Teva Pharmaceutical Industries Limited

Teva Pharmaceuticals Usa, Inc.

Gideon Pilarski

Claude Singer

Marioara Mendelovici

Nina Finkelstein

Lilach Hedvati

Ziv Dee-Noor

Yuriy Raizi

Michael Pesachovich

Sharon Tomer

Ben-Zion Dolitzky

Tamar Nidam

Valerie Niddam-Hildesheim

Neomi Gershon

Greta Sterimbaum

Eduard Schwartz

Ariel Mittelman

Ilya Avrutov

Nurit Perlman

Revital Ramaty

Nada Kosutic Hulita

Marina Kalujny

Greta Sterinbaum

Edward Schwartz

Ziv Dee Noor

Solid state forms of Sitagliptin salts (e.g. Sitagliptin sulfate, Formula I), processes for preparing the solid state forms, and pharmaceutical compositions thereof, are provided. These compounds are of a class of dipeptidyl peptidase IV enzyme inhibitors which are useful, for example, for the manufacture of a medicament for the treatment of type 2 diabetes mellitus. 

Solid state forms of sitagliptin salts

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

Method for the preparation of Pregabalin and salts thereof

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 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 are a method for making (&#xb1;)-1-Cyclopropyl-6-fluoro-1,4-dihydro-8-methoxy-7-(3-methyl-1-piperazinyl)-4-oxo-3-quinolenecarboxylic acid, commonly known as gatifloxacin, in high purity, in a suspension in a dipolar aprotic solvent.

Synthesis of gatifloxacin

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 present invention provides substantially pure cilostazol. The present invention also provides cilostazol particles that have reduced particle size.

Substantially pure cilostazol and processes for making same

Substantially pure cilostazol and processing for making same

Disclosed are processes for preparing novel carbamate intermediates of paroxetine comprising dealkylating N-alkylparoxetine by reaction thereof with a haloalkyl ester of a haloformic acid, in a suitable organic solvent. Also disclosed are processes for preparing paroxetine comprising hydrolyzing the novel carbamate intermediates in a suitable solvent. Paroxetine prepared by the above processes can be neutralized with hydrogen chloride and crystallized as paroxetine hydrochloride anhydrous, hemihydrate or as a solvate of isopropanol. The invention is further directed to the novel carbamate intermediates formed by the disclosed processes.

Preparation of paroxetine involving novel intermediates

The present invention relates to a process of preparing benzisoxazole methane sulfonic acid-chloride (BOS&#x2014;Cl) as an zonisamide intermediate via chlorination of benzisoxazole methane sulfonate. The present invention also discloses a process of preparing zonisamide via amidation of BOS&#x2014;Cl. More particularly, the present invention provides a process of preparing zonisamide, comprising the steps of: a) chlorinating BOS, salts or esters thereof, with SOClin an organic solvent and/or in the presence of a catalyst to form BOS&#x2014;Cl; and b) amidating BOS&#x2014;Cl in the presence of ammonia selected from the group consisting of aqueous ammonia in a biphasic system, masked ammonia and dry ammonia to form zonisamide.

Method for preparing benzisoxazole methane sulfonyl chloride and its amidation to form zonisamide

Pharmaceutical compositions containing substantially pure and stable gabapentin are disclosed wherein gabapentin contains an anion of a mineral acid, such as chloride, in amounts greater than 20 ppm.

Stable gabapentin containing more than 20 ppm of chlorine ion

The present invention provides processes for preparing cilostazol and processes for purifying cilostazol by recrystallization.

Growing community of inventors

Holon, Israel

Gideon Pilarski