Hoffmann-la Roche Inc.

F. Hoffmann-la Roche Ag

Helmut Jacobsen

Synese Jolidon

Alexander Flohr

Thomas Luebbers

Karlheinz Baumann

Erwin Goetschi

Jens-Uwe Peters

Guido Galley

Eric Argirios Kitas

Annick Goergler

Laurence Mosbach-Ozmen

Peter Nelboeck-Hochstetter

The invention relates to compounds of formula wherein the substituents are as described in claim. 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.

Modulators of amyloid beta

The invention relates to compounds of formula wherein R, R, R, R, X and Y are as defined herein and to pharmaceutically active acid addition salts thereof. The compounds can 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.

Modulators for amyloid beta

The invention relates to compounds of formula wherein hetaryl I, hetaryl II, and Rare as described herein. 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.

The invention relates to malonamide derivatives of formula wherein each of the variables are as defined in the specification and to pharmaceutically acceptable acid addition salts thereof. The compounds are &#x3b3;-secretase inhibitors. Thus, the invention also relates to pharmaceutical compositions containing these compounds and to a method of treating Alzheimer's disease by administering the compounds of the invention.

Malonamide derivatives

The present invention relates to a novel animal model for amyloidopathies, especially Alzheimer' disease overexpressing human BACE and human APP London. This novel animal model exhibits several aspects of amyloidopathy. The present invention also relates to a method for producing the double transgenic animals, to cells and cell lines derived from these animals and to a kit comprising these cells. Moreover, a method for the evaluation of the in vivo effects of beta-secretase activity on A-beta peptide generation, amyloidosis, neurodegeneration and AD pathology in these animals is provided.

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Schopfheim, Germany

Helmut Jacobsen