C - Chemistry – Metallurgy – 07 – J
Patent
C - Chemistry, Metallurgy
07
J
C07J 1/00 (2006.01) A61K 31/66 (2006.01) A61K 31/70 (2006.01) A61K 47/48 (2006.01) C07F 9/09 (2006.01) C07F 9/547 (2006.01) C07F 9/553 (2006.01) C07F 9/572 (2006.01) C07F 9/576 (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 19/04 (2006.01) C07H 19/10 (2006.01) C07H 19/20 (2006.01) C07J 5/00 (2006.01) C07J 7/00 (2006.01) C07J 51/00 (2006.01) C07J 63/00 (2006.01) C07J 71
Patent
CA 2108041
2108041 9217185 PCTABS00016 The invention provides compounds of formula (I) and the pharmaceutically acceptable salts 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 (a) moiety; R1 is C1-C8 alkyl, C6-C10 aryl or C7-C12 aralkyl, with the proviso that when [D] is the residue of a drug having a reactive hydroxyl functional group, said functional group being attached directly to the phosphorus atom of the (a) moiety via an oxygen-phosphorus bond, then R1, taken together with the adjacent oxygen atom, can also be the residue of a drug having a reactive hydroxyl functional group, said functional group being attached directly to the phosphorus atom of the (b) moiety via an oxygen-phosphorus bond, -OR1 being the same as or different from [D]; 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 targeted drug delivery, especially to the brain.
Swabey Ogilvy Renault
University Of Florida
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