Xanthines and their therapeutic use

Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Heterocyclic carbon compounds containing a hetero ring...

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514263, 514265, 544118, 544267, 544268, 544269, 544270, 544271, 544272, 544273, A61K 31522, A61K 315377, C07D47304, C07D47306

Patent

active

061242888

ABSTRACT:
The subject invention concerns a compound of the formula (i): ##STR1## in which Q represents heteroaryl or heterocyclo optionally substituted with one or more substituents selected from the group consisting of C.sub.1-6 alkyl (optionally substituted with one or more halogens), C.sub.1-6 alkyl--S(O)n-- (where n is 0, 1 or 2), --CO.sub.2 H (or C.sub.1-6 alkyl esters thereof or C.sub.1-6 alkyl amides thereof), halogen, C.sub.1-6 alkoxy, CN, NO.sub.2 and NR.sub.7 R.sub.8;
R.sub.1 -R.sub.5, which may be the same or different, each represent C.sub.1-6 alkyl (optionally substituted with one or more halogens), C.sub.1-6 alkyl--S(O)n-- (where n is 0, 1 or 2), --CO.sub.2 H (or C.sub.1-16 alkyl esters thereof or C.sub.1-6 alkyl amides thereof), halogen, C.sub.1-6 alkoxy, CN, NO.sub.2, NR.sub.7 R.sub.8 or H (provided R.sub.1 -R.sub.6 are not all H simultaneously);
R.sub.6 represents H, C.sub.1-6 alkyl, --CO.sub.2 H (or C.sub.1-6 alkyl esters thereof or C.sub.1-6 alkyl amides thereof), --CN, C.sub.1-6 alkyl optionally substituted by --CO.sub.2 H (or C.sub.1-6 alkyl esters thereof or C.sub.1-6 alkyl amides thereof), C.sub.1-6 alkoxy or --CN; and
R.sup.7 and R.sub.8, which may be the same or different, each represent H, C.sub.1-6 alkyl, C.sub.1-6 Alkylcarbonyl, C.sub.1-6 alkoxycarbonyl, arylsulphonyl, heteroarylsulphonyl, heterocyclosulphonyl, arylcarbonyl, heteroarylcarbonyl, heterocyclocarbonyl or C.sub.1-6 alkylsulphonyl, or R.sub.7, R.sub.8 and the nitrogen to which they are attached form a 5 or 6 membered heterocyclic ring;
and pharmaceutically-acceptable salts thereof.

REFERENCES:
patent: 5223504 (1993-06-01), Noverola
patent: 5821366 (1998-10-01), Montana
Jacob, J. Autoimmunity 5, Supp. A, 133, 1992.
Jacob, C.O. (1992) Studies on the Role of Tumor Necrosis Factor in Murine and Human Autoimmunity. Journal of Autoimmunity 5(Supl. A): 133-143.
Ram, V.J., H.K. Pandey, A.J. Vlietinck (1982) Purine Analogues As Potential Chemotherapeutic Agents. III. J. Heterocyclic Chem. 19: 153-155.
Merlos, M. et al. (1990) Structure-activity relationships in a series of xanthine derivatives with antibronchoconstrictory and bronchodilatory activities. Eur. J. Med. Chem. 25:653-658.

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