Abstract: The present technology is directed to compounds of formula (II) as well as compositions thereof and methods related to modulation of FXR. In particular, the present compounds and compositions may be used to treat FXR-mediated disorders and conditions, including, e.g., liver disease, hyperlipidemia, hypercholesteremia, obesity, metabolic syndrome, cardiovascular disease, gastrointestinal disease, and atherosclerosis, and renal disease.
Abstract: The present disclosure relates to crystalline solid forms of a stimulator of soluble guanylate cyclase (sGC), Compound I: Also provided herein are methods for the preparation of these solid forms. The invention also relates to pharmaceutical formulations and dosage forms comprising these solid forms and their uses thereof, alone or in combination with one or more additional agents, for treating and/or preventing various diseases or disorders; these diseases or disorders are ones that may benefit from sGC stimulation or from an increase in the concentration of nitric oxide (NO) and/or cyclic guanosine monophosphate (cGMP).
Type:
Grant
Filed:
July 6, 2017
Date of Patent:
January 12, 2021
Assignee:
Cyclerion Therapeutics, Inc.
Inventors:
Vasu Sethuraman, Ahmad Hashash, Song Xue, Robert C. Livingston, Kwame Wiredu Nti-Addae
Abstract: This invention relates to a process for preparing electron deficient olefins, such as 2-cyanoacrylates, using an acid catalyzed two-step process including a transesterification reaction followed by a Knoevenagel condensation reaction.
Type:
Grant
Filed:
June 12, 2019
Date of Patent:
January 12, 2021
Assignee:
Henkel IP & Holding GmbH
Inventors:
Cormac Duffy, Marisa Phelan, Barry Burns
Abstract: The disclosure provides a pharmaceutical composition comprising a therapeutically effective amount of a compound of Formula (I): (I) or an isotope labelled analog thereof, or a pharmaceutically acceptable salt thereof, wherein: each of R1, R2, R3, R6 and R7 represents H or F, R4 represents H or CH3 R5 represents H or C1-C4alkyl, wherein at least two of R1, R2, R3, R6 and R7 represent F, together with at least one pharmaceutically acceptable carrier, excipient and/or diluent.
Type:
Grant
Filed:
November 17, 2017
Date of Patent:
December 29, 2020
Assignee:
INTEGRATIVE RESEARCH LABORATORIES SWEDEN AB
Abstract: Certain compounds of formula I: I and salts including pharmaceutically acceptable salts thereof are disclosed. Also disclosed are pharmaceutical compositions comprising a compound of formula I, processes for preparing compounds of formula I, intermediates useful for preparing compounds of formula I and therapeutic methods using a compound of formula I.
Type:
Grant
Filed:
June 16, 2017
Date of Patent:
December 1, 2020
Assignees:
Rutgers, The State University of New Jersey, The Curators of the University of Missouri
Inventors:
William J. Welsh, Raymond Birge, Vladyslav Kholodovych, Youyi Peng, Thomas Walter Comollo, Stanley G. Kimani, Kamlendra Singh
Abstract: The present disclosure relates to a cannabidiol compound and compositions thereof and processes for preparing the compound and compositions. The processes include an acid-catalyzed reaction of a suitably selected and substituted di-bromo-olivetol or derivative thereof with a suitably selected and substituted cyclic alkene to produce a dibromo-cannabidiol compound or derivative thereof. The dibromo-cannabidiol compound or derivative thereof can be produced in high yield, high stereospecificity, or both. It can then be converted under reducing conditions to a cannabidiol compound or derivatives thereof.
Abstract: This invention describes a method of conjugating a cell binding agent such as an antibody with an effector group (e.g., a cytotoxic agent) or a reporter group (e.g., a radionuclide), whereby the reporter or effector group is first reacted with a bifunctional linker and the mixture is then used without purification for the conjugation reaction with the cell binding agent. The method described in this invention is advantageous for preparation of stably-linked conjugates of cell binding agents, such as antibodies with effector or reporter groups. This conjugation method provides in high yields conjugates of high purity and homogeneity that are without inter-chain cross-linking and inactivated linker residues.
Type:
Grant
Filed:
February 1, 2019
Date of Patent:
October 27, 2020
Assignee:
IMMUNOGEN, INC.
Inventors:
Brenda A. Kellogg, Rajeeva Singh, Ravi V. Chari
Abstract: A positron emission tomography (PET) radiotracer for imaging lactate uptake, wherein the tracer is a [18F]-labelled lactate derivative which is [18F]-3-fluoro-2-hydroxypropionic acid: Also, a process for the radiosynthesis of the [18F]-labelled lactate derivative. Further, the use of the [18F]-labelled lactate derivative for imaging lactate uptake in living cells, especially in humans.
Type:
Grant
Filed:
September 8, 2017
Date of Patent:
October 13, 2020
Assignee:
GRANDIS
Inventors:
Pierre Sonveaux, Daniel Labar, Vincent Van Hée, Gwenaël Dehon, Raphaël Frédérick
Abstract: Compounds of Formula (I), which are activators of long form cyclic nucleotide phosphodiesterase-4 (PDE4) enzymes, are provided. Methods and uses of these compounds for the treatment or prevention of disorders requiring a reduction of second messenger responses mediated by cyclic 3?,5?-adenosine monophosphate (cAMP) are also described.
Abstract: Pyradizine derivatives that activity the excitatory amino acid transporter 2 (EAAT2) of the formula: and methods of use thereof for treating or preventing diseases, disorders, and conditions with glutamate toxicity.
Type:
Grant
Filed:
January 13, 2017
Date of Patent:
September 29, 2020
Assignees:
THE BRIGHAM AND WOMEN'S HOSPITAL, INC., OHIO STATE UNIVERSITY
Abstract: A multifunctional broad spectrum antimicrobial composition is described. The composition can be incorporated into a wood preservative, or used as an additive to provide antimicrobial properties to water-based wood coatings. The composition is a concentrated water-miscible emulsion containing 3-iodo-2-propynyl N-butylcarbamate (IPBC), carbendazim (BCM) and propiconazole (PPCZ), and has antimicrobial activity against a wide variety of fungal organisms, including surface molds, blue stain fungi and wood rotting fungi. The composition can act as an in-can preservative and is useful for antimicrobial protection of wood and wood-based substrates.
Abstract: A solvent is at least partially separated from a catalyst. The catalyst comprises nickel and a bidentate phosphorus-containing ligand. The method for separation involves distilling a catalyst solution. The ratio of 2-pentenenitrile to 3-pentenenitrile in distillation column bottoms is controlled to reduce the amount of 3-pentenenitrile which is isomerized to form 2-methyl-3-butenenitrile. Isomerization of 3-pentenenitrile to 2-methyl-3-butenenitrile and subsequent isomerization of 2-methyl-3-butenenitrile to 2-methyl-2-butenenitrile, and/or hydrocyanation of 2-methyl-3-butenenitrile to methylglutaronitrile represents a loss in adiponitrile yield in a process for making adiponitrile.
Type:
Grant
Filed:
July 16, 2014
Date of Patent:
September 1, 2020
Assignee:
INVISTA North America S.a r.l.
Inventors:
Sudhir N. V. K. Aki, James M. Garner, William J. Tenn, III, Thomas E. Vos
Abstract: A hydrogenation reaction catalyst used for a reaction of 1,4-anhydroerythritol and hydrogen to produce 3-hydroxytetrahydrofuran includes a carrier, at least one oxide selected from the group consisting of an oxide of a Group 6 element and an oxide of a Group 7 element, the oxide being supported on the carrier, and a metal other than a Group 6 element and a Group 7 element, the other metal being supported on the carrier. The amount of the oxide supported on the carrier in terms of a metal atom forming the oxide is 0.01 to 10% by weight based on the total amount of the oxide and the carrier being 100% by weight. The molar ratio in terms of metal of the other metal to the Group 6 element and Group 7 element forming the oxide [other metal/Group 6 element and Group 7 element] is 50/1 to 1/4.
Abstract: An antibiotic compound of formula (III): or a salt or stereoisomer thereof; wherein R1-R3 and R5-R10 are independently selected from the group consisting of H, alkyl group, substituted alkyl group, halogen, OH, NH2 and SH; R4 is H, alkyl group or substituted alkyl group; X1-X2 are independently selected from the group consisting of ?O, ?S, NH, H, alkyl, halogen, OH, SH and NH2; W is a saturated acyclic hydrocarbon chain of 1 to 15 carbon atoms; and Z is a neutral or positively charged organic group. The compounds are useful in treating bacterial diseases.
Type:
Grant
Filed:
November 15, 2018
Date of Patent:
August 18, 2020
Inventors:
Pavel Dibrov, Elena Dibrov, Grant Pierce
Abstract: The present invention relates to compounds having a benzotropolone core, and compositions containing said compounds acting as ATG4B inhibitors, thereby inhibiting autophagy. Moreover, the present invention provides processes for the preparation of the disclosed compounds, as well as methods of using them, for instance as a medicine, in particular for the treatment of cell proliferative disorders, such as cancer.
Inventors:
Koen Augustyns, Matthias Cleenewerck, Guido R. Y. De Meyer, Jurgen Joossens, Ammar Kurdi, Pieter Van Der Veken, Christel Vangestel, Sigrid Stroobants, Wim Martinet
Abstract: Disclosed are the anti-bacterial activity and the anti-tumor activity of a class of new spiro three-membered ring and spiro five-membered ring peptide deformylase inhibitor. The spiro three-membered ring and spiro five-membered ring peptide deformylase inhibitor of the present invention, as a class of new anti-bacterial agent, are effective against many antibiotic-resistant Gram-positive strains by inhibiting the activity of the peptide deformylase required in the synthesis of bacterial proteins, and do not affect the synthetic process of the main proteins of the human body, thus selectively killing bacteria.
Abstract: The disclosed subject matter provides N-hydroxylsulfonamide derivative compounds of formulae (I), (II) or (III) as drawn below, pharmaceutical compositions comprising such compounds, kits comprising such compounds, and methods of using such compounds or pharmaceutical compositions. In particular, the disclosed subject matter provides methods of using such compounds or pharmaceutical compositions for treating heart failure.
Type:
Grant
Filed:
October 18, 2016
Date of Patent:
August 4, 2020
Assignees:
Cardioxyl Pharmaceuticals, Inc., The Johns Hopkins University
Inventors:
Vincent Jacob Kalish, Lisa Marie Frost, Frederick Arthur Brookfield, Stephen Martin Courtney, John P. Toscano
Abstract: The present invention relates to 5-substituted 2-(morpholin-4-yl)-1,7-naphthyridine compounds of general formula (I) or (Ib), to methods of preparing said compounds, to intermediate compounds useful for preparing said compounds, to pharmaceutical compositions and combinations comprising said compounds and to the use of said compounds for manufacturing a pharmaceutical composition for the treatment or prophylaxis of a disease, in particular of a hyperproliferative disease as a sole agent or in combination with other active ingredients.
Type:
Grant
Filed:
January 6, 2017
Date of Patent:
August 4, 2020
Assignee:
BAYER PHARMA AKTIENGESELLSCHAFT
Inventors:
Ulrich Lücking, Marcus Koppitz, Julien Lefranc, Lars Wortmann, Antje Margret Wengner, Gerhard Siemeister, Ulf Bömer, Benjamin Bader, Philip Lienau, Hans Schick
Abstract: A series of novel EHop-016 derivatives is presented herein via designing and synthesizing compounds that mimics its more favorable “U-shaped” conformation that appears to be critical for inhibitory activity against Rac. Based on modeling studies on EHop-016, compounds with a more rigid structural conformation can mimic this “U-shaped” conformation would improve the anti-migration activity against metastatic cells. Compounds are disclosed that inhibit RhoGTPases that are useful for inhibiting hyperprofilerative and neoplastic diseases, for instance compounds of formula (I) Specifically, the compounds inhibit the GTPases Rac and Cdc42 that are overactive or overexpressed in signaling pathways in cancer and metastasis. Methods for treatment of cancer and hyperproliferative diseases are disclosed.