Abstract: The invention provides novel phosphorus imidazoquinoline amine derivatives, having agonistic activities to Toll-like receptors (TLRs), in particular TLR7 and/or TLR8, pharmaceutical compositions thereof, and methods of treatment, reduction or prevention of certain diseases or conditions mediated by or associated with TLR7 and/or TLR8, e.g., cancer, graft rejection, autoimmunity, inflammation allergy, asthma, infection, sepsis, and immunodeficiency.
Abstract: Provided herein are small molecule activators of Nicotinamide Phosphoribosyltransferase (NAMPT), compositions comprising the compounds, and methods of using the compounds and compositions.
Type:
Grant
Filed:
January 9, 2018
Date of Patent:
September 27, 2022
Assignee:
SANFORD BURNHAM PREBYS MEDICAL DISCOVERY INSTITUTE
Inventors:
Stephen Gardell, Anthony B. Pinkerton, Eduard Sergienko, Hampton Sessions
Abstract: The invention relates to a composition and use of the composition in the treatment of a disorder, for example, a neurological disease associated with retinoid signaling. The invention also includes the use of a retinoid encapsulated in nanoparticles. The retinoid encapsulated nanoparticles are adapted to increasing lifespan and conferring neuroprotective effects such as preserving motor units, reducing motor impairment, or reducing neuroinflammation in a subject.
Type:
Grant
Filed:
June 15, 2018
Date of Patent:
September 20, 2022
Assignee:
Dignity Health
Inventors:
Rachael Sirianni, David Alexandro Medina, Eugene Chung
Abstract: This invention addresses tetrahydro-N, N-dimethyl-2,2diphenyl-3-furanmethanamine hydrochloride (ANAVEX2-73, AV2-73, or A2-73) in a method of treatment for neurodevelopmental disorders. Particular reference is made to the treatment of autism spectrum disorder, cerebral palsy, Rett syndrome, Angelman syndrome, Williams syndrome, pervasive developmental disorder not otherwise specified (PDD-NOS), childhood disintegrative disorder, and Smith-Magenis syndrome. Additional reference is made to multiple sclerosis.
Abstract: The invention provides capsaicinoid prodrug compounds, pharmaceutical compositions, and their use in the treatment of medical conditions, such as pain, and in agonizing TRPV1 activity.
Abstract: Thalidomide analogs and methods of using the thalidomide analogs are disclosed. Some embodiments of the disclosed compounds exhibit anti-angiogenic and/or anti-inflammatory activity. Certain embodiments of the disclosed compounds are non-teratogenic.
Type:
Grant
Filed:
October 29, 2020
Date of Patent:
September 13, 2022
Assignees:
The USA, as represented by the Secretary, Department of Health and Human Services, University Court of the University of Aberdeen
Inventors:
Nigel H. Greig, Weiming Luo, David Tweedie, Neil Vargesson, Shaunna Beedie, William Douglas Figg
Abstract: The present invention relates to certain compounds, in particular, indole derivatives that function as inhibitors of bacterial metallo-beta-lactamases. The present invention also relates to processes for the preparation of these compounds, to pharmaceutical compositions comprising them, and to their use in the treatment of a bacterial infection.
Type:
Grant
Filed:
November 30, 2016
Date of Patent:
September 13, 2022
Assignee:
Oxford University Innovation Limited
Inventors:
Jürgen Brem, Anna M. Rydzik, Michael A. McDonough, Christopher J. Schofield, Angus Morrison, Joanne Hewitt, Andrew Pannifer, Philip Jones
Abstract: Described herein are small molecule splicing modulator compounds that modulate splicing of mRNA, such as pre-mRNA, encoded by genes, and methods of use of the small molecule splicing modulator compounds for modulating splicing and treating diseases and conditions.
Type:
Grant
Filed:
October 15, 2021
Date of Patent:
September 6, 2022
Assignee:
Skyhawk Therapeutics, Inc.
Inventors:
Michael Luzzio, Kathleen McCarthy, William Haney
Abstract: Provided in some embodiments are titration packages, kits, and methods of treating pulmonary arterial hypertension comprising prescribing and/or administering to a patient in need thereof 2-(((1r,4r)-4-(((4-chloropbenyl)(pbenyl)carbamoyloxy)methyl)cyclohexyi)methoxy)acetic acid (Compound 1), or a pharmaceutically acceptable salt, hydrate, or solvate thereof, via a titration scheme that comprises the up-titration of Compound 1, or a pharmaceutically acceptable salt, hydrate, or solvate thereof, over a period of no more than about nine weeks until an optimized dose is administered.
Abstract: The invention provides a compound of formula (I): or a pharmaceutically-acceptable salt thereof, that is an inhibitor of JAK kinases. The invention also provides pharmaceutical compositions comprising such compound, a crystalline form, methods of using such compound to treat inflammatory skin diseases and other diseases, and processes and intermediates useful for preparing such compound.
Type:
Grant
Filed:
March 30, 2021
Date of Patent:
August 23, 2022
Assignee:
THERAVANCE BIOPHARMA R&D IP, LLC
Inventors:
Jennifer Kozak, Ryan Hudson, Gary E. L. Brandt, Robert Murray McKinnell
Abstract: Described herein are embodiments of squarylium compounds for use as filters in light-emitting and/or display devices. One problem of known quarylium dyes is that strong nucleophiles can attack the electron-deficient cyclobutene ring which can lead to a loss of the dye's colour. Another potential drawback with squaraine dyes can be their tendency to form aggregates, which can lead to a substantial broadening of their absorption bands. Use of the present compounds in filters address these problems.
Abstract: Synthesis of O-benzotriazole and O-imidazole synthons are described. Uses of synthons in synthesis of azapeptides and other peptidomimetics, azapeptides and other peptidomimetics synthesized from the synthons and uses of azapeptides and other peptidomimetics are also described.
Type:
Grant
Filed:
January 7, 2021
Date of Patent:
August 16, 2022
Assignee:
THE FEINSTEIN INSTITUTES FOR MEDICAL RESEARCH
Abstract: The invention provides a method for treating a neurodegenerative disorder in a subject in need of such treatment, comprising administrating to said subject a compound with (substituted phenyl)-propenal moiety.
Abstract: The present invention relates to a novel tryptophan hydroxylase inhibitor and a pharmaceutical composition including same, wherein the novel tryptophan hydroxylase inhibitor has an excellent inhibitory effect on TPH1, and thus can be usefully used for the prevention or treatment of disorders, such as metabolic disorders, cancer, digestive or cardiovascular system disorders, related to TPH1 activity. In particular, the novel tryptophan hydroxylase inhibitor has an excellent treatment effect on inflammatory bowel disorders, and thus can be usefully used for the treatment of inflammatory bowel disorder.
Type:
Grant
Filed:
August 24, 2018
Date of Patent:
August 9, 2022
Assignees:
Gwangju Institute of Science and Technolgy, Korea Advanced Institute of Science and Technology, KyungPook National University Industry-Academic Cooperation Foundation, Curacle Co., LTD.
Inventors:
Jin Hee Ahn, Hail Kim, Jaemyoung Suh, In-Kyu Lee, Kwang-eun Kim, Kun-Young Park, Eun Jung Bae, Ko Eun Shong, Suvarna Haus-habhau Pagire, Ajin Lim, Jae-Han Jeon, Haushabhau Shivaji Pagire, Haiying Zhang, Myung-Hwa Kim, Jung-In Pyo
Abstract: The present invention addresses the problem of providing a compound for prophylaxis and/or treatment of central inflammatory diseases, or a pharmacologically acceptable salt thereof. The present invention addresses a compound of a general formula (I) or a pharmacologically acceptable salt thereof as a means to solve the problem. [R1: a C1-C6 alkyl group or the like, R2: a C1-C6 alkyl group or the like, A: a 5-membered aromatic hetero-ring or the like, R3, R3?: a C1-C6 alkyl group or the like.
Abstract: The present invention relates to an improved asymmetric synthesis of azaspiro or diazaspiro compound (hereafter referred to as the compound 5, (5A) or (5N)) or their pharmaceutically acceptable salts and derivatives; through the formation of intermediate compounds 4, (4A) or (4N) respectively. The process comprises an unusual substrate specific highly diastereoselective as well as enantio-enriched 1-substituted 2-azaspiro[3.3]heptane or 1-substituted 2-diazaspiro[3.3]heptane compounds with high diastereoselectivity by addition of a cyclobutane carboxylate anion to a Davis-Ellman's imine, followed by reduction and cyclisation resulting in the selective formation of azaspiro or diazaspiro intermediate compound 4, (4A) or (4N); which on subsequently removing the sulfinyl group provides corresponding azaspiro or diazaspiro compound 5, (5A) or (5N) respectively.
Abstract: Bromine induced lactamization of vinyl acetohydroxamates facilitated syntheses of monocyclic ?-lactams suitable for incorporation of a thiomethyl and extended functionality at the C(4) position. Elaboration of the resulting substituted N-hydroxy-2-azetidinones allowed incorporation of functionalized ?-amino substituents appropriate for enhancement of antibiotic activity. Evaluation of antibacterial activity against a panel of Gram-positive and Gram-negative bacteria revealed structure-activity-relationships (SAR) and identification of potent new monobactam antibiotics. The corresponding bis-catechol conjugate, 42, has excellent activity against Gram-negative bacteria including carbapenemase and carbacephalosporinase producing strains of Acinetobacter baumannii which have been listed by the WHO as being of critical concern worldwide.
Type:
Grant
Filed:
October 2, 2018
Date of Patent:
August 2, 2022
Assignee:
University of Notre Dame du Lac
Inventors:
Marvin J. Miller, Serena Carosso, Rui Liu, Patricia Miller
Abstract: The present disclosure provides pharmaceutical combinations of orally administered docetaxel and a P-gp inhibitor. The pharmaceutical combinations are suitable for the treatment of cancer in a subject and for reducing or preventing toxicity, hypersensitivity-type infusion reactions, and other negative outcomes resulting from or associated with intravenously administered docetaxel (e.g., Taxotere® or docetaxel formulated with polysorbate 80) therapy in a subject suffering from cancer.
Type:
Grant
Filed:
October 29, 2020
Date of Patent:
July 19, 2022
Assignee:
Athenex HK Innovative Limited
Inventors:
Min-Fun Rudolf Kwan, E. Douglas Kramer, David Lawrence Cutler, Johnson Yiu-Nam Lau, Wing Kai Chan
Abstract: The present disclosure relates to a new salt of escitalopram and its solid state forms, processes for the preparation thereof, pharmaceutical compositions thereof, and methods of use thereof.