Hoffmann-la Roche Inc.

Siena Biotech S.p.a.

Other

Basilea Pharmaceutica Ag

F. Hoffmann-la Roche Ag

Roland Humm

Hans Hilpert

Thomas Johannes Woltering

Thorsten Muser

Mark Rogers-Evans

Alexander Mayweg

David Banner

Harald Mauser

Bernd Kuhn

Sabine Kolczewski

Jean-Marc Plancher

Wolfgang Wostl

Wolfgang Guba

Robert Narquizian

Hans Iding

Fabienne Ricklin

Theodor Stoll

Christian Schnider

Delphine Gaufreteau

Dietmar Knopp

Emmanuel Pinard

Peter Mohr

Uwe Grether

Luca Claudio Gobbi

Katrin Groebke Zbinden

Wolfgang Haap

Paul Hebeisen

Alfred Binggeli

Benoit Hornsperger

Beat Wirz

Hans-Peter Maerki

Bjoern Bartels

Narendra Panday

Christian D Lerner

Markus Boehringer

Markus Meyer

Jacques Himber

Giuseppe Cecere

Christoph Martin Stahl

Valerie Runtz-Schmitt

Didier Rombach

Maria-Clemencia Hernandez

Peter Weiss

Roger Wermuth

Eoin Power

Emanuele Gabellieri

Angélique Patiny-Adam

Bernd Brodbeck

Andrés Miguel Olivares Morales

Lukas Kreis

Alexander V Mayweg

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 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 is concerned with indolin-2-one derivatives of general formula wherein   The compounds may be used in the treatment of CNS diseases related to positive (psychosis) and negative symptoms of schizophrenia, substance abuse, alcohol and drug addiction, obsessive-compulsive disorders, cognitive impairment, bipolar disorders, mood disorders, major depression, treatment resistant depression, anxiety disorders, Alzheimer's disease, autism, Parkinson's disease, chronic pain, borderline personality disorder, neurodegenerative disease, sleep disturbances, chronic fatigue syndrome, stiffness, inflammatory disease, asthma, Huntington's disease, ADHD, amyotrophic lateral sclerosis, effects in arthritis, autoimmune disease, viral and fungal infections, cardiovascular diseases, ophthalmology and inflammatory retinal diseases and balance problems, epilepsy and neurodevelopmental disorders with co morbid epilepsy.

Indolin-2-one derivatives

The present invention is concerned with indolin-2-one derivatives of general formula    The compounds may be used in the treatment of CNS diseases related to positive (psychosis) and negative symptoms of schizophrenia, substance abuse, alcohol and drug addiction, obsessive-compulsive disorders, cognitive impairment, bipolar disorders, mood disorders, major depression, treatment resistant depression, anxiety disorders, Alzheimer's disease, autism, Parkinson's disease, chronic pain, borderline personality disorder, neurodegenerative disease, sleep disturbances, chronic fatigue syndrome, stiffness, inflammatory disease, asthma, Huntington's disease, ADHD, amyotrophic lateral sclerosis, effects in arthritis, autoimmune disease, viral and fungal infections, cardiovascular diseases, ophthalmology and inflammatory retinal diseases and balance problems, epilepsy and neurodevelopmental disorders with co-morbid epilepsy.

The present invention relates to compounds having the general formula (Ia) or (Ib), optionally in the form of a pharmaceutically acceptable salt, solvate, polymorph, codrug, cocrystal, prodrug, tautomer, racemate, enantiomer, or diastereomer or mixture thereof, which are useful in treating, ameloriating or preventing a viral disease, in particular influenza.

Pyrimidone derivatives and their use in the treatment, amelioration or prevention of a viral disease

Provided herein is a compound of formula I: as wells as a pharmaceutical composition, a process of making and a method of using a compound of formula I. The compounds of formula I are BACE1 inhibitors useful for the treatement of, for example, Alzheimer's Disease.

Fluoromethyl-5,6-dihydro-4H-[1,3]OXAZINES

This invention relates to compounds of the formula wherein Rto Rare as described below, or to pharmaceutically acceptable salts thereof. These compounds are BACE2 inhibitors and can be used as medicaments for the therapeutic and/or prophylactic treatment of diseases such as diabetes, particularly type 2 diabetes, and other metabolic disorders.

1,4,5,6-tetrahydro-pyrimidin-2-ylamine compounds

This invention relates to compounds of the formula wherein A, B and Rto Rare as described below, or to pharmaceutically acceptable salts thereof. These compounds are BACE1 and/or BACE2 inhibitors and can be used as medicaments for the therapeutic and/or prophylactic treatment of diseases such as Alzheimer's disease, diabetes, particularly type 2 diabetes, and other metabolic disorders.

2,5,6,7-tetrahydro-[1,4]oxazepin-3-ylamine or 2,3,6,7-tetrahydro-[1,4]oxazepin-5-ylamine compounds

This invention relates to dihydropyrimidinones of the formula wherein X and Rto Rare as defined in the description, as well as pharmaceutically acceptable salts thereof. These compounds are BACE2 inhibitors and can be used as medicaments for the treatment or prevention of diseases such as diabetes.

Dihydropyrimidinones

The present invention relates to N-[3-(5-Amino-3,3a,7,7a-tetrahydro-1H-2,4-dioxa-6-aza-inden-7-yl)-phenyl]-amides of formula I having BACE1 and/or BACE2 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 and type 2 diabetes.

N-[3-(5-amino-3,3a,7,7a-tetrahydro-1H-2,4-dioxa-6-aza-inden-7-yl)-phenyl]-amides as BACE1 and/or BACE2 inhibitors

The invention is concerned with novel dicarboxamide derivatives of formula (I) wherein A, B, R, D and E are as defined in the description and in the claims, as well as physiologically acceptable salts thereof. These compounds inhibit the coagulation factor Xa and can be used as medicaments.

Dicarboxamide derivatives

The present invention relates to phosphinic acid derivatives of formula I wherein R, R, Rand Rare described hereinabove. These compounds can be used in the treatment or prevention of a disease related to the inhibition of &#x3b2;-secretase, inter alia for the treatment of Alzheimer's disease.

Phosphinic acids

Compounds of formula I are providedas well as pharmaceutically acceptable salts and esters thereof, wherein Rto R, A, Aand n have the significance indicated in the specification.

Indolyl derivatives

Oxazole derivatives

Process for the preparation of vinyl-pyrrolidinone cephalosporin derivatives

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Auggen, Germany

Roland Humm