RU95116371A - COMPLEX 17-DEOXY-CORTICOSTEROID-21 (0) -SERVATES OF CARBONIC ACIDS, METHOD OF THEIR RECEIVING, CONTAINING THEIR MEDICINAL PROPERTIES, METHOD OF ITS PRODUCTION AND METHOD OF TREATING DERMATOSIS - Google Patents

Claims (6)

1. Complex 17-deoxycorticoid-21 is a carboxylic acid ester of the formula (I)

in which A represents CHOH or CHCl in any spatial arrangement;
CH ₂ , C = O, or (9) (11) is a double bond;
Y represents hydrogen, fluorine or chlorine;
Z is hydrogen, fluorine or methyl;
R (1) means, if necessary, substituted or annelated aryl, heteroaryl;
/ (C ₁ - C ₄ ) - alkyl / is saturated, starting with C _{2 is} also singly unsaturated, since C _{3 is} also repeatedly unsaturated or cyclic, branched due to other alkyl groups with O, S, N heteroatoms or substituted, moreover, the positions 1, 2 are saturated or unsaturated (1, 2 is a double bond);
R (2) is hydrogen, α- or β-methyl.  2. The complex 17-deoxycorticoid-21 is a carboxylic ester of the formula (I) according to claim 1, characterized in that in it: R (1) has the meaning indicated in paragraph 1; A stands for CHOH (β-configuration); Y denotes F; Z is hydrogen; R (2) is α-methyl. 3. The method of obtaining the compounds of formula (I) under item 1, characterized in that a) a compound of formula (II)

in which R (4) denotes OH, and the remaining substituents have the above meanings, they enter into interaction a1) with an activated carboxylic acid of formula (III), preferably with an acid halide or anhydride or azolide
R (5) - CO - / (C ₁ - C ₄ ) -alkyl / - R (1) (III),
moreover, / (C ₁ - C ₄ ) -alkyl / and R (1) have the above values and R (5) means Cl, Br, O [- CO - / (C ₁ - C ₄ ) -alkyl / - R (1 )] ₁ -, OC (O) CF ₃ or another activated acid radical, or a2) with the carboxylic acid itself of formula (III), in which R (5) = OH, and other substituents are indicated in formula (III), in the presence of water-cleaving reagent (DSSl, etc.), or b) the compounds of formula (II)

in which R (4) is Br, J, an aryl or alkyl sulfate ester group, and the other substituents are as defined in the case of formula (I), they are reacted with a salt, preferably a salt of Na or K or a trialkylammonium salt of a carboxylic acid of the formula (Iii)
R (5) - CO - / (C ₁ - C ₄ ) -alkyl / - R (1),
in which R (5) means - / O ^- Me ⁺ /, and the other substituents are as indicated in the case of formula (III), wherein Me ⁺ preferably denotes an alkali metal salt or a trialkyl ammonium salt cation.  4. Drug, characterized in that it contains as an active substance the compounds of formula (I) according to claim 1 in an effective amount.  5. A method of treating dermatoses, characterized in that an effective amount of a compound of formula (I) according to claim 1, combined with pharmaceutically conventional additives, is applied to the affected skin.  6. The method of obtaining a medicinal product for the treatment of dermatoses, characterized in that they mix an effective amount of the compounds of formula I with pharmaceutical additives.