Patents Examined by Deepak R. Rao
  • Patent number: 10377698
    Abstract: Diphenethylamine derivatives for use as highly active analgesics, diuretics, anxiolytics, for the treatment of neurodegenerative, psychiatric and neuropsychiatric disorders, and also as anti-itch, anti-addiction, anti-inflammatory, anti-obesity, anti-epileptic, anti-convulsant, anti-seizure, anti-stress, anti-psychotic and anti-depressant medications and their pharmaceutically acceptable salts and easily accessible derivatives thereof (e.g. esters, ethers, amides), processes for their preparation and their application in the manufacture of pharmaceutical products.
    Type: Grant
    Filed: March 30, 2016
    Date of Patent: August 13, 2019
    Assignee: University of Innsbruck
    Inventors: Helmut Schmidhammer, Mariana Spetea, Elena Guerrieri
  • Patent number: 10377725
    Abstract: The present invention relates to a phenyl amino pyrimidine compound or a polymorph of a salt thereof, specifically, to N-(cyanomethyl)-4-(2-((4-(2?,2?,6?,6?-d4-morpholino)phenyl)amino)pyrimidin-4-yl)benzamide, or a pharmaceutically acceptable salt thereof, or a polymorph of a solvate thereof, that is, a compound shown in formula I or salt thereof, or a polymorph of a solvate thereof. The polymorph is suitable for preparing a pharmaceutical composition for suppressing non-receptor tyrosine kinases (such as JAK kinase).
    Type: Grant
    Filed: June 24, 2016
    Date of Patent: August 13, 2019
    Assignee: Suzhou Zelgen Biopharmaceuticals Co., Ltd.
    Inventors: Binhua Lv, Chengwei Li, Dan Xiao
  • Patent number: 10369148
    Abstract: The present invention provides 2,4-pyrimidinediamine compounds that inhibit the IgE and/or IgG receptor signaling cascades that lead to the release of chemical mediators, intermediates and methods of synthesizing the compounds and methods of using the compounds in a variety of contexts, including in the treatment and prevention of diseases characterized by, caused by or associated with the release of chemical mediators via degranulation and other processes effected by activation of the IgE and/or IgG receptor signaling cascades.
    Type: Grant
    Filed: December 1, 2016
    Date of Patent: August 6, 2019
    Assignee: Rigel Pharmaceuticals, Inc.
    Inventors: Rajinder Singh, Ankush Argade, Donald G. Payan, Susan Molineaux, Sacha J. Holland, Jeffrey Clough, Holger Keim, Somasekhar Bhamidipati, Catherine Sylvain, Hui Li, Alexander B. Rossi
  • Patent number: 10370339
    Abstract: The present invention relates to benzimidazol-2-amines of general formula (I), in which R1, R2, R3, R4, R5, R6, R7 and R8 are as defined herein, 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: June 3, 2016
    Date of Patent: August 6, 2019
    Assignee: BAYER PHARMA AKTIENGESELLSCHAFT
    Inventors: Sven Ring, Olaf Panknin, Katja Zimmermann, Judith Günther, Lars Bärfacker
  • Patent number: 10364258
    Abstract: The present invention relates to compounds and methods useful as inhibitors of phosphodiesterase 4 (PDE4) for the treatment or prevention of inflammatory diseases and other diseases involving elevated levels of cytokines and proinflammatory mediators.
    Type: Grant
    Filed: August 24, 2018
    Date of Patent: July 30, 2019
    Assignee: Tetra Discovery Partners, LLC
    Inventors: Mark E. Gurney, Timothy J. Hagen, Xuesheng Mo, A. Samuel Vellekoop, Donna L. Romero, Robert F. Campbell, Joel R. Walker, Lei Zhu
  • Patent number: 10344027
    Abstract: The present invention provides compounds for the prevention or treatment of cancer or a bacterial or viral infection. Additionally, the present invention provides compositions and methods for using these compounds and compositions in the prevention or treatment of cancer or a bacterial or viral infection in a subject.
    Type: Grant
    Filed: October 24, 2018
    Date of Patent: July 9, 2019
    Assignee: Inhibikase Therapeutics, Inc.
    Inventors: Milton H. Werner, Terence A. Kelly
  • Patent number: 10344016
    Abstract: Bromotriazole intermediates are useful in the synthesis of agonists of the APH receptor.
    Type: Grant
    Filed: December 3, 2018
    Date of Patent: July 9, 2019
    Assignee: AMGEN INC.
    Inventors: Paul John Dransfield, Zice Fu, Julie Anne Heath, Jeffrey T. Mihalic, Vatee Pattaropong
  • Patent number: 10335410
    Abstract: Disclosed are chemical entities which are compounds of formula (I): or pharmaceutically acceptable salts thereof; wherein Y, Ra, Ra?, Rb, Rc, X1, X2, X3, Rd, Z1, and Z2 have the values described herein and stereochemical configurations depicted at asterisked positions indicate absolute stereochemistry. Chemical entities according to the disclosure can be useful as inhibitors of Sumo Activating Enzyme (SAE). Further provided are pharmaceutical compositions comprising a compound of the disclosure and methods of using the compositions in the treatment of proliferative, inflammatory, cardiovascular, and neurodegenerative diseases or disorders.
    Type: Grant
    Filed: March 16, 2018
    Date of Patent: July 2, 2019
    Assignee: Millennium Pharmaceuticals, Inc.
    Inventors: Matthew O. Duffey, Dylan England, Brian Scott Freeze, Zhigen Hu, Steven Langston, Charles McIntyre, Hirotake Mizutani, Koji Ono, He Xu
  • Patent number: 10336711
    Abstract: The invention described herein relates to certain pyrimidinetrione N-substituted glycine derivatives of formula (I) which are antagonists of HIF prolyl hydroxylases and are useful for treating diseases benefiting from the inhibition of this enzyme, anemia being one example.
    Type: Grant
    Filed: June 29, 2018
    Date of Patent: July 2, 2019
    Assignee: GlaxoSmithKline LLC
    Inventors: Duke M. Fitch, Antony N. Shaw, Kenneth Wiggall
  • Patent number: 10336780
    Abstract: The invention provides compounds of the formula: R1 is OR11, or NR5R5?; R2 is H or F; R5 is H, C1-C6alkyl, OH, C(?O)R6, O(C?O)R6 or O(C?O)OR6; R5 is H or C1-C6alkyl; R6 is C1-C6alkyl or C3-C7cycloalkyl; R13 is H, phenyl, pyridyl, benzyl, indolyl or naphthyl wherein the phenyl, pyridyl, benzyl, indolyl and naphthyl is optionally substituted with 1, 2 or 3 R22; and the other variables are as defined in the claims, which are of use in the treatment of cancer, and related aspects.
    Type: Grant
    Filed: December 3, 2018
    Date of Patent: July 2, 2019
    Assignee: MEDIVIR AB
    Inventors: Richard Bethell, Anders Eneroth, Bjorn Klasson, Fredrik Oberg
  • Patent number: 10335495
    Abstract: The present invention relates to biomolecule conjugates which comprise a biomolecule wherein at least one non-natural amino acid (NNAA) is integral to the structure of the biomolecule and wherein the NNAA is a point of attachment of a linker to which a payload, particularly a cytotoxic agent, is attached. More specifically, this invention relates to conjugates of cell-binding agents and active release products comprising cytotoxic agents wherein the conjugates are produced by means of a cycloaddition reaction. Methods of production, pharmaceutical compositions and methods of use are provided.
    Type: Grant
    Filed: December 3, 2015
    Date of Patent: July 2, 2019
    Assignee: CELGENE CORPORATION
    Inventors: Eric Schwartz, Laura Akullian D'Agostino, Hernan Cuervo, Wesley Austin
  • Patent number: 10329279
    Abstract: This invention provides a method for enantioselective synthesis of cis-imidazolines and related structures through chiral resolution. A chiral acid is used to separate enantiomeric precursors of the cis-imidazolines from a racemic mixture by selective crystallization. Both enantiomers can be cyclized into the desired cis-imidazoline by complementary pathways. Compounds can be synthesized according to the invention with an enantiomeric excess as high as 99%. Cis-imidazolines such as Nutlin-3a prepared according to this invention may be used for treating cancer, killing senescent cells, or treating senescence-associated conditions.
    Type: Grant
    Filed: April 17, 2018
    Date of Patent: June 25, 2019
    Assignee: Unity Biotechnology, Inc.
    Inventors: Thomas W. von Geldern, Bradley Backes, Bing Chen
  • Patent number: 10328078
    Abstract: The invention provides compounds effective as inhibitors of monocarboxylate transporters such as MCT1 and MCT4, which can be used for treatment of medical conditions wherein treatment of the condition with a compound having an inhibitor effect on MCT1, MCT4, or both is medically indicated. Compounds of the invention can have antitumor, antidiabetes, anti-inflammatory, or immunosuppressive pharmacological effects, and can be effective for treatment of cancer and of type II diabetes.
    Type: Grant
    Filed: January 22, 2016
    Date of Patent: June 25, 2019
    Assignee: The Scripps Research Institute
    Inventors: Thomas D. Bannister, Hui Wang, Chao Wang, John L. Cleveland
  • Patent number: 10323020
    Abstract: The present application relates to novel substituted piperidinyltetrahydroquinolines, to processes for their preparation, to their use for the treatment and/or prevention of diseases and to their use for preparing medicaments for the treatment and/or prevention of diseases, in particular for the treatment and/or prevention of diabetic microangiopathies, diabetic ulcers on the extremities, in particular for promoting wound healing of diabetic foot ulcers, diabetic heart failure, diabetic coronary microvascular heart disorders, peripheral and cardial vascular disorders, thromboembolic disorders and ischaemias, peripheral circulatory disturbances, Raynaud's phenomenon, CREST syndrome, microcirculatory disturbances, intermittent claudication, and peripheral and autonomous neuropathies.
    Type: Grant
    Filed: December 19, 2017
    Date of Patent: June 18, 2019
    Assignee: BAYER PHARMA AKTIENGESELLSCHAFT
    Inventors: Eva Maria Becker-Pelster, Philipp Buchgraber, Anja Buchmüller, Karen Engel, Volker Geiss, Andreas Göller, Herbert Himmel, Raimund Kast, Andreas Knorr, Dieter Lang, Gorden Redlich, Carsten Schmeck, Hanna Tinel, Frank Wunder
  • Patent number: 10314840
    Abstract: The present invention provides 2,4-pyrimidinediamine compounds that inhibit the IgE and/or IgG receptor signaling cascades that lead to the release of chemical mediators, intermediates and methods of synthesizing the compounds and methods of using the compounds in a variety of contexts, including in the treatment and prevention of diseases characterized by, caused by or associated with the release of chemical mediators via degranulation and other processes effected by activation of the IgE and/or IgG receptor signaling cascades.
    Type: Grant
    Filed: February 27, 2017
    Date of Patent: June 11, 2019
    Assignee: Rigel Pharmaceuticals, Inc.
    Inventors: Rajinder Singh, Ankush Argade, Donald G. Payan, Susan Molineaux, Sacha J. Holland, Jeffrey Clough, Holger Keim, Somasekhar Bhamidipati, Catherine Sylvain, Hui Li, Alexander B. Rossi
  • Patent number: 10316016
    Abstract: Described herein are amorphous and crystalline forms of pharmaceutically acceptable salts of the lysine specific demethylase-1 inhibitor 4-[2-(4-aminopiperidin-1-yl)-5-(3-fluoro-4-methoxy-phenyl)-1-methyl-6-oxo-1,6-dihydropyrimidin-4-yl]-2-fluorobenzonitrile. Also described are pharmaceutical compositions suitable for administration to a mammal that include the lysine specific demethylase-1 inhibitor, and methods of using the lysine specific demethylase-1 inhibitor for treating diseases or conditions that are associated with lysine specific demethylase-1 activity.
    Type: Grant
    Filed: July 10, 2018
    Date of Patent: June 11, 2019
    Assignee: CELGENE QUANTICEL RESEARCH, INC.
    Inventors: Young K. Chen, Toufike Kanouni, Stephen W. Kaldor, Jeffrey Alan Stafford, James Marvin Veal, Paula Alessandra Tavares-Greco, Matthew Michael Kreilein
  • Patent number: 10316031
    Abstract: The present invention provides compounds for the prevention or treatment of cancer or a bacterial or viral infection. Additionally, the present invention provides compositions and methods for using these compounds and compositions in the prevention or treatment of cancer or a bacterial or viral infection in a subject.
    Type: Grant
    Filed: October 24, 2018
    Date of Patent: June 11, 2019
    Assignee: Inhibikase Therapeutics, Inc.
    Inventors: Milton H. Werner, Terence A. Kelly
  • Patent number: 10308619
    Abstract: The present invention provides aromatic 4,6-bis-trichloromethyl-s-triazin-2-yl compounds of formula (I), a process for producing para-disubstituted benzonitriles as precursor to give compounds of formula (I) and a process for the production thereof.
    Type: Grant
    Filed: June 21, 2016
    Date of Patent: June 4, 2019
    Assignee: Covestro Deutschland AG
    Inventors: Thomas Rölle, Koichi Kawamura, Guiseppe Chiovetta
  • Patent number: 10307426
    Abstract: Compounds and salts thereof that are useful as JAK kinse inhibitors are described herein. Also provided are pharmaceutical compositions that include such a JAK inhibitor and a pharmaceutically acceptable carrier, adjuvant or vehicle, and methods of treating or lessening the severity of a disease or condition responsive to the inhibition of a Janus kinase activity in a patient.
    Type: Grant
    Filed: May 21, 2018
    Date of Patent: June 4, 2019
    Assignee: Genentech, Inc.
    Inventors: Mark Zak, F. Anthony Romero, Yun-Xing Cheng
  • Patent number: 10308610
    Abstract: The present invention relates to compounds which are inhibitors of phosphodiesterase type 10A and to their use for the manufacture of a medicament and which thus are suitable for treating or controlling of medical disorders selected from neurological disorders and psychiatric disorders, for ameliorating the symptoms associated with such disorders and for reducing the risk of such disorders.
    Type: Grant
    Filed: December 13, 2017
    Date of Patent: June 4, 2019
    Assignees: ABBVIE DEUTSCHLAND GMBH & CO. KG, ABBVIE INC.
    Inventors: Hervé Geneste, Michael Ochse, Karla Drescher, Jürgen Dinges, Clarissa Jakob