公开(公告)号：EP3371175A2

公开(公告)日：2018-09-12

申请号：EP16854241.3

申请日：2016-10-05

申请人： Epizyme Inc ,  The Regents of the University of Colorado, a body corporate

发明人： KEILHACK, Heike ,  WATERS, Nigel, J. ,  VIBHAKAR, Rajeev

IPC分类号： C07D405/14 ,  C07D211/86 ,  C07D405/12

CPC分类号： A61K31/501 ,  A61K31/4412 ,  A61K31/4436 ,  A61K31/4468 ,  A61K31/4545 ,  A61K31/496 ,  A61K31/5377

摘要： The disclosure provides a method of treating a medulloblastoma in a subject in need thereof comprising administering to the subject a therapeutically-effective amount of an enhancer of a zeste homolog 2 (EZH2) inhibitor. In a preferred embodiment of this method, the subject is pediatric and the EZH2 inhibitor is Tazemetostat.

公开(公告)号：EP3360870A1

公开(公告)日：2018-08-15

申请号：EP18156411.3

申请日：2014-02-12

申请人： Novartis AG

发明人： BURKS, Heather Elizabeth ,  DECHANTSREITER, Michael A. ,  HE, Guo ,  NUNEZ, Jill ,  PEUKERT, Stefan ,  SPRINGER, Clayton ,  SUN, Yingchuan ,  THOMSEN, Noel Marie-France ,  TRIA, George Scott ,  YU, Bing

IPC分类号： C07D333/64 ,  C07D333/66 ,  C07D409/04 ,  C07D409/10 ,  C07D409/12 ,  C07D413/04 ,  C07D413/12 ,  C07D417/12 ,  A61K31/381 ,  A61P35/00

CPC分类号： A61K31/381 ,  A61K31/397 ,  A61K31/4025 ,  A61K31/404 ,  A61K31/41 ,  A61K31/4196 ,  A61K31/422 ,  A61K31/4245 ,  A61K31/428 ,  A61K31/4436 ,  A61K31/4745 ,  A61K31/506 ,  A61K31/5377 ,  A61K45/06 ,  A61P35/00 ,  C07D333/64 ,  C07D333/66 ,  C07D409/04 ,  C07D409/10 ,  C07D409/12 ,  C07D413/04 ,  C07D413/12 ,  C07D417/12

摘要： The present invention relates to compounds of formula I:

in which n, m, X, Y 1 , R 1 , R 2 , R 3 , R 4 and R 5 are defined in the Summary of the Invention; capable of being both potent antagonists and degraders of estrogen receptors. The invention further provides a process for the preparation of compounds of the invention, pharmaceutical preparations comprising such compounds and methods of using such compounds and compositions in the management of diseases or disorders associated with aberrant estrogen receptor activity.

公开(公告)号：EP3360554A1

公开(公告)日：2018-08-15

申请号：EP16853620.9

申请日：2016-10-05

申请人： Toyama Chemical Co., Ltd. ,  Public University Corporation Nagoya City University

发明人： SHIMANE, Kazuki ,  TANAKA, Yasuhito

IPC分类号： A61K31/4439 ,  A61K31/4422 ,  A61K31/443 ,  A61K31/4436 ,  A61P1/16 ,  A61P31/20

CPC分类号： C07D409/04 ,  A61K31/4422 ,  A61K31/443 ,  A61K31/4436 ,  A61K31/4439 ,  A61P31/20 ,  C07D213/80 ,  C07D405/10 ,  C07D409/10

摘要： An anti-hepatitis B virus agent comprising a compound represented by general formula [1],

wherein R 1 represents an aryl group, which may be substituted, or the like; R 2 represents an aryl group, which may be substituted, or the like; and R 3 represents a hydrogen atom or the like; or a salt thereof.

公开(公告)号：EP2400951B1

公开(公告)日：2018-08-15

申请号：EP10745727.7

申请日：2010-02-24

申请人： Mayne Pharma LLC

发明人： LOUPENOK, Leon

IPC分类号： A61K45/06 ,  A61K31/00 ,  A61K31/192 ,  A61K31/203 ,  A61K31/4436 ,  A61K9/00 ,  A61K9/107 ,  A61K9/12

CPC分类号： A61K31/203 ,  A61K9/0014 ,  A61K9/1075 ,  A61K9/122 ,  A61K31/00 ,  A61K31/192 ,  A61K31/4436 ,  A61K45/06 ,  Y10S514/938 ,  Y10S514/939 ,  Y10S514/941 ,  Y10S514/945 ,  A61K2300/00

摘要： The present invention relates to a novel oil in water emulsion aerosol foam composition containing an active agent for the treatment of various chronic and acute skin conditions, particularly acne and psoriasis; and processes for preparing the emulsion aerosol foam compositions. In particular, the present invention relates to oil in water emulsion aerosol foam compositions containing a retinoid in the oil phase.

公开(公告)号：EP3347462A1

公开(公告)日：2018-07-18

申请号：EP16845050.0

申请日：2016-09-08

申请人： Lau, Warren C.

发明人： Lau, Warren C.

IPC分类号： C12N9/12 ,  A61K38/45

CPC分类号： A61K31/497 ,  A61K31/44 ,  A61K31/4436 ,  A61K31/444 ,  A61K31/496 ,  A61K31/4965 ,  A61K31/4985 ,  A61K31/5025 ,  A61K31/519 ,  A61K31/5377 ,  C07K2319/23 ,  C12N9/12 ,  C12N9/1205 ,  C12Y207/10002

摘要： The present invention provides methods for inhibiting Fyn kinase, using 5-3-pyridin-2-amine, 6-3-imidazo[1,2-a] pyrazine, 6-3-imidazo[1,2-b] pyridazine, N-(5-imidazo [2,1-b][1,3,4] thiadiazol-2-yl)-amine, 4-3-1H-pyrazolo[3,4-b] pyridine, and N-(3-imidazo [1,2-b] pyridazin-6-yl) amine compounds and methods of treatment, prevention, inhibition or amelioration of diseases and conditions associated with Fyn kinase using such compounds.

公开(公告)号：EP3344618A1

公开(公告)日：2018-07-11

申请号：EP16757904.4

申请日：2016-08-30

申请人： Bayer Pharma Aktiengesellschaft

发明人： JIMENEZ, Nunez Eloisa ,  ACKERSTAFF, Jens ,  ELLERBROCK, Pascal ,  HILLISCH, Alexander ,  MEIER, Katharina ,  HEITMEIER, Stefan ,  TERSTEEGEN, Adrian ,  STAMPFUSS, Jan

IPC分类号： C07D403/12 ,  C07D405/14 ,  C07D413/14 ,  A61K31/4412 ,  A61K31/4433 ,  A61K31/4436 ,  A61K31/4439 ,  A61K31/444 ,  C07D401/12 ,  C07D403/06 ,  C07D403/14 ,  C07D405/06 ,  C07D409/12 ,  C07D409/14 ,  C07D487/04 ,  C07D213/69 ,  A61P7/00 ,  A61P9/00

CPC分类号： A61K31/4412 ,  A61K31/4433 ,  A61K31/4436 ,  A61K31/4439 ,  A61K31/444 ,  A61P1/00 ,  A61P7/02 ,  A61P27/02 ,  C07D213/69 ,  C07D401/12 ,  C07D403/06 ,  C07D403/12 ,  C07D403/14 ,  C07D405/06 ,  C07D405/14 ,  C07D409/12 ,  C07D409/14 ,  C07D413/14 ,  C07D487/04

摘要： The invention relates to substituted oxopyridine derivatives and methods for the production thereof, as well as to the use thereof in the production of medicaments for treating and/or preventing diseases, especially diseases of the cardiovascular system, preferably thrombotic or thromboembolic diseases, as well as oedemas, and also ophthalmological diseases.

公开(公告)号：EP3192794A4

公开(公告)日：2018-06-27

申请号：EP15839901

申请日：2015-09-10

申请人： SHIONOGI & CO

发明人： KAWASUJI TAKASHI ,  MIKAMIYAMA HIDENORI ,  SUZUKI NAOYUKI ,  MASUDA KOJI ,  SUGIMOTO HIDEKI ,  OKANO AZUSA ,  YOSHIDA MIHO ,  SUGIYAMA SHUICHI ,  ASAHI KENTAROU ,  KOZONO IORI ,  MIYAZAKI KEISUKE ,  OZASA HIROKI ,  MIYAGAWA MASAYOSHI

IPC分类号： C07D231/56 ,  A61K31/381 ,  A61K31/397 ,  A61K31/40 ,  A61K31/416 ,  A61K31/427 ,  A61K31/428 ,  A61K31/4436 ,  A61K31/4525 ,  A61P31/18 ,  A61P43/00 ,  C07D333/72 ,  C07D409/12 ,  C07D493/04 ,  C12N9/99

CPC分类号： C07D493/04 ,  A61K31/381 ,  A61K31/397 ,  A61K31/40 ,  A61K31/416 ,  A61K31/427 ,  A61K31/428 ,  A61K31/4436 ,  A61K31/4525 ,  A61P31/18 ,  C07D231/56 ,  C07D333/72 ,  C07D409/12 ,  C07D519/00 ,  C12N9/99

摘要： The present invention provides useful compounds for HIV protease inhibitor. A compound represented by formula or its pharmaceutically acceptable salt Formula: wherein ring A is R 4 is -Y-Z, hydrogen atom, halogen, hydroxy and the like, R 5 is hydrogen atom, halogen, hydroxy and the like, R 6 is each independently halogen, hydroxy, carboxy and the like, ring A may be substituted with said R 6 at any substitutable position(s), a is an integer of 0 to 7, ring B is substituted or unsubstituted aromatic carbocyclyl, or substituted or unsubstituted aromatic heterocyclyl, ring C is substituted or unsubstituted aromatic carbocyclyl, substituted or unsubstituted non-aromatic carbocyclyl, substituted or unsubstituted aromatic heterocyclyl, or substituted or unsubstituted non-aromatic heterocyclyl, R 1 is -Y-Z, substituted or unsubstituted alkyl, substituted or unsubstituted alkenyl, substituted or unsubstituted alkynyl and the like, R 2 and R 3 are each independently -Y-Z or hydrogen atom, provided that at least one of R 1 , R 2 , R 3 and R 4 is a group represented by formula: -Y-Z, Y is a bond, or a spacer of any combination selected from the group consisting of -O-, -S-, -NR 7 -, -C(=O)-, -SO-, -SO 2 -, -NR 7 -C(=O)-, -C(=O)-NR 7 -, -NR 7 -C(=O)-NR 7 -, -NR 7 -C(=O)-O-, -SO 2 -NR 7 -, -NR 7 -SO 2 -, substituted or unsubstituted alkylene, substituted or unsubstituted alkenylene, substituted or unsubstituted alkynylene, substituted or unsubstituted aromatic carbocyclediyl, substituted or unsubstituted non-aromatic carbocyclediyl, substituted or unsubstituted aromatic heterocyclediyl and substituted or unsubstituted non-aromatic heterocyclediyl, R 7 are each independently hydrogen atom, hydroxy, carboxy and the like, and Z is substituted aromatic carbocyclyl, substituted non-aromatic carbocyclyl, substituted aromatic heterocyclyl or substituted non-aromatic heterocyclyl.

公开(公告)号：EP3063143B1

公开(公告)日：2018-05-16

申请号：EP14800191.0

申请日：2014-10-29

申请人： Novartis AG

发明人： BAGDANOFF, Jeffrey T. ,  DING, Yu ,  HAN, Wooseok ,  HUANG, Zilin ,  JIANG, Qun ,  JIN, Jeff Xianming ,  KOU, Xiang ,  LEE, Patrick ,  LINDVALL, Mika ,  MIN, Zhongcheng ,  PAN, Yue ,  PECCHI, Sabina ,  PFISTER, Keith Bruce ,  POON, Daniel ,  RAUNIYAR, Vivek ,  WANG, Xiaojing Michael ,  ZHANG, Qiong ,  ZHOU, Jianguang ,  ZHU, Shejin

IPC分类号： C07D405/14 ,  C07D413/14 ,  C07D213/73 ,  C07D401/04 ,  C07D401/06 ,  C07D401/12 ,  C07D403/06 ,  C07D405/04 ,  C07D409/04 ,  C07D241/20 ,  A61K31/4418 ,  A61P35/00

CPC分类号： A61K31/497 ,  A61K31/44 ,  A61K31/4433 ,  A61K31/4436 ,  A61K31/4439 ,  A61K31/4545 ,  A61K31/4965 ,  A61K31/506 ,  A61K31/5355 ,  A61K31/5377 ,  A61K31/5383 ,  A61K31/553 ,  A61K45/06 ,  A61K2121/00 ,  C07D213/73 ,  C07D241/20 ,  C07D401/04 ,  C07D401/06 ,  C07D401/12 ,  C07D403/06 ,  C07D405/04 ,  C07D405/14 ,  C07D409/04 ,  C07D413/14 ,  C07D498/04

摘要： The present invention provides a compound of Formula (I) or a salt thereof; and therapeutic uses of these compounds. The present invention further provides pharmaceutical compositions comprising these compounds, and compositions comprising these compounds with a therapeutic co-agent.

公开(公告)号：EP3177299A4

公开(公告)日：2018-04-04

申请号：EP15829092

申请日：2015-08-03

申请人： ALIOS BIOPHARMA INC

发明人： BLATT LAWRENCE M ,  BEIGELMAN LEONID ,  SMITH DAVID BERNARD ,  WANG GUANGYI

IPC分类号： A61K31/7068 ,  A61K31/166 ,  A61K31/41 ,  A61K31/4184 ,  A61K31/4188 ,  A61K31/437 ,  A61K31/4436 ,  A61K31/4709 ,  A61K31/506 ,  A61K31/513 ,  A61K31/517 ,  A61K31/519 ,  A61K31/675 ,  A61K31/7056 ,  A61K38/16 ,  A61K38/21 ,  A61K39/155 ,  A61K39/42 ,  A61P11/00 ,  A61P31/14

CPC分类号： A61K31/7068 ,  A61K31/437 ,  A61K31/4436 ,  A61K31/7056 ,  A61K38/162 ,  A61K38/21 ,  A61K39/42 ,  A61K2039/505 ,  C12N7/00 ,  C12N2760/18511 ,  A61K2300/00

摘要： Disclosed herein are a combination of compounds and methods of using the combination of compounds for ameliorating, treating and/or preventing a paramyxovirus viral infection.

公开(公告)号：EP3004059B1

公开(公告)日：2017-09-20

申请号：EP14732767.0

申请日：2014-05-28

申请人： Bristol-Myers Squibb Company

发明人： AHMAD, Saleem ,  NEGASH, Lidet, A.

IPC分类号： C07D211/86 ,  C07D211/90 ,  A61K31/44 ,  A61P3/00

CPC分类号： C07D211/90 ,  A61K31/4412 ,  A61K31/4436 ,  A61K31/4439 ,  A61K31/444 ,  A61K45/06 ,  C07D211/78 ,  C07D211/86 ,  C07D401/04 ,  C07D409/04 ,  C07D409/14 ,  C07D417/04

摘要： The present invention provides compounds of Formula (I): or a stereoisomer, or a pharmaceutically acceptable salt thereof, wherein all of the variables are as defined herein. These compounds are monoacylglycerol acyltransferase type 2 (MGAT2) inhibitors which may be used as medicaments.

摘要翻译： 本发明提供式（I）的化合物或其立体异构体或其药学上可接受的盐，其中所有变量如本文所定义。 这些化合物是可用作药物的单酰甘油酰基转移酶2型（MGAT2）抑制剂。