POLYMORPHS OF 1-CYCLOPROPYL-7-([S,S] - 2,8-DIAZADI

专利名称：POLYMORPHS OF 1-CYCLOPROPYL-7-([S,S] -2,8-DIAZADICYCLO [4.3.0] NON-8-YL) -6-FLUORO-1,4-DIHYDRO-8-METHOXY-4-OXO-3-QUINOLINE CARBOXYLIC ACID

HYDROCHLORIDE AND METHODS FOR THEPREPARATION THEREOF

发明人：TURCHETTA, Stefano,AROMATARIO,

Valentina

申请号：EP04791330.6申请日：20041028公开号：EP1685130B1公开日：20081210

摘要：Two novel crystalline forms, designated form A and form B of the antibacterialagent 1-cyclopropyl-7-([S,S])-2,8-diazadicyclo[4.3.0]non-8-yl)-6-fluoro-1,4-dihydro-8-methoxy-4-oxo-3-quinoline carboxylic acid hydrochloride of formula (I), the preparationthereof, and their pharmaceutical compositions are described. These crystalline forms,which are characterized by greater stability and ease of preparation and of formulation,can be produced by industrially applicable methods which comprises the steps of: a)suspending 1-cyclopropyl-7-([S,S])-2,8-diazadicyclo-[4.3.0]non-8-yl)-6-fluoro-1,4-dihydro-8-methoxy-4-oxo-3-quinoline carboxylic acid hydrochloride in a solvent selected from analcohol and a polyalcohol, b) heating the mixture under reflux, c) cooling, d) isolating theproduct which is separated, (form A) and additionally, e) reslurrying the solid at reflux in asolvent selected from alcohols and polyols or mixtures thereof, in which the resulting

mixture has an overall water content of between 2.5% and 0.01% by weight, f) isolatingthe product (form B).

申请人：CHEMI SPA

地址：IT

国籍：IT

代理机构：Pistolesi, Roberto

更多信息请下载全文后查看