公开(公告)号：US20210171508A1

公开(公告)日：2021-06-10

申请号：US16761365

申请日：2018-11-02

申请人： Calico Life Sciences LLC ,  AbbVie Inc.

发明人： Kathleen Ann Martin ,  Carmela Sidrauski ,  Jennifer M. Frost ,  Lei Shi ,  Yunsong Tong ,  Michael J. Dart ,  Kathleen J. Murauski

IPC分类号： C07D405/12 ,  C07D213/40 ,  C07D487/04 ,  C07D213/75 ,  C07D309/14 ,  C07D235/14 ,  C07D207/08 ,  C07D263/32 ,  C07D413/14 ,  C07D205/04 ,  A61K45/06

摘要： Provided herein are compounds, compositions, and methods useful for modulating the integrated stress response (ISR) and for treating related diseases; disorders and conditions.

公开(公告)号：US20210171439A1

公开(公告)日：2021-06-10

申请号：US16771387

申请日：2018-12-10

申请人： VenatoRx Pharmaceuticals, Inc.

发明人： Christopher J. BURNS ,  Glen COBURN ,  Bin LIU ,  Jiangchao YAO ,  Christopher BENETATOS ,  Steven A. Boyd ,  Stephen M. CONDON

IPC分类号： C07C233/64 ,  A61K45/06 ,  C07D211/46 ,  C07D307/66 ,  C07D265/30 ,  C07D309/14

摘要： Described herein are hepatitis B capsid assembly modulators and pharmaceutical compositions comprising said compounds. The subject compounds and compositions are useful for the treatment of hepatitis B.

公开(公告)号：US10941129B2

公开(公告)日：2021-03-09

申请号：US16303646

申请日：2017-05-23

申请人： Institute of Materia Medica, Chinese Academy of Medical Sciences ,  Tianjin Chase Sun Pharmaceutical Co., LTD

发明人： Zhiqiang Feng ,  Xiaoguang Chen ,  Yang Yang ,  Fangfang Lai ,  Ming Ji ,  Lijing Zhang ,  Yi Zheng ,  Nina Xue ,  Ke Wang ,  Ling Li

IPC分类号： C07D295/155 ,  C07C233/36 ,  C07C255/54 ,  C07D405/12 ,  C07C311/05 ,  C07D319/18 ,  C07D207/16 ,  C07C45/61 ,  C07C231/12 ,  C07D401/14 ,  A61P35/00 ,  C07C211/29 ,  C07C229/36 ,  C07C235/34 ,  C07D221/00 ,  C07D265/30 ,  C07D407/12 ,  C07D269/02 ,  C07C271/64 ,  C07C227/12 ,  C07C269/02 ,  C07D207/08 ,  C07D309/14 ,  C07D319/16 ,  A61K31/36 ,  A61K31/165 ,  A61K31/277 ,  A61K45/06

摘要： The present invention discloses a benzyl phenyl ether derivative, a preparation method therefor, and a pharmaceutical composition and uses thereof. Specifically, the invention relates to benzyl phenyl ether derivatives represented by formula (I), a pharmaceutically-acceptable salt thereof, a stereoisomer thereof, a preparation method therefor, a pharmaceutical composition containing the one or more compounds, and uses of the compounds in treating diseases related to PD-1/PD-L1 signal channels, such as cancers, infectious diseases and autoimmune diseases.

公开(公告)号：US20210024462A1

公开(公告)日：2021-01-28

申请号：US17065463

申请日：2020-10-07

申请人： JANSSEN SCIENCES IRELAND UNLIMITED COMPANY

发明人： Koen VANDYCK ,  Stefaan Julien LAST ,  Geert ROMBOUTS ,  Wim Gaston VERSCHUEREN ,  Pierre Jean-Marie Bernard RABOISSON

IPC分类号： C07C311/37 ,  C07C311/14 ,  A61K31/18 ,  A61K31/337 ,  A61K31/341 ,  A61K31/351 ,  A61K31/4164 ,  A61K31/426 ,  A61K31/44 ,  A61K31/4453 ,  A61K31/4468 ,  C07C311/16 ,  C07C311/20 ,  C07C311/51 ,  C07D211/96 ,  C07D305/08 ,  C07D307/22 ,  C07D205/04 ,  C07D207/273 ,  C07D213/42 ,  C07D307/60 ,  C07D213/81 ,  C07D213/82 ,  C07D333/38 ,  C07D333/48 ,  C07D233/90 ,  C07D491/107 ,  C07D207/14 ,  C07D207/36 ,  C07D277/56 ,  C07D211/28 ,  C07D295/13 ,  C07D211/56 ,  C07D211/76 ,  C07D295/26 ,  C07D307/68 ,  C07D493/08 ,  A61K31/34 ,  A61K31/397 ,  A61K31/495 ,  A61K31/5375 ,  A61K31/55 ,  C07D223/06 ,  C07D233/84 ,  C07D309/14 ,  A61K31/401 ,  A61K45/06

摘要： Inhibitors of HBV replication of Formula (I) including stereochemically isomeric forms, and salts, hydrates, solvates thereof, wherein B, R1, R2 and R4 have the meaning as defined herein. The present invention also relates to processes for preparing said compounds, pharmaceutical compositions containing them and their use, alone or in combination with other HBV inhibitors, in HBV therapy.

公开(公告)号：US10435383B2

公开(公告)日：2019-10-08

申请号：US15560858

申请日：2016-02-01

申请人： OKINAWA INSTITUTE OF SCIENCE AND TECHNOLOGY SCHOOL CORPORATION

发明人： Fujie Tanaka ,  Sherida Johnson

IPC分类号： C07D307/22 ,  C07D309/14

摘要： The present invention can provide novel C-glycoside derivatives which are biologically important under high stereoselective, mild, atom economical condition.

公开(公告)号：US20190284153A1

公开(公告)日：2019-09-19

申请号：US16324884

申请日：2017-08-11

申请人： CHIA TAI TIANQING PHARMACEUTICAL GROUP CO., LTD. ,  Lianyungang Runzhong Pharmaceutical Co., Ltd. ,  CENTAURUS BIOPHARMA CO., LTD.

发明人： Guangming Sang ,  Lin Liu ,  Aiming Zhang ,  Jiabin Qiao ,  Xiaopeng Guo ,  Xiquan Zhang ,  Chunguang Xia

IPC分类号： C07D309/14 ,  A61P3/10

摘要： The present application relates a crystal of a compound represented by Formula (I), a salt thereof, and a crystal of the salt thereof, a method for preparing the crystal of the compound represented by Formula (I), the salt thereof, and the crystal of the salt thereof, a crystal comprising the compound represented by Formula (I), a crystal composition comprising the crystal of the salt thereof, a pharmaceutical composition thereof, and medical uses thereof.

公开(公告)号：US10399933B2

公开(公告)日：2019-09-03

申请号：US15564153

申请日：2016-04-01

申请人： BRISTOL-MYERS SQUIBB COMPANY

发明人： James Aaron Balog ,  Weiwei Guo ,  Audris Huang ,  Jay A. Markwalder ,  Weifang Shan ,  David K. Williams ,  Susheel Jethanand Nara ,  Saumya Roy

IPC分类号： C07D309/14 ,  C07C275/40 ,  C07D211/10 ,  A61K31/17 ,  A61K31/196 ,  A61K31/277 ,  A61K31/351 ,  A61K31/382 ,  A61K31/397 ,  A61K31/428 ,  A61K31/437 ,  A61K31/445 ,  A61K31/501 ,  A61K31/505 ,  A61K31/506 ,  A61K31/519 ,  A61K31/5375 ,  A61K31/5377 ,  A61K31/538 ,  A61K39/395 ,  C07C229/42 ,  C07C255/58 ,  C07D205/04 ,  C07D211/14 ,  C07D239/47 ,  C07D265/36 ,  C07D277/64 ,  C07D295/155 ,  C07D309/04 ,  C07D335/02 ,  C07D401/12 ,  C07D405/12 ,  C07D405/14 ,  C07D409/12 ,  C07D413/12 ,  C07D417/12 ,  C07D471/04 ,  C07D487/04 ,  C07D407/12 ,  C07D487/08 ,  C07D265/30 ,  C07D207/08 ,  C07D211/08 ,  C07D307/22 ,  C07C255/57 ,  C07C235/38 ,  C07C235/56 ,  C07C233/81 ,  C07C275/42 ,  C07D207/12 ,  C07D239/34 ,  C07D317/46 ,  C07D413/14 ,  C07D471/08 ,  C07C275/30 ,  A61K45/06

摘要： There are disclosed compounds of formula (I) that modulate or inhibit the enzymatic activity of indoleamine-2,3-dioxygenase (IDO), pharmaceutical compositions containing said compounds and methods of treating proliferative disorders, such as cancer, viral infections and/or inflammatory disorders utilizing the compounds of the invention.

公开(公告)号：US10399932B2

公开(公告)日：2019-09-03

申请号：US15564146

申请日：2016-04-01

申请人： BRISTOL-MYERS SQUIBB COMPANY

发明人： James Aaron Balog ,  Emily Charlotte Cherney ,  Jay A. Markwalder ,  Steven P. Seitz ,  Weifang Shan ,  David K. Williams ,  Audris Huang ,  Susheel Jethanand Nara ,  Saumya Roy ,  Soodamani Thangavel ,  Ramesh Kumar Sistla ,  Srinivas Cheruku ,  Srinivasan Thangathirupathy ,  Yadagiri Kanyaboina ,  Nagalakshmi Pulicharla

IPC分类号： C07D309/14 ,  C07D405/12 ,  C07D413/12 ,  C07D335/02 ,  C07D211/10 ,  C07D265/30 ,  C07D409/12 ,  C07C275/40 ,  A61K31/17 ,  A61K31/196 ,  A61K31/277 ,  A61K31/351 ,  A61K31/382 ,  A61K31/397 ,  A61K31/428 ,  A61K31/437 ,  A61K31/445 ,  A61K31/501 ,  A61K31/505 ,  A61K31/506 ,  A61K31/519 ,  A61K31/5375 ,  A61K31/5377 ,  A61K31/538 ,  A61K39/395 ,  C07C229/42 ,  C07C255/58 ,  C07D205/04 ,  C07D211/14 ,  C07D239/47 ,  C07D265/36 ,  C07D277/64 ,  C07D295/155 ,  C07D309/04 ,  C07D401/12 ,  C07D405/14 ,  C07D417/12 ,  C07D471/04 ,  C07D487/04 ,  C07D407/12 ,  C07D487/08 ,  C07D207/08 ,  C07D211/08 ,  C07D307/22 ,  C07C255/57 ,  C07C235/38 ,  C07C235/56 ,  C07C233/81 ,  C07C275/42 ,  C07D207/12 ,  C07D239/34 ,  C07D317/46 ,  C07D413/14 ,  C07D471/08 ,  C07C275/30 ,  A61K45/06

摘要： There are disclosed compounds of formula (I) that modulate or inhibit the enzymatic activity of indoleamine-2,3-dioxygenase (IDO), pharmaceutical compositions containing said compounds and methods of treating proliferative disorders, such as cancer, viral infections and/or inflammatory disorders utilizing the compounds of the invention.

公开(公告)号：US10391068B2

公开(公告)日：2019-08-27

申请号：US14419797

申请日：2013-08-06

申请人： TRUSTEES OF BOSTON UNIVERSITY ,  UNIVERSITA DI PERUGIA

发明人： Emiliano Biasini ,  David A. Harris ,  Aaron Beeler ,  Brian R. Fluharty ,  Maria Letizia Barreca ,  Nunzio Iraci ,  Oscar Ingham

IPC分类号： A61K31/18 ,  A61K31/41 ,  A61K45/06 ,  A61K31/145 ,  A61K31/365 ,  C07C337/08 ,  C07D307/33 ,  C07D309/14 ,  A61K31/7008

摘要： The invention provides compositions and methods for treatment of neurodegenerative diseases or disorders, particularly neurodegenerative diseases and disorders associated with protein aggregation. The present invention is based on the discovery of binding regions on the surface of PrPc, referred to as PrPc Binding Domains (PBD). In particular, the inventors have identified six different binding regions on PrPc, referred to herein as PrP-binding domain-1 (PBD-1), PrP-binding domain-2 (PBD-2), PrP-binding domain-3 (PBD-3), PrP-binding domain-4 (PBD-4), PrP-binding domain-5 (PBD-5), and PrP-binding domain-6 (PBD-6), herein. The PBD-1 to PBD-6 are each defined by a cluster of amino acids located in the globular domain of the protein, e.g., in the C-terminal half of the protein (i.e., in residues 120-230). One embodiment uses residues 127-226.

公开(公告)号：US10376531B2

公开(公告)日：2019-08-13

申请号：US16023232

申请日：2018-06-29

申请人： Pfizer Inc.

发明人： Spiros Liras ,  Vincent Mascitti ,  Benjamin Thuma

IPC分类号： C07D493/08 ,  A61K31/357 ,  A61K31/706 ,  C07D309/14 ,  C07H13/04 ,  C07H15/26 ,  A61K31/7008 ,  A61K31/7056 ,  A61K38/46 ,  C07H15/08 ,  C07H15/12 ,  C07K5/065 ,  A61K47/64

摘要： Compounds of Formula (A) are described herein and the uses thereof for the treatment of diseases, conditions and/or disorders mediated by pharmaceutical compositions and the uses thereof as asialoglycoprotein receptor (ASGPR) targeting agents.