FIVE-MEMBERED HETEROCYCLIC PYRIDINE COMPOUNDS AND PREPARATION METHOD AND USE THEREOF Russian patent published in 2018 - IPC C07D471/04 C07D487/04 C07D495/04 C07D519/00 A61K31/437 A61K31/444 A61K31/4545 A61K31/496 A61K31/5025 A61K31/519 A61K31/5377 A61K31/635 A61P35/00 A61P35/04 

Abstract RU 2668074 C2

FIELD: chemistry.

SUBSTANCE: invention relates to the field of organic chemistry, namely a heterocyclic compound of formula (X) and a pharmaceutically acceptable salt thereof, where X, Y and Z, each separately constitute N or C and at least two of them - X, Y or Z – are represent N, and when X represents N, Z represents N; represents a simple or a double bond; W and V are selected from H or unsubstituted C1-C4 alkyl; R1 represents a substituted with 1-2 substituents or unsubstituted mono- or bicyclic C6-C10 aryl; substituted with 1 or 2 substituents or unsubstituted mono- or bicyclic 5-9 membered heteroaryl containing 2-3 heteroatoms selected from N, O and S; wherein the substituent is halogen, nitro, cyano, hydroxyl; unsubstituted or trihaloid substituted C1-C6 alkyl, C1-C6 alkoxy, C1-C6 alkylcarbonyl, -NRaRb, -OC(O)-Rf, unsubstituted phenyl or phenyl substituted with 1-3 R3, or unsubstituted monocyclic 5-6 membered heteroaryl, containing 1 to 2 heteroatoms selected from N and S, or a 5-6 membered heteroaryl containing 1 to 2 heteroatoms, selected from N, substituted by 1 R4; R2 represents C1-C4 alkoxycarbonyl; -NRcRd; substituted with 1-3 substituents or unsubstituted mono- or bicyclic C6-C10 aryl; substituted with 1 substituent or unsubstituted mono- or bicyclic 5-10 membered heteroaryl containing 1 to 2 heteroatoms selected from N, O and S; or substituted by 1 substituent or unsubstituted monocyclic partially unsaturated 6-membered heterocyclyl containing 1 heteroatom selected from N; wherein the substituent is halogen, C2 alkylenedioxy, unsubstituted or trihaloid- or NRcRd-substituted C1-C6 alkyl either C3-C6 cycloalkyl, C1-C6 alkoxy, C1-C6 sulfamide, -NRaRb, -C(O)R', morpholinyl or unsubstituted or substituted R" piperidinyl, wherein R3 is a halogen, cyano, C1-C2 alkylenedioxy, unsubstituted or trihaloid- or morpholinyl substituted C1-C6 alkyl, C1-C6 alkoxy, -NRaRb, -C(O)R' or morpholinyl; R4 represents halogen, unsubstituted C1-C6 alkyl either unsubstituted or C1-C6 alkoxycarbonyl substituted piperidinyl; R' represents C1-C6 alkyl, C1-C6 alkoxy, -NRaRb, C1-C6 alkyl substituted 6-membered heterocyclyl containing 2 nitrogen atoms; R" represents C1-C6 alkyl, C3-C6 cycloalkyl, C1-C6 alkylcarbonyl, C1-C6 alkoxycarbonyl, C3-C6 cycloalkylcarbonyl or substituted benzoyl, wherein the substituent is selected from trihaloid substituted C1 alkyl; Ra and Rb are presents H, C1-C6 alkyl or C1-C6 alkylcarbonyl; Rc and Rd are presents H or C1-C6 alkyl or Rc and Rd, together with the N atom to which they are attached, form a 6-membered heterocyclyl containing one oxygen atom; Rf is C1-C6 alkyl or unsubstituted 5-membered heteroaryl containing one oxygen atom. Invention also relates to the use of a compound of formula (X), a drug on its basis and a method of treatment.

.

EFFECT: technical result: new heterocyclic compounds useful for the treatment of diseases associated with abnormal cell proliferation are obtained.

12 cl, 2 dwg, 5 tbl, 145 ex

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RU 2 668 074 C2

Authors

Shen Tszinkan

Gen Mejyuj

Din Tszyan

Syu Bin

Aj Tszin

Ma Yujchi

Van Syu

Pen Sya

Chen Yuelej

Chen Dantsi

Men Tao

Ma Lanpin

Tszi Inchun

Dates

2018-09-26Published

2014-06-18Filed