Pyrimidines With Chalcogen Bonded Directly To A Ring Carbon Of Said Pyrimidine Moiety Patents (Class 514/269)
  • 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: 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: 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
  • Patent number: 9315493
    Abstract: The present invention provides: a compound represented by general formula (I) below, that has both angiotensin II receptor antagonism and a PPAR? activation effect and that is useful as a preventative and/or therapeutic agent for high blood pressure, cardiac disease, arteriosclerosis, type-2 diabetes, and the like; and a drug composition containing the compound. General formula (I) (in the formula: ring A represents a pyridine ring; ring B represents a tetrazole ring or an oxadiazol-5(4H)-one ring; X represents C—R5 or a nitrogen atom; R1 represents an alkyl group; R2 represents an alkyl group or a cycloalkyl group; and R3, R4, and R5 each independently represents a hydrogen atom, a halogen atom, an alkyl group, an alkoxy group or similar.
    Type: Grant
    Filed: March 13, 2012
    Date of Patent: April 19, 2016
    Assignee: KOWA COMPANY, LTD.
    Inventors: Toru Miura, Seiichi Sato, Hajime Yamada, Junya Tagashira, Toshiaki Watanabe, Ryohei Sekimoto, Rie Ishida, Hitomi Aoki, Tadaaki Ohgiya
  • Patent number: 9315521
    Abstract: The present invention features compounds having the Formula (Ia) and (Ib) (e.g., a compound of any of Formulas ((Ia-2)-(Ia-21)), including other tautomers, stereoisomers, E/Z stereoisomers, prodrugs, pharmaceutically acceptable salts, and compositions thereof. The invention also features methods for treating or preventing pain (e.g., neuropathic pain), inflammation, or epilepsy in a patient by administering an effective amount of a compound of Formula (Ia) or (Ib). The invention also features a method for treating or preventing pain (e.g., neuropathic pain), inflammation, or epilepsy in a patient that includes administering to a patient in need thereof an effective amount of a compound of Formula (IIa) or (IIb) (e.g., a compound of any of Formulas ((IIa-2)-(IIa-6)). The compounds described herein (e.g., a compound of Formulas (Ia), (Ib), (IIa), or (IIb)) can also be used as anticonvulsants.
    Type: Grant
    Filed: April 22, 2015
    Date of Patent: April 19, 2016
    Assignee: Université Laval
    Inventors: Giorgio Attardo, Sasmita Tripathy, Martin Gagnon
  • Patent number: 9241939
    Abstract: The invention relates to a pharmaceutical combination which comprises (a) a phosphoinositide 3-kinase inhibitor compound and (b) a compound which modulates the Ras/Raf/Mek pathway for the treatment of a proliferative disease, especially a solid tumor disease; a pharmaceutical composition comprising such a combination; the use of such a combination for the preparation of a medicament for the treatment of a proliferative disease; a commercial package or product comprising such a combination as a combined preparation for simultaneous, separate or sequential use; and to a method of treatment of a warm-blooded animal, especially a human.
    Type: Grant
    Filed: December 19, 2014
    Date of Patent: January 26, 2016
    Assignee: Novartis AG
    Inventors: Carlos Garcia-Echeverria, Sauveur-Michel Maira, Darrin Stuart, Susan Wee, Christine Fritsch, Tobi Nagel
  • Patent number: 9216959
    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: February 18, 2014
    Date of Patent: December 22, 2015
    Assignee: Melior Pharmaceuticals I, Inc.
    Inventors: Andrew G. Reaume, Michael S. Saporito
  • Patent number: 9167815
    Abstract: A composition having a stable and high fungicidal effect against a cultivated crop infected by a plant pathogen is provided. An agricultural or horticultural fungicide composition containing, as active ingredients, (a) fluazinam or its salt and (b) a strobilurin compound or its salt is provided; in addition, a method for controlling a plant pathogen by applying the subject agricultural or horticultural fungicide composition to a plant or a soil is provided; and furthermore, a method for controlling a plant pathogen by applying (a) fluazinam or its salt and (b) a strobilurin compound or its salt to a plant or a soil is provided.
    Type: Grant
    Filed: May 25, 2012
    Date of Patent: October 27, 2015
    Assignee: ISHIHARA SANGYO KAISHA, LTD.
    Inventors: Koji Sugimoto, Takanori Suzuki, Koudai Yamamoto
  • Patent number: 9168291
    Abstract: ?-mannosylceramides or salts or solvates thereof in a pharmaceutically acceptable carrier, for use as a Type I NKT cell agonist in conjunction with a therapeutically effective amount of ?-galactosylceramide or a salt or a solvate thereof, and/or at least one or more T-cell co-stimulatory molecules, disclosed. Compositions comprising ?-mannosylceramide, as well as methods of treatment of tumors are also provided.
    Type: Grant
    Filed: August 7, 2014
    Date of Patent: October 27, 2015
    Assignees: The United States of America, as represented by the Secretary, Department of Health and Human Services, The University of Birmingham
    Inventors: Jay A. Berzofsky, Jessica J. O'Konek, Masaki Terabe, Petr A. Illarionov, Gurdyal S. Besra
  • Patent number: 9156817
    Abstract: Compounds of Formula (I) promote axonal outgrowth angiogenesis and can therefore be used to reduce central nerve injuries such as head injury and spinal cord injury, cerebral infarction, ischemic heart diseases, peripheral arterial occlusive diseases, or after-effects of these diseases. in which Nx group is preferably a 6-membered aromatic ring containing two nitrogen atoms; R0, R1 and R2 are each independently a hydrogen atom, an alkyl group, or an amino group; E is an oxygen atom or an —NR8 group (wherein R8 is an alkyl group or the like); n is an integer of 0 to 5; X and Y are each a connecting bond, a cycloalkyl group, or —CO—; and Q is a hydrogen atom or a phenyl group.
    Type: Grant
    Filed: July 22, 2014
    Date of Patent: October 13, 2015
    Assignee: DAIICHI SANKYO COMPANY, LIMITED
    Inventors: Naohiro Takemoto, Kenji Murata, Norihito Murayama, Chikaomi Yamada
  • Patent number: 9145374
    Abstract: The present invention relates to methods of inhibiting shikimate pathway, comprising administering to a subject a pharmaceutically acceptable composition comprising a compound having a formula: or pharmaceutically acceptable salts thereof.
    Type: Grant
    Filed: January 10, 2014
    Date of Patent: September 29, 2015
    Assignee: NATIONAL TSING HUA UNIVERSITY
    Inventors: Wen-Ching Wang, Shih-Ching Chou, Ming-Hua Hsu
  • Patent number: 9139518
    Abstract: A compound of the formula (I): a pharmaceutically acceptable salt or solvate thereof, where R1 is optionally substituted lower alkyl, Y is —S(O)2—, R2 is hydrogen or optionally substituted lower alkyl, R7 is hydrogen or optionally substituted lower alkyl, X is a group of the formula: where R5 and R6 are each independently hydrogen, a group of the formula: is optionally substituted cycloalkylene, p is 0, and q is 1 or 2, Z is optionally substituted carbocyclyl or optionally substituted heterocyclyl, and provided that a compound wherein Z is fused heterocyclyl consisting of three rings or optionally substituted pyrimidinyl is excluded.
    Type: Grant
    Filed: June 25, 2010
    Date of Patent: September 22, 2015
    Assignee: SHIONOGI & CO., LTD.
    Inventors: Takayuki Okuno, Naoki Kouyama, Masahiro Sakagami
  • Patent number: 9139564
    Abstract: Compound of Table I are described. They are useful as stimulators of sGC, particularly NO-independent, heme-dependent stimulators. These compounds may be useful for treating, preventing or managing various disorders that are herein disclosed.
    Type: Grant
    Filed: December 26, 2012
    Date of Patent: September 22, 2015
    Assignee: IRONWOOD PHARMACEUTICALS, INC.
    Inventors: Charles Kim, Takashi Nakai, Joel Moore, Nicholas Robert Perl, G-yoon Jamie Im, Timothy Claude Barden, Rajesh R. Iyengar, Daniel P. Zimmer, Angelika Fretzen, Paul Allan Renhowe