公开(公告)号：US12065459B2

公开(公告)日：2024-08-20

申请号：US16672114

申请日：2019-11-01

申请人： Achillion Pharmaceuticals, Inc.

发明人： Jason Allan Wiles ,  Venkat Rao Gadhachanda ,  Qiuping Wang ,  Godwin Pais ,  Akihiro Hashimoto ,  Dawei Chen ,  Xiangzhu Wang ,  Atul Agarwal ,  Milind Deshpande ,  Avinash S. Phadke

IPC分类号： C07F9/572 ,  A61K9/00 ,  A61K31/404 ,  A61K31/4045 ,  A61K31/407 ,  A61K31/4162 ,  A61K31/4178 ,  A61K31/4184 ,  A61K31/4188 ,  A61K31/4192 ,  A61K31/437 ,  A61K31/4439 ,  A61K31/444 ,  A61K31/4709 ,  A61K31/496 ,  A61K31/501 ,  A61K31/506 ,  A61K31/519 ,  A61K31/549 ,  A61K31/55 ,  A61K31/675 ,  A61K31/683 ,  C07B59/00 ,  C07D209/12 ,  C07D209/14 ,  C07D209/30 ,  C07D209/40 ,  C07D209/42 ,  C07D209/44 ,  C07D209/88 ,  C07D401/14 ,  C07D403/06 ,  C07D403/08 ,  C07D403/12 ,  C07D403/14 ,  C07D405/12 ,  C07D405/14 ,  C07D413/06 ,  C07D413/14 ,  C07D417/06 ,  C07D417/12 ,  C07D417/14 ,  C07D471/04 ,  C07D471/08 ,  C07D487/04 ,  C07D487/14 ,  C07D491/113 ,  C07D495/04 ,  C07D513/04 ,  C07F5/02 ,  C07F7/08 ,  C07F9/6558 ,  C07F9/6561

CPC分类号： C07F9/5728 ,  A61K9/0014 ,  A61K9/0019 ,  A61K9/0048 ,  A61K9/0053 ,  A61K31/404 ,  A61K31/4045 ,  A61K31/407 ,  A61K31/4162 ,  A61K31/4178 ,  A61K31/4184 ,  A61K31/4188 ,  A61K31/4192 ,  A61K31/437 ,  A61K31/4439 ,  A61K31/444 ,  A61K31/4709 ,  A61K31/496 ,  A61K31/501 ,  A61K31/506 ,  A61K31/519 ,  A61K31/549 ,  A61K31/55 ,  A61K31/675 ,  A61K31/683 ,  C07B59/002 ,  C07D209/12 ,  C07D209/14 ,  C07D209/30 ,  C07D209/40 ,  C07D209/42 ,  C07D209/44 ,  C07D209/88 ,  C07D401/14 ,  C07D403/06 ,  C07D403/08 ,  C07D403/12 ,  C07D403/14 ,  C07D405/12 ,  C07D405/14 ,  C07D413/06 ,  C07D413/14 ,  C07D417/06 ,  C07D417/12 ,  C07D417/14 ,  C07D471/04 ,  C07D471/08 ,  C07D487/04 ,  C07D487/14 ,  C07D491/113 ,  C07D495/04 ,  C07D513/04 ,  C07F5/025 ,  C07F5/027 ,  C07F7/0812 ,  C07F9/65583 ,  C07F9/6561 ,  C07F9/65616 ,  C07B2200/05

摘要： Compounds, methods of use, and processes for making inhibitors of complement factor D comprising Formula I, or a pharmaceutically acceptable salt or composition thereof wherein R12 or R13 on the A group is an aryl, heteroaryl or heterocycle (R32) are provided. The inhibitors described herein target factor D and inhibit or regulate the complement cascade at an early and essential point in the alternative complement pathway, and reduce factor D's ability to modulate the classical and lectin complement pathways. The inhibitors of factor D described herein are capable of reducing the excessive activation of complement, which has been linked to certain autoimmune, inflammatory, and neurodegenerative diseases, as well as ischemia-reperfusion injury and cancer.

公开(公告)号：US20240246913A1

公开(公告)日：2024-07-25

申请号：US18563606

申请日：2022-05-27

申请人： Oxford University Innovation Limited

发明人： Christopher SCHOFIELD ,  Jurgen BREM ,  Tharindi PANDUWAWALA ,  Alistair FARLEY ,  Edgars SUNA

IPC分类号： C07D209/42 ,  A61K31/405 ,  A61K31/421 ,  A61K31/4439 ,  A61P31/04 ,  C07D401/04 ,  C07D403/06 ,  C07D409/06 ,  C07D413/06 ,  C07D413/14 ,  C07D417/06

CPC分类号： C07D209/42 ,  A61K31/405 ,  A61K31/421 ,  A61K31/4439 ,  A61P31/04 ,  C07D401/04 ,  C07D403/06 ,  C07D409/06 ,  C07D413/06 ,  C07D413/14 ,  C07D417/06

摘要： The present invention relates to certain compounds that function as inhibitors of bacterial metallo-beta-lactamases. The present invention also relates to processes for the preparation of these compounds, to pharmaceutical compositions comprising them, and to their use in the treatment of a bacterial infection.

公开(公告)号：US12018033B2

公开(公告)日：2024-06-25

申请号：US17883331

申请日：2022-08-08

申请人： Forward Therapeutics, Inc.

发明人： Toufike Kanouni

IPC分类号： C07D487/10 ,  C07D209/42 ,  C07D401/06 ,  C07D401/12 ,  C07D403/06 ,  C07D403/12 ,  C07D405/12 ,  C07D487/04

CPC分类号： C07D487/10 ,  C07D209/42 ,  C07D401/06 ,  C07D401/12 ,  C07D403/06 ,  C07D403/12 ,  C07D405/12 ,  C07D487/04

摘要： Provided herein are inhibitors of protein arginine deiminases (PADs), pharmaceutical compositions comprising the compounds, and methods for using the compounds for the treatment of diseases.

公开(公告)号：US11873282B2

公开(公告)日：2024-01-16

申请号：US17027707

申请日：2020-09-22

申请人： University of Tennessee Research Foundation

发明人： Ramesh Narayanan ,  Duane D. Miller ,  Thamarai Ponnusamy ,  Dong-Jin Hwang ,  Yali He

IPC分类号： C07D209/08 ,  A61P5/26 ,  C07D401/12 ,  C07D235/06 ,  C07D471/04 ,  C07D231/56 ,  C07D249/18 ,  C07D215/06 ,  C07D217/04 ,  C07D209/88 ,  C07D209/86 ,  A61P35/00 ,  A61P25/00 ,  A61P17/10 ,  A61P17/14 ,  C07D209/42 ,  A61K31/403 ,  A61K31/404 ,  A61K31/416 ,  A61K31/4184 ,  A61K31/4192 ,  A61K31/437 ,  A61K31/47 ,  A61K31/472

CPC分类号： C07D209/08 ,  A61K31/403 ,  A61K31/404 ,  A61K31/416 ,  A61K31/4184 ,  A61K31/4192 ,  A61K31/437 ,  A61K31/47 ,  A61K31/472 ,  A61P5/26 ,  A61P17/10 ,  A61P17/14 ,  A61P25/00 ,  A61P35/00 ,  C07D209/42 ,  C07D209/86 ,  C07D209/88 ,  C07D215/06 ,  C07D217/04 ,  C07D231/56 ,  C07D235/06 ,  C07D249/18 ,  C07D401/12 ,  C07D471/04

摘要： This invention provides novel indole, indazole, benzimidazole, benzotriazole, indoline, quinolone, isoquinoline, and carbazole selective androgen receptor degrader (SARD) compounds, pharmaceutical compositions and uses thereof in treating hyperproliferations of the prostate including pre-malignancies and benign prostatic hyperplasia, prostate cancer, advanced prostate cancer, castration resistant prostate cancer, other AR-expressing cancers, androgenic alopecia or other hyper androgenic dermal diseases, Kennedy's disease, amyotrophic lateral sclerosis (ALS), abdominal aortic aneurysm (AAA), and uterine fibroids, and to methods for reducing the levels (through degradation) and/or activity (through inhibition) of any androgen receptor including androgen receptor-full length (AR-FL) including pathogenic and/or resistance mutations, AR-splice variants (AR-SV), and pathogenic polyglutamine (polyQ) polymorphisms of AR in a subject.

公开(公告)号：US11795162B2

公开(公告)日：2023-10-24

申请号：US16639807

申请日：2018-08-17

申请人： Saint Louis University

发明人： Thomas Burris ,  John K. Walker ,  Carissa S. Hampton ,  Keith McCormick Haynes ,  Kristine Griffett ,  Cyrielle Billon ,  Sadichha Sitaula

IPC分类号： C07D209/42 ,  C07D413/04 ,  C07D231/14 ,  C07D277/56 ,  C07D277/82 ,  C07D307/68 ,  C07D333/38 ,  C07D401/04 ,  C07D409/04 ,  C07D409/12 ,  C07D417/04 ,  C07F5/02

CPC分类号： C07D413/04 ,  C07D209/42 ,  C07D231/14 ,  C07D277/56 ,  C07D277/82 ,  C07D307/68 ,  C07D333/38 ,  C07D401/04 ,  C07D409/04 ,  C07D409/12 ,  C07D417/04 ,  C07F5/027

摘要： In one aspect, the present disclosure describes new estrogen receptor-related orphan receptor (EER) inverse agonist compounds. Also described are pharmaceutical formulations, methods of synthesis and uses thereof.

公开(公告)号：US11690824B2

公开(公告)日：2023-07-04

申请号：US17046463

申请日：2019-04-10

申请人： THE GENERAL HOSPITAL CORPORATION ,  RHODE ISLAND HOSPITAL, A LIFESPAN-PARTNER ,  EMORY UNIVERSITY

发明人： Frederick M. Ausubel ,  Wooseong Kim ,  Eleftherios Mylonakis ,  William M. Wuest

IPC分类号： A61K31/404 ,  C07D209/36 ,  C07D209/42 ,  A61P31/04 ,  A61K31/41 ,  A61K31/4439 ,  A61K31/7036 ,  C07D401/06 ,  C07D403/04 ,  C07D405/06

CPC分类号： A61K31/404 ,  A61K31/41 ,  A61K31/4439 ,  A61K31/7036 ,  A61P31/04 ,  C07D209/36 ,  C07D209/42 ,  C07D401/06 ,  C07D403/04 ,  C07D405/06

摘要： The present application provides compounds of formula: Methods of using these compounds for killing bacterial growth and treating bacterial infections are also provided.

公开(公告)号：US20230039586A1

公开(公告)日：2023-02-09

申请号：US17811731

申请日：2022-07-11

申请人： NIDO BIOSCIENCES, INC.

发明人： Bakary-Barry TOURE ,  Mark Andrew GALLOP

IPC分类号： C07D405/14 ,  C07D413/12 ,  C07D405/12 ,  C07D401/12 ,  C07D209/42 ,  C07D307/85 ,  C07D403/12 ,  C07D403/04 ,  C07D471/04 ,  C07D495/04

摘要： Provided herein are compounds that bind to BF3 of an androgen receptor (AR), which can modulate the AR for the treatment of Kennedy's disease

公开(公告)号：US20220324803A1

公开(公告)日：2022-10-13

申请号：US17615821

申请日：2020-06-09

申请人： Teon Therapeutics, Inc.

发明人： Jiwen Liu

IPC分类号： C07D209/42 ,  C07D231/56 ,  C07D471/04 ,  C07D401/06 ,  A61K45/06

摘要： Disclosed herein are compounds, compositions, and methods for modulating the prostaglandin E2 receptor 4 (EP4) with the compounds and compositions disclosed herein. Also described are methods of treating diseases or disorders that are mediated by the action of prostaglandin E2 (PGE2) at the prostaglandin E2 receptor 4 (EP4), such as cancer, with EP4 antagonists.

公开(公告)号：US20220306654A1

公开(公告)日：2022-09-29

申请号：US17640135

申请日：2020-09-04

申请人： NATIONAL UNIVERSITY CORPORATION HOKKAIDO UNIVERSITY

发明人： Hajime ITO ,  Koji KUBOTA

IPC分类号： C07F5/02 ,  C07D307/06 ,  C07D333/38 ,  C07D209/42 ,  C07D333/10

摘要： Disclosed are a method for producing a highly reactive intermediate, which comprises: preparing an electron-accepting active compound (1), preparing a piezoelectric material (3), and applying mechanical strain to the piezoelectric material (3) in the presence of the electron-accepting active compound (1) and the piezoelectric material (3), and subjecting the compound (1) to one-electron reduction to generate a corresponding highly reactive intermediate; a redox reaction method using the method for producing the same; and a method for producing a redox reaction product.

公开(公告)号：US20220289677A1

公开(公告)日：2022-09-15

申请号：US17750560

申请日：2022-05-23

申请人： B. G. Negev Technologies and Applications Ltd., At Ben-Gurion University

发明人： Barak AKABAYOV

IPC分类号： C07D209/42

摘要： Disclosed herein are compounds that are selective DNA primase and/or gyrase inhibitors. Further disclosed are pharmaceutical compositions comprising these compounds, and the uses of these compounds for treating disorders associated with microbial infections.