Patents Issued in February 4, 2016
  • Publication number: 20160031789
    Abstract: A process for preparing acrylic acid from methanol and acetic acid, comprising (i) contacting a gaseous stream S0 comprising methanol, oxygen and inert gas with an oxidation catalyst to obtain a gaseous stream S1 comprising formaldehyde and inert gas; (ii) removing at least a portion of the inert gas present in S1 from at least a portion of the formaldehyde present in S1 by absorbing this formaldehyde in an absorbent to obtain a gaseous stream S2 comprising the portion of the inert gas removed, and to obtain a stream S3 comprising absorbent and absorbate comprising formaldehyde; (iii) optionally removing a portion or the entirety of the absorbent present in stream S3, such that a stream S3a remains from stream S3, and producing a stream S4 from at least stream S3 or stream S3a and a stream S5 comprising acetic acid; and (iv) contacting stream S4 in gaseous form with an aldol condensation catalyst to obtain a gaseous stream S6 comprising acrylic acid.
    Type: Application
    Filed: July 9, 2015
    Publication date: February 4, 2016
    Applicant: BASF SE
    Inventors: Lukas SCHULZ, Nicolai Tonio Woerz, Tim Blaschke, Marco Hartmann, Frank Huetten
  • Publication number: 20160031790
    Abstract: A method for the manufacture of 1,8-octanedioic acid comprises: reacting gamma-valerolactone with an alcohol in the presence of an acid or a base catalyst to provide an alkyl pentenoate, converting the alkyl pentenoate in the presence of a metathesis initiator to provide the dialkyl octenedioate, reacting the dialkyl octenedioate with hydrogen in the presence of a hydrogenation catalyst to provide a dialkyl 1,8-octanedioate and hydrolyzing the dialkyl 1,8-octanedioate to provide the 1,8-octanedioic acid.
    Type: Application
    Filed: March 11, 2014
    Publication date: February 4, 2016
    Inventors: ERICH J. MOLITOR, BRIAN D. MULLEN
  • Publication number: 20160031791
    Abstract: A process for the production of acetic acid and dimethyl ether by contacting a mixture of methanol and methyl acetate with a zeolite catalyst wherein the zeolite has a 2-dimensional channel system comprising at least one channel having a 10-membered ring and having at least 5% of its cation exchange capacity occupied by one or more alkali metal cations.
    Type: Application
    Filed: February 22, 2013
    Publication date: February 4, 2016
    Applicant: BP CHEMICALS LIMITED
    Inventors: Thomas Edward CLARK, John Glen SUNLEY
  • Publication number: 20160031792
    Abstract: A method for recovering a composition enriched in 3-hydroxypropionic acid from a fermentation broth comprising 3-hydroxypropionic acid and/or salts thereof comprises the steps of: (a) providing the fermentation broth having a pH of from about 2 to about 8 comprising: 3-hydroxypropionic acid and/or salts thereof, (b) acidifying the fermentation broth; (c) reducing the total sulfate ion and phosphate ion (d) distilling the resulting reduced ion aqueous solution and (e) recovering the product.
    Type: Application
    Filed: March 14, 2014
    Publication date: February 4, 2016
    Applicant: Cargill, Incorporated
    Inventors: Timothy Walter ABRAHAM, Erik ALLEN, John J. HAHN, Paraskevas TSOBANAKIS, Eric Christopher BOHNERT, Christopher Lawrence FRANK
  • Publication number: 20160031793
    Abstract: Processes for the purification of bio-based acrylic acid to crude and glacial acrylic acid are provided. The bio-based acrylic acid is produced from hydroxypropionic acid, hydroxypropionic acid derivatives, or mixtures thereof. The purification includes some or all of the following processes: extraction, drying, distillation, and melt crystallization. The produced glacial or crude acrylic acid contains hydroxypropionic, hydroxypropionic acid derivatives, or mixtures thereof as an impurity.
    Type: Application
    Filed: October 1, 2015
    Publication date: February 4, 2016
    Inventors: Jane Ellen Godlewski, Janette Villalobos Lingoes, Juan Estaban Velasquez, Dimitris Ioannis Collias
  • Publication number: 20160031794
    Abstract: Organic oligomers of acylglycerol having general formula (I): Formula (I), in which M1 and Q1 are organic groups; G11 is a hydroxylpropyl group; G12 and G13 are ?/??-acylglycerols; n is a natural integer from the range [0; 8]; m is a natural integer from the range [0; 4]; and p is a natural integer from the range [0; 3].
    Type: Application
    Filed: March 12, 2014
    Publication date: February 4, 2016
    Applicants: Agronutrition, Institut National Polytechnique De Toulouse, Institut National De La Recherche Agronomique
    Inventors: Zephirin MOULOUNGUI, Zaher ABDEL BAKI, Romain VALENTIN, Bachar ZEBIB
  • Publication number: 20160031795
    Abstract: This invention provides a compound having the structure wherein ?, ?, X, Y, and R1-R11 are defined herein. This invention also provides a pharmaceutical composition comprising the above compounds, a method of inhibiting the activity and/or levels of a matrix metalloproteinase (MMP), a method of inhibiting the production of a cytokine in a population of cells, a method of inhibiting the production of a growth factor in a population of cells, and a method of inhibiting NF?-B activation in a population of cells.
    Type: Application
    Filed: October 14, 2015
    Publication date: February 4, 2016
    Applicants: THE RESEARCH FOUNDATION OF STATE UNIVERSITY OF NEW YORK, CHEM-MASTER INTERNATIONAL, INC.
    Inventors: FRANCIS JOHNSON, LORNE GOLUB
  • Publication number: 20160031796
    Abstract: Substantially stable to degradation Fesoterodine fumarate, a process for its preparation and a process for the synthesis of specific degradation impurities of Fesoterodine fumarate are disclosed.
    Type: Application
    Filed: June 23, 2015
    Publication date: February 4, 2016
    Applicant: Dipharma Francis S.r.l.
    Inventors: Pietro ALLEGRINI, Emanuele ATTOLINO, Renzo GRAZIOSI
  • Publication number: 20160031797
    Abstract: The present invention relates to a novel class of nuclear receptor binding agents (NRBAs). The NRBA compounds are applicable for use in the prevention and/or treatment of a variety of diseases and conditions including, inter alia, prevention and treatment of hormone-related diseases, cancers, inflammation, osteoporosis, peripheral vascular disease, reducing circulating lipid levels, and cardiovascular disease.
    Type: Application
    Filed: June 8, 2015
    Publication date: February 4, 2016
    Inventors: James T. DALTON, Christina Herring, Duane D. MILLER, Seoung-Soo HONG, Yali HE, Michael L. MOHLER, Ramesh NARAYANAN, Zhongzhi WU
  • Publication number: 20160031798
    Abstract: The present invention concerns 2-amino-3-mmethyl-hex-5-enoic acid, its use for the production of peptides such as bacitracins and a method for producing it.
    Type: Application
    Filed: September 9, 2015
    Publication date: February 4, 2016
    Inventors: Martin Mansson, Christine Senstad, Jon Efskind, Vidar Bjornstad
  • Publication number: 20160031799
    Abstract: A method for treating a p62-mediated disease (e.g., multiple myeloma) in a subject, the method comprising administering to the subject a therapeutically effective amount of at least one p62-ZZ inhibitor compound.
    Type: Application
    Filed: June 1, 2015
    Publication date: February 4, 2016
    Inventors: Xiang-Qun Xie, Garson David Roodman, Kyaw-Zeyar Myint, Noriyoshi Kurihara
  • Publication number: 20160031800
    Abstract: Provided are methods for the synthesis of compounds including chiral kynurenine compounds, intermediates useful for the synthesis thereof, and related compounds. For example, methods are provided for the synthesis of L-4-chlorokynurenine.
    Type: Application
    Filed: March 14, 2014
    Publication date: February 4, 2016
    Inventors: Alexander TRETYAKOV, Keith E. DROUET, William SANDERS
  • Publication number: 20160031801
    Abstract: This invention relates to novel 2-amino-3-hydroxypropanoic acid derivatives and pharmaceutically acceptable salts thereof. This invention also provides compositions comprising a compound of this invention and the use of such compositions in methods of treating diseases and conditions that are beneficially treated by administering an NMDA glycine-site antagonist.
    Type: Application
    Filed: August 4, 2015
    Publication date: February 4, 2016
    Applicant: Concert Pharmaceuticals, Inc.
    Inventor: Craig E. Masse
  • Publication number: 20160031802
    Abstract: The present invention pertains to novel 3, 10, and/or 12a-substituted tetracycline compounds. These tetracycline compounds can be used to treat numerous tetracycline compound-responsive states, such as bacterial infections and neoplasms, as well as other known applications for minocycline and tetracycline compounds in general, such as blocking tetracycline efflux and modulation of gene expression.
    Type: Application
    Filed: July 8, 2013
    Publication date: February 4, 2016
    Inventors: Upul Bandarage, Jackson Chen, Mohamed Y. Ismail, Mark L. Nelson, Kwasi Ohemeng
  • Publication number: 20160031803
    Abstract: The present invention includes bis- and tris-benzamide compounds that block AR signaling and have activity against prostate cancer. Uses for these compounds, and pharmaceutical compositions containing the same, also are provided.
    Type: Application
    Filed: July 6, 2015
    Publication date: February 4, 2016
    Applicant: The Board of Regents of the University of Texas System
    Inventors: Jung-Mo AHN, Ganesh RAJ
  • Publication number: 20160031804
    Abstract: Augmented or synergized anti-inflammatory constructs are disclosed including terpenes covalently conjugated with other anti-inflammatory molecules such as nonsteroidal anti-inflammatory drugs, vanilloids, amino acids and polyamines; and anti-inflammatory molecules covalently conjugated with specific amino acids. For the latter, further conjugation with a choline bioisostere further augments the anti-inflammatory activity.
    Type: Application
    Filed: March 14, 2014
    Publication date: February 4, 2016
    Inventors: Jeffrey D. Laskin, Ned D. Heindel, Diane E. Heck, Carl Jeffrey Lacey, Sherri C. Young
  • Publication number: 20160031805
    Abstract: The present invention is directed to compounds of formula I: wherein A is n is 0, 1, or 2; m is 0 or 1; R1 is H or C1-6alkyl and R2 is H, C1-6alkyl, C1-6alkaryl, aryl, or heteroaryl; and X is O or NH. Tautomers, enantiomers, and diastereomers, as well as pharmaceutically acceptable salt forms, of compounds of formula I are also within the scope of the invention. Methods of preparing and using the compounds of formula I are also described.
    Type: Application
    Filed: April 3, 2014
    Publication date: February 4, 2016
    Inventors: Carlo BALLATORE, Kurt R. BRUNDEN, Virginia M.Y. LEE, Amos B. SMITH, John Q. TROJANOWSKI, Xiaozhao WANG
  • Publication number: 20160031806
    Abstract: The present invention is directed to methods comprising adding ammonia, either as an ammonium salt or as a gas at pressures below 0.01 MPa, to a sulfuryl fluoride solution to form the anion of bis(fluorosulfonyl)amine under conditions well suited for large-scale production. The bis(fluorosulfonyl)amine so produced can be isolated by methods described in the prior art, or isolated as an organic ion pair, such as an alkylammonium solid salt, or as an ionic liquid.
    Type: Application
    Filed: October 14, 2015
    Publication date: February 4, 2016
    Inventor: Martin Reid JOHNSON
  • Publication number: 20160031807
    Abstract: The disclosed subject matter provides N-substituted hydroxylamine derivative compounds, pharmaceutical compositions and kits comprising such compounds, and methods of using such compounds or pharmaceutical compositions. In particular, the disclosed subject matter provides methods of using such compounds or pharmaceutical compositions for treating heart failure.
    Type: Application
    Filed: October 9, 2015
    Publication date: February 4, 2016
    Inventors: Vincent Jacob Kalish, Frederick Arthur Brookfield, Stephen Martin Courtney, Lisa Marie Frost, John P. Toscano
  • Publication number: 20160031808
    Abstract: Provided herein are new processes for the preparation of aminosulfone intermediates for the synthesis of 2-[1-(3-ethoxy-4-methoxyphenyl)-2-methylsulfonylethyl]-4-acetylaminoisoindoline-1,3-dione, which is useful for preventing or treating diseases or conditions related to an abnormally high level or activity of TNF-?. Further provided herein are processes for the commercial production of (S)-1-(3-ethoxy-4-methoxyphenyl)-2-methanesulfonylethylamine.
    Type: Application
    Filed: October 14, 2015
    Publication date: February 4, 2016
    Inventors: Jasti Venkateswaralu, Chinnapillai Rajendiran, Nallamaddi Ravikumar Reddy, Terrence Joseph Connolly, Alexander L. Ruchelman, Jeffrey Eckert, Anthony Joseph Frank
  • Publication number: 20160031809
    Abstract: Methods and systems for on-site generation of peracid chemistry, namely peroxycarboxylic acids and peroxycarboxylic acid forming compositions, are disclosed. In particular, an adjustable biocide formulator or generator system is designed for on-site generation of peroxycarboxylic acids and peroxycarboxylic acid forming compositions from sugar esters. Methods of using the in situ generated peroxycarboxylic acids and peroxycarboxylic acid forming compositions are also disclosed.
    Type: Application
    Filed: October 8, 2015
    Publication date: February 4, 2016
    Inventors: Paul R. Kraus, Richard J. Mehus, Katherine M. Sanville, Thomas C. Rustad
  • Publication number: 20160031810
    Abstract: The disclosed compounds have antiviral activity against C-type virus, an optical isomer thereof, a pharmaceutically acceptable salt thereof, a method for preparing the same, and a pharmaceutical composition containing the same as an active ingredient for preventing or treating liver disease caused by hepatitis C virus. The benzidine derivative according to the present invention has excellent antiviral activity against hepatitis C virus and exhibits excellent medicinal activity in the living body, and thus the pharmaceutical composition containing the same as an active ingredient can be useful as a pharmaceutical composition for preventing or treating liver disease, such as acute hepatitis C, chronic hepatitis C, cirrhosis, or hepatocellular carcinoma, caused by C-type virus.
    Type: Application
    Filed: October 15, 2015
    Publication date: February 4, 2016
    Applicants: POSTECH ACADEMY-INDUSTRY FOUNDATION, SEOUL NATIONAL UNIVERSITY R&DB FOUNDATION
    Inventors: Sung Key Jang, Byeong Moon Kim, IL Hak Bae, Jin Kyu Choi, Sun Ju Keum, Seung Gi Lee, Hee Sun Kim
  • Publication number: 20160031811
    Abstract: Disclosed herein are compounds of formula (I) wherein L1, L2, L3, R1, R4, R5, and R6 are as defined in the specification. Compounds of formula (I) are EP4 agonists useful in the treatment of glaucoma, osteoporosis, bone fracture, periodontal bone loss, orthopedic implant, alopecia, neuropathic pain, and related disorders. Pharmaceutical compositions and methods of treating conditions or disorders are also described.
    Type: Application
    Filed: March 14, 2014
    Publication date: February 4, 2016
    Inventors: Stephen Douglas Barrett, Bradlee David Germain, Adam Uzieblo, Fred Lawrence Ciske, Gregory William Endres, Andriy Kornilov, Kirk M. Maxey, James Paul O'Malley, Thomas Allen Owen
  • Publication number: 20160031812
    Abstract: Disclosed herein are small molecule heterocyclic inhibitors of sepiapterin reductase (SPR), and prodrugs and pharmaceutically acceptable salts thereof. The Also featured are pharmaceutical compositions of the compounds and uses of these compounds for the treatment or prevention of pain (e.g., inflammatory pain, nociceptive pain, functional pain, and neuropathic pain).
    Type: Application
    Filed: September 14, 2015
    Publication date: February 4, 2016
    Inventor: Julian Blagg
  • Publication number: 20160031813
    Abstract: Disclosed are compounds which inhibit the activity of NAMPT, compositions containing the compounds and methods of treating diseases during which NAMPT is expressed.
    Type: Application
    Filed: November 11, 2011
    Publication date: February 4, 2016
    Inventors: Michael L. Curtin, Anil Vasudevan, Kevin Woller
  • Publication number: 20160031814
    Abstract: Disclosed herein inter alia are compositions and methods useful in the treatment of diseases, for example pain, neurodegeneration, or mood disorders, and for modulating the activity of a K2P channel.
    Type: Application
    Filed: July 31, 2015
    Publication date: February 4, 2016
    Inventors: Daniel L. Minor, JR., Sviatoslav N. Bagriantsev, Adam R. Renslo
  • Publication number: 20160031815
    Abstract: The present invention relates to new arylaminoalcohol derivatives of formula (I), and to a method for the preparation of such compounds: I The invention also relates to the use of these compounds as medicaments, and in particular for the prevention and/or the treatment of parasitic diseases caused by apicomplexan parasites such as malaria and toxoplasmosis. Finally, the invention relates to pharmaceutical compositions containing such compounds of formula (I) as active principles.
    Type: Application
    Filed: March 14, 2014
    Publication date: February 4, 2016
    Applicant: INSTITUT DE RECHERCHE POUR LE DEVELOPPEMENT
    Inventors: Ignacio ALDANA MORAZA, Silvia Victoria BLAIR TRUJILLO, Eric DEHARO, Giovanny GARAVITO, Adela MENDOZA LIZALDEZ, Silvia PEREZ-SILANES
  • Publication number: 20160031816
    Abstract: The present invention provides compounds of Formula (I): or a stereoisomer, or a pharmaceutically acceptable salt thereof, wherein all of the variables are as defined herein. These compounds are monoacylglycerol acyltransferase type 2 (MGAT2) inhibitors which may be used as medicaments.
    Type: Application
    Filed: October 14, 2015
    Publication date: February 4, 2016
    Inventors: Huji Turdi, Jon J. Hangeland, R. Michael Lawrence, Dong Cheng, Saleem Ahmad, Wei Meng, Robert Paul Brigance, Pratik Devasthale, Guohua Zhao
  • Publication number: 20160031817
    Abstract: The invention relates to 3-piperidone compounds, and in particular, to (2S)-phenyl-3-piperidone and its synthesis method. Use of the thus-synthesized 3-piperidone compounds as potent neurokinin-1 (NK1) receptor antagonists is also provided.
    Type: Application
    Filed: March 17, 2014
    Publication date: February 4, 2016
    Inventors: Teck Peng Loh, Peng Wang, Jingmei Huang, Peng Fei Jackson Koh
  • Publication number: 20160031818
    Abstract: The invention relates to metabolites of cabozantinib (I) as well as uses thereof.
    Type: Application
    Filed: March 17, 2014
    Publication date: February 4, 2016
    Inventors: Dana T. Aftab, Sriram Naganathan, Wei Xu, Steven Lacy, Linh Nguyen
  • Publication number: 20160031819
    Abstract: Novel base addition salts of nitroxoline with improved solubility and increased urine secretion under physiological conditions are described. Pharmaceutical compositions and methods of treatment using the pharmaceutical compositions are also described.
    Type: Application
    Filed: March 17, 2014
    Publication date: February 4, 2016
    Inventor: Ke PAN
  • Publication number: 20160031820
    Abstract: This invention provides compounds of formula (I): wherein R1, R2, G, m, n, p and q have values as described in the specification, useful as inhibitors of HDAC6. The invention also provides pharmaceutical compositions comprising the compounds of the invention and methods of using the compositions in the treatment of proliferative, inflammatory, infectious, neurological or cardiovascular diseases or disorders.
    Type: Application
    Filed: July 7, 2015
    Publication date: February 4, 2016
    Inventors: Christopher Blackburn, Jeffrey P. Ciavarri, Kenneth M. Gigstad, He Xu
  • Publication number: 20160031821
    Abstract: The present disclosure is directed to a reactive ester agent for conjugating a click-reactive group to a carrier molecule or solid support. The reactive ester agent has the general formula IA, wherein the variables R1, R2, R3, Ra and L are described throughout the application.
    Type: Application
    Filed: July 28, 2015
    Publication date: February 4, 2016
    Inventors: Kyle GEE, Aimei CHEN, Hee Chol KANG
  • Publication number: 20160031822
    Abstract: Disclosed are novel pharmaceutical compositions containing 3?-[(2Z)-[1-(3,4-dimethylphenyl)-1,5-dihydro-3-methyl-5-oxo-4H-pyrazol-4-ylidene]hydrazino]-2?-hydroxy-[1,1?-biphenyl]-3-carboxylic acid bis-(monoethanolamine) (eltrombopag olamine) and processes for preparing the same.
    Type: Application
    Filed: September 11, 2015
    Publication date: February 4, 2016
    Applicant: NOVARTIS AG
    Inventors: Shivakumar Kapsi, Francis X. Muller
  • Publication number: 20160031823
    Abstract: Disclosed herein are compounds of formula (I), and methods of inhibiting histone deacetylase (“HDAC”) enzymes (e.g., HDAC1, HDAC2, and HDAC3) using compounds of formula (I).
    Type: Application
    Filed: March 14, 2014
    Publication date: February 4, 2016
    Inventors: Vincent Jacques, James R. Rusche
  • Publication number: 20160031824
    Abstract: The present invention provides novel compounds of Formula (I), and pharmaceutically acceptable salts, solvates, hydrates, polymorphs, co-crystals, tautomers, stereoisomers, isotopically labeled derivatives, prodrugs, and pharmaceutical compositions thereof. The present invention also provides methods and kits using the inventive compounds and pharmaceutical compositions for treating and/or preventing diseases associated with protein aggregation, such as amyloidoses (e.g., Parkinson's disease and Alzheimer's disease), treating and/or preventing neurodegenerative diseases, treating and/or preventing diseases associated with Tar DNA binding protein 43 kDa, reducing or preventing protein aggregation, and/or modulating E3 ubiquitin ligase in a subject in need thereof.
    Type: Application
    Filed: March 17, 2014
    Publication date: February 4, 2016
    Applicants: Whitehead Institute for Biomedical Research, Massachusetts Institute of Technology
    Inventors: Susan L. Lindquist, Stephen L. Buchwald, Daniel Tardiff, Nathan Jui
  • Publication number: 20160031825
    Abstract: Substituted dihydropyrimidinones of formula 1 which are inhibitors of neutrophil elastase activity and which are useful as medicaments for the treatment of, inter alia, COPD.
    Type: Application
    Filed: July 27, 2015
    Publication date: February 4, 2016
    Inventors: Stefan PETERS, Ralf ANDERSKEWITZ, Gerd MORSCHHAEUSER, Thorsten OOST
  • Publication number: 20160031826
    Abstract: Disclosed herein are pyrimidine compounds of formula I and formula II and methods for treating or preventing a viral infection, such as infections caused by dengue virus in a subject, comprising administering to said subject an effective amount of a pyrimidine compound of formula I or formula II.
    Type: Application
    Filed: March 14, 2014
    Publication date: February 4, 2016
    Inventors: Priscilla Yang, Nathanael S. Gray, Chandrasekhar Miduturu, Margaret J. Clark
  • Publication number: 20160031827
    Abstract: It is an object of the present invention to provide a novel form of (S)-trans-{4-[({2-[({1-[3,5-bis(trifluoromethyl)phenyl]ethyl}{5-[2-(methylsulfonyl)ethoxy]pyrimidin-2-yl}amino)methyl]-4-(trifluoromethyl)phenyl}(ethyl)amino)methyl]cyclohexyl}acetic acid, which is useful for preventing and/or treating diseases such as dyslipidemia. (S)-trans-{4-[({2-[({1-[3,5-bis(Trifluoromethyl)phenyl]ethyl}{5-[2-(methylsulfonyl)ethoxy]pyrimidin-2-yl}amino)methyl]-4-(trifluoromethyl)phenyl}(ethyl)amino)methyl]cyclohexyl}acetic acid hydrochloride.
    Type: Application
    Filed: May 30, 2014
    Publication date: February 4, 2016
    Applicant: KOWA COMPANY, LTD.
    Inventors: Koichi YAMAZAKI, Kennosuke MATSUDA, Taichi KUSAKABE, Tadaaki OHGIYA, Kimiyuki SHIBUYA
  • Publication number: 20160031828
    Abstract: The present invention relates generally to the field of antimicrobial compounds and to methods of making and using them. These compounds are useful for treating, preventing, and reducing the risk of microbial infections in humans and animals.
    Type: Application
    Filed: October 16, 2015
    Publication date: February 4, 2016
    Inventors: Erin M. Duffy, Ashoke Bhattacharjee, Hardwin O'Dowd, Marco DeVivo, Yanming Du, Sandra Sinishtaj, Yuanqing Tang, Brian T. Wimberly
  • Publication number: 20160031829
    Abstract: Substituted bicyclic dihydropyrimidinones of formula 1 which are inhibitors of neutrophil elastase and useful as medicaments for the treatment of, inter alia, COPD.
    Type: Application
    Filed: July 27, 2015
    Publication date: February 4, 2016
    Inventors: Thorsten OOST, Ralf ANDERSKEWITZ, Christian GNAMM, Holger HOESCH, Gerd MORSCHHAEUSER, Stefan PETERS, Uwe Joerg RIES
  • Publication number: 20160031830
    Abstract: Substituted dihydropyrimidinones of formula 1 which are neutrophil elastase inhibitors and useful as medicaments for the treatment of, inter alia, COPD.
    Type: Application
    Filed: July 27, 2015
    Publication date: February 4, 2016
    Inventors: Stefan PETERS, Ralf ANDERSKEWITZ, Christian GNAMM, Holger HOESCH, Gerd MORSCHHAEUSER, Thorsten OOST, Uwe Joerg RIES
  • Publication number: 20160031831
    Abstract: Substituted bicyclic dihydropyrimidinones of formula 1 and their use as inhibitors of neutrophil elastase activity.
    Type: Application
    Filed: July 27, 2015
    Publication date: February 4, 2016
    Inventors: Thorsten OOST, Ralf ANDERSKEWITZ, Christian GNAMM, Gerd MORSCHHAEUSER, Stefan PETERS, Uwe Joerg RIES
  • Publication number: 20160031832
    Abstract: A new class of antibiotics effective against methicillin-resistant Staphylococcus aureus (MRSA) is disclosed. Compounds of this class can impair cell-wall biosynthesis by binding to both the allosteric and the catalytic domains of penicillin-binding protein (PBP) 2a. This class of antibiotics holds promise in reversing obsolescence of staphylococcal PBPs as important targets for antibiotics. Embodiments of the invention thus provide novel antibacterial compounds that target penicillin-binding proteins and/or other important cellular targets. Methods for inhibiting the growth and/or replication of bacteria using the compounds described herein are also provided. Various embodiments exhibit activity against gram positive bacteria, including drug-resistant strains of Staphylococcus aureus.
    Type: Application
    Filed: March 5, 2014
    Publication date: February 4, 2016
    Applicant: University of Notre Dame Du Lac
    Inventors: Mayland CHANG, Shahriar MOBASHERY, Renee BOULEY
  • Publication number: 20160031833
    Abstract: Disclosed herein are DKP microcrystals made by an improved method where they do not irreversibly self-assemble into microparticles. The microcrystals can be dispersed by atomization and re-formed by spray drying into particles having spherical shell morphology. Active agents and excipients can be incorporated into the particles by spray drying a solution containing the components to be incorporated into microcrystalline diketopiperazine particles. In particular, the microcrystalline particle compositions are suitable for pulmonary drug delivery of one or more peptides, proteins, nucleic acids and/or small organic molecules.
    Type: Application
    Filed: March 14, 2014
    Publication date: February 4, 2016
    Inventors: Bryan R. Wilson, Joseph J. Guarneri, Marshall L. Grant
  • Publication number: 20160031834
    Abstract: The invention relates to a novel method for producing polyisocyanurates comprising isocyanate groups, based on 2,4- and 2,6-toluylene diisocyanate (TDI) and to the use thereof in coating compositions.
    Type: Application
    Filed: March 7, 2014
    Publication date: February 4, 2016
    Inventors: Josef SANDERS, Andreas HECKING, Reinhard HALPAAP, Frank RICHTER, Oswald WILMES, Jan BUSCH, Tim LODDENKEMPER, Friedhelm STEFFENS, Stefan GROTH
  • Publication number: 20160031835
    Abstract: Compounds of general formula (I), (II), (III) and (V) are described for use in modulating microtubule polymerisation and in the treatment of associated disease states. Use of compounds (I), (III) and (V) in the treatment of kinase-associated disease states is also described. Further described are novel compounds of formula (II), (III) and (V).
    Type: Application
    Filed: July 28, 2015
    Publication date: February 4, 2016
    Inventors: Christopher John Burns, Andrew Frederick Wilks, Michael Francis Harte, Harrison Sikanyika, Emmanuelle Fantino
  • Publication number: 20160031836
    Abstract: The invention is directed, in part, to selective cancer treatment regimes based on assaying for the presence or absence of a mutation in a nucleic acid that encodes MLL1 or for the presence of reduced levels of MLL1.
    Type: Application
    Filed: March 14, 2014
    Publication date: February 4, 2016
    Applicant: Novartis AG
    Inventors: Wenlai zhou, Jinyun CHEN, Christopher WILSON, Yaoyu CHEN
  • Publication number: 20160031837
    Abstract: The present invention provides methods of inducing proliferation of and/or differentiating cells comprising contacting cells with compounds within the methods of the invention. The present invention further provides cells obtainable by the methods of the invention. Liver disease affects more than 500 million people worldwide. Organ transplantation is the gold standard for treatment of liver failure, but organ shortages are acute.
    Type: Application
    Filed: March 14, 2014
    Publication date: February 4, 2016
    Applicants: The Broad Institute, Inc., Massachusetts institute of Technology
    Inventors: Sangeeta Bhatia, Jing Shan, Michelle Palmer, Nathan Ross
  • Publication number: 20160031838
    Abstract: The present disclosure generally relates to compounds having cellular anti-proliferative activities, and more particularly relates to compounds which inhibit the activity of human SMYD2, a SET and MYND domain-containing protein lysine methyltransferase.
    Type: Application
    Filed: July 29, 2015
    Publication date: February 4, 2016
    Inventors: Gary G. Chiang, William N. Pappano, Ramzi F. Sweis, Zhi Wang