Pyrimidines With Chalcogen Bonded Directly To A Ring Carbon Of Said Pyrimidine Moiety Patents (Class 514/269)
  • Patent number: 10758538
    Abstract: The present subject matter relates to a compound represented by the general formula (I) or (I?) or a pharmacologically acceptable salt thereof; pharmaceutical compositions containing at least one of these compounds; methods of making at least one of these compounds; methods of using at least one of these compounds for treating and/or preventing various cancers and/or proliferation disorders; methods of using at least one of these compounds for monitoring the effectiveness of an anticancer therapy against various cancers. In one embodiment, the subject matter relates to compounds that bind with a level of specificity to heat shock protein 70 (Hsp70). In another embodiment, the subject matter relates to compounds that bind with a level of specificity to inhibit both heat shock protein 70 (Hsp70) and heat shock cognate protein 70 (Hsc70).
    Type: Grant
    Filed: July 17, 2018
    Date of Patent: September 1, 2020
    Assignee: Memorial Sloan-Kettering Cancer Center
    Inventors: Gabriela Chiosis, Tony Taldone, Anna Rodina, Pallav Patel, Yanlong Kang
  • Patent number: 10752618
    Abstract: The present invention provides improved, commercially viable and consistently reproducible processes for the preparation of pure and stable crystalline Raltegravir potassium Form 3 and pharmaceutical composition thereof.
    Type: Grant
    Filed: September 13, 2017
    Date of Patent: August 25, 2020
    Assignee: LUPIN LIMITED
    Inventors: Purna Chandra Ray, Samir Shanteshwar Shabade, Surinder Kumar Arora, D. Rajput Lalitkumar, B. Shivdavkar Radhakrishna, G. Varade Shantanu, D. Ausekar Govind, Girij Pal Singh, Shreyas Pandurang Deshmukh, Gaurav Amrut Patil
  • Patent number: 10669261
    Abstract: The present invention provides compounds of Formula (I): wherein all variables are as defined in the specification, and compositions comprising any of such novel compounds. These compounds are APJ agonists which may be used as medicaments, in particular for treating cardiovascular disorders.
    Type: Grant
    Filed: December 15, 2016
    Date of Patent: June 2, 2020
    Assignee: Bristl-Myers Squibb Company
    Inventors: Michael C. Myers, R. Michael Lawrence, Donna M. Bilder, Wei Meng, Zulan Pi, Robert Paul Brigance, Heather Finlay
  • Patent number: 10611755
    Abstract: The invention relates to compounds having the structure of formula (I) which can be used for the treatment of or against influenza infections.
    Type: Grant
    Filed: January 19, 2017
    Date of Patent: April 7, 2020
    Assignee: Janssen Sciences Ireland UC
    Inventors: Tim Hugo Maria Jonckers, David Craig McGowan, Jérôme Émile Georges Guillemont, Werner Constant J Embrechts, Guillaume Jean Maurice Mercey, Christophe Francis Robert Nestor Buyck, Wendy Mia Albert Balemans, Pierre Jean-Marie Bernard Raboisson
  • Patent number: 10556860
    Abstract: The present invention provides hTERT modulators and methods for producing and using the same. In particular, the present invention provide a compound of the formula as described herein. Some aspects of the invention are based on the characterization of the effect of hTERT core promoter region mutants on the 5-12 G-quadruplex structure and its stability. It is believed that some of the compounds of the invention bind selectively to the G-quadruplex in the hTERT core promoter mutant, which results in reversal of the effect of mutant promoter activation.
    Type: Grant
    Filed: November 30, 2016
    Date of Patent: February 11, 2020
    Assignee: ARIZONA BOARD OF REGENTS
    Inventors: Laurence Hurley, Vijay Gokhale, HyunJin Kang, Kui Wu
  • Patent number: 10548848
    Abstract: The present invention belongs to the field of pharmaceutical industry and relates to a pharmaceutical composition comprising an intragranulate phase and an extragranulate phase, wherein the pharmaceutically active ingredient (API) 2-({6-[(3R)-3-aminopiperidin-1-yl]-3-methyl-2,4-dioxo-3,4-dihydropyrimidin-1(2H)-yl}methyl)benzonitrile or a pharmaceutically acceptable salt thereof, is present in the intragranulate phase, wherein said intragranulate phase is free from microcrystalline cellulose. Further, the present invention relates to a process for preparing the same.
    Type: Grant
    Filed: June 16, 2016
    Date of Patent: February 4, 2020
    Assignee: Hexal AG
    Inventors: Thomas Kohr, Christian Wawra, Marco Marchesan
  • Patent number: 10472363
    Abstract: The present disclosure relates to stimulators of soluble guanylate cyclase (sGC), pharmaceutical formulations comprising them and their uses thereof, alone or in combination with one or more additional agents, for treating various diseases, wherein an increase in the concentration of nitric oxide (NO) or an increase in the concentration of cyclic Guanosine Monophosphate (cGMP), or both, or an upregulation of the NO pathway is desirable.
    Type: Grant
    Filed: September 1, 2017
    Date of Patent: November 12, 2019
    Assignee: Cyclerion Therapeutics, Inc.
    Inventors: Glen Robert Rennie, Rajesh R. Iyengar, Thomas Wai-Ho Lee, Paul Allan Renhowe, Joon Jung
  • Patent number: 10421744
    Abstract: The present invention provides, in part, compounds of Formula I: and pharmaceutically acceptable salts thereof; processes for the preparation of; intermediates used in the preparation of; and compositions containing such compounds or salts, and their uses for treating D1-mediated (or D1-associated) disorders including, e.g., schizophrenia (e.g., its cognitive and negative symptoms), cognitive impairment (e.g., cognitive impairment associated with schizophrenia, AD, PD, or pharmacotherapy therapy), and Parkinson's disease.
    Type: Grant
    Filed: September 6, 2018
    Date of Patent: September 24, 2019
    Assignee: PFIZER INC.
    Inventors: Michael Aaron Brodney, Jennifer Elizabeth Davoren, Amy Beth Dounay, Ivan Viktorovich Efremov, David Lawrence Firman Gray, Michael Eric Green, Jaclyn Louise Henderson, Chewah Lee, Scot Richard Mente, Steven Victor O'Neil, Bruce Nelsen Rogers, Lei Zhang
  • Patent number: 10414735
    Abstract: The present teachings relate to hydroxypyrimidinone derivatives of Formula IV, pharmaceutical compositions thereof, and methods of using such compounds to treat bacterial infections.
    Type: Grant
    Filed: November 9, 2016
    Date of Patent: September 17, 2019
    Assignee: FORGE THERAPEUTICS, INC.
    Inventors: Min Teng, Baskar Nammalwar, Konstantin Taganov, David T. Puerta
  • Patent number: 10351553
    Abstract: Provided herein are compounds of the formula: or pharmaceutically acceptable salts thereof, and compositions comprising such compounds for use in the treatment of diseases or conditions responsive to modulation of the small conductance calcium-activated potassium channel (SK channel).
    Type: Grant
    Filed: March 28, 2018
    Date of Patent: July 16, 2019
    Assignee: Cadent Therapeutics, Inc.
    Inventors: Dipak Vasantrao Amrutkar, Kelly Foster, Thomas Amos Jacobsen, Martin R. Jefson, Gregg F. Keaney, Janus Schreiber Larsen, Karin Sandager Nielsen
  • Patent number: 10292991
    Abstract: The described invention relates to small molecule therapeutic compounds capable of reducing the incidence of intracerebral hemorrhage and brain microhemorrhages identified using zebrafish and mouse models of intracerebral hemorrhage and brain microhemorrhages.
    Type: Grant
    Filed: August 2, 2017
    Date of Patent: May 21, 2019
    Assignee: Unity Health Toronto
    Inventors: Xiao-Yan Wen, R. Loch Macdonald, Andrew Baker, Tom A. Schweizer
  • Patent number: 10292395
    Abstract: In crop production in the fields of agriculture, horticulture and the like, the damage caused by insect pests etc. is still immense, and insect pests resistant to existing insecticides have emerged. Under such circumstances, the development of novel agricultural and horticultural insecticides is desired. The present invention provides an agricultural and horticultural insecticide comprising, as an active ingredient, a 3H-pyrrolopyridine compound represented by the general formula (1): (wherein A1, A2, and A3 each represent a nitrogen atom or a CH group, R1 represents an ethyl group, R2 and R4 each represent a hydrogen atom, R3 and R7 each represent a haloalkyl group, R5 and R6 each represent a fluorine atom, and m represents 0 or 2), an N-oxide thereof or a salt thereof; and a method for using the agricultural and horticultural insecticide.
    Type: Grant
    Filed: November 30, 2016
    Date of Patent: May 21, 2019
    Assignee: Nihon Nohyaku Co., Ltd.
    Inventors: Ikki Yonemura, Yusuke Sano, Akiyuki Suwa, Shunpei Fujie
  • Patent number: 10251883
    Abstract: The present invention relates to compounds and pharmaceutically acceptable salts thereof and formulations comprising the compounds or a pharmaceutically acceptable salts thereof that are useful in modulating lyn kinase activity. In particular, the compounds or a pharmaceutically acceptable salts thereof are useful for treating or preventing a disease or disorder including cardiovascular disease, dyslipidemia, dyslipoproteinemia, a disorder of glucose metabolism, metabolic syndrome (i.e., Syndrome X), a peroxisome proliferator activated receptor-associated disorder, septicemia, a thrombotic disorder, type II diabetes, obesity, pancreatitis, hypertension, renal disease, inflammation, or impotence.
    Type: Grant
    Filed: August 23, 2017
    Date of Patent: April 9, 2019
    Assignee: Melior Pharmaceuticals I, Inc.
    Inventors: Andrew G. Reaume, Michael S. Saporito
  • Patent number: 10226461
    Abstract: Provided herein are formulations, processes, solid forms and methods of use relating to 2-(tert-butylamino)-4-((1R,3R,4R)-3-hydroxy-4-methylcyclohexylamino)-pyrimidine-5-carboxamide.
    Type: Grant
    Filed: October 9, 2017
    Date of Patent: March 12, 2019
    Assignee: Signal Pharmaceuticals, LLC
    Inventors: Hon-Wah Man, Marie Georges Beauchamps, Mohit Atul Kothare, Nanfei Zou
  • Patent number: 10221157
    Abstract: The present invention relates to novel compounds of formula I: or a pharmaceutically acceptable salt thereof, wherein the integers are as defined in the description. The claimed compounds are useful for the treatment of a bacterial infection. Also claimed is a composition comprising a pharmaceutically acceptable carrier and, as active ingredient, a therapeutically effective amount of the claimed compounds, the use of the claimed compounds or compositions for the manufacture of a medicament for the treatment of a bacterial infection and a process for preparing the claimed compounds.
    Type: Grant
    Filed: August 4, 2017
    Date of Patent: March 5, 2019
    Assignee: Janssen Pharmaceutica NV
    Inventors: Jean-Francois Bonfanti, Philippe Muller, Frederic Marc Maurice Doublet, Jerome Michel Claude Fortin, Nacer Lounis
  • Patent number: 10188652
    Abstract: In the present invention, compound such as (1R,2S)-2-(((2,4-dimethylpyrimidin-5-yl)oxy)methyl)-2-(3-fluorophenyl)-N-(5-fluoropyridin-2-yl) cyclopropanecarboxamide have been found to be potent orexin receptor antagonists, and may be useful in the treatment of sleep disorders such as insomnia, as well as for other therapeutic uses.
    Type: Grant
    Filed: October 21, 2015
    Date of Patent: January 29, 2019
    Assignee: Eisai R&D Management Co., Ltd.
    Inventors: Margaret Moline, Gina Pastino, Yurie Akimoto, Yasuhiro Zaima, Nobuya Suzuki, Nobuo Yoshida
  • Patent number: 10160751
    Abstract: The present invention provides compounds of Formula (I); and the pharmaceutically acceptable salts thereof, which are inhibitors of the ROMK (Kir1.1) channel. The compounds may be used as diuretic and/or natriuretic agents and for the therapy and prophylaxis of medical conditions including cardiovascular diseases such as hypertension, heart failure and chronic kidney disease and conditions associated with excessive salt and water retention.
    Type: Grant
    Filed: February 8, 2016
    Date of Patent: December 25, 2018
    Inventors: Alexander Pasternak, Jessica Frie, Shuzhi Dong, Takao Suzuki, Shouning Xu
  • Patent number: 10085986
    Abstract: The present invention provides compounds of formula (1) and pharmaceutically acceptable salts thereof, wherein R1, R2, Y and Z are as defined in the specification, processes for their preparation, pharmaceutical compositions containing them and their use in therapy.
    Type: Grant
    Filed: July 5, 2012
    Date of Patent: October 2, 2018
    Assignee: Takeda Pharmaceutical Company Limited
    Inventors: Xiao-Ling Fan Cockcroft, William Farnaby, Natasha Kinsella, Kevin Merchant, David Miller
  • 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
  • Patent number: 10015960
    Abstract: A sticker adjuvant that may be used in agrochemical compositions is disclosed. The sticker adjuvant is a polyether amide or a polyether imide formed by the reaction of a polyether polyamine with a polyfunctional monomer. The polyfunctional monomer may be a polyacid, a di-functional acyl halide, an acid anhydride, a poly(acid anhydride) and a mixture thereof.
    Type: Grant
    Filed: December 8, 2016
    Date of Patent: July 10, 2018
    Assignee: HUNTSMAN PETROCHEMICAL LLC
    Inventors: Matthew T. Meredith, Alan J Stern, Dilek Saylik
  • Patent number: 9949978
    Abstract: The present application relates to novel bicyclically substituted uracil derivatives, to processes for preparation thereof, to the use thereof alone or in combinations for treatment and/or prophylaxis of diseases, and to the use thereof for production of medicaments for treatment and/or prophylaxis of diseases.
    Type: Grant
    Filed: October 7, 2016
    Date of Patent: April 24, 2018
    Assignee: Bayer Pharma Aktiengesellschaft
    Inventors: Chantal Fürstner, Jens Ackerstaff, Alexander Straub, Heinrich Meier, Hanna Tinel, Katja Zimmermann, Adrian Tersteegen, Dmitry Zubov, Raimund Kast, Jens Schamberger, Martina Schäfer, Kirsten Börngen
  • Patent number: 9938248
    Abstract: Disclosed is a method for preparing a compound of Formula 1 wherein Q and Z are as defined in the disclosure comprising distilling water from a mixture comprising a compound of Formula 2, a compound of Formula 3, a base comprising at least one compound selected from the group consisting of alkaline earth metal hydroxides of Formula 4 wherein M is Ca, Sr or Ba, alkali metal carbonates of Formula 4a wherein M1 is Li, Na or K, 1,5-diazabicyclo[4.3.0]non-5-ene and 1,8-diazabicyclo[5.4.0]undec-7-ene, and an aprotic solvent capable of forming a low-boiling azeotrope with water.
    Type: Grant
    Filed: October 30, 2017
    Date of Patent: April 10, 2018
    Assignee: E.I. du Pont de Nemours and Company
    Inventor: Gary David Annis
  • Patent number: 9902712
    Abstract: The present invention relates to the field of medicine, provided herein are novel nitrogenous heterocyclic compounds, their preparation methods and their uses as drugs, especially for treatment and prevention of tissue fibrosis. Also provided herein are pharmaceutically acceptable compositions comprising the nitrogenous heterocyclic compounds and the uses of the compositions in the treatment of human or animal tissue fibrosis, especially for human or animal renal interstitial fibrosis, glomerular sclerosis, liver fibrosis, pulmonary fibrosis, IPF, peritoneal fibrosis, myocardial fibrosis, dermatofibrosis, postsurgical adhesion, benign prostatic hyperplasia, skeletal muscle fibrosis, scleroderma, multiple sclerosis, pancreatic fibrosis, cirrhosis, myosarcoma, neurofibroma, pulmonary interstitial fibrosis, diabetic nephropathy, alzheimer disease or vascular fibrosis.
    Type: Grant
    Filed: December 19, 2014
    Date of Patent: February 27, 2018
    Assignee: SUNSHINE LAKE PHARMA CO., LTD.
    Inventors: Jiancun Zhang, Xiaojun Wang, Yingjun Zhang, Runfeng Lin, Yi Yu, Liang Chen, Jihua Lin
  • Patent number: 9901549
    Abstract: The invention relates to therapeutic compositions for the treatment of dry eye, more specifically to compositions comprising a TRPM8 receptor agonist ligand. Furthermore, the invention relates to therapeutic compositions for the treatment of epiphora, more specifically to compositions comprising a TRPM8 receptor antagonist.
    Type: Grant
    Filed: August 3, 2016
    Date of Patent: February 27, 2018
    Assignees: UNIVERSIDAD MIGUEL HERNÁNDEZ DE ELCHE, CONSEJO SUPERIOR DE INVESTIGACIONES CIENTÍFICAS (C.S.I.C.)
    Inventors: Carlos Belmonte Martínez, Juana Gallar Martinez, Antonio Ferrer Montiel, Asia Fernández Carvajal, Félix Viana De La Iglesia
  • Patent number: 9873674
    Abstract: Compounds having a c-Rel inhibiting property according to the formula: (1) wherein R1 and R2 are each independently selected from hydrogen atom and hydrocarbon groups having at least one and up to thirty carbon atoms and optionally substituted with one or more heteroatoms selected from halogen, nitrogen, oxygen, and sulfur; R3 is selected from hydrocarbon groups having at least one and up to thirty carbon atoms and optionally substituted with one or more heteroatoms selected from halogen, nitrogen, oxygen, and sulfur; and X1, X2, and X3 are each independently selected from oxygen and sulfur atoms. Methods for treating diseases and conditions associated with c-Rel overexpression by administering compounds of Formula (1) or a pharmaceutical composition thereof to a subject afflicted with such a disease or condition are also described.
    Type: Grant
    Filed: September 19, 2013
    Date of Patent: January 23, 2018
    Assignee: CORNELL UNIVERSITY
    Inventors: Hsiou-Chi Liou, Mei-Ling Liou, Samedy Ouk
  • Patent number: 9856234
    Abstract: The present invention relates to a heterocyclic compound of the general formula (I) and their use and preparation, methods of making the compounds, compositions containing at least one of said compounds, and methods of treatment using at least one compound. In particular, compounds of the general formula (I) are useful for inhibiting glycogen synthase kinase 3 (GSK-3).
    Type: Grant
    Filed: January 31, 2014
    Date of Patent: January 2, 2018
    Assignees: ABBVIE DEUTSCHLAND GMBH & CO. KG, ABBVIE INC.
    Inventors: Sean Colm Turner, Margaretha Henrica Maria Bakker, Kent D. Stewart
  • Patent number: 9850214
    Abstract: Disclosed are chemical entities which are inhibitors of Nedd8-activating enzyme (NAE), namely, the compound {(1S,2S,4R)-4-[(6-{[(1R,2S)-5-chloro-2-methoxy-2,3-dihydro-1H-inden-1-yl]amino}pyrimidin-4-yl)oxy]-2-hydroxycyclopentyl}methyl sulfamate and pharmaceutically acceptable salts thereof; solid state forms thereof; and prodrugs thereof. Also disclosed are methods of using the chemical entities to treat disorders such as cancer.
    Type: Grant
    Filed: July 8, 2014
    Date of Patent: December 26, 2017
    Assignee: MILLENNIUM PHARMACEUTICALS, INC.
    Inventors: Ashley Sue McCarron, Todd B. Sells, Matthew Stirling, Stephen G. Stroud
  • Patent number: 9828383
    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: August 7, 2017
    Date of Patent: November 28, 2017
    Assignee: Pharmacyclic s LLC
    Inventors: Norbert Purro, Mark Stephen Smyth, Erick Goldman, David D. Wirth
  • Patent number: 9828351
    Abstract: The present disclosure relates generally, but not exclusively, to compounds and their use as enzyme interacting agents, in particular, agents which interact with one or more enzymes in the sphingolipid biosynthesis pathway. The disclosure further relates to the use of such compounds as research tools, use in therapy, to compositions and agents comprising said compounds, and to methods of treatment using said compounds.
    Type: Grant
    Filed: June 26, 2015
    Date of Patent: November 28, 2017
    Assignees: MONASH UNIVERSITY, UNIVERSITY OF SOUTH AUSTRALIA, CENTRAL ADELAIDE LOCAL HEALTH NETWORK INCORPORATED
    Inventors: Bernard Luke Flynn, Luigi Aurelio, Carmen Vittoria Scullino, Bing Hui Wang, Stuart Maxwell Pitson, Melissa Rose Pitman
  • Patent number: 9777001
    Abstract: The present invention provides compounds of Formula (I): or stereoisomers, tautomers, or pharmaceutically acceptable salts thereof, wherein all the variables are as defined herein. These compounds are selective factor XIa inhibitors or dual inhibitors of FXIa and plasma kallikrein. This invention also relates to pharmaceutical compositions comprising these compounds and methods of treating thromboembolic and/or inflammatory disorders using the same.
    Type: Grant
    Filed: January 30, 2015
    Date of Patent: October 3, 2017
    Assignee: Bristol-Myers Squibb Company
    Inventors: James R. Corte, Indawati De Lucca, Tianan Fang, Wu Yang, Yufeng Wang, Andrew K. Dilger, Kumar Balashanmuga Pabbisetty, William R. Ewing, Yeheng Zhu, Ruth R. Wexler, Donald J. P. Pinto, Michael J. Orwat, Leon M. Smith, II
  • Patent number: 9770023
    Abstract: The present invention relates to novel fungicidal active compound combinations or compositions comprising a phenylamidine compound of formula (I) and further active compounds (II) and (III) selected from the groups (A), (B) and/or (C), to a process for preparing these active compound combinations or compositions and to the use thereof as biologically active compound combinations or compositions, especially for the control of phytopathogenic fungi in plants and/or in the protection of materials and/or as plant growth regulators.
    Type: Grant
    Filed: February 10, 2015
    Date of Patent: September 26, 2017
    Assignee: BAYER CROPSCIENCE AKTIENGESELLSCHAFT
    Inventors: Andreas Goertz, Thomas Seitz, Peter Dahmen, Ulrike Wachendorff-Neumann
  • Patent number: 9763945
    Abstract: The present invention relates to compounds and pharmaceutically acceptable salts thereof and formulations comprising the compounds or a pharmaceutically acceptable salts thereof that are useful in modulating lyn kinase activity. In particular, the compounds or a pharmaceutically acceptable salts thereof are useful for treating or preventing a disease or disorder including cardiovascular disease, dyslipidemia, dyslipoproteinemia, a disorder of glucose metabolism, metabolic syndrome (i.e., Syndrome X), a peroxisome proliferator activated receptor-associated disorder, septicemia, a thrombotic disorder, type II diabetes, obesity, pancreatitis, hypertension, renal disease, inflammation, or impotence.
    Type: Grant
    Filed: November 13, 2015
    Date of Patent: September 19, 2017
    Assignee: Melior Pharmaceuticals I, Inc.
    Inventors: Andrew G. Reaume, Michael S. Saporito
  • Patent number: 9750252
    Abstract: An arylalkyloxypyrimidine derivative represented by the formula (I) wherein R1 is an alkyl group, a cycloalkyl group, an alkenyl group, an alkynyl group, a haloalkyl group, a haloalkenyl group, a haloalkynyl group, an alkoxyalkyl group, a dioxolane group and the like; R2 and R3 are each a hydrogen atom, an alkyl group and the like; X is an alkyl group, a cycloalkyl group, an alkenyl group, an alkynyl group, a haloalkyl group, a haloalkenyl group, a haloalkynyl group, a trialkylsilyl group and the like; Y is CH or a nitrogen atom; q is an integer of 1 to 3; m is an integer of 0 to 5; and n is 0 or 1 or a salt thereof, and an agrohorticultural insecticide containing the compound as an active ingredient and a method of use thereof.
    Type: Grant
    Filed: February 1, 2013
    Date of Patent: September 5, 2017
    Assignee: Nihon Nohyaku., Ltd.
    Inventors: Eikou Satoh, Tetsuya Murata, Hiroto Harayama, Motofumi Nakano, Kosuke Fukatsu, Kayo Inukai, Ryota Kasahara, Yutaka Abe, Nobuyuki Hayashi, Naoya Fujita
  • Patent number: 9713617
    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: December 21, 2016
    Date of Patent: July 25, 2017
    Assignee: Pharmacyclics LLC
    Inventors: Norbert Purro, Mark Stephen Smyth, Erick Goldman, David D. Wirth
  • Patent number: 9700547
    Abstract: The use of at least one compound of formula I or II or pharmaceutically acceptable salts thereof, for preparing a pharmaceutical composition that acts by inhibiting the phosphorylase uridine enzyme, and the use of the compounds for preparing a pharmaceutical composition that acts by inhibiting the human phosphorylase uridine enzyme, which can be optionally used in combination with at least one antineoplastic, wherein the inhibition increases the effectiveness of antineoplastic and decreases the side effects caused by the administration of antineoplastics.
    Type: Grant
    Filed: September 2, 2014
    Date of Patent: July 11, 2017
    Assignee: União Brasileira de Educação e Assistência, Mantenedora da Pucrs
    Inventors: Luiz Augusto Basso, Pablo Machado, Daiana Renck, Diógenes Santiago Santos
  • Patent number: 9695131
    Abstract: Substituted uracil derivatives of formula (I), processes for their preparation, their use alone or in combinations for the treatment and/or prophylaxis of diseases, and their use for preparing medicaments for the treatment and/or prophylaxis of diseases.
    Type: Grant
    Filed: November 5, 2014
    Date of Patent: July 4, 2017
    Assignee: Bayer Pharma Aktiengesellschaft
    Inventors: Chantal Fürstner, Jens Ackerstaff, Alexander Straub, Heinrich Meier, Hanna Tinel, Katja Zimmermann, Dmitry Zubov, Jens Schamberger
  • Patent number: 9687486
    Abstract: This invention provides a method of treating a subject suffering from atherosclerosis or a myeloproliferative neoplasm which comprises administering to the subject an amount of a Lyn kinase activator effective to activate Lyn kinase so as to thereby treat the subject.
    Type: Grant
    Filed: December 20, 2013
    Date of Patent: June 27, 2017
    Assignee: THE TRUSTEES OF COLUMBIA UNIVERSITY IN THE CITY OF NEW YORK
    Inventors: Alan R. Tall, Nan Wang
  • Patent number: 9669034
    Abstract: The present invention relates to 4-aryl-N-phenyl-1,3,5-triazin-2-amines containing a sulfoximine group of general formula (I) or (Ia) as described and defined herein, and methods for their preparation, their use for the treatment and/or prophylaxis of disorders, in particular of hyper-proliferative disorders and/or virally induced infectious diseases and/or of cardiovascular diseases. The invention further relates to intermediate compounds useful in the preparation of said compounds of general formula (I) or (Ia).
    Type: Grant
    Filed: May 21, 2012
    Date of Patent: June 6, 2017
    Assignee: BAYER INTELLECTUAL PROPERTY GMBH
    Inventors: Ulrich Lücking, Rolf Bohlmann, Arne Scholz, Gerhard Siemeister, Mark Jean Gnoth, Ulf Bömer, Dirk Kosemund, Philip Lienau, Gerd Rühter, Carsten Schultz-Fademrecht
  • Patent number: 9662303
    Abstract: The present invention provides a compound for treating cancer including an isolated form of dibenzyl trisulfide (DTS) provided in an effective amount to act as an agent against human diseases, including various forms of cancer. The present invention also provides a compound for treating cancer including DTS isolated from Petiveria alliacea L. (guinea hen weed) for providing an effective, potent anti-proliferation and/or cytotoxic activity on a wide range of cancer cell lines. The present invention further provides DTS derivatives (e.g. DTS-albumin complexes) in effective dosage for providing a potent anti-proliferation and/or cytotoxic activity on a wide range of cancer cell lines. Additionally, the present invention provides methods of isolating and/or providing the DTS and/or its derivatives in an effective amount for providing a potent anti-proliferation and/or cytotoxic activity on cancer cell lines.
    Type: Grant
    Filed: May 18, 2007
    Date of Patent: May 30, 2017
    Assignee: PG-Pharma, LLC
    Inventors: Lawrence A.D. Williams, H. George Levy
  • Patent number: 9657001
    Abstract: There is provided compounds of formula I, wherein E1, E2, E3, E4, L1, Y1, Y2, Y3, Ra and z have meanings provided in the description, and pharmaceutically-acceptable salts thereof, which compounds are useful in the treatment of diseases in which inhibition of leukotriene C4 synthase is desired and/or required, and particularly in the treatment of respiratory diseases and inflammation.
    Type: Grant
    Filed: May 4, 2016
    Date of Patent: May 23, 2017
    Assignee: ASTRAZENECA AB
    Inventors: Robert Ronn, Carl Jonas Lindh, Erik Ringberg, Hanna Birgitta Ellinor Andersson, Peter Nilsson, Wesley Ralph Schaal, Magnus Munck af Rosenschöld, Antonios Nikitidis, Grigorios Nikitidis, Petra Johannesson, Christian Tyrchan
  • Patent number: 9649311
    Abstract: Compressed tablets for oral administration containing raltegravir in the form of a pharmaceutically acceptable salt are described. The tablets comprise: (A) an intragranular component comprising (i) an effective amount of an alkali metal salt of raltegravir, (ii) optionally a first superdisintegrant, and (iii) a binder; and (B) an extragranular component comprising (i) a second superdisintegrant, (ii) a filler, and (iii) a lubricant. Methods for preparing the tablets and the use of the tablets, optionally in combination with other anti-HIV agents, for the inhibition of HIV integrase, for the treatment or prophylaxis of HIV infection, or for the treatment, delay in the onset, or prophylaxis of AIDS are also described.
    Type: Grant
    Filed: October 21, 2010
    Date of Patent: May 16, 2017
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Majid Mahjour, Feng Li, Decheng Ma, Sutthilug Sotthivirat
  • Patent number: 9616075
    Abstract: The disclosure relates to a method of treating and/or preventing brain impairment in a subject that has or is susceptible to ammonia neurotoxicity (increased plasma ammonia), by administering a Na-; —K+-2CI- cotransporter isoform 1 (“NKCC1”) inhibitor to the selected subject under conditions effective to treat and/or prevent brain impairment. The disclosure further relates to methods of maintaining the fundamental function of astrocytic potassium buffering and inhibiting accumulation of potassium star rounding astrocytes, both of which involve contacting astrocytes with a NKCC 1 inhibitor.
    Type: Grant
    Filed: March 15, 2013
    Date of Patent: April 11, 2017
    Assignee: University of Rochester
    Inventors: Maiken Nedergaard, Alexander Stanley Thrane, Vinita Rangroo Thrane
  • Patent number: 9540382
    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: June 3, 2013
    Date of Patent: January 10, 2017
    Assignee: Pharmacyclics LLC
    Inventors: Norbert Purro, Mark Smyth, Erick Goldman, David D. Wirth
  • Patent number: 9539221
    Abstract: The use of ?-adrenergic inverse agonists provides a new and highly efficient way of treating a number of pulmonary airway diseases, including asthma, emphysema, and chronic obstructive pulmonary diseases. In general, such a method comprises administering a therapeutically effective amount of a ?-adrenergic inverse agonist to the subject to treat the pulmonary airway disease. Particularly preferred inverse agonists include nadolol and carvedilol.
    Type: Grant
    Filed: October 8, 2004
    Date of Patent: January 10, 2017
    Assignees: EGB ADVISORS, LLC, INVION, INC.
    Inventor: Richard A. Bond
  • Patent number: 9471130
    Abstract: The described embodiments include a computing device with an entity (a processor, a processor core, etc.) and a controller. In these embodiments, the controller, using an idle duration history, predicts a duration of a next idle period for the entity. Based on the predicted duration of the next idle period, the controller configures the entity to operate in a corresponding idle state.
    Type: Grant
    Filed: October 25, 2013
    Date of Patent: October 18, 2016
    Assignee: ADVANCED MICRO DEVICES, INC.
    Inventors: Manish Arora, Nuwan S. Jayasena, Michael J. Schulte
  • Patent number: 9428499
    Abstract: The present disclosure is related to heteroaryl compounds as MEK inhibitors. These compounds include heteroaryl compounds of formula I, their pharmaceutically acceptable salts, combinations with suitable medicament and pharmaceutical compositions thereof. The present disclosure also includes processes of preparation of the compounds and their use in methods of treatment.
    Type: Grant
    Filed: March 11, 2013
    Date of Patent: August 30, 2016
    Assignee: LUPIN LIMITED
    Inventors: Bhavesh Dave, Rakesh Kumar Banerjee, Samiron Phukan, Abhijit Datta Khoje, Rajkumar Hangarge, Jitendra Sambhaji Jadhav, Venkata P. Palle, Rajender Kumar Kamboj
  • Patent number: 9382214
    Abstract: The present invention relates to processes and intermediates for preparing Gonadotropin-Releasing Hormone (GnRH) receptor antagonists of structure (VI); and stereoisomers and pharmaceutically acceptable salts thereof.
    Type: Grant
    Filed: June 19, 2014
    Date of Patent: July 5, 2016
    Assignee: Neurocine Biosciences, Inc.
    Inventors: Donald J. Gallagher, Laszlo R. Treiber, Robert Michael Hughes, Onorato Campopiano, Peng Wang, Yuxin Zhao, Shine K. Chou, Michael Allen Ouellette, Donald Nicholas Hettinger
  • Patent number: 9376450
    Abstract: Heteroaryloxyheterocyclyl compounds, and compositions containing them, and processes for preparing such compounds. Provided herein also are methods of treating disorders or diseases treatable by inhibition of PDE10, such as obesity, non-insulin dependent diabetes, schizophrenia, Huntington's Disease, bipolar disorder, obsessive-compulsive disorder, and the like.
    Type: Grant
    Filed: May 10, 2013
    Date of Patent: June 28, 2016
    Assignee: AMGEN INC.
    Inventors: Jennifer R. Allen, Daniel B. Horne, Essa Hu Harrington, Matthew R. Kaller, Holger Monenschein, Thomas T. Nguyen, Andreas Reichelt, Robert M. Rzasa
  • Patent number: 9370578
    Abstract: The present invention relates to an oral dosage form comprising crystalline lopinavir and crystalline ritonavir. The invention further relates to methods of preparing said oral dosage forms containing the above pharmaceutical active agents.
    Type: Grant
    Filed: March 6, 2013
    Date of Patent: June 21, 2016
    Assignee: ratiopharm GmbH
    Inventors: Dominique Meergans, Konstantin Holfinger
  • Patent number: 9326509
    Abstract: The present invention relates to plant-protecting active ingredient mixtures comprising, as active components, a neonicotinoid and one or two fungicides selected from pyraclostrobin and boscalid, in synergistically effective amounts and to a method of improving the health of plants by to the plants or the locus thereof by applying said mixtures.
    Type: Grant
    Filed: February 20, 2006
    Date of Patent: May 3, 2016
    Assignee: BASF SE
    Inventors: Dirk Voeste, Martin P. Mascianica, Hendrik Ypema, Henry Van Tuyl Cotter