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US 2016/0243106 A1Published application
Slow-release conjugates of sn-38
AssigneeProLynx LLC
InventorsGary W. ASHLEY, Eric L. SCHNEIDER
Life of this patent
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Abstract
Conjugates of SN-38 that provide optimal drug release rates and minimize the formation of the corresponding glucuronate are described. The conjugates release SN-38 from a polyethylene glycol through a β-elimination mechanism.
Claims20
A conjugate of formula (I)
- wherein
- PEG is linear or branched and, when q is 2-8, multi-armed, polyethylene glycol;
- X is O, NH, (CH2)m, OC(═O)(CH2)m, or NHC(═O)(CH2)m wherein m=1-6;
- L is (CH2)r or (CH2CH2O)p(CH2)r, wherein r=1-10 and p=1-10;
- R1 is CN or SO2NR22, wherein each R2 is independently alkyl, aryl, heteroaryl, alkylalkenyl, alkylaryl, or alkylheteroaryl, each optionally substituted, or two R2 taken together can form a ring;
- Y is COR3 or SO2R3, wherein R3═OH, alkoxy, or NR42, wherein each R4 is independently alkyl, substituted alkyl, or two R4 taken together can form a ring;
- and
- q is 1-8.
5 more elements
A pharmaceutical formulation comprising SN-38 in a mixture of DMSO and polyethylene glycol.
Dependencies are inferred from the claim text.