公开(公告)号：US20240294504A1

公开(公告)日：2024-09-05

申请号：US18663765

申请日：2024-05-14

申请人： The Broad Institute, Inc. ,  THE GENERAL HOSPITAL CORPORATION

发明人： Deborah HUNG ,  Christoph ERNST ,  Tomohiko KAWATE

IPC分类号： C07D401/14 ,  A61K31/085 ,  A61K31/135 ,  A61K31/40 ,  A61K31/415 ,  A61K31/454 ,  A61K31/4545 ,  A61K31/505 ,  A61P31/04 ,  C07C43/225 ,  C07D207/34 ,  C07D213/73 ,  C07D213/74 ,  C07D231/12 ,  C07D239/26 ,  C07D401/04

CPC分类号： C07D401/14 ,  A61K31/085 ,  A61K31/135 ,  A61K31/40 ,  A61K31/415 ,  A61K31/454 ,  A61K31/4545 ,  A61K31/505 ,  A61P31/04 ,  C07C43/225 ,  C07D207/34 ,  C07D213/73 ,  C07D213/74 ,  C07D231/12 ,  C07D239/26 ,  C07D401/04

摘要： Compounds, pharmaceutical compositions, and methods of use of said compounds and pharmaceutical compositions for treating or preventing a microbial infection or for inducing antimicrobial activity against a microbial infection.

公开(公告)号：US20240254079A1

公开(公告)日：2024-08-01

申请号：US18239892

申请日：2023-08-30

申请人： ARCUS BIOSCIENCES, INC.

发明人： Joel Worley BEATTY ,  Samuel Lawrie DREW ,  Matthew EPPLIN ,  Jeremy Thomas Andre FOURNIER ,  Balint GAL ,  Tezcan GUNEY ,  Karl T. HAELSIG ,  Clayton HARDMAN ,  Steven Donald JACOB ,  Jenna Leigh JEFFREY ,  Jaroslaw KALISIAK ,  Kenneth Victor LAWSON ,  Manmohan Reddy LELETI ,  Erick Allen LINDSEY ,  Artur Karenovich MAILYAN ,  Debashis MANDAL ,  Guillaume MATA ,  Hyunyoung MOON ,  Jay Patrick POWERS ,  Brandon Reid ROSEN ,  Yongli SU ,  Anh Thu TRAN ,  Zhang WANG ,  Xuelei YAN ,  Kai YU

IPC分类号： C07C317/32 ,  A61K31/10 ,  A61K31/277 ,  A61K31/343 ,  A61K31/353 ,  A61K31/365 ,  A61K31/381 ,  A61K31/404 ,  A61K31/415 ,  A61K31/416 ,  A61K31/4174 ,  A61K31/4192 ,  A61K31/4196 ,  A61K31/421 ,  A61K31/423 ,  A61K31/426 ,  A61K31/428 ,  A61K31/437 ,  A61K31/44 ,  A61K31/4412 ,  A61K31/47 ,  A61K31/4709 ,  A61K31/472 ,  A61K31/4965 ,  A61K31/50 ,  A61K31/5025 ,  A61K31/505 ,  A61K31/519 ,  A61K31/538 ,  A61K39/395 ,  A61K45/06 ,  C07C255/53 ,  C07C317/22 ,  C07C317/36 ,  C07D209/34 ,  C07D211/86 ,  C07D213/57 ,  C07D213/71 ,  C07D213/73 ,  C07D213/74 ,  C07D213/84 ,  C07D215/48 ,  C07D217/04 ,  C07D231/12 ,  C07D231/56 ,  C07D233/64 ,  C07D237/20 ,  C07D239/42 ,  C07D241/12 ,  C07D249/06 ,  C07D249/08 ,  C07D263/32 ,  C07D263/57 ,  C07D265/36 ,  C07D277/30 ,  C07D277/56 ,  C07D277/64 ,  C07D307/83 ,  C07D311/22 ,  C07D333/64 ,  C07D401/04 ,  C07D401/10 ,  C07D409/10 ,  C07D413/10 ,  C07D471/04 ,  C07D487/04

CPC分类号： C07C317/32 ,  A61K31/10 ,  A61K31/277 ,  A61K31/343 ,  A61K31/353 ,  A61K31/365 ,  A61K31/381 ,  A61K31/404 ,  A61K31/415 ,  A61K31/416 ,  A61K31/4174 ,  A61K31/4192 ,  A61K31/4196 ,  A61K31/421 ,  A61K31/423 ,  A61K31/426 ,  A61K31/428 ,  A61K31/437 ,  A61K31/44 ,  A61K31/4412 ,  A61K31/47 ,  A61K31/4709 ,  A61K31/472 ,  A61K31/4965 ,  A61K31/50 ,  A61K31/5025 ,  A61K31/505 ,  A61K31/519 ,  A61K31/538 ,  A61K39/3955 ,  A61K45/06 ,  C07C255/53 ,  C07C317/22 ,  C07C317/36 ,  C07D209/34 ,  C07D211/86 ,  C07D213/57 ,  C07D213/71 ,  C07D213/73 ,  C07D213/74 ,  C07D213/84 ,  C07D215/48 ,  C07D217/04 ,  C07D231/12 ,  C07D231/56 ,  C07D233/64 ,  C07D237/20 ,  C07D239/42 ,  C07D241/12 ,  C07D249/06 ,  C07D249/08 ,  C07D263/32 ,  C07D263/57 ,  C07D265/36 ,  C07D277/30 ,  C07D277/56 ,  C07D277/64 ,  C07D307/83 ,  C07D311/22 ,  C07D333/64 ,  C07D401/04 ,  C07D401/10 ,  C07D409/10 ,  C07D413/10 ,  C07D471/04 ,  C07D487/04 ,  C07C2602/08 ,  C07C2602/10

摘要： Compounds that inhibit HIF-2α, and compositions containing the compound(s) and methods for synthesizing the compounds, are described herein. Also described are the use of such compounds and compositions for the treatment of a diverse array of diseases, disorders, and conditions, including cancer- and immune-related disorders that are mediated, at least in part, by HIF-2α.

公开(公告)号：US20240245673A1

公开(公告)日：2024-07-25

申请号：US18532424

申请日：2023-12-07

申请人： Pfizer Inc.

发明人： James Matthew Frick ,  Michelle Renee Garnsey ,  Brian Stephen Gerstenberger ,  Xinjun Hou ,  Magdalena Korczynska ,  Alpha Albert Lee ,  Luong Tien Nguyen ,  Usa Reilly ,  Matthew Christopher Robinson ,  Alexandria Paige Taylor ,  Thomas Reynold Vargo ,  Lei Zhang

IPC分类号： A61K31/4709 ,  A61K31/415 ,  A61K31/4178 ,  A61K31/4192 ,  A61K31/427 ,  A61K31/454 ,  A61K31/496 ,  A61K31/5377 ,  A61K45/06 ,  C07D207/34 ,  C07D215/38 ,  C07D231/12 ,  C07D249/06 ,  C07D401/04 ,  C07D401/12 ,  C07D401/14 ,  C07D403/12 ,  C07D403/14 ,  C07D405/12 ,  C07D405/14 ,  C07D409/04 ,  C07D413/04 ,  C07D413/12 ,  C07D417/12 ,  C07D417/14 ,  C07D471/10 ,  C07D487/04 ,  C07D487/08 ,  C07D495/04

CPC分类号： A61K31/4709 ,  A61K31/415 ,  A61K31/4178 ,  A61K31/4192 ,  A61K31/427 ,  A61K31/454 ,  A61K31/496 ,  A61K31/5377 ,  A61K45/06 ,  C07D207/34 ,  C07D215/38 ,  C07D231/12 ,  C07D249/06 ,  C07D401/04 ,  C07D401/12 ,  C07D401/14 ,  C07D403/12 ,  C07D403/14 ,  C07D405/12 ,  C07D405/14 ,  C07D409/04 ,  C07D413/04 ,  C07D413/12 ,  C07D417/12 ,  C07D417/14 ,  C07D471/10 ,  C07D487/04 ,  C07D487/08 ,  C07D495/04

摘要： The invention relates to compounds of Formula (I)




and pharmaceutically acceptable salts thereof as defined in the description; to their use in medicine; to compositions containing them; to processes for their preparation; and to intermediates used in such processes. The compounds of Formula (I) may inhibit the activity of papain-like protease (PLpro) and may be useful in the treatment of viral infections, in particular viral infections associated with PLpro activity and/or expression such as coronaviruses infections.

公开(公告)号：US12043600B2

公开(公告)日：2024-07-23

申请号：US17285155

申请日：2019-10-17

申请人： SYNGENTA CROP PROTECTION AG

发明人： Farhan Bou Hamdan ,  Matthias Weiss ,  Atul Mahajan ,  Jagadeesh Prathap Kilaru ,  Ramya Rajan ,  Laura Quaranta ,  Stefano Rendine ,  Mathias Blum ,  Martin Pouliot ,  Simon Williams ,  Thomas James Hoffman

IPC分类号： C07D231/16 ,  A01N43/56 ,  A01N43/647 ,  C07D231/12 ,  C07D231/22 ,  C07D249/06

CPC分类号： C07D231/16 ,  A01N43/56 ,  A01N43/647 ,  C07D231/12 ,  C07D231/22 ,  C07D249/06

摘要： Compounds of the formula (I), wherein the substituents are as defined in claim 1, useful as a pesticides, especially as fungicides.

公开(公告)号：US12006292B2

公开(公告)日：2024-06-11

申请号：US17659730

申请日：2022-04-19

申请人： Konica Minolta, Inc.

发明人： Yukiko Nakai ,  Kouji Sugama ,  Kazuaki Nakamura ,  Toyoko Shibata

IPC分类号： C07D231/12 ,  C09J7/25 ,  G03G9/087 ,  G03G15/20 ,  B41J11/00 ,  C08F212/08 ,  C08F220/18 ,  C08F257/02 ,  C08F285/00 ,  G03G9/09

CPC分类号： C07D231/12 ,  C09J7/25 ,  G03G9/08708 ,  G03G9/08728 ,  G03G15/2064 ,  B41J11/0021 ,  C08F212/08 ,  C08F220/1806 ,  C08F257/02 ,  C08F285/00 ,  G03G9/0922

摘要： Provided is a compound that is fluidized by light irradiation and reversibly non-fluidized, is not significantly colored, and improves fixability and exhibits excellent image stability and color reproducibility when used for a toner.
Provided is a compound represented by the following general formula (1), which is fluidized by light irradiation and reversibly non-fluidized:






wherein
Z1 and Z2 are CH or N, and Z1≠Z2;
R1 is an aromatic hydrocarbon group having a substituent Ra selected from the group consisting of an alkyl group, an alkoxy group and a halogen atom at each of two ortho positions with respect to Z1; and
R2 is a substituted or unsubstituted aromatic heterocyclic group.

公开(公告)号：US20240092745A1

公开(公告)日：2024-03-21

申请号：US18094916

申请日：2023-01-09

申请人： Graybug Vision, Inc.

发明人： Ming Yang ,  John G. Bauman ,  Jeffrey L. Cleland ,  Nu Hoang ,  Emmett Cunningham

IPC分类号： C07D271/04 ,  C07D231/12 ,  C07D403/06 ,  C07D403/12 ,  C07D417/04 ,  C07D417/14 ,  C07D487/04 ,  C07D495/04 ,  C07D513/04

CPC分类号： C07D271/04 ,  C07D231/12 ,  C07D403/06 ,  C07D403/12 ,  C07D417/04 ,  C07D417/14 ,  C07D487/04 ,  C07D495/04 ,  C07D513/04

摘要： The present invention provides new prodrugs of therapeutically active compounds, including oligomeric prodrugs, and compositions to treat medical disorders, for example glaucoma, a disorder or abnormality related to an increase in intraocular pressure (IOP), a disorder requiring neuroprotection, age-related macular degeneration, or diabetic retinopathy.

公开(公告)号：US11919865B2

公开(公告)日：2024-03-05

申请号：US17350066

申请日：2021-06-17

申请人： EIDOS THERAPEUTICS, INC.

发明人： Pooran Chand ,  Yogesh Kumar Gupta ,  Rakesh Kumar Kumawat ,  Mamoun Alhamadsheh ,  Robert Zamboni

IPC分类号： C07D231/12 ,  C07C309/04 ,  C07C309/30

CPC分类号： C07D231/12 ,  C07C309/04 ,  C07C309/30 ,  C07B2200/13

摘要： Provided herein are improved processes for the preparation of a compound of Formula IX (AG-10). Also provided herein are pharmaceutically acceptable salts of Formula I and Formula Ib




as well as crystalline types of Formula IX (AG-10). The processes described herein provide improved yields and efficiency, while the pharmaceutically acceptable salts and crystalline forms provide unexpected pharmacokinetic properties. Other features and aspects of the present disclosure will be apparent to a person of skill in the art upon reading the remainder of the specification.

公开(公告)号：US20240025858A1

公开(公告)日：2024-01-25

申请号：US18257373

申请日：2021-12-15

申请人： GW Research Limited

发明人： Alan James SILCOCK ,  Antoine MILLET ,  Karen Ka-Yen TSE ,  Paul Stuart HINCHLIFFE ,  Andrew SHARPE ,  Iain David SIMPSON ,  Joanne PEACH ,  Stefano LEVANTO

IPC分类号： C07D231/12 ,  C07C39/23 ,  C07D249/06 ,  C07D239/34 ,  C07D213/65 ,  C07D213/74 ,  C07D213/16 ,  C07D213/14 ,  C07D405/04 ,  C07D263/32 ,  C07D249/08 ,  C07D261/08 ,  C07D233/64 ,  C07D271/10 ,  C07D213/64 ,  C07D405/06 ,  C07C215/50 ,  C07C213/08 ,  C07C43/23 ,  C07C41/30 ,  C07D271/06 ,  A61P25/08

CPC分类号： C07D231/12 ,  C07C39/23 ,  C07D249/06 ,  C07D239/34 ,  C07D213/65 ,  C07D213/74 ,  C07D213/16 ,  C07D213/14 ,  C07D405/04 ,  C07D263/32 ,  C07D249/08 ,  C07D261/08 ,  C07D233/64 ,  C07D271/10 ,  C07D213/64 ,  C07D405/06 ,  C07C215/50 ,  C07C213/08 ,  C07C43/23 ,  C07C41/30 ,  C07D271/06 ,  A61P25/08

摘要： The present invention relates to a group of novel compounds, methods for their manufacture and the use of these compounds as research tools and as pharmaceuticals. The novel compounds are analogues of cannabidiol (CBD). CBD is a non-psychoactive cannabinoid which has been used to treat various diseases and disorders. While such treatments hold promise, there remains a need in the art for more effective treatments and this has been brought about by way of novel cannabidiol compounds.

公开(公告)号：US11851428B2

公开(公告)日：2023-12-26

申请号：US17328814

申请日：2021-05-24

申请人： ONO PHARMACEUTICAL CO., LTD. ,  VANDERBILT UNIVERSITY

发明人： Craig W. Lindsley ,  Joshua M. Wieting ,  Kevin M. Mcgowan ,  Jerod S. Denton ,  Kentaro Yashiro ,  Haruto Kurata ,  Yoko Sekioka ,  Takahiro Mori ,  Yuzo Iwaki

IPC分类号： C07D213/36 ,  C07D231/12 ,  C07D249/08 ,  C07D401/04 ,  A61K31/454 ,  C07D471/04 ,  C07C255/57 ,  C07C317/28 ,  C07D209/30 ,  C07D213/89 ,  C07D231/56 ,  C07D235/16 ,  C07D237/24 ,  C07D239/47 ,  C07D249/18 ,  C07D257/04 ,  C07D265/36 ,  C07D271/10 ,  C07D285/14 ,  C07D295/04 ,  C07D513/04

CPC分类号： C07D471/04 ,  C07C255/57 ,  C07C317/28 ,  C07D209/30 ,  C07D213/89 ,  C07D231/56 ,  C07D235/16 ,  C07D237/24 ,  C07D239/47 ,  C07D249/08 ,  C07D249/18 ,  C07D257/04 ,  C07D265/36 ,  C07D271/10 ,  C07D285/14 ,  C07D295/04 ,  C07D401/04 ,  C07D513/04

摘要： Disclosed is a compound of formula (I):






wherein all symbols are defined in the description. Also disclosed are pharmaceutical compositions comprising the compounds, methods of making the compounds, kits comprising the compounds, and methods of using the compounds, compositions and kits for treatment of disorders associated with TREK-1, TREK-2 or both TREK-1 and TREK-2 dysfunction in a mammal.

公开(公告)号：US20230390246A1

公开(公告)日：2023-12-07

申请号：US18092709

申请日：2023-01-03

申请人： The Board of Trustees of the Leland Stanford Junior University

发明人： Isabella A. Graef ,  Mamoun M. Alhamadsheh

IPC分类号： A61K31/415 ,  C07D231/12 ,  C07D237/08

CPC分类号： A61K31/415 ,  C07D231/12 ,  C07D237/08

摘要： Disclosed herein are compounds and compositions thereof which find use in increasing stability of proteins particularly proteins that tend to misfold and form aggregates. Also provided herein are methods for using these compounds and compositions for increasing stability of proteins and thereby decreasing aggregate formation by these proteins. Also disclosed herein are heterobifunctional compounds that include a TTR binding compound connected to a targeting moiety via a linker, for use in disrupting PPIs of a target protein.