发明授权
- 专利标题: Targeted drug delivery via phosphonate derivatives
- 专利标题(中): 目标药物通过磷酸盐衍生物递送
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申请号: US553548申请日: 1990-07-13
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公开(公告)号: US5177064A公开(公告)日: 1993-01-05
- 发明人: Nicholas S. Bodor
- 申请人: Nicholas S. Bodor
- 申请人地址: FL Gainesville
- 专利权人: University of Florida
- 当前专利权人: University of Florida
- 当前专利权人地址: FL Gainesville
- 主分类号: A61K31/56
- IPC分类号: A61K31/56 ; A61K31/66 ; A61K31/675 ; A61K31/70 ; A61K31/7042 ; A61K31/7052 ; A61K31/7064 ; A61K31/7068 ; A61K31/7072 ; A61K31/7076 ; A61K31/708 ; A61K45/00 ; A61K47/48 ; A61P29/00 ; A61P31/12 ; A61P43/00 ; C07F9/40 ; C07F9/553 ; C07F9/572 ; C07F9/576 ; C07F9/58 ; C07F9/59 ; C07F9/645 ; C07F9/6506 ; C07F9/6509 ; C07F9/6512 ; C07F9/6547 ; C07F9/6558 ; C07F9/6561 ; C07H15/252 ; C07H19/04 ; C07H19/048 ; C07H19/052 ; C07H19/056 ; C07H19/10 ; C07H19/12 ; C07H19/20 ; C07H19/207 ; C07H19/23 ; C07H19/24 ; C07J51/00
摘要:
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; R.sub.1 is C.sub.1 -C.sub.8 alkyl, C.sub.6 -C.sub.10 aryl or C.sub.7 -C.sub.12 aralkyl; R.sub.2 is hydrogen, C.sub.1 -C.sub.8 alkyl, C.sub.6 -C.sub.10 aryl, C.sub.4 -C.sub.9 heteroaryl, C.sub.3 -C.sub.7 cycloalkyl, C.sub.3 -C.sub.7 cycloheteroalkyl or C.sub.7 -C.sub.12 aralkyl; and R.sub.3 is selected from the group consisting of C.sub.1 -C.sub.8 alkyl; C.sub.2 -C.sub.8 alkenyl having one or two double bonds; (C.sub.3 -C.sub.7 cycloalkyl)--C.sub.r H.sub.2r --wherein r is zero, one, two or three, the cycloalkyl portion being unsubstituted or bearing 1 or 2 C.sub.1 -C.sub.4 alkyl substituents on the ring portion; (C.sub.6 -C.sub.10 aryloxy)C.sub.1 -C.sub.8 alkyl; 2--, 3-- or 4-- pyridyl; and phenyl-C.sub.r H.sub.2r -- 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.
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