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Claims for Patent: 8,207,126

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Claims for Patent: 8,207,126

Title:Compounds for enzyme inhibition
Abstract: Peptide-based compounds including heteroatom-containing, three-membered rings efficiently and selectively inhibit specific activities of N-terminal nucleophile (Ntn) hydrolases. The activities of those Ntn having multiple activities can be differentially inhibited by the compounds described. For example, the chymotrypsin-like activity of the 20S proteasome may be selectively inhibited with the inventive compounds. The peptide-based compounds include at least three peptide units, an epoxide or aziridine, and functionalization at the N-terminus. Among other therapeutic utilities, the peptide-based compounds are expected to display anti-inflammatory properties and inhibition of cell proliferation.
Inventor(s): Smyth; Mark S. (Foster City, CA), Laidig; Guy J. (Menlo Park, CA)
Assignee: Onyx Therapeutics, Inc. (South San Francisco, CA)
Application Number:13/334,466
Patent Claims: 1. A method, which comprises mixing a compound having the formula: ##STR00029## or a pharmaceutically acceptable salt thereof, with one or more pharmaceutically acceptable carriers.

2. The method of claim 1, wherein each of the one or more pharmaceutically acceptable carriers is independently selected from a binder, a disintegrating agent, a lubricant, a corrigent, a solubilizing agent, a suspension aid, an emulsifying agent, a coating agent, a cyclodextrin, and a buffer.

3. The method of claim 1, wherein each of the one or more pharmaceutically acceptable carriers is independently selected from: (1) a sugar selected from lactose, glucose, and sucrose; (2) a starch selected from corn starch, potato starch, and substituted or unsubstituted .beta.-cyclodextrin; (3) cellulose or a derivative selected from sodium carboxymethyl cellulose, ethyl cellulose, and cellulose acetate; (4) powdered tragacanth; (5) malt; (6) gelatin; (7) talc; (8) an excipient selected from cocoa butter and suppository waxes; (9) an oil selected from peanut oil, cottonseed oil, safflower oil, sesame oil, olive oil, corn oil, and soybean oil; (10) propylene glycol; (11) a polyol selected from glycerin, sorbitol, mannitol, and polyethylene glycol; (12) an ester selected from ethyl oleate and ethyl laurate; (13) agar; (14) a buffering agent selected from magnesium hydroxide and aluminum hydroxide; (15) alginic acid; (16) pyrogen-free water; (17) isotonic saline; (18) Ringer's solution; (19) ethyl alcohol; (20) phosphate buffer solutions; and (21) other non-toxic compatible substances employed in pharmaceutical formulations.

4. The method of claim 1, wherein at least one of the one or more pharmaceutically acceptable carriers is a cyclodextrin.

5. The method of claim 1, wherein at least one of the one or more pharmaceutically acceptable carriers is a substituted or unsubstituted .beta.-cyclodextrin.

6. The method of claim 1, wherein at least one of the one or more pharmaceutically acceptable carriers is a buffer.

7. The method of claim 1, wherein the composition further comprises an anti-oxidant.

8. The method of claim 7, wherein the anti-oxidant is citric acid.

9. A method, which comprises: (i) providing a composition that includes: (a) a compound having the formula: ##STR00030## or a pharmaceutically acceptable salt thereof; and (b) one or more pharmaceutically acceptable carriers; wherein the composition is in a solid form that is suitable for reconstitution in a sterile injectable medium; and (ii) mixing the composition with a sterile injectable medium.

10. The method of claim 9, wherein the sterile injectable medium is sterile water.

11. The method of claim 9, wherein each of the one or more pharmaceutically acceptable carriers is independently selected from a binder, a disintegrating agent, a lubricant, a corrigent, a solubilizing agent, a suspension aid, an emulsifying agent, a coating agent, a cyclodextrin, and a buffer.

12. The method of claim 9, wherein each of the one or more pharmaceutically acceptable carriers is independently selected from: (1) a sugar selected from lactose, glucose, and sucrose; (2) a starch selected from corn starch, potato starch, and substituted or unsubstituted .beta.-cyclodextrin; (3) cellulose or a derivative selected from sodium carboxymethyl cellulose, ethyl cellulose, and cellulose acetate; (4) powdered tragacanth; (5) malt; (6) gelatin; (7) talc; (8) an excipient selected from cocoa butter and suppository waxes; (9) an oil selected from peanut oil, cottonseed oil, safflower oil, sesame oil, olive oil, corn oil, and soybean oil; (10) propylene glycol; (11) a polyol selected from glycerin, sorbitol, mannitol, and polyethylene glycol; (12) an ester selected from ethyl oleate and ethyl laurate; (13) agar; (14) a buffering agent selected from magnesium hydroxide and aluminum hydroxide; (15) alginic acid; (16) pyrogen-free water; (17) isotonic saline; (18) Ringer's solution; (19) ethyl alcohol; (20) phosphate buffer solutions; and (21) other non-toxic compatible substances employed in pharmaceutical formulations.

13. The method of claim 9, wherein at least one of the one or more pharmaceutically acceptable carriers is a cyclodextrin.

14. The method of claim 9, wherein at least one of the one or more pharmaceutically acceptable carriers is a substituted or unsubstituted .beta.-cyclodextrin.

15. The method of claim 9, wherein at least one of the one or more pharmaceutically acceptable carriers is a buffer.

16. The method of claim 9, wherein the composition further comprises an anti-oxidant.

17. The method of claim 16, wherein the anti-oxidant is citric acid.

18. The method of claim 9, wherein step (ii) provides a second composition that is in the form of an aqueous solution, dispersion, suspension or emulsion.

19. The method of claim 18, wherein the second composition is in a form suitable for intravenous administration.

20. A composition prepared by the method as claimed in claim 1.

21. A composition prepared by the method as claimed in claim 9.
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