Abstract: This invention provides combinatorial chemistry libraries containing thiourea and urea compounds. In addition, the invention relates to methods for constructing combinatorial chemistry libraries containing thiourea and urea compounds. Furthermore, this invention relates to methods for the identification of bioactive thiourea and urea compounds as well as compositions and therapeutic methods for treating cancer.

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: Contraceptive activity as well as anti-microbial, particularly anti-viral protection is provided by contraceptive compositions containing a thiourea compound of the invention exhibiting spermicidal or sperm-immobilizing activity. Preferred compounds of the invention are cyclohexenyl-substituted thiourea compounds.

Abstract: Contraceptive activity as well as anti-microbial, particularly anti-viral protection is provided by contraceptive compositions containing a thiourea compound of the invention exhibiting spermicidal or sperm-immobilizing activity. Preferred compounds of the invention are cyclohexenyl-substituted thiourea compounds.

Abstract: The invention provides BTK inhibitors, methods for their identification and use, and pharmaceutical compositions comprising BTK inhibitors, including allergy treatments.

Abstract: The invention provides methods for treating cancer and compounds that are useful for the treatment of tumors, as well as pharmaceutical compositions comprising the compounds, and synthetic methods and intermediates useful for preparing the compounds.

Abstract: Compounds are described that bind to tubulin causing tubulin depolymerization and inhibiting tubulin polymerization. The compounds of the invention are therapeutically effective to inhibit cellular proliferation, for example, as effective anti-cancer agents. The compounds can also induce cytotoxicity in cells such as leukemia cells. The chemical structure of the compounds includes a furan, thiophene, thiazole, oxazole, or imidazole group at one end of the molecule (head) and a hydrophobic, aliphatic chain at the other end of the molecule (tail).

Abstract: Methods of inhibiting virus replication of in a cell infected with a resistant strain of HIV that includes administering to the infected cell a virus replication inhibiting amount of an aryl phosphate derivative of d4T.

Abstract: The invention provides compounds which inhibit reverse transcriptase (RT) and which inhibit replication of a retrovirus, such as human immunodeficiency virus-1 (HIV-1). The compound of the invention are phenoxyethyl-thiourea-pyridines. The invention additionally provides a method for inhibiting reverse transcriptase activity of a retrovirus, such as HIV-1, comprising contacting the retrovirus with a compound of the invention. The invention additionally provides a method for inhibiting replication of a retrovirus, such as HIV-1, comprising contacting the retrovirus with a compound of the invention.

Abstract: Methods for treating hemorrhagic fever viral infections by administering an aryl phosphate derivative of d4T having an electron-withdrawing substituent on the aryl group and an amino acid substituent on the phosphate group are described. A preferred aryl phosphate derivative of d4T is d4T-5′-[p-bromophenyl methoxyalaninyl phosphate].

Abstract: Quinazoline compounds and methods for the treatment of cancer and for the treatment of allergic reactions.

Abstract: The present invention describes a therapeutic method useful for treating or preventing a condition of platelet aggregation in a subject including administering a pharmaceutically effective amount of a compound or composition that inhibits JAK-3 and/or tyrosine phosphorylation of STAT-3 and inhibits thrombin induced platelet aggregation. The condition of platelet aggregation includes hematopoietic and cerbrovascular diseases.

Abstract: Acute lymphoblastic leukemia (ALL) and acute myeloid leukemia (AML) are common leukemias in both children and adults. Current treatment strategies are inadequate and often result in patient toxicity and relapse. Accordingly, the need exists for a T-cell-specific immunotoxin with sufficient stability and efficacy to eliminate cell populations associated with various T-cell malignancies. The present invention addresses this concern by providing a biotherapeutic agent (e.g., an immunoconjugate or immunotoxin) comprising a monoclonal antibody (MoAb TXU-7) specific to mammalian T-cell/myeloid antigen CD7 linked to the pokeweed antiviral protein (PAP). The CD7 antigen is expressed on human T-lineage lymphoid cells and leukemic progenitor cells in T-lineage lymphoid malignancies. PAP is a member of the hemitoxin group of toxins and inactivates ribosomes by the removal of a single adenosine from the conserved loop sequence found near the 3′ terminus of all larger RNAs.

Abstract: The present invention is directed to derivatives of piperidinylethyl, phenoxyethyl, and fluorophenethyl bromopyridyl thioureas, which have been found to be effective non-nucleoside inhibitors (NNRTI) of NNI-resistant and multi-drug resistant human immunodeficiency virus (HIV)-1 reverse transcriptase (RT). The present invention is further directed to methods of using the above derivatives to treat patients with NNI-resistant or multi-drug resistant human immunodeficiency virus (HIV)-1.

Abstract: Novel organic arsonic compounds are described as tumor inhibiting, and cancer treating compounds. Methods and compositions for inhibiting tumor cells and treating cancer are also provided.

Abstract: Embodiments of the present invention provide methods for inhibiting tumor cell growth, or treating cancer cells, in a subject through the administration of a cathepsin inhibitor or inhibitors. Methods for inhibiting inflammatory disease cells as well as other cathepsin expressing cells in a subject with a cathepsin inhibitor or inhibitors are also within the present invention. Furthermore, the present invention relates to inducing cytotoxicity or apoptosis in cells by administering a cytotoxic or an apoptotic dose of a cathepsin inhibitor or inhibitors to the cell. Finally, the present invention relates to the administering of cathepsin expressing vectors to tumor cells so as to inhibit the tumor cells growth.

Abstract: Specific Ikaros mutations, as well as the correlation of the presence of the specific Ikaros mutations and other wild-type non-DNA binding Ikaros isoforms with lymphoid cell abnormality is provided in the in the invention. Methods for detecting and treating lymphoid cell abnormality, including hematologic malignancy, are also provided.

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: Methods and compositions for treating ADV infections and HIV/ADV co-infections by administering an aryl phosphate derivative of d4T having an electron withdrawing substituent on the aryl group and an amino acid substituent on the phosphate group are described. Preferred aryl phosphate derivatives of d4T are d4T-5′-[p-bromophenyl methoxyalaninyl phosphate] and d4T-5′-[p-chlorophenyl methoxyalaninyl phosphate].

Abstract: Novel aromatic and heterocyclic thiazolyl thiourea compounds, pharameutical compositions including such, and methods for their use are disclosed. The compounds are effective agents for the treatment of HIV infection, including non-nucleoside inhibitor-resistant, and multi-drug resistant strains of HIV.