Teva Pharmaceutical Industries Limited

Biogal Gyogyszergyar Rt.

Yeda Research and Develpment & Co. Ltd

Teva Gyogyszergyar Zartkoruen Mukodo Reszvenytarsasag

Teva Pharmaceuticals Usa, Inc.

Biogal Gy&oacute;gyszergy&aacute;r Rt.

Biogal Gryogyszergyar Rt.

Ben-Zion Dolitzky

Judith Aronhime

Gennady Nisnevich

Boris Pertsikov

Igor Rukhman

Jean Hildesheim

Julia Kaftanov

Shlomit Wizel

Marioara Mendelovici

Evgeny Shapiro

Dov Diller

Shoshana Ben-Valid

Jenny Shammai

Ofer Reany

Tamar Nidam

Gideon Pilarsky

Boaz Gome

Ronit Yahalomi

Sergey Finogueev

Nissim Garti

Marina Etinger

Barnaba Krochmal

Yana Berkovich

Yigael Gozlan

Claude Singer

Valerie Niddam-Hildesheim

Neomi Gershon

Ilan Kor

Anita Liebermann

Ruth Arnon

Revital Lifshitz-Liron

Anton Frenkel

Gideon Pilarski

Boris Tishin

Greta Sterimbaum

Santiago Ini

Igor Lifshitz

Michael Yuzefovich

Rina Aharoni

Michal Schwartz

Hagit Eisen-Nevo

Anchel Schwartz

Michael Pinchasov

David Leonov

Sergei Fine

Serguei Finogueev

Eli Lancry

Yaron Shmuely

Boris Fedotev

Alisa Berlin

Ilan Kor-Sade

Thomas Bayer

Evgeni Flyaks

Dina Blasberger

Irit Pinchasi

Inna Perutski

Eran Luvchick

Reuven Izsak

IIan Kor

Igal Gozlan

Gannady A Nisnevich

Marko Kordova

Provided are a method of making irbesartan via a Suzuki coupling reaction and a novel intermediate, 2-butyl-3-(4'-bromobenzyl)-1,3-diazaspiro[4.4]non-1-ene-4-one, for such process. The novel process includes the step of reacting such intermediate with a protected imidazolephenylboronic acid.

Synthesis of irbesartan

The present invention provides 3-benzyloxy-2-aminopyridine (BOPA), 3-(2-Hydroxyethyl)-2-methyl-9-hydoxy-4H-pyrido[1,2-a]pyrimidine-4-one (HMBP), 3-(2-Chloroethyl)-2-methyl-9-hydoxy-4H-pyrido[1,2-a]pyrimidine-4-one (CMHP) and 3-(2-chloroethyl)-6,7,8,9-tetrahydro-9-hydroxy-2-methyl-4H-pyrrido[1,2-a]-pyrimidin-4-one (CMHTP) useful as intermediates for the preparation of paliperidone. The present invention also provides processes for preparing these intermediates and for preparing paliperidone.

Process for the synthesis of CMHTP and intermediates thereof

Provided is a crystalline (polymorphic) form of fexofenadine hydrochloride, denominated fexofenadine hydrochloride Form XVI.

Polymorphic Form XVI of fexofenadine hydrochloride

This invention relates to an improved process of preparing carvedilol, as well as a new crystalline hydrate and solvate and forms of carvedilol, processes for the manufacture thereof, and pharmaceutical compositions thereof.

Carvedilol

The invention provides a composition comprising a mixture of polypeptides, wherein each polypeptide (a) is a copolymer of the amino acids L-glutamic acid, L-alanine, L-tyrosine, and L-lysine, and (b) may be in the form of a pharmaceutically acceptable salt; and wherein in the mixture (i) the polypeptides have an average molecular weight in the range 13,500 to 18,500 daltons, (ii) 13% to 38% of the polypeptides have a diethylamide group instead of a carboxyl group present at one end thereof, and (iii) 68% of the polypeptides have a molecular weight between 7,000 and 41,000 daltons. In an embodiment, the average molecular weight is 16,000 daltons. The invention also provides a method of treating a human subject afflicted with a neurodegenerative disease comprising administering to the human subject a therapeutically effective amount of any of the disclosed compositions so as to thereby treat the human subject.

Mixtures of polypeptides, compositions containing and processes for preparing same, for treating neurodegenerative diseases

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

Provided are novel crystalline and amorphous forms of ibandronic acid, methods for their preparation, and pharmaceutical compositions containing them. Also provided are methods for purifying and assaying ibandronic acid in any crystalline form (or amorphous).

Solid and crystalline ibandronic acid

The invention encompasses aripiprazole crystalline forms, methods of preparing the same, and pharmaceutical compositions having aripiprazole crystalline forms.

Methods of preparing aripiprazole crystalline forms

The subject invention provides an improved process for obtaining a mixture of polypeptides having nonuniform amino acid sequences, where each polypeptide consists essentially of alanine, glutamic acid, tyrosine and lysine where the resulting mixture of polypeptides comprises less than 0.3% brominated tyrosine and less than 1000 ppm metal ion impurities.

Process for preparation of mixtures of polypeptides using purified hydrobromic acid

This invention encompasses methods of synthesizing olanzapine without solvents or by using low boiling organic solvents.

Methods of synthesizing olanzapine

Provides are crystalline forms of nateglinide, labeled Forms A, C, D, F, G, I, J, K, L, M, N, 0, P, Q, T, U, V, Y, &#x3b1;, &#x3b2;, &#x3b3;, &#x3b4;, &#x3b5;, &#x3c3;, &#x3b8; and &#x3a9;, processes for their preparation and processes for preparation of other crystalline forms of nateglinide. Also provided are their pharmaceutical formulations and methods of administration.

Polymorphic forms of nateglinide

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 invention encompasses synthesizing 7-(4-bromobutoxy)-3,4-dihydrocarbostyril by mixing 7-hydroxy-tetrahydroquinolinone, dibromobutane, and at least one base to form a reaction mixture; heating the reaction mixture; cooling the reaction mixture; and isolating the 7-(4-bromobutoxy)-3,4-dihydrocarbostyril from the reaction mixture. The invention also encompasses using phase transfer catalysts during the reaction.

Method of making 7-(4-bromobutoxy)-3,4-dihydrocarbostyril

Provides are crystalline forms of nateglinide, labeled Forms A, C, D, F, G, I, J, K, L, M, N, O, P, Q, T, U, V, Y, &#x3b1;, &#x3b2;, &#x3b3;, &#x3b4;, &#x3b5;, &#x3c3;, &#x3b8; and &#x3a9;, processes for their preparation and processes for preparation of other crystalline forms of nateglinide. Also provided are their pharmaceutical formulations and methods of administration.

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Petach Tiqva, Israel

Ben-Zion Dolitzky