FIELD: pharmaceutics.
SUBSTANCE: invention relates to novel heterocyclic compound of formula (I), or to its enantiomer and diastereoisomer, and to its additive salt with pharmaceutically acceptable acid or base, where X and Y are a carbon atom or a nitrogen atom, and they can not simultaneously represent two carbon atoms or two nitrogen atoms; Het fragment of the group 
an optionally substituted, aromatic or nonaromatic 5-7-membered ring containing, in addition to nitrogen, 1 to 3 hetero atoms selected from O, S and N, wherein the nitrogen may be substituted with a group representing a hydrogen atom, (C1-C6)alkyl group or a group -C(O)-O-Alk; R1 and R2 – (C1-C6)alkyl group, or R1 and R2 with the nitrogen atom carrying them, form a 4- to 7-membered heterocycloalkyl which may contain, in addition to the nitrogen atom, another heteroatom selected from oxygen, SO2 and NR, where R is (C1-C6)alkyl group, (C1-C6)alkylsulfonyl group, (C1-C6)polyhaloalkyl group or a group -C(O)-O-Alk; R3 represents (C1-C6)alkyl group, (C2-C6)alkenyl group, (C2-C6)alkynyl group, a cycloalkyl group, (C3-C4)cycloalkyl-(C1-C6)an alkyl group or a heteroaryl group; R4 is an aryl, heteroaryl, cycloalkyl or (C1-C6)alkyl group; R5 represents a hydrogen atom; Ra, Rb, Rc and Rd independently of each other, are a hydrogen atom, a halogen atom, (C1-C6)alkyl group, (C1-C6)alkoxy group, a hydroxy group, (C1-C6)polyhaloalkyl group, or a trifluoromethoxy group, or substituents of one of the pairs (Ra,Rb), (Rb,Rc) or (Rc,Rd) together with the carbon atoms carrying them form a 5-7-membered ring which may contain 1 to 2 heteroatoms selected from oxygen, wherein one or more of the ring carbon atoms defined above can be deuterated; “aryl” means a phenyl, naphthyl, biphenyl or indenyl group; “heteroaryl” means any mono- or bicyclic 5-10-membered group having at least one aromatic moiety and containing from 1 to 2 heteroatoms, selected from O, S and N; “cycloalkyl” means any mono- or bicyclic, non-aromatic, carbocyclic 4-9-membered group; alkyl, aryl, heteroaryl, cycloalkyl and heterocycloalkyl groups thus defined can be substituted by 1-3 groups selected from (C1-C6)alkyl optionally substituted by hydroxy or methoxy, (C3-C6)spiro, (C1-C6)alkoxy, (C1-C6)alkyl-S-, hydroxy, oxo (or N-oxide, as appropriate), cyano, NR'R'', (C1-C6)polyhaloalkyl, trifluoromethoxy, or halogen, it is assumed that R' and R'' independently of each other are (C1-C6)an alkyl group; wherein the Het fragment of the group 
, as defined above, may be substituted by a group, selected from hydroxy. Invention also relates to process for preparation of the compound of formula (I), a pharmaceutical composition based on the compound of formula (I) and use of the compound of formula (I).
EFFECT: new heterocyclic compounds possessing inhibitory activity of Bcl-2 family proteins have been obtained.
38 cl, 3 tbl, 166 ex
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