AGENTS CAUSING APOPTOSIS AND INTENDED FOR TREATING CANCER, IMMUNE AND AUTOIMMUNE DISEASES Russian patent published in 2016 - IPC C07D417/14 C07D471/04 A61K31/428 A61K31/4427 A61K31/4725 A61P35/00 

Abstract RU 2594282 C2

FIELD: chemistry.

SUBSTANCE: invention refers to heterocyclic compounds of formula (I) or to therapeutically acceptable salt thereof, where X represents benzo [d] thiazolyl, optionally substituted with one or two R4; Y1 represents a pirrolil, pyrazolyl, triazolyl or pyridinyl; where Y1 is optionally substituted with one or two substitutes independently selected from a group consisting of R5, CO(O)R5, CO(O)H and CN; L1 selected from group comprising (CR6R7)q, (CR6R7)s-O-(CR6R7)r, (CR6R7)s-C(O)-(CR6R7)r, (CR6R7)s-S(O)2-(CR6R7)r and (CR6R7)s-NR6A-(CR6R7)r; and Y2 is selected from a group consisting of C3-4 alkyl with branched chain, C5-7 cycloalkyl, C6-7 cycloalkyl, phenyl, piperidinyl, morpholinyl and tetrahydropiranyl; where the phenyl is optionally condensed with benzene; where Y2 optionally substituted with one, two or three substitutes independently selected from a group consisting of R8, OR8, SO2R8, CO(O)R8, NHR8, N(R8)2, C(O)H, OH, CN, NO2, F, Cl, Br and I; or L1 represents a bond; and Y2 is selected from a group consisting of C5 cycloalkyl, phenyl, tetrahydropiranyl and piperidinyl; where C5 cycloalkyl and tetrahydropiranyl presented by Y2 are optionally condensed with benzene; Z1 is selected from group consisting of or ; R1, R2 and R3 are absent; R4, in each case is independently selected from group consisting of OR12 and halogen; R5, in each case is independently selected from group consisting of C1-6 alkyl, C1-6 hydroxyalkyl, phenyl and cyclopropyl; R6A represents C1-6 alkyl; each R6 and7, in each case are independently selected from group consisting of hydrogen, R15 and CO(O)R15; R8, in each case is independently selected from group consisting of C1-6 alkyl, C2-6 alkynyl, phenyl, piperidinyl and morpholinyl; where R8 C1-6 alkyl and C2-6 alkynyl are optionally substituted with one, two or three substitutes independently selected from a group consisting of R16, OR16, SO2R16, C(O)R16, NHR16, N(R16)2, OH and F; where R8 phenyl is optionally substituted with one Cl; Rk, in each case represents C1-6 alkyl; R12 is C1-4 alkyl; R15, in each case is independently selected from a group consisting of C1-4 alkyl and phenyl; where R15 C1-4 alkyl is optionally substituted with one substitute selected from a group consisting of C1-4 alkoxy, morpholinyl and C6cycloalkyl; R16, in each case is independently selected from a group consisting of C1-4 alkyl, C1-4 hydroxyalkyl, phenyl, tetrahydropiranyl, morpholinyl, 1,4-dioxanyl, dioxydotiomorfolinyl and pyridinyl; q equals to 1, 2 or 3; s, r, m, n and p equals to 0; or where the compound is selected from a group specified in item 1. Invention also relates to pharmaceutical composition based on the above compounds and method of cancer treating.

EFFECT: technical result allows obtaining new heterocyclic compounds effective in cancer treating.

9 cl, 3 tbl, 188 ex

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RU 2 594 282 C2

Authors

Van Le

Douerti Dzhordzh

Van Silu

Tao Chzhi-Fu

Branko Milan

Kanzer Aaron R.

Uendt Majkl D.

Sun Syaokhun

Frej Robin

Khansen Todd M.

Sallivan Dzherard M.

Dzhadd Endryu

Sauers Endryu

Dates

2016-08-10Published

2012-10-11Filed