Patents Issued in December 13, 2016
  • Process for the preparation of Rosuvastatin calcium and preparation of its novel intermediates
    Patent number: 9518028
    Abstract: The present invention relates to process for the preparation of 7-[4-(4-fluorophenyl)-6-isopropyl-2-(N-methyl-N-methylsulfonylamino)pyrimidin-5-yl]-(3R,5S)-dihydroxy-(E)-6-heptenoic acid calcium having formula (I). The compound of formula (I) has adopted name “Rosuvastatin Calcium”. The present invention is also related to novel intermediates of formula (4) and formula (5) used in preparation of formula (I), and process of their preparation.
    Type: Grant
    Filed: November 18, 2013
    Date of Patent: December 13, 2016
    Assignee: SUVEN LIFE SCIENCES LIMITED
    Inventors: Udaya Bhaskara Rao Siripalli, Veera Reddy Arava, Rajendiran Chinnapillai, Anji Reddy Middekadi, Naresh Raju Makaraju, Venkateswarlu Jasti
  • Certain chemical entities, compositions, and methods
    Patent number: 9518029
    Abstract: Chemical entities based on quinoxaline that are kinase inhibitors are described. Specifically quinoxaline derivatives of Formula I, containing a diarylamide or diarylurea substructure that inhibit Braf mutant kinase activity, pharmaceutical compositions containing the inhibitor compounds and methods of treatment of cancer comprising administering an effective amount of the Braf inhibitor compound are described.
    Type: Grant
    Filed: September 14, 2012
    Date of Patent: December 13, 2016
    Assignee: NeuPharma, Inc.
    Inventors: Xiangping Qian, Yong-Liang Zhu
  • Purification of aryltriazoles
    Patent number: 9518030
    Abstract: Impure aryltriazoles such as benzotriazole and tolyltriazole that are contaminated with dark colored impurities can be purified by conversion to an aryltriazole acid salt by treatment with aqueous acid. The aryltriazole acid salt is water soluble whereas the dark colored impurities are not. The aryltriazole acid salt solution is separated from the dark colored impurities and the aryltriazole acid salt is isolated by precipitation. The free aryltriazole may be recovered by neutralization with base.
    Type: Grant
    Filed: November 30, 2015
    Date of Patent: December 13, 2016
    Inventor: Randolph K Belter
  • Photo-sensitive resin composition, cured film, method for forming a pixel, solid state image sensor, color filter and ultraviolet absorber
    Patent number: 9518031
    Abstract: Provided is a photo-sensitive composition capable of yielding pixels having a high translucency and a large refractive index, with a less amount of development residue in the process of formation. The photo-sensitive resin composition contains an ultraviolet absorber represented by Formula (I); a photo-polymerization initiator; and a polymerizable monomer: wherein each of R1, R2 and R3 independently represents a hydrogen atom or an alkyl group having 1 to 10 carbon atoms; one of R4 and R5 represents an electron withdrawing group, and the other of R4 and R5 represents —SO2R6, —CO2R6, —COR6, —CN or —CONR6R7; each of R6 and R7 independently represents a hydrogen atom, alkyl group having 1 to 8 carbon atoms or aryl group.
    Type: Grant
    Filed: September 28, 2015
    Date of Patent: December 13, 2016
    Assignee: FUJIFILM Corporation
    Inventors: Yutaro Norizuki, Yukie Watanabe, Kazutaka Takahashi
  • Small molecule inhibitors of USP1 deubiquitinating enzyme activity
    Patent number: 9518032
    Abstract: Provided are small molecule inhibitors of ubiquitin specific protease 1 (USP1) activity and methods for their use in treating and characterizing cancers. The small molecule USP1 inhibitors of the invention are particularly useful in the treatment of cancers that are resistant to DNA cross-linking agents.
    Type: Grant
    Filed: April 29, 2011
    Date of Patent: December 13, 2016
    Assignees: Dana-Farber Cancer Institute, Inc., The Brigham and Women's Hospital, Inc.
    Inventors: Alan D. D'Andrea, Gregory D. Cuny, Ross L. Stein, Marcie Glicksman, April Case, Jun Xian, David Wilson, Min Huang
  • (4E)-4-(4-substituted benzylideneamino)-2,3-dihydro-3-substituted-2-thioxothiazole-5-carbonitriles as A2AR antagonist and process for preparation thereof
    Patent number: 9518033
    Abstract: The present invention provides (4E)-4-(4-substituted benzylideneamino)-2,3-dihydro-3-substituted-2-thioxothiazole-5-carbonitriles of general formula A, below, and a process for the preparation thereof. The compounds of present invention are useful in the treatment of central nervous disorders including, Parkinson disease, Huntington's disease, attention disorder, cognition, Alzheimer disease, depression and hypertension.
    Type: Grant
    Filed: January 3, 2014
    Date of Patent: December 13, 2016
    Assignee: Council of Scientific & Industrial Research
    Inventors: Pratibha Mehta Luthra, Chandrabhushan Mishra
  • Synthesis of chiral enaminones, their derivatives, and bioactivity studies thereof
    Patent number: 9518034
    Abstract: This invention provides enantioenriched heterocyclic enaminone compounds with quaternary stereogenic centers and novel methods of preparing the compounds. Methods include the method for the preparation of a compound of formula (I): comprising treating a compound of formula (II): with a transition metal catalyst under alkylation conditions.
    Type: Grant
    Filed: October 14, 2014
    Date of Patent: December 13, 2016
    Assignee: California Institute of Technology
    Inventors: Brian M. Stoltz, Dennis A. Dougherty, Douglas Duquette, Noah Duffy
  • Method for preparing glycidol using glycerol and glycidol obtained thereby
    Patent number: 9518035
    Abstract: A method for preparing glycidol using glycerol includes mixing glycerol with urea in the presence of at least one zinc-based catalyst selected from the group consisting of Zn(NO3)2, ZnCl2, ZnO and Zn(OAc)2 under a pressure of 0.5-10 kPa at a temperature of 100-170° C. to obtain glycerol carbonate; filtering the glycerol carbonate mixed with the zinc-based catalyst through an adsorbent including a polymer resin coordinated with amine groups to separate the zinc-based catalyst and glycerol carbonate from each other; and carrying out reaction of the glycerol carbonate separated from the zinc-based catalyst in the presence of an anion alkali metal salt catalyst that is Na, K, Rb, Cs or a mixture thereof containing at least one anion selected from the group consisting of Cl?, Br?, I?, NO3?, NO2? and acetate under a pressure of 0.13-6.67 kPa at a temperature of 140-250° C. to obtain glycidol.
    Type: Grant
    Filed: February 4, 2016
    Date of Patent: December 13, 2016
    Assignee: KOREA INSTITUTE OF SCIENCE AND TECHNOLOGY
    Inventors: Hyun Joo Lee, Byoung Sung Ahn, Sang Deuk Lee, Ji Sik Choi, Hyejeong Lee, Hye Jin Lee
  • Method for producing ethylene oxide
    Patent number: 9518036
    Abstract: [Problem] To provide a novel technology by which energy efficiency can be further improved in a process for producing ethylene oxide.
    Type: Grant
    Filed: March 28, 2014
    Date of Patent: December 13, 2016
    Assignee: NIPPON SHOKUBAI CO., LTD.
    Inventors: Akimasa Watanabe, Takahiro Takinami, Noriji Morikawa
  • Method for producing N,N-dialkylhomofarnesic acid amide
    Patent number: 9518037
    Abstract: Provided are: a method for producing N,N-dialkylhomofarnesic acid amide, which is a precursor of (±)-3a,6,6,9a-tetramethyldodecahydronaphtho[2.1-b]furan that is useful as a fragrance, at a high recovery rate of a raw material, at a high purity and at a high yield; and a method for producing (±)-3a,6,6,9a-tetramethyldodecahydronaphtho[2.1-b]furan. It is a method for producing N,N-dialkylhomofarnesic acid amide, said method including reacting nerolidol with N,N-dialkylformamide dimethyl acetal under the conditions that the N,N-dialkylformamide dimethyl acetal can be refluxed, wherein the molar ratio of the N,N-dialkylformamide dimethyl acetal to the nerolidol is in a range of 1.5 to 3.
    Type: Grant
    Filed: October 4, 2013
    Date of Patent: December 13, 2016
    Assignee: KAO CORPORATION
    Inventors: Kenji Tanino, Takashi Aoki
  • Condensation product of theanine derivative and carboxylic acid coumarin derivative, its intermediate, preparation method and use thereof
    Patent number: 9518038
    Abstract: The present invention relates to a compound as represented by formula (I), which is a condensation product of a theanine derivative and a carboxylic acid coumarin derivative, compounds as represented by formula (II) and formula (III), both of which are intermediates of the condensation product, a method for preparing these compounds, a pharmaceutical composition comprising the compounds, and a use thereof in preparing a medicament for prevention and treatment of tumors, inflammation, cardiovascular diseases, immune deficiency diseases and the like.
    Type: Grant
    Filed: September 25, 2013
    Date of Patent: December 13, 2016
    Assignee: Shandong Yingdong Yinghao Biotechnology, Inc.
    Inventors: Guoying Zhang, Ying Zhang, Benhao Wu, Guohua Zhang
  • Polymer-fixed derivatives of dithiolane or dithiane
    Patent number: 9518039
    Abstract: Derivatives of 1,3-dithianes and 1,3-dithiolanes of the general formula 1a or salts thereof of the general formula 1b where P=polymeric support, m=1 or 2, Z is an organic linker or X=inorganic or organic anion, processes for preparation thereof and use thereof.
    Type: Grant
    Filed: September 23, 2014
    Date of Patent: December 13, 2016
    Assignee: KARLSRUHER INSTITUT FUER TECHNOLOGIE
    Inventors: Nicole Jung, Simone Graessle, Stefan Braese
  • GDF-8 inhibitors
    Patent number: 9518040
    Abstract: Described are GCF-8 inhibitors of the formula (I), and pharmaceutically acceptable salts thereof, wherein n, R1, R2, R5, R6, X and Z are defined herein. Also provided are pharmaceutical compositions comprising the same. Such compounds and compositions are useful in methods for inhibiting GDF-8 in a cell and methods for treating a patient suffering from a disease or disorder, wherein the patient would therapeutically benefit from an increase in mass or strength of muscle tissue.
    Type: Grant
    Filed: August 24, 2015
    Date of Patent: December 13, 2016
    Assignee: Rigel Pharmaceuticals, Inc.
    Inventors: Somasekhar Bhamidipati, Marina Gelman, Pingyu Ding, Rajinder Singh, Jeffrey Clough, Todd Kinsella, Donald Payan
  • (+)-5-(3,4-difluorophenyl)-5-[(3-methyl-2-oxopyridin-1(2H)-yl)methyl]imidazolidine-2,4-dione and drug containing same
    Patent number: 9518041
    Abstract: Provided is (+)-5-(3,4-difluorophenyl)-5-[(3-methyl-2-oxopyridin-1(2H)-yl)methyl]imidazolidine-2,4-dione or a salt thereof. Also provided is a drug containing as the active ingredient (+)-5-(3,4-difluorophenyl)-5-[(3-methyl-2-oxopyridin-1(2H)-yl)methyl]imidazolidine-2,4-dione or a salt thereof.
    Type: Grant
    Filed: June 6, 2014
    Date of Patent: December 13, 2016
    Assignee: KAKEN PHARMACEUTICAL CO., LTD.
    Inventors: Noriyuki Kamei, Daigo Kamimura, Yoshitake Sumikawa, Shota Tokuoka
  • Nitrogen-containing heterocyclic compound
    Patent number: 9518042
    Abstract: The present invention provides a compound having a cholinergic muscarinic M1 receptor positive allosteric modulator activity and useful as an agent for the prophylaxis or treatment of Alzheimer's disease, schizophrenia, pain, sleep disorder, Parkinson's disease dementia, dementia with Lewy bodies, and the like. The present invention relates to a compound represented by the formula (I) or a salt thereof. wherein each symbol is as described in the specification, or a salt thereof.
    Type: Grant
    Filed: February 2, 2016
    Date of Patent: December 13, 2016
    Assignee: Takeda Pharmaceutical Company Limited
    Inventors: Masami Yamada, Shinkichi Suzuki, Takahiro Sugimoto, Minoru Nakamura, Hiroki Sakamoto, Makoto Kamata
  • Method for preparing 1-(4-(4-(3,4-dichloro-2-fluorophenylamino)-7-methoxyquinazolin-6-yloxy)piperidin-1-yi)prop-2-en-1-one
    Patent number: 9518043
    Abstract: The present invention relates to a novel method for preparing 1-(4-(4-(3,4-dichloro-2-fluorophenylamino)-7-methoxyquinazolin-6-yloxy)piperidin-1-yl)prop-2-en-1-one in a simpler process as compared with conventional methods by allowing 4-(3,4-dichloro-2-fluorophenylamino)-7-methoxyquinazolin-6-ol to react with an N-acyl piperidine derivative in an inert polar protic solvent in the presence of a base.
    Type: Grant
    Filed: January 27, 2014
    Date of Patent: December 13, 2016
    Assignee: Hanmi Pharm. Co., Ltd.
    Inventors: Keuk Chan Bang, Jae Hyuk Jung, Young Ho Moon
  • Prostaglandin receptor EP2 antagonists, derivatives, compositions, and uses related thereto
    Patent number: 9518044
    Abstract: The present invention is directed to compounds of Formula IC: wherein the substituents are described herein. These compounds and their pharmaceutically acceptable salts thereof are prostaglandin receptor EP2 antagonists.
    Type: Grant
    Filed: June 19, 2012
    Date of Patent: December 13, 2016
    Assignee: Emory University
    Inventors: Jianxiong Jiang, Thota Ganesh, Yuhong Du, Pahk Thepchatri, Yi Quan, Ray J. Dingledine
  • Process for manufacturing benzoxazinones
    Patent number: 9518045
    Abstract: The present invention relates to a process for manufacturing benzoxazinones of formula (I), wherein the variables are defined according to the description, by reacting carbamates of formula (II) are reacted with carbamat-benzoxazinones of formula (III) in the presence of a base.
    Type: Grant
    Filed: August 9, 2013
    Date of Patent: December 13, 2016
    Assignee: BASF SE
    Inventors: Maximilian Dochnahl, Roland Goetz, Joachim Gebhardt, Uwe Josef Vogelbacher, Timo Frassetto, Michael Rack, Volker Maywald, Bernd Wolf
  • Substituted aminopyrimidine compounds and methods of use
    Patent number: 9518046
    Abstract: The invention relates to the preparation and use of new aminopyrimidine derivatives as drug candidates in free form or in pharmaceutically acceptable salt form and formulations thereof for the modulation of a disorder or disease which is mediated by the activity of the PI3K enzymes. The invention also provides pharmaceutically acceptable compositions comprising such compounds and methods of using the compositions in the treatment of disorders or diseases, such as disorders of immunity and inflammation in which PI3K enzymes play a role in leukocyte function, and hyperproliferative disorders associated with PI3K activity, including but not restricted to leukemias and solid tumors, in mammals, especially humans.
    Type: Grant
    Filed: March 15, 2015
    Date of Patent: December 13, 2016
    Assignees: CALITOR SCIENCES, LLC, SUNSHINE LAKE PHARMA CO., LTD.
    Inventors: Ning Xi, Liang Wang, Zuping Wu, Xuejin Feng, Yanjun Wu
  • Process for the industrial synthesis of lurasidone
    Patent number: 9518047
    Abstract: Disclosed is a process for the industrial synthesis of Lurasidone from (1R,2R)-cyclohexane-1,2-diyldimethanol (1), 3-(piperazin-1-yl)benzo[d]isothiazole (3) and (3aR,4R,7R,7aS)-3a,4,7,7a-tetrahydro-4,7-methanoisobenzofuran-1,3-dione (6).). Said process is optimised to obtain Lurasidone with high yields and high purities by preparing highly pure synthesis intermediates, using critical raw materials and reagents in amounts close to the stoichiometric amounts, increasing productivity and reducing the costs and environmental impact of the process.
    Type: Grant
    Filed: October 16, 2014
    Date of Patent: December 13, 2016
    Assignee: PROCOS S.P.A.
    Inventors: Tommaso Angelini, Piergiorgio Bettoni, Jacopo Roletto, Paolo Paissoni
  • Process for the preparation of teneligliptin
    Patent number: 9518048
    Abstract: A process for the preparation of teneligliptin.
    Type: Grant
    Filed: August 28, 2013
    Date of Patent: December 13, 2016
    Assignee: Glenmark Pharmaceuticals Limited
    Inventors: Suresh Mahadev Kadam, Bipin Parsottam Kansagra, Ramchandran Vishnue Kale, Jayant Prakashrao Patil, Venkataramana Reddy Yemireddy, Shailendra Nilkanth Bhadane, Uddhav Popat Chaudhar, Ulhas Digambar Patil, Shekhar Bhaskar Bhirud
  • Salt forms of (S)-quinuclidin-3-yl (2-(2-(4-fluorophenyl)thiazol-4-yl)propan-2-yl)carbamate
    Patent number: 9518049
    Abstract: The present invention relates to novel salt forms of (S)-Quinuclidin-3-yl (2-(2-(4-fluorophenyl)thiazol-4-yl)propan-2-yl)carbamate useful as an inhibitor of glucosylceramide synthase (GCS) and for the treatment metabolic diseases, such as lysosomal storage diseases, either alone or in combination with enzyme replacement therapy, and for the treatment of cancer.
    Type: Grant
    Filed: March 14, 2014
    Date of Patent: December 13, 2016
    Assignee: GENZYME CORPORATION
    Inventors: Craig S. Siegel, Jin Zhao
  • Cyclohexyl and quinuclidinyl carbamate derivatives having ?2 adrenergic agonist and M3 muscarinic antagonist activity
    Patent number: 9518050
    Abstract: The present invention relates to novel compounds having ?2 adrenergic agonist and M3 muscarinic antagonist dual activity, to pharmaceutical compositions containing them, to the process for their preparation and to their use in respiratory therapies.
    Type: Grant
    Filed: December 17, 2013
    Date of Patent: December 13, 2016
    Assignee: Almirall, S.A.
    Inventors: Laia Sole Feu, Ines Carranco Moruno, Jose Aiguade Bosch, Carlos Puig Duran, Silvia Fonquerna Pou
  • Pyrroloquinoline alkaloids as antimalarial agents and process for the preparation thereof
    Patent number: 9518051
    Abstract: The patent provides novel compounds with potential anti-malarial activity and process of synthesis thereof. Further, the process for the synthesis of known antimalarial natural products marinoquinazolinone A-F, aplidiopsamine A and their potential antimalarial analogs is disclosed.
    Type: Grant
    Filed: February 8, 2013
    Date of Patent: December 13, 2016
    Assignee: Council of Scientific & Industrial Research
    Inventors: Santosh Baburao Mhaske, Jyoti Reveji Lande
  • 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
  • Fluorinated integrin antagonists
    Patent number: 9518053
    Abstract: The present invention relates to fluorinated compounds of formula I and methods of synthesizing these compounds. The present invention also relates to pharmaceutical compositions containing the fluorinated compounds of the invention, and methods of treating macular degeneration, diabetic retinopathy (DR), macular edema, diabetic macular edema (DME), and macular edema following retinal vein occlusion (RVO), by administering these compounds and pharmaceutical compositions to subjects in need thereof.
    Type: Grant
    Filed: February 7, 2014
    Date of Patent: December 13, 2016
    Assignee: SciFluor Life Sciences, Inc.
    Inventors: Ben C. Askew, Richard W. Heidebrecht, Takeru Furuya, Mark E. Duggan, D. Scott Edwards
  • 2-(azaindol-2-yl) benz imidazoles as PAD4 inhibitors
    Patent number: 9518054
    Abstract: Compounds of formula (I) wherein; R1 is hydrogen or C1-6alkyl; R2 is hydrogen, C1-6alkyl, perhalomethylC0-5alkyl-O—, or C1-6alkoxy; R3 is hydrogen, C1-6alkyl, or C1-6alkoxyC1-6alkyl; R4 is hydrogen, C1-6alkyl, perhalomethylC1-6alkyl; or unsubstituted C3-6cycloalkylC1-6alkyl; A is C—R5 or N; B is C—R6 or N; D is C—R7 or N; with the proviso that at least one of A, B, and D, is N; R5 is hydrogen or C1-6alkyl; R6 is hydrogen or C1-6alkyl; R7 is hydrogen, C1-6alkyl, C1-6alkoxy, or hydroxy; R8 is hydrogen or C1-6alkyl, with the proviso that one of R4 and R8 is hydrogen; R9 is hydrogen or hydroxy; R10 is hydrogen or C1-6alkyl; and salts thereof are PAD4 inhibitors and may be useful in the treatment of various disorders, for example rheumatoid arthritis, vasculitis, systemic lupus erythematosus, ulcerative colitis, cancer, cystic fibrosis, asthma, cutaneous lupus erythematosis, and psoriasis.
    Type: Grant
    Filed: August 3, 2015
    Date of Patent: December 13, 2016
    Assignee: GLAXO GROUP LIMITED
    Inventors: Stephen John Atkinson, Michael David Barker, Matthew Campbell, Hawa Diallo, Clement Douault, Neil Stuart Garton, John Liddle, Robert John Sheppard, Ann Louise Walker, Christopher Wellaway, David Matthew Wilson
  • Imidazopyridyl compounds as aldosterone synthase inhibitors
    Patent number: 9518055
    Abstract: This invention relates to imidazopyridyl compounds of the structural formula: or their pharmaceutically acceptable salts, wherein the variable are defined herein. The inventive compounds selectively inhibit aldosterone synthase. This invention also provides for pharmaceutical compositions comprising the compounds of Formula I or their salts as well as potentially to methods for the treatment, amelioration or prevention of conditions that could be treated by inhibiting aldosterone synthase.
    Type: Grant
    Filed: October 16, 2015
    Date of Patent: December 13, 2016
    Assignee: Merck Sharp & Dohme
    Inventors: Amjad Ali, D. Jonathan Bennett, Jaiqiang Cai, Emma Carswell, Andrew Cooke, Scott B. Hoyt, Michael Lo, Clare London, John MacLean, Min K. Park, Paul Ratcliffe, Jerry Andrew Taylor, Brent Whitehead, Yusheng Xiong
  • Inhibitors of influenza viruses replication
    Patent number: 9518056
    Abstract: Methods of inhibiting the replication of influenza viruses in a biological sample or patient, of reducing the amount of influenza viruses in a biological sample or patient, and of treating influenza in a patient, comprises administering to said biological sample or patient an effective amount of a compound represented by Structural Formula (I): or a pharmaceutically acceptable salt thereof, wherein the values of Structural Formula (IA) are as described herein. A compound is represented by Structural Formula (IA) or a pharmaceutically acceptable salt thereof, wherein the values of Structural Formula (IA) are as described herein. A pharmaceutical composition comprises an effective amount of such a compound or pharmaceutically acceptable salt thereof, and a pharmaceutically acceptable carrier, adjuvant or vehicle.
    Type: Grant
    Filed: November 2, 2015
    Date of Patent: December 13, 2016
    Assignee: Vertex Pharmaceuticals Incorporated
    Inventors: Paul S. Charifson, Michael P. Clark, Upul K. Bandarage, Randy S. Bethiel, John J. Court, Hongbo Deng, Ioana Davies, John P. Duffy, Luc J. Farmer, Huai Gao, Wenxin Gu, Dylan H. Jacobs, Joseph M. Kennedy, Mark W. Ledeboer, Brian Ledford, Francois Maltais, Emanuele Perola, Tiansheng Wang, M. Woods Wannamaker, Randal Byrn, Yi Zhou, Chao Lin, Min Jiang, Steven Jones, Ursula A. Germann, Francesco G. Salituro, Ann Dak-Yee Kwong
  • Derivatives and methods of treating hepatitis B infections
    Patent number: 9518057
    Abstract: Provided herein are compounds useful for the treatment of HBV infection in a subject in need thereof, pharmaceutical compositions thereof, and methods of inhibiting, suppressing, or preventing HBV infection in the subject.
    Type: Grant
    Filed: December 30, 2015
    Date of Patent: December 13, 2016
    Assignee: NOVIRA THERAPEUTICS, INC.
    Inventors: George D. Hartman, Scott Kuduk
  • Process for the preparation of N,N-dicyclopropyl-4-(1,5-dimethyl-1H-pyrazol-3-ylamino)-6-ethyl-1-methyl-1,6-dihydroimidazo[4,5-d]pyrrolo[2,3-b]pyridine-7-carboxamide
    Patent number: 9518058
    Abstract: The invention relates to an improved process for synthesizing N,N-dicyclopropyl-4-(1,5-dimethyl-1H-pyrazol-3-ylamino)-6-ethyl-1-methyl-1,6-dihydroimidazo[4,5-d]pyrrolo[2,3-b]pyridine-7-carboxamide of the formula: (I) Compound (I) is currently in clinical trials for the treatment of myeloproliferative disorders, such as polycythaemia vera, thrombocythaemia and primary myelofibrosis.
    Type: Grant
    Filed: August 28, 2014
    Date of Patent: December 13, 2016
    Assignee: Bristol-Myers Squibb Company
    Inventors: Martin D. Eastgate, Gregory L. Beutner, Benjamin Cohen, Nicolas Cuniere, Lopa V. Desai, Monica Fitzgerald, Qi Gao, Michael Bryan Hay, Michael Joseph Lawler, Paul C. Lobben, Christopher S. Regens, Thorsten Rosner, Neil Strotman, Carolyn S. Wei, Yi Xiao, Bin Zheng, Keming Zhu
  • Inhibitor crystalline form and preparation method and use thereof
    Patent number: 9518059
    Abstract: The present invention relates to new crystalline forms of the inhibitor, 5-fluoro-3-phenyl-2-[(S)-1-(9H-purin-6-ylamino)-propyl]-3H-quinazoline-4-one; the present invention also relates to methods for preparing the new crystalline forms of 5-fluoro-3-phenyl-2-[(S)-1-(9H-purin-6-ylamino)-propyl]-3H-quinazolin-4-one, pharmaceutical compositions containing the new crystalline forms thereof, and uses thereof for the treatment and/or prevention of diseases such as chronic lymphocytic leukemia and indolent non-Hodgkin's lymphoma.
    Type: Grant
    Filed: December 2, 2015
    Date of Patent: December 13, 2016
    Assignee: HANGZHOU PUSHAI PHARMACEUTICAL TECHNOLOGY
    Inventors: Zhonghua Zhang, Xiaoxia Sheng, Xiaohong Sheng
  • Substituted pyrrolo[3,4-c]pyrazoles as PKC kinase inhibitors
    Patent number: 9518060
    Abstract: The present invention relates to compounds and pharmaceutically acceptable salts of Formulas A and B: wherein A, B, R1, R2, R3, R4, R5, R6, R7, R8, R9 and R10 are as defined above. The invention further relates to pharmaceutical compositions comprising the compounds and pharmaceutically acceptable salts and to methods of treating diabetes mellitus and its complications, cancer, ischemia, inflammation, central nervous system disorders, cardiovascular disease, Alzheimer's disease and dermatological disease pression, virus diseases, inflammatory disorders, or diseases in which the liver is a target organ.
    Type: Grant
    Filed: October 3, 2014
    Date of Patent: December 13, 2016
    Assignee: PFIZER INC.
    Inventors: Hui Li, Seiji Nukui, Stephanie Anne Scales, Min Teng, Chunfeng Yin
  • Substituted pyrazolylpyrazole derivative and use of same as herbicide
    Patent number: 9518061
    Abstract: Provided is a compound capable of effectively control worst weeds of higher leaf stages that present practical problems. A specific pyrazolylpyrazole derivative of formula (1) is disclosed that is able to solve the above-mentioned problems.
    Type: Grant
    Filed: August 11, 2014
    Date of Patent: December 13, 2016
    Assignee: KYOYU AGRI CO., LTD.
    Inventors: Ken Matsubara, Makoto Niino
  • Compounds and compositions for use in phototherapy and in treatment of ocular neovascular disease and cancers
    Patent number: 9518062
    Abstract: The invention relates generally to anti-angiogenesis agents and related methods of using to anti-angiogenesis agents for biomedical applications including direct monotherapy and combination therapy for treatment of an angiogenesis related condition. In an embodiment, the invention provides a class of opioid compounds and structurally related opioid derivatives exhibiting anti-VEGF activity for use in therapeutic procedures, including phototherapy. Opioid compounds and structurally related opioid derivatives of the invention may be administered alone or in combination with administration of a phototherapy agent and/or other therapeutic agent.
    Type: Grant
    Filed: June 26, 2014
    Date of Patent: December 13, 2016
    Assignee: Mallinckrodt LLC
    Inventors: Gary L. Cantrell, Raghavan Rajagopalan, Amolkumar Karwa, Richard B. Dorshow
  • Organic electroluminescent materials and devices
    Patent number: 9518063
    Abstract: A new class of compounds containing aza-dibenzothiophene or aza-dibenzofuran are provided. The compounds may be used in organic light emitting devices giving improved stability, improved efficiency, long lifetime and low operational voltage. In particular, the compounds may be used as the host material of an emissive layer having a host and an emissive dopant, or as a material in an enhancement layer.
    Type: Grant
    Filed: June 10, 2015
    Date of Patent: December 13, 2016
    Assignee: Universal Display Corporation
    Inventors: Chun Lin, Bin Ma, Raymond Kwong, Alexey Borisovich Dyatkin, Yonggang Wu, Zeinab M. Elshenawy
  • Imidazothiadiazole and imidazopyridazine derivatives as protease activated receptor 4 (PAR4) inhibitors for treating platelet aggregation
    Patent number: 9518064
    Abstract: The present invention provides imidazothiadiazole compounds of Formula (I); Wherein W, Y, R0, R2, R4, Ra, Rb, 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: December 13, 2016
    Assignees: Bristol-Myers Squibb Company, Universite De Montreal
    Inventors: Alain Martel, François Tremblay, Anne Marinier, Eldon Scott Priestley, Shoshana L. Posy, R. Michael Lawrence, Michael M. Miller
  • IRAK inhibitors and uses thereof
    Patent number: 9518065
    Abstract: The present invention provides compounds of the general formula I: or a pharmaceutically acceptable salt thereof, wherein each variable is as defined and described herein, as inhibitors of one or more interleukin-1 receptor-associated kinases (“IRAK”).
    Type: Grant
    Filed: September 25, 2014
    Date of Patent: December 13, 2016
    Assignee: Nimbus Iris, Inc.
    Inventors: Donna Romero, Craig E. Masse, Shaughnessy Robinson, Jeremy Robert Greenwood, Geraldine C. Harriman
  • GAK modulators
    Patent number: 9518066
    Abstract: The present invention relates to a class of novel isothiazolo[4,3-b]pyridine derivatives and a method for their preparation, as well as to pharmaceutical compositions comprising one or more of said isothiazolo[4,3-b]pyridine derivatives and one or more pharmaceutically acceptable excipients. The present invention further relates to the use of said novel isothiazolo[4,3-b]pyridine derivatives as biologically active ingredients, more specifically as medicaments for the treatment of disorders and pathologic conditions such as, but not limited to, cell-proliferative and neurodegenerative diseases.
    Type: Grant
    Filed: July 4, 2014
    Date of Patent: December 13, 2016
    Assignee: Katholieke Universiteit Leuven, K.U. Leuven R&D
    Inventors: Piet Herdewijn, Steven De Jonghe, Sona Kovachova, Lei Chang, Michal Sala
  • Trifluoroborate mass spectrometric tags
    Patent number: 9518067
    Abstract: The invention provides compositions and methods for mass spectrometric (MS), organic synthesis, and applications of organo-trifluoroborate, for example, as mass tags for use in negative ion mode. When subject to MS fragmentation, organo-trifluoroborates preferentially undergo neutral losses of hydrogen fluoride (HF) or boron trifluoride (BF3) molecules, transferring the negative charge to the rest of the molecule. Such a fragmentation pattern is used to detect and quantitate analytes of interest after derivatization with organo-trifluoroborates.
    Type: Grant
    Filed: April 23, 2016
    Date of Patent: December 13, 2016
    Assignee: CellMosaic, Inc.
    Inventor: Yumei Huang
  • Compounds containing hydrido-tricyano-borate anions
    Patent number: 9518068
    Abstract: The present invention relates to compounds containing hydrido-tricyano-borate anions, their preparation and their use, in particular as part of electrolyte formulations for electrochemical or optoelectronic devices.
    Type: Grant
    Filed: May 23, 2012
    Date of Patent: December 13, 2016
    Assignee: MERCK PATENT GMBH
    Inventors: Nikolai (Mykola) Ignatyev, Michael Schulte, Kentaro Kawata, Tomohisa Goto, Eduard Bernhardt, Vera Bernhardt-Pitchougina, Helge Willner
  • Catalytic method for obtaining substituted (triorganosilyl)alkynes and their derivatives
    Patent number: 9518069
    Abstract: New (triorganosilyl)alkynes and their derivatives having general formula R1—C?C—Z are provided along with methods for the preparation of (triorganosilyl)alkynes and their derivatives having the general formula R1—C?C—Z. The methods may include silylative coupling of terminal alkynes with halogenotriorganosilanes in the presence of an iridium catalyst and a tertiary amine.
    Type: Grant
    Filed: July 10, 2015
    Date of Patent: December 13, 2016
    Assignee: ADAM MICKIEWICZ UNIVERSITY
    Inventors: Ireneusz Kownacki, Bogdan Marciniec, Beata Dudziec, Agnieszka Kownacka, Mariusz Majchrzak, Mateusz Szulc, Bartosz Orwat
  • Use of cyclohexa-2,5-dien-1-yl-silanes as precursors for gaseous hydrosilanes
    Patent number: 9518070
    Abstract: A method of making hydrosilanes having a formula R1R2R3SiH by reacting a compound having formula I: in solution using a strong Lewis acid. This way, e.g., alkenes or carbonyl compounds can be hydrosilylated in good yields using the cyclohexa-2,5-dien-1-yl-silanes of general formula I as transfer hydrosilylating agents in the presence of a strong Lewis acid as catalyst with concomitant formation of an arene solvent.
    Type: Grant
    Filed: September 4, 2014
    Date of Patent: December 13, 2016
    Assignee: TECHNISCHE UNIVERSITAET BERLIN
    Inventors: Martin Oestreich, Antoine Simonneau
  • Hydrosilylation method
    Patent number: 9518071
    Abstract: A method (P) for hydrosilylating at least one compound (C), including at least one unsaturation in the presence of an organosilicon compound (O) including at least one hydrogen atom per molecule bonded directly to a silicon atom, and of a catalytic hydrosilylation system including a structured porous material (A) including pores and an inorganic structure consisting of silicon oxide walls, in which metal nanoparticles are contained.
    Type: Grant
    Filed: December 20, 2013
    Date of Patent: December 13, 2016
    Assignees: BLUESTAR SILICONES FRANCE SAS, UNIVERSITE CLAUDE BERNARD LYON 1
    Inventors: Chloe Thieuleux, Reine Sayah El Rayes, Marie-Line Zanota, Valerie Meille, Richard Vivier, Sebastien Marrot
  • Ester-functional silanes and the preparation and use thereof; and use of iminium compounds as phase transfer catalysts
    Patent number: 9518072
    Abstract: A method for producing a reaction product comprising an ester-functional silane, the method comprising: i) reacting a composition comprising: a) a haloorganosilane, b) a metal salt of a carboxy-functional compound, c) a phase transfer catalyst comprising a bicyclic amidine, an iminium compound, or a mixture thereof, provided that the iminium compound is not an acyclic guanidinium compound or pyridinium compound, and d) a co-catalyst, provided that the co-catalyst is optional when the phase transfer catalyst comprises the iminium compound.
    Type: Grant
    Filed: November 14, 2012
    Date of Patent: December 13, 2016
    Assignee: Dow Corning Corporation
    Inventors: Michael Wolfgang Backer, John Michael Gohndrone, Don Lee Kleyer, Xiaobing Zhou
  • Siloxane compound and process for producing the same
    Patent number: 9518073
    Abstract: A siloxane compound comprises a plurality of siloxane repeating units and at least a portion of the siloxane repeating units are cyclosiloxane repeating units conforming to a specified structure. A process for producing such siloxane compounds is also provided. A process and kit for producing a cross-linked silicone polymer using the described siloxane compounds is also provided. A light emitting diode (LED) comprises an encapsulant, and the encapsulant comprises a cross-linked silicone polymer produced from the described siloxane compounds.
    Type: Grant
    Filed: April 3, 2014
    Date of Patent: December 13, 2016
    Assignee: Milliken & Company
    Inventors: Yuzhou Liu, Keith A. Keller, Michael E. Wilson
  • Method for producing fluorine-containing substituted compound and fluorine-containing substituted compound
    Patent number: 9518074
    Abstract: A method for producing a fluorine-containing substituted compound, the method including: introducing an organofluorine compound and an organolithium compound into a microreactor provided with a flow path capable of mixing a plurality of liquids, to thereby obtain a reaction product; and introducing, into the microreactor, the reaction product and an electrophile exhibiting electrophilic effect on the reaction product, to thereby obtain a fluorine-containing substituted compound.
    Type: Grant
    Filed: December 31, 2015
    Date of Patent: December 13, 2016
    Assignees: Kyoto University, Taiyo Nippon Sanso Corporation
    Inventors: Junichi Yoshida, Aiichiro Nagaki
  • Group 5 cyclopentadienyl transition metal-containing precursors for deposition of group 5 transition metal-containing films
    Patent number: 9518075
    Abstract: Transition metal-containing precursors are disclosed. Also disclosed are methods of synthesizing and using the disclosed precursors to deposit transition metal-containing films on one or more substrates via a vapor deposition process.
    Type: Grant
    Filed: December 13, 2013
    Date of Patent: December 13, 2016
    Assignee: L'Air Liquide, Société Anonyme pour l'Etude et l'Exploitation des Procédés Georges Claude
    Inventors: Clément Lansalot-Matras, Wontae Noh
  • Apparatus and process for preparing reactive lignin with high yield from plant biomass for production of fuels and chemicals
    Patent number: 9518076
    Abstract: Provided are methods for aqueous isolation of depolymerized lignin in high yield from a lignin-containing biomass composition, comprising positioning a lignin-containing biomass composition into a flowthrough thermal reactor chamber to provide for passage of an aqueous fluid therethrough, contacting the lignin biomass composition with the aqueous fluid under elevated temperature conditions sufficient to provide for lignin release and depolymerization, flowing the aqueous fluid through the reactor chamber under the elevated temperature conditions, to provide an output aqueous fluid comprising released depolymerized lignin, and collecting the depolymerized lignin.
    Type: Grant
    Filed: April 30, 2013
    Date of Patent: December 13, 2016
    Assignee: Washington State University
    Inventors: Bin Yang, Dhrubojyoti Dey Laskar
  • Electrochemical synthesis of chloro-chitosan
    Patent number: 9518077
    Abstract: The present disclosure provides methods for producing chitosan derivatives and the derivatives formed by these methods. The processes of the present disclosure utilize electrochemical methods to functionalize and/or modify amine and/or hydroxyl groups present on chitosan, to form new derivatives. In embodiments, a chloro-chitosan derivative may be prepared. The altered cationic affinity of these derivatives make them excellent candidates for biomedical applications, including pharmaceuticals, as well as food applications.
    Type: Grant
    Filed: February 1, 2013
    Date of Patent: December 13, 2016
    Assignee: The Research Foundation for the State University of New York
    Inventors: Gary P. Halada, Prashant Kumar Jha