Loma Linda University

Sepracor, Inc.

Other

Encore Pharmaceuticals, Inc.

Naturon Pharmaceutical Corporation

William J Wechter

John D McCracken

Darko Kantoci

James W Young

Nancy M Gray

Barry H Levine

Elaine J Benaksas

Neal S Bricker

David E Murray

Timothy J Barberich

Stephen L Matson

Elaine Benaksas Schwartz

E David Murray, Jr

The present invention concerns esters of R-enantiomers of a non-steroidal anti-inflammatory drug, which is substantially free from the S-enantiomer. The compounds of the invention may be used in treating a disease or illness in a mammal. To this end, a composition comprising a compound mentioned above, or a pharmaceutically acceptable salt thereof where salt formation occurs, is administered to the mammal in an amount sufficient to elicit a chemopreventative effect or a chemoprotective effect or a therapeutic effect or a prophylactic effect.

R-NSAID esters and their use

The present invention is generally related to the discovery of the therapeutic benefit of administering &#x3b3;-tocopherol and &#x3b3;-tocopherol derivatives. More specifically, the use of &#x3b3;-tocopherol and racemic LLU-&#x3b1;, (S)-LLU-&#x3b1;, or &#x3b3;-tocopherol derivatives as antioxidants and nitrogen oxide scavengers which treat and prevent high blood pressure, thromboembolic disease, cardiovascular disease, cancer, natriuretic disease, the formation of neuropathological lesions, and a reduced immune system response are disclosed.

Use of &#x3b3;-tocopherol and its oxidative metabolite LLU-&#x3b1; in the treatment of disease

The present invention is generally related to the discovery of the therapeutic benefit of administering &ggr;-tocopherol and &ggr;-tocopherol derivatives. More specifically, the use of &ggr;-tocopherol and racemic LLU-&agr;, (S)-LLU-&agr;, or &ggr;-tocopherol derivatives as antioxidants and nitrogen oxide scavengers which treat and prevent high blood pressure, thromboembolic disease, cardiovascular disease, cancer, natriuretic disease, the formation of neuropathological lesions, and a reduced immune system response are disclosed.

Use of &ggr;-tocopherol and its oxidative metabolite LLU-&agr; in the treatment of disease

This invention relates to the use of enantiomerically pure R-NSAIDs for the treatment of inflammation. Preferably, the R-NSAID used is R-flurbiprofen and is administered in a dose of at least 5 milligrams per kilogram of body weight per day. The anti-inflammatory action of R-NSAIDs is due to their ability to interfere with the biosynthesis of COX-2 by inhibiting COX-2 mRNA synthesis, rather than by just blocking the action of the enzyme itself. In order to effect the inhibition of COX-2 mRNA synthesis, the R-NSAID must be present at relatively high doses. Because the R-NSAID is selective in its action, that is, it does not inhibit either COX-1 mRNA synthesis or the COX-1 enzyme itself, it can be administered in the required high doses because the tissue protective effects of prostaglandins made through the COX-1 pathway are not interfered with.

Method for treatment of inflammation with R-NSAIDS

A method of preventing or delaying the onset of symptoms of Alzheimer's Disease includes the step of administering to a patient in need of such treatment a composition having an effective Alzheimer's Disease prophylactic amount of an enantiomerically stable R-NSAID or a pharmaceutically acceptable salt thereof, the composition being substantially free of the S-enantiomer of the selected R-NSAID.

Prophylactic composition and method for alzheimer's Disease

Compounds, methods and compositions are provided for inducing natriuresis in a mammal. Methods for isolating and synthesizing the natriuretic compounds are also provided. Therapeutic methods using the natriuretic compounds are also provided. The natriuretic compounds are capable of inducing sodium excretion in a mammal without inducing corresponding prolongated potassium excretion.

Natriuretic compounds

Compounds, methods and compositions are provided for inducing natriuresis in a mammal. Methods for isolating and synthesizing the natriuretic compounds are also provided. Therapeutic methods using the natriuretic compounds are also provided. The natriuretic compounds are capable of inducing sodium excretion in a mammal without inducing corresponding prolonged potassium excretion.

The present invention is generally related to the discovery of the therapeutic benefit of administering .gamma.-tocopherol and .gamma.-tocopherol derivatives. More specifically, the use of .gamma.-tocopherol and racemic LLU-.alpha., (S)-LLU-.alpha., or .gamma.-tocopherol derivatives as antioxidants and nitrogen oxide scavengers which treat and prevent high blood pressure, thromboembolic disease, cardiovascular disease, cancer, natriuretic disease, the formation of neuropathological lesions, and a reduced immune system response are disclosed.

Use of .gamma.-tocopherol and its oxidative metabolite LLU-.alpha. in

A composition for use in preventing colorectal cancer and other neoplastic diseases, such as breast cancer, includes an enantiomerically stable R-NSAID or a pharmaceutically acceptable salt thereof in an amount effective to elicit a chemoprotective effect. The composition is substantially free of the S-enantiomer of the R-NSAID. Therapeutic use of the composition is accompanied by reduced adverse side effects. A method of treating cystic fibrosis likewise includes the step of administering to a patient in need of such treatment a composition having an effective cystic fibrosis therapeutic amount of an enantiomerically stable R-NSAID or a pharmaceutically acceptable salt thereof, the composition being substantially free of the S-enantiomer of the selected R-NSAID.

Method and composition for treating cystic fibrosis

A composition for use in preventing colorectal cancer and other neoplastic diseases includes an enantiomerically stable R-NSAID or a pharmaceutically acceptable salt thereof in an amount effective to elicit a chemoprotective effect. The composition is substantially free of the S-enantiomer of the R-NSAID. Therapeutic use of the composition is accompanied by reduced adverse side effects.

Colorectal chemoprotective composition and method of preventing

A compound having the formula I ##STR1## in which R.sub.1, R.sub.2 independently are OH, OOC--R.sub.3 or O--R.sub.3, and

Natriuretic and anti-hypertensive compounds

Methods are disclosed utilizing optically pure R(-) etodolac for the treatment of pain, including but not limited to pain associated with toothaches, headaches, sprains, joint pain and surgical pain, for example dental pain and ophthalmic pain, while substantially reducing adverse effects which are associated with the administration of the racemic mixture of etodolac. The optically pure R(-) etodolac is also useful in treating pyrexia while substantially reducing the adverse effects associated with the administration of the racemic mixture of etodolac.

Antipyretic and analgesic methods of using optically pure R-etodolac

A purified naturally occurring natriuretic compound, identified as Natriuretic Hormone, and a method for isolation of the compound. The natriuretic compound has a molecular weight of about 360, a molecular formula of C.sub.21 H.sub.28 O.sub.5 and with a steroidal nucleus. The compound is useful as a diuretic in the treatment of diseases such as heart disease and hypertension.

Growing community of inventors

Redlands, CA, United States of America

William J Wechter