USE OF VITAMIN D DERIVATIVE FOR TREATING DERMATOLOGICAL STATES, VITAMIN D DERIVATIVE, PROCESS OF ITS PREPARATION AND PHARMACEUTICAL COMPOSITION CONTAINING THEREOF

摘要

PCT No. PCT/EP96/00176 Sec. 371 Date Jul. 21, 1997 Sec. 102(e) Date Jul. 21, 1997 PCT Filed Jan. 17, 1996 PCT Pub. No. WO96/22776 PCT Pub. Date Aug. 1, 1996A method of using vitamin D derivatives of the formula IMAGE I wherein X is =CH2 or H,H; Y is a moiety-CH(CH3)-(A)n-C(O)-OR1(a)-CH(CH3)-CH2-O-C(O)-R2(b)or-C(O)-OR1(c);A is -CH=CH- or CH2-CH2-R1 is lower alkyl, cycloalkyl, cycloalkylmethyl, -CH2R3 or -CH2-CH2R3; R2 is lower alkyl, cycloalkyl or R3; R3 is hydroxy-lower alkyl, hydroxy-cycloalkyl or trifluoromethyl-hydroxy-lower-alkyl; n is 0 or 1; and the dotted bond in the five membered ring is optional; in the treatment of dermatological conditions, in particular keratinization disorders such as psoriasis, as well as acne and photodamaged skin, is described. Vitamin D derivatives of the formula I above, wherein X, Y, A, R1, R2, R3 and n are as set forth above; with the proviso that X is H,H when Y is -CH(CH3)-CH2-OC(O)-C(OH)(CH3)2 and the dotted bond in the five-membered ring is not present; as well as a process for the preparation of the compounds of formula I, and pharmaceutical compositions containing a compound of the formula I wherein X, Y, A, R1, R2, R3 and n are set forth above; with the proviso that X is H,H when Y is -CH(CH3)-CH2-OC(O)-C(OH)(CH3)2 and the dotted bond in the five-membered ring is not present, are also described.