N-SUBSTITUTED DERIVATIVES OF (3R, 4R)-3-ETHYL-4-[(1-METHYL-1H-IMIDAZOL-5-YL) METHYL]-2-PYROLIDONE OR THEIR PHARMACEUTICALLY ACCEPTABLE ACID ADDITION SALTS HAVING ANTIGLAUKOMIC ACTIVITY Russian patent published in 1994 - IPC

FIELD: medicine. SUBSTANCE: the products: N-substituted derivatives of (3R, 4R)-3-ethyl-4-[(1-methyl-1H-imidazol-5-yl)methyl]-2-pyrrolidone of the formula 1 reported in the specification wherein R is R-(C₁-C₂₀)-alkyl, optionally substituted for a trimethylsilyl group, hydroxy, acetoxy or an isopropoxycarbonyl group, norbornyl, (C₁-C₄)-alkylbenzyl or 3,4-dimethoxybenzyl group or their pharmaceutically acceptable acid addition salts having antiglaucomic activity. Reagent 1: (3R,4R)-3-methyl-4-[(1-methyl-1H-imidazol-5-yl)methyl] -2-pyrrolidone. Reagent 2: an acylating agent: halogen or cyanoformate of the formula: XCO₂R or an anhydride of the formula: n¹O₂COCO₂n wherein R is as defined above; X is halogen or a cyano group; R¹ is a hydrocarbon group, or p-nitrophenylcarbonate of the formula: O₂N=(C₆-H₄)-COOR wherein R is as defined above. EFFECT: improved properties of the N-substituted derivatives. 6 dwg, 1 tbl