Patents Examined by Kahsay Habte
  • Patent number: 10604534
    Abstract: In its many embodiments, the present invention provides certain C5-C6-oxacyclic fused iminothiadiazine dioxide compounds bearing an ether linker, including compounds Formula (I): or a tautomer thereof, and pharmaceutically acceptable salts of said compounds and said tautomers, wherein RN, R1, R2, RA, ring A, ring C, and m are as defined herein. The novel compounds of the invention are useful as BACE inhibitors and/or for the treatment and prevention of various pathologies related thereto. Pharmaceutical compositions comprising one or more such compounds (alone and in combination with one or more other active agents), and methods for their preparation and use, including for the possible treatment of Alzheimer's disease, are also disclosed.
    Type: Grant
    Filed: February 6, 2017
    Date of Patent: March 31, 2020
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Shawn P. Walsh, Jared N. Cumming, Xing Dai
  • Patent number: 10604507
    Abstract: Described herein are compounds that are melanocortin subtype-2 receptor (MC2R) modulators, methods of making such compounds, pharmaceutical compositions and medicaments comprising such compounds, and methods of using such compounds in the treatment of conditions, diseases, or disorders that would benefit from modulation of MC2R activity.
    Type: Grant
    Filed: August 27, 2019
    Date of Patent: March 31, 2020
    Assignee: CRINETICS PHARMACEUTICALS, INC.
    Inventors: Sangdon Han, Yunfei Zhu, Sun Hee Kim, Jian Zhao, Shimiao Wang
  • Patent number: 10597382
    Abstract: The present invention discloses compounds of Formula (I), or pharmaceutically acceptable salts, ester, stereoisomer, tautomer, solvate, hydrate, or combination thereof: which inhibit the Apoptosis signal-regulating kinase 1 (ASK-1), which associated with autoimmune disorders, neurodegenerative disorders, inflammatory diseases, chronic kidney disease, cardiovascular disease. The present invention further relates to pharmaceutical compositions comprising the aforementioned compounds for administration to a subject suffering from ASK-1 related disease. The invention also relates to methods of treating an ASK-1 related disease in a subject by administering a pharmaceutical composition comprising the compounds of the present invention. The present invention specifically relates to methods of treating ASK-1 associated with hepatic steatosis, including non-alcoholic fatty liver disease (NAFLD) and non-alcohol steatohepatitis disease (NASH).
    Type: Grant
    Filed: August 27, 2018
    Date of Patent: March 24, 2020
    Assignee: Enanta Pharmaceuticals, Inc.
    Inventors: Guoqiang Wang, Jing He, Bin Wang, Ruichao Shen, Brett Granger, Yat Sun Or
  • Patent number: 10597392
    Abstract: The present invention provides compounds of formula I: which are useful as modulators of GPR6, pharmaceutical compositions thereof, methods for treatment of conditions associated with GPR6, processes for making the compounds and intermediates thereof.
    Type: Grant
    Filed: November 30, 2018
    Date of Patent: March 24, 2020
    Assignee: Takeda Pharmaceutical Company Limited
    Inventors: Stephen Hitchcock, Maria Hopkins, Shota Kikuchi, Holger Monenschein, Holly Reichard, Huikai Sun, Todd Macklin
  • Patent number: 10597404
    Abstract: The present invention relates to novel crystalline forms of dolutegravir, process for its preparation and pharmaceutical composition comprising them.
    Type: Grant
    Filed: August 19, 2016
    Date of Patent: March 24, 2020
    Assignee: Laurus Labs Ltd.
    Inventors: Ram Thaimattam, Rajesh Edupuganti, Venkata Sunil Kumar Indukuri, Srihari Raju Kalidindi, Satyanarayana Chava
  • Patent number: 10597390
    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: August 7, 2015
    Date of Patent: March 24, 2020
    Assignee: Janssen Sciences Ireland UC
    Inventors: Tim Hugo Maria Jonckers, Pierre Jean-Marie Bernard Raboisson, Jérôme Émile Georges Guillemont, David Craig McGowan, Werner Constant Johan Embrechts, Ludwig Paul Cooymans, Antoine Benjamin Michaut
  • Patent number: 10590095
    Abstract: Compositions and processes for producing high purity acesulfame potassium are described. One process comprises the steps of providing a crude acesulfame potassium composition comprising acesulfame potassium and acetoacetamide, concentrating the crude acesulfame potassium composition to form a water stream and an intermediate acesulfame potassium composition comprising acesulfame potassium and less than 33 wppm acetoacetamide, and separating the intermediate acesulfame potassium composition to form the finished acesulfame potassium composition comprising acesulfame potassium and less than 33 wppm acetoacetamide. The concentrating step is conducted at a temperature below 90° C. and the separating step is conducted at a temperature at or below 35° C.
    Type: Grant
    Filed: February 12, 2019
    Date of Patent: March 17, 2020
    Assignee: Celanese International Corporation
    Inventors: Christoph Mollenkopf, Peter Groer, Arvind Yadav
  • Patent number: 10590096
    Abstract: Compositions and processes for producing high purity acesulfame potassium are described. One process comprises the steps of forming a cyclic sulfur trioxide adduct; hydrolyzing the cyclic sulfur trioxide adduct to form an acesulfame-H composition comprising acesulfame-H; neutralizing the acesulfame-H in the acesulfame-H composition to form a crude acesulfame potassium composition comprising acesulfame potassium and less than 2800 wppm acetoacetamide-N-sulfonic acid, wherein the neutralizing step is conducted or maintained at a pH at or below 11.0; and treating the crude acesulfame potassium composition to form the finished acesulfame potassium composition comprising acesulfame potassium and less than 37 wppm acetoacetamide-N-sulfonic acid.
    Type: Grant
    Filed: February 12, 2019
    Date of Patent: March 17, 2020
    Assignee: Celenese International Corporation
    Inventors: Christoph Mollenkopf, Peter Groer, Arvind Yadav
  • Patent number: 10590097
    Abstract: A process for producing acesulfame potassium, the process comprising the steps of providing a cyclizing agent composition comprising a cyclizing agent and a solvent and having an initial temperature, cooling the cyclizing agent composition to form a cooled cyclizing agent composition having a cooled temperature less than 35° C., reacting an acetoacetamide salt with the cyclizing agent in the cooled cyclizing agent composition to form a cyclic sulfur trioxide adduct composition comprising cyclic sulfur trioxide adduct; and, forming from the cyclic sulfur trioxide adduct in the cyclic sulfur trioxide adduct composition the finished acesulfame potassium composition comprising non-chlorinated acesulfame potassium and less than 39 wppm 5-chloro-acesulfame potassium. The cooled temperature is at least 2° C. less than the initial temperature.
    Type: Grant
    Filed: February 12, 2019
    Date of Patent: March 17, 2020
    Assignee: Celanese International Corporation
    Inventors: Christoph Mollenkopf, Peter Groer, Arvind Yadav
  • Patent number: 10590098
    Abstract: Improved processes for producing high purity acesulfame potassium. In one embodiment, the process comprises the steps of contacting a solvent, e.g., dichloromethane, and a cyclizing agent, e.g., sulfur trioxide, to form a cyclizing agent composition and reacting an acetoacetamide salt with the cyclizing agent in the composition to form a cyclic sulfur trioxide adduct. The contact time is less than 60 minutes. The process also comprises forming from the cyclic sulfur trioxide adduct composition a finished acesulfame potassium composition comprising non-chlorinated, e.g., non-chlorinated, acesulfame potassium and less than 35 wppm 5-halo acesulfame potassium, preferably less than 5 wppm.
    Type: Grant
    Filed: February 12, 2019
    Date of Patent: March 17, 2020
    Assignee: Celanese International Corporation
    Inventors: Christoph Mollenkopf, Peter Groer, Arvind Yadav
  • Patent number: 10590112
    Abstract: This invention relates to new benzazepine carboxamide compounds of the formula wherein X and R1 to R6 are as defined in the description and in the claims, as well as pharmaceutically acceptable salts thereof. These compounds are TLR8 agonists and may therefore be useful as medicaments for the treatment of diseases such as cancer, autoimmune diseases, inflammation, sepsis, allergy, asthma, graft rejection, graft-versus-host disease, immunodeficiencies, and infectious diseases.
    Type: Grant
    Filed: December 7, 2018
    Date of Patent: March 17, 2020
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Fabian Dey, Lisha Wang, Hongying Yun, Weixing Zhang, Zhiwei Zhang, Wei Zhu
  • Patent number: 10584124
    Abstract: Provided herein are compound of Formula I-IV and pharmaceutically acceptable salts thereof which exhibit rearranged during transfection (RET) kinase inhibition. In particular, provided herein are novel crystalline forms of 4-(6-(4-((6-methoxypyridin-3-yl)methyl)piperazin-1-yl)pyridin-3-yl)-6-(1-methyl-1H-pyrazol-4-yl)pyrazolo[1,5-a]pyridine-3-carbonitrile (Formula I), 6-(2-hydroxy-2-methylpropoxy)-4-(6-(6-((6-methoxypyridin-3-yl)methyl)-3,6-diazabicyclo[3.1.1]heptan-3-yl)pyridin-3-yl)pyrazolo[1,5-a]pyridine-3-carbonitrile (Formula II), 6-(2-hydroxy-2-methylpropoxy)-4-(6-(6-(6-methoxynicotinoyl)-3,6-diazabicyclo[3.1.
    Type: Grant
    Filed: October 10, 2018
    Date of Patent: March 10, 2020
    Assignee: Array Biopharma Inc.
    Inventors: Andrew T. Metcalf, David Fry, Elizabeth A. McFaddin, Gabrielle R. Kolakowski, Julia Haas, Tony P. Tang, Yutong Jiang
  • Patent number: 10576059
    Abstract: Substituted phenylpyrrolecarboxamide compounds such as those represented by Formula A can be used in the treatment of HIV infection and related conditions.
    Type: Grant
    Filed: July 24, 2019
    Date of Patent: March 3, 2020
    Assignees: New York Blood Center, Inc., The United States of America, as Represented by the Secretary, Department of Human Services
    Inventors: Asim Kumar Debnath, Francesca Curreli, Peter D. Kwong, Young Do Kwon
  • Patent number: 10577381
    Abstract: The present disclosure provides prodrugs of biologically active 2,4-pyrimidinediamine compounds, compositions comprising the prodrugs, intermediates and methods for synthesizing the prodrugs and methods of using the prodrugs in a variety of applications.
    Type: Grant
    Filed: November 28, 2018
    Date of Patent: March 3, 2020
    Assignee: Rigel Pharmaceuticals, Inc.
    Inventors: Rajinder Singh, Somasekhar Bhamidipati, Esteban Masuda, Thomas Sun, Valentino J. Stella
  • Patent number: 10570105
    Abstract: The present invention includes methods/processes and intermediates for preparing compounds having structural Formula (XI): wherein Y is C1-C12 alkylene or C1-C12 alkenylene; and R8 and R12 are independently C1-C12 alkyl.
    Type: Grant
    Filed: May 9, 2019
    Date of Patent: February 25, 2020
    Assignee: Firmenich Incorporated
    Inventors: Catherine Tachdjian, Donald S. Karanewsky, Xiao-Qing Tang, Qing Chen, Peter Leeming, Tayyab Rashid, Daniel Levin
  • Patent number: 10562908
    Abstract: The present invention relates to ortho substituted phenylpyrazolo- and pyrrolo-pyridazine derivatives having dual pharmacological activity towards both the ?2? subunit, in particular the ?2?-1 subunit, of the voltage-gated calcium channel and the ?-opioid receptor, to processes of preparation of such compounds, to pharmaceutical compositions comprising them, and to their use in therapy, in particular for the treatment of pain.
    Type: Grant
    Filed: November 30, 2017
    Date of Patent: February 18, 2020
    Assignee: ESTEVE PHARMACEUTICALS, S.A.
    Inventors: Marina Virgili-Bernado, Monica Alonso-Xalma, Carmen Almansa-Rosales
  • Patent number: 10562884
    Abstract: Described herein are compounds that are melanocortin subtype-2 receptor (MC2R) modulators, methods of making such compounds, pharmaceutical compositions and medicaments comprising such compounds, and methods of using such compounds in the treatment of conditions, diseases, or disorders that would benefit from modulation of MC2R activity.
    Type: Grant
    Filed: June 5, 2019
    Date of Patent: February 18, 2020
    Assignee: CRINETICS PHARMACEUTICALS, INC.
    Inventors: Sangdon Han, Yunfei Zhu, Sun Hee Kim, Jian Zhao, Shimiao Wang
  • Patent number: 10556896
    Abstract: The present invention relates to novel crystalline forms of compound (I), (3-Amino-oxetan-3-ylmethyl)-[2-(5,5-dioxo-5,6,7,9-tetrahydro-5lambda*6*-thia-8-aza-benzocyclohepten-8-yl)-6-methyl-quinazolin-4-yl]-amine and pharmaceutical compositions comprising the crystalline forms thereof disclosed herein, which may be used for the treatment or prophylaxis of a viral disease in a patient relating to respiratory syncytial virus (RSV) infection or a disease caused by RSV infection.
    Type: Grant
    Filed: August 8, 2018
    Date of Patent: February 11, 2020
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Wei Zhang, Lin Wang, Wei Li
  • Patent number: 10556892
    Abstract: Disclosed herein, inter alia, are compositions and methods for modulating the activity of N-acylethanolamine acid amidase for the treatment of a pathological state, including pain, an inflammatory condition, or a neurodegenerative disorder.
    Type: Grant
    Filed: May 16, 2017
    Date of Patent: February 11, 2020
    Assignees: The Regents of the University of California, Fondazione Istituto Italiano di Technologia
    Inventors: Daniele Piomelli, Rita Scarpelli, Marco Migliore, Roger Heim, Miguel Garcia-Guzmàn
  • Patent number: 10550115
    Abstract: The invention relates to compounds of formula (I), particularly for the use thereof as a medicament, especially in the treatment or prevention of neurogenerative disorders. The invention also relates to the methods for producing said compounds, and to the pharmaceutical compositions containing same.
    Type: Grant
    Filed: October 10, 2016
    Date of Patent: February 4, 2020
    Assignees: Institut Du Cerveau et de la Moëlle Epiniere, Centre National de la Recherche Scientifique (CNRS), Sorbonne Universite, Assistance Publique-Hopitaux de Paris, Institut National de la Sante et de la Recherche Medicale (INSERM), Universite Paris-SUD
    Inventors: Bruno Figadere, Laurent Ferrie, Gael Le Douaron, Rita Raisman-Vozari, Patrick Michel, Julia Sepulveda