DERIVATIVES OF 1,2,5-THIADIAZOLE, INTERMEDIATE COMPOUNDS, METHODS OF SYNTHESIS AND PHARMACEUTICAL COMPOSITION Russian patent published in 2000 - IPC

FIELD: organic chemistry, pharmacy. SUBSTANCE: invention describes the novel derivatives of 1,2,5-thiadiazole or its quaternized form taken among compounds of the general formula (I) where W means oxygen or sulfur atom; R is taken among the group consisting of hydrogen, halogen atom, R⁴,-OR⁴,-SR⁴,-SO₂R⁴ and -Z-C_4-12-(cycloalkylalkyl); R⁴ is taken among the group consisting of C_1-15-alkyl, C_2-15-alkenyl and C_2-15-alkynyl each of that is substituted optionally with one or more substituents taken independently among the group consisting of halogen atom, -CF₃, phenyl and phenoxy-group where phenyl and phenoxy-group are substituted optionally with one or more substituents taken independently among the group consisting of halogen atom, -CN, C_1-4-alkyl, C_1-4-alkoxy-group, -OF₃,-CF₃ or R is taken among the group consisting of -OR⁵Y,-SR⁵Y,OR⁵-Z-Y,-SR⁵ZY,-O-R⁵-Z-R⁴ where Z means oxygen or sulfur atom; R⁵ means C_1-15-alkyl; Y means 5- or 6-membered heterocyclic group taken among thienyl, pyridyl and thiazolidonyl; G is taken among azacyclic or azabicyclic ring system or G means optionally substituted C₃-C₈-cycloalkyl where cycloalkyl substituents are taken among R¹ and R² or optionally substituted C_1-6-alkyl where substituent is NR⁵R⁷; R⁶ and R⁷ both mean hydrogen atom or C_1-6-alkyl; one of R¹ and R¹ means hydrogen atom and another means hydrogen atom or C_1-6-alkyl; R³ means hydrogen atom or C_1-5-alkyl; m = 0, 1 or 2; p = 0, 1 or 2; q = 1 or 2; r = 0, 1 or 2; means a single or double bond under condition that if W means oxygen atom and G means alkyl then R is taken among the group consisting of hydrogen atom, R⁴,-OR⁴,-SR⁴,-SO₂R⁴,-Z-C_4-12-(cycloalkylalkyl) each of that is optionally substituted with one or more substituents taken independently among the group consisting of halogen atom and -CF₃; or R is taken among the group consisting of OR⁵Y,-SR⁵Y,OR⁵-Z-Y,-SR⁵ZY,-O-R⁵-Z-R⁴ where Z means oxygen or sulfur atom; R⁵ means C_1-5-alkyl. Invention relates to also its pharmaceutically acceptable salt or solvate. Invention relates to therapeutic active azacyclic or azabicyclic compounds, method of their synthesis and pharmaceutical compositions including indicated compounds. New compounds are useful for treatment of patients with diseases of central nervous system caused by dysfunction of muscarine cholinergic system. EFFECT: new compounds indicated above, improved methods of synthesis, valuable pharmacological properties. 24 cl, 5 tbl