Hoffmann-la Roche Inc.

F. Hoffmann-la Roche Ag

Michael Reutlinger

Hasane Ratni

Bjoern Bartels

Peter Mohr

Hans Peter Maerki

Benoit Hornsperger

Werner Neidhart

Roland Jakob-Roetne

Anja Limberg

Roberto Iacone

Markus Rudolph

Greta Vastakaite

Walter Vifian

Jérôme Charles Sarie

Xinlan Aloise Ford Cook

Bernd Kuhn

Guido Galley

Luca Claudio Gobbi

Eric Argirios Kitas

Rosa Maria Rodriguez Sarmiento

Cosimo Dolente

Sandra Steiner

Annick Goergler

Giuseppe Cecere

Andreas Koblet

Valerie Runtz-Schmitt

Maria-Clemencia Hernandez

Christian Schnider

Daniela Krummenacher

Andres Miguel Olivares Morales

Nicolas Zorn

Jaclyn Ivy Wamsteeker Cusulin

Eoin Cornelius O'Connor

Frédéric Knoflach

Stefan Berchtold

Eoin Cornelius O`CONNOR

Virginie Brom

Roland Jakob-roetne

Delphine Gaufreteau

Claudio Zambaldo

Matilde Piras

Fionn Susannah O'hara

Compounds having the general formula (I) wherein R, R, R, R, Rand X are as described herein, compositions including the compounds and methods of using the compounds.

Substituted benzo[f][1,2,4]triazolo[4,3-a][1,4]diazepines as GABA A GAMMA1 positive allosteric modulators

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

The invention provides novel compounds having the general formula (I) wherein R, R, R, R, R, R, R, R, R, R, Rand Rare as described herein, compositions including the compounds and methods of using the compounds.

Difluoroketamide derivatives as HtrA1 inhibitors

The invention provides novel compounds having the general formula (I) wherein R, R, R, R, R, R, R, R, R, Rand Rare as described herein, compositions including the compounds and methods of using the compounds.

Trifluoromethylpropanamide derivatives as HTRA1 inhibitors

The invention provides novel compounds having the general formula (I) wherein R, R, R, R, R, R, R, R, A, X and Rare as described herein, compositions including the compounds and methods of using the compounds.

Difluoroketamide derivatives as HTRA1 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 invention provides novel compounds having the general formula (I) wherein R, R, R, R, R, R, R, X, A and Rare as described herein, compositions including the compounds and methods of using the compounds.

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.

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; and Rmay be different if n is 2 or 3; Ris hydrogen, lower alkyl, lower alkyl substituted by halogen, halogen, CN, lower alkoxy or lower alkoxy substituted by halogen; X is CH or N; m is 1, 2 or 3; -( )is &#x2014;(CH)&#x2014;; n is 1, 2 or 3; Ar is a five membered heteroaryl group, selected from formula (A), (B), (C), (D), (E) or (F), wherein Ris hydrogen, methyl or chloro; Ris hydrogen or methyl; Ris F, Cl, CHFor CF; 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-infarct dementia, dementia pugilistica or Down syndrome. 

The invention provides novel compounds having the general formula (I) wherein R, R, R, R, R, R, R, Rand Rare as described herein, compositions including the compounds and methods of using the compounds.

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Basel, Switzerland

Michael Reutlinger