Crystal modification C of 8-cyano-1-cyclopropyl-7-(1S,6S-2,8-diazabicyclo-[4.3.0]nonan-8-yl)-6-fluoro-1,4-dihyro-4-oxo-3-quinoline carboxylic
AssigneeBayer Aktiengesellschaft
InventorsHubert Rast, Thomas Himmler
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Abstract
The present invention relates to a defined crystal modification of 8-cyano-1-cyclopropyl-7-(1S,6S-2,8-diazabicyclo[4.3.0]nonan-8-yl)-6-fluoro-1,4-dihydro-4-oxo-3-quinolinecarboxylic acid of the formula (1), to processes for its preparation and to its use in pharmaceutical preparations. The crystal modification can be distinguished from other crystal modifications of 8-cyano-1-cyclopropyl-7-(1S,6S-2,8-diazabicyclo[4.3.0]nonan-8-yl)-6-fluoro-1,4-dihydro-4-oxo-3-quinolinecarboxylic acid of the formula (1) by its characteristic X-ray powder diffractogram and its differential thermodiagram (see description).
Claims4
8-Cyano- 1-cyclopropyl-7-(1S,6S-2,8-diazabicyclo[4.3.0]nonan-8-yl)-6-fluoro-1,4-dihydro-4-oxo-3-quinolinecarboxylic acid (CCDC) of the crystal modification C, characterized in that it has an X-ray powder diffractogram with the following reflection signals (2 theta) of high and medium intensity.
- 2 θ (2 theta) 5.7 12.6 15.5 17.2 20.2 26.4 27.
8-Cyano-1-cyclopropyl-7-(1S,6S-2,8-diazabicyclo[4.3.0]nonan-8-yl)6-fluoro-1,4-dihydro-4-oxo-3-qinolinecarboxylic acid (CCDC) of the crystal modification C, characterized in that it has an X-ray powder diffractogram with the following reflection signals (2 theta) of high and medium intensity
- 2 θ (2 theta) 5.7 12.6 15.5 17.2 20.2 26.4 27
- and a melting point, determined by DTA, of from 235° C. to 237° C.
A compound that is 8-Cyano-1-cyclopropyl-7-(1S, 6S-2,8-diazabicyclo[4.3.0]nonan-8-yl)-6-fluoro-1,4-dihydro-4-oxo-3-quinolinecarboxylic acid (CCDC) of the crystal modification C, obtainable by exposing CCDC of unknown modification or amorphous CCDC to a relative atmospheric humidity of at least 92% until there is no further weight increase, then drying the product and subsequently heating it to a temperature above the rearrangement temperature.
Process for preparing CCDC of the crystal modification C, characterized in that CCDC of unknown modification or amorphous CCDC is exposed to a relative atmospheric humidity of at least 92% until there is no further weight increase, then drying the product and subsequently heating it to a temperature above the rearrangement temperature.
Dependencies are inferred from the claim text.