Patents Examined by Jeffrey H Murray
  • Broad spectrum antiviral compounds
    Patent number: 10919922
    Abstract: Antiviral compounds comprising prodrugs with differing side chains derived from a tyrosine substance in the form of a tyrosine amide in which the amide substituent side chain is an alkyl ether, thioether, or alkene. Embodiments of the compounds have a range of effective lipophilicity values allowing variation in aqueous solubility, oral bioavailability, cell permeability and in vivo activation properties. The embodiments have promoieties derived from a single amino acid, which are expected to have low toxicity. The features described above also make possible a novel “precision medicine” approach to treatment of viral infections, whereby the prodrug variations can be exploited to match optimal activation of the prodrug to a given patient or strain of virus.
    Type: Grant
    Filed: October 31, 2017
    Date of Patent: February 16, 2021
    Assignee: University of Southern California
    Inventors: Charles E. McKenna, Boris A. Kashemirov, Jaijun Fan, Jinglei Lyu
  • Diketopiperazine salts for drug delivery and related methods
    Patent number: 10912821
    Abstract: Drug delivery systems have been developed based on the formation of diketopiperazine carboxylate salts and microparticles containing the same. The systems may further comprise a bioactive agent. Related methods for making and using the biologically active agent delivery compositions are also provided. In certain embodiments, the pharmaceutically acceptable salts described can be formed by removal of solvent by methods including distillation, evaporation, spray drying or lyophilization.
    Type: Grant
    Filed: January 27, 2020
    Date of Patent: February 9, 2021
    Assignee: MannKind Corporation
    Inventors: Andrea Leone-Bay, Destardi Moye-Sherman, Bryan R. Wilson
  • Certain chemical entities, compositions, and methods
    Patent number: 10912784
    Abstract: Chemical entities that are bufalin derivatives, pharmaceutical compositions and methods of treatment of cancer are described.
    Type: Grant
    Filed: September 26, 2019
    Date of Patent: February 9, 2021
    Assignee: SUZHOU NEUPHARMA CO., LTD.
    Inventor: Xiangping Qian
  • Thienopyrimidinones as ubiquitin-specific protease 7 inhibitors
    Patent number: 10906916
    Abstract: The disclosure relates to inhibitors of USP7 inhibitors useful in the treatment of cancers, neurodegenerative diseases, immunological disorders, inflammatory disorders, cardiovascular diseases, ischemic diseases, viral infections and diseases, and bacterial infections and diseases, having the Formula: where R1, R2, R3, R5, R5?, X1, X2, n, and m are described herein.
    Type: Grant
    Filed: July 18, 2019
    Date of Patent: February 2, 2021
    Assignee: Valo Early Discovery, Inc.
    Inventors: Stephanos Ioannidis, Adam Charles Talbot, Bruce Follows, Alexandre Joseph Buckmelter, Minghua Wang, Ann-Marie Campbell, David R. Lancia, Jr.
  • Fused heteroaryl pyridyl and phenyl benzenesuflonamides as CCR2 modulators for the treatment of inflammation
    Patent number: 10899765
    Abstract: Compounds are provided that act as potent antagonists of the CCR2 receptor. The compounds are generally aryl sulfonamide derivatives and are useful in pharmaceutical compositions, methods for the treatment of CCR2-mediated diseases and as controls in assays for the identification of CCR2 antagonists.
    Type: Grant
    Filed: January 11, 2019
    Date of Patent: January 26, 2021
    Assignee: ChemoCentryx, Inc.
    Inventors: Antoni Krasinski, Sreenivas Punna, Solomon Ungashe, Qiang Wang, Yibin Zeng
  • Crystalline form of compound suppressing protein kinase activity, and application thereof
    Patent number: 10899744
    Abstract: Provided are a compound as represented by structural formula (I) ({5-[(1R)-1-(2,6-dichloro-3-fluorophenyl)ethoxy]-6-aminopyridazin-3-yl}-N-{4-[((3S,5R)-3,5-di methylpiperazinyl)carbonyl]phenyl}carboxamide hydrochloride) and a novel crystalline form of a hydrate or solvate of the compound. Further provided are a manufacturing method of the compound and crystalline form, a related intermediate, a pharmaceutical composition comprising the compound, an application using the compound or the crystalline form for preparing a pharmaceutical product for treating a disease, symptom, or disorder, and a therapeutic method for treating a disease, symptom, or disorder.
    Type: Grant
    Filed: June 1, 2017
    Date of Patent: January 26, 2021
    Assignee: XCOVERY HOLDINGS, INC.
    Inventors: Congxin Liang, Yongbin Ma, Wei He
  • Pyrazine compounds and uses thereof
    Patent number: 10898481
    Abstract: The present disclosure novel pyrazine compounds targeting adenosine receptors (especially A1 and A2, particularly A2a). The present disclosure also relates to pharmaceutical compositions comprising one or more of the compounds as an active ingredient, and use of the compounds in the treatment of adenosine receptor (AR) associated diseases, for example cancer such as NSCLC, RCC, prostate cancer, and breast cancer.
    Type: Grant
    Filed: June 24, 2020
    Date of Patent: January 26, 2021
    Inventors: Changhe Qi, Honchung Tsui, Qingbei Zeng, Zhenfan Yang, Xiaolin Zhang
  • 4-methyldihydropyrimidinone compounds and pharmaceutical use thereof
    Patent number: 10899717
    Abstract: The present invention relates to 4-methyldihydropyrimidinone compounds, or pharmaceutically acceptable salts thereof, having ROR? antagonist activity, pharmaceutical compositions comprising the same, and pharmaceutical use thereof. A compound of Formula (1) or (2) or a pharmaceutically acceptable salt thereof, a pharmaceutical composition comprising the same, and pharmaceutical use thereof are provided.
    Type: Grant
    Filed: February 27, 2019
    Date of Patent: January 26, 2021
    Assignee: JAPAN TOBACCO INC.
    Inventors: Takayuki Sakai, Taku Ikenogami
  • Pyrrolo[1,2-B]pyridazine derivatives
    Patent number: 10875866
    Abstract: A compound of Formula (I): pharmaceutically acceptable salts thereof, deuterated analogs thereof, compositions thereof, and methods of treating disease using a compound thereof, wherein the variable substituents are disclosed herein.
    Type: Grant
    Filed: July 11, 2019
    Date of Patent: December 29, 2020
    Assignee: Gilead Sciences, Inc.
    Inventors: Stephen Ammann, Elizabeth M. Bacon, Gediminas Brizgys, Elbert Chin, Chienhung Chou, Jeromy J. Cottell, Marilyn Ndukwe, James G. Taylor, Nathan E. Wright, Zheng-Yu Yang, Sheila M. Zipfel
  • Triazolo[4,5-d] pyramidine derivatives and their use as purine receptor antagonists
    Patent number: 10875868
    Abstract: Compounds of formula (I) that are capable of acting as purine receptor antagonists, pharmaceutical compositions including the compounds, and methods of making the compounds, are. disclosed. The compounds and compositions can be used in treating or preventing disorders related to purine receptor hyperfunctioning.
    Type: Grant
    Filed: December 2, 2019
    Date of Patent: December 29, 2020
    Assignee: VERNALIS (R&D) LIMITED
    Inventors: Samantha Jane Bamford, Roger John Gillespie, Richard Simon Todd
  • Triazolo-pyrimidine compounds and uses thereof
    Patent number: 10858365
    Abstract: The present disclosure relates to novel triazolo-pyrimidine compounds targeting adenosine receptors (especially A1 and A2, particularly A2a). The present disclosure also relates to pharmaceutical compositions comprising one or more of the compounds as an active ingredient, and use of the compounds in the treatment of adenosine receptor (AR) associated diseases, for example cancer such as NSCLC, RCC, prostate cancer, and breast cancer.
    Type: Grant
    Filed: June 24, 2020
    Date of Patent: December 8, 2020
    Inventors: Qingbei Zeng, Changhe Qi, Honchung Tsui, Zhenfan Yang, Xiaolin Zhang
  • Processes for the preparation of pyrimidinylcyclopentane compounds
    Patent number: 10858324
    Abstract: The present invention relates to a process for the preparation of a compound of formula (I) wherein R1 is as defined herein, which is useful as an intermediate in the preparation of active pharmaceutical compounds.
    Type: Grant
    Filed: August 29, 2019
    Date of Patent: December 8, 2020
    Assignee: GENENTECH, INC.
    Inventors: Hans Iding, Reinhard Reents, Michelangelo Scalone, Francis Gosselin
  • Bicyclic amines as novel JAK kinase inhibitors
    Patent number: 10851116
    Abstract: The present invention relates to a compound according to formula I wherein R1 is alkyl; n is 1 or 2; R2 is selected from the group consisting of hydrogen, cyano, —SO2Ra, —SO2NRbRc, —C(O)Rb, phenyl and 5- and 6-membered heteroaryl or pharmaceutically acceptable salts, hydrates, or solvates thereof. The invention relates further to pharmaceutical compositions comprising said compounds, and to methods of treating proliferative or inflammatory skin disorders with said compounds.
    Type: Grant
    Filed: January 19, 2018
    Date of Patent: December 1, 2020
    Assignee: LEO Pharma A/S
    Inventors: Daniel Rodriguez Greve, Tue Heesgaard Jepsen, Mogens Larsen, Andreas Ritzen
  • Compositions and methods of using the same for treatment of neurodegenerative and mitochondrial disease
    Patent number: 10851109
    Abstract: The disclosure is directed to compounds and pharmaceutically acceptable salts thereof for the treatment and/or prevention of neurodegenerative and/or mitochondrial diseases, such as Parkinson's disease and Leigh's disease. The compounds and pharmaceutically acceptable salts thereof are of the class of nitrogenous bases, for example, pyrimidines, purines, pteridines, and pharmaceutically acceptable salts thereof.
    Type: Grant
    Filed: November 15, 2018
    Date of Patent: December 1, 2020
    Assignee: Mitokinin LLC
    Inventors: Daniel de Roulet, Robert Devita
  • Compounds for treating spinal muscular atrophy
    Patent number: 10851101
    Abstract: Provided herein are compounds of Formula (I): and forms thereof, including compositions thereof and uses therewith for treating spinal muscular atrophy.
    Type: Grant
    Filed: August 15, 2019
    Date of Patent: December 1, 2020
    Assignees: PTC Therapeutics, Inc., F. Hoffman-La Roche AG
    Inventors: Hongyan Qi, Soongyu Choi, Amal Dakka, Gary Mitchell Karp, Jana Narasimhan, Nikolai Naryshkin, Anthony A. Turpoff, Marla L. Weetall, Ellen Welch, Matthew G. Woll, Tianle Yang, Nanjing Zhang, Xiaoyan Zhang, Xin Zhao, Luke Green, Emmanuel Pinard, Hasane Ratni
  • Heterocyclic inhibitors of monocarboxylate transporters
    Patent number: 10851113
    Abstract: The invention provides heterocyclic compounds of formula A, B, and C as described herein that inhibit monocarboxylate transporters, such as MCT1 and MCT4. Compounds of the invention can be used for treatment of a condition in a patient, wherein the condition is characterized by the heightened activity or by the high prevalence of MCT1 and/or MCT4, such as cancer or type II diabetes.
    Type: Grant
    Filed: June 13, 2019
    Date of Patent: December 1, 2020
    Assignee: THE SCRIPPS RESEARCH INSTITUTE
    Inventors: Thomas D. Bannister, William R. Roush, Jun Yong Choi, Reji Nair, Andy S. Tsai, Jitendra K. Mishra, John L. Cleveland
  • Benzopyrazole compounds and analogues thereof
    Patent number: 10849883
    Abstract: Disclosed are compounds of formula I, and pharmaceutically acceptable salts thereof. The compounds are inhibitors of the complement system. Also provided are pharmaceutical compositions comprising a compound of formula I, and methods involving use of the compounds and compositions in the treatment and prevention of diseases and conditions characterized by aberrant complement system activity.
    Type: Grant
    Filed: February 1, 2017
    Date of Patent: December 1, 2020
    Assignee: BioCryst Pharmaceuticals, Inc.
    Inventors: Pravin L. Kotian, Yarlagadda S. Babu, Weihe Zhang, Lakshminarayana Vogeti, Minwan Wu, Venkat R. Chintareddy, Krishnan Raman
  • Bicyclic and tricyclic pyrimidine tyrosine kinase inhibitors with antitubulin activity and methods of treating a patient
    Patent number: 10844075
    Abstract: Bicyclic and tricyclic pyrimidine tyrosine kinase inhibitors with antitubulin activity are provided in the present invention. The compositions of the present invention possess dual activity in a single agent of potent vascular endothelial growth factor receptor inhibitory activity as well as antitubulin activity. Water soluble salts of these compositions are also described. Methods of treating a patient having cancer, macular degeneration, and arthritis with the compositions and salts thereof of the present invention are disclosed.
    Type: Grant
    Filed: July 2, 2019
    Date of Patent: November 24, 2020
    Assignee: Duquesne University of the Holy Spirit
    Inventor: Aleem Gangjee
  • Thiazole derivatives useful as mutant IDH1 inhibitors for treating cancer
    Patent number: 10836759
    Abstract: A compound of Formula II or a pharmaceutically acceptable salt thereof, wherein CyN is a cyclic amine group bound via a nitrogen atom; X is C or N; R1 and R2 are each independently a halogen, CN, CF3, CHF2, CH2F, a C1-C10alkyl group, a C1-C10alkoxy group, a di(C1-C5alkyl)amino; m and n are each independently 1, 2, or 3, and represents either a single bond or a double bond, wherein the racemic mixture of 3-(4-(4-chlorophenyl)thiazol-2-yl)-1-(2-ethyl-5-methoxyphenyl)-6-(2-methylprop-1-en-1-yl)-5-(piperazine-1-carbonyl)pyridin-2(1H)-one atropisomers is excluded.
    Type: Grant
    Filed: June 21, 2017
    Date of Patent: November 17, 2020
    Assignees: THE UNIVERSITY OF NORTH CAROLINA AT CHAPEL HILL, THE UNITED STATES OF AMERICA, AS REPRESENTED BY THE SECRETARY, DEPARTMENT OF HEALTH AND HUMAN SERVICES
    Inventors: Matthew Brian Boxer, Xiaodong Wang, Kyle Ryan Brimacombe, Mindy Irene Emily Davis, Yuhong Fang, Matthew Hall, Ajit Jadhav, Surendra Karavadhi, Li Liu, Natalia Martinez, Andrew Louis McIver, Rajan Pragani, Jason Matthew Rohde, Anton Simeonov, Wei Zhao, Min Shen
  • Tetracyclic heterocycle compounds useful as HIV integrase inhibitors
    Patent number: 10829499
    Abstract: The present invention relates to Tetracyclic Heterocycle Compounds of Formula and pharmaceutically acceptable salts or prodrug thereof, wherein A, X, R1, R2, R3 and R7 are as defined herein. The present invention also relates to compositions comprising at least one Tetracyclic Heterocycle Compound, and methods of using the Tetracyclic Heterocycle Compounds for treating or preventing HIV infection in a subject.
    Type: Grant
    Filed: June 20, 2019
    Date of Patent: November 10, 2020
    Assignee: MERCK SHARP & DOHME CORP.
    Inventors: Thomas H. Graham, Tao Yu, Yonglian Zhang, John A. McCauley