Patents Examined by Ebenezer O. Sackey
  • Patent number: 11407735
    Abstract: The present invention describes specific crystalline forms of N-[4-(Chlorodifluoromethoxy)phenyl]-6-[(3R)-3-hydroxypyrrolidin-1-yl]-5-(1H-pyrazol-5 -yl)pyridine-3-carboxamide. The present invention further relates to methods for preparing said crystalline forms, pharmaceutical compositions comprising said crystalline forms, and methods of using said crystalline forms and pharmaceutical compositions to treat disease.
    Type: Grant
    Filed: May 14, 2020
    Date of Patent: August 9, 2022
    Assignee: NOVARTIS AG
    Inventors: Stephanie Kay Dodd, Arnaud Grandeury, Emmanuel Suffert, Evgenia Rousaki
  • Patent number: 11390609
    Abstract: The present invention relates to a Rho-associated protein kinase inhibitor of formula (I), a pharmaceutical composition comprising the same, a preparation method thereof, and a use of the same in preventing or treating a disease mediated by Rho-associated protein kinase (ROCK).
    Type: Grant
    Filed: June 29, 2018
    Date of Patent: July 19, 2022
    Assignee: BEIJING TIDE PHARMACEUTICAL CO., LTD.
    Inventors: Yanping Zhao, Hongjun Wang, Gong Li, Yuanyuan Jiang, Xiang Li, Bin Liu, Weiting Zhong, Kai Liu, Fajie Li, Liying Zhou, Yanan Liu
  • Patent number: 11389434
    Abstract: The inventors demonstrate for the first time the activation of the Hedgehog (HH) signaling pathway in normal and abnormal human mast cells (MCs). These results prompt the inventors to explore the consequence of the inhibition of the HH pathway, especially the canonical pathway, on MC proliferation. They demonstrate that Hedgehog inhibitors inhibit proliferation and induces apoptosis of mast cells. Accordingly the present invention relates to a method of treating a mast cell disease in a patient in need there of comprising administering to the patient a therapeutically effective amount of a Hedgehog inhibitor.
    Type: Grant
    Filed: May 17, 2018
    Date of Patent: July 19, 2022
    Assignees: INSERM, FONDATION IMAGINE, UNIVERSITE PARIS DESCARTES, ASSISTANCE PUBLIQUE-HOPITAUX DE PARIS (APHP), CENTRE NATIONAL DE LA RECHERCHE SCIENTIFIQUE (CNRS)
    Inventors: Leila Maouche-Chretien, Christine Bodemer, Olivier Hermine, Laura Polivka
  • Patent number: 11352356
    Abstract: The present invention provides compounds and compositions thereof which are useful as inhibitors of plasma kallikrein and which exhibit desirable characteristics for the same.
    Type: Grant
    Filed: June 22, 2020
    Date of Patent: June 7, 2022
    Assignee: Takeda Pharmaceutical Company Limited
    Inventors: Nikolaos Papaioannou, Sarah Jocelyn Fink, Thomas Allen Miller, Gerald Wayne Shipps, Jr., Jeremy Mark Travins, David Edward Ehmann, Alastair Rae, John Mark Ellard
  • Patent number: 11312708
    Abstract: A process for preparing compounds of formula (I), or a salt or solvate thereof, including Brexpiprazole, which process comprises cyclization of a compound of formula (II) or (III), or a salt or solvate thereof. The invention also refers to intermediates of said process.
    Type: Grant
    Filed: February 7, 2020
    Date of Patent: April 26, 2022
    Assignee: CRYSTAL PHARMA, S.A.U.
    Inventors: Alfonso Pérez Encabo, José Ángel Turiel Hernandez, Yolanda Fernández Sainz, Antonio Lorente Bonde-Larsen
  • Patent number: 11286262
    Abstract: The present invention provides industrially suitable processes for preparing intermediates in the production of substituted polycyclic pyridone derivatives having a cap-dependent endonuclease inhibitory activity. In the process as shown below, wherein each symbol is as defined in the specification, an optically active substituted tricyclic pyridone derivative of the formula (VII) is obtained in high yield and high enantioselectivity by subjecting a compound of the formula (III) or (VI) to intramolecular cyclization with controlling stereochemistry to obtain a compound of the formula (IV) having a removable functional group on an asymmetric carbon, and then removing the functional group thereof.
    Type: Grant
    Filed: October 5, 2018
    Date of Patent: March 29, 2022
    Assignee: SHIONOGI & CO., LTD.
    Inventors: Kazuya Okamoto, Tatsuhiko Ueno
  • Patent number: 11285153
    Abstract: A substituted pyrimidine piperazine compound and uses thereof, and a pharmaceutical composition containing the compound and uses thereof. Wherein the compound has Formula (I), or a stereoisomer, a geometric isomer, a tautomer, an N-oxide, a hydrate, a solvate, a metabolite, a pharmaceutically acceptable salt or a prodrug thereof. The substituted pyrimidine piperazine compound and the pharmaceutical composition containing the compound can be used to inhibit 5-hydroxytryptamine reuptake and/or activate the 5-HT1A receptors. Also, a method of preparing such compounds and pharmaceutical compositions, and uses thereof in the treatment of central nervous system dysfunction.
    Type: Grant
    Filed: September 21, 2018
    Date of Patent: March 29, 2022
    Assignee: SUNSHINE LAKE PHARMA CO., LTD.
    Inventors: Chuanfei Jin, Wenhe Zhong, Haiping Liang, Yingjun Zhang
  • Patent number: 11273160
    Abstract: Disclosed herein are methods for treating a subject afflicted with a cancer having an activating RET alteration by administering an effective amount of a selective RET inhibitor, e.g., Compound 1 or pharmaceutically acceptable salts thereof, including, e.g., administering an amount of 60 mg to 400 mg of the selective RET inhibitor once daily.
    Type: Grant
    Filed: December 18, 2020
    Date of Patent: March 15, 2022
    Assignee: BLUEPRINT MEDICINES CORPORATION
    Inventors: Erica Evans Raab, Beni B. Wolf
  • Patent number: 11254683
    Abstract: The disclosure is directed to compounds of Formula I Pharmaceutical compositions comprising compounds of Formula I, as well as methods of their use and preparation, are also described.
    Type: Grant
    Filed: August 5, 2020
    Date of Patent: February 22, 2022
    Assignee: Prelude Therapeutics Incorporated
    Inventors: Juan Luengo, Hong Lin, Michael Hawkins, Rupa Shetty, Philip Pitis, Gisela Saborit Villarroya
  • Patent number: 11253616
    Abstract: The present invention includes an engineered cell comprising a chimeric antigen receptor (CAR) further comprising a nucleic acid molecule comprising a suicide gene comprising a ligand binding domain and a suicide domain wherein the ligand binding domain is capable of binding to radiolabeled tracer or a small molecule suicide switch. This invention also includes methods for inducing apoptosis of an engineered cell, methods for assessing the efficacy or toxicity of an adoptive cell therapy in a subject, methods for detecting the quantity of engineered T cells in a subject, methods for monitoring an immunotherapy treatment in a subject and methods of imaging engineered T cells in a subject. In some embodiments, the imaging is performed via Positron Emission Topography (PET). This invention further includes a chemical inducer of dimerization (CID), wherein the CID is a Bis-Trimethoprim (Bis-TMP).
    Type: Grant
    Filed: September 6, 2018
    Date of Patent: February 22, 2022
    Assignee: The Trustees of the University of Pennsylvania
    Inventors: Michael Farwell, Mark Sellmyer, Katheryn M. Lohith
  • Patent number: 11253516
    Abstract: The present invention relates to a N2,N4-diphenylpyrimidin-2,4-diamine derivative, a method for preparing the same, and a pharmaceutical composition for the prevention or treatment of cancer, containing the same as an active ingredient. The derivative shows a relatively weak EGFR activity inhibitory effect on wild-type EGFR, a high inhibitory ability on EGFR mutation, and a high inhibitory ability on even FLT3 and FLT3 mutation, and thus, can be effectively used for the treatment of cancer with EGFR mutation or cancer with FLT3 or a mutation thereof, and the derivative shows a synergy effect at the time of combination administration, and thus can be effectively used for the treatment of combination administration.
    Type: Grant
    Filed: June 12, 2018
    Date of Patent: February 22, 2022
    Assignee: Korea Research Institute of Chemical Technology
    Inventors: Kwangho Lee, Inji Shin, Gildon Choi, Chong Hak Chae, Hyeon Jeong Choe, Myoung Eun Jung, Byeong Uk Jeon, Byoung Chul Cho, Chae Won Park, Hwan Kim, Krishna Babu Duggirala
  • Patent number: 11252963
    Abstract: Compounds of formula (I) as defined herein, to processes for preparing them, to pesticidal, in particular insecticidal, acaricidal, molluscicidal and nematicidal compositions comprising them and to methods of using them to combat and control pests such as insect, acarine, mollusc and nematode pests.
    Type: Grant
    Filed: August 9, 2018
    Date of Patent: February 22, 2022
    Assignee: SYNGENTA PARTICIPATIONS AG
    Inventors: Denis Gribkov, Myriem El Qacemi, André Stoller, André Jeanguenat, Aurelien Bigot
  • Patent number: 11247983
    Abstract: Disclosed are compounds of formula (I), pharmaceutical compositions comprising such compounds and methods/uses of using the same, for example, for treating a JAK-related disorder, such as cancer, cancer cachexia or an immune disorder: wherein R1 is methyl or ethyl; R2 is selected from methyl, ethyl, methoxy and ethoxy; R3 is selected from hydrogen, chlorine, fluorine, bromine and methyl; R4 is selected from methyl, ethyl and —CH2OCH3; R5 and R6 are each individually methyl or hydrogen; and R7 is selected from methyl, ethyl, —(CH2)2OH and —(CH2)2OCH3, or a pharmaceutically acceptable salt thereof.
    Type: Grant
    Filed: April 28, 2020
    Date of Patent: February 15, 2022
    Assignee: Dizal (Jiangsu) Pharmaceutical Co., Ltd.
    Inventors: Annika Birgitta Margareta Astrand, Neil Patrick Grimster, Sameer Kawatkar, Jason Grant Kettle, Magnus K. Nilsson, Linette Ruston, Qibin Su, Melissa Vasbinder, Jon James Winter-Holt, Richard Donald Woessner, Claudio Edmundo Chuaqui, James McCabe
  • Patent number: 11241013
    Abstract: The present invention relates to benzimidazole ethers and related compounds which are of use in the field of agriculture as fungicides.
    Type: Grant
    Filed: October 17, 2018
    Date of Patent: February 8, 2022
    Inventors: Christopher John Urch, Roger John Butlin, Stephania Christou, Rebecca Kathryn Booth
  • Patent number: 11242353
    Abstract: The present invention is directed to heterocyclic SV40 Factor (LSF) inhibitors and their uses. In some implementations, the present invention discloses small-molecule compounds of Formula (I). In some implementations, the compounds of Formula (I) are used in methods for inhibiting LSF in a subject. In some implementations, the compounds of Formula (I) are used in methods for treating cancer in a subject.
    Type: Grant
    Filed: January 22, 2021
    Date of Patent: February 8, 2022
    Assignee: TRUSTEES OF BOSTON UNIVERSITY
    Inventors: Scott E. Schaus, Ulla Hansen, John A. Kavouris, Emily A. York, Niranjana Pokharel
  • Patent number: 11241428
    Abstract: The present invention relates to novel heteroaryl amide derivatives of formula (1) as selective inhibitors of histone deacetylase 1 and 2 (hdac1-2) to processes for their preparation, to pharmaceutical compositions comprising said compounds and to the use of said compounds for manufacturing a medicament for the treatment of pathological conditions or diseases that can improve by inhibition the activity of histone deacetylase class I, particularly HDAC1 and HDAC2, such as cancer, neurodegenerative diseases, Infectious diseases, inflammatory diseases, heart failure and cardiac hypertrophy, diabetes, polycystic kidney disease, sickle cell disease and ?-thalassemia disease and to methods for the treatment of the diseases mentioned above.
    Type: Grant
    Filed: July 9, 2018
    Date of Patent: February 8, 2022
    Assignee: Medibiofarma, S.L.
    Inventors: Julio Castro Palomino Laria, Juan Camacho Gómez, Rodolfo Rodríguez Iglesias
  • Patent number: 11236103
    Abstract: The present application provides compounds that modulate CDK protein function. Methods of making the compounds, compositions containing the compounds, and uses of the compounds for treating or ameliorating of diseases, disorders, or conditions associated with CDK proteins, are also disclosed.
    Type: Grant
    Filed: July 25, 2019
    Date of Patent: February 1, 2022
    Assignee: BioTheryX, Inc.
    Inventors: Kyle W. H. Chan, Aparajita Hoskote Chourasia, Paul E. Erdman, Leah Fung, David Aaron Hecht, Frank Mercurio, Robert Sullivan, Joseph P. Vacca
  • Patent number: 11229636
    Abstract: The present invention provides substituted tetrahydroquinolinone and related compounds of formula (I), which are therapeutically useful as modulators of Retinoic acid receptor-related orphan receptors (RORs), more particularly as ROR? modulators. These compounds are useful in the treatment and prevention of diseases and/or disorder, in particular their use in diseases and/or disorder mediated by ROR? receptor. The present invention also provides preparation of the compounds and pharmaceutical formulations comprising at least one of the substituted tetrahydroquinolinone or related compounds of formula (I), together with a pharmaceutically acceptable carrier, diluent or excipient therefor.
    Type: Grant
    Filed: December 10, 2019
    Date of Patent: January 25, 2022
    Assignee: AURIGENE DISCOVERY TECHNOLOGIES LIMITED
    Inventors: Ravi Kotrabasaiah Ujjinamatada, Chetan Pandit
  • Patent number: 11230532
    Abstract: The present disclosure provides pyrimidine compounds of Formula 1 and uses thereof, for example, for the potential treatment of diseases associated with P2X purinergic receptors: In certain aspects, the present disclosure provides P2X3 and/or P2X2/3 antagonists which are useful, for example, for the potential treatment of visceral organ, cardiovascular and pain-related diseases, conditions and disorders.
    Type: Grant
    Filed: April 13, 2020
    Date of Patent: January 25, 2022
    Assignee: AFFERENT PHARMACEUTICALS, INC.
    Inventors: Ronald Charles Hawley, Prabha Ibrahim, Anthony P. Ford, Joel R. Gever
  • Patent number: 11230554
    Abstract: The present invention provides methods of treating or preventing autoimmune diseases with 2,4-pyrimidinediamine compounds, as well as methods of treating, preventing or ameliorating symptoms associated with such diseases. Specific examples of autoimmune diseases that can be treated or prevented with the compounds include rheumatoid arthritis and/or its associated symptoms, systemic lupus erythematosis and/or its associated symptoms and multiple sclerosis and/or its associated symptoms.
    Type: Grant
    Filed: March 21, 2019
    Date of Patent: January 25, 2022
    Assignee: Rigel Pharmaceuticals, Inc.
    Inventors: Rajinder Singh, Ankush Argade, Hui Li, Somasekhar Bhamidipati, David Carroll, Catherine Sylvain, Jeffrey Clough, Holger Keim