Abstract: The present invention relates to a compound with the following formula (I): (I) or a salt and/or a pharmaceutically acceptable solvate thereof, in particular for use as a drug, in particular in the treatment of cancer, as well as to the pharmaceutical compositions that contain same and to the methods for preparing same.
Type:
Grant
Filed:
September 2, 2015
Date of Patent:
June 18, 2019
Assignee:
PIERRE FABRE MEDICAMENT
Inventors:
El Bachir Kaloun, Serge Grisoni, Anna Kruczynski, Philippe Schmitt
Abstract: This disclosure relates generally to the facile and selective mono-perfluoro and -polyfluoroarylation of Meldrum's acid to generate a versatile synthon for highly fluorinated alpha-phenyl acetic acid derivatives which provide straightforward access to fluorinated building blocks. The reaction takes place quickly and all products were isolated without the need for chromatography. An embodiment provides an alternative strategy to access alpha-arylated Meldrum's acids which avoids the need for aryl-Pb(IV) salts or diaryliodonium salts and provides access to the tertiary product which was not previously synthetically accessible. The synthetic versatility and utility of the Meldrum's acid products is demonstrated by subjecting the products to several derivatizations of the Meldrum's acid products as well as photocatalytic hydrodefluorination which provide access to difficult but valuable synthetic targets such as multifluorinated aromatics.
Type:
Grant
Filed:
August 31, 2015
Date of Patent:
June 11, 2019
Assignee:
The Board of Regents for Oklahoma State University
Abstract: The invention relates to benzodiazepine derivatives of formula (A) useful as CCK2/gastrin receptor antagonists, their preparation and their use in the treatment or prevention of disorders associated with CCK2/gastrin receptors, disorders caused by or associated with hypergastrinaemia, and gastric acid-related disorders.
Type:
Grant
Filed:
August 7, 2015
Date of Patent:
June 4, 2019
Assignee:
TRIO MEDICINES LTD
Inventors:
Malcolm James Boyce, Liv Thomsen, Donald Alan Gilbert, David Wood
Abstract: The present invention claims complexing [18F] fluoride anion with diaryl and aryl fused-[2.2.2]cryptand to form [18F] fluoride diaryl and aryl fused-cryptate complexes suitable for performing radio-labeling reactions to generate [18F] fluorinated species.
Type:
Grant
Filed:
August 19, 2012
Date of Patent:
June 4, 2019
Inventors:
Yousry M. A. Naguib, Ashraf Naguib, Ahmed Naguib
Abstract: Methods and systems for making intermediates in the synthesis of onapristone are provided. Aspects include the photoconversion of onapristone synthesis intermediates using a narrow band frequency light source.
Abstract: Described herein are nucleic acid prodrugs and nucleic acid prodrugs comprising chiral phosphorous moieties. Also described herein are methods of making and using nucleic acid prodrugs and nucleic acid prodrugs comprising chiral phosphorous moieties.
Type:
Grant
Filed:
May 27, 2016
Date of Patent:
June 4, 2019
Assignee:
WAVE LIFE SCIENCES LTD.
Inventors:
Gregory L. Verdine, Meena, Naoki Iwamoto
Abstract: The invention provides various novel compositions of berberine in combination with pharmacologically active organic acids, and related methods of their use in treating various diseases or disorders. The invention further provides various novel compounds prepared from berberine and pharmacologically active organic acids and prepared from ursodeoxycholic acid and pharmacologically active organic bases, and pharmaceutical compositions thereof, and methods of their preparation and therapeutic use in treating and/or preventing various diseases or disorders.
Abstract: The invention relates to polymorphous crystal modifications of a DPP-IV inhibitor, the preparation thereof and the use thereof for preparing a medicament.
Type:
Grant
Filed:
October 5, 2017
Date of Patent:
May 28, 2019
Assignee:
Boehringer Ingelheim International GmbH
Inventors:
Peter Sieger, Dirk Kemmer, Peter Kohlbauer, Thomas Nicola, Martin Renz
Abstract: The invention encompasses novel pyrazolyltriazolylpyridines of the general formula (I) in which the radicals A1-A4, W, Q, R1, R5 and Z1-Z3 have the meanings given in the description. Also described are processes for preparing the compounds of the formula (I). The compounds according to the invention are especially suitable for controlling insects and arachnids in agriculture, and ectoparasites in veterinary medicine.
Type:
Grant
Filed:
June 15, 2015
Date of Patent:
May 28, 2019
Assignee:
BAYER ANIMAL HEALTH GMBH
Inventors:
Hans-Georg Schwarz, Werner Hallenbach, Ulrich Görgens, Kerstin Ilg, Andreas Turberg
Abstract: The disclosure is directed to compounds and compositions that inhibit Ataxia Telengiectasia And Rad3-Related (ATR) Protein Kinase and methods of their use.
Type:
Grant
Filed:
April 12, 2017
Date of Patent:
May 28, 2019
Assignee:
Atrin Pharmaceuticals LLC
Inventors:
Henry Joseph Breslin, Oren Gilad, Gerhard Sperl, Eric J. Brown, Laura Butler
Abstract: The present invention provides inventive stitched polypeptides, pharmaceutical compositions thereof, and methods of making and using inventive stitched polypeptides.
Type:
Grant
Filed:
September 23, 2016
Date of Patent:
May 28, 2019
Assignee:
President and Fellows of Harvard College
Abstract: The present invention relates to azaindole acetic acid derivatives of formula (I), wherein R1 and R2 are as described in the description, and their use as prostaglandin receptor modulators, most particularly as prostaglandin D2 receptor modulators, in the treatment of various prostaglandin-mediated diseases and disorders, to pharmaceutical compositions containing these compounds and to processes for their preparation.
Type:
Grant
Filed:
December 14, 2017
Date of Patent:
May 28, 2019
Assignee:
IDORSIA PHARMACEUTICALS LTD
Inventors:
Hamed Aissaoui, Christoph Boss, Patrick Bouis, Julien Hazemann, Romain Siegrist
Abstract: A method of identifying or evaluating skin-care actives that improve the metabolism of a skin cell. The method includes contacting cells with a stressor and a test agent and determining a response of the cells to the stressor and test agent, based on the change in metabolic indicators associated with glycolysis and/or oxidative phosphylation. The test agent may be identified as a skin-care active when the oxidative phosphorylation and/or glycolysis response corresponds to an improvement in cellular metabolism.
Abstract: Described herein in part are silanol based therapeutic payloads comprising a silanol terminus, a divalent spacer moiety, and a drug moiety capable of effecting a target cell or tissue.
Type:
Grant
Filed:
December 18, 2018
Date of Patent:
May 21, 2019
Assignee:
BlinkBio, Inc.
Inventors:
Hanh N. Nguyen, Leslie O. Ofori, Jutta Wanner, Douglas S. Werner
Abstract: The invention provides a method for producing halogenated carbonates, the method comprising reacting a halogenated alcohol or diol with a solid source of carbonyl moiety as a base in an ether.
Type:
Grant
Filed:
September 20, 2016
Date of Patent:
May 21, 2019
Assignee:
UCHICAGO ARGONNE, LLC
Inventors:
Trevor L. Dzwiniel, Krzysztof Pupek, Gregory K. Krumdick
Abstract: A method for measuring concentration of dehydrogenase and substrate thereof in the presence of living cells, wherein an electron mediator that is hard to be reduced by living cells, for example, a compound represented by Formula (I), an electron mediator represented by the Formula (I) and a measurement reagent for dehydrogenase and substrate thereof including the electron mediator are disclosed. A-L-M??(I), wherein A represents a structural part containing at least one anionic group, M represents a structural part for mediating electron transfer and L represents a linker part for linking the A to the M.
Abstract: A compound for an organic photoelectric device is represented by Chemical Formula 1, and an organic photoelectric device, an image sensor and an electronic device include the same.
Type:
Grant
Filed:
November 25, 2015
Date of Patent:
May 14, 2019
Assignee:
Samsung Electronics Co., Ltd.
Inventors:
Seon-Jeong Lim, Takkyun Ro, Tadao Yagi, Kyung Bae Park, Sung Young Yun, Yong Wan Jin, Chul-Joon Heo
Abstract: This invention relates macrocyclic purine derivatives, processes for their preparation, pharmaceutical compositions, and their use in treating viral infections.
Type:
Grant
Filed:
July 12, 2013
Date of Patent:
May 7, 2019
Assignee:
Janssen Sciences Ireland UC
Inventors:
Jean-Francois Bonfanti, Jerome Michel Claude Fortin, Philippe Muller, Frederic Marc Maurice Doublet, Pierre Jean-Marie Bernard Raboisson, Eric Pierre Alexandre Arnoult