Abstract: This invention relates to the new use of neurokinin-1 receptor antagonists as a treatment of pulmonary fibrosis conditions promoted by mechanical injury to the lungs. Specifically, when the mechanical injury to the lungs is induced by mechanical ventilation or by the act of coughing in a subset of patients with pulmonary fibrosis conditions who cough. The invention further relates to pharmaceutical compositions comprising neurokinin-1 receptor antagonist drugs and to combinations for such uses.
Abstract: The present invention provides: a methyl 1-{2-[(3S,4R)-1-[(3R,4R)-1-cyclopentyl-3-fluoro-4-(4-methoxyphenyl)pyrrolidine-3-carbonyl]-4-(methoxymethyl)pyrrolidin-3-yl]-5-(trifluoromethyl)phenyl}piperidine-4-carboxylate 1/2 ethane-1,2-disulfonic acid which is represented by formula (1) and is excellent in crystallinity; and a method for producing the same; and a production intermediate thereof; and a production method using this compound.
Abstract: This disclosure provides compounds and compositions for activating pyruvate kinase R (PKR) and related methods of manufacturing and using these compounds and compositions.
Type:
Grant
Filed:
June 18, 2021
Date of Patent:
December 19, 2023
Assignee:
NOVO NORDISK HEALTH CARE AG
Inventors:
Anna Ericsson, Neal Green, Gary Gustafson, David R. Lancia, Jr., Gary Marshall, Lorna Mitchell, David Richard, Zhongguo Wang
Abstract: Disclosed are complexes and methods of using the complexes as catalysts for addition of amines to unsaturated electrophiles, as well as novel compounds produced by the disclosed complexes and methods. The disclosed methods may utilize the disclosed complexes as catalysts for adding unprotected primary amines and secondary amines to unsaturated electrophiles in an enantioselective manner to produce novel compounds which may include amino substituted succinimide compounds.
Abstract: A method for treating a mammal having an autoimmune disease, wherein said method comprises administering a SCD1 polypeptide inhibitor to said mammal, wherein said SCD1 polypeptide inhibitor is a compound having Formula (II): or a pharmaceutically acceptable salt thereof; wherein: R1 is halo; X is —(C?O)NR4—; Y is ?and R2, R3, and R4 are each independently H or an unsubstituted alkyl.
Type:
Grant
Filed:
August 24, 2021
Date of Patent:
December 5, 2023
Assignee:
Mayo Foundation for Medical Education and Research
Abstract: Provided herein are compounds of Formula (I), or pharmaceutically acceptable salts thereof, pharmaceutical compositions that include a compound described herein (including pharmaceutically acceptable salts of a compound described herein) and methods of synthesizing the same. Also provided herein are methods of treating diseases and/or conditions with a compound of Formula (I), or a pharmaceutically acceptable salt thereof.
Type:
Grant
Filed:
November 22, 2021
Date of Patent:
November 21, 2023
Assignee:
Aligos Therapeutics, Inc.
Inventors:
Sandrine Vendeville, Yannick Debing, Pierre Jean-Marie Bernard Raboisson
Abstract: Provided herein are certain compounds useful as HTT modulators. Such compound are useful in the treatment of Huntington's disease.
Type:
Grant
Filed:
May 12, 2021
Date of Patent:
November 7, 2023
Assignee:
CHDI Foundation, Inc.
Inventors:
Celia Dominguez, Elizabeth M. Doherty, Longbin Liu, Matthew Lee, Mark Stuart Chambers, Karine Fabienne Malagu, Perla Breccia, Alan F. Haughan, Huw D. Vater, Andrew J. Stott, William R. K. Esmieu, Stephen John Webster, Amanda J. Van De Poël
Abstract: The present invention relates to novel methods and therapies for treating, preventing or delaying the onset of type 1 diabetes. In one aspect, the invention provides a method of preventing, delaying the onset of, or delaying the progression of, type 1 diabetes (T1D) in an individual, the method comprising providing in the individual an anti-inflammatory compound; and a pancreatic autoantigen or a derivative or variant thereof; thereby preventing, delaying the onset of, or delaying the progression of, T1D in the individual.
Type:
Grant
Filed:
August 7, 2018
Date of Patent:
November 7, 2023
Assignee:
St. Vincent's Institute of Medical Research
Inventors:
Helen E. Thomas, Thomas W. H. Kay, Balasubramanian Krishnamurthy, Gaurang Jhala
Abstract: Disclosed are compounds of Formula I: or a pharmaceutically acceptable salt, a solvate, a tautomer, a stereoisomer or a deuterated analog thereof, wherein R1, R2, R3, A, E, L, and G are as described in any of the embodiments described in this disclosure; compositions thereof; and uses thereof.
Type:
Grant
Filed:
April 22, 2021
Date of Patent:
November 7, 2023
Assignee:
Opna Bio SA
Inventors:
Songyuan Shi, John Buell, Zuojun Guo, Cuong Ly, Wayne Spevak, Mark Vander Wal, Jack Walleshauser, Chao Zhang, Jiazhong Zhang
Abstract: Methods for treating certain androgen receptor-positive forms of cancer using inhibitors of the CREB binding protein bromodomain are disclosed. In some methods, the AR-positive forms of cancer may be breast cancer, including triple negative forms, hormone receptor positive forms, and HER2-positive forms. In other methods, the AR-positive forms of cancer may be prostate cancer, including metastatic castration resistant prostate cancer. In some embodiments, methods of treating prostate cancer comprise the step of administering to a patient in need thereof the compound (1R,3R)-3-[(7S)-2-[(R)-(5-fluoro-2-methoxyphenyl)(hydroxy)methyl]-6-(methoxycarbonyl)-7-methyl-3H,6H,7H,8H,9H-imidazo[4,5-f]quinolin-3-yl]cyclohexane-1-carboxylic acid, or a pharmaceutically acceptable salt thereof.
Abstract: The present invention relates to a novel compounds for inhibiting nicotinamide phosphoribosyltransferase (NamPT), a composition comprising the same, and various uses thereof.
Abstract: The present disclosure relates to compounds of formula I that are useful as modulators of ?7 nAChR, compositions comprising such compounds, and the use of such compounds for preventing, treating, or ameliorating disease, particularly disorders of the central nervous system such as cognitive impairments in Alzheimer's disease, Parkinson's disease, and schizophrenia, as well as for L-DOPA induced-dyskinesia and inflammation
Type:
Grant
Filed:
March 5, 2021
Date of Patent:
October 24, 2023
Assignee:
Merck Sharp & Dohme LLC
Inventors:
Brendan M. Crowley, Ian M. Bell, Andrew John Harvey
Abstract: The invention relates to prodrug compounds of formula I: wherein R2, R3, R5, R7 and X are as defined herein. The invention also provides pharmaceutically acceptable compositions comprising the compounds of the invention and methods of using the compositions in the treatment of various disorders, including pain. The compounds of formula I possess advantageous solubility and physicochemical properties.
Type:
Grant
Filed:
August 20, 2020
Date of Patent:
October 3, 2023
Assignee:
VERTEX PHARMACEUTICALS INCORPORATED
Inventors:
Corey Anderson, Sara Sabina Hadida Ruah, Julian Marian Charles Golec, Beili Zhang, Benjamin Joseph Littler, Ali Keshavarz-Shokri, Tim Edward Alcacio, Daniel T. Belmont
Abstract: This invention relates to compounds that are agonists of the muscarinic M1 and/or M4 receptor and which are useful in the treatment of diseases mediated by the muscarinic M1 and M4 receptors. Also provided are pharmaceutical compositions containing the compounds and the therapeutic uses of the compounds. Compounds provided are of formula where Y, R1, R2 and R4 are as defined herein.
Type:
Grant
Filed:
September 17, 2020
Date of Patent:
October 3, 2023
Assignee:
Heptares Therapeutics Limited
Inventors:
Giles Albert Brown, Barry John Teobald, Benjamin Gerald Tehan
Abstract: The present disclosure provides methods for treating or preventing a viral infection with one or more arylamide compounds, or pharmaceutically acceptable salts thereof, or compositions comprising the same, and pharmaceutical compositions comprising one or more arylamide compounds and at least one antiviral agent.
Type:
Grant
Filed:
June 4, 2021
Date of Patent:
October 3, 2023
Assignee:
Innovation Pharmaceuticals Inc.
Inventors:
Jane A. Harness, Leo Ehrlich, Warren Kyle Weston
Abstract: The present disclosure is concerned with biaryl aminomaleimide compounds for the treatment of disorders associated with heme oxygenase-1 (HO-1) signaling dysfunction such as, for example, kidney diseases (e.g., chronic kidney disease, acute kidney injury). 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 invention.
Type:
Grant
Filed:
November 17, 2021
Date of Patent:
September 12, 2023
Assignees:
Southern Reserach Institute, The UAB Research Foundation, The United States Government as represented by the Department of Veterans Affairs
Inventors:
Mark J. Suto, Bini Mathew, Anupam Agarwal, Amie M. Traylor
Abstract: A method of synthesizing a 2-hydroxyphenyl-5-pyrimide ketone represented by the following chemical formula (I), including: weighing 0.048 g of a palladium complex, 0.8413 g of chromone-3-formaldehyde and 2.5719 g of ammonium formate into a 100 mL round bottom flask, then adding 50 mL of anhydrous methanol to dissolve, heating to reflux for 36 h, then stopping the reaction, performing column chromatography with petroleum ether and dichloromethane in a volume ratio of 1:1, and then naturally volatilizing the first component to obtain a light yellow crystal, namely the 2-hydroxyphenyl-5-pyrimidine ketone; wherein the chemical formula of the compound (I) is as follows: and an use of compound (I) as a catalyst in the reaction of benzophenone imine and trimethylsilyl nitrile showing a good catalytic performance, with a conversion rate of 69.1%.
Type:
Grant
Filed:
July 29, 2021
Date of Patent:
September 5, 2023
Assignees:
Intelligent Manufacturing Institute of Hefei University Technology, Hefei University of Technology
Abstract: Disclosed are compounds of Formula (I?) methods of using the compounds for inhibiting HPK1 activity and pharmaceutical compositions comprising such compounds. The compounds are useful in treating, preventing or ameliorating diseases or disorders associated with HPK1 activity such as cancer.
Type:
Grant
Filed:
September 9, 2020
Date of Patent:
August 22, 2023
Assignee:
Incyte Corporation
Inventors:
Oleg Vechorkin, Jun Pan, Alexander Sokolsky, Evan Styduhar, Wenqing Yao
Abstract: Methods for treating diffuse intrinsic pontine glioma (DIPG) comprising administration of a therapeutically effective amount of an alkylating hexitol (such as dianhydrogalacitol, diacetyldianhydrogalacitol, and dibromodulcitol) are disclosed. Such methods may further comprise administration of other anti-cancer agents. In preferred embodiments, the secondary anti-cancer agent is an inhibitor of Wee1 tyrosine kinase (such as adavosertib). Methods of treating malignancies in general comprising administration of a combination of an alkylating hexitol and an inhibitor of Wee1 tyrosine kinase are also disclosed.
Type:
Grant
Filed:
November 2, 2018
Date of Patent:
August 8, 2023
Assignee:
Del Mar Pharmaceuticals (BC) Limited
Inventors:
Anne Steinø, Jeffrey A. Bacha, Dennis M. Brown