Abstract: Targeted drug conjugates which enable a large number of molecules of drug to be directed to a cell by a single molecule of antibody are provided. The invention also provides intermediates for the synthesis of such conjugates and cytotoxic drugs modified in accordance with the cluster concept of the invention.

Abstract: The present invention provides adducts of human t-PA derivatives, which comprise a t-PA derivative that lacks the Finger, Growth Factor and Kringle 1 domains, bound to an amphipathic molecule. The invention also provides methods for preparing the adducts and compositions for the treatment of thromboembolic disorders.

Abstract: 1-Carba(1-dethia)cephem antibacterial agents possessing a 3-(substituted or unsubstituted)thiazolo group are provided. Further provided is a method for treating bacterial infections in man and other animals and a pharmaceutical formulation utilizing said 1-carba(1-dethia)cephems.

Abstract: A method for the recombinant production of zymogen forms of human protein C is described. These zymogen forms differ from native zymogen protein C in their increased sensitivity to activation by thrombin and thrombin/thrombomodulin. DNA compounds, vectors, and transformants useful in the method are also disclosed.

Abstract: The present invention comprises novel DNA compounds which encode human protein C activity. A variety of eukaryotic and prokaryotic recombinant DNA expression vectors have been constructed that comprise the novel protein C activity-encoding DNA and drive expression of protein C activity when transformed into an appropriate host cell. The novel expression vectors can be used to produce protein C derivatives, such as non-carboxylated, non-glycosylated, or non-hydroxylated protein C, and to produce protein C precursors, such as nascent or zymogen protein C, and to produce subfragments of protein C, such as active or inactive light and heavy chain. The recombinant-produced protein C activity is useful in the treatment and prevention of a variety of vascular disorders.

Abstract: This invention provides the use of certain tetra-substituted imidazolidin-2-one derivatives in the treatment of susceptible neoplasms in mammals. Also provided are certain novel tetra-substituted imidazolidin-2-one derivatives and pharmaceutical formulations employing them.

Abstract: N-alkylamino-3,4,4-substituted piperidines are provided which are useful as peripheral opioid antagonists.

Abstract: .beta.-Hydroxy-.alpha.-amino acids are obtained via serine hydroxymethyltransferase catalyzed condensation of aldehydes with glycine. The predominant product with most aldehydes is the L-erythro diastereomer. For example, succinic semialdehyde methylester is condensed with glycine in the process to provide L-erythro .alpha.-amino hydroxy adipic acid mono methyl ester.

Abstract: The invention is a method for selectively isolating cells which secrete higher levels of monoclonal antibody than did the parental culture from which they were derived. The method is based on the membrane characteristics of the cell and requires the use of a cell sorter. At present, the invention's best mode utilizes fluorescent probes in conjunction with a fluorescence activated cell sorter. The method is based on the correlation of a high level of cell surface immunoglobulin with high monoclonal antibody secretion rates. The invention provides a predictable and rapid process for selecting high monoclonal antibody producing cells.

Abstract: This compound provides the compound (-)-N"-cyano-N-3-pyridyl-N'-1,2,2-trimethylpropylguanidine, its salts and pharmaceutical formulations, and its method of use for opening potassium channels in mammals.

Abstract: A novel method for isolating transposable elements was used to isolate an approximately 1.6 kb insertion sequence from Streptomyces. The method entails transforming a cell with a plasmid containing a repressor gene, so that the introduction of a transposable element into the gene allows the expression of a selectable marker in a second host cell. The novel insertion sequence isolated from Streptomyces lividans CT2 has been designated IS493.

Abstract: This invention provides the use of certain indenesulfonamide derivatives in the treatment of susceptible neoplasms in mammals. Also provided are certain novel indenesulfonamide derivatives and their pharmaceutical formulations.

Abstract: This invention provides the use of certain benzenesulfonamide derivatives in the treatment of susceptible neoplasms in mammals. Also provided are certain novel benzenesulfonamide derivatives and their pharmaceutical formulations.

Abstract: The invention relates to a compound of formula (I) ##STR1## in which R.sup.1 and R.sup.2 are each hydrogen, halo, hydroxy, nitro, C.sub.1-4 alkylcarbonyl, hydroxy-C.sub.1-4 alkyl, R.sup.3 is hydrogen or optionally substituted phenylsulphonyl, R.sup.4 is optionally substituted phenyl, benzofuranyl or dihydrobenzofuranyl, and R.sup.5 is hydrogen or C.sub.1-4 alkyl; and salts thereof. These compounds are useful dopaminergic agents.

Abstract: The present invention provides a method of inhibiting gastric acid secretion in mammals by administering a 5-HT1A agonist compound or a pharmaceutically acceptable salt thereof.

Abstract: This invention provides certain sulfonimidamide compounds, formulations and method of use of these compounds in treating susceptible neoplasms.

Abstract: A process for separating an anomeric mixture of alpha and beta 2-deoxy-2,2-difluoro-D-ribofuranosyl-1-alkylsulfonates by contacting the anomeric mixture with a solvent; heating; adding a countersolvent; and lowering the temperature.

Abstract: Chiral epoxybutyrates are prepared in high yield from novel dihydro-3R-substituted sulfonyloxy-4R-hydroxy-2-(3H)furanones via based catalyzed alcoholysis. The product chiral epoxy butyrates are useful intermediates for the synthesis of 1-carba-1-dethia cephem antibiotics.

Abstract: A process for providing an alpha-anomer enriched ribofuranosyl sulfonate from a beta-anomer ribofuranosyl sulfonate; comprising treating a beta-anomer ribofuranosyl sulfonate or anomeric mixture thereof with a conjugate anion of a sulfonic acid source at elevated temperatures in an inert solvent.

Abstract: This invention relates to intermediates and processes thereto, for the preparation of 5,6-dihydropyrro[2,3-d]pyrimidines which are useful for the treatment of susceptible neoplasms