Hoffmann-la Roche Inc.

Remynd Nv

F. Hoffmann-la Roche Ag

Walter Vifian

Hasane Ratni

Matthias Heinrich Nettekoven

Henner Knust

Claus Riemer

Bjoern Bartels

Mark Rogers-Evans

Thomas Johannes Woltering

Wolfgang Haap

Wolfgang Guba

Ulrike Obst Sander

Cosimo Dolente

Gerard Griffioen

Katrien Princen

Anja Limberg

Michael Reutlinger

Giuseppe Cecere

Andreas Koblet

Xinlan Aloise Ford Cook

Michael Patrick Dillon

Jens-Uwe Peters

Jean-Marc Plancher

Caterina Bissantz

Bo Han

Christophe Grundschober

Xihan Wu

Andreas Kuglstatter

Philipp Cueni

Joanie Marie Caroon

Nadine Grether

Virginie Brom

Thomas Woltering

Delphine Gaufreteau

Claudio Zambaldo

Matilde Piras

Fionn Susannah O'hara

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 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 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.

The present invention relates to a compound of formula (IA), wherein Gis lower alkyl; lower alkyl substituted by one or more halogens; cycloalkyl; tetrahydropyran-4-yl; phenethyl; phenethyl substituted by one or more halogens; phenoxymethyl; phenoxymethyl substituted by one or more halogens; benzyloxyethyl; benzyloxy-ethyl substituted by one or more halogens; or is &#x2014;NRR; Ris hydrogen or lower alkyl; Ris lower alkyl; tetrahydropyran-4-yl; &#x2014;CH-cycloalkyl; or cycloalkyl optionally substituted by lower alkyl substituted by one or more halogens; or Rand Rform together with the N-atom to which they are attached a heterocycloalkyl group with 4 or 5 carbon atoms, which is optionally substituted by one or more substituents selected from halogen; or lower alkyl substituted by one or more halogens; X is &#x2014;CH&#x2014; or &#x2014;(CH)&#x2014;; Ar is phenyl or pyridinyl; Ris halogen; lower alkyl; lower alkyl substituted by one or more halogens; or lower alkoxy; n is 1 or 2; or to a pharmaceutically active salt thereof, to a stereoisomeric form, including an individual diastereoisomer or enantiomer of the compound of formula (IA) as well as to a racemic or non-racemic mixture thereof. The present invention also relates to the use of a compound of formula (IA) for treating certain neurodegenerative disorders characterized by cytotoxic TAU misfolding and/or aggregation. 

Piperazine thiazole derivatives useful in the treatment of tauopathies such as Alzheimer's disease

The invention relates to the use of a compound of formula I wherein

Oxytocin receptor agonists for the treatment of CNS diseases

The present application relates to compounds of formula wherein R, R, R, R, and n are defined hereinor to a pharmaceutically active salt thereof. The present compounds are high potential NK-3 receptor antagonists for the treatment of depression, pain, psychosis, Parkinson's disease, schizophrenia, anxiety and attention deficit hyperactivity disorder (ADHD).

Pyrrolidine compounds

The present invention relates to compounds of formula wherein R, R, R, R, Z, and n are as defined hereinor to a pharmaceutically active salt thereof. Compounds of the invention are high potential NK-3 receptor antagonists for the treatment of depression, pain, psychosis, Parkinson's disease, schizophrenia, anxiety and attention deficit hyperactivity disorder (ADHD).

Pyrrolidine derivatives

The present invention relates to a compound of formula (IA), wherein Gis lower alkyl; lower alkyl substituted by one or more halogens; cycloalkyl; tetrahydropyran-4-yl; phenethyl; phenethyl substituted by one or more halogens; phenoxymethyl; phenoxymethyl substituted by one or more halogens; benzyloxyethyl; benzyloxy-ethyl substituted by one or more halogens; or is &#x2014;NRR; Ris hydrogen or lower alkyl; Ris lower alkyl; tetrahydropyran-4-yl; &#x2014;CH-cycloalkyl; or cycloalkyl optionally substituted by lower alkyl substituted by one or more halogens; or Rand Rform together with the N-atom to which they are attached a heterocycloalkyl group with 4 or 5 carbon atoms, which is optionally substituted by one or more substituents selected from halogen; or lower alkyl substituted by one or more halogens; X is &#x2014;CH&#x2014;or &#x2014;(CH)&#x2014;; Ar is phenyl or pyridinyl; Ris halogen; lower alkyl; lower alkyl substituted by one or more halogens; or lower alkoxy; n is 1 or 2; or to a pharmaceutically active salt thereof, to a stereoisomeric form, including an individual diastereoisomer or enantiomer of the compound of formula (IA) as well as to a racemic or non-racemic mixture thereof. The present invention also relates to the use of a compound of formula (IA) for treating certain neurodegenerative disorders characterized by cytotoxic TAU misfolding and/or aggregation. 

Piperazine thiazole derivatives useful in the treatment of tauopathies such as alzheimer's disease

The present invention relates to a compound of formula (IA) The present invention also relates to the use of the compound of formula IA for treating certain neurodegenerative disorders characterized by cytotoxic TAU misfolding and/or aggregation. 

1, 2, 4-thiadiazol-5-ylpiperazine derivatives useful in the treatment of neurodegenerative diseases

The invention provides compounds of formula wherein R, R, R, R, R, and Rare as defined hereinor a pharmaceutically suitable acid addition salt thereof. The present compounds are high potential NK-3 receptor antagonists useful for the treatment of depression, pain, psychosis, Parkinson's disease, schizophrenia, anxiety and attention deficit hyperactivity disorder (ADHD).

The invention relates to a compound of formula wherein A is defined herein or to pharmaceutically active salts, stereoisomeric forms, including individual diastereoisomers and enantiomers of the compound of formula I as well as racemic and non-racemic mixtures thereof. The present compounds are high potential NK-3 receptor antagonists for the treatment of depression, pain, psychosis, Parkinson's disease, schizophrenia, anxiety and attention deficit hyperactivity disorder (ADHD).

Methyl-pyrrolidine ether derivatives

The present application relates to compounds of formula wherein the definitions are as described herein. The present compounds are high potential NK-3 receptor antagonists that are useful for the treatment of depression, pain, psychosis, Parkinson's disease, schizophrenia, anxiety and attention deficit hyperactivity disorder (ADHD).

Piperidine derivatives as NK3 receptor antagonists

The present invention relates to a compounds of formula I 

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Gelterkinden, Switzerland

Walter Vifian