Boronic Acid Salts Useful in Parenteral Formulations
First Claim
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1. A parenteral pharmaceutical formulation comprising a therapeutically effective amount of a pharmaceutically acceptable base addition salt of a boronic acid of formula (I):
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Abstract
Salts of a peptide boronic acid drug, for example of Cbz-(R)-Phe-(S)—Pro-(R)-Mpg-B(OH)2. The counter-ion to the boronate may be an alkali metal or derived from a strongly basic organic nitrogen-containing compound.
44 Citations
29 Claims
- 1. A parenteral pharmaceutical formulation comprising a therapeutically effective amount of a pharmaceutically acceptable base addition salt of a boronic acid of formula (I):
- 15. A formulation in parenteral dosage form comprising a therapeutically effective amount of a pharmaceutically acceptable base addition salt of a boronic acid of formula (II):
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23. A pharmaceutical product comprising a sealed container containing in the form of a finely divided solid, ready for reconstitution to form a liquid parenteral formulation, a therapeutically effective amount of a boronate salt which consists essentially of a single pharmaceutically acceptable base addition salt of a boronic add formula (II):
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24. A pharmaceutical formulation adapted for parenteral administration, whether directly or after combining with a liquid, and comprising
a) a first species selected from a boronic acid of formula (I), and boronate ions of said boronic acid and equilibrium forms of said boronic acid and said boronate ions:
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28. A medicament adapted for parenteral administration and comprising a therapeutically effective amount of a pharmaceutically acceptable base addition salt of a boronic acid which is a selective thrombin Inhibitor and has a neutral aminoboronic acid residue capable of binding to the thrombin S1 subsite linked through a peptide linkage to a hydrophobic moiety capable of binding to the thrombin S2 and 53 subsites, the salt comprising a cation having a valency n and having an observed stoichiometry consistent with a notional stoichiometry (boronic acid:
- cation) of n;
1. - View Dependent Claims (29)
- cation) of n;
Specification