Abstract: This invention provides novel anti-tumour compounds of the formula ##STR1## wherein R.sub.1 and R.sub.2 are hydrogen or together form an alkyl-, alkoxy- or OH-substituted aromatic group, which optionally contains an N atom as a hetero-atom; R is --COCH.sub.3 or --C.tbd.C--R.sub.4 and R.sub.4 is H or trimethylsilyl; and R.sub.3 is H or --COCF.sub.3 ; and acid addition salts thereof; as well as compositions containing these compounds.

Abstract: A sequence directed reagent is constructed by conjugating a methyl naphthoquinone derivative to a hexamethylamino linker attached to the 5' terminus of an oligonucleotide. Annealing this modified fragment of DNA to its complementary sequence allows for target modification subsequent to photochemical activation. The product of this reaction is a covalent crosslink between the reagent and target strands resulting from an alkylation of DNA by the photoexcited quinone. The modified sequence is not labile to acid, base or reductants, and blocks the exonuclease activity of the Klenow fragment of DNA polymerase I. In another embodiment, a highly reactive moiety, such as Br is attached to the methyl group of the naphthoquinone derivative. This reagent is similarly linked to an oligonucleotide probe. Activation of this probe linked alkylating agent is by a reductive signal which may either naturally occur within the cell, such as an enzyme, or introduced into the media containing the target molecule.

Abstract: A method of hydrating mucous secretions in the lungs of a subject in need of such treatment is disclosed. The method comprises administering to the lungs of the subject a uridine triphosphate such as uridine 5'-triphosphate (UTP) or uridine 5'-O-(3-thiotriphosphate) (UTP.gamma.S) in an amount effective to hydrate lung mucous secretions. The method is useful for treating patients aflicted with cystic fibrosis. Pharmaceutical formulations and methods of making the same are also disclosed.

Abstract: A process for preparing 2',3'-dideoxyadenosine of the formula ##STR1## wherein B is adenine, wherein R.sup.1 is hydrogen, C.sub.1-12 acyl, C.sub.1-12 alkyl, C.sub.7-8 aralkyl, or silyl, said process comprising:reducing a nucleoside of the formula IIIa or IIIb ##STR2## wherein R.sup.2 is hydrogen, C.sub.1-12 acyl, C.sub.1-12 alkyl, C.sub.7-8 aralkyl or silyl; X is Cl, Br or I; R.sup.5 is C.sub.1-12 acyl and B is adenine, with hydrogen in the presence of a palladium catalyst and aqueous solvent mixture of acetonitrile or ethyl acetate and water, said aqueous solvent containing a base selected from the group consisting of sodium hydroxide/sodium acetate and sodium carbonate/sodium acetate, wherein said solvent has a pH of 9-11.

Abstract: A process for stereospecific preparation of glycosyl azides by reacting a metal azide with a glycosyl phosphate triester having the phosphate group cis to the adjacent C-2 substituent is disclosed.

Abstract: New 9-deoxo-9,12-epoxy erythromycin derivatives are disclosed which have improved antibacterial properties. Compositions comprising the erythromycin derivatives and methods of treating mammalian patients with the erythromycin derivatives are also disclosed.

Abstract: Certain salts of 4"-deoxy-4"-epi-methylamino avermectin Bla/Blb such as: the benzoic acid salt, gallic acid salt, citric acid salt, benzenesulfonic acid salt and salicyclic acid salt, phosphoric acid salt, tartaric acid salt or maleic acid salt, exhibit enhanced stability, a property which serves to provide greater shelf life and a product of greater safety for the user and the environment.

Abstract: This invention comprises a series of N.sup.6 -substituted adenosine analogues bearing functionalized chains for the covalent attachment to probes or solid supports. In these compounds coronary vasodilation in the open thorax dog model, typical of A.sub.2 -adenosine receptor agonists, is shown. The potency is modulated by distal structural changes in the chain, with the highest A.sub.2 -potency observed for two methylamides, a primary amine congener, and a biotin conjugate. These compounds have antihypertensive activity and certain components are charged and are excluded from crossing the blood-brain barrier.

Abstract: The present invention relates to compounds of the formula I[CH.sub.3 --(CH.sub.2).sub.29 --O--].sub.m --R (I)whereinif m stands for 1, thenR represents a group derived from a mono- or di- or oligosaccharide by removing the hydrogen atom from the hydroxyl group being in the 1(alpha) or 1(beta) position, or the O-protected, preferably acetylated derivative thereof,if m stands for 2, thenR represents a group derived by removing a hydrogen atom attached to the carbon atom being in position 1 of the reaction product of glucose and mono-, di- or triethylene glycol or the O-protected, preferably O-acetylated derivative thereof.

Abstract: The present invention relates to a novel compound represented by the following formula [I] which is useful as a synthetic intermediate of a 2-alkynyladenosine.The present invention also relates to a process for producing the compound and a process for producing a 2-alkynyladenosine [IV] by way of the compound.Further, the present invention relates to a 2-alkynyladenosine derivative represented by the following formula [V] having excellent storage stability and, to a method of storing the 2-alkynyladenosine in the form of that derivative. ##STR1## wherein R.sup.1 through R.sup.4 represent a hydrogen atom or a protective group, and n denotes an integer of 1 to 15, provided that R.sup.1 through R.sup.4 do not represent a hydrogen atom simultaneously.

Abstract: The invention resides in oligosaccharide derivatives which are obtained by the enzynmatic cleavage of carbohydrates linked to proteins through asparagine groups. The oligosaccharide moieties of the instant invention are 1-amino-1-deoxyoligosaccharide compounds which are cleaved from a glycoprotein with an aminohydrolase enzyme, wherein the amino group of the oligosaccharide is subsequently substituted with a fluorescent reporter compound. The compounds of the instant invention are characterized by the glycosylamine bonds exhibiting less than 10% hydrolysis at 25.degree. C. in aqueous solution over a two days at pH values between 4-10.

Abstract: A method and compositions are provided for synthesizing polynucleotides wherein the exocyclic amino groups of 5'-O-protected-2'O-alkylsilyl-adenosine phosphoramidite and 5'-O-protected-2'-O-alkylsilylguanosine phosphoramidite monomers are protected with dialkylformamidine. In a preferred embodiment, the ribonucleoside phosphoramidite monomers are activated with ethylthiotetrazole.

Abstract: This invention provides a pullulanase having a high degree of pH stability under acidic conditions, which is produced by cultivation of a microorganism belonging to the genus Bacillus, particularly Bacillus circulans SV-98 (FERM P-12161). This enzyme is useful, for example, in the manufacture of glucose and maltose from starch.

Abstract: The present invention is directed to compounds useful as probes for characterizing and studying the adenosine A.sub.2 receptor. The present invention is also directed to methods of treating central nervous system disorders and cardiovascular disorders which include treating hypertension and thrombosis by administering said compounds.

Abstract: The present invention discloses a compound of the formula: ##STR1## where R.sub.1 is hydrogen or the group ##STR2## where R.sub.3 and R.sub.4 are the same or different and are hydrogen, C.sub.1 to C.sub.12 linear or branched alkyl, C.sub.3 to C.sub.7 cycloalkyl, C.sub.6 to C.sub.10 aryl unsubstituted or substituted with C.sub.1 to C.sub.6 linear or branched alkyl, C.sub.1 to C.sub.6 linear or branched alkoxy, nitro, amino, amino substituted with at least one C.sub.1 to C.sub.6 linear or branched alkyl or phenyl, C.sub.2 to C.sub.10 aralkyl, C.sub.4 to C.sub.8 heteroaryl wherein said heteroatom is nitrogen, phosphorous, sulfur or oxygen, and R.sub.2 is hydrogen, or taken together with R.sub.5, forms a chemical bond, and R is a monosaccharide radical selected from the group consisting essentially of glucose, fructose, ribose, 2-deoxyribose, mannose, galactose, xylose and arabinose.

Abstract: 4,6-O-hydroxyphosphoryl-glucosamine derivatives as shown in the following formula [I] and their pharmaceutically-acceptable salts: ##STR1## wherein R.sub.1 and R.sub.2 represent a hydrogen atom or a hydroxy group; one of R.sub.3 and R.sub.4 represents --OCO(CH.sub.2).sub.n CH.sub.3, --CH.sub.2 (CH.sub.2).sub.n CH.sub.3, or --O--CH.sub.2 (CH.sub.2).sub.n CH.sub.3, and the other represents a hydrogen atom; l is an integer of 4-16; m is an integer of 4-16; and n is an integer of 6-18.

Abstract: The present invention relates to novel oligonucleotides having phosphorodithioate internucleotide linkages which may be used for the treatment of diseases caused by viruses.

Abstract: An acid heteropolysaccharide P-318 which comprises galactose, galacturonic acid, N-acetylfucosamine and pyruvic acid in a ratio of about 2:3:1:1, a sulfated heteropolysaccharide P-318 having a 10% or less sulfur content which is prepared by sulfating said acid heteropolysaccharide and a process for preparing an acid heteropolysaccharide P-318 which comprises culturing Pseudomonas sp. 318 to produce the acid heteropolysaccharide P-318 and collecting the thus produced acid heteropolysaccharide P-318. The sulfated polysaccharide P-318 of the invention shows a strong antiviral activity in spite of a lower content of sulfate.

Abstract: A process for preparing erythromycin A oxime or a salt thereof which comprises reacting erythromycin A with hydroxylamine using an acid, is disclosed. Erythromycin A oxime and the salts thereof are useful as intermediates for the synthesis of macrolide antibiotics.

Abstract: N-Acetyl-.beta.-D-glucosamine derivatives represented by the formula ##STR1## wherein R.sup.1 denotes a substituted alkyl group of 1 to 4 carbon atoms having a hydroxyl group, carboxyl group, sulfonic acid group or phosphoric acid group, or an alkali metal salt thereof, or a substituted phenyl group having a hydroxyl group, carboxyl group, sulfonic acid group, phosphoric acid group or said substituted alkyl group, or an alkali metal salt thereof, and R.sup.2, R.sup.3 and R.sup.4 each independently denote a hydrogen atom, halogen atom or nitro group, a process for producing the same, reagents for determining N-acetyl-.beta.-D-glucosaminidase activity containing said derivatives as effective ingredients, and a method for determining N-acetyl-.beta.-D-glucosaminidase activity using said derivatives.