Abstract: The current invention discloses hydroxyamidino derivatives useful as nitric oxide synthase inhibitors.

Abstract: The current invention discloses hydroxyamidino derivatives useful as nitric oxide synthase inhibitors.

Abstract: Process for the synthesis of .alpha.-substituted acrylic acids of general formula (I) and their application to the synthesis of N-(mercaptoacyl)aminoacid derivatives of formula (II).

Abstract: The present invention relates to new fluorobutenyl (thio)ethers of the formula (I) ##STR1## in which R.sup.1 represents hydrogen or halogen,R.sup.2 and R.sup.3 independently of one another represent hydrogen or in each case optionally substituted alkyl, cycloalkyl, aryl, aralkyl or hetaryl,R.sup.4 represents hydrogen, or represents in each case optionally substituted alkyl, alkenyl, cycloalkyl, aryl, aralkyl, hetaryl and additionally represent a metal ion equivalent or an ammonium ion if Z represents oxygen,X represents oxygen or sulphur,Y represents oxygen or sulphur,Z represents oxygen, sulphur or the radical NR.sup.5 in whichR.sup.5 represents hydrogen, in each case optionally substituted alkyl, aryl, aralkyl, hetaryl or the radical ##STR2## in which R.sup.6 and R.sup.7 independently of one another represent hydrogen, in each case optionally substituted alkyl, aryl, aralkyl, or together represent optionally substituted alkanediyl andR.sup.

Abstract: The present invention relates to mixtures of .alpha.-amino acids and/or derivatives thereof and cyclopentane-.beta.-amino acids and/or derivatives thereof, dipeptides of the abovementioned .alpha.-amino acids and cyclopentane-.beta.-amino acids and mixtures of the abovementioned mixtures and dipeptides which have an improved tolerability in warm-blooded animals compared with the pure cyclopentane-.beta.-amino acids.

Abstract: Amidino derivatives of formula (I) and salts, and pharmaceutically acceptable esters and amides thereof, in which: R.sup.1 is a C.sub.1-6 straight or branched chain alkyl group, a C.sub.2-6 alkenyl group, a C.sub.2-6 alkynyl group, a C.sub.3-6 cycloalkyl group or a C.sub.3-6 cycloalkylC.sub.1-6 alkyl group; Q is an alkylene, alkenylene or alkynylene group having 3 to 6 carbon atoms and which may optionally be substituted by one or more C.sub.1-3 alkyl groups; a group of formula --(CH.sub.2).sub.p X(CH.sub.2).sub.q -- where p is 2 or 3, q is 1 or 2 and X is S(O).sub.x where x is 0, 1 or 2, O or NR.sup.2 where R.sup.2 is H or C.sub.1-6 alkyl; or a group of formula --(CH.sub.2).sub.r A(CH.sub.2).sub.s -- where r is 0, 1 or 2, s is 0, 1 or 2 and A is a 3 to 6 membered carbocyclic or heterocyclic ring which may optionally be substituted by one or more suitable substituents such as C.sub.1-6 alkyl, C.sub.1-6 alkoxy, hydroxy, halo, nitro, cyano, trifluoro C.sub.1-6 alkyl, amino, C.sub.1-6 alkylamino or diC.sub.

Abstract: Novel compounds of Formula I and methods of making and using the compounds which are useful as fungicides, particularly in the agricultural field: ##STR1## wherein C.sub.1 and C.sub.2 are carbon atoms which are part of an aromatic ring; W is alkoxyimino, alkoxymethylene or alkylthiomethylene; R.sub.1 is independently selected from the group consisting of halogen, cyano, C.sub.1 -C.sub.4 alkyl, C.sub.1 -C.sub.4 alkoxy, wherein the alkyl or alkoxy are optionally substituted by halogen, and p is 0, 1, or 2; Z is --CH.sub.2 --, --CH(OH)--, --CO--, --O--, --S--, NR.sub.2 wherein R.sub.2 is hydrogen or a lower aliphatic group, --CH.sub.2 CH.sub.2 --, --CH.dbd.CH--, ##STR2## --CH.sub.2 O--, --CH.sub.2 S--, --CH.sub.2 S(O)--, --OCH.sub.2 --, --SCH.sub.2 --, --S(O)CH.sub.2 --, --CH.sub.2 ON.dbd.C(R.sub.3)-- or --CH.dbd.NB wherein B is --O--CO--, --N.dbd.CR.sub.3, or --CR.sub.3 R.sub.4 -- wherein R.sub.3 and R.sub.4 are independently hydrogen or C.sub.1 -C.sub.

Abstract: A method for the topical or systemic treatment of disorders mediated by proteases which result in skin or mucosal lesions, and in particular, pemphigus, cicatricial pemphigoid, bullous pemphigoid, lichen planus, and canker sores, is disclosed wherein the host is treated with an effective amount of N-acetyl ysteine or a derivative thereof, or its pharmaceutically acceptable salt, optionally in a pharmaceutically acceptable diluent or carrier for systemic or topical delivery.

Abstract: Esters of alkanoyl L-carnitines wherein the alkanoyl is a saturated or unsaturated, straight or branched alkanoyl having 2-26 carbon atoms, optionally .omega.-substituted with trialkylammonium, dialkylsulfonium, hydroxyl, carboxyl, halogen, methanesulfonyl and hydroxysulfonyl, are useful for preparing pharmaceutical compositions for the treatment of endotoxic shock.

Abstract: Urea-containing hydroxyethylamine peptide compounds are effective as retroviral protease inhibitors, and in particular as inhibitors of HIV protease.

Abstract: A compound of the formula ##STR1## with R being hydrogen, alkyl, cycloalkyl or aryl, which may be substituted with halogen or alkyl, and R' and R.sup.a being hydroxyl, or --O-alkyl, pharmaceutically acceptable salts thereof; or mixtures thereof. An anti-neoplastic composition comprises the compound described above and a pharmaceutically acceptable carrier. In vitro and in vivo methods of preventing or inhibiting the growth and proliferation of neoplastic cells and/or tumors comprise contacting the cells with or administering to a subject an anti-growth and proliferation effective amount of the compound described above.

Abstract: Derivatized drugs are prepared with a linker consisting of a malonate, wherein the drug is linked through a methylene to the 2-position carbon of the malonate.

Abstract: A lubricant additive having antiwear and antioxidant properties is the reaction product of a sulfur-containing carboxylic acid and an etheramine, preferably 3,3'-thiodipropionic acid and N-isoeicosyloxypropyl-1,3-diaminopropane which is post reacted with an aliphatic alcohol, preferably oleyl alcohol, an aliphatic amine, preferably a tert-C.sub.12 to C.sub.14 amine and/or a trialkyl phosphite, preferably a tributylphosphite. The post-reaction product contains at least one ester, amide and/or phosphonate functional group.

Abstract: An N-acylamino acid compound represented by the general formula (1):R--CO--(NH--X--CO).sub.n --OR.sup.1 (1)wherein (NH--X--CO) is an amino acid residue, X in (NX--X--CO) is variable with the kind of amino acid to be used, R--CO is a saturated or an unsaturated fatty acid residue having 6 to 24 carbon atoms, R.sup.1 is hydrogen atom, sodium atom, potassium atom, or methyl group and n is an integer in the range of from 1 to 3, indicating that at least one histidine is contained as a component amino acid is disclosed, which is obtained by causing an N-hydroxysuccinimide ester to react with an amino acid or a peptide.The compound excels in antioxidizing power, emulsifying power, antibacterial power, chelating power, infrared absorbing power, and humidity-retaining power.

Abstract: Compounds having the properties of morphinic substances, particularly anasia, with beneficial effects on behaviour and with peripheral effects without their major drawbacks (tolerence, addiction), the blood-brain barrier and having the following formula :H.sub.2 N--CH(R.sub.1)--CH(R.sub.2)--S--S--CH(R.sub.3)--CH(R.sub.4)--A--B--Zwherein: AB preferably represents a CO amide bond, R.sub.2 et R.sub.3 preferably represent a hydrogen atom, R.sub.1 et R.sub.4 preferably represent, independently of each other, a benzyl grouping, --CH.sub.2 CH.sub.2 SCH.sub.3, --CH.sub.2 --CH.sub.2 --S(O)--CH.sub.3 or --CH.sub.2 --CH(CH.sub.3) .sub.2, Z may represent a --CH(R.sub.5)[CH(R.sub.6)].sub.n --COO(R.sub.7) grouping wherein: R.sub.5 may represent a hydrogen atom, a methyl grouping, a benzyl grouping or a phenyl grouping, R.sub.6 may represent a hydrogen atom and may also form a hydrocarbon cycle with R.sub.5, or Z may represent a heterocyclic grouping, and preferably a morpholinyl grouping. No drawings.

Abstract: Di-, tri- and poly-perfluoroalkyl-substituted alcohols and acids and derivatives thereof are described which are prepared from perfluoroalkyl iodides and di-, tri- or polyallyl alcohols or acids. These compounds contain two or more perfluoroalkyl-iodoalkyl or perfluoroalkyl-alkenyl groups and one or two alcohol or acid groups or derivatized alcohol or acid functions. They can be reacted with isocyanates, epoxy compounds, anhydrides, acids or acid derivatives to prepare a great variety of oil- and water-repellent compositions which are useful for oil- and water-repellent treatment of textiles, glass, paper, leather and other substrates.

Abstract: The invention relates to new optically active amino acid derivatives of the general formula (I) ##STR1## in which n, R, R.sub.1, R.sub.2, R.sub.3, X and A have the meaning given in the description, which amino acid derivatives contain sulphoxide or sulphone groups, to two basic synthetic routes for the preparation from sulphur-containing amino acids, to the polymerization of these monomers and to the use of the polymers as optically active adsorbents for chromatographic resolution of racemates to give the enantiomers.

Abstract: Low molecular weight polyaldehydes are prepared by converting the acetal groups of the low molecular weight polyacetal to aldehyde groups or by reacting an aldehyde-containing reagent (e.g., glyoxal) with a polyamide.

Abstract: A selective and high yield process for S-acylating glutathione, comprising the eaction between glutathione and an acyl chloride or a carboxylic anhydride in trifluoroacetic acid is described.

Abstract: Disclosed is a method for extracting an amino acid ester from a hydrous solution which comprises adding thereto a water-insoluble organic solvent and then an amount of a base effective to liberate only a portion of the amino acid ester in free base form, and transferring the thus liberated amino acid ester in the free base form into the organic layer, and repeating the neutralization-extraction steps until all of the amino acid ester has been extracted.

Abstract: The invention comprises compositions and methods for the treatment of psoriasis.

Abstract: The invention relates to new optically active sulphur-containing amino acid derivatives, a process for their preparation, their polymerisation to give optically active polymers and the use of these optically active polymers as adsorbents for chromatographic separation of racemates into enantiomers.

Abstract: The present application discloses pesticidally active compounds of formula I:QQ.sup.1 CR.sup.1 .dbd.CR.sup.2 CR.sup.3 .dbd.CR.sup.4 C(.dbd.X.sup.1)NR.sup.5 R.sup.6or a salt thereof, wherein Q is an monocyclic aromatic ring, or Q is a dihalovinyl group or a group R.sup.7 --C.dbd.C-- where R.sup.7 is C.sub.1-4 alkyl, tri C.sub.1-4 alkylsilyl, halogen or hydrogen; Q.sup.1 is a 1,2-cyclopropyl ring optionally substituted by one or more groups selected from C.sub.1-3 alkyl, halo, C.sub.1-3 haloalkyl, alkynyl, or cyano; R.sup.1, R.sup.2, R.sup.3 and R.sup.4 are the same or different with at least one being hydrogen and the others being independently selected from hydrogen, halo, C.sub.1-4 alkyl or C.sub.1-4 haloalkyl; X.sup.1 is oxygen or sulphur; R.sup.5 is C.sub.1-8 hydrocarbyl optionally substituted, halo, cyano, trifluoromethyl, trifluoromethylthio or C.sub.1-6 alkoxy; and R.sup.6 is selected from:(A) --Y.dbd.X.sup.2 --(R.sup.8).sub.a where X.sup.2 is O or S, Y is carbon, R.sup.8 is hydrogen, C.sub.

Abstract: Oligomers with polydiene sequences and crosslinkable grafts are useful as coatings for protecting metal surfaces as well as inking buffers. The oligomers contain a polydiene sequence of 1-100 diene links, from 1 to 20 polar functional groups, and from 1-20 acrylic or methacrylic groups.

Abstract: This invention relates to cysteine derivatives of the formula[I] and salts thereof. ##STR1## The compounds of this invention are useful for immunomodulator and treatment of liver disorder.

Abstract: Compounds of formula I ##STR1## wherein R.sub.1 and R.sub.2 are the same or different and each represent hydrogen, alkyl, alkenyl, cycloalkyl, aryl or aralkyl are produced by a new environmentally acceptable process.

Abstract: This invention relates to a glutathione-S-lower fatty acid derivative of the formula ##STR1## [wherein R.sub.1 is a lower alkyl group which may be substituted; R.sub.2 is a hydrogen atom; R.sub.3 is a hydrogen atom or a lower alkyl group which may be substituted; R.sub.4 is a hydroxyl group, a lower alkoxy group which may be substituted; n means 1] or a salt thereof, and a method for production thereof.The glutathione-S-lower fatty acid derivative of the present invention or a salt thereof shows an excellent antihepatopathic activity and can be used with advantage as a drug for the treatment of various hepatic disorders.

Abstract: Antimicrobial compounds of the formula ##STR1## wherein R.sup.1 is selected from the group consisting of H, an amine protective group, and a moiety of the formula ##STR2## wherein R.sup.2, R.sup.5, and R.sup.6 are independently selected from H and an amine protective group;R.sup.3 and R.sup.4 are independently selected from H, lower alkyl, aryl, arylalkyl, CH.sub.2 OR, CH.sub.2 SR or CH(CH.sub.3)OR;R=H, propargyl lower alkyl, arylalkyl or aryl;wherein R.sup.1 and R.sup.2 or R.sup.5 and R.sup.6 can be joined to form a ring; and wherein when R.sup.1 and R.sup.2 or R.sup.5 and R.sup.6 are both H, the compound is either in free base form or in salt form.

Abstract: Novel thiol-terminated hydroxyamides, and processes for their preparation and use are provided. These hydroxyamide compounds may be prepared by the reaction of a mercapto-functional alkyl ester, such as methylmercaptopropionate, with a molar excess of an alcohol-substituted amine, such as a b-hydroxyalkyl amine. The thiol-terminated hydroxyamides are useful as polymerization chain transfer agents, particularly when it is desirable to form polymers or oligomers containing functional hydroxyamide end groups. By chain terminating such polymers or oligomers with reactive hydroxyamide end groups the polymers or oligomers can be further reacted with acid-containing monomers or polymers to form block or graft copolymers.

Abstract: Novel mercapto-acylamino acids of the formula ##STR1## wherein Q is hydrogen or R.sup.7 CO--;R.sup.1 is lower alkyl, cyclolower alkyl, aryl or heteroaryl;R.sup.2 is hydrogen; lower alkyl; cyclolower alkyl; lower alkyl substituted with hydroxy, lower alkoxy, mercapto, lower alkylthio, aryl or heteroaryl; aryl; or heteroaryl;R.sup.3 is --OR.sup.5 or --NR.sup.5 R.sup.6 ;R.sup.4 and R.sup.9 are independently --(CH.sub.2).sub.q R.sup.8, provided that when R.sup.4 and R.sup.9 are both hydrogen, R.sup.2 is biphenylyl, phenoxyphenyl, phenylthiophenyl, naphthyl, heteroaryl, or lower alkyl substituted with hydroxy, lower alkoxy, mercapto or lower alkylthio;R.sup.5 and R.sup.6 are independently selected from the group consisting of hydrogen, lower alkyl, hydroxy lower alkyl, lower alkoxy lower alkyl and aryl lower alkyl, or R.sup.5 and R.sup.6 together with the nitrogen to which they are attached form a 5-7 membered ring;R.sup.7 is hydrogen, lower alkyl or aryl;R.sup.

Abstract: This invention relates to novel compounds of the formula [I], which are useful for treatment of various diseases such as immunodeficiency and autoimmune diseases caused by immune disorders, processes for preparing the compounds and compositions containing the compounds as active ingredients.

Abstract: Anchimeric chelates are disclosed which are capable of rapidly forming stable chelates with radionuclide metals at or below physiological temperature. Bifunctional anchimeric chelates having these same properties are also disclosed which are useful for radiolabeling target specific molecules such as monoclonal antibodies and fragments thereof.

Abstract: Compounds of formula I ##STR1## wherein R.sub.1 and R.sub.2 are the same or different and each represent hydrogen, alkyl, alkenyl, cycloalkyl, aryl or aralkyl are produced by a new environmentally acceptable process.

Abstract: Novel chemical compounds are provided which selectively inhibit the metabolism of dipeptidase (E.C.3.4.13.11) and therefore are useful in combination with antibacterial products. These chemical compounds are z-2-acylamino-3-monosubstituted propenoates.

Abstract: A process for preparing dipeptides with N-terminal non-proteinogenous amino acids of the formula ##STR1## in which R.sup.1 to R.sup.6 have the meaning stated in the description, from compounds of the formula ##STR2## is described.

Abstract: New 3-(1-aminoalkylphosphinyl)-(2-substituted)propionic acids are described which display antibacterial activity and potentiate carbapenem antibiotics.

Abstract: The subject invention involves halogenated amino acid derivatives useful as antimicrobial agents having the structure: ##STR1## wherein --R is hydrogen or 2-aminoethyl; --R' is hydroxy, alkoxy, aryloxy, or an amino acid residue bonded at the amino nitrogen; --R" is hydrogen or an amino acid residue bonded at the carbonyl carbon; --X is halogen; and --Y is hydrogen or halogen.

Abstract: The invention relates to a process for the enantiomer-selective preparation of .gamma.-keto-.delta.-amino acid derivatives of the formula I ##STR1## characterized in that a compound of the formula II ##STR2## is converted, using a trialkylchlorosilane, into a compound of the formula III ##STR3## this compound is then reacted with a diazoacetate of the formula N.sub.2 CH.sub.2 COOR.sup.4 (R.sup.4 .noteq.H) to give a cyclopropane compound of the formula IV ##STR4## and then the compound IV is converted, by ring-opening and removal of the silyl groups, and where appropriate saponification, into the compound of the formula I, R.sup.1, R.sup.2, R.sup.3, R.sup.4 and R.sup.5 having the meanings indicated in claim 1.

Abstract: Novel ester derivatives of carboxylic acid medicaments of formula (I), wherein R--COO--represents the acyloxy residue of a carboxylic acid drug or medicament, n is an integrer from 1 to 3, and R.sub.1 and R.sub.2 are the same or different and are selected from a group consisting of an alkyl, an alkenyl, an aryl, an aralkyl, a cycloalkyl and which group may be unsubstituted or substituted, or R.sub.1 and R.sub.2 together with the N forms a 4-, 5-, 6- or 7-membered heterocyclic ring, which in addition to the nitrogen atom may contain one or two further heteroatoms selected from the group consisting of nitrogen, oxygen and sulfur and which heterocyclic group may be substituted. These compounds are highly biolabile prodrug forms of the corresponding carboxylic acid compounds and are highly susceptible to undergoing enzymatic hydrolysis in vivo whereas they are highly stable in aqueous solution.

Abstract: Disclosed are some new aminoethylphosphinic acid derivatives useful as antibacterial agents.

Abstract: Compounds which are inhibitors of cholesterol biosynthesis (by inhibiting de novo squalene biosynthetis), and thus are useful as hypocholesterolemic agents and antiatherosclerotic agents, are provided which have the structure ##STR1## wherein R.sup.2 is a metal ion, lower alkyl or H; R.sup.3 is a metal ion or lower alkyl;R is R.sup.1 --(CH.sub.2).sub.n --, R.sup.1 --(CH.sub.2).sub.m --O-- orR.sup.1 --(CH.sub.2).sub.m --OCH.sub.2 --, wherein n is 1 to 4 and m is 0 to 3, andR.sup.1 is R.sup.5 --Q.sup.1 --Q.sup.2 --Q.sup.3 -- wherein R.sup.5, Q.sup.1, Q.sup.2 and Q.sup.3 are as defined herein.New intermediates, new methods of preparation and a method for using such compounds to inhibit cholesterol biosynthesis are also provided.

Abstract: Lubricants are stablized against oxidative degradation by the incorporation therein of hydroxylamines substituted with thioalkanoic acid residues of the formula ##STR1## wherein R and R.sub.1 are independently H, alkyl or aryl, X is independently OR.sub.2 SR.sub.2 or NR.sub.3 R.sub.4 wherein Rhd 2 is H, alkyl, cycloalkyl or aralkyl, and R.sub.3 and R.sub.4 are independently H, alkyl or aryl and n is 1 or 2.

Abstract: Novel compounds of the formula (I), a process for their preparation and their use as collagenase inhibitors are described: ##STR1## in which, R.sub.1 is hydrogen, alkyl, or optionally substituted aryl;R.sub.2 is hydrogen, or acyl such as ##STR2## where Z is optionally substituted aryl; R.sub.3 is C.sub.3-6 alkyl;R.sub.4 is hydrogen, alkyl, --CH.sub.2 --R.sub.10 where R.sub.10 is optionally substituted phenyl or heteroaryl, or a group ##STR3## where R.sub.11 is hydrogen, alkyl, or --CH.sub.2 --Ph where Ph is optionally substituted phenyl, and R.sub.12 is hydrogen or alkyl; andR.sub.5 is hydrogen, alkyl, or a group ##STR4## where R.sub.13 is hydrogen, or alkyl, and R.sub.14 is hydroxy, alkoxy, or --NR.sub.6 R.sub.7, where each of R.sub.6 and R.sub.7 is hydrogen or alkyl, or R.sub.6 and R.sub.7 together with the nitrogen atom to which they are bonded form a 5-, 6- or 7-membered ring with an optional oxygen or sulphur atom in the ring or an optional further nitrogen atom optionally substituted by alkyl.

Abstract: The process described makes it possible to obtain optically pure 4-amino-3-hydroxycarboxylic acids by means of a series of stereoselective steps. The starting material is an alpha-amino acid in the L or D configuration, with which Meldrum's acid is reacted. The resulting pyrrolone derivative is reduced prior to opening of the pyrrolidine ring. The invention also relates to the new products obtained by the said process and to the pyrrolone derivatives obtained as intermediates.

Abstract: Polyhaloalkene compounds of the formula: ##STR1## wherein X is sulfur, oxygen, or nitrogen, Y.sup.1 and Y.sup.2 are fluorine, Z is hydrogen or the same as Y.sup.1 and Y.sup.2, and n is 1-4; provided that:(A) when X is sulfur, Z is fluorine and R is thienyl or substituted thienyl, thianaphthyl or substituted thianaphthyl, thiazolinyl or substituted thiazolinyl, oxadiazolyl or substituted oxadiazolyl, 3,4,4-trifluoro-3-butenyloxycarbonylmethyl, thiadiazolyl substituted by halogen or R.sup.2 S, wherein R.sup.2 is 3,4,4-trifluoro-3-butenyl or R.sup.2 is phenylmethyl or phenylthiomethyl each optionally substituted by halogen or nitro; or R is thiadiazolyl substituted by R.sup.3, wherein R.sup.3 is substituted aryl, arylalkyl, aryloxyalkyl, alkylthio, haloalkylthio, haloarylthio, cyanoalkylthio, arylalkylthio, aryloxyalkylthio, arylthioalkylthio, heterocycloalkylthio, alkenylthio, haloalkenylthio, halocycloalkylalkenylthio, wherein said aryl or heterocyclic groups of R.sup.

Abstract: In the process of hydrocarboxylating an .alpha.-enamide with CO and H.sub.2 O or an organic hydroxyl compound to produce an N-acyl-.alpha.-amino acid or ester, respectively, the improvement comprising using as the .alpha.-enamide reactant, an .alpha.-enamide which has a chiral center that is essentially all L or D, thereby producing a reaction mixture containing diastereomeric N-acyl-.alpha.-amino acids or esters having two chiral centers, said mixture having essentially no enantiomeric pairs.

Abstract: The invention relates to novel processes and intermediates for the preparation of 5-amino-4-hydroxyvaleric acid derivatives of the formula ##STR1## in which R.sup.1 represents hydrogen, optionally substituted alkyl, cycloalkyl, cycloalkyl-lower alkyl, aryl, aryl-lower alkyl or the radical of a natural amino acid, R.sup.2 represents hydrogen, optionally substituted alkyl, cycloalkyl, cycloalkyl-lower alkyl, aryl, aryl-lower alkyl, amino, hydroxy, mercapto, sulphinyl, sulphonyl or the radical of a natural amino acid, and R.sup.3 represents optionally substituted hydroxy or amino, by sigmatropic rearrangement of a suitable allyl ester, halolactonisation of the resulting .gamma.,.delta.-unsaturated acid or of a suitable derivative thereof, exchange of halogen for a nitrogen-containing nucleophile, opening of the lactone ring and freeing of the amino group. Compounds of the formula I are starting materials for the preparation of renin-inhibitors which have an anti-hypertensive action.

Abstract: A novel process for the preparation of 2-(10,11-dihydro-10-oxodibenzo[b, f]thiepin-2-yl)propionic acid which shows high anti-inflammatory and analgetic action is disclosed. The process starts from a propiophenone derivative having the formula (II): ##STR1## wherein R.sup.1 is hydrogen or a lower alkyl group, which is once converted into a haloacetal compound via a halo-ketone compound, and then converted into the desired dibenzothiepin derivative through a combination of rearrangement, hydrolysis and ring closure in variable sequences.

Abstract: Substituted alkadienes of the formula: ##STR1## in which R.sub.1 is hydroxy or acetoxy, R.sub.2 is hydrogen, carboxy, alkoxycarbonyl, phenyl or benzoyl, andR.sub.3 is alkylthio or alkoxy and R.sub.4 is naphthoyl or optionally substituted benzoyl,or R.sub.3 is alkoxycarbonyl, cycloalkyloxycarbonyl or cyano and R.sub.4 is alkyl, naphthyl, optionally substituted phenyl, alkylthio, naphthylmethanethio, optionally substituted benzylthio, optionally substituted phenylthio, naphthylthio, phenethylthio or allylthio,or R.sub.3 and R.sub.4 form, with the carbon atom to which they are attached, a ring-system of formula: ##STR2## in which R.sub.5 is hydrogen or alkoxy and X is methylene or S inhibit 5-lipoxygenase and are useful, for example, as anti-inflammatories.

Abstract: Novel asymmetric thioethers of the formula ##STR1## in which the general symbols have the following meanings: a is an integer of from 1 to 7,R.sup.o represents hydrogen or C.sub.1-7 -alkanoyl,R.sup.1 represents C.sub.1-3 -alkyl which may be substituted at the terminal carbon atom by a free or acylated hydroxy group, by a halogen atom having an atomic number of at most 17, or by methoxy, or represents C.sub.1-3 -perfluoroalkyl,R.sup.2 represents an optionally unsaturated aliphatic radical having from 5 to 15 carbon atoms,A represents ethylene or alternatively, if R.sup.1 represents a halogenated radical and/or B represents phenylene or ethylene, a single bond or vinylene,B represents a single bond, ethynylene or phenylene,R.sup.3 represents hydroxy, C.sub.