Patents Examined by Sagar Patel
  • C-anilinoquinazoline compounds and their use in treating cancer
    Patent number: 10829479
    Abstract: The invention concerns compounds of Formula (I): or pharmaceutically acceptable salts thereof, wherein R1, R2, R3 and R4 have any of the meanings hereinbefore defined in the description; process for their preparation; pharmaceutical compositions containing them and their use in treating KIT mediated diseases.
    Type: Grant
    Filed: March 5, 2019
    Date of Patent: November 10, 2020
    Assignee: AstraZeneca AB
    Inventors: Jason Kettle, Stuart Pearson, Martin Packer, James Smith, Tudor Grecu
  • Compositions and methods for the treatment of Parkinson's disease
    Patent number: 10829454
    Abstract: The invention relates to the compounds of formula I, formula II and formula III or its pharmaceutical acceptable salts, as well as polymorphs, solvates, enantiomers, stereoisomers and hydrates thereof. The pharmaceutical compositions comprising an effective amount of compounds of formula I, formula II and formula III, and methods for treating or preventing Parkinson's disease may be formulated for oral, buccal, rectal, topical, transdermal, transmucosal, intravenous, parenteral administration, syrup, or injection. Such compositions may be used to treatment or management of Parkinson's disease such as Parkinson's disease, scleroderma, restless leg syndrome, hypertension and gestational hypertension.
    Type: Grant
    Filed: September 2, 2016
    Date of Patent: November 10, 2020
    Assignee: Cellix Bio Private Limited
    Inventor: Mahesh Kandula
  • Compounds for inhibiting NS3 and compositions containing the inhibited protein
    Patent number: 10821096
    Abstract: Imidazole-based compounds as hepatitis C virus (HCV) inhibitors. The compounds have an imidazole core that is disubstituted via amide links. Also described are a pharmaceutical composition incorporating the imidazole-based compound, a method of preparing these compounds, and a method for using the pharmaceutical composition in the treatment of HCV infection.
    Type: Grant
    Filed: August 6, 2020
    Date of Patent: November 3, 2020
    Assignee: King Abdulaziz University
    Inventors: Moustafa E. El-Araby, Abdelsattar Mansour Omar, Mahmoud Abdelkhalek El-Faky, Sameh Hamdy Abdelmageed Soror, Maan Talaat Khayat, Hani Zakariah Asfour, Faida Hassan Bamane
  • CDK2/4/6 inhibitors
    Patent number: 10800783
    Abstract: This invention relates to compounds of general Formula (I) and pharmaceutically acceptable salts thereof, in which R1, R2, R2A, R2B, R3, R4, R5A, R5B, R6, R7, R8, R9, p, q and r are as defined herein, to pharmaceutical compositions comprising such compounds and salts, and to methods of using such compounds, salts and compositions for the treatment of abnormal cell growth, including cancer.
    Type: Grant
    Filed: January 17, 2019
    Date of Patent: October 13, 2020
    Assignee: Pfizer Inc.
    Inventors: Douglas Carl Behenna, Ping Chen, Kevin Daniel Freeman-Cook, Robert Louis Hoffman, Mehran Jalaie, Asako Nagata, Sajiv Krishnan Nair, Sacha Ninkovic, Martha Alicia Ornelas, Cynthia Louise Palmer, Eugene Yuanjin Rui
  • TDO2 Inhibitors
    Patent number: 10800780
    Abstract: Presently provided are inhibitors of cellularly expressed TDO2 and pharmaceutical compositions thereof, useful for modulating an activity of tryptophan 2, 3 dioxygenase; treating immunosuppression; treating a medical conditions that benefit from the inhibition of tryptophan degradation; enhancing the effectiveness of an anti-cancer treatment comprising administering an anti-cancer agent; and treating tumor-specific immunosuppression associated with cancer.
    Type: Grant
    Filed: December 23, 2016
    Date of Patent: October 13, 2020
    Assignees: Genentech, Inc., NewLink Genetics Corporation
    Inventors: Xingyu Lin, Po-wai Yuen, Rohan Mendonca, Brendan Parr, Richard Pastor, Zhonghua Pei, Lewis Gazzard, Firoz Jaipuri, Sanjeev Kumar, Xiaokai Li, Roheeth Pavana, Hima Potturi, Venkata Velvadapu, Jesse Waldo, Zuhui Zhang, Guosheng Wu, Benjamin Douglas Sellers
  • Toll-like receptor 7 (TLR7) agonists having heteroatom-linked aromatic moieties, conjugates thereof, and methods and uses therefor
    Patent number: 10793569
    Abstract: Compounds having a structure according to formula (I) or (II) where R1, R2, R3, R4, Ar and X1 are as defined herein, are agonists for the Toll-like receptor 7 (TLR7) and can be used as adjuvants for stimulating the immune system. Some such compounds can be used in conjugates for targeted delivery to the organ or tissue of intended action.
    Type: Grant
    Filed: May 1, 2020
    Date of Patent: October 6, 2020
    Assignee: BRISTOL-MYERS SQUIBB COMPANY
    Inventors: Liqi He, Sanjeev Gangwar, Yam B. Poudel, Prasanna Sivaprakasam
  • Opioid antagonists and methods related thereto
    Patent number: 10787456
    Abstract: Disclosed is a composition and method for a therapeutic treatment that is able to combat certain conditions such as alcohol dependence, opioid abuse treatment, neurological disorders, neuropathic pain, and fibromyalgia. The novel gliotoxin analog compound acts by acting as an antagonist to one or more opioid receptors, which, when present leads to the inhibition of conditions, providing increased performance over known treatments. The disclosed compounds also shows the ability to cross the blood-brain-barrier in a highly efficient manner.
    Type: Grant
    Filed: October 30, 2018
    Date of Patent: September 29, 2020
    Assignee: TEXAS TECH UNIVERSITY SYSTEM
    Inventors: Nadezhda German, Mohammad Anwar Hossain
  • Bicyclic compounds as ATX inhibitors
    Patent number: 10787459
    Abstract: The invention provides novel compounds having the general formula (I) wherein R1, R2, R9, Y, W, m, n, p and q are as defined herein, compositions including the compounds and methods of using the compounds.
    Type: Grant
    Filed: April 10, 2019
    Date of Patent: September 29, 2020
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Patrick Di Giorgio, Jerome Hert, Daniel Hunziker, Patrizio Mattei, Markus Rudolph, Petra Schmitz
  • 2-(morpholin-4-yl)-1,7-naphthyridines
    Patent number: 10772893
    Abstract: The present invention relates to substituted 2-(morpholin-4-yl)-1,7-naphthyridine compounds of general formula (I) or (Ib), to methods of preparing said compounds, to intermediate compounds useful for preparing said compounds, to pharmaceutical compositions and combinations comprising said compounds and to the use of said compounds for manufacturing a pharmaceutical composition for the treatment or prophylaxis of a disease, in particular of a hyperproliferative disease as a sole agent or in combination with other active ingredients.
    Type: Grant
    Filed: May 8, 2018
    Date of Patent: September 15, 2020
    Assignee: BAYER PHARMA AKTIENGESELLSCHAFT
    Inventors: Lars Wortmann, Ulrich Lücking, Julien Lefranc, Hans Briem, Marcus Koppitz, Knut Eis, Franz Von Nussbaum, Benjamin Bader, Antje Margret Wengner, Gerhard Siemeister, Wilhelm Bone, Philip Lienau, Joanna Grudzinska-Goebel, Dieter Moosmayer, Uwe Eberspächer, Hans Schick
  • Bridged bicyclic compounds and their derivatives as neuroprotective agents and methods of use thereof
    Patent number: 10759735
    Abstract: Neuroprotective compounds for reducing neurological damage due to cellular stress in an individual are of Formula 1: or an enantiomer, diastereomer, racemic mixture or a pharmaceutically acceptable salt thereof, wherein: Ar=aryl; Y=aryl substituent (ortho, meta, or para) selected from the group consisting of: alkyl, alkyloxy, alkylamino, R5R6N, and halo; X?O, N, or S; R?H, alkyl, aryl, OH, alkyloxy, aryloxy, NH2, alkylamino, R5R6N, or arylamino; R1 and R2=alkylcarbonyl, arylcarbonyl, alkyl, or H, individually; R3=arylCH?CH, alkylCH?CH, alkyl; R4?H, alkyl, or aryl; and R5 and R6=alkyl, individually. Methods of reducing neurological damage due to cellular stress in an individual include administering to the individual during or after the cellular stress a neuroprotective compound of Formula I in a therapeutically effective amount to restore synaptic function during or after the cellular stress.
    Type: Grant
    Filed: January 11, 2019
    Date of Patent: September 1, 2020
    Assignee: Florida Atlantic University Board of Trustees
    Inventors: Salvatore D. Lepore, Kenneth Dawson-Scully, Elijah J. St. Germain, Samantha L. Maki, Wesley L. Bollinger, Nadia K. Sial
  • Syntheses of N-heterocyclic carbenes and intermediates therefor
    Patent number: 10759763
    Abstract: A method of preparing a 2,6 disubstituted anilines includes, reacting a 2-amino isophthalic acid diester with sufficient Grignard reagent R2CH2MgX to form the corresponding diol product, dehydrating the diol product to the corresponding dialkene; and hydrogenating the diol product to form the corresponding aniline. The 2,6 disubstituted anilines can be used to produce N-Heterocyclic Carbenes (NHCs). The NHCs can find application in various fields such as organic synthesis, catalysis and macromolecular chemistry. Palladium catalysts containing the NHCs are also described.
    Type: Grant
    Filed: December 22, 2017
    Date of Patent: September 1, 2020
    Assignee: UMICORE AG & CO. KG
    Inventors: Steven P. Nolan, Sebastien Meiries
  • Process for the preparation of DL-proline co-crystal of Dapagliflozin
    Patent number: 10759772
    Abstract: The present invention relates to a process For the preparation of Dapagliflozin DL-Proline co-crystal and its use in the preparation/purification of Dapagliflozin. The invention also provides a process for the preparation of Dapagliflozin (R,S)-1.2-propanediol monohydrate.
    Type: Grant
    Filed: April 28, 2017
    Date of Patent: September 1, 2020
    Assignee: Aurobindo Pharma Ltd
    Inventors: Senthilkumar Natrajan, Kishore Karumanchi, Vittal Tangirala, Sivakumaran Meenakshisunderam
  • Bone fracture repair by targeting of agents that promote bone healing
    Patent number: 10744203
    Abstract: Aspects of the present disclosure generally relate to compounds for targeting and healing bone fractures. Some of these compounds include a negatively charged oligopeptide comprising an acidic oligopeptide, a linker, which may be hydrolyzable or may be a substrate for the protease cathepsin K, and at least one molecule that promotes bone healing. In some compounds the molecule that promotes bone healing is an anabolic compound that inhibits GSK3?, in some compounds the molecule that promotes the healing of bone fracture is a pro-inflammatory agent such as PGE1. Other embodiments include methods of treating a bone fracture comprising administering a therapeutic amount of any one of the compounds disclosed herein.
    Type: Grant
    Filed: January 31, 2019
    Date of Patent: August 18, 2020
    Assignees: Purdue Research Foundation, University of Utah
    Inventors: Stewart Andrew Low, Philip S. Low, Christopher Galliford, Jindrich Kopecek, Jiyan Yang
  • Acyclic antivirals
    Patent number: 10745427
    Abstract: Disclosed herein are nucleotide analogs, methods of synthesizing nucleotide analogs and methods of treating diseases and/or conditions such as a HBV and/or HDV and/or HIV infection with one or more nucleotide analogs.
    Type: Grant
    Filed: March 9, 2017
    Date of Patent: August 18, 2020
    Assignee: Janssen BioPharma, Inc.
    Inventors: Leonid Beigelman, Guangyi Wang, Minghong Zhong
  • Triazole furan compounds as agonists of the APJ receptor
    Patent number: 10736883
    Abstract: Compounds of Formula (I) and Formula (II), pharmaceutically acceptable salt thereof, stereoisomers of any of the foregoing, or mixtures thereof are agonists of the APJ Receptor and have use in treating cardiovascular and other conditions. Compounds of Formula (I) and Formula (II) have the following structures: (I); (II). Intermediates (V) are also claimed.
    Type: Grant
    Filed: November 3, 2017
    Date of Patent: August 11, 2020
    Assignee: AMGEN INC.
    Inventors: Matthew Brown, Ning Chen, Xiaoqi Chen, Yinhong Chen, Alan C. Cheng, Richard V. Connors, Jeffrey Deignan, Paul John Dransfield, Xiaohui Du, Zice Fu, James S. Harvey, Julie Anne Heath, Lars V. Heumann, Jonathan Houze, Frank Kayser, Aarif Yusuf Khakoo, David j. Kopecky, Su-Jen Lai, Zhihua Ma, Julio C. Medina, Jeffrey T. Mihalic, Steven H. Olson, Vatee Pattaropong, Gayathri Swaminath, Xiaodong Wang, Malgorzata Wanska, Wen-Chen Yeh
  • Substituted heteropentadieno-pyrrolopyrimidine ribonucleosides for therapeutic use
    Patent number: 10730905
    Abstract: Substituted heteropentadieno-pyrrolopyrimidine ribonucleosides of general formula I, where R is selected from the group comprising furan-2-yl, furan-3-yl, benzofuran-2-yl, methylsulfanyl, methoxy, amino, dimethylamino, methyl or chloro, and pharmaceutically acceptable salt thereof, their optical isomers and mixtures of such optical isomers.
    Type: Grant
    Filed: July 31, 2017
    Date of Patent: August 4, 2020
    Assignees: USTAV ORGANICKE CHEMIE A BIOCHEMIE AV CR, V.V.I., UNIVERZITA PALACKEHO V OLOMOUCI
    Inventors: Michal Hocek, Anna Tokarenko, Sabina Smolen, Marian Hajduch, Petr Dzubak
  • Tubulysin analogs and methods for their preparation
    Patent number: 10723727
    Abstract: The present invention is directed to novel cytotoxic tubulysin analogs and derivatives, to antibody drug conjugates thereof, and to methods for using the same to treat medical conditions including cancer.
    Type: Grant
    Filed: January 27, 2017
    Date of Patent: July 28, 2020
    Assignee: Pfizer Inc.
    Inventors: Chakrapani Subramanyam, Lawrence N. Tumey, Longfei Xie, Carolyn Leverett, Beth C. Vetelino, Sai Chetan K. Sukuru, Sarah Hudson, Venkata Ramana Doppalapudi, Abhijit S. Bhat
  • Process for preparation of luliconazole
    Patent number: 10703744
    Abstract: A process for the preparation of luliconazole and salts thereof is disclosed.
    Type: Grant
    Filed: December 9, 2015
    Date of Patent: July 7, 2020
    Assignee: GLENMARK LIFE SCIENCES LIMITED
    Inventors: Shekhar Bhaksar Bhirud, Kumar Hari Bhushan, Sunil Sudhakar Zhope, Shailesh Govind Ghadigaonkar, Pardeep Singh, Shekhar Ashok Deshmukh, Prem Chand
  • Method for producing kakeromycin and derivatives thereof
    Patent number: 10703732
    Abstract: Provided is a production method of kakeromycin and a derivative thereof showing an antifungal activity and cytotoxicity and expected as a new antifungal agent or anticancer agent, by chemical synthesis. A production method of a compound represented by the formula (1): wherein R is an optionally substituted hydrocarbon group or an optionally substituted heterocyclic group; and n is 0 or 1, or a salt thereof, including a step of subjecting a compound represented by the formula (2): wherein R and n are as defined above, or a salt thereof, to an oxidation reaction.
    Type: Grant
    Filed: September 21, 2018
    Date of Patent: July 7, 2020
    Assignees: OP BIO FACTORY CO., LTD., SEED RESEARCH INSTITUTE CO., LTD.
    Inventors: Teruhiko Ishikawa, Morita Iwami
  • 5-bromo-indirubins
    Patent number: 10703718
    Abstract: Disclosed herein are compositions and methods for treating cancer, FLT3-AML, and CML.
    Type: Grant
    Filed: February 9, 2018
    Date of Patent: July 7, 2020
    Assignee: CITY OF HOPE
    Inventors: Sangkil Nam, David Horne, Jun Xie