公开(公告)号：EP4410291A3

公开(公告)日：2024-08-14

申请号：EP24164213.1

申请日：2019-05-08

申请人： DIZAL (JIANGSU) PHARMACEUTICAL CO., LTD.

发明人： LI, Zhengtao ,  ZHONG, Wei ,  WANG, Jiabing ,  ZENG, Qingbei ,  TSUI, Honchung ,  YANG, Zhenfan ,  ZHANG, Xiaolin

IPC分类号： C07D409/12 ,  A61P35/00 ,  C07D401/14 ,  C07D471/04 ,  A61K31/517

CPC分类号： A61P35/00 ,  C07D471/04 ,  C07D401/14 ,  A61K45/06

摘要： Disclosed are compounds inhibiting ErbBs (e.g. HER2), pharmaceutically acceptable salts, hydrates, solvates or stereoisomers thereof and pharmaceutical compositions comprising the compounds. The compound and the pharmaceutical composition can effectively treat diseases associated ErbBs (especially HER2), including cancer.

公开(公告)号：EP4371562A3

公开(公告)日：2024-08-14

申请号：EP24150698.9

申请日：2018-05-25

申请人： Cancer Research Technology Limited ,  The Institute of Cancer Research: Royal Cancer Hospital

发明人： BELLENIE, Benjamin Richard ,  CHEUNG, Kwai Ming Jack ,  DAVIS, Owen Alexander ,  HOELDER, Swen ,  HUCKVALE, Rosemary ,  LLOYD, Matthew Garth

IPC分类号： C07D403/12 ,  C07D413/14 ,  C07D215/42 ,  C07D401/12 ,  C07D403/14 ,  C07D407/14 ,  C07D413/12 ,  A61P35/00 ,  A61K31/4704

CPC分类号： C07D403/12 ,  C07D413/14 ,  C07D215/42 ,  C07D401/12 ,  C07D403/14 ,  C07D407/14 ,  C07D413/12 ,  A61P35/00

摘要： The present invention relates to compounds of formula I that function as inhibitors of BCL6 (B-cell lymphoma 6) activity:

wherein X1, X2, X3, R1, R2, R3, R4 and R5 are each as defined herein. The present invention also relates to processes for the preparation of these compounds, to pharmaceutical compositions comprising them, and to their use in the treatment of proliferative disorders, such as cancer, as well as other diseases or conditions in which BCL6 activity is implicated.

公开(公告)号：EP3865476B1

公开(公告)日：2024-08-14

申请号：EP21150116.8

申请日：2015-08-24

IPC分类号： C07D215/22 ,  A61K31/496 ,  A61P25/18 ,  C07D401/12

CPC分类号： A61K31/496 ,  A61P25/18 ,  C07D215/22

公开(公告)号：EP4410794A1

公开(公告)日：2024-08-07

申请号：EP22884768.7

申请日：2022-07-21

申请人： China Pharmaceutical University

发明人： WU, Xiaoxing ,  CHEN, Xiaoyu ,  LI, Wenqiang ,  SHU, Chengxia ,  LUO, Guangmei ,  YANG, Kexin

IPC分类号： C07D487/04 ,  C07D401/04 ,  C07D401/14 ,  C07D405/14 ,  C07D491/107 ,  C07D241/26 ,  C07D241/02 ,  A61K31/497 ,  A61P35/00

CPC分类号： A61K31/497 ,  A61K31/506 ,  A61K31/519 ,  A61K31/55 ,  A61P35/00 ,  C07D241/02 ,  C07D241/26 ,  C07D401/04 ,  C07D401/14 ,  C07D405/14 ,  C07D487/04 ,  C07D491/107 ,  C07D519/00

摘要： The present invention belongs to the field of medicinal chemistry, and particularly relates to synthesis, a preparation method and the use of an inhibitor containing dual targets SHP2 and CDK4/6, wherein the inhibitor comprises three compounds of general formulas I-III and pharmaceutically acceptable salts, enantiomers, diastereomers, tautomers, solvates, polymorphs or prodrugs thereof. According to the present invention, a class of brand-new SHP2 and CDK4/6 dual-target inhibitors are prepared by means of a pharmacophore fusion and reasonable drug design method, so that the problems of drug resistance, poor drug effect, etc., of the existing SHP2 inhibitor and CDK4/6 inhibitor are solved; the great significance of the present invention is providing the first SHP2 and CDK4/6 dual-target inhibitor, which provides a basis for solving the problem of drug resistance of kinase and phosphatase in the later period; in addition, the embodiments of the present invention prove that the SHP2 inhibitor and the CDK4/6 inhibitor have a synergistic effect, which provides a theoretical support for the subsequent development of SHP2 dual-target inhibitors.

公开(公告)号：EP4410792A1

公开(公告)日：2024-08-07

申请号：EP22875192.1

申请日：2022-09-30

申请人： Xizang Haisco Pharmaceutical Co., Ltd.

发明人： LI, Yao ,  ZHANG, Haoliang ,  CHEN, Lei ,  FANG, Linyong ,  WANG, Long ,  LUO, Yufeng ,  TANG, Pingming ,  YU, Yan ,  ZHANG, Chen ,  YAN, Pangke

IPC分类号： C07D471/04 ,  C07D401/14 ,  A61K31/496 ,  A61K31/4375 ,  A61P35/00

CPC分类号： C07D401/14 ,  A61P35/00 ,  A61K31/4375 ,  C07D471/04 ,  A61K31/496

摘要： Provided are a compound represented by formula (1), a stereoisomer, pharmaceutically acceptable salt, solvate, and eutectic or deuterated compound thereof, or a pharmaceutical composition comprising same, and a use thereof as a PARP-1 inhibitor in the preparation of a medication for treating related diseases. Each group in formula (I) is as defined in the description.

公开(公告)号：EP4410777A1

公开(公告)日：2024-08-07

申请号：EP22872243.5

申请日：2022-09-27

申请人： CHIA TAI TIANQING PHARMACEUTICAL GROUP CO., LTD.

发明人： FENG, Fan ,  YU, Ding ,  ZHANG, Xiquan ,  WANG, Yueting

IPC分类号： C07D231/56 ,  C07D401/14 ,  C07D403/14 ,  A61K31/416 ,  A61K31/44 ,  A61K31/445 ,  A61K31/506 ,  A61P35/00

CPC分类号： A61K31/416 ,  A61K31/445 ,  A61K31/44 ,  A61K31/506 ,  A61P35/00 ,  C07D231/56 ,  C07D401/14 ,  C07D403/14

摘要： The present disclosure relates to a combined pharmaceutical composition of a CDK4/6 inhibitor and an aromatase inhibitor, and the use thereof in the treatment of breast cancer. Compared with separate administration of any agent in the composition, the combined pharmaceutical composition of the present disclosure yields a better therapeutic effect on slowing tumor growth or even eliminating tumors.

公开(公告)号：EP3786157B1

公开(公告)日：2024-08-07

申请号：EP18916025.2

申请日：2018-12-25

IPC分类号： C07D249/06 ,  C07D401/12 ,  C07D405/12 ,  C07D403/10 ,  A61P35/02 ,  A61K31/496 ,  A61K31/5377 ,  A61K31/551

CPC分类号： A61P35/02 ,  C07D403/10 ,  C07D249/06 ,  C07D401/12 ,  C07D405/12 ,  A61K31/496 ,  A61K31/5377 ,  A61K31/551

公开(公告)号：EP4405345A2

公开(公告)日：2024-07-31

申请号：EP22873290.5

申请日：2022-09-21

申请人： Nanyang Technological University

发明人： GRÜBER, Gerhard ,  SHIN, Joon ,  AMARAVADHI, Venkata Krishna Harikishore ,  WONG, Chui Fann ,  RAGUNATHAN, Priya

IPC分类号： C07D401/12 ,  A61K31/4402 ,  A61P31/04 ,  G16C20/64

CPC分类号： A61P31/04 ,  C07D401/12 ,  G16C20/30 ,  A61K45/06

公开(公告)号：EP4405344A2

公开(公告)日：2024-07-31

申请号：EP22793913.9

申请日：2022-09-23

申请人： Xenon Pharmaceuticals Inc.

发明人： BURFORD, Kristen ,  LOFSTRAND, Verner ,  KIM, Jung Yun ,  CLEMENT, Helen ,  CHARIFSON, Paul ,  CLARK, Michael

IPC分类号： C07D401/12 ,  C07D405/04 ,  C07D413/14 ,  C07D405/14 ,  C07D401/14 ,  C07D405/12 ,  A61K31/4433 ,  A61K31/444 ,  A61K31/4439 ,  A61K31/443 ,  A61K31/506 ,  A61P25/08

CPC分类号： C07D401/12 ,  C07D405/04 ,  C07D413/14 ,  C07D405/14 ,  C07D401/14 ,  C07D405/12

公开(公告)号：EP3601239B1

公开(公告)日：2024-07-31

申请号：EP18770877.1

申请日：2018-03-23

IPC分类号： C07D401/14 ,  C07D491/107 ,  C07D495/10 ,  C07D471/20 ,  A61K31/497 ,  A61P35/00 ,  C07D405/14 ,  C07D491/113 ,  C07D491/20 ,  C07D513/10 ,  C07F9/6558 ,  C07D471/10

CPC分类号： C07D471/10 ,  A61P35/00 ,  C07D401/14 ,  C07D471/20 ,  C07D495/10 ,  C07D491/107 ,  C07D491/113 ,  C07D491/20 ,  C07D513/10 ,  C07D405/14 ,  C07F9/65583