Three Or More Carboxamide Groups Patents (Class 564/153)
  • Patent number: 10350311
    Abstract: Iohexol particles, contrast agent compositions comprising iohexol particles, methods of preparing iohexol particles, and methods of administering iohexol particles are provided herein. The iohexol particles of the present invention substantially dissolve in water within about 60 seconds when tested using Modified United States Pharmacopeia Method 641.
    Type: Grant
    Filed: March 4, 2015
    Date of Patent: July 16, 2019
    Assignee: Otsuka Pharmaceutical Co., Ltd.
    Inventors: Ji{hacek over (r)}í Prokop, Ivan Hlavá{hacek over (c)}ek, Petr Zahradník, Ji{hacek over (r)}í Malinak
  • Patent number: 10065923
    Abstract: A compound that thickens or gels a fluid organic substance to a desired viscosity or homogeneously stabilizes a composition containing a fluid organic substance, a thickening/stabilizing agent containing the compound, a thickened/stabilized composition containing the thickening/stabilizing agent and a fluid organic substance, and a method for producing a thickened/stabilized composition. The compound is represented by the following formula (1): In the formula, R1 and R2 are different from each other and represent an aliphatic hydrocarbon group having not less than 4 carbon atoms, and n represents an integer of 1 to 3. The thickening/stabilizing agent of the present invention contains the compound.
    Type: Grant
    Filed: May 1, 2015
    Date of Patent: September 4, 2018
    Assignees: DAICEL CORPORATION, YAMAGUCHI UNIVERSITY
    Inventors: Yuichi Sakanishi, Takashi Saeki, Mami Itoh
  • Patent number: 10011560
    Abstract: Alternative continuous downstream processes for the production of 5-acetamido-N,N?-bis(2,3-dihydroxypropyl)-2,4,6-triiodoisophthalamide (“Compound A”) are described. Compound A is a key intermediate in the production of iodixanol and iohexol, which are two of the biggest commercially available non-ionic x-ray contrast media agents.
    Type: Grant
    Filed: May 24, 2017
    Date of Patent: July 3, 2018
    Assignee: GE HEALTHCARE AS
    Inventors: Torfinn Haaland, Arne Askildsen, Rita Heskestad Kalleberg, Sumihar Silalahi, Alf Martin Farbrot, Inger Dagny Saanum
  • Patent number: 9410142
    Abstract: One aspect of the invention is a salt comprising guanidinium groups, as shown in formula I. Another aspect of the invention is a salt comprising guanidinium groups, as shown in formula II. Another aspect of the invention is a salt comprising guanidinium groups, as shown in formula III. Another aspect of the invention is a salt comprising guanidinium groups, as shown in formula IV. Yet another aspect of the invention is a salt comprising guanidinium groups, as shown in formula I, II, III, and IV further comprising independently for each occurrence citrate, phosphate, or sulfate anion. Also disclosed are compositions comprising a protein and a salt comprising guanidinium groups, as shown in formula I, II, III, and IV. Also provided are methods of increasing shelf life of an aqueous solution of a protein and decreasing the amount of protein aggregation in an aqueous solution of a protein.
    Type: Grant
    Filed: November 11, 2011
    Date of Patent: August 9, 2016
    Assignee: Massachusetts Institute of Technology
    Inventors: Bernhardt L. Trout, II, Diwakar Shukla, Curtiss P. Schneider
  • Patent number: 9096495
    Abstract: The present invention relates to a process for the preparation of given carboxamido compounds, in particular of 2,4,6-triiodoisophthalic acid derivatives, as useful intermediates for the preparation of X-ray contrast media among which is iopamidol. The said process comprises reacting suitable N-sulfinyl intermediate compounds with a commercially available ?-hydroxyacid or a salt thereof.
    Type: Grant
    Filed: March 12, 2010
    Date of Patent: August 4, 2015
    Assignee: Bracco Imaging S.P.A.
    Inventors: Pier Lucio Anelli, Marino Brocchetta, Roberta Fretta, Luciano Lattuada, Armando Mortillaro
  • Publication number: 20150147273
    Abstract: A method for determining whether compound 0118 is a candidate treatment for a patient includes processing, via a processor, image data of tissue of interest of a patient including a cancer to determine whether a radiolabeled analog of compound 0118 is present in the tissue of interest represented in the image data and generating a signal indicating that compound 0118 is a candidate treatment for the patient in response to the determining that the radiolabeled analog of compound 0118 is present in a predetermined amount in the tissue of interest represented in the image data, wherein the presence of the radiolabeled analog of compound 0118 in the tissue of interest indicates presence of a sub-type of cancer having a galectin-1 molecular target, which is a sub-type of treatable by compound 0118.
    Type: Application
    Filed: June 10, 2013
    Publication date: May 28, 2015
    Applicant: Koninklijke Philips N.V.
    Inventors: Tilman Lappchen, Holger Gruell, Marc Stefan Robillard, Johan Lub
  • Publication number: 20150141646
    Abstract: In certain aspects, compounds and uses thereof are provided. In certain aspects, compound-conjugates and uses thereof are provided.
    Type: Application
    Filed: May 14, 2013
    Publication date: May 21, 2015
    Applicant: Concortis Biosystems, Corp., a wholly owned subsidary of Sorrento Therapeutics, Inc,
    Inventors: Zhenwei Miao, Yufeng Hong, Tong Zhu
  • Publication number: 20150119706
    Abstract: Biodegradable computed tomography (CT) contrast agents comprising a polyiodinated aryl contrast agent that is crosslinked by an organic disulfide are described herein. The contrast agents can be used to image a tissue region by administering an effective amount of the biodegradable CT contrast agent to a subject, allowing a sufficient amount of time for the biodegradable CT contrast agent to enter the tissue region, and performing x-ray computed tomography imaging of the tissue region of the subject.
    Type: Application
    Filed: October 31, 2014
    Publication date: April 30, 2015
    Inventors: Zheng-Rong Lu, Erlei Jin, Xiaohui Wu
  • Patent number: 9012687
    Abstract: The present invention provides a process for isolating kukoamine by solid phase extraction using a polyamide or a derivative thereof as an adsorbent. Said process is convenient, economical and environmental-friendly, and obtains highly purified kukoamines with a high yield.
    Type: Grant
    Filed: April 24, 2014
    Date of Patent: April 21, 2015
    Assignee: City University of Hong Kong
    Inventors: Hon-Yeung Cheung, Yuan-Yuan Li, Rui Di
  • Patent number: 8986609
    Abstract: The present invention relates to a terminal sterilization process for biodegradable PEG-based insoluble hydrogels using irradiation. The presence of a protective solvent ensures that the hydrogel remains intact with functionally preserved three-dimensional and physicochemical properties.
    Type: Grant
    Filed: October 28, 2010
    Date of Patent: March 24, 2015
    Assignee: Ascendis Pharma A/S
    Inventors: Harald Rau, Tobias Voigt, Ulrich Hersel
  • Publication number: 20150065752
    Abstract: The present invention provides a process for isolating kukoamine by solid phase extraction using a polyamide or a derivative thereof as an adsorbent. Said process is convenient, economical and environmental-friendly, and obtains highly purified kukoamines with a high yield.
    Type: Application
    Filed: April 24, 2014
    Publication date: March 5, 2015
    Applicant: City University of Hong Kong
    Inventors: Hon-Yeung Cheung, Yuan-Yuan Li, Rui Di
  • Publication number: 20150065681
    Abstract: Disclosed herein is a method of preparing prepolymer particles. The method includes injecting a prepolymer in a solution state by bottom-up type injection to form prepolymer particles by removing a solvent from the prepolymer in a solution state. The method can prepare prepolymer particles, which can be used in solid-state polymerization, using a bottom-up type flash process.
    Type: Application
    Filed: August 22, 2014
    Publication date: March 5, 2015
    Inventors: Jin Kyu KIM, So Young KWON, Sang Kyun IM, Ki Yon LEE, Suk Min JUN, Gook Geon BAE
  • Publication number: 20150060361
    Abstract: A draw solute including an oligomer having an amino acid repeating unit with an ionic moiety and a counter ion thereof, and a forward osmosis water treatment device and method using the same are provided.
    Type: Application
    Filed: August 25, 2014
    Publication date: March 5, 2015
    Inventors: Bo Kyung JUNG, Won Cheol JUNG, Seung Rim YANG, Sung Soo HAN
  • Patent number: 8969619
    Abstract: This invention relates to the synthesis of iodixanol (1,3-bis(acetamido)-N,N?-bis[3,5-bis(2,3-dihydroxypropylaminocarbonyl)-2,4,6-triiodophenyl]-2-hydroxypropane), more specifically to the dimerisation of 5-acetamido-N,N?-bis(2,3-dihydroxypropyl)-2,4,6-triiodo-isophthalamide with propyleneglycol as solvent.
    Type: Grant
    Filed: November 19, 2009
    Date of Patent: March 3, 2015
    Assignee: GE Healthcare AS
    Inventors: Hanne Jorunn H. Johnsen, Lars Terje Holmaas, Trond Kjernli, Ole Magne Homestad
  • Patent number: 8962887
    Abstract: This invention relates to the synthesis of iodixanol (1,3-bis(acetamido)-N,N?-bis[3,5-bis(2,3-dihydroxypropylaminocarbonyl)-2,4,6-triiodophenyl]-2-hydroxypropane), more specifically to the dimerization of 5-acetamido-N,N?-bis(2,3-dihydroxypropyl)-2,4,6-triiodo-isophthalamide with a solvent mixture comprising 1-methoxy-2-propanol and water or methanol.
    Type: Grant
    Filed: November 19, 2009
    Date of Patent: February 24, 2015
    Assignee: GE Healthcare AS
    Inventor: Ole Magne Homestad
  • Patent number: 8962886
    Abstract: This invention relates to the synthesis of iodixanol (1,3-bis(acetamido)-N,N?-bis[3,5-bis(2,3-dihydroxypropylaminocarbonyl)-2,4,6-triiodophenyl]-2-hydroxypropane), more specifically to the dimerisation of 5-acetamido-N,N?-bis(2,3-dihydroxypropyl)-2,4,6-triiodo-isophthalamide with methanol as solvent.
    Type: Grant
    Filed: November 19, 2009
    Date of Patent: February 24, 2015
    Assignee: GE Healthcare AS
    Inventors: Hanne Jorunn H. Johnsen, Lars Terje Holmaas, Ole Magne Homestad
  • Patent number: 8951999
    Abstract: This invention relates to compounds of formula I, their use as inhibitors of the microsomal prostaglandin E2 synthase-1 (mPGES-1), pharmaceutical compositions containing them, and their use as medicaments for the treatment and/or prevention of inflammatory diseases and associated conditions such as inflammatory/nociceptive pain. A, M, R1, R2, R7, Ra, Rb, Q3, Q4, Q6, Z2, Z4, Z5, Z6 and W have meanings given in the description.
    Type: Grant
    Filed: October 20, 2010
    Date of Patent: February 10, 2015
    Assignee: Orexo AB
    Inventors: Henning Priepke, Henri Doods, Raimund Kuelzer, Roland Pfau, Dirk Stenkamp, Robert Roenn, Benjamin Pelcman
  • Patent number: 8946475
    Abstract: The present invention provides methods for preparing a polymeric compound of Formula I: or pharmaceutically acceptable salt thereof. The present invention also provides useful intermediates for preparing the compound of Formula I or pharmaceutically acceptable salt thereof.
    Type: Grant
    Filed: December 19, 2012
    Date of Patent: February 3, 2015
    Assignee: Cellceutix Corporation
    Inventors: Robert W. Kavash, Haizhong Tang, Carol Mulrooney, Dahui Liu
  • Publication number: 20150030670
    Abstract: The present invention is directed to a new class of lipids, more specifically ether-lipids having a polar headgroup, as well as vesicles comprising these lipids, methods of their preparation as well as their uses in medical applications, wherein the ether-lipids are represented by general formula I
    Type: Application
    Filed: March 11, 2013
    Publication date: January 29, 2015
    Applicant: MERCK PATENT GmbH
    Inventors: Michael Wilhelm Platscher, Raymond Behrendt, Viola Groehn, Simone Rachel Hoertner, Marco Silvio Passafaro, Finn Bauer
  • Publication number: 20150030669
    Abstract: The present invention is directed to carrier systems comprising ether-lipids conjugated to one or more bioactive ligands and exposed on the surface of the carrier system for use in targeted delivery and/or antigen display systems. Optionally one or more further bioactive agents may be encapsulated or embedded within or attached to or adsorbed onto the carrier system. The present invention is further directed to methods of their preparation and their uses in medical applications, such as targeted delivery of bioactive agents to specific tissues or cells and antigen display systems for the study, diagnosis, and treatment of traits, diseases and conditions that respond to said bioactive agents.
    Type: Application
    Filed: March 11, 2013
    Publication date: January 29, 2015
    Applicant: MERCK PATENT GMBH
    Inventors: Michael Wilhelm Platscher, Raymond Behrendt, Viola Groehn, Simone Rachel Hoertner, Marco Silvio Passafaro, Finn Bauer
  • Publication number: 20150025250
    Abstract: Compounds of the formula I wherein R2a and R2b are independently H, halo, C1-C4alkyl, C1-C4haloalkyl or C1-C4alkoxy, or R2a and R2b together with the carbon atom to which they are attached form a C3-C6cycloalkyl; R3 is a C5-C10 alkyl, optionally substituted with 1-3 substituents independently selected from halo, C1-C4haloalkyl, C1-C4alkoxy, C1-C4haloalkoxy; or R3 is a C2-C4alkyl chain with at least 2 chloro or 3 fluoro substituents; or R3 is C3-C7cycloalkylmethyl, optionally substituted with 1-3 substituents independently selected from C1-C4alkyl, halo, C1-C4haloalkyl, C1-C4alkoxy, C1-C4haloalkoxy; R4 is C1-C6alkyl, C1-C6haloalkyl, C1-C6alkoxy, C1-C6haloalkoxy, C1-C6alkylamino, C1-C6dialkylamino or; R4 is Het or Carbocyclyl, either of which is optionally substituted with 1-3 substituents R4 is Het, carbocyclyl, C1-C6alkyl, C1-C6haloalkyl, C1-C6alkoxy or C1-C6haloalkoxy; n is 1, 2 or 3; for the use in the prophylaxis or treatment of a disorder characterised by inappropriate expression or activation of cat
    Type: Application
    Filed: October 2, 2014
    Publication date: January 22, 2015
    Inventors: Susana AYESA, Urszula GRABOWSKA, Ellen HEWITT, Daniel JONSSON, Bjorn KLASSON, Pia KAHNBERG, Stina LUNDGREN, Jan TEJBRANT, Daniel WIKTELIUS
  • Patent number: 8912332
    Abstract: The present invention describes tripodal catechol derivatives with a flexible basic framework for the functionalization of surfaces, and methods for their production and use. The central atom of the flexible framework is hereby a tertiary aliphatic carbon atom. The remaining fourth bridgehead position is easily suitable to be further functionalized via so-called click reactions, e.g. with biomolecules, dyes, radiomarkers, polyethylene glycol or active agents.
    Type: Grant
    Filed: September 7, 2011
    Date of Patent: December 16, 2014
    Assignee: Justus-Liebig-Universitaet Giessen
    Inventors: Wolfgang Maison, Faiza Khalil, Elisa Franzmann
  • Patent number: 8901351
    Abstract: A compound represented by formula (I): wherein, in formula (I), R represents a hydrogen atom or an alkyl group having 1 to 4 carbon atom(s); Ra represents a hydrogen atom, an alkyl group, an aryl group, or a heterocyclic group; X represents a halogen atom, or an alkyl- or aryl-sulfonyloxy group; L represents a divalent linking group; Z represents a (n+1)-valent organic group; and n represents an integer of 1 to 6, a plurality of Rs and Ras and Xs may be the same or different from each other, respectively, and when n represents 2 to 6, a plurality of Ls may be the same or different from each other.
    Type: Grant
    Filed: February 22, 2013
    Date of Patent: December 2, 2014
    Assignee: FUJIFILM Corporation
    Inventors: Akihito Amao, Hirotaka Kitagawa
  • Publication number: 20140350113
    Abstract: Described herein are small-molecule mimics of CD4, which both enter the Phe43 cavity and target Asp368 of gp120, the HIV-1 envelope protein. Also described herein are methods of using these compounds to inhibit the transmission or progression of HIV infection. These compounds exhibit antiviral potency greater than that of a known antiviral, NBD-556, with 100% breadth against clade B and C viruses. Importantly, the compounds do not activate HIV infection of CD4-negative, CCR5-positive cells, in contrast to NBD-556.
    Type: Application
    Filed: December 14, 2012
    Publication date: November 27, 2014
    Inventors: Joseph Sodroski, Judith M. LaLonde, Amos B. Smith, III, Peter D. Kwong, Young Do Kwon, David M. Jones, Alexander W. Sun, Joel R. Courter, Takahiro Soeta, Toyoharu Kobayashi, Amy M. Princiotto, Xueling Wu, John R. Mascola, Ame Schon, Emesto Freire, Navid Madani, Matthew Le-Khac, Wayne A. Hendrickson
  • Publication number: 20140341960
    Abstract: Provided is a gelling agent containing N-acyl acidic amino acid dialkylamide having a DL form ratio (D form/L form (weight/weight)) of 5/95-20/80 or 80/20-95/5, and using the gelling agent, a gel composition, particularly a rod-like gel composition, superior in transparency and strength, and superior in compatibility and spreadability when applied to the skin, hair and the like is provided.
    Type: Application
    Filed: July 31, 2014
    Publication date: November 20, 2014
    Applicant: AJINOMOTO CO., INC.
    Inventors: Gaku HATTORI, Masahiro INO
  • Publication number: 20140323568
    Abstract: The present invention includes bis- and tris-benzamide compounds that block AR signaling and have activity against prostate cancer. Uses for these compounds, and pharmaceutical compositions containing the same, also are provided.
    Type: Application
    Filed: April 23, 2014
    Publication date: October 30, 2014
    Applicant: The Board of Regents of the University of Texas System
    Inventors: Jung-Mo AHN, Ganesh RAJ
  • Publication number: 20140315786
    Abstract: The present invention relates to targeting an intracellular enzyme for release of covalently linked bioactives which results in a synergistic effect between the bioactives. The present invention relates to the use of bioactives that are directly connected covalently or through a covalent molecular linker which have increased therapeutic activity when released as the free bioactives by intracellular enzymes as compared to when the bioactives are administered individually (i.e. not covalently linked). Further, methods are described of administering to patients in need thereof, bioactives as linked bioactives having increased therapeutic activity. Accordingly, this invention also relates to methods of treating patients for certain diseases.
    Type: Application
    Filed: March 16, 2012
    Publication date: October 23, 2014
    Applicant: Catabasis Pharmaceuticals, Inc.
    Inventors: Michael R. Jirousek, Jill C. Milne, David Carney, Jean E. Bemis, Chi B. Vu
  • Publication number: 20140308342
    Abstract: The present invention relates to chimeric (preferably, bifunctional) compounds, compositions comprising those compounds and methods of treating cancer in a patient or subject, especially including metastatic cancer where cancer cells exhibit overexpression (heightened expression) of cell surface urokinase-type plasminogen activator receptor (urokinase receptor) compared to normal (non-cancerous) cells. The compounds preferably covalently bind to the urokinase receptor and recruit native antibodies of the patient or subject where the antibodies can selectively degrade and/or deactivate targeted cancer cells through antibody-dependent cellular phagocytosis and/or antibody-dependent cellular cytotoxicity (ADCC) against a large number and variety of cancers, thus providing cancer cell death and/or an inhibition of growth, elaboration and/or metastasis of the cancer, including remission and cure of the patient's cancer.
    Type: Application
    Filed: November 7, 2012
    Publication date: October 16, 2014
    Inventors: David A. Spiegel, Charles E. Jakobsche
  • Patent number: 8859590
    Abstract: Inhibitors of BACE1 and compositions containing them are described. Use of the inhibitors and compositions containing them to treat Alzheimer's disease are described.
    Type: Grant
    Filed: December 4, 2009
    Date of Patent: October 14, 2014
    Assignee: Purdue Research Foundation
    Inventor: Arun K. Ghosh
  • Patent number: 8859605
    Abstract: Compounds of the formula I wherein R1a is H; and R1b is C1-C6alkyl, Carbocyclyl or Het; or R1a and R1b together define a saturated cyclic amine with 3-6 ring atoms; R2a and R2b are independently H, halo, C1-C4alkyl, C1-C4haloalkyl or C1-C4alkoxy, or R2a and R2b together with the carbon atom to which they are attached form a C3-C6cycloalkyl; R3 is a branched C5-C10 alkyl chain, C2-C4haloalkyl or —CH2C3-C7 cycloalkyl; R4 is C1-C6alkyl, C1-C6haloalkyl, C1-C6alkylamino or C1-C6dialkylamino; for use in the prophylaxis or treatment of a disorder characterised by inappropriate expression or activation of cathepsin S.
    Type: Grant
    Filed: December 10, 2010
    Date of Patent: October 14, 2014
    Assignee: Medivir UK Ltd
    Inventors: Susana Ayesa, Peter Carlqvist, Karolina Ersmark, Urszula Grabowska, Ellen Hewitt, Daniel Jonsson, Pia Kahnberg, Bjorn Klasson, Peter Lind, Lourdes Oden, Kevin Parkes, Daniel Wiktelius
  • Patent number: 8859816
    Abstract: A process for the manufacture of polyamide is described. Also described, is a process comprising a stage of initial polymerization under pressure starting from monomers and a stage of finishing in the liquid phase at atmospheric pressure. The finishing stage can employ an injection of inert gas along a direction essentially parallel to that of the flow of the liquid reaction stream.
    Type: Grant
    Filed: July 12, 2011
    Date of Patent: October 14, 2014
    Assignee: Rhodia Operations
    Inventor: Sébastien Lomel
  • Patent number: 8853281
    Abstract: Compounds of the formula I wherein R1a is H; and R1b is C1-C6 alkyl, Carbocyclyl or Het; or R1a and R1b together define a saturated cyclic amine with 3-6 ring atoms; R2a and R2b are H, halo, C1-C4alkyl, C1-C4haloalkyl, C1-C4alkoxy; or R2a and R2b together with the carbon atom to which they are attached form a C3-C6cycloalkyl; R3 is a branched C5-C10alkyl chain, C2-C4haloalkyl or C3-C7cycloalkylmethyl, R4 is Het, Carbocyclyl, optionally substituted as defined in the specification and pharmaceutically acceptable salts, hydrates and N-oxides thereof; are inhibitors of cathepsin S and have utility in the treatment of psoriasis, autoimmune disorders and other disorders such as asthma, arteriosclerosis, COPD and chronic pain.
    Type: Grant
    Filed: December 18, 2009
    Date of Patent: October 7, 2014
    Assignee: Medivir UK Ltd
    Inventors: Susana Ayesa, Anna Karin Belfrage, Bjorn Classon, Urszula Grabowska, Ellen Hewitt, Vladimir Ivanov, Daniel Jönsson, Pia Kahnberg, Peter Lind, Magnus Nilsson, Lourdes Odén, Mikael Pelcman, Horst Wähling
  • Publication number: 20140296343
    Abstract: Methods and compounds for treating neurological and other disorders are provided. Included is the administering to a subject in need thereof an effective amount of a compound having binding and/or modulation specificity for a TrkB receptor molecule.
    Type: Application
    Filed: March 31, 2014
    Publication date: October 2, 2014
    Inventors: Frank M. LONGO, Stephen M. MASSA, Sandeep GUPTA
  • Publication number: 20140294733
    Abstract: The present invention relates to dendrimer synthesis. Specifically, the present invention relates to dendrimer compositions (e.g., scaffolds) capable of copper-free click conjugation for use in the synthesis of functionalized dendrimers, and methods of use of the same.
    Type: Application
    Filed: November 20, 2012
    Publication date: October 2, 2014
    Inventors: James R. Baker, JR., Baohua M. Huang, Thommey P. Thomas
  • Publication number: 20140288221
    Abstract: An aromatic amide compound having the following general formula (I) is provided: wherein, X1 and X2 are independently C(O)HN or NHC(O); G1, G2 and G3 are independently hydrogen, C(O)HN-phenyl, or NHC(O)-phenyl, wherein at least one of G1, G2 and G3 is C(O)HN-phenyl or NHC(O)-phenyl; Q1, Q2, and Q3 are independently hydrogen, C(O)HN-phenyl, or NHC(O)-phenyl, wherein at least one of Q1, Q2, and Q3 is C(O)HN-phenyl or NHC(O)-phenyl; R5 is halo, haloalkyl, alkyl, alkenyl, aryl, heteroaryl, cycloalkyl, or heterocyclyl; and m is from 0 to 4.
    Type: Application
    Filed: June 5, 2014
    Publication date: September 25, 2014
    Inventors: Kamlesh P. Nair, Steven D. Gray
  • Patent number: 8835672
    Abstract: A new compound, (S)-5-(2-acetoxypropanamido)-2,4,6-triiodoisophthalic acid, of formula II (S)-5-(2-acetoxypropanamido)-2,4,6-triiodoisophthalic acid. Said new compound is of use for the production of triiodinated contrast agent, especially lopamidol, with low content of acetyl and hydroxyacetyl analogs. The new compound may be formed from 5-amino-2,4,6-triiodoisophtalic acid by acylating with (S)-1-chloro-1-oxopropan-2-yl acetate. The new compound may then be converted to the respective acid dichloride by reacting with a chlorinating reagent, which is a further object of the present invention, followed by the amidation with 2-amino-1,3-propanediol and acetate hydrolysis.
    Type: Grant
    Filed: February 2, 2012
    Date of Patent: September 16, 2014
    Assignee: Hovione Inter Limited
    Inventors: Jose Manuel Galindro, Ana Cristina Cruz, João José Bandarra, William Heggie
  • Patent number: 8835685
    Abstract: The present invention relates to a process for the preparation of 5-[(2-hydroxyacyl)amino]-2,4,6-triiodo-1,3-benzendicarboxamidic derivatives comprising the Smiles rearrangement of a suitable precursor, by contact of an aqueous solution of this latter with an anion exchanger solid phase.
    Type: Grant
    Filed: July 14, 2011
    Date of Patent: September 16, 2014
    Assignee: Bracco Imaging S.p.A.
    Inventors: Pier Lucio Anelli, Marino Brocchetta, Enrico Cappelletti, Ornella Gazzotti
  • Publication number: 20140234365
    Abstract: The present invention relates to novel 2-hydroxyhippuric acid analogs, and methods for their synthesis and use. Such analogs are designed to provide a protected or functional moiety such as a free thiol (—SH) group or a protected thiol group, thereby providing a convenient linkage chemistry for coupling under mild conditions to a suitable group on a target protein, polypeptide, solid phase or detectable label.
    Type: Application
    Filed: September 27, 2012
    Publication date: August 21, 2014
    Applicant: ALERE SAN DIEGO, INC.
    Inventor: Mariusz Banaszczyk
  • Publication number: 20140228595
    Abstract: Processes include producing hexanediol (HDO), hexamethylenediamine (HMD), adiponitrile (ADN), adipamide (ADM) and derivatives thereof from fermentation broths containing diammonium adipate (DAA), monoammonium adipate (MAA) and/or adipic acid (AA).
    Type: Application
    Filed: September 12, 2011
    Publication date: August 14, 2014
    Applicant: BioAmber S.A.S.
    Inventors: Olan S. Fruchey, Leo E. Manzer, Dilum Dunuwila, Brian T. Keen, Brooke A. Albin, Nye A. Clinton, Bernard D. Dombek
  • Patent number: 8802896
    Abstract: Disclosed is a polyether compound which is useful as a curing agent or the like, a curing agent using the compound and a producing method of the compound. The polyether compound of the present invention is represented by the following general formula (1). (In the formula, R1 represents a hydrogen atom or a methyl group and R2 represents a hydrogen atom or —C(?O)—C(R3)?CH2. R3 represents a hydrogen atom or a methyl group. R1, R2 and R3 may be the same as or different from each other.
    Type: Grant
    Filed: September 30, 2013
    Date of Patent: August 12, 2014
    Assignee: FUJIFILM Corporation
    Inventors: Akihito Amao, Hirotaka Kitagawa
  • Publication number: 20140213611
    Abstract: The present invention provides compounds of formula (I): compositions comprising such compounds; the use of such compounds in therapy (for example in the treatment or prevention of a disease or condition in which plasma kallikrein activity is implicated); and methods of treating patients with such compounds; wherein R1 to R9 are as defined herein.
    Type: Application
    Filed: July 6, 2012
    Publication date: July 31, 2014
    Applicant: KalVista Pharmaceuticals Limited
    Inventors: David Michael Evans, Rebecca Louise Davie, Hannah Joy Edwards, David Philip Rooker
  • Patent number: 8791076
    Abstract: The invention relates to compounds of Formula I: and pharmaceutically acceptable salts and prodrugs thereof, wherein R1, R2, and R3 are defined as set forth in the specification. The compounds are agonists of neurotrophin (such as nerve growth factor) receptors.
    Type: Grant
    Filed: August 31, 2011
    Date of Patent: July 29, 2014
    Inventors: Pablo Villoslada, Angel Messeguer
  • Patent number: 8785641
    Abstract: The present invention describes tripodal catechol derivatives with an adamantyl basic framework for the functionalization of surfaces, methods for their production and use. The remaining fourth bridgehead position is easily suitable to be further functionalised via so-called click reactions, by way of example with biomolecules, dyes, radiomarkers, polyethylene glycol or active agents.
    Type: Grant
    Filed: September 7, 2011
    Date of Patent: July 22, 2014
    Assignee: Justus-Liebig-Universitat Giessen
    Inventors: Wolfgang Maison, Faiza Khalil, Elisa Franzmann
  • Publication number: 20140200257
    Abstract: The invention provides poly(ethylene glycol)-lipid conjugates for use in drug delivery.
    Type: Application
    Filed: January 11, 2012
    Publication date: July 17, 2014
    Applicant: ALNYLAM PHARMACEUTICALS, INC.
    Inventors: Kallanthottathil G Rajeev, Muthiah Manoharan, Muthusamy Jayaraman, Martin Maier, Jayaprakash K. Nair, David Butler
  • Patent number: 8778221
    Abstract: An aromatic amide compound having the following general formula (I) is provided: wherein, X1 and X2 are independently C(O)HN or NHC(O); G1, G2 and G3 are independently hydrogen, C(O)HN-phenyl, or NHC(O)-phenyl, wherein at least one of G1, G2 and G3 is C(O)HN-phenyl or NHC(O)-phenyl; Q1, Q2, and Q3 are independently hydrogen, C(O)HN-phenyl, or NHC(O)-phenyl, wherein at least one of Q1, Q2, and Q3 is C(O)HN-phenyl or NHC(O)-phenyl; R5 is halo, haloalkyl, alkyl, alkenyl, aryl, heteroaryl, cycloalkyl, or heterocyclyl; and m is from 0 to 4.
    Type: Grant
    Filed: August 27, 2012
    Date of Patent: July 15, 2014
    Assignee: Ticona LLC
    Inventors: Kamlesh P. Nair, Steven D. Gray
  • Patent number: 8772296
    Abstract: Benzamide derivatives of formula I are described and have therapeutic utility, particularly in the treatment of diabetes, obesity and related conditions and disorders: wherein R1, R2, R3, R4, R5, R6, R7, R8, and n are as defined herein.
    Type: Grant
    Filed: May 31, 2007
    Date of Patent: July 8, 2014
    Assignee: Amgen Inc.
    Inventors: Jay P. Powers, Michael Degraffenreid, Lisa Julian, Jacob Kaizerman, Dustin McMinn, Yosup Rew, Daqing Sun, Xuelei Yan, Zhulun Wang, Felix Gonzalez Lopez De Turiso
  • Publication number: 20140187499
    Abstract: The invention relates to substituted anionic compounds consisting of a backbone made up of a discrete number u of between 1 and 8 (1?u?8) of identical or different saccharide units, linked via identical or different glycosidic bonds, said saccharide units being chosen from the group consisting of pentoses, hexoses, uronic acids, N-acetylhexosamines in cyclic form or in open reduced form, which are randomly substituted. It also relates to the process for the preparation thereof and to the pharmaceutical compositions comprising same.
    Type: Application
    Filed: November 13, 2013
    Publication date: July 3, 2014
    Inventors: Gérard SOULA, Emmanuel DAUTY, Richard CHARVET
  • Patent number: 8766003
    Abstract: The present invention relates to a process for the preparation of iodinated phenols; in particular; it relates to a process including the direct iodination, with suitably activated iodine, of 3,5-disubstituted phenol compounds to the corresponding 3,5-disubstituted-2,4,6-triiodophenols, which are useful intermediates for the synthesis of x-ray contrast media, and to the preparation of the contrast media themselves.
    Type: Grant
    Filed: June 9, 2011
    Date of Patent: July 1, 2014
    Assignee: Bracco Imaging S.p.A.
    Inventors: Attilio Citterio, Elisa Battistini, Davide Belnome, Federica Buonsanti, Luciano Lattuada, Gabriella Leonardi, Fulvio Uggeri, Evelin Vignale, Massimo Visigalli
  • Patent number: 8766002
    Abstract: An improved synthesis method for preparation of iodixanol, and a purification process through macroporous adsorption resin chromatographic column and recrystallization are provided. The synthesis method relates to dimerization of 5-acetamido-N,N?-bis(2,3-dihydroxypropyl)-2,4,6-triiodo-isophthalamide (compound A) to prepare iodixanol, wherein excessive side reactions such as alkylation are effectively inhibited by controlling the pH of the reaction mixture with a boron-containing acidic substance or salts thereof such as boric acid. In this way, the conversion rate of compound A to iodixanol is 85-90%. The iodixanol crude product is purified by a macroporous adsorption resin chromatographic column, obtaining iodixanol product with recovery of 90-95% and purity of 96-98%. The iodixanol crude product is recrystallized in mixed solvent containing 2-methoxyethanol, obtaining iodixanol product with recovery of 90-95% and purity of greater than 99%.
    Type: Grant
    Filed: November 26, 2009
    Date of Patent: July 1, 2014
    Assignee: Imax Diagnostic Imaging Holding Limited
    Inventors: Zhiqi Hu, Huoying Zhang
  • Publication number: 20140179877
    Abstract: The invention relates to a macromolecule comprising a polymer central core having at least two atoms to which at least two monomers are attached forming a dendrimeric structure comprising at least three polymer bonds, at least two linear polymers (b) being bond to said polymer bonds, wherein said polymers (b) at least have terminal functional groups for cytotoxic agents and at least on extended polymer (a) having a size of at least 1 carbon atoms longer than said polymers (b) and at least a terminal functional group for a targeting agent. The invention also relates to a macromolecule conjugate as well as a macromolecule biotin conjugate comprising said macromolecule, methods to produce said macromolecules as well as kits or system comprising said macromolecules and method of treating a mammal by said macromolecules.
    Type: Application
    Filed: July 18, 2013
    Publication date: June 26, 2014
    Inventors: Rune NILSSON, Bengt SANDBERG, Scott WILBUR