Patents Examined by Zinna Northington
  • Process for the manufacturing of (6aR,10aR)-7-propyl-6,6a,7,8,9,10,10a,11-octahydro-[1,3]dioxolo[4?,5?:5,6]benzo[1,2-G]quinoline and (4aR,10aR)-1-propyl-1,2,3,4,4a,5,10,10a-octahydro-benzo[G]quinoline-6,7-diol
    Patent number: 11168056
    Abstract: The present invention relates to a new process for manufacturing (6aR,10aR)-7-propyl-6,6a,7,8,9,10,10a,11-octahydro-[1,3]dioxolo[4?,5?:5,6]benzo[1,2-g]quinoline with formula (Ib) below, (4aR,10aR)-1-Propyl-1,2,3,4,4a,5,10,10a-octahydro-benzo[g]quinoline-6,7-diol with formula (I) below and salts thereof. Both compounds are for use in the treatment of neurodegenerative diseases and disorders such as Parkinson's Disease. The invention also relates to new intermediate compounds of said process.
    Type: Grant
    Filed: May 18, 2020
    Date of Patent: November 9, 2021
    Assignee: H. Lundbeck A/S
    Inventors: Mikkel Fog Jacobsen, Martin Juhl, Frans Dennis Therkelsen, Kåre Søndergaard, Tobias Gylling Frihed
  • Crystal of benzofuran derivative free base and preparation method
    Patent number: 11155537
    Abstract: This application describes a crystal of a benzofuran derivative free base and a preparation method. Specifically, this application describes crystal A, crystal B, crystal C, and crystal D of N-((4,6-dimethyl-2-carbonyl-1,2-dihydropyridin-3-yl)methyl)-5-ethyl-6-(ethyl(tetrahydro-2H-pyran)4-yl)amino)-2-(piperidin-1-ylmethyl)benzofuran-4-carboxamide and a preparation method for the crystals. The crystals of the compound of formula (I) have great crystal stability and provides improved uses in clinical treatment.
    Type: Grant
    Filed: May 17, 2018
    Date of Patent: October 26, 2021
    Assignee: Jiangsu Hengrui Medicine Co., Ltd.
    Inventors: Likun Wang, Zhenxing Du, Qiyun Shao, Chao Xu
  • Salts of a heterocyclic compound and crystalline forms, processes for preparing, therapeutic uses, and pharmaceutical compositions thereof
    Patent number: 11136304
    Abstract: The present disclosure relates to salts of (R)-1-(8-fluoroisochroman-1-yl)-N-methylmethanamine, crystalline forms thereof, and methods of preparation thereof, which are useful in the treatment of CNS disorders.
    Type: Grant
    Filed: March 13, 2020
    Date of Patent: October 5, 2021
    Assignee: Sunovion Pharmaceuticals Inc.
    Inventors: Nandkumar Nivritti Bhogle, Takahiko Hashizuka, Robert Joseph Prytko, John R. Snoonian, Harold Scott Wilkinson, Haitao Zhang
  • Ring-fused thiazolino 2-pyridones in combination with a drug against tuberculosis
    Patent number: 11129816
    Abstract: Described is a composition that includes: (i) a drug against tuberculosis inhibiting the cytochrome b subunit of the bc1 complex, said cytochrome b subunit being encoded by the gene qcrB, in Mycobacterium tuberculosis, or a pharmaceutically acceptable salt thereof, and (ii) a compound of Formula II, or a pharmaceutically acceptable salt thereof.
    Type: Grant
    Filed: October 5, 2018
    Date of Patent: September 28, 2021
    Assignees: Quretech Bio AB, Washington University in St. Louis
    Inventors: Christina Leigh Stallings, Gregory Alexander Harrison, Fredrik Almqvist, Souvik Sarkar
  • Process for the preparation of fluopicolide
    Patent number: 11130735
    Abstract: The present invention relates to an improved process for the preparation of substituted pyridylmethyl-benzamide derivatives of formula (I), in particular 2,6-Dichloro-N-{[3-chloro-5-(trifluoromethyl)-2-pyridyl]methyl}benzamide (Fluopicolide), from substituted 2-(Aminomethyl)pyridine derivatives which are obtained by Raney-Nickel hydrogenation.
    Type: Grant
    Filed: November 21, 2018
    Date of Patent: September 28, 2021
    Inventors: Wahed Ahmed Moradi, Albert Schnatterer
  • Methods for preparation of substituted pyridines and related novel compounds
    Patent number: 11117893
    Abstract: The present invention relates to novel methods of preparation of substituted pyridines and the compounds produced therefrom. In particular, the present invention provides efficient methods for the construction of diversely substituted pyridines, with varying substitution patterns under simple and metal-free conditions with high atom- and pot-economy and excellent functional group tolerance, and which are useful for the synthesis of natural products.
    Type: Grant
    Filed: September 24, 2019
    Date of Patent: September 14, 2021
    Assignee: Union University
    Inventors: Edmond Blake Watkins, Dilipkumar Uredi, Damoder Reddy Motati
  • Compounds, compositions, and methods for increasing CFTR activity
    Patent number: 11098035
    Abstract: The present disclosure is directed to disclosed compounds that increase cystic fibrosis transmembrane conductance regulator (CFTR) activity as measured in human bronchial epithelial (hBE) cells.
    Type: Grant
    Filed: July 12, 2019
    Date of Patent: August 24, 2021
    Assignee: Proteostasis Therapeutics, Inc.
    Inventors: Cecilia M. Bastos, Benito Munoz, Bradley Tait
  • Pyran dervatives as CYP11A1 (cytochrome P450 monooxygenase 11A1) inhibitors
    Patent number: 11098032
    Abstract: Compounds of formula (I) wherein R1, R2, R3, R4, R5, R23, R24, L, A and B are as defined in claim 1, or pharmaceutically acceptable salts thereof are disclosed. The compounds of formula (I) possess utility as cytochrome P450 monooxygenase 11A1 (CYP11A1) inhibitors. The compounds are useful as medicaments in the treatment of steroid receptor, particularly androgen receptor, dependent diseases and conditions, such as prostate cancer.
    Type: Grant
    Filed: June 8, 2020
    Date of Patent: August 24, 2021
    Assignee: ORION CORPORATION
    Inventors: David Din Belle, Mikko Mäkelä, Mikko Passiniemi, Pekka Pietikäinen, Petteri Rummakko, Eija Tiainen, Matti Vaismaa, Gerd Wohlfahrt
  • Insoluble complex or solvate thereof, pharmaceutical composition and use thereof
    Patent number: 11084790
    Abstract: The present invention provides a complex of formula (I) or a solvate thereof (wherein n is 1 to 4), a pharmaceutical composition, and use of the pharmaceutical composition in the prevention or treatment of surgical pain, intraoperative pain and postsurgical pain. The technical solution according to the present invention provides a medicament which can be produced by a simple production process and can stably release a local anesthetic in body for a long period. The medicament can be released for at least three days or more, which can prolong the analgesic effect on the postsurgical pain, can be used conveniently by the physician and the patient, and has a good treatment compliance.
    Type: Grant
    Filed: March 26, 2018
    Date of Patent: August 10, 2021
    Assignee: Fruithy Holdings Limited
    Inventors: Shanchun Zhang, Yihua Wang, Jiashi Peng, Kaisheng Cheng, Xiao Wang, Shu Gao, Hongzhang Sun, Xiaorong Lu
  • Process for making esters of 2,5-furandicarboxylic acid
    Patent number: 11078174
    Abstract: A process is provided for making esters of FDCA, in which an aqueous feed comprising glucaric acid is first reacted with a high boiling first alcohol in the presence of an acid catalyst and with removing water during the reaction, to form a first product mixture comprising a first ester of FDCA and the high boiling first alcohol, then unreacted high boiling first alcohol is removed from the first product mixture. The first ester of FDCA and the high boiling first alcohol is then transesterified with a lower boiling second alcohol selected from the group consisting of methanol, ethanol, isopropanol and n-propanol, to form a second product mixture comprising a second ester of FDCA with the lower boiling second alcohol, and the second ester of FDCA with the lower boiling second alcohol is recovered.
    Type: Grant
    Filed: June 20, 2018
    Date of Patent: August 3, 2021
    Assignee: ARCHER DANIELS MIDLAND COMPANY
    Inventors: Pam Anklam, William Chris Hoffman, Stephen J. Howard, Alexandra Sanborn, Mitchell Schultz, John G. Soper
  • Compounds and methods of use
    Patent number: 11077101
    Abstract: Compounds are provided according to Formula (I): and pharmaceutically acceptable salts thereof, and pharmaceutical compositions thereof; wherein X1, X2, X3, X4, Y, A, L1, L2, R1, R2, R5, m and n are as defined herein. Compounds of the present invention are contemplated useful for the prevention and treatment of a variety of conditions.
    Type: Grant
    Filed: July 18, 2019
    Date of Patent: August 3, 2021
    Assignee: Tango Therapeutics, Inc.
    Inventors: Kevin M. Cottrell, John P. Maxwell, Douglas A. Whittington
  • Compound for inhibiting nicotinamide phosphoribosyltransferase and composition containing same
    Patent number: 11078195
    Abstract: The present invention relates to a novel compounds for inhibiting nicotinamide phosphoribosyltransferase (NamPT), a composition comprising the same, and various uses thereof.
    Type: Grant
    Filed: March 17, 2017
    Date of Patent: August 3, 2021
    Inventors: Hyun Seok Kim, Gyoon Hee Han
  • Activating pyruvate kinase R
    Patent number: 11071725
    Abstract: This disclosure provides compounds and compositions for activating pyruvate kinase R (PKR) and related methods of manufacturing and using these compounds and compositions.
    Type: Grant
    Filed: May 1, 2020
    Date of Patent: July 27, 2021
    Assignee: FORMA Therapeutics, Inc.
    Inventors: Anna Ericsson, Neal Green, Gary Gustafson, David R. Lancia, Jr., Gary Marshall, Lorna Mitchell, David Richard, Zhongguo Wang
  • Electron donor, and method for synthesizing 4, 4?-bipyridine using electron donor
    Patent number: 11066367
    Abstract: Provided are an electron donor that is easy to handle and can be used to carry out a coupling reaction economically and efficiently through simple operations under mild conditions in a short period of time, and a method for synthesizing 4,4?-bipyridine using the electron donor. The electron donor includes a mixture of a dispersion product obtained by dispersing sodium in a dispersion solvent and 1,3-dimethyl-2-imidazolidinone, and this electron donor is used in the method for synthesizing 4,4?-bipyridine.
    Type: Grant
    Filed: September 27, 2018
    Date of Patent: July 20, 2021
    Assignee: Kobelco Eco-Solutions Co., Ltd.
    Inventors: Yoshiaki Murakami, Miyuki Fukushima, Kazuhiko Takai, Sobi Asako
  • Salts of a heterocyclic compound and crystalline forms, processes for preparing, therapeutic uses, and pharmaceutical compositions thereof
    Patent number: 11066380
    Abstract: The present disclosure relates to salts of (R)-1-(8-fluoroisochroman-1-yl)-N-methylmethanamine, crystalline forms thereof, and methods of preparation thereof, which are useful in the treatment of CNS disorders.
    Type: Grant
    Filed: March 13, 2020
    Date of Patent: July 20, 2021
    Assignee: Sunovion Pharmaceuticals Inc.
    Inventors: Nandkumar Nivritti Bhogle, Takahiko Hashizuka, Robert Joseph Prytko, John R. Snoonian, Harold Scott Wilkinson, Haitao Zhang
  • Pyrrole compounds, a process for their preparation and pharmaceutical
    Patent number: 11058689
    Abstract: Compounds of formula (I): wherein A1, A2, Ra, Rb, Rc, Rd, R3, R4, R5 and T are as defined in the description. Medicinal products containing the same which are useful in treating pathologies involving a deficit in apoptosis, such as cancer, auto-immune diseases, and diseases of the immune system.
    Type: Grant
    Filed: May 4, 2020
    Date of Patent: July 13, 2021
    Assignees: LES LABORATOIRES SERVIER, VERNALIS (R&D) LTD
    Inventors: Arnaud Le Tiran, Thierry Le Diguarher, Jérôme-Benoît Starck, Jean-Michel Henlin, Anne-Françoise Guillouzic, Guillaume De Nanteuil, Olivier Geneste, Imre Fejes, János Tatai, Miklós Nyerges, James Edward Paul Davidson, James Brooke Murray, I-Jen Chen, Didier Durand
  • Precursors for radiofluorination
    Patent number: 11053200
    Abstract: A method for producing a radiofluorinated compound having an aromatic or heteroaromatic ring carrying [18F] fluorine as first substituent, a bonding unit, which can bind to a peptide or peptide mimetic, and a spacer group connected via bond A1 to the bonding unit and via bond A2 to the ring, wherein the bonding unit has second substituent(s) —OH, —CONH, and/or —COOH. The steps include (a) providing a precursor having the ring carrying a substituent Y, bonding unit with the second substituent(s), and spacer group, wherein substituent Y is —N+(R1R2R3), —NO2, —Cl, —Br, —F, or —I, and R1, R2, and R3 are independently C1-C6 alkyl; and (b) reacting the precursor with a [18F] fluoride anion in the presence of an activation salt to the radiofluorinated compound, which has a cation N+(R4R5R6R7) with R4, R5, R6, and R7 being independently C1-C6 alkyl, wherein the substituent Y is replaced by [18F] fluoride.
    Type: Grant
    Filed: January 31, 2020
    Date of Patent: July 6, 2021
    Assignee: ABX advanced biochemical compounds GmbH
    Inventors: René Martin, René Smits, Ronny Hesse, Alexander Hoepping, Marco Müller, Sandra Hübner
  • Optically active pyrrolidine compound and method for producing same
    Patent number: 11053217
    Abstract: The present invention provides: a methyl 1-{2-[(3S,4R)-1-[(3R,4R)-1-cyclopentyl-3-fluoro-4-(4-methoxyphenyl)pyrrolidine-3-carbonyl]-4-(methoxymethyl)pyrrolidin-3-yl]-5-(trifluoromethyl)phenyl}piperidine-4-carboxylate 1/2 ethane-1,2-disulfonic acid which is represented by formula (1) and is excellent in crystallinity; and a method for producing the same; and a production intermediate thereof; and a production method using this compound.
    Type: Grant
    Filed: September 28, 2018
    Date of Patent: July 6, 2021
    Assignee: MITSUBISHI TANABE PHARMA CORPORATION
    Inventors: Joji Tsurumoto, Kenji Morokuma
  • Small molecule MDM2 protein degraders
    Patent number: 11046703
    Abstract: The present disclosure provides compounds represented by Formula I: wherein R1a, R1b, R2a, R2b, R3a, R3b, R4, A, L, X, Y, and Z are as defined as set forth in the specification. The present disclosure also provides compounds of Formula I for use to treat cancer or any other disease, condition, or disorder that is responsive to degradation of MDM2 protein.
    Type: Grant
    Filed: October 7, 2019
    Date of Patent: June 29, 2021
    Assignee: THE REGENTS OF THE UNIVERSITY OF MICHIGAN
    Inventors: Shaomeng Wang, Angelo Aguilar, Yangbing Li, Jiuling Yang, Donna McEachern
  • Muscarinic M1 receptor positive allosteric modulators
    Patent number: 11040026
    Abstract: The present invention relates to compounds of formula (I), or their isotopic forms, stereoisomers, tautomers or pharmaceutically acceptable salt(s) thereof as muscarinic M1 receptor positive allosteric modulators (M1 PAMs). The present invention describes the preparation, pharmaceutical composition and the use of compound formula (I).
    Type: Grant
    Filed: August 31, 2017
    Date of Patent: June 22, 2021
    Assignee: Suven Life Sciences Limited
    Inventors: Ramakrishna Nirogi, Anil Karbhari Shinde, Abdul Rasheed Mohammed, Rajesh Kumar Badange, Pradeep Jayarajan, Gopinadh Bhyrapuneni, Venkateswarlu Jasti