公开(公告)号：EP3416958A1

公开(公告)日：2018-12-26

申请号：EP17753951.7

申请日：2017-02-17

申请人： Dana Farber Cancer Institute, Inc. ,  President and Fellows of Harvard College ,  The General Hospital Corporation

发明人： WAGNER, Gerhard ,  ARTHANARI, Haribabu ,  NÄÄR, Anders ,  BUHRLAGE, Sara Jean ,  NISHIKAWA, Joy Luz ,  BOESZOERMENYI, Andras Pal ,  SANGLARD, Dominique

IPC分类号： C07D401/12 ,  C07D231/40

CPC分类号： C07D295/26 ,  C07C337/06 ,  C07C2601/02 ,  C07C2601/14 ,  C07D311/16 ,  C07D317/66 ,  C07D333/70

摘要： Provided herein are compounds (e.g., compounds of Formulae (I), (II), and (III)) which are anti-fungal agents and can be used in the treatment of diseases, including infectious diseases. The invention provides methods of treating diseases in a subject (e.g., infectious diseases such as fungal infections), and methods of killing or inhibiting the growth of fungi in or on a subject or biological sample. The compounds may be used in subjects, in clinical settings, or in agricultural settings.

公开(公告)号：EP2975023B1

公开(公告)日：2018-05-30

申请号：EP14763790.4

申请日：2014-03-13

申请人： Takeda Pharmaceutical Company Limited

发明人： FUJIYASU, Jiro ,  ASANO, Toru ,  YAMAKI, Susumu ,  KANEKO, Osamu ,  KOIKE, Yuka ,  IMAIZUMI, Tomoyoshi ,  URANO, Yasuharu ,  SATOU, Tomohki ,  SASAMURA, Satoshi

IPC分类号： C07D333/40 ,  C07C279/18 ,  C07D307/81 ,  C07D333/68 ,  C07D333/70 ,  C07D217/26 ,  C07D333/24 ,  A61K31/381 ,  A61K31/24 ,  A61K31/343 ,  A61K31/472 ,  A61P13/12

CPC分类号： C07D333/70 ,  A61K31/24 ,  A61K31/343 ,  A61K31/381 ,  A61K31/472 ,  C07C279/18 ,  C07C2602/08 ,  C07C2602/10 ,  C07D217/26 ,  C07D307/81 ,  C07D333/24 ,  C07D333/40 ,  C07D333/68

摘要： [Problem] To provide a compound which is useful as an agent for preventing and/or treating kidney diseases. [Means for Solution] The present inventors have studied compounds having a trypsin inhibitory activity, and have confirmed that a guanidinobenzoic acid ester compound has a trypsin inhibitory activity, thereby completing the present invention. The guanidinobenzoic acid ester compound of the present invention can be used as an agent for preventing and/or treating kidney diseases (for example, chronic kidney disease, acute glomerulonephritis, acute kidney injury, and the like) as an agent which will substitute low-protein diet therapy, and/or as an agent for preventing and/or treating trypsin-related diseases (for example, chronic pancreatitis, gastroesophageal reflux disease, hepatic encephalopathy, influenza, and the like).

公开(公告)号：EP2855426B1

公开(公告)日：2017-01-04

申请号：EP13730284.0

申请日：2013-05-23

申请人： Orion Corporation

发明人： AHLMARK, Marko ,  DIN BELLE, David ,  KAUPPALA, Mika ,  LUIRO, Anne ,  PAJUNEN, Taina ,  PYSTYNEN, Jarmo ,  TIAINEN, Eija ,  VAISMAA, Matti ,  MESSINGER, Josef

IPC分类号： C07C255/53 ,  A61K31/277 ,  A61P25/00 ,  C07C255/54 ,  C07C255/57 ,  C07D333/24 ,  C07D333/60 ,  C07C311/29 ,  C07C317/22 ,  C07C321/28 ,  C07C321/30 ,  C07D265/30 ,  C07D207/08 ,  C07D207/337 ,  C07D277/30

CPC分类号： A61K31/277 ,  A61K31/198 ,  A61K31/341 ,  A61K31/343 ,  A61K31/381 ,  A61K31/382 ,  A61K31/40 ,  A61K31/5377 ,  C07C255/53 ,  C07C255/54 ,  C07C255/57 ,  C07C255/59 ,  C07C309/66 ,  C07C311/29 ,  C07C317/46 ,  C07C323/29 ,  C07C323/62 ,  C07D207/337 ,  C07D211/14 ,  C07D213/57 ,  C07D213/62 ,  C07D231/12 ,  C07D231/14 ,  C07D277/30 ,  C07D277/34 ,  C07D277/74 ,  C07D295/155 ,  C07D295/192 ,  C07D307/54 ,  C07D307/80 ,  C07D307/81 ,  C07D309/06 ,  C07D309/12 ,  C07D309/22 ,  C07D333/24 ,  C07D333/28 ,  C07D333/60 ,  C07D333/70

摘要： Compounds of formula (I), wherein R1 is as defined in the claims, exhibit COMT enzyme inhibiting activity and are thus useful as COMT inhibitors. Methods of treatment and pharmaceutical dosage forms are also disclosed.

摘要翻译： 式（I）化合物，其中R 1如权利要求中所定义，表现出COMT酶抑制活性，因此可用作COMT抑制剂。 还公开了治疗方法和药物剂型。

公开(公告)号：EP3004057A4

公开(公告)日：2016-11-02

申请号：EP14806807

申请日：2014-06-03

申请人： C&C RES LAB

发明人： PARK CHAN HEE ,  LEE SANG HWI ,  IM JUNHWAN ,  LEE SOON OK ,  KIM HOE MOON ,  MOON SUNG HYUN ,  KIM SEUNGHEE ,  KIM JONGMIN ,  KO KWANG SEOK ,  CHOI BU YOUNG ,  KIM BYUNGHO

IPC分类号： C07D209/42 ,  A61K31/404 ,  A61P29/00 ,  A61P35/00

CPC分类号： C07D495/04 ,  C07D209/42 ,  C07D277/68 ,  C07D307/86 ,  C07D333/68 ,  C07D333/70 ,  C07D401/12 ,  C07D403/12 ,  C07D409/12 ,  C07D413/12 ,  C07D417/04 ,  C07D471/04 ,  C07D491/10 ,  C07D513/04

摘要： A heterocyclic derivative represented by formula (I), or a pharmaceutically acceptable salt or a stereoisomer thereof, which has an inhibitory effect on the activation of STAT3 protein, and is useful for the prevention or treatment of diseases associated with the activation of STAT3 protein.

公开(公告)号：EP2923574A4

公开(公告)日：2016-10-12

申请号：EP13853426

申请日：2013-10-31

申请人： SUMITOMO CHEMICAL CO

发明人： MUKUMOTO FUJIO ,  TAMAKI HIROAKI ,  KUSAKA SHINTARO ,  IWAKOSHI MITSUHIKO

IPC分类号： A01N43/12 ,  A01C1/00 ,  A01G7/06 ,  A01N25/00 ,  A01N43/36 ,  A01N43/40 ,  A01N43/54 ,  A01N43/56 ,  A01N43/80 ,  A01N47/02 ,  A01N47/04 ,  A01N47/06 ,  A01N47/32 ,  A01P21/00

CPC分类号： A01N43/12 ,  A01G1/001 ,  A01N43/36 ,  A01N43/40 ,  A01N43/54 ,  A01N43/56 ,  A01N43/80 ,  A01N47/02 ,  A01N47/04 ,  A01N47/06 ,  A01N47/32 ,  C07D333/70 ,  C07D409/04

摘要： The present invention provides a method for promoting plant growth, which comprises treating a plant with a compound represented by the following Formula (1): provided that a method for promoting plant growth which comprises treating plants with a compound corresponding to any one of the following (1) to (8) is excluded: (1) Methyl 4-(trifluoromethyl)benzo[b]thiophene-2-carboxylate, (2) Methyl 5-(trifluoromethyl)benzo[b]thiophene-2-carboxylate, (3) Methyl 6-(trifluoromethyl)benzo[b]thiophene-2-carboxylate, (4) Methyl 7-(trifluoromethyl)benzo[b]thiophene-2-carboxylate, (5) Ethyl 4-(trifluoromethyl)benzo[b]thiophene-2-carboxylate, (6) Ethyl 5-(trifluoromethyl)benzo[b]thiophene-2-carboxylate, (7) Ethyl 6-(trifluoromethyl)benzo[b]thiophene-2-carboxylate, and (8) Ethyl 7-(trifluoromethyl)benzo[b]thiophene-2-carboxylate.

公开(公告)号：EP3059237A1

公开(公告)日：2016-08-24

申请号：EP14854084.2

申请日：2014-10-20

申请人： Suzhou Vigonvita Life Sciences Co. Ltd. ,  Topharman Shanghai Co., Ltd. ,  Shanghai Institute Of Materia Medica Chinese Academy of Sciences

发明人： LIU, Zheng ,  WU, Chunhui ,  LIU, Yongjian ,  ZHANG, Rongxia ,  HE, Yang ,  TIAN, Guanghui ,  SHEN, Jingshan

IPC分类号： C07D409/12 ,  C07D333/70

CPC分类号： C07D409/12 ,  C07D333/54 ,  C07D333/70

摘要： The present invention relates to the methods for preparing brexpiprazole, the analogs, key intermediates, and salts thereof, specifically, the present invention relates to a new method for preparing brexpiprazole, the analogs, key intermediates, and salts thereof, and the key intermediates, and salts thereof provided during the preparation. The preparation method has a mild reaction condition, stable intermediate, easy operation, and uses cheap and easy-to-get reagents, thus it saves the synthesis cost, shortens the production cycle, improves the yield and product quality, and is suitable for mass production.

摘要翻译： 本发明涉及一种用于制备brexpiprazole，所述类似物，关键中间体的方法，以及它们的盐，具体地，本发明涉及一种新的方法用于制备brexpiprazole，所述类似物，关键的中间体，以及它们的盐，以及关键中间体， 和盐在制备过程中它们提供。 该制备方法具有反应条件温和，稳定的中间，容易操作，并且使用便宜和容易获得的试剂，从而节省了合成成本，缩短生产周期，提高产量和产品质量，并且是适合于大规模 生产。

公开(公告)号：EP3004057A1

公开(公告)日：2016-04-13

申请号：EP14806807.5

申请日：2014-06-03

申请人： C&C Research Laboratories

发明人： PARK, Chan Hee ,  LEE, Sang Hwi ,  IM, Junhwan ,  LEE, Soon Ok ,  KIM, Hoe Moon ,  MOON, Sung Hyun ,  KIM, Seunghee ,  KIM, Jongmin ,  KO, Kwang Seok ,  CHOI, Bu Young ,  KIM, Byungho

IPC分类号： C07D209/42 ,  A61K31/404 ,  A61P35/00 ,  A61P29/00

CPC分类号： C07D495/04 ,  C07D209/42 ,  C07D277/68 ,  C07D307/86 ,  C07D333/68 ,  C07D333/70 ,  C07D401/12 ,  C07D403/12 ,  C07D409/12 ,  C07D413/12 ,  C07D417/04 ,  C07D471/04 ,  C07D491/10 ,  C07D513/04

摘要： A heterocyclic derivative represented by formula (I), or a pharmaceutically acceptable salt or a stereoisomer thereof, which has an inhibitory effect on the activation of STAT3 protein, and is useful for the prevention or treatment of diseases associated with the activation of STAT3 protein.

公开(公告)号：EP1896395B1

公开(公告)日：2015-07-15

申请号：EP06785306.9

申请日：2006-06-21

申请人： Merck Sharp & Dohme Corp.

发明人： GRIMM, Jonathan ,  HARRINGTON, Paul ,  HEIDEBRECHT, Richard, Jr. ,  MILLER, Thomas ,  OTTE, Karin ,  SILIPHAIVANH, Phieng ,  SLOMAN, David ,  STANTON, Matthew ,  WILSON, Kevin ,  WITTER, David ,  KATTAR, Solomon ,  TEMPEST, Paul

IPC分类号： C07D413/14 ,  C07D215/06 ,  C07D215/12 ,  C07C255/60 ,  C07D213/82 ,  C07D215/40 ,  C07D319/16 ,  C07D319/18 ,  C07D231/40 ,  C07D333/20 ,  C07D333/38 ,  C07D333/70 ,  C07C311/08 ,  C07C311/46 ,  C07D249/08 ,  C07D261/14 ,  C07C233/75 ,  C07C233/80 ,  C07C235/42 ,  C07D295/185

CPC分类号： C07C235/78 ,  C07C233/75 ,  C07C233/80 ,  C07C235/42 ,  C07C235/56 ,  C07C235/74 ,  C07C235/84 ,  C07C255/60 ,  C07C311/08 ,  C07C311/16 ,  C07C311/46 ,  C07C2602/08 ,  C07D207/06 ,  C07D207/327 ,  C07D209/14 ,  C07D209/20 ,  C07D211/06 ,  C07D213/40 ,  C07D213/56 ,  C07D213/82 ,  C07D215/06 ,  C07D215/12 ,  C07D215/40 ,  C07D231/40 ,  C07D249/08 ,  C07D261/14 ,  C07D265/30 ,  C07D277/28 ,  C07D277/46 ,  C07D277/56 ,  C07D295/135 ,  C07D295/155 ,  C07D295/185 ,  C07D307/68 ,  C07D319/16 ,  C07D319/18 ,  C07D333/20 ,  C07D333/38 ,  C07D333/70 ,  C07D413/14 ,  C07D495/04

公开(公告)号：EP2882430A1

公开(公告)日：2015-06-17

申请号：EP13827453.5

申请日：2013-08-09

申请人： McMaster University

发明人： BROWN, Eric ,  ALITNI, Soumaya

IPC分类号： A61K31/165 ,  A61K31/12 ,  A61K31/135 ,  A61K31/357 ,  A61K31/44 ,  A61K31/4523 ,  A61P31/04 ,  A61P31/06

CPC分类号： A01N43/40 ,  A01N35/02 ,  A01N37/28 ,  A01N37/38 ,  A01N43/12 ,  A61K31/165 ,  C07C323/22 ,  C07C323/48 ,  C07C323/62 ,  C07D213/04 ,  C07D333/70

摘要： Anti-bacterial compounds have been identified having the general structures defined by Formula (I), Formula (II), and Formula (III).

公开(公告)号：EP2838891A1

公开(公告)日：2015-02-25

申请号：EP13710076.4

申请日：2013-02-22

申请人： Takeda Pharmaceutical Company Limited

发明人： TAKAKURA, Nobuyuki ,  BANNO, Yoshihiro ,  TERAO, Yoshito ,  OCHIDA, Atsuko ,  MORIMOTO, Sachie ,  KITAMURA, Shuji ,  TOMATA, Yoshihide ,  YASUMA, Tsuneo ,  IKOMA, Minoru ,  MASUDA, Kei

IPC分类号： C07D333/60 ,  C07D407/14 ,  C07D417/12 ,  C07D495/04 ,  C07D307/82 ,  A61K31/381 ,  A61K31/343 ,  A61K31/4355 ,  A61K31/4365 ,  A61P3/04

CPC分类号： C07D333/60 ,  C07D307/79 ,  C07D307/80 ,  C07D307/81 ,  C07D307/84 ,  C07D333/54 ,  C07D333/64 ,  C07D333/70 ,  C07D405/04 ,  C07D405/12 ,  C07D409/06 ,  C07D409/12 ,  C07D417/12 ,  C07D495/04

摘要： The present invention provides a compound having a GOAT inhibitory action, which is useful for the prophylaxis or treatment of obesity and the like, and has superior efficacy. The present invention is a compound represented by the formula (I): wherein each symbol is as defined in the specification, or a salt thereof.

摘要翻译： 本发明提供具有GOAT抑制作用的化合物，其可用于预防或治疗肥胖症等，并且具有优异的功效。 本发明是由式（I）表示的化合物：其中每个符号如说明书中所定义，或其盐。