Abstract: Disclosed are compounds which inhibit .beta.-amyloid peptide release and/or its synthesis, and, accordingly, have utility in treating Alzheimer's disease. Also disclosed are pharmaceutical compositions comprising a compound which inhibits .beta.-amyloid peptide release and/or its synthesis as well as methods for treating Alzheimer's disease both prophylactically and therapeutically with such pharmaceutical compositions.

Abstract: Modulators of neurotransmitter release including substituted guanidines, N"-aminoguanidines, and N,N'N",N"'-tetrasubstituted hydrazinedicarboximidamides, and pharmaceutical compositions thereof are disclosed. Also disclosed are methods involving the use of such neurotransmitter release modulators for the treatment or prevention of pathophysiologic conditions characterized by the release of excessive or inappropriate levels of neurotransmitters. Also disclosed are screening assays for compounds which selectively inhibit glutamate release. Also disclosed are methods of blocking voltage sensitive sodium and calcium channels in mammalian nerve cells.

Abstract: The present invention relates to a process to aminate electrophilic aromatic compounds by vicarious nucleophilic substitution of hydrogen using quaternary hydrazinium salts. The use of trialkylhydrazinium halide, e.g., trimethylhydrazinium iodide, as well as hydroxylamine, alkoxylamines, and 4-amino-1,2,4-triazole to produce aminated aromatic structures, such as 1,3-diamino-2,4,6-trinitrobenzene (DATB), 1,3,5-triamino-2,4,6-trinitrobenzene (TATB) and 3,5-diamino-2,4,6-trinitrotoluene (DATNT), is described. DATB and TATB are useful insensitive high explosives. TATB is also used for the preparation of benzenehexamine, a starting material for the synthesis of novel materials (optical imaging devices, liquid crystals, ferromagnetic compounds).

Abstract: The present invention relates to a method of forming a 1,3-diamino-3-substituted-2-propanol chemical intermediate from which various chemicals, such as selected protease-inhibitors and other drugs, as well as polymers, can be synthesized.The method includes contacting a nitromethyl amino acid compound with at least one reducing agent to form the 1,3-diamino-3-substituted-2-propanol chemical intermediate.

Abstract: This invention is directed to compounds of formula I: ##STR1## wherein the variables are as described herein. Compounds within the scope of the present invention possess useful properties, more particularly pharmaceutical properties. They are especially useful for inhibiting the production or physiological effects of TNF in the treatment of a patient suffering from a disease state associated with a physiologically detrimental excess of tumor necrosis factor (TNF). Compounds within the scope of the present invention also inhibit cyclic AMP phosphodiesterase, and are useful in treating a disease state associated with pathological conditions that are modulated by inhibiting cyclic AMP phosphodiesterase, such disease states including inflammatory and autoimmune diseases, in particular type IV cyclic AMP phosphodiesterase.

Abstract: Phytosanitary composition for use especially in affording protection to plants from undesirable plant species. The composition is characterized in that it contains at least one benzamidic compound associated with at least one cyclodextrine to improve mobility in the ground and/or the biological afficacy of the benzamidic derivative. The invention also concerns a method of preparing the phytosanitary composition.

Abstract: The invention relates to herbicidal compositions comprising:(a) a 4-benzoylisozaxole of formula I: ##STR1## wherein R, R.sup.1 and R.sup.2 are as defined in the description and (b) a chloroacetamide herbicide.

Abstract: The invention relates to an herbicidal composition comprising N-[2-(3,3,3-trifluoropropyl)-phenylsulfonyl]-N'-(4-methoxy-6-methyl-1,3,5- triazin-2-yl)-urea or an agrochemically tolerated salt thereof, and a synergistic amount of an herbicide which is 3,5-dibromo-4-hydroxybenzonitrile or 3,6-dichloro-2-methoxybenzoic acid.

Abstract: A continuous process for the preparation of 2-hydroxy-4-methylthiobutanoic acid which includes introducing sulfuric acid into a first reactor including a continuous stirred tank reactor and introducing 2-hydroxy-4-methylthiobutanenitrile into the first reactor. 2-hydroxy-4-methylthiobutanenitrile is continually hydrolyzed within the first reactor to produce an intermediate aqueous hydrolysis solution containing 2-hydroxy-4-methylthiobutanamide. The intermediate aqueous hydrolysis solution is continuously introduced into a plug flow reactor. 2-hydroxy-4-methylthiobutanamide is continually hydrolyzed within the plug flow reactor to produce an aqueous hydrolyzate product solution containing 2-hydroxy-4-methylthiobutanoic acid. 2-hydroxy-4-methylthiobutanoic acid is recovered from the aqueous hydrolyzate product solution.

Abstract: Compounds of the formula (I) and their salts with inorganic and organic acids, ##STR1## in which R.sub.1 is a hydrogen atom or a trimethylsilyl group, R.sub.2, R.sub.3, R.sub.4, and R.sub.5 are, independently of each other, a hydrogen atom, a (C.sub.1 -C.sub.4) alkyl group, a hydroxy-(C.sub.2 -C.sub.3) alkyl group, an alkoxy-(C.sub.2 -C.sub.3) group, an amino-(C.sub.2 -C.sub.3) group, or a 2,3-dihydroxypropyl group, and in which R.sub.1, R.sub.2, R.sub.3, R.sub.4 and R.sub.5 are not simultaneously hydrogen atoms, and processes for their preparation and use as hair-coloring agents.

Abstract: The subject invention provides a method of preparing an allylic amine having the structure: ##STR1## wherein R.sub.1, R.sub.2, R.sub.3, R.sub.4 and R.sub.5 are each independently hydrogen, halogen, cyano, nitro, linear or branched chain alkyl, aryl, etc.; wherein each alkyl or arylalkyl if present is independently unsubstituted or substituted by fluoro, cyano, nitro, linear or branched chain acyl, dialkylamino, etc.; wherein each aryl if present is independently unsubstituted or substituted by fluoro, cyano, nitro, linear or branched chain alkyl, arylmercapto, etc.; and wherein each of R.sub.1, R.sub.2, R.sub.3, R.sub.4 and R.sub.5 optionally is covalently bonded linking pairwise a suitable atom from each to form from 0 to about 10 rings, wherein each ring contains between about four and about twelve atoms, using disubstituted sulfur diimides prepared in situ. Also provided are methods of preparing cyclic allylic amines in which allylic double bonds are endocyclic and exocyclic.

Abstract: This invention relates to the use of a family of chiral .alpha.-substituted benzylamine reagents during chemical synthesis. Specifically, the reagents can be used in an auxiliary manner to deliver either a substituted or unsubstituted nitrogen atom while simultaneously bestowing an asymmetric bias toward the formation and separation of the diastereomeric intermediates that result from reaction of the reagents with racemic substrates also having one or more asymmetric atoms. The chiral auxiliary portion of the reagents can then be readily removed at some later and convenient stage of the overall synthetic scheme. The initial nitrogen-delivery reaction, asymmetric separation procedures, and removal of the chiral auxiliary can all be conducted under routine experimental conditions, including the final debenzylation, such that the overall method is adaptable to large-scale chemistry.

Abstract: A process for producing diamines by reacting a dialdehyde with ammonia and hydrogen in the presence of a hydrogenation catalyst to produce the corresponding diamine, where a solvent comprising an alcohol is used in the reaction and the concentration of water in the reaction mixture is 5 to 15% by weight.

Abstract: A process for preparing an enantiomeric form of 2-amino-3-(4-alkylaminophenyl)-propanoic acid of formula (I) or a salt thereof: ##STR1## in which Alk represents an alkyl radical containing 1 to 2 carbon atoms, from (L)-phenylalanine to obtain the (S)-enantiomer of 2-amino-3-(4-alkylaminophenyl)-propanoic acid, or from (D)-phenylalanine to obtain the (R)-enantiomer of 2-amino-3-(4-alkylaminophenyl)propanoic acid.

Abstract: Provided a process for producing higher content of trans 1,4-bis(aminomethyl)cyclohexane which is used as the raw material for producing polyamides or polyurethanes having physically and chemically excellent properties from 1,4-bis(aminomethyl)cyclohexane which is generally produced by hydrogenation of p-xylylenediamine.That is, a mixture of cis and trans 1,4-bis(aminomethyl)cyclohexane is isomerized by heating at 120 to 250.degree. C. in the presence of a platinum group catalyst to change to trans isomer. 1,4-bis(aminomethyl)cyclohexane containing more than 80% trans isomer is produced by combining this isomerization technique and crystallization technique.

Abstract: The present invention provides a process for effectively racemizing an amine compound in which an asymmetric carbon is located at the .beta.-position of the amino group or more distant therefrom, which comprises reacting the amine compound with a complex of an alkali metal and a polycyclic aromatic hydrocarbon.

Abstract: The present invention relates to a process for the preparation of 3,5-difluoroaniline by reacting 3,5-difluorochlorobenzene with ammonia in the presence of a solvent in the presence of a copper compound and at least one metal selected from the group consisting of copper, iron, cobalt, nickel, chromium, molybdenum and zinc, at 100 to 250.degree. C.

Abstract: The present invention includes purified and isolated quassinoids and synthetically derived quassinoid analogs based on a picrasane carbon skeleton. Novel sidechains at C-15 incorporating water solubilizing agents such as glycine are discussed. Therapeutic methods taking advantage of anticancer, antiviral, and herbistatic properties of these quassinoids are disclosed, including use against solid tumors and human immunodeficiency virus infected cells.

Abstract: Disclosed are compounds which inhibit .beta.-amyloid peptide release and/or its synthesis, and, accordingly, have utility in treating Alzheimer's disease. Also disclosed are pharmaceutical compositions comprising a compound which inhibits .beta.-amyloid peptide release and/or its synthesis as well as methods for treating Alzheimer's disease both prophylactically and therapeutically with such pharmaceutical compositions.

Abstract: An .alpha.-hydrazino acid derivative of general formula (I) is described, wherein R.sub.1, R.sub.2, R.sub.3 are hydrogen or a carbon radical, such that when R.sub.2 and R.sub.3 are different, C* is an asymmetric carbon of L, D or DL configuration, and R.sub.4 and R.sub.5 are a protecting group, characterized in that R.sub.4 is a benzyl ArCH.sub.2 radical of formula (a), wherein Ar is a phenyl radical or phenyl substituted by one or more X groups; X being hydrogen, halogen, a nitro or alkyl radical; and in that R.sub.5 is a Y--O--CO group, where Y is a carbon radical different from R.sub.4.