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US 8,703,907 B2Granted
Controlled drug release from dendrimers
AssigneeProLynx LLC
InventorsGary Ashley, Daniel V. Santi
Life of this patent
Estimating the term…
Abstract
The invention relates to compositions that comprise dendrimers useful in medical and veterinary applications that provide controlled release of drugs, such as peptides, nucleic acids and small molecules. The drugs are covalently coupled to the dendrimer through a linkage that releases the drug or a prodrug through controlled beta elimination.
Claims18
A dendrimer coupled to a multiplicity of substituents of the formula
- at least one or both R1 and R2 is independently CN;
- NO2;
- optionally substituted aryl;
- optionally substituted heteroaryl;
- optionally substituted alkenyl;
- optionally substituted alkynyl;
- COR3 or SOR3 or SO2R3 wherein
- R3 is H or optionally substituted alkyl;
- aryl or arylalkyl, each optionally substituted;
- heteroaryl or heteroarylalkyl, each optionally substituted;
- or
- OR or NR2 wherein each R is independently H or optionally substituted alkyl;
- SR4 wherein
- R4 is optionally substituted alkyl;
- aryl or arylalkyl, each optionally substituted;
- or
- heteroaryl or heteroarylalkyl, each optionally substituted;
- wherein R1 and R2 may be joined to form a 3-8 member ring;
- and
- wherein one and only one of R1 and R2 may be H or may be alkyl, arylalkyl or heteroarylalkyl, each optionally substituted;
- each R5 is independently H or is alkyl, alkenylalkyl, alkynylalkyl, aryl, arylalkyl, heteroaryl or heteroarylalkyl, each optionally substituted;
- D is a residue of a drug or prodrug coupled through O, S, or N;
- Y is absent and X is O or S;
- or
- Y is NBCH2 and X is O;
- wherein B is alkyl, aryl, arylalkyl, heteroaryl or heteroarylalkyl, each optionally substituted;
- and
- wherein said coupling to the dendrimer is through any of R1, R2, R5 or B.
25 more elements
A dendrimer coupled to a multiplicity of substituents of the formula
- at least one, or both R1 and R2 is independently CN;
- NO2;
- optionally substituted aryl;
- optionally substituted heteroaryl;
- optionally substituted alkenyl;
- optionally substituted alkynyl;
- COR3 or SOR3 or SO2R3 wherein
- R3 is H or optionally substituted alkyl;
- aryl or arylalkyl, each optionally substituted;
- heteroaryl or heteroarylalkyl, each optionally substituted;
- or
- OR or NR2 wherein each R is independently H or optionally substituted alkyl;
- SR4 wherein
- R4 is optionally substituted alkyl;
- aryl or arylalkyl, each optionally substituted;
- or
- heteroaryl or heteroarylalkyl, each optionally substituted;
- wherein R1 and R2 may be joined to form a 3-8 member ring;
- and
- wherein one and only one of R1 and R2 may be H or may be alkyl, arylalkyl or heteroarylalkyl, each optionally substituted;
- each R5 is independently H or is alkyl, alkenylalkyl, alkynylalkyl, aryl, arylalkyl, heteroaryl or heteroarylalkyl, each optionally substituted;
- Y is absent and X is O or S;
- or
- Y is NBCH2 and X is O;
- wherein B is alkyl, aryl, arylalkyl, heteroaryl or heteroarylalkyl, each optionally substituted;
- and
- L is a nucleofuge,
- wherein said coupling to the dendrimer is through any of R1, R2, R5 or B.
25 more elements
A compound of the formula
- M-(J-D)m
- wherein M is a dendrimer, D is a drug and J is a joining moiety that releases D by a beta elimination mechanism, wherein m is an integer of at least 8.
Dependencies are inferred from the claim text.