CETP INHIBITORS Russian patent published in 2014 - IPC C07D263/22 C07D413/10 C07D413/04 C07D417/10 C07D417/14 A61K31/421 A61K31/422 A61K31/427 A61P9/00 

FIELD: chemistry.

SUBSTANCE: invention relates to compound of formula I, or its pharmaceutically acceptable salt where: X stands for -O-; Z stands for -C(=O)-; Y stands for -(CRR¹)-, where R¹ is selected from -C₁-C₂alkyl; R stands for H or -C₁-C₅alkyl; R⁵ stands for H; R² and B each is selected from A¹ and A², where one of R² and B stands for A¹, and the other from R² and B stands for A²; where A¹ has structure (a); A² is selected from the group, which includes phenyl, pyridyl, pyrazolyl, thienyl, 1,2,4-triazolyl and imodazolyl; A³ is selected from the group including phenyl, thiazolyl and pyrazolyl; A⁴ is selected from the group, including phenyl, pyridyl, thiazolyl, pyrazolyl, 1,2,4-triazolyl, pyrimidinyl, piperidinyl, pyrrolidinyl and asetidinyl; A² is optionally substituted with 1-3 substituents, independently selected from halogen atom, -OCH₃ and -OCF₃ and -C₁-C₃alkyl, optionally substituted with 1-3 halogen atoms; A³ is substituted with one A⁴ group and is optionally substituted with 1-2 substituents, independently selected from halogen atom, -OH, -OCH₃, -OCF₃ and -C₁-C₃alkyl, optionally substituted with 1-3 halogen atoms; A⁴ is optionally substituted with 1-3 substituents, independently selected from the group, which includes: (a) -C₁-C₅alkyl, optionally substituted with 1-3 halogen atoms and optionally substituted with group -OH, (b) -C₂-C₄alkenyl, optionally substituted with 1-3 halogen atoms, (c) -C(=O)C₁-C₂alkyl, optionally substituted with 1-3 halogen atoms and optionally substituted with one group selected from -OH, -CO₂CH₃, -C(=O)CH₃, -NR³R⁴ and -OC₁-C₂alkyleneOC₁-C₂alkyl, (d) -C(=O)H, (e) -CO₂H, (f) -CO₂C₁-C₄alkyl, optionally substituted with one group, selected from -C(=O)C₁-C₂alkyl, -OH, -CO₂CH₃, -CO₂H, -NR³R⁴ and -OC₁-C₂alkyleneOC₁-C₂alkyl, (g) -OH, (h) -S(O)_xC₁-C₂alkyl, (i) halogen atom, (j) -CN, (k) -NO₂, (l) -C(=O)NR³R⁴, (m) -OC₁-C₂alkyleneOC₁-C₂alkyl, (n) -OC₁-C₃alkyl, optionally substituted with 1-3 halogen atoms, (o) -C(=O)OC₁-C₂alkyl, optionally substituted with 1-3 halogen atoms and optionally substituted with one group, selected from -OH, -CO₂CH₃, -NR³R⁴ and -OC₁-C₂alkyleneOC₁-C₂alkyl, (q) -NR³R⁴ and (r) -S(O)_xNR³R⁴, on condition that A⁴ stands for heterocyclic group, attached to A³ by means of ring carbon atom in A⁴, at least, one substituent in A⁴ must be selected from R^e, where R^e is selected from the group including: (a) -C₁-C₅alkyl, substituted with -OH group and optionally substituted with 1-3 halogen atoms, (b) -C₂-C₄alkenyl, optionally substituted with 1-3 halogen atoms, (c) -C(=O)C₁-C₂alkyl, optionally substituted with 1-3 halogen atoms and optionally substituted with one group selected from -OH, -CO₂CH₃, -C(=O)CH₃, -NR³R⁴ and -OC₁-C₂alkyleneOC₁-C₂alkyl, (d) -C(=O)H, (e) -CO₂H, (f) -CO₂C₁-C₄alkyl, optionally substituted with one group, selected from -C(=O)C₁-C₂alkyl, -OH, -CO₂CH₃, -CO₂H, -NR³R⁴ and -OC₁-C₂alkyleneOC₁-C₂alkyl, (g) -OH, (h) -S(O)_xC₁-C₂alkyl, (i) -CN, (j) -NO₂, (k) -C(=O)NR³R⁴, (l) -OC₁-C₂alkyleneOC₁-C₂alkyl, (m) -C(=O)C₁-C₂alkyl, optionally substituted with 1-3 halogen atoms and optionally substituted with one group, selected from -OH, -CO₂CH₃, -NR³R⁴ and -OC₁-C₂alkyleneOC₁-C₂alkyl, (n) -NR³R⁴(=O)OC₁-C₂alkyl, (o) -NR³R⁴ and (p) -S(O)_xNR³R⁴; p equals 0, 1 or 2; and R^a is selected from halogen atom, -CH₃, -CF₃, -OCH₃ and -OCF₃; R³ and R⁴ each is independently selected from H and CH₃; and x equals 0, 1 or 2.

EFFECT: formula (I) compound is applied for medication, which possesses properties of CETP inhibitor, for increase of HDL-C and for reduction of LDL-C Technical result is compounds, inhibiting cholesterol ether transferring protein (CETP).

10 cl, 140 ex