 Dense star polymers and dendrimers |
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| Glycerin derivatives and inhibition of blood PAF |
| OF THE INVENTION The glycerine derivatives of the invention are compounds of the formula ##STR3## ... |
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| Oligonucleotide derivatives and production thereof |
| Gist In view of the state of the art as described above, the present inventors have developed an ... |
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| Process for synthesizing macrocyclic chelates |
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| 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 ... |
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| Peptide-containing polyethylene glycol derivatives and application thereof |
| OF THE PREFERRED EMBODIMENTS The present invention will hereinafter be explained in more detail. T... |
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| Modified HIL-6 |
| OF THE INVENTION Described below is the chemical modification with PEG of at least one amino group ... |
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| Construction of geometrical objects from polynucleotides |
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Composition and method for inhibiting platelet aggregation
| Details |
Inventors: Boyer, Jose; Douglass, III, James G.; Shaver, Sammy R.; Bednarski, Krzysztof; Yerxa, Benjamin R.; Olins, Gillian M.;
Assignee: Inspire Pharmaceuticals, Inc. (Durham, NC) University of North Carolina (Chapel Hill, NC)
Primary Examiner: Lewis; Patrick
Assistant Examiner:
Attorney, Agent or Firm: Howrey LLP Kung; Viola T.
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. The method comprises administering to a subject a pharmaceutical composition comprising a therapeutic effective amount of P2Y.sub.12 receptor antagonist compound, wherein said amount is effective to bind the P2Y.sub.12 receptors on platelets and inhibit ADP-induced platelet aggregation. The P2Y.sub.12 receptor antagonist compounds useful for this invention include mononucleoside 5'-monophosphates, mononucleoside polyphosphates, and dinucleoside polyphosphates of general Formula I, or salts thereof. The present invention also provides novel compounds of mononucleoside 5'-monophosphates, mononucleoside polyphosphates, and dinucleoside polyphosphates. The present invention further provides pharmaceutical formulations comprising mononucleoside 5'-monophosphates, mononucleoside polyphosphates, or dinucleoside polyphosphates. |
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DETAILED DESCRIPTION OF THE INVENTION This invention is provides a method of preventing or treating diseases or conditions associated with platelet aggregation.
The method also provides a method of treating thrombosis.
The method comprises administering to a subject a pharmaceutical composition comprising a therapeutic effective amount of P2Y.
sub.
12 receptor antagonist compound, wherein said amount is effective to bind the P2Y.
sub.
12 receptors on platelets and inhibit ADP-induced platelet aggregation.
The P2Y.
sub.
12 receptor antagonist compounds useful for this invention include compound of general Formula I and salts thereof: ##STR00003## wherein: X.
sub.
1, X.
sub.
2, and X.
sub.
3 are independently oxygen, methylene, monochloromethylene, dichloromethylene, monofluoromethylene, difluoromethylene, or imido; T.
sub.
1, T.
sub.
2, W, and V are independently oxygen or sulfur; m=0, 1 or 2; n=0 or 1; p=0, 1, or 2; where the sum of m+n+p is from 0 to 5; (from monophosphate to hexaphosphate) M=H, or a pharmaceutically-acceptable inorganic or organic counterion; D.
dbd.
O or CH.
sub.
2 B' is a purine or a pyrimidine residue according to general Formulae IV and V which is linked to the 1'-position of the furanose or carbocycle via the 9- or 1-position of the base, respectively; Y'.
dbd.
H, OH, or OR.
sub.
1; Z'.
dbd.
H, OH, or OR.
sub.
2; with the proviso that when A=M, at least one of Y' and Z' is OR.
sub.
1 or OR.
sub.
2; A=M, or A is a nucleoside residue which is defined as: ##STR00004## and which is linked to the phosphate chain via the 5'-position of the furanose or carbocycle; wherein: D.
sub.
2=O or CH.
sub.
2; Z.
dbd.
H, OH, or OR.
sub.
3; Y=H, OH, or OR.
sub.
4; with the proviso that at least one of Y', Z', Y and Z is equal to OR.
sub.
1, OR.
sub.
2, OR.
sub.
4 or OR.
sub.
3 respectively.
B is a purine or a pyrimidine residue according to general Formulae IV and V which is linked to the 1' position of the furanose or carbocycle via the 9- or 1-position of the base, respectively; R.
sub.
1, R.
sub.
2, R.
sub.
3, and/or R.
sub.
4 are residues which are linked directly to the 2'- and/or 3'-hydroxyls of the respective furanose or carbocycle via a carbon atom according to Formula II, or linked directly to two (2'- and 3'-)hydroxyls of the respective furanose or carbocycle via a common carbon atom according to Formula II, such that from one to four independent residues of R
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Gene Therapy 
