FIELD: pharmacology.
SUBSTANCE: invention relates to a new tetrahydropyridopyrimidine compound of the general formula (I) or a pharmaceutically acceptable salt thereof. The compounds possess an inhibitory activity against the androgen receptor (AR) and can be used to treat a tumour associated with activity (AR). In the general formula
,
X is a halogen atom or halogen-C1-3an alkyl group; R is a phenyl group which is substituted by R1 and can also be substituted by R2, or a 5- or 6-membered heteroaryl group which contains 1 to 3 heteroatoms selected from a nitrogen, oxygen or sulfur atom and which is substituted by R1 and can also be substituted by R2; R1 represents a hydrogen atom, a phenyl group, a hydroxy-C1-6alkyl group, hydroxy-C3-7cycloalkyl group,C1-6an alkoxy group which may be substituted by Ra, C3-7 a cycloalkylaminosulfonyl group, a (6-7) membered monocyclic heterocycloalkylsulfonyl group, with two nitrogen atoms or a nitrogen atom and an oxygen atom in the ring; halogen-C1-3alkoxycarbonylamino group, halogen-C1-3alkylcarbonylamino group, a (5-7)membered monocyclic heterocycloalkanecarbonyl group,containing a nitrogen atom in the ring, and substituted with hydroxy-C1-6alkyl group, or - (CH2)n-C(=O)-NHRf; R2 is a hydrogen atom, a halogen atom or a halogen-C1-3an alkyl group; Ra is C1-6alkylpyrazolyl group, a triazolyl group, a tetrazolyl group or a C1-6 alkylsulfonylpiperazinyl group; Rf is halogen-C1-3alkyl group, hydroxy-C1-6alkyl group, hydroxy-C3-7cycloalkyl group, hydroxy-C3-7cycloalkyl-C1-6alkyl group C1-6alkyl group, substituted by Rfa; Rfa is C a 1-6alkylpyrazolyl group, halogen-C1-3alkylthiazolyl group, an oxadiazolyl group or a halogen-C1-3alkyloxadiazolyl group; and n is an integer from 0 to 3.
EFFECT: obtaining of a new compound.
20 cl, 5 tbl, 63 ex
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Authors
Dates
2017-11-22—Published
2015-05-28—Filed