Novel cytotoxic compounds and their Use
AssigneeArdenia Investments, Ltd.
InventorOleg Strelchenok
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Abstract
Novel amides of polyunsaturated fatty acids with cysteamine-S-phosphate have been synthesized. Combinations of the all-trans-retinoic acid and/or amides of the 13-cis-retinoic acid with O-phospho-L-tyrosine, and N-docosahex-aenoyl-cysteamine-S-phosphate, N-eicosapentaenoyl-cysteamine-S-phosphate, N-arachidonoyl-cysteamine-S-phosphate, N-α-linolenoyl-cysteamine-S-phosphate, and N-γ-linolenoyl-cysteamine-S-phosphate and their analogues N-docosahex-aenoyl-O-phospho-2-aminoethanol, N-eicosapentaenoyl-O-phospho-2-aminoethanol, N-arachidonoyl-O-phospho-2-aminoethanol, N-α-linolenoyl-O-phospho-2-aminoethanol, N-γ-linolenoyl-O-phospho-2-aminoethanol in different compositions exhibit a marked cell-growth inhibiting effect and display anti-tumour activity.
Claims23
A substantially pure compound selected from the group consisting of N-docosahexaenoyl-cysteamine-S-phosphate, N-eicosapentaenoyl-cysteamine-S-phosphate, N-arachidonoyl-cysteamine-S-phosphate, N-α-linolenoyl-cysteamine-S-phosphate, and N-γ-linolenoyl-cysteamine-S-phosphate.
A pharmaceutical preparation, characterized in that it comprises a therapeutically effective amount of a compound selected from the group consisting of N-docosahexaenoyl-O-phospho-2-aminoethanol, N- eicosapentaenoyl O-phospho-2-aminoethanol, N-arachidonoyl O-phospho-2-aminoethanol, N-α-linolenoyl O-phospho-2-aminoethanol, and N-γ-linolenoyl O-phospho-2-aminoethanol.
A pharmaceutical preparation, characterized in that it comprises a therapeutically effective amount of a compound selected from the group consisting of N-docosahexaenoyl-O-phospho-2-aminoethanol, N-eicosapentaenoyl O-phospho-2-aminoethanol, N-arachidonoyl O-phospho-2-aminoethanol, N-α-linolenoyl O-phospho-2-aminoethanol, and N-γ-linolenoyl O-phospho-2-aminoethanol in combination with a therapeutically effective amount of N-(all-trans-retinoyl)-O-phospho-L-tyrosine.
A pharmaceutical preparation, characterized in that it comprises a therapeutically effective amount of a compound selected from the group consisting of N-docosahexaenoyl-O-phospho-2-aminoethanol, N-eicosapentaenoyl O-phospho-2-aminoethanol, N-arachidonoyl O-phospho-2-aminoethanol, N-α-linolenoyl O-phospho-2-aminoethanol, and N-γ-linolenoyl O-phospho-2-aminoethanol in combination with a therapeutically effective amount of N-(13-cis-retinoyl)-O-phospho-L-tyrosine.
A pharmaceutical preparation, characterized in that it comprises a therapeutically effective amount of N-docosahexaenoyl-cysteamine-S-phosphate and one of N-(all-trans-retinoyl)-O-phospho-L-tyrosine or N-(13-cis-retinoyl)-O-phospho-L-tyrosine.
A pharmaceutical preparation, characterized in that it comprises a therapeutically effective amount of N-eicosapentaenoyl-cysteamine-S-phosphate and one of N-(all-trans-retinoyl)-O-phospho-L-tyrosine or N-(13-cis-retinoyl)-O-phospho-L-tyrosine.
A pharmaceutical preparation, characterized in that it comprises a therapeutically effective amount of N-arachidonoyl-cysteamine-S-phosphate and one of N-(all-trans-retinoyl)-O-phospho-L-tyrosine or N-(13-cis-retinoyl)-O-phospho-L-tyrosine.
A pharmaceutical preparation, characterized in that it comprises a therapeutically effective amount of N-α-linolenoyl-cysteamine-S-phosphate and one of N-(all-trans-retinoyl)-O-phospho-L-tyrosine or N-(13-cis-retinoyl)-O-phospho-L-tyrosine.
A pharmaceutical preparation, characterized in that it comprises a therapeutically effective amount of N-γ-linolenoyl-cysteamine-S-phosphate and one of N-(all-trans-retinoyl)-O-phospho-L-tyrosine or N-(13-cis-retinoyl)-O-phospho-L-tyrosine.
Use of a compound for the manufacture of a pharmaceutical preparation, said compound being selected from the group consisting of N-docosahexaenoyl-O-phospho-2-aminoethanol, N-eicosapentaenoyl O-phospho-2-aminoethanol, N-arachidonoyl O-phospho-2-aminoethanol, N-α-linolenoyl O-phospho-2-aminoethanol, and N-γ-linolenoyl O-phospho-2-aminoethanol.
Use of a compound for the manufacture of a pharmaceutical preparation for the treatment of cancer, said compound being selected from the group consisting of N-docosahexaenoyl-O-phospho-2-aminoethanol, N- eicosapentaenoyl O-phospho-2-aminoethanol, N-arachidonoyl O-phospho-2-aminoethanol, N-α-linolenoyl O-phospho-2-aminoethanol, and N-γ-linolenoyl O-phospho-2-aminoethanol.
A method for treating a patient suffering from cancer, said method comprising the step of administering to the patient an effective amount of a compound selected from the group consisting of N-docosahexaenoyl-cysteamine-S-phosphate, N-eicosapentaenoyl-cysteamine-S-phosphate, N-arachidonoyl-cysteamine-S-phosphate, N-α-linolenoyl-cysteamine-S-phosphate, and N-γ-linolenoyl-cysteamine-S-phosphate.
A method for treating a patient suffering from cancer, said method comprising the step of administering to the patient an effective amount of a compound selected from the group consisting of N-docosahexaenoyl-cysteamine-S-phosphate, N-eicosapentaenoyl-cysteamine-S-phosphate, N-arachidonoyl-cysteamine-S-phosphate, N-α-linolenoyl-cysteamine-S-phosphate, and N-γ-linolenoyl-cysteamine-S-phosphate in admixture or simultaneously with N-(all-trans-retinoyl)-O-phospho-L-tyrosine.
A method for treating a patient suffering from cancer, said method comprising the step of administering to the patient an effective amount of a compound selected from the group consisting of N-docosahexaenoyl-cysteamine-S-phosphate, N-eicosapentaenoyl-cysteamine-S-phosphate, N-arachidonoyl-cysteamine-S-phosphate, N-α-linolenoyl-cysteamine-S-phosphate, and N-γ-linolenoyl-cysteamine-S-phosphate in admixture or simultaneously with N-(13-cis-retinoyl)-O-phospho-L-tyrosine.
Dependencies are inferred from the claim text.