Hoffmann-la Roche Inc.

Basilea Pharmaceutica Ag

Genentech, Inc.

F. Hoffmann-la Roche Ag

Roche Vitamins Inc.

Beat Wirz

Hans Iding

Jean Ackermann

Kurt Hilpert

David Banner

Paul Hadvary

Hans Peter Wessel

Klaus Gubernator

Wolfgang Wostl

Hans Hilpert

Gerard Schmid

Synese Jolidon

Andrew William Thomas

Rene Wyler

Rosa Maria Rodriguez-Sarmiento

Reinhard Reents

Matthias Heinrich Nettekoven

Mark Rogers-Evans

Stephan Roever

Michelangelo Scalone

Paul Hebeisen

Francis Gosselin

Richard Barner

Paul Spurr

Bernd Kuhn

Peter Mohr

Uwe Grether

Katrin Groebke Zbinden

Wolfgang Haap

Konrad H Bleicher

Ulrike Obst Sander

Alfred Binggeli

Rosa Maria Rodriguez Sarmiento

Thomas B Tschopp

Ludvik Labler

Klaus Muller

Daniela Krummenacher

Scott J Savage

Chong Han

Ulrich Zutter

G Erard Schmid

Klaus M Uller

Josepf Hubscher

Hans-Peter Maerki

Fabienne Ricklin

Kurt Puentener

Narendra Panday

Urs Schwitter

Uwe Bornscheuer

Markus Meyer

Ulrike Obst

Roland Humm

Stefan Hildbrand

Jean-Michel Adam

Bruno Lohri

Olaf Grassmann

Martin Karpf

Hans-Juergen Mair

Roland Meier

Urs Weiss

Ernst Kupfer

Stefan Abrecht

Pascal Dott

Steven Paul Hanlon

Ren&eacute; Trussardi

Bernard Orsat

Scott Savage

Kazimierz Michal Pietrusiewicz

Wioleta Swierczynska

Martin Steffen Weiss

Ioannis Pavlidis

Han Min Tong

Stefan Schmid

Scott Borthwick

René Wyler

The present disclosure relates to processes for preparing (cyclopentyl[d]pyrimidin-4-yl)piperazine compounds, and more particularly relates to processes for preparing (R)-4-(5-methyl-7-oxo-6,7-dihydro-5H-cyclopenta[d] pyrimidin-4-yl)piperazine and N-protected derivatives thereof, which may be used as an intermediate in the synthesis of Ipatasertib (i.e., (S)-2-(4-chlorophenyl)-1-(4-((5R,7R)-7-hydroxy-5-methyl-6,7-dihydro-5H-cyclopenta[d]pyrimidin-4-yl)piperazin-1-yl)-3-(isopropylamino)-propan-1-one). The present disclosure additionally relates to various compounds that are intermediates employed in these processes.

Process for preparing (cyclopentyl[d]pyrimidin-4-yl)piperazine 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 processes to manufacture crystalline N-[(3S)-1-[4-[(3-fluorophenyl)methoxy]phenyl]-5-oxo-pyrrolidin-3-yl]acetamide. Also disclosed are compounds useful as intermediates in the methods of the invention.

Process to manufacture N-[(3S)-1-[4-[(3-fluorophenyl)methoxy]phenyl]-5-oxo-pyrrolidin-3-yl]acetamide

The invention is concerned with processes for the manufacture of the pyrrolidine-3,4-dicarboxamide derivative of formula (I), and the intermediates useful for those processes of manufacture.

Processes for the manufacture of a pyrrolidine-3,4-dicarboxamide derivative

The invention is concerned with cyclic amines of formula (I) wherein Xto X, Yto Y, R, Rand n are as defined in the description and in the claims, as well as physiologically acceptable salts thereof. These compounds inhibit coagulation factor Xa and can be used as medicaments and for treating diseases associated with coagulation factor Xa.

Cyclic amines

The invention is concerned with new phosphine ligands of the formula I wherein

Phosphine ligands

The present invention relates to compounds of the formula I: wherein Rto Rare as defined in the description and claims, and pharmaceutically acceptable salts thereof. The compounds are useful for the treatment and/or prophylaxis of diseases which are associated with the modulation of CB1 receptors, such as obesity.

Pyrazinecarboxamide derivatives as CB1 antagonists

The present invention relates to compounds of the formula wherein X and Rto Rare as defined in the description and claims, and pharmaceutically acceptable salts thereof. The compounds are useful for the treatment and/or prophylaxis of diseases which are associated with the modulation of CB1 receptors, such as obesity.

Pyridine-3-carboxamide derivatives as CB1 inverse agonists

The invention relates to racemic or enantiomerically pure 4-pyrrolidino derivatives, processes for their preparation, pharmaceutical compositions comprising said derivatives, and their use in the prevention and treatment of a disease which is mediated by a monoamine oxidase B inhibitor, in particular Alzheimer's disease and senile dementia.

4-pyrrolidino-phenyl-benzyl ether derivatives

The present invention relates to a process for the preparation of enantiopure intermediates useful in the synthesis of valuable pharmaceutically active compounds, e.g. MAOB inhibitors, and to novel intermediates of formulae I and II wherein R, R, Rand Rare as defined in the description and claims.

Process for the preparation of enantiopure pyrrolidin-2-one derivatives

The invention relates to racemic or enantiomerically pure 4-pyrrolidino derivatives, processes for their preparation, pharmaceutical compositions comprising said derivatives, and their use in the prevention and treatment of illness, in particular which is mediated by monoamine oxidase B inhibitors, in particular Alzheimer's disease or senile dementia.

4-Pyrrolidino-phenyl-benzyl ether derivatives

The present invention relates to a new process for the preparation compounds of formula Iwherein R, R, Rand n are as described in the description which process comprises reacting compounds of formula IIwherein R, R, R, n and Rare as described in the description, with a protease in an aqueous system containing an organic co-solvent. The compound of formula I are useful for the preparation of 1,5-benzothiazepines which are useful as enzyme inhibitors, such as protease, interleukin-1&#x3b2;-converting enzyme, elastase or angiotensin converting enzyme, GPCR antagonists (cholecystokinin, angiotensin II receptor).

Substituted 2-amino-3-(2-amino-phenylsulfanyl)-propionic acids

Compounds of formula I are providedas well as pharmaceutically acceptable salts and esters thereof, wherein Rto R, A, Aand n have the significance indicated in the specification.

Indolyl derivatives

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Reinach, Switzerland

Beat Wirz