NEW TETRAHYDROPYRIMIDINE CONNECTION OR ITS SALT Russian patent published in 2017 - IPC C07D471/04 A61K31/519 A61K31/553 A61P35/00 A61P5/28 A61P13/08 

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-C_1-3an 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-C_1-6alkyl group, hydroxy-C_3-7cycloalkyl group,C_1-6an alkoxy group which may be substituted by Ra, C_3-7 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-C_1-3alkoxycarbonylamino group, halogen-C_1-3alkylcarbonylamino group, a (5-7)membered monocyclic heterocycloalkanecarbonyl group,containing a nitrogen atom in the ring, and substituted with hydroxy-C_1-6alkyl group, or - (CH₂)_n-C(=O)-NHRf; R² is a hydrogen atom, a halogen atom or a halogen-C_1-3an alkyl group; Ra is C_1-6alkylpyrazolyl group, a triazolyl group, a tetrazolyl group or a C_1-6 alkylsulfonylpiperazinyl group; Rf is halogen-C_1-3alkyl group, hydroxy-C_1-6alkyl group, hydroxy-C_3-7cycloalkyl group, hydroxy-C_3-7cycloalkyl-C_1-6alkyl group C_1-6alkyl group, substituted by Rfa; Rfa is C a _1-6alkylpyrazolyl group, halogen-C_1-3alkylthiazolyl group, an oxadiazolyl group or a halogen-C_1-3alkyloxadiazolyl group; and n is an integer from 0 to 3.

EFFECT: obtaining of a new compound.

20 cl, 5 tbl, 63 ex