公开(公告)号：US12215093B2

公开(公告)日：2025-02-04

申请号：US18467022

申请日：2023-09-14

Applicant: Tempest Therapeutics, Inc.

Inventor： Yalda Bravo ,  Austin Chih-Yu Chen ,  Jinyue Ding ,  Robert Gomez ,  Heather Lam ,  Joe Fred Nagamizo ,  Renata Marcella Oballa ,  David Andrew Powell ,  Tao Sheng

IPC: C07D231/56 ,  C07D209/42 ,  C07D401/10 ,  C07D403/10 ,  C07D405/12 ,  C07D417/10 ,  C07D471/04

Abstract: Compounds, compositions and methods are provided for modulating the activity of EP2 and EP4 receptors, and for the treatment, prevention and amelioration of one or more symptoms of diseases or disorders related to the activity of EP2 and EP4 receptors. In certain embodiments, the compounds are antagonists of both the EP2 and EP4 receptors.

公开(公告)号：US12187722B2

公开(公告)日：2025-01-07

申请号：US17439735

申请日：2020-03-13

Applicant: The General Hospital Corporation

Inventor： Xu Wu ,  Pranab Maiti ,  Chandrasekhar Abbineni ,  Krishna Chaitanya Talluri ,  Sunil Kumar Panigrahi ,  Gopala Krishna Jarugumilli ,  Yang Sun

IPC: A61P35/00 ,  A61K31/165 ,  A61K31/18 ,  A61K31/195 ,  A61K31/196 ,  A61K31/24 ,  A61K31/397 ,  A61K31/401 ,  A61K31/405 ,  A61K31/41 ,  A61K31/416 ,  A61K31/4184 ,  A61K31/4196 ,  A61K31/428 ,  A61K31/44 ,  A61K31/4439 ,  A61K31/4704 ,  A61K31/496 ,  A61K31/4965 ,  C07C211/26 ,  C07C211/55 ,  C07C211/56 ,  C07C211/60 ,  C07C225/22 ,  C07C229/44 ,  C07C229/48 ,  C07C229/58 ,  C07C237/40 ,  C07C255/58 ,  C07C311/44 ,  C07C317/28 ,  C07C323/63 ,  C07D205/04 ,  C07D207/16 ,  C07D207/34 ,  C07D209/08 ,  C07D211/62 ,  C07D213/74 ,  C07D213/79 ,  C07D213/80 ,  C07D215/227 ,  C07D231/14 ,  C07D231/56 ,  C07D233/61 ,  C07D233/64 ,  C07D235/06 ,  C07D235/08 ,  C07D235/18 ,  C07D239/42 ,  C07D239/48 ,  C07D239/88 ,  C07D241/20 ,  C07D241/28 ,  C07D249/08 ,  C07D249/10 ,  C07D257/04 ,  C07D275/06 ,  C07D277/28 ,  C07D295/135 ,  C07D295/155 ,  C07D317/32 ,  C07D401/06 ,  C07D401/12 ,  C07D471/04

Abstract: The present disclosure compounds, as well as their compositions and methods of use. The compounds inhibit the activity of the TEAD transcription factor, and are useful in the treatment of diseases related to the activity of TEAD transcription factor including, e.g., cancer and other diseases.

公开(公告)号：US20240409504A1

公开(公告)日：2024-12-12

申请号：US18812888

申请日：2024-08-22

Applicant: Duke University

Inventor： Dennis J. Thiele ,  Bushu Dong ,  Alexander M. Jaeger ,  Philip F. Hughes ,  Timothy Haystead ,  Jiyong Hong

IPC: C07C275/30 ,  A61P35/00 ,  C07C211/40 ,  C07C255/60 ,  C07C275/28 ,  C07C275/34 ,  C07C275/40 ,  C07C275/42 ,  C07C279/18 ,  C07C279/28 ,  C07C281/06 ,  C07C311/46 ,  C07C317/36 ,  C07C317/42 ,  C07D213/40 ,  C07D213/75 ,  C07D223/04 ,  C07D229/02 ,  C07D231/56 ,  C07D233/64 ,  C07D241/24 ,  C07D249/14 ,  C07D271/12 ,  C07D285/10 ,  C07D317/66 ,  C07D333/20 ,  C07D333/36 ,  C07D333/72 ,  C07D405/04 ,  C07D405/12 ,  C07D417/12

Abstract: This disclosure relates to compounds, pharmaceutical compositions comprising them, and methods of using the compounds and compositions for treating diseases related to Heat Shock Transcription Factor 1 (HSF1) activity and/or function. More particularly, this disclosure relates to methods of inhibiting HSF1 activity with these compounds and pharmaceutical compositions thereof, and methods of treating diseases associated with HSF1 activity and/or function, such as cancer.

公开(公告)号：US12122751B2

公开(公告)日：2024-10-22

申请号：US18356977

申请日：2023-07-21

Applicant: Translatum Medicus Inc.

Inventor： Xiangdong Jiao ,  Kanjai Khumtaveeporn

IPC: C07D231/56

CPC classification number: C07D231/56

Abstract: 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

Applicant: Insilico Medicine IP Limited

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

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

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

Abstract: 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

Applicant: ARCUS BIOSCIENCES, INC.

Inventor： 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: 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 classification number: 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

Abstract: 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

Applicant: Relay Therapeutics, Inc. ,  D. E. Shaw Research, LLC

Inventor： 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: 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 classification number: 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

Abstract: 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

Applicant: RUTGERS, THE STATE UNIVERSITY OF NEW JERSEY

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

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

CPC classification number: C07D231/56 ,  A61K31/4409 ,  A61P31/06

Abstract: 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

Applicant: JIANGSU ATOM BIOSCIENCE AND PHARMACEUTICAL CO., LTD.

Inventor： Dongfang SHI ,  Changjin FU ,  Yan YANG

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

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

Abstract: 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

Applicant: The Board of Regents of the University of Oklahoma

Inventor： Weidong Wang ,  Venkateswararao Eeda

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

CPC classification number: C07C233/73 ,  C07D317/54

Abstract: 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.