Carbonyl, Thiocarbonyl, Or Nitrogen, Other Than As Nitro Or Nitroso, Bonded Directly To The Sugar Ring Patents (Class 536/27.22)
  • Publication number: 20020146737
    Abstract: The invention relates to nucleoside derivatives with photolabile protecting groups of general formula (I), where R1=H, F, Cl, Br, I, NO2; R2=H, CN, where R1 and R2 are not simultaneously H; R3=H, 1-4 C alkyl, phenyl; R4=H or a conventional functional group for the synthesis of oligonucleotides; R5=H, OH, halogen or XR6, where X=O or S and R6=a conventional nucleotide protecting group; B=adenine, cytosine, guanine, thymine, uracil, 2,6-diaminopurin-9-yl, hypoxanthin-9-yl, 5-methylcytosin-1-yl, 5-amino-4-imidazolcarboxamid-1-yl or 5-amino-4-imidazolcarboxamid-3-yl, where, if B=adenine, cytosine or guanine the primary amine functionality, optionally, carries a permanent protecting group. Furthermore, these derivatives may be used for the light-controlled synthesis of oligonucleotides on a DNA chip.
    Type: Application
    Filed: March 29, 2002
    Publication date: October 10, 2002
    Inventors: Wolfgang Pfleiderer, Sigrid Buhler, Heiner Giegrich
  • Publication number: 20020058641
    Abstract: The present invention relates to compounds of the formula.
    Type: Application
    Filed: June 5, 2001
    Publication date: May 16, 2002
    Inventors: Simon John Mantell, Peter Thomas Stephenson
  • Publication number: 20020037872
    Abstract: N6 heterocyclic 5′ modified adenosine derivatives that are adenosine A1 receptor partial or full agonists, and as such, are useful for modifying cardiac activity, modifying adipocyte function, treating central nervous system disorders, and treating diabetic disorders and obesity in mammals, and especially in humans.
    Type: Application
    Filed: June 8, 2001
    Publication date: March 28, 2002
    Applicant: CV Therapeutics, Inc.
    Inventors: Venkata P. Palle, Jeff A. Zablocki, Prabha N. Ibrahim, Vaibhav Varkhedkar, Luiz Belardinelli
  • Publication number: 20010020089
    Abstract: The present invention relates to the compounds of the formula: 1
    Type: Application
    Filed: February 20, 2001
    Publication date: September 6, 2001
    Inventors: Simon John Mantell, Sandra Marina Monaghan, Peter Thomas Stephenson
  • Patent number: 6232297
    Abstract: Compounds and methods are provided to treat inflammatory conditions with certain A2A adenosine receptor antagonists.
    Type: Grant
    Filed: June 15, 1999
    Date of Patent: May 15, 2001
    Assignee: University of Virginia Patent Foundation
    Inventors: Joel M. Linden, Gail W. Sullivan, Ian J. Sarembock, Timothy MacDonald, Mark Okusa
  • Patent number: 6180615
    Abstract: 2-adenosine propargyl phenyl ether compositions having the following formula: and methods for using the compositions as A2A receptor agonists to stimulate mammalian coronary vasodilatation for therapeutic purposes and for purposes of imaging the heart.
    Type: Grant
    Filed: June 22, 1999
    Date of Patent: January 30, 2001
    Assignee: CV Therapeutics, Inc.
    Inventors: Jeff A. Zablocki, Venkata P. Palle, Elfatih O. Elzein, Grigory Nudelman
  • Patent number: RE37045
    Abstract: Compounds of the formula are disclosed, wherein R1, represents secondary alkyl; aralkyl; cycloalkyl; heteroaryl substituted alkyl; norbornyl; and substituted secondary alkyl, aralkyl, cycloalkyl, heteroaryl substituted alkyl, norbornyl; and para-substituted phenyl groups; and R2 and R3 are hydrogen or pharmacologically acceptable acyl groups. The compounds of the invention are useful as cardiovascular vasodilator or anti-hypertensive agents. The therapeutically useful compounds of the invention as well as similar 5-N and N-6 substituted adenosine 5-uronamides are prepared, in accordance with a novel process, from isopropylidene (or otherwise suitably blocked) inosine-5′-uronic acid. Isopropylideneinosine-5′-uronic acid is reacted with a suitable inorganic acid halide, such as thionyl chloride, to yield 6-halogeno-9-[2′,3′-O-isopropylidene-&bgr;-D-ribofuranosyl-5-uronic acid halide]-9H-purine.
    Type: Grant
    Filed: January 21, 1999
    Date of Patent: February 6, 2001
    Assignee: Discovery Therapeutics, Inc.
    Inventors: Ray A. Olsson, Robert D. Thompson