Teva Pharmaceutical Industries Limited

Viviana Braude

Nina Finkelstein

Shlomit Wizel

Barnaba Krochmal

Judith Aronhime

Claude Singer

Tamar Nidam

Anita Liberman

Gideon Pilarsky

Kobi Chen

Yuriy Raizi

Shalom Shabat

Serguei Fine

Crystalline pantoprazole sodium Forms II, IV, V, VI, VIII, IX, X, XI, XII, XIII, XIV, XV, XVI, XVII, XVIII, XIX and XX; pantoprazole sodium solvates containing water, acetone, butanol, methylethylketone, dimethylcarbonate, propanol and 2-methylpropanol; and amorphous pantoprazole sodium are disclosed.

Solid states of pantoprazole sodium, processes for preparing them and processes for preparing known pantoprazole sodium hydrates

The present invention provides a process comprising admixing a thioether with about 1.05 to about 1.6 molar equivalents of an active chlorine-containing oxidant, preferably sodium hypochlorite, and about 2.5 to about 5.0 molar equivalents of an alkali metal base; and recovering a sulfoxide that is preferably pantoprazole, lansoprazole, omeprazole, or rabeprazole. The process may further comprise contacting the sulfoxide with a source of sodium ions, preferably sodium hydroxide, to produce the sodium salt of the sulfoxide. The invention also relates to novel chlorinated derivatives of pantoprazole including 5-(difluoromethoxy)-2-[[(3,4-dimethoxy-2-pyridinyl)-chloromethyl]sulfinyl]-1H-benzimidazole and 5-(difluoromethoxy)-2-[[(3,4-dimethoxy-2-pyridinyl)-chlorohydroxymethyl]sulfinyl]-1H-benzimidazole and processes for making them. The invention also relates to processes of quantifying and identifying a compound other than pantoprazole in a mixture of pantoprazole and at least one other compound.

Process for preparing 2-[(pyridinyl)methyl]sulfinyl-substituted benzimidazoles and novel chlorinated derivatives of pantoprazole

Provided are processes for the preparation of sildenafil base and the citrate salt of sildenafil. Also provided are sildenafil citrate water adduct and a method of preparing pharmaceutical compositions comprising combining the sildenafil citrate and/or sildenafil citrate water adduct with at least one pharmaceutically-acceptable excipient.

Methods for the production of sildenafil base and citrate salt

The present invention provides improved methods of converting R&#x2014;N-(4-morpholiyl-3-fluorophenyl)-2-oxo-5-oxazolidinyl-methyl azide (III) to the intermediate S&#x2014;N-(4-morpholinyl-3-fluorophenyl)-2-oxo-5-oxazolidinyl-methyl amine (II) that involve the production of fewer by-products than previous methods. The amine (II) may then be converted into linezolid (I) of high chemical purity with respect to the inactive R-enantiomer and bis-linezolid (IV), and is in high yield, without the need for tedious, complicated purification steps, such as chromatography.

Processes for the preparation of linezolid intermediate

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Kadima, Israel

Viviana Braude