Abstract: The invention relates to a process for the hydrogenation of sugars and sugar mixtures to sugar alcohols or sugar alcohol mixtures wherein the sugars or sugar mixtures are hydrogenated with hydrogen in an aqueous solution at elevated temperature and elevated pressure by using a shell catalyst comprising a mixture of a pure Raney metal and a Raney metal alloy and wherein the shell catalyst has an essentially catalytically inactive core functioning as a carrier and a catalytically active shell.

Abstract: Novel oligonucleotides, method for improving the hybridization properties of oligonucleotides and novel processes for preparing 3'-phosphorylated oligonucleotides.

Abstract: The present invention provides certain 6-hetarylalkyloxy pyrimidine derivatives of formula II ##STR1## wherein R is (i) a cyclic group having at least one 5- or 6-membered heterocyclic ring, optionally with a carbocyclic or heterocyclic ring fused thereto, the or each heterocyclic ring having at least one hetero atom chosen from O, N, or S, or a substituted derivative thereof; or (ii) phenyl or a substituted derivative thereof,R.sup.2 is selected from H, C.sub.1 -C.sub.5 alkyl, halogen or NH.sub.2,R.sup.4 and R.sup.5 which are the same or different are selected fromH, NH.sub.2 or NO.sub.n where n=1 or 2, or R.sup.4 and R.sup.5 together with the pyrimidine ring form a 5-or 6-membered ring structure containing one or more heterocyclic atoms, and pharmaceutically acceptable salts thereof, exhibit the ability to deplete O.sup.6 -alkylguanine-DNA alkyltransferase (ATase) activity.

Abstract: The present invention relates to 2,6-diaminopurine-.beta.-D-ribofuranuronamide derivatives of the following formula (I). These compounds and their salts and solvates are useful as anti-inflammatory agents, particularly in the treatment of patients with inflammatory conditions who are susceptible to leukocyte-induced tissue damage.

Abstract: Novel multicyclic erythromycin compounds and pharmaceutically acceptable salts and esters thereof having antibacterial activity having a formula ##STR1## pharmaceutical compositions comprising a therapeutically effective amount of a compound of the invention in combination with a pharmaceutically acceptable carrier, as well as a method for treating bacterial infections by administering to a mammal a pharmaceutical composition containing a therapeutically-effective amount of a compound of formula (I).

Abstract: The present invention provides novel compounds and methods for purifying oligonucleotides. The compounds according to the invention are multimeric oligonucleotides comprising a multimerization domain for inducing multimeric oligonucleotide aggregation, a hybridization domain that is complementary to a target oligonucleotide whose isolation is desired, and a linker domain connecting the multimerization domain and the hybridization domain. Other compounds of the invention comprise dendrimers having oligonucleotides with hybridization domains linked thereto.The methods of the invention comprise contacting the compounds of the invention with a solution containing a target oligonucleotide whose purification is desired. The target oligonucleotide hybridizes to the hybridization domain of the inventive compounds, thereby forming an aggregate. Synthetic failure sequences (N-1, N-2, etc.

Abstract: A composition for inactivating a target nucleic acid which comprises an oligonucleoside alkyl or arylphosphonate analogue which is complementary to the sequence of the target nucleic acid and includes a functional group which reacts with the target nucleic acid to render the target nucleic acid inactive or nonfunctional.

Abstract: The present invention is directed to a method of synthesizing sulfurized oligonucleotide analogs by reacting an oligonucleotide analog containing a phosphorous(III) linkage with a dithiocarbonic acid diester polysulfide having the formula ##STR1## to produce a sulfurized oligonucleotide analog. The diester polysulfide reagent is useful in solution and solid phase oligonucleotide analog synthesis.

Abstract: Site 1- and site 2-selective derivatives of cAMP have been found to inhibit the of a variety of cancer and leukemic cells. The compounds have been found to have a synergistic effect in cancer and leukemic cell growth inhibition when a site 1-selective compounds is used in combination with a site 2-selective compound.

Abstract: A process for producing solid polycarboxylic acid salts from polysaccharides with gaseous nitrogen dioxide and dinitrogen tetroxide to at least partially convert the primary alcohol groups of the polysaccharides into carboxyl groups and form a solid polycarboxylic acid and then mixing the polycarboxylic acid with a solid neutralizing agent to at least partially neutralized the carboxylic acid groups of the polycarboxylic acid.

Abstract: The present invention relates to compounds of formula (IV): ##STR1## wherein R.sup.a and R.sup.b each represent a hydrogen atom or together form an alkylidene group.

Abstract: There are provided vanadium compositions for use in the treatment of hypertension, obesity and diabetes, in particular improved oral compositions comprising oxovanadium (IV) chelates of monoprotic, bidentate oxygen, oxygen and oxygen, nitrogen coordinating ligands especially kojic acid, maltol and ethyl maltol.

Abstract: The present invention provides a novel class of oligonucleotides useful for antisense purposes. The oligonucleotides of the invention comprise both deoxyribonucleotides with "natural" 3'-5' internucleotide linkages and ribonucleotides with 2'-5' internucleotide linkages. Because of their conformation structure, oligonucleotides according to the invention possess uniform intra-phosphate distances throughout the oligonucleotide chain, allowing them to bind efficiently to complementary DNA and RNA with "natural" 3'-5' internucleotide linkages. The oligonucleotides according to the invention advantageously exhibit diminished immune stimulation and significantly reduced effect on both complement and coagulation as compared to 3'-5' oligonucleotides.

Abstract: Treatment of animals or humans carrying or infected with HTLV-I, HTLV-I (including HTLV-I-associated leukemias or lymphomas), non-A, non-B hepatitis virus, hepatitis B virus, EBV, equine infectious anaemia or other lentiviruses or having antibodies to said viruses is disclosed using the compound 3'-azido-3'-deoxythymidine or a pharmaceutically acceptable basic salt thereof.Also disclosed is the use of the 5'-mono-, di- and triphosphate of 3'-azido-3'-deoxythymidine or a pharmaceutically acceptable basic salt thereof for the same purpose.

Abstract: Methods and compounds are provided for solid phase synthesis of oligonucleotides and related polymers by condensing protected monomer-O-?1,3,2-dichalcogen-substituted-phospholane! synthons in the presence of a catalytic base. Compounds of the invention include 2-N-substituted-1,3,2-dichalcogen-substituted-phospholane precursors of the above synthons, the protected monomer-O-?1,3,2-dichalcogen-substituted-phospholane! synthons, and P-chiral oligonucleotides and related P-chiral polymers.

Abstract: Improved oral dosage formulations for acid-labile dideoxy purine nucleoside derivatives such as ddA, ddI, and ddG, have been developed by incorporating selected water-insoluble buffering systems in the formulation. These novel formulations provide reduced mass dosage units in the form of convenient, palatable chewable/dispersible tablets or a dry powder sachet. The reduced mass requirement, necessary to allow tablets of reasonable size, was achieved in part by an unexpected 20 to 25% increase in drug bioavailability resulting from use of the selected buffering systems comprised of an insoluble magnesium antacid agent and either dihydroxyaluminum sodium carbonate or calcium carbonate.

Abstract: A coupling unit of a (6-4) photoproduct represented by the formula (I): ##STR1## wherein R.sup.1 represents a protective group, R.sup.2 represents a methyl group or a 2-cyanoethyl group, and R.sup.3 represents ##STR2## wherein R.sup.5 represents a methyl group or a 2-cyanoethyl group, and R.sup.6 represents a --N(R')(R") group, a N-morpholino group, a N-pyrrolidinyl group or a 2,2,6,6-tetramethyl-N-piperidyl group where R' and R" each represent a lower alkyl group,a process for preparing the same, a process for preparing an oligonucleotide containing a (6-4) photoproduct by using the same, and a process for preparing DNA containing a (6-4) photoproduct by using the same are disclosed.

Abstract: The invention describes complexes between VB.sub.12 analogues and either GCSF or EPO that retain both significant affinity for intrinsic factor (IF) in the VB.sub.12 portion of the complex and significant bioactivity of the GCSF or EPO portion of the complex. The invention also concerns a process for the synthesis of these complexes. This is achieved at least in part, by using a spacer compound, which is linked covalantly between the VB.sub.12 portion and the GCSF or EPO. The complexes preferably have the formulaV--X--A--Y--ZwhereinV is vitamin B.sub.12 or a vitamin B.sub.12 analogue, or derivative, bonded to X either through a carboxylate group pendant to the corrin nucleus of VB.sub.12 or through the central cobalt atom or to a functional group introduced onto the VB.sub.12 molecule, X is selected from: --NHNH--, --NH--, --O--, --S--, --SS--or --CH.sub.2 --, and A is an optionally substituted, saturated or unsaturated, branched or linear, C.sub.

Abstract: There are provided vanadium compositions for use in the treatment of hypertension, obesity and diabetes, in particular improved oral compositions comprising oxovanadium (IV) chelates of monoprotic, bidentate oxygen, oxygen and oxygen, nitrogen coordinating ligands especially kojic acid, maltol and ethyl maltol.

Abstract: Antimicrobial compounds having the formula ##STR1## as well as pharmaceutically acceptable salts, esters or prodrugs thereof; pharmaceutical compositions comprising such compounds; methods of treating bacterial infections by the administration of such compounds; and processes for the preparation of the compounds.