Patents Examined by Douglas M Willis
  • Substituted pyrrolo[2,3-d]pyrimidines as EGFR inhibitors
    Patent number: 11786534
    Abstract: The present invention provides a novel compound inhibiting EGFR or a salt of the compound. According to one embodiment of the present invention, provided is a compound represented by general formula (I) or a pharmaceutically acceptable salt thereof.
    Type: Grant
    Filed: February 14, 2020
    Date of Patent: October 17, 2023
    Assignee: TAIHO PHARMACEUTICAL CO., LTD.
    Inventors: Fuyuki Yamamoto, Takashi Mizutani, Hidefumi Kasuga, Hirokazu Fuchida, Shoki Hara, Yu Kobayakawa, Yoshio Ogino
  • Substituted pyrazolo[4,3-d]pyrimidines and imidazo[5,1 -f][1,2,4]triazines as androgen receptor and phosphodiesterase dual inhibitors
    Patent number: 11787812
    Abstract: The present disclosure provides androgen receptor (AR) and phosphodiesterase 5 (PDE-5) inhibitor compounds of the formula (I): and compositions including said compounds. The compounds can provide dual functionality for inhibiting AR and inhibiting PDE-5. The present disclosure also provides methods of using said compounds and compositions for inhibiting AR and PDE-5 in a biological system or biological sample. Also provided are methods of preparing said compounds and compositions, and synthetic precursors of said compounds.
    Type: Grant
    Filed: December 10, 2021
    Date of Patent: October 17, 2023
    Assignee: ILDONG PHARMACEUTICAL CO., LTD.
    Inventors: Yoonsuk Lee, Kyung Sun Kim, Jeong-Ah Kim, Anna Moon, Dongkeun Song, Juyoung Jung, Jun-Su Ban, Soo-Jin Lee
  • Methods for treating Crohn's disease using 3-((1R,3s,5S)-3-((7-((5-methyl-1H-pyrazol-3-yl)amino)-1,6-naphthyridin-5-yl)amino)-8-azabicyclo[3.2.1]octan-8-yl)propanenitrile
    Patent number: 11780852
    Abstract: Disclosed are methods for treating Crohn's disease using a compound of the formula: or a pharmaceutically-acceptable salt thereof.
    Type: Grant
    Filed: February 10, 2021
    Date of Patent: October 10, 2023
    Assignee: Theravance Biopharma R&D IP, LLC
    Inventors: Ryan Hudson, Jennifer Kozak, Dante D. Podesto, Xiaojun Huang, Venkat R. Thalladi
  • Substituted N-pyrimidin-4-yl-3-aminopyrrolo[3,4-C]pyrazoles as protein kinase C inhibitors
    Patent number: 11780853
    Abstract: The present invention relates to protein kinase C beta II inhibiting compounds of Formula (A): wherein A, B, R1, R2, R3, R4, R5, R6, R7, R8, R9, and R10 are as defined herein. The invention further relates to pharmaceutical compositions comprising the compounds of Formula (A), or pharmaceutically acceptable salts thereof, and methods for treating a disease or disorder selected from the group consisting of Alzheimer's disease, cancer, a cardiovascular disease, a central nervous system disorder, depression, a dermatological disease, diabetes mellitus, a complication arising from diabetes mellitus, a disease in which the liver is a target organ inflammation, an inflammatory disorder, ischemia, and a viral disease.
    Type: Grant
    Filed: December 1, 2021
    Date of Patent: October 10, 2023
    Assignee: PFIZER INC.
    Inventors: Hui Li, Seiji Nukui, Stephanie Anne Scales, Min Teng, Chunfeng Yin
  • Process for preparing substituted imidazo[1,2-?]pyrazines
    Patent number: 11781168
    Abstract: Described are processes for preparing substituted imidazo[1,2-a]pyrazine compounds of formula (I): by reacting a compound of formula (xi): with carbonyldiimidazole to form the compound of formula (I).
    Type: Grant
    Filed: April 26, 2021
    Date of Patent: October 10, 2023
    Assignee: PROMEGA CORPORATION
    Inventors: Anton Shakhmin, Thomas Kirkland, Joel Walker, Thomas Machleidt, Mary Hall, Keith V. Wood
  • Crystalline forms of 4-(tert-butoxyamino)-6-(6-(trifluoromethyl)pyridin-2-yl)-N-(2-(trifluoromethyl)pyridin-4-yl)-1,3,5-triazin-2-amine
    Patent number: 11773079
    Abstract: The invention discloses a crystal of 4-(tert-butoxyamino)-6-(6-(trifluoromethyl)pyridin-2-yl)-N-(2-(trifluoromethyl)pyridin-4-yl)-1,3,5-triazin-2-amine compound, a mesylate salt and crystal thereof, a preparation method thereof, a composition containing thereof, and a use thereof for inhibiting activity of mutant IDH2 and treating cancer.
    Type: Grant
    Filed: April 27, 2021
    Date of Patent: October 3, 2023
    Assignees: Chia Tai Tianqing Pharmaceutical Group Co, Ltd., Lianyungang Runzhong Pharmaceutical Co., Ltd., Centaurus Biopharma Co., Ltd.
    Inventors: Ticong Huang, Huifeng Xiao, Rui Zhao, Fei Liu, Wei Wei, Hongjiang Xu, Xiaojin Wang, Jingli Wu
  • Substituted diazaspiroalkanes as androgen receptor modulators
    Patent number: 11771687
    Abstract: Provided herein are hydantoin compounds useful for the prevention or treatment of hyperproliferative diseases or disorders.
    Type: Grant
    Filed: November 9, 2020
    Date of Patent: October 3, 2023
    Assignee: The Regents of the University of California
    Inventors: Michael E. Jung, Charles L. Sawyers, Samedy Ouk, Chris Tran, John Wongvipat
  • Substituted [1,2,4]triazolo[4,3-a]pyrazines as ion channel modulators
    Patent number: 11767325
    Abstract: The present invention is directed to, in part, fused heteroaryl compounds of Formula (II-II): and compositions thereof, 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 neurological disorders (e.g., Dravet syndrome, epilepsy), pain, and neuromuscular disorders are also provided herein.
    Type: Grant
    Filed: November 25, 2020
    Date of Patent: September 26, 2023
    Assignee: PRAXIS PRECISION MEDICINES, INC.
    Inventors: Kiran Reddy, Gabriel Martinez Botella, Andrew Mark Griffin, Brian Edward Marron, Carlos Loya
  • Substituted benzimidazoles as inhibitors of transforming growth factor-? kinase
    Patent number: 11767298
    Abstract: The present invention provides inhibitors of TAK1 having formula (I) and methods of using such compounds to treat various diseases.
    Type: Grant
    Filed: February 22, 2021
    Date of Patent: September 26, 2023
    Assignee: Duke University
    Inventors: Emily Derbyshire, Timothy A. J. Haystead, Philip F. Hughes
  • Process for preparing substituted indolines
    Patent number: 11760759
    Abstract: The invention provides novel methods for preparing substituted indoline compounds and their synthetic precursors.
    Type: Grant
    Filed: February 26, 2021
    Date of Patent: September 19, 2023
    Assignee: IMMUNOGEN, INC.
    Inventors: Baudouin Gérard, Richard A. Silva, Michael Louis Miller, Manami Shizuka
  • Substituted pyrazolo[1,5-a]pyrimidines as TYK2 pseudokinase ligands
    Patent number: 11753411
    Abstract: Described herein are TYK2 pseudokinase ligands of Formula (I?), methods of utilizing these TYK2 pseudokinase ligands in the treatment of diseases, disorders or conditions, and pharmaceutical compositions containing such compounds: wherein X, Y, L1, R1, R2, R3, R4, R5, R6, and R8 are defined in the specification.
    Type: Grant
    Filed: November 5, 2020
    Date of Patent: September 12, 2023
    Assignee: VENTYX BIOSCIENCES, INC.
    Inventors: Raju Mohan, John Nuss, Jason Harris, Shendong Yuan
  • 4-((6bR,10aS)-3-methyl-2,3,6b,9,10,10a-hexahydro-1H-pyrido[3?,4?:4,5]pyrrolo[1,2,3-de]quinoxalin-8(7H)-yl)-1-(4-((6bR,10aS)-3-methyl-2,3,6b,9,10,10a-hexahydro-1H-pyrido[3?4?:4,5]pyrrolo[1,2,3-de]quinoxalin-8(7H)-yl)phenyl)butan-1-one for treating conditions of the central nervous system and cardiac disorders
    Patent number: 11753419
    Abstract: The invention relates to a particular substituted heterocycle fused gamma carboline, the compound of Formula I, and new methods and uses pertaining thereto, and pharmaceutical compositions thereof, such as methods of use in the treatment of diseases involving the 5-HT receptor, the serotonin transporter (SERT), and/or pathways involving dopamine D2 receptor signaling, sodium channel activity, and/or norepinephrine transporter activity.
    Type: Grant
    Filed: December 10, 2020
    Date of Patent: September 12, 2023
    Assignee: INTRA-CELLULAR THERAPIES, INC.
    Inventors: Peng Li, Robert E Davis, Kimberly Vanover
  • Substituted pyrrolo[2,1-f][1,2,4]triazine compounds as JAK2 V617F inhibitors
    Patent number: 11753413
    Abstract: The present application provides pyrrolotriazine compounds that modulate the activity of the V617F variant of JAK2, which are useful in the treatment of various diseases, including cancer.
    Type: Grant
    Filed: June 17, 2021
    Date of Patent: September 12, 2023
    Assignee: Incyte Corporation
    Inventors: Zhiyong Yu, Liangxing Wu, Wenqing Yao
  • Substituted pyrazlo[3,4-c]pyridines as selective BTK kinase inhibitors
    Patent number: 11739090
    Abstract: Disclosed are a class of BTK kinase inhibitor compounds with a high activity and a high selectivity and the use thereof in the preparation of a drug for treating BTK target-related diseases. Specifically, disclosed are a compound shown as formula (I), and an isomer and a pharmaceutically acceptable salt thereof.
    Type: Grant
    Filed: September 25, 2020
    Date of Patent: August 29, 2023
    Assignee: JUMBO DRUG BANK CO., LTD.
    Inventors: Chunli Shen, XiaWei Wei, Chengde Wu, Guoping Hu, Ning Jiang, Wei Zheng, Jian Li, Shuhui Chen
  • Substituted pyrazolopyrazines, imidazopyrazines and [1,2,4]triazolopyrazines as allosteric SHP2 inhibitors
    Patent number: 11739093
    Abstract: The present disclosure is directed to compounds of Formula IV: as inhibitors of SHP2 and their use in the treatment of diseases associated with SHP2. Also disclosed are pharmaceutical compositions comprising the same.
    Type: Grant
    Filed: July 22, 2019
    Date of Patent: August 29, 2023
    Assignee: REVOLUTION MEDICINES, INC.
    Inventors: Brian R. Blank, Jennifer Pitzen, Gang Wang, Walter S. Won, Christos Tzitzilonis, Jie Jack Li, Elena S. Koltun, Naing Aay, Andreas Buckl, Kevin Mellem, Christopher Semko, Ash Jogalekar, Gert Kiss, Adrian Gill
  • Substituted benzo[f][1,2,4]triazolo[4,3-a][1,4]diazepines as GABA A GAMMA1 positive allosteric modulators
    Patent number: 11739095
    Abstract: Compounds having the general formula (I) wherein R1, R2, R3, R4, R5 and X are as described herein, compositions including the compounds and methods of using the compounds.
    Type: Grant
    Filed: March 30, 2021
    Date of Patent: August 29, 2023
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Giuseppe Cecere, Luca Gobbi, Maria-Clemencia Hernandez, Frédéric Knoflach, Andreas Koblet, Eoin Cornelius O'Connor, Andres Miguel Olivares Morales, Michael Reutlinger, Valerie Runtz-Schmitt, Jaclyn Ivy Wamsteeker Cusulin, Nicolas Zorn
  • Substituted benzodiazoliums as ENaC inhibitors
    Patent number: 11739094
    Abstract: Compounds of general formula (I) wherein R1, R2, R3, R4, R5 and X are as defined herein are inhibitors of the epithelial sodium channel (ENaC) and are useful for the treatment or prevention respiratory diseases and conditions, skin conditions and ocular conditions.
    Type: Grant
    Filed: November 24, 2020
    Date of Patent: August 29, 2023
    Assignee: ENTERPRISE THERAPEUTICS LIMITED
    Inventors: Clive McCarthy, Jonathan David Hargrave, Duncan Alexander Hay, Thomas Beauregard Schofield, Naomi Went
  • N-acyl-(3-substituted)-(8-substituted)-5,6-dihydro-[1,2,4]triazolo[4,3-a]pyrazines as selective NK-3 receptor antagonists
    Patent number: 11731974
    Abstract: A method for treating and/or preventing polycystic ovary syndrome (PCOS) including the administration, to a patient in need thereof, of a pharmaceutically effective amount of a compound of Formula I or a pharmaceutically acceptable solvate thereof.
    Type: Grant
    Filed: October 8, 2020
    Date of Patent: August 22, 2023
    Assignee: Ogeda SA
    Inventors: Hamid R. Hoveyda, Guillaume Dutheuil, Graeme Fraser
  • Substituted pyrazolo[3,4-d]pyrimidines as mTOR inhibitors
    Patent number: 11731973
    Abstract: The invention relates to novel mTOR inhibitor compounds having the formula (I) or a pharmaceutically acceptable salt thereof, compositions comprising the mTOR inhibitor compounds, methods for producing the same, and the use thereof.
    Type: Grant
    Filed: June 19, 2020
    Date of Patent: August 22, 2023
    Assignee: GALDERMA RESEARCH & DEVELOPMENT
    Inventors: Laurence Clary, Jean-François Fournier, Gilles Ouvry, Yushma Bhurruth-Alcor, Etienne Thoreau, Loïc Tomas
  • Substituted 1,2,4-triazoles as intermediates in the synthesis of TYK2 inhibitors
    Patent number: 11731956
    Abstract: Described herein are compounds, for example, 1,2,4-triazole-substituted N-heteroaryl amines, that are useful in treating a TYK2-mediated disorder. In some embodiments, the TY-K2-mediated disorder is an autoimmune disorder, an inflammatory disorder, a proliferative disorder, an endocrine disorder, a neurological disorder, or a disorder associated with transplantation.
    Type: Grant
    Filed: August 19, 2022
    Date of Patent: August 22, 2023
    Assignee: Alumis Inc.
    Inventors: Bohan Jin, Qing Dong, Gene Hung, Stephen W. Kaldor