Patents Issued in March 31, 2015
  • Patent number: 8993728
    Abstract: The present invention provides novel antibodies that recognize the extracellular domain of a human CLCP1 antigen; nucleic acids encoding the antibodies; vectors carrying the nucleic acids in an expressible manner; transformed cells containing the vectors; methods for producing the antibodies; diagnostic methods for cancer or prognosis of cancer, immunohistological or immunocytological assay methods, and kits for determining the expression level of CLCP1 in cells or tissues, all of which use the antibodies; pharmaceutical compositions comprising the antibodies; agents for treating or preventing CLCP1-expressing cancer; agents for inhibiting growth, migration, invasion, or metastasis of CLCP1-expressing cancer cells; immunostaining agents for staining CLCP1-expressing cancer cells; and agents for treating or preventing CLCP1-expressing tumor.
    Type: Grant
    Filed: July 16, 2009
    Date of Patent: March 31, 2015
    Assignees: Medical and Biological Laboratories Co., Ltd., Oncomics Co., Ltd.
    Inventors: Ken-ichiro Ono, Takashi Takahashi
  • Patent number: 8993729
    Abstract: Transgenes encoding exogenous antibodies are stably integrated into donor cells and are present in the somatic tissue of chimeric birds. The transgenes encode exogenous antibodies and are preferably expressed in the oviduct for collection in the egg. Tissue specificity is provided by selecting the content of the transgene accordingly. Birds whose genome is comprised of trangene-derived exogenous antibody-encoding DNA express exogenous antibodies having desirable chemical properties with increased therapeutic utility compared to antibodies derived from bacterial expression systems.
    Type: Grant
    Filed: July 16, 2012
    Date of Patent: March 31, 2015
    Assignee: Synageva Biopharma Corp.
    Inventors: Lei Zhu, Wen Zhou, Robert J. Etches
  • Patent number: 8993730
    Abstract: This invention relates to chimeric and humanized antibodies that specifically bind the BCR complex, and particularly chimeric and humanized antibodies to the BCR complex. The invention also relates to methods of using the antibodies and compositions comprising them in the diagnosis, prognosis and therapy of diseases such as cancer, autoimmune diseases, inflammatory disorders, and infectious disease.
    Type: Grant
    Filed: September 23, 2013
    Date of Patent: March 31, 2015
    Assignee: MacroGenics, Inc.
    Inventors: Leslie S. Johnson, Ling Huang
  • Patent number: 8993731
    Abstract: A humanized agonistic antibody which binds human PD-1 comprising a heavy chain wherein the variable domain of the heavy chain comprises the sequence given in SEQ ID NO:1 for CDR-H1, the sequence given in SEQ ID NO: 2 for CDR-H2 and the sequence given in SEQ ID NO: 3 for CDR-H3 and the heavy chain framework region is derived from human sub-group sequence VH4 3-1 4-30.4+JH4 (SEQ ID NO: 33). The disclosure also extends to therapeutic uses of the antibody molecules, compositions and methods for producing said antibody molecules.
    Type: Grant
    Filed: March 9, 2011
    Date of Patent: March 31, 2015
    Assignee: UCB Biopharma SPRL
    Inventor: Kerry Louise Tyson
  • Patent number: 8993732
    Abstract: The present invention, pertains in general to the field of stabilization of FSH formulations, in particular liquid FSH formulations. The stabilization is achieved by the addition of salts comprising pharmaceutically acceptable alkali metal cations, in preferred embodiments by the addition of pharmaceutically acceptable salts, i.e. sodium salts or potassium salts.
    Type: Grant
    Filed: July 28, 2011
    Date of Patent: March 31, 2015
    Assignee: Ferring B.V.
    Inventors: Helen Ulrika Sjögren, Heidi Louise Bagger
  • Patent number: 8993733
    Abstract: Procedure for obtaining a composition that contains growth factors, which comprises the steps of heat-treating a platelet-rich plasma or the supernatant of a platelet-rich plasma that contains released growth factors in order to increase its temperature, for eliminating the complement and reducing the immunoglobulins present therein, and lyophilizing the plasma or supernatant in order to obtain a final dry composition that can easily be transported, handled and stored, thereby facilitating periodic or chronic treatments with blood compounds. It has been shown that when the final dry composition is resuspended, a once again humid composition is obtained that maintains its biological properties intact.
    Type: Grant
    Filed: July 27, 2012
    Date of Patent: March 31, 2015
    Inventor: Eduardo Anitua Aldecoa
  • Patent number: 8993734
    Abstract: The present invention provides improved methods for the manufacturing of IVIG products. These methods offer various advantages such as reduced loss of IgG during purification and improved quality of final products. In other aspects, the present invention provides aqueous and pharmaceutical compositions suitable for intravenous, subcutaneous, and/or intramuscular administration. In yet other embodiments, the present invention provides methods of treating a disease or condition comprising administration of an IgG composition provided herein.
    Type: Grant
    Filed: May 27, 2010
    Date of Patent: March 31, 2015
    Assignees: Baxter International Inc., Baxter Healthcare SA
    Inventors: Leopold Bruckschwaiger, Sonja Svatos, Julia Nürnberger, Wolfgang Teschner, Harald Arno Butterweck, Hans-Peter Schwarz, Thomas Gundinger, Bernhard Koelbl, Reinhard Grausenburger, Azra Pljevljakovic
  • Patent number: 8993735
    Abstract: The invention relates to a method for producing a lignin-based substrate for soil improvement having a water-storing property, characterized by the following steps: providing lignin, oxidizing the lignin in either an aqueous alkaline suspension or a pH-neutral aqueous suspension, the pH-neutral aqueous suspension being converted into an alkaline substance after the lignin has been oxidized, cross-linking the lignin in an aqueous alkaline medium using multifunctional compounds, and neutralizing, drying, and comminuting the lignin.
    Type: Grant
    Filed: February 10, 2011
    Date of Patent: March 31, 2015
    Assignee: Technische Universität Dresden
    Inventors: Lars Passauer, Falk Liebner, Klaus Fischer, Joachim Katzur
  • Patent number: 8993736
    Abstract: The present disclosure provides a photoreactive synthetic regulator of protein function. The present disclosure further provides a light-regulated polypeptide that includes a subject synthetic regulator. Also provided are cells and membranes comprising a subject light-regulated polypeptide. The present disclosure further provides methods of modulating protein function, involving use of light.
    Type: Grant
    Filed: October 29, 2009
    Date of Patent: March 31, 2015
    Assignee: The Regents of the University of California
    Inventors: Dirk Trauner, Ehud Y. Isacoff, Richard H. Kramer, Matthew R. Banghart, Doris L. Fortin, Alexandre Mourot
  • Patent number: 8993737
    Abstract: In various embodiments, the present invention provides fluorescent dyes that are linked to another species through an amino acid or peptide linker. In an exemplary embodiment, the dye is linked to a polyphosphate nucleic acid through an amino acid or peptide linker. These conjugates find use in single molecule DNA sequencing and other applications. In various embodiments, the dye moiety is a cyanine dye. Cyanine dyes that are highly charged, such as those including multiple sulfonate, alkylsulfonate, carboxylate and/or alkylcarboxylate moieties are examples of cyanine dyes of use in the compounds of the invention.
    Type: Grant
    Filed: August 25, 2011
    Date of Patent: March 31, 2015
    Assignee: Pacific Biosciences, Inc.
    Inventor: Gene Shen
  • Patent number: 8993738
    Abstract: The present invention provides modified nucleosides, analogs thereof and oligomeric compounds prepared therefrom. More particularly, the present invention provides modified nucleosides and analogs thereof that are useful for incorporation at the terminus of an oligomeric compound. Such oligomeric compounds can also be included in a double stranded composition. In some embodiments, the oligomeric compounds provided herein are expected to hybridize to a portion of a target RNA resulting in loss of normal function of the target RNA.
    Type: Grant
    Filed: April 26, 2011
    Date of Patent: March 31, 2015
    Assignee: Isis Pharmaceuticals, Inc.
    Inventors: Thazha P. Prakash, Punit P. Seth, Eric E. Swayze
  • Patent number: 8993739
    Abstract: A process for the preparation of compound of Formula (I) is provided.
    Type: Grant
    Filed: March 12, 2012
    Date of Patent: March 31, 2015
    Assignee: Wockhardt Ltd.
    Inventors: Kiran Kumar Gangakhedkar, Furqan Mohammed Diwan, Aniruddha Varangaonkar, Keshav Deo
  • Patent number: 8993740
    Abstract: The present invention relates to a method for preparation of the tetrasaccharide lacto-N-neotetraose (LNnt, formula (I)) especially in large scale, as well as intermediates in the synthesis, a new crystal form (polymorph) of LNnt, and the use thereof in pharmaceutical or nutritional compositions.
    Type: Grant
    Filed: February 21, 2011
    Date of Patent: March 31, 2015
    Assignee: Glycom A/S
    Inventors: István Bajza, Gyula Dekany, Károly Ágoston, Ignacio Figuero-Pérez, Julien Boutet, Markus Hederos, Ferenc Horváth, Piroska Kovács-Pénzes, Lars Kröger, Christoph Röhrig, Andreas Schroven, Ioannis Vrasidas, Péter Trinka, László Kalmár, Irme Kovács, Sándor Demkó, Ágnes Ágoston, Christian Risinger
  • Patent number: 8993741
    Abstract: The present invention includes an isolated nucleic acid comprising a nucleic acid sequence encoding a SMN?7 degron and the encoded polypeptide. The invention also includes inhibitors of SMN?7 degron. The invention also includes compositions and methods for mitigating SMN deficiency by targeting inhibition of factors that mediate SMN?7-degron dependent degradation of SMN?7.
    Type: Grant
    Filed: November 17, 2010
    Date of Patent: March 31, 2015
    Assignee: The Trustees of the University of Pennsylvania
    Inventors: Gideon Dreyfuss, Sungchan Cho
  • Patent number: 8993742
    Abstract: The invention relates to polarized cell tubulo-vesicular structure localization signals. The localization signals are utilized as research tools or are linked to polypeptides of interest or therapeutic molecules. Disclosed are methods of making and using polypeptides and modified polypeptides as signals to localize therapeutics, experimental compounds, peptides, proteins and/or other macromolecules to the tubulo-vesicular structures of polarized cells. The polypeptides of the invention optionally include linkage to reporters, epitopes and/or other experimental or therapeutic molecules. The invention also encompasses polynucleotides encoding the localization signals and vectors comprising these polynucleotides.
    Type: Grant
    Filed: December 20, 2010
    Date of Patent: March 31, 2015
    Assignee: Intrexon Corporation
    Inventor: Thomas David Reed
  • Patent number: 8993743
    Abstract: The present invention relates to a nucleic acid molecule encoding a chimeric protein having the biochemical activity of a surface active protein, wherein said chimeric protein comprises: (a) an N-terminal portion of a first surface active protein, wherein the N-terminal portion is devoid of between 0 and 10 of the most N-terminal amino acids of the mature first surface active protein; and, C-terminally thereof, (b) a C-terminal portion of a second surface active protein, wherein the C-terminal portion is devoid of between 0 and 10 of the most C-terminal amino acids of the mature second surface active protein. The present invention further relates to a vector, a non-human host and a method for the production of a chimeric protein having the biochemical activity of a surface active protein. In addition, the present invention relates to a chimeric protein encoded by the nucleic acid molecule of the invention and a composition comprising the chimeric protein.
    Type: Grant
    Filed: February 18, 2011
    Date of Patent: March 31, 2015
    Assignee: B.R.A.I.N. Biotechnology Research and Information Network AG
    Inventors: Guido Meurer, Esther Gabor, Anke Bachert, Jürgen Eck
  • Patent number: 8993744
    Abstract: Disclosed herein are computationally optimized broadly reactive dengue virus E polypeptide sequences for DENV-1, DENV-2, DENV-3 and DENV-4. Also disclosed are dengue virus E protein fragments (such as the E protein ectodomain and DIII domain) fused to the molecular adjuvant P28. The disclosed nucleic acid and polypeptide sequences can be used as vaccines for immunization against dengue virus infection. In some cases, the vaccine includes a virus-like particle containing the universal dengue virus E protein, or fragment thereof, or the vaccine is a DNA molecule encoding the VLP.
    Type: Grant
    Filed: May 23, 2011
    Date of Patent: March 31, 2015
    Assignee: University of Pittsburgh—Of the Commonwealth System of Higher Education
    Inventors: Ted M. Ross, Nikolaos Vasilakis
  • Patent number: 8993745
    Abstract: Double-stranded RNA (dsRNA) induces sequence-specific post-transcriptional gene silencing in many organisms by a process known as RNA interference (RNAi). Using a Drosophila in vitro system, we demonstrate that 19-23 nt short RNA fragments are the sequence-specific mediators of RNAi. The short interfering RNAs (siRNAs) are generated by an RNase III-like processing reaction from long dsRNA. Chemically synthesized siRNA duplexes with overhanging 3? ends mediate efficient target RNA cleavage in the lysate, and the cleavage site is located near the center of the region spanned by the guiding siRNA. Furthermore, we provide evidence that the direction of dsRNA processing determines whether sense or antisense target RNA can be cleaved by the produced siRNP complex.
    Type: Grant
    Filed: September 10, 2010
    Date of Patent: March 31, 2015
    Assignees: Max-Planck-Gesellschaft zur Förderung der Wissenschaften E.V., Massachusetts Institute of Technology, Whitehead Institute for Biomedical Research, University of Massachusetts
    Inventors: Thomas Tuschl, Sayda Mahgoub Elbashir, Winfried Lendeckel
  • Patent number: 8993746
    Abstract: This invention relates to modified double-stranded oligoribonucleic acid (dsRNA) having improved stability in cells and biological fluids, and methods of making and identifying dsRNA having improved stability, and of using the dsRNA to inhibit the expression or function of a target gene.
    Type: Grant
    Filed: March 27, 2012
    Date of Patent: March 31, 2015
    Assignee: Alnylam Pharmaceuticals, Inc.
    Inventors: Hans-Peter Vornlocher, Ingo Roehl, Philipp Hadwiger, Tracy Stage Zimmermann, Muthiah Manoharan, Kallanthottathil G. Rajeev, Akin Akinc
  • Patent number: 8993747
    Abstract: The present invention relates to a process for the production of alkali cellulose for the production of alkali cellulose and, optionally, cellulose ethers from cellulose in the presence of alkali and, if applicable, with alkylating and/or hydroxyalkylating agent(s) comprising the reaction of a cellulose with an alkali metal hydroxide, wherein the alkali metal hydroxide is mixed with cellulose in a mixing apparatus, the mixing apparatus (1) having an upper region (20, 102a, 202a) with a first cross-section and a lower region (21, 102b, 202b) with a second cross-section, the second cross-section being the same as or smaller than the first cross-section and comprising at least one non-horizontally oriented mixing device (23, 27, 121, 221, 224).
    Type: Grant
    Filed: January 8, 2010
    Date of Patent: March 31, 2015
    Assignee: Dow Global Technologies LLC
    Inventors: Matthias Sprehe, Bettina Hoelzer
  • Patent number: 8993748
    Abstract: Process for the preparation of trivalent iron complexes with mono-, di- and polysaccharide sugars, consisting of the activation of the sugar by oxidation with nascent bromine generated in situ by reaction between an alkaline or alkaline earth bromine and an alkaline hypochlorite, the complexation of the activated sugar in solution with a ferric salt dissolved in an aqueous solution, the purification of the resulting solution through ultrafiltration and finally the stabilization of the trivalent iron-sugar complex by heating at a temperature between 60° C. and 100° C. for a period between 1 and 4 hours at a pH between 9.0 and 11.0.
    Type: Grant
    Filed: March 24, 2014
    Date of Patent: March 31, 2015
    Assignee: BIOFER S.p.A.
    Inventors: Stefania Sacchi, Mauro Montorsi, Egidio Marchi
  • Patent number: 8993749
    Abstract: A process for producing an eriocitrin-containing material comprises the steps of: preparing an eriocitrin-containing citrus extract from a citrus fruit using an extractant; and separating eriocitrin from the citrus extract. The step of separating eriocitrin from the citrus extract comprises the steps of: bringing the citrus extract into contact with a porous synthetic adsorption resin such that eriocitrin in the citrus extract is adsorbed on the porous synthetic adsorption resin, the porous synthetic adsorption resin comprising a phenol-formaldehyde resin as a main framework and having amino and phenolic hydroxyl groups; and eluting the eriocitrin adsorbed on the porous synthetic adsorption resin using an elution solvent.
    Type: Grant
    Filed: December 26, 2008
    Date of Patent: March 31, 2015
    Assignee: Pokka Corporation
    Inventors: Masanori Hiramitsu, Toshikazu Omori, Kenji Yamaguchi, Hiroaki Bessho
  • Patent number: 8993750
    Abstract: The present invention relates to novel compounds of Formula (I): which act as 5HT2C receptor modulators. These compounds are useful in pharmaceutical compositions whose use includes the treatment of obesity.
    Type: Grant
    Filed: July 9, 2014
    Date of Patent: March 31, 2015
    Assignee: Arena Pharmaceuticals, Inc.
    Inventors: Brian Smith, Jeffrey Smith
  • Patent number: 8993751
    Abstract: The present invention relates to a process for preparing tetrazole-substituted anthranilic acid diamide derivatives of the formula (I) in which R1, R2, R3, R4, Q and Z have the meanings given in the description, by reacting benzoxazinones with amines.
    Type: Grant
    Filed: August 24, 2012
    Date of Patent: March 31, 2015
    Assignee: Bayer Intellectual Property GmbH
    Inventors: Sergii Pazenok, Werner Lindner, Hartmut Scheffel
  • Patent number: 8993752
    Abstract: In one aspect, the invention relates to compounds having the formula: where R1, R2, R3, R4, and R5 are as defined in the specification, or a pharmaceutically acceptable salt thereof. These compounds have neprilysin inhibition activity. In another aspect, the invention relates to pharmaceutical compositions comprising such compounds; methods of using such compounds; and process and intermediates for preparing such compounds.
    Type: Grant
    Filed: July 8, 2013
    Date of Patent: March 31, 2015
    Assignee: Theravance Biopharma R&D IP, LLC
    Inventors: Roland Gendron, Adam D. Hughes
  • Patent number: 8993753
    Abstract: The present invention relates to a process for the stereoselective preparation of compounds of formulae (1A) and (1B) and the salts thereof, particularly the physiologically acceptable salts thereof with inorganic or organic acids and bases, which have valuable pharmacological properties, particularly an inhibitory effect on signal transduction mediated by tyrosine kinases, the use thereof for the treatment of diseases, particularly tumoral diseases as well as benign prostatic hyperplasia (BPH), diseases of the lungs and airways.
    Type: Grant
    Filed: January 14, 2014
    Date of Patent: March 31, 2015
    Assignee: Boehringer Ingelheim International GmbH
    Inventors: Markus Ostermeier, Juergen Daeubler, Guenther Huchler, Stephan Kling, Marco Santagostino
  • Patent number: 8993754
    Abstract: Provided is an iridium complex having a substructure represented by the following formula (1), which is a luminescent element material capable of luminescence with high brightness/high efficiency and excellent in durability and can be used in a luminescent element, etc.
    Type: Grant
    Filed: August 23, 2010
    Date of Patent: March 31, 2015
    Assignee: National Institute of Advanced Industrial Science and Technology
    Inventor: Hideo Konno
  • Patent number: 8993755
    Abstract: The present application includes a compound of Formula I or II: or a pharmaceutically acceptable salt, solvate, and/or ester thereof, compositions containing such compounds, therapeutic methods that include the administration of such compounds, and therapeutic methods that include the administration of such compounds with at least one additional active agent.
    Type: Grant
    Filed: January 17, 2014
    Date of Patent: March 31, 2015
    Assignee: Gilead Sciences, Inc.
    Inventors: Michael Graupe, Randall L. Halcomb
  • Patent number: 8993756
    Abstract: The instant invention provides compounds of formula I which are JAK3 inhibitors. Specifically, the compounds of formula I are pyrrolo[2,3-d]pyrimidine derivative compounds. The instant invention also provides methods of treating JAK-mediated diseases such as rheumatoid arthritis, asthma, COPD and cancer, by administering the pyrrolo[2,3-d]pyrimidine-derivative compounds of formula I.
    Type: Grant
    Filed: November 30, 2012
    Date of Patent: March 31, 2015
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Sean P. Ahearn, Matthew Christopher, Christopher Dinsmore, Joon Jung, Qinglin Pu, Alexey Rivkin, Mark E. Scott, David J. Witter, Hyun Chong Woo, Brandon Cash
  • Patent number: 8993757
    Abstract: The invention relates to a N-piperidin-4-yl derivative having the general Formula I or a pharmaceutically acceptable salt thereof, to pharmaceutical compositions comprising the same and to the use of said N-piperidin-4-yl derivatives for the treatment and prevention of endometriosis, for the treatment and prevention of pre-menopausal and peri-menopausal hormone-dependent breast cancer, for contraception, or for the treatment of uterine fibroids or other menstrual-related disorders.
    Type: Grant
    Filed: September 14, 2012
    Date of Patent: March 31, 2015
    Assignee: Merck Sharp & Dohme B.V.
    Inventors: Ines Huisman, Marcelis Van Der Stelt, Wouter Wiedenhof, Charles Anthony Graham Baker-Glenn, Wesley Peter Blackaby, Naimisha Trivedi
  • Patent number: 8993758
    Abstract: Disclosed herein are compounds of formula (I) and methods of inhibiting IKK? and the NF-?B signaling and mTOR pathways.
    Type: Grant
    Filed: November 22, 2011
    Date of Patent: March 31, 2015
    Assignees: Board of Regents of the University of Nebraska, The Board of Regents, University of Texas System
    Inventors: Amarnath Natarajan, Qianyi Chen, Vashti C. Bryant, Rajkumar Rajule
  • Patent number: 8993759
    Abstract: A transamination process is described to prepare polyamine product mixtures from reactants comprising mixed nitrogen-containing compounds with binary carbon spacing between nitrogen-containing groups (a binary component). A second nitrogen-containing component with a second carbon atom spacing between nitrogen-containing groups may also be employed. The molar ratio between the binary and second components can be adjusted to customize the product composition for desired end uses.
    Type: Grant
    Filed: October 20, 2011
    Date of Patent: March 31, 2015
    Assignee: DOW Global Technologies LLC
    Inventor: Stephen W. King
  • Patent number: 8993760
    Abstract: The subject invention concerns compositions and methods for blocking cancer cell growth or proliferation and/or inducing cancer cell death. Compositions of the present invention are compounds that inhibit Rho-protein associated kinase function. Compounds of the invention include piperazinyl pyridines, piperazinylmethyl pyridines, piperazinyl ureas and carbamates, piperazinyl pyridines and quinoilines (including isoquinliones) as well as piperazinyl (including piperazinylmethyl) pyridines and quinolines (including isoquinolines). Compounds of the invention disrupt Rho-kinase activation and function and significantly inhibit tumor cell growth and induce tumor cell death.
    Type: Grant
    Filed: June 22, 2009
    Date of Patent: March 31, 2015
    Assignees: University of South Florida, Yale University
    Inventors: Said M. Sebti, Andrew D. Hamilton
  • Patent number: 8993761
    Abstract: The present invention provides low hygroscopic forms of aripiprazole and processes for the preparation thereof which will not convert to a hydrate or lose their original solubility even when a medicinal preparation containing the anhydrous aripiprazole crystals is stored for an extended period.
    Type: Grant
    Filed: January 25, 2013
    Date of Patent: March 31, 2015
    Assignee: Otsuka Pharamceutical Co. Ltd.
    Inventors: Takuji Bando, Satoshi Aoki, Junichi Kawasaki, Makoto Ishigami, Youichi Taniguchi, Tsuyoshi Yabuuchi, Kiyoshi Fujimoto, Yoshihiro Nishioka, Noriyuki Kobayashi, Tsutomu Fujimura, Masanori Takahashi, Kaoru Abe, Tomonori Nakagawa, Koichi Shinhama, Naoto Utsumi, Michiaki Tominaga, Yoshihiro Ooi, Shohei Yamada, Kenji Tomikawa
  • Patent number: 8993762
    Abstract: Improved synthetic methods for the production of thaxtomin analogs, particularly thaxtomin A, and intermediates therefore such as substituted tryptophans and in particular, 4-nitro-L-tryptophan, and substituted phenyl acrylic acids are disclosed. Bioassays show that the synthetic thaxtomin A is not significantly different from the natural one in herbicidal activity.
    Type: Grant
    Filed: March 15, 2013
    Date of Patent: March 31, 2015
    Assignee: Marrone Bio Innovations, Inc.
    Inventors: Huazhang Huang, Dong Yan, Zhijie Xue, Hongbo Zhang
  • Patent number: 8993763
    Abstract: The present invention provides an sulfonamide derivative having DP receptor antagonistic activity and a pharmaceutical composition comprising the said compound as an active ingredient, and further a therapeutic agent for treating allergic diseases. A compound of the general formula (II): wherein the ring A is an aromatic carbocyclic ring etc.; the ring B is a nitrogen-containing non-aromatic heterocyclic ring etc.; the ring C is an aromatic carbocyclic ring etc.; R1 is carboxy etc.; R2 is independently a halogen atom etc.; R3 is optionally substituted alkyloxy etc.; R4 is independently a halogen atom etc.; R5 is independently optionally substituted alkyl etc.; M is sulfonyl etc.; Y is a single bond etc.; L1 is a single bond etc.; L2 is a single bond etc.; k is 0, 1, 2, 3 or 4; n is 0, 1 or 2; and q is 0, 1, 2 or 3; provided that a) k is not 0 when the ring B is a 6-membered nitrogen-containing heterocyclic ring containing one or two nitrogen atom(s) and the ring C is a benzene ring, etc.
    Type: Grant
    Filed: September 25, 2006
    Date of Patent: March 31, 2015
    Assignee: Shionogi & Co., Ltd.
    Inventors: Akira Kugimiya, Masahiko Fujioka, Yuki Tachibana, Takami Murashi, Naohiro Onodera
  • Patent number: 8993764
    Abstract: There is provided a method for the synthesis of norbuprenorphine, and ultimately buprenorphine, utilizing oripavine as the starting material. Conventional methods of producing buprenorphine utilize thebaine as the starting material, requiring an O-demethylation step, typically a low to moderate yield transformation. The present use of oripavine as a starting material does not require an O-demethylation step, since the oripavine molecule lacks an O-3 methyl group.
    Type: Grant
    Filed: December 18, 2006
    Date of Patent: March 31, 2015
    Assignee: Mallinckrodt LLC
    Inventors: Anthony Mannino, Erik R. Hoefgin, Lloyd P. Hill, Henry J. Buehler
  • Patent number: 8993765
    Abstract: The present invention relates to tetrahydro-azacarboline derivatives of formula (I): having the substituents as described herein which are melanin-concentrating hormone (MCH-1) receptor antagonists. The present invention also relates to pharmaceutical compositions including these compounds, and methods of preparation and use thereof.
    Type: Grant
    Filed: December 20, 2011
    Date of Patent: March 31, 2015
    Assignee: Albany Molecular Research, Inc.
    Inventors: Matthew D. Surman, Peter R. Guzzo, Emily Freeman
  • Patent number: 8993766
    Abstract: The present invention relates to a method for preparing tetrabenazine (TBZ) and dihydrotetrabenazine (DTBZ), and more specifically to a method for preparing tetrabenazine (TBZ) and dihydrotetrabenazine (DTBZ) by using simple and short reaction processes of using 6,7-dimethoxy-1,2,3,4-tetrahydroisoquinoline and 4-methyl-2-(3-(trimethylsilyl)prop-1-ene-2-yl)pentane as starting materials to sequentially perform an alkylation reaction, an Aza-Prins cyclization reaction in the presence of an oxidant and an oxidation reaction.
    Type: Grant
    Filed: September 14, 2012
    Date of Patent: March 31, 2015
    Assignee: Korea Institute of Science and Technology
    Inventors: Sun Joon Min, Yong Seo Cho, Jae Kyun Lee, Ae Nim Pae, Young Wook Son
  • Patent number: 8993767
    Abstract: The present invention relates to multiphoton activable organic compounds responding to the following formula (I). The present invention also relates to a method of synthesizing the compounds of the invention, to an aqueous solution comprising at least one compound of the invention, and to their specific uses. The present invention also concerns a method of liberating organic ligands, said method involving the step of irradiating a compound according to the invention.
    Type: Grant
    Filed: January 12, 2011
    Date of Patent: March 31, 2015
    Assignee: Centre National de la Recherche Scientifique
    Inventors: Peter Dalko, Morgane Petit, David Ogden, Francine Acher
  • Patent number: 8993768
    Abstract: Disclosed are compounds that inhibit RNase H activity of retroviruses, for example, a compound of formula (I) wherein R1, R2, and R3 are as described herein, as well as pharmaceutically acceptable salts, solvates, stereoisomers, and prodrugs thereof. Pharmaceutical compositions comprising such compounds, as well as methods of use, and treatment or prevention of infection by human immunodeficiency virus (HIV).
    Type: Grant
    Filed: May 10, 2012
    Date of Patent: March 31, 2015
    Assignee: The United States of America, as represented by the Secretary, Department of Health and Human Services
    Inventors: John A. Beutler, Stuart F. J. LeGrice, Craig Thomas, Jian-Kang Jiang, Suhman Chung, Jennifer Wilson
  • Patent number: 8993769
    Abstract: The invention disclosed in this document is related to the field of processes to produce certain 2-(pyridine-3-yl)thiazoles as intermediates for the synthesis of pesticidal thiazole amides.
    Type: Grant
    Filed: May 30, 2013
    Date of Patent: March 31, 2015
    Assignee: Dow AgroSciences, LLC.
    Inventors: Ronald Ross, Jr., Carl DeAmicis, Yuanming Zhu
  • Patent number: 8993770
    Abstract: An improved process for preparing dabigatran etexilate, as well as analogous compounds of formula 7, is described.
    Type: Grant
    Filed: February 15, 2013
    Date of Patent: March 31, 2015
    Assignee: Boehringer Ingelheim International GbmH
    Inventors: Frieder Gnad, Stefan Schmitt, Hermann Mueller-Boetticher, Helmut Heitger, Seigfried Meineck, Rolf Dach, Ingo Heddesheimer
  • Patent number: 8993771
    Abstract: Provided herein are compounds useful for the treatment of HBV infection in man.
    Type: Grant
    Filed: March 12, 2014
    Date of Patent: March 31, 2015
    Assignee: Novira Therapeutics, Inc.
    Inventor: George D. Hartman
  • Patent number: 8993772
    Abstract: 4-Amino-5-fluoro-3-halo-6-(substituted)picolinates are conveniently prepared from 4,5,6-trichloropicolinonitrile by a series of steps involving fluorine exchange, amination, halogen exchange, halogenation, nitrile hydrolysis, esterification, and transition metal assisted coupling.
    Type: Grant
    Filed: March 24, 2014
    Date of Patent: March 31, 2015
    Assignee: Dow AgroSciences, LLC.
    Inventors: Yuanming Zhu, Gregory T. Whiteker, James M. Renga, Kim E. Arndt, Gary Roth, David E. Podhorez, Scott P. West, Yang Cheng
  • Patent number: 8993773
    Abstract: A novel process for preparing thiazolidinediones, preferably Pioglitazone, as described. Also described are novel intermediates involved in its synthesis and process for their preparation and use in medicine.
    Type: Grant
    Filed: September 24, 2012
    Date of Patent: March 31, 2015
    Assignee: Cadila Healthcare Limited
    Inventors: Bipin Pandey, Vidya Bhushan Lonray, Braj Bhushan Lohray
  • Patent number: 8993774
    Abstract: A process of production of an aromatic alcohol or a heterocyclic aromatic alcohol, containing a step of reacting an aromatic amine or a heterocyclic aromatic amine having an aromatic ring or a heterocyclic aromatic ring having thereon at least one substituent —CHR1NR2R3 (wherein R1, R2 and R3 each independently represent hydrogen, an alkyl group having from 1 to 4 carbon atoms, or a benzyl group), with an alcohol, in the presence of a basic catalyst.
    Type: Grant
    Filed: December 22, 2011
    Date of Patent: March 31, 2015
    Assignee: Mitsubishi Gas Chemical Company, Inc.
    Inventors: Yutaka Kanbara, Takafumi Abe, Norio Fushimi
  • Patent number: 8993775
    Abstract: The present invention refers to the synthesis of precatalysts and the use of such precatalysts in ethylene oligomerization reactions for the selective production of alpha-olefins. More specifically, it refers to the preparation and use of coordination compounds containing polydentate ligands comprising Group 6 and 10 transition metal compounds, in particular chromium (III) and nickel (II). Such catalytic precursors present high catalytic activity and selectivity for the production of alpha-olefins.
    Type: Grant
    Filed: September 30, 2011
    Date of Patent: March 31, 2015
    Assignees: Petroleo Brasileiro S.A.—Petrobras, Universidade Federal do Rio Grande do Sul-UFRGS
    Inventors: Osvaldo de Lazaro Casagrande Junior, Carlos Rene Klotz Rabello, Lucilene Losch de Oliveira, Ana Helena Dias Pereira dos Santos, Roberta Campedelli, Adao Lauro Bergamo
  • Patent number: 8993776
    Abstract: The present invention relates to novel heterocyclic alkanol derivatives, to processes for preparing these compounds, to compositions comprising these compounds and to their use as biologically active compounds, in particular for controlling harmful microorganisms in crop protection and in the protection of materials and as plant growth regulators.
    Type: Grant
    Filed: March 13, 2013
    Date of Patent: March 31, 2015
    Assignee: Bayer Intellectual Property GmbH
    Inventors: Carl Friedrich Nising, Pierre Cristau, Hendrik Helmke, Gorka Peris, Tomoki Tsuchiya, Pierre Wasnaire, Jürgen Benting
  • Patent number: 8993777
    Abstract: The present invention is a method for producing a phenyl-substituted heterocyclic derivative represented by general formula (1), which has a step wherein a heteroaromatic compound represented by general formula (2) is reacted with a phenol derivative represented by general formula (3) in the presence of a nickel compound, 1,2-bis(dicyclohexylphosphino)ethane, and a base.
    Type: Grant
    Filed: October 10, 2012
    Date of Patent: March 31, 2015
    Assignee: National University Corporation Nagoya University
    Inventors: Kenichiro Itami, Junichiro Yamaguchi, Kei Muto