公开(公告)号：EP3393468A1

公开(公告)日：2018-10-31

申请号：EP16880113.2

申请日：2016-12-22

申请人： X4 Pharmaceuticals, Inc.

发明人： ARBEIT, Robert D ,  RAGAN, Paula Marie

IPC分类号： A61K31/395 ,  A61K31/47 ,  A61K31/4709 ,  A61K31/4725 ,  C07D235/14 ,  C07D401/04

CPC分类号： A61K31/4709 ,  A61K9/0053 ,  A61K9/485 ,  A61K9/4858 ,  A61K9/4866 ,  C07D235/14 ,  C07D401/04 ,  C07D401/12

摘要： The present invention relates to methods of treating patients with WHIM syndrome or related disorders, such as myelokathexis, in which X4P-001 is administered in order to reduce the activity of CXCR4. The methods demonstrate surprising effectiveness, with comparatively little toxicity.

公开(公告)号：EP3388425A1

公开(公告)日：2018-10-17

申请号：EP16873130.5

申请日：2016-12-09

申请人： Teijin Pharma Limited

发明人： HOSODA, Shinnosuke ,  UNOKI, Gen ,  WATANABE, Hidekazu ,  SASAKI, Kosuke ,  SHIBATA, Jun ,  YOKOYAMA, Emi ,  HORIE, Kyohei ,  TAKAGI, Kenichiro

IPC分类号： C07D263/48 ,  A61K31/421 ,  A61K31/422 ,  A61K31/4245 ,  A61K31/426 ,  A61K31/427 ,  A61K31/428 ,  A61K31/433 ,  A61K31/4439 ,  A61K31/454 ,  A61K31/4709 ,  A61K31/4725 ,  A61K31/497 ,  A61K31/498 ,  A61K31/501 ,  A61K31/5377 ,  A61P21/00 ,  A61P21/04 ,  A61P43/00 ,  C07C335/12

摘要： A compound, represented by the following formula or a medically acceptable salt thereof, having an effect of regulating the activity of an androgen receptor. In the formula, X represents S, O; Z represents (R a ) n -A-(CR 13 R 14 ) 0-1 -(CR 11 R 12 ) 0-1 -; A represents aryl, heteroaryl; R 1 represents alkyl, cycloalkyl, alkenyl, alkynyl, alkoxyalkyl, aryl, arylalkyl, heterocycle, heterocyclic alkyl; R 2 represents hydrogen, halogen, alkyl, cycloalkyl, phenyl; R3 represents hydrogen, halogen, alkyl, cycloalkyl, alkoxyalkyl, alkenyl, alkynyl, cycloalkenyl, aryl, arylalkyl, heterocycle, heterocyclic alkyl, acyl, cycloalkylcarbonyl, benzoyl, spiroalkyl, adamantyl, silyl, R 31 R 32 NCO-; R 4 and R 5 represent hydrogen, halogen, alkyl, phenyl, and cycloalkyl.

公开(公告)号：EP2552444B1

公开(公告)日：2018-10-10

申请号：EP11724017.6

申请日：2011-03-31

申请人： Council of Scientific & Industrial Research

发明人： KUMARAVEL, Somasundaram ,  CHANDRA, Nagasuma

IPC分类号： A61K31/4725 ,  G01N33/15 ,  A61P35/00

CPC分类号： G01N33/94 ,  A61K31/4725

摘要： The present invention relates to identification of a compound which inhibits the enzyme NMPRTase and glioma cancer cell growth and further used for glioma therapy. Pre-B-cell colony enhancing factor 1 gene (PBEF1) encodes nicotinamide phosphoribosyltransferase (NMPRTase), which catalyzes the rate limiting step in the salvage pathway of NAD metabolism in mammalian cells. PBEF1 transcript and protein levels have been shown to be elevated in glioblastoma and a chemical inhibitor of NMPRTase has been shown to specifically inhibit cancer cells. Here a structure based drug discovery approach has been reported with an aim to develop novel inhibitors for glioblastoma therapy. Present invention relates to virtual screening using docking of ligands from a large library of 13,000 compounds against NMPRTase as the macromolecular target resulting in short listing of 34 possible ligands, of which six were tested experimentally, using the NMPRTase enzyme inhibition assay and further with the glioma cell viability assays. Of these, two compounds were found to be significantly efficacious in inhibiting the conversion of nicotinamide to NAD, and out of which one compound, 3-amino-2-benzyl-7-nitro-4-(2-quinolyl-)-1,2-dihydroisoquinolin-1-one, was found to inhibit the growth of a PBEF1 over expressing glioma derived cell line U87 also.

公开(公告)号：EP3381915A1

公开(公告)日：2018-10-03

申请号：EP16865804.5

申请日：2016-11-21

申请人： NHWA Pharma Corporation

发明人： CHEN, Yin ,  DOU, Fei ,  QIU, Yinli ,  YU, Minquan ,  ZHANG, Guisen

IPC分类号： C07D413/14 ,  C07D217/24 ,  C07D405/12 ,  C07D417/12 ,  C07D401/12 ,  C07D239/88 ,  C07D239/90 ,  A61K31/517 ,  A61K31/4725 ,  A61K31/506 ,  A61K31/496

CPC分类号： C07D413/14 ,  A61K31/4725 ,  A61K31/496 ,  A61K31/506 ,  A61K31/517 ,  C07D217/24 ,  C07D239/88 ,  C07D239/90 ,  C07D401/12 ,  C07D405/12 ,  C07D409/12 ,  C07D417/12

摘要： The present invention relates to a lactam compound derivative, a medicine composition comprising the lactam compound derivative, and uses of the composition and the lactam compound derivative in preparation of a medicine for preventing or treating schizophrenia, the lactam compound derivative having a structure as shown in Formula I.

公开(公告)号：EP2638021B1

公开(公告)日：2018-09-26

申请号：EP11839513.6

申请日：2011-11-10

申请人： Innocrin Pharmaceuticals, Inc.

发明人： HOEKSTRA, William, J. ,  SCHOTZINGER, Robert, J. ,  RAFFERTY, Stephen, William

IPC分类号： C07D249/04 ,  C07D401/06 ,  C07D413/10 ,  A61K31/4192 ,  A61K31/4725 ,  A61P35/00 ,  A61P9/00

CPC分类号： A61K31/4725 ,  A01N43/647 ,  A61K31/4192 ,  A61K31/422 ,  A61K31/4709 ,  A61K45/06 ,  C07D249/04 ,  C07D401/06 ,  C07D405/12 ,  C07D409/14 ,  C07D413/10 ,  C07D413/12 ,  A61K2300/00

摘要： The instant invention describes compounds having metalloenzyme modulating activity, and methods of treating diseases, disorders or symptoms thereof mediated by such metalloenzymes.

公开(公告)号：EP2935222B1

公开(公告)日：2018-09-05

申请号：EP13821599.1

申请日：2013-12-20

申请人： Epizyme, Inc.

发明人： DUNCAN, Kenneth, W. ,  CHESWORTH, Richard ,  BORIACK-SJODIN, Paula Ann ,  MUNCHHOF, Michael, John ,  JIN, Lei

IPC分类号： C07D217/12 ,  A61K31/472 ,  A61K31/4725 ,  C07D401/12 ,  C07D405/12 ,  A61P35/00 ,  A61P3/04 ,  A61P3/10 ,  A61P7/06

CPC分类号： A61K31/4725 ,  A61K31/496 ,  A61K31/498 ,  A61K31/506 ,  A61K31/5377 ,  A61K31/538 ,  A61P3/04 ,  A61P3/10 ,  A61P7/06 ,  A61P35/00 ,  C07D217/04 ,  C07D217/12 ,  C07D401/12 ,  C07D401/14 ,  C07D405/12 ,  C07D405/14 ,  C07D413/12 ,  C12N9/1007 ,  Y02A50/414

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 PRMT5 activity. Methods of using the compounds for treating PRMT5-mediated disorders are also described.

公开(公告)号：EP3359154A1

公开(公告)日：2018-08-15

申请号：EP16854369.2

申请日：2016-10-06

申请人： Suzhou Yunxuan Yiyao Keji Youxian Gongsi

发明人： ZHANG, Xiaohu

IPC分类号： A61K31/4725 ,  A61K31/444 ,  A61P43/00

CPC分类号： C07D401/14 ,  A61K31/444 ,  A61K31/4709 ,  A61K31/4725 ,  A61K31/506 ,  A61K31/517 ,  A61K31/53 ,  A61K31/541 ,  A61K45/06 ,  A61P35/02 ,  C07D401/04 ,  C07D401/12 ,  C07D403/12 ,  C07D409/14 ,  C07D417/14 ,  C07D471/04 ,  C07D487/04 ,  C07D498/04 ,  C07D513/04

摘要： Inhibitors of Wnt signaling pathway with structures of Formula I are disclosed, together with their pharmaceutical salts. Applications of compounds of Formula I in inhibiting or modulating the Wnt signaling pathway are also disclosed. Compounds of Formula I can treat disorders caused by aberrant activation of the Wnt signaling pathway.

公开(公告)号：EP3351248A1

公开(公告)日：2018-07-25

申请号：EP17200784.1

申请日：2009-12-30

申请人： Ardelyx, Inc.

发明人： Charmot, Dominique ,  Jacobs, Jeffrey W. ,  Leadbetter, Michael Robert ,  Navre, Marc ,  Carreras, Chris ,  Bell, Noah

IPC分类号： A61K31/472 ,  A61K31/4725 ,  A61P1/00 ,  A61P7/10 ,  A61P9/04 ,  A61P9/12 ,  A61K45/06 ,  A61K47/55

CPC分类号： A61K31/4725 ,  A61K31/18 ,  A61K31/472 ,  A61K31/517 ,  A61K31/662 ,  A61K31/675 ,  A61K45/06 ,  A61K47/55 ,  A61P1/00 ,  A61P7/10 ,  A61P9/04 ,  A61P9/12 ,  C07C311/29 ,  C07D215/14 ,  C07D217/04 ,  C07D217/14 ,  C07D217/16 ,  C07D401/12 ,  C07F9/3808 ,  C07F9/3834 ,  C07F9/3882 ,  C07F9/5765 ,  C07F9/60 ,  C07F9/65583 ,  Y02A50/414

摘要： The present disclosure is directed to compounds and methods for the treatment of disorders associated with fluid retention or salt overload, such as heart failure (in particular, congestive heart failure), chronic kidney disease, end-stage renal disease, liver disease, and peroxisome proliferator-activated receptor (PPAR) gamma agonist-induced fluid retention. The present disclosure is also directed to compounds and methods for the treatment of hypertension. The present disclosure is also directed to compounds and methods for the treatment of gastrointestinal tract disorders, including the treatment or reduction of pain associated with gastrointestinal tract disorders. The methods generally comprise administering to a mammal in need thereof a pharmaceutically effective amount of a compound, or a pharmaceutical composition comprising such a compound, that is designed to be substantially active in the gastrointestinal (GI) tract to inhibit NHE-mediated antiport of sodium ions and hydrogen ions therein. More particularly, the method comprises administering to a mammal in need thereof a pharmaceutically effective amount of a compound, or a pharmaceutical composition comprising such a compound, that inhibits NHE-3, -2 and/or -8 mediated antiport of sodium and/or hydrogen ions in the GI tract and is designed to be substantially impermeable to the layer of epithelial cells, or more specifically the epithelium of the GI tract. As a result of the compound being substantially impermeable, it is not absorbed and is thus essentially systemically non-bioavailable, so as to limit the exposure of other internal organs (e.g., liver, heart, brain, etc.) thereto. The present disclosure is still further directed to a method wherein a mammal is administered such a compound with a fluid-absorbing polymer, such that the combination acts as described above and further provides the ability to sequester fluid and/or salt present in the GI tract

公开(公告)号：EP3339304A1

公开(公告)日：2018-06-27

申请号：EP16382629.0

申请日：2016-12-20

申请人： Laboratorios del Dr. Esteve, S.A.

发明人： ALMANSA-ROSALES, Carmen ,  YENES-MINGUEZ, Susana ,  VIRGILI-BERNADÓ, Marina ,  ALONSO-XALMA, Mónica

IPC分类号： C07D401/12 ,  C07D405/12 ,  C07D409/02 ,  C07D409/06 ,  C07D417/12 ,  A61K31/47 ,  A61K31/4725

CPC分类号： C07D409/06 ,  C07D401/12 ,  C07D405/12 ,  C07D409/02 ,  C07D417/12

摘要： The present invention relates to new compounds of formula (I):

showing great affinity and activity towards the subunit α2δ of voltage-gated calcium channels (VGCC), especially the α2δ-1 subunit of voltage-gated calcium channels or dual activity towards subunit α2δ of voltage-gated calcium channels (VGCC), especially the α2δ-1 subunit of voltage-gated calcium channels, and the noradrenaline transporter (NET).

公开(公告)号：EP2815747B8

公开(公告)日：2018-06-27

申请号：EP12868824.9

申请日：2012-12-12

申请人： Kyukyu Pharmaceutical Co., Ltd.

发明人： ISHISE, Akihiro ,  NISHIKAWA, Hisanobu

IPC分类号： A61K47/10 ,  A61K47/20 ,  A61K9/70 ,  A61K31/4525 ,  A61K31/445 ,  A61K31/4725

CPC分类号： A61K9/7007 ,  A61K9/006 ,  A61K31/445 ,  A61K31/4525 ,  A61K31/4709 ,  A61K31/4725 ,  A61K47/10 ,  A61K47/20 ,  A61K47/38

摘要： Providedis an intraoral soluble-type filmpreparation inwhich an unpleasant taste of a drug is masked. The intraoral soluble-type film preparation comprises a drug layer containing: a drug having a bitter taste and/or an astringent taste; an alkyl sulfate at a content of 3/4 mol or more with respect to 1 mol of the drug; and a water-soluble polymer.