Hoffmann-la Roche Inc.

Roche Vitamins Inc.

Basilea Pharmaceutica Ag

F. Hoffmann-la Roche Ag

Paul Spurr

Bernd Buettelmann

Beat Wirz

Steven Paul Hanlon

Mark Rogers-Evans

Georg Jaeschke

Juergen Wichmann

Thomas Johannes Woltering

Eric Vieira

Roland Jakob-Roetne

Andrew William Thomas

Sabine Kolczewski

Michelangelo Scalone

Matthew C Lucas

Simona Maria Ceccarelli

Hans Iding

Uwe Bornscheuer

Stephan Bachmann

Stefan Hildbrand

Richard Hugh Philip Porter

Milan Soukup

Pius Waldmeier

Fabienne Hoffmann-Emery

Christophe Pfleger

Stephen Deems Gabriel

Shaoning Wang

Pingsheng Zhang

Jason Yang

Amit Srivastava

René Trussardi

Miall Cedilote

Zhiming Dong

Doreen Miller

Bernard Orsat

Kewei Yang

Claude Stritt

Uwe Klinkhammer

Valérie Verhoeven

Jodie Brice

Christelle Carl

Martin Binder

Georg Trickes

Ioannis Pavlidis

Martin Steffen Weiss

Mario Mazzuchelli

Rene Trussardi

Daniel Bailey

Pingsheng Zhan

The invention provides a process for manufacturing 5-ethyl-4-methyl-N-[4-[(2S) morpholin-2-yl]phenyl]-1H-pyrazole-3-carboxamide (Formula I), or a pharmaceutically acceptable salt thereof, on an industrial scale, comprising a one-pot process for manufacturing 5-ethyl-4-methyl-1H-pyrazole-3-carboxylic acid (1).

Process for the preparation of substituted pyrazole derivatives

The present invention relates to compounds according to Formula (II): or a stereoisomer, tautomer or pharmaceutically acceptable salt or ester thereof, wherein A, Rand Rare defined herein. Also described are pharmaceutically acceptable compositions of Formula (II) compounds as well as methods for utilizing the compounds of Formula (II) and the pharmaceutically acceptable compositions of Formula (II) compounds as antibacterial agents and &#x3b2;-lactamase inhibitors, useful in the treatment of infectious diseases.

Diazabicyclooctane compounds

The present invention relates to a mutant transaminase with increased transaminase activity relative to the wild-type transaminase, a fusion protein comprising the transaminase, a polynucleotide coding for the transaminase, a host cell comprising the polynucleotide, mutant transaminase and/or fusion protein, a method of producing an amine with the mutant transaminase or fusion protein and the use of the mutant transaminase or fusion protein for the production of an amine.

Mutant transaminases as well as methods and uses relating thereto

The present invention provides methods for preparing 5-[2-[7-(trifluoromethyl)-5-[4-(trifluoromethyl)phenyl]pyrazolo[1,5-a]pyrimidin-3-yl]ethynyl]-2-pyridinamine (compound A), which is useful for the treatment of depression and other CNS disorders. The present methods are useful for preparing compound A on large scale in manufacturing facilities. 

Methods for the preparation of 5-[2-[7 (trifluoromethyl)-5-[4-(trifluoromethyl)phenyl]pyrazolo [1,5-A]pyrimidin-3-yl[ethynyl]-2-pyridinamine

The present invention relates to diazole derivatives of the general formula wherein A, E, R, Rand Rare as defined in application and pharmaceutical compositions containing them. The invention also relates to use of such compounds for the treatment of diseases mediated by the metabotropic glutamate receptors (mGluR), such as anxiety, chronic and acute pain, protection against liver damage, urinary incontinence, obesity, Fragile-X and autism, Alzheimer's disease, epilepsy, schizophrenia, ischemia, Huntington's chorea, amyotrophic lateral sclerosis (ALS), dementia caused by AIDs, and Parkinson's disease.

Diazole derivatives

The present invention is concerned with novel hydroxy-methyl isoxazole derivatives of formula I wherein R, Rand Rare as described herein, as well as pharmaceutically acceptable salts and esters thereof. The active compounds of the present invention have affinity and selectivity for GABA A &#x3b1;5 receptor. Further the present invention is concerned with the manufacture of the active compounds of formula I, pharmaceutical compositions containing them and their use as pharmaceuticals.

Substituted isoxazoles

The present invention relates to a process for the manufacture of compounds of formula Ia or Ib and pharmaceutically acceptable additional salts thereof, wherein R is lower alkyl. The compounds of formula Ia or Ib are valuable intermediate products for the manufacture of compounds that are pharmaceutically active as adenosine A2a receptor antagonist or metabotropic Glutamate receptor 2 antagonist. Such compounds are important in the regulation of many aspects of cellular metabolism and in the modulation of different central nervous system activities.

Process for the preparation of isonicotinic acid derivatives

The present invention relates to a process for preparation of amino substituted benzothiazole derivatives of formula I wherein with sulphoxide/HBr/solvent to give the desired products of formula I for R is hydrogen (formula IA) or for R is &#x2014;C(O)R' (formula IB) 

Cyclization process for substituted benzothiazole derivatives

Process for preparation of 2-phenyl acetic acid derivatives

Process for producing cephalosporin derivatives

The present invention concerns a process for the preparation of a 2,5 disubstituted pyridine of the formula (I) ##STR1## which comprises the steps of a) reacting a compound of the formula (II)

Process for the manufacture of 2,5-disubstituted pyridines

The invention is concerned with a process for making a compound of formula ##STR1## wherein R.sup.1 is hydrogen, alkyl, cyclo-alkyl, alkenyl, aryl or an amino protecting group; and

Process for making 3-amino-pyrolidine derivatives

A process for making a compound of formula ##STR1## wherein R signifies a C.sub.1-23 -alkyl group or a C.sub.2-23 -alkenyl group containing 1 to 3 double bonds, comprising the steps of (a) reacting a compound of formula ##STR2## with an acylating agent which is in a mixture comprising (i) an organic solvent and (ii) a lipase which is present in suspension, so as to form the compound of formula I; and (b) recovering the compound of formula I is provided for. The process can be used to make (11Z,13Z)-7,10-dihydro-10-hydroxy-retinyl acetate, an starting material for the production of vitamin A acetate.

Enzymatic acylation

A process for the manufacture of compounds of formula ##STR1##

Process for the manufacture of imidazodiazepine derivatives

The invention is concerned with a process for the preparation of a benzo[a]quinolizinone derivative of the formula ##STR1## by reacting a compound of the formula ##STR2## wherein X is halogen and Ph is phenyl, with carbon monoxide in the presence of a carbonylation catalyst and in the presence of (S)-3-ethoxypyrrolidine or a lower alkanol or water; where a lower alkyl ester of the 10-chloro-6,7-dihydro-4-oxo-3 -phenyl-4H-benzo[a]quinolizine-1-carboxylic acid has been obtained, converting this into the corresponding free acid; and, where the 10-chloro-6,7-dihydro-4-oxo-3-phenyl-4H-benzo[a]quinolizine-1-carboxylic acid has been obtained, reacting a reactive derivative thereof with (S)-3-ethoxypyrrolidine. The compound of formula I is useful for the treatment or prophylaxis of sleep disorders.

Process for the preparation of a benzo(a)quinolizione derivative

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Riehen, Switzerland

Paul Spurr