公开(公告)号：US20220265658A1

公开(公告)日：2022-08-25

申请号：US17625522

申请日：2020-07-08

申请人： Idorsia Pharmaceuticals Ltd.

发明人： Michael AMBUEHL ,  Elvire FOURNIER ,  Amandine FRAICHARD ,  Sylvie FROIDEVAUX ,  Oliver GEISELER ,  Charlyse HERRMANN ,  Francis HUBLER ,  Mark MURPHY ,  Dorte RENNEBERG ,  Simon STAMM ,  Markus VON RAUMER

IPC分类号： A61K31/519 ,  A61K47/10 ,  A61K47/14 ,  A61K47/22 ,  A61K47/44 ,  A61K9/107 ,  A61K9/48

摘要： The invention relates to pharmaceutical compositions, which are self-emulsifying, self-microemulsifying, or self-nanoemulsifying in aqueous medium, comprising the compound: 2-(2,2-Difluoro-propyl)-5-[1-(2-fluoro-6-methyl-phenyl)-piperidin-4-yl]-7-(2-trifluoromethyl-benzyl)-2,4,5,7-tetrahydro-pyrazolo[3,4-d]pyrimidin-6-one and a mixture of excipients comprising one or more lipophilic excipient(s); one or more hydrophilic surfactant(s); and optionally one or more hydrophilic co-solvent(s). The invention further relates to a crystalline form of said compound, and its use for the preparation of the present compositions. The invention further relates to pharmaceutical uses of the compositions for the prevention/prophylaxis or treatment of diseases and disorders related to pathogenic events associated with elevated levels of C5a and/or with C5aR activation.

公开(公告)号：US20230373967A1

公开(公告)日：2023-11-23

申请号：US18251814

申请日：2021-11-04

申请人： Idorsia Pharmaceuticals Ltd

发明人： Timo RAGER ,  Markus VON RAUMER

IPC分类号： C07D401/14

CPC分类号： C07D401/14 ,  C07B2200/13

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

公开(公告)号：US20210300894A1

公开(公告)日：2021-09-30

申请号：US17345844

申请日：2021-06-11

申请人： IDORSIA PHARMACEUTICALS LTD

发明人： Bibia HEIDMANN ,  Markus VON RAUMER

IPC分类号： C07D401/06

摘要： The present invention relates to crystalline forms of N-[1-(5-cyano-pyridin-2-ylmethyl)-1H-pyrazol-3-yl]-2-[4-(1-trifluoromethyl-cyclopropyl)-phenyl]-acetamide, pharmaceutical compositions comprising said crystalline forms and their use as T-type calcium channel blockers in the treatment or prevention of diseases or disorders where T-type calcium channels are involved.

公开(公告)号：US20200061061A1

公开(公告)日：2020-02-27

申请号：US16489227

申请日：2017-11-06

申请人： IDORSIA PHARMACEUTICALS LTD

发明人： Marc BELLET ,  Martin BOLLI ,  Martine CLOZEL ,  Marc IGLARZ ,  Philipp KOHLER ,  Ivan SCHINDELHOLZ ,  Markus VON RAUMER

IPC分类号： A61K31/506 ,  A61K31/41 ,  A61K31/4418 ,  A61K31/549 ,  A61K31/4035 ,  A61P9/12

摘要： 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.

公开(公告)号：US20200017534A1

公开(公告)日：2020-01-16

申请号：US16335973

申请日：2017-09-21

申请人： IDORSIA PHARMACEUTICALS LTD

发明人： Daniel LEUENBERGER ,  Stefan REBER ,  Markus VON RAUMER

IPC分类号： C07F9/6558

摘要： The invention relates to crystalline forms of 4-((R)-2-{[6-((S)-3-methoxy-pyrrolidin-1-yl)-2-phenyl-pyrimidine-4 carbonyl]-amino}-3-phosphono-propionyl)-piperazine-1-carboxylic acid butyl ester hydrochloride, processes for the preparation thereof, pharmaceutical compositions comprising said crystalline forms, pharmaceutical compositions prepared from such crystalline forms and their use as a medicament, especially as a P2Y12 receptor antagonist.

公开(公告)号：US20200002317A1

公开(公告)日：2020-01-02

申请号：US16489194

申请日：2018-02-26

申请人： IDORSIA PHARMACEUTICALS LTD

发明人： Martin BOLLI ,  Philipp KOHLER ,  Ivan SCHINDELHOLZ ,  Markus VON RAUMER

IPC分类号： C07D403/12 ,  A61P9/12

摘要： 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.

公开(公告)号：US20240116913A1

公开(公告)日：2024-04-11

申请号：US18263847

申请日：2022-01-28

申请人： Idorsia Pharmaceuticals Ltd

发明人： Markus VON RAUMER

IPC分类号： C07D413/14 ,  A61K9/20 ,  A61K31/5377

CPC分类号： C07D413/14 ,  A61K9/2013 ,  A61K9/2018 ,  A61K9/2027 ,  A61K9/2054 ,  A61K9/2095 ,  A61K31/5377 ,  C07B2200/13

摘要： The present invention relates to a crystalline form of (4-Methyl-2-[1,2,3]triazol-2-yl-phenyl)-[(R)-3-(3-[1,2,3]triazol-2-yl-benzyl)-morpholin-4-yl]-methanone, a process for the preparation thereof, pharmaceutical compositions comprising the same and its use as an orexin receptor antagonist in the prevention and/or treatment of various orexin receptor-mediated disorders such as Binge-Eating Disorder (BED).

公开(公告)号：US20230391757A1

公开(公告)日：2023-12-07

申请号：US18319402

申请日：2023-05-17

申请人： IDORSIA PHARMACEUTICALS LTD

发明人： Martin BOLLI ,  Markus VON RAUMER

IPC分类号： C07D403/12 ,  A61P9/12 ,  A61K31/4035 ,  A61K31/41 ,  A61K31/4418 ,  A61K31/506 ,  A61K31/549

CPC分类号： C07D403/12 ,  A61P9/12 ,  A61K31/4035 ,  A61K31/41 ,  A61K31/4418 ,  A61K31/506 ,  A61K31/549 ,  C07B2200/13 ,  A61P13/12

摘要： 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.

公开(公告)号：US20230255987A1

公开(公告)日：2023-08-17

申请号：US18016299

申请日：2021-07-14

申请人： Idorsia Pharmaceuticals Ltd

发明人： Stephan BUCHMANN ,  Amandine FRAICHARD ,  Charlyse HERRMANN ,  Céline LIENHART ,  Markus VON RAUMER ,  Tobias WERK

IPC分类号： A61K31/675 ,  A61K9/08 ,  A61K47/18 ,  A61K47/24 ,  A61K47/02

CPC分类号： A61K31/675 ,  A61K9/08 ,  A61K47/183 ,  A61K47/24 ,  A61K47/18 ,  A61K47/02

摘要： The present invention relates to an aqueous pharmaceutical composition comprising the P2Y12 receptor antagonist 4-((R)-2-{[6-((S)-3-methoxy-pyrrolidin-1-yl)-2-phenyl-pyrimidine-4-carbonyl]-amino}-3-phosphono-propionyl)-piperazine-1-carboxylic acid butyl ester and a pharmaceutically acceptable buffer and its use as a medicament by parenteral administration.

公开(公告)号：US20220275011A1

公开(公告)日：2022-09-01

申请号：US17741427

申请日：2022-05-10

申请人： Idorsia Pharmaceuticals Ltd

发明人： Daniel LEUENBERGER ,  Stefan REBER ,  Markus VON RAUMER

IPC分类号： C07F9/6558

摘要： The invention relates to crystalline forms of 4-((R)-2-{[6-((S)-3-methoxy-pyrrolidin-1-yl)-2-phenyl-pyrimidine-4-carbonyl]-amino}-3-phosphono-propionyl)-piperazine-1-carboxylic acid butyl ester hydrochloride, processes for the preparation thereof, pharmaceutical compositions comprising said crystalline forms, pharmaceutical compositions prepared from such crystalline forms and their use as a medicament, especially as a P2Y12 receptor antagonist.