Abstract: Provided are embodiments of para-substituted 1,1-dialkyl-4-phenylpiperazin-1-ium iodides advantageous for modulating inflammation that have been synthesized and their electrophysiology activities for ?9, ?9?10, and ?7 nAChRs compared. The para position contained alkyl or aryl amides, or heterocyclic isosteres for the amide, and the alkyl groups were varied at the ammonium piperazine nitrogen to see if compensatory changes in size at this position of the molecule impacted function. The compounds were characterized with two-electrode voltage-clamp measurements on Xenopus oocytes expressing nAChRs. General, the compounds were more potent for ?9-containing receptors than for ?7, and the majority were either full or strong partial agonists for ?9-containing nAChR.
Type:
Grant
Filed:
September 6, 2022
Date of Patent:
January 30, 2024
Assignee:
University of Florida Research Foundation, Inc.
Inventors:
Nicole Alana Horenstein, Roger Lee Papke, Hina Andleeb
Abstract: Provided herein are small molecule inhibitors of ASH1L activity and small molecules that facilitate ASH1L degradation and methods of use thereof for the treatment of disease, including acute leukemia, solid cancers and other diseases dependent on activity of ASH1L.
Type:
Grant
Filed:
May 12, 2017
Date of Patent:
January 30, 2024
Assignee:
The Regents of the University of Michigan
Inventors:
Jolanta Grembecka, Tomasz Cierpicki, David Rogawski, Dmitry Borkin, Szymon Klossowski, Zhuang Jin, Deanna Montgomery, Jing Deng, Marta Krotoska, Hao Li
Abstract: The present disclosure relates to a novel compound or a salt thereof, a composition for detecting cysteine, a fluorescent probe, and a composition for diagnosing cancer, which contain the same, a method for detecting cysteine, a method for providing information for diagnosing cancer, and a method for producing the novel compound. According to the present disclosure, there may be provided a method of synthesizing and purifying a fluorescent probe for cysteine detection and applying the same to diagnose cervical cancer by detecting cysteine in human urine.
Type:
Grant
Filed:
October 28, 2021
Date of Patent:
January 30, 2024
Inventors:
Do Kyoung Kim, Chang Wook Jeong, Jong Min An
Abstract: The present disclosure relates to HIF-1? prolyl hydroxylase inhibitors, compositions which comprise the HIF-1? prolyl hydroxylase inhibitors described herein and to methods for controlling, inter alia, Peripheral Vascular Disease (PVD), Coronary Artery Disease (CAD), heart failure, ischemia, and anemia.
Type:
Grant
Filed:
July 27, 2022
Date of Patent:
January 30, 2024
Assignee:
Akebia Therapeutics, Inc.
Inventors:
Richard Masaru Kawamoto, Shengde Wu, Artem G. Evdokimov, Kenneth D Greis, Angelique Sun Boyer, Namal C. Warshakoon
Abstract: The present invention relates to reagents which are suitable to be used in mass spectrometry as well as methods of mass spectrometric determination of analyte molecules using said reagents.
Type:
Grant
Filed:
January 21, 2021
Date of Patent:
January 30, 2024
Assignee:
Roche Diagnostics Operations, Inc.
Inventors:
Dieter Heindl, Hans-Peter Josel, Uwe Kobold, Christoph Seidel, Martin Rempt, Andreas Leinenbach, Giuseppe Prencipe, Silvia Baecher, Simon Ferdinand Loibl, Anna-Skrollan Geiermann, Jelena Milic, Nicole Pirkl
Abstract: This invention relates to novel compounds and pharmaceutical compositions comprising. Compounds of the invention useful as modulators of Rho-associated protein kinase (ROCK), for example ROCK1 and/or ROCK2 inhibitors. Methods of treatment employing the compounds are also contemplated by the present invention. The compounds of the invention are useful in treating ROCK mediated diseases.
Type:
Grant
Filed:
August 26, 2022
Date of Patent:
January 23, 2024
Assignee:
Redx Pharma PLC
Inventors:
Clifford D. Jones, Peter Bunyard, Gary Pitt, Liam Byrne, Thomas Pesnot, Nicolas E. S. Guisot
Abstract: The invention provides compositions and methods for intrathecal administration of the compound MCOPPB or a pharmaceutically acceptable salt thereof for treating pain, such as neuropathic pain suffered by an adult human.
Type:
Grant
Filed:
May 24, 2021
Date of Patent:
January 16, 2024
Assignee:
Centrexion Therapeutics Corporation
Inventors:
James N. Campbell, Barton Harley Manning
Abstract: The present application belongs to the field of medicine. In particular, the present application relates to a diarylthiohydantoin compound as an androgen receptor antagonist or a pharmaceutically acceptable salt thereof, a preparation method of the same, a pharmaceutical composition comprising the compound, and a use thereof in treating a cell proliferative disease mediated by androgen. The compound of the present application has good antagonistic effect on androgen receptor and exhibits excellent antitumor effect.
Type:
Grant
Filed:
October 15, 2021
Date of Patent:
January 9, 2024
Assignee:
CHIA TAI TIANQING PHARMACEUTICAL GROUP CO., LTD.
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.
Type:
Grant
Filed:
November 9, 2022
Date of Patent:
January 2, 2024
Assignee:
Enanta Pharmaceuticals, Inc.
Inventors:
Joseph D. Panarese, Samuel Bartlett, Guoqiang Wang, Yat Sun Or
Abstract: Disclosed are novel compounds that accumulate in Gram-negative bacteria. Also disclosed are method of antimicrobial treatment using the compounds.
Type:
Grant
Filed:
May 3, 2021
Date of Patent:
January 2, 2024
Assignee:
The Board of Trustees of the University of Illinois
Inventors:
Paul J. Hergenrother, Michelle Richter, Andrew Riley, Bryon S. Drown, Martin Chavez, Sarah Tasker, Alfredo Garcia
Abstract: The present invention provides tricyclic fused thiophene derivatives, as well as their compositions and methods of use, that modulate the activity of Janus kinase (JAK) and are useful in the treatment of diseases related to the activity of JAK including, for example, inflammatory disorders, autoimmune disorders, cancer, and other diseases.
Abstract: Described herein are small molecule splicing modulator compounds that modulate splicing of mRNA, such as pre-mRNA, encoded by genes, pharmaceutical compositions comprising the same, and methods of use of the small molecule splicing modulator compounds for modulating splicing and treating diseases and conditions.
Type:
Grant
Filed:
July 30, 2021
Date of Patent:
December 19, 2023
Assignee:
Skyhawk Therapeutics, Inc.
Inventors:
Michael Luzzio, Brian Lucas, Daniel Brian Horne, Tiansheng Wang
Abstract: The present application relates to compounds comprising an ester, a thioester, or a hydrazide moiety and methods of synthesizing these compounds. The present application also relates to pharmaceutical compositions containing the compounds and methods of treating cell proliferative disorders mediated by the Hedgehog (Hh) signaling pathway, such as cancer, by administering the compounds and pharmaceutical compositions to subjects in need thereof.
Abstract: Described herein are bisphosphonate quinolone compounds, conjugates and pharmaceutical formulations thereof that can include a bisphosphonate and a quinolone, where the quinolone can be releasably coupled to the bisphosphonate. Also provided herein are methods of making and methods of using the bisphosphonate quinolone compounds, conjugates and pharmaceutical formulations thereof.
Type:
Grant
Filed:
December 11, 2020
Date of Patent:
December 12, 2023
Assignees:
BIOVINC, LLC, UNIVERSITY OF SOUTHERN CALIFORNIA
Inventors:
Frank H. Ebetino, Shuting Sun, Mark W. Lundy, Charles E. McKenna, Eric Richard, Parish Sedghizadeh, Keivan Sadrerafi, Philip T. Cherian
Abstract: Disclosed is a compound of Formula I or a pharmaceutically acceptable salt thereof, preparation methods thereof, pharmaceutical composition comprising the same, and use thereof in the treatment of diseases such as pancreatic cancer.
Type:
Grant
Filed:
July 9, 2021
Date of Patent:
November 28, 2023
Assignee:
CHONGQING UNIVERSITY OF ARTS AND SCIENCES
Abstract: The invention relates to compounds of formula (I): or a salt or solvate thereof, wherein the variables are as described herein. Compounds of formula (I) and pharmaceutical compositions thereof are antagonists of toll-like receptors such as TLR7, TLR8 and/or TLR9 that are useful for inhibiting immune response and treating diseases associated with undesirable immune response.
Type:
Grant
Filed:
May 20, 2022
Date of Patent:
November 28, 2023
Assignee:
DYNAVAX TECHNOLOGIES CORPORATION
Inventors:
Albert Frederick Candia, III, Richard Thomas Beresis, Robert L. Coffman
Abstract: 2-((1r,4r)-4-(imidazo[4,5-d]pyrrolo[2,3-b]pyridin-1(6H)-yl)cyclohexyl)acetonitrile compounds, pharmaceutical compositions containing them, methods of making them, and methods of using them including methods for treating disease states, disorders, and conditions mediated by JAK, such as inflammatory bowel disease.
Type:
Grant
Filed:
March 16, 2021
Date of Patent:
November 28, 2023
Assignee:
Janssen Pharmaceutica NV
Inventors:
Genesis M. Bacani, Wenying Chai, Tatiana Koudriakova, Paul J. Krawczuk, Kevin D. Kreutter, Kristi Leonard, Michele C. Rizzolio, Mark Seierstad, Russell C. Smith, Mark S. Tichenor, Jennifer D. Venable, Aihua Wang
Abstract: A method of treating an ocular nerve injury in a subject in need thereof, the method comprising administering a therapeutically effective amount of baicalein or an analog thereof.
Type:
Grant
Filed:
February 9, 2022
Date of Patent:
November 28, 2023
Assignees:
THE HONG KONG POLYTECHNIC UNIVERSITY
Inventors:
Chi Wai Do, Chi ho To, Li Pan, Dongfeng Chen, Kin-Sang Cho