New vitamin=D derivs. - are cell differentiators and proliferation inhibitors useful for treating psoriasis and malignant tumours

摘要

Vitamin D derivs. of formula 8I) are new. In (I), R1 = H, OH or 1-9C acyloxy; R2 = H or 1-9C acyloxy; A = a direct bond or -CH2-; B, D = H or together form another bond in the E configuration. One of R3 and R4 = OH or 1-9C acyloxy and the other is H, or both gps. together form = O. X = -(CH2)n- or -(CH2)nO- (where n = 1-3); R5, R6 = independently up to 4C alkyl, CF3 or together form a 5-6 membered (un)satd. or aromatic carbocycle or heterocycle. 14 cpds. are specifically claimed, including (5Z,7E,22E)-(1S,3R,24R) -9,10-seco-24a-homo 5,7,10(19),22-cholestatetraer -1,3,24-triol. Also claimed is a method for preparing (I) from the corresp. enone of formula (II), where R1 = H or protected OH and R2' = a protecting gp. USE/ADVANTAGE - For the treatment of diseases associated with abnormal mitosis, namely psoriasis and malignant tumours. (I) have only a weak effect on calcium and phosphate metabolism, and therefore fewer side effects at high doses.