Synthesis of taxol enhancers
    73.
    发明授权
    Synthesis of taxol enhancers 失效
    紫杉醇增强剂的合成

    公开(公告)号:US06825235B2

    公开(公告)日:2004-11-30

    申请号:US10193076

    申请日:2002-07-10

    IPC分类号: A61K3116

    摘要: Disclosed is a method of preparing a thiohydrazide product compound from a hydrazide starting compound. The hydrazide starting compound is represented by Structural Formula (I): The thiohydrazide product compound is represented by Structural Formula (II): In Structural Formulas (I)-(II), R1 and R2 are independently an aliphatic group, a substituted aliphatic group, an aryl group or a substituted aryl group, or R1 and R2 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. When R2 is an aryl group or a substituted aryl group, then R5 is a hydrazine protecting group; and when R2 is an aliphatic or substituted aliphatic group, then R5 is —H or a hydrazine protecting group. R10 is —H or a substituted or unsubstituted alkyl group. The method comprising the step of reacting the starting compound with a thionylating reagent.

    摘要翻译: 公开了从酰肼起始化合物制备硫代酰肼产物化合物的方法。 酰肼起始化合物由结构式(I)表示:硫代酰肼产物化合物由结构式(II)表示:在结构式(I) - (II)中,R 1和R 2独立地为脂族基团,取代的脂族基团 ,芳基或取代的芳基,或者R 1和R 2与它们所键合的碳原子和氮原子一起形成任选地与芳环稠合的非芳族杂环。 当R 2为芳基或取代芳基时,R 5为肼保护基; 当R 2为脂肪族或取代的脂族基团时,R 5为-H或肼保护基。 R 10为-H或取代或未取代的烷基。 该方法包括使起始化合物与亚硫酰化试剂反应的步骤。

    1-Glyoxylamide indolizines for treating lung and ovarian cancer
    79.
    发明申请
    1-Glyoxylamide indolizines for treating lung and ovarian cancer 审中-公开
    1-乙酰氧基吲哚啉用于治疗肺癌和卵巢癌

    公开(公告)号:US20050272766A1

    公开(公告)日:2005-12-08

    申请号:US11088253

    申请日:2005-03-23

    IPC分类号: A61K31/437 A61K31/4745

    CPC分类号: A61K31/437 A61K31/4745

    摘要: 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.

    摘要翻译: 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。