Hoffmann-la Roche Inc.

Dainippon Sumitomo Pharma Co., Ltd.

F. Hoffmann-la Roche Ag

Erwin Goetschi

Thomas Johannes Woltering

Juergen Wichmann

Geo Adam

Silvia Gatti McArthur

Vincent Mutel

Synese Jolidon

Alexander Alanine

Thomas Luebbers

Wylie Solang Palmer

Karlheinz Baumann

Alexander Flohr

Silvia Gatti Mcarthur

Hasane Ratni

Mark Rogers-Evans

Patrick Schnider

Caterina Bissantz

Raffaello Masciadri

Anja Limberg

Helmut Jacobsen

Emmanuel Pinard

Roland Jakob-Roetne

Henner Knust

Andrew William Thomas

Luke Green

Masanori Itoh

Makoto Sunagawa

Christophe Grundschober

Theresa Maria Ballard

Katsumi Kubota

Jürgen Wichmann

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 present invention is concerned with spiro-dihydrotetraazabenzoazulenes, i.e. spiro-5,6-dihydro-4H-2,3,5,10b-tetraaza-benzo[e]azulenes of formula I wherein R, R, R, X, Y, Z, m and n are as described herein. The compounds according to the invention act as V1a receptor modulators and are useful as therapeutics acting peripherally and centrally in the conditions of dysmenorrhea, male or female sexual dysfunction, hypertension, chronic heart failure, inappropriate secretion of vasopressin, liver cirrhosis, nephrotic syndrome, anxiety, depressive disorders, obsessive compulsive disorder, autistic spectrum disorders, schizophrenia, and aggressive behavior.

Spiro-5,6-dihydro-4H-2,3,5,10b-tetraaza-benzo[e]azulenes

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

Heteroaryl substituted piperidines

The invention relates to compounds of formula wherein R, R, R3, R4, and Ar are as defined in the specification and claims, or to pharmaceutically active acid addition salts of such compounds. Compounds of formula I are modulators for amyloid beta and 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 for amyloid beta

The present invention relates to compounds of formula (I) wherein A, E G, J, L, M, R, R, and Rare as defined in the specification and claims. The invention also relates to pharmaceutical compositions containing such compounds and methods for preparing the compounds and compositions. The compounds are metabotropic glutamate receptor antagonists and are useful for the treatment of a variety of CNS disorders.

Substituted pyrazolo [1,5-A] pyrimidines as metabotropic glutamate antagonists

The invention relates to methods for the treatment of Alzheimer's disease, cerebral amyloid angiopathy, hereditary cerebral hemorrhage with amyloidosis, Dutch-type (HCHWA-D), multi-infarct dementia, dementia pugilistica and Down syndrome which comprise administering a therapeutically effective amount of a compound of formula I whereinR, R, R, V, W, Y, and Z are as defined herein or a pharmaceutically active acid addition salt of such compounds. The invention also relates to a subgenus of such compounds and pharmaceutical compositions containing them, as well as methods for their manufacture.

Heterocyclic gamma secretase modulators

The present invention relates to compounds of formula (I), a process for the manufacture thereof, pharmaceutical compositions containing them, and their use for treating CNS disorders: wherein A, B, X, Y, R, R, Rand Rare as defined in the description and claims.

Pyridine derivatives as mGluR2 antagonists

Substituted pyrazolo [1,5-a] pyrimidines as metabotropic glutamate antagonists

The present invention relates to compounds of formula (I): wherein Rto R, A, M, L, E, G, and J are as defined in the description and claims. The invention also relates to a process for the manufacture of such compounds, pharmaceutical compositions containing them, and methods for treating CNS disorders.

Acetylenyl-pyrazolo-pyrimidine derivatives

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.

The present invention relates to compounds of formula (Ia), a process for the manufacture thereof, pharmaceutical compositions containing them, and their use for treating CNS disorders: wherein A, B, R, R, Rand Rare as defined in the description and claims.

Phenyl-substituted pyrimidine derivatives as mGluR antagonists

Compounds as metabotropic glutamate receptor antagonists

In particular, the present invention is concerned with compounds of the general formula (I) 

Spiropiperidine glycinamide derivatives

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Reinach, Switzerland

Erwin Goetschi