Home | Links | Contact Us | More About Intellectual Property | Bookmark
Search patents:
Home Gene Therapy Nucleoside-analogs

 Compositions for photodynamic therapy
I claim: 1. A pharmaceutical composition useful for photodynamic therapy which composition contains,...


 Amplifier molecules for enhancement of diagnosis and therapy
As used herein, an "amplifier" or "amplifier molecule" is a chemical compound having a ...


 Peptide-containing polyethylene glycol derivatives and application thereof
OF THE PREFERRED EMBODIMENTS The present invention will hereinafter be explained in more detail. T...


 Modified HIL-6
OF THE INVENTION Described below is the chemical modification with PEG of at least one amino group ...


 Construction of geometrical objects from polynucleotides
By means of the present invention, DNA, RNA and similar polymers may be produced by synthesizing a ...


 Starburst conjugates
In its broadest aspect, the present invention is directed to polymer conjugate materials comprising ...


 Intermediates for providing functional groups on the 5' end of oligonucleotides
We claim: 1. A partially protected alcohol of the formula: ##STR10## wherein Y.sup.1 is selected ...


 Antiviral polynucleotide conjugates
OF THE INVENTION The present invention provides polynucleotide conjugates characterized by the ...


 Azlactone activated polyalkylene oxides conjugated to biologically active nucleophiles
OF THE PREFERRED EMBODIMENT The azlactone activated polyalkylene oxides of the present invention ...


 Biologically compatible linear block copolymers of polyalkylene oxide and peptide units
INCLUSIVE OF PREFERRED EMBODIMENTS We have discovered that linear block copolymers comprising ...


 Nucleoside analogs

Details
Inventors: Kim, Choung Un; Martin, John C.; Luh, Bing Uh; Misco, Peter F.;
Assignee: Institute of Organic Chemistry and Biochemistry of the Academy of (CZ); Rega Stichting, v.z.w. (BE)
Primary Examiner: Berch; Mark L.
Assistant Examiner:
Attorney, Agent or Firm: Hensley; Max D.

Provided are compounds of the following formulae: A phosphonomethoxymethyoxymethyl purine/pyrimidine derivative of the formula ##STR1## wherein X and X' are the same or different and are hydrogen or alkyl. R and R' are the same or different and are hydrogen, alkyl, hydroyalkyl or alkanoyl and B is a purine or pyrimidine base. A compound of formula (II) or (VIII) ##STR2## wherein the broken line is an optional bond; X, R and X' are the same or different and are H or alkyl with 1 to 6 carbon atoms; and B is cytosine, 5-ethylcytosine, 5-methylcytosine, thymine, uracil, 5-chlorouracil, 5-bromouracil, 5-ethyluracil, 5-iodouracil, 5-propyluracil or 5-vinyluracil, any one of which is substituted at the 1-position; wherein in the compound of formula (II), Y and Z are the same or different and are H; OH; alkyl having 1 to 6 carbon atoms; alkyl having 1 to 6 carbon atoms which is substituted with halogen, hydroxy, amino or azido; or are taken together to form an oxygen atom or a methylene group; or are taken together with X' to complete a cyclic phosphonate having the structure of formula (III) ##STR3## wherein R.sup.b is H or OH; wherein in the compound of formula (VIII), Y is halogen, phenylthio or phenylseleno; and the pharmaceutically acceptable salts thereof. B is a purine or pyrimidine base.

DETAILED DESCRIPTION OF THE INVENTION The compounds of the present invention can exist as optical isomers.
Both the racemic and diasteromeric mixtures of these isomers which may exist for certain compounds, as well as the individual optical isomers, are all within the scope of the present invention.
While the racemic mixtures can be separated into their individual isomers through well-known techniques such as, for example, the separation of diastereomeric salts formed with optically active adjuncts, e.
g.
, acids or bases followed by conversion back to the optically active substrates, in most instances, for the compounds of the present invention, the preferred optical isomer can be synthesized by means of stereospecific reactions, beginning with the appropriate stereoisomer of the desired starting material.
As indicated above, the present invention also pertains to pharmaceutically acceptable non-toxic salts of these compounds, containing, for example, Na.
sup.
+, Li.
sup.
+, K.
sup.
+, Ca.
sup.
++ and Mg.
sup.
++.
Such salts may include those derived by combination of appropriate cations such as alkali and alkaline earth metal ions or ammonium and quaternary amino ions with the acid anion moiety of the phosphonic acid group.
Metal salts can be prepared by reacting the metal hydroxide with a compound of this invention.
Examples of metal salts which can be prepared in this way are salts containing Li.
sup.
+, Na.
sup.
+, and K.
sup.
+.
A less soluble metal salt can be precipitated from the solution of a more soluble salt by addition of the suitable metal compound.
In addition, salts may be formed from acid addition of certain organic and inorganic acids, e.
g.
, HCl, HBr, H .
sub.
2 SO.
sub.
4 or organic sulfonic acids, with basic centers of the purine, specifically guanine, or pyrimidine base.
Finally, it is to be understood that compounds of the present invention in their unionized, as well as zwitterionic form, and/or in the form, of solvates are also considered part of the present invention.
Compounds of the present invention also exist in subclasses, with two broad subclasses being those wherein B is either a purine or a pyrimidine base



Related patents
  Hydrophobic multicomponent heparin conjugates, a preparing method and a use thereof
To accomplish those objectives, the present invention provides hydrophobic muiticomponent heparin conjugates in which heparin is coupled with macromolecules and ...
  Gas permeable bioreactor and method of use
OF THE PREFERRED EMBODIMENTS Like numbered apparatus elements in FIGS. 1-11 are the same. Referring to the drawings, FIG. 1 is a cross-sectional side view of a ...
  Method for treating diseases of the inner ear using adamantane derivatives
OF THE INVENTION As already mentioned, the use of adamantane derivatives is possible or conceivable in many cases of diseases of the inner ear. Preferably, adamantane ...
  Polyalkylene oxide-containing urethane polyols with sulphonic acid groups
What is claimed is: 1. Sulphonic acid group-containing polyalkylene oxide-containing urethane polyols corresponding to the formula: ##STR16## wherein X represents an NH....
  Herpes treatment
I claim: 1. A method for the control of herpes virus infections in man which comprises contacting the herpes lesions, topically or by injection, with a dose of L-lysine L...
  Dense star polymers and dendrimers
OF ILLUSTRATIVE EMBODIMENTS In the dense star polymers of the present invention, the core is covalently bonded to at least one core branch, preferably at least two, ...
  Glycerin derivatives and inhibition of blood PAF
OF THE INVENTION The glycerine derivatives of the invention are compounds of the formula ##STR3## wherein one of the residues R.sup.1, R.sup.2 and R.sup.3 is group U of ...
  Oligonucleotide derivatives and production thereof
Gist In view of the state of the art as described above, the present inventors have developed an immobilized oligonucleotide which is useful in purification of nucleic ...
  Process for synthesizing macrocyclic chelates
The invention is a process for synthesizing a 12 membered ring tetraaza macromolecule. The process involves condensing an amide of ethylene diamine having a general ...
  Immunoconjugates joined by thioether bonds having reduced toxicity and improved selectivity
I claim: 1. A method for producing a 1:1 protein:anitbody tioether-linked immunoconjugate as a predominant species, comprising the steps of: combining a protein selected ...

0.004

Archive: All patents - Links

Copyright (c)2006 Eipa-patents.org - All rights reserved