Abstract: The subject matter described herein is directed to ferroportin inhibitor compounds of Formula I or I? and pharmaceutical salts thereof, methods of preparing the compounds, pharmaceutical compositions comprising the compounds, and methods of administering the compounds for prophylaxis and/or treatment of diseases caused by a lack of hepcidin or iron metabolism disorders, particularly iron overload states, such as thalassemia, sickle cell disease and hemochromatosis, and also kidney injuries.
Type:
Grant
Filed:
June 15, 2023
Date of Patent:
January 21, 2025
Assignee:
Global Blood Therapeutics, Inc.
Inventors:
Qing Xu, Carsten Alt, Zhe Li, Shahul Nilar, Peter Michael Rademacher, Calvin Wesley Yee
Abstract: Compounds that inhibit p38? MAPK protein, and methods of using the same, are provided for treating or preventing diseases such as cancer or inflammatory diseases.
Type:
Grant
Filed:
June 7, 2023
Date of Patent:
January 21, 2025
Assignee:
University of Maryland, Baltimore
Inventors:
Paul S. Shapiro, Alexander D. Mackerell, Jr., Jeffrey D. Hasday, Steven Fletcher
Abstract: Substituted pyridazinone compounds, conjugates, and pharmaceutical compositions for use in the treatment of neuromuscular diseases, such as Duchenne Muscular Dystrophy (DMD), are disclosed herein. The disclosed compounds are useful, among other things, in the treating of DMD and modulating inflammatory inhibitors IL-1, IL-6 or TNF-?.
Type:
Grant
Filed:
September 1, 2023
Date of Patent:
January 21, 2025
Assignee:
EDGEWISE THERAPEUTICS, INC.
Inventors:
Kevin Hunt, Kevin Koch, Alan Russell, Stephen Schlachter, Paul Winship, Chris Steele
Abstract: Novel compounds of the structural formula (I), and the pharmaceutically acceptable salts thereof, are inhibitors of Nav1.8 channel activity and may be useful in the treatment, prevention, management, amelioration, control and suppression of diseases mediated by Nav1.8 channel activity. The compounds of the present invention may be useful in the treatment, prevention or management of pain disorders, cough disorders, acute itch disorders, and chronic itch disorders.
Type:
Grant
Filed:
May 24, 2022
Date of Patent:
January 14, 2025
Assignee:
Merck Sharp & Dohme LLC
Inventors:
Ashok Arasappan, Ian M. Bell, Michael J. Breslin, Christopher James Bungard, Christopher S. Burgey, Harry R. Chobanian, Jason M. Cox, Anthony T. Ginnetti, Deodial Guy Guiadeen, Kristen L. G. Jones, Mark E. Layton, Hong Liu, Jian Liu, James J. Perkins, Shawn J. Stachel, Linda M. Suen-Lai, Zhe Wu
Abstract: This disclosure is directed to substituted Imidazolo[2,1-b]oxazole, Imidazolo[2,1-b]thiazole, Imidazolo[2,1-b]oxadiazole, Imidazolo[2,1-b]oxadiathiazole derivatives of compounds that are antagonists of orexin receptors, and which are useful in the treatment or prevention of neurological and psychiatric disorders and diseases in which orexin receptors are involved or implicated. 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 orexin receptors are involved.
Abstract: Donor-acceptor type thermally activated delayed fluorescent emitters based on imidazo[1,2-F]phenanthridine and analogues for full color displays and lighting applications.
Type:
Grant
Filed:
September 1, 2022
Date of Patent:
January 7, 2025
Assignee:
Arizona Board of Regents on behalf Arizona State University
Abstract: The invention relates to 1,2,5-benzothiadiazepine derivatives of formula (I). These compounds are bile acid modulators having apical sodium-dependent bile acid transporter (ASBT) and/or liver bile acid transport (LBAT) inhibitory activity. The invention also relates to pharmaceutical compositions comprising these compounds and to the use of these compounds in the treatment of cardiovascular diseases, fatty acid metabolism and glucose utilization disorders, gastrointestinal diseases and liver diseases.
Type:
Grant
Filed:
February 3, 2023
Date of Patent:
January 7, 2025
Assignee:
Albireo AB
Inventors:
Per-Göran Gillberg, Jan Mattsson, Ingemar Starke, Santosh S. Kulkarni
Abstract: The present disclosure relates to mTOR inhibitors. Specifically, the embodiments are directed to compounds and compositions inhibiting mTOR, methods of treating diseases mediated by mTOR, and methods of synthesizing these compounds.
Type:
Grant
Filed:
April 10, 2023
Date of Patent:
January 7, 2025
Assignee:
REVOLUTION MEDICINES, INC.
Inventors:
Christopher Michael Semko, Gang Wang, G. Leslie Burnett, James Bradley Aggen, Gert Kiss, James Joseph Cregg, Micah James Evans Gliedt, Jennifer Pitzen, Julie Chu-Li Lee, Walter Won, Arun P. Thottumkara, Adrian Liam Gill
Abstract: This disclosure is directed to substituted Imidazolo[2,1-b]oxazole, Imidazolo[2,1-b]thiazole, Imidazolo[2,1-b]oxadiazole, Imidazolo[2,1-b]oxadiathiazole derivatives of compounds that are antagonists of orexin receptors, and which are useful in the treatment or prevention of neurological and psychiatric disorders and diseases in which orexin receptors are involved or implicated. 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 orexin receptors are involved.
Abstract: Disclosed herein are compounds effective for activation of Tie-2 and inhibition of HPTP-beta. The compounds can provide effective therapy for vascular disorders that can include, for example, retinopathies, ocular edema, and ocular neovascularization.
Abstract: Novel pyrido[3,4-e][1,2,4]triazolo[4,3-c]pyrimidine compounds, a method of synthesizing said compounds, a pharmaceutical composition comprising said compounds and a suitable carrier, and a method of using the compounds. The pyrido[3,4-e][1,2,4]triazolo[4,3-c]pyrimidine compounds, identified as CK2 inhibitors, are useful as anticancer and/or antitumor agents, and as agents for treating other kinase-associated conditions including inflammation, pain, and certain immunological disorders, and other types of diseases such as diabetes, viral infection, neurodegenerative diseases.
Abstract: Oxazolidinones having structures represented by structural formula I, preparation methods therefor, and pharmaceutical uses thereof, in particular an application of said compounds and salts or compositions thereof in the treatment of a bacterial infection. In the formula: R1 is a methyl group, an ethyl group, a propyl group, a cyclopropyl group, or a vinyl group; R2 is F; and R3 is F, CH3, C2H5, CF3, CHF2, CH2F, or a cyclopropyl group.
Abstract: The present invention relates to a medicament for treating or preventing central nervous system disease whose cause is related to abnormal aggregation of proteins in the brain, which comprises as an active ingredient a compound of formula (1) or a pharmaceutically acceptable salt thereof, wherein R1 and R2 are hydrogen, etc., R3 and R4 are hydrogen, C1-6 alkyl, etc., R5 is halogen, C1-6 alkyl, etc., R6 is hydrogen, halogen, etc., X is oxygen, etc., Y is carbon, etc., m and n are an integer of 0, 1, etc., r and s are 0, 1, 2, etc., Hy is pyridine ring, etc., which has an action of suppressing or reducing the accumulation of abnormal aggregation of proteins in the brain.
Abstract: Provided herein, inter alia, are splice modulator compounds. The compounds include optically pure, stereospecific analogs of FD-895. The methods provided herein allow, for example, for scalable preparation of said compounds, and further allow, for example, use of said compounds for inhibiting spliceosome activity.
Type:
Grant
Filed:
January 12, 2022
Date of Patent:
December 24, 2024
Assignee:
THE REGENTS OF THE UNIVERSITY OF CALIFORNIA
Inventors:
Michael D. Burkart, Warren C. Chan, James J. La Clair, Kelsey A. Trieger, Catriona Jamieson
Abstract: Disclosed herein is a solid Form A of 1-(6-ethyl-8-fluoro-4-methyl-3-(3-methyl-1,2,4-oxadiazol-5-yl)quinolin-2-yl)-N-(tetrahydro-2H-pyran-4-yl)piperidin-4-amine hydrochloride exhibiting at least X-ray lines (in degrees 2?±0.2) at 4.30, 8.59, 12.88, 18.82 and 21.34 in a powder diffraction pattern when measured using Cu K? radiation. The solid Form A is an antagonist of the kappa-opioid receptor (KOR) and is useful for treating conditions that benefit from the same. Compositions comprising the solid Form A, as well as related methods of use are also disclosed.
Type:
Grant
Filed:
July 3, 2024
Date of Patent:
December 24, 2024
Assignee:
Neumora Therapeutics, Inc.
Inventors:
Brian Van Dyke, Yawei Shi, Mengya Ma, Lori Jean Van Orden
Abstract: Provided are a phenanthroimidazole derivative, and a preparation method therefor, and an application thereof. The phenanthroimidazole derivative has a structural formula as shown in Formula (I), R being an electron donor group, wherein by taking a phenanthroimidazole group containing a trifluoromethyl phenyl group as an electron acceptor, and in virtue of the properties of the specific electron donor group R, the phenanthroimidazole derivative containing a light-absorbing photosensitive group of a series D-?-A structure is synthesized, and can be used as a photoinitiator, which is used in the technical field of UV light-curing systems or 3D printing.
Abstract: A structural analog of Cyclotheonellazole A, and a synthetic method therefor and an application method thereof are provided. A compound with a structure of formula (I) and a pharmaceutically acceptable salt thereof are provided. The formula (I) is as follows: R1, R2, R3 and R4 are independently selected form the group consisting of H, a C1-C6 alkyl group, a C1-C6 alkoxy group, a halogen group, a hydroxyl group, an amino group, a nitro group, a cyano group, and a sulfydryl group. Based on the total synthetic route of Cyclotheonellazole A, the classical reverse synthesis analysis is utilized, the structural modification is purposefully carried out, a mother nucleus of the natural product remains unchanged, and the structural analog 1a is obtained by replacing a left side chain with a simple formylamine, thereby confirming the excellent protease inhibitory activity thereof, and having a strong application prospect in the pharmaceutical industry.
Type:
Grant
Filed:
December 4, 2023
Date of Patent:
December 10, 2024
Assignee:
The Second People's Hospital of Shenzhen (Shenzhen Institute of Geriatrics)
Abstract: A ketoamide compound and a preparation method, a pharmaceutical composition, and a use thereof. Specifically, the ketoamide compound shown in formula (A), a racemate, an enantiomer, or a diastereoisomer thereof, or any mixture of same, or a pharmaceutically active metabolite thereof, or a pharmaceutically acceptable salt, solvate, or prodrug thereof. The ketoamide compound can effectively inhibit coronavirus or Ebola virus, and thereby implement the prevention or treatment of diseases related to coronavirus or diseases related to Ebola virus.
Type:
Grant
Filed:
August 9, 2019
Date of Patent:
November 26, 2024
Assignees:
Shanghai Institute of Materia Medica, Chinese Academy of Sciences, Fudan University
Abstract: The present invention relates to a compound of the Formula: and pharmaceutically salts thereof. The compound of the present invention inhibits Pol?. This novel therapeutic compound is therefore useful for the treatment and/or prevention of diseases and conditions in which Pol? activity is implicated, such as, for example but not limited to, the treatment and/or prevention of cancer. The present invention also relates to pharmaceutical compositions comprising the novel therapeutic compound defined herein, to processes for synthesising the compound and to their use for the treatment of diseases and/or conditions in which Pol? activity is implicated.
Type:
Grant
Filed:
March 8, 2024
Date of Patent:
November 19, 2024
Assignee:
Breakpoint Therapeutics GmbH
Inventors:
Andrea Guerrero Corella, Stuart Robert Flanagan, Jonathan Hollick, Julien Gilbert Jacques Malassis, Matthew Raymond Smith, Ian Andrew Yule, Jonathan Mark Bentley