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Claims for Patent: 5,780,676

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Claims for Patent: 5,780,676

Title: Compounds having selective activity for Retinoid X Receptors, and means for modulation of processes mediated by Retinoid X Receptors
Abstract: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.
Inventor(s): Boehm; Marcus F. (San Diego, CA), Heyman; Richard A. (Encinitas, CA), Zhi; Lin (San Diego, CA), Hwang; Chan Kou (San Diego, CA), White; Steve (San Diego, CA), Nadzan; Alex (San Diego, CA)
Assignee: Ligand Pharmaceuticals Incorporated (San Diego, CA)
Application Number:08/485,386
Patent Claims: 1. 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:

3-methyl-7-ethyl-9-(2,6,6-trimethyl-1-cyclohexen-1-yl)-2E,4E,6Z,8E-nonatetr anoic acid,

3-methyl-7-propyl-9-(2,6,6-trimethyl-1-cyclohexen-1-yl)-2E,4E,6Z,8E-nonatet ranoic acid,

3-methyl-7-isopropyl-9-(2,6,6-trimethyl-1-cyclohexen-1-yl)-2E,4E,6Z,8E-nona tetranoic acid,

3,6,7-trimethyl-9-(2,6,6-trimethyl-1-cyclohexen-1-yl)-2E,4E,6Z,8E-nonatetra noic acid,

3-methyl-7-t-butyl-9-(2,6,6-trimethyl-1-cyclohexen-1-yl)-2E,4E,6Z,8E-nonate tranoic acid,

3-methyl-5-{2-[2-(2,6,6-trimethylcyclohexen-1-yl)ethenyl]phenyl}-2E,4E-pent adienoic acid,

3-methyl-5-{2-[2-(2,6,6-trimethylcyclohexen-1-yl)ethenyl]cyclohexyl}-2E,4E- pentadienoic acid,

(2E,4E)-3-methyl-6-{1-[2,6,6-trimethyl-1-cyclohexenyl)ethenyl]cyclopropyl}- 2,4-hexadienoic acid,

(2E,4E,6Z)-7-(5,5,8,8-tetramethyl-5,6,7,8-tetrahydro-2-naphthyl)-3,8-dimeth yl-nona-2,4,6-trienoic acid, and

(2E,4E,6Z)-7-(3,5,5,8,8-pentamethyl-5,6,7,8-tetrahydro-2-naphthyl)-3-methyl -octa-2,4,6-trienoic acid.

2. 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.

3. A therapeutic process according to claim 2, wherein said compound is at least three times more potent an activator of a Retinoid X Receptor than a Retinoic Acid Receptor.

4. A therapeutic process according to claim 2, wherein said compound is at least five times more potent an activator of a Retinoid X Receptor than a Retinoic Acid Receptor.

5. 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.

6. 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.

7. 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.

8. A pharmaceutical composition according to claim 7, wherein said compound is at least three times more potent an activator of a Retinoid X Receptor than a Retinoic Acid Receptor.

9. A pharmaceutical composition according to claim 7, wherein said compound is at least five times more potent an activator of a Retinoid X Receptor than a Retinoic Acid Receptor.

10. 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.

11. A pharmaceutical composition according to claim 10, wherein said compound is at least three times more potent an activator of a Retinoid X Receptor than a Retinoic Acid Receptor.

12. A pharmaceutical composition according to claim 10, wherein said compound is at least five times more potent an activator of a Retinoid X Receptor than a Retinoic Acid Receptor.

13. 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.

14. A method according to claim 13, wherein said compound is at least three times more potent an activator of a Retinoid X Receptor than a Retinoic Acid Receptor.

15. A method according to claim 13, wherein said compound is at least five times more potent an activator of a Retinoid X Receptor than a Retinoic Acid Receptor.

16. 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.

17. A method according to claim 16, wherein said compound is at least three times more potent an activator of a Retinoid X Receptor than a Retinoic Acid Receptor.

18. A method according to claim 16, wherein said compound is at least five times more potent an activator of a Retinoid X Receptor than a Retinoic Acid Receptor.

19. 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.

20. A composition according to claim 19, wherein said first compound is at least three times more potent an activator of a Retinoid X Receptor than a Retinoic Acid Receptor.

21. A composition according to claim 19, wherein said first compound is at least five times more potent an activator of a Retinoid X Receptor than a Retinoic Acid Receptor.

22. A composition according to claim 19, wherein the inhibition of cellular proliferation achieved by said composition at a given concentration is greater than the additive effect achieved by using each of said first and second compounds alone at said given concentration.

23. A composition according to claim 19, wherein said second compound is selected from the group consisting of interferon, methotrexate, fluorouracil, and ARA-C.
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