Derivatives of indole, having antiviral activity

 

The invention relates to new indole derivative of the formula Iin which R1is hydrogen, (NISS. )alkyl, (NISS. )alkylsulfonyl, optionally substituted aryl, optionally substituted aryl(NISS. )alkyl, C3-C6cycloalkyl(NISS. )alkyl, morpholinyl(NISS. )alkyl, sulfamoyl, optionally substituted lower alkyl, carbarnoyl, optionally substituted lower alkyl or phenyl, lower alkylsulfonyl, morpholinylcarbonyl, thienyl(NISS. )alkyl, optionally substituted lower alkoxycarbonyl or carboxyla, pyridyl(NISS. )alkyl, optionally substituted phenylsulfonyl, thienylmethyl, phenylcarbinol, lower alkoxycarbonyl; R2is hydrogen, optionally substituted phenyl, optionally substituted phenyl(NISS. )alkyl, phenylcarbamoyl, lower alkyl, optionally substituted phenylsulfonyl, optionally substituted phenylsulfinyl, morpholino(NISS. )alkyl despite the fact that each of these substituted phenyl groups may carry substituents selected from halogen, trialsandrea lower alkyl, lower alkoxyl, azido, nitro, amino, phenyl, lower alkoxycarbonyl, amino (substituted lower alkyl or lower alkylcarboxylic), Renny (NISS. )alkyl, hydroxy, (NISS. )alkoxy, nitro, phenylsulfonyl, phenyl(NISS. )alkoxy, carboxy, NISS. alkoxycarbonyl, optionally substituted by phenyl; X is hydroxy, amino, optionally substituted lower alkyl or lower alkoxy(NISS. )alkyl; Y is - COOR (where R is hydrogen, lower alkyl, optionally substituted phenyl), tetrazolyl, optionally substituted Triticum, imidazolyl, triazolyl, thiazolyl, pyrazolyl, phenyl, optionally substituted by carboxypropyl, lower alkoxyl or hydroxy-group; provided that excluded the compounds in which each of R1- R6is hydrogen, R4is hydroxy, and Y is SOOS2H5their tautomers, pharmaceutically acceptable salts or hydrates, which have the integrase inhibitory activity, which allows their use in pharmaceutical compositions against HIV infection. 3 S. and 13 C. p. F.-ly, 16 PL.

Description text in facsimile form (see graphic part)

Claims

1. Derivatives of indole of the formula

in which R1means hydrogen, (ness.)alkyl, (ness.)alkylsulfonyl, optionally substituted aryl, optionally substituted aryl(ness.)Ala is PWM-alkyl, carbarnoyl, optionally substituted lower alkyl or phenyl, lower alkylsulfonyl, morpholinylcarbonyl, thienyl(ness.)alkyl, optionally substituted lower alkoxycarbonyl or carboxyla, pyridyl(ness.)alkyl, optionally substituted phenylsulfonyl, thienylmethyl, phenylcarbinol, lower alkoxycarbonyl;

R2means hydrogen, optionally substituted phenyl, optionally substituted phenyl(ness.)alkyl, phenylcarbamoyl, lower alkyl, optionally substituted phenylsulfonyl, optionally substituted phenylsulfinyl, morpholino(ness.) alkyl, despite the fact that each of these substituted phenyl groups may carry substituents selected from halogen, trialsandrea lower alkyl, lower alkoxyl, azido, nitro, amino, phenyl, lower alkoxycarbonyl, amino (substituted lower alkyl or lower alkylcarboxylic), aryl(ness.)of alkyl, NISS.of alkyl, carboxyl;

R3, R4, R5and R6each independently mean hydrogen, halogen, trigosamine (ness.)alkyl, hydroxy, (ness.)alkoxy, nitro, phenylsulfonyl, phenyl(ness.)alkoxy, carboxy, NISS.alkoxycarbonyl, optionally substituted by phenyl;

X is hydroxy, amino, optional replacement is optionally substituted by phenyl), tetrazolyl, optionally substituted Triticum, imidazolyl, triazolyl, thiazolyl, pyrazolyl, phenyl, optionally substituted by carboxypropyl, lower alkoxyl or hydroxy-group;

provided that excluded the compounds in which each of R1, R2, R3, R5and R6means hydrogen, R4means hydroxy, and Y means SOOS2H5,

their tautomers, pharmaceutically acceptable salts or hydrates.

2. Connection on p. 1, where R1and R2at the same time does not mean hydrogen when Y is a COOR (where R has the above value).

3. Connection on p. 1, where R1and R2at the same time does not mean hydrogen, when X represents hydroxy and Y represents COOR (where R has the above value).

4. The compound according to any one of paragraphs.1-3, where R1means hydrogen or optionally substituted phenylsulfonyl.

5. The compound according to any one of paragraphs.1-3, where R2means hydrogen, optionally substituted phenyl or optionally substituted phenyl(ness.)alkyl.

6. The compound according to any one of paragraphs.1-3, where each of R1, R2, R3and R5and R6independently from each other represents a hydrogen or halogen.

7. Connection on p. 6, where X is a hydroxy-group.

9. Connection on p. 1, where Y means triazolyl, tetrazolyl, optionally substituted Triticum, imidazolyl, thiazolyl or pyrazolyl.

10. The compound according to any one of paragraphs.1-3, where R1means hydrogen or optionally substituted phenylsulfonyl, R2means hydrogen, optionally substituted phenyl or optionally substituted phenyl(ness.)alkyl, R3, R4, R5and R6each independently of one another denotes hydrogen or halogen, and X is a hydroxy-group.

11. The compound according to any one of paragraphs.1-3, where R1means hydrogen or optionally substituted phenylsulfonyl, R2means hydrogen, optionally substituted phenyl or optionally substituted phenyl(ness.)alkyl, R3, R4, R5and R6each independently of one another denotes hydrogen or halogen, X is hydroxy and Y means tetrazolyl, thiazolyl or imidazolyl.

12. The compound according to any one of paragraphs.1-3, where R1means hydrogen or optionally substituted phenylsulfonyl, R2means hydrogen, optionally substituted phenyl or optionally substituted phenyl(ness.)alkyl, the radicals R3, R4, R5and R6each independently mean hydrogen or halogen, X is gidrol, R2means hydrogen, optionally substituted phenyl(ness.)alkyl, the radicals R3, R4, R5and R6each independently mean hydrogen or halogen, X is a hydroxy-group, and Y denotes tetrazolyl, optionally substituted Triticum, imidazolyl, triazolyl, thiazolyl or pyrazolyl.

14. Connection on p. 13, where R1means hydrogen or phenylsulfonyl, optionally substituted with halogen, R2means hydrogen, optionally substituted by halogen phenyl or phenylmethyl, optionally substituted with halogen, R4denotes halogen, the radicals R3, R5and R6all at the same time signify hydrogen, X signifies a hydroxy-group, a Y indicates tetrazolyl.

15. Pharmaceutical composition containing as active ingredient a derivative of indole according to any one of paragraphs.1-14 and intended for inhibiting integrase.

16. Pharmaceutical composition containing as active ingredient a derivative of indole according to any one of paragraphs.1-14 acting against HIV infection.

 

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