Retinoid antagonists and use thereof

Details Retinoid antagonists and use thereof Retinoid antagonists and use thereof

C - Chemistry, Metallurgy

07

C

C07C 57/42 (2006.01) A61K 31/00 (2006.01) A61K 31/19 (2006.01) A61K 31/203 (2006.01) A61K 31/231 (2006.01) A61K 31/232 (2006.01) C07C 45/00 (2006.01) C07C 45/29 (2006.01) C07C 45/71 (2006.01) C07C 47/232 (2006.01) C07C 47/47 (2006.01) C07C 59/64 (2006.01) C07C 59/72 (2006.01) C07C 69/734 (2006.01)

Patent

CA 2366186

The present invention relates to novel retinoid antagonists of the formula (I) wherein the dotted bond is optional; and, when the dotted bond is present, R1 is lower alkyl and R2 is hydrogen; and, when the dotted bond is absent, R1 and R2 taken together are methylene to form a cis-substituted cyclopropyl ring; R3 is hydroxy or lower alkoxy; R4 is alkyl or alkoxy; and R5 and R6 are, independently, a C4-12 alkyl group or a mono- or polycyclic C5-12-hydrocarbon group which are linked to the phenyl ring through a quaternary carbon atom, and pharmaceutically acceptable salts of carboxylic acids of formula (I); the use of retinoid antagonists, their pharmaceutically acceptable salts or pharmaceutically acceptable hydrolyzable esters, for the manufacture of a medicament for the treatment of T-helper cell type 2 (Th2)-mediated immune diseases, for the manufacture of a medicament for the treatment of osteoporosis and for use in the treatment of preneoplastic and neoplastic diseases.

La présente invention concerne des antagonistes rétinoïques et certains des sels d'acides carboxyliques pharmaceutiquement acceptables, représentés par la formule (I). Dans cette formule, le tireté est une liaison facultative. Lorsque celle-ci est présente, R<1> est alkyle inférieur et R<2> est hydrogène, mais lorsque cette liaison est absente, R<1> et R<2> pris ensemble sont méthylène pour former un cyclopropyle cis-substitué. R<3> est hydroxy ou alcoxyle inférieur. R<4> est alkyle ou alcoxyle. R<5> et R<6> sont, indépendamment, un groupe C4-C12 alkyle ou un groupe C5-C12 hydrocarbure monocyclique ou polycyclique qui sont liés au cycle phényle par un carbone quaternaire. On utilise des antagonistes retinoïques, leurs sels pharmaceutiquement acceptables ou leurs esters hydrolysables pharmaceutiquement acceptables, pour la fabrication d'un médicament destiné au traitement des maladies immunes liées au lymphocyte T-4 de type 2 (Th2), pour la fabrication d'un médicament destiné au traitement de l'ostéoporose et au traitement des maladies prénéoplasiques et néoplasiques.

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