Abstract: A process can prepare a 3-glycidyloxypropylalkoxysilane of formula (I), (R?)O—(CH2)3—Si(OR)3 (I), where R groups are independently a methyl or ethyl group and R? represents an H2C(O)CHCH2— group. The process includes reacting (i) a functionalized alkene of formula (II), (R?)O—C3H5 (II), where R? represents an H2C(O)CHCH2— group, with (ii) at least one hydroalkoxysilane of formula (III), HSi(OR)3 (III), where R groups are independently a methyl or ethyl group. The reacting takes place in the presence of (iii) a Karstedt catalyst or a catalyst having hexachloroplatinic acid as a homogeneous catalyst, and (iv) 2-ethylhexanoic acid, isononanoic acid, or both. The process further includes obtaining a product of the reacting.
Type:
Grant
Filed:
August 8, 2018
Date of Patent:
November 5, 2019
Assignee:
Evonik Degussa GmbH
Inventors:
Markus Rudek, Susann Witzsche, Stefan Bade, Claudia Drescher, Burkhard John, Torsten Peterle
Abstract: and 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.
Abstract: Provided herein are maytansinoid compounds, derivatives thereof, conjugates thereof, and methods of treating or preventing proliferative diseases with the same.
Abstract: The present disclosure provides methods and reagents useful for analyzing protein-protein interfaces such as interfaces between a presenter protein (e.g., a member of the FKBP family, a member of the cyclophilin family, or PIN1) and a target protein. In some embodiments, the target and/or presenter proteins are intracellular proteins. In some embodiments, the target and/or presenter proteins are mammalian proteins.
Type:
Grant
Filed:
May 9, 2018
Date of Patent:
November 5, 2019
Assignee:
Revolution Medicines, Inc.
Inventors:
Gregory L. Verdine, M. James Nichols, Sharon A. Townson, Uddhav Kumar Shigdel, Seung-Joo Lee, Dylan T. Stiles, Neville J. Anthony
Abstract: An exemplary embodiment relates to novel protein modulators capable of altering function of the mutant CFTR protein and their use for treating diseases associated with CFTR protein malfunction. The invention provides compositions, pharmaceutical preparations and methods of correcting the cellular alteration of a mutant CFTR protein wherein the CFTR mutation is a mutation ?F508-CFTR, or another mutation of class II.
Type:
Grant
Filed:
December 15, 2015
Date of Patent:
November 5, 2019
Assignee:
INSTYTUT BIOCHEMII I BIOFIZYKI PAN
Inventors:
Norbert Odolczyk, Piotr Zielenkiewicz, Grzegorz Wieczorek, Aleksander Edelman, Danielle Tondelier, Janine Fritsch
Abstract: The present invention provides cyclic dimers of alpha acids and polymers derived therefrom. Also provided are processes for preparing and methods of using the cyclic dimers and the polymers derived from the cyclic dimers.
Type:
Grant
Filed:
March 5, 2015
Date of Patent:
October 29, 2019
Assignee:
Novus International, Inc.
Inventors:
Graciela B. Arhancet, Matthew Mahoney, Xiaojun Wang
Abstract: The present disclosure provides macrocyclic compounds of Formula (I). The provided compounds are able to bind protein kinases and may be useful in modulating (e.g., inhibiting) the activity of a protein kinase in a subject or cell and/or in treating or preventing a disease (e.g., proliferative disease, genetic disease, hematological disease, neurological disease, painful condition, psychiatric disorder, or metabolic disorder) in a subject in need thereof. Also provided are pharmaceutical compositions, kits, methods, and uses that include or involve a compound described herein.
Type:
Grant
Filed:
July 21, 2015
Date of Patent:
October 29, 2019
Assignee:
Dana-Farber Cancer Institute, Inc.
Inventors:
Nathanael S. Gray, Hwan Geun Choi, Yanke Liang
Abstract: This disclosure is directed to non-aromatic difluoro analogues of resorcylic acid lactones, pharmaceutical compositions comprising non-aromatic difluoro analogues of resorcylic acid lactones, and methods of treatment comprising non-aromatic difluoro analogues of resorcylic acid lactones.
Type:
Grant
Filed:
May 27, 2016
Date of Patent:
October 8, 2019
Assignee:
University of North Carolina at Greensboro
Inventors:
Mitchell P. Croatt, Lara Fakhouri, Nicholas H. Oberlies, Cedric Pearce
Abstract: This invention provides for a compound of formula (I) or a pharmaceutically acceptable salt thereof, wherein R1-R3, n, p, L1 and L2 are defined herein. The compounds of formula (I) and pharmaceutically acceptable salts thereof are cationic lipids useful in the delivery of biologically active agents to cells and tissues.
Type:
Grant
Filed:
December 17, 2014
Date of Patent:
October 1, 2019
Assignee:
Novartis AG
Inventors:
Luis Brito, Delai Chen, Gabriel Grant Gamber, Andrew Geall, Kevin Love, Thomas Zabawa, Frederic Zecri
Abstract: Compounds of formula (I) defined herein are useful as a dopamine D1 receptor positive allosteric modulators (D1 PAM) and can be used as an active ingredient of a pharmaceutical composition for preventing and/or treating cognitive impairment, schizophrenia negative symptom, CIAS, Parkinson's disease, Alzheimer's disease, Huntington's disease, depression, ADHD, drug dependency, or the like.
Abstract: The present invention relates to a method for producing N-substituted sulfonamide compounds including a step of reacting a sulfonamide compound of general formula (1) with a halogenated organic compound of general formula (2) in the presence of cesium carbonate or potassium carbonate in an organic solvent to produce an N-substituted sulfonamide compound of general formula (3).
Abstract: The invention relates to a process for preparing concentrated solutions of polymerization inhibitor, that can be used for the production, purification and storage of monomer compositions. This process comprises a step in which at least one polymerization inhibitor in the molten state is mixed with a solvent.
Type:
Grant
Filed:
February 22, 2016
Date of Patent:
September 24, 2019
Assignee:
Rhodia Operations
Inventors:
Jacques Cavezzan, Sébastien Lomel, Christian Rouyer, Terry Chamberlain
Abstract: A pharmaceutical composition comprising an ailanthone (AIL) compound or a derivative thereof, for the treatment of diseases or conditions caused by, dependent from, or associated with excessive androgen receptor activity. Ailantone compounds have been discovered to be a potent inhibitor of both full-length AR (AR-FL) and constitutively-active truncated AR splice variants (AR-Vs), and are found to possess favorable drug-like properties such as good bioavailability, high solubility, lack of CYP inhibition, and low hepatotoxicity. Methods of treatment are also provided.
Abstract: Provided are a novel compound or a salt thereof, and a pharmaceutical composition comprising the same, which selectively and strongly inhibit JAK3, exhibit an excellent activity for suppressing the growth of human peripheral blood monocytes and an excellent oral absorbability, and exhibits an activity of inhibiting IL-2-induced IFN-? production in vivo. A compound represented by formula (I) [wherein X represents —CH?CH—, —NH—, a sulfur atom or an oxygen atom; and n represents an integer of 0 to 2], or a salt thereof.
Abstract: An exemplary embodiment relates to novel protein modulators capable of altering function of the mutant CFTR protein and their use for treating diseases associated with CFTR protein malfunction. The invention provides compositions, pharmaceutical preparations and methods of correcting the cellular alteration of a mutant CFTR protein wherein the CFTR mutation is a mutation ?F508-CFTR, or another mutation of class II.
Type:
Grant
Filed:
December 15, 2015
Date of Patent:
September 24, 2019
Assignee:
INSTYTUT BIOCHEMII I BIOFIZYKI PAN
Inventors:
Norbert Odolczyk, Piotr Zielenkiewicz, Grzegorz Wieczorek, Aleksander Edelman, Danielle Tondelier, Janine Fritsch
Abstract: The disclosure includes high purity compounds having CCR5 and/or CCR2 antagonism, or salts thereof, high purity intermediates thereto and processes for synthesizing the same.
Abstract: Pateamine A derivatives and pharmaceutical compositions that include the derivatives. The pateamine A derivatives are ?-amino pateamine A derivatives that lack the C5-methyl group of pateamine A.
Type:
Grant
Filed:
March 31, 2016
Date of Patent:
September 10, 2019
Assignee:
The Texas A&M University System
Inventors:
Daniel Romo, Ken Hull, Mingzhao Zhu, Omar Robles
Abstract: Antimicrobial treated articles and compounds. The article includes a substrate and an antimicrobial mixture of an effective amount of at least one antimicrobial silanol quaternary ammonium compound, at least one essential oil and the balance water. In one embodiment, the antimicrobial mixture is forming in a reaction medium for mixing the at least one antimicrobial silanol quaternary ammonium compound and the at least one essential oil together prior to treating the substrate.
Abstract: Provided herein are methods of producing compounds, such as cyclohexanone, hexanediamine, hexanediol, hexamethylenediamine, caprolactam and nylon, from 5-(halomethyl)furfural.
Type:
Grant
Filed:
May 12, 2015
Date of Patent:
September 10, 2019
Assignee:
MICROMIDAS, INC.
Inventors:
Makoto Nathanael Masuno, Dimitri A. Hirsch-Weil, Ryan L. Smith, John Albert Bissell, II
Abstract: The invention relates to certain compounds or pharmaceutically acceptable salts, solvates, clathrates, or prodrugs thereof, that are useful as immunosuppressive agents and for treating and preventing inflammatory conditions, allergic disorders, and immune disorders.
Type:
Grant
Filed:
February 3, 2017
Date of Patent:
September 3, 2019
Assignee:
PRCL RESEARCH INC.
Inventors:
Shoujun Chen, Gary Bohnert, Jun Jiang, Zhiqiang Xia