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1. WO2016083992 - EXTRAITS TITRÉS DE CYNARA SCOLYMUS ET LEURS UTILISATIONS

Note: Texte fondé sur des processus automatiques de reconnaissance optique de caractères. Seule la version PDF a une valeur juridique

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CLAIMS

1. An extract of Cynara scolymus or a fraction of extract of Cynara scolymus or a mixture of said extract with one or more of said fractions or a mixture of said fractions, titrated in total caffeoylquinic acids, in chlorogenic acid and in cynaropicrin, wherein

total caffeoylquinic acids represent from 8% to 16% by weight of said extract or of said fraction or of said mixture in dry form, chlorogenic acid represents from 3.5% to 7% by weight of said extract or of said fraction or of said mixture in dry form, and said cynaropicrin represents from 0.2% to 4% by weight of said extract or of said fraction or of said mixture in dry form or wherein

total caffeoylquinic acids represent from 25% to 48% by weight of said fraction in dry form, chlorogenic acid represents from 1 1 % to 21 % by weight of said fraction in dry form, and said cynaropicrin represents from 1 % to 10% by weight of said fraction in dry form

in association with one or more anti-tumour or anti-inflammatory compounds, for use in the prevention and/or in the treatment of an inflammatory and/or pre-tumour and/or tumour pathological condition characterised by a constitutive or anomalous activation of the STAT3 transcription factor.

2. The extract of Cynara scolymus or fraction of extract of Cynara scolymus or mixture of said extract with one or more of said fractions or mixture of said fractions for use according to claim 1 , wherein

said total caffeoylquinic acids represent from 9% to 15% by weight of said extract or of said fraction or of said mixture in dry form, said chlorogenic acid represents from 3.5% to 5.5% by weight of said extract or of said fraction or of said mixture in dry form, and said cynaropicrin represents from 0.2% to 3% by weight of said extract or of said fraction or of said mixture in dry form or wherein

said total caffeoylquinic acids represent from 25% to 35% by weight of said fraction in dry form, said chlorogenic acid represents from 1 1 % to 15% by weight of said fraction in dry form, and said cynaropicrin represents from 1 % to 8% by weight of said fraction in dry form.

3. The extract of Cynara scolymus or fraction of extract of Cynara scolymus or mixture of said extract with one or more of said fractions or mixture of said fractions according to any one of claims 1 or 2, wherein said extract, said fraction or said mixture is in a dry, lyophilised or fluid form and is obtained from Cynara leaves, f lower-heads or mixtures thereof.

4. The extract of Cynara scolymus or fraction of extract of Cynara scolymus or mixture of said extract with one or more of said fractions or mixture of said fractions in association with one or more anti-tumour compounds and/or anti-inflammatory compounds for use according to any one of claims 1 to 3, wherein said association is carried out by concomitant or sequential administration of said extract or of said fraction, or of said mixture, with said one or more anti-tumour compounds and/or with said one or more anti-inflammatory compounds.

5. The extract of Cynara scolymus or fraction of extract of Cynara scolymus or mixture of said extract with one or more of said fractions or mixture of said fractions in association with one or more anti-tumour compounds for use according to any one of claims 1 to 4, wherein said one or more anti-tumour compounds are selected from the group comprising cisplatinum, doxorubicin, pemetrexed, methotrexate, vinorelbine, gemcitabine and taxol.

6. The extract of Cynara scolymus or fraction of extract of Cynara scolymus or mixture of said extract with one or more of said fractions or mixture of said fractions in association with one or more anti-tumour compounds for use according to any one of claims 1 to 5, wherein said pathological state is a tumour pathological state selected from the group comprising: prostate cancer, multiple myeloma, leukaemia, lymphoma, melanoma, carcinoma of the ovaries, breast cancer, renal cell carcinoma, pancreatic adenocarcinoma, lung cancer, brain cancer, erythroleukaemia, squamous-cell carcinoma of the head and neck, colon cancer, malignant pleural mesothelioma.

7. The extract of Cynara scolymus or fraction of extract of Cynara scolymus or mixture of said extract with one or more of said fractions or mixture of said fractions in association with one or more anti-tumour compounds for use according to claim

6. wherein said brain tumour is glioma, brain meningioma, medulloblastoma, wherein said lymphoma is Sezary syndrome, EBV associated Buckitt lymphoma, Samiri HSV-dependent lymphoma, cutaneous T-cell related lymphoma; wherein said leukaemia is HTLV-l-dependent leukaemia, chronic lymphocytic leukaemia (CLL), acute myelogenous leukaemia (AML), megakaryocyte leukaemia, large granular lymphocytes leukaemia (LGL).

8. The extract of Cynara scolymus or fraction of extract of Cynara scolymus or mixture of said extract with one or more of said fractions or mixture of said fractions in association with one or more anti-tumour compounds for use according to any one of claims 1 to 7, wherein said pathological condition is a tumour resistant to treatment with chemotherapeutic agents which do not inhibit STAT3.

9. The extract of Cynara scolymus or fraction of extract of Cynara scolymus or mixture of said extract with one or more of said fractions or mixture of said fractions in association with one or more anti-inflammatory compounds for use according to any one of claims 1 to 4, wherein said inflammatory condition is an inflammation caused by viral infections such as infection by H pylori, infections by hepatitis B virus, infections by HPV (human papilloma virus), Epstein-Barr virus infections.

10. A composition comprising as active pharmaceutical ingredients:

a) an extract of Cynara scolymus or a fraction of extract of Cynara scolymus or a mixture of said extract with one or more of said fractions or a mixture of said fractions, titrated in total caffeoylquinic acids, in chlorogenic acid and in cynaropicrin, wherein

total caffeoylquinic acids represent from 8% to 16% by weight of said extract or of said fraction or of said mixture in dry form, chlorogenic acid represents from 3.5% to 7% by weight of said extract or of said fraction or of said mixture in dry form, and said cynaropicrin represents from 0.2% to 4% by weight of said extract or of said fraction or of said mixture in dry form;

or wherein

total caffeoylquinic acids represent from 25% to 48% by weight of said fraction in dry form, chlorogenic acid represents from 1 1 % to 21 % by weight of said fraction in dry form, and said cynaropicrin represents from 1 % to 10% by weight of said fraction in dry form;

b) one or more anti-tumour and/or anti-inflammatory compounds;

and a carrier and/or diluent and/or excipient for use in the prevention and/or treatment of an inflammatory and/or pre-tumour and/or tumour pathological condition characterised by a constitutive or anomalous activation of the STAT3 transcription factor.

1 1. The composition for use according to claim 10, wherein

said total caffeoylquinic acids represent from 9% to 15% by weight of said extract or of said fraction or of said mixture in dry form, said chlorogenic acid represents from 3.5% to 5.5% by weight of said extract or of said fraction or of said mixture in dry form, and said cynaropicrin represents from 0.2% to 3% by weight of said extract or of said fraction or of said mixture in dry form; or wherein

said total caffeoylquinic acids represent from 25% to 35% by weight of said fraction in dry form, said chlorogenic acid represents from 1 1 % to 15% by weight of said fraction in dry form, and said cynaropicrin represents from 1 % to 8% by weight of said fraction in dry form.

12. The composition for use according to claims 10 or 11 , wherein said one or more anti-tumour compounds are selected from the group comprising cisplatinum, doxorubicin, pemetrexed, methotrexate, vinorelbine, gemcitabine and taxol.

13. The composition for use according to any one of claims 10 to 12, wherein said pathological condition is a tumour pathological condition selected from the group comprising: prostate cancer, multiple myeloma, leukaemia, lymphoma, melanoma, carcinoma of the ovaries, breast cancer, renal cell carcinoma, pancreatic adenocarcinoma, lung cancer, brain cancer, erythroleukaemia, squamous-cell carcinoma of the head and neck, colon cancer, malignant pleural mesothelioma.

14. The composition for use according to claim 13, wherein said brain tumour is glioma, brain meningioma, medulloblastoma, wherein said lymphoma is Sezary syndrome, EBV associated Buckitt lymphoma, Samiri HSV-dependent lymphoma, cutaneous T-cell related lymphoma; wherein said leukaemia is HTLV-l-dependent leukaemia, chronic lymphocytic leukaemia (CLL), acute myelogenous leukaemia (AML), megakaryocytic leukaemia, large granular lymphocytes leukaemia (LGL).

15. The composition for use according to any one of claims 10 to 14, wherein said pathological condition is a tumour resistant to treatment with chemotherapeutic agents that do not inhibit STAT3.

16. The composition for use according to claim 10 or 1 1 , wherein said inflammatory condition and/or pre-tumour condition is an inflammation caused by viral infections such as infection by H pylori, infection by hepatitis B virus, infections by HPV (human papilloma virus), Epstein-Barr virus infections.

17. A kit for concomitant or sequential administration of an extract of Cynara scolymus or a fraction of extract of Cynara scolymus or a mixture of said extract with one or more of said fractions or a mixture of said fractions and one or more anti-tumour compounds and/or one or more anti-inflammatory compounds, comprising:

- one or more aliquots of an extract of Cynara scolymus or a fraction of extract of Cynara scolymus or a mixture of said extract with one or more of said fractions or a mixture of said fractions, titrated in total caffeoylquinic acids, in chlorogenic acid and in cynaropicrin, wherein total caffeoylquinic acids represent from 8% to 16% by weight of said extract or of said fraction or of said mixture in dry form, chlorogenic acid represents from 3.5% to 8% by weight of said extract or of said fraction or of said mixture in dry form, and said cynaropicrin represents from 0.2% to 4% by weight of said extract or of said fraction or of said mixture in dry form, and

- one or more aliquots of one or more anti-tumour compounds and/or one or more aliquots of one or more anti-inflammatory compounds for use in the prevention and/or in the treatment of an inflammatory and/or pre-tumour and/or tumour pathological condition characterised by a constitutive or anomalous activation of the STAT3 transcription factor.

18. The kit according to claim 17, wherein said total caffeoylquinic acids represent from 9% to 15% by weight of said extract or of said fraction or of said mixture in dry form, said chlorogenic acid represents from 3.5% to 5.5% by weight of said extract or of said fraction or of said mixture in dry form, and said cynaropicrin represents from 0.2% to 3% by weight of said extract or of said fraction or of said mixture in dry form.

19. The kit according to claim 17 or 18, wherein said one or more anti-tumour compounds is/are selected from the group comprising cisplatinum, doxorubicin, pemetrexed, methotrexate, vinorelbine, gemcitabine and taxol.

20. The kit according to any one of claims 17 to 19, wherein said pathology is a tumour pathology selected from the group comprising: prostate cancer, multiple myeloma, leukaemia, lymphoma, melanoma, carcinoma of the ovaries, breast cancer, renal cell carcinoma, pancreatic adenocarcinoma, lung cancer, brain cancer, erythroleukaemia, squamous-cell carcinoma of the head and neck, colon cancer, malignant pleural mesothelioma.

21. The kit according to claim 20, wherein brain tumour is glioma, brain meningioma, medulloblastoma, wherein said lymphoma is Sezary syndrome, EBV associated Buckitt lymphoma, Samiri HSV-dependent lymphoma, cutaneous T-cell related lymphoma; wherein said leukaemia is HTLV-l-dependent leukaemia, chronic lymphocytic leukaemia (CLL), acute myelogenous leukaemia (AML), megakaryocyte leukaemia, large granular lymphocytes leukaemia (LGL).

22. The kit according to any one of claims 17 to 21 , wherein said pathological condition is a tumour resistant to treatment with chemotherapeutic agents that do not inhibit STAT3.

23. The kit according to claim 17 or 20-21 , wherein said inflammatory and/or pre-tumour condition may be an inflammation caused by viral infections (as noted in the literature), such as infections by H pylori, infections by hepatitis B virus, infections by HPV (human papilloma virus), infections by Epstein-Barr virus.