Boronate ester compounds and pharmaceutical compositions thereof
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Abstract
The present invention provides novel compounds useful as proteasome inhibitors. The invention also provides pharmaceutical compositions comprising the compounds of the invention and methods of using the compositions in the treatment of various diseases.
54 Citations
15 Claims
- 1. A compound of formula (II):
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2. 2,2′
- -{2-[(1R)-1-({[(2,5-Dichlorobenzoyl)-amino]acetyl}amino)-3-methylbutyl]-5-oxo-1,3,2-dioxaborolane-4,4-diyl}diacetic acid, characterized by formula (III);
- -{2-[(1R)-1-({[(2,5-Dichlorobenzoyl)-amino]acetyl}amino)-3-methylbutyl]-5-oxo-1,3,2-dioxaborolane-4,4-diyl}diacetic acid, characterized by formula (III);
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3. 4-(R,S)-(Carboxymethyl)-2-((R)-1-(2-(2,5-dichlorobenzamido)acetamido)-3-methylbutyl)-6-oxo-1,3,2-dioxaborinane-4-carboxylic acid, characterized by formula (IV):
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4. A compound of formula (IIIa):
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5. A compound of formula (IVa):
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6. A crystalline form of 2,2′
- -{2-[(1R)-1-({[(2,5-dichlorobenzoyl)amino]acetyl}amino)-3-methyl butyl]-5-oxo-1,3,2-dioxaborolane-4,4-diyl}diacetic acid, comprising an x-ray powder diffraction pattern having characteristic peaks expressed in degrees two-theta at approximately 6.4, 8.3, 15.1, 16.4, and 19.1.
- View Dependent Claims (7, 8)
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9. A crystalline form of 2,2′
- -{2-[(1R)-1-({[(2,5-dichlorobenzoyl)amino]acetyl}amino)-3-methylbutyl]-5-oxo-1,3,2-dioxaborolane-4,4-diyl}diacetic acid, comprising an x-ray powder diffraction pattern having characteristic peaks expressed in degrees two-theta at approximately 5.8, 7.6, 11.6, 11.9, 16.7, 18.2, 19.6, 20.0, and 22.4.
- View Dependent Claims (10, 11)
- 12. A crystalline form of 4-(R,S)-(carboxymethyl)-2-((R)-1-(2-(2,5-dichlorobenzamido)acetamido)-3-methylbutyl)-6-oxo-1,3,2-dioxaborinane-4-carboxylic acid, comprising an x-ray powder diffraction pattern having characteristic peaks expressed in degrees two-theta at approximately 5.7, 7.6, 11.4, 11.8, 16.5, 18.1, 19.4, 19.8, and 22.2.
Specification