公开(公告)号：US12077509B2

公开(公告)日：2024-09-03

申请号：US18213055

申请日：2023-06-22

申请人： Arvinas Operations, Inc.

发明人： Hanqing Dong ,  Keith R. Hornberger ,  Lawrence B. Snyder

IPC分类号： A61K31/166 ,  A61K31/02 ,  A61K31/277 ,  A61K31/496 ,  A61K31/497 ,  A61K31/501 ,  A61K31/506 ,  A61K45/06 ,  A61K47/10 ,  C07D205/04 ,  C07D209/48 ,  C07D211/76 ,  C07D213/72 ,  C07D221/20 ,  C07D231/12 ,  C07D233/42 ,  C07D237/08 ,  C07D239/24 ,  C07D241/04 ,  C07D401/04 ,  C07D401/14

CPC分类号： C07D233/42 ,  A61K31/02 ,  A61K31/166 ,  A61K31/277 ,  A61K31/496 ,  A61K31/497 ,  A61K31/501 ,  A61K31/506 ,  A61K45/06 ,  A61K47/10 ,  C07D205/04 ,  C07D209/48 ,  C07D211/76 ,  C07D213/72 ,  C07D221/20 ,  C07D231/12 ,  C07D237/08 ,  C07D239/24 ,  C07D241/04 ,  C07D401/04 ,  C07D401/14

摘要： The present disclosure relates to bifunctional compounds, which find utility to degrade (and inhibit) Androgen Receptor. In particular, the present disclosure is directed to compounds, which contain on one end a cereblon ligand which binds to the E3 ubiquitin ligase and on the other end a moiety which binds Androgen Receptor, such that Androgen Receptor is placed in proximity to the ubiquitin ligase to effect degradation (and inhibition) of Androgen Receptor. The present disclosure exhibits a broad range of pharmacological activities associated with compounds according to the present disclosure, consistent with the degradation/inhibition of Androgen Receptor.

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：US11999802B2

公开(公告)日：2024-06-04

申请号：US16757026

申请日：2018-10-18

申请人： Novartis AG

发明人： James E. Bradner ,  Andrei Golosov ,  Carleton Proctor Goold ,  Carla Patricia Pinto Guimaraes ,  Marc Horst Peter Hild ,  Gregory Motz ,  Nathan Thomas Ross ,  Jonathan M. Solomon ,  Rohan Eric John Beckwith ,  Seth Carbonneau

IPC分类号： C07K19/00 ,  A61K31/4545 ,  A61K31/46 ,  A61K35/12 ,  C07D209/48 ,  C07D213/81 ,  C07D401/14 ,  C07D451/02 ,  C07K14/435 ,  C07K14/705 ,  C07K14/725 ,  C07K16/18 ,  C07K16/28 ,  C12N9/06 ,  C12N15/63 ,  C12N15/86 ,  G01N33/68

CPC分类号： C07K19/00 ,  A61K31/4545 ,  A61K31/46 ,  A61K35/12 ,  C07D209/48 ,  C07D213/81 ,  C07D401/14 ,  C07D451/02 ,  C07K14/435 ,  C07K14/705 ,  C07K14/7051 ,  C07K14/70521 ,  C07K14/70575 ,  C07K16/18 ,  C07K16/2803 ,  C07K16/2815 ,  C07K16/2863 ,  C07K16/2875 ,  C07K16/2887 ,  C07K16/2896 ,  C12N9/003 ,  C12N15/63 ,  C12N15/86 ,  C12Y105/01003 ,  G01N33/6803 ,  C07K2317/622 ,  C07K2319/02 ,  C07K2319/03 ,  C07K2319/20 ,  C07K2319/35 ,  C07K2319/81 ,  C07K2319/95 ,  C12N2740/15043

摘要： The invention provides compositions including a fusion polypeptide and methods for making a fusion polypeptide that includes a COF1/CRBN-binding polypeptide, COF2/CRBN-binding polypeptide, or COF3/CRBN-binding polypeptide and a heterologous polypeptide of interest.

公开(公告)号：US11964945B2

公开(公告)日：2024-04-23

申请号：US16888484

申请日：2020-05-29

申请人： Arvinas Operations, Inc.

发明人： Andrew P. Crew ,  Keith R. Hornberger ,  Lawrence B. Snyder ,  Kurt Zimmermann ,  Jing Wang ,  Hanqing Dong

IPC分类号： C07D401/14 ,  A61K31/02 ,  A61K31/166 ,  A61K31/277 ,  A61K31/496 ,  A61K31/497 ,  A61K31/501 ,  A61K31/506 ,  A61K45/06 ,  A61K47/10 ,  C07D205/04 ,  C07D209/48 ,  C07D211/76 ,  C07D213/72 ,  C07D221/20 ,  C07D231/12 ,  C07D233/42 ,  C07D237/08 ,  C07D239/24 ,  C07D241/04 ,  C07D401/04

CPC分类号： C07D233/42 ,  A61K31/02 ,  A61K31/166 ,  A61K31/277 ,  A61K31/496 ,  A61K31/497 ,  A61K31/501 ,  A61K31/506 ,  A61K45/06 ,  A61K47/10 ,  C07D205/04 ,  C07D209/48 ,  C07D211/76 ,  C07D213/72 ,  C07D221/20 ,  C07D231/12 ,  C07D237/08 ,  C07D239/24 ,  C07D241/04 ,  C07D401/04 ,  C07D401/14

摘要： The present disclosure relates to bifunctional compounds, which find utility to degrade and (inhibit) Androgen Receptor. In particular, the present disclosure is directed to compounds, which contain on one end a cereblon ligand which binds to the E3 ubiquitin ligase and on the other end a moiety which binds Androgen Receptor, such that Androgen Receptor is placed in proximity to the ubiquitin ligase to effect degradation (and inhibition) of Androgen Receptor. The present disclosure exhibits a broad range of pharmacological activities associated with compounds according to the present disclosure, consistent with the degradation/inhibition of Androgen Receptor.

公开(公告)号：US11919857B2

公开(公告)日：2024-03-05

申请号：US17257736

申请日：2019-01-17

申请人： LANZHOU INSTITUTE OF CHEMICAL PHYSICS, CHINESE ACADEMY OF SCIENCES

发明人： Junxi Liu ,  Yaming Zhang

IPC分类号： C07D209/48 ,  A61P9/00 ,  A61P39/06

CPC分类号： C07D209/48 ,  A61P9/00 ,  A61P39/06 ,  C07B2200/07

摘要： The present invention discloses a phthalide derivative, the structure of said derivative is represented by Formula (I) or Formula (II). The present invention also discloses the preparation method and use of said derivative. The phthalide compound obtained through structure modifications in the present invention enhances the chemical stability and pharmacological activity of the phthalide compound, facilitating the improvement of the druggability of such compounds.

公开(公告)号：US20240025845A1

公开(公告)日：2024-01-25

申请号：US18025134

申请日：2021-09-07

申请人： KOREA RESEARCH INSTITUTE OF BIOSCIENCE AND BIOTECHNOLOGY

发明人： Jong Seog AHN ,  Sung Kyun KO ,  Jae Hyuk JANG ,  Jun Pil JANG ,  Jae Kyung JUNG ,  Nam Doo KIM ,  Bo Yeon KIM ,  Joon Suk PARK

IPC分类号： C07C311/08 ,  C07C237/52 ,  C07D209/48 ,  C07D333/34 ,  C07D213/64 ,  A61P35/00 ,  C07C311/44 ,  C07C311/29 ,  C07C311/21 ,  C07D333/18 ,  C07D231/16 ,  C07D215/36 ,  C07D403/04 ,  C07C311/14 ,  C07D271/12 ,  C07D319/18 ,  C07C311/13

CPC分类号： C07C311/08 ,  C07C237/52 ,  C07D209/48 ,  C07D333/34 ,  C07D213/64 ,  A61P35/00 ,  C07C311/44 ,  C07C311/29 ,  C07C311/21 ,  C07D333/18 ,  C07D231/16 ,  C07D215/36 ,  C07D403/04 ,  C07C311/14 ,  C07D271/12 ,  C07D319/18 ,  C07C311/13 ,  C07C2601/02

摘要： Provided is a metastasis-inhibiting composition containing a methylsulfonamide-based derivative compound as an active ingredient. More specifically, the compounds inhibit the activity of chromosome segregation 1-like (CSE1L), and suppress intracellular nuclear transport to inhibit the movement and/or invasion of cancer cells, and thus effectively inhibit metastasis.

公开(公告)号：US20240018101A1

公开(公告)日：2024-01-18

申请号：US18032499

申请日：2021-10-20

申请人： University of San Diego

发明人： Peter M. Iovine ,  Gopi Nath Vemuri ,  Jake Hughes

IPC分类号： C07C323/61 ,  C07D209/48 ,  C07C323/47 ,  A61K47/22 ,  A61K47/20

CPC分类号： C07C323/61 ,  C07D209/48 ,  C07C2601/14 ,  A61K47/22 ,  A61K47/20 ,  C07C323/47

摘要： Multifunctional amine-containing bolaamphiphilic compositions comprising hydrocarbon terpenes, methods of preparing such compositions, and the use of these compositions in gene delivery applications are disclosed.

公开(公告)号：US20230278955A1

公开(公告)日：2023-09-07

申请号：US18117358

申请日：2023-03-03

申请人： KYOTO UNIVERSITY ,  NATIONAL UNIVERSITY CORPORATION TOKYO UNIVERSITY OF AGRICULTURE AND TECHNOLOGY

发明人： Mizuki WATANABE ,  Risa ASANO ,  Kazuo NAGASAWA ,  Motonari UESUGI

IPC分类号： C07C401/00 ,  C07D495/04 ,  C07D209/48 ,  C07D211/46 ,  A61K31/593 ,  C07D295/125 ,  A61K31/59 ,  A61P1/16 ,  A61P9/00 ,  A61P3/04 ,  A61P3/10 ,  A61P35/00

CPC分类号： C07C401/00 ,  C07D495/04 ,  C07D209/48 ,  C07D211/46 ,  A61K31/593 ,  C07D295/125 ,  A61K31/59 ,  A61P1/16 ,  A61P9/00 ,  A61P3/04 ,  A61P3/10 ,  A61P35/00 ,  C07C2601/14 ,  C07C2602/24

摘要： The present invention relates to vitamin D3 derivatives of the following formula, wherein each symbol has the same meaning as defined herein, and pharmaceutical or medical use thereof for treating metabolic disease, liver disease, obesity, diabetes, cardiovascular disease, or cancer in a patient in need thereof.

公开(公告)号：US20230167058A1

公开(公告)日：2023-06-01

申请号：US17931341

申请日：2022-09-12

申请人： THE TRUSTEES OF COLUMBIA UNIVERSITY IN THE CITY OF NEW YORK

发明人： Brent R. STOCKWELL ,  Hengrui LIU ,  Farhad FOROUHAR ,  Qian WANG

IPC分类号： C07D209/48 ,  A61P35/00 ,  C07D295/16 ,  C07D487/04 ,  C07F7/22 ,  C07D409/04 ,  C07D277/42 ,  C07D403/06 ,  C07D455/02

CPC分类号： C07D209/48 ,  A61P35/00 ,  C07D295/16 ,  C07D487/04 ,  C07F7/2224 ,  C07D409/04 ,  C07D277/42 ,  C07D403/06 ,  C07D455/02

摘要： The present disclosure provides, inter alia, compounds to modulate GPX4 activity. Also provided are pharmaceutical compositions containing same compounds. Further provided are methods for treating or ameliorating the effects of a cancer in a subject, methods of modulating GPX activity in a subject, methods of inducing ferroptosis in a cell, and methods for treating or ameliorating the effects of a cancer in a subject using the compounds or composition in combination with other therapeutic agents.

公开(公告)号：US20230159446A1

公开(公告)日：2023-05-25

申请号：US18088447

申请日：2022-12-23

申请人： NANJING IMMUNOPHAGE BIOTECH CO., LTD.

发明人： Guohuang FAN ,  Hongyu YANG ,  Kin Chiu FONG ,  Jianfei WANG

IPC分类号： C07C311/46 ,  C07D211/12 ,  C07D211/14 ,  C07D215/36 ,  C07D241/44 ,  C07D239/93 ,  C07D209/48 ,  C07D239/42 ,  C07D235/08 ,  C07D401/12 ,  C07D231/56

CPC分类号： C07C311/46 ,  C07D211/12 ,  C07D211/14 ,  C07D215/36 ,  C07D241/44 ,  C07D239/93 ,  C07D209/48 ,  C07D239/42 ,  C07D235/08 ,  C07D401/12 ,  C07D231/56

摘要： The present invention provides compounds of Formula (I) which can be used as CCR8 inhibitors, which can be used as treatment or prevention of cancer using CCR8 inhibitors targeted tumor specific T regulatory cells.