Abstract: This invention provides novel indole, indazole, benzimidazole, benzotriazole, indoline, quinolone, isoquinoline, and carbazole selective androgen receptor degrader (SARD) compounds, pharmaceutical compositions and uses thereof in treating hyperproliferations of the prostate including pre-malignancies and benign prostatic hyperplasia, prostate cancer, advanced prostate cancer, castration resistant prostate cancer, other AR-expressing cancers, androgenic alopecia or other hyper androgenic dermal diseases, Kennedy's disease, amyotrophic lateral sclerosis (ALS), abdominal aortic aneurysm (AAA), and uterine fibroids, and to methods for reducing the levels (through degradation) and/or activity (through inhibition) of any androgen receptor including androgen receptor-full length (AR-FL) including pathogenic and/or resistance mutations, AR-splice variants (AR-SV), and pathogenic polyglutamine (polyQ) polymorphisms of AR in a subject.
Type:
Grant
Filed:
March 14, 2022
Date of Patent:
October 29, 2024
Assignees:
University of Tennessee Research Foundation, Oncternal Therapeutics, Inc.
Inventors:
Ramesh Narayanan, Duane D. Miller, Thamarai Ponnusamy, Dong-Jin Hwang, Yali He, Jayaprakash Pagadala, Christopher C. Coss, James T. Dalton, Charles B. Duke
Abstract: The present invention is directed to processes for making and compositions containing quinolines such as formula I or pharmaceutically acceptable salts thereof wherein: X1 is H, Br, CI, or X2 is H, Br, CI, or n1 is 1-2; and n2 is 1-2.
Abstract: The invention in this disclosure is related to the processes of making Bindarit or derivatives thereof. Specifically, the present invention provides, in part, new processes for making 2-((1-benzyl-1H-indazol-3-yl)methoxy)-2-methylpropanoic acid and its derivatives. By way of non-limiting example, synthesis and purification processes of 2-((1-benzyl-1H-indazol-3-yl)methoxy)-2-methylpropanoic acid are provided by the invention in this disclosure.
Abstract: A first aspect of the invention relates to betahistine, or a pharmaceutically acceptable salt thereof, and a monoamine oxidase inhibitor, for use in the treatment or prevention of one or more symptoms of vertigo in a subject. A second aspect of the invention relates to a method of treating or preventing one or more symptoms of vertigo in a subject, said method comprising administering to the subject (i) betahistine, or a pharmaceutically acceptable salt thereof, and (ii) a monoamine oxidase inhibitor.
Abstract: The present invention provides compositions and methods of use for treating, preventing, or ameliorating a disease, disorder, or condition associated with a chemokine receptor such as CXCR4.
Abstract: The invention relates to modulators of Embryonic Ectoderm Development (EED) and/or Polycomb Repressive Complex 2 (PRC2) useful in the treatment of disorders and diseases associated with EEC and PRC2, being macrocyclic azolopyridine derivatives and compositions thereof of Formula I: or a pharmaceutically acceptable salt, prodrug, solvate, hydrate, enantiomer, isomer, or tautomer thereof, wherein X1, X2, X3, A1, A2, Y, R1, R2, R3, and R4 are as described herein.
Type:
Grant
Filed:
December 20, 2022
Date of Patent:
October 8, 2024
Assignee:
Fulcrum Therapeutics, Inc.
Inventors:
Ivan Viktorovich Efremov, Steven Kazmirski, Qingyi Li, Lorin A. Thompson, III, Owen Brendan Wallace, Shawn Donald Johnstone, Feng Zhou, Peter Rahl
Abstract: There is provided the crystal of a heterocyclic amide compound and a method for producing the same wherein the heterocyclic amide compound defined as a compound having useful activity as herbicide contains a novel crystal, as shown in formula (1):
Abstract: A novel benzoheterocycle compound or a pharmaceutically acceptable salt thereof showed a high anti-proliferative effect against cancer cell lines. Using this, a pharmaceutical composition for preventing or treating cancer disease can comprise the compound or a pharmaceutically acceptable salt thereof as an active ingredient. In addition, a health functional food composition for preventing or improving cancer disease can include the compound or a pharmaceutically acceptable salt thereof as an active ingredient. The pharmaceutical composition or health functional food composition can effectively prevent or treat various cancer diseases.
Type:
Grant
Filed:
August 16, 2019
Date of Patent:
September 24, 2024
Assignee:
INDUSTRY ACADEMIC COOPERATION FOUNDATION KEIMYUNG UNIVERSITY
Abstract: To provide a fused thiophene molecule having further sufficiently high hole mobility. Disclosed is a fused thiophene molecule that has seven aromatic rings containing three thiophene rings in one molecule and in which the seven aromatic rings have one or two naphthalene structures. And, semiconductor devices including a layer using the fused thiophene molecule are disclosed.
Abstract: Disclosed are compounds having potency in the modulation of NMDA receptor activity. Such compounds can be used in the treatment of conditions such as depression and related disorders. Orally delivered formulations and other pharmaceutically acceptable delivery forms of the compounds, including intravenous formulations, are also disclosed.
Abstract: A novel organic compound is provided. A novel organic compound having a hole-transport property is provided. A novel hole-transport material is provided. A novel light-emitting element is provided. Alight-emitting element with a favorable lifetime is provided. A light-emitting element with favorable emission efficiency is provided. An organic compound having a substituted or unsubstituted benzonaphthofuran skeleton, a substituted or unsubstituted carbazole skeleton, and a substituted or unsubstituted amine skeleton is provided. Alternatively, a light-emitting element that uses the hole-transport material is provided.
Type:
Grant
Filed:
July 24, 2019
Date of Patent:
September 10, 2024
Assignee:
Semiconductor Energy Laboratory Co., Ltd.
Abstract: Provided herein are compounds that are broad-spectrum protein kinase binding agents, detectable tracers comprising such compounds, and method of use thereof for the detection of protein kinases.
Type:
Grant
Filed:
August 15, 2022
Date of Patent:
September 3, 2024
Assignee:
Promega Corporation
Inventors:
Cesear Corona, Poncho Meisenheimer, Matthew Robers, James Vasta
Abstract: Cost effective, semi-continuous flow methods and systems for synthesizing the antimalarial drug hydroxychloroquine (HCQ) in high yield are provided. The synthesis method that uses simple, inexpensive reagents to obtain the crucial intermediate 5-(ethyl(2-hydroxyethyl)-amino)pentan-2-one, vertical-integration of the starting material 5-iodopentan-2-one and the integration of continuous stirred tank reactors.
Type:
Grant
Filed:
February 25, 2019
Date of Patent:
August 27, 2024
Assignee:
Virginia Commonwealth University
Inventors:
Frank B. Gupton, Saeed Ahmad, Hari P. R. Gunuru, Nakul S. Telang
Abstract: Described herein are compounds that inhibits the membrane proximal external region (MPER) of a viral envelope (Env), as well as and compositions thereof. Further provided herein are methods for treating or preventing a viral infection comprises administering to a subject in need thereof an agent or compound that inhibits the MPER of a viral Env. In certain embodiments, the viral infection is an HIV infection.
Abstract: The present invention relates to a compound according to formula (I) and pharmaceutically acceptable salts, hydrates, or solvates thereof. The invention further relates to said compounds for use in therapy, to pharmaceutical compositions comprising said compounds, to methods of treating diseases, e.g., dermal diseases, with said compounds, and to the use of said compounds in the manufacture of medicaments.
Type:
Grant
Filed:
December 1, 2023
Date of Patent:
August 20, 2024
Assignee:
Leo Pharma A/S
Inventors:
Mark Andrews, Mogens Larsen, Alan Jessiman, Patrick Johnson, Kevin Neil Dack
Abstract: Crystalline form I and form II of (2S,5R)-5-(2-chlorophenyl)-1-(2?-methoxy-[1,1?-biphenyl]-4-carbonyl)pyrrolidine-2-carboxylic acid and preparation processes thereof. Also, a method for treating an inflammatory disease in a patient in need thereof, which includes administering to the patient a therapeutically effective amount of the crystalline form I or the crystalline form II of (2S,5R)-5-(2-chlorophenyl)-1-(2?-methoxy-[1,1?-biphenyl]-4-carbonyl) pyrrolidine-2-carboxylic acid.
Abstract: In one aspect, the present invention provides a method for treating or ameliorating the effects of a HER2 positive cancer in a subject. In some embodiments, the method comprises administering a combination therapy comprising an anti-HER2 antibody and tucatinib. In some embodiments, the method further comprises administering a chemotherapeutic agent (e.g., an antimetabolite) to the subject. Pharmaceutical compositions and kits are also provided herein.
Abstract: The present invention provides: a method for producing an epoxyalkane capable of obtaining an epoxide in a high yield while attaining a high olefin conversion rate and a high selectivity for epoxides even when an olefin includes a long carbon chain, and a solid oxidation catalyst used in the method. The method for producing an epoxyalkane of the present invention comprises reacting an olefin with an oxidant in the presence of a solid oxidation catalyst, wherein the solid oxidation catalyst comprises a transition metal and a carrier that supports the transition metal, and the carrier is a metal oxide having a silyl group represented by the following general formula (1): R1R2R3Si—??(1) wherein R1, R2, and R3 are each independently a single bond, a hydrocarbon group, a halogenated hydrocarbon group, an alkoxy group, or a halogen, and at least one of R1, R2, and R3 is a hydrocarbon group having 3 or more carbon atoms or a halogenated hydrocarbon group having 3 or more carbon atoms.
Abstract: The present invention aims to provide a compound that may be useful for the prophylaxis or treatment of constipation and the like. The present invention provides a compound represented by the following formula (I): wherein each symbol is as described in the specification, or a salt thereof.