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AssigneeLigand Pharmaceuticals Incorporated
InventorsMarcus F. Boehm, Richard A. Heyman, Lin Zhi, Chan Kou Hwang, Steve White, Alex Nadzan
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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 poiyenoic acid derivatives including carbocyclic polyenoic acids. The disclosed methods employ compounds for modulating processes selectively mediated by Retinoid X Receptors.
A pharmaceutical composition comprising in a pharmaceutically acceptable vehicle suitable for enteral, parenteral, or topical administration, one or more compound, or a pharmaceutically acceptable ester, amide or salt thereof, said compound selected from the group consisting of:
A therapeutic process comprising administering to a subject a compound which in a co-transfection assay is more potent an activator of a Retinoid X Receptor than a Retinoic Acid Receptor, wherein said compound is useful to modulate in vivo lipid metabolism, in vivo lipid homeostasis, in vivo skin-related processes, in vivo autoimmune diseases, in vivo fatty acid metabolism, in vivo malignant cell development, in vivo premalignant lesions, in vivo programmed cell death, or in vivo endocrinological processes.
A therapeutic process comprising administering to a subject a compound which in a co-transfection assay is more potent an activator of a Retinoid X Receptor than a Retinoic Acid Receptor, wherein said compound is useful to treat dermatological conditions, keratinization disorders, proliferative disorders, differentiation disorders, comedolytic activity, cancer, inflammatory diseases, hyperlipidemia, cardiovascular disorders, apolipoprotein Al metabolism, AP-1 metabolism, or plasma HDL levels.
A therapeutic process comprising administering to a subject a compound which in a co-transfection assay is more potent an activator of a Retinoid X Receptor than a Retinoic Acid Receptor, wherein said compound is useful to treat acne, psoriasis, aging, wrinkling, acute promyelocytic leukemia, mammary cancer, prostate cancer, lung cancer, cancers of the aerodigestive pathway, skin cancer, bladder cancer, sarcomas, or leukoplakias.
A pharmaceutical composition comprising a compound which is more potent an activator of a Retinoid X Receptor than a Retinoic Acid Receptor in a co-transfection assay in combination with a pharmaceutically acceptable vehicle.
A pharmaceutical composition comprising a compound which modulates a process mediated by a Retinoid X Receptor in combination with a pharmaceutically acceptable vehicle, wherein said compound selectively activates one or more Retinoid X Receptors in preference to Retinoic Acid Receptors.
A method for modulating a process mediated by one or more Retinoid X Receptors, said method comprising causing said process to be conducted in the presence of at least one compound which is more potent an activator of one or more of the Retinoid X Receptors than one or more of the Retinoic Acid Receptors in a co-transfection assay, wherein said process is the in vivo modulation of lipid metabolism, lipid homeostasis, hyperlipidemia, skin-related processes, autoimmune diseases, fatty acid metabolism, malignant cell development, premalignant lesions, programmed cell death, endocrinological processes, or AP-1 metabolism.
A method for treating a mammalian subject requiring Retinoid X Receptor therapy comprising administering to such a subject a pharmaceutically effective amount of a compound which is more potent an activator of a Retinoid X Receptor than a Retinoic Acid Receptor in a co-transfection assay, wherein said process is the in vivo modulation of lipid metabolism, lipid homeostasis, hyperlipidemia, skin-related processes, autoimmune diseases, fatty acid metabolism, malignant cell development, premalignant lesions, programmed cell death, endocrinological processes, or AP-1 metabolism.
A composition effective to inhibit abnormal cellular proliferation comprising a first compound which is more potent an activator of a Retinoid X Receptor than a Retinoic Acid Receptor in a co-transfection assay in combination with a second compound which affects cellular proliferation or is a cell-cycle modulator.
Dependencies are inferred from the claim text.