Patents Examined by Noble Jarrell
  • Process for the production of trioxane from aqueous formaldehyde sources
    Patent number: 9546148
    Abstract: The present invention relates to a process for producing cyclic acetal comprising i) preparing a liquid reaction mixture comprising a) a formaldehyde source, b) an aprotic compound and c) a catalyst; wherein the total amount of protic compounds is less than 40 wt.-%, based on the total weight of the reaction mixture; and ii) converting the formaldehyde source into cyclic acetals.
    Type: Grant
    Filed: November 23, 2012
    Date of Patent: January 17, 2017
    Assignee: Ticona GmbH
    Inventors: Michael Haubs, Jurgen Lingnau, Klaus Kurz
  • Method for producing dabigatran etexilate methansulphonate
    Patent number: 9546154
    Abstract: An improved method of preparing dabigatran etexilate mesylate (1-salt), is described.
    Type: Grant
    Filed: August 6, 2015
    Date of Patent: January 17, 2017
    Assignee: Boehringer Ingelheim International GmbH
    Inventors: Michael Guenter Wohlgemuth, Volker Brenk, Ingo Heddesheimer, Bernhard Schmitz
  • Phospholipid drug analogs
    Patent number: 9540407
    Abstract: Provided in some embodiments are compositions comprising a compound having a structure according to Formula A or Formula B: or a pharmaceutically acceptable salt, tautomer or hydrate thereof, where X2 is a bond or linker, X3 is bond or —PO4—, and X1, R1, R2, R3, and n are described herein. Also provided in some embodiments are methods for making and using such compounds and compositions.
    Type: Grant
    Filed: September 29, 2015
    Date of Patent: January 10, 2017
    Assignee: UROGEN PHARMA LTD
    Inventors: Roberto Maj, Franco Pattarino, Emanuela Mura, Alcide Barberis
  • Histone deacetylase inhibitors
    Patent number: 9540395
    Abstract: This invention relates to generally inhibiting histone deacetylase (HDAC) enzymes (e.g., HDAC1, HDAC2, and HDAC3).
    Type: Grant
    Filed: February 28, 2012
    Date of Patent: January 10, 2017
    Assignee: BIOMARIN PHARMACEUTICAL INC.
    Inventors: Vincent Jacques, James R. Rusche, Norton P. Peet, Jasbir Singh
  • N-prop-2-ynyl carboxamide derivatives and their use as TRPA1 antagonists
    Patent number: 9533952
    Abstract: Compounds of formula I, wherein A, B, X, Z and R1-R6, are as defined in the claims, exhibit TRPA 1 activity and are thus useful as TRPA1 modulators.
    Type: Grant
    Filed: September 30, 2013
    Date of Patent: January 3, 2017
    Assignee: ORION CORPORATION
    Inventors: Riina Arvela, Terhi Heikkinen, Patrik Holm, Peteris Prusis, Mattias Roslund, Harri Salo
  • C-9 oxygen functionalized labdane derivates
    Patent number: 9527827
    Abstract: This invention relates to diterpenes of general formula (1) belonging to labdane class, isolated from Leucas stelligera, being useful for prevention, treatment, inhibition or controlling growth and proliferation of mycobacterial activity in mammals. The invention further discloses process for isolation of the fractions containing the same.
    Type: Grant
    Filed: August 6, 2012
    Date of Patent: December 27, 2016
    Assignee: COUNCIL OF SCIENTIFIC & INDUSTRIAL RESEARCH
    Inventors: Swati Joshi, Roshan Rajan Kulkarni, Ketaki Dilip Shurpali, Sampa Sarkar, Dhiman Sarkar
  • 2-pyridinecarboxamide derivatives, compositions containing such compounds, and methods of treatment
    Patent number: 9527838
    Abstract: Novel pyridine-2-carboxamide derivatives of formula I and pharmaceutically acceptable salts thereof are disclosed as useful for treating or preventing type 2 diabetes and similar conditions. The compounds are effective as glucokinase activating agents. Pharmaceutical compositions and methods of treatment are also included. The present invention relates to novel pyridine-2-carboxamide derivatives and salts thereof which are effective as glucokinase activating agents. Moreover, it relates to compositions containing such compounds, and methods of treatment.
    Type: Grant
    Filed: December 12, 2013
    Date of Patent: December 27, 2016
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Songnian Lin, Emma R. Parmee, Jiayi Xu
  • ATX modulating agents
    Patent number: 9522889
    Abstract: Disclosed are bicyclic aryl compounds of formula (I), that can modulate the activity of the autotaxin (ATX) enzyme. This invention further relates to compounds that are ATX inhibitors, and methods of making and using such compounds in the treatment of demyelination due to injury or disease, as well as for treating proliferative disorders such as cancer.
    Type: Grant
    Filed: July 26, 2013
    Date of Patent: December 20, 2016
    Assignee: BIOGEN MA INC.
    Inventors: Kevin Guckian, Gnanasambandam Kumaravel, Bin Ma, Sha Mi, Hairuo Peng, Zhaohui Shao, Lihong Sun, Arthur Taveras, Deping Wang, Zhili Xin, Lei Zhang
  • Quinazolinone derivatives as PARP inhibitors
    Patent number: 9522905
    Abstract: The present invention provides compounds of formula (I), their use as PARP inhibitors as well as pharmaceutical compositions comprising said compounds of formula (I) wherein R1, R2, R3, L, X, Y and Z have defined meanings.
    Type: Grant
    Filed: November 12, 2013
    Date of Patent: December 20, 2016
    Assignee: Janssen Pharmaceutica NV
    Inventors: Jerome Emile Jorges Guillemont, Ludo Edmond Josephine Kennis, Josephus Carolus Mertens, Jacobus Alphonsus Josephus Van Dun, Maria Victorina Francisca Somers, Walter Boudewijn Leopold Wouters
  • Pyrazolopyridines and pyrazolopyrimidines
    Patent number: 9518052
    Abstract: A compound having the structure: or a pharmaceutically acceptable salt or solvate thereof, wherein A and A? are C or N, where C may be substituted by halo or C1-C6 alkyl; R and R0 are selected from the group consisting of H, C1-C6 alkyl, —(CH2)n—W, etc., where W is 5- or 6-membered heteroaryl or heterocyclic containing N, S and/or O atoms, —NR?SO2—R?, etc., where R? and R? are C1-C6 alkyl, etc.; wherein each alkyl, etc., may be substituted; or, R and R0 and the N atom to which they are bonded together to form a monocyclic or bicyclic heterocyclic ring, etc.; R1 is H, halo or cyano; R2 and R2? are H, C1-C6 alkyl, etc.; X is a bond, etc.; R3 is H, C1-C4 alkyl, etc.; Y is a bond, —(CH2)m—, etc. The invention also relates to compositions and uses in the treatment of various diseases.
    Type: Grant
    Filed: May 13, 2015
    Date of Patent: December 13, 2016
    Assignee: Pfizer Inc.
    Inventors: Jotham Wadsworth Coe, Christoph Martin Dehnhardt, Peter Jones, Yogesh Anil Sabnis, Joseph Walter Strohbach, Florian Michel Wakenhut, Gavin Alistair Whitlock
  • Purification of intermediates used in the preparation of heterobifunctional linkers
    Patent number: 9518017
    Abstract: The present invention is directed to a method of separating a monocarboxylic represented by the following structural formula: (I) from a dicarboxylic acid represented by the following structural formula: (II) using silica chromatography.
    Type: Grant
    Filed: June 26, 2014
    Date of Patent: December 13, 2016
    Assignee: ImmunoGen, Inc.
    Inventor: Wayne C. Widdison
  • Fluorescent probe for high-sensitivity pancreatic fluid detection, and method for detecting pancreatic fluid
    Patent number: 9506102
    Abstract: A fluorescent probe for detecting pancreatic fluid containing a compound or salt thereof represented by formula (I) below. (In the formula, A represents an amino acid residue or N-substituted amino acid residue, with A forming an amide bond with the adjacent NH in the formula; R1 represents a hydrogen atom or 1 to 4 same or different substituent groups that bond with a benzene ring; R2, R3, R4, R5, R6, and R7 each independently represent a hydrogen atom, a hydroxyl group, an alkyl group, or a halogen atom; R8 and R9 each independently represent a hydrogen atom or an alkyl group; and X represents a C1-C3 alkylene group).
    Type: Grant
    Filed: May 29, 2013
    Date of Patent: November 29, 2016
    Assignee: THE UNIVERSITY OF TOKYO
    Inventors: Yasuteru Urano, Masayo Sakabe, Tetsuo Nagano, Takeaki Ishizawa, Suguru Yamashita, Norihiro Kokudo, Mako Kamiya
  • Functional food additives
    Patent number: 9505738
    Abstract: Novel compounds, and in particular to diacylglycerol (1, 3-DAG) and alpha-lipoic acid (LA) and/or dihydro-alpha-lipoic acid (DHLA) derivatives. In particular these novel compounds are used as functional food additives. These may for example be used as nutraceuticals and/or pharmaceuticals in the prevention and treatment of obesity, diabetes, atherosclerosis, oxidative stress and other lifestyle-related diseases.
    Type: Grant
    Filed: December 6, 2013
    Date of Patent: November 29, 2016
    Inventor: Paresh Dutta
  • Compositions and methods for the treatment of neurologic diseases
    Patent number: 9499526
    Abstract: The invention relates to the compounds of formula I 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, and methods for the treatment of neurologic diseases may be formulated for oral, buccal, rectal, topical, transdermal, transmucosal, intravenous, parenteral administration, syrup, or injection. Such compositions may be used to treatment of depression, Alzheimer's disease, multiple sclerosis, Batten disease, multiple sclerosis, Parkinson's disease (PD) and restless legs syndrome (RLS).
    Type: Grant
    Filed: April 19, 2013
    Date of Patent: November 22, 2016
    Assignee: CELLIX BIO PRIVATE LIMITED
    Inventor: Mahesh Kandula
  • Tridentate cyclometalated metal complexes with six-membered coordination rings
    Patent number: 9502671
    Abstract: Tridentate cyclometalated complexes with rigid six-membered coordination rings of General Formula I having tunable emission wavelengths in the visible range. These emitters are suitable for full color displays and lighting applications.
    Type: Grant
    Filed: July 24, 2015
    Date of Patent: November 22, 2016
    Assignee: Arizona Board of Regents on behalf of Arizona State University
    Inventors: Jian Li, Zhi-Qiang Zhu
  • Quinoline derivatives and uses thereof
    Patent number: 9493420
    Abstract: This disclosure provides a new class of compounds referred to as “reversed chloroquines” (RCQs), which are highly effective against CQR and CQS malaria parasites. RCQs are hybrid molecules, which include an antimalarial quinoline analog (such as chloroquine) moiety and a CQR reversal moiety. Exemplary RCQ chemical structures are provided. Also provided are pharmaceutical compositions including the disclosed RCQ compounds, and methods of using such compounds and compositions for the treatment of malaria and inhibition of CQR or CQS Plasmodium sp. (such as P. falciparum).
    Type: Grant
    Filed: July 25, 2013
    Date of Patent: November 15, 2016
    Assignee: Portland State University
    Inventors: David H. Peyton, Steven Burgess
  • Biaryl- or heterocyclic biaryl-substituted cyclohexene derivative compounds as CETP inhibitors
    Patent number: 9493430
    Abstract: The present invention provides biaryl- or heterocyclic biaryl-substituted cyclohexene derivative compounds, isomers thereof, or pharmaceutically acceptable salts. The compounds of the invention show a CETP inhibitory effect that increases HDL-cholesterol levels and reduces LDL-cholesterol levels. Pharmaceutical compositions comprising the compounds are useful for the prevention or treatment of dyslipidemia or dyslipidemia-related diseases.
    Type: Grant
    Filed: January 29, 2014
    Date of Patent: November 15, 2016
    Assignee: Chong Kun Dang Pharmaceutical Corp.
    Inventors: Jae Kwang Lee, Jung Taek Oh, Jae Won Lee, Seo Hee Lee, Il-Hyang Kim, Jae Young Lee, Su Yeal Bae, Se Ra Lee, Yun Tae Kim
  • Method for producing purified amine compound
    Patent number: 9493418
    Abstract: A method for producing a purified amine compound represented by the formula (1), including: step (A) of reacting a crude form of the amine compound represented by the formula (1) with a hydrogen halide in the presence of water and an organic solvent insoluble in water; step (B) of separating a phase in which a hydrogen halide salt of the amine compound represented by the formula (1) produced in step (A) is dissolved from the other phase(es); step (C) of precipitating the hydrogen halide salt of the amine compound represented by the formula (1) from the phase obtained in step (B) in which the hydrogen halide salt of the amine compound represented by the formula (1) is dissolved; and step (D) of isolating the hydrogen halide salt of the amine compound represented by the formula (1) precipitated in step (C), and reacting the salt with a base.
    Type: Grant
    Filed: December 11, 2013
    Date of Patent: November 15, 2016
    Assignee: SUMITOMO CHEMICAL COMPANY, LIMITED
    Inventor: Tadafumi Matsunaga
  • Polymorphs
    Patent number: 9493462
    Abstract: The invention relates to polymorphous crystal modifications of a DPP-IV inhibitor, the preparation thereof and the use thereof for preparing a medicament.
    Type: Grant
    Filed: January 13, 2016
    Date of Patent: November 15, 2016
    Assignee: Boehringer Ingelheim International GmbH
    Inventors: Peter Sieger, Dirk Kemmer, Peter Kohlbauer, Thomas Nicola, Martin Renz
  • Crystalline forms of genistein
    Patent number: 9492425
    Abstract: The disclosure relates to new crystalline forms of genistein. The disclosed crystalline forms include crystalline genistein sodium salt dihydrate; crystalline genistein potassium salt dihydrate; crystalline genistein calcium salt; crystalline genistein magnesium salt; crystalline genistein L-lysine salt; crystalline genistein N-methylglucamine salt; crystalline genistein N-ethylglucamine salt; crystalline genistein diethylamine salt; and crystalline genistein monohydrate. The disclosure also relates to the novel genistein salts represented by these crystalline forms. Therapeutic compositions containing at least one of these crystalline forms of genistein and/or a genistein salt and a pharmaceutically acceptable carrier are described.
    Type: Grant
    Filed: April 20, 2015
    Date of Patent: November 15, 2016
    Assignee: AXCENTUA PHARMACEUTICALS AB
    Inventors: Anders Berkenstam, Stefan Rehnmark, Michael-Robin Witt, Keith Lorimer, Stephen Watt