QUINAZOLINE EFFECTIVE AS ION CHANNEL MODULATORS Russian patent published in 2012 - IPC C07D239/94 C07D401/04 C07D401/12 C07D403/04 C07D403/12 C07D403/14 C07D405/14 C07D405/04 C07D405/12 A61K31/517 A61P25/00 A61P29/00 A61P23/00 A61P19/00 

FIELD: medicine, pharmaceutics.

SUBSTANCE: present invention refers to new compounds of formula I or their pharmaceutically acceptable salts exhibiting the properties of voltage-dependent sodium channel inhibitors, such as NaV1.8. The latter play a central role in generating the action potentials in all excitable cells such as neurons and myocytes, and can be used for treating such diseases as epilepsy, irritable bowel syndrome, chronic pain, etc. In the compounds of formula I: R¹ and R² together with nitrogen atom a substituted ring selected from: (A),(B),(C),(D) or (E), which are specified in the patent claim, where in the ring (A): each of m₁ and n₁ is independently equal to 0-3, provided m₁+n₁ is equal to 3-4; z₁ is equal to 0-4; Sp¹ represents -O-, -S-, -NR'- or C₁-C₄alkylidene linker in which one methylene ring is optionally or independently substituted by -O-, provided Sp¹ is bound with carbonyl group through an atom different from carbon; the ring B¹ represents a 5-6-members saturated or aromatic, monocyclic or heterocyclic ring containing 1-4 heteroatoms selected from O or N with the ring B¹ is optionally substituted by w₁ independent variants -R¹¹ with w₁ being equal to 0-1; where in the ring (B): G₂ represents CH; each of m₂ and n₂ is independently equal to 0-3, provided m₂+n₂ is equal to 2-4; p₂ is equal to 0-2; q₂ is equal to 0 or 1; z₂ is equal to 0-4; Sp² represents a bond or C₁-C₆alkylidene linker in which up to two methylene links are optionally or independently substituted by -O-. The other radical values are specified in the patent claim.

EFFECT: making new compounds of formula I or to their pharmaceutically acceptable salts showing the properties of voltage-dependent sodium channel inhibitors.

67 cl, 4 tbl, 503 ex