Nitrogen Attached Directly Or Indirectly To The Purine Ring System By Nonionic Bonding Patents (Class 544/276)
  • Hetrocyclic compounds that are inhibitors of the enzyme DPP-IV
    Publication number: 20030199528
    Abstract: The present invention relates to therapeutically active and selective inhibitors of the enzyme DPP-IV, pharmaceutical compositions comprising the compounds and the use of such compounds for and the manufacture of medicaments for treating diseases that are associated with proteins that are subject to inactivation by DPP-IV, such as type 2 diabetes and obesity. The present inhibitors are novel purine derivatives, attached at position 8 of the purine skeleton to a diamine.
    Type: Application
    Filed: January 28, 2003
    Publication date: October 23, 2003
    Inventors: Anders B. Kanstrup, Christian Klarner Sams, Jane Marie Lundbeck, Lise Brown Christiansen, Andrew Neil Bowler
  • PNA monomer and precursor
    Publication number: 20030195332
    Abstract: This application relates to monomers of the general formula (I) for the preparation of PNA (peptide nucleic acid) oligomers and provides method for the synthesis of both predefined sequence PNA oligomers and random sequence PNA oligomers: 1
    Type: Application
    Filed: January 24, 2003
    Publication date: October 16, 2003
    Inventors: Sung Kee Kim, Hyunil Lee, Jong Chan Lim, Hoon Choi, Jae Hoon Jeon, Sang Youl Ahn, Sung Hee Lee
  • Substituted nitrogen heterocyclic derivatives and pharmaceutical use thereof
    Publication number: 20030191086
    Abstract: Various substituted nitrogen heterocyclic derivatives and their pharmaceutically acceptable salt derivatives are provided for use as medicaments, and particularly, as antimitotic, anti-viral, anti-cancer, anti-degenerative, immunosuppressive, and anti-microbial drugs or, vaccines. These heterocyclic derivatives can be used as an active agent in a pharmaceutical, as well as a diagnostic utility. To this end, several families of heterocyclic derivatives are provided including pyrrolopyrimidines, pyrazolopyrimidines, purines, and imidazopyridines. In particular, certain tri-substituted and tetra-substituted purines and pyrazolopyrimidines and their deaza analogues are provided for inhibiting cyclin-dependent kinase (“cdk”) proteins, viruses, and immunostimulation.
    Type: Application
    Filed: February 5, 2003
    Publication date: October 9, 2003
    Applicant: USTAV EXPERIMENTALNI BOTANIKY AV CR
    Inventors: Jan Hanus, Vladimir Krystof, Marian Hajduch, Jaroslav Vesely, Miroslav Strnad
  • Kinase inhibitor scaffolds and methods for their preparation
    Publication number: 20030191312
    Abstract: General methods for the solution phase as well as solid phase synthesis of various substituted heteroaryls has been demonstrated. These substituted heteroaryls can be further elaborated by aromatic substitution with amines at elevated temperature or by anilines, boronic acids and phenols via palladium catalyzed cross-coupling reactions.
    Type: Application
    Filed: October 12, 2002
    Publication date: October 9, 2003
    Applicant: IRM LLC, a Delaware Limited Liability Company
    Inventors: Sheng Ding, Qiang Ding, Nathanael S. Gray
  • Stereoselective synthesis of nucleoside analogues
    Publication number: 20030187262
    Abstract: The invention is a process for stereoselectively producing a dioxolane nucleoside analogue from an anomeric mixture of &bgr; and &agr; anomers represented by the following formula A or formula B: 1
    Type: Application
    Filed: February 24, 2003
    Publication date: October 2, 2003
    Applicant: BioChem Pharma Inc.
    Inventors: Alex Cimpoia, Yi Fong Wang
  • Purine derivatives, process for their preparation and use thereof
    Publication number: 20030187261
    Abstract: The present invention relates to new purine derivatives and their deaza- and aza-analogues, methods for preparing said derivatives, and to their use in suitable utilities, in particular their use in diagnostics and therapeutic methods. The invention relates in particular to purine derivatives with an inhibitory effect on for example cyclin-dependent kinase proteins (sdks), viruses, and proliferation of haemotapoietic and cancer cells.
    Type: Application
    Filed: December 19, 2002
    Publication date: October 2, 2003
    Inventors: Libor Havlicek, Vladimir Krystof, Vera Siglerova, Rene Lenobel, Henri Van Onckelen, Zwi Nisan Berneman, Herman Slegers, Edgard Esmans, Miroslav Strnad, Katrien Vermeulen
  • Novel telomerase inhibitors
    Publication number: 20030186978
    Abstract: The present invention relates to novel telomerase inhibitors possessing antitumor activity and to a process for preparing the same. Furthermore, these compounds enhance the efficacy of other chemotherapeutic agents, in the treatment of cancer.
    Type: Application
    Filed: May 23, 2003
    Publication date: October 2, 2003
    Inventors: Alberto Bargiotti, Antonella Ermoli, Maria Menichincheri, Ermes Vanotti, Luisella Bonomini, Antonella Fretta
  • Inhibitors for de novo-RNA polymerases and methods of identifying targets for same
    Publication number: 20030187000
    Abstract: A polymerase inhibitor has first moiety coupled to a second moiety via an optional linker in which the first moiety binds to an initiation nucleotide binding site of a polymerase and forms at least two hydrogen bonds with an RNA template strand that is associated with the polymerase, and in which the second moiety comprised a compound that binds to a site proximal to the nucleotide binding site of the polymerase and thereby increases the affinity of the polymerase inhibitor to the polymerase.
    Type: Application
    Filed: December 27, 2002
    Publication date: October 2, 2003
    Inventors: Nanhua Yao, Haoyun An, Todd Appleby, Shahul Nilar, Yili Ding, Zhi Hong
  • Novel heterocyclic antibacterial compounds
    Publication number: 20030181719
    Abstract: The invention provides heterocyclic organic compounds that inhibit bacterial DNA polymerase IIIC and type II bacterial topoisomerase. The invention further provides compounds that are useful as intermediates in the synthesis of such heterocyclic organic compounds. Syntheses and uses of such heterocyclic organic molecules are also described.
    Type: Application
    Filed: June 17, 2002
    Publication date: September 25, 2003
    Inventors: Chengxin Zhi, George E. Wright
  • Peptide nucleic acids
    Publication number: 20030180734
    Abstract: A novel class of compounds, known as peptide nucleic acids, bind complementary ssDNA and RNA strands more strongly than a corresponding DNA. The peptide nucleic acids generally comprise ligands such as naturally occurring DNA bases attached to a peptide backbone through a suitable linker.
    Type: Application
    Filed: May 23, 2002
    Publication date: September 25, 2003
    Inventors: Ole Buchardt, Michael Egholm, Peter Eigil Nielsen, Rolf Henrik Berg
  • Combinatorial library synthesis and pharmaceutically active compounds produced thereby
    Patent number: 6620796
    Abstract: The invention provides new methods for synthesis of nucleotide-based compounds and new libraries of such compounds. Compounds of the invention are useful for a variety of therapeutic applications, including treatment of viral or bacterial infections and associated diseases and disorders.
    Type: Grant
    Filed: November 8, 2000
    Date of Patent: September 16, 2003
    Assignee: Micrologix Biotech Inc.
    Inventors: Wenqiang Zhou, Yi Jin, Arlene Roland, Radhakrishnan Iyer
  • RNA interference mediated inhibition of epidermal growth factor receptor gene expression using short interfering nucleic acid (siNA)
    Publication number: 20030170891
    Abstract: The present invention concerns methods and reagents useful in modulating EGFR (HER1, HER2, HER3, and/or HER4) gene expression in a variety of applications, including use in therapeutic, diagnostic, agricultural, target validation, and genomic discovery applications. Specifically, the invention relates to short interfering nucleic acid (siNA) or short interfering RNA (siRNA) molecules capable of mediating RNA interference (RNAi) against epidermal growth factor receptor targets.
    Type: Application
    Filed: September 19, 2002
    Publication date: September 11, 2003
    Inventor: James A. McSwiggen
  • Substituted pyrazinones, pyridines and pyrimidines as corticotropin releasing factor ligands
    Publication number: 20030171380
    Abstract: Compounds provided herein are novel substituted pyrazinones, pyridines and pyrimidines of Formula (I) and (II): 1
    Type: Application
    Filed: May 14, 2002
    Publication date: September 11, 2003
    Inventors: Argyrios G. Arvanitis, Paul J. Gilligan, Richard A. Hartz
  • Piperidines
    Publication number: 20030171360
    Abstract: Compounds, compositions and methods are provided which are useful in the treatment of diseases through the inhibition of sodium ion flux through voltage-dependent sodium channels. More particularly, the invention provides substituted piperidines, and compositions containing these compounds. Also provided are methods using the compounds of the invention for the treatment of central or peripheral nervous system disorders, particularly pain and chronic pain by blocking sodium channels associated with the onset or recurrance of the indicated conditions. The compounds, compositions and methods of the present invention are of particular use for treating neuropathic or inflammatory pain by the inhibition of ion flux through a channel that includes a PN3 subunit.
    Type: Application
    Filed: November 1, 2002
    Publication date: September 11, 2003
    Applicant: Icagen, Inc.
    Inventors: Michael F. Gross, Robert N. Atkinson, Matthew S. Johnson
  • Certain alkylene diamine-substituted heterocycles
    Publication number: 20030158197
    Abstract: The present invention also provides a general method to whereby mono-, bi-, or tricyclic heterocycles may be modified to obtain potent antagonists at the NPY1 receptor.
    Type: Application
    Filed: November 8, 2002
    Publication date: August 21, 2003
    Applicant: NEUROGEN CORPORATION
    Inventors: Raymond F. Horvath, Jennifer N. Tran, Stephane De Lombaert, Kevin J. Hodgetts, Philip A. Carpino, David A. Griffith
  • Compounds useful as reversible inhibitors of cathepsin S
    Publication number: 20030158406
    Abstract: Disclosed are cathepsin S reversible inhibitory compounds of the formulas (I), (Ia) and (II), (IIa) as defined herein. The compounds are useful for treating autoimmune diseases. Also disclosed are processes for making such novel compounds.
    Type: Application
    Filed: February 13, 2003
    Publication date: August 21, 2003
    Applicant: Boehringer Ingelheim Pharmaceuticals, Inc.
    Inventors: Charles L. Cywin, Michel J. Emmanuel, Tina Morwick, Denice M. Spero, David S. Thomson, Yancey D. Ward
  • Pyrrolidinyl peptide nucleic acids
    Publication number: 20030157500
    Abstract: The invention discloses compounds of the formula: 1
    Type: Application
    Filed: May 31, 2002
    Publication date: August 21, 2003
    Inventor: Gordon Lowe
  • Synthesis and purification of valacyclovir
    Publication number: 20030153757
    Abstract: The present invention relates to protected valacyclovir, N-tert-butoxycarbonyl-L-valine 2-[(2-amino-1,6-dihydro-6-oxo-9H-purin-9-yl)methoxy] ethyl ester, and a method of making it. The present invention further relates to a method of making valacyclovir including the steps of coupling an amine protected valine selected from N-t-butoxycarbonyl valine and N-formyl valine with acyclovir using a coupling agent to form a protected valacyclovir, and deprotecting the protected valacyclovir to form valacyclovir or a pharmaceutically acceptable salt thereof. The present invention further relates to valacyclovir in pure form, a method of making pure valacyclovir, and to compositions containing pure valacyclovir.
    Type: Application
    Filed: November 13, 2002
    Publication date: August 14, 2003
    Inventors: Marina Yu Etinger, Lev M. Yudovich, Michael Yuzefovich, Gennady A. Nisnevich, Ben Zion Dolitzky, Boris Pertsikov, Boris Tishin, Dina Blasberger
  • Tetrahydropurinones and derivatives thereof as corticotropin releasing factor receptor ligands
    Publication number: 20030149059
    Abstract: Compounds provided herein are novel substituted tetrahydropurinones of Formula (I): 1
    Type: Application
    Filed: July 10, 2002
    Publication date: August 7, 2003
    Inventor: Richard A. Hartz
  • A2A adenosine receptor antagonists
    Publication number: 20030149060
    Abstract: Disclosed are novel A2A adenosine receptor antagonists, useful for treating various disease states, for example cardiovascular disorders, including tissue damage due to ischemia, CNS diseases, including Parkinson's disease, depression, and the like.
    Type: Application
    Filed: December 18, 2002
    Publication date: August 7, 2003
    Inventor: Gloria Cristalli
  • Nucleoside derivatives for library preparation
    Publication number: 20030143561
    Abstract: Nucleoside derivatives as building blocks for templated libraries are described.
    Type: Application
    Filed: June 20, 2002
    Publication date: July 31, 2003
    Applicant: Nuevolution A/S
    Inventors: Henrik Pedersen, Christian Klarner Sams, Frank Abilgaard Slok, Lene Hyldtoft, Michael Anders Godskesen
  • Conformationally constrained L-nucleosides
    Publication number: 20030144501
    Abstract: L-nucleosides are conformationally constrained by at least one additional ring formed by a bridge connecting at least two atoms within a sugar moiety of the nucleoside. While a single additional ring is formed by bridging C1-C4 atoms, two additional rings are formed by bridging both C1-C2, and C3-C4 atoms, or C1-C3 and C2-C4 atoms by bridges having the general structure A—B—Z. The conformationally constrained nucleosides may be incorporated into oligonucleotides and dinucleotides, and it is contemplated that compositions including the conformationally constrained nucleosides may have superior viral inhibitory or antineoplastic properties.
    Type: Application
    Filed: February 14, 2003
    Publication date: July 31, 2003
    Inventor: Kanda S. Ramasamy
  • 4'-thio-L-xylofuranosyl nucleosides, precursors thereof, preparation and use thereof
    Publication number: 20030144235
    Abstract: Compounds represented by the formula 1: 1
    Type: Application
    Filed: September 9, 2002
    Publication date: July 31, 2003
    Inventors: John A. Secrist, Kamal N. Tiwari, John A. Montgomery
  • Oligonucleotide analogues
    Publication number: 20030144231
    Abstract: Novel oligomers, and synthesis thereof, comprising one or more bi-, tri, or polycyclic nucleoside analogues are disclosed herein. The nucleoside analogues have a “locked” structure, termed Locked Nucleoside Analogues (LNA). LNA's exhibit highly desirable and useful properties. LNA's are capable of forming nucleobase specific duplexes and triplexes with single and double stranded nucleic acids. These complexes exhibit higher thermostability than the corresponding complexes formed with normal nucleic acids. The properties of LNA's allow for a wide range of uses such as diagnostic agents and therapeutic agents in a mammal suffering from or susceptible to, various diseases.
    Type: Application
    Filed: July 29, 2002
    Publication date: July 31, 2003
    Inventors: Jesper Wengel, Poul Nielsen
  • Process for recovery of the desired cis-1,3-oxathiolane nucleosides from their undesired trans-isomers
    Patent number: 6600044
    Abstract: A process for the preparation of 1,3-oxathiolane nucleoside analogues in predominantly the cis-form, from mixture of cis-/trans-1,3-oxathiolane nucleosides or their protected derivatives thereof, comprising: (i) treatment of the cis-/trans-1,3-oxathiolane nucleosides (or protected derivatives thereof) with a pyrimidine base (or it derivatives thereof) and an acid, (ii) adding a suitable acid to the obtained cis-/trans-mixture of isomers, (iii) selective crystallization of the desired cis-isomer salt from a solvent or combination of solvents, and (iv) treatment of the predominantly cis-isomer salt with a suitable base to offer the free 1,3-oxathiolane nucleosides, and thereafter optionally repeating steps (i) to (iv) inclusive.
    Type: Grant
    Filed: June 18, 2001
    Date of Patent: July 29, 2003
    Assignee: Brantford Chemicals Inc.
    Inventors: K. S. Keshava Murthy, Gurijala V. Reddy, Zhi-xian Wang, Chandrawansha B. W. Senanayake
  • Substituted pyrimidines, processes for their preparation, and their use as pesticides and fungicides
    Patent number: 6596727
    Abstract: Substituted 4-amino- and 4-alkoxy-cycloalkylpyrimidines, processes for their preparation, and their use as pesticides and fungicides The invention relates to compounds of the formula in which R1, R2, R3 and Q are as defined in the description, X is NH or oxygen and E is a bond or a 1- to 4-membered carbon chain, to a process for their preparation, to agents containing them, and to their use in the control of pests and as fungicides.
    Type: Grant
    Filed: March 15, 1996
    Date of Patent: July 22, 2003
    Assignee: Hoechst Aktiengesellschaft
    Inventors: Wolfgang Schaper, Rainer Preuss, Gerhard Salbeck, Peter Braun, Werner Knauf, Burkhard Sachse, Anna Waltersdorfer, Manfred Kern, Peter Lümmen, Werner Bonin
  • Process for the production of purine derivatives and intermediates therefor
    Publication number: 20030130512
    Abstract: A process for preparing purine derivatives, such as famciclovir and penciclovir, by reacting two intermediates and using a palladium(0) catalyst and a ligand. Intermediates useful in the process are also claimed.
    Type: Application
    Filed: February 19, 2003
    Publication date: July 10, 2003
    Inventors: Richard Freer, Graham Richard Geen, Thomas Weir Ramsay, Andrew Colin Share, Neil Michael Smith
  • Purine derivatives inhibitors of tyrosine protein kinase SYK
    Patent number: 6589950
    Abstract: Disclosed are compounds of the formula in free or salt form, wherein X, R1, R2, R3, and R4 are as defined in the specification, their preparation and their use as pharmaceuticals, particularly for the treatment of inflammatory or obstructive airways disease.
    Type: Grant
    Filed: March 19, 2002
    Date of Patent: July 8, 2003
    Assignee: Novartis AG
    Inventors: Stephen Paul Collingwood, Judy Hayler, Darren Mark Le Grand, Henri Mattes, Keith Allan Menear, Clive Victor Walker, Xiao-Ling Cockcroft
  • Oligonucleotide labeling reactants based on acyclonucleosides and conjugates derived thereof
    Publication number: 20030118999
    Abstract: The invention relates to a labeling reactant of formula (I) useful for labeling an oligonucleotide 1
    Type: Application
    Filed: November 2, 2001
    Publication date: June 26, 2003
    Inventor: Jari Hovinen
  • Pharmaceutical composition for the treatment of CNS and other disorders
    Publication number: 20030119837
    Abstract: The present invention relates to a method of treating disorders of the Central Nervous System (CNS) and other disorders in a mammal, including a human, by administering to the mammal a CNS-penetrant &agr;7 nicotinic receptor agonist. It also relates to pharmaceutical compositions containing a pharmaceutically acceptable carrier and a CNS-penetrant &agr;7 nicotinic receptor agonist.
    Type: Application
    Filed: August 28, 2002
    Publication date: June 26, 2003
    Applicant: Pfizer Inc.
    Inventors: Brian Thomas O'Neill, Jotham Wadsworth Coe, Christopher J. O'Donnell
  • Crystalline forms of valacyclovir hydrochloride
    Publication number: 20030114470
    Abstract: Provided are novel polymorphs and pseudopolymorphs of valacyclovir hydrochloride and pharmaceutical compositions containing these. Also provided are methods for making the novel polymorphs and pseudopolymorphs, which include valacyclovir hydrochloride monohydrate and valacyclovir hydrochloride dihydrate.
    Type: Application
    Filed: September 6, 2002
    Publication date: June 19, 2003
    Inventors: Shlomit Wizel, Judith Aronhime, Valerie Niddam-Hildesheim, Ben-Zion Dolitzky, Marina Yu Etinger, Michael Yuzefovich, Gennady A. Nisnevich, Boris Pertsikov, Boris Tishin, Dina Blasberger
  • Antiviral guanine derivatives
    Patent number: 6579981
    Abstract: A compound of formula (I) or a salt or acyl derivative thereof, in which X represents chlorine, C1-6 alkoxy, phenoxy, phenyl C1-6 alkoxy, NH2, —OH or —SH, is useful in treating viral infections.
    Type: Grant
    Filed: September 23, 1994
    Date of Patent: June 17, 2003
    Assignee: Novartis International Pharmaceutical Ltd.
    Inventors: Richard Lewis Jarvest, Michael Raymond Harnden
  • Acyclic nucleoside derivatives
    Patent number: 6576763
    Abstract: Compounds of the Formula I where one of R1 and R2 is —C(O)CH(CH(CH3)2)NH2 or —C(O)CH(CH(CH3)CH2CH3)NH2; the other of R1 and R2 is —C(═O)C3-C21 saturated or monounsaturated, optionally substituted alkyl; and R3 is OH or H; and pharmaceutically acceptable salts thereof have utility as enhanced bioavailability antivirals against herpes and retroviral infections.
    Type: Grant
    Filed: April 17, 2000
    Date of Patent: June 10, 2003
    Assignee: Medivir AB
    Inventors: Per Engelhardt, Marita Hogberg, Nils-Gunnar Johansson, Xiao-Xiong Zhou, Bjorn Lindborg, M. Robert Leanna, Michael Rasmussen
  • Heterocyclic compounds that are inhibitors of the enzyme DPP-IV
    Publication number: 20030105077
    Abstract: The present invention relates to therapeutically active and selective inhibitors of the enzyme DPP-IV of formula I, pharmaceutical compositions comprising the compounds and the use of such compounds for and the manufacture of medicaments for treating diseases that are associated with proteins that are subject to inactivation by DPP-IV, such as type 2 diabetes and obesity.
    Type: Application
    Filed: June 28, 2002
    Publication date: June 5, 2003
    Inventors: Anders Bendtz Kanstrup, Christian Klarner Sams, Jane Marie Lundbeck, Lise Brown Christiansen, Marit Kristiansen
  • Methods of using chemical libraries to search for new kinase inhibitors
    Patent number: 6573044
    Abstract: The generation of selective inhibitors for specific protein kinases would provide new tools for analyzing signal transduction pathways and possibly new therapeutic agents. We have invented an approach to the development of selective protein kinase inhibitors based on the unexpected binding mode of 2,6,9-trisubstituted purines to the ATP binding site of human CDK2. The most potent inhibitor, purvalanol B (IC50=6 nM), binds with a 30-fold greater affinity than the known CDK2 inhibitor, flavopiridol. The cellular effects of this class of compounds were examined and compared to those of flavopiridol by monitoring changes in mRNA expression levels for all genes in treated cells of Saccharomyces cerevisiae using high-density oligonucleotide probe arrays.
    Type: Grant
    Filed: December 22, 1998
    Date of Patent: June 3, 2003
    Assignees: The Regents of the University of California, Affymetrix, Inc., Centre National de la Recherche Scientifique
    Inventors: Nathanael S. Gray, Peter Schultz, Lisa Wodicka, Laurent Meijer, David J. Lockhart
  • Antiviral guanine derivatives
    Patent number: 6573378
    Abstract: A compound of formula (I) or a salt or acyl derivative thereof, in which X represents chlorine, C1-6 alkoxy, phenoxy, phenyl C1-6 alkoxy, NH2, —OH or —SH, is useful in treating viral infections.
    Type: Grant
    Filed: December 15, 1994
    Date of Patent: June 3, 2003
    Assignee: Novartis International Pharmaceutical Ltd.
    Inventors: Richard Lewis Jarvest, Michael Raymond Harnden
  • Purine inhibitors of phosphodiesterase (PDE)
    Publication number: 20030100571
    Abstract: Purine phosphodiesterase 7 (PDE 7) inhibitors of the following formulas 1
    Type: Application
    Filed: June 17, 2002
    Publication date: May 29, 2003
    Inventors: Wayne Vaccaro, Jacques Y. Roberge, Katerina Leftheris, William J. Pitts, Joseph Barbosa
  • Heterocycle substituted purine derivatives as potent antiproliferative agents
    Publication number: 20030092909
    Abstract: The compounds of the present invention are 2,6,9-trisubstituted purine derivatives which are inhibitors of cyclin/cdk complexes. The compounds of the current invention also are potent inhibitors of human cellular proliferation. As such, the compounds of the present invention constitute pharmaceutical compositions with a pharmaceutically acceptable carrier. Such compounds are useful in treating a disorder mediated by elevated levels of cell proliferation in a mammal compared to a healthy mammal by administering to such mammal an effective amount of the compound.
    Type: Application
    Filed: September 6, 2002
    Publication date: May 15, 2003
    Inventor: Michael Peter Trova
  • Synthesis of substituted 1,3-dioxolanes and substituted 1,3-oxathiolanes with antiviral properties
    Publication number: 20030087918
    Abstract: Disclosed are compounds of the formula
    Type: Application
    Filed: February 12, 2002
    Publication date: May 8, 2003
    Applicant: BioChem Pharma Inc.
    Inventors: Bernard Belleau, Pierette Belleau, Dilip Dixit, Nghe Nguyen-Ba
  • NITROGEN SUBSTITUTED BIARYL PURINE DERIVATIVES AS POTENT ANTIPROLIFERATIVE AGENTS
    Publication number: 20030087906
    Abstract: The compounds of the present invention are 2,6,9-trisubstituted purine derivatives which are inhibitors of cyclin/cdk complexes. The compounds of the current invention also are potent inhibitors of human cellular proliferation. As such, the compounds of the present invention constitute pharmaceutical compositions with a pharmaceutically acceptable carrier. Such compounds are useful in treating a disorder mediated by elevated levels of cell proliferation in a mammal compared to a healthy mammal by administering to such mammal an effective amount of the compound.
    Type: Application
    Filed: September 11, 2001
    Publication date: May 8, 2003
    Inventor: Michael Peter Trova
  • Process for the production of purine derivatives and intermediates therefor
    Patent number: 6555685
    Abstract: A process for preparing purine derivatives, such as famiciclovir and penciclovir, by reacting, in the presence of a palladium (0) catalyst and a ligand, a compound of the formula with a compound of the formula wherein X is H, OH or halo; Y is a leaving group; and R1 and R2 are selected independently from C1-12alkyl, aryl, C1-12alkylaryl, C1-12alkylsilyl, arylsilyl and C1-12alkyldiarylsilyl or are joined together to form a moiety of the formula wherein R3 and R4 are selected independently from H, C1-12alkyl and aryl.
    Type: Grant
    Filed: November 1, 2000
    Date of Patent: April 29, 2003
    Assignee: Novartis International Pharmaceutical Ltd.
    Inventors: Richard Freer, Graham Richard Geen, Thomas Weir Ramsay, Andrew Colin Share, Neil Michael Smith
  • Substituted nitrogen heterocyclic derivatives and pharmaceutical use thereof
    Patent number: 6552192
    Abstract: Various substituted nitrogen heterocyclic derivatives and their pharmaceutically acceptable salt derivatives are provided for use as medicaments, and particularly, as antimitotic, anti-viral, anti-cancer, anti-degenerative, immunosuppressive, and anti-microbial drugs or vaccines. These heterocyclic derivatives can be used as an active agent in a pharmaceutical, as well as a diagnostic utility. To this end, several families of heterocyclic derivatives are provided including pyrrolopyrimidines, pyrazolopyrimidines, purines, and imidazopyridines. In particular, certain tri-substituted and tetra-substituted purines and pyrazolopyrimidines and their deaza analogues are provided for inhibiting cyclin-dependent kinase (“cdk”) proteins, viruses, and immunostimulation.
    Type: Grant
    Filed: July 12, 2001
    Date of Patent: April 22, 2003
    Assignee: Ustau Experimentalni Botaniky AV-CR
    Inventors: Jan Hanu{haeck over (s)}, Vladimír Kry{haeck over (s)}tof, Marián Hajdúch, Jaroslav Veselý, Miroslav Strnad
  • Fatty acid esters of nucleoside analogs
    Patent number: 6548486
    Abstract: New compounds of the general formula (I): Nu-O-Fa, wherein O represents an oxygen, Nu is a nucleoside or nucleoside analogue, and Fa is an acyl group of a mono-unsaturated C18 or 20 fatty acid. The invention also concerns anti viral pharmaceutical and veterinary compositions comprising a compound of formula (I) alone in a combination with a pharmaceutically acceptable carrier.
    Type: Grant
    Filed: September 21, 1994
    Date of Patent: April 15, 2003
    Assignee: Norsk Hydro a.s.
    Inventors: Are Dalen, Finn Myhren, Bernt Børretzen, Kjell Torgeir Stokke
  • Antiviral nucleoside analogues
    Patent number: 6545001
    Abstract: The invention relates to cis-nucleosides of formula (I): and pharmaceutically acceptable salts thereof, wherein X, R3, R4 and are as defined herein. The nucleosides can be in racemic form or in the form of their (+) or (−) enantiomers. The compounds are useful for treating HBV and/or HIV infections, alone or in combination with other therapeutic agents.
    Type: Grant
    Filed: June 29, 2001
    Date of Patent: April 8, 2003
    Assignee: BioChem PHARMA, Inc.
    Inventor: Nghe Nguyen-Ba
  • A2B adenosine receptor antagonists
    Publication number: 20030064999
    Abstract: Disclosed are novel compounds that are A2B adenosine receptor antagonists, useful for treating various disease states, in particular asthma and diarrhea.
    Type: Application
    Filed: June 27, 2002
    Publication date: April 3, 2003
    Inventors: Venkata Palle, Vaibhav Varkhedkar, Jeff Zablocki, Dengming Xiao
  • Method and compositions for the synthesis of dioxolane nucleosides with beta-configuration
    Publication number: 20030060476
    Abstract: The present invention relates to methods and compositions for preparing biologically important nucleoside analogues containing 1,3-dioxolane sugar rings. In particular, this invention relates to the stereoselective synthesis of the beta (cis) isomer by glycosylating the base with an intermediate of formula (II) below a temperature of about −10° C.
    Type: Application
    Filed: October 2, 2002
    Publication date: March 27, 2003
    Applicant: Biochem Pharma Inc.
    Inventors: Tarek Mansour, Alex Cimpoia, Krzysztof Bednarski
  • Synthesis of selenium-derivatized nucleosides, nucleotides, phosphoramidites, triphosphates and nucleic acids
    Publication number: 20030055016
    Abstract: The present invention provides selenium derivatives of nucleosides, nucleoside phosphoramidites, nucleotides, nucleotide triphosphates, oligonucleotides, polynucleotides, and larger nucleic acids and methods for their synthesis. Selenium derivatives of both ribonucleic acids and deoxyribonulcleic acids, as well as methods for their synthesis, crystallization and uses in structural determinations, particularly by X-ray crystallographic techniques are disclosed. The selenium derivatives of the present invention are also useful as food supplements.
    Type: Application
    Filed: March 22, 2002
    Publication date: March 20, 2003
    Inventor: Zhen Huang
  • Compounds for the treatment of ischemia
    Publication number: 20030055021
    Abstract: A3 agonists having Formula I are described herein as well as methods of using such A3 agonists and pharmaceutical compositions containing such A3 agonists.
    Type: Application
    Filed: March 15, 2002
    Publication date: March 20, 2003
    Inventors: Michael P. DeNinno, Hiroko Masamune
  • Pyrimidine compounds and their use as modulators of chemokine receptor activity
    Publication number: 20030040523
    Abstract: The invention provides certain heterocyclic compounds, processes, and intermediates used in their preparation, pharmaceutical compositions containing them and their use in therapy; in formula (I), A is a group of formula (a) or (b).
    Type: Application
    Filed: August 9, 2002
    Publication date: February 27, 2003
    Inventors: Roger Bonnert, Peter Cage, Fraser Hunt, Iain Walters, Paul Willis
  • Method of manufacture of 1,3-oxathiolane nucleosides
    Patent number: 6518425
    Abstract: Processes for the preparation of 1,3-oxathiolane nucleosides are provided that include efficient methods for the preparation of the 1,3-oxathiolane ring and subsequent condensation of the 1,3-oxathiolane with a pyrimidine or purine base. Using the processes described herein, the compounds can be provided as isolated enantiomers.
    Type: Grant
    Filed: May 15, 2000
    Date of Patent: February 11, 2003
    Assignees: Emory University, Triangle Pharmaceuticals, Inc.
    Inventors: George R. Painter, Dennis C. Liotta, Merrick R. Almond, Darryl G. Cleary, Josè D. Soria, Marcos Sznaidman