Plural Acyclic Chalcogens Bonded Directly At The 2- And At The 4- Or 5- Positions Of The 1,3-diazole Ring [e.g., N-(5-nitro-2-furfuryliden)-1- Amino-hydantoin, Etc.] Patents (Class 548/316.1)
  • Patent number: 9035052
    Abstract: The present invention is directed to solvates and various polymorphic forms of (E)-1-[[[5-(4-chlorophenyl)-2-furanyl]methylene]amino]-3-[4-(4-methyl-1-piperazinyl)butyl]-2,4-imidazolidinedione dihydrochloride and pharmaceutical compositions thereof.
    Type: Grant
    Filed: March 15, 2013
    Date of Patent: May 19, 2015
    Assignee: Warner Chilcott Company, LLC
    Inventors: Nancy Lee Redman-Furey, Nicholas William Geary, Tammy Baker
  • Publication number: 20140336120
    Abstract: A method and composition for the treatment of ischemic neuronal reperfusion injury are provided. The composition can include a compound which is a combination of dantrolene and a residue of FMOC-valine. This composition can be used to provide a faster and higher CNS penetration than heretofore experienced with dantrolene. In another form, dantrolene may be formulated as a pro-drug, a pro-pro-drug and the like.
    Type: Application
    Filed: May 8, 2014
    Publication date: November 13, 2014
    Applicant: Howard University
    Inventors: Harpal S. Mangat, Pradeep K. Karla
  • Publication number: 20140275112
    Abstract: Disclosed herein are methods and compositions comprising compounds capable of normalizing neuronal calcium dyshomeostasis. Also disclosed are methods comprising these compounds for treating neuronal or neurological disorders, including Alzheimer's disease, Parkinson's disease, Huntington's disease, fronto-temporal dementia, Pick's disease, chronic traumatic encepholopathy, traumatic brain injury, stroke, cerebellar ataxia, multiple sclerosis, Down syndrome, and aging-related CNS disorders.
    Type: Application
    Filed: March 14, 2014
    Publication date: September 18, 2014
    Applicant: Rosalind Franklin University of Medicine and Science
    Inventors: Grace E. Stutzmann, Russell Dahl
  • Patent number: 8759384
    Abstract: Compounds represented by Formula I and II, or pharmaceutically acceptable salts thereof: inhibit bacterial 2-epimerase and are useful anti-infective agents.
    Type: Grant
    Filed: May 11, 2009
    Date of Patent: June 24, 2014
    Inventors: David J. Bearss, Hariprasad Vankayalapati, Yong Xu, Charles Erec Stabbins, Vincent A. Fischetti
  • Patent number: 8536213
    Abstract: The invention relates to (among other things) oligomer-dantrolene conjugates and related compounds. A conjugate of the invention, when administered by any of a number of administration routes, exhibits advantages over previously administered compounds.
    Type: Grant
    Filed: November 14, 2008
    Date of Patent: September 17, 2013
    Assignee: Nektar Therapeutics
    Inventors: Jennifer Riggs-Sauthier, Wen Zhang
  • Patent number: 8476449
    Abstract: The present invention is a compound represented by the following formula (1) or a salt thereof. Furthermore, the present invention is an imaging agent used for imaging a tau protein, the imaging agent containing a compound represented by the formula (1) below or a salt thereof. In the formula (1), R3 is a radioactive iodine.
    Type: Grant
    Filed: February 24, 2011
    Date of Patent: July 2, 2013
    Assignees: Nihon Medi-Physics Co., Ltd., Kyoto University
    Inventors: Hideo Saji, Masahiro Ono, Ikuya Seki
  • Publication number: 20130123215
    Abstract: The present invention relates to novel 2,5-dioxoimidazolidin-1-yl-3-phenylurea derivatives, processes for preparing them, pharmaceutical compositions containing them and their use as pharmaceuticals as modulators of the N-formyl peptide receptor like-1 (FPRL-1) receptor.
    Type: Application
    Filed: November 9, 2012
    Publication date: May 16, 2013
    Applicant: ALLERGAN, INC.
    Inventor: Allergan, Inc.
  • Publication number: 20130028966
    Abstract: The invention provides compounds represented by the formulae: (I) and (II) where the compounds are useful in treating, for example, viral and/or parasitic infections. Also provided are pharmaceutical compositions comprising the compounds and methods of treatment using the compounds.
    Type: Application
    Filed: April 13, 2011
    Publication date: January 31, 2013
    Applicant: THE REGENTS OF THE UNIVERSITY OF CALIFORNIA
    Inventors: Benhur Lee, Michael E. Jung, Jihye Lee, Frederic Vigant, Peter J. Bradley, Michael C. Wolf, Bettina E. Hajagos
  • Publication number: 20120330024
    Abstract: The present invention is a compound represented by the following formula (1) or a salt thereof. Furthermore, the present invention is an imaging agent used for imaging a tau protein, the imaging agent containing a compound represented by the formula (1) below or a salt thereof. In the formula (1), R3 is a radioactive iodine.
    Type: Application
    Filed: February 24, 2011
    Publication date: December 27, 2012
    Applicants: Kyoto University, Nihon Medi-Physics Co., Ltd.
    Inventors: Hideo Saji, Masahiro Ono, Ikuya Seki
  • Publication number: 20110046185
    Abstract: The invention relates to compounds of formula (I) wherein the groups R and R? A, D, E, G, L, p and R1 to R10 have the stated meanings and to their physiologically compatible salts. Said compounds are suitable, for example, as anti-obesity drugs.
    Type: Application
    Filed: August 6, 2010
    Publication date: February 24, 2011
    Applicant: SANOFI-AVENTIS
    Inventors: Gerhard JAEHNE, Peter BELOW, Siegfried STENGELIN, Matthias GOSSEL, Thomas KLABUNDE, Irvin WINKLER
  • Publication number: 20100317705
    Abstract: The invention relates to (among other things) oligomer-dantrolene conjugates and related compounds. A conjugate of the invention, when administered by any of a number of administration routes, exhibits advantages over previously administered compounds.
    Type: Application
    Filed: November 14, 2008
    Publication date: December 16, 2010
    Applicant: Nektar Therapeutics
    Inventors: Jennifer Riggs-Sauthier, Wen Zhang
  • Publication number: 20100144723
    Abstract: The invention relates to A 1-(biphenyl-4-ylmethyl)imidazolidine-2,4-dione derivative having the general Formula I wherein R1 is H, (C1-6)alkyl (optionally substituted with oxo, OR4, COOR5, halogen or CN), (C2-6)alkenyl, (C2-6)alkynyl, (C3-6)cycloalkyl or (C3-6)cycloalkyl(C1-3)alkyl; R2 and R2? are independently H or (C1-3)alkyl; or R2 and R2? form together with the carbon atom to which they are bound a (C3-5)cycloalkyl group; R3 represents H or 1 to 4 F substituents; Y represents or NR8R9; X represents CHR6, CF2, O, S, SO or SO2; R4 and R5 are (C1-6)alkyl; R6 is H, OR7 or CN; R7 is (C1-3)alkyl; R8 is (C5-7)cycloalkyl comprising a heteroatom selected from O, S, SO and SO2; R9 is H or (C1-4)alkyl; o and m represent the ortho or meta position of the substituent Y—CH2; or a pharmaceutically acceptable salt thereof; as well as to the use of said 1-(biphenyl-4-ylmethyl)imidazolidine-2,4-dione derivatives in the treatment of pain such as for example peri-operative pain, chronic pain, neuropathic pain, cancer
    Type: Application
    Filed: December 1, 2009
    Publication date: June 10, 2010
    Inventors: Marcelis van der Stelt, Joseph Maria Gerardus Barbara Cals
  • Publication number: 20100105719
    Abstract: The present invention relates to imidazolidinecarboxamide derivatives of the general formula I, wherein R, R1, R2, X and Y are as defined herein, or pharmaceutically usable salts thereof and the use thereof as medicinal substances.
    Type: Application
    Filed: October 2, 2009
    Publication date: April 29, 2010
    Applicant: SANOFI-AVENTIS
    Inventors: Gerhard ZOLLER, Stefan PETRY, Gunter MÜLLER, Norbert TENNAGELS
  • Publication number: 20090093531
    Abstract: The present invention provides for methods of using tert-butyl alcohol (TBA) co-solvent systems in the formulation and production of a pharmaceutical agent with low solubility. The present invention also provides for pharmaceutical compositions made using the novel co-solvent system. In one embodiment, the invention provides for a method of making dantrolene sodium (DS) formulation for intravenous use (DS-IV). This instantaneous reconstitution of the DS-IV product constitutes a significant improvement in the pharmacotherapy of patients undergoing malignant hyperthermia during surgery.
    Type: Application
    Filed: September 5, 2008
    Publication date: April 9, 2009
    Inventor: Ahmad Malkawi
  • Patent number: 6809101
    Abstract: It is found out that compounds represented by the formula (I): wherein R1 is an optionally substituted carbocyclic group or an optionally substituted heterocyclic group; and R2 and R3 taken together with the adjacent carbon atom form an optionally substituted heterocyclic group having one or more of oxo and/or thioxo; have an HCV RNA-dependent RNA synthase inhibitory effect.
    Type: Grant
    Filed: February 27, 2003
    Date of Patent: October 26, 2004
    Assignee: Shionogi & Co., Ltd.
    Inventors: Toshio Fujishita, Kenji Abe
  • Patent number: 6420568
    Abstract: A process for making 1,3-disubstituted-4-oxocyclic ureas of general formula (I): wherein R1, R2, and R3 are independently selected from the group consisting of nil, Cl, F, Br, NH2, NO2, COOH, CH3SO2NH, SO3H, OH, alkoxy, alkyl, alkoxycarbon hydroxyalkyl, carboxyalkyl, and acyloxy; R4 is selected from the group consisting of a substituted or unsubstituted alkyl, alkenyl alkynyl, alkylacyl, and heteroalkyl; and A is a substituted or unsubstituted, saturated or unsaturated, straight-chain or branched alkyl or alkenyl amino group comprised of 1-7 carbon atoms; or A is a substituted or unsubstituted, saturated or unsaturated heterocycle having 5, 6, or 7 members containing at least one nitrogen, and R4 is attached to this nitrogen; wherein said 1,3-disubstituted tuted-4-oxocyclic urea is made without isolation of intermediates and comprising the steps: (Ia) reacting a l-substituted-4-oxocyclic urea with a carbon chain containing at least two leaving groups in the presence of a mild base and a solv
    Type: Grant
    Filed: October 27, 2000
    Date of Patent: July 16, 2002
    Assignee: The Procter & Gamble Company
    Inventors: Patricia Ann Matson, Michael Selden Godlewski
  • Patent number: 6414151
    Abstract: A process for making 1-[[[5-(4-chlorophenyl)-2-furanyl]methylene]amino]-3-[4-(4-methyl-1-piperizinyl)butyl]-2,4-imidazolidinedione having the formula: is disclosed. The process circumvents the use of sodium hydride and isolation of reaction intermediates following the initial coupling of the hydantoin intermediate and 4-N-methylpiperizine.
    Type: Grant
    Filed: October 27, 2000
    Date of Patent: July 2, 2002
    Assignee: The Procter & Gamble Company
    Inventors: Patricia Ann Matson, Michael Selden Godlewski, Daniel Joseph Quarroz, Yves Guggisberg
  • Patent number: 6277997
    Abstract: The present invention relates to a process for the preparation of compounds of formula I wherein R1 and R2 are as defined in the specification as well as to the novel intermediates obtained by said process.
    Type: Grant
    Filed: October 20, 2000
    Date of Patent: August 21, 2001
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Michelangelo Scalone, Ulrich Zutter
  • Patent number: 6222039
    Abstract: The present invention relates to a process for the preparation of compounds of formula I wherein R1 and R2 are as defined in the specification as well as to the novel intermediates obtained by said process.
    Type: Grant
    Filed: July 7, 1999
    Date of Patent: April 24, 2001
    Assignee: Hoffman-La Roche Inc.
    Inventors: Michelangelo Scalone, Ulrich Zutter