| 摘要 |
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, -OR1', 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 |
