Abstract: Compounds of Formula I or a stereoisomer, tautomer, prodrug or pharmaceutically acceptable salt thereof are provided, which are useful for the treatment of hyperproliferative diseases. Methods of using compounds of Formula I or a stereoisomer, tautomer, prodrug or pharmaceutically acceptable salt thereof, for in vitro, in situ, and in vivo diagnosis, prevention or treatment of such disorders in mammalian cells, or associated pathological conditions are disclosed.
Type:
Grant
Filed:
March 31, 2020
Date of Patent:
April 25, 2023
Assignee:
Array BioPharma Inc.
Inventors:
James F. Blake, Mark Laurence Boys, Mark Joseph Chicarelli, Adam W. Cook, Mohamed S. A. Elsayed, Jay Bradford Fell, John P. Fischer, Ronald Jay Hinklin, Yutong Jiang, Oren T. McNulty, Macedonio J. Mejia, Martha E. Rodriguez, Christina E. Wong
Abstract: The present disclosure is directed to a method of combatting opioid dependence in a subject experiencing a depressive episode. The method comprises treating the subject with an opioid agonist whilst managing their depression or depressive disorder using a step-wise interactive process, particularly where the process involves virtual cognitive behavioral therapy comprising a program for self-treatment. The self-treatment program could be embodied as a mobile medical application.
Abstract: The invention provides methods for treating triple negative breast cancer (TNBC), by co-administration of a BET bromodomain inhibitor selected from 1-benzyl-6-(3,5-dimethylisoxazol-4-yl)-N-methyl-1H-imidazo[4,5-b]pyridin-2-amine (Compound I), 1-benzyl-6-(3,5-dimethylisoxazol-4-yl)-1H-imidazo[4,5-b]pyridin-2-amine, and pharmaceutically acceptable salts/co-crystals thereof, and a second therapeutic agent to a subject in need thereof. The second therapeutic agent can be a PARP inhibitor, such as, e.g., talazoparib, olaparib or veliparib.
Type:
Grant
Filed:
September 13, 2019
Date of Patent:
March 21, 2023
Assignee:
Zenith Epigenetics Ltd.
Inventors:
Eric Campeau, Laura Tsujikawa, Sanjay Lakhotia
Abstract: A compound of formula (I): EAG-EDG-EAG?? (I) wherein each EAG is an electron accepting group; and EDG is an electron-donating group of formula (IIa): The compound of formula (I) may be used in a photosensitive layer of an organic photodetector wherein the photosensitive layer comprises the compound of formula (I) and an electron donor. A photosensor may comprise the organic photodetector and a light source, e.g. a near infra-red light source.
Abstract: This disclosure relates to JAK1 pathway inhibitors and the use thereof in treating gastrointestinal diseases or disorders such as ulcerative colitis.
Type:
Grant
Filed:
December 19, 2019
Date of Patent:
March 7, 2023
Assignee:
Incyte Corporation
Inventors:
Krishnaswamy Yeleswaram, Paul Smith, Gregory F. Hollis
Abstract: The present invention relates to a novel phosphor-tetrazine and a use thereof and, more particularly, provides a novel compound having high fluorescence amplification efficiency in various wavelength ranges by using a compound having a novel core skeleton called tert-butyl (3-(7-(6-methyl-1,2,4,5-tetrazin-3-yl)-3-oxo-9-phenyl-1H-pyrrolo[3,4-b]indolizin-2(3H)-yl)propyl)carbamate.
Type:
Grant
Filed:
May 31, 2018
Date of Patent:
February 21, 2023
Assignees:
Spark Biopharma, Inc., Seoul National University R&DB Foundation
Abstract: The present invention provides compounds which bind to the ubiquitously expressed E3 ligase protein cereblon (CRBN) and their use for the treatment of abnormal cellular proliferation. The present invention also provides compounds that may be used as synthetic intermediates in the synthesis of bifunctional compounds used for targeted protein degradation.
Type:
Grant
Filed:
October 16, 2020
Date of Patent:
February 21, 2023
Assignee:
C4 Therapeutics, Inc.
Inventors:
Christopher G. Nasveschuk, Fabian Dey, Annick Goergler, Bernd Kuhn, Roger Norcross, Stephan Roever, Philipp Schmid
Abstract: The present disclosure provides, inter alia, compounds with MASP-2 inhibitory activity, compositions of such compounds and methods of making and using such compounds.
Type:
Grant
Filed:
May 29, 2019
Date of Patent:
February 21, 2023
Assignee:
OMEROS CORPORATION
Inventors:
Neil S. Cutshall, Jennifer Lynn Gage, Franz A. Gruswitz, Juhienah Khalaf, Thomas L. Little, Markus Metz, Jeremiah H. Nguyen, Peter Kurt Nollert von Specht, Jennifer Tsoung, Michael Cicirelli, Sara Rebecca Goldstein, Santosh Kumar Keshipeddy, Do Yeon Kwon, Robert Huerta Lemus, Sudheer Babu Vaddela
Abstract: An organic light-emitting material contains a 6-silyl-substituted isoquinoline ligand. The organic light-emitting material is a metal complex containing a 6-silyl-substituted isoquinoline ligand and may be used as a light-emitting material in a light-emitting layer of an organic electroluminescent device. These new complexes can provide redder and saturated emission and meanwhile demonstrate a significantly improved lifetime and efficient and excellent device performance. Further disclosed are an electroluminescent device and a compound formulation including the metal complex.
Abstract: Methods of treating patients diagnosed with cancer harboring an IDH-1 mutation are provided, including the therapeutic administration of a certain inhibitor of a mutant IDH-1 as a single agent, or in combination with azacitidine (AZA).
Type:
Grant
Filed:
May 16, 2019
Date of Patent:
February 14, 2023
Assignee:
FORMA Therapeutics, Inc.
Inventors:
Patrick F. Kelly, Alan Collis, Jeff Davis, Duncan Walker, Susan Ashwell, Blythe Thomson, Wei Lu
Abstract: Disclosed herein are kinase inhibitory compounds, such as a receptor-interacting protein-1 (RIP1) kinase inhibitor compounds, as well as pharmaceutical compositions and combinations comprising such inhibitory compounds. The compounds may have a structure according to Formula I The disclosed compounds, pharmaceutical compositions, and/or combinations may be used to treat or prevent a kinase-associated disease or condition, particularly a RIP1-associated disease or condition.
Type:
Grant
Filed:
November 6, 2020
Date of Patent:
February 14, 2023
Assignee:
Rigel Pharmaceuticals, Inc.
Inventors:
Yan Chen, Jiaxin Yu, Simon Shaw, Ihab Darwish, Vanessa Taylor, Somasekhar Bhamidipati, Zhushou Luo, Rao Kolluri
Abstract: Disclosed are compounds having potency in the modulation of NMDA receptor activity. Such compounds can be used in the treatment of conditions such as depression and related disorders as well as other disorders.
Abstract: Isoquinoline compounds for treating various diseases and pathologies are disclosed. More particularly, the present invention concerns the use of an isoquinoline compound or analogs thereof, in the treatment of disorders characterized by the activation of Wnt pathway signaling (e.g., cancer, abnormal cellular proliferation, angiogenesis, fibrotic disorders, bone or cartilage diseases, and osteoarthritis), the modulation of cellular events mediated by Wnt pathway signaling, as well as genetic diseases and neurological conditions/disorders/diseases due to mutations or dysregulation of the Wnt pathway and/or of one or more of Wnt signaling components. Also provided are methods for treating Wnt-related disease states.
Type:
Grant
Filed:
January 22, 2021
Date of Patent:
January 10, 2023
Assignee:
BioSplice Therapeutics, Inc.
Inventors:
Sunil Kumar KC, Chi Ching Mak, Brian Walter Eastman, Jianguo Cao, Venkataiah Bollu, Gopi Kumar Mittapalli, Chandramouli Chiruta
Abstract: The present invention describes the use of a 5HT3-antagonist, in combination with a 6-propylamino-4,5,6,7-tetrahydro-1,3-benzothiazole-2-amine, to reduce adverse effects and to facilitate the neuroprotective treatment of a patient suffering from a synucleinopathic disorder to enable a therapeutically effective 6-propylamino-4,5,6,7-tetrahydro-1,3-benzothiazole-2-amine daily dose without the dose-limiting adverse effects caused by pramipexole when administered alone.
Type:
Grant
Filed:
August 31, 2020
Date of Patent:
January 10, 2023
Assignee:
CHASE THERAPEUTICS CORPORATION
Inventors:
Thomas N. Chase, Kathleen E. Clarence-Smith
Abstract: Provided herein are methods of preparing a desired enantiomer 6-[amino(4-chlorophenyl)(1-methyl-1H-imidazol-5-yl) methyl]-4-(3-chlorophenyl)-1-methyl-2(1H)-quinolinone, otherwise known as tipifarnib.
Abstract: The disclosure is directed to crystalline forms and mixtures thereof of R-fasoracetam. Such crystalline forms include Form II monohydrate R-fasoracetam and the anhydrate form of R-fasoracetam. The disclosure further includes mixtures of the anhydrate form of R-fasoracetam together with one or more of Form I monohydrate R-fasoracetam and Form II monohydrate R-fasoracetam.
Abstract: Disclosed herein is a pharmaceutical combination for use in the prevention, delay of progression or treatment of cancer, wherein the pharmaceutical combination exhibits a synergistic efficacy. The pharmaceutical combination comprises a humanized antagonist monoclonal antibody against PD- and a RAF inhibitor. Also disclosed herein is a combination for use in the prevention, delay of progression or treatment of cancer in a subject, comprising administering to the subject a therapeutically effective amount of a humanized antagonist monoclonal antibody against PD-1 and a therapeutically effective amount of a RAF inhibitor.
Type:
Grant
Filed:
November 16, 2020
Date of Patent:
December 27, 2022
Assignee:
BEIGENE SWITZERLAND GMBH
Inventors:
Jing Song, Lai Wang, Kang Li, Tong Zhang, Lusong Luo, Min Wei, Zhiyu Tang, Guoliang Zhang, Changyou Zhou
Abstract: The present disclosure provides for compounds according to Formula I or Formula II and their pharmaceutically acceptable salts, stereoisomers, and/or tautomers thereof. Also provided are pharmaceutical compositions and the compounds of formulae I and II for use in methods of treating cancers, via inhibition of MAT2A, including some cancers in which the gene encoding methylthioadenosine phosphorylase (MTAP) is deleted and/or not fully functioning.
Type:
Grant
Filed:
March 28, 2019
Date of Patent:
December 13, 2022
Assignee:
SERVIER PHARMACEUTICALS LLC
Inventors:
Zenon D. Konteatis, Mingzong Li, Peng Liu, Matthew Medeiros, Samuel K. Reznik, Zhihua Sui, Jeremy M. Travins, Janeta Popovici-Muller, Shubao Zhou, Guangning Ma
Abstract: The present invention provides compounds of Formula (I) useful as inhibitors of PAD4, compositions thereof, and methods of treating PAD4-related disorders, wherein each of Ring A, L, Q, R1, R2, R3, R4, R7, and R8 along with other variables are as defined herein.
Type:
Grant
Filed:
August 7, 2019
Date of Patent:
December 13, 2022
Assignee:
Bristol-Myers Squibb Company
Inventors:
Anurag S. Srivastava, Robert J. Cherney, Khehyong Ngu