Pyrimidines With Chalcogen Bonded Directly To A Ring Carbon Of Said Pyrimidine Moiety Patents (Class 514/269)
  • Patent number: 11406635
    Abstract: Solid pharmaceutical dosage forms comprising (S)-ethyl 2-amino-3-(4-(2-amino-6-((R)-1-(4-chloro-2-(3-methyl-1H-pyrazol-1-yl)phenyl)-2,2,2-trifluoroethoxy)pyrimidin-4-yl)phenyl)propanoate (telotristat) are disclosed, as well as methods of making them and compositions useful in their manufacture.
    Type: Grant
    Filed: November 19, 2019
    Date of Patent: August 9, 2022
    Assignee: TerSera Therapeutics LLC
    Inventors: Jinling Chen, Matthew S. Deaver, Richard J. Holl, Kalyan Nuguru
  • Patent number: 11390605
    Abstract: The invention provides compounds having the general formula I: and pharmaceutically acceptable salts thereof, wherein the variables R1, R2, R3 and R4 have the meaning as described herein, and compositions containing such compounds and methods for using such compounds and compositions.
    Type: Grant
    Filed: August 18, 2017
    Date of Patent: July 19, 2022
    Assignee: ARIZONA BOARD OF REGENTS ON BEHALF OF ARIZONA STATE UNIVERSITY
    Inventors: Sidney Hecht, Omar Khdour, Arnaud Chevalier
  • Patent number: 11291641
    Abstract: Embodiments herein disclose methods relating to diabetic nephropathy (DN); methods for preventing the onset and also for preventing the progressing of DN, as well as the treatment of DN in diabetic subjects comprising administering reparixin and/or ladarixin which are inhibitors of CXCL8 receptor CXCR1 and CXCR2 activation.
    Type: Grant
    Filed: October 3, 2017
    Date of Patent: April 5, 2022
    Assignees: THE CHILDREN'S MEDICAL CENTER CORPORATION, DOMPE FARMACEUTICI S.P.A.
    Inventors: Paolo Fiorina, Roberto Bassi, Andrea Vergani, Marcello Allegretti
  • Patent number: 11254645
    Abstract: The present disclosure relates to a method for preparing tolimidone on large scale with maintaining high purity and uniform particle size distribution, and more specifically, a method suitable for preparing tolimidone on industrially large scale by using tetrabutyl ammonium bromide catalyst and recrystallization in ethanol, which can prepare highly pure tolimidone in a time shorter than prior arts while maintaining water content and particle size distribution constantly.
    Type: Grant
    Filed: January 11, 2018
    Date of Patent: February 22, 2022
    Assignee: BUKWANG PHARMACEUTICAL CO., LTD.
    Inventors: Kwang Ok Lee, Kyung Hwa Lee, Eun Ju Jeong
  • Patent number: 11234914
    Abstract: The present invention relates to the use of monosubstiuted urea derivatives of the formula I as self-tanning substance, for increasing melanin synthesis, for improving melanin transport and/or improving the distribution of melanin in suprabasal layers, and to preparations comprising these urea derivatives.
    Type: Grant
    Filed: October 2, 2017
    Date of Patent: February 1, 2022
    Assignee: MERCK PATENT GMBH
    Inventors: Julian Osthoff, Hansjuergen Driller, Christophe Carola, Robin Back, Michael Krohn
  • Patent number: 11219213
    Abstract: A fungicidal composition comprising active components A and B, wherein the active component A is benzisothiazolinone, and the active component B is flutriafol; and the weight ratio of the two components is 1:30-30:1. Also provided are a preparation method and use of the composition. Test results show that the fungicidal composition provided in the present invention has an obvious synergistic effect, and more importantly, the application rate is reduced and the cost is reduced. The fungicidal composition is effective in controlling certain specific fungal diseases of the crops. Through the combination of different fungicides with different mechanisms and modes of action, the application rate of each single agent is effectively reduced, and a good effect on broadening the fungicidal spectrum, retarding the fungal resistance and improving the control effect is exhibited.
    Type: Grant
    Filed: August 8, 2016
    Date of Patent: January 11, 2022
    Assignee: ADAMA HUIFENG (JIANGSU), LTD.
    Inventors: Hangen Zhong, Hongjin Ji
  • Patent number: 11207307
    Abstract: Suspensions of pump inhibitors (PPIs) are disclosed. The suspension may include a PPI, a copolymer of ethylene oxide and propylene oxide; simethicone emulsion; Sodium Bicarbonate; and Sodium Citrate, USP (Dihydrate). The suspensions have desirable viscosities and enhanced stability.
    Type: Grant
    Filed: June 16, 2017
    Date of Patent: December 28, 2021
    Assignee: AZURITY PHARMACEUTICALS, INC.
    Inventors: Ken Fallin, Kaity Renaud, Peter Mione, Neal Muni, Anisa Gandhi
  • Patent number: 11207278
    Abstract: The present disclosure relates to compositions and methods for the diagnosis and treatment or prevention of proteinopathies, particularly MUC1-associated kidney disease (ADTKD-MUC1 or MKD), Retinitis Pigmentosa (e.g., due to rhodopsin mutations), autosomal dominant tubulo-interstitial kidney disease due to UMOD mutation(s) (ADTKD-UMOD), and other forms of toxic proteinopathies resulting from mutant protein accumulation in the ER or other secretory pathway compartments and/or vesicles, among others. The disclosure also identifies and provides TMED9-binding agents as capable of treating or preventing proteinopathies of the secretory pathway, and further provides methods for identifying additional TMED9-binding agents.
    Type: Grant
    Filed: January 28, 2021
    Date of Patent: December 28, 2021
    Assignees: The Broad Institute, Inc., Dana-Farber Cancer Institute, Inc., The Brigham and Women's Hospital, Inc.
    Inventors: Anna Greka, Moran Dvela-Levitt, Maria Alimova, Eric Lander, Todd R. Golub, Florence Wagner, Brian Chamberlain, Valeria Padovano, Joseph Growney
  • Patent number: 11172684
    Abstract: Provided is the use of or compositions or formulations comprising Burkholderia species, filtrate, supernatant, extract, pesticidally active compound or metabolite derived therefrom as an insecticide, particularly against infestation of Corn Rootworm larvae, and/or as crop yield enhancer.
    Type: Grant
    Filed: November 1, 2018
    Date of Patent: November 16, 2021
    Assignee: MARRONE BIO INNOVATIONS, INC.
    Inventors: Ratnakar Asolkar, Marja Koivunen, Pamela G. Marrone, Ana-Lucia Cordova-Kreylos, Huazhang Huang
  • Patent number: 11136309
    Abstract: Provided are compounds having metalloenzyme modulating activity, and methods of treating diseases, disorders or symptoms thereof mediated by such metalloenzymes.
    Type: Grant
    Filed: January 17, 2020
    Date of Patent: October 5, 2021
    Assignee: PHASEBIO PHARMACEUTICALS, INC.
    Inventors: Steven Sparks, Christopher M. Yates, Sammy R. Shaver
  • Patent number: 11040041
    Abstract: The present invention is concerned with the treatment of Pulmonary Arterial Hypertension (PAH) by administering Paliperidone. The instant invention further relates to use of a pharmaceutical composition comprising Paliperidone, for the treatment of PAH.
    Type: Grant
    Filed: January 22, 2020
    Date of Patent: June 22, 2021
    Assignee: Cipla (UK) Limited
    Inventors: Karl Roberts, Geena Malhotra, Dhiraj Abhyankar, Kalpana Joshi, Jeevan Ghosalkar
  • Patent number: 11034659
    Abstract: Cystic fibrosis is developed through mutation of Cystic Fibrosis Transmembrane conductance Regulator (CFTR), which is one type of chloride channel. An object of the present invention is to provide compounds effective in the treatment of cystic fibrosis that open a chloride channel different from CFTR, which is the cause of the disease, and do not depend on CFTR. Compounds of the present invention are compounds or pharmaceutically acceptable salts thereof that open calcium dependent chloride channels (CaCCs) via G-protein coupled receptor 39 (GPR39) agonism to have strong chloride ion-secretory action, and are represented by the following general formula (I): General formula (I): wherein, X represents a carboxyl group or a tetrazolyl group; Q represents a C1-C3 alkylene group, an oxygen atom, a sulfur atom, etc.; G represents a phenyl group where the phenyl group may have 1 to 3 substituents independently selected from the group consisting of a halogen atom, a cyano group, a C1-C6 alkyl group, etc.
    Type: Grant
    Filed: December 26, 2017
    Date of Patent: June 15, 2021
    Assignee: Daiichi Sankyo Company, Limited
    Inventors: Yasuyuki Takeda, Yamato Suzuki, Toshiharu Noji, Hidenobu Murafuji, Satoshi Muneoka, Hidekazu Inoue, Bitoku Takahashi, Rie Inaba
  • Patent number: 11033548
    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 27, 2019
    Date of Patent: June 15, 2021
    Assignee: Melior Pharmaceuticals I, Inc.
    Inventors: Andrew G. Reaume, Michael S. Saporito
  • Patent number: 11014909
    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), Parkinson's disease and chronic apathy.
    Type: Grant
    Filed: May 21, 2020
    Date of Patent: May 25, 2021
    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: 10988710
    Abstract: Surfactants of the general formula (I) in which R1 is a linear or branched akyl radical having 6 to 20, especially 10 to 16 C atoms, R2 and R3 independently of one another are H or H3CO, and M is hydrogen, an alkali metal or a moiety N+R4R5R6, in which R4, R5 and R6 independently of one another are hydrogen, an alkyl group having 1 to 6 C atoms or a hydroxyalkyl group having 2 to 6 C atoms, are readily incorporated into laundry detergents or cleaning products, possess outstanding performance qualities and can be prepared on the basis of renewable raw materials.
    Type: Grant
    Filed: February 2, 2018
    Date of Patent: April 27, 2021
    Assignees: Henkel AG & Co. KGaA, Studiengesellschaft Kohle mbH
    Inventors: Christian Kropf, Alexander Schulz, Hendrik Hellmuth, Roberto Rinaldi, Hebert Jesus Estevez Rivera
  • Patent number: 10980777
    Abstract: The present application relates to compounds of formula (I), wherein A, R, R1, and R2 are as defined in the specification, pharmaceutical compositions containing such compounds and to their use in therapy.
    Type: Grant
    Filed: August 17, 2018
    Date of Patent: April 20, 2021
    Assignee: Istituto Europeo di Oncologia S.r.l.
    Inventors: Mario Varasi, Anna Cappa, Paola Vianello, Loris Moretti, Luca Sartori, Ciro Mercurio
  • Patent number: 10959431
    Abstract: The present invention relates to pesticidal mixtures comprising 4-[5-(3,5-dichlorophenyl)-5-(trifluoromethyl)-4H-isoxazol-3-yl]-N-[(4R)-2-ethyl-3-oxo-isoxazolidin-4-yl]-2-methyl-benzamide or 4-[5-(3,5-dichloro-4-fluoro-phenyl)-5-(trifluoromethyl)-4H-isoxazol-3-yl]-N-[(4R)-2-ethyl-3-oxo-isoxazolidin-4-yl]-2-methyl-benzamide as compound I; and 2) one fungicidal compound II, wherein compound II is selected from the group consisting of pydiflumetofen, N-[(5-chloro-2-isopropyl-phenyl)methyl]-N-cyclopropyl-3-(difluoromethyl)-5-fluoro-1-methyl-pyrazole-4-carboxamide, mefentrifluconazole, picarbutrazox, oxathiapiproline, 2-{3-[2-(1-{[3,5-bis(difluoromethyl-1H-pyrazol-1-yl]acetyl}piperidin-4-yl)-1,3-thiazol-4-yl]-4,5-dihydro-1,2 oxazol-5-yl}phenyl methanesulfonate, 2-{3-[2-(1-{[3,5-bis(difluoromethyl)-1H-pyrazol-1-yl]acetyl}piperidin-4-yl)-1,3-thiazol-4-yl]-4,5-dihydro-1,2-oxazol-5 yl}-3-chlorophenyl methanesulfonate, N?-(2,5-dimethyl-4-phenoxy-phenyl)-N-ethyl-N-methyl-formamidine, N?-[4-(4,5-dichlorothiazol-2-yl)oxy-
    Type: Grant
    Filed: October 4, 2017
    Date of Patent: March 30, 2021
    Assignee: BASF SE
    Inventor: Markus Gewehr
  • Patent number: 10940151
    Abstract: The invention features methods for treating or reducing the likelihood of developing a renal disease by administering to a subject in need thereof an agent that decreases expression of a pathogenic APOL1. The agents of the method target various signaling pathways and decrease the level of the pathogenic APOL1 polypeptide.
    Type: Grant
    Filed: November 2, 2018
    Date of Patent: March 9, 2021
    Assignee: Beth Israel Deaconess Medical Center, Inc.
    Inventors: David J. Friedman, Martin R. Pollak
  • Patent number: 10933054
    Abstract: Provided herein are methods and compositions for treating cancers, inflammatory diseases, rasopathies, and fibrotic disease involving aberrant Ras superfamily signaling through the binding of compounds to the GTP binding domain of Ras superfamily proteins including, in certain cases, K-Ras and mutants thereof, and a novel method for assaying such compositions.
    Type: Grant
    Filed: October 16, 2019
    Date of Patent: March 2, 2021
    Assignee: Shy Therapeutics LLC
    Inventors: Yaron R. Hadari, Luca Carta, Michael Schmertzler, Theresa M. Williams, Charles H. Reynolds, Rebecca Hutcheson
  • Patent number: 10919896
    Abstract: The present invention relates to compounds of formula (I), and salts and solvates thereof, that function as inhibitors of cell division cycle 7 (Cdc7) kinase enzyme activity: wherein X, R1, R2, and n are each as defined herein. The present invention also relates to processes for the preparation of these compounds, to pharmaceutical compositions comprising them, and to their use in the treatment of proliferative disorders, such as cancer, as well as other diseases or conditions in which Cdc7 kinase activity is implicated.
    Type: Grant
    Filed: September 22, 2017
    Date of Patent: February 16, 2021
    Assignee: Cancer Research Technology Limited
    Inventors: Emma L. Carswell, Mark David Charles, Anne Cochi, Benjamin J. Dugan, Chukuemeka Tennyson Ekwuru, Fred Elustondo, Katherine M. Fowler, Frederic Georges Marie Leroux, Nathaniel J. T. Monck, Gregory R. Ott, Jonathan R. Roffey, Gurwinder Sidhu, Neil Tremayne
  • Patent number: 10875832
    Abstract: The present teachings relate to hydroxypyrimidinone derivatives of Formula II, pharmaceutical compositions thereof, and methods of using such compounds to treat bacterial infections.
    Type: Grant
    Filed: July 15, 2019
    Date of Patent: December 29, 2020
    Assignee: FORGE THERAPEUTICS, INC.
    Inventors: Min Teng, Baskar Nammalwar, Konstantin Taganov, David T. Puerta
  • Patent number: 10844064
    Abstract: The present patent application discloses at least the compounds according to Formula I? shown below, or pharmaceutically acceptable salts thereof, wherein ring D, ring A, ring E, JB, n, JD, J, X, Z, Z1, RC1, RC2, Y, R9, o and W are as defined herein.
    Type: Grant
    Filed: September 16, 2015
    Date of Patent: November 24, 2020
    Assignee: Cyclerion Therapeutics, Inc.
    Inventors: Glen Robert Rennie, Nicholas Perl, Ara Mermerian, Joon Jung, Lei Jia, Rajesh R. Iyengar, G-Yoon Jamie Im, Timothy Claude Barden, James Edward Sheppeck, Paul Allan Renhowe, Takashi Nakai, Thomas Wai-Ho Lee, Karthik Iyer
  • 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: 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: 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: 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: 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: 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