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    • 9. 发明授权
    • Paclitaxel enhancer compound
    • 紫杉醇增强剂化合物
    • US07750042B2
    • 2010-07-06
    • US12077729
    • 2008-03-20
    • Keizo KoyaLijun SunShoujun ChenNoriaki TatsutaYaming WuMitsunori OnoZhi-Qiang Xia
    • Keizo KoyaLijun SunShoujun ChenNoriaki TatsutaYaming WuMitsunori OnoZhi-Qiang Xia
    • A61K31/335A61K31/20C07C327/38C07C243/18
    • C07D307/68A45D2008/006A61K31/337A61K31/505A61K31/53A61K31/5377A61K47/58C07C327/56C07C2601/02C07C2601/04C07C2601/08C07C2601/14C07D209/42C07D209/44C07D213/83C07D261/18C07D333/38C07D333/68
    • One embodiment of the present invention is a compound represented by the Structural Formula (I): Y is a covalent bond of a substituted or unsubstituted straight chained hydrocarbyl group. In addition, Y, taken together with both >C═Z groups to which it is bonded, is a substituted or unsubstituted aromatic group. Preferably, Y is a covalent bond or —C(R7R8)—. R1 is an aliphatic group, a substituted aliphatic group, a non-aromatic heterocyclic group, or a substituted non-aromatic heterocyclic group, R2-R4 are independently —H, an aliphatic group, a substituted aliphatic group, a non-aromatic heterocyclic group, a substituted non-aromatic heterocyclic group, an aryl group or a substituted aryl group, or R1 and R3 taken together with the carbon and nitrogen atoms to which they are bonded, and/or R2 and R4 taken together with the carbon and nitrogen atoms to which they are bonded, form a non-aromatic heterocyclic ring optionally fused to an aromatic ring. R5-R6 are independently —H, an aliphatic group, a substituted aliphatic group, an aryl group or a substituted aryl group. R7 and R8 are each independently —H, an aliphatic or substituted aliphatic group, or R7 is —H and R8 is a substituted or unsubstituted aryl group, or, R7 and R8, taken together, are a C2-C6 substituted or unsubstituted alkylene group. Z is ═O or ═S. Also disclosed are pharmaceutical compositions comprising the compound of the present invention and a pharmaceutically acceptable carrier or diluent.
    • 本发明的一个实施方案是由结构式(I)表示的化合物:Y是取代或未取代的直链烃基的共价键。 此外,Y与它所键合的两个> C = Z基团一起是取代或未取代的芳族基团。 优选Y为共价键或-C(R 7 R 8) - 。 R1是脂肪族基团,取代脂肪族基团,非芳族杂环基团或取代的非芳族杂环基团,R2-R4独立地是-H,脂肪族基团,取代的脂肪族基团,非芳香族杂环基 ,取代的非芳族杂环基,芳基或取代的芳基,或者R 1和R 3与它们所键合的碳原子和氮原子一起,和/或R 2和R 4与碳和氮原子一起 形成与芳环稠合的非芳族杂环。 R5-R6独立地是-H,脂族基团,取代的脂族基团,芳基或取代的芳基。 R 7和R 8各自独立地为-H,脂族或取代的脂族基团,或者R 7为-H且R 8为取代或未取代的芳基,或者R 7和R 8一起为C 2 -C 6取代或未取代的亚烷基 。 Z为═O或═S。 还公开了包含本发明化合物和药学上可接受的载体或稀释剂的药物组合物。