US2002193434A1PendingUtilityA1
Anti-tumor composition
Est. expiryApr 3, 2018(expired)· nominal 20-yr term from priority
A61P 43/00A61P 35/00A61K 31/28A61K 31/555A61K 31/282A61K 33/243A61K 31/395A61K 31/075
53
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Claims
Abstract
The present invention provides composition having as active ingredients a stilbene derivative and a platinum coordination compound which is highly efficacious and highly safe for treating tumors, particularly for the treatment of solid or malignant tumors and thus methods of cancer and tumor treatment using the composition are also provided.
Claims
exact text as granted — not AI-modified1 . A composition comprising:
a stilbene derivative and a platinum coordination compound.
2 . The composition of claim 1 , wherein said stilbene derivative has a cis-stilbene skeleton.
3 . The composition of claim 1 , wherein said platinum coordination compound comprises a compound selected from the group consisting of cis-dichloro diamine platinum (II), cis-diamminediacoplatinum (II)-ion, chloro (diethylene -criamine)-platinum (II) chloride, dichloro (ethylene diamine)- platinum (II), diammine(1,1-cyclobutane dicarboxylate) platinum (II), spiroplatin, iproplatin, diammine (2-ethylmalonate)-platinum (II), ethylene diammine malonate platinum (II), aqua (1,2-diaminodichlohexane)-sulfate platinum (II) , (1,2-diaminocyclohexane) malonate platinum (II), (4-caloxyphthalate)-(1,2-diaminocyclohexane)-platinum (II), (1,2-diaminocyclohexane)-(isocitrate)-platinum (II), (1,2-diaminocyclohexane)-cis (pyruvate) platinum (II), (1,2-diaminocyclohexane)-oxalate platinum (II), Ormaplatin, tetraplatin, and Nedaplatin.
4 . The composition of claim 1 , wherein said stilbene derivative comprises a compound selected from the group consisting of compounds represented by formulas (1) and (2):
wherein
R 1 , R 2 and R 3 are each independently a lower alkoxy group;
R 4 , R 5 and R 6 are each independently selected from the group consisting of: hydrogen, a halogen, a nitro group, a hydroxyl group, a lower alkoxy group, a phosphoric acid ester, a phosphoric acid amide, an amino lower alkoxy group, a lower alkyl amino lower alkoxy group, a di-lower alkyl amino lower alkoxy group, a mercapto group, a lower alkyl thio group, an amino group, a lower alkyl amino group, a di-lower alkyl amino group, a lower alkyl group, an amino lower alkyl group, a trifluoromethyl group, a lower alkanoyl group, a lower alkanoyl amino group and an amino acid acylamino group;
X is a hydrogen atom or a nitrile group; and
Het is a heterocyclic ring;
or a salt, hydrate, solvate, metabolite, or pharmaceutically acceptable precursor thereof.
5 . The composition of claim 1 , wherein said stilbene derivative is represented by formula (1):
or a salt, hydrate, solvate thereof;
wherein
R 1 , R 2 , R 3 and R 5 are each a methoxy group;
R 4 is an amino group or an amino acid acylamino group; and
R 6 and X are hydrogen.
6 . The composition of claim 1 , wherein said stilbene derivative is represented by formula (3):
7 . The composition of claim 1 , wherein said platinum coordination compound is cis-dichloro diamine platinum (II).
8 . The composition of claim 1 , wherein said stilbene derivative is:
9 . The composition of claim 1 , wherein said stilbene derivative is:
10 . A method for inhibiting cancer or tumor growth comprising administering to a subject in need of treatment the composition of claim 1 in an amount sufficient to inhibit cancer or tumor growth.
11 . The method of claim 10 , wherein said tumor is a malignant or solid tumor.
12 . The method of claim 10 , further comprising administering at least one other anti-neoplastic or anti-tumor drug.
13 . The method of claim 10 , wherein administering comprises intravenous administration or infusion.
14 . A method of treating, ameliorating or suppressing a tumor comprising administering to a subject in need of treatment a stilbene derivative and a platinum coordination compound in an amount sufficient to treat, ameliorate or suppress the tumor.
15 . The method of claim 14 , wherein said stilbene derivative and said platinum coordination compound are administered sequentially.
16 . The method of claim 14 , wherein said stilbene derivative and said platinum coordination compound are administered by separate routes.
17 . The method of claim 14 , wherein the effects of administering the combination of the stilbene derivative and the platinum coordination compound are greater than the combined effects of either administered alone.
18 . The method of claim 14 , wherein said stilbene derivative has a cis-stilbene skeleton.
19 . The method of claim 14 , wherein said platinum coordination compound comprises a compound selected from the group consisting of cis-dichloro diamine platinum (II), cis-diamminediacoplatinum (II)-ion, chloro (diethylene -criamine)-platinum (II) chloride, dichloro (ethylene diamine)- platinum (II), diammine(1,1-cyclobutane dicarboxylate) platinum (II), spiroplatin, iproplatin, diammine (2-ethylmalonate)-platinum (II), ethylene diammine malonate platinum (II), aqua (1,2-diaminodichlohexane)-sulfate platinum (II), (1,2-diaminocyclohexane) malonate platinum (II), (4-caloxyphthalate)-(1,2-diaminocyclohexane)-platinum (II), (1,2-diaminocyclohexane)-(isocitrate)-platinum (II), (1,2-diaminocyclohexane)-cis (pyruvate) platinum (II), (1,2-diaminocyclohexane)-oxalate platinum (II), Ormaplatin, tetraplatin, and Nedaplatin.
20 . The method of claim 14 , wherein said stilbene derivative comprises a compound selected from the group consisting of compounds represented by formulas (1) and (2):
wherein
R 1 , R 2 and R 3 are each independently a lower alkoxy group;
R 4 , R 5 and R 6 are each independently selected from the group consisting of: hydrogen, a halogen, a nitro group, a hydroxyl group, a lower alkoxy group, a phosphoric acid ester, a phosphoric acid amide, an amino lower alkoxy group, a lower alkyl amino lower alkoxy group, a di-lower alkyl amino lower alkoxy group, a mercapto group, a lower alkyl thio group, an amino group, a lower alkyl amino group, a di-lower alkyl amino group, a lower alkyl group, an amino lower alkyl group, a trifluoromethyl group, a lower alkanoyl group, a lower alkanoyl amino group and an amino acid acylamino group;
X is a hydrogen atom or a nitrile group; and
Het is a heterocyclic ring;
or a salt, hydrate, solvate, metabolite, or pharmaceutically acceptable precursor thereof.
21 . The method of claim 14 , wherein said stilbene derivative is represented by formula (1):
or a salt, hydrate, solvate thereof;
wherein
R 1 , R 2 , R 3 and R 5 are each a methoxy group;
R 4 is an amino group or an amino acid acylamino group; and
R 6 and X are hydrogen.
22 . The method of claim 14 , wherein said stilbene derivative is represented by formula (3):
23 . The method of claim 14 , wherein said platinum coordination compound is cis-dichloro diamine platinum (II).
24 . The method of claim 14 , wherein said stilbene derivative is:
25 . The method of claim 14 , wherein said stilbene derivative is:Join the waitlist — get patent alerts
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