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Claims for Patent: 4,442,101

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Claims for Patent: 4,442,101

Title: Sesquihydrate of naphthyridine derivative, and process for the preparation thereof
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.
Inventor(s): Ichihashi; Hitoshi (Kyoto, JP), Tanaka; Terukazu (Osaka, JP), Imasato; Yu (Toyonaka, JP)
Assignee: Dainippon Pharmaceutical Co., Ltd. (Osaka, JP) Laboratoire Roger Bellon (Neuilly sur Seine, FR)
Application Number:06/345,916
Patent Claims: 1. 1-Ethyl-6-fluo ro-1,4-dihydro-4-oxo-7-(1-piperazinyl)-1,8-naphthyridine-3-carboxylic acid.sesquihydrate.

2. A method for treatment of a bacterial infectious disease which comprises orally administering to a warm-blood animal an effective dose of the sesquihydrate defined in claim 1.

3. A process for the preparation of 1-ethyl-6-fluoro-1,4-dihydro-4-oxo-7-(1-piperazinyl)-1,8-naphthyridine-3-c arboxylic acid.sesquihydrate which comprises heating 1-ethyl-6-fluoro-1,4-dihydro-4-oxo-7-(1-piperazinyl)-1,8-naphthyridine-3-c arboxylic acid at a temperature above about 60.degree. C. in the presence of water in an amount sufficient to form the sesquihydrate.

4. A process according to claim 3 which comprises heating 1-ethyl-6-fluoro-1,4-dihydro-4-oxo-7-(1-piperazinyl)-1,8-naphthyridine-3-c arboxylic acid.trihydrate at a temperature above about 60.degree. C. in the presence of water.

5. A process according to claim 3 which comprises heating 1-ethyl-6-fluoro-1,4-dihydro-4-oxo-7-(1-piperazinyl)-1,8-naphthyridine-3-c arboxylic acid.anhydrate at a temperature above about 60.degree. C. in the presence of water in an amount sufficient to form the sesquihydrate.

6. A process according to claim 3 which comprises heating anhydrate and/or trihydrate of 1-ethyl-6-fluoro-1,4-dihydro-4-oxo-7-(1-piperazinyl)-1,8-naphthyridine-3-c arboxylic acid at a temperature above about 60.degree. C. and a relative humidity above 30%.

7. A process according to claim 6 which is carried out under a relative humidity above 80%.

8. A process according to claim 3 which comprises suspending anhydrate and/or trihydrate of 1-ethyl-6-fluoro-1,4-dihydro-4-oxo-7-(1-piperazinyl)-1,8-naphthyridine-3-c arboxylic acid in water and heating the suspension at a temperature above about 60.degree. C.

9. A process according to claim 3 which comprises dissolving anhydrate and/or trihydrate of 1-ethyl-6-fluoro-1,4-dihydro-4-oxo-7-(1-piperazinyl)-1,8-naphthyridine-3-c arboxylic acid in an aqueous alkaline solution or aqueous acidic solution, and neutralizing the solution by addition of an acid or alkali, and keeping it at a temperature above about 60.degree. C.

10. A process according to claim 3 which comprises dissolving a salt of 1-ethyl-6-fluoro-1,4-dihydro-4-oxo-7-(1-piperazinyl)-1,8-naphthyridine-3-c arboxylic acid in water, and neutralizing the solution by addition of an acid or alkali, and keeping it at a temperature above about 60.degree. C.

11. An antibacterial composition comprising as an active ingredient an antibacterially effective amount of the sesquihydrate defined in claim 1 and a pharmaceutically acceptable carrier therefor.
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