ALKYLTHIOPYRIMIDINES AS CRTH2 ANTAGONISTS Russian patent published in 2013 - IPC C07D239/38 C07D239/47 C07D239/58 A61K31/505 A61P35/02 A61P17/00 A61P1/04 A61P11/00 A61P29/00 

FIELD: medicine, pharmaceutics.

SUBSTANCE: invention refers to new alkylthiopyrimidines of formula III or pharmaceutically acceptable salts thereof: In the compound III X represents a direct bond; R² means hydrogen, halogen, (C₁-C₆)alkyl, (C₃-C₇)cycloalkyl, -NR^8aR^8b or the group -SR³; each R³ independently represents (C₁-C₆)alkyl, optionally mono-, di- or trisubstituted by halogen; or (C₃-C₇)cycloalkyl; R^4a and R^4b represent hydrogen; R⁶ represents aryl; or heteroaryl; wherein aryl and heteroaryl are optionally substituted in a substituted position by one or more substitutes specified in a group consisting of (a) halogen; (b) cyano; (c) nitro; (a) hydroxy; (e) guanidino; (f) heteroaryl; (g) phenyl; (h) phenyloxy; (i) benzyl; (j) benzyloxy (k) -NR^8aR^8b; (1) -C(O)R⁹; (m)-C(O)NR^8aR^8b, (n) - OC(O)NR^8aR^8b; (o) -C(O)OR⁹; (p) -NR⁷C(O)0R⁹; (q) -NR⁷C(O)R⁹; (r) sulphamoyl; (s) (C₁-C₆) alkylsulphonyl; (t) (C₁-C₆)alkylaminosulphonyl; (i) di(C₁-C₆)alkylaminosulphonyl; (v) (C₁-C₆)alkyl, optionally mono-, di- or trisubstituted by halogen; (w) (C₁-C₆) alkoxy, optionally mono-, di- or trisubstituted by halogen; and (x)(C₁-C₆)alkylthio, optionally mono-, di- or trisubstituted by halogen R⁷ represents hydrogen. The other radical values are specified in the patent claim.

EFFECT: compounds possess CRTH2 (G-protein related chemoattractant receptor expressed on Th2 cells) antagonist activity and are applicable for treating and preventing the diseases related to CRTH2, including treating allergic diseases, eosinophil and basophile related diseases.

14 cl, 6 dwg, 1 tbl