Abstract: Provided are compounds having metalloenzyme modulating activity, and methods of treating diseases, disorders or symptoms thereof mediated by such metalloenzymes.
Type:
Grant
Filed:
January 17, 2020
Date of Patent:
October 5, 2021
Assignee:
PHASEBIO PHARMACEUTICALS, INC.
Inventors:
Steven Sparks, Christopher M. Yates, Sammy R. Shaver
Abstract: The present invention provides for certain sulfonyl ureas and related compounds which have advantageous properties and show useful activity in the inhibition of activation of the NLRP3 inflammasome. Such compounds are useful in the treatment of a wide range of disorders in which the inflammation process, or more specifically the NLRP3 inflammasome, have been implicated as being a key factor.
Type:
Grant
Filed:
August 7, 2019
Date of Patent:
September 28, 2021
Assignees:
The Provost, Fellows, Foundation Scholars, And The Other Members Of Board, Of The College Of The Holy And Undivided Trinity Of Queen Elizabeth Near Dublin, The University Of Queensland
Inventors:
Luke O'Neill, Rebecca Coll, Matthew Cooper, Avril Robertson, Kate Schroder
Abstract: The invention relates to compounds and methods for restoring or preserving cholesterol efflux in a cell infected with Human Immunodeficiency Virus (HIV) by preventing or decreasing an interaction between Negative Regulatory Factor (Nef) protein and Calnexin protein, and methods for screening for such compounds.
Type:
Grant
Filed:
April 6, 2020
Date of Patent:
September 28, 2021
Assignee:
THE GEORGE WASHINGTON UNIVERSITY, A CONGRESSIONALLY CHARTERED NOT-FOR-PROFIT CORPORATION
Inventors:
Alexei Adzhubei, Michael Bukrinsky, Ruth Hunegnaw
Abstract: A novel structure of an opioid antagonist is provided. One of the exemplary compounds of the present disclosure has the structure of Formula (II). The present disclosure overcomes the discomfort of conventional opioid antagonist due to rapid absorption and improves the patient compliance thereof.
Type:
Grant
Filed:
June 20, 2019
Date of Patent:
September 28, 2021
Assignee:
TAIWANJ PHARMACEUTICALS CO., LTD.
Inventors:
Syaulan S. Yang, Kuang Yuan Lee, Yan-Feng Jiang
Abstract: The present invention relates to substituted quinoxaline and pyridopyrazine derivatives of Formula (I) wherein the variables have the meaning defined in the claims. The compounds according to the present invention are useful as pI3K? inhibitors. The invention further relates to pharmaceutical compositions comprising said compounds as an active ingredient as well as the use of said compounds as a medicament.
Type:
Grant
Filed:
March 29, 2018
Date of Patent:
September 28, 2021
Assignee:
Janssen Pharmaceutica NV
Inventors:
Patrick René Angibaud, Olivier Alexis Georges Querolle, Didier Jean-Claude Berthelot, Christophe Meyer, Matthieu Philippe Victor Willot, Lieven Meerpoel, Thierry François Alain Jean Jousseaume
Abstract: Compounds of formula (II) are provided for stabilizing protein transthyretin (TTR) and inhibiting amyloid fibril formation, for example, transthyretin-mediated amyloid fibril formation, and for treating, preventing, or ameliorating one or more symptoms of amyloid diseases, for example, transthyretin-related amyloidosis (ATTR).
Type:
Grant
Filed:
November 20, 2015
Date of Patent:
September 14, 2021
Assignee:
BSIM Therapeutics, S.A.
Inventors:
Rui Manuel Pontes Meireles Ferreira de Brito, Carlos José Vieira Simões, Teresa Margarida Vasconcelos Dias de Pinho e Melo, Bruno Lourenço da Silva Victor, Zaida Catarina Lourenço de Almeida, Ana Lúcia Cabral Cardoso Lopes, Bruno Filipe Oliveira Nascimento
Abstract: Provided herein are radiolabeled compounds useful for minimally invasive imaging techniques. An exemplary radiolabeled compound provided herein is useful as a radiotracer for position emission tomography imaging of voltage gated sodium channels. Methods for prepared unlabeled and labeled compounds, and diagnostic methods using the compounds are also provided.
Abstract: The present invention includes novel substituted bicyclic compounds, and compositions comprising the same, that can be used to treat or prevent hepatitis B virus (HBV) infections in a patient. In certain embodiments, the compounds and compositions of the invention are capsid inhibitors.
Type:
Grant
Filed:
March 20, 2018
Date of Patent:
August 24, 2021
Assignee:
Arbutus Biopharma Corporation
Inventors:
Andrew G. Cole, Bruce D. Dorsey, Ramesh Kakarla, Steven Kultgen, Jorge Quintero
Abstract: Novel Iridium complexes having three different bidentate ligands useful for phosphorescent emitters in OLEDs are disclosed. At least one of the three different bidentate ligands is a carbene ligand.
Type:
Grant
Filed:
September 7, 2019
Date of Patent:
August 24, 2021
Assignee:
UNIVERSAL DISPLAY CORPORATION
Inventors:
Jui-Yi Tsai, Chuanjun Xia, Chun Lin, Adrian U. Palacios, Enrique Oñate, Miguel A. Esteruelas, Pierre-Luc T. Boudreault, Sonia Bajo, Montserrat Oliván
Abstract: Adducts are described formed between pyrrole derivatives of formula (I) an carbon allotropes in which the carbon is sp2 hybridized, such as for example carbon nanotubes, graphene or nanographites, carbon black. The pyrrole derivatives bear substituents on the nitrogen atom suitable for improving the physicochemical characteristics of said allotropes. A process for preparing said adducts is also described. The adducts are formed with a pyrrole of formula (I) wherein X is selected from the group consisting of: The other substituents are as defined in the claims.
Abstract: The present invention relates to a composition for preventing or treating a muscular disease or improving muscle function. The composition includes suberic acid or a pharmaceutically acceptable salt thereof as an active ingredient.
Type:
Grant
Filed:
January 5, 2018
Date of Patent:
August 24, 2021
Assignee:
INDUSTRY-ACADEMIC COOPERATION FOUNDATION, YONSEI UNIVERSITY
Abstract: Compounds having the following Formula (I), or a pharmaceutically acceptable salt thereof, and methods of their use and preparation are disclosed:
Type:
Grant
Filed:
July 3, 2019
Date of Patent:
August 24, 2021
Assignee:
Gilead Sciences, Inc.
Inventors:
Mark J. Bartlett, Britton Kenneth Corkey, Jennifer Leigh Cosman, Elfatih Elzein, Xiaofen Li
Abstract: The present invention provides a compound of formula (I) or a pharmaceutically acceptable salt thereof; (I) or a pharmaceutically acceptable salt, tautomer, or stereoisomer thereof, wherein the variables are as defined herein. The present invention further provides pharmaceutical compositions comprising such compounds; and methods of using such compounds for treating joint damage or injury in a mammal, for inducing hyaline cartilage production or for inducing differentiation of chondrogenic progenitor cells into mature chondrocytes.
Type:
Grant
Filed:
June 7, 2018
Date of Patent:
August 17, 2021
Assignee:
Novartis AG
Inventors:
Ha-Soon Choi, Jiqing Jiang, James Paul Lajiness, Bao Nguyen, Hank Michael James Petrassi
Abstract: The disclosure relates to compounds of formula (I): R1-NH—CH(R2)-P(?O)(OH)—CH2-C(R3)(R4)-CONH—C(R5)(R6)-COOR7, where R1 to R7 are as defined in the claims, for use of same in the treatment and/or prevention of ocular inflammation, and more particularly for improving the process of ocular healing. Thus, the compounds of formula (I) are used, in particular, to prevent neovascularisation, or to prevent or treat an ocular inflammation linked to a keratitis, scleritis, episcleritis, uveitis, cataract, synechia, macular oedema, detachment of the retina, ocular hypertension and degeneration of the optical nerve caused by glaucoma.
Abstract: Complement Factor D inhibitors, pharmaceutical compositions, and uses thereof, as well as processes for their manufacture are provided. The compounds provided include Formula I, Formula II, Formula III, Formula IV, and Formula V, or a pharmaceutically acceptable salt, prodrug, isotopic analog, N-oxide, or isolated isomer thereof, optionally in a pharmaceutically acceptable composition. The inhibitors described herein target Factor D and inhibit or regulate the complement cascade.
Type:
Grant
Filed:
August 29, 2019
Date of Patent:
August 10, 2021
Assignee:
Achillion Pharmaceuticals, Inc.
Inventors:
Jason Allan Wiles, Avinash S. Phadke, Milind Deshpande, Atul Agarwal, Dawei Chen, Venkat Rao Gadhachanda, Akihiro Hashimoto, Godwin Pais, Qiuping Wang, Xiangzhu Wang, Joel Charles Barrish, William Greenlee, Kyle J. Eastman
Abstract: The present invention provides, in part, compositions comprising an inhibitor of cyclin-dependent kinase 7 (CDK7) and sulfobutyl ether-?-cyclodextrin. Also provided are methods of using a disclosed composition for treating proliferative diseases. The present invention also provides methods of making disclosed compositions.
Abstract: Benzimidazole derivatives of formula (I): wherein: R1 is —(CH2)m-R4 or R2 is halo, —(CH2)m—NH2 or —(CH2)n—C(?NH)—NH2; R3 is H or F; R4 is —NH—(CH2)2—(NH)r—R5, —NH—(CHR5R6) or a group of the following formula (A): (A) W is —(CH2)m—, —CH2—O—CH2—, —CH2—S—CH2—, —(CH2)r—S(O)2—CH2— or —(CH2)r—NR5—CH2—; m is an integer of 1 to 3; n is 1 or 2; p is 1 and V is CH; or p is O and V is N; q is 0 or 1; r is 0 or 1; R5 is H, —SO2Me, —SO2Et, —SO2CF3, —COMe, —CONMe2, —CONH2 or —CH2CH2SO2Me; R6 is H or C1-C6 alkyl; and R7 is —SO2Me, —SO2Et, —SO2CF3, —COMe, —CONMe2, —CONH2 or —CH2CH2SO2Me; and the pharmaceutically acceptable salts thereof are inhibitors of RSV and can therefore be used to treat or prevent an RSV infection.
Abstract: Methods of treating mitochondrial fatty acid b-oxidation and/or transport disorders arising from mutant proteins in the mitochondrial fatty acid ?-oxidation and transport metabolic pathways in patients are provided. The methods modulate the mitochondrial fatty acid ?-oxidation pathway at the last step so that the product of the mutant protein accumulates and stabilizes the mutant protein and/or the substrate(s)/product(s) of the down stream reactions accumulate and possibly bind to allosteric sites on the mutant protein to stabilize it. Trimetazidine pharmacodynamics function as such in the ?-oxidation pathway. Further, a synergistic effect is observed where trimetazidine and PPAR? agonist combination enhanced enzyme activity and presence significantly more than either alone.
Type:
Grant
Filed:
November 15, 2017
Date of Patent:
August 3, 2021
Assignee:
University of Pittsburgh—Of the Commonwealth System of Higher Education
Abstract: This application describes compounds that can act as opioid receptor ligands, which compounds can be used in the treatment of, for example, pain and pain related disorders.
Type:
Grant
Filed:
December 1, 2017
Date of Patent:
August 3, 2021
Assignee:
Trevena, Inc.
Inventors:
Dennis Yamashita, Dimitar Gotchev, Philip Pitis, Xiao-Tao Chen, Guodong Liu, Catherine C. K. Yuan