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

• Main Authors: CLAVENNA GAETANO, MANTOVANINI MARCO
• Format: Patent
• Language: English; Italian
• Published: 29.11.1995
• Edition: 6
• Subjects: HUMAN NECESSITIES; HYGIENE; MEDICAL OR VETERINARY SCIENCE; PREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES

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. Sono descritti acidi ?-amminoalchiltartronici e loro esteri di formula generale (I) (FORMULA I) dove i sostituenti hanno i significati descritti di seguito, e il loro uso nella terapia del dismetabolismo osseo.