Benzothiophenes, formulations containing same, and methods

Details Benzothiophenes, formulations containing same, and methods Benzothiophenes, formulations containing same, and methods

C - Chemistry, Metallurgy

07

D

C07D 409/06 (2006.01) A61K 31/44 (2006.01) A61K 31/495 (2006.01) A61K 31/55 (2006.01)

Patent

CA 2199351

The present invention provides class of compounds of formula I (See Fig. I) (I) and their pharmaceutically acceptable salts in which R1 is hydrogen, hydroxy, alkoxy, alkoxycarbonyloxy, alkylcarbonyloxy, arylcarbonyloxy; R~ is hydrogen, hydroxy, alkoxy, alkoxycarbonyloxy, alkylcarbonyloxy, alkylsulfonyloxy, arylcarbonyloxy, Cl or Br; R3 and R4 are independently C1-C4 alkyl, or combine with the nitrogen atom to which they are attached to form a pyrrolidino, piperidino, or hexamethyleneimino ring; X is selected from (See Fig. II, III, IV, V, VI, and VII) and Y is -CO-, -CHOH-, or -CH2-. The compounds and pharmaceutical compositions containing the compounds, either alone or in combination with either progestin or estrogen, are useful for alleviating the symptoms of osteoporosis, cardiovascular related pathological conditions such as hyperlipidemia, and estrogen-dependent cancer. The compounds of the present invention also are useful for inhibiting uterine fibroid disease and endometriosis in - 44 - women and aortal smooth muscle cell proliferation, particularly restenosis, in humans.

La présente invention porte sur une catégorie de composés possédant la formule I (voir fig. I) et sur leurs sels acceptables du point de vue pharmaceutique, dans lesquels R1 est un hydrogène, un hydroxy, un alkoxy, un alkoxycarbonyloxy, un alkylcarbonyloxy, un arylcarbonyloxy; R est un hydrogène, un hydroxy, un alkoxy, un alkoxycarbonyloxy, un alkylcarbonyloxy, un alkylsulfonyloxy, un arylcarbonyloxy, un Cl ou un Br; R3 et R4 sont indépendamment un alkyle en C1-C4 ou se combinent à un atome d'azote auquel ils se fixent pour former une cycle pyrrolidino, pipéridino ou hexaméthylèneimino; X est choisi parmi (voir fig. II, III, IV, V, VI et VII) et Y est un -CO-, un CHOH- ou un -CH2-. Les composés et les préparations pharmaceutiques qui les contiennent, soit seuls ou en combinaison avec la progestine ou un oestrogène, permettent de soulager les symptômes de l'ostéoporose, de maladies cardiovasculaires, telles que l'hyperlipidémie, et de cancers oestrogéno-dépendants. Les composés visés par la présente invention permettent aussi d'inhiber les fibromes utérins et l'endométriose chez la femme, et la prolifération des cellules des muscles lisses de l'aorte, particulièrement la resténose, chez l'humain.

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