Abstract: Described herein are compounds and methods for tethering proteins. For example, dimers of Protein X listed in Table 1 are described, where the dimers are formed by the covalent bonding of a cysteine on the first monomer to a cysteine on the second monomer via a cyclic disulfide linker. The covalently attached dimers exhibit increased stabilization and can be used to treat neurodegenerative diseases (such as, for example, Parkinson's Disease, ALS, Alzheimer's Disease, Huntington's Disease, Epilepsy, Frontotemporal Dementia, and/or DMD), cancer, autoimmune disease, and/or Celiac disease.
Abstract: The present invention provides a method of producing a heterocyclic compound useful as an agent for the prophylaxis and/or treatment of Alzheimer's disease and the like. The present invention relates to a method of producing 1,5-anhydro-2,4-dideoxy-2-(4-fluoro-5-methyl-1-oxo-6-(4-(1H-pyrazol-1-yl)benzyl)-1,3-dihydro-2H-isoindol-2-yl)-L-threo-pentitol or a salt thereof, which comprises reacting 4-fluoro-3-hydroxy-5-methyl-6-[4-(1H-pyrazol-1-yl)benzyl]-2-benzofuran-1(3H)-one or a salt thereof, 3-fluoro-2-formyl-4-methyl-5-[4-(1H-pyrazol-1-yl)benzyl]benzoic acid or a salt thereof, or a mixture thereof, with 2-amino-1,5-anhydro-2,4-dideoxy-L-threo-pentitol.
Abstract: The present invention relates to trifluoroacetyl hydrazide compounds and medical uses thereof. The compounds have a structure of the following formula: The compounds showed multifunctional mechanisms, including inhibition of glutamate excitotoxicity, activation of MEF2 transcriptional activity, clearance of free radicals, and promotion of nerve differentiation, and has a better protective effect on cells especially nerve cells. The compound can be used to prepare prophylactic or therapeutic medicaments with cytoprotective effects, for the prevention or treatment of diseases related to glutamate receptor activation, MEF2 disorders or excessive free radicals generation. The diseases include, for example, neurodegenerative diseases such as Alzheimer's disease, Parkinson and stroke, and the free radicals related diseases such as heart disease, myocardial ischemia, diabetes and other cardiovascular and cerebrovascular diseases.
Abstract: Disclosed herein are antibacterial compounds, pharmaceutical compositions including the antibacterial compounds, and methods of treating bacterial infections using the compounds and compositions.
Type:
Grant
Filed:
March 20, 2017
Date of Patent:
July 7, 2020
Assignee:
Wayne State University
Inventors:
Fazlul H. Sarkar, Subhash Padhye, Bernhard Max Biersack, Hossein Salimnia
Abstract: The disclosure relates to a method of treating or preventing eye pain in a subject in need thereof. The method includes administering a compound of formula (I), R1—NH—CH(R2)—P(?O)(OH)—CH2—C(R3)(R4)—CONH—C(R5)(R6)—COOR7, to the subject.
Abstract: It is intended to provide a novel bisphosphonic acid compound or a salt thereof which shows a remarkable inhibitory effect on ectopic calcification, and a pharmaceutical composition comprising the same. The present invention provides a bisphosphonic acid compound represented by the following formula (1) or a pharmaceutically acceptable salt thereof: wherein represents a single bond or a double bond; A represents a saturated cyclic hydrocarbon or a saturated heterocyclic ring comprising a sulfur atom or an oxygen atom; and R1 and R2 each independently represent an alkyl group, an alkenyl group, an alkynyl group, an alkoxy group, an aryloxy group, a haloalkoxy group, a haloalkyl group, a halogen atom or a hydrogen atom.
Abstract: The disclosure relates to the field of medicine, in particular to the field of veterinary medicine. The disclosure specifically relates to muscarinic antagonists (including long acting muscarinic antagonists (LAMAs)) for the treatment of airway disease, such as pulmonary disease, preferably recurrent airway obstruction (RAO), summer pasture associated obstructive pulmonary disease (SPAOPD), and inflammatory airway disease (IAD) in animals, preferably equines such as horses.
Type:
Grant
Filed:
May 8, 2019
Date of Patent:
June 16, 2020
Inventors:
Balazs Albrecht, Michael Aven, Janine Lamar
Abstract: The present invention relates to indole compounds, and pharmaceutically acceptable compositions thereof, useful as antagonists of P2X7, and for the treatment of P2X7-related disorders.
Abstract: Antimicrobial and foamable alcoholic compositions, where the compositions include at least about 40 wt. % of a C1-4 alcohol and one or more silane surfactants selected from (1) zwitterionic silane surfactants, (2) polyalkoxylated silane surfactants that contain at least one silane group and at least one polyalkylene oxide chain.
Type:
Grant
Filed:
November 1, 2018
Date of Patent:
June 9, 2020
Assignee:
GOJO Industries, Inc.
Inventors:
Evan D. Hillman, Daniel J. Lacks, Mitchell J. Cohen
Abstract: The present invention provides compounds of Formula (I): or a stereoisomer, tautomer, or pharmaceutically acceptable salt or solvate thereof, wherein all the variables are as defined herein. These compounds are selective LPA receptor inhibitors.
Type:
Grant
Filed:
December 18, 2018
Date of Patent:
May 26, 2020
Assignee:
Bristol-Myers Squibb Company
Inventors:
Yan Shi, Peter Tai Wah Cheng, Ying Wang, Jun Shi, Shiwei Tao, Jun Li, Lawrence J. Kennedy, Robert F. Kaltenbach, III, Hao Zhang, James R. Corte
Abstract: A compound having formula I that is useful for C?O reduction is provided: wherein: M is a transition metal; X1, X2 are each independently a counterion; and R1, R2, R3 are each independently H, C1-6 alkyl, C6-15 aryl, or C6-15 heteroaryl.
Type:
Grant
Filed:
October 3, 2017
Date of Patent:
May 19, 2020
Assignee:
UNIVERSITY OF SOUTHERN CALIFORNIA
Inventors:
Sri Narayan, Travis J. Williams, Zhiyao Lu, Debanjan Mitra
Abstract: A compound of formula (Ia) or (Ib) or a pharmaceutically acceptable salt thereof. The compound is an inhibitor of a histone deacetylase, and as such is useful in therapy, e.g. in the treatment of autoimmune disorders, mental disorders, neurodegenerative disorders, and hyperproliferative disorders.
Type:
Grant
Filed:
November 16, 2016
Date of Patent:
May 19, 2020
Assignee:
KANCERA AB
Inventors:
Kristin Hammer, Mattias Jönsson, Lars Krüger
Abstract: The present invention relates to a process for the preparation of a hydrogel-linked prodrug releasing a tag moiety-biologically active moiety conjugate, to a hydrogel-linked prodrug releasing a tag moiety-bio logically active moiety conjugate obtainable by such process, to pharmaceutical compositions comprising said prodrug and their use as a medicament.
Type:
Grant
Filed:
April 16, 2014
Date of Patent:
May 19, 2020
Assignee:
Ascendis Pharma A/S
Inventors:
Harald Rau, Nora Kaluza, Ulrich Hersel, Thomas Knappe, Burkhardt Laufer
Abstract: The present invention relates to a 6-phenoxypyrimidine derivative, a method for preparing the compound and a pharmaceutical composition containing the compound as an active ingredient. Because the 6-phenoxypyrimidine compound represented by Chemical Formula 1 according to the present invention has an activity of inhibiting the production of nitric oxide (NO) as an inflammation-related factor, it is useful in treating and preventing inflammatory diseases including immunological diseases.
Type:
Grant
Filed:
June 22, 2018
Date of Patent:
May 12, 2020
Assignee:
Korea Institute of Science and Technology
Inventors:
Eun Joo Roh, Karam Mohamed Hasan Fara Ahmed, So Ra Paik, Woo Young Hur, Elkamhawy Ahmed
Abstract: The present invention relates to novel compounds of formula (I) and methods for the manufacture of inhibitors of deubiquitylating enzymes (DUBs). In particular, the invention relates to the inhibition of ubiquitin C-terminal hydrolase 30 or ubiquitin specific peptidase 30 (USP30). The invention further relates to the use of DUB inhibitors in the treatment of conditions involving mitochondrial dysfunction and in the treatment of cancer.
Type:
Grant
Filed:
February 16, 2017
Date of Patent:
May 5, 2020
Assignee:
MISSION THERAPEUTICS LIMITED
Inventors:
Karl Richard Gibson, Alison Jones, Mark Ian Kemp, Andrew Madin, Martin Lee Stockley, Gavin Alistair Whitlock, Michael D. Woodrow
Abstract: A process for preparing, 1,1,3-Trioxo-1,2-benzothiazole-6-carboxamide of formula (I) comprising: reacting 2-chloro-sulfonyl-terephthalic acid dialkyl ester of formula (II) with ammonia (N H3) or ammonium containing-salt; wherein R represents a branched or non-branched C1-C12 alkyl.
Type:
Grant
Filed:
December 28, 2016
Date of Patent:
April 28, 2020
Assignee:
ADAMA AGAN LTD.
Inventors:
Avihai Yacovan, Yaniv Barda, Sima Mirilashvili, Shmuel A. Baron
Abstract: The present invention accordingly provides novel compounds of formula (I) wherein R1, R2, R3 and R4 are as defined in the claims. The invention further relates to their in treatment or prevention of steroid hormone dependent diseases or disorders, such as steroid hormone dependent diseases or disorders requiring the inhibition of the 17?-HSD1 enzyme and/or requiring the lowering of the endogenous estradiol concentration.
Type:
Grant
Filed:
December 22, 2015
Date of Patent:
April 21, 2020
Assignee:
Forendo Pharma LTD
Inventors:
Leena Hirvelä, Pasi Koskimies, Risto Lammintausta, Marjo Hakola, Maire Eloranta
Abstract: The invention provides a method of inhibiting casein kinase 1? (CK1?), comprising contacting the CK1? with a compound of formula (I), as defined herein; such as compound SR-3029. We demonstrate that CSNK1D is amplified and/or overexpressed in human breast tumors and that CK1? can be medically targeted in human breast cancer subtypes overexpressing this kinase. The invention further provides a method of treating cancer, such as a breast cancer, melanoma, glioblastoma, medulloblastoma, renal, bladder or colon cancer, or a cancer that metastasizes to the brain, lung, or bone provided that both elevated CK1? and ?-catenin dependence are involved in those metastatic diseases. The cancer can be a breast cancer of the triple negative subclass of breast cancers (TNBC), or can be an HER+ breast cancer.
Type:
Grant
Filed:
October 5, 2016
Date of Patent:
March 31, 2020
Assignee:
The Scripps Research Institute
Inventors:
William R. Roush, Derek R. Duckett, John L. Cleveland, Laura H. Rosenberg