Abstract: 2,4,6-trihydroxy-&agr;-p-methoxyphenylacetophenone (also identified herein as “D-58”), or its pharmaceutically acceptable derivatives such as salt and ester forms, is administered for inhibiting inflammatory reactions. The treatment can be remedial or prophylactic. Examples of the conditions that can be treated include acute inflammatory reactions and allergic inflammatory reactions, and specific examples include allergy, asthma, arthritis, psoriasis, skin sunburn, inflammatory pelvic disease, inflammatory bowel disease, urethritis, uvitis, senusitis, pneumonitis, encephalitis, meningitis, myocarditis, nephritis, osteomyelitis, myositis, hepatitis, gastritis, enteritis, dermatitis, gingivitis, appendicitis, pancreatitis, cholocystitis and cholangitis. The 2,4,6-trihydroxy-&agr;-p-methoxyphenylacetophenone can be administered by various routes as needed.

Abstract: Organometallic oxovanadium (IV) complexes having potent spermicidal activity, particularly those having at least one bidentate ligand. Preferred compounds are stable oxovanadium (IV) complexes having, as ancillary ligands linked via nitrogen or oxygen-metal bonds, bis and/or mono-1,10-phenanthroline; 2,2′-bipyridyl; or 2-hydroxyacetophenone.

Abstract: A method for preventing and treating ALS by administering a phytoestrogen, preferably genistein.

Abstract: Novel tubulin binding compounds (SPIKETS) having potent tubulin depolymerization activity and inhibitory activity against tubulin polymerization. The compounds are effective agents for inhibiting cellular proliferation, for example, in cancer cells. The compounds are adapted to interact favorably with a novel SP binding pocket on tubulin, which pocket is useful for screening of anti-tubulin, anti-proliferation, and anti-cancer drugs.

Abstract: Novel tubulin binding compounds having potent tubulin depolymerization activity and inhibitory activity against tubulin polymerization. The compounds are effective agents for inhibiting cellular proliferation, for example, in cancer cells. The compounds are adapted to interact favorably with a novel tubulin binding pocket, which pocket is useful for screening of anti-tubulin, anti-proliferation, and anti-cancer drugs.

Abstract: Inhibitors of JAK3 kinase for the treatment of allergy inhibit mast cell degranulation an dmediator release.

Abstract: The invention provides novel JAK-3 inhibitors that are useful for treating leukemia and lymphoma. The compounds are also useful to treat or prevent skin cancer, as well as sunburn and UVB-induced skin inflammation. In addition, the compounds of the present invention prevent the immunosuppressive effects of UVB radiation, and are useful to treat or prevent autoimmune diseases, inflammation, and transplant rejection. The invention also provides pharmaceutical compositions comprising compounds of the invention, as well as therapeutic methods for their use.

Abstract: Novel spermicidal compounds which are organometallic cyclopentadienyl metal complexes, particularly vanadium IV complexes, are described including corresponding contraceptive and therapeutic compositions and method for providing contraception and selective killing of testicular germ cells. Included among the vanadium complexes are vanadocene dichloride, vanadocene dibromide, bis (methyl cyclopentadienyl) vanadium dichloride, vanadocene diiodide, vanadocene di-pseudobalides, and others. Most active found was vanadocene diselenocyanate.

Abstract: 6,7-Dimethoxy-4-anilinoquinaozolines of the formula: or pharmaceutically acceptable acid addition salts thereof are disclosed. These novel compounds are useful for inducing apoptosis and preventing metastases of brain tumor cells.

Abstract: Novel phenylethyl-thiourea (PHET) compounds as inhibitors of reverse transcriptase and effective agents for the treatment of HIV infection, including mutant, drug-sensitive, drug-resistant, and multi-drug resistant strains of HIV.

Abstract: Inhibitors of JAK3 kinase for the treatment of allergy inhibit mast cell degranulation an dmediator release.

Abstract: The invention provides calanolide compounds used as Tec family/BTK inhibitors, methods for their identification and use, and pharmaceutical compositions comprising calanolide Tec family/BTK inhibitors.

Abstract: Novel compounds that are potent inhibitors of HIV reverse transcriptase (RT) are described in the invention. These novel compounds also inhibit replication of a retrovirus, such as human immunodeficiency virus-1 (HIV-1). The novel compounds of the invention include analogs and derivatives of phenethylthiazolylthiourea (PETT), of dihydroalkoxybenzyloxopyrimidine (DABO), and of 1-[(2-hydroxyethoxy)methyl]-6-(phenylthio)thymine (HEPT). The invention additionally provides a composite HIV reverse-transcriptase (RT) nonnucleoside inhibitor (NNI) binding pocket constructed from a composite of multiple NNI-RT complexes The composite RT-NNI binding pocket provides a unique and useful tool for designing and identifying novel, potent inhibitors of reverse transcriptase.

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

Abstract: Novel pharmaceutical compositions including melamine derivatives and methods for the treatment of cancer including prostate, brain, breast, and leukemia are described. The methods are directed to administering a therapeutically effective amount of a pharmaceutical composition including melamine derivatives having potent cytotoxic activity.

Abstract: Compounds of the formula: wherein: Ra is iodo, (C1-C4)hydroxyalkyl, benzyloxy, OCF3, SCF3, SO3H, SO2F, SO2NR2R3 where R2 is hydrogen or (C1-C4)alkyl and R3 is hydrogen, (C1-C4)alkyl, or phenyl, NR2R4 where R2 is hydrogen or (C1-C4)alkyl and R4 is phenyl; or a group of the formula wherein R5 and R6 are each independently, hydrogen, (C1-C4)alkyl, or (C1-C4) perfluoroalkyl, and R7 is hydrogen, halo, hydroxy, (C1-C4)alkyl, (C1-C4)alkoxy, (C1-C4)hydroxyalkyl, or N(R2)2, where R2 is hydrogen or (C1-C4)alkyl; n is an integer of 1-4; Rb is each, independently, hydrogen, halo, hydroxy, mercapto, (C1-C4)alkyl, (C1-C4)alkoxy, (C1-C4)thioalkyl, (C1-C4)hydroxyalkyl, nitro, cyano, methylenedioxy, ethylenedioxy, COCH3, CF3, OCF3, SCF3, COOH, SO3H, SO2F, phenyl, or phenyl substituted by a group selected from halo, hydroxy, mercapto, (C1-C4)alkyl, (C1-C4) alkoxy, (C1-C4)thioalkyl, (C1-C4)hydroxyalkyl, amino, nitro, cyano, CF3, COOH, SO3H, SO2NR2R3, SO2F where R2 is H or (C1-C4)alkyl and

Abstract: Novel tubulin binding compounds having potent tubulin depolymerization activity and inhibitory activity against tubulin polymerization. The compounds are effective agents for inhibiting cellular proliferation, for example, in cancer cells. The compounds are adapted to interact favorably with a novel tubulin binding pocket, which pocket is useful for screening of anti-tubulin, anti-proliferation, and anti-cancer drugs.

Abstract: Novel alkyl ketone compounds having potent cytotoxic activity are described as anti-tumor agents and are particularly effective against leukemia and breast tumor cells.

Abstract: 2,4,6-trihydroxy-&agr;-p-methoxyphenylacetophenone (also identified herein as “D-58”), or its pharmaceutically acceptable derivatives such as salt and ester forms, is administered for inhibiting inflammatory reactions. The treatment can be remedial or prophylactic. Examples of the conditions that can be treated include acute inflammatory reactions and allergic inflammatory reactions, and specific examples include allergy, asthma, arthritis, psoriasis, skin sunburn, inflammatory pelvic disease, inflammatory bowel disease, urethritis, uvitis, senusitis, pneumonitis, encephalitis, meningitis, myocarditis, nephritis, osteomyelitis, myositis, hepatitis, gastritis, enteritis, dermatitis, gingivitis, appendicitis, pancreatitis, cholocystitis and cholangitis. The 2,4,6-trihydroxy-&agr;-p-methoxyphenylacetophenone can be administered by various routes as needed.

Abstract: Novel phenylethyl-thiourea (PHET) compounds as inhibitors of reverse transcriptase and effective agents for the treatment of HIV infection, including mutant, drug-sensitive, drug-resistant, and multi-drug resistant strains of HIV.