DERIVATIVES OF 3-AMINOMETHYLQUINOLONE-2 AS INHIBITORS OF NO-SYNTHETASE AND METHOD FOR THEIR PREPARING, BIOLOGICALLY ACTIVE COMPOUNDS AND PHARMACEUTICAL COMPOSITION BASED ON THEREOF Russian patent published in 2006 - IPC C07D215/227 C07D401/12 C07D413/12 C07D405/12 A61K31/4704 A61K31/4709 A61K31/4741 A61P9/00 A61P1/00 A61P25/00 

FIELD: organic chemistry, biochemistry, medicine, pharmacy.

SUBSTANCE: invention relates to new derivatives of 3-aminomethylquinolone-2 of the general formula (1)

(2)

or (3) wherein R₁ means hydrogen atom (H) or Alk; R₂ is taken among Alk; -OAlk, -SCH₃, -Hal, -CF₃, 3,4-OCH₂CH₂O-, 3,4-OCH₂O-, 4-OCF₃, 2-Ph, -OPh, -NHCOR, 2-OCH₃, 5-Ph, 4-Obzk, 3-NO₂, 2-CH₃, 5-iPr, di-OAlk, di-Hal; or R₂ represents halogen atom and alkyl group, or halogen atom and alkoxy-group taken simultaneously and independently of one another; or R₂ represents the group -CONR₄R₅ wherein each R₄ and R₅ means independently of one another the group Alk, or they form the group -(CH₂)_n- wherein n = 2-6. R means -CH₃; R₃ means hydrogen atom (H); X is taken among hydrogen atom (H), 6-(C₁-C₃)-Alk, 6-iPr, 6-iBu; 7-(C₁-C₂)-Alk, 8-(C₁-C₂)-Alk, 6-(C₁-C₂)-OAlk, 6-OCF_3, 7-(C₁-C₂)-Alk, 7-SCH₃, 6,7-OCH₂O-, 6,7-OCH₂CH₂O-, 5,6,7-OCH₃, 6-F; X and Y are similar or different and taken among 7,8-CH₃, 6,8-CH₃, 5,8-CH₃, 5,7-CH₃, 6,7-CH₃, 6,7-OCH₃, 6-CH₃, 7-Cl. Also, invention relates to a method for preparing indicated compounds and to pharmaceutical composition inhibiting activity of NO-synthetase based on these compounds. Invention provides preparing new compounds and pharmaceutical composition based on thereof for aims preparing medicinal agents for treatment 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.

19 cl, 1 tbl, 95 ex