Use of crth2 antagonist compounds in therapy

Details Use of crth2 antagonist compounds in therapy Use of crth2 antagonist compounds in therapy

C - Chemistry, Metallurgy

07

D

C07D 209/08 (2006.01) A61K 31/404 (2006.01) A61K 31/426 (2006.01) A61K 31/427 (2006.01) A61K 31/4709 (2006.01) C07D 401/06 (2006.01) C07D 413/06 (2006.01) C07D 417/06 (2006.01)

Patent

CA 2543199

Compounds of general formula (I) wherein R1, R2 , R3 and R4 are independently hydrogen, halo,C1-C6 alkyl, -O(C1-C6 alkyl), -CON(R11)2 , -SO11, -SO2R11, - SO2N(R11)2, -N(R11)2, -NR11COR11, -CO2R11, -COR11, -SR11, -OH, -NO2 or -CN; each R11 is independently hydrogen or C1 -C6 alkyl; R5 and R6 are each independently hydrogen, or C1-C6 alkyl or together with the carbon atom to which they are attached forrn a C3-C7 cycloalkyl group; R7 is hydrogen or C1- C6 alkyl; R8 is an aromatic moiety optionally substituted with one or more substituents selected from halo, C1-C6 alkyl, -O(C1-C6)alkyl, -CON(R11)2, - SOR11, -SO2R11 , -SO2N(R11)2, -N(R11)2, -NR11COR11, -CO2R11, -COR11, -SR11, - OH, -NO2 or -CN; wherein R11 is as defined above; R9 is hydrogen, or C1-C6 alkyl; provided that: R8 is not phenyl substituted with -COOH; when any two of R1, R2 , R3 and R4 are hydrogen, neither of the other two of R1, R2 , R3 and R4 is C3-C6 alkyl; and their pharmaceutically acceptable salts, hydrates, solvates, complexes or prodrugs are useful in the preparation of pharmaceuticals for the treatment of allergic diseases such as asthma, allergic rhinitis and atopic dermatitis.

La présente invention a trait à des composés de formule générale (I), dans laquelle : R?1¿, R?2¿, R?3¿ et R?4¿ sont indépendamment hydrogène, halo, alkyle en C¿1?-C¿6?, -O(alkyle en C¿1?-C¿6?), -CON(R?11¿)¿2?, -SOR?11¿, -SO¿2?R?11¿, -SO¿2?N(R?11¿)¿2?, -N(R?11¿)¿2?, -NR?11¿COR?11¿, -CO¿2?R?11¿, -COR?11¿, -SR?11¿, -OH, -NO¿2? ou CN ; chaque R?11¿ est indépendamment hydrogène ou alkyle en C¿1?-C¿6 ?; R?5¿ et R?6¿ sont chacun indépendamment hydrogène ou alkyle en C¿1?-C¿6? ou ensemble avec l'atome de carbone auquel ils sont liés forment un groupe cycloalkyle en C¿3?-C¿7?; R?7¿ est hydrogène ou alkyle en C¿1?-C¿6 ?; R?8¿ est un groupe fonctionnel aromatique éventuellement substitué avec un ou des substituants choisis parmi halo, alkyle en C¿1?-C¿6?, -O(alkyle en C¿1?-C¿6?), -CON(R?11¿)¿2?, -SOR?11¿, -SO¿2?R?11¿, -SO¿2?N(R?11¿)¿2?, -N(R?11¿)¿2?, -NR?11¿COR?11¿, -CO¿2?R?11¿, -COR?11¿, -SR?11¿, -OH, -NO¿2? ou CN où R?11¿ est tel que défini plus haut ; R?9¿ est hydrogène ou alkyle en C¿1?-C¿6 ?; à condition que : R?8¿ de soit pas phényle substitué par -COOH ; lorsque deux parmi R?1¿, R?2¿, R?3¿ et R?4¿ sont hydrogène, aucun des deux autres parmi R?1¿, R?2¿, R?3¿ et R?4¿ n'est alkyle en C¿3?-C¿6?; ainsi qu'à leurs sels, hydrates, solvates, complexes ou prodrogues pharmaceutiquement acceptables utiles dans la préparation de produits pharmaceutiques pour le traitement de maladies allergiques telles que l'asthme, la rhinite allergique et la dermatite atopique.

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