Patents Examined by Laura L. Stockton
  • Patent number: 11358959
    Abstract: Compounds having activity as inhibitors of G12C mutant KRAS protein are provided. The compounds have the following structure (I) or a pharmaceutically acceptable salt, stereoisomer or prodrug thereof, wherein B, Z, Ra, Rb, Rc, R1, L, L1 and E are as defined herein. Methods associated with preparation and use of such compounds, pharmaceutical compositions comprising such compounds and methods to modulate the activity of G12C mutant KRAS protein for treatment of disorders, such as cancer, are also provided.
    Type: Grant
    Filed: January 25, 2018
    Date of Patent: June 14, 2022
    Inventors: Liansheng Li, Jun Feng, Yuan Liu, Pingda Ren, Yi Liu
  • Patent number: 11358947
    Abstract: Provided herein are inhibitors of transmembrane protein 16A (TMEM 16A), a Ca2+-activated CI? channel expressed widely in mammalian epithelia, as well as in vascular smooth muscle and some tumors and electrically excitable cells. TMEM16A inhibitors have potential utility for treatment or management of disorders of epithelial fluid and mucus secretion, hypertension, some cancers, pain, and other diseases.
    Type: Grant
    Filed: April 17, 2018
    Date of Patent: June 14, 2022
    Assignees: The Regents of the University of California
    Inventors: Marc O. Anderson, Alan S. Verkman, Puay Wah Phuan
  • Patent number: 11358977
    Abstract: Compounds, and pharmaceutically acceptable salts thereof, useful as inhibitors of sodium channels are provided. The compounds have the formula (I) wherein R is H or CH2OPO(OH)2. Also provided are pharmaceutical compositions comprising the compounds or pharmaceutically acceptable salts and methods of using the compounds, pharmaceutically acceptable salts, and pharmaceutical compositions in the treatment of various disorders, including pain.
    Type: Grant
    Filed: May 16, 2018
    Date of Patent: June 14, 2022
    Assignee: Vertex Pharmaceuticals Incorporated
    Inventors: Licong Jiang, Sara Sabina Hadida Ruah
  • Patent number: 11358960
    Abstract: This application features pyrazol-3-one compounds that activate pro-apoptotic BAX. Also featured are methods of using such compounds, e.g., for the treatment or prevention of diseases, disorders, and conditions associated with deregulated apoptosis of cells (e.g., insufficient apoptosis of diseased or damaged cells or essentially the absence of apoptosis of diseased or damaged cells).
    Type: Grant
    Filed: October 6, 2020
    Date of Patent: June 14, 2022
    Assignee: Dana-Farber Cancer Institute, Inc.
    Inventors: Loren D. Walensky, Evripidis Gavathiotis
  • Patent number: 11352382
    Abstract: The present invention relates to mito-lonidamine compounds, compositions and methods of use in the treatment of cancer.
    Type: Grant
    Filed: January 3, 2019
    Date of Patent: June 7, 2022
    Assignees: The Medical College of Wisconsin, Inc., Aix-Marseille Universite
    Inventors: Balaraman Kalyanaraman, Micael J. Hardy, Olivier Ouari
  • Patent number: 11345696
    Abstract: The present invention provides compounds useful for treating or preventing an IL-1R-mediated disease or disorder. In certain embodiments, the disease or disorder comprises scleroderma.
    Type: Grant
    Filed: August 12, 2019
    Date of Patent: May 31, 2022
    Assignee: Drexel University
    Inventors: Sandhya Kortagere, Carol M. Artlett
  • Patent number: 11339166
    Abstract: The present invention discloses compounds according to Formula I: wherein R1, R2, R3a, R3b, X, Y1, Y2, Y3, and Z are as defined herein. The present invention relates to compounds, methods for their production, pharmaceutical compositions comprising the same, and methods of treatment using the same, for the prophylaxis and/or treatment of inflammatory diseases, autoinflammatory diseases, autoimmune diseases, proliferative diseases, fibrotic diseases, transplantation rejection, diseases involving impairment of cartilage turnover, congenital cartilage malformation, diseases involving impairment of bone turnover, diseases associated with hypersecretion of TNF?, interferons, IL-6, IL-12 and/or IL-23, respiratory diseases, endocrine and/or metabolic diseases, cardiovascular diseases, dermatological diseases, and/or abnormal angiogenesis associated diseases by administering the compound of the invention.
    Type: Grant
    Filed: November 26, 2018
    Date of Patent: May 24, 2022
    Assignee: GALAPAGOS NV
    Inventors: Luke Jonathan Alvey, Denis Maurice Annoot, Florence Marie-Emilie Bonnaterre, Denis Bucher, Béranger Duthion, Hélène Marie Jary, Christophe Peixoto, Taoues Temal-Laib, Amynata Tirera, Nicolas Desroy
  • Patent number: 11337956
    Abstract: Compounds which directly inhibit IRE-1? activity in vitro, prodrugs, and pharmaceutically acceptable salts thereof. Such compounds and prodrugs are useful for treating diseases associated with the unfolded protein response or with regulated IRE1-dependent decay (RIDD) and can be used as single agents or in combination therapies.
    Type: Grant
    Filed: June 3, 2019
    Date of Patent: May 24, 2022
    Assignee: Fosun Orinove Pharmatech, Inc.
    Inventors: Qingping Zeng, Andras Toro, John Bruce Patterson, Warren Stanfield Wade, Zoltan Zubovics, Yun Yang, Zhipeng Wu
  • Patent number: 11332463
    Abstract: The present disclosure relates to compounds of formula I that are useful as modulators of 7 nAChR, compositions comprising such compounds, and the use of such compounds for preventing, treating, or ameliorating disease, particularly disorders of the central nervous system such as cognitive impairments in Alzheimer's disease, Parkinson's disease, and schizophrenia, as well as for L-DOPA induced-dyskinesia and inflammation (I).
    Type: Grant
    Filed: April 29, 2019
    Date of Patent: May 17, 2022
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Brendan M. Crowley, Brian T. Campbell, Harry R. Chobanian, James I. Fells, Deodial G. Guiadeen, Thomas J. Greshock, Kenneth J. Leavitt, Vanessa L. Rada, Ian M. Bell
  • 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
  • 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
  • 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
    Inventors: Raj Raheja, Robin M. Jackman
  • 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
  • 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
    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
  • 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
  • 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
  • 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
    Inventors: Ram Shankar Upadhayaya, Raghava Kethiri, Sachin Madan, Santosh Kumar Kotturi Rajaiah
  • 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
  • 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
    Inventors: John Mulcahy, Hassan Pajouhesh, George Miljanich, Anton Delwig, Jacob Beckley, Grant Masaaki Shibuya, Justin Du Bois
  • 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
    Inventors: Shaomeng Wang, Weiguo Xiang, Fuming Xu, Longchuan Bai, Ester Fernandez-Salas, Donna McEachern