Actelion Pharmaceuticals Ltd

Idorsia Pharmaceuticals Ltd

Other

Martin Bolli

Oliver Nayler

Claus Mueller

Boris Mathys

Christoph Boss

Beat Steiner

David Lehmann

Thomas Weller

Martine Clozel

Walter Fischli

Michael Scherz

Jörg Velker

Christoph Binkert

Cyrille Lescop

Corinna Grisostomi

Lubos Remen

John Gatfield

Cornelia Zumbrunn

Christine Brotschi

Jodi T Williams

Christoph Sager

Thierry Sifferlen

Bibia Heidmann

Daniel Bur

Markus Von Raumer

Marc Iglarz

Marc Bellet

Hamed Aissaoui

Sylvia Richard-Bildstein

Markus Gude

Gunther Schmidt

Stefan Abele

Patrick Sieber

Keith Morrison

Ivan Schindelholz

Alexander Treiber

Judith Marfurt

J)org Velker

Joerg Velker

Philipp Kohler

Nayler Oliver

The present invention relates to pyridin-3-yl derivatives of Formula (I) wherein R, R, R, R, R, Ar, L, m and n are as described in the description, their preparation, to pharmaceutically acceptable salts thereof, and to their use as pharmaceuticals, to pharmaceutical compositions containing one or more compounds of Formula (I), and especially to their use as LPA1 receptor modulators.

Pyridin-3-yl derivatives

The present invention relates to compounds of Formula (I) wherein Ar, R, R, R, and Rare as described in the description, their preparation, to pharmaceutically acceptable salts thereof, and to their use as pharmaceuticals, to pharmaceutical compositions containing one or more compounds of Formula (I), and especially to their use as Galectin-3 inhibitors.

(2-acetamidyl)thio-beta-D-galactopyranoside derivatives

The present invention relates to compounds of Formula (I) wherein Ar, Ar, R, R, and Rare as described in the description, their preparation, to pharmaceutically acceptable salts thereof, and to their use as pharmaceuticals, to pharmaceutical compositions containing one or more compounds of Formula (I), and especially to their use as Galectin-3 inhibitors.

(Hetero)aryl-methyl-thio-beta-D-galactopyranoside derivatives

The present invention relates to pyridinyl derivatives of Formula (I) Formula (I) wherein R, R, R, R, R, R, Ar, L, W, Z, m and n are as described in the description, their preparation, to pharmaceutically acceptable salts thereof, and to their use as pharmaceuticals, to pharmaceutical compositions containing one or more compounds of Formula (I), and especially to their use as LPA1 receptor modulators.

Alkoxy-substituted pyridinyl derivatives as LPA1 receptor antagonists and their use in the treatment of fibrosis

The present invention relates to compounds of Formula (I) wherein Ar, Rand Rare as described in the description, and A is 4,5-dihydroisoxazole-3,5-diyl, imidazolidin-4-one-1,3-diyl, oxazol-2-one-3,5-diyl and oxazolidine-2-one-3,5-diyl, 1,2,3-triazole-1,4-diyl, isoxazole-3,5-diyl, imidazole-1, 4-diyl, and isothiazole-3,5-diyl; and their preparation, to pharmaceutically acceptable salts thereof, and to their use as pharmaceuticals, to pharmaceutical compositions containing one or more compounds of Formula (I), and especially to their use as Galectin-3 inhibitors.

Alpha-D-galactopyranoside derivatives

The present invention relates to compounds of Formula (I) wherein Ar, A, B, and Rare as described in the description, their preparation, to pharmaceutically acceptable salts thereof, and to their use as pharmaceuticals, to pharmaceutical compositions containing one or more compounds of Formula (I), and especially to their use as Galectin-3 inhibitors.

Spiro derivatives of Alpha-D-galactopyranosides

The present invention relates to compounds of Formula (I) wherein X, Ar, Ar, L, n, m, and Rare as described in the description, their preparation, to pharmaceutically acceptable salts thereof, and to their use as pharmaceuticals, to pharmaceutical compositions containing one or more compounds of Formula (I), and especially to their use as Galectin-3 inhibitors.

Hydroxyheterocycloalkane-carbamoyl derivatives

The present invention concerns novel crystalline forms of {5-(4-bromo-phenyl)-6-[2-(5-bromo-pyrimidin-2-yloxy)-ethoxy]-pyrimidin-4-yl}-sulfamide, processes for the preparation thereof, pharmaceutical compositions comprising said crystalline forms, pharmaceutical compositions prepared from such crystalline forms, and their use as endothelin receptor antagonists. It also relates to new uses of {5-(4-bromo-phenyl)-6-[2-(5-bromo-pyrimidin-2-yloxy)-ethoxy]-pyrimidin-4-yl}-sulfamide, either alone or in combination with other active ingredients or therapeutic agents.

Crystalline forms of a 4-pyrimidinesulfamide derivative aprocitentan

The present invention relates to compounds of Formula (I)

2-hydroxycycloalkane-1-carbamoyl

The present invention relates to compounds of Formula (I) wherein Ar, Ar, L, n, and Rare as described in the description, their preparation, to pharmaceutically acceptable salts thereof, and to their use as pharmaceuticals, to pharmaceutical compositions containing one or more compounds of Formula (I), and especially to their use as Galectin-3 inhibitors.

Galectin-3 inhibiting 2-hydroxycycloalkane-1-carbamoyl derivatives

The present invention concerns the compound aprocitentan, {5-(4-bromo-phenyl)-6-[2-(5-bromo-pyrimidin-2-yloxy)-ethoxy]-pyrimidin-4-yl}-sulfamide: and its use as endothelin receptor antagonist, in combination with an SGLT-2 inhibitor. The invention further relates to pharmaceutical compositions comprising aprocitentan in combination with said SGLT-2 inhibitor. The invention further relates to such pharmaceutical compositions comprising crystalline forms of aprocitentan.

Combination of a 4-pyrimidinesulfamide derivative with an SGLT-2 inhibitor for the treatment of endothelin related diseases

The present invention concerns the compound aprocitentan, {5-(4-bromo-phenyl)-6-[2-(5-bromo-pyrimidin-2-yloxy)-ethoxy]-pyrimidin-4-yl}-sulfamide, and its use as endothelin receptor antagonist, in combination with other active ingredients or therapeutic agents including an angiotenin receptor blocker, and/or a calcium channel blocker, and preferably a diuretic which is a thiazide-like diuretic, in the prophylaxis or treatment of certain endothelin related diseases. The invention further relates to pharmaceutical compositions comprising aprocitentan in combination with said other active ingredients or therapeutic agents. The invention further relates to such pharmaceutical compositions comprising novel crystalline forms of aprocitentan.

Combinations of a 4-pyrimidinesulfamide derivative with active ingredients for the treatment of endothelin related diseases

The present invention concerns novel crystalline forms of {5-(4-bromo-phenyl)-6 [2 (5 bromo-pyrimidin-2-yloxy)-ethoxy]-pyrimidin-4-yl}-sulfamide, processes for the preparation thereof, pharmaceutical compositions comprising said crystalline forms, pharmaceutical compositions prepared from such crystalline forms, and their use as endothelin receptor antagonists. It also relates to new uses of {5-(4-bromo-phenyl)-6-[2-(5-bromo-pyrimidin-2-yloxy)-ethoxy]-pyrimidin-4-yl}-sulfamide, either alone or in combination with other active ingredients or therapeutic agents.

The invention relates to 2,5-disubstituted benzoxazole and benzothiazole derivatives of Formula (I) wherein L, X, Y, and ring (A) are as described in the description, their preparation and their use as pharmaceutically active compounds. Said compounds may be useful for the prevention or treatment of diseases or disorders associated with impaired reactive oxygen species (ROS) production, and/or for the prevention or treatment of various fibrotic diseases.

NADPH oxidase 4 inhibitors

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Allschwil, Switzerland

Martin Bolli