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US 2002/0173489 A1Published application
Compositions containing a mixture of phosphorous compounds and alkylglycerols
OwnerHansjorg Eiblinventor
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Abstract
The object of the invention is to provide a medicament which is suitable for the treatment of tumors, such as via topical administration. Another object of the invention is to provide a medicament which, in general, can also be used in other forms of administration, such as in intravenous form, which combines good effectiveness against tumors, lower toxicity and which can, therefore, be generally used in tumor therapy.
Claims67
A compound of the formula
- R-Y-P⊖2-X-R1 (I′)
- wherein R is a saturated or unsaturated hydrocarbon radical of 12 to 24 carbon atoms which may also be halogen-substituted,
- X is oxygen, -NH or -NR2-,
- Y is oxygen or -NH-,
- R1 is C1-C8-alkyl, unsaturated C3-C8-alkyl, optionally unsaturated C3-C8-alkyl which is substituted with halogen, amino, C1-C6-alkylamino, di-C1-C6-alkylamino, tri-C1-C6-alkylamino, hydroxyl, carboxyl, C3-C8-cycloalkyl or phenyl, C2-alkyl which is substituted with hydrogen, hydroxyl, carboxyl, C3-C8-cycloalkyl or phenyl;
- unsaturated C2-alkyl which is substituted with di-C1-C6-alkylamino, tri-C1-C6-alkylamino, C3-C8-cycloalkyl orphenyl;
- C2-alkyl which is substituted with amino, C1-C6-alkylamino, di-C1-C6-alkylamino or tri-C1-C6-alkylamino when X is oxygen, -NH- or -NR2- and Y is -NH-, or when X is -NH- or -NR2-, Y is oxygen and R has the meanings previously defined;
- 2-tert. -butoxycarbonyl-aminoethyl, 2-tert.-butoxycarbonylethyl, 2,3-isopropylidenedioxy-propyl-(1), 2,3-dibenzyloxypropyl-(1), 1,3-disbenzyloxypropyl-(2) or N-C1-C6-alkylamino-C2-C6-alkyl when X is oxygen and Y and R have the meanings previously defined;
- 2,3-dihydroxypropyl-(1) when X is -NH- and Y and R have the meanings previously defined;
- and
- R2 is 2,3-dihydroxypropyl-(1), C1-C8-alkyl or C2-C8-alkyl which is unsaturated and/or substituted with halogen, amino, C1-C6-alkylamino, di-C1-C6-alkylamino, tri-C1-C6-alkylamino, hydroxyl, carboxyl, C3-C8-cycloalkyl or phenyl;
- and physiologically acceptable salts thereof.
9 more elements
Composition comprising
- a) a compound of the formula
- R-Y-PO⊖2-X-R1
- wherein R is a saturated or unsaturated hydrocarbon radical of 12 to 24 carbon atoms, which may also be halogen-substituted;
- X is oxygen, -NH- or -NR2-;
- Y is oxygen or -NH-;
- R1 is C1-C8-alkyl, C2-C8-alkyl which is unsaturated or optionally substituted with halogen, amino, C1-C6-alkylamino, di-C1-C6-alkylamino, tri-C1-C6-alkylamino, hydroxyl, carboxyl, C3-C8-cycloalkyl, phenyl, 2-tert.-butoxycarbonylaminoethyl, 2-tert.-butoxycarbonylethyl, 2,3-iso-propylidenedioxypropyl-(1), 2,3-dibenzyloxypropyl-(1), 1,3-dibenzyloxypropyl-(2), N-C1-C6-alkylamino-C2-C6-alkyl when X is oxygen, or 2,3-dihydroxypropyl-(1) when X is -NH-, and
- R2 is 2,3-dihydroxypropyl-(1), C1-C8-alkyl or C2-C8-alkyl which is unsaturated or optionally substituted with halogen, amino, C1-C6-alkylamino, di-C1-C6-alkylamino, tri-C1-C6-alkylamino, hydroxyl, carboxyl, C3-C8-cycloalkyl or phenyl, provided, however, that hexadecylphosphocholine is excepted, or a physiologically acceptable salt thereof;
- and
- b) an alkylglycerol of the formula
- 6
- wherein one of R3 and R4 is alkyl of 2 to 9 carbon atoms and the other is hydrogen.
8 more elements
Dependencies are inferred from the claim text.