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Claims for Patent: 8,207,125

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Claims for Patent: 8,207,125

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:13/334,288
Patent Claims: 1. A compound having the formula: ##STR00031##

2. A pharmaceutically acceptable salt of a compound having the formula: ##STR00032##

3. The pharmaceutically acceptable salt of claim 2, wherein the pharmaceutically acceptable salt is a citrate salt.

4. A composition comprising a compound having the formula: ##STR00033## or a pharmaceutically acceptable salt thereof; and one or more pharmaceutically acceptable carriers.

5. The composition of claim 4, wherein the composition comprises a compound having the formula: ##STR00034## and one or more pharmaceutically acceptable carriers.

6. The composition of claim 4, wherein the composition comprises a pharmaceutically acceptable salt of a compound having the formula: ##STR00035## and one or more pharmaceutically acceptable carriers.

7. The composition of claim 4, 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.

8. The composition of claim 4, 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 (3-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.

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

10. The composition of claim 4, wherein at least one of the one or more pharmaceutically acceptable carriers is a substituted or unsubstituted (3-cyclodextrin.

11. The composition of claim 4, wherein at least one of the one or more pharmaceutically acceptable carriers is a buffer.

12. The composition of claim 4, wherein the composition further comprises an anti-oxidant.

13. The composition of claim 12, wherein the anti-oxidant is citric acid.

14. The composition of claim 4, wherein the composition further comprises one or more other therapeutic agents.

15. The composition of claim 14, wherein at least one of the one or more other therapeutic agents is a chemotherapeutic agent.

16. The composition of claim 4, wherein the composition is in a form suitable for intravenous administration.

17. The composition of claim 4, wherein the compound or salt is in hydrated form.

18. The composition of claim 4, wherein the composition is in a solid form that is suitable for reconstitution in a sterile injectable medium.

19. A composition comprising: (i) a compound having the formula: ##STR00036## or a pharmaceutically acceptable salt thereof; and (ii) water.

20. The composition of claim 19, wherein the water is sterile water.

21. The composition of claim 19, wherein the composition further comprises one or more other pharmaceutically acceptable carriers.

22. The composition of claim 21, wherein each of the one or more other 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.

23. The composition of claim 21, wherein each of the one or more other pharmaceutically acceptable carriers is each 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 3-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.

24. The composition of claim 21, wherein at least one of the one or more other pharmaceutically acceptable carriers is a cyclodextrin.

25. The composition of claim 21, wherein at least one of the one or more other pharmaceutically acceptable carriers is a substituted or unsubstituted 3-cyclodextrin.

26. The composition of claim 21, wherein at least one of the one or more other pharmaceutically acceptable carriers is a buffer.

27. The composition of claim 19, wherein the composition further comprises an anti-oxidant.

28. The composition of claim 27, wherein the anti-oxidant is citric acid.

29. The composition of claim 19, wherein the composition is in the form of an aqueous solution, dispersion, suspension or emulsion.

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