Abstract: The invention is directed to a process and intermediates for the preparation of 1.alpha.,23(S),25-trihydroxycholecalciferol and 1.alpha.,23(R),25-trihydroxycholecalciferol. The end-products, 1.alpha.,23(S),25-trihydroxycholecalciferol and 1.alpha.,23(R),25-trihydroxycholecalciferol, are useful for the treatment of disease states which are characterized by insufficient amounts of 1,25 dihydroxycholecalciferol.

Abstract: Veterinarian composition for the treatment of herpes virus in animals comprising a pyrimidine nucleoside, or veterinarianically acceptable acid addition salte thereof, of the formula ##STR1## wherein A is OR.sup.3, SR.sup.3, NR.sup.3 R.sup.4 or NHacyl wherein R.sup.3 and R.sup.4 are the same or different and are hydrogen, lower alkyl of 1 to 7 carbon atoms, aralkyl, or aryl;NHacyl is alkanoyl or aroyl amide;B is oxygen or sulfur;X is halogen, alkylsulfonyl or arylsulfonyl;Y is halogen, amino, monoalkyl- or monoaralkylamino, dialkylamino, aminomethyl, hydroxymethyl, lower alkyl, aryl, aralkyl, vinyl and substituted vinyl or ethynyl and substituted ethynyl;Z is methyne or nitrogen;R.sup.1 and R.sup.2 are the same or different and are hydrogen acyl or aroyl,in a veterinarianically acceptable carrier.

Abstract: A class of novel azole dinucleotide compounds and methods for their production are provided. Compounds of the class typically have pharmacological properties and are well tolerated, being useful, for example, in treating leukemias in warm blooded animals.

Abstract: Antiviral (3-ethoxypropionate) esters of (+)-cyclaradine having the formula: ##STR1## In the monoester Ry and Rz are hydrogen. In the diester Ry is the 3-ethoxypropionyl group and Rz is hydrogen. In the triester, Ry and Rz are each 3-ethoxypropionyl groups.

Abstract: Compounds having the formula ##STR1## wherein ##STR2## R.sub.1 is hydrogen, benzyl or alkanoyl, X is C.sub.2-4 alkylene; andZ-W is alkyl, phenylalkyl or pyridylalkyl which can have an oxygen atom as part of the alkyl chain and their use as CNS agents, antidiarrheals and antiemetics. Processes for their preparation and intermediates therefor are described.

Abstract: The present invention relates to a method for preparing inner ester derivatives of gangliosides and pharmaceutical compositions containing such derivatives to be used in treating disorders of the nervous system. The pharmaceutical compositions of the present invention promote nerve regeneration by stimulating nerve sprouting.

Abstract: N.sup.6 -Tricyclic adenosines and pharmaceutically acceptable acid addition salts having highly desirable central nervous system and cardiovascular properties, processes for their manufacture and pharmaceutical compositions and methods for using said compounds and compositions are described.

Abstract: This invention relates to quercetin or fisetin derivatives substituted on the oxygen in the 3 position by groups such as lower alkyl, cycloalkyl, methanesulfonyl or paratoluenesulfonyl.The derivatives substituted by methanesulfonyl or paratoluenesulfonyl are obtained from a 3-O-glycoside whose phenol OH groups are blocked in the form of benzoate, and from which the OH in the 3 position is released by the action of concentrated HCl; this OH is esterified by mesityl chloride or paratoluenesulfonic acid chloride, and the benzoate groups are eliminated by soda treatment. The O derivatives substituted by alkyl or cycloakyl are prepared from a suitably substituted acetonitrile or metadiphenol; the resulting derivative reacts with 3,4-dibenzyloxybenzoic acid and the resulting flavone is debenzylated by hydrogenolysis.The derivatives, object of this invention, are useful in preventive or curative therapy of ocular and nervous complications from diabetes and are also useful as hypolipidemic or hypoglycemic agents.

Abstract: Sulfamates of the following formula (I): ##STR1## wherein R.sup.1 and R.sup.2 are as herein defined have been found to exhibit anticonvulsant activity and are thus useful in the treatment of conditions such as epilepsy. Further, pharmaceutical compositions containing a compound of formula (I) as well as methods for their use and intermediates form part of the present invention.

Abstract: Dioxolane and benzodioxin derivatives, intermediates therefor, synthesis thereof, and the use of the compounds for the control of pests.

Abstract: Processes for preparing (S) or (R) epihalohydrin and an (S) substituted glycerol intermediate are disclosed.

Abstract: The present invention pertains to a process for preparing ketones employing a silica catalyzed oxidation of a secondary alcohol with calcium hypochlorite in acetonitrile.

Abstract: A method of combating arthropods, comprising applying to the arthropods, or to a habitat infested therewith an arthropodicidally effective amount of an antibiotic which (a) is colorless, very readily soluble in water and in pyridine but insoluble in other customary organic solvents, gives a positive reaction with ninhydrin, sodium metaperiodate/benzidine and potassium permanganate and gives a yellow coloration with iron (III) chloride, (b) has the UV and IR spectra substantially as shown in FIGS. 1 and 2, (c) on chemical degradation yields uracil, an amino-hexuronic acid and an amino-acid containing a pyridine ring, (d) on paper electrophoresis proves to be an amphoteric substance and has an isoelectric point at about pH 6 and (e) consists of the elements carbon, hydrogen, oxygen and nitrogen, or one or more active components of the antibiotic mixture, the active agent being applied alone or in admixture with a diluent or carrier.

Abstract: Beta-glycosyl C-nucleoside compounds showing growth inhibitory activity against leukemic cells, of the following formula, are provided: ##STR1## wherein X is NR.sub.10, S or OR.sub.10 is H or alkyl with 1 to 6 carbon atoms. ##STR2## wherein R.sub.6, R.sub.7 and R.sub.8 are independently selected from H or alkyl of 1 to 6 carbon atoms; or ##STR3## wherein R.sub.16, R.sub.11 and R.sub.12 are independently selected from H or alkyl of 1-6 carbon atoms;R.sub.3 is OH, SR.sub.13, or OR.sub.9 ;R.sub.4 is OH, SR.sub.14, or OR.sub.15 ;R.sub.9, R.sub.13, R.sub.14 and R.sub.15 are individually selected from C.sub.1 -C.sub.6 alkyl and C.sub.1 to C.sub.6 acyl;R.sub.5 is OH or H,R'.sub.5 is OH or H with the provison that at least one of R.sub.5 or R'.sub.5 is H; excluding 2-deazoxoformycin; andHCl salts thereof.

Abstract: A method for treating schizophrenia without precipitating neurological side effects such as extrapyramidal syndrome and tardive dyskinesia by administering prior to or concomitantly with haloperidol a diphenylalkyladenosine or diphenylalkyl-2-amino-adenosine is described as well as pharmaceutical compositions therefor.

Abstract: There is described a novel process for producing hydroquinone derivatives of the formula ##STR1## wherein R is an ether protecting group, and their conversion into d-.alpha.-tocopherol, starting from compounds of the formula ##STR2## wherein R is an ether protecting group and R.sup.1 is hydrogen or an ether protecting group.

Abstract: Benzo-fused, tetrachlorinated heterocyclic compounds are prepared by first reacting pyrocatechol or a pyrocatechol derivative with tetrachloroethylene carbonate, with the addition of a tertiary amine, and then adding phosphorus pentachloride, without intermediate isolation.

Abstract: Thermally-denatured DNA MD-011 having an antitumor activity was obtained by heating the substance separated from the disrupted cells of bacteria belonging to genus Mycobacterium.

Abstract: New process for preparing the pheromone active compound lineatin (3,3,7-trimethyl-2,9-dioxatricyclo[3,3,1,0.sup.4,7 ]-nonane), by reacting a 2,2-dimethyl-3,4-pentadienal of formula 1, in which R.sub.1 and R.sub.2 is each hydrogen or lower alkyl, with .beta.-methylallyl magnesium halide; the formed 2,5,5-trimethylocta-1,6,7-trien-4-ol derivative of formula 2 is subjected to oxidation which does not attack the double bonds; the formed 2,5,5-trimethylocta-1,6,7-trien-4-one derivative of formula 3 is subjected to pyrolysis; the formed 1,4,4-trimethyl-6-methylenebicyclo[3,2,0]heptan-3-one derivative of formula 4 is subjected to oxidation; the resulting 5,5,9-trimethyl-2,6-dioxa-7-oxo-bicyclo[4,2,0]octylspiro[2,7]-decane derivative of formula 5 is subjected to oxidation; the resulting 1,5,5-trimethyl-4-oxabicyclo[4,2,0]-octan-3,7-dione of formula 6 is reduced in a per se known manner to lineatin of formula 7. Compounds 2, 3, 4 and 5 are novel.

Abstract: The invention concerns a method for the synthesis of 6'-ethyl spectinomycin and analogs thereof, including intermediates utilized in the method. The method comprises converting an enamine by a Grignard addition to various novel dienones not hitherto known. The dienones are then hydrogenated and deblocked to obtain 6'-ethyl spectinomycin and analogs thereof. The 6'-ethyl spectinomycin and analogs thereof prepared by the invention exhibit especially good antibacterial activity.