New tartronic acid derivs. - useful in treatment of, e.g., Paget's syndrome and osteoporosis

摘要

Tartronic acid derivs. of formula (I), and their optically active forms, enantiomers, diastereomers and related mixts., and their salts, are new: Ra, Rb = H, an alkali(ne earth) metal, an ammonium or 1-10C alkylammonium cation, 1-4C alkyl, 1-4C alkoxyethyl, alkyl or p-methoxybenzyl; B = H, 2-12C acyl, or a gp. of formula (i) Q = CH2, O or S; R = phenyl, 4-biphenyl, 3,4,4-tri-(1-4C alkoxyphenyl, 3,5-di(1-4C alkoxy)phenyl, 4-hydroxy-3,5-di(1-4C alkoxy) phenyl (and 1-7C acyloxy derivs.), 4-hydroxy-3,5-di-tert-butylphenyl, 3,5-di-trifluoromethylphenyl, fur-2-yl, 5-dimethylaminomethyl-fur-2-yl, 7-methoxy-coumarin-4-yl, 6,7-dimethoxy-coumarin-4-yl, 4-oxo-thiazolidin-3-yl (substd.), 1-12C alkyl, 2-12C alkenyl, 2-12C alkynyl, 3-12C cycloalkyl, 3-12C cycloalkenyl, or R2R3N(CH2)mCHR1; R1 = H, phenyl, benzyl or 1-4C alkyl; R2, R3 = H, 1-4C alkyl, boc, fmoc, benzyloxycarbonyl, aminocarbonyl p-methoxybenzyloxycarbonyl or 1-4C alkylaminocarbonyl; or NR2R3 = a gp. of formula (II), or when R3 is H, 1-4C alkyl, 1-4C acyl, aminocarbonyl, benzyl, 1-4C alkoxy-carbonyl or p-methoxybenzyl, then CR1NR2 may be linked to form a 5-7 membered N-heterocycle; X = a bond, CH2, O, S or NRc; Rc = H, 1-4C alkyl, 1-4C alkoxycarbonyl, aminocarbonyl, boc, fmoc, benzyloxycarbonyl, p-methoxy-benzyloxycarbonyl, phenyl, benzyl or benzhydryl; m = 0-3; n = 1-12; p = 2 or 3; provided that m and n are not both O when Ra, Rb, B and R1 are H and R2, R3 are H or Me or NR2R3 is piperidine.