Patents Examined by Laura L. Stockton
  • Small molecule agonists and antagonists of NR2F6 activity in humans
    Patent number: 11324719
    Abstract: The present technology is directed to modulators of nuclear receptor activity, specifically to the modulation of NR2F6 activity and NR2F6 utilizing compounds, and the immune modulation and modulation of cancer stem cell activity through administration of compounds described herein to humans.
    Type: Grant
    Filed: November 21, 2017
    Date of Patent: May 10, 2022
    Assignee: KCL Therapeutics, Inc.
    Inventors: Harry M. Lander, David R. Koos
  • Pharmaceutical compounds
    Patent number: 11319312
    Abstract: This invention relates to compounds that are agonists of the muscarinic M1 and/or M4 receptor and which are useful in the treatment of diseases mediated by the muscarinic M1 and M4 receptors. Also provided are pharmaceutical compositions containing the compounds and the therapeutic uses of the compounds. Compounds provided are of formula where X1; X2; X3; X4; R1 R2 and R4 are as defined herein.
    Type: Grant
    Filed: October 13, 2020
    Date of Patent: May 3, 2022
    Inventors: Giles Albert Brown, Barry John Teobald, Benjamin Gerald Tehan
  • Organophosphate derivatives
    Patent number: 11306111
    Abstract: Provided herein are organophosphates and pharmaceutical compositions comprising said compounds.
    Type: Grant
    Filed: July 30, 2018
    Date of Patent: April 19, 2022
    Assignee: JANUARY THERAPEUTICS, INC.
    Inventors: Raj Raheja, Robin M. Jackman
  • Heterocyclic naphthoquinones derivatives for use in the treatment of cancers including Cushing disease
    Patent number: 11306063
    Abstract: The present invention concerns heterocyclic naphthoquinones derivatives for use in the treatment of Cushing disease and other cancers, in particular via the inhibition of Ubiquitin Specific Proteases (USP) 8 and/or 2.
    Type: Grant
    Filed: August 7, 2017
    Date of Patent: April 19, 2022
    Assignees: Commissariat a l'Energie Atomique et aux Energies Alternatives, Universite d'Aix Marseille
    Inventors: Marie-Odile Fauvarque, Magda Mortier, Catherine Pillet, Carmen Aguilar, Emmanuelle Soleilhac, Caroline Barette, Vincent Remusat, Thierry Terme, Patrice Vanelle
  • 2-cyanopyrimidin-4-yl carbamate or urea derivative or salt thereof, and pharmaceutical composition including same
    Patent number: 11299478
    Abstract: Provided is a 2-cyanopyrimidin-4-yl carbamate or urea derivative or pharmaceutically acceptable salt thereof, a process for the preparation thereof, and a pharmaceutical composition comprising the same. The 2-cyanopyrimidin-4-yl carbamate or urea derivative or pharmaceutically acceptable salt thereof selectively inhibits cathepsin K and therefore can be usefully applied for preventing or treating osteoporosis.
    Type: Grant
    Filed: March 20, 2019
    Date of Patent: April 12, 2022
    Assignee: HANLIM PHARMACEUTICAL CO., LTD.
    Inventors: Kyung-Hee Kim, Jung-Wook Chin, Ji-Hoon Lee, Shin-Ae Kim, Kyung-Jin Jung, Jun-Woo Kim, Sang-Hyun Min, Ji-Hoon Yu, Ju-Suk Lee, Won-Seok Lee, Jae-Young Song, Eung-Seok Lee, Tae-Cheon Jeong, Jung-Ae Kim
  • Antagonists of the muscarinic acetylcholine receptor M4
    Patent number: 11299481
    Abstract: Disclosed herein are substituted hexahydro-1H-cyclopenta[c]pyrrole compounds, which may be useful as antagonists of the muscarinic acetylcholine receptor M4 (mAChR M4). Also disclosed herein are methods of making the compounds, pharmaceutical compositions comprising the compounds, and methods of treating disorders using the compounds and compositions.
    Type: Grant
    Filed: October 20, 2018
    Date of Patent: April 12, 2022
    Assignee: Vanderbilt University
    Inventors: Craig W. Lindsley, P. Jeffrey Conn, Darren W. Engers, Julie L. Engers, Kayla J. Temple, Aaron M. Bender, Logan A. Baker
  • 3,6-methano-1H-pyrrolo[3,2-b]pyridine and 3,6-methano-1H-pyrrolo[3,2-C]pyridine compounds and medicaments using same
    Patent number: 11292794
    Abstract: The present disclosure provides a compound that is useful for the treatment and prophylaxis of rabies. The present disclosure provides a compound represented by formula XXIF or formula XXIB: wherein R1, R2A, R2B, R3, and R4 are defined in the specification, a solvent, or a pharmaceutically acceptable salt thereof, use of such a compound, solvate, or pharmaceutically acceptable salt thereof for the treatment or prophylaxis of rabies and cancer, a pharmaceutical composition comprising such a compound, solvate, or pharmaceutically acceptable salt thereof, and a method for the treatment or prophylaxis of rabies and cancer using the same.
    Type: Grant
    Filed: February 14, 2020
    Date of Patent: April 5, 2022
    Assignee: Oita University Institute of Advanced Medicine, Inc.
    Inventors: Hiroyuki Kouji, Kentaro Yamada, Akira Katoh, Toshimasa Ishizaki, Shigeru Matsuoka, Akira Nishizono, Tadashi Mishina, Atsushi Yoshimori
  • 11,13-modified saxitoxins for the treatment of pain
    Patent number: 11279706
    Abstract: Provided herein are compounds, pharmaceutical compositions comprising the compounds, methods of preparing the compounds, and methods of using the compounds and compositions in treating conditions associated with voltage-gated sodium channel function where the compounds are 11,13-modified saxitoxins according to Formula (I): where R1, X1, and X2 are as described herein.
    Type: Grant
    Filed: March 29, 2018
    Date of Patent: March 22, 2022
    Assignees: SITEONE THERAPEUTICS, INC., THE BOARD OF TRUSTEES OF THE LELAND STANFORD JUNIOR UNIVERSITY
    Inventors: John Mulcahy, Hassan Pajouhesh, George Miljanich, Anton Delwig, Jacob Beckley, Grant Masaaki Shibuya, Justin Du Bois
  • Condensed heterocyclic derivates as BCL-2 inhibitors for the treatment of neoplastic diseases
    Patent number: 11279711
    Abstract: The disclosure includes compounds of Formula (A): wherein R1, R2, R3, R4, R5, R6, R7, R8, R9, R10, R11, and R12, j, k, m, n, Y, W, W1, W2, W3, V, L, Z1, Q1, Q2, Q3, and Q4, are defined herein. Also disclosed is a method for treating a neoplastic disease, an autoimmune disease, or a neorodegenerative disease with these compounds.
    Type: Grant
    Filed: February 20, 2020
    Date of Patent: March 22, 2022
    Assignee: Newave Pharmaceutical Inc.
    Inventors: Yi Chen, Yan Lou
  • Fused pyrimidine compounds as BRD4 and JAK2 dual inhibitors and methods for use thereof
    Patent number: 11279703
    Abstract: The present invention relates to fused pyrimidine compounds, particularly pyrrolopyrimidine and thienopyrimidine compounds and derivatives thereof, pharmaceutical compositions thereof, and methods of inhibiting BRD4 and/or JAK2, as well as methods of treating various diseases and conditions, such as cancer and leukemia, with such compounds. Bromodomain binding and JAK activity are included.
    Type: Grant
    Filed: December 1, 2017
    Date of Patent: March 22, 2022
    Assignee: APTOSE BIOSCIENCES INC.
    Inventors: Ram Shankar Upadhayaya, Raghava Kethiri, Sachin Madan, Santosh Kumar Kotturi Rajaiah
  • BET bromodomain protein degraders with cleavable linkers
    Patent number: 11267822
    Abstract: The present disclosure provides compounds represented by Formula (I): Formula (I) and the pharmaceutically acceptable salts and solvates thereof, wherein R1, R2a, R2b, R3a, R3b, R4, Y, ?, Ar, W, L, and B are as defined as set forth in the specification. The present disclosure also provides compounds of Formula (I)I for use to treat a condition or disorder responsive to inhibition and/or degradation of BET bromodomains such as cancer.
    Type: Grant
    Filed: September 12, 2018
    Date of Patent: March 8, 2022
    Assignee: THE REGENTS OF THE UNIVERSITY OF MICHIGAN
    Inventors: Shaomeng Wang, Weiguo Xiang, Fuming Xu, Longchuan Bai, Ester Fernandez-Salas, Donna McEachern
  • KV7 channel activators compositions and methods of use
    Patent number: 11261162
    Abstract: Provided herein are optionally substituted benzoimidazol-1,2-yl amides, pharmaceutical compositions comprising a therapeutically effective amount of such compounds and a pharmaceutically acceptable excipient, and methods of treating Kv7 associated diseases, such as, epilepsy, amyotrophic lateral sclerosis, various types of pain, hyperexcitability, a dyskinesia, dystonia, mania and tinnitus with such compounds and pharmaceutical compositions.
    Type: Grant
    Filed: October 22, 2020
    Date of Patent: March 1, 2022
    Assignee: KNOPP BIOSCIENCES, LLC
    Inventors: Michael E. Bozik, Scott S. Harried, Lynn Resnick, George T. Topalov, Justin K. Belardi, Charles A. Flentge, David A. Mareska, James S. Hale
  • Dianilinopyrimidine compound for inhibiting kinase activity
    Patent number: 11254696
    Abstract: Disclosed are a dianilino pyrimidine compound having an inhibitory effect on protein tyrosine kinase, pharmaceutically acceptable salts, crystal forms, prodrugs, metabolites, hydrates, solvates, stereoisomers or isotopic derivatives thereof, a pharmaceutical composition containing these compounds, as well as preparation and use of these compounds. The compound has a structure as represented by formula (I), and may be used for treating ALK-mediated cancer-related symptoms, such as non-small cell lung cancer, breast cancer, nerve tumors, esophagus cancer, soft tissue cancer, lymphoma, or leukemia.
    Type: Grant
    Filed: December 12, 2018
    Date of Patent: February 22, 2022
    Assignee: Shenzhen TargetRx, Inc.
    Inventors: Yihan Wang, Huanyin Li
  • Small molecule regulators of steroid receptor coactivators and methods of use thereof
    Patent number: 11253517
    Abstract: Small molecule regulators of steroid receptor coactivator (SRC) family proteins are provided, as well as methods for their use in treating or preventing SRC-related diseases. The SRC-related diseases can include cancer, metabolic disorders, human immunodeficiency virus, neurodegenerative disorders, and/or inflammatory diseases. Also provided are methods for regulating SRC family proteins in a cell.
    Type: Grant
    Filed: November 21, 2019
    Date of Patent: February 22, 2022
    Assignee: BAYLOR COLLEGE OF MEDICINE
    Inventors: Bert W. O'Malley, David Michael Lonard, Jin Wang, Jianming Xu, Jianwei Chen
  • Fused imidazo-piperidine JAK inhibitors
    Patent number: 11254669
    Abstract: The invention provides compounds of formula (I): where the variables are defined in the specification, or a pharmaceutically-acceptable salt thereof, that are useful as JAK kinase inhibitors. The invention also provides pharmaceutical compositions comprising such compounds, methods of using such compounds to treat respiratory diseases, and processes and intermediates useful for preparing such compounds.
    Type: Grant
    Filed: November 11, 2019
    Date of Patent: February 22, 2022
    Assignee: THERAVANCE BIOPHARMA R&D IP, LLC
    Inventors: Paul R. Fatheree, Gary E. L. Brandt, Cameron Smith, Steven D. E. Sullivan, Lori Jean Van Orden
  • Method for the preparation of thiocarbonates
    Patent number: 11247979
    Abstract: Process for the preparation of a compound with at least one five-membered cyclic monothiocarbonate group wherein a) a compound with at least one epoxy group is used as starting material b) the compound is reacted with phosgene or an alkyl chloroformate thus giving an adduct and c) the adduct is reacted with a compound comprising anionic sulfurthus obtaining the compound with at least one five-membered cyclic monothiocarbonate group.
    Type: Grant
    Filed: August 7, 2018
    Date of Patent: February 15, 2022
    Assignee: BASF SE
    Inventors: Peter Rudolf, Indre Thiel, Markus Jegelka, Jan-Dirk Arndt, Joaquim Henrique Teles
  • Spirocyclic ROR-gamma modulators
    Patent number: 11242350
    Abstract: Described herein are retinoic acid related-related orphan nuclear receptor (ROR) modulators and methods of utilizing ROR-gamma modulators in the treatment of diseases, disorders or conditions. Also described herein are pharmaceutical compositions containing such compounds.
    Type: Grant
    Filed: March 11, 2019
    Date of Patent: February 8, 2022
    Assignee: ESCALIER BIOSCIENCES B.V.
    Inventors: Raju Mohan, John Nuss, Jason Harris, Shendong Yuan
  • Method for producing benzimidazole derivative
    Patent number: 11242332
    Abstract: The present invention relates to a process to prepare a benzimidazole derivative useful as a medicament, an intermediate for preparing the medicament, and a process to prepare the intermediate.
    Type: Grant
    Filed: March 14, 2018
    Date of Patent: February 8, 2022
    Assignee: Sumitomo Dainippon Pharma Co., Ltd.
    Inventors: Shingo Mizushima, Shoukou Lee, Yoko Takahashi
  • Method for preparing aryl 2-tetrazol-1-yl keto with improved selectivity
    Patent number: 11236054
    Abstract: The present disclosure relates to a method for preparing aryl 2-tetrazol-2-yl ketone of the following Formula 1a with improved selectivity: wherein R1 and R2 are the same as defined herein.
    Type: Grant
    Filed: February 27, 2020
    Date of Patent: February 1, 2022
    Assignee: SK BIOPHARMACEUTICALS CO., LTD.
    Inventors: Kyuwoong Lee, Kyungmi Cha, Suyeon Yeom, Jiseon Woo
  • Compounds and methods for the targeted degradation of androgen receptor
    Patent number: 11236051
    Abstract: The present disclosure relates to bifunctional compounds, which find utility to degrade (and inhibit) Androgen Receptor. In particular, the present disclosure is directed to compounds, which contain on one end a cereblon ligand which binds to the E3 ubiquitin ligase and on the other end a moiety which binds Androgen Receptor, such that Androgen Receptor is placed in proximity to the ubiquitin ligase to effect degradation (and inhibition) of Androgen Receptor. The present disclosure exhibits a broad range of pharmacological activities associated with compounds according to the present disclosure, consistent with the degradation/inhibition of Androgen Receptor.
    Type: Grant
    Filed: July 24, 2020
    Date of Patent: February 1, 2022
    Assignee: Arvinas Operations, Inc.
    Inventors: Andrew P. Crew, Kurt Zimmermann, Hanqing Dong, Lawrence B. Snyder