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公开(公告)号：EP3027192A1
公开(公告)日：2016-06-08
申请号：EP14831872.8
申请日：2014-08-01
申请人： Pharmacyclics, LLC
IPC分类号： A61K31/52 , A61K31/519 , A61P35/00
CPC分类号： A61K31/519 , A61K31/343 , A61K45/06 , A61K2300/00
摘要： Described herein are combinations of ACK inhibitors and HDAC inhibitors in the treatment of diseases and disorders characterized by the presence or development of solid tumors.
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公开(公告)号：EP2530083B1
公开(公告)日：2016-04-27
申请号：EP12166295.1
申请日：2006-12-28
申请人： Pharmacyclics LLC
发明人： Honingberg, Lee , Vernier, Erik , Pan, Zhengying
IPC分类号： C07D487/04 , A61K31/519 , A61P29/00
CPC分类号： A61K31/52 , A61K9/4825 , A61K31/00 , A61K31/519 , A61K39/3955 , A61K45/06 , A61K2300/00 , C07D487/04 , C07K16/2887 , C07K2317/24
摘要： Disclosed herein are compounds that form covalent bonds with Bruton's tyrosine kinase (Btk). Also described arc irreversible inhibitors of Btk. Methods for the preparation of the compounds are disclosed. Also disclosed are pharmaceutical compositions that include the compounds. Methods of using the Btk inhibitors are disclosed, alone or in combination with other therapeutic agents, for the treatment of autoimmune diseases or conditions, heteroimmune diseases or conditions, cancer, including lymphoma, and inflammatory diseases or conditions.
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23.发明公开2-(2-HYDROXYBIPHENYL-3-YL)-1H-BENZOIMIDAZOLE-5-CARBOXAMIDINE DERIVATIVES AS FACTOR VIIA INHIBITORS FOR THE TREATMENT OF THROMBOEMBOLIC DISORDERS 审中-公开2-（2-羟基联苯-3-基）-1H-苯并咪唑-5-甲脒衍生物作为凝血因子Ⅶa抑制剂用于治疗血栓栓塞性病症的
公开(公告)号：EP2982668A3
公开(公告)日：2016-04-13
申请号：EP15164898.7
申请日：2003-12-03
申请人： Pharmacyclics LLC
发明人： KOLESNIKOV, Aleksandr , RAI, Roopa , SHRADER, William, Dvorak , TORKELSON, Steven, M. , WESSON, Kieron, E. , YOUNG, Wendy, B.
IPC分类号： C07D235/18 , C07D401/12 , C07D403/10 , C07D407/12 , C07D471/04
CPC分类号： C07D235/18 , C07D235/12 , C07D235/16 , C07D401/12 , C07D403/10 , C07F9/094 , C07F9/12 , C07F9/65128 , C12Q1/56
摘要： The present invention relates to 2-(2-hydroxybiphenyl-3-yl)-1H-benzoimidazole-5-carboxamidine derivatives as factor VIIa inhibitors for the treatment of thromboembolic disorders, cancers and rheumatoid arthritis. Processes for preparing these inhibitors and intermediates thereof are also disclosed.
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公开(公告)号：EP2265590B1
公开(公告)日：2016-04-13
申请号：EP09733489.0
申请日：2009-04-15
申请人： Pharmacyclics, LLC
IPC分类号： C07D235/06 , C07D235/08 , C07D235/10 , C07D235/12 , C07D235/14
CPC分类号： A61K45/06 , A61K31/40 , A61K31/404 , A61K31/4439 , A61K31/5377 , C07D207/337 , C07D209/08 , C07D209/12 , C07D209/14 , C07D235/06 , C07D307/79 , C07D307/80 , C07D333/54 , C07D333/56 , C07D401/06 , C07D401/12 , C07D405/06 , C07D409/06 , C07D471/04 , Y02A50/40
摘要： Described herein are compounds and pharmaceutical compositions containing such compounds, which inhibit the activity of histone deacetylase 8 (HDAC8). Also described herein are methods of using such HDAC8 inhibitors, alone and in combination with other compounds, for treating diseases or conditions that would benefit from inhibition of HDAC8 activity.
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公开(公告)号：EP3344254A1
公开(公告)日：2018-07-11
申请号：EP16763673
申请日：2016-08-31
申请人： PHARMACYCLICS LLC
发明人： BILOTTI ELIZABETH , GRAEF THORSTEN
IPC分类号： A61K31/519 , A61K31/454 , A61K31/573 , A61K35/00
CPC分类号： A61K31/573 , A61K9/0053 , A61K9/20 , A61K9/48 , A61K31/454 , A61K31/519 , A61K2300/00
摘要： Disclosed herein are pharmaceutical combinations, dosing regimen, and methods of administering a combination of a BTK inhibitor (e.g., ibrutinib), an immunomodulatory agent, and a steroid for the treatment of a hematologic malignancy.
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公开(公告)号：EP3220912A4
公开(公告)日：2018-06-20
申请号：EP15860051
申请日：2015-11-17
申请人： PHARMACYCLICS LLC
发明人： CHANG BETTY Y , BEAUPRE DARRIN , KUO HSU-PING
IPC分类号： A61K31/519 , A61K31/517 , A61K45/06 , A61P35/00
CPC分类号： A61K31/517 , A61K31/519 , A61K45/06
摘要： Provided are compositions for and methods of treating a B-cell malignancy in a subject in need thereof, by administering to the subject a therapeutically effective amount of a combination comprising an inhibitor of a BTK inhibitor and a TLR inhibitor.
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27.发明公开PROCEDE DE PREPARATION DE SEL DE TOSYLATE DE L'ABEXINOSTAT ET FORME CRISTALLINE ASSOCIEE 审中-公开制备盐酸阿比森林酯盐及相关结晶形式的方法
公开(公告)号：EP3252044A1
公开(公告)日：2017-12-06
申请号：EP17166690.2
申请日：2014-03-03
申请人： Pharmacyclics LLC
IPC分类号： C07D307/85 , A61K31/343 , A61P29/00 , A61P35/00
CPC分类号： C07D307/85 , C07C309/30
摘要： Procédé de préparation du Tosylate d'abexinostat de formule (II) :
et sa forme cristalline 1 caractérisée par son diagramme de diffraction X sur poudre, son spectre Raman, et son spectre RMN à l'état solide 13 C CP/MAS.摘要翻译： 用于制备甲苯磺酸酯的abexinostat式（II）的：其特征在于，上粉末其衍射图案X和其结晶形式1，其拉曼光谱，NMR谱和固态13C CP / MAS。
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公开(公告)号：EP3226864A1
公开(公告)日：2017-10-11
申请号：EP15864946.7
申请日：2015-12-02
申请人： Pharmacyclics LLC
IPC分类号： A61K31/445 , C07D487/04 , C09B31/147
CPC分类号： A61K31/519 , A61K31/7068 , C09B31/147 , A61K2300/00
摘要： Disclosed are methods of treating fibrosis in a patient, comprising administering to a patient in need thereof a therapeutically effective amount of an ACK inhibitor (e.g., a BTK inhibitor, such as for example an irreversible BTK inhibitor, such as for example, ibrutinib).
摘要翻译： 公开了治疗患者纤维化的方法，其包括向有需要的患者施用治疗有效量的ACK抑制剂（例如，BTK抑制剂，例如不可逆的BTK抑制剂，例如依鲁替尼）。
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29.发明公开NOVEL SALTS OF 3-[(DIMETHYLAMINO)METHYL]-N-{2-[4-(HYDROXYCARBAMOYL) PHENOXY]ETHYL}-1-BENZOFURAN-2-CARBOXAMIDE, RELATED CRYSTALLINE FORMS, METHOD FOR PREPARING THE SAME AND PHARMACEUTICAL COMPOSITIONS CONTAINING THE SAME 审中-公开新型3 - [（二甲基氨基）甲基] -N- {2- [4-（羟基氨基甲酰氨基）苯氧基]乙基} -1-苯并呋喃-2-甲酰胺的盐，相关的结晶形式，制备它们的方法和含有它们的药物组合物 相同
公开(公告)号：EP3189040A1
公开(公告)日：2017-07-12
申请号：EP15767627.1
申请日：2015-09-03
申请人： Pharmacyclics LLC
IPC分类号： C07D307/85 , A61K31/343 , A61P35/00
摘要： wherein HA is naphthalene-1,5-disulfonic acid, naphthalene-2-sulfonic acid, oxalic acid, benzenesulfonic acid, or sulfuric acid, or hydrates thereof, and crystalline forms thereof characterized by the powder X-ray diffraction diagram and the 13C CP/MAS NMR solid state spectrum. Also described are compositions, methods of use and preparation thereof.
摘要翻译： 本文描述了3 - [（二甲基氨基）甲基] -N- {2- [4-（羟基氨基甲酰基）苯氧基]乙基} -1-苯并呋喃-2-甲酰胺，特别是式（I） I））其中HA是萘-1,5-二磺酸，萘-2-磺酸，草酸，苯磺酸或硫酸，或其水合物及其结晶形式，其特征在于粉末X射线衍射图和 13C CP / MAS NMR固态光谱。 还描述了组合物，使用方法或其制备。
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30.发明公开COMBINATIONS OF BRUTON'S TYROSINE KINASE INHIBITORS AND CYP3A4 INHIBITORS 审中-公开酪氨酸激酶抑制剂与CYP3A4抑制剂的组合
公开(公告)号：EP2968341A4
公开(公告)日：2016-11-23
申请号：EP14774808
申请日：2014-03-12
申请人： PHARMACYCLICS LLC
IPC分类号： A61K31/519 , A61K31/427 , A61K31/496 , A61K31/5377 , A61K45/06 , A61P31/00 , A61P31/12
CPC分类号： A61K31/519 , A61K31/426 , A61K31/427 , A61K31/496 , A61K31/5377 , A61K36/752 , A61K45/06 , A61K2300/00
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