Patents Examined by Douglas M Willis
  • Patent number: 11124517
    Abstract: The present disclosure relates to crystalline forms of Baricitinib and processes for preparation thereof. The present disclosure also relates to pharmaceutical composition containing these crystalline forms and use of these crystalline forms for preparing JAK inhibitor drugs and preparing drugs treating rheumatoid arthritis. The crystalline forms of the present disclosure have one or more improved properties compared with crystalline forms of the prior art and have significant values for future drug optimization and development.
    Type: Grant
    Filed: May 23, 2018
    Date of Patent: September 21, 2021
    Inventors: Minhua Chen, Yanfeng Zhang, Qiyue Liu, Xiaoyu Zhang
  • Patent number: 11116741
    Abstract: The present invention relates to the use of a serotoninergic receptor antagonist, such as sarpogrelate or compositions thereof, for the treatment and/or prevention of heart damages in mammals.
    Type: Grant
    Filed: April 11, 2018
    Date of Patent: September 14, 2021
    Assignee: CEVA SANTE ANIMALE
    Inventors: Estelle Ayme-Dietrich, Jérôme Guyonnet, Roland Lawson, Luc Maroteaux, Laurent Monassier
  • Patent number: 11117901
    Abstract: The present invention relates to substituted pyrazolo-quinazoline derivatives which modulate the activity of Choline Kinase (ChoK). The compounds of this invention are therefore useful in treating diseases caused by an altered choline metabolism, such as cancer, cell proliferative disorders, infectious diseases of different origin, immune-related disorders and neurodegenerative disorders. The present invention also provides methods for preparing these compounds, pharmaceutical compositions comprising these compounds, and methods of treating diseases utilizing pharmaceutical compositions comprising these compounds.
    Type: Grant
    Filed: July 3, 2018
    Date of Patent: September 14, 2021
    Assignee: NERVIANO MEDICAL SCIENCES S.R.L.
    Inventors: Alessandra Badari, Elena Casale, Marcella Nesi, Francesca Quartieri
  • Patent number: 11111246
    Abstract: The invention relates to Substituted-Quinoxaline-Type Bridged-Piperidine Compounds, compositions comprising an effective amount of a Substituted-Quinoxaline-Type Bridged-Piperidine Compound and methods to treat or prevent a condition, such as pain, comprising administering to an animal in need thereof an effective amount of a Substituted-Quinoxaline-Type Bridged-Piperidine Compound.
    Type: Grant
    Filed: December 6, 2019
    Date of Patent: September 7, 2021
    Assignee: Purdue Pharma L.P.
    Inventors: Jiangchao Yao, John W. F. Whitehead, Naoki Tsuno, Kouki Fuchino
  • Patent number: 11111248
    Abstract: The present invention relates to a crystal form of 2-(6-methyl-pyridin-2-yl)-3-(6-amido-quinolin-4-yl)-5,6-dihydro-4h-pyrrolo[1,2-b]pyrazole (Galunisertib or LY2157299), represented by formula (I). Compared with the known solid form of Galunisertib, the crystal form of the present invention has advantages in terms of solubility, hygroscopicity, crystal stability, morphology and the like. The present invention also relates to a process of preparing the crystal forms of Galunisertib, a pharmaceutical composition thereof and a use thereof in the preparation of a medicament for the prevention and/or treatment of diseases associated with TGF-beta.
    Type: Grant
    Filed: March 17, 2017
    Date of Patent: September 7, 2021
    Assignee: Hangzhou SoliPharma Co., Ltd.
    Inventors: Xiaohong Sheng, Xiaoxia Sheng, Jing Wang
  • Patent number: 11111218
    Abstract: A new crystalline form of 5-amino-2,3-dihydro-1,4-phthalazinedione (luminol) is provided. Advantageous uses for this crystalline form as a detecting agent or as an agent for forensic purposes are disclosed, as well a pharmaceutical composition containing said crystalline form.
    Type: Grant
    Filed: February 15, 2017
    Date of Patent: September 7, 2021
    Assignee: METRIOPHARM AG
    Inventors: Thomas Martin, Josef Breu, Juliane Fleissner, Wolfgang Brysch, Jörg Von Wegerer
  • Patent number: 11103511
    Abstract: The present invention provides an application of N-benzyl tryptanthrin derivative as tryptophan dioxygenase (TDO) inhibitor, and more specifically an application of N-benzyl tryptanthrin derivative or a pharmaceutically acceptable salt thereof. Said derivative has a structural general formula as represented by formula 1, wherein each group is defined as in the specification. The derivative of the present invention has a good TDO inhibiting activity and can be used to prepare a treatment for diseases associated with TDO activity and expression.
    Type: Grant
    Filed: June 5, 2018
    Date of Patent: August 31, 2021
    Assignee: FUDAN UNIVERSITY
    Inventor: Qing Yang
  • Patent number: 11091495
    Abstract: The present invention relates to compounds that inhibit Polycomb Repressive Complex 2 (PRC2) activity. In particular, the present invention relates to compounds, pharmaceutical compositions and methods of use, such as methods of treating cancer using the compounds of Formula (I) and pharmaceutical compositions of the present invention.
    Type: Grant
    Filed: December 9, 2020
    Date of Patent: August 17, 2021
    Assignee: MIRATI THERAPEUTICS, INC.
    Inventors: Matthew Arnold Marx, Matthew Randolph Lee, Thomas P. Bobinski, Aaron Craig Burns, Nidhi Arora, James Gail Christensen, John Michael Ketcham
  • Patent number: 11084823
    Abstract: The present invention relates to a compound represented by the Chemical Formula 1 defined in the present specification, or a pharmaceutically acceptable salt thereof. The compound according to the present invention can be usefully used for the prevention or treatment of diseases which are associated with kinase inhibitory actions.
    Type: Grant
    Filed: March 19, 2018
    Date of Patent: August 10, 2021
    Assignee: Daewoong Pharmaceutical Co., Ltd.
    Inventors: In Woo Kim, Ja Kyung Yoo, Ji Duck Kim, Sun Ah Jun, Jun Hee Lee
  • Patent number: 11084825
    Abstract: Disclosed herein are heterocyclic compounds that inhibit the binding of menin and MLL or MLL fusion proteins. Also described are specific irreversible inhibitors of menin-MLL interaction. Also disclosed are pharmaceutical compositions that include the compounds. Methods of using the menin-MLL irreversible inhibitors are disclosed, alone or in combination with other therapeutic agents, for the treatment of autoimmune diseases or conditions, heteroimmune diseases or conditions, cancer, including lymphoma, leukemia and other diseases or conditions dependent on menin-MLL inter-action; or a pharmaceutically acceptable salt thereof.
    Type: Grant
    Filed: December 31, 2019
    Date of Patent: August 10, 2021
    Assignee: BIOMEA FUSION, LLC
    Inventors: Thomas Butler, Jim Palmer, Ravi Upasani, Matthew Welsch, Sridhar Vempati, Brendan Kelly, Edward Painter
  • Patent number: 11078207
    Abstract: Provided are a novel pyrimidine compound that inhibits HER2 activity and exhibits brain penetration properties, or a salt thereof, and a pharmaceutical composition comprising the same. A compound represented by the following formula (I), or a salt thereof: wherein R1 represents a C1-C4 alkyl group optionally having a C1-C4 alkoxy group as a substituent, or a C3-C4 cycloalkyl group; R2 represents a hydrogen atom, a halogen atom, a C1-C6 alkyl group optionally having 1 to 5 C1-C4 alkoxy groups or fluorine atoms each as a substituent(s), or a C1-C6 alkoxy group; R3 represents a hydrogen atom, or a C1-C4 alkyl group optionally having 1 to 5 fluorine atoms as a substituent(s); R4 represents a hydrogen atom or a C1-C4 alkyl group; and R5 represents a phenyl group optionally having 1 to 3 substituents selected from fluorine atoms and chlorine atoms.
    Type: Grant
    Filed: October 8, 2020
    Date of Patent: August 3, 2021
    Assignee: TAIHO PHARMACEUTICAL CO., LTD.
    Inventors: Masayuki Nakamura, Takahiro Asai, Satoru Iguchi, Kei Oguchi
  • Patent number: 11077107
    Abstract: Disclosed are compounds of the formula (I) wherein the groups R1 to R3 have the meanings given in the claims and in the specification. The compounds of the invention are suitable for the treatment of diseases characterized by excessive or abnormal cell proliferation pharmaceutical preparations containing such compounds and their uses as a medicament.
    Type: Grant
    Filed: April 19, 2019
    Date of Patent: August 3, 2021
    Inventors: Harald Engelhardt, Davide Gianni, Christian Smethurst
  • Patent number: 11071724
    Abstract: Compositions for treating presbyopia may include active pharmaceutical ingredients of pilocarpine HCl, phenylephrine HCl, pheniramine maleate, and ketorolac tromethamine. Other ingredients may include boric acid, polyethylene glycol, propylene glycol, and BAK (benzalkonium chloride). The pilocarpine HCl may be in a range of 0.1% to 2%. The phenylephrine HCl may be in a range of 0.1% to 1.5%. The pheniramine maleate may be in a range of 0.07% to 0.35%. The ketorolac tromethamine may be in a range of 0.01% to 0.6%. The boric acid may be in a range of 0.5% to 1.5%. The polyethylene glycol may be in a range of 0.1% to 1%. The propylene glycol may be in a range of 0.1% to 1%. The BAK may be in a range of 0.005% to 0.01%. The solvent may be mostly water.
    Type: Grant
    Filed: October 2, 2019
    Date of Patent: July 27, 2021
    Assignee: OCULAR SCIENCE, INC.
    Inventors: Anthony Sampietro, Damien Goldberg, Amy Frost, Brian Holdorf
  • Patent number: 11072582
    Abstract: The present invention is directed to novel compounds of formula (I) and their use in treating and/or preventing metabolic diseases.
    Type: Grant
    Filed: July 15, 2020
    Date of Patent: July 27, 2021
    Assignee: Epics Therapeutics
    Inventors: Hamid R. Hoveyda, Didier Schils, Ludivine Zoute, Julien Parcq
  • Patent number: 11066407
    Abstract: The present invention provides methods for the preparation of certain optionally substituted heterocycle fused gamma-carbolines of Formula 2F, as shown below and as further defined herein:
    Type: Grant
    Filed: December 12, 2019
    Date of Patent: July 20, 2021
    Assignee: INTRA-CELLULAR THERAPIES, INC.
    Inventors: John Charles Tomesch, Peng Li, Wei Yao, Qiang Zhang, James David Beard, Andrew S. Thompson, Hua Cheng, Lawrence P. Wennogle
  • Patent number: 11066363
    Abstract: The application relates to a compound of Formula (I): which modulates the activity of ALK or SRPK, a pharmaceutical composition comprising the compound, and a method of treating or preventing a disease in which ALK or SRPK plays a role.
    Type: Grant
    Filed: October 30, 2019
    Date of Patent: July 20, 2021
    Assignee: DANA-FARBER CANCER INSTITUTE, INC.
    Inventors: John Hatcher, Nathanael S. Gray, Hwangeun Choi, Pasi Janne, Tinghu Zhang
  • Patent number: 11066412
    Abstract: Disclosed herein are novel bifunctional compounds and their uses for the treatment and/or prophylaxis of cancers.
    Type: Grant
    Filed: November 16, 2018
    Date of Patent: July 20, 2021
    Assignee: Academia Sinica
    Inventors: Te-Chang Lee, Tsann-Long Su, Tai-Lin Chen
  • Patent number: 11059829
    Abstract: In some embodiments, the invention relates to crystalline solid forms, including hydrates, polymorphs, and salt forms, of (S)-4-(8-amino-3-(1-(but-2-ynoyl)pyrrolidin-2-yl)imidazo[1,5-a]pyrazin-1-yl)-N-(pyridin-2-yl)benzamide. In some embodiments, the invention relates to amorphous solid forms of (S)-4-(8-amino-3-(1-(but-2-ynoyl)pyrrolidin-2-yl)imidazo[1,5-a]pyrazin-1-yl)-N-(pyridin-2-yl)benzamide. In some embodiments, the invention also relates to pharmaceutical compositions containing the solid forms, and methods for treating conditions or disorders by administering to a subject a pharmaceutical composition that includes the forms, including pharmaceutical compositions and methods for overcoming the effects of acid reducing agents.
    Type: Grant
    Filed: April 30, 2020
    Date of Patent: July 13, 2021
    Assignee: Acerta Pharma B.V.
    Inventors: Fritz Blatter, Tim Ingallinera, Tjeerd Barf, Edwin Aret, Cecile Krejsa, Jerry Evarts
  • Patent number: 11059824
    Abstract: The present invention relates to TLR7 agonists according to Formula I and their use in the treatment of diseases such as cancer and infectious disease.
    Type: Grant
    Filed: May 24, 2019
    Date of Patent: July 13, 2021
    Assignee: Primmune Therapeutics, Inc.
    Inventors: Stephen E. Webber, James Richard Appleman
  • Patent number: 11053265
    Abstract: An optically active 2,3-bisphosphinopyrazine derivative represented by the following general formula (1): wherein R1 represents a group selected from a branched alkyl group having 3 or more carbon atoms, an adamantyl group, an optionally substituted cycloalkyl group, and an optionally substituted aryl group; R2 represents a group selected from a branched alkyl group having 3 or more carbon atoms, an adamantyl group, and an optionally substituted cycloalkyl group, provided that when R1 is a tert-butyl group, R1 and R2 are not the same; R3 represents a monovalent substituent; n represents an integer of 0 to 4; and * represents an asymmetric center on a phosphorus atom.
    Type: Grant
    Filed: September 28, 2018
    Date of Patent: July 6, 2021
    Assignees: NIPPON CHEMICAL INDUSTRIAL CO., LTD., NATIONAL UNIVERSITY CORPORATION HOKKAIDO UNIVERSITY
    Inventors: Hajime Ito, Hiroaki Iwamoto, Tsuneo Imamoto, Ken Tamura