FIELD: organic chemistry, pharmacy. SUBSTANCE: invention relates to compounds of the formula (I) R4-A-CH(R3)N(R2)B-R1 where A means optionally substituted phenyl group under condition that groups -CH(R3)N(R2)B-R1 and -OR4 are at 1,2-position in ring carbon atoms relative to one another and under condition that ring atom at orthoposition with respect to OR4-bound group (and, therefore, at 3-position with respect to -CHR3NR2-binding group) is not substituted; B means pyridyl or pyridazinyl; R1 in ring B at 1,3- or 1,4-position with respect to -CH(R3)N(R2)-binding group and means carboxy-, carbamoyl- or tetrazolyl-group; or R1 means the group of the formula -CONRaRa1 where Ra means hydrogen atom or C1-6-alkyl; Ra1 means C1-6-alkyl; or R1 means the group of the formula -CONHSO2Rb where Rb means C1-6-alkyl, trifluoromethyl or 5-membered heteroaryl taken among isoxazolyl and thiadiazolyl optionally substituted with C1-6-alkyl or C1-4- alkanoylamino-group; R2 means C1-6-alkyl; R3 means hydrogen atom; R4 means C1-4-alkyl, C3-7-cycloalkyl-C1-3-alkyl or C3-7-cycloalkyl where indicated C1-6-alkyl is optionally substituted with hydroxy-group or halogen atom, or their pharmaceutically acceptable salt or ester hydrolysable in vivo. Compounds are antagonists of the pain- enhancing effect of prostaglandins of type E. Invention discloses also method of synthesis of indicated compounds, intermediate compounds used for their synthesis, pharmaceutical composition for elimination of pain and method of analgesia. EFFECT: valuable medicinal properties of compounds and pharmaceutical composition. 11 cl, 1 tbl, 68 ex
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Authors
Dates
2002-05-20—Published
1996-06-17—Filed