发明名称 WATER SOLUABLE PRODRUGS OF ANTI-TUMOR ACTION
摘要 1. A composition comprising an anti-tumor drug conjugated to a water soluble polymer or metal chelator and wherein said a water soluble polymer or metal chelator is selected from the group consisting of poly (d-glutamic acid), poly (l-glutamic acid), poly (dlglutamic acid), poly (d-aspartic acid), poly (l-aspartic acid), poly (dl-aspartic acid)and copolymers thereof, where the anti-tumor drug is paclitaxel, docetaxel, etopside, teniposide camptothecin or epothilone. 2. The composition of claim 1 wherein the anti-tumor drug is selected from paclitaxel, docetaxe and camptothecin. 3. The composition of claim 2, wherein said polymer is further defined as a copolymer with polycaprolactone, polyglycolic acid and polylactic acid. 4. The composition of any preceding claim, wherein said polymer/copolymer has a molecular weight of from about 5,000 to about 100,000, preferably from about 20,000 to about 80,000. 5. The composition of any preceding claim, wherein said water soluble polymer is conjugated to the 2'-and/or the 7-hydroxyl of paclitaxel or docetaxel. 6. The composition of any preceding claim, comprising from 2 to 35% by weight of said anti-tumor drug. 7. The composition of claim 1, wherein paclitaxel is conjugated with polyglutamic acid. 8. Use of said composition of any preceding claim of treating cancer for decreasing at least one symptom of a systemic autoimmune disease and for inhibiting arterial restenosis or arterial occlusion following vascular trauma. 9. Use of claim 8, wherein said cancer is breast cancer, ovarian cancer, malignant melanoma, lung cancer, gastric cancer, colon cancer, head and neck cancer or leukemia or or Kaposi's sarcoma. 10. An implantable medical device, in particular stent, wherein said device is coated with a composition comprising paclitaxel conjugated to water soluable polyamino acids in an amount effective to inhibit smooth muscle cell proliferation.
申请公布号 EA002400(B1) 申请公布日期 2002.04.25
申请号 EA19980000817 申请日期 1997.03.11
申请人 PG-TXL COMPANY, L.P. 发明人 LI, CHUN;WALLACE, SIDNEY;YU, DONG-FANG;YOUNG, DAVID, G.
分类号 A61K31/335;A61K31/337;A61K31/47;A61K31/4738;A61K31/4745;A61K31/70;A61K31/7042;A61K31/7048;A61K47/48;A61K51/00;A61K51/04;A61L31/10;A61L31/16;A61P9/00;A61P35/00;A61P37/02;A61P43/00 主分类号 A61K31/335
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