Additional Nitrogen Bonded Directly To The 2-position Of The Purine Ring System Patents (Class 536/27.61)
  • Patent number: 10662194
    Abstract: The invention relates to substituted 6-anilino-9-heterocyclylpurine derivatives of formula I wherein R denotes one to five substituents independently selected from the group hydrogen, halogen, hydroxy, amino, alkyloxy and alkyl group, R2 is selected from the group comprising amino, halogen, hydroxy, thio, and alkylthio group, Cyc is five- or six-membered heterocyclic ring containing one oxygen atom. The derivatives are useful for inhibition of plant stress.
    Type: Grant
    Filed: December 9, 2015
    Date of Patent: May 26, 2020
    Assignee: UNIVERZITA PALACKEHO V OLOMOUCI
    Inventors: Marek Zatloukal, Lucie Plihalova, Jana Klaskova, Lukas Spichal, Radoslav Koprna, Karel Dolezal, Miroslav Strnad
  • Patent number: 10472383
    Abstract: This invention claims aqueous compositions that comprise triphosphates of 2?-deoxynucleoside derivatives that have, instead of a 3?-OH moiety, a 3?-ONH2 moiety; wherein said compositions contain less than 0.5 mole percent contaminating triphosphate having a 3?-OH moiety, as well as processes for providing such compositions. The compositions further must contain insubstantial amounts of hydroxylamine.
    Type: Grant
    Filed: March 16, 2017
    Date of Patent: November 12, 2019
    Inventor: Steven A Benner
  • Patent number: 8859522
    Abstract: This disclosure relates to an improved process for the preparation of regadenoson, pharmaceutically acceptable salts thereof, and hydrates thereof, and for the preparation of intermediates useful in the synthesis of regadenoson. The disclosure also relates to a new crystalline form of regadenoson. Processes for the preparation of the crystalline form, compositions containing the crystalline form, and methods of use thereof are also described.
    Type: Grant
    Filed: April 26, 2012
    Date of Patent: October 14, 2014
    Assignee: Reliable Biopharmaceutical Corporation
    Inventors: Luzviminda T. Wooldridge, Chun Ma, Sourena Nadji
  • Publication number: 20140286903
    Abstract: This invention is directed to compounds of Formula (I) having the structure that are useful in the treatment of viral infections in mammals, particularly in humans, mediated, at least in part, by a virus in the Flaviviridae family of viruses.
    Type: Application
    Filed: November 8, 2012
    Publication date: September 25, 2014
    Applicants: INHIBITEX, INC., UNIVERSITY COLLEGE CARDIFF CONSULTANTS LIMITED
    Inventors: Stanley Chamberlain, John Vernachio, Srinivas K. Battina, Changalvala V.S. Ramamurty, C. Srinivas Rao, Chris McGuigan, Andrea Brancale
  • Publication number: 20140213539
    Abstract: Disclosed is a synthesis suitable for large scale manufacture of an A2A-adenosine receptor agonist, and also relates to polymorphs of that compound, and to methods of isolating a specific polymorph.
    Type: Application
    Filed: August 19, 2013
    Publication date: July 31, 2014
    Applicant: Gilead Sciences, Inc.
    Inventors: Jeff Zablocki, Elfatih Elzein, Robert Seemayer, Travis Lemons
  • Publication number: 20140206857
    Abstract: A method for the preparation of 2-(4-methoxycarbonylpyrazol-1-yl)adenosine of formula 1a and 2-(4-ethoxycarbonylpyrazol-1-yl)adenosine of formula 1b by reaction of 2-hydrazinoadenosine of formula III and the sodium salt of 3,3-dimethoxy-2-methoxycarbonylpropen-1-ol of formula Va or the sodium salt of 3,3-diethoxy-2-ethoxycarbonylpropen-1-ol of formula Vb in combination with a solvent and an acidic agent.
    Type: Application
    Filed: August 9, 2012
    Publication date: July 24, 2014
    Inventors: Lubomir Kvapil, Pavel Hradil, Martin Grepl, Petr Slezar, Barbora Dvorakova
  • Publication number: 20140194615
    Abstract: A method for the preparation of 2-[4-[(methylamino)carbonyl]-1-H-pyrazol-1-yl]adenosine monohydrate of formula I by reaction of 2-(4-methoxycarbonylpyrazol-1-yl) adenosine of formula III with a solution of methylamine in a non-aqueous solvent, optionally in combination with another inert solvent, to produce anhydrous 2-[4-[(methylamino)carbonyl]-1-H-pyrazol-1-yl]adenosine, which is converted to 2-[4-[(methylamino)carbonyl]-1-H-pyrazol-1-yljadenosine monohydrate of formula I by addition of water.
    Type: Application
    Filed: August 14, 2012
    Publication date: July 10, 2014
    Inventors: Lubomir Kvapil, Pavel Hradil, Martin Grepl, Petr Slezar, Barbora Dvorakova
  • Publication number: 20140163216
    Abstract: Provided herein are compounds, compositions and methods for the treatment of liver disorders, including HCV infections. In one embodiment, compounds and compositions of nucleoside derivatives are disclosed, which can be administered either alone or in combination with other anti-viral agents.
    Type: Application
    Filed: February 14, 2014
    Publication date: June 12, 2014
    Applicants: Centre National de la Recherche Scientifique, Idenix Pharmaceuticals, Inc.
    Inventors: Dominique SURLERAUX, Gilles GOSSELIN
  • Publication number: 20140045781
    Abstract: This disclosure relates to an improved process for the preparation of regadenoson, pharmaceutically acceptable salts thereof, and hydrates thereof, and for the preparation of intermediates useful in the synthesis of regadenoson. The disclosure also relates to a new crystalline form of regadenoson. Processes for the preparation of the crystalline form, compositions containing the crystalline form, and methods of use thereof are also described.
    Type: Application
    Filed: April 26, 2012
    Publication date: February 13, 2014
    Applicant: Reliable Biopharmaceutical Corporation
    Inventors: Luzviminda T Wooldridge, Chun Ma, Sourena Nadji
  • Publication number: 20140011763
    Abstract: The present invention relates to novel 1,2,3-triazolyl purine derivatives. The invention also relates to using the derivatives to treat cancer and various viral infections.
    Type: Application
    Filed: July 8, 2013
    Publication date: January 9, 2014
    Applicant: RESEARCH FOUNDATION OF THE CITY UNIVERSITY OF NEW YORK
    Inventor: Mahesh K. Lakshman
  • Publication number: 20130237491
    Abstract: The present invention relates to the use of nucleoside derivatives of formula Ia wherein the symbols are as defined in the specification, and of pharmaceutically acceptable salts thereof and to pharmaceutical compositions containing such compounds.
    Type: Application
    Filed: April 12, 2013
    Publication date: September 12, 2013
    Applicant: Roche Palo Alto LLC
    Inventors: Rene Robert Devos, Christopher John Hobbs, Wen-Rong Jiang, Joseph Armstrong Martin, John Herbert Merrett, Isabel Najera, Nobuo Shimma, Takuo Tsukuda
  • Patent number: 8524883
    Abstract: Disclosed is a synthesis suitable for large scale manufacture of an A2A-adenosine receptor agonist, namely, (1-{9-[(4S,2R,3R,5R)-3,4-dihydroxy-5-(hydroxymethyl)oxolan-2-yl]-6-aminopurin-2-yl}pyrazol-4-yl)-N-methylcarboxamide. Also, disclosed are polymorphs of this compound and methods for isolating a specific polymorph. Also, disclosed are pharmaceutical compositions and methods for preparing pharmaceutical compositions.
    Type: Grant
    Filed: December 21, 2011
    Date of Patent: September 3, 2013
    Assignee: Gilead Sciences, Inc.
    Inventors: Jeff Zablocki, Elfatih Elzein, Robert Seemayer, Travis Lemons
  • Publication number: 20130136693
    Abstract: The present invention provides novel crystalline polymorphic forms of 2-cyclohexylmethylidenehydrazino adenosine, also known as binodenoson, methods of making the same, and methods for the manufacture of a pharmaceutical composition by employing such crystal forms, in particular, for the use of binodenoson in a subject, in need thereof, as a pharmacological stress agent to produce coronary vasodilation.
    Type: Application
    Filed: July 11, 2012
    Publication date: May 30, 2013
    Applicant: King Pharmaceuticals Research and Development, Inc
    Inventors: Allan R. Moorman, Michael H. O'Neal
  • Publication number: 20130058866
    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: August 29, 2012
    Publication date: March 7, 2013
    Inventors: Jeff A. Zablocki, Elfatih O. Elzein, Venkata P. Palle, Luiz Belardinelli
  • 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
  • Patent number: 8278435
    Abstract: The present disclosure provides a process for the preparation of 2-adenosine N-pyrazole compounds exemplified by the structure shown below that are potent and selective agonists for A2A adenosine receptor, compositions comprising these compounds, and methods for using these compounds to stimulate mammalian coronary vasodilation for imaging the heart.
    Type: Grant
    Filed: December 14, 2010
    Date of Patent: October 2, 2012
    Assignee: Gilead Sciences, Inc.
    Inventors: Jeff A. Zablocki, Elfatih O. Elzein, Venkata Palle, Luiz Belardinelli
  • Publication number: 20120245335
    Abstract: The disclosed invention provides compositions and methods of treating a Flaviviridae infection, including hepatitis C virus, West Nile Virus, yellow fever virus, and a rhinovirus infection in a host, including animals, and especially humans, using a (2?R)-2?-deoxy-2?-fluoro-2?-C-methyl nucleosides, or a pharmaceutically acceptable salt or prodrug thereof.
    Type: Application
    Filed: June 7, 2012
    Publication date: September 27, 2012
    Applicant: GILEAD PHARMASSET LLC
    Inventor: Jeremy Clark
  • Publication number: 20120232029
    Abstract: Embodiments of the invention are to compounds, methods, and compositions for use in the treatment of viral infections. More specifically embodiments of the invention are 2?,4?-substituted nucleoside compounds useful for the treatment of viral infections, such as HIV, HCV, and HBV infections.
    Type: Application
    Filed: December 13, 2011
    Publication date: September 13, 2012
    Applicant: Pharmasset, Inc.
    Inventors: MICHAEL JOSEPH SOFIA, Jinfa Du
  • Publication number: 20120142626
    Abstract: Disclosed herein are 2?-spiro-nucleosides and derivatives thereof useful for treating a subject infected by hepatitis C virus or dengue virus.
    Type: Application
    Filed: November 30, 2011
    Publication date: June 7, 2012
    Applicant: Pharmasset, Inc.
    Inventors: JINFA DU, Michael Joseph Sofia
  • 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: 8193339
    Abstract: This invention relates to a process of stereoselectively synthesizing a ?-nucleoside compound of formula (I): wherein R1, R2, and B are as defined in the specification; each of R3 and R4, independently, is H or fluoro. The process includes reacting, in the presence of a transition metal salt, a tetrahydrofuran compound of formula (II): wherein R1, R2, and L are as defined in the specification, with a nucleobase derivative; and each of R3 and R4, independently, is H or fluoro.
    Type: Grant
    Filed: November 6, 2008
    Date of Patent: June 5, 2012
    Assignee: Pharmaessentia Corp.
    Inventors: Chi-Yuan Chu, Wei-Der Lee, Wensen Li, Chan Kou Hwang
  • 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
  • Publication number: 20120052046
    Abstract: Phosphoramidate compounds derived from guanine bases having enhanced therapeutic potency are provided, and these compounds in particular have enhanced potency with respect to treatment of viral infections, such as hepatitis C virus. Pharmaceutical compositions, methods of preparing the compounds, and methods of using the compounds and compositions to treat viral infections are also provided.
    Type: Application
    Filed: January 11, 2010
    Publication date: March 1, 2012
    Inventors: Stanley Chamberlain, Jeff Hutchins, Karolina Madela, Christopher McGuigam, John Vernachio, Mohamed Aljarah, Arnaud Gilles
  • Patent number: 8106183
    Abstract: Disclosed is a synthesis suitable for large scale manufacture of an A2A-adenosine receptor agonist, and also relates to polymorphs of that compound, and to methods of isolating a specific polymorph.
    Type: Grant
    Filed: April 22, 2010
    Date of Patent: January 31, 2012
    Assignee: Gilead Sciences, Inc.
    Inventors: Jeff Zablocki, Elfaith Elzein
  • Patent number: 8106029
    Abstract: Myocardial imaging methods are provided that are accomplished by administering doses of a pharmaceutical composition comprising one or more adenosine A2A receptor agonists, in particular regadenoson, useful for, among other indications, myocardial imaging and coronary vasodilation, in an amount sufficient to achieve at least a minimal increase in average coronary peak flow velocity.
    Type: Grant
    Filed: December 14, 2009
    Date of Patent: January 31, 2012
    Assignee: Gilead Sciences, Inc.
    Inventors: Toufigh Gordi, Ann Walls Olmsted, Hsiao Dee Lieu, Luiz Belardinelli
  • Patent number: 8071565
    Abstract: Compounds of formula (I): or stereoisomers or pharmaceutically acceptable salts thereof, wherein W, R1, 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: July 11, 2007
    Date of Patent: December 6, 2011
    Assignee: Novartis AG
    Inventors: Robin Alec Fairhurst, Roger John Taylor
  • 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: 20110130559
    Abstract: This application provides a process for preparing enantiomerically pure ?-D-dioxolane nucleosides. In particular, a new synthesis of (?)-DAPD, suitable for large scale development, is described. In one embodiment the invention provides a process for preparing a substantially pure ?-D- or ?-L-1,3-dioxolane nucleosides comprising a) preparing or obtaining an esterified 2,2-dialkoxy ethanol; b) cyclizing the esterified 2,2-dialkoxy ethanol with glycolic acid to obtain a 1,3-dioxolane lactone; c) resolving the 1,3-dioxolane lactone to obtain a substantially pure D- or L-lactone; d) selectively reducing and activating the D- or L-chiral lactone to obtain a substantially pure D- or L-1,3-dioxolane; e) coupling the D- or L-1,3-dioxolane to an activated and/or protected purine or pyrimidine base; and f) optionally purifying the nucleoside to obtain a substantially pure protected ?-D- or ?-L-1,3-dioxolane nucleoside.
    Type: Application
    Filed: August 27, 2010
    Publication date: June 2, 2011
    Applicant: Gilead Sciences, Inc.
    Inventors: Marcos Sznaidman, George R. Painter, Merrick R. Almond, Darryl G. Cleary, Amir Pesyan
  • Publication number: 20110092451
    Abstract: The present invention comprises compounds useful as antiviral or antitumor agents. The compounds comprise nucleotide analogues that comprise tetrahydrofuranyl or tetrahydrothienyl moeities with quaternary centers at the 3? position. The nucleotide analogues can be used to inhibit cancer or viruses. Accordingly, the compounds of the present invention are useful for treating, preventing, and/or inhibiting diseases or conditions associated with cancers and viruses. Thus, the present invention also comprising pharmaceutical formulations comprising the compounds and methods of using the compounds and formulations to inhibit viruses or tumors and treat, prevent, or inhibit the foregoing diseases.
    Type: Application
    Filed: March 18, 2009
    Publication date: April 21, 2011
    Applicant: INSTITUT DE RECHERCHES CLINIQUES DE MONTREAL
    Inventor: Yvan Guindon
  • Patent number: 7915232
    Abstract: The present invention relates to the use of nucleoside derivatives of formula Ia wherein the symbols are as defined in the specification, and of pharmaceutically acceptable salts thereof which inhibit HCV polymerase and are useful for treating a patient suffering from a HCV infection and to pharmaceutical compositions containing such compounds.
    Type: Grant
    Filed: September 14, 2009
    Date of Patent: March 29, 2011
    Assignee: Roche Palo Alto LLC
    Inventors: Joseph Armstrong Martin, John Herbert Merrett, Isabel Najera, Rene Robert Devos, Christopher John Hobbs, Wen Rong Jiang, Nobuo Shimma, Takuo Tsukuda
  • Publication number: 20110064671
    Abstract: The present invention relates to a method of increasing blood brain barrier permeability in a subject. This method involves selecting a subject who would benefit from increased blood brain barrier permeability and subjecting the selected subject to a treatment. That treatment increases adenosine level and/or bioavailability, modulates adenosine receptors, and/or increases CD73 level and/or activity under conditions effective to increase blood brain barrier permeability in the subject. Methods of decreasing blood brain barrier permeability in a subject, treatment of a subject for a disorder or condition of the central nervous system, and screening compounds effective in increasing blood brain barrier permeability, as well as pharmaceutical agents are also disclosed.
    Type: Application
    Filed: March 10, 2009
    Publication date: March 17, 2011
    Applicant: CORNELL UNIVERSITY
    Inventor: Margaret S. Bynoe
  • Publication number: 20110044904
    Abstract: The present invention provides novel crystalline polymorphic forms of 2-cyclohexylmethylidenehydrazino adenosine, also known as binodenoson, methods of making the same, and methods for the manufacture of a pharmaceutical composition by employing such crystal forms, in particular, for the use of binodenoson in a subject, in need thereof, as a pharmacological stress agent to produce coronary vasodilation.
    Type: Application
    Filed: February 27, 2009
    Publication date: February 24, 2011
    Inventors: Allan R. Moorman, Michael H. O'Neill
  • Publication number: 20110009354
    Abstract: The crystal structure of the complex of S-adenosylmethionine methyl ester with h?doMetDC F223A, a mutant where the stacking of the aromatic rings of F7, adenine and F223 would be eliminated. The structure of this mutant with the ester shows that the ligand still maintains a syn conformation aided by pi-pi interactions to F7, hydrogen bonds to the backbone of Glu67, and electrostatic interactions. Several series of AdoMet substrate analogues with a variety of substituents at the 8 position of adenine were synthesized and analyzed for their ability to inhibit hAdoMetDC. To understand these results, virtual modeling of the enzyme inhibitor complexes and the crystal structures of human AdoMetDC with 5?-deoxy-5?-[N-methyl-N-[2-(aminooxy)ethyl]amino-8-methyl]adenosine (MAOEMA) and 5?-deoxy-5?-[N-methyl-N-[4-(aminooxy)butyl]amino-8-ethyl]adenosine (MAOBEA) at the active site have been determined experimentally.
    Type: Application
    Filed: August 1, 2008
    Publication date: January 13, 2011
    Inventors: John A. Secrist, III, Steve Ealick, Shridhar Bale, Anthony E. Pegg, Diane E. McCloskey, Wayne C. Guida
  • Patent number: 7807653
    Abstract: The present invention relates to nucleoside diphosphate mimics and nucleoside triphosphate mimics, which contain diphosphate or triphosphate moiety mimics and optionally sugar-modifications and/or base-modifications. The nucleotide mimics of the present invention, in a form of a pharmaceutically acceptable salt, a pharmaceutically acceptable prodrug, or a pharmaceutical formulation, are useful as antiviral, antimicrobial, and anticancer agents. The present invention provides a method for the treatment of viral infections, microbial infections, and proliferative disorders. The present invention also relates to pharmaceutical compositions comprising the compounds of the present invention optionally in combination with other pharmaceutically active agents.
    Type: Grant
    Filed: June 14, 2007
    Date of Patent: October 5, 2010
    Assignee: Biota Scientific Management Pty Ltd
    Inventors: Phillip D. Cook, Guangyi Wang, Thomas W. Bruice, Nicholas A. Boyle, Janet M. Leeds, Jennifer L. Brooks, Marija Prhavc, Maria Eugenia Ariza, Patrick C. Fagan, Yi Jin, Vivek K. Rajwanshi, Kathleen D. Tucker
  • Publication number: 20100179313
    Abstract: Disclosed is a synthesis suitable for large scale manufacture of an A2A-adenosine receptor agonist, and also relates to polymorphs of that compound, and to methods of isolating a specific polymorph.
    Type: Application
    Filed: January 13, 2010
    Publication date: July 15, 2010
    Inventors: Jeff Zablocki, Elfaith Elzein
  • Publication number: 20100160620
    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, 2009
    Publication date: June 24, 2010
    Inventors: Jeff A. Zablocki, Elfatih O. Elzein, Venkata P. Palle, Luiz Belardinelli
  • 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: 7696181
    Abstract: Disclosed are novel compounds that are partial and full A1 adenosine receptor agonists, useful for treating various disease states, in particular tachycardia and atrial flutter, angina, myocardial infarction and hyperlipidemia. The structure of the compounds is given by Formula (I): wherein R1, R2, R3, R4, R5, X, Y, Z, and T are as described herein.
    Type: Grant
    Filed: August 24, 2006
    Date of Patent: April 13, 2010
    Assignee: CV Therapeutics, Inc.
    Inventors: Prabha Ibrahim, Elfatih Elzein, Kevin Shenk, Robert Jiang, Jeff Zablocki, Xiaofen Li, Christopher Morrison, Thao Perry, Dengming Xiao
  • Patent number: 7625877
    Abstract: The present invention provides a 4?-C-substituted-2-haloadenosine derivative represented by the following formula [I], [II], or [III]: wherein X represents a halogen atom, R1 represents an ethynyl group or a cyano group, and R2 represents hydrogen, a phosphate residue, or a phosphate derivative residue. The present invention also provides a pharmaceutical composition containing the derivative and a pharmaceutically acceptable carrier therefor. The derivative is useful as a medicine for the treatment of Acquired Immune Deficiency Syndrome (AIDS).
    Type: Grant
    Filed: November 19, 2007
    Date of Patent: December 1, 2009
    Assignee: Yamasa Corporation
    Inventors: Satoru Kohgo, Hiroshi Ohrui, Eiichi Kodama, Masao Matsuoka, Hiroaki Mitsuya
  • Publication number: 20090286971
    Abstract: The present invention for the stereoselective preparation of 2-deoxy-?-D-adenine nucleosides wherein a blocked 2-deoxy-?-D-arabinofuranosyl halide is coupled with the salt of an adenine derivative.
    Type: Application
    Filed: May 4, 2009
    Publication date: November 19, 2009
    Inventors: William E. Bauta, Brian D. Burke, Brian E. Schulmeier, William R. Cantrell, JR., Dennis P. Lovett, Jose Puente
  • Patent number: 7553823
    Abstract: 2-adenosine C-pyrazole compounds having formula (a) 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: Grant
    Filed: September 15, 2006
    Date of Patent: June 30, 2009
    Assignee: CV Therapeutics, Inc.
    Inventors: Jeff A. Zablocki, Elfatih O. Elzein, Venkata P. Palle
  • Patent number: 7544794
    Abstract: This invention relates to the field of nucleic acid chemistry, more specifically to the field of compositions and processes that are nucleic acid analogs. More specifically, this invention relates to compositions that allow the sequencing of oligonucleotides by synthesis, and processes for sequencing by synthesis that exploit these compositions. Most specifically, the instant invention discloses compositions of matter that are 5?-triphosphates of ribo- and 2?-deoxyribonucleosides wherein the 3?-OH group is replaced by a 3?-ONHR group in the alpha configuration, wherein R is either a H or CH3 group. Also disclosed are these triphosphates where the nucleobase carries, via a linker, a reporter groups, such as a fluorescent species that can be used in single- or multi-copy DNA sequencing, or a tag that can be visualized by ultramicroscopy. Also disclosed are processes that use these compositions to do sequencing by synthesis.
    Type: Grant
    Filed: March 11, 2006
    Date of Patent: June 9, 2009
    Inventor: Steven Albert Benner
  • Publication number: 20090131651
    Abstract: Synthesis of 2-substituted adenosines of formula (I) using 2-nitro pentabenzoyl adenosine, or 2-nitro pentaacetyl adenosine, as intermediate is described: Formula (I) wherein R=C1-6 alkoxy (straight or branched), a phenoxy group (unsubstituted, or mono-, or di-substituted by halo, amino, CF3—, cyano, nitro, C1-4 alkyl, or C1-4 alkoxy), a benzyloxy group (unsubstituted, or mono-, or di-substituted by halo, amino, CF3—, cyano, nitro, C1-6 alkyl, or C1-6 alkoxy), or a benzoyl group (unsubstituted, or mono-, or di-substituted by halo, amino, CF3—, cyano, nitro, C1-6 alkyl, or C1-6 alkoxy). The methods provide improved yield and purity of product.
    Type: Application
    Filed: December 3, 2004
    Publication date: May 21, 2009
    Inventors: Giles Albert Brown, Edward Daniel Savory, Jacqueline Valerie Anne Ouzman, Alison Margaret Stoddart
  • Patent number: 7514417
    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: April 7, 2009
    Assignee: CV Therapeutics, Inc.
    Inventors: Elfatih Elzein, Rao Kalla, Thao Perry, Jeff Zablocki, Xiaofen Li
  • Patent number: 7470784
    Abstract: 2-Chloro-9-(2-deoxy-2-fluoro-?-D-arabinofuranosyl)-9H-purin-6-amine is synthesized by reacting a 2-chloro-6-substituted purine with a protected and activated 2-deoxy-2-fluoro-D-arabinofiranose; and reacting with a base such as ammonia to provide 2-chloro-9-(2-deoxy-2-fluoro-?-D-arabinofuranosyl)-9H-purin-6-amine. When the purine reactant is substituted in the 6 position with a halogen, a reaction step with an alkoxide is carried out prior to the reaction with ammonia.
    Type: Grant
    Filed: August 16, 2005
    Date of Patent: December 30, 2008
    Assignee: Southern Research Institute
    Inventors: John A. Montgomery, Anita T. Fowler, John A. Secrist, III
  • 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: 7339053
    Abstract: The present invention provides a 4?-C-substituted-2-haloadenosine derivative represented by the following formula [I], [II], or [III]: (wherein X represents a halogen atom, R1 represents an ethynyl group or a cyano group, and R2 represents hydrogen, a phosphate residue, or a phosphate derivative residue). The present invention also provides a pharmaceutical composition containing the derivative and a pharmaceutically acceptable carrier therefor. Such derivative is useful as medicine for the treatment of Acquired Immune Deficiency Syndrome (AIDS).
    Type: Grant
    Filed: March 24, 2005
    Date of Patent: March 4, 2008
    Assignee: Yamasa Corporation
    Inventors: Satoru Kohgo, Hiroshi Ohrui, Eiichi Kodama, Masao Matsuoka, Hiroaki Mitsuya
  • Patent number: 7262176
    Abstract: Disclosed are novel compounds that are A3 adenosine receptor agonists, useful for treating various disease states, including cancer, cardiac ischemia, leukopenia, and neutropennia.
    Type: Grant
    Filed: November 25, 2003
    Date of Patent: August 28, 2007
    Assignee: CV Therapeutics, Inc.
    Inventors: Elfatih Elzein, Venkata Palle, Vaibhav Varkhedkar, Jeff Zablocki
  • Patent number: 7238676
    Abstract: The present invention relates to compounds of the formula and pharmaceutically acceptable salts and solvates thereof, to processes for the preparation of, intermediates used in the preparation of, and compositions containing such compounds and the uses of such compounds as adenosine A2a receptor agonists.
    Type: Grant
    Filed: June 15, 2004
    Date of Patent: July 3, 2007
    Assignee: Pfizer Inc.
    Inventors: Simon John Mantell, Sandra Marina Monaghan, Peter Thomas Stephenson
  • Patent number: 7112574
    Abstract: Novel C2,8-disubstituted adenosine derivatives disclosed herein have been found to be potent adenosine receptor agonists, in particular for the A2A receptor. The said compounds have biological activity against conditions such as hypertension, ischemic heart disease, ischemic brain disease, psychosis and wound healing. Further, the invention also discloses a process for the preparation of such compounds and pharmaceutical compositions comprising them.
    Type: Grant
    Filed: March 3, 2002
    Date of Patent: September 26, 2006
    Assignees: Universiteit Leiden, Can-Fite Biopharma Ltd.
    Inventors: Erica Van Tilburg, Ad Ijzerman