公开(公告)号：US12098134B2

公开(公告)日：2024-09-24

申请号：US17283950

申请日：2019-08-16

申请人： INDUSTRY ACADEMIC COOPERATION FOUNDATION KEIMYUNG UNIVERSITY

发明人： Young Ho Seo

IPC分类号： C07D235/12 ,  A23L33/00 ,  A23L33/10 ,  A61P35/00 ,  C07D263/57 ,  C07D277/66

CPC分类号： C07D235/12 ,  A23L33/10 ,  A23L33/30 ,  A61P35/00 ,  C07D263/57 ,  C07D277/66

摘要： A novel benzoheterocycle compound or a pharmaceutically acceptable salt thereof showed a high anti-proliferative effect against cancer cell lines. Using this, a pharmaceutical composition for preventing or treating cancer disease can comprise the compound or a pharmaceutically acceptable salt thereof as an active ingredient. In addition, a health functional food composition for preventing or improving cancer disease can include the compound or a pharmaceutically acceptable salt thereof as an active ingredient. The pharmaceutical composition or health functional food composition can effectively prevent or treat various cancer diseases.

公开(公告)号：US11584722B2

公开(公告)日：2023-02-21

申请号：US16500774

申请日：2018-04-04

申请人： Xiamen Vivohealths Technology Co., Ltd.

发明人： Xianming Deng ,  Shengcai Lin ,  Chensong Zhang

IPC分类号： C07D233/60 ,  C07D233/61 ,  C07D235/10 ,  C07D235/12

摘要： Disclosed in the invention are a type of compounds having aldolase selective inhibitory activity, a method for the preparation thereof, a pharmaceutical composition comprising the same, and use of these compounds in the manufacture of a medicament for inhibiting triglyceride and cholesterol synthesis, for reducing fatty acid synthesis, for preventing and/or treating obesity and type II diabetes, for preventing and/or treating tumor, for preventing and/or treating Parkinson's disease, for preventing and/or treating Alzheimer's disease or for prolonging the lifespan of mammals:

公开(公告)号：US20210300869A1

公开(公告)日：2021-09-30

申请号：US17032428

申请日：2020-09-25

申请人： Vitae Pharmaceuticals, LLC

发明人： David A. Claremon ,  Lawrence Wayne Dillard ,  Yi Fan ,  Stephen D. Lotesta ,  Suresh B. Singh ,  Colin M. Tice ,  Wei Zhao ,  Linghang Zhuang

IPC分类号： C07D209/10 ,  C07D405/14 ,  C07D401/06 ,  C07D235/10 ,  C07D235/12 ,  C07D401/12 ,  C07D405/06 ,  C07D471/04 ,  C07D235/26 ,  C07D401/14

摘要： Provided are indole, benzoimidazole, pyrrolopyridine, and imidazopyridine derivatives and pharmaceutical compositions thereof, which are useful in the treatment of diseases and disorders mediated by ROR. Such derivatives include e.g., those having the Formula II. as well as pharmaceutically acceptable salts thereof. The disclosed derivatives may be used for treating one or more inflammatory, metabolic, autoimmune and other diseases or disorders.

公开(公告)号：US20210238165A1

公开(公告)日：2021-08-05

申请号：US16604208

申请日：2018-04-09

申请人： Navitor Pharmaceuticals, Inc.

发明人： Sarah MAHONEY ,  Lisa MOLZ ,  Sridhar NARAYAN ,  Eddine SAIAH

IPC分类号： C07D403/10 ,  C07D498/04 ,  C07D209/42 ,  C07D405/12 ,  C07D471/04 ,  C07D403/06 ,  C07D401/12 ,  C07D413/12 ,  C07D235/12 ,  C07D413/14 ,  C07D401/04

摘要： The present invention provides compounds, compositions thereof, and methods of using the same. Compositions comprising a compound of this invention or a pharmaceutically acceptable derivative thereof and a pharmaceutically acceptable carrier, adjuvant, or vehicle. The amount of the compound in compositions of this invention is such that it is effective to measurably inhibit Rheb, in a biological sample or in a patient.

公开(公告)号：US11053203B2

公开(公告)日：2021-07-06

申请号：US16185304

申请日：2018-11-09

申请人： Ecolab USA Inc.

发明人： Pradeep Cheruku ,  Suresh R. Sriram ,  James Joseph Michels

IPC分类号： C07D235/12 ,  C07D235/18 ,  C07D235/08 ,  C07D401/04 ,  C23F11/14

摘要： 2-substituted benzimidazoles and methods of preparing the same are disclosed. The compositions may include a compound or salt thereof, an acid, and a polar aprotic solvent. The compositions may be used to inhibit corrosion of a metal surface in contact with an aqueous system, and provide enhanced protection against corrosion of metals in the aqueous system.

公开(公告)号：US20200377457A1

公开(公告)日：2020-12-03

申请号：US16999015

申请日：2020-08-20

申请人： YALE UNIVERSITY

发明人： William L. Jorgensen ,  Richard J. Bucala

IPC分类号： C07D209/18 ,  C07D235/12 ,  C07D235/24 ,  C07D249/06 ,  C07D263/58 ,  C07D275/04 ,  C07D307/80 ,  C07D307/83 ,  C07D401/04 ,  C07D401/06 ,  C07D403/04 ,  C07D405/06 ,  C07D413/04 ,  C07D417/04

摘要： The invention provides novel heterocyclic compounds, pharmaceutical compositions and methods of treatment that modulate levels of MIF expression and treat disorders associated with high or low levels of MIF expression.

公开(公告)号：US10590110B2

公开(公告)日：2020-03-17

申请号：US16385599

申请日：2019-04-16

申请人： CINRX PHARMA, LLC

发明人： Catherine Pearce ,  Jon Isaacsohn ,  Piyush Patel

IPC分类号： C07D401/14 ,  A61K31/454 ,  C07D235/12 ,  A61P1/04 ,  A61P1/08 ,  C07B59/00

摘要： Deuterated domperidone compositions, methods of synthesis, methods of use, and dosing formulations providing beneficial safety and other effects.

公开(公告)号：US20190300562A1

公开(公告)日：2019-10-03

申请号：US16356384

申请日：2019-03-18

申请人： Epizyme, Inc.

发明人： Edward James OLHAVA

IPC分类号： C07H19/16 ,  C07D235/12 ,  A61K31/4184 ,  A61K31/7076

摘要： The present invention provides an efficient process for the synthesis of (2R,3R,4S,5R)-2-(6-amino-9H-purin-9-yl)-5-((((1r,3S)-3-(2-(5-(tert-butyl)-1H-benzo[d]imidazol-2-yl)ethyl)cyclobutyl)(isopropyl)amino)methyl)tetrahydrofuran-3,4-diol and hydrates thereof and methods for treating disorders in which DOT1-mediated protein methylation plays a part, such as cancer and neurological disorders, by administering these compounds and pharmaceutical compositions to subjects in need thereof. The present invention also provides novel crystalline forms of (2R,3R,4S,5R)-2-(6-amino-9H-purin-9-yl)-5-((((1r,3S)-3-(2-(5-(tert-butyl)-1H-benzo[d]imidazol-2-yl)ethyl)cyclobutyl)(isopropyl)amino)methyl)tetrahydrofuran-3,4-diol and hydrates thereof (Form A, Form B, and Form C), characterized by a unique X-ray diffraction pattern and Differential Scanning Calorimetry profile, as well as a unique crystalline structure.

公开(公告)号：US20190300561A1

公开(公告)日：2019-10-03

申请号：US16356198

申请日：2019-03-18

申请人： Epizyme, Inc.

发明人： Edward J. OLHAVA

IPC分类号： C07H19/16 ,  C07D235/12 ,  A61K31/4184 ,  A61K31/7076

摘要： The present invention provides an efficient process for the synthesis of (2R,3R,4S,5R)-2-(6-amino-9H-purin-9-yl)-5-((((1r,3S)-3-(2-(5-(tert-butyl)-1H-benzo[d]imidazol-2-yl)ethyl)cyclobutyl)(isopropyl)amino)methyl)tetrahydrofuran-3,4-diol and hydrates thereof and methods for treating disorders in which DOT 1-mediated protein methylation plays a part, such as cancer and neurological disorders, by administering these compounds and pharmaceutical compositions to subjects in need thereof. The present invention also provides novel crystalline forms of (2R,3R,4S,5R)-2-(6-amino-9H-purin-9-yl)-5-((((1r,3S)-3-(2-(5-(tert-butyl)-1H-benzo[d]imidazol-2-yl)ethyl)cyclobutyl)(isopropyl)amino)methyl)tetrahydrofuran-3,4-diol and hydrates thereof (Form A, Form B, and Form C), characterized by a unique X-ray diffraction pattern and Differential Scanning Calorimetry profile, as well as a unique crystalline structure.

公开(公告)号：US20190241543A1

公开(公告)日：2019-08-08

申请号：US16385599

申请日：2019-04-16

申请人： CINRX PHARMA, LLC

发明人： Catherine Pearce ,  Jon Isaacsohn ,  Piyush Patel

IPC分类号： C07D401/14 ,  A61K31/454 ,  C07B59/00 ,  C07D235/12 ,  A61P1/08 ,  A61P1/04

摘要： Deuterated domperidone compositions, methods of synthesis, methods of use, and dosing formulations providing beneficial safety and other effects.