Abstract: The present invention relates to a ubiquitin-specific peptidase 24 inhibitor, a medicinal composition and a method of delaying or reversing multidrug resistance in cancers using the same. The USP24 inhibitor, which includes a shUSP24 RNA and/or a carbonyl substituted phenyl compound, can serve as a chemosensitizing agent for inhibiting the drug pump out, cancer stemness and genomic instability of cancer cells, thereby being applied to a medicinal composition and a method for delaying or reversing multidrug resistance in cancers.
Abstract: Disclosed herein are compounds of formula (I): and salts thereof. Also disclosed are compositions comprising compounds of formula I and compounds of formula I for use in treating or preventing bacterial infections.
Type:
Grant
Filed:
March 9, 2018
Date of Patent:
May 28, 2024
Assignee:
RUTGERS, THE STATE UNIVERSITY OF NEW JERSEY
Inventors:
Edmond J. LaVoie, Ajit Parhi, Yi Yuan, Yongzheng Zhang, Yangsheng Sun
Abstract: The present invention provides a compound of Formula (I) Formula (I) or the pharmaceutically acceptable salts thereof, which are PRMT5 inhibitors.
Type:
Grant
Filed:
August 5, 2019
Date of Patent:
May 28, 2024
Assignee:
Merck Sharp & Dohme LLC
Inventors:
David Witter, Shuhei Kawamura, Michelle Machacek, Ryan Quiroz, Michael H. Reutershan, Sebastian Schneider, Phieng Siliphaivanh, Yingchun Ye, Charles S. Yeung
Abstract: The present invention provides novel compounds having the general formula (I) wherein R1 to R6, and m are as described herein, compositions including the compounds and methods of using the compounds.
Type:
Grant
Filed:
October 17, 2019
Date of Patent:
May 28, 2024
Assignee:
Hoffmann-La Roche Inc.
Inventors:
Song Feng, Chungen Liang, Yongfu Liu, Xuefei Tan, Jun Wu, Jianping Wang
Abstract: The present disclosure provides compounds for the inhibition of soluble epoxide hydrolase and associate disease conditions, as well as a method of treating or preventing disorders in a subject by inhibition of soluble epoxide hydrolase.
Type:
Grant
Filed:
July 3, 2019
Date of Patent:
May 21, 2024
Assignee:
EicOsis, LLC
Inventors:
Bruce D. Hammock, Sung Hee Hwang, Karen M. Wagner, Cynthia B. McReynolds
Abstract: The present invention provides a novel compound for effectively preventing nerve damage and protecting nerves, and a preparation method thereof. Besides, the present invention also provides a pharmaceutical composition comprising the novel compound, and a use of the novel compound for preventing nerve damage and protecting nerves.
Abstract: Provided are aminopyridine compounds and pharmaceutically acceptable compositions thereof which exhibit inhibition activity against certain mutated forms of EGFR.
Type:
Grant
Filed:
August 26, 2022
Date of Patent:
May 14, 2024
Assignees:
Yuhan Corporation, Janssen Biotech, Inc.
Inventors:
Byoungmoon Lee, Hyunjoo Lee, Gyu Jin Lee, Su Bin Choi, Sol Park, Heejun Kim, Misong Kim, Young Ae Yoon, Kwan Hoon Hyun, Tae Kyun Kim, Jae Young Sim, Marian C. Bryan, Scott Kuduk, James Campbell Robertson
Abstract: The present application provides bicyclic amines of Formula (I): and their pharmaceutically acceptable salts thereof, that are inhibitors of cyclin-dependent kinase 2 (CDK2), as well as pharmaceutical compositions thereof, and methods of treating cancer using the same.
Type:
Grant
Filed:
December 9, 2022
Date of Patent:
May 7, 2024
Assignee:
Incyte Corporation
Inventors:
Joshua Hummel, David M. Burns, Ding-Quan Qian, Xiaozhao Wang
Abstract: Novel pyrazolo[1,5-c]pyrimidine compounds, a method of synthesizing said compounds, a pharmaceutical composition comprising said compounds and a suitable carrier, and a method of using the compounds. The pyrazolo[1,5-c]pyrimidine compounds, identified as CK2 inhibitors, are useful as anticancer and/or antitumor agents, and as agents for treating other kinase-associated conditions including inflammation, pain, and certain immunological disorders, and other types of diseases such as diabetes, viral infection, neurodegenerative diseases.
Abstract: The present invention relates to highly polarizable 3D organic perovskites of the general formula ABX3, prepared by introducing halogen functional groups in the A-site cation (in which the A and B sites are occupied by organic cations and the X site is a monovalent non-metallic counterion). The (DCl)(NH4)(BF4)3 crystal exhibits a strong linear electrooptic (EO) effect with an effective EO coefficient of 20 pmV?1, which is 10 times higher than that of metal halide perovskites. These 3D organic perovskites are solution processed and compatible with silicon, and illustrate the potential of rationally-designed all-organic perovskites for use in on-chip modulators, electro-optic devices, piezoelectric devices, or silicon photonics devices.
Type:
Grant
Filed:
September 1, 2021
Date of Patent:
April 30, 2024
Assignee:
HUAWEI TECHNOLOGIES CANADA CO., LTD.
Inventors:
Meng-Jia Sun, Chao Zheng, Sjoerd Hoogland, Edward Hartley Sargent
Abstract: The present disclosure relates to the use of cannabidiol (CBD) for the reduction of total convulsive seizure frequency in the treatment of “treatment-resistant epilepsy” (TRE). In particular, the disclosure relates to the use of CBD of treating TRE when the TRE is Dravet syndrome; myoclonic absence seizures or febrile infection related epilepsy syndrome (FIRES). The disclosure further relates to the use of CBD in combination with one or more anti-epileptic drugs (AEDs).
Type:
Grant
Filed:
May 19, 2023
Date of Patent:
April 23, 2024
Assignee:
GW Research Limited
Inventors:
Geoffrey Guy, Stephen Wright, Orrin Devinsky
Abstract: Compounds for treating cancer and, particularly, to compounds that are 5-(3-substituted phenyl)-pyrimido[4,5-d]pyrimidine-2,4,7(1H,3H,8H)-trione analogues and their use as anticancer agents.
Type:
Grant
Filed:
November 10, 2023
Date of Patent:
April 23, 2024
Assignee:
KING FAISAL UNIVERSITY
Inventors:
Katharigatta N. Venugopala, Pran Kishore Deb, Vinuta Kamat, Rangappa Santosh, Boja Poojary, Manohar S. Kugaji, Vijay M. Kumbar, Mohamed A. Morsy, Bandar Aldhubiab, Mahesh Attimarad, Anroop B. Nair, Nagaraja Sreeharsha
Abstract: Provided are compounds of Formula (I): or a pharmaceutically acceptable salt thereof, wherein X, R1, R2, and R3 are as defined herein. Also provided is a pharmaceutically acceptable composition comprising a compound of Formula (I), or a pharmaceutically acceptable salt thereof. Also provided are methods of using a compound of Formula (I), or a pharmaceutically acceptable salt thereof.
Abstract: Provided herein are compounds of the Formula (I): (I) and tautomers, stereoisomers and pharmaceutically acceptable salts and solvates thereof, wherein Rx, Ry, W, X, Y, Z, Ring A and (AA) have the meanings given in the specification, which are inhibitors of RET kinase and are useful in the treatment and prevention of diseases which can be treated with a RET kinase inhibitor, including RET-associated diseases and disorders.
Type:
Grant
Filed:
September 6, 2019
Date of Patent:
April 23, 2024
Assignee:
ARRAY BIOPHARMA INC.
Inventors:
James F. Blake, Donghua Dai, Julia Haas, Yutong Jiang, Dean Kahn, Gabrielle R. Kolakowski, Elizabeth A. McFaddin, Megan L McKenney, Andrew T. Metcalf, David A. Moreno, Brett Prigaro, Ginelle A. Ramann, Li Ren, Shane M. Walls, Hailong Zhang
Abstract: The present invention relates to novel compounds having a histone deacetylase 6 (HDAC6) inhibitory activity, optical isomers thereof or pharmaceutically acceptable salts thereof, a pharmaceutical use thereof, and a method for preparing the same. According to the present invention, the novel compounds, optical isomers thereof or pharmaceutically acceptable salts thereof have the histone deacetylase 6 (HDAC6) inhibitory activity, and are effective in preventing or treating HDAC6-related diseases, comprising infectious diseases; neoplasm; internal secretion; nutritional and metabolic diseases; mental and behavioral disorders; neurological diseases; eye and ocular adnexal diseases; circulatory diseases; respiratory diseases; digestive diseases; skin and subcutaneous tissue diseases; musculoskeletal system and connective tissue diseases; and teratosis or deformities, and chromosomal aberration.
Type:
Grant
Filed:
July 25, 2019
Date of Patent:
April 16, 2024
Assignee:
Chong Kun Dang Pharmaceutical Corp.
Inventors:
Chang Sik Lee, Jung Taek Oh, Hokeun Yun, Hyeseung Song, Hyunjin Michael Kim
Abstract: In one aspect, the disclosure relates to methods for preparation of terpene and terpene-like molecules. In a further aspect, the disclosure relates to the products of the disclosed methods, i.e., terpene and terpene-like molecules prepared using the disclosed methods. Intermediates for the synthesis of a wide variety of terpenoids are ?-allyl Knoevenagel adducts or quasi ?-allyl Knoevenagel adducts are disclosed. In various aspects, methods of preparing terpenoids through these intermediates are disclosed. The methods can comprise ?-alkylation of an allylic electrophile followed by ring-closure metathesis to a polycyclic terpenoid structure. In a further aspect, the disclosure pertains to terpenoid frameworks, and compounds prepared via disclosed oxidation and substitution reactions on the disclosed terpenoid frameworks. This abstract is intended as a scanning tool for purposes of searching in the particular art and is not intended to be limiting of the present disclosure.
Type:
Grant
Filed:
September 15, 2017
Date of Patent:
April 9, 2024
Assignee:
University of Florida Research Foundation, Inc.
Abstract: Substituted cyclohexyl chemical entities of Formula (I): wherein Ra, G, and Rb have any of the values described herein, and compositions comprising such chemical entities; methods of making them; and their use in a wide range of methods, including metabolic and reaction kinetic studies; detection and imaging techniques; radioactive therapies; modulating and treating disorders mediated by nociceptin activity or dopamine signaling; treating neurological disorders, neurodegenerative diseases, depression, and schizophrenia; enhancing the efficiency of cognitive and motor training; and treating peripheral disorders, including renal, respiratory, gastrointestinal, liver, genitourinary, metabolic, and inflammatory disorders.
Type:
Grant
Filed:
June 15, 2022
Date of Patent:
April 2, 2024
Assignee:
Dart Neuroscience, LLC
Inventors:
Jillian Basinger Thompson, Brett C. Bookser, Scott Burley, Pablo Garcia-Reynaga, Andrew Hudson, Marco Peters, Benjamin Pratt, Aaron Thompson, Joe Tran, Lino Valdez
Abstract: Pharmaceutical compositions are provided according to aspects of the present disclosure which include a compound having chemical structural formula I: where R1 is selected from the group consisting of: an alkyl group, a heteroalkyl group, an aryl group, a heteroaryl group, an alkenyl group, a heteroalkenyl group, an alkynyl group, a heteroalkynyl group, a cycloalkyl group, a hetercycloalkyl group, an alkylcycloalkyl group, a heteroalkyl cycloalkyl group, an aralkyl group, a heteroaralkyl group, an alkoxy group, a polar group, an ester and a charged group; a pharmaceutically acceptable hydrolysable, or enzymatically cleavable, prodrug form thereof; and/or a pharmaceutically acceptable salt thereof; where R4? is H or an alkoxy group; where both R5 and R3? are OH, or where one or both OH groups is optionally modified as a pharmaceutically acceptable hydrolysable, or enzymatically cleavable, prodrug form thereof; and/or a deuterated form thereof; and/or a pharmaceutically acceptable salt thereof; and a pharma
Abstract: A method for the oxidation of ethylene to form ethylene oxide which comprises treating an aqueous stream in a cycle water treatment unit containing an anion exchange resin to reduce the content of the impurities.
Type:
Grant
Filed:
March 4, 2022
Date of Patent:
March 12, 2024
Assignee:
Scientific Design Company, Inc.
Inventors:
Saurabh Katiyar, Saurabh H. Parikh, Jason P. Durand