To obtain a new dihydrobenzofluorene compound useful for inhibition of bone loss or bone resorption, concretely for inhibition of diseased state relating to cardiovascular organ including osteoporosis and hyperlipidemia.
This compound is expressed by formula I {R1 is H, OH, a 1-4C alkoxy, a group of the formula OCOAr [Ar is a (substituted)phenyl], a 2-6C OSO2-alkyl, etc.; R2 is a halogen or R1; R3 is 1-piperidinyl, 1-pyrrolidinyl, 4-morpholino, etc.; (n) is 2 or 3}, its salt or solvated product, e.g. 3,8- methoxy-11-{4-[2-(1-piperidinyl)ethoxy]phenyl}-11H-5,5-dihydrobenzo[a]fluorene hydrochloride. The compound of the formula I can be produced by reacting a compound of formula II [R1a is H or a group of the formula OR5 (R5 is an OH-protecting group); R2a is a halogen or R1a] with a compound of the formula R3-(CH2)n-Q (Q is Br or Cl) and optionally removing the OH-protecting group from the product.
CROWELL THOMAS ALAN
JONES CHARLES DAVID
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