N-Substituted imidazolecarboxamide derivatives

Details N-Substituted imidazolecarboxamide derivatives N-Substituted imidazolecarboxamide derivatives

1977-11-07

1979-02-20

Rotman, Alan L.

Drug, bio-affecting and body treating compositions

Antigen, epitope, or other immunospecific immunoeffector

Parasitic organism or component thereof or substance...

548301, 548337, A61K 31415, C07D23364

Patent

active

041407881

ABSTRACT:
N-Substituted imidazolecarboxamide compounds represented by the formula; ##STR1## wherein R.sub.1 is hydrogen atom, lower alkyl, lower alkenyl, aralkyl, R.sub.2 is hydrogen atom, lower alkyl, lower alkenyl, aralkyl, 1-adamantyl, R.sub.3 is hydrogen atom, lower alkyl, aralkyl; with the proviso that one of R.sub.1, R.sub.2 or R.sub.3 is not hydrogen when the other two are hydrogen, are produced by reacting aminomalonamide derivative with orthoformate derivative in high yields. The compounds (I) exhibit anti-tumor activity against experimental tumors such as Sarcoma 180 in mice.

REFERENCES:
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Noller Chemistry of Organic Compounds end ed., pp. 244-245, Philadelphia, Saunders, 1957.
Schipper et al., Jour. Amer. Chem. Soc. 1952, vol. 74, pp. 350-353.
Sakaguchi et al., Jour. of Antibiotics 1975, vol. 28, pp. 798-803.
Tsujino et al., Proceedings of the First Intersectional Congress of IAMS 1974, vol. 3, pp. 441-443.
Saito Oyo-yakuri 1970, vol. 4, pp. 521-524.
Cunningham et al. Immunology 1968, vol. 14, pp. 599-600 & the page facing p. 600.
Miller et al., Jour. Amer. Chem. Soc. 1952, vol. 74, pp. 2892-2893.
Sakaguchi et al., Cancer Research 1975, vol. 35, pp. 1643-1648.
Sakaguchi et al., Proceedings of the First Intersectional Congress of IAMS 1974, vol. 3, pp. 539-541.

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