Carbonyl, Thiocarbonyl, Additional Hetero Ring Or Nitrogen, Other Than As Nitro Or Nitroso, Attached Indirectly To The Sugar Ring By Acyclic Nonionic Bonding Patents (Class 536/27.23)
  • Patent number: 9029343
    Abstract: Disclosed are compounds, pharmaceutical compositions containing the compounds, and the uses of the compounds and compositions as modulators of histone methyltransferases, and for treating diseases influenced by modulation of histone methyltransferase activity.
    Type: Grant
    Filed: December 5, 2011
    Date of Patent: May 12, 2015
    Assignee: Epizyme, Inc.
    Inventors: Richard Chesworth, Kevin W. Kuntz, Edward J. Olhava, Michael A. Patane
  • Publication number: 20150050659
    Abstract: Protected fluorescent reagent compounds and their methods of synthesis are provided. The compounds are useful in various fluorescence-based analytical methods, including the analysis of highly multiplexed optical reactions in large numbers at high densities, such as single molecule real time nucleic acid sequencing reactions. The compounds contain fluorescent dye elements, that allow the compounds to be detected with high sensitivity at desirable wavelengths, binding elements, that allow the compounds to be recognized specifically by target biomolecules, and protective shield elements, that decrease undesirable contacts between the fluorescent dye elements and the bound target biomolecules and that therefore decrease photodamage of the bound target biomolecules by the fluorescent dye elements.
    Type: Application
    Filed: August 5, 2014
    Publication date: February 19, 2015
    Inventors: Lubomir SEBO, Jeremiah HANES, Gene SHEN, Louis BROGLEY, Stephen YUE, Frank ZHENG, Yuri LAPIN, John LYLE, Honey OSUNA, Andrei FEDOROV
  • Publication number: 20150005251
    Abstract: Disclosed herein are nucleosides, nucleotides and analogs thereof, pharmaceutical compositions that include one or more of nucleosides, nucleotides and analogs thereof, and methods of synthesizing the same. Also disclosed herein are methods of ameliorating and/or treating a paramyxovirus viral infection, with a nucleoside, a nucleotide and an analog thereof.
    Type: Application
    Filed: June 24, 2014
    Publication date: January 1, 2015
    Inventors: Natalia Dyatkina, Guangyi Wang, Leonid Beigelman, Vivek Kumar Rajwanshi
  • Publication number: 20140256668
    Abstract: The present disclosure relates to compounds of formula (I-A) using the compounds wherein Ring A and the variables X, Y, R3a, R3b, R3c, R3d, R4, R5, R5?, and m are defined herein, to pharmaceutical compositions comprising the compounds, and methods of using the compounds.
    Type: Application
    Filed: May 23, 2013
    Publication date: September 11, 2014
    Applicant: MILLENNIUM PHARMACEUTICALS, INC.
    Inventors: Stephen CRITCHLEY, Thomas G. Gant, Steven P. Langston, Edward J. Olhava, Stephane Peluso
  • Publication number: 20140100184
    Abstract: Structure and mechanism based design was used to design potent ribose containing inhibitors of DOT1L with IC50 values as low as 38 nM. These ribose containing inhibitors exhibit only weak or no activities against four other representative histone lysine and arginine methyltransferases, G9a, SUV39H1, PRMT1 and CARM1.
    Type: Application
    Filed: August 30, 2013
    Publication date: April 10, 2014
    Applicant: BAYLOR COLLEGE OF MEDICINE
    Inventors: Yongcheng SONG, Pinhong CHEN, Jiasheng DIAO, Gang CHENG, Lisheng DENG, Justin L. ANGLIN, Venkataram B.V. PRASAD, Yang YAO
  • Publication number: 20140051846
    Abstract: Disclosed are O-protected compounds of the formula (I): wherein B is an optionally protected nucleobase, and R1-R3 are as described herein, a method of preparing such compounds, and a method of preparing oligonucleotides such as RNA starting from such compounds. The O-protected compounds have one or more advantages, for example, the 2?-O-protected compound is stable during the various reaction steps involved in oligonucleotide synthesis; the protecting group can be easily removed after the synthesis of the oligonucleotide, for example, by reaction with tetrabutylammonium fluoride; and/or the O-protected groups do not generate DNA/RNA alkylating side products, which have been reported during removal of 2?-O-(2-cyanoethyl)oxymethyl or 2?-O-[2-(4-tolylsulfonyl)ethoxymethyl groups under similar conditions.
    Type: Application
    Filed: March 29, 2012
    Publication date: February 20, 2014
    Applicant: TheUnited ofAmerica,asrepresentedbythe Secre -tary,Department ofHealthand Human Service
    Inventors: Serge L. Beaucage, Jacek Cieslak
  • Publication number: 20130338094
    Abstract: The present disclosure relates to compounds of formula (I-A) using the compounds wherein Ring A and the variables X, Y, R3a, R3b, R3c, R3d, R4, R5, R5?, and m are defined herein, to pharmaceutical compositions comprising the compounds, and methods of using the compounds.
    Type: Application
    Filed: May 23, 2013
    Publication date: December 19, 2013
    Applicant: MILLENNIUM PHARMACEUTICALS, INC.
    Inventors: Stephen CRITCHLEY, Thomas G. Gant, Steven P. Langston, Edward J. Olhava, Stephane Peluso
  • Publication number: 20130310333
    Abstract: Disclosed are compounds, pharmaceutical compositions containing the compounds, and the uses of the compounds and compositions as modulators of histone methyltransferases, and for treating diseases influenced by modulation of histone methyltransferase activity.
    Type: Application
    Filed: December 5, 2011
    Publication date: November 21, 2013
    Applicant: EPIZYME, INC.
    Inventors: Richard Chesworth, Kevin Wayne Kuntz, Edward James Olhava, Michael A. Patane
  • Publication number: 20130210664
    Abstract: The present invention relates to immobilization compounds, immobilization products and preparations thereof as well as methods and uses for the identification of methyltransferase interacting compounds or for the purification or identification of methyltransferase proteins.
    Type: Application
    Filed: August 4, 2011
    Publication date: August 15, 2013
    Applicant: Cellzome AG
    Inventors: John Harrison, Glynn Addison, Nigel Ramsden, Gerard Drewes
  • Publication number: 20130203694
    Abstract: Rel proteins as a novel therapeutic agent for treating bacterial threats. More specifically, a novel class of compounds of Formula (I) as disclosed herein which possess anti-bacterial activity and which inhibit RelA, RelSeq or RelSpo synthetic activity or bacterial spore formation. Also, pharmaceutical compositions of such compounds and a method of combating bacteria, or treating bacterial infections, by administering to a subject in need thereof such compounds or pharmaceutical compositions.
    Type: Application
    Filed: August 3, 2011
    Publication date: August 8, 2013
    Applicant: YISSUM RESEARCH DEVELOPMENT CO. OF THE HEBREW UNIVERSITY OF JERUSALEM LTD.
    Inventors: Ezequiel Wexselblatt, Joshua Katzhendler, Gad Glaser, Sigal Ben Yehuda, Roee Vidavski, Hafiz Mawasi, Ilana Kaspy, Yaara Oppenheimer-Shaanan
  • Publication number: 20130203836
    Abstract: The present invention provides nucleosides of formula (1) and oligonucleotides comprising at least on nucleoside of formula (2):Formula (1) and Formula (2). Another aspect of the invention relates to a method of inhibiting the expression of a gene in call, the method comprising (a) contacting an oligonucleotide of the invention with the cell; and (b) maintaining the cell from step (a) for a time sufficient to obtain degradation of the mRNA of the target gene.
    Type: Application
    Filed: March 31, 2011
    Publication date: August 8, 2013
    Applicants: ISIS PHARMACEUTICALS, INC., ALNYLAM PHARMACEUTICALS, INC.
    Inventors: Kallanthottathil G. Rajeev, Muthiah Manoharan, Eric E. Swayze, Thazha P. Prakash
  • Publication number: 20130045475
    Abstract: This disclosure provides novel reversibly terminated ribonucleotides which can be used as a reagent for DNA sequencing reactions. Methods of sequencing nucleic acids using the disclosed nucleotides are also provided.
    Type: Application
    Filed: October 23, 2012
    Publication date: February 21, 2013
    Applicant: ALERE SAN DIEGO, INC.
    Inventor: Alere San Diego, Inc.
  • Publication number: 20130045942
    Abstract: The present invention provides N6-substituted adenosine derivatives and N6-substituted adenine derivatives, manufacturing methods thereof, a pharmaceutical composition comprising the said compounds above, and uses of these compounds in manufacturing medicaments and health-care products for treating insomnia, convulsion, epilepsy, and Parkinson's diseases, and preventing and treating dementia.
    Type: Application
    Filed: December 10, 2009
    Publication date: February 21, 2013
    Applicant: INSTITUTE OF MATERIA MEDICA, CHINESE ACADEMY OF MEDICAL SCIENCES
    Inventors: Jiangong Shi, Jianjun Zhang, Zhenggang Yue, Min Li, Chenggen Zhu, Ying Zhang, Jiachen Zi, Yafang Wang, Xiaona Fan, Ruiming Xu, Sheng Lin, Yan Li, Yongchun Yang, Li Sheng
  • Publication number: 20130040907
    Abstract: Described herein are compounds useful in the modulation of blood uric acid levels, formulations containing them and methods of making and using them. In some embodiments, the compounds described herein are used in the treatment or prevention of disorders related to aberrant levels of uric acid.
    Type: Application
    Filed: May 4, 2012
    Publication date: February 14, 2013
    Applicant: Ardea Biosciences Inc.
    Inventors: Esmir GUNIC, Jean-Luc GIRARDET, Jean-Michel VERNIER, Martina E. TEDDER, David A. PAISNER
  • Patent number: 8334364
    Abstract: [Problems] A derivative of a nucleic acid antimetabolite is demanded which can show a high therapeutic effect at a low dose. [Means For Solving Problems] Disclosed is a high molecular weight derivative of a nucleic acid antimetabolite, which is characterized by comprising a high molecular weight compound comprising a polyethylene glycol moiety and a polymer moiety having a carboxyl group in a side chain and a nucleoside derivative which can act as a nucleic acid antimetabolite, wherein the carboxyl group in the side chain is bound to a hydroxyl group in the nucleoside derivative via an ester bond. Also disclosed is a method for producing the high molecular weight derivative.
    Type: Grant
    Filed: November 1, 2007
    Date of Patent: December 18, 2012
    Assignee: Nipon Kayaku Kabushiki Kaisha
    Inventors: Keiichiro Yamamoto, Kazutoshi Takashio
  • Publication number: 20120258927
    Abstract: This invention relates to compounds that inhibit E1 activating enzymes, pharmaceutical compositions comprising the compounds, and methods of using the compounds. The compounds are useful for treating disorders, particularly cell proliferation disorders, including cancers, inflammatory and neurodegenerative disorders; and inflammation associated with infection and cachexia.
    Type: Application
    Filed: June 19, 2012
    Publication date: October 11, 2012
    Applicant: Millenium Pharmaceuticals, Inc.
    Inventors: Steven P. Langston, Edward J. Olhava, Stepan Vyskocil
  • Patent number: 8258115
    Abstract: The present invention refers to new salts of S-adenosyknethionine (SAMe) with improved stability and containing at least 70% by weight of SAMe.
    Type: Grant
    Filed: October 22, 2007
    Date of Patent: September 4, 2012
    Assignee: Gnosis SpA
    Inventors: Ermanno Valoti, Daniele Giovannone, Marco Berna
  • Patent number: 8252919
    Abstract: The present invention relates to a method for producing a 2?-hydroxy-protected nucleoside derivative by reacting a ribonucleoside with an acylating or a carbamoylating reagent in the presence of a metal complex consisting of a copper compound and an optically active ligand. By the method according to the present invention, a 2?-hydroxy-protected ribonucleoside derivative, which is an important intermediate for producing an oligonucleoside, can be easily produced with good regioselectivity from a nucleoside derivative of which 2?,3?-hydroxy groups are not protected.
    Type: Grant
    Filed: February 26, 2009
    Date of Patent: August 28, 2012
    Assignee: Kaneka Corporation
    Inventors: Hirofumi Maeda, Akio Fujii, Masaru Mitsuda
  • Patent number: 8242258
    Abstract: Aspects of the invention include 2? protected nucleoside monomers that are protected at the 2? site with orthoester-type protecting groups. The 2? protected monomers also include a second, aryl carbonate-type, protecting group. Aspects of the invention further include nucleic acids that include the protecting groups of the invention, as well as methods of synthesizing nucleic acids using the protecting groups of the invention.
    Type: Grant
    Filed: December 3, 2007
    Date of Patent: August 14, 2012
    Assignees: Agilent Technologies, Inc., The Regents of the University of Colorado
    Inventors: Douglas J. Dellinger, Brian Stell, Marvin H. Caruthers
  • Publication number: 20120184724
    Abstract: A nucleoside monomer that is protected by a thionocarbamate protecting group and contains one or more 2H, 13C, or 15N isotopes in the ribose and/or base part is provided, as well as a method for making a polynucleotide that uses the same. Also provided is a polynucleotide synthesis method that employs a diamine to deprotect a protected polynucleotide.
    Type: Application
    Filed: December 28, 2011
    Publication date: July 19, 2012
    Applicant: AGILENT TECHNOLOGIES, INC.
    Inventors: Agnieszka B. Sierzchala, Brian Phillip Smart, Douglas J. Dellinger, Geraldine Dellinger, Joel Myerson, Zoltan Timar
  • Patent number: 8202985
    Abstract: Nucleotide monomers, polynucleotides, methods of making each, and methods of deprotecting each, are disclosed. An embodiment of the nucleotide monomer, among others, includes a nucleotide monomer having a heterobase protecting group selected from structures I through III as described herein. An embodiment of the polynucleotide, among others, includes a plurality of nucleotide moieties having a heterobase protecting group selected from one of structures I through III as described herein.
    Type: Grant
    Filed: March 23, 2006
    Date of Patent: June 19, 2012
    Assignees: Agilent Technologies, Inc., The Regents of the University of Colorado
    Inventors: Douglas J. Dellinger, Zoltan Timar, Agnieszka Sierzchala, Geraldino Dellinger, Marvin H. Caruthers
  • Publication number: 20120142625
    Abstract: The present invention relates to substituted purine and 7-deazapurine compounds. The present invention also relates to pharmaceutical compositions containing these compounds and methods of treating disorders in which DOT1-mediated protein methylation plays a part, such as cancer and neurological disorders, by administering these compounds and pharmaceutical compositions to subjects in need thereof.
    Type: Application
    Filed: December 2, 2011
    Publication date: June 7, 2012
    Applicant: EPIZYME, INC.
    Inventors: Edward J. Olhava, Richard Chesworth, Kevin W. Kuntz, Victoria M. Richon, Roy M. Pollock, Scott R. Daigle
  • Patent number: 8193164
    Abstract: A compound of formula (I), or stereoisomers or pharmaceutically acceptable salts thereof, wherein, R1a, R1b, R2a, R2b, U1, U2, X1, X2 and L are as defined herein.
    Type: Grant
    Filed: April 19, 2007
    Date of Patent: June 5, 2012
    Assignee: Novartis AG
    Inventors: Robin Alec Fairhurst, Roger John Taylor
  • Patent number: 8188100
    Abstract: A compound of formula (I), or stereoisomers or pharmaceutically acceptable salts thereof, formula (1), or stereoisomers or pharmaceutically acceptable salts thereof, wherein A, U1, U2, R1a, R1b, R2 and R3 have the meanings as indicated in the specification, are useful for treating conditions mediated by activation of the adenosine A2A receptor, especially inflammatory or obstructive airways diseases. Pharmaceutical compositions that contain the compounds and a process for preparing the compounds are also described.
    Type: Grant
    Filed: September 13, 2007
    Date of Patent: May 29, 2012
    Assignee: Novartis AG
    Inventors: Robin Alec Fairhurst, Roger John Taylor
  • Patent number: 8188222
    Abstract: [Problems] A derivative of a nucleic acid antimetabolite is demanded which can show a higher therapeutic effect at a lower dose. [Means for Solving Problems] Disclosed is a high molecular weight derivative a nucleic acid antimetabolite, which is characterized by comprising a high molecular weight compound comprising a polyethylene glycol moiety and a polymer moiety having a carboxyl group in a side chain and a nucleoside derivative which can act as a nucleic acid antimetabolite, wherein the nucleoside derivative is bound to the carboxyl group in the side chain of the high molecular weight compound via a highly hydrophobic linker.
    Type: Grant
    Filed: November 6, 2007
    Date of Patent: May 29, 2012
    Assignee: Nippon Kayaku Kabushiki Kaisha
    Inventors: Keiichiro Yamamoto, Kazutoshi Takashio
  • Publication number: 20120108800
    Abstract: Provided is a new production method for the synthesis of an NC type nucleoside efficiently and conveniently in a high yield without unnecessary protecting group conversion steps. It relates to a step of producing a compound represented by the formula (II): or a salt thereof, by inverting a compound represented by the formula (I): and a method of producing a compound represented by the formula (III): or a salt thereof (wherein each symbol is as defined in the specification), which includes the step.
    Type: Application
    Filed: June 22, 2010
    Publication date: May 3, 2012
    Inventors: Shumpei Murata, Tadashi Umemoto, Kenichi Miyata, Yoji Hayase
  • Patent number: 8168766
    Abstract: A compound of formula (A) or salt thereof: wherein each of R1, R2, and R3 independently represents hydrogen, alkyl, aryl, acyl, sulfonyl, or silyl; P represents hydrogen or a hydroxy protective group. This compound may be used an intermediate for making a 2-deoxy-2,2-difluoro-D-ribofuranosyl nucleosides, such as gemcitabine.
    Type: Grant
    Filed: August 31, 2009
    Date of Patent: May 1, 2012
    Assignee: ScnioPharm Taiwan Ltd.
    Inventors: Julian Paul Henschke, Yung Fa Chen, George Charles Schloemer
  • Publication number: 20120094948
    Abstract: The invention relates to analogous compounds of 6-thioguanosine triphosphate of general formula (I). A compound of the general formula (I); wherein the dashed bond in the sugar moiety can be either single or double and wherein R1, R2, R3, R4 or R5, equal or different between each other, have general formula -(Int)m-Ter, wherein m is between 0 and 12 and Int and Ter are Internal and Terminal building blocks, wherein Int is selected from the group consisting of formula (II); and Ter is selected from the group consisting of formula (III).
    Type: Application
    Filed: December 20, 2011
    Publication date: April 19, 2012
    Inventors: Giancarlo Naccari, Sergio Baroni
  • Patent number: 8153781
    Abstract: Disclosed are conjugates comprising a dendrimer and a ligand, which is a functionalized congener of an agonist or antagonist of a receptor of the G-protein coupled receptor (GPCR) superfamily, for example, wherein the functionalized congener is an A1 adenosine receptor agonist having a purine nucleoside moiety and a functional group at the N6 position of the purine nucleoside moiety, wherein the functional group has the formula (I): N6H—Ar1—CH2—C(?O)NH—R1 (I), wherein Ar1 and R1 as defined herein. Also disclosed are pharmaceutical compositions, methods of treating various diseases, and a diagnostic method employing such conjugates.
    Type: Grant
    Filed: June 20, 2008
    Date of Patent: April 10, 2012
    Assignees: The United States of America as represented by the Secretary, Department of Health and Human Services, Inserm
    Inventors: Kenneth A. Jacobson, Yoonkyung Kim, Athena Klutz, Beatrice Hechler, Christian Gachet
  • Patent number: 8133880
    Abstract: The invention relates to Purine Derivatives having the formula; The invention also relates to pharmaceutical compositions comprising an effective amount of the Purine Derivative; and methods for treating or preventing an ischemic condition, reperfusion injury, a cellular proliferative disorder, a cardiovascular disease, a neurological disorder, a skin disorder, a radiation-induced injury, a wound, or an inflammatory disease comprising administering an effective amount of the Purine Derivative to a subject in need thereof.
    Type: Grant
    Filed: November 12, 2010
    Date of Patent: March 13, 2012
    Assignee: Inotek Pharmaceuticals Corporation
    Inventors: Prakash Jagtap, Andrew L. Salzman, Csaba Szabo
  • Publication number: 20120053143
    Abstract: The invention discloses triacetyl-3-hydroxyphenyladenosine represented by formula (I), the preparation, the pharmaceutical composition and the use thereof. Specially, the invention discloses a new compound of 2?,3?,5?-tri-O-acetyl-N6-(3-hydroxyphenyl)adenosine. Using hypoxanthine nucleoside as starting material, the compound is prepared by acetylating with acetic anhydride, chlorinating with thionyl chloride, and being substituted with 3-hydroxy aniline. The invention also discloses the pharmaceutical composition comprising triacetyl-3-hydroxyphenyladenosine. The dosage forms of the said pharmaceutical composition include tablet, capsule, pill, injection, sustained release preparation, controlled release preparation or particulate delivery system. The medicament for treatment or precaution of hyperlipemia prepared by the compound of the invention has the advantages of significant hypolipidemic activity, less toxicity and adverse effect as well as slow metabolism in vivo.
    Type: Application
    Filed: March 10, 2009
    Publication date: March 1, 2012
    Applicant: INSTITUTE OF MATARIA MEDICA, CHINESE ACADEMY OF MEDICAL SCIENCES
    Inventors: Haibo Zhu, Song Wu, Linghua Hao, Kai Qu, Ping Zhu, Xing Wang, Wei Li
  • Publication number: 20110144320
    Abstract: 2-adenosine N-pyrazole compounds having the following formula: and methods for using the compounds as A2A receptor agonists to stimulate mammalian coronary vasodilatation for therapeutic purposes and for purposes of imaging the heart.
    Type: Application
    Filed: December 14, 2010
    Publication date: June 16, 2011
    Inventors: Jeff A. Zablocki, Elfatih O. Elzein, Venkata P. Palle, Luiz Belardinelli
  • Publication number: 20110059180
    Abstract: The invention relates to a method for preparing nanoparticles based on functional amphiphilic molecules or macromolecules, optionally in the presence of at least one colipide, enabling the encapsulation of therapeutic agents, especially anti-tumoral agents, and the use thereof for the transport and vectorisation of therapeutic agents, especially anti-tumoral agents.
    Type: Application
    Filed: November 28, 2008
    Publication date: March 10, 2011
    Inventors: Philippe Barthelemy, Michel Camplo, Nathalie Campins, Bruno Chauffert, Florence Bouyer
  • Patent number: 7897759
    Abstract: Disclosed are structurally modified, metabolically stable nucleosides having antitumor activity wherein the formation of toxic metabolites is blocked and antimicrobial activity. The disclosure further relates to pharmaceutical compositions comprising one or more disclosed modified nucleosides and to methods of use thereof.
    Type: Grant
    Filed: June 30, 2008
    Date of Patent: March 1, 2011
    Assignee: MUSC Foundation for Research Development
    Inventors: Giuseppe Gumina, Roger L. White
  • Publication number: 20110028706
    Abstract: The present invention provides a method for producing an inosine derivative represented by the following general formula (1) including the steps of subjecting an inosine derivative of general formula (3) to dithiocarbonylation and carrying out radical reduction of the obtained compound. According to the present invention there can be produced compounds useful as anti-AIDS drugs on industrial scale. wherein R1 may be the same or different and are each benzyl group, benzhydryl group or trityl group, each of which may have a substituent in general formulas (1) and (3).
    Type: Application
    Filed: July 30, 2010
    Publication date: February 3, 2011
    Applicant: Ajinomoto Co., Inc.
    Inventors: Takayoshi TORII, Kunisuke Izawa, Doo Ok Jang, Dae Hyan Cho
  • Patent number: 7863253
    Abstract: The invention relates to Purine Derivatives; compositions comprising an effective amount of a Purine Derivative; and methods for treating or preventing an ischemic condition, reperfusion injury, a cellular proliferative disorder, a cardiovascular disease, a neurological disorder, a skin disorder, a radiation-induced injury, a wound, or an inflammatory disease comprising administering an effective amount of a Purine Derivative to a subject in need thereof.
    Type: Grant
    Filed: September 19, 2005
    Date of Patent: January 4, 2011
    Assignee: Inotek Pharmaceuticals Corporation
    Inventors: Prakash Jagtap, Andrew L. Salzman, Csaba Szabo
  • Patent number: 7795236
    Abstract: The present invention provides an 8-modified purinenucleoside derivative which is useful for diseases associated with an abnormality of plasma uric acid level. An 8-modified purinenucleoside derivative represented by the following formula (I), a prodrug thereof or a pharmaceutically acceptable salt thereof, or a hydrate or solvate thereof, is useful for the prevention or treatment of gout, hyperuricemia, urinary lithiasis, hyperuricemic nephropathy or the like. In the formula, n is 1 or 2; RA is a hydrogen atom or a hydroxyl group; R1 is a hydrogen atom, a hydroxyl group, a thiol group, an amino group or a chlorine atom; ring J represents an optionally substituted 2-naphthyl group, or a group represented by the following general formula (II) wherein Y represents a single bond or a connecting group; ring Z represents an optionally substituted aryl group or heteroaryl group or the like; and R2 to R4, P1 and Q represents a halogen atom, a cyano group or the like.
    Type: Grant
    Filed: March 13, 2007
    Date of Patent: September 14, 2010
    Assignee: Kissei Pharmaceutical Co., Ltd.
    Inventors: Kazuya Tatani, Yoshinori Nonaka, Norihiko Kikuchi
  • Patent number: 7792576
    Abstract: Injuries to the central nervous system, particularly spinal cord injuries, are treated by administering a purine nucleoside or analog to the patient and, optionally, electrically stimulating the site of injury.
    Type: Grant
    Filed: February 20, 2007
    Date of Patent: September 7, 2010
    Assignee: Purdue Research Foundation
    Inventors: Richard B. Borgens, Scott A. Shapiro
  • Publication number: 20100204172
    Abstract: Disclosed are compounds that are AGT inactivators that include a folate residue, e.g., a compound of formula (I), wherein X1, X2, R1, and R2 are as described herein. Also disclosed is a pharmaceutical composition comprising a compound of the invention and a pharmaceutically acceptable carrier. Also disclosed are methods of enhancing the chemotherapeutic treatment of tumor cells and inactivating AGT in a tumor cell. The methods comprise, inter alia, administering a compound or pharmaceutically acceptable salt of formula (I).
    Type: Application
    Filed: March 12, 2008
    Publication date: August 12, 2010
    Applicants: Department of Health and Human Services, The Penn State Research Foundation
    Inventors: Robert C. Moschel, Anthony E. Pegg, Sahar Javanmard, Natalia Loktionova, Gary Pauly
  • Patent number: 7749981
    Abstract: The present invention provides a drug-eluting stent, wherein the stent is coated with one or more non-nucleotide P2Y12 receptor antagonist compounds or a pharmaceutically acceptable salt, solvate, or hydrate thereof. When the stent is placed in a narrowed or damaged arterial vessel, a therapeutically effective amount of the P2Y12 receptor antagonist compound is eluted continuously from the stent to the local environment of the stent. The P2Y12 receptor antagonist compound-eluting stents are useful in preventing thrombosis and restenosis, and are effective in inhibiting the contraction of vascular smooth muscle cells, inhibiting cell proliferation, and reducing inflammation.
    Type: Grant
    Filed: November 4, 2005
    Date of Patent: July 6, 2010
    Assignee: Inspire Pharmaceuticals, Inc.
    Inventors: José L. Boyer, James G. Douglass, III, Sammy R. Shaver
  • Publication number: 20100152434
    Abstract: Therapeutically active nucleosides and associated methods are provided. In one aspect, a nucleoside molecule having a general structural similar to ATP. Such nucleosides have a structure that allows binding to, and subsequent regulation of, protein kinase molecules. As such, the nucleosides of the present invention have may be capable of treating a variety of kinase-related medical disorders.
    Type: Application
    Filed: November 30, 2009
    Publication date: June 17, 2010
    Inventor: Matt A. Peterson
  • Patent number: 7737126
    Abstract: A compound of formula (I) and salts and solvates thereof are disclosed. Compounds of formula (I) are agonists of the adenosine A2A receptor and are believed to be of potential use in the treatment of inflammatory diseases such as asthma and chronic obstructive pulmonary disease.
    Type: Grant
    Filed: May 23, 2005
    Date of Patent: June 15, 2010
    Assignee: Glaxo Group Limited
    Inventors: Philip Blatcher, Richard Peter Charles Cousins, Derek Norman Evans
  • Patent number: 7691825
    Abstract: The present invention provides compounds of the formula wherein R1, R2, R3 and n have meaning as described in the specification, methods for their preparation, and pharmaceutical compositions containing them. The compounds of formula (I) are adenosine A2B receptor agonists and, thus, may be employed for the treatment of diseases in mammals that are mediated by the A2B receptor including, but not limited to, septic shock, cystic fibrosis, impotence, diarrhea, and cardiac diseases. Cardiac diseases include hyperplasia consequent to hypertension, arteriosclerosis, and heart attack. The present invention also provides methods for the induction of pharmacological stress to facilitate coronary imaging of areas of ischemia by employing compounds of formula (I). The compounds of formula (I) may be labeled, e.g., with radioactive isotopes, and therefore are useful in kinetic binding experiments.
    Type: Grant
    Filed: June 4, 2007
    Date of Patent: April 6, 2010
    Assignee: King Pharmaceuticals Research and Development, Inc.
    Inventors: Pier Giovanni Baraldi, Pier Andrea Borea, Allan R. Moorman, Delia Preti
  • Publication number: 20090197825
    Abstract: Described herein are compounds useful in the modulation of blood uric acid levels, formulations containing them and methods of using them. In some embodiments, the compounds described herein are used in the treatment or prevention of disorders related to aberrant levels of uric acid.
    Type: Application
    Filed: November 26, 2008
    Publication date: August 6, 2009
    Applicant: ARDEA BIOSCIENCES, INC.
    Inventors: Barry D. QUART, Jean-Luc GIRARDET, Esmir GUNIC, Li-Tain YEH
  • Publication number: 20090069556
    Abstract: Disclosed are structurally modified, metabolically stable nucleosides having antitumor activity wherein the formation of toxic metabolites is blocked and antimicrobial activity. The disclosure further relates to pharmaceutical compositions comprising one or more disclosed modified nucleosides and to methods of use thereof.
    Type: Application
    Filed: June 30, 2008
    Publication date: March 12, 2009
    Inventors: Guiseppe Gumina, Roger L. White
  • Patent number: 7485717
    Abstract: Orthogonally protected 3?-amino nucleoside monomers and efficient methods for their synthesis are described. The methods employ selective protection of the 3?-amino group in the presence of the unprotected nucleoside base.
    Type: Grant
    Filed: June 30, 2005
    Date of Patent: February 3, 2009
    Assignee: Geron Corporation
    Inventors: Sergei M. Gryaznov, Krisztina Pongracz, Daria Zielinska
  • Patent number: 7414036
    Abstract: Adenosine analogue-type A3 receptor agonists having the formula wherein D is N or CH; E is O; X1 is a group of the formula —CR20R2 1-CYCLE, where R20 and R21 are the same or different and are H, F or CH3; CYCLE is where G is N, CH, CF, CCH3 or CCF3, M is H, Y is —O— or N?, and Z is —N? when Y is O, or is O when Y is —N?; R5 is H, CH3, I, Br, Cl, CF3, OH or NH2; and R8 is —NR9R10, —CHR9R10 or —N?CR9R10, where R9 and R10 are the same and are C1-C4 alkyl, C1-C4 alkenyl or C1-C4 alkoxyalkyl X2 is mono-N— or di-N,N—(C1-C4)alkylaminocarbonyl, mono-N—or di-N,N—(C3-C5)cycloalkyl-aminocarbonyl or N-(C1-C4)alkyl-N-(C3-C5)cycloalkylamino-carbonyl; X3 is OH or NH2; X4 is OH; X5 is H , halogen, (C1-C10)alkyl , (C2-C10)alkenyl , (C2-C10)alkynyl , or either of the latter two groups where terminally substituted by an aryl or heteroaryl group and, when having a terminal methyl group, optionally further terminally substituted by hydroxyl.
    Type: Grant
    Filed: July 26, 2004
    Date of Patent: August 19, 2008
    Assignee: Muscagen Limited
    Inventors: Luis Garcia Sevillano, Christopher McGuigan, Robin Havard Davies
  • Patent number: 7381714
    Abstract: Disclosed are novel compounds that are partial and full A1 adenosine receptor agonists having the structure of Formula I: which are useful for treating various disease states, in particular tachycardia and atrial flutter, angina, and myocardial infarction.
    Type: Grant
    Filed: May 19, 2006
    Date of Patent: June 3, 2008
    Assignee: CV Therapeutics, Inc.
    Inventors: Elfatih Elzein, Rao Kalla, Thao Perry, Jeff Zablocki, Xiaofen Li
  • Patent number: 7368438
    Abstract: This invention is directed to a method of preventing or treating diseases or conditions associated with platelet aggregation. The method is also directed to a method of treating thrombosis or related disorders. The method comprises administering to a subject a pharmaceutical composition comprising an effective amount of a non-nucleotide compound, preferably a P2Y12 receptor antagonist compound, wherein said amount is effective to inhibit platelet aggregation. The compounds useful for this invention include compounds of general Formula I and III-XI, or salts, hydrates, and solvates thereof. The present invention also provides novel compounds according to Formula I and III-XI.
    Type: Grant
    Filed: October 21, 2004
    Date of Patent: May 6, 2008
    Assignee: Inspire Pharmaceuticals, Inc.
    Inventors: Robert Plourde, Jr., Sammy R. Shaver, José L. Boyer, Melwyn A. Abreo, Lorenzo J. Alfaro-Lopez, Yangbo Feng, Daniel F. Harvey, Tatyana V. Khasonova, Chi Tu
  • Patent number: 7358235
    Abstract: Analogs or derivatives of nitrobenzylthioinosine compounds. The use of these new analogs of nitrobenzylthioinosine and methods for the treatment of pain and various other indications using these analogs of nitrobenzylthioinosine as well as pharmaceutical compositions including analogs of nitrobenzylthioinosine.
    Type: Grant
    Filed: October 6, 2004
    Date of Patent: April 15, 2008
    Assignees: Gruenenthal GmbH, Leiden University
    Inventors: Claudia Puetz, Corinna Sundermann, Bernd Sundermann, Adriaan Pieter Ijzerman, Reynier Tromp, Jacobien Von Frijtag Drabbe Kuenzel