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  Crystalline form of the zoledronic acid, a process to obtain it and the pharmaceutical composition comprising itUSPTO Application #: 20080090784Title: Crystalline form of the zoledronic acid, a process to obtain it and the pharmaceutical composition comprising it Abstract: A new crystalline form of the Zoledronic acid, characterized by its X-rays diffractogram as well as by its spatial atomic distribution in the red crystalline and its curves of thermal analysis. There is also included a method to obtain this crystalline form, which includes the synthesis of the corresponding acid and the pharmaceutical composition this crystalline form comprises. (end of abstract) Agent: Akerman Senterfitt - West Palm Beach, FL, US Inventors: Rafael A. Labriola, Dora G. Tombari, Adriana Vecchioli USPTO Applicaton #: 20080090784 - Class: 514094000 (USPTO) Related Patent Categories: Drug, Bio-affecting And Body Treating Compositions, Designated Organic Active Ingredient Containing (doai), Phosphorus Containing Other Than Solely As Part Of An Inorganic Ion In An Addition Salt Doai, Nitrogen Containing Hetero Ring, Hetero Ring Is Five-membered, Two Or More Hetero Atoms In The Five-membered Ring, Diazoles (including Hydrogenated) The Patent Description & Claims data below is from USPTO Patent Application 20080090784. Brief Patent Description - Full Patent Description - Patent Application Claims
FIELD OF THE INVENTION [0001] This invention refers to a new crystalline form of zoledronic acid, characterized by its diffractogram of X-rays as well as by its spatial atomic distribution in the crystalline network and its thermal analysis curves. [0002] There is also included a method to obtain this crystalline form, which comprises the synthesis of the corresponding acid and the pharmaceutical composition comprised by this crystalline form. BACKGROUND OF THE INVENTION [0003] Zoledronic acid (I) is a bisphosphonic acid, which acts as an inhibitor of bone osteoclastic resorption. This compound, chemically called 1-hydroxy-2-(1-imidazoyl) ethydilene bisphosphonic acid, is sold in the USA under the trade name of Zometa.RTM. (zoledronic acid for injectables). [0004] Zoledronic acid belongs to the family of the bisphosphonates well known for its features useful when treating diseases caused by dysfunctions in the metabolism of calcium and phosphorous [see for example K. R. Williams--J. C'hem. Ed. 81, 1406 (2004)]. [0005] There exist several patents describing methods for the obtention of bisphosphonates, particularly for zoledronic acid and its salts. DE 3626058 (1988); U.S. Pat. No. 4,777,163 (1988); EP 258618 (1988); U.S. Pat. No. 4,939,130 (1990) could be mentioned. [0006] In Chemical Abstract Services, there are various forms of free zoledronic acid and its salts registered: [0007] 1. Anhydrous Zoledronic acid (RN: 118072-93- 8). [0008] 2. Monohydrate Zoledronic acid (RN: 165800-06-6). [0009] 3. Zoledronic Acid, anhydrous disodium salt (RN: 131654-46-1). [0010] 4. Zoledronic Acid, monohydrate disodium salt (RN: 165800-07-7) [0011] 5. Zoledronic Acid, monohydrate trisodium salt (RN: 165 800-08-8). [0012] 6. Zoledronic Acid, magnesium salt (RN: 157432-59-2). [0013] 7. Zoledronic Acid, zinc salt (RN: 157432-58-I). [0014] U.S. Pat. No.4,939,130 describes that the zoledronic acid obtained has a melting point of 239.degree. C. [0015] Particularly, in the request of patent US Ser. No. 2005/0054616 diverse crystalline forms are described for the free acid and its sodium salts. [0016] Seven crystalline forms of zoledronic acid are described in this document, identified as forms I, II, XII, XV, XVIII, XX and XXVI through their diffractograms of X-rays and TGA (Thermogravimetric Analysis). [0017] The use of methansulphonic acid as a solvent in the preparation of alendronic acid and its salts is described in U.S. Pat. No. 4,922,007 (1990) and EP 462663 (1991). SUMMARY OF THE INVENTION [0018] This invention refers to a new polymorphic form of zoledronic: acid which exists in the form of a trihydrate, and to its method of obtaining it. [0019] The existence of a new crystalline stable form and of a simple and reproducible method for obtaining it widens the spectrum of possibilities for the design of new pharmaceutical forms. [0020] The use of the methansulfonic acid as a solvent to prepare zoledronic acid results in a homogeneous reaction. [0021] In other preparations where a diluent is used [see for instance U.S. Pat. No. 4,777,163 (1988) Example 1; US 2005/0054616 (2005) Examples 1-8], the reaction occurs in a heterogeneous phase. Continue reading... Full patent description for Crystalline form of the zoledronic acid, a process to obtain it and the pharmaceutical composition comprising it Brief Patent Description - Full Patent Description - Patent Application Claims Click on the above for other options relating to this Crystalline form of the zoledronic acid, a process to obtain it and the pharmaceutical composition comprising it patent application. ###  How KEYWORD MONITOR works... a FREE service from FreshPatents1. Sign up (takes 30 seconds). 2. Fill in the keywords to be monitored. 3. Each week you receive an email with patent applications related to your keywords. Start now! - Receive info on patent apps like Crystalline form of the zoledronic acid, a process to obtain it and the pharmaceutical composition comprising it or other areas of interest. ### Previous Patent Application: Materials and methods to potentiate cancer treatment Next Patent Application: Lpa receptor agonists and antagonists and methods of use Industry Class: Drug, bio-affecting and body treating compositions ### FreshPatents.com Support Thank you for viewing the Crystalline form of the zoledronic acid, a process to obtain it and the pharmaceutical composition comprising it patent info. IP-related news and info Results in 6.07034 seconds Other interesting Feshpatents.com categories: Accenture , Agouron Pharmaceuticals , Amgen , AT&T , Bausch & Lomb , Callaway Golf |
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