Abstract: Methods and assemblies for improving the reaction kinetics of, conserving reactants utilized in, and/or producing a more pure reaction product of, liquid-phase reactions that involve volatile reactants and products are provided. The methods and assemblies herein provide for a feed of reaction liquid to two or more absorption zones, wherein the temperature and/or feed rate of the liquid is independently adjusted prior to introduction into at least one of the two or more absorption zones. More particularly, the temperature and feed rate of the liquid as delivered to each absorption zone can be adjusted independently to optimize the absorption of at least a portion of any gaseous reactants and byproducts from the gaseous product stream and/or to optimize reaction zone conditions. Reaction kinetics may thus be improved, or substantially maintained.
Abstract: The present invention relates to a novel process for the preparation of 1-H-pyrrolidine-2,4-dione derivatives and to novel intermediates and to a process for their preparation.
Abstract: The present invention relates to modulators of ATP-Binding Cassette (“ABC”) transporters or fragments thereof, including CF Transmembrane Regulator (“CFTR”), compositions thereof, and methods therewith. The present invention also relates to methods of treating ABC transporter mediated diseases using such modulators.
Type:
Grant
Filed:
November 14, 2013
Date of Patent:
October 7, 2014
Assignee:
Vertex Pharmaceuticals Incorporated
Inventors:
Sara S. Hadida Ruah, Mark T. Miller, Ashvani K. Singh, Thomas Cleveland, Lewis R. Makings, Matthew Hamilton, Peter D. J. Grootenhuis
Abstract: Described herein are compounds that are estrogen receptor modulators. Also described are pharmaceutical compositions and medicaments that include the compounds described herein, as well as methods of using such estrogen receptor modulators, alone and in combination with other compounds, for treating diseases or conditions that are mediated or dependent upon estrogen receptors.
Abstract: The present invention relates to novel bipyridyl derivatives of formula (I) and to the use of such compounds in which the inhibition, regulation and/or modulation of signal transduction by ATP consuming proteins like kinases plays a role, particularly to inhibitors of TGF-beta receptor kinases, and to the use of such compounds for the treatment of kinase-induced diseases, in particular for the treatment of tumors.
Type:
Grant
Filed:
June 7, 2011
Date of Patent:
September 30, 2014
Assignee:
Merck Patent GmbH
Inventors:
Guenter Hoelzemann, Dieter Dorsch, Alfred Jonczyk, Christiane Amendt, Frank Zenke
Abstract: Fluorosulfuric acid esters can be produced by reacting alcohols with sulfuryl fluoride (SO2F2) in the presence of a base and water. As a substrate thereof, optically active secondary alcohols are preferable, and optically active ?-hydroxyesters and optically active 4-hydroxyprolines are particularly preferable. By performing the reaction in a two-phase system in the presence of a reaction solvent immiscible with water, a desired reaction proceeds particularly well. The present invention is a production method solving all the problems involved in conventional techniques while being industrially practicable.
Abstract: The present invention provides compounds having formula (I): and additionally provides methods for the synthesis thereof, compositions thereof, and methods for the use thereof in the treatment of various disorders including cancer, metastasis and disorders involving increased angiogenesis, wherein R1-R6, Ra-Rc, Q, Y1, Y2 and n are as defined herein.
Type:
Grant
Filed:
November 30, 2012
Date of Patent:
September 16, 2014
Assignee:
Sloan-Kettering Institute for Cancer Research
Inventors:
Samuel J. Danishefsky, Christoph Gaul, Jon T. Njardarson
Abstract: Embodiments provided herein relate to molecules, compositions, and methods for light absorption. In some embodiments, the molecules and/or compositions can be used to absorb ultraviolet light. In some embodiments, the ultraviolet light absorption compound can be used in a sunscreen composition. In some embodiments, the compound includes an azobenzene group for the absorption of ultraviolet light.
Abstract: Novel fluorescent markers of Formula I: are disclosed herein, wherein X and Y are independently or together absent or are independently selected from R and R1 are independently selected from H and alkyl; Ar is phenyl or heteroaryl; L is absent or a spacer selected from the group consisting of —NH—; —(CH2)nNH—; —NHSO2—; —(CH2)nNHCO—; -(cycloalkyl)NHCO—; —(CH2)nNHSO2—; -(cycloalkyl)NHSO2—; —CONH(CH2)nNHCO—; —CONH(cycloalkyl)NHCO—; —NHCO(CH2)nNHCO—; —NHCO(cycloalkyl)NHCO—; —(CH2)nSO2NH—; -(cycloalkyl)SO2NH—; —(CH2)nNHCSNH—; -(cycloalkyl)NHCSNH—; —CR?CR1—; —C?C—; —(CH2)nN?CH—; -(cycloalkyl)N?CH—; —N?CH(CH2)—; —N?CH(cycloalkyl)-; n is an integer ranging from 1 to 5; F is a fluorophore selected from the group consisting of fluorescein, rhodamine, eosin, thionine, safranin, coumarin, methoxycoumarin, dansyl, BODIPY and BODIPY derivatives; and wherein X, Y and L may be positioned in a 1,3,5; 1,2,3; 1,3,4 or in a 3,4,5 configuration respectively.
Abstract: The invention relates to a novel way to synthesize acrylonitrile from a renewable raw material and more particularly relates to a method for producing acrylonitrile by the ammoxidation of glycerol in gaseous phase. The method can be implemented in a single step, or the glycerol can be previously submitted to a dehydration step. The acrylonitrile thus obtained meets the requirements of green chemistry.
Abstract: The new active compound combinations comprising compounds of the formula (I) and the active compounds (1) to (3) recited in the description possess very good insecticidal and/or acaricidal properties.
Type:
Grant
Filed:
July 11, 2007
Date of Patent:
August 26, 2014
Assignee:
Bayer CropScience AG
Inventors:
Reiner Fischer, Wolfram Andersch, Thomas Bretschneider, Anton Kraus, Heike Hungenberg, Olga Malsam
Abstract: A polyfunctional polyoxyalkylene compound represented by the following formula (1): wherein Z represents a hydroxyl group-removed residue of pentaerythritol or dipentaerythritol, R represents a hydrocarbon group having 1 to 24 carbon atoms, OA1 and OA2 represent an oxyalkylene group having 2 to 4 carbon atoms, L1 and L2 represent an alkylene group which may have an ester bond or the like in the alkylene chain or at the terminal end, and X represents a functional group capable of reacting chemically; R, OA1, OA2, L1, and L2 are the same or different from one another in one molecule, m and n are an average number of moles of the oxyalkylene group added, m represents 5 to 1,000, and n represents 0 to 1,000; p and q represent 0 or 1; r1+r2=4 or 6; and r1 and r2 are an integer of 2 or more.
Abstract: The invention relates to (among other things) oligomer-PTK inhibitor conjugates and related compounds. A compound of the invention, when administered by any of a number of administration routes, exhibits advantages over PTK inhibitor compounds lacking a water soluble, non peptidic oligomer.
Abstract: The present invention discloses various immunosuppressants, salts and polymorphs thereof useful in the treatment of various disorders, including peripheral neuropathy. The invention also discloses pharmaceutical formulations utilizing the immunosuppressants, alone or in combination with other compounds, useful in treating disorders such as peripheral neuropathy. The present invention also discloses a method of treating peripheral neuropathy with immunosuppressants disclosed herein.
Type:
Grant
Filed:
March 6, 2013
Date of Patent:
August 19, 2014
Assignee:
Novartis AG
Inventors:
David Leppert, Erik Wallstroem, Barbara Nuesslein-Hildesheim
Abstract: The present invention relates in part to a process for the preparation of a proline derivative of formula I wherein, R1 is C1-7-alkyl or wherein R4 is selected from the group consisting of C1-7-alkyl, halogen-C1-7-alkyl and phenyl optionally substituted by halogen; R2 is halogen or halogen-C1-7-alkyl; and R3 is selected from the group consisting of hydrogen, halogen, halogen-C1-7-alkyl, C1-7-alkoxy, halogen-C1-7-alkoxy and a 5- or 6-membered heterocyclic ring containing one or two nitrogen atoms, said ring being optionally substituted by C1-7-alkyl or halogen. The proline derivatives of the formula I are preferential inhibitors of the cysteine protease Cathepsin S and are therefore useful to treat metabolic diseases like diabetes, atherosclerosis, abdominal aortic aneurysm, peripheral arterial disease and diabetic nephropathy.
Type:
Grant
Filed:
November 8, 2012
Date of Patent:
August 5, 2014
Assignee:
Hoffmann-La Roche Inc.
Inventors:
Bjoern Bartels, Fritz Bliss, Philipp Cueni, Christophe Pfleger, Ulrich Zutter
Abstract: The invention relates to the 5S,4R-enantiomer of 2-(5-methyl-2-oxo-4-phenyl-pyrrolidin-1-yl)-acetamide with cognition enhancing activity of high pharmacological value and to its preparation method which includes the synthesis of 5S-methyl-4R-phenylpyrrolidin-2-one, its N-alkylation with ethyl haloacetate and the treatment of intermediate ethyl 2-(5S-methyl-2-oxo-4R-phenyl-pyrrolidin-1-yl)-acetate with ammonia.
Type:
Grant
Filed:
November 4, 2010
Date of Patent:
July 29, 2014
Assignee:
JSC Grindeks
Inventors:
Ivars Kalvins, Antons Lebedevs, Aleksandrs Cernobrovijs, Maija Dambrova, Liga Zvejniece, Maksims Vorona, Grigorijs Veinbergs
Abstract: This invention relates generally to stimulating neurogenesis (e.g., post-natal neurogenesis, e.g., post-natal hippocampal neurogenesis) and protecting from neuron cell death.
Type:
Grant
Filed:
January 14, 2013
Date of Patent:
July 29, 2014
Assignee:
Board of Regents of the University of Texas System
Inventors:
Steven L. McKnight, Andrew A. Pieper, Joseph M. Ready, Jef K. De Brabander
Abstract: The invention is directed to arylpyrrolidines compounds which exhibit excellent insecticidal efficacy and which may be used as in the agrochemical field or in the vield of veterinary medicine. The compounds are represented by formula (I): wherein the respective substituents are defined in the specification.
Abstract: Provided are a thiol-reactive polyoxyalkylene-modified lipid which can be used to chemically modify bioactive substances and which can be used for drug delivery systems such as liposomes and a method for producing the same. The polyoxyalkylene-modified lipid is represented by the following formula (1): (wherein, R1 and R2 are hydrocarbon groups which are the same as or different from each other and which contain 4 to 24 carbon atoms, R3 is a divalent hydrocarbon group containing 1 to 6 carbon atoms, OA is oxyalkylene groups containing 2 to 4 carbon atoms, n is the average addition mole number of the oxyalkylene groups and is 5 to 1,000, and Z is a group containing either maleimide or iodoacetamide.
Abstract: This invention relates to compounds of formula (I) which are activators of glucokinase and thus may be useful for the management, treatment, control, or adjunct treatment of diseases, where increasing glucokinase activity is beneficial.
Type:
Grant
Filed:
July 12, 2013
Date of Patent:
October 7, 2014
Assignee:
Novo Nordisk A/S
Inventors:
Anthony Murray, Jesper Lau, Lone Jeppesen, Per Vedsoe, Michael Ankersen, Jane Marie Lundbeck, Marit Kristiansen, Maria Carmen Valcarce Lopez, Dharma Rao Polisetti, Govindan Subramanian, Robert Carl Andrews, Daniel P. Christen, Jeremy T. Cooper, Kalpathy Chidambareswaran Santhosh