ARYL-SUBSTITUTED CARBOXAMIDE DERIVATIVES AS CALCIUM OR SODIUM CHANNEL BLOCKERS Russian patent published in 2016 - IPC C07D213/65 C07D215/40 C07D241/18 C07D401/12 C07D401/14 C07D405/12 C07D405/14 C07D409/12 C07D413/12 C07D417/12 C07D471/04 A61K31/44 A61K31/443 A61K31/4433 A61K31/4436 A61K31/4439 A61K31/444 A61K31/4706 A61K31/4709 A61K31/4725 A61K31/497 A61K31/506 A61P1/18 A61P9/06 A61P13/10 A61P19/02 A61P25/04 A61P25/08 A61P25/14 A61P25/16 A61P25/18 A61P25/20 A61P25/22 A61P25/28 A61P29/00 A61P35/00 

FIELD: medicine, pharmaceutics.

SUBSTANCE: invention refers to aryl-substituted carboxamide derivatives of formula (I)

or their pharmaceutically acceptable salts, wherein in formula (I) R represents hydrogen; R¹ is independently specified in a group consisting of: (1) hydrogen, (2) halogen, (3) hydroxyl, (4) -O_n-C_1-6 alkyl, wherein alkyl is unsubstituted or substituted by one or more substitutes optionally specified in R⁷, (5) -O_n-heterocylic group specified in piperidinyl, pyrrolidinyl, tetrahydropyranyl, tetrahydrofuranyl and oxetanyl; n has the value of 0 or 1; when n has the value of 0, a chemical bond is present instead of O_n; p has the value of 1 or 2; when p is equal to two, R¹ can be identical or different from each other; R² represents C_1-6 alkyl, which is unsubstituted or substituted by one or more substitutes, independently specified in R⁷; or R² together with R¹ forms C₃-C₆ cycloalkyl; X represents 1,2-C₃ cycloalkylene; W, Y and Z are independently specified in nitrogen atom or carbon atom; at least one of W, Y and Z represents nitrogen, and simultaneously W, Y and Z are other than carbon; R³, R⁴, R⁵ and R⁶ are such as presented in the patent claim; Ar means aryl, which represents mono- or bi-carbocyclic or mono or bi-heterocyclic ring containing 0-3 heteroatoms specified in O, N and S, including phenyl, furyl, oxazolyl, thiazolyl, imidazolyl, pyridyl, piperidinyl, pyrimidinyl, isooxazolyl, triazolyl, tetrahydronaphthyl, benzofuranyl, benzothiophenyl, indolyl, benzoimidazolyl, quinolyl, isoquinolyl, quinoxalinyl, pyrazolo [1,5-a] pyridyl, thieno [3,2-b] pyrrolyl, wherein aryl is optionally substituted by 1-3 substitutes specified in the patent claim. Also the invention refers to compounds of formula (II)

and their aryl-substituted carboxamide derivatives specified in cl. 3 of the patent claim, a pharmaceutical composition, a method of treating and using.

EFFECT: aryl-substituted carboxamide derivatives exhibiting blocking activity on T-type calcium channels or voltage-dependent channels.

10 cl, 6 tbl, 464 ex