Hoffmann-la Roche Inc.

Hoffmann-le Roche Inc.

F. Hoffmann-la Roche Ag

Bjoern Bartels

Thomas Johannes Woltering

Wolfgang Guba

Ulrike Obst Sander

Cosimo Dolente

Wolfgang Haap

Hasane Ratni

Jens-Uwe Peters

Werner Neidhart

Roland Jakob-Roetne

Anja Limberg

Michael Reutlinger

Mark Rogers-Evans

Walter Vifian

Christian Schnider

Andreas Kuglstatter

Guido Galley

Roger Wermuth

Philipp Cueni

Greta Vastakaite

Luca Claudio Gobbi

Matthias Koerner

Rosa Maria Rodriguez Sarmiento

Giuseppe Cecere

Valerie Runtz-Schmitt

Sandra Steiner

Angélique Patiny-Adam

Fritz Bliss

Jérôme Charles Sarie

Andrés Miguel Olivares Morales

Georg Jaeschke

Alexander Flohr

Katrin Groebke Zbinden

Annick Goergler

Kurt Puentener

Rosa Maria Rodriguez-Sarmiento

Urs Schwitter

Roland Humm

Ulrich Zutter

Jean-Michel Adam

Fabienne Hoffmann-Emery

Olaf Grassmann

Maria-Clemencia Hernandez

Xinlan Aloise Ford Cook

Andreas Koblet

Didier Rombach

Christophe Pfleger

Shaoning Wang

Ralph Diodone

Dieter Muri

Karlheinz Baumann

Serena Maria Fantasia

Lilli Anselm

Daniela Krummenacher

Thomas Hartung

René Trussardi

Benno Rothenhaeusler

Frederic Ran

Stefan Berchtold

Haap Wolfgang

The invention provides novel heterocyclic compounds having the general formula (I), and pharmaceutically acceptable salts thereof, wherein the variables are as described herein. Further provided are pharmaceutical compositions including the compounds, processes of manufacturing the compounds and methods of using the compounds as medicaments, in particular methods of using the compounds for the treatment or prevention of acute neurological disorders, chronic neurological disorders and/or cognitive disorders.

Benzodiazepine derivatives as GABA A gamma 1 PAM

The invention provides novel heterocyclic compounds having the general formula (I) or (II), and pharmaceutically acceptable salts thereof, wherein the variables are as described herein. Further provided are pharmaceutical compositions including the compounds, processes of manufacturing the compounds and methods of using the compounds as medicaments, in particular methods of using the compounds for the treatment or prevention of acute neurological disorders, chronic neurological disorders and/or cognitive disorders.

Benzodiazepine derivatives as GABA a GAMMA1 PAM

The present invention relates to compounds of formula (I), wherein R is hydrogen or halogen, wherein R may be different if n=2 or 3; n is 1, 2 or 3; (II) is a disubstituted bicyclo[1,1,1]pentane or bicyclo[2,2,2]octane as defined below: (III) or (IV); or to a pharmaceutically active acid addition salt thereof, to a racemic mixture or to its corresponding enantiomer and/or an optical isomer and/or stereoisomer thereof. The compounds may be used for the treatment of Alzheimer's disease, cerebral amyloid angiopathy, hereditary cerebral hemorrhage with amyloidosis, Dutch-type (HCHWA-D), multi-infarct dementia, dementia pugilistica or Down syndrome. 

Triazolo-azepine derivatives

The invention provides new pyrimidine compounds having the general formula (I), wherein R, R, R, n, and X are as described herein, compositions including the compounds, processes of manufacturing the compounds and methods of using the compounds. 

Pyrimidine derivatives

The present invention relates to a compound of formula I, HetAr is a five or six membered heteroaryl group, selected from wherein Ris hydrogen, halogen, lower alkyl, lower alkoxy or lower alkyl substituted by halogen, and may be the same or different, if two Roccur; Ris lower alkyl or a mono- or polydeutered derivative thereof, lower alkyl substituted by halogen or lower alkoxy, lower alkenyl unsubstituted or substituted by halogen, cycloalkyl or CH-cycloalkyl unsubstituted or substituted by halogen, heterocycloalkyl or CH-heterocycloalkyl unsubstituted or substituted by lower alkyl; Ris halogen, lower alkyl, lower alkyl substituted by halogen, lower alkoxy substituted by halogen or S(O)-lower alkyl; n is 1, 2 or 3; if n is &#x3e;1, then Rmay be the same or different; or to a pharmaceutically active acid addition salt thereof, to a racemic mixture or to its corresponding enantiomer and/or an optical isomer and/or stereoisomer thereof. The compounds may be used for the treatment of Alzheimer's disease, cerebral amyloid angiopathy, hereditary cerebral hemorrhage with amyloidosis, Dutch-type (HCHWA-D), multi-infarct dementia, dementia pugilistica or Down syndrome. 

Phenoxytriazoles

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 to a compound of formula I, 1-1 or 1-2 wherein Ris hydrogen, lower alkyl, lower alkyl substituted by halogen, halogen, lower alkoxy, or lower alkoxy substituted by halogen; Rmay be different if n=2 or 3 n is 1, 2 or 3 Ar is a six membered heteroaryl group, selected from wherein Ris hydrogen, lower alkyl, lower alkyl substituted by halogen, halogen or lower alkoxy; Ris hydrogen or halogen; or to a pharmaceutically active acid addition salt thereof. The compounds may be used for the treatment of Alzheimer's disease, cerebral amyloid angiopathy, hereditary cerebral hemorrhage with amyloidosis, Dutch-type (HCHWA-D), multi-infarct dementia, dementia pugilistica or Down syndrome. 

Bicyclic heteroaryl derivatives

The present invention relates to a compound of formula (I), wherein Ris hydrogen, lower alkyl, lower alkyl substituted by halogen, halogen, lower alkoxy or lower alkoxy substituted by halogen; R may be the same or different, if n=2 or 3; n is 1, 2 or 3; m is 1, 2 or 3; Ar is a five or six membered heteroaryl group, selected from (II), (III), (IV) or (V) wherein Ris hydrogen, lower alkyl, lower alkyl substituted by halogen, halogen or lower alkoxy; Ris hydrogen or halogen; -( ) m-is &#x2014;(CH)&#x2014; or to pharmaceutically active acid addition salts thereof. The compounds may be used for the treatment of Alzheimer's disease, cerebral amyloid angiopathy, hereditary cerebral hemorrhage with amyloidosis, Dutch-type (HCHWA-D), multi-in-farct dementia, dementia pugilistica or Down syndrome. 

Bridged piperidine derivatives

The present invention relates to compounds of formula  

Triazolopyridines

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.

Pyridyl-triazabicycles

The present invention relates to a compound of formula I wherein  The compounds may be used for the treatment of Alzheimer's disease, cerebral amyloid angiopathy, hereditary cerebral hemorrhage with amyloidosis, Dutch-type (HCHWA-D), multi-infarct dementia, dementia pugilistica or Down syndrome.

Fused pyrimidine derivatives

The present invention relates to compounds of formula I,   The compounds may be used for the treatment of Alzheimer's disease, cerebral amyloid angiopathy, hereditary cerebral hemorrhage with amyloidosis, Dutch-type (HCHWA-D), multi-infarct dementia, dementia pugilistica or Down syndrome.

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Schopfheim, Germany

Bjoern Bartels