Janssen Pharmaceutica Nv

Tibotec Pharmaceuticals Ltd.

Noramco Gmbh

Azad Pharma Ag

Hartmut B Zinser

Cheryl A Grice

Neelakandha S Mani

Laurent Gomez

John J M Wiener

Piet Tom Bert Paul Wigerinck

Christa C Chrovian

Xiaohu Deng

Genesis M Bacani

Yong Gong

Virginia M Tanis

Susanne Lochner

Alejandro Santillán, Jr

Jimmy T Liang

Alice Lee-Dutra

Matteo Conza

Diego Broggini

Aaron M Kearney

Kathleen C Sappey

Vit Lellek

Adrienne M Landry-Bayle

Kia Sepassi

Kristine Nerkararyan

Eugene Y Cheung

Alvah T Wickboldt

Tamar Danielyan

Mikayel Movsisyan

Mariam Gharibyan

Meri Grigoryan

Birgit M Ebert

Nicolaas Martha Felix Goyvaerts

Peter Hermann Hölzle

Alejandro Santillan

Anne M Fourie

John J Wiener

John JM Wiener

Anne M Fourine

Kathleen C Sappy

The present invention relates to a novel route of synthesis for the opioid receptor antagonist Buprenorphine or a pharmaceutically acceptable salt thereof, starting from thebaine, wherein the route comprises the reaction of thebaine with a dienophile; forming an alkylated reaction product by reaction with a Grignard-reagent; formation of an cyanamide; deprotection of the cyanamide- and the phenolic-oxygen-moiety, wherein the cleavage of one or both groups is performed in the presence of an alkali or alkaline earth sulfide; followed by derivatization with a cyclopropyl-halogen and hydrogenation to yield Buprenorphine.

Process for the synthesis of buprenorphine

The present invention is directed to a process for the preparation of opioid compounds such as buprenorphine, naltrexone, naloxone, nalbuphone, nalbuphine, and the like.

Process for the preparation of opioid compounds

The present invention is directed to a process for the preparation of sulfamide derivatives.

Process for the preparation of sulfamide derivatives

A process for the preparation of N-isobutyl-N-(2-hydroxy-3-amino-4-phenylbutyl)-p-nitrobenzenesulfonylamide derivatives in which a (1-benzyl-2-hydroxy-3-isobutylamino-propyl)-carbamic acid derivative is reacted with a p-nitrophenylsulfonyl halide to provide the desired product in a high yield and degree of purity.

Methods for the preparation of N-isobutyl-N-(2-hydroxy-3-amino-4-phenylbutyl)-p-nitrobenzenesulfonylamide derivatives

Thiazolopyridin-2-yloxy-phenyl and thiazolopyrazin-2-yloxy-phenyl amine compounds are described, which are useful as LTA4 hydrolase (LTA4H) modulators. Such compounds may be used in pharmaceutical compositions and methods for modulation of LTA4H and for the treatment of disease states, disorders, and conditions mediated by LTA4 hydrolase activity.

Thiazolopyridin-2-yloxy-phenyl and thiazolopyrazin-2-yloxy-phenyl amines as modulators of leukotriene A4 hydrolase

The present invention relates to a process for the preparation of (3R,3aS,6aR)-hexahydrofuro[2,3-b]furan-3-yl (1S,2R)-3-[[(4-aminophenyl)sulfonyl](isobutyl) amino]-1-benzyl-2-hydroxypropylcarbamate as well as intermediates for use in said process. More in particular the invention relates to processes for the preparation of (3R,3aS,6aR)-hexahydrofuro[2,3-b]furan-3-yl (1S,2R)-3-[[(4-aminophenyl)sulfonyl](isobutyl)amino]-1-benzyl-2-hydroxypropylcarbamate which make use of 4-amino-N-((2R,3S)-3-amino-2-hydroxy-4-phenylbutyl)-N-(isobutyl)benzene sulfonamide intermediate, and to processes amenable to industrial scaling up. (3R,3aS,6aR)-hexahydrofuro[2,3-b]furan-3-yl (1S,2R)-3-[[(4-aminophenyl)sulfonyl](isobutyl)amino]-1-benzyl-2-hydroxypropylcarbamate is particularly useful as HIV protease inhibitors.

Process for the preparation of (3R,3aS,6aR)-hexahydrofuro [2,3-b] furan-3-yl (1S,2R)-3[[(4-aminophenyl) sulfonyl] (isobutyl) amino]-1-benzyl-2-hydroxypropylcarbamate

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Schaffhausern, Switzerland

Hartmut B Zinser