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US 2002/0119956 A1Published application
Methods and compositions for inhibition of angiogenesis with phthaloyl glutamic acid derivatives
OwnerRobert D'Amatoinventor
Life of this patent
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Abstract
The present invention comprises a group of compounds that effectively inhibit angiogenesis. More specifically, thalidomide and various related compounds such as EM-12 and its derivatives have been shown to inhibit angiogenesis and to treat disease states resulting from angiogenesis. Importantly, these compounds can be administered orally.
Claims36
A compound comprising the following formula:
- 19
- Wherein R1, R2, R3, and R4 are independently selected from —H;
- —OH;
- ═O;
- straight chained and branched alkanes, alkenes, alkynes;
- cyclic alkanes, alkenes and alkynes;
- combinations of cyclic and acyclic alkanes, alkenes and alkynes;
- alcohol, aldehyde, ketone, carboxylic acid, ester, or ether moieties in combination with acyclic, cyclic, or combination acycli/cyclic moieties;
- aza;
- amino;
- —NO2, —ONO2, —SO2 or —O—SO3, PO3, OPO2, OPO3;
- and halogens;
- R9 is a moiety selected from one of the following formulas:
- 20
- where R11-R16 are each independently selected from:
- 21
- or —O— where Y is optional and is the same as defined above for R1;
- and R10 is the same as defined above for R1, or R10 is ═O.
15 more elements
A method of treating undesired angiogenesis in a human or animal comprising administering to the human or animal with undesired angiogenesis a composition comprising an effective amount of a compound comprising the following formula
- 26
- wherein R1, R2, R3, and R4 are independently selected from —H;
- —OH;
- ═O;
- straight chained and branched alkanes, alkenes, alkynes;
- cyclic alkanes, alkenes and alkynes;
- combinations of cyclic and acyclic alkanes, alkenes and alkynes;
- alcohol, aldehyde, ketone, carboxylic acid, ester, or ether moieties in combination with acyclic, cyclic, or combination acyclic/cyclic moieties;
- aza;
- amino;
- —NO2, —ONO2, —SO2 or —O—SO3, PO3, OPO2, OPO3;
- and halogens;
- R9 is a moiety selected from one of the following formulas:
- 27
- where R11-R16 are each independently selected from:
- 28
- or —O—where Y is optional and is the same as defined above for R1;
- and R10 is the same as defined above for R1, or R10 is ═O.
15 more elements
Dependencies are inferred from the claim text.