Abstract: A highly storage-stable composition for vaginal administration of clindamycin is disclosed which is useful for the treatment of bacterial vaginosis. The composition is a vaginal suppository containing an antimicrobially effective amount of clindamycin dispersed in a Hard Fat NF suppository base. Hard Fat NF suppository bases provide a clindamycin product having long term storage stability while providing efficacy against bacterial vaginosis which is equivalent to clindamycin vaginal creams.

Abstract: A method of producing .alpha.-tocopherol from non-.alpha.-tocopherols is disclosed. In the disclosed method, non-.alpha.-tocopherols are hydroxymethylated and reduced to .alpha.-tocopherol in a single step by reacting formaldehyde or a formaldehyde-producing compound with the non-.alpha.-tocopherol under catalytic reducing conditions in a reaction mixture containing the non-.alpha.-tocopherol, formaldehyde or formaldehyde-producing compound and boric acid or a boric acid-producing compound dispersed in a solvent of an azeotropic mixture of trimethyl borate and methanol and a non-polar organic solvent.

Abstract: The present invention is directed to a method for making in vivo a lecithin gel which provides for the sustained release of a biologically active compound contained in the gel. The present invention is also directed to a method for the sustained treatment of a human or other mammal with a therapeutic amount of a biologically active compound using the gel for the sustained release of the biologically active compound.

Abstract: Compounds of formula I: ##STR1## are disclosed. The compounds inhibit the binding of endothelin to its receptors.

Abstract: A process for stabilizing fully or partially refined marine oil is disclosed. Here marine oil is treated with silica having a surface area greater than 500 m.sup.2 per gram. Then the silica treated oil is soft vacuum steam deodorized at a temperature between 140.degree. C. and about 210.degree. C. Finally the oil is treated with a combination of lecithin, ascorbyl palmitate and tocopherol in ratios of 6-3:4-2:8-4 the range of 1000 parts per million to 4000 parts per million.

Abstract: The present invention is directed to a process, and novel intermediates used in the manufacture of, dicarboxamides of the formula I ##STR1## wherein A, G, L, Q, X and Y have the meaning given in the specification, starting from corresponding N-substituted aspartic acid and from corresponding amines G-NHCH(X,Y), via corresponding N-substituted oxazolidinone and N,N-substituted aspartates.

Abstract: A process for the conversion of the sodium salt of 2-keto-L-gulonic acid, which is present in an aqueous fermentation solution, into an alcoholic solution of the free acid and, if desired, into an alkyl ester of the acid comprises a) recovering the sodium 2-keto-L-gulonate monohydrate from an aqueous fermentation solution by crystallization involving evaporation, cooling or displacement and, if desired, pulverizing the thus-obtained crystallizate by grinding, b1) suspending the optionally ground sodium 2-keto-L-gulonate monohydrate obtained in step a) in a lower alcohol, leaving the crystals to swell and thereafter adding an acid of low water content, whereby the measured pH value should lie above 1.5, or b2) adding the optionally ground sodium 2-keto-L-gulonate monohydrate obtained in step a) together with an about stoichiometric amount of an acid of low water content to a lower alcohol using a wet grinding system, whereby the measured pH value should lie above 1.

Abstract: New carotenoids of the formula ##STR1## wherein R and n have the significances given herein, are useful for pigmenting the egg yolk, integuments and/or subcutaneous fat of poultry and the meat and/or integuments of fish and crustacea when included in the feed of the poultry, fish or crustacea. As well as such carotenoids and method of pigmenting the invention further embraces the pertinent carotenoid-enriched feed for poultry, fish or crustacea, the premixes for incorporation in such feeds and beadlets containing one or more of these carotenoids for incorporation in such premixes and the use of the carotenoids in the pigmenting method. The process of manufacturing such carotenoids, which more specifically may be designated as carotenoid ketones, monoesters and diesters, also represents an aspect of the invention.

Abstract: (Z)-1?1-(4-Methoxybenzylidene)-1,2,3,4,5,6,7,8-octahydro-isoquinolin-2-yl!a lkanones of the formula ##STR1## wherein R is lower alkanoyl, can be produced under specific reaction conditions in a one-pot process in an advantageous manner by a Bischler-Napieralski cyclization of N-(2-cyclohex-1-enylethyl)-2-(4-methoxyphenyl)-acetamide and subsequent lower-alkanoylation of the resulting 1-(4-methoxybenzyl)-3,4,5,6,7,8-hexahydro-isoquinoline of the formula ##STR2## under an inert gas atmosphere and, if desired converted to dextomethorphan in a known manner.

Abstract: The process for manufacturing ascorbic acid 2-mono-phosphates from ascorbic acid 2-polyphosphates, in particular 2-triphosphates by subjecting the ascorbic acid 2-triphosphates to drying conditions.

Abstract: A method for the detection of poor metabolizers of drugs using PCR technology is described comprising a) optionally amplifying a gene coding for an enzyme known to be responsible for the metabolization of drugs, thereby separating it from possible closely related pseudogens, b) amplifying different allelic forms of the gene of step a) and c) detecting the product of step b). Primers for amplification of the genes responsible for the debrisoquine or acetylation phenotype are also disclosed.

Abstract: A process for oxidizing primary and secondary alcohols to the corresponding aldehydes and ketones is disclosed. The oxidation is carried out by reacting the primary or secondary alcohol with an organic N-chloro compound oxidizing agent in the presence of a catalyst of the formula: ##STR1## wherein the substituent groups are as defined in the specification.

Abstract: Compounds of formula (I) wherein R.sup.1 -R.sup.7, R.sup.10, X and the dotted bond have the meaning given in the specification, bind selectively to retinoid RXR receptors and are useful as antiproliferative agents for dermatological and oncological indications.

Abstract: A method of reducing neurotoxic injury due to acute or chronic neurological insults by administering an anthranilic acid derivative is disclosed.

Abstract: A novel process for the manufacture of a .gamma.-halotiglic aldehyde HalH.sub.2 C--CH.dbd.C(CH.sub.3)--CHO ?I!, wherein Hal signifies chlorine or bromine, comprises haloalkoxylating a 1-alkoxy-2-methyl-1,3-butadiene H.sub.2 C.dbd.CH--C(CH.sub.3).dbd.CH--OR.sup.1 ?II!, wherein R.sup.1 signifies C.sub.1-4 -alkyl, using a particular halogenating agent in a C.sub.1-4 -alkanol (R.sup.2 OH) and hydrolyzing the thus-obtained .gamma.-halotiglic aldehyde dialkyl acetal HalH.sub.2 C--CH.dbd.C(CH.sub.3)--CH(OR.sup.1)(OR.sup.2) ?III! to the desired .gamma.-chloro- or .gamma.-bromotiglic aldehyde I. The halogenating agent used in this process is selected from an alkali metal hypochlorite, an alkali metal hypobromite, an alkaline earth metal hypochlorite, an alkaline earth metal hypobromite, tert.butyl hypochlorite, N-bromoacetamide, 1.3-dichloro-5,5-dimethylhydantoin and 1,3-dibromo-5,5-dimethylhydantoin. Further aspects of the present invention are the use of the thus-manufactured .gamma.

Abstract: A process for the conversion of lutein or of its esters into zeaxanthin by base-catalyzed isomerization is disclosed. The process is carried out by heating an optionally pre-treated lutein-containing material in a mixture of an aqueous solution of an alkali hydroxide and either dimethyl sulphoxide or an organic solvent based on saturated aliphatic and/or aromatic hydrocarbons at temperatures in the range from about 50.degree. C. to about 120.degree. C. The process is carried out in the presence of a phase transfer catalyst when an organic solvent based on hydrocarbons is used. Being carotenoids, lutein and zeaxanthin are used correspondingly, especially as pigments for egg yolk, the integuments and the subcutaneous fat of poultry, the flesh and the integuments of fish and crustaceans, as well as foodstuffs. Zeaxanthin is preferably used in many applications, since in comparable dosages it produces a more intensive golden yellow pigmentation than lutein.

Abstract: Novel processes and intermediates useful for the manufacture of the Wittig ester salts are disclosed. The Wittig ester salts are known as important C.sub.5 building blocks for the manufacture of various polyenecarboxylic acid esters in the field of carotenoid chemistry.

Abstract: The compounds of formula I ##STR1## wherein R.sup.1 -R.sup.9, R.sup.15, A, X, Y, Z and n have the meaning given in the specification are active as protein kinase inhibitors and can be used as medicaments, particularly for the treatment of inflammatory skin disorders and alopecia.

Abstract: A process is disclosed for the manufacture of amides, including peptides, in which a carboxylic acid is reacted with a primary or secondary amine in the presence of a carbodiimide and a catalytic amount of N-hydroxy compound.

Abstract: A D-sorbitol dehydrogenase in homogenous form, which catalyzes the oxidation of D-sorbitol to L-sorbose, has a molecular structure consisting of homologous subunits of molecular weight 79,000.+-.5,000 each, a substrate specificity for polyols and an optimum pH of 6.0-7.0. Said D-sorbitol dehydrogenase is producible by a process comprising cultivating a microorganism belonging to the genus Gluconobacter or Acetobacter, or a mutant or variant thereof, which is capable of producing the D-sorbitol dehydrogenase in the cells and isolating it from the cells, e.g. by disrupting the cells and isolation from cell-free extract of the disrupted cells. The so-isolated D-sorbitol dehydrogenase is useful for catalyzing the oxidation of D-sorbitol to L-sorbose, the latter being an important intermediate for the production of vitamin C.