Abstract: A series of subunit selective allosteric modulators of NMDA receptor function according to Formula (I) is provided herein. Also provided is a method of treating neurological disorders such as Alzheimer's disease Parkinson's disease, schizophrenia, depression, stroke, psychosis and the like using compounds of Formula (I), optionally in combination with one or more further active agent. Pharmaceutical compositions containing a compound of Formula (I) and optionally one or more active agent for treating such disorders may be provided in the form of a tablet, capsule, pill, gel, granules, aerosol, aqueous buffer or a nanoparticle formulation, emulsion, liposome, etc.
Type:
Grant
Filed:
February 9, 2019
Date of Patent:
August 29, 2023
Assignee:
Emory University
Inventors:
Dennis Liotta, Stephen F. Traynelis, David Menaldino, Matthew Epplin
Abstract: The present invention discloses compounds of Formula (I), and pharmaceutically acceptable salts thereof: which inhibit the protein(s) encoded by hepatitis B virus (HBV) or interfere with the function of the HBV life cycle of the hepatitis B virus and are also useful as antiviral agents. The present invention further relates to pharmaceutical compositions comprising the aforementioned compounds for administration to a subject suffering from HBV infection. The invention also relates to methods of treating an HBV infection in a subject by administering a pharmaceutical composition comprising the compounds of the present invention.
Type:
Grant
Filed:
July 10, 2020
Date of Patent:
August 29, 2023
Assignee:
Enanta Pharmaceuticals, Inc.
Inventors:
Joseph Panarese, Samuel Bartlett, Dexter Davis, Nathaniel Kenton, Yat Sun Or
Abstract: The present invention relates to a method for preparing a lyophilized solid pharmaceutical composition comprising a) a compound having the formula (I): and/or a compound having the formula (II): ?and b) two different sodium phosphate salts, wherein the two different sodium phosphate salts are NaH2PO4·2H2O and Na2HPO4·2H2O, and wherein the quantity of the NaH2PO4·2H2O and Na2HPO4·2H2O present in the composition is chosen such that the molar ratio of both NaH2PO4·2H2O and Na2HPO4·2H2O to compound (I) or compound (II) ranges from 0.02 to 0.5.
Type:
Grant
Filed:
January 20, 2021
Date of Patent:
August 8, 2023
Assignee:
VASOPHARM GMBH
Inventors:
Peter Scheurer, Frank Tegtmeier, Reinhard Schinzel
Abstract: A reagent composition for a Karl Fischer titration includes (1) sulfur dioxide or a derivative thereof, (2) a derivative of imidazole, (3) an alcohol, and (4) at least one amino acid that is present in an amount that is greater than zero and up to about 10 weight percent based on a total weight of the reagent composition. Moreover, a molar ratio of the derivative of imidazole to the sulfur dioxide or derivative thereof is greater than 1:1. Iodine is optionally included in a one-component reagent and excluded in a two-component reagent. This disclosure further provides a method for determining an amount of water in a sample via Karl Fischer titration. The method includes the step of providing the sample, providing the reagent composition, which optionally includes the iodine (I2), and titrating the sample with the reagent composition.
Abstract: Disclosed are a quinazolinone derivative, a preparation method therefor, a pharmaceutical composition, and applications. Provided are a compound represented by formula I, a pharmaceutically acceptable salt, a solvate, a crystal form, a eutectic crystal, a stereoisomer, an isotope compound, a metabolite, or a prodrug thereof. Generation or activity of a cell factor can be regulated, and accordingly, cancers and inflammatory diseases can be effectively treated.
Abstract: Described herein is a process for the preparation of a compound of Formula I, wherein R1 and R2 each have the meanings provided in the description. Also described is a process for the preparation of pharmaceutically-active compounds including the process for the preparation of compounds of Formula I.
Abstract: The present invention relates to a method of treatment for chronic pain, opioid dependence, alcohol use disorder or autism using a class of pyrimidinone compounds, an adenylyl cyclase 1 (AC1) inhibitor. The invention described herein also pertains to pharmaceutical compositions and methods for treating diseases in mammals using those compounds disclosed herein.
Type:
Grant
Filed:
October 6, 2020
Date of Patent:
July 4, 2023
Assignee:
Purdue Research Foundation
Inventors:
Daniel P. Flaherty, Richard M. van Rijn, Val J. Watts, Jason A. Scott
Abstract: The present disclosure provides pladienolide compounds, pharmaceutical compositions containing such compounds, and pladienolide compounds for use in methods of medical treatment. These compounds may be useful in the treatment of cancer, particularly cancers in which agents that target the spliceosome and mutations therein are known to be useful.
Type:
Grant
Filed:
April 11, 2019
Date of Patent:
June 20, 2023
Assignee:
EISAI R&D MANAGEMENT CO., LTD.
Inventors:
Andrew Cook, Dominic Reynolds, Cheng Zhong, Ryan Brawn, Shelby Ellery, Thiwanka Samarakoon, Xiang Liu, Sudeep Prajapati, Megan Sheehan, Jason T. Lowe, James Palacino
Abstract: The present disclosure provides methods of inhibiting the interaction of menin with MLL1, MLL2 and MLL-fusion oncoproteins with compositions of Formula (II-A). The methods are useful for the treatment of leukemia, solid cancers, diabetes and other diseases dependent on activity of MLL1, MLL2, MLL fusion proteins, and/or menin. Compositions of Formula (II-A) for use in these methods are also provided.
Type:
Grant
Filed:
July 30, 2020
Date of Patent:
June 13, 2023
Assignees:
KURA ONCOLOGY, INC., THE REGENTS OF THE UNIVERSITY OF MICHIGAN
Inventors:
Tao Wu, Liansheng Li, Yi Wang, Pingda Ren, Jolanta Grembecka, Tomasz Cierpicki, Szymon Klossowski, Jonathan Pollock, Dmitry Borkin
Abstract: The present disclosure is directed to inhibitors of SHP2, such as pyrazine compounds, and their use in the treatment of disease associated with SHP2 modulation, such as Noonan Syndrome, Leopard Syndrome, juvenile myelomonocytic leukemias, neuroblastoma, melanoma, acute myeloid leukemia and cancers of the breast, lung and colon. Also disclosed are pharmaceutical compositions comprising the same.
Type:
Grant
Filed:
June 18, 2020
Date of Patent:
May 30, 2023
Assignee:
REVOLUTION MEDICINES, INC.
Inventors:
Elena S. Koltun, Kevin Mellem, Adrian Gill, Gert Kiss, Christopher Semko, Naing Aay, Andreas Buckl, Ashutosh Jogalekar, Walter Won
Abstract: The disclosure provides compounds and salts that show high selectivity and inhibitory activity for mTORC1 and uses thereof for the treatment of disease, such as Formula I: or a pharmaceutically acceptable salt thereof.
Abstract: The present disclosure relates to novel triazolo-pyrimidine compounds targeting adenosine receptors (especially A1 and A2, particularly A2a). The present disclosure also relates to pharmaceutical compositions comprising one or more of the compounds as an active ingredient, and use of the compounds in the treatment of adenosine receptor (AR) associated diseases, for example cancer such as NSCLC, RCC, prostate cancer, and breast cancer.
Abstract: Bicyclic and tricyclic pyrimidine tyrosine kinase inhibitors with antitubulin activity are provided in the present invention. The compositions of the present invention possess dual activity in a single agent of potent vascular endothelial growth factor receptor inhibitory activity as well as antitubulin activity. Water soluble salts of these compositions are also described. Methods of treating a patient having cancer, macular degeneration, and arthritis with the compositions and salts thereof of the present invention are disclosed.
Abstract: The disclosure provides compounds and salts that show high selectivity and inhibitory activity for mTORC1 and uses thereof for the treatment of disease, such as Formula X: or a pharmaceutically acceptable salt thereof.
Abstract: This application relates to quinazoline derivatives of formula (I), pharmaceutical compositions comprising the compounds of formula (I), and the use of the compounds of formula (I) in the treatment or prevention of a viral infection, of a virus-induced disease, of cancer or of an allergy.
Type:
Grant
Filed:
February 28, 2019
Date of Patent:
March 7, 2023
Assignee:
JANSSEN SCIENCES IRELAND UNLIMITED COMPANY
Inventors:
David Craig Mc Gowan, Werner Constant Johan Embrechts, Jérôme Émile Georges Guillemont, Ludwig Paul Cooymans, Tim Hugo Maria Jonckers, Pierre Jean-Marie Raboisson
Abstract: Novel Gi/o-biased muscarinic agonists selectively activate only one specific signaling pathway and are novel pharmacophores for development of new painkillers (analgesics). Methods of making and using these agonists are also described. The muscarinic agonists are of the formula: or an analog, derivative or pharmaceutically acceptable salt thereof, wherein: R1=H or Me; R2=H, Me, Et, OMe, OEt, F, Cl, Br, I, or NO2; and R3=H, Me, Et, OMe, or CO2Me (R3 may be bonded to any carbon of the rings).
Abstract: A method is disclosed for treating a cancer in a subject that involves administering to the subject a therapeutically affective amount of a geranylgeranyltransferase I (GGTase I) inhibitor, such as GGTI-2418, wherein the cancer comprises a defective PTEN, a hyperactivated FBXL2, or a low level of IP3R3. In some embodiments, the method further involves administering to the subject a therapeutically affective amount of an Akt inhibitor.
Type:
Grant
Filed:
June 6, 2018
Date of Patent:
February 21, 2023
Assignees:
H. LEE MOFFITT CANCER CENTER AND RESEARCH INSTITUTE, INC., NEW YORK UNIVERSITY
Inventors:
Said M. Sebti, Michele Pagano, Shafi Kuchay
Abstract: The present disclosure novel pyrazine compounds targeting adenosine receptors (especially A1 and A2, particularly A2a). The present disclosure also relates to pharmaceutical compositions comprising one or more of the compounds as an active ingredient, and use of the compounds in the treatment of adenosine receptor (AR) associated diseases, for example cancer such as NSCLC, RCC, prostate cancer, and breast cancer.
Abstract: The present invention provides processes of synthesis and purification of a bromodomain inhibitor, Compound 1, which compound includes crystalline forms, amorphous forms, solvates, and hydrates thereof. Embodiments of the disclosure relate to chemical synthesis routes of Compound 1 that provide a scalable method that results in highly pure final product. A further embodiment relates to methods to isolate the most stable polymorph of Compound 1 by crystallization from formic acid and water.
Type:
Grant
Filed:
July 23, 2019
Date of Patent:
January 31, 2023
Assignee:
CELGENE QUANTICEL RESEARCH, INC.
Inventors:
John Fitzgerald Traverse, Kelvin Hin-Yeong Yong, Antonio Christian Ferretti, Hekla Alite, Jonathan Moseley, Antonio Maria Ruda, David Primer, Steven Philp