Hoffmann-la Roche Inc.

Siena Biotech S.p.a.

Genentech, Inc.

Covagen Ag

F. Hoffmann-la Roche Ag

David Banner

Harald Mauser

Hans Hilpert

Jean Ackermann

Kurt Hilpert

Klaus Gubernator

Wolfgang Haap

Bernd Kuhn

Hans Peter Wessel

Gerard Schmid

Mark Rogers-Evans

Alexander Mayweg

Paul Hadvary

Beat Wirz

Thomas B Tschopp

Ludvik Labler

Jens-Uwe Peters

Thomas Luebbers

Thomas Johannes Woltering

Wolfgang Wostl

Wolfgang Guba

Robert Narquizian

Klaus Muller

G Erard Schmid

Uwe Grether

Jean-Marc Plancher

Holger Kuehne

Roland Humm

Lilli Anselm

Eoin Power

Beat Spinnler

Emmanuel Pinard

Simona Maria Ceccarelli

Guido Hartmann

Klaus M Uller

Luca Claudio Gobbi

Katrin Groebke Zbinden

Tanja Schulz-Gasch

Benoit Hornsperger

Fabienne Ricklin

Ulrike Obst

Dragan Grabulovski

Christoph Martin Stahl

Didier Rombach

Julian Bertschinger

Werner Lesslauer

Delphine Gaufreteau

Hansruedi Lotscher

Emanuele Gabellieri

Dietrich Stuber

Matteo Andreini

Massimiliano Travagli

Jean-Baptiste Blanc

Michael Hennig

Ruben Alvarez Sanchez

Rudolf E Minder

Simon Brack

Sarah Batey

Rubén Alvarez Sánchez

Daniel Schlatter

Jörg Benz

Michela Valacchi

Peter Hartman

Rubén Alvarez Sanchez

Alexander V Mayweg

The invention relates to a compound of formula (I) wherein A, Aand Rto Rare defined as in the description and in the claims. The compound of formula (I) can be used as a medicament.

Pyridine derivatives

The invention relates to a compound of formula (I) wherein A, B, D and Rto Rare defined as in the description and in the claims. The compound of formula (I) can be used as a medicament.

Cyclic amides

The present invention relates to a polypeptide binding to a chymase (EC 3.4.21.39), wherein the polypeptide comprises or consists of an amino acid sequence selected from the group consisting of: (a) GVTLFVALYDY(X)A(X)(X)(X)(X)(X)LSFHKGEKFQIL(X)(X)(X)(X) (X)(X)G(X)(X)WEARSLTTGETGYIPSNYVAPVDSIQ (SEQ ID NO: 1), wherein (X) is R, N, Q, E, K, H, S, T, C, or D; (X) is E, T, D, Q, L, P, A, S, C, M, N, E, G, A, V or I; (X) is R, T, H, N, K, S, C, N or Q; (X) is S, W, T, C, N, Q, F or Y; (X) is T, H, L, F, C, S, M, N, Q, R, K, G, A, V, I, P, Y or W; (X) is D, Q, H, E, S, T, C, N, R or K; (X) is D, N, R, E, Q, S, T, C, K or D; (X) is M, W, G, F, A, T, C, S, N, Q, Y, V, L, I or P; (X) is T, H, S, D, C, N, Q, R, K, E or absent; (X) is V, T, Q, G, A, L, I, P, S, C, M, N or absent; (X) is P, A, D, G, K, V, L, I, E, R, M, H or absent; (X) is N, V, P, I, E, T, S, A, G, L, C, M, Q or D; (X) is D, E, T, P, G, A, V, L, I, S, C, M, N or Q, and (X) is W, Y, L, G, A, V, I, P, M, or F; (b) an amino acid sequence which is at least 85% identical to the amino acid sequence of (a), wherein the identity determination excludes amino acid positions (X) to (X).

Chymase binding compounds and medical uses thereof

The invention relates to a compound of formula (I) 

Azetidine derivatives

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

The invention relates to a compound of formula (I) wherein Ato Aand Rto Rare defined as in the description and in the claims. The compound of formula (I) can be used as a medicament.

Pyrrolidine derivatives

The invention relates to a compound of formula (I) wherein A and Rto Rare defined as in the description and in the claims. The compound of formula (I) can be used as a medicament.

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

The invention relates to a compound of formula (I) wherein Ato Aand Rto Rare defined as in the description and in the claims. The compound of formula (I) can be used, for example, as inhibitors of the cysteine protease cathepsin.

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 2-Amino-5,5-difluoro-5,6-dihydro-4H-[1,3]oxazin-4-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.

2-amino-5,5-difluoro-5,6-dihydro-4H-[1,3]oxazin-4-yl)-phenyl]-amides

The present invention relates to 3-Amino-5-phenyl-5,6-dihydro-2H-[1,4]oxazines 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.

3-amino-5-phenyl-5,6-dihydro-2H-[1,4]oxazines

The invention relates to a compound of formula (I) wherein A, R-Rare as defined in the description and in the claims. The compound of formula (I) can be used as a medicament.

Proline derivatives

The invention is concerned with the novel sulfonamide derivatives of formula (I) wherein A, Rto R, X and Y are as defined in the description and in the claims, as well as physiologically acceptable salts thereof. These compounds inhibit chymase and can be used as medicaments.

Sulfonamide derivatives

This invention relates to 5,6-dihydro-4H-[1,3]oxazin-2-ylamine compounds of the formula wherein Rto Rare as defined in the description and in the claims, 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.

Amino oxazine derivatives

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David Banner