Patents Examined by Kahsay Habte
  • Patent number: 10730849
    Abstract: Compounds of general formula (Ia), compounds of general formula (Ia?), compounds of general formula (Ib), compounds of general formula (Ib?), compounds of general formula (I), compounds of general formula (I?), and their pharmaceutically acceptable salts, wherein R1, R2, R3, R4, R5, R6, R8, R9, X1, X2, and X3 are defined herein, that may be useful as inductors of type I interferon production, specifically as STING active agents, are provided. Also provided are processes for the synthesis and use of compounds of the disclosure.
    Type: Grant
    Filed: July 16, 2019
    Date of Patent: August 4, 2020
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Michael D. Altman, Brandon D. Cash, Wonsuk Chang, Jared N. Cumming, Andrew M. Haidle, Timothy J. Henderson, James P. Jewell, Matthew A. Larsen, Rui Liang, Jongwon Lim, Min Lu, Ryan D. Otte, Tony Siu, Benjamin Wesley Trotter, Sriram Tyagarajan
  • Patent number: 10723710
    Abstract: A process for the preparation of diaminophenothiazinium compounds is described, which allows achieving quickly and effectively a high degree of purity of the same.
    Type: Grant
    Filed: May 16, 2017
    Date of Patent: July 28, 2020
    Assignee: ICROM S.P.A.
    Inventors: Matteo Colombo, Paola Daverio, Stella Borrelli
  • Patent number: 10723728
    Abstract: The invention provides a method of sustained delivery of a lactam, imide, amide, sulfonamide, carbamate or urea containing parent drug by administering to a patient an effective amount of a prodrug compound of the invention wherein upon administration to the patient, release of the parent drug from the prodrug is sustained release. Prodrug compounds suitable for use in the methods of the invention are labile conjugates of parent drugs that are derivatized through carbonyl linked prodrug moieties. The prodrug compounds of the invention can be used to treat any condition for which the lactam, imide, amide, sulfonamide, carbamate or urea containing parent drug is useful as a treatment.
    Type: Grant
    Filed: August 14, 2019
    Date of Patent: July 28, 2020
    Assignee: ALKERMES PHARMA IRELAND LIMITED
    Inventors: Laura Cook Blumberg, Julius F. Remenar, Orn Almarsson, Tarek A. Zeidan
  • Patent number: 10723729
    Abstract: The present invention provides a compound of formula I, having BACE1 inhibitory activity, their manufacture, pharmaceutical compositions containing them and their use as therapeutically active substances. The active compounds of the present invention are useful in the therapeutic and/or prophylactic treatment of e.g. Alzheimer's disease.
    Type: Grant
    Filed: July 16, 2019
    Date of Patent: July 28, 2020
    Assignee: Hoffmann-Le Roche Inc.
    Inventors: Bjoern Bartels, Cosimo Dolente, Wolfgang Guba, Wolfgang Haap, Ulrike Obst Sander, Jens-Uwe Peters, Thomas Woltering
  • Patent number: 10723756
    Abstract: This disclosure features chemical entities (e.g., a compound that modulates (e.g., agonizes) Stimulator of Interferon Genes (STING), or a pharmaceutically acceptable salt, and/or hydrate, and/or coccrystal, and/or drug combination of the compound) that are useful, e.g., for treating a condition, disease or disorder in which a decrease or increase in STING activity (e.g., a decrease, e.g., a condition, disease or disorder associated with repressed or impaired STING signaling) contributes to the pathology and/or symptoms and/or progression of the condition, disease or disorder (e.g., cancer) in a subject (e.g., a human). This disclosure also features compositions as well as other methods of using and making the same.
    Type: Grant
    Filed: January 11, 2017
    Date of Patent: July 28, 2020
    Assignee: Innate Tumor Immunity Inc.
    Inventors: Gary Glick, Shomir Ghosh, Edward James Olhava, William R. Roush, Roger Jones
  • Patent number: 10717747
    Abstract: The present invention relates to a method for the manufacture of 2-(3-(alkyl or alkenyl)morpholino)-ethan-1-ols by reduction of 8a-(alkyl and alkenyl)hexahydrooxazolo[2,3-c][1,4]oxazines encompassing a process for producing 2-(3-(4-propylheptyl)morpholino)ethan-1-ol with the INN name delmopinol. The invention also relates to 1-chloro-4-propylhept-3-ene, 1-iodo-4-propylhept-3-ene, 8a-(4-5 propylheptyl)hexahydrooxazolo[2,3-c][1,4]oxazine, 8a-(4-propylhept-3-en-1-yl)hexahydrooxazolo[2,3-c][1,4]oxazine and 2-(3-(4-propylhept-3-en-1-yl)morpholino)ethan-1-ol which are intermediates in the delmopinol process.
    Type: Grant
    Filed: December 20, 2017
    Date of Patent: July 21, 2020
    Assignee: Lundbeck Pharmaceuticals Italy S.P.A.
    Inventors: Carla De Faveri, Mariano Stivanello
  • Patent number: 10709688
    Abstract: This invention provides a pharmaceutical composition for treating or preventing synucleinopathy comprising a compound represented by formula (I), or a pharmaceutically acceptable salt thereof.
    Type: Grant
    Filed: March 31, 2017
    Date of Patent: July 14, 2020
    Assignees: Tohoku University, National University Corporation Okayama University
    Inventors: Kohji Fukunaga, Hiroyuki Miyachi, Hiroaki Ishida, Shintaro Ban
  • Patent number: 10703719
    Abstract: A method for producing (2S,5S)/(2R,5R)-5-hydroxypiperidine-2-carboxylic acid represented by the formula (10) below: the method including removing the protecting group from the hydroxyl group in a compound represented by formula (7) below: (wherein P represents a protecting group, R3 represents an alkyl group containing 1 to 4 carbon atoms, and A represents an alkyl group containing 1 to 10 carbon atoms, an aryl group containing 6 to 12 carbon atoms, an alkyloxy group containing 1 to 4 carbon atoms, or an aralkyloxy group containing 7 to 20 carbon atoms) to synthesize a compound represented by formula (8) below: (wherein R3 represents an alkyl group containing 1 to 4 carbon atoms, and A represents an alkyl group containing 1 to 10 carbon atoms, an aryl group containing 6 to 12 carbon atoms, an alkyloxy group containing 1 to 4 carbon atoms, or an aralkyloxy group containing 7 to 20 carbon atoms).
    Type: Grant
    Filed: April 27, 2018
    Date of Patent: July 7, 2020
    Assignee: API CORPORATION
    Inventors: Jun Takehara, Masato Murai, Takashi Ohtani, Tomoko Maeda, Tsugihiko Hidaka
  • Patent number: 10703738
    Abstract: Compounds of general formula (Ia), compounds of general formula (Ia?), compounds of general formula (Ib), compounds of general formula (Ib?), compounds of general formula (I), compounds of general formula (I?), and their pharmaceutically acceptable salts, wherein R1, R2, R3, R4, R5, R6, R8, R9, X1, X2, and X3 are defined herein, that may be useful as inductors of type I interferon production, specifically as STING active agents, are provided. Also provided are processes for the synthesis and use of compounds of the disclosure.
    Type: Grant
    Filed: July 16, 2019
    Date of Patent: July 7, 2020
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Michael D. Altman, Brandon D. Cash, Wonsuk Chang, Jared N. Cumming, Andrew M. Haidle, Timothy J. Henderson, James P. Jewell, Matthew A. Larsen, Rui Liang, Jongwon Lim, Min Lu, Ryan D. Otte, Tony Siu, Benjamin Wesley Trotter, Sriram Tyagarajan
  • Patent number: 10708263
    Abstract: The present invention discloses salts of a Compound 1: useful in the prophylaxis and/or treatment of inflammatory conditions, autoimmune diseases, proliferative diseases, allergy, transplant rejection, diseases involving degradation and/or disruption of cartilage homeostasis, congenital cartilage malformations, and/or diseases associated with hypersecretion of IL6 or interferons.
    Type: Grant
    Filed: July 10, 2017
    Date of Patent: July 7, 2020
    Assignee: GALAPAGOS NV
    Inventors: Piet Wigerinck, Nicolas Luc Sabourault
  • Patent number: 10689353
    Abstract: This invention relates to a method for the manufacture of optically pure (S)-6-chloro-(cyclopropylethynyl)-1,4-dihydro-4-(trifluoromethyl)-2H-3,1-benzoxazin-2-one. Specifically, this invention relates to a flow synthesis method for the manufacture of (S)-6-chloro-(cyclopropylethynyl)-1,4-dihydro-4-(trifluoromethyl)-2H-3,1-benzoxazin-2-one.
    Type: Grant
    Filed: February 15, 2018
    Date of Patent: June 23, 2020
    Assignee: NELSON MANDELA METROPOLITAN UNIVERSITY
    Inventors: Paul Watts, Sravanthi Chada
  • Patent number: 10689377
    Abstract: The present invention relates to compounds that inhibit KRas G12C. In particular, the present invention relates to compounds that irreversibly inhibit the activity of KRas G12C, pharmaceutical compositions comprising the compounds and methods of use therefor.
    Type: Grant
    Filed: November 14, 2018
    Date of Patent: June 23, 2020
    Assignees: Mirati Therapeutics, Inc., Array Biopharma Inc.
    Inventors: James F. Blake, Laurence E. Burgess, Mark Joseph Chicarelli, James Gail Christensen, Adam Cook, Jay Bradford Fell, John P. Fischer, Matthew Arnold Marx, Macedonio J. Mejia, Pavel Savechenkov, Guy P. A. Vigers, Christopher Ronald Smith, Martha E. Rodriguez
  • Patent number: 10683311
    Abstract: The present disclosure relates to fungicidal active compounds, more specifically to trisubstitutedsilylphenoxyhetero-cycles and analogues thereof, processes and, intermediates for their preparation and use thereof as fungicidal active compound, particularly in the form of fungicide compositions. The present disclosure also relates to methods for the control of phytopathogenic fungi of plants using these compounds or compositions comprising thereof.
    Type: Grant
    Filed: October 28, 2016
    Date of Patent: June 16, 2020
    Assignee: Bayer CropScience Aktiengesellschaft
    Inventors: Jérémy Dufour, Philippe Desbordes, Christophe Dubost, Mathieu Gourgues, Ruth Meissner, Andrew Pettinger, Philippe Rinolfi, Valérie Toquin, Ulrike Wachendorff-Neumann
  • Patent number: 10669283
    Abstract: A compound represented by the general formula (1) below or a pharmacologically acceptable salt thereof: [In the formula (1), R1 and R2 may be the same or different and each represents a hydrogen atom, a halogen atom, a hydroxyl group, a carboxy group, a cyano group, an optionally substituted C1-6 alkyl group et al.; R3 represents a hydrogen atom; R4 represents an optionally substituted 4- to 10-membered monocyclic heterocyclic group containing 1 to 4 heteroatoms selected from an oxygen atom, a nitrogen atom, and a sulfur atom; X represents a group represented by the following formula: —CH2—, —CH2—CH2—, —CH2—CH2—CH2—, or —CH2—O—CH2—; and Z represents a hydrogen atom or a hydroxyl group].
    Type: Grant
    Filed: December 26, 2017
    Date of Patent: June 2, 2020
    Assignee: MEIJI SEIKA PHARMA CO., LTD.
    Inventors: Keiji Tamura, Takeru Yamakawa, Satoshi Isshiki, Yoshinari Wakiyama, Shohei Ouchi, Takashi Matsuhira, Natsuki Ishida, Yuji Tabata
  • Patent number: 10662202
    Abstract: Provided herein is a method for the synthesis of cephalosporin antibiotic compounds comprising a palladium-catalyzed coupling reaction.
    Type: Grant
    Filed: November 6, 2018
    Date of Patent: May 26, 2020
    Assignee: Merck Sharp & Dohm Corp.
    Inventors: David Waller, Gregory Gazda, Zachary Minden, Lisa Barton, Clifton Leigh
  • Patent number: 10660893
    Abstract: The present invention is directed to spirocyclic compounds which are inhibitors of tryptophan hydroxylase (TPH), particularly isoform 1 (TPH1), that are useful in the treatment of diseases or disorders associated with peripheral serotonin including, for example, gastrointestinal, cardiovascular, pulmonary, inflammatory, metabolic, and low bone mass diseases, as well as serotonin syndrome, and cancer.
    Type: Grant
    Filed: May 30, 2019
    Date of Patent: May 26, 2020
    Assignee: ROIVANT SCIENCES, GmbH
    Inventors: Stéphane De Lombaert, Daniel R. Goldberg, Kenneth Brameld, Eric Brian Sjogren, Andrew Scribner
  • Patent number: 10654857
    Abstract: Compounds of formula (I) wherein R1, R2, A, W, m, n, p and q are as described herein, compositions including the compounds and methods of using the compounds as autotaxin inhibitors.
    Type: Grant
    Filed: December 19, 2018
    Date of Patent: May 19, 2020
    Assignee: Hoffman-La Roche Inc.
    Inventors: Patrick Di Giorgio, Jerome Hert, Daniel Hunziker, Holger Kuehne, Patrizio Mattei, Markus Rudolph
  • Patent number: 10654861
    Abstract: A series of substituted fused pentacyclic benzimidazole derivatives, and analogues thereof, being potent modulators of human TNF? activity, are accordingly of benefit in the treatment and/or prevention of various human ailments, including autoimmune and inflammatory disorders; neurological and neurodegenerative disorders; pain and nociceptive disorders; cardiovascular disorders; metabolic disorders; ocular disorders; and oncological disorders.
    Type: Grant
    Filed: March 31, 2017
    Date of Patent: May 19, 2020
    Assignee: UCB Biopharma SRL
    Inventors: Michael Louis Robert Deligny, Jag Paul Heer, Jean Keyaerts, Luce Elsa Lepissier, Martin Alexander Lowe
  • Patent number: 10654874
    Abstract: Provided is a compound represented by the formula (I): wherein each symbol is as defined in the specification, or a salt thereof, which has an AMPA (?-amino-3-hydroxy-5-methyl-4-isoxazolepropionic acid) receptor potentiating action. The compound of the present invention is useful as a prophylactic or therapeutic drug for depression, schizophrenia, Alzheimer's disease or attention deficit hyperactivity disorder (ADHD) and the like.
    Type: Grant
    Filed: January 24, 2019
    Date of Patent: May 19, 2020
    Assignee: Takeda Pharmaceutical Company Limited
    Inventors: Masakuni Kori, Toshihiro Imaeda, Shinji Nakamura, Masashi Toyofuku, Eiji Honda
  • Patent number: 10654808
    Abstract: The present invention relates to a tyrosine kinase inhibitor and a pharmaceutical composition comprising same.
    Type: Grant
    Filed: April 7, 2016
    Date of Patent: May 19, 2020
    Assignee: GUANGDONG RAYNOVENT BIOTECH CO., LTD.
    Inventors: Chaofeng Long, Zhengxia Chen, Xiaoxin Chen, Yang Zhang, Zhuowei Liu, Peng Li, Shuhui Chen, Guibai Liang, Cheng Xie, Zhengwei Li, Zhifei Fu, Guoping Hu, Jian Li