Abstract: Disclosed in the present invention is a method for preparing nilotinib intermediate 3-(4-methyl-1H-imidazol-1-yl)-5trifluoromethyl phenylamine (I). The method comprises the following steps: taking trifluorotoluene as an initial material, and preparing the nilotinib intermediate (I) by nitration, bromization, condensation and reduction successively Compared with the prior art, the preparation method has the following advantages: a relatively high yield, the raw materials are easily obtained, a concise process and few side reactions, and is adapted to industrial production, so the development of an economic technology of the bulk drug is promoted.
Abstract: Cytotoxic dimers comprising CBI-based and/or CPI-based sub-units, antibody drug conjugates comprising such dimers, and to methods for using the same to treat cancer and other conditions.
Type:
Grant
Filed:
August 2, 2018
Date of Patent:
August 27, 2019
Assignee:
Pfizer Inc.
Inventors:
Andreas Maderna, Matthew David Doroski, Zecheng Chen, Hud Lawrence Risley, Jeffrey Michael Casavant, Christopher John O'Donnell, Alexander M. Porte, Chakrapani Subramanyam
Abstract: A compound, or a pharmaceutically acceptable salt or ester thereof, having a structure of: wherein X is a divalent linking moiety; and R1-R10 are each individually H, optionally-substituted alkyl, optionally-substituted alkoxy, optionally-substituted aryl, optionally-substituted cycloalkyl, optionally-substituted heterocyclic, halogen, amino, or hydroxy, provided that at least one of R3 or R8 is an optionally-substituted alkyl, a substituted alkoxy, optionally-substituted aryl, optionally-substituted cycloalkyl, optionally-substituted heterocyclic, or halogen.
Type:
Grant
Filed:
October 10, 2018
Date of Patent:
August 6, 2019
Assignees:
University of Pittsburgh—Of the Commonwealth System of Higher Education, The United States of America as represented by the Department of Veterans Affairs
Abstract: The present invention relates to the synthesis of succinimides, in particular to a method for the synthesis of a succinimide compound, comprising the step of reacting an alkyne, with carbon monoxide and ammonia or an amine, in the presence of an iron catalyst, wherein the reaction is carried out in an amine liquid phase and/or in the absence of an ether solvent. The succinimides may be reduced to quaternary ammonium cations which may be used as structure directing agents in the synthesis of molecular sieves.
Type:
Grant
Filed:
June 27, 2018
Date of Patent:
July 30, 2019
Assignee:
ExxonMobil Chemical Patents Inc.
Inventors:
Kirk D. Schmitt, Stephen Zushma, Allen W. Burton
Abstract: A new scalable process to control the particle size and the particle size distribution, comprising 5 steps: (i) suspension preparation in a mixture of solvents in which the API and/or excipient is partially soluble in one of the solvents; (ii) particle size reduction of the suspension; (iii) aging; (iv) stopping the aging by solvent removal; and (v) optionally, a step of isolating the processed ingredients in the form of powder.
Type:
Grant
Filed:
January 27, 2015
Date of Patent:
June 25, 2019
Assignee:
Hovione International Ltd.
Inventors:
Eunice Costa, Marcio Temtem, Luis Sobral, Constanca Cacela, Peter Villax
Abstract: Compounds of formula (I), wherein the substituents are as defined in claim 1, and the agrochemically acceptable salts, stereoisomers, enantiomers, tautomers and N-oxides of those compounds, can be used as insecticides and can be prepared in a manner known per se.
Type:
Grant
Filed:
December 10, 2015
Date of Patent:
June 18, 2019
Assignee:
Syngenta Participations AG
Inventors:
Ottmar Franz Hueter, Andrew Edmunds, Andre Jeanguenat, Pierre Joseph Marcel Jung, Anke Buchholz, Michel Muehlebach
Abstract: The present disclosure relates to prostate specific membrane antigen (PSMA) targeted compounds conjugated to near-infra red (NIR) dyes and methods for a method for synthesizing a compound of the formula:
Abstract: Anti-angiogenic treatments, treatments of hyperpermeability disorders, treatments of neuropathic and neurodegenerative disorders, pain treatments, methods of reducing the risk of pre-eclampsia and compounds for use in such methods are described.
Type:
Grant
Filed:
October 17, 2013
Date of Patent:
May 28, 2019
Assignee:
The University of Nottingham
Inventors:
Steven James Harper, David Owen Bates, Melissa Gammons, Jonathan Morris
Abstract: Provided herein are compounds of formula I: and salts thereof and compositions and uses thereof. The compounds are useful as inhibitors of LSD1. Also included are pharmaceutical compositions comprising a compound of formula I or a pharmaceutically acceptable salt thereof, and methods of using such compounds and salts in the treatment of various LSD1-mediated disorders.
Type:
Grant
Filed:
July 24, 2017
Date of Patent:
May 28, 2019
Assignees:
GENENTECH, INC., CONSTELLATION PHARMACEUTICALS, INC.
Inventors:
Brian K. Albrecht, James Edmund Audia, Alexandre Cote, Martin Duplessis, Victor S. Gehling, Andrew Charles Good, Jean-Christophe Harmange, Yves LeBlanc, Christopher G. Nasveschuk, Alexander M. Taylor, Rishi G. Vaswani
Abstract: The present invention relates to bendamustine derivatives and related compounds of formula (VII), (VIII) and (IX), and medical uses thereof in particular in cancer therapy.
Abstract: The present application relates to substituted heterocycles compound of Formula I and pharmaceutical compositions thereof useful for the inhibition of BET protein function by binding to bromodomains (Formula I).
Type:
Grant
Filed:
December 11, 2015
Date of Patent:
May 21, 2019
Assignee:
Zenith Epigenetics Ltd.
Inventors:
Samuel David Brown, Craig Alan Coburn, Olesya Kharenko
Abstract: Aspects of the present disclosure generally relate to compounds for targeting and healing bone fractures. Some of these compounds include a negatively charged oligopeptide comprising an acidic oligopeptide, a linker, which may be hydrolyzable or may be a substrate for the protease cathepsin K, and at least one molecule that promotes bone healing. In some compounds the molecule that promotes bone healing is an anabolic compound that inhibits GSK3?, in some compounds the molecule that promotes the healing of bone fracture is a pro-inflammatory agent such as PGE1. Other embodiments include methods of treating a bone fracture comprising administering a therapeutic amount of any one of the compounds disclosed herein.
Type:
Grant
Filed:
May 29, 2016
Date of Patent:
May 7, 2019
Assignees:
Purdue Research Foundation, University of Utah Research Foundation
Inventors:
Stewart Andrew Low, Philip S. Low, Christopher Galliford, Jindrich Kopecek, Jiyan Yang
Abstract: The invention concerns compounds of Formula (I): or pharmaceutically acceptable salts thereof, wherein R1, R2, R3 and R4 have any of the meanings hereinbefore defined in the description; process for their preparation; pharmaceutical compositions containing them and their use in treating KIT mediated diseases.
Type:
Grant
Filed:
April 26, 2018
Date of Patent:
April 30, 2019
Assignee:
AstraZeneca AB
Inventors:
Jason Kettle, Stuart Pearson, Martin Packer, James Smith
Abstract: The present invention provides crystalline Forms FUM-P3, FUM-P4, MLA-P3 and MLA-P4 of compound formula 1 and related methods of treating and/or preventing a disease, such as a central nervous system disease (e.g., an anxiety disorder), using a crystalline Form FUM-P3, FUM-P4, MLA-P3 and MLA-P4 of compound formula 1 and/or pharmaceutical compositions thereof.
Type:
Grant
Filed:
August 25, 2017
Date of Patent:
April 23, 2019
Assignees:
Bionomics Limited, Ironwood Pharmaceuticals, Inc.
Inventors:
Bernard Luke Flynn, Dharam Paul, Andrew John Harvey, Vasu V. Sethuraman, Raymond E. Forslund, Song Xue, Rob Livingston, Ahmad Hashash
Abstract: The present invention relates to a compound of formula (I): wherein R1 is R3—IPU and R2 is the acyloxy residue of diclofenac, and specified by the following structures: wherein OH—R3—IPU is selected from and R4 and R5 may be the same or different selected from H and CH3 and salts, solvates and hydrates thereof.
Abstract: The present disclosure is directed to methods for dehydrogenatively coupled hydrosilanes and alcohols, the methods comprising contacting an organic substrate having at least one organic alcohol moiety with a mixture of at least one hydrosilane and sodium and/or potassium hydroxide, the contacting resulting in the formation of a dehydrogenatively coupled silyl ether. The disclosure further described associated compositions and methods of using the formed products.
Type:
Grant
Filed:
July 26, 2016
Date of Patent:
April 16, 2019
Assignee:
California Institute of Technology
Inventors:
Anton Toutov, Kerry Betz, Andrew M. Romine, Robert H. Grubbs
Abstract: The invention provides 1,4-dihydropyridine derivatives of formula (I) wherein R1 is optionally substituted C6-24aryl group or 5 to 6 membered heteroaryl group comprising 1 to 3 nitrogen atoms or other heteroatoms like oxygen and sulphur, and combinations thereof; R2 and R3 are independently hydrogen or C1-6alkyl group; R4 and R5 are independently hydrogen, C1-6alkyl group optionally substituted with amino, mono- or di(C1-6alkyl)amino, or with 5 to 24 membered optionally fused heterocyclic ring attached by nitrogen and optionally comprising additional 1 to 3 N, O, S heteroatoms and optionally substituted with C1-6alkyl group or C1-6 alkoxy group; R6 is C1-6alkyl, C3-7cycloalkyl, C3-7cycloalkylC1-6alkyl or arylC1-6alkyl group; and stereoisomers including enantiomers, diastereomers, racemic mixtures, mixture of enantiomers and combination thereof, as well as polymorphs, pharmaceutically acceptable salts, solvates, esters and prodrugs thereof for use in the therapeutic or prophylactic treatment of a disorder medi
Type:
Grant
Filed:
November 22, 2012
Date of Patent:
April 16, 2019
Assignee:
Richter Gedeon NYRT.
Inventors:
Ferenc Fülöp, László Vigh, Zsolt Török, Botond Penke, Ibolya Horváth, Gábor Balogh, Sándor Bernáth, Ákos Hunya
Abstract: A method and compound includes mixing dichloroglyoxime with an alcohol containing an alkyne functional group in methanol to create a mixture; adding a salt compound and water to the mixture to create bis-isoxazole diol; and nitrating the bis-isoxazole diol to create 3,3?-bis-isoxazole-5,5?-bis-methylene dinitrate, which has the structural formula: The alcohol containing an alkyne functional group may include propargyl alcohol. The salt compound may include sodium bicarbonate. The method may include nitrating the bis-isoxazole diol with nitric acid. The nitric acid may include at least a concentration of 90% nitric acid in water. Alternatively, the method may include nitrating the bis-isoxazole diol with 100% nitric acid and acetic anhydride. The salt compound and the water may be added to the mixture over at least a six-hour period. The method may include mixing the mixture after adding the salt compound and the water for at least ten hours.
Type:
Grant
Filed:
August 25, 2017
Date of Patent:
April 2, 2019
Assignee:
The United States of America as represented by the Secretary of the Army
Inventors:
Jesse J. Sabatini, Gregory W. Drake, Leah A. Wingard, Eric C. Johnson
Abstract: This invention is directed to benzenesulfonamide compounds, as stereoisomers, enantiomers, tautomers thereof or mixtures thereof; or pharmaceutically acceptable salts, solvates or prodrugs thereof, for the treatment of diseases or conditions associated with voltage-gated sodium channels, such as epilepsy.
Type:
Grant
Filed:
May 19, 2017
Date of Patent:
April 2, 2019
Assignee:
Xenon Pharmaceuticals Inc.
Inventors:
Jean-Christophe Andrez, Kristen Nicole Burford, Sultan Chowdhury, Charles Jay Cohen, Christoph Martin Dehnhardt, Robert Joseph Devita, James Roy Empfield, Thilo Focken, Michael Edward Grimwood, Syed Abid Hasan, James Philip Johnson, Jr., Alla Yurevna Zenova