Janssen Pharmaceutica Nv

Janssen Sciences Ireland Unlimited Company

Yolande Lydia Lang

Michel Joseph Maurice André Guillaume

Alfred Elisabeth Stappers

Carina Leys

Sigrid Carl Maria Stokbroekx

Shane Barry Robinson

Sigrid Carl Stokbroekx

Michel Joseph Guillaume

Johan Erwin Edmond Weerts

Georges Joseph Cornelius Hoornaert

Frans Josef Cornelius Compernolle

Armin Roessler

Bart Petrus Anna Maria Jozef Medaer

Tomasz Kozlecki

Wim Albert Alex Aelterman

Anne Faure

Peter Jozef Maria Van Remoortere

Hua Mao

Stefan Marcel Herman Leurs

Dirk De Smaele

Lars Ulmer

Thierry Brossette

Ioannes Nicolaos Houpis

Jean François Alexandre Lucas Hegyi

Julius W J Dickens

Dominique Paul Michel DeprÉ

Dirk Janssen Pharmaceutica NV De Smaele

Armin Cilag Ag Pharmaceutical & Chem Roessler

Julius WJ Dickens

Stefan Marcel Leurs

Dominique Paul Michel Depre

Wim Albert Aelterman

Johan Erwin Weerts

Jean Francois Hegyi

Peter Jozef Van Remoortere

Julius W Dickens

The present invention relates to an improved process for preparing [(1S,2R)-3-[[(4-aminophenyl)-sulfonyl](2-methylpropyl)amino]-2-hydroxy-1-(phenylmethyl)-propyl]-carbamic acid (3R,3aS,6aR)-hexahydrofuro[2,3-b]furan-3-yl ester&#x2014;which compound is also known under its INN as darunavir&#x2014;by reacting carbonic acid 2,5-dioxo-1-pyrrolidinyl [(3R,3aS,6aR)-hexahydrofuro[2,3-b]furan-3-yl]ester with 4-amino-N-[(2R,3S)-3-amino-2-hydroxy-4-phenylbutyl]-N-(2-methylpropyl)-benzenesulfonamide in ethanol as solvent. Furthermore said process allows for darunavir to be isolated immediately in its ethanolate form, i.e. darunavir monoethanolate, which is the marketed form of darunavir under the tradename Prezista&#x2122;.

Simplified procedure for the preparation of darunavir

The present invention relates to an improved process for preparing [(1S,2R)-3-[[(4-aminophenyl)-sulfonyl](2-methyl-propyl)amino]-2-hydroxy-1-(phenylmethyl)-propyl]-carbamic acid (3R,3aS,6aR)-hexahydrofuro[2,3-b]furan-3-yl ester&#x2014;which compound is also known under its INN as darunavir&#x2014;by reacting carbonic acid 2,5-dioxo-1-pyrrolidinyl[(3R,3aS,6aR)-hexahydrofuro[2,3-b]furan-3-yl]ester with 4-amino-N-[(2R,3S)-3-amino-2-hydroxy-4-phenylbutyl]-N-(2-methylpropyl)-benzenesulfonamide in ethanol as solvent. Furthermore said process allows for darunavir to be isolated immediately in its ethanolate form, i.e. darunavir monoethanolate, which is the marketed form of darunavir under the tradename Prezista&#x2122;.

This invention provides novel crystalline forms of mono-HCl salts and a mono-HCl salt hydrate of JNJ-26481585, an inhibitor of histone deacetylases. The invention also relates to processes for production of these forms, to intermediates used in these processes, to pharmaceutical compositions comprising these forms, and to the use of these forms in medical treatment for instance as a medicine to inhibit proliferative conditions, such as cancer and leukemia.

Mono-hydrochloric salts of an inhibitor of histone deacetylase

The present invention relates to the fumarate salt of (alpha S, beta R)-6-bromo-alpha-[2-(dimethylamino)ethyl]-2-methoxy-alpha-1-naphthalenyl-beta-phenyl-3-quinolineethanol, pharmaceutical compositions comprising as active ingredient said salt and to processes for their preparation.

Fumarate salt of (alpha S, beta R)-6-bromo-alpha-[2-(dimethylamino)ethyl]-2-methoxy-alpha-1-naphthalenyl-beta-phenyl-3-quinolineethanol

The present invention concerns the use of dibutyl tin oxide for regioselective catalytic diol mono-tosylation at a concentration lower than 2 mol %. The present invention also concerns the use of a generic acetal compound of Formula (Ic) in a catalytic process for regioselective diol mono-tosylation, wherein Y is selected from the group of Calkyl, phenyl and benzyl. The concentration of the generic acetal compound of Formula (Ic) is less than about 2 mol %, preferably ranges between about 2 mol % and about 0.0005 mol %, preferably ranges between about 0.1 mol % and about 0.005 mol %. 

Process for regioselective mono-tosylation of diols

The present invention relates to a novel process for the production of [2-(4-fluoro-benzyl)-phenyl]-acetic acid, a compound obtainable from phthalic anhydride. The process comprises the subsequent steps a) through e): In an alternative embodiment, the step e) is replaced by the steps f1) and f2): The present invention provides a process for the production of [2-(4-fluoro-benzyl)-phenyl]-acetic acid which is suitable for industrial scale reactors (e.g. which is cleaner and more efficient). Also, [2-(4-fluoro-benzyl)-phenyl]-acetic acid is obtained as a crystalline material with a purity &#x3e;95%.

Process for the production of [2-(4-fluoro-benzyl)-phenyl]-acetic acid

The present invention concerns processes for the preparation of each of the 4 diastereomers of formula (I)in stereochemically pure form from either of two enantiomerically pure precursors. The tetracyclic ringsystem having trans-fused five and seven membered rings is formed in an acid-catalysed cyclization reaction. The invention further relates to the thus obtained cis-fused tetracyclic alcohol intermediates, the methanamine end-products, the methanamine end-products for use as a medicine, in particular as CNS active medicines.

Preparation of trans-fused 3,3a,8,12b-tetrahydro-2h-dibenzo[3,4:6,7]cyclohepta[1,2-b]furan derivatives

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Vosselaar, Belgium

Yolande Lydia Lang