发明授权
US5817742A Polymer-conjugated malonic acid derivatives and their use as medicaments
and diagnostic agents
失效
聚合物共轭丙二酸衍生物及其作为药物和诊断剂的用途
- 专利标题: Polymer-conjugated malonic acid derivatives and their use as medicaments and diagnostic agents
- 专利标题(中): 聚合物共轭丙二酸衍生物及其作为药物和诊断剂的用途
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申请号: US718524申请日: 1996-09-11
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公开(公告)号: US5817742A公开(公告)日: 1998-10-06
- 发明人: Alexander Toepfer , Gerhard Kretzschmar , Eckart Bartnik , Wolfgang Schmidt , Brigitte Horsch
- 申请人: Alexander Toepfer , Gerhard Kretzschmar , Eckart Bartnik , Wolfgang Schmidt , Brigitte Horsch
- 申请人地址: DEX Frankfurt
- 专利权人: Hoechst Aktiengesellschaft
- 当前专利权人: Hoechst Aktiengesellschaft
- 当前专利权人地址: DEX Frankfurt
- 优先权: DEX4408248.7 19940311
- 主分类号: A61K31/785
- IPC分类号: A61K31/785 ; A61K31/70 ; A61K31/7028 ; A61P29/00 ; A61P31/04 ; A61P31/12 ; A61P35/00 ; A61P43/00 ; C07H3/04 ; C07H3/06 ; C07H15/04 ; C07H15/207 ; C07H17/04 ; C08G69/10 ; C08G69/48 ; C08G73/06 ; C08G73/10
摘要:
Polymer-based polyvalent malonic acid derivatives having anti-adhesive properties are described. The compounds comprise a polyamino acid linked to a group of formula (I). In formula (I), R.sup.1 and R.sup.2 together form a six-membered carbocylic or heterocyclic ring, containing at least one substituent selected from R.sup.4, R.sup.5, and R.sup.6. R.sup.3 is H, (CH.sub.2) .sub.m X or CH.sub.2 O(CH.sub.2).sup.m X.sup.1. The polyamino acid and the group of formula II are linked via R.sup.4, R.sup.5, or R.sup.6, or optionally via a spacer of formula --�Q.sup.1 --(CH.sub.2).sub.p --Q.sup.2 --!.sub.r. A and B independently are O, S, NH, HN--CO, OC--NH, O--CO, OC--O, NH--CO--O, --O--CO--NH, S--CO, SC--O, O--CS--S, S--CS--OS, NH--CS--S, S--CS--NH, or CH.sub.2. Z is a pyranose, furanose, open-chain polyalcohol or Y--X.sup.6. Y is --O--(CX.sup.2,X.sup.3).sub.n, -(CX.sup.2,X.sup.3).sub.n, --CH.sub.2 --(CX.sup.2,X.sup.3).sub.n or a saturated or unsaturated six-membered carbo- or heterocyclic group having at least one substituent R.sup.9, or a combination of the chain --O--(CX.sup.2,X.sup.3).sub.n, or -(CX.sup.2,X.sup.3).sub.n, and the carbocyclic or heterocyclic group, in which R.sup.4, R.sup.5, and R.sup.6 independently are H, OH, --O--(CH.sub.2) .sub.q X.sup.4, --CH.sub.2 O(CH.sub.2) .sub.q X.sup.5, or HNC(O)CH.sub.3, and X, X.sup.1, X.sup.2, and X.sup.3 independently are H, NH.sub.2, COOH, OH, CH.sub.2 OH, CH.sub.2 NH.sub.2, C.sub.1 -C.sub.20 -alkyl, or C.sub.6 -C.sub.10 -aryl, X.sup.4 and X.sup.5 independently are --NH-- or --O--, and X.sup.6 is OH or --C(R.sup.3) (COOH).sub.2. m, n, and q independently can be 1-20. In the linker, Q.sup.1 is CH.sub.2 or --CO--, Q.sup.2 is --NH-- or --CO--NH--, p is 1-6, and r is 0 or 1. Methods of preparing the compounds, and their use as medicaments or diagnostic agents also are disclosed. ##STR1##
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