Abstract: 1 The invention relates to a method and agents for permanently styling hair, characterised in that they contain a keratin reduction agent in the form of N,N-disubstituted mercaptoacetamide of general formula (I) or salts thereof, R1 and R2 representing a straight-chain or branched alkyl radical, monohydroxyalkyl or polyhydroxyalkyl or carboxyalkyl, each with 1 to 6 carbon atoms. The invention also relates to a method for producing these mercaptoacetamides and to the novel mercaptoacetamide N-ethyl-N-2′-hydroxy-ethylmercaptoacetamide. The inventive agent enables the hair to be styled gently and evenly, at a pH range—4.5 to 9.5—which is gentle on skin and hair, without causing allergic or sensitizing reactions.

Abstract: Compounds of Formula I are disclosed as inhibitors having activity against the aspartyl proteases, plasmepsin and cathepsin D. The compounds are therefore useful for treatment of diseases such as malaria and Alzheimer's disease. In preferred compounds of Formula I, Y is an dialkoxyphosphonate, or &agr;-hydroxyamide group and Z is an acyl or &agr;-ketocarbamate functionality. Intermediates in the solid phase synthesis of compounds of Formula I, in which compounds are attached to a solid support, are also disclosed.

Abstract: The present invention relates to new lipopolyamines (including salts thereof) characterised by a symmetrical, highly flexible lipophilic moiety having buffering capacity at physiological pH, and to the use thereof for the in vivo or in vitro introduction of biologically active materials, such as, for example, DNA, RNA, ribozymes, antisense DNA, PNA, peptides and proteins, into eukaryotic cells.

Abstract: The present invention relate to thio-substituted pentanedioic acid derivatives that inhibit N-Acetylated &agr;-Linked Acidic Dipeptidase (NAALADase) enzyme activity, pharmaceutical compositions comprising the same, and methods of using the same to inhibit NAALADase enzyme activity, to effect neuronal activities, to inhibit angiogenesis, and to treat glutamate abnormalities, compulsive disorders and prostate diseases.

Abstract: The invention relates to a process for preparing cis-N-methyl-4-(3,4-dichlorophenyl)-1,2,3,4-tetrahydro-1-naphthylamine, or racemic sertraline, corresponding to formula (I) in salt form, starting with 4-(3,4-dichlorophenyl)tetralone of formula (II) according to which (a) the 4-(3,4-dichlorophenyl)tetralone of formula (II) is reacted with N-methylformamide in the presence of formic acid, (b) the reaction medium obtained according to (a) is treated with a base, and (c) the racemic sertraline salt is separated out by selective crystallization with an acid. The invention also relates to N-methylformamide-4-(3,4-dichlorophenyl)-1,2,3,4-tetrahydro-1-naphthylamine and to its use to obtain racemic sertraline.

Abstract: A compound having formula (I): wherein R1 is a saturated or unsaturated chain of 1-5 carbons in length; and R2 is a saturated or unsaturated chain of 3-10 carbons in length; and A is selected from the group consisting of COOL and CONR′—R″, wherein L is a lipid moiety selected from the group consisting of glycerol, C3-20 fatty acid monoglycerides, C3-20 fatty acid diglycerides, hydroxy-C2-6-alkyl esters of C3-20 fatty acids, hydroxy-C2-6-alkyl esters of lysophosphatidic acids, lyso plasmalogens, lysophospholipids, lysophosphatidic acid amides, glycerophosphoric acids, sphingolipids, lysophosphatidylethanolamines, and N-mono and N,N-di-(C1-4)alkyl derivatives of the amines thereof; and R′ and R″ are each independently selected from the group consisting of hydrogen and a lower alkyl group comprising 1-5 carbon atoms; and pharmaceutically acceptable salts thereof. In addition, there is provided methods for using these compositions.

Abstract: A method for manufacturing a color coupler used in a silver halide photographic light-sensitive material using an ammonium trihalide. Said method for manufacturing the color coupler comprising the following step: a step for halogenating a coupling position of a four equivalent coupler using a halogenating agent, wherein said halogenating agent is said ammonium trihalide.

Abstract: The present invention relates to gel compositions comprising alkyl amides of tri-basic carboxylic acids and methods of making gel compositions.

Abstract: Compounds of Formula I wherein the substituents are as described in the specification or pharmaceutically acceptable salts or stereochemically isomeric forms thereof, useful for treating diseases related to calcium imbalance and metabolism.

Abstract: The subject invention concerns mercaptoalkylacyl compounds of formula (I): ##STR1## The compounds of the subject invention can be used to inhibit matrix metalloproteinases and/or TNF.alpha.- and L-selectin sheddase-mediated diseases including degenerative diseases and cancers. The subject invention also concerns methods of using the compounds of the invention to treat or prevent conditions associated with matrix metalloproteinases or that are mediated by TNF.alpha. or L-selectin sheddase.

Abstract: Nortriptyline functionalized compounds are provided for conjugation to antigenic compositions, particularly poly(amino acids), and enzymes. The antigenic conjugates are employed for the production of antibodies, which find use in immunoassays for the determination of nortriptyline in a sample, while the enzyme conjugates find use in an enzyme assay for the determination of nortriptyline in a sample.

Abstract: Compounds of the formula ##STR1## are useful as intermediates to new herbicidal 4-benzoylisoxazoles.

Abstract: In a process for preparing N-alkenylcarboxamides by dehydration of N-(2-hydroxyalkyl)carboxamides and/or diethers thereof in the presence of a catalyst, molecular sieves, in particular zeolites, are used as catalyst.

Abstract: The invention relates to a carbamide of the general formulaR.sub.1 --CO--NH--C(R.sub.2)(R.sub.3)--X--Ywhich is protected by a temporary protective group and whereinR.sub.1 --CO means a carbonyl residue which can be provided as a unit for the chain of a peptide, and can have one or a plurality of amino acid residues;R2 and R3 mean resides of the carbamide which do not participate in their function, whereby R2 and R3 can be identical or different, but are different when one of the two residues means a hydrogen atom;X means an oxygen atom or a sulphur atom, andY means a protective group for X.The invention further relates to a process for producing the protected carbamide and to utilisation of the protected carbamide.The protected carbamide according to the invention can also be linked to a carrier material.

Abstract: Methods and compositions for treating CF by mobilizing mutant forms of CFTR, which retain at least some functional activity, to the plasma membrane where they can mediate chloride ion transport are disclosed.

Abstract: The invention concerns activated amphetamine derivatives, a process for their production as well as their use for producing immunogens or detection conjugates carrying amphetamine groups. A further subject matter of the invention are new conjugates carrying amphetamine groups, a process for the production thereof as well as their use for the production of antibodies or for the determination of amphetamine or derivatives thereof.

Abstract: This invention relates to a process for the preparation of an .alpha.-chloroketone compound comprising the steps of(i) cyclizing an alkynyl amide to form a 5-methyleneoxazoline ##STR1## (ii) chlorinating the 5-methyleneoxazoline using trichloroisocyanuric acid to produce a chlorinated oxazoline intermediate ##STR2## and (iii) hydrolyzing the chlorinated oxazoline intermediate with an aqueous acid to produce the desired monochloroketone ##STR3## wherein Z is alkyl or substituted alkyl, aryl or substituted aryl, heteroaryl or substituted heteroaryl or phenylene,R is a hydrogen atom or alkyl, andR.sup.1 and R.sup.2 are each independently an alkyl or substituted alkyl group, or R.sup.1 and R.sup.2 together with the carbon atom to which they are attached form a cyclic structure.Additionally, when R is a hydrogen atom, a dichloroketone can be conveniently formed through adjustment of reaction conditions.

Abstract: A method for preparing a diarylalanine compound is provided. The method includes reacting a diarylaminopropanediol with a reducing agent to form a diarylaminopropanol compound and/or contacting a serine ester derivative with an aryl metal reagent to form diarylaminopropanediol. A diarylmethyloxazolidinone compound is also provided.

Abstract: This invention relates to a process for the preparation of an .alpha.-chloroketone compound comprising the steps of(i) cyclizing an alkynyl amide to form a 5-methyleneoxazoline ##STR1## (ii) chlorinating the 5-methyleneoxazoline using trichloroisocyanuric acid to produce a chlorinated oxazoline intermediate ##STR2## and (iii) hydrolyzing the chlorinated oxazoline intermediate with an aqueous acid top produce the desired monochloroketone ##STR3## wherein Z is alkyl or substituted alkyl, aryl or substituted aryl, heteroaryl or substituted heteroaryl or phenylene,R is a hydrogen atom or alkyl, andR.sup.1 and R.sup.2 are each independently an alkyl or substituted alkyl group, or R.sup.1 and R.sup.2 together with the carbon atom to which they are attached form a cyclic structure.Additionally, when R is a hydrogen atom, a dichioroketone can be conveniently formed through adjustment of reaction conditions.

Abstract: A compound of the formula ##STR1## wherein R.sup.1 and R.sup.2 independently represent H or an optionally substituted hydrocarbon group; R.sup.3 represents an optionally substituted hydrocarbon group; R.sup.4 represents H or a hydrocarbon group; ring A represents a substituted benzene ring; X represents a C.sub.2-4 alkylene group etc.; and Y represents a bond or a lower alkylene group, or salts thereof is useful as prophylactic or therapeutic agents of diseases related with melatonin activity.

Abstract: A process for preparing bis(hydroxymethyl) compounds of the formula (I) ##STR1## wherein X.sup.1 and X.sup.2 represent identical or different electronegative groups, which process entails reacting C--H-acidic compounds of the formula (II) ##STR2## wherein X.sup.1 and X.sup.2 are as defined above, with formaldehyde, wherein the reaction is carried out in an anhydrous medium.

Abstract: The present invention provides:a process for producing an alkali metal salt of an arylmercaptan compound, represented by general formula (3): ##STR1## which process comprises reacting a disulfide compound represented by general formula: ##STR2## with a hydroxide of an alkali metal M.sup.1 in the presence of a sulfur compound represented by general formula (2):H.sub.(2-i) S(M.sup.1).sub.i (2)a process for producing an alkoxycarbonylalkylthioaryl compound represented by general formula (5): ##STR3## which process comprises reacting the above-mentioned alkalimetal salt of an arylmercaptan compound with a halogenofattyacid ester compound represented by general formula (4):X.sup.1 R.sup.2 COOR.sup.3 (4)at pH 7-10; and a process for producing the above-mentioned alkoxycarbonylalkylthioaryl compound, which process comprises reacting the above-mentioned disulfide compound with the above-mentioned hydroxide of an alkali metal M.sup.

Abstract: Method and reagent composition for covalent attachment of target molecules, such as nucleic acids, onto the surface of a substrate. The reagent composition includes groups capable of attracting the target molecule as well as groups capable of covalently binding to the target molecule, once attracted. Optionally, the composition can contain photoreactive groups for use in attaching the reagent composition to the surface.

Abstract: This invention relates to a process for the preparation of an .alpha.-chloroketone compound comprising the steps of(i) cyclizing an alkynyl amide to form a 5-methyleneoxazoline ##STR1## (ii) chlorinating the 5-methyleneoxazoline using trichloroisocyanuric acid to produce a chlorinated oxazoline intermediate ##STR2## and (iii) hydrolyzing the chlorinated oxazoline intermediate with an aqueous acid to produce the desired monochloroketone ##STR3## wherein Z is alkyl or substituted alkyl, aryl or substituted aryl, heteroaryl or substituted heteroaryl or phenylene,R is a hydrogen atom or alkyl, andR.sup.1 and R.sup.2 are each independently an alkyl or substituted alkyl group, or R.sup.1 and R.sup.2 together with the carbon atom to which they are attached form a cyclic structure.Additionally, when R is a hydrogen atom, a dichloroketone can be conveniently formed through adjustment of reaction conditions.

Abstract: Methods and compositions for treating CF by mobilizing mutant forms of CFTR, which retain at least some functional activity, to the plasma membrane where they can mediate chloride ion transport are disclosed.

Abstract: Chiral hydroxyethylamine, hydroxyethylurea or hydroxyethylsulfonamide isostere containing retroviral protease and renin inhibitors can be prepared by multi-step syntheses that utilize key chiral amine intermediates. This invention is a cost effective method of obtaining such key chiral amine intermediates enantiomerically, diastereomerically and chemically pure. The method is suitable for large scale (multikilogram) productions. This invention also encompasses organic acid and inorganic acid salts of the amine intermediates.

Abstract: Compounds of the formula ##STR1## These compounds are useful for inhibiting the growth or replication of retroviruses such as HIV.

Abstract: Novel compounds, 1,2-N-acyl-N-methylene-ethylenediamines of formula (I) are useful as dispersants, rust inhibitors, curing promoters for epoxy resins, electroconductivity-imparting agents, mold lubricants, etc. ##STR1## where R is a hydrogen atom or a hydrocarbon group. An electroconductive paste with excellent electroconductivity and much improved long-term stability is obtained by mixing 100 parts by weight of a thermosetting resin with from 250 to 900 parts by weight of a metal filler and from 1 to 50 parts by weight of the 1,2-N-acyl-N-methylene-ethylenediamine; or by adding from 250 to 900 parts by weight of a metal filler coated with the 1,2-N-acyl-N-methylene-ethylenediamine to 100 parts by weight of a thermosetting resin.

Abstract: The invention relates to a compounds selected from these of formula (I): ##STR1## in which: R.sub.1, R.sub.2, R.sub.3 and A are as defined in the description, and a medicinal product containing the same useful for treating a melatoninergic disorder.

Abstract: The invention relates to compounds of formula ##STR1## and salts, pharmaceutical compositions, intermediates and processes of preparation thereof.

Abstract: Novel substituted fluorene compunds of Formula I are active as melatonergic agents: ##STR1## wherein: X=H, halogen, OH or OZ;Z=C.sub.1-6 alkyl; --(CH.sub.2).sub.m --CF.sub.3 (m=0-2); CD.sub.3 ; or ##STR2## n=1 or 2; and R=C.sub.1-6 alkyl, C.sub.3-6 cycloalkyl, C.sub.2-4 alkenyl, halogen substituted C.sub.1-6 alkyl, or C.sub.1-6 alkoxy substituted C.sub.1-6 alkyl.

Abstract: Preparation of N-alkenyl carboxamides of the general formula I ##STR1## in which the radicals R.sup.1 to R.sup.4 independently stand for hydrogen or for aliphatic, cycloaliphatic, or aromatic radicals, which optionally carry inert substituents, wherein an amide of the general formula II ##STR2## in which the radical R.sup.1 has the above meaning, and a carbonyl compound of the general formula III ##STR3## in which the radicals R.sup.2 to R.sup.4 have the above meanings, are caused to react in the presence of a base, said reaction being eithera) carried out in the presence of a carboxylic acid derivative of the general formula IV ##STR4## in which the radical R.sup.5 stands for hydrogen or an alkyl or aryl group and X is a halogen, alkoxy, or carboxylalkyl radical, orb) continued in the presence of a carboxylic acid derivative of the formula IV, and the amide of the formula I is isolated.

Abstract: A process comprises contacting, in the presence of a catalyst, hydrogen sulfide or a mercaptan such as, for example, n-dodecyl mercaptan with an .alpha.,.beta.-unsaturated carbonyl or .alpha.,.beta.-unsaturated cyano compound such as, for example, methyl acrylate wherein the catalyst comprises a pyridine derivative such as, for example, 4-(dimethylamino)pyridine or an ion exchange resin such as, for example, "AMBERLYST A-21" to produce a 3-hydrocarbylthio derivative of the .alpha.,.beta.-unsaturated carbonyl or .alpha.,.beta.-unsaturated cyano compound such as, for example, methyl 3-(dodecylthio)propionate.

Abstract: The present invention relates, by way of novel industrial products, to compounds which are structurally related to 15-deoxyspergualin and which have the formula ##STR1## in which: A is a single bond, a group --CH.sub.2 --, a group --CH.sub.2 O--, a group --CH.sub.2 NH--, a group --CH(OH)--, a group --CHF-- or a group --CH(OCH.sub.3)--, andn is equal to 6 or 8,and their addition salts.These novel compounds are useful especially as immunosuppressants. The invention further relates to the method of preparing said compounds.

Abstract: A method for preparing a diarylalanine compound is provided. The method includes reacting a diarylaminopropanediol with a reducing agent to form a diarylaminopropanol compound and/or contacting a serine ester derivative with an aryl metal reagent to form diarylaminopropanediol. A diarylmethyloxazolidinone compound is also provided.

Abstract: New lipopolyamines of general formula (I), their salts, their preparation and their use. ##STR1## n=1 to 5 and m=2 to 6 R represents a radical ##STR2## (R.sub.1 and R.sub.2 : aliphatic radical containing 12 to 22 carbon atoms; R: hydrogen atom or alkyl radical optionally substituted with phenyl), or a radical ##STR3## (X=CH.sub.2, CO; R.sub.3 and R.sub.4 aliphatic radical containing 11 to 21 carbon atoms), their preparation and their use.The lipopolyamines of general formula (I) are especially useful as vectors for the transfection of eukaryotic cells.

Abstract: A method of producing an aminobutene derivative of formula (I) by allowing a butenol derivative of formula (II) to react with an amide derivative of formula (III) is disclosed. The aminobutene derivative of formula (I) can be deprotected to produce an aminobutene derivative of formula (I-1) or an aminobutene derivative of formula (I-2): ##STR1## The aminobutene derivative of formula (I-A) can also be deprotected to produce the aminobutene derivative of formula (I-B). Any or all of the above aminobutene derivatives are useful as intermediates for producing anti-ulcer drugs, and anti-ulcer drugs having an inhibitory effect on gastric acid secretion based on the antagonism against histamine H.sub.2 receptor.

Abstract: The present invention provides a salicylate analogue having the structure ##STR1## wherein R is selected from the group consisting of hydrogen, methyl, ethyl, n-propyl, i-propyl, n-butyl, i-butyl; pentyl, hexyl, heptyl, octyl, nonyl, decyl, undecyl, phenyl, naphthyl and cyclohexyl; wherein R1 is selected from the group consisting of hydrogen, a C1-C12 alkyl group, F, Cl, Br, I, CO.sub.2 H, CONHR, CONR.sub.2, CO.sub.2 R, C.tbd.N, CHO, COR, SO.sub.3, SO.sub.2 NHR, SO.sub.2 NR.sub.2, OH, OR, OCOR, SH, SR, OCONHR, OCONR.sub.2, SCOR, SCONHR, SCONR.sub.2 and NH2, NHR, NHCOR and NR2; and wherein R1 is in the 3-, 4-, 5- or 6-position, or a combination thereof. Also provided are various pharmaceutical compositions of the novel compounds of the present invention.

Abstract: Certain N-acyl-cycloalkylamine derivatives are useful as melatonergic agents.

Abstract: The invention relates to a compound selected from those of formula (I): ##STR1## in which R, R.sub.1, R.sub.2 and R.sub.3 are as defined herein for use in the treatment of a disorder of the melatoninergic system.

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: Monocarboxamides of formula I ##STR1## wherein R is a radical of formula ##STR2## C.sub.9 -C.sub.19 alkyl, C.sub.9 -C.sub.19 alkenyl or C.sub.9 -C.sub.19 alkdienyl,wherein each R.sup.2 independently of the other is a hydrogen atom or C.sub.1 -C.sub.4 alkyl, each R.sup.3 independently of one another is a hydrogen atom or a hydroxyl group and at least one R.sup.3 is a hydroxyl group, and R.sup.1 is a radical of formula ##STR3## are suitable for curing epoxy resins, in ##STR4## are suitable for curing epoxy resins, in particular for cold curing.

Abstract: New melatonergic agents are phenyl alkanyl or phenyl alkyl substituted carboxamides and ureas of Formula I: ##STR1## wherein: R.sub.1 =C.sub.1-3 alkyl, allyl, C.sub.3-6 cycloalkyl substituted C.sub.1-4 alkyl;R.sub.2 =hydrogen, halogen or C.sub.1-4 alkoxy;R.sub.3 =hydrogen or C.sub.1-4 alkyl;R.sub.4 =C.sub.1-4 alkyl, C.sub.1-4 alkyl substituted amino, carboxylic acid substitutedC.sub.1-4 alkyl or C.sub.3-6 cycloalkyl, C.sub.3-6 cycloalkyl, or straight or branched chain C.sub.2-4 alkenyl;A=a linear C.sub.2-4 alkanediyl or alkenediyl chain, provided that A not be --CH.sub.2 CH.sub.2 -- when X is a bond; andX=a covalent bond or oxygen.

Abstract: There are provided with a novel N-substituted-3-halopropiolamide compound, a method of producing the compound, and a composition for controlling noxious organisms containing the compound. The present compound exhibits superior antimicrobial and antifungal effects. Pest control agents containing the compound can advantageously be used for wide applications.

Abstract: Lipid-selective antioxidants of the formula I(A).sub.a (L)(X).sub.a, (I),in whichA=an antioxidative component,L=a bridging member,X=a lipophilic componenta and a'=independently of one another the numbers 1 or 2.The compounds are used for the protection of lipid-containing substances against oxidation and in pharmaceuticals for the prophylaxis and treatment of diseases in which bioradicals are involved, in particular of coronary, circulatory and vascular diseases.

Abstract: A method for synthesizing enantiomerically enriched chemical intermediates with predetermined chirality is described. The method comprises formation of a pseudoephedrine amide, followed by stereoselective alkylation at the alpha carbon. The chiral auxiliary can then be cleaved off, affording chiral end products useful for further transformations. The enantiomeric enrichment of the chiral end products may exceed 98%, and the chiral auxiliary can be recovered. Novel amides of pseudoephedrine used in this method are also disclosed.

Abstract: A novel pseudoceramide which has improved dispersibility in aqueous solutions and which can be produced by an economical manufacturing process. The process for producing new pseudoceramides and cosmetic compositions containing the new pseudoceramides are also disclosed.

Abstract: A glycerin derivative having the following formula (I) or (I') and a pharmacologically acceptable salt thereof are useful to treat diseases caused by the platelet activating factor.

Abstract: The present invention is directed to novel amphetamine derivatives which are synthesized for the covalent attachment to antigens (proteins or polypeptides) for the preparation of antibodies or receptors to amphetamine and amphetamine metabolites. The resulting novel antigens may be used for the production of antibodies or receptors using standard methods. Once generated, the antibodies or receptors and the novel derivatives which are covalently attached to proteins, polypeptides or labels may be used in the immunoassay process.

Abstract: The invention relates to a process for preparing optically active methionine amide in high ee purities in which a mixture of D- and L-methionine amide or the Schiff bases thereof is at least partly converted, optionally in the presence of 0.5-4 equivalents of an aldehyde, relative to the amount of methionine amide, and water, in the presence of an organic solvent, using less than 1.2 equivalents of L- or D-mandelic acid, respectively, relative to the amount of D- or L-methionine amide, respectively, or the Schiff bases thereof, present in the mixture of D- and L-methionine amide or the Schiff bases thereof, into a salt of methionine amide and mandelic acid, a portion consisting substantially of one of the diastereoisomers of the salt is separated from the reaction mixture obtained, and the salt is converted into the optically active methionine. A high degree of optical purity is obtained.