Targeted drug delivery via phosphonate derivatives

Details Targeted drug delivery via phosphonate derivatives Targeted drug delivery via phosphonate derivatives

C - Chemistry, Metallurgy

07

F

C07F 9/547 (2006.01) A61K 31/66 (2006.01) A61K 31/70 (2006.01) A61K 47/48 (2006.01) C07F 9/40 (2006.01) C07F 9/553 (2006.01) C07F 9/572 (2006.01) C07F 9/576 (2006.01) C07F 9/58 (2006.01) C07F 9/59 (2006.01) C07F 9/645 (2006.01) C07F 9/6506 (2006.01) C07F 9/6509 (2006.01) C07F 9/6512 (2006.01) C07F 9/6547 (2006.01) C07F 9/6558 (2006.01) C07F 9/6561 (2006.01) C07H 15/252 (2006.01) C07H 19/00 (2006.01) C07H 19/048 (2006.01) C07H 19/052 (2006.01) C07H 19/056 (2006.01) C07H 19/10 (2006.01) C07H 19/12 (2006.01) C

Patent

CA 2087194

2087194 9200988 PCTABS00010 The invention provides compounds of formula (I) 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 moiety (I'); 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)-CrH2r- 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-CrH2r- 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 targered drug delivery, especially to the brain.

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