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Details for Patent: 8,207,124

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Details for Patent: 8,207,124

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)
Filing Date:Dec 22, 2011
Application Number:13/334,263
Claims:1. A method for reducing the rate of p53 protein degradation in one or more cells, the method comprising contacting one or more cells with a compound having the formula: ##STR00033## or a pharmaceutically acceptable salt thereof.

2. The method of claim 1, wherein at least one of the one or more cells is a cancer cell.

3. The method of claim 1, wherein said contacting is in vitro.

4. The method of claim 1, wherein said contacting is in vivo.

5. The method of claim 4, wherein the compound or pharmaceutically acceptable salt thereof is in the form of a composition comprising the compound or pharmaceutically acceptable salt thereof and one or more pharmaceutically acceptable carriers.

6. The method of claim 5, 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.

7. The method of claim 5, 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.

8. The method of claim 5, wherein at least one of the one or more pharmaceutically acceptable carriers is a cyclodextrin.

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

10. The method of claim 5, wherein at least one of the one or more pharmaceutically acceptable carriers is a buffer.

11. The method of claim 5, wherein the composition further comprises an anti-oxidant.

12. The method of claim 11, wherein the anti-oxidant is citric acid.

13. A method for inhibiting cell proliferation that is associated with a cyclin-related cancer, the method comprising contacting at least one cell associated with a cyclin-related cancer with a compound having the formula: ##STR00034## or a pharmaceutically acceptable salt thereof.

14. The method of claim 13, wherein said contacting is in vitro.

15. The method of claim 13, wherein said contacting is in vivo.

16. The method of claim 15, wherein the compound or pharmaceutically acceptable salt thereof is in the form of a composition comprising the compound or pharmaceutically acceptable salt thereof and one or more pharmaceutically acceptable carriers.

17. The method of claim 16, 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.

18. The method of claim 16, 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.

19. The method of claim 16, wherein at least one of the one or more pharmaceutically acceptable carriers is a cyclodextrin.

20. The method of claim 16, wherein at least one of the one or more pharmaceutically acceptable carriers is a substituted or unsubstituted .beta.-cyclodextrin.

21. The method of claim 16, wherein at least one of the one or more pharmaceutically acceptable carriers is a buffer.

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

23. The method of claim 22, wherein the anti-oxidant is citric acid.

24. A method for inhibiting the growth of a p53-related cancer or a cyclin-related cancer in a subject, the method comprising administering to the subject an effective amount of a compound having the formula: ##STR00035## or a pharmaceutically acceptable salt thereof.

25. The method of claim 24, wherein the compound or pharmaceutically acceptable salt thereof is in the form of a composition comprising the compound or pharmaceutically acceptable salt thereof and one or more pharmaceutically acceptable carriers.

26. The method of claim 25, 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.

27. The method of claim 25, 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.

28. The method of claim 25, wherein the composition further comprises an anti-oxidant.

29. The method of claim 28, wherein the anti-oxidant is citric acid.

30. The method of claim 24, wherein compound or pharmaceutically acceptable salt thereof is administered by intravenous administration.
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