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Boronic acid salts useful in parenteral formulations

  • US 7,371,729 B2
  • Filed: 09/09/2003
  • Issued: 05/13/2008
  • Est. Priority Date: 09/09/2002
  • Status: Expired due to Fees
First Claim
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1. A parenteral pharmaceutical formulation comprising a pharmaceutically acceptable base addition salt of a boronic acid of formula (VIII):


  • X-(R)-Phe-(S)-Pro-(R)-Mpg-B(OH)2



    (VIII),wherein X is R6

    (CH2)p

    C(O)—

    , R6

    (CH2)p

    S(O)2

    , R6

    (CH2)p

    NH—

    C(O)—

    or R6

    (CH2)p

    O—

    C(O)—

    , wherein p is 0, 1, 2, 3, 4, 5 or 6 and R6 is H or a 5 to 13-membered cyclic group which is unsubstituted or substituted by 1, 2 or 3 substituents selected from halogen;

    amino;

    nitro;

    hydroxy;

    a C5-C6 cyclic group;

    C1-C4 alkyl and C1-C4 alkyl containing, or linked to the cyclic group through, an in-chain O atom, the aforesaid alkyl groups optionally being substituted by a substituent selected from halogen, amino, nitro, hydroxy and a C5-C6 cyclic group,wherein the salt in the parenteral pharmaceutical formulation is a salt of the boronic acid with an alkali metal, an aminosugar, a guanidine or an amine of formula (XI);

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