公开(公告)号：EP3033339B1

公开(公告)日：2018-02-28

申请号：EP14727401.3

申请日：2014-05-12

申请人： Merck Patent GmbH

发明人： TSAKLAKIDIS, Christos ,  STAEHLE, Wolfgang ,  LEUTHNER, Birgitta

IPC分类号： C07D413/14 ,  C07D413/12 ,  C07D417/12 ,  C07D249/04 ,  C07D487/04 ,  C07D271/10 ,  A61K31/4245 ,  A61K31/4439 ,  A61K31/428 ,  A61K31/519 ,  A61K31/423 ,  A61K31/4192 ,  A61P35/00 ,  A61P31/00 ,  A61P25/00

CPC分类号： C07D413/12 ,  A61K31/4192 ,  A61K31/423 ,  A61K31/4245 ,  A61K31/428 ,  A61K31/4439 ,  A61K31/519 ,  A61K45/06 ,  C07D249/04 ,  C07D263/57 ,  C07D271/10 ,  C07D413/14 ,  C07D417/12 ,  C07D487/04 ,  Y02A50/465 ,  A61K2300/00

摘要： Compounds of the formula I in which R, W, R1, R4, X1, X2, X3, X4 and q have the meanings indicated in claim 1, are inhibitors of fatty acid synthase, and can be employed, inter alia, for the treatment of diseases such as cancer, cardiovascular diseases, central nervous system injury and different forms of inflammation.

公开(公告)号：EP3277276A1

公开(公告)日：2018-02-07

申请号：EP16774100.8

申请日：2016-03-30

申请人： Calithera Biosciences Inc.

发明人： GROSS, Matthew I. ,  BENNETT, Mark, K. ,  MOLINEAUX, Christopher

IPC分类号： A61K31/433 ,  A61K31/501 ,  A61K31/4245 ,  A61P31/12 ,  A61P35/00 ,  A61P37/00

摘要： In some aspects, the invention relates to a method of treating cancer, a myeloproliferative disease, an immunological disease, a neurological disease, or a viral infection, comprising orally administering a compound of formula I, formula II, formula III, formula IV, formula V, and/or formula VI, wherein the compound is administered with a meal (e.g., with food as defined herein) or in fed mode.

公开(公告)号：EP3277275A1

公开(公告)日：2018-02-07

申请号：EP16774164.4

申请日：2016-03-31

申请人： Monsanto Technology LLC

发明人： WALKER, Daniel P. ,  MILLER, William H.

IPC分类号： A61K31/4245 ,  C07D271/06 ,  C07D333/10

CPC分类号： C07D333/38 ,  C07D271/06 ,  C07D333/12 ,  C07D333/22

摘要： Provided herein are processes for the preparation of 2-thiophenecarbonyl chloride, which is useful, for example, in the preparation of 3,5-disubstituted-1,2,4-oxadiazoles, such as tioxazafen (3-phenyl-5-(2-thienyl)-1,2,4-oxadiazole).

公开(公告)号：EP3265460A1

公开(公告)日：2018-01-10

申请号：EP16758437.4

申请日：2016-02-19

申请人： Eli Lilly and Company

发明人： HU, Zhi Long ,  LIU, Lian Zhu ,  MA, Tianwei ,  ZHANG, Haizhen ,  ZHOU, Jingye

IPC分类号： C07D405/14 ,  C07D309/02 ,  C07D233/58 ,  C07D233/56 ,  C07D235/04 ,  C07D249/08 ,  A61K31/4196 ,  A61K31/4245 ,  A61P3/10

CPC分类号： C07D405/14 ,  A61K2121/00 ,  A61P3/10 ,  C07D413/14 ,  C07D471/04 ,  C07D498/04

摘要： wherein R, R1-R3 are as described herein; methods of treating patients for diabetes using the compounds, and processes for preparing the compounds

公开(公告)号：EP3148539A4

公开(公告)日：2018-01-03

申请号：EP15803976

申请日：2015-06-01

申请人： CHDI FOUNDATION INC

发明人： DOMINGUEZ CELIA ,  MUN OZ-SANJUAN IGNACIO ,  LUCKHURST CHRISTOPHER A ,  ALLEN DANIEL R ,  RAPHY GILLES ,  BÛRLI ROLAND W ,  BRECCIA PERLA ,  HAUGHAN ALAN F ,  WISHART GRANT ,  HUGHES SAMANTHA J ,  JARVIS REBECCA E ,  VATER HUW D ,  PENROSE STEPHEN D ,  WALL MICHAEL ,  STOTT ANDREW J ,  SAVILLE-STONES ELIZABETH

IPC分类号： C07D231/54 ,  A61K31/423 ,  A61K31/4245 ,  A61K31/4709 ,  A61P25/28 ,  C07D275/04 ,  C07D277/60 ,  C07D401/04 ,  C07D403/04 ,  C07D417/04

CPC分类号： C07D417/04 ,  C07C259/08 ,  C07D231/54 ,  C07D231/56 ,  C07D239/70 ,  C07D239/74 ,  C07D239/88 ,  C07D275/04 ,  C07D277/60 ,  C07D401/04 ,  C07D403/04

摘要： Provided are certain histone deacetylase (HDAC) inhibitors of Formula I, or pharmaceutically acceptable salts thereof, compositions thereof, and methods of their use. The condition or disorder mediated by HDAC comprises a neurodegenerative pathology. Accordingly, also provided is a method of treating a neurodegenerative pathology mediated by HDAC in a subject in need of such a treatment, comprising administering to the subject a therapeutically effective amount of at least one compound, or pharmaceutically acceptable salt thereof, described herein.

公开(公告)号：EP3256465A2

公开(公告)日：2017-12-20

申请号：EP16749947.4

申请日：2016-02-12

申请人： University of Southern California

发明人： LONGO, Valter D. ,  BALASUBRAMANIAN, Priya ,  NEAMATI, Nouri ,  WEI, Min

IPC分类号： C07D405/12 ,  C07D405/14 ,  A61K31/55 ,  A61K31/4245 ,  A61K31/4184 ,  A61K39/395 ,  A61P25/00 ,  A61P25/28

CPC分类号： C07D413/12 ,  A61K31/4245 ,  A61K31/55 ,  A61K45/06 ,  A61K2039/505 ,  A61P25/00 ,  A61P35/00 ,  C07D307/68 ,  C07D405/06 ,  C07D405/12 ,  C07D405/14 ,  C07K16/26 ,  C07K16/2869 ,  C07K2317/21 ,  C07K2317/33 ,  C07K2317/34 ,  C07K2317/75 ,  C07K2317/76

摘要： Compounds and methods for treating diseases or conditions affected by the activity or expression of genes/proteins related to human GH, GHR, STAT5, SOCS, IGF-1, insulin are provided. Monoclonal antibodies for treating diseases or conditions related to growth hormone and growth hormone receptor activity are also provided.

公开(公告)号：EP2559689B1

公开(公告)日：2017-11-29

申请号：EP12185448.3

申请日：2007-09-24

申请人： PTC Therapeutics, Inc.

发明人： Almstead, Neil G. ,  Hwang, Peter Seongwoo ,  Moon, Young-Choon

IPC分类号： C07D271/06 ,  A61K31/4245

CPC分类号： A61K31/4245 ,  C07D271/06

摘要： The present invention relates to preparation processes for crystalline forms of 3-[5-(2-fluorophenyl)-[1,2,4]oxadiazol-3-yl]-benzoic acid, pharmaceutical compositions and dosage forms comprising the crystalline forms, methods of making the crystalline forms and methods for their use for the treatment, prevention or management of diseases ameliorated by modulation of premature translation termination or nonsense-mediated mRNA decay.

公开(公告)号：EP3246322A1

公开(公告)日：2017-11-22

申请号：EP15877758.1

申请日：2015-12-15

申请人： National University Corporation Kobe University

发明人： MATSUBARA, Ryosuke ,  ANDO, Akihiro ,  HAYASHI, Masahiko

IPC分类号： C07D271/08 ,  A61K31/4245 ,  A61P9/10 ,  A61P25/08 ,  A61P25/28 ,  A61P35/00

CPC分类号： C07D271/08 ,  A61K31/4245

摘要： The present invention provides: a furoxan compound having a fluorine atom as a substituent group on the ring structure thereof; and a novel nitric oxide donor including the compound. The present invention relates to a fluorofuroxan compound represented by general formula (1) or (2). The compound of formula (1) can be manufactured by reacting a fluoride salt with a nitrofuroxan compound to substitute the nitro group with a fluoro group. The compound of formula (2) can be manufactured by subjecting the compounds of formula (1) to isomerization by irradiation with light.

摘要翻译： 本发明提供：在其环结构上具有氟原子作为取代基的呋喃酮化合物; 和包含该化合物的新型一氧化氮供体。 本发明涉及由通式（1）或（2）表示的氟代糠醛化合物。 式（1）化合物可以通过使氟化物盐与硝基糠醛化合物反应以用硝基取代硝基来制造。 式（2）的化合物可以通过将式（1）的化合物用光照射进行异构化来制备。

公开(公告)号：EP2970131B1

公开(公告)日：2017-11-15

申请号：EP14715525.3

申请日：2014-03-14

申请人： Epizyme, Inc.

发明人： CHESWORTH, Richard ,  MITCHELL, Lorna, Helen ,  SHAPIRO, Gideon

IPC分类号： C07D231/12 ,  C07D233/54 ,  C07D249/06 ,  C07D263/32 ,  C07D285/06 ,  A61K31/4245 ,  A61P35/00

CPC分类号： C07D285/10 ,  A61P35/00 ,  C07D231/12 ,  C07D231/14 ,  C07D233/54 ,  C07D233/64 ,  C07D249/06 ,  C07D261/08 ,  C07D263/32 ,  C07D285/06 ,  C07D405/12

摘要： Described herein are compounds of Formula (I), pharmaceutically acceptable salts thereof, and pharmaceutical compositions thereof. Compounds of the present invention are useful for inhibiting arginine methyltransferase activity. Methods of using the compounds for treating arginine methyltransferase-mediated disorders are also described.

公开(公告)号：EP3097097B1

公开(公告)日：2017-10-04

申请号：EP15701944.9

申请日：2015-01-19

申请人： F. Hoffmann-La Roche AG

发明人： GAO, Lu ,  LIANG, Chungen ,  WANG, Lisha ,  YUN, Hongying

IPC分类号： C07D413/04 ,  A61K31/4245 ,  A61P31/00

CPC分类号： C07D413/04