Patents Examined by Douglas M Willis
  • Fasudil for the treatment of schizophrenia
    Patent number: 11478482
    Abstract: The present invention provides an antipsychotic drug comprising fasudil or a pharmaceutically acceptable salt thereof as an active agent for the treatment of schizophrenia, including schizophrenia caused by dysfunction of ARHGAP10.
    Type: Grant
    Filed: January 31, 2022
    Date of Patent: October 25, 2022
    Assignee: NATIONAL UNIVERSITY CORPORATION TOKAI NATIONAL HIG
    Inventors: Norio Ozaki, Kiyofumi Yamada, Taku Nagai, Daisuke Mori, Yuko Arioka, Itaru Kushima
  • 2-(3?-(hydroxymethyl)-1-methyl-5-((5-(2-methyl-4-(oxetan-3-yl)piperazin-1-yl)pyridin-2-yl)amino)-6-oxo-1,6-dihydro-[3,4?-bipyridin]-2?-yl)-7,7-dimethyl-7,8-dihydro-2H-cyclopenta[4,5]pyrrolo[1,2-a]pyrazin-1(6H)-one as a BTK inhibitor
    Patent number: 11478474
    Abstract: The present invention relates to heteroaryl heterocyclic compounds, e.g., the compound of the formula shown below, pharmaceutical compositions comprising same, methods for preparing same, and uses thereof.
    Type: Grant
    Filed: October 20, 2021
    Date of Patent: October 25, 2022
    Assignee: HUTCHISON MEDIPHARMA LIMITED
    Inventors: Guangxiu Dai, Kun Xiao
  • Substituted pyrrolo[1,2-c]pyrimidines as hepatitis B antiviral agents
    Patent number: 11472808
    Abstract: The present invention discloses substituted pyrrolo[1,2-c]pyrimidines, such as the compound which inhibit the protein(s) encoded by hepatitis B virus (HBV) or interfere with the function of the HBV life cycle of the hepatitis B virus and are also useful as antiviral agents. The present invention further relates to pharmaceutical compositions comprising the aforementioned compounds for administration to a subject suffering from HBV infection. The invention also relates to methods of treating an HBV infection in a subject by administering a pharmaceutical composition comprising the compounds of the present invention.
    Type: Grant
    Filed: June 4, 2020
    Date of Patent: October 18, 2022
    Assignee: Enanta Pharmaceuticals, Inc.
    Inventors: Yao-Ling Qiu, Xiaowen Peng, Wei Li, Xuri Gao, Jorden Kass, Byung-Chul Suh, Hui Cao, Jiajun Zhang, Yat Sun Or
  • Crystalline forms of 8-(2-fluorobenzyl)-6-(3-(trifluoromethyl)-1H-1,2,4-triazol-5-yl)imidazo[1,2-a]pyrazine as sGC stimulators
    Patent number: 11466015
    Abstract: The present disclosure relates to crystalline forms of 8-(2-fluorobenzyl)-6-(3-(trifluoromethyl)-1H-1,2,4-triazol-5-yl)imidazo[1,2-a]pyrazine, depicted below as a compound of Formula (I): which are useful as a stimulator of soluble guanylate cyclase (sGC). The present disclosure also provides pharmaceutically acceptable compositions comprising the crystalline forms and methods of using said compositions in the treatment of various disorders.
    Type: Grant
    Filed: March 7, 2019
    Date of Patent: October 11, 2022
    Assignee: Cyclerion Therapeutics, Inc.
    Inventors: Kwame W. Nti-Addae, Leena Kumari Prasad, Thomas Storz
  • Co-crystals of neflamapimod (VX-745)
    Patent number: 11466008
    Abstract: Provided herein are co-crystal forms comprising 5-(2,6-dichlorophenyl)-2-(2,4-difluorophenylthio)-6H-pyrimido[1,6-b]pyridazin-6-one (VX-745): and compositions thereof, useful as inhibitors of one or more protein kinases and which exhibit desirable characteristics for the same.
    Type: Grant
    Filed: September 18, 2018
    Date of Patent: October 11, 2022
    Assignee: EIP Pharma, LLC
    Inventors: John Jahangir Alam, Jeffrey Douglas Wilson
  • Substituted pyridines as apoptosis signal-regulating kinase 1 inhibitors
    Patent number: 11466033
    Abstract: The present invention discloses compounds of Formula (I), and pharmaceutically acceptable salts and esters thereof: which inhibit the Apoptosis signal-regulating kinase 1 (ASK-1), which associated with autoimmune disorders, neurodegenerative disorders, inflammatory diseases, chronic kidney disease, cardiovascular disease. The present invention further relates to pharmaceutical compositions comprising the aforementioned compounds for administration to a subject suffering from ASK-1 related disease. The invention also relates to methods of treating an ASK-1 related disease in a subject by administering a pharmaceutical composition comprising the compounds of the present invention. The present invention specifically relates to methods of treating ASK-1 associated with hepatic steatosis, including non-alcoholic fatty liver disease (NAFLD) and non-alcohol steatohepatitis disease (NASH).
    Type: Grant
    Filed: March 24, 2020
    Date of Patent: October 11, 2022
    Assignee: Enanta Pharmaceuticals, Inc.
    Inventors: Brett Granger, Yong He, Guoqiang Wang, Yat Sun Or
  • Substituted lactams showing serotonin 5-HT receptor activity
    Patent number: 11466007
    Abstract: The present invention relates to a medicament for treating neuropsychiatric diseases, comprising a compound of Formula (1): or a pharmaceutically acceptable salt thereof, as an active ingredient.
    Type: Grant
    Filed: July 22, 2019
    Date of Patent: October 11, 2022
    Assignee: SUMITOMO PHARMA CO., LTD.
    Inventors: Hidefumi Yoshinaga, Yohei Ikuma, Junya Ikeda, Satoshi Adachi, Harunobu Mitsunuma, Yoshinori Aihara, Jeremy Besnard, Andrew Simon Bell
  • Process for preparing soluble guanylate cyclase stimulators
    Patent number: 11466014
    Abstract: The invention relates to novel methods for preparing 3-substituted 1,2,4-triazole compounds of Formula IA: as sGC stimulators. The method comprises reacting the amidrazone compound represented by Formula IIA: or a salt thereof, with a carboxylic acid, an activated ester, a thioester, an acid halide, a thioacyl halide, or an acid anhydride in the presence of a base.
    Type: Grant
    Filed: March 7, 2019
    Date of Patent: October 11, 2022
    Assignee: Cyclerion Therapeutics, Inc.
    Inventor: Thomas Storz
  • Substituted pyrrolo[2,1-f][1,2,4]triazines as KIT and/or PDGFR-? inhibitors
    Patent number: 11459334
    Abstract: Provided in the present invention are a substituted pyrrolotriazine compound, a pharmaceutical composition thereof and a use thereof, the pyrrolotriazine compound being a compound represented by formula (I), or a pharmaceutically acceptable salt, prodrug, hydrate or solvent compound, crystalline form, stereoisomer or isotope variant thereof. The compound and composition of the present invention may be used in the treatment of conditions associated with KIT and/or PDGFR?.
    Type: Grant
    Filed: April 15, 2019
    Date of Patent: October 4, 2022
    Assignee: Shenzhen TargetRx, Inc.
    Inventors: Yihan Wang, Huanyin Li
  • Substituted pyrrolo[2,3-d]pyrimidines as JAK inhibitors
    Patent number: 11459333
    Abstract: Described herein are Janus kinase (JAK) inhibitors of the Formula (I?): and methods of utilizing JAK inhibitors of the Formula (I?) in the treatment of diseases, disorders, or conditions. Also described herein are pharmaceutical compositions containing such compounds.
    Type: Grant
    Filed: August 7, 2020
    Date of Patent: October 4, 2022
    Assignee: VIMALAN BIOSCIENCES, INC.
    Inventors: Raju Mohan, John Nuss, Jason Harris, Shendong Yuan
  • Substituted 2-azabicyclo[3.1.0]hexanes as TRK kinases inhibitors
    Patent number: 11459332
    Abstract: Provided are certain TRK inhibitors of formula (I): pharmaceutical compositions thereof, and methods of use thereof.
    Type: Grant
    Filed: March 13, 2019
    Date of Patent: October 4, 2022
    Assignee: Fochon Biosciences, Ltd.
    Inventors: Hongbin Liu, Haohan Tan, Chengxi He, Xianlong Wang, Qihong Liu, Zhifu Li, Zuwen Zhou, Yuwei Gao, Lihua Jiang, Li Linghu, Shu Lin, Xingdong Zhao, Weibo Wang
  • Substituted [1,2,4]triazolo[4,3-a]pyrazines as phosphodiesterase inhibitors
    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
  • Substituted pyrazolo[1,5-a]pyrimidines as tropomyosin receptor kinase inhibitors
    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
  • Pyrazolopyrimidine inhibitors of JAK kinases and uses thereof
    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
  • Tricyclic amine compounds as CDK2 inhibitors
    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
  • Substituted benzo[f]imidazo[1,5-a][1,4]diazepines as GABA(a) receptor modulators
    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
  • Aminoimidazopyridazines as kinase inhibitors
    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
  • Substituted 1,2,3,4-tetrahydroquinolines as inhibitors of repair enzyme 8-oxoguanine deoxyribonucleic acid glycosylase activity
    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
  • Triazolo-azepine derivatives
    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
  • Triazoloquinazolinone synthesis
    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