公开(公告)号：US20190023695A1

公开(公告)日：2019-01-24

申请号：US16068308

申请日：2016-01-14

申请人： SHANDONG UNIVERSITY

发明人： Hongxiang LOU ,  Bin SUN ,  Jun LIU

IPC分类号： C07D405/04 ,  A61P7/02

CPC分类号： C07D405/04 ,  A61P7/02 ,  C07D213/30

摘要： A novel terpene derivative-based PAR1 inhibitor, a preparation method thereof and a pharmaceutical composition including the same or a salt thereof, as well as a use of the PAR1 inhibitor and the salt thereof in preparation of medicaments for preventing and/or treating thrombotic diseases. The structural formula of the compound is as follows: The compound has the advantages of clear target, novel structure, low bleeding risk, high safety, outstanding active effect, low preparation cost and the like, and has a great application prospect in the preparation of the medicaments for treating the thrombotic diseases

公开(公告)号：US20190010154A1

公开(公告)日：2019-01-10

申请号：US15747867

申请日：2016-07-28

申请人： BRISTOL-MYERS SQUIBB COMPANY

发明人： Yeheng Zhu ,  Andrew K. Dilger ,  William R. Ewing ,  Michael J. Orwat ,  Donald J.P. Pinto

IPC分类号： C07D487/04 ,  A61P7/02

CPC分类号： C07D487/04 ,  A61P7/02 ,  C07D401/14 ,  C07D403/12 ,  C07D403/14

摘要： The present invention provides compounds of Formula (I): or stereoisomers, tautomers, or pharmaceutically acceptable salts thereof, wherein all the variables are as defined herein. These compounds are selective factor XIa inhibitors or dual inhibitors of FXIa and plasma kallikrein. This invention also relates to pharmaceutical compositions comprising these compounds and methods of treating thromboembolic and/or inflammatory disorders using the same.

公开(公告)号：US20180355056A1

公开(公告)日：2018-12-13

申请号：US15739414

申请日：2016-06-24

申请人： Jorg EDER ,  Stefan EWERT ,  Ulrich HASSIEPEN ,  Yasser KHDER ,  Lorenz MAYR ,  Samu MELKKO ,  Nikolaus SCHIERING

发明人： Jorg EDER ,  Stefan EWERT ,  Ulrich HASSIEPEN ,  Yasser KHDER ,  Lorenz MAYR ,  Samu MELKKO ,  Nikolaus SCHIERING

IPC分类号： C07K16/36 ,  C07K16/40 ,  A61K45/06 ,  A61K39/395 ,  A61P7/02

CPC分类号： C07K16/36 ,  A61K39/3955 ,  A61K45/06 ,  A61K2039/505 ,  A61P7/02 ,  C07K16/40 ,  C07K2317/21 ,  C07K2317/33 ,  C07K2317/34 ,  C07K2317/55 ,  C07K2317/56 ,  C07K2317/565 ,  C07K2317/76 ,  C07K2317/92

摘要： The present invention relates to monoclonal antibodies and antigen binding fragments thereof that bind to human Factor XI and activated Factor XI (“Factor XIa”), and pharmaceutical compositions and methods of treatment comprising the same.

公开(公告)号：US20180346424A1

公开(公告)日：2018-12-06

申请号：US15513982

申请日：2015-09-22

申请人： BAYER PHARMA AKTIENGESELLSCHAFT

发明人： Susanne RÖHRIG ,  Alexander HILLISCH ,  Stefan HEITMEIER ,  Martina Victoria SCHMIDT ,  Karl-Heinz SCHLEMMER ,  Adrian TERSTEEGEN ,  Henrik TELLER

IPC分类号： C07D213/69 ,  C07D405/06 ,  C07D401/12 ,  A61P7/02 ,  A61P27/02

CPC分类号： C07D213/69 ,  A61K9/0048 ,  A61K9/0095 ,  A61K9/2018 ,  A61K9/2027 ,  A61K9/2059 ,  A61K31/00 ,  A61K47/36 ,  A61P1/04 ,  A61P7/02 ,  A61P27/02 ,  A61P29/00 ,  C07D401/12 ,  C07D405/06

摘要： The invention relates to substituted oxopyridine derivatives and to processes for preparation thereof, and also to the use thereof for production of medicaments for treatment and/or prophylaxis of diseases, especially of cardiovascular disorders, preferably thrombotic or thromboembolic disorders, and oedemas, and also ophthalmic disorders.

公开(公告)号：US20180142010A1

公开(公告)日：2018-05-24

申请号：US15580760

申请日：2016-06-22

申请人： Alexion Pharmaceuticals, Inc.

发明人： Leonard BELL ,  Camille BEDROSIAN

IPC分类号： C07K16/18 ,  A61K39/095 ,  A61K39/395 ,  A61P27/02 ,  A61P37/06 ,  A61P19/02 ,  A61P11/00 ,  A61P9/00 ,  A61P7/00 ,  A61P7/02 ,  A61P13/12 ,  A61P15/06 ,  A61P17/00 ,  A61P25/28 ,  A61P21/04 ,  A61P29/00 ,  A61P5/14 ,  A61P3/10 ,  A61P17/06 ,  A61P25/02 ,  A61P31/04 ,  A61P31/12

CPC分类号： C07K16/18 ,  A61K39/095 ,  A61K39/3955 ,  A61K2039/545 ,  A61P3/10 ,  A61P5/14 ,  A61P7/00 ,  A61P7/02 ,  A61P9/00 ,  A61P11/00 ,  A61P13/12 ,  A61P15/06 ,  A61P17/00 ,  A61P17/06 ,  A61P19/02 ,  A61P21/04 ,  A61P25/02 ,  A61P25/28 ,  A61P27/02 ,  A61P29/00 ,  A61P31/04 ,  A61P31/12 ,  A61P37/06 ,  C07K2317/24 ,  C07K2317/76 ,  A61K2300/00

摘要： The present disclosure relates to, inter alia, a method of treating a patient in need of treatment with a C5 inhibitor or a method for inhibiting formation of terminal complement in a patient, comprising administering an effective amount of a C5 inhibitor, such as eculizumab or an eculizumab variant, to a patient who is or will be in compliance with vaccination with a Neisseria meningococcal Type B specific vaccine.

公开(公告)号：US20180118749A1

公开(公告)日：2018-05-03

申请号：US15541040

申请日：2015-08-26

申请人： Jansssen Pharmaceutica NV

发明人： Jose Ignacio ANDRES GIL ,  Christa C. Chrovian ,  Michael A. Letavic ,  Jason C. Rech ,  Dale A. Rudolph ,  Akinola Soyode Johnson

IPC分类号： C07D487/04 ,  A61P27/06 ,  A61P13/12 ,  A61P33/00 ,  A61P31/04 ,  A61P35/00 ,  A61P17/10 ,  A61P19/02 ,  A61P13/10 ,  A61P17/06 ,  A61P31/00 ,  A61P17/00 ,  A61P11/06 ,  A61P11/00 ,  A61P37/08 ,  A61P25/04 ,  A61P25/00 ,  A61P25/24 ,  A61P25/18 ,  A61P25/22 ,  A61P25/28 ,  A61P25/08 ,  A61P25/16 ,  A61P3/10 ,  A61P7/02 ,  A61P1/00 ,  A61P9/12 ,  A61P19/10

CPC分类号： C07D487/04 ,  A61P1/00 ,  A61P3/10 ,  A61P7/02 ,  A61P9/12 ,  A61P11/00 ,  A61P11/06 ,  A61P13/10 ,  A61P13/12 ,  A61P17/00 ,  A61P17/06 ,  A61P17/10 ,  A61P19/02 ,  A61P19/10 ,  A61P25/00 ,  A61P25/04 ,  A61P25/08 ,  A61P25/16 ,  A61P25/18 ,  A61P25/22 ,  A61P25/24 ,  A61P25/28 ,  A61P27/06 ,  A61P31/00 ,  A61P31/04 ,  A61P33/00 ,  A61P35/00 ,  A61P37/08

摘要： The present invention is directed to compounds of Formula (I), which includes enantiomer and diasteromers thereof: These compounds are suitable for use in the treatment of diseases associated with P2X7 receptor activity such as diseases of the autoimmune and inflammatory system, diseases of the nervous and neuro-immune system, diseases involved with neuroinflammation of the Central Nervous System (CNS) or diseases of the cardiovascular, metabolic, gastrointestinal and urogenital systems.

公开(公告)号：US20180028726A1

公开(公告)日：2018-02-01

申请号：US15551781

申请日：2016-03-08

申请人： NATIONAL UNIVERSITY CORPORATION YAMAGATA UNIVERSITY ,  OTSUKA CHEMICAL CO., LTD.

发明人： Masaru TANAKA ,  Hiroyuki ISHITOBI

IPC分类号： A61L33/06 ,  A61L31/16 ,  C08F293/00 ,  A61L31/10

CPC分类号： A61L33/064 ,  A61L29/00 ,  A61L31/00 ,  A61L31/10 ,  A61L31/16 ,  A61L2300/42 ,  A61P7/02 ,  C08F293/005 ,  C08F297/00

摘要： The present invention addresses the problem of providing a block copolymer that has excellent adhesion to a base material and that can impart excellent antithrombogenicity to the base material surface, and providing a medical device comprising the block copolymer. The block copolymer according to the present invention comprises an A block and a B block. The A block is capable of containing intermediate water. The B block is more hydrophobic than the A block. The medical device according to the present invention is obtained by coating a medical device with an antithrombotic coating agent containing the block copolymer.

公开(公告)号：US20180000795A1

公开(公告)日：2018-01-04

申请号：US15542948

申请日：2016-01-15

申请人： MERCK SHARP & DOHME CORP.

发明人： Eric Mertz ,  Weiguo Liu ,  Scott D. Edmondson ,  Amjad Ali ,  Ying-Duo Gao ,  Santhosh F. Neelamkavil ,  Sung-Sau So ,  Remond Moningka ,  Wanying Sun ,  Alan Hruza ,  Linda L. Brockunier

IPC分类号： A61K31/435 ,  A61K31/195 ,  C07D221/18 ,  C07D401/10

CPC分类号： A61K31/435 ,  A61K31/195 ,  A61K31/4375 ,  A61P7/02 ,  A61P7/04 ,  C07D221/04 ,  C07D221/18 ,  C07D401/10

摘要： The present invention provides a compound of Formula (I) and pharmaceutical compositions comprising one or more said compounds, and methods for using said compounds for treating or preventing thromboses, embolisms, hypercoagulability or fibrotic changes. The compounds are selective Factor XIa inhibitors or dual inhibitors of Factor XIa and plasma kallikrein.

公开(公告)号：US20170119906A1

公开(公告)日：2017-05-04

申请号：US15209363

申请日：2016-07-13

申请人： Sangamo BioSciences, Inc.

发明人： Brigit E. Riley

IPC分类号： A61K48/00 ,  A61K38/37 ,  C07K14/755 ,  A61K45/06 ,  C12N15/86 ,  C12N7/00

CPC分类号： A61K48/0058 ,  A61K38/00 ,  A61K38/37 ,  A61K45/06 ,  A61K48/00 ,  A61P7/02 ,  C07K14/755 ,  C12N7/00 ,  C12N15/86 ,  C12N15/907 ,  C12N2750/14143 ,  C12N2750/14145 ,  C12N2750/14171 ,  C12N2830/008 ,  C12N2830/42 ,  C12N2830/60

摘要： Described herein are constructs used for liver-specific expression of a transgene.

公开(公告)号：US20170073330A1

公开(公告)日：2017-03-16

申请号：US15361589

申请日：2016-11-28

申请人： BRISTOL-MYERS SQUIBB COMPANY

发明人： Michael J. Orwat ,  Donald J.P. Pinto ,  Leon M. Smith, II ,  Shefali Srivastava

IPC分类号： C07D401/14 ,  C07D217/26 ,  C07D413/14 ,  C07D487/10 ,  C07D471/10 ,  C07D491/113 ,  C07D487/04 ,  C07D491/107 ,  C07D401/10 ,  C07D487/08

CPC分类号： C07D401/14 ,  A61K31/4725 ,  A61K31/496 ,  A61K31/5377 ,  A61K31/541 ,  A61K31/55 ,  A61K31/551 ,  A61P7/02 ,  C07B2200/13 ,  C07D217/26 ,  C07D401/04 ,  C07D401/10 ,  C07D413/14 ,  C07D471/10 ,  C07D487/04 ,  C07D487/08 ,  C07D487/10 ,  C07D491/10 ,  C07D491/107 ,  C07D491/113

摘要： The present invention provides compounds of Formula (I): or stereoisomers, pharmaceutically acceptable salts thereof, wherein all of the variables are as defined herein. These compounds are inhibitors of factor XIa and/or plasma kallikrein which may be used as medicaments.

摘要翻译： 或立体异构体，其药学上可接受的盐，其中所有变量如本文所定义。 这些化合物是可用作药物的因子XIa和/或血浆激肽释放酶的抑制剂。