The University of New Mexico

Other

University Patents, Inc.

Terence J Scallen

Galen D Knight

Paul L Mann

Cary J Morrow

Eugene Mash

The invention discloses a method for the treatment of diseases, particularly those diseases characterized by diminished or aberrant cellular function, including AIDS, cancer, and Alzheimer's Disease. The method comprises administering a therapeutically effective amount of rosuvastatin enantiomer compounds in their (3R, 5R), (3S, 5R), or (3S, 5S) configurations, or pharmaceutically acceptable salts thereof. Biologically-active rosuvastatin enantiomer compounds with (3R, 5R), (3S, 5R), and (3S, 5S) stereochemistry are also disclosed.

Rosuvastatin enantiomer compounds

The invention discloses a method for the treatment of diseases, particularly those diseases characterized by diminished or aberrant cellular function, including AIDS, cancer, and Alzheimer's Disease. The method comprises administering a therapeutically effective amount of rosuvastatin enantiomer compounds in their (3R,5R), (3S,5R), or (3S,5S) configurations, or pharmaceutically acceptable salts thereof. Biologically-active rosuvastatin enantiomer compounds with (3R,5R), (3S,5R), and (3S,5S) stereochemistry are also disclosed.

Compounds termed &ldquo;vitaletheine modulators&rdquo; which include beta-alanyl-taurine and carbobenzoxy beta-alanyl-taurine are synthesized and added to culture media for in vitro culture of cells such as mammalian or plant cells. The compounds support cell vitality, and provide increased cellular life span, increased cellular bioproductivity, improved cellular function, and adaption of resistant cells to culturing. The compounds further delay senescence, optimize growth and maturation, and increase population doublings. Carbobenzoxy beta-alanyl-taurine is produced by coupling &bgr;-alanine, which has it's terminal amine protected with a carbobenzoxy (CBZ) group, to N-hydroxysuccinimide to produce an active ester of &bgr;-alanine, coupling two of the active esters to cystamine to produce a CBZ-protected &bgr;-alethine having an internal disulfide bond, isolating and purifying the CBZ-protected &bgr;-alethine, and reacting the CBZ-protected &bgr;-alethine with iodine to oxidize the disulfide bond to obtain carbobenzoxy beta-alanyl-taurine. Beta-alanyl-taurine is produced by the same procedure except that after oxidizing with iodine, the carbobenzoxy beta-alanyl-taurine is irradiated with UV radiation to remove the CBZ-protecting group.

In vitro cell culture in media containing beta-alanyl-taurine or carbobenzoxy beta-alanyl-taurine

&bgr;-alethine is employed in the differentiation, phenotypic expression, and vitalization of cells, for both in vivo and in vitro applications. Particular applications include the use of &bgr;-alethine in the treatment of immune disorders and diseases, and in the promotion of cell cultures.

&bgr;-alethine use in cell culture and therapy

Compounds termed 'vitaletheine modulators' which include beta-alanyl-taurine and carbobenzoxy beta-alanyl-taurine are synthesized and added to culture media for in vitro culture of cells such as mammalian or plant cells. The compounds support cell vitality, and provide increased cellular life span, increased cellular bioproductivity, improved cellular function, and adaption of resistant cells to culturing. Carbobenzoxy beta-alanyl-taurine is produced by coupling .beta.-alanine, which has it's terminal amine protected with a carbobenzoxy (CBZ) group, to N-hydroxysuccinimide to produce an active ester of .beta.-alanine, coupling two of the active esters to cystamine to produce a CBZ-protected .beta.-alethine having an internal disulfide bond, isolating and purifying the CBZ-protected .beta.-alethine, and reacting the CBZ-protected .beta.-alethine with iodine to oxidize the disulfide bond to obtain carbobenzoxy beta-alanyl-taurine. Beta-alanyl-taurine is produced by the same procedure except that after oxidizing with iodine, the carbobenzoxy beta-alanyl-taurine is irradiated with UV radiation to remove the CBZ-protecting group.

In vitro cell culture in media containing beta-alanyl-taurine or

Biomodulators, which regulate cellular differentiation and proliferation, as well as methods of use thereof, e.g., for treating various conditions, e.g., cancer, senescence, immunological disorders and vascular disease; for stimulating normal tissue architecture after injury; for vaccination; for stimulating the production of biologically important molecules by cells or organs in culture; for maintaining organs or tissues outside of a body after removal from the body and prior to transplantation; and for producing of vascular grafts for transplantation; are provided.

Treatment of aberrant cellular states with biomodulators

The invention provides cell modulators comprising certain biologically-active enantiomers of mevalonate and mevalonolactone derivatives. The compounds are broadly clinically useful, particularly in cancer management and treatment or immunological diseases or disorders.

Cell differentiation induction with mevalonate and mevalonolactone

The invention provides cell modulators comprising certain biologically-active enantiomers of mevalonate and mevalonolactone derivatives. The compounds are broadly clinically useful, particularly in cancer management and treatment of immunological diseases or disorders.

A method for treating neoplasia using sulfur-containing derivatives of carboxy-amino-amides, comprising vitaletheine and vitalethine and related compounds, is provided.

Therapeutic use of vitaletheine modulators in neoplasia

Cholesterol biosynthesis inhibitors are described which are derivatives of coenzyme A having the general formula ##STR1## wherein n is 1 to 3, inclusive, and CoA is coenzyme A minus a hydrogen atom from a sulfhydryl substituent. They are produced by reacting coenzyme A with a fluorinated 3-hydroxy-3-methylglutaric anhydride of the general formula ##STR2## in dilute aqueous alkali.

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Albuquerque, NM, United States of America

Terence J Scallen