Hoffmann-la Roche Inc.

F. Hoffmann-la Roche Ag

Anja Limberg

Hasane Ratni

Werner Neidhart

Roland Jakob-Roetne

Claus Riemer

Ulrike Reiff

Frank Herting

Henner Knust

Georg Fertig

Bjoern Bartels

Manfred Kubbies

Matthias Heinrich Nettekoven

Michael Weidner

Michael Reutlinger

Matthias Koerner

Karlheinz Baumann

Sabine Kolczewski

Theodor Stoll

Ulrich Tibes

Philippe Jablonski

Hans Hilpert

Guido Galley

Thomas Luebbers

Rosa Maria Rodriguez Sarmiento

Klaus-Peter Kuenkele

Kenichi Kawasaki

Greta Vastakaite

Synese Jolidon

Andrew William Thomas

Luke Green

Erwin Goetschi

Gerd Zimmermann

Petra Rueger

Walter Vifian

Matthias Rueth

Xihan Wu

Sandra Steiner

Daniela Brunner

Eric Prinssen

Bernhard Goller

Ulrike Leser-Reiff

Jérôme Charles Sarie

Bavani G Shankar

Jessica Malberg

Rainer Haag

Georg Jaeschke

Guy Georges

Alexander Flohr

Caterina Bissantz

Olaf Mundigl

Hans-Willi Krell

Annick Goergler

Rosa Maria Rodriguez-Sarmiento

Adelbert Grossmann

Andreas Koblet

Christian Schnider

Daniela Krummenacher

Stefan Berchtold

Aude Lemarchand

Björn Bartels

Georges Guy

Roland Jakob-roetne

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 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 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 present invention relates to compounds of formula  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 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.

The present invention is concerned with indolin-2-one and 1,3-dihydro-pyrrolo[3,2-c]pyridin-2-one derivatives of general formula I wherein Ar, A, R, R, R, X and n are as described herein and pharmaceutically acceptable salts thereof for treatment of central nervous system disorders 

Indolin-2-one and 1,3-dihydro-pyrrolo[3,2-c]pyridin-2-one derivatives

The present invention is concerned with 2-oxo-2,3-dihydro-indoles of general formula (I) wherein Ar, X, X, R, R, R, m, n and the dotted line are as defined herein which compounds are useful for treating certain central nervous system disorders as described herein.

Indolin-2-one or pyrrolo-pyridin/pyrimidin-2-one derivatives

The present invention is concerned with 2-oxo-2,3-dihydro-indoles of general formula wherein is phenyl or a heteroaryl group, selected from pyridinyl, pyrimidinyl, imidazolyl, isoxazolyl or pyrazolyl; is phenyl or pyridinyl, wherein the N atom in the pyridinyl group may be on all free positions;

2-oxo-2,3-dihydro-indoles for the treatment of CNS disorders

The present invention relates to compounds of formula I hetaryl I, hetaryl II, R, R, R, Y,m, and o or to pharmaceutically active acid addition salts thereof. The present compounds of formula I are modulators for amyloid beta and thus, they may be useful for the treatment or prevention of a disease associated with the deposition of &#x3b2;-amyloid in the brain, in particular Alzheimer's disease, and other diseases such as cerebral amyloid angiopathy, hereditary cerebral hemorrhage with amyloidosis, Dutch-type (HCHWA-D), multi-infarct dementia, dementia pugilistica and Down syndrome.

The invention relates to compounds of formula where hetaryl I, hetaryl II,

Heteroaryl substituted piperidines

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Basel, Switzerland

Anja Limberg