Abstract: The present invention provides stem-loop and circular oligonucleotides each with at least one Watson-Crick binding (WC) domain and at least one corresponding Hoogsteen binding (H) domain separated from each other by linker domains. Each WC domain has sufficient complementarity to bind to one strand of a defined nucleic acid target by Watson-Crick base pairing in an anti-parallel orientation. Each corresponding H domain is capable of binding to the WC domain by Hoogsteen base pairing in an anti-parallel manner. The present invention also provides methods of making and using these oligonucleotides as well as kits and pharmaceutical compositions containing these oligonucleotides.

Abstract: A process for the enhanced production of antigenic particles consisting essentially of hepatitis B S protein and preS.sub.2 protein. Also disclosed are novel DNA molecules and hosts transformed with these molecules.

Abstract: The present invention provides human interleukin-8 (IL-8) analogs that are modified in the Glu4 Leu5 Arg6 region, and have a core structure corresponding to the IL-8 (7-51) sequence are provided. These neutrophil binding analogs display altered IL-8 activities that can be exploited for therapeutic and other purposes. Such antagonists include those in which, for example, the Leu5 and/or Arg6 residues are replaced, and in which the Glu4 and/or Leu5 residues are deleted. Also provided are biologically active human interleukin-8 (IL-8) analogs comprising a core sequence that includes IL-8 (1-51), IL-8 (3-51) or IL-8 (4-51). The invention also provides pharmaceutical compositions containing the aforementioned analogs.

Abstract: Two novel linear DNA plasmids are described. Also, novel fragments of the plasmids containing the autonomous replication sequence (ARS), and thus capable of self-maintenance as extra chromosomal elements are provided. These novel DNA sequences of the present invention are useful in a vector for self-maintenance in Pichia pastoris and are also useful as plasmid vectors which can be shuttled between yeast and bacteria.

Abstract: Gem-Dichlorocyclopropanes (Analog II derivatives) which demonstrate antiproliferative activity toward MCF-7 cells, in vitro and are generally not reversed by estradiol or having intrinsic estrogenicity (except the hydroxyphenyl derivative Compound 30). In general the cyclopropane compounds have the formula: ##STR1## or any pharmaceutically acceptable salt thereof. X is selected from a group consisting of hydrogen and halogen atoms. The group R.sub.1 may he a hydrogen atom, an alkyl group, an acyl group, or an arylalkyl group. The group R.sub.2 may be a hydrogen atom, an unsubstituted aryl group or a substituted aryl group. The group R.sub.3 may be a hydrogen atom, an alkyl group, a cycloalkyl group, a substituted aryl group or an unsubstituted aryl group. The group R.sub.4 may be a hydrogen atom, an unsubstituted aryl group or a substituted aryl group. The R.sub.4 is absent when R.sub.

Abstract: Chiral catalysts for enantioselectively epoxidizing a prochiral olefin and for enantioselectively oxidizing a prochiral sulfide are disclosed, together with methods of using such catalysts. In accordance with one aspect of the invention, the catalyst is a salen derivative which has the following general structure: ##STR1## In accordance with another aspect of the present invention is a method of, producing an epoxychroman using a chiral catalyst. In accordance with this method, a chromene derivative, an oxygen atom source, and a chiral catalyst are reacted under such conditions and for such time as is needed to epoxidize said chromene derivative. In accordance with yet another aspect of this invention is a method of enantioselectively epoxidizing a cis-cinnamate derivative to make taxol or an analog thereof. In accordance with another aspect a method of disproportionation of hydrogen peroxide using the catalysts of the present invention is disclosed.

Abstract: Diphenylcyclopropyl analogs in which one or more of the phenyl rings includes alkoxy substituents including a dialkylaminoalkoxy group, an unsubstituted piperazine alkoxy group, a substituted piperazine alkoxy group, an unsubstituted piperidine alkoxy group, and a substituted piperidine alkoxy group, and which may have one or two alkyl groups bonded to the cyclopropane. The compounds are useful as antiestrogens and anti-tumor agents.

Abstract: Fabry disease results from an X-linked deficiency in the enzyme .alpha.-galactosidase A. The present invention is directed to recombinant human .alpha.-galactosidase A and provides baculovirus expression vectors and recombinant virus that provide stable expression of extracellular and intracellular levels of this enzyme in an insect cell culture. The recombinant-derived enzyme can be used in enzyme replacement therapy to treat Fabry patients. Composition useful in therapeutic administration of .alpha.-galactosidase A are also provided.

Abstract: Diphenylcyclopropyl analogs in which one or more of the phenyl rings includes alkoxy substituents including a dialkylaminoalkoxy group, an unsubstituted piperazine alkoxy group, a substituted piperazine alkoxy group, an unsubstituted piperidine alkoxy group, and a substituted piperidine alkoxy group, and which may have one or two alkyl groups bonded to the cyclopropane. The compounds are useful as antiestrogens and anti-tumor agents.

Abstract: Diphenylcyclopropyl analogs in which one or more of the phenyl rings includes alkoxy substituents including a dialkylaminoalkoxy group, an unsubstituted piperazine alkoxy group, a substituted piperazine alkoxy group, an unsubstituted piperidine alkoxy group, and a substituted piperidine alkoxy group, and which may have one or two alkyl groups bonded to the cyclopropane. The compounds are useful as antiestrogens and anti-tumor agents.

Abstract: The present invention relates to compounds of the formula ##STR1##

Abstract: A process for the enhanced production of antigenic particles consisting essentially of hepatitis B S protein and preS.sub.2 protein. Also disclosed are novel DNA molecules and hosts transformed with these molecules.

Abstract: Protein tyrosine kinase inhibitors are provided of formula (I): ##STR1## wherein R.sup.2 is H, OH, halo or O(C.sub.1 -C.sub.4)alkyl; R.sup.2 is OH, halo or O(C.sub.1 -C.sub.4)alkyl; R.sup.1 is ##STR2## wherein R.sup.4 is H, OH, halo, CH.sub.2 OH, C(O)CH.sub.3, C(O)N(R).sub.2 wherein each R is H or (C.sub.1 -C.sub.4)alkyl; or C(O)R wherein R.sup.6 is OH or O(C.sub.1 -C.sub.4)alkyl; and R.sup.5 is OH, CH.sub.2 OH, C(O)CH.sub.3, C(O)N(R).sub.2 or C(O)R.sup.6 ; or a pharmaceutically acceptable salt thereof, which inhibit the pathological proliferation or growth of mammalian cells, such as cancer cells.

Abstract: The present invention relates to bis-imidazolyl compounds of the formula: ##STR1## and polymers having the above-identified bis-imidazolyl compounds as a polymerizable unit. The present invention further relates to a method for scavenging trace quantities of metal ions from various effluents sources using the polymers of the instant invention. The instant invention also is directed to the use of the above-identified polymers as corrosion inhibiting agents and as a film for use in gel electrophoresis.

Abstract: This invention relates to Lactobacillus, skim milk, Lactobacillus Growth Factor (LGF) and Lactobacillus compositions and methods of employing the compositions for preventing urogenital infections. More particularly, this invention relates to the ability of strains of hydrophobic or hydrophilic Lactobacillus to adhere to biomaterials, and intestinal, vaginal and uroepithelial cells, to resist the action of certain antimicrobial agents and to dominate the urogenital flora.

Abstract: This invention relates to a process for forming an amide or an ester from a reaction between an amine or an alcohol, respectively and an acylating derivative of a carboxylic acid, in the presence of an effective amount of a compound having the formula: ##STR1## and N-oxides thereof and salts thereof.

Abstract: The present invention relates to promoter elements from human type I transglutaminase (TGase I) genes for controlled gene expression of both human TGase I and heterologous proteins. These promoter elements permit tissue-specific expression of genes, e.g. for use in human gene therapy and for testing pharmaceutical agents with artificial skin. Additionally, the subject promoter elements can provide differential regulation under physiological conditions or in the presence of exogenously added factors including calcium and retinoic acid.

Abstract: The present invention relates to novel compounds useful for the treatment and prophylaxis of degenerative bone disorders and to the preparation thereof. These compounds are particularly characterized by two active moieties, the first of which possesses "bone-seeking" affinity and the second which is an inhibition of the enzyme carbonic anhydrase and/or an inhibitor of bone resorption. The novel compounds of this invention can be administered as pharmaceutically acceptable compositions and in convenient dosage unit form in a method for the treatment and prophylaxis of degenerative bone disorders.

Abstract: The present invention relates to bis-imidazolyl compounds of the formula: ##STR1## and polymers having the above-identified bis-imidazolyl compounds as a polymerizable unit. The present invention further relates to a method for scavenging trace quantities of metal ions from various effluents sources using the polymers of the instant invention. The instant invention also is directed to the use of the above-identified polymers as corrosion inhibiting agents and as a film for use in gel electrophoresis.

Abstract: The compounds of the present invention are adaptable as blocking or protecting groups for an amine composition useful in peptide synthesis. The present invention is directed to a method of protecting an amino group of an organic molecule during a reaction which modifies a portion of the molecule other than the protected amino group.