Abstract: Novel phosphorylating reagents are provided which are useful in DNA synthesis and purification procedures. The reagents are substituted phosphines which are particularly useful in the phosphorylation of nucleoside and solid supported oligonucleotides at the 5'-hydroxyl position. Phosphorylation using these reagents is easily and accurately monitored colorimetrically.

Abstract: Silazanes and related compounds are prepared by (a) providing a precursor containing at least one Si--N bond, cleaving an Si--N bond in the precursor in the presence of hydrogen or a hydrogen donor, and reacting the cleavage product with a second cleavage product or with a compound containing an Si--H bond, an N--H bond, or both, to produce an initial silazane product having at least one newly formed Si--N bond or (b) providing one or more reactants which contain an Si--H bond and an N--H bond, and causing reaction to occur between the two bonds in the presence of a transition metal catalyst to form an initial silazane product having newly formed Si--N bonds. Further products may result from additional reaction of either type. Novel compounds, including siloxazanes and high molecular weight polysilazanes, are provided. The compounds may be pyrolyzed to yield ceramic materials such as silicon nitride, silicon carbide and silicon oxynitride.

Abstract: Novel compounds useful as renin inhibitors are provided. The compounds are hydroxyazido derivatives having the structural formula ##STR1## wherein the substituents R.sub.1 through R.sub.7 are as defined herein. Analogs of these compounds which are ketozaido derivatives are also provided. Additionally disclosed re methods for using the novel compounds to treat hypertension, and pharmaceutical compositions containing the compounds. Of particular interest are formulations for oral administration.

Abstract: A novel atrial peptide-degrading enzyme (ADE) is provided in isolated, purified form. The enzyme has a molecular weight of approximately 160,000 Daltons as measured by gel filtration chromatography, and is effective to cleave atrial peptides such as APII, APIII and ANF. Also provided are novel compounds useful as inhibitors of the enzyme and thus useful as blood pressure lowering agents, pharmaceutical compositions containing the inhibitors, and methods of using the inhibitors.

Abstract: Novel photolabile photochemical reagents are disclosed. The reagents are useful in a variety of biochemical and chemical contexts, including nucleic hybridization assays and chemical phosphorylation of hydroxyl-containing compounds. The reagents are particularly useful for introducing cleavable sites into oligonucleotide or polynucleotide chains, i.e., sites which are cleavable upon photolysis. The reagents are also useful in both 5'- and 3'-phosphorylation of oligonucleotide or polynucleotide chains.

Abstract: Oligomers and polymers are prepared substantially free of error sequences by sequentially adding monomers, which are terminally blocked and have active functionalities protected, to a growing chain bound to a support through a selectively cleavable linkage. After each addition, unblocked terminal groups are capped. At the completion of monomer addition, enzymatic hydrolysis interfering protecting groups are removed along with the capping group and failure sequences enzymatically degraded. The terminal blocking group may then be removed. The completed oligomer or polymer may be cleaved from the support prior or subsequent to enzymatic degradation but after completion of the sequence.

Abstract: A method is provided for preparing preceramic polymers and and silicious ceramic materials which derive therefrom. The preceramic polymers are polysiloxanes which are synthesized by catalytically activating Si--H bonds in a hydridosiloxane starting material and replacing the activated hydrogen atoms with non-hydrogen substituents. These preceramic polysiloxanes are pyrolyzed in a selected atmosphere to give the desired ceramic product. Ceramic products which may be prepared by this technique include silica, silicon oxynitride, silicon carbide, and metal silicates.

Abstract: Skin permeation enhancer compositions are provided which increase the permeability of skin to transdermally administered pharmacologically active agents. The compositions contain a lower aliphatic ester of a lower aliphatic carboxylic acid such as ethyl acetate and a lower alkanol such as propylene glycol. Methods and transdermal drug delivery systems for using the compositions are also provided.

Abstract: A method for radiosensitizing hypoxic tumor cells in a warm-blooded animal is provided. The method involves administration of a nicotinamide compound having the structural formula ##STR1## wherein X is O or S, and Z is H, OR, SR or NHR where R is as defined herein. Exemplary compounds for use in conjunction with the disclosed method include: 5-hydroxynicotinamide; 5-hydroxynicotinamide, sodium salt; 5-(2,3-dihydroxypropoxy)nicotinamide; 5-aminonicotinamide; 5-(2-methoxyethylamino)nicotinamide; and 5-acetamidonicotinamide.

Abstract: A method is provided for preparing preceramic polymers and silicious ceramic materials which derive therefrom. The preceramic polymers are polysiloxanes which are synthesized by catalytically activating Si-H bonds in a hydridosiloxane starting material and replacing the activated hydrogen atoms with non-hydrogen substituents. These preceramic polysiloxanes are pyrolyzed in a selected atmosphere to give the desired ceramic product. Ceramic products which may be prepared by this technique include silica, silicon oxynitride, silicon carbide, and metal silicates.

Abstract: Methods and formulations are provided for alleviating the dryness of mucosal membranes in the upper and lower respiratory tract and gastrointestinal tract. The compositions are formulated into aerosol sprays and delayed release tablets which include eriodictyon fluid which is a Yerba Santa extract. The formulations may additionally contain other components such as preservatives, bronchodilators, choleretics, antibiotics, topical anesthetics, coloring agents, emulsifiers, and the like. The Yerba Santa-based compositions of the invention are administered to an affected patient to alleviate or prevent dryness on the mucosal membranes of the respiratory and gastrointestinal tracts.

Abstract: Skin permeation enhancer compositions are provided which increase the permeability of skin to transdermally administered pharmacologically active agents. The compositions contain a sorbitan ester in addition to the selected pharmacologically active agent, and may also contain a C.sub.1 -C.sub.4 aliphatic alcohol. Methods and transdermal drug delivery systems for using the compositions are also provided.

Abstract: Novel methods for assaying a nucleic acid analyte are provided, which employ polynucleotides having oligonucleotide sequences substantially homologous to a sequence of interest in the analyte, where the presence or absence of hybridization at a predetermined stringency provides for the release of a label from a support. Particularly, various techniques are employed for binding a label to a support, whereupon cleavage of either a single or double strand, a label may be released from a support, where the release of the label can be detected as indicative of the presence of a particular oligonucleotide sequence in a sample. The method finds use in diagnosis of disease, genetic monitoring, and analysis of nucleic acid mixtures.

Abstract: A method for enhancing the permeability of the skin or other biological membrane to a material such as a drug is disclosed. In the method, the drug is delivered in conjunction with ultrasound having a frequency of above about 10 MHz. The method may also be used in conjunction with chemical permeation enhancers and/or with iontophoresis.

Abstract: 15,16-Seco-19-nor progestins are provided which display elevated progestational activity with a minimum of ancillary hormonal activity. Processes for the preparation of the novel progestins are provided as are methods of use. A preferred method of use is in the suppression of ovulation in the human female.

Abstract: A light-curable orthodontic bracket adhesive composition is provided for bonding an orthodontic bracket to the surface of a human tooth. The composition contains a particulate filler material, an acrylate-based resin, and a photoinitiator composition effective to catalyze polymerization upon irradiation. A method of using the composition is also provided.

Abstract: This invention provides a novel disinfectant composition which is an aqueous solution containing hypochlorite and a tertiary aliphatic alcohol t-butanol. The alcohol acts as an odor masking agent and as a stabilizer for hypochlorite ions while itself possessing disinfecting properties. The composition is useful as a disinfectant.

Abstract: Method and laminated composite for administering buprenorphine transdermally to treat pain. The composite comprises an impermeable backing layer and a reservoir layer containing buprenorphine and optionally a permeation enhancer combined with a pressure-sensitive adhesive with the amounts of buprenorphine and optional enhancer being sufficient to cause the buprenorphine to pass through the skin at a rate in excess of about 0.05 mcg/cm.sup.2 /hr.

Abstract: A novel liquid developer composition for use in electrophotographic processes, particularly consecutive color toning, is described. The composition contains, dispersed in a hydrocarbon medium, toner particles of colorant-containing resin and an antistatic agent substantially immiscible with the resin. The antistatic agent effectively eliminates the image staining frequently obtained in consecutive color toning processes. Methods for preparing and using the novel composition are also provided.

Abstract: An improved method for detecting peroxidatively active materials in a sample is provided, the method incorporating antimalarial drugs such as quinine, quinidine, chloroquine, primaquine, and quinacrine as modulating compounds. In a preferred embodiment, the method is a fecal occult blood test (FOBT), in which a fecal specimen is contacted with a chromogen and a hydroperoxide in the presence of a selected quinoline derivative. The method enables careful modulation of test sensitivity and specificity, and further provides an FOBT in which interference from dietary meat ingestion is substantially eliminated.