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    • 1. 发明申请
    • PACLITAXEL ENHANCER COMPOUNDS
    • PACLITAXEL增强化合物
    • US20150344420A1
    • 2015-12-03
    • US14826889
    • 2015-08-14
    • Synta Pharmaceuticals Corp.
    • Keizo KoyaLijun SunShoujun ChenNoriaki TatsutaYaming WuMitsumori Ono
    • C07C327/56
    • A61K31/381A61K31/16A61K31/165A61K31/277A61K31/337A61K31/44A61K31/505A61K31/53A61K47/58C07C327/56C07C2601/02C07C2601/04C07C2601/08C07C2601/14C07D209/42C07D209/44C07D213/83C07D261/18C07D305/14C07D307/68C07D333/38C07D333/68C07D407/12
    • Disclosed is a compound represented by the Structural Formula (I): Y is a covalent bond, a phenylene group or 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 and R2 are independently an aryl group or a substituted aryl group, R3 and R4 are independently —H, an aliphatic group, a substituted aliphatic group, an aryl group or a substituted aryl group.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.Also disclosed is a method of treating a subject with cancer by administering to the subject a compound of Structural Formula (I) in combination with Paclitaxel or an analog of Paclitaxel.
    • 公开了由结构式(I)表示的化合物:Y是共价键,亚苯基或取代或未取代的直链烃基。 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) - 。 R 1和R 2独立地是芳基或取代的芳基,R 3和R 4独立地是-H,脂族基团,取代的脂族基团,芳基或取代的芳基。 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。 还公开了通过向受试者施用结合式(I)的化合物与紫杉醇或紫杉醇的类似物组合来治疗患有癌症的受试者的方法。