公开(公告)号：EP3157907B1

公开(公告)日：2018-08-29

申请号：EP15727997.7

申请日：2015-06-11

申请人： Flamma S.P.A.

发明人： RENCUROSI, Anna ,  PREVITALI, Massimo ,  DELLA NEGRA, Federico ,  MORMILE, Francesco ,  CANEVOTTI, Renato

IPC分类号： C07D239/46 ,  C07D239/50 ,  C07D487/04

CPC分类号： C07D487/04 ,  C07D239/46 ,  C07D239/48 ,  C07D239/50

摘要： The present invention relates to a process for preparation of triazolo[4,5-d] pyrimidine cyclopentane compounds of formula (I), and pharmaceutically acceptable salts thereof. The invention also provides novel compounds that can be used as intermediates in the process for preparing triazolo[4,5-d] pyrimidine cyclopentane compounds. The process and the intermediates are particularly useful for the preparation of ticagrelor and pharmaceutically acceptable salts thereof.

公开(公告)号：EP3354647A1

公开(公告)日：2018-08-01

申请号：EP16847874.1

申请日：2016-07-11

申请人： Zhejiang Bossan Pharmaceutical Co. Ltd.

发明人： MA, Dawei ,  YU, Qiang ,  YUAN, Junying ,  XIA, Hongguang ,  CAI, Dongpo ,  WANG, Kailiang ,  ZHANG, Chen ,  XIA, Shanghua

IPC分类号： C07D401/12 ,  C07D401/14 ,  C07D405/14 ,  C07D239/48 ,  A61K31/506 ,  A61P35/00

CPC分类号： C07D401/14 ,  A61K31/506 ,  A61P35/00 ,  C07D239/48 ,  C07D401/12 ,  C07D405/14

摘要： The present invention provides an EGFR kinase inhibitor and a preparation method and use thereof. Specifically, the present invention provides a compound as shown in formula (I), the definition of each group therein being as described in the description. Said compound is an efficient EGFR inhibitor.

公开(公告)号：EP2694484B1

公开(公告)日：2018-07-18

申请号：EP12712666.2

申请日：2012-04-10

申请人： Janssen Sciences Ireland UC

发明人： MC GOWAN, David ,  RABOISSON, Pierre Jean-Marie Bernard ,  EMBRECHTS, Werner ,  JONCKERS, Tim, Hugo, Maria ,  LAST, Stefaan, Julien ,  PIETERS, Serge, Maria, Aloysius ,  VLACH, Jaromir

IPC分类号： C07D239/48 ,  C07D401/12 ,  C07D403/12 ,  C07D405/12 ,  C07D413/12 ,  C07D471/04 ,  A61K31/505 ,  A61K31/506

CPC分类号： A61K31/505 ,  A61K31/506 ,  A61K31/5377 ,  C07D239/48 ,  C07D401/12 ,  C07D403/12 ,  C07D405/12 ,  C07D413/12 ,  C07D471/04 ,  C07D487/04 ,  C07D495/04

摘要： This invention relates to pyrimidine derivatives, processes for their preparation, pharmaceutical compositions, and their use in treating viral infections such as HCV or HBV.

公开(公告)号：EP3239135A4

公开(公告)日：2018-07-11

申请号：EP15871995

申请日：2015-12-28

申请人： SHANGHAI INST MATERIA MEDICA CAS

发明人： SHEN JIANHUA ,  WANG YIPING ,  CHEN XINDE ,  XU WENWEI ,  WANG KAI

IPC分类号： C07D239/52 ,  A61K31/513 ,  A61K31/541 ,  A61P3/10 ,  A61P9/10 ,  A61P27/02 ,  C07D239/48 ,  C07D401/04 ,  C07D403/04 ,  C07D409/04

CPC分类号： C07D239/54 ,  A61K31/513 ,  A61K31/541 ,  C07D239/48 ,  C07D239/52 ,  C07D239/545 ,  C07D239/56 ,  C07D401/04 ,  C07D401/12 ,  C07D403/04 ,  C07D403/06 ,  C07D409/04 ,  C07D413/04

摘要： The present invention relates to pyrimidone compounds used as Lp-PLA 2 inhibitors and pharmaceutical compositions thereof. The structure of the pyrimidone compounds is represented by general formula (I), wherein R 1 , R 2 , R 3 , X, Ar, Y and n are defined as in the specification and claims. The compounds of general formula (I) in the present invention, stereoisomers and pharmaceutically acceptable salts thereof can be used as Lp-PLA 2 inhibitors for preventing, treating and/or ameliorating diseases associated with the activity of Lp-PLA 2 enzyme.

公开(公告)号：EP2271631B1

公开(公告)日：2018-07-04

申请号：EP09734422.0

申请日：2009-04-22

申请人： Portola Pharmaceuticals, Inc.

发明人： SONG, Yonghong ,  XU, Qing ,  BAUER, Shawn, M. ,  JIA, Zhaozhong, J. ,  MEHROTRA, Mukund ,  PANDEY, Anjali

IPC分类号： C07D239/48 ,  C07D401/04 ,  C07D401/14 ,  C07D403/04 ,  C07D471/04 ,  C07D473/16 ,  A61K31/506 ,  A61K31/52 ,  A61P9/00 ,  A61P29/00 ,  A61P35/00

CPC分类号： C07D471/04 ,  C07D239/48 ,  C07D401/04 ,  C07D401/14 ,  C07D403/04 ,  C07D403/14 ,  C07D473/16

摘要： The present invention is directed to compounds of formula I-II and pharmaceutically acceptable salts, esters, and prodrugs thereof which are inhibitors of syk and/or JAK kinase. The present invention is also directed to intermediates used in making such compounds, the preparation of such a compound, pharmaceutical compositions containing such a compound, methods of inhibition syk and/or JAK kinase activity, methods of inhibition the platelet aggregation, and methods to prevent or treat a number of conditions mediated at least in part by syk and/or JAK kinase activity, such as undesired thrombosis and Non Hodgkin's Lymphoma.

公开(公告)号：EP3328496A1

公开(公告)日：2018-06-06

申请号：EP16833717.8

申请日：2016-08-02

申请人： H. Lee Moffitt Cancer Center And Research Institute, Inc.

发明人： MAHAJAN, Nupam P. ,  MAHAJAN, Kiran N. ,  LAWRENCE, Nicholas J. ,  LAWRENCE, Harshani R.

IPC分类号： A61P35/00 ,  A61K31/506 ,  C07D239/02

CPC分类号： C07D405/12 ,  A61P35/00 ,  C07D239/48 ,  C07D401/12 ,  C07D403/12 ,  C07D405/14

摘要： Described are cancer therapies and anti-cancer compounds. In particular, disclosed are inhibitors of ACK1 tyrosine kinase and their use in the treatment of cancer. Methods of screening for new ACK1 tyrosine kinase inhibitors are also disclosed. In specific example, compound having Formula I are disclosed.

公开(公告)号：EP3274345A1

公开(公告)日：2018-01-31

申请号：EP16713818.9

申请日：2016-03-24

申请人： Fraunhofer-ges. zur Förderung der Angewandten Forschung E.V. ,  Yissum Research and Development Company of the Hebrew University of Jerusalem Ltd.

发明人： BURGER-KENTISCHER, Anke ,  MATTES, Angela ,  ZATSEPIN, Maria ,  GOLDBLUM, Amriam

IPC分类号： C07D405/14 ,  C07D405/04 ,  G01N33/00 ,  C07D231/12 ,  C07D401/04 ,  C07D401/10 ,  C07D401/12 ,  C07D235/30 ,  C07D239/48 ,  C07D239/94 ,  C07D413/12 ,  C07D471/04 ,  C07D295/13

CPC分类号： C07D405/04 ,  C07D231/12 ,  C07D235/30 ,  C07D239/48 ,  C07D239/94 ,  C07D295/13 ,  C07D401/04 ,  C07D401/10 ,  C07D401/12 ,  C07D405/14 ,  C07D413/12 ,  C07D471/04 ,  G01N2333/70596 ,  G01N2500/04

摘要： The present invention relates to a compound or a pharmaceutically acceptable salt thereof or a solvate thereof or a pharmaceutical composition comprising said compound, a process for obtaining or screening for a toll-like receptor 9 (TLR9) antagonist and a toll-like receptor 9 (TLR9) antagonist or a pharmaceutically acceptable salt thereof or a solvate thereof, preferably being obtainable thereby.

公开(公告)号：EP3239135A1

公开(公告)日：2017-11-01

申请号：EP15871995.5

申请日：2015-12-28

申请人： Shanghai Institute Of Materia Medica Chinese Academy of Sciences

发明人： SHEN, Jianhua ,  WANG, Yiping ,  CHEN, Xinde ,  XU, Wenwei ,  WANG, Kai

IPC分类号： C07D239/52 ,  C07D239/48 ,  C07D403/04 ,  C07D401/04 ,  C07D409/04 ,  A61K31/513 ,  A61K31/541 ,  A61P9/10 ,  A61P3/10 ,  A61P27/02

CPC分类号： C07D239/54 ,  A61K31/513 ,  A61K31/541 ,  C07D239/48 ,  C07D239/52 ,  C07D239/545 ,  C07D239/56 ,  C07D401/04 ,  C07D401/12 ,  C07D403/04 ,  C07D403/06 ,  C07D409/04 ,  C07D413/04

摘要： The present invention relates to pyrimidone compounds used as Lp-PLA 2 inhibitors and pharmaceutical compositions thereof. The structure of the pyrimidone compounds is represented by general formula (I), wherein R 1 , R 2 , R 3 , X, Ar, Y and n are defined as in the specification and claims. The compounds of general formula (I) in the present invention, stereoisomers and pharmaceutically acceptable salts thereof can be used as Lp-PLA 2 inhibitors for preventing, treating and/or ameliorating diseases associated with the activity of Lp-PLA 2 enzyme.

摘要翻译： 本发明涉及用作Lp-PLA2抑制剂的嘧啶酮化合物及其药物组合物。 嘧啶酮化合物的结构由通式（I）表示，其中R 1，R 2，R 3，X，Ar，Y和n如说明书和权利要求书中所定义。 本发明的通式（I）的化合物，其立体异构体和药学上可接受的盐可以用作Lp-PLA2抑制剂，用于预防，治疗和/或改善与Lp-PLA2酶的活性有关的疾病。

公开(公告)号：EP3218358A1

公开(公告)日：2017-09-20

申请号：EP15791315.3

申请日：2015-11-10

申请人： PIQUR Therapeutics AG ,  Universität Basel

发明人： CMILJANOVIC, Vladimir ,  HEBEISEN, Paul ,  BEAUFILS, Florent ,  BOHNACKER, Thomas ,  RAGEOT, Denise ,  SELE, Alexander ,  WYMANN, Matthias ,  LANGLOIS, Jean-Baptiste

IPC分类号： C07D239/48 ,  C07D401/04 ,  C07D401/14 ,  C07D403/04 ,  C07D405/14 ,  C07D413/14 ,  C07D491/048 ,  C07D491/056 ,  C07D491/20 ,  C07D498/08 ,  C07D519/00 ,  A61K31/53 ,  A61K31/506 ,  A61P35/00

CPC分类号： C07D401/04 ,  C07D239/48 ,  C07D401/14 ,  C07D403/04 ,  C07D405/14 ,  C07D413/14 ,  C07D491/048 ,  C07D491/056 ,  C07D491/20 ,  C07D498/08 ,  C07D519/00

摘要： The invention relates to novel phosphoinositide 3-kinase (PI3K),mammalian target of rapamycin (mTOR)and PI3K-related kinase(PIKKs)inhibitor compounds of formula (I), wherein X1, X2 and X3 are N or CH, with the proviso that at least two of X1, X2 and X3 are N; Y is N or CH, These compounds are useful, either alone or in combination with further therapeutic agents, for treating disorders mediated by lipid kinases.

摘要翻译： 本发明涉及式（I）的新型磷酸肌醇3-激酶（PI3K），哺乳动物雷帕霉素靶标（mTOR）和PI3K相关激酶（PIKKs）抑制剂化合物，其中X1，X2和X3是N或CH，条件是 X1，X2和X3中至少两个是N; Y是N或CH，这些化合物可单独使用或与另外的治疗剂组合使用，用于治疗由脂质激酶介导的病症。

公开(公告)号：EP3113779A4

公开(公告)日：2017-09-20

申请号：EP15757776

申请日：2015-03-05

申请人： CELGENE AVILOMICS RES INC

发明人： WESTLIN WILLIAM FREDERICK III ,  RINGHEIM GARTH

IPC分类号： A61K31/505 ,  A61P29/00 ,  A61P37/00 ,  C07D239/48

CPC分类号： A61K31/505 ,  A61K9/1652 ,  C07D239/48

摘要： The present invention provides methods of treating, stabilizing or lessening the severity or progression of a disease or disorder associated with Bruton's tyrosine kinase (BTK) TEC and interleukin-2-inducible T-cell kinase (ITK).

摘要翻译： 本发明提供治疗，稳定或减轻与布鲁顿酪氨酸激酶（BTK）TEC和白细胞介素-2诱导型T细胞激酶（ITK）相关的疾病或病症的严重性或进展的方法。