The United States of America as Represented by the Department of Health

The United States of America as Represented by the Secretary of

The United States of America, as Represented by the Secretary, Department of Health and Human Services

Arizona State University

Brigham Young University

The United States of America as Represented by the Secretary of Health

Peter M Blumberg

Zoltan Szallasi

George R Pettit

Michael R Boyd

James Brislin McMahon

Victor E Marquez

Paul Alan Cox

John H Cardellina, Ii

John A Beutler

Gordon M Cragg

Marc C Nicklaus

Shaomeng Wang

George W Milne

Arpad Szallasi

Jeewoo Lee

Nancy E Lewin

Rajiv Sharma

Junichi Ishitoya

Nancy A Sharkey

Larry V Pearce

Krik R Gustafson

Owen S Weislow

The present invention relates to novel compositions comprising an agonist and an antagonist, in certain ratios which allow for the onset of agonist action followed quickly by alleviation by antagonist action, and methods of use in personal defense and law enforcement.

Agonist/antagonist compositions and methods of use

Method of treating cancer using C-26 modified bryostatin

The present invention is directed to preparations of birdseed treated with capsaicin or capsaicin derivatives or analogues thereof in an amount sufficient to be unpalatable to animals having capsaicin sensitive receptors, and more specifically to mammals such as rodents. These 'hot' compounds, extracts or whole plant material containing these compounds may be coated on, impregnated in or combined (e.g., mixed) with birdseed to repel troublesome mammals which recognize these compounds as 'hot'. These 'hot' compounds, in contrast, will not repel birds because birds do not recognize these compounds as 'hot' since they do not have capsaicin sensitive receptors. The invention is further directed to a method of selectively repelling animals having capsaicin sensitive receptors, which comprises feeding the treated birdseed of the invention to birds, in an amount effective for repelling animals having capsaicin sensitive receptors, thereby discouraging said animals from eating the treated birdseed.

Treated bird seed preferentially palatable to birds but not to animals

Conformationally constrained diacylglycerol analogues, pharmaceutical compositions comprising such analogues, and methods of using such analogues as agonists and antagonists of protein kinase C.

Conformationally constrained diacylglycerol analogues

The present invention is directed to preparations of birdseed treated with capsaicin or capsaicin derivatives or analogs thereof in an amount sufficient to be unpalatable to animals having capsaicin sensitive receptors, and more specifically to mammals such as rodents. These 'hot' compounds, extracts or whole plant material containing these compounds may be coated on, impregnated in or combined (e.g., mixed) with birdseed to repel troublesome mammals which recognize these compounds as 'hot'. These 'hot' compounds, in contrast, will not repel birds because birds do not recognize these compounds as 'hot' since they do not have capsaicin sensitive receptors. The invention is further directed to a method of selectively repelling animals having capsaicin sensitive receptors, which comprises feeding the treated birdseed of the invention to birds, in an amount effective for repelling animals having capsaicin sensitive receptors, thereby discouraging said animals from eating the treated birdseed.

Treated bird seed preferentially palatable to birds but not palatable to

The present invention relates to a method of inhibiting a protein kinase C-mediated biological response, such as, hyperplasia. The method comprises administering to a mammal a non-tumor promoting 12-deoxyphorbol ester. Phorbol esters suitable for use in the method include 12-deoxyphorbol 13-monoesters wherein the ester is a formate, acetate, propionate, butyrate, pentanoate, hexanoate, benzoate or phenylacetate ester.

Method of inhibiting hyperplasia to a mammal in need thereof

The present invention relates to an antiviral composition and to methods of treating patients with viral infections. The antiviral composition of the present invention comprises prostratin, a phorbol ester derivative, and a pharmaceutically acceptable carrier. The present composition while having antiviral activity does not have substantial tumor promoting activity and does not have other substantial adverse toxicological properties that would preclude its use in antiviral therapy.

Antiviral composition

The present invention relates to a method of inhibiting the protein kinase C-mediated biological response inflammation. The method comprises administering to a mammal a non-tumor promoting 12-deoxyphorbol ester. Phorbol esters suitable for use in the method include 12-deoxyphorbol 13-monoesters wherein the ester is a formate, acetate, propionate, butyrate, pentanoate, hexanote, benzoate or phenylacetate ester. The invention also relates to novel 12-deoxyphorbol 13-monoesters, wherein the ester can be a formate, propionate, butyrate or pentanoate ester, and to pharmaceutical compositions comprising same.

Phorbol ester pharmaceutical compositions and their use for treating

The present invention provides a method of inhibiting neoplasia and tumor promotion. The method comprises administering to a mammal, particularly a human, in need thereof an effective amount of a 12-deoxyphorbol ester, particularly a 12-deoxyphorbol 13-monoester such as 12-deoxyphorbol 13-acetate (prostratin) and 12-deoxyphorbol 13-phenylacetate (dPP).

Method of inhibiting neoplasia and tumor promotion

The present invention relates to a method for desensitizing a subject animal, which comprises administering to the subject animal a therapeutically effective desensitizing amount of resiniferatoxin for desensitizing the subject animal to neurogenic inflammation, to chemically and thermally induced pain and to responses involving sensory afferent pathways sensitive to capsaicin and to responses involving the hypothalamic temperature control region, and a pharmaceutically acceptable carrier therefor.

Composition of resiniferatoxin and analogues thereof to cause sensory

The present invention relates to labelled resiniferatoxin and congeners thereof. Preferably, the labelled compounds of the invention are radio or fluorescently labelled. The invention is further directed to compositions comprising these labelled compounds, as well as to methods of using these compounds.

Labelled resiniferatoxin, compositions thereof, and methods for using

The present invention relates to a new class of compounds having a variable spectrum of activities for capsaicin-like responses, compositions thereof, processes for preparing the same, and uses thereof. Compounds of the invention are prepared by combining phorbol related diterpenses and homovanillac acid analogs via esterification at the exocyclic hydroxy group of the diterpene. Examples of these compounds include 20-homovanillyl-mezerein and 20-homovanillyl-12-deoxyphorbol-13-phenylacetate.

Growing community of inventors

Frederick, MD, United States of America

Peter M Blumberg