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US 2012/0258996 A1Published application
Novel ligands that modulate rar receptors
AssigneeGalderma Research & Development
InventorsThibaud BIADATTI, Laurence DUMAIS, Catherine SOULET, Sandrine TALANO, Sebastien DAVER
Life of this patent
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Abstract
Novel ligand compounds having the general formula (I): and pharmaceutical/cosmetic compositions comprised thereof are useful in human and veterinary medicine or, alternatively, in cosmetics.
Claims21
A method:
- 1) for treating a disorder of keratinization selected from the group consisting of ichtyoses, an ichthyosiform condition, Darier's disease, palmoplantar keratoderma, a leucoplakiform condition, cutaneous lichen and mucosal (oral) lichen,
- 2) for treating a dermatological condition, disorder or affliction having an inflammatory immunoallergic component, with or without cell proliferation disorder, selected from the group consisting of cutaneous psoriasis, mucosal psoriasis, ungual psoriasis, psoriatic rheumatism, cutaneous atopy, eczema, respiratory atopy and gingival hypertrophy,
- 3) for treating a dermal or epidermal proliferation, whether benign or malignant and whether or not of viral origin, common warts, flat warts and epidermodysplasia verruciformis, florid or oral papillomatoses, T lymphoma, and the proliferations which can be induced by ultraviolet radiation, basal cell and prickle cell epithelioma, precancerous skin lesions and keratoacanthomas,
- 4) for treating immune dermatoses, lupus erythematosus, immune bullous disease, collagen disease or scleroderma,
- 5) for the treatment of a dermatological or general condition having an immunological component,
- 6) for the treatment of a skin disorder due to exposure to UV radiation, for repairing or combating skin aging, whether photoinduced or chronologic, or for reducing actinic keratoses and pigmentations, or any pathology associated with chronologic or actinic aging, xerosis,
- 7) for combating a disorder of the sebaceous function selected from the group consisting of hyperseborrhoea of acne and simple seborrhoea,
- 8) for treating disorders of cicatrization or for repairing stretch marks,
- 9) for the treatment of a disorder of pigmentation, hyperpigmentation, melasma, hypopigmentation or vitiligo,
- 10) for the treatment of conditions of the metabolism of lipids, obesity, hyperlipidaemia or non-insulin-dependent diabetes,
- 11) for the treatment of inflammatory conditions, arthritis,
- 12) for the treatment of cancerous or precancerous conditions,
- 13) for the treatment of alopecia of various origins, or alopecia due to chemotherapy or to radiation,
- 14) for the treatment of a disorder of the immune system selected from the group consisting of asthma, type I diabetes mellitus, multiple sclerosis or other selective dysfunctions of the immune system, or
- 15) for the treatment of a condition of the cardiovascular system, arteriosclerosis or hypertension,
- comprising administering to an individual in need of such treatment, a thus effective amount of a pharmaceutical composition comprising a pharmaceutically effective amount of at least one ligand compound having the formula (I) below:
- in which:
- R1 is a hydrogen atom, an alkyl radical of 1 to 4 carbon atoms or a —CF3 radical;
- R2 is a hydrogen atom, an alkyl or alkoxy radical of 1 to 4 carbon atoms or a chlorine atom;
- R3 is a hydrogen atom or a linear or branched alkyl or alkoxy radical of 1 to 10 carbon atoms optionally substituted with a methoxy group;
- R4 is a hydrogen atom or an alkyl radical of 1 to 3 carbon atoms;
- R5 is a hydrogen atom or an alkyl radical of 1 to 3 carbon atoms;
- or alternatively R4 and R5 form, together with the bond —N—C(═Y)—, a pyrrolidine, pyrrolidinone, piperidine or piperidinone ring;
- Y is two hydrogen atoms or a hetero atom;
- Ar is a 1,4-phenyl, 2,5-pyridyl, 5,2-pyridyl or 2,5-thiophenyl ring;
- X is an oxygen atom optionally substituted with an alkyl or alkylamine radical or a C—C single bond;
- A is a hydrogen atom or the following formula:
- in which,
- Q is an oxygen atom or an —NH— bond;
- R6 is a hydrogen atom, an alkyl radical of 1 to 6 carbon atoms, a cycloalkyl radical of 3 to 6 carbon atoms or a —C(O)CH3 or —C(O)CH2CH3 radical;
- R7 and R7′ represent, independently of each other, a hydrogen atom or a hydroxyl group, with the proviso that R7 and R7′ are not simultaneously a hydroxyl group;
- n is 0, 1, 2, 3, 4 or 5;
- or a salt of a compound of formula (I) when R3 is a hydrogen atom, or a geometrical isomer of a compound of formula (I);
- formulated into a pharmaceutically and physiologically acceptable medium therefor.
31 more elements
Dependencies are inferred from the claim text.