Nitrogen Containing Hetero Ring Patents (Class 514/43)
  • Publication number: 20150023913
    Abstract: The present disclosure is generally directed to antiviral compounds, and more specifically directed to combinations of compounds which can inhibit the function of the NS5A protein encoded by Hepatitis C virus (HCV), compositions comprising such combinations, and methods for inhibiting the function of the NS5A protein.
    Type: Application
    Filed: July 2, 2013
    Publication date: January 22, 2015
    Inventors: Piyasena Hewawasam, Omar D. Lopez, Yong Tu, Alan Xiangdong Wang, Ningning Xu, John F. Kadow, Nicholas A. Meanwell, Samayamuthula Venkata Satya Arun Kumar Gupta, Indasi J. Gopi Kumar, Suresh Kumar Ponugupati, Makonen Belema
  • Publication number: 20150025000
    Abstract: The present invention features interferon-free therapies for the treatment of HCV. The therapies comprise administering 2R,6S,13aS,14aR,16aS,Z)-N-(cyclopropylsulfonyl)-6-(5-methylpyrazine-2-carboxamido)-5,16-dioxo-2-(phenanthridin-6-yloxy)-1,2,3,5,6,7,8,9,10,11,13a,14,14a,15,16,16a-exadecahydrocyclopropa[e]pyrrolo[1,2-a][1,4]diazacyclopentadecine-14a-carboxamide (Compound I), or a pharmaceutically acceptable salt thereof, and another anti-HCV agent. Preferably, the therapies are both interferon- and ribavirin-free. The other anti-HCV agent can be a HCV polymerase inhibitor, an HCV NS5A inhibitor, an HCV entry inhibitor, a cyclophilin inhibitor, or an internal ribosome entry site inhibitor. Preferably, the other anti-HCV agent is an HCV polymerase inhibitor. Also preferably, the other anti-HCV agent is an HCV NS5A inhibitor. Also preferably, the other anti-HCV agent is administered concurrently with Compound I or a pharmaceutically acceptable salt thereof.
    Type: Application
    Filed: October 6, 2014
    Publication date: January 22, 2015
    Applicant: ABBVIE INC.
    Inventors: Barry M. Bernstein, Scott C. Brun
  • Publication number: 20150018292
    Abstract: The present invention relates to a novel alkaloid and novel bioactive alkaloid fractions derivable from Ribes preferably selected among Ribes Rubrum and Ribes nigrum; methods of manufacturing such bioactive Ribes alkaloid fractions and their use for the inhibition of IKK-?, PDE4 and/or PDE5 and in addition their promoting effect on mitochondrial biogenesis and function; their therapeutic or non-therapeutic applications as nutritive or medicinal products in the management of conditions associated with impaired mitochondrial function or IKK-?, PDE4 and/or PDE5 activity, such as inflammation, neurodegeneration, dyslipidemia, type 2 diabetes mellitus, impaired wound healing, sarcopenia and other conditions associated with muscle dysfunction or tiredness and fatigue, or where optimization of muscular or cognitive function is desired; extracts, juices or concentrates of Ribes comprising such alkaloids; compostions comprising such alkaloids, including pharmaceutical compositions, nutritive product such as functional
    Type: Application
    Filed: July 14, 2014
    Publication date: January 15, 2015
    Inventors: Morten Sloth Weidner, Ida Sloth Weidner
  • Publication number: 20150018296
    Abstract: The present invention is directed to therapeutic methods and compositions involving cyclohexenone compounds where said compounds inhibit farnesyltransferase or Ras. The therapeutic methods (e.g. for treating cancers) comprise contacting a tumor with a cyclohexenone compound and an anticancer agent.
    Type: Application
    Filed: March 13, 2014
    Publication date: January 15, 2015
    Applicant: Golden Biotechnology Corporation
    Inventors: Sheng-Yung Liu, Wu-Che Wen, Chih-Ming Chen
  • Publication number: 20150011488
    Abstract: Epicatechins, Epicatechin Oligomers, or Thiolated Epicatechins are applied (A) directly to a genital wart in the form of a cream, ointment, paste or solution, (B) directly to the genital wart wherein such cream, ointment, paste or solution contains as an additional active ingredient a skin permeabilizing agent, (C) following electrosurgical resection or removal of the genital wart in such form of a cream, ointment, paste or solution, (D) following chemical resection or extirpation of the genital wart in such form, (E) following surgical resection or removal of the genital wart in such form, wherein said Epicatechins, Epicatechin Oligomers, or Thiolated Epicatechins both provide antiviral activity against multiple strains of human pappilomavirus (HPV) and promote healing following resection polymers contained in a vehicle. Disclosed are the compositions, therapeutical kits containing such composition, methods of treatment using such composition, and methods of enhancing the stability of such composition.
    Type: Application
    Filed: March 10, 2014
    Publication date: January 8, 2015
    Applicant: CACAO BIO-TECHNOLOGIES, LLC
    Inventors: Daniel PRESTON, Randall B. MURPHY
  • 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: 20150005250
    Abstract: The subject invention pertains to methods and compositions for the detection and treatment of myelodysplastic syndromes based on impaired telomerase function.
    Type: Application
    Filed: October 15, 2012
    Publication date: January 1, 2015
    Inventors: Dana E. Rollison, Pearlie K. Burnette
  • Publication number: 20150005245
    Abstract: Sialic acid derivatives of the formula (I) in which the symbols have the definitions stated in the description are suitable as medicaments, more particularly for diseases whose course is influenced by Siglec ligands.
    Type: Application
    Filed: December 21, 2012
    Publication date: January 1, 2015
    Inventors: Reinhard Brossmer, Horst Prescher
  • Publication number: 20140377223
    Abstract: The present invention relates to novel Substituted Biphenylene Compounds of Formula (I): and pharmaceutically acceptable salts thereof, wherein Y1, Y2, R1, R2, R4, Ra and Rb are as defined herein. The present invention also relates to compositions comprising at least one Substituted Biphenylene Compound, and methods of using the Substituted Biphenylene Compounds for treating or preventing HCV infection in a patient.
    Type: Application
    Filed: July 21, 2011
    Publication date: December 25, 2014
    Inventors: Joseph A. Kozlowski, Bandarpalle B. Shankar
  • Publication number: 20140378407
    Abstract: The present invention relates to a process of preparing a stable pharmaceutical composition of compounds which are susceptible to hydrolysis comprising a. Addition of required quantity of pharmaceutically acceptable lyophilization excipients optionally in Water for Injection in a formulation vessel; b. Addition of organic solvent to form a appropriate proportion of aqueous and organic solvent; c. Maintaining the temperature of the formulation vessel from the range ?5±1° C. to ?5±3° C.; d. Addition of required quantity of compound susceptible to hydrolysis to form a solution and lyophilizing the solution.
    Type: Application
    Filed: March 29, 2012
    Publication date: December 25, 2014
    Applicant: Fresenius Kabi Oncology Limited
    Inventors: Dhiraj Khattar, Rajesh Khanna, Sanjay Motwani, Minakshi Garg, Vikas Chandel, Mukti Yadav, Vijay Kumar Kyama, Vikas Bhandari
  • 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: 8916538
    Abstract: The present application relates to solid state forms, for example, crystalline forms of 2?-C-methyluridine-5?-(O-phenyl-N—(S)-1-(isopropoxycarbonyl)ethyl)thiophosphoramidate, pharmaceutical compositions that can include one or more solid forms of 2?-C-methyluridine-5?-(O-phenyl-N—(S)-1-(isopropoxycarbonyl)ethyl)thiophosphoramidate, and methods of treating or ameliorating diseases and/or conditions with one or more solid forms of 2?-C-methyluridine-5?-(O-phenyl-N—(S)-1-(isopropoxycarbonyl)ethyl)thiophosphoramidate. Also disclosed herein are methods of treating diseases and/or conditions with one or more solid forms of 2?-C-methyluridine-5?-(O-phenyl-N—(S)-1-(isopropoxycarbonyl)ethyl)thiophosphoramidate in combination with one or more other agents.
    Type: Grant
    Filed: March 11, 2013
    Date of Patent: December 23, 2014
    Assignee: Vertex Pharmaceuticals Incorporated
    Inventors: Anuj K. Kuldipkumar, Ales Medek, Lori Ann Ferris, Praveen Mudunuri, Young Chun Jung, David Richard Willcox, Michael Waldo, William Aloysius Nugent
  • Patent number: 8916528
    Abstract: A resveratrol-containing composition capable of providing a therapeutic benefit to a subject such as modulation of a biological activity, improving cell transplantation therapy, or improving macular degeneration or dystrophy treatments. The compositions comprise trans-resveratrol, a metal chelator, one or more additional antioxidants such as quercetin, gamma-tocotrienol, or apple polyphenols, allicin, and nucleotides.
    Type: Grant
    Filed: November 16, 2012
    Date of Patent: December 23, 2014
    Assignee: Resveratrol Partners, LLC
    Inventor: William F. Sardi
  • Patent number: 8916535
    Abstract: The invention relates to the therapeutic uses of 2?,5?-oligoadenylate derivative compounds, more particularly for the treatment of chronic fatigue syndrome (CFS) and in the treatment of infection by a gamma-retrovirus.
    Type: Grant
    Filed: November 10, 2011
    Date of Patent: December 23, 2014
    Assignee: Protea Biopharma N.V.
    Inventors: Christiaan Roelant, Kenny De Meirleir
  • Patent number: 8916536
    Abstract: The present invention relates to novel bisphosphonate duplex drugs, methods for preparing said compound; pharmaceutical compositions containing the same; as well as the use of said compounds in human and veterinary medicine, and, in particular, for treating tumors, viral infections; or dental disorders.
    Type: Grant
    Filed: August 3, 2011
    Date of Patent: December 23, 2014
    Inventor: Herbert Schott
  • Patent number: 8912162
    Abstract: The present invention relates to parenteral formulations for certain long chain saturated and monounsaturated fatty acid derivatives of 1-?-D-arabinofuranosylcytosine (cytarabine). In particular, the present invention relates to a parenteral pharmaceutical composition and a method of the preparation thereof, in order to accommodate therapeutically effective doses of the said derivatives ameliorating compliance in treatment of cancer.
    Type: Grant
    Filed: July 1, 2011
    Date of Patent: December 16, 2014
    Assignee: Clavis Pharma ASA
    Inventors: Sayeh Ahrabi, Finn Myhren, Ole Henrik Eriksen
  • Publication number: 20140363396
    Abstract: Hepatitis C is treated by administering once daily ribavirin, taribavirin, other derivatives or pharmaceutically acceptable salts thereof. Hepatitis C may also be treated by administering any of the foregoing compounds once daily in combination with interferon and/or direct-acting antivirals. Once daily dosage forms administered for treating hepatitis C may comprise between 800 mg and 1400 of ribavirin. Once daily dosage forms administered for treating hepatitis C may also comprise between 800 mg and 4000 mg of taribavirin.
    Type: Application
    Filed: February 1, 2013
    Publication date: December 11, 2014
    Applicant: KADMON PHARMACEUTICALS LLC
    Inventor: Samuel Waksal
  • Publication number: 20140363395
    Abstract: Compounds, compositions and methods are provided for the prophylaxis and treatment of infections caused by viruses of the Pneumovirinae subfamily of Paramyxoviridae and diseases associated with such infection.
    Type: Application
    Filed: July 24, 2014
    Publication date: December 11, 2014
    Inventors: Theodore J. Nitz, Janet A. Gaboury, Christopher J. Burns, Sylvie Laquerre, Daniel C. Pevear, Thomas A. Lessen, David J. Rys
  • Patent number: 8906879
    Abstract: The present invention relates to a method of treating cancer in a human and to pharmaceutical combinations useful in such treatment. In particular, the method relates to a cancer treatment method that includes administering 4-amino-1-(2-deoxy-2,2-difluoro-?-D-erythro-pentofuranosyl)pyrimidin-2(1H)-on 2?, 2?-difluoro-2?-deoxycytidine, or a pharmaceutically acceptable salt thereof, and N-{3-[3-cyclopropyl-5-(2-fluoro-4-iodo-phenylamino)6,8-dimethy; -2,4,7-trioxo-3,4,6,7-tetrahydro-2H-pyrido[4,3-d]pyrimidin-1-yl]phenyl}acetamide, or a pharmaceutically acceptable salt or solvate thereof, to a human in need thereof.
    Type: Grant
    Filed: December 20, 2011
    Date of Patent: December 9, 2014
    Assignee: GlaxoSmithKline Intellectual Property (No. 2) Limited
    Inventors: Douglas J. DeMarini, Ngocdiep T. Le
  • 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: 8906880
    Abstract: Disclosed herein are phosphoramidate prodrugs of nucleoside derivatives for the treatment of viral infections in mammals, which is a compound, its stereoisomer, salt (acid or basic addition salt), hydrate, solvate, or crystalline form thereof, represented by the following structure: Also disclosed are methods of treatment, uses, and processes for preparing each of which utilize the compound represented by formula I.
    Type: Grant
    Filed: April 17, 2014
    Date of Patent: December 9, 2014
    Assignee: Gilead Pharmasset LLC
    Inventors: Jinfa Du, Dhanapalan Nagarathnam, Michael Joseph Sofia, Peiyuan Wang
  • Publication number: 20140357567
    Abstract: Provided herein are methods for treating subjects having a cancer, such as a relapsed or refractory solid tumor, wherein the method comprises administering to the subject a cytidine analog. In certain of the methods, the cytidine analog is administered alone or in combination with one or more anti-cancer agents. Also provided are methods for using a cytidine analog, to treat diseases and disorders including disorders related to abnormal cell proliferation, hematologic disorders, and immune disorders, among others. In certain of the methods, the cytidine analog is formulated in an oral dosage form and administered orally.
    Type: Application
    Filed: June 17, 2014
    Publication date: December 4, 2014
    Inventors: Kyle J. MACBETH, Aaron N. NGUYEN, Jorge DIMARTINO
  • Publication number: 20140356373
    Abstract: The invention relates to compositions and methods for treating lupus. The methods typically comprise the step of administrating one or more compounds selected from isoindigo, indigo, indirubin, or derivatives thereof, such as, Meisoindigo and NATURA in an amount sufficient to treat the lupus; preferably by modulating cytokine expression. Preferably the compound is in an amount less than sufficient to substantially inhibit cyclin dependent kinases.
    Type: Application
    Filed: June 6, 2014
    Publication date: December 4, 2014
    Applicant: NATROGEN THERAPEUTICS INTERNATIONAL, INC.
    Inventors: Longgui Wang, Simon K. Mencher
  • Publication number: 20140356458
    Abstract: The present invention includes embodiments for treatment and/or prevention of sickle cell disease that employ Hydroxyfasudil or Isocoronarin D alone or either in conjunction with each other or an inducer of HbF production. The compounds may act synergistically, and the compounds employed circumvent the side effects seen with Hydroxyurea.
    Type: Application
    Filed: September 13, 2012
    Publication date: December 4, 2014
    Applicant: KING ABDULLAH UNIVERSITY OF SCIENCE AND TECHNOLOGY
    Inventors: Magbubah Essack, Vladimir Bajic, Aleksandar Radovanovic
  • Patent number: 8901092
    Abstract: Embodiments of the invention include functionalized polysaccharides and compositions and structures including the same. In an embodiment, the invention includes an active agent delivery composition including a polysaccharide functionalized with a coupling group, wherein the polysaccharide lacks charged groups at a pH of between 6 and 8; and a complex comprising a nucleic acid and a transfection agent. In an embodiment, the invention includes an active agent delivery structure including a matrix comprising a polysaccharide covalently cross-linked through the residue of a coupling group on the polysaccharide, the polysaccharide lacking charged groups at a pH of between 6 and 8; and a nucleic acid delivery complex disposed within the active agent delivery structure. In an embodiment, the invention includes a material for medical applications including glycogen functionalized with coupling groups at a degree of substitution of between about 0.01 and 0.5. Other embodiments are also included herein.
    Type: Grant
    Filed: December 22, 2011
    Date of Patent: December 2, 2014
    Assignee: SurModics, Inc.
    Inventor: Joram Slager
  • Patent number: 8900566
    Abstract: The present disclosure relates to compounds, compositions and methods for the treatment of hepatitis C virus (HCV) infection. Also disclosed are pharmaceutical compositions containing such compounds and methods for using these compounds in the treatment of HCV infection.
    Type: Grant
    Filed: September 18, 2013
    Date of Patent: December 2, 2014
    Assignee: Bristol-Myers Squibb Company
    Inventors: Makonen Belema, Van N. Nguyen
  • 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: 8900565
    Abstract: Described herein are compounds and pharmaceutical compositions containing such compounds, which inhibit the activity of histone deacetylase 8 (HDAC8). Also described herein are methods of using such HDAC8 inhibitors, alone and in combination with other compounds, for treating diseases or conditions that would benefit from inhibition of HDAC8 activity.
    Type: Grant
    Filed: November 21, 2012
    Date of Patent: December 2, 2014
    Assignee: Pharmacyclics, Inc.
    Inventors: Joseph J. Buggy, Sriram Balasubramanian, Erik Verner, Vincent W. F. Tai, Chang-Sun Lee
  • Publication number: 20140349938
    Abstract: The invention features methods of diagnosing a subject as having, or at risk of developing ALS by determining the frequency of Gems in cells obtained from the subject. These methods include diagnosing the severity or monitoring the progression of ALS by determining the Gem frequency in a subject. Also, the invention features methods of identifying compounds useful for the treatment of ALS as well as methods for the treatment of ALS.
    Type: Application
    Filed: June 1, 2012
    Publication date: November 27, 2014
    Applicant: President and Fellows of Harvard College
    Inventors: Robin Reed, Shi Chen, Yong Yu, Tomohiro Yamazaki
  • Patent number: 8895520
    Abstract: A method of treatment of a human patient suffering from myeloid neoplasias, includes administrating a therapeutically effective amount of 5-aminoimidazole-4-carboxamide (acadesine), acadesine precursors or acadesine derivatives.
    Type: Grant
    Filed: October 26, 2011
    Date of Patent: November 25, 2014
    Assignees: Universite Nice Sophia Antipolis, Centre Hospitalier Universitaire de Nice, INSERM (Institut National de la Sante et de la Recherche Medicale)
    Inventors: Thomas Cluzeau, Patrick Auberger, Guillaume Robert
  • Publication number: 20140343007
    Abstract: The present invention relates to pharmaceutical compositions and combination therapies for treating patents having a neoplasm or proliferative disorder, the combination comprises an inhibitor of the eIF4E gene product and a chemotherapeutic agent, wherein said combination therapy overcomes resistance developed in patients during anti-neoplastic treatment. The present invention also provides for the use of a combination therapy for treating patients having a neoplasm, a proliferative disorder, pre-neoplasm or a precancerous lesion, comprising an inhibitor of the eIF4E gene product, a chemotherapeutic agent, and a therapeutically effective amount of a hedgehog pathway inhibitor, and the method of using said combination therapy.
    Type: Application
    Filed: September 13, 2012
    Publication date: November 20, 2014
    Applicant: UNIVERSITE DE MONTREAL
    Inventors: Katherine Borden, Hiba Zahreddine, Biljana Culjkovic Kraljacic
  • Publication number: 20140341851
    Abstract: The present invention discloses compounds of Formula (I), or pharmaceutically acceptable salts, esters, or prodrugs thereof: which inhibit RNA-containing virus, particularly the hepatitis C virus (HCV). Consequently, the compounds of the present invention interfere with the life cycle of the hepatitis C virus and are also useful as antiviral agents. The present invention further relates to pharmaceutical compositions comprising the aforementioned compounds for administration to a subject suffering from HCV infection. The invention also relates to methods of treating an HCV infection in a subject by administering a pharmaceutical composition comprising the compounds of the present invention.
    Type: Application
    Filed: April 4, 2014
    Publication date: November 20, 2014
    Applicant: ENANTA PHARMACEUTICALS, INC.
    Inventors: YAO-LING QIU, Ce Wang, Xiaowen Peng, Hui Cao, Lu Ying, Xuri Gao, Bin Wang, Yat Sun Or
  • Publication number: 20140341850
    Abstract: A new class of haloalkyl heteroaryl benzamides is described. These compounds show strong activity against hepatitis viruses.
    Type: Application
    Filed: August 5, 2014
    Publication date: November 20, 2014
    Applicant: Romark Laboratories, L.C.
    Inventors: Jean-Francois Rossignol, J. Edward Semple
  • Patent number: 8889791
    Abstract: Provided are novel biocompatible copolymers and compositions comprising the copolymers. The copolymers and degradation products thereof are non-toxic and typically have an LCST between room temperature and 37° C. so that they are liquid at room temperature and gelled at 37° C. which facilitates their use in humans, for example for wound treatment and as a cellular growth matrix or niche. The copolymer comprises numerous ester linkages in its backbone so that the copolymers are erodeable in situ. Degradation products of the polymer are soluble and non-toxic. The copolymer is amine-reactive so that it can conjugate with proteins, such as collagen. Active ingredients, such as drugs, can be incorporated into compositions comprising the copolymer.
    Type: Grant
    Filed: October 10, 2007
    Date of Patent: November 18, 2014
    Assignee: University of Pittsburgh-Of the Commonwealth System of Higher Education
    Inventors: Jianjun Guan, William R. Wagner, Kazuro Lee Fujimoto
  • Publication number: 20140335074
    Abstract: Methods are provided herein for enhancing the effectiveness of medical therapies by administering agents that suppress a biological damage response that is inducible by the medical therapy administered to a subject. In certain embodiments, a method is provided for administering an anti-senescent cell agent that suppresses a biological response comprising cellular senescence that is induced by the medical therapy.
    Type: Application
    Filed: December 13, 2012
    Publication date: November 13, 2014
    Inventors: Judith Campisi, Marco Demaria
  • Patent number: 8883135
    Abstract: The invention provides crystalline solid forms of (((S)-1-{(S)-2-[4-(4?-{[6-((2R,5S)-2,5-dimethyl-4-methylcarbamoyl-piperazin-1-yl)-pyridine-3-carbonyl]-amino}-2?-trifluoromethoxy-biphenyl-4-yl)-1H-imidazol-2-yl]-pyrrolidine-1-carbonyl}-2-methyl-propyl)-carbamic acid methyl ester. The invention also provides pharmaceutical compositions comprising such crystalline solid forms, methods of using such crystalline solid forms to treat hepatitis C virus infection, and processes useful for preparing such crystalline solid forms.
    Type: Grant
    Filed: April 25, 2013
    Date of Patent: November 11, 2014
    Assignee: Theravance Biopharma R&D IP, LLC
    Inventors: Venkat R. Thalladi, Jerry Nzerem, Xiaojun Huang, Weijiang Zhang
  • Publication number: 20140328795
    Abstract: In an embodiment of the present disclosure there is provided a method of inactivating enveloped DNA virus particles in a biological sample. In an embodiment, such a method comprises contacting the biological sample with an effective amount of an antiviral composition comprising PD 404,182 In some embodiments, the DNA virus is the Herpes Simplex virus-1 (HSV-1) or the Herpes Simplex Virus-2 (HSV-2). In another embodiment of the present disclosure, there is provided a method of treating, preventing, or reducing a viral infection caused by an enveloped DNA virus in a subject in need thereof. In yet another embodiment, there is provided a method of preventing transmission of a viral infection to a subject in need thereof.
    Type: Application
    Filed: September 10, 2013
    Publication date: November 6, 2014
    Applicants: The Texas A&M University System, The Scripps Research Institute
    Inventors: Zhilei Chen, Karrupiah Chockalingam, Ana M. Chamoun-Emanuelli, Rudo Simeon, Michael Bobardt, Philippe Gallay
  • Publication number: 20140322165
    Abstract: The present invention provides, among other things, compounds represented by the general Formula I: and pharmaceutically acceptable salts thereof, wherein X, Y, R1A, R1B, R2, and R3 are as defined in classes and subclasses herein and compositions (e.g., pharmaceutical compositions) comprising such compounds, which compounds are useful as inhibitors of hepatitis C virus polymerase, and thus are useful, for example, as medicaments for the treatment of HCV infection.
    Type: Application
    Filed: July 8, 2014
    Publication date: October 30, 2014
    Inventors: Sam SK Lee, Wang Shen, Xiaoling Zheng, Irina C. Jacobson
  • Patent number: 8871735
    Abstract: The invention provides a method of reducing infarct size and/or limiting, decreasing and/or inhibiting reperfusion injury and/or ameliorating heart failure in a patient comprising administering a pharmaceutically effective amount of at least one compound capable of inhibiting AC5 to the patient. The compound capable of inhibiting AC5 is particularly effective when administered during or after reperfusion in patients suffering from an ischemic injury.
    Type: Grant
    Filed: November 5, 2012
    Date of Patent: October 28, 2014
    Assignee: Rutgers, The State University of New Jersey
    Inventors: Stephen F. Vatner, Dorothy E. Vatner
  • Publication number: 20140315848
    Abstract: Provided herein are methods for treating or preventing a cancer, comprising administering an effective amount of a TOR kinase inhibitor and an effective amount of a cytidine analog to a patient having a cancer.
    Type: Application
    Filed: April 16, 2014
    Publication date: October 23, 2014
    Applicant: Signal Pharmaceuticals, LLC
    Inventor: HEATHER RAYMON
  • 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
  • Publication number: 20140309186
    Abstract: A method, computer-readable medium, and system for identifying one or more metabolites associated with a disease, comprising: comparing gene expression data from diseased cells to gene expression data from control cells in order to deduce genes that are differentially-regulated in the diseased cells relative to the control cells; based on enzyme function and pathway data for all human metabolites that utilize the genes that are differentially-regulated in the disease cells, identifying one or more metabolites whose intracellular levels are higher or lower in diseased cells than in control cells, and thereby associating the one or more metabolites with the disease.
    Type: Application
    Filed: June 24, 2014
    Publication date: October 16, 2014
    Inventors: Jeffrey Skolnick, Adrian K. Arakaki, John McDonald, Roman Mezencev, Nathan Bowen
  • Publication number: 20140309187
    Abstract: Crystalline solid forms and the amorphous form of the anti-HCV compound 5-(3,3-dimethylbutyn-1-yl)-3-[(cis-4-hydroxy-4-{[(3S)-tetrahydrofuran-3-yloxy]methyl}cyclohexyl){[(1R)-4-methylcyclohex-3-en-1-yl]carbonyl}amino]thiophene-2-carboxylic acid (Compound I) were prepared and characterized in the solid state: Also provided are processes of manufacture and methods of using the crystalline forms.
    Type: Application
    Filed: June 24, 2014
    Publication date: October 16, 2014
    Inventors: Ahmad Hashash, Scott Wolckenhauer, Bing Shi
  • Publication number: 20140308243
    Abstract: The present invention discloses compounds of Formula (I), and pharmaceutically acceptable salts, esters, or prodrugs thereof: Q-G-A-L-B—Z—W??(I), which inhibit RNA-containing virus, particularly the hepatitis C virus (HCV). Consequently, the compounds of the present invention interfere with the life cycle of the hepatitis C virus and are also useful as antiviral agents. The present invention further relates to pharmaceutical compositions comprising the aforementioned compounds for administration to a subject suffering from HCV infection. The invention also relates to methods of treating an HCV infection in a subject by administering a pharmaceutical composition comprising the compounds of the present invention.
    Type: Application
    Filed: April 16, 2014
    Publication date: October 16, 2014
    Applicant: ENANTA PHARMACEUTICALS, INC.
    Inventors: Yao-Ling Qiu, Hui Cao, Xiaowen Peng, Zhigang Chen, Yat Sun Or
  • Patent number: 8859512
    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: November 30, 2012
    Date of Patent: October 14, 2014
    Assignees: University College Cardiff Consultants Limited, K.U. Leuven Research and Development
    Inventors: Christopher McGuigan, Jan Balzarini, Marco Migliore
  • Patent number: 8859513
    Abstract: The invention relates to the novel use of 1-beta-D-ribofuranosyl-1H-1,2,4-triazole-3-carboxamide for the treatment of infectious salmon anaemia caused by the infectious salmon anaemia or ISA virus in salmonids.
    Type: Grant
    Filed: June 8, 2010
    Date of Patent: October 14, 2014
    Assignee: Laboratorio de Diagnostico Gam, S.A.
    Inventors: Ana Maria Sandino, Geraldine Mlynarz Zylberberg, Matilde Jashes Morgues, Eugenio Spencer Ossa
  • Patent number: 8859502
    Abstract: Provided are methods for treating MLL-rearranged ALL by administering to a patient an HDAC inhibitor alone or in combination with a DNA demethylating agent. Also provided are methods of treating MLL-rearranged infant ALL. Methods of treating cells by these agents are also provided. Additionally, disclosed is a method for screening for compounds capable to treat MLL-rearranged ALL, in particular, MLL-rearranged infant ALL. In one embodiment, the HDAC inhibitor is romidepsin.
    Type: Grant
    Filed: September 9, 2011
    Date of Patent: October 14, 2014
    Assignee: Celgene Corporation
    Inventors: Ronald Stam, Dominique J. P. M. Stumpel
  • Patent number: 8858939
    Abstract: The invention pertains to methods for treating ectopic pregnancy. More particularly, the present invention relates to methods for treating unruptured ectopic pregnancy using a non-surgical method comprising the administration of an EGFR inhibitor alone or in combination with an anti-metabolite e.g. methotrexate (MTX). The methodology is potentially applicable to treatment of unruptured ectopic pregnancies of all sizes.
    Type: Grant
    Filed: October 1, 2010
    Date of Patent: October 14, 2014
    Assignee: Monash University
    Inventors: Stephen Tong, Ulrika W. Nilsson, Terence Grant Johns
  • Publication number: 20140303112
    Abstract: The present invention relates to a method for treating disease or condition susceptible to amelioration by AMPK activators and compounds of formula which are useful to activate AMP-activated protein kinase (AMPK) and the use of the compounds in the prevention or treatment of disease, including pre-diabetes, type 2 diabetes, syndrome X, metabolic syndrome and obesity.
    Type: Application
    Filed: April 9, 2013
    Publication date: October 9, 2014
    Inventors: Han-Min CHEN, Cheng-Yi KUO, Chun-Fang HUANG, Jiun-Tsai LIN
  • Publication number: 20140301979
    Abstract: Described herein are 4-methyl-piperazine-1-carbothioic acid amide derivatives and analogs, as well as compositions containing the same, for the treatment or prophylaxis of viral infections and diseases associated therewith, particularly those viral infections and associated diseases caused by hemorrhagic fever viruses, such as Arenaviruses.
    Type: Application
    Filed: June 25, 2014
    Publication date: October 9, 2014
    Applicant: SIGA TECHNOLOGIES, INC.,
    Inventors: Sean M. AMBERG, Dongcheng DAI, Tove C. BOLKEN, Dennis E. HRUBY