RU2000102889A - APPLICATION OF KOLKHINOL DERIVATIVES AS A MEANS DAMAGING VESSELS - Google Patents

Claims (12)

l. The use of colquinol derivatives to obtain compositions for the treatment of diseases affecting the process of vascular formation, where the colhinol derivative has the formula

where R ₁ , R ₂ , R ₃ and R ₆ independently represent H, optionally substituted alkyl, cycloalkyl, alkenyl, alkynyl, aralkyl, alkanoyl, PO ₃ H ₂ ;
X is carbonyl (CO), thiocarbonyl (CS), methylene (CH ₂ ) or CHR ₄ group;
R ₄ is OH, O-alkyl or NR ₈ R ₉ ;
R ₅ and R _{7 are} independently H, alkyl, halogen, hydroxy, alkoxy, nitro, or amino;
R ₈ is an H 2 O 2
R ₉ is H, alkyl or cycloalkyl;
and their pharmaceutically acceptable salts, solvates and hydrates. 2. The use according to claim 1, wherein at least one of R ₁ , R ₂ , R ₃ and R ₆ is PO ₃ H ₂ . 3. The use according to claim 2, where R ₆ is PO ₃ H ₂ . 4. The use according to any one of claims 1 to 3, where R ₁ , R ₂ and R ₃ are alkyl. 5. The use according to any one of claims _{1 to 4} , where R ₄ represents an acylamino group. 6. The use according to claim 1, wherein R ₆ is PO ₃ H, R ₁ , R ₂ and R ₃ is alkyl, and R ₄ represents an acylamino group. 7. Compounds of formula I in which at least one of R ₁ , R _2, R ₃ and R ₆ is PO ₃ H ₂ . 8. The compound according to claim 7, in which R ₆ is PO ₃ H ₂ . 9. The compound according to claim 8, in which R ₁ , R ₂ and R ₃ represent alkyl, R ₄ represents an acylamino group. 10. The compound according to claim 7 of the formula

where R ₁ , R ₂ and R ₃ independently represent H, optionally tiled alkyl, cycloalkyl, alkenyl, alkynyl, alkanoyl or PO ₃ H ₂ ;
R ₆ is PO ₃ H ₂ ;
R ₄ is H or NR ₈ R ₉ ;
R ₅ and R _{7 are} independently H, alkyl, halogen, alkoxy, nitro or amino;
R ₈ is a halogen free
and R ₉ is H, alkyl or cycloalkyl,
and its pharmaceutically acceptable salts, solvates and hydrates. 11. The compound of the formula

where R ₁ , R ₂ and R ₃ independently represent H, optionally substituted alkyl, cycloalkyl, alkenyl, alkynyl, alkanoyl or PO ₃ H ₂ ;
R ₆ is H, optionally substituted alkyl, cycloalkyl, alkenyl, alkynyl or PO ₃ H ₂ ;
R ₄ is H or NR ₈ R ₉ ;
R ₅ and R _{7 are} independently H, alkyl, halogen, nitro or amino;
R ₈ is an option for an ally
and R ₉ is H, alkyl or cycloalkyl, provided that when R ₁ , R ₂ and R _{3 are} all methyl groups and R ₄ is hydrogen, acetylamino, acetylmethylamino, amino, methylamino or dimethylamino, then R _{6 is} not hydrogen, stands, hydroxyethyl or acetoxyethyl,
and its pharmaceutically acceptable salts, solvates and hydrates. 12. The compound according to claim 11, in which R ₁ , R ₂ and R ₃ represent alkyl and R ₄ represents acylamino group.