Patents Examined by Valerie Rodriguez-Garcia
  • 5-aryl-1H-pyrrole-3-carbonitrile and a pharmaceutical product using the same
    Patent number: 10173977
    Abstract: The present invention provides a production method of a sulfonylpyrrole compound useful as a pharmaceutical product, a production method of an intermediate used for the method, and a novel intermediate. The present invention relates to a method of producing sulfonylpyrrole compound (VIII), which includes reducing compound (III) and hydrolyzing the reduced product to give compound (IV), subjecting compound (IV) to a sulfonylation reaction to give compound (VI), and subjecting compound (VI) to an amination reaction.
    Type: Grant
    Filed: January 13, 2016
    Date of Patent: January 8, 2019
    Assignee: Takeda Pharmaceutical Company Limited
    Inventors: Tomomi Ikemoto, Hideya Mizufune, Toshiaki Nagata, Misayo Sera, Naohiro Fukuda, Takeshi Yamasaki
  • Process for preparing amines
    Patent number: 10167255
    Abstract: The present invention refers to a process for preparing amines comprising reacting a compound of the formula R1—CO—R2 comprising a carbonyl moiety with a amine compound of the formula HNR3R4 and carbon monoxide in the presence of a catalyst.
    Type: Grant
    Filed: December 10, 2013
    Date of Patent: January 1, 2019
    Assignee: STUDIENGESELLSCHAFT KOHLE MBH
    Inventors: Benjamin List, Denis Alexandrovich Chusov
  • Derivatives of korormicin useful as antibiotics
    Patent number: 10166213
    Abstract: An antibiotic compound is of formula (I): R1-R3, R5 and R6 are independently selected from H, alkyl group, substituted alkyl group, halogen, OH, NH2, or SH; R4 is H, alkyl group or substituted alkyl group. X1-X2 are independently selected from O, S, NH, H, alkyl, halogen, OH, SH, or NH2. Y is an acyclic hydrocarbon chain having 4 to 20 carbon atoms or a substituted acyclic hydrocarbon chain having 4 to 20 carbon atoms, but does not include an oxygen atom. Z is CH3 or any neutral or positively charged group. The compound can also be a salt or stereoisomer of formula (I). The compounds are useful in treating bacterial diseases.
    Type: Grant
    Filed: April 22, 2016
    Date of Patent: January 1, 2019
    Inventors: Pavel Dibrov, Elena Dibrov, Grant Pierce
  • Compositions comprising thienopyrimidine and thienopyridine compounds and methods of use thereof
    Patent number: 10160769
    Abstract: The present disclosure relates generally to thienopyrimidine and thienopyridine compounds and methods of use thereof. In particular embodiments, the present disclosure provides compositions comprising thienopyrimidine and thienopyridine compounds of Formula 3: and methods of use to inhibit the interaction of menin with MLL1, MLL2 and MLL-fusion oncoproteins.
    Type: Grant
    Filed: October 18, 2016
    Date of Patent: December 25, 2018
    Assignee: The Regents of the University of Michigan
    Inventors: Jolanta Grembecka, Tomasz Cierpicki, Dmitry Borkin, Jay L. Hess, Duxin Sun, Xiaoqin Li, Kevin Greenman, Mohamed Ibrahim, Artem Plekhov
  • Crystalline arylalkylamine compound and process for producing the same
    Patent number: 10144708
    Abstract: The present invention provides novel crystal forms of arylalkylamine compounds. Specifically, the novel crystal forms of 4-(3S-(1R-(1-naphthyl)ethylamino)pyrrolidin-1-yl)phenylacetic acid have excellent stability and therefore are useful as pharmaceutical ingredients. The present invention also provides industrially advantageous processes for producing the arylalkylamine compounds.
    Type: Grant
    Filed: March 30, 2017
    Date of Patent: December 4, 2018
    Assignee: MITSUBISHI TANABE PHARMA CORPORATION
    Inventors: Hiroshi Miyazaki, Takao Komasaka, Joji Tsurumoto, Takeshi Uemura, Yuuji Morita
  • Process for the preparation of Verapamil hydrochloride
    Patent number: 10144703
    Abstract: A process for the preparation of 5-(3,4-dimethoxyphenylethyl) methyl-amino-2-(3,4-dimethoxyphenyl)-2-isopropyl valeronitrile, which is known as Verapamil is described. A process for improving the purity of verapamil and therefore of its hydrochloride represented as the compound of formula I, by efficient removal of the impurities formed, affording a product of purity greater than 99% is described.
    Type: Grant
    Filed: May 10, 2016
    Date of Patent: December 4, 2018
    Assignee: PIRAMAL ENTERPRISES LIMITED
    Inventors: Dhileep Kumar Krishnamurthy, Milind Gharpure, Narender Rao Somisetti, Murali Rajappa, Rajshekar Aareddy, Damodhar Kasireddy
  • Method for the phosgenation of compounds comprising hydroxyl, thiol, amino and/or formamide groups
    Patent number: 10118145
    Abstract: A method of reacting phosgene with a second compound containing one or more of hydroxyl, thil, amino and/or formamide groups, wherein phosgene has a GHS hazard identification of GHS06 and is obtainable from the reaction of carbon monoxide and chlorine and wherein the second compound is capable of a chemical reaction with phosgene is provided.
    Type: Grant
    Filed: August 18, 2015
    Date of Patent: November 6, 2018
    Assignee: BAYER AKTIENGESELLSCHAFT
    Inventors: Jens Stefan Roggan, Leslaw Mleczko, Konstantinos Metaxas, Michael Gottfried, Ilja Peckermann, Stephan Schubert, Ekkehard Barth
  • P-toluenesulfonate for MEK kinase inhibitor, and crystal form thereof and preparation method therefor
    Patent number: 10118911
    Abstract: Disclosed are a p-toluenesulfonate of a MEK kinase inhibitor, and a crystal form thereof and a preparation method thereof. Specifically disclosed are a 2-((2-fluorine-4-iodophenyl)amino)-1-methyl-4-((6-methylpyridine-3-group)oxygroup)-6-carbonyl-1,6-dihydropyridine-3-formamide p-toluenesulfonate (a compound represented by formula (I)), a crystal form I, and a preparation method thereof. The obtained crystal form I of the compound of formula (I) has good crystal form stability and chemical stability, and the crystallization solvent used has low toxicity and low residue, and is more suitable for use in clinical treatment.
    Type: Grant
    Filed: March 8, 2016
    Date of Patent: November 6, 2018
    Assignee: Jiangsu Hengrui Medicine Co., Ltd.
    Inventors: Guaili Wu, Xiaohui Gao, Lin Bian, Junlei Jia
  • Process for the preparation of saroglitazar pharmaceutical salts
    Patent number: 10112898
    Abstract: The present invention relates to an improved process for the preparation of pyrroles derivatives having hypolipidemic and hypocholesteremic activities. In particular, the invention relates to an improved process for the preparation of 2-ethoxy-3-(4-(2-(2-methyl-5-(4-(methylthio)phenyl)-1H-pyrrol-1-yl)ethoxy)phenyl)propanoate and its pharmaceutically acceptable salts, hydrates, solvates, polymorphs or intermediates thereof. The invention also relates to an improved process for the preparation of mesylate compound (A1).
    Type: Grant
    Filed: September 5, 2014
    Date of Patent: October 30, 2018
    Assignee: Cadila Healthcare Limited
    Inventors: Shri Prakash Dhar Dwivedi, Ramesh Chandra Singh, Jagdish Maganlal Patel, Vikas Patel, Vishwadeepak Rama Pati Tripathi, Pranav Jitendra Gangwar, Jigar Mukundbhai Raval
  • N-hydroxybenzamides as HDAC inhibitors for the treatment of parasitic diseases
    Patent number: 10106493
    Abstract: Compounds of formula wherein n is 0, 1 or 2; X is and Ar is a benzyl substituted at the meta position by a C1 to C8 alkoxy group, or a pharmaceutically acceptable salt thereof, for treating, preventing or inhibiting a parasitic disease, such as toxoplasmosis, in a subject are provided. Methods for preparing the compounds are also presented.
    Type: Grant
    Filed: July 17, 2014
    Date of Patent: October 23, 2018
    Assignees: INSTITUT DE RECHERCHE POUR LE DEVELOPPEMENT (I.R.D.), UNIVERSITE DE MONTPELLIER, CENTRE NATIONAL DE LA RECHERCHE SCIENTIFIQUE
    Inventors: Denis Sereno, Gilles Labesse, Jean-Francois Alexandre Guichou, Corinne Loeuillet, Deborah Isabelle Garcia, Stephane Delbecq
  • Substituted pyrimidine compounds as phosphatidylinositol 3-kinase delta inhibitor and use thereof
    Patent number: 10077258
    Abstract: The present invention belongs to the field of medicinal chemistry, and relates to substituted pyrimidine compounds as phosphatidylinositol 3-kinase (PI3K) ? inhibitor and a use thereof. In particular, the present invention provides a compound as shown by formula I or an isomer, pharmaceutically acceptable salt, solvate or prodrug thereof, the preparation methods of same and pharmaceutical compositions containing these compounds and a use of these compounds or compositions for treating cancer, hyperblastosis diseases or inflammatory diseases. The compounds of the present invention have a good inhibiting activity on PI3K? and have a high selectivity. It is hoped that these will be therapeutic agents for cancer, hyperblastosis diseases or inflammatory diseases.
    Type: Grant
    Filed: March 4, 2016
    Date of Patent: September 18, 2018
    Assignee: NANJING SANHOME PHARMACEUTICAL CO., LTD.
    Inventors: Yong Wang, Xiaorong Liu, Dandan Huang, Yan Zhang, Yumei Kai
  • Thieno-indole moieties and methods of treating using the same
    Patent number: 10071074
    Abstract: The present invention relates to a novel class of alkylating agents comprising a thieno-indole moiety linked to a DNA-binding moiety, which have cytotoxic activity and are useful in treating diseases such as cancer, cellular proliferation disorders and viral infections. The present invention also provides methods for preparing these compounds, pharmaceutical compositions comprising them and methods of treating diseases utilizing such compounds or the pharmaceutical composition containing them. The invention also relates to the use of this novel class of alkylating agents in the preparation of conjugates.
    Type: Grant
    Filed: November 23, 2016
    Date of Patent: September 11, 2018
    Assignee: NERVIANO MEDICAL SCIENCES S.R.L.
    Inventors: Italo Beria, Michele Caruso, Vittoria Lupi, Paolo Orsini, Matteo Salsa, Achille Panzeri
  • Synthesis of sulfur containing ammonium and phosphonium borates
    Patent number: 10065936
    Abstract: The present invention relates to the preparation of sulfur containing ammonium and phosphonium borates KA, wherein K is a compound of formula (I), and A is an anion of formulae (IIa) or (IIb) by bringing into contact ammonium borates with sulfur containing ammonium or phosphonium halides or sulfonates.
    Type: Grant
    Filed: February 5, 2016
    Date of Patent: September 4, 2018
    Assignee: Gotion Inc.
    Inventors: Nicole Holub, Juergen Herbel
  • Process for the production of cannabidiol and delta-9-tetrahydrocannabinol
    Patent number: 10059683
    Abstract: The present disclosure relates to the preparation of a cannabidiol compound or a derivative thereof. The cannabidiol compound or derivatives thereof can be prepared by an acid-catalyzed reaction of a suitably selected and substituted di-halo-olivetol or derivative thereof with a suitably selected and substituted cyclic alkene to produce a dihalo-cannabidiol compound or derivative thereof. The dihalo-cannabidiol compound or derivative thereof can be produced in high yield, high stereospecificity, or both. It can then be converted under reducing conditions to a cannabidiol compound or derivatives thereof.
    Type: Grant
    Filed: June 30, 2016
    Date of Patent: August 28, 2018
    Assignee: Noramco, Inc.
    Inventors: Lukas Dialer, Denis Petrovic, Ulrich Weigl
  • Thiadiazolyl-oximinoacetic acid derivative compounds
    Patent number: 10059680
    Abstract: Thiadiazolyl-oximinoacetic acid derivatives have been synthesized, which are useful in the manufacture of cephalosporin antibiotic compounds. Compound (1) (TATD) is commercially available (CAS No. 76028-96-1). It has now been discovered that the thiadiazolyl-oximinoacetic acid derivative compound (1) (TATD) can be prepared from dimethyl malonate (SM 1, CAS No. 108-59-8) according to methods described herein. The methods provide products having desirable purity.
    Type: Grant
    Filed: December 18, 2015
    Date of Patent: August 28, 2018
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Kristos Adrian Moshos, Valdas Jurkauskas
  • Compositions and methods for acylating lactams
    Patent number: 10040784
    Abstract: This disclosure provides methods for intermolecular enantioselective C-acylation of lactams with quaternary stereogenic centers by applying a chiral Ni catalyst. The methods comprise treating a lactam with a chiral Ni catalyst, an aryl nitrile, and an aryl halide.
    Type: Grant
    Filed: March 9, 2017
    Date of Patent: August 7, 2018
    Assignee: California Institute of Technology
    Inventors: Brian M. Stoltz, Masaki Hayashi, Satoshi Hashimoto
  • Process for manufacturing acrylic acid, acrylonitrile and 1,4-butanediol from 1,3-propanediol
    Patent number: 10035749
    Abstract: The present invention is in the field of producing bio-based commodity organic chemicals such as bio-acrylic acid, bio-acrylonitrile, and bio-1,4-butanediol using renewable carbon sources as feedstock. In the first stage of the present invention, bio-1,3-propanediol is derived from renewable carbon sources through microbial fermentation. In the second stage of the present invention, bio-1,3-propanediol is converted into bio-acrylic acid or bio-acrylonitrile or bio-1,4-butanediol.
    Type: Grant
    Filed: September 3, 2014
    Date of Patent: July 31, 2018
    Assignee: Myriant Corporation
    Inventors: Vijay Gnanadesikan, Ramnik Singh, Rajesh Dasari, Montgomery Alger
  • Dichroic pigment compounds and compositions containing the same
    Patent number: 10023743
    Abstract: A compound serving as a dichroic pigment which has a maximum absorption wavelength in a range of 350 nm to 510 nm is represented by the following Formula (1): In Formula (1), R1 represents a hydrogen atom or a C1-C20 alkyl group; R2 through R4 are substituents which are not hydrogen atoms and each independently represent a C1-C4 alkyl group; n, m, and p are each independently an integer of 0 to 2; and Ar1 represents a nitrogen-containing saturated heterocyclic group which is a 5 to 8-membered ring and in which (i) N is bonded to a phenylene group and (ii) at least one ?-position is an oxygen atom or a sulfur atom.
    Type: Grant
    Filed: February 17, 2016
    Date of Patent: July 17, 2018
    Assignee: SUMITOMO CHEMICAL COMPANY, LIMITED
    Inventors: Noriyuki Hida, Haruki Okawa
  • Method of treating hypertension
    Patent number: 10022377
    Abstract: Disclosed herein are compositions and methods for the treatment of pulmonary hypertension, including pulmonary arterial hypertension. The methods include administering to a patient in need thereof an effective amount of anagrelide or derivative thereof. The compositions include an effective amount of anagrelide or derivative thereof, in some instances combined with one or more additional agents for the treatment of pulmonary hypertension.
    Type: Grant
    Filed: November 24, 2016
    Date of Patent: July 17, 2018
    Assignee: Cipla Limited
    Inventors: Geena Malhotra, Kalpana Joshi
  • Mitotic kinesin inhibitors and methods of use thereof
    Patent number: 10017482
    Abstract: This invention relates to inhibitors of mitotic kinesins, particularly KSP, and methods for producing these inhibitors.
    Type: Grant
    Filed: November 21, 2016
    Date of Patent: July 10, 2018
    Assignee: Array BioPharma Inc.
    Inventors: Jeremy Hans, Eli M. Wallace, Qian Zhao, Joseph P. Lyssikatos, Thomas D. Aicher, Ellen Laird, John Robinson, Shelley Allen