Abstract: Methods of treating a human infected with human immunodeficiency virus (HIV), such as a human with AIDS, with the purina nucleotides 2',3'-dideoxy-2'-beta-fluoroadenosine (FddA) and 2',3'-dideoxy-2'-beta-fluoroinosine (FddI) are disclosed. These nucleotides are stable in an acid environment and thus can be used for oral administration. Methods of inhibiting human immunodeficiency virus replication in a human T cell using these purina nucleotides are also disclosed.

Abstract: Purine nucleosides active against human immunodeficiency virus which are substituted at the 2'-position by a strong electronegative group such as fluorine are stable in an acid environment and thus can be used for oral administration.

Abstract: A family of metalloproteinases exist which cleave extracellular matrix molecules. These metalloproteinases are secreted in a latent inactive form and require activation in order to specifically cleave the preferred substrate. A series of peptides have been prepared based on the complete sequence analysis of type IV Procollagenase. Peptide inhibitors were synthesized which correspond to cysteine repeat regions and histidine containing regions; the mechanism of action of these peptides involves inhibition of binding of the enzyme to the substrate. Peptide inhibitors were synthesized which correspond to the peptide cleaved off during activation, and constitute a novel class of metalloproteinase inhibitors. These inhibitors are members of a series of peptides which contain the core amino acid sequence PRCG. The cysteine residue is required for activity.

Abstract: The present invention relates to esters of 3-demethylthiocolchicine and N-acyl analogs thereof having the following formula: ##STR1## wherein R is O-CO-alkyl, O-CO-CH.sub.2 Oalkyl, O-CO-Phenyl, O-COOalkyl; the alkyl group having from 1 to 4 carbon atoms and the Ac group representing acetyl and its higher homologs, benzoyl, alkoxyacetyl, or haloacetyl.The invention further relates to processes for preparing these ester compounds, pharmaceutical compositions thereof and methods for treating diseases such as gout, Mediterranean fever and liver disorders.

Abstract: The invention involves the treatment of cancer in humans by administering water soluble derivatives of taxol. The types of cancer so treatable are those sensitive to treatment with taxol.

Abstract: A histidine rich antigen, designated PfHRP-II, has been synthesized from a recombinant DNA clone containing a genomic fragment of Plasmodium falciparum. PfHRP-II is a protein exported from the parasite into the body fluid. This protein passes through the host erythrocyte in concentrated packets and is released from the infected erythrocyte into the body fluid. The antigen has been isolated and is useful for protection against malaria.

Abstract: Grooming and/or foraging opportunities are provided for caged animals, specifically to nonhuman primates, in order to enrich the environment thereof thus to reduce boredom and stress of the animals. By increasing normative behavior, the inventive method and apparatus reduce abnormal behavior and broaden the behavioral repertoire of the animal. The inventive structure includes a hard backing board of Plexiglass, Lexan, metal or other similar materials, covered with a natural or artificial cloth, fur, fleece, carpeting or the like. Food particles of different sizes with rough edges may be rubbed into the cloth material to elicit foraging activities from the animal.

Abstract: The invention provides an improved method for obtaining optically active amines, carbamates, and isocyanates by thermal fragmentation of optically active ureas through refluxing the ureas in C.sub.3 -C.sub.7 alcohol solution with or without catalytic amounts of alkali metal.

Abstract: This invention concerns anti-hypertensive compositions and a method of lowering blood pressure in mammals. The active component of the compositions is a compound of the formula: ##STR1## wherein R.sub.1 and R.sub.2 are independently chosen from straight chain and branched chain C.sub.1 -C.sub.12 alkyl groups and benzyl, with the proviso that no branch occur on the alpha carbon atom of the alkyl groups; or R.sub.1 and R.sub.2 together with the nitrogen atom they are bonded to form a pyrrolidino, piperidino, piperazino or morpholino group, M.sup.+ is a pharmaceutically acceptable cation, wherein X is the valence of the cation.

Abstract: A process for preparing hydroxy-substituted-4-alkoxyphenylacetic acids by reacting a 4-alkoxyphenylacetic acid with bromine and then treating the brominated acid with a strong base and a copper salt to form the desired hydroxy-substituted-4-alkoxyphenylacetic acid.

Abstract: Several analogues of hexamethylene bis[acetamide] were found to be effective differentiating agents. The most effective of these compounds was 3,3'-(1,6-hexandiyl)bis[5,5-dimethyl-2,4-imidazolinedione].

Abstract: This invention relates to processes for producing uromodulin, a glycoprotein having a molecular weight of 85 kilo daltons. This glycoprotein, which is isolated from crude urine, as well as its carbohydrate derivatives, are useful as immunosuppressive agents or anti-inflammatory agents.

Abstract: Cyclopentenyl pyrimidine compounds have potent anti-viral, anti-tumor and differentiating activity. Of these compounds, cyclopentenyl cytosine has proved to be particularly effective in a variety of tumors, as well as having good antiviral activity and potent differentiating properties.

Abstract: The new compound 3-deazaneplanocin A has been discovered to have potent anti-viral, anti-tumor activity and differentiating activity. A simple method for preparing 3-deazaneplanocin A has been developed involving nucleophilic substitution, which method can also be used to prepare a great variety of carbocyclic nucleosides.

Abstract: Water-soluble derivatives of camptothecin have the formulae: ##STR1## wherein R' is selected from the group consisting of R=CO CH.sub.2 NH.sub.2.HClR=CO CH.sub.2 NHCH.sub.3.HClR=CO CH.sub.2 NHC.sub.2 H.sub.5.HClR=CO CH.sub.2 N(C.sub.2 H.sub.5).sub.2.HClR=CO CH(NH.sub.2) CH.sub.2 CH.sub.2 CH.sub.2 CH.sub.2 CH.sub.2 NH.sub.2.2HClR=CO CH(NH.sub.2) CH.sub.2 CH.sub.2 COOH. HClR=CO CH.sub.2 CH.sub.2.COO.sup.- Na.sup.+R=HPO.sub.3.sup.- Na.sup.

Abstract: Compounds which are active against retroviruses have the following formulaHOH.sub.2 C--CH.dbd.C.dbd.CH--Bwherein B is a purine or pyrimidine heterocyclic ring which is preferably selected from the group consisting of cytosine, 5-halo substituted cytosine, 5-alkyl substituted cytosine, 6-aminopurine, 2,6-diaminopurine, 6-hydroxypurine, 2-amino-6-hydroxypurine, 3-deazapurines, 7-deazapurines, 8-azapurines, and 6-azapyrimidines.