Abstract: The invention relates to new phosphorylating agents, a process for producing said compounds and their use in a process for the phosphorylation of organic hydroxyl compounds to obtain intermediate products useful for the production of polynucleotides. The phosphorylation is achieved without side reactions at the purine- or pyrimidine bases.

Abstract: This invention provides novel aminopolyol derivative represented by the general formula ##STR1## wherein each of R and R' represents a hydrogen atom, or an alkyl or aryl group or R and R', taken together, form an alkylene group, R.sup.1 represents a lower alkyl group, R.sup.2 represents a hydrogen atom or an acyl group, and R.sup.3 represents a lower alkyl group; and a process for production thereof.The aminopolyol derivatives of formula (I) are useful as intermediates for the synthesis of amino sugars such as 3-epi.daunosamine, acosamine, ristosamine and daunosamine which is the sugar moiety of daunomycin useful as an anti-cancer agent.

Abstract: Cyclopropane derivatives of the formula ##STR1## wherein Ar is phenyl or phenyl monosubstituted or polysubstituted by F, Cl, Br, C.sub.1-4 alkyl, C.sub.1-4 alkoxy, C.sub.2-4 alkenyloxy, C.sub.1-4 alkylthio, OH, SH, CN, methylenedioxy or CF.sub.3 ; and R is H, C.sub.1-4 alkyl or benzyl, or a physiologically acceptable acid addition salt thereof, have valuable pharmacological properties, e.g., as antidepressants.

Abstract: The invention relates to novel dioxaheterocyclic compounds of the formula I ##STR1## in which R.sub.1 represents an unsubstituted or substituted aromatic or heteroaromatic radical or an unsubstituted or lower alkylated, mono- or bi-cyclic cycloaliphatic hydrocarbon radical or an .alpha.-branched aliphatic hydrocarbon radical, each of R.sub.2 and R.sub.3, independently of the other, represents hydrogen or lower alkyl, and each of R.sub.4 and R.sub.5, independently of the other, represents hydrogen, lower alkyl or halogen, and A represents the radical --O--R.sub.6, wherein R.sub.6 represents hydrogen or an unsubstituted or substituted aliphatic or araliphatic hydrocarbon radical or A represents the radical ##STR2## in which each of R.sub.7 and R.sub.8, independently of the other, represents hydrogen or lower alkyl, or R.sub.7 and R.sub.

Abstract: Disclosed herein are 1-aminomethyl-phthalans represented by the formula ##STR1## wherein R, R.sub.1, and R.sub.2 are independently selected from hydrogen, hydroxy, loweralkoxy of 1 to 3 carbon atoms, loweralkenyloxy of 1 to 3 carbon atoms, thiomethyl, halo, or ##STR2## wherein R.sub.5 and R.sub.6 are independently selected from hydrogen, loweracyl of 1 to 4 carbon atoms or sulfonyl of the formula ##STR3## wherein R.sub.7 is loweralkyl of 1 to 4 carbon atoms; or R and R.sub.1, or R.sub.1 and R.sub.2 can be taken together to form a methylenedioxy or ethylenedioxy bridge; with the proviso that at least one of R, R.sub.1 or R.sub.2 must be other than hydrogen; and R.sub.3 and R.sub.4 are independently selected from hydrogen; loweralkyl of 1 to 4 carbon atoms; halo-substituted loweralkyl of 1 to 4 carbon atoms; arylalkyl of the formula ##STR4## wherein m is 0, 1 or 2, p is 0 or 1, R.sub.8 is hydrogen or loweralkyl of 1 to 4 carbon atoms and R.sub.9 and R.sub.

Abstract: Tensio-active cyclic polyethers of the general formula: ##STR1## where A refers to a hydrophile block chosen from the amine, ammonium, ammonio alkyl carboxylate, ammonio alkyl sulfonate, amide, sulfonamide, ether, thioether, hydroxyl, ester and acid groupings.These polyethers may be prepared (1) by reaction of alcohol or of undecylenic acid with thioacetic acid, (2) saponification with an alkaline base, (3) reaction of the product obtained in (2) with the tetramer of epichlorohydrin or of epibromohydrin, (4) reaction of mesylate or tosylate of the compound obtained in (3) either (a) with dimethylamine or methylethanolamine, the resulting compound being able to be salified or alkylated, or (b) with the mercapto ethanol or mercapto glycerol; the compounds thereby obtained being then able to be submitted to reactions of polyaddition of ethylene oxide and/or of glycidol oxide.These tensio-active cyclic polyethers are suitable for use in the cosmetic, textile, insecticide and similar industries.

Abstract: Perfluoro(2,2-dimethyl-1,3-dioxole) forms oligomers on standing in the presence of an ether. The preferred ethers are aliphatic and cycloaliphatic, especially tetrahydrofuran. Free radical generators, especially peroxydicarbonates, may be added to the reaction medium. The oligomers have a degree of polymerization of about 2-8. They are useful as lubricants, hydraulic fluids, heat transfer agents, and plasticizers, and as intermediates to oligomeric acid fluorides and acids, which acids are useful surfactants.

Abstract: The invention relates to an oligosaccharide which contains 4-8 monosaccharide units and which is characterized in that it contains at least one glucosamine unit which is 3-0-sulfated, and at least one additional glucosamine unit, whereby these units are linked via an intermediate monosaccharide unit, which is bound to the reducing end of the 3-0-sulfated glucosamine unit. The invention further relates to a pharmaceutical composition containing one or more such oligosaccharides, and to a process for the preparation of these oligosaccharides.

Abstract: Perhalogenated dioxoles, halogenated dioxolanes, a process for making the dioxoles and dioxolanes, and polymers of dioxole and dioxolane monomers.

Abstract: This invention relates to new organic compounds that are prodrugs of the antiviral agent Ara-A which is 9-(.beta.-D-arabinofuranosyl)adenine. These compounds by virtue of their high lipid solubility will penetrate the stratum cornium and on entry the enzymatic cleavage will regenerate the antiviral compound Ara-A.

Abstract: The novel antibiotic, oxanosine, having the structure ##STR1## inhibits the growth of Gram-negative bacteria and has antiviral activity. It is produced by cultivation of an oxanosine-producing microorganism of the genus Streptomyces, preferably Streptomyces capreolus MG265-CF3, ATCC No. 31963.

Abstract: A new dioxolanic amine is disclosed, with pharmacological activity of the following structural formula I: ##STR1## as well as its pharmaceutically acceptable salts, possessing intense vasodilatory, anti-angina and anti-arrhythmic activity, accompanied by a low toxicity; its method of preparation; pharmaceutical compositions containing the said compounds; and the treatment and prevention various pathological conditions with the use of said compositions. Also disclosed are new dioxolanic compound of the following structural formula II: ##STR2## which is an intermediate compound in the preparation of the formula I compound; and its method of preparation.

Abstract: The invention relates to novel oxime derivatives of diphenyl ethers of the formula ##STR1## wherein Q is an aliphatic or araliphatic ether or ester radical, R.sub.1 is halogen or a nitro, cyano or trifluoromethyl group, each of R.sub.2 and R.sub.3 is hydrogen, halogen or a nitro or cyano group, R.sub.4 is hydrogen or halogen and X is hydrogen, halogen or a member selected from the group consisting of cyano, nitro, lower alkyl, lower alkanoyl, carboxylic acid lower alkyl ester or carboxamide. These compounds have good selective herbicidal action, they inhibit plant growth, and can be employed as safeners for protecting cultivated plants from the phytotoxic action of aggressive agrochemicals.

Abstract: Described is a process for preparing solanone and norsolanadione using chemical intermediates: which provide an organoleptically improved smoking tobacco product and additives therefor.

Abstract: A chondroitin or a chondroitin sulfate covalently or ionically bonded to a drug substance of the group consisting of chloramphenicol, methotrexate, adriamycin, vinblastine, vincristine, vindesine, 6-mercaptopurine, 5-fluorouracil, the penicillin antibiotics, the cephalosporin antibiotics, and the 1-oxacephalosporin antibiotics to form a prodrug which, when injected into animal tissue, undergoes natural conversion in the physiological environment to provide controlled release of the drug or an active drug complex.

Abstract: A novel antitumor agent designated herein as rebeccamycin is produced by fermentation of Nocardia aerocolonigenes (ATCC 39243). Rebeccamycin and its 5'-N-methyl and 5',2",3",6"-tetraacetate derivatives exhibit activity against experimental animal tumor systems.

Abstract: Compounds having the formula ##STR1## 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 invention provides an organoleptically improved smoking tobacco product and additives therefor as well as methods of making the same.

Abstract: Diseases and ailments accompanied by gastric and gastroduodenal lesions treated by administering a compound of the formula (I) ##STR1## in which R represents hydrogen or alkyl containing 1 to 5 carbon atoms and R.sub.1 and R.sub.2, identical or different, both represent alkoxy containing 1 to 3 carbon atoms, or both represent halogen, or R.sub.1 represents hydrogen and R.sub.2 represents halogen, nitro or trifluoromethyl, or R.sub.1 and R.sub.2 form a methylenedioxy group at adjacent carbon atoms, as well as pharmaceutically acceptable salts thereof, particularly alkali metal, alkaline earth metal, or amine salts of said acid.

Abstract: The invention is concerned with novel dithioketal derivatives of 1-(2-aryl-2-oxoethyl)-1H-imidazoles and sulfones and sulfoxides derived therefrom, said compounds being useful as antimicrobial agents.