FIELD: medicine; pharmaceuticals.
SUBSTANCE: invention relates to compounds of formula I possessing RORγ inhibitor properties activity and a pharmaceutical composition based thereon for treating RORγ-mediated diseases or conditions. In general formula I A1 is NR1 or CR1, where R1 is H or methyl, where methyl, if present, is optionally substituted with one or more F; cyclopropyl part can be optionally substituted with one or more methyl and one or more F; A2-A5 are N or CR2-CR5, respectively, provided that one of four positions A in A2-A5 can be N; R2-R5 independently are H, halogen, or C(1-6) alkyl; R6 and R7 independently are H, methyl, or hydroxyl, wherein all alkyl groups, if present, optionally substituted with one or more F; R8 is H or C(1-2) alkyl; A9-A12 are N or CR9-CR12, respectively, provided that one of the four positions A in A9-A12 can be N; R9-R12 independently are H, halogen, C(1-3) alkoxy, or C(1-6) alkyl; R13 is H, C(1-6) alkyl, C(2-6) alkenyl, C(3-6) cycloalkyl, C(3-6) cycloalkyl-C(1-4) alkyl, C(2-5) heterocycloalkyl, C(2-5) heterocycloalkyl-C(1-4) alkyl, C(6-10) aryl, C(6-10)aryl-C(1-4) alkyl, C(1-9) heteroaryl or C(1-9) heteroaryl-C(1-4) alkyl, all groups are optionally substituted with one or more halogen, amino, hydroxyl, cyano, C(1-3) alkoxy, C(1-3) alkoxycarbonyl, (di)C(1-3)alkylamino or C(1-3)alkyl; and R14 is H, C(1-6)alkyl, C(2-6)alkenyl, C(3-6)cycloalkyl, C(3-6)cycloalkyl-C(1-4)alkyl, C(2-5)heterocycloalkyl, C(2-5)heterocycloalkyl-C(1-4)alkyl, C(6-10)aryl, C(6-10)aryl-C(1-4)alkyl, C(1-9)heteroaryl or C(1-9)heteroaryl-C(1-4)alkyl, all groups are optionally substituted with one or more halogen, amino, hydroxyl, cyano, C(1-3)alkoxy, C(1-3)alkoxycarbonyl, (di)C(1-3)alkylamino or C(1-3)alkyl; or R13 and R14 are condensed and form ring containing 5–7 atoms by combining R13, which is C(1-6) alkyl or C(2-6) alkenyl, with an independent substituent within the definition of R14, all groups are optionally substituted with one or more halogen, amino, hydroxy, cyano, C(1-3)alkoxy, C(1-3)alkoxycarbonyl, (di)C(1-3)alkylamino or C(1-3)alkyl.
(formula I)
EFFECT: disclosed are RORγ modulators.
18 cl, 168 ex
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