Hoffmann-la Roche Inc.

F. Hoffmann-la Roche Ag

Fabienne Hoffmann-Emery

Urs Schwitter

Jean-Michel Adam

Christophe Pfleger

Olaf Grassmann

Rene Trussardi

Ralph Diodone

Thomas Hartung

Frederic Ran

Benno Rothenhaeusler

Bjorn Bartels

Pius Waldmeier

Gerard Moine

Hans Hilpert

Hasane Ratni

Mark Rogers-Evans

Roland Jakob-Roetne

Michelangelo Scalone

Walter Hunkeler

Torsten Hoffmann

Bjoern Bartels

Kurt Puentener

Paul Spurr

Stefan Hildbrand

Andrew Sleight

Ursula Hoffmann

Roland Meier

Serena Maria Fantasia

Helmut Werner Stahr

Goesta Rimmler

René Trussardi

Pascal Dott

Daniel Vincent Fishlock

Pankaj Rege

Georg Wuitschik

Christian Moessner

Fran&ccedil;ois Jenck

James Richard Martin

Sonja Nick

Fabian Feyen

The invention provides processes to manufacture substituted 1-[4-(Pyridin-2-yloxy)-cyclohexyl]-5,6-dihydro-4H-2,3,5,10b-tetraaza-benzo[e]azulenes. Also disclosed are compounds useful as intermediates in the methods of the invention.

Synthesis of trans-8-chloro-5-methyl-1 -[4-(pyridin-2-yloxy)-cyclohexyl]-5,6-dihydro-4H-2,3,5,10B-tetraaza-benzo[e]azulene and crystalline forms thereof

The present invention relates to a process for the preparation of 7-(4,7-diazaspiro[2.5]octan-7-yl)-2-(2,8-dimethylimidazo[1,2-b]pyridazin-6-yl)pyrido[1,2-a]pyrimidin-4-one derivatives useful as pharmaceutically active compounds.

Process for the preparation of 7-(4,7-diazaspiro[2.5]octan-7-yl)-2-(2,8-dimethylimidazo [1,2-B]pyridazin-6-yl)pyrido[1,2-a]pyrimidin-4-one derivatives

Synthesis of trans-8-chloro-5-methyl-1-[4-(pyridin-2-yloxy)-cyclohexyl]-5,6-dihydro-4H-2,3,5,10B-tetraaza-benzo[e]azulene and crytalline forms thereof

The present invention relates to a process for the preparation of 2-pyrazolo[1,5-a]pyrazin-2-ylpyrido[1,2-a]pyrimidin-4-one derivatives useful as pharmaceutically active compounds.

Process for the preparation of 2-pyrazolo[1,5-a]pyrazin-2-ylpyrido[1,2-a]pyrimidin-4-one compounds

The present invention provides processes to manufacture substituted 1-[4-(Pyridin-2-yloxy)-cyclohexyl]-5,6-dihydro-4H-2,3,5,10b-tetraaza-benzo[e]azulenes. Also disclosed are compounds useful as intermediates in the methods of the invention.

Synthesis of trans-8-chloro-5-methyl-1-[4-(pyridin-2-yloxy)-cyclohexyl]-5,6-dihydro-4H-2,3,5,10B-tetraaza-benzo[E]azulene and crytalline forms thereof

The invention relates to a novel process for the preparation of (3S,4S)- or (3R,4R)-1-benzyl-4-(halogen-aryl)-pyrrolidine-3-carboxylic acids of formula I or salts thereof, wherein X and Y are each independently hydrogen or a halogen atom, with the proviso that at least one of X or Y is a halogen atom. The compounds of formula I are useful as starting materials or intermediates for the preparation of pharmaceutically active compounds, especially for compounds, which are useful for the treatment of central nervous system disorders.

Process for the preparation of pyrollidine-3-carboxylic acids

The invention relates to a process for the optical resolution of a dibenzo[b,d]azepinone derivative of formula II, wherein Ris hydrogen or halogen and Ris either C-alkyl optionally substituted with C-cycloalkyl or benzyl which is optionally substituted with C-alkoxy, to obtain a (S)-7-amino-5H,7H-dibenzo[b,d]azepin-6-one of formula I, wherein Ris as in the compound of formula II. The (S)-7-amino-5H,7H-dibenzo[b,d]azepin-6-one of formula I can be used as a chiral building block for the preparation of malonamide derivatives which have the potential to act as &#x3b3;-secretase inhibitors and therefore may be useful in the treatment of Alzheimer's disease and cancer.

Process for preparation of enantiomerically pure compounds

The present invention relates to a new crystalline modification of 2-(3,5-bis-trifluoromethyl-phenyl)-N-[6-(1,1-dioxo-1&#x3bb;-thiomorpholin-4-yl)-4-(4-fluoro-2-methyl-phenyl)-pyridin-3-yl]-N-methyl-isobutyramide characterized by the following X-ray diffraction pattern obtained with a Cu, radiation at 2&#x3b8; (2Theta)=4.5, 6.4, 7.5, 7.7, 8.0, 8.2, 10.0, 10.2, 10.9, 11.1, 12.9, 13.4, 14.0, 14.5, 15.1, 15.6, 16.2, 16.5, 17.3, 17.5, 18.0, 18.9, 19.3, 19.5, 19.9, 20.1, 20.6, 21.0, 21.4, 22.7, 23.1 and 23.6 and an infrared spectrum having sharp bands at 2925, 2854, 1637, 1604, 1484, 1395, 1375, 1285, 1230, 1172, 1125, 1082, 999, 943, 893, 868, 860, 782, 705, 684 cm, and wherein the extrapolated melting point (DSC) is 137.2&#xb0; C.

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Process for preparation of 2-phenyl acetic acid derivatives

Imidazodiazepine derivative

A process is described for preparing certain 4-alkyl- or 4-aryl-pyridine derivatives.

Process for the preparation of pyridine derivatives

The present invention relates to a process for manufacturing diazepine derivatives of the general formula I

Method of making diazepine derivatives

Growing community of inventors

Weil am Rhein, Germany

Fabienne Hoffmann-Emery