Patents Issued in September 4, 2018
  • Process for producing long chain amino acids and dibasic acids
    Patent number: 10065921
    Abstract: There is disclosed a process for the production of long chain amino acid and long chain dibasic acid, comprising: (1) reacting long chain keto fatty acid with hydroxylamine or subjecting keto fatty acid to an ammoximation reaction to yield an oxime fatty acid; (2) subjecting the oxime fatty acid to the Beckmann rearrangement to yield a mixture of two amide fatty acids; (3) hydrolyzing the mixed amide fatty acids to produce long chain amino acid, long chain dibasic acid, short chain alkylamine, and alkanoic acid.
    Type: Grant
    Filed: July 7, 2017
    Date of Patent: September 4, 2018
    Assignee: VITAWORKS IP, LLC
    Inventor: Songzhou Hu
  • Solabegron zwitterion and uses thereof
    Patent number: 10065922
    Abstract: This application relates to solabegron zwitterion useful for the treatment of lower urinary tract symptoms such as, for example, overactive bladder and prostate disorders. Additionally, this application relates to pharmaceutical compositions and methods of treatment utilizing the solabegron zwitterion for treating lower urinary tract symptoms. This application also relates to methods of preparing solabegron hydrochloride from the solabegron zwitterion.
    Type: Grant
    Filed: October 24, 2016
    Date of Patent: September 4, 2018
    Assignee: Velicept Therapeutics, Inc.
    Inventors: Raymond E. Stevens, Dalian Zhao, Bingidimi Itute Mobele
  • Thickening stabilizer and thickening stabilization composition using same
    Patent number: 10065923
    Abstract: A compound that thickens or gels a fluid organic substance to a desired viscosity or homogeneously stabilizes a composition containing a fluid organic substance, a thickening/stabilizing agent containing the compound, a thickened/stabilized composition containing the thickening/stabilizing agent and a fluid organic substance, and a method for producing a thickened/stabilized composition. The compound is represented by the following formula (1): In the formula, R1 and R2 are different from each other and represent an aliphatic hydrocarbon group having not less than 4 carbon atoms, and n represents an integer of 1 to 3. The thickening/stabilizing agent of the present invention contains the compound.
    Type: Grant
    Filed: May 1, 2015
    Date of Patent: September 4, 2018
    Assignees: DAICEL CORPORATION, YAMAGUCHI UNIVERSITY
    Inventors: Yuichi Sakanishi, Takashi Saeki, Mami Itoh
  • Preparation and biological evaluation of viridicatumtoxin analogs
    Patent number: 10065924
    Abstract: In one aspect, the present invention provides novel derivatives of viridicatumtoxin of the formula wherein the variables are as defined herein. The application also provides compositions, methods of treatment, and methods of synthesis thereof.
    Type: Grant
    Filed: July 22, 2015
    Date of Patent: September 4, 2018
    Assignee: WILLIAM MARSH RICE UNIVERSITY
    Inventors: Kyriacos C Nicolaou, Christopher R. H. Hale, Christian Nilewski, Heraklidia Ioannidou, Abdellatif El Marrouni
  • Carbodiimides, method for the production and use thereof
    Patent number: 10065925
    Abstract: The invention relates to novel carbodiimides having terminal urea and/or urethane groups, to processes for the production thereof and to the use thereof as a stabilizer in ester-based polymers especially in films for protection from hydrolytic degradation.
    Type: Grant
    Filed: November 3, 2015
    Date of Patent: September 4, 2018
    Assignee: LANXESS Deutschland GmbH
    Inventors: Wilhelm Laufer, Volker Wenzel
  • Use of substituted dihydrooxindolylsulfonamides, or the salts thereof, for increasing the stress tolerance of plants
    Patent number: 10065926
    Abstract: The invention relates to the use of substituted dihydrooxindolylsulfonamides or salts thereof of the formula (I) where the radicals in the general formula (I) correspond to the definitions given in the description, for enhancing stress tolerance in plants to abiotic stress, and/or for increasing plant yield.
    Type: Grant
    Filed: October 2, 2014
    Date of Patent: September 4, 2018
    Assignee: BAYER CROPSCIENCE AKTIENGESELLSCHAFT
    Inventors: Jens Frackenpohl, Guido Bojack, Hendrik Helmke, Stefan Lehr, Thomas Mueller, Lothar Willms, Jan Dittgen, Dirk Schmutzler, Udo Bickers, Harry Strek, Rachel Baltz
  • ?-ketoacylic isoniazid compounds, process for producing said compounds, use of the compounds in the treatment of tuberculosis
    Patent number: 10065927
    Abstract: The instant invention relates to compounds of formula I wherein: R is selected from H, Me or Cl, and R? is selected from: H, NH2, NHCOCH3 NHCOCF3 or NHCOCH2Cl. The invention further provides a process for obtaining the compounds of formula I and their use.
    Type: Grant
    Filed: January 14, 2016
    Date of Patent: September 4, 2018
    Assignee: FUNDACÃO OSWALDO CRUZ (FIOCRUZ)
    Inventors: Núbia Boechat, Frederico Silva Castelo Branco
  • Quinolinone compound and use thereof
    Patent number: 10065928
    Abstract: Provided herein are a quinolinone compound, pharmaceutical composition thereof, and use of the compound or the pharmaceutical composition in drug preparation, the drug being used to prevent, manage, treat or relieve diseases related to HIF and/or EPO of a patient, including anemia, vascular disease, myocardial ischemia, dysmetabolism, or for wound healing.
    Type: Grant
    Filed: September 1, 2015
    Date of Patent: September 4, 2018
    Assignee: SUNSHINE LAKE PHARMA CO., LTD.
    Inventors: Yinglin Zuo, Xiaojun Wang, Yingjun Zhang, Liang Wen, Shoutao Wu, Xiaofeng Yuan
  • Pyrazole compounds and their use as T-type calcium channel blockers
    Patent number: 10065929
    Abstract: The invention relates to compounds of formula (I) wherein X, Y, R1, R2, (R4)n, and (R5)m are as defined in the description, and to pharmaceutically acceptable salts of such compounds. These compounds are useful as calcium T-channel blockers.
    Type: Grant
    Filed: December 19, 2017
    Date of Patent: September 4, 2018
    Assignee: IDORSIA PHARMACEUTICALS LTD
    Inventors: Romain Siegrist, Bibia Heidmann, Simon Stamm, John Gatfield, Olivier Bezencon
  • Method for producing pyrimidine-1-ol compound, and intermediate thereof
    Patent number: 10065930
    Abstract: There are provided a method for producing 2,4-disubstituted pyrimidine-5-ol, and particularly, 2,4-dimethylpyrimidine-5-ol and an intermediate thereof used in industrial production. The production method according to the present invention includes a step of producing 2,4-disubstituted pyrimidine-5-ol according to a hydrolysis reaction of a 2,4-disubstituted-5-(4-(nitrophenyl)oxy)pyrimidine compound and is suitable for industrial production since an inexpensive and easily available starting material can be used, regioselectivity of a substituent group is easily controlled, impurities are easily controlled, and 2,4-disubstituted pyrimidine-5-ol can be produced without using reagents and intermediates causing health problems, risks and the like.
    Type: Grant
    Filed: August 3, 2015
    Date of Patent: September 4, 2018
    Assignee: Eisai R&D Management Co., Ltd.
    Inventor: Yuzo Watanabe
  • Quinazolin crotyl compound dimaleate crystals and preparation methods and uses thereof
    Patent number: 10065931
    Abstract: Disclosed are crystal forms K, E, F and G of the dimaleate of the compound as shown in formula I, and preparation methods and uses thereof. The crystal forms K, E, F and G have superior storage stability and solubility, so that they are more suitable for being used as the drug substance for drug product preparations.
    Type: Grant
    Filed: May 3, 2016
    Date of Patent: September 4, 2018
    Assignee: HANGZHOU HUADONG MEDICINE GROUP BIOPHARMACEUTICAL CO. LTD.
    Inventors: Yubin Lv, Jianming Yin, Xuehui Huang, Bangliang Li
  • Certain chemical entities, compositions, and methods
    Patent number: 10065932
    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: October 16, 2017
    Date of Patent: September 4, 2018
    Assignee: NeuPharma, Inc.
    Inventors: Xiangping Qian, Yong-Liang Zhu
  • Method for preparing gadobutrol
    Patent number: 10065933
    Abstract: The present disclosure relates to a novel method for preparing high-purity gadobutrol. The present disclosure can be easily applied to a large scale production because purity of intermediate can be managed via simple and mild process and accordingly, high-purity or ultra high-purity gadobutrol that has higher purity than previous gadobutrol can be prepared in high yield therethrough.
    Type: Grant
    Filed: December 28, 2015
    Date of Patent: September 4, 2018
    Assignee: ST PHARM CO., LTD.
    Inventors: Geun Jho Lim, Sun Ki Chang, Chang Ho Byeon, Hoe Jin Yoon, Moon Soo Kim
  • Substituted urea derivatives and pharmaceutical uses thereof
    Patent number: 10065934
    Abstract: Provided herein are novel substituted urea derivatives, and pharmaceutical compositions thereof. Also provided herein are uses of the compounds or pharmaceutical compositions thereof for preventing, managing, treating or lessening a proliferative disease, and modulating the activity of protein kinase.
    Type: Grant
    Filed: July 16, 2015
    Date of Patent: September 4, 2018
    Assignee: SUNSHINE LAKE PHARMA CO., LTD.
    Inventors: Changchung Cheng, Yingjun Zhang, Bing Liu, Bohua Long, Yu Chen, Zhixin Cheng
  • Derivatives of (Z)-1,2-diphenylethene
    Patent number: 10065935
    Abstract: The present invention relates to the new chemical compounds containing (Z)-1,2-diphenylethene moiety in the structures, particularly the new derivatives of cis-stilbene, the new derivatives of 4,5-diphenyl-1,3-oxazole, the new derivatives of 1-methyl-4,5-diphenyl-1H-imidazole and pharmaceutically acceptable salts thereof. The invention relates also to the application of aforementioned compounds as a microtubule-interfering agents (MIAs). The new derivatives, because of their potential antimitotic and antiangio-genic activity, can be used as ingredients in the preparations used in the treatment of cancer.
    Type: Grant
    Filed: March 28, 2013
    Date of Patent: September 4, 2018
    Assignee: Uniwersytet Medyczny IM. Karola Marcinkowskiego
    Inventors: Tomasz Stefański, Jakub Różański, Renata Mikstacka, Stanislaw Sobiak
  • Synthesis of sulfur containing ammonium and phosphonium borates
    Patent number: 10065936
    Abstract: The present invention relates to the preparation of sulfur containing ammonium and phosphonium borates KA, wherein K is a compound of formula (I), and A is an anion of formulae (IIa) or (IIb) by bringing into contact ammonium borates with sulfur containing ammonium or phosphonium halides or sulfonates.
    Type: Grant
    Filed: February 5, 2016
    Date of Patent: September 4, 2018
    Assignee: Gotion Inc.
    Inventors: Nicole Holub, Juergen Herbel
  • FLT3 receptor antagonists
    Patent number: 10065937
    Abstract: The invention pertains to novel FLT3 receptor antagonists of general formula (1). The compounds are useful for the treatment or the prevention of pain disorders, cancer and autoimmune diseases.
    Type: Grant
    Filed: July 30, 2015
    Date of Patent: September 4, 2018
    Assignees: INSERM (INSTITUT NATIONAL DE LA SANTE ET DE LA RECHERCHE MEDICALE), UNIVERSITE DE MONTPELLIER, CENTRE NATIONAL DE LA RECHERCHE SCIENTIFIQUE (CNRS), UNIVERSITE DE STRASBOURG
    Inventors: Jean Valmier, Jean-Philippe Leyris, Didier Rognan, Martine Schmitt
  • Method for producing hydride using unsaturated compound having carbon number of 4 as raw material
    Patent number: 10065938
    Abstract: The present invention relates to a method for producing a hydride having a carbon number of 4, comprising contacting, in liquid phase, an unsaturated compound having a carbon number of 4 as a raw material with a solid catalyst obtained by loading a metal element belonging to Groups 9 to 11 of the long periodic table on a support, thereby performing hydrogenation to produce a corresponding hydride having a carbon number of 4, wherein hydrogenation is performed in the presence of, as a solvent, a 1,4-butanediol having a nitrogen component concentration of 1 ppm by weight to 1 wt % in terms of nitrogen atom.
    Type: Grant
    Filed: June 23, 2016
    Date of Patent: September 4, 2018
    Assignee: MITSUBISHI CHEMICAL CORPORATION
    Inventors: Yusuke Izawa, Masaru Utsunomiya, Norikazu Konishi, Kouta Tanaka
  • Chromene derivatives and their analogs as Wnt pathway antagonists
    Patent number: 10065939
    Abstract: Compounds of formula (IIc); wherein X3 and X4 independently from each other are N or CR8 wherein R8 may be same or different; Y1, Y2, Y3 and Y4 independently from each other are N or CR9 wherein R9 may be same or different and wherein up to 3 of the group Y1, Y2, Y3 and Y4 may be N; their solvates, hydrates, and pharmaceutically acceptable salts, their use for modulating the Wnt signalling pathway activity and their use as a medicament, preferably for the treatment of cancer.
    Type: Grant
    Filed: May 19, 2016
    Date of Patent: September 4, 2018
    Assignees: Deutsches Krebsforschungszentrum, Ruprecht-Karls-Universität Heidelberg
    Inventors: Michael Boutros, Rajendra-Prasad Maskey, Corinna Koch, Florian Fuchs, Sandra Steinbrink, Daniel Gilbert
  • Episulfide compound and optical material composition containing same
    Patent number: 10065940
    Abstract: According to the present invention, it is possible to provide an optical material composition that contains an episulfide compound represented by formula (1) and an episulfide compound represented by formula (2). According to this optical material composition, it is possible to suppress a reduction in the yield rate caused by molding defects, and possible to obtain an optical material having excellent dyeability. (In formula (1), m and p are each an integer between 0 and 4, and n and q are each an integer between 0 and 2.) (In formula (2), m is an integer between 0 and 4 and n is an integer between 0 and 2).
    Type: Grant
    Filed: March 1, 2016
    Date of Patent: September 4, 2018
    Assignee: MITSUBISHI GAS CHEMICAL COMPANY, INC.
    Inventors: Yoshihiko Nishimori, Teruo Kamura, Hiroshi Horikoshi
  • Aminotriazine derivative and pharmaceutical composition comprising the same
    Patent number: 10065941
    Abstract: The present invention provides novel compounds having a P2X3 and/or P2X2/3 receptor antagonistic activity. A compound of Formula (I): wherein Ra and Rb, and Rd and Re are taken together to form oxo or the like; R4a and R4b are hydrogen or the like; n is 1 or the like; R2 is aryl or the like; s and s? is 0 or the like; R9 and R9? are halogen or the like; R20a and R20b are hydrogen, alkyl or the like; u is 1 to 4; R13 is hydrogen or the like, or its pharmaceutically acceptable salt.
    Type: Grant
    Filed: June 29, 2017
    Date of Patent: September 4, 2018
    Assignee: SHIONOGI & CO., LTD.
    Inventor: Hiroyuki Kai
  • Crystalline (2S)-3-[(3S,4S)-3-[(1R)-1-hydroxyethyl]-4-(4-methoxy-3-{[1-(5-methylpyridin-2-yl)azetidin-3-yl]oxy}phenyl)-3-methylpyrrolidin-1-yl]-3-oxopropane-1,2-diol
    Patent number: 10065942
    Abstract: The invention provides crystalline (2S)-3-[(3S,4S)-3-[(1R)-1-hydroxyethyl]-4-(4-methoxy-3-{[1-(5-methylpyridin-2-yl)azetidin-3-yl]oxy}phenyl)-3-methylpyrrolidin-1-yl]-3-oxopropane-1,2-diol, and pharmaceutical compositions thereof. The invention further provides methods of using this compound to treat overactive bladder.
    Type: Grant
    Filed: August 28, 2015
    Date of Patent: September 4, 2018
    Assignee: Eli Lilly and Company
    Inventors: Ping Huang, Seth Dietrich Ribe
  • Pyrrolidine derivatives as angiotensin II type 2 antagonists
    Patent number: 10065943
    Abstract: The invention relates to heterocyclic angiotensin II type 2 (AT2) receptor antagonists of formula (I), and pharmaceutically acceptable salts thereof, ((I) in which all of the variables are as defined in the specification, pharmaceutical compositions thereof, combinations thereof, and their use as medicaments, particularly for the treatment of neuropathic or inflammatory pain.
    Type: Grant
    Filed: January 12, 2016
    Date of Patent: September 4, 2018
    Assignee: Novartis AG
    Inventors: Jane Brown, Thomas David McCarthy, Alan Naylor, John Paul Watts
  • Administration regime for nitrocatechols
    Patent number: 10065944
    Abstract: A compound of formula (I) where R1, R2, X, Y, n, m, R3, R4, R5, R6 and R7 are as defined herein, for use in the prophylaxis or treatment of a central and peripheral nervous system disorder, wherein the compound of formula (I) is administered prior to sleep, before bedtime or at bedtime.
    Type: Grant
    Filed: August 9, 2013
    Date of Patent: September 4, 2018
    Assignee: BIAL-PORTELA & CA, S.A.
    Inventors: Patricio Manuel Vieira Araujo Soares Da Silva, Teresa Lucia Silva Pereira Nunes, Lyndon Christopher Wright, Pedro Nuno Leal Palma, David Alexander Learmonth
  • Isoquinoline derivatives as MGAT2 inhibitors
    Patent number: 10065945
    Abstract: The compounds of Formula I act as MGAT2 inhibitors and can be useful in preventing, treating or acting as a remedial agent for hyperlipidemia, diabetes mellitus and obesity.
    Type: Grant
    Filed: January 20, 2015
    Date of Patent: September 4, 2018
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Richard Berger, Timothy A. Blizzard, Brian T. Campbell, Helen Y. Chen, John S. Debenham, Sunita V. Dewnani, Byron Dubois, Candido Gude, Zack Zhiqiang Guo, Bart Harper, Zhiyong Hu, Songnian Lin, Ping Liu, Ming Wang, Feroze Ujjainwalla, Jiayi Xu, Libo Xu, Rui Zhang
  • Benzazole compounds and methods for making and using the compounds
    Patent number: 10065946
    Abstract: Disclosed are novel benzazole compounds and compositions comprising the compounds. The compounds are useful as kinase inhibitors including interleukin receptor associated kinases (IRAK) inhibitors. Also disclosed are methods of making and using the compounds and compositions. The disclosed compounds and/or compositions may be used to treat or prevent an IRAK-associated disease or condition.
    Type: Grant
    Filed: August 2, 2016
    Date of Patent: September 4, 2018
    Assignee: Rigel Pharmaceuticals, Inc.
    Inventors: Rose Yen, Yan Chen, Rajinder Singh, Vanessa Taylor
  • Forms of R)-3-(4-(2-(2-methyltetrazol-5-yl)pyridin-5-yl)-3-fluorophenyl)-5-hydroxymethyl oxazolidin-2-one dihydrogen phosphate
    Patent number: 10065947
    Abstract: A crystalline form of crystalline (R)-3-(4-(2-(2-methyltetrazol-5-yl)-pyridin-5-yl)-3-fluorophenyl)-5-hydroxymethyl oxazolidin-2-one dihydrogen phosphate, methods of making the crystalline form and pharmaceutical compositions comprising the crystalline form are useful antibiotics. Further, the derivatives of the present invention may exert potent antibacterial activity versus various human and animal pathogens, including Gram-positive bacteria such as Staphylococi, Enterococci and Streptococi, anaerobic microorganisms such as Bacteroides and Clostridia, and acid-resistant microorganisms such as Mycobacterium tuberculosis and Mycobacterium avium. Accordingly, the compositions comprising the crystalline form may be used in antibiotics.
    Type: Grant
    Filed: May 3, 2018
    Date of Patent: September 4, 2018
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Katharina Reichenbacher, Robert J. Duguid, Jacqueline A. Ware, Douglas Phillipson
  • Histone deacetylase inhibitors and compositions and methods of use thereof
    Patent number: 10065948
    Abstract: Provided are certain histone deacetylase (HDAC) inhibitors of Formula I, or pharmaceutically acceptable salts thereof, compositions thereof, and methods of their use. The condition or disorder mediated by HDAC comprises a neurodegenerative pathology. Accordingly, also provided is a method of treating a neurodegenerative pathology mediated by HDAC in a subject in need of such a treatment, comprising administering to the subject a therapeutically effective amount of at least one compound, or pharmaceutically acceptable salt thereof, described herein.
    Type: Grant
    Filed: June 1, 2015
    Date of Patent: September 4, 2018
    Assignee: CHDI Foundation, Inc.
    Inventors: Celia Dominguez, Ignacio Muñoz-Sanjuán, Roland W. Bürli, Christopher A. Luckhurst, Daniel R. Allen, Gilles Raphy, Perla Breccia, Alan F. Haughan, Grant Wishart, Samantha J. Hughes, Rebecca E. Jarvis, Huw D. Vater, Stephen D. Penrose, Michael Wall, Andrew J. Stott, Elizabeth A. Saville-Stones
  • Method of preparing glucosylceramide synthase inhibitors
    Patent number: 10065949
    Abstract: The invention relates to a method of preparing inhibitors of glucosylceramide synthase (GCS) useful 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: May 12, 2017
    Date of Patent: September 4, 2018
    Assignee: GENZYME CORPORATION
    Inventors: Craig S. Siegel, Rayomand Gimi, Michael Reardon, Jin Zhao
  • Substituted thiazoles as HIV integrase inhibitors
    Patent number: 10065950
    Abstract: [Problem] Provided is a novel 1,3,4,8-tetrahydro-2H-pyrido[1,2-a]pyrazine derivative or a pharmaceutically acceptable salt thereof, or a solvate thereof, which is useful as an anti-HIV agent. [Solving Means] The present invention provides a compound represented by the following formula [I] wherein each symbol is as defined in the specification, or a pharmaceutically acceptable salt thereof, or a solvate thereof.
    Type: Grant
    Filed: February 25, 2011
    Date of Patent: September 4, 2018
    Assignee: Japan Tobacco Inc.
    Inventors: Susumu Miyazaki, Yuki Bessho, Kaoru Adachi, Seiji Kawashita, Hirotaka Isoshima, Kengo Oshita, Shunichi Fukuda
  • Small molecule transcription modulators of bromodomains
    Patent number: 10065951
    Abstract: This disclosure relates generally to compounds and compositions comprising one or more indole analogs. These compounds are useful for treating diseases associated with NF-kB and p53 activity, such as cancer and inflammatory diseases.
    Type: Grant
    Filed: May 29, 2015
    Date of Patent: September 4, 2018
    Assignee: Icahn School of Medicine at Mount Sinai
    Inventors: Ming-MIng Zhou, Guillermo Gerona-Navarro, Yoel Rodriguez-Fernandez, Patrizia Casaccia
  • Valbenazine salts and polymorphs thereof
    Patent number: 10065952
    Abstract: Provided herein are salts of (S)-2-amino-3-methyl-butyric acid (2R,3R,11bR)-3-isobutyl-9,10-dimethoxy-1,3,4,6,7,11b-hexahydro-2H-pyrido[2,1-a]isoquinolin-2-yl ester in amorphous and crystalline forms, and processes of preparation, and pharmaceutical compositions thereof. Also provided are methods of their use for treating, preventing, or ameliorating one or more symptoms of neurological disorders and diseases including hyperkinetic movement disorders or diseases.
    Type: Grant
    Filed: October 28, 2016
    Date of Patent: September 4, 2018
    Assignee: Neurocrine Biosciences, Inc.
    Inventors: Kevin McGee, Scott Zook, Andrew Carr, Thierry Bonnaud
  • Imidazo[1,2-A]pyridine derivatives for use as inhibitors of human immunodeficiency virus replication
    Patent number: 10065953
    Abstract: The disclosure generally relates to compounds of formula I, including compositions and methods for treating human immunodeficiency virus (HIV) infection. The disclosure provides novel inhibitors of HIV, pharmaceutical compositions containing such compounds, and methods for using these compounds in the treatment of HIV infection.
    Type: Grant
    Filed: August 25, 2015
    Date of Patent: September 4, 2018
    Assignee: ViiV HEALTHCARE UK (NO.5) LIMITED
    Inventors: Timothy P. Connolly, Kyle J. Eastman, B. Narasimhulu Naidu, Kevin Peese
  • Substituted imidazo[4,5-c]pyridines as SSAO inhibitors
    Patent number: 10065954
    Abstract: Specific compounds of formula (Ia): and pharmaceutically acceptable salts thereof. Pharmaceutical compositions of the specific compounds of formula (Ia) and pharmaceutically acceptable salts thereof. A method for inhibiting tumor growth in a subject that includes administering to the subject an effective amount of a compound selected from the specific compounds of formula (Ia) and pharmaceutically acceptable salts thereof. A method for modulating semicarbazide-sensitive amine oxidase activity in a subject that includes administering to the subject an effective amount of a compound selected from the specific compounds of formula (Ia) and pharmaceutically acceptable salts thereof.
    Type: Grant
    Filed: September 17, 2015
    Date of Patent: September 4, 2018
    Assignee: PROXIMAGEN LIMITED
    Inventors: Max Espensen, Lee Patient, Edward Savory
  • Dihydroindolizinone derivative
    Patent number: 10065955
    Abstract: A compound represented by general formula (I) (wherein all symbols are as defined in the description) or a salt, solvate, N-oxide form or prodrug thereof is a potent FXIa inhibitor, has excellent oral absorption properties and kinetics in blood, can exert a potent anti-coagulation activity over a long period of time after being administered orally, and has a discrepancy between the anti-coagulation activity thereof and the CYP-inhibiting activity thereof. Therefore, the compound or the salt, solvate, N-oxide form or prodrug thereof can be used as an efficient prophylactic and/or therapeutic agent for vascular occlusive diseases.
    Type: Grant
    Filed: December 9, 2015
    Date of Patent: September 4, 2018
    Assignee: ONO PHARMACEUTICAL CO., LTD.
    Inventors: Motoyuki Tanaka, Takashi Kondo, Yasuo Hirooka, Taihei Nishiyama, Atsushi Hiramatsu, Tomoyuki Koda, Sho Kouyama
  • Ethynyl derivatives
    Patent number: 10065956
    Abstract: The present invention relates to compounds that may be used for the treatment of Parkinson's disease, anxiety, emesis, obsessive compulsive disorder, autism, neuroprotection, cancer, depression and diabetes type 2. Compounds of formula I are representative, where substituents are defined herein: or a pharmaceutically acceptable salt or acid addition salt, a racemic mixture, or its corresponding enantiomer and/or optical isomer and/or stereoisomer thereof.
    Type: Grant
    Filed: September 18, 2017
    Date of Patent: September 4, 2018
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Barbara Biemans, Wolfgang Guba, Georg Jaeschke, Jean-Marc Plancher, Antonio Ricci, Daniel Rueher, Eric Vieira, Fionn O'Hara
  • Beta-lactamase inhibitors
    Patent number: 10065957
    Abstract: This invention pertains generally to compounds of Formula (A), as further described herein, which act as beta-lactamase inhibitors, and salts, crystalline forms and formulations thereof. In certain aspects, the invention pertains to methods of using such compounds in combination with a beta-lactam antibiotic to treat infections caused by Gram-negative bacteria, including drug-resistant strains.
    Type: Grant
    Filed: September 28, 2017
    Date of Patent: September 4, 2018
    Assignee: Novartis AG
    Inventors: Anthony Casarez, Markus Furegati, Guido Koch, Xiaodong Lin, Flavio Ossola, Folkert Reck, Robert Lowell Simmons, Qingming Zhu
  • Methods and compounds for treating Paramyxoviridae virus infections
    Patent number: 10065958
    Abstract: Provided are methods for treating Paramyxoviridae virus infections by administering ribosides, riboside phosphates and prodrugs thereof, of Formula I: wherein the 1? position of the nucleoside sugar is substituted. The compounds, compositions, and methods provided are particularly useful for the treatment of Human parainfluenza and Human respiratory syncytial virus infections.
    Type: Grant
    Filed: February 4, 2015
    Date of Patent: September 4, 2018
    Assignee: GILEAD SCIENCES, INC.
    Inventors: Richard L. Mackman, Jay P. Parrish, Adrian S. Ray, Dorothy Agnes Theodore
  • Electronic device
    Patent number: 10065959
    Abstract: The present application relates to an electronic device comprising a heteroaromatic compound of a formula (I) as functional material, in particular as electron-transport material and as matrix material for emitter compounds.
    Type: Grant
    Filed: November 4, 2013
    Date of Patent: September 4, 2018
    Assignee: Merck Patent GmbH
    Inventors: Junyou Pan, Amir Hossain Parham, Rene Peter Scheurich, Thomas Rudolph
  • NK-3 receptor selective antagonist compounds, pharmaceutical composition and methods for use in NK-3 receptors mediated disorders
    Patent number: 10065960
    Abstract: The present invention is directed to novel compounds of formula I and their use as therapeutic compounds.
    Type: Grant
    Filed: July 14, 2015
    Date of Patent: September 4, 2018
    Assignee: Ogeda SA
    Inventors: Hamid R. Hoveyda, Marie-Odile Roy, Graeme L. Fraser, Guillaume Dutheuil
  • Chiral N-acyl-5,6,7,(8-substituted)-tetrahydro-[1,2,4]triazolo[4,3-a]pyrazines as selective NK-3 receptor antagonists, pharmaceutical composition, methods for use in NK-3 receptor mediated disorders and chiral synthesis thereof
    Patent number: 10065961
    Abstract: The present invention relates to novel compounds of Formula I and their use in therapeutic treatments. The invention further relates to a novel chiral synthesis of 5,6,7,(8-substituted)-tetrahydro-[1,2,4]triazolo[4,3-a]pyrazines using N-sp3 protective groups. The invention also provides intermediates for use in the synthesis of compounds of Formula I.
    Type: Grant
    Filed: September 8, 2016
    Date of Patent: September 4, 2018
    Assignee: Ogeda SA.
    Inventors: Hamid R. Hoveyda, Guillaume Dutheuil, Graeme L. Fraser, Marie-Odile Roy, Mohamed E. Bousmaqui, Frederic Batt
  • Amino pryan ring derivative and composition and use thereof
    Patent number: 10065962
    Abstract: The present disclosure relates to an amino pyran ring derivative and a composition and use thereof, and in particular, to an amino pyran ring derivative represented by general formula (I) or a stereoisomer, a pharmaceutically acceptable salt or a prodrug thereof, a pharmaceutical composition comprising the derivative, and their medical use in the manufacture of a di-peptidyl peptidase IV (DPP-IV) inhibitor, in formula (I) the substituents are defined the same as those in the specification.
    Type: Grant
    Filed: May 14, 2015
    Date of Patent: September 4, 2018
    Assignee: SICHUAN HAISCO PHARMACEUTICAL CO., LTD
    Inventors: Chen Zhang, Jianmin Wang, Caihu Li, Yonggang Wei
  • Heterocyclic compounds as PI3K-? inhibitors
    Patent number: 10065963
    Abstract: This application relates to compounds of Formula (I): or pharmaceutically acceptable salts or stereoisomers thereof, which are inhibitors of PI3K-? which are useful for the treatment of disorders such as autoimmune diseases, cancer, cardiovascular diseases, and neurodegenerative diseases.
    Type: Grant
    Filed: November 4, 2016
    Date of Patent: September 4, 2018
    Assignee: Incyte Corporation
    Inventors: Artem Shvartsbart, Stacey Shepard, Andrew P. Combs, Lixin Shao, Nikoo Falahatpisheh, Ge Zou, Eddy W. Yue, Ravi Kumar Jalluri
  • Pyrimidine-5-carboxamides as spleen tyrosine kinase inhibitors
    Patent number: 10065964
    Abstract: The present invention relates to compounds of formula (Ia), (Ib) or (Ic): to pharmaceutically acceptable salts therefore and to pharmaceutically acceptable solvates of said compounds and salts, wherein the substituents are defined herein; to compositions containing such compounds; and to the uses of such compounds in the treatment of various diseases, particularly asthma, COPD, allergic rhinitis, chronic sinusitis, atopic dermatitis, psoriasis, rosacea, alopecia, allergic conjunctivitis and dry eye disease.
    Type: Grant
    Filed: December 13, 2016
    Date of Patent: September 4, 2018
    Assignee: Ziarco Pharma Ltd.
    Inventors: Gavin A. Whitlock, Paul Alan Glossop
  • Imidazo[1,2-B][1,2,4]triazine derivatives as antiparasitic agents
    Patent number: 10065965
    Abstract: A compound of Formula (I), or a salt thereof, compositions comprising the compound, processes for its preparation and its use in therapy, for example in the treatment of parasitic diseases such as Chagas disease, Human African Trypanosomiasis (HAT) and leishmaniasis, particularly visceral leishmaniasis (VL).
    Type: Grant
    Filed: May 26, 2016
    Date of Patent: September 4, 2018
    Assignees: GlaxoSmithKline Intellectual Property Development Limited, The University of Dundee
    Inventors: Stephen Brand, Elisabet Viayna Gaza, Ian Gilbert, Eun Jung Ko, Maria Marco Martin, Timothy James Miles, Lars Henrik Sandberg, Michael George Thomas
  • Substituted pyrido[2,3-d]pyrimidines as inhibitors of protein kinases
    Patent number: 10065966
    Abstract: The present invention provides compounds of formula I-h: useful as inhibitors of protein kinases, pharmaceutically acceptable compositions thereof, and methods of using the same.
    Type: Grant
    Filed: May 25, 2017
    Date of Patent: September 4, 2018
    Assignees: Celgene CAR LLC, Sanofi
    Inventors: Laura Akullian D'Agostino, Robert Tjin Tham Sjin, Deqiang Niu, Joseph John McDonald, Zhendong Zhu, Haibo Liu, Hormoz Mazdiyasni, Russell C. Petter, Juswinder Singh, Matthieu Barrague, Alexandre Gross, Mark Munson, Darren Harvey, Andrew Scholte, Sachin Maniar
  • Compounds that are ERK inhibitors
    Patent number: 10065967
    Abstract: Disclosed are the ERK inhibitors of formula (1): and the pharmaceutically acceptable salts thereof. Also disclosed are methods of treating cancer using the compounds of formula (I).
    Type: Grant
    Filed: July 21, 2017
    Date of Patent: September 4, 2018
    Assignee: Merck, Sharp & Dohme Corp.
    Inventors: Jongwon Lim, Xianhai Huang, Ronald D. Ferguson, Wei Zhou, Christopher W. Boyce, Phieng Siliphaivanh, David J. Witter, Milana M. Maletic, Joseph A. Kozlowski, Kevin J. Wilson
  • Crystalline forms of a bruton's tyrosine kinase inhibitor
    Patent number: 10065968
    Abstract: Described herein is the Bruton's tyrosine kinase (Btk) inhibitor 1-((R)-3-(4-amino-3-(4-phenoxyphenyl)-1H-pyrazolo[3,4-d]pyrimidin-1-yl)piperidin-1-yl)prop-2-en-1-one, including crystalline forms, solvates and pharmaceutically acceptable salts thereof. Also disclosed are pharmaceutical compositions that include the Btk inhibitor, as well as methods of using the Btk inhibitor, alone or in combination with other therapeutic agents, for the treatment of autoimmune diseases or conditions, heteroimmune diseases or conditions, cancer, including lymphoma, and inflammatory diseases or conditions.
    Type: Grant
    Filed: February 21, 2018
    Date of Patent: September 4, 2018
    Assignee: Pharmacyclics LLC
    Inventors: Norbert Purro, Mark S. Smyth, Erick Goldman, David D. Wirth
  • Method for producing carboxylic acid anhydride, method for producing carboxylic imide, and method for manufacturing electrophotographic photosensitive member
    Patent number: 10065969
    Abstract: A method for producing a carboxylic acid anhydride includes heating a composition containing a specific compound in a solvent to yield the carboxylic acid anhydride. The solvent is an aprotic polar solvent having a boiling point of 50° C. or more.
    Type: Grant
    Filed: June 22, 2016
    Date of Patent: September 4, 2018
    Assignee: CANON KABUSHIKI KAISHA
    Inventors: Kei Tagami, Akihito Saitoh, Kunihiko Sekido, Michiyo Sekiya, Masashi Nishi
  • Tricyclic PI3K inhibitor compounds and methods of use
    Patent number: 10065970
    Abstract: Described herein are tricyclic compounds with phosphoinositide-3 kinase (PI3K) modulation activity or function having the Formula I structure: or stereoisomers, tautomers, or pharmaceutically acceptable salts thereof, and with the substituents and structural features described herein. Also described are pharmaceutical compositions and medicaments that include the Formula I compounds, as well as methods of using such PI3K modulators, alone and in combination with other therapeutic agents, for treating diseases or conditions that are mediated or dependent upon PI3K dysregulation.
    Type: Grant
    Filed: September 7, 2016
    Date of Patent: September 4, 2018
    Assignee: Genentech, Inc.
    Inventors: Marie-Gabrielle Braun, Keira Garland, Emily Hanan, Hans Purkey, Steven T. Staben, Robert Andrew Heald, Jamie Knight, Calum Macleod, Aijun Lu, Guosheng Wu, Siew Kuen Yeap