Teva Pharmaceutical Industries Limited

Teva Gyogyszergyar Zartkoruen Mukodo Reszvenytarsasag

Corus Pharma, Inc.

Biogal Gyogyszergyar Rt.

Teva Gyógyszergyár Zártkörüen Müködö Részvénytárasaság

Claude Singer

Anita Liberman

Judith Aronhime

Tamar Nidam

Nina Finkelstein

Gideon Pilarski

Csaba Szabo

Irena Veinberg

Marioara Mendelovici

Lilach Hedvati

Viktor Gyollai

Michael Pesachovich

Ziv Dee-Noor

Neomi Gershon

Eduard Schwartz

Yuriy Raizi

Evgeni Valdman

Ben-Zion Dolitzky

Nissim Garti

Ferenc Korodi

Yana Berkovich

Istvan Bodi

Erika Feher

Erika Magyar

Anita Liebermann

Lorant Gyuricza

Sharon Tomer

Valerie Niddam-Hildesheim

Greta Sterimbaum

Gideon Pilarsky

Joseph Schwarz

Kobi Chen

Julia Hrakovsky

Ruth Tenengauzer

Ehud Amir

Ramy Lidor

Viviana Braude

Szabolcs Salyi

Erzsebet Meszaros Sos

Arina Ceausu

Anita Lieberman

Ziv Dee Noor

Lev Khondo

Tania Lessen

Erszebet Meszaros-Sos

Mathi Mathivanan

Edward Schwartz

Szabolcs Szoke

Processes for preparing and purifying Pregabalin and salts thereof are provided.

Method for the preparation of Pregabalin and salts thereof

Processes are provided for preparing mupirocin calcium dihydrate from pseudomonic acid in a two phase system by using an organic carboxylate. A highly pure composition of amorphous mupirocin calcium is provided, and processes for its preparation by solvent removal, lyophilization and precipitation with use of an anti-solvent. Pharmaceutical compositions of amorphous form, and methods of using them to treat infections are also provided. Also provided are combined processes for preparing mupirocin calcium dihydrate and amorphous, by producing amorphous form first, followed by conversion of amorphous form into the dihydrate through crystallization from an aqueous solution. Also provided are processes for removing the water of crystallization of the dihydrate to obtain mupirocin calcium anhydrate.

Processes for preparing crystalline and amorphous mupirocin calcium

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

The present invention provides a stable 2-(2-pyridylmethyl) sulfinyl-1H-benzimidazole (lansoprazole) comprising either greater than 500 ppm and not more than about 3,000 ppm water or greater than 200 ppm and not more than about 5,000 ppm alcohol, or both. The present invention provides a method of preparing a stable lansoprozole as well as a pharmaceutical composition containing same. The present invention further provides a method of purifying lansoprazole that is substantially free of sulfone and sulfide derivatives.

Stable iansoprazole containing more than 500 ppm, up to about 3,000 ppm water and more than 200 ppm, up to about 5,000 ppm alcohol

The present invention provides a stable 2-(2-pyridylmethyl)sulfinyl-1H-benzimidazole (lansoprazole) and a method for stabilizing lansoprazole by use of a weakly basic material. The present invention also provides a method for the preparation of a stable lansoprazole.

Method of stabilizing lansoprazole

The invention relates to pure (R)-CMH and to the optical resolution of CMH-racemate, a key intermediate in the synthesis of (S)-Pregabalin. The invention also relates to the process for optically purifying (R)-CMH and to the process for isolating (S)-CMH from the mother liquor.

Optical resolution of 3-carbamoylmethyl-5-methyl hexanoic acid

The present invention provides a method for preparing a substantially pure lansoprazole containing less than about 0.2% (wt/wt) impurities including sulfone/sulfide derivatives. The present invention also provides a process for recrystallizing lansoprazole to obtain a lansoprazole containing less than about 0.1% (wt/wt) water.

Method for the purification of lansoprazole

The invention relates to pure (R)&#x2014;CMH and to the optical resolution of CMH-racemate, a key intermediate in the synthesis of (S)-Pregabalin. The invention also relates to the process for optically purifying (R)&#x2014;CMH and to the process for isolating (S)&#x2014;CMH from the mother liquor.

Provided is a process for preparation of amorphous form of an active pharmaceutical ingredient.

Process for preparation of amorphous form of a drug

The present invention encompasses Pregabalin substantially free of Lactam and a process for obtaining Pregabalin substantially free of Lactam comprising extracting an acidic mixture containing a complex of Pregabalin with a strong mineral acid, with C-alcohol; and combining the organic phase with an organic base.

Pregabalin free of lactam and a process for preparation thereof

A Pregabalin having a low level of 3-isobutylglutaric acid is provided.

Pregabalin free of isobutylglutaric acid and a process for preparation thereof

The invention relates to the &#x3b2; polymorph of Aztreonam, which contains less than 2.5% by weight residual solvent and to a process of making said polymorph. In the process of the invention, a polymorph of Aztreonam is dissolved in an absolute Calcohol in the presence of a base to form a solution, an acid is added to the solution, and the solution is stirred efficiently.

Aztreonam &#x3b2; polymorph with very low residual solvent content

The present invention relates to lamotrigine, a useful agent for anti-epilepsia. New crystal forms of lamotrigine containing molecules of the solvent in stoichiometric ratios are disclosed. The present invention also provides processes for preparing the new crystal forms of lamotrigine.

Crystal forms of lamotrigine and processes for their preparations

The present invention relates to the L-lysine salt of aztreonam and methods for making the L-lysine salt of aztreonam.

Aztreonam L-lysine and methods for the preparation and analysis thereof

Provided are novel Zaleplon crystalline Forms II, III, IV and V, which are useful for the treatment of insomnia. Also provided are processes for making Forms I, II, and V using precipitation methods.

Process for purifying N-[3-(3-cyanopyrazolo[1,5-a]pyrimidin-7-yl)phenyl]-N-ethylacetamide(zaleplon) and crystalline forms of zaleplon accessible with the process

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Kfar Saba, Israel

Claude Singer