New 24-benzyl-vitamin D derivs. as hypercalcaemic agents - used to treat hyperproliferative disorders e.g. psoriasis or tumours

摘要

24-Benzyl-vitamin D derivs. (I) are new, where R1 = H; OH; or 1-9C alkanoyloxy; R2 = H; or 1-9C alkanoyl; R3, R4 = H; F; Cl; Br; I; or alkyl, alkyloxy, dialkylamino or alkylthio with 1-8C in alkyl gps. 3 Cpds. (I) are i.e. (5Z,7E,22E)-(1S,3R,24S) -24-benzyl-9,10- secochola-5,7,10(19)22 -tetraene-1,3,24-tril (IA) and the corresp. 24-(4-methoxybenzyl) and 24-(4-fluorobenzyl) cpds. USE/ADVANTAGE - Cpds. (I) are hypercalcaemic agents which also have antiproliferative and cell differentiation activity. They are useful in the treatment of hyperproliferative disorders such as psoriasis and malignant tumours, e.g. leukaemia and breast cancer, and aged skin and for the acceleration of wound heating. Daily dosage is 1 mg, pref. 0.5 mg. The cell differentiation and hypercalcaemic activities of cpds. (I) is more widely sepd. than in 24-cycloalkylmethyl-vitamin D cpds. known from EP-421561.