| 摘要 |
FIELD: organic chemistry, pharmacy. SUBSTANCE: invention relates to derivatives of pyrazole of the general formula (I) <EMI ID=0.221 HE=30 WI=24 TI=CHI> or their pharmaceutically acceptable acid additive salts where A means CH<SB>2</SB>; R<SB>1</SB> is C<SB>1-6</SB>-alkyl or phenyl; X<SB>1</SB> - covalent bond or S; R<SB>3</SB> is C<SB>1-6</SB>-alkyl; Y is 2,4,6-trisubstituted phenyl where a substituent is taken from chlorine atom, methyl- or trifluoromethyl-group being phenyl has not more one trifluoromethyl-group as a substituent; Z - a group of the formula (a) <EMI ID=0.222 HE=24 WI=30 TI=CHI> where R<SB>4</SB> - H or C<SB>1-6</SB>-alkoxy-group; R<SB>5</SB> - H, -CH<SB>2</SB>OR<SB>6</SB>; R<SB>6</SB> - H or C<SB>1-6</SB>-alkyl; or a group of the formula (b) <EMI ID=0.223 HE=24 WI=27 TI=CHI> where K and J - CH or one of them means CH and another - nitrogen; R<SB>14</SB> - hydroxy-, alkoxy-group or a group X<SB>2</SB>-(CH<SB>2</SB>)<SB>r</SB>OR<SB>6</SB> where X<SB>2</SB> - covalent bond or oxygen atom; r = 1 or 2. Compounds show an activity of antagonists of corticotropin-releasing factor. EFFECT: enhanced effectiveness of compounds and composition as antagonists. 9 cl, 4 tbl, 13 ex |
