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Rosuvastatin Zinc Salt Rosuvastatin-Zinksalz Sel De Zinc De Rosuvastatine

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Rosuvastatin Zinc Salt Rosuvastatin-Zinksalz Sel De Zinc De Rosuvastatine (19) TZZ Z_¥__T (11) EP 2 013 188 B1 (12) EUROPEAN PATENT SPECIFICATION (45) Date of publication and mention (51) Int Cl.: of the grant of the patent: C07D 239/42 (2006.01) A61K 31/505 (2006.01) 07.09.2016 Bulletin 2016/36 A61P 3/06 (2006.01) (21) Application number: 07733847.3 (86) International application number: PCT/HU2007/000030 (22) Date of filing: 12.04.2007 (87) International publication number: WO 2007/119085 (25.10.2007 Gazette 2007/43) (54) ROSUVASTATIN ZINC SALT ROSUVASTATIN-ZINKSALZ SEL DE ZINC DE ROSUVASTATINE (84) Designated Contracting States: • TÁPAI, Sándorné AT BE BG CH CY CZ DE DK EE ES FI FR GB GR 2230 Gyömrö (HU) HU IE IS IT LI LT LU LV MC MT NL PL PT RO SE SI SK TR (74) Representative: Stolmár & Partner Designated Extension States: Patentanwälte PartG mbB et al AL BA HR MK RS Blumenstraße 17 80331 München (DE) (30) Priority: 13.04.2006 HU 0600293 (56) References cited: (43) Date of publication of application: EP-A- 1 336 405 WO-A-01/60804 14.01.2009 Bulletin 2009/03 WO-A-03/068739 WO-A-2004/108691 WO-A-2006/017698 (73) Proprietor: Egis Gyógyszergyár Nyilvánosan Múködö • DATABASE WPI Derwent Publications Ltd., Részvénytársaság London, GB; AN 2006-089591 XP002448430 1106 Budapest (HU) ZHAO ZHIQUAN [CN]: "An Anti-hyperlipemia Composition" & WO 2005/123082 A (LUNAN (72) Inventors: PHARMACEUTICAL COMPANY L [CN];) 2005 • VÁGÓ, Pál • GRAUL A ET AL: "ATORVASTATIN CALCIUM" 1173 Budapest (HU) DRUGS OF THE FUTURE, BARCELONA, ES, vol. • SIMIG, Gyula 22, no. 9, 1997, pages 956-968, XP000904817 1126 Budapest (HU) ISSN: 0377-8282 • CLEMENTIS, György 1118 Budapest (HU) Remarks: • TÖMPE, Péter Thefile contains technical information submitted after 1116 Budapest (HU) the application was filed and not included in this specification Note: Within nine months of the publication of the mention of the grant of the European patent in the European Patent Bulletin, any person may give notice to the European Patent Office of opposition to that patent, in accordance with the Implementing Regulations. Notice of opposition shall not be deemed to have been filed until the opposition fee has been paid. (Art. 99(1) European Patent Convention). EP 2 013 188 B1 Printed by Jouve, 75001 PARIS (FR) EP 2 013 188 B1 Description FIELD OF THE INVENTION 5 [0001] The present invention relates to the zinc salt of (+)-7-[4-(4-fluorophenyl)-6-isopropyl-2-(N-methyl-N-methyl- sulphonylamino)pyrimidin-5-yl]-(3R,5S)-dihydroxy-(E)-6-heptenecarboxylic acid of the Formula (I), 10 15 20 25 its hydrates, process for their preparation, medicinal products containing said salts and the use of said salts in the medicine. (+)-7-[4-(4-fluorophenyl)-6-isopropyl-2-(N-methyl-N-methyl-sulphonyl- amino)-pyrimidin-5-yl]-(3R,5S)-dihydroxy-(E)-6- 30 heptene-carboxylic acid of the Formula (II) [0002] 35 40 45 50 is known under the International Nonproprietary Name (INN) rosuvastatin. TECHNICAL BACKGROUND OF THE INVENTION [0003] Rosuvastatin of the Formula (II) has been disclosed for the first time in European Patent No. 521471. The 55 calcium salt of rosuvastatin is used in the medicine for the treatment of hypercholesterolemia, hyperlipoproteinemia and atherosclerosis. [0004] The health authorities are setting strict quality criteria towards pharmaceutically active ingredients. Some of these criteria are related to the chemical purity and stability of the pharmaceutically active ingredients. Other official 2 EP 2 013 188 B1 requirement is the manufacture of the medicinal product in satisfactory quality and that the medicinal product shall have appropriate stability. Such criteria are determined by and published in the corresponding articles of pharmacopoeias. [0005] In the case of rosuvastatin of the Formula (II), basic requirements for the active pharmaceutical ingredient intended for the use in medicinal products are high purity, appropriate stability and the possibility of simple formulation. 5 [0006] According to published International Patent Application No. WO 00/042024, the amorphous rosuvastatin of the Formula (II) obtained according to the process of European Patent No. 521471 can be used in the pharmaceutical technology with great difficulties. In order to eliminate this disadvantage, crystalline forms having more advantageous physical properties than the amorphous product are prepared. The manufacture of crystalline rosuvastatin calcium salt, however, is a manufacturing process requiring high production volume and results in great loss of material. 10 [0007] The basic problem in the manufacture of the calcium salt of rosuvastatin resides in the fact that the primary product obtained is poorly filterable and can not be purified in an easy way. Published International Patent Application WO 04/14872 discloses non-crystalline product having advantageous filterability. According to the process of said ap- plication, the calcium salt of advantageous particle size is prepared by reacting an alkaline metal, ammonium, methyl- ammonium or tris(hydroxymethyl)-methylammonium salt of rosuvastatin with calcium chloride in an aqeuous solution. 15 [0008] In the published International Patent Application No. WO 01/60804, there are disclosed high purity ammonium-, lithium- or magnesium salts of rosuvastatin of the Formula (II) in order to solve production problems which arose during the manufacture of amorphous rosuvastatin. Starting from the above-mentioned salts, it is possible to prepare amorphous rosuvastatin in a quality suitable for the manufacture of medicinal products. [0009] Published International Patent Application WO 2005/051921 discloses a similar process, wherein isopropy- 20 lammonium or cyclohexylammonium salts of rosuvastatin are produced in high purity and said salts are transformed into sodium salt or high purity amorphous calcium salt of rosuvastatin. [0010] Published International Patent Application No. WO 2005/040134 discloses amorphous rosuvastatin calcium salt of high diastereomeric purity. [0011] In WO 2005/123082 A1 is described a pharmaceutical composition comprising acipimox and rosuvastatin or 25 its pharmaceutically acceptable salts, esters or solvates. As preferred rosuvastatin salts are mentioned sodium salts, calcium salts, potassium salts, magnesium salts, zinc salts, and iron salts. As suitable rosuvastatin esters are mentioned esters formed with aliphatic alcohols, aromatic alcohols, heterocyclic alcohols, in particular methyl esters, ethyl esters, allyl esters, phenyl esters of rosuvastatin. [0012] WO 2004/108691 A1 describes a process for the production of rosuvastatin calcium (2:1). 30 [0013] The process comprises the following steps: a) reaction of a (1-6C) alkyl ester of (E)-(6-{2-[4-(4-fluorophenyl)-6-isopropyl-2-[methyl (methylsulfonyl) amino] py- rimidin-5-yl] vinyl} (4R, 6S) -2, 2-dimethyl [1, 3] dioxan-4-yl) acetic acid in a water miscible organic solvent with aqueous acid at an elevated temperature; 35 b) reaction of the resulting solution with an aqueous alkali metal hydroxide and optionally washing the resulting aqueous alkali metal salt solution with a suitable organic solvent; c) adjustment of the pH of the resulting solution to between pH6 and pH 11; 40 d) removal of the water miscible organic solvent; e) optional filtration of the resulting mixture; 45 f) addition of a water soluble calcium salt to the filtrate so as to form (E)-7- [4-(4- fluorophenyl)-6-isopropyl-2- [methyl (methylsulfonyl) amino] pyrimidin-5-yl] (3R, 5S)-3, 5- dihydroxyhept-6-enoic acid calcium salt; and g) isolation of the product of step f). 50 [0014] A. Graul et al. Drugs of the future 1997, 22(9), 956-968 describes the synthesis of Atorvastatin calcium, its pharmaceutical activity and clinical studies done with the compound. [0015] EP 1 336 405 describes formulations of atorvastatin stabilized with alkali metal additions. The amorphous atorvastatin may be one or more of atorvastatin calcium, atorvastatin magnesium, atorvastatin aluminum, atorvastatin iron, and atorvastatin zinc. In the examples amorphous atorvastatin and atorvastatin magnesium is used as the phar- 55 maceutical ingredient. [0016] WO 2006/017698 describes pharmaceutical compositions comprising a statin and an omega-3 oil. As statins are used pravastatin, fiuvastatin, atorvastatin, lovastatin, simvastatin, rosuvastatin, and cerivastatin. Preferred statin salts are a calcium salt of pravastatin, a calcium salt of fluvastatin, a magnesium salt of pravastatin and a zinc salt of 3 EP 2 013 188 B1 pravastatin. [0017] WO 03/068739describes a method ofmanufacturing an amorphous formof the hemi-calcium saltof atorvastatin. [0018] According to the disclosed process, the primary product amorphous rosuvastatin calcium salt is crystallized in the first stage, the product thus obtained is subsequently transformed into the amorphous form. 5 [0019] In summary, it can be concluded that according to the state of the art, the manufacture of rosuvastatin calcium salt suitable for the preparation of medicinal products is a particularly intricate process. The crude product must be submitted to further purification and crystallization steps in order to obtain a suitable product with regard to purity and physical properties. The known processes are difficult to operate in an industrial scale process and the use of such known processes often results in a significant loss of material and is therefore uneconomical. 10 SUMMARY OF THE INVENTION [0020] The objective of our research-development work was to develop a new salt of [(+)-7-[4-(4-fluorophenyl)-6- isopropyl-2-(N-methyl-N-methylsulphonyl-amino)pyrimidin-5-yl]-(3R,5S)-dihydroxy-(E)-6-heptenecarboxylic
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