Idorsia Pharmaceuticals Ltd

The present invention relates to novel oligosaccharide-carrier protein conjugates of Formula (I), and their use as pharmaceuticals, in particular as vaccines. The invention also concerns related aspects including oligosaccharide intermediates of Formulae (II) and (III), as well as processes for the preparation of the conjugates. Furthermore, the invention relates to pharmaceutical compositions comprising the oligosaccharide-carrier protein conjugates, as well as the use of the oligosaccharide-carrier protein conjugates of Formula (IV) in biological assays.

The present invention relates to compounds of Formula (I), their synthesis and use as CCR6 receptor modulators for the treatment or prevention of various diseases, conditions or disorders.

The present invention relates to macrocyclic compounds of Formula (I) wherein Ar 1 , Ar 2 , R 1 , R 2 , R 3 , R 4 , and X 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), to their use as modulators of CFTR alone or in combination with one or more therapeutically active ingredients acting as CFTR potentiators or CFTR correctors.

The invention relates to crystalline form of (3S,7S,10R,13R)-13-benzyl-20-fluoro-7-isobutyl-N-(2-(3-methoxy-1,2,4-oxadiazol-5-yl)ethyl)-6,9-dimethyl-1, 5,8,11-tetraoxo-10-(2,2,2-trifluoroethyl)-1,2,3,4,5,6,7,8,9,10,11,12,13,14-tetradecahydro-[1]oxa[4,7,10,14]tetraazacycloheptadecino[16,17-f]quinoline-3-carboxamide; processes for the preparation thereof, pharmaceutical compositions containing such crystalline form, pharmaceutical compositions prepared from such crystalline form, and their use as a medicament, especially as CFTR modulators.

The present invention concerns the compounds of formula (I) wherein R 1 , R 2 , R 3 , X, and Y are as described in the description, and their use as antagonists of the LPA 1 receptor, in combination with one or more therapeutically active ingredients acting as anti-fibrotic agent(s); such as especially pirfenidone and/or nintedanib, in the prevention and/or treatment of fibrotic diseases. The invention further relates to pharmaceutical compositions comprising the compounds of formula (I) in combination with one or more therapeutically active ingredients acting as anti-fibrotic agent(s) such as pirfenidone or nintedanib.

The present invention relates to a stable hydrate of clazosentan disodium salt, pharmaceutical formulations manufactured using the same and their use as medicaments.

The present invention relates to a pharmaceutical combination comprising a first active ingredient which is the CXCR3 antagonist 1-{(R)-2-(2-Hydroxy-ethyl)-4-[2-trifluoromethyl-4-(2-trifluoromethyl-pyrimidin-5-yl)-thiazol-5-yl]-piperazin-1-yl}-2-(3-methyl-[1,2,4]triazol-1-yl)-ethanone, or a pharmaceutically acceptable salt thereof, and a second active ingredient which is an anti-CD3 monoclonal antibody (mAb); and to the use of the pharmaceutical combination in the prevention, prophylaxis and/or treatment of (auto-)immune/inflammatory mediated disorders, including type 1 diabetes (T1D) (especially autoimmune T1D), multiple sclerosis, organ transplant rejection (especially renal and heart allograft rejection), thyroid eye disease, rheumatoid arthritis, ulcerative colitis, crohn's disease, celiac disease, atherosclerosis, psoriasis, lung inflammation, and psoriatic arthritis.

The present invention relates to pyridin-3-yl derivatives of Formula (I) wherein R 1 , R 2 , R 3 , R 4 , R 5 , Ar 1 , 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.

The present invention concerns the compound aprocitentan, {5-(4-bromo-phenyl)-6-[2-(5-bromo-pyrimidin-2-yloxy)-ethoxy]-pyrimidin-4-yl}-sulfamide: Formula (I) and its use as endothelin receptor antagonist in a method of treating hypertension including resistant hypertension in a subject in need thereof, said method comprising administering to the subject a pharmaceutical composition comprising a clinically proven effective amount of aprocitentan, or a pharmaceutically acceptable salt thereof.

The present invention concerns novel crystalline forms of aprocitentan sodium salt, 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.