Patents Examined by Lawrence E. Crane
  • Patent number: 10744149
    Abstract: A method for reducing or maintaining platelet inhibition in a patient by administering cangrelor prior to an invasive procedure is described. The method of this invention can be used for patients in need of antiplatelet therapy or at risk of thrombosis. The method can further be used in patients who were previously treated with long-acting platelet inhibitors without increasing the risk of excessive bleeding.
    Type: Grant
    Filed: March 18, 2019
    Date of Patent: August 18, 2020
    Assignee: Chiesi Farmaceutici S.p.A.
    Inventors: Lisa Ruderman Chen, Simona Skerjanec, Dawn Bell, Jayne Prats, Meredith Todd
  • Patent number: 10745435
    Abstract: The invention relates to deoxynucleotide prodrugs and pharmaceutical preparations thereof. The deoxynucleotide prodrugs include, but are not limited to, The invention further relates to methods of treatment of a mitochondrial DNA (mtDNA) depletion syndrome (MDS) by administering a therapeutically-effective amount of a deoxynucleotide prodrug of the present invention.
    Type: Grant
    Filed: November 16, 2016
    Date of Patent: August 18, 2020
    Assignee: CERECOR, INC.
    Inventors: Stephen B. Thomas, Patrick J. Crutcher
  • Patent number: 10730904
    Abstract: In this method, an oligonucleotide represented by formula (II) [wherein Y1, Q, Base, r and r? are each as defined in claim 1] is prepared by using, as a synthesis unit, a novel nucleoside monomer compound represented by formula (I) [wherein X, R1, Y, Base, Z, Ar, R2, R3 and n are each as defined in claim 1]. The novel nucleoside monomer compound is a nucleoside, the base moiety of which is substituted with an aromatic-hydrocarbon-ring-carbonyl or -thiocarbonyl group having at least one hydrophobic group. The method can dispense with column-chromatographic purification in every reaction, and enables base elongation not only in the 3?-direction but also in the 5?-direction, thus attaining efficient liquid-phase mass synthesis of an oligonucleotide.
    Type: Grant
    Filed: January 4, 2019
    Date of Patent: August 4, 2020
    Inventors: Mitsuru Nonogawa, Toshiaki Nagata, Hideki Saito, Tsuneo Yasuma
  • Patent number: 10723755
    Abstract: Compositions and compounds of nucleoside phosphoramidites and modified oligonucleotides, each comprising one or more charge-neutralizing moieties according to the formula V wherein represents the point of attachment to the nucleoside phosphoramidite or the oligonucleotide, optionally through a spacer group. The nucleoside phosphoramidites permit facile attachment of the neutralizing moieties on the backbones of the modified oligonucleotides. The modified oligonucleotides can be used as therapeutic agents (i.e., oligotherapeutics) for the treatment of cancer, autoimmune disorders, genetic diseases, infectious diseases, neurological diseases, inflammatory diseases, metabolic diseases and others.
    Type: Grant
    Filed: November 18, 2015
    Date of Patent: July 28, 2020
    Inventors: David R. Tabatadze, Ivan Yanachkov
  • Patent number: 10717759
    Abstract: Provided herein is a method for synthesizing polynucleic acids, comprising the steps of (a) providing an acidic solution substantially free of nucleic acid polymerase and lipids, but containing mononucleotides and a monovalent salt; (b) drying and resolubilizing the mixture of step (a) a plurality of times; and (c) recovering polynucleic acids from a resolubilized mixture of step (b). In certain aspects, the method further uses a low pH, e.g. about 3; it can utilize monophosphates, such as AMP rather than ATP; and it can be used with a polynucleotide template to form a sequence at least partially complementary to said template. Thus, both single-stranded and double-stranded polynucleic acids are provided. Ammonia salts have been used to obtain RNA lengths from 10 to 300 nucleotides after 16 half hour cycles and an effective temperature includes between 80° C. and 100° C.
    Type: Grant
    Filed: March 20, 2019
    Date of Patent: July 21, 2020
    Assignees: The Regents of the University of California, Sorbonne Universite
    Inventors: David W. Deamer, Marie-Christine Maurel, Laura Da Silva
  • Patent number: 10689413
    Abstract: Provided is a preparation method of a composition enriched in compound Sp-1. The method performs isomer separation on a reaction product from the first step, and then performs a two-step chemical synthesis, so as to prepare a composition comprising high-purity compound Sp-1, wherein the HPLC purity of the single isomer Sp-1 is 90% or more. Provided is a composition enriched in compound Sp-1. The composition has an inhibitory effect on tumor cell proliferation in vitro significantly higher than that of NUC-1031 and compound Rp-1. Also provided are the use of the composition, and a pharmaceutical composition comprising the composition and at least one pharmaceutically acceptable excipient.
    Type: Grant
    Filed: September 13, 2016
    Date of Patent: June 23, 2020
    Assignee: BrightGene Bio-Medical Technology Co., Ltd.
    Inventors: Jiandong Yuan, Yangqing Huang, Linfeng Miao, Jianing Gu, Chaohua Liang, Zhengye Wang, Zhanli Sun
  • Patent number: 10683321
    Abstract: Provided herein are compounds, compositions and methods for the treatment of Flaviviridae infections, including HCV infections. In certain embodiments, compounds and compositions of nucleoside derivatives are disclosed, which can be administered either alone or in combination with other anti-viral agents. In certain embodiments, the compounds are 4?-OR nucleosides of Formula I: or a pharmaceutically acceptable salt thereof, wherein Base, PD, R, Z1, Z2, Z3, and Z4 are as defined herein.
    Type: Grant
    Filed: December 17, 2014
    Date of Patent: June 16, 2020
    Assignee: Idenix Pharmaceuticals LLC
    Inventors: David Dukhan, Cyril B. Dousson, Adel M. Moussa, Benjamin Alexander Mayes, Alistair James Stewart
  • Patent number: 10682368
    Abstract: Provided are methods of treating feline Coronavirus infections using carbanucleoside compounds having a 1?-(4-aminopyrrolo[2,1-f][1,2,4]triazin-7-yl) substituent, or a pharmaceutically acceptable salt thereof. An exemplary compound is (2R,3R,4S,5R)-2-(4-aminopyrrolo[2,1-f][1,2,4]triazin-7-yl)-3,4-dihydroxy-5-(hydroxymethyl)tetrahydrofuran-2-carbonitrile.
    Type: Grant
    Filed: March 13, 2018
    Date of Patent: June 16, 2020
    Inventors: Michel Joseph Perron, Niels C. Pedersen
  • Patent number: 10676738
    Abstract: The present disclosure provides double stranded nucleic acid comprising first and second oligonucleotides wherein the second oligonucleotide is complementary to the first oligonucleotide. At least one of the first and second oligonucleotides comprises a 5? modified nucleoside or 5? modified nucleotide having Formula IIb: wherein Bx is a heterocyclic base moiety, T2 is an internucleoside linking group linked to one of the oligonucleotides, and each of q1 to q7 are selected from a list of substituents. In certain embodiments, T2 is a phosphodiester or phosphorothioate linkage and formula IIb is a 5?-nucleotide. In certain embodiments, T2 is a non-phosphate linkage and formula IIb is a 5?-nucleoside. In certain embodiments, the present double stranded nucleic acid provides oligonucleotides that are expected to hybridize to a portion of a target RNA resulting in loss of normal function of the target RNA.
    Type: Grant
    Filed: July 28, 2015
    Date of Patent: June 9, 2020
    Assignee: Ionis Pharmaceuticals, Inc.
    Inventors: Thazha P. Prakash, Punit P. Seth, Eric E. Swayze
  • Patent number: 10669301
    Abstract: Methods of preparing synthetic oligonucleotides containing at least one phosphotriester linkage conjugated to a monosaccharide are disclosed, where the synthetic oligonucleotides are prepared from nucleosidic phosphoramidite building blocks, preferably followed by removal of protecting groups to provide monosaccharide-conjugated oligonucleotides.
    Type: Grant
    Filed: August 30, 2018
    Date of Patent: June 2, 2020
    Assignee: AM CHEMICALS LLC
    Inventors: Andrei Pavel Guzaev, Vladimir Y. Vvedenskiy
  • Patent number: 10669300
    Abstract: Disclosed are methods of separating the diastereoisomers of gemcitabine-[phenyl-(benzoxy-L-alaninyl)]-phosphate (NUC-1031), or salts thereof, using crystallisation. In particular, crystallisation from isopropyl alcohol provides gemcitabine-[phenyl-(benzoxy-L-alaninyl)]-(S)-phosphate in high diastereoisomeric purity: Also disclosed is a crystalline form of gemcitabine-[phenyl-(benzoxy-L-alaninyl)]-(S)-phosphate.
    Type: Grant
    Filed: September 29, 2015
    Date of Patent: June 2, 2020
    Assignee: NuCana plc
    Inventor: Hugh Griffith
  • Patent number: 10660912
    Abstract: Disclosed is a combination of gemcitabine-[phenyl-benzoxy-L-alaninyl)]-phosphate (chemical name: 2?-Deoxy-2?,2?-difluoro-D-cytidine-5?-O-[phenyl (benzoxy-L-alaninyl)]phosphate) (NUC-1031) and a platinum-based anticancer agent selected from carboplatin, dicycloplatin, oxaliplatin, satraplatin and nedaplatin. The combinations are useful in the treatment of cancer and particularly ovarian cancer.
    Type: Grant
    Filed: October 5, 2015
    Date of Patent: May 26, 2020
    Assignee: NuCana plc
    Inventor: Hugh Griffith
  • Patent number: 10653774
    Abstract: The present invention provides highly active cyclic-di-nucleotide (CDN) immune stimulators that activate DCs via a recently discovered cytoplasmic receptor known as STING (Stimulator of Interferon Genes). In particular, the CDNs of the present invention are provided in the form of a composition comprising one or more cyclic purine dinucleotides induce STING-dependent type I interferon production, wherein the cyclic purine dinucleotides present in the composition are substantially pure 2?,5?,2?,5? and 2?,5?,3?,5? CDNs, and preferably Rp,Rp stereoisomers thereof.
    Type: Grant
    Filed: July 31, 2017
    Date of Patent: May 19, 2020
    Inventors: Thomas W. Dubensky, Jr., David B. Kanne, Meredith Lai Ling Leong, Edward Emile Lemmens, Laura H. Glickman, Russell E. Vance
  • Patent number: 10654884
    Abstract: Provided are novel purine nucleoside/nucleotide analogues compounds, pharmaceutically acceptable salts thereof, and pharmaceutical compositions thereof, which are inhibitors of CD73 and are useful in the treatment of cancer.
    Type: Grant
    Filed: April 23, 2015
    Date of Patent: May 19, 2020
    Assignee: Boehringer Ingelheim International GmbH
    Inventors: Salvacion Cacatian, David A. Claremon, Lanqi Jia, Angel Morales-Ramos, Suresh B. Singh, Shankar Venkatraman, Zhenrong Xu, Yajun Zheng
  • Patent number: 10653710
    Abstract: Provided are methods and compositions for treating hematological malignancies in patients carrying an IDH1 mutation using a combination of an inhibitor of mutant IDH1 enzyme, (S)-N-((S)-1-(2-chlorophenyl)-2-((3,3-difluorocyclobutyl)amino)-2-oxoethyl)-1-(4-cyanopyridin-2-yl)-N-(5-fluoropyridin-3-yl)-5-oxopyrrolidine-2-carboxamide, or a pharmaceutically acceptable salt thereof (COMPOUND 2) and a DNA demethylating agent.
    Type: Grant
    Filed: October 14, 2016
    Date of Patent: May 19, 2020
    Assignees: Agios Pharmaceuticals, Inc., Celgene Corporation
    Inventors: Samuel V. Agresta, Krishnan Viswanadhan, Jorge DiMartino, Vivek Saroj Kumar Chopra, Kyle J. MacBeth, Robert Douglas Knight, Laurie Kenvin, Qiang Xu
  • Patent number: 10654882
    Abstract: The present invention provides a nicotinamide mononucleotide derivative, or salt thereof, which is a compound represented by general formula (1), wherein R1 and R2 respectively and independently represent a hydrogen atom or acyl group having 3 to 30 carbon atoms, the hydrocarbon group bound to the carbonyl carbon of the acyl group is a linear or branched, saturated or unsaturated hydrocarbon group, and at least one of R1 and R2 is the acyl group.
    Type: Grant
    Filed: November 16, 2016
    Date of Patent: May 19, 2020
    Assignee: SHOWA DENKO K.K.
    Inventor: Daisuke Yagyu
  • Patent number: 10653711
    Abstract: Embodiments of the present invention relate to 6-6 bicyclic aromatic ring substituted nucleoside analogues, including, for example, the following compound: Embodiments of the present invention also relate to uses of the disclosed compounds for the inhibition of protein arginine methyltransferase 5 (PRMT5).
    Type: Grant
    Filed: August 25, 2016
    Date of Patent: May 19, 2020
    Assignee: Janssen Pharmaceutica NV
    Inventors: Tongfei Wu, Dirk Brehmer, Lijs Beke, An Boeckx, Gaston Stanislas Marcella Diels, Ronaldus Arnodus Hendrika Joseph Gilissen, Edward Charles Lawson, Vineet Pande, Marcus Cornelis Bernardus Catharina Paradé, Wim Bert Griet Schepens, Johannes Wilhelmus John F. Thuring, Marcel Viellevoye, Weimei Sun, Lieven Meerpoel
  • Patent number: 10646503
    Abstract: The present disclosure provides pharmaceutical compositions comprising cytidine analogs for oral administration, wherein the compositions release the cytidine analog substantially in the stomach. Also provided are methods of treating diseases and disorders using the oral formulations provided herein.
    Type: Grant
    Filed: September 25, 2019
    Date of Patent: May 12, 2020
    Assignee: Celgene Corporation
    Inventors: John F. Traverse, William W. Leong, Jeffrey B. Etter, Mei Lai, Jay Thomas Backstrom
  • Patent number: 10590410
    Abstract: Methods for processing polynucleotide-containing biological samples, and materials for capturing polynucleotide molecules such as RNA and/or DNA from such samples are provided. The RNA and/or DNA is captured by polyamindoamine (PAMAM (Generation 0)) bound to a surface, such as the surface of magnetic particles. The methods and materials have high efficiency of binding RNA and of DNA, and of release, and thereby permit quantitative determinations. The binding particles can be coated with PAMAM (Generation 0) dendrimer which is amide-bonded to the binding particles, wherein at least a portion of the nucleic acids in the biological sample become reversibly bonded to the binding particles.
    Type: Grant
    Filed: October 12, 2018
    Date of Patent: March 17, 2020
    Assignee: HANDYLAB, INC.
    Inventors: Sundaresh N. Brahmasandra, Elizabeth Craig
  • Patent number: 10590160
    Abstract: The invention provides a process for the preparation of nicotinamide mononucleotide having formula (I): The method involves the protection of nicotinamide riboside by ketalization, followed by phosphorylation and then deprotection to provide nicotinamide mononucleotide.
    Type: Grant
    Filed: March 24, 2016
    Date of Patent: March 17, 2020
    Inventors: Anthony Sauve, Farheen Sultana Mohammad