HETEROCYCLE-SUBSTITUTED PIPERAZINO-DIHYDROTHIENOPYRIMIDINES Russian patent published in 2013 - IPC C07D495/04 C07D519/00 A61K31/519 A61P1/00 A61P11/00 A61P25/00 

FIELD: chemistry.

SUBSTANCE: invention relates to dihydrothienopyrimidinesulphoxides of formula 1, and pharmaceutically acceptable salts thereof , where X denotes SO, R¹ denotes H, R² denotes H or a residue selected from C₁-C₁₀alkyl, which is optionally substituted with one or more residues selected from OR^2.1, where R^2.1 denotes H or C₁-C₆alkyl, R^2.2 and R^2.3 independently denote H or C₁-C₆alkyl, where Het is a 6-member monocyclic, saturated heterocycle containing 1 heteroatom selected from N or O, and where the hetaryl is a 5-11-member mono- or bicyclic, optionally anellated heteroaryl containing 1, 2 or 3 heteroatoms independently selected from N, S or O, and where the cycloalkyl can be saturated, or R² denotes a monocyclic C₃-cycloalkyl, which is optionally substituted with a residue selected from a branched or linear C₁-C₆alkanol, C₁-C₃alkylene-OR^2.1, or R² denotes phenyl which is optionally substituted with a halogen, or R² denotes a residue selected from Het and hetaryl, each optionally substituted with one or more residues selected from halogen, OH, oxo group and OR^2.1, C₁-C₆alkyl, and where R³ denotes a bicyclic 9-11-member unsaturated or partially saturated heterocycle which is optionally substituted with one or more residues selected from a group comprising F, O, Br, CF₃, CN, OH, methyl, ethyl, propyl, isopropyl, -O-methyl, -O-ethyl, phenyl, NR^2.2R^2.3, where the phenyl is optionally substituted with F, Cl or Br. The invention also relates to pharmaceutical compositions based on said compounds, having phosphodiesterase 4 (PDE4) inhibiting activity.

EFFECT: obtaining novel compounds and pharmaceutical compositions based thereon, which can be used in medicine to treat respiratory or gastrointestinal complaints or diseases, inflammatory diseases of joints, skin or eyes, diseases of the peripheral or central nervous system or cancers.

20 cl, 1 tbl, 156 ex