公开(公告)号：EP4365178A1

公开(公告)日：2024-05-08

申请号：EP22832136.0

申请日：2022-06-29

申请人： Shanghai Allist Pharmaceuticals Co., Ltd.

发明人： LUO, Huibing ,  JIANG, Jiajun ,  WANG, Jiapo ,  ZHOU, Huayong

IPC分类号： C07D519/00 ,  C07F7/18 ,  C07D471/04 ,  C07C53/18 ,  C07C51/41 ,  A61K31/519 ,  A61P35/00 ,  A61P35/02

CPC分类号： A61K31/519 ,  A61P35/00 ,  A61P35/02 ,  C07C51/41 ,  C07C53/18 ,  C07D471/04 ,  C07D519/00 ,  C07F7/18

摘要： Disclosed in the present invention are a nitrogen-containing heterocyclic compound, and a preparation method therefor, an intermediate thereof, and an application thereof. The present invention provides a nitrogen-containing heterocyclic compound as represented by formula (I), a stereoisomer thereof, or a pharmaceutically acceptable salt thereof. The nitrogen-containing heterocyclic compound as represented by formula (I), the stereoisomer thereof, or the pharmaceutically acceptable salt thereof provided by the present invention has the activity of inhibiting proliferation of Ba/F3 KRAS-G12D cells, AGS cells, Ba/F3 KRAS-G12V cells expressing KRAS G12D and/or KRAS G12V mutant proteins, and also shows good in vivo tumor suppression activity; the present invention is expected to treat and/or prevent a variety of diseases mediated by KRAS G12D and/or KRAS G12V.

公开(公告)号：EP3245200A1

公开(公告)日：2017-11-22

申请号：EP16700075.1

申请日：2016-01-07

申请人： Boehringer Ingelheim International GmbH

发明人： HECKEL, Armin ,  FRATTINI, Sara ,  KLEY, Joerg

IPC分类号： C07D403/12 ,  C07D405/14 ,  C07D401/14 ,  C07D403/14 ,  A61K31/497 ,  A61P11/00

CPC分类号： C07D403/12 ,  A61K31/497 ,  A61K31/5377 ,  A61K31/551 ,  A61K31/675 ,  A61K45/06 ,  C07C53/18 ,  C07D401/14 ,  C07D403/14 ,  C07D405/14 ,  C07F9/650994

摘要： The present invention relates to compounds of formula (I) or the tautomers or pharmacologically acceptable acid addition salts thereof, characterized by a topological polar surface area value (TPSA) of at least 145, wherein R1, R2, R3, R4, X, and Z- have one of the meanings as defined in the specification, to the use of compounds of formula (I) as medicaments, to pharmaceutical compositions comprising at least one compound of formula (I), as well as to medicament combinations containing one or more compounds of formula (I). The compounds are ENaC inhibitors useful for the treatment of respiratory diseases and allergic diseases of the airways.

公开(公告)号：EP2240206B1

公开(公告)日：2017-03-22

申请号：EP09700768.6

申请日：2009-01-08

申请人： Lantheus Medical Imaging, Inc.

发明人： CESATI, Richard R. ,  HARRIS, Thomas D. ,  ROBINSON, Simon P. ,  LOOBY, Richard J. ,  CHEESMAN, Edward H. ,  YALAMANCHILI, Padmaja ,  CASEBIER, David S.

IPC分类号： A61K49/10 ,  A61K51/04 ,  C07C271/22 ,  C07D257/02 ,  C07D403/12 ,  C07D213/56 ,  C07C259/14 ,  C07D209/20 ,  C07C259/06 ,  C07C53/18

CPC分类号： C07D257/02 ,  A61K49/103 ,  A61K49/106 ,  A61K51/04 ,  C07C53/18 ,  C07C259/06 ,  C07C259/14 ,  C07C271/22 ,  C07C2601/14 ,  C07D209/20 ,  C07D213/56 ,  C07D403/12

公开(公告)号：EP3052099A4

公开(公告)日：2017-03-15

申请号：EP14850990

申请日：2014-09-29

申请人： MERCK SHARP & DOHME

发明人： BARR KENNETH JAY ,  SCOTT MARK E ,  THOMPSON CHRISTOPHER F ,  ANTHONY NEVILLE ,  CAMMARANO CAROLYN MICHELLE ,  BAKSHI RAMAN KUMAR ,  MOHANTY SUBHENDU KUMAR ,  KORAPALA CHANDRA SEKHAR ,  LATTHE PRASHANT R ,  KAMBAM VYJAYANTHI N ,  SARKAR SUJIT KUMAR ,  THATAI JAYANTH THIRUVELLORE

IPC分类号： A61K31/435 ,  A61K31/4439

CPC分类号： A61K31/4439 ,  A61K31/437 ,  A61K31/444 ,  A61K31/497 ,  A61K31/501 ,  A61K31/506 ,  A61K31/517 ,  A61K31/519 ,  A61K45/06 ,  C07B2200/07 ,  C07C53/06 ,  C07C53/18 ,  C07D207/08 ,  C07D207/09 ,  C07D401/06 ,  C07D401/12 ,  C07D401/14 ,  C07D403/12 ,  C07D413/14 ,  C07D471/04 ,  C07D495/04 ,  A61K2300/00

摘要： The present invention provides compounds of Formula (I), pharmaceutical compositions thereof, and method of using the same in the treatment or prevention of diseases mediated by the activation of β3-adrenoceptor.

公开(公告)号：EP2880026B1

公开(公告)日：2017-02-22

申请号：EP13747625.5

申请日：2013-08-02

申请人： Bristol-Myers Squibb Company

发明人： YANG, Wu ,  CORTE, James, R. ,  GILLIGAN, Paul, J. ,  PINTO, Donald, J.P., Pinto ,  EWING, William, R. ,  DILGER, Andrew, K. ,  WANG, Yufeng ,  FANG, Tianan ,  PABBISETTY, Kumar, B. ,  SMITH II, Leon, M.

IPC分类号： C07D401/04 ,  C07D471/08 ,  C07D487/08 ,  C07D487/18 ,  A61K31/439 ,  A61P7/00

CPC分类号： C07D471/08 ,  C07C53/18 ,  C07D401/04 ,  C07D471/18 ,  C07D487/08 ,  C07D487/18 ,  C07H17/02

摘要： The present invention provides compounds of Formula (X):(Formula (X), 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：EP2271658B1

公开(公告)日：2016-11-09

申请号：EP09732769.6

申请日：2009-04-20

申请人： Reata Pharmaceuticals, Inc.

发明人： JIANG, Xin ,  VISNICK, Melean ,  GREINER, Jack ,  LIU, Xiaofeng ,  SZUCS, Stephen, S.

IPC分类号： C07D317/28 ,  C07D257/04 ,  C07D261/08 ,  C07D493/08 ,  C07D209/48 ,  C07D303/36 ,  C07C255/47

CPC分类号： C07C255/47 ,  C07C53/18 ,  C07D209/48 ,  C07D257/04 ,  C07D261/08 ,  C07D303/36 ,  C07D317/28 ,  C07D493/08 ,  C07F9/09 ,  C07J63/008

公开(公告)号：EP3086790A1

公开(公告)日：2016-11-02

申请号：EP14875495.5

申请日：2014-10-10

申请人： Purdue Pharma LP

发明人： LOCKMAN, Jeffrey ,  TAFESSE, Laykea ,  PARK, Jae, Hyun ,  YOUNGMAN, Mark

IPC分类号： A61K31/485 ,  C07D221/08 ,  C07D471/08

CPC分类号： C07D221/28 ,  C07C53/18 ,  C07D221/08 ,  C07D471/08 ,  C07D491/18

摘要： The application is directed to compounds of Formula I or II: and pharmaceutically acceptable salts and solvates thereof, wherein R', R", R"' R
1 , R
2 , R
3 , R
4 , R
4a , and R
20 are defined as set forth in the specification. The invention is also directed to use of compounds of Formula I or II and the pharmaceutically acceptable salts and solvates thereof to treat disorders responsive to the modulation of one or more opioid receptors. Certain compounds of the invention are especially useful for treating pain.

摘要翻译： 本发明涉及式I或II化合物及其药学上可接受的盐和溶剂化物，其中R'，R“，R”'R 1，R 2，R 3，R 4，R 4a和R 20定义如说明书 。 本发明还涉及使用式I或II的化合物及其药学上可接受的盐和溶剂化物来治疗对一种或多种阿片受体调节作用的病症。 本发明的某些化合物特别适用于治疗疼痛。

公开(公告)号：EP3068758A1

公开(公告)日：2016-09-21

申请号：EP14861658.4

申请日：2014-11-14

申请人： The Wistar Institute Of Anatomy And Biology

发明人： MESSICK, Troy E. ,  SMITH, Garry R. ,  REITZ, Allen B. ,  LIEBERMAN, Paul M.

IPC分类号： C07C229/56

CPC分类号： C07D207/327 ,  C07C53/18 ,  C07C63/66 ,  C07C65/19 ,  C07C65/28 ,  C07C211/27 ,  C07C217/84 ,  C07C229/56 ,  C07C229/64 ,  C07C233/11 ,  C07C233/64 ,  C07C233/65 ,  C07C235/58 ,  C07C255/54 ,  C07C255/55 ,  C07C311/08 ,  C07C311/16 ,  C07C311/17 ,  C07C317/14 ,  C07C317/44 ,  C07C2601/02 ,  C07D207/08 ,  C07D207/12 ,  C07D207/14 ,  C07D207/16 ,  C07D209/08 ,  C07D211/70 ,  C07D213/55 ,  C07D213/64 ,  C07D213/74 ,  C07D215/14 ,  C07D231/12 ,  C07D235/06 ,  C07D239/26 ,  C07D249/06 ,  C07D277/30 ,  C07D295/155 ,  C07D307/79 ,  C07D333/54 ,  C07D401/04 ,  C07D401/10 ,  C07D403/10 ,  C07D409/10 ,  C07D417/10 ,  C07D471/04 ,  C07D487/04

摘要： The invention provides EBNA1 inhibitors, and pharmaceutical compositions comprising the same, that are useful for the treatment of diseases caused by EBNA1 activity such as, but not limited to, cancer, infectious mononucleosis, chronic fatigue syndrome, multiple sclerosis, systemic lupus erythematosus and/or rheumatoid arthritis. The compounds and compositions of the invention are further useful for the treatment of diseases caused by latent Epstein-Barr Virus (EBV) infection. The compounds and compositions of the invention are further useful for the treatment of diseases caused by lytic EBV infection.

摘要翻译： 本发明提供EBNA1抑制剂及其组合物，其可用于治疗由EBNA1活性引起的疾病，例如但不限于癌症，感染性单核细胞增多症，慢性疲劳综合征，多发性硬化症，系统性红斑狼疮和/ 或类风湿性关节炎。 本发明的化合物和组合物还可用于治疗潜伏性EB病毒（EBV）感染引起的疾病。 本发明的化合物和组合物还可用于治疗由溶血性EBV感染引起的疾病。

公开(公告)号：EP3057943A1

公开(公告)日：2016-08-24

申请号：EP14790956.8

申请日：2014-10-16

申请人： Eisai R&D Management Co., Ltd.

发明人： REYNOLDS, Dominic ,  HAO, Ming-Hong ,  WANG, John ,  PRAJAPATI, Sudeep ,  SATOH, Takashi ,  SELVARAJ, Anand

IPC分类号： C07D239/48 ,  C07D405/12 ,  C07D413/12 ,  A61K31/505 ,  A61P35/00

CPC分类号： A61K31/505 ,  A61K31/506 ,  A61K31/5377 ,  C07C53/18 ,  C07D239/48 ,  C07D401/12 ,  C07D403/12 ,  C07D405/12 ,  C07D413/12

摘要： Provided herein are compounds of Formula I useful as FGFR4 inhibitors, as well as methods of use of the same.

摘要翻译： 本文提供了可用作FGFR4抑制剂的式I化合物，以及其用途的方法。

公开(公告)号：EP3031791A1

公开(公告)日：2016-06-15

申请号：EP14197236.4

申请日：2014-12-10

申请人： Solvay SA

发明人： The designation of the inventor has not yet been filed

IPC分类号： C07C17/02 ,  C07C51/58

CPC分类号： C07C51/58 ,  C07C17/04 ,  C07C53/18 ,  C07C19/12

摘要： The present invention concerns a halogenation process, in which a 1,1-dihaloethene CX2=CH2 (I) with at least one halogenation agent. The invention concerns further a process for the manufacture of chlorodifluoroacetic acid chloride (CDFAC), which comprise the steps of (a) chlorination of VF2, and (b) an oxidation process. Another object of the present invention is a process for the manufacture of agriculturally or pharmaceutically active compounds, comprising the halogenation and/or oxidation process.

摘要翻译： 本发明涉及一种卤化方法，其中1,1-二卤乙烯CX 2 = CH 2（I）与至少一种卤化剂。 本发明进一步涉及氯二氟乙酰氯（CDFAC）的制备方法，其包括以下步骤：（a）将VF2氯化，和（b）氧化方法。 本发明的另一个目的是制备包含卤化和/或氧化方法的农业或药物活性化合物的方法。