Patents Issued in October 16, 2018
  • Synthesis routes for prostaglandins and prostaglandin intermediates using metathesis
    Patent number: 10100028
    Abstract: Methods of synthesizing prostaglandins, prostaglandin analogs and their synthetic intermediates are described. The methods can comprise metal-catalyzed metathesis reactions. Also provided are synthetic intermediates that can be used in the synthesis of the prostaglandins and prostaglandin analogs.
    Type: Grant
    Filed: September 30, 2014
    Date of Patent: October 16, 2018
    Assignee: Patheon API Services Inc.
    Inventors: George Petros Yiannikouros, Panos Kalaritis, Chaminda Priyapushpa Gamage, Denis Viktorovich Arefyev
  • Combretastatin analogs
    Patent number: 10100029
    Abstract: The present invention relates novel heterocyclic analogs of combretastatin, their synthesis, and their use as anti-cancer compounds. In particular, compounds of Formula (I), Formula (II), and Formula (V) are provided.
    Type: Grant
    Filed: December 20, 2017
    Date of Patent: October 16, 2018
    Assignee: BioVentures, LLC
    Inventors: Narsimha Reddy Penthala, Peter Crooks, Vijayakumar Sonar
  • Carboxymethyl piperidine derivative
    Patent number: 10100030
    Abstract: The present invention provides a new compound which has NK1 receptor antagonist activity, whose CYP3A4 inhibitory activity is reduced compared to aprepitant, and which are useful for the prevention or treatment of cancer-chemotherapy-induced nausea and vomiting. That is, the present invention relates to carboxymethyl piperidine derivatives represented by the following formula (I) or a pharmaceutically acceptable salt thereof. Wherein, ring A is a benzene ring or the like; ring B is a pyridine ring or the like; R1 is C1-6 alkyl or C1-6 alkoxy; R2 and R3 are a hydrogen atom or methyl; and n is an integral number from 0 to 5.
    Type: Grant
    Filed: November 6, 2014
    Date of Patent: October 16, 2018
    Assignee: KISSEI PHARMACEUTICAL CO., LTD.
    Inventors: Kazuo Shimizu, Takashi Miyagi, Kohsuke Ohno, Yasunori Ueno, Yusuke Onda, Hikaru Suzuki
  • Manufacturing process for triazine, pyrimidine and pyridine derivatives
    Patent number: 10100031
    Abstract: The invention relates to a method of manufacturing triazine, pyrimidine and pyridine derivatives of formula (I), wherein U, V, W and Z are nitrogen or carbon atoms, whereby at least one of U, V and W is nitrogen, and the other substituents are defined as in the specification, by condensing a corresponding halo-triazine, pyrimidine or pyridine in a type of Suzuki coupling with a pyridyl- or pyrimidinyl-borane, wherein the amino function is protected as a formamidine. The invention further relates to suitable intermediates and methods of manufacturing of such intermediates. Furthermore the invention relates to pure 5-(4,6-dimorpholino-1,3,5-triazin-2-yl)-4-(trifluoromethyl)pyridin-2-amine in solid form.
    Type: Grant
    Filed: April 20, 2015
    Date of Patent: October 16, 2018
    Assignees: UNIVERSITAET BASEL, PIQUR THERAPEUTICS AG
    Inventors: Paul Hebeisen, Florent Beaufils, Jean-Baptiste Langlois
  • Crystalline forms of 3-(4-amino-1-oxo-1,3 dihydro-isoindol-2-yl)-piperidine-2,6-dione
    Patent number: 10100032
    Abstract: The invention relates to novel crystalline forms of 3-(4-amino-l-oxo-l,3 dihydro-isoindol-2-yl)-piperidine-2,6-dione, including a novel urea cocrystal of 3-(4-amino-l-oxo-l,3 dihydro-isoindol-2-yl)-piperidine-2,6-dione; a novel gallic acid cocrystal of 3-(4-amino-l-oxo-1,3 dihydro-isoindol-2-yl)-piperidine-2,6-dione; a novel propyl gallate cocrystal of 3-(4-amino-l-oxo-1,3 dihydro-isoindol-2-yl)-piperidine-2,6-dione; and a novel L-tartaric acid cocrystal of 3-(4-amino-1-oxo-1,3 dihydro-isoindol-2-yl)-piperidine-2,6-dione. The preparation and characterization of the novel crystalline forms according to various embodiments of the invention are described. The invention also relates to pharmaceutical compositions containing the novel crystalline forms, and the therapeutic use of the novel crystalline forms.
    Type: Grant
    Filed: December 2, 2016
    Date of Patent: October 16, 2018
    Assignee: AMPLIO PHARMA, LLC
    Inventors: Scott L. Childs, Shreenivas R. Lingireddy, Nathan Barishansky
  • Processes for the preparation of pesticidal compounds
    Patent number: 10100033
    Abstract: This application relates to efficient and economical synthetic chemical processes for the preparation of pesticidal thioethers and pesticidal sulfoxides. Further, the present application relates to certain novel compounds necessary for their synthesis. It would be advantageous to produce pesticidal thioethers and pesticidal sulfoxides efficiently and in high yield from commercially available starting materials.
    Type: Grant
    Filed: December 22, 2017
    Date of Patent: October 16, 2018
    Assignee: Dow AgroSciences LLC
    Inventors: Xiaoyong Li, Erich Molitor, Gary Alan Roth, Matthias S. Ober, Patrick Hanley, Tina T. Staton
  • Process for preparing an anti-cancer agent, 1-((4-(4-fluoro-2-methyl-1H-indol-5-yloxy)-6-methoxyquinolin-7-yloxy)methyl)cyclopropanamine, its crystalline form and its salts
    Patent number: 10100034
    Abstract: The present invention relates a new process to synthesize 1-((4-(4-Fluoro-2-methyl-1H-indol-5-yloxy)-6-methoxyquinolin-7-yloxy)methyl)cyclopropanamine (AL3818). A stable crystalline form of A13818 has been prepared. Salts and their crystalline forms of AL3818 have been also prepared. Anti-cancer and optometric activities of AL3818 and its salts have been further tested. New process has been outlined in Scheme I.
    Type: Grant
    Filed: July 25, 2017
    Date of Patent: October 16, 2018
    Assignee: Advenchen Pharmaceuticals, LLC
    Inventors: Guoqing Paul Chen, Changren Yan
  • Substituted 2-[3-(1-methyl-piperidin-4-yl)-propylamino]-pyrimidine-5-carboxylic acids and amides and methods of making the same
    Patent number: 10100035
    Abstract: The present invention relates to certain intermediates useful in the preparation of certain benzoimidazol-2-yl pyrimidines and processes for preparing them.
    Type: Grant
    Filed: September 20, 2017
    Date of Patent: October 16, 2018
    Assignee: Janssen Pharmaceutica NV
    Inventors: Diego Broggini, Matteo Conza, Oliver Flögel, Stefan Horns, Susanne Lochner, Guangrong Tang, Zhaobin Wang, Lucie Lovelle
  • Lappaconitine aza-cinnamic acid derivatives with anti-tumor activities and a method of preparing the same
    Patent number: 10100036
    Abstract: A lappaconitine aza-cinnamic acid derivative having the following formula (I): X is C or N, and R1, R2, and R3 are independently H or lower alkyl. A method of preparing the lappaconitine aza-cinnamic acid derivative of formula (I) is also disclosed.
    Type: Grant
    Filed: September 25, 2017
    Date of Patent: October 16, 2018
    Assignee: SHAANXI UNIVERSITY OF SCIENCE AND TECHNOLOGY
    Inventors: Chengyuan Liang, Minyi Jia, Xingke Ju, Lei Tian, Danni Tian, Shunjun Ding
  • Activity-based probe compounds, compositions, and methods of use
    Patent number: 10100037
    Abstract: Activity-based probe compounds for use in labeling a cysteine protease are provided. The compounds are targeted to the protease through a specific targeting element. The compounds additionally include a detectable element, such as a fluorescent label, a radiolabel, or a chelator. In some cases, the compounds additionally include a quenching element that is released upon reaction with the protease. Also provided are compositions comprising the compounds and methods for using the compounds, for example in labeling a protease in an animal and in visualizing a tumor in an animal.
    Type: Grant
    Filed: March 15, 2014
    Date of Patent: October 16, 2018
    Assignee: The Board of Trustees of the Leland Stanford Junior University
    Inventors: Matthew S. Bogyo, Martijn Verdoes
  • Isoquinolin-3-yl carboxamides and preparation and use thereof
    Patent number: 10100038
    Abstract: Isoquinoline compounds for treating various diseases and pathologies are disclosed. More particularly, the present invention concerns the use of an isoquinoline compound or analogs thereof, in the treatment of disorders characterized by the activation of Wnt pathway signaling (e.g., cancer, abnormal cellular proliferation, angiogenesis, fibrotic disorders, bone or cartilage diseases, and osteoarthritis), the modulation of cellular events mediated by Wnt pathway signaling, as well as genetic diseases and neurological conditions/disorders/diseases due to mutations or dysregulation of the Wnt pathway and/or of one or more of Wnt signaling components. Also provided are methods for treating Wnt-related disease states.
    Type: Grant
    Filed: January 30, 2018
    Date of Patent: October 16, 2018
    Assignee: Samumed, LLC
    Inventors: Sunil Kumar KC, Chi Ching Mak, Brian Walter Eastman, Jianguo Cao, Venkataiah Bollu, Gopi Kumar Mittapalli, Chandramouli Chiruta
  • Allisartan isoproxil polymorph, its preparation method and pharmaceutical
    Patent number: 10100039
    Abstract: Disclosed are polymorph of allisartan isoproxil and a pharmaceutical composition thereof. The polymorph is non-electrostatic, highly flowable and highly stable, and can be used for treating hypertension and complications thereof.
    Type: Grant
    Filed: June 5, 2015
    Date of Patent: October 16, 2018
    Assignee: SHENZHEN SALUBRIS PHARMACEUTICALS CO., LTD
    Inventors: Duanming Tan, Jun Ou
  • Compounds and uses thereof for the modulation of hemoglobin
    Patent number: 10100040
    Abstract: Provide herein are compounds and pharmaceutical compositions suitable as modulators of hemoglobin, methods and intermediates for their preparation, and methods for their use in treating disorders mediated by hemoglobin and disorders that would benefit from tissue and/or cellular oxygenation.
    Type: Grant
    Filed: March 10, 2014
    Date of Patent: October 16, 2018
    Assignee: Global Blood Therapeutics, Inc.
    Inventors: Zhe Li, Qing Xu, Brian W. Metcalf, Stephen L. Gwaltney, II, Jason R. Harris, Calvin W. Yee
  • Pyrazolyl substituted tetrahydropyranylsulfones
    Patent number: 10100041
    Abstract: The invention relates to pyrazolyl substituted tetrahydropyranylsulfones as voltage gated calcium channel blockers, to pharmaceutical compositions containing these compounds and also to these compounds for use in the treatment and/or prophylaxis of pain and further diseases and/or disorders.
    Type: Grant
    Filed: October 7, 2016
    Date of Patent: October 16, 2018
    Assignee: GRÜNENTHAL GMBH
    Inventors: Stefan Schunk, Melanie Reich, René Michael Koenigs
  • [5,6]—fused bicyclic antidiabetic compounds
    Patent number: 10100042
    Abstract: Novel compounds of the structural formula (I), and the pharmaceutically acceptable salts thereof, are agonists of G-protein coupled receptor 40 (GPR40) and may be useful in the treatment, prevention and suppression of diseases mediated by the G-protein-coupled receptor 40. The compounds of the present invention may be useful in the treatment of Type 2 diabetes mellitus, and of conditions that are often associated with this disease, including obesity and lipid disorders, such as mixed or diabetic dyslipidemia, hyperlipidemia, hypercholesterolemia, and hypertriglyceridemia.
    Type: Grant
    Filed: August 3, 2015
    Date of Patent: October 16, 2018
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Helen Chen, Duane DeMong, Paul E. Finke, Christopher W. Plummer
  • Substituted aldehyde compounds and methods for their use in increasing tissue oxygenation
    Patent number: 10100043
    Abstract: Provided are cycloalkyl- and cycloalkenyl-substituted benzaldehydes and heteroaldehydes of formula (I) that act as allosteric modulators of hemoglobin, methods and intermediates for their preparation, pharmaceutical compositions containing the modulators, and methods for their use in treating disorders mediated by hemoglobin and disorders that would benefit from increased tissue oxygenation.
    Type: Grant
    Filed: March 14, 2014
    Date of Patent: October 16, 2018
    Assignees: Global Blood Therapeutics, Inc., Cytokinetics, Inc.
    Inventors: Brian Metcalf, Chihyuan Chuang, Zhe Li
  • Methods for preparing brexpiprazole, key intermediates thereof and salts thereof
    Patent number: 10100044
    Abstract: The present invention relates to the methods for preparing brexpiprazole, the analogs, key intermediates, and salts thereof, specifically, the present invention relates to a new method for preparing brexpiprazole, the analogs, key intermediates, and salts thereof, and the key intermediates, and salts thereof provided during the preparation. The preparation method has a mild reaction condition, stable intermediate, easy operation, and uses cheap and easy-to-get reagents, thus it saves the synthesis cost, shortens the production cycle, improves the yield and product quality, and is suitable for mass production.
    Type: Grant
    Filed: October 20, 2014
    Date of Patent: October 16, 2018
    Assignees: Suzhou Vigonvita Life Sciences Co., Ltd., Topharman Shanghai Co., Ltd., Shanghai Institute of Materia Medica, Chinese Academy of Sciences
    Inventors: Zheng Liu, Chunhui Wu, Yongjian Liu, Rongxia Zhang, Yang He, Guanghui Tian, Jingshan Shen
  • 3-aryl-2H-pyrazolo[4,3-b]pyridine compounds and their use as AMPA receptor modulators
    Patent number: 10100045
    Abstract: Provided herein are compounds of Formula (I), and pharmaceutically acceptable salts, N-oxides, or solvates thereof, Also provided herein are pharmaceutical compositions comprising compounds of Formula (I) and methods of using compounds of Formula (I).
    Type: Grant
    Filed: October 23, 2017
    Date of Patent: October 16, 2018
    Assignee: Janssen Pharmaceutica NV
    Inventors: Michael K. Ameriks, Brian Ngo Laforteza, Brad M. Savall, Warren Stanfield Wade, Stephen Todd Meyer, Márió Gyuris
  • Inhibitors of lysine specific demethylase-1
    Patent number: 10100046
    Abstract: The present invention relates generally to compositions and methods for treating cancer and neoplastic disease. Provided herein are substituted heterocyclic derivative compounds and pharmaceutical compositions comprising said compounds. The subject compounds and compositions are useful for inhibition of lysine specific demethylase-1. Furthermore, the subject compounds and compositions are useful for the treatment of cancer, such as prostate cancer, breast cancer, bladder cancer, lung cancer and/or melanoma and the like.
    Type: Grant
    Filed: January 10, 2018
    Date of Patent: October 16, 2018
    Assignee: CELGENE QUANTICEL RESEARCH, INC.
    Inventors: Young K. Chen, Toufike Kanouni, Zhe Nie, Jeffrey Alan Stafford, James Marvin Veal
  • Piperidine derivatives as orexin receptor antagonist
    Patent number: 10100047
    Abstract: The present invention discloses a series of piperidine derivatives as orexin receptor antagonists and compositions thereof, and relates to the application thereof in preparing medications for the treatment of insomnia, chronic obstructive pulmonary disease, obstructive sleep apnea, hypersomnia, anxiety, obsessive-compulsive disorder, panic attack, nicotine addiction, or binge eating disorder.
    Type: Grant
    Filed: February 27, 2015
    Date of Patent: October 16, 2018
    Assignees: SHANGHAI HAIYAN PHARMACEUTICAL TECHNOLOGY CO., LTD., YANGTZE RIVER PHARMACEUTICAL GROUP CO., LTD.
    Inventors: Haiying He, Songliang Wu, Yang Zhang, Biao Ma, Yuan Chen, Yuhe Wang, Shuhui Chen, Qiang Lv, Jiong Lan, Xing Liu
  • Heterocyclic compounds and their use as glycogen synthase kinase-3 inhibitors
    Patent number: 10100048
    Abstract: The present invention relates to novel heterocyclic compounds which are useful for inhibiting glycogen synthase kinase 3 (GSK-3), methods of making the compounds, compositions containing the compounds, and methods of treatment using the compounds.
    Type: Grant
    Filed: September 30, 2015
    Date of Patent: October 16, 2018
    Assignee: ABBVIE DEUTSCHLAND GMBH & CO. KG
    Inventors: Sean Colm Turner, Margaretha Henrica Maria Bakker, Marcel van Gaalen, Falko Ernst Wolter, Wilfried Hornberger, Marjoleen Nijsen
  • JAK kinase inhibitor compounds for treatment of respiratory disease
    Patent number: 10100049
    Abstract: The invention provides compounds of formula (I): wherein X is and the variables are defined in the specification, or a pharmaceutically-acceptable salt thereof, that are useful as JAK kinase inhibitors. The invention also provides pharmaceutical compositions comprising such compounds, methods of using such compounds to treat respiratory diseases, and processes and intermediates useful for preparing such compounds.
    Type: Grant
    Filed: November 2, 2016
    Date of Patent: October 16, 2018
    Assignee: THERAVANCE BIOPHARMA R&D IP, LLC
    Inventors: Paul R. Fatheree, John R. Jacobsen, Anne-Marie Beausoleil, Gary E. Brandt, Melissa Fleury, Lan Jiang, Cameron Smith, Steven D. E. Sullivan, Lori Jean Van Orden
  • Kinase inhibitors
    Patent number: 10100050
    Abstract: Compounds of formula (I) defined herein are p38 MAPK inhibitors and are useful as anti-inflammatory agents in the treatment of, inter alia, diseases of the respiratory tract.
    Type: Grant
    Filed: December 22, 2016
    Date of Patent: October 16, 2018
    Assignee: CHIESI FARMACEUTICI S.p.A.
    Inventors: Carmelida Capaldi, Elisabetta Armani, Andrew Steven Robert Jennings, Christopher Hurley
  • Compound of 5-hydroxyl-1,7-naphthyridine substituted by aryloxy or heteroaryloxy, preparation method thereof and pharmaceutical use thereof
    Patent number: 10100051
    Abstract: A compound of 5-hydroxyl-1,7-naphthyridine substituted by aryloxy or heteroaryloxy, a preparation method thereof and a pharmaceutical use thereof are provided. In particular, the compound has the following Formula (I), wherein R2 and R3 are each independently H; R1 is H or C1-C3 alkyl; Ar is an aromatic ring or a heteroaromatic ring selected from a naphthalene ring, a pyridine ring, a thiophene ring, a furan ring and a substituted benzene ring. Pharmaceutically acceptable salts of the present compound, are provided, as well as uses of the compound or pharmaceutically acceptable salts thereof in the preparation of a medicine for inhibiting HIF prolyl hydroxylase or a medicine for promoting the generation of endogenous EPO.
    Type: Grant
    Filed: December 14, 2015
    Date of Patent: October 16, 2018
    Assignee: SHENYANG SUNSHINE PHARMACEUTICAL CO. LTD.
    Inventors: Yunlong Zhou, Suixiong Cai, Guangfeng Wang, Lingling Jiao, Ping Min, Yu Jing, Ming Guo
  • Compounds for the treatment of hepatitis B virus infection
    Patent number: 10100052
    Abstract: The present disclosure generally relates to compounds and pharmaceutical compositions which may be used in methods of treating a hepatitis B virus infection.
    Type: Grant
    Filed: May 16, 2017
    Date of Patent: October 16, 2018
    Assignee: GILEAD SCIENCES, INC.
    Inventors: Evangelos Aktoudianakis, Eda Canales, Elbert Chin, Kevin S. Currie, Ashley Anne Katana, Darryl Kato, John O. Link, Samuel E. Metobo, Roland D. Saito, Zheng-Yu Yang
  • Process for the preparation of 8-(4-aminophenoxy)-4H-pyrido[2,3-b]pyrazin-3-one derivatives
    Patent number: 10100053
    Abstract: The present invention pertains generally to the field of organic chemical synthesis, and in particular to certain methods for the synthesis of 8-(4-aminophenyoxy)-4H-pyrido[2,3-b]pyrazin-3-one and related compounds (denoted herein as (3)) from 4-(4-aminophenyoxy)pyridine-2,3-diamine and related compounds (denoted herein as (1)), by reaction with glyoxylic acid (denoted herein as (2)). The compounds (3) are useful in the synthesis of known anti-cancer agents, such as 1-(5-tert-butyl-2-(4-methyl-phenyl)-pyrazol-3-yl)-3-[2-fluoro-4-[(3-oxo-4H-pyrido[2,3-b]pyrazin-8-yl)oxy]phenyl]urea.
    Type: Grant
    Filed: June 28, 2017
    Date of Patent: October 16, 2018
    Assignees: Cancer Research Technology Limited, Institute of Cancer Research: Royal Cancer Hosp. (The)
    Inventors: Alfonso Zambon, Dan Niculescu-Duvaz, Richard Chubb, Caroline Joy Springer
  • Pyrido[2,3-d]pyrimidines as anticancer agents
    Patent number: 10100054
    Abstract: The pyrido[2,3-d]pyrimidine derivatives as anticancer agents include 5-(substituted-phenyl)-2-(3-methyl-5-oxo-2H-pyrazol-1(5H)-yl)-7-(pyridin-3-yl)pyrido[2,3-d]pyrimidin-4(3H)-one derivatives having the formula: where R is hydrogen; 2-halo, 3-halo, or 4-halo (Cl, Br, or F); 2-methoxy, 3-methoxy, or 4-methoxy (OCH3); 2-nitro, 3-nitro, or 4-nitro (NO2); 4-isopropyl, 4-methyl, or 4-cyano (CN); 2-hydroxy or 3-hydroxy (OH), 3-chloro and 5-chloro; 2-methoxy and 5-methoxy, 3-methoxy and 5-methoxy, or 3-methoxy and 4-methoxy; 3,4,5-trimethoxy; or 2-hydroxy and 4-hydroxy; or a pharmaceutically acceptable salt thereof. The derivatives may be useful in treating various cancers, including hepatic, colon, prostate, breast, and lung cancer.
    Type: Grant
    Filed: April 3, 2018
    Date of Patent: October 16, 2018
    Assignee: KING SAUD UNIVERSITY
    Inventors: Nagy Mahmoud Hassan Khalifa, Mohamed A. Al-Omar, Hamad M. Alkahtani, Ahmed H. Bakheit
  • Imidazopyrroloquinoline salt, method for producing the same, medicament, cosmetic, and food
    Patent number: 10100055
    Abstract: There is provided a production method for the purpose of improving the solubility of an arginine-residue imidazopyrroloquinoline in water and making the purity thereof high. There is provided a compound represented by general formula (1): wherein n is 1, 2, 3 or 4; and M is an alkali metal or ammonium.
    Type: Grant
    Filed: December 18, 2017
    Date of Patent: October 16, 2018
    Assignee: MITSUIBISHI GAS CHEMICAL COMPANY, INC.
    Inventor: Kazuto Ikemoto
  • SHIP1 modulators and methods related thereto
    Patent number: 10100056
    Abstract: Compounds of formula (I): where R1, R2, R3, R4a, R4b, R5, R6 and R7 are defined herein, or stereoisomers or pharmaceutically acceptable salts thereof, are described herein. Such compounds have activity as SHIP1 modulators, and thus may be used to treat any of a variety of diseases, disorders or conditions that would benefit from SHIP1 modulation. Compositions comprising a compound of formula (I) in combination with a pharmaceutically acceptable carrier or diluent are also disclosed, as are methods of SHIP1 modulation by administration of such compounds to an animal in need thereof.
    Type: Grant
    Filed: February 27, 2014
    Date of Patent: October 16, 2018
    Assignee: Aquinox Pharmaceuticals (Canada) Inc.
    Inventors: Lloyd F. Mackenzie, Curtis Harwig, David Bogucki, Jeffery R. Raymond, Jeremy D. Pettigrew
  • Imidazopyrimidine and imidazotriazine derivative, and pharmaceutical composition comprising the same
    Patent number: 10100057
    Abstract: The present disclosure provides a compound of Chemical Formula (1) or a pharmaceutically acceptable salt thereof, and a pharmaceutical composition comprising the same: wherein X, Z, R1 and R2 are as defined in the specification. The compound of Chemical Formula (1) or pharmaceutically acceptable salt thereof acts as a positive allosteric modulator of metabotropic glutamate receptor subtype 5 (mGluR5), thereby being useful in the prevention or treatment of disorder mediated by glutamate dysfunction and mGluR5.
    Type: Grant
    Filed: July 31, 2017
    Date of Patent: October 16, 2018
    Assignee: SK BIOPHARMACEUTICALS CO., LTD.
    Inventors: Chun Eung Park, Young Koo Jang, Yong Je Shin, Ji Yeon Kim, Seung Mo Ham, Yong Gil Kim, Hye Kyung Min, Soo Bong Cha, Hyo Jun Jung, Ju Young Lee, Seung Nam Han, Jin Yong Chung, Eun Ju Choi, Chan Mi Joung, Jong Sil Park, Ji Won Lee, Nahm Ryune Cho, Eun Ju Ryu, Cheol Young Maeng
  • Fused heterocyclic compounds as CaM kinase inhibitors
    Patent number: 10100058
    Abstract: The present disclosure relates to compounds that are CaM Kinase inhibitors and to their use in the treatment of various disease states, including atrial fibrillation and myocardial infarction. In particular embodiments, the general structure of the compounds is given by Formula I: wherein R1, R2, R3, R4, R5, R6, R9 and R10 are as described herein, to methods for the preparation and use of the compounds and to pharmaceutical compositions containing the same.
    Type: Grant
    Filed: November 29, 2017
    Date of Patent: October 16, 2018
    Assignee: Gilead Sciences, Inc.
    Inventors: Elfatih Elzein, Rao V. Kalla, Dmitry Koltun, Xiaofen Li, Eric Q. Parkhill, Thao Perry, Scott Preston Simonovich, Jeff Zablocki, Christopher Allen Ziebenhaus
  • Apelin receptor (APJ) agonists and uses thereof
    Patent number: 10100059
    Abstract: This disclosure is directed to agonists of the apelin receptor (APJ) and uses of such agonists.
    Type: Grant
    Filed: December 9, 2016
    Date of Patent: October 16, 2018
    Assignee: Research Triangle Institute
    Inventors: Scott P. Runyon, Rangan Maitra, Sanju Narayanan, James Barnwell Thomas, Kenneth S. Rehder, Srinivas Olepu
  • Asymmetric synthesis of funapide
    Patent number: 10100060
    Abstract: This invention is directed to asymmetric synthesis of funapide, which is useful for the treatment and/or prevention of sodium channel-mediated diseases or conditions, such as pain.
    Type: Grant
    Filed: June 16, 2017
    Date of Patent: October 16, 2018
    Assignee: Xenon Pharmaceuticals Inc.
    Inventors: Ronen Ben-David, Jian Chen, Michael A. Christie, Mina Gadelrab Dimitri, Graciela Noemi Gershon, Linli He, Nelson G. Landmesser, Daniel V. Levy, Orel Yosef Mizrahi, Partha S. Mudipalli, Harlan F. Reese, Joseph A. Sclafani, Yi Wang
  • Oxazepine compound and agricultural/horticultural insecticide containing said compound as active ingredient, and method for using the same
    Patent number: 10100061
    Abstract: An oxazepine compound, or salt thereof, has General Formula (I): wherein R1, R2, R3 and R4 may be identical or different, representing a hydrogen atom, halogen atom, alkyl group, etc.; R5 and R6 may be identical or different, representing a hydrogen atom, alkyl group, or phenyl group, pyridyl group, etc., that may be substituted together with a carbon atom to which R5 or R6 is bonded; R7 represents a hydrogen atom, alkyl group, alkynyl group, cyano alkyl group, alkoxy alkyl group, etc.; Y represents an oxygen atom, S, NH, etc.; Y1 represents a C?O, C?S, CH2 group, etc.; A represents a CH group, etc.; and m represents 0 or 1], as well as an agricultural/horticultural insecticide using such oxazepine compound or salt thereof as its active ingredient, and method for using the same.
    Type: Grant
    Filed: August 18, 2015
    Date of Patent: October 16, 2018
    Assignee: NIHON NOHYAKU CO., LTD.
    Inventors: Nobuyuki Hayashi, Toshihiko Shigenari, Kosuke Fukatsu
  • Methods for the acylation of maytansinol
    Patent number: 10100062
    Abstract: Disclosed is a method of preparing an amino acid ester of maytansinol by reacting maytansinol with an N-carboxyanhydride of an amino acid (NCA) in the presence of a drying agent. Also disclosed is an improved method of preparing an amino acid ester of maytansinol in which a nucleophile is added to the reaction mixture after completion of the reaction between maytansinol and an N-carboxyanhydride of an amino acid.
    Type: Grant
    Filed: September 19, 2017
    Date of Patent: October 16, 2018
    Assignee: IMMUNOGEN, INC.
    Inventors: Wayne C. Widdison, Robert Yongxin Zhao
  • Compounds that inhibit Mcl-1 protein
    Patent number: 10100063
    Abstract: Provided herein are myeloid cell leukemia 1 protein (Mcl-1) inhibitors, methods of their preparation, related pharmaceutical compositions, and methods of using the same. For example, provided herein are compounds of Formula I, and pharmaceutically acceptable salts thereof and pharmaceutical compositions containing the compounds. The compounds and compositions provided herein may be used, for example, in the treatment of diseases or conditions, such as cancer.
    Type: Grant
    Filed: December 12, 2016
    Date of Patent: October 16, 2018
    Assignee: AMGEN INC.
    Inventors: Sean P. Brown, Yunxiao Li, Mike Elias Lizarzaburu, Brian S. Lucas, Nick A. Paras, Joshua Taygerly, Marc Vimolratana, Xianghong Wang, Ming Yu, Manuel Zancanella, Liusheng Zhu, Ana Gonzalez Buenrostro, Zhihong Li
  • Purine inhibitors of human phosphatidylinositol 3-kinase delta
    Patent number: 10100064
    Abstract: The instant invention provides compounds of formula (I) which are PI3K-delta inhibitors, and as such are useful for the treatment of PI3K-delta-mediated diseases such as inflammation, asthma, COPD and cancer.
    Type: Grant
    Filed: June 9, 2015
    Date of Patent: October 16, 2018
    Assignee: MERCK SHARP & DOHME CORP.
    Inventors: Meredeth Ann McGowan, Kin Chiu Fong, Neville John Anthony, Hua Zhou, Jason D. Katz, Lihu Yang, Chaomin Li, Yuan Tian, Changwei Mu, Baijun Ye, Feng Shi, Xiaoli Zhao, Jianmin Fu, Yabin Li
  • Compound for labeling mitochondria and method of producing the same
    Patent number: 10100065
    Abstract: This invention relates to a compound for labeling mitochondria and a method of producing the same, wherein the compound is represented by Chemical Formula 1 or Chemical Formula 2 below, and is useful in labeling mitochondria. In Chemical Formulas 1 and 2, n is 4 or 10.
    Type: Grant
    Filed: April 4, 2017
    Date of Patent: October 16, 2018
    Assignee: KOREA INSTITUTE OF SCIENCE AND TECHNOLOGY
    Inventors: Jun-Seok Lee, Dhiraj P. Murale, Seong-Cheol Hong, Seok Lee
  • Modulators of sestrin-GATOR2 interaction and uses thereof
    Patent number: 10100066
    Abstract: The present invention provides compounds, compositions thereof, and methods of using the same.
    Type: Grant
    Filed: October 21, 2016
    Date of Patent: October 16, 2018
    Assignee: Navitor Pharmaceuticals, Inc.
    Inventors: Kristina Michelle Fetalvero, Sridhar Narayan, David John O'Neill, Eddine Saiah, Shomit Sengupta
  • Method for producing cyanoalkyl fluorosilanes
    Patent number: 10100067
    Abstract: Cyanoalkylfluorosilanes are prepared in exceptionally high yield by the reaction of the corresponding cyanoalkylchlorosilanes with specific metal fluorides. The products are useful in lithium ion battery electrolyte composition.
    Type: Grant
    Filed: November 2, 2016
    Date of Patent: October 16, 2018
    Assignee: WACKER CHEMIE AG
    Inventor: Frank Deubel
  • Amidine group—or guanidine group—containing silane
    Patent number: 10100068
    Abstract: A silane of the formula (I) containing at least one aliphatic amidine group- or guanidine group-containing alkoxy group, to a method for producing same, to conversion products thereof, and to the use thereof as a catalyst in curable compositions, in particular based on silane group-containing polymers. The silane of the formula (I) is largely odorless and non-volatile at room temperature. The silane accelerates the hydrolysis and condensation reaction of silane groups very effectively without impairing the storage stability of silane group-containing polymers. Additionally, the silane is very tolerable in silane group-containing compositions, whereby such compositions are not prone to separate, migrate, or evaporate the catalyst.
    Type: Grant
    Filed: April 16, 2015
    Date of Patent: October 16, 2018
    Assignee: SIKA TECHNOLOGY AG
    Inventors: Urs Burckhardt, Rita Cannas
  • Rapid-curing, migration-free composition based on organic polymers containing silane groups
    Patent number: 10100069
    Abstract: The invention relates to a composition comprising at least one organic polymer that contains silane groups and at least one catalyst of formula (I). The composition is low in emissions and low-odor, has a good shelf-life, cures rapidly to form a mechanically high-quality, durable material with a very low propensity for migration-related defects such as exudation or dirt retention by the substrate. The composition is particularly suitable for use as an adhesive, sealant or coating.
    Type: Grant
    Filed: April 16, 2015
    Date of Patent: October 16, 2018
    Assignee: SIKA TECHNOLOGY AG
    Inventors: Urs Burckhardt, Rita Cannas
  • Borate-based base generator, and base-reactive composition comprising such base generator
    Patent number: 10100070
    Abstract: A compound capable of providing a composition having high storage stability without reacting with a base-reactive compound, even when stored in a mixed state with the base-reactive compound, as well as capable of generating a strong base by irradiation of light (active energy rays) or heating. A base generator comprises the compound and a base-reactive composition comprises the base generator and the base-reactive compound. The compound is represented by the general formula (A).
    Type: Grant
    Filed: January 22, 2015
    Date of Patent: October 16, 2018
    Assignee: FUJIFILM Wako Pure Chemical Corporation
    Inventors: Nobuhiko Sakai, Kosuke Yanaba
  • Heterocyclic selenamonophosphites protected on a hydroxyl group and processes for preparation thereof
    Patent number: 10100071
    Abstract: Novel heterocyclic selenamonophosphites protected on the hydroxyl group, processes for preparation thereof and the use thereof as ligand.
    Type: Grant
    Filed: December 6, 2016
    Date of Patent: October 16, 2018
    Assignee: EVONIK DEGUSSA GMBH
    Inventors: Katrin Marie Dyballa, Robert Franke, Claudia Weilbeer, Detlef Selent, Armin Börner
  • Phosphonate compounds for treatment of complement mediated disorders
    Patent number: 10100072
    Abstract: Compounds, methods of use, and processes for making inhibitors of complement factor D comprising Formula I, or a pharmaceutically acceptable salt or composition thereof wherein R12 or R13 on the A group is a phosphonate (R32) are provided. The inhibitors described herein target factor D and inhibit or regulate the complement cascade at an early and essential point in the alternative complement pathway, and reduce factor D's ability to modulate the classical and lectin complement pathways. The inhibitors of factor D described herein are capable of reducing the excessive activation of complement, which has been linked to certain autoimmune, inflammatory, and neurodegenerative diseases, as well as ischemia-reperfusion injury and cancer.
    Type: Grant
    Filed: May 26, 2017
    Date of Patent: October 16, 2018
    Assignee: Achillion Pharmaceuticals, Inc.
    Inventors: Jason Allan Wiles, Akihiro Hashimoto, Venkat Rao Gadhachanda, Godwin Pais, Qiuping Wang, Dawei Chen, Xiangzhu Wang, Atul Agarwal, Milind Deshpande, Avinash Phadke
  • Method for preparing low-molecular lignin derivative
    Patent number: 10100073
    Abstract: A method of preparing a low-molecular lignin derivative comprises the step of: preparing lignin by hydrolyzing lignocellulosic biomass with an acid; preparing a first mixture by mixing 100 parts by weight of the lignin and 500 parts or more by weight of a phenolic compound; preparing a second mixture by mixing the first mixture with a solvent including the hydrophobic polar solvent; and recovering a low-molecular lignin derivative from the second mixture.
    Type: Grant
    Filed: May 22, 2014
    Date of Patent: October 16, 2018
    Assignee: CJ CHEILJEDANG CORP.
    Inventors: Min Ho Jung, Sun Joo Moon, Jeung Yil Park, Sang Mok Lee, Da Eun Kim, Young Ran Kim, Jung Min Kim, Jin Hwa Chang
  • Regioselective silyl exchange of per-silylated oligosaccharides
    Patent number: 10100074
    Abstract: The present invention provides novel, regioselectively-acylated oligosaccharide compounds and methods for preparing them. In another aspect, the. invention provides a method for preparing a selectively-acylated oligosaccharide. The method includes forming a reaction mixture containing a protected oligosaccharide and an acylating agent. The protected oligosaccharide includes at least three hydroxyl moieties and each hydroxyl moiety is protected with a silyl protecting group. The reaction mixture is formed under conditions sufficient to selectively replace at least one silyl protecting group with a —C(0)-C1_6 alkyl group, and the selectively-acylated oligosaccharide comprises at least one —C(0)-C1_6 alkyl group and at least one silyl protecting group.
    Type: Grant
    Filed: December 18, 2015
    Date of Patent: October 16, 2018
    Assignee: The Regents of the University of California
    Inventors: Jacquelyn Gervay-Hague, Matthew Schombs
  • Process for the preparation of sofosbuvir
    Patent number: 10100075
    Abstract: The present disclosure relates to processes for the preparation of sofosbuvir or of its pharmaceutically acceptable salts. The present disclosure also provides intermediates useful in the synthesis of sofosbuvir.
    Type: Grant
    Filed: December 19, 2014
    Date of Patent: October 16, 2018
    Assignee: Mylan Laboratories Limited
    Inventors: Vipin Kumar Kaushik, Vijaya Krishna Ravi, Srinivas Vakiti, Bhavanisankar Tirumalaraju
  • Modified nucleosides for the treatment of viral infections and abnormal cellular proliferation
    Patent number: 10100076
    Abstract: The disclosed invention is a composition for and a method of seating a Flaviviridae (including BVDV and HCV), Orthomyxoviridae (including Influenza A and B) or Paramyxoviridae (including RSV) infection, or conditions related to abnormal cellular proliferation, in a host, including animals, and especially humans, using a nucleoside of general formula (I)-(XXIII) or its pharmaceutically acceptable salt or prodrug. This invention also provides an effective process to quantify the viral load, and in particular BVDV, HCV or West Nile Virus load, in a host, using real-time polymerase chain reaction (“RT-PCR”). Additionally, the invention discloses probe molecules that can fluoresce proportionally to the amount of virus present in a sample.
    Type: Grant
    Filed: June 3, 2013
    Date of Patent: October 16, 2018
    Assignee: Gilead Pharmasset LLC
    Inventors: Lieven Stuyver, Kyoichi Watanabe
  • 6-aryl-9-glycosylpurines and use thereof
    Patent number: 10100077
    Abstract: 6-aryl-9-glycosidpurines of general formula I and pharmaceutically acceptable salts thereof with alkali metals, ammonia, amines, or addition salts with acids, wherein Gly represents ?-D-arabinofuranosyl or ?-D-2?-deoxyribofuranosyl, Ar represents benzyl or furfuryl, each of which can be unsubstituted or substituted by one or more, preferably one to three, substituents selected from the group comprising hydroxyl, alkyl, halogen, alkoxy, amino, mercapto, carboxyl, cyano, amido, sulfo, sulfamido, acyl, acylamino, acyloxy, alkylamino, dialkylamino, alkylmercapto, trifluoromethyl, trifluoromethoxy, for use as antisenescent and UV protective compounds in animals.
    Type: Grant
    Filed: September 14, 2015
    Date of Patent: October 16, 2018
    Assignee: UNIVERZITA PALACKEHO V OLOMOUCI
    Inventors: Karel Dolezal, Lucie Plihalova, Hana Vylicilova, Marek Zatloukal, Ondrej Plihal, Jiri Voller, Miroslav Strnad, Magdalena Bryksova, Jitka Vostalova, Alena Rajnochova Svobodova, Jitka Ulrichova, Lukas Spichal