DERIVATIVES OF BENZO[G]QUINOLINE FOR TREATMENT OF GLAUCOMA AND MYOPIA, METHOD FOR THEIR PREPARING AND PHARMACEUTICAL COMPOSITION Russian patent published in 2007 - IPC C07D401/12 A61K31/505 A61P27/06 A61P27/10

Abstract RU 2300532 C2

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

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RU 2 300 532 C2

Authors

Markshtejn Rudol'F

Gull' Peter

Pombo-Vill'Jar Ehsteban

Dates

2007-06-10—Published

2002-07-08—Filed