FIELD: organic chemistry, medicine, pharmacy.
SUBSTANCE: invention relates to derivatives of carboxylic acids of the formula (I): 
wherein R1 means -COOH, -COOR4, -CH2OH, -CONR5SO2R6, -CONR7R8, -CH2NR5SO2R6, -CH2NR9COR10, -CH2NR9CONR5SO2R6, -CH2SO2NR9COR10, tetrazole, 1,2,4-oxasizol-5-one, 1,2,4-oxadiazol-5-thione, 1,2,4-thiadiazol-5-one or 1,2,3,5-oxathiadiazol-2-one; A means: (ii) (C1-C6)_alkylene; (iii) (C2-C6)-alkenylene; (iv) (C2-C6)-alkynylene; (v) -O-(C1-C3)-alkylene; (vii) -NR20-(C1-C3)-alkylene; (viii) -CONR21-(C1-C3)-alkylene; (ix) (C1-C3)-alkylene-O-(C1-C3)-alkylene; (xi) (C1-C3)-alkylene-NR20-(C1-C3)-alkylene; (xiv) -(C1-C4)-alkylene-Cyc1; cycle B means (C6-C10)-unsaturated mono- or bicarbocyclic fragment or 5-10-membered saturated, partially saturated or unsaturated mono- or biheterocyclic fragment comprising 1 atom of sulfur, nitrogen or oxygen; R2 means (C1-C6)-alkoxy-group, halogen atom; m = 0, 1; n = 1 if -D-R3 is added to B cycle in ortho-position with respect to -A-R; n = 0 if -D-R3 is added to B cycle in position distinct from ortho-position with respect to -A-R1; Q mans (1) (i) -(C1-C4)-alkylene, (C2-C4)-alkenylene-Cyc2; (ii0 -(C1-C4)-alkylene-Z-Cyc3; (iii) (C1-C4)-alkyl substituted with substitute(s) chosen from -NR24R25, -S(O)pR26, cyano-group, -NR23COR27, -NR23SO2R28 and -NR23CONR24R25; (iv) (C1-C4)-alkoxy-(C1-C4)-alkoxy-group, -NR23COR27, -COR28, -OSO2R28, -NR23SO2R28; (v) C6-unsaturated monocarbocyclic fragment or 6-membered fully saturated monoheterocyclic fragment comprising 1 atom of nitrogen that is substituted with 1-5 R30 wherein one of R30 is bound with a cycle by position distinct from position 1; (vi) 9-membered fully saturated, partially saturated or unsaturated biheterocyclic fragment comprising 2 atoms chosen from nitrogen, sulfur and oxygen that can be unsubstituted or substituted with 1-5 R30; (vii) -T-Cyc5; (viii) -L-Cyc6-1, -L-(C3-C6)-cycloalkyl, -L-(C2-C4-alkylene)-Cyc6-2, or -L-(C1-C4-alkylene)q-Cyc6-3 wherein cycloalkyl is unsubstituted; (2) (i) phenoxy-group; (ii) benzyloxy-group; (iii) hydroxy-(C1-C4)-alkyl; (iv) (C1-C4)-alkoxy-(C1-C4)-alkyl, or (iv) (C1-C4)-alkylene-O-benzyl, or (v) cyano-group; (vi) -NR33R34; (vii) -CONR33R34; D means (1) -CH2-, -O-CH2-, -CONH-, -NHSO2-, -NHCO- or -CO-CH(CH3)-,; (2) -(CH2)3-, -(CH2)5-, -CH=CH-(CH2)3- and so on; R3 means (1) (C1-C6)-alkyl or (2) (C6-C10) fully or partially saturated or unsaturated mono- bicarbocyclic fragment, or 5-15-membered partially or fully saturated or unsaturated mono-, bi- or triheterocyclic fragment comprising 1-3 atoms of nitrogen, oxygen or sulfur and substituted with 1-5 R42 or unsubstituted fragment, or its nontoxic salt. Also, invention relates to a pharmaceutical composition possessing antagonistic activity to EP3 and/or EP4 and comprising the effective amount of compound of the formula (I), or its nontoxic salt and a pharmaceutically acceptable carrier, and to using these compounds in treatment of diseases mediated by activity of EP3 and/or EP4. Invention proposes derivatives of carbocyclic acids possessing antagonistic activity to EP3 and/or EP4.
EFFECT: valuable medicinal properties of compounds and pharmaceutical composition.
17 cl, 1369 ex
