N-glycosides Wherein The N Is Part Of An N-hetero Ring Which Hetero Ring Is Part Of A Polycyclo Ring System Containing An N-hetero Ring And An Additional Hetero Ring (e.g., Rebeccamycin, Etc.) Patents (Class 536/27.1)
  • Patent number: 10953029
    Abstract: The present invention is directed to 4?-substituted nucleoside derivatives of Formula (I) and their use in the inhibition of HIV reverse transcriptase, the prophylaxis of infection by HIV, the treatment of infection by HIV, and the prophylaxis, treatment, and delay in the onset or progression of AIDS and/or ARC. The present invention also provides processes for the preparation of 4?-substituted nucleoside derivatives of Formula (I) and derivatives thereof.
    Type: Grant
    Filed: September 19, 2016
    Date of Patent: March 23, 2021
    Assignee: Merck Sharp & Dohme Corp.
    Inventor: Vinay M. Girijavallabhan
  • Patent number: 9677123
    Abstract: The present invention relates to novel degenerate nucleobase analogs and degenerate nucleobase oligomers derived therefrom, and methods of using such degenerate nucleobase oligomers.
    Type: Grant
    Filed: March 7, 2007
    Date of Patent: June 13, 2017
    Assignee: Siemens Healthcare Diagnostics Inc.
    Inventor: Thomas R. Battersby
  • Patent number: 9522159
    Abstract: Methods and devices are disclosed for treating or preventing infections in a subject due to Pseudomonas aeruginosa using coformycin analogs and inhibitors of Pseudomonas aeruginosa 5?-methylthioadenosine deaminase (MTADA).
    Type: Grant
    Filed: September 10, 2013
    Date of Patent: December 20, 2016
    Assignees: Albert Einstein College of Medicine, Inc., Victoria Link Limited
    Inventors: Vern L. Schramm, Peter Charles Tyler, Richard Fröhlich
  • Patent number: 9457039
    Abstract: 2?-disubstituted substituted nucleoside derivatives of formula (I) and pharmaceutically acceptable salts thereof are disclosed: (1), wherein A is N3 or NH2 and X, Y, R1, R2, R3, R4, R5 and R18 are as defined herein. Compositions comprising at least one 2?-disubstituted nucleoside derivative, and methods of using the 2?-disubstituted nucleoside derivatives for treating or preventing HCV infection in a patient are disclosed.
    Type: Grant
    Filed: October 11, 2013
    Date of Patent: October 4, 2016
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Vinay Girijavallabhan, Stephane Bogen, Weidong Pan, Qun Dang, Ian Davies
  • Patent number: 9329179
    Abstract: The invention provides devices and methods for surface patterning the substrate of a microfluidic device, and for detection and analysis of interactions between molecules by mechanically trapping a molecular complex while substantially expelling solvent and unbound solute molecules. Examples of molecular complexes include protein-protein complexes and protein-nucleic acid complexes.
    Type: Grant
    Filed: October 6, 2011
    Date of Patent: May 3, 2016
    Assignee: California Institute of Technology
    Inventors: Stephen R. Quake, Sebastian J. Maerkl
  • Patent number: 9242988
    Abstract: Compounds of Formula (I) are disclosed, wherein R1, R2, R3, R4, R5, and R18 are defined herein. The compounds encompassed by Formula (I) include compounds which are HCV NS5B inhibitors and other compounds which can be metabolized in vivo to HCV NS5B inhibitors. The compounds and their pharmaceutically acceptable salts are useful for the prophylaxis or treatment of infection by HCV and the prophylaxis, treatment, or delay in the onset of disease caused by HCV. The compounds and their salts can be employed as ingredients in pharmaceutical compositions, optionally in combination with other antivirals, immunomodulators, antibiotics or vaccines.
    Type: Grant
    Filed: October 11, 2013
    Date of Patent: January 26, 2016
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Vinay Girijavallabhan, Stephane Bogen, Weidong Pan, Qun Dang, Ian Davies
  • Patent number: 9102634
    Abstract: Enantiomerically enriched (1 S,4R)-2-oxa-3-azabicyclo[2.2.1]hept-5-ene of formula wherein PG1 is an amino-protective group, are prepared from cyclopentadiene via hetero-Diels-Alder cycloaddition with protected 1-C-nitroso-?-D-ribofuranosyl halides of formula wherein X is a halogen atom selected from fluorine, chlorine, bromine and iodine, PG2 is a hydroxyl-protective group and PG3 is a 1,2-diol-protective group.
    Type: Grant
    Filed: August 25, 2010
    Date of Patent: August 11, 2015
    Inventors: Manuela Franzen, Christian Noti
  • Patent number: 9040498
    Abstract: The present invention relates to novel 1,2,3-triazolyl purine derivatives. The invention also relates to using the derivatives to treat cancer and various viral infections.
    Type: Grant
    Filed: July 8, 2013
    Date of Patent: May 26, 2015
    Assignee: Research Foundation of the City University of New York
    Inventor: Mahesh K. Lakshman
  • Patent number: 9029335
    Abstract: Provided herein are novel bicyclic nucleosides, oligomeric compounds that include such bicyclic nucleosides and methods of using the oligomeric compounds. More particularly, the novel bicyclic nucleosides comprise a furanose ring system having a bridge comprising a 4?-methylene group attached to a 2?-sulfoxide or sulfone group and optionally including one or more substituent groups attached to the 4?-methylene and or the 5?-position. In certain embodiments, the oligomeric compounds provided herein are expected to hybridize to a portion of a target RNA resulting in loss of normal function of the target RNA.
    Type: Grant
    Filed: October 9, 2013
    Date of Patent: May 12, 2015
    Assignee: Isis Pharmaceuticals, Inc.
    Inventors: Thazha P. Prakash, Eric E. Swayze
  • Patent number: 8987437
    Abstract: The invention provides synthetic processes and synthetic intermediates that can be used to prepare compounds having useful anti-HIV properties.
    Type: Grant
    Filed: May 18, 2012
    Date of Patent: March 24, 2015
    Assignee: Gilead Sciences, Inc.
    Inventors: Richard Hung Chiu Yu, Brandon Heath Brown, Richard P. Polniaszek, Benjamin R. Graetz, Keiko Sujino, Duong Duc-Phi Tran, Alan Scott Triman, Kenneth M. Kent, Steven Pfeiffer
  • Patent number: 8969545
    Abstract: Alkynyl-derivatized cap analogs, alkynyl-modified capped RNA, 1,4-disubstituted triazole-derivatized capped RNA, methods of preparation, methods of isolation, and uses thereof are provided. The “click” modification facilitates detection and isolation of capped RNAs and the 1,4-disubstituted triazole derivatives formed by the “click” reaction are useful for producing RNA transcripts and encoded protein.
    Type: Grant
    Filed: October 18, 2012
    Date of Patent: March 3, 2015
    Assignee: Life Technologies Corporation
    Inventors: Anilkumar R. Kore, Shanmugasundaram Muthian, Kyle Gee
  • Patent number: 8957200
    Abstract: The present invention provides novel 3?,5?-linked bicyclic nucleosides and oligomeric compounds prepared therefrom. The bicyclic nucleosides provided herein are useful for enhancing one or more properties of the oligomeric compounds they are incorporated into such as nuclease resistance.
    Type: Grant
    Filed: June 6, 2011
    Date of Patent: February 17, 2015
    Assignee: Isis Pharmaceuticals, Inc.
    Inventors: Punit P. Seth, Eric E. Swayze, Stephen Hanessian, Benjamin R. Schroeder
  • Patent number: 8927520
    Abstract: The present invention relates to compounds of formula (I): wherein Rj, R2, R3, R4, Xi, X2, X3 and Z are as defined in claim 1. The compounds are useful in the prevention and/or treatment of bacterial infections.
    Type: Grant
    Filed: December 22, 2011
    Date of Patent: January 6, 2015
    Assignees: Institut Pasteur, Institut Curie
    Inventors: Sylvie Pochet, Gilles Labesse, Muriel Gelin, Liliane Assairi, Olivier Dussurget, Guillaume Poncet-Montange
  • Publication number: 20140378402
    Abstract: Disclosed is a pharmaceutical composition containing as an active ingredient a compound represented by formula (I) or a physiologically acceptable salt thereof, and a method for treating cancer, the method including administering the compound represented by formula (I) or the physiologically acceptable salt thereof.
    Type: Application
    Filed: January 29, 2013
    Publication date: December 25, 2014
    Applicant: NATIONAL UNIVERSITY CORPORATION NARA INSTITUTE OF SCIENCE AND TECHNOLOGY
    Inventors: Shigenobu Yano, Takashi Shibahara, Shunichiro Ogura
  • Patent number: 8912318
    Abstract: Embodiments are disclosed herein that involve C5-functionalized nucleic acids, which can be used for detecting a target in a nucleic acid. Particular embodiments disclose methods for making these compounds, wherein the compounds can be formed by coupling of an intermediate with a linker. Certain embodiments disclose the use of these compounds for detecting single nucleotide polymorphisms, and for increasing the thermal affinity of nucleic acid complements as compared to unmodified nucleic acid complements. In addition, the disclosed compounds can decrease enzymatic degradation of nucleic acids.
    Type: Grant
    Filed: June 19, 2013
    Date of Patent: December 16, 2014
    Assignee: University of Idaho
    Inventors: Patrick Jerzy Hrdlicka, Pawan Kumar, Michael E. Østergaard
  • Patent number: 8906869
    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. The invention further encompasses a number of miRNAs, which are altered in human ovarian cancer, with the most significantly deregulated miRNAs being miR-214, -199a*, -200a, -100, -12Sb, and let-7 cluster. Further, the invention illustrates that frequent deregulation of miR-214, -199a*, -200a and -100 in ovarian cancers and their alterations are associated with high grade and late stage tumor.
    Type: Grant
    Filed: July 8, 2013
    Date of Patent: December 9, 2014
    Assignee: University of South Florida
    Inventor: Jin Q. Cheng
  • Patent number: 8901086
    Abstract: This invention encompasses combination therapies including TCN, TCN-P, TCN-PM and/or related compounds and one or more additional anti-cancer agents, for example, taxanes a molecule that modulates the HER2/neu (erbB2) receptor, anthracyclin compounds, epidermal growth factor receptor inhibitor compounds, one or more platinum compounds and bortezomib and derivatives 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: May 3, 2012
    Date of Patent: December 2, 2014
    Assignee: University of South Florida
    Inventors: Jin Q. Cheng, Said M. Sebti
  • Patent number: 8865666
    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: April 23, 2012
    Date of Patent: October 21, 2014
    Assignee: University of South Florida
    Inventors: Jin Q. Cheng, Said M. Sebti
  • Patent number: 8846637
    Abstract: Provided herein are 2?-amino and 2?-thio bicyclic nucleosides and oligomenc compounds prepared therefrom. The novel bicyclic nucleosides provided herein are expected to be useful for enhancing one or more properties of the oligomeric compounds they are incorporated into such as nuclease resistance.
    Type: Grant
    Filed: June 2, 2011
    Date of Patent: September 30, 2014
    Assignee: Isis Pharmaceuticals, Inc.
    Inventors: Punit P. Seth, Thazha P. Prakash, Eric E. Swayze
  • Patent number: 8841275
    Abstract: Disclosed herein are 2?-spiro-nucleosides and derivatives thereof useful for treating a subject infected by hepatitis C virus or dengue virus.
    Type: Grant
    Filed: November 30, 2011
    Date of Patent: September 23, 2014
    Assignee: Gilead Pharmasset LLC
    Inventors: Jinfa Du, Michael Joseph Sofia
  • Patent number: 8759318
    Abstract: Phosphoramidate compounds derived from guanine bases having enhanced therapeutic potency are provided, and these compounds in particular have enhanced potency with respect to treatment of viral infections, such as hepatitis C virus. Pharmaceutical compositions, methods of preparing the compounds, and methods of using the compounds and compositions to treat viral infections are also provided.
    Type: Grant
    Filed: January 11, 2010
    Date of Patent: June 24, 2014
    Assignees: Inhibitex, Inc., University College Cardiff Consultants Limited
    Inventors: Stanley Chamberlain, Jeff Hutchins, Karolina Madela, Christopher McGuigan, John Vernachio, Mohamed Aljarah, Arnaud Gilles
  • Patent number: 8691779
    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: April 20, 2012
    Date of Patent: April 8, 2014
    Assignee: University of South Florida
    Inventors: Jin Q. Cheng, Said M. Sebti
  • Patent number: 8686130
    Abstract: The present invention relates to novel unnatural fluorescent nucleic acid bases, that is, a purine base, a 1-deazapurine base, and a 1,7-deazapurine base each having a functional group which consists of two or more heterocyclic moieties linked together, at the 6-position thereof (the 6-position of purine ring). The present invention also relates to a compound containing the unnatural base, a derivative thereof, and a nucleic acid containing a nucleotide having the unnatural base. The present invention also relates to a method of preparing the nucleic acid. The unnatural base of the present invention has excellent fluorescence characteristics and also has excellent properties as a universal base.
    Type: Grant
    Filed: October 6, 2010
    Date of Patent: April 1, 2014
    Assignees: Riken, Tagcyx Biotechnologies
    Inventors: Ichiro Hirao, Michiko Hirao, Shigeyuki Yokoyama, Tsuneo Mitsui
  • Patent number: 8673867
    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: April 23, 2012
    Date of Patent: March 18, 2014
    Assignee: University of South Florida
    Inventors: Jin Q. Cheng, Said M. Sebti
  • Patent number: 8673868
    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: April 23, 2012
    Date of Patent: March 18, 2014
    Assignee: University of South Florida
    Inventors: Jin Q. Cheng, Said M. Sebti
  • Patent number: 8637475
    Abstract: 2? and/or 3? prodrugs of 1?, 2?, 3? or 4?-branchednucleosides, and their pharmaceutically acceptable salts and derivatives are described. These prodrugs are useful in the prevention and treatment of Flaviviridae infections, including HCV infection, and other related conditions. Compounds and compositions of the prodrugs of the present invention are described. Methods and uses are also provided that include the administration of an effective amount of the prodrugs of the present invention, or their pharmaceutically acceptable salts or derivatives. These drugs may optionally be administered in combination or alteration with further anti-viral agents to prevent or treat Flaviviridae infections and other related conditions.
    Type: Grant
    Filed: June 24, 2011
    Date of Patent: January 28, 2014
    Assignees: Idenix Pharmaceuticals, Inc., University of Cagliari, The Centre National de la Recherché Scientifique, L'Universite Montpelier II
    Inventors: Richard Storer, Gilles Gosselin, Jean-Pierre Sommadossi
  • Patent number: 8637648
    Abstract: This invention relates generally to compositions comprising noribogaine and an excipient to facilitate transport across the blood brain barrier.
    Type: Grant
    Filed: June 21, 2011
    Date of Patent: January 28, 2014
    Assignee: Demerx, Inc.
    Inventors: Deborah C. Mash, Robert M. Moriarty
  • Publication number: 20140011989
    Abstract: A tetrapyrrolic photosensitizer and imaging compound having a substituent other than hydrogen at its 10 carbon atom which substituent may contain a PAA nanoparticle.
    Type: Application
    Filed: July 9, 2012
    Publication date: January 9, 2014
    Applicant: PHOTOLITEC, LLC
    Inventors: Ravindra K. Pandey, Anurag Gupta, Penny Joshi, Manivannan Ethirajan, Avinash Srivatsan
  • Patent number: 8623834
    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: April 23, 2012
    Date of Patent: January 7, 2014
    Assignee: University of South Florida
    Inventors: Jin Q. Cheng, Said M. Sebti
  • Patent number: 8609627
    Abstract: The present invention is directed to compounds, compositions and methods for treating or preventing cancer and viral infections, in particular, HIV, HCV, Norovirus, Saporovirus, HSV-1, HSV-2, Dengue virus, Yellow fever, and HBV in human patients or other animal hosts. The compounds are certain 6-substituted purine monophosphates, and pharmaceutically acceptable, salts, prodrugs, and other derivatives thereof. In particular, the compounds show potent antiviral activity against HIV-1, HIV-2, HCV, Norovirus, Saporovirus, HSV-1, HSV-2, Dengue virus, Yellow fever, and HBV.
    Type: Grant
    Filed: February 9, 2010
    Date of Patent: December 17, 2013
    Assignees: RFS Pharma, LLC, Emory University
    Inventors: Jong Hyun Cho, Steven J. Coats, Raymond F. Schinazi, Hongwang Zhang, Longhu Zhou
  • Patent number: 8580763
    Abstract: The present invention provides 2,6-dinitrogen-containing substituted purine compounds of formula (A) or salts or solvates thereof or the solvates of salts thereof, as well as pharmaceutical compositions containing such compounds. The compounds of the present invention have the characteristics of lower toxicity, broad anticancer spectrum, higher anticancer activity, good stability and the like. The compounds are useful for the manufacture of an antitumor medicament. The present invention also provides a process for preparing these compounds.
    Type: Grant
    Filed: April 17, 2008
    Date of Patent: November 12, 2013
    Assignees: Zhanggui Wu, Zhe Jiang Medicine Co., Ltd
    Inventors: Zhanggui Wu, Weidong Ye, Jianyong Yuan, Gang Chen
  • Patent number: 8541391
    Abstract: The invention relates to novel crystalline forms of 5,6-dichloro-2-(isopropylamino)-1-(?-L-ribofuranosyl)-1H-benzimidazole (Maribavir), pharmaceutical compositions thereof and their use in medical therapy.
    Type: Grant
    Filed: October 27, 2011
    Date of Patent: September 24, 2013
    Assignee: ViroPharma Incorporated
    Inventors: Eugene C. Amparo, Cristina Stoica, Mihaela Pop, Jaroslaw Mazurek
  • Patent number: 8541562
    Abstract: It is an object of the present invention to provide a novel molecule for antisense therapies which is not susceptible to nuclease degradation in vivo and has a high binding affinity and specificity for the target mRNAs and which can efficiently regulate expression of specific genes. The novel artificial nucleoside of the present invention has an amide bond introduced into a bridge structure of 2?,4?-BNA/LNA. The oligonucleotide containing the 2?,4?-bridged artificial nucleotide has a binding affinity for a single-stranded RNA comparable to known 2?,4?-BNA/LNA and has an increased nuclease resistance over LNA. Particularly, it is expected to be applied to nucleic acid drugs because of its much stronger binding affinity for single-stranded RNAs than S-oligo's affinity.
    Type: Grant
    Filed: October 19, 2010
    Date of Patent: September 24, 2013
    Assignee: Osaka University
    Inventors: Satoshi Obika, Yoshiyuki Hari, Tetsuya Kodama, Aiko Yahara, Masaru Nishida
  • Patent number: 8541569
    Abstract: The present invention provides building blocks and methods for synthesizing very pure RNA in a form that can efficiently be modified at the 3? end. Reverse RNA monomer phosphoramidites have been developed for RNA synthesis in 5??3? direction, leading to very clean oligo synthesis that allows for the introduction of various modifications at the 3?-end cleanly and efficiently. Higher coupling efficiency per step have been observed during automated oligo synthesis with the reverse RNA amidites disclosed herein, resulting in a greater ability to achieve higher purity and produce very long oligonucleotides. The use of the reverse RNA phosphoramidites in the synthetic process of this invention leads to oligonucleotides free of N+1 species.
    Type: Grant
    Filed: February 19, 2010
    Date of Patent: September 24, 2013
    Assignee: ChemGenes Corporation
    Inventors: Suresh C. Srivastava, Naveen P. Srivastava
  • Patent number: 8518901
    Abstract: The invention encompasses novel compounds and pharmaceutically acceptable salts thereof and compositions including therapeutically or prophylactically effective amounts of such compounds or pharmaceutically acceptable salts thereof. The invention also encompasses methods for treating or preventing diseases and disorders associated abnormal cell growth, for example, treating or preventing cancer or tumor growth, which methods include administering to a mammal in need thereof a composition comprising a therapeutically or prophylactically effective amount of a compound of the invention or a pharmaceutically acceptable salt thereof.
    Type: Grant
    Filed: September 23, 2009
    Date of Patent: August 27, 2013
    Assignee: The Johns Hopkins University
    Inventors: Ramachandra S. Hosmane, Venu Raman, Raj Kumar
  • Patent number: 8518908
    Abstract: Embodiments are disclosed herein that involve C5-functionalized nucleic acids, which can be used for detecting a target in a nucleic acid. Particular embodiments disclose methods for making these compounds, wherein the compounds can be formed by coupling of an intermediate with a linker. Certain embodiments disclose the use of these compounds for detecting single nucleotide polymorphisms, and for increasing the thermal affinity of nucleic acid complements as compared to unmodified nucleic acid complements. In addition, the disclosed compounds can decrease enzymatic degradation of nucleic acids.
    Type: Grant
    Filed: March 9, 2012
    Date of Patent: August 27, 2013
    Assignee: University of Idaho
    Inventors: Patrick J. Hrdlicka, Pawan Kumar, Michael E. Østergaard
  • Publication number: 20130157970
    Abstract: Compounds of formula (I): wherein X, Y, and Z are defined herein. Also disclosed are pharmaceutical compositions and therapeutical methods related to these compounds.
    Type: Application
    Filed: December 13, 2012
    Publication date: June 20, 2013
    Applicant: National Health Research Institutes
    Inventor: National Health Research Institutes
  • Patent number: 8461128
    Abstract: Many pathogens, including Mycobacterium tuberculosis and Yersinia pestis, rely on an iron acquisition system based on siderophores, secreted iron-chelating compounds with extremely high Fe(III) affinity. The compounds of the invention are inhibitors of domain salicylation enzymes, which catalyze the salicylation of an aroyl carrier protein (ArCP) domain to form a salicyl-ArCP domain thioester intermediate via a two-step reaction. The compounds include the intermediate mimic 5?-O—[N-(salicyl)sulfamoyl]-adenosine (salicyl-AMS) and analogs thereof. These compounds are inhibitors of the salicylate activity of MbtA, YbtE, PchD, and other domain salicylation enzymes involved in the biosynthesis of siderophores. Therefore, these compounds may be used in the treatment of infection caused by microorganisms which rely on siderphore-based iron acquisition systems.
    Type: Grant
    Filed: April 14, 2006
    Date of Patent: June 11, 2013
    Assignees: Sloan-Kettering Institute for Cancer Research, Cornell Research Foundation, Inc.
    Inventors: Derek Shieh Tan, Luis E. N. Quadri, Jae-Sang Ryu, Justin Scott Cisar, Julian Alberto Ferreras, Xuequan Lu
  • Publication number: 20130131013
    Abstract: The present invention relates to novel compositions of therapeutic cyclodextrin containing polymeric compounds designed as a carrier for small molecule therapeutics delivery and pharmaceutical compositions thereof. These cyclodextrin-containing polymers improve drug stability and solubility, and reduce toxicity of the small molecule therapeutic when used in vivo. Furthermore, by selecting from a variety of linker groups and targeting ligands the polymers present methods for controlled delivery of the therapeutic agents. The invention also relates to methods of treating subjects with the therapeutic compositions described herein. The invention further relates to methods for conducting pharmaceutical business comprising manufacturing, licensing, or distributing kits containing or relating to the polymeric compounds described herein.
    Type: Application
    Filed: January 11, 2013
    Publication date: May 23, 2013
    Applicant: CERULEAN PHARMA INC.
    Inventor: CERULEAN PHARMA INC.
  • Patent number: 8435959
    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: March 29, 2005
    Date of Patent: May 7, 2013
    Assignee: University of South Florida
    Inventors: Jin Q. Cheng, Said M. Sebti
  • Patent number: 8394950
    Abstract: This invention relates to compounds that are analogues of coformycin, pharmaceutical compositions containing the compounds, and methods of using the compounds for treating protozoan parasite infections, especially malaria.
    Type: Grant
    Filed: February 22, 2007
    Date of Patent: March 12, 2013
    Assignees: Industrial Research Limited, Albert Einstein College of Medicine of Yeshiva University
    Inventors: Richard Hubert Furneaux, Peter Charles Tyler, Gary Brian Evans, Vern L. Schramm, Kami Kim, Richard Fröhlich
  • Publication number: 20130041144
    Abstract: Provided herein are novel 5?-(S)—CH3 substituted bicyclic nucleosides, oligomeric compounds prepared therefrom and methods of using the oligomeric compounds. More particularly, the furanose ring of each of the novel 5?-(S)—CH3 substituted bicyclic nucleosides includes a 2? to 4? bridging group. The 5?-(S)—CH3 substituted bicyclic nucleosides are expected to be useful for enhancing one or more properties of the oligomeric compounds they are incorporated into such as for example increasing the binding affinity. In certain embodiments, the oligomeric compounds provided herein hybridize to a portion of a target RNA resulting in loss of normal function of the target RNA.
    Type: Application
    Filed: March 10, 2011
    Publication date: February 14, 2013
    Applicant: Isis Pharmaceuticals, Inc.
    Inventors: Michael T. Migawa, Thazha P. Prakash, Charles Allerson, Balkrishen Bhat, Punit P. Seth, Eric E. Swayze
  • Patent number: 8329664
    Abstract: A compound for use in the treatment or prophylaxis of viral infections such, for example as chicken pox or shingles caused by the Varicella Zoster virus, said compound having the general formula (II): wherein X is O, S, NH or CH2, Y is O, S or NH, Z is O, S or CH2, R1 is C1-6 alkyl, preferably n-alkyl, e.g., n-pentyl or n-hexyl, and one of R2 and R3 is OH, and the other of R3 and R2 is a neutral, non-polar amino acid moiety, or a pharmaceutically acceptable salt or hydrate thereof. Said neutral, non-polar amino acid moiety R2 or R3 may be (IV): in which R4, R5, R6 and R7 are each independently H or C1-2 alkyl. In preferred embodiments, one of R2 or R3 is valine, leucine, isoleucine or alanine, particularly valine.
    Type: Grant
    Filed: May 9, 2007
    Date of Patent: December 11, 2012
    Assignees: University College Cardiff Consultants Limited, K.U. Leuven Research and Development
    Inventors: Christopher McGuigan, Jan Balzarini, Marco Migliore
  • Publication number: 20120301424
    Abstract: The present invention relates to novel compositions of therapeutic cyclodextrin containing polymeric compounds designed as a carrier for small molecule therapeutics delivery and pharmaceutical compositions thereof. These cyclodextrin-containing polymers improve drug stability and solubility, and reduce toxicity of the small molecule therapeutic when used in vivo. Furthermore, by selecting from a variety of linker groups and targeting ligands the polymers present methods for controlled delivery of the therapeutic agents. The invention also relates to methods of treating subjects with the therapeutic compositions described herein. The invention further relates to methods for conducting pharmaceutical business comprising manufacturing, licensing, or distributing kits containing or relating to the polymeric compounds described herein.
    Type: Application
    Filed: August 10, 2012
    Publication date: November 29, 2012
    Applicant: CERULEAN PHARMA INC.
    Inventors: Jianjun Cheng, Mark E. Davis, Kay T. Khin
  • Publication number: 20120270827
    Abstract: The present invention provides novel chemical compounds, and methods for their use. In particular, the present invention provides indole derivatives (e.g. as shown in Formula (I)) and related compounds and methods of using indole derivatives and related compounds as therapeutic agents to treat a number of conditions, including those associated with viral infection and cardiovascular diseases.
    Type: Application
    Filed: June 11, 2012
    Publication date: October 25, 2012
    Applicant: THE REGENTS OF THE UNIVERSITY OF MICHIGAN
    Inventors: Leroy B. Townsend, John C. Drach
  • Patent number: 8288526
    Abstract: The present invention provides a method for producing an inosine derivative represented by the following general formula (1) including the steps of subjecting an inosine derivative of general formula (3) to dithiocarbonylation and carrying out radical reduction of the obtained compound. According to the present invention there can be produced compounds useful as anti-AIDS drugs on industrial scale. wherein R1 may be the same or different and are each benzyl group, benzhydryl group or trityl group, each of which may have a substituent in general formulas (1) and (3).
    Type: Grant
    Filed: July 30, 2010
    Date of Patent: October 16, 2012
    Assignee: Ajinomoto Co., Inc.
    Inventors: Takayoshi Torii, Kunisuke Izawa, Doo Ok Jang, Dae Hyan Cho
  • Patent number: 8278283
    Abstract: The present disclosure describes 6-disubstituted bicyclic nucleosides, oligomeric compounds prepared therefrom and methods of using the oligomeric compounds. More particularly, the 6-disubstituted bicyclic nucleosides each comprise a 2?-O—C(Ri)(R2)-4? or 2?-O—C=(R3)(R.4)-4? bridge wherein each R is, independently a substituent group and Ri and R2 include H. The 6-disubstituted bicyclic nucleosides are useful for enhancing properties of oligomeric compounds including nuclease resistance. In certain embodiments, the oligomeric compounds provided herein hybridize to a portion of a target RNA resulting in loss of normal function of the target RNA.
    Type: Grant
    Filed: July 1, 2008
    Date of Patent: October 2, 2012
    Assignee: Isis Pharmaceuticals, Inc.
    Inventors: Punit P. Seth, Eric E. Swayze
  • Patent number: 8278426
    Abstract: Provided herein are saturated and unsaturated carbocyclic bicyclic nucleosides, oligomeric compounds prepared therefrom and methods of using these oligomeric compounds. The saturated and unsaturated carbocyclic bicyclic nucleosides are useful for enhancing properties of oligomeric compounds including nuclease resistance.
    Type: Grant
    Filed: June 6, 2008
    Date of Patent: October 2, 2012
    Assignee: Isis Pharmaceuticals, Inc.
    Inventors: Punit P. Seth, Eric E. Swayze
  • Patent number: 8278282
    Abstract: This invention relates to novel compounds that have various medicinal applications, e.g. for the treatment and/or prevention of viral infections.
    Type: Grant
    Filed: February 7, 2008
    Date of Patent: October 2, 2012
    Assignee: Novartis AG
    Inventors: Zheng Yin, Jeyaraj Duraiswamy, Yen Liang Chen
  • Patent number: 8278425
    Abstract: Provided herein are bicyeMc nucleosides comprising a substituted amino group in the bridge, oligomeric compounds having at least one of these bicyclic nucleosides and methods of using the oligomeric compounds. The bicyclic nucleosides comprising a substituted amino group in the bridge are useful for enhancing properties of oligomeric compounds including nuclease resistance, in certain embodiments, the oligomeric compounds hybridize to a portion of a target RNA resulting in loss of normal function of the target RNA.
    Type: Grant
    Filed: May 22, 2008
    Date of Patent: October 2, 2012
    Assignee: Isis Pharmaceuticals, Inc.
    Inventors: Thazha P. Prakash, Balkrishin Bhat, Eric E. Swayze