Retinoic acid agonist as a prophylactic and therapeutic...

Details Retinoic acid agonist as a prophylactic and therapeutic... Retinoic acid agonist as a prophylactic and therapeutic...

A - Human Necessities

61

K

A61K 31/695 (2006.01) A61K 31/00 (2006.01) A61K 31/19 (2006.01) A61K 31/40 (2006.01) A61K 31/4025 (2006.01) A61K 31/415 (2006.01) A61K 31/4155 (2006.01) A61K 31/455 (2006.01) A61K 31/47 (2006.01) A61K 31/475 (2006.01) A61K 31/495 (2006.01) A61K 31/498 (2006.01) A61K 31/53 (2006.01) A61K 31/535 (2006.01) A61K 31/55 (2006.01)

Patent

CA 2307613

Therapeutic or preventive agents for systemic lupus erythematosus, glomerulonephritis, lupus nephritis, idiopathic thrombocytopenic purpura or autoimmune anemia, which can be substituted for conventional steroid preparations or immunosuppressive agents. The active ingredients of the therapeutic or preventive agents are agonists for retinoic acid receptors, particularly retinoic acid receptor, subtype .alpha. (i.e., RAR .alpha.), and examples of the agonists include (1) carboxylic acid derivatives bearing fused rings as represented by general formula (I) wherein rings L and M are fused with each other, and are each independently an optionally substituted aromatic hydrocarbon ring or an optionally substituted heterocycle; rings A and B are each independently an optionally substituted aromatic hydrocarbon ring or a heterocycle; and D is optionally protected carboxyl, and (2) 4-{[(3,5- bistrimethylsilylphenyl)carbonyl]amino}benzoic acid and 4-{2-[5-(3- methoxymethyl-5,6,7,8-tetrahydro-5,5,8,8-tetramethylnaphthalen-2-yl)- pyrrolyl]}benzoic acid.

L'invention porte sur des agents thérapeutiques ou préventifs agissant sur le lupus érythémateux, la néphrite glomérulaire, la néphrite lupique, la purpura thrombopénique idiopathique ou l'anémie auto-immune, et se substituant aux préparations usuelles de stéroïdes et aux agents immunosuppresseurs. Les ingrédients actifs desdits agents thérapeutiques ou préventifs sont des agonistes des récepteurs de l'acide rétinoïque et en particulier de son sous-type .alpha. (le RAR .alpha.). Parmi les exemples d'agonistes se trouvent: (1) des dérivés de l'acide carboxylique à anneaux fusionnés de formule générale (I) (dans laquelle: les anneaux L et M fusionnés entre eux sont chacun indépendamment un cycle d'hydrocarbure aromatique facultativement substitué ou un hétérocycle facultativement substitué; les cycles A et B sont chacun indépendamment un cycle d'hydrocarbure aromatique facultativement substitué ou un hétérocycle; et D est un carboxyle facultativement protégé), et (2) l'acide 4-([(3,5-bistriméthylsilylphényl)carbonyl]amino) benzoïque, et l'acide 4-(2-[5-(3-méthoxyméthyl-5,6,7,8-tétrahydro-5,5,8,8-tétraméthylnaphtalène-2-yl)-pyrrolyl]) benzoïque.

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