公开(公告)号：US12110283B2

公开(公告)日：2024-10-08

申请号：US17372029

申请日：2021-07-09

Applicant: VisEn Medical, Inc.

Inventor： Kevin Groves ,  Bagna Bao

IPC: C07D401/06 ,  A61K31/433 ,  A61K31/4439 ,  A61K31/444 ,  A61K31/506 ,  A61K49/00 ,  C07D209/14 ,  C07D209/60 ,  C07D401/14 ,  C07D417/14 ,  C09B23/01 ,  C09B23/08 ,  G01N21/64 ,  G01N33/58

CPC classification number: C07D401/06 ,  A61K31/433 ,  A61K31/4439 ,  A61K31/444 ,  A61K31/506 ,  A61K49/0002 ,  A61K49/0032 ,  A61K49/0052 ,  C07D209/14 ,  C07D209/60 ,  C07D401/14 ,  C07D417/14 ,  C09B23/0008 ,  C09B23/0033 ,  C09B23/083 ,  C09B23/086 ,  G01N21/6458 ,  G01N33/582 ,  G01N2333/988 ,  Y02A50/30

Abstract: The invention provides agents that target carbonic anhydrase, which can be used as imaging agents or therapeutic agents. The agents can be used to image tumor hypoxia as well as other physiological processes in a subject.

公开(公告)号：US20240327334A1

公开(公告)日：2024-10-03

申请号：US18390287

申请日：2023-12-20

Applicant: Enanta Pharmaceuticals, Inc.

Inventor： Xuri GAO ,  Bin WANG ,  Hui CAO ,  Jiajun ZHANG ,  Yuk Ming SIU ,  Jiang LONG ,  Wei LI ,  Matthew C. RHODES ,  Xuechao XING ,  Jianming YU ,  Scott MITCHELL ,  Yat Sun OR

IPC: C07C233/56 ,  A61K31/166 ,  A61K31/277 ,  A61K31/337 ,  A61K31/365 ,  A61K31/381 ,  A61K31/397 ,  A61K31/40 ,  A61K31/403 ,  A61K31/415 ,  A61K31/4152 ,  A61K31/416 ,  A61K31/4192 ,  A61K31/42 ,  A61K31/421 ,  A61K31/426 ,  A61K31/427 ,  A61K31/4402 ,  A61K31/4439 ,  A61K31/47 ,  A61K31/4709 ,  A61K31/495 ,  A61K31/4965 ,  A61K31/505 ,  A61K31/506 ,  A61K31/535 ,  A61K31/662 ,  A61P31/14 ,  C07C243/30 ,  C07C255/46 ,  C07C255/66 ,  C07D205/04 ,  C07D207/16 ,  C07D209/52 ,  C07D209/56 ,  C07D213/40 ,  C07D215/12 ,  C07D231/08 ,  C07D231/12 ,  C07D231/56 ,  C07D239/26 ,  C07D241/12 ,  C07D249/06 ,  C07D263/32 ,  C07D263/34 ,  C07D265/02 ,  C07D277/28 ,  C07D295/185 ,  C07D305/08 ,  C07D307/58 ,  C07D333/20 ,  C07D333/24 ,  C07D401/04 ,  C07D401/12 ,  C07D403/12 ,  C07D417/12 ,  C07D417/14 ,  C07F9/40

CPC classification number: C07C233/56 ,  A61K31/166 ,  A61K31/277 ,  A61K31/337 ,  A61K31/365 ,  A61K31/381 ,  A61K31/397 ,  A61K31/40 ,  A61K31/403 ,  A61K31/415 ,  A61K31/4152 ,  A61K31/416 ,  A61K31/4192 ,  A61K31/42 ,  A61K31/421 ,  A61K31/426 ,  A61K31/427 ,  A61K31/4402 ,  A61K31/4439 ,  A61K31/47 ,  A61K31/4709 ,  A61K31/495 ,  A61K31/4965 ,  A61K31/505 ,  A61K31/506 ,  A61K31/535 ,  A61K31/662 ,  A61P31/14 ,  C07C243/30 ,  C07C255/46 ,  C07C255/66 ,  C07D205/04 ,  C07D207/16 ,  C07D209/52 ,  C07D209/56 ,  C07D213/40 ,  C07D215/12 ,  C07D231/08 ,  C07D231/12 ,  C07D231/56 ,  C07D239/26 ,  C07D241/12 ,  C07D249/06 ,  C07D263/32 ,  C07D263/34 ,  C07D265/02 ,  C07D277/28 ,  C07D295/185 ,  C07D305/08 ,  C07D307/58 ,  C07D333/20 ,  C07D333/24 ,  C07D401/04 ,  C07D401/12 ,  C07D403/12 ,  C07D417/12 ,  C07D417/14 ,  C07F9/4015

Abstract: The present invention discloses compounds of Formula (I), and pharmaceutically acceptable salts, thereof:




which inhibit coronavirus replication activity. The invention further relates to pharmaceutical compositions comprising a compound of Formula (I) or a pharmaceutically acceptable salt thereof, and methods of treating or preventing a coronavirus infection in a subject in need thereof, comprising administering to the subject a therapeutically effective amount of a compound of Formula (I) or a pharmaceutically acceptable salt thereof.

公开(公告)号：US20240317729A1

公开(公告)日：2024-09-26

申请号：US18667078

申请日：2024-05-17

Applicant: YALE UNIVERSITY ,  GLAXOSMITHKLINE INTELLECTUAL PROPERTY DEVELOPMENT LIMITED ,  CAMBRIDGE ENTERPRISE LIMITED

Inventor： CRAIG M. CREWS ,  DENNIS BUCKLEY ,  ALESSIO CIULLI ,  WILLIAM L. JORGENSEN ,  PETER C. GAREISS ,  INGE VAN MOLLE ,  JEFFREY GUSTAFSON ,  HYUN-SEOP TAE ,  JULIEN MICHEL ,  DENTON WADE HOYER ,  ANKE G. ROTH ,  JOHN DAVID HARLING ,  IAN EDWARD DAVID SMITH ,  AFJAL HUSSAIN MIAH ,  SEBASTIEN ANDRE CAMPOS ,  JOELLE LE

IPC: C07D413/14 ,  A61K31/422 ,  A61K31/427 ,  A61K31/437 ,  A61K31/4439 ,  A61K31/454 ,  A61K31/5377 ,  A61K38/05 ,  A61K38/06 ,  A61K45/06 ,  A61K47/54 ,  A61K47/55 ,  A61K47/64 ,  C07D207/16 ,  C07D207/26 ,  C07D401/06 ,  C07D401/10 ,  C07D403/06 ,  C07D405/06 ,  C07D405/12 ,  C07D413/06 ,  C07D413/12 ,  C07D417/12 ,  C07D417/14 ,  C07D471/04 ,  C07J43/00 ,  C12N9/00

CPC classification number: C07D413/14 ,  A61K31/422 ,  A61K31/427 ,  A61K31/437 ,  A61K31/4439 ,  A61K31/454 ,  A61K31/5377 ,  A61K38/05 ,  A61K38/06 ,  A61K45/06 ,  A61K47/545 ,  A61K47/55 ,  A61K47/64 ,  C07D207/16 ,  C07D207/26 ,  C07D401/06 ,  C07D401/10 ,  C07D403/06 ,  C07D405/06 ,  C07D405/12 ,  C07D413/06 ,  C07D413/12 ,  C07D417/12 ,  C07D417/14 ,  C07D471/04 ,  C07J43/003 ,  C12N9/93

Abstract: The present invention relates to bifunctional compounds, which find utility as modulators of targeted ubiquitination, especially inhibitors of a variety of polypeptides and other proteins which are degraded and/or otherwise inhibited by bifunctional compounds according to the present invention. In particular, the present invention is directed to compounds, which contain on one end a VHL ligand which binds to the ubiquitin ligase and on the other end a moiety which binds a target protein such that the target protein is placed in proximity to the ubiquitin ligase to effect degradation (and inhibition) of that protein. The present invention exhibits a broad range of pharmacological activities associated with compounds according to the present invention, consistent with the degradation/inhibition of targeted polypeptides.

公开(公告)号：US20240308992A1

公开(公告)日：2024-09-19

申请号：US18662284

申请日：2024-05-13

Applicant: Biopolar Youtang(Guangdong) Pharmaceutical Co., Ltd.

Inventor： Zhijian LV ,  Li ZHONG

IPC: C07D409/04 ,  A61K31/4965 ,  A61K31/497 ,  A61K31/4985 ,  A61K31/519 ,  A61K31/5377 ,  A61K31/538 ,  A61K31/541 ,  C07D241/20 ,  C07D409/14 ,  C07D413/14 ,  C07D417/04 ,  C07D417/14 ,  C07D471/04 ,  C07D487/04

CPC classification number: C07D409/04 ,  A61K31/4965 ,  A61K31/497 ,  A61K31/4985 ,  A61K31/519 ,  A61K31/5377 ,  A61K31/538 ,  A61K31/541 ,  C07D241/20 ,  C07D409/14 ,  C07D413/14 ,  C07D417/04 ,  C07D417/14 ,  C07D471/04 ,  C07D487/04

Abstract: Provided are a compound as represented by formula I serving as a DRK2 inhibitor, or a stereoisomer or optical isomer, a pharmaceutically acceptable salt, a prodrug or a solvate thereof. Further provided are a preparation method for the compound, a pharmaceutical composition thereof, and the use thereof as a Drak2 inhibitor and in the preparation of a drug for preventing and/or treating a Drak2-related disease.

公开(公告)号：US20240308982A1

公开(公告)日：2024-09-19

申请号：US18576068

申请日：2022-07-07

Applicant: DANA-FARBER CANCER INSTITUTE, INC.

Inventor： Nathanael S. Gray ,  John Hatcher

IPC: C07D401/14 ,  A61K31/506 ,  C07D417/14

CPC classification number: C07D401/14 ,  A61K31/506 ,  C07D417/14

Abstract: Disclosed are bifunctional compounds and pharmaceutically acceptable salts and stereoisomers thereof that that are potent and selective degraders of LRRK2. Also disclosed are pharmaceutical compositions containing same, and methods of making and using the compounds to treat diseases and disorders associated with LRRK2. In some embodiments, the disease or disorder is a neurodegenerative disorder. Parkinson's disease (PD), an inflammatory bowel disease (IBD), Crohn's disease (CD), leprosy (Hansen's disease), tuberculosis, meningioma, breast cancer, lung cancer or thyroid cancer.

公开(公告)号：US12091407B2

公开(公告)日：2024-09-17

申请号：US18295133

申请日：2023-04-03

Applicant: vTv Therapeutics LLC

Inventor： Adnan M. M. Mjalli ,  Dharma Rao Polisetti ,  Jareer Nabeel Kassis ,  Matthew J. Kostura ,  Mustafa Guzel ,  Otis Clinton Attucks ,  Robert Carl Andrews ,  Samuel Victory ,  Suparna Gupta

IPC: C07D417/12 ,  A61K31/4168 ,  A61K31/4188 ,  A61K31/428 ,  A61K31/437 ,  A61P1/16 ,  C07D235/30 ,  C07D417/14 ,  C07D471/04 ,  C07D513/04

CPC classification number: C07D417/12 ,  A61K31/4168 ,  A61K31/4188 ,  A61K31/428 ,  A61K31/437 ,  A61P1/16 ,  C07D235/30 ,  C07D417/14 ,  C07D471/04 ,  C07D513/04

Abstract: Substituted fused imidazole derivatives, methods of their preparation, pharmaceutical compositions comprising a substituted fused imidazole derivative, and methods of use in treating renal diseases are provided. The substituted fused imidazole derivatives may control the activity or the amount or both the activity and the amount of heme-oxygenase.

公开(公告)号：US20240300936A1

公开(公告)日：2024-09-12

申请号：US18568365

申请日：2022-06-09

Applicant: AVELOS THERAPEUTICS INC.

Inventor： Ki Seon BAEK ,  Ja Heouk KHOO ,  Soongyu CHOI ,  Young Whan PARK ,  Simon WARD ,  Darren LE GRAND ,  Ryan WEST ,  Penelope TURNER ,  Samuele MARAMAI ,  Tristan REUILLON

IPC: C07D413/14 ,  A61K31/506 ,  A61K31/53 ,  A61K31/5377 ,  A61P35/00 ,  C07D401/14 ,  C07D403/04 ,  C07D403/14 ,  C07D405/14 ,  C07D417/14 ,  C07D471/04 ,  C07D513/04

CPC classification number: C07D413/14 ,  A61K31/506 ,  A61K31/53 ,  A61K31/5377 ,  A61P35/00 ,  C07D401/14 ,  C07D403/04 ,  C07D403/14 ,  C07D405/14 ,  C07D417/14 ,  C07D471/04 ,  C07D513/04

Abstract: This invention relates to compounds which are microtubule associated serine/threonine-like kinase (MASTL) inhibitors and the use of the compounds in the treatment of diseases and medical conditions mediated by MASTL, for example in the treatment of cancer and other target related diseases.

公开(公告)号：US20240300905A1

公开(公告)日：2024-09-12

申请号：US18583526

申请日：2024-02-21

Applicant: Prosetta Biosciences, Inc.

Inventor： Dennis Solas ,  Anuradha F. Lingappa ,  Vishwanath R. Lingappa

IPC: C07D239/94 ,  A61P31/18 ,  A61P33/06 ,  A61P35/00 ,  C07D401/12 ,  C07D401/14 ,  C07D403/12 ,  C07D403/14 ,  C07D405/14 ,  C07D417/14

CPC classification number: C07D239/94 ,  A61P31/18 ,  A61P33/06 ,  A61P35/00 ,  C07D401/12 ,  C07D401/14 ,  C07D403/12 ,  C07D403/14 ,  C07D405/14 ,  C07D417/14

Abstract: Disclosed are novel heterocyclic compounds such as novel quinazoline compounds and pharmaceutical compositions thereof which may be used to treat or prevent malaria, HIV infection and cancer.

公开(公告)号：US12084436B2

公开(公告)日：2024-09-10

申请号：US17426971

申请日：2020-01-29

Applicant: Takeda Pharmaceutical Company Limited

Inventor： Masahiro Ito ,  Takeshi Yamamoto ,  Keiko Kakegawa ,  Hideyuki Sugiyama ,  Tohru Miyazaki ,  Yasuyoshi Arikawa ,  Tomohiro Okawa ,  Jinichi Yonemori ,  Osamu Kubo ,  Akinori Toita ,  Takuto Kojima ,  Fumiaki Kikuchi ,  Minoru Sasaki ,  Misaki Homma ,  Yasuhiro Imaeda ,  Hironobu Maezaki ,  Shiinobu Sasaki ,  Ayumu Sato ,  Hirotaka Kamitani ,  Yasutomi Asano ,  Hironori Kokubo ,  Masato Yoshikawa

IPC: C07D413/10 ,  C07D271/06 ,  C07D413/14 ,  C07D417/14

CPC classification number: C07D413/10 ,  C07D271/06 ,  C07D413/14 ,  C07D417/14

Abstract: The present invention provides a heterocyclic compound having a HDAC inhibitory action, which is useful for the treatment of central nervous system diseases including neurodegenerative diseases, and the like, and a medicament comprising the compound.
The present invention relates to a compound represented by the formula (I):




wherein each symbol is as described in the description, or a salt thereof.

公开(公告)号：US12084414B2

公开(公告)日：2024-09-10

申请号：US17506276

申请日：2021-10-20

Applicant: eXIthera Pharmaceuticals, Inc.

Inventor： Robert A. Chrusciel ,  Robert C. Gadwood ,  Neil J. Hayward ,  Michael J. Melnick ,  Manuel A. Navia ,  Toni J. Poel ,  Frans L. Stassen ,  Catherine A. Stewart

IPC: C07D205/08 ,  C07D401/06 ,  C07D401/14 ,  C07D403/06 ,  C07D405/14 ,  C07D409/06 ,  C07D417/06 ,  C07D417/14

CPC classification number: C07D205/08 ,  C07D401/06 ,  C07D401/14 ,  C07D403/06 ,  C07D405/14 ,  C07D409/06 ,  C07D417/06 ,  C07D417/14

Abstract: The present invention provides compounds and compositions that inhibit Factor XIa or kallikrein and methods of using these compounds and composition.