Abstract: A compound of formula (I), wherein R1 is an optionally substituted aryl or an optionally substituted heteroaryl, R2 is an optionally substituted aryl or an optionally substituted heteroaryl, and R3 is an optionally substituted alkylamino, an optionally substituted cycloalkylamino, an optionally substituted arylamino, an optionally substituted heterocyclylamino, an optionally substituted heterocyclyl, and an optionally substituted dialkylamino. A pharmaceutical composition which includes the compound of formula (I) and a pharmaceutically acceptable carrier and/or excipient. A method of treating colorectal cancer in a subject, whereby a therapeutically effective amount of the compound of formula (I) is administered to the subject.
Type:
Grant
Filed:
September 24, 2021
Date of Patent:
January 4, 2022
Assignee:
King Abdulaziz University
Inventors:
Moustafa E. El-Araby, Abdelsattar M. Omar, Martin K. Safo, Radwan S. Elhaggar, Tamer M. Abdelghany, Mostafa H. Ahmed
Abstract: The present invention provides a compound of Formula I: wherein R is H or F; or a pharmaceutically acceptable salt thereof, and the use of compounds of Formula I for treatment of neurodegenerative diseases, such as Alzheimer's disease.
Type:
Grant
Filed:
June 14, 2019
Date of Patent:
January 4, 2022
Assignee:
Eli Lilly and Company
Inventors:
Nicolas Jacques Francois Dreyfus, Andrew Faller
Abstract: An N-substituted imidazole carboxylate compound is of formula (I). In formula (I), C* is an R-type chiral carbon atom, R1 and R2 are independently selected from H, methyl, ethyl, cyclopropyl, cyclobutyl or isopropyl, or R1 and R2 form a C2˜5 alkylenyl group; R3 is a substituted or unsubstituted C1-18 saturated or unsaturated aliphatic hydrocarbon or aromatic hydrocarbon, in which the aliphatic hydrocarbon comprises a straight chain, branched chain or cyclic aliphatic hydrocarbyl. The compound or pharmaceutically acceptable salts thereof can be used to prepare central inhibitory drugs that exert sedative, hypnotic and/or anesthetic effects on humans or animals, and can produce rapid and reversible anesthetic effects, and can be rapidly metabolized into an inactive etomidate acid, and after drug withdrawal, the wake-up quality is good; and the body's corticosteroid function can be rapidly recovered after a single administration or continuous administration.
Type:
Grant
Filed:
January 31, 2018
Date of Patent:
December 28, 2021
Assignee:
WEST CHINA HOSPITAL, SICHUAN UNIVERSITY
Inventors:
Jin Liu, Jun Yang, Wensheng Zhang, Bowen Ke, Lei Tang, Bin Wang
Abstract: This invention relates to the large-scale production of psilocybin for use in medicine. More particularly, it relates to a method of obtaining high purity crystalline psilocybin, particularly, in the form of Polymorph A. It further relates to a method for the manufacture of psilocybin and intermediates in the production thereof and formulations containing psilocybin.
Type:
Grant
Filed:
April 13, 2021
Date of Patent:
November 23, 2021
Assignee:
COMPASS PATHFINDER LIMITED
Inventors:
Derek John Londesbrough, Christopher Brown, Julian Scott Northen, Gillian Moore, Hemant Kashinath Patil, David E. Nichols
Abstract: The present invention relates to salt forms of the Fibroblast Growth Factor Receptors (FGFR) inhibitor 3-(2,6-difluoro-3,5-dimethoxyphenyl)-1-ethyl-8-(morpholin-4-ylmethyl)-1,3,4,7-tetrahydro-2H-pyrrolo[3?,2?:5,6]pyrido[4,3-d]pyrimidin-2-one, including methods of preparation thereof, where the compound is useful in the treatment of FGFR mediated diseases such as cancer.
Abstract: The application is directed to compounds of formula (I): and their salts and solvates, wherein R1, R2, R3, A1, A2, A3, and n are as set forth in the specification, as well as to a method for their preparation, pharmaceutical compositions comprising the same, and use thereof for the treatment and/or prevention of a lysosomal storage disease, such as Gaucher's, and other diseases or disorders that are synucleinopathies.
Type:
Grant
Filed:
December 28, 2017
Date of Patent:
November 16, 2021
Assignee:
Minoryx Therapeutics S.L.
Inventors:
Ana Maria García Collazo, Xavier Barril Alonso, Elena Cubero Jordà, Marc Revés Vilaplana, Richard Spurring Roberts
Abstract: This invention relates to a crystalline form of 1-((2R,4R)-2-(1H-benzo[d]imidazol-2-yl)-1-methylpiperidin-4-yl)-3-(4-cyanophenyl)urea maleate, and to pharmaceutical compositions thereof, to intermediates and methods for the production and isolation of such crystalline forms and compositions, and to methods of using such crystalline forms and compositions in the treatment of abnormal cell growth in mammals, especially humans.
Abstract: Disclosed herein are compositions for assessing peptidoglycan (PG) biosynthesis in bacteria using modified D-amino acids covalently attached to a molecular rotor and visualizing the labeled PG in bacteria based upon the enhanced fluorescence of the molecular rotor incorporated in the PG. The resultant, labeled peptidoglycan structures are amenable for identification by microscopic visualization, flow cytometry or other suitable methods.
Type:
Grant
Filed:
February 7, 2019
Date of Patent:
November 9, 2021
Assignee:
Indiana University Research and Technology Corporation
Inventors:
Michael VanNieuwenhze, Yves Brun, Erkin Kuru, Edward Hall
Abstract: The present invention provides novel purine based compounds of formula 1, method of preparation of purine based compounds and its composition useful for inhibiting signalling through Toll-like receptors. These compounds are useful in inhibiting immune stimulation involving toll-like receptor 9 (TLR9). These can be used in treatment of autoimmune disease and inflammation where aberrant activation of TLR9 plays role.
Type:
Grant
Filed:
November 5, 2018
Date of Patent:
November 9, 2021
Assignee:
Council of Scientific & Industrial Research
Abstract: The present invention is directed to substituted certain reversed indazolyl-spiro[2.2]pentane-carbonitrile derivatives of Formula (I): and pharmaceutically acceptable salts thereof, wherein R1, R2, R3, X, Y, and Z are as defined herein, which are potent inhibitors of LRRK2 kinase and may be useful in the treatment or prevention of diseases in which the LRRK2 kinase is involved, such as Parkinson's Disease and other diseases and disorders described herein. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which LRRK-2 kinase is involved.
Type:
Grant
Filed:
October 8, 2018
Date of Patent:
November 2, 2021
Assignee:
Merck Sharp & Dohme Corp.
Inventors:
David Annunziato Candito, Thomas H. Graham, John Acton, Ryan Wing-Kun Chau, Joanna L. Chen, J. Michael Ellis, Peter H. Fuller, Anmol Gulati, Hakan Gunaydin, Solomon Kattar, Mitchell Henry Keylor, Blair T. Lapointe, Ping Liu, Weiguo Liu, Joey L. Methot, Santhosh F. Neelamkavil, Vladimir Simov, Ling Tong, Harold B. Wood
Abstract: By using ion exchange column chromatography or calcium carbonate to an aqueous solution containing a compound A represented by the following formula and citric acid, citric acid in the aqueous solution is removed and a crystalline compound A is obtained by being thereafter subjected to several steps. Further a high-purity noncrystalline compound A is obtained by using calcium carbonate, sulfuric acid, an organic solvent and the like to the aqueous solution containing the compound A and citric acid to remove citric acid and the crystalline compound A in the solution. The configuration of the crystalline compound A is an SS isomer in the RS notation system. The configuration of the noncrystalline compound A is an SR isomer.
Abstract: Derivatives of N,N-diethyl-N?-phenyl-piperazine, a silent agonist of the mammalian ?7 nicotinic acetylcholine receptor, are provided. These silent agonists control the desensitization state of the receptor. Further provided are pharmaceutical compositions that allow the administration of the silent agonists of the disclosure to a subject animal or human in need of treatment for a pathological condition arising from such as inflammation. The novel silent agonists also may be co-administered to a patient simultaneously or consecutively with a type II positive allosteric modulator to modulate the activity of the receptor.
Type:
Grant
Filed:
April 16, 2020
Date of Patent:
October 26, 2021
Assignee:
University of Florida Research Foundation, Inc.
Inventors:
Nicole Alana Horenstein, Roger Lee Papke, Marta Quadri
Abstract: A compound of formula (I), wherein R1 is an optionally substituted aryl or an optionally substituted heteroaryl, R2 is an optionally substituted aryl or an optionally substituted heteroaryl, and R3 is an optionally substituted alkylamino, an optionally substituted cycloalkylamino, an optionally substituted arylamino, an optionally substituted heterocyclylamino, an optionally substituted heterocyclyl, and an optionally substituted dialkylamino. A pharmaceutical composition which includes the compound of formula (I) and a pharmaceutically acceptable carrier and/or excipient. A method of treating colorectal cancer in a subject, whereby a therapeutically effective amount of the compound of formula (I) is administered to the subject.
Type:
Grant
Filed:
October 25, 2019
Date of Patent:
October 26, 2021
Assignee:
King Abdulaziz University
Inventors:
Moustafa E. El-Araby, Abdelsattar M. Omar, Martin K. Safo, Radwan S. Elhaggar, Tamer M. Abdelghany, Mostafa H. Ahmed
Abstract: This invention relates to the large-scale production of psilocybin for use in medicine. More particularly, it relates to a method of obtaining high purity crystalline psilocybin, particularly, in the form of Polymorph A. It further relates to a method for the manufacture of psilocybin and intermediates in the production thereof and formulations containing psilocybin.
Type:
Grant
Filed:
February 10, 2021
Date of Patent:
October 19, 2021
Assignee:
COMPASS PATHFINDER LIMITED
Inventors:
Derek John Londesbrough, Christopher Brown, Julian Scott Northen, Gillian Moore, Hemant Kashinath Patil, David E. Nichols
Abstract: The present invention relates to a cyano-substituted heteroarylpyrimidinone derivative represented by formula (I), a preparation method therefor and a use thereof as a therapeutic agent, in particular a use as an acetyl-CoA carboxylase (ACC) inhibitor, and the definition of each substituent in formula (I) is the same as the definition in the description.
Abstract: The present invention features improved compounds, especially the compound having the structure (1). Compositions and methods of identifying patients having cancer using biomarkers (e.g., PDE3A, PDE3B, SLFN12 and/or CREB3L1) that correlate with drug sensitivity and consequently treating a stratified patient population with an agent of the invention.
Type:
Grant
Filed:
February 1, 2018
Date of Patent:
October 12, 2021
Assignees:
The Broad Institute, Inc., Dana-Farber Cancer Institute, Inc., Bayer Aktiengesellschaft, Bayer Pharma Aktiengesellschaft
Inventors:
Timothy A. Lewis, Xiaoyun Wu, Heidi Greulich, Matthew Meyerson, Manuel Ellermann, Philip Lienau, Knut Eis, Antje Margret Wengner, Charlotte Christine Kopitz, Martin Lange
Abstract: This invention relates to thienopyrimidinones and their use as inhibitors of TRPA1 activity, pharmaceutical compositions containing the same, and methods of using the same as agents for treatment and/or prevention of fibrotic diseases, inflammatory and auto-immune diseases and CNS-related diseases.
Type:
Grant
Filed:
October 15, 2020
Date of Patent:
October 5, 2021
Assignee:
Boehringer Ingelheim International GmbH
Inventors:
Martin Thomas Fleck, Florian Paul Christian Binder, Georg Dahmann, Joerg P. Hehn, Annekatrin Charlotte Heimann, Jens Willwacher
Abstract: The present invention includes substituted 2,3-dihydro-1H-indene analogs, and compositions comprising the same, that can be used to treat or prevent hepatitis B virus (HBV) infections in a patient.
Type:
Grant
Filed:
April 24, 2018
Date of Patent:
September 28, 2021
Assignee:
Arbutus Biopharma Corporation
Inventors:
Yingzhi Bi, Bruce D. Dorsey, Christopher Brooks Moore
Abstract: A compound represented by Formula (I): wherein or the like, Y1 is O or the like; Z1 is C(R4) or N; Z2a is C(R5a) or the like; Z3a is C(R6) or the like; R4, R5a and R6 are each independently a hydrogen atom or the like; R1 is substituted or unsubstituted aromatic carbocyclyl or the like; R2a, R2b, R2c and R2d are each independently a hydrogen atom or the like; X is N(R7a) or the like; R7a is a hydrogen atom or the like; R3 is or the like, Ring B is a 6-membered aromatic carbocycle or the like; R9a and R10a are each independently halogen or the like; n is an integer from 1 to 5; m is an integer from 0 to 4; and p1 is an integer from 0 to 3, or a pharmaceutically acceptable salt thereof.
Abstract: The present invention discloses to a hydrochloride salt, a citrate salt, a phosphate salt or a sulfate salt of compound 1, the crystal forms of the aforementioned salts, and a preparation method thereof. The present invention also relates their use in the preparation of a medicament for the treatment of cerebral apoplexy or epilepsy.
Type:
Grant
Filed:
August 3, 2017
Date of Patent:
September 21, 2021
Assignee:
HARBIN PHARMACEUTICAL GROUP CO., LTD. GENERAL PHARMACEUTICAL FACTORY