RU2007105735A - ACTIVE SUBSTANCES, PHARMACEUTICAL COMPOSITION, METHOD FOR PRODUCING AND APPLICATION - Google Patents

Claims (11)

1. The use as active substances of pharmaceutical compositions having activity against influenza viruses, substituted esters of 4-aminomethyl-5-hydroxy-1H-indole-3-carboxylic acids of the general formula 1, or their racemates, or their optical isomers, or their pharmaceutically acceptable salts and / or hydrates:

where R ¹ represents an amino group substituent selected from optionally substituted C _1-6 alkyl, optionally substituted aryl, optionally substituted heterocyclyl; R ₁ ⁴ and R ₂ ⁴ independently represent an amino group substituent selected from hydrogen, optionally substituted C _1-6 alkyl, C _3-8 optionally substituted cycloalkyl, R ₁ ⁴ and R ₂ ⁴ together with the nitrogen atom to which they are attached form an optionally substituted azaheterocyclyl or guanidyl; R ² represents an “alkyl” substituent selected from hydrogen, an optionally substituted mercapto group, an optionally substituted amino group, an optionally substituted hydroxyl, R ³ represents lower alkyl; R ⁵ represents a cyclic system substituent selected from hydrogen, halogen, cyano, optionally substituted aryl or optionally substituted heterocyclyl, excluding compounds in which: R ¹ represents hydrogen, alkyl or cycloalkyl; R ₁ ⁴ and R ₂ ⁴ independently represent an amino substituent selected from hydrogen, optionally substituted alkyl, optionally substituted cycloalkyl, or R ₁ ⁴ and R ₂ ⁴ together with the nitrogen atom to which they are attached mean azaheterocyclyl or guanidyl ; R ³ is optionally substituted lower alkyl; but R ² represents hydrogen, or a substituted mercapto group, or a substituted amino group, or a substituted hydroxyl; R ⁵ - represents bromine, or R ² represents a substituted mercapto group or a substituted amino group, R ⁵ represents hydrogen, or R ² - represents hydrogen or a substituted mercapto group, R ⁵ means fluorine. 2. The use according to claim 1 of ethyl esters of 4-aminomethyl-6-aryl (or heterocyclyl) -5-hydroxy-1H-indole-3-carboxylic acids of the general formula 1.1, or their racemates, or their optical isomers, or their pharmaceutically acceptable salts and / or hydrates:

where R ¹ , R ² , R ₁ ⁴ and R ₂ ⁴ have the above meanings; Ar is aryl or a 5-6 membered heterocyclyl comprising at least one heteroatom selected from N, O or S. 3. The use according to claim 1 of ethyl esters of 4-aminomethyl-6-aryl (or pyridyl) -5-hydroxy-1-methylindole-3-carboxylic acids of the general formula 1.2, or their racemates, or their optical isomers, or their pharmaceutically acceptable salts and / or hydrates:

where R ² , R ₁ ⁴ and R ₂ ⁴ have the above meanings; Ar ₁ represents aryl or pyridyl. 4. The use according to claim 1 of ethyl esters of 6-aryl (or pyridyl) -2,4-bis (aminomethyl) -5-hydroxy-1-methylindole-3-carboxylic acids of the general formula 1.3, or their racemates, or their optical isomers , or their pharmaceutically acceptable salts and / or hydrates:

where R ₁ ⁴ , R ₂ ⁴ and Ar ₁ have the above meanings; R ₃ ⁴ and R ₄ ⁴ independently represent an amino substituent selected from hydrogen, optionally substituted alkyl, optionally substituted cycloalkyl, optionally substituted aryl, or optionally substituted heterocyclyl, or R ₃ ⁴ and R ₄ ⁴ together with a nitrogen atom, with which they are linked, form optionally substituted azaheterocyclyl or guanidyl via R ₃ ⁴ and R ₄ ⁴ . 5. The use according to claim 1 of ethyl esters of 6-aryl (or pyridyl) -2,4-bis (aminomethyl) -5-hydroxy-1-methylindole-3-carboxylic acids of the general formula 1.4, or their racemates, or their optical isomers , or their pharmaceutically acceptable salts and / or hydrates:

where R ₁ ⁴ , R ₂ ⁴ and Ar ₁ have the above meanings. 6. The use according to claim 1 of ethyl esters of 6-aryl (or pyridyl) -2,4-bis (dimethylaminomethyl) -5-hydroxy-1-methylindole-3-carboxylic acids of the general formula 1.5, or their racemates, or their optical isomers , or their pharmaceutically acceptable salts and / or hydrates:

where Ar ₁ has the above meaning. 7. The use according to claim 1 of ethyl esters of 2,4-bis (dimethylaminomethyl) -5-hydroxy-1-methyl-6- (3-pyridinyl) -indole-3-carboxylic acid of the formula 1.5 (1), 2-dimethylaminomethyl- 5-hydroxy-1-methyl-6- (3-pyridinyl) -4- (1-pyrrolylmethyl) -indole-3-carboxylic acid of the formula 1.5 (2), 2-dimethylaminomethyl-5-hydroxy-4- (1-imidazolylmethyl ) -1-methyl-6- (3-pyridinyl) -indole-3-carboxylic acid of the formula 1.5 (3), 2-dimethylaminomethyl-5-hydroxy-4-guanidinylmethyl-1-methyl-6- (3-pyridinyl) - indole-3-carboxylic acid of the formula 1.5 (4), 4-dimethylaminomethyl-5-hydroxy-1-methyl-6- (3-pyridinyl) -2- (1-pyrrolylmethyl) -indole-3-carboxylic acid of formula 1.5 (5) or their racemates, or their optical isomers or pharmaceutically acceptable salts and / or hydrates thereof:

8. A pharmaceutical composition having activity against influenza viruses, containing as an active substance, at least one compound according to any one of claims 1 to 7 in an effective amount. 9. A method of obtaining a pharmaceutical composition according to claim 8 by mixing the active substance with an inert excipient and / or solvent, characterized in that at least one compound according to any one of claims 1 to 7 is used as the active substance in an effective amount. 10. A medicine in the form of tablets, capsules or injections in a pharmaceutically acceptable package for the prevention and treatment of diseases caused by influenza viruses, based on the pharmaceutical composition of claim 8. 11. A method for the prevention and treatment of diseases caused by influenza viruses by administering to a patient a medicament according to claim 10.