Amino and alkylaminoalkenoate ester derivatives of aminochloroni

Details Amino and alkylaminoalkenoate ester derivatives of aminochloroni Amino and alkylaminoalkenoate ester derivatives of aminochloroni

1982-07-19

1984-03-06

Daus, Donald G.

Drug, bio-affecting and body treating compositions

Antigen, epitope, or other immunospecific immunoeffector

Bacterium or component thereof or substance produced by said...

544409, C07D24116, C07D24120, A01K 31495

Patent

active

044354002

ABSTRACT:
The present invention relates to aminoalkenoate ester derivatives of 2-amino-5-chloro-3-nitropyrazine useful as sensitizers of hypoxic tumor cells to therapeutic radiation. It also relates to the process of preparing such compounds by reaction of 2-amino-5,6-dichloro-3-nitro-pyrazine with an amino or alkylamino substituted .alpha.,.beta.-unsaturated alkenoate ester. In addition the application relates to pharmaceutical compositions containing such compounds and to methods of treatment comprising administering such compounds to patients undergoing radiation treatment to enhance the effectiveness of such treatment by sensitizing hypoxic tumor cells to therapeutic radiation.

REFERENCES:
patent: 3660397 (1972-05-01), Jones et al.
Cragoe, et al.; "N-Amidino-3 amino-5 Substituted-6 Halopyrazine Carboxamides," J. Med. Chem:10, pp. 66-75, 1967.
Chin et al., "Screening . . . Radiosensitizers," Chem. Abst., 89:20966z.
Anderson, R. F. et al., "Radiosensitization . . . by Nitropyridium Compounds," Br. J. Cancer, 37, Suppl. III, pp. 103-106 (1978).
Rauth et al., "In Vitro Testing . . . Radiosensitizers," Chem. Abst. 85:40894f (1976).
Denekamp et al., "Hypoxic Cells Radiosensitizers," Chem. Abst. 82:93112w.
Ainsworth et al., Can. J. Biochem., 10156, pp. 457-461 (1978).
Adams et al., Lancet, pp. 186-188, Jan. (1976).
Olive, P. L., Cancer Res., 39, pp. 4512-4515, Nov. (1979).

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