公开(公告)号：US20240352017A1

公开(公告)日：2024-10-24

申请号：US18758953

申请日：2024-06-28

申请人： K36 Therapeutics, Inc.

发明人： Terrence Joseph Connolly ,  Chad Arthur Lewis

IPC分类号： C07D473/34 ,  A61K31/52 ,  C07B59/00

CPC分类号： C07D473/34 ,  A61K31/52 ,  C07B59/002

摘要： The invention provides deuterium-enriched piperidinyl-methyl-purine amines and related compounds, pharmaceutical compositions, their use for inhibiting NSD2, and their use in the treatment of a disease or condition, such as cancer.

公开(公告)号：US12065459B2

公开(公告)日：2024-08-20

申请号：US16672114

申请日：2019-11-01

申请人： Achillion Pharmaceuticals, Inc.

发明人： Jason Allan Wiles ,  Venkat Rao Gadhachanda ,  Qiuping Wang ,  Godwin Pais ,  Akihiro Hashimoto ,  Dawei Chen ,  Xiangzhu Wang ,  Atul Agarwal ,  Milind Deshpande ,  Avinash S. Phadke

IPC分类号： C07F9/572 ,  A61K9/00 ,  A61K31/404 ,  A61K31/4045 ,  A61K31/407 ,  A61K31/4162 ,  A61K31/4178 ,  A61K31/4184 ,  A61K31/4188 ,  A61K31/4192 ,  A61K31/437 ,  A61K31/4439 ,  A61K31/444 ,  A61K31/4709 ,  A61K31/496 ,  A61K31/501 ,  A61K31/506 ,  A61K31/519 ,  A61K31/549 ,  A61K31/55 ,  A61K31/675 ,  A61K31/683 ,  C07B59/00 ,  C07D209/12 ,  C07D209/14 ,  C07D209/30 ,  C07D209/40 ,  C07D209/42 ,  C07D209/44 ,  C07D209/88 ,  C07D401/14 ,  C07D403/06 ,  C07D403/08 ,  C07D403/12 ,  C07D403/14 ,  C07D405/12 ,  C07D405/14 ,  C07D413/06 ,  C07D413/14 ,  C07D417/06 ,  C07D417/12 ,  C07D417/14 ,  C07D471/04 ,  C07D471/08 ,  C07D487/04 ,  C07D487/14 ,  C07D491/113 ,  C07D495/04 ,  C07D513/04 ,  C07F5/02 ,  C07F7/08 ,  C07F9/6558 ,  C07F9/6561

CPC分类号： C07F9/5728 ,  A61K9/0014 ,  A61K9/0019 ,  A61K9/0048 ,  A61K9/0053 ,  A61K31/404 ,  A61K31/4045 ,  A61K31/407 ,  A61K31/4162 ,  A61K31/4178 ,  A61K31/4184 ,  A61K31/4188 ,  A61K31/4192 ,  A61K31/437 ,  A61K31/4439 ,  A61K31/444 ,  A61K31/4709 ,  A61K31/496 ,  A61K31/501 ,  A61K31/506 ,  A61K31/519 ,  A61K31/549 ,  A61K31/55 ,  A61K31/675 ,  A61K31/683 ,  C07B59/002 ,  C07D209/12 ,  C07D209/14 ,  C07D209/30 ,  C07D209/40 ,  C07D209/42 ,  C07D209/44 ,  C07D209/88 ,  C07D401/14 ,  C07D403/06 ,  C07D403/08 ,  C07D403/12 ,  C07D403/14 ,  C07D405/12 ,  C07D405/14 ,  C07D413/06 ,  C07D413/14 ,  C07D417/06 ,  C07D417/12 ,  C07D417/14 ,  C07D471/04 ,  C07D471/08 ,  C07D487/04 ,  C07D487/14 ,  C07D491/113 ,  C07D495/04 ,  C07D513/04 ,  C07F5/025 ,  C07F5/027 ,  C07F7/0812 ,  C07F9/65583 ,  C07F9/6561 ,  C07F9/65616 ,  C07B2200/05

摘要： Compounds, methods of use, and processes for making inhibitors of complement factor D comprising Formula I, or a pharmaceutically acceptable salt or composition thereof wherein R12 or R13 on the A group is an aryl, heteroaryl or heterocycle (R32) are provided. The inhibitors described herein target factor D and inhibit or regulate the complement cascade at an early and essential point in the alternative complement pathway, and reduce factor D's ability to modulate the classical and lectin complement pathways. The inhibitors of factor D described herein are capable of reducing the excessive activation of complement, which has been linked to certain autoimmune, inflammatory, and neurodegenerative diseases, as well as ischemia-reperfusion injury and cancer.

公开(公告)号：US20240270741A1

公开(公告)日：2024-08-15

申请号：US18408088

申请日：2024-01-09

申请人： Cogent Biosciences, Inc.

发明人： Jay Bradford Fell ,  John E. Robinson ,  John P. Fischer ,  Logan E. Vine ,  Martha E. Rodriguez ,  Jennifer Fulton ,  Tanna Bettendorf ,  Bradley J. Newhouse ,  Robert A. Rieger ,  Cori A. Malinky ,  Aaron Christopher Smith ,  Toya D. Scaggs ,  Joshua Dahlke ,  Ravi Kumar Jalluri ,  Mark Joseph Chicarelli ,  Leah J. Salituro ,  Macedonio J. Mejia ,  Payal Chatterjee

IPC分类号： C07D471/04 ,  A61K31/437 ,  A61K31/438 ,  A61K31/439 ,  A61K31/4545 ,  A61K31/496 ,  A61K31/4985 ,  A61K31/506 ,  A61K31/5377 ,  A61K31/541 ,  A61K31/661 ,  C07B59/00 ,  C07D519/00 ,  C07F9/6561

CPC分类号： C07D471/04 ,  A61K31/437 ,  A61K31/438 ,  A61K31/439 ,  A61K31/4545 ,  A61K31/496 ,  A61K31/4985 ,  A61K31/506 ,  A61K31/5377 ,  A61K31/541 ,  A61K31/661 ,  C07B59/002 ,  C07D519/00 ,  C07F9/6561 ,  C07B2200/05

摘要： A compound having the following structure of Formula (I):




or a stereoisomer, salt, or tautomer thereof, wherein R1, R2, R5, A, B, X, and Y are as defined herein. Pharmaceutical composition comprising the compounds, and their use in methods of treating diseases are also described.

公开(公告)号：US12054463B2

公开(公告)日：2024-08-06

申请号：US16646630

申请日：2018-10-30

申请人： The Trustees of Columbia University in the City of New York

发明人： Dileep Kumar ,  J. John Mann ,  Akiva Mintz ,  Kiran Kumar Solingapuram Sai

IPC分类号： C07D239/94 ,  A61K51/04 ,  C07B59/00 ,  C07D401/04 ,  C07D401/12 ,  C07D403/04 ,  C07D471/04 ,  C07D487/04 ,  C07D491/04

CPC分类号： C07D239/94 ,  A61K51/0459 ,  C07B59/002 ,  C07D401/04 ,  C07D401/12 ,  C07D403/04 ,  C07D471/04 ,  C07D487/04 ,  C07D491/04

摘要： The present disclosure relates to radiolabeled compounds and methods of uses for diagnosis, monitoring, and treatment of various degenerative neurological disorders, neuropsychiatric disorders, brain injuries, vascular diseases, and cancers. Radiolabled compounds for imaging of microtubules or microtubules and other targets using positron-emission tomography (PET) are specifically disclosed.

公开(公告)号：US12054458B2

公开(公告)日：2024-08-06

申请号：US18186043

申请日：2023-03-17

申请人： DEUTSCHES KREBSFORSCHUNGSZENTRUM ,  RUPRECHT-KARLS-UNIVERSITAET HEIDELBERG

发明人： Jens Cardinale ,  Martin Schaefer ,  Klaus Kopka ,  Matthias Eder ,  Ulrike Bauder-Wuest ,  Michael Eisenhut ,  Martina Benesova ,  Uwe Haberkorn ,  Frederik L. Giesel

IPC分类号： C07D213/61 ,  A61K38/00 ,  A61K51/04 ,  A61P35/00 ,  C07B59/00 ,  C07K7/02 ,  G01N33/574

CPC分类号： C07D213/61 ,  A61K51/04 ,  A61K51/0455 ,  A61P35/00 ,  C07B59/002 ,  C07K7/02 ,  G01N33/57434 ,  A61K38/00 ,  C07B2200/05

摘要： The present invention generally relates to the field of radiopharmaceuticals and their use in nuclear medicine as tracers and imaging agents for various disease states of prostate cancer.

公开(公告)号：US12012394B2

公开(公告)日：2024-06-18

申请号：US16277643

申请日：2019-02-15

申请人： Washington University

发明人： Zhude Tu ,  Paul T. Kotzbauer ,  Xuyi Yue ,  Dhruva D. Dhavale

IPC分类号： C07D401/12 ,  C07B59/00 ,  C07D405/12 ,  A61K51/04

CPC分类号： C07D401/12 ,  C07B59/002 ,  C07D405/12 ,  A61K51/0455 ,  A61K2123/00 ,  C07B2200/05

摘要： The present invention generally relates to various compounds that are useful as α-synuclein ligands. The invention further relates to methods of using these compounds and their radiolabeled analogs for the detection of synucleinopathies, including Parkinson's disease (PD).

公开(公告)号：US20240189460A1

公开(公告)日：2024-06-13

申请号：US18474218

申请日：2023-09-25

申请人： Nuclidium AG ,  University of Basel

发明人： Leila JAAFAR-THIEL ,  Melpomeni FANI ,  Jacopo MILLUL ,  Francesco DE ROSE

IPC分类号： A61K51/08 ,  A61K51/04 ,  C07B59/00

CPC分类号： A61K51/083 ,  A61K51/0482 ,  C07B59/002 ,  A61K2123/00 ,  C07B2200/05

摘要： The present disclosure relates to the field of nuclear imaging and therapy, and more specifically to high purity copper radiotracer compositions useful in imaging, such as positron emission tomography (PET) and single-photon emission computerized tomography (SPECT), and therapy. More specifically, the present disclosure relates to novel compositions useful in imaging and treatment of conditions such as prostate cancer, somatostatin receptor-expressing tumors, like neuroendocrine tumor, epithelial tumors, as well as to methods wherein such compositions are prepared.

公开(公告)号：US20240100199A1

公开(公告)日：2024-03-28

申请号：US18352435

申请日：2023-07-14

申请人： Lantheus Medical Imaging, Inc.

发明人： Richard R. Cesati ,  Heike S. Radeke ,  Suresh K. Pandey ,  Ajay Purohit ,  Simon P. Robinson

IPC分类号： A61K51/04 ,  C07D311/56 ,  C07D401/12 ,  C07D237/14 ,  C07D237/16 ,  C07B59/00 ,  C07F7/08 ,  A61K49/00 ,  B01J19/24 ,  C07D237/04 ,  C07D403/12 ,  C07F7/12

CPC分类号： A61K51/0459 ,  C07D311/56 ,  C07D401/12 ,  C07D237/14 ,  C07D237/16 ,  C07B59/002 ,  C07F7/0812 ,  A61K49/0004 ,  B01J19/24 ,  C07D237/04 ,  C07D403/12 ,  C07F7/12 ,  B01J2219/24 ,  C07B2200/05

摘要： The present invention provides compounds with imaging moieties for imaging a subject. The present invention also relates to systems, compositions, and methods for the synthesis and use of imaging agents, or precursors thereof. An imaging agent precursor may be converted to an imaging agent using the methods described herein. In some cases, a composition or plurality of imaging agents is enriched in 18F. In some cases, an imaging agent may be used to image an area of interest in a subject, including, but not limited to, the heart, cardiovascular system, cardiac vessels, brain, and other organs.

公开(公告)号：US20240093265A1

公开(公告)日：2024-03-21

申请号：US17942555

申请日：2022-09-12

申请人： Concert Pharmaceuticals, Inc.

发明人： Roger Tung

IPC分类号： C12Q1/28 ,  A61K31/195 ,  A61K31/4709 ,  A61K31/485 ,  A61K31/49 ,  C07B59/00 ,  C07D221/28 ,  C07D471/08 ,  G01N33/49 ,  G01N33/493

CPC分类号： C12Q1/28 ,  A61K31/195 ,  A61K31/4709 ,  A61K31/485 ,  A61K31/49 ,  C07B59/002 ,  C07D221/28 ,  C07D471/08 ,  G01N33/491 ,  G01N33/493

摘要： This disclosure relates to novel morphinan compounds and their derivatives, pharmaceutically acceptable salts, solvates, and hydrates thereof. This disclosure also provides compositions comprising a compound of this disclosure and the use of such compositions in methods of treating diseases and conditions that are beneficially treated by administering a σ1 receptor agonist that also has NMDA antagonist activity.

公开(公告)号：US20240092766A1

公开(公告)日：2024-03-21

申请号：US18108053

申请日：2023-02-10

申请人： Vertex Pharmaceuticals Incorporated

发明人： Sara S. HADIDA RUAH ,  Peter D.J. GROOTENHUIS ,  Fredrick VAN GOOR ,  Jinglan ZHOU ,  Brian BEAR ,  Mark T. MILLER ,  Jason McCARTNEY ,  Mehdi Michel Jamel NUMA ,  Xiaoqing YANG

IPC分类号： C07D405/12 ,  C07D471/04 ,  A61K31/445 ,  A61K31/496 ,  A61K31/5377 ,  C07D405/14 ,  C07D403/12 ,  G01N33/50 ,  G01N33/68 ,  C07B59/00 ,  C07D487/04

CPC分类号： C07D405/12 ,  C07D471/04 ,  A61K31/445 ,  A61K31/496 ,  A61K31/5377 ,  C07D405/14 ,  C07D403/12 ,  G01N33/5008 ,  G01N33/6872 ,  C07B59/002 ,  C07D487/04 ,  G01N2333/705 ,  G01N2500/02 ,  G01N2500/10 ,  C07B2200/05

摘要： Compounds of the present invention and pharmaceutically acceptable compositions thereof, are useful as modulators of ATP-Binding Cassette (“ABC”) transporters or fragments thereof, including Cystic Fibrosis Transmembrane Conductance Regulator (“CFTR”). The present invention also relates to methods of treating ABC transporter mediated diseases using compounds of the present invention.