SUBSTITUTED 3-PYRIDYLMETHYLAMINES AND FOCUSED LIBRARY Russian patent published in 2004 - IPC

FIELD: organic chemistry, medicine, pharmacology. SUBSTANCE: invention relates to new substituted 3-pyridylmethyl- amines of the general formula (1) or (2) given below as separate stereoisomers, their racemates, bases or salts of pharmacologically acceptable acid HX eliciting high activity with respect to nicotine receptors. Invention relates also to the focused library comprising new 3- -substituted pyridines of the general formula (1) or (2) wherein R¹ represents CN, -C(O)R⁵, -CH₂R⁶; R² represents hydrogen atom or inert substituent; R³ represents hydrogen atom or inert substituent; or R² and R³ in common represent groups -CH₂CH₂CH₂- or CH₂CH₂CH₂CH₂; R⁴ represents hydrogen atom, inert substituent, NH-protective substituent, electrophilic substituent, nucleophilic substituent, -COCR⁷R⁸NR⁹R¹⁰; R⁵ represents hydrogen atom, -OH, -OR^1′, NR¹²R¹³; R⁶ represents chlorine, bromine or iodine atom, -OH, ; each among R⁷, R⁸, R⁹, R¹⁰, R¹¹, R¹², R¹³ represents independently: hydrogen atom, inert substituent; or R¹⁰ represents NH-protective substituent, electrophilic substituent, nucleophilic substituent, -C(O)CR⁷R⁸NR⁹R¹⁰; or R⁷ and R⁸ represent amino acid residue under condition that each among R⁷, R¹², R¹³ represents independently: hydrogen atom, inert substituent and R¹⁰ represents hydrogen atom, inert substituent, NH-protective substituent, electrophilic substituent, nucleophilic substituent; or CR⁷R⁸ in common represent 1,1-cycloalkylene; or NR⁹R¹⁰ in common and NR¹²R¹³ in common represent independently azaheterocyclyl or substituted azaheterocyclyl; or R¹² represents hydrogen atom, inert substituent and R¹³ represents NH-protective substituent, electrophilic substituent, nucleophilic substituent; HX represents pharmacologically acceptable acid (hydrochloric, acetic, maleic, fumaric and so on acid). EFFECT: valuable medicinal and pharmacological properties of compounds. 14 cl, 1 tbl, 7 ex