DERIVATIVES OF PHENYL-3-AMINOMETHYLQUINOLONE-2 AS INHIBITORS OF NO-SYNTHASE, METHOD FOR THEIR PREPARING, BIOLOGICALLY ACTIVE COMPOUNDS AND PHARMACEUTICAL COMPOSITION BASED ON THEREOF Russian patent published in 2006 - IPC C07D401/12 C07D215/227 C07D413/12 C07D491/56 C07D405/12 A61K31/4704 A61K31/4709 A61K31/4741 A61P9/00 A61P15/00 A61P11/06 

FIELD: organic chemistry, biochemistry, medicine, pharmacy.

SUBSTANCE: invention relates to novel amino- and hydroxy-derivatives of phenyl-3-aminomethylquinolone-2 of the general formula (1):

wherein R1, R2, R3 and R4 are independently similar or different and R1 is chosen from hydrogen atom (H), Alk, OAlk; R2 is chosen from H, Alk, OAlk, -OCF₃; R3 is chosen from H, Alk, OAlk, -SCH₃; R4 is chosen from H. Alk, OAlk, or R2 and R3 are chosen from -(CH₂)₃, -OCH₂O-, -OCH₂CH₂O-; R5 means H or Alk; R6, R7 and R9 mean H; R8 is chosen independently from the following substitutes:

wherein n = 1, 2, 3; Het represents furan; R represents hydrogen atom or alkyl. In case of hydroxy-derivatives at least one among R6, R7, R8 or R9 is -OH and other represent H. Also, invention relates to methods for synthesis of these compounds and to a pharmaceutical composition based on these compounds inhibiting activity of NO-synthase. Invention provides preparing novel compounds and pharmaceutical compositions based on thereof in aims for treatment of diseases associated with hyperactivity of phagocytizing cells, for example, rheumatic arthritis, asthma and others.

EFFECT: improved preparing method, valuable medicinal and biochemical properties of compounds and pharmaceutical composition.

32 cl, 1 tbl, 132 ex