专利快速检索-快速检索全球专利，免费商用专利数据库-IPRDB

1. 发明申请

WO2022258796A1 DISPERSIBLE TABLET FOR ORAL ADMINISTRATION 审中-公开
公开(公告)号：WO2022258796A1
公开(公告)日：2022-12-15
申请号：PCT/EP2022/065797
申请日：2022-06-10
申请人： ACTELION PHARMACEUTICALS LTD
发明人： VAN HOVE, Ben , BOIY, Annelies
IPC分类号： A61K9/20 , A61K9/00 , A61K31/506 , A61P9/12
摘要： The present invention is directed to pharmaceutical compositions or dispersible tablets for oral administration comprising N-[5-(4-bromophenyl)-6-[2-[(5-bromo-2-pyrimidinyl)oxy]ethoxy]-4-pyrimidinyl]-N'-propylsulfamide (macitentan), the use of said pharmaceutical compositions or dispersible tablets for the treatment of pulmonary hypertension and the process for preparing such dispersible tablets.

2. 发明申请

WO2021156227A1 METHODS OF TREATING AND ASSESSING PULMONARY ARTERIAL HYPERTENSION WITH SELEXIPAG 审中-公开
公开(公告)号：WO2021156227A1
公开(公告)日：2021-08-12
申请号：PCT/EP2021/052374
申请日：2021-02-02
申请人： ACTELION PHARMACEUTICALS LTD
发明人： COTTREEL, Emmanuelle , PERCHENET, Loïc
IPC分类号： A61K31/4965 , A61P9/00 , A61P9/12
摘要： The present disclosure provides methods for treating pulmonary arterial hypertension in a patient in need thereof, comprising (a) performing magnetic resonance imaging (MRI) on the right ventricle of the patient to provide a MRI baseline image; (b) administering a therapeutically effective amount of selexipag; (c) performing MRI on the right ventricle of the patient to provide a MRI test image; and (d) comparing the MRI baseline image with the MRI test image.

3. 发明申请

WO2021152060A1 CONTROLLED RELEASE SELEXIPAG COMPOSITION 审中-公开
公开(公告)号：WO2021152060A1
公开(公告)日：2021-08-05
申请号：PCT/EP2021/052059
申请日：2021-01-29
申请人： ACTELION PHARMACEUTICALS LTD
发明人： LUYTEN, Katrien , VAN DROOGENBROECK, Annelien
IPC分类号： A61K9/50 , A61K31/4965 , A61P3/10 , A61P9/12 , A61P11/00 , A61P13/12
摘要： The present invention is concerned with controlled release compositions for oral administration comprising 2-{4-[N-(5,6-diphenylpyrazin-2-yl)-N- isopropylamino]butyloxy}-N-(methylsulfonyl)acetamide (selexipag, NS-304, ACT- 293987) and its pharmaceutically acceptable salts and/or 2-(4-((5,6-diphenylpyrazin-2-yl)(isopropyl)amino)butoxy)acetic acid (metabolite of selexipag, MRE-269, ACT- 333679) and its pharmaceutically acceptable salts; and with processes for preparing such controlled release compositions as well as to uses thereof.

4. 发明申请

WO2021105331A1 METHODS OF TREATING PULMONARY ARTERIAL HYPERTENSION 审中-公开
公开(公告)号：WO2021105331A1
公开(公告)日：2021-06-03
申请号：PCT/EP2020/083593
申请日：2020-11-27
申请人： ACTELION PHARMACEUTICALS LTD
发明人： MARESTA, Alessandro , PERCHENET, Loïc
IPC分类号： A61K31/4965 , A61K31/4985 , A61K31/505 , A61K31/506 , A61K31/519 , A61K31/53 , A61P9/12 , A61K45/06
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).

5. 发明申请

WO2021105164A1 PHARMACEUTICAL COMPOSITION FOR THE TREATMENT OF PULMONARY VASCULAR DISEASE AND/OR CARDIAC DYSFUNCTION IN FONTAN-PALLIATED PATIENTS 审中-公开
公开(公告)号：WO2021105164A1
公开(公告)日：2021-06-03
申请号：PCT/EP2020/083289
申请日：2020-11-25
申请人： ACTELION PHARMACEUTICALS LTD
发明人： CSONKA, Dénes , FARES, Wassim , HOOGKAMER, Hans , TORFS, Koen
IPC分类号： A61K9/00 , A61K31/343 , A61K31/4965 , A61K31/506 , A61K31/5575 , A61K31/5578 , A61K45/06 , A61P9/10 , A61K31/505
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 for use in the treatment of pulmonary vascular disease and/or cardiac dysfunction in functional single ventricular heart disease patients, especially in Fontan-palliated patients. Moreover, the present invention relates to the use of high doses of macitentan for the manufacture of a medicament as well as to a method for the treatment of said diseases. Further, the present invention relates to a dosage regimen as well as to a combination of macitentan with one or more phosphodiesterase type 5 (PDE5) inhibitors, prostacyclin analogues, prostacyclin receptor agonists or soluble guanylate cyclase stimulators. Besides, the present invention relates to a pharmaceutical composition for the treatment of pulmonary vascular disease and/or cardiac dysfunction in functional single ventricular heart disease patients, especially in Fontan-palliated patients comprising a high dose of macitentan. Moreover, the present invention relates to the use of high doses aprocitentan for the same purpose.

6. 发明申请

WO2020128017A1 PHARMACEUTICAL COMPOSITION FOR THE TREATMENT OF PULMONARY ARTERIAL HYPERTENSION 审中-公开
公开(公告)号：WO2020128017A1
公开(公告)日：2020-06-25
申请号：PCT/EP2019/086754
申请日：2019-12-20
申请人： ACTELION PHARMACEUTICALS LTD
发明人： CSONKA, Dénes , FARES, Wassim , HOOGKAMER, Hans , TORFS, Koen
IPC分类号： A61K31/506 , A61P9/12 , A61P11/00
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.

7. 发明申请

WO2018162527A1 PHARMACEUTICAL COMPOSITION COMPRISING SELEXIPAG 审中-公开
公开(公告)号：WO2018162527A1
公开(公告)日：2018-09-13
申请号：PCT/EP2018/055551
申请日：2018-03-07
申请人： ACTELION PHARMACEUTICALS LTD
发明人： HELLERBRAND, Klaus , SCHLICKER-SPAIN, Alexandra
IPC分类号： A61K47/10 , A61K9/19 , A61K31/4965 , A61P17/02 , A61P9/12
摘要： The invention relates to aqueous pharmaceutical compositions comprising the compound 2-{4-[N-(5,6-diphenylpyrazin-2-yl)-N-isopropylamino]butyloxy}-N-(methylsulfonyl) acetamide; glycine; polysorbate 20; and an aqueous phosphate buffer, wherein the relative amounts are as described in the description, wherein the pH of said pharmaceutical composition is between about 7 and 8; to lyophilized pharmaceutical compositions prepared from said aqueous compositions, and to reconstituted aqueous compositions thereof which are suitable for i.v. administration. The invention further relates to processes for the preparation of said compositions, and to their use for the treatment of diseases and disorders which are related to IP receptor.

8. 发明申请

WO2017179002A1 ANTIBACTERIAL BIAROMATIC DERIVATIVES WITH OXETANE-3-YLOXY SUBSTITUTION 审中-公开
标题翻译：具有OXETANE-3-YLOXY取代基的抗菌BIAROMATIC衍生物
公开(公告)号：WO2017179002A1
公开(公告)日：2017-10-19
申请号：PCT/IB2017/052133
申请日：2017-04-13
申请人： ACTELION PHARMACEUTICALS LTD
发明人： CREN, Sylvaine , RUEEDI, Georg , ZUMBRUNN, Cornelia
IPC分类号： C07D417/14 , C07D498/04 , A61P31/04 , A61K31/5383 , A61K31/542
摘要： The invention relates to antibacterial compounds of formula (I), wherein U 1 represents N or CH, U 2 represents N or CH, U 3 represents N or CH, it being understood that at most two of U 1 , U 2 , U 3 can represent N at the same time; V 1 represents N or CH, V 2 represents N, CH or C(OH) and V 3 represents N, CH or C(OH), it being understood that at most two of V 1 , V 2 and V 3 can represent N at the same time; the dotted line "----- " represents a bond or is absent; X represents CH or N; and Q represents O or S. It further relates pharmaceutical compositions containing these compounds and the uses of these compounds in the manufacture of medicaments for the treatment of bacterial infections. These compounds are useful antimicrobial agents effective against a variety of human and veterinary pathogens including among others Gram-positive and Gram-negative aerobic and anaerobic bacteria.
摘要翻译：本发明涉及式（I）的抗菌化合物，其中U 1代表N或CH，U 2代表N或CH，U 3表示N或CH，应该理解的是，U 1，U 2，U 3中至多两个，可以同时代表N; V 1表示N或CH，V 2表示N，CH或C（OH），并且V 3表示N，CH或C（OH）），应该理解，V 1，V 2和V 3中的至多两个可以同时表示N; 虚线“-----” 代表债券或不存在; X代表CH或N; Q代表O或S.它进一步涉及含有这些化合物的药物组合物以及这些化合物在制备用于治疗细菌感染的药物中的用途。这些化合物是有效对抗各种人类和兽医病原体的有用的抗微生物剂，其中包括革兰氏阳性和革兰氏阴性好氧和厌氧细菌。

9. 发明申请

WO2017085198A1 N-SUBSTITUTED INDOLE DERIVATIVES AS PGE2 RECEPTOR MODULATORS 审中-公开
标题翻译： N取代的吲哚衍生物作为PGE2受体调节剂
公开(公告)号：WO2017085198A1
公开(公告)日：2017-05-26
申请号：PCT/EP2016/078028
申请日：2016-11-17
申请人： ACTELION PHARMACEUTICALS LTD
发明人： FRETZ, Heinz , LYOTHIER, Isabelle , POTHIER, Julien , RICHARD-BILDSTEIN, Sylvia , SIFFERLEN, Thierry , WYDER PETERS, Lorenza , POZZI, Davide , CORMINBOEUF, Olivier
IPC分类号： C07D403/12 , C07D413/14 , C07D403/14 , C07D409/14 , C07D417/14 , A61K31/506 , A61P35/00 , A61P25/00 , A61P9/00 , A61P11/00 , A61P15/00
CPC分类号： C07D413/14 , C07D403/12 , C07D403/14 , C07D409/14 , C07D417/14
摘要： The present invention relates to derivativesof formula (I) wherein (R 1 )n, R 2 , R 3 , R 4a , R 4b , R 5a , R 5b and Ar 1 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), and especially to their use as modulators of the prostaglandin 2 receptors EP2 and/or EP4.
摘要翻译：本发明涉及式（I）的衍生物，其中（R 1）n，R 2，R 3，R 3， R 4a，R 4b，R 5a，R 5b和Ar 1的取代基取代。如描述中所述，它们的制备，其药学上可接受的盐，以及它们作为药物的用途，含有一种或多种式（I）化合物的药物组合物，并且尤其涉及它们作为前列腺素2 受体EP2和/或EP4。

10. 发明申请

WO2016207785A1 NADPH OXIDASE 4 INHIBITORS 审中-公开
标题翻译： NADPH氧化酶4抑制剂
公开(公告)号：WO2016207785A1
公开(公告)日：2016-12-29
申请号：PCT/IB2016/053672
申请日：2016-06-21
申请人： ACTELION PHARMACEUTICALS LTD
发明人： AISSAOUI, Hamed , BOLLI, Martin , BOSS, Christoph , RICHARD-BILDSTEIN, Sylvia , SIEBER, Patrick
IPC分类号： C07D263/54 , C07D263/58 , C07D277/62 , C07D413/14 , C07D413/12 , C07D417/12 , A61K31/423 , A61K31/428
CPC分类号： C07D413/12 , C07D263/54 , C07D263/58 , C07D277/62 , C07D413/14 , C07D417/12 , C07D417/14 , C07D471/10 , C07D491/107
摘要： The invention relates to 2,5-disubstituted benzoxazole and benzothiazole derivatives of Formula (I) 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.
摘要翻译：本发明涉及式（I）式（I）的2,5-二取代的苯并恶唑和苯并噻唑衍生物，其中L，X，Y和环（A）如说明书中所述，其制备及其作为药物活性化合物的用途。所述化合物可用于预防或治疗与受损的活性氧（ROS）产生和/或用于预防或治疗各种纤维化疾病相关的疾病或病症。

你已经成功收藏专利！

检索式保存成功!

IPRDB

热门服务

关于我们

友情链接

联系方式