Hoffmann-la Roche Inc.

F. Hoffmann-la Roche Ag

Pius Waldmeier

Philippe Pflieger

Daniel Hunziker

Ulrike Obst Sander

Yi Ren

Werner Mueller

Roumen Nikolaev Radinov

Hendrik Moorlag

Corey James Brumsted

Andrew William Thomas

Fabienne Hoffmann-Emery

Steven Paul Hanlon

Chrisitan Lerner

Hans Hilpert

Mark Rogers-Evans

Roland Jakob-Roetne

Bernd Buettelmann

Stephan Roever

Michelangelo Scalone

Paul Hebeisen

Matthew C Lucas

Torsten Hoffmann

Hans Iding

Matthew Wright

Kurt Puentener

Urs Schwitter

Ulrich Widmer

Christian D Lerner

Paul Spurr

Yvo Crameri

Stefan Hildbrand

Shaoning Wang

Stephen Deems Gabriel

Christophe Pfleger

Constantinos G Panousis

Helmut Werner Stahr

Pascal Dott

René Trussardi

Goesta Rimmler

Sonja Nick

Christian Lerner

According to the present invention there are provided novel processes for the manufacture of the compound of formula 1 as well as intermediates and novel synthesis routes for key intermediates used in those processes.

Processes for the manufacture of propane-1-sulfonic acid (3-[5-(4-chloro-phenyl)-1H-pyrrolo[2,3-b]pyridine-3-carbonyl]-2,4-difluoro-phenyl)-amide

Processes for the manufacture of propane-1-sulfonic acid {3-[5-(4-chloro-phenyl)-1H-pyrrolo[2,3-b]pyridine-3-carbonyl]-2,4-difluoro-phenyl}-amide

Processes for the manufacture of propane-1-sulfonic acid {3-[5-(4-chloro-phenyl)-1 H-pyrrolo[2,3-b]pyridine-3-carbonyl]-2,4-difluoro-phenyl}-amide

The present invention relates to a process for the preparation of a compound of formula (I) wherein Rand Rare as defined herein, which is useful as an intermediate in the preparation of active pharmaceutical compounds.

Process for the preparation of isoxazolyl-methoxy nicotinic acids

The present invention relates to compounds of formula I wherein Rto R, R, Rand Rare as defined in the description and claims and Rsignifies a bicyclic heteroaryl group or a cyanophenyl group, as well as pharmaceutically acceptable salts thereof. The compounds are glucocorticoid receptor antagonists useful for the treatment and/or prevention of diseases such as diabetes, dyslipidemia, obesity, hypertension, cardiovascular diseases, adrenal imbalance or depression.

2,3-diaryl- or heteroaryl-substituted 1,1,1-trifluoro-2-hydroxypropyl compounds

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 compounds of formula I wherein R.sup.1a to R.sup.1e and R.sup.2 to R.sup.5 are as defined in the description and claims, and pharmaceutically acceptable salts thereof. The compounds are glucocorticoid receptor antagonists useful for the treatment and/or prevention of diseases such as diabetes, dyslipidemia, obesity, hypertension, cardiovascular diseases, adrenal imbalance or depression.

Substituted benzene compounds as modulators of the glucocorticoid receptor

The present invention relates to compounds formula I: and pharmaceutically acceptable salts thereof, wherein Rto Rare as defined in the description and claims for use as HDL-cholesterol raising agents in the treatment and/or prophylaxis of diseases or disorders that can be treated with such agents such as dyslipidemia.

2-trifluoromethylnicotinamide derivatives as HDL-cholesterol raising agents

The present invention relates to a process for preparation of a compound of formula I wherein

Synthesis of GlyT-1 inhibitors

The invention relates to the preparation of enantiomerically pure (S)-1,1,1-trifluoro-2-propanol by asymmetric hydrogenation of 1,1,1-trifluoroacetone which process comprises hydrogenating 1,1,1-trifluoroacetone in the presence of a ruthenium phosphine complex catalyst represented by formulaRu(E)(E')(L)(A)

Asymmetric hydrogenation of 1,1,1-trifluoroacetone

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 the preparation of ethanesul fonyl-piperidine derivatives

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

Process for the preparation of pyridine derivatives

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Wegenstetten, Switzerland

Pius Waldmeier