公开(公告)号：US20230339872A1

公开(公告)日：2023-10-26

申请号：US18309634

申请日：2023-04-28

申请人： Sanford Burnham Prebys Medical Discovery Institute

发明人： Layton H. SMITH ,  Anthony B. PINKERTON ,  Paul HERSHBERGER ,  Patrick MALONEY ,  Danielle MCANALLY

IPC分类号： C07D277/82 ,  C07D263/58 ,  C07D513/04 ,  A61P3/00 ,  A61P9/00

CPC分类号： C07D277/82 ,  C07D263/58 ,  C07D513/04 ,  A61P3/00 ,  A61P9/00

摘要： Provided herein are agonists of the apelin receptor for the treatment of disease. The compounds disclosed herein are useful for the treatment of a range of cardiovascular, renal and metabolic conditions.

公开(公告)号：US20230295140A1

公开(公告)日：2023-09-21

申请号：US18201715

申请日：2023-05-24

申请人： Acucela Inc.

发明人： Mark W. ORME ,  Edison S. ZUNIGA ,  Vladimir A. KUKSA ,  Russell Stuart CRAFT ,  Eduardo Moreno SAVEEDRA ,  Johannes Wilhelm Georg MEISSNER ,  Jacobus Antonius Joseph den HARTOG ,  Albert Cornelis DROS

IPC分类号： C07D413/12 ,  C07D235/08 ,  C07D249/18 ,  C07D261/20 ,  C07D263/56 ,  C07D263/58 ,  C07D277/64 ,  C07D277/82 ,  C07D413/04 ,  C07D491/107

CPC分类号： C07D413/12 ,  C07D235/08 ,  C07D249/18 ,  C07D261/20 ,  C07D263/56 ,  C07D263/58 ,  C07D277/64 ,  C07D277/82 ,  C07D413/04 ,  C07D491/107

摘要： Provided herein are compounds and methods of use thereof for the modulation of VAP-1 activity.

公开(公告)号：US20230242496A1

公开(公告)日：2023-08-03

申请号：US18001516

申请日：2021-06-15

申请人： Icahn School of Medicine At Mount Sinai

发明人： Jian JIN ,  Marta FILIZOLA ,  Aneel AGGARWAL ,  Samir PAREKH ,  Abhijeet KAPOOR ,  Shashidhar S. JATIANI ,  H. Umit KANISKAN ,  Jianping HU ,  Yudao SHEN ,  Fanye MENG ,  Lihuai QIN ,  Yulin HAN ,  Xufen YU ,  Chengwei ZHANG ,  Prashasti KUMAR ,  Rinku JAIN ,  Clement LEE

IPC分类号： C07D279/16 ,  C07D265/36 ,  C07C321/28 ,  C07D249/18 ,  C07D215/48 ,  C07D239/74 ,  C07D231/56 ,  C07D277/64 ,  C07D235/06 ,  C07D335/06 ,  C07D209/34 ,  C07D263/58 ,  C07D285/14 ,  C07D217/02 ,  C07D417/12 ,  C07D239/42 ,  C07D233/64 ,  C07D403/04 ,  C07D215/38 ,  C07D239/72 ,  C07C311/46 ,  C07D295/135 ,  C07D239/48 ,  C07D235/16 ,  C07D215/227 ,  C07D295/26 ,  C07D239/54 ,  C07D405/12

CPC分类号： C07D279/16 ,  C07D265/36 ,  C07C321/28 ,  C07D249/18 ,  C07D215/48 ,  C07D239/74 ,  C07D231/56 ,  C07D277/64 ,  C07D235/06 ,  C07D335/06 ,  C07D209/34 ,  C07D263/58 ,  C07D285/14 ,  C07D217/02 ,  C07D417/12 ,  C07D239/42 ,  C07D233/64 ,  C07D403/04 ,  C07D215/38 ,  C07D239/72 ,  C07C311/46 ,  C07D295/135 ,  C07D239/48 ,  C07D235/16 ,  C07D215/227 ,  C07D295/26 ,  C07D239/54 ,  C07D405/12

摘要： Disclosed are compounds that are chemical inhibitors of SOX11. The compounds disclosed are useful in treatment of various cancers.

公开(公告)号：US11560518B2

公开(公告)日：2023-01-24

申请号：US16754870

申请日：2018-10-10

申请人： DAI NIPPON PRINTING CO., LTD.

发明人： Mami Motooka ,  Ken-ichi Okuyama ,  Kazuyuki Okada ,  Terutaka Takahashi ,  Mitsuru Endo ,  Shunsuke Irie ,  Tsuyoshi Sakaguchi ,  Kei Akiyama ,  Kohei Ishikawa

IPC分类号： C09K19/38 ,  C08F22/24 ,  G02B5/30 ,  C07D263/58 ,  C07D277/82 ,  C07D417/14 ,  C07D519/00

摘要： A polymerizable liquid crystal compound represented by the following general formula (1): (the symbols in the general formula (1) are as described in the DESCRIPTION.)

公开(公告)号：US20220304984A1

公开(公告)日：2022-09-29

申请号：US17618829

申请日：2020-06-12

申请人： VANDERBILT UNIVERSITY

发明人： H. Charles Manning ,  Michael Schulte

IPC分类号： A61K31/42 ,  C07D209/42 ,  C07D307/85 ,  C07D333/70 ,  C07D235/24 ,  C07D263/58 ,  C07D277/68 ,  C07D471/04 ,  C07D491/048 ,  C07D495/04 ,  C07D498/04 ,  C07D513/04 ,  C07D487/04 ,  C07D473/00 ,  C07D207/34 ,  C07D333/40 ,  C07D307/68 ,  C07D231/20 ,  C07D275/03 ,  C07D261/18 ,  C07D233/90 ,  C07D277/56 ,  C07D263/40 ,  C07D249/12 ,  C07D285/08 ,  C07D271/07 ,  C07D285/13 ,  C07D271/113 ,  A61K45/06 ,  A61K31/404 ,  A61K31/343 ,  A61K31/381 ,  A61K31/4184 ,  A61K31/423 ,  A61K31/428 ,  A61K31/437 ,  A61K31/4355 ,  A61K31/4365 ,  A61K31/519 ,  A61K31/52 ,  A61K31/401 ,  A61K31/341 ,  A61K31/415 ,  A61K31/425 ,  A61K31/4164 ,  A61K31/426 ,  A61K31/421 ,  A61K31/4196 ,  A61K31/433 ,  A61K31/4245

摘要： These compounds are glutamine transporter inhibitors, e.g., alanine, serine, cysteine-preferring transporter 2 (ASCT2) inhibitors. Glutamine transporter inhibitors are useful to treat a variety of diseases, disorders, or conditions including cancer.

公开(公告)号：US20220298125A1

公开(公告)日：2022-09-22

申请号：US17830532

申请日：2022-06-02

申请人： THE UNIVERSITY COURT OF THE UNIVERSITY OF EDINBURGH

发明人： Anne Marie Jeanne BOUILLOT ,  Olivier MIRGUET ,  John LIDDLE ,  Anne Louise WALKER

IPC分类号： C07D263/58 ,  C07D413/12 ,  C07C211/13 ,  C07C211/27 ,  C07C215/10 ,  C07C223/02 ,  C07C229/26 ,  C07C279/14 ,  C07C309/30

摘要： A compound of formula (I) or a salt thereof are provided: wherein R1, X and R3 are defined in the specification, useful in the treatment of disorders mediated by KMO such as acute pancreatitis, chronic kidney disease, other conditions associated with systemic inflammatory response syndrome (SIRS), Huntington's disease, Alzheimer's disease, spinocerebellar ataxias, Parkinson's disease, AIDS-dementia complex, amylotrophic lateral sclerosis (ALS), depression, schizophrenia, sepsis, cardiovascular shock, severe trauma, acute lung injury, acute respiratory distress syndrome, acute cholecystitis, severe burns, pneumonia, extensive surgical procedures, ischemic bowel, severe acute hepatic disease, severe acute hepatic encephalopathy or acute renal failure.

公开(公告)号：US11306056B2

公开(公告)日：2022-04-19

申请号：US17093506

申请日：2020-11-09

申请人： Cardioxyl Pharmaceuticals, Inc. ,  The Johns Hopkins University

发明人： John P. Toscano ,  Frederick Arthur Brookfield ,  Andrew D. Cohen ,  Stephen Martin Courtney ,  Lisa Marie Frost ,  Vincent Jacob Kalish

IPC分类号： C07C311/00 ,  C07C317/00 ,  C07C323/00 ,  C07D231/00 ,  C07C311/48 ,  C07C317/14 ,  C07C323/67 ,  C07D213/74 ,  C07D261/10 ,  C07D263/58 ,  C07D285/125 ,  C07D295/096 ,  C07D307/82 ,  C07D333/62 ,  C07D309/12 ,  C07D317/14 ,  C07D231/18 ,  C07D333/34

摘要： The invention relates to N-hydroxysulfonamide derivatives that donate nitroxyl (HNO) under physiological conditions and are useful in treating and/or preventing the onset and/or development of diseases or conditions that are responsive to nitroxyl therapy, including heart failure and ischemia/reperfusion injury. Novel N-hydroxysulfonamide derivatives release HNO at a controlled rate under physiological conditions, and the rate of HNO release is modulated by varying the nature and location of functional groups on the N-hydroxysulfonamide derivatives.

公开(公告)号：US20210395238A1

公开(公告)日：2021-12-23

申请号：US17466394

申请日：2021-09-03

申请人： ACTELION PHARMACEUTICALS LTD

发明人： Hamed AISSAOUI ,  Martin BOLLI ,  Christoph BOSS ,  Sylvia RICHARD-BILDSTEIN ,  Patrick SIEBER

IPC分类号： C07D413/12 ,  C07D413/14 ,  C07D417/12 ,  C07D263/54 ,  C07D263/58 ,  C07D277/62 ,  A61P11/00 ,  A61P35/04 ,  C07D417/14 ,  C07D471/10 ,  C07D491/107

摘要： The invention relates to 2,5-disubstituted benzoxazole and benzothiazole derivatives of Formula (I) wherein L, X, Y, and ring (A) are as described in the description, their preparation and their use as pharmaceutically active compounds. Said compounds may be useful for the prevention or treatment of diseases or disorders associated with impaired reactive oxygen species (ROS) production, and/or for the prevention or treatment of various fibrotic diseases.

公开(公告)号：US11034691B2

公开(公告)日：2021-06-15

申请号：US16437007

申请日：2019-06-11

申请人： The Scripps Research Institute

发明人： Edward Roberts ,  Hugh Rosen ,  Mariangela Urbano ,  Miguel Guerrero

IPC分类号： C07D471/04 ,  C07D239/26 ,  C07D213/78 ,  C07D241/42 ,  C07D249/08 ,  C07D263/32 ,  C07D271/10 ,  C07D413/14 ,  C07D213/38 ,  C07D213/55 ,  C07D213/61 ,  C07D213/75 ,  C07D213/80 ,  C07D215/12 ,  C07D217/18 ,  C07D235/14 ,  C07D237/08 ,  C07D239/30 ,  C09B55/00 ,  C07D213/40 ,  C07D211/16 ,  C07D285/12 ,  C07D271/06 ,  C07D413/12 ,  C07D413/06 ,  C07D413/04 ,  C07D409/12 ,  C07D405/12 ,  C07D405/06 ,  C07D401/12 ,  C07D333/20 ,  C07D309/14 ,  C07D309/06 ,  C07D241/16 ,  C07D263/58 ,  C07C255/63

摘要： The invention provides compounds effective as sphingosine-1-phosphate receptor modulators for treatment of cardiopulmonary diseases, such as hypertension (including malignant hypertension), angina, myocardial infarction, cardiac arrhythmias, congestive heart failure, coronary heart disease, atherosclerosis, angina pectoris, dysrhythmias, cardiomyothopy (including hypertropic cardiomyothopy), heart failure, cardiac arrest, bronchitis, asthma, chronic obstructive pulmonary disease, cystic fibrosis, croup, emphysema, pleurisy, pulmonary fibrosis, pneumonia, pulmonary embolus, pulmonary hypertension, mesothelioma, ventricular conduction abnormalities, complete heart block, adult respiratory distress syndrome, sepsis syndrome, idiopathic pulmonary fibrosis, scleroderma, systemic sclerosis, retroperitoneal fibrosis, prevention of keloid formation, or cirrhosis.

公开(公告)号：US20210163402A1

公开(公告)日：2021-06-03

申请号：US16926536

申请日：2020-07-10

申请人： Epiodyne, Inc.

发明人： Julio Cesar Medina ,  Lawrence R McGee ,  Zhi-Liang Wei ,  Corinne Sadlowski ,  Frederick Seidl ,  Ulhas Bhatt ,  Xiaodong Wang ,  Thomas Nguyen ,  David Sperandio ,  Pingyu Ding ,  Alok Nerurkar ,  Yihong Li ,  Jason Duquette

IPC分类号： C07C233/78 ,  C07C275/24 ,  C07C271/20 ,  C07C237/48 ,  C07D213/40 ,  C07C237/30 ,  C07D217/14 ,  C07D209/34 ,  C07C233/62 ,  C07D207/16 ,  C07D209/14 ,  C07D231/56 ,  C07C237/38 ,  C07D263/58 ,  C07D295/13 ,  C07D471/04 ,  C07D241/24 ,  C07D401/12 ,  C07D217/06 ,  A61P23/00

摘要： Compounds are provided having the structure of Formula (I): or a pharmaceutically acceptable isomer, racemate, hydrate, solvate, isotope, or salt thereof, wherein A, B, L, R3, R4, R5, R6, R8, m and n are as defined herein. Such compounds modulate the opioid receptor, particulare the mu-opioid receptor (MOR) and/or the kappa-opioid receptor (KOR), and/or the delta-opioid receptor (DOR). Products containing such compounds, as well as methods for their use and preparation, are also provided.