| 摘要 |
FIELD: medicine, pharmaceutics.SUBSTANCE: invention refers to new sulphonamide compounds of the structure as followsor to its pharmaceutically acceptable salt, wherein a bicyclic aromatic heterocycle consisting of pyridine condensed with benzene; one of Y and Z is CR, whereas the other one is a chemical bond; the ring B is (a) mono- or bicyclic aromatic hydrocarbon having 6-11 carbon atoms as circular atoms; (b) 5-11-merous mono- or bicyclic aromatic heterocycle containing carbon atoms and 1-4 heteroatoms specified in oxygen, sulphur and nitrogen atoms; or (c) 4-12-merous mono- or bicyclic non-aromatic heterocycle containing carbon atoms and 1-4 heteroatoms specified in oxygen, sulphur and nitrogen atoms; ring C: benzene, R: (a) H; (b) C-Calkyl, which can be optionally substituted by 1-3 groups specified in halogen, oxo and hydroxy; (c) C-Ccycloalkyl; (d) C-Calkoxy group; or (e) halogen; each of R, R, Rand independently represents(a) H; (b) C-Calkyl, which can be optionally substituted by 1-3 groups specified in C-Calkoxy group, halogen and hydroxy; (c) C-Ccycloalkyl; (d) C-Calkoxy group; (e) phenyl; (f) 6-merous monocyclic aromatic heterocyclic group containing carbon atoms and 1-4 heteroatoms specified in oxygen, sulphur and nitrogen atoms; (g) 5-merous monocyclic non-aromatic heterocyclic group containing carbon atoms and 1-4 heteroatoms specified in oxygen, sulphur and nitrogen atoms; or (h) halogen, each of R, R, Rand Rindependently means (a) H; (b) C-Calkyl, which can be optionally substituted by 1-7 groups specified in C-Ccycloalkyl (wherein cycloalkyl can be optionally substituted by 1 group specified in C-Calkyl and C-Chalogenalkyl), C-Calkoxy group, C-Chalogenoalkoxy, halogen and hydroxy; (c) C-Ccycloalkyl; (d) C-Calkoxy group, which can be optionally substituted by 1-3 groups specified in C-Ccycloalkyl, C-Calkoxy group and halogen; (e) C-Ccycloalkoxy group; (f) phenyl, which can be optionally substituted by 1 group specified in halogen; (g) 6-merous monocyclic aromatic heterocyclic group containing carbon atoms and 1-4 heteroatoms specified in oxygen, sulphur and nitrogen atoms; (h) phenoxy group; (j) halogen; or (k) hydroxy, each of Rand R: H, n means 0 or 1, X is (a) a carboxy group; (b) C-Calkoxycarbonyl; (c) hydroxy-C-C-alkyl, (d) aminocarbonyl, wherein a nitrogen atom can be optionally substituted by one group specified in C-Calkyl, C-Calkoxy group and nitrile; or (e) C-Calkanoyl. The invention also refers to a pharmaceutical composition based on the declared compound and to using the declared compound.EFFECT: produced are new sulphonamide compounds possessing TRPM8 antagonist activity.16 cl, 20 tbl, 242 ex |
