Anti-arthritic pyrazolo-triazine derivatives

Details Anti-arthritic pyrazolo-triazine derivatives Anti-arthritic pyrazolo-triazine derivatives

1987-05-14

1988-08-30

Ford, John M.

Organic compounds -- part of the class 532-570 series

Organic compounds

Heterocyclic carbon compounds containing a hetero ring...

544212, 544220, 540548, C07D41714, C07D51314, C07D48704

Patent

active

047678585

ABSTRACT:
The invention features compounds having anti-arthritic activity and having the formula ##STR1## wherein X is an alkyl group having between 1 and 8, inclusive, carbon atoms and Y is a hydroxyalkylamino group having between 2 and 8, inclusive, carbon atoms; a dialkylamino group having between 2 and 12, inclusive, carbon atoms; a carboxyalkylamino group having between 2 and 9, inclusive, carbon atoms; a heterocycloalkyl group having between 2 and 5, inclusive, carbon atoms and having nitrogen as a hetero atom; an alkylthioalkylamino group having between 3 and 10, inclusive, carbon atoms; or a heteroarylalkylthioalkylamino group having between 5 and 14, inclusive, carbon atoms and having nitrogen as a hetero atom.
The invention further features compounds having similar activity and having the formula ##STR2## wherein A is H, an alkyl group having between 1 and 8, inclusive, carbon atoms, an aralkyl group having between 6 and 14, inclusive, carbon atoms, an aryl group having between 5 and 14, inclusive, carbon atoms, or a heteroaryl group having between 3 and 12, inclusive, carbon atoms and having nitrogen as a hetero atom; and B is H, benzyl, a carboalkoxy group having between 2 and 8, inclusive, carbon atoms, an alkyl group having between 1 and 8, inclusive, carbon atoms, or an alkyl group having between 3 and 8, inclusive, carbon atoms.
The invention additionally features compounds having similar activity and having the formula ##STR3## wherein r is an integer between 2 and 4, inclusive.

REFERENCES:
patent: 3865824 (1975-02-01), Kobe et al.
Senga et al., J. Med. Chem., 1982, vol. 25, pp. 243-249.
Senga et al., J. Het. Chem., 1975, vol. 12, No. 1, pp. 893-898.
Capuano et al., Chemische Berichte, "Darstellung von Pyrazolo-, Triazolo-, Oxazolo- und Thiazolo- S-Triazinen mit Bruckenkopf-Stickstoff Sowie Eines N-Athoxycarbonyl-Isopurins", 104:3039-3047 (1971).
Kobe et al., J. Heterocyclic Chemistry, "The Synthesis and Chemical Reactions of Certain Pyrazolo [1,5-a]-1,3,5-Triazines (1)", 11:199-204 (1974).
Durant et al., J. Medicinal Chemistry, "Cyanoguanidine-Thiourea Equivalence in the Development of the Histamine H.sub.2 -Receptor Antagonist, Cimetidine", 20:901-906, (1977).

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