Abstract: Monomeric and dimeric anti-cancer drug aldehyde conjugate compounds and pharmaceutically acceptable salts thereof. Specifically, monomeric and dimeric aldehyde conjugates of 1-2, dihetero-substituted anti-cancer drugs, including monomeric and dimeric aldehyde conjugates of anthracyclines, are provided. Also provided are pro-drugs which, after administration, release monomeric aldehyde conjugates. Further provided are pharmaceutical and therapeutic compositions containing anti-cancer drug aldehyde conjugates and methods of treating cancer using the aldehyde conjugates.

Abstract: Aryl phosphate derivatives of d4T with para-bromo substitution on the aryl group show markedly increased potency as anti-HIV agents without undesirable levels of cytotoxic activity. In particular, these derivatives are potent inhibitors of HIV reverse transcriptase. In a preferred aspect of the present invention, the phosphorus of the aryl phosphate group is further substituted with an amino acid residue that may be esterified or substituted, such as a methoxy alaninyl group.

Abstract: The present invention relates to a process for effectively preparing L-ribose, which is recognized as being highly important in relation to the development of new antiviral medicines, from 1,4-lactone compound.

Abstract: The invention includes compositions and methods useful for treatment of a virus infection in a mammal by double-targeting the virus (i.e. targeting the virus at more than one stage of the virus life cycle) and thereby inhibiting virus replication. The compositions of the invention include compounds which comprise a phosphocholine moiety covalently conjugated with one or more antiviral agents (e.g. nucleoside analogue, protease inhibitor, etc.) to a lipid backbone. The invention also includes pharmaceutical compositions and kits for use in treatment of a virus infection in mammals. The methods of the invention comprise administering a compound of the invention, a pharmaceutically acceptable salt thereof, or a pharmaceutical composition of the invention, in an amount effective to treat the infection, to a mammal infected with a virus. Additionally, the invention includes compositions and methods useful for combating a cancer in a mammal and for facilitating delivery of a therapeutic agent to a mammalian cell.

Abstract: Disclosed are a crystallizing method of doxorubicin hydrochloride from a doxorubicin hydrochloride-containing solution, particularly a method for carrying out the crystallization under a condition of 40° C. or higher, and a doxorubicin hydrochloride crystalline aggregate having particularly an excellent solubility in water.

Abstract: There are disclosed novel Stavudine solvates as follows: Stavudine NN-dimethyllacetamide solvates; Stavudine NN-dimethylacrylamide solvates and Stavudine NN-dimethylpropionamide solvates and processes for producing Stavudine NN-dimethylacetamide solvates, Stavudine NN dimethylacrylamide solvates and Stavudine NN dimethylpropionamide solvates which results in pure Stavudine.

Abstract: Cellulose particles are described that have cationic groups in their interior. In one aspect, at least 10%, and preferably 50% or more, of the cationic groups are present within the particle interior. Also disclosed are particular combinations of such cellulose particles with certain water-soluble polymers that are well suited for use in the papermaking industry.

Abstract: A cytotoxic agent comprising one or more modified doxorubicins/daunorubicin linked to a cell binding agent. A therapeutic composition for killing selected cell populations comprising: (A) a cytotoxic amount of one or more modified doxorubicins/daunorubicins covalently bonded to a cell binding agent through a linking group, and (B) a pharmaceutically acceptable carrier. A method for killing selected cell populations comprising contacting target cells or tissue containing target cells with an effective amount of a cytotoxic agent comprising one or more modified doxorubicins/daunorubicins linked to a cell binding agent. Novel sulfur-containing modified doxorubicins/daunorubicins.

Abstract: Methods for the regioselective alkylation at the 2′-hydroxy position over the 3′-hydroxy position of nucleosides and nucleoside analogs, forming 2′-O-ester modified compounds, are disclosed. Reduction and derivatization of the 2′-O-ester provides 2′-O-modified nucleosides and nucleoside analogs useful for the synthesis of oligomeric compounds having improved hybridization affinity and nuclease resistance.

Abstract: Disclosed are a method for the reduction of an oligosaccharide mixture and an oligosaccharide mixture prepared thereby. In accordance with the disclosed invention, a mixture of oligosaccharides having a given DP profile is reduced to a DE of essentially zero by catalytically hydrogenating the mixture under reaction conditions sufficient to preserve the DP profile of the mixture, which reaction conditions typically include a reaction temperature ranging from about 50° C. to about 150° C. and a reaction pressure ranging up to about 1500 psi. Surprisingly, when the mixture is a malto-oligosaccharide mixture, the reduced mixture will have a superior color-fastness and thermal stability as compared to a similar unreduced mixture of malto-oligosaccharides, and also low reactivity towards nitrogen-containing species.

Abstract: C-nucleosides are synthesized by a method in which a sugar is derivatized in a single step to provide a heterocycle at the C1 position, and then the heterocycle is aromatized in another single step. In one class of preferred embodiments a cyano sugar is converted into thiocarboxamide, and subsequently condensed to form an azole ring. In a second class of preferred embodiments a cyano sugar is condensed with an amino acid to provide the azole ring. In a third class of preferred embodiments a halo sugar is condensed with a preformed heterocycle to provide the azole ring.

Abstract: The present invention contemplates a system for rapidly isolating nucleic acids. The system comprises an insoluble silica matrix and a buffered aqueous salt solution containing salt at a concentration of at least 3 molar and a buffering agent at a concentration sufficient to provide a buffering capacity corresponding to that which either tris(hydroxymethyl)aminomethane or phosphate ion at a concentration of 0.1 to 1 molar would provide in the solution. Methods of using the system are also contemplated.

Abstract: Synthetic processes are provided wherein oligomers are prepared using phosphoramidite compositions. Oligomers having phosphodiester, phosphorothioate, phosphorodithioate covalent linkages are prepared that can include other covalent linkages. Also provided are compositions useful in such processes.

Abstract: Methods and intermediates for the preparation of oligomers containing diastereomerically enriched phosphorothioate linkages are disclosed.

Abstract: The use is disclosed of at least substantially water-insoluble ethers which are fluid and/or at least plastically deformable at working temperature and have flash points of at least 80° C., of mono- and/or polyfunctional alcohols of natural and/or synthetic origin or corresponding solutions of such ethers in ecologically acceptable water-insoluble oils as the dispersed oil phase of water-based O/W-emulsion drilling fluids which are suitable for the environmentally acceptable development of geological formations and which contain, if desired, insoluble, finely particulate weighting agents for the formation of water-based O/W-emulsion drilling muds and/or further additives, such as emulsifiers, fluid-loss additives, wetting agents, alkali reserves and/or auxiliary substances for the inhibition of drilled rock of high water-sensitivity.

Abstract: A process for the production of a compound of the formula: wherein R1 is hydrogen, alkyl, C1-C16 substituted alkyl, aryl, substituted aryl, aralkyl, substituted aralkyls, alkenyl, substituted alkenyl, alkynyl, substituted alkynyl, cyano, carboxy, carboxy esters, carboxamido, N-mono substituted and N,N-disubstituted carboxamido with alkyl, aralkyl and aryl groups; R2 is hydrogen, alkyl C1-C16 substituted alkyl, aryl, substituted aryl, aralkyl, substituted aralkyls, alkenyl, substituted alkenyl, alkynyl, substituted alkynyl; R3 is alkyl C2-C6, branched alkyl, aryl C2-C, substituted aryl and R4 is halogen or H.

Abstract: A method for controlling bacterial and fungal diseases in plants which includes applying a chitosan metal chelate complex having at least two metal ion species to the plant. Chitosan metal complexes for application to control bacterial and fingal diseases in plants are also disclosed.

Abstract: A method for the identification of agents which inhibit chitin synthesis, thus exhibiting potential fungicidal and insecticidal activity, involves the incubation of test samples in neutral Saccharomyces cerevisiae cultures containing calcofluor white, a fluorochrome that causes lethal chitin hyper-polymerization in the yeast. Cultures containing samples that inhibit chitin synthesis exhibit enhanced growth because the growing fungus is rescued from the adverse effects of calcofluor white. In the practice of the invention, the test sample is added to a S. cerevisiae culture or culture area containing calcofluor white and the culture is incubated with the test sample for such time under such conditions sufficient to observe yeast cell growth inhibition in a corresponding culture or culture area containing calcofluor but no test sample.

Abstract: Novel orthoesters are provided which can be used as a 2′-hydroxyl protecting groups or 2′-modification in the synthesis of polymers containing ribonucleic acid (RNA) nucleotides. The RNA comprising the orthoester can be handled and analyzed while 2′-modified, thereby minimizing potential degradation. The orthoester is stable during oligonucleotide synthesis. The orthoester is subsequently modified and can then be removed under mild acidic conditions. The ease and dependability of this process and the quality of the RNA product synthesized with this invention are comparable to that previously associated only with DNA synthesis.

Abstract: This invention is directed to novel substituted nucleotide bases with a crosslinking arm which accomplish crosslinking between specific sites on adjoining strands of oligonucleotides a oligodeoxynucleotides. The invention is also directed to oligonucleotides comprising at least one of these crosslinking agents and to the use of the resulting novel oligonucleotides for diagnostic and therapeutic purposes.