Abstract: The invention concerns compounds of formula (I) having antiviral activity, in particular, having an inhibitory activity on the replication of the respiratory syncytial virus (RSV). The invention further concerns pharmaceutical compositions comprising these compounds and the compounds for use in the treatment of respiratory syncytial virus infection.
Type:
Grant
Filed:
April 19, 2019
Date of Patent:
July 25, 2023
Assignee:
Janssen Sciences Ireland Unlimited Company
Inventors:
David Francis Alain Lançois, Jérome Émile Georges Guillemont, Pierre Jean-Marie Bernard Raboisson, Peter Rigaux, Antoine Benjamin Michaut, Sabrina Dany France Quatrevaux, Sovy Chao, Dirk André Emmy Roymans
Abstract: The present invention provides a crystalline form of a benzodiazepine derivative hydrochloride of Formula I or its ethanolate, wherein R is methyl or ethyl. The present invention also provides a method of preparing the crystal form of the compound of Formula I and a pharmaceutical composition comprising the crystal form.
Type:
Grant
Filed:
February 13, 2019
Date of Patent:
July 25, 2023
Assignee:
JIANGSU NHWALUOKANG PHARMACEUTICAL RESEARCH AND DEVELOPMENT CO., LTD.
Abstract: The disclosure provides compounds of Formula (I-A) and (I-B) and the pharmaceutically acceptable salts thereof. The variables, R, R2, R3, X1, X2, X3, Y1, Y, and Z are defined herein. Certain compounds of Formula (I-A) and (I-B) act as selective mitochondrial protonophore uncouplers that do not affect plasma membrane potential. These compounds are useful for treating or decreasing the risk of conditions responsive to mitochondrial uncoupling, such as cancer, obesity, type II diabetes, fatty liver disease, insulin resistance, Parkinson's disease, ischemia reperfusion injury, heart failure, non-alcoholic fatty liver disease (NALFD), and non-alcoholic steatohepatitis (NASH), Because mitochondrial uncouplers decrease the production of reactive oxygen species (ROS), which are known to contribute to age-related cell damage, the compounds are useful for increasing lifespan. Compounds and salts of Formulae (I-A) and (I-B) are also useful for regulating glucose homeostasis or insulin action in a patient.
Type:
Grant
Filed:
April 22, 2019
Date of Patent:
July 25, 2023
Assignee:
VIRGINIA TECH INTELLECTUAL PROPERTIES, INC.
Inventors:
Webster L. Santos, Yumin Dai, Jose A. Santiago-Rivera, Jacob H. Murray
Abstract: Solid forms of Compound (I): are disclosed. Pharmaceutical compositions comprising the same, methods of treating disorders and conditions mediated by BTK activity using the same, and methods for making Compound (I) and solid forms thereof are also disclosed.
Abstract: Disclosed herein are heterocyclic compounds according to formula (I) having the structure that inhibit the binding of menin and MLL or MLL fusion proteins. Also described are specific irreversible inhibitors of menin-HLL interaction. Also disclosed are pharmaceutical compositions that include compounds according to formula (I). Methods of using the menin-HLL irreversible inhibitors are disclosed, alone or in combination with other therapeutic agents, for the treatment of autoimmune diseases or conditions, heteroimmune diseases or conditions, cancer, including lymphoma, leukemia and other diseases or conditions dependent on menin-MLL interaction.
Type:
Grant
Filed:
June 18, 2021
Date of Patent:
July 18, 2023
Assignee:
BIOMEA FUSION, LLC
Inventors:
Thomas Butler, Jim Palmer, Ravi Upasani, Matthew Welsch, Sridhar Vempati, Brendan Kelly, Edward Painter
Abstract: Cellular biological activities are tightly controlled by intracellular signaling processes initiated by extracellular signals. Protein tyrosine phosphatases, which remove phosphate groups from tyrosine phosphorylated signaling molecules, play equally important tyrosine roles as protein kinases in signal transduction. SHP-2, a cytoplasmic SH2 domain containing protein tyrosine phosphatase, is involved in the signaling pathways of a variety of growth factors and cytokines. Recent studies have clearly demonstrated that this phosphatase plays an important role in transducing signal relay from the cell surface to the nucleus, and is a critical intracellular regulator in mediating cell proliferation and differentiation.
Type:
Grant
Filed:
September 28, 2018
Date of Patent:
July 18, 2023
Assignees:
D. E. Shaw Research, LLC, Relay Therapeutics, Inc.
Inventors:
Alexander M. Taylor, W. Patrick Walters, Mark Andrew Murcko, Fabrizio Giordanetto, Eric Therrien, Sathesh Bhat, Markus Kristofer Dahlgren
Abstract: The present invention provides a compound that have excellent harmful arthropod controlling effects, the compounds being represented by formula (I) [wherein Q represents a group represented by formula Q1 or the like, Z represents an oxygen atom or a sulfur atom, A1 represents a nitrogen atom or CR6a, A2 represents a nitrogen atom or CR6b, A3 represents a nitrogen atom or CR6c, A4 represents CR1a or the like, A5 represents a nitrogen atom or CR6e or the like, A6 represents a nitrogen atom or CR6f, R6a represents a hydrogen atom or the like, R6b represents a C1-C6 chain hydrocarbon group or the like, R6c, R6e, R6f are identical to or different from each other, and each represents a C1-C6 chain hydrocarbon group or the like, R1a represents a C1-C6 chain hydrocarbon group or the like, R2 represents a C1-C6 chain hydrocarbon group or the like, R3 represents a C1-C6 chain hydrocarbon group or the like, and n is 0, 1 or 2] or its N oxide compound.
Abstract: The invention provides various novel compositions of berberine in combination with pharmacologically active organic acids, and related methods of their use in treating various diseases or disorders. The invention further provides various novel compounds prepared from berberine and pharmacologically active organic acids and prepared from ursodeoxycholic acid and pharmacologically active organic bases, and pharmaceutical compositions thereof, and methods of their preparation and therapeutic use in treating and/or preventing various diseases or disorders.
Abstract: The invention relates to pharmaceutical compositions comprising, compounds of Formula Q: wherein W is —N(H)—, or —N(CH3)—, and Y is —C(?O)— or —O—, in free base or pharmaceutically acceptable salt form, and methods of use in the treatment of diseases involving 5-HT2A receptor, serotonin transporter (SERT) pathway and/or the dopamine D2 receptor pathway, and methods of treating conditions of the central nervous system therewith.
Type:
Grant
Filed:
October 16, 2020
Date of Patent:
June 20, 2023
Assignee:
INTRA-CELLULAR THERAPIES, INC.
Inventors:
Peng Li, Qiang Zhang, Robert Davis, Lawrence P. Wennogle
Abstract: The invention provides compounds of Formula (A) that may inhibit ENPP1, and that are accordingly useful for treatment of disorders related to ENPP1. The invention further provides pharmaceutical compositions containing these compounds and methods of using these compounds to treat or prevent disorders related to ENPP1.
Abstract: Crystalline forms of Compound (I): are disclosed. Pharmaceutical compositions comprising the same, methods of inhibiting BTK using the same, and methods for making crystalline forms of Compound (I) are also disclosed.
Type:
Grant
Filed:
January 7, 2021
Date of Patent:
June 6, 2023
Assignee:
Principia Biopharma Inc.
Inventors:
Pasit Phiasivongsa, Jiang Zhu, Kolbot By, Mohammad Reza Masjedizadeh
Abstract: The present invention provides phenyl-2-hydroxy-acetylamino-2-methyl-phenyl compounds, such as compounds of formula I: pharmaceutical compositions comprising the compounds, and methods of using the compounds to treat physiological disorders such as pancreatic cancer.
Type:
Grant
Filed:
April 11, 2018
Date of Patent:
May 23, 2023
Assignee:
ELI LILLY AND COMPANY
Inventors:
Marta Maria Cifuentes-Garcia, Maria Cristina Garcia Paredes
Abstract: Provided are heteroaryl heterocyclic compounds of formula (I), pharmaceutical compositions comprising same, methods for preparing same, and uses thereof, wherein the variables are as defined in the description. The compounds are Btk inhibitors.
Abstract: Disclosed in the present invention are a crystal form of a [1,2,4]triazolo[1,5-c]pyrimidine compound and a preparation method thereof. Further disclosed is a use of the crystal form in the preparation of a medicament for treating A2A receptor related diseases.
Type:
Grant
Filed:
April 28, 2019
Date of Patent:
May 16, 2023
Assignee:
Medshine Discovery Inc.
Inventors:
Kevin X. Chen, Yanxin Yu, Xinde Chen, Li Zhang, Zhaoguo Chen, Cheng Xie
Abstract: The present disclosure provides compounds represented by Formula (I-1): and pharmaceutically acceptable salts thereof, and methods of using the same. The compounds and methods have a range of utilities as therapeutics, diagnostics, and research tools. In particular, the subject compositions and methods are useful for reducing signaling output of oncogenic proteins.
Type:
Grant
Filed:
March 2, 2022
Date of Patent:
May 16, 2023
Assignee:
Kumquat Biosciences Inc.
Inventors:
Baogen Wu, Xiangzhu Wang, Xiaoming Li, Zhiyong Chen, Pingda Ren, Yi Liu
Abstract: Provided herein, inter alia, are substituted imidazo[1,5-?]pyrazine compounds, compositions and methods for treating or preventing an IRE1?-related disease or disorder. In certain embodiments, the disease or disorder is selected from the group consisting of a neurodegenerative disease, a demyelinating disease, cancer, an eye disease, a fibrotic disease, and diabetes.
Type:
Grant
Filed:
August 31, 2018
Date of Patent:
May 16, 2023
Assignees:
Optikira LLC, The Regents of the University of California
Inventors:
Richard M. Keenan, Bradley J. Backes, Dustin J. Maly, Charles Reynolds, Ben Whittaker, Jamie Knight, Jonathan Mark Sutton, George Hynd, Feroz R. Papa, Scott A. Oakes
Abstract: The invention relates to compounds of formula (I) which are inhibitors of kinase activity, pharmaceutical formulations containing the compounds and their uses in treating and preventing viral infections and disorders caused or exacerbated by the viral infection wherein R1, R2, R3, R4a, R4b, R4c, R5, W, X, Y and Z are defined herein.
Type:
Grant
Filed:
January 15, 2019
Date of Patent:
May 16, 2023
Assignee:
GLAXOSMITHKLINE INTELLECTUAL PROPERTY DEVELOPMENT LIMITED
Inventors:
Nicholas Paul Barton, Sophie Marie Bertrand, Kenneth David Down, Matthew Gray
Abstract: This invention is in the area of cell cycle inhibiting compounds for the treatment of disorders involving abnormal cellular proliferation, and include selective CDK2 inhibitors for medical therapy and their pharmaceutically acceptable salts and compositions.
Abstract: Provided are compounds of formula (I): or cosmeceutically acceptable or pharmaceutically acceptable salts thereof. Additionally provided are cosmeceutical and/or pharmaceutical compositions comprising the compounds of formula (I), or the cosmeceutically acceptable or pharmaceutically acceptable salts thereof. Also provided are therapeutic and/or cosmetic methods using the cosmeceutical and/or pharmaceutical compositions comprising the compounds of formula (I), or the cosmeceutically acceptable or pharmaceutically acceptable salts thereof, for modulating cyclic adenosine monophosphate response element binding (CREB)-binding protein (CBP)/?-catenin mediated signaling in treating skin related diseases, conditions, or disorders mediated by aberrant CBP/?-catenin signaling and cosmetic methods for treating skin conditions mediated by aberrant CBP/?-catenin signaling.
Abstract: Disclosed is a novel class of MDM2-p53 inhibitor compounds having an imidaxopyrolone structure, and specifically disclosed are compounds represented by formulas (I-1) and (I-2) and pharmaceutically acceptable salts thereof.
Type:
Grant
Filed:
March 12, 2019
Date of Patent:
May 2, 2023
Assignees:
LUOXIN PHARMACEUTICAL (SHANGHAI) CO., LTD., SHANDONG LUOXIN PHARMACEUTICAL GROUP STOCK CO., LTD., MEDSHINE DISCOVERY INC.
Inventors:
Kevin X Chen, Xiaobing Yan, Jianglei Huang, Yuekun Nie, Guoping Hu, Jian Li, Shuhui Chen, Jiaqiang Dong, Tie-Lin Wang