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    • 139. 发明申请
    • 1-Glyoxylamide indolizines for treating lung and ovarian cancer
    • 1-乙酰氧基吲哚啉用于治疗肺癌和卵巢癌
    • US20050272766A1
    • 2005-12-08
    • US11088253
    • 2005-03-23
    • Keizo KoyaLijun SunHao LiMitsunori Ono
    • Keizo KoyaLijun SunHao LiMitsunori Ono
    • A61K31/437A61K31/4745
    • 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. Z1 and Z2 are independently ═O, ═S, ═N—OR12 or ═NR12 R1 and R2 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 R1 and R2 are not both —H. Alternatively, —NR1R2, taken together, is a substituted or unsubstituted non-aromatic nitrogen-containing heterocyclic group or a substituted or unsubstituted nitrogen-containing heteroaryl group. R3 is a substituted or unsubstituted aryl group or a substituted or unsubstituted aliphatic group. X is a covalent bond, —C(R4R5)—, —N(R4)—, —O—, —S—, —S(O)—, —S(O)2—, —C(═O)—, —C(═O)—N(R4)—, or —N(R4)—C(═O)—. R4 and R5 are independently —H or a substituted or unsubstituted aliphatic group. R12 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独立地是-O,-S,-N-OR 12或-NR 12, R 1和R 2独立地是-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团, 芳基或取代的芳基,条件是R 1和R 2不同时为-H。 或者,-NR 1 R 2 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。 R 3是取代或未取代的芳基或取代或未取代的脂族基。 X是共价键,-C(R 4 R 5) - , - N(R 4) - , - O - , - ,-S(O) - , - S(O)2 - , - C( - ) - >) - 或-N(R 4) - C(-O) - 。 R 4和R 5独立地是-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。
    • 140. 发明授权
    • 1-glyoxylamide indolizines for treating cancer
    • 用于治疗癌症的1-乙醛酰胺中氮茚
    • US06861436B2
    • 2005-03-01
    • US10244088
    • 2002-09-13
    • Keizo KoyaLijun SunMitsunori OnoWeiwen YingHao Li
    • Keizo KoyaLijun SunMitsunori OnoWeiwen YingHao Li
    • A61K31/437A61K31/444A61K31/4709A61K31/496A61P35/00C07D471/04A61K31/44A61K31/47C07D215/38C07D215/46C07D221/02
    • C07D471/04
    • Disclosed is a compound represented by Structural Formula (I): Ring A is substituted or unsubstituted and optionally fused to an aryl group. Z1 and Z2 are independently ═O, ═S, ═N—OR12 or ═NR12 R1 and R2 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 R1 and R2 are not both —H. Alternatively, —NR1R2, taken together, is a substituted or unsubstituted non-aromatic nitrogen-containing heterocyclic group or a substituted or unsubstituted nitrogen-containing heteroaryl group. R3 is a substituted or unsubstituted aryl group or a substituted or unsubstituted aliphatic group. X is a covalent bond, —C(R4R5)—, —N(R4)—, —O—, —S—, —S(O)—, —S(O)2—, —C(═O)—, —C(═O)—N(R4)—, or —N(R4)—C(═O)—. R4 and R5 are independently —H or a substituted or unsubstituted aliphatic group. R12 is —H or a substituted or unsubstituted alkyl group.
    • 公开了由结构式(I)表示的化合物:环A是取代或未取代的且任选地与芳基稠合.Z1和Z2独立地为= O,= S,= N-OR12或= NR12R1,R2独立地为-H ,脂肪族基团,取代脂肪族基团,未取代的非芳香族杂环基团,取代的非芳香族杂环基团,芳基或取代的芳基,条件是R1和R2不同时为-H。 或者,-NR 1 R 2一起为取代或未取代的非芳香族含氮杂环基或取代或未取代的含氮杂芳基.R 3为取代或未取代的芳基或取代或未取代的脂族基.X为 共价键,-C(R4R5) - , - N(R4) - , - O - , - S - , - S(O) - , - S(O) C(= O)-N(R4) - 或-N(R4)-C(= O) - 。R4和R5独立地为-H或取代或未取代的脂族基.R12为-H或取代或未取代的 烷基。