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    • 47. 发明申请
    • 1-GLYOXYLAMIDE INDOLIZINES FOR TREATING LUNG AND OVARIAN CANCER
    • 1-GLYOXYLAMIDE INDOLIZINES FOR TRANTING LUNG AND OVARIAN CANCER
    • WO2005099824A1
    • 2005-10-27
    • PCT/US2005/009519
    • 2005-03-22
    • SYNTHA PHARMACEUTICALS, CORP.LI, HaoKOYA, KeizoSUN, LijunONO, Mitsunori
    • LI, HaoKOYA, KeizoSUN, LijunONO, Mitsunori
    • A61P35/00
    • A61K31/437A61K31/4745
    • A method of treating a subject having lung cancer or ovarian cancer, comprising administering to the subject an effective amount of a compound represented by Structural Formula (I) or a pharmaceutically acceptable salt, solvate, or polymorph thereof: Ring A is substituted or unsubstituted and optionally fused to an aryl group. Z 1 and Z 2 are independently=O, =S, =N-OR 12 or =NR 12 , R 1 and R 2 are independently -H, an aliphatic group, a substituted aliphatic group, an unsubstituted non-aromatic heterocylic group, a substituted non-aromatic heterocylic group, an aryl group or a substituted aryl group, provided that R 1 and R 2 are not both -H. Alternatively, -NR 1 R 2 , taken together, is a substituted or unsubstituted non-aromatic nitrogen-containing heterocyclic group or a substituted or unsubstituted nitrogen-containing heteroaryl group. R 3 is a substituted or unsubstituted aryl group or a substituted or unsubstituted aliphatic group. X is a covalent bond, -C(R 4 R 5 )-, -N(R 4 )-, -O-, -S-, -S(O)-, -S(O) 2 -, -C(=O)-, -C(=O)-N(R 4 )-, or -N(R 4 )-C(=O)-. R 4 and R 5 are independently -H or a substituted or unsubstituted aliphatic group. R 12 is -H or a substituted or unsubstituted alkyl group.
    • 一种治疗患有肺癌或卵巢癌的受试者的方法,其包括向所述受试者施用有效量的由结构式(I)表示的化合物或其药学上可接受的盐,溶剂化物或多晶型物:环A是取代或未取代的, 任选地与芳基稠合。 Z 1和Z 2独立地为= O,= S,= N-OR 12或= NR 12,R 1和R 2独立地为-H,脂族基团,取代的脂族基团,未取代的非芳族杂环基团,取代的非芳族杂环基 基团,芳基或取代的芳基,条件是R1和R2不同时为-H。 或者,-NR 1 R 2一起是取代或未取代的非芳族含氮杂环基或取代或未取代的含氮杂芳基。 R3是取代或未取代的芳基或取代或未取代的脂族基团。 X是共价键,-C(R4R5) - , - N(R4) - , - O - , - S - , - S(O) - , - S(O) ,-C(= O)-N(R 4) - 或-N(R 4)-C(= O) - 。 R 4和R 5独立地为-H或取代或未取代的脂族基团。 R 12是-H或取代或未取代的烷基。