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US 8,946,405 B2Granted
Controlled release from solid supports
AssigneeProLynx LLC
InventorsGary Ashley, Daniel V. Santi
Life of this patent
Estimating the term…
Abstract
The invention relates to solid supports useful in medical applications that provide controlled release of drugs, such as peptides, nucleic acids and small molecules. The drugs are covalently coupled to the solid support through a linkage that releases the drug or a prodrug through controlled beta elimination.
Claims16
A composition of the formula
- wherein m=0 or 1;
- 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 OR9 or N(R9)2 wherein each R9 is independently H or optionally substituted alkyl, or both R9 groups taken together with the nitrogen to which they are attached form a heterocyclic ring;
- or SR4 wherein R4 is optionally substituted alkyl;
- aryl or arylalkyl, each optionally substituted;
- or heteroaryl or heteroarylalkyl, each optionally substituted;
- wherein R1 and R2 are joined to form a 3-8 membered ring;
- and wherein one and only one of R1 and R2 is H or is 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 one of R1, R2, R5 or B is coupled to a solid support.
19 more elements
A composition of the formula
- wherein m=0 or 1;
- 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 OR9 or N(R9)2 wherein each R9 is independently H or optionally substituted alkyl, or both R9 groups taken together with the nitrogen to which they are attached form a heterocyclic ring;
- or SR4 wherein R4 is optionally substituted alkyl;
- aryl or arylalkyl, each optionally substituted;
- or heteroaryl or heteroarylalkyl, each optionally substituted;
- wherein R1 and R2 are joined to form a 3-8 membered ring;
- and wherein one and only one of R1 and R2 is H or is 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 is through any of R1, R2, R5 or B.
19 more elements
A drug-solid support conjugate, wherein the drug is connected to the solid support via a linker;
- the drug molecule is attached to the linker through O, S, or N of formula (1), (2), or (3);
- and the drug is released from the conjugate under physiological conditions through a beta-elimination reaction.
Dependencies are inferred from the claim text.