Nitrogen Atoms Occupy 1 And 3- Positions Patents (Class 514/86)
  • Publication number: 20100099645
    Abstract: This invention provides methods of increasing or enhancing the synthesis and levels of phospholipids, synapses, synaptic proteins, and synaptic membranes by a neural cell or brain cell; methods of treating a subject with a memory disorder, memory impairment, neurological disorder, or brain disease or disorder, comprising administering to the subject a composition comprising an omega-3 fatty acid, an omega-6 fatty acid, uridine, a metabolic precursor thereof, or a combination thereof.
    Type: Application
    Filed: May 23, 2006
    Publication date: April 22, 2010
    Inventors: Richard J. Wurtman, Ingrid Richardson
  • Patent number: 7687480
    Abstract: The present invention relates to phosphonate compounds, compositions containing them, processes for obtaining them, and their use for treating a variety of medical disorders, e.g., osteoporosis and other disorders of bone metabolism, cancer, viral infections, and the like.
    Type: Grant
    Filed: October 26, 2007
    Date of Patent: March 30, 2010
    Assignee: The Regents of the University of California
    Inventors: Karl Y. Hostetler, James R. Beadle, Ganesh D. Kini
  • Publication number: 20100074889
    Abstract: The present invention discloses compounds of formula (I), or its ?-L enantiomer, or a pharmaceutically acceptable salt, ester, stereoisomer, tautomer, solvate, prodrug, or combination thereof: which inhibit, preventing or treating abnormal cellular proliferation and/or a viral infection, particularly by HIV, HCV or HBV. Consequently, the compounds of the present invention interfere with the replication cycle of a virus and are also useful as antiviral agents, or interfere with host cellular biochemical process and are also useful as antiproliferative agents. The present invention further relates to pharmaceutical compositions comprising the aforementioned compounds for administration to a subject suffering from viral infection and/or cell proliferation. The invention also relates to methods of treating a viral infection and/or cell proliferation in a subject by administering a pharmaceutical composition comprising the compounds of the present invention.
    Type: Application
    Filed: September 11, 2009
    Publication date: March 25, 2010
    Inventors: Yao-Ling Qiu, Ce Wang, Xiaowen Peng, Lu Ying, Yat Sun Or
  • Publication number: 20100075914
    Abstract: The present invention relates to methods for treating, killing, and/or inhibiting the growth of Herpes viruses in human subjects comprising topically administering to a human subject in need thereof a nanoemulsion composition having antiviral properties.
    Type: Application
    Filed: April 17, 2009
    Publication date: March 25, 2010
    Inventors: Mary R. FLACK, Susan Marie CIOTTI, Tarek HAMOUDA, Joyce A. SUTCLIFFE, James R. Baker, JR.
  • Publication number: 20100063004
    Abstract: This invention relates to a novel topical pharmaceutical composition. In particular, this invention is an overnight topical composition for treating cold sores.
    Type: Application
    Filed: December 3, 2007
    Publication date: March 11, 2010
    Inventors: Ranjan Ray Chaudhuri, Satish Ramchandra Dipali, Phillip E. West
  • Publication number: 20100022478
    Abstract: The present invention relates to novel compounds that contain PNA units substituted with phosphonic acid ester functions or phosphonic acid functions, and have at least one chiral center. The compounds may be used for the treatment of viral diseases, such as AIDS.
    Type: Application
    Filed: July 20, 2007
    Publication date: January 28, 2010
    Inventors: Thomas Lindhorst, Birgit Werner, Holger Bock
  • Publication number: 20100009895
    Abstract: The present invention relates to novel methods for selective localization of active agents both at and in mitochondria within living cells, as well as corresponding active agents that penetrate through the cell membrane into the cells without further adjuvants and there can be localized both at and in mitochondria. These active agents are substituted with at least one monohydroxy mononitrophenyl rest or monohydroxy dinitrophenyl rest.
    Type: Application
    Filed: October 23, 2007
    Publication date: January 14, 2010
    Inventors: Thomas Lindhorst, Birgit Werner, Stefan Piper
  • Patent number: 7642249
    Abstract: The present invention is directed to dihydrogen phosphate salt 2-(3-{6-[2-(2,4-dichloro-phenyl)-ethylamino]-2-methoxy-pyrimidin-4-yl}-phenyl)-2-methyl-propionic acid of Formula (III), a pharmaceutical composition comprising a pharmaceutically effective amount of the compound of Formula (III), and a pharmaceutically acceptable carrier; and a method of treating a patient suffering from a PGD2-mediated disorder including, but not limited to, allergic disease (such as allergic rhinitis, allergic conjunctivitis, atopic dermatitis, bronchial asthma and food allergy), systemic mastocytosis, disorders accompanied by systemic mast cell activation, anaphylaxis shock, bronchoconstriction, bronchitis, urticaria, eczema, diseases accompanied by itch (such as atopic dermatitis and urticaria), diseases (such as cataract, retinal detachment, inflammation, infection and sleeping disorders) which is generated secondarily as a result of behavior accompanied by itch (such as scratching and beating), inflammation, chronic obs
    Type: Grant
    Filed: April 11, 2008
    Date of Patent: January 5, 2010
    Assignee: Aventis Pharmaceuticals Inc.
    Inventors: Beverly Langevin, Edward Orton, Daniel Sherer
  • Publication number: 20090318386
    Abstract: The invention relates to novel active compound combinations of certain cyclic ketoenols and certain active compounds that together have unexpectedly good insecticidal and acaricidal properties.
    Type: Application
    Filed: August 27, 2009
    Publication date: December 24, 2009
    Inventors: Reiner Fischer, Christoph Erdelen, Thomas Bretschneider
  • Publication number: 20090264339
    Abstract: This invention relates to heterocyclic compounds of the formulas shown in the specification. It also relates to methods for treating inflammatory diseases or immune diseases, developmental or degenerative diseases, and tissue injuries with one of the heterocyclic compounds.
    Type: Application
    Filed: November 3, 2008
    Publication date: October 22, 2009
    Applicant: TaiGen Biotechnology Co., Ltd.
    Inventors: Chi-Feng Yen, Cheng-Kung Hu, Chang-Pin Huang, Ying-Huey Huang, Gholam Hossein Hakimelahi, Chi-Hsin Richard King
  • Patent number: 7605137
    Abstract: This invention provides a method for treating tumor in a subject comprising administering to the subject an effective amount of: (1) VNP40101M, or its equivalent; and (2) a nucleoside, or a nucleoside analog. This invention also provides a method for inhibiting tumor cell growth comprising contacting the tumor cell with effective amounts of: (1) VNP40101M, or its equivalent; and (2) a nucleoside, or a nucleoside analog. The present invention relates to the treatment of cancer, comprising administering to a subject in need thereof an effective amount of VNP40101M in combination with a nucleoside.
    Type: Grant
    Filed: March 25, 2005
    Date of Patent: October 20, 2009
    Assignee: Vion Pharmaceuticals, Inc.
    Inventors: Ivan King, Mario Sznol, Michael Belcourt, Li-Mou Zheng
  • Publication number: 20090215726
    Abstract: Compounds and compositions are provided for treatment, prevention, or amelioration of a variety of medical disorders associated with viral infections and/or cell proliferation. The compounds provided herein are 5-phosphono-pent-2-en-1-yl nucleosides and esters thereof.
    Type: Application
    Filed: March 30, 2006
    Publication date: August 27, 2009
    Inventors: Karl Y. Hosterler, James R. Beadle, Hyunah Choo
  • Publication number: 20090203647
    Abstract: This present disclosure is related to the field of 5-fluoro pyrimidines and their derivatives and to the use of these compounds as fungicides.
    Type: Application
    Filed: January 22, 2009
    Publication date: August 13, 2009
    Applicant: DOW AGROSCIENCES LLC
    Inventors: Zoltan L. Benko, Timothy Boebel, Nneka T. Breaux, Kristy Bryan, George E. Davis, Jeffrey B. Epp, Beth Lorsbach, Timothy P. Martin, Kevin G. Meyer, Bassam S. Nader, W. J. Owen, Mark A. Pobanz, James M. Ruiz, Frisby D. Smith, Michael T. Sullenberger, Jeffery D. Webster, Chenglin Yao, David H. Young
  • Publication number: 20090181931
    Abstract: The present invention relates to pyrimidine compounds and their use as pharmacologically active agents capable of suppressing and inhibiting viruses (e.g., oncolytic viruses). The subject compounds and compositions are particularly useful in treating and suppressing human oncolytic adenovirus infection.
    Type: Application
    Filed: January 16, 2008
    Publication date: July 16, 2009
    Applicant: ONCOLYS BIOPHARMA, INC.
    Inventors: Yasuo Urata, Masaaki Ouchi, Toshiyoshi Fujiwara
  • Publication number: 20090156545
    Abstract: Compounds and compositions are provided for treatment, prevention, or amelioration of a variety of medical disorders associated with viral infections and/or cell proliferation. The compounds provided herein are obtained by attaching the phosphonate nucleoside of interest to alkyloxyalkyl-phosphate or alkyl-phosphate in a phosphate-phosphono anhydride linkage to provide a modified nucleoside phosphonate drug.
    Type: Application
    Filed: March 30, 2006
    Publication date: June 18, 2009
    Inventors: Karl Y. Hostetler, James R. Beadle, Jacqueline C. Ruiz
  • Publication number: 20090143335
    Abstract: The present invention relates to a pharmaceutical composition comprising gaboxadol or a pharmaceutically acceptable salt thereof and one or more inhibitors of PAT1 and/or one or more inhibitors of OAT. The present invention further relates to a pharmaceutical composition comprising from about 0.5 mg to about 50 mg gaboxadol or a pharmaceutically acceptable salt thereof, wherein the composition provides an in vivo plasma profile comprising a mean Tmax which is longer than about 20 minutes.
    Type: Application
    Filed: October 17, 2008
    Publication date: June 4, 2009
    Applicant: H. LUNDBECK A/S
    Inventors: Mie Larsen, Carsten Uhd Nielsen, Birger Brodin Larsen, Rene Holm
  • Publication number: 20090131372
    Abstract: The invention is related to phosphorus substituted compounds with activity for treating metabolic diseases and/or disorders, e.g., diabetes and hypercholesterolemia, compositions containing such compounds, and therapeutic methods that include the administration of such compounds, as well as to processes and intermediates useful for preparing such compounds.
    Type: Application
    Filed: June 24, 2008
    Publication date: May 21, 2009
    Inventors: James M. Chen, Xiaowu Chen, Aesop Cho, Lee S. Chong, Maria Fardis, Thorsten Kirschberg, Steven Krawczyk, Hyung-Jung Pyun, William J. Watkins
  • Publication number: 20090105147
    Abstract: This disclosure relates to novel di-aryl-pyrimidine (DAPY) compounds and pharmaceutically acceptable salts thereof. This disclosure also provides compositions comprising a compound of this disclosure and the use of such compositions in methods of treating diseases and conditions that are beneficially treated by administering a non-nucleoside reverse transcriptase inhibitor (NNRTI).
    Type: Application
    Filed: October 17, 2008
    Publication date: April 23, 2009
    Applicant: Concert Pharmaceuticals Inc.
    Inventor: Craig E. Masse
  • Publication number: 20090099136
    Abstract: Disclosed are dioxolane thymine phosphoramidate compounds, compositions, and methods for using dioxolane thymine phosphoramidate compounds and compositions to treat viral infections, such as HIV infections.
    Type: Application
    Filed: October 15, 2008
    Publication date: April 16, 2009
    Applicant: PHARMASSET, INC.
    Inventors: MICHAEL JOSEPH SOFIA, PEIYUAN WANG, SUGUNA H. RACHAKONDA, JINFA DU
  • Publication number: 20090099135
    Abstract: Embodiments of the present invention provide compositions for controlling a target pest including a pest control product and at least one active agent, wherein: the active agent can be capable of interacting with a receptor in the target pest; the pest control product can have a first activity against the target pest when applied without the active agent and the compositions can have a second activity against the target pest; and the second activity can be greater than the first activity.
    Type: Application
    Filed: January 16, 2008
    Publication date: April 16, 2009
    Applicant: TyraTech, Inc.
    Inventor: Essam Enan
  • Patent number: 7511027
    Abstract: A method for the treatment for hepatitis delta infection in a host, that includes administering an effective amount of a nucleoside or a nucleoside analog that suppresses the expression of the hepatitis B surface or preS1 antigen in the host 100-fold or more relative to pretreatment values in vivo; or to not more than 1 microgram per milliliter in vivo. In a preferred embodiment, the nucleoside is L-FMAU, or a pharmaceutically acceptable salt or prodrug thereof.
    Type: Grant
    Filed: November 22, 2002
    Date of Patent: March 31, 2009
    Assignees: Georgetown University, University of Georgia Research Foundation, Inc.
    Inventors: John L. Casey, Brent E. Korba, Paul J. Cote, John L. Gerin, Bud C. Tennant, Chung K. Chu
  • Publication number: 20090075939
    Abstract: The invention is related to compounds of Formula (I): or a pharmaceutically acceptable salt, solvate, ester, and/or phosphonate thereof, compositions containing such compounds, and therapeutic methods that include the administration of such compounds.
    Type: Application
    Filed: June 26, 2008
    Publication date: March 19, 2009
    Inventors: Gong-Xin He, Choung U. Kim, Michael L. Mitchell, Lianhong Xu
  • Publication number: 20090062237
    Abstract: This document relates to methods and materials involved in evaluating immune competence in a subject. For example, methods and materials for evaluating immune competence in a subject to BK virus (BKV) are provided. Also provided are isolated peptides, compositions, and methods useful for evaluating whether or not a subject is BKV immunocompetent. Also provided are methods for treating BK virus nephropathy in a subject that is BKV immune incompetent.
    Type: Application
    Filed: June 13, 2008
    Publication date: March 5, 2009
    Applicant: Mayo Foundation for Medical Education and Research
    Inventors: Roshini Sarah Abraham, Vijay Nandakumar
  • Publication number: 20090023685
    Abstract: A solution of 2.5-20% cidofovir is administered as droplets having a mean size of about 1 micron to about 20 microns either nebulized or as a spray to an individual having recurrent respiratory papillomatosis.
    Type: Application
    Filed: July 4, 2008
    Publication date: January 22, 2009
    Inventors: B. Louise Giles, Blair Seifert
  • Publication number: 20090005334
    Abstract: A compound which comprises a backbone having a plurality of chiral carbon atoms, the backbone bearing a plurality of ligands each being individually bound to a chiral carbon atom of the plurality of chiral carbon atoms, the ligands including one or more pair(s) of adjacent ligands each containing a moiety selected from the group consisting of a naturally occurring nucleobase and a nucleobase binding group, wherein moieties of the one or more pair(s) are directly linked to one another via a linker chain; building blocks for synthesizing the compound; and uses of the compound, particularly in antisense therapy.
    Type: Application
    Filed: February 19, 2008
    Publication date: January 1, 2009
    Applicant: Bio-Rad Laboratories Inc.
    Inventor: David Segev
  • Publication number: 20080312189
    Abstract: The invention provides methods for treating and/or preventing cerebral autosomal dominant arteriopathy with subcortical infarcts and leukoencephalopathy (CADASIL) in a patient in need thereof by administering a therapeutically effective amount of at least one cholinesterase inhibitor. The invention also provides methods for treating and/or preventing neurovascular diseases caused by one or more mutations of the human Notch3 gene by administering a therapeutically effective amount of at least one cholinesterase inhibitor. In one embodiment, the cholinesterase inhibitor is donepezil, a stereoisomer thereof and/or a pharmaceutically acceptable salt thereof.
    Type: Application
    Filed: March 4, 2005
    Publication date: December 18, 2008
    Applicant: EISAI CO., LTD.
    Inventor: Raymond Pratt
  • Patent number: 7465734
    Abstract: This invention provides a method for identifying potential therapeutic agents by contacting a target cell with a candidate therapeutic agent which is a selective substrate for an endogenous, intracellular enzyme in the cell which is enhanced in its expression as a result of selection by biologic or chemotherapy. This invention also provides methods and examples of molecules for selectively killing a pathological cell by contacting the cell with a prodrug that is a selective substrate for an endogenous, intracellular enzyme. The prodrug is subsequently converted to a cellular toxin. Further provided by this invention is a method for treating a pathology characterized by pathological, hyperproliferative cells in a subject by administering to the subject a prodrug that is a selective substrate for an endogenous, overexpressed, intracellular enzyme, and converted by the enzyme to a cellular toxin in the hyperproliferative cell.
    Type: Grant
    Filed: February 20, 2001
    Date of Patent: December 16, 2008
    Assignee: Celmed Oncology (USA), Inc.
    Inventor: H. Michael Shepard
  • Publication number: 20080293648
    Abstract: This invention provides methods, novel formulations and kits to reduce the toxicity of anticancer drugs. Disclosed are therapeutics and treatment methods employing anticancer drags that exhibit a known toxicity, including, for example, adriamycin, campthothecin, and the like, chemically linked to a phosphonoformic acid partial ester resulting in a novel formulation that significantly decreases drug-related toxicity, enhances synergy with other chemotherapeutic drugs and provides increased efficacy against drug-resistant cancers.
    Type: Application
    Filed: December 19, 2007
    Publication date: November 27, 2008
    Applicant: Saha Pharmaceuticals, Inc.
    Inventor: Jayanta Saha
  • Publication number: 20080286230
    Abstract: Provided herein are compounds, compositions and methods for the treatment of liver disorder, including HCV and/or HBV infections. Specifically, compound and compositions of nucleoside derivatives are disclosed, which can be administered either alone or in combination with other anti-viral agents.
    Type: Application
    Filed: December 27, 2007
    Publication date: November 20, 2008
    Inventors: Jean-Pierre Sommadossi, Gilles Gosselin, Claire Pierra, Christian Perigaud, Suzanne Peyrottes
  • Publication number: 20080269170
    Abstract: The disclosure relates to compounds of formula (I): wherein R1-R5, A and Y are as defined in the disclosure, to compositions comprising said compounds, and to processes for making and methods of using the same.
    Type: Application
    Filed: January 9, 2008
    Publication date: October 30, 2008
    Applicant: sanofi-aventis
    Inventors: Michael Bosch, Monsif Bouaboula, Pierre Casellas, Samir Jegham, Serge Mignani, Jean-Flaubert Nguefack, Jacob-Alsboek Olsen, Bernard Tonnerre, Jean Wagnon
  • Publication number: 20080249066
    Abstract: Described herein are compounds useful in the treatment of viral diseases, compositions comprising them and methods of using them. The compounds comprise a nucleoside or nucleoside analog linked, commonly through a phosphate group to one of a selected group of lipids. In some embodiments, the compounds described herein are useful for treating HIV infection, AIDS and other viral infections.
    Type: Application
    Filed: March 24, 2008
    Publication date: October 9, 2008
    Applicant: ARDEA BIOSCIENCES, INC.
    Inventors: Barry D. Quart, Zhi Hong
  • Publication number: 20080221061
    Abstract: Methods and compositions are provided for treating lung diseases, including but not limited to infections and small cell and non-small cell lung cancer, by conjugating a drug of interest to glycerol ethers or glycerol phosphate ethers.
    Type: Application
    Filed: December 15, 2005
    Publication date: September 11, 2008
    Applicant: The Regents of The University of California
    Inventors: Karl Y. Hostetler, Beadle R. James
  • Patent number: 7419967
    Abstract: The present invention relates to a novel class of sulfonamides which are aspartyl protease inhibitors. In one embodiment, this invention relates to a novel class of HIV aspartyl protease inhibitors characterized by specific structural and physicochemical features. This invention also relates to pharmaceutical compositions comprising these compounds. The compounds and pharmaceutical compositions of this invention are particularly well suited for inhibiting HIV-1 and HIV-2 protease activity and consequently, may be advantageously used as anti-viral agents against the HIV-1 and HIV-2 viruses. This invention also relates to methods For inhibiting the activity of HIV aspartyl protease using the compounds of this invention and methods for screening compounds for anti-HIV activity.
    Type: Grant
    Filed: August 25, 2005
    Date of Patent: September 2, 2008
    Assignee: Vertex Pharmaceuticals Incorporated
    Inventors: Michael R Hale, Clarence W Andrews, III, Eric S Furfine, Ronald G Sherrill, Andrew Spaltenstein, Gregory T Lowen
  • Publication number: 20080207554
    Abstract: This invention relates to the fields of organic chemistry, pharmaceutical chemistry, biochemistry, molecular biology and medicine. In particular it relates to compounds that activate RNaseL, and to the use of the compounds for treating and/or ameliorating a disease or a condition, such as a viral infection.
    Type: Application
    Filed: January 30, 2008
    Publication date: August 28, 2008
    Applicant: Alios BioPharma, Inc.
    Inventors: Leonid Beigelman, Lawrence M. Blatt, Harri Lonnberg
  • Publication number: 20080153783
    Abstract: Pyrimidine I and pyrimidinone II phosphonate compounds and methods for viral inhibition are disclosed. The compounds include at least one phosphonate group covalently attached at any site.
    Type: Application
    Filed: November 1, 2005
    Publication date: June 26, 2008
    Applicant: GILEAD SCIENCES, INC.
    Inventors: Haolun Jin, Choung U. Kim
  • Publication number: 20080145349
    Abstract: The present invention relates to a composition for noxious organisms-controlling agent having a synergistic effect and a method for using said composition, which comprises, as active ingredients thereof, one or more compounds selected from the phthalamide derivatives represented by general formula (I) being useful as an insecticide or acaricide and one or more compounds selected from the compounds having insecticidal, acaricidal or nematocidal activity: wherein R1, R2 and R3 may be the same or different and each represent hydrogen atom, C3-C6 cycloalkyl, -A1-Qp, etc., each of X and Y may be the same or different and represents hydrogen atom, halogen atom, etc., n is an integer of 1 to 4, m is an integer of 1 to 5, and each of Z1 and Z2 represents O or S.
    Type: Application
    Filed: February 6, 2008
    Publication date: June 19, 2008
    Inventors: Kazuyuki Sakata, Masayuki Morimoto, Hiroshi Kodama, Tetsuyosi Nishimatsu
  • Publication number: 20080132470
    Abstract: The present invention provides a synergistic insecticidal composition comprising as essential active ingredients a neuronal sodium channel antagonist in combination with one or more compounds selected from the group consisting of pyrethroids, pyrethroid-type compounds, recombinant nucleopolyhedroviruses capable of expressing an insect toxin, organophosphates, carbamates, formamidines, macrocyclic lactones, amidinohydrazones, GABA antagonists and acetylcholine receptor ligands. Also provided are methods for synergistic insect control and crop protection.
    Type: Application
    Filed: October 31, 2007
    Publication date: June 5, 2008
    Inventors: Michael Frank Treacy, Raymond Frank Borysewicz, Kurt Allen Schwinghammer, Paul E. Rensner, Hassan Oloumi-Sadeghi
  • Publication number: 20080076740
    Abstract: The invention is related to phosphorus substituted anti-viral inhibitory compounds, compositions containing such compounds, and therapeutic methods that include the administration of such compounds, as well as to processes and intermediates useful for preparing such compounds.
    Type: Application
    Filed: July 27, 2006
    Publication date: March 27, 2008
    Inventors: Zhenhong R. Cai, Salman Y. Jabri, Haolun Jin, Choung U. Kim, Samuel E. Metobo, Michael R. Mish, Richard M. Pastor
  • Patent number: 7273856
    Abstract: Described herein are compounds of formula (I) useful as antagonists of tachykinins in general, and in particular of neurokinin A; and the pharmaceutical formulations comprising the compounds of formula (I)
    Type: Grant
    Filed: October 28, 2002
    Date of Patent: September 25, 2007
    Assignee: Menarini Ricerche S.P.A.
    Inventors: Alessandro Sisto, Valerio Caciagli, Maria Altamura, Alessandro Giolitti, Valentina Fedi, Antonio Guidi, Danilo Giannotti, Nicholas Harmat, Rossano Nannicini, Franco Pasqui, Carlo Alberto Maggi
  • Patent number: 7208481
    Abstract: The present invention relates to methods of use of aminodiphosphonate to modulate apolipoprotein E levels and the use of such compounds in therapy, including cardiovascular and neurological disease states.
    Type: Grant
    Filed: February 14, 2003
    Date of Patent: April 24, 2007
    Assignee: ILEX Products, Inc.
    Inventors: Hieu Trung Phan, Lân Mong Nguyen, Raymond Azoulay, Vinh Van Diep, Eric Joseph Niesor, Craig Leigh Bentzen, Yves Gyon Gellin, Anne Perez, Jean-Luc Thulliard
  • Patent number: 7129227
    Abstract: A method of treating viral infections, and in particular HIV-1, hepatitis B virus, and herpesviruses, is disclosed. The method comprises administering to a subject in need of such treatment an infection-combating amount of a phospholipid or phospholipid derivative.
    Type: Grant
    Filed: October 4, 1999
    Date of Patent: October 31, 2006
    Assignees: Wake Forest University, University of North Carolina at Chapel Hill
    Inventors: Louis S. Kucera, Susan L. Morris-Natschke, Khalid S. Ishaq
  • Patent number: 7115592
    Abstract: Novel compounds are provided having formula (I) where R1, R2, R3, R4, Z, X and * are defined herein. Also provided are antiviral methods for use and processes for synthesis of the compounds of formula (I).
    Type: Grant
    Filed: June 16, 2004
    Date of Patent: October 3, 2006
    Assignees: Institute of Organic Chemistry, Biochemistry of the Academy of Sciences of the Czech Republic
    Inventors: Jan M. R. Balzarini, Erik D. A. De Clercq, Antonin Holy, Dana Hockova
  • Patent number: 7071176
    Abstract: Aryl phosphate derivatives of d4T with para-bromo substitution on the aryl group show markedly increased potency as anti-HIV agents without undesirable levels of cytotoxic activity. In particular, these derivatives are potent inhibitors of HIV reverse transcriptase. In a preferred aspect of the present invention, the phosphorus of the aryl phosphate group is further substituted with an amino acid residue that may be esterified or substituted, such as a methoxy alaninyl group.
    Type: Grant
    Filed: December 1, 2003
    Date of Patent: July 4, 2006
    Assignee: Parker Hughes Institute
    Inventors: Faith M. Uckun, Rakesh Vig
  • Patent number: 7018989
    Abstract: Aryl substituted phosphoryl derivatives of the formula In which Ar is phenyl, naphthyl, or pyridyl, Y is O or S, X1 is O, NR3, S, CR3R4, CR3W1 or CW1W2, X2 and X6 are a bond or X6 is CH2 and X2 is O, NR3, S, CR3R4, CR3W1 or CW1W2, R3 and R4 are H, alkyl or phenyl, groups, W1 and W2 are heteroatoms, X3 is alkylene, X4 is oxygen or CH2, X5 is a bond or CH2, Z is O, NR5, S, alkyl or phenyl, R5 is H, alkyl or phenyl, J is H, alkyl, phenyl, or a heterocyclic or polycyclic group, Q is O, NR6, S, CR6R7, CR6W3 or CW3W4, R6 and R7 are H, alkyl or phenyl, and W3 and W4 are hetero atoms, T1 and T2 are H or CH2R8, R8 is H, OH or F, or T1 and T2 together are —CH?CH— or —C(R9)(R10)C(R11)(R12)—, R9 is H, halogeno, CN, NH2, CO-alkyl, or alkyl, R10, R11, and R12 are H, N3, halogen, CN, NH2, CO-alkyl, or alkyl, and B is a purine or pyrimidine base, have antiviral activity, as for example against HIV. Particularly preferred are thymine and adenine derivatives of amino acid phenoxyphosphoroamidates.
    Type: Grant
    Filed: August 12, 2002
    Date of Patent: March 28, 2006
    Assignee: University College Cardiff Consultants, LTD
    Inventors: Christopher McGuigan, Jan Balzarini
  • Patent number: 6936602
    Abstract: Compounds of the general formula (I): or salts thereof, which exhibit CCR5 antagonism and exert preventive and therapeutic effects against HIV infections: wherein R1 is a 5- to 6-membered aromatic ring which bears a substituent represented by the general formula: R-Z1-X-Z2- (wherein R1 is hydrogen or optionally substituted hydrocarbyl; X is optionally substituted alkylene; and Z1 and Z2 are each a heteroatom) and may be further substituted, with R being optionally bonded to the aromatic ring to form another ring; Y is optionally substituted imino; and R2 and R3 are each optionally substituted aliphatic hydrocarbyl or an optionally Substituted hetero-alicyclic group.
    Type: Grant
    Filed: June 15, 2000
    Date of Patent: August 30, 2005
    Assignee: Takeda Chemical Industries, Ltd.
    Inventors: Mitsuru Shiraishi, Masanori Baba, Yoshio Aramaki, Naoyuki Kanzaki, Osamu Nishimura
  • Patent number: 6919322
    Abstract: Novel FBPase inhibitors of the formula I are useful in the treatment of diabetes and other conditions associated with elevated blood glucose.
    Type: Grant
    Filed: March 7, 2001
    Date of Patent: July 19, 2005
    Assignee: Metabasis Therapeutics, Inc.
    Inventors: Brett C. Bookser, Qun Dang, K. Raja Reddy
  • Patent number: 6878697
    Abstract: This invention relates to compounds of the general formula: in which RA, RB, RC, RD, w, x, y, and z are as defined herein, and to their preparation and use.
    Type: Grant
    Filed: June 21, 2002
    Date of Patent: April 12, 2005
    Assignee: Ariad Pharmaceuticals, Inc.
    Inventors: Chester A. Metcalf, III, William C. Shakespeare, Tomi K. Sawyer, Yihan Wang, Regine Bohacek
  • Patent number: 6835386
    Abstract: The present invention provides a device, preferably a collar or ear tag, capable of the controlled, sustained release of an effective amount of an active ingredient that can protect an animal against arthropod pests, comprising a reservoir containing a novel gel formulation comprising a fatty acid, an organic solvent which is a linear aliphatic ester, a silicone-based fluid, or a combination thereof, and an active ingredient that can protect the animal against one or more arthropod pests.
    Type: Grant
    Filed: October 18, 2002
    Date of Patent: December 28, 2004
    Assignee: Pfizer Inc.
    Inventor: Luis Gutierrez
  • Patent number: 6818633
    Abstract: Novel compounds are provided having formula (I) where R1, R2, R3, R4, Z, X and * are defined herein. Also provided are antiviral methods for use and processes for synthesis of the compounds of formula (I).
    Type: Grant
    Filed: June 28, 2002
    Date of Patent: November 16, 2004
    Assignees: Institute of Organic Chemistry and Biochemistry Academy of Sciences of the Czech Republic, Rega Stichting v.z.w.
    Inventors: Jan M. R. Balzarini, Erik D. A. De Clercq, Antonin Holy
  • Patent number: 6812247
    Abstract: A metal complex and its use for binding or cleaving a nucleic acid. The metal complex has the formula: M is Pt, Pd, Ni, Co, or Cu; X is aryl, heteroaryl, cyclyl, or heterocyclyl; Y is halogen, tosylate, mesylate, triflate, pyrophosphate, or carboxylate; each of A1 and A2, independently, is N or C; each of A3 and A4, independently, is N, S, or O, wherein A1, A2, A3, and A4 taken together have one positive charge; and each of R1 and R2, independently, is alkyl, aryl, heteroaryl, alkoxyl, aryloxyl, heteroaryloxyl, alkoxylcarbonyl, aryloxylcarbonyl, or heteroaryloxylcarbonyl.
    Type: Grant
    Filed: September 30, 2002
    Date of Patent: November 2, 2004
    Assignee: Academia Sinica
    Inventors: Kuang-Lieh Lu, Jih-Ru Hwu, Shwu-Chen Tsay, Sheng-Fa Yu, Jui-Te Hung, Jiann-Jyh Huang