Nitrogen Atoms Occupy 1 And 3- Positions Patents (Class 514/86)
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Publication number: 20100099645Abstract: 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: ApplicationFiled: May 23, 2006Publication date: April 22, 2010Inventors: Richard J. Wurtman, Ingrid Richardson
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Patent number: 7687480Abstract: 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: GrantFiled: October 26, 2007Date of Patent: March 30, 2010Assignee: The Regents of the University of CaliforniaInventors: Karl Y. Hostetler, James R. Beadle, Ganesh D. Kini
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Publication number: 20100074889Abstract: 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: ApplicationFiled: September 11, 2009Publication date: March 25, 2010Inventors: Yao-Ling Qiu, Ce Wang, Xiaowen Peng, Lu Ying, Yat Sun Or
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Publication number: 20100075914Abstract: 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: ApplicationFiled: April 17, 2009Publication date: March 25, 2010Inventors: Mary R. FLACK, Susan Marie CIOTTI, Tarek HAMOUDA, Joyce A. SUTCLIFFE, James R. Baker, JR.
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Publication number: 20100063004Abstract: This invention relates to a novel topical pharmaceutical composition. In particular, this invention is an overnight topical composition for treating cold sores.Type: ApplicationFiled: December 3, 2007Publication date: March 11, 2010Inventors: Ranjan Ray Chaudhuri, Satish Ramchandra Dipali, Phillip E. West
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Publication number: 20100022478Abstract: 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: ApplicationFiled: July 20, 2007Publication date: January 28, 2010Inventors: Thomas Lindhorst, Birgit Werner, Holger Bock
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Publication number: 20100009895Abstract: 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: ApplicationFiled: October 23, 2007Publication date: January 14, 2010Inventors: Thomas Lindhorst, Birgit Werner, Stefan Piper
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Patent number: 7642249Abstract: 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 obsType: GrantFiled: April 11, 2008Date of Patent: January 5, 2010Assignee: Aventis Pharmaceuticals Inc.Inventors: Beverly Langevin, Edward Orton, Daniel Sherer
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Publication number: 20090318386Abstract: 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: ApplicationFiled: August 27, 2009Publication date: December 24, 2009Inventors: Reiner Fischer, Christoph Erdelen, Thomas Bretschneider
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Publication number: 20090264339Abstract: 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: ApplicationFiled: November 3, 2008Publication date: October 22, 2009Applicant: TaiGen Biotechnology Co., Ltd.Inventors: Chi-Feng Yen, Cheng-Kung Hu, Chang-Pin Huang, Ying-Huey Huang, Gholam Hossein Hakimelahi, Chi-Hsin Richard King
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Patent number: 7605137Abstract: 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: GrantFiled: March 25, 2005Date of Patent: October 20, 2009Assignee: Vion Pharmaceuticals, Inc.Inventors: Ivan King, Mario Sznol, Michael Belcourt, Li-Mou Zheng
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Publication number: 20090215726Abstract: 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: ApplicationFiled: March 30, 2006Publication date: August 27, 2009Inventors: Karl Y. Hosterler, James R. Beadle, Hyunah Choo
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Publication number: 20090203647Abstract: 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: ApplicationFiled: January 22, 2009Publication date: August 13, 2009Applicant: DOW AGROSCIENCES LLCInventors: 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
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Publication number: 20090181931Abstract: 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: ApplicationFiled: January 16, 2008Publication date: July 16, 2009Applicant: ONCOLYS BIOPHARMA, INC.Inventors: Yasuo Urata, Masaaki Ouchi, Toshiyoshi Fujiwara
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Publication number: 20090156545Abstract: 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: ApplicationFiled: March 30, 2006Publication date: June 18, 2009Inventors: Karl Y. Hostetler, James R. Beadle, Jacqueline C. Ruiz
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Publication number: 20090143335Abstract: 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: ApplicationFiled: October 17, 2008Publication date: June 4, 2009Applicant: H. LUNDBECK A/SInventors: Mie Larsen, Carsten Uhd Nielsen, Birger Brodin Larsen, Rene Holm
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Publication number: 20090131372Abstract: 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: ApplicationFiled: June 24, 2008Publication date: May 21, 2009Inventors: James M. Chen, Xiaowu Chen, Aesop Cho, Lee S. Chong, Maria Fardis, Thorsten Kirschberg, Steven Krawczyk, Hyung-Jung Pyun, William J. Watkins
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Publication number: 20090105147Abstract: 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: ApplicationFiled: October 17, 2008Publication date: April 23, 2009Applicant: Concert Pharmaceuticals Inc.Inventor: Craig E. Masse
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Publication number: 20090099136Abstract: 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: ApplicationFiled: October 15, 2008Publication date: April 16, 2009Applicant: PHARMASSET, INC.Inventors: MICHAEL JOSEPH SOFIA, PEIYUAN WANG, SUGUNA H. RACHAKONDA, JINFA DU
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Publication number: 20090099135Abstract: 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: ApplicationFiled: January 16, 2008Publication date: April 16, 2009Applicant: TyraTech, Inc.Inventor: Essam Enan
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Patent number: 7511027Abstract: 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: GrantFiled: November 22, 2002Date of Patent: March 31, 2009Assignees: 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
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Publication number: 20090075939Abstract: 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: ApplicationFiled: June 26, 2008Publication date: March 19, 2009Inventors: Gong-Xin He, Choung U. Kim, Michael L. Mitchell, Lianhong Xu
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Publication number: 20090062237Abstract: 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: ApplicationFiled: June 13, 2008Publication date: March 5, 2009Applicant: Mayo Foundation for Medical Education and ResearchInventors: Roshini Sarah Abraham, Vijay Nandakumar
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Publication number: 20090023685Abstract: 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: ApplicationFiled: July 4, 2008Publication date: January 22, 2009Inventors: B. Louise Giles, Blair Seifert
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Publication number: 20090005334Abstract: 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: ApplicationFiled: February 19, 2008Publication date: January 1, 2009Applicant: Bio-Rad Laboratories Inc.Inventor: David Segev
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Publication number: 20080312189Abstract: 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: ApplicationFiled: March 4, 2005Publication date: December 18, 2008Applicant: EISAI CO., LTD.Inventor: Raymond Pratt
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Patent number: 7465734Abstract: 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: GrantFiled: February 20, 2001Date of Patent: December 16, 2008Assignee: Celmed Oncology (USA), Inc.Inventor: H. Michael Shepard
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Publication number: 20080293648Abstract: 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: ApplicationFiled: December 19, 2007Publication date: November 27, 2008Applicant: Saha Pharmaceuticals, Inc.Inventor: Jayanta Saha
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Publication number: 20080286230Abstract: 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: ApplicationFiled: December 27, 2007Publication date: November 20, 2008Inventors: Jean-Pierre Sommadossi, Gilles Gosselin, Claire Pierra, Christian Perigaud, Suzanne Peyrottes
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Publication number: 20080269170Abstract: 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: ApplicationFiled: January 9, 2008Publication date: October 30, 2008Applicant: sanofi-aventisInventors: Michael Bosch, Monsif Bouaboula, Pierre Casellas, Samir Jegham, Serge Mignani, Jean-Flaubert Nguefack, Jacob-Alsboek Olsen, Bernard Tonnerre, Jean Wagnon
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Publication number: 20080249066Abstract: 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: ApplicationFiled: March 24, 2008Publication date: October 9, 2008Applicant: ARDEA BIOSCIENCES, INC.Inventors: Barry D. Quart, Zhi Hong
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Publication number: 20080221061Abstract: 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: ApplicationFiled: December 15, 2005Publication date: September 11, 2008Applicant: The Regents of The University of CaliforniaInventors: Karl Y. Hostetler, Beadle R. James
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Patent number: 7419967Abstract: 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: GrantFiled: August 25, 2005Date of Patent: September 2, 2008Assignee: Vertex Pharmaceuticals IncorporatedInventors: Michael R Hale, Clarence W Andrews, III, Eric S Furfine, Ronald G Sherrill, Andrew Spaltenstein, Gregory T Lowen
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Publication number: 20080207554Abstract: 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: ApplicationFiled: January 30, 2008Publication date: August 28, 2008Applicant: Alios BioPharma, Inc.Inventors: Leonid Beigelman, Lawrence M. Blatt, Harri Lonnberg
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Publication number: 20080153783Abstract: 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: ApplicationFiled: November 1, 2005Publication date: June 26, 2008Applicant: GILEAD SCIENCES, INC.Inventors: Haolun Jin, Choung U. Kim
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Publication number: 20080145349Abstract: 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: ApplicationFiled: February 6, 2008Publication date: June 19, 2008Inventors: Kazuyuki Sakata, Masayuki Morimoto, Hiroshi Kodama, Tetsuyosi Nishimatsu
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Publication number: 20080132470Abstract: 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: ApplicationFiled: October 31, 2007Publication date: June 5, 2008Inventors: Michael Frank Treacy, Raymond Frank Borysewicz, Kurt Allen Schwinghammer, Paul E. Rensner, Hassan Oloumi-Sadeghi
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Publication number: 20080076740Abstract: 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: ApplicationFiled: July 27, 2006Publication date: March 27, 2008Inventors: Zhenhong R. Cai, Salman Y. Jabri, Haolun Jin, Choung U. Kim, Samuel E. Metobo, Michael R. Mish, Richard M. Pastor
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Patent number: 7273856Abstract: 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: GrantFiled: October 28, 2002Date of Patent: September 25, 2007Assignee: 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
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Patent number: 7208481Abstract: 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: GrantFiled: February 14, 2003Date of Patent: April 24, 2007Assignee: 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
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Patent number: 7129227Abstract: 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: GrantFiled: October 4, 1999Date of Patent: October 31, 2006Assignees: Wake Forest University, University of North Carolina at Chapel HillInventors: Louis S. Kucera, Susan L. Morris-Natschke, Khalid S. Ishaq
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Patent number: 7115592Abstract: 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: GrantFiled: June 16, 2004Date of Patent: October 3, 2006Assignees: Institute of Organic Chemistry, Biochemistry of the Academy of Sciences of the Czech RepublicInventors: Jan M. R. Balzarini, Erik D. A. De Clercq, Antonin Holy, Dana Hockova
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Patent number: 7071176Abstract: 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: GrantFiled: December 1, 2003Date of Patent: July 4, 2006Assignee: Parker Hughes InstituteInventors: Faith M. Uckun, Rakesh Vig
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Patent number: 7018989Abstract: 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: GrantFiled: August 12, 2002Date of Patent: March 28, 2006Assignee: University College Cardiff Consultants, LTDInventors: Christopher McGuigan, Jan Balzarini
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Patent number: 6936602Abstract: 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: GrantFiled: June 15, 2000Date of Patent: August 30, 2005Assignee: Takeda Chemical Industries, Ltd.Inventors: Mitsuru Shiraishi, Masanori Baba, Yoshio Aramaki, Naoyuki Kanzaki, Osamu Nishimura
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Patent number: 6919322Abstract: Novel FBPase inhibitors of the formula I are useful in the treatment of diabetes and other conditions associated with elevated blood glucose.Type: GrantFiled: March 7, 2001Date of Patent: July 19, 2005Assignee: Metabasis Therapeutics, Inc.Inventors: Brett C. Bookser, Qun Dang, K. Raja Reddy
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Patent number: 6878697Abstract: 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: GrantFiled: June 21, 2002Date of Patent: April 12, 2005Assignee: Ariad Pharmaceuticals, Inc.Inventors: Chester A. Metcalf, III, William C. Shakespeare, Tomi K. Sawyer, Yihan Wang, Regine Bohacek
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Patent number: 6835386Abstract: 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: GrantFiled: October 18, 2002Date of Patent: December 28, 2004Assignee: Pfizer Inc.Inventor: Luis Gutierrez
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Patent number: 6818633Abstract: 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: GrantFiled: June 28, 2002Date of Patent: November 16, 2004Assignees: 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
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Patent number: 6812247Abstract: 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: GrantFiled: September 30, 2002Date of Patent: November 2, 2004Assignee: Academia SinicaInventors: Kuang-Lieh Lu, Jih-Ru Hwu, Shwu-Chen Tsay, Sheng-Fa Yu, Jui-Te Hung, Jiann-Jyh Huang