Abstract: Alternative methods for the detection and measurement of proteases in biological samples and compounds which allow for such detection are required to allow for rapid and selective identification of these enzymes. Compounds which allow for selective identification of these enzymes are provided with assays and kits for their use.
Abstract: The invention provides a new method for the preparation of the dimeric Pd(l) tri-tert.-butylphosphine bromide complex, characterized by the chemical formula [Pd(?-Br)(PtBu3)]2. The method is based on a comproportionation reaction in which a Pd(ll) compound (?PdBr2) is reacted with a Pd(0) compound (?Pd(PtBu3)2) in organic solvents to yield the [Pd(?-Br)(PtBu3)]2 compound having the Pd atoms in the formal oxidation state +1. Unreacted PdBr2 may be reused in the process. The method is straightforward and applicable for industrial scale production and provides high product yields. Further, a new process for the isomerization of allyl ethers of the general type R1—C(O)—O—CH(R2)—C(R3)?CH2 employing the compound Pd?-Br)(PtBu3)]2 as a catalyst is disclosed.
Abstract: Provided in some embodiments are compositions comprising a compound having a structure according to Formula A or Formula B: or a pharmaceutically acceptable salt, tautomer or hydrate thereof, where X2 is a bond or linker, X3 is bond or —PO4—, and X1, R1, R2, R3, and n are described herein. Also provided in some embodiments are methods for making and using such compounds and compositions.
Abstract: The present invention describes branched and functionalized siloxanes and methods for making such compounds. The compounds have a variety of uses. One preferred application is as novel planarizing material for lithography, in which case functionalized branched siloxane, such as an epoxy-modified branched siloxane is particularly useful.
Type:
Grant
Filed:
February 16, 2011
Date of Patent:
October 13, 2015
Assignee:
BOARD OF REGENTS, THE UNIVERSITY OF TEXAS SYSTEM
Inventors:
C. Grant Willson, Tsuyoshi Ogawa, B. Michael Jacobsson
Abstract: The present invention relates to photochromic double-fused naphthopyrans of the general formula (I) or (II) and the use thereof in plastics of all kinds, particularly for ophthalmic purposes. The photochromic compounds according to the invention are characterized by two distinct absorption bands of the open form in the visible wavelength range, i.e. two conventional photochromic dyes, each having only one discrete absorption band, can be replaced with dye molecules of this type. The compounds according to the invention, moreover, have a very good lifetime with a very high performance.
Type:
Grant
Filed:
September 26, 2012
Date of Patent:
October 6, 2015
Assignee:
Rodenstock GmbH
Inventors:
Udo Weigand, Herbert Zinner, Yven Rohlfing
Abstract: The present invention relates to a process for the integrated preparation of 2-substituted 4-hydroxy-4-methyltetrahydropyrans and of 2-substituted 4-methyltetrahydropyrans.
Type:
Grant
Filed:
October 14, 2013
Date of Patent:
September 22, 2015
Assignee:
BASF SE
Inventors:
Timon Stork, Oskar Röder, Klaus Ebel, Ralf Pelzer, Wolfgang Krause, Karl Beck
Abstract: Compounds useful in the synthesis of compounds for treating pain, cancer, inflammation, neurodegenerative disease or Typanosoma cruzi infection in a mammal.
Type:
Grant
Filed:
January 14, 2015
Date of Patent:
September 8, 2015
Assignee:
Array BioPharma, Inc.
Inventors:
Julia Haas, Steven W. Andrews, Yutong Jiang, Gan Zhang
Abstract: The present disclosure provides methods to produce substituted furans (e.g., halomethylfurfural, hydroxymethylfurfural, and furfural), by acid-catalyzed conversion of biomass using a gaseous acid in a multiphase reactor, such as a fluidized bed reactor.
Type:
Grant
Filed:
June 6, 2012
Date of Patent:
September 8, 2015
Assignee:
MICROMIDAS, INC.
Inventors:
Makoto N. Masuno, John Bissell, Ryan L. Smith, Brian Higgins, Alex Be. Wood
Abstract: The present invention relates to novel strigolactam derivatives, to processes and intermediates for preparing them, to plant growth regulator compositions comprising them and to methods of using them for controlling the growth of plants and/or promoting the germination of seeds.
Type:
Grant
Filed:
May 7, 2013
Date of Patent:
September 1, 2015
Assignee:
Syngenta Participations AG
Inventors:
Emmanuelle Villedieu-Percheron, Didier Zurwerra, Mathilde Denise Lachia, Hanno Christian Wolf, Pierre Joseph Marcel Jung, Franciscus Lanfermeijer, Paul Van Den Wijngaard, Claudio Screpanti, Alain De Mesmaeker
Abstract: Abexinostat tosylate of formula (II): and its crystalline form I characterized by its X-Ray powder diffraction diagram, its Raman spectrum and its solid-state 13C CP/MAS NMR spectrum. Medicinal products containing the same which are useful in the treatment of cancer.
Abstract: The present invention provides N-(1-(substituted-phenyl)ethyl)-9H-purin-6-amines derivatives that modulate the activity of phosphoinositide 3-kinases (PI3Ks) and are useful in the treatment of diseases related to the activity of PI3Ks including, for example, inflammatory disorders, immune-based disorders, cancer, and other diseases.
Type:
Grant
Filed:
December 19, 2011
Date of Patent:
August 4, 2015
Assignee:
Incyte Corporation
Inventors:
Yun-Long Li, Andrew P. Combs, Eddy W. Yue, Thomas P. Maduskuie, Jr., Richard B. Sparks
Abstract: The invention provides a method of forming an iron hydroxypyrone compound comprising reacting a hydroxypyrone with a non-carboxylate iron salt in an aqueous solution, and precipitating the iron hydroxypyrone compound from the aqueous solution having a pH of greater than 7.
Abstract: The present invention provides a kind of benzopyrone compounds having a structure of formula (I) and the pharmaceutically acceptable salts or prodrugs thereof, and the pharmaceutical compositions containing such compounds, which can be used to regulate the novel estrogen receptor ER-a36, and prevent and/or treat the related diseases mediated by the ER-a36 receptor, such as cancers, etc.
Abstract: Preparation of acyclovir 2/3 hydrate comprises mixing acyclovir with water at weight ratio of 1:5˜50, dissolving at 50˜100° C., filtering, cooling filtrate at 0˜30° C. to precipitate crystal, collecting the crystal by filtration, and drying the crystal at 0˜150° C. for 0.5˜24 hours to obtain acyclovir 2/3 hydrate. The preparation process is simple and suitable for industrial production. The prepared product has good and stable crystal form.
Abstract: A process is provided for the synthesis of furan and related compounds by vapor phase decarbonylation of furfural and derivatives. The reaction rate, conversion, and selectivity are enhanced by adding water to the feed. The process can be run at lower temperatures than in similar processes run with essentially dry furan and related compounds.
Abstract: The present invention provides fused pyrrole derivatives of Formula I: wherein V, W, X, Y, L, Q, Ar, Z, R1 and R6 are defined herein, that modulate the activity of phosphoinositide 3-kinases (PI3Ks) and are useful in the treatment of diseases related to the activity of PI3Ks including, for example, inflammatory disorders, immune-based disorders, cancer, and other diseases.
Abstract: Provided in some embodiments are compositions comprising a compound having a structure according to Formula A or Formula B: or a pharmaceutically acceptable salt, tautomer or hydrate thereof, where X2 is a bond or linker, X3 is bond or —PO4—, and X1, R1, R2, R3, and n are described herein. Also provided in some embodiments are methods for making and using such compounds and compositions.
Abstract: The present disclosure provides processes for the preparation of a compound of Formula I: which is useful as an antiviral agent. The disclosure also provides compounds that are synthetic intermediates to compounds of formula.
Type:
Grant
Filed:
May 6, 2014
Date of Patent:
June 2, 2015
Assignee:
Gilead Sciences, Inc.
Inventors:
Jared Wayne Evans, Shinji Fujimori, Grace M. Huynh, Qi Liu, Martin Gerald Teresk
Abstract: The present invention relates to processes and intermediates for preparing compounds useful as inhibitors of ATR kinase, such as aminopyrazine-isoxazole derivatives and related molecules. The present invention also relates to compounds useful as inhibitors of ATR protein kinase. The invention relates to pharmaceutically acceptable compositions comprising the compounds of this invention; methods of treating of various diseases, disorders, and conditions using the compounds of this invention; processes for preparing the compounds of this invention; intermediates for the preparation of the compounds of this invention; and solid forms of the compounds of this invention. The compounds of this invention have formula I or II: wherein the variables are as defined herein.
Type:
Grant
Filed:
September 28, 2012
Date of Patent:
May 19, 2015
Assignee:
Vertex Pharmaceuticals Incorporated
Inventors:
Jean-Damien Charrier, John Studley, Francoise Yvonne Theodora Marie Pierard, Steven John Durrant, Benjamin Joseph Littler, Robert Michael Hughes, David Andrew Siesel, Paul Angell, Armando Urbina, Yi Shi