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公开(公告)号：US20240131009A1
公开(公告)日：2024-04-25
申请号：US18401886
申请日：2024-01-02
发明人： Martine CLOZEL , Luca PIALI
IPC分类号： A61K31/426 , A61K9/00 , A61K31/22 , A61K31/225 , A61K31/27 , A61K31/4015
CPC分类号： A61K31/426 , A61K9/0053 , A61K31/22 , A61K31/225 , A61K31/27 , A61K31/4015
摘要： The present invention relates to a pharmaceutical combination comprising a first active ingredient which is (R)-5-[3-chloro-4-(2,3-dihydroxy-propoxy)-benz[Z]ylidene]-2-([Z] propylimino)-3-o-tolyl-thiazolidin-4-one or a pharmaceutically acceptable salt thereof and a second active ingredient which is selected from the group consisting of methyl fumarate, dimethyl fumarate, (N,N-diethylcarbamoyl)methyl methyl (2E)but-2-ene-1,4-dioate, and 2-(2,5-dioxopyrrolidin-1-yl)ethyl methyl (2E)but-2-ene-1,4-dioate, or a pharmaceutically acceptable salt thereof.
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公开(公告)号：US20240091223A1
公开(公告)日：2024-03-21
申请号：US18261923
申请日：2022-01-28
发明人： Katie AMSSOMS , Eddy DE PROOST , Wenyu DONG , Paul HARTMAN KOK , Rene HOLM , Kristof KIMPE , Greet MEURS , Maxim VERSTRAETEN
IPC分类号： A61K31/497 , A61K9/19 , A61K47/10 , A61K47/26
CPC分类号： A61K31/497 , A61K9/19 , A61K47/10 , A61K47/26
摘要： The present invention relates to a pharmaceutical composition comprising the calcium; {4-[(5,6-diphenylpyrazin-2-yl) (propan-2-yl)amino]butoxy}acetate, in particular to long-acting injectables comprising the same, the use of the pharmaceutical composition for the treatment or prevention of specific diseases, and a process to produce it.
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公开(公告)号：US11612600B2
公开(公告)日：2023-03-28
申请号：US17736434
申请日：2022-05-04
发明人： Dénes Csonka , Wassim Fares , Hans Hoogkamer , Koen Torfs
IPC分类号： A61K31/506 , A61K45/06 , A61P9/12
摘要： The present invention relates to high doses of macitentan (INN), i.e. propylsulfamic acid [5-(4-bromo-phenyl)-6-[2-(5-bromo-pyrimidin-2-yloxy)-ethoxy]-pyrimidin-4-yl]-amide or pharmaceutically acceptable salts, solvates, hydrates or morphological forms thereof, or of aprocitentan, for use in the treatment and/or prevention of chronic thromboembolic pulmonary hypertension (CTEPH). Moreover, the present invention relates to the use of high doses of macitentan or of aprocitentan for the manufacture of a medicament for the treatment and/or prevention of CTEPH, as well as to a method for the treatment and/or prevention of CTEPH comprising administering high doses of macitentan or of aprocitentan to a patient. Further, the present invention relates to a dosage regimen for the treatment and/or prevention of CTEPH as well as to a combination of macitentan, or of aprocitentan, with one or more phosphodiesterase type 5 (PDE5) inhibitors, prostacyclin analogues, prostacyclin receptor agonists or soluble guanylate cyclase stimulators. Moreover, the present invention relates to a pharmaceutical composition for the treatment of CTEPH comprising a high dose of macitentan or of aprocitentan.
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公开(公告)号：US20230032813A1
公开(公告)日：2023-02-02
申请号：US17780064
申请日：2020-11-27
发明人： Alessandro MARESTA , Loïc PERCHENET
IPC分类号： A61K31/506 , A61K31/505 , A61K31/4985 , A61K31/519 , A61K31/496 , A61K31/4965 , A61P9/12 , A61P11/00 , A61K9/00
摘要： The disclosure relates to methods of reducing the risk of disease progression in a patient with pulmonary arterial hypertension (PAH), comprising administering to a patient in need thereof, an initial triple combination therapy of an endothelin receptor antagonist (ERA), a phosphodiesterase type 5 (PDE-5) inhibitor, and a prostacyclin receptor agonist (IP receptor agonist).
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公开(公告)号：US11464777B2
公开(公告)日：2022-10-11
申请号：US17515132
申请日：2021-10-29
发明人： Dénes Csonka , Wassim Fares , Hans Hoogkamer , Koen Torfs
IPC分类号： A61K31/506 , A61P9/12 , A61K31/4965 , A61K31/4985
摘要： The present invention relates to high doses of macitentan, i.e. propylsulfamic acid [5-(4-bromo-phenyl)-6-[2-(5-bromo-pyrimidin-2-yloxy)-ethoxy]-pyrimidin-4-yl]-amide or pharmaceutically acceptable salts, solvates, hydrates or morphological forms thereof, or of aprocitentan, for use in the treatment and/or prevention of pulmonary arterial hypertension (PAH). Moreover, the present invention relates to the use of high doses of macitentan, or of aprocitentan, for the manufacture of a medicament for the treatment and/or prevention of PAH, as well as to a method for the treatment and/or prevention of PAH comprising high doses of macitentan or of aprocitentan. Further, the present invention relates to a dosage regimen for the treatment and/or prevention of PAH as well as to a combination of macitentan, or of aprocitentan, with one or more phosphodiesterase type 5 (PDE5) inhibitors, prostacyclin analogues, prostacyclin receptor agonists or soluble guanylate cyclase stimulators. Therein, PAH is preferably mild or moderate PAH. Moreover, the present invention relates to a pharmaceutical composition for the treatment of PAH comprising a high dose of macitentan or of aprocitentan.
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公开(公告)号：US20220257594A1
公开(公告)日：2022-08-18
申请号：US17612014
申请日：2020-05-20
发明人： Carol ZHAO , Johanna COLVIN RIESEN , Gary Arnold PALMER , Michael KEATING , Brian HARTLINE , Wade BENTON , Camelia DUMITRESCU , Mehul Bipinchandra SHAH
IPC分类号： A61K31/4965 , A61K45/06 , A61P9/12
摘要： The present disclosure provides methods of transitioning a patient being treated for pulmonary arterial hypertension with a non-selexipag prostacyclin pathway agent (PPA) to selexipag.
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公开(公告)号：US20210186966A1
公开(公告)日：2021-06-24
申请号：US17116983
申请日：2020-12-09
IPC分类号： A61K31/506 , A61K9/16 , A61K9/20 , A61K9/28
摘要： The invention relates to stable pharmaceutical compositions comprising the compound of the below formula, or pharmaceutically acceptable salts, solvates, hydrates or morphological forms thereof
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公开(公告)号：US20210052555A1
公开(公告)日：2021-02-25
申请号：US17090756
申请日：2020-11-05
发明人： Jasper DINGEMANSE , Matthias HOCH , Andreas KRAUSE
IPC分类号： A61K31/426 , A61K9/00
摘要： The present invention relates to a dosing regimen for (R)-5-[3-chloro-4-(2,3-dihydroxy-propoxy)-benz[Z]ylidene]-2-([Z]-propylimino)-3-o-tolyl-thiazolidin-4-one.
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公开(公告)号：US10603428B2
公开(公告)日：2020-03-31
申请号：US14894114
申请日：2013-05-30
申请人： WEIBEL CDS AG
发明人： Ludwig Daniel Weibel
摘要： A device (1) for dispensing a fluid, in particular to a patient, comprising a container (15), in particular an at least partly collapsible container, with an interior (17) for receiving the fluid. The container (15) comprises a closure piece (20) which is rigidly arranged in the container (15) in particular and on which a dispensing opening (24) is formed, wherein the fluid can be dispensed out of the interior (17) through the dispensing opening. The device (1) comprises a pump device (40) driven by a pump drive (50) in order to pump the fluid out of the interior (17) of the container (15). The pump device (40) is fluidically arranged between the interior (17) and the dispensing opening (24) so that the fluid can be pumped out of the interior (17) to the dispensing opening (24) by the pump device (40).
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公开(公告)号：US10189839B2
公开(公告)日：2019-01-29
申请号：US15038015
申请日：2014-11-18
发明人： Daniel Bur , Corinna Grisostomi , Oliver Nayler , Lubos Remen , Magali Vercauteren , Richard Welford
IPC分类号： C07D471/04 , C07D498/12 , C07D513/14 , C07D471/14
摘要： The present invention relates to compounds of the formula (I) wherein R1a, R1b, R2, R3, and X are as described in the description, to 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 methods for the preparation of such compounds of formula (I), and especially to their use as TPH modulators.
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