Abstract: N.sup.6, 2-disubstituted or 2-substituted 1'-desoxy-1'-(6-amino-9-purinyl)-.beta.-D-ribofuranuronic acid amides, N-substituted amides, N,N-disubstituted amides, thioamides, N-substituted thioamides and N,N-disubstituted thioamidesare effective against raised blood pressure.

Abstract: The present invention relates to the precursor protein of amyloid plaque core (APC) polypeptide, to fragments of the precursor protein and to the diagnostic use of the precursor protein and of the fragments. Furthermore, the invention relates to the DNA coding for the precursor protein, to fragments of this DNA and to the diagnostic use of the DNA and of the fragments.

Abstract: The present invention relates to new and useful nucleside thiophosphoramidite, polynucleotide dithioate phosphoramidite and polynucleotide phosphorothioamidate phosphoramidite compounds as well as the process whereby these compounds can be used for synthesizing new monoucleotides and polynucleotides having phosphorodithioate, phosphorothioamidate, phosphorothiotriesters and phosphorothioate internucleotide linkages.

Abstract: The reaction of protected monosaccharides or oligosaccharides or protected monosaccharide and oligosaccharide derivatives containing an anomeric hydroxyl group with secondary .alpha.-haloenamines affords high yields of protected glycosyl halides, which are valuable intermediates for the introduction of sugar groups in the synthesis of oligosaccharides, glycolipids or glycopeptides.

Abstract: 4-substituted anthracyclinones of formula (I) ##STR1## wherein R represents a hydrogen atom or a straight or branched alkyl, alkenyl or alkynyl group having from 1 to 10 carbon atoms, are intermediates in the preparation of antitumor anthracycline glycosides of formula (IX): ##STR2## wherein R is as defined above and R.sub.1 is a hydrogen atom or a hydroxy group, and pharmaceutically acceptable salts thereof.

Abstract: Antibacterial compounds are disclosed having the formula ##STR1## and pharmaceutically acceptable salts thereof, wherein R.sup.1 is --NR.sup.4 R.sup.6, where R.sup.4 and R.sup.6 are independently selected from the group consisting of hydrogen, loweralkyl and arylalkyl or, together, R.sup.4 and R.sup.6 form a nitrogen-containing heterocycle attached at the nitrogen atom; R.sup.2 is selected from the group consisting of hydrogen, --OH and, when R.sup.3 is methylene, oxygen so as to form an epoxide; and R.sup.3 is selected from the group consisting of --CH.sub.2 OH, --NR.sup.4 R.sup.6, --(CH.sub.2).sub.n NR.sup.4 R.sup.6 and, when R.sup.2 is oxygen, methylene so as to form an epoxide, where n is 1-4 and R.sup.4 and R.sup.6 are as previously defined, with the proviso that when R.sup.2 is --OH, R.sup.3 may not be --NR.sup.4 R.sup.6 ; or R.sup.2 and R.sup.3 together are.dbd.CH.sub.2.

Abstract: A method for synthesis of oligonucleotide analogs having dithiophosphate internucleosidic linkages is described. Monohalohydrocarbylthiophosphoramidites are utilized to prepare nucleoside thiophosphoramidite intermediates which are activated for nucleoside coupling with tetrazole catalysts. Sulfur oxidation and dehydrocarbylation of the coupled thiophosphite intermediates provide oligonucleotide analogs having achiral dithiophosphate internucleosidic linkages.

Abstract: 5-(.alpha.-D-glucopyranosyloxymethyl)-furan-2-carboxaldehyde (GMF) is produced from isomaltulose by heating a solution of isomaltulose in a strongly polar aprotic solvent in the presence of an acidic ion-exchanger, either batchwise or by percolation of the solution through a column filled with the ion-exchanger. Novel derivatives of GMF of the formula (I) ##STR1## wherein R' is a hydrogen atom, an acyl group or an alkyl group and X represents --CH.sub.2 OH, --COOH, --C(H).dbd.NOH, --CN, --CH.sub.2 NHR" or --CH.dbd.CR"R'", where R" is a hydrogen atom, an acyl or aryl group or an alkyl group with up to 20 C atoms and R'" is a hydrogen atom, --NO.sub.2, --CN, --COOalkyl or acyl are described, and also their preparation and use for the preparation of surface-active compounds.

Abstract: The present invention provides condensed quinoline compounds represented by the following general formula (I): ##STR1## in which Z is NH, X is hydrogen, L is lower alkoxy, M is NHQ, Q is --SO.sub.2 CH.sub.3, Y is --NHR, and R is: ##STR2## These compounds are effective for inhibiting KB-cell growth and prolongation of the life span of mice implanted with tumor P-388.

Abstract: A 46,000 Dalton thermostable, very acidic protease, which has been named thermopsin, was purified to homogeneity from the culture medium of Sulfolobus acidocaldarius by a five-step procedure including column chromatographies on DEAE-Sepharose CL-6B, phenyl-Sepharose CL-4B, Sephadex G-100, MonoQ (FPLC), and gel filtration (HPLC). The enzyme is a single polypeptide chain having proteolytic activity over pH range 0 to 11 at temperatures between 0.degree. C. and 100.degree. C., with maximal activity at approximately pH 2 and 90.degree. C. Antibodies directed against thermopsin have been prepared. Through studies using various aspartic protease inhibitors, thiol and metalloprotease inhibitors, and serine protease inhibitors, it was determined that, although similar to some aspartic proteases, the active site of thermopsin is clearly not identical to that of other aspartic proteases.

Abstract: A compound of the formula ##STR1## wherein the radicals A, X, R.sup.1, R.sup.2 and R.sup.3 are defined as follows: ##STR2## R.sup.2 : H; or R.sup.2 constitutes together with R.sup.3 with a carbon - carbon bondR.sup.3 : H; F; Cl; Br; I; N.sub.3 ; CN; C.tbd.CH; OH; OCH.sub.3 ; CH.sub.2 OH; and when R.sup.3 is F; Cl; Br; I; N.sub.3 ; CN; C.tbd.CH; OH; OCH.sub.3 or CH.sub.2 OH it may have either the cis-configuration or trans-configuration relative to the hydroxymethyl function at position 4', or R.sup.3 constitutes together with R.sup.2 a carbon - carbon bond, and therapeutically acceptable salts thereof, for use in therapy, in particular for the treatment of HIV infections.

Abstract: A method of linking nucleosides with a siloxane bridge comprising reacting a 3'-silylated-5'-protected nucleoside with an unprotected nucleoside is disclosed. The silylated and unprotected nucleosides may be either monomeric nucleosides or the terminal nucleosides of an oligonucleotide or oligonucleotide analog. A method of synthesizing an oligonucleotide analog having siloxane internucleoside linkages is also disclosed. The method of synthesis comprises silylating a 5'-protected nucleoside with a bifunctional silylating reagent to form a 3'-silylated nucleoside, reacting the silylated nucleoside with an unprotected nucleoside in the presence of a base catalyst and repeating these steps to form an oligonucleotide analog. A modified solid phase synthesis method for preparing an oligonucleotide analog having siloxane internucleoside linkages is also disclosed.

Abstract: This invention is directed to N (amino)-protected-2'-O-methyl (methoxy)-5'-dimethoxytrityl (dimethoxytrityl) ribonucleosides (Group I compounds) and to N-protected-2'-O-methyl-5'-dimethoxytrityl-3'-ribonucleoside cyanoethyl N,N-diisopropyl phosphoramidites (Group II compounds). This invention is further directed to the processes involved in producing these compounds. The purification processes produce products in Group I with purity in excess of 99.50% and up to 99.8%. The purity of the products in Group II ranges in excess of 99.8% and up to 99.9%.

Abstract: Enzyme-donor fragments and other unstructured peptides are stabilized against proteolytic degradation by including a mixture of soluble, random-sequence peptides in the assay medium or in the medium in which the enzyme-donor fragment or other peptide is stored.

Abstract: The present invention relates to novel derivatives of 2'-deoxyuridine substituted in the 5-, 3'- or 5'-position by .alpha.-aminoacyl groups, to a process for their preparation and the drugs in which they are present.These derivatives have the following general formula: ##STR1## in which R is selected from an alkyl or alkenyl radical having from 1 to 4 carbon atoms, an aryl radical or a halogen, it being possible for said alkyl, alkenyl and aryl radicals to contain at least one halogen substituent, and a radical of the formula --NH--R.sub.1, in which R.sub.1 is an amino acid residue or a peptide residue containing from 2 to 6 amino acids; andR' and R" are selected from a hydroxyl radical and a radical of the formula --NH--R.sub.1, in which R.sub.1 is as defined above,with the proviso that R' and R" are not simultaneously --NH--R.sub.1 and that, when R is --NH--R.sub.1, R' and R" are simultaneously a hydroxyl group.Application: treatment of cancers and viral infections.

Abstract: Sequence-specific oligonucleotides are provided having substantially pure chiral Sp phosphorothioate, chiral Rp phosphorothioate, chiral Sp alkylphosphonate, chiral Rp alkylphosphonate, chiral Sp phosphoamidate, chiral Rp phosphoamidate, chiral Sp phosphotriester, and chiral Rp phosphotriester linkages. The novel oligonucleotides are prepared via a stereospecific SN.sub.2 nucleophilic attack of a phosphodiester, phosphorothioate, phosphoramidate, phosphotriester or alkylphosphonate anion on the 3' position of a xylonucleotide. The reaction proceeds via inversion at the 3' position of the xylo reactant species, resulting in the incorporation of phosphodiester, phosphorothioate, phosphoramidate, phosphotriester or alkylphosphonate linked ribofuranosyl sugar moieties into the oligonucleotide.

Abstract: An improved process for the preparation of 2' and 3'-(halo-substituted)-2',3'-dideoxy nucleosides by reacting a protected anhydrothymidine compound with a halogenating composition containing a substituted organoaluminum compound which exhibits greater solubility in conventional solvents than AlF.sub.3.

Abstract: The N-phosphorylation of basic nitrogenous drug compounds to produce pro-drugs with enhanced water solubility or lipid solubility, or reduced toxicity, is disclosed. Drugs containing amine, amidine, guanidine, isourea, isothiourea and biguanide functions may be converted to such pro-drugs. The pro-drugs are hydrolyzed in the body, regenerating the original drugs with the release of a salt of phosphoric acid.

Abstract: The compounds of the invention include novel linking agents comprising 2-substituted-3-protected-1,3,2-oxazaphosphacycloalkanes and their phosphoramidite precursors. The compounds of the invention further include conjugates of the above linking agents with oligonucleotides and polymer supports. The compounds of the present invention are useful for linking organic moieties, such as fluorescent or chromogenic dyes, to polymer supports and oligonucleotides, particularly single- and double-stranded DNA and RNA fragments.

Abstract: The present invention discloses trifluorofucoses and methods of making the same. Also disclosed are trifluorofucose analogs of fucose-containing oligosaccharides, and conjugates of trifluorofucose. Compositions are prepared which combine the trifluorofucose-containing oligosaccharides or trifluorofucose conjugates of the present invention with a pharmaceutically acceptable carrier or diluent. Tumor cell metastasis, autoimmune responses or inhibition of an inflammatory process may be inhibited by such compositions.