FIELD: pharmaceuticals.
SUBSTANCE: invention relates to a compound of formula (Ia) or a pharmaceutically acceptable salt thereof, wherein the XY group is -NHSO2 - or -SO2NH-; R1 is H; R2 is selected from COOH and a tetrazolyl group; R3 is selected from H, Cl and C1-C6-alkyl; R4 is selected from H, Cl and F; R5 is selected from H, C1-C6-alkyl, C≡CH, C1-C6-haloalkyl, SO2-C1-C6-alkyl, Cl, C1-C6-alkoxy, OH, C1-C6-hydroxyalkyl, C1-C6-alkylthio, pyrazolyl, C3-C7-cycloalkyl, C3-C7-heterocycloalkyl containing one heteroatom selected from oxygen, and C1-C6-haloalkoxy; R6 is H; R7 is selected from H, CN, C1-C6-haloalkyl, Cl, F, SO2-C1-C6-alkyl, SO2NR13R14, 5–6-membered monocyclic heteroaryl, and C1-C6-alkyl, where the specified heteroaryl group is optionally substituted with one or more substituents selected from C1-C6-alkyl; R8 is selected from H, C1-C6-alkyl, C1-C6-haloalkyl and halogen; R9 is H, C1-C3-alkyl or halogen; R10 and R11 together with the nitrogen to which they are attached form an azepanyl group, where one carbon in said azepanyl group is replaced by a group selected from O; or R10 and R11 together with the nitrogen to which they are attached form an azetidinyl, pyrrolidinyl or piperidinyl group, wherein: (a) said azetidinyl, pyrrolidinyl or piperidinyl group is substituted with one or more groups selected from C1-C6-alkyl , CN, C3-C7-cycloalkyl, OH, C1-C6-alkoxy, halogen, C1-C6-haloalkyl and oxazolyl, where the specified oxazolyl group in turn is optionally additionally substituted with one group selected from C1-C6-alkyl, or (b) one carbon in said piperidinyl group is replaced by a group selected from CO; or R10 and R11 together with the nitrogen to which they are attached form an 8-membered bicyclic heterocycloalkyl group wherein one carbon in the bicyclic heterocycloalkyl ring is optionally replaced by a group selected from O and NH and said bicyclic heterocycloalkyl group is optionally substituted by one or more groups selected from C1-C6-alkyl and OH; or R10 and R11 together with the nitrogen to which they are attached form a 6–12-membered bicyclic group containing a spirocyclic carbon atom, where one carbon in the bicyclic group is replaced by a group selected from O and NH and said bicyclic group is optionally substituted one or more groups selected from C1-C6-alkyl; and each R13 and R14 is independently H. The invention also relates to a pharmaceutical composition having an ERAP1 modulating activity based on the said compound.
EFFECT: obtaining new compounds and a pharmaceutical composition based on them which can be used in medicine for the treatment of proliferative, immune, viral or inflammatory disorders.
58 cl, 3 dwg, 2 tbl, 338 ex
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