63379-66-8Relevant academic research and scientific papers
Targeted drug delivery via phosphonate derivatives
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, (2008/06/13)
The invention provides compounds of the formula STR1 or a pharmaceutically acceptable salt thereof, wherein [D] is the residue of a drug having a reactive functional group, said functional group being attached, directly or through a bridging group, via an oxygen-phosphorus bond to the phosphorus atom of the STR2 moiety; R1 is C1 -C8 alkyl, C6 -C10 aryl or C7 -C12 aralkyl; R2 is hydrogen, C1 -C8 alkyl, C6 -C10 aryl, C4 -C9 heteroaryl, C3 -C7 cycloalkyl, C3 -C7 cycloheteroalkyl or C7 -C12 aralkyl; and R3 is selected from the group consisting of C1 -C8 alkyl; C2 -C8 alkenyl having one or two double bonds; (C3 -C7 cycloalkyl)--Cr H2r --wherein r is zero, one, two or three, the cycloalkyl portion being unsubstituted or bearing 1 or 2 C1 -C4 alkyl substituents on the ring portion; (C6 -C10 aryloxy)C1 -C8 alkyl; 2--, 3-- or 4-- pyridyl; and phenyl-Cr H2r -- wherein r is zero, one, two or three and phenyl is unsubstituted, or is substituted by 1 to 3 alkyl each having 1 to 4 carbon atoms, alkoxy having 1 to 4 carbon atoms, halo, trifluoromethyl, dialkylamino having 2 to 8 carbon atoms or alkanoylamino having 2 to 6 carbon atoms. The compounds are adapted for targeted drug delivery, especially to the brain.
