Proactively manage your pharmacy inventory
Deep knowledge on
small-molecule drugs and
the 110,000 global patents
Manage your formulary budget
Find generic entry opportunities
Anticipate generic drug launch
Drug patents …
… from Kazakhstan to Kalamazoo
Upgrade to enjoy subscriber-only features like email alerts and data export. See the Plans and Pricing
|Title:||Crystal modification of CDCH a process for its preparation and pharmaceutical formulations comprising this modification|
|Abstract:||The invention relates to the new monohydrate of 1-cyclopropyl-7-([S,S]-2,8-diazabicyclo-[4.3.0]non-8-yl)6-fluoro-1,4-dihyd ro-8-methoxy-4-oxo-3-quinolinecarboxylic acid hydrochloride (CDCH), a process for its preparation and pharmaceutical formulations which comprise this monohydrate as the active compound.|
|Inventor(s):||Grunenberg; Alfons (Dormagen, DE), Bosche; Patrick (Odenthal, DE)|
|Assignee:||Bayer Aktiengesellschaft (Leverkusen, DE)|
1. Monohydrate of CDCH, of the formula ##STR2## which has a characteristic peak at 168.1 ppm in the .sup.13 C-NMR spectrum and a band at 2.THETA.=26.7 in the X-ray diffractogram.
2. Compound according to claim 1 in the prismatic crystal form.
3. Process for the preparation of the CDCH monohydrate according to claim 1, characterized in that anhydrous CDCH is treated with an amount of water which is at least sufficient for thorough mixing and hydration until the stoichiometric content of water of crystallization has been absorbed and conversion of the crystals is complete, the crystals of the monohydrate thus obtained are separated off and the adsorbed water present is removed.
4. Process according to claim 3, characterized in that a suspension of the anhydrous CDCH in aqueous media is stirred until hydration and conversion of the crystals is complete.
5. Process according to claim 3, characterized in that, to prepare the monohydrate in the form of prisms, anhydrous CDCH or CDCH monohydrate in the form of needles is dissolved in media having a water content which is stoichiometrically sufficient but limited to 10%, and the solvent is then removed.
6. Process according to claim 3, characterized in that anhydrous CDCH is exposed to humidity until the crystals have been converted quantitatively.
7. An antibacterial composition comprising an antibacterially effective amount of a compound according to claim 1 and a pharmaceutically acceptable carrier.
8. An antibacterial composition comprising an antibacterially effective amount of a compound according to claim 2 and a pharmaceutically acceptable carrier.
9. A method of combating bacteria in a patient comprising administering to said patient an antibacterially effective amount of a compound according to claim 1.
10. A method of combating bacteria in a patient comprising administering to said patient an antibacterially effective amount of a compound according to claim 2.
Drugs may be covered by multiple patents or regulatory protections. All trademarks and applicant names are the property of their respective owners or licensors. Although great care is taken in the proper and correct provision of this service, thinkBiotech LLC does not accept any responsibility for possible consequences of errors or omissions in the provided data. The data presented herein is for information purposes only. There is no warranty that the data contained herein is error free. thinkBiotech performs no independent verifification of facts as provided by public sources nor are attempts made to provide legal or investing advice. Any reliance on data provided herein is done solely at the discretion of the user. Users of this service are advised to seek professional advice and independent confirmation before considering acting on any of the provided information. thinkBiotech LLC reserves the right to amend, extend or withdraw any part or all of the offered service without notice.