FIELD: organic chemistry, medicine, ophthalmology, pharmacy.
SUBSTANCE: invention relates to novel derivatives of benzo[g]quinoline of the formula (I): as a free base or acid-additive salt used in treatment of glaucoma and myopia, and to a method for their synthesis and a pharmaceutical composition. In compound of the formula (I) each A and B means hydrogen atom (H); X means -CH2; Y means sulfur atom (S); R1 means H or (C1-C4)-alkyl wherein this compound can be in form of a free base or acid-additive salt. Method for synthesis of compound of the formula (I) by claim 1 or its salt involves the conversion step of alkoxy-group in compound of the formula (II):
wherein A, B, X, Y and R1 have values given in claim 1; R3 means (C1-C4)-alkyl to hydroxy-group, and conversion of synthesized compounds of the formula (I) to free base or its acid-additive salt.
EFFECT: improved method of synthesis, valuable medicinal properties of compounds and pharmaceutical composition.
7 cl, 1 ex
Authors
Dates
2007-06-10—Published
2002-07-08—Filed