公开(公告)号：EP2562155B1

公开(公告)日：2019-06-05

申请号：EP11772045.8

申请日：2011-04-20

申请人： Taisho Pharmaceutical Co., Ltd. ,  FUJIFILM Toyama Chemical Co., Ltd.

发明人： TAKASHIMA, Hajime ,  TSURUTA, Risa ,  YABUUCHI, Tetsuya ,  OKA, Yusuke ,  URABE, Hiroki ,  SUGA, Yoichiro ,  TAKAHASHI, Masato ,  UNEUCHI, Fumito ,  KOTSUBO, Hironori ,  SHOJI, Muneo ,  KAWAGUCHI, Yasuko

IPC分类号： C07C259/06 ,  A61K31/166 ,  A61K31/337 ,  A61K31/341 ,  A61K31/343 ,  A61K31/351 ,  A61K31/357 ,  A61K31/36 ,  A61K31/381 ,  A61K31/397 ,  A61K31/40 ,  A61K31/4015 ,  A61K31/402 ,  A61K31/403 ,  A61K31/4035 ,  A61K31/404 ,  A61K31/4045 ,  A61K31/407 ,  A61K31/415 ,  A61K31/416

CPC分类号： C07C233/83 ,  C07C235/84 ,  C07C237/36 ,  C07C259/06 ,  C07C271/22 ,  C07C271/28 ,  C07C309/30 ,  C07C311/08 ,  C07C317/28 ,  C07C317/44 ,  C07C323/41 ,  C07C323/62 ,  C07C2601/02 ,  C07C2601/04 ,  C07C2601/08 ,  C07C2601/14 ,  C07C2601/16 ,  C07C2601/18 ,  C07C2602/08 ,  C07D205/04 ,  C07D205/12 ,  C07D207/10 ,  C07D207/12 ,  C07D207/27 ,  C07D207/327 ,  C07D209/08 ,  C07D209/12 ,  C07D209/14 ,  C07D209/44 ,  C07D209/52 ,  C07D211/14 ,  C07D211/18 ,  C07D211/38 ,  C07D211/46 ,  C07D211/56 ,  C07D211/70 ,  C07D213/38 ,  C07D213/40 ,  C07D213/54 ,  C07D213/61 ,  C07D213/64 ,  C07D213/65 ,  C07D213/70 ,  C07D213/74 ,  C07D213/81 ,  C07D215/14 ,  C07D217/04 ,  C07D217/12 ,  C07D231/12 ,  C07D231/56 ,  C07D233/61 ,  C07D235/04 ,  C07D257/04 ,  C07D261/08 ,  C07D263/14 ,  C07D263/32 ,  C07D263/56 ,  C07D265/30 ,  C07D265/36 ,  C07D265/38 ,  C07D267/10 ,  C07D271/12 ,  C07D277/20 ,  C07D277/30 ,  C07D277/62 ,  C07D277/66 ,  C07D285/12 ,  C07D295/08 ,  C07D295/12 ,  C07D295/14 ,  C07D295/16 ,  C07D305/06 ,  C07D305/08 ,  C07D307/14 ,  C07D307/18 ,  C07D307/52 ,  C07D307/54 ,  C07D307/78 ,  C07D307/81 ,  C07D307/82 ,  C07D307/87 ,  C07D309/04 ,  C07D309/14 ,  C07D317/30 ,  C07D317/60 ,  C07D319/18 ,  C07D319/20 ,  C07D333/24 ,  C07D405/06 ,  C07D413/06 ,  C07D471/04 ,  C07D471/10 ,  C07D487/08 ,  C07D491/20 ,  C07D498/04 ,  C07D498/08 ,  C07F9/091

摘要： Provided is a novel compound which is useful as a pharmaceutical composition by inhibiting an LpxC activity, thereby exhibiting potent antimicrobial activity against gram-negative bacteria including Pseudomonas aeruginosa and its drug resistant bacteria. Provided is a hydroxamic acid derivative represented by the following general formula [1] or a pharmaceutically acceptable salt thereof:

公开(公告)号：EP3416948A1

公开(公告)日：2018-12-26

申请号：EP17705416.0

申请日：2017-02-16

申请人： The University Of Queensland ,  The Provost, Fellows, Foundation Scholars, and the other members of Board, of the College of the Holy & Undiv. Trinity of Queen Elizabeth near Dublin

发明人： O'NEILL, Luke ,  COLL, Rebecca ,  COOPER, Matthew ,  ROBERTSON, Avril ,  SCHRODER, Kate ,  MACLEOD, Angus Murray ,  MILLER, David John

IPC分类号： C07D231/18 ,  C07C307/06 ,  C07C307/08 ,  C07C307/10 ,  C07D295/26 ,  A61P29/00

CPC分类号： C07D295/26 ,  C07C307/06 ,  C07C307/10 ,  C07C2601/14 ,  C07C2602/08 ,  C07C2603/10 ,  C07D231/18

摘要： The present invention relates to compounds of formula (I), and pharmaceutically acceptable salts, solvates and prodrugs thereof: Formula (I) wherein Q is selected from O, S and Se; J is S or Se; W1 and W2, when present, are independently selected from N and C; R1 and R2 are independently selected from the group consisting of hydrogen, C1-C12alkyl, C2-C12alkenyl, C2-C12alkynyl, aryl, heterocyclyl, heteroaryl, cycloalkyl, cycloalkenyl, amino, amido, alkylthio, acyl, arylalkyl and acylamido, all of which may be optionally substituted; and wherein at least one of W1 and W2 is present and is a nitrogen atom and when R1 and R2 are cyclic then the respective W1 or W2 may form part of the ring structure. The present invention also relates to pharmaceutical compositions including such compounds, to methods of treatment using such compounds, in particular in relation to NLRP3 inflammasome mediated disorders, and to associated diagnostic uses.

公开(公告)号：EP3411354A1

公开(公告)日：2018-12-12

申请号：EP17701167.3

申请日：2017-01-27

申请人： Bayer CropScience Aktiengesellschaft

发明人： SÄMANN, Christoph ,  HIMMLER, Thomas

IPC分类号： C07C209/68 ,  C07C211/57

CPC分类号： C07C209/68 ,  C07C2602/08 ,  C07C211/57

摘要： The invention relates to a method for producing substituted 4-aminoindane derivatives of general formula (I) by cyclization, formula (I), in which R, n, R1, R2, R3, R4, Q1 and Q2 have the meanings as indicated in the description.

公开(公告)号：EP3408256A1

公开(公告)日：2018-12-05

申请号：EP17707970.4

申请日：2017-01-24

申请人： Takeda Pharmaceutical Company Limited

发明人： GOLDBY, Anne ,  LIWICKI, Gemma ,  MACK, Stephen ,  TEALL, Martin ,  WHITE, Katy

IPC分类号： C07C233/23 ,  C07D309/08 ,  C07D309/14 ,  C07C271/24 ,  C07D231/12 ,  C07D231/14 ,  C07C311/06 ,  C07D237/14 ,  C07C317/30 ,  C07D239/42 ,  C07D413/12 ,  C07C233/41 ,  C07D261/10 ,  C07C235/36 ,  C07D205/04

CPC分类号： C07D309/14 ,  C07B2200/07 ,  C07C233/23 ,  C07C233/41 ,  C07C235/36 ,  C07C237/20 ,  C07C271/24 ,  C07C311/06 ,  C07C317/30 ,  C07C2601/02 ,  C07C2601/04 ,  C07C2602/08 ,  C07D205/04 ,  C07D213/61 ,  C07D213/64 ,  C07D231/12 ,  C07D231/14 ,  C07D237/14 ,  C07D239/42 ,  C07D261/10 ,  C07D277/04 ,  C07D295/027 ,  C07D295/135 ,  C07D305/08 ,  C07D309/08 ,  C07D413/12

摘要： The present invention provides compounds of formula (I) and pharmaceutically acceptable salts thereof, wherein R1, R2, R3, R4a and R4b are as defined in the specification, processes for their preparation, pharmaceutical compositions containing them and their use in therapy. The compounds of formula (I) are mGluR7 modulators.

公开(公告)号：EP3400071A1

公开(公告)日：2018-11-14

申请号：EP17736458.5

申请日：2017-01-06

申请人： The Board of Trustees of the University of Illinois ,  The University of Texas Southwestern Medical center ,  Katzenellenbogen, John ,  Katzenellenbogen, Benita ,  Kim, Sung Hoon ,  Madak-Erdogan, Zeynep ,  Shaul, Philip

发明人： KATZENELLENBOGEN, John ,  KATZENELLENBOGEN, Benita ,  KIM, Sung Hoon ,  MADAK-ERDOGAN, Zeynep ,  SHAUL, Philip

IPC分类号： A61P35/00 ,  A61K31/00 ,  C07K14/705 ,  G01N33/574

CPC分类号： C07C39/17 ,  C07C39/12 ,  C07C39/14 ,  C07C39/23 ,  C07C39/367 ,  C07C39/42 ,  C07C43/196 ,  C07C49/733 ,  C07C49/755 ,  C07C57/38 ,  C07C235/34 ,  C07C255/47 ,  C07C2601/14 ,  C07C2602/08 ,  C07C2602/10 ,  C07C2603/74

摘要： Provided are compounds of formulae provided herein. The compounds may include pathway-preferential estrogens (PaPEs) derivatives with tissue-selective activities. Also provided are pharmaceutical compositions comprising the compounds, as well as methods of treating a disease or condition including administering the compounds. The disease or condition may include postmenopausal symptoms, cardiovascular disease, stroke, vascular disease, bone disease, metabolic disease, arthritis, osteoporosis, obesity, vasomotor/hot flush, cognitive decline, cancer including breast cancer.

公开(公告)号：EP2639216B1

公开(公告)日：2018-07-11

申请号：EP11839101.0

申请日：2011-11-08

申请人： Kaneka Corporation

发明人： YAMAMOTO, Shohei ,  NISHIHACHIJO, Masakatsu ,  TANAKA, Rie ,  KAWANO, Shigeru ,  FUJII, Akio

IPC分类号： C07C29/17 ,  C07C45/63 ,  C07C45/65 ,  C12P7/22 ,  C12P7/38 ,  C07B53/00 ,  C07C45/62 ,  C07D241/04

CPC分类号： C07B53/00 ,  C07B2200/07 ,  C07C29/175 ,  C07C45/62 ,  C07C45/63 ,  C07C45/65 ,  C07C2602/08 ,  C07D241/04 ,  C12P7/22 ,  C12P7/38 ,  C07C49/697 ,  C07C35/52

摘要： An optically active ketone represented by the following formula (2): wherein, Ar 1 represents a furyl group, a thienyl group or a C 6-20 aryl group; X 1 represents a halogen atom, and * indicates an asymmetric carbon atom, is produced by stereoselectively reducing an enone compound represented by the following formula (1) : wherein, Ar 1 and X 1 represent the same as the above.

公开(公告)号：EP3318546A1

公开(公告)日：2018-05-09

申请号：EP16197769.9

申请日：2016-11-08

申请人： Justus-Liebig-Universität Gießen

发明人： Schreiner, Peter R. ,  Combe, Sascha H.

IPC分类号： C07C17/00 ,  C07C17/14 ,  C07C19/01 ,  C07C19/07 ,  C07C22/02 ,  C07C22/04 ,  C07C23/08 ,  C07C23/10 ,  C07C23/16 ,  C07C23/28 ,  C07C255/50 ,  C07C69/78 ,  C07C205/06 ,  C07C67/307 ,  C07C201/12 ,  C07B39/00 ,  C07C253/30

CPC分类号： C07C67/307 ,  C07B39/00 ,  C07C17/14 ,  C07C201/12 ,  C07C253/30 ,  C07C2602/08 ,  C07C2602/14 ,  C07C2602/18 ,  C07C69/76 ,  C07C22/04 ,  C07C23/08 ,  C07C23/10 ,  C07C23/16 ,  C07C22/08 ,  C07C25/02 ,  C07C255/50 ,  C07C205/11

摘要： The invention provides a process for the production of halogenated or pseudo-halogenated hydrocarbons comprising the usage of at least one halogenating or pseudo-halogenating agent which contains at least one halogen-atom or pseudo-halogen substituent per formular unit in combination with substituted or unsubstituted N- hydroxyphthalimide and a metal-containing salt-like compound or a carboxylic or sulfonic acid with or without solvent.

摘要翻译： 本发明提供了一种制备卤代或假卤代烃的方法，其包括使用至少一种卤化或假卤化剂，所述卤化或假卤化剂含有每个单位单元至少一个卤素原子或假卤素取代基与取代或未取代的 N-羟基邻苯二甲酰亚胺和含金属的盐样化合物或羧酸或磺酸，有或没有溶剂。

公开(公告)号：EP3233070A1

公开(公告)日：2017-10-25

申请号：EP14908546.6

申请日：2014-12-16

申请人： ADT Pharmaceuticals, Inc.

发明人： PIAZZA, Gary A. ,  CHEN, Xi ,  KEETON, Adam B.

IPC分类号： A61K31/165

CPC分类号： C07C235/38 ,  A61K31/167 ,  A61K31/255 ,  A61K31/325 ,  A61K45/06 ,  C07C271/44 ,  C07C309/66 ,  C07C2602/08 ,  A61K2300/00

摘要： Disclosed are compounds, for example, compounds of formula (I), wherein R, R0 R1-R8, n, X, Y, Y1, and E are as described herein, pharmaceutical compositions containing such compounds, and methods of treating or preventing a disease or condition, for example, cancer.

摘要翻译： 公开了化合物，例如其中R 1，R 2，R 1，R 2，n，X，Y，Y 1和E如本文所述的式（I）化合物，含有这些化合物的药物组合物，以及 治疗或预防疾病或病症，例如癌症。

公开(公告)号：EP3061764A4

公开(公告)日：2017-08-30

申请号：EP14847060

申请日：2014-09-26

申请人： UNIV BEIJING

发明人： YI CHENGQI ,  XIA BO ,  ZHOU ANKUN

IPC分类号： C07H21/04 ,  C07C247/10 ,  C07H1/00 ,  C09K11/06 ,  C12Q1/68 ,  G01N21/64

CPC分类号： C07H19/06 ,  C07C247/10 ,  C07C2602/08 ,  C07H1/00 ,  C07H19/23 ,  C07H21/00 ,  C12Q1/6858 ,  C12Q1/6869 ,  Y02P20/582 ,  C12Q2525/117 ,  C12Q2535/101 ,  C12Q2537/164

摘要： The present invention relates to a 5-formylcytosine specific chemical labeling method and related applications in aspects such as sequencing, detection, imaging, and diagnosis. In the method, a condensation reaction occurs between an active methylene group in an active methylene compound containing a side-chain reactive group and an aldehyde group in 5-formylcytosine or a 1-substituted derivative of 5-formylcytosine, and at the same time an intramolecular reaction occurs between the side-chain reactive group of the active methylene compound and a 4-amino group of cytosine to implement ring closing. By means of the 5-formylcytosine specific chemical labeling method and related compounds of the present invention, detection of the content of 5-formylcytosine in nucleic acid molecules, and specific concentration of 5-formylcytosine-containing nucleic acid samples, and analysis of sequence distribution information of 5-formylcytosine and/or single-base resolution sequence information in nucleic acid molecules and the like may be implemented. The present invention provides various effective research methods in the research fields of epigenetics and nucleic acid biochemistry.

摘要翻译： 本发明涉及5-甲酰基胞嘧啶特异性化学标记方法以及在诸如测序，检测，成像和诊断等方面的相关应用。 在该方法中，在含有侧链反应性基团的活性亚甲基化合物中的活性亚甲基和5-甲酰基胞嘧啶中的醛基或5-甲酰基胞嘧啶的1-取代衍生物之间发生缩合反应，并且同时 在活性亚甲基化合物的侧链反应性基团和胞嘧啶的4-氨基之间发生分子内反应以实现闭环。 通过本发明的5-甲酰基胞嘧啶特异性化学标记方法和相关化合物，检测核酸分子中5-甲酰基胞嘧啶的含量和含5-甲酰基胞嘧啶的核酸样品的特定浓度，以及序列分布的分析 可以实施核酸分子等中的5-甲酰基胞嘧啶和/或单碱基分辨序列信息的信息。 本发明为表观遗传学和核酸生物化学研究领域提供了各种有效的研究方法。

公开(公告)号：EP2418942B1

公开(公告)日：2017-08-23

申请号：EP10765133.3

申请日：2010-04-14

申请人： Sanford-Burnham Medical Research Institute

发明人： PELLECCHIA, Maurizio

IPC分类号： A01N35/00 ,  C07C235/66 ,  A61K31/166

CPC分类号： G01N33/564 ,  C07C39/14 ,  C07C49/83 ,  C07C235/66 ,  C07C311/29 ,  C07C2601/02 ,  C07C2601/08 ,  C07C2601/14 ,  C07C2602/08 ,  C07D277/64 ,  C07D417/10 ,  C12Q1/6883 ,  C12Q1/6886 ,  G01N33/57407 ,  G01N2800/042 ,  G01N2800/046 ,  G01N2800/065 ,  G01N2800/10 ,  G01N2800/101 ,  G01N2800/102 ,  G01N2800/104 ,  G01N2800/105 ,  G01N2800/122 ,  G01N2800/127 ,  G01N2800/202 ,  G01N2800/205 ,  G01N2800/222 ,  G01N2800/226 ,  G01N2800/24 ,  G01N2800/28 ,  G01N2800/2821 ,  G01N2800/285 ,  G01N2800/32 ,  G01N2800/325 ,  G01N2800/328 ,  G01N2800/347 ,  G01N2800/52