Nitrogen Containing Hetero Ring Patents (Class 514/43)
  • Patent number: 10344046
    Abstract: The present invention discloses compounds of formula (I): which exhibit antiviral properties. The present invention further relates to pharmaceutical compositions comprising the aforementioned compounds for administration to a subject in need of anti-HBV treatment. The invention also relates to methods of treating a HBV infection in a subject by administering a pharmaceutical composition comprising the compounds of the present invention.
    Type: Grant
    Filed: March 15, 2018
    Date of Patent: July 9, 2019
    Assignee: Spring Bank Pharmaceuticals, Inc.
    Inventors: Radhakrishnan P. Iyer, Seetharamaiyer Padmanabhan
  • Patent number: 10251903
    Abstract: The present invention is directed to a process for making Nucleoside Phosphoramidate Compounds of formula (I): which are useful for the treatment and prophylaxis of HCV infection. The present invention is also directed to compounds that are useful as synthetic intermediates for making the compounds of formula (I).
    Type: Grant
    Filed: October 20, 2015
    Date of Patent: April 9, 2019
    Assignees: Merck Sharp & Dohme Corp., Idenix Pharmaceuticals LLC
    Inventors: Bryon L. Simmons, Kevin R. Campos, Artis Klapars, Alistair J. Stewart, Benjamin A. Mayes, Peter E. Maligres, Alan Hyde, Steven Mark Silverman, Yong-Li Zhong, Adel M. Moussa, Kenneth Baker, Kara Van Valkenburg
  • Patent number: 10238678
    Abstract: The present invention features a method for the treatment of Hepatitis C in a human in need thereof comprising administering a compound of Formulas (II) or (IIB) described herein or a pharmaceutically acceptable salt thereof in combination with one or more alternative Hepatitis C therapeutic agents.
    Type: Grant
    Filed: July 20, 2015
    Date of Patent: March 26, 2019
    Assignee: GlaxoSmithKline LLC
    Inventors: Jill Walker, Christian Voitenleitner
  • Patent number: 10239912
    Abstract: Compounds that modulate the conversion of AMP to adenosine by 5?-nucleotidase, ecto, and compositions containing the compounds and methods for synthesizing the compounds, are described herein. The use of such compounds and compositions for the treatment and/or prevention of a diverse array of diseases, disorders and conditions, including cancer- and immune-related disorders, that are mediated by 5?-nucleotidase, ecto is also provided.
    Type: Grant
    Filed: January 6, 2017
    Date of Patent: March 26, 2019
    Assignee: ARCUS BIOSCIENCES, INC.
    Inventors: Laurent Pierre Paul Debien, Juan Carlos Jaen, Jaroslaw Kalisiak, Kenneth V. Lawson, Manmohan Reddy Leleti, Erick Allen Lindsey, Dillon Harding Miles, Eric Newcomb, Jay Patrick Powers, Brandon Reid Rosen, Ehesan Ul Sharif
  • Patent number: 10179144
    Abstract: The present disclosure describes various formulations and compositions for improving one's vitality and health. The formulations may be particularly useful for treating or alleviating at least erectile dysfunction, increasing muscle mass, and encouraging saliva and tear production. In one example such a composition may include 1-methylfolate, methylcobalamin, n-acetylcysteine, pterostilbene, and nicotinamide riboside.
    Type: Grant
    Filed: January 10, 2018
    Date of Patent: January 15, 2019
    Inventor: Roger F. Duronio
  • Patent number: 10160750
    Abstract: The present invention provides compounds of Formula (I): or stereoisomers, tautomers, or pharmaceutically acceptable salts thereof, wherein all the variables are as defined herein. These compounds are selective factor XIa inhibitors or dual inhibitors of FXIa and plasma kallikrein. This invention also relates to pharmaceutical compositions comprising these compounds and methods of treating thromboembolic and/or inflammatory disorders using the same.
    Type: Grant
    Filed: June 16, 2016
    Date of Patent: December 25, 2018
    Assignee: Bristol-Myers Squibb Company
    Inventors: Leon M. Smith, II, Donald J. P. Pinto, James R. Corte, William R. Ewing
  • Patent number: 10076534
    Abstract: The inventors have determined, contrary to the prior art and experience, how to successfully use triciribine to treat ovarian cancer by one or a combination of (i) administering triciribine only to patients which according to a diagnostic test described below, exhibit enhanced sensitivity to the drug; (ii) use of a described dosage level that minimizes the toxicity of the drug but yet still exhibits efficacy; or (iii) use of a described dosage regimen that minimizes the toxicity of the drug.
    Type: Grant
    Filed: July 25, 2016
    Date of Patent: September 18, 2018
    Assignee: University of South Florida
    Inventor: Jin Q. Cheng
  • Patent number: 10072262
    Abstract: The present invention relates to new triphosphate-modified oligonucleotides which may act as RIG-I ligands as well as a new method allowing the synthesis and purification in high yield and purity suitable for pharmaceutical applications.
    Type: Grant
    Filed: March 27, 2015
    Date of Patent: September 11, 2018
    Assignee: Rheinische Friedrich-Wilhelms-Universität Bonn
    Inventors: Marion Goldeck, Jasper Van Den Boorn, János Ludwig, Christine Schuberth-Wagner
  • Patent number: 10058507
    Abstract: Compositions which comprise delivery vehicles having stably associated therewith non-antagonistic combinations of two or more agents, such as antineoplastic agents, are useful in achieving non-antagonistic effects when combinations of drugs are administered.
    Type: Grant
    Filed: January 7, 2016
    Date of Patent: August 28, 2018
    Assignee: CELATOR PHARMACEUTICALS, INC.
    Inventors: Paul Tardi, Troy Harasym, Murray Webb, Clifford Shew, Andrew Janoff, Lawrence Mayer, Marcel Bally
  • Patent number: 10047114
    Abstract: The present invention discloses compounds of formula (I): which exhibit antiviral properties. The present invention further relates to pharmaceutical compositions comprising the aforementioned compounds for administration to a subject in need of anti-HBV treatment. The invention also relates to methods of treating a HBV infection in a subject by administering a pharmaceutical composition comprising the compounds of the present invention.
    Type: Grant
    Filed: November 12, 2015
    Date of Patent: August 14, 2018
    Assignee: Spring Bank Pharmaceuticals, Inc.
    Inventors: Radhakrishnan P. Iyer, Seetharamaiyer Padmanabhan
  • Patent number: 9861651
    Abstract: The invention provides a method of preventing or treating hearing loss in a mammal in need thereof. The method involves administering to the mammal an agent that increases intracellular NAD+ in the mammal. The invention also provides a method of determining if a compound acts as a neuroprotective agent.
    Type: Grant
    Filed: July 15, 2013
    Date of Patent: January 9, 2018
    Assignee: CORNELL UNIVERSITY
    Inventors: Kevin Brown, Anthony Sauve, Samie Jaffrey
  • Patent number: 9849116
    Abstract: Pharmaceutical compositions of (R)-pramipexole and one or more secondary therapeutic agents such as, for example, dopamine agonists, dopaminergic agonists, COMT inhibitors, MOA inhibitors, excitatory amino acid antagonists, growth factors, neurotrophic factors, antioxidants, anti-inflammatory agents, immunomodulators, anti-glutamatergics, ion channel blockers, ?-amino-3-hydroxy-5-methyl-4-isoxazolepropionic acid (AMPA) receptor antagonists, heat shock protein inducers/protein disaggregators and downregulators, monoamine oxidase type B (MOAB) inhibitors, multi-target agents, kinase inhibitors, Bcl inducers, histone deacetylase (HDAC) mediators, glial modulators, mitochondrial energy promoting agents, myostatin inhibitors, caspase inhibitors and combinations thereof or those related to mitochondrial dysfunction or increased oxidative stress are disclosed.
    Type: Grant
    Filed: October 8, 2015
    Date of Patent: December 26, 2017
    Assignee: Knopp Biosciences LLC
    Inventors: Michael E. Bozik, Valentin Gribkoff, Thomas Petzinger, Jr.
  • Patent number: 9828408
    Abstract: The invention provides compounds of the formula: wherein B is a nucleobase selected from the groups (a) to (d): and the other variables are as defined in the claims, which are of use in the treatment or prophylaxis of hepatitis C virus infection, and related aspects.
    Type: Grant
    Filed: November 23, 2016
    Date of Patent: November 28, 2017
    Assignee: MEDIVIR AB
    Inventors: Genadiy Kalayanov, Staffan Torssell, Horst Wahling
  • Patent number: 9821173
    Abstract: An anti-cancer agent includes Au(I) purinyl, indolyl, or azaindolyl analogues encapsulated in sterically hindered phosphine ligands.
    Type: Grant
    Filed: February 10, 2014
    Date of Patent: November 21, 2017
    Assignee: Case Western Reserve University
    Inventor: Anthony J. Berdis
  • Patent number: 9815864
    Abstract: Disclosed herein are nucleosides, nucleotides and analogs thereof, pharmaceutical compositions that include one or more of nucleosides, nucleotides and analogs thereof, and methods of synthesizing the same, of the Formula (I). Also disclosed herein are methods of ameliorating and/or treating a disease and/or a condition, including an infection from a norovirus, with a nucleoside, a nucleotide and an analog thereof.
    Type: Grant
    Filed: June 24, 2014
    Date of Patent: November 14, 2017
    Assignee: Alios BioPharma, Inc.
    Inventors: Leonid Beigelman, Jerome Deval, Zhinan Jin
  • Patent number: 9784728
    Abstract: The present invention refers to a fluorescent fusion polypeptide capable of changing its localization within the cell from the cell cytoplasmic membrane to the retention vesicles, upon an increase in the concentration of second messengers within the cell cytoplasm, comprising a membrane localization peptide, a second messenger transduction protein binding peptide, a reticulum retention signal and a fluorescent peptide wherein: a. the membrane localization peptide is located at the N-terminus of the fluorescent fusion polypeptide and is physically bound, optionally through a linker, to the fluorescent peptide, which in turn is physically bound, optionally through a linker, to the second messenger transduction protein binding peptide; and b. the second messenger transduction protein binding peptide is physically bound, optionally through a linker, to the reticulum retention signal, which in turn is located at the C-terminus of the fluorescent fusion polypeptide.
    Type: Grant
    Filed: July 8, 2013
    Date of Patent: October 10, 2017
    Assignee: INNOVATIVE TECHNOLOGIES IN BIOLOGICAL SYSTEMS S.L.
    Inventors: Danel Kortazar Zabala, Aida Clarisa Salado Pogonza, Jorge Gámiz Mata, Meritxell Roura Ferrer, Rosa Mella López, Patricia Villacé Lozano
  • Patent number: 9757596
    Abstract: The present invention relates to a composition comprising at least 3 different diols, wherein said diols have the general structure (CH2)nH2O2, wherein n is the number of CH2 and being between 3 to 10, in a total amount of from about 0.1 to about 50% (v/v), a method for producing the composition and its use, such as in therapy. The composition may be a pharmaceutical, cosmetic, antimicrobial or preservative composition. The composition is useful in inactivating microorganisms or preventing their growth.
    Type: Grant
    Filed: November 29, 2005
    Date of Patent: September 12, 2017
    Assignee: AMBRIA DERMATOLOGY AB
    Inventors: Jan Faergemann, Thomas Hedner
  • Patent number: 9718851
    Abstract: The present invention provides nucleoside phosphoramidate compounds of Formula I, where R1, R2a, R2b, R4, R5a, R5b, Rb5, Rb6 and D are as defined herein. The invention further includes pharmaceutical compositions comprising a compound of Formula I, methods of use of these compounds for treating a viral infection, and methods of producing these compounds.
    Type: Grant
    Filed: November 5, 2015
    Date of Patent: August 1, 2017
    Assignee: Enanta Pharmaceuticals, Inc.
    Inventors: Jay R. Luly, Bin Wang, Guoqiang Wang, Yat Sun Or
  • Patent number: 9670238
    Abstract: The present invention relates to a novel compound represented by formula (1), or salt thereof, wherein R is hydroxy group or hydrogen atom; R1 and R2 are the same or different, and are each independently benzyl group which may have a substituent. The present invention provides therapeutically agents, which have remarkable stability against cytidine deaminase, a metabolic enzyme, can be absorbed in vivo by oral administration and inhibit protein synthesis by being incorporated easily into nucleic acid bio-synthesis in vivo for replacing injection agent (5-azacytidine or 2?-deoxy-5-azacytidine) used in clinic for treating myeloma.
    Type: Grant
    Filed: November 18, 2016
    Date of Patent: June 6, 2017
    Assignee: Ohara Pharmaceutical Co., Ltd.
    Inventors: Magoichi Sako, Xiong Luo
  • Patent number: 9655914
    Abstract: This application relates to combination therapies including triciribine compounds and epidermal growth factor receptor inhibitor compounds, particularly erlotinib-like compounds and compositions with reduced toxicity for the treatment and prevention of tumors, cancer, and other disorders associated with abnormal cell proliferation.
    Type: Grant
    Filed: December 28, 2015
    Date of Patent: May 23, 2017
    Assignee: University of South Florida
    Inventors: Jin Q. Cheng, Said M. Sebti
  • Patent number: 9598457
    Abstract: Disclosed herein are nucleotide analogs, methods of synthesizing nucleotide analogs and methods of treating diseases and/or conditions such as a HCV infection with one or more nucleotide analogs.
    Type: Grant
    Filed: December 19, 2013
    Date of Patent: March 21, 2017
    Assignee: Alios BioPharma, Inc.
    Inventors: David Bernard Smith, Leonid Beigelman, Guangyi Wang, Michael Hunter Welch
  • Patent number: 9556216
    Abstract: The present invention provides a compound of formula A: or a pharmaceutically acceptable salt thereof, wherein B, Q, R1, R5, R6, R7, R8 and Z are as defined herein, which is a 2?-branched nucleoside useful for the treatment or prevention of viral infections, particularly dengue fever, yellow fever, West Nile virus, Japanese encephalitis virus, tick-borne encephalitis virus, Kunjin virus, Murray Valley encephalitis, St Louis encephalitis, Omsk hemorrhagic fever virus, bovine viral diarrhea virus, Zika virus and Hepatitis C virus.
    Type: Grant
    Filed: August 27, 2013
    Date of Patent: January 31, 2017
    Assignee: Novartis AG
    Inventors: Sampath-Kumar Anandan, Virender Singh Aulakh, Martijn Fenaux, Xiaodong Lin, Liang Mao, Oliver Saunders, Zachary Kevin Sweeney, Fumiaki Yokokawa, Weidong Zhong
  • Patent number: 9539274
    Abstract: The present invention provides methods, compositions, formulations, and kits related to acadesine, or a prodrug, analog, or salt thereof, and/or a blood clotting inhibitor for preventing or reducing adverse side effects in a patient. The type of patient that may benefit includes a patient with decreased left ventricular function, a patient with a prior myocardial infarction, a patient undergoing non-vascular surgery, or a fetus during labor and delivery.
    Type: Grant
    Filed: March 27, 2015
    Date of Patent: January 10, 2017
    Assignee: Pericor Therapeutics, Inc.
    Inventor: Dennis T. Mangano
  • Patent number: 9526742
    Abstract: A pharmaceutical composition including at least one epigenome-modifying compound, for a use thereof in the treatment of genetic muscular diseases linked to a conformational disorder of at least one protein, said disorder causing the cellular degradation of the protein.
    Type: Grant
    Filed: July 16, 2013
    Date of Patent: December 27, 2016
    Assignee: GENETHON
    Inventor: Isabelle Richard
  • Patent number: 9518079
    Abstract: The inventors have determined, contrary to the prior art and experience, how to successfully use triciribine to treat tumors and cancer by one or a combination of (i) administering triciribine only to patients which according to a diagnostic test described below, exhibit enhanced sensitivity to the drug; (ii) use of a described dosage level that minimizes the toxicity of the drug but yet still exhibits efficacy; or (iii) use of a described dosage regimen that minimizes the toxicity of the drug.
    Type: Grant
    Filed: July 15, 2015
    Date of Patent: December 13, 2016
    Assignee: University of South Florida
    Inventors: Jin Q. Cheng, Said M. Sebti
  • Patent number: 9498492
    Abstract: This application relates to combination therapies including triciribine and related compounds and taxanes and compositions with reduced toxicity for the treatment and prevention of tumors, cancer, and other disorders associated with abnormal cell proliferation.
    Type: Grant
    Filed: July 1, 2015
    Date of Patent: November 22, 2016
    Assignee: University of South Florida
    Inventors: Jin Q. Cheng, Said M. Sebti
  • Patent number: 9486522
    Abstract: This application relates to combination therapies including triciribine and related compounds and trastuzumab or a salt thereof and compositions with reduced toxicity for the treatment and prevention of tumors, cancer, and other disorders associated with abnormal cell proliferation.
    Type: Grant
    Filed: October 13, 2015
    Date of Patent: November 8, 2016
    Assignee: University of South Florida
    Inventors: Jin Q. Cheng, Said M. Sebti
  • Patent number: 9486492
    Abstract: This application relates to combination therapies including triciribine and related compounds and bortezomib and derivatives thereof analogs and compositions with reduced toxicity for the treatment and prevention of tumors, cancer, and other disorders associated with abnormal cell proliferation.
    Type: Grant
    Filed: October 19, 2015
    Date of Patent: November 8, 2016
    Assignee: University of South Florida
    Inventors: Jin Q. Cheng, Said M. Sebti
  • Patent number: 9486470
    Abstract: This application encompasses combination therapies including triciribine and related compounds and one or more platinum compounds and compositions with reduced toxicity for the treatment and prevention of tumors, cancer, and other disorders associated with abnormal cell proliferation.
    Type: Grant
    Filed: August 21, 2015
    Date of Patent: November 8, 2016
    Assignee: University of South Florida
    Inventors: Jin Q. Cheng, Said M. Sebti
  • Patent number: 9480698
    Abstract: Oligonucleotide analogs are provided that incorporate 5-aza-cytosine in the oligonucleotide sequence, e.g., in the form of 5-aza-2?-deoxycytidine (decitabine) or 5-aza-cytidine. In particular, oligonucleotide analogs rich in decitabine-deoxyguanosine islets (DpG and GpD) are provided to target the CpG islets in the human genome, especially in the promoter regions of genes susceptible to aberrant hypermethylation. Such analogs can be used for modulation of DNA methylation, such as effective inhibition of methylation of cytosine at the C-5 position. Methods for synthesizing these oligonucleotide analogs and for modulating nucleic acid methylation are provided. Also provided are phosphoramidite building blocks for synthesizing the oligonucleotide analogs, methods for synthesizing, formulating and administering these compounds or compositions to treat conditions, such as cancer and hematological disorders.
    Type: Grant
    Filed: December 22, 2015
    Date of Patent: November 1, 2016
    Assignee: ASTEX PHARMACEUTICALS, INC.
    Inventors: Pasit Phiasivongsa, Sanjeev Redkar
  • Patent number: 9447137
    Abstract: In one aspect, the invention relates to substituted gemcitabine aryl amide analogs, derivatives thereof, and related compounds; synthesis methods for making the compounds; pharmaceutical compositions comprising the compounds; and methods of treating viral disorders and disorders of uncontrolled cellular proliferation using the compounds and compositions. This abstract is intended as a scanning tool for purposes of searching in the particular art and is not intended to be limiting of the present invention.
    Type: Grant
    Filed: November 7, 2013
    Date of Patent: September 20, 2016
    Assignee: NUCORION PHARMACEUTICALS, INC.
    Inventor: Zucai Suo
  • Patent number: 9433635
    Abstract: The inventors have determined, contrary to the prior art and experience, how to successfully use triciribine to treat ovarian cancer by one or a combination of (i) administering triciribine only to patients which according to a diagnostic test described below, exhibit enhanced sensitivity to the drug; (ii) use of a described dosage level that minimizes the toxicity of the drug but yet still exhibits efficacy; or (iii) use of a described dosage regimen that minimizes the toxicity of the drug.
    Type: Grant
    Filed: November 6, 2014
    Date of Patent: September 6, 2016
    Assignee: University of South Florida
    Inventor: Jin Q. Cheng
  • Patent number: 9428813
    Abstract: Disclosed herein are methods for detecting, diagnosing and/or prognosing a malignant adrenocortical tumor. Also disclosed are methods of treating a malignant adrenocortical tumor, such as ACC. In some examples, the method of diagnosing and/or prognosing includes obtaining a sample comprising genomic DNA from a subject at risk of acquiring or suspected to have an adrenocortical tumor; isolating genomic DNA from the sample; and measuring the level of one or more methylated genomic CpG dinucleotide sequences in one or more of the adrenocortical genomic targets in the sample, wherein an increase in the level of methylation of the one or more genomic CpG dinucleotide sequences in the sample compared to a control indicates a malignant adrenocortical tumor.
    Type: Grant
    Filed: March 12, 2013
    Date of Patent: August 30, 2016
    Assignee: The United States of America, as Represented by the Secretary, Dept. of Health & Human Services
    Inventors: Electron Kebebew, Nesrin S. Rechache, Paul S. Meltzer, Yong-hong Wang
  • Patent number: 9416154
    Abstract: The present invention relates to 5?-Substituted Nucleoside Derivatives of Formula (I): (I) and pharmaceutically acceptable salts thereof, wherein X, Y, Z, R1, R2 and R3 are as defined herein and B is a 7-deaza-9-purinyl moiety. The present invention also relates to compositions comprising at least one 5?-Substituted Nucleoside Derivative, and methods of using the 5?-Substituted Nucleoside Derivatives for treating or preventing HCV infection in a patient.
    Type: Grant
    Filed: July 10, 2012
    Date of Patent: August 16, 2016
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Vishal A. Verma, Ashok Arasappan, F. George Njoroge, Vinay Girijavallabhan, Stephane L. Bogen, Qun Dang, David B. Olsen
  • Patent number: 9408863
    Abstract: The present invention relates to 5?-Substituted Nucleoside Analogs of Formula (I): and pharmaceutically acceptable salts thereof, wherein B, X, Z, R1, R2, R3 and R3? are as defined herein. The present invention also relates to compositions comprising at least one 5?-Substituted Nucleoside Analog, and methods of using the 5?-Substituted Nucleoside Analogs for treating or preventing HCV infection in a patient.
    Type: Grant
    Filed: July 10, 2012
    Date of Patent: August 9, 2016
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Vishal A. Verma, Ashok Arasappan, F. George Njoroge, Kevin X. Chen
  • Patent number: 9358248
    Abstract: Oligonucleotide analogs are provided that incorporate 5-aza-cytosine in the oligonucleotide sequence, e.g., in the form of 5-aza-2?-deoxycytidine (decitabine) or 5-aza-cytidine. In particular, oligonucleotide analogs rich in decitabine-deoxyguanosine islets (DpG and GpD) are provided to target the CpG islets in the human genome, especially in the promoter regions of genes susceptible to aberrant hypermethylation. Such analogs can be used for modulation of DNA methylation, such as effective inhibition of methylation of cytosine at the C-5 position. Methods for synthesizing these oligonucleotide analogs and for modulating nucleic acid methylation are provided. Also provided are phosphoramidite building blocks for synthesizing the oligonucleotide analogs, methods for synthesizing, formulating and administering these compounds or compositions to treat conditions, such as cancer and hematological disorders.
    Type: Grant
    Filed: May 14, 2013
    Date of Patent: June 7, 2016
    Assignee: ASTEX PHARMACEUTICALS, INC.
    Inventors: Pasit Phiasivongsa, Sanjeev Redkar
  • Patent number: 9321800
    Abstract: The invention provides compounds of formula I, wherein R1, R2 and R3 have values defined in the specification and a pharmaceutically acceptable salt thereof; or an optical isomer thereof; or a mixture of optical isomers, as well as compositions comprising such compounds and therapeutic methods that utilize such compounds and/or compositions.
    Type: Grant
    Filed: April 19, 2010
    Date of Patent: April 26, 2016
    Assignee: Gilead Sciences, Inc.
    Inventors: Aurelie Bourderioux, Michal Hocek, Petr Naus
  • Patent number: 9322049
    Abstract: The invention provides a method of increasing a deacetylated activity of SIRT6 by contacting SIRT6 with an agent that binds SIRT6 and reduces the Km of SIRT6 for a substrate, thereby increasing the deacetylase activity of SIRT6. The invention also provides compounds of the formulas (II) and (III).
    Type: Grant
    Filed: December 14, 2010
    Date of Patent: April 26, 2016
    Assignee: CORNELL UNIVERSITY
    Inventors: Anthony Sauve, Ping Xu
  • Patent number: 9321798
    Abstract: Phosphorodiamidate derivatives of e.g. gemcitabine are provided for use in treating cancer. In one embodiment, the two amidate motifs each comprises NR?R? where R? is H and R? is CR5R6CO2R7, where R6 is H, R5 is the side chain, including H and C1, of a naturally occurring alpha amino acid, and R7 is branched or unbranched, substituted or unsubstituted, acyclic or cyclic alkyl, including t-butyl-CH2-, benzyl and C3 to C6 cycloalkyl. Formula (I).
    Type: Grant
    Filed: October 5, 2011
    Date of Patent: April 26, 2016
    Assignee: NuCana BioMed Limited
    Inventor: Christopher McGuigan
  • Patent number: 9297046
    Abstract: The present invention concerns an in vitro method for diagnosing a myeloid tumor or a lymphoid tumor in a subject, which comprises the step of analyzing a biological sample from said subject by (i) detecting the presence of a mutation in the Ten Eleven Translocation protein family member 2 gene (TET2) coding for the polypeptide having the sequence SEQ ID NO:2, and/or (ii) analyzing the expression of the TET2 gene; wherein the detection of such a TET2 mutation, of the absence of expression of TET2 or of the expression of a truncated TET2 is indicative of a subject developing or predisposed to develop a myeloid tumor or a lymphoid tumor.
    Type: Grant
    Filed: March 21, 2012
    Date of Patent: March 29, 2016
    Assignees: ASSISTANCE PUBLIQUE—HOPITAUX DE PARIS, CENTRE HENRI BECQUEREL, INSTITUT NATIONAL DE LA SANTE ET DE LA RECHERCHE MEDICALE (INSERM), INSTITUT GUSTAVE-ROUSSY, UNIVERSITE PARIS DESCARTES, UNIVERSITE PIERRE ET MARIE CURIE, UNIVERSITE PARIS-SUD 11
    Inventors: Franck Viguie, Olivier Bernard, Michaela Fontenay, Christian Bastard, Francois Delhommeau, William Vainchenker
  • Patent number: 9265783
    Abstract: This application relates to combination therapies including triciribine compounds and epidermal growth factor receptor inhibitor compounds, particularly erlotinib-like compounds and compositions with reduced toxicity for the treatment and prevention of tumors, cancer, and other disorders associated with abnormal cell proliferation.
    Type: Grant
    Filed: November 27, 2013
    Date of Patent: February 23, 2016
    Assignee: University of South Florida
    Inventors: Jin Q. Cheng, Said M. Sebti
  • Patent number: 9260469
    Abstract: The invention is directed to processes for synthesizing bicyclic nucleoside antiviral compounds and for synthesizing the intermediates used in the process. The invention is also directed to novel intermediate compounds useful in the process. The antiviral compounds are useful in the treatment of herpes zoster (i.e., varicella zoster virus, VZV, shingles) and for the prevention of post herpetic neuralgia (PHN) resulting from this viral infection.
    Type: Grant
    Filed: October 7, 2011
    Date of Patent: February 16, 2016
    Assignee: ContraVir Pharmaceuticals, Inc.
    Inventors: Yanling Wang, Yuan Wang, Xungui He, Chuanjun Liu, Jirang Zhu, Jie Li, Qingzhong Cheng, Mingyong Yuan
  • Patent number: 9211299
    Abstract: This application encompasses combination therapies including triciribine and related compounds and one or more platinum compounds and compositions with reduced toxicity for the treatment and prevention of tumors, cancer, and other disorders associated with abnormal cell proliferation.
    Type: Grant
    Filed: November 27, 2013
    Date of Patent: December 15, 2015
    Assignee: University of South Florida
    Inventors: Jin Q. Cheng, Said M. Sebti
  • Patent number: 9192645
    Abstract: This application relates to combination therapies including triciribine and related compounds and bortezomib and derivatives thereof analogs and compositions with reduced toxicity for the treatment and prevention of tumors, cancer, and other disorders associated with abnormal cell proliferation.
    Type: Grant
    Filed: July 1, 2014
    Date of Patent: November 24, 2015
    Assignee: University of South Florida
    Inventors: Jin Q. Cheng, Said M. Sebti
  • Patent number: 9186403
    Abstract: This application relates to combination therapies including triciribine and related compounds and trastuzumab or a salt thereof and compositions with reduced toxicity for the treatment and prevention of tumors, cancer, and other disorders associated with abnormal cell proliferation.
    Type: Grant
    Filed: November 26, 2013
    Date of Patent: November 17, 2015
    Assignee: University of South Florida
    Inventors: Jin Q. Cheng, Said M. Sebti
  • Patent number: 9173892
    Abstract: Acadesine derivatives as a drug, as well as the derivatives for the treatment of cancer and in particular for the treatment of chronic myeloid leukemia are described. Also, product containing the derivatives and at least one second active ingredient as a combination product for simultaneous, separate or sequential administration, in the treatment of cancer, as well as a pharmaceutical composition containing the derivatives and a pharmaceutically acceptable carrier are described. Finally, a method for inhibiting the in vitro cell proliferation including the placement of an in vitro cell in contact with the derivatives and methods for synthesis of said derivatives and methods for synthesis of the derivatives are described.
    Type: Grant
    Filed: April 17, 2012
    Date of Patent: November 3, 2015
    Assignees: Universite Nice Sophia Antipolis, Centre National De La Recherche Scientifique, Institut National De La Sante De La Recherche Medicale
    Inventors: Rachid Benhida, Patrick Auberger, Vincent Malnuit, Mohsine Driowya, Alexandre Puissant, Guillaume Robert
  • Patent number: 9115162
    Abstract: The inventors have determined, contrary to the prior art and experience, how to successfully use triciribine to treat tumors and cancer by one or a combination of (i) administering triciribine only to patients which according to a diagnostic test described below, exhibit enhanced sensitivity to the drug; (ii) use of a described dosage level that minimizes the toxicity of the drug but yet still exhibits efficacy; or (iii) use of a described dosage regimen that minimizes the toxicity of the drug.
    Type: Grant
    Filed: April 17, 2013
    Date of Patent: August 25, 2015
    Assignee: University of South Florida
    Inventors: Jin Q. Cheng, Said M. Sebti
  • Patent number: 9101641
    Abstract: This application relates to combination therapies including triciribine and related compounds and taxanes and compositions with reduced toxicity for the treatment and prevention of tumors, cancer, and other disorders associated with abnormal cell proliferation.
    Type: Grant
    Filed: November 26, 2013
    Date of Patent: August 11, 2015
    Assignee: University of South Florida
    Inventors: Jin Q. Cheng, Said M. Sebti
  • Patent number: 9085599
    Abstract: The present invention relates to 2?-allene-substituted nucleoside derivatives of the general formula (I): As well as pharmaceutical compositions comprising such compounds and methods to treat or prevent an HIV infection, HBV infection, HCV infection or abnormal cellular proliferation, comprising administering said compounds or compositions. In addition, the present invention includes processes for the preparation of such compounds, and the related ?-D and ?-L-nucleoside derivatives.
    Type: Grant
    Filed: March 16, 2012
    Date of Patent: July 21, 2015
    Assignee: Enanta Pharmaceuticals, Inc.
    Inventors: Yat Sun Or, Jun Ma, Guoqiang Wang, In Jong Kim, Jiang Long, Yao-Ling Qiu
  • Patent number: 9040501
    Abstract: Provided herein are compounds used to inhibit the deamination enzyme responsible for the inactivation of therapeutic compounds, and methods of using them.
    Type: Grant
    Filed: November 14, 2013
    Date of Patent: May 26, 2015
    Assignee: Otsuka Pharmaceutical Co., Ltd.
    Inventors: Sergel Belyakov, Bridget Duvall, Dana Ferraris, Gregory Hamilton, Mark Vaal