Patents Examined by Nyeemah A. Grazier
  • Patent number: 10383831
    Abstract: Compounds according to Formula I are provided: and salts thereof, wherein R1, R2, R3, R4, R5, R6, R13, A, X and Y are as defined herein. Methods for preparing compounds of Formula I are also provided, as well as methods of treating cellular proliferative disorders, such as cancer, using compounds of Formula I.
    Type: Grant
    Filed: August 2, 2016
    Date of Patent: August 20, 2019
    Assignee: Temple University—Of The Commonwealth System Of Higher Education
    Inventors: M. V. Ramana Reddy, E. Premkumar Reddy
  • Patent number: 10377720
    Abstract: A process for preparing, 2-[[[1-(4-chlorophenyl)-1H-pyrazol-3-yl]oxy]methyl]-N-hydroxy-benzenamine of formula (I) comprising: mixing 1-(4-chlorophenyl)-3-[(2 -nitrophenyl)methoxy]-1H-pyrazole of formula (II) with a nitrogen-containing base, a sulfur compound, a solvent and a platinum-based catalyst in the presence of hydrogen.
    Type: Grant
    Filed: May 9, 2016
    Date of Patent: August 13, 2019
    Assignee: Adama Makhteshim Ltd.
    Inventors: Gal Suez, Michael Grabarnick, Alexander Frenklah, Heinz Steiner
  • Patent number: 10377770
    Abstract: The present invention provides compounds of Formula (A): (I) as described herein, and salts thereof, and therapeutic uses of these compounds for treatment of disorders associated with Raf kinase activity. The invention further provides pharmaceutical compositions comprising these compounds, and compositions comprising these compounds and a therapeutic co-agent, and methods of using the compositions and combinations to treat conditions including cancers.
    Type: Grant
    Filed: December 15, 2016
    Date of Patent: August 13, 2019
    Assignee: Novartis AG
    Inventors: Robert John Aversa, Matthew T. Burger, Michael Patrick Dillon, Thomas A. Dineen, Jr., Rajesh Karki, Savithri Ramurthy, Vivek Rauniyar, Richard Robinson, Patrick James Sarver
  • Patent number: 10370344
    Abstract: The invention provides compounds of formula (I) wherein X is O or S; R1 is H, OH, SH, nitro, NH2, NHC1-6alkyl, N(C1-6alkyl)2, halo, haloC1-6alkyl, CN, C1-6-alkyl, OC1-6alkyl, C1-6alkylCOOH, C1-6alkylCOOC1-6alkyl, C2-6-alkenyl, C3-10cycloalkyl, C6-10aryl, C1-6alkylC6-10aryl, heterocyclyl, heteroaryl, CONH2, CONHC1-6alkyl, CON(C1-6alkyl)2, OCOC1-6alkyl, or is an acidic group, such as a group comprising a carboxyl, phosphate, phosphinate, sulfate, sulfonate, or tetrazolyl group; R2 is as defined for R1 or R1 and R2 taken together can form a 6-membered aromatic ring optionally substituted by up to 4 groups R5; R3 is H, halo (preferably fluoro), or CHal3 (preferably CF3); each R5 is defined as for R1; V1 is a covalent bond, —O—, or a C1-20alkyl group, or C2-20-mono or multiply unsaturated alkenyl group; said alkyl or alkenyl groups being optionally interrupted by one or more heteroatoms selected from O, NH, N(C1-6 alkyl), S, SO, or SO2; M1 is absent or is a C5-10 cyclic group or a C5-15 aromatic group; and R
    Type: Grant
    Filed: February 24, 2017
    Date of Patent: August 6, 2019
    Assignee: Avexxin AS
    Inventors: George Kokotos, Berit Johansen, Victoria Magrioti, Michael Tsakos
  • Patent number: 10374169
    Abstract: The present invention relates to an organic hole transport material having a compound of the structure shown in formula (I), wherein R1-R2 independently represent hydrogen, C1-C8 substituted or substituted alkyl, C2-C8 substituted or unsubstituted alkenyl, C2-C8 substituted or unsubstituted alkynyl, or C6-C10 substituted or substituted aryl, the substituents being C1-C4 alkyl or halogen. Device experiments show that the organic hole transport material of the present invention has high glass-transition temperature and high thermal stability; a hole-only organic semiconductor diode device and an organic electroluminescent device manufactured by the organic hole transport material have good hole transport performance, high and stable current efficiency, and a long device life.
    Type: Grant
    Filed: November 30, 2016
    Date of Patent: August 6, 2019
    Inventors: Kam-Hung Low, Chin-Hsin Chen, Zhe Li, Lei Dai, Lifei Cai
  • Patent number: 10370329
    Abstract: A process for the resolution of racemic 2-(3-ethoxy-4-methoxyphenyl)-1-(methylsulphonyl)-eth-2-ylamine using novel chiral salts is disclosed. An L-phenylalanine p-toluene-sulfonamide salt of (S)-2-(3-ethoxy-4-methoxyphenyl)-1-(methylsulphonyl)-eth-2-ylamine and a di-p-toluoyl-L-tartaric acid salt of (S)-2-(3-ethoxy-4-methoxyphenyl)-1-(methylsulphonyl)-eth-2-ylamine are also provided.
    Type: Grant
    Filed: April 22, 2016
    Date of Patent: August 6, 2019
    Inventors: Ramesh Dandala, Sureshbabu Jayachandra, Vipin Kumar Kaushik, Nageshwara Rao Achanta, Sivaprasad Dorasala
  • Patent number: 10364254
    Abstract: The present invention relates to novel compounds or pharmaceutically acceptable salts thereof, corresponding pharmaceutical compositions and treatment methods or uses as antibacterials for bacterial infections.
    Type: Grant
    Filed: August 15, 2016
    Date of Patent: July 30, 2019
    Assignee: GlaxoSmithKline Intellectual Property Development Limited
    Inventors: Haifeng Cui, Alan Hennessy, Qi Jin, Timothy James Miles, Stephen Frederick Moss, Neil David Pearson
  • Patent number: 10357451
    Abstract: An object of the present invention is to provide an enteral nutrition that is simply injected and suppresses gastro-esophageal reflux. The present invention provides an enteral nutrition comprising 0.1 to 1.0 mass % of alginic acid and/or sodium salt thereof, calcium, and 0.1 to 3.5 parts by mass of a chelating agent per part by mass of the calcium.
    Type: Grant
    Filed: November 8, 2013
    Date of Patent: July 23, 2019
    Assignee: SAN-EI GEN F.F.I., INC.
    Inventors: Makoto Nakauma, Sayaka Ishihara, Satomi Nakao
  • Patent number: 10351576
    Abstract: The present invention relates to compounds of Formula I, a stereoisomer, enantiomer, a pharmaceutically acceptable salt or an amino acid conjugate thereof; wherein variables are as defined herein; and their pharmaceutical compositions, which are useful as modulators of the activity of Farnesoid X receptors (FXR).
    Type: Grant
    Filed: April 29, 2016
    Date of Patent: July 16, 2019
    Assignee: Novartis AG
    Inventors: Donatella Chianelli, Xiaodong Liu, Valentina Molteni, John Nelson, Jason Roland, Paul Vincent Rucker, David Charles Tully
  • Patent number: 10343984
    Abstract: The present invention relates to a process for the preparation of the compound N-(3,5-dimethylphenyl)-N?-(2-trifluoromethylphenyl) guanidine of formula (I) which comprises reacting a salt of a compound of formula (II) or a mixture of the salt of the compound of formula (II) and a compound of formula (II) with a compound of formula (III), in the presence of a polar organic solvent; a crystalline solid form of the compound of formula (I), in particular crystalline solid form A; to a pharmaceutical composition comprising them; and to their use as a medicament, in particular to the treatment of a condition mediated by Rho-GTPase cell proteins.
    Type: Grant
    Filed: August 10, 2016
    Date of Patent: July 9, 2019
    Assignee: CHEMO RESEARCH. S.L.
    Inventor: José Amato
  • Patent number: 10344020
    Abstract: The disclosure generally relates to compounds of formula I, including their salts, as well as compositions and methods of using the compounds. The compounds are ligands of the NR2B receptor and may be useful for the treatment of various disorders of the central nervous system.
    Type: Grant
    Filed: October 13, 2016
    Date of Patent: July 9, 2019
    Assignee: Bristol-Myers Squibb Company
    Inventors: Imadul Islam, Srinivasan Thangathirupathy, Jayakumar Sankara Warrier, Srinivas Cheruku, Poornima Shetty, Grandhi Venkat Ram Krishna Mohan Gupta, John E. Macor
  • Patent number: 10329254
    Abstract: The invention relates to a novel process for the preparation of rac-6-Chloro-2,3,4,9-tetrahydro-1H-carbazole-1-carboxamide (I) in pharmaceutically acceptable polymorphic form, through the conversion of a 3-bromo-2-oxo-cyclohexanecarboxylic acid alkyl ester into 6-chloro-2,3,4,9-tetrahydro-1H-carbazole-1-carboxylic acid alkyl ester, which in turn is processed to yield the final product.
    Type: Grant
    Filed: April 20, 2016
    Date of Patent: June 25, 2019
    Inventors: Enrica Diodato, Katia Marcucci, Russell Thomas, Paul Wiedenau, Martin Rettig, Huw Roberts
  • Patent number: 10329253
    Abstract: The present invention relates to a process for the synthesis of molecules that have a pyrrole ring bonded to a diol. In particular, the invention relates to the synthesis of molecules that have the pyrrole ring and a diol derived from serinol by means of a process that does not demand the use of solvents or chemical catalysts. The process consists of a first reaction phase that takes place without any solvents and/or organic diluents, giving rise to an intermediate compound, and a second phase in which the intermediate compound is converted into the required compound by heating the reaction mixture to a temperature ranging from 100° to 200° C. for an interval in the range of 1 to 500 minutes, or by adding a carbon allotrope or its derivatives.
    Type: Grant
    Filed: June 12, 2015
    Date of Patent: June 25, 2019
    Assignee: Politencnico di Milano
    Inventors: Vincenzina Barbera, Attilio Citterio, Maurizio Stefano Galimberti, Gabriella Leonardi, Roberto Sebastiano, Suresh Udhavrao Shisodia, Antonio Marco Valerio
  • Patent number: 10329252
    Abstract: The present invention provides a compound represented by General Formula (I). The compound according to the present invention prevents the liquid crystal composition from being deteriorated due to light, has high compatibility with the liquid crystal composition, and does not impair the storage stability of the liquid crystal composition, thus the compound is useful as a constituent member of a liquid crystal composition. Since the liquid crystal composition and the liquid crystal display element containing the compound of the present invention exhibit UV resistance and have a high VHR, it is possible to obtain a liquid crystal display element with excellent display quality in which display defects such as burn-in and display unevenness do not occur or are suppressed.
    Type: Grant
    Filed: August 23, 2016
    Date of Patent: June 25, 2019
    Inventors: Yoshio Aoki, Ayaki Hosono
  • Patent number: 10329292
    Abstract: The present invention relates to substituted xanthine derivatives, pharmaceutical compositions containing them and their use in therapy, particularly in the treatment of conditions having an association with TRPC5 containing ion channels.
    Type: Grant
    Filed: July 10, 2018
    Date of Patent: June 25, 2019
    Assignees: Boehringer Ingelheim International GmbH, Hydra Biosciences, Inc.
    Inventors: Kai Gerlach, Christian Eickmeier, Achim Sauer, Stefan Just, Bertrand L. Chenard
  • Patent number: 10308671
    Abstract: The present invention is concerned with derivatives of 3,5-diphenyl-diazole compounds, which are effective therapeutic agents for use in treating diseases linked to protein aggregation and/or neurodegenerative diseases such as Alzheimer's disease (AD), Parkinson's disease (PD), and Transmissible spongiform encephalopathies (TSEs) such as Creutzfeldt-Jakob disease (CJD). The therapeutic effect is caused by the inhibition of the protein aggregation in the affected tissue, such as the brain. 3,5-Diphenyl-diazole derivatives have been shown to be effective in inhibiting aggregation of proteins but are also characterized by their poor solubility in aqueous solutions. The prodrugs of the invention are modified 3,5-diphenyl-diazole derivatives, which are characterized by their improved solubility in aqueous solutions, and by their increased bioavailability.
    Type: Grant
    Filed: December 14, 2016
    Date of Patent: June 4, 2019
    Assignee: Max-Planck-Gesellschaft zur Forderung
    Inventors: Armin Giese, Felix Schmidt, Christian Griesinger, Andrei Leonov, Sergey Ryazanov
  • Patent number: 10301260
    Abstract: The present invention provides compounds of Formula (I): or a stereoisomer, a tautomer, a pharmaceutically acceptable salt, a polymorph, or a solvate thereof, wherein all of the variables are as defined herein. These compounds are GPR40 G protein-coupled receptor modulators which may be used as medicaments.
    Type: Grant
    Filed: May 6, 2015
    Date of Patent: May 28, 2019
    Assignee: Bristol-Myers Squibb Company
    Inventors: Xiang-Yang Ye, Bruce A. Ellsworth, Elizabeth A. Jurica
  • Patent number: 10287248
    Abstract: The present invention relates to novel processes for the preparation of apremilast of formula I, or a pharmaceutically acceptable salt thereof.
    Type: Grant
    Filed: March 15, 2016
    Date of Patent: May 14, 2019
    Assignee: CIPLA LIMITED
    Inventors: Dharmaraj Ramachandra Rao, Geena Malhotra, Srinivas Laxminarayan Pathi, Ravikumar Puppala, Suryanarayana Durga Yarra
  • Patent number: 10285958
    Abstract: The invention relates to a combination of two or more pharmaceutically active substances, of which at least one is a metabolic product (“metabolite”) of the other (“parent substance”), wherein in particular the dosages thereof are selected such that genotypically or phenotypically related variability in the conversion of the parent substance to the metabolite in particular individuals is compensated for.
    Type: Grant
    Filed: May 27, 2013
    Date of Patent: May 14, 2019
    Inventors: Stefan Willmann, Thomas Eiβing, Kristin Dickschen
  • Patent number: 10285979
    Abstract: A breast cancer therapeutic agent containing 5?-hydroxy-5-nitro-indirubin-3?-oxime as active ingredient has been disclosed. Further, a breast cancer therapeutic agent containing 5?-hydroxy-5-nitro-indirubin-3?-oxime as cyclin-dependent kinase (CDK) inhibitor, wherein said breast cancer is triple negative breast cancer (TNBC) and/or an estrogen receptor (ER) positive breast cancer including the tamoxifen-resistant estrogen receptor (ER) positive breast cancer has been disclosed.
    Type: Grant
    Filed: May 15, 2017
    Date of Patent: May 14, 2019
    Assignee: ANYGEN CO., LTD.
    Inventors: Jae il Kim, Seon-Myung Kim, San Ho Kim, Moon Young Park