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Last Updated: October 23, 2021

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Claims for Patent: 9,770,406


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Summary for Patent: 9,770,406
Title:Medicament for the treatment of viral skin and tumour diseases
Abstract: The invention relates to a medicament containing a compound of general formula (I), where R.sub.1=independently, a straight or branched, saturated, singly- or multiply-unsaturated, optionally substituted C.sub.11-C.sub.21 alkyl, alkylene or alkinyl group, preferably a C.sub.11-C.sub.15 alkyl, alkylene or alkinyl group, particularly a C.sub.11-C.sub.13 alkyl, alkylene or alkinyl group, most preferably a C.sub.13 alkyl group, R.sub.2=independently, a straight or branched C.sub.1-C.sub.8 alkyl, alkylene or alkinyl group, preferably a C.sub.1-C.sub.6 alkyl, alkylene or alkinyl group, in particular a C.sub.2-C.sub.4 alkyl, alkylene or alkinyl group, most preferably a C.sub.3 alkyl group, a --[CH.sub.2--(CH.sub.2)m-O].sub.nH group with n=1 to 10, preferably n=1 to 5, to m=1 to 5, preferably m=1 to 3, a --CH.sub.2--[CH--(OH)].sub.p[CH.sub.2--R.sub.3]- group, where R.sub.3=independently H or OH, p=1 to 7, preferably p=1 to 4, a pentose group or a hexose group, as therapeutically active agent, alone or in combination with one or several further pharmaceutical agents as a combination preparation for the treatment of viral skin diseases and/or tumor diseases, in particular caused by human papilloma virus (HPV) and/or herpes viruses and a topically acting medicament formulation and the use thereof.
Inventor(s): Chang; Yunik (Sonoma, CA), Lathrop; Robert (Fort Collins, CO), Bohm; Erwin (Ladenburg, DE), Gander-Meisterernst; Irene (Stockdorf, DE), Greger; Regina (Iffeldorf, DE), Holldack; Johanna (Aarhus C, DK), Moebius; Ulrich (Gauting-Unterbrunn, DE)
Assignee: Medigene AG (Planegg/Martinsried, DE)
Application Number:12/887,250
Patent Litigation and PTAB cases: See patent lawsuits and PTAB cases for patent 9,770,406
Patent Claims: 1. A pharmaceutical composition comprising: (i) a compound having the formula A-B (I), wherein A is a radical having the formula ##STR00005## and wherein B is a radical having the formula --O--R.sub.2 (III), and wherein R.sub.1 is, independent of each other, an unbranched or branched, saturated, singly or multiply unsaturated, optionally substituted C.sub.13-C.sub.21 alkyl, alkylene, or alkynyl radical, and R.sub.2 is, independent of each other, an unbranched or branched C.sub.1-C.sub.8 alkyl, alkylene, or alkynyl radical; and (ii) a mixture of catechols comprising 2-20% (w/w) of (-)-epicatechol, 2-20% (w/w) of (-)-epicatechol gallate, 1-25% (w/w) of (-)-epigallocatechol, 40-75% (w/w) of (-) -epigallocatechol gallate, 0.05-5% (w/w) of (-)-gallocatechol, and 0.5-20% (w/w) of (-)-gallocatechol gallate; and wherein the pharmaceutical comprises at least 5-50% (w/w) of the compound of formula (I).

2. The pharmaceutical composition of claim 1, wherein said pharmaceutical composition comprises 1-30% (w/w) of said mixture of catechols and at least 10-50% (w/w) of said compound of formula (I).

3. The pharmaceutical composition of claim 2, wherein said pharmaceutical composition comprises 2-20% (w/w) of said mixture of catechols.

4. The pharmaceutical composition of claim 3, wherein said pharmaceutical composition comprises 15-18% (w/w) of said mixture of catechols.

5. The pharmaceutical composition of claim 2, wherein said pharmaceutical composition comprises at least 25-50% (w/w) of said compound of formula (I).

6. The pharmaceutical composition of claim 5, wherein said pharmaceutical composition comprises at least 35-50% (w/w) of said compound of formula (I).

7. The pharmaceutical composition of claim 1, wherein said mixture of catechols comprises 5-7% (w/w) of said (-)-epicatechol gallate.

8. The pharmaceutical composition of claim 1, wherein said mixture of catechols comprises 0.1-0.6% (w/w) of said (-)-gallocatechol.

9. The pharmaceutical composition of claim 1, wherein said mixture of catechols comprises 1-5% (w/w) of said (-)-gallocatechol gallate.

10. The pharmaceutical composition of claim 1, wherein said mixture of catechols comprises 10.8% (w/w) of (-)-epicatechol, 6.5% (w/w) of (-)-epicatechol gallate, 9.2% (w/w) of (-)-epigallocatechol, 54.8% (w/w) of (-)-epigallocatechol gallate, and/or 4.0% (w/w) of (-)-gallocatechol gallate.

11. The pharmaceutical composition of claim 1, wherein said pharmaceutical composition comprises at least 10-50% (w/w) of said compound of formula (I).

12. The pharmaceutical composition of claim 11, wherein said pharmaceutical composition comprises at least 25-50% (w/w) of said compound of formula (I).

13. The pharmaceutical composition of claim 12, wherein said pharmaceutical composition comprises at least 35-50% (w/w) of said compound of formula (I).

14. The pharmaceutical composition of claim 1, wherein said catechols are isolated from a tea extract.

15. The pharmaceutical composition of claim 1, wherein one or more additional pharmaceutical compound(s) is/are administered simultaneously or separately.

16. The pharmaceutical composition of claim 15, wherein said one or more additional pharmaceutical compound(s) is/are amphiphilic.

17. The pharmaceutical composition of claim 1, further comprising additives and/or auxiliary substances.

18. The pharmaceutical composition of claim 17, wherein said additives and/or auxiliary substances are hydrophobic and are selected from the group consisting of petroleum jelly, wax, oleyl alcohol, propylene glycol monostearate, and propylene glycol monopalmitostearate.

19. A pharmaceutical composition comprising 35% (w/w) of a compound having the formula A-B (I), wherein A is a radical having the formula ##STR00006## and wherein B is a radical having the formula --O--R.sub.2 (III), and wherein R.sub.1 is, independent of each other, an unbranched or branched, saturated, singly or multiply unsaturated, optionally substituted C.sub.13-C.sub.21 alkyl, alkylene, or alkynyl radical, and R.sub.2 is, independent of each other, an unbranched or branched C.sub.1-C.sub.8 alkyl, alkylene, or alkynyl radical; and wherein said pharmaceutical composition further comprises 15% (w/w) of a mixture of catechols comprising 2-20% (w/w) of (-)-epicatechol, 2-20% (w/w) of (-)-epicatechol gallate, 1-25% (w/w) of (-)-epigallocatechol, 40-75% (w/w) of (-)-epigallocatechol gallate, 0.05-5% (w/w) of (-)-gallocatechol, and 0.5-20% (w/w) of (-)-gallocatechol gallate, 24.5% (w/w) of petroleum jelly, 20% (w/w) of wax, 5% (w/w) of propylene glycol monostearate or propylene glycol monopalmitostearate, and 0.5% (w/w) of oleyl alcohol.

20. A method of treating a papilloma virus-induced skin disease or papilloma virus-induced benign tumor disease in a patient, said method comprising administering to a patient a pharmaceutical composition of claim 1.

21. The method of claim 20, wherein said papilloma virus-induced skin disease or benign tumor disease is caused by HPV 1, 2, 3, 4, 5, 6, 8, 9, 11, 12, 13, 14, 15, 16, 17, 18, 19-29, 31, 32, 34, 36-38, 46-50, 56, or 58.

22. The method of claim 20, wherein said papilloma virus-induced skin diseases are warts or genital warts and the papilloma virus-induced benign tumors are of the skin and/or mucosa.

23. The method of claim 22, wherein said papilloma virus-induced benign tumors of the skin and/or mucosa are verrucae plantares, verrucae vulgares, verrucae planae juveniles, epidermodysplasia verruciformis, Condylomata acuminata, Condylomata plana, bowenoid papulosis, papillomas on the larynx and oral mucosa, or focal epithelial hyperplasia.

24. The method of claim 20, wherein said pharmaceutical composition is applied topically.

25. The method of claim 24, wherein said pharmaceutical composition is applied genitally or vaginally.

26. The pharmaceutical composition of claim 1, wherein the compound of formula (I) is isopropyl myristate.

27. The pharmaceutical composition of claim 1, wherein said mixture of catechols comprises 4-15% (w/w) of (-)-epicatechol, 2-20% (w/w) of (-)-epicatechol gallate, 3-15% (w/w) of (-)-epigallocatechol, 40-75% (w/w) of (-)-epigallocatechol gallate, 0.1-1% (w/w) of (-)-gallocatechol, and 1-10% (w/w) of (-)-gallocatechol gallate.

28. The pharmaceutical composition claim 19, wherein said mixture of catechols comprises 1, 4-15% (w/w) of (-)-epicatechol, 2-20% (w/w) of (-)-epicatechol gallate, 3-15% (w/w) of (-)-epigallocatechol, 40-75% (w/w) of (-)-epigallocatechol gallate, 0.1-1% (w/w) of (-)-gallocatechol, and 1-10% (w/w) of (-)-gallocatechol gallate.

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