公开(公告)号：EP4327877A3

公开(公告)日：2024-04-24

申请号：EP23202655.9

申请日：2019-04-17

申请人： XRad Therapeutics, Inc.

发明人： FU, Jianmin ,  SUN, Yue ,  WU, Guosheng ,  LU, Aijun ,  ZHANG, Shuang ,  GOODNOW, Robert ,  GILMER, Tona ,  KASTAN, Michael ,  KIRSCH, David ,  WANG, Yaode

IPC分类号： C07D471/10 ,  C07D471/20 ,  C07D471/04 ,  A61K31/444 ,  A61K31/4545 ,  A61K31/4745 ,  A61K31/502 ,  A61P35/00

CPC分类号： A61K45/06 ,  A61P35/00 ,  C07D471/04 ,  C07D471/10 ,  C07D471/20 ,  C07D491/20 ,  C07D519/00

摘要： Provided herein are compounds of the Formula (I), (II), and (III):


and

as well as pharmaceutically acceptable salts thereof, wherein the substituents are those disclosed in the specification. These compounds, and the pharmaceutical compositions containing them, are useful for the treatment of oncologic diseases.

公开(公告)号：EP2825044B1

公开(公告)日：2018-08-15

申请号：EP13760317.1

申请日：2013-03-13

申请人： Merck Sharp & Dohme Corp.

发明人： BELYK, Kevin M. ,  CLEATOR, Edward ,  KUO, Shen-Chun ,  MALIGRES, Peter Emmanuel ,  XIANG, Bangping ,  YASUDA, Nobuyoshi ,  YIN, Jianguo

IPC分类号： C07D471/20

CPC分类号： C07D471/20

摘要： The invention encompasses a novel process for making piperidinone carboxamide indane and azainane derivatives, which are CGRP receptor antagonists useful for the treatment of migraine, utilizing a highly effective spiroacid synthesis.

公开(公告)号：EP2968288B1

公开(公告)日：2018-07-04

申请号：EP14770645

申请日：2014-03-10

申请人： MERCK SHARP & DOHME

发明人： PASTERNAK ALEXANDER ,  DING FA-XIANG ,  DONG SHUZHI ,  TANG HAIFENG ,  JIANG JINLONG ,  GU XIN ,  YANG CANGMING ,  BISWAS DIPSHIKHA

IPC分类号： C07D471/10 ,  A61K31/24 ,  A61K31/401 ,  A61K31/403 ,  A61K31/405 ,  A61K31/407 ,  A61K31/41 ,  A61K31/417 ,  A61K31/4178 ,  A61K31/4184 ,  A61K31/435 ,  A61K31/438 ,  A61K45/06 ,  A61P9/12 ,  C07D471/20 ,  C07D498/20

CPC分类号： C07D471/10 ,  A61K31/24 ,  A61K31/401 ,  A61K31/403 ,  A61K31/405 ,  A61K31/407 ,  A61K31/41 ,  A61K31/417 ,  A61K31/4178 ,  A61K31/4184 ,  A61K31/435 ,  A61K31/4422 ,  A61K31/444 ,  A61K31/472 ,  A61K31/4965 ,  A61K31/497 ,  A61K31/4995 ,  A61K31/501 ,  A61K31/506 ,  A61K31/519 ,  A61K31/5386 ,  A61K31/55 ,  A61K31/551 ,  A61K31/554 ,  A61K31/585 ,  A61K31/675 ,  A61K45/06 ,  C07D471/20 ,  C07D498/20 ,  A61K2300/00

摘要： The present invention provides compounds of Formula I and the pharmaceutically acceptable salts thereof, which are inhibitors of the ROMK (Kir1.1) channel. The compounds may be used as diuretic and/or natriuretic agents and for the therapy and prophylaxis of medical conditions including cardiovascular diseases such as hypertension, heart failure and chronic kidney disease and conditions associated with excessive salt and water retention.

公开(公告)号：EP3312897A1

公开(公告)日：2018-04-25

申请号：EP16810992.4

申请日：2016-06-15

申请人： Kunshan Go-Visionox Opto-Electronics Co., Ltd. ,  Tsinghua University

发明人： DUAN, Lian ,  ZHANG, Dongdong ,  LIU, Song ,  XIE, Jing ,  ZHAO, Fei

IPC分类号： H01L51/50

CPC分类号： H01L51/006 ,  C07C211/61 ,  C07C255/58 ,  C07C317/36 ,  C07C2603/24 ,  C07C2603/97 ,  C07D209/80 ,  C07D209/86 ,  C07D219/02 ,  C07D221/20 ,  C07D241/48 ,  C07D265/38 ,  C07D285/14 ,  C07D403/10 ,  C07D403/14 ,  C07D413/10 ,  C07D413/14 ,  C07D417/04 ,  C07D417/10 ,  C07D417/14 ,  C07D471/20 ,  C07D487/14 ,  C07D487/16 ,  C07F1/02 ,  C07F3/02 ,  C07F3/06 ,  H01L51/0008 ,  H01L51/0052 ,  H01L51/0056 ,  H01L51/0059 ,  H01L51/0061 ,  H01L51/0067 ,  H01L51/0068 ,  H01L51/0069 ,  H01L51/007 ,  H01L51/0071 ,  H01L51/0072 ,  H01L51/0077 ,  H01L51/0092 ,  H01L51/50 ,  H01L51/5016 ,  H01L51/5024 ,  H01L51/5056 ,  H01L51/5072 ,  H01L2051/0063 ,  H01L2251/5376 ,  H01L2251/558

摘要： Disclosed is an organic electroluminescent device, comprising a substrate and light emitting units formed in sequence on the substrate, characterized in that, each of the light emitting units comprises a first electrode layer (1), a light emitting layer (2) and a second electrode layer (3), the light emitting layer comprises a host material and a dye, the host material is made of materials having both electron transport capability and hole transport capability; at least one material in the host material has a CT excited triplet state energy level T 1 greater than its n-π excited triplet state energy level S 1 , and T 1 -S 1 ≤ 0.3eV; or, at least one material in the host material has a CT excited triplet state energy level T 1 greater than its n-π excited triplet state energy level S 1 , and T 1 -S 1 ≥ 1eV, with the difference between its n-π excited second triplet state energy level and its CT excited first singlet state energy level being in the range of -0.1eV to 0.1eV. The organic electroluminescent device configuration can sufficiently utilize the triplet state energy in the host material and the dye to increase the luminous efficiency and prolong the service life of the device.

摘要翻译： 本发明公开了一种有机电致发光器件，包括衬底和在衬底上依次形成的发光单元，其特征在于，每个发光单元包括第一电极层（1），发光层（2）和第二电极层 所述发光层包括主体材料和染料，所述主体材料由具有电子传输能力和空穴传输能力的材料制成; 主体材料中的至少一种材料具有大于其n-π激发三重态能级S1的CT激发三重态能级T1，并且T1-S1≤0.3eV; 或者，主体材料中的至少一种材料具有大于其n-π激发三重态能级S1的CT激发三重态能级T1，并且T1-S1≥1eV，其n-π激发第二三重态之间的差异 状态能级及其CT激发的第一单态能级在-0.1eV至0.1eV的范围内。 有机电致发光器件结构可充分利用主体材料和染料中的三重态能量来提高发光效率并延长器件的使用寿命。

公开(公告)号：EP2846798B1

公开(公告)日：2018-04-04

申请号：EP13788067.0

申请日：2013-05-03

申请人： Merck Sharp & Dohme Corp.

发明人： BELL, Ian, M. ,  FRALEY, Mark ,  BIFTU, Tesfaye ,  ZHU, Cheng ,  NAIR, Anilkumar ,  MITCHELL, Helen

IPC分类号： C07D471/20 ,  A61K31/4523 ,  A61K31/45 ,  A61K31/451 ,  A61P25/06

CPC分类号： C07D471/20 ,  A61K9/4858 ,  A61K31/45 ,  A61K31/451 ,  A61K31/4523

摘要： The present invention is directed to aliphatic spirolactam derivatives which are antagonists of CGRP receptors and useful in the treatment or prevention of diseases in which CGRP is involved, such as migraine. The invention is also directed to pharmaceutical\compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which CGRP is involved.

公开(公告)号：EP2684880B1

公开(公告)日：2018-02-28

申请号：EP12755073.9

申请日：2012-03-09

申请人： Daiichi Sankyo Company, Limited

发明人： SUGIMOTO, Yuuichi ,  UOTO, Kouichi ,  MIYAZAKI, Masaki ,  SETOGUCHI, Masaki ,  TANIGUCHI, Toru ,  YOSHIDA, Keisuke ,  YAMAGUCHI, Akitake ,  YOSHIDA, Shoko ,  WAKABAYASHI, Takanori

IPC分类号： C07D471/20 ,  A61K31/407 ,  A61K31/437 ,  A61K31/4439 ,  A61K31/506 ,  A61K31/5377 ,  A61P35/00 ,  A61P35/02 ,  A61P43/00 ,  C07D487/10 ,  C07D519/00

CPC分类号： C07D487/20 ,  A61K9/14 ,  A61K9/1623 ,  A61K9/1652 ,  A61K9/2018 ,  A61K9/2054 ,  A61K9/2059 ,  C07D471/20 ,  C07D487/10

摘要： A novel compound that inhibits interaction between murine double minute 2 (Mdm2) protein and p53 protein and exhibits anti-tumor activity is provided. The present invention provides a dispiropyrrolidine derivative represented by the following formula (1) having various substituents that inhibits interaction between Mdm2 protein and p53 protein and exhibits anti-tumor activity, wherein R 1 , R 2 , R 3 , ring A, and ring B in formula (1) respectively have the same meanings as defined in the specification.

公开(公告)号：EP3172208A4

公开(公告)日：2017-12-06

申请号：EP15824385

申请日：2015-07-21

申请人： GLAXOSMITHKLINE IP DEV LTD

发明人： WAN ZEHONG ,  ZHANG XIAOMIN ,  WANG JIAN

IPC分类号： C07D487/14 ,  A61K31/519 ,  A61P25/28

CPC分类号： C07D487/14 ,  C07D471/14 ,  C07D471/20 ,  C07D487/04 ,  C07D491/20 ,  C07D498/14 ,  C07D513/14

摘要： The present invention relates to novel compounds that inhibit Lp-PLA2 activity, processes for their preparation, to compositions containing them and to their use in the treatment of diseases associated with the activity of Lp-PLA2, for example atherosclerosis, Alzheimer's disease.

公开(公告)号：EP3148535A4

公开(公告)日：2017-11-29

申请号：EP15799729

申请日：2015-05-26

申请人： PURDUE PHARMA LP

发明人： YOUNGMAN MARK ,  TAFESSE LAYKEA ,  GOEHRING R RICHARD ,  YU JIANMING

IPC分类号： C07D471/20 ,  A61K31/4166 ,  A61P29/00

CPC分类号： C07D471/20 ,  C07B59/002 ,  C07B2200/05 ,  C07D489/09

摘要： In one aspect, the invention provides compounds of Formula I: (I) and pharmaceutically acceptable salts and solvates thereof, wherein R1, R2, R3, R4, R5, Y, Za are defined as set forth in the disclosure. The invention also provides compounds of any one of Formulae II to VII, IA to IC, and IIA to IIC, and pharmaceutically acceptable salts and solvates thereof. Other aspects of the invention include the use of compounds of Formulae I to VII, IA to IC, and IIA to IIC, and pharmaceutically acceptable salts and solvates thereof for the treatment of disorders responsive to modulation of one or more opioid receptors. In certain embodiments, the Compounds of the Invention are useful for treating pain.

公开(公告)号：EP3172211A1

公开(公告)日：2017-05-31

申请号：EP15825267.6

申请日：2015-07-21

申请人： GlaxoSmithKline Intellectual Property Development Limited

发明人： WAN, Zehong ,  ZHANG, Xiaomin ,  WANG, Jian ,  SENDER, Matthew Robert ,  MANAS, Eric Steven ,  RIVERO, Raphael Anthony ,  PERO, Joseph E. ,  NEIPP, Christopher Ernst ,  PATEL, Vipulkumar Kantibhai

IPC分类号： C07D487/14 ,  C07D487/20 ,  C07D491/20 ,  C07D513/12 ,  A61K31/519 ,  A61K31/527 ,  A61P25/28 ,  A61P9/10

CPC分类号： C07D487/14 ,  C07D471/14 ,  C07D471/20 ,  C07D487/04 ,  C07D491/20 ,  C07D498/14 ,  C07D513/14 ,  H05K999/99

摘要： The present invention relates to novel compounds that inhibit Lp-PLA2 activity, processes for their preparation, to compositions containing them and to their use in the treatment of diseases associated with the activity of Lp-PLA2, for example atherosclerosis, Alzheimer's disease.

摘要翻译： 本发明涉及抑制Lp-PLA2活性的新化合物，其制备方法，含有它们的组合物及其用于治疗与Lp-PLA2的活性有关的疾病，例如动脉粥样硬化，阿尔茨海默氏病。

公开(公告)号：EP3164401A1

公开(公告)日：2017-05-10

申请号：EP15732007.8

申请日：2015-07-02

申请人： Boehringer Ingelheim International GmbH

发明人： WEINSTABL, Harald ,  GOLLNER, Andreas ,  RAMHARTER, Juergen ,  WUNBERG, Tobias

IPC分类号： C07D471/20 ,  C07D487/20 ,  A61K31/437 ,  A61P35/00

CPC分类号： A61K31/437 ,  A61K31/407 ,  A61K31/427 ,  A61K31/635 ,  A61K45/06 ,  C07D471/20 ,  C07D471/22 ,  C07D487/20 ,  C07D491/20

摘要： The present invention relates to compounds of formula (I) wherein the groups R1 to R3, R7, U, V, W, X, Y, n and q are as defined herein, their use as inhibitors of MDM2-p53 interaction, pharmaceutical compositions which contain compounds of this kind, their use as medicaments, especially as agents for treatment and/or prevention of oncological diseases and synthetic intermediates.

摘要翻译： 本发明涉及其中基团R 1至R 3，R 7，U，V，W，X，Y，n和q如本文所定义的式（I）化合物，它们作为MDM2-p53相互作用抑制剂的用途，药物组合物 其含有这种化合物，它们作为药物的用途，特别是用作治疗和/或预防肿瘤疾病和合成中间体的药剂。