Hoffmann-la Roche Inc.

Remynd Nv

F. Hoffmann-la Roche Ag

Giuseppe Cecere

Guido Galley

Roger David Norcross

Philippe Pflieger

Maria-Clemencia Hernandez

Andreas Koblet

Valerie Runtz-Schmitt

Luca Claudio Gobbi

Hong Shen

Yimin Hu

Angélique Patiny-Adam

Matthias Heinrich Nettekoven

Emmanuel Pinard

Hasane Ratni

Mark Rogers-Evans

Henner Knust

Katrin Groebke Zbinden

Bjoern Bartels

Walter Vifian

Gerard Griffioen

Katrien Princen

Angelique Patiny-Adam

Andres Miguel Olivares Morales

Andrés Miguel Olivares Morales

Andrew William Thomas

Bernd Buettelmann

Annick Goergler

Michael Reutlinger

Roland Humm

Bernhard Fasching

Sandra Steiner

Christian Schnider

Philipp Schmid

Nicolas Zorn

Frédéric Knoflach

Jaclyn Ivy Wamsteeker Cusulin

Eoin Cornelius O'Connor

Alina Tirla

Etienne Rauber

Roger Norcross

Guillaume DÉCORET

Eoin Cornelius O`CONNOR

Jaclyn Wamsteeker Cusulin

The invention provides novel heterocyclic compounds having the general formula (I), and pharmaceutically acceptable salts thereof, wherein the variables are as described herein. Further provided are pharmaceutical compositions including the compounds, processes of manufacturing the compounds and methods of using the compounds as medicaments, in particular methods of using the compounds for the treatment or prevention of acute neurological disorders, chronic neurological disorders and/or cognitive disorders.

Benzodiazepine derivatives as GABA A gamma 1 PAM

The invention provides novel heterocyclic compounds having the general formula (I) or (II), and pharmaceutically acceptable salts thereof, wherein the variables are as described herein. Further provided are pharmaceutical compositions including the compounds, processes of manufacturing the compounds and methods of using the compounds as medicaments, in particular methods of using the compounds for the treatment or prevention of acute neurological disorders, chronic neurological disorders and/or cognitive disorders.

Benzodiazepine derivatives as GABA a GAMMA1 PAM

The invention provides novel compounds having the general formula (I) or (II) wherein R, R, R, R, W, Y and Z are as described herein, compositions including the compounds and methods of using the compounds.

Isoxazolyl ether derivatives as GABA&#x3b1;5 PAM

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

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

The present invention relates to compounds of formula of formula I wherein R, R, Rand L are as described herein, compositions containing compounds of formula I, methods of manufacture of compounds of formula I and methods of treating psychiatric, metabolic, cardiovascular or sleep disorders with compounds of formula I. 

Substituted pyrazino[2,2-a]isoquinoline derivatives

The present invention relates to compounds of formula of formula I wherein R, R. R, R, R, R, R, L, Land N are as described herein, compositions containing compounds of formula I, methods of manufacture of compounds of formula I and methods of treating psychiatric, metabolic, cardiovascular or sleep disorders with compounds of formula I. 

Substituted azetidine derivatives

The present invention relates to compounds TAAR receptor antagonists of formula I wherein X, R, L, Ar and Rare as described herein, compositions containing compounds of formula I, methods of manufacture of compounds of formula I and methods of treating psychiatric disorders with compounds of formula I. 

6-amino-5,6,7,8-tetrahydronaphthalen-2-yl or 3-aminochroman-7-yl derivatives

The present invention relates to compounds of formula of formula I wherein X, R, L, Ar, Rand n are as described herein, compositions containing compounds of formula I, methods of manufacture of compounds of formula I and methods of treating psychiatric disorders with compounds of formula I. 

Morpholin-pyridine 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 compounds of formula of formula I wherein X, L and Rare as described herein, compositions containing compounds of formula I, methods of manufacture of compounds of formula I and methods of treating psychiatric, metabolic, cardiovascular or sleep disorders with compounds of formula I. 

2-oxa-5-azabicyclo[2.2.1]heptan-3-yl derivatives

The present invention relates to compounds of formula of formula I wherein X, Ar, R, m and n are as described herein, compositions containing compounds of formula I, methods of manufacture of compounds of formula I and methods of treating psychiatric disorders with compounds of formula I. 

5-oxa-2-azabicyclo[2.2.2]OCTAN-4-yl and 5-oxa-2-azabicyclo[2.2.1]heptan-4-yl 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

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Basel, Switzerland

Giuseppe Cecere