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Last Updated: March 28, 2024

Claims for Patent: 9,132,113


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Summary for Patent: 9,132,113
Title:Compositions and methods of use of phorbol esters
Abstract: Methods and compositions containing a phorbol ester or a derivative of a phorbol ester are provided for the treatment of cytopathic diseases. Cytopathic diseases may be caused by a variety means such as viral infections like HIV and AIDS in a mammalian subject. The methods and compositions of the invention are effective for inhibiting de novo HIV infection, upregulating viral expression from latent provirus, inhibiting HIV-induced cytopathic effects, down regulating the HIV receptor, increasing ThI cytokine expression, and decreasing Th2 cytokine expression. Additional compositions and methods are provided which employ a phorbol ester or derivative compound in combination with at least one additional agent such as those used in HAART protocols or therapeutic agents used to treat opportunistic infections due to HIV in mammalian subjects.
Inventor(s): Han; Zheng Tao (Zhengzhou, CN), Chang; Richard L. (Pinebrook, NJ)
Assignee: BIOSUCCESS BIOTECH COMPANY (Los Angeles, CA)
Application Number:13/794,467
Patent Claims:1. A method for treating HIV infection or disease-in a mammalian subject comprising administering an effective amount of a phorbol ester of Formula II, a pharmaceutically-acceptable salt, isomer, enantiomer, solvate, hydrate, or polymorph thereof to said mammalian subject ##STR00017## ##STR00018## ##STR00019##

2. The method of claim 1, wherein the phorbol ester is 12-O-tetradecanoylphorbol-13-acetate.

3. The method of claim 1, further comprising administering at least one secondary or anti-retroviral or other adjunctive therapeutic agent with said phorbol ester.

4. The method of claim 3, wherein the at least one secondary anti-retroviral or other adjunctive therapeutic agent is administered to said subject simultaneously with, prior to, or after, administration of said phorbol ester.

5. The method of claim 3, wherein the at least one secondary anti-retroviral or other adjunctive therapeutic agent is selected from the group consisting oft protease inhibitors, nucleoside reverse transcriptase, non-nucleoside reverse transcriptase inhibitors, combination drugs, entry and fusion inhibitors, acyclovir, adefovir dipivoxil, aldesleukin, amphotericin b, azithromycin, calcium hydroxylapatite, clarithromycin, doxorubicin, dronabinol, entecavir, epoetin alfa, etoposide, fluconazole, ganciclovir, immunoglobulins, interferon alfa-2, isoniazid, itraconazole, megestrol, paclitaxel, peginterferon alfa-2, pentamidine, poly-1-lactic acid, ribavirin, rifabutin, rifampin, somatropin, testosterone, trimetrexate, valganciclovir; integrase inhibitors, microbicides, and IL-2.

6. The method of claim 1, wherein said effective amount is between about 10 and 1500 .mu.g of said phorbol ester every other day.

7. The method of claim 1, wherein said effective amount is between about 150 to 500 .mu.g of said phorbol ester every other day.

8. The method of claim 1, wherein said effective amount of said phorbol ester is administered once per day.

9. A method for treating one or more symptoms or conditions of HIV infection or AIDS in a mammalian subject comprising administering an effective amount of phorbol ester of Formula II, a pharmaceutically-acceptable salt, isomer, enantiomer, solvate, hydrate, or polymorph thereof to said mammalian subject ##STR00020## ##STR00021## ##STR00022## R is selected from hydrogen, and substituted derivatives thereof.

10. The method of claim 9, wherein the phorbol ester is 12-O-tetradecanoylphobol-13-acetate.

11. The method of claim 9, further comprising administering at least one secondary anti-retroviral or other adjunctive therapeutic agent with said phorbol ester.

12. The method of claim 11, wherein the at least one secondary anti-retroviral or other adjunctive therapeutic agent is administered simultaneously with, prior to, or after, administration of said phorbol ester.

13. The method of claim 11, wherein the at least one secondary anti-retroviral or other adjunctive therapeutic agent is selected from the group consisting oft protease inhibitors, nucleoside reverse transcriptase, non-nucleoside reverse transcriptase inhibitors, combination drugs, entry and fusion inhibitors, acyclovir, adefovir dipivoxil, aldesleukin, amphotericin b, azithromycin, calcium hydroxylapatite, clarithromycin, doxorubicin, dronabinol, entecavir, epoetin alfa, etoposide, fluconazole, ganciclovir, immunoglobulins, interferon alfa-2, isoniazid, itraconazole, megestrol, paclitaxel, peginterferon alfa-2, pentamidine, poly-1-lactic acid, ribavirin, rifabutin, rifampin, somatropin, testosterone, trimetrexate, valganciclovir; integrase inhibitors, microbicides, and IL-2.

14. The method of claim 9, wherein the one or more symptoms is selected from the group consisting of oral lesions, fatigue, skin thrush, fever, lack of appetite, diarrhea, apthous ulcers, malabsorbtion, thrombocytopenia, weight loss, anemia, and lymph node enlargement, mycobacterium avium complex, salmonellosis, syphilis, neuroshyphilis, turberculosis, bacillary angiomatosis, aspergillosis, candidiasis, coccidioidomycosis, listeriosis, pelvic inflammatory disease, Burkitt's lymphoma, cryptococcal meningitis, histoplasmosis, Kaposi's sarcoma, lymphoma, systemic non-Hodgkin's lymphoma, primary CNS lymphoma, cryptosporidiosis, isosporiasis, microsporidiosis, pneumocystis carinii pneumonia, toxoplasmosis, cytomegalovirus, hepatitis, herpes simplex, herpes zoster, human papiloma virus, molluscum contagiosum, oral hairy leukoplakia, and progressive multifocal leukoencephalopathy.

15. A method for treating HIV infection in a mammalian subject with AIDS comprising administering an effective amount of a phorbol ester of Formula II, a pharmaceutically-acceptable salt, isomer, enantiomer, solvate, hydrate, or polymorph thereof, to said mammalian subject ##STR00023## ##STR00024## ##STR00025##

16. The method of claim 15, wherein the phorbol ester is 12-O-tetradecanoylphorbol-13-acetate.

17. A method for activating latent reservoirs of HIV comprising administering an effective amount of a phorbol ester of Formula II, a pharmaceutically-acceptable salt, isomer, enantiomer, solvate, hydrate, or polymorph thereof to said mammalian subject ##STR00026## ##STR00027## ##STR00028##

18. The method of claim 17, wherein the phorbol ester is 12-O-tetradecanoylphorbol-13-acetate.

19. The method of claim 17, further comprising administering a secondary anti-retroviral or other adjunctive therapeutic agent with said phorbol ester.

20. The method of claim 19, wherein the secondary anti-retroviral or adjunctive therapeutic agent is administered to said subject simultaneously with, prior to, or after, administration of said phorbol ester.

21. The method of claim 19, wherein the secondary anti-retroviral or adjunctive therapeutic agent is selected from the group consisting of protease inhibitors, nucleoside reverse transcriptase, non-nucleoside reverse transcriptase inhibitors, combination drugs, entry and fusion inhibitors, acyclovir, adefovir dipivoxil, aldesleukin, amphotericin b, azithromycin, calcium hydroxylapatite, clarithromycin, doxorubicin, dronabinol, entecavir, epoetin alfa, etoposide, fluconazole, ganciclovir, immunoglobulins, interferon alfa-2, isoniazid, itraconazole, megestrol, paclitaxel, peginterferon alfa-2, pentamidine, poly-1-lactic acid, ribavirin, rifabutin, rifampin, somatropin, testosterone, trimetrexate, valganciclovir; integrase inhibitors, microbicides, and IL-2.

22. The method of claim 17, wherein said effective amount is between about 10 and 1500 .mu.g of said phorbol ester every other day.

23. The method of claim 17, wherein said effective amount is between about 150 to 500 .mu.g of said phorbol ester every other day.

24. The method of claim 17, wherein said effective amount of said phorbol ester is administered once per day.

25. A method of increasing the expression of Th1 cytokines comprising administering an effective amount of a phorbol ester of Formula II, a pharmaceutically-acceptable salt, isomer, enantiomer, solvate, hydrate, or polymorph thereof to said mammalian subject ##STR00029## ##STR00030## ##STR00031##

26. The method of claim 25, wherein the phorbol ester is 12-O-tetradecanoylphorbol-13-acetate.

27. The method of claim 25, further comprising administering a secondary or other adjunctive therapeutic agent with said phorbol ester.

28. The method of claim 27, wherein the secondary or adjunctive therapeutic agent is administered to said subject simultaneously with, prior to, or after, administration of said phorbol ester.

29. The method of claim 27, wherein the secondary or adjunctive therapeutic agent is selected from the group consisting oft protease inhibitors, nucleoside reverse transcriptase, non-nucleoside reverse transcriptase inhibitors, combination drugs, entry and fusion inhibitors, acyclovir, adefovir dipivoxil, aldesleukin, amphotericin b, azithromycin, calcium hydroxylapatite, clarithromycin, doxorubicin, dronabinol, entecavir, epoetin alfa, etoposide, fluconazole, ganciclovir, immunoglobulins, interferon alfa-2, isoniazid, itraconazole, megestrol, paclitaxel, peginterferon alfa-2, pentamidine, poly-1-lactic acid, ribavirin, rifabutin, rifampin, somatropin, testosterone, trimetrexate, valganciclovir; integrase inhibitors, microbicides, and IL-2.

30. The method of claim 25, wherein said effective amount is between about 10 and 1500 .mu.g of said phorbol ester every other day.

31. The method of claim 25, wherein said effective amount is between about 150 to 500 .mu.g of said phorbol ester every other day.

32. The method of claim 25, wherein said effective amount of said phorbol ester is administered once per day.

Details for Patent 9,132,113

Applicant Tradename Biologic Ingredient Dosage Form BLA Approval Date Patent No. Expiredate
Eli Lilly And Company HUMATROPE somatropin For Injection 019640 06/23/1987 ⤷  Try a Trial 2027-01-31
Eli Lilly And Company HUMATROPE somatropin For Injection 019640 10/16/1986 ⤷  Try a Trial 2027-01-31
Eli Lilly And Company HUMATROPE somatropin For Injection 019640 02/04/1999 ⤷  Try a Trial 2027-01-31
Emd Serono, Inc. SAIZEN somatropin For Injection 019764 10/08/1996 ⤷  Try a Trial 2027-01-31
Emd Serono, Inc. SAIZEN somatropin For Injection 019764 08/29/2000 ⤷  Try a Trial 2027-01-31
Emd Serono, Inc. SAIZEN somatropin For Injection 019764 01/16/2007 ⤷  Try a Trial 2027-01-31
Ferring Pharmaceuticals Inc. ZOMACTON somatropin For Injection 019774 05/25/1995 ⤷  Try a Trial 2027-01-31
>Applicant >Tradename >Biologic Ingredient >Dosage Form >BLA >Approval Date >Patent No. >Expiredate

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