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  Novel crystalline forms of aripiprazoleUSPTO Application #: 20080085903Title: Novel crystalline forms of aripiprazole Abstract: The present invention provides novel crystalline forms of aripiprazole and aripiprazole hydrochloride, processes for their preparation and pharmaceutical compositions containing them. (end of abstract) Agent: Caesar, Rivise, Bernstein, Cohen & Pokotilow, Ltd. - Philadelphia, PA, US Inventors: Bandi Parthasaradhi Reddy, Kura Rathnakar Reddy, Rapolu Raji Reddy, Dasari Muralidhara Reddy, Kesireddy Subash Chander Reddy USPTO Applicaton #: 20080085903 - Class: 514253080 (USPTO) Related Patent Categories: Drug, Bio-affecting And Body Treating Compositions, Designated Organic Active Ingredient Containing (doai), Heterocyclic Carbon Compounds Containing A Hetero Ring Having Chalcogen (i.e., O,s,se Or Te) Or Nitrogen As The Only Ring Hetero Atoms Doai, Hetero Ring Is Six-membered Consisting Of Two Nitrogens And Four Carbon Atoms (e.g., Pyridazines, Etc.), 1,4-diazine As One Of The Cyclos, Piperazines (i.e., Fully Hydrogenated 1,4-diazines), Additional Hetero Ring Attached Directly Or Indirectly To The Piperazine Ring By Nonionic Bonding, , , , , , The Patent Description & Claims data below is from USPTO Patent Application 20080085903. Brief Patent Description - Full Patent Description - Patent Application Claims
FIELD OF THE INVENTION [0001] The present invention provides novel crystalline forms of aripiprazole and aripiprazole hydrochloride, processes for their preparation and pharmaceutical compositions containing them. BACKGROUND OF THE INVENTION [0002] Aripiprazole of formula (I): or 7-[4-[4-(2,3-Dichlorophenyl)-1-piperazinyl]butoxy]-3,4-dihydro-2(1H)-quin- olinone and its salts are useful for treating schizophrenia and their therapeutic uses were disclosed in U.S. Pat. No. 5,006,528. [0003] Processes for the preparation of aripiprazole and its salts were described in U.S. Pat. No. 5,006,528. These processes do not produce well defined, reproducible crystalline forms. [0004] Thus there is a need for stable and reproducible crystalline forms of aripiprazole and its salts. [0005] We have discovered two novel crystalline forms of aripiprazole and four novel crystalline forms of aripiprazole hydrochloride. The novel forms have been found to be stable over the time and reproducible and so, suitable for pharmaceutical preparations. [0006] Thus, the object of the present invention is to provide stable novel crystalline forms of aripiprazole, processes for preparation of the novel crystalline forms and pharmaceutical compositions containing these novel crystalline forms. [0007] Another object of the present invention is to provide stable novel crystalline forms of aripiprazole hydrochloride, processes for preparation of the novel crystalline forms and pharmaceutical compositions containing these novel crystalline forms. [0008] Since the novel crystalline forms of aripiprazole hydrochloride are obtained with high purity, preparation of aripiprazole via the crystalline forms of aripiprazole hydrochloride serves as a means of producing pure aripiprazole. SUMMARY OF THE INVENTION [0009] According to one aspect of the present invention, there is provided a novel crystalline form of aripiprazole, designated as Form I, characterized by an x-ray powder diffraction pattern having peaks expressed as 2.theta. at about 8.7, 11.6, 16.3, 17.7, 18.6, 20.3, 23.4, 24.9 degrees. FIG. 1 shows typical Form I x-ray powder diffraction pattern. [0010] According to another aspect of the present invention there is provided a process for preparation of the Form I of aripiprazole comprising the steps of: a) dissolving aripiprazole in a suitable solvent; b) refluxing for about 30 minutes to 1 hour; c) cooling slowly to about 15.degree. C. to 25.degree. C.; d) maintaining for about 2 hour to 4 hours at about 15.degree. C. to 25.degree. C.; and e) filtering the solid separated. [0011] The suitable solvent is selected from the group consisting of acetone, ethyl acetate, methanol or ethanol. [0012] According to another aspect of the present invention, there is provided a novel crystalline form of aripiprazole, designated as Form II, characterized by an x-ray powder diffraction pattern having peaks expressed as 2.theta. at about 12.7, 15.1, 17.5, 18.2, 18.8, 19.5, 20.6, 21.2, 22.6, 23.3, 24.2, 24.9, 27.6, 30.0, 31.6, 35.8 degrees. FIG. 2 shows typical Form II x-ray powder diffraction pattern. [0013] According to another aspect of the present invention there is provided a process for preparation of the Form II of aripiprazole, which comprises dissolving aripiprazole in tetrahydrofuran and vacuum drying at about 25.degree. C. or spray drying. [0014] According to another aspect of the present invention, there is provided a novel crystalline form of aripiprazole hydrochloride, designated as Form A, characterized by an x-ray powder diffraction pattern having peaks expressed as 2.theta. at about 6.2, 8.5, 11.5, 15.2, 15.5, 16.8, 17.2, 18.3, 18.9, 19.6, 20.6, 21.3, 23.4, 24.1, 24.7, 25.9, 27.5, 28.3, 28.9, 32.8 degrees. FIG. 3 shows typical Form A x-ray powder diffraction pattern. [0015] According to another aspect of the present invention there is provided a process for preparation of the Form A of aripiprazole hydrochloride comprising the steps of: a) dissolving aripiprazole in methanol or isopropyl alcohol; Continue reading... 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