ISOFLAVONE DERIVATIVES

摘要

The present invention relates to isoflavone, isoflavan-4-one and isoflavane derivatives of general formula (I), their salts, pharmaceutical compositions containing the compounds of general formula (I), and to a process for preparing the same. In general formula (I), if n is 0, R?5 and R6¿ together stand for an oxo group and the dotted line means a double bond, R1 represents C¿1-18?alkyl substituted by alkylcarbonyl, carboxy, sulfonic acid, hydroxy, phenoxy, piperidino, morpholino or piridino or by a (C1-4alkyl)2N-(CH2)mCO(CH2)p- or by (C1-4alkyl)2N-(CH2)mOCO(CH2)p- group; or stands for C3-6cycloalkyl or cycloalkenyl; or if n is 1, R?5 and R6¿ together stand for an oxo group and the dotted line means a double bond, R1 represents C¿1-18?alkyl optionally substituted by alkyl-carbonyl, alkoxycarbonyl, carboxy, sulfonic acid, hydroxy, phenoxy, piperidino, morpholino or piridino or by a (C1-4alkyl)2N-(CH2)mCO(CH2)p- group; or stands for C3-6-cycloalkyl or cycloalkenyl or C2-6alkenyl; or if n is 0 or 1, R?5 and R6¿ together stand for an oxo group or stand separately for hydrogen and the dotted line does not mean a chemical bond, R1 represents C¿1-18?alkyl optionally substituted by alkyl-carbonyl, alkoxycarbonyl, carboxy, sulfonic acid, hydroxy, alkoxy, phenyl optionally substituted by a halo atom, phenoxy, piperidino, morpholino or piridino or by a (C1-4alkyl)2N-(CH2)mCO(CH2)p- group; or stands for C3-6-cycloalkyl or C2-6alkenyl; or R stands for C1-8alkyl, halogen, C1-4alkoxymethyl, C2-5-acyloxymethyl, or hydroxymethyl; R?4¿ stands for hydrogen or C¿1-4?alkyl; R?2 and R3¿ stand for hydrogen or C¿1-6?alkoxy; R?5 and R6¿ together stand for an oxo group or separately stand for hydrogen; the dotted line means a double bond being optionally present; n is 0 or 1; m is an integer from 1 to 4; and p is an integer from 1 to 4. The compounds of general formula (I) can be used for the prevention and treatment of osteoporosis. They are prepared by methods well known in the organic chemistry.