Patents Examined by Douglas M Willis
  • Patent number: 11453672
    Abstract: Provided are pharmaceutical compositions comprising substituted pyrazolo[1,5-a]pyrimidine compounds and the use thereof. The compositions may comprise the substituted pyrazolo[1,5-a]pyrimidine compound or a pharmaceutically acceptable salt, prodrug, hydrate or solvate, polymorph, stereoisomer or isotopic variant thereof, and can be used for treating diseases treatable with Trk kinase inhibitors.
    Type: Grant
    Filed: December 18, 2018
    Date of Patent: September 27, 2022
    Assignee: SHENZHEN TARGETRX, INC.
    Inventors: Yihan Wang, Jiuyang Zhao
  • Patent number: 11453673
    Abstract: The present invention provides a compound of Formula I: wherein R1 is methyl, ethyl or cyclopropyl; R2 is hydrogen, methyl, or ethyl; R3 is methyl or AA; and R4 is C2-C4 alkyl, BB; or a pharmaceutically acceptable salt thereof; for use as a PDE1 inhibitor.
    Type: Grant
    Filed: January 13, 2019
    Date of Patent: September 27, 2022
    Assignee: ELI LILLY AND COMPANY
    Inventors: Nicholas Paul Camp, Chafiq Hamdouchi, Jayana Pankaj Lineswala, John Richard Morphy, Qing Shi
  • Patent number: 11453671
    Abstract: Compounds of formula (I) wherein R1, R2, R3, R4, R5 and R6 are as defined herein, and salts thereof that are useful as JAK kinse inhibitors are described herein. Also provided are pharmaceutical compositions that include such a JAK inhibitor and a pharmaceutically acceptable carrier, adjuvant or vehicle, and methods of treating or lessening the severity of a disease or condition responsive to the inhibition of a Janus kinase activity in a patient.
    Type: Grant
    Filed: June 16, 2020
    Date of Patent: September 27, 2022
    Assignee: Genentech, Inc.
    Inventors: Mark Edward Zak, Naomi S. Rajapaksa, Yun-Xing Cheng, Jessica Grandner, Daniel G. M. Shore, Marian C. Bryan
  • Patent number: 11447495
    Abstract: Substituted benzo[f]imidazo[1,5-?][1,4]diazepines of formula (I?) target alpha-4 and alpha-5 GABAA receptors for use in the treatment of airway hyperresponsiveness and inflammation in asthma. Compounds selectively partition to the peripheral compartment and have reduced CNS effects.
    Type: Grant
    Filed: August 16, 2017
    Date of Patent: September 20, 2022
    Assignees: UWM Research Foundation, Inc., The Trustees of Columbia University in the City of New York
    Inventors: Alexander E. Arnold, Douglas C. Stafford, James M. Cook, Charles W. Emala, Gloria Forkuo, Rajwana Jahan, Revathi Kodali, Guanguan Li, Michael Rajesh Stephen
  • Patent number: 11447494
    Abstract: The present application provides tricyclic amine compounds, which are inhibitors of cyclin-dependent kinase 2 (CDK2), of Formula (I): as well as pharmaceutical compositions thereof, and methods of treating cancer using the same.
    Type: Grant
    Filed: April 30, 2020
    Date of Patent: September 20, 2022
    Assignee: Incyte Corporation
    Inventors: Qinda Ye, Ken Mukai, Liangxing Wu, Wenqing Yao
  • Patent number: 11440887
    Abstract: Noncovalent small-molecule inhibitors of the enzyme OGG1, methods of their manufacture, and applications for their administration are provided. Small molecule inhibitors were shown to be selective for inhibiting OGG1 over multiple repair enzymes, including other base excision repair enzymes, and it displayed no toxicity in two human cell lines. The inhibitors provide a tool for the study of the role of OGG1 in multiple disease-related pathways, and a therapeutic target for the treatment thereof.
    Type: Grant
    Filed: August 7, 2018
    Date of Patent: September 13, 2022
    Assignee: The Board of Trustees of the Leland Stanford Junior University
    Inventors: Eric T. Kool, Yuki Tahara
  • Patent number: 11440913
    Abstract: Compounds having formula (I), and enantiomers, and diastereomers, stereoisomers, pharmaceutically-acceptable salts thereof, (I) are useful as kinase modulators, including RIPK1 modulation. All the variables are as defined herein.
    Type: Grant
    Filed: October 29, 2018
    Date of Patent: September 13, 2022
    Assignee: Bristol-Myers Squibb Company
    Inventors: Michael E. Mertzman, Carolyn Diane Dzierba, Jason M. Guernon, Amy C. Hart, Guanglin Luo, John E. Macor, William J. Pitts, Jianliang Shi, Steven H. Spergel
  • Patent number: 11440915
    Abstract: The present invention relates to compounds of formula (I), wherein R is hydrogen or halogen, wherein R may be different if n=2 or 3; n is 1, 2 or 3; (II) is a disubstituted bicyclo[1,1,1]pentane or bicyclo[2,2,2]octane as defined below: (III) or (IV); or to a pharmaceutically active acid addition salt thereof, to a racemic mixture or to its corresponding enantiomer and/or an optical isomer and/or stereoisomer thereof. The compounds may be used for the treatment of Alzheimer's disease, cerebral amyloid angiopathy, hereditary cerebral hemorrhage with amyloidosis, Dutch-type (HCHWA-D), multi-infarct dementia, dementia pugilistica or Down syndrome.
    Type: Grant
    Filed: December 17, 2018
    Date of Patent: September 13, 2022
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Bjoern Bartels, Xinlan Aloise Ford Cook, Hasane Ratni, Michael Reutlinger, Walter Vifian
  • Patent number: 11434243
    Abstract: The invention relates to an improved process for preparing triazoloquinazolinones of Formula (I), including 9-benzyl-2-(4-methylphenyl)-2,6-dihydro[1,2,4]triazolo[4,3-c]quinazoline-3,5-dione, pharmaceutical compositions comprising the compounds of Formula (I), including 9-benzyl-2-(4-methylphenyl)-2,6-dihydro[1,2,4]triazolo[4,3-c]quinazoline-3,5-dione, prepared by the improved process, and methods of treatment using the compounds of Formula (I), including 9-benzyl-2-(4-methylphenyl)-2,6-dihydro[1,2,4]triazolo[4,3-c]quinazoline-3,5-dione, prepared by the improved process.
    Type: Grant
    Filed: December 19, 2018
    Date of Patent: September 6, 2022
    Assignee: GABATHER AB
    Inventors: Thomas Jagusch, Peter Adrianus Hubertus Zenhorst, Paula Anna Adriana Van Der Aa, Govert Arie Verspui, Martin Kas, Martina Scigelova
  • Patent number: 11434231
    Abstract: There are provided compounds, their preparation and their use in the treatment of KRAS-driven cancers. The compounds according to the invention (general formula Class III) disrupt dimerization of KRAS and are inhibitors of KRAS mutants such as KRAS G12D, KRAS G12V and KRAS 12C. Embodiments of the compounds according to the invention are selective inhibitors of KRAS mutants over the wild-type (WT) KRAS.
    Type: Grant
    Filed: July 8, 2020
    Date of Patent: September 6, 2022
    Inventors: Xiaohong Tian, Jian Hui Wu, Qianhui Yi
  • Patent number: 11420975
    Abstract: The present invention relates to a compound of formula I or a pharmaceutically acceptable salt, a solvate, an active metabolite, a polymorph, an ester, an optical isomer or a prodrug thereof, a pharmaceutical composition comprising the compound of formula I, and use of the compound, as a Bruton's tyrosine kinase inhibitor with high selectivity for BTK(C481S) mutant, in the manufacture of a medicament for preventing or treating a heteroimmune disease, an autoimmune disease or a cancer.
    Type: Grant
    Filed: January 13, 2022
    Date of Patent: August 23, 2022
    Assignee: TRANSTHERA SCIENCES (NANJING), INC.
    Inventor: Rongyao Chen
  • Patent number: 11414423
    Abstract: The present invention provides substituted 1,2,3,4,5,6-hexahydroazepino[4,5-b]indoles and methods of using the compounds for treating brain disorders.
    Type: Grant
    Filed: June 11, 2021
    Date of Patent: August 16, 2022
    Assignee: The Regents of the University of California
    Inventors: David E. Olson, Florence Wagner
  • Patent number: 11414422
    Abstract: 1-(3,4-Dihydro-1H-pyrido[4, 3-b]indol-2(5H)-yl)-2-hydroxyethanones are disclosed. The compounds are inhibitors of human cGAS in interferon-producing cell types. They are thus useful as therapeutic agents for treating cGAS-related autoimmune diseases in humans.
    Type: Grant
    Filed: February 5, 2019
    Date of Patent: August 16, 2022
    Assignee: The Rockefeller University
    Inventors: Lodoe Lama, Thomas Tuschl, Daisuke Tomita, Dinshaw Patel, J. Fraser Glickman, Taku Kamei, Michael Miller, Yasutomi Asano, Rei Okamoto, Shogo Hashizume, Jumpei Aida, Toshihiro Imaeda, Mayako Michino, Takanobu Kuroita
  • Patent number: 11414431
    Abstract: The present invention provides compounds of Formula I?: compositions thereof, and methods of using the same for the inhibition of TYK2, and the treatment of TYK2-mediated disorders.
    Type: Grant
    Filed: October 15, 2019
    Date of Patent: August 16, 2022
    Assignee: Nimbus Lakshmi, Inc.
    Inventors: Craig E. Masse, Jeremy Robert Greenwood, Sayan Mondal
  • Patent number: 11414421
    Abstract: The present invention relates to an improved process for the preparation of 7-cyclopentyl-N,N-dimethyl-2-{[5-(piperazin-1-yl)pyridin-2-yl]amino}-7H-pyrrolo[2,3-d]pyrimidine-6-carboxamide succinate (1/1) compound of formula-1a and its novel crystalline forms.
    Type: Grant
    Filed: January 10, 2019
    Date of Patent: August 16, 2022
    Assignee: NATCO PHARMA LTD
    Inventors: Arunkumar Thiriveedhi, Swapna Kondaveeti, Sathish Thumati, Naresh Ghanta, Janaki Rama Rao Ravi, Durga Prasad Konakanchi, Pulla Reddy Muddansani, Venkaiah Chowdary Nannapaneni
  • Patent number: 11414394
    Abstract: A process for producing a hydrate of a hydrochloride salt of 2,2?-((((((2-acetylnaphtho[2,3-b]furan-4,9-diyl)bis(oxy))bis(carbonyl))bis(azanediyl))bis(ethane-2,1-diyl))bis(azanediyl))diacetic acid of the formula: wherein the process comprises the following step: recrystallizing the hydrochloride salt of 2,2?-((((((2-acetylnaphtho[2,3-b]furan-4,9-diyl)bis(oxy))bis(carbonyl))bis(azanediyl))bis(ethane-2,1-diyl))bis(azanediyl))diacetic acid, in the presence of hydrochloric acid and a recrystallization solvent; wherein the recrystallization solvent is methanol, ethanol, 2-propanol, diethyl ether, ethyl acetate, benzene, toluene, acetone, dichloromethane, chloroform, hexane, dimethylformamide, acetonitrile, or water; or mixed solvent thereof.
    Type: Grant
    Filed: August 28, 2020
    Date of Patent: August 16, 2022
    Assignees: SUMITOMO PHARMA ONCOLOGY, INC., SUMITOMO PHARMA CO., LTD.
    Inventors: Hitoshi Ban, Seiji Kamioka, Yusuke Sawayama, Chiang Jia Li
  • Patent number: 11414419
    Abstract: The present disclosure is directed, in part, to substituted purines, or pharmaceutically acceptable salts thereof, represented by formula (VIII): for the treatment and/or prevention of neurodegenerative disease, mitochondrial disease, fibrosis, and/or cardiomyopathy.
    Type: Grant
    Filed: June 21, 2018
    Date of Patent: August 16, 2022
    Assignee: MITOKININ, INC.
    Inventors: Daniel de Roulet, Robert Devita
  • Patent number: 11414420
    Abstract: The invention provides new pyrimidine compounds having the general formula (I), wherein R1, R2, R3, n, and X are as described herein, compositions including the compounds, processes of manufacturing the compounds and methods of using the compounds.
    Type: Grant
    Filed: November 26, 2018
    Date of Patent: August 16, 2022
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Bjoern Bartels, Xinlan Aloise Ford Cook, Hasane Ratni, Michael Reutlinger, Walter Vifian
  • Patent number: 11407748
    Abstract: The present invention aims to provide a heterocyclic compound having an AMPA receptor potentiator effect, which is expected to be useful as an agent for the prophylaxis or treatment of depression, Alzheimer's disease, schizophrenia, attention deficit hyperactivity disorder (ADHD) and the like. The present invention relates to a compound represented by the formula (I): wherein each symbol is as described in the specification, or a salt thereof.
    Type: Grant
    Filed: October 4, 2018
    Date of Patent: August 9, 2022
    Assignee: Takeda Pharmaceutical Company Limited
    Inventors: Shinji Nakamura, Satoshi Mikami, Tomoaki Hasui, Tohru Yamashita, Shinji Morimoto, Hidekazu Tokuhara, Norio Oyabu, Masami Yamada, Atsuko Ochida, Kazuaki Takami, Xin Liu
  • Patent number: 11407751
    Abstract: The present invention provides methods for the preparation of substituted heterocycle fused gamma-carbolines, such as Formula 2J, as shown below, intermediates useful in producing them and methods for producing such intermediates and such heterocycle fused gamma-carbolines, and as further defined herein:
    Type: Grant
    Filed: October 7, 2019
    Date of Patent: August 9, 2022
    Assignee: INTRA-CELLULAR THERAPIES, INC.
    Inventors: John Charles Tomesch, Peng Li, Qiang Zhang, Andrew S. Thompson