公开(公告)号：US12128028B2

公开(公告)日：2024-10-29

申请号：US17258273

申请日：2019-07-05

申请人： METRION BIOSCIENCES LIMITED

发明人： Marc Rogers ,  Robert Kirby ,  Gakujun Shomi ,  Takuya Matsuo ,  Satoru Kobayashi ,  Junichiro Kanazawa ,  Nobutaka Yamaoka ,  Makoto Torizuka ,  Koichi Suzawa

IPC分类号： A61K31/4164 ,  A61K31/4178 ,  A61K31/439 ,  A61K31/4439 ,  A61K31/454 ,  A61K31/46 ,  A61K31/5377 ,  A61K31/55 ,  C07D233/28 ,  C07D235/02 ,  C07D401/06 ,  C07D401/12 ,  C07D403/06 ,  C07D403/12 ,  C07D405/12 ,  C07D409/12 ,  C07D471/08 ,  C07D491/107

CPC分类号： A61K31/4164 ,  A61K31/4178 ,  A61K31/439 ,  A61K31/4439 ,  A61K31/454 ,  A61K31/46 ,  A61K31/5377 ,  A61K31/55 ,  C07D233/28 ,  C07D235/02 ,  C07D401/06 ,  C07D401/12 ,  C07D403/06 ,  C07D403/12 ,  C07D405/12 ,  C07D409/12 ,  C07D471/08 ,  C07D491/107

摘要： The invention relates to heterocyclic sulfonamide derivatives and their use in the treatment and prophylaxis of autoimmune, inflammatory, cardiovascular, neuronal, auditory, renal and metabolic mediated diseases, and to compositions containing said derivatives and processes for their preparation.

公开(公告)号：US20240350458A1

公开(公告)日：2024-10-24

申请号：US18580822

申请日：2022-07-21

申请人： Simona Rapposelli ,  Eugenio Gaudio ,  Fabrizio Dal Piaz

发明人： Simona Rapposelli ,  Eugenio Gaudio ,  Fabrizio Dal Piaz

IPC分类号： A61K31/4178 ,  A61K31/404 ,  A61K31/4155 ,  A61K31/4439 ,  A61P5/00 ,  C07D209/34 ,  C07D401/06 ,  C07D403/06 ,  C07D409/06

CPC分类号： A61K31/4178 ,  A61K31/404 ,  A61K31/4155 ,  A61K31/4439 ,  A61P5/00 ,  C07D209/34 ,  C07D401/06 ,  C07D403/06 ,  C07D409/06

摘要： The invention relates to a 2-oxoindole compound of Formula (I) or a pharmaceutically acceptable salt thereof, wherein R1 and R2 are, independently from each other, hydrogen, 1H-imidazolyl, thienyl and 1-methyl-1H-imidazolyl, 2-methyl-1H-imidazolyl, 2-aminopyridinyl, 1H-pyrazolyl, with the proviso that one of R1 and R2 is hydrogen; or R1 and R2 together form 9H-fluorene R3 is hydrogen, (C1-C3)alkyl, halogen or NO2; for use as a 14-3-3 protein modulator of a tumor selected from the group consisting of a lymphoma, chronic lymphocytic leukaemia (CLL), Ewing sarcoma, colon cancer, melanoma and anaplastic thyroid cancer (ATC). The invention relates also new 2-oxoindole compound of Formula (I) or a pharmaceutically acceptable salt thereof.

公开(公告)号：US20240336604A1

公开(公告)日：2024-10-10

申请号：US18294663

申请日：2022-08-03

申请人： THE UNITED STATES OF AMERICA, AS REPRESENTED BY THE SECRETARY, DEPT. OF HEALTH AND HUMAN SERVICES ,  THE UNIVERSITY OF NORTH CAROLINA AT CHAPEL HILL

发明人： Disha GANDHI ,  Kevin FRANKOWSKI ,  Marc FERRER ,  R. Benjamin FREE ,  David R. SIBLEY ,  Amy E. MORITZ ,  Noel Terrence SOUTHALL ,  Xin HU ,  Amber KELLEY

IPC分类号： C07D413/06 ,  A61K31/4025 ,  A61K31/424 ,  A61K31/426 ,  A61K31/454 ,  A61K31/496 ,  A61K31/5377 ,  C07D207/416 ,  C07D277/14 ,  C07D401/06 ,  C07D403/06 ,  C07D498/10

CPC分类号： C07D413/06 ,  A61K31/4025 ,  A61K31/424 ,  A61K31/426 ,  A61K31/454 ,  A61K31/496 ,  A61K31/5377 ,  C07D207/416 ,  C07D277/14 ,  C07D401/06 ,  C07D403/06 ,  C07D498/10

摘要： Compounds of Formula I, Formula II, and Formula III and the pharmaceutically acceptable salts thereof are disclosed. The variables R1-10 are disclosed herein. The compounds are useful for treating central nervous system disorders, especially those involving substance use disorder and/or withdrawal syndrome. Pharmaceutical compositions containing compounds of Formula I or Formula II or Formula III and methods of treatment comprising administering compounds of Formula I or Formula II or Formula III are also disclosed.

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：US12084414B2

公开(公告)日：2024-09-10

申请号：US17506276

申请日：2021-10-20

申请人： eXIthera Pharmaceuticals, Inc.

发明人： 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分类号： C07D205/08 ,  C07D401/06 ,  C07D401/14 ,  C07D403/06 ,  C07D405/14 ,  C07D409/06 ,  C07D417/06 ,  C07D417/14

CPC分类号： C07D205/08 ,  C07D401/06 ,  C07D401/14 ,  C07D403/06 ,  C07D405/14 ,  C07D409/06 ,  C07D417/06 ,  C07D417/14

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

公开(公告)号：US20240287004A1

公开(公告)日：2024-08-29

申请号：US18411842

申请日：2024-01-12

申请人： Cornell University

发明人： Joseph P. Vacca ,  Sarah Elizabeth Bettigole

IPC分类号： C07D239/42 ,  C07D213/76 ,  C07D401/06 ,  C07D403/06

CPC分类号： C07D239/42 ,  C07D213/76 ,  C07D401/06 ,  C07D403/06

摘要： Provided herein are small molecule inhibitors for the targeting or IRE1 protein family members. Binding may be direct or indirect. Further provided herein are methods of using IRE1 small molecule inhibitors for use in treating or ameliorating cancer in a subject. Moreover, IRE1 small molecule inhibitors described herein are for the treatment of cancer, where the cancer is a solid or hematologic cancer.

公开(公告)号：US20240270736A1

公开(公告)日：2024-08-15

申请号：US18521254

申请日：2023-11-28

申请人： Kumquat Biosciences Inc.

发明人： Baogen Wu ,  Liansheng Li ,  Pingda Ren ,  Zhiyong Chen ,  Siling Zhao ,  Xiuwen Zhu

IPC分类号： C07D417/12 ,  A61K45/06 ,  C07C235/88 ,  C07D207/16 ,  C07D209/18 ,  C07D241/44 ,  C07D401/04 ,  C07D403/06 ,  C07D493/06

CPC分类号： C07D417/12 ,  A61K45/06 ,  C07C235/88 ,  C07D207/16 ,  C07D209/18 ,  C07D241/44 ,  C07D401/04 ,  C07D403/06 ,  C07D493/06

摘要： The present disclosure provides compounds and pharmaceutically acceptable salts thereof, and methods of using the same. The compounds and methods have a range of utilities as therapeutics, diagnostics, and research tools. In particular, the subject compositions and methods are useful for reducing signaling output of oncogenic proteins.

公开(公告)号：US12043621B2

公开(公告)日：2024-07-23

申请号：US17206542

申请日：2021-03-19

申请人： Trustees of Boston University ,  Massachusetts Institute of Technology

发明人： Arturo Vegas ,  Sean Quinnell ,  Daniel Sheehy ,  Kelly Tan ,  Luke Ceo ,  Stephen Thomas Nestor ,  Angela Nicole Koehler ,  Becky Leifer ,  Shelby Doyle

IPC分类号： C07D471/14 ,  A61K45/06 ,  C07D207/09 ,  C07D211/96 ,  C07D213/85 ,  C07D401/04 ,  C07D401/10 ,  C07D401/14 ,  C07D403/06 ,  C07D403/12 ,  C07D405/04 ,  C07D409/04 ,  C07D417/06 ,  C07D417/14 ,  C07D471/04 ,  C07D495/04 ,  C07K16/28

CPC分类号： C07D417/14 ,  A61K45/06 ,  C07D207/09 ,  C07D211/96 ,  C07D213/85 ,  C07D401/04 ,  C07D401/10 ,  C07D401/14 ,  C07D403/06 ,  C07D403/12 ,  C07D405/04 ,  C07D409/04 ,  C07D417/06 ,  C07D471/04 ,  C07D495/04 ,  C07K16/2866

摘要： The technology described herein is directed to IL-4 and/or IL-13 inhibitors and uses thereof.

公开(公告)号：US20240239776A1

公开(公告)日：2024-07-18

申请号：US18530758

申请日：2023-12-06

申请人： Janssen Pharmaceutica NV

发明人： Jesus Alcazar ,  Michael K. Ameriks ,  Cynthia B. Berry ,  Pablo Garcia-Reynaga ,  Andrew V. Samant ,  J. A. Vega-Ramiro

IPC分类号： C07D413/06 ,  C07D401/06 ,  C07D401/14 ,  C07D403/06 ,  C07D413/14

CPC分类号： C07D413/06 ,  C07D401/06 ,  C07D401/14 ,  C07D403/06 ,  C07D413/14

摘要： Azaspirocycle compounds of Formula (I), and pharmaceutically acceptable salts, isotopes, N-oxides, solvates, and stereoisomers thereof, pharmaceutical compositions containing them, methods of making them, and methods of using them including methods for treating disease states, disorders, and conditions associated with MGL modulation, such as those associated with pain, psychiatric disorders, neurological disorders (including, but not limited to major depressive disorder, treatment resistant depression, anxious depression, autism spectrum disorders, Asperger syndrome, bipolar disorder), cancers and eye conditions:






wherein X, R1, R2, R2b, R3, m, n, o, and p are defined herein.

公开(公告)号：US20240239746A1

公开(公告)日：2024-07-18

申请号：US18288309

申请日：2022-04-19

申请人： SUNSHINE LAKE PHARMA CO., LTD.

发明人： Jiancheng WANG ,  Yingxun ZHANG ,  Chuanwen YANG ,  Qiao ZONG ,  Facheng MA ,  Xiaohong DING ,  Xiaojun WANG

IPC分类号： C07D207/34 ,  C07D403/06 ,  C12N9/18 ,  C12P13/02

CPC分类号： C07D207/34 ,  C07D403/06 ,  C12N9/18 ,  C12P13/02 ,  C12Y301/01

摘要： A preparation method for a pyrrole amide compound, as shown in formula (II). The preparation method includes: reacting a compound of formula (III) with a compound of formula (IV) in the presence of a palladium catalyst and a ligand, wherein X is Br or I; R is H, D, F, Cl, Br, C1-4 alkyl, C1-4 alkoxy, C1-4 haloalkyl or C1-4 haloalkoxy; and PG1 is benzyl or substituted benzyl.