| 摘要 |
Phosphonic acid derivs. of formula (I) and their salts are new. R1 is an aromatic residue Z is a bond or -[(CH2)n-Z1]-(1a) n is 0-3 Z1 is O, opt. oxidised S or opt. aliphatic substd. imino. alk1 and alk2 are each alkylene R1 and R2 are each aliphatic gps. 17 cpds. are specifically claimed e.g. 3-[N-(3-phenylpropyl)-N, N-dimethylammoniol]-1- hydroxy-propane-1, 1-diphosphonate and its salts. prepn. of (I) e.g. by reacting RA-N(R2)-alk-C(PO3H2)-OH with Rb-Y under reducing conditions and with a cpd. Rb'=O (RA = R3; R3 and RB' = R1 -Zo-alk1; Y is a reactive OH gp., ZO = O, S or opt. aliphatic-substd. imino; Z1 is -NRo-; Ro = an amino protecting gp) is claimed. USE/ADVANTAGE - Calcium metabolism regulating agents. (I) can be used in treatment of inflammatory conditions in joints, musculosketal degenerative processes e.g. osteoporosis and in treatment of calcium deposition in blood vessels or in prosthetic implants.
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