Patents Examined by Ebenezer O. Sackey
  • Pyrazole derivative as ALK5 inhibitor and uses thereof
    Patent number: 10954232
    Abstract: The present disclosure relates to a novel substituted pyrazole derivative having an effect of inhibiting serine/threonine kinase activity targeting receptor ALK5 of TGF-?, and a pharmaceutical composition including the compound of the present disclosure as an active ingredient may be useful in preventing and/or treating cancers, autoimmune diseases, fibrotic diseases, inflammatory diseases, neurodegenerative diseases, infectious diseases, pulmonary diseases, cardiovascular diseases or metabolic diseases, or other diseases associated with a decrease in TGF family signaling activity.
    Type: Grant
    Filed: June 30, 2017
    Date of Patent: March 23, 2021
    Assignee: HANMI PHARMACEUTICAL CO., LTD.
    Inventors: Kyung Ik Lee, Young Hee Jung, Ji Young Song, Seung Ah Jun
  • Sigma receptor binders
    Patent number: 10954217
    Abstract: Provided herein, inter alia, are compounds and methods of treating diseases including cancer, neurological disease, alcohol withdrawal, depression and anxiety, and neuropathic pain.
    Type: Grant
    Filed: April 29, 2017
    Date of Patent: March 23, 2021
    Assignee: BOARD OF REGENTS, THE UNIVERSITY OF TEXAS SYSTEM
    Inventors: Stephen F. Martin, James J. Sahn, Kathryn Taylor Linkens
  • Solid forms of an epidermal growth factor receptor kinase inhibitor
    Patent number: 10946016
    Abstract: The present invention provides a solid form and compositions thereof, which are useful as an inhibitor of EGFR kinases and which exhibit desirable characteristics for the same.
    Type: Grant
    Filed: June 22, 2018
    Date of Patent: March 16, 2021
    Assignee: Celgene CAR LLC
    Inventor: Mei Lai
  • Kinase inhibitors
    Patent number: 10941115
    Abstract: There are provided compounds of formula I, wherein R1A to R1E, R2 to R4, R5a, L and X1 to X3 have meanings given in the description, which compounds have anti-inflammatory activity (e.g. through inhibition of one or more of members of: the family of p38 mitogen-activated protein kinase enzymes; Syk kinase; and members of the Src family of tyrosine kinases) and have use in therapy, including in pharmaceutical combinations, especially in the treatment of inflammatory diseases, including inflammatory diseases of the lung, eye and intestines.
    Type: Grant
    Filed: July 10, 2019
    Date of Patent: March 9, 2021
    Assignee: Oxular Acquisitions Limited
    Inventors: Thomas Matthew Baker, Matthew Colin Thor Fyfe, Geraint Jones, Stephen Malcolm Thom
  • Compound and photoelectric device, image sensor and electronic device including the same
    Patent number: 10937970
    Abstract: A compound of Chemical Formula 1, and a photoelectric device, an image sensor, and an electronic device including the same are disclosed: In Chemical Formula 1, each substituent is the same as defined in the detailed description.
    Type: Grant
    Filed: October 31, 2018
    Date of Patent: March 2, 2021
    Assignee: Samsung Electronics Co., Ltd.
    Inventors: Taejin Choi, Sang Mo Kim, Sung Young Yun, Youn Hee Lim, Katsunori Shibata, Hiromasa Shibuya, Gae Hwang Lee, Norihito Ishii, Dong-Seok Leem, Yong Wan Jin, Yeong Suk Choi, Jong Won Choi, Hyesung Choi
  • Process for preparing bortezomib, intermediates, and crystalline forms thereof
    Patent number: 10934315
    Abstract: The present disclosure provides a process for preparing Bortezomib, intermediates, and crystalline forms thereof.
    Type: Grant
    Filed: November 1, 2018
    Date of Patent: March 2, 2021
    Assignee: PHARMACORE BIOTECH CO., LTD.
    Inventors: Wei-Hong Tseng, Vallapa Soong, Hsing Yu Chang, Shen Han Yang
  • Compositions and methods for treating cancer
    Patent number: 10927070
    Abstract: Provided herein are compositions and methods for treating, inhibiting and/or reducing the severity of cancer in subjects in need thereof. The methods include providing an agent that inhibits expression or activity of ONECUT2 and administering a therapeutically effective amount of the agent so as to treat, inhibit and/or reduce the severity of cancer in the subject.
    Type: Grant
    Filed: May 26, 2017
    Date of Patent: February 23, 2021
    Assignee: Cedars-Sinai Medical Center
    Inventors: Michael Freeman, Mirja Rotinen, Ramachandran Murali, Sungyong You
  • Efficient process for the preparation of sitagliptin through a very effective preparation of the intermediate 2,4,5-trifluorophenylacetic acid
    Patent number: 10913747
    Abstract: Object of the present invention is an efficient process for the preparation of the active pharmaceutical ingredient Sitagliptine and the 2,4,5-trifluorophenylacetic acid (TFAA) and salt thereof, which is a key intermediate for the synthesis of Sitagliptine.
    Type: Grant
    Filed: May 15, 2018
    Date of Patent: February 9, 2021
    Assignee: F.I.S.—FABBRICA ITALIANA SINTETICI S.P.A.
    Inventors: Ottorino De Lucchi, Pierluigi Padovan, Elena Brasola
  • Heterocyclic degronimers for target protein degradation
    Patent number: 10905768
    Abstract: This invention provides heterocyclic compounds that bind to E3 Ubiquitin Ligase (typically through cereblon) (“Degrons”), which can be used as is or linked to a Targeting Ligand for a selected Target Protein for therapeutic purposes and methods of use and compositions thereof as well as methods for their preparation.
    Type: Grant
    Filed: May 11, 2020
    Date of Patent: February 2, 2021
    Assignee: C4 Therapeutics, Inc.
    Inventors: Andrew J. Phillips, Chris G. Nasveschuk, James A. Henderson, Yanke Liang, Mark E. Fitzgerald, Minsheng He, Ryan E. Michael
  • Kinase inhibitors for the treatment of disease
    Patent number: 10906878
    Abstract: The invention relates to compounds and their use in the treatment of disease. Novel irreversible inhibitors of wild-type and mutant forms of EGFR, FGFR, ALK, ROS, JAK, BTK, BLK, ITK, TEC, and/or TXK and their use for the treatment of cell proliferation disorders are described.
    Type: Grant
    Filed: May 6, 2019
    Date of Patent: February 2, 2021
    Assignee: DANA FARBER CANCER INSTITUTE, INC.
    Inventors: Nathanael S. Gray, Hwan G. Choi, Li Tan
  • Benzylamino substituted quinazolines and derivatives as SOS1 inhibitors
    Patent number: 10898487
    Abstract: The present invention encompasses compounds of formula (I), wherein the groups R1 to R7 have the meanings given in the claims and specification, their use as inhibitors of SOS1, pharmaceutical compositions which contain compounds of this kind and their use as medicaments/medical uses, especially as agents for treatment and/or prevention of oncological diseases.
    Type: Grant
    Filed: December 21, 2017
    Date of Patent: January 26, 2021
    Assignee: Boehringer Ingelheim International GmbH
    Inventors: Dirk Kessler, Christiane Kofink, Matthew Russell Netherton, Juergen Ramharter, Tobias Wunberg
  • Method for synthesizing novel chiral ligand, metal chelate, a variety of non-natural amino acids, maraviroc and key intermediate thereof
    Patent number: 10875883
    Abstract: Disclosed is a method for synthesizing a novel chiral ligand, a metal chelate, a variety of non-natural amino acids, Maraviroc and a key intermediate thereof. In the invention, (R)-2-methyl proline is selected and used as a starting raw material, (S)-?3-amino acid is obtained by asymmetric resolution induced by using a nickel chelate, and Maraviroc is synthesized by using (S)-3-amino-3-phenylpropionic acid as a key intermediate with a high yield and the ee value reaching 98.2% or more. The method of the present invention has widely available materials, mild synthetic process conditions, is easy to control, and produces a product of a high optical purity.
    Type: Grant
    Filed: September 19, 2017
    Date of Patent: December 29, 2020
    Assignee: SHANGHAI INSTITUTE OF MATERIA MEDICA, CHINESE ACADEMY OF SCIENCES
    Inventors: Hong Liu, Jiang Wang, Shengbin Zhou, Panfeng Peng, Yong Nian, Shuni Wang, Shuangjie Shu, Hao Shen, Hualiang Jiang, Kaixian Chen
  • Process for preparing (cyclopentyl[d]pyrimidin-4-yl)piperazine compounds
    Patent number: 10870626
    Abstract: The present disclosure relates to processes for preparing (cyclopentyl[d]pyrimidin-4-yl)piperazine compounds, and more particularly relates to processes for preparing (R)-4-(5-methyl-7-oxo-6,7-dihydro-5H-cyclopenta[d] pyrimidin-4-yl)piperazine and N-protected derivatives thereof, which may be used as an intermediate in the synthesis of Ipatasertib (i.e., (S)-2-(4-chlorophenyl)-1-(4-((5R,7R)-7-hydroxy-5-methyl-6,7-dihydro-5H-cyclopenta[d]pyrimidin-4-yl)piperazin-1-yl)-3-(isopropylamino)-propan-1-one). The present disclosure additionally relates to various compounds that are intermediates employed in these processes.
    Type: Grant
    Filed: September 18, 2019
    Date of Patent: December 22, 2020
    Assignees: F. Hoffman-La Roche AG, Genentech, Inc.
    Inventors: Francis Gosselin, Chong Han, Hans Iding, Reinhard Reents, Scott Savage, Beat Wirz
  • Salt of quinazoline derivative, preparation method therefor and application thereof
    Patent number: 10870627
    Abstract: A salt of a quinazoline derivative (N-[4-(3-chlorine-4-fluoroanilino)]-7-(3-morpholinepropanol)-6-(2-fluoroacrylamide)-quinazoline, the structure thereof is as represented by formula I). Compared with a known quinazoline derivative, the salt of the quinazoline derivative has one or more improved properties and at least has better water solubility, wherein a citrate, a benzene sulfonate, and an ethanedisulphonate thereof further have better crystallinity and are not easy to absorb moisture.
    Type: Grant
    Filed: September 22, 2017
    Date of Patent: December 22, 2020
    Assignee: SHANGHAI PHARMACEUTICALS HOLDING CO., LTD.
    Inventors: Guangxin Xia, Di Li, Ning Zhou, Ao Chen, Liang Zhao, Jiansheng Han, Yanjun Liu
  • Dibenzo azepine compounds and their use in the treatment of otic diseases and disorders
    Patent number: 10865188
    Abstract: The present disclosure provides crystalline Compound I and crystalline Compound II, pharmaceutical compositions comprising one of said crystalline compounds suitable for intratympanic administration, and methods for treating otic disorders using the crystalline compounds and the pharmaceutical compositions.
    Type: Grant
    Filed: March 4, 2019
    Date of Patent: December 15, 2020
    Assignee: Pipeline Therapeutics, Inc.
    Inventors: Thomas Jon Seiders, Catherine Yuling Lee, Yiwei Li
  • Inhibitors of cyclin-dependent kinase 7 (CDK7)
    Patent number: 10865206
    Abstract: The present invention provides novel compounds of Formula (I) and pharmaceutically acceptable salts, solvates, hydrates, tautomers, stereoisomers, isotopically labeled derivatives, and compositions thereof. Also provided are methods and kits involving the compounds or compositions for treating or preventing proliferative diseases (e.g., cancers (e.g., leukemia, melanoma, multiple myeloma), benign neoplasms, angiogenesis, inflammatory diseases, autoinflammatory diseases, and autoimmune diseases) in a subject. Treatment of a subject with a proliferative disease using a compound or composition of the invention may inhibit the aberrant activity of cyclin-dependent kinase (e.g., CDK7), and therefore induce cellular apoptosis and/or inhibit transcription in the subject.
    Type: Grant
    Filed: May 15, 2019
    Date of Patent: December 15, 2020
    Assignee: Syros Pharmaceuticals, Inc.
    Inventors: Stephane Ciblat, Anzhelika Kabro, Melissa Leblanc, Serge Leger, Jason J. Marineau, Tom Miller, Stephanie Roy, Darby Schmidt, M. Arshad Siddiqui, Kevin Sprott, Dana K. Winter, Amy Ripka, Dansu Li, Guoli Zhang
  • Pyridone derivatives for the treatment of viral infections and further diseases
    Patent number: 10865193
    Abstract: This invention relates to pyridone derivatives, processes for their preparation, pharmaceutical compositions, and their use in therapy.
    Type: Grant
    Filed: June 5, 2019
    Date of Patent: December 15, 2020
    Assignee: JANSSEN SCIENCES IRELAND UNLIMITED COMPANY
    Inventors: David Craig McGowan, Pierre Jean-Marie Bernard Raboisson
  • Compounds
    Patent number: 10858367
    Abstract: Provided are novel compounds that inhibit LRRK2 kinase activity, processes for their preparation, compositions containing them and their use in the treatment of or prevention of diseases associated with or characterized by LRRK2 kinase activity, for example Parkinson's disease, Alzheimer's disease and amyotrophic lateral sclerosis (ALS).
    Type: Grant
    Filed: January 23, 2018
    Date of Patent: December 8, 2020
    Assignee: GLAXOSMITHKLINE INTELLECTUAL PROPERTY DEVELOPMENT LIMITED
    Inventors: Xiao Ding, Feng Ren, Yingxia Sang, Weiqiang Xing, Yang Zhan, Baowei Zhao
  • C3-carbon linked glutarimide degronimers for target protein degradation
    Patent number: 10849982
    Abstract: This invention provides Degronimers that have carbon-linked E3 Ubiquitin Ligase targeting moieties (Degrons), which can be linked to a targeting ligand for a protein that has been selected for in vivo degradation, and methods of use and compositions thereof as well as methods for their preparation.
    Type: Grant
    Filed: November 9, 2018
    Date of Patent: December 1, 2020
    Assignee: C4 Therapeutics, Inc.
    Inventors: Andrew J. Phillips, Chris G. Nasveschuk, James A. Henderson, Yanke Liang, Minsheng He, Kiel Lazarski, Gesine Kerstin Veits, Harit U. Vora
  • Heterocyclic compounds as RET kinase inhibitors
    Patent number: 10844067
    Abstract: The present invention relates to compounds of formula I that function as inhibitors of RET (rearranged during transfection) kinase enzyme activity: wherein HET, X1, X2, X3, X4, integer a and R3 are each as defined herein. The present invention also relates to processes for the preparation of these compounds, to pharmaceutical compositions comprising them, and to their use in the treatment of proliferative disorders, such as cancer, as well as other diseases or conditions in which RET kinase activity is implicated.
    Type: Grant
    Filed: April 18, 2017
    Date of Patent: November 24, 2020
    Assignee: Cancer Research Technology Limited
    Inventors: Allan Michael Jordan, Rebecca Newton, Bohdan Waszkowycz, Jonathan Mark Sutton, George Hynd, Silvia Paoletta, Euan Alexander Fraser Fordyce