Abstract: A fumarate salt and a maleate salt of compound (I) represented by the following structural formula, as well as their corresponding pharmaceutical compositions, are disclosed. Particular single crystalline forms of 1:1 compound (I) fumarate and 1:1 compound (I) maleate are characterized by a variety of properties and physical measurements. Methods of preparing specific crystalline forms of 1:1 compound (I) fumarate and 1:1 compound (I) maleate are also disclosed. The present invention also provides methods of treating a subject with a cancer.
Type:
Grant
Filed:
February 10, 2021
Date of Patent:
June 6, 2023
Assignee:
UNIVERSITY HEALTH NETWORK
Inventors:
Peter Brent Sampson, Miklos Feher, Heinz W. Pauls
Abstract: Pharmaceutical compositions comprising a RelA enzyme inhibitor and a bactericidal antibiotic, wherein said RelA enzyme inhibitor binds to the RelA enzyme in bacteria to reduce biofilm formation and to degrade biofilms that have been formed. The pharmaceutical compositions can be used to treat bacterial biofilm diseases.
Type:
Grant
Filed:
May 14, 2018
Date of Patent:
June 6, 2023
Assignee:
DREXEL UNIVERSITY
Inventors:
Hai-Feng Ji, Garth David Ehrlich, Donald Carl Hall, Jr., Jaroslaw E. Krol, John P. Cahill
Abstract: Disclosed are heterocyclic heteroaromatic macrocyclic ether compounds, pharmaceutically acceptable salts of the compounds and pharmaceutical compositions thereof. Also disclosed are methods of treating or preventing cancer using the heterocyclic heteroaromatic macrocyclic ether compounds, pharmaceutically acceptable salts of the compounds, and pharmaceutical compositions thereof.
Type:
Grant
Filed:
November 11, 2021
Date of Patent:
June 6, 2023
Assignee:
Nuvalent, Inc.
Inventors:
Joshua Courtney Horan, Xinxing Tang, Scot Richard Mente, Henry Efrem Pelish, Matthew D. Shair, Anupong Tangpeerachaikul
Abstract: A lotion for the topical application to reduce a swimmer's friction when swimming in water made by combining an aqueous phase comprising and at least one humectant with an oil phase. The at least one humectant is present in the aqueous phase in the range of from 45 to 97 wt. %. The oil phase comprises at least one surfactant and at least one oil, and is present in the lotion in the range of about 5 to 45 wt. %. The surfactant is present in the oil phase in the range of from about 0.1 to 25 wt. %. The lotion is stable, homogenous and hydrophobic, and reduces friction when swimming in water, with the lotion applied to a swimmer.
Abstract: A compound, as defined herein, or pharmaceutical composition containing the compound, for use in treating IDH1 or IDH2 mutant cancer and having the structure: (I).
Type:
Grant
Filed:
March 16, 2021
Date of Patent:
May 16, 2023
Assignee:
Eli Lilly and Company
Inventors:
Renato Alejandro Bauer, Serge Louis Boulet, Timothy Paul Burkholder, Patric James Hahn, Zoran Rankovic
Abstract: The present disclosure is concerned with small molecule modulators of KLF15 signaling useful for treating various disorders such as, for example, kidney disease (e.g., chronic kidney disease), heart disease, obesity, or a neurodegenerative disorder (e.g., amyotrophic lateral sclerosis (ALS), Alzheimer's disease, Parkinson's disease, spinal muscular atrophy, traumatic brain injury, vascular dementia, Huntington's disease, mental retardation, and attention deficit and hyperactivity disorder (ADHD)). This abstract is intended as a scanning tool for purposes of searching in the particular art and is not intended to be limiting of the present invention.
Type:
Grant
Filed:
April 29, 2021
Date of Patent:
May 9, 2023
Assignees:
Icahn School of Medicine at Mount Sinai, The United States Government as represented by the Department of Veterans Affairs, The Research Foundation for the State University of New York
Abstract: The present invention provides compounds and pharmaceutical compositions including the compounds for the treatment of a skin disease associated with proteolytic activity of one or more KLK proteases, wherein the compounds are according to formula (I): wherein R is as described herein.
Abstract: Provided herein are opioid receptor modulators and pharmaceutical compositions comprising said compounds.
Type:
Grant
Filed:
April 5, 2022
Date of Patent:
April 25, 2023
Assignee:
EPIODYNE, INC.
Inventors:
Julio Cesar Medina, Alok Nerurkar, Corinne Sadlowski, Frederick Seidl, Heng Cheng, Jason Duquette, John Lee, Martin Holan, Pingyu Ding, Xiaodong Wang, Tien Widjaja, Thomas Nguyen, Ulhas Bhatt, Yihong Li, Zhi-liang Wei
Abstract: A compound, as defined herein, or pharmaceutical composition containing the compound, for use in treating IDH1 or IDH2 mutant cancer and having the structure: (I).
Type:
Grant
Filed:
March 16, 2021
Date of Patent:
April 18, 2023
Assignee:
Eli Lilly and Company
Inventors:
Renato Alejandro Bauer, Serge Louis Boulet, Timothy Paul Burkholder, Raymond Gilmour, Patric James Hahn, Zoran Rankovic
Abstract: The present invention provides a compound which has an effect of inhibiting amyloid ßproduction, especially an effect of inhibiting BACE1, and which is useful as a therapeutic or prophylactic agent for diseases induced by production, secretion and/or deposition of amyloid ßproteins. A compound of Formula (I) wherein R3 is each independently alkyl optionally substituted with halogen, cyano, alkyloxy, haloalkyloxy or non-aromatic carbocyclyl, or the like; t is integer from 0 to 3; R5 is a hydrogen atom or halogen; R6 is selected from the group consisting of a hydrogen atom, halogen, and substituted or unsubstituted alkyl; ring B is a substituted or unsubstituted pyrazine or the like; or a pharmaceutically acceptable salt thereof.
Abstract: There is disclosed herein a composition for treating gastrointestinal or neurological disorders, constipation, functional constipation, irritable bowel syndrome, diverticulitis, travelers diarrhoea, chronic idiopathic nausea, IBD-associated constipation and diarrhoea, pseudo-obstruction, diabetic gastroparesis, cyclic vomiting, reflux esophagitis, autism enteropathy, flatulence, halitosis, chronic fatigue, bloating, proctalgia fugax, Parkinson's disease, MS, Alzheimer's Disease, Motor Neuron Disease or autism, the composition comprising: (i) at least two anti-clostridial agents selected from the group consisting of: vancomycin, vancomycin derivatives, a multi-valent polymer of vancomycin, aminoglycosides, nitroimidazoles, ansamysins, nifuroxazide, colchicine, prucalopride, prokinetic agent and 5-aminosalicylic acid; or (ii) at least one anti-clostridial agent selected from the above combined with an opioid blocking agent.
Abstract: The present invention relates to biomarkers associated with CTCL, including TOX, PLS3, KIR3DL2, GATA3 and RUNX3, where increased expression, relative to normal control, of one or more of TOX, PLS3, KIR3DL2, and/or GATA3 is associated with CTCL and decreased expression of RUNX3, relative to normal control, is associated with CTCL. One or more of these biomarkers may be used to diagnose CTCL and/or design and monitor treatment.
Type:
Grant
Filed:
June 18, 2021
Date of Patent:
March 7, 2023
Assignee:
UNIVERSITY OF PITTSBURGH—OF THE COMMONWEALTH SYSTEM OF HIGHER EDUCATION
Inventors:
Larisa J. Geskin, Brittany Lynn O'Neill Dulmage, Louis D. Falo, Jr.
Abstract: Disclosed herein are compound embodiments that are useful for treating a variety of diseases, particularly neurological diseases, motor neuron diseases, copper deficiency-related diseases, and/or mitochondrial deficiencies. The compound embodiments described herein also can be used in PET methods. Also disclosed herein are embodiments of methods of making and using the compound embodiments, as well as pharmaceutical formulations comprising the disclosed compound embodiments.
Type:
Grant
Filed:
February 26, 2020
Date of Patent:
March 7, 2023
Assignee:
Oregon State University
Inventors:
Joseph Beckman, James Hurst, John Sirois, Chris Beaudry
Abstract: Biologically active cannabidiol analogs comprising a compound of the formula wherein one of R1 or R2 or both is/are the residue of a moiety formed by the reaction of an amino group of the amino acid ester of R1 or R2 or both with a dicarboxylic acid or a dicarboxylic acid derivative and the other R1 or R2 (in the case of the mono) is the residue of a dicarboxylic acid or dicarboxylic acid derivative or Hydrogen (H), (i.e. underivatized), and salts thereof. These CBD analogs are be useful in pain management in oncology and other clinical settings in which neuropathy is presented. Furthermore, these CBD-analogs are useful in blocking the addictive properties of opiates.
Type:
Grant
Filed:
June 9, 2020
Date of Patent:
March 7, 2023
Assignee:
UNIVERSITY OF MISSISSIPPI
Inventors:
Mahmoud A. ElSohly, Soumyajit Majumdar, Waseem Gul, Mohammad Khalid Ashfaq, Kenneth Joseph Sufka, Hannah Marie Harris
Abstract: The present invention relates to a cocrystal of beta-sitosterol or a pharmaceutically acceptable ester thereof or an edible acceptable ester thereof and an organic carboxylic acid coformer, an hydrate crystal form of beta-sitosterol having 1.25 molecules of water per molecule of beta-sitosterol and a combination that comprises a cocrystal of beta-sitosterol and an organic carboxylic acid; and the hydrate crystal form of beta-sitosterol having 1.25 molecules of water per molecule of beta-sitosterol. It also relates to processes for their preparation, and compositions containing them, as well as their use as a medicament or dietary supplement or functional food, and in particular in the prophylaxis and/or treatment of a disease or conditions that involves an alteration of lipid metabolism, circulating levels of lipids in the blood and/or lipid composition in tissues and organs.
Type:
Grant
Filed:
June 22, 2018
Date of Patent:
February 28, 2023
Assignees:
CENTER FOR INTELLIGENT RESEARCH IN CRYSTAL ENGINEERING, S.L., ALIMENTOMICA, S.L.
Inventors:
Rafel Prohens López, Rafael Barbas Cañero, Anna Portell Bueso, Mariona Palou March, Francisca Serra Vich, Andreu Palou March
Abstract: A process A for the production of compounds of formula I is provided. Process A includes Step A of reacting compounds of formula II with 2,3-dihalopropionitrile or 2-haloacrylonitrile in the presence of DIPEA. A process B for the production of compounds of formula III is also provided. Process B includes Step B of reacting compounds of formula I with Br2 in the presence of DIPEA. A process C for the production of compounds of formula IV is further provided. Process C includes Step C of reacting compounds of formula III with di(C1-C4-alkoxy)methane and either POCl3, or a mixture comprising POCl3 and DMF, in the presence of DIPEA. Additionally, the use of DIPEA as a base in the production of compounds of formula I, compounds of formula III, or compounds of formula IV is provided.
Abstract: The present invention provides a compound of formula (I) or a pharmaceutically acceptable salt thereof, pharmaceutical compositions comprising a compound of the invention, a method for manufacturing compounds of the invention and therapeutic uses thereof.
Type:
Grant
Filed:
August 13, 2019
Date of Patent:
February 7, 2023
Assignee:
AMGEN INC.
Inventors:
John R. Butler, Daniel Erlanson, Russell Graceffa, Jeffrey Iwig, Joon Won Jeong, Ryan D. White, Yongwei Wu, Shuyan Yi, Xiao Mei Zheng, Jesse M. McFarland, Abhisek Banerjee
Abstract: A method of controlling phytopathogenic diseases on useful plants or on propagation material thereof, which comprises applying to the useful plants, the locus thereof or propagation material thereof a combination of components (A) and (B) in a synergistically effective amount, wherein component (A) is a compound of formula I compound of formula I wherein R is hydrogen or methoxy; Q is R1 is hydrogen, halogen or C1-C6alkyl; R2 is hydrogen, halogen, C1-C6alkyl, C2-C6alkenyl, C3-C6alkinyl, C3-C6cycloalkyl-C3-C6alkinyl, halophenoxy, halophenyl-C3-C6alkinyl, C(C1-C4alkyl)=NO—C1-C4alkyl, C1-C6haloalkyl, C1-C6haloalkoxy, C2-C6haloalkenyl, or C2-C6haloalkenyloxy; R3 is hydrogen, halogen, C1-C6alkyl; R4, R5 and R6, independently from each other, are hydrogen, halogen or —?—R7; with the proviso that at least one of R4, R5 and R6 is different from hydrogen; R7 is hydrogen, C1-C6alkyl, C1-C6haloalkyl or C1-C4alkoxyalkyl; and R8 is hydrogen or methoxy; and agrochemically acceptable salts/isomers/structural is
Abstract: Disclosed are a class of anti-HBV tetrahydroisoxazolo[4,3-c]pyridine compounds and pharmaceutically acceptable salts thereof or isomers thereof, the compounds being represented by the formula (I).
Type:
Grant
Filed:
November 16, 2018
Date of Patent:
February 7, 2023
Assignee:
Medshine Discovery Inc.
Inventors:
Lifang Wu, Fei Sun, Jinhua Du, Charles Z. Ding, Shuhui Chen, Xiquan Zhang, Hongjiang Xu, Ling Yang