公开(公告)号：EP3466937A1

公开(公告)日：2019-04-10

申请号：EP17806522.3

申请日：2017-05-25

申请人： Canon Kabushiki Kaisha

发明人： NISHIDE Yosuke ,  YAMADA Naoki ,  OHRUI Hiroki ,  IWAWAKI Hironobu ,  SHIOBARA Satoru ,  YAMAGUCHI Tomona ,  TAKAHASHI Tetsuo ,  ITABASHI Masumi ,  MIYASHITA Hirokazu ,  KAMATANI Jun

IPC分类号： C07D307/93 ,  C07D333/78 ,  C07D409/06 ,  C07D409/12 ,  C07D491/048 ,  C07D495/04 ,  H01L27/146 ,  H01L51/42

摘要： The present invention provides an organic compound represented by general formula [1] described in claims. In general formula [1], Ar 1 and Ar 2 are each independently selected from an aryl group having 6 or more and 18 or less carbon atoms and a heteroaryl group having 3 or more and 15 or less carbon atoms. In general formula [1], R 1 to R 3 are each a hydrogen atom or a substituent. R 4 is an electron-withdrawing substituent. X 1 is oxygen or sulfur. Y 1 to Y 3 are each independently selected from a carbon atom and a nitrogen atom.

公开(公告)号：EP3052492B1

公开(公告)日：2019-03-27

申请号：EP14781644.1

申请日：2014-10-03

申请人： Cancer Research Technology Limited

发明人： JONES, Keith ,  RYE, Carl ,  CHESSUM, Nicola ,  CHEESEMAN, Matthew ,  PASQUA, Adele Elisa ,  PIKE, Kurt Gordon ,  FAULDER, Paul Frank

IPC分类号： C07D405/14 ,  C07D405/12 ,  C07D407/12 ,  C07D409/12 ,  C07D417/12 ,  C07D417/14 ,  C07D471/04 ,  C07D487/08 ,  C07D491/056 ,  A61P35/00 ,  A61K31/357 ,  A61K31/404 ,  A61K31/428 ,  A61K31/436 ,  C07D319/18

公开(公告)号：EP2838893B1

公开(公告)日：2019-03-13

申请号：EP13719444.5

申请日：2013-04-18

申请人： Bayer CropScience AG

发明人： BRAUN, Christoph ,  CRISTAU, Pierre ,  DAHMEN, Peter ,  DESBORDES, Philippe ,  ES-SAYED, Mazen ,  LACHAISE, Hélène ,  RINOLFI, Philippe ,  SCHMIDT, Jan-Peter ,  TSUCHYIA, Tomoki ,  VORS, Jean-Pierre ,  WACHENDORFF-NEUMANN, Ulrike

IPC分类号： C07D403/12 ,  C07D405/12 ,  C07D409/12 ,  A01N43/10

公开(公告)号：EP3061749B1

公开(公告)日：2019-02-27

申请号：EP14855498.3

申请日：2014-10-23

申请人： Chugai Seiyaku Kabushiki Kaisha

发明人： MURATA, Takeshi ,  HARA, Sousuke ,  NIIZUMA, Satoshi ,  HADA, Kihito ,  KAWADA, Hatsuo ,  SAKAITANI, Masahiro ,  SHIMADA, Hideaki ,  NAKANISHI, Yoshito

IPC分类号： C07D403/12 ,  C07D217/24 ,  C07D401/06 ,  C07D401/12 ,  C07D403/06 ,  C07D403/14 ,  C07D405/04 ,  C07D405/12 ,  C07D409/12 ,  C07D239/90 ,  A61K31/517 ,  A61K31/519 ,  A61P11/00 ,  A61P35/00 ,  A61P35/04

公开(公告)号：EP3189047B1

公开(公告)日：2018-12-26

申请号：EP15763756.2

申请日：2015-09-03

申请人： Bristol-Myers Squibb Company

发明人： SHI, Jun ,  EWING, William R. ,  NIELSEN, Laura ,  HU, Zilun ,  QUAN, Mimi L.

IPC分类号： C07D403/12 ,  C07D401/06 ,  C07D401/12 ,  C07D403/06 ,  C07D409/12 ,  A61K31/395 ,  A61P7/02

CPC分类号： C07D409/12 ,  C07D401/06 ,  C07D401/12 ,  C07D403/06 ,  C07D403/12

摘要： The present invention provides compounds of Formula (I) or stereoisomers, tautomers, or pharmaceutically acceptable salts thereof, wherein all the variables are as defined herein. These compounds are selective Factor XIa inhibitors or dual inhibitors of FXIa and plasma kallikrein. This invention also relates to pharmaceutical compositions comprising these compounds and methods of treating thromboembolic and/or inflammatory disorders using the same.

公开(公告)号：EP3411370A1

公开(公告)日：2018-12-12

申请号：EP17702109.4

申请日：2017-01-31

申请人： Hexal AG

发明人： BORN, Max ,  LANGES, Christoph ,  LENGAUER, Hannes

IPC分类号： C07D409/12 ,  A61K31/4704 ,  A61K31/496 ,  A61P25/18 ,  A61P25/24 ,  A61P25/28

CPC分类号： C07D409/12

摘要： The present invention relates to a brexpiprazole dihydrate crystalline form having a particle size distribution of d50 of at most 10 µm and less than 5% w/w of brexpiprazole anhydrate . The present invention also relates to a process for preparing this brexpiprazole dihydrate crystalline form and to pharmaceutical compositions thereof. The present invention also relates to a process for determining the absence of brexpiprazole anhydrate in this brexpiprazole dihydrate crystalline form. This brexpiprazole dihydrate crystalline form is used for the preparation of pharmaceutical compositions having delayed release properties upon intramuscular injection .

公开(公告)号：EP3395814A1

公开(公告)日：2018-10-31

申请号：EP18177131.2

申请日：2014-10-23

申请人： Blueprint Medicines Corporation

发明人： BIFULCO, Neil Jr. ,  DIPIETRO, Lucian V. ,  HODOUS, Brian L. ,  MIDUTURU, Chandrasekhar V.

IPC分类号： C07D403/12 ,  C07D401/04 ,  C07D401/12 ,  C07D235/30 ,  C07D405/12 ,  C07D403/14 ,  C07D409/12 ,  A61K31/498 ,  A61P35/00 ,  C07D239/84 ,  C07D471/04 ,  C07D475/00

CPC分类号： C07D401/04 ,  C07D235/30 ,  C07D239/84 ,  C07D401/12 ,  C07D403/12 ,  C07D403/14 ,  C07D405/12 ,  C07D409/12 ,  C07D471/04 ,  C07D475/00

摘要： Described herein are inhibitors of FGFR-4, pharmaceutical compositions including such compounds, and methods of using such compounds and compositions.

公开(公告)号：EP2747570B1

公开(公告)日：2018-09-19

申请号：EP12750774.7

申请日：2012-08-24

申请人： Syngenta Participations AG

发明人： CASSAYRE, Jérôme Yves ,  RENOLD, Peter ,  PITTERNA, Thomas ,  EL QACEMI, Myriem

IPC分类号： A01N43/50 ,  C07D331/04 ,  C07D409/12 ,  C07D413/12 ,  C07D413/14

CPC分类号： A01N43/80 ,  A01N37/42 ,  A01N37/50 ,  A01N43/20 ,  A01N43/40 ,  A01N43/42 ,  C07D413/12 ,  C07D413/14 ,  C07F7/1804

摘要： The present invention provides compounds of formula (I) wherein G1 is oxygen; R1 is hydrogen; R2 is group (P) L is a bond, methylene or ethylene; one of A1 and A2 is S, SO or SO2 and the other is —C(R4)R4—; R3 is hydrogen or methyl; each R4 is independently hydrogen or methyl; Y2 and Y3 are independently CH or nitrogen, wherein Y2 and Y3 are not both nitrogen; X2 is C—X6 or nitrogen; X1, X3 and X6 are independently hydrogen, halogen or trihalomethyl, wherein at least two of X1, X3 and X6 are not hydrogen; X4 is trifluoromethyl, difluoromethyl or chlorodifluoromethyl. The invention also provides intermediates useful for the preparation of compounds of formula (I), as well as methods of controlling insects, acarines, nematodes or molluscs using the compounds of formula (I).

公开(公告)号：EP3372594A1

公开(公告)日：2018-09-12

申请号：EP16861623.3

申请日：2016-11-04

申请人： Humanwell Healthcare (Group) Co., Ltd.

发明人： WANG, Xuehai ,  XU, Yong ,  SHENG, Xijun ,  ZHANG, Xiaolin ,  XIA, Hangui ,  YANG, Zhongwen ,  YUE, Yang ,  HUANG, Lu ,  XIAO, Qiang

IPC分类号： C07D409/12 ,  C07D401/12 ,  C07D401/14 ,  C07D409/14 ,  C07D413/14 ,  C07D239/48 ,  A61K31/5377 ,  A61K31/506 ,  A61P35/00

CPC分类号： A61K31/506 ,  A61K9/0019 ,  A61K9/08 ,  A61K9/12 ,  A61K9/14 ,  A61K9/20 ,  A61K9/48 ,  A61K31/5377 ,  A61K45/06 ,  A61K2300/00 ,  A61P35/00 ,  C07D239/48 ,  C07D401/12 ,  C07D401/14 ,  C07D409/12 ,  C07D409/14 ,  C07D413/14

摘要： The present invention provides a pyrimidine derivative and a use thereof. The pyrimidine derivative is the compound shown in formula I or a pharmaceutically acceptable salt, hydrate, solvate, metabolite or prodrug thereof, wherein, R 1 , R 2 , R 3 , R 4 and R 5 are, for example, as defined in the specification. The compound can act as an ALK inhibitor, and is for preparing an anti-tumor medicament for suppressing an anaplastic lymphoma kinase.

公开(公告)号：EP3339307A8

公开(公告)日：2018-08-29

申请号：EP16382627.4

申请日：2016-12-20

申请人： Laboratorios del Dr. Esteve, S.A.

发明人： ALMANSA-ROSALES, Carmen ,  VIRGILI-BERNADÓ, Marina ,  ALONSO-XALMA, Monica

IPC分类号： C07D409/12 ,  C07D237/30 ,  C07D217/02 ,  A61K31/4709 ,  A61K31/4725 ,  A61K31/502 ,  A61K31/517 ,  A61P25/00 ,  A61P29/00

CPC分类号： C07D409/12 ,  A61P25/00 ,  A61P29/00 ,  C07D215/14 ,  C07D217/02 ,  C07D237/30

摘要： The present invention relates to new compounds of formula (I):

showing great affinity and activity towards the subunit α2δ of voltage-gated calcium channels (VGCC), especially the α2δ-1 subunit of voltage-gated calcium channels or dual activity towards the subunit α2δ of voltage-gated calcium channels (VGCC), especially the α2δ-1 subunit of voltage-gated calcium channels, and the noradrenaline transporter (NET).