Teva Pharmaceutical Industries Limited

Algatechnologies Ltd.

Santiago Ini

Mili Abramov

Anita Liberman

Yaron Shmuely

Tamas Koltai

Sigalit Levi

Eran Turgeman

Judith Aronhime

Ben-Zion Dolitzky

Evgeny Shapiro

Kobi Chen

Michal Rafilovich

Eli Lancry

Dina Berezovsky

Osnat Porter-Kleks

Alexei Ploutno

Naama Chasid

Ron Bar-Shavit

The invention encompasses novel amorphous and crystalline forms of carvedilol phosphate, carvedilol hydrogen phosphate, and carvedilol dihydrogen phosphate as well as methods of making the novel amorphous and crystalline forms. Also disclosed are pharmaceutical compositions comprising the novel amorphous and crystalline forms and uses thereof.

Amorphous carvedilol dihydrogen phosphate

Carvedilol phosphate

The present invention relates to a process for preparing paliperidone from its intermediate 3-(2-chloroethyl)-6,7,8,9-tetrahydro-9-hydroxy-2-methyl-4H-pyrrido[1,2-a]-pyrimidin-4-one.

Process for the synthesis of 9-hydroxy risperidone (paliperidone)

(S)-N,N-Dimethyl-3-(1-naphthalenyloxy)-3-(2-thienyl)propanamine maleate (DNT-maleate) and polymorphs of DNT-maleate, compositions of DNT-maleate and its polymorphs, processes for the preparation of DNT-maleate and its polymorphs, and processes for the preparation of duloxetine hydrochloride from DNT-maleate are provided.

DNT-maleate and methods of preparation thereof

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

The invention encompasses 2-(N-methyl-propanamine)-3-(2-naphthol)thiophene, a duloxetine hydrochloride impurity, as well as its use as a reference marker and reference standard.

2-(N-methyl-propanamine)-3-(2-naphthol)thiophene, an impurity of duloxetine hydrochloride

A chiral resolution process for the preparation of (S)-AT-OL, and a process for the racemization of AT-OL are provided.

Process for the preparation of (S)-(-)-N,N-dimethyl-3-(2-thienyl)-3-hydroxypropananine, a duloxetine intermediate

Process for the purification of duloxetine HCl is provided.

Process for the purification of duloxetine hydrochloride

DNT-Oxal crystalline forms and processes for making DNT-Oxal crystalline forms are provided.

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Haifa, Israel

Santiago Ini