Enzyme Inactivation By Chemical Treatment Patents (Class 435/184)
  • Patent number: 10301304
    Abstract: The present invention relates to a compound useful as a selective inhibitor of PI3K?. The invention also provides pharmaceutically acceptable compositions comprising said compounds and methods of using the compositions in the treatment of various disease, conditions, or disorders.
    Type: Grant
    Filed: September 25, 2014
    Date of Patent: May 28, 2019
    Assignee: VERTEX PHARMACEUTICALS INCORPORATED
    Inventors: Michael John Boyd, Alex Aronov, Hardwin O'Dowd, Jeremy Green
  • Patent number: 10301283
    Abstract: Provided herein are 2-(2,4-difluorophenyl)-1,1-difluoro-1-(5-substituted-pyridin-2-yl)-3-(1H-tetrazol-1-yl)propan-2-ols and 1-(2,4-difluorophenyl)-2,2-difluoro-2-(5-substituted-pyridin-2-yl)ethanones and processes for their preparation.
    Type: Grant
    Filed: February 1, 2018
    Date of Patent: May 28, 2019
    Assignee: Dow Agrosciences, LLC
    Inventors: William J. Hoekstra, Nakyen Choy, Carl DeAmicis, Daniel Knueppel, Jim Renga, Michael T. Sullenberger, Gregory Whiteker, Yuanming Zhu, Gary D. Gustafson
  • Patent number: 10206893
    Abstract: Compounds that modulate the oxidoreductase enzyme indoleamine 2,3-dioxygenase, and compositions containing the compounds, are described herein. The use of such compounds and compositions for the treatment and/or prevention of a diverse array of diseases, disorders and conditions, including cancer- and immune-related disorders, that are mediated by indoleamine 2,3-dioxygenase is also provided.
    Type: Grant
    Filed: February 1, 2017
    Date of Patent: February 19, 2019
    Assignee: Flexus Biosciences, Inc.
    Inventors: Hilary Plake Beck, Juan Carlos Jaen, Maksim Osipov, Jay Patrick Powers, Maureen Kay Reilly, Hunter Paul Shunatona, James Ross Walker, Mikhail Zibinsky, James Aaron Balog, David K. Williams, Jay A. Markwalder, Steven P. Seitz, Emily Charlotte Cherney, Liping Zhang, Weifang Shan, Weiwei Guo, Audris Huang
  • Patent number: 10174130
    Abstract: The present invention relates to a process for the liquefaction of starch present in a starch slurry comprising degraded starch and having a DE of from 0.05 to 9. Preferably, the invention relates to a process for the liquefaction of starch present in a starch slurry comprising degraded starch, said starch slurry having a high dry substance. Further preferably, the invention relates to a continuous process for liquefaction of starch present in a starch slurry comprising degraded starch and having a high dry substance.
    Type: Grant
    Filed: August 7, 2013
    Date of Patent: January 8, 2019
    Assignee: Cargill, Incorporated
    Inventors: Frank Derez, Jos Willy Ghislain Corneel De Sadeleer, Joost Ketsman, Luigi Nataloni
  • Patent number: 9951014
    Abstract: Compounds and related methods for inhibition of mammalian and bacterial nitric oxide synthase.
    Type: Grant
    Filed: November 4, 2015
    Date of Patent: April 24, 2018
    Assignee: Northwestern University
    Inventors: Richard B. Silverman, Qing Jing, Soosung Kang, Heng-Yen Wang
  • Patent number: 9908899
    Abstract: The compounds provided herein are phenyl analine amides and are useful for inhibiting histone deacteylase (“HDAC”) enzymes, such as HDAC1, HDAC2, and HDAC3.
    Type: Grant
    Filed: October 28, 2016
    Date of Patent: March 6, 2018
    Assignee: BIOMARIN PHARMACEUTICAL INC.
    Inventors: Vincent Jacques, James R. Rusche, Norton P. Peet, Jasbir Singh
  • Patent number: 9789095
    Abstract: Provided herein are methods for identifying compounds that are inhibitors of a calcium-activated chloride channel. Aminothiophene and aminothiazole compounds, and compositions comprising these compounds, described herein that inhibit efflux of chloride through a calcium-activated chloride channel are useful for treating diseases, disorders, and sequelae of diseases, disorders, and conditions that are associated with aberrantly increased chloride and fluid secretion, for example, secretory diarrhea.
    Type: Grant
    Filed: April 16, 2015
    Date of Patent: October 17, 2017
    Assignee: The Regents of the University of California
    Inventors: Alan S. Verkman, Ricardo De La Fuente Gonzalez
  • Patent number: 9694081
    Abstract: The invention relates to compositions comprising (i) biocompatible hydrogel and (ii) one or more therapeutic agents contained within said hydrogel; wherein the hydrogel is cross-linked utilizing a cross-linker comprising a peptide sequence that is capable of being degraded by an enzyme; the therapeutic agent being effective as a treatment of a condition related to the presence of the enzyme.
    Type: Grant
    Filed: June 17, 2011
    Date of Patent: July 4, 2017
    Assignee: The Trustees Of The University Of Pennsylvania
    Inventors: Jason Alan Burdick, Robert C. Gorman, Joseph H. Gorman, III, Brendan Patrick Purcell
  • Patent number: 9586962
    Abstract: Disubstituted octahydropyrrolo[3,4-c]pyrrole compounds are described, which are useful as orexin receptor modulators. Such compounds may be useful in pharmaceutical compositions and methods for the treatment of diseased states, disorders, and conditions mediated by orexin activity, such as insomnia.
    Type: Grant
    Filed: April 20, 2012
    Date of Patent: March 7, 2017
    Assignee: Janssen Pharmaceutica NV
    Inventors: Michael A. Letavic, Dale A. Rudolph, Brad M. Savall, Brock T. Shireman, Devin Swanson
  • Patent number: 9540395
    Abstract: This invention relates to generally inhibiting histone deacetylase (HDAC) enzymes (e.g., HDAC1, HDAC2, and HDAC3).
    Type: Grant
    Filed: February 28, 2012
    Date of Patent: January 10, 2017
    Assignee: BIOMARIN PHARMACEUTICAL INC.
    Inventors: Vincent Jacques, James R. Rusche, Norton P. Peet, Jasbir Singh
  • Patent number: 9464138
    Abstract: The present invention relates to a method for producing a domain antibody in a yeast, wherein the formation of disulfide bridges in the domain antibody is promoted. The method encompasses the addition of oxidizing agents, preferably oxidizing metal ions, preferably one or more selected from Cu2+, Fe2+, Fe3+ and Zn2+.
    Type: Grant
    Filed: April 30, 2010
    Date of Patent: October 11, 2016
    Assignee: Ablynx N.V.
    Inventors: Peter Schotte, Patrick Stanssens, Christine Labeur, Jean-Luc Jonniaux, Marc Jozef Lauwereys
  • Patent number: 9241994
    Abstract: The present inventor discovered stabilizing agents/stabilizing conditions for suppressing isomerization reactions of sc(Fv)2. It was also discovered that the above-mentioned isomerization reactions can be suppressed through use of freeze-dried formulations. As disclosed herein, by applying the discovered stabilizing agents/stabilizing conditions or the freeze-dried formulation, the isomerization reaction of an sc(Fv)2-type molecule from the bivalent scFv type to the single chain diabody type, and/or the isomerization reaction from a single chain diabody type to a bivalent scFv type can be suppressed in both directions or one direction.
    Type: Grant
    Filed: June 9, 2006
    Date of Patent: January 26, 2016
    Assignee: Chugai Seiyaku Kabushiki Kaisha
    Inventor: Tomoyuki Igawa
  • Patent number: 9182402
    Abstract: Compositions and methods are provided for preventing or attenuating cancer progression or blocking metastasis in prostate cancer and other cancers (e.g., ovarian carcinoma, endometrial cancer, renal cell carcinoma) that are characterized by overexpression of the type II cell surface serine protease hepsin, based on the discovery of multiple disclosed compounds having activity as specific hepsin inhibitors.
    Type: Grant
    Filed: January 16, 2014
    Date of Patent: November 10, 2015
    Assignee: Fred Hutchinson Cancer Research Center
    Inventors: Valeri I. Vasioukhin, John R. Chevillet
  • Publication number: 20150148345
    Abstract: Provided herein are methods, compositions, and kits for treating myeloproliferative disorders or neoplasms, including polycythemia vera, primary myelofibrosis, thrombocythemia, and essential thrombocythemia.
    Type: Application
    Filed: November 25, 2014
    Publication date: May 28, 2015
    Inventors: Brian Lannutti, Sarah Meadows, Christophe Queva, Matthew Robert Warr, James Andrew Whitney
  • Publication number: 20150148375
    Abstract: The present invention relates to bicyclic heterocycles which are inhibitors of BET proteins such as BRD2, BRD3, BRD4, and BRD-t and are useful in the treatment of diseases such as cancer.
    Type: Application
    Filed: November 26, 2014
    Publication date: May 28, 2015
    Applicant: Incyte Corporation
    Inventors: Eddy W. Yue, Andrew P. Combs, Andrew W. Buesking
  • Publication number: 20150147304
    Abstract: The invention relates to a method of inducing Foxp3 expression in a T cell comprising (i) stimulating a T cell (ii) inhibiting signalling via PI3K alpha or PI3K delta or m-TOR or Akt in said T cell, wherein said inhibition is commenced 10 to 22 hours after the stimulation of (i). The invention also relates to certain uses of PI3K inhibitors, PI3K inhibitors for particular uses, and kits.
    Type: Application
    Filed: October 29, 2014
    Publication date: May 28, 2015
    Inventor: Matthias Michael Merkenschlager
  • Publication number: 20150148373
    Abstract: The invention provides heterocyclic guanidine compounds that inhibit F1F0-ATPase, and methods of using heterocyclic guanidine compounds as therapeutic agents to treat medical disorders, such as an immune disorder, inflammatory condition, or cancer.
    Type: Application
    Filed: June 7, 2013
    Publication date: May 28, 2015
    Inventors: Alexander R. Hurd, Clarke B. Taylor, Peter L. Toogood
  • Publication number: 20150141408
    Abstract: The present invention relates to tricyclic pyrrolo derivatives which modulate the activity of protein kinases and are therefore useful in treating diseases caused by dysregulated protein kinase activity. The present invention also provides methods for preparing these compounds, pharmaceutical compositions comprising these compounds, and methods of treating diseases utilizing such these compounds or the pharmaceutical compositions containing them.
    Type: Application
    Filed: January 30, 2015
    Publication date: May 21, 2015
    Applicant: NERVIANO MEDICAL SCIENCES S.R.L.
    Inventors: Marina Caldarelli, Mauro Angiolini, Italo Beria, Maria Gabriella Brasca, Francesco Casuscelli, Roberto D'Alessio, Andrea Lombardi Borgia
  • Publication number: 20150141422
    Abstract: Disclosed herein are new heterocyclic compounds and compositions and their application as pharmaceuticals for the treatment of disease. Methods of inhibiting PAS Kinase (PASK) activity in a human or animal subject are also provided for the treatment of diseases such as diabetes mellitus.
    Type: Application
    Filed: January 26, 2015
    Publication date: May 21, 2015
    Inventors: John M. McCall, Donna L. Romero, Michael Clare
  • Publication number: 20150141463
    Abstract: The present invention provides novel substituted pyrazolone compounds, pharmaceutical acceptable salts and formulations thereof useful in modulating the protein tyrosine kinase activity, and in modulating cellular activities such as proliferation, differentiation, apoptosis, migration and invasion. The invention also provides pharmaceutically acceptable compositions comprising such compounds and methods of using the compositions in the treatment of hyperproliferative disorders in mammals, especially humans.
    Type: Application
    Filed: January 20, 2015
    Publication date: May 21, 2015
    Applicants: CALITOR SCIENCES, LLC, SUNSHINE LAKE PHARMA CO., LTD.
    Inventors: Ning Xi, Yanjun Wu, Min Liao, Yanming Feng
  • Publication number: 20150140033
    Abstract: The present invention describes vaccines that comprise C. perfringens Type alpha toxoids, antigenic fragments thereof, inactivated antigenic fragments of C. perfringens Type alpha toxins, or any combination thereof. The present invention further describes methods of using with these vaccines to protect animals against clostridial diseases. The present invention also describes methods of making these vaccines.
    Type: Application
    Filed: January 29, 2015
    Publication date: May 21, 2015
    Inventors: Huchappa Jayappa, Kevin O'Connell
  • Publication number: 20150140635
    Abstract: A boronic or borinic acid compound is used to inhibit the activity of a sulfenic acid-containing protein. Thus, a biologically-active sulfenic acid-containing protein is contacted with an activity-inhibiting effective amount of a boronic or borinic acid compound of Formula I or a salt, hydrate or solvate thereof, whose components are disclosed within, and that contact is maintained for a time sufficient to inhibit the biological activity of the protein.
    Type: Application
    Filed: December 19, 2014
    Publication date: May 21, 2015
    Inventors: Stephen Benkovic, Chunyu Liu, John W. Tomsho
  • Publication number: 20150140013
    Abstract: Provided herein are methods and compositions related to modulation of the rate of asymmetric proliferation of cancer cells. In some embodiments, the methods described herein relate to the treatment of cancer, at least in part, via the modulation of the rate of asymmetric proliferation of cancer cells.
    Type: Application
    Filed: January 23, 2015
    Publication date: May 21, 2015
    Applicant: THE GENERAL HOSPITAL CORPORATION
    Inventor: Sridhar RAMASWAMY
  • Publication number: 20150141424
    Abstract: Compounds which directly inhibit IRE-1? activity in vitro, prodrugs, and pharmaceutically acceptable salts thereof. Such compounds and prodrugs are useful for treating diseases associated with the unfolded protein response or with regulated IRE1-dependent decay (RIDD) and can be used as single agents or in combination therapies.
    Type: Application
    Filed: January 12, 2015
    Publication date: May 21, 2015
    Inventors: Qingping ZENG, Andras TORO, John Bruce PATTERSON, Warren Stanfield WADE, Zoltan ZUBOVICS, Yun YANG, Zhipeng WU
  • Patent number: 9034903
    Abstract: Inhibitors of the soluble epoxide hydrolase (sEH) are provided that incorporate multiple pharmacophores and are useful in the treatment of diseases. In some embodiments, the present invention provides a method for monitoring the activity of a soluble epoxide hydrolase, the method including contacting the soluble epoxide hydrolase with an amount of a compound of the present invention sufficient to produce a detectable change in the fluorescence of the soluble epoxide hydrolase by interacting with one or more tryptophan residues present in the catalytic site of said sEH.
    Type: Grant
    Filed: February 1, 2013
    Date of Patent: May 19, 2015
    Assignee: The Regents of the University of California
    Inventors: Bruce D. Hammock, Kin Sing Lee, Christophe Morisseau
  • Publication number: 20150133442
    Abstract: The invention features compositions and methods for inhibiting the Pin1 protein, and the treatment of disorders characterized by elevated Pin1 levels.
    Type: Application
    Filed: June 7, 2013
    Publication date: May 14, 2015
    Inventors: Kun Ping Lu, Matthew Brian Boxer, Mindy Irene Emily Davis, Rajan Pragani, Min Shen, Anton Momtchilov Simeonov, Shuo Wei, Xiao Zhen Zhou
  • Publication number: 20150133424
    Abstract: The present disclosure is related to heteroaryl compounds as MEK inhibitors. These compounds include heteroaryl compounds of formula I, their pharmaceutically acceptable salts, combinations with suitable medicament and pharmaceutical compositions thereof. The present disclosure also includes processes of preparation of the compounds and their use in methods of treatment.
    Type: Application
    Filed: March 11, 2013
    Publication date: May 14, 2015
    Inventors: Bhavesh Dave, Rakesh Kumar Banerjee, Samiron Phukan, Abhijit Datta Khoje, Rajkumar Hangarge, Jitendra Sambhaji Jadhav, Venkata P. Palle, Rajender Kumar Kamboj
  • Publication number: 20150133564
    Abstract: Provided are a novel compound, preparing method thereof, and use thereof as inhibitor of histone demethylase. The compound represented by Chemical Formula 1 has activity which inhibits histone demethylase and thus is capable of specifically and effectively inhibit activity of histone demethylase.
    Type: Application
    Filed: April 2, 2014
    Publication date: May 14, 2015
    Applicants: SNU R&DB FOUNDATION, INDUSTRY-ACADEMIC COOPERATION FOUNDATION, YONSEI UNIVERSITY, KOREA INSTITUTE OF SCIENCE AND TECHNOLOGY
    Inventors: Dong-Chan OH, Seong-Hwan KIM, Jongheon SHIN, Hak Cheol KWON, So Hee KWON
  • Publication number: 20150133422
    Abstract: The present invention embodiments relate to compound of Formula I or pharmaceutically acceptable enantiomers, salts or solvates thereof. The invention further relates in certain embodiments to the use of the compounds of Formula I as TDO2 inhibitors. The invention also relates in certain embodiments to the use of the compounds of Formula I for the treatment and/or prevention of cancer, neurodegenerative disorders such as Parkinson's disease, Alzheimer's disease and Huntington's disease, chronic viral infections such as HCV and HIV, depression, and obesity. The invention also relates in certain embodiments to a process for manufacturing compounds of Formula I.
    Type: Application
    Filed: November 8, 2013
    Publication date: May 14, 2015
    Inventors: Stefano Crosignani, Sandra Cauwenberghs, Frederik Deroose
  • Publication number: 20150133402
    Abstract: This invention provides, among other things, novel compounds useful for treating bacterial infections, pharmaceutical compositions containing such compounds, as well as combinations of these compounds with at least one additional therapeutically effective agent.
    Type: Application
    Filed: November 7, 2014
    Publication date: May 14, 2015
    Inventors: STEPHEN J. BAKER, VINCENT S. HERNANDEZ, RASHMI SHARMA, JAMES A. NIEMAN, TSUTOMU AKAMA, YONG-KANG ZHANG, JACOB J. PLATTNER, MICHAEL RICHARD KEVIN ALLEY, RAJESHWAR SINGH, FERNANDO ROCK
  • Patent number: 9029401
    Abstract: The present invention provides compounds for the inhibition of soluble epoxide hydrolase and associated disease conditions.
    Type: Grant
    Filed: February 14, 2012
    Date of Patent: May 12, 2015
    Assignee: The Regents of the University of California
    Inventors: Bruce D. Hammock, Sung Hee Hwang, Aaron T. Wecksler, Christophe Morisseau
  • Publication number: 20150126581
    Abstract: Provided herein are methods for inhibiting expression of DOHH in a cell, and for inhibiting hypusination of eIF5A in a cell, the methods comprising contacting a cell with a miRNA or a nucleic acid molecule encoding the miRNA, wherein the miRNA binds to the 3?UTR of the DOHH mRNA and wherein binding results in a reduction in DOHH expression. Also provided are methods for reducing cellular proliferation and for treating diseases associated with abnormal cellular proliferation.
    Type: Application
    Filed: March 8, 2013
    Publication date: May 7, 2015
    Applicant: The University of Western Australia
    Inventors: Peter Leedman, Keith Giles, Michael Epis, Andrew Barker
  • Publication number: 20150119419
    Abstract: 6-Amino isoquinoline compounds are provided that influence, inhibit or reduce the action of a kinase. Pharmaceutical compositions including therapeutically effective amounts of the 6-aminoisoquinoline compounds and pharmaceutically acceptable carriers are also provided. Various methods using the compounds and/or compositions to affect disease states or conditions such as cancer, obesity and glaucoma are also provided.
    Type: Application
    Filed: December 26, 2014
    Publication date: April 30, 2015
    Inventors: Mitchell A. deLong, Susan M. Royalty, Jill Marie Sturdivant, Geoffrey Richard Heintzelman
  • Publication number: 20150119439
    Abstract: The invention provides saturated acyl guanidine compounds that inhibit F1F0-ATPase, and methods of using saturated acyl guanidine compounds as therapeutic agents to treat medical disorders, such as an immune disorder, inflammatory condition, or cancer.
    Type: Application
    Filed: June 7, 2013
    Publication date: April 30, 2015
    Inventors: Alexander R. Hurd, Clarke B. Taylor, Peter L. Toogood, Chad A. Van Huis
  • Publication number: 20150119348
    Abstract: Natural occurring inhibitors of cyclin-dependent protein kinase 5 (Cdk5), isolated from the root of Rhodiola rosea are structurally different from the known Cdk inhibitors. They show selectivity among different Cdks and efficacy to inhibit Cdk via a mixed-type of inhibition, which should lead to less toxicity and side-effects. They are useful in preventing and treating diseases and disorders associated with aberrant Cdk5 activities, such as acute and/or chronic pain, neuropathic pain, diabetes mellitus, cancer, neurodegenerative diseases and neuropathological disorders.
    Type: Application
    Filed: December 30, 2014
    Publication date: April 30, 2015
    Inventors: Nancy Yuk-Yu IP, Fanny Chui-Fun IP, Wing Yu FU, Guangmiao FU
  • Publication number: 20150119330
    Abstract: Inhibitors of fibroblast activation protein alpha (FAP) and Prolyl Oligopeptidase (POP) are disclosed, along with their use in various therapies related to conditions, diseases, and disorders involving abnormal cell proliferation such as malignancies and angiogenesis, and in neural disorders such as Alzheimer's disease. Stalk portions of the inhibitor molecules, and substrates of FAP and POP, are also disclosed and may be used, for example, in screening methods for identifying such inhibitors.
    Type: Application
    Filed: May 3, 2013
    Publication date: April 30, 2015
    Inventors: Patrick A. McGee, Kenneth W. Jackson, Victoria J. Christiansen
  • Patent number: 9017956
    Abstract: Provided herein are uses of genes for HOG, Ras and cAMP signal transduction pathways to treat fungal infection. To regulate the HOG pathway of Cryptococcus neoformans, roles of SSK1, TCO2, SSK2, PBS2, HOG1, ENA1 and NHA1 genes were investigated to find that a biosynthesis level of ergosterol is increased when these genes are inhibited. When the genes are inhibited, a large amount of ergosterol is distributed on a fungal cell membrane. Accordingly, since there are many working points of an ergosterol-binding antifungal agent, an efficiency of the ergosterol-binding antifungal agent can be considerably improved. To regulate the Ras and cAMP pathways of Cryptococcus neoformans, roles of RAS1, RAS2, CDC24, GPA1, CAC1, ACA1, PKA1, HSP12 and HSP122 genes were investigated to find that a sensitivity to a polyene- or azole-based drug is increased when these genes are inhibited.
    Type: Grant
    Filed: April 15, 2013
    Date of Patent: April 28, 2015
    Assignee: Nutrex Technology Co., Ltd.
    Inventors: Yong-Sun Bahn, Young-Joon Ko, Shin-Ae Maeng, Kwang Woo Jung, Gyu Bum Kim
  • Publication number: 20150110744
    Abstract: There is provided peptides for inhibiting growth of cancer cells, the peptides comprising the amino acid sequence RxKxKxxxxR wherein K and R are respectively lysine and arginine amino acid residues, each x is independently an amino acid, and 5 wherein the peptide has 50% or less amino acid sequence identity with the amino acid sequence RSKAKNPLYR (SEQ ID. No. 2). Each x amino acid may independently be an amino acid residue selected from the group consisting of alanine (A), valine (V), leucine (L), isoleucine (I), threonine (T) and serine (S) amino acid residues. There is also provided chimeric proteins incorporating a peptide of the amino acid sequence 10 RxKxKxxxxR, nucleic acids encoding for the peptide, expression vectors including a nucleic acid encoding the peptide for expression of the peptide, and methods for use of the peptide for inhibiting growth of cancer cells.
    Type: Application
    Filed: January 24, 2013
    Publication date: April 23, 2015
    Inventor: Michael Valentine Agrez
  • Publication number: 20150111872
    Abstract: The present invention discloses compounds according to Formula I: Wherein R1a, R1b, R2, R4, R5, R6a, R6b, R7, R8, W, X, Cy, and the subscript a are as defined herein. The present invention relates to compounds inhibiting autotaxin (NPP2 or ENPP2), methods for their production, pharmaceutical compositions comprising the same, and methods of treatment using the same, for the prophylaxis and/or treatment of diseases involving fibrotic diseases, proliferative diseases, inflammatory diseases, autoimmune diseases, respiratory diseases, cardiovascular diseases, neurodegenerative diseases, dermatological disorders, and/or abnormal angiogenesis associated diseases by administering the compound of the invention.
    Type: Application
    Filed: December 17, 2014
    Publication date: April 23, 2015
    Applicant: GALAPAGOS NV
    Inventors: Nicolas DESROY, Bertrand HECKMANN, Reginald Christophe Xavier BRYS, Agnès Marie JONCOUR, Christophe PEIXOTO, Xavier Marie BOCK
  • Publication number: 20150104846
    Abstract: The present invention provides a method for preserving biological components in pancreatic juice, and a kit suited for this method. The method involves adding, to a pancreatic juice-containing biological sample, at least one sulfonyl fluoride-containing protease inhibitor and at least one trypsin-like serine protease inhibitor belonging to a group of amino acid chloromethyl ketones.
    Type: Application
    Filed: December 19, 2014
    Publication date: April 16, 2015
    Applicant: OLYMPUS CORPORATION
    Inventors: Rie KATAOKA, Nao MORIYA, Hiromi SANUKI
  • Publication number: 20150099750
    Abstract: The instant invention describes compounds having metalloenzyme modulating activity, and methods of treating diseases, disorders or symptoms thereof mediated by such metalloenzymes.
    Type: Application
    Filed: December 1, 2014
    Publication date: April 9, 2015
    Inventors: William J. Hoekstra, Stephen W. Rafferty, Christopher M. Yates, Robert J. Schotzinger, Michael R. Loso, Michael T. Sullenberger
  • Publication number: 20150094314
    Abstract: A method of modulating ribonucleotide reductase activity in a neoplastic cell includes administering to the cell an amount of a ribonucleotide reductase allosteric modulator (RRAmod), the amount being effective to inhibit neoplastic cell growth.
    Type: Application
    Filed: March 21, 2013
    Publication date: April 2, 2015
    Inventor: Chris Dealwis
  • Publication number: 20150094520
    Abstract: A method of reducing or inhibiting kinase activity of C-KIT in a cell or a subject, and the use of such compounds for preventing or treating in a subject a cell proliferative disorder and/or disorders related to C-KIT using a compound of the present invention: or a solvate, hydrate, tautomer or pharmaceutically acceptable salt thereof. The present invention is further directed to methods for treating conditions such as cancers and other cell proliferative disorders.
    Type: Application
    Filed: December 8, 2014
    Publication date: April 2, 2015
    Inventors: Carl R. ILLIG, Shelley K. BALLENTINE, Jinsheng CHEN, Sanath K. MEEGALLA, M. Jonathan RUDOLPH, Mark J. WALL, Kenneth J. WILSON, Renee Louise DESJARLAIS, Carl M. MANTHEY, Christopher J. MOLLOY
  • Publication number: 20150094305
    Abstract: The present invention provides compounds, compositions thereof, and methods of using the same.
    Type: Application
    Filed: September 25, 2014
    Publication date: April 2, 2015
    Inventors: Donna ROMERO, Craig E. MASSE, Shaughnessy ROBINSON, Jeremy Robert GREENWOOD, Geraldine C. HARRIMAN
  • Publication number: 20150087628
    Abstract: K-Ras is the most frequently mutated oncogene in human cancer. Disclosed herein are compositions and methods for modulating K-Ras and treating cancer.
    Type: Application
    Filed: April 10, 2013
    Publication date: March 26, 2015
    Inventors: Jonathan Ostrem, Ulf Peters, Kevan M. Shokat
  • Publication number: 20150087043
    Abstract: Described herein are monomers capable of forming a biologically useful multimer when in contact with one, two, three or more other monomers in an aqueous media. In one aspect, such monomers may be capable of binding to another monomer in an aqueous media (e.g. in vivo) to form a multimer, (e.g. a dimer). Contemplated monomers may include a ligand moiety, a linker element, and a connector element that joins the ligand moiety and the linker element. In an aqueous media, such contemplated monomers may join together via each linker element and may thus be capable of modulating one or more biomolecules substantially simultaneously, e.g., modulate two or more binding domains on a protein or on different proteins.
    Type: Application
    Filed: April 11, 2014
    Publication date: March 26, 2015
    Applicants: Coferon, Inc, Cornell University
    Inventors: Lee Daniel Arnold, Maneesh Pingle, Douglas S. Werner
  • Publication number: 20150087632
    Abstract: The present invention provides cyclobutyl substituted pyrrolopyrimidines and pyrrolopyridines of Formula I: wherein X, Y, Z, L, A, R5, n and m are defined above, as well as their compositions and methods of use, that modulate the activity of Janus kinases (JAKs) and are useful in the treatment of diseases related to the activity of JAKs including, for example, inflammatory disorders, autoimmune disorders, cancer, and other diseases.
    Type: Application
    Filed: December 1, 2014
    Publication date: March 26, 2015
    Applicant: INCYTE CORPORATION
    Inventors: James D. Rodgers, Stacey Shepard, Wenyu Zhu, Lixin Shao, Joseph Glenn
  • Publication number: 20150080344
    Abstract: There are provided, inter alia, acyclic nucleoside phosphonate compounds having reduced toxicity and enhanced antiviral activity, and pharmaceutically accepted salts and solvates thereof. There are also provided methods of using the disclosed compounds for inhibiting viral RNA-dependent RNA polymerase, inhibiting viral reverse transcriptase, inhibiting replication of virus, including hepatitis C virus or a human retrovirus, and treating a subject infected with a virus, including hepatitis C virus or a human retrovirus.
    Type: Application
    Filed: September 29, 2014
    Publication date: March 19, 2015
    Inventors: Karl Y. Hostetler, James R. Beadle, Nadejda Valiaeva
  • Publication number: 20150079634
    Abstract: The present invention is related to a method to reduce peptide amidation activity in a given cell line, cell lines with reduced peptide amidation activity, and uses thereof.
    Type: Application
    Filed: April 16, 2013
    Publication date: March 19, 2015
    Inventors: Mihaela Skulj, Dominik Gaser
  • Publication number: 20150080398
    Abstract: Provided herein are 3,5-diaminopyrazoles, for example, compounds of Formula IA, that are useful for modulating regulated-in-COPD kinase activity, and pharmaceutical compositions thereof. Also provided herein are methods of their use for treating, preventing, or ameliorating one or more symptoms of a RC kinase-mediated disorder, disease, or condition.
    Type: Application
    Filed: November 24, 2014
    Publication date: March 19, 2015
    Inventors: Erik Dean RAAUM, Garrett Thomas POTTER, Tai Wei LY