Hoffmann-la Roche Inc.

F. Hoffmann-la Roche Ag

Philipp Cueni

Bjoern Bartels

Mark Rogers-Evans

Thomas Johannes Woltering

Jens-Uwe Peters

Wolfgang Haap

Wolfgang Guba

Ulrike Obst Sander

Matthias Koerner

Cosimo Dolente

Walter Vifian

Ulrich Zutter

Christophe Pfleger

Dieter Muri

Andreas Kuglstatter

Fritz Bliss

A process for preparing the compound of formula I comprising:a) coupling a compound of formula 2 wherein a leaving group O&#x2014;SO&#x2014;R is selected from the triflate group, the tosylate group, the mesylate group, the besylate group, the nosylate group or the brosylate group,with a suitable boronic acid, a trifluoroborate or a boronic acid esterunder argon condition and in the presence of a catalyst and a base in a suitable solvent and then isolating the product as an acid addition saltto afford the compound of formula Ia andb) converting the acid addition salt of formula Iawherein the acid HX comprises suitable organic or inorganic acids into the compound of formula I by treatment with at least a stoichiometric equivalent of a suitable base.

Process for preparation of 2-(6-nitropyridin-3-yl)-9H-dipyrido[2,3-b;3',4&#x2032;-d]pyrrole

The present invention provides a compound of formula I, having BACE1 inhibitory activity, their manufacture, pharmaceutical compositions containing them and their use as therapeutically active substances. The active compounds of the present invention are useful in the therapeutic and/or prophylactic treatment of e.g. Alzheimer's disease.

BACE1 inhibitors

The present invention relates in part to a process for the preparation of a proline derivative of formula I wherein,  The proline derivatives of the formula I are preferential inhibitors of the cysteine protease Cathepsin S and are therefore useful to treat metabolic diseases like diabetes, atherosclerosis, abdominal aortic aneurysm, peripheral arterial disease and diabetic nephropathy.

Process for the preparation of proline derivatives

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Basel, Switzerland

Philipp Cueni