New 10,19-methylene-9,10-seco-pregnane derivs. - useful as vitamin=D analogues with anti-proliferative activity

摘要

9,10-Secopregnane derivs. of formula (I) are new. In (I), R1 is 1-10C alkyl or 2-10C alkenyl, opt. contg. 1-3 additional functional gps. R2 and R3 are H, 1-6C alkanoyl, or 3-6C alkenoyl. Specific (I) are alpha-hydroxy-10,19 methylene-ergocalciferol alpha-hydroxy-10,19- methylene-cholecalciferol, alpha,25-dihydroxy-10,19 methylene-chlorocalciferol. USE/ADVANTAGE - (I) are vitamin D analogues with approx. the same activity as known vitamin D cpds. (contg. a 10,19 double bond) w.r.t. proliferation inhibiton and cell differentiation, but with reduced activity w.r.t. Ca and phosphate metabolisation and with better chemical stability. They may be used in the treatment of tumours, psoriasis, etc.