Patents Examined by Douglas M Willis
  • Substituted pyrazolo[1,5-a]pyrimidines as inhibitors of interferon signaling
    Patent number: 11634423
    Abstract: The present invention provides a compound of Formula I: wherein R is or a pharmaceutically acceptable salt thereof, useful for treating psoriasis, systemic lupus erythematosus, or type 1 diabetes.
    Type: Grant
    Filed: February 5, 2021
    Date of Patent: April 25, 2023
    Assignee: Eli Lilly and Company
    Inventors: Thomas John Bleisch, Zhaogen Chen, Theodore Curtis Jessop
  • Substituted pyrazolo[1,5-a]pyrazines as negative allosteric modulators of group II metabotropic glutamate receptor
    Patent number: 11633395
    Abstract: Provided are a compound that is useful for the prevention of and/or as a treatment agent for a disease in which a group II mGlu receptor is involved; and a medical application of said compound. Provided is a compound represented by formula (I) or a pharmaceutically acceptable salt thereof.
    Type: Grant
    Filed: November 22, 2018
    Date of Patent: April 25, 2023
    Assignee: SUMITOMO PHARMA CO., LTD.
    Inventors: Yohei Ikuma, Kengo Tojo, Ryo Fukazawa, Shuji Masumoto
  • Process for the synthesis of linker-drug vc-seco-DUBA
    Patent number: 11633492
    Abstract: The compound of formula (II) is an advantageous intermediate for improving the process of synthesizing the linker-drug vc-seco-DUBA, as well as for the overall process for preparing an antibody-drug conjugate comprising the vc-seco-DUBA linker-drug. The methods of making the compound of formula (II) can include recovery of the compound as a solid, such as via crystallization, in high yields and purity.
    Type: Grant
    Filed: November 22, 2018
    Date of Patent: April 25, 2023
    Assignee: Byondis B.V.
    Inventors: Vladimir Janousek, Martin Kas
  • Substituted pyrrolo[3,4-d]imidazoles as JAK inhibitors
    Patent number: 11629148
    Abstract: The present disclosure relates to substituted pyrrollo[3,4-D]imidazoles as JAK inhibitor compounds and uses thereof. Specifically, the present disclosure discloses a compound represented by formula (I), optical isomer thereof, geometric isomer thereof, a tautomer thereof or a mixture of various isomers, or a pharmaceutically acceptable salt thereof, or a prodrug thereof, or a metabolite thereof. The present disclosure also relates to the application of the compounds in the treatment of JAK-related diseases or disorders.
    Type: Grant
    Filed: August 24, 2021
    Date of Patent: April 18, 2023
    Assignee: HENAN MEDINNO PHARMACEUTICAL TECHNOLOGY CO., LTD.
    Inventors: Liang Lu, Hai Huang, Longzheng Zhang, Saisai Zhao, Jixuan Zhang
  • Substituted [1,2,4]triazolo[4,3-a]pyrazines as modulators of sodium channel activity
    Patent number: 11629146
    Abstract: The present invention is directed to, in part, fused heteroaryl compounds and compositions useful for preventing and/or treating a disease or condition relating to aberrant function of a voltage-gated, sodium ion channel, for example, abnormal late/persistent sodium current. Methods of treating a disease or condition relating to aberrant function of a sodium ion channel including Dravet syndrome or epilepsy are also provided herein.
    Type: Grant
    Filed: November 28, 2017
    Date of Patent: April 18, 2023
    Assignee: PRAXIS PRECISION MEDICINES, INC.
    Inventors: Kiran Reddy, Gabriel Martinez Botella, Andrew Mark Griffin, Brian Edward Marron
  • Antibody-drug conjugates comprising substituted benzo[e]pyrrolo[1,2-?][1,4]diazepines
    Patent number: 11628223
    Abstract: A novel antibody-pyrrolodiazepine derivative and a novel antibody-pyrrolodiazepine derivative conjugate using the same, comprising substituted benzo[e]pyrrolo[1,2-a][1,4]diazepines represented by the [Formula 24], [Formula 25], [Formula 26], and/or [Formula 27].
    Type: Grant
    Filed: September 28, 2018
    Date of Patent: April 18, 2023
    Assignee: DAIICHI SANKYO COMPANY, LIMITED
    Inventors: Narihiro Toda, Yusuke Ota, Fuminao Doi, Masaki Meguro, Ichiro Hayakawa, Shinji Ashida, Takeshi Masuda, Takashi Nakada, Mitsuhiro Iwamoto, Naoya Harada, Tomoko Terauchi, Daisuke Okajima, Kensuke Nakamura, Hiroaki Uchida, Hirofumi Hamada
  • Substituted [1,2,4]triazolo[1,5-a]pyrimidines for stabilizing microtubules
    Patent number: 11623927
    Abstract: The present disclosure provides compounds of formula (I) or (II) or a pharmaceutically acceptable salt or stereoisomer thereof, wherein Rx-R8 are defined herein. Also provided are compositions comprising a compound described herein and a pharmaceutically effective excipient, methods of stabilizing microtubules in a patient comprising administering to the patient a microtubule-stabilizing amount of a compound described herein, methods of treating cancer in a patient comprising administering to the patient a therapeutically effective amount of a compound described herein, and methods of treating a neurodegenerative disease in a patient comprising administering to the patient a therapeutically effective amount of a compound described herein.
    Type: Grant
    Filed: February 28, 2019
    Date of Patent: April 11, 2023
    Assignees: The Trustees of the University of Pennsylvania, The Regents of the University of California
    Inventors: Kurt R. Brunden, Virginia M. Y. Lee, John Q. Trojanowski, Carlo Ballatore, Killian Oukoloff, Amos B. Smith, III
  • Aminopyrrolotriazines as kinase inhibitors
    Patent number: 11618753
    Abstract: The disclosure relates to compounds of formula I which are useful as kinase modulators including RIPK 1 modulation. The disclosure also provides methods of making and using the compounds for example in treatments related to necrosis or inflammation as well as other indications.
    Type: Grant
    Filed: January 24, 2019
    Date of Patent: April 4, 2023
    Assignee: Bristol-Myers Squibb Company
    Inventors: Scott Hunter Watterson, Murugaiah Andappan Murugaiah Subbaiah, Carolyn Diane Dzierba, Hua Gong, Jason M. Guernon, Junqing Guo, Amy C. Hart, Guanglin Luo, John E. Macor, William J. Pitts, Jianliang Shi, Brian Lee Venables, Carolyn A. Weigelt, Yong-Jin Wu, Zhizhen Barbara Zheng, Sing-Yuen Sit, Jie Chen
  • Substituted imidazo[1,5-a]pyrazines for modulation of IRE1
    Patent number: 11613544
    Abstract: Described herein, inter alia, are certain substituted imidazo[1,5-a]pyrazines of formula (I) and methods of using the same for modulating the activity of Ire1.
    Type: Grant
    Filed: September 24, 2020
    Date of Patent: March 28, 2023
    Assignees: The Regents of the University of California, University of Washington Through Its Center For Commercialization
    Inventors: Bradley J. Backes, Dustin J. Maly, Scott A. Oakes, Feroz R. Papa, Gayani Perera, Likun Wang
  • Substituted pyridines, pyridazines, pyrimidines, and 1,2,4-triazines as TYK2 inhibitors
    Patent number: 11613548
    Abstract: Described herein are compounds of Formula (XVII) that are TYK2 inhibitors, methods of making such compounds, pharmaceutical compositions and medicaments comprising such compounds, and methods of Using such compounds in the treatment of conditions, diseases, or disorders that would benefit from modulation of TYK2 activity.
    Type: Grant
    Filed: May 5, 2022
    Date of Patent: March 28, 2023
    Assignee: SUDO BIOSCIENCES LIMITED
    Inventors: Anjali Pandey, Gregory Dietsch, Bhaskar Chaudhuri, Seetharaman Manojveer, Mahesh Thakkar, Athisayamani Jeyaraj Duraiswamy, Sukesh Kalva
  • Substituted pyrrolo[2,3-d]pyrimidines as Bruton's Tyrosine Kinase inhibitors
    Patent number: 11613543
    Abstract: The invention relates to compounds of the formula (I) (I) or a pharmaceutically acceptable salt thereof, wherein the substituents are as defined in the specification; to intermediates in the preparation of the compounds, to pharmaceutical compositions comprising the compounds and to use of the compounds in the treatment of disease.
    Type: Grant
    Filed: March 22, 2019
    Date of Patent: March 28, 2023
    Assignee: NOVARTIS AG
    Inventors: Luca Arista, Christina Hebach, Gregory John Hollingworth, Philipp Holzer, Patricia Imbach-Weese, Julien Lorber, Rainer Machauer, Niko Schmiedeberg, Anna Vulpetti, Thomas Zoller
  • Substituted pyrimido[5,4-d]pyrimidines as HER2 inhibitors
    Patent number: 11608343
    Abstract: The present invention relates to new [1,3]diazino[5,4-d]pyrimidines and derivatives of Formula (I) wherein the groups R1, R2, R3 and R4 have the meanings given in the claims and specification, their use as inhibitors of HER2 and its mutants, pharmaceutical compositions which contain such compounds and their use as medicaments, especially as agents for treatment and/or prevention of oncological diseases.
    Type: Grant
    Filed: April 6, 2021
    Date of Patent: March 21, 2023
    Assignee: Boehringer Ingelheim International GmbH
    Inventors: Birgit Wilding, Dietrich Boese, Harald Engelhardt, Julian Fuchs, Ralph Neumueller, Mark Petronczki, Dirk Scharn, Matthias Treu
  • Substituted tetrahydropyrazolo[3,4-d]pyrimidines and tetrahydropyrazolo[4,3-d]pyrimidines as C5A receptor modulators
    Patent number: 11608341
    Abstract: The present invention relates to derivatives of formula (I) wherein Ring A, X, Y, Z, RA, R1, R2, R3 and R4 are as described in the description, to their preparation, to pharmaceutically acceptable salts thereof, and to their use as pharmaceuticals, to pharmaceutical compositions containing one or more compounds of formula (I), and especially to their use as C5a receptor modulators.
    Type: Grant
    Filed: January 9, 2019
    Date of Patent: March 21, 2023
    Assignee: Idorsia Pharmaceuticals Ltd.
    Inventors: Sylvie Froidevaux, Francis Hubler, Mark Murphy, Dorte Renneberg, Simon Stamm
  • Substituted heteroaryls as thermally assisted delayed fluorescent materials
    Patent number: 11603370
    Abstract: Thermally assisted delayed fluorescent materials with triad-type materials for use in full color displays and lighting applications with the following generic structures are provided:
    Type: Grant
    Filed: October 9, 2020
    Date of Patent: March 14, 2023
    Assignee: Arizona Board of Regents on Behalf of Arizona State University
    Inventor: Jian Li
  • Process for preparing highly pure temozolomide
    Patent number: 11597731
    Abstract: The present invention provides a new process for preparation of imidazo-tetrazine class of chemical entity useful as anticancer agent. The present invention provides a commercially and economically viable process for preparation of Temozolomide of formula (VI). Present invention also relates to an intermediate compound of formula (III) and its preparation useful in the process for preparing Temozolomide.
    Type: Grant
    Filed: July 17, 2021
    Date of Patent: March 7, 2023
    Assignee: SHIVALIK RASAYAN LIMITED
    Inventors: Akshay Kant Chaturvedi, Bijan Kumar Panda, Amit Kumar, Deepali Chaturvedi
  • Substituted imidazoles as PLXDC2 ligands
    Patent number: 11597717
    Abstract: Provided are compounds of Formula Y-Z: The compounds target plexin domain containing 2 (PLXDC2). The compounds can be used to treat conditions such as inflammatory or immune-mediated diseases, diabetes, infectious diseases, and cancers. The compounds can be used to treat such specific conditions as systemic lupus erythematosus, rheumatoid arthritis, multiple sclerosis, autoimmune encephalitis, diabetic nephropathy, diabetic retinopathy, psoriasis, and inflammatory bowel disease, among other conditions.
    Type: Grant
    Filed: September 29, 2021
    Date of Patent: March 7, 2023
    Assignee: Landos Biopharma, Inc.
    Inventors: Josep Bassaganya-Riera, Andrew Leber, Raquel Hontecillas, Nuria Tubau-Juni
  • Substituted pyrrolizines for the treatment of hepatitis B
    Patent number: 11591334
    Abstract: The present invention relates to a bicyclic nucleocapsid inhibitor and the use of the same as a drug in the treatment of hepatitis B. In particular, disclosed is a compound having a structure shown by the following formula (A1): or a stereoisomer or a tautomer thereof, or a pharmaceutically acceptable salt, a hydrate, or a solvate thereof, that can be used as an HBV inhibitor, wherein the definition of each group is as described in detail in the description. The present invention also relates to a pharmaceutical composition comprising the compound and the use of the same in the treatment of hepatitis B.
    Type: Grant
    Filed: May 4, 2018
    Date of Patent: February 28, 2023
    Assignee: SHANGHAI LONGWOOD BIOPHARMACEUTICALS CO., LTD.
    Inventors: Zhe Wang, Guoqin Fan, Cenbin Lu, Sai Yang, Xiaoguang Wang
  • Substituted [1,2,4]triazolo[4,3-a]pyrazines as modulators of mGlu5 receptors
    Patent number: 11591337
    Abstract: Disclosed are triazole, imidazole and pyrrole condensed piperazine derivatives and their use as allosteric modulators of mGlus receptor activity, pharmaceutical compositions comprising such compounds, and methods of treatment therewith. Compounds of the invention can be used for the treatment and/or prevention of neurological and psychiatric disorders associated with glutamate dysfunction such as schizophrenia or cognitive decline, dementia or cognitive impairment, or other pathologies that can be related either directly or indirectly to glutamate dysfunction, i.e., disorders treatable by positive allosteric modulation (PAM) or by negative allosteric modulation (NAM) of mGluR5.
    Type: Grant
    Filed: January 17, 2019
    Date of Patent: February 28, 2023
    Assignee: Recordati Industria Chimica e Farmaceutica S.p.A.
    Inventors: Davide Graziani, Carlo Riva, Sergio Menegon, Valerio Tazzari
  • Solid forms of (R)-N-(2-(5-fluoropyridin-3-yl)-8-isopropylpyrazolo[ 1,5-a][1,3,5]triazin-4-yl)-2,3,4,9-tetrahydro-1H-carbazol-3-amine maleate as aryl hydrocarbon receptor (AHR) inhibitors
    Patent number: 11591339
    Abstract: The present invention provides solid forms of (R)—N-(2-(5-fluoropyridin-3-yl)-8-isopropylpyrazolo[1,5-a][1,3,5]triazin-4-yl)-2,3,4,9-tetrahydro-1H-carbazol-3-amine maleate (Compound 2) represented by the formula:
    Type: Grant
    Filed: November 25, 2020
    Date of Patent: February 28, 2023
    Assignee: IKENA ONCOLOGY, INC.
    Inventors: Alfredo C. Castro, James Martin Nolan, III, Sarah Jean Bethune, Corinne Marie Folberth
  • Substituted pyrrolo[2,3-d]pyrimidines as janus kinase inhibitors
    Patent number: 11591333
    Abstract: The present invention provides a method for preparing a pyrrolopyrimidine compound and application thereof. Specifically, the present invention provides a compound represented by formula I or pharmaceutically-acceptable salts thereof, a pharmaceutical composition containing the compound or its salts, and a method for preparing the pharmaceutical composition and an application of the pharmaceutical composition as an immunosuppressive drug.
    Type: Grant
    Filed: February 22, 2017
    Date of Patent: February 28, 2023
    Assignees: CINAKATE PHARM TECH (SHANGHAI) CO., LTD., CINKATE PHARMACEUTICAL INTERMEDIATES CO., LTD.
    Inventors: Na Liu, Lixia Bao, Zhepeng Wei, Yufeng Zhou, Bin Rong, Lihui Zhao, Fei Xiao