Smithkline Beecham Corporation

Glaxosmithkline LLC

Olon S.p.a.

Smithkline Beecham Farmaceutici

Silvano Ronzoni

Giulio Dondio

Stefano Maiorana

Giorgio Bertolini

Mara Sada

Mario Grugni

Giorgio Cignarella

Corrado Colli

Filippo Nisic

Romano Di Fabio

Stefania Bertuolo

Daniela Barlocco

Vittorio Vecchietti

Roberto Colle

Giuseppe Giardina

Davide Graziani

Giuseppe Arnaldo Maria Giardina

Aldo Bianchi

Faris Garis

Cinzia Biaggi

Pier Andrea Gatti

Adolfo Prandi

Giovanni Palombi

Subject-matter of the present invention is a process for preparing intermediates for the synthesis of optically active beta-amino alcohols by enzymatic reduction of the corresponding beta-amino ketones. Subject-matter of the invention are also said novel synthesis intermediates and the use thereof in the preparation of active pharmaceutical ingredients, among which vilanterol and the salts thereof.

Process for preparing intermediates for the synthesis of optically active beta-amino alcohols by enzymatic reduction and novel synthesis intermediates

The present invention relates to a process for the preparation of a novel and versatile synthesis intermediate and its use in the preparation of umeclidinium. The invention also relates to some reference standards allowing to detect impurity traces recurring in the preparation of umeclidinium and a process for their preparation.

Process for the preparation of a novel umeclidinium synthesis intermediate

Diastereoselective and enantioselective synthetic routes for the preparation of compounds of formula (I): or derivatives thereof,wherein:

Preparation of benzosuberonylpiperidine compounds

Compounds of formula (I) or a derivative thereof, wherein; R is Calkyl, Ccycloalkyl, Calkoxy, hydroxy, halo, Calkenyl, Calkynyl, amino, Calkylamino, di(Calkyl)amino, hydroxyCalkyl, CalkoxyCalkyl, aminoCalkyl, (Calkyl)aminoCalkyl, di(Calkyl)aminoCalkyl; Ris hydrogen or R; Ris hydroxy, Calkoxy, amino, Calkylamino, di(Calkyl)amino; Ris hydrogen or Calkyl; Rand Rare each independently selected from the list consisting of perhaloCalkyl, hydrogen, halo, Calkyl, Calkoxy, hydroxy, amino, Calkylamino, di(Calkyl)amino, hydroxyCalkyl, CalkoxyCalkyl, aminoCalkyl, (Calkyl)aminoCalkyl, di(Calkyl)aminoCalkyl, aryl, and COX wherein X may be hydroxy, Calkoxy, Calkyl, amino, Calkylamino, or di(Calkyl)amino; with the proviso that, when Ris hydrogen, then Rand Rare not both hydrogen; and wherein any alkyl group or the alkyl moiety of any group containing such a moiety may be substituted one or more times by halo; are ligands of the ORL-1 receptor and are useful in therapy. 

Benzosuberonylpiperdine compounds as analgesics

Compounds of formula I, or a salt thereof or a hydrate thereof, as follows:wherein

Compounds

Heterocycle-condensed morphinoid derivatives (II)

Compounds, or solvates or salts thereof, of formula (I):

Diarylalkenylamine derivatives

Heterocycle-condensed morphinoid derivatives

Substituted hydroisoquinoline derivatives and their use as

Diaryldiamine derivatives and their use as delta opiod (ANT)-agonists

Octahydro-1H-pyrrolo�3,2-g!and �2,3-g!isoquinoline derivatives

##STR1## Compounds of formula (I) in which, R is linear or branched alkyl, cycloalkyl, cycloalkylalkyl, alkenyl, aryl, aralkyl or furan-2-yl alkyl; R.sub.1 and R.sub.2, which may be the same or different, are each hydrogen, hydroxy, alkoxy, or halogen; R.sub.3 is hydrogen, hydroxy or alkoxy; 'Het' is optionally substituted single or fused heteroxyclic ring, containing from 5 to 10 ring atoms and comprising up to four heteratoms in the or each ring, selected from oxygen, nitrogen and sulphur; R.sub.4 and R.sub.5, which may be the same or different, are each hydrogen alkyl, halogen, nitro; CF, cyano, alkoxy carbonyl, NH, alkylcarbonylamino, hydroxy, alkoxy, or benzyl, are selective delta receptor agonists and are useful in the treatment of pain.

Hydroisoquinoline derivatives

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Milan, Italy

Silvano Ronzoni