Patents Issued in January 25, 2018
  • Publication number: 20180022755
    Abstract: The problem to be solved by the present invention is to provide a compound suitable for a pharmaceutical composition, specifically a pharmaceutically composition for treating nocturia. The inventors have assumed that inhibition of nocturnal activity of placental leucine aminopeptidase (P-LAP), i.e. aminopeptidase that cleaves AVP, would maintain and/or increase an endogenous AVP level to enhance the antidiuretic effect, which would contribute to a decreased number of nocturnal voids, and have extensively studied compounds which inhibit P-LAP. As a result, the inventors have found that (2R)-3-amino-2-(bi-cyclic pyridylmethyl)-2-hydroxy-propanoic acid derivatives have excellent P-LAP inhibitory activity. The inventors have evaluated antidiuretic effects in water-loaded rats and have found that the compounds increase endogenous AVP levels by inhibiting P-LAP and consequently reduce urine production.
    Type: Application
    Filed: November 27, 2015
    Publication date: January 25, 2018
    Applicants: Astellas Pharma Inc., KOTOBUKI PHARMACEUTICAL CO., LTD.
    Inventors: Kenichi KAWAGUCHI, Akihiro ISHIHATA, Akira KANAI, Yusuke INAGAKI, Masashi HIRAMOTO, Kentaro ENJO, Hajime TAKAMATSU
  • Publication number: 20180022756
    Abstract: Disclosed herein are compounds, and pharmaceutical compositions that include such compounds, for preventing or treating hearing loss. The compounds and pharmaceutical compositions described herein prevent or treat hair cell death. In addition, the compounds and pharmaceutical compositions described herein protect against kidney damage in an individual receiving an aminoglycoside antibiotic. Methods of using the compounds, alone or in combination with other therapeutic agents, are also disclosed.
    Type: Application
    Filed: February 5, 2016
    Publication date: January 25, 2018
    Inventors: Julian Simon, Graham Johnson, Edwin W. Rubel, David W. Raible, Mario D. Gonzalez, Peter C. Meltzer, Weishi Miao
  • Publication number: 20180022757
    Abstract: Methods of making compounds of Formula I are disclosed:
    Type: Application
    Filed: June 30, 2017
    Publication date: January 25, 2018
    Inventors: Anna Chiu, John Enquist, JR., Nolan Griggs, Christopher Hale, Norihiro Ikemoto, Katie Ann Keaton, Matt Kraft, Scott E. Lazerwith, Michel Leeman, Zhihui Peng, Kate Schrier, Jonathan Trinidad, Jochem Van Herpt, Andrew W. Waltman
  • Publication number: 20180022758
    Abstract: The present invention provides bicyclic heterocyclyl kinase enzyme inhibitor compounds of formula (I), which are therapeutically useful as kinase inhibitors, particularly IRAK4 inhibitors. wherein A, Y, Z, X1, X2, X3, R1, R3, ‘m’, ‘n’ and ‘p’ have the meanings given in the specification and pharmaceutically acceptable salt or stereoisomer thereof that are useful in the treatment and prevention of diseases or disorder, in particular their use in diseases or disorder mediated by kinase enzyme, particularly IRAK4 enzyme. The present invention also provides pharmaceutical composition comprising at least one of the compounds of compound of formula (I) together with a pharmaceutically acceptable carrier, diluent or excipient therefor.
    Type: Application
    Filed: August 2, 2017
    Publication date: January 25, 2018
    Inventors: Venkateshwar Rao Gummadi, Susanta Samajdar
  • Publication number: 20180022759
    Abstract: The present disclosure relates generally to compounds and compositions, and their use as kinase inhibitors.
    Type: Application
    Filed: September 29, 2017
    Publication date: January 25, 2018
    Inventors: Anthony A. Estrada, Jianwen A. Feng, Brian Fox, Colin Philip Leslie, Joseph P. Lyssikatos, Alfonso Pozzan, Zachary K. Sweeney, Javier de Vicente Fidalgo
  • Publication number: 20180022760
    Abstract: To provide novel pesticides, especially insecticides or acaricides. A condensed heterocyclic compound represented by the formula (1) or its salt or an N-oxide thereof: wherein D substituted with —S(O)nR1 is a ring represented by any one of D1, D2 and D3, Q is a ring represented by any one of Q1, Q2, Q3 and Q4, R1 is C1-C6 alkyl, C1-C6 haloalkyl, (C1-C6) alkyl optionally substituted with R1a, C2-C6 alkenyl, C2-C6 haloalkenyl, C2-C6 alkynyl, C2-C6 haloalkynyl, C3-C6 cycloalkyl, C3-C6 halocycloalkyl, C3-C6 cycloalkyl (C1-C6) alkyl, C3-C6 halocycloalkyl (C1-C6) alkyl or hydroxy (C1-C6) alkyl, R1a is C1-C8 alkoxycarbonyl, and n is an integer of 0, 1 or 2.
    Type: Application
    Filed: February 12, 2016
    Publication date: January 25, 2018
    Applicant: Nissan Chemical Industries, Ltd.
    Inventors: Takao KUDO, Yukihiro MAIZURU, Ayano TANAKA, Kenkichi NOTO, Hiroto MATSUI, Masaki KOBAYASHI
  • Publication number: 20180022761
    Abstract: Mono-substituted TSA precursor Si-containing film forming compositions are disclosed. The precursors have the formula: (SiH3)2N—SiH2—X, wherein X is selected from a halogen atom; an isocyanato group; an amino group; an N-containing C4-C10 saturated or unsaturated heterocycle; or an alkoxy group. Methods for forming the Si-containing film using the disclosed mono-substituted TSA precursor are also disclosed.
    Type: Application
    Filed: August 31, 2017
    Publication date: January 25, 2018
    Inventors: Jean-Marc GIRARD, Peng ZHANG, Antonio SANCHEZ, Manish KHANDELWAL, Gennediy ITOV, Reno PESARESI
  • Publication number: 20180022762
    Abstract: A tris[3-(alkoxysilyl)propyl] isocyanurate from the group of tris[3-(trialkoxysilyl)propyl] isocyanurate, tris[3-(alkyldialkoxysilyl)propyl] isocyanurate and tris[3-(dialkylalkoxysilyl)propyl] isocyanurate is prepared by hydrosilylation, by a) initially charging a mixture of at least one hydroalkoxysilane from the group of hydrotrialkoxysilane, hydroalkyldialkoxysilane, hydrodialkylalkoxysilane [called H-silane(s) for short] and a Pt catalyst, b) heating the mixture to a temperature of 40 to 170° C., c) then adding or metering in 1,3,5-triallyl-1,3,5-triazine-2,4,6(1H,3H,5H)-trione, at least one carboxylic acid and at least one alcohol as cocatalyst while mixing, and d) leaving the mixture to react and then working up the product mixture thus obtained.
    Type: Application
    Filed: July 24, 2017
    Publication date: January 25, 2018
    Applicant: Evonik Degussa GmbH
    Inventors: Philipp ALBERT, Eckhard JUST
  • Publication number: 20180022763
    Abstract: The present invention features compounds effective in inhibiting active against Hepatitis C virus (“HCV”) polymerase. The invention also features processes of making such compounds, compositions comprising such compounds, and methods of using such compounds to treat HCV infection.
    Type: Application
    Filed: May 5, 2017
    Publication date: January 25, 2018
    Applicant: AbbVie Inc.
    Inventors: Jaclyn Chau, Hui-Ju J. Chen, David A. DeGoey, John Hartung, Nathan Ide, Vikram Kalthod, Allan C. Krueger, Yi-Yin Ku, Tongmei Li, John T. Randolph, Rolf Wagner, Geoff T. Halvorsen, Christopher C. Marvin, Eric Voight, Brian S. Brown, Steven R. Martinez, Anurupa Shrestha, Howard R. Heyman
  • Publication number: 20180022764
    Abstract: The invention relates to a process comprising the following process steps: a) introducing an ethylenically unsaturated compound; b) adding a monophosphine ligand and a compound which comprises Pd, or adding a complex comprising Pd and a monophosphine ligand; c) adding an aliphatic alcohol; d) supplying CO; e) heating the reaction mixture, the ethylenically unsaturated compound being reacted to form an ester; where the monophosphine ligand is a compound of formula (I) where R1 is selected from —(C1-C12)-alkyl, —O—(C1-C12)-alkyl, —O—(C6-C20)-aryl, —(C6-C20)-aryl, —(C3-C12)-cycloalkyl, —(C3-C12)-heterocycloalkyl, —(C3-C20)-heteroaryl; R2 is selected from —(C6-C20)-aryl, —(C3-C12)-cycloalkyl, —(C3-C12)-heterocycloalkyl, —(C3-C20)-heteroaryl; R3 is —(C3-C20)-heteroaryl; and R1, R2 and R3 may each independently be substituted by one or more substituents selected from —(C1-C12)-alkyl, —(C3-C12)-cycloalkyl, —(C3-C12)-heterocycloalkyl, —O—(C1-C12)-alkyl, —O—(C1-C12)-alkyl-(C6-C20)-aryl, —O—(C3-C12)-cycloalky
    Type: Application
    Filed: July 14, 2017
    Publication date: January 25, 2018
    Applicant: EVONIK DEGUSSA GMBH
    Inventors: Kaiwu DONG, Ralph JACKSTELL, Matthias BELLER, Dirk FRIDAG, Dieter HESS, Katrin Marie DYBALLA, Frank GEILEN, Robert FRANKE
  • Publication number: 20180022765
    Abstract: The invention relates to a process comprising the following process steps: a) introducing a first alcohol, the first alcohol having 2 to 30 carbon atoms; b) adding a phosphine ligand and a compound which comprises Pd, or adding a complex comprising Pd and a phosphine ligand; c) adding a second alcohol; d) supplying CO; e) heating the reaction mixture, the first alcohol reacting with CO and the second alcohol to form an ester; where the phosphine ligand is a compound of formula (I) where m and n are each independently 0 or 1; R1, R2, R3, R4 are each independently selected from —(C1-C12)-alkyl, —(C3-C12)-cycloalkyl, —(C3-C12)-heterocycloalkyl, —(C6-C20)-aryl, —(C3-C20)-heteroaryl; at least one of the R1, R2, R3, R4 radicals is a —(C3-C20)-heteroaryl radical; and R1, R2, R3, R4, if they are —(C1-C12)-alkyl, —(C3-C12)-cycloalkyl, —(C3-C12)-heterocycloalkyl, —(C6-C20)-aryl or —(C3-C20)-heteroaryl, may each independently be substituted by one or more substituents selected from —(C1-C12)-alkyl, —(C3-C12)-c
    Type: Application
    Filed: July 14, 2017
    Publication date: January 25, 2018
    Applicant: EVONIK DEGUSSA GMBH
    Inventors: Kaiwu DONG, Ralf JACKSTELL, Helfried NEUMANN, Matthias BELLER, Dirk FRIDAG, Dieter HESS, Katrin Marie DYBALLA, Frank GEILEN, Robert FRANKE
  • Publication number: 20180022766
    Abstract: Compounds, methods of use, and processes for making inhibitors of complement factor D comprising Formula I, or a pharmaceutically acceptable salt or composition thereof wherein R12 or R13 on the A group is an ether (R32) are provided. The inhibitors described herein target factor D and inhibit or regulate the complement cascade at an early and essential point in the alternative complement pathway, and reduce factor D's ability to modulate the classical and lectin complement pathways. The inhibitors of factor D described herein are capable of reducing the excessive activation of complement, which has been linked to certain autoimmune, inflammatory, and neurodegenerative diseases, as well as ischemia-reperfusion injury and cancer.
    Type: Application
    Filed: August 14, 2017
    Publication date: January 25, 2018
    Applicant: Achillion Pharmaceuticals, Inc.
    Inventors: Jason Allan Wiles, Venkat Rao Gadhachanda, Godwin Pais, Akihiro Hashimoto, Qiuping Wang, Dawei Chen, Xiangzhu Wang, Atul Agarwal, Milind Deshpande, Avinash S. Phadke
  • Publication number: 20180022767
    Abstract: Compounds, methods of use, and processes for making inhibitors of complement factor D comprising Formula I, or a pharmaceutically acceptable salt or composition thereof are provided. The inhibitors described herein target factor D and inhibit or regulate the complement cascade at an early and essential point in the alternative complement pathway, and reduce factor D's ability to modulate the classical and lectin complement pathways. The inhibitors of factor D described herein are capable of reducing the excessive activation of complement, which has been linked to certain autoimmune, inflammatory, and neurodegenerative diseases, as well as ischemia-reperfusion injury and cancer.
    Type: Application
    Filed: September 11, 2017
    Publication date: January 25, 2018
    Applicant: Achillion Pharmaceuticals, Inc.
    Inventors: Jason Allan Wiles, Avinash S. Phadke, Xiangzhu Wang, Dawei Chen, Akihiro Hashimoto, Venkat Rao Gadhachanda, Godwin Pais, Qiuping Wang, Atul Agarwal, Milind Deshpande
  • Publication number: 20180022768
    Abstract: Alkylphosphocholine analogs incorporating a chelating moiety that chelates a radioactive metal isotope are disclosed herein. The alkylphophocholine analogs, which can be used to treat or detect solid tumors, have the formula: R1 includes a chelating agent that is chelated to a metal atom, wherein the metal atom is a positron or single photon emitting metal isotope with a half life of greater than or equal to 4 hours, or an alpha, beta or Auger emitting metal isotope with a half life of greater than 6 hours and less than 30 days; a is 0 or 1; n is an integer from 12 to 30; m is 0 or 1; Y is —H, —OH, —COOH, —COOX, —OCOX, or —OX, wherein X is an alkyl or an arylalkyl; R2 is —N+H3, —N+H2Z, —N+HZ2, or —N+Z3, wherein each Z is independently an alkyl or an aroalkyl; and b is 1 or 2.
    Type: Application
    Filed: November 4, 2016
    Publication date: January 25, 2018
    Inventors: Jamey Weichert, Anatoly Pinchuk, Reinier Hernandez
  • Publication number: 20180022769
    Abstract: A series of fluorine-containing bisphosphonic acids in which an alkylamine side chain is added, a series of fluorine-containing bisphosphonic acids in which an amino group substituted by a heterocyclic group or a heterocyclic group containing a nitrogen atom is added, to the carbon atom of P—C(F)—P, and a series of fluorine-containing bisphosphonate derivatives in which the acid moiety thereof is esterified by an alkoxymethyl group such as POM group, n-butanoyloxymethyl (BuOM) group and the like, that is, the fluorine-containing bisphosphonic acid and fluorine-containing bisphosphonate derivative represented by the following formula (I): wherein each symbol is as defined in the DESCRIPTION, can efficiently induce proliferation of peripheral blood ?? T cells that express V?2V?2 T cell receptor having superior cytotoxicity against tumor cells and virus infected cells, immunize tumor cells and virus infected cells, and can induce cytotoxicity by ?? T cells.
    Type: Application
    Filed: February 1, 2016
    Publication date: January 25, 2018
    Applicant: Nagasaki University
    Inventors: Yoshimasa TANAKA, Satoshi MIZUTA, Hiroshi UEDA
  • Publication number: 20180022770
    Abstract: A compound of the formula II (I) in which X is substituted pyrrolide with the general structure of (II) in which Ra-Rd are independently selected from H, C1-C4 alkyl, C1-C4 alkoxy, aryl, aryloxy, dialkylamino, diarylamino, halogen, trifluoromethyl, cyano, nitro, sulfonyl and sulfinyl. Y is C1-C6 alkoxy, C1-C10 aryloxy, optionally substituted; R1 is selected from H, C1-C12 alkyl and 5- to 18-membered aryl, optionally substituted; R2 is selected from C1-C12-alkyl, 5- to 18-membered aryl, optionally substituted; R3 is selected from C1-C12 alkyl, 5- to 18-membered aryl, optionally substituted; and 15 124-R11 are independently selected from H, C1-C4 alkyl and halogen. The compounds are particularly effective precursors of metathesis catalysts for the polymerisation of dicyclopentadiene.
    Type: Application
    Filed: March 8, 2016
    Publication date: January 25, 2018
    Inventors: Georg Frater, Henrik Gulyas, Levente Ondi
  • Publication number: 20180022771
    Abstract: Organometallic compounds comprising a chloroquinoline moiety and uses the compounds. The compounds are, for example, manganese or rhenium complexes of a ligand comprising a chloroquinoline moiety. The compounds can be used in, for example, methods of inhibiting cell growth.
    Type: Application
    Filed: January 4, 2016
    Publication date: January 25, 2018
    Inventors: William E. GEIGER, Kevin LAM, Jon E. RAMSEY, Claire F. VERSCHRAEGEN
  • Publication number: 20180022772
    Abstract: Diastereomer mixture comprising diastereomers of the formulae (I.1) and (I.
    Type: Application
    Filed: July 14, 2017
    Publication date: January 25, 2018
    Applicant: EVONIK DEGUSSA GMBH
    Inventors: Kaiwu DONG, Helfried NEUMANN, Ralf JACKSTELL, Matthias BELLER, Dirk FRIDAG, Dieter HESS, Katrin Marie DYBALLA, Frank GEILEN, Robert FRANKE
  • Publication number: 20180022773
    Abstract: Compound of formula (I) where R2, R4 are each independently selected from —(C1-C12)-alkyl, —(C3-C12)-cycloalkyl, —(C3-C12)-heterocycloalkyl, —(C6-C20)-aryl; the R1, R3 radicals are each a —(C3-C20)-heteroaryl radical; R1, R3 may each independently be substituted by one or more substituents selected from —(C1-C12)-alkyl, —(C3-C12)-cycloalkyl, —(C3-C12)-heterocycloalkyl, —O—(C1-C12)-alkyl, —O—(C1-C12)-alkyl-(C6-C20)-aryl, —O—(C3-C12)-cycloalkyl, —S—(C1-C12)-alkyl, —S—(C3-C12)-cycloalkyl, —COO—(C1-C12)-alkyl, —COO—(C3-C12)-cycloalkyl, —CONH—(C1-C12)-alkyl, —CONH—(C3-C12)-cycloalkyl, —CO—(C1-C12)-alkyl, —CO—(C3-C12)-cycloalkyl, —N—[(C1-C12)-alkyl]2, —(C6-C20)-aryl, —(C6-C20)-aryl-(C1-C12)-alkyl, —(C6-C20)-aryl-O—(C1-C12)-alkyl, —(C3-C20)-heteroaryl, —(C3-C20)-heteroaryl-(C1-C12)-alkyl, —(C3-C20)-heteroaryl-O—(C1-C12)-alkyl, —COOH, —OH, —SO3H, —NH2, halogen; R2, R4, if they are —(C1-C12)-alkyl, —(C3-C12)-cycloalkyl, —(C3-C12)-heterocycloalkyl or —(C6-C20)-aryl, may each independently be substituted by one or
    Type: Application
    Filed: July 14, 2017
    Publication date: January 25, 2018
    Applicant: EVONIK DEGUSSA GMBH
    Inventors: Kaiwu DONG, Ralf JACKSTELL, Helfried NEUMANN, Matthias BELLER, Dirk FRIDAG, Dieter HESS, Katrin Marie DYBALLA, Frank GEILEN, Robert FRANKE
  • Publication number: 20180022774
    Abstract: The present invention relates to an improved, commercially viable and industrially advantageous process for the preparation of sofosbuvir, which uses reagents that are less expensive and easier to handle.
    Type: Application
    Filed: May 8, 2017
    Publication date: January 25, 2018
    Inventors: Srinivas Reddy Desi Reddy, Srinivas Rao Velivela
  • Publication number: 20180022775
    Abstract: The present invention further provides method of preparing nanocrystals of a hydrophobic therapeutic agent such as fluticasone or triamcinolone, pharmaceutical compositions (e.g., topical or intranasal compositions) thereof and methods for treating and/or preventing the signs and/or symptoms of disorders such as blepharitis, meibomian gland dysfunction or skin inflammation or a respiratory disease (e.g., asthma).
    Type: Application
    Filed: July 26, 2017
    Publication date: January 25, 2018
    Inventors: Thomas CAVANAGH, Shikha P. Barman, Tian Hao, Thomas B. Leland, Ritesh V. Thekkedath
  • Publication number: 20180022776
    Abstract: The present invention regards specific IBAT inhibitors useful in the prophylaxis and/or treatment of a liver disease. It also relates to compositions comprising these IBAT inhibitors, a method for treatment of the disorders and a kit comprising the substances or the compositions.
    Type: Application
    Filed: October 2, 2017
    Publication date: January 25, 2018
    Inventors: Per-Göran Gillberg, Hans Graffner, Ingemar Starke
  • Publication number: 20180022777
    Abstract: Compounds having activity for lowering parathyroid hormone levels are described. In one embodiment, the compounds are comprised of a contiguous sequence of subunits, X1-X2-X3-X4-X5-X6-X7, wherein the X1 subunit comprises a thiol-containing moiety and the distribution of charge on the X2-X7 subunits provides the desired activity. Methods of using the compounds for treating hyperparathyroidism, bone disease and/or hypercalcemic disorders are also described, and in particular, methods for lowering plasma PTH and serum calcium are provided. The compounds can be used to treat subjects having, for example: primary, secondary or tertiary hyperparathyroidism; hypercalcemia of malignancy; metastatic bone disease; or osteoporosis.
    Type: Application
    Filed: June 21, 2017
    Publication date: January 25, 2018
    Inventors: Felix Karim, Amos Baruch, Derek Maclean, Kanad Das, Qun Yin
  • Publication number: 20180022778
    Abstract: The present invention provides novel peptide inhibitors of the interleukin-23 receptor, and related compositions and methods of using these peptide inhibitors to treat or prevent a variety of diseases and disorders, including inflammatory bowel disease.
    Type: Application
    Filed: February 24, 2017
    Publication date: January 25, 2018
    Inventors: Gregory Bourne, Ashok Bhandari, Xiaoli Cheng, Brian Troy Frederick, Jie Zhang, Dinesh V. Patel, David Liu
  • Publication number: 20180022779
    Abstract: The present invention provides compositions and methods for regulating arterial tone based on the discovery herein of novel expression and regulation of hemoglobin alpha and cytochrome B5 reductase 3 and the effects on NO and NOS.
    Type: Application
    Filed: July 7, 2017
    Publication date: January 25, 2018
    Applicant: University of Virginia Patent Foundation
    Inventors: Benjamin M. Gaston, Adam C. Straub, Brant E. Isakson, Linda Columbus
  • Publication number: 20180022780
    Abstract: The invention relates to novel, biologically active, stabilized Adrenomedullin (ADM) compounds. The invention further relates to the compounds for use in a method for the treatment and/or prevention of diseases, especially of cardiovascular, edematous and/or inflammatory disorders, and to medicaments comprising the compounds for treatment and/or prevention of cardiovascular, edematous and/or inflammatory disorders.
    Type: Application
    Filed: September 24, 2015
    Publication date: January 25, 2018
    Inventors: Donald BIERER, Ingo FLAMME, Johannes KÖBBERLING, Bernd RIEDL, Annette BECK-SICKINGER, Ria SCHOENAUER, Jan-Patrick FISCHER
  • Publication number: 20180022781
    Abstract: The present invention relates to polypeptide for engineering integrase chimeric proteins and their use in gene therapy. In particular, the present invention relates to a polypeptide which comprises the amino acid sequence ranging from the amino acid residue at position 617 to the amino acid residue at position 622 in SEQ ID NO: 1 or a function conservative thereof.
    Type: Application
    Filed: February 12, 2016
    Publication date: January 25, 2018
    Applicants: INSERM (INSTITUT NATIONAL DE LA SANTE ET DE LA RECHERCHE MEDICALE), CENTRE NATIONAL DE LA RECHERCHE SCIENTIFIQUE (CNRS), UNIVERSITE PARIS DIDEROT - PARIS 7, COMMISSARIAT A L'ENERGIE ATOMIQUE ET AUX ENERGIES ALTERNATIVES, CNAM - CONSERVATOIRE NATIONAL DES ARTS ET METIERS
    Inventors: Antoine BRIDIER-NAHMIAS, Michel WERNER, Pascale LESAGE
  • Publication number: 20180022782
    Abstract: The present invention relates to DNA sequences encoding Vmp-like polypeptides of pathogenic Borrelia, the use of the DNA sequences in recombinant vectors to express polypeptides, the encoded amino acid sequences, application of the DNA and amino acid sequences to the production of polypeptides as antigens for immunoprophylaxis, immunotherapy, and immunodiagnosis. Also disclosed are the use of the nucleic acid sequences as probes or primers for the detection of organisms causing Lyme disease, relapsing fever, or related disorders, and kits designed to facilitate methods of using the described polypeptides, DNA segments and antibodies.
    Type: Application
    Filed: May 31, 2017
    Publication date: January 25, 2018
    Inventor: Steven J. NORRIS
  • Publication number: 20180022783
    Abstract: In one aspect, the invention relates to a composition including a first polypeptide having the sequence set forth in SEQ ID NO: 1 and a second polypeptide having the sequence set forth in SEQ ID NO: 2. In one embodiment, the composition includes about 120 ?g/ml of a first polypeptide including the amino acid sequence set forth in SEQ ID NO: 1, 120 ?g/ml of a second polypeptide including the amino acid sequence set forth in SEQ ID NO: 2, about 2.8 molar ratio polysorbate-80 to the first polypeptide, about 2.8 molar ratio polysorbate-80 to the second polypeptide, about 0.5 mg/ml aluminum, about 10 mM histidine, and about 150 mM sodium chloride. In one embodiment, a dose of the composition is about 0.5 ml in total volume. In one embodiment, two-doses of the composition induce a bactericidal titer against diverse heterologous subfamily A and subfamily B strains in a human.
    Type: Application
    Filed: October 10, 2017
    Publication date: January 25, 2018
    Inventors: Annaliesa Sybil Anderson, Rasappa Gounder Arumugham, John Erwin Farley, Leah Diane Fletcher, Shannon Lea Harris, Kathrin Ute Jansen, Thomas Richard Jones, Lakshmi Khandke, Bounthon Loun, John Lance Perez, Gary Warren Zlotnick
  • Publication number: 20180022784
    Abstract: It is described a Clostridium difficile (C-difficile) toxins A and/or B as a target for therapy, including passive immunotherapy, and particularly prevention of C-difficile intoxication in human or other animals. It is also described a polypeptide comprising a portion of C-difficile toxins A and/or B sequence being an epitope for anti-toxins A and/or B antibody. It disclosed a method for generating a neutralizing antibody directed against C-difficile toxins A and/or B. It is also provided a novel formulation that combines key toxins A and/or B epitope antibodies, located in three key domains of toxins A and/or B, for neutralisation of the toxins A and/or B, at any stage of toxins A and/or B intoxication related to C-difficile infection. The novel formulation of toxins A and/or B epitope antibodies are useful in immunotherapy, for 10 therapeutic and/or prophylactic mediation of C-difficile intoxication.
    Type: Application
    Filed: February 19, 2016
    Publication date: January 25, 2018
    Inventors: Simon Gaudreau, Martin Cloutier, Louis-Charles Fortier, Frederic Leduc, Maxime Tremblay, Steeve Veronneau, Djorjde Gbric, Jean-Francois Larrivee
  • Publication number: 20180022785
    Abstract: The invention provides an improved host strain for production of desired protein.
    Type: Application
    Filed: August 15, 2017
    Publication date: January 25, 2018
    Applicant: Albumedix A/S
    Inventors: Christopher John Arthur Finnis, Jennifer Mary Mclaughlan, Per Kristoffer Nordeide, Preethi Ramaiya
  • Publication number: 20180022786
    Abstract: The present invention relates to C-terminal modified Protoxin II peptides that selectively inhibit the Nav1.7 sodium channel; the present invention also relates to pharmaceutical compositions useful for prophylactic or therapeutic treatment of a disorder responsive to the blockade of sodium ion channels, especially Nav1.7 sodium ion channels; the present invention further provides methods of treating a disorder responsive to the blockade of sodium channels, and particularly Nav1.7 sodium channels, in a mammal sulfuring from excess activity of said channels.
    Type: Application
    Filed: July 14, 2017
    Publication date: January 25, 2018
    Inventors: Donald James Kyle, Jae Hyun Park
  • Publication number: 20180022787
    Abstract: This disclosure relates to vectors, isolated cells, compositions, and methods for the treatment of critical limb ischemia and associated disorders. One aspect of the disclosure relates to a vector comprising a nucleic acid encoding a 165A isoform VEGF protein and a promoter that regulates expression of the nucleic acid encoding the VEGF.
    Type: Application
    Filed: May 29, 2017
    Publication date: January 25, 2018
    Inventors: Jan Nolta, Karen Pepper, Fernando Fierro, Gerhard Bauer
  • Publication number: 20180022788
    Abstract: The present invention provides methods for inhibiting interleukin-3 receptor-expressing cells, and, in particular, inhibiting the growth of such cells by using a diphtheria toxin-human interleukin-3 conjugate (DT-IL3) that is toxic to cells expressing the interleukin-3 receptor. In preferred embodiments, the DT-IL3 conjugate is a fusion protein comprising amino acids 1-388 of diphtheria toxin fused via a peptide linker to full-length, human interleukin-3. In certain embodiments, the methods of the present invention relate to the administration of a DT-IL3 conjugate to inhibit the growth of cancer cells and/or cancer stem cells in humans, which cells express one or more subunits of the interleukin-3 receptor. Exemplary cells include myeloid leukemia cancer stem cells.
    Type: Application
    Filed: March 10, 2017
    Publication date: January 25, 2018
    Applicant: SCOTT & WHITE MEMORIAL HOSPITAL
    Inventor: Arthur E. Frankel
  • Publication number: 20180022789
    Abstract: Gelatin particles include: gelatin that serves as a main component; and an auxiliary component carried on the gelatin, the gelatin particles being configured such that where the particle size of the gelatin particles is X, the ratio A/B of the average concentration A (mass %) of the auxiliary component contained in a surface part having a thickness of 0.01X from the surface of the gelatin particles based on the total mass of the gelatin particles to the average concentration B (mass %) of the auxiliary component contained in an inner part of the particles deeper than the surface part based on the total mass of the gelatin particles is less than 0.25.
    Type: Application
    Filed: July 14, 2017
    Publication date: January 25, 2018
    Inventors: Natsumi HIRAYAMA, Chie INUI, Akihiro MAEZAWA, Yasuhiko TABATA
  • Publication number: 20180022790
    Abstract: The disclosure provides a composition comprising immunoglobulin from an equine that has been hyper-immunized with a filovirus immunogen. The disclosure further provides methods of making such compositions and methods of using such compositions, e.g., for treating Ebola virus infection.
    Type: Application
    Filed: January 28, 2016
    Publication date: January 25, 2018
    Inventors: Frederick Wayne HOLTSBERG, Mohammad Javad AMAN, Paul H. WALZ, Stephanie R. OSTROWSKI
  • Publication number: 20180022791
    Abstract: This disclosure relates to agrochemical and biological control compositions for combating pests, more specifically plant pests, comprising at least one polypeptide, which specifically binds to a pest. The disclosure further provides methods for protecting or treating a plant or a part of a plant from an infection or other biological interaction with a plant pathogen, at least comprising the step of applying directly or indirectly to a plant or to a part of a plant, an agrochemical composition, under conditions effective to protect or treat a plant or a part of a plant against a infection or biological interaction with a plant pathogen. Further provided are methods for producing such agrochemical compositions and formulations, to polypeptides with a specific pesticidal activity comprised within an agrochemical formulation, to nucleic acids encoding such polypeptide and to plants comprising chimeric genes comprising such nucleic acids.
    Type: Application
    Filed: October 4, 2017
    Publication date: January 25, 2018
    Applicant: AGROSAVFE N.V.
    Inventors: Peter Verheesen, Chris De Jonghe, Inge Elodie Van Daele, Miguel Francesco Coleta De Bolle, João Filipe Veloso Vieira, Karin Thevissen, Bruno Cammue
  • Publication number: 20180022792
    Abstract: There is provided agents for modulation of a chronic inflammatory response wherein the agent modulates the biological activity of tenascin-C. There is also provided methods of identifying agents modulating tenascin-C and chronic inflammation. There are also provided uses of such agents.
    Type: Application
    Filed: July 22, 2015
    Publication date: January 25, 2018
    Inventors: Kim Suzanne Midwood, Brian Maurice John Foxwell
  • Publication number: 20180022793
    Abstract: The present invention provides compositions and methods of controlling the direction and/or movement of migratory cells. Specifically, the invention is directed to the identification of novel chemorepellents and unimodal fugetaxins, their agonists and antagonists which alter or affect the movement of cells involved in immune, inflammatory or cancerous phenotypes.
    Type: Application
    Filed: April 6, 2017
    Publication date: January 25, 2018
    Inventors: Hyun Kang, Scott Sacane, Jonathan L. Moon, Erica B. Goodhew, Lopa Bhatt, Stacey L. Rose, Milton H. Werner
  • Publication number: 20180022794
    Abstract: The present invention relates to active form specific anti-Rho GTPase conformational single domain antibodies and their uses in particular in the therapeutic and diagnostic fields. In particular, the present invention relates to a single domain antibody wherein the amino acid sequences of CDR1-IMGT, CDR2-IMGT and CDR3-IMGT have at least 90% of identity with the amino acid sequences of the CDR1-IMGT, CDR2-IMGT and CDR3-IMGT of the H12, B6, 4P75, 4SP1, 4SNP36, 4SNP61, 5SP10, 5SP11, 5SP58, 5SNP47, 5SNP48, 5SNP65, B20, B15, B5, B71, E3, A6, G12, NB61, 212B, 111B or 404F (hs2dAb) single domain antibody which are defined in Table B.
    Type: Application
    Filed: February 2, 2016
    Publication date: January 25, 2018
    Inventors: Aurelien OLICHON, Laura KELLER, Gilles FAVRE, Nicolas BERY, Patrick CHINESTRA
  • Publication number: 20180022795
    Abstract: The present invention provides compositions and methods for regulating the specificity and activity of T cells. In one embodiment, the invention provides a type of chimeric antigen receptor (CAR) wherein the CAR is termed a “KIR-CAR” which is a CAR design comprising a component of a receptor naturally found on natural killer (NK) cells. In one embodiment, the NK receptor includes but is not limited to a naturally occurring activating and inhibitory receptor of NK cells known as a killer cell immunoglobulin-like receptor (KIR).
    Type: Application
    Filed: July 24, 2017
    Publication date: January 25, 2018
    Inventors: Michael Milone, Enxiu Wang
  • Publication number: 20180022796
    Abstract: The present invention concerns chimeric or humanized antibodies or antigen-binding fragments thereof that comprise specific CDR sequences, disclosed herein. Preferably, the antibodies or fragments comprise specific heavy and light chain variable region sequences disclosed herein. More preferably, the antibodies or fragments also comprise specific constant region sequences, such as those associated with the nG1m1,2 or Km3 allotypes. The antibodies or fragments may bind to a human histone protein, such as H2B, H3 or H4. The antibodies or fragments are of use to treat a variety of diseases that may be associated with histones, such as autoimmune disease (e.g.
    Type: Application
    Filed: September 22, 2017
    Publication date: January 25, 2018
    Inventors: Chien-Hsing Chang, Hans J. Hansen, David M. Goldenberg
  • Publication number: 20180022797
    Abstract: The present invention provides compositions comprising anti-transthyretin antibodies. The compositions are particularly useful for diagnosis, prognosis and/or treatment of amyloid diseases or symptoms thereof.
    Type: Application
    Filed: September 26, 2017
    Publication date: January 25, 2018
    Inventors: Xin JIANG, Jeffery W. KELLY, Justin CHAPMAN
  • Publication number: 20180022798
    Abstract: Provided herein are proteins, antibodies, assays and methods useful for modulating growth factor levels and/or activities. In some embodiments, such growth factors are members of the TGF-? superfamily of proteins.
    Type: Application
    Filed: August 8, 2017
    Publication date: January 25, 2018
    Inventors: Thomas Schurpf, Nagesh K. Mahanthappa, Michelle Straub
  • Publication number: 20180022799
    Abstract: The present invention relates generally to the methods for the treatment and diagnosis of conditions mediated by IL-5 and excess eosinophil production, and more specifically to mAbs, Fabs, chimeric and humanized antibodies. More particularly, methods are provided for reducing eosinophils in a human in need thereof, which method comprises administering to said human a composition comprising at least one anti-IL-5 antibody, wherein at least one anti-IL-5 antibody provides a mean maximum plasma concentration of said anti-IL-5 antibody of at least about 1.03±0.21 ?g/mL, an Area Under the Curve(0-inf) value of at least about 15.5±2.7 ?g*day/mL and a serum half-life of about 16.2±2.1 days to about 21.7±2.8 days.
    Type: Application
    Filed: October 10, 2017
    Publication date: January 25, 2018
    Inventors: Bela Rajiv PATEL, Deborah SMITH, Deborah J. TOMPSON, Parnian ZIA-AMIRHOSSEINI
  • Publication number: 20180022800
    Abstract: The invention relates to methods of treating chronic intestinal inflammation and/or inflammatory bowel disease by administering an antagonist of oncostatin-M (OSM) and/or OSM receptor-? (OSMR). The invention also relates to methods for diagnosing or prognosing chronic intestinal inflammation and/or inflammatory bowel disease in an individual and for predicting whether or not an individual will respond to an anti-TNF? therapy. The methods comprise measuring OSM and/or OSMR in the individual.
    Type: Application
    Filed: January 28, 2016
    Publication date: January 25, 2018
    Inventors: Nathaniel Richard West, Benjamin Michael Joseph Owens, Ahmed Nabil Hegazy, Fiona Margaret Powrie
  • Publication number: 20180022801
    Abstract: The present invention is directed to antibodies and fragments thereof and humanized versions thereof having binding specificity for IL-6. Another embodiment of this invention relates to the antibodies described herein, and binding fragments thereof, comprising the sequences of the VH, VL and CDR polypeptides described herein, and the polynucleotides encoding them. The invention also contemplates conjugates of anti-IL-6 antibodies and binding fragments thereof conjugated to one or more functional or detectable moieties. The invention also contemplates methods of making said anti-IL-6 antibodies and binding fragments thereof. Embodiments of the invention also pertain to the use of anti-IL-6 antibodies, and binding fragments thereof, for the diagnosis, assessment and treatment of diseases and disorders associated with IL-6.
    Type: Application
    Filed: August 4, 2017
    Publication date: January 25, 2018
    Inventors: Leon F. GARCIA-MARTINEZ, Anne Elisabeth CARVALHO JENSEN, Katie ANDERSON, Benjamin H. DUTZAR, Ethan W. OJALA, Brian R. KOVACEVICH, John A. LATHAM, Jeffrey T.L. SMITH
  • Publication number: 20180022802
    Abstract: The present disclosure is directed to progastrin monoclonal antibodies, fragments thereof, compositions comprising progastrin monoclonal antibodies, and methods of making and using progastrin monoclonal antibodies and compositions thereof. The present disclosure is directed to methods of treating colorectal cancer with progastrin monoclonal antibodies and compositions comprising progastrin monoclonal antibodies or fragments thereof. The present disclosure is further directed to methods comprising detection of progastrin, including methods of diagnosing colorectal cancer and methods of monitoring efficacy of anti-cancer therapy in subjects suffering from colorectal cancer.
    Type: Application
    Filed: March 6, 2017
    Publication date: January 25, 2018
    Inventors: Julie PANNEQUIN, Laure Boudier, Dominique Joubert, Frédéric Hollande
  • Publication number: 20180022803
    Abstract: Provided are antibodies, and antigen-binding fragments thereof, which specifically bind to an extracellular poor loop of an alpha 1a subunit of L-type voltage gated calcium channel, and related compositions, kits, and methods of use thereof, for instance, administration to a subject in need thereof to modify an immune response, for example, in the treatment of cancer.
    Type: Application
    Filed: February 16, 2016
    Publication date: January 25, 2018
    Inventors: Wilfred Arthur Jefferies, Kyung Bok Choi, Shawna Rose Stanwood, Franz Fenninger, Brett Alexander Eyford, Lonna Munro, Cheryl Gurine Pfeifer, Reinhard Gabathuler
  • Publication number: 20180022804
    Abstract: The disclosure provides compositions and methods for the treatment of ocular conditions associated with angiogenesis comprising administering an antibody that targets a tyrosine phosphatase inhibitor in a subject.
    Type: Application
    Filed: July 19, 2017
    Publication date: January 25, 2018
    Inventors: Kevin Peters, Michael Allen Flynn