The University of Mississippi

Bethesda Pharmaceuticals, Inc.

Mitchell A Avery

Harrihar A Pershadsingh

Larry Walker

Nakul Telang

The present invention provides a method of preventing or treating one or more of the following medical conditions, or treating symptoms of one or more of the following medical conditions: amebic infections, giardiasis, estrogen deficient states, osteoporosis, cardiovascular heart disease, high cholesterol levels, hyperlipidemia, cancer by administering to a subject having, or predisposed to, one or more of the conditions, a therapeutically effective amount of a compound of the present invention and a pharmaceutically acceptable carrier.

Antigiardial agents and use thereof

This invention provides new chemical entities useful for treating a variety of clinical disorders including those that are influenced by the activity of peroxisome proliferator activated receptors (PPAR). The structures of the compounds and methods to design, make and use the compounds are provided. Compounds and methods for administering therapeutic compositions comprising the compounds in cases of the disease psoriasis are provided. An exemplary compound having the formula compound is 5adamantan-2-yl-pentanoic acid {2-[4-(2,4-dioxo-thiazolidin-5-yl-methyl)-phenoxy]-ethyl}-methyl-amide is provided.

Design and synthesis of optimized ligands for PPAR

The present invention relates to methods for use in producing epothilones and analogs and derivatives thereof. A general method according to the present invention broadly comprises performing an aldol condensation of a first compound with a second compound thereby to form a third compound selected from the formulas:and stereoisomers thereof, and performing a macrolactonization of the third compound. The present invention also provides chemical compounds, and methods for producing such chemical compounds, that are useful in producing epothilones and analogs and derivatives thereof.

Synthesis of epothilones and related analogs

This invention comprises administering to a human or animal in need of treatment an effective amount of an antioxidant lipoic acid derivative and/or pharmaceutically acceptable salts and solvates thereof for the treatment or prevention of pathological (inflammatory, proliferative and degenerative diseases, e.g. diabetes mellitus, atherosclerosis, Alzheimer's disease and chronic viral diseases) and non-pathological (e.g. skin aging and wrinkle formation) conditions caused by oxidative damage. Methods of synthesizing novel antioxidant lipoic acid derivatives and their use in preventing or treating diseases or conditions caused by oxidative stress and other free radical mediated conditions are described. Another aspect of this invention is the use of these antioxidant compositions for the protection of skin from damage caused by ultraviolet radiation and dessication, and to provide improved skin feel by desquamating, cleansing and clarifying the skin. The compositions described in this invention increase cellular viability of epidermal cells, promote cytoprotection, and decrease the production of inflammatory mediators such as inflammatory cytokines in these cells. The antioxidant compositions are incorporated into sunscreen products, soap, moisturizing lotions, skin toners, and other skin care products.

Antioxidants

The present invention describes methods for synthesizing novel dithiolane derivatives, ligands with high affinity for the nuclear hormone receptors, peroxisome proliferator-activated receptor-&ggr; (PPAR&ggr;) and/or PPAR&agr;. Methods for using these compounds in the treatment of endocrine, skin, cardiovascular, immunological, neurological, neuropsychiatric, neoplastic and chronic viral diseases of various organs, including the eye are described. Methods of treating proliferative and inflammatory diseases, degenerative diseases, and age-related dysregulations, caused by an hereditary (genetic) condition or an environmental insult are also provided. In addition, methods are provided for treating conditions and diseases comprising the step of administering to a human or an animal in need thereof a therapeutic amount of pharmacological compositions comprising a pharmaceutically acceptable carrier, a PPAR&agr; agonist, and a second agent selected from the following: a PPAR&ggr; ligand, or an RXR ligand (rexinoid), or a PPAR&ggr;/RXR ligand, effective to reverse, slow, stop, or prevent the pathological inflammatory or degenerative process.

Dithiolane derivatives

This invention provides new thiazolindinedione derivatives and new arylacetic acid derivatives. These compounds are useful for the treatment of cardiovascular diseases, certain endocrine diseases, certain inflammatory diseases, certain neoplastic (malignant) and non-malignant proliferative diseases, certain neuro-psychiatric disorders, certain viral diseases, and diseases associated with these viral infections as discussed herein.

1,2-dithiolane derivatives

This invention provides new thiazolindinedione derivatives and new arylacetic acid derivatives. These compounds are useful for the treatment of certain cardiovascular certain diseases, certain endocrine diseases, certain inflammatory diseases, certain neoplastic (malignant) and non-malignant proliferative diseases, certain neuro-psychiatric disorders, certain viral diseases, and diseases associated with these viral infections as discussed herein.

1,2-Dithiolane derivatives

The present invention provides thiazolidinediones which are useful as antiproliferative, antiinflammatory and antiinfective agents. These compounds are useful for the treatment of certain endocrine diseases including diabetes, certain malignant and non-malignant proliferative diseases including prostate cancer, breast cancer, psoriasis, and acne, certain cardiovascular disorders including hypertension and occlusive vascular diseases.

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Oxford, MS, United States of America

Mitchell A Avery