SULPHONAMIDE COMPOUNDS POSSESSING TRPM8 ANTAGONIST ACTIVITY Russian patent published in 2015 - IPC C07D217/22 C07D215/38 C07D401/12 C07D405/12 C07D409/12 C07D413/12 C07D417/12 C07D471/04 A61K31/47 A61K31/4709 A61K31/4725 A61K31/4353 A61P29/00 

Abstract RU 2563030 C2

FIELD: medicine, pharmaceutics.

SUBSTANCE: invention refers to new sulphonamide compounds of the structure as follows or to its pharmaceutically acceptable salt, wherein a bicyclic aromatic heterocycle consisting of pyridine condensed with benzene; one of Y and Z is CR2d, 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, R1: (a) H; (b) C1-C6alkyl, which can be optionally substituted by 1-3 groups specified in halogen, oxo and hydroxy; (c) C3-C7cycloalkyl; (d) C1-C6alkoxy group; or (e) halogen; each of R2a, R2b, R2c and independently represents(a) H; (b) C1-C6 alkyl, which can be optionally substituted by 1-3 groups specified in C1-C6alkoxy group, halogen and hydroxy; (c) C3-C7cycloalkyl; (d) C1-C6alkoxy 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 R3a, R3b, R3c and R3d independently means (a) H; (b) C1-C6alkyl, which can be optionally substituted by 1-7 groups specified in C3-C7cycloalkyl (wherein cycloalkyl can be optionally substituted by 1 group specified in C1-C6alkyl and C1-C6halogenalkyl), C1-C6alkoxy group, C1-C6halogenoalkoxy, halogen and hydroxy; (c) C3-C7cycloalkyl; (d) C1-C6alkoxy group, which can be optionally substituted by 1-3 groups specified in C3-C7cycloalkyl, C1-C6alkoxy group and halogen; (e) C3-C7cycloalkoxy 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 R5 and R6: H, n means 0 or 1, X is (a) a carboxy group; (b) C1-C6alkoxycarbonyl; (c) hydroxy-C1-C6-alkyl, (d) aminocarbonyl, wherein a nitrogen atom can be optionally substituted by one group specified in C1-C6alkyl, C1-C6alkoxy group and nitrile; or (e) C2-C7alkanoyl. 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

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RU 2 563 030 C2

Authors

Tsudzuki Jasujuki

Savamoto Dajsukeh

Sakamoto Tosiaki

Kato Taku

Niva Jasuki

Avaj Nobumasa

Dates

2015-09-20Published

2012-03-15Filed