公开(公告)号：US20240336611A1

公开(公告)日：2024-10-10

申请号：US18547190

申请日：2022-02-23

申请人： Insilico Medicine IP Limited

发明人： Aleksandrs ZAVORONKOVS ,  Aleksandr ALIPER ,  Vladimir ALADINSKIY ,  Andrey KUKHARENKO ,  Luoheng QUIN ,  Xin CHENG

IPC分类号： C07D471/08 ,  A61K31/4178 ,  A61K31/422 ,  A61K31/427 ,  A61K31/4375 ,  A61K31/438 ,  A61K31/4439 ,  A61K31/496 ,  A61K31/4995 ,  C07D401/14 ,  C07D403/14 ,  C07D413/14 ,  C07D417/14 ,  C07D471/04 ,  C07D471/10 ,  C07D487/10

CPC分类号： C07D471/08 ,  A61K31/4178 ,  A61K31/422 ,  A61K31/427 ,  A61K31/4375 ,  A61K31/438 ,  A61K31/4439 ,  A61K31/496 ,  A61K31/4995 ,  C07D401/14 ,  C07D403/14 ,  C07D413/14 ,  C07D417/14 ,  C07D471/04 ,  C07D471/10 ,  C07D487/10

摘要： Provided are TNIK and/or MAP4K4 kinases inhibitors for the treatment of disease. In one aspect, disclosed herein are kinase inhibitors having a structure of Formulas (A), (A*), (I), (II), (AA), (B), (C), (D), (B*), (C*) and (D*). Further described herein are pharmaceutical composition comprising these compounds and methods of using these compounds. In one aspect, disclosed herein are methods of treating a disease or condition by administering the kinases inhibitors described herein.

公开(公告)号：US20240327334A1

公开(公告)日：2024-10-03

申请号：US18390287

申请日：2023-12-20

申请人： Enanta Pharmaceuticals, Inc.

发明人： 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分类号： 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分类号： 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

摘要： 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

申请人： YALE UNIVERSITY ,  GLAXOSMITHKLINE INTELLECTUAL PROPERTY DEVELOPMENT LIMITED ,  CAMBRIDGE ENTERPRISE LIMITED

发明人： 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分类号： 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分类号： 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

摘要： 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：US20240316190A1

公开(公告)日：2024-09-26

申请号：US18495541

申请日：2023-10-26

申请人： Augusta University Research Institute, Inc.

发明人： Samir N. Khleif ,  Mikayel Mkrtichyan

IPC分类号： A61K39/39 ,  A61K31/427 ,  A61K31/52 ,  A61K31/5377 ,  A61K39/00 ,  A61K45/06

CPC分类号： A61K39/39 ,  A61K31/427 ,  A61K31/52 ,  A61K31/5377 ,  A61K45/06 ,  A61K2039/55511

摘要： It has been discovered that PIK3δ (PIK3delta) selectively modulates the activation and proliferation of natural Tregs. Methods of modulating immune responses by modulating PIK3δ bioavailability or biological activity are provided.

公开(公告)号：US20240301417A1

公开(公告)日：2024-09-12

申请号：US18570892

申请日：2022-06-15

申请人： Sanford Burnham Prebys Medical Discovery Institute

发明人： Cynthia LEBEAUPIN ,  Randal J. KAUFMAN ,  Clementine DRUELLE

IPC分类号： C12N15/113 ,  A61K31/421 ,  A61K31/427 ,  A61K31/433 ,  A61K31/4439 ,  A61K31/444 ,  A61K31/4545 ,  A61K31/497 ,  A61K31/506 ,  A61K31/5377 ,  A61K49/00 ,  A61P35/00

CPC分类号： C12N15/113 ,  A61K31/421 ,  A61K31/427 ,  A61K31/433 ,  A61K31/4439 ,  A61K31/444 ,  A61K31/4545 ,  A61K31/497 ,  A61K31/506 ,  A61K31/5377 ,  A61K49/0008 ,  A61P35/00 ,  C12N2310/11 ,  C12N2310/351

摘要： Described herein are compositions and methods useful for detecting and treating pathologies associated with ATF in hepatocytes. A method of detecting a condition, a method of inhibiting a protein, a method of inhibiting a gene, and a method of treatment are disclosed herein. The present disclosure includes, but is not limited to, the development and testing of Atf6-specific short, synthetic, single-stranded antisense oligodeoxynucleotides (ASOs) in vitro and in vivo and future screening for ATF6 inhibitors.

公开(公告)号：US20240293377A1

公开(公告)日：2024-09-05

申请号：US18409703

申请日：2024-01-10

申请人： The United States Government As Represented By The Department Of Veterans Affairs ,  Wayne State University

发明人： ARUN K. RISHI ,  NAVNATH GAVANDE

IPC分类号： A61K31/427 ,  A61K31/282 ,  A61K31/40 ,  A61K31/4164 ,  A61K31/704 ,  A61K47/54

CPC分类号： A61K31/427 ,  A61K31/282 ,  A61K31/40 ,  A61K31/4164 ,  A61K47/557 ,  A61K31/704

摘要： Described herein are compositions and methods for treating cancer in a subject. The compositions include selective NF-κB inhibitor inhibitors. The methods include inhibiting the binding of CARP-1 with NEMO.

公开(公告)号：US20240279207A1

公开(公告)日：2024-08-22

申请号：US18032067

申请日：2021-10-14

申请人： The Broad Institute, Inc. ,  Bayer Aktiengesellschaft

发明人： Léa Bouché ,  Daniel Korr ,  Antonius ter Laak ,  Michael Kröber ,  Naomi Barak ,  Roman Hillig ,  Roland Neuhaus ,  Stefan Gradl ,  Jörg Wichard ,  Ernesto Amaury Fernamdez-Montalvan ,  Matyas Gorjanacz ,  Vera Pütter ,  Andreas Stutter ,  Steven James Ferrara

IPC分类号： C07D405/04 ,  A61K31/397 ,  A61K31/4025 ,  A61K31/404 ,  A61K31/4155 ,  A61K31/4192 ,  A61K31/422 ,  A61K31/4245 ,  A61K31/427 ,  A61K31/433 ,  A61K31/437 ,  A61K31/443 ,  A61K31/4525 ,  A61K31/4709 ,  A61K31/4725 ,  A61K31/496 ,  A61K31/498 ,  A61K31/5025 ,  A61K31/5365 ,  A61K31/5377 ,  A61K31/539 ,  A61P35/00 ,  C07D405/14 ,  C07D409/14 ,  C07D413/14 ,  C07D417/14 ,  C07D471/04 ,  C07D487/04 ,  C07D491/107 ,  C07D498/04

CPC分类号： C07D405/04 ,  A61K31/397 ,  A61K31/4025 ,  A61K31/404 ,  A61K31/4155 ,  A61K31/4192 ,  A61K31/422 ,  A61K31/4245 ,  A61K31/427 ,  A61K31/433 ,  A61K31/437 ,  A61K31/443 ,  A61K31/4525 ,  A61K31/4709 ,  A61K31/4725 ,  A61K31/496 ,  A61K31/498 ,  A61K31/5025 ,  A61K31/5365 ,  A61K31/5377 ,  A61K31/539 ,  A61P35/00 ,  C07D405/14 ,  C07D409/14 ,  C07D413/14 ,  C07D417/14 ,  C07D471/04 ,  C07D487/04 ,  C07D491/107 ,  C07D498/04

摘要： The present invention provides acyl sulfonamide compounds of general formula (I):






in which R1, R2, R3, R4, R5, R6, Ra and Rb are as described and defined herein, methods of preparing said compounds, intermediate compounds useful for preparing said compounds, pharmaceutical compositions and combinations comprising said compounds, and the use of said compounds for manufacturing pharmaceutical compositions for the treatment or prophylaxis of diseases, in particular of hyperproliferative disorders, as a sole agent or in combination with other active ingredients as well as methods of treatment and/or prophylaxis of diseases, particularly cancer, more particularly cancer in which KAT6A and/or KAT6B is focally amplified, said method comprising administering an effective amount of at least one compound of formula (I) to a subject in need thereof.

公开(公告)号：US20240279201A1

公开(公告)日：2024-08-22

申请号：US18565426

申请日：2022-06-01

申请人： Fengtian Xue ,  Yan Shu ,  Yong Ai

发明人： Fengtian Xue ,  Yan Shu ,  Yong Ai

IPC分类号： C07D401/12 ,  A61K31/423 ,  A61K31/427 ,  A61K31/428 ,  A61K31/4375 ,  A61K31/4439 ,  A61K31/4709 ,  A61K31/496 ,  A61K31/498 ,  A61K31/517 ,  A61K31/69 ,  A61K45/06 ,  A61K47/55 ,  A61K47/60 ,  A61P1/16 ,  A61P35/00 ,  C07D401/14 ,  C07D403/12 ,  C07D413/12 ,  C07D417/12 ,  C07D417/14 ,  C07D471/04 ,  C07F5/02

CPC分类号： C07D401/12 ,  A61K31/423 ,  A61K31/427 ,  A61K31/428 ,  A61K31/4375 ,  A61K31/4439 ,  A61K31/4709 ,  A61K31/496 ,  A61K31/498 ,  A61K31/517 ,  A61K31/69 ,  A61K45/06 ,  A61K47/551 ,  A61K47/60 ,  A61P1/16 ,  A61P35/00 ,  C07D401/14 ,  C07D403/12 ,  C07D413/12 ,  C07D417/12 ,  C07D417/14 ,  C07D471/04 ,  C07F5/025

摘要： Compounds and compositions are provided as inhibitors of the Wnt/beta-catenin pathway and/or activators of the adenosine monophosphate-activated kinase (AMPK) pathway for the treatment of diseases that implicate the same. Such diseases include cancer or a metabolic disease. Cancers that may be treated by these compounds and compositions include adrenocortical cancer, hepatocellular cancer, hepatoblastoma, malignant melanoma, ovarian cancer, Wilm's tumor, Barrett's esophageal cancer, prostate cancer, colon cancer, colorectal cancer, rectal cancer, pancreatic cancer, bladder cancer, breast cancer (e.g. triple negative breast cancer), gastric cancer, head & neck cancer, lung cancer, mesothelioma, cervical cancer, uterine cancer, myeloid leukemia cancer, lymphoid leukemia cancer, pilometricoma cancer, medulloblastoma cancer, glioblastoma, and familial adenomatous polyposis. Metabolic diseases include type 2 diabetes, obesity, hyperlipidemia, alcoholic or non-alcoholic fatty liver disease, and liver fibrosis.

公开(公告)号：US20240269111A1

公开(公告)日：2024-08-15

申请号：US18561103

申请日：2022-05-16

申请人： METANOIA BIO INC.

发明人： Margaretha ROUX ,  Slavica TUDZAROVA-TRAJKOVSKA ,  Abraham VAN WYK

IPC分类号： A61K31/404 ,  A61K31/196 ,  A61K31/245 ,  A61K31/352 ,  A61K31/381 ,  A61K31/403 ,  A61K31/41 ,  A61K31/4155 ,  A61K31/422 ,  A61K31/427 ,  A61K31/444 ,  A61K31/47 ,  A61K31/4709 ,  A61K31/498 ,  A61K31/501 ,  A61K31/506 ,  A61K31/519 ,  A61K45/06

CPC分类号： A61K31/404 ,  A61K31/196 ,  A61K31/245 ,  A61K31/352 ,  A61K31/381 ,  A61K31/403 ,  A61K31/41 ,  A61K31/4155 ,  A61K31/422 ,  A61K31/427 ,  A61K31/444 ,  A61K31/47 ,  A61K31/4709 ,  A61K31/498 ,  A61K31/501 ,  A61K31/506 ,  A61K31/519 ,  A61K45/06

摘要： The disclosure provides compositions and methods for treating ocular neovascular diseases and conditions with HIF1-α Pathway Inhibitors and PFKFB3 Inhibitors. Exemplary ocular neovascular diseases and conditions treated using the provided compositions and methods include diabetic retinopathy, diabetic macular edema, age-related macular degeneration, and choroidal neovascular membranes.

公开(公告)号：US12048691B2

公开(公告)日：2024-07-30

申请号：US17525619

申请日：2021-11-12

申请人： SPERO THERAPEUTICS, INC.

发明人： Akash Jain ,  Ching-Kuo Jim Chow

IPC分类号： A61K9/20 ,  A61K31/427 ,  A61P31/04

CPC分类号： A61K31/427 ,  A61K9/2009 ,  A61K9/2027 ,  A61K9/2054 ,  A61P31/04

摘要： The disclosure provides a tebipenem pivoxil HBr formulation in the form of a tablet core comprising at least 70% (w/w) tebipenem pivoxil HBr, and in certain embodiment more than 80% (w/w) tebipenem pivoxil HBr. The disclosure provides a tebipenem pivoxil HBr tablet core comprising at least 70% w/w tebipenem pivoxil HBr, 5-25% w/w of a diluent, 0.5 to 5% w/w of a glidant, 0.5 to 5% w/w of a lubricant, and optionally 0.5 to 5% w/w of disintegrant. The disclosure provides methods of treating a patient who has a bacterial infection such as complicated urinary tract infection (cUTI), acute and chronic pyelonephritis, an upper or lower respiratory infection, or bacteremia by administering a formulation of the disclosure to the patient.