DERIVATIVES OF METHYLENEDIPHOSPHONIC ACID, PROCESS OF THEIR PREPARATION AND ANTIPHLOGISTIC AND ANTIRHEUMATIC PHARMACEUTICAL PREPARATION

摘要

Cpds. (I) are new (where R1 is H or opt. branched 1-4C alkyl; R2 is H, alkyl (opt. substd. by hydroxy, mercapto, one or more halo, alkoxycarbon or -NZ1Z2), phenyl (opt. substd. by one or more halo, nitro, lower alkyl, lower alkoxy, trifluoromethyl, amino, carboxy or alkoxy carbonyl gps.), -CX-NZ1Z2, a 5 or 6-membered heterocyclic gp. having 1 or 2 heteroatoms chosen from N and S or a 6-R4-benzoxazole, benzthiazole or benzimidazol-2-yl (Gp.A), Z1, Z2 independently are H or lower alkyl; X is O, NH or S; R4 is H or halo, pref. chloro; R3 is H or hydroxy and n is 0-10 with the condition that when n is 0, then R3 is hydroxy). Antiinflammatories and antirheumatics, used to treat arthritic states, such as rheumatoid arthritis. (I) are administered orally, rectally or parenterally in adult daily doses of 100 mg-5g as several unit doses e.g. capsules contg. 10-500 mg of (I).