Patents Examined by Valerie Rodriguez-Garcia
  • Substituted indoline derivatives as dengue viral replication inhibitors
    Patent number: 11053196
    Abstract: The present invention concerns substituted indoline derivatives, methods to prevent or treat dengue viral infections by using said compounds and also relates to said compounds for use as a medicine, more preferably for use as a medicine to treat or prevent dengue viral infections. The present invention furthermore relates to pharmaceutical compositions or combination preparations of the compounds, to the compositions or preparations for use as a medicine, more preferably for the prevention or treatment of dengue viral infections. The invention also relates to processes for preparation of the compounds.
    Type: Grant
    Filed: May 18, 2018
    Date of Patent: July 6, 2021
    Assignees: Janssen Pharmaceuticals, Inc., Kathalieke Universiteif Leuven
    Inventors: Jean-François Bonfanti, Bart Rudolf Romanie Kesteleyn, Dorothée Alice Marie-Eve Bardiot, Arnaud Didier M Marchand, Erwin Coesemans, Benoît Christian Albert Ghislain De Boeck, Pierre Jean-Marie Bernard Raboisson
  • TYK2 inhibitors, uses, and methods for production thereof
    Patent number: 11040967
    Abstract: The present invention provides compounds of formula I useful as inhibitors of Tyrosine Kinase 2 (Tyk2) solid forms and compositions thereof, methods of producing the same, and methods of using the same in the treatment of Tyk2-mediated diseases.
    Type: Grant
    Filed: May 21, 2019
    Date of Patent: June 22, 2021
    Assignee: Nimbus Lakshmi, Inc.
    Inventors: Jeremy Robert Greenwood, Craig E. Masse, Jon P. Lawson, Jean-Baptiste Arlin, David Pearson, Jonathan James Loughrey
  • Bicyclic heterocyclic derivatives as MNK1 and MNK2 modulators and uses thereof
    Patent number: 11040978
    Abstract: The present invention relates to compounds of Formula (Ib-I) that act as inhibitors of the MAP kinase interacting kinases MNK2a, MNK2b, MNK1a, and MNK1b. The present invention further relates to pharmaceutical compositions comprising these compounds, and to the use of the compounds for the preparation of a medicament for the prophylaxis and treatment of diseases (e.g., proliferative diseases (e.g., cancer), inflammatory diseases, Alzheimer's disease), as well as methods of treating these diseases.
    Type: Grant
    Filed: June 5, 2019
    Date of Patent: June 22, 2021
    Assignee: Agency for Science, Technology and Research
    Inventors: Kassoum Nacro, Athisayamani Jeyaraj Duraiswamy, Lohitha Rao Chennamaneni
  • Factor XIIa inhibitors
    Patent number: 11014920
    Abstract: The present invention provides a compound of Formula I and pharmaceutical compositions comprising one or more said compounds, and methods for using said compounds for treating or preventing thromboses, embolisms, hypercoagulability or fibrotic changes. The compounds are selective Factor XIIa inhibitors.
    Type: Grant
    Filed: November 13, 2017
    Date of Patent: May 25, 2021
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Jacqueline D. Hicks, Brian Alexander McKittrick, Brent R. Whitehead, Matthew Lombardo, Xiaoqing Han, Jerry A. Taylor, Hong Dong Chu, Sung-Sau So, Peter Orth, Zhicai Wu
  • Synergistic pharmaceutical combination for the treatment of squamous cell carcinoma of head and neck
    Patent number: 10980776
    Abstract: The present invention relates to a pharmaceutical combination for use in the treatment of squamous cell carcinoma, comprising a CDK inhibitor selected from the compounds of formula (I); or a pharmaceutically acceptable salt thereof and one or more antineoplastic agents selected from sorafenib, lapatinib, erlotinib, cisplatin, 5-fluorouracil, docetaxel or cetuximab or a pharmaceutically acceptable salt thereof. The said pharmaceutical combination exhibits synergy when used in the treatment of squamous cell carcinoma of head and neck (SCCHN). The invention also relates to a pharmaceutical composition comprising the said combination and a method for the treatment of squamous cell carcinoma of head and neck (SCCHN), using a therapeutically effective amount of said combination.
    Type: Grant
    Filed: February 8, 2019
    Date of Patent: April 20, 2021
    Assignee: PIRAMAL ENTERPRISES LIMITED
    Inventors: Veena Agarwal, Arun Balakrishnan, Giridharan Periyasamy
  • Crystalline eravacycline bis-hydrochloride
    Patent number: 10975029
    Abstract: The invention relates to crystalline eravacycline bis-hydrochloride and to a process for its preparation. Furthermore, the invention relates to the use of crystalline eravacycline bis-hydrochloride for the preparation of pharmaceutical compositions. The invention further relates to pharmaceutical compositions comprising an effective amount of crystalline eravacycline bis-hydrochloride. The pharmaceutical compositions of the present invention can be used as medicaments, in particular for treatment and/or prevention of bacterial infections e.g. caused by Gram negative pathogens or Gram positive pathogens, in particular caused by multidrug resistant Gram negative pathogens. The pharmaceutical compositions of the present invention can thus be used as medicaments for e.g. the treatment of complicated intra-abdominal and urinary tract infection.
    Type: Grant
    Filed: January 20, 2017
    Date of Patent: April 13, 2021
    Assignee: Sandoz AG
    Inventor: Hannes Lengauer
  • Crystal forms of tetrahydro-n,n-dimethyl-2,2-diphenyl-3-furanmethanamine hydrochloride, processes of making such forms, and their pharmaceutical compositions
    Patent number: 10966952
    Abstract: Polymorphic forms of tetrahydro-N,N-dimethyl-2,2-diphenyl-3-furanmethanamine hydrochloride (ANAVEX2-73) and a metabolite of tetrahydro-N,N-dimethyl-2,2-diphenyl-3-furanmethanamine hydrochloride (ANAVEX2-73) are disclosed and characterized. Compositions and method for treatment of Alzheimer's disease that includes the polymorphic forms and metabolite of tetrahydro-N,N-dimethyl-2,2-diphenyl-3-furanmethanamine hydrochloride (ANAVEX2-73).
    Type: Grant
    Filed: July 29, 2019
    Date of Patent: April 6, 2021
    Assignee: ANAVEX LIFE SCIENCES CORP.
    Inventors: Linda Sharon Daintree, Daniel Mark Ledger, Lucy Anne Leonard, Peter York
  • Therapeutic agent for liver diseases
    Patent number: 10966969
    Abstract: Disclosed is a pharmaceutical composition for preventing or treating a fatty liver disease containing, as an active ingredient, a pyrazole-based compound or a pharmaceutically acceptable salt thereof. 3-phenyl-4-alkyl-1-(pyridin-2-yl)-1H-pyrazol-5-ol or a pharmaceutically acceptable salt thereof is capable of effectively inhibiting fatty liver, hepatic inflammation and hepatic fibrosis, and is useful for preventing or treating NAFLD, in particular, NASH.
    Type: Grant
    Filed: September 14, 2018
    Date of Patent: April 6, 2021
    Assignee: APTABIO THERAPEUTICS INC.
    Inventors: Sung Hwan Moon, Soo Jin Lee, Sung Chan Lee, Yun Soo Bae
  • Thromboxane receptor antagonists
    Patent number: 10966994
    Abstract: The invention relates to novel chemical entities that act as thromboxane (TX) A2 receptor, or T prostanoid receptor (TP), antagonists and to their use in the treatment of human diseases in which thromboxane (TX) A2 and of all other agents that act as incidental ligands of TP play a role. Compounds are-represented by the formula (I): wherein: R1 is selected from the group consisting of a difluoromethoxy group, a trifluoromethoxy group, a difluoromethyl group, a primary amide, a secondary amide group, a tertiary amide group, and a nitrile group; and R2 is selected from the group consisting of an alkyl group of 6 or fewer carbons and a halogenated alkyl group of 6 or fewer carbons, wherein R2 is not tert butyl, or a pharmaceutically acceptable salt thereof.
    Type: Grant
    Filed: July 22, 2019
    Date of Patent: April 6, 2021
    Assignee: ATXA THERAPEUTICS LIMITED
    Inventors: B. Therese Kinsella, Helen Reid
  • 2-(3,4-dihydroxyphenyl)ethyl 3-hydroxybutanoate, composition, and method for improving function of aortic endothelial cell
    Patent number: 10947179
    Abstract: The disclosure relates to a compound, 2-(3,4-dihydroxyphenyl)ethyl 3-hydroxybutanoate, for improving aortic endothelial cell function and use thereof. The compound is capable of inhibiting inflammatory response of the human aortic endothelial cells caused by a saturated fatty acid, and preventing an occurrence and progression of atherosclerosis. The compound is capable of reducing human aortic endothelial inflammation caused by a saturated fatty acid, for example, reducing the mRNA levels of interleukin-6 (IL-6), and is capable of effectively protecting the function of mitochondria in human aortic endothelium from being damaged by a saturated fatty acid, for example, increasing the expression of mitochondrial complex I.
    Type: Grant
    Filed: September 26, 2019
    Date of Patent: March 16, 2021
    Assignee: XI'AN JIAOTONG UNIVERSITY
    Inventors: Jian-Kang Liu, Xu-Yun Liu, Ya-Chong Hu, Lin Zhao, Yong-Yao Wang, Cai-Yue Zhu, Zhen Wang, Jing Lou, Qing-Qing Ma, Yu-Xia Zhang, Qing-Lin Jiang, Xiao-Hong Xu, Ting-Hua Zhang, Jian-Gang Long
  • Salt type and crystal type of 4h-pyrazolo [1, 5-alpha] benzimidazole compound and preparation method and intermediate thereof
    Patent number: 10941150
    Abstract: Disclosed in the present invention are a salt type and crystal type of 4H-pyrazolo[1, 5-alpha]benzimidazole compound and the preparation method and intermediate thereof. The 4H-pyrazolo[1,5-alpha]benzimidazole compound has the structure of Compound 2.
    Type: Grant
    Filed: August 22, 2019
    Date of Patent: March 9, 2021
    Assignees: HUBEI BIO-PHARMACEUTICAL INDUSTRIAL TECHNOLOGICAL INSTITUTE INC., HUMANWELL HEALTHCARE (GROUP) CO., LTD.
    Inventors: Xuehai Wang, Charles Z. Ding, Jie Shen, Shuhui Chen, Lie Li, Gang Li, Yong Xu, Cailin Wang, Ronghua Tu, Jimeng Wang, Yang YuE, Biao Deng, Hailiang Chen, Hui Liu, Wenjie Sun, Cong Wang, Lu Huang, Zheng Wang, Weidong Li
  • Crystalline forms of 5-chloro-N4-[-2-(dimethylphosphoryl) phenyl]-N2-{2-methoxy-4-[4-(4-methylpiperazin-1-yl) piperidin-1-yl] phenyl} pyrimidine-2,4-diamine
    Patent number: 10934317
    Abstract: Crystalline forms of brigatinib, pharmaceutical compositions comprising the same, and methods of their preparation and use of the same are disclosed herein.
    Type: Grant
    Filed: June 3, 2019
    Date of Patent: March 2, 2021
    Assignee: ARIAD Pharmaceuticals, Inc.
    Inventors: Leonard W. Rozamus, Pradeep Sharma
  • Crystalline forms of 4-(2-((1R,2R)-2-hydroxycyclohexylamino)benzothiazol-6-yloxy)-N-methylpicolinamide
    Patent number: 10934273
    Abstract: This application relates to various crystalline forms of 4-(2-((1R,2R)-2-hydroxycyclohexylamino)benzothiazol-6-yloxy)-N-methylpicolinamide hydrochloride salts as well as compositions and methods of using the same. In some embodiments the crystalline forms also contain water (“hydrates”). These materials are useful in the treatment of various diseases, including glioblastoma multiforme, breast cancer, pancreatic cancer and other solid tumors.
    Type: Grant
    Filed: October 13, 2017
    Date of Patent: March 2, 2021
    Assignee: Novartis AG
    Inventors: Arnaud Grandeury, Liladhar Murlidhar Waykole
  • Heterocyclic containing cyclopropyl FXR modulators
    Patent number: 10899723
    Abstract: The present technology is directed to compounds of formula (II) as well as compositions thereof and methods related to modulation of FXR. In particular, the present compounds and compositions may be used to treat FXR-mediated disorders and conditions, including, e.g., liver disease, hyperlipidemia, hypercholesteremia, obesity, metabolic syndrome, cardiovascular disease, gastrointestinal disease, and atherosclerosis, and renal disease.
    Type: Grant
    Filed: September 27, 2017
    Date of Patent: January 26, 2021
    Assignee: Hepagene Therapeutics (HK) Limited
    Inventor: Xiaodong Xu
  • Solid forms of an sGC stimulator
    Patent number: 10889577
    Abstract: The present disclosure relates to crystalline solid forms of a stimulator of soluble guanylate cyclase (sGC), Compound I: Also provided herein are methods for the preparation of these solid forms. The invention also relates to pharmaceutical formulations and dosage forms comprising these solid forms and their uses thereof, alone or in combination with one or more additional agents, for treating and/or preventing various diseases or disorders; these diseases or disorders are ones that may benefit from sGC stimulation or from an increase in the concentration of nitric oxide (NO) and/or cyclic guanosine monophosphate (cGMP).
    Type: Grant
    Filed: July 6, 2017
    Date of Patent: January 12, 2021
    Assignee: Cyclerion Therapeutics, Inc.
    Inventors: Vasu Sethuraman, Ahmad Hashash, Song Xue, Robert C. Livingston, Kwame Wiredu Nti-Addae
  • Process for preparing electron deficient olefins
    Patent number: 10889542
    Abstract: This invention relates to a process for preparing electron deficient olefins, such as 2-cyanoacrylates, using an acid catalyzed two-step process including a transesterification reaction followed by a Knoevenagel condensation reaction.
    Type: Grant
    Filed: June 12, 2019
    Date of Patent: January 12, 2021
    Assignee: Henkel IP & Holding GmbH
    Inventors: Cormac Duffy, Marisa Phelan, Barry Burns
  • Azetidine derivatives useful as modulators of cortical catecholaminergic neurotransmission
    Patent number: 10875829
    Abstract: The disclosure provides a pharmaceutical composition comprising a therapeutically effective amount of a compound of Formula (I): (I) or an isotope labelled analog thereof, or a pharmaceutically acceptable salt thereof, wherein: each of R1, R2, R3, R6 and R7 represents H or F, R4 represents H or CH3 R5 represents H or C1-C4alkyl, wherein at least two of R1, R2, R3, R6 and R7 represent F, together with at least one pharmaceutically acceptable carrier, excipient and/or diluent.
    Type: Grant
    Filed: November 17, 2017
    Date of Patent: December 29, 2020
    Assignee: INTEGRATIVE RESEARCH LABORATORIES SWEDEN AB
    Inventors: Clas Sonesson, Fredrik Pettersson
  • Aryl and heteroaryl amides for use as anti-proliferative, anti-thrombotic, and anti-viral agents
    Patent number: 10851096
    Abstract: Certain compounds of formula I: I and salts including pharmaceutically acceptable salts thereof are disclosed. Also disclosed are pharmaceutical compositions comprising a compound of formula I, processes for preparing compounds of formula I, intermediates useful for preparing compounds of formula I and therapeutic methods using a compound of formula I.
    Type: Grant
    Filed: June 16, 2017
    Date of Patent: December 1, 2020
    Assignees: Rutgers, The State University of New Jersey, The Curators of the University of Missouri
    Inventors: William J. Welsh, Raymond Birge, Vladyslav Kholodovych, Youyi Peng, Thomas Walter Comollo, Stanley G. Kimani, Kamlendra Singh
  • Process for the production of cannabidiol and delta-9-tetrahydrocannabinol
    Patent number: 10844035
    Abstract: The present disclosure relates to a cannabidiol compound and compositions thereof and processes for preparing the compound and compositions. The processes include an acid-catalyzed reaction of a suitably selected and substituted di-bromo-olivetol or derivative thereof with a suitably selected and substituted cyclic alkene to produce a dibromo-cannabidiol compound or derivative thereof. The dibromo-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: July 13, 2018
    Date of Patent: November 24, 2020
    Assignee: PURISYS LLC
    Inventors: Lukas Dialer, Denis Petrovic, Ulrich Weigl
  • Methods for preparing antibody-drug conjugates
    Patent number: 10815309
    Abstract: This invention describes a method of conjugating a cell binding agent such as an antibody with an effector group (e.g., a cytotoxic agent) or a reporter group (e.g., a radionuclide), whereby the reporter or effector group is first reacted with a bifunctional linker and the mixture is then used without purification for the conjugation reaction with the cell binding agent. The method described in this invention is advantageous for preparation of stably-linked conjugates of cell binding agents, such as antibodies with effector or reporter groups. This conjugation method provides in high yields conjugates of high purity and homogeneity that are without inter-chain cross-linking and inactivated linker residues.
    Type: Grant
    Filed: February 1, 2019
    Date of Patent: October 27, 2020
    Assignee: IMMUNOGEN, INC.
    Inventors: Brenda A. Kellogg, Rajeeva Singh, Ravi V. Chari