Abstract: A 7-(4-((5-(2-bromobenzylideneamino)-2-thioxo-1,3,4-thiadiazol-3(2H)-yl)methyl)piperazin-1-yl)-1-cyclopropyl-6-fluoro-4-oxo-1,4-dihydroquinoline-3-carboxylic acid compound, its synthesis, and its use as an anti-inflammation agent.
Type:
Grant
Filed:
October 9, 2023
Date of Patent:
March 5, 2024
Assignee:
KING FAISAL UNIVERSITY
Inventors:
Mai Mostafa Khalaf Ali, Hany Mohamed Abd El-Lateef Ahmed, Amer A. Amer, Antar Ahmed Abdelhamid Ahmed
Abstract: A P2X3 and/or P2X2/3 receptor antagonist of formula (I), a pharmaceutical composition comprising the same, and a use thereof in preparing a drug for preventing or treating a disease mediated by the P2X3 and/or P2X2/3 receptor antagonist.
Type:
Grant
Filed:
May 27, 2022
Date of Patent:
March 5, 2024
Assignee:
BEIJING TIDE PHARMACEUTICAL CO., LTD.
Inventors:
Yanping Zhao, Hongjun Wang, Gong Li, Xiang Li, Yuanyuan Jiang, Kai Liu, Yeming Wang, Liying Zhou, Yanan Liu, Ning Shao, Fengping Xiao
Abstract: This disclosure relates to salt forms of compounds capable of activating PPAR? for use in drug substance and drug product development, and related compositions and methods.
Abstract: Methods and compositions for agonizing a type-2 orexin receptor (OX2R) in a cell determined to be in need thereof, including the general method of (a) administering to a subject a cyclic guanidinyl OX2R agonist and (b) detecting a resultant enhanced wakefulness or increased resistance to diet-induced accumulation of body fat, or abbreviated recovery from general anesthesia or jet lag.
Type:
Grant
Filed:
October 21, 2022
Date of Patent:
February 20, 2024
Assignee:
Board of Regents, The University of Texas System
Inventors:
Jef De Brabander, Daniel Rosenbaum, Qiren Liang, Wentian Wang
Abstract: The present disclosure relates to novel nucleotide precursors and nucleotide analogs that can be incorporated into oligonucleotides, including double-stranded oligonucleotides such as siRNAs. Oligonucleotides containing these analogs have superior biological activity, for example, increased in vitro stability and improved in vivo potency especially duration of action. The improved oligonucleotides are useful for silencing (e.g., reducing or eradicating) the expression of a target gene. In particular embodiments, this invention encompasses specific nucleotide analogs to be included in double-stranded RNAs (dsRNAs), and especially in siRNAs, that can hybridize to messenger RNAs (mRNAs) of interest, so as to reduce or block the expression of target genes of interest. The present compounds have general formula (I), wherein each of Ra, Rb, Rc and Rd is independently, H or a (C1-C6) alkyl group and B is a heterocyclic nucleobase.
Abstract: The present disclosure relates to stimulators of soluble guanylate cyclase (sGC), pharmaceutically acceptable salts, pharmaceutical formulations comprising them as well as their phosphate ester prodrugs, and their uses alone or in combination with one or more additional agents, for treating various diseases, wherein an increase in the concentration of nitric oxide (NO) and/or an increase in the concentration of cyclic Guanosine Monophosphate (cGMP), or both, or the upregulation of the NO pathway is desirable. The compounds are of Formula I.
Type:
Grant
Filed:
December 19, 2018
Date of Patent:
February 13, 2024
Assignee:
Tisento Therapeutics Inc.
Inventors:
Glen Robert Rennie, Paul Allan Renhowe, Takashi Nakai, Ara Mermerian, Helen Cumberbatch
Abstract: A process prepares a compound containing at least one cyclic monothiocarbonate group, wherein a salt of an acidic compound with at least one acidic hydrogen atom is reacted with a compound of formula (I), wherein one of the groups R1 to R4 is a group of formula (II), -A-X, with A representing an organic group with at least one carbon atom and X representing a halide, and the remaining groups R1 to R4 independently from each other represent hydrogen or an organic group with 1 to 50 carbon atoms.
Type:
Grant
Filed:
January 17, 2020
Date of Patent:
February 13, 2024
Assignee:
BASF SE
Inventors:
Peter Rudolf, Indre Thiel, Markus Jegelka, Bernd Bruchmann, Elliot Christ
Abstract: Fused and bridged compounds of Formula (I), and pharmaceutically acceptable salts, isotopes, N-oxides, solvates, and stereoisomers thereof, pharmaceutical compositions containing them, methods of making them, and methods of using them including methods for treating disease states, disorders, and conditions associated with MGL modulation, such as those associated with pain, psychiatric disorders, neurological disorders (including, but not limited to major depressive disorder, treatment resistant depression, anxious depression, autism spectrum disorders, Asperger syndrome, bipolar disorder), cancers and eye conditions: wherein R1a, R1b, R2, and R3, are defined herein.
Type:
Grant
Filed:
March 25, 2021
Date of Patent:
February 6, 2024
Assignee:
Janssen Pharmaceutica NV
Inventors:
Michael K. Ameriks, Brian Ngo Laforteza, Suchitra Ravula, Jamie M. Schiffer, Brice M. Stenne
Abstract: The present invention relates to compounds of formula (1): wherein Q is selected from O or S; R1 is a 5-membered nitrogen-containing heteroaryl group substituted with R6 and optionally further substituted; R2 is an alpha, alpha?-substituted cyclic group which may optionally be further substituted; R3 and R4 are each independently hydrogen, halogen, —OH, —NH2, —CN, —R5, —OR5, —NHR5 or —N(R5)2; or R3 and R4 together with the carbon atom to which they are attached may form a 3 to 7 membered saturated or unsaturated, optionally substituted cyclic group; R5 is independently an optionally substituted C1-C4 alkyl group; and R6 is any group comprising a nitrogen atom. 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:
March 1, 2019
Date of Patent:
January 30, 2024
Assignee:
INFLAZOME LIMITED
Inventors:
David Miller, Jimmy Van Wiltenburg, Matthew Cooper
Abstract: Tropomyosin-related kinase inhibitors (Trk inhibitors) are small molecule compounds useful in the treatment of disease. Trk inhibitors can be used as pharmaceutical agents and in pharmaceutical compositions. Trk inhibitors are useful in the treatment of inflammatory diseases, autoimmune disease, defects of bone metabolism and/or cancer, and are particularly useful in the treatment of osteoarthritis (OA), pain, and pain associated with OA. Trk inhibitors are also useful for inhibiting tropomyosin-related kinase A (TrkA), tropomyosin-related kinase B (TrkB), tropomyosin-related kinase C (TrkC), and/or c-FMS (the cellular receptor for colony stimulating factor-1 (CSF-1)).
Type:
Grant
Filed:
August 8, 2022
Date of Patent:
January 23, 2024
Assignee:
GENZYME CORPORATION
Inventors:
John L. Kane, Jr., Gloria Matthews, Markus Metz, Michael Kothe, Jinyu Liu, Andrew Scholte
Abstract: The present invention discloses a pyridinylcyanoguanidine derivative or a pharmaceutically acceptable salt thereof, which is useful as an NAMPT inhibitor, and useful as a potential agent for the chemotherapy of a variety of diseases associated with abnormal NAD+ expression. The pyridinylcyanoguanidine derivative has a parent structure including cyanoguanidine attached to piperazine or pyrrolidine by an intermediate aliphatic chain, to which a side arylformyl (or heterocyclylformyl) group and pyridinyl (or substituted pyridinyl) group are attached. This structure comes from the structural optimization of FK866, a high-efficiency NAMPT inhibitor. In the structure, the substituted formyl piperazine and substituted formyl pyrrolidine are the further optimizations on the basis of FK866, which strengthens the interaction with NAMPT.
Abstract: The present invention provides a curable composition containing a compound represented by General Formula A and a compound represented by General Formula B. ArL-Sp-Pol)n??(General Formula A) In General Formula A, Ar represents an n-valent group containing a nitrogen-containing fused aromatic ring as a partial structure; L represents a linking group such as —O— and —C(?O)O—; Sp represents a single bond or a divalent linking group; Pol represents a hydrogen atom or a polymerizable group; n represents 1 or 2; and the compound represented by General Formula A has at least one polymerizable group. In General Formula B, R?, R?, and R?? are each independently a hydrogen atom or a substituent; R? and R? or R? and R?? may be bonded to each other to form a ring that may have a substituent; and W is a hydrogen atom or a substituent.
Abstract: A gold(III) complex, a conjugate of the gold(iII) complex, a pharmaceutical composition comprising the gold(III) complex and uses and a process for preparing the gold(III) complex. The complex comprises a group of (S{circumflex over (?)}C)-cyclometallated gold(III) complexes containing a 1,1-dithio ligand, which exhibit antibacterial activity against multiresistant microorganisms or against biofilm activity or biofilm disruption. The gold(III) complex has efficacy against a variety of microorganisms and low toxicity.
Type:
Grant
Filed:
April 29, 2019
Date of Patent:
January 9, 2024
Inventors:
Sara Maria Soto Gonzalez, Carlos Ratia Loncan, Virginio Cepas Lopez, Yuly Lopez Cubillos, Fernando Lopez Ortiz, Maria Jose Iglesias Valdes-Solis, Raquel Maria Gonzalez Soengas
Abstract: The invention relates to pyrazolo-pyridine compounds which inhibit mitogen-activated protein kinase kinase 4 (MKK4) and in particular, selectively inhibit MKK4 over protein kinases JNK1 and MKK7. The compounds are useful for promoting liver regeneration or reducing or preventing hepatocyte death. They are further useful for treating osteoarthritis or rheumatoid arthritis, or CNS-related diseases.
Type:
Grant
Filed:
January 30, 2019
Date of Patent:
January 2, 2024
Assignee:
HepaRegeniX GmbH
Inventors:
Bent Praefke, Philip Klövekorn, Roland Selig, Wolfgang Albrecht, Stefan Laufer
Abstract: The present disclosure relates generally to eukaryotic initiation factor 2B modulators, or a pharmaceutically acceptable salt, stereoisomer, mixture of stereoisomers or prodrug thereof, and methods of making and using thereof.
Type:
Grant
Filed:
November 19, 2021
Date of Patent:
December 26, 2023
Assignee:
Denali Therapeutics Inc.
Inventors:
Robert A. Craig, II, Javier de Vicente Fidalgo, Anthony A. Estrada, Jianwen A. Feng, Brian M. Fox, Christopher R. H. Hale, Katrina W. Lexa, Maksim Osipov, Travis Remarchuk, Zachary K. Sweeney
Abstract: The present invention relates to reagents which are suitable to be used in mass spectrometry as well as methods of mass spectrometric determination of analyte molecules using said reagents.
Type:
Grant
Filed:
January 21, 2021
Date of Patent:
December 19, 2023
Assignee:
Roche Diagnostics Operations, Inc.
Inventors:
Dieter Heindl, Hans-Peter Josel, Uwe Kobold, Christoph Seidel, Martin Rempt, Andreas Leinenbach, Giuseppe Prencipe, Silvia Baecher, Simon Ferdinand Loibl, Anna-Skrollan Geiermann, Jelena Milic, Nicole Pirkl
Abstract: This invention relates to compounds of formula (I) and methods of treatment using the compounds. The compounds of the invention can be used in combination with antibacterial agents to treat bacterial infections. More specifically, the compounds of formula (I) can be used in combination with a class of antibacterial agents known as carbapenems. The novel compounds of the present invention are enzyme inhibitors and more particularly are metallo-?-lactamase inhibitors.
Type:
Grant
Filed:
September 16, 2022
Date of Patent:
December 19, 2023
Assignee:
INFEX Therapeutics Limited
Inventors:
Ian Cooper, David Orr, Andrew Wilkinson, Jonathan Finlayson, Adam Bunt, Pia Appelqvist, Hans Wallberg, Fredrik Wångsell