- Manufacture of high-purity meloxicam via its novel potassium salt monohydrate
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An improved procedure for the manufacture of 4-hydroxy-2- methyl-N-(5-methyl-1,3-thiazol-2-yl)-2H-1,2-benzothiazine-3-carboxamide 1,1-dioxide (meloxicam) is described. The key intermediate of this protocol is the new potassium salt monohydrate of meloxicam, which makes possible the efficient removal of impurities, resulting in an environmentally friendly manufacturing process of the high-purity (>99.90%) drug substance.
- Mezei, Tibor,Mesterhazy, Norbert,Bako, Tibor,Porcs-Makkay, Marta,Simig, Gyula,Volk, Balazs
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- USE OF NON-STEROIDAL ANTI-INFLAMMATORY DRUGS MELOXICAM AND PIROXICAM, ADMINISTERED INTRAVAGINALLY, FOR INTERRUPTION OF A WOMAN'S OVULATION PROCESS
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The invention relates to the use of the non-steroidal anti-inflammatory compounds meloxicam and piroxicam to inhibit ovulation in women, the medication being administered by topically vaginal delivery.
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Page/Page column
(2014/07/09)
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- Process for the Purification of Meloxicam
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A process for purifying meloxicam form I from a crude meloxicam, which comprises: i. contacting the crude meloxicam with an amine in a non-aqueous solvent to form a meloxicam salt;ii. isolating the meloxicam salt;iii. dissolving the meloxicam salt in an aqueous solvent to form a salt solution; andiv. adding an acid to the salt solution to precipitate free meloxicam.
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Page/Page column 2
(2008/12/05)
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- Process for the purification of meloxicam
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The present invention relates to a process for the purification of meloxicam and in particular of the impurity composed of 4-hydroxy-2-methyl-N-ethyl-N′-(5-methyl-2-thiazolyl)-2H-1,2-benzothiazine-3-carboxamide-1,1-dioxide and to meloxicam containing a quantity of less than 0.05% of the above-mentioned impurity (“ethylamide”).
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Page/Page column 3; 4
(2008/06/13)
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- Process for the preparation of crystalline form-1 of 4-hydroxy-2-methyl-N-(5-methyl-2-thiazolyl)-2H-1,2-benzothiazine-3-carboxamide-1,1-dioxide
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The present invention is related to an improved process for preparing crystalline Form I of meloxicam, which produces the Form I in high yield.
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Page/Page column 2-3
(2010/02/15)
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- PROCESS FOR PREPARATION OF HIGH-PURITY MELOXICAM AND MELOXICAM POTASSIUM SALT
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The invention provides a process for the preparation of high purity meloxicam of the Formula (II). The meloxicam raw product is reacted with the solution of potassium hydroxide or potassium carbonate, whereby high purity meloxicam potassium sait monohydrate is produced. Said sait is subsequently treated with minerai or organic acid to yield high-purity meloxicam.
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- Process for the purification of meloxicam
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Process for the purification of meloxicam and in particular of the impurity composed of 4-hydroxy-2-methyl-N-ethyl-N'-(5-methyl-2-thiazolyl)-2H-1,2-benzothiazine-3-carboxamide-1,1-dioxide comprising the following steps: a) the meloxicam is treated in crude form with an alcohol solution of an alkaline alcoholate at a temperature between 25 and 35°C.b) the solution obtained in step (a) is acidified to a pH between 1.5 and 4.0 and the precipitated product composed of meloxicam is filtered, the wet filtered product obtained from the previous step is crushed in a polar aprotic solvent and the product of the crushing is isolated by means of filtration and drying.
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Page/Page column 4-5
(2008/06/13)
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- Method for the treatment and prevention of cachexia
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Cachexia, including anorexia and other forms of weight loss, is a frequent complication of acute and chronic infections, and result from induction of cytokines, prostaglandins, and other inflammatory mediators that are critical for pathogen elimination. The present invention includes methods for the treatment or prevention of cachexic conditions while maintaining the production of factors essential for infection control through the administration of an effective amount of a cyclooxygenase-2 selective inhibiting compound.
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- Effect of structural modification of enol-carboxamide-type nonsteroidal antiinflammatory drugs on COX-2/COX-1 selectivity
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Meloxicam (5), an NSAID in the enol-carboxamide class, was developed on the basis of its antiinflammatory activity and relative safety in animal models. In subsequent screening in microsomal assays using human COX-1 and COX-2, we discovered that it possessed a selectivity profile for COX-2 superior to piroxicam and other marketed NSAIDs. We therefore embarked on a study of enol-carboxamide type compounds to determine if COX-2 selectivity and potency could be dramatically improved by structural modification. Substitution at the 6- and 7-positions of the 4-oxo-1,2-benzothiazine-3- carboxamide, alteration of the N-methyl substituent, and amide modification were all examined. In addition we explored several related systems including the isomeric 3-oxo-1,2-benzothiazine-4-carboxamides, thienothiazines, indolothiazines, benzothienothiazines, naphthothiazines, and 1,3- and 1,4- dioxoisoquinolines. While a few examples were found with greater potency in the COX-2 assay, no compound tested had a better COX-2/COX-1 selectivity profile than that of 5.
- Lazer, Edward S.,Miao, Clara K.,Cywin, Charles L.,Sorcek, Ronald,Wong, Hin-Chor,Meng, Zhaoxing,Potocki, Ian,Hoermann, MaryAnn,Snow, Roger J.,Tschantz, Matt A.,Kelly, Terence A.,McNeil, Daniel W.,Coutts, Simon J.,Churchill, Laurie,Graham, Anne G.,David, Eva,Grob, Peter M.,Engel, Wolfhard,Meier, Hans,Trummlitz, Günter
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p. 980 - 989
(2007/10/03)
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- 4-HYDROXY-2H-1,2-BENZOTHIAZINE-3-CARBOXAMIDE-1,1,-DIOXIDES AND SALTS THEREOF
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Compounds of the formula wherein R1 is hydrogen, methyl or ethyl; R2 is methyl, ethyl or n-propyl; and Y is hydrogen, methyl, methoxy, fluorine or chlorine; and non-toxic, pharmacologically acceptable salts thereof formed with an inorganic or organic base. The compounds as well as their salts are useful as antiphlogistics.
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