (3-6C)alkenylene, (3-6C)alkynylene or cyclo(3-6C)alkylene;Ar.sup.2 is optionally substituted phenylene, or a 6 membered heterocyclene moiety containing up to three nitrogen atoms;R.sup.1 and R.sup.2 together form a group of the formula --A.sup.2 --X--A.sup.3 -- wherein each of A.sup.2 and A.sup.3 is (1-6C)alkylene and X is oxy, thio, sulphinyl, sulphonyl or imino; andR.sup.3 is (1-6C)alkyl, (2-6C)alkenyl, (2-6C)alkynyl or substituted (1-4C)alkyl;or a pharmaceutically-acceptable salt thereof.The compounds of the invention are inhibitors of the enzyme 5-lipoxygenase.

Abstract: Processes, intermediates, and products involved in preparing cyclohexanediones of the formula ##STR1## are disclosed. An aldehyde of the formula R--CHO is reacted with a ketone type compound of the formula (R.sub.1)(R.sub.2)C.dbd.C.dbd.O at a temperature below about 110.degree. C. to give a polymer having the repeating unit --OCH(R)C(R.sub.1)(R.sub.2)CO].sub.n wherein n ranges from about 2 to about 1,000. The polymer is hydrolyzed with alcoholic or aqueous base to produce a mixture of an unsaturated acid of the formula R--CH.dbd.C(R.sub.1)--COOH and a hydroxy ester or acid of the formula R--CH(OH)C(R.sub.1)(R.sub.2)--COOR.sub.3, the mixture is then contacted with an esterifying agent to convert the acids to esters. The ester mixture is contacted with a dehydrating agent to convert the hydroxy ester to unsaturated ester of the formula R--CH.dbd.C(R.sub.1)--COOR.sub.3.

Abstract: An enantioselective process for the preparation of hemicaronic aldehyde with a cis or trans structure and novel intermediates.

Abstract: A process for the preparation of 5-chloro-2-pentanone starting from a ketal of a levulinic ester, followed by hydrogenation, and then reaction with hydrochloric acid. The process involves first purifying the ketal of the levulinic ester by distillation, making the hydrogenation catalysts for the ketal alkaline, and reacting the 3-(2-methyl-1,3-dioxolan-2-yl)propan-1-ol formed in this hydrogenation with hydrochloric acid to obtain 5-chloro-2-pentanone.

Abstract: A compound of a 3,5,6-trihydroxyhexanoic acid derivative of the formula: ##STR1## wherein P.sup.1 and P.sup.2 are independently hydrogen atoms or hydroxy-protecting groups, or together form a ring, and R is an alkyl group is effectively prepared by a process comprising steps of:reacting a butyronitrile derivative of the formula: ##STR2## wherein P.sup.1 and P.sup.2 are the same as defined above with an .alpha.-haloacetate of the formula:X--CH.sub.2 --COOR (III)wherein X is a halogen atom, and R is the same as defined above in the presence of a metallic catalyst selected from the group consisting zinc and zinc-copper to form a keto acid derivative of the formula: ##STR3## wherein P.sup.1, P.sup.2 and R are the same as defined above, and then reducing the obtained keto-acid derivative of the formula (IV).

Abstract: The present invention involves process for the preparation of compounds having the chemical structure: ##STR1## wherein Ar--H is an aromatic compound which is activated to an electrophilic attack, and wherein --Y is an aliphatic group having a labile moiety, especially where the labile moiety is a terminally unsaturated moiety: --C.tbd.CH, ##STR2## or aldehydes in the form of their acetals. The process comprises the step of reacting Ar--H and ##STR3## wherein --X is --Cl or --Br, and where the reaction step is carried out in a solvent medium at a temperature of from about -40.degree. C. to about -100.degree. C. using stannic chloride as a catalyst.

Abstract: The invention concerns new polyfunctional ethylenic monomers of the general formula (I): ##STR1## where R=cyano, substituted or unsubstituted acyl, substituted or unsubstituted alkoxycarbonyl or substituted or unsubstituted aryloxycarbonyl; R.sub.1 and R.sub.2 each represent --CHR.sub.3 R.sub.4 where R.sub.3 and R.sub.4 may be identical or different and represent H or an alkyl, alkenyl or aralkyl group. R.sub.1 and R.sub.2 may, alternatively, together form a radical --CH.sub.2 --(CR.sub.5 R.sub.6).sub.n --CHR.sub.7 where n=0 or 1 and R.sub.5, R.sub.6 and R.sub.7 may be identical or different and represent H or CH.sub.3.Particular monomers are: 2-cyano-4,4-dimethoxy-3-hydroxy-1-butene; 2-cyano-4,4-dibutoxy-3-hydroxy-1-butene; 4,4-dibutoxy-2-ethoxycarbonyl-3-hydroxy-1-butene; 2-butoxycarbonyl-4,4-dibutoxy-3-hydroxy-1-butene; 4,4-dimethoxy-2-hydroxythoxycarbonyl-1-butene; 4,4-dimethoxy-2-dimethylaminoethoxycarbonyl -3-hydroxy-1-butene; and 4,4-dimethoxy-2-ethoxycarbonyl-3-hydroxy-1-butene.

Abstract: There are disclosed halogenated dioxolanes of a specified formula, dioxoles made therefrom, polymers of the dioxoles, and processes for making the dioxolanes.

Abstract: Compounds of formula I ##STR1## wherein Ar is an optionally substituted phenyl ring; B is a single bond, a group --(CH.sub.2 OCH.sub.2).sub.n being n=1 or 2, a 2,4-disubstituted-1,3-dioxolane ring or a 2,4-disubstituted-1,3-thioxolane ring, R is a single bond, an optionally substituted methylene or ethylene group and T is 2-, 3- or 4-pyridyl, an optionally salified or esterified carboxy group or a carboxyamide group. Said compounds are useful in treatment of respiratory diseases.

Abstract: The present invention relates to compounds of the formula ##STR1## or a pharmaceutically acceptable salt thereof, wherein R is alkyl of 5 to 14 carbon atoms, alkenyl of 5 to 14 carbon atoms or alkynyl of 5 to 14 carbon atoms; R.sup.1 is lower alkylene or phenylene; and R.sup.2 is hydrogen, lower alkyl or a pharmaceutically acceptable cation.