Patents Examined by Laura L. Stockton
  • Patent number: 11028073
    Abstract: The invention discloses a butylphthalide-telmisartan heterocomplex, a preparation method and an application thereof. The invention specifically relates to an optically active ring-opening butylphthalide-telmisartan heterocomplex shown in formula I or a pharmaceutically acceptable salt or ester thereof, a preparation method thereof, a pharmaceutical composition containing the compounds, and a pharmaceutical application thereof, particularly application in prevention and treatment of neuroinflammation-related diseases, including ischemic stroke, Alzheimer's disease, brain trauma, Parkinson's disease, multiple sclerosis, depression and so on.
    Type: Grant
    Filed: January 4, 2018
    Date of Patent: June 8, 2021
    Inventors: Zhangjian Huang, Tao Pang, Cunfang Wang, Wenbin Zeng, Jinxiang Deng, Weijie Wu, Tingyu Huang
  • Patent number: 11028095
    Abstract: Disclosed are compounds having potency in the modulation of NMDA receptor activity. Such compounds can be used in the treatment of conditions such as depression and related disorders. Orally delivered formulations and other pharmaceutically acceptable delivery forms of the compounds, including intravenous formulations, are also disclosed.
    Type: Grant
    Filed: August 1, 2017
    Date of Patent: June 8, 2021
    Assignee: Aptinyx Inc.
    Inventor: M. Amin Khan
  • Patent number: 11028087
    Abstract: The present invention relates to novel 2,6-disubstituted-9-cyclopentyl-9H-purines of general formula I, capable of inhibiting the activity of kinases such as FLT3, CDKs and PDGFRs in cancer and other related proliferative diseases. The invention further includes pharmaceutical compositions containing the 2,6-disubstituted-9-cyclopentyl-9H-purines. Compounds of the present invention can be used as active ingredients of a pharmaceutical compositions for treating acute myeloid leukemia (AML).
    Type: Grant
    Filed: March 19, 2018
    Date of Patent: June 8, 2021
    Inventors: Tomas Gucky, Eva Reznickova, Radek Jorda, Vladimir Krystof, Miroslav Strnad, Tereza Radosova Muchova, Vladimir Divoky
  • Patent number: 11028054
    Abstract: The present invention provides 1, 4, 6-trisubstituted-2-alkyl-1H-benzo[d]imidazole derivatives as dihydroorotate oxygenase inhibitor compounds of formula (I), which may be therapeutically useful as DHODH inhibitors, in which R1 to R3 and ‘m’ have the meanings given in the specification, and pharmaceutically acceptable salts or stereoisomer thereof that are useful in the treatment and prevention in diseases or disorder, in particular their use in diseases or disorder where there is an advantage in inhibiting DHODH. The present invention also provides methods for synthesizing 1, 4, 6-trisubstituted-2-alkyl-1H-benzo[d]imidazole derivatives of formula (I). The present invention also provides pharmaceutical formulations comprising at least one of the DHODH inhibitor compound of formula (I) together with a pharmaceutically acceptable carrier, diluent or excipient.
    Type: Grant
    Filed: February 23, 2018
    Date of Patent: June 8, 2021
    Assignee: Merck Patent GmbH
    Inventors: Siva Sanjeeva Rao Thunuguntla, Subramanya Hosahalli, Sunil Kumar Panigrahi, Matthias Schwarz, Michael Arit
  • Patent number: 11028055
    Abstract: The present disclosure provides compounds of Formula (I). The compounds described herein may be useful in treating and/or preventing proliferative diseases (e.g., cancer). Also provided in the present disclosure are pharmaceutical compositions, kits, methods, and uses including or using a compound described herein.
    Type: Grant
    Filed: November 30, 2016
    Date of Patent: June 8, 2021
    Assignees: Children's Medical Center Corporation, Beth Israel Deaconess Medical Center, Inc.
    Inventors: Bruce R. Zetter, Lijun Sun
  • Patent number: 11021466
    Abstract: Provided herein are small molecule inhibitors for the targeting or IRE1 protein family members. Binding may be direct or indirect. Further provided herein are methods of using IRE1 small molecule inhibitors for use in treating or ameliorating cancer in a subject. Moreover, IRE1 small molecule inhibitors described herein are for the treatment of cancer, where the cancer is a solid or hematologic cancer.
    Type: Grant
    Filed: August 16, 2019
    Date of Patent: June 1, 2021
    Assignee: Cornell University
    Inventors: Joseph P. Vacca, Dansu Li, Sarah Bettigole
  • Patent number: 11013718
    Abstract: Provided are novel compounds of Formula (I or Ia?): and pharmaceutically acceptable salts thereof, which are useful for treating a variety of diseases, disorders or conditions, associated with LSD1. Also provided are pharmaceutical compositions comprising the novel compounds of Formula (I or Ia?), pharmaceutically acceptable salts thereof, and methods for their use in treating one or more diseases, disorders or conditions, associated with LSD1.
    Type: Grant
    Filed: November 1, 2019
    Date of Patent: May 25, 2021
    Assignee: Constellation Pharmaceuticals, Inc.
    Inventors: Francois Brucelle, Victor S. Gehling, Avinash Khanna
  • Patent number: 11014881
    Abstract: Described herein are hepatitis B capsid assembly modulators and pharmaceutical compositions comprising said compounds. The subject compounds and compositions are useful for the treatment of hepatitis B.
    Type: Grant
    Filed: November 1, 2019
    Date of Patent: May 25, 2021
    Inventors: Christopher J. Burns, Glen Coburn, Bin Liu, Jiangchao Yao, Christopher Benetatos, Steven A. Boyd, Stephen M. Condon, Thomas Haimowitz
  • Patent number: 11014943
    Abstract: Disclosed in the present application are a compound represented by formula (I), or a pharmaceutically acceptable salt, a tautomer thereof, a stereoisomer thereof, or a geometrical isomer thereof, and uses thereof in the preparation of drugs for treating or preventing multiple myeloma.
    Type: Grant
    Filed: February 28, 2018
    Date of Patent: May 25, 2021
    Inventors: Jian Xiong, Cheng Xie, Kevin X Chen, Xiongbin Xu, Xuejin Zhang, Zhen Gong, Jian Li, Shuhui Chen, Aiming Zhang, Zhulian Jiang, Xiquan Zhang, Xin Tian
  • Patent number: 11008311
    Abstract: The preparation method for the compound, composition and application thereof in preparing an angiotensin II receptor antagonist or application in preparing medicine for preventing and/or treating hypertension, chronic heart failure and diabetic nephropathy. After entering a human body, when releasing azilsartan, the compound releases hydroxyligustrazine or NO at the same time, thus generating a synergistic effect with azilsartan. The compound therefore has stronger and longer blood pressure lowering effect, more obvious and longer lasting heart rate lowering effect and high safety, and achieves ideal protective effect for heart and kidney functions.
    Type: Grant
    Filed: May 19, 2017
    Date of Patent: May 18, 2021
    Inventors: Sijun Lei, Xiang Fang, Yongkai Chen, Wei Feng, Chaodong Wang
  • Patent number: 10995087
    Abstract: Disclosed are a crystal form of a URAT1 inhibitor, and a preparation method therefor.
    Type: Grant
    Filed: November 20, 2018
    Date of Patent: May 4, 2021
    Inventors: Jianfei Wang, Yang Zhang, Wenyuan Zhu, Jian Li, Shuhui Chen
  • Patent number: 10995067
    Abstract: Disclosed herein are novel uses of a polyhydroxylated pyrrolidine for the manufacture of a medicament for treating Fabry disease (FD). Accordingly, the present disclosure provides a method of treating a subject having or suspected of having FD. The method includes the step of, administering to the subject a therapeutically effective amount of a compound of formula (I), a salt, an ester or a solvate thereof, wherein: R1 is H, or C1-3 amine optionally substituted with —COR2; R2 is alkyl or alkene optionally substituted with cycloalkyl or phenyl having at least one substituent selected from the group consisting of, halo, alkyl, haloalkyl, and alkoxyl; so as to ameliorate, alleviate mitigate and/or prevent symptoms associated with the FD. According to preferred embodiments of the present disclosure, the compound of formula (I) is a chaperon of a mutated human lysosomal ?-galactosidase A (?-Gal A).
    Type: Grant
    Filed: June 14, 2017
    Date of Patent: May 4, 2021
    Inventor: Wei-Chieh Cheng
  • Patent number: 10995089
    Abstract: The present invention concerns a compound of formula (I): H or one of its pharmaceutically acceptable salts, especially for use as inhibitors of the ERK kinase activity in particular ERK2 activity, it also concerns prodrugs of these compounds.
    Type: Grant
    Filed: November 17, 2016
    Date of Patent: May 4, 2021
    Inventors: Jean-François Guichou, Cédric Bories, Clément Geoffroy, Charline Duquenne, Muriel Gelin, Gilles Labesse, Yannick Bessin, Loic Mathieu
  • Patent number: 10988466
    Abstract: This invention relates to certain novel pyrazine derivatives (Formula I) as SHP2 inhibitors which is shown as formula I, their synthesis and their use for treating a SHP2 mediated disorder. More particularly, this invention is directed to fused heterocyclic group derivatives useful as inhibitors of SHP2, methods for producing such compounds and methods for treating a SHP2-mediated disorder.
    Type: Grant
    Filed: March 23, 2018
    Date of Patent: April 27, 2021
    Assignee: Jacobio Pharmaceuticals Co., Ltd.
    Inventors: Cunbo Ma, Panliang Gao, Shaojing Hu, Zilong Xu, Huifeng Han, Xinping Wu, Di Kang
  • Patent number: 10988484
    Abstract: Provided herein are compounds that modulate glucose uptake activity and are useful for treating cancer, autoimmune diseases, inflammation, infectious diseases, and metabolic diseases. In certain embodiments, the compounds modulate glucose uptake activity by modulating cellular components, including, but not limited to those related to glycolysis and the known transporters/co-transporters of glucose such as GLUT1 and other GLUT family members/alternative hexose transporters. In certain embodiments, the compounds have the structure of formula I: wherein the variables have the values disclosed herein.
    Type: Grant
    Filed: April 29, 2019
    Date of Patent: April 27, 2021
    Assignee: Kadmon Corporation, LLC
    Inventors: Kellen L. Olszewski, Ji-In Kim, Masha V. Poyurovsky, Kevin G. Liu, Anthony Barsotti, Koi Morris
  • Patent number: 10988465
    Abstract: The present invention provides compounds, compositions thereof, and methods of using the same.
    Type: Grant
    Filed: June 21, 2017
    Date of Patent: April 27, 2021
    Inventors: Elyse Marie Josee Bourque, Renato Skerlj
  • Patent number: 10981900
    Abstract: The present disclosure relates to a series of tricyclic compounds and the use thereof as receptor agonists of sphingosine-1-phosphate subtype 1 (S1P1), and in particular relates to compounds as shown in formula (I) or pharmaceutically acceptable salts thereof.
    Type: Grant
    Filed: February 28, 2018
    Date of Patent: April 20, 2021
    Inventors: Peng Zhang, Lingyun Wu, Jun Yin, Jian Li, Shuhui Chen
  • Patent number: 10975287
    Abstract: Disclosed are compounds having the formula: wherein Ra, R1, R2, R3, R4, R5, R6, R7, and R8, are as defined herein, or a salt, particularly a pharmaceutically acceptable salt, thereof.
    Type: Grant
    Filed: April 5, 2017
    Date of Patent: April 13, 2021
    Inventors: Adam Kenneth Charnley, Michael G. Darcy, Jason W. Dodson, Terry V. Hughes, Yue Li, Yiqian Lian, Neysa Nevins, Joshi M. Ramanjulu
  • Patent number: 10975078
    Abstract: The invention provides compounds of Formula (I) as described herein, along with pharmaceutically acceptable salts, pharmaceutical compositions containing such compounds, and methods to use these compounds, salts and compositions for treating viral infections, particularly infections caused by hepatitis B virus, and reducing the occurrence of serious conditions associated with HBV.
    Type: Grant
    Filed: March 4, 2020
    Date of Patent: April 13, 2021
    Assignee: NOVARTIS AG
    Inventors: Jiping Fu, Wooseok Han, Subramanian Karur, Peichao Lu, Keith Bruce Pfister, Joseph Michael Young
  • Patent number: 10968210
    Abstract: Disclosed are compounds of Formula A, or a salt thereof: Formula (A), wherein: Het, Q and R1A to R4A are defined herein, which compounds have properties for blocking Nav 1.7 ion channels found in peripheral and sympathetic neurons. Also described are pharmaceutical formulations comprising the compounds of Formula A or their salts, and methods of treating cough, itch, acute pain and neuropathic pain disorders using the same.
    Type: Grant
    Filed: November 13, 2017
    Date of Patent: April 6, 2021
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Thomas J. Greshock, James Mulhearn, Anthony J. Roecker, Tianying Jian, Gang Zhou, Liangqin Guo, Walter Won, Ting Zhang, Rajan Anand, John E. Stelmach, Deping Wang, Ronald M. Kim, Mark E. Layton, Christopher S. Burgey, Philippe G. Nantermet