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US 8,367,617 B2Granted
Crystalline peptide epoxy ketone protease inhibitors and the synthesis of amino acid keto-epoxides
AssigneeOnyx Therapeutics, Inc.
InventorsPasit Phiasivongsa, Louis C. Sehl, William Dean Fuller, Guy J. Laidig
Life of this patent
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Abstract
The invention relates to crystalline peptide keto epoxide compounds, methods of their preparation, and related pharmaceutical compositions. This invention also relates to methods for the preparation of amino acid keto-epoxides. Specifically, allylic ketones are stereoselectively converted to the desired keto epoxides.
Claims8
Crystalline compound 1 having the formula:
- and peaks as determined by XRPD at 2θ values 6.10;
- 8.10;
- 9.32;
- 10.10;
- 11.00;
- 12.14;
- 122.50;
- 13.64;
- 13.94;
- 17.14;
- 17.52;
- 18.44;
- 20.38;
- 21.00;
- 22.26;
- 23.30;
- 24.66;
- 25.98;
- 26.02;
- 27.84;
- 28.00;
- 28.16;
- 29.98;
- 30.46;
- 32.98;
- 33.22;
- 34.52;
- and 39.46.
25 more elements
Crystalline compound 1 having the formula:
- and a DSC thermogram as shown in FIG. 1.
Crystalline compound 1 having the formula:
- and an XRPD pattern as shown in FIG. 2.
Dependencies are inferred from the claim text.