公开(公告)号：US20230028660A1

公开(公告)日：2023-01-26

申请号：US17899297

申请日：2022-08-30

申请人： The University of Sydney

发明人： Michael KASSIOU ,  William JORGENSEN ,  Lenka MUNOZ

IPC分类号： C07D213/75 ,  C07D213/82 ,  C07D241/24 ,  C07D307/66 ,  C07D317/66

摘要： The present invention relates to new pharmaceutical agents, and to their use in the treatment of proliferative diseases, such as cancer (in particular, brain cancer).

公开(公告)号：US20220220101A1

公开(公告)日：2022-07-14

申请号：US17710386

申请日：2022-03-31

申请人： Ottawa Hospital Research Institute ,  University of Ottawa

发明人： Jean-Simon Diallo ,  Christopher Noyce Boddy ,  Mark Dornan ,  Ramya Krishnan ,  Rozanne Arulanandam ,  Fabrice Le Boeuf ,  Jeffrey Smith ,  Andrew Macklin

IPC分类号： C07D413/06 ,  C07D237/14 ,  C07D207/38 ,  C07D307/60 ,  C07D307/66 ,  C07D401/06 ,  C07D403/06 ,  C07D405/04 ,  C07D405/12 ,  C07D409/06 ,  C07D307/30 ,  C07D307/58 ,  C07D405/06 ,  A61K45/06 ,  A61K31/501 ,  C12N7/00 ,  C07D207/36 ,  C07D207/456 ,  C07D317/64 ,  C07D417/06 ,  C07D471/04 ,  A61P35/02 ,  C07D209/48 ,  C07D231/08

摘要： Provided are compounds that enhance the efficacy of viruses by increasing spread of the virus in cells, increasing the titer of virus in cells, or increasing the antigen expression from a virus, gene or trans-gene expression from a virus, or virus protein expression in cells. Other uses, compositions and methods of using same are also provided.

公开(公告)号：US11261378B2

公开(公告)日：2022-03-01

申请号：US15539666

申请日：2015-12-17

申请人： DIC CORPORATION

发明人： Masahiro Horiguchi ,  Sayaka Nose ,  Akihiro Koiso

IPC分类号： C09K19/54 ,  C07C69/753 ,  C07C69/76 ,  C07D333/22 ,  C07D339/06 ,  C07D339/08 ,  C07D407/12 ,  C07D409/12 ,  C07C323/21 ,  C07D413/12 ,  C07D417/04 ,  C07D417/06 ,  C07D249/06 ,  C07C327/48 ,  C07C251/24 ,  C07D207/452 ,  C07C251/86 ,  C07C251/88 ,  C07D209/12 ,  C07D277/82 ,  C07D513/04 ,  C08F20/10 ,  G02B5/30 ,  C07C69/94 ,  C07C69/75 ,  C09K19/34 ,  C07D409/14 ,  C07D305/06 ,  C07C251/78 ,  C07D403/04 ,  C07D209/40 ,  C07D303/48 ,  C09K19/32 ,  C07D495/04 ,  C07C69/757 ,  C07C245/08 ,  C07D333/36 ,  C07D307/66 ,  C07D403/12 ,  C07D417/12 ,  C07D265/16 ,  C07D249/04 ,  C07D213/74 ,  C07C251/18 ,  C07D409/06 ,  C07D333/76 ,  C07D277/64 ,  C07D209/88 ,  C09K19/38 ,  G02F1/13363 ,  C09K19/04 ,  C08F220/30

摘要： The present invention aims to provide a polymerizable compound that has high storage stability without causing crystal precipitation when added to a polymerizable composition and to provide a polymerizable composition containing the polymerizable compound. A polymer film produced by polymerization of the polymerizable composition has a low haze, high thickness uniformity, low occurrence of nonuniform orientation, high surface hardness, high adhesiveness, and good appearances and fewer orientation defects even after ultraviolet irradiation. The present invention also aims to provide a polymer produced by polymerization of the polymerizable composition and an optically anisotropic body produced from the polymer.

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：US20200262804A1

公开(公告)日：2020-08-20

申请号：US16791252

申请日：2020-02-14

申请人： Midwestern University

发明人： Mark Jon Olsen ,  Jean Paul Seerden

IPC分类号： C07D307/66 ,  A61P35/04

摘要： Isotopically-stabilized tetronimide compounds comprising one or more deuterium atoms, derivatives, and intermediates, thereof, including methods for their synthesis, pharmaceutical compositions thereof, and methods of using these compounds to interact with target molecules in cell-free samples, cell- and tissue-based assays, animal models, and in a subject are disclosed. One aspect relates to molecules that modulate the expression or catalytic activity of aspartyl (asparaginyl) β-hydroxylase (ASPH) within or on the surface of a cell. Other aspects of the invention relate to use of the molecules disclosed herein to diagnose, ameliorate, or treat cell proliferation disorders and related diseases. Related aspects include uses of the compounds to modulate the activity of viruses, as anti-hyperlipidemia agents, and as agents to ameliorate or treat thrombosis and related cardiovascular and metabolic disorders.

公开(公告)号：US10259804B2

公开(公告)日：2019-04-16

申请号：US15514157

申请日：2015-09-23

申请人： Shifa Biomedical Corporation

发明人： Nabil Elshourbagy ,  Shaker Mousa ,  Harold Meyers

IPC分类号： C07D405/12 ,  C07D405/14 ,  C07D307/66

摘要： Endothelial Lipase (EL) inhibitors and methods of using such inhibitors for treating conditions implicating EL are provided herein. The present invention meets the needs in the field by providing small molecule inhibitors of EL function that can be used therapeutically to raise HDL cholesterol levels in blood, and can be used in the prevention and/or treatment of cholesterol and lipoprotein metabolism disorders, including, but not limited to, familial hypercholesterolemia, atherogenic dyslipidemia, atherosclerosis, and, more generally, cardiovascular disease (CVD).

公开(公告)号：US20190076380A1

公开(公告)日：2019-03-14

申请号：US16037963

申请日：2018-07-17

申请人： Elcelyx Therapeutics, Inc.

发明人： Alain D. BARON ,  Mark S. FINEMAN ,  Nigel R.A. BEELEY

IPC分类号： A61K31/155 ,  C07D249/14 ,  A61K9/16 ,  C07D207/06 ,  A61K9/28 ,  C07D409/12 ,  C07D401/04 ,  C07D307/66 ,  C07D211/14 ,  C07D207/34 ,  A61K9/20 ,  A61K31/40 ,  A61K31/454 ,  A61K31/343 ,  A61K31/485 ,  A61K31/137 ,  A61K31/357 ,  A61K9/00 ,  C07D317/58 ,  C07D307/52 ,  A61K31/341 ,  A61K31/4196 ,  C07D405/12 ,  C07D251/18 ,  A61K31/53 ,  C07D251/10 ,  C07D255/02 ,  A61K31/55 ,  A61K45/06 ,  C07C279/26 ,  A61K9/24 ,  A61K31/4453 ,  A61K31/36 ,  A61K31/381

摘要： Provided herein are methods for treating certain conditions, including diabetes, obesity, and other metabolic diseases, disorders or conditions by administrating a composition comprising a biguanide or related heterocyclic compound, e.g., metformin. Also provided herein are biguanide or related heterocyclic compound compositions, and methods for the preparation thereof for use in the methods of the present invention. Also provided herein are compositions comprising metformin and salts thereof and methods of use.

公开(公告)号：US20190002453A1

公开(公告)日：2019-01-03

申请号：US16131275

申请日：2018-09-14

申请人： Midwestern University

发明人： Mark Jon Olsen ,  John Michael Thomas

IPC分类号： C07D417/04 ,  C12Q1/26 ,  C07D409/04 ,  C07D405/12 ,  A61P35/00 ,  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：US20180009798A1

公开(公告)日：2018-01-11

申请号：US15651842

申请日：2017-07-17

申请人： MIDWESTERN UNIVERSITY

发明人： Mark Jon Olsen ,  John Michael Thomas

IPC分类号： C07D417/04 ,  C07D409/04 ,  C07D405/12 ,  C07D405/04 ,  C07D307/66 ,  C12Q1/26 ,  C07D307/32

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：US09771356B2

公开(公告)日：2017-09-26

申请号：US14430101

申请日：2013-09-20

申请人： Rhode Island Hospital ,  Midwestern University

发明人： Jack R. Wands ,  Suzanne De La Monte ,  Arihiro Aihara ,  Mark Jon Olsen ,  John-Michael Thomas

IPC分类号： C07D307/26 ,  C07D405/04 ,  C07D417/04 ,  C07D307/66 ,  C07D307/32 ,  C07D405/12 ,  C07D409/04 ,  C12Q1/26

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-hydroxylase (e.g., Asparatyl (asparaginyl) β-hydroxylase (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.