公开(公告)号：EP3126352B1

公开(公告)日：2018-10-17

申请号：EP15721378.6

申请日：2015-04-03

申请人： Syros Pharmaceuticals, Inc.

发明人： SPROTT, Kevin ,  MARINEAU, Jason, J. ,  SCHMIDT, Darby ,  BRADLEY, Michael ,  CIBLAT, Stephane ,  SIDDIQUI, M., Arshad ,  KABRO, Anzhelika ,  LEBLANC, Melissa ,  LEGER, Serge ,  ROY, Stephanie ,  WINTER, Dana, K. ,  MILLER, Tom ,  RIPKA, Amy ,  LI, Dansu

IPC分类号： C07D401/14 ,  C07D413/14 ,  C07D403/04 ,  C07D403/14 ,  C07D405/04 ,  C07D409/04 ,  C07D411/14 ,  C07D417/04 ,  C07D417/14 ,  C07D471/04 ,  C07D487/04 ,  C07D487/10 ,  C07D498/10 ,  A61K31/506 ,  A61P37/00 ,  A61P31/00 ,  A61P29/00

CPC分类号： C07D401/14 ,  A61K31/506 ,  A61K31/5377 ,  A61K31/551 ,  A61K45/06 ,  C07D403/04 ,  C07D403/14 ,  C07D405/04 ,  C07D409/04 ,  C07D411/14 ,  C07D413/14 ,  C07D417/04 ,  C07D417/14 ,  C07D451/04 ,  C07D471/04 ,  C07D471/10 ,  C07D487/04 ,  C07D487/10 ,  C07D498/10

摘要： The present invention provides novel compounds of Formula (I) and Formula (II) and pharmaceutically acceptable salts, solvates, hydrates, tautomers, stereoisomers, isotopically labeled derivatives, and compositions thereof. Also provided are methods and kits involving the compounds or compositions for treating or preventing proliferative diseases (e.g., cancers (e.g., leukemia, melanoma, multiple myeloma), benign neoplasms, angiogenesis, inflammatory diseases, autoinflammatory diseases, and autoimmune diseases) in a subject. Treatment of a subject with a proliferative disease using a compound or composition of the invention may inhibit the aberrant activity of cyclin-dependent kinase 7 (CDK7), and therefore, induce cellular apoptosis and/or inhibit transcription in the subject.

公开(公告)号：EP3380457A1

公开(公告)日：2018-10-03

申请号：EP16863619.9

申请日：2016-11-09

申请人： Hangzhou Jennifer Biotech Co., Ltd.

发明人： RUAN, Benfang, Helen ,  RUAN, Jennifer, Jin

IPC分类号： C07D257/04 ,  C07D401/04 ,  C07D403/04 ,  C07D405/04 ,  C07D409/04 ,  C07D413/04 ,  C07D417/04 ,  G01N21/31 ,  C12Q1/34 ,  C12Q1/32

CPC分类号： C07D257/04 ,  C07D401/04 ,  C07D403/04 ,  C07D405/04 ,  C07D409/04 ,  C07D413/04 ,  C07D417/04 ,  C12Q1/32 ,  G01N21/78 ,  G01N2333/90611 ,  G01N2333/90616

摘要： A class of compounds of monosulfonic phenyltetrazole, with the structure of 2-(R1 phenyl)-5 (2-sulfonic phenyl)-2H-tetrazole. The 2-sulfonic phenyl tetrazolium salt of this invention has advantages of low toxicity, short synthetic route, easy control of purity and quality. As the 2-sulfonic phenyl tetrazolium salts has almost no absorption at 450 nm where the reduzate has greater absorption, spectrophotometry can simply and rapidly determine the activity of glutamate dehydrogenase, or the content of NADH/NADPH.

公开(公告)号：EP3345596A3

公开(公告)日：2018-10-03

申请号：EP17202827.6

申请日：2013-09-20

申请人： RHODE ISLAND HOSPITAL ,  Midwestern University

发明人： WANDS, Jack R. ,  DE LAMONTE, Suzanne ,  AIHARA, Arihiro ,  OLSEN, Mark Jon ,  THOMAS, John-Michael

IPC分类号： A61K31/341 ,  A61P35/00 ,  C07D405/12 ,  C07D409/04 ,  C07D417/04 ,  C07D307/32 ,  C07D307/66 ,  C07D405/04

CPC分类号： C07D417/04 ,  A61P35/00 ,  C07D307/32 ,  C07D307/66 ,  C07D405/04 ,  C07D405/12 ,  C07D409/04 ,  C12Q1/26

摘要： The present invention relates to compounds which modulate (e.g., inhibit) the activity of beta-hydrolase (e.g., ASPH), including novel 2-aryl-5-amino-3(2H)-furanone and 2-heteroaryl-5-amino-3(2H)-furanone compounds, pharmaceutical compositions thereof, methods for their synthesis, and methods of using these compounds to modulate the activity of ASPH in an a cell-free sample, a cell-based assay, and in a subject. Other aspects of the invention relate to use of the compounds disclosed herein to ameliorate or treat cell proliferation disorders.

公开(公告)号：EP3368531A1

公开(公告)日：2018-09-05

申请号：EP16790849.0

申请日：2016-10-26

申请人： FMC Corporation

发明人： SELBY, Thomas Paul ,  PATEL, Kanu Maganbhai ,  STEVENSON, Thomas Martin

IPC分类号： C07D405/14 ,  C07D213/71 ,  C07D401/12 ,  C07D237/16 ,  C07D405/04 ,  C07D409/04 ,  C07D409/14

摘要： wherein X, R1, R2, R3, R4, R5, n, R6, R7, G and W are as defined in the disclosure. Also disclosed is a process for preparing the compounds of Formulae 2 and 4.

公开(公告)号：EP3360869A1

公开(公告)日：2018-08-15

申请号：EP18157384.1

申请日：2013-12-27

申请人： UBE INDUSTRIES, LTD.

发明人： Iwase, Noriaki ,  Nishida, Hiroshi ,  Okudo, Makoto ,  Ito, Masaaki ,  Kono, Shigeyuki ,  Matoyama, Masaaki ,  Ushiyama, Shigeru ,  Okanari, Eiji ,  Matsunaga, Hirofumi ,  Nishikawa, Kenji ,  Kimura, Tomio

IPC分类号： C07D333/36 ,  A61K31/381 ,  A61K31/427 ,  A61K31/443 ,  A61P13/00 ,  A61P25/00 ,  A61P29/00 ,  A61P35/00 ,  A61P37/02 ,  A61P43/00 ,  C07D409/04 ,  C07D409/14 ,  C07D417/12 ,  A61P37/00

摘要： A compound represented by the general formula (I) for use in the treatment and/or prevention of a disease accompanying fibrosis, an immunological or inflammatory disease, a central or peripheral nervous system disease, an urologic disease, or a cancer-related disease, more specifically for use in the treatment and/or prevention of non-alcoholic steatohepatitis.

公开(公告)号：EP3354648A1

公开(公告)日：2018-08-01

申请号：EP16847758.6

申请日：2016-02-29

申请人： Guizhou Bailing Group Pharmaceutical Co., Ltd.

发明人： CHEN, Lijuan ,  WEI, Yuquan

IPC分类号： C07D409/04 ,  C07D407/04 ,  C07D407/14 ,  C07D409/14 ,  C07D405/04 ,  C07D311/16 ,  A61K31/37 ,  A61K31/4709 ,  A61K31/55 ,  A61P35/00 ,  A61P29/00

CPC分类号： C07D409/04 ,  A61K31/37 ,  A61K31/4709 ,  A61K31/55 ,  A61P35/00 ,  C07D311/16 ,  C07D405/04 ,  C07D407/04 ,  C07D407/12 ,  C07D407/14 ,  C07D409/12 ,  C07D409/14

摘要： The present Invention pertains to the field of chemical medicine, particularly to 4-substituted coumarin derivatives and preparation methods and applications thereof. The Invention provides 4-substituted coumarin derivatives with a structural formula as shown in Formula I. The Invention also provides preparation methods and applications for the above 4-substituted coumarin derivatives. The compounds provided in the Invention have strong anti-tumor activity with IC50 for plural tumor cell lines between 0.01-5 nM, and it also performs better to inhibit microtubule polymerization and has diversified biological activities and low toxicity, providing new options for drug-sensitive and drug-resistant tumor cells.

公开(公告)号：EP3342767A1

公开(公告)日：2018-07-04

申请号：EP17183750.3

申请日：2009-11-24

申请人： Arena Pharmaceuticals, Inc.

发明人： TRAN, Thuy-Anh ,  IBARRA, Jason B. ,  SHIN, Young-Jun ,  ULLMAN, Brett ,  ZOU, Ning ,  ZENG, Xi

IPC分类号： C07D231/12 ,  C07D231/18 ,  C07D231/54 ,  C07D231/56 ,  C07D401/04 ,  C07D405/04 ,  C07D409/04 ,  A61K31/415 ,  A61K31/4155 ,  A61K31/416 ,  A61P9/00 ,  A61P11/00

CPC分类号： C07D409/04 ,  A61P9/00 ,  A61P11/00 ,  C07D231/12 ,  C07D231/18 ,  C07D231/54 ,  C07D231/56 ,  C07D401/04 ,  C07D405/04

摘要： Pyrazole derivatives of Formula la and pharmaceutical compositions thereof that modulate the activity of the PGI2 receptor.

Compounds of the present invention and pharmaceutical compositions thereof are directed to methods useful in the treatment of: pulmonary arterial hypertension (PAH) and related disorders; platelet aggregation; coronary artery disease; myocardial infarction; transient ischemic attack; angina; stroke; ischemia-reperfusion injury; restenosis; atrial fibrillation; blood clot formation in an angioplasty or coronary bypass surgery individual or in an individual suffering from atrial fibrillation; atherosclerosis; atherothrombosis; asthma or a symptom thereof; a diabetic-related disorder such as diabetic peripheral neuropathy, diabetic nephropathy or diabetic retinopathy; glaucoma or other disease of the eye with abnormal intraocular pressure; hypertension; inflammation; psoriasis; psoriatic arthritis; rheumatoid arthritis; Crohn's disease; transplant rejection; multiple sclerosis; systemic lupus erythematosus (SLE); ulcerative colitis; ischemia-reperfusion injury; restenosis; atherosclerosis; acne; type 1 diabetes; type 2 diabetes; sepsis; and chronic obstructive pulmonary disorder (COPD).

公开(公告)号：EP3325465A2

公开(公告)日：2018-05-30

申请号：EP16738457.7

申请日：2016-07-14

申请人： Syngenta Participations AG

发明人： EL QACEMI, Myriem ,  JEANGUENAT, André ,  PITTERNA, Thomas ,  STOLLER, André

IPC分类号： C07D403/04 ,  A01N43/56 ,  A01N43/653 ,  A01N43/80 ,  A01N43/82 ,  C07D407/04 ,  C07D409/04 ,  C07D413/04 ,  C07D417/04

CPC分类号： C07D403/04 ,  A01N43/56 ,  A01N43/653 ,  A01N43/76 ,  A01N43/78 ,  A01N43/80 ,  A01N43/82 ,  A01N53/00 ,  C07D407/04 ,  C07D409/04 ,  C07D413/04 ,  C07D417/04

摘要： Compounds of formula (I) as defined herein, to processes for preparing them, to pesticidal, in particular insecticidal, acaricidal, molluscicidal and nematicidal compositions comprising them and to methods of using them to combat and control pests such as insect, acarine, mollusc and nematode pests.

公开(公告)号：EP1945209B1

公开(公告)日：2018-05-30

申请号：EP06851682.2

申请日：2006-08-11

申请人： United States Government As Represented By The Secretary of The United States Army And The U.S. Army Medical Research & Materiel Command

发明人： BAVARI, Sina ,  PANCHAL, Rekha, G. ,  GUSSIO, Rick

IPC分类号： A01N43/50 ,  A61K31/415 ,  A61K31/4184 ,  A61K31/00 ,  A61K31/427 ,  A61K31/423 ,  A61K31/428 ,  C07D405/14 ,  C07D405/06 ,  C07D407/06 ,  C07D209/12 ,  C07D409/04 ,  C07D209/14 ,  C07D401/06 ,  C07D209/10 ,  C07D403/04 ,  C07D333/56 ,  C07D333/60 ,  C07D401/12

CPC分类号： A61K31/4184 ,  A61K31/423 ,  A61K31/427 ,  A61K31/428 ,  C07D209/10 ,  C07D209/12 ,  C07D209/14 ,  C07D333/56 ,  C07D333/60 ,  C07D401/06 ,  C07D401/12 ,  C07D403/04 ,  C07D405/06 ,  C07D405/14 ,  C07D407/06 ,  C07D409/04 ,  Y02A50/406 ,  Y02A50/473

摘要： Disclosed herein are methods of inhibiting, reducing or preventing growth of or destroying bacteria of at least one bacterial strain which comprises contacting the bacteria with the compounds disclosed herein. Also disclosed are methods of treating, inhibiting or preventing an infection or intoxication caused by bacteria of at least one bacterial strain in a subject and pharmaceutical and cosmetic compositions comprising the compounds disclosed herein.

公开(公告)号：EP3292101A1

公开(公告)日：2018-03-14

申请号：EP16725289.9

申请日：2016-05-06

申请人： Bristol-Myers Squibb Company

发明人： DUAN, Jingwu ,  DHAR, T.G. Murali ,  MARCOUX, David ,  SHI, Qing ,  BATT, Douglas G. ,  LIU, Qingjie ,  CHERNEY, Robert J. ,  CORNELIUS, Lyndon A.M. ,  SRIVASTAVA, Anurag S. ,  BEAUDOIN BERTRAND, Myra ,  WEIGELT, Carolyn A.

IPC分类号： C07D209/30 ,  C07D215/36 ,  C07D409/04 ,  C07D417/04 ,  A61K31/35 ,  A61K31/403 ,  A61K31/407 ,  A61P3/00 ,  A61P11/06 ,  A61P35/00 ,  A61P37/08

CPC分类号： C07F9/65742 ,  C07D209/30 ,  C07D209/60 ,  C07D209/70 ,  C07D215/36 ,  C07D221/10 ,  C07D401/06 ,  C07D401/12 ,  C07D403/06 ,  C07D403/12 ,  C07D405/06 ,  C07D409/04 ,  C07D409/06 ,  C07D413/06 ,  C07D413/10 ,  C07D413/12 ,  C07D417/04 ,  C07D417/06 ,  C07D417/12 ,  C07D417/14 ,  C07D471/04 ,  C07D491/052 ,  C07D491/107 ,  C07D493/08 ,  C07D495/04 ,  C07D495/08

摘要： or stereoisomers, tautomers, pharmaceutically acceptable salts, solvates, or prodrugs thereof, wherein all substituents are defined herein. Also provided are pharmaceutical compositions comprising the same. Such compounds and compositions are useful in methods for modulating RORγ activity in a cell and methods for treating a subject suffering from a disease or disorder in which the subject would therapeutically benefit from modulation of RORγ activity, for example, autoimmune and/or inflammatory disorders.