TRIAZOLOPYRIDINES AS PHOSPHODIESTERASE INHIBITORS FOR TREATING SKIN DISEASES Russian patent published in 2015 - IPC C07D471/04 A61K31/437 A61P17/00 

FIELD: medicine, pharmaceutics.

SUBSTANCE: present invention refers to compounds of general formula I, their pharmaceutically acceptable salts or N-oxides. In general formula , R₁ represents C_1-6alkoxy, such as methoxy or hydroxy; R₂ represents C_3-5cycloalkyl, which is optionally substituted by one substitute specified in R₄, wherein R₄ means C_1-4alkyl, which is optionally substituted by hydroxy, C_1-4alkoxy, group -OC(O)NR₅R₆, wherein each of R₅ and R₆ independently represents a hydrogen atom, C_1-4alkyl, C_3-6cycloalkyl, or R₅ and R₆ together with a nitrogen atom where they are attached to, form pyrrolidinyl, group -NHC(O)R₇, wherein R₇ means C_1-4alkyl, C_3-5cycloalkyloxy or pyrrolidinyl, or benzyloxygroup; -C(O)NR₇R₈, wherein each of R₇ and R₈ independently represents a hydrogen atom or C_1-4alkyl, which in turn can be substituted by hydroxy, oxo, cyano, group -SO₂C_1-4alkyl, group -SO₂NR₁₁R₁₂, wherein each of R₁₁ and R₁₂ independently represents a hydrogen atom or C_1-4alkyl, group -NHSO₂C_1-4alkyl, group -NHC(O)C_1-4alkyl, group -C(O)NR₇R₈, wherein R₇ and R₈ together with a nitrogen atom, where they are attached to, form morpholinyl, -OC(O)C_2-6alkenyl, phenyl, pyridinyl or C_3-6cycloalkyl, or R₇ and R₈ together with a nitrogen atom where they are attached to, form 5-6-merous cycle specified in morpholinyl, piperidinyl, piperazinyl substituted by C_1-4alkyl, or pyrrolidinyl; -COOR₇, wherein R₇ means a hydrogen atom or C_1-4alkyl; A represents phenyl optionally one or two-substituted by cyano, halogen, hydroxyl, C_1-4alkyl, halogenC_1-4alkyl, C_1-4alkoxy, halogenC_1-4alkoxy, C_1-4alkoxyC_1-4alkoxy, -SO₂C_1-4alkyl, group -C(O)OR₃, wherein R₃ means a hydrogen atom or C_1-4alkyl, -C(O)R₃, wherein R₃ means C_1-4alkyl, amino, C_1-4alkylamino or diC_1-4alkylamino, -NR₅R₆, wherein R₅ and R₆ independently mean hydrogen, -C(O)C_1-4alkyl or -SO₂C_1-4alkyl, -C_1-4alkylNR₅R₆, wherein R₅ and R₆ independently mean hydrogen or -SO₂C_1-4alkyl, or -C_1-4alkylC(O)OR₃, wherein R₃ means C_1-4alkyl, -SO₂NR₁₁R₁₂, wherein R₁₁ and R₁₂ independently mean a hydrogen atom or C_1-4alkyl substituted by hydroxy, or R₁₁ and R₁₂ together with a nitrogen atom where they are attached to, form morpholinyl; pyrrolidinyl optionally substituted by cyano; pyrimidinyl; thiophenyl optionally substituted by C_1-4acyl; piperidinyl; 4,5-dihydro-2H-pyridazinone substituted by C_1-4alkyl; dihydrobenzofuranone; oxoindanyl; or dihydro-oxoindolyl; X and Y represent either C and N, or N and C, respectively.

EFFECT: there are prepared new compounds, which possess the inhibitory activity on PDE4.

6 cl, 53 ex