公开(公告)号：US11926619B2

公开(公告)日：2024-03-12

申请号：US17045952

申请日：2019-04-08

Applicant: EISAI R&D MANAGEMENT CO., LTD.

Inventor： Gregg F. Keaney ,  John Wang ,  Baudouin Gerard ,  Kenzo Arai ,  Xiang Liu ,  Guo Zhu Zheng ,  Kazunobu Kira ,  Lisa A. Marcaurelle ,  Marta Nevalainen ,  Ming-Hong Hao ,  Morgan Welzel O'Shea ,  Parcharee Tivitmahaisoon ,  Sudeep Prajapati ,  Tuoping Luo ,  Nicholas C. Gearhart ,  Jason T. Lowe ,  Yoshihiko Kotake ,  Satoshi Nagao ,  Regina Mikie Kanada Sonobe ,  Masayuki Miyano ,  Norio Murai ,  Andrew Cook ,  Shelby Ellery ,  Atsushi Endo ,  James Palacino ,  Dominic Reynolds

IPC: C07D407/12 ,  A61K31/365 ,  A61K31/4427 ,  A61K31/497 ,  A61K45/06 ,  A61P35/00 ,  C07D313/00 ,  C07D405/12 ,  C07D405/14 ,  C07D407/06 ,  C07D407/14 ,  C07D413/12 ,  C07D417/12 ,  C07D487/08 ,  C07D487/10 ,  C07D491/107

CPC classification number: C07D407/06 ,  A61K45/06 ,  A61P35/00 ,  C07D313/00 ,  C07D405/12 ,  C07D405/14 ,  C07D413/12 ,  C07D417/12 ,  C07D487/08 ,  C07D487/10 ,  C07D491/107

Abstract: The present disclosure provides novel pladienolide compounds, pharmaceutical compositions containing such compounds, and methods for using the compounds as therapeutic agents. These compounds may be useful in the treatment of cancers, particularly cancers in which agents that target the spliceosome and mutations therein are known to be useful. Also provided herein are methods of treating cancers by administering at least one compound disclosed herein and at least one additional therapy.

公开(公告)号：US20240067952A1

公开(公告)日：2024-02-29

申请号：US18243169

申请日：2023-09-07

Applicant: YALE UNIVERSITY

Inventor： David A. Spiegel ,  Charles E. Jakobsche

IPC: C12N9/96 ,  A61K45/06 ,  C07D493/10 ,  A61K31/165 ,  A61K31/365 ,  C07C279/12 ,  A61K47/60 ,  A61K47/54 ,  A61K31/352 ,  A61K38/05 ,  A61K38/48 ,  C07D491/107 ,  C07K5/062

CPC classification number: C12N9/96 ,  A61K45/06 ,  C07D493/10 ,  A61K31/165 ,  A61K31/365 ,  C07C279/12 ,  A61K47/60 ,  A61K47/54 ,  A61K31/352 ,  A61K38/05 ,  A61K38/482 ,  C07D491/107 ,  C07K5/06026

Abstract: The present invention relates to chimeric (preferably, bifunctional) compounds, compositions comprising those compounds and methods of treating cancer in a patient or subject, especially including metastatic cancer where cancer cells exhibit overexpression (heightened expression) of cell surface urokinase-type plasminogen activator receptor (urokinase receptor) compared to normal (non-cancerous) cells. The compounds preferably covalently bind to the urokinase receptor and recruit native antibodies of the patient or subject where the antibodies can selectively degrade and/or deactivate targeted cancer cells through antibody-dependent cellular phagocytosis and/or antibody-dependent cellular cytotoxicity (ADCC) against a large number and variety of cancers, thus providing cancer cell death and/or an inhibition of growth, elaboration and/or metastasis of the cancer, including remission and cure of the patient's cancer.

公开(公告)号：US11912659B2

公开(公告)日：2024-02-27

申请号：US17232511

申请日：2021-04-16

Applicant: The Wistar Institute of Anatomy and Biology

Inventor： Troy E. Messick ,  Garry R. Smith ,  Allen B. Reitz ,  Paul M. Lieberman ,  Mark E. McDonnell ,  Yan Zhang ,  Marianne Carlsen ,  Shuai Chen

IPC: C07D209/08 ,  C07D403/12 ,  C07D405/14 ,  C07D401/12 ,  C07D405/12 ,  C07D409/12 ,  C07D487/08 ,  C07D471/08 ,  C07D417/12 ,  A61P35/00 ,  A61P31/20 ,  A61K31/404 ,  A61K31/41 ,  A61K31/4155 ,  A61K31/422 ,  A61K31/426 ,  A61K31/427 ,  A61K31/433 ,  A61K31/435 ,  A61K31/437 ,  A61K31/4375 ,  A61K31/4439 ,  A61K31/454 ,  A61K31/4725 ,  A61K31/496 ,  A61K31/501 ,  A61K31/506 ,  A61K31/517 ,  A61K31/519 ,  A61K31/5377 ,  A61K31/541 ,  A61K31/551 ,  A61K45/06 ,  C07D277/62 ,  C07D401/10 ,  C07D401/14 ,  C07D403/10 ,  C07D403/14 ,  C07D413/10 ,  C07D417/10 ,  C07D471/04 ,  C07D471/10 ,  C07D487/04 ,  C07D491/107

CPC classification number: C07D209/08 ,  A61K31/404 ,  A61K31/41 ,  A61K31/4155 ,  A61K31/422 ,  A61K31/426 ,  A61K31/427 ,  A61K31/433 ,  A61K31/435 ,  A61K31/437 ,  A61K31/4375 ,  A61K31/4439 ,  A61K31/454 ,  A61K31/4725 ,  A61K31/496 ,  A61K31/501 ,  A61K31/506 ,  A61K31/517 ,  A61K31/519 ,  A61K31/5377 ,  A61K31/541 ,  A61K31/551 ,  A61K45/06 ,  A61P31/20 ,  A61P35/00 ,  C07D277/62 ,  C07D401/10 ,  C07D401/12 ,  C07D401/14 ,  C07D403/10 ,  C07D403/12 ,  C07D403/14 ,  C07D405/12 ,  C07D405/14 ,  C07D409/12 ,  C07D413/10 ,  C07D417/10 ,  C07D417/12 ,  C07D471/04 ,  C07D471/08 ,  C07D471/10 ,  C07D487/04 ,  C07D487/08 ,  C07D491/107

Abstract: The present invention provides EBNA1 inhibitors, and/or pharmaceutical compositions comprising the same, that are useful for the treatment of diseases caused by EBNA1 activity, such as, but not limited to, cancer, infectious mononucleosis, chronic fatigue syndrome, multiple sclerosis, systemic lupus erythematosus and/or rheumatoid arthritis. The present invention further provides EBNA1 inhibitors, and/or pharmaceutical compositions comprising the same, that are useful for the treatment of diseases caused by latent Epstein-Barr Virus (EBV) infection and/or lytic EBV infection.

公开(公告)号：US20240051940A1

公开(公告)日：2024-02-15

申请号：US18264308

申请日：2022-02-07

Applicant: ACCUTAR BIOTECHNOLOGY INC.

Inventor： Yimin QIAN ,  Robert LUO ,  Wei HE ,  Jie Fan

IPC: C07D401/14 ,  C07D401/12 ,  C07D471/10 ,  C07D471/04 ,  C07D403/14 ,  C07D491/107 ,  C07D471/08 ,  C07D487/08 ,  C07D487/04 ,  C07D413/14 ,  C07D498/10 ,  A61K45/06

CPC classification number: C07D401/14 ,  C07D401/12 ,  C07D471/10 ,  C07D471/04 ,  C07D403/14 ,  C07D491/107 ,  C07D471/08 ,  C07D487/08 ,  C07D487/04 ,  C07D413/14 ,  C07D498/10 ,  A61K45/06 ,  C07B2200/05

Abstract: The disclosure provides sulfonamides based compounds and pharmaceutical compositions thereof, which are useful for inhibiting one or more mutations of EGFR, as well as methods for using such compounds to treat cancer associated with EGFR mutations.

公开(公告)号：US11891365B2

公开(公告)日：2024-02-06

申请号：US17238321

申请日：2021-04-23

Applicant: Valo Health, Inc.

Inventor： Xiaozhang Zheng ,  Pui Yee Ng ,  Bingsong Han ,  Jennifer R. Thomason ,  Mary-Margaret Zablocki ,  Cuixian Liu ,  Heather Davis ,  Aleksandra Rudnitskaya ,  David R. Lancia, Jr. ,  Kenneth W. Bair ,  David S. Millan ,  Matthew W. Martin

IPC: A61K31/5513 ,  C07D267/14 ,  C07D291/08 ,  C07D413/06 ,  C07D419/06 ,  C07D413/12 ,  C07D413/04 ,  C07D267/12 ,  C07D243/14 ,  C07D401/06 ,  C07D401/10 ,  C07D403/06 ,  C07D403/10 ,  C07D405/06 ,  C07D413/14 ,  C07D417/04 ,  C07D471/04 ,  C07D498/04 ,  C07D498/08 ,  C07D493/08 ,  C07D413/08 ,  C07D491/107 ,  C07D495/10

CPC classification number: C07D267/14 ,  C07D243/14 ,  C07D267/12 ,  C07D291/08 ,  C07D401/06 ,  C07D401/10 ,  C07D403/06 ,  C07D403/10 ,  C07D405/06 ,  C07D413/04 ,  C07D413/06 ,  C07D413/08 ,  C07D413/12 ,  C07D413/14 ,  C07D417/04 ,  C07D471/04 ,  C07D491/107 ,  C07D493/08 ,  C07D495/10 ,  C07D498/04 ,  C07D498/08

Abstract: The present disclosure relates to inhibitors of zinc-dependent histone deacetylases (HDACs) useful in the treatment of diseases or disorders associated with an HDAC, e.g., HDAC6, having a Formula I:




where R, L, X1, X2, X3, X4, Y1, Y2, Y3, and Y4 are described herein.

公开(公告)号：US11890281B2

公开(公告)日：2024-02-06

申请号：US17029376

申请日：2020-09-23

Applicant: Relay Therapeutics, Inc.

Inventor： Alexander M. Taylor ,  André Lescarbeau ,  Jing Wang ,  Yanyan Zhang ,  Gaodeng Lian

IPC: A61K31/4985 ,  A61K45/06 ,  C07D519/00 ,  C07D401/14 ,  C07D221/20 ,  C07D491/107

CPC classification number: A61K31/4985 ,  A61K45/06 ,  C07D401/14 ,  C07D519/00 ,  C07B2200/13 ,  C07D221/20 ,  C07D491/107

Abstract: The disclosure is in part directed to crystalline forms of (R)-1′-(3-(3,4-dihydro-1,5-naphthyridin-1(2H)-yl)-1H-pyrazolo[3,4-b]pyrazin-6-yl)-3H-spiro[benzofuran-2,4′-piperidin]-3-amine, its salt, and variants thereof.

公开(公告)号：US20240025893A1

公开(公告)日：2024-01-25

申请号：US18029289

申请日：2020-09-30

Applicant: Asahi Kasei Pharma Corporation ,  Vernalis (R&D) Limited

Inventor： Koichiro ARAI ,  Kenichiro TAKABA ,  Masakazu ATOBE ,  Misato TAKASHIMA ,  Naomi AONO ,  Andrew John POTTER ,  Daniel Paul MADDOX

IPC: C07D471/04 ,  C07D417/08 ,  C07D417/14 ,  C07D498/18 ,  C07D491/107 ,  A61P35/02 ,  A61P19/02

CPC classification number: C07D471/04 ,  C07D417/08 ,  C07D417/14 ,  A61P19/02 ,  C07D491/107 ,  A61P35/02 ,  C07D498/18

Abstract: A compound represented by the general formula (1) or a salt thereof, which has a superior IRAK-4 inhibitory activity, and is useful as active ingredients of medicaments for prophylactic treatment and/or therapeutic treatment of diseases relating to IRAK-4 inhibition.

公开(公告)号：US20240018118A1

公开(公告)日：2024-01-18

申请号：US18134990

申请日：2023-04-14

Applicant: C 4 Therapeutics, Inc.

Inventor： Christopher G. Nasveschuk ,  Corey Don Anderson ,  James A. Henderson ,  Victoria Garza ,  Moses Moustakim ,  Morgan Welzel O'shea

IPC: C07D401/04 ,  C07D471/06 ,  C07D487/06 ,  C07D498/06 ,  C07D413/04 ,  C07D417/04 ,  C07D403/04 ,  C07D491/107 ,  C07D513/20 ,  C07D209/92 ,  C07F5/02 ,  C07D401/14 ,  C07D498/08 ,  C07D405/14 ,  C07D417/14

CPC classification number: C07D401/04 ,  C07D417/14 ,  C07D487/06 ,  C07D498/06 ,  C07D413/04 ,  C07D417/04 ,  C07D403/04 ,  C07D491/107 ,  C07D513/20 ,  C07D209/92 ,  C07F5/025 ,  C07D401/14 ,  C07D498/08 ,  C07D405/14 ,  C07D471/06

Abstract: The invention provides tricyclic compounds that degrade neosubstrates for use in the treatment of disorders described herein, including, for example, abnormal cellular proliferation, neurodegenerative diseases, and autoimmune diseases.

公开(公告)号：US20230416205A1

公开(公告)日：2023-12-28

申请号：US18037999

申请日：2021-11-19

Applicant: Denali Therapeutics Inc

Inventor： Alex L. Bagdasarian ,  Cyril Bucher ,  Robert A. Craig, II ,  Javier de Vicente Fidalgo ,  Anthony A. Estrada ,  Brian M. Fox ,  Cheng Hu ,  Benjamin J. Huffman ,  Katrina W. Lexa ,  Lizanne G. Nilewski ,  Maksim Osipov ,  Arun Thottumkara

IPC: C07D217/24 ,  C07D401/12 ,  C07D471/04 ,  C07D401/14 ,  C07D493/08 ,  C07D491/107 ,  C07D413/08 ,  C07D405/12 ,  C07D417/12 ,  C07D487/04 ,  C07D417/14 ,  C07D498/04 ,  C07D405/14 ,  C07D495/04

CPC classification number: C07D217/24 ,  C07D401/12 ,  C07D471/04 ,  C07D401/14 ,  C07D493/08 ,  C07D491/107 ,  C07D413/08 ,  C07D405/12 ,  C07D417/12 ,  C07D487/04 ,  C07D417/14 ,  C07D498/04 ,  C07D405/14 ,  C07D495/04

Abstract: The present disclosure relates generally to small molecule modulators of NLR Family Pyrin Domain Containing 3 (NL-RP3), or a pharmaceutically acceptable salt, isotopically enriched analog, stereoisomer, mixture of stereoisomers, or prodrug thereof, methods of making and intermediates thereof, and methods of using thereof.

公开(公告)号：US11851422B2

公开(公告)日：2023-12-26

申请号：US17811008

申请日：2022-07-06

Applicant: Aligos Therapeutics, Inc. ,  Katholieke Universiteit Leuven

Inventor： Koen Vandyck ,  Dorothée Alice Marie-Eve Bardiot ,  Pierre Jean-Marie Bernard Raboisson ,  Leonid Beigelman ,  Antitsa Dimitrova Stoycheva ,  Sandro Boland ,  Arnaud Didier Marie Marchand

IPC: C07D401/12 ,  C07D401/14 ,  C07D403/12 ,  C07D403/14 ,  C07D405/14 ,  C07D413/12 ,  C07D413/14 ,  C07D487/04 ,  C07D491/04 ,  C07D491/107 ,  C07D498/04 ,  A61P31/14 ,  A61K31/403 ,  A61K31/422 ,  A61K31/4439 ,  A61K31/497 ,  A61K31/519 ,  A61K31/437 ,  A61K31/4709 ,  A61K31/407 ,  A61K31/4155 ,  A61K31/538 ,  A61K31/5377 ,  A61K31/4245 ,  A61K31/553 ,  A61K31/4192

CPC classification number: C07D403/12 ,  C07D403/14 ,  C07D405/14 ,  C07D413/12 ,  C07D413/14 ,  C07D487/04 ,  C07D491/107 ,  C07D498/04

Abstract: Provided herein are compounds of Formula (I), or pharmaceutically acceptable salts thereof, pharmaceutical compositions that include a compound described herein (including pharmaceutically acceptable salts of a compound described herein) and methods of synthesizing the same. Also provided herein are methods of treating diseases and/or conditions with a compound of Formula (I), or a pharmaceutically acceptable salt thereof.