HETEROCYCLIC JANUS KINASE 3 INHIBITORS Russian patent published in 2011 - IPC C07D471/04 C07D471/14 C07D451/04 A61K31/437 A61P11/06 A61P37/06 A61P17/00 A61P25/28 A61P35/00 

FIELD: chemistry.

SUBSTANCE: invention relates to a compound of formula (I), in which X denotes N or CR³, M denotes (CH₂)_m; m equals 0 or 1, R¹ denotes H or lower alkyl which can be substituted with a group selected from a group consisting of mono- or di-lower alkylamino and -O-lower alkyl, R² denotes H or lower alkyl, R³ denotes H or lower alkyl substituted with a group selected from a group consisting of halogen, mono- or di-lower alkylamino and cyclic amino, R⁴¹ denotes H or pyridine which can be substituted with a cyano group, R⁴² denotes a bridged polycyclic hydrocarbon or a bridged azacyclic hydrocarbon, each of which can be substituted, R⁵ denotes a group selected from a group consisting of halogen, cyano, lower alkyl-carbonyl, lower alkyl-oxycarbonyl, hydroxycarbonyl, formyl, amidinooxycarbonyl, guanidinooxycarbonyl, guanidino, carbamoyl, -C(=O)-5- or -6-member heterocycloalkyl, -C(=O)-5- or -6-member heteroaryl, lower alkyl, lower alkenyl, -O-lower alkyl, 5- or 6-member heterocycloalkyl and 5-member heteroaryl, each of which can be substituted, provided that when R⁵ denotes a 5-member heteroaryl, X denotes -CR³; or R⁴¹ and R¹⁵ can be bonded through a defined functional group to form divalent groups shown below: (I-A) (I-B) or (I-C), in which R^A denotes H or acyl, which can be substituted, provided that the term "substituted" with respect to R⁴ and/or R⁵ denotes substitution with one or more substitutes selected from a group comprising the following substitutes: (a). halogen; (b) -OH, -O-R², -O-phenyl, -OCO-R^Z-OCONH-R^Z oxo (=O); (c) -SH, -S-R², -S-phenyl, -S-heteroaryl, -SO-R², -SO-phenyl, -SO-heteroaryl, -SO₃H, -SO₂-R^Z, -SO₂-phenyl, - SO₂-heteroaryl, sulphamoyl, which can be substituted with one or two R^Z groups; (d) amino, which can be substituted with one or two R^Z groups, -NHCO-R^Z, -NHCO-phenyl, -NHCO₂-R^Z, -NHCONH₂, -NHCONH-R^Z, -NHSO₂-R⁰, -NHSO₂-phenyl, -NHSO₂NH₂, -NO₂, =N-O-R^Z; (e) -CHO, -CO-R^Z, -CO₂H, -CO₂-R^Z, carbamoyl, which can be substituted with one or two R^Z groups, -CO-cyclic amino, -COCO-R^Z, cyano; (f) R^Z; (g) phenyl, which can be substituted with one or more groups selected from substitutes described above in paragraphs from (a) to (f), a 5- or 6-member heterocycloalkyl, a 5- or 6-member heteroaryl, a 5- or 6-member heterocycloaryl; or pharmaceutically acceptable salts thereof. The invention also relates to a method of producing compounds of formula II, a pharmaceutical composition based on said compounds which is a Janus kinase 3 inhibitor, a method of treating and/or preventing different immunopathological diseases, including autoimmune diseases, inflammatory diseases and allergic diseases.

EFFECT: novel compounds are obtained and described, which can be used as an active ingredient of an agent for treating or preventing diseases caused by undesirable cytokine signal transmission or diseases caused by pathological cytokine signal transmission.

14 cl, 579 ex, 72 tbl