Pharmaceutical composition having enhanced antitumor activity and/or reduced side effects, containing an antitumor agent and an hydroximic acid derivative
AssigneeN-Gene Research Laboratories, Inc.
InventorBalázs Sumegi
Life of this patent
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Abstract
Pharmaceutical compositions having enhanced antitumor activity or reduced side effects. The compositions include both (A) a known active substance having antitumor effect or a pharmaceutically suitable salt thereof and (B) an effective amount of a hydroximic acid derivative of formula (I) or a therapeutically useful acid addition salt thereof. Also disclosed are methods for reducing side effects in patients requiring treatment for tumors.
Claims10
A pharmaceutical composition having antitumor activity with reduced side effect(s) comprising an enhanced effective amount of a known active substance having antitumor effect selected from the group consisting of cisplatin and carboplatin or, optionally, a pharmaceutically suitable acid addition salt thereof and an effective amount of a hydroximic acid derivative of the formula I
- wherein,
- R1 represents a hydrogen atom or a C1-5 alkyl group,
- R2 stands for a hydrogen atom, a C1-5 alkyl group, a C3-8 cycloalkyl group or a phenyl group optionally substituted by a hydroxy or a phenyl group, or
- R1 and R2 together with the nitrogen atom they are attached to form a 5 to 8 membered ring optionally containing one or more further nitrogen, oxygen or sulfur atom(s) and said ring can be condensed with another alicyclic or heterocyclic ring, preferably a benzene, naphthalene, quinoline, isoquinoline, pyridine or pyrazoline ring, furthermore, optionally, the nitrogen and/or sulfur heteroatom(s) are present in the form of an oxide or dioxide,
- R3 means a hydrogen atom, a phenyl group, a naphthyl group or a pyridyl group wherein said groups can be substituted by one or more halo atom(s) or C1-4 alkoxy group(s),
- Y is a hydrogen atom, a hydroxy group, a C1-24 alkoxy group optionally substituted by an amino group, a C2-24 polyalkenyloxy group containing 1 to 6 double bond(s), a C1-25 alkanoyl group, a C3-9 alkenoyl group or a group of the formula R7—COO— wherein R7 represents a C2-30 polyalkenyl group containing 1 to 6 double bond(s),
- X stands for a halo atom, an amino group, a C1-4 alkoxy group, or
- X forms with B an oxygen atom, or
- X and Y together with the carbon atoms they are attached to and the —NR—O—CH2— group being between said carbon atoms form a ring of the formula a
- wherein
- Z represents an oxygen atom or a nitrogen atom,
- R stands for a hydrogen atom or
- R forms with B a chemical bond,
- A is a C1-4 alkylene group or a chemical bond or a group of the formula b,
- wherein
- R4 represents a hydrogen atom, a C1-5 alkyl group, a C3-8 cycloalkyl group or a phenyl group optionally substituted by a halo atom, a C1-4 alkoxy group or a C1-5 alkyl group,
- R5 stands for a hydrogen atom, a C1-4 alkyl group or a phenyl group,
- m has a value of 0, 1 or 2,
- n has a value of 0, 1 or 2,
- or a physiologically acceptable acid addition salt thereof in admixture with one or more conventional carrier(s),
- wherein the antitumor activity is against tumors sensitive to the combination.
A pharmaceutical composition having antitumor activity with reduced side effect(s) comprising an enhanced effective amount of cisplatin and O-(3-piperidino-2-hydroxy-1-propyl)-nicotinic amidoxime, wherein said antitumor activity is against tumors sensitive to said composition.
A pharmaceutical composition having antitumor activity with reduced side effect(s) comprising an enhanced effective amount of carboplatin or a pharmaceutically acceptable acid addition salt thereof, and O-(3-piperidino-2-hydroxy-1-propyl)-nicotinic amidoxime, or a pharmaceutically acceptable acid addition salt thereof, wherein said antitumor activity is against tumors sensitive to said composition.
Dependencies are inferred from the claim text.