Patents Examined by Matthew Coughlin
  • Pentacyclic pyridoindolobenzo[b,e]diazepines and thiazepines for treating CNS disorders
    Patent number: 9695199
    Abstract: The present invention discloses pyridoinolobenzo[b,e]diazepine and thiazepine derivatives of Formula 1, wherein X is NR10, S, S(O), or S(O)2. Y is a single bond or no bond. A and B are independently (CH2)m and (CH2)n respectively; and the subscripts ‘m’ and ‘n’ independently vary from 1 to 4. R1 to R9 are various electron donating, electron withdrawing, hydrophilic, or lipophilic groups selected to optimize the physicochemical and biological properties of compounds of Formula I.
    Type: Grant
    Filed: February 6, 2017
    Date of Patent: July 4, 2017
    Assignee: DAYA DRUG DISCOVERIES, INC.
    Inventor: Parthasarathi Rajagopalan
  • Chemical crosslinkers and compositions thereof
    Patent number: 9695189
    Abstract: Cleavable crosslinkers of Formula (I) useful reagents in biochemical drug research and development such as antibody drug conjugates are disclosed.
    Type: Grant
    Filed: March 1, 2013
    Date of Patent: July 4, 2017
    Inventor: Mark Quang Nguyen
  • Reactions of thiadiazolyl-oximinoacetic acid derivative compounds
    Patent number: 9695196
    Abstract: This disclosure relates to an improved synthesis of cephalosporin antibiotic compounds such as ceftolozane, and compositions and methods of use thereof. Thiadiazolyl-oximinoacetic acid compounds such as TATD can be reacted to yield the activated thiadiazolyl-oximinoacetic acid methanesulfonate ester compounds useful in the manufacture of cephalosporin antibiotic compounds.
    Type: Grant
    Filed: June 19, 2015
    Date of Patent: July 4, 2017
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Kristos Adrian Moshos, Valdas Jurkauskas, Manuel Scanu, Michele Benotti
  • Protein labeling with cyanobenzothiazole conjugates
    Patent number: 9689868
    Abstract: The invention provides compounds and methods for site-specifically labeling proteins with cyanobenzothiazole derivatives of formula I. For example, the invention provides methods for labeling the N-terminus of a protein that terminates with a cysteine residue. The invention also provides methods for isolating an N-terminally labeled protein and methods for detecting an N-terminally labeled protein.
    Type: Grant
    Filed: September 30, 2016
    Date of Patent: June 27, 2017
    Assignee: PROMEGA CORPORATION
    Inventors: Jessica Kelts, Poncho Meisenheimer, John Shultz
  • Imidazothiadiazole and imidazopyrazine derivatives as protease activated receptor 4 (PAR4) inhibitors for treating platelet aggregation
    Patent number: 9688695
    Abstract: The present invention provides thiazole compounds of Formula I wherein W, Y, R0, R2, R4, R5, R6, R7, X1, X2, X3 and X4 are as defined herein, or a stereoisomer, tautomer, pharmaceutically acceptable salt, prodrug ester or solvate form thereof, wherein all of the variables are as defined herein. These compounds are inhibitors of platelet aggregation and thus can be used as medicaments for treating or preventing thromboembolic disorders.
    Type: Grant
    Filed: April 24, 2013
    Date of Patent: June 27, 2017
    Assignee: BRISTOL-MYERS SQUIBB COMPANY
    Inventors: Jacques Banville, Roger Rémillard, Edward H. Ruediger, Daniel H. Deon, Marc Gagnon, Laurence Dubé, Julia Guy, Eldon Scott Priestley, Shoshana L. Posy, Brad D. Maxwell, Pancras C. Wong, R. Michael Lawrence, Michael M. Miller
  • Substituted condensed pyrimidine compounds
    Patent number: 9688683
    Abstract: Novel substituted condensed pyrimidine compounds of general formula (I) in which the chemical groupings, substituents and indices are as defined in the description, and to their use as medicaments, in particular as medicaments for the treatment of conditions and diseases that can be treated by inhibition of the PDE4 enzyme.
    Type: Grant
    Filed: February 9, 2016
    Date of Patent: June 27, 2017
    Assignee: GRÜNENTHAL GMBH
    Inventors: Florian Jakob, Ingo Konetzki, Tobias Craan, Antonio Nardi, Christian Hesslinger
  • Catalysts for metathesis reactions including enantioselective olefin metathesis, and related methods
    Patent number: 9687834
    Abstract: The present invention provides compositions comprising metal complexes, and related methods. In some embodiments, metal complexes of the invention may be useful as catalysts for chemical reactions, including metathesis reactions, wherein the catalysts exhibit enhanced activity and stereoselectivity. In some embodiments, the invention may advantageously provide metal complexes comprising a stereogenic metal atom. Such metal complexes may be useful in enantioselective catalysis.
    Type: Grant
    Filed: January 23, 2009
    Date of Patent: June 27, 2017
    Assignees: Trustees of Boston College, Massachusetts Institute of Technology
    Inventors: Steven J. Malcolmson, Amir H. Hoveyda, Simon J. Meek, Richard R. Schrock
  • Long chain base sphingosine kinase inhibitors
    Patent number: 9688668
    Abstract: The invention relates to inhibitors of Sphingosine Kinase enzymatic activity, and methods of treating diseases and disorders by administering inhibitors of Sphingosine Kinase enzymatic activity.
    Type: Grant
    Filed: February 8, 2013
    Date of Patent: June 27, 2017
    Assignee: University of Virginia Patent Foundation
    Inventors: Webster L. Santos, Kevin R. Lynch, Timothy L. Macdonald, Andrew Kennedy, Yugesh Kharel, Mithun Rajendra Raje, Joseph Houck
  • Amino-substituted isothiazoles
    Patent number: 9682995
    Abstract: The present invention relates to isothiazoles of general formula (I) which inhibit the mitotic checkpoint: in which A, R1 and R2 are as defined in the claims, to methods of preparing said compounds, to intermediate compounds useful for preparing said compounds, to pharmaceutical compositions and combinations comprising said compounds and to the use of said compounds for manufacturing a pharmaceutical composition for the treatment or prophylaxis of a disease, in particular of neoplasms, as a sole agent or in combination with other active ingredients.
    Type: Grant
    Filed: January 28, 2014
    Date of Patent: June 20, 2017
    Assignee: BAYER PHARMA AKTIENGESELLSCHAFT
    Inventors: Lars Bärfacker, Stefan Prechtl, Gerhard Siemeister, Antje Margret Wengner, Jens Ackerstaff, Katrin Nowak-Reppel, Benjamin Bader, Philip Lienau, Detlef Stöckigt, Tobias Heinrich
  • Androgen receptor modulators and methods for their use
    Patent number: 9682933
    Abstract: Compounds having a structure of Structure I: or a pharmaceutically acceptable salt, tautomer or stereoisomer thereof, wherein R1, R2, R3, R4, R6, Y1 and Y2 are as defined herein, and wherein at least one of R3 or R4 is a straight-chain C1-C6 haloalkyl, are provided. Uses of such compounds for treatment of various indications, including prostate cancer, as well as methods of treatment involving such compounds are also provided.
    Type: Grant
    Filed: May 29, 2015
    Date of Patent: June 20, 2017
    Assignees: British Columbia Cancer Agency Branch, The University of British Columbia
    Inventors: Luping Yan, Raymond J. Andersen, Marianne Dorothy Sadar, Nasrin R. Mawji, Carmen Adriana Banuelos
  • Polyether carbonate polyol production method
    Patent number: 9676905
    Abstract: The invention relates to a method for producing polyether carbonate polyols by attaching alkylene oxides and carbon dioxide to one or more H-functional starters in the presence of a double-metal cyanide catalyst, characterized in that (alpha) a suspending agent which contains no H-functional groups is provided in a reactor, (ss) optionally, a moiety of alkylene oxide is added to the mixture from step (alpha) at temperatures of 90 to 150 DEG C., and the addition of the alkylene oxide compound is then interrupted; and (gamma) one or more H-functional starters are continuously metered into the reactor during the reaction.
    Type: Grant
    Filed: August 23, 2013
    Date of Patent: June 13, 2017
    Assignee: Covestro Deutschland AG
    Inventors: Thomas Ernst Müller, Christoph Gürtler, Jörg Hofmann, Matthias Wohak, Stefanie Braun, Aurel Wolf, Ilja Peckermann
  • Crystal of pyrrole derivative and method for producing the same
    Patent number: 9676713
    Abstract: The present invention provides a production intermediate of an atropisomer of a pyrrole derivative having excellent mineralocorticoid receptor antagonistic activity, a method for producing the same, and a crystal thereof. A method for producing an atropisomer of a pyrrole derivative including a step of resolving a compound represented by the following general formula (I) [wherein R1 represents a methyl group or a trifluoromethyl group, R2 represents a hydrogen atom or a C1-C3 alkoxy group, and n represents an integer selected from 1 to 3] into its atropisomers, characterized by using an optically active amine having a cinchonine skeletal formula, and a crystal of (S)-1-(2-hydroxyethyl)-4-methyl-N-[4-(methylsulfonyl)phenyl]-5-[2-(trifluoromethyl)phenyl]-1H-pyrrole-3-carboxamide.
    Type: Grant
    Filed: November 15, 2016
    Date of Patent: June 13, 2017
    Assignee: Daiichi Sankyo Company, Limited
    Inventors: Masashi Watanabe, Takahiro Okachi, Michiaki Kawahara, Hiroshi Nagasawa, Noritada Sato, Takashi Takita, Gen Hasegawa
  • Bis-indolic derivatives, a process for preparing the same and their uses as a drug
    Patent number: 9676715
    Abstract: Novel bis-indolic derivatives, processes for their preparation, and their potential use as new antibacterial drugs.
    Type: Grant
    Filed: July 20, 2012
    Date of Patent: June 13, 2017
    Assignee: UNIVERSITE JOSEPH FOURIER
    Inventors: Jean-Noël Denis, Marcelle Claude Jolivalt, Louis Maurin Max Maurin, Matthieu Jeanty
  • Myxovirus therapeutics, compounds, and uses related thereto
    Patent number: 9676727
    Abstract: This disclosure relates to antiviral compounds disclosed herein and uses related thereto. In certain embodiments, the disclosure relates to pharmaceutical compositions. Typically, the pharmaceutical composition comprises a compound of formula I: or salt, prodrug, or ester thereof wherein X, Y, and R1 and R10 to R13 are described herein.
    Type: Grant
    Filed: July 7, 2016
    Date of Patent: June 13, 2017
    Assignees: Emory University, Children's Healthcare of Atlanta, Inc.
    Inventors: Richard K. Plemper, James P. Snyder, Aiming Sun
  • Use of quaternary pyridinium salts as vasoprotective agents
    Patent number: 9675601
    Abstract: The invention relates to the use of quaternary pyridinium salts of formula (I), wherein R is NH2, CH3, or N(H)CH2OH group, and X is pharmaceutically acceptable counterion, for the preparation of vasoprotective agent for the treatment or prevention of conditions or diseases associated with dysfunction of vascular endothelium, oxidative stress, and/or insufficient production of endothelial prostacyclin PGI2, in particular but not exclusively if the above coincides with hypercholesterolemia, hypertriglyceridemia or low HDL level.
    Type: Grant
    Filed: May 4, 2016
    Date of Patent: June 13, 2017
    Assignee: Pharmena Spólka Akcyjna (Pharmena S.A.)
    Inventors: Jerzy Gębicki, Stefan Chłopicki
  • Small molecule inhibitors of superoxide dismutase expression
    Patent number: 9669014
    Abstract: Disclosed are new small molecules and the uses thereof for inhibiting superoxide dismutase (SOD) expression. Also disclosed are pharmaceutical compositions comprising the small molecule inhibitors which may be administered in methods of treating diseases or disorders associated with elevated SOD expression or activity, including neurological diseases and disorders such as amyotrophic lateral sclerosis (ALS).
    Type: Grant
    Filed: March 29, 2016
    Date of Patent: June 6, 2017
    Assignee: Northwestern University
    Inventors: Teepu Siddique, Thomas J. Lukas, Hasan Arrat, Gary E. Schiltz
  • Compositions and methods for the treatment of inflammation and lipid disorders
    Patent number: 9670153
    Abstract: The invention relates to the compounds of formula I and formula II or its pharmaceutical acceptable salts, as well as polymorphs, solvates, enantiomers, stereoisomers and hydrates thereof. The pharmaceutical compositions comprising an effective amount of compounds of formula I or formula II; and methods for treating or preventing inflammation and lipid disorders may be formulated for oral, buccal, rectal, topical, transdermal, transmucosal, intravenous, parenteral administration, syrup, or injection. Such compositions may be used to treatment of hypertriglyceridemia, steatohepatitis, cystinosis and inflammatory diseases.
    Type: Grant
    Filed: August 17, 2013
    Date of Patent: June 6, 2017
    Assignee: CELLIX BIO PRIVATE LIMITED
    Inventor: Mahesh Kandula
  • Process for preparing acylglycinates and compositions comprising such compounds
    Patent number: 9662287
    Abstract: A process for preparing acylglycinates of the formula (I) wherein R1 is a linear or branched, saturated alkanoyl group having 6 to 30 carbon atoms, or is a linear or branched, singly or multiply unsaturated alkenoyl group having 6 to 30 carbon atoms, and Q+ is a cation, wherein glycine is reacted with fatty acid chloride R1Cl, in water and in the presence of a basic alkali metal compound which yields cations Q+, but in the absence of organic solvents, at 25-50° C. Also described are compositions comprising acylglycinates of the formula (I).
    Type: Grant
    Filed: July 11, 2012
    Date of Patent: May 30, 2017
    Assignee: Clariant International Ltd.
    Inventors: Peter Klug, Franz-Xaver Scherl
  • Quinoline carboxamide and quinoline carbonitrile derivatives as mGluR2-negative allosteric modulators, compositions, and their use
    Patent number: 9663506
    Abstract: The present invention provides quinoline carboxamide and quinoline carbonitrile compounds of formula (I) wherein ring A, RQ, -L-, R1, n, R2, and R3 are as defined herein. The compounds of the invention are useful as non-competitive mGluR2 antagonists, or mGluR2 negative allosteric modulators (NAMs), and in methods of treating a patient (preferably a human) for diseases or disorders in which the mGluR2-NAM receptor is involved, including potentially Alzheimer's disease, cognitive impairment, schizophrenia and other mood disorders, pain disorders and sleep disorders, by administering to the patient a therapeutically effective amount of a compound of the invention, or a pharmaceutically acceptable salt thereof.
    Type: Grant
    Filed: February 18, 2016
    Date of Patent: May 30, 2017
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Christopher James Bungard, Antonella Converso, Pablo De Leon, Barbara Hanney, Timothy John Hartingh, Jesse Josef Manikowski, Peter J. Manley, Robert Meissner, Zhaoyang Meng, James J. Perkins, Michael T. Rudd, Youheng Shu
  • Production of acetic acid with high conversion rate
    Patent number: 9663437
    Abstract: A process for producing acetic acid comprising the steps of reacting carbon monoxide and at least one of methanol and a methanol derivative in a first reactor under conditions effective to produce a crude acetic acid product; separating the crude acetic acid product into at least one derivative stream, at least one of the at least one derivative stream comprising residual carbon monoxide; and reacting at least a portion of the residual carbon monoxide with at least one of methanol and a methanol derivative over a metal catalyst in a second reactor to produce additional acetic acid. Preferably the second reactor is a homogeneous reactor and a reactor carbon monoxide partial pressure is less than 1.05 MPa.
    Type: Grant
    Filed: February 8, 2012
    Date of Patent: May 30, 2017
    Assignee: CELANESE INTERNATIONAL CORPORATION
    Inventors: G. Paull Torrence, Brian W. Hokkanen, Ronald David Shaver