1,2-diazoles (including Hydrogenated) Patents (Class 546/275.4)
  • Patent number: 10806733
    Abstract: Provided are substituted benzaldehydes and derivatives thereof that act as allosteric modulators of hemoglobin, methods and intermediates for their preparation, pharmaceutical compositions comprising the modulators, and methods for their use in treating disorders mediate by hemoglobin and disorders that would benefit from increased tissue oxygenation.
    Type: Grant
    Filed: June 25, 2018
    Date of Patent: October 20, 2020
    Assignee: Global Blood Therapeutics, Inc.
    Inventors: Brian Metcalf, Chihyuan Chuang
  • Patent number: 10807967
    Abstract: Disclosed herein is a method of preparing N-acyl anthranilamide (I), including: reacting a substituted anthranilic acid (II) with pyrazolecarboxylic acid (III) under the action of a phosphorus reagent and a base to obtain an intermediate benzoxazinone (IV); and subjecting the intermediate benzoxazinone (IV) and a protonic acid salt of methylamine to a ring-opening reaction to obtain N-acyl anthranilamide (I), as shown in the following reaction scheme: where X is hydrogen, chloro or cyano group; and HY is hydrohalic acid, sulfuric acid, phosphoric acid or a carboxylic acid. The method has the advantages of simple operation, mild reaction conditions, less waste and high overall yield, and thus is suitable for industrial production.
    Type: Grant
    Filed: November 25, 2019
    Date of Patent: October 20, 2020
    Assignee: MAX (RUDONG) CHEMICALS CO., LTD.
    Inventors: Baochuan Guan, Tianhao Zhang, Qiuju Sheng, Bangchi Chen
  • Patent number: 10793547
    Abstract: Compounds of Formula (I): pharmaceutically acceptable salts thereof, deuterated derivatives of any of the foregoing, and metabolites of any of the foregoing are disclosed. Pharmaceutical compositions comprising the same, methods of treating cystic fibrosis using the same, and methods for making the same are also disclosed. Also disclosed are solid state forms of Compound 1 and salts and solvates thereof.
    Type: Grant
    Filed: December 8, 2017
    Date of Patent: October 6, 2020
    Assignee: Vertex Pharmaceuticals Incorporated
    Inventors: Alexander Russell Abela, Timothy Alcacio, Corey Anderson, Paul Timothy Angell, Minson Baek, Jeremy J. Clemens, Thomas Cleveland, Lori Ann Ferris, Peter Diederik Jan Grootenhuis, Raymond Stanley Gross, Anton V. Gulevich, Sara Sabina Hadida Ruah, Clara Kuang-Ju Hsia, Robert M. Hughes, Pramod Virupax Joshi, Ping Kang, Ali Keshavarz-Shokri, Haripada Khatuya, Paul John Krenitsky, Jason McCartney, Mark Thomas Miller, Prasuna Paraselli, Fabrice Jean Denis Pierre, Yi Shi, Muna Shrestha, David Andrew Siesel, Kathy Stavropoulos, Andreas P. Termin, Fredrick F. Van Goor, Johnny Uy, Timothy John Young, Jinglan Zhou
  • Patent number: 10722502
    Abstract: Disclosed are crystalline free base an solvate forms of 2-hydroxy-6-((2-(1-isopropyl-1H-pyrazol-5-yl)pyridin-3-yl)methoxy)benzaldehyde (or Compound 1), such as the free base Form I, Form II and Material N. Also disclosed are crystalline free base solvates of 2-hydroxy-6-((2-(1-isopropyl-1H-pyrazol-5-yl)pyridin-3-yl)methoxy)benzaldehyde (or Compound 1).
    Type: Grant
    Filed: October 18, 2018
    Date of Patent: July 28, 2020
    Assignee: Global Blood Therapeutics, Inc.
    Inventors: Zhe Li, Stephan D. Parent, Travis Houston
  • Patent number: 10710977
    Abstract: Provided is a novel process for selectively producing the E-geometrical isomer or Z-geometrical isomer of an oximino compound useful as a medicine or agrochemical. In the process, a mixture of geometrical isomers of an oximino compound represented by formula (EZ)-1 is mixed with an acidic compound to produce the E-isomer of the oximo compound represented by the formula (E)-1 or the Z-isomer of the oximino compound represented by the formula (Z)-1 in high yields with high stereoselectivity.
    Type: Grant
    Filed: February 8, 2018
    Date of Patent: July 14, 2020
    Assignee: Nissan Chemical Corporation
    Inventors: Daisuke Tanima, Yoshiyuki Kusuoka, Keisuke Tsuji
  • Patent number: 10689348
    Abstract: The present application relates to the use of heterocyclic compounds for controlling animal pests including arthropods, insects and nematodes, to novel heterocyclic compounds, to processes for their preparation and to intermediates for preparing the heterocyclic compounds.
    Type: Grant
    Filed: August 9, 2019
    Date of Patent: June 23, 2020
    Assignee: Bayer Cropscience AG
    Inventors: Eike Kevin Heilmann, Joerg Greul, Axel Trautwein, Hans-Georg Schwarz, Isabelle Adelt, Roland Andree, Peter Luemmen, Maike Hink, Martin Adamczewski, Mark Drewes, Angela Becker, Arnd Voerste, Ulrich Goergens, Kerstin Ilg, Johannes-Rudolf Jansen, Daniela Portz
  • Patent number: 10577345
    Abstract: Disclosed herein are processes for synthesizing 2-hydroxy-6-((2-(1-isopropyl-1H-pyrazol-5-yl)-pyridin-3-yl)methoxy)benzaldehyde (also referred to herein as Compound (I)) and intermediates used in such processes. Compound (I) binds to hemoglobin and increases it oxygen affinity and hence can be useful for the treatment of diseases such as sickle cell disease.
    Type: Grant
    Filed: August 10, 2018
    Date of Patent: March 3, 2020
    Assignee: Global Blood Therapeutics, Inc.
    Inventors: Zhe Li, Nathan Guz, Yiyang Shao, Julieana Cocuz, Markus Frieser, George Petros Yiannikouros, Liang Liao
  • Patent number: 10538520
    Abstract: Benzamide and nicotinamide compounds and uses of the compounds. The compounds can be used to treat, for example, cancers such hematopoietic cancers (e.g., leukemia).
    Type: Grant
    Filed: October 1, 2018
    Date of Patent: January 21, 2020
    Assignee: OncoTartis Inc.
    Inventors: Alexander Polinsky, Lioubov Korotchkina, Slavoljub Vujcic, Olga Chernova
  • Patent number: 10214508
    Abstract: The present invention provides a compound having a cholinergic muscarinic M1 receptor positive allosteric modulator activity and useful as a medicament such as a prophylactic or therapeutic drug for Alzheimer's disease, schizophrenia, pain, sleep disorder, Parkinson's disease dementia, dementia with Lewy bodies and the like, and the like. The present invention relates to a compound represented by the formula (I) or a salt thereof. wherein each symbol is as described in the attached DESCRIPTION.
    Type: Grant
    Filed: June 11, 2015
    Date of Patent: February 26, 2019
    Assignee: Takeda Pharmaceutical Company Limited
    Inventors: Masaki Ogino, Eiji Kimura, Shinkichi Suzuki, Tomoko Ashizawa, Toshihiro Imaeda, Ikuo Fujimori, Ryosuke Arai
  • Patent number: 10155718
    Abstract: A method for preparing 3-methyl-2-nitrobenzoic acid is disclosed wherein 1,3-dimethyl-2-nitrobenzene is combined with an oxidation catalayst in the presence of an oxygen source and an initiator, provided that less than 99% of the 1,3-dimethyl-2-nitrobenzene is oxidized. A method for preparing compounds of Formula 7 and Formula 11 is also disclosed wherein the method is characterized by using 3-methyl-2-nitrobenzoic acid as prepared by the method disclosed above wherein R1 is C1-C7 alkyl, C3-C6 cycloalkyl or C4-C7 alkylcycloalkyl.
    Type: Grant
    Filed: November 21, 2017
    Date of Patent: December 18, 2018
    Assignee: FMC CORPORATION
    Inventor: Donald J. Dumas
  • Patent number: 10137118
    Abstract: Disclosed are crystalline free base ansolvate forms of 2-hydroxy-6-((2-(1-isopropyl-1H-pyrazol-5-yl)pyridin-3-yl)methoxy)benzaldehyde (or Compound 1), such as the free base Form I, Form II and Material N. Also disclosed are crystalline free base solvates of 2-hydroxy-6-((2-(1-isopropyl-1H-pyrazol-5-yl)pyridin-3-yl)methoxy)benzaldehyde (or Compound 1).
    Type: Grant
    Filed: November 1, 2017
    Date of Patent: November 27, 2018
    Assignee: Global Blood Therapeutics, Inc.
    Inventors: Zhe Li, Stephan D. Parent, Travis Houston
  • Patent number: 10130608
    Abstract: A method of treating or preventing multiple sclerosis includes administering a therapeutically effective amount of a cyclohexane derivative represented by Formula (I): wherein A is a substituent represented by Formula (IIa) or (IIb): R1 and R2 are each independently a hydrogen atom, chlorine atom, C1-C3 haloalkyl, C1-C4 alkyl, C1-C4 alkoxy, or cyano; R3 is a hydrogen atom or chlorine atom; R4 is a fluorine atom, hydroxymethyl, or hydroxyl; R5 and R6 are each independently a hydrogen atom, fluorine atom, C1-C3 haloalkyl, carboxyl, methoxycarbonyl, ethoxycarbonyl, C1-C4 alkoxy, hydroxyl, or C2-C5 alkylcarbonyloxy, or optionally together form oxo; R7 and R8 are each independently a hydrogen atom or fluorine atom; Y is an oxygen atom or sulfur atom; and Z is a nitrogen atom or methine or a pharmaceutically acceptable salt thereof to a mammal.
    Type: Grant
    Filed: April 13, 2017
    Date of Patent: November 20, 2018
    Assignee: Toray Industries, Inc.
    Inventors: Kozue Takagaki, Mie Kaino, Hiroe Hirokawa
  • Patent number: 10077249
    Abstract: Disclosed herein are processes for synthesizing 2-hydroxy-6-((2-(1-isopropyl-1H-pyrazol-5-yl)-pyridin-3-yl)methoxy)benzaldehyde (also referred to herein as Compound (I)) and intermediates used in such processes. Compound (I) binds to hemoglobin and increases it oxygen affinity and hence can be useful for the treatment of diseases such as sickle cell disease.
    Type: Grant
    Filed: May 11, 2017
    Date of Patent: September 18, 2018
    Assignee: Global Blood Therapeutics, Inc.
    Inventors: Zhe Li, Nathan Guz, Yiyang Shao, Julieana Cocuz, Markus Frieser, George Petros Yiannikouros, Liang Liao
  • Patent number: 10034879
    Abstract: Provided are substituted benzaldehydes and derivatives thereof that act as allosteric modulators of hemoglobin, methods and intermediates for their preparation, pharmaceutical compositions comprising the modulators, and methods for their use in treating disorders mediate by hemoglobin and disorders that would benefit from increased tissue oxygenation.
    Type: Grant
    Filed: December 22, 2017
    Date of Patent: July 31, 2018
    Assignee: Global Blood Therapeutics, Inc.
    Inventors: Brian Metcalf, Chihyuan Chuang
  • Patent number: 10029986
    Abstract: Provided is a novel pesticide, particularly a fungicide and a nematicide. An alkynyl pyridine-substituted amide compound represented by formula (I), its N-oxide or a salt thereof, and a pesticide containing it. [In the formula, G1 is a structure represented by G1-1a, G1-3a, G1-27a, etc.; X1 is a halogen atom, difluoromethyl, trifluoromethyl, etc.; Y1 is a halogen atom, etc.; Y2, Y3, R4 and R5 independently represent a hydrogen atom, etc.; R1 is a hydrogen atom, a halogen atom, methyl, methoxy, etc.; R2 is a hydrogen atom, a halogen atom, etc., or R1 and R2 together form an alkylene chain thereby to form a cyclopropyl group together with the carbon atom to which R1 and R2 are bonded, or R1 and R2 together form C1-C2 alkylidene or C1-C2 haloalkylidene; R3 is a hydrogen atom, methyl, etc.; and R6 is C1-C4 alkyl, C3-C6 cycloalkyl, C1-C4 alkoxy(C1-C4)alkyl, etc.
    Type: Grant
    Filed: February 18, 2015
    Date of Patent: July 24, 2018
    Assignee: Nissan Chemical Industries, Ltd.
    Inventors: Takeshi Mita, Motoyoshi Iwasa, Yusuke Nanjo, Taichi Shimomiya, Hidehito Kuwahara, Hotaka Imanaka
  • Patent number: 9988356
    Abstract: The present application provides processes for making pesticidal compounds and compounds useful both as pesticides and in the making of pesticidal compounds.
    Type: Grant
    Filed: September 26, 2017
    Date of Patent: June 5, 2018
    Assignee: Dow AgroSciences LLC
    Inventors: Qiang Yang, Beth Lorsbach, Gregory Whiteker, Gary Roth, Carl DeAmicis, Thomas Clark, Kaitlyn Gray, Belgin Canturk, Elisabeth J. Kane, Yu Zhang, Joseck M. Muhuhi
  • Patent number: 9969717
    Abstract: The present invention relates to a process for preparing substituted anthranilic acid derivatives of the formula (I) in which R1, R2, R3 and R4 are each as defined in the description, by conversion of compounds of the general formula (IV) in the presence of a palladium catalyst and carbon monoxide. The present invention likewise relates to compounds of the general formula (IV).
    Type: Grant
    Filed: April 20, 2017
    Date of Patent: May 15, 2018
    Assignee: Bayer Intellectual Property GmbH
    Inventors: Thomas Himmler, Sergii Pazenok, Frank Volz, Norbert Lui
  • Patent number: 9901095
    Abstract: The present application provides processes for making pesticidal compounds and compounds useful both as pesticides and in the making of pesticidal compounds.
    Type: Grant
    Filed: April 12, 2017
    Date of Patent: February 27, 2018
    Assignee: Dow AgroSciences LLC
    Inventors: Qiang Yang, Beth Lorsbach, Greg Whiteker, Gary Roth, Carl DeAmicis, Thomas Clark, Kaitlyn Gray, Yu Zhang, Joseck M. Muhuhi
  • Patent number: 9896444
    Abstract: The present invention relates to compounds of formula (I): in which Y, Y1, R1, R2, R3 and R4 are defined in the Summary of the Invention; capable of inhibiting the tyrosine kinase enzymatic activity of the Abelson protein (ABL1), the Abelson-related protein (ABL2) and related chimeric proteins, in particular BCR-ABL1. The invention further provides a process for the preparation of compounds of the invention, pharmaceutical preparations comprising such compounds and methods of using such compounds in the treatment of cancers.
    Type: Grant
    Filed: March 21, 2016
    Date of Patent: February 20, 2018
    Assignee: Novartis AG
    Inventors: Pascal Furet, Robert Martin Grotzfeld, Wolfgang Jahnke, Darryl Jones, Paul William Manley, Andreas Marzinzik, Xavier Francois Andre Pelle, Bahaa Salem, Joseph Schoepfer
  • Patent number: 9896430
    Abstract: This disclosure relates to the field of preparation of 3-(3-chloro-1H-pyrazol-1-yl)pyridine and intermediates therefrom. These intermediates are useful in the preparation of certain pesticides.
    Type: Grant
    Filed: April 12, 2017
    Date of Patent: February 20, 2018
    Assignee: Dow AgroSciences LLC
    Inventors: Xiaoyong Li, Qiang Yang, Beth Lorsbach
  • Patent number: 9879029
    Abstract: The present invention provides thieno[2,3-c]pyrrol-4-one compounds that inhibit activity of extracellular-signal-regulated kinase (ERK) and may be useful in the treatment of cancer.
    Type: Grant
    Filed: December 15, 2015
    Date of Patent: January 30, 2018
    Assignee: Eli Lilly and Company
    Inventors: Guillermo S. Cortez, Sajan Joseph, Johnathan Alexander McLean, William Thomas McMillen, Michael John Rodriguez, Gaiying Zhao
  • Patent number: 9862702
    Abstract: The present application provides processes for making pesticidal compounds and compounds useful both as pesticides and in the making of pesticidal compounds.
    Type: Grant
    Filed: April 27, 2017
    Date of Patent: January 9, 2018
    Assignee: Dow AgroSciences LLC
    Inventors: Qiang Yang, Beth Lorsbach, Gary Roth, Noormohamed M. Niyaz, Jeffrey Nissen, Ronald Ross, Jr., Greg Whiteker, Carl DeAmicis, Kaitlyn Gray, Yu Zhang
  • Patent number: 9840490
    Abstract: 3-(3-Chloro-1H-pyrazol-1-yl)pyridine is prepared by cyclizing 3-hydrazinopyridine-dihydrochloride with commercially available 3-ethoxyacrylonitrile to provide 3-(3-amino-1H-pyrazol-1-yl)pyridine, and by converting the amino group to a chloro group by a Sandmeyer reaction.
    Type: Grant
    Filed: December 23, 2016
    Date of Patent: December 12, 2017
    Assignee: Dow AgroSciences LLC
    Inventors: Xiaoyong Li, Qiang Yang, Gary Roth, Beth Lorsbach
  • Patent number: 9796682
    Abstract: The present application provides processes for making pesticidal compounds and compounds useful both as pesticides and in the making of pesticidal compounds.
    Type: Grant
    Filed: December 6, 2016
    Date of Patent: October 24, 2017
    Assignee: Dow AgroSciences LLC
    Inventors: Qiang Yang, Beth Lorsbach, Gregory Whiteker, Gary Roth, Carl DeAmicis, Thomas Clark, Kaitlyn Gray, Belgin Canturk, Elisabeth J. Kane, Yu Zhang, Joseck M. Muhuhi
  • Patent number: 9723839
    Abstract: The present application provides processes for making pesticidal compounds and compounds useful both as pesticides and in the making of pesticidal compounds.
    Type: Grant
    Filed: July 29, 2016
    Date of Patent: August 8, 2017
    Assignee: Dow AgroSciences LLC
    Inventors: Qiang Yang, Beth Lorsbach, Gregory Whiteker, Carl DeAmicis, Joseck M. Muhuhi
  • Patent number: 9661849
    Abstract: The present application provides processes for making pesticidal compounds and compounds useful both as pesticides and in the making of pesticidal compounds.
    Type: Grant
    Filed: August 18, 2015
    Date of Patent: May 30, 2017
    Assignee: Dow AgroSciences LLC
    Inventors: Qiang Yang, Beth Lorsbach, Greg Whiteker, Gary Roth, Carl DeAmicis, Thomas Clark, Kaitlyn Gray, Yu Zhang, Joseck M. Muhuhi
  • Patent number: 9586948
    Abstract: The present invention relates to inhibitors of IRAK4 of Formula (I) and provides compositions comprising such inhibitors, as well as methods therewith for treating IRAK4-mediated or -associated conditions or diseases.
    Type: Grant
    Filed: October 3, 2013
    Date of Patent: March 7, 2017
    Assignee: MERCK SHARP & DOHME CORP.
    Inventors: W. Michael Seganish, Jennifer Hanisak, Guoqing Li, Rui Zhang, Haiqun Tang
  • Patent number: 9580405
    Abstract: The present application provides processes for making pesticidal compounds and compounds useful both as pesticides and in the making of pesticidal compounds.
    Type: Grant
    Filed: May 27, 2016
    Date of Patent: February 28, 2017
    Assignee: Dow AgroSciences LLC
    Inventors: Qiang Yang, Beth Lorsbach, Gregory Whiteker, Gary Roth, Carl DeAmicis, Daniel I. Knueppel, Ann M. Buysse, Kaitlyn Gray, Xiaoyong Li, Joseck M. Muhuhi, Ronald Ross, Jr., David E. Podhorez, Yu Zhang
  • Patent number: 9580403
    Abstract: 3-(3-Chloro-1H-pyrazol-1-yl)pyridine is prepared by cyclizing 3-hydrazinopyridine-dihydrochloride with commercially available 3-ethoxyacrylonitrile to provide 3-(3-amino-1H-pyrazol-1-yl)pyridine, and by converting the amino group to a chloro group by a Sandmeyer reaction.
    Type: Grant
    Filed: January 6, 2016
    Date of Patent: February 28, 2017
    Assignee: Dow AgroSciences LLC
    Inventors: Xiaoyong Li, Qiang Yang, Gary Roth, Beth Lorsbach
  • Patent number: 9572342
    Abstract: A composition comprising a compound of formula (I): in which R1, R2, R3, R4, R5, R6, A, Q and n can have the definitions stated in the description, and at least one biological control agent selected from bacteria, fungi or yeasts, protozoas, viruses, entomopathogenic nematodes, and botanical extracts, or products produced by microorganisms including proteins or secondary metabolites, and optionally an inoculant, for reducing overall damage of plants and plant parts as well as losses in harvested fruits or vegetables caused by insects, nematodes and phytopathogens.
    Type: Grant
    Filed: December 17, 2012
    Date of Patent: February 21, 2017
    Assignee: BAYER INTELLECTUAL PROPERTY GMBH
    Inventors: Rüdiger Fischer, Heiki Hungenberg
  • Patent number: 9573931
    Abstract: 3-(3-Chloro-1H-pyrazol-1-yl)pyridine is prepared by coupling 3-bromopyridine with commercially available 3-aminopyrazole, purifying the 3-(3-amino-1H-pyrazol-1-yl)pyridine by crystallization, and converting the amino group to a chloro group by a Sandmeyer reaction.
    Type: Grant
    Filed: May 3, 2016
    Date of Patent: February 21, 2017
    Assignee: Dow AgroSciences LLC
    Inventors: Qiang Yang, Beth Lorsbach, Carl DeAmicis, Ann Buysse, Ronald Ross, Jr., Xiaoyong Li
  • Patent number: 9540342
    Abstract: The present application provides processes for making pesticidal compounds and compounds useful both as pesticides and in the making of pesticidal compounds.
    Type: Grant
    Filed: January 6, 2016
    Date of Patent: January 10, 2017
    Assignee: Dow AgroSciences LLC
    Inventors: Qiang Yang, Beth Lorsbach, Gregory Whiteker, Gary Roth, Carl DeAmicis, Thomas Clark, Kaitlyn Gray, Belgin Canturk, Elisabeth J. Kane, Yu Zhang, Joseck M. Muhuhi
  • Patent number: 9447048
    Abstract: The present application provides processes for making pesticidal compounds and compounds useful both as pesticides and in the making of pesticidal compounds.
    Type: Grant
    Filed: January 6, 2016
    Date of Patent: September 20, 2016
    Assignee: Dow AgroSciences LLC
    Inventors: Qiang Yang, Beth Lorsbach, Greg Whiteker, Carl DeAmicis, Kaitlyn Gray, Yu Zhang, Joseck M. Muhuhi
  • Patent number: 9434712
    Abstract: The present application provides processes for making pesticidal compounds and compounds useful both as pesticides and in the making of pesticidal compounds.
    Type: Grant
    Filed: January 6, 2016
    Date of Patent: September 6, 2016
    Assignee: Dow AgroSciences LLC
    Inventors: Qiang Yang, Beth Lorsbach, Gary Roth, Noormohamed M. Niyaz, Jeffrey Nissen, Ronald Ross, Jr., Greg Whiteker, Carl DeAmicis, Kaitlyn Gray, Yu Zhang
  • Patent number: 9422265
    Abstract: This disclosure relates to the field of preparation of 3-(3-chloro-1H-pyrazol-1-yl)pyridine and intermediates therefrom. These intermediates are useful in the preparation of certain pesticides.
    Type: Grant
    Filed: August 19, 2015
    Date of Patent: August 23, 2016
    Assignee: Dow AgroSciences LLC
    Inventors: Xiaoyong Li, Qiang Yang, Beth Lorsbach
  • Patent number: 9371310
    Abstract: 3-(3-Chloro-1H-pyrazol-1-yl)pyridine is prepared by coupling 3-bromopyridine with commercially available 3-aminopyrazole, purifying the 3-(3-amino-1H-pyrazol-1-yl)pyridine by crystallization, and converting the amino group to a chloro group by a Sandmeyer reaction.
    Type: Grant
    Filed: March 24, 2015
    Date of Patent: June 21, 2016
    Assignee: Dow AgroSciences LLC
    Inventors: Qiang Yang, Beth Lorsbach, Carl DeAmicis, Ann M. Buysse, Ronald Ross, Jr., Xiaoyong Li
  • Patent number: 9340526
    Abstract: The present invention relates to a process for preparing 1-pyridyl-substituted pyrazoles, comprising the reaction of acetyleneketones with pyridylhydrazine derivatives to give 1-pyridyl-substituted dihydro-1H-pyrazoles, the further reaction thereof with elimination of water to give 1-pyridyl-substituted trihalomethylpyrazoles, and the further processing thereof.
    Type: Grant
    Filed: March 23, 2015
    Date of Patent: May 17, 2016
    Assignee: Bayer Intellectual Property GmbH
    Inventors: Sergii Pazenok, Norbert Lui, Harry Blaschke
  • Patent number: 9328096
    Abstract: The present invention relates to compounds of Formula I and their pharmaceutically acceptable salts, wherein the substituents are as described herein, and their use in medicine, in particular as TrkA antagonists.
    Type: Grant
    Filed: May 6, 2015
    Date of Patent: May 3, 2016
    Assignee: Pfizer Inc.
    Inventors: Sharanjeet Kaur Bagal, Jingrong Jean Cui, Samantha Elizabeth Greasley, Elizabeth Ann Lunney, Indrawan James McAlpine, Asako Nagata, Sacha Ninkovic, Kiyoyuki Omoto, Sarah Elizabeth Skerratt, Robert Ian Storer, Joseph Scott Warmus
  • Patent number: 9260396
    Abstract: The present application provides processes for making pesticidal compounds and compounds useful both as pesticides and in the making of pesticidal compounds.
    Type: Grant
    Filed: May 21, 2015
    Date of Patent: February 16, 2016
    Assignee: Dow AgroSciences LLC
    Inventors: Qiang Yang, Beth Lorsbach, Greg Whiteker, Carl DeAmicis, Kaitlyn Gray, Yu Zhang, Joseck M. Muhuhi
  • Patent number: 9255083
    Abstract: The present application provides processes for making pesticidal compounds and compounds useful both as pesticides and in the making of pesticidal compounds.
    Type: Grant
    Filed: May 21, 2015
    Date of Patent: February 9, 2016
    Assignee: Dow AgroSciences LLC
    Inventors: Qiang Yang, Beth Lorsbach, Gary Roth, Noormohamed M. Niyaz, Jeffrey Nissen, Ronald Ross, Jr., Greg Whiteker, Carl DeAmicis, Kaitlyn Gray, Yu Zhang
  • Patent number: 9255081
    Abstract: 3-(3-Chloro-1H-pyrazol-1-yl)pyridine is prepared by cyclizing 3-hydrazinopyridine.dihydrochloride with commercially available 3-ethoxyacrylonitrile to provide 3-(3-amino-1H-pyrazol-1-yl)pyridine, and by converting the amino group to a chloro group by a Sandmeyer reaction.
    Type: Grant
    Filed: March 24, 2015
    Date of Patent: February 9, 2016
    Assignee: Dow AgroSciences LLC
    Inventors: Xiaoyong Li, Qiang Yang, Gary Roth, Beth Lorsbach
  • Patent number: 9226924
    Abstract: A method treats or prevents neuropathic pain with a synergistically-enhanced analgesic effect at a dose at which a calcium channel ?2? ligand does not produce any side effects as well as which agent does not produce any new side effects on the central nervous system. The therapeutic agent or a prophylactic agent used in the method includes as effective ingredients a cyclohexane derivative or a pharmaceutically acceptable salt thereof or a prodrug thereof, and a calcium channel ?2? ligand.
    Type: Grant
    Filed: December 19, 2014
    Date of Patent: January 5, 2016
    Assignee: Toray Industries, Inc.
    Inventors: Naoki Izumimoto, Hidenori Mochizuki
  • Patent number: 9169214
    Abstract: Disclosed herein are compounds and compositions thereof which find use in increasing stability of proteins particularly proteins that tend to misfold and form aggregates. Also provided herein are methods for using these compounds and compositions for increasing stability of proteins and thereby decreasing aggregate formation by these proteins. Also disclosed herein are heterobifunctional compounds that include a TTR binding compound connected to a targeting moiety via a linker, for use in disrupting PPIs of a target protein.
    Type: Grant
    Filed: March 14, 2013
    Date of Patent: October 27, 2015
    Assignee: The Board of Trustees of the Leland Stanford Junior University
    Inventors: Isabella A. Graef, Mamoun M. Alhamadsheh
  • Patent number: 9156813
    Abstract: This disclosure relates to the field of preparation of 3-(3-chloro-1H-pyrazol-1-yl)pyridine and intermediates therefrom. These intermediates are useful in the preparation of certain pesticides.
    Type: Grant
    Filed: May 21, 2015
    Date of Patent: October 13, 2015
    Assignee: Dow AgroSciences LLC
    Inventors: Xiaoyong Li, Qiang Yang, Beth Lorsbach
  • Patent number: 9150553
    Abstract: The present invention relates to novel carboxamide compounds of the formula I and their use for the manufacture of a medicament. The carboxamide compounds are prodrugs of inhibitors of calpain (calcium dependant cysteine proteases). The invention therefore also relates to the use of these carboxamide compounds for treating a disorder associated with an elevated calpain activity.
    Type: Grant
    Filed: December 29, 2008
    Date of Patent: October 6, 2015
    Assignee: AbbVie Deutschland GmbH & Co. KG
    Inventors: Wilfried Hornberger, Helmut Mack, Andreas Kling, Achim Moeller, Barbara Vogg, Jürgen Delzer, Gisela Backfisch, Armin Beyerbach
  • Patent number: 9115115
    Abstract: 3-(3-chloro-1H-pyrazol-1-yl)pyridine is prepared by cyclizing 3-hydrazinopyridine-•dihydrochloride with a dialkyl maleate to provide an alkyl 5-oxo-2-(pyridin-3-yl)pyrazolidine-3-carboxylate, by chlorinating to provide an alkyl 3-chloro-1-(pyridin-3-yl)-4,5-dihydro-1H-pyrazole-5-carboxylate, by oxidizing to provide an alkyl 3-chloro-1-(pyridin-3-yl)-1H-pyrazole-5-carboxylate, by converting the ester to the carboxylic acid by hydrolysis to provide 3-chloro-1-(pyridin-3-yl)-1H-pyrazole-5-carboxylic acid hydrochloride, and by removing the carboxylic acid by a decarboxylation reaction.
    Type: Grant
    Filed: March 24, 2015
    Date of Patent: August 25, 2015
    Assignee: Dow AgroSciences LLC
    Inventors: Qiang Yang, Beth Lorsbach, David E. Podhorez
  • Patent number: 9108946
    Abstract: The present application provides processes for making pesticidal compounds and compounds useful both as pesticides and in the making of pesticidal compounds.
    Type: Grant
    Filed: October 17, 2014
    Date of Patent: August 18, 2015
    Assignee: Dow AgroSciences LLC
    Inventors: Qiang Yang, Beth Lorsbach, Gregory T. Whiteker, Gary Roth, Carl DeAmicis, Daniel I. Knueppel, Ann M. Buysse, Kaitlyn Gray, Xiaoyong Li, Joseck M. Muhuhi, Ronald Ross, Jr., David E. Podhorez, Yu Zhang
  • Patent number: 9102654
    Abstract: The present application provides processes for making pesticidal compounds and compounds useful both as pesticides and in the making of pesticidal compounds.
    Type: Grant
    Filed: October 17, 2014
    Date of Patent: August 11, 2015
    Assignee: Dow AgroSciences LLC
    Inventors: Qiang Yang, Beth Lorsbach, Gary Roth, Noormohamed M. Niyaz, Jeffrey Nissen, Ronald Ross, Jr., Gregory T. Whiteker, Carl DeAmicis, Kaitlyn Gray, Yu Zhang
  • Patent number: 9102655
    Abstract: The present application provides processes for making pesticidal compounds and compounds useful both as pesticides and in the making of pesticidal compounds.
    Type: Grant
    Filed: October 17, 2014
    Date of Patent: August 11, 2015
    Assignee: Dow AgroSciences LLC
    Inventors: Qiang Yang, Beth Lorsbach, Gregory T. Whiteker, Gary Roth, Carl DeAmicis, Thomas P. Clark, Kaitlyn Gray, Belgin Canturk, Elisabeth J. Kane, Yu Zhang, Joseck M. Muhuhi
  • Patent number: 9085552
    Abstract: This disclosure relates to the field of preparation of 3-(3-chloro-1H-pyrazol-1-yl)pyridine and intermediates therefrom. These intermediates are useful in the preparation of certain pesticides.
    Type: Grant
    Filed: October 17, 2014
    Date of Patent: July 21, 2015
    Assignee: Dow AgroSciences LLC
    Inventors: Xiaoyong Li, Qiang Yang, Beth Lorsbach