BENZOTHIAZOLE CYCLOBUTYL AMINE DERIVATIVES AS LIGANDS OF HISTAMINE H-RECEPTORS, PHARMACEUTICAL COMPOSITION BASED THEREON, METHOD FOR SELECTIVE MODULATION OF EFFECTS OF HISTAMINE H-RECEPTORS AND METHOD OF TREATING CONDITION OR DISORDER MODULATED BY HISTAMINE H-RECEPTORS Russian patent published in 2013 - IPC C07D417/04 C07D417/08 C07D417/12 C07D417/14 C07D277/62 C07D487/04 A61K31/428 A61K31/435 A61K31/495 A61K31/5375 A61P3/00 A61P11/00 A61P25/00 A61K51/04 

FIELD: chemistry.

SUBSTANCE: invention relates to compounds of formula (I), stereoisomers, trans- and cis-isomers, racemates or pharmaceutically acceptable salts thereof, having modulating activity on histamine H₃-receptors. In formula (I) m equals 0; one of R₁ and R₂ is selected from a group which includes hydrogen, C_1-10alkoxycarbonyl, amido-, carboxy-, C_3-8cycloalkyl, halogen, -NR_AR_B, (NR_AR_B)carbonyl, or a group of formula -L₂-R₆; the other of R₁ and R₂ is selected from a group which includes hydrogen, halogen; each of R_3a and R_3b is independently selected from a group which includes hydrogen; each of R₄ and R₅ is independently selected from a group which includes C_1-10alkyl and C_1-10hydroxyalkyl; or R₄ and R₅, taken together with a nitrogen atom to which each is bonded, form a heteroaromatic ring of the type (a) or (b), where Q₁ is O or C; Q₂ is -N(R₂₀)-; R₂₀ is selected from a group which includes hydrogen and C_1-10alkoxycarbonyl; each of p1 and p2 is independently equal to 1, 2 or 3; each of q1, q2, q3, q4 and q5 are independently equal to 0, 1 or 2; and wherein each carbon atom in the ring is substituted with hydrogen or 0, 1 or 2 substitutes, independently selected from a group which includes hydrogen, hydroxy group, fluorine, C_1-10alkyl, C_1-10hydroxyalkyl and C_1-10fluoroalkyl; R₆ is a phenyl, heterocycle or heterocycloC_1-4alkyl, wherein the heterocycle is a 4-6-member aromatic or non-aromatic ring which contains 1 or 2 heteroatoms independently selected from N, O and S, optionally condensed with a benzene ring, wherein the phenyl or heterocycle can be unsubstituted or optionally substituted with one or more substitutes independently selected from a group which includes C_1-4alkoxy, C_1-4alkyl, cyano, halogen and oxo-; L is a bond or C_1-4alkylene; L₂ is a bond, C_1-4alkylene, -C(=O)-, -SO₂N(R_14a)-, -N(R_14a)SO₂-, -C(O)N(R_14a)-, -N(R_l4a)C(O)- or -N(R₁₅)-; R₁₀ is selected from a group which includes hydrogen; R_14a is selected from a group which includes hydrogen; R₁₅ is selected from a group which includes hydrogen; and R_A and R_B are independently selected from a group which includes hydrogen, C_1-10alkyl, C_1-10acyl, C_1-4halogenalkyl, C_1-10alkoxycarbonyl, C_3-8cycloalkyl and C_3-8cycloalkylcarbonyl. The invention also relates to a pharmaceutical composition which contains compounds of formula (I), a method for selective modulation of effects of histamine H₃-receptors, use of said compounds in producing a medicament for treating a condition or disorder modulated by histamine H₃-receptors, as well as specific compounds of formula (I).

EFFECT: improved properties of compounds.

18 cl, 2 tbl, 154 ex