FIELD: pharmaceuticals.
SUBSTANCE: invention relates to a novel compound or a pharmaceutically acceptable salt of Formula (A) having the properties of an NAE inhibitor (Neddβ activating enzyme). In the Formula (A)
is a single or double bond; X is -O- or -CH=; Y is -NH- or -O-; R1 is a hydrogen atom or a hydroxy group; R2 is a hydrogen atom or a hydroxy group; R3 is an ethynylene group or a 5-membered monocyclic heteroarylene group containing one to two heteroatoms selected from the group consisting of N, S and O; R4 is a bond, a methylene group or a C3-C7 cycloalkylidene group; R5 is a C3-C7 saturated cycloalkyl group, a C6-C10 unsaturated cycloalkyl group selected from phenyl, naphthyl, indanyl, which may contain one or more groups R6, or a 5-6 membered monocyclic or 9-10 membered bicyclic unsaturated heterocycloalkyl group, which contains one to three heteroatoms selected from the group consisting of N, S and O, and which may contain one or more groups R6; R6 is a halogen atom, a hydroxy group, a cyano group, a C1-C6 alkyl group, which may contain one phenoxy group as substituents, a carbamoyl group, a C1-C6 alkoxycarbonyl group, a 6-membered monocyclic or bicyclic unsaturated heterocycloalkyl group containing one heteroatom N, 4-6 membered monocyclic or 8-membered bicyclic saturated heterocycloalkyl group, which contains one to four heteroatoms selected from the group consisting of N, S and O, and which may contain one or more groups, or a halogen atom, a hydroxy group, a carboxyl group or a C1-C6 alkyl group as substituents, an amino group, a mono- or di-(C1-C4alkyl)amino group which may have one hydroxy group or a phenyl group as substituents, C1-C6 alkoxy group which may contain one or more groups selected from a halogen atom, C3-C7 saturated cycloalkyl group, or a 5-membered monocyclic unsaturated heterocycloalkyl group, containing one to three heteroatoms of N, a benzyloxy group which may contain one or more carbamoyl groups as substituents, a C1-C6alkylthio group, a C1-C6alkylsulfonyl group or an aminosulfonyl group when there are two or more groups R6, R6 of this set may be the same or different.
EFFECT: compounds can be used as antitumor agents.
9 cl, 3 dwg, 21 tbl, 143 ex
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Authors
Dates
2018-06-19—Published
2015-06-24—Filed