公开(公告)号：US12122751B2

公开(公告)日：2024-10-22

申请号：US18356977

申请日：2023-07-21

申请人： Translatum Medicus Inc.

发明人： Xiangdong Jiao ,  Kanjai Khumtaveeporn

IPC分类号： C07D231/56

CPC分类号： C07D231/56

摘要： The invention in this disclosure is related to the processes of making Bindarit or derivatives thereof. Specifically, the present invention provides, in part, new processes for making 2-((1-benzyl-1H-indazol-3-yl)methoxy)-2-methylpropanoic acid and its derivatives. By way of non-limiting example, synthesis and purification processes of 2-((1-benzyl-1H-indazol-3-yl)methoxy)-2-methylpropanoic acid are provided by the invention in this disclosure.

公开(公告)号：US12103915B2

公开(公告)日：2024-10-01

申请号：US18529689

申请日：2023-12-05

申请人： Insilico Medicine IP Limited

发明人： Xiao Ding ,  Jinxin Liu ,  Feng Ren ,  Jianfei Wan ,  Wei Zhu

IPC分类号： C07D231/56 ,  A61P35/00 ,  C07D209/44 ,  C07D215/14 ,  C07D401/04 ,  C07D403/08 ,  C07D471/04 ,  C07D487/04

CPC分类号： C07D231/56 ,  A61P35/00 ,  C07D209/44 ,  C07D215/14 ,  C07D401/04 ,  C07D403/08 ,  C07D471/04 ,  C07D487/04

摘要： The disclosure provides for compounds and methods for modulating or inhibiting TEAD. Further provided herein are pharmaceutical compositions comprising the TEAD inhibitors and methods of treatment using the TEAD inhibitors or the pharmaceutical compositions.

公开(公告)号：US12103907B2

公开(公告)日：2024-10-01

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：US20240287058A1

公开(公告)日：2024-08-29

申请号：US17921580

申请日：2021-04-29

申请人： Relay Therapeutics, Inc. ,  D. E. Shaw Research, LLC

发明人： Alessandro BOEZIO ,  Lucian V. DIPIETRO ,  Cary Griffin FRIDRICH ,  Hakan GUNAYDIN ,  Ravi KURUKULASURIYA ,  André LESCARBEAU ,  Mary M. MADER ,  Thomas H. MCLEAN ,  Levi CharlesThomas PIERCE ,  Kevin David RAYNOR ,  Kelley C. SHORTSLEEVES ,  Yong TANG ,  Alexander M. TAYLOR ,  W. Patrick WALTERS ,  Hanmo ZHANG ,  Fabrizio GIORDANETTO ,  Yakov PECHERSKY ,  Qi WANG ,  Bren-Jordan ATIENZA ,  Megan BERTRAND-LAPERLE ,  Andrew J. BURNIE ,  Fei CHEN ,  Sampada CHITALE ,  Shorena GELOZIA ,  Jean-Benoit GIGUERE ,  Elodie LANDAGARAY ,  Alexandre LARIVEE ,  Thomas LEPITRE ,  Gaetan MAERTENS ,  Johanne OUTIN ,  Mohan PAL ,  Claudio STURINO ,  Kashif TANVEER ,  Rakesh THORAT ,  Naresh VEMULA ,  Elaine B. KRUEGER ,  Yue PAN ,  Michael Paul DENINNO ,  Yves BOUSQUET ,  Antoine JOBIN-DES LAURIERS ,  Jessica LEE ,  Tarek MOHAMED

IPC分类号： C07D471/04 ,  A61K31/4035 ,  A61K31/404 ,  A61K31/4155 ,  A61K31/416 ,  A61K31/428 ,  A61K31/437 ,  A61K31/4375 ,  A61K31/4545 ,  A61K31/472 ,  A61K31/506 ,  A61K31/517 ,  A61K31/519 ,  A61K31/536 ,  A61K31/69 ,  C07D209/46 ,  C07D209/48 ,  C07D217/24 ,  C07D231/56 ,  C07D239/82 ,  C07D265/18 ,  C07D275/06 ,  C07D401/04 ,  C07D403/04 ,  C07D403/12 ,  C07D405/06 ,  C07D409/12 ,  C07D409/14 ,  C07D417/12 ,  C07D487/04 ,  C07D519/00 ,  C07F5/02

CPC分类号： C07D471/04 ,  A61K31/4035 ,  A61K31/404 ,  A61K31/4155 ,  A61K31/416 ,  A61K31/428 ,  A61K31/437 ,  A61K31/4375 ,  A61K31/4545 ,  A61K31/472 ,  A61K31/506 ,  A61K31/517 ,  A61K31/519 ,  A61K31/536 ,  A61K31/69 ,  C07D209/46 ,  C07D209/48 ,  C07D217/24 ,  C07D231/56 ,  C07D239/82 ,  C07D265/18 ,  C07D275/06 ,  C07D401/04 ,  C07D403/04 ,  C07D403/12 ,  C07D405/06 ,  C07D409/12 ,  C07D409/14 ,  C07D417/12 ,  C07D487/04 ,  C07D519/00 ,  C07F5/025

摘要： The present disclosure relates to novel compounds and pharmaceutical compositions thereof, and methods for inhibiting the activity of PI3K-α enzymes with the compounds and compositions of the disclosure. The present disclosure further relates to, but is not limited to, methods for treating disorders associated with PI3K-α signaling with the compounds and compositions of the disclosure.

公开(公告)号：US12060330B2

公开(公告)日：2024-08-13

申请号：US17517569

申请日：2021-11-02

申请人： RUTGERS, THE STATE UNIVERSITY OF NEW JERSEY

发明人： Joel S. Freundlich ,  David Alland ,  Matthew B. Neiditch ,  Pradeep Kumar ,  Glenn Capodagli ,  Divya Awasthi ,  Sean Ekins

IPC分类号： C07D231/56 ,  A61K31/4409 ,  A61P31/06

CPC分类号： C07D231/56 ,  A61K31/4409 ,  A61P31/06

摘要： The invention provides compounds of formula I:




and salts thereof wherein R1-R5 have any of the meanings described in the specification. The compounds are useful for treating bacterial infections (e.g. tuberculosis).

公开(公告)号：US20240262808A1

公开(公告)日：2024-08-08

申请号：US18557919

申请日：2022-04-28

申请人： JIANGSU ATOM BIOSCIENCE AND PHARMACEUTICAL CO., LTD.

发明人： Dongfang SHI ,  Changjin FU ,  Yan YANG

IPC分类号： C07D403/04 ,  A61K31/416 ,  A61K31/4192 ,  A61K31/4439 ,  A61P19/06 ,  C07D231/56 ,  C07D401/04 ,  C07D405/14 ,  C07D409/04

CPC分类号： C07D403/04 ,  A61K31/416 ,  A61K31/4192 ,  A61K31/4439 ,  A61P19/06 ,  C07D231/56 ,  C07D401/04 ,  C07D405/14 ,  C07D409/04

摘要： It discloses a compound shown in general formula (1) or a pharmaceutically acceptable salt thereof and a method for preparation of the compound; the compound is a xanthine oxidase inhibitor with xanthine oxidase inhibiting activity; the compound has an excellent xanthine oxidase inhibitory activity and has potential application value in anti-gout drugs, anti-hyperuricemia drugs, etc.

公开(公告)号：US11999677B2

公开(公告)日：2024-06-04

申请号：US17666692

申请日：2022-02-08

申请人： The Board of Regents of the University of Oklahoma

发明人： Weidong Wang ,  Venkateswararao Eeda

IPC分类号： C07C233/73 ,  A61K31/166 ,  A61P3/10 ,  C07C237/22 ,  C07C311/46 ,  C07D213/40 ,  C07D231/56 ,  C07D317/54

CPC分类号： C07C233/73 ,  C07D317/54

摘要： Benzylamino-oxoethyl benzamide compounds for use in treating diseases and conditions associated with abnormal cell function related to endoplasmic reticulum (ER) stress. For example, the compounds can be used as suppressors of ER stress-induced pancreatic β-cell dysfunction and death, for example in the treatment of Type 1 and Type 2 diabetes. The compounds can also be used in treatments for chronic heart disease, neurodegenerative diseases, retinal degeneration, and other metabolic disorders associated with ER stress.

公开(公告)号：US20240158355A1

公开(公告)日：2024-05-16

申请号：US18262037

申请日：2022-01-19

申请人： Baylor College of Medicine

发明人： Martin Matzuk ,  Zhifeng Yu ,  Angela Ku ,  Justin Anglin ,  Feng Li ,  Damian Young ,  Ying-Chu Chen ,  Melek Ucisik ,  John Faver ,  Stephen Palmer ,  Rajesh Sharma ,  Choel Kim

IPC分类号： C07D231/56 ,  C07D401/04 ,  C07D403/04

CPC分类号： C07D231/56 ,  C07D401/04 ,  C07D403/04

摘要： In one aspect, the present disclosure provides compounds which inhibit bromodomain testis (BRDT). In some embodiments, the compounds inhibit bromodomain-2 of BRDT. In another aspect, the present disclosure provides a method of inhibiting BRDT in a male subject, the method comprising administering to the male subject a therapeutically effective amount of a compound of the disclosure. In some embodiments, the method provides a contraceptive effect in the male subject.

公开(公告)号：US11926632B2

公开(公告)日：2024-03-12

申请号：US17353199

申请日：2021-06-21

申请人： PMV Pharmaceuticals, Inc.

发明人： Binh Vu ,  Romyr Dominique ,  Hongju Li ,  Bruce Fahr ,  Yi Chen

IPC分类号： C07D487/10 ,  C07C237/40 ,  C07D213/36 ,  C07D213/38 ,  C07D213/73 ,  C07D213/81 ,  C07D215/12 ,  C07D231/56 ,  C07D239/42 ,  C07D401/04 ,  C07D401/12 ,  C07D405/12 ,  C07D413/12 ,  C07D417/12 ,  C07D487/08 ,  C07D491/107

CPC分类号： C07D487/10 ,  C07C237/40 ,  C07D213/36 ,  C07D213/38 ,  C07D213/73 ,  C07D213/81 ,  C07D215/12 ,  C07D231/56 ,  C07D239/42 ,  C07D401/04 ,  C07D401/12 ,  C07D405/12 ,  C07D413/12 ,  C07D417/12 ,  C07D487/08 ,  C07D491/107

摘要： Mutations in oncogenes and tumor suppressors contribute to the development and progression of cancer. The present disclosure describes compounds and methods that restore DNA binding affinity of p53 mutants. The compounds of the present disclosure can bind to mutant p53 and restore the ability of the p53 mutant to bind DNA and activate downstream effectors involved in tumor suppression. The disclosed compounds can be used to reduce the progression of cancers that contain a p53 mutation.

公开(公告)号：US20240081145A1

公开(公告)日：2024-03-07

申请号：US18482667

申请日：2023-10-06

申请人： Samsung Display Co., LTD.

发明人： Seulong Kim ,  Heungsu Park

IPC分类号： H10K85/60 ,  C07D231/56 ,  C07D239/26 ,  C07D251/24 ,  C07D403/10

CPC分类号： H10K85/654 ,  C07D231/56 ,  C07D239/26 ,  C07D251/24 ,  C07D403/10 ,  H10K85/6572 ,  H10K50/11

摘要： Disclosed are an organic light-emitting device including a first compound represented by Formula 1 below and a second compound represented by Formula 2 below, and an electronic apparatus including the organic light-emitting device. The variables in Formula 1 and Formula 2 are the same as described in the present specification.