Formulation of boronic acid compounds
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Abstract
The invention relates to the formulation of pharmaceutical compounds. More particularly, the invention provides stable, pharmaceutically acceptable compositions prepared from boronic add compounds and methods for preparing the compositions. The invention also provides novel boronate ester compounds. The invention further provides boronic add anhydride compounds useful in the methods of the invention.
18 Citations
92 Claims
- 1. A compound having formula (1):
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13. The compound D-mannitol N-(2-pyrazine)carbonyl-L-phenylalanine-L-leucine boronate.
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14. A compound having formula (8):
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15. A compound having formula (9):
- 16. A composition comprising a compound of formula (2)
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30. A composition, comprising D-mannitol N-(2-pyrazine)carbonyl-L-phenylalanine-L-leucine boronate in a lyophilized powder.
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31. A composition, comprising a compound of formula (8):
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32. A composition, comprising a compound of formula (9):
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33. A method for formulating a boronic acid compound, the method comprising:
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(a) preparing an aqueous mixture comprising (i) a boronic acid compound; and
(ii) a compound having at least two hydroxyl groups separated by at least two connecting atoms in a chain or ring, the chain or ring comprising carbon atoms, and optionally, a heteroatom or heteroatoms which can be N, S, or O; and
(b) lyophilizing the mixture. - View Dependent Claims (34, 35, 36, 37, 38, 39, 40, 41, 42, 43, 44, 45, 46, 47, 48, 49, 50, 51, 78)
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52. A method for formulating a boronic acid compound, the method comprising:
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(a) preparing a boronic acid anhydride compound;
(b) mixing the boronic acid anhydride compound with water and a compound having at least two hydroxyl groups separated by at least two connecting atoms in a chain or ring, the chain or ring comprising carbon atoms, and, optionally, a heteroatom or heteroatoms which can be N, S, or O to produce an aqueous mixture; and
(c) lyophilizing the mixture. - View Dependent Claims (53, 54, 55, 56, 57, 58, 59, 60, 61, 62, 63, 64, 65, 66, 67, 68, 69, 70, 71, 72, 73, 74, 75, 76, 77)
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- 79. A boronic acid anhydride compound comprising one or more compounds of formulae (4) and (5):
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90. A boronic acid anhydride compound, comprising an anhydride of N-(2-pyrazine)carbonyl-L-phenylalanine-L-leucine boronic acid.
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91. A boronic acid anhydride compound comprising a boroxine having formula (7):
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92. A boronic acid anhydride compound consisting essentially of a boroxine having formula (7):
Specification