Abstract: There is provided an alkali metal salt of 4-chloro-N-[2-[(4-chlorophenyl)methyl]-3-oxo-1,2,4-thiadiazol-5-yl]benzamide and formulations thereof. This salt finds particular utility in the treatment or prevention of a disorder or condition ameliorated by the activation of AMPK.
Abstract: The present invention relates to a pharmaceutical composition for the prevention or treatment of solid cancers or blood cancers such as acute leukemia or chronic leukemia, including, as an active ingredient, a 1,2-naphthoquinone derivative compound or a pharmaceutically acceptable salt thereof, wherein the 1,2-naphthoquinone derivative compound has excellent effects in killing cancer cells of various solid cancers, acute leukemia, and chronic leukemia, and thus, can be useful as a pharmaceutical composition for the prevention or treatment of cancer, in particular, solid cancers, acute leukemia, or chronic leukemia.
Type:
Grant
Filed:
April 4, 2019
Date of Patent:
June 27, 2023
Assignee:
YUNGJIN PHARM. CO., LTD.
Inventors:
Ki Ryang Kweon, Jun Young Heo, Min Ho Shong, Jeong Su Han, Min Jeong Ryu
Abstract: Disclosed are compounds of formula I as described herein, and pharmaceutically acceptable salts thereof. The compounds are inhibitors of plasma kallikrein. Also provided are pharmaceutical compositions comprising at least one compound of the invention, and methods involving use of the compounds and compositions of the invention in the treatment and prevention of diseases and conditions characterized by unwanted plasma kallikrein activity.
Type:
Grant
Filed:
November 9, 2021
Date of Patent:
June 27, 2023
Assignee:
BioCryst Pharmaceuticals, Inc.
Inventors:
Pravin L. Kotian, Yarlagadda S. Babu, Minwan Wu, Venkat R. Chintareddy, V. Satish Kumar, Weihe Zhang
Abstract: An object of the present invention is to provide a novel plant growth inhibiting agent and a plant growth inhibiting method using the same. The plant growth inhibiting agent of the present invention comprises, as an active ingredient, a compound represented by the following formula (I?) and/or a salt thereof. In the formula (I?), R1a represents a substituted or unsubstituted C1 to C20 alkyl group, a substituted or unsubstituted C6 to C14 aryl group, a substituted or unsubstituted C3 to C13 heteroaryl group, or the like; R2 represents a substituted or unsubstituted C1 to C20 alkylene group, a substituted or unsubstituted C6 to C14 arylene group, or the like; R3a represents OH, a substituted or unsubstituted C1 to C6 alkoxy group, or the like; X represents an oxygen atom; Y represents a substituent; q represents any integer of 0 to 3; n represents 0 or 1; and m represents 0 or 1.
Type:
Grant
Filed:
September 10, 2021
Date of Patent:
June 27, 2023
Assignees:
National University Corporation Kumamoto University, Nippon Soda Co., Utd.
Inventors:
Hayato Ishikawa, Tokio Tani, Shinichiro Sawa, Takashi Ishida, Yusuke Fukushima, Jun Inagaki
Abstract: The invention relates to functionalised dioxaborolane or dioxaborinane derivatives of formula (I), wherein R1 is covalently bonded to the boron atom by a carbon atom; one of R2, R3, R?3 or R4 is a radical of formula —X; or one of R1, R2, R3, R?3 or R4 is a radical of formula —X; and X is a functionalised radical. The invention relates to the method for preparing same and the uses thereof.
Type:
Grant
Filed:
January 6, 2022
Date of Patent:
June 20, 2023
Assignees:
ECOLE SUPERIEURE DE PHYSIQUE ET DE CHIMIE INDUSTRIELLES DE LA VILLE DE PARIS, CENTRE NATIONAL DE LA RECHERCHE SCIENTIFIQUE
Abstract: Provided herein are dibenzocyclooctyne compounds useful as reagents in 1,3-dipolar cycloaddition reactions, and methods for their preparation.
Type:
Grant
Filed:
April 29, 2022
Date of Patent:
June 13, 2023
Assignee:
Massachusetts Institute of Technology
Inventors:
Ronald T. Raines, Brian Gold, Jesus M. Dones, Nile S. Abularrage, Brian James Graham
Abstract: Provided are methods useful for preventing and mitigating radiation injury, including acute radiation syndrome, comprising administering to a subject a therapeutically effective amount of a compound represented by formula I or a pharmaceutically acceptable salt thereof, wherein Z is —O— or —N(H)—.
Type:
Grant
Filed:
April 25, 2022
Date of Patent:
June 13, 2023
Assignees:
Georgetown University, The Board of Regents of the University of Oklahoma
Inventors:
Milton L. Brown, Yali Kong, Courtney Houchen, Sripathi M. Sureban, Parthasarathy Chandrakesan
Abstract: Disclosed crystalline Siponimod fumaric acid, solid state forms (polymorphs) thereof, processes for preparation thereof and pharmaceutical compositions thereof.
Type:
Grant
Filed:
January 22, 2019
Date of Patent:
June 13, 2023
Assignee:
TEVA PHARMACEUTICALS INTERNATIONAL GMBH
Inventors:
Marisa Martinelli, Pavel Kolesa, Maurizio Paiocchi, Matteo Toso, Roberta Volonté, Piero Paravidino
Abstract: Provided herein are compounds and pharmaceutical compositions comprising said compounds that are useful for treating cancers. Specific cancers include those that are mediated by YAP/TAZ or those that are modulated by the interaction between YAP/TAZ and TEAD.
Type:
Grant
Filed:
May 15, 2019
Date of Patent:
May 30, 2023
Assignee:
VIVACE THERAPEUTICS, INC.
Inventors:
Andrei W. Konradi, Tracy Tzu-Ling Tang Lin
Abstract: The invention provides a compound of Formula I, Pharmaceutical compositions comprising such compounds and the use of such compounds in the treatment of phosphoinositide 3-kinase related diseases and disorders such as cancer. The instant application further relates to the treatment of histone deacetylase related disorders and diseases related to both histone deacetylase and phosphoinositide 3-kinase.
Abstract: One embodiment of the invention relates to the treatment of diseases associated with increased butyrylcholinesterase (BuChE) enzyme activity such Alzheimer's Disease (AD), involving administering an effective amount of a compound selected from a group of new N, N?-disubstituted benzylamine derivatives (1-8) of 4-aminoantipyrine (ampyrone). The kinetic studies of two potent compounds 4-(Bis(4-iodobenzyl) amino)-1,5-dimethyl-2-phenyl-1,2-dihydro-3H-pyrazol-3-one (5) (IC50=2.43±0.4 and Ki=5.67±0.5 ?M) and 4-(Bis(2-bromobenzyl) amino)-1,5-dimethyl-2-phenyl-1,2-dihydro-3H-pyrazol-3-one (6) (IC50=0.7±0.2 and Ki=2.4±0.4 ?M), revealed them as a competitive and a non-competitive inhibitor of BuChE, respectively. Galantamine Hydrobromide was used as standard inhibitor with IC50=40.83±0.4 and Ki=21.5±0.7 ?M (Mixed type Inhibitor). The metabolite of aminophenazone, 4-aminoantipyrine (A) is also being reported here as an inhibitor of BuChE for the first time.
Type:
Grant
Filed:
August 9, 2021
Date of Patent:
May 9, 2023
Inventors:
Hina Siddiqui, Muhammad Iqbal Choudhary, Atia-tul- Wahab, Atta-ur- Rahman, Fazila Rizvi, Sheeba Wajid
Abstract: The present invention sets forth new compounds that potently block activation of ABA receptors. In some aspects, these compounds can be used to enhance germination of crop seeds to stand establishment and to increase transpiration and photosynthetic yields when water is not limiting plant growth.
Type:
Grant
Filed:
June 19, 2020
Date of Patent:
May 9, 2023
Assignee:
The Regents of The University of California
Abstract: Provided herein are azo prodrugs of small-molecule isoindoline-1,3-diones and isoindoles anti-inflammatory inhibitors according to formula IA, in particular PDE4 inhibitors, which prodrugs can be administered orally to a subject in need thereof, whereby the prodrugs are cleaved in the colon and the PDE4 inhibitor released.
Abstract: In one aspect, the invention relates to compounds having the formula: where X, Ra, Rb, R2, and R7 are as defined in the specification, or a pharmaceutically acceptable salt thereof. These compounds are prodrugs of compounds having neprilysin inhibition activity. In another aspect, the invention relates to pharmaceutical compositions comprising these compounds; methods of using these compounds; and processes and intermediates for preparing these compounds.
Abstract: Disclosed are compounds of Formula 1, including all geometric and stereoisomers, tautomers, N-oxides, and salts thereof, wherein A, Q, R1, R2, R3, R4, W and Y are as defined in the disclosure. Also disclosed are compositions containing the compounds of Formula 1 and methods for controlling plant disease caused by a fungal pathogen comprising applying an effective amount of a compound or a composition of the invention.
Type:
Grant
Filed:
November 5, 2019
Date of Patent:
April 25, 2023
Assignee:
FMC Corporation
Inventors:
James Francis Bereznak, Andrew Edmund Taggi, Stephen P. Bolgunas
Abstract: The present invention provides a novel dosage principle for compounds of formula I and pharmaceutically acceptable derivatives thereof as defined in the claims, wherein said compound or pharmaceutically acceptable derivative thereof is intravenously administered to said patient over a period of at least about 8 hours, wherein the dose of the compound of formula I or pharmaceutically acceptable derivative thereof is at least the molar equivalent of about 45 mg/m2 of the dihydrochloride salt of the compound of formula I-B as defined in the claims.
Type:
Grant
Filed:
May 15, 2018
Date of Patent:
April 25, 2023
Assignee:
Basilea Pharmaceutica International AG
Inventors:
Marc Engelhardt, Anne Schmitt-Hoffmann, Patrice Larger
Abstract: The compounds of the present invention are represented by the following compounds having Formula (I): where the substituents R, R1-R5, k, m, n, and q are as defined herein. These compounds are used in the treatment of cancer, immunologic disorders, autoimmune disorders, neurodegenerative disorders, or inflammatory disorders, infectious disease, or for providing immunosuppression for transplanted organs or tissues.
Type:
Grant
Filed:
February 17, 2021
Date of Patent:
April 18, 2023
Assignee:
CORNELL UNIVERSITY
Inventors:
Gang Lin, Carl Nathan, Pradeep K. Singh, Lei Shi, Laura Kirkman
Abstract: The present invention relates to compounds of formula (I): wherein Q is selected from O or S; R1 is a saturated or unsaturated hydrocarbyl group, wherein the hydrocarbyl group may be straight-chained or branched, or be or include cyclic groups, wherein the hydrocarbyl group may optionally be substituted, and wherein the hydrocarbyl group may optionally include one or more heteroatoms N, O or S in its carbon skeleton; and R2 is a cyclic group substituted at the a-position, wherein R2 may optionally be further substituted. The present invention further relates to salts, solvates and prodrugs of such compounds, to pharmaceutical compositions comprising such compounds, and to the use of such compounds in the treatment and prevention of medical disorders and diseases, most especially by the inhibition of NLRP3.
Type:
Grant
Filed:
October 3, 2018
Date of Patent:
April 11, 2023
Assignee:
INFLAZOME LIMITED
Inventors:
David Miller, Stephen Thom, Stephen St-Gallay, Jonathan Shannon, Paul Leeson
Abstract: Provided herein are unsymmetrical bis(azolium) salts, unsymmetrical CCC-NHC metal complexes, and methods of forming the same. The unsymmetrical bis(azolium) salts include a central aryl ring that is substituted with two heterocyclic rings in an ortho, meta, or para fashion. The unsymmetrical CCC-NHC metal complexes include metalated unsymmetrical bis(azolium) salts. The method of forming the unsymmetrical CCC-NHC metal complexes includes reacting a dihalogenated benzene with a first azole to form a mono(azole)benzene, reacting the mono(azole)benzene with a second azole to form an unsymmetrical bis(azole)benzene, alkylating the unsymmetrical bis(azole)benzene to form an unsymmetrical bis(azolium) salt, and metalating the unsymmetrical bis(azolium) salt to form the unsymmetrical CCC-NHC metal complex. Also provided are a bis-ligated CCC-NHC metal complex and an unsymmetrical bimetallic complex.
Type:
Grant
Filed:
February 22, 2021
Date of Patent:
April 4, 2023
Assignee:
Mississippi State University
Inventors:
Thedford Keith Hollis, Charles Edwin Webster
Abstract: The present invention generally relates to 6-amino-2,4-dihydropyrano [2,3-c] pyrazoles as a ubiquitin specific protease 7 (USP7) inhibitor useful for the treatment of diseases mediated by malfunction of USP7, such as inflammation, cancer, and immunological disorders. The invention described herein also pertains to pharmaceutical compositions and methods for treating diseases mediated by malfunction of USP7, in mammals using compounds disclosed herein.