Abstract: The present invention relates to compounds of formula (I): (I) wherein Q is selected from O or S; R1 is an optionally substituted hydrocarbyl group which may optionally include one or more heteroatoms N, O or S in its carbon skeleton, provided that the hydrocarbyl group includes at least one heteroatom N, O or S in its carbon skeleton or is substituted with a substituent comprising at least one heteroatom N, O or S, and provided that the atom of R1 which is attached to the sulfur atom of the remainder of the molecule is not a ring atom of a cyclic group; R2 is an ?,??-substituted cyclic group which may optionally be further substituted; R3 and R4 are each independently hydrogen, halogen, —OH, —NH2, —CN, —R5, —OR5, —NHRs 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; and R5 is independently optionally substituted C1-C4 alkyl.
Type:
Grant
Filed:
March 1, 2019
Date of Patent:
December 17, 2024
Assignee:
INFLAZOME LIMITED
Inventors:
Matthew Cooper, David Miller, Jimmy Van Wiltenburg, Jonathan Shannon, Stephen St-Gallay
Abstract: The present invention relates to pharmaceutical compounds of Formula (I): as further described herein, and pharmaceutical compositions containing such compounds, as well as methods of using these compounds to modulate the activity of aryl hydrocarbon receptor (AhR) and to treat conditions comprising inflammation inside the intestinal tract and certain disorders of the central nervous system affected by the gut-brain axis, including IBD, ulcerative colitis, Crohn's disease, Huntington's disease, and multiple sclerosis.
Abstract: The present invention relates to a method for preparing 2-alkoxy-4-amino-5-methylpyridines of the formula (I) and/or 2-alkoxy-4-alkylamino-5-methylpyridines of the formula (II) from the corresponding 2-haloaminopyridines and the appropriate alcohols in the presence of base, and to the compounds resulting therefrom.
Abstract: The compounds represented by Formula (I), which are peripheral alkyl and alkenyl chains extended benzene derivatives, are useful as dual autotaxin (ATX)/histone deacetylase (HD AC) inhibitors. These compounds may be included in a pharmaceutical composition along with a pharmaceutically acceptable carrier, and be used in a therapeutically effective amount for prophylaxis or treatment of various diseases and disorders.
Abstract: A 4,4?-divinylazoarylene-bridged diruthenium catalyst bearing two Ru(CO)(3-methoxypyridin-2-olate)(PiPr3)2 moieties, its synthesis, and its use as a catalyst.
Abstract: Disclosed herein are kinase inhibitory compounds, such as a receptor-interacting protein-1 (RIP1) kinase inhibitor compounds, as well as pharmaceutical compositions and combinations comprising such inhibitory compounds. The disclosed compounds, pharmaceutical compositions, and/or combinations may be used to treat or prevent a kinase-associated disease or condition, particularly a RIP1-associated disease or condition.
Type:
Grant
Filed:
March 10, 2022
Date of Patent:
December 3, 2024
Assignee:
Rigel Pharmaceuticals, Inc.
Inventors:
Simon Shaw, Somasekhar Bhamidipati, Vanessa Taylor, Kyle Defrees
Abstract: The present invention provides crystalline forms of (E)-6-(4-Phenylcyclohexyl)-5-(3-trifluoromethylbenzyl)-1H-pyrimidine-2,4-dione, and methods of making and using the same.
Type:
Grant
Filed:
August 7, 2023
Date of Patent:
November 12, 2024
Assignee:
Corcept Therapeutics Incorporated
Inventors:
Hazel Joan Hunt, Lorraine Donaghy, Keith Lorimer, Nathan Jay Dixon, Jeffrey Mark Dener
Abstract: Described herein are heterocycle substituted pyridine derivative antifungal agents and pharmaceutical compositions comprising said compounds. The subject compounds and compositions are useful for the treatment of fungal diseases and infections.
Type:
Grant
Filed:
September 23, 2022
Date of Patent:
November 12, 2024
Assignee:
Basilea Pharmaceutica International AG, Allschwil
Inventors:
Michael Trzoss, Jonathan Covel, Karen Joy Shaw, Peter Webb
Abstract: The present disclosure provides compositions comprising artemisinin-derived trimers and tetramers; methods of preparing these compositions; and methods for their use as medicaments.
Abstract: The present disclosure provides compounds that are cGAS antagonists, methods of preparation of the compounds, pharmaceutical compositions comprising the compounds, and their use in medical therapy.
Type:
Grant
Filed:
June 13, 2023
Date of Patent:
November 5, 2024
Assignees:
IMMUNESENSOR THERAPEUTICS, INC., THE BOARD OF REGENTS OF THE UNIVERSITY OF TEXAS SYSTEM
Inventors:
Jian Qiu, Qi Wei, Matt Tschantz, Heping Shi, Youtong Wu, Huiling Tan, Lijun Sun, Chuo Chen, Zhijian Chen
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: 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 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.