Ligand Pharmaceuticals, Inc.

The Salk Institute for Biological Studies

Baylor College of Medicine

Other

Eisai Inc.

Richard Alan Heyman

Marcus F Boehm

Ronald Mark Evans

David John Mangelsdorf

Gregor Eichele

Ranjan Mukherjee

Christina Thaller

Rosemary Cesario

Lin Zhi

Alex M Nadzan

Chan Kou Hwang

Christina S Berger

Robert B Stein

Steve White

Luc J Farmer

Lin Zhang

Stanley M Hollenberg

Anthony E Oro

Beth Ann Badea

William W Lamph

Laura J Dardashti

Deepak S Lala

Stacie Canan Koch

Eric D Bischoff

Emiliana Borrelli

Chan Kou (Jack) Hwang

Klaus Damm

Margaret A Harmon

Stacie Canan-Koch

Compounds, compositions, and methods for modulating processes mediated by Retinoid X Receptors using retinoid-like compounds which have activity selective for members of the subclass of Retinoid X Receptors (RXRs), in preference to members of the subclass of Retinoic Acid Receptors (RARs). Examples of such compounds are bicyclic benzyl, pyridinyl, thiophene, furanyl, pyrrole, and polyenoic acid derivatives including carbocyclic polyenoic acids. The disclosed methods employ compounds for modulating processes selectively mediated by Retinoid X Receptors.

Compounds having selective activity for retinoid X receptors, and means for modulation of processes mediated by retinoid X receptors

Methods and compositions for the treatment of anti-estrogen resistant breast cancer using retinoid compounds which are modulators of Retinoid X Receptors.

Methods and pharmaceutical compositions for treatment of anti-estrogen resistant breast cancer using RXR modulators

In accordance with the present invention, there are provided methods to modulate processes mediated by retinoid receptors, employing high affinity, high specificity ligands for such receptors. In one aspect of the present invention, there are provided ligands which are more selective for the retinoid X receptor than is retinoic acid (i.e., rexoids). In another aspect of the present invention, alternative ligands (other than retinoic acid) have been discovered which are capable of inducing retinoic acid receptor mediated processes. In yet another aspect, methods have been developed for the preparation of such retinoid receptor ligands from readily available compounds.

Means for the modulation of processes mediated by retinoid receptors and compounds useful therefor

A method for modulating lipid metabolism in a subject by administering 9-cis retinoic acid is presented. The 9-cis retinoic acid is more specific for the retinoid X receptor than is retinoic acid.

The present invention discloses a new selective method for inducibly and genetically ablating specific cell lineages in transgenic cell populations, e.g., in transgenic animals. The new method, which permits the production of stable transgenic perigees, and thus can be used at various stages of development of a transgenic cell population, allows both the timing and the degree of cellular ablation to be controlled. As a result the method can be used for a variety of therapeutic applications, as well as to study cell lineages and organogenesis, plus the capacity that residual stem cells have for regeneration.

Inducible HSV-TK in transformed cell populations

Means for the modulation of processes mediated by retinold receptors and compounds useful therefor

Dimer-selective RXR modulator compounds having agonist, partial agonist and/or antagonist activity in the context of an RXR homodimer and/or RXR heterodimers are provided. Also provided are pharmaceutical compositions incorporating such dimer-selective RXR modulator compounds and methods for their therapeutic use.

Dimer-selective RXR modulators and methods for their use

This invention relates to methods and compositions for the treatment of non-insulin-dependent diabetes mellitus using an RXR agonist alone or in combination with a PPAR&ggr; agonist such as a thiazolidinedione compound.

Treating NIDDM with RXR agonists

Compounds and compositions useful for modulation of processes mediated by RXR

Compounds, compositions, and methods for modulating processes mediated by Retinoid X Receptors using retinoid-like compounds which have activity selective for members of the subclass of Retinoid X Receptors (RXRs), in preference to members of the subclass of Retinoic Acid Receptors (RARs). Examples of such compounds are bicyclic benzyl, pyridinyl, thiophene, furanyl, and pyrrole derivatives. The disclosed methods employ compounds for modulating processes selectively mediated by Retinoid X Receptors.

In accordance with the present invention, there is provided a method for the treatment of subjects afflicted with steroid or steroid-like hormone-responsive disease states. The invention method comprises administering to the subject an effective amount of a ligand which selectively interacts with the receptor subtype associated with the steroid or steroid-like hormone-responsive disease state, wherein said ligand interacts with said receptor subtype to a significantly greater extent than with other subtypes of the same receptor class.

Use of selective ligands for treatment of disease states responsive to

Compounds having selective activity for retinoid X receptors, and means

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Encinitas, CA, United States of America

Richard Alan Heyman