Sesquihydrate of naphthyridine derivative, and process for the p

Details Sesquihydrate of naphthyridine derivative, and process for the p Sesquihydrate of naphthyridine derivative, and process for the p

1982-02-04

1984-04-10

Lee, Mary C.

Drug, bio-affecting and body treating compositions

Antigen, epitope, or other immunospecific immunoeffector

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

544362, 544363, C07D48704, A61K 31495

Patent

active

044421010

ABSTRACT:
Novel 1-ethyl-6-fluoro-1,4-dihyono-4-oxo -7-(1-piperazinyl)-1,8-naphthyridine-3-carboxylic acid.sesquihydrate (ATT-2266.sesquihydrate). The aforesaid compound can be prepared by heating 1-ethyl-6-fluoro-1,4-dihydro-4-oxo -7-(1-piperazinyl)-1,8-naphthyridine-3-carboxylic acid at a temperature above about 60.degree. C. in the presence of water in an amount sufficient to form the sesquihydrate. This sesquihydrate is much more stable than the anhydrate and the trihydrate and is superior to the anhydrate in the rate of dissolution and transference into the body through the intestines. Thus, it is especially useful as a pharmaceutical compound.

REFERENCES:
patent: 3149104 (1964-09-01), Lesher et al.
patent: 3590036 (1971-06-01), Lesher et al.
patent: 3849421 (1974-11-01), Nakagome et al.
patent: 4017622 (1977-04-01), Minami et al.
patent: 4146719 (1979-03-01), Irikura
patent: 4352803 (1982-10-01), Matsumoto et al.
patent: 4359578 (1982-11-01), Matsumoto et al.
Yuasa, R. et al., Yakugaku Zasshi, 102 (5), 469-476, (1982) "Pharmaceutical Studies on Hydrates of Am-715, Physical Characteristics and Intestinal Absorption."

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